Medicinal & Aromatic Plants Abstracts
Vol. 31, No. 5, October 2009

Pharmacology & Toxicology


2009-05-2329 Abbas, S.; Wink, M. (Institute of Pharmacy and Molecular Biotechnology, Department of Biology, University of Heidelbergim Neuenheimer Field 364 96120 Heidelberg, Germany) Epigallocatechin gallate from green tea (Camellia sinensis) increases lifespan and stress resistance in Caenorhabditis elegans. Planta Medica v. 75(3): p. 216-221, 2009 (Eng; 30 ref).

Epigallocatechin gallate (EGCG) is a major green tea (Camellia sinensis Theaceae) leaves. Their effects on lifespan and stress resistance in wild-type N2 and transgenic strains of C. elegans hsp-16.2/GFP, mev-l(knl gest that the increased mean lifespan and stress resistance in C. elegans apparently depend, among other factors, on the antioxidant properties of EGCG.


2009-05-2330 Abdel-Kader, M.S.; Alqasoumi, S.I.; Al-Taweel, A.M. (Department of Pharmacognosy, College of Pharmacy, King Saud University; P.O. Box 2457, Riyadh 11451, Kingdom of Saudi Arabia) Hepatoprotective constituents from Cleome droserifolia. Chemical & Pharmaceutical Bulletin v 57(6): p. 620-624, 2009 ( Eng; 23 ref).

The effect of ethanol extract from aerial parts of Cleome droserifolia (Cleomaceae) was evaluated through the quantification of biochemical parameters and confirmed using histopathology analysis. Efficient hepatoprotective effect was achieved by crude extract, fractions and some pure compounds. The phytochemical studies showed that the petroleum ether fraction afforded two known guaiane sesquiterpenes, buchariol and teucladiol in addition to daucosterol (beta-sitosterol glucoside). The CHCl3 fraction afforded three known flavonoid derivatives, 5,3'-dihydroxy-3,6,7,4',5'-pentamethoxyflavone, 5'-hydroxy-3,6,7,3',4',5'-hexamethoxyflavone and luteolin and a known dolabellane diterpene. The active parts of the MeOH fraction afforded the previously unreported 3'-methoxy-3,5,4'-trihydroxy flavone-7-neohesperidoside and a known megastigmane norterpene: (6S,9R)-roseoside.


2009-05-2331 Abe, M.; Ito, Y.; Oyunzul, L.; Oki-Fujino, T.; Yamada, S*. (Department of Pharmacokinetics and Pharmacodynamics and Global Center of Excellence (COE) Program, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan) Pharmacologically relevant receptor binding characteristics and 5 alpha-reductase inhibitory activity of free fatty acids contained in Saw palmetto extract. Biological & Pharmaceutical Bulletin v. 32(4): p. 646-650, 2009 (Eng; 28 ref).

Saw palmetto Serenoa repens (Palmae) extract (SPE), used widely for the treatment of benign prostatic hyperplasia (BPH) has been shown to bind alpha 1- adrenergic, muscarinic and 1,4-dihydropyridine (1,4-DHP) calcium channel antagonist receptors. Major constituents of SPE are lauric acid, oleic acid, myristic acid, palmitic acid and linoleic acid. Study was conducted to investigate binding offinities of these fatty acids for pharmacologically relevant (alpha 1-adrenergic, muscarinic and 1,4,-DHP) receptors. On the basis of result obtained it is suggested that lauric acid and oleic acid bind noncompetitively to alpha 1-adrenergic, muscarinic and 1,4-DHP calcium channel antagonist receptors. A novel method of determining 5 alpha-reductase activity was developed using LC/MS. With this method, SPE was shown to inhibit 5 alpha-reductase activity in rat liver with an IC 50 of 101 microg/ml. Similarly, all the fatty acids except palmitic acid inhibited 5 alpha-reductase activity, with IC50 values of 42.1 to 67.6 microg/ml. In conclusion, lauric acid, oleic acid, myristic acid, and linoleic acid, major constituents of SPE, exerted binding activities of alpha 1-adrenergic, muscarinic and 1,4-DHP receptors and inhibited 5 alpha-reductase activity.


2009-05-2332 Ahamed, B.M.K.; Krishna, V.; Malleshappa, K.H. ( Department of Biochemistry, Basaveshwara Medical College, Hospital and Research Centre, Rajiv Gandhi University, Chitradurga, Karnataka, India) In vivo wound healing activity of the methanolic extract and its isolated constituent, gulonic acid y-lactone, obtained from Grewia tiliaefolia. Planta Medica v. 75(5): p. 478-482, 2009 (Eng; 26 ref).

Bioassay-directed fractionation and chromatography of the methanolic extract of Grewia tiliaefolia (Tiliaceae) stem bark has resulted in the isolation of gulonic acid gamma-lactone. The methanolic extract and the isolated constituent were studied for their potency on three different cutaneous wound models, viz., excision, incision and dead space wounds in Wistar rats. In the excision wound model, healing was assessed by the rate of wound contraction and period of epithelisation. In the incision wound model, the degree of healing was analysed by determining the skin breaking strength. In the dead space wound model, the parameters used to confirm the healing process were weight of granulation tissue, its tensile strength, hydroxyproline content and histological studies. The extract as well as the constituent demonstrated wound healing activity. Topical application of gulonic acid gamma-lactone (0.2 percent w/w ointment) caused faster epithelialisation with 94.02 percent wound contraction on day 16 post-wounding, while in control animals the duration of healing was extended up to 22 days with 79.53 percent wound contraction.


2009-05-2333 Ahmad, N.S.; Farman, M.; Najmi, M.H.; Mian, K.B.; Hasan, A. (College of Medical Sciences, National University of Sciences and Technology, Rawalpindi 46000, Pakistan) Pharmacological basis for use of Pistacia integerrima leaves in hyperuricemia and gout . Journal of Ethnopharmacology v. 117(3): p. 478-482, 2008 (Eng ; 38 ref).

Pistacia integerrima is an important component of commonly dispensed traditional dosage forms. We wished to determine whether polyphenolic constituents of this plant could be useful in oxidative stress and have potential to counter hyperuricemia. Radical scavenging activity was determined by 1,1-diphenyl-2-picrylhydrazyl (DPPH) and xanthine oxidase (XO) inhibitory activity assay in vitro. Fructose (FRS) induced hyperuricemic animal model was used to asses the serum uric acid (UA) lowering effect by plant products. Ethyl acetate and n-BuOH fractions had the highest DPPH radical scavenging activity. Fifty percent inhibitory concentration (IC50) was 6 and 7.6 microg/ml respectively. It was less than quercetin (IC50 0.95 microg/ml) and ascorbic acid (IC50 1.76 microg/ml). Xanthine oxidase inhibitory activity was comparable between n-BuOH and EtOAc (IC50 19 and 20 microg/ml) extracts but less than quercetin (IC50 0.65 microg/ml) and allopurinol (IC50 0.10 microg/ml). The antioxidant activity as well as the inhibitory activity towards the enzyme XO by quercetin-3-0-beta-D-glucopyranoside (5), kaempferol-3-O- beta-D-glucopyranoside (6), quercetin-3-O-(6"-O-syringyl)-beta-D-glucopyranoside (7), kaempferol-3-0- (4"-0-galloyl)-alpha-L-arabinopyranoside (8), rutin (4) together with aglycons, quercetin (1), kaempferol (2) and apigenin (3) was promising to continue in vivo hypouricemic studies. Ethyl acetate extract had dose dependent UA lowering effect in hyperuricemic mice. This effect was comparable with quercetin but less than allopurinol.


2009-05-2334 Ahmed, F.; Reza, M.S.H.; Shahid, I.Z.; Khatun, A.; Islam, K.K.; Ali, M.R. (Pharmacy Discipline, Khulna University, Khulna-9208, Bangladesh) Antibacterial and antinociceptive activity of Hoya parasitica. Hamdard Medicus v. 51(3): p. 22-26, 2008 (Eng; 11 ref).

The ethanol extract of leaves of Hoya parasitica syn H. acuta (Apocynaceae) was tested for its antinociceptive activities. The extract showed moderate antibacterial activity against both gram-positive and gram-negative bacteria. It also produced significant (P less than 0.01) writhing inhibition in Swiss albino mice at oral dose of 500 mg/kg body weight comparable to the standard drug diclofenac sodium.


2009-05-2335 Ambujakshi, H.R.; Khanam, S. (Acharya and B.M. Reddy College of Pharmacy, Bangalore-560090) Hypoglycemic activity from the leaves of Lagerstroemia speciosa (L) Pers. Biomed v. 2(1): p. 50-53, 2007 (Eng; 8 ref).

The study was undertaken to evaluate the antidiabetic potential of Lagerstroemia speciosa (Lythraceae) in alloxan (120 mg/kg) induced diabetic rats. The toluene and methanolic extracts of leaves of Lagerstroemia speciosa at dose of 500 mg/kg p.o. for 21 days resulted in significant reduction in serum glucose and cholesterol. It is found that the toluene and methanolic extracts of leaves of Lagerstroemia speciosa possess antidiabetic activity in diabetic induced rats. Glibenclamide was used as standard reference drug.


2009-05-2336 Ansari, M.N.; Bhandari, U. (Department of Pharmacology, Faculty of Pharmacy, Jamia Hamdard, New Delhi-110062, India) Cardioprotective activity of Zingiber officinale Roscoe in rats. Hamdard Medicus v. 51(3): p. 38-41, 2008 (Eng; 16 ref).

In the present study ethanolic extract of Zingiber officinale (Zingiberaceae) was prepared and studied for antioxidant and cardioprotective effect against isoproterenol (ISO) induced myocardial necrosis in rats. Results indicated that the ethanolic extract (200 mg/kg body wt, po) for 20 days post treatment improved biochemical parameters induced by ISO. In conclusion ethanolic extract augment endogenous myocardical antioxidants and protect rats against mycardial necrosis and associated oxidative stress.


2009-05-2337 Arafat, O.M.; Tham, S.Y.; Sadikun, A.; Zhari, I.; Haughton, P.J.; Asmawi, M.Z. (School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800 Penang, Malaysia) Studies on diuretic and hypouricemic effects of Orthosiphon stamineus methanol extracts in rats . Journal of Ethnopharmacology v. 118(3): p. 354-360, 2008 (Eng ; 42 ref).

The diuretic effect of different methanol extracts was examined by treating different groups of Sprague-Dawley rats with single (2 g/kg) oral doses of methanol and methanol: water (1:1) extracts. Hydrochlorothiazide (10 mg/kg) was used as positive control in acute study. Methanol and methanol water (1:1) extracts at 0.5 g/kg were administered for a period of 7 consecutive days. Cumulative urine volume and electrolytes (Na+ and K+) concentrations at different time intervals were measured. On the other hand, hypouricemic activity of methanol:water extract (1:1) was experimented using different oral single doses (0.25, 0.5, 1 and 2 g/kg). Allopurinol was used as positive control. Uric acid concentration in serum was analyzed by using RP-HPLC at 280 nm. Sodium and potassium excretion increased significantly (p less than 0.05 and less than 0.01) in the first 8 h of treatment with a single dose (2g/kg) of the extracts in a pattern comparable to that of the known diuretic hydrochlorothiazide. Meanwhile, repeated administration of 0.5 g/kg methanol:water (1:1) extract showed a significant increase in urine volume (from day 3 to day 7) (p less than 0.01) and electrolytes excretion (Na+ and K+) from day 2 to day 7 (p less than 0.05 and 0.01). On the other hand, 0.5,1 and 2 g/kg of methanol: water (1:1) extract and the standard allopurinol reduced the serum urate level in hyperuricemic rats at hour 6. These results provided an evidence of the high tendency of methanol: water (1:1) extract of Orthosiphon stamineus towards diuretic and hypouricemic effects in rats.


2009-05-2338 Arun, M.; Asha, V.V. (Molecular Ethnopharmacology Lab, Rajiv Gandhi Centre for Biotechnology, Thiruvananthapuram, Kerala 695014, India) Gastroprotective effect of Dodonaea viscosa on various experimental ulcer models . Journal of Ethnopharmacology v. 118(3): p. 460-465, 2008 (Eng ; 41 ref).

Dodonaea viscosa (Sapindaceae) is used as a medicinal herb by the tribes of Shola forest regions of Western Ghats. Studies were performed in two different models (ethanol and indomethacin induced gastric ulcer) in wistar rats. Gastric protection was evaluated by measuring the ulcer index, gastric glutathione assay, alkaline phosphate assay and histopathological studies. Gastric secretion studies were done by pyloric ligation experiment. Water and ethanol extract (500 mg/kg body weight) showed moderate activity compared to hexane extract. Hexane extract of Dodonaea viscosa dose dependently inhibited ethanol induced gastric lesions, causing 90 percent protection at 500 mg/kg, 81 percent protection at 250 mg/kg, and 70 percent protection at 125 mg/kg and it also dose dependently inhibited indomethacin induced gastric lesions, causing 92 percent protection at 500 mg/kg, 77 percent protection at 250 mg/kg, and 52 percent protection at 125 mg/kg. The various -degrees of inhibition were statistically significant (p less than 0.05). Further in gastric secretion studies, it found that hexane extract of Dodonaea viscosa (500 mg/kg) decreased the amount of total acid in gastric juice. Dodonaea viscosa hexane extract thus inhibits acid secretion to prevent ulcer aggravation. Acute toxicity study with a higher dose of 1250 mg/kg did not manifest any toxicological signs in rats. Preliminary phytochemical screening of the crude extract gave positive results for the presence of flavanoids, saponins, bitter principles and phenols.


2009-05-2339 Aslam, M.; Siddiqi, N.U.; Naqvi, S.W.I.* ( Department of Chemistry, G.F. (P.G.) College, Shahjahanpur-242001, UP, India) Neem, Azadirachta indica A. Juss a boon to mankind. Hamdard Medicus v. 51(3): p. 118-130, 2008 (Eng; 89 ref).

Azadrachta indica syn Melia azadarichta (Meliaceae, common name: Neem) has been extensively used in Unani, Ayurveda and Homeopathic medicine and has become a cynosure of modern medicine. In Sanskrit the name Arishta meaning "the cure all" is given to Neem whereas Ayurveda regards the tree as "cure all ailments". The importance of the tree has also been recognized by US National Academy of Sciences by titling the Neem as "The tree for solving global problems". Present review provides current information on chemical constituents of Neem oil, roots, trunk bark and leaves etc; their biological activities and uses in agriculture.


2009-05-2340 Barrera, E.D.C.; Suarez, L.E.C.* (Universidad Nacional de Colombia, Facultad de Ciencias, Departamento de Quimica, Laboratorio de Investigation en Productos Naturales Vegetalea; AA 14490, Cra 30 45-03, Ciudad Universitaria, Bogota D.C., Colombia) Three new 7,3',8.5'-connected bicyclo 3.2.1 octanoids and other neolignans from leaves of Nectandra amazonum NEES. (Lauraceae). Chemical & Pharmaceutical Bulletin v 57(6): p. 639-642, 2009 ( Eng; 22 ref).

Three new 7.3', 8.5'-connected (macrophyllin-type) bicyclo3.2.1octanoid neolignans (nectamazins A-C), were isolated from leaves of Nectandra amazonum (Lauraceae) along with seven known neolignans. Their structures were characterized by spectroscopic methods (1D, 2D NMR) and the absolute configuration was assigned on the basis of circular dichroism (CD) spectra supported by nuclear Overhauser effect spectroscopy (NOESY) correlations. The new compounds showed inhibition activity against platelet activating factor (PAF)-induced aggregation of rabbit platelets (antiplatelet).


2009-05-2341 Beghalia, M.; Ghalem, S.; Allali, H.; Belouatek, A.; Marouf, A. (Laboratory of Organic Chemistry, Natural Products and Analysis (COSNA), Department of Chemistry, Faculty of Sciences, University aboubekr Belkaid BP 119, 13000 Tlemcen, Algeria) Effects of an aqueous extract from Ammodaucus leucotrichus on calcium oxalate crystllization in vitro. Medicinal Plants v. 1(1): p. 37-39, 2008 (Eng; 14 ref).

The synthetic urine was prepared immediately before use by mixing with a T-type mixing chamber equal volumes of solutions A and B. Both solutions were prepared by dissolving chemicals of reagent-grade purity in deionised and redistilled water. Mixture agitation was maintained to prevent sedimentation. The crystal size development was monitored by polarized microscopy at different time intervals by proceedings as follows: Sample drops were examined every five minutes by polarising optical microscopy. The same experimental procedure was followed for the study of crystallization in the presence of inhibitors. As shown with Ammodocus leucotrichus (Apiaceae) the inhibitory effect was not dose dependent; the best inhibitory concentrations (97.25 percent and 97.85 percent) was observed at concentration of (75 percent) and (100 percent) mM/L, respectively, the inhibitory effect of Ammodocus plant involved growth crystal phases. The growth and agglomeration of calcium oxalate crystals are differently modulated by Ammodoucs. This is useful to formulate the dosage to prevent urinary calculi.


2009-05-2342 Berginc, J.; Zakelj, S.; Ursic, D.; Kristl, A. ( Faculty of Pharmacy, University of Ljubljana, Askerceva 7, 1000 Ljubljana, Slovenia) Aged garlic extract stimulates P-glycoprotein and multidrug resistance associated protein 2 mediated effluxes. Biological & Pharmaceutical Bulletin v. 32(4): p. 694-699, 2009 (Eng; 24 ref).

Influence of aged garlic (Allium sativum Liliaceae) extract (AGE) was studied on the transport function and electrophysiological parameters of the small intestinal mucosa. Aged garlic extract induced increase of the absolute value of the transepithelial potential difference and of the short-circuit current in both, permeability models tested (rat jejunum, Caco-2 cell monolayers) without affecting transepithelial electrical resistance. It also caused a significant increase of the P-glycoprotein and multidrug resistance associated protein 2 mediated effluxes through rat jejunum of marker substrates Rhodamine 123 and 2,4-dinitrophenyl-.S-glutathione, respectively. Rhodamine 123 efflux through the Caco-2 cell monolayers was not altered by aged garlic extract, whereas the efflux of 2,4-dinitrophenyl-S-glutathione increased significantly. So altered activity of the important transport proteins could significantly change the pharmacokinetic properties of conventional medicines taken concomitantly with aged garlic extracts.


2009-05-2343 Bustanji, Y.; Taha, M.O.; Al-Masri, I.M.; Mohammad, M.K. (Faculty of Pharmacy, University of Jordan, Amman 11942, Jordan) Docking simulations and in vitro assay unveil potent inhibitory action of papaverine against protein tyrosine phosphatase 1B. Biological & Pharmaceutical Bulletin v. 32(4): p. 640-645, 2009 (Eng; 38 ref).

Papaverine is a member of isoquinoline alkaloids isolated from opium poppy, (Papaver somniferum Papaveraceae). The structural similarity between papaverine and berberine, a known inhibitor of human protein tyrosine phosphatase 1B (h-PTP 1B), prompted to investigate the potential of papaverine as h-PTP 1B inhibitor. The investigtion included simulated docking experiments to fit papaverine into the binding pocket of h-PTP 1B. Papaverine was found to readily dock within the binding pocket of h-PTP 1B in a low energy orientation via an optimal set of attractive interactions. Experimentally, papaverine illustrated potent in vitro inhibitory effect against recombinant h-PTP 1B (IC 50 = 1.20 microM). In vivo papaverine significantly decreased fasting blood glucose level of Balb/c mice. These findings should encourage screening of other natural alkaloids for possible anti-h-PTP 1B activities.


2009-05-2344 Cai, B.X.; Jin, S. L.; Luo, D.*; Lin, X.F.; Gao, J. (Department of Dermatology, The First Affiliated Hospital of Nanjing Medical University; Nanjing 210029, P. R. China) Ginsenoside Rb1 suppresses ultraviolet radiation-induced apoptosis by inducing DNA repair. Biological & Pharmaceutical Bulletin v 32(5): p. 837-841, 2009 (Eng; 31 ref).

The functional role of ginsenoside Rb1 was investigated in UV-induced DNA damage and apoptosis in HaCaT (keratinocyte cell line) cells, and Xpc- knockout mouse keratinocytes. Flow cytometry and Hoechst 33258 staining were performed in analyzing UV-induced apoptosis in keratinocytes treated with ginsenoside Rb1. The ImmunoDotBlot assay was used to detect cyclobutane pyrimidine dimers, the main sign of DNA damage. Western blot analysis was applied for analyzing Xeroderma pigmentosum-C (XPC) and excision repair cross-complementing 1 (ERCC1), two of the NER proteins. Ginsenoside Rb1 inhibited UV-induced apoptosis of keratinocytes and caused a notable reduction in UV-specific DNA lesions. which was due to induction of DNA repair. This reduction was not observed in Xpc- knockout keratinocytes. Ginsenoside Rb1 induced the expression of specific components of the NER complex, such as XPC and ERCC1. Results demonstrate that ginsenoside Rb1 can protect cells from apoptosis induced by UV radiation by inducing DNA repair.


2009-05-2345 Capettini, L.S.A.; Campos, L.V.A.; dos Santos, M.H.; Nagem, T.J.; Lemos, V.S.; Cortes, S.F. (Department of Pharmacology, Institute of Biological Sciences, Federal University of Minas Gerais, Belo Horizonte, MG, Brazil) Vasodilator and antioxidant effect of xanthones isolated from Brazilian medicinal plants. Planta Medica v. 75(2): p. 145-148, 2009 (Eng; 14 ref).

Six xanthones viz., xanthone(1), 1 -hydroxy-xanthone (2), 4-hydroxyxanthone (3), 1-hydroxy-8-methoxy-xanthone (4), 1,3-dihydroxy-7-methoxyxanthone (5) and 2,6,8-trihydoxy-1-methoxyxanthone (6) were found to induced concentration-dependent vasorelaxant effects in enobthelium-intact mice aortic rings. The presence of a hydroxy group in position 1 seemed to decrease the vasodilator effect while a hydroxy in position 4 and an increased number of hydroxy groups improved the vasorelaxatory potential of xanthones. All xanthones showed antioxidant activity but their potencies did not correlate with the vasodilatory effect. Results suggest that the tested xanthones are potentially vasorelaxant and antioxidants but the two activities are not interrelated.


2009-05-2346 Castardo, J.C.; Prudente, A.S.; Ferreira, J.; Guimaraes, C.L.; Monache, F.D.; Filho, V.C.; Otuki, M.F.; Cabrini, D.A. (Depepartment of Pharmacology, Universidade Federal do Parana, PR Brazil) Anti-inflammatory effects of hydroalcoholic extract and two biflavonoids from Garcinia gardneriana leaves in mouse paw oedema . Journal of Ethnopharmacology v. 118(3): p. 405-411, 2008 (Eng ; 33 ref).

Garcinia gardneriana (Clusiaceae) is widely distributed in Brazil and used in folk medicine to treat inflammation, pain, and urinary tract and other infections. The results showed that hydroalcoholic extracts from Garcinia gardneriana HEGG from the leaves, bark and seeds reduced carrageenan-induced mouse paw inflammation. in addition to diminishing the myeloperoxidase activity in the stimulated tissues. The reduction of neutrophil infiltration by treatment with the HEGG from leaves was confirmed by histology. The leaf extract also reduced the paw oedema evoked by bradykinin, histamine, prostaglandin E2 and 12-O-tetradecanoylphorbol acetate. However, it partially decreased substance P and compound 48/80-caused paw oedema, without any influence on the arachidonic acid-induced oedema. Both of the isolated compounds, fukugetin and GB-2a, prevented the carrageenan-induced paw oedema. In conclusion, this study showed important antiinflammatory effects of HEGG through its interaction with different intracellular signaling pathways, without interfering with the formation of arachidonic acid (AA) metabolites.


2009-05-2347 Chandan, B.K.; Saxena, A.K.; Shukla, S.; Sharma, N.; Gupta, D.K.; Singh, K.; Suri, J.; Bhadauria, M.; Qazi, G.N. ( Indian Institute of Integrative Medicine, Canal Road, Jammu-Tawi 180016, J&K, India) Hepatoprotective activity of Woodfordia fruticosa Kurz flowers against carbon tetrachloride induced hepatotoxicity. Journal of Ethnopharmacology v. 119(2): p. 218-224, 2008 (Eng ; 35 ref).

Petroleum ether (WF1), chloroform (WF2), ethyl alcohol (WF3) and aqueous (WF4) extracts of the flowers of Woodfordia fruticosa (Lythraceae) were evaluated for hepatoprotective activity against carbon tetrachloride induced hepatotoxicity using biochemical markers, hexobarbitone sleep time, bromosulphalein (BSP) clearance test and effect on bile flow and bile solids. The aqueous extract (WF4) was most potent among the four extracts studied in detail. WF4 showed significant hepatoprotective activity against carbon tetrachloride induced hepatotoxicity as evident by restoration of serum transaminases, alkaline phosphatase, bilirubin and triglycerides. The restoration of microsomal aniline hydroxylase and amidopyrine-N-demethylase activities indicated the improvement in functional status of endoplasmic reticulum. Restoration of lipid peroxidation and glutathione contents suggests the antioxidant property of WF4. The recovery in bromosulphalein clearance and stimulation of bile flow suggested the improved excretory and secretary capacity of hepatocytes. Light microscopy of the liver tissue further confirmed the reversal of damage induced by hepatotoxin. Present study showed that the aqueous extract of Woodfordia fruticosa significantly restores physiological integrity of hepatocytes. WF4 did not show any sign of toxicity up to oral dose of 2 g/kg in mice.


2009-05-2348 Chang, C.Y.; Huang, Z.N.; Yu, H.H.; Chang, L.H.; Li, S.L.; Chen, Y.P.; Lee, K.Y.; Chuu, J.J. (Institute of Biotechnology, College of Engineering, Southern Taiwan University, Tainan, Taiwan) The adjuvant effects of Antrodia camphorata extracts combined with anti-tumor agents on multidrug resistant human hepatoma cells . Journal of Ethnopharmacology v. 118(3): p. 387-395, 2008 (Eng ; 42 ref).

The objectives of this study were to investigate the adjuvant antitumor effects of Antrodia camphorata in human hepatoma cells (C3A and PLC/PRF/5) which are resistance to most antitumor agents, elucidate the possible regulation pathways, and measure the tumor growth and survival rate in xenograft-nude mice after combined with antitumor agents. We have found that Antrodia camphorata extracts, when combined with antitumor agents, showed adjuvant antiproliferative effects on hepatoma cells (in vitro) and on xenografted cells in tumor-implanted nude mice (in vivo), which then extended their median survival days. Furthermore, solid-state extracts of Antrodia camphorata (AC-SS) showed its adjuvant effects through the inhibition of MDR gene expressions and the pathway of COX-2- dependent inhibition of p-AKT, which ultimately resulted in the induction of apoptosis in hepatoma cells.


2009-05-2349 Chen, A.; Wang, H.; Zhang, J.; Wu, X.; Liao, J.; Li, H.; Cai, W.; Luo, X.; Ju, G. (Depepartment of Anatomy & Neurobiology, Xiangya School of Medicine, Central South University, Changsha 410013, China) BYHWD rescues axotomized neurons and promotes functional recovery after spinal cord injury in rats . Journal of Ethnopharmacology v. 117(3): p. 451-456, 2008 (Eng ; 37 ref).

Buyang Huanwu Decoction (BYHWD), a Chinese prescription that has been used for hundreds of years to treat paralysis, has gained attention recently due to its significant neuroprotective properties. This study was to investigate whether BYHWD treatment protected axotomized rubrospinal neurons (RN) following spinal cord injury (SCI) in rats. Adult rats received a right lateral funiculus transection at the level between C3 and 04, and were either treated with BYHWD or with distilled water (DW) via gastrogavage. Effects on RN viability and atrophy were determined by Nissl staining, axon regeneration was examined by biotinylated dextran amine (BDA) tracing techniques and functional recovery was studied by a test of forelimb usage during spontaneous vertical exploration. RN cell number and mean somal size were 20 percent and 29 percent higher, respectively, in BYHWD-treated rats relative to DW-treated rats. There were a small number of BDA-labeled axons in the caudal of injury site in BYHWD-treated rats, whereas no caudal axonal regeneration was detected in DW-treated rats. BYHWD-treated rats used the injured forelimb more often than rats treated with DW. These results indicate that administration of BYHWD following SCI protects injured neurons, promotes regeneration, and enhances functional recovery.


2009-05-2350 Chen, C.C.; Hsu, C.Y.; Chen, C.Y.; Liu, H.K. ( Division of Medicinal Chemistry, National Research Institute of chinese Medicine, Taipei, Taiwan, ROC) Fructus corni suppresses hepatic gluconeogenesis related gene transcription, enhances glucose responsiveness of pancreatic beta-cells, and prevents toxin induced beta-cell death . Journal of Ethnopharmacology v. 117(3): p. 483-490, 2008 (Eng ; 41 ref).

Fructus Corni, the fruits of Cornus officinalis is one important ingredient in Quei Fu Di Huang Wan, a Chinese herbal mixture. In the present study, additional antidiabetic actions of Fructus Corni on transcriptional regulation of hepatic gluconeogenesis or beta-cell functions were investigated. Insulin mimetic action of Fructus Corni on dexamethasone and 8-bromo-cAMP induced phosphoenolpyruvate carboxykinase (PEPCK) expression in H4IIE cells was investigated. Besides, BRIN-BD11 cells were used to evaluate both insulinotropic and beta-cell protective effect of Fructus Corni. Firstly, both methanol extract (CO-W-M) and fraction (CO-W-M2) had potent insulin mimic activity on PEPCK expression. Secondly, possibility of both loganin and ursolic acid as the responsible compounds was excluded. Moreover, indication of the existence of phenolic compounds in CO-W-M2 was noticed. In the presence of CO-W-M2, not only was the viability of BRIN-BD11 cells treated with alloxan, streptozotcin, or cytokine mix all significantly increased but also glucose-stimulated insulin secretion was potentiated. The ability of CO-W-M2 to reduce gene expression for hepatic gluconeogenesis, to protect beta-cell against toxic challenge, and to enhance insulin secretion strengthen the role of Fructus Corni in diabetes therapy.


2009-05-2351 Chen, J.; Ma, M.; Lu, Y.; Wang, L.; Wu, C.; Duan, H. (Department of Experimental Haematology, Beijing Institute of Radiation Medicine (BIRM), Beijing, P.R. China) Rhaponticin from rhubarb rhizomes alleviates liver steatosis and improves blood glucose and lipid profiles in KK/Ay diabetic mice. Planta Medica v. 75(5): p. 472-477, 2009 (Eng; 36 ref).

Several stilbene compounds including rhaponticin were isolated from extracts of rhubarb Rheum fronzenbachii (Polygonaceae) rhizomes. The effect of rhaponti-cin were examined on glucose utilization, lipid metabolism, and liver and heart function in a KK/Ay type 2 diabetic mouse model. The results showed that oral ad-ministration of rhaponticin (125 mg/kg) significantly reduced blood glucose levels and improved oral glucose tolerance of KK/Ay diabetic mice. Elevated plasma triglyceride (TG), low density lipo-protein (LDL), cholesterol (CHO), non-esterified free fatty acids (NEFA), and insulin levels were also markedly attenuated. Serum enzymatic activities in the rhaponticin-treated group significantly decreased in comparison to the untreated model group. Livers of rhaponticin-treated mice had relatively normal cellular size and decreased fibrosis and steatosis.


2009-05-2352 Choi, Y.H.; Yan, G.H. (Department of Anatomy and Histology and Embryology, Yanbian University School of Basic Medical Sciences; 1829 JuZi Street, YanJi City 133000, Jilin, China) Ellagic acid attenuates immunoglobulin E-mediated allergic response in mast cells. Biological & Pharmaceutical Bulletin v. 32(6): p. 1118-1121, 2009 (Eng; 18 ref).

Ellagic acid is a polyphenol found in certain fruits and nuts, such as raspberries, straberries, walnuts, longan seed, mango kernel and pomegranate. Present study demonstrated that ellagic acid attenuates immunoglobulin (Ig)E-mediated allergic response in mast cells and in vivo. Oral administration of ellagic acid inhibited anti-dinitrophenyl (DNP) IgE-mediated passive cutaneous anaphylaxis. Ellagic acid dose-dependently reduced histamine release and the expression and secretion of pro-inflammatory cytokines, such as tumour necrosis factor-alpha and interleukin-6 in rat peritoneal mast cells (KPMC) activated by anti-DNP IgE. Moreover, ellagic acid suppressed an increase in intracellular calcium ion concentration (Ca2+i) in RPMC. Furthermore, ellagic acid decreased the activation of nuclear factor-kappa B (NF-keppaB). Decreased NF-keppaB activity as well as reduced calcium might be involved in the inhibitory effect of ellagic acid on the secretory response. Results provide possibility that ellagic acid may serve as an effective therapeutic agent for allergic diseases.


2009-05-2353 Choquenet, B.; Couteau, C.; Paparis, E.; Coiffard, L.J.M. (Faculty of Pharmacy, Universite de Nantes, Nantes Atlantique Universites, Nantes, France) Interest of ferulic acid ethyl ester in photoprotective creams: Measure of efficacy by in vitro method. Natural Product Research v. 22(16): p. 1467-1471, 2008 (Eng; 15 ref).

Topical sunscreens have been used for many years on exposed areas to protect the skin from the damaging effects of ultraviolets. If the sunscreens were essential, it is suggested that they have adverse effects. We chose to study ferulic acid ethyl ester (FAEE) as agent which could potentially be used in natural sunscreen products. FAEE was incorporated at various concentrations into O/W emulsions. Total of 30 mg of product exactly weighed were spread on poly(methylmethacrylate) plates over the whole surface (25 cm2). So, sun protection factor (SPF) and PF-UVA of the creams were measured in vitro. Transmission measurements between 290 and 400 nm were carried out using a spectrophotometer equipped with an integrating sphere. Incorporated in O/W creams, at a concentration of 10 percent, FAEE give a SPF similar to that of benzymidazilate, a filter permitted in EU.


2009-05-2354 Coelho, R.G.; Gonzalez, F.G.; Sannomia, M.; Di Stasi, L.C.; Vilegas, W. (Dept de Quimica Organica, Instituto de Quimica de Araraquara, UNESP-Sao Paulo State University, Araraquara, SP, Brazil) Gastric anti-ulcer activity of leaf fractions obtained of polar extract from Wilbrandia ebracteata in mice. Natural Product Research v. 23(1): p. 51-59, 2009 (Eng; 13 Ref).

Leaf fractions of Wilbrandia ebracteata were investigated for anti-ulcerogenic effects in ethanol and indomethacin-induced gastric ulcer assays in mice. Protective antiulcer effects were detected only in the ethanol-induced ulcer assay effects after pre-treatment with MeOH extract, MeOH chlorophyll-free, chlorophyll residue, HEX, DCM, aqueous MeOH fraction, ethyl acetate (EtOAc) and aqueous fractions. A potent antiulcerogenic effect was determined after pre-treatment of animals with EtOAc fraction, which was fractionated for isolation of active constituents. Seven flavonoids, 3',4',5,6,7,8-hexahydroxyflavonol, orientin, isoorientin, vitexin, isovitexin, luteolin, 6-methoxy-luteolin were isolated from the leaves of W. ebracteata (Cucurbitaceae) by chromatographic methods and identified by their spectral data. The data suggest that flavonoids are active anti-ulcerogenic compounds from leaves of W. ebracteata . The ability of scavenging free radicals was evaluated by DPPH reduction assay by TLC of flavonoids isolated.


2009-05-2355 Deshmukh, P.B.; Choudhari, C. (Department of Chemistry, Science College, Nanded-431 605, Maharashtra, India) Effect of Semecarpus anacardium (Bhallataka) nut oil on some muscle enzymes of albino rat. Bioinfolet v. 6(3): p. 235-237, 2009 (Eng; 13 ref).

Semecarpus anacardium (Bhallataka, Anacardiaceae) pericarp oil extract was orally administered to albino rats of either sex. The LD50 was found to be 1 gm / kg bw / day for 4 days. Alterations in activity of enzymes of thigh muscles indicated muscular dystrophy and weakness in treated rats.


2009-05-2356 Ding, L.; Qiu, L.; Zhang, J.; Guo, B.* (Department of Biochemical Pharmacy, School fo Pharmacy, Second Military Medical University; 325 Guohe Road, Shanghai 200433, China) Camptothecin-induced cell proliferation inhibition and apoptosis enhanced by DNA methyltransferase inhibitor, 5-Aza-2'-deoxycytidine. Biological & Pharmaceutical Bulletin v. 32(6): p. 1105-1108, 2009 (Eng; 23 ref).

Using two-dimentional electrophoresis analysis and matrix assisted laser deorption/ionization-time of flight (MALDI-TOF)-MS/MS identification, the hepatocellular carcinoma cell line SMMC-7721' was investigated for changes of protein expression following the treatment with camptothecin (CPT), an active component of the Chinese tree, Camptotheca acuminata (Nyssaceae). Proteomic resuts showed that CPT treatment caused decreased expression of galectiri-1 in SMMC-7721 cells. Quantitative real- time reverse transcription-polymerase chain reaction (RT-PCR) analysis confirmed mRNA expression changes in galectin-1. Protein expression levels of DNA methyltransferases (DNMTs) were downregulated in response to CPT. The DNMT inhibitor 5-aza-2'-deoxycytidine (DAC) sensitized SMMC-7721 cells to the cytotoxic effect of CPT. Results indicate that inhibition of DNMT activity by CPT may play a role in CPT-induced cell proliferation inhibition and apoptosis.


2009-05-2357 Ding, Y.; Nguyen, H.T.; Choi, E.M.; Bae, K.W.; Kim, Y.H. (College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea) Rhusonoside A, a new magastigmane glycoside from Rhus sylvestris, increases the function of osteoblastic MC3T3-E1 cells. Planta Medica v. 75(2): p. 158-162, 2009 (Eng; 11 ref).

Chemical investigation of the stems and leaves of Rhus sylvestris (Anacardiaceae) afforded a new megastigmane glycoside named rhusonoside A (1), along with four known compounds: dihydroquercetin (2), astragalin (3), hyperin (4), and kaempferol-3-O-rutinoside (5). Their structures were determined by a combination of spectroscopic analysis and application of the modified Mosher's method. The effect of compounds 1 -5 on the function of osteoblastic MC3T3-E1 cells was examined by determining cell viability, alkaline phosphatase (ALP) activity, collagen synthesis, and mineralization. Rhusonoside A significantly increased the function of osteoblastic MC3T3-E1 cells. Cell viability, ALP activity, and collagen synthesis were increased dose dependently, up to 155.39 percent, 171.27 percent, and 134.25 percent, respectively, of the basal value at 10 microM (P less than 0.05). In addition, 0.1 microM of compound 1 significantly increased mineralization of MC3T3-E1 cells to 142.78 percent (P less than 0.05) of the basal value.


2009-05-2358 Dong, H.; He, L.; Huang, M.; Dong, Y. (Department of Pharmacy, The First Affiliated Hospital of Medical College, Xi'an Jiaotong University, Xi'an, PR China) Anti-inflammatory components isolated from Atractylodes macrocephala Koidz. Natural Product Research v. 22(16): p. 1418-1427, 2008 (Eng; 7 ref).

The petroleum ether-ether (1:1) extract of Atractylodis macrocephalaej was screened by cell membrane chromatography (CMC) and subsequently separated by column chromatography (CC) and high performance liquid chromatography (HPLC). Five components were isolated and identified as atractylenolide III 1, atractylenolide I 2, 14-acetoxy-12-senecioyloxytetradeca-2E,8E, 10E-trien-4,6-diyn-1 -ol 3, 14-acetoxy-12-alpha-methylbutyl-2E,8E, 1 OE-trien-4,6-diyn-1-ol 4 and 14-acetoxy-12-beta-methylbutyl-2E,8E,10E-trien-4,6-diyn-1-ol 5 by routine spectrometric methods. The data of 5 and 13C-NMR data of 3 and 4 were reported for the first time. Further in vivo experiments showed that the five components exhibited significant inhibiting effects both on the ear edema induced by xylene and on the peritoneal capillary permeability induced by acetic acid in mice.


2009-05-2359 El-Abhar, H.S.; Hammad, L.N.A.; Gawad, H.S.A. ( Depepartment of Pharmacology & Toxicology, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, 11562 Cairo, Egypt) Modulating effect of ginger extract on rats with ulcerative colitis . Journal of Ethnopharmacology v. 118(3): p. 367-372, 2008 (Eng ; 45 ref).

Male Wistar rats received 3 different doses of GE, sulfasalazine, or vehicle for 3 consecutive days before induction of UC by intra-rectal acetic acid administration, and continued further for 7 days after the induction. The colonic mucosal injury was assessed by macroscopic scoring, and histological examination. Furthermore, the mucosal content of malondialdehyde (MDA), protein carbonyl (PCO), and reduced glutathione (GSH) with the catalase (CAT) and superoxide dismutase (SOD) activity, were appraised as parameters of the redox state. Acute inflammatory response was determined by measuring myeloperoxidase (MPO), tumor necrosis factor (TNF-alpha), and prostaglandin E2 (PGE2). All parameters were altered in ulcerated rats, and improved in animals receiving GE, an effect that was comparable to that of the standard sulfasalazine, especially at the highest dose level. Colonic mucosal injury parallels with the histological and biochemical evaluations. Results showed a valuable effect of ginger Zingiber officinale extract against acetic acid-induced ulcerative colitis possibly by its antioxidant and antiinflammatory properties.


2009-05-2360 Evidente, A.; Kireev, A.S.; Jenkins, A.R.; Romero, A.E.; Steelant,.W.F.A.; Slambrouck, S.V.; Kornienko, A. ( Dipartimento di Scienze, del Suolo, della Planta, dell'Ambiente e delle Produzioni, Animali, Universita di Napoli Federico II, Portici, Italy) Biological evaluation of structurally diverse Amaryllidaceae alkaloids and their synthetic derivatives; discovery of novel leads for anticancer drug design. Planta Medica v. 75(5): p. 501-507, 2009 (Eng; 57 ref).

Twenty-nine Amarylidaceae alkaloids and their derivatives belonging to the five most common groups were evaluated for antiproliferative, apoptosis-inducing, and antiinvasive activities in vitro. The antiprolifera-tive properties of each test compound are in agreement with those reported in the literature, while the high potency of amarbellisine is reported for the first time. It was also found that with the exception of ungeremine, amarbellisine, and hippeastrine, the antiproliferative effect of the potent compounds is apoptosis mediated. Thus, apoptosis in Jurkat cells was triggered by narciclasine, narciclasine tetraacetate, C10b-R-hydroxypancratistatin, cis-dihydronarciclasine, trans-dihydronarciclasine, lycorine, 1-O-acetyllycorine, lycorine-2-one, pseudolycorine, and haemanthamine. The collagen type I invasion assay revealed potent antiinvasive properties associated with N-methyllycorine iodide, hippeastrine, clivimine, buphanamine, and narciclasine tetraacetate, all of which were tested at non-toxic concentrations. The antiinvasive activity of buphanamine is particularly promising because this alkaloid is not toxic to cells even at much higher doses.


2009-05-2361 Feng, Y.L.; Li, H.R.; Rao, Y.; Luo, X.J.; Xu, L.Z. ; Wang, Y.S.; Yang, S.I.; Kitanaka, S. (National Pharmaceutical Engineering Centre for Solid Preparation in Chinese Herbal Medicine, Jiangxi University of Traditional Chinese Medicine; Nanchang 330006, P.R. China) Two sulfated triterpenoidal saponins from the barks of Zygophyllum fabago L.. Chemical & Pharmaceutical Bulletin v 57(6): p. 612-614, 2009 ( Eng; 5 ref).

Two new sulfated triterpenoid saponins, zygophylosides Q and R, were isolated from the barks of Zygophyllum fabago (Zygophyllaceae). Their structures were elucidated as 3beta,24,28,30-tetrahydro-urs-20-ene-24-O-sulphonyl-3-O-beta-D-glucopy ranosyl-30-O-beta-D-glucopyranoside and 3beta,24,28,30-tetrahydro-urs-20-ene-24-O-sulphonyl-3-O-{1beta-D-xylop yranosyl}-30-O-beta-D-glucopyranoside, respectively, by spectral and chemical evidence.


2009-05-2362 Ge, H.M.; Jiao, R.H.; Zhang, Y.F.; Zhang, J.; Wang, Y.r.; Tan, R.X. (Institute of Functional Biomolecules, State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing, P.R. China) Cytotoxicity and phytotoxicity of trichothecene macrolides from Myrothecium gramminum. Planta Medica v. 75(3): p. 227-229, 2009 (Eng; 19 ref).

1H-NMR guided fractionation of the EtOAc extract from the culture of fungus M. gramminum (Tuberculariaceae) (strain no. 3.1968) led to the isolation of eight trichothecene macrolides (1-8), all being substantially inhibitory against HepG2 (human hepatocellular carcinoma) and KB (human nasopharynyeal epidermoid tumor) cell lines with IG50 values ranging from 2.2 to 12.2 microg/mL. Their inactivity to or weaker action on Vero cells (IC50 values more than 20 microg/mL, originated from the African green monkey kidney) highlighted preliminarily the nature of the selective cytotoxicity of the fungal metabolites against the test cancer cell lines. In addition, verrucarin A and roridin A were found to be potent inhibitors of the radial growth of Echinochoa crusgalli (Gramineae) with correspending IC50 values of (7.96 plus or minus 0.31) x 10 -6 and (9.18 plus or minus 0.44 x 10 -6 M, respectively).


2009-05-2363 Gong, T.; Wang, D.X.; Chen, R.Y.; Liu, P.; Yu, D.Q. (Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 1 Xian Nong Tan Street, Beijing 100050, People's Republic of China) Novel benzil and isoflavone derivatives from Millettia dielsiana. Planta Medica v. 75(3): p. 236-242, 2009 (Eng; 25 ref).

The analysis of vine stem extract from Millettia dielsiana (Leguminosae) yieided a novel benzil (1) and five new prenylated isoflavones (2-6) together with three known isoflavones (7-10) and one known flavone (11), and their structures were elucidated on the basis of chemical and spectral analysis. The absolute configuration of the 3",4"-diols in 6 was determined by observing the CD induced after addition of dimolybdenum tetraacetate in DMSO solution (Snatzke's method). Some isolates were tested for their antiinflammatory and antithrombase activities and cytotoxicities. Compound 2, barbigerone, and genistein showed significant antiinflammatory activity, with inhibitory ratios 59.1 percent, 59.5 percent, and 58.5 percent, respectively, at 10 microM, while compound 4 exhibited moderate cytotoxicity.


2009-05-2364 Ha, H.H.; Park, S.Y.; Ko, W.S.; Kim, Y.H. ( Depepartment of Molecular Biology, College of Natural Sciences, Pusan National University, Jangieon-dong, Keumjeong-gu, Pusan 609-735, Republic of Korea) Gleditsia sinensis thorns inhibit the production of NO through NF-kB suppression in LPS-stimulated macrophages. Journal of Ethnopharmacology v. 118(3): p. 429-434, 2008 (Eng ; 37 ref).

The thorns of Gleditsia sinensis (Leguminosae) have been used in traditional medicine for the treatment of inflammatory diseases including swelling, suppuration, carbuncle and skin diseases in China and Korea. In this study, we investigated the mechanism responsible for antiinflammatory effects of{Gleditsia sinensis thorns in RAW 264.7 macrophages. The aqueous extract of Gleditsia sinensis thorns (AEGS) inhibited LPS-induced NO secretion as well as inducible nitric oxide synthase (iNOS) expression, without affecting cell viability. Furthermore, AEGS suppressed LPS-induced NF-KB activation, phosphorylation and degradation of IKB-alpha phosphorylation of extracellular signal-regulated kinase 1/2 (ERK1/2) and c-Jun N-terminal kinase (JNK). These results suggest that AEGS has the inhibitory effects on LPS-induced NO production and iNOS expression in macrophages through blockade in the phosphorylation of MAPKs, following IKB-alpha degradation and NF-KB activation.


2009-05-2365 Han, M.; Fu, S.; Gao, J.Q.; Fang, X.L.* ( Department of Pharmaceutics, School of Pharmacy, Fudan University; Lane 826, Zhangheng Road, Shanghai 201203, China) Evaluation of intestinal absorption of ginesenoside Rg1 incorporated in microemulsion using parallel artificial membrane permeability assay. Biological & Pharmaceutical Bulletin v. 32(6): p. 1069-1074, 2009 (Eng; 34 ref).

Ginsenoside Rg1 (Rg1) main ingredient of Panax notoginseng (Araliaceae). Its water-in-oil (W/O) microemulsions (MEs) and parallel artificial membrane permeability assay (PAMPA.) were utilized for the evaluation of in vitro permeability of early drug candidates, as well as rat in vivo pharmacokinetics and in vitro permeability measurements, to investigate the effect of w/o ME on Rg1 absorption. Correlation between various models was performed to estimate the feasibility of PAMPA in the application of pharmaceutical preparation studied. After being administrated intraduodenally to rats, most of MEs can enhance the intestinal absorption of Rg1 to various extents with relative bioavailability ranging from 268 to 1270 percent using drug solution as control. This enhanced, absorption of Rg1 may be related to its increased membrane permeability induced by ME as exhibited in the PAMPA and rat in vitro permeability measurements. Meanwhile, rat in vivo pharmacokinetics-PAMPA correlation is signifincant for ME, representing a potential prospect for the application of PAMPA in the study of pharmaceutical preparation in some conditions.


2009-05-2366 Hussain, M.; Khurshid, M.; Tahavi, M.; Azim, R. ( Department of Botany, Govt. Postgraduate College, Abbottabad, Pakistan) Pollen allergy, an environmental hazard. Hamdard Medicus v. 51(3): p. 157-162, 2008 (Eng; 18 ref).

Allergens are antigenic substances capable of sensitizing the body in such a way that unusual responses occur in hypersensitive individuals. Almost any substance whether of biological, chemical or synthetic origin, may prove to be allergenic. However, most of the allergens are composed of plant or animal matter, they merit consideration in a treatise on natural products. The author trapped the airborne pollengrains in the years 2003-2004. Grains of Poaceae, Cyperaceae were found to be maximum in the air during the months of February to April. Some important aeroallergenic pollen types were Broussonetia, Amaranthus, Prosopsis, Xanthium and Cynodon. Pollen of family Poaceae dominated with a range from 20-45 percent to air spores and are highly allergenic.


2009-05-2367 Ishikawa, T.; dos Santos Donatini, R.; Diaz, I.E.C.; Yoshida, M.; Bacchi, E.M.; Kato, E.T.M. (Departamento de Farmacia, Faculdade de Ciencias Farmaceuticas, Universidade de Sao Paulo, C.P.66083, CEP 05508-000, Sao Paulo, SP, Brazil) Evaluation of gastroprotective activity of Plinia edulis (Vell.) Sobral (Myrtaceae) leaves in rats . Journal of Ethnopharmacology v. 118(3): p. 527-529, 2008 (Eng ; 23 ref).

Plinia edulis an arboreous species popularly known as Cambuca is native to the Brazilian Atlantic Rain Forest. Despite its traditional uses, no reports are available on the safety of this utilization or on the relationship between the antiulcer activity of its extract and its phytochemical compounds. This paper reports on the investigation of the acute toxicity and gastroprotective effect of the aqueous ethanol extract of leaves of Plinia edulis on HCl/ethanol-induced ulcers. In order to correlate the secondary metabolites and the efficacy of the crude drug in traditional medicine, the extract was submitted to chromatographic fractionation after solvent partition. The extract did not show acute toxicity in mice treated with 5 g/kg P.O., but exhibited significant antiulcer activity in rats at doses of 100, 200, and 400 mg/kg p.o., more active than the reference drug lansoprazole. The ethyl acetate fraction yielded beta-armyrin, oleanolic acid, ursolic acid, and maslinic acid, which were identified based on spectrometric analyses. Since antiulcerogenic activity is not restricted to one class of compounds in plants, the triterpenoids isolated in the extract can be associated with the observed effect.


2009-05-2368 Ishida, T.; Takeda, T.; Koga, T; Yahata, M.; Ike, A.; Kuramoto, C.; Taketoh, J.; Hashiguchi, I.; Akamine, A.; Ishm, Y.R ; et al. (Graduate School of Pharmaceutical Sciences, Kyushu University, Kyushu University; 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582, Japan) Attenuation of 2,3,7,8-tetrachlorodibenzo-p-dioxin toxicity by resveratrol: A comparative study with different routes of administration. Biological & Pharmaceutical Bulletin v 32(5): p. 876-881, 2009 (Eng; 38 ref).

Effect of oral resveratrol were examined on the sub-acute toxic effect of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) in C57BL/6J mice. A TCDD-induced wasting syndrome was not alleviated by treating mice for 28 d with oral resveratrol. However, subcutaneous injection of resveratrol for 5 d significantly improved the symptoms. Neither oral nor subcutaneous administration of resveratrol alleviated TCDD-induced hepatomegaly and thymic atrophy. Steatosis produced by TCDD was markedly counteracted by co-treatment with oral resveratrol. The reason for the lack of protective effect via subcutaneous injection route was assumed to be due to the minor accumulation of hepatic lipids 5 d after TCDD treatment. To clarify the mechanisms, the activity of ethoxyresorufin O-deethylase and the content of thiobarbituric acid-reactive substances in the liver were measured. Both indices increased by TCDD treatment were significantly suppressed by injection of resveratrol. In contrast, oral resveratrol failed to rescue them. In agreement with the greater protective effects of resveratrol, studies indicated that the area under the curve extrapolated to infinity was 8.2-times greater following subcutaneous injection compared with oral administration. These data suggest that the oral resveratrol is an agent capable of combating dioxin toxicity and increasing the bioavailability of this polyphenol enhances its protective effect.


2009-05-2369 Jeong, S.; Chae, K.; Jung, Y.S.; Rho, Y.H.; Lee, J.; Ha, J.; Yoon, K.H.; Kim, G.C.; Oh, K.S.; Shin, S.S.; Yoon, M. ( Department of Life Sciences, Mokwon University, Taejon 302-729, Republic of Korea) The Korean traditional medicine Gyeongshingangjeehwan inhibits obesity through the regulation of leptin and PPARalpha action in OLETF rats. Journal of Ethnopharmacology v. 119(2): p. 245-251, 2008 (Eng ; 39 ref).

Gyeongshingangjeehwan (GGEx), which comprises Liriope platyphylla (Liliaceae, Platycodon grandiflorum (Campanulaceae), Schisandra chinesis (Magnoliaceae), and Ephedra sinica (Ephedraceae), has traditionally been used as an antiobesity drug in Korean local clinics, although there is no evidence concerning the scientific analyses of its effects and mechanism(s) of action. Thus, we investigated the effects of GGEx on obesity, as well as the mechanism by which GGEx functions, in Otsuka Long-Evans Tokushima Fatty (OLETF) male rats. Compared with obese OLETF control rats, administration of GGEx for 8 weeks significantly decreased food intake and plasma leptin levels as well as body weight gain and abdominal fat in OLETF rats. GGEx treatment not only decreased circulating triglycerides, but also inhibited lipid accumulation in the liver. GGEx increased the hepatic mRNA levels of PPARalpha target genes responsible for fatty acid beta-oxidation. Consistent with the in vivo data, GGEx elevated PPARalpha reporter gene expression in NMu2Li liver cells. These results suggest that GGEx may effectively prevent obesity and hypertriglyceridemia in part through the inhibition of feeding and the activation of hepatic PPARalpha.


2009-05-2370 Jeong, G.S.; Lee, D.S.; Kwon, T.O.; Lee, H.S.; An, R. B.; Kim, Y. C. (Institute of Radiological Imaging Science, Wonkwang University, Iksan 570-749, Korea) Cytoprotective constituents of the heartwood of Caesalpinia sappan on glutamate-induced oxidative damage in HT22 cells. Biological & Pharmaceutical Bulletin v 32(5): p. 945-949, 2009 (Eng; 29 ref).

The bioassay-guided fractionation of a MeOH extract of the heartwood of Caesalpinia sappan (Leguminosae) provided two compounds, sappanchalcone (2) and 4-O-methylepisappanol (3), together with a methoxy-chalconc, isoliquiritigenin 2'-methyl ether and three aromatic compounds, 4-O-methylsappanol (4), cae-salpine J, pluchoic acid. At concentrations of 20-40 microM, compound 2 showed significant cytoprotective effects against glutamate-induced oxidative stress through the induction of heme oxygenase (HO)-1 in HT22-immortalized hippocampal cells. Compound 3 also showed moderate neuroprotective effect at 40 microM, but compounds did not show any protective effects against glutamate-induced cytotoxicity in HT22 cells.


2009-05-2371 Ji, W.; Gong, B.Q. (State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, 130 Road Meilong, Shanghai 200237, China) Hypolipidemic activity and mechanism of purified herbal extract of Salvia miltiorrhiza in hyperlipidemic rats. Journal of Ethnopharmacology v. 119(2): p. 291-298, 2008 (Eng ; 45 ref).

Sprague-Dawley-male rats on a high-fat/high-cholesterol diet were treated orally with PSME, GW3965 (a selective liver X receptor agonist) or vehicle alone. Gene expression analysis and transactivation assays were used to clarify the molecular mechanisms of action of purified Salvia miltiorrhiza extract (PSME). The concentrations of plasma total cholesterol, low-density lipoprotein cholesterol (LDL-cholesterol) and triglycerides in rats treated with PSME at 150 mg kg day-1 were significantly decreased accompanied with significantly decreased concentrations of liver total cholesterol and triglycerides. In both drug-treated rats, the concentration of high-density lipoprotein cholesterol (HDL-cholesterol) was significantly elevated. Intriguingly, short heterodimer partner (SHP) mRNA level was significantly higher in PSME-treated rats (P less than 0.01), accompanied with the significantly decreased mRNA level of sterol regulatory element binding protein 1c (SREBPlc), which contributed to the decreases of liver and plasma triglycerides through a farnesoid X receptor-SHP-SREBPlc pathway. ATP-binding Cassette Transporter B11 (ABCB11) and murine Mdr2 P-glycoprotein (also known as ABCB4) were significantly induced by PSME, which were responsible for biliary cholesterol solubility by proper biliary secretion of bile salts and phospholipids. The transactivation assays were used to identify PSME as a farnesoid X receptor/liver X receptor alpha coagonist. These results indicated that PSME as a farnesoid X receptor/liver X receptor alpha coagonist largely improved the lipid profiles in the hyperlipidemic rats.


2009-05-2372 Jia, Q.; Su, W.; Peng, W.; Li, P.; Wang, Y. ( School of Life Science, Sun Yat-Sen University, Guangzhou 510275, PR China) Anti-diarrhoea and analgesic activity of the methanol extract and its fractions of Jasminum amplexicaule Buch.-Ham. (Oleaceae). Journal of Ethnopharmacology v. 119(2): p. 299-304, 2008 (Eng ; 33 ref).

Jasminum amplexicaule (Oleaceae) has been commonly used in the traditional medicine in dysentery, diarrhoea and bellyache in China. In the present work, the methanol extract of Jasminum amplexicaule and different fractions of this extract were studied for antidiarrhoea and analgesic activities. The antidiarrhoea activities were investigated using castor oil-induced, magnesium sulphate-induced diarrhoea models, antienteropooling assay and gastrointestinal motility models in mice. The analgesic activities were studied using hot-plate, writhing and formalin models in mice. At the doses of 100, 200 and 400 mg/kg, the methanol extract (ME) showed significant and dose-dependent antidiarrhoea and analgesic activity in these models. The chloroform fraction (CHF), ethyl acetate fraction (EAF) and the residual methanol fraction (RMF) exhibited similar activity using a dose of 200 mg/kg in these models. The pharmacological activities of the n-butanol fraction (BUF) were lesser than the ME extract and other fractions. These results may support the fact that this plant is traditionally used to cure diarrhoea and pain.


2009-05-2373 Jin, X.; Shen, G.; Gao, F.; Zheng, X.; Xu, X.; Shen, F.; Li, G.; Gong, J.; Wen, L.; Yang, X.; Bie, X. (Depepartment of Traditional Chinese Medicine, Second Affiliated Hospital School of Medicine, Zhejiang University, #88 Jiefang Road, Hangzhou 310009, China) Traditional Chinese drug ShuXueTong facilitates angiogenesis during wound healing following traumatic brain injury . Journal of Ethnopharmacology v. 117(3): p. 473-477, 2008 (Eng ; 20 ref).

ShuXueTong injection is a traditional Chinese drug designed to treat the patients of "blood stasis and stagnation (yu xue yu zhi)", including subacute brain trauma. We hypothesized that ShuXueTong may promote the brain wound healing by facilitating angiogenesis. Thus this study was designed to explore this hypothesis. By means of microvessel count, Western blotting, immunocytochemistry, methyl thiazolyl tetrazolium assay and etc., the effect of ShuXueTong on the angiogenesis of brain wound was studied and then its influence on the VEGF/VEGFR-2 pathway were explored. ShuXueTong facilitates angiogenesis in the brain wound and improves the neurological function of the traumatized rats. VEGF expression in the lesion was elevated due to ShuXueTong induction. The in vitro experiment revealed VEGFR-2 and SRF expression in the endothelial cells were enhanced when exposed to ShuXueTong for merely 1 d. Moreover, ShuXueTong promoted the endothelial cell proliferation via the VEGF/VEGFR-2 pathway. The mechanism of the therapeutic effect of ShuXueTong on traumatic brain injury lies at least partly in the enhanced angiogenesis in the lesion.


2009-05-2374 Jorge, M.P.; Madjarof, C.; Ruiz, A.L.T.G.; Fernandes, A.T.; Rodrigues, R.A.F.; de Oliveira Sousa, I.M.; Foglio, M.A.; de Carvalho, J.E. (CPQBA, P.O. Box 6171, University of Campinas, UNICAMP13083-970, SP, Brazil) Evaluation of wound healing properties of Arrabidaea chica Verlot extract . Journal of Ethnopharmacology v. 118(3): p. 361-366, 2008 (Eng ; 30 ref).

Arrabidaea chica (Bignoniaceae), popularly known as Crajiru, has been traditionally used as wound healing agent. Investigate in vitro and in vivo healing properties of Arrabidaea chica leaves extract (AC). AC was evaluated in vitro in fibroblast growth stimulation (0.25-250 (xg/mL) and collagen production stimulation (250 microg/mL) assays. Allantoin (0.25-250 microg/mL) and vitamin C (25 microg/mL) were used as controls respectively. DPPH and Folin-Ciocalteau assays were used for antioxidant evaluation, using trolox (0.25-250 microg/mL) as reference antioxidant. To study wound healing properties in rats, AC (100 mg/mL, 200 microL/wound/day) was topically administered during 10 days and wound area was evaluated every day. Allantoin (100 mg/mL 200 microL/wound/day) was used as standard drug. After treatment, wound sites were removed for histopathological analysis and total collagen determination. AC stimulated fibroblast growth in a concentration dependent way (ECso = 30 microg/mL), increased in vitro collagen production and demonstrated moderate antioxidant capacity. In vivo, AC reduced wound size in 96 percent, whereas saline group showed only 36 percent wound healing. AC efficiency seems to involve fibroblast growing stimulus and collagen synthesis both in vitro and in vivo, beyond moderate scavenging activity, corroborating Crajiru folk use.


2009-05-2375 Kambhoja, S.; Kumar, S. (Department of Pharmacognosy, The oxford College of Pharmacy, J.P. Nagar, I-Phase, Bangalore-560078) Antibacterial activity of fresh leaves of Triticum aestivum Linn. Biomed v. 2(1): p. 99-102, 2007 (Eng; 6 ref).

The shoot of Triticum aestivum (Gramineae) often referred as wheat grass or green blood. Antimicrobial activity of the successive extract of the fresh leaves of Triticum aestivum was evaluated against both gram positive and gram-negative bacterial strains by zone of inhibition study. The results revealed that the alcoholic and aqueous extracts were active against both gram positive and gram negative bacterial strains.


2009-05-2376 Khan, R.; Malik, A.; Adhikari, A.; Qadir, M.I.; Choudhary, M.I. (International Centre for Chemical and Biological Sciences, HEJ Research Institute of Chemistry, University of Karachi, Karachi-75270, Pakistan) Conferols A and B, new anti-inflammatory 4-hydroxyisoflavones from Caragana conferta. Chemical & Pharmaceutical Bulletin v. 57(4): p. 415-417, 2009 (Eng; 15 ref).

Conferols A and B the new 4-hydroxyisoflavones, were isolated from the dichloromethane sub- fraction of the methanolic extract of Caragana conferta (Papilionaceae) along with 3'5'-dihydroxy, 7,4'-dimethoxyisoflavone, E-cinnamic acid tetracosyl 3,4--dihydroxy-E'-cinnamate, docosyl 3,4-dihydroxy-E-cinnamate, beta-sitos-terol, beta-sitostrerol 3-O-beta-D-glucopyranoside, stigmasterol and lupeol. The structures of the new compounds were elucidated through spectroscopic techniques including MS and 2D-NMR. The compounds showed significant antiinflammatory activity in the respiratory burst assay.


2009-05-2377 Kim, M.S.; Park, S.B.; Suk, K.; Kim, I.K.; Kim, S.Y.; Kim, J.A.; Lee, S.H.; Kim, S.H.* (CMRI, IHBR, Department of Pharmacology, School of Medicine, Kyungpook National University; Daegu 700-422, Republic of Korea) Gallotannin isolated from Euphorbia species, 1,2,6-tri-O-galloyl-beta-D-allose, decreases nitric oxide production through inhibition of nuclear factor-kappaB and downstream inducible nitric oxide synthase expression in macrophages. Biological & Pharmaceutical Bulletin v. 32(6): p. 1053-1056, 2009 (Eng; 33 ref).

Gallotannins, plant secondary metabolites are water-soluble polvphenols with wide-ranging biological activities. The inhibitory effects of seven gallotannins isolated from Euphorbia spp (Euphorbiaceae) were examined on the LPS-induced nitric oxide (NO) is well known as a mediator of inflammation. production and underlying mechanisms of action. Among the seven gallotannins, gallotannins and gallotannin 23 significantly reduced LPS-induced NO production in macrophages. Gallotannin 15 and 23 (0.1-10 microg/ml) dose-dependently decreased gene expression and production of iNOS. In addition, gallotannin 15 and 23 (0.1-10 microg/ml) dose-dependently inhibited LPS-induced activation of nuclear factor (NF)-kappaB as indicated by inhibition of degradation of I-kappaBalpha, nuclear translocation of NF-kappaB, and NF-kappaB-dependent gene reporter assay. Results suggest that gallotannins possess an antiinflammatory effect on the LPS-induced inflammation.


2009-05-2378 Koh, E.M.; Kim, H.J.; Kim, S.; Choi, W.H.; Choi, Y.H.; Ryu, S.Y.; Kim, Y.S.; Koh, W.S.; Park, S.Y. (Korea Institute of Toxicology, Daejeon, 305-343 Korea) Modulation of macrophage function by compounds isolated from Zingiber officinale. Planta Medica v. 75(2): p. 148-151, 2009 (Eng; 17 ref).

Bioactivity-guided fractionation of Zingiber officinale (Zingiberaceae) led to isolation of 14 compounds, {4} gingerol (1), {6}-gin gerol (2), {8}-gingerol (3), {10}-gingerol (4), {6}-paradol (5), {4} shogaol (6), {6}-shogaol (7), 1-dehydro-{10}-gingerdione (8) {10}-gingerdione (9), hexahydrocurcumin (10), tetrahydrocurcumin (11), gingerenohe A (12), 1,7-bis-(4' hydroxyl-3' methoxy phenyl)-5-methoxyhepthan-3-one (13), and methoxy-{10}-gingerol (14). Using the RAW 264.7 cell line, the inhibitory effect on nitric oxide production induced by lipopolysaccharide and the stimulatory effects on phagocytosis of these compounds were evaluated. Compounds 7, 8, and 9 significantly decreased lipopolysaccharide-induced nitric oxide production, and compound 7 and 8 significantly reduced inducible nitric oxide syrthase expression. Among them, compound 8 also showed significant stimulatory effects on phagocytosis.


2009-05-2379 Kolios, L.; Selmisch, S.; Daub, F.; Rack, T.; Tezval, M.; Stuermer, K.M.; Stuermer, E.K. (Department of Trauma and Reconstructive Surgery, Georg-August-University of Goettingen, Goettingen, Germany) Equol but not genistein improves early metaphyseal fracture healing in osteoporotic rats. Planta Medica v. 75(5): p. 459-465, 2009 (Eng; 28 ref).

Study was conducted to determine if the soy Glycine max (Leguminosae) metabolite equol and the native isoflavone genistein, in comparison to 17beta-estradiol, improve metaphyseal fracture healing in ovariectomy-induced osteoporotic bone of the rat. Forty-eight 12-week-old female rats developed severe osteoporosis ten weeks after ovariectomy. After metaphyseal tibial osteotomy and standardized stable internal fixation, changes in callus morphology were evaluated in ovariectomized rats (C) and under standardized 17beta-estradiol (E), equol (EQ) and genistein (G) supplemented rats over a period of five weeks. Estrogen and equol were able to improve the elasticity of callus formation significantly in postmenopausal osteoporotic bone. The effects of estrogen were more anabolic than those of equol and were visible in changes to the trabecular bone. However, in terms of the whole body, equol seemed to induce less of an adverse reaction than estrogen. Genistein as an osteoclast inhibitor influenced callus stiffness and negatively impacted trabecular structure in severely osteoporotic bones. The metaphyseal osteotomy model ovariectomized rats allows an accurate study of the therapeutic effects of antiosteoporotic substances on the fracture healing process.


2009-05-2380 Kumar, K.J.S; Wang, S.Y.* (Department of Forestry, National Chung-Hsing University, 250 Kuo-Kuang Road, Taichung 402 Taiwan) Lucidone inhibits iNOS and COX-2 expression in LPS-induced RAW 264.7 murine macrophage cells via NF-kB and MAPKs signaling pathway. Planta Medica v. 75(5): p. 494-500, 2009 (Eng; 20 ref).

The antiinflammatory mechanism of lucidone isolated from the fruits of Lindera erythrocarpa (Lauraceae) was investigated. Data indicated that lucidone significantly inhibits the production of NO and PGE2 autacoids in LPS-induced RAW 264.7 murine macrophage cells. Moreover, it also notably decreased the secretion of tumour necrosis factor-alpha (TNF-alpha). Consistent with these observations, the mRNA and protein expression levels of iNOS and COX-2 were also inhibited by lucidone in a dose-dependent manner. Lucidone also reduced the translocation of NF-kappaB induced by LPS, which is associated with the prevention of the degradation of 1-kappaB, and subsequently decreased p65/p50 protein levels in the nucleus. Lucidone also inhibited NF-kappaB activation by impairing the binding of NF-kappaB to its cis-acting element. In addition, lucidone inhibited JNK and p38MAPKs signals, which are the most significant signals involved in NO, PGE2 and TNF-alpha production; NF-kappaB/AP-1 activation was also inhibited by lucidone. Taken together, the antiinflammatory activity of lucidone might be caused by the inhibition of iNOS and COX-2 expressions through downregulation of NF-kappaB and AP-1 binding.


2009-05-2381 Kundu, R.; Dasgupta, S.; Biswas, A.; Bhattacharya, A.; Pal, B.C.; Bandyopadhyay, D.; Bhattacharya, S.; Bhattacharya, S. (Depepartment of Zoology, School of Life Science, Visva-Bharati (A Central University), Santiniketan 731235, India) Cajanus cajan Linn. (Leguminosae) prevents alcohol-induced rat liver damage and augments cytoprotective function. Journal of Ethnopharmacology v. 118(3): p. 440-447, 2008 (Eng ; 39 ref).

Chronic doses of alcohol (3.7g/ kg) orally administered to rats for 28 days and liver function marker enzymes such as GPT, GOT. ALP and antioxidant enzyme activities were determined. Effect of methanol-aqueous fraction (MAF2) at a dose of 50mg/kg body weight on alcohol treated rats was noted. Alcohol effected significant increase in liver marker enzyme activities and reduced the activities of antiopxidant enzymes. Co-administration of MAF2 reversed the liver damage due to alcohol; it decreased the activities of liver marker enzymes and augmented antioxidant enzyme activities. We also demonstrate significant decrease of the phase II detoxifying enzyme, UDP-glucuronosyl transferase (UGT) activity along with a three- and two-fold decrease of UGT2B gene and protein expression respectively. MAF2 co-administration normalized UGT activity and revived the expression of UGT2B with a concomitant expression and nuclear translocation of Nrf2, a transcription factor that regulates the expression of many cytoprotective genes.


2009-05-2382 Kushima, K.; Iida, K.; Nagaoka, Y.; Kawaratani, Y. ; Sakaguchi, M.; Baba, K.; Hara, Y.; Uesato, S.* (Department of Life Science and Biotechnology, Faculty of Chemistry, Material and Bioengineering, Kansai University, 3-3-35 Yamate-cho, Suita, Osaka 564-8680, Japan) Inhibitory effect of (-)-epigallocatechin and (-)-epigallocatechin gallate against heregulin beta1-induced migration/invasion of the MCF-7 breast carcinoma cell line. Biological & Pharmaceutical Bulletin v 32(5): p. 899-904, 2009 (Eng; 29 ref).

(-)-Epigallocatechin-3-gallate (EGCG) in green tea inhibits the metastasis of some cancer cell lines. Cell migration/invasion assays using Boyden chambers demonstrated that (-)-epigallocatechin (EGC), another green tea catechin, inhibited heregulin-beta1 (HRG)-induced migration/invasion of MCF-7 human breast carcinoma cells to approximately the same extent as EGCG. Assays of cytoskeletal reorganization, Western blotting and immunoprecipitation suggested that EGCG inhibited the migration/invasion by suppressing the HRG-stimulated activation of epidermal growth factor receptor-related protein B2 (ErbB2)/ErbB3/protein kinase B (Akt), whereas EGC did so through pathways including the disruption of the HRG-stimulated activation of ErbB2/ErbB3 but not Akt. EGC, as well as EGCG, could play an important role against the promotion of metastasis of breast cancer cells.


2009-05-2383 Lam, F.F.Y.; Yeung, J.H.K.; Chan, K.M.; Or, P.M.Y. (Department of Pharmacology, Faculty of Medicine, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong SAR, Hong Kong, China) Dihydrotanshinone, a lipophilic component of Salvia miltiorrhiza (danshen), relaxes rat coronary artery by inhibition of calcium channels. Journal of Ethnopharmacology v. 119(2): p. 318-321, 2008 (Eng ; 27 ref).

Dihydrotanshinone is a lipophilic component of the medicinal herb Salvia miltiorrhiza (danshen) belonging to the family of Labiatae. In this study, we have investigated the mechanisms of its relaxant effect on rat-isolated coronary artery. Rat coronary artery rings were precontracted with 1 microM 5-hydroxytryptamine (5-HT). Involvement of endothelium-dependant mechanisms were investigated by pretreatment of the artery rings with a cyclooxygenase inhibitor flurbiprofen (10 microM), a nitric oxide synthase inhibitor NG-nitro-L-arginine methyl ester (L-NAME, 100 (microM), a muscarinic receptor antagonist atropine (100 nM), and by mechanical removal of the endothelium. Involvement of endothelium-independent mechanisms was investigated in endothelium-denuded artery rings pretreated with a beta3-adrenoceptor antagonist pro-pranolol (100 microM), an adenylyl cyclase inhibitor 9-(tetrahydro-2-furanyl)- 9H-purine-6-amine (SQ22536, 100 microM), a guanylyl cyclase inhibitor 1H-1,2,4oxadiazolo4,3-aquinoxalin-1-one (ODQ, 10 microM), and a potassium channel inhibitor tetraethylammonium (TEA, 10 mM). Involvement of Ca2+ channels was investigated in artery rings incubated with Ca2+-free buffer and primed with 1 microM 5-HT for 5 min prior to adding CaCl2 to elicit contraction. Dihydrotanshinone relaxed the 5-HT-precontracted coronary artery rings with an IC50 value of 10.39 plus or minus 1.69 microM. None of the above inhibitors or antagonists tested produced a significant change on the vasorelaxant effect of dihydrotanshinone, except ODQ caused a 50 percent reduction. Pre-incubation of the artery rings for 10 min with dihydrotanshinone (100 microM) abolished the CaCl2-induced vasoconstriction.


2009-05-2384 Lee, Y.H.; Jung, M.G.; Kang, H.B.; Choi, K.C.; Haam, S.; Jun, W.; Kim, Y.J.; Cho, H.Y.; Yoon, H.G. (Department of Food Science and Nutrtion, The University of Suwon, Kyunggi-do 445-743, South Korea) Effect of anti-histone acetyltransferase activity from Rosa rugosa Thunb. (Rosaceae) extracts on androgen receptor-mediated transcriptional regulation . Journal of Ethnopharmacology v. 118(3): p. 412-417, 2008 (Eng ; 27 ref).

For the present study, Rosa rugosa methanol extract (RRME) was obtained from stem part of Rosa rugosa using methanol extraction. Histone acetyltransferase assay were performed to measure the inhibitory effect on acetylation, reporter assay, real-time PCR and ChIP assay were performed to measure androgen receptor-mediated transcriptional regulation, and MTT test were performed to measure cell viability. RRME inhibited both p300 and CBP (60-70 percent at 100 microg/ml) activity. We show RRME mediates agonist-dependent androgen receptor (AR) activation and suppresses antagonist-dependent inhibition. RRME treatment also decreased transcription of AR regulated genes and also reduced histone H3 and AR acetylalion in the promoters of prostate-specific antigen (PSA) and beta-2-microglobuIin (B2M). Finally, RRME treatment reduced the growth of LNCaP, a human prostate cancer cell line. These results demonstrate RRME is a potent HAT inhibitor which reduced AR and histone acetylation leading to decreased AR-mediated transcription and reduced LNCaP cell growth.


2009-05-2385 Lee, S.U.; Shim, K.S.; Ryu, S.Y.; Min, Y.K.; Kim, S.H. (Laboratory of Chemical Genomics, Korea Research Instiute of Chemical Technology, Daejeon, orea) Machilin isolated from Myristica fragrans stimulates osteoblast differentiation. Planta Medica v. 75(2): p. 152-157, 2009 (Eng; 21 ref).

This study evaluated the stimulatory effects of machilin A and structurally related lignans isolated from Myristica fragrans on osteoblast differentiation. In two in vitro osteoblast differentiation models, machilin A stimulated osteoblast differentiation via activation of p38 MAP kinase. Lignans isolated from M. fragrans also stimulated osteoblast differentiation in MC3T3-E1 cells; the lignans included macelignan, machilin F, nectandrin B, safrole, licarin A, licarin B, myristargenol, and meso-dihydroguaiaretic acid. These data suggest that lignans have anabolic activity in bone metabolism.


2009-05-2386 Li, X.; Li, C.; Ji. X.; Song, Z.; Wang, L.; Zhang, J.; Zhang, Y. (The Key Laboratory of Cardiovascular Remodeling and Function Research, Shandong University of Qilu Hospital, 250012 Jinan, Shandong Province, China) Huang-Lian-Jie-Du-Tang inhibits myocardial remodeling in a rat model of metabolic syndrome. Journal of Ethnopharmacology v. 119(2): p. 259-265, 2008 (Eng ; 27 ref).

Huang-Lian-Jie-Du-Tang (HLJDT) is a traditional Chinese herbal medicine and a potential anti-inflammatory agent. HLJDT has been used successfully to treat inflammation in diabetic rats. The current study is aimed to evaluate the effectiveness of HLJDT on myocardial remodeling in a rat model of metabolic syndrome (MS). Twenty-one MS rats were divided into two groups: the MS group and the MS + HLJDT group. Ten Wister rats were a normal control group (NC group). HLJDT (1.04 g/100 g) was orally administered daily for 12 weeks in the MS + HLJDT group. The trial lasted 12 weeks. Changes of echocardiography, histological staining, transmission electron microscope (TEM), and molecular biology examinations were made. After treatment, in the MS + HLJDT group, Masson staining and echocardiography data revealed decreased collagen fibers compared with the MS group. Messenger RNA levels of IL-6, ICAM-1, TNF-alpha, TGF-beta1, NF-kappaB in left ventricular tissues were lower than in the MS group, and volume of mitochondria and the phenotype of cardiac muscle cells in TEM were close to normal. The results suggested that HLJDT reduced myocardial collagen deposition and inhibited cardiac remodeling in a rat model of MS.


2009-05-2387 Li, Y.N.; Wu, Y.L.; Jia, Z.H.; Qi, J.S. ( Biochemistry Dep, Hebei Medical University, Shijiazhuang City 050017, Hebei, PR China) Interaction between COX-2 and iNOS aggravates vascular lesion and antagonistic effect of ginsenoside. Journal of Ethnopharmacology v. 119(2): p. 305-311, 2008 (Eng ; 40 ref).

Ginseng, the root of Panax ginseng (Araliaceae), is one of the most widely used Chinese herbs with hypotensive and cardiotonic actions for thousands of years, but the underlying mechanisms have not been well determined. Ginsenoside, the effective components of ginseng, has antiinflammatory and antioxidative effects. Cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) are key enzymes in inflammation and oxidative stress, respectively, which have close interaction, aggravating their damaging effects. This study investigated whether COX-2 interacted with iNOS in vascular endothelial lesion and the protective effect of ginsenoside. SD male rats were fed with high L-methionine (3 percent, w/w) to induce vascular endothelial lesion, and the rats in ginsenoside group were fed ginsenoside solution (0.8 mg/kg/d). The mRNA expression and protein contents of COX-2 and iNOS were detected by RT-PCR and Western blotting, respectively. The interaction between COX-2 and iNOS was analyzed by co-immunoprecipitation and laser confocal microscopy. The content of NT, a specific marker of peroxynitrite, was evaluated by Western blotting. The morphological changes of vascular endothelium were observed. Compared with control group, the transcription and protein levels of both COX-2 and iNOS increased obviously and their interaction enhanced significantly in model group, in accord with the increased NT content and the pathological alterations of aorta. In ginsenoside group, all these alterations were attenuated significantly (P less than 0.01 or P less than 0.05). It is proved that there exists interaction between COX-2 and iNOS, aggravating endothelial lesion through peroxynitrite and ginsenoside might antagonize their interaction, playing a protective role.


2009-05-2388 Li, H.; Li, S.L.; Gong, L.; Wang, J.L.; Li, Y.Z.; Wu, Z.H. (Department of Integrated Traditional Chinese and Western Medicine, Qilu Hospital of Shandong University, Jinan 250012, Shandong, PR China ) The effects of an herbal medicine Bu-Wang-San on learning and memory of ovariectomized female rat . Journal of Ethnopharmacology v. 117(3): p. 427-432, 2008 (Eng ; 39 ref).

Bu-Wang-San (BWS) is a traditional Chinese herbal medicine for the treatment of learning and memory impairment. The effect of BWS on neuroprortection and how BWS increases CA1 dendritic spine synapse density in menopaused women was investigated in the model of ovariectomized (OVX) rats. BWS consists of Panax ginseng, Acorus gramineus, Poria cocos and Polygala tenuifolia. Sixteen OVX rats were divided into two groups, the OVX group and OVX + BWS group. After 3 months, Morris water maze was used to assess spatial acquisition and spatial retention. Swim time, swim distance, swim speed, quadrant time and platform crossing were recorded. The ultrastructure of the pyramidal cell and spine synapse density were examined by transmission electron microscopy (TEM). In the spatial acquisition and spatial retention phase of testing, BWS group functioned significantly better than control group. Ultrastructurai observation of the hippocampal CA1 region of OVX group showed swelling of mitochondria, the broken and reduced cristas and even crista dissolution; however, the mitochondria were protected well in BWS group. In addition, BWS significantly increased spine synapse density. These results suggested that BWS could improve cognitive ability of menopause-induced learning and memory impairment. The positive effect of BWS on rat learning and memory was associated with increase of spinal synapse density and protection of mitochondrial function of the pyramidal cell in hippocampal CA1 region from menopause-induced injury.


2009-05-2389 Li, H.; Zhang, Y.Y.; Tan, H.W.; Jia, Y.F.; Li, D. (Depepartment of Pharmacology, School of Pharmacy, Fudan University, Shanghai 200032, China) Therapeutic effect of tripterine on adjuvant arthritis in rats. Journal of Ethnopharmacology v. 118(3): p. 479-484, 2008 (Eng ; 19 ref).

Tripterygium wilfordii a perennial vine, is used in traditional Chinese medicine for treatment of rheumatoid arthritis. This study was to determine whether tripterine isolated from Tripterygium wilfordii had therapeutic effects on adjuvant arthritis. Adjuvant arthritis (AA) was induced in rats on day 0. Tripterine 5, 10 and 20 mg kg-1 day-1, or prednisone 10 mg kg-1 day-1 was given to rats intragastrically from day 19 to day 24. Tripterine significantly inhibited paw swelling and bone destruction in AA rats. Serum level of IgG anti-Mycobacterium tuberculosis antibodies and delayed-type hypersensitivity (DTH) induced by Mycobacterium tuberculosis were also decreased by tripterine. The effects of tripterine were associated with decreased interleukin-1beta (IL-1beta) mRNA expression in ankle joint synovial membrane and tumor necrosis factor-alpha (TNF-alpha) mRNA expression in homogenized paws from adjuvant-induced arthritic rats. These findings suggested that tripterine had a therapeutic effect on adjuvant arthritis.


2009-05-2390 Li, X.; Xu, L.; Wu, P.; Xie, H.; Huang, Z.; Ye, W. ; Wei, X. (Key Laboratory of Plant Resources Conservation and Sustainable Utilization, South China Botanical Garden, Chinese) Prenylflavonols from the leaves of Macaranga sampsonii. Chemical & Pharmaceutical Bulletin v. 57(5): p. 495-498, 2009 (Eng; 18 ref).

Four novel prenylflavonols, macaranones A-D , were isolated from the leaves of Macaranga sampsonii (Euphorbiaceae). Their structures were elucidated on the basis of spectroscopic data. Macaranones C and D represent first two examples of flavonols having an unusual peltogynoid skeleton which is formed from a 2'-geranylflavonol by cyclization between 3-OH and C-1" of the 2'-geranyl substituent of the flavpnol. Compounds were evaluated for the cytotoxicity against several human cancer cell lines.


2009-05-2391 Liang, H.; Lai, B.; Yuan, Q. (State Key Laboratory of Chemical Resource Engineering, Beijing University of Chemical Technology, Beijing 100029, China) Sulforaphane induces cell-cycle arrest and apoptosis in cultured human lung adenocarcinoma LTEP-A2 cells and retards growth of LTEP-A2 xenografts in vivo. Journal of Natural Products v. 71(11): p.1911-1914, 2008 (Eng ; 32 ref).

Sulforaphane (1), a glucosinolate-derived isothiocyanate found in the cruciferous vegetable broccoli, is considered an anticarcinogenic component. In the present study, the proliferation and apoptosis induction in human lung adenocarcinoma LTEP-A2 cells by 1 was investigated. Compound 1 caused G2/M-phase arrest (p less than 0.05) and increase of apoptotic cell fraction (p less than 0.05) in a time- and dose-dependent manner. Intraperitoneal injection of 1 significantly inhibited growth of LTEP-A2 xenografts in nude mice, and 9 days after tumor cell implantation with 100 mg/kg intraperitoneal injection of 1, the average tumor weights in 1-treated mice was more than 70 percent lower than that of the control mice.


2009-05-2392 Lin, Q.Y.; Jin, L.J.; Cao, Z.H.; Li, H.Q.; Xu, Y.P. (Depepartment of Bioscience and Biotechnology, Dalian University of Technology, No. 2 Linggong Road, Ganjingzi District, Dalian 116024, People's Republic of China) Protective effect of Acanthopanax senticosus extract against endotoxic shock in mice. Journal of Ethnopharmacology v. 118(3): p. 495-502, 2008 (Eng ; 42 ref).

In this study, we evaluated protective effect of Acanthopanax senticosus syn. Eleutherococcus senticosus extract (ASE) and a possible signaling pathway involved during endotoxic shock induced by intraperitioneal injection lipopolysaccharide (LPS) and D-galactosamine (D-GalN) in BALB/c mice. Mice were intraperitoneal administrated with ASE (100, 200 or 400 mg/kg) prior to injection of 50 microg/kg LPS and 1 g/kg D-CalN. The levels of tumor necrosis-alpha (TNF-alpha) and interleukin-10 (IL-10) in serum and liver. Treatment of mice with ASE prior to LPS/D-GalN injection significantly improved the survival rate. ASE pretreatment inhibited the elevation of TNF-alpha in serum and liver. ASE also decreased iNOS level in liver and the overproduction of nitric oxide (NO) in serum. In addition, IL-10 levels in serum and liver were markedly enhanced. ASE pretreatment inhibited NF-KB activation in liver of mice. Moreover, infiltration of inflammatory cells into the heart, liver and lung of mice was also attenuated by ASE pretreatment. These results suggested that ASE protected mice against LPS/D-GalN-induced endotoxic shock involving inhibition of NF-kB activation, which caused down-regulation of TNF-alpha and involved up-regulation of IL-10. Acanthopanax senticosus may thus prove beneficial in the prevention of endotoxic shock.


2009-05-2393 Lin, A.S.; Lin, C.R.; Du, Y.C.; Lubken, T.; Chiang, M.Y.; Chen, I.H.; Wu, C.C.; Hwang, T.L.; Chen, S.L.; Yen, M.H. (Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung 807, Taiwan) Acasiane A and B and farnesirane A and B, diterpene derivatives from the roots of Acacia farnesiana. Planta Medica v. 75(3): p. 256-261, 2009 (Eng; 18 ref).

Four new diterpenes, acasiane A (1), a acasiane B (2), farnesirane A (3), and farnesirane B (4), along with three known diterpenes (5-7), two titriterpenes (8 and 9), and eight flavonoids (10-17) were isolated from the roots of Acacia farnesiana (Leguminosae). The structures and relative configurations of these compounds were determined by various spectroscopic and X-ray analyses. All isolated compounds were evaluated for in vitro cytotoxic activities against six human cancer cell lines thc MTT method. Betulinic acid (8) displayed moderate cytotoxicity (1.70-5.74 microg/mL) towards five human cancer cell lines and the flavonoids had slight effects. In addition, 8, diosmetin (13), and 3'4'5-trihy-droxy-7-methoxyflavone (15), slightly inhibited superoxide anion generation or elastase release by human neutrophils, indicating moderate antiinflammatory activities.


2009-05-2394 Liu, R.H.; Tang, X.Y.; Dai, D.Z.; Dai, Y. ( Research Div of Pharmacology, China Pharmaceutical Univ, Nanjing 210009, China) Ethanol extracts of Rehmannia complex (Di Huang) containing no Corni fructus improve early diabetic nephropathy by combining suppression on the ET-ROS axis with modulate hypoglycemic effect in rats . Journal of Ethnopharmacology v. 118(3): p. 466-472, 2008 (Eng ; 51 ref).

Liuwei Dihuang (Rehmannia complex, RC) decoction, a classic prescription of Traditional_Chinese, Medicine(TCM), has been used in treating diabetic nephropathy (DN). Among the 6 crude medicines which contains Corni fructus is recognized as the active fraction for its effectiveness. It aimed to investigate, first, if without Corni fructus a modified RC could be still effective, second, if the ethanol extracts could be better than that of water extract and third, the beneficial effect is mainly stemmed from suppressing the endothelin (ET-1) pathway associated with a moderate hypoglycemic effect. Diabetes for 8 weeks was induced by a single dose of streptozotocin (STZ, 65 mg/kg, i.p.) in rats and treated with RC extracts in either 95 percent, 70 percent ethanol or water separately during 5-8th week. The efficacy of extracts was compared with aminoguanidine (AMG). An increase in albumin and creatinine in 24h urine, blood urea nitrogen (BUN) was found in STZ rats. Oxidative stress was found in renal cortex in association with upregulated plasma ET-1 and mRNA of ETA, decreased MMP 2,9 (matrix matelloproteinases) and increased hydroxyproline. The RC without Corni fructus was very effective in alleviating DN and ethanol extracts provided greater effects against water extracts. The efficacy in alleviating DN is attributed to normalizing the activated ET system, oxidative stress and MMP 2,9 in combination with a moderate hypoglycemic activity.


2009-05-2395 Liu, J.F.; Shao, M.; Zhai, D.W.; Liu, K.; Wu, L.J. (School of Traditional Chinese Medicine, Shenyang Pharmaceutical University, Liaoning, P.R. China) Protective effect of 4-methoxy-5-hydroxycanthin-6-one, a natural alkaloid, on dextran sulfate sodium-induced rat colitis. Planta Medica v. 75(2): p. 142-145, 2009 (Eng; 19 ref).

The effect of 4-methoxy-5-hydroxycanthin-6-one (CAN), isolated from Picrasma quassioides (Simarubaceae) on ulcerative colitis induced in rats in comparison with the positive control drug, sulfasalazine (SASP). Given orally for several days, CAN significantly reduced the severity of colitis and mitigated changes in colon length, colon mucosa myeloperoxidase (MPO) activity, and the level of tumour necrosis factor-alpha (TNF-alpha) in serum. The effect of CAN was similar to that of SASP. These results suggest that CAN treatment might be an effective therapeutic intervention against ulcerative colitis.


2009-05-2396 Liu, G.T.; Su, H.M.; Lii, C.K.; Sheen, L.Y ( Department of Nutrition Chung Shan Medical University, No. 110, Sec. 1, Chein Kuo N. Road, Taichung, Taiwan 402, Republic of China) Effect of supplementation with garlic oil on activity of Th1 and Th2 lymphocytes from rats. Planta Medica v. 75(3): p. 205-210, 2009 (Eng; 30 ref).

The effect of supplernentation with garlic (Allum sativum Liliaceae) oil were studied on the activity of Thl and Th2 cells. Rats were administered by gavage with garlic oil (10-200 mg/kg) or corn oil every other day for 2 weeks. Cervical lymph nodes were collected to assay the lymphocyte proliferation rate and the production of Thl in-terleukin 2 (IL-2) and interferon gamma(lFN-gamma) and the Th2 cytokines 1L-4 and IL-10 upon stimulation with concanavalin A. Garlic oil enhanced the lymphocyte proliferation rate accompanied by an elevated production of all four cytokines when given at a dose of 100 mg/kg. At 200 mg/ kg, the production of IL-4 and IL-10 was further enhanced but IFN-gamma production was suppressed. The ratio of FFN-gamma to, IL-4 was enhanced by 50 mg/kg garlic oil but suppressed by 200 mg/kg garlic oil. In conclusion, supplemental garlic oil has a dual effect on Thl-Th2 cell balance: an enhanced T cell response towards the Thl type at low doses and towards the Th2 type at high doses.


2009-05-2397 Luo, P.; Zhang, Z.; Yi, T.; Zhang, H.; Liu, X.; Mo, Z. (West China School of Pharmacy, Sichuan University, No. 17, Section 3, Ren-Min-Nan-Lu Road, Chengdu, Sichuan 610041, China) Anti-inflammatory activity of the extracts and fractions from Erigeron multiradiatus through bioassay-guided procedures. Journal of Ethnopharmacology v. 119(2): p. 232-237, 2008 (Eng ; 17 ref).

In order to isolate and identify the active components of Erigeron multiradiatus for antiinflammatory activity, a preliminary phytochemical study and a bioassay-guided fractionation and purification process was performed. The dry whole plant Erigeron multiradiatus (Compositae) was extracted with 50 percent ethanol and then separated into CHCl3, n-BuOH, and aqueous fractions. The antiinflammatory activities of each fraction were investigated using two in vivo inflammation models. These results exhibited varying degrees of antiinflammatory activities and the n-BuOH fraction showed the strongest antiinflammatory activities. The n-BuOH fraction was then subjected to separation and purification using macroporous resins column chromatography and Sephadex LH-20 leading to two flavonoids glucuronides identified as scutellarein-7-O-beta-glucuronide and apigenin-7-O-beta-glucuronide. Furthermore, LC-MS/MS identification and quantification of isolated compounds were also performed. Scutellarein-7-O-beta-glucuronide and apigenin-7-O-beta-glucuronide were considered as major components and principally responsible for the antiinflammatory activity of Erigeron multiradiatus.


2009-05-2398 Luo, J.; Min, S.; Wei, K.; Cao, J. (Department of Anesthesiology, The First Affiliated Hospital Chongqing Medical University, Chongqing 400016, China) Ion channel mechanism and ingredient bases of Shenfu decoction's cardiac electrophysiological effects . Journal of Ethnopharmacology v. 117(3): p. 439-445, 2008 (Eng ; 30 ref).

Ion channel mechanism of cardiac electrophysiological effects of Shenfu Decoction (SFD, Ginseng Panax (Araliaceae) and Aconiti Praeparatae Aconitum carmichaeli (Ranunculaceae) decoction a traditional Chinese medicine (TCM) prescription, and its ingredient bases were investigated in guinea pigs. After administration of an injection made from SFD (Shenfu Injection, SFI), the indexes of transmembrane action potential (TAP) in vivo and sodium channels in isolated ventricular myocyte were assayed by suspended microelectrodes and patch clamp techniques respectively, and ingredients of SFD were compared with. After administration of SFI, the action potential amplitude (APA) and maximum velocity (Vmax) of TAP decreased. In the presence of either SFI or Fuzi active ingredient (FZAI)(5, 10, and 15 percent), not any other ingredient, the density of voltage-dependent sodium current (INa) decreased significantly, while the inhibition ratio of SFI was larger. EC50 of SFI was less than the one of FZAI, and SFI displayed effects on INa in wider voltage scope than FZAI in current-voltage curve. Both SFI and FZAI shifted the steady-state inactivation curve of sodium channels to the left, and the recovery curve to the right. The results indicated that the cardiac electrophysiological effects of SFI were exerted by blocking sodium channels, and FZAI contributed to such effects most but inferior to SFI, which justified its use in antiarrhythima, myocardial protection, etc..


2009-05-2399 Luo, L.H.; Kim, H.J.; Nguyen, D.H.; Lee, H.B.; Lee, N.H.; Kim, E.K. (Department of Biological Engineering, National Lab of Skin Bioactive Material, Inha University; 253 Yonghyun-dong, Nam-gu, Incheon 402-751, South Korea) Depigmentation of melanocytes by (2Z, 8Z)-matricaria acid methyl ester isolated from Erigeron breviscapus. Biological & Pharmaceutical Bulletin v. 32(6): p. 1091-1094, 2009 (Eng; 32 ref).

To discover an active skin depigmenting agent, a novel inhibitor of melanin biosynthesis from the methanol extract of Erigeron breviscapus (Asteraceae) using a bioactivity-guided fractionation and identified it as (2Z,8Z)-matricaria acid methyl ester by means of spectroscopic analysis. The compound showed strong whitening activity in melan-a cell. Compared with arbutin (IC50=4.0 mM) as a positive control, the depigmentation IC50 value for (2Z,8Z)-matricaria acid methyl ester was 25.4 microM in B16F10 melanoma cell. Moreover, its inhibitory effect on tyrosinase, the key enzyme of melanogenesis, was examined by in vivo and in vitro tyrosinase assay and Western blot. The results indicate that (2Z,8Z)-matricaria acid methyl ester could be useful for treating hyper-pigmentation as skin-whitening agents.


2009-05-2400 Mani, T.T.; Senthil Kumar, R.*; Saravana, M.; nayathulla, ; Rajkapoor, B. (Department of Pharmaceutical Chemistry, Bharathi College of Pharmacy, Bharathinagar-571422, Maddur (Tq), Mandya (Dt), Karnataka, India) Antitumor activity of Pandanus fascicularis Lam. on Dalton's Ascitic lymphoma (DAL) in mice. Hamdard Medicus v. 51(3): p. 27-31, 2008 (Eng; 17 ref).

Antitumour activity of ethanol extract Pandanus fascicularis P. odoratissimus (Pandanaceae) (EPF) was evaluated against Dalton's ascitic lymphoma (DAL) tumour model on dose dependent manner. The activity was assessed using survival time, average increase in body weight haematological parameters and solid tumour volume. Oral administration of EPF increased the survival time and decreased the average body weight of the tumour bearing mice. After 14 days of inoculation. EPF was able to reverse the changes in the haematological parameters, protein and PCV consequent to tumour inoculation. Oral administration of EPF was effective in reducing solid tumour mass development induced by DAL cells. The results showed that EPF possess significant activity in dose dependent manner.


2009-05-2401 Mao, Q.Q.; Ip, S.P.; Tsai, S.H.; Che, C.T. (School of Chinese Medicine, The Chinese University of Hong Kong, Shatin, N.T., Hong Kong) Antidepressant-like effect of peony glycosides in mice. Journal of Ethnopharmacology v. 119(2): p. 272-275, 2008 (Eng ; 24 ref).

The root part of Paeonia lactiflora (Ranunculaceae), known as peony, is often used in Chinese herbal formulae for the treatment of depression-like disorders. Previous studies in our laboratory have shown that an ethanol extract of peony produced antidepressive effects in mouse models of depression. It is well known that peony contains glycosides such as paeoniflorin and albiflorin, yet it remains unclear whether the total glycosides of peony (TCP) are effective. The antidepressant-like effects of TCP was determined by using animal models of depression including forced swim and tail suspension tests. The acting mechanism was explored by determining the effect of TCP on the activities of monoamine oxidases. Intragastric administration of TGP at 80 and 160 mg/kg for seven days caused a significant reduction of immobility time in both forced swim and tail suspension tests, yet TGP did not stimulate locomotor activity in the open-field test. In addition, TGP treatment antagonized reserpine-induced ptosis and inhibited the activities of monoamine oxidases in mouse cerebrum. These results suggest that the antidepressive effects of TGP are mediated, at least in part, by the inhibition of monoamine oxidases.


2009-05-2402 Martin-Herrera, D.; Abdala, S.; Benjumea, D.; Gutierrez-Luis, J. (Unidad de Farmacologia y Farmacognosia, Facultad de Farmacia, Universidad de La Laguna, Tenerife, Islas Canarias, Spain) Diuretic activity of some Withania aristata Ait. fractions . Journal of Ethnopharmacology v. 117(3): p. 496-499, 2008 (Eng ; 30 ref).

We previously reported on the significant dose-dependent diuretic effects produced in laboratory rats by hot water infusions and methanol extracts of Withania aristata where notable increases were observed in the excretion of water and sodium, with an interesting potassium-saving effect. The present study gives the results of the diuretic effects in rats of the hexane, dichloromethane, ethyl acetate, butanol and methanol-water fractions of the previously studied methanol extract. Water excretion rate, pH, density, conductivity and content of Na+, K+ and Cl- were measured in the urine of the rats when subjected to hypersaline conditions. Of the above fractions, the methanol:water extract (100 mg/kg) showed the most interesting diuretic activity (25 percent), which suggested that increase in the polarity of the extracting solvent led to an increase in the concentration of the polar compounds responsible for the diuretic effect. These data, together with previous results on the aqueous and methanol extracts, reaffirm assertions made regarding the effectiveness of the extracts of this plant against urinary pathologies in the Canary Islands folk medicine.


2009-05-2403 Martinez, A.L.; Gonzalez-Trujano, M.E.*; Pellicer, F.; Lopez-Munoz, F.; Navarrete, A. (Instituto Nacional de Psiquiatria Ramon de la Fuente Muniz, Mexico, D.F. Mexico) Antinociceptive effect and GC/MS analysis of Rosmarinus officinalis L. essential oil from its aerial parts. Planta Medica v. 75(5): p. 508-511, 2009 (Eng; 20 ref).

The antinociceptive properties of the essential oil obtained from Rosmarinus officinalis (Lamiaceae) aerial parts were examined using a rat model of arthritic pain. The essential oil (100, 300 and 600 mg/kg, i.p.) produced a dose-dependent antinociceptive effect, manifested as a significant reduction in the dysfunction in the pain-induced functional impairment model in the rat (PIFIR model), mainly at high doses. Chemical constituents of the essential oil were further analyzed by GC/MS. The major compounds in the essential oil were alpha-pinene, camphenen, beta-pinene, myrcene, alpha-phellandrene, eucalyptol, 2-bornanone, camphor, isoborneol, borneol and borneol acetate. The antinociceptive effects of essential oil were tested in combination with 0.12 mg/kg WAY100635, s.c. (an antagonist of 5-HT1A receptors) or 1 mg/kg naloxone, i.p. (an antagonist of endogenous opioids receptors), demonstrating in both cases an inhibition of the antinociceptive response. This study suggests an involvement, at least in part, of the serotonergic system via-5-HT1A receptors and endogenous opioids in the antinociceptive effect of essential oil in the PIFIR model.


2009-05-2404 Mathew, A.J.; Atulya, M.; Joseph, A. (Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, Karnataka, India 576104) Antioxidant and antidiabetic acivity of Mimosa pudica Linn. in streptozotocin induced diabetic rats. Biomed v. 3(2): p. 155-164, 2008 (Eng; 24 ref).

The aqueous extract of Mimosa pudica was found to inhibit the generation of superoxide, hydroxyl radical, lipid peroxidation by Fe 2+/ascorbate system as well as Fe 3+/ascorbate/ADP system and nitric oxide radical in vitro. Concentrations needed for 50 per cent inhibition of these free radicals were 26.3, 156.2, 106.5, 122.1 and 101.2 microg/ml respectively. Administration of M. pudica 100, 500 mg/kg, b.wt. to normal rats increased glucose tolerance significantly (P less than 0.001) from 60 min. M. pudica was also found to reduce serum glucose level in streptozotocin induced diabetic rats significantly (P less than 0.005) at a dose level of 150 mg/kg, b.wt. from 2nd hour. Continued administration (15 days) of the extract 75, 150 mg/kg, body weight produced 41.1 percent and 48.3 percent reduction in the elevated serum glucose level produced by streptozotocin administration. The animals treated with M.pudica extract, the decrease in body weight was completely suppressed as compared with diabetic group. Elevated hepatic and renal enzymes produced by streptozotocin were found to be reduced (P less than 0.001) by M. pudica extract.


2009-05-2405 Matsuda, H.; Asao, Y.; Nakamura, S.; Hamao, M.; Sugimoto, S.; Hongo, M.; Pongipriyadacha, Y.; Yoshikawa, M. (Kyoto Pharmaceutical University, Misasagi, Yamashina-ku, Kyoto 607-8412, Japan) Antidiabetogenic constituents from the Thai traditional medicine Cotylelobium melanoxylon. Chemical & Pharmaceutical Bulletin v. 57(5): p. 487-494, 2009 (Eng; 39 ref).

The methanolic extracts from the wood and bark of Cotylelobium melanoxylon (Dipterocaraceae) were found to inhibit plasma glucose elevation aftec sucrose loading in rats and triglyceride elevation after olive oil loading in mice. A new stilbene dimer, melanoxylin A, together with the known stilbene dimers and a trimer (vaticanol G) and a lignan were isolated from the wood extract, and a new stilbene trimer, melanoxylin B, together with the known stilbene dimers and trimers (voticanols A, E, and G) were isolated from the bark eztract. The main constituents, vaticanols A, E, and/or G, inhibited plasma glucose and triglyceride elevation after sucrose loading in rats and olive oil loading in mice, respectively. In addition, vaticanols A, E, and/or G inhibited the enzyme activities of rat intestinal alpha-glucosidase, porcine pancreatic lipase, and rat lens aldpose reductase.


2009-05-2406 Matsuda, H.; Akaki, J.; Nakamura, S.; Okazaki, Y.; Kojima, H.; Tamesada, M.; Yoshikawa, M. (Kyoto Pharmaceutical University, Misasagi, Yamashina-ku, Kyoto 607-8412, Japan) Apoptosis-inducing effects of sterols from the dried powder of cultured mycelium of Cordyceps sinensis. Chemical & Pharmaceutical Bulletin v. 57(4): p. 411-414, 2009 (Eng; 25 ref).

The methanolic extract and its ethyl acetate-soluble fraction from the dried powder of cultured Cordyceps sinensis mycelium showed cytotoxic effects on promyelocytic leukemia HL-60 cells. Sitosterol (1), 5alpha,8alpha-epidi-oxy-2ZE-ergosta-6,22-dien-3beta-ol (2), 5alpha, 8alpha-epidioxy-22E-ergosta-6,9(11),22-trien-3beta-ol (3), 5alpha,6alpha-epoxy-5alpha-er-gosta-7,22-dien-3beta-ol (4), and ergosterol (5) were isolated from the ethyl acetate fraction. Among the isolated compounds, 2-4 with a peroxide ring or an epoxide ring showed substantial cytotoxic activity with IC50 values of 7.3-7.8 microg/ml, but 1 and 5 showed only moderate activity. Furthermore, apoptosis of HL-60 cells was observed 24 h after treatment with 2-4 (10, 20 microg/ml) using the TdT-mediated dUTP nick-end labeling method, and their apoptosis-inducing activities are suggested to be dependent on the activation of caspases-3/7.


2009-05-2407 Morikawa, T.; Wang, L.B.; Nakamura, S.; Ninomiya, K.; Yokoyama, E.; Mastsuda, H.; Muraoka, O.; Li-Jun, W.; Yoshikawa, M. (Pharmaceutical Research and Technology Institute, Kinki University; 3-4 1 Kowakae, Higashi-osaka, Osaka 577-8502, Japan) Medicinal flowers. XXVII.1) New flavanone and chalcone glycosides, arenariumosides I, II, III, and IV, and tumor necrosis factor-alfa inhibitors from everlasting, flowers of Helichrysun arenarium. Chemical & Pharmaceutical Bulletin v. 57(4): p. 361-367, 2009 (Eng; 70 ref).

The methanolic extract from the flowers of Helichrysum arenarium (Asteraceae) was found to show inhibitory effect on tumour necrosis factor-alpha (TNF-alpha, 1 ng/ml)-induced cytotoxicity in L929 cells. From the methanolic extract, 50 constituents including four new flavanone and chalcone glycosides named arenariumosides I, II, III, and IV were isolated. The stereostructures of I-IV were elucidated on the basis of chemical and physicochemical evidence. Among the constituents, naringenin 7-O-beta-D-glucopyranoside, apigenin 7-O-beta-D-glucopyranoside, apigenin 7-O-gentiobioside and apigenin 7,4'-di-O-beta-D-glucopyranoside significantly inhibited TNF-alpha-induced cytotoxicity in L929 cells at 30 microM.


2009-05-2408 Muthu, A.K.; Sethupathy, S.; Manavalan, R.; Karar, P.K. (Department of Pharmacy, annamalai University, Annamalai Nagar 608002, TN, India) Isolation of flavonoids from Dolichos biflorus Linn. and evaluation of their antilipidemic activity in rabbits fed with high fat diet. Hamdard Medicus v. 51(3): p. 108-114, 2008 (Eng; 19 ref).

Flavonoids from Dolichos biflorus (Leguninosae) were isolated and screened for antilipidemic activity on rabbits fed with high fat diet (HFD). Methanolic extract was fractionated with hexane, chloroform ethyl acetate and methanol. Ethyl acetate fration which showed maximum flavonoid yield, was fractionated and estimatd for flavonoids (total phenol) content. High fat diet rabbits showed significantly increased level of plasma and tissue total cholesterol, triglyceride, free fatty acids, phospholipids, plasma LDL cholesterol and decreased level of plasma HDL cholesterol. Administration of isolated flavonoids high fat diet rabbits showed near to normal (control) level of the above lipid profiles in plasma and tissues. Hence it is concluded that flavonoids possessed antilipidemic activity in high fat diet fed rabbits.


2009-05-2409 Nadasi, E.; Prantner, I.; David, T.; Ember, I. ( Department of Public Health and Preventive Medicine, Faculty of Medicine, University of Pecs, H-7624 Pecs, Szigeti ut 12. Hungary) Effect of a plant-originated natural compound CODTM extract, on C-MYC, HA-RAS and P53 gene experession in short-term animal experiments. Acta Alimentaria v. 37(1): p. 87-92, 2008 (Eng; 15 ref).

Several plant-originated natural compounds were shown to exhibit chemopreventive effect in carcinogenesis. COD(TM) extract, a complex plant extract made from several tropical plants with possible cancer preventive effect was investigated in animal expenments. Ha-ras, c-mye and p53 gene expressions were investigated 24, 48 and 72 h after COD(TM) extract and dimethylbenz(a)-anthracene (DMBA) treatment in CBA/Ca(H-2K) mice. COD(TM) extract administered together with DMBA diminished c-myc, p53 and Ha-ras gene expressions both in the 24 and 48 h experiments, but not in the 72 h experiment.


2009-05-2410 Nagarajan, K.; Shafeeq, K.A.M.M.; Mazumder, A.; Ghosh, L.K.; Jha, S.; Suriya Prabha, K.; Sakthivel, M. (Periyar College of Pharmaceutical Sciences for Girls, K. Sathanoor Main Road, Trichy-620021, TN, India) Hepatoprotective effect of ethanol extract from leaves of Phyllanthus emblica in rats. Hamdard Medicus v. 51(3): p. 87-91, 2008 (Eng; 18 ref).

The antioxidant activity of ethanol extract from the leaves of Phyllanthus emblica (Euphorbiaceae) was evaluated by various biochemical marker parameters, including super oxide dismutase (SOD - anion radical scavenging), catalase (CAT - hydrogen peroxide scavnging). glutathione peroxidase (GPX), glutathione reductase (GRD - reducing power) glutathione transferase (GTS) and thio-barbituric acid reactive substances (TBARS) measurement. Hepato cellular damage was induced by administration of CCl4 (ip) in male albino Sprague-Dawley strain rats. The reduced levels of marker parameters attained normal level, after administration of ethanolic extract except GTS. The increased concentration of TBARS with CCI4 treated rats attains normal level after administration of ethanolic extract of the same plant. An antioxidant property appears to be predominantly responsible for the hepatoprotective action of the drug.


2009-05-2411 Nahata, A.; Patil, U.K.; Dixit, V.K. (Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Vishwavidyalaya, Sagar, M.P. ) Effect of Convolvulus pluricaulis Choisy. on learning behaviour and memory enhancement activity in rodents. Natural Product Research v. 22(16): p. 1472-1482, 2008 (Eng; 19 ref).

The present study was undertaken to investigate the effects of Convolvulus pluricaulis (CP), syn; Convolvulus microphyllus (Convolvulaceae) considered as Shankhpushpi on 1earning and memory in rodents. Nootropic activity using Cook and Weidley's Pole Climbing Apparatus, passive avoidance paradigms and active avoidance tests were used to test learning and memory. The ethanolic extract of CP and its ethyl acetate and aqueous fractions were evaluated for their memory enhancing properties. Two doses (100 and 200 mgkg-1 p.o.) of the ethanolic extract and ethyl acetate and aqueous fractions were administered in separate groups of animals. Both the doses of all the extracts of CP significantly improved learning and memory in rats. Furthermore, these doses significantly reversed the amnesia induced by scopolamine (0.3 mgkg-1 i.p.). Nootropic activity was compared using piracetam as the standard. Moreover, CP has exhibited potent memory-enhancing effects in the step-down and shuttle-box avoidance paradigms. Further studies are necessitated to identify the exact mechanism of action.


2009-05-2412 Nasu, Y.; Iwashita, M.; Saito, M.; Fushiya, S.; Nakahata, N. (Department of Cellular Signaling, Graduate School of Pharmaceutical Sciences, Tohoku University; Aoba 6-3, Aramaki, Aoba-ku, Sendai 980-8578, Japan) Inhibitory effects of Atractylodis Lanceae Rhizoma and Poria on collagen- or thromboxane A2-induced aggregation in rabbit platelets. Biological & Pharmaceutical Bulletin v 32(5): p. 856-860, 2009 (Eng; 26 ref).

The effect of Kampo medicines were studied on platelet aggregation using rabbit platelets in vitro. Collagen and U46619, a thromboxane A2 receptor agonist, caused rabbit platelet aggregation, which was potently inhibited by pretreatment of platelets with Kami-shoyo-san and Toki-shakuyaku-san in vitro. Toki-shigyaku-ka-goshuyu-shokyo-to, however, did not significantly inhibit collagen- or U46619-induced platelet aggregation. Therefore, the effect on platelet aggregation of two herbal medicines, Atrractylodis Lanceae Rhizoma and Poria were examined both of which are contained in Kami-shoyo-san and Toki-shakuyaku-san but not in Toki- shigyaku-ka- goshuyu-shokyo-to. As the results indicate, Atractylodis Lanceae Rhizoma inhibited platelet aggregation by collagen but not by U46619. Poria effectively inhibited U46619-induced platelet aggregation and it partially inhibited collagen-induced platelet aggregation. On the other hand, Atractylodis Lanceae Rhizoma and Poria did not inhibit adrenaline/adenosine diphosphate- or adrenaline/serotonin-induced platelet aggregation. These results suggest the possibility that the inhibition of platelet aggregation by two medicines, is one of the mechanisms underlying the improvement of Hiesho. Furthermore, Atractylodis Lanceae Rhizoma and Poria are possible herbal medicines for inhibition of platelet aggregation.


2009-05-2413 Ngarivhume, T.; Dzomba, P.; Gwizangwe, I.; Zendera, C.H.; Katsvanga, C.A.T.; Jimu, L.; Moyo, M.; Chagonda, T. ( Chemistry Department, Walter Sisulu University, Mthatha, South Africa) Anaesthetic effects of Adenia gummifera distillates on Apis mellifera (Honeybee). Natural Product Research v. 22(15): p. 1370-1378, 2008 (Eng; 22 ref).

The anaesthetic activities of steam distillates of Adenia gummifera stem on Apis mellifera were evaluated by a diffusion method. Live, direct and fractional (61-80 degreeC fraction) distillates had greater anaesthetic effect while vacuum distillates were mild. The anaesthetic activity significantly increased with concentration up to 6 percent (v/v), and then it levelled off, while excessive exposure was lethal. The number of bees in a given volume had no significant effect on anaesthetic activity but container volume (Fcal = 66.4; F 3,8 = 4.07) and bee-distillate distance (fcal = 31.0; F2,6 = 5.14) did, suggesting the rate of diffusion of active component could be the determining factor. The active component is likely to contain amines and the rest halogenated alkane.


2009-05-2414 Nguelefack-Mbuyo, P.E.; Nguelefack, T.B.; Dongmo, A.B.; Afkir, S.; Azebaze, A.G.B.; Dimo, T.; Legssyer, A.; Kamanyi, A. ; Ziyyat, A. (Depepartment of Animal Biology and Physiology, Laboratory of Animal Physiology, University of Yaounde I, BP 812 Yaounde, Cameroon) Anti-hypertensive effects of the methanol/methylene chloride stem bark extract of Mammea africana in L-NAME-induced hypertensive rats . Journal of Ethnopharmacology v. 117(3): p. 446-450, 2008 (Eng ; 26 ref).

The methanol/methylene chloride (CH3OH/CH2Cl2) extract from the stem bark of Mammea africana was showed to possess vasodilating effect in the presence and the absence of N-omega-nitro-L-arginine methyl ester (L-NAME). The present study was designed to evaluate the effects of the methanol/methylene chloride from the stem bark of Mammea africana. The extract (200 mg/(kgday)) was administered orally in rats treated concurrently with L-NAME (40 mg/(kgday)). L-Arginine (100 mg/(kgday)) and captopril (20 mg/(kg day))were used as positive controls. Bodyweight, systolic arterial blood pressure and heart rate were measured weekly throughout the experiment period (28 days). At the end of treatment, animals were killed and the cardiac mass index evaluated. The aorta was used to evaluate the endothelium-dependant relaxation to carbachol. The aorta contraction induced by noradrenalin was also examined and expressed as a percentage of that induced by KCl. The extract neither affected the body weight nor the heart rate. The extract as captopril completely prevented the development of arterial hypertension. Both the substances failed to restore the endothelium-dependent vascular relaxation and increased the vascular contraction to norepinephrine in relation to KC1 contraction. They also significantly reduced the left ventricular hypertrophy induced by L-NAME. These findings are in agreement with the traditional use of Mammea africana in the treatment of arterial hypertension and indicate that it may have a beneficial effect in patients with NO deficiency but will be unable to improve their endothelium-dependent vasorelaxation.


2009-05-2415 Nugroho, A.E.; Ikawa, Z.; ardiiman, ; Maeyama, K.* (Department of Pharmacology, Informational Biomedicine, Ehime University Graduate School of Medicine; Shitsukawa, Toon, Ehime 791-0295, Japan) Effects of benzylidenecyclopentanone analogues of curcumin on histamine release from mast cells. Biological & Pharmaceutical Bulletin v 32(5): p. 842-849, 2009 (Eng; 40 ref).

Curcumin a constitutent from the rhizomes of the plant Curcuma longa (Zingiberaceae) and its fourteen analogues were studied for their effects on histamine release from rat basophilic leukemia (RBL-2H3) cells. After screening, four slected compounds were studied for their concentration-dependent effects on histamine release and Ca ion uptake. In RBL-2H3 cells and rat peritoneal mast cells stimulated with antigen or compound 48/80, respectively, the methoxy-hydroxy analogue was more potent than curcumin in inhibiting histamine release. In contrast, the inhibitory effects of methyl/ethyl analogues were less potent than those of curcumin. Moreover, these compounds abrogated histamine release induced by increased intracellular Ca ions concentrations in response to stimulants such as thapsigargin and ionomycin. These compounds also showed potent inhibitory effects on 45Ca ions uptake in RBL-2H3 cells. The mechanism of the inhibitory effects of these curcumin analogues on histamine release appeared to be related to blockade of Ca ions signaling events. These results provide useful information to guide the development of new synthetic compounds for the treatment of allergic and inflammatory diseases related to histamine or mast cells.


2009-05-2416 Olsen, H.T.; Stafford, G.I.; van Staden, J.; Christensen, S.B.; Jager, A.K. (Depepartment of Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Denmark) Isolation of the MAO-inhibitor naringenin from Mentha aquatica L. . Journal of Ethnopharmacology v. 117(3): p. 500-502, 2008 (Eng ; 20 ref).

To isolate the compound(s) responsible for the MAO-inhibitory activity. Six extracts of varying polarity of Mentha aquatica were tested in a photometric peroxidase linked MAO bioassay. The 70 percent ethanol extract had highest inhibitory activity. (S)-Naringenin was isolated from the extract by bioassay guided fractionation on VLC and preparative TLC. The structure of the compound was determined by 1H, 13C and 13C-DEPT NMR and optical rotation. The IC50 values for MAO inhibition by naringenin were 342 plus or minus 33 microM for the rat liver mitochondrial fraction, 955 plus or minus 129 microM for MAO-A and 288 plus or minus 18 microM for MAO-B. The content of naringenin in Mentha aquatica might explain its use in traditional medicine for depression-like conditions.


2009-05-2417 Palacios-Espinosa, F.; Deciga-Campos, M.; Mata, R. (Departament de Farmacia, Facultad de Quimico, Universidad Nacional Autonoma de Mexico, Mexico, D.F. 04510, Mexico) Antinociceptive, hypoglycemic and spasmolytic effects of Brickellia veronicifolia . Journal of Ethnopharmacology v. 118(3): p. 448-454, 2008 (Eng ; 32 ref).

In order to complete the preclinical pharmacological profile of Brickellia veronicifolia (Asteraceae) first the antinociceptive effect of an organic extract (BVE) and isolated metabolites on the hot plate and writhing tests was assessed. Then, their potential hypoglycemic effects were analyzed in normoglycemic and diabetic rats; in addition, an oral glucose tolerance test (OGTT) was performed. Finally, the spasmolytic activity of BVE was assessed in vivo using the gastrointestinal motility test (GMT) in mice. The results revealed that BVE (100-600 mg/kg), 6-methoxysalicylic acid (1), 2-methoxybenzoic acid (2), benzyl-2,6-dimethoxybenzoate (3), and taraxasteryl acetate (4) showed significant analgesic effects. Compounds 2 and 3 were the most active (1-100 mg/kg) in the hot plate and writhing tests, respectively. In the antidiabetic assays, BVE (100 mg/kg) showed an important hypoglycemic action. Furthermore, at the same dose, it provoked a significant postprandial decrease of blood glucose level after 30 min of a glucose challenge. Finally, the GMT in mice revealed the spasmolytic activity in vivo of BVE (31.6 mg/kg).


2009-05-2418 Pasi, S.; Aligiannis, N.; Paratsinis, H.; Skaltsounis, A.L.; Chinou, I.B. (Department of Pharmacognosy and Natural Products Chemistry, School of Pharmacy, University of Athens, Athens, Greece) Biologically active triterpenoids from Cephalaria ambrosioides. Planta Medica v. 75(2): p. 163-167, 2009 (Eng; 22 ref).

The roots of Cephalaria ambrosioides (Dipsacaceae) yielded a new triterpene, 6alpha-hydroxyhederagenic acid (1), in addition to the known triterpene hederagenic acid (2) and four corresponding saponins, leontoside A (or akeboside Stb) (3), kalopanax saponin A (or alpha-hederin) (4), saponin PG (or sapindoside B) (5), and dipsacoside B (6). Their structures were elucidated on the basis of their spectral data (MS, 1D and 2D NMR) and by some chemical transformations. The extract and all isolated compounds were evaluated for their antimicrobial, molluscicidal and in vitro cytotoxic activities. All compounds showed strong antimicrobial activity (MIC values 1.80 - 2.50 microg/mL), with 5 and 6 exhibiting, activities comparable to those of standard antibiotics. Moreover, compounds 3-5 were active against all assayed cancer cell lines, whereas compounds 3 and 4 exhibited higher activities against Biomphalaria glabrata snails, with MIC of 5.4 and 6.2 microg/mL, respectively.


2009-05-2419 Prabhakar, T.; Nagarathna, P.K.M.; Ramesh, K.; Rao, S.T. (Karnataka College of Pharmacy, Thirumenahalli, Hegde Nagar, Main Road, Bangalore-560064) Effect of root extracts on anti-inflammatory activity of Sida cordifolia (Linn). in rats. Biomed v. 2(1): p. 95-98, 2007 (Eng; 15 ref).

The antiinflammatory activity of chloroform, methanol and aqueous extracts of Sida cordifolia(Malvaceae) was carried out using the technique of carrageenan induced paw edema in albino rats. The aqueous extract showed maximum antiinflammatory effect among the tested extracts when compared with control group. Diclofenac sodium (100 mg/kg) was used as reference standard in the present study.


2009-05-2420 Pyo, J.S.; Roh, S.H.; Kim, D.K.; Lee, J.G.; Lee, Y.Y.; Hong, S.S.; Kwon, S.W.; Park, J.H. (College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul, Korea) Anti-cancer effect of betulin on a human lung cancer cell line: A pharmacoproteomic approach using 2 D SDS PAGE coupled with nano-HPLC tandem mass spectrometry. Planta Medica v. 75(2): p. 127-131, 2009 (Eng; 14 ref).

In order to identify the molecular players involved in betulin-induced apoptosis, cellular proteins were applied to two-dimensional sodium dodecyl sulfate polyacrylamide gel electro-phoresis (2 D SDS PAGE) for differential proteomic analysis. As a result, four downregulated proteins and three upregulated proteins were identified by nano-HPLC MS/MS. The four downregulated proteins were poly(rC)-binding protein 1, iso-form 1 of 3-hydroxyacyl-CoA dehydrogenase type 2, heat shock protein 90-alpha 2, and enoyl-CoA hydratase; the three upregulated proteins were aconitate hydratase, malate dehydrogenase, and splicing factor arginine/serine-rich 1. These differentially expressed proteins explained the cytotoxicity of betulin against human lung cancer A549 cells, and the proteomic approach was thus shown to be a potential tool for understanding the pharmacological activities of pharmacophores. Betulin is a representative compounds of Betula platyphylla (Betulaceae).


2009-05-2421 Qi, Q.; You, Q.; Gu, H.; Zhao, L.; Liu, W.; Lu, N. ; Guo, Q. (Jiangsu Key Laboratory of Carcinogenesis and Intervention, China Pharmaceutical University, 24 Tong Jia Xiang Nanjing, Jiangsu 210009, China) Studies on the toxicity of gambogic acid in rats . Journal of Ethnopharmacology v. 117(3): p. 433-438, 2008 (Eng ; 23 ref).

To study the chronic toxicity of gambogic acid (GA). the major active ingredient of gamboges, a brownish to orange resin extracted from the Garcinia hanburyi (Guttiferae) in Southeast Asia, using Sprague-Dawley rat as an animal model and provide further theoretical support for clinical applications of this promising natural anticancer agent. GA was administered orally at dosages of 120, 60 and 30 mg/kg once every other day for a total of 13 weeks. Then we carried out the chronic toxicity studies including general body parameters, hematological, serum biochemistry, histopathological, and viscera examination. The results from the studies demonstrated that rats treated with high dose (120 mg/kg) of GA for a long time can lead to the damage on the kidney and liver. An innocuous dose was established to be 60 mg/kg after administration to rats for a total of 13 weeks at a frequency of one administration every other day. This dose was approximately 18.0 (body weight) or 9.6 (body surface area) times higher then that of the dose (200 mg/60 kg, every other day) used for human trials. The studies demonstrated that the toxicity targets in the rats were the kidney and liver. These results provide further theoretical support for clinical applications of this promising natural anticancer agent.


2009-05-2422 Raj, K.; Misra, N.; Pachauri, G.; Sharma, M.; Tamrakar, A.K.; Singh, A.B.; Srivastava, A.K.; Kiran, K.P.; Rao, C.V.N.; Prubhu, S.R. (Medicinal & Process Chemistry division, Central Drug Research Institute, Lucknow, UP, India) Novel class of hybrid natural products as antidiabetic agents. Natural Product Research v. 23(1): p. 60-69, 2009 (Eng; 22 ref).

A number of O-alkylated xanthone, carbazoles and coumarins have been synthesised and screened for their in vitro antidiabetic activity, such as glucose-6-phosphatase, glycogen phosphorylase and alpha glucosidase inhibitors. Compounds which were showing significant percentage inhibition were also tested for in vivo antihyperglycemic activity in sucrose loaded normal and streptozotocin (STZ)- induced diabetic rats. These compounds show 22.1, 24.4 and 26.7 percent and 20.8, 25.0, 20.5 percent lowering in sucrose loaded normal rats and STZ-induced diabetic rats at a dose of 100 mg kg-1.


2009-05-2423 Ratnasooriya, W.D.; Fernando, T.S.P. (Depepartment of Zoology, University of Colombo, Colombo 03, Sri Lanka) Effect of black tea brew of Camellia sinensis on sexual competence of male rats . Journal of Ethnopharmacology v. 118(3): p. 373-377, 2008 (Eng ; 33 ref).

In Sri Lankan traditional medicine black tea brew (BTB) of Camellia sinensis (Theaceae) is claimed to have male sexual stimulant activity. As this claim is not scientifically tested and proven, this study was undertaken to evaluate the effects of BTB on male sexual competence. Different doses of BTB made from Sri Lankan high grown dust grade no 1 tea (84, 167 and 501 mg/ml) or water were orally administered to separate groups of rats (n = 9 per group) and 3 h later their sexual behaviour were monitored (for 15 min) using receptive females. The overall results showed that BTB possesses marked aphrodisiac activity (in terms of prolongation of latency of ejaculation shortening of mount- and intromission latencies and elevation of serum testosterone level). The aphrodisiac action had a rapid onset and appears to be mediated via inhibition of anxiety and elevation of serum testosterone level. Further, this aphrodisiac action was not associated with impairment of other sexual parameters like libido, sexual motivation, sexual arousal, sexual vigour or penile erection. BTB was also nontoxic (in terms of overt signs, liver and renal toxicity). It is concluded that BTB can function as a quick acting, safe, oral aphrodisiac which may also be useful in certain forms of sexual inadequacies such as premature ejaculation and impaired libido and other sexual functions.


2009-05-2424 Ren, Y.; Shen, L.; Zhang, D.W.; Dai, S.J. (School of Pharmaceutical Science, Yantai University; Yantai 264005, People's Republic of China) Two new sesquiterpenoids from Solanum lyratum with cytotoxic activities. Chemical & Pharmaceutical Bulletin v. 57(4): p. 408-410, 2009 (Eng; 11 ref).

Two new sesquiterpenoids, lyratol C and lyratol D, together with two known sesquiterpenoids, dehydrovomifoliol and blumenol A were isolated from the whole plant of Solanum lyratum (Schisandraceae). Their structures were established by spectroscopic analyses. In vitro the four compounds showed significant cytotoxic activities against three human cancer cell lines, namely, HONE-1 nasopharyngeal, KB oral epidermoid carcinoma, and HT29 colorectal carcinoma cells, and gave IC50 values in the range 3.7-8.1 microM.


2009-05-2425 Rhiouani, H.; El-Hillaly, J.; Israili, Z.H.; Lyoussi, B. (Laboratory of Physiology-Pharmacology and Environmental Health, Depepartment of Biology, Faculty of Sciences, Dhar El Mehraz, Fez, Morocco) Acute and sub-chronic toxicity of an aqueous extract of the leaves of Herniaria glabra in rodents . Journal of Ethnopharmacology v. 118(3): p. 378-386, 2008 (Eng ; 42 ref).

In the acute study in mice, the crude aqueous extract of HG plant caused dose-dependent general behavior adverse effects and mortality. The no-observed adverse effect levels (NOAEL) of the HG extract was 5 g/kg and the lowest-observed adverse effect levels (LOAEL) was 5.5 g/kg. Mortality increased with increasing doses: the calculated LD50 was 8.50 plus or minus 0.42 g/kg in mice. In the sub-chronic study in rats, daily oral administration of the crude HG extract for up to 90 days resulted in a significant attenuation of the normal increase in the body weight. At the highest dose, the HG-extract caused a significant increase in erythrocytes, leukocytes (WBC), platelets, and eosinophils, but it had no effect on the differential WBC counts (lymphocytes, monocytes, neutrophils and basophils). Only at the highest dose, the HG-extract caused a significant increase in serum levels of the liver enzymes, alanine aminotransferase and aspartate aminotransferase, as well as serum creatinine, indicating toxic effect of the high dose of the extract on the liver and kidney. The organ toxicity was confirmed by histopathological examination, which showed centrolobular sinusoidal congestion, disruption of the central vein and hepatocellular necrosis in the liver, and interstitial and intraglomerular congestion, tubular atrophy, and inflammation in the kidney. This study also revealed the hypoglycemic activity of the HG-extract in normoglycemic rats. The suppression of the normal weight gain and the hypoglycemic action of HG-extract should be investigated further for possible therapeutic implications. Because of the relatively high NOAEL values in the acute study in mice, and lack of mortality or clinically significant changes in the biological (except for hypoglycemia) and hematological parameters in rats after 90 days of daily dosing, it may be concluded that the HG extract does not appear to have significant toxicity (except at high doses). In view of the doses consumed empirically in traditional medicine in Morocco, there is a wide margin of safety for the therapeutic use of Herniaria glabra.


2009-05-2426 Roome, T.; Dar, A.; Ali, S.; Naqvi, S.; Choudhary, M.I. (Pharmacology Section, H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan) A study on antioxidant, free radical scavenging, anti-inflammatory and hepatoprotective actions of Aegiceras corniculatum (stem) extracts. Journal of Ethnopharmacology v. 118(3): p. 514-521, 2008 (Eng ; 33 ref).

The n-hexane, ethyl acetate and methanol extracts, derived from Aegiceras corniculatum (Aegicerataceae) stems, scavenged superoxide anions and hydroxyl radicals in nitro blue tetrazolium reduction and deoxyribose degradation assays, respectively. All the extracts inhibited the process of lipid peroxidation at its initiation step. Additionally, in rat liver microsomes n-hexane and ethyl acetate extracts also caused termination of radical chain reaction supporting their scavenging action towards lipid peroxy radicals. Moreover, increased production of O2- in human neutrophils, stimulated by phorbol-12-myristate-13-acetate (PMA) and/or opsonized zymosan were also suppressed (IC50 approx 3-20 microg/mL). Thereby, revealing the ability of plant extracts to antagonize the oxidative stress via interference with NADPH oxidase metabolic pathway. These in vitro results coincide with the reduction in the glucose oxidase-induced paw edema in mice in the presence of ethyl acetate and methanol extracts (10, 50, and 100 mg/kg, i.p.). Plant extracts (250, 500 and 1000 mg/kg p.o.) also significantly protected the carbon tetrachloride (CC14)-induced oxidative tissue injury in rat liver. This was reflected by a approx 60 percent decline in the levels of serum aminotransferase enzymes. Aegiceras corniculatum extracts found to possess pronounced antioxidant effect that may be at least in part related to its antiinflammatory and hepatoprotective activities.


2009-05-2427 Roseghini, R.; Falcao, G.M.; Costa, J.F.O.; Clarencio, J.; Nascimen, H.; Velozo, E.; Schaer, R.; Vale, V.; Costa, S.L.; Costa, M.F.D., et al. (Instituo de Ciencias da Saude, Av, Reitor Miguel Calmon S/N Vale do Canela CEP; 40 110-100 Salvador Bahia Brazil) The flavonoid rutin but not the alkaloid arborinine induces apoptosis in a B-cell hybridoma cell line. Planta Medica v. 75(5): p. 488-493, 2009 (Eng; 30 ref).

The effects of arborinine, an alkaloid extracted from Erthela bahiensis (Rutaceae) and of rutin, a flavonoid obtainecl from Dimorphandra mollis (Leguminosae) were studied on the viability and function of a murine B-cell hybridoma as a tumour model. The flavonoid rutin at 50 microM induced an increase in the number of apoptotic cells of one- to five fold and reduction in cellular proliferation and monoclorral antibody production. Less but still significant necrosis also induced by rutin under the same experiemental conditions. On the other hand, the alkaloid bornine exerted no significant effects on the studied parameters.


2009-05-2428 Roy, B.; Karki, R.; Venkatesh, D.P. (Acharya and B.M. Reddy College of Pharmacy, Soldevanahalli, Bangalore-560090) Formulation and evaluation of rapid dissolving tablets of diclofenac sodium for the treatment of arthritis. Biomed v. 3(2): p. 165-174, 2008 (Eng; 11 ref).

Formulation of rapidly dissolving tablets using different amount of sublimating agents were prepared by the technique of sublimation in order to obtain new formulation containing diclofenac sodium for arthritis disease treatment. Eight different formulation of rapidy dissolving tablets of diclofenace sodium were prepared, which contain camphor and ammonium bicarbonate in various combinations. Tablets were prepared by direct compression method and physiochemical parameters were evaluated. All the formulation gave the satisfactory result in terms of physicochemical property, wetting time disintegration time and dissolution time. The best rapidly dissolving tablet performance and best in vitro drug release profile was achieved by using camphor at 10 percent concentration. The chosen tablet containing 25 mg of diclofenac sodium released drug within 10 min to achieve the desired therapeutic concentration.


2009-05-2429 Sharma, N.; Passey, C.; Sharma, Y. (Department of Pharmacognosy and Phytochemistry, DISPAR, Pushp Vihar, Sector-3, New Delhi-110017, India) Toxic or tonic unexploited and emerging potential of Nerium species. Hamdard Medicus v. 51(3): p. 171-175, 2008 (Eng; 23 ref).

Nerium oleander and other Nerium species such as N. indicum and N. odorum (Apocynaceae) popularly known for their toxic effects have been recently shown to be beneficial in ailments other than congestive heart failure for which these were previously utilized. Their neuroprotective action can be exploited to find a possible remedy for neurodegenerative disorders like Alzheimer's disease. The present article deals with the pharmaognostic study, pharmacology and potential of the plant as a future remedy for neurodegradation.


2009-05-2430 Sheng, R.; Gu, Z.J.; Xie, M.J.; Zhou, W.X.; Guo, C. (Suzhou Institute of Chinese Materia Medica and Department of Pharmacology, Medical School of Suzhou University, Suzhou, P.R. China) EGCG inhibits proliferation of cardiac fibroblasts in rats with cardiac hypertrophy. Planta Medica v. 75(2): p. 113-120, 2009 (Eng; 35 ref).

Epigallocatechin gallate (EGCG) at doses of 25, 50 and 100 mg/kg was administered to rats with cardiac hypetrophy intragastrically for 6 weeks. The results showed that EGCG at 25-100 mg/kg dose-dependently reduced heart weight indices, decreased atrial natriuretic polypeptide and endothelin levels in plasma, but increased nitrite (the oxidative product of NO) levels in the serum and in the myocardium. EGCG also reduced the hydroxyproline concentration and decreased the proliferating cell nuclear antigen expression in the hypertrophic myocardium. EGCG remarkably inhibited pressure overload-induced c-myc increase in Western blot analysis. In cultured newborn rat cardiac fibroblasts, treatment with EGCG at 12.5-200 mg/L for 6-48 h decreased cell proliferation induced by serum. EGCG at 12.5-100 mg/L dose-dependently inhibited cell proliferation and DNA synthesis of fibroblasts induced by angiotensin II (Ang II) at 1 micromol/L. EGCG also significantly increased nitrite levels in culture medium, and up-regulated inducible nitric oxide synthase protein expression if compared with the Ang II group. The inhibitory effect of EGCG on cell proliferation induced by Ang II was partly blocked by pretreatment with N omega-nitro-L-arginine methyl ester hydrochloride. These results suggest that EGCG inhibits the proliferation of cardiac fibroblasts both in vivo and in vitro thereby preventing myocardial fibrosis in cardiac hypertrophy.


2009-05-2431 Shi, Y.; Sun, J.; He, H.; Guo, H.; Zhang, S. ( College of Food Sience and Technology Huazhong Agricultural University, Wuhan 430070, People's Republic of China) Hepatoprotective effects of Ganoderma lucidum peptides against D-galactosamine-induced liver injury in mice . Journal of Ethnopharmacology v. 117(3): p. 415-419, 2008 (Eng ; 27 ref).

Ganoderma lucidum (GL), a traditional Chinese medicinal mushroom, has been widely used for the treatment of chronic hepatopathy of various etiologies. The hepatoprotective activity of peptides from Ganoderma lucidum GLP) was evaluated against D-galactosamine (D-GalN)-induced hepatic injury in mice. GLP was administered via gavage daily for 2 weeks at doses of 60, 120 and 180 mg/kg, respectively. Control groups were given the same amount of physiological saline synchronously. Then the mice from D-GalN control and GLP-treated groups were treated with D-GalN (750 mg/kg) suspended in normal saline by intraperitoneal injection. D-GalN-induced hepatic damage was manifested by a significant increase in the activities of marker enzymes (AST, ALT) in serum and MDA level in liver, and by a significant decrease in activity of SOD and GSH level in liver. Pretreatment of mice with GLP reversed these altered parameters to normal values. The biochemical results were supplemented by histopathological examination of liver sections. The best hepatoprotective effects of GLP were observed after treatment with the dose of 180 mg/kg as it was evidenced from biochemical parameters and liver histopathological characters which were similar to those of normal control group. Results of this study revealed that GLP could afford a significant protection in the alleviation of D-GalN-induced hepatocellular injury.


2009-05-2432 Shields, M.; Niazi, U.; Badal, S.; Yee, T.; Sutcliffe, M.J.; Delgoda, R. (Natural Products Institute, Faculty of Pure and Applied Sciences, University of the West Indies, Jamaica, West Indies) Inhibition of CYP1A1 by quassinoids found in Picrasma excelsa. Planta Medica v. 75(2): p. 137-141, 2009 (Eng; 15 ref).

Properties of infusions of the plant Picrasma excelsa (Simaroubaceae) were examined against a panel of cytochrome P450 (CYP) enzymes, which are primarily responsible for the metabolism of a majority of drugs on the market. The two major ingredients, quassin and neoquassin, were isolated and used for further characterization. Inhibition of the activities of heterologously expressed CYP microsomes was monitored, and the most potent inhibition was found to be against CYP1A1, with 1C50 values of 9.2 microM and 11.9 microM for quassin and neoquassin, respectively. The moderate inhibition against the CYP1A1 isoform by quassin and neoquassin displayed partial competitive inhibition kinetics, inhibition constants (Ki) of 10.8 plus or minus 1.6 microM, for quassin and competitive inhibition kinetics, with a Ki of 11.3 plus or minus 0.9 microM, for neoquassin. Two inhibitors were docked into the active site of a model of CYP1A1, which provided insight at the atomic level into the structure-activity relationship of quassinoids with respect to CYP isoform known to be an activator of carcinogens, thus providing a basis for the search for more potent inhibitors of CYP1A1 that may have implications in chemoprotection.


2009-05-2433 Shih, C.D.; Kuo, D.H.; Huang, C.W.; Gu, Y.H.; Chen, F.A. (Department of Pharmacy and Graduate Institute of Pharmaceutical Technology, Tajen University, 20 Weishin Road, Yanpu Township, Pingtung County 90741, Taiwan, ROC) Autonomic nervous system mediates the cardiovascular effects of Rhodiola sacra radix in rats. Journal of Ethnopharmacology v. 119(2): p. 284-290, 2008 (Eng ; 37 ref).

The aim of this study was to evaluate the cardiovascular activity of water- Soluble fraction (WtF) and n-butanol-soluble fraction (BtF) of Rhodiola sacra (Crassulaceae) radix and to explore its mechanism of action in propofol anesthetized Sprague-Dawley rats. The changes of blood pressure, heart rate and cardiac contractility after systemic administration of the extracts (10-75 mg/kg) were examined for at least 40 min. Different antagonists were used to evaluate the mechanisms of cardiovascular effects of the extracts. Intravenous injection of the WtF (10, 25, 35, 50 or 75 mg/kg) exhibited dose-dependent hypotension and increases in heart rate and cardiac contractility. In contrast, mild alterations in the same cardiovascular parameters were detected only at high dose (75 mg/kg) BtF. The WtF-induced hypotensive, positive inotropic and chronotropic effects were significantly abolished by pretreatment with hexamethonium (30 mg/kg, i.v.) or reserpine (5 mg/kg, i.v.), whereas the hypotensive, but not the positive inotropic or chronotropic effect was potentiated by captopril (2.5 mg/kg, i.v.). Pretreatment with methylatropine (1 mg/kg, i.v.), on the other hand, reversed the positive inotropic and chronotropic but not the hypotensive effects of WtF. The WtF-induced cardiovascular responses were not affected in rats pretreated with NG-nitro-L-arginine methyl ester (20 mg/kg. i.v.). We conclude that systemic administration of the WtF of Rhodiola sacra radix elicited a potent hypotensive effect that was mediated by the withdrawal of sympathetic vasomotor tone and interaction with the circulatory angiotensin system. The positive inotropic and chronotropic effects of WtF may result from a direct vagal inhibition on the heart.


2009-05-2434 Shu, H.; Hayashida, M.; Arita, H.; Huang, W.; Xiao, L.; Chiba, S.; Sekiyama, H.; Hanaoka, K. (Department of Anesthesiology, First Affiliated Hospital of Sun Yat-Sen University, 58, Zhongshan 2nd Road, Guangzhou 510080, PR China) High doses of processed aconiti tuber inhibit the acute but potentiate the chronic antinociception of morphine. Journal of Ethnopharmacology v. 119(2): p. 276-283, 2008 (Eng ; 37 ref).

It investigated the effects of processed Aconiti tuber (PAT) obtained from tuber of Aconitum carmichaeli (Ranunculaceae) an oriental herbal medicine, at analgesic doses on acute morphine antinociception in morphine-naive mice and morphine tolerance in morphine-tolerant mice. In acute experiments, mice received subcutaneous (s.c.) morphine (2, 5, or lO mg/kg) and oral distilled water or PAT (0.3, 1.0, or 3.0 g/kg). The mechanical nociceptive threshold (MNT) and thermal nociceptive latency (TNL) were measured with the tail pressure test and tail flick test, respectively, before, and at 30, 60,90, and 120 min after s.c. morphine injection. In chronic experiments, mice received s.c. morphine 10 mg/kg) and oral distilled water or PAT (0.3, 1.0, or 3.0 g/kg) once daily for 11 days. MNT was measured before, and at 60 min after, and TNL was measured before, and at 30 min after, daily morphine injections on days 1-11. PAT at analgesic doses inhibited the acute antinociceptive effect of morphine dose-dependently in morphine-naive mice. In contrast, PAT at analgesic doses potentiated the chronic antinociceptive effect of morphine dose-dependently by inhibiting the development of morphine tolerance dose-dependently. These effects of PAT on acute and chronic morphine antinociception were mediated through activation of kappa-opioid receptors. These results indicated that chronic co-administration of PAT at analgesic doses with morphine could provide better-maintained morphine analgesia in a long term morphine treatment after initial inhibition of acute morphine antinociception for a brief period of time.


2009-05-2435 Sohn, S.H.; Chung, H.S.; Ko, E.; Jeong, H.J.; Kim, S.H.; Jeong, J.H.; Kim, Y.; Shin, M.; Hong, M.; Bae, H.* (Department of Physiology, College of Oriental Medicine, Kyung Hee University; Seoul 130-701, Republic of Korea) The genome-wide expression profile of Nelumbinis semen on lipopolysaccharide-stimulated BV-2 microglial cells. Biological & Pharmaceutical Bulletin v. 32(6): p. 1012-1020, 2009 (Eng; 37 ref).

Effects of Nelumbinis semen (NS) were determined by analyzing nitric oxide production and proinflammatory cytokines using enzyme-linked immunosorbent assay. The mechanism was evaluated in BV-2 cells with or without NS treated with LPS for various lengths of time using oligonucleotide microarray and real time reverse transcription-polymerase chain reaction. The oligonucleotide microarray analysis revealed that mitogen activated protein kinase (MARK) signaling pathway-related genes were down-regulated in LPS activated BV-2 cells by pretreatment with NS. In addition, significant decreases in Noslap gene expression were observed with NS pretreatment. Cluster linked pathway analysis using the Kyoto Encyclopedia of Genes and Genomes database revealed that the effects of NS were closely associated with the regulation of mitochondrial functions. These results suggested that NS can affect the MAPK signaling pathway and mitochondria functions in BV-2 cells activated with LPS.


2009-05-2436 Sousa, P.J.C.; Arauja, J.S.; Pereira, L.L.S.; Modro, M.N.R.; Maia, J.G.S.; Araujo, M.T.F.; Carvalho, J.C.T.; Perazzo*, F.F. (Laboratorio de Pesquisa em Farmacos, Universidade Federal do Amapa, Rod. JK, km 02, CEP 68902-303, Macapa, Amapa, Brazil) Phytochemical and toxicological evaluations of the essential oil from the bark of Aniba canellila (H.B.K.) Mez.. Journal of Essential Oil Research v. 21(4): p. 381-384, 2009 ( Eng; 26 ref).

The essential oil of Aniba canellila (Lauraceae) extracted from the bark (OEAC) yielded 1.0 percent and the major constituents were 1-nitro-2-phenylethane and methyl eugenol, both identified by GC/MS and GC-FID. The observed LD 50 (oral) was 720 plus minus 66.4 mg/kg. The doses used in the subacute toxicity study (1/10 and 1/20 of the LD 50) were administered in rats for 30 days, and the biochemical parameters were observed. The results suggested that the oil presented low toxicity in rats in the used dosages.


2009-05-2437 Suh, K.S.; Choi, E.M.; Kwon, M.; Chon, S.; Oh, S.; Woo, J.T.; Kim, S.W.; Kim, Y.S. (Department of Endocrinology and Metabolism, Kyung Hee University School of Medicine, Hoegi-dong, Dongdaemun-gu, Seoul 130-701, Republic of Korea) Kaempferol attenuates 2-deoxy-D-ribose-induced oxidative cell damage in MC3T3-E1 osteoblastic cells. Biological & Pharmaceutical Bulletin v. 32(4): p. 746-749, 2009 (Eng; 25 ref).

Kaempferol; a natural flavonoid, was investigated to determine whether it could influence dRib-inductd cellular dysfunction and oxidative cell damage in the MC3T3-E1 mouse osteoblastic cell line. Osteoblastic cells were treated with 30 mM dRib in the presence or absence of kaempferol and markers of osteoblast function and lipid peroxidation were subsequently examined. Kaempferol (10 -9 -10 -5 M) significantly inhibited the dRib-induced decrease in growth of MC3T3-E1 osteoblastic cells. In addition, treatment with kaempferol resulted in a significant elevation of alkaline phosphatase (ALP) activity, collagen content, and mineralization in the cells. Treatment with kaempferol increased osteoprotegerin secretion and decreased malondialdehyde contents of MC3T3-E1 osteoblastic cells in the presence of 30 mM dRib. Results suggest that kaempferol inhibits dRib-induced osteoblastic cell damage and may be useful for the treatment of diabetes-related bone diseases.


2009-05-2438 Sun, H.X.; Peng, X.Y. (College of Animal Sciences, Zhejiang University, Kaixuan Road 268, Hangzhou 310029, Zhejiang, China) Protective effect of triterpenoid fractions from the rhizomes of Astilbe chinensis on cyclophosphamide-induced toxicity in tumor-bearing mice. Journal of Ethnopharmacology v. 119(2): p. 312-317, 2008 (Eng ; 25 ref).

The objectives of this study were to investigate the protective effect of the triterpenoid fractions from the rhizomes of Astilbe chinensis (Saxifragaceae) (ATF) on cyclophosphamide (CTX)-induced toxicity in tumor-bearing mice. The mice inoculated with mouse sarcoma S180 cells were treated with saline or CTX alone, or co-treated with CTX and ATF. The blood, femur bone, and serum samples were collected for determination of the haematological and biochemical parameters and splenocytes were for assay of proliferation, the activity of natural killer (NK) cells, and production of interleukin-2 (IL-2). ATF significantly increased the peripheral white blood cell (WBC) count and bone marrow cellularity (BMC) in CTX-treated S180-bearing mice. Increase of aspartate transanimase (AST), alanine transaminase (ALT), urea nitrogen (BUN), and creatinine in the serum of CTX-treated mice was significantly reversed by ATF. The lowered levels of splenocytes proliferation, NK cells activity, and IL-2 production from splenocytes in S180-bearing mice after CTX treatment were also increased by ATF administration. ATF provides significant protection against CTX-induced hematotoxicity, hepatotoxicity, nephrotoxicity, and immunotoxicity, and might be helpful in abrogation of CTX-induced toxicity during the chemotherapy.


2009-05-2439 Tamrakar, A.K.; Yadav, P.P.; Tiwari, P.; Maurya, R.; Srivastava, A.K. (Division of Biochemistry, Central Drug Research Institute, Lucknow-226001, ) Identification of pongamol and karanjin as lead compounds with antihyperglycemic activity from Pongamia pinnata fruits . Journal of Ethnopharmacology v. 118(3): p. 435-439, 2008 (Eng ; 23 ref).

Streptozotocin-induced diabetic rats and hyperglycemic, hyperlipidemic and hyperinsulinemic db/db mice were used to investigate the antihyperglycemic activity of pongamol and karangin isolated from the fruits of Pongamia pinnata. In streptozotocin-induced diabetic rats, single dose treatment of pongamol and karanjin lowered the blood glucose level by 12.8 percent (p less than 0.05) and 11.7 percent (p less than 0.05) at 50 mg/kg dose and 22.0 percent (p less than 0.01) and 20.7 percent (p less than 0.01) at 100 mg/kg dose, respectively after 6 h post-oral administration. The compounds also significantly lowered blood glucose level in db/db mice with percent activity of 35.7 (p less than 0.01) and 30.6 (p less than 0.01), respectively at 100 mg/kg dose after consecutive treatment for 10 days. The compounds were observed to exert a significant inhibitory effect on enzyme protein tyrosine phosphatase-1 B (EC 3.1.3.48). The results showed that pongamol and karangin isolated from the fruits of Ponngamia pinnata possesses significant antihyperglycemic activity in Streptozotocin-induced diabetic rats and type 2 diabetic db/db mice and protein tyrosine phosphatase-1 B may be the possible target for their activity.


2009-05-2440 Tan, Y.X.; Yan, R.Y.; Wang, H.Q.; Chen, R.Y.; Yu, D.Q. (Institute of Materia Medica Chinese Academy of Medical, Sciences & Peaking Union, Medical College, No.1 Xian Nong Tan Street, Xuan Wu District, Beijing 100050, People's Republic of China) Wittiorumins A-F, antioxidant diels-alder-type adducts from Morus wittiorum. Planta Medica v. 75(3): p. 349-255, 2009 (Eng; 9 ref).

Six new Diels-Alder-type adducts wittiorumins A-F (1-6) along with the three known compounds chalcomoracin, mulberrofuran J, and mongolicin F, were isolaed from the stem bark of Morus wittiorum (Moraceae). Their structures including their absolute configurations were determined on the basis of spectroscopic analysis and chemical methods. Some of the isolated compounds were assayed for their antioxidant activities, among which compounds 1-3 were active as antioxidants, with inhibitory ratios of 73.0 percent, 82.0 percent, and 82.0 percent respectvely, at a concentration of 10 -5 M.


2009-05-2441 Tang, H.; Min, G.; Ge, B.; Li, Y.; Liu, X.; Jiang, S. (Key Laboratory for Natural Medicine of Gansu Province, Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences, Lanzhou 730000, PR China) Evaluation of protective effects of Chi-Zhi-Huang decoction on phase I drug metabolism of liver injured rats by cocktail probe drugs . Journal of Ethnopharmacology v. 117(3): p. 420-426, 2008 (Eng ; 28 ref).

Chi-Zhi-Huang decoction (PGR) is one of the traditional Chinese medicine (TCM) preparations with unique effect on withdrawing jaundice and has been used to treat icteric patients in China for many years. In this research, we aim at to evaluate the potential activity of PGR in restoring hepatic drug metabolism in a damaged liver. A cocktail approach with caffeine (10 mg/kg), dapsone (10 mg/kg) and chlorzoxazone (20 mg/kg) respectively as probe drug of cytochrome P450 (CYP) isoform of CYP 1A2, 3A4 and 2E1 was used to evaluate its possible effects on Phase 1 oxidative metabolism. Pretreated with three dosages of PGR water extract (0.75, 1.5 and 3 g/kg, po) for 5 days, male Wistar rats (220-240 g) were intoxicated by phenylisothiocyanate (PITC, 100 mg/kg, po) 24 h before probes intravenous injection. The pharmacokinetics of the probes in the blood was determined simultaneously by HPLC, and their non-compartmental parameters were used to evaluate the metabolic difference among the groups. Moreover, the levels of liver enzymes (ALT, AST, ALP) and bilirubins were also measured for insight of liver function. The findings in this study suggest that PGR induces CYP 3A4, does not have much effect on CYP 2E1, and inhibits CYP 1A2 at high dosage. The current pharmacokinetic approach allowed the protective effects of PGR on oxidative drug metabolism in damaged liver to be systemically examined and will certainly help in the explanation of synergistic effect of the composites formula.


2009-05-2442 Tatiya, A.U.; Surana, S.S.; Sonara, G.B.; Surana, S.J. (Department of Pharmacognosy, R.C. Patel College of Pharmacy, Shirpur-425405, Dist. Dhule, Maharastra) Antihistaminic and hypotensive activity of steam bark of Machilus macrantha. Biomed v. 3(2): p. 175-181, 2008 (Eng; 17 ref).

The Objective of this study was screening of various extracts of Machilus macrantha(Lauraceae) bark for their possible antihistaminic and parasympatholytic activity. The preliminary phytochemical study of bark of Machilus macrantha revealed that the presence of alkaloid, tannins, steroid and mucilage. Results of pharmacological screening indicate that all extracts of Machilus macrantha bark showed dose dependent inhibitory activity against contraction induced by ach and histamine on isolated goat tracheal chain compared with the standard drugs like chlorpheniramine maleate and atropine. Chloroform and total alkaloid fraction at dose (10-40 mg/ml) of bark showed significant antihistaminic and parasympatholytic activity and prominent hypotensive activity at 1-4 microg/ml compared to the standard minoxidil (vasodilator). Results obtained from pharmacological screening thus indicate that the bark may find its utility in treating asthma and hypertension.


2009-05-2443 Temkitthawon, P.; Viyoch, J.; Limpeanchob, N.; Pongamornkul, W.; Sirikul, C.; Kumpila, A.; Suwanborirux, K.; Ingkaninan, K. (Department of Pharmaceutical Chemistry and Pharmacognosy, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok 65000, Thailand) Screening for phosphodiesterase inhibitory activity of Thai medicinal plants. Journal of Ethnopharmacology v. 119(2): p. 214-217, 2008 (Eng ; 11 ref).

Phosphodiesterases (PDEs) are a group of enzymes that have powerful effects on cellular signaling because they regulate the second messenger, cAMP or cGMP. PDE inhibitors have been used for treatment of many indications such as cardiovascular diseases, chronic obstructive pulmonary diseases, erectile dysfunction and pulmonary hypertension. The aim of the study was to search for sources of PDE inhibitors from Thai biodiversity. Some Thai medicinal plants used as aphrodisiac and neurotonic agents together with plants from Leguminosae collected from the North of Thailand were screened for PDE inhibitory activity using a radioassay. Seven from nineteen aphrodisiac and neurotonic plants as well as three from twelve Leguminosae plants showed potent PDEs inhibitory activity. The concentrations that could inhibit 50 percent PDE activity (IC50) of the active extracts were determined in comparison to the standard inhibitor, 3-isobutyl-1-methylxanthine (IBMX). Betula alnoides, Hiptage benghalensis, Leea indica and Senna surrattensis showed IC50 values in the range of microgram per milliliter while IBMX standard showed an IC50 value of 0.68 plus or minus 0.13 microg/ml.


2009-05-2444 Tian, J.; Yang, X.; Di, Y.; Ma, Y.; Li, L.; Li, L. ; He, H.; Hao, X. (State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, P.R. China) Antioxidant lignans from Mananthes patentiflora. Planta Medica v. 75(5): p. 534-537, 2009 (Eng; 10 ref).

A new tetrahydrofuranoketone lignan (1) and two new tetrahydrofuranoketone lignan glycosides (2, 3) were isolated from the ethanol extract of the aerial part of Mananthes patentiflora (Acanthaceae). The structure elucidations of these compounds were mainly established on the basis of 1D; 2D NMR and HR-mass spectroscopic analysis. All three compounds revealed potent antioxidant activities within the concentration range tested (0.08-50.0 microM) against H2O2 induced impairment in PC12 cells.


2009-05-2445 Tsai, H.H.; chen, I.J.; Lo, Y.C. (Depepartment of Pharmacology College of Medicine, Kaohsiung Medical University, Kaohsiung 807, Taiwan) Effects of San-Huang-Xie-Xin-Tang on U46619-induced increase in pulmonary arterial blood pressure . Journal of Ethnopharmacology v. 117(3): p. 457-462, 2008 (Eng ; 44 ref).

San-Huang-Xie-Xin-Tang (SHXT), composed of Coptidis rhizoma, Scutellariae radix and Rhei rhizoma, is traditionally used to treat hypertension. Our aim was to investigate the pharmacology effect of SHXT on a thromboxane A2 analogue U46619-induced increase in pulmonary hypertension and protein expression in primary pulmonary smooth muscle cells (PASMCs). Arterial blood pressure and isometric tension in the aorta and pulmonary artery of rats were measured by pressure and force transducers, respectively. Protein expressions on PASMCs were detected by Western blotting. SHXT significantly attenuated U46619-induced increase in arterial blood pressure. The inhibitory effect of SHXT on pulmonary arterial pressure was greater than systemic arterial pressure in U46619 treated rats. Similarly, the inhibitory effect of SHXT on U46619-induced vasoconstriction in rat pulmonary arterial rings was greater than that in aortic rings. In U46619 treated PASMCs, SHXT down-regulated expression of phosphodiesterase type 5 (PDE5), Rho-kinase (ROCK) IL, cyclooxygenase-2 (COX-2) and up-regulated expression of soluble guanylyl cyclase (sGC) alpha1, and sGCbeta1. SHXT attenuated U46619-induced increase in systemic and pulmonary arterial blood pressure. Inhibition of PDE5, ROCK-I1, COX-2 and stimulation of sGC may play important roles in the cardiovascular effects of SHXT.


2009-05-2446 Tsujimoto, M.; Horie, M.; Honda, H.; Takara, K.; Nishiguchi, K. (Department of Clinical Pharmacy, Faculty of Pharmaceutical Sciences, Kyoto Pharmaceutical University; 5 Nakauchicho, Misasagi, Yamashina-ku, Kyoto 607-8414, Japan) The structure-activity correlation on the inhibitory effects of flavonids on cytochrome P450 3A activity. Biological & Pharmaceutical Bulletin v. 32(4): p. 671-676, 2009 (Eng).

The inhibitory potentials on cytochrome P450 (CYP) 3A activity of 23 flavonoids were studied using human liver microsomes, and tried to identify the molecular features that cause the inhibition of CYP3A. The activity of testosterone 6beta3-hydroxylate was evaluated to quantify GYPSA activity. Quantification Theory I was analyzed in which extreme values of the inhibitory effects of CYP3A activity were tested with flavonoids supplied at a level of 10 microM. The inhibitory effects ranged widely from 1.5 microM to more than 100 microM for the half maximal inhibitory concentration. Because the inhibitory effects were only weakly correlated with the pKa, value, the inhibitory effects could not be accounted for by the molecular characteristics of the flavonoids. On the other hand flavones with the basal structure and hy-droxylation at positions 7 and 4' showed significantly increased inhibitory effects on CYP3A activity. In addition, the hydroxylation of position 2' and 3', methoxylation of position 4', and the isoflavone basal structure significantly decreased the inhibitory effects on CYP3A activity. In conclusion, the basal structure and the substituents of flavonoids are important in the inhibitory effects of flavonoids on CYP3A activity.


2009-05-2447 Tu, J.; Sun, H.X.; Ye, Y.P. (College of Animal Sciences, Zhejiang University, Kaixuan Road 268, Hangzhou, Zhejiang 310029, China) Immunomodulatory and antitumor activity of triterpenoid fractions from the rhizomes of Astilbe chinensis. Journal of Ethnopharmacology v. 119(2): p. 266-271, 2008 (Eng ; 30 ref).

The mice inoculated with mouse tumor cell lines were treated per os with ATF at the doses of 20,40,60 mg/kg for 10 days. The effects of ATF on the growth of transplantable tumor, splenocyte proliferation, the activity of natural killer (NK) cells, and production of interleukin-2 (IL-2) from splenocytes in tumor-bearing mice were measured. Meanwhile, the effects of ATF on 2,4-dinitrofluorobenzene (DNFB)-induced delayed type hypersensitivity (DTH) reaction and the sheep red blood cell (SRBC)-induced antibody response in naive mice were also studied. ATF could not only significantly inhibit the growth of mice transplantable tumor, but also remarkably increase splenocytes proliferation, NK cells activity, and the level of IL-2 secreted by splenocytes in tumor-bearing mice, promote the DTH reaction and enhance anti-SRBC antibody level in nai've mice, which indicated that the ATF could improve both specific and non-specific cellular and humoral immune response. The antitumor activity of ATF might be achieved by improving immune response, and ATF could act as antitumor agent with immunomodulatory activity.


2009-05-2448 Twardowschy, A.; Freitas, C.S.; Baggio, C.H.; Mayer, B.; dos Santos, A.C.; Pizzolatti, M.G.; Zacarias, A.A.; dos Santos, E.P.; Otuki, M.F.; Marques, M.C.A. (Depepartment of Pharmacology, Universidade Federal do Parana, PR, Brazil) Antiulcerogenic activity of bark extract of Tabebuia avellanedae, Lorentz ex Griseb. Journal of Ethnopharmacology v. 118(3): p. 455-459, 2008 (Eng ; 26 ref).

Tabebuia avellanedae is commonly used for the treatment of peptic ulcers. This study was carried out with the ethanolic extract of bark from Tabebuia avellanedae (EET) (30-1000 mg/kg) to determine its gastroprotective activity and to clarify the pathways involved in this effect. Acute gastric ulceration in rats was produced by oral administration of ethanol and ibuprofen. After ethanol administration, the gastric wall mucus was examined. Chronic gastric ulceration was produced by injection of acetic acid in rat gastric subserosa. Anti-secretory studies were undertaken using Shay rat pylorus ligature technique and measurement of enzymatic activity of H+, K+-ATPase in vitro. Administration of EET p.o. or i.p. significantly inhibited gastric mucosa damage induced by ethanol and ibuprofen. The antiulcer effect was further confirmed by enhanced gastric mucus production. In pylorus ligature rats, EET significantly reduced the basal gastric acid secretion and total acidity; moreover, it inhibited the increase in total acidity induced by histamine. In addition, EET reduced the activity of H+, K+, ATPase. The results obtained in the present pharmacological assay indicate that this plant has a protective action against gastric lesions, involving the maintenance of protective factors, such as mucus and prostaglandin, besides the reduction of gastric total acidity.


2009-05-2449 Wahab, A.; Ahmed, E.; Nawaz, S.A.; Sharif, A.; Haq, R.U.; Malik, A.; Choudhary, M.I.; Raza, M. (Institute of Neurophysiology, Charite-Universitatsmedizin Berlin, Berlin, Germany) A pharmacological and toxicological evaluation of Haloxylon recurvum. Natural Product Research v. 22(15): p. 1317-1326, 2008 (Eng; 29 ref).

Haloxylon recurvum (Chenopodiaceae) is distributed chiefly from the Mediterranean region to Central and South Asia and traditionally applied externally for a variety of disorders. It investigated the in vivo toxic potential of crude methanolic extract of the whole plant and its n-hexane, chloroform, butanol, ethylacetate and aqueous soluble fractions by determining their acute toxicity and acute neurotoxicity in mice using Lorke's method and inverted screen test. In vitro studies were also conducted in order to investigate its antilipoxygenase, antibacterial and antifungal activities. All the fractions showed a narrow margin of safety in mice, except the aqueous fraction, which did not produce any mortality even at the highest tested dose (5000 mg kg-1). At non-lethal doses, only the aqueous fraction (TD50 1264 mgkg-1) was found to produce neurotoxicity in mice. In in vitro lipoxygenase inhibition assay, the ethylacetate fraction showed the most significant inhibitory activity. Crude methanolic extract and its butanol soluble fraction showed the most potent antifungal and antibacterial activity for all the materials tested. Thus, this report verifies the traditionally reported toxicity of this plant, as the majority of its components have exhibited a narrow margin of safety, however, they have been found active in in vitro studies, therefore, further studies are required in order to isolate the most active toxic compounds and differentiate them from these fractions.


2009-05-2450 Wan, A.K.S.; Leung, S.W.S.; Zhu, D.Y ; Man, R.Y.K. (Department of Pharmacology, Li Ka Shing Faculty of Medicine, The University of Hong Kong, 2/F Faculty of Medicine Building, 21 Sassoon Road, Hong Kong SAR, China) Vascular effects of different lipophilic components of "Danshen", a tradional chinese medicine, in the isolated porcine oronary artery. Journal of Natural Products v. 71(11): p.1825-1828, 2008 (Eng ; 24 ref).

"Danshen" has been used for the treatment of various cardiovascular diseases in the People's Republic of China for many years. Two different forms of "Danshen" exist, whith the roots of Salvia miltiorrhiza (Labiatae) being the traditional form and the roots of Salvia przewalskii being a surrogate used in the western areas of mainland China. The most abundant lipophilic diterpene quinones present in S. miltiorrhiza} and S. przewalskii roots, tanshinone IIA(1) and cryptotanshinone (2), inhibited contraction of the isolated procine coronary artery to the thromboxane A2 analogue, U46619. Przewaquinone A (3), a lipophilic diterpene quinone present only in S. przewalskii induced a similar but greater inhibitory action on vascular contraction than 1 and 2. This effect of 3 was endothelium-independent and reversible. The present results suggest that 3 is more potent than 1 and 2 and may contribute to a great extent to the ability of S. przewalskii roots to inhibit vascular contractions.


2009-05-2451 Wang, G.Y.; Lv, Q.H.; Dong, Q; Xu, R.Z.; Dong, Q.H. (Department of Surgery, Sir Run Run Shaw Hospital, School of Medicine, Zhejiang University, Hangzhou, China) Berbamine induces fas-mediated apoptosis in human hepatocellular carcinoma HepG2 cells and inhibits its tumor growth in nude mice. Journal of Asian Natural Products Research v. 11(3-4): p. 219-228, 2009 (Eng; 19 ref).

Berbamine, a natural compound from ihe plant Berberis amurensis is a traditional Chinese medicine mainly used in stimulating normal hematopoiesis in clinic. Our previous studies demonstrated that berbamine has antileukemia activity. In this study, we investigated the anticancer activity of berbamine against human hepatocellular carcinoma (HCC) HepG2 cells in vitro and in vivo. Berbamine treatment decreased the cell growth in a dose-dependent manner with an IC50 value of 34.5 plus or minus 0.5 microM. Flow cytometric analysis of apoptosis using Annexin V/propidium iodide staining showed that the percentage of apoptotic cells was increased in a time-dependent manner. Berbamine treatment increased the expression level of Fas and P53, caused depolarization of mitochondrial membrane and decrease of membrane potential, and activated caspase-3, -8, and -9 in HepG2 cells. Berbamine-induced apoptosis could be blocked by the broad caspase inhibitor z-VAD-fmk. HepG2 human HCC xenograft mice treated with berbamine showed a significant reduction in tumor growth rates compared to saline-treated mice. These studies suggest that berbamine exerts anticancer effects on human HCC HepG2 cells in vivo and in vitro, the induction of p53 and the activity of the Fas apoptotic system may participate in the anticancer activity of berbamine in HepG2 cells.


2009-05-2452 Wang, Y.Z.; Cao, B.; Li, S.X.; Zang, Z.H.; Zhang, J.Z.; Chen, H. (Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazard, Tianjin 300162, China) Effect of proliferation, cell cycle, and Bcl-2s of MCF-7 cells by resveratrol. Journal of Asian Natural Products Research v. 11(3-4): p. 378-388, 2009 (Eng; 12 ref).

The goals were to examine the dual-directional regulation effects of resveratrol (1) in vitro by using MCF-7 cells (estradiol receptor-positive cells), study its mechanism of action, and give a systematical analysis of the regulatory networks of each related factor. An MTT test and growth curve showed that the proliferation of MCF-7 cells was inhibited by a high concentration of 1, and that its IC50 was 8.70 X 10 to power -5 plus or minus 0.23 mol/l. However, 1 induced the proliferation of MCF-7 cells at 10 to power -7 - 10 to power -5 mol/l, and resulted in a peak proliferation at 1.0 X 10 to power -7 mol/1. A high concentration of 1 arrested cell cycle progression at the G1 phase, and a typical "sub-G1 peak" of apoptotic cells was also observed by flow cytometry. The proliferation index of MCF-7 cells increased significantly with a low concentration of 1 (p less than 0.05). 1 in high concentrations induced Bax, caspase-3, and cyclin-dependent kinase (CDK) inhibitor P21 expression, whereas the expressions of cyclin CDK2, Bcl-2, and proliferating cell nuclear antigen (PCNA) were decreased by 1 treatment. Conversely, treatment with low concentrations of 1 decreased the expression of P21 and Bax, while the expressions of cyclin CDK2, Bcl-2, and PCNA were increased. These results suggest that 1 had a dual-regulatory effect on MCF-7 cells. CDK-associated protein was a key factor at both the high and low concentrations used in this study. Resveratrol (1), trans-3,5,4'-trihydroxystilbene, is a kind of natural polyphenolic compounds whose structure is similar to diethylstilbestrol. It exists widely in grapes, peanuts, and giant knotweed rhizomes.


2009-05-2453 Wang, C.H.; Wang, R.; Cheng, X.M.; He, Y.Q.; Wang, Z.T.; Wu, C.; Cao, J. (The Institute of Traditional Chinese Medicine, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai, China) Comparative pharmacokinetic study of paeoniflorin after oral administration of decoction of radix Paeoniae rubra and radix Paeoniae alba in rats . Journal of Ethnopharmacology v. 117(3): p. 467-472, 2008 (Eng ; 14 ref).

An investigation was designed and conducted to compare the pharmacokinetics difference of paeoniflorin after oral administration of the extracts of Radix Paeoniae Rubra and Radix Paeoniae Alba to rats on separate occasions. Quantification of paeoniflorin in rat plasma was achieved using a simple and rapid HPLC method for pharmacokinetic study. After oral administration of decoctions of Radix Paeoniae Rubra and Radix Paeoniae Alba, paeoniflorin was absorbed and reached a maximum concentration of 3.69 plus or minus 1.46 and 1.46 plus or minus 0.29 microg/ml at 1.67 plus or minus 0.43 and 0.80 plus or minus 0.35 h respectively. Compared to the AUC (18.85 plus or minus 7.54 microg h/ml) after oral administration of the paeoniflorin solution, a smaller AUC (10.61 plus or minus 1.51 microgh/ml) and a larger AUC (24.89 plus or minus 7.41 microgh/ml) of paeoniflorin after oral administration of the decoctions of Radix Paeoniae Alba and Radix Paeoniae Rubra were obtained, respectively. There were statistically significant differences in pharmacokinetic parameters of paeoniflorin including the t max, Cmax, AUC, t 1/2. CL, and Vd among the animals orally administered the decoctions of Radix Paeoniae Rubra and Radix Paeoniae Alba. In particular, the parameters of tmax, Cmax. and AUC of paeoniflorin were remarkably increased when oral administering paeoniflorin in the decoctions of Radix Paeoniae Rubra, but t1/2, Vd, and CL were decreased in comparison of the decoction of Radix Paeoniae Alba.


2009-05-2454 Wang, Y.; Deng, M.; Zhang, S.Y.; Zhou, Z.K.; Tian, W.X. (College of Life Science, Graduate University of Chinese Academy of Sciences, P.O. Box 3908, Beijing 100049, China) Parasitic Loranthus from Loranthaceae rather than Viscaceae potently inhibits fatty acid synthase and reduces body weight in mice. Journal of Ethnopharmacology v. 118(3): p. 473-478, 2008 (Eng ; 27 ref).

The previous results have shown one species of parasitic loranthus Taxillus chinensis exhibits potent inhibition on fatty acid synthase (FAS) that is proposed to be a potential therapeutic target for treatment of obesity. However, the medicinal parasitic loranthus come from tens of plants of two families, the Loranthaceae and the Viscaceae. This study was carried out to figure out whether these parasitic loranthus from the two families have similar inhibitory ability on FAS, and whether the parasitic loranthus with potent inhibitory ability on FAS significantly reduce body weight of animal. CD-1 mice were used to test the effects of samples on their body weight and food intake in 20 days. The reversible and irreversible inhibition on FAS was assayed to study the inhibitory ability of sixteen different medicinal plants from these two families, which were collected in nature. The reversible inhibitory ability of the extracts from the Loranthaceae was nearly 400-fold stronger than that from the Viscaceae. The species from the genus Taxillus Tieghem showed the best effect on FAS in both reversible and irreversible inhibition. Moreover, the difference in host plants did not affect markedly on the inhibitory ability of parasitic loranthus. The medicinal herb with high inhibitory ability on FAS significantly reduced the body weight and food intake of mice by oral administration. medicinal herbs from the family Loranthaceae. rather than those from the family Viscaceae, like Viscum spp. should be suitable to apply as botanical sources of parasitic loranthus for weight control. The herbs from genus Taxillus Tieghem are the best.


2009-05-2455 Wang, Y.L.; Li, R.P.; Gub, M.L.; Zhang, G.; Zhang, N.; Ma, Y.L. (Department of Pharmacognosy, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, People's Republic of China) Bakkenolides from Petasites tricholobus and their neuroprotective effects related to antioxidant activities. Planta Medica v. 75(3): p. 230-235, 2009 (Eng; 18 ref).

Four novel bakkenolides - bakkenolide-Ia, bakkenolide-IIa, bakkenolide-IIIa and bak-kenolide-IVa - were isolated from the extract of the rhizome of Petasites tricholobus (Asteraceae). The structure were characterized by using NMR (1H, 13C, 1H-1H COSY, HMQC, HMBC, and NOESY) and mass spectrorpetry. The neuroprotective activity of the bakkenolides was assayed with primary cultured neurons exposed to oxygen-glucose deprivation and oxidative insults. Antioxidant activity of the bakkenolides was evaluated by cell-free bioassays. The in vitro assay results showed that all these compounds exhibited significant neuroprotective and antioxidant activities.


2009-05-2456 Wansi, J.D.; Nwozo, S.O.; Mibaze, L.M.; Devkota, K.P.; Moladje, S.M.D.; Fomum, Z.T.; Sewald, N. (Department of Chemistry, University of Douala, Faculty of Science, Douala, Cameroon) Amides from the stem bark of Fagara macrophylla. Planta Medica v. 75(5): p. 517-521, 2009 (Eng; 15 ref).

Five new amide alkaloids, N-(4-hydroxyphene-thyl)octacosanamide (1), N-(4-hydroxyphene-thyl)hexacosanamide (2), N-(4-hydroxyphene-thyl)decanamide (3), N-vanilloyltyramine (4), and N-{O-docosanoylvanilloyl}tyramine (5), were isolated from Fagara macrophylla (Rutaceae) together with 15 known compounds. Their structures were established by using spectroscopic techniques, chemical reactions, and comparison with previously known analogues. A cytotoxicity assay was performed with the isolates, in which compounds 4, 8, and 9 were found to possess moderate to weak activity against human lung adenocarcinoma cell line A549 with IC50 values of 30.5, 11.5, and 3.5 microg/mL, respectively.


2009-05-2457 Washiyama, M.; Sasaki, Y.; Hosokawa, T.; Nagumo, S.* (Department of Medicinal Plant Science, Hoshi, University, 2-4-41 Ebara, Shinagawa, Tokyo 142-8501, Japan) Antiinflammatory constituents of Sappan Lignum. Biological & Pharmaceutical Bulletin v 32(5): p. 941-944, 2009 (Eng; 22 ref).

An in vitro assay was performed to isolate seven compounds from methanolic extract of Sappan Lignum (CSE) extract of Caesalpinia sappan (Leguminosae). These compounds were evaluated for their inhibitory effects on nitric oxide (NO) and prostaglandin E2 (PGE2) production and their suppressive effects on tumour necrosis factor-alpha (TNF-alpha), interleukin-6 (IL-6), cyclooxygenase-2 only (COX-2), and inducible nitric oxide synthase (iNOS) mRNA expression. As a result, brazilin was found to inhibit NO production. Compounds sappanchalcone and protosaponin D and E inhibited both NO and PGE2 production and suppressed TNF-alpha, IL-6, COX-2, and iNOS mRNA expression. An examination of carrageenin-induced mouse paw edema suggested that the CSE contained active compounds other than the main constituent in CSE. It was thus revealed that several compounds and mechanisms contributed to/the antiiniflammatory effect of CSE.


2009-05-2458 Wroblewska, M.; Juskiewicz, J.; Frejnagel, S.; Oszmianski, J.; Zdunczyk, Z. (Institute of Animal Reproduction and Food Research of the Polish Acaemy of Sciences, 10 uwima Str., 10-747 Olsztyn. Poland) Physiological influence of Chokeberry phenolics in model diet. Acta Alimentaria v. 37(2): p. 221-232, 2008 (Eng; 43 ref).

Seven groups of Wistar rats (8 males in each) were fed for 4 weeks diets with chokeberry (Aronia melanocarpa Rosaceae) juice, added every day to diets at a dose of 1.5, 3 and 6 ml per rat or diets were supplemented with polyphenolics extract to reach the same level of phenolics. Chokeberry juice increased stomach pH from 3.44 to 3.69-3.85 and ileal pH from 6.16 to 6.23-6.46. Alkalisation of digesta was less distinct with diets containing polyphenolics extract. Both chokeberry products decreased the concentration of caecal ammonia, especially at medium and high doses. The highest dose of chokeberry juice increased beta-glucosidase and had no effect on beta-glucuronidase activities in the caecal digesta. To compare with the control group, the highest dose of chokeberry juice and extract numerically decreased triglycerides and increased content of butyrate in short chain fatty acids sum of caecal digesta, index of antioxidant status of rats were similar in all treatments. Physiological results of applying relatively low amount of phenolic extract in the diet were similar to when applying high doses of chokeberry juice.


2009-05-2459 Wu, C.R.; Lin, L.W.; Hsieh, C.L.; Wang, W.H.; Lin, Y.T.; Hsieh, M.T. (Graduate Institute of Chinese Pharmaceutical Sciences, China Medical University, 91, Hsueh Shih Road, Taichung 40421, Taiwan, ROC) Petroleum ether extract of Cnidium monnieri ameliorated scopolamine-induced amnesia through adrenal gland-mediated mechanism in male rats . Journal of Ethnopharmacology v. 117(3): p. 403-407, 2008 (Eng ; 21 ref).

Our previous study indicated petroleum ether layer of Cnidium monnieri (Umbelliferae) and its ingredient osthole could alleviate scopolamine-induced amnesia in female rats. Hence, this study was desired to investigate the mechanism of the ameliorating effects of petroleum ether layer of CM on the performance impairment of inhibitory avoidance task and Morris water maze induced by scopolamine in male rats. CM at 0.1-0.6 g/kg orally administered 60 min before the training trial ameliorated the scopolamine-induced performance impairment on inhibitory avoidance learning and water maze in male rats. Only adrenalectomy but not peripheral cholinergic antagonist scopolamine methylbromide and catecholaminergic neurotoxin 6-hydroxydopamine blocked the ameliorating effects of CM on scopolamine-induced performance impairment in rats. Therefore, we demonstrated that the ameliorating effects of CM on scopolamine-induced performance impairment may be related to activating the adrenal gland and central acetylcholinergic neuron, instead of peripheral nervous system.


2009-05-2460 Xie, F.; Zhang, M.; Zhang, C.F.; Wang, Z.T.; Yu, B.Y.; Kou, J.P. (Key Laboratory of Modern Chinese Medicines (China Pharmaceutical University), Ministry of Education, Nanjing 210038, PR China) Anti-inflammatory and analgesic activities of ethanolic extract and two limonoids from Melia toosendan fruit . Journal of Ethnopharmacology v. 117(3): p. 463-466, 2008 (Eng ; 15 ref).

The fruit of Melia toosendan (MTF) is a traditional Chinese herbal medicine in the treatment of stomachache and many acute or chronic inflammations, as well as ascariasis. The ethanolic extract of MTF and two limonoids, isotoosendanin (1) and 1-O-tigloyl-1-O-debenzoylohchinal (2) were evaluated for their antitinflammatory and analgesic activities. Acetic acid-induced vascular permeability and lemda-carrageenan-induced hind paw edema tests in mice were used to investigate antiinflammatory activity; and acetic acid-induced writhing and hot-plate tests in mice were used to determine analgesic effect. Both the ethanolic extract and two limonoids displayed significant antiinflammatory effects. Although the ethanolic extract showed remarkable analgesic effects in both writhing and hot-plate tests, the two limonoids had analgesic effects just in writhing test.


2009-05-2461 Xu, T.T.; Yang, X.W.; Wang, B.; Xu, W.; Zhao, Y.Y. ; Zhang, Q.Y.* (Department of Natural Medicines, School of Pharmaceutical Sciences, School of Pharmaceutical Sciences, Peking University Health Science Center No. 38 Xueyuan Road Beijing 100191 P.R. China) Metabolism of hibifolin by human intestinal bacteria. Planta Medica v. 75(5): p. 483-487, 2009 (Eng; 28 ref).

Hibifolin the flavonoid of the flowers of Abelmoschus manihot (Malvaceae) was incubated with human intestinal bacteria, and four metabolites (1-4) were obtained from the incubated solution by chromatographic methods. The structures of the four metabolites were elucidated as gossypetin 8-O-beta-D-4"-deoxy-Delta4" -glucuropyranoside (1), gossypetin (2), quercetin (3), and 8-methoxy-quercetin (4), respectively, on the basis of UV, NMR, and MS data. Metabolite 1 was obtained as a new compound with a specific beta-D-4"-deoxy-delta4"-glucuropyranosyl moiety, which was formed through a unique and novel metabollic pathway.


2009-05-2462 Xu, D.; Sheng, Y.; Zhou, Z.Y.; Liu, R.; Leng, Y.; Ji-Kai, L. (State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650204, China) Sesquiterpenes from cultures of the basidiomycete Clitocybe conglobata and their 11 beta-hydroxy- steroid dehydrogenase inhibitory activity. Chemical & Pharmaceutical Bulletin v. 57(4): p. 433-435, 2009 (Eng; 11 ref).

A new drimane sesquiterpenoid, 3-keto-drimenol (1), were isolated from cultures of the basidiomycete Clitocybe conglobata together with 3beta-hydroxy-11-acetyldrimene (2), 3beta-hydroxydrimenol (3), 11,12-dihydroxy-drimene (4), 4betap-hydroxy-11,12-O-isopropyldrimene (5), and 3beta,11,12-trihydroxydrimene (6). Their structures were established from MS and NMR experiments. Compounds 1, 3, and 6 showed inhibitory activities against two isozymes of 11beta-hydroxysteroid dehydrogenases with IC50 1.7-8.0 microg/ml (human 11beta-HSD1), 10.7- 24.1 microg/ml (mouse 11beta-HSD1); 177.0-220.0 microg/ml (human 11beta-HSD2), 250.5-500.2 microg/ml (mouse 11beta-HSD2), respectively, which catalyze the interconversion of active cortisol and inactive cortisone.


2009-05-2463 Yakubu, M.T.; Akanji, M.A.; Oladiji, A.T.; Adesokan, A.A. (Medicinal Plants Research Laboratory, Depepartment of Biochemistry, University of Ilorin, PMB 1515, Ilorin, Nigeria) Androgenic potentials of aqueous extract of Massularia acuminata (G. Don) Bullock ex Hoyl. stem in male Wistar rats. Journal of Ethnopharmacology v. 118(3): p. 508-513, 2008 (Eng ; 38 ref).

This study sought to assess the androgenic potentials of aqueous extract of Massularia acuminata stem in male rats for 21 days. Male rats weighing between 220 and 260g were completely randomized into four groups: A, B, C and D. Group A, the control received orally 1 ml of distilled water (the vehicle) while groups B, C and D were orally administered with 1 ml each corresponding to 250, 500 and 1000 mg/kg body weight of the plant extract, respectively for 21 days. Rats were sacrificed 24 h after 1,7 and 21 days. Compared with the control, extract administration at all the doses produced significant increase (P less than 0.05) in testes-body weight ratio, testicular protein, glycogen, sialic acid, cholesterol, testosterone, luteinizing and follicle stimulating hormone concentrations throughout the period of administration. Testicular gamma glutamyl transferase activities were decreased significantly (P less than 0.05) after the first dose and was sustained throughout the experimental period. The available evidence in this study suggests that aqueous extract of Massularia acuminata (Rubiaceae) stem has androgenic potential which may stimulate male sexual maturation and enhance normal testicular function.


2009-05-2464 Yan, F.L.; Guo, L.Q.; Wang, C.M.; Zhang, J.X. ( Pharmacy College, Xinxiang Medical University, Xinxiang 453003, China) Chemical constituents of Isodon nervosus and their cytotoxicity. Journal of Asian Natural Products Research v. 11(3-4): p. 324-329, 2009 (Eng; 9 ref).

Two new ent-kaurane diterpenoids, 6,20,15alpha-trihydroxy-6,7-seco-1alpha,7-olide-ent-kaur-16-ene (1) and 7beta,12alpha-dihydroxy-6beta,15beta-diacetoxy-7alpha,20-epoxy-ent-kau r-2,16-dien-1-one (2), together with the six known compounds, were isolated from the aerial part of Isodon nervosus (Labiatae). The structures of the new compounds were determined by spectral methods (1D, 2D NMR, and MS). Six compounds were assayed for their cytotoxicity against HL60, SMMC-7721, and HeLa human cell lines. Compounds 5, 7, and 8 showed significant cytotoxicity.


2009-05-2465 Yang, X.N.; Wang, Y.J.; Liu, Y.S.; Tang, X. ( School of Pharmacy, Schenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, Liaoning Province, PR China) Pharmacokinetics of salvianolic acids after intravenous injection, with and without Panax quinquefolium protopanaxadiol saponins, in rats . Journal of Ethnopharmacology v. 117(3): p. 408-414, 2008 (Eng ; 28 ref).

The purpose of the present study was to examine the effects on Panax quinquefolium protopanaxadiol saponins (PQDS) extracts on the plasma protein binding and pharmacokinetic of salvianolic acids extracts extracted from the traditional Chinese medical Salvia miltiorrhizza Salvianolic acids are used to treat myocardial ischemia, and PQDS has similar functions. It is expected to achieve a better therapeutic efficacy if the two extracts are developed as a compound prescription for injection. An established high-performance liquid chromatographic technique coupled with microdialysis was used. Male Sprague-Dawley rats were given salvianolic acids extracts and a compound of the two extracts via femoral vein. It was found that there were significant differences in the percentage protein binding as well as the pharmacokinetic parameters. The rat plasma protein binding of the four salvianolic acids increased by different degrees at three dose levels (25, 50, 100 mg/kg of salvianolic acid B) when the two extracts were administered together. Also, their elimination half-life was prolonged, and their plasma concentrations remained stable longer after administration of a dose of 50 mg/kg (salvianolic acid B). The results indicated that the PQDS extracts could delay the excretion of salvianolic acids as well as maintain the blood concentration higher than salvianolic acids extracts administered alone.


2009-05-2466 Yang, W.M.; Chang, M.S.; Park, S.K. (Depepartment of Prescriptionology, College of Oriental Medicine, Kyung Hee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul 130-701, Republic of Korea) Effects of Psoralea corylifolia on the cAMP-responsive element modulator (CREM) expression and spermatogenesis in rats . Journal of Ethnopharmacology v. 117(3): p. 503-506, 2008 (Eng ; 23 ref).

Psoralea corylifolia (Leguminosae) (PC) is a medicinal herb used to improve male reproductive function in Korean traditional medicine. It has been used for treatment of male infertility including sexual dysfunction by improving kidney function. To investigate the effect of PC on spermatogenesis, the cAMP-responsive element modulator (CREM) in rat testes was evaluated using sperm analysis, the reverse-transcription polymerase chain reaction, and Western blot analysis. PC was administered to 10-week-old male Wistar rats for 56 consecutive days, the sperm formation period of the rat. The PC-treated rats had increased sperm counts with enhanced levels of CREM messenger RNA and protein, suggesting that PC induces spermatogenesis via CREM activation in rat testes.


2009-05-2467 Yang, S.S.; Wang, G.J.; Lin, Y.Y.; Kuo, Y.H.; Lee, T.H.* (Graduate Institute of Pharmacogonosy, Taipei Medical University, Taipei, Taiwan) New constituents with iNOS inhibitory activity from mycelium of Antrodia camphorata. Planta Medica v. 75(5): p. 512-516, 2009 (Eng; 16 ref).

Constituents of mycelium of Antrodia camphorata (Polyporaceae) antroquinonol B (1), 4-acetyl-antroquinonol B(2), 2,3-(methylenedioxy)-6-methylbenzene-1,4-diol (3) and 2,4-dimethoxy-6-methylbenzene-1,3-diol (4) along with antrodin D (5) were isolated by the guidance of an inducible nitric oxide synthase (iNOS) inhibitory assay and identified on the basis of their spectroscopic analysis. The effect of these compounds on the inhibition of NO production in lipopolysaccharide (LPS)-activated murine macrophages was further evaluated. Compounds 4 and 5 significantly inhibited NO production without any cytotoxicity. The IC50 values being 32.2 plus or minus 0.1 and 26.3 plus or minus 1.6 microg/mL, respectively. Compounds 1 and 2 possessed greater effects on inhibition, with-IC50 values of 16.2 plus or minus 0.8 and 14.7 plus or minus 2.8 microg/mL, respectively, but displayed cytotoxicity at considerably higher concentration. Compound 3 showed the lowest percent cell viability of 45.5 plus or minus 1.8 percent as observed in treated cell at a concentration of 16.8 microg/mL.


2009-05-2468 Yang, X.; Kuenzi, P.; Plitzko, I.; Potterat, O.; Hamburger, M. (Institute of Pharmaceutical Biology, University of Basel, Basel, Switzerland) Bicyclononane aldehydes and antiproliferative constituents from Amomum tsao-ko. Planta Medica v. 75(5): p. 543-546, 2009 (Eng; 13 ref).

A racemic mixture of a new bicyclononane aldehyde, (1RS,5SR, 6RS)-5-hydroxybicyclo {4.3.0}non-2-ene-2-carbaldehyde (1) was isolated from the fruits of Amomum tsao-ko (Zingiberaceae) together with 12 known compounds (2-13). The structure of new compound was determined on the basis of extensive spectroscopic analysis, including 1D and 2D NMR data. The antiproliferative activity of all the compounds was assessed in the murine neuroblastoma cell line N2a.


2009-05-2469 Yang, X.Z.; Zhu, J.Y.; Tang, C.P.; Ke, C.Q.; Lin, G.; Cheng, T.Y.; Rudd, J.A.; Ye, Y. (State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, P.R. China) Alkaloids from roots of Stemona sessilifolia and their antitussive activities. Planta Medica v. 75(2): p. 174-177, 2009 (Eng; 26 ref).

Protostemonamide (1), a new protostemonine-type alkaloid, and 12 known compounds were isolated from the roots of Stemona sessilifolia. Their structures were elucidated by 1D and 2D NMR spectral and other spectroscopic studies. The main alkaloidal constituents, protostemonine, stemospironine, and maistemonine, showed significant antitussive activity in a citric acid-induced guinea pig cough model following peripheral administration; stemonamine had antitussive activity following i.c.v. administration.


2009-05-2470 Ye, X.; Ng, T.B. (Department of Biochemistry, Faculty of Medicine, The Chinese Univesity of Hong Kong, Shatin, New Territories, Hong Kong, China, PRC) A trypsin-chymotrypsin inhibitor with antiproliferative activity from small glossy black soybeans. Planta Medica v. 75(5): p. 550-556, 2009 (Eng; 32 ref).

A trypsin inhibitor with a molecular mass of about 19 kDa was isolated from seeds of Chinese black soybean Glycine max (Leguminosae) cv. "Small Glossy Black". It was isolated using a protocol that comprised ion exchange chromatography on Q-Sepharose, SP-Sepharose and DEAE-cellulose. It was adsorbed on all three ion exchangers. It inhibited trypsin with an IC50 of 19 microM and chymotrypsin with an IC50 of 14.3 microM. Its trypsin inhibitory activity was stable in the pH range pH 3 - pH 13 and in the temperature range 0 degree C - 60 degree C. The trypsin inhibitor was inhibited by dithiothreitol (from 5 to 25 mM) in a dose-dependent manner. It exhibited an N-terminal sequence highly homologous to Kunitz-type trypsin inhibitors. It inhibited HIV-1 reverse transcriptase with an IC50 of 0.16 microM, and suppressed proliferation of MCF-7 breast cancer cells with an IC50 of 4.3 microM and HepG2 hepatoma cells with an IC50 higher than 25 microM. The trypsin inhibitor lacked antifungal activity and mitogenic activity toward mouse splenocytes.


2009-05-2471 Yokoi, H.; Mizukami, H.; Nagatsu, A.; Ohno, T.; Tanabe, H.; Inoue, M. (Laboratory of Medicinal Resources, School of Pharmacy, Aichi Gakuin University; 1-100 Kusumoto-cho, Chikusa-ku, Nagoya 464-8650, Japan) Peroxisome proliferator-activated receptor gamma ligands isolated from Adlay seed (Coix lacryma-jobi L. var. ma-yuen Stapf.). Biological & Pharmaceutical Bulletin v. 32(4): p. 735-740, 2009 (Eng; 36 ref).

Through screening for natural ligands against peroxisome proliferator-activated receptor gamma (PPARgamma) using the PPARgamma luciferase reporter assay, 6 hydroxy unsaturated fatty acids were isolated from Adlay seed Coix lacryma-jobi var. ma-yuen (Gramineae) extracts with acetone and 70 percent ethanol. The structures of these compounds were determined via spectral anaysis as 13-hydroxy-(9E,11E) -octadecadienoic acid (13-.E,E-HODE), 9-hydroxy-(10E,12E)-octadecadienoic acid. (9-E,E-HODE), 9-hydroxy-(10E)-octadecenoic acid, 10-hydroxy-(8E)-octadecenoic acid 8-hydroxy -(9E)- octadecenoic acid, 11-hydroxy-(9Z)-octadecenoic acid 9-E,E-HODE exhibited the most potent PPARgamma agonist activity of the isolated hydroxy unsaturated fatty acids. 9-E,E-HODE and 13-E,E-HODE are the respective geometrical isomers of 9-hydroxy-(10E, 12Z)-octadecadienoic acid and 13-hydroxy-(9Z,11E)-octadecadienoic acid, both of which are likely to be natural PPARgamma agonists produced in various mammalian cells, suggesting that 9-E,E-HODE may also act as PPARgama agonist.


2009-05-2472 Yoon, S.S.; Rhee, Y.H.; Lee, H.J.; Lee, E.O.; Lee, M.H.; Ahn, K.S.; Lim, H.T.; Kim, S.H. (College of Oriental Medicine, Kyunghee University, 1 Hoegi-dong, Dongdaemum-gu, Seoul 130-701, Republic of Korea) Uncoupled protein 3 and p38 signal pathways are involved in anti-obesity activity of Solanum tuberosum L. cv. Bora Valley . Journal of Ethnopharmacology v. 118(3): p. 396-404, 2008 (Eng ; 24 ref).

The ethanol extract of Solanum tuberosum (ESTBV), a new purple potato variety, significantly inhibited the proliferation and differentiation of 3T3-L1 cells as well as reduced the cellular leptin level. ESTBV also significantly attenuated the levels of insulin and leptin at 500 mg/kg in high fat diet fed rats. In addition, ESTBV significantly reduced total fat and whole body lipid in a therapeutic experiment, which was confirmed by MRI scanning and also significantly inhibited the retroperitoneal and epididymal fats in a preventive experiment compared with control. Similarly, the levels of total cholesterol, triglyceride and low density lipoprotein (LDL) were significantly reduced at a lower dose 200 mg/kg of ESTBV in a preventive experiment than at 500 mg/kg in a therapeutic experiment. Furthermore, body weight gain was significantly suppressed by over 4 weeks treatment of ESTBV compared with control. Interestingly, the expression of p38 mitogen-activated protein kinase (MAPK) was significantly downregulated in 3T3-L1 cells by ESTBV and the expression of uncoupled protein 3 (UCP-3) was activated in fats and liver tissues of ESTBV treated group compared with high fat diet control. ESTBV has antiobesity potential via inhibition of lipid metabolism through p38 MAPK and UCP-3 pathways.


2009-05-2473 Yu, F.; Gao, J.; Zeng, Y.; Liu, C.X. (Department of Pharmaceutical Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China) Inhibition of coix seed extract on fatty acid synthase, a novel target for anticancer activity. Journal of Ethnopharmacology v. 119(2): p. 252-258, 2008 (Eng ; 35 ref).

After the treatment with Coix Coix lacryma-jobi (Poaceae) seed extract (10 microl/ml), the residual activity of fatty acid synthase (FAS) as overall reaction, beta-ketoacyl reduction, enoyl reduction, and acetyl acetyl coenzyme A (AcAcCoA) reduction was separately detected at 340 nm in the UV-190 spectrophotometer. After rats were administrated Coix seed extract (2.5, 5.0, and 10.0 ml/kg) intragastrically for 10 days consecutively, activities of FAS, malate dehydrogenase (MDH), lipid protein lipase (LPL), hepatic lipase (HL), triglyceride (TG), and glucose-6-phosphate dehydrogenase (G-6-PD) in the plasma, liver and fatty tissues were determined. Experiments in vitro showed that the inhibition of Coix seed extract on FAS activity was significant and dose dependent, and two active sites inhibited were beta-ketoacyl reductases (KR) and enoyl reductase (ER). Experiments in vivo showed that Coix seed extract inhibited FAS activity in the liver, and elevated LPL and HL activity in the plasma, and effected G-6-PD activity. The study supports that FAS is a novel target for anticancer activity, and provides a theoretical foundation for the wide application of Coix seed extract in traditional medicine.


2009-05-2474 Yuliana, N.D.; Khatib, A.; Link-Struensee, A.M.R.; Ijzerman, A.P.; Rungkat-Zakaria, F.; Choi, Y.H.; Verpoorte, R. ( Division of Pharmacognosy, Section Metabolomics, Institute of Biology, Leiden University, Leiden, The Netherlands) Adenosine A1 receptor binding activity of methoxy flavonoids from Orthosiphon stamineus. Planta Medica v. 75(2): p. 132-136, 2009 (Eng; 27 ref).

Abioassay-gui-ded fractionation of a methafiol-water extract of Orthosiphon stamineus syn. O. grandiflorus or Clerodendranthus spicatus (Lamiaceae) leaves using the adenosine A1 receptor binding assay resulted in the isolation of seven methoxy flavonoids as active ligands with Ki values in the micromolar range. The Hill slope values are not significantly different from.unity (within 0.9-1.4), which indicates the antagonist effect to A1-R. The results of this study provide a scientific foundation for the traditional use of O. stamineus in kidney stone treatment, as the affinity of the active compounds isolated from it as adenosine A1 receptor ligands allows them to be associated with diuretic activity, which is one possible treatment for renal lithiasis.


2009-05-2475 Zeng, X.; He, H.; Yang, Y.; Yang, X.; Wu, L.; Yu, J.; Li, L. (College of Life Sciences, Zhejiang University, Hangzhou, Zhejiang 310058, PR China) Temporal effect of guanxin No. 2 on cardiac function, blood viscosity and angiogenesis in rats after long-term occlusion of the left anterior descending coronary artery. Journal of Ethnopharmacology v. 118(3): p. 485-494, 2008 (Eng ; 31 ref).

Male Sprague-Dawley rats (180-200g) were randomly divided into three groups: sham-operated, coronary artery ligation (CAL), and CAL plus Guanxin II (GX II. 10.0 g raw materials/kg/d, bid, p.o.). The experiment was carried out at 4 time points as the 3rd, 7th, 14th, and 28th day after ligation. It was found that on the one hand, GX II could significantly improve the heart function, and remarkably decrease infarct size and inhibit ventricular remodeling. On the other hand. GX II showed some unique effects such as angiogenesis which was induced in the left ventricular tissue. This result was consistent with the finding of an augmented vascular endothelial growth factor (VEGF) expression in this area. The studies demonstrated that GX II exerted extensively beneficial cardioprotective effect on CAL rats, it might stimulate angiogenesis of ischemic region to compensate blood supply to the heart via upregulated VEGF expression. The GX II was prepared of Salvia miltiorrhiza, Ligusticum chuanxiong, Paeonia lactiflora, Carthamus tinctorius and Dalbergia odorifera.


2009-05-2476 Zhang, H.F.; Hu, X.M.; Wang, L.X.; Xu, S.Q.; Zeng, F.D. (Department of Pharmacology, Medical College of Wuhan University of Science and Technology, Wuhan, P.R. China) Protective effects of scutellarin against cerebral ischemia in rats: Evidence for inhibition of the apoptosis-inducing factor pathway. Planta Medica v. 75(2): p. 121-126, 2009 (Eng; 25 ref).

Effect of scutellarin (SCU) extracted from Erigeron breviscapus (Asteraceae) were studied on brain injury through the inhibition of mediated apoptosis induced by transient focal brain ischemia in rats. Rats were treated with Scu for 7 d and then subjected to cerebral ischemia/reperfusion (I/R) injury induced by a middle cerebral artery occlusion (MCAO). After 2h of ischemia and 22 h of reperfusion, the infarct volume and the neurological deficit were determined by TTC staining and Longa's score. In situ end-labeling of nuclear DNA fragments (TUNEL) was employed to determine the degree of DNA fragmentation. NAD content and PARP activity in brain homogenate were determined. The expression of AIF in the nucleus was analyzed by Western blot. Study showed that Scu significantly reduced the infarct volume and ameliorated the neurological deficit. An increase in the number of TUNEL-positive cells and a decrease in the NAD level were also observed after 2 h of ischemia and 22 h of reperfusion. At the same time, Scu (50 and 75 mg kg -1, i.g.) treatment reversed brain NAD depletion and reduced DNA fragmentation. Scu also inhibited PARP overactivation and AIF translocation from the mitochondria to the nucleus following cerebral I/R. These findings suggested that the neuroprotective effects of Scu on brain ischemic injury-induced apoptosis might be associated with inhibition of PARP-dependent mitochondrial dysfunction and subsequent translocation of AIF.