Indian Journal of Experimental Biology

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VOLUME 48

NUMBER 3

MARCH 2010

CODEN: IJEB (A6) 48 (3) 181-328 (2010)

ISSN: 0019-5189 (Print); 0975-1009 (Online)

 

CONTENTS

 

Special Issue on New Drug Discovery from Natural Products

 

Foreword

185

 

 

Preface

187

 

 

Review Articles

 

Impact of natural products in modern drug development

191

Sukh Dev

 

 

 

Natural products drug discovery research in India: Status and appraisal

199

Kamlesh K Bhutani & Vikrantsinh M Gohil

 

 

 

Drug development from natural products: Exploiting synergistic effects

208

Gudrun Ulrich-Merzenich, D Panek, H Zeitler, H Vetter & H Wagner

 

 

 

Natural products drug discovery: Accelerating the clinical candidate development using reverse pharmacology approaches

220

Bhushan Patwardhan & Ashok D B Vaidya

 

 

 

Natural toxins and their therapeutic potential

228

V K Kapoor

 

 

 

Arjunolic acid: A novel phytomedicine with multifunctional therapeutic applications

238

Thiagarajan Hemalatha, Sivasami Pulavendran, Chidambaram Balachandran, Bhakthavatsalam Murali Manohar & Rengarajulu Puvanakrishnan

 

 

 

Papers

 

Antiproliferative cardenolides from Pentopetia androsaemifolia Decne. from the Madagascar rain forest

248

Eba Adou, James S Miller, Fidisoa Ratovoson, Chris Birkinshaw, Rabodo Andriantsiferana, Vincent E Rasamison & David G I Kingston

 

 

 

Screening of natural products for therapeutic activity against solid tumors

258

Bassem S El-Menshawi, Walid Fayad, Khaled Mahmoud, Salwa M El-Hallouty,
May El-Manawaty, Maria H臠g Olofsson & Stig Linder

 

 

 

Synthesis, biological evaluation and molecular docking of aryl hydrazines and hydrazides for anticancer activity

265

Vikrantsinh M Gohil, Satyam K Agrawal, Ajit K Saxena, Divita Garg, C Gopimohan & Kamlesh K Bhutani

 

 

 

Anti-ulcer and antioxidant activity of GutGardTM

269

Moumita Mukherjee, Natarajan Bhaskaran, R Srinath, H N Shivaprasad, J Joshua Allan, D Shekhar & Amit Agarwal

 

 

β-Amyrin from Ardisia elliptica Thunb. is more potent than aspirin in inhibiting collagen- induced platelet aggregation

275

Jianhong Ching, Tung-Kian-Chua, Lee-Cheng Chin, Aik-Jiang Lau, Yun-Keng Pang, Johannes Murti Jaya, Chay-Hoon Tan & Hwee-Ling Koh

 

 

 

Amelioration of tamoxifen-induced liver injury in rats by grape seed extract, black seed extract and curcumin

280

Hesham A El-Beshbishy, Ahmed M Mohamadin, Ayman A Nagy & Ashraf B Abdel-Naim

 

 

 

Elucidation of possible mechanism of analgesic action of Valeriana wallichii DC. chemotype (patchouli alcohol) in experimental models

289

Sangeeta Pilkhwal Sah, Chandra S Mathela & Kanwaljit Chopra

 

 

 

Antihyperglycemic activity of compounds isolated from Indian medicinal plants

294

Akanksha , Arvind K Srivastava & Rakesh Maurya

 

 

 

Comparative effect of Ocimum sanctum, Commiphora mukul, folic acid and ramipril on lipid peroxidation in experimentally-induced hyperlipidemia

299

Naresh Khanna, Deepika Arora, Sumita Halder, Ashish K Mehta, Gobind R Garg,
Suman B Sharma & Prabha Mahajan

 

 

 

Comparative evaluation of Bacopa monniera and Panax quniquefolium in experimental anxiety and depressive models in mice

306

Manavi Chatterjee, Pinki Verma & Gautam Palit

 

 

 

Antileishmanial phenylpropanoids from Alpinia galanga (Linn.) Willd.

314

Amandeep Kaur, Ranvir Singh, Chinmoy Sankar Dey, Shyam Sunder Sharma,
Kamlesh K Bhutani & Inder Pal Singh

 

 

 

Assessment of protective role of polyherbal preparation, Livinia, against anti-tubercular drug induced liver dysfunction

318

Kavita Gulati, Arunabha Ray & V K Vijayan

 

 

 

On-line HPLC-DPPH method for antioxidant activity of Picrorhiza kurroa Royle ex Benth. and characterization of kutkoside by Ultra-Performance LC-electrospray ionization quadrupole time-of-flight mass spectrometry

323

Pamita Bhandari, Neeraj Kumar, Bikram Singh & Paramvir S Ahuja

 

 

覧覧覧覧覧覧

 

Announcement

 

International Biennial Conference

on

New Developments in Drug Discovery from Natural Products and Traditional Medicines

(2024 November, 2010)

 

The conference will be held at National Institute of Pharmaceutical Education and Research (NIPER), Phase X, Sector - 67, S.A.S. Nagar 160062, India. The topics covered in the conference will focus on frontiers of natural product and traditional medicines based drug discovery programs; participation of the pharmaceutical industries in natural drug development programme; and possible collaboration of scientists/researchers globally for drug discovery from natural products. The registration for participation will be opened from March 1, 2010. For further details, please contact Professor K. K. Bhutani, Organizing Secretary-cum-convener, Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), Sector-67, SAS Nagar 160062, India. E-mail: ddnptm@niper.ac.in; kkbhutani@niper.ac.in. Telefax: 0172-2232208; 0172-2292036 (Websites: www.niper-ddnptm.com; www.naturalproducts-niper.com; www.niper.gov.in).

 

 

Review Articles

 

Indian Journal of Experimental Biology

Vol. 48, March 2010, pp.191-198

 

Impact of natural products in modern drug development

Sukh Dev

Formerly, INSA Research Professor Indian Institute of Technology Delhi, New Delhi 110 016, India

 

Usage of natural substances as therapeutic agents in modern medicine has sharply declined from the predominant position held in the early decades of last century, but search for bioactive molecules from nature (plants, animals, microflora) continues to play an important role in fashioning new medicinal agents. With the advent of modern techniques, instrumentation and automation in isolation and structural characterisation, we have on hand an enormous repository of natural compounds. In parallel to this, biology has also made tremendous progress in expanding its frontiers of knowledge. An interplay of these two disciplines constitutes the modern thrust in research in the realm of compounds elaborated by nature. The purpose of this article is to underline how natural products research continues to make significant contributions in the domain of discovery and development of new medicinal products. It is proposed to present the material under several heads, each of which has made natural products research relevant in the search for new and better medication.

 

Indian Journal of Experimental Biology

Vol. 48, March 2010, pp.199-207

 

Natural products drug discovery research in India: Status and appraisal

Kamlesh K Bhutani* & Vikrantsinh M Gohil

Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER),
Sector 67, SAS Nagar 160 062, India

Discovery of a new drug is time consuming and laborious process. Natural products have long been a thriving source for the discovery of new drugs due to their chemical diversity and ability to act on various biological targets. The phytochemical exploration of indigeneous flora has contributed to some extent in this race for the discovery of new drugs. The traditional Indian systems of medicine has been a part of our lifestyle since ages and the classical texts like Ayurveda and Charak Samhita have served as materia medica for this purpose. This review focuses on the contributions made from India in the drug discovery and development process and provides future directions in the area.

 

Indian Journal of Experimental Biology

Vol. 48, March 2010, pp.208-219

 

Drug development from natural products: Exploiting synergistic effects

Gudrun Ulrich-Merzenicha, D Panekb, H Zeitlerb, H Vettera& H Wagnerc

aMedical Policlinic of the Rheinische Friedrich-Wilhelms-University of Bonn, Wilhelmstr. 35-37, D-53111 Bonn, Germany

bInternal Medical Clinic I (CETA) of the Rheinische Friedrich-Wilhelms-University of Bonn,
Sigmund-Freud-Str. 25, D-53227 Bonn, Germany

cDepartment of Pharmacy, Centre of Pharma Research, Ludwig-Maximilians-University,
Butenandstr. 5-13, House B, D-81377 Munich, Germany

 

Drug development in phytomedicine has been focused in the past on the discovery and analysis of new structures from natural products. The search aimed at the determination of the single 殿ctive principle in plants, based on the assumption that a plant has one or a few ingredients which determine its therapeutic effects. But traditional systems of medicines like Ayurveda, traditional Chinese medicine or the European phytotherapy generally assume that a synergy of all ingredients of the plants will bring about the maximum of therapeutic efficacy. This approach has for long been impossible to investigate since adequate methods to standardize complex plant mixtures as well as to rationalize complex mode of actions were lacking. The introduction of high throughput technologies provides the opportunity to determine profiles of plants and to systematically explore the mode of action of combinatory drug regimes. The present review highlights the concept of synergy and gives examples of synergistic effects of plant constituents. It elaborates on how the high throughput technologies can be used in drug development from natural products with the aim of creating evidence-based plant medications in prevention and treatment of different diseases in the form of new single treatments or new combinatory drug regimes while exploiting synergy-effects.

 

Indian Journal of Experimental Biology

Vol. 48, March 2010, pp.220-227

 

Natural products drug discovery: Accelerating the clinical candidate development using reverse pharmacology approaches

Bhushan Patwardhana* & Ashok D B Vaidyab

aInterdisciplinary School of Health Sciences, University of Pune, Pune 411 007, India

bKasturba Health Society Medical Research Center, Vile Parle, Mumbai 400 056, India

The pharmaceutical industry is facing serious challenges as the drug discovery process is becoming extremely expensive, riskier and critically inefficient. A significant shift from single to multi targeted drugs especially for polygenic syndromes is being witnessed. Strategic options based on natural product drug discovery, ethnopharmacology and traditional medicines are re-emerging to offer good base as an attractive discovery engine. Approaches based on reverse pharmacology may offer efficient development platforms for herbal formulations. Relevant case studies from India and other countries where such approaches have expedited the drug discovery and development process by reducing time and economizing investments with better safety are discussed.

 

Indian Journal of Experimental Biology

Vol. 48, March 2010, pp.228-237

 

Natural toxins and their therapeutic potential

V K Kapoor

G H G Khalsa College of Pharmacy, Gurusar Sadhar, Ludhiana 141 104, India

 

Plants have been extensively investigated for exploring their therapeutic potentials, but there are comparatively scanty reports on drugs derived from animal kingdom, except for hormones. During last decade, the toxins that are used for defense by the animals, have been isolated and found useful tools for physiological and pharmacological studies, besides giving valuable leads to drug development. Toxins with interesting results have been isolated from the venoms of snakes, scorpions, spiders, snails, lizards, frogs and fish. The present review describe about some toxins as drugs and their biological activities. Some fungal, bacterial and marine toxins have also been covered in this article.

 

 

Indian Journal of Experimental Biology

Vol. 48, March 2010, pp.238-247

 

Arjunolic acid: A novel phytomedicine with multifunctional
therapeutic applications

Thiagarajan Hemalatha1, Sivasami Pulavendran1, Chidambaram Balachandran2, Bhakthavatsalam Murali Manohar3 & Rengarajulu Puvanakrishnan1*

1Department of Biotechnology, Central Leather Research Institute, Adyar, Chennai 600 020, India,
2Department of Veterinary Pathology, Madras Veterinary College, Vepery, Chennai 600 007 India,
3Centre for Animal Health Studies, Tamil Nadu Veterinary and Animal Sciences University, Madhavaram Milk Colony, Chennai 600 051 India.

 

Herbal plants with antioxidant activities are widely used in Ayurvedic medicine for cardiac and other problems. Arjunolic acid is one such novel phytomedicine with multifunctional therapeutic applications. It is a triterpenoid saponin, isolated earlier from Terminalia arjuna and later from Combretum nelsonii, Leandra chaeton etc. Arjunolic acid is a potent antioxidant and free radical scavenger. The scientific basis for the use of arjunolic acid as cardiotonic in Ayurvedic medicine is proven by its vibrant functions such as prevention of myocardial necrosis, platelet aggregation and coagulation and lowering of blood pressure, heart rate and cholesterol levels. Its antioxidant property combined with metal chelating property protects organs from metal and drug induced toxicity. It also plays an effective role in exerting protection against both type I and type II diabetes and also ameliorates diabetic renal dysfunctions. Its therapeutic multifunctionality is shown by its wound healing, antimutagenic and antimicrobial activity. The mechanism of cytoprotection conferred by arjunolic acid can be explained by its property to reduce the oxidative stress by enhancing the antioxidant levels. Apart from its pathophysiological functions, it possesses dynamic insecticidal property and it is used as a structural molecular framework in supramolecular chemistry and nanoscience. Esters of arjunolic acid function as gelators of a wide variety of organic liquids. Experimental studies demonstrate the versatile effects of arjunolic acid, but still, further investigations are necessary to identify the functional groups responsible for its multivarious effects and to study the molecular mechanisms as well as the probable side effects/toxicity owing to its long-term use. Though the beneficial role of this triterpenoid has been assessed from various angles, a comprehensive review of its effects on biochemistry and organ pathophysiology is lacking and this forms the rationale of this review.

Indian Journal of Experimental Biology

Vol. 48, March 2010, pp.220-227

 

Papers

 

Indian Journal of Experimental Biology

Vol. 48, March 2010, pp.248-257

 

Antiproliferative cardenolides from Pentopetia androsaemifolia Decne. from the Madagascar rain forest

aEba Adou, bJames S Miller, cFidisoa Ratovoson, cChris Birkinshaw, dRabodo Andriantsiferana, dVincent E Rasamison & aDavid G I Kingston1

aDepartment of Chemistry, M/C 0212, Virginia Polytechnic Institute and State University, Blacksburg, VA 24061, USA

bMissouri Botanical Garden, PO Box 299, St. Louis, Missouri 63166-0299,

cMissouri Botanical Garden, BP 3391, Antananarivo 101, Madagascar,

dCentre National d但pplication des Recherches Pharmaceutiques, BP 702, Antananarivo 101, Madagascar

Received 4 November 2009; revised 11 December 2009

Plant natural products have historically been very important to drug discovery and development, particularly in the anticancer field. This is illustrated by a discussion of the structures and activities of camptothecin and its analogues, paclitaxel (Taxol), the vinca alkaloids vinblastine and vincristine, and podophyllotoxin and its analogues. A description of the isolation of one new and three known cardenolides from the Madagascar plant Pentopetia androsaemifolia is then provided as an example of this approach to drug discovery. The paper concludes with a brief discussion of betulinic acid, an old compound which is being developed into an anticancer and anti-HIV agent, and ipomoeassin F, an interesting antiproliferative compound isolated from a plant collected in Suriname.

 

Indian Journal of Experimental Biology

Vol. 48, March 2010, pp.258-264

 

Screening of natural products for therapeutic activity against solid tumors

Bassem S El-Menshawi1, Walid Fayad2, Khaled Mahmoud1, Salwa M El-Hallouty1, May El-Manawaty1,
Maria H臠g Olofsson2 & Stig Linder*2

1Department of Pharmacognosy, Pharmaceutical Sciences Division, National Research Centre, Dokki, Giza 12622, Egypt
2Department of Oncology-Pathology, Cancer Center Karolinska, Karolinska Institute, S-171 76 Stockholm, Sweden

Received 4 November 2009; revised 11 December 2009

Most of the currently used cancer therapeutics are natural products. These agents were generally discovered based on their toxicity to tumour cells using various bioassays. Although the exact mechanisms of action of the most commonly used cancer therapeutics such as anthracyclins, podophyllotoxins and camptothecin are incompletely understood, it is becoming increasingly clear that these agents often show complex modes of action at the cellular level, interacting with numerous targets. Such complex modes of action may be the very reason for clinical efficacy. For discovering new cytotoxic anticancer drugs sophisticated screening methods were used. The principles of such screening projects conducted, using collections of purified natural products or extracts from plants have been described. By performing simple but robust pre-screening tests such as the brine shrimp assay, bioactive extracts can be identified. Extracts (65) prepared from a collection of Egyptian plants were identified that showed cytotoxity on HepG2 cells. Interestingly, 22 (33%) of these raw extracts, induced > 2-fold induction of caspase-cleavage activity in a colon carcinoma cell line, consistent with induction of apoptosis. Only a fraction of the diversity of the biosphere has been tested for biological activity and novel cancer therapeutics remains to be discovered.

 

Indian Journal of Experimental Biology

Vol. 48, March 2010, pp.265-268

 

Synthesis, biological evaluation and molecular docking of aryl hydrazines and hydrazides for anticancer activity

Vikrantsinh M Gohila, Satyam K Agrawalc, Ajit K Saxenac, Divita Gargb, C Gopimohanb & Kamlesh K Bhutania*

aDepartment of Natural Products, bCentre for Pharmacoinformatics, National Institute of Pharmaceutical
Education and Research (NIPER)
Sector-67, SAS Nagar, Punjab 160 062, India
cDepartment of Pharmacology, Indian Institute of Integrative Medicine (CSIR),
Canal Road, Jammu 180 001, India

Received 4 November 2009; revised 14 December 2009

Aryl hydrazine and hydrazide analogues were synthesized based on p-tolyl hydrazine, isolated as a breakdown product of a secondary metabolite from the mushroom, Agaricus bisporus, and tested to be highly active molecule than 5-fluorouracil in in vitro anticancer studies. The synthesized analogues were tested for anticancer activity using NCI protocol. Anolgues 12 and 15 emerged as molecules with significant in vitro anticancer activity. Molecular docking study revealed the binding orientations of aryl hydrazines and hydrazides analogues in the active sites of thymidylate synthase.

 

Indian Journal of Experimental Biology

Vol. 48, March 2010, pp.269-274

 

Anti-ulcer and antioxidant activity of GutGardTM

Moumita Mukherjee1, Natarajan Bhaskaran2, R Srinath1, H N Shivaprasad2*,
J Joshua Allan2, D Shekhar2 & Amit Agarwal2

1PES College of Pharmacy, Bengaluru 560 050, India

2R & D Centre, Natural Remedies Pvt. Ltd., Bengaluru 560 100, India

Received 4 November 2009; revised 2 December 2009

The present study was undertaken to determine the anti-ulcer and antioxidant potential of GutGardTM, a standardized extract of Glycyrrhiza glabra commonly known as licorice. Effect of various doses (12.5, 25, and 50 mg/kg, po) of GutGardTM was studied on gastric ulcers in pylorus ligation-, cold-restraint stress- and indomethacin induced gastric mucosal injury in rats. Anti-ulcer activity was evaluated by measuring the ulcer index, gastric content, total acidity, and pH of gastric fluid. GutGardTM dose dependently decreased gastric content, total acidity, ulcer index and increased pH of gastric fluid in pylorus ligation ulcer model. In cold-restraint stress- and indomethacin induced ulcer models all the doses of GutGardTM decreased the ulcer index and increased the pH of gastric fluid. The antioxidant activity was evaluated by the oxygen radical absorbance capacity (ORAC) assay. GutGardTM exhibited potent antioxidant activity with high hydrophilic and lipophilic ORAC value. GutGardTM possessed anti-ulcerogenic properties that might be afforded via cytoprotective mechanism by virtue of its antioxidant properties. These results supported the ethnomedical uses of licorice in the treatment of gastric ulcer.

 

Indian Journal of Experimental Biology

Vol. 48, March 2010, pp.275-279

 

β-Amyrin from Ardisia elliptica is more potent than aspirin in
inhibiting collagen-induced platelet aggregation

Jianhong Chinga,, Tung-Kian Chuab, Lee-Cheng China, Aik-Jiang Laua, Yun-Keng Panga, Johannes Murti Jayaa,
Chay-Hoon Tanc & Hwee-Ling Koha*

aDepartment of Pharmacy, National University of Singapore, 18 Science Drive 4, Singapore 117543
bMinistry of Education, Singapore
cDepartment of Pharmacology, Yong Loo Lin School of Medicine, National University of Singapore,
10 Medical Drive, Singapore 117597

Received 4 November 2009

Ardisia elliptica Thunberg (Myrsinaceae) is a medicinal plant traditionally used for alleviating chest pains, treatment of fever, diarrhoea, liver poisoning and parturition complications. The objectives of the study were to investigate the effect of A. elliptica on collagen induced platelet aggregation and to isolate and purify potential antiplatelet components. Fresh A. elliptica leaves were extracted using methanol (70% v/v) by Soxhlet extraction and the extract was analysed for its inhibition of collagen-induced platelet aggregation. Inhibition of platelet aggregation was assessed by incubating the extracts with rabbit blood and collagen in a whole blood aggregometer and measuring the impedance. The leaf extract was found to inhibit platelet aggregation with an IC50 value of 167 μg/ml. Using bioassay guided fractionation, b-amyrin was isolated and purified. The IC50 value of b-amyrin was found to be 4.5 μg/ml (10.5 μM) while that of aspirin was found to be 11 μg/ml (62.7 μM), indicating that b-amyrin was six times as active as aspirin in inhibiting platelet aggregation. This paper is the first report that β-amyrin isolated from A. elliptica is more potent than aspirin in inhibiting collagen-induced platelet aggregation. In conclusion, A. elliptica leaves were found to inhibit collagen-induced platelet aggregation and one of the bioactive components responsible for the observed effect was determined to be b-amyrin.

 

Indian Journal of Experimental Biology

Vol. 48, March 2010, pp.280-288

 

Amelioration of tamoxifen-induced liver injury in rats by grape seed extract,
black seed extract and curcumin

Hesham A El-Beshbishya*, Ahmed M Mohamadinb, Ayman A Nagyc & Ashraf B Abdel-Naimd

aMedical Laboratories Technology Dept., Facuty of Applied Medical Sciences, bClinical Biochemistry Dept.,
Facuty of Medicine Taibah University, Al-Madinah Al-Munawwarah, Saudi Arabia
cForensic Medicine and Clinical Toxicology Dept., Faculty of Medicine, Tanta University, Egypt
dPharmacology and Toxicology Dept., Faculty of Pharmacy, King AbdulAziz University, Jeddah, Saudi Arabia.

Received 5 November 2009; revised 3 December 2009

Liver injury was induced in female rats using tamoxifen (TAM). Grape seeds (Vitis vinifera) extract (GSE), black seed (Nigella sativa) extract (NSE), curcumin (CUR) or silymarin (SYL) were orally administered to TAM-intoxicated rats. Liver histopathology of TAM-intoxicated rats showed pathological changes. TAM-intoxication elicited declines in liver antioxidant enzymes levels (glutathione peroxidase, glutathione reductase, superoxide dismutase and catalase), reduced glutathione (GSH) and GSH/GSSG ratio plus the hepatic elevations in lipid peroxides, oxidized glutathione (GSSG), tumor necrosis factor-alpha (TNF-a) and serum liver enzymes; alanine transaminase, aspartate transaminase, alkaline phosphatase, lactate dehydrogenase and gamma glutamyl transferase levels. Oral intake of NSE, GSE, CUR or SYL to TAM-intoxicated rats, attenuated histopathological changes and corrected all parameters mentioned above. Improvements were prominent in case of NSE (similarly SYL) > CUR > GSE. Data indicated that NSE, GSE or CUR act as free radicals scavengers and protect TAM-induced liver injury in rats.

 

Indian Journal of Experimental Biology

Vol. 48, March 2010, pp.289-293

 

Elucidation of possible mechanism of analgesic action of Valeriana wallichii DC chemotype (patchouli alcohol) in experimental animal models

Sangeeta Pilkhwal Sah1, Chandra S Mathela2* & Kanwaljit Chopra3

1Department of Pharmaceutical Sciences, Kumaun University Nainital, Uttarakhand 263 136, India.

2Department of Chemistry, Kumaun University Nainital, Uttarakhand, 263 001, India.

3University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, 160 014, India

Received 4 November 2009; revised 11 December 2009

Valeriana wallichii (Family Valerianaceae), popularly named as Indian valerian, exists as three chemotypes. Aim of the study was to evaluate the effect of V. wallichii chemotype (patchouli alcohol) extract (DCME) and essential oil (VPAEO) on experimental models of nociception and to elucidate its possible mechanism of action. Analgesic effect was evaluated using acetic acid induced writhing and tail flick model. DCME and VPAEO (40 and 80 mg/kg, p.o.) significantly inhibited the number of writhings as compared to vehicle treated group. None of the doses of DCME and VPAEO exhibited any effect in tail flick model suggesting only peripheral analgesic activity. When studied for mechanism of action in acetic acid induced writhing, subeffective dose of essential oil significantly potentiated the effect of aspirin while no potentiation was seen in case of extract. These data suggest that essential oil VPAEO exerted peripheral analgesic via inhibition of prostaglandin synthesis.

 

Indian Journal of Experimental Biology

Vol. 48, March 2010, pp.294-298

 

Antihyperglycemic activity of compounds isolated from Indian medicinal plants

Akankshaa, Arvind K Srivastavab & Rakesh Mauryaa*

aMedicinal and Process Chemistry Division, bDivision of Biochemistry, Central Drug Research Institute,
CSIR, Lucknow 226 001, India

Received 4 November 2009; revised 3 December 2009

Eleven antidiabetic Indian medicinal plants were investigated in streptozotocin induced diabetic rat model and provided scientific validation to prove their antihyperglycemic activity. Antidiabetic principles from five plants were isolated. All the compounds isolated were evaluated for antihyperglycemic activity in streptozotocin induced diabetic rat model and activities were compared with standard drug metformin. Some compounds were also screened in db/db mice. Two compounds (PP-1 and PP-2) inhibited significantly the activity of PTPase-1B in an in vitro system. This might be the underlying mechanism of antihyperglycemic activity of these compounds.

 

Indian Journal of Experimental Biology

Vol. 48, March 2010, pp. 299-305

 

Comparative effect of Ocimum sanctum, Commiphora mukul, folic acid and ramipril on lipid peroxidation in experimentally-induced hyperlipidemia

Naresh Khanna#, Deepika Arora#, Sumita Halder#, Ashish K Mehta*, Gobind R Garg#,
Suman B Sharma** & Prabha Mahajan#

Department of Pharmacology#, Physiology* and Biochemistry**, University College of
Medical Sciences, Delhi 110 095, India

Received 3 July 2009; revised 8 December 2009

Treatment with C. mukul and O. sanctum, showed a significant decrease in cholesterol and triglyceride levels respectively. O. sanctum also significantly increased serum HDL-cholesterol compared to control. Serum MDA levels were significantly reduced in all the treated groups compared to control suggesting that each of the drugs under study were effective in their free radical scavenging action. Erythrocyte SOD activity was increased in all the treatment groups with C. mukul showing the maximum effect followed by O. sanctum, folic acid and ramipril. The erythrocyte CAT activity was significantly increased in all the drug treated groups with maximum increase seen in O. sanctum and ramipril treated groups, whereas lesser effects were observed with C. mukul and folic acid groups. Thus, the indigenous drugs C. mukul and O. sanctum had beneficial effect on hypercholesterolemic rabbit model, both in terms of lipid profile as well as antioxidant potential. Ocimum sanctum was found to be the most promising of all the drugs. Moreover, it could be hypothesized that these plant products along with folic acid and ramipril can be explored for synergistic effect for treatment for hypercholesterolemic conditions.

 

Indian Journal of Experimental Biology

Vol. 48, March 2010, pp.306-313

 

Comparative evaluation of Bacopa monniera and Panax quniquefolium in experimental anxiety and depressive models in mice

Manavi Chatterjee, Pinki Verma & Gautam Palit*

Division of Pharmacology, Central Drug Research Institute, CSIR, Lucknow 226 001, India

Received 4 November 2009; revised 2 December 2009

The present study was undertaken to compare medicinal plants against mixed anxiety-depressive disorder (MAD) to evaluate their potency in combating MAD disorders. Previous studies from our lab have shown that Bacopa monniera (BM), and Panax quniquefolium (PQ) have significant adaptogenic properties. Hence, we have further confirmed their activity in stress related disorders like anxiety and depression in animal model, rodents and assessed their efficacy. In our experimental protocol, gross behaviour was observed through Digiscan animal activity monitor. Anxiety was studied through light dark test, elevated plus maze test and holeboard test. Depression experiments were conducted following tail suspension test and forced swim test. Further, rotarod test was also used to study any defects in motor in-coordination in mice. It was observed that BM at the dose of 80 mg/kg (po) and PQ at 100 mg/kg (po) were effective as an anti-anxiety as well anti-depressant activity and had no motor in-coordination in mice. Hence, these extracts can be used as a potent therapeutic agent in treating mixed anxiety-depressive disorder (MAD).

 

Indian Journal of Experimental Biology

Vol. 48, March 2010, pp.314-317

 

Antileishmanial phenylpropanoids from Alpinia galanga (Linn.) Willd.

Amandeep Kaura, Ranvir Singhb, Chinmoy Sankar Deyb, Shyam Sundar Sharmac,
Kamlesh K Bhutania & Inder Pal Singha*

Department of aNatural Products, bBiotechnology and cPharmacology and Toxicology, National Institute of Pharmaceutical
Education and Research (NIPER), Sector-67,
S.A.S. Nagar, 160 062, India

Received 4 November 2009; revised 11 December 2009

Hexane, chloroform and ethyl acetate extracts (100 オg/ml) of Alpinia galanga rhizomes exhibited significant activity in vitro against promastigotes of L. donovani. Twelve compounds namely, methyleugenol (1), p-coumaryl diacetate (2), 1'-acetoxychavicol acetate (3), 1'-acetoxyeugenol acetate (4), trans-p-acetoxycinnamyl alcohol (5), trans-3,4-dimethoxycinnamyl alcohol (6), p-hydroxybenzaldehyde (7), p-hydroxycinnamaldehyde (8), trans-p-coumaryl alcohol (9), galangin (10), trans-p-coumaric acid (11) and galanganol B (12) were isolated from these extracts. Of these, compounds 2, 3, 4 and 5 were found most active in vitro against promastigotes of L. donovani with IC50 values of 39.3, 32.9, 18.9 and 79.9 オM respectively. This is the first report of antileishmanial activity of the extracts and isolated constituents of A. galanga.

 

Indian Journal of Experimental Biology

Vol. 48, March 2010, pp.318-322

 

Assessment of protective role of polyherbal preparation, Livina, against
anti-tubercular drug induced liver dysfunction

Kavita Gulati, Arunabha Ray* & V K Vijayan

Department of Pharmacology and Clinical Research Centre,
Vallabhbhai Patel Chest Institute, University of Delhi, Delhi 10 007, India

Received 4 November 2009; revised 2 December 2009

The present study evaluated the possible protective role of Livina (a polyherbal preparation) against anti-tubercular therapy (ATT)-induced liver dysfunction in patients of pulmonary tuberculosis. Patients were given intensive phase treatment with 4-drugs (rifampicin, INH, pyrazinamide and ethambutol) used for anti-tubercular therapy for 2 months, followed by a 4-month continuous phase treatment with 2 drugs (rifampicin and INH) under clinical advice and supervision. Both qualitative and quantitative measures of liver function were assessed, at different time intervals, before and after ATT. Analysis of data showed that the incidence of qualitative manifestations of liver dysfunction were greater in the placebo treated group as compared to the test drug group. None of the patients of either group showed clinical jaundice. Most signific changes ant were observed in the SGOT and SGPT levels in the placebo group, wherein the levels of both enzymes were higher at 4 and 8 weeks post泡TT, as compared to the respective baseline (0 week) values. When Livina (2 capsules twice daily) was given with ATT drugs, incidence of qualitative manifestation of liver dysfunction was insignificant and SGOT and SGPT levels were also significantly lower than the placebo+ATT drugs treated group. These results indicate that the test drug (Livina) was efficacious, against ATT-induced hepatic dysfunction in patients of pulmonary tuberculosis.

 

Indian Journal of Experimental Biology

Vol. 48, March 2010, pp.323-328

 

Online HPLC-DPPH method for antioxidant activity of Picrorhiza kurroa Royle ex Benth. and characterization of kutkoside by Ultra-Performance LC-electrospray ionization quadrupole time-of-flight mass spectrometry

Pamita Bhandari, Neeraj Kumar, Bikram Singh* & Paramvir S Ahuja

Natural Plant Products Division, Institute of Himalayan Bioresource Technology (CSIR), Palampur,
Himachal Pradesh, 176 061, India

Received 4 November 2009; revised 11 December 2009

Picrorhiza kurroa Royle ex Benth., is widely used in the Indian systems of medicine for the treatment of various liver ailments. Since, the role of oxiュdative stress in the pathogenesis of liver injury has become generally recognized, in present study the free radical scavenging effect of P. kurroa was assessed by on-line HPLC-DPPH and colorimetric DPPH methods. The comparative study on antioxidant activity of P. kurroa extracts by both methods revealed that colorimetric method showed very less free radical scavenging effect while HPLC-DPPH method showed high activity. Further, the kutkoside, an important ingredient of a potent hepatoprotective formulation 徒utkin/ picroliv was investigated for its chemical composition by ultra-performance liquid chromatography coupled with diode array detection/electrospray ionization quadrupole time-of-flight mass spectrometry (UPLC-DAD/ESI-QTOF-MS). Kutkoside was considered to be a single compound and reported as picroside-II or kutkoside, however, present investigation illustrated that kutkoside is a mixture of iridoid glycosides namely, picroside II, picroside IV and 6-ferulloylcatalpol.