ETHNOPHARMACOLOGY: POTENTIAL SOURCE OF MODERN DRUG DISCOVERY

Ravindra Kumar Rawal*, Saurabh Bhattacharya and B.P.S. Sagar

Department of Pharmacy, IEC-CET, Knowledge Park–I, Greater Noida, U.P, India.

* Email: rsingh_rawal@hotmail.com

Abstract
This review covers the general area of disease and problems such as malaria, cancer, AIDS, Hypertension, body pain, fever. After a brief history of
ethnopharmacology, we discuss the scientific approaches that have been used in the screening of medicinal plants and identify some medicinal plants
that are used successfully in the treatment of these diseases. It is evident that few medicinal plants are continuously being screened for their
pharmacological properties and many interesting results with crude extracts have occasionally been obtained through the isolation and identification of
the active principles. However, as a source of new drugs, some medicinal plants are understudied, considering the high percentage of plants not yet
screened for their biochemical composition or for their pharmacological properties. The earlier three decades some new drugs have been derived from
plants such as Vinblastine or Vincristine, Etoposide: Paclitaxel, Topotecan, Homoharringtonine, MichellamineB, Prostratin,calanolide, Flavopiridol,
Morphine, Codeine, Dextromethorphan, Rivastigmine, Pethidine, Bromocryptine, Atracurium, Sodium cromoglycate, Methyl sergide.

Introduction
Ethnopharmacology is the branch of Ethnobotany which deals the study of scienctific material used by ethnic group as medicine (Traditional
medicine). They include mostly flowering parts but use of animals and minerals is also seen in few culture like Indian (Siddha system) and Chinese as
a medicine. Word Ethnnopharmacology does not include the Indian and Chinese traditional system of medicine properly but belongs to the group of
people which does not have proper education and theoretical hard written document .Introduction covers small ethnic group where globalization is on
their floor so that there is chance of loss of cultural heritage, leads to knowledge loss.
Ethnopharmacology more emphasize with the few specialist who possess the proper knowledge of diagnostic method disease state that treated by
potent product. These specialists included in religious practices are like ‘saint’ of ethnic society (Dravidian culture).These saints use very potent drug
in disease state which leads to be source of the semi synthetic molecules.
In the process of ethnopharmacological based drug discovery and further advancement of Ethnopharmacology, interdisciplinary subject specialists
like Anthropologist, Chemist, Pharmacologist, Pharmacognosy experts, can play a major role.
The aim of this paper is the study of plants which are very important in new drug discovery and have shown potent activity against diseases in the past.
In India, there are a large number of ethnic groups and tribes which use these plants from a long time.
This paper covers all categories of drugs like Anti-cancer. Anti-viral, Analgesic, Cardiotonic etc., normally derived from plants.

History
Ethno - botanical uses of plants reported from different parts of India:
Apatani 158 Kala C P (2005
Arunachal Pradesh 56 Tiwari K C et al
(1996)
Arunachal Pradesh 464 Haridasan K et al
(2002)
Assamese 35 Islam M (1996)
Bhil 62 Jadhav D (2006)
Cape Comorin 89 Jeeva S et al (2005)
Chakma 63 Sarmah R et al
(2006)
Chellipale 51 Udayan P S et al
(2005)
Khasi, Jaintia 100 Kharkongor P and
Joseph (1997)
Meghalaya 55 Kharduit J (1999)
Kaadar 41 Udayan P S et al
(2005)
Meitei 20 Huidr om and Singh
B K (1996)

% contribution of traditional source in drug discovery in developing of new molecules

 Figure.2. All small molecule new chemical entities, 1981-
2002, by source
“S*”: Made by total synthesis, but the pharmacophore is/was from a natural product. “ND”: Derived from a natural product and is usually a semisynthetic modification. “NM”: Natural Product Mimic “N”:
Natural product. “S”: Totally synthetic drug. (For further information see the reference

The general process involved in herbal drug discovery

A. Information about ethno-medicinal utility of drug

B. Scientific evaluation
(i) Morphological evaluation
(ii) Microscopical evaluation
(iii) Extraction
(iv) Separation, purification, and chemical characterization of molecules
(v) Pharmacological evaluation / Test for biological activity

Drug Original molecule Biological source and Clinical use Traditional use
origin
Atracurium Tubocurarine Chondodendron Muscle-Relaxant Paralyzing dart
tomentosum(brazil) poison
Bromocryptine Ergotamine Claviceps perpurea Antiparkinson’sdisease Childbirth aid
(Europe)
cabergoline ---------------- --------------------- ----------------------- ------------
Methyl sergide ---------------- -------------------- ----------------------- -------------
Neostigmine physostigmine Physostigma Myasthenia gravis Poison
venenosum
Dextromethorphan morphine Papaver somniferum Opoid analgesic Analgesic
Pethidine morphine Papaver somniferum Cough supressant Analgesic
Etoposide podophyllotoxin Podophyllum Anti-ancer Purgative and wart
hexandram (India) treatment
Sodium cromoglycate khellin Ammi visnaga (Egypt) Anti-asthmatic Bronchial infection
Rivastigmine physostigmine Physostigma Myasthenia gravis Ordeal poison
venenosum (west
Africa)

Classification of Drugs according to pharmacological activity / functional category:

• Analgesics : Aspirin: Salix species, Morphine, Codeine, Papaver somniferum
• Cardiotonic : Digitalin: Digitalis purpurea
• Malaria: Quinine: Cinchona spp, Artemsinin: Artemisia annua
• Antihypertensive: Reserpine: Rauwolfia serpentina
• Memory enhancement: Physostigmine: Physostigma venenosum
• Muscle relaxant: Tubocurarine: Chondrodendron spp.
•
Some Important Plant based Anticancer Drugs
• Vinblastine/Vincristine: Catharanthus roseus
• Etoposide: Podophyllum species
 • Paclitaxel/Docetaxel: Taxus species
• Topotecan/Irinotecan: Camptotheca acuminata
• Homoharringtonine: Cephalotaxus harringtonia
• Flavopiridol: Synthetic based on rohutikine from Dysoxylum binectariferum
• Combretastatins: Combretum caffrum
Some Important Potential Anti-AIDS Agent Discovery

1. MICHELLAMINE B
• 1987: Collected from Ancistrocladus korupensis leaves. (Korup National Park, Mundemba, S. West Cameroon).

• 1989: Michellamine B isolated. Active against a range of HIV-1 and HIV-2 strains (Boyd et al., J. Med. Chem, 1994, 37, 1740-45

Michellamine B PROSTRATIN

2. PROSTRATIN

• Dr. Paul Cox carried out in 1980s from Western Samoan.

• Traditional use of Homalanthus nutans in treatment of “yellow” fever.

3. Calanolide B

• Calanolide B from tree species Calophyllum teysmannii var. inophylloide in Sarawak, Malaysia.
 ( +) Calanolide A (-) calanolide B

Opportunities:

• Highly successful track in drug discovery history

• Low level of side effect
• Excellent biological and chemical diversity for finding novel leads and drugs
• Empirical knowledge in the treatment of various diseases accumulated throughout its long history
• Strong potential to integrate with cutting edge technology and science
• Significant advances of high throughput technologies in natural product research

Challenges

• Reliable of information
• Loss of species and knowledge
• Intellectual property right issues
• Shortening of screening life time of traditional sources
• Challenge of complex chemistry of plant molecules
• High cost to identify active metabolites
• Cumulative output of active and toxic constituents
• Less quantity of active compound.
• Redundancy of known metabolites
• Reproducibility of searched metabolites
• Re-supply difficulties
• Application of new technologies make research an increasingly complex process with inherent considerable risks of failure
• longer evaluation and test period of new product

Challenges meet
 • Joint efforts of the scientists in various plant disciplines like Anthropologist, botanist chemist and pharmacologist
• Substantial transfer of biological diversity to metabolite chemical diversity through international agreement like International Cooperative
Biodiversity Group (ICBG) promoted by National Cancer Institute, (NCI-Frederick, Maryland,USA)
• Target based identification
• Ensured plant metabolite re-supply by innovative biotechnologies
• Productive application of combinatorial biosynthesis and biotransformation

Re-supply by plant cultivation

• Species variability and genetics

• Germination & seedling
• Plantation density
• Flowering and biology of reproduction
• In vitro preservation
• Diseases sensitivity & Pests sensitivity
• Perfection of in situ dosage techniques
• Localization of the molecule
• Dynamics of secondary metabolite content
• Selection of genotypes and creation of hybrids
• Establishment of farming timetable if possible

Re-supply by Innovative Biotechnologies

• Bioreactors for Scale-up Production of Plant Cell and Tissue Cultures

Conclusion
• Traditional plants rich source of drug discovery.
• Excellent biological and chemical diversity for finding novel drugs
• Empirical knowledge in the treatment of various diseases accumulated throughout its long ethnic history
• Researcher should focus on re-supply of metabolite by biotechnological technique.
Reference
1. Farnsworth NR, et al. Medicinal Plants in Therapy. Bull. W.H.O. 63:965-981 (1985)
2. M.F. Balandrin, A.D. Kinghorn and N.R. Farnsworth. In Human Medicinal Agents from
Plants (A.D. Kinghorn and M.F. Balandrin, eds.), Symposium Series No. 534, American
Chemical Society, Washington, D.C. 2-12 (1993).
3. N.R. Farnsworth, 0. Akerele, A.S. Bingel, D.D. Soejarto and Z. Guo, Bull. WHO 63, 965-981 (1985)

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