International Journal of Innovative Pharmaceutical ... · Bitter Melon, Bitter Gourd, Karela, Balsam Pear.[25] Cucurbitaceae.[26] Anti-viral, Anti-malarial, Anti-helminthic, Anti-

REVIEW ARTICLE Gupta Shivram et.al / IJIPSR / 2 (7), 2014, 1533-1554

Department of Pharmacognosy ISSN (online) 2347-2154

Available online: www.ijipsr.com July Issue 1533

SOME EVALUATED POTENTIAL THERPEUTIC AGENTS IN

HERBALISM AND THEIR PROPOSED DOSAGE FORMS

1Gupta Shivram*,

2Kharjul Mangesh,

3Bhairy Srinivas,

4Maurya Sandeep,

5Upadhyay Anand

1Department of Pharmacognosy, Shivajirao S. Jondhle College of Pharmacy, Asangaon, Thane-

421601, Maharashtra, INDIA 2,3,4,5

Department of Pharmacology, Shivajirao S. Jondhle College of Pharmacy, Asangaon,

Thane-421601, Maharashtra, INDIA

Corresponding Author:

Gupta Shivram

Department of Pharmacognosy

Shivajirao S. Jondhle College of Pharmacy

Maharashtra, INDIA

Email: [email protected]

Phone: +91-7208673842

International Journal of Innovative

Pharmaceutical Sciences and Research www.ijipsr.com

Abstract

Herbal medicines are an important part of healthcare throughout the world. In the last few years there has been an

exponential growth in the field of herbal medicine and these drugs are gaining popularity both in developing and

developed countries. Worldwide it is estimated that 80% of the population uses herbs. The practice of traditional

medicine using medicinal plants is as old as the origin of man. This type of health care was described as Herbalism

or Botanical medicine. Medicinal plants play an important role in the treatment of various diseases, especially in

the developing countries due to their cost effectiveness. The beneficial uses of medicinal plants in traditional

system of medicine of many cultures are extensively documented. Several plants have been used as dietary

adjuvant and in treating the number of diseases even without any knowledge on their proper functions and

constituents. This review work deals with the key bioactive compounds and the role of medicinal plants in herbal

medicine in India and their earlier investigation. The bioactive ingredients that have the therapeutic activity in

plants used in traditional practice are mostly unidentified. Substances found in medicinal plants, containing the

healing property of plants is known as the active principle. Chemical principles from natural sources have become

much simpler and have contributed significantly to the development of new drugs from medicinal plants.

Biologically active compounds from natural sources have always been of great interest to scientists for the new

drug developments.

Keywords: Herbalism, Medicinal Plants, Phytochemicals, Proposed dosage form, Preclinical Studies.




INTRODUCTION

HERBAL DRUGS

The main source of primary health care is herbal medicines throughout world and according to

WHO more than 70% of world population uses herbal drugs for satisfying their principal health

needs[1,2].

Being largest producer of medicinal herbs India is called as botanical garden of world and both in

developed & developing countries herbal medicines gaining popularity because of their natural

origin.[3]

In developing countries like India, 2/3 population uses medicinal herbs for primary health care

needs [4].

Officially India has record of 45,000 plant species and various estimations prove that India has

7,500 species of medicinal importance [5].

Global sales of herbal medicines are growing about 10% annually and over 25% of our medicines

contains compounds obtained from plants are proved to be effective against chronic diseases and

multidrug resistance bacteria[6].

Herbalism involves use of whole plant or parts of plants to treat injuries or illnesses. There is

continuous growth in acceptance of herbalism due to to Low/Minimum cost, potency and

efficiency, enhanced tolerance, More protection, fewer side-effects, complete accessibility

recyclable nature.[7]

PHYTOCHEMICALS IN HERBAL DRUG THERAPY

Photochemical are chemical compounds that occur naturally in plants that have protective or

disease preventive properties. Each type of fruit or vegetable may contain hundreds of

photochemical [8].

Phytochemicals identified from traditional medicinal plants present an exciting opportunity for

the development of new types of therapeutics. Phytochemicals can offer a new avenue to greatly

impact the onset and progression of chronic diseases, oxidant stress and ageing. The

phytoprotectants act as bioenhancers of several physical and biochemical processes. [9]




Fig. 1: Human health and scope of herbal medicines

Table No 1: Pharmacognostic Details Of Medicinal Plants

Scientific

name

Common

name

Family Pharmacological actions

Anti-cancer plants

Bauhinia

variegate. [10]

Camel’s foot

tree, Orchid

tree[11],

Mountain

Ebony.[12]

Caesalpiniaceae.

[13]

Antiulcer, Hepato-Protective, Anti

Hyperlipidemic, Bronchitis, Leprosy, Tumors

[14], Immunomodulatory, Antimicrobial.[15]

Catharanthus

Roseus L. [16]

Vinca

rosea.[17]

Apocynaceae.[18] Anti Hyperglycemic, Antineoplastic,

Antidiabetic, Antifeedant, Antisterility

Anthelminthic, Antidiarrheal. [19]

Anti-diabetic plants

Gymnema

sylvestre [20]

Gurmar, Mera-

Singi,

Periploca Of

Woods, Cow

Plant,

Australian Cow

Plant.[21]

Asclepiadaceae.[22] Normoglycemic and Hypolipidemic activity,

Radio protective activity, Snake venom

neutralizing effect,[21] Antiflu, Antihistaminic,

Antipyretic, Antiviral, Hypotensive,

Immunostimulant, Mutagenic, Sedative,

Serotoninergic, [23]

Momordica

charntia[24]

Bitter Melon,

Bitter Gourd,

Karela, Balsam

Pear.[25]

Cucurbitaceae.[26] Anti-viral, Anti-malarial, Anti-helminthic, Anti-

cancerous, Abortifacient, Anti-fertility, Anti-

diabetic.[27]

Tinospora

cordifolia [28]

Tinospora,

Giloe, Gulbel,

Gurcha,

Amrita,

Guduchi.[29]

Menispermaceae.

[30]

Adaptogen, Antianemic, Antiimmunosuppressant,

Antineoplastic, Antiperiodic, Antispasmodic,

Antiviral, Aphrodisiac, Choleretic, Deobstruent,

Diuretic, Hepatoprotective, Hypoglycemic,

Lipolytic, Mitogenic. [31]




Table No 2: Phytochemical Details of Medicinal Plants

Medicinal plants name Major Active phytochemicals

Bauhinia variegate. Cyanidin glucoside, Malvidin glucoside, Peonidin glucoside, [32] kaempferol,

ombuin, Kaempferol-3-glucoside, lupeol, β-sitosterol, rutin, quercetin,

quercitrin, apigenin, hesperidin.[33]

Catharanthus Roseus L. Vincristine, Vinblastine, [34] Loganin, Secologanin.[35]

Gymnema sylvestre Gymnemic Acids (I,II,III,IV), Gymnemagenin (I,II,III,IV,V,VI),

Gymnestrogenin,[36] Gymnemasaponin III, Gymnemasaponin IV,

Gymnemasaponin V. [21]

Momordica charntia β-momorcharin, Vicine, [38], Charantin [39], Momordicin [40], Sitosterol

glucoside , Stigmasterol glucoside, Momordicosides K and L, [41]

Charantosides ( I , II, III, IV, V, VI ), Karavilosides ( I , II , III, IV, V),

Momordicosides A&B [42]

Tinospora cordifolia Berberine[43], Tinosporin, isocolumbin, palmatine, tinocordiside,

tinocordifolioside , cordioside, [44] Columbin, Tinosporaside, Cordifolioside

A, jatrorhizine, tembeterine, cholin, [45], Tinoscorside A, Tinoscorside B,

Tinoscorside C, Tinoscorside D, Syringin. [46]

Table No 3: Phytochemical structures with their pharmacological actions

Name

of

plant

Phytochemical Structure Pharmacological activity

Ba

uh

inia

vari

egate

Cyanidin glucoside

(R1=OH, R2=H),

Malvidin glucoside

(R1=R2=OH),

Peonidin glucoside

(R1=R2=OCH3)

[43]

Anti-cancer [32]

Kaempferol

[48]

Antifungal[49],

Anti-inflammatory [50]

Ombuin

[51]

Cytotoxic activity [52]

Kaempferol-3-

glucoside

[53]

Antioxidant [54]




Lupeol

[55]

Anti-Urolithiatic Activity,

Hyperoxaluria, Anti-

Arthritic,Cardioprotective

Activity[56], Anti Tumour[57],

Antihepatotoxicity,

Antihyperglycemic

Hypotensive, Antiedemic [58]

Apoptosis Inducing activity [59]

β-sitosterol

[60]

Immune Modulation, Rheumatoid

Arthritis, Anti-HIV/FIV

Infection, Anti-Cancer, Anti

Pulmonary Tuberculosis [61]

Stimulatory Activity., Anti-

Inflammatory [62]

Rutin

[63]

Antioxidant [64], Thrombolytic

Agent [65] Hypoglycemic And

Antidiabetic Activity[66]

Antidepressant [67]

Quercetin

[68]

Antifungal [49] anti-tumor [69]

antiviral [70] Hypoglycemic &

Antidiabetic[66] Cardiotonic

[71] Gastroprotective[72]

Allergy, Asthma.[73]

Quercitrin

[74]

Antibacterial [75] Diuretic [76]

Antidiarrhoeal [77]

Apigenin

[68]

Apoptosis Inducing activity

[59] Cardiotonic [71]

Antitumour [78]

Hesperidin

[79]

Blood Vessel Disorders,

Antiinflammatory [79]




Cath

ara

nth

us

Ro

seu

s L

.

Vincristine

[35]

Anticancer [35]

Vinblastine

[35]

Anticancer [35]

Loganin

[35]

Antiviral (Hepatitis C) [80], Anti

Amnesic Hepatprotective &

Anticholestatic [81] Alleviates

Diabetes-Induced Memory

Impairments. [82]

Secologanin

[35]

Muscle Relaxant [83]

Gym

nem

a s

ylve

stre

Gymnemic acid I

(R1=Tigoyl, R2=Ac)

Gymnemic acid II

(R1=2-

Methylbutyroyl,

R2=Ac)

Gymnemic acid III

(R1=2-

Methylbutyroyl,

R2=H)

Gymnemic acid IV

(R1=Tigoyl, R2=H)

[37]

Antidiabetic [37]

Gymnemagenin I

(R=H, R1=H)

Gymnemagenin III

(R=Ac, R1=Ac )

Gymnemagenin IV

(R=R1=Bz)

Gymnemagenin V

(R=H, R1=C(Ph)3)

[23]

Antidiabetic[23]




Gymnemagenin II

(R=H )

Gymnemagenin VI

(R=Ac)

[23]

Antidiabetic [23]

Gymnestrogenin

[37]

Antidiabetic [37]

Gymnemasaponin III

(R1=β-glc, R2= β-

glc0- β-glc, R3=H),

Gymnemasaponin IV

(R1= β-glc0- β-glc,

R2= β-glc, R3=H)

Gymnemasaponin V

(R1= β-glc0-β-glc,

R2=β-glc0-β-glu,

R3=H)

[21]

Antihyperglycemic effect [84],

Leishmanicidal activity[85]

Mo

mor

dic

a c

ha

rnti

a

β-momorcharin

[86]

Antidiabetic [86]

Vicine

[87]

Antidiabetic [87]

Charantin

[42]

Antidiabetic [42]

Momordicin

[40]

Antidiabetic [40]




Sitosterol glucoside

[41]

Antidabetic [41]

Stigmasterol

glucoside

[41]

Antidabetic [41]

Momordicoside K

(R=Me)

Momordicoside L

(R=H) [41]

Hypoglycaemic /

Antihyperglycaemic [88,89]

Charantoside I

[42]

Antidiabetic [90]

Charantoside II

[42]

Antidiabetic [90]

Charantosides III

R=β-D-

glucopyranosyl

[42]

Antidiabetic [90]

Charantosides IV

R=β-D-allopyranosyl

[42]

Antidiabetic [90]

Charantosides V

R=β-D-

glucopyranosyl [42]

Antidiabetic [90]




Charantosides VI

R=β-D-allopyranosyl

[42]

Antidiabetic [90]

Karaviloside I

R1=Me, R2= β-D-

glucopyranosyl

[42]

Antidiabetic [90]

Karaviloside II

R1=Me, R2= β-D-

allopyranosyl [42]

Antidiabetic [90]

Karaviloside III

R1=H, R2= β-D-

allopyranosyl

[42]

Antidiabetic [90]

Karaviloside IV

R1= β-D-

allopyranosyl R2=H

[42]

Antidiabetic [90]

Karaviloside V R1=

β-D-allopyranosyl

R2= β-D-

allopyranosyl

[42]

Antidiabetic [90]

Momordicoside A

(R=β gentiobiosyl)

Momordicoside B

(R= Glu-pyr-glu-pyr-

xyl-pyr.) [42]

Inhibit Tumor Growth [38]

Tin

osp

ora

co

rdif

olia

Berberine

[91]

Antidiabetic [91]




Tinosporin

[92]

Antidiabetic [92]

Isocolumbin

[91]

Antidiabetic [91]

Palmatine

[91]

Antidiabetic [91]

Tinocordiside

[92]

Antidiabetic [92]

Tinocordifolioside

[91]

Antidiabetic [91]

Cordioside

[91]

Antidiabetic [91]

Columbin

[45]

Antidiarrhoeal [29] Schizonticidal

[91]

Tinosporaside

[45]

Antihyperglycemic [93]

Immunomodulatory [91]




Cordifolioside A

[45]

Antidiarrhoeal [29]

Immunomodulatory [91]

Jatrorhizine

[91]

Antimicrobial, Antimalarial [91],

Antioxidant [94]

Tembeterine

[91]

Antinociceptive [91]

cholin

[92]

Antidiarrhoeal, Antimicrobial,

Antihelmithic [29]

Tinoscorside A

(R=Formyl)

Tinoscorside B

(R=Acetyl )

[46]

Antidiarrhoeal [29]

Tinoscorside C

(R1=H, R2=S,

R3=OH )

[46]

Antidiarrhoeal [29]

Tinoscorside D

[46]

Antidiarrhoeal [29]

Syringin

[91]

Antidiarrhoeal [29],

Immunomodulatory,

Hypotensive,

Anti-Inflammatory [91]




Table No 4: Pharmacological mechanism of action of some phytochemical

Name Of

Plant

Active Phytochemicals Mechanism Of Action

Bauhinia

variegata

Cyanidin glucoside,

Malvidin glucoside,

Peonidin glucoside,

Kaempferol galactoside

The bark extract shows , there is decrease in rate of tumor

incidence, number of papillomas along with the decrease tumour

yield and burden. Other effects observed are depleted level of

glutathione was restored.[33]

Catharanthus

Roseus L.

Vincristine and

Vinblastine

Antimitotic phytochemicals (Vinblastine and vincristine) bind

with tubilin and prevents formation of microtubules which help in

the formation of mitotic spindle and also blocks mitosis & causes

metaphase arrest.[34]

Gymnema

sylvestre

Gymnemic acids

(I,II,III,IV),

Gymnemagenin

(I,II,III,IV,V,VI)

Gymnestrogenin.

The gymnemic acid is acts as antidiabetic, which exhibits the

pharmacological actions like regeneration of islet cells, increased

insulin secretion, inhibition of glucose absorption from intestine,

increases utilization of glucose by increasing the activities of

enzymes in insulin dependent pathways, an increase in

phosphorylase activity, decrease in gluconeogenic enzymes and

sorbitol dehydrogenase. gymnemic acid corrects the metabolic

derangements in the liver, kidney, and muscles.[37,95]

Momordica

charntia

β-momorcharin,

Vicine,

polypeptide-p , Charantin

,

Momordicin ,

Sitosterol glucoside ,

Stigmasterol glucoside

The extract shows antidiabetic effects such as increase glucose

utilization by the liver, decrease gluconeogenesis by inhibiting

glucose-6-phosphatase and fructose-1,6-bisphosphatase, improve

glucose oxidation through the shunt pathway by activating

glucose-6-phosphate dehydrogenase, increased cellular uptake of

glucose, promotes insulin release, regeneration and or repair of

beta cells in pancreas.[96]

Tinospora

cordifolia

Berberine ,

Tinosporin, isocolumbin,

Palmatine,

Tinocordiside ,

Tinocordifolioside ,

Cordioside,

β-Sitosterol

dichloromethane extract shows 100% inhibition of α-glucosidase

activity and other effects such as regeneration of b-cells of islets

of Langerhans. Thedistinct effect observed was inhibitory effect

on adrenaline-induced hyperglycemia.[97,98]




Table No 5: Preclinical studies

Name of

medicinal

plant

Animal

model

used

Experimental design &

pharmacological effect

Conclusion Proposed

Pharmaceutic

al dosage form

Mode

of

adminis

tration

Bauhinia

variegate

Mice[99] In vitro cytotoxic studies in rat

liver tumour and human cancer

cell lines was carried by

evaluating various biochemical

parameters like serum

glutamate oxaloacetate

transaminase (SGOT),

serum glutamate pyruvate

transaminase (SGPT),

alkalinephosphatase (ALP),

total bilirubin for

chemopreventive activity

[99]

Administration of

EBV significantly

decreased the level of

SGPT, SGOT, ALP,

total bilirubin, which

indicates the

carcinogenic

inhibitory activity.

[99]

Flower given

with cow milk,

leaves

decoction.

[100]

Paste [101]

Orally,

Topical

( for

skin

infectio

ns)

[101]

Catharant

hus

Roseus

female

mice

[102]

Intraperitonial administration

of ethanolic extract of leaves

was found active on

CA0ehrlich ascites in female

mice[102]

Out of total (130) indole

alkaloids , 25 are in

dimeric nature. They

found effective on

leukp1534. [102]

Ethanolic %

chloroform leaf

extract.[102]

Intraperi

toneally,

Orally.

[102]

Gymnema

sylvestre

alloxaniz

ed rabbits

[103]

Inhibition of gluconeogenic

enzymes and recovery of

hepatic damages during

hypoglycemic phase. [103]

Dried leaf powder of

Gymnema sylvestre

demonstrated

hypoglycemic effects in

alloxanized rabbits.

[103]

Powder [103] Oral

[103]

Momordic

a charntia

adult

male

albino

rats [104]

Effects of bitter melon was

evaluated by estimating Hb

A1c%, concentration and

quantity of insulin release

from pancreas of diabetic rats

as compared to control. [104]

bitter melon extract has

hypoglycaemic effects

by reducing serum

glucose concentration ,

increasing serum insulin

level and inducing

peripheral glucose

uptake and inhibiting

intestinal glucose

absorption. [104]

M. charantia is

dried,

powdered, and

placed into

capsules to

make pills.

[105]

Oral

Tinospora

cordifolia

Female

albino

rats [106]

Hypoglycemic potential of

Tinospora cordifolia was

evaluated by measuring

activities of hepatic glycogen

synthase and glycogen

phosphorylase activity. [106]

Antidiabetic affects of

Tinospora cordifolia

may be due to increased

hepatic glycogen

synthase and decreased

glycogen phosphorylase

activity without altering

serum insulin

levels.[106]

Infusion,

tincture,

powder [31]

Oral




CONCLUSION

This study reveals the role of active phytochemical in various diseases as in recent years, there

has been renewed interest in the treatment against different diseases using herbal drugs as they are

generally non-toxic and World Health Organization has also recommended the evaluation of the

effectiveness of plants in condition where we lack safe modern drugs. The interest in Nature as a

source of potential chemotherapeutic agents continues. Natural products and their derivatives

represent more than 50% of all the drugs in clinical use in the world. The information furnished

in this review work will contributes to the botanical medicine for various disease conditions.

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