Active Constituent of Crude Drugs Used in Indigenous System Chemistry of Natural Product M. Pharm pharmaceutical chemistry

1. Active Constituent of Crude Drugs used in Indigenous System
Diabetic therapy
Gymnema sylvestre
BOTANICAL NAME: Gymnema sylvestre, FAMILY: Asclepiadaceae (milk weed).
COMMON NAME Sanskrit: Meshashringi, madhunashini, Hindi: Gur-mar booti, merasingi,
ENGLISH NAME: Sugar destroyer and periploca of wood
PART USED: Leaves, root and stem FLOWER (Pale yellow and bell shaped) LEAVES (Narrow
tipped elliptic smooth green leaves)
CHEMICAL CONSTITUENTS: Contain Triterpene saponins belonging to oleanane and
dammaene classes.
 Oleanane saponins are: 1.Gymnemic acid 2.Gymnemagasaponin
 Dammarene saponins are: 1. Gymnestogenin 2. Gurmarine 3. Gymnemasies
Besides this, other plant constituents are 1. Flavone 2. Trimethylamine 3.Hentriacontane 4.
Pentatriacontane 5. Phytin 6. Tartaric acid 7. Formic acid 8. Anthraquinone derivatives 9. d-
quercitol 10. Beta-chlorophylls.

2. USES: Gymnema sylvestre is used as:
 Anti-diabetic, For weight loss.
 In asthma.
 In snake bite.
 As anti-inflammatory.
 Anti-hypercholesterolemic.
 In constipation.
 In arthritis.
 In cardiopathy.
 In microbial infection.
 In some respiratory problems like cough.
 In cancer treatment.
MOA:
1. Gymnemic acid destroys the ability to discriminate sweet taste. The atomic arrangement
of gymnemic acid is similar with glucose molecule. So they fill the receptor location on the
taste buds thereby preventing its activation by sugar molecule. Similarly gymnemic acid fill
the receptor location in the absorbtive external layer of the intestine, thereby preventing
the sugar molecule absorbtion by the intestine. In the result of this low blood sugar level
occur.
2. There are some possible mechanisms by which the gymnemic acid exerts its hypoglycemic
activity are:
 It increases the secretion of insulin.
 It promotes regeneration of islet cells of pancreas.
 It increases utilization of glucose.
 It causes inhibition of glucose absorption from intestine.
Salacia reticulate
 It is native to India and Sri Lanka It contain root,leaves and stem of an herb Salacia
reticulata Belong to Family- Celastraceae Subfamily:- Hippocrateaceae Also known as
Kothala-himbutu
 Synonyms:- Svarna mula- The bark of the root is golden colored Saptachakra- When
the root is cut it shows 7 wheel like structures.
 Chemical constituents- Antidiabetic: Mangiferine, Kotalanol, Salacinol, 13 MRT
 Other constituents:- 1.3diketones, dulcitol. leucopelargonidine, glycosidal tannin,
triterpenoids lambertic acid, kotalgenin 16-acetatemeryterfonic acid.
 Use: Diabetes Treatments, Diabetic neuropathy Treatments, Diabetic foot ulcers
Treatments, Diabetic microangiopathy Treatments, Diabetic nephropathy
Treatments, Gonorrhea, and Joint pain. Asthma, Menstrual problems.

3. Moa: Salacia Reticulata is a medicinal herb from Ayurveda which appears to have anti-
diabetic activities, namely by inhibiting carbohydrate uptake from the intestines by
inhibiting a-glucosidases, amylase enzyme which involves in the conversion of
carbohydrates to sugar it appears quite effective at this, similar to Acarbose in potency.
Pterocarpus marsupiam
 Parts of the Indian kino (heartwood, leaves, flowers) biological name Pterocarpus
marsupium, Family: Leguminosae. Common Name: Malabar kino, Indian kino tree or
vijayasar
 Chemical constituents: Genus Pterocarpus contains rich sources of polyphenolic
compounds. The plant contains pterostilbene 45%, alkaloids 0.4%, tannins 5%,
protein.
 Non-glucosidal tannins: Kinotannic acid, Kinonin (C28H24012), Kinored
(C28H22011), Pyrocatechin, Pyrocatechin acid & small quantities of resin, pectin and
gallic acid.
 Flavonol glycoside: 6 hydroxy3.5.7.4tetramethoxyflavone, 6-0 rhamnopyranoside, 8-
hydroxy 4'-methoxy isoflavone 7-Oglucopyranoside.
 Marsupin and Pterostilbene significantly lower the blood glucose levels useful in
NIDDM.

4.  Root contains benzofuranone, marsupin, dihydro chalcone, pterosupin. stilbene.
pterostilbene. homoisoflavonepteromarsupone, isoliquiritigenin. transstilbene,
liquiritigenin.
Mechanism:
 Postprandial hyperglycemia is the earliest metabolic abnormality to occur in type 2
diabetes. This state initiates the development of microvascular and macrovascular
complications. Most of the currently available anti-diabetic therapies reduce fasting
blood glucose but have little impact on postprandial hyperglycemia. In this view, P.
marsupium at a dose of 200 mg/kg could be a better drug in the treatment of type 2
diabetes. Reduction in blood glucose may be mediated through enhanced insulin
secretion by regeneration of B-cells of islets of Langerhans.
 It also reduces the elevated levels of the cytokine TNF-alpha because TNF-α
mediates insulin resistance also through indirect effects including increasing free
fatty acids in circulation, stimulation of insulin counter-regulatory hormones,
impairment of endothelial function, or inhibiting the glucose-stimulated insulin
release by pancreatic B-cells.
 Weight loss in diabetes is also generally due to continuous excretion of glucose from
the body. Long-term presence of TNF-a has an appetite suppressing effect. Improved
body weight occurs after drug treatment due to TNF-a modulation.
 Other Uses: Used in diarrhoea. Bleeding and gout problems. Skin problems.
Intestinal parasites. Dental problems. Anti microbial properties. Hyperlipidemia.
Arthritis
Swertia chirata
 Parts used: Whole plant, Swertia chirata Family: Gentianaceae, Common Names:
Indian gentian, Bhunimba
 Chemical Constituents: Bioactive compounds belonging to different classes such as:
1. xanthones and their derivatives, lignans, alkaloids, flavonoids, and terpenoids.
Chiratin was the first isolated from xanthone.
2. The pharmacological efficacy of S. chirayita has been partly attributed to the
biological activity of major phytoconstituents including amarogentin, swertiamarin,
mangiferin, swerchirin, sweroside, amaroswerin, and gentiopicrin. Amarogentin is
reported to be antidiabetic.

5. v) Increases peripheral utilisation of glucose.
vi) Increases hepatic and muscle glycogen content. Promotes beta cell repair and
regeneration.
vii) Exerts insulin like action by reducing the glycated haemoglobin levels.
viii) Inhibits dipeptidyl peptidase VI mediates glucagon.
Other Uses: Hepatoprotective activity. Anti ulcer. CNS depressant activity. Anti
inflammatory. Antimicrobial.
Trigonella foenum graccum
Synonym: Fenugreek, Methi Biological source: Consist of seeds and leaves of Trigonella
foenum-gracum Family : Fabaceae
Chemical constituents:
1. Flavonoids (Quercetin and kaempferol, Luteolin, Naringenin, Vitexin.
2. 4-hydroxy isoleucine (unusual amino acid), 3. Diosgenin & Yamogenin (saponin), 4.
Trigonelline (alkaloid) and, 5. Galactomannan (Soluble fiber).

6. 3. Galactomannan: Also exert hypoglycemic effect by increasing production of GLP-1
stimulates insulin release, glucagon production and delay the gastric emptying a- Amylase
and Sucrase activity.
Liver dysfunction- Phyllanthus niruri
Biological source: It consists of all aerial parts of the plant Phyllanthus niruri belonging to
the family Euphorbiaceae. It contains not less than 0.25% of total phyllanthin and
hypophyllanthin on dried basis.
MOA:
1. Inhibits viral DNA polymerase of Hepatitis-B virus:- DNA polymerase is one of the
enzymes which are responsible for the synthesis of DNA molecules and after the inhibition
of these enzymes there is no formation of the DNA molecule of the virus. So the net result is
a multiplication of these viruses totally affected.
2. Phyllanthin binds to hepatitis B surface antigen:- when the phyllanthin binds on the
hepatitis B surface antigen damage, of cell wall of the virus is prominently occur by this
mechanism phyllanthin act as anti- Hepatitis agent.
Uses: It has antioxidant properties. It has antimicrobial properties. It has anti- inflammatory
properties. It may help lower blood sugar. It may help prevent kidney stones.