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G U R U G H A S I D A S V I S H WAV I D YA L AYA
D E PA R T M E N T O F P H A R M A C Y
SEMINAR ON
DRUGS UDED IN DIABETIC THERAPY
G Y M N E M A S Y LV E S T R E A N D P T E R C A R P O U S M A R S U P I U M
S U B J E C T: C H E M I S T R Y O F N AT U R A L P R O D U C T S
SUBMITTED TO : Dr JAGDISH SIR
S U B M I T T E D B Y : P R I YA T I WA R I
M.PHARMA 1ST SEMESTER
ROLL NO: 20703007
ENROLLMENT NO : 06332
TABLE OF CONTENTS
1.INTRODUCTION OF DISEASE
2.GYMNEMA SYLVESTRE
3.PTEROCARPOUS MARSUPIUM
Type 2 diabetes begins with insulin resistance, a condition in which cells fail to
respond to insulin properly. As the disease progresses, a lack of insulin may also
develop. This form was previously referred to as "non insulin-dependent diabetes
mellitus" (NIDDM) or "adult-onset diabetes". The most common cause is a
combination of excessive body weight and insufficient exercise.
Gestational diabetes is the third main form, and occurs when pregnant women
without a previous history of diabetes develop high blood sugar levels.
GYMNEMA
SYLVESTRE
Synonyms ;- gudmar, madhunashini,
gymnema
Classification ;-
Kingdom: Plantae;
Class: Dicotyledoneae;
Family: Asclepiadaceae;
Genus: Gymnema;
Species: sylvestre R.Br
Botanical Synonym:- Asclepias geminata
Roxb., Periploca sylvestris Retz
CHEMICAL COSTITUENTS
Microscopic characters
Gymnemic acid
Mixture of triterpenes , saponin and
colour ;- green anthraquinone derivatives
Alkoloids
Odour :- pleasant and aromatic
odour Betain
Choline
Taste :- tasteless
Trimethylamine
Size;- 3-5 × 1-2 cm Lupeol
31
CH3
32 H3C
OR1 30
Gymnemagenin 22
21
20
Gymnemic acid 13 18
19 OH 29
14
12 17
33 34 CH2 OR2 28
6 10 11 16
1
5 9 OH 27
15
CH3
2 4 26
8
3
23
HOOC O 7
24
O CH2OH
OH
OH
OH
MECHANISMS OF GYmNEMA SYLVESTRE FOR
ANTI DIABETIC EFFECT:-
The gymnemic acids are the main constituents of gymnema and are a mixture of at
least 17 different saponins .
The gymnemic acids have been shown to have antidiabetic, antilipidemic and anti-
inflammatory properties.
The phytochemical delays the absorption of glucose into the blood.
The atomic arrangement of gymnemic acid molecules is the same as that of
glucose molecules.
Therefore, gymnemic acids fill the receptors in the taste bud leading to a
prevention of activating the sugar molecules that are present in consumed food.
Additionally, the acids fill the receptors located in the absorptive external layers of
the intestine so as to prevent the absorption of glucose by the intestines . This
results in low blood sugar.
In addition, the acids have been found to stimulate the pancreas to produce insulin
which is required for glycemic control and treating adult onset diabetes mellitus.
The acids also increase the excretion of cholesterol in faeces and can act as a laxative,
cough suppressant and a diuretic.
The gymnemic acids have been shown to interfere with the ability of the taste buds
present on the tongue to taste sweet or bitter. Researchers believe that the ability of the
acids to inhibit the sweet taste means that it also inhibits the intake of glucose.
The possible mechanisms by which the leaves extract of G. sylvestre or (Gymnemic acid)
possess its hypoglycemic acid effects are:
1) It promotes regeneration of islet cells,
2) It increases secretion of insulin,
3) It causes inhibition of glucose absorption from intestine,
4) It increases utilization of glucose as it increase the activities of enzymes responsible
for utilization of glucose by insulin-dependent pathways, an increase in phosphorylase
activity, decrease in gluconeogenic enzymes and sorbitol dehydrogenase
PTEROCARPOUS MARSUPIUM
Synonyms :-
Malabar kino, Indian kino tree, vijayasa , bijasal , red
sandal Wood , rakta chandan.
Family: Fabaceae
Subfamily: Faboideae
Genus: Pterocarpus
Species: P. marsupium
The primary chemical components of P.
Chemical constituent;- marsupium are
pterosupin,
Kenotannic acid
pterostilbene,
liquiritigenin,
K- pyrocatechin(catechol)
epicatechin,
Resin
kinotannic acid,
kino-red beta-eudesmol,
Santal
marsupol,
Pterocarpin
carpusin
homopterocarpin marsupinol,
PTEROCARPUS MARSUPIAM
chemical structure:-
pterocarpin
MECHANISM OF ACTION
1. β-cell Regeneration
There is evidence to suggest that (-)-
epicatechinis effective in β-cell
regeneration
2. Insulin Release
The same study showed that (-)-
epicatechin in the water extract of PM
bark increased the cAMP content of the
islets of pancreas in rats with an
associated increase in insulin release and
conversion of proinsulin to insulin.
3. Increase in activity of oxidative enzymes
Glycolysis and tricarboxylic acid (TCA) cycle are central pathways which oxidize glucose
and are important in the regulation of glucose homeostasis.
Dysregulation of glycolysis occurs in diabetes due to reduction in the amount and/or activity
of regulatory enzymes of glycolysis. Reduction of TCA cycle flux in tissues such as skeletal
muscle and peripheral neurons have been observed in diabetes.
4.α-amylase & α-glucosidase Inhibitory Effects
Aqueous extract of the PM latex had shown a marked α-glucosidase inhibitory activity .
5.Effects on TNF-α and Peroxisome Proliferator Activator Receptors(PPARs)
The inflammatory cytokine tumor necrosis factor TNF-α is elevated in type 2 diabetes and it is
known to cause insulin resistance .
TNF-αhas a direct inhibitory effect on insulin signaling[49] in addition to indirect effects
leading to insulin resistance. Aqueous extract of PM heartwood decreased TNF-α to the
normal levels in diabetic.
TNF-α down regulates peroxisome proliferator activator receptors(PPARs) which are nuclear
receptors that regulate metabolic events of cells.
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