Abstract
METABOLIC CONVERSION OF GUGGULSTERONE: A HYPOLIPIDEMIC AGENT

*Dr. Niharika Verma

ABSTRACT

Guggulsterone is an active constituent of guggulipid, an ayurvedic drug, and is reported to have hypolipidaemic activity. Since Guggulipid is a mixture of E- and Z- isomer, it is necessary to understand the biophase behaviour of individual isomer of guggulsterone. The initiation of the pharmacokinetic study was, therefore, made with Zguggulsterone. High Performance Liquid Chromatographic analysis of treated rat serum and bile samples at post dose administration of Z- guggulsterone, showed the presence of isomerized product namely E- guggulsterone. A large variety of E- and Z- isomerisation reactions catalyzed by aconitate isomerase (aconitase) is reported in the literature. Isomerization reaction of guggulsterone in the presence of the quoted enzyme was, therefore, studied. This study was expected to assess the in-vitro biotransformation of Z- to E- guggulsterone.

Keywords: Hypolipidemic agent, Aconitate isomerase, Guggulipid, Pharmacokinetic, Biotransformation, Isomerization.


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