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Abstract

EVALUATION OF CYTOCHROME P450 INHIBITION PROPERTIES OF TRIGONELLINE HYDROCHLORIDE BY USING TANDEM MASS SPECTROMETRY

Kanaga Sabapathi S.* and Vrushabendra Swamy BM

ABSTRACT

The objective of this study was to assess the inhibitory potential of Trigonelline hydrochloride on 8 human CYP450 isoforms (CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2B6, CYP2C8, CYP2E1 and CYP3A4) in vitro using pooled human liver microsomes. Trigonelline hydrochloride was tested at 8 different concentrations (100, 33, 11, 3.7, 1.2, 0.4, 0.1, 0.05 μM). Standard CYP inhibitors were used as positive controls for each CYP isozyme tested. The production of selective metabolites reflects CYP450 activity and the formation of metabolites, in the presence of increasing concentration of Trigonelline hydrochloride, was monitored using LC-MS/MS and IC50 was determined using graphpad prism 5.

Keywords: Trigonelline, CYP Inhibition, CYP450 isoforms, IC50, Human liver microsomes, LC-MS/MS.


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