Title

Application of Ultra High-performance Liquid Chromatography Tandem Mass Spectrometry to Investigate the Regioselective Glucuronidation of Icaritin in Vitro

Document Type

Article

Publication Date

2-13-2018

Abstract

Icaritin is one of the Epimedium products with various biological activities. In the present study, we developed a rapid, reliable and robust UHPLC-MS/MS method to simultaneously determine unconjugated icaritin and its multiple glucuronides (icaritin-3-glucuronide, icaritin-7-glucuronide and icaritin-3,7-diglucuronide) in microsomal incubation systems, and applied it to study icaritin regioselective glucuronidation in vitro. We identified the involvement of human UDP-glucuronosyltransferase (UGT) isoforms in icaritin metabolism and further studied the kinetic profiles of icaritin glucuronidation using pooled human liver microsomes (HLMs), pooled rat liver microsomes (RLMs), pooled human intestine microsomes (HIMs) and UGTs, respectively. We also evaluated regioselective glucuronidation of icaritin by UGT isoforms and conducted time-dependent experiment to elucidate the metabolic pathways for icaritin clearance. Catalytic efficiency of microsomes is determined according to rank orders of total intrinsic clearance (CL

Publication Title

Journal of Pharmaceutical and Biomedical Analysis

Volume

154

First Page

444

Last Page

453

PubMed ID

29587224

Comments

This article was published in Journal of Pharmaceutical and Biomedical Analysis, Volume 154, Pages 444-453.

The published version is available at https://doi.org/10.1016/j.jpba.2018.02.029.

Copyright © 2018.

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