Use of isoform-specific UGT metabolism to determine and predict baicalein metabolism by human liver microsomes
- Author:
Qiong ZHOU
1
Author Information
1. School of Nursing
- Publication Type:Journal Article
- Keywords:
Baicalein;
Metabolism;
UDP-glucurohnosy transferase
- From:
Chinese Pharmaceutical Journal
2012;47(15):1208-1211
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE: To determine the UGT-isoform specific metabolic fingerprint (GSMF) of baicalein, and to determine and predict its glucuronidation behavior in liver microsomes by using isoform-specific metabolism rates and kinetics. METHODS: In vitro glucuronidation rates and profiles were measured using 12 kinds of expressed UGTs and human liver microsomes. RESULTS: GSMF experiments showed that UGT1A9 was the most active isoform for baicalein metabolism. Isoform-specific metabolism and a comparison of the kinetic parameters suggested that UGT1 A9 was likely the main isoform responsible for the liver metabolism of baicalein. Correlation study also clearly showed that UGT isoform-specific metabolism could describe the metabolism rates and profile of baicalein in human liver microsomes. CONCLUSION: Baicalein is metabolized mainly by UGT1A9.GSMF and isoform-specific metabolism profile of baicalein can determine and predict its glucuronidation rates and profile in human liver microsomes. Copyright 2012 by the Chinese Pharmaceutical Association.
