Identification and characterization of human UDP‐glucuronosyltransferases responsible for the in vitro glucuronidation of bergenin
作者： Haojing Song , Jin Wang , Rui Zhang , Xiaoyan Liu , Guiyan Yuan
DOI: 10.1002/BMC.3027
关键词:
摘要: Glucuronidation plays critical role in the elimination of bergenin; however metabolic mechanism UDP-glucuronosyltransferases (UGTs) process remains to be investigated. In this study, kinetics bergenin glucuronidation by pooled human liver microsomes (HLMs) and 12 recombinat UGT isozymes were The can shown HLMs with a Km value 231.62 ± 14.08 µm Vmax 2.17 ± 0.21 nmol/min/(mg protein). Among UGTs investigated, UGT1A1 was identified as major isoform catalyzing [Km 200.37 ± 26.73 µm 1.88 ± 0.26 nmol/min/(mg protein)]. glucuronosyltransferase activities inhibited phenylbutazone, estradiol bilirubin. results demonstrate that is specifically catalyzed UGT1A1. Copyright © 2013 John Wiley & Sons, Ltd.
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