Quantitative regioselectivity of glucuronidation of quercetin by recombinant UDP-glucuronosyltransferases 1A9 and 1A3 using enzymatic kinetic parameters

被引：35

作者：

Chen, YK ^{[1
]}

Chen, SQ ^{[1
]}

Li, X ^{[1
]}

Zeng, S ^{[1
]}

机构：

[1] Zhejiang Univ, Coll Pharmaceut Sci, Dept Drug Metab & Pharmaceut Anal, Hangzhou 310031, Peoples R China

来源：

XENOBIOTICA | 2005年 / 35卷 / 10-11期

基金：

中国国家自然科学基金; 俄罗斯科学基金会;

关键词：

regioselectivity; quercetin; UGT1A3; UGT1A9; glucuronidation; Bac-to-Bac;

D O I：

10.1080/00498250500372172

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Quercetin has been suggested to exert its pharmacological effects, at least in part, via its metabolites, such as glucuronides. Quantitative regioselectivity analyses are important to understand the contributions of UDP-glucuronosyltransferases (UGTs) to the pharmacological activity of quercetin. The present work obtained active UGT1A9 and UGT1A3 enzymes with a Bac-to-Bac expression system, and quercetin was metabolized by each of them to four monoglucuronides (7-, 3-, 4'- and 3'-glucuronide). Enzymatic kinetic parameters of each glucuronide were calculated to elucidate quantitatively UGT1A9's and UGT1A3's regioselectivities for quercetin. UGT1A3's highest glucuronidation efficiency was observed for the 3'-glucuronide, then the 3-, 4'- and 7-glucuronide. The catalytic efficiency order for UGT1A9 was 3- > 7- > 3'- > 4'-glucuronide.

引用

页码：943 / 954

页数：12

共 28 条

[1] Dietary wine phenolics catechin, quercetin, and resveratrol efficiently protect hypercholesterolemic hamsters against aortic fatty streak accumulation [J].