Identification of UDP-glucuronosyltransferase isoforms involved in hepatic and intestinal glucuronidation of phytochemical carvacrol

被引：16

作者：

Dong, Rui-Hua ^{[2
]}

Fang, Zhong-Ze ^{[1
]}

Zhu, Liang-Liang ^{[1
]}

Ge, Guang-Bo ^{[1
]}

Yang, Ling ^{[1
]}

Liu, Ze-Yuan ^{[2
]}

机构：

[1] Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian 116023, Peoples R China

[2] Acad Mil Med Sci, Affiliated Hosp, Dept Clin Pharmacol, Beijing 100071, Peoples R China

来源：

XENOBIOTICA | 2012年 / 42卷 / 10期

基金：

中国国家自然科学基金;

关键词：

UDP-glucuronosyltransferase; carvacrol; human liver microsomes; human intestinal microsomes; LIVER CYTOCHROME-P450 ENZYMES; IN-VITRO; DRUG-GLUCURONIDATION; ANTIOXIDANT ACTIVITY; NOMENCLATURE UPDATE; GENE SUPERFAMILY; ESSENTIAL OILS; SUBSTRATE; THYMOL; XENOBIOTICS;

D O I：

10.3109/00498254.2012.682614

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

1. Carvacrol (2-methyl-5-(1-methylethyl)-phenol), one of the main components occurring in many essential oils of the family Labiatae, has been widely used in food, spice and pharmaceutical industries. 2. The carvacrol glucuronidation was characterized by human liver microsomes (HLMs), human intestinal microsomes (HIMs) and 12 recombinant UGT (rUGT) isoforms. 3. One metabolite was identified as a mono-glucuronide by liquid chromatography/mass spectrometry with HLMs, HIMs, rUGT1A3, rUGT1A6, rUGT1A7, rUGT1A9 and rUGT2B7. 4. The study with a chemical inhibition, rUGT, and kinetics study demonstrated that rUGT1A9 was the major isozyme responsible for glucuronidation in HLMs, and rUGT1A7 played a major role for glucuronidation in HIMs.

引用

页码：1009 / 1016

页数：8

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