Glucuronidation of aurantio-obtusin: identification of human UDP-glucuronosyltransferases and species differences

被引：10

作者：

Mi, Bao-Li ^{[1
]}

Sun, Qi ^{[2
]}

Qu, Yan-Qing ^{[3
]}

Gao, Xiao-Xu ^{[1
]}

Yu, Zhen-Wen ^{[1
]}

Ge, Guang-Bo ^{[4
]}

Cai, Shan-Shan ^{[1
]}

Zhang, Jie ^{[1
]}

Zheng, Yan-Chao ^{[1
]}

Zhang, Zhen-Qiu ^{[1
]}

机构：

[1] Liaoning Univ Tradit Chinese Med, Pharmaceut Coll, Dalian 116600, Peoples R China

[2] JiLin Aodong Med Ind Grp Co Ltd, Dept Res & Dev, Dunhua, Peoples R China

[3] Yantaishan Hosp, Yantai, Shandong, Peoples R China

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

来源：

XENOBIOTICA | 2014年 / 44卷 / 08期

关键词：

Aurantio-obtusin; species difference; UDP-glucuronosyltransferase (UGT); METABOLISM; BIOAVAILABILITY; ELUCIDATION;

D O I：

10.3109/00498254.2014.895881

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

1. The aurantio-obtusin's glucuronide was detected when aurantio-obtusin was incubated with human liver microsomes (HLMs). Recombinant UGT isoforms screening experiment showed that UGT1A8 was the major isoform contributed to the glucuronidation. 2. The metabolic profiles for aurantio-obtusin in liver microsomes from different species were similar, however, the intrinsic clearance values (V-max/K-m) among the species were: Monkey > Human > Rat > Rabbit > Dog > Pig > Mouse > Guinea pig.

引用

页码：716 / 721

页数：6

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