Etoxazole is Metabolized Enantioselectively in Liver Microsomes of Rat and Human in Vitro

文献类型： 外文期刊

第一作者： Yao, Zhoulin

作者： Yao, Zhoulin;Nie, Jing;Ye, Jingqing;Li, Zuguang;Yao, Zhoulin;Yao, Zhoulin;Qian, Mingrong;Zhang, Hu;Yao, Zhoulin;Qian, Mingrong;Zhang, Hu

作者机构：

期刊名称：ENVIRONMENTAL SCIENCE & TECHNOLOGY （ 影响因子：9.028； 五年影响因子：9.922 ）

ISSN：

年卷期：

页码：

收录情况： SCI

摘要： Acaricide etoxazole belongs to the ovicides/miticides diphenyloxazole class, affecting adults to lay sterile eggs by inhibiting chitin biosynthesis possibly. The reverse phase HPLC-MS/MS method was used to determine the etoxazole enantiomers. The enantioselective degradation behavior of rac-etoxazole in liver microsomes of rat and human in vitro with NADPH was dramatically different. The t(1/2) of (R)-etoxazole was 15.23 min in rat liver microsomes and 30.54 min in human liver microsomes, while 21.73 and 23.50 min were obtained for (S)-etoxazole, respectively. The V-max of (R)-etoxazole was almost 5-fold of (S)-etoxazole in liver microsomes of rat in vitro. However, the V-max of (S)-etoxazole was almost 2-fold of (R)-etoxazole in liver microsomes of human in vitro. The CLint of etoxazole was also shown the enantioselectivity on the contrary in liver microsomes of rat and human. These results indicated that the metabolism of two etoxazole enantiomers was selective in liver microsomes of rat and human in vitro, and enantioselectivity in the two kinds of liver microsomes was in the difference in degradation performance. The reason might be related to the composition and content involved in the enzyme system.

分类号： X

  • 相关文献
作者其他论文 更多>>

微信小程序