Species differences for stereoselective metabolism of ethofumesate and its enantiomers in vitro

文献类型: 外文期刊

第一作者: Zhu, W.

作者: Zhu, W.;Dang, Z.;Liu, Y.;Lv, C.;Diao, J.;Zhou, Z.;Qiu, J.

作者机构:

关键词: Ethofumesate;liver microsomes;stereoselective metabolism;rabbit;rat

期刊名称:XENOBIOTICA ( 影响因子:1.908; 五年影响因子:1.917 )

ISSN: 0049-8254

年卷期: 2009 年 39 卷 9 期

页码:

收录情况: SCI

摘要: 1. The stereoselective metabolism of ethofumesate (ETO) and its enantiomers in rabbit and rat liver microsomes have been studied by chiral high-performance liquid chromatography (HPLC) method. Two metabolites were detected in both liver microsomes in the presence of beta-nicotinamide adenine dinucleotide phosphate (NADPH). 2. The T-1/2 of (+)-ETO and (-)-ETO in rabbit liver microsomes were 12.2 and 4.7 min of rac-ETO and 25.9 and 6.7 of ETO enantiomers. However, the T-1/2 of (+)-ETO and (-)-ETO in rat liver microsomes were 5.3 and 5.9 min of rac-ETO and 7.8 and 10.6 of ETO enantiomers. The stereoselective selectivity is similar to the in vivo study. 3. After incubation of ETO enantiomers, stereoselectivity was present in the formation of ETO-OH enantiomer in rabbit liver microsomes, but stereoselectivity was not evident in rat liver microsomes. 4. There was no chiral inversion from the (+)-ETO to (-)-ETO or inversion from (-)-ETO to (+)-ETO in both rabbit and rat liver microsomes.

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