Species differences for stereoselective metabolism of ethofumesate and its enantiomers in vitro |
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| Authors: | W Zhu Z Dang J Qiu Y Liu C Lv J Diao |
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| Institution: | 1. Department of Applied Chemistry, China Agricultural University, Beijing, P. R. China;2. Chinese Academy of Agricultural Sciences, China Institute of Quality Standards and Testing Technology for Agri-products, Beijing, P. R. China |
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| Abstract: | 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 β-nicotinamide adenine dinucleotide phosphate (NADPH). The T1/2 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 T1/2 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. 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. 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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| Keywords: | Ethofumesate liver microsomes stereoselective metabolism rabbit rat |
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