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Enantioselective Metabolism of Flufiprole in Rat and Human Liver Microsomes

文献类型： 外文期刊

作者： Lin, Chunmian 1 ; Miao, Yelong 1 ; Qian, Mingrong 2 ; Wang, Qiang 2 ; Zhang, Hu 2 ;

作者机构： 1.Zhejiang Univ Technol, Coll Biol & Environm Engn, Hangzhou 310014, Zhejiang, Peoples R China

2.Zhejiang Acad Agr Sci, Inst Qual & Standard Agr Prod, Hangzhou 310021, Zhejiang, Peoples R China

关键词： flufiprole;enantioselective metabolism;liver microsomes;HPLC-MS/MS

期刊名称：JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY （ 影响因子：5.279； 五年影响因子：5.269 ）

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收录情况： SCI

摘要： The enantioselective metabolism of flufiprole in rat and human liver microsomes in vitro was investigated in this study. The separation and determination were performed using a liquid chromatography system equipped with a triple quadrupole mass spectrometer and a Lux Cellulose-2 chiral column. The enantioselective metabolism of rac-flufiprole was dramatically different in rat and human liver microsomes in the presence of the beta-nicotinamide adenine dinucleotide phosphate' regenerating system. The half-lives (t(1/2)) of flufiprole in rat and human liver microsomes were 7.22 and 21.00 min, respectively, for R-(+)-flufiprole; whereas the values were 11.75 and 17.75 min, respectively, for S-(-)-flufiprole. In addition, the V-max of R-(+)-flufiprole was about 3-fold that of S-(-)-flufiprole in rat liver microsomes, whereas its value in the case of S-(-)-flufiprole was about 2-fold that of R-(+)-flufiprole in 'human liver microsomes. The CLint of rac-flufiprole also showed opposite enantioselectivy in rat and human liver microsomes. The different compositions and contents of metabolizing enzyme in the two liver microsomes might be the reasons for the difference in the metabolic behavior of the two enantiomers.

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