Enantioselective metabolism of phenylpyrazole insecticides by rat liver microsomal CYP3A1, CYP2E1 and CYP2D2
نویسندگان
چکیده
The stereoselective difference of chiral pesticide enantiomers is an important factor risk evaluation and the subject has received wide attention. In present work, enantioselective metabolism phenylpyrazole insecticides including fipronil, ethiprole flufiprole in rat liver microsomes was investigated vitro. result showed remarkable enantioselectivity for fipronil with EF values 0.11–0.58. metabolite fipronil-sulfone formed degradation fipronil. R-Ethiprole to S-ethiprole transformation observed, but not R-ethiprole. No observed 0.49–0.51. enzymatic assays that inhibition ratio R-fipronil 1.5–2.1times corresponding on CYP2E1 CYP2D2 activity, leading metabolism. homology modeling molecular docking further revealed S-fipronil (?7.56 kcal mol?1) R-ethiprole (?6.45 performed better binding CYP2D2, respectively. results provided useful data ecological safety human health.
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ژورنال
عنوان ژورنال: Pesticide Biochemistry and Physiology
سال: 2021
ISSN: ['0048-3575', '1095-9939']
DOI: https://doi.org/10.1016/j.pestbp.2021.104861