title: Etoxazole is Metabolized Enantioselectively in Liver Microsomes of Rat and Human in Vitro.
abstract: 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 t1/2 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 Vmax of (R)-etoxazole was almost 5-fold of (S)-etoxazole in liver microsomes of rat in vitro. However, the Vmax 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.
authors.affiliation: College of Chemical Engineering, Zhejiang University of Technology , Hangzhou 310014, China.|Zhejiang Citrus Research Institute, Zhejiang Academy of Agricultural Sciences , Taizhou 318020, China.|Institute of Quality and Standard for Agricultural Products, Key Laboratory of Detection for Pesticide Residues and Control of Zhejiang Province, State Key Laboratory Breeding Base for Zhejiang Sustainable Pest and Disease Control, and MOA Key Laboratory for Pesticide Residue Detection, Zhejiang Academy of Agricultural Sciences , Hangzhou 310021, China.
authors.forename: Zhoulin
authors.initials: Z
authors.lastname: Yao
authors.affiliation: Institute of Quality and Standard for Agricultural Products, Key Laboratory of Detection for Pesticide Residues and Control of Zhejiang Province, State Key Laboratory Breeding Base for Zhejiang Sustainable Pest and Disease Control, and MOA Key Laboratory for Pesticide Residue Detection, Zhejiang Academy of Agricultural Sciences , Hangzhou 310021, China.
authors.forename: Mingrong
authors.initials: M
authors.lastname: Qian
authors.affiliation: Institute of Quality and Standard for Agricultural Products, Key Laboratory of Detection for Pesticide Residues and Control of Zhejiang Province, State Key Laboratory Breeding Base for Zhejiang Sustainable Pest and Disease Control, and MOA Key Laboratory for Pesticide Residue Detection, Zhejiang Academy of Agricultural Sciences , Hangzhou 310021, China.
authors.forename: Hu
authors.initials: H
authors.lastname: Zhang
authors.affiliation: College of Chemical Engineering, Zhejiang University of Technology , Hangzhou 310014, China.
authors.forename: Jing
authors.initials: J
authors.lastname: Nie
authors.affiliation: College of Chemical Engineering, Zhejiang University of Technology , Hangzhou 310014, China.
authors.forename: Jingqing
authors.initials: J
authors.lastname: Ye
authors.affiliation: College of Chemical Engineering, Zhejiang University of Technology , Hangzhou 310014, China.
authors.forename: Zuguang
authors.initials: Z
authors.lastname: Li
mesh_terms: D000818:Animals; D006801:Humans; D007306:Insecticides / Q000378:metabolism*; D008862:Microsomes, Liver / Q000378:metabolism*; D009249:NADP / Q000378:metabolism; D010080:Oxazoles / Q000378:metabolism*; D051381:Rats; D013237:Stereoisomerism; D053719:Tandem Mass Spectrometry
chemical_list: D007306:Insecticides; D010080:Oxazoles; D009249:NADP; C508136:etoxazole