Environmental Health Science Laboratory, Sumitomo Chemical Company Ltd., 1-98-3 Kasugadenaka, Konohana-ku Osaka, Japan.
J Agric Food Chem. 2011 Apr 13;59(7):2786-91. doi: 10.1021/jf102567z. Epub 2010 Dec 6.
Synthetic pyrethroids, a major insecticide group, are used worldwide to control agricultural and household pests. Mammalian metabolism of pyrethroids was substantially launched in the 1960s and 1970s by the research groups of Professor Casida and Sumitomo Chemical Co., which made great contributions to the elucidation of their metabolic fates. They showed that ester hydrolysis and oxidation play predominant roles in mammalian metabolism of pyrethroids and that rapid metabolism leads to low mammalian toxicity. These metabolic reactions are mediated by carboxylesterases and CYP isoforms, the resultant metabolites then undergoing various conjugation reactions. In general, there are substantially neither significant species differences in metabolic reactions of pyrethoids nor metabolic differences among their chiral isomers except with fenvalerate, one isomer of which yields a lipophilic conjugate causing toxicity.
拟除虫菊酯是一类重要的杀虫剂，在世界范围内被用于防治农业和家庭害虫。20 世纪 60 年代和 70 年代，Casida 教授和住友化学公司的研究小组极大地推动了对哺乳动物拟除虫菊酯代谢的研究，为阐明其代谢命运做出了巨大贡献。他们表明酯水解和氧化在哺乳动物拟除虫菊酯代谢中起主要作用，快速代谢导致低哺乳动物毒性。这些代谢反应由羧酸酯酶和 CYP 同工酶介导，生成的代谢物随后进行各种结合反应。一般来说，拟除虫菊酯的代谢反应在种间差异不大，其手性异构体之间也没有代谢差异，除了氰戊菊酯以外，氰戊菊酯的一个异构体产生一种亲脂性结合物导致毒性。
