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合成拟除虫菊酯在哺乳动物体内的生物转化及酶促反应

Biotransformation and enzymatic reactions of synthetic pyrethroids in mammals.

作者信息

Mikata Kazuki, Isobe Naohiko, Kaneko Hideo

机构信息

Sumitomo Chemical Co., Ltd, Kasugadenaka, Osaka, Japan.

出版信息

Top Curr Chem. 2012;314:113-35. doi: 10.1007/128_2011_254.

Abstract

Synthetic pyrethroids, a major insecticide group, are used worldwide for controlling indoor and agricultural pests. Extensive mammalian metabolism studies have been carried out since the late 1960s, and major metabolic reactions have been found to be oxidation of the acid or alcohol moiety, ester cleavage, and conjugation reactions. In addition, various conjugation reactions occur in mammals, forming hydrophilic and lipophilic conjugates. Pyrethroids are generally rapidly metabolized in mammals and completely excreted from the body in a short period. Human and laboratory animals share similar metabolic reactions for pyrethroids. Oxidation reactions in humans are mediated by several CYP isoforms. On the other hand, ester bonds of pyrethroids are hydrolyzed mainly by carboxylesterase(s).

摘要

合成拟除虫菊酯是一类主要的杀虫剂,在全球范围内用于控制室内和农业害虫。自20世纪60年代末以来,已经进行了广泛的哺乳动物代谢研究,发现主要的代谢反应是酸或醇部分的氧化、酯裂解和结合反应。此外,哺乳动物中会发生各种结合反应,形成亲水性和亲脂性结合物。拟除虫菊酯在哺乳动物中通常会迅速代谢,并在短时间内从体内完全排出。人类和实验动物对拟除虫菊酯有相似的代谢反应。人类的氧化反应由几种细胞色素P450同工酶介导。另一方面,拟除虫菊酯的酯键主要由羧酸酯酶水解。

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