Evaluating the enantioselective degradation and novel metabolites following a single oral dose of metalaxyl in mice

文献类型： 外文期刊

第一作者： Zhang, Ping

作者： Zhang, Ping;Zhu, Wentao;Wang, Dezhen;Wang, Xinru;Wang, Yao;Zhou, Zhiqiang;Qiu, Jing

作者机构：

关键词： Metalaxyl;Enantioselectivity;Degradation;Metabolite;Mice

期刊名称：PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY （ 影响因子：3.963； 五年影响因子：4.454 ）

ISSN：

年卷期：

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收录情况： SCI

摘要： Metalaxyl [N-(2,6-dimethylphenyl)-N-(methoxyacetyl)-D,L-alaninemethylester] is a systemic fungicide widely used in agriculture. In this study, the enantioselective distribution, degradation and excretion of metalaxyl were investigated after oral gavage administration of rac-metalaxyl to mice. Concentration of metalaxyl and its enantiomers was determined by HPLC-MS/MS. The results showed that R-metalaxyl was much higher than S-metalaxyl in heart, liver, lung, urine and feces. As for the strong first pass effect, concentrations of metalaxyl in liver were much higher than those in other tissues. The total body clearance (CL) of metalaxyl in mice was 1.77 L h(-1) kg(-1) and degradation half-lives of (t(1/2)) of S-metalaxyl and R-metalaxyl in liver were 2.2 h and 3.0 h, respectively. Such results indicated the enantioselectivity of metalaxyl lies in distribution, degradation and excretion processes in mice. Main metabolites were also determined and biotransformation reactions were hydroxylation, demethylation and didemethylation. Furthermore, metabolite concentrations in urine and feces were much higher than those in tissues. These results may have potential implications to predict toxicity and provide additional information associated with adverse health effects for risk assessment of metalaxyl. (C) 2014 Elsevier Inc. All rights reserved.

分类号： S4

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