In vitro metabolism of atrazine, terbuthylazine, ametryne, and terbutryne in rats, pigs, and humans.
In vitro metabolism of atrazine, terbuthylazine, ametryne, and terbutryne in rats, pigs, and humans.
复制标题
阿特拉津、特丁嗪、莠灭净和特丁炔在大鼠、猪和人类体内的体外代谢。
DOI：
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发表时间：
1996
影响因子：
3.9
通讯作者：
R. Böcker
中科院分区：
文献类型：
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作者：
D. Lang;D. Criegee;A. Grothusen;R. Saalfrank;R. Böcker
用大鼠、猪和人的肝微粒体研究了四种s-三嗪类除草剂（阿特拉津、特丁基嗪、阿米丁和特丁基嗪）的体外代谢。建立了紫外检测的高效液相色谱分析方法。主要的I相反应是n -单脱烷基反应、异丙基或叔丁基部分的羟基化反应和底物的亚砜化反应。在该体系中没有发现双烷基化、2-羟基化或叔丁基部分的裂解。在所有物种中，2-甲基硫代-s-三嗪的亚砜化催化作用超过其他代谢反应的3-4倍。总的来说，所有物种都产生相同类型的代谢物，但代谢物的比例存在物种特异性差异。用手性高效液相色谱技术研究了一种新的阿特拉津异丙基羟基化代谢物的种特异性立体选择性形成。这种代谢物的立体选择性产生在不同的物种中是不同的，其S/R比在大鼠中为76:24，在猪中为49:51，在人中为28:72。
The in vitro metabolism of four s-triazine herbicides (atrazine, terbuthylazine, ametryne, and terbutryne) was studied using liver microsomes from rats, pigs, and humans. New HPLC methods with UV detection were developed for the analyses of the incubations. Principal phase I reactions were N-monodealkylation, hydroxylation of the isopropyl or tert-butyl moiety, and sulfoxidation of the substrates in all species. Bidealkylation, 2-hydroxylation, or cleavage of the tert-butyl moiety could not be found in this system. The sulfoxidation of the 2-methylthio-s-triazines exceeded catalysis of the other metabolic reactions by 3-4-fold in all species. In general, all species produced the same types of metabolites, but with species-specific differences in the ratios of the metabolites. Species-specific stereoselective formation of a new chiral isopropyl-hydroxylated metabolite from atrazine was investigated using chiral HPLC techniques. The stereoselective production of this metabolite was different in the different species, with S/R ratios of 76:24 in rats, 49:51 in pigs, and 28:72 in humans.