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首页> 外文期刊>Environmental toxicology and chemistry >SEMIPREPARATIVE ENANTIOSEPARATION OF METHAMIDOPHOS BY HPLC-UV AND PRELIMINARY IN VITRO STUDY OF BUTYRYLCHOLINESTERASE INHIBITION
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SEMIPREPARATIVE ENANTIOSEPARATION OF METHAMIDOPHOS BY HPLC-UV AND PRELIMINARY IN VITRO STUDY OF BUTYRYLCHOLINESTERASE INHIBITION

机译：高效液相色谱-紫外半定量对苯二酚的对映体分离及对丁酰胆碱酯酶抑制作用的体外初步研究

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摘要

Many chiral pesticides are introduced into the environment as racemates, although their pesticidal activity is usually the result of preferential reactivity of only one enantiomer, while the other enantiomer may have toxic effects against nontarget organisms. Methamidophos (O,S-dimethyl phosphoratnidothioate), a chiral compound, is an insecticide widely used in agriculture in both developed and developing countries. However, this pesticide has a high toxicity not only to targeted insects but also to human and animals. In the present study, the enantiomers of methamidophos were cnantiomerically separated by a sernipreparative chirat liquid chromatography at the multimilligram scale on a polysaccharide-based chiral stationary phase and a preliminary evaluation of their in vitro inhibition of plasma butyrylcholinesterase (BChE) of hens was performed. In the present study, our first effort was to resolve the racemic mixture of methamidophos and to that end reversed-phase, normal-phase, and polar organic elution conditions were investigated in four different polysaccharide-based chiral phases. The best performance was achieved on a cellulose tris(3,5-dimethylphenylcarba-mate) phase under normal phase. This chromatographic condition allowed the separation of 225 mg of methamidophos enantiomers with a high degree of chiral purity (>98%) in a short analysis time. Significant differences were found between the concentration that causes 50% of enzyme inhibition (IC50) of the three isoforms of methamidophos. (-)-Methamidophos showed an IC50 approximately three times larger than the (+)-enantiomer for plasma BChE of hens.
机译：尽管手性农药的杀虫活性通常是仅一种对映异构体优先发生反应的结果，而另一种对映异构体可能对非目标生物具有毒性作用，但许多手性农药却以消旋体形式引入环境。甲胺磷（O，S-二甲基磷酰胺基硫酸酯）是一种手性化合物，是发达国家和发展中国家农业中广泛使用的杀虫剂。但是，该农药不仅对目标昆虫具有高毒性，而且对人和动物具有高毒性。在本研究中，甲胺磷的对映异构体在多糖基手性固定相上以毫克级规模通过Sernipreparative Chirat液相色谱进行对映体拆分，并对其体外抑制母鸡血浆丁酰胆碱酯酶（BChE）进行了初步评估。在本研究中，我们的首要工作是解决甲胺磷的外消旋混合物，并为此在四种基于多糖的手性相中研究了反相，正相和极性有机洗脱条件。在正相下的纤维素三（3,5-二甲基苯基氨基甲酸酯）相上获得了最佳性能。此色谱条件可在短时间内分离出225 mg甲氨磷的对映异构体，具有较高的手性纯度（> 98％）。在引起甲胺磷的三种亚型的酶抑制（IC50）50％的浓度之间发现了显着差异。 （-）-甲胺磷的IC50约为母鸡血浆BChE的（+）-对映异构体的三倍。

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