Studies on the metabolism of diethyl 4-nitrophenyl phosphorothionate (parathion) in vitro.
Studies on the metabolism of diethyl 4-nitrophenyl phosphorothionate (parathion) in vitro.
复制标题
4-硝基苯基硫代磷酸二乙酯（对硫磷）体外代谢的研究。
作者：
R. A. Neal
1.通过使用[（32）P]硫代磷酸根离子和从各种动物肝脏中分离的微粒体，检查了硫代磷酸根离子的体外代谢。2.经体外代谢产物分析，确定了磷酰氧磷在该体系中的主要代谢产物为对硝基苯磷酸二乙酯、磷酸氢二乙酯、硫代磷酸氢二乙酯和对硝基苯酚。3.导致硫代磷酸氢二乙酯和对硝基苯酚形成的反应需要将氯磷定代谢为其活性抗乙酰胆碱酯酶对氧磷所需的相同辅因子（NADPH和氧）。4.用苯巴比妥和3，4-苯并芘对雄性大鼠进行预处理，使每单位重量肝脏中的酶活性增加约65-130%。5.通过在氮气气氛和含一氧化碳气氛中孵育，可抑制氯磷定的代谢。纯氧也有抑制作用。这些结果进行了讨论的最大活动，以及系统的某些组件的氧化不稳定性的氧不足。
1. The metabolism of the phosphorothionate parathion in vitro was examined by using [(32)P]parathion and microsomes isolated from the livers of various animal species. 2. The major metabolic products of parathion in this system in vitro were identified as diethyl 4-nitrophenyl phosphate (paraoxon), diethyl hydrogen phosphate, diethyl hydrogen phosphorothionate and p-nitrophenol. 3. The reaction leading to the formation of diethyl hydrogen phosphorothionate and p-nitrophenol requires the same cofactors (NADPH and oxygen) required for metabolism of parathion to its active anti-acetylcholinesterase paraoxon. 4. The enzyme activity towards parathion per unit weight of liver is increased some 65-130% by pretreatment of male rats with phenobarbital and 3,4-benzopyrene. 5. The metabolism of parathion is inhibited by incubation in a nitrogen atmosphere and in an atmosphere containing carbon monoxide. Pure oxygen is also inhibitory. These results are discussed in terms of a deficiency of oxygen for maximal activity as well as the lability of some component of the system to oxidation.