Tsyrlov I B, Rivkind N B, Lyakhovich V V
Biol Bull Acad Sci USSR. 1979 Jan-Feb;6(1):28-34.
The severity of the induced effect of the polycyclic hydrocarbon 3-methylcholanthrene on monooxygenase of the microsomal fraction of the liver as a function of the number of binding sites for this inducer in the active site of cytochrome P-450 was investigated. In vivo models, in which the primary bounding and metabolism of a polycyclic hydrocarbon in the microsomes is increased or sharply inhibited, are presented. It is concluded that in the mechanism of induction by 3-methylcholanthrene, the activation of synthesis of specific protein (cytochrome P-448) is accomplished not by the initial molecule of the inducer, but by products of its primary metabolism in the microsomes.
研究了多环烃3-甲基胆蒽对肝脏微粒体部分单加氧酶的诱导作用强度与该诱导剂在细胞色素P-450活性位点结合位点数量之间的关系。文中介绍了体内模型,在这些模型中,多环烃在微粒体中的初级结合和代谢会增加或受到显著抑制。得出的结论是,在3-甲基胆蒽的诱导机制中,特定蛋白质(细胞色素P-448)合成的激活不是由诱导剂的初始分子完成的,而是由其在微粒体中的初级代谢产物完成的。