Abakumova O Iu, Kutsenko N G, Lerman M I
Biokhimiia. 1978 Nov;43(11):2092-9.
N-methyl-N-nitrosourea is metabolised by mouse liver microsomes yielding highly reactive product(s) capable of alkylating cellular macromolecules. Based on cofactor requirement (NADPH, oxygen), inhibition (NaN3) and induction by phenobarbital, 3,4-benz(a)pyrene, and MNU, the reaction is cytochrome P-450-dependent. Analysis of the kinetics and dose dependence of alkylation in vivo and in tissue homogenates confirms the fact that MNU must undergo metabolic activation in vivo.
N-甲基-N-亚硝基脲在小鼠肝脏微粒体中代谢,产生能够烷基化细胞大分子的高活性产物。根据辅因子需求(NADPH、氧气)、抑制作用(叠氮化钠)以及苯巴比妥、3,4-苯并(a)芘和N-甲基-N-亚硝基脲的诱导作用,该反应是细胞色素P-450依赖性的。体内和组织匀浆中烷基化动力学和剂量依赖性分析证实了N-甲基-N-亚硝基脲在体内必须经过代谢活化这一事实。