Byus C V, Costa M, Sipes I G, Brodie B B, Russell D H
Proc Natl Acad Sci U S A. 1976 Apr;73(4):1241-5. doi: 10.1073/pnas.73.4.1241.
The parenteral administration of a single dose of 3-methylcholanthrene to rats caused an increase in the liver of the concentration of 3', 5'-cAMP and of the activity of cAMP-dependent protein kinase (ATP:protein phosphotransferase, EC 2.7.1.37). These events were followed by an increased activity of ornithine decarboxylase (L-ornithine carboxy-lase, EC 4.1.1.17), the enzyme that controls the biosynthesis of polyamines. Finally, the activity of benzo[a]pyrene hydroxylase, as well as the amount of cytochrome P-448, was increased. Similarly, after the administration of phenobarbital, there was first an increase in the cAMP concentration and in the activity of cAMP-dependent protein kinase, then the induction of ornithine decarboxylase, and finally, an enhanced activity of ethylmorphine N-demethylase and an increased content of cytochrome P-450. These data suggest that the drug-induced processes in liver that increase the activities of the oxidative, and presumably other, drug-metabolizing enzymes include the following sequence of events: (1) increase in cAMP concentration and/or activation of cAMP-dependent protein kinase; (2) induction of ornithine decarboxylase; and, (3) induction of drug-metabolizing enzymes.
给大鼠单次肠胃外注射3-甲基胆蒽,会导致其肝脏中3',5'-环磷酸腺苷(3',5'-cAMP)的浓度以及环磷酸腺苷依赖性蛋白激酶(ATP:蛋白磷酸转移酶,EC 2.7.1.37)的活性增加。这些变化之后,鸟氨酸脱羧酶(L-鸟氨酸羧化酶,EC 4.1.1.17)的活性增强,该酶控制着多胺的生物合成。最后,苯并[a]芘羟化酶的活性以及细胞色素P-448的量增加。同样,给予苯巴比妥后,首先是环磷酸腺苷浓度和环磷酸腺苷依赖性蛋白激酶的活性增加,接着是鸟氨酸脱羧酶的诱导,最后是乙基吗啡N-脱甲基酶的活性增强以及细胞色素P-450含量增加。这些数据表明,药物诱导肝脏中氧化酶以及可能其他药物代谢酶活性增加的过程包括以下一系列事件:(1)环磷酸腺苷浓度增加和/或环磷酸腺苷依赖性蛋白激酶激活;(2)鸟氨酸脱羧酶的诱导;以及(3)药物代谢酶的诱导。