Razzouk C, Agazzi-Léonard E, Batardy-Grégoire M, Mercier M, Poncelet F, Roberfroid M
Toxicol Lett. 1980 Jan;5(1):61-7. doi: 10.1016/0378-4274(80)90149-6.
The kinetic properties of the N-hydroxylation of 2-acetylaminofluorene (2-AAF) are studied with microsomal preparations of livers from both control and 3-methylcholanthrene (3-MC)-pretreated rats and hamsters. The level of basal enzymatic activity is higher in hamster than in rat liver; 3-MC induces the activity in both animals. When added in vitro to incubation mixture, 3-MC competitively inhibits the N-hydroxylase activity. When fed to rats simultaneously with 2-AAF, 3-MC suppresses the carcinogenicity of the acetylated arylamine by inhibiting the first step in its activation pathway. Hamster tissues are not protected by this pretreatment because the level of N-hydroxylase activity is too high.
利用来自对照大鼠和仓鼠以及经3-甲基胆蒽（3-MC）预处理的大鼠和仓鼠肝脏的微粒体制剂，研究了2-乙酰氨基芴（2-AAF）N-羟基化的动力学特性。仓鼠肝脏中基础酶活性水平高于大鼠肝脏；3-MC可诱导两种动物的该活性。当在体外添加到孵育混合物中时，3-MC竞争性抑制N-羟化酶活性。当与2-AAF同时喂给大鼠时，3-MC通过抑制其活化途径的第一步来抑制乙酰化芳胺的致癌性。仓鼠组织不受这种预处理的保护，因为N-羟化酶活性水平过高。
