Cresteil T, Lesca P
Chem Biol Interact. 1983 Nov;47(2):145-56. doi: 10.1016/0009-2797(83)90154-0.
Pretreatment of rats by ellipticines enhanced the microsomal concentration of cytochrome P-450, benzo[alpha]pyrene (BP) metabolism and activation and, a smaller extent, ethoxycoumarin deethylation, but not acetanilide hydroxylation. This increased BP biotransformation was essentially due to the formation of bay-region metabolites, BP 9,10-diol, BP 7,8-diol and 9-hydroxy-BP, or to the formation of BP 7,8-diol-9,10-epoxide- and of 9-hydroxy-BP 4,5-oxide-DNA adducts. In the ellipticine series, 9-fluoroellipticine (9-FE) presents a slight inducing potency compared with the parent and 9-hydroxy molecules. Pretreatment of mice with 9-hydroxyellipticine (9-OHE) led also to an increased mutagenicity of BP and to an augmentation of skin carcinogenesis by 7,12-dimethylbenz[alpha]anthracene (DMBA). These results clearly show that 9-OHE induces the biosynthesis of cytochrome P-450 which markedly stimulates the mutagenic and carcinogenic potentialities of polycyclic aromatic hydrocarbons (PAH).
用玫瑰树碱对大鼠进行预处理可提高微粒体细胞色素P - 450的浓度、苯并[a]芘（BP）的代谢与活化，在较小程度上还可提高乙氧香豆素脱乙基作用，但对乙酰苯胺羟基化作用无影响。这种BP生物转化的增加主要是由于湾区代谢物的形成，如BP 9,10 -二醇、BP 7,8 -二醇和9 -羟基 - BP，或由于BP 7,8 -二醇 - 9,10 -环氧化物和9 -羟基 - BP 4,5 -氧化物 - DNA加合物的形成。在玫瑰树碱系列中，与母体和9 -羟基分子相比，9 -氟玫瑰树碱（9 - FE）的诱导能力较弱。用9 -羟基玫瑰树碱（9 - OHE）对小鼠进行预处理也会导致BP的致突变性增加以及7,12 -二甲基苯并[a]蒽（DMBA）引起的皮肤致癌作用增强。这些结果清楚地表明，9 - OHE诱导细胞色素P - 450的生物合成，这显著刺激了多环芳烃（PAH）的致突变和致癌潜力。
