DiGiovanni J, Slaga T J, Berry D L, Juchau M R
Drug Metab Dispos. 1977 May-Jun;5(3):295-301.
The metabolism of 7,12-dimethylbenz[a]anthracene (DMBA) in epidermal homogenates from 3-methylcholanthrene-pretreated mice was analyzed with high-pressure liquid chromatography. Metabolism was undetectable in the absence of pretreatment. Specific activities in epidermal homogenates from pretreated mice were found to be approximately 100 to 1000 times lower than those observed in comparable incubations containing hepatic microsomes from MC-pretreated rats. The major metabolite formed was identified as 7-hydroxymethyl-12-methylbenz[a]anthracene. Each of the known hydroxymethyl metabolites also was present in detectable quantities. The K-region diol was not measurably present in incubations with mouse skin homogenates or rat liver microsomes from MC-pretreated animals. 7,8-Benzoflavone, 5,6-benzoflavone, and 17-beta-estradiol were found to be potent inhibitors of the metabolic transformation of DMBA by epidermal homogenates in vitro, whereas butylated hydroxytoluene and 1,1,1-trichloro-2,3-propene oxide had little effect on or enhanced metabolite formation from DMBA in vitro.
采用高压液相色谱法分析了经3-甲基胆蒽预处理的小鼠表皮匀浆中7,12-二甲基苯并[a]蒽（DMBA）的代谢情况。在未进行预处理时未检测到代谢现象。发现预处理小鼠表皮匀浆中的比活性比在含有经MC预处理大鼠肝微粒体的类似孵育中观察到的比活性低约100至1000倍。形成的主要代谢产物被鉴定为7-羟甲基-12-甲基苯并[a]蒽。每种已知的羟甲基代谢产物也以可检测的量存在。在与经MC预处理动物的小鼠皮肤匀浆或大鼠肝微粒体的孵育中未检测到可测量的K-区域二醇。发现7,8-苯并黄酮、5,6-苯并黄酮和17-β-雌二醇是体外表皮匀浆对DMBA代谢转化的有效抑制剂，而丁基化羟基甲苯和1,1,1-三氯-2,3-环氧丙烷对体外DMBA的代谢产物形成影响很小或有增强作用。
