Pelkonen O, Sotaniemi E, Mokka R
Chem Biol Interact. 1977 Jan;16(1):13-22. doi: 10.1016/0009-2797(77)90150-8.
The specific metabolism of benzo(a)pyrene (BP) in adult human liver samples was studied by using triated BP and thin-layer chromatographic separation of metabolites and by using the conventional fluorometric assay. The incubation in vitro of BP with human liver homogenates yielded the usual pattern of metabolites, including several dihydrodiols, phenols and quinones, as well as products bound convalently to protein. Interindividual variation in the production of different metabolites were very large, several ten-fold. The over-all metabolism was inhibited by aminopyrine and SKF 525A but not by 7,8-benzoflavone. The formation of dihydrodiols was inhibited by several epoxide hydratase inhibitors with consequent accumulation of phenols and an unidentified metabolite (possibly BP 4,5-oxide). Radiometric measurement of phenols, total dihydrodiols and individual dihydrodiols correlated well with the fluorometric assay of BP hydroxylase activity.
采用氚标记的苯并(a)芘以及代谢物的薄层色谱分离法，并结合传统的荧光测定法，对成人肝脏样本中苯并(a)芘（BP）的特定代谢情况进行了研究。BP与人肝脏匀浆的体外温育产生了常见的代谢物模式，包括几种二氢二醇、酚类和醌类，以及与蛋白质共价结合的产物。不同代谢物生成过程中的个体差异非常大，可达几十倍。氨基比林和SKF 525A可抑制总体代谢，但7,8-苯并黄酮无此作用。几种环氧水合酶抑制剂可抑制二氢二醇的形成，从而导致酚类和一种未鉴定代谢物（可能是BP 4,5-氧化物）的积累。酚类、总二氢二醇和个别二氢二醇的放射性测量与BP羟化酶活性的荧光测定法相关性良好。
