Jellinck P H, Smith G, Newcombe A M
Chem Biol Interact. 1975 Nov;11(5):459-68. doi: 10.1016/0009-2797(75)90013-7.
A close correlation has been observed between the ability of aromatic polycyclic hydrocarbons and 7,8-benzoflavone (7,8-BF) to induce hepatic aryl hydrocarbon hydroxylase (AHH) in vivo and to inhibit the induced enzyme system in vitro. The activity of this mono-oxygenase was measured by the conversion of 14C-labeled dimethylbenz(a)anthracene (DMBA) or benzo(a)pyrene (BP) to water-soluble products by rat liver preparations (8000 X g supernatant). DMBA as substrate had the advantage over BP in giving a wider range of ethyl acetate-soluble metabolites and allowing the observation of changes in the pattern of these products following injection or addition of the inducing agents. This property was used to detect low concentration (0.1 muM) of polycyclic hydrocarbons which are strong AHH inducers and which may also be carcinogenic. The liver preparation was active for several months when stored at --20 degrees. A possible mechanism of action for the in vitro behaviour of polycyclic hydrocarbons and 7,8-BF towards AHH is proposed.
已观察到芳香族多环烃和7,8 - 苯并黄酮（7,8 - BF）在体内诱导肝芳烃羟化酶（AHH）以及在体外抑制诱导酶系统的能力之间存在密切相关性。通过大鼠肝脏制剂（8000×g上清液）将14C标记的二甲基苯并(a)蒽（DMBA）或苯并(a)芘（BP）转化为水溶性产物来测定这种单加氧酶的活性。以DMBA作为底物比BP更具优势，因为它能产生范围更广的乙酸乙酯可溶性代谢物，并能观察到在注射或添加诱导剂后这些产物模式的变化。利用这一特性来检测低浓度（0.1μM）的多环烃，这些多环烃是强效AHH诱导剂，也可能具有致癌性。肝脏制剂在-20℃储存时可保持活性数月。本文提出了多环烃和7,8 - BF对AHH体外作用的一种可能作用机制。
