Blaich G, Göttlicher M, Cikryt P, Metzler M
Institute of Pharmacology and Toxicology, University of Würzburg, FRG.
Eur J Drug Metab Pharmacokinet. 1987 Oct-Dec;12(4):259-62. doi: 10.1007/BF03189909.
Pretreatment of male Syrian golden hamsters with 7,8-benzoflavone (7,8-BF) leads to a marked increase of cytochrome P450 and cytochrome b5 levels in the liver, whereas phenobarbital (PB) and 3-methylcholanthrene (MC) induce cytochrome P450 but not cytochrome b5 7,8-BF pretreatment has only minor effects on the activities of aryl hydrocarbon hydroxylase and 7-ethoxycoumarin-O-deethylase, but 7-ethoxyresorufin-O-deethylase is increased 3-fold. In contrast to PB, pretreatment with 7,8-BF or MC reduces the oxidative metabolism of diethylstilbestrol (DES) by hepatic microsomes in vitro. The cytosolic level of the aromatic hydrocarbon (Ah) receptor in hamster liver is decreased by 7,8-BF and slightly enhanced by MC pretreatment. PB increases the receptor level 1.5-fold. The affinity of 7,8-BF to the Ah receptor in vitro is of the same order of magnitude as that of the known ligands 5,6-benzoflavone and 2,3,7,8-tetrachlorodibenzofurane. PB and DES show no binding to the receptor protein.
用7,8-苯并黄酮（7,8-BF）对雄性叙利亚金黄地鼠进行预处理会导致肝脏中细胞色素P450和细胞色素b5水平显著增加，而苯巴比妥（PB）和3-甲基胆蒽（MC）诱导细胞色素P450但不诱导细胞色素b5。7,8-BF预处理对芳烃羟化酶和7-乙氧基香豆素-O-脱乙基酶的活性只有轻微影响，但7-乙氧基试卤灵-O-脱乙基酶增加了3倍。与PB相反，用7,8-BF或MC预处理会降低体外肝微粒体对己烯雌酚（DES）的氧化代谢。7,8-BF可降低仓鼠肝脏中芳烃（Ah）受体的胞质水平，而MC预处理则使其略有升高。PB使受体水平增加1.5倍。7,8-BF在体外对Ah受体的亲和力与已知配体5,6-苯并黄酮和2,3,7,8-四氯二苯并呋喃的亲和力处于同一数量级。PB和DES与受体蛋白无结合。
