Kapitulnik J, Poppers P J, Buening M K, Fortner J G, Conney A H
Clin Pharmacol Ther. 1977 Oct;22(4):475-84. doi: 10.1002/cpt1977224475.
Addition of 10(-4) M 7,8-benzoflavone to homogenates of human liver samples obtained by autopsy or surgical biopsy increased the rate of benzo[a]pyrene hydroxylation up to 11-fold. 7,8-Benzoflavone also increased the rates of hydroxylation of zoxazolamine and antipyrine at 10(-4) M but inhibited these reactions at 10(-6) M. The effects of 7,8-benzoflavone on the hydroxylation of benzo[a]pyrene and zoxazolamine in microsomes from human liver were similar to those in homogenates. Addition of 7,8-benzoflavone to homogenates of surgical biopsy samples of human liver had little or no effect on the rates of oxidative metabolism of 7-ethoxycoumarin, coumarin, and hexobarbital. Marked individuality for the activating and inhibiting effects of 7,8-benzoflavone was observed in different liver samples. This individuality may result both from the presence of multiple monooxygenases in varying amounts and proportions in the different liver samples and from a selective effect of 7,8-benzoflavone on certain of the monooxygenases.
向通过尸检或手术活检获得的人肝脏样本匀浆中添加10⁻⁴ M的7,8-苯并黄酮，可使苯并[a]芘的羟化速率提高至11倍。7,8-苯并黄酮在10⁻⁴ M时也能提高唑沙宗和安替比林的羟化速率，但在10⁻⁶ M时会抑制这些反应。7,8-苯并黄酮对人肝脏微粒体中苯并[a]芘和唑沙宗羟化的影响与在匀浆中的情况相似。向人肝脏手术活检样本匀浆中添加7,8-苯并黄酮对7-乙氧基香豆素、香豆素和己巴比妥的氧化代谢速率几乎没有影响。在不同的肝脏样本中观察到7,8-苯并黄酮的激活和抑制作用存在明显的个体差异。这种个体差异可能是由于不同肝脏样本中多种单加氧酶的含量和比例不同，以及7,8-苯并黄酮对某些单加氧酶的选择性作用所致。
