Salem Z, Murray T, Yunis A A
J Lab Clin Med. 1981 Jun;97(6):881-6.
Fresh-frozen human liver tissue was assayed for its ability to reduce the nitrogroup of R--NO2 to the amine. All 10 livers examined exhibited demonstrable reductase activity. The reduction was potentiated by NADPH and abolished by boiling the liver homogenates. The nitroreductase activity varied among the different livers by as much as severalfold. These findings show that ability of the human liver to reduce R--NO2 and support the hypothesis that certain toxic intermediates of the nitroreduction of R--NO2 may be responsible for the aplastic anemia associated with this drug.
对新鲜冷冻的人体肝脏组织进行了检测,以评估其将R-NO2的硝基还原为胺的能力。所检测的全部10个肝脏均表现出可证实的还原酶活性。NADPH可增强这种还原作用,而将肝脏匀浆煮沸则可消除这种还原作用。不同肝脏之间的硝基还原酶活性差异高达数倍。这些发现表明人体肝脏具有还原R-NO2的能力,并支持以下假说:R-NO2硝基还原的某些毒性中间体可能是导致与该药物相关的再生障碍性贫血的原因。