Enzymatic reduction of chloramphenicol and nitrosochloramphenicol by rat liver microsomal preparations.
Enzymatic reduction of chloramphenicol and nitrosochloramphenicol by rat liver microsomal preparations.
复制标题
大鼠肝微粒体制剂酶促还原氯霉素和亚硝基氯霉素。
作者：
Lim,LO;Yunis,AA
氯霉素（CAP）和亚硝基氯霉素（NO-CAP）在体外经大鼠肝微粒体代谢还原为芳香胺。还原需要厌氧条件，并由nadph依赖性还原酶系统介导。CAP和NO-CAP的减少都是时间和浓度依赖的。与CAP相比，NO-CAP （0.5 mM）的还原速度很快，在90-120分钟内发生完全转化。在250毫米时，no - cap减少量下降。NO-CAP （0.05 ~ 2.5 mM）存在时，CAP代谢被抑制17% ~ 91%。这些结果表明，CAP和NO-CAP是由相似的微粒体还原酶系统代谢的，NO-CAP是不稳定的，很容易进一步还原为芳香胺。
Chloramphenicol (CAP) and nitrosochloramphenicol (NO-CAP) were metaboli-cally reduced to aromatic amines by rat liver microsomes in vitro. The reduction required anaerobic conditions and was mediated by a NADPH-dependent reductase system. Both CAP and NO-CAP reduction were time and concentration dependent. Compared to CAP, NO-CAP (0.5 mM) reduction was rapid with complete conversion occurring in 90–120 min. At 2.5 mMNO-CAP reduction was depressed. In the presence of NO-CAP (0.05–2.5 mM) CAP metabolism was inhibited from 17 to 91 %. These results indicate that CAP and NO-CAP are metabolized by similar microsomal reductase systems and NO-CAP is unstable, readily reduced further to the aromatic amine.