Müller M
Surgery. 1983 Jan;93(1 Pt 2):165-71.
Metronidazole and related 5-nitroimidazoles are relatively nontoxic. Reduction of their nitro group, however, leads to the production of short-lived cytotoxic intermediates, which finally decompose into nontoxic end products. The toxicity of the intermediates is due to their interaction with deoxyribonucleic acid and possibly with other macromolecules. Metabolic pathways of low redox potential that are linked to ferredoxin or flavodoxin-like electron transport components reduce nitroimidazoles with great efficacy. Such pathways are characteristic of susceptible anaerobic protozoa and bacteria and are absent in nonsusceptible aerobic cells of the host.
甲硝唑及相关的5-硝基咪唑类药物相对无毒。然而,其硝基的还原会导致产生寿命短暂的细胞毒性中间体,这些中间体最终分解为无毒的终产物。中间体的毒性是由于它们与脱氧核糖核酸以及可能与其他大分子相互作用所致。与铁氧化还原蛋白或类黄素氧化还原蛋白样电子传递成分相关的低氧化还原电位代谢途径能高效还原硝基咪唑类药物。此类途径是易感厌氧原生动物和细菌所特有的,而在宿主的非易感需氧细胞中不存在。