Kohanski Michael A, Dwyer Daniel J, Hayete Boris, Lawrence Carolyn A, Collins James J
Center for BioDynamics and Center for Advanced Biotechnology, Boston University, Boston, MA 02215, USA.
Cell. 2007 Sep 7;130(5):797-810. doi: 10.1016/j.cell.2007.06.049.
Antibiotic mode-of-action classification is based upon drug-target interaction and whether the resultant inhibition of cellular function is lethal to bacteria. Here we show that the three major classes of bactericidal antibiotics, regardless of drug-target interaction, stimulate the production of highly deleterious hydroxyl radicals in Gram-negative and Gram-positive bacteria, which ultimately contribute to cell death. We also show, in contrast, that bacteriostatic drugs do not produce hydroxyl radicals. We demonstrate that the mechanism of hydroxyl radical formation induced by bactericidal antibiotics is the end product of an oxidative damage cellular death pathway involving the tricarboxylic acid cycle, a transient depletion of NADH, destabilization of iron-sulfur clusters, and stimulation of the Fenton reaction. Our results suggest that all three major classes of bactericidal drugs can be potentiated by targeting bacterial systems that remediate hydroxyl radical damage, including proteins involved in triggering the DNA damage response, e.g., RecA.
抗生素作用模式分类是基于药物与靶点的相互作用以及由此产生的细胞功能抑制对细菌是否具有致死性。我们在此表明,三类主要的杀菌抗生素,无论药物与靶点的相互作用如何,都会在革兰氏阴性菌和革兰氏阳性菌中刺激产生高度有害的羟基自由基,这最终导致细胞死亡。相比之下,我们还表明抑菌药物不会产生羟基自由基。我们证明,杀菌抗生素诱导羟基自由基形成的机制是氧化损伤细胞死亡途径的最终产物,该途径涉及三羧酸循环、NADH的短暂消耗、铁硫簇的不稳定以及芬顿反应的刺激。我们的结果表明,通过靶向修复羟基自由基损伤的细菌系统,包括参与触发DNA损伤反应的蛋白质(如RecA),所有三类主要的杀菌药物都可以得到增强。