Department of Pharmacy and Pharmacology, University of Bath, Bath, BA2 7AY, UK.
Biometals. 2021 Apr;34(2):315-328. doi: 10.1007/s10534-020-00281-x. Epub 2021 Jan 11.
Iron is an essential nutrient for virtually all microbes and limiting the concentration of available iron is a potential strategy to be used as an alternative to antibiotic treatment. In this study we analysed the antimicrobial activity of two chelators, specifically 3-hydroxy-1,2-dimethyl-4(1H)-pyridone (deferiprone, DFP), which is clinically approved for the treatment of iron overload disorders, and its 1,2-diethyl homologue, CP94. Both compounds showed moderate activity towards planktonically growing P. aeruginosa cells, and the mechanism of action of these chelators was indeed by limiting the amount of free iron. Surprisingly, the compounds behaved very differently when the cells were grown in biofilms. DFP also showed inhibitory effects on biofilm formation but in contrast, CP94 stimulated this process, in particular at high concentrations. We hypothesised that CP94 behaves as an iron carrier, which was confirmed by our observation that it had antimicrobial synergy with the toxic metals, gallium and copper. This suggests that P. aeruginosa produces a biofilm-specific transport protein that recognises CP94 but not the closely related compound DFP.
铁是几乎所有微生物的必需营养物质,限制可用铁的浓度是一种潜在的策略,可以替代抗生素治疗。在这项研究中,我们分析了两种螯合剂的抗菌活性,特别是临床上用于治疗铁过载疾病的 3-羟基-1,2-二甲基-4(1H)-吡啶酮(地拉罗司,DFP)及其 1,2-二乙基同系物 CP94。这两种化合物对浮游生长的铜绿假单胞菌细胞都表现出中等活性,这些螯合剂的作用机制确实是通过限制游离铁的含量。令人惊讶的是,当细胞在生物膜中生长时,这些化合物的行为非常不同。DFP 也显示出对生物膜形成的抑制作用,但相反,CP94 刺激了这个过程,特别是在高浓度时。我们假设 CP94 作为一种铁载体,这一点得到了我们的观察结果的证实,即它与有毒金属镓和铜具有协同抗菌作用。这表明铜绿假单胞菌产生了一种生物膜特异性的转运蛋白,它可以识别 CP94,但不能识别密切相关的化合物 DFP。