Department of Membrane Transport, Division BIOCEV, Institute of Physiology of the Czech Academy of Sciences, Průmyslová 595, 252 50 Vestec, Czech Republic.
Department of Membrane Transport, Division BIOCEV, Institute of Physiology of the Czech Academy of Sciences, Průmyslová 595, 252 50 Vestec, Czech Republic.
Biochim Biophys Acta Biomembr. 2017 Oct;1859(10):1851-1858. doi: 10.1016/j.bbamem.2017.06.005. Epub 2017 Jun 7.
We compared the potency of four derivatives of the antimicrobial peptide halictine-2 against six Candida species. Observed activity was peptide and species specific. Halictines rapidly permeabilized cell membranes and caused the leakage of cytosolic components. Their killing potential was enhanced by the commercial antimicrobial agent octenidine dihydrochloride. The effect on C. glabrata cells did not depend on the activity of Cdr pumps, but was influenced by their lipid composition. The pre-treatment of cells with myriocin, an inhibitor of sphingolipid synthesis, enhanced the peptides' activity, whereas pre-treatment with terbinafine and fluconazole, inhibitors of sterol synthesis, significantly weakened their efficacy. The killing efficacy of peptides increased in combination with amphotericin B. Thus the mode of action of halictines is likely to depend on the plasma-membrane sterols, which might explain the observed differences among the tested Candida species.
我们比较了四种抗菌肽 halictine-2 的衍生物对六种念珠菌的效力。观察到的活性是肽和物种特异性的。Halictines 迅速穿透细胞膜并导致细胞溶质成分泄漏。它们的杀菌潜力通过商业抗菌剂奥替尼啶二盐酸盐得到增强。对 C. glabrata 细胞的影响不依赖于 Cdr 泵的活性，但受其脂质组成的影响。用鞘氨醇合成抑制剂 myriocin 预处理细胞可增强肽的活性，而用抑制固醇合成的 terbinafine 和 fluconazole 预处理则显著降低其功效。与两性霉素 B 联合使用时，肽的杀菌效果增加。因此，halictines 的作用模式可能依赖于质膜固醇，这可能解释了测试的念珠菌物种之间的观察到的差异。
