Department of Biochemistry, Yanka Kupala State University of Grodno, 230030 Grodno, Belarus.
Laboratory of Molecular Biophysics, Department of Microbiology and Biotechnology, Faculty of Biology, University of Bialystok, 15-245 Białystok, Poland.
Molecules. 2023 Jan 27;28(3):1252. doi: 10.3390/molecules28031252.
Search for novel antimicrobial agents, including plant-derived flavonoids, and evaluation of the mechanisms of their antibacterial activities are pivotal objectives. The goal of this study was to compare the antihemolytic activity of flavonoids, quercetin, naringenin and catechin against sheep erythrocyte lysis induced by α-hemolysin (αHL) produced by the strain NCTC 5655. We also sought to investigate the membrane-modifying action of the flavonoids. Lipophilic quercetin, but not naringenin or catechin, effectively inhibited the hemolytic activity of αHL at concentrations (IC = 65 ± 5 µM) below minimal inhibitory concentration values for growth. Quercetin increased the registered bacterial cell diameter, enhanced the fluidity of the inner and surface regions of bacterial cell membranes and raised the rigidity of the hydrophobic region and the fluidity of the surface region of erythrocyte membranes. Our findings provide evidence that the antibacterial activities of the flavonoids resulted from a disorder in the structural organization of bacterial cell membranes, and the antihemolytic effect of quercetin was related to the effect of the flavonoid on the organization of the erythrocyte membrane, which, in turn, increases the resistance of the target cells (erythrocytes) to αHL and inhibits αHL-induced osmotic hemolysis due to prevention of toxin incorporation into the target membrane. We confirmed that cell membrane disorder could be one of the direct modes of antibacterial action of the flavonoids.
寻找新型抗菌剂,包括植物来源的类黄酮,并评估其抗菌活性的机制,是至关重要的目标。本研究的目的是比较类黄酮(槲皮素、柚皮素和儿茶素)对由 NCTC 5655 株产生的α-溶血素(αHL)诱导的绵羊红细胞溶血的抗溶血活性。我们还试图研究类黄酮的膜修饰作用。亲脂性槲皮素而不是柚皮素或儿茶素,在低于最小抑菌浓度值的浓度(IC = 65 ± 5 μM)下有效抑制αHL 的溶血活性。槲皮素增加了登记的细菌细胞直径,增强了细菌细胞膜的内部和表面区域的流动性,并提高了疏水区的刚性和红细胞膜表面区域的流动性。我们的研究结果表明,类黄酮的抗菌活性是由于细菌细胞膜结构组织的紊乱所致,而槲皮素的抗溶血作用与类黄酮对红细胞膜组织的作用有关,这反过来又增加了靶细胞(红细胞)对αHL 的抵抗力,并抑制了由于阻止毒素掺入靶膜而导致的αHL 诱导的渗透性溶血。我们证实,细胞膜紊乱可能是类黄酮的一种直接抗菌作用模式。