Department of Chemistry, University of Nevada, Reno, Reno, Nevada.
Department of Biochemistry and Molecular Biology, University of Nevada, Reno, Nevada.
Biophys J. 2019 Mar 19;116(6):1064-1074. doi: 10.1016/j.bpj.2019.02.005. Epub 2019 Feb 15.
Bombolitins, a class of peptides produced by bees of the genus Bombus, target and disrupt cellular membranes, leading to lysis. Antimicrobial peptides exhibit various mechanisms of action resulting from the interplay between peptide structure, lipid composition, and cellular target membrane selectivity. Herein, two bombolitins displaying significant amino-acid-sequence similarity, BII and BL6, were assessed for antimicrobial activity as well as correlated dodecylphosphocholine (DPC) micelle binding and membrane-induced peptide conformational changes. Infrared and circular dichroism spectroscopies were used to assess the structure-function relationship of each bombolitin, and the results indicate that BII forms a rigid and helically ordered secondary structure upon binding to DPC micelles, whereas BL6 largely lacks secondary structural order. Moreover, the binding affinity of each peptide to DPC micelles was determined, revealing that BL6 displayed a difference in binding affinity by over two orders of magnitude. Further investigations into the growth-inhibitory activity of the two bombolitins were performed against Escherichia coli and Saccharomyces cerevisiae. Interestingly, BII specifically targeted S. cerevisiae, whereas BL6 more effectively inhibited E. coli growth. Overall, the antimicrobial selectivity and specificity of BII and BL6 are largely dependent on the primary as well as secondary structural content of the peptides and the membrane composition.
蜂皇肽是由蜜蜂属(Bombus)产生的一类肽,靶向并破坏细胞膜,导致裂解。抗菌肽具有多种作用机制,这些机制是由肽结构、脂质组成和细胞靶膜选择性之间的相互作用产生的。本文评估了两种具有显著氨基酸序列相似性的蜂皇肽 BII 和 BL6 的抗菌活性以及相关的十二烷基磷酸胆碱(DPC)胶束结合和膜诱导肽构象变化。红外和圆二色性光谱用于评估每种蜂皇肽的结构-功能关系,结果表明 BII 在与 DPC 胶束结合时形成刚性和螺旋有序的二级结构,而 BL6 则缺乏二级结构有序性。此外,还确定了每种肽与 DPC 胶束的结合亲和力,表明 BL6 的结合亲和力差异超过两个数量级。进一步研究了两种蜂皇肽对大肠杆菌和酿酒酵母的生长抑制活性。有趣的是,BII 特异性靶向 S. cerevisiae,而 BL6 更有效地抑制 E. coli 的生长。总的来说,BII 和 BL6 的抗菌选择性和特异性在很大程度上取决于肽的一级和二级结构含量以及膜组成。