Université de Strasbourg/CNRS, UMR7177, Institut de Chimie, Strasbourg, France.
Antimicrob Agents Chemother. 2013 Jul;57(7):2955-66. doi: 10.1128/AAC.02498-12. Epub 2013 Apr 15.
Hydramacin-1 (HM1) from the metazoan Hydra exerts antimicrobial activity against a wide range of bacterial strains. Notably, HM1 induces the aggregation of bacterial cells, accompanied by precipitation. To date, the proposed mechanism of peptide-lipid interaction, termed the barnacle model, has not been described on the molecular level. Here, we show by biochemical and biophysical techniques that the lipid-peptide interactions of HM1 are initiated by electrostatic and hydrophobic effects, in particular, by tryptophan and neighboring polar amino acid residues that cause an interfacial localization of the peptide between two self-contained lipid bilayers. The high binding constants of HM1 upon lipid interaction are in the range of other potent antimicrobial peptides, e.g., magainin, and can be reasonably explained by two distinct epitopes on the surface of the peptide's global structure, which both contain SWT(K/R) motifs. The residues of this motif favor localization of the peptide in the head group region of phospholipid bilayers up to a penetration depth of 4 Å and a minor participation of the lipids' hydrocarbon regions. Our results expand the knowledge about the molecular modes of action antimicrobial peptides use to tackle their target cells. Furthermore, the aggregation of living bacteria by HM1 was observed for a broad range of Gram-positive and Gram-negative bacteria. Therefore, the detailed view of peptide-lipid interactions described by the barnacle model consolidates it among the established models.
来自后生动物水螅的 Hydramacin-1(HM1)对多种细菌菌株具有抗菌活性。值得注意的是,HM1 诱导细菌细胞聚集,并伴有沉淀。迄今为止,肽-脂相互作用的拟议机制,称为藤壶模型,尚未在分子水平上进行描述。在这里,我们通过生化和生物物理技术表明,HM1 的脂质-肽相互作用是通过静电和疏水作用引发的,特别是通过色氨酸和相邻的极性氨基酸残基引起肽在两个自包含脂质双层之间的界面定位。HM1 与脂质相互作用的高结合常数在其他强效抗菌肽(例如,magainin)的范围内,可以通过肽的全局结构表面上的两个不同表位来合理地解释,这两个表位都含有 SWT(K/R)基序。该基序的残基有利于肽在磷脂双层的头部基团区域中定位,直到穿透深度为 4 Å,并且脂质的烃区域的参与较小。我们的结果扩展了关于抗菌肽用于解决其靶细胞的分子作用模式的知识。此外,HM1 观察到广泛的革兰氏阳性和革兰氏阴性细菌的活细菌聚集。因此,藤壶模型所描述的肽-脂相互作用的详细观点使其在已建立的模型中得到巩固。