Faculty of Chemistry, University of Gdansk, Wita Stwosza 63, 80-308 Gdansk, Poland.
Faculty of Chemistry, University of Gdansk, Wita Stwosza 63, 80-308 Gdansk, Poland.
Biochim Biophys Acta Biomembr. 2018 Nov;1860(11):2242-2251. doi: 10.1016/j.bbamem.2018.09.004. Epub 2018 Sep 7.
In this paper, we examine antimicrobial and cytotoxic activities, self-assembly and interactions with anionic and zwitterionic membranes of short arginine-rich lipopeptides: C-RRRR-NH, C-RRRR-NH, C-RRRR-NH, and C-PRRR-NH. They show a tendency to self-assembly into micelles, but it is not required for antimicrobial activity. The membrane binding of the lipopeptides can be accompanied by other factors such as: peptide aggregation, pore formation or micellization of phospholipid bilayer. The shortening of the acyl chain results in compounds with a lower haemolytic activity and a slightly improved antimicrobial activity against Gram-positive bacteria, what indicates enhanced cell specificity. Results of coarse-grained molecular dynamics simulations indicate different organization of membrane lipids upon binding of arginine-based lipopeptides and the previously studied lysine-based ones.
在本文中，我们研究了短精氨酸丰富的脂肽：C-RRRR-NH、C-RRRR-NH、C-RRRR-NH 和 C-PRRR-NH 的抗菌和细胞毒性活性、自组装以及与阴离子和两性离子膜的相互作用。它们表现出自组装成胶束的趋势，但这不是抗菌活性所必需的。脂肽与膜的结合可能伴随着其他因素，如：肽聚集、孔形成或磷脂双层的胶束化。酰链的缩短导致化合物的溶血活性降低，对革兰氏阳性菌的抗菌活性略有提高，这表明细胞特异性增强。粗粒度分子动力学模拟的结果表明，在结合精氨酸脂肽和之前研究的赖氨酸脂肽时，膜脂的组织方式不同。
