Self-Assembly and Antimicrobial Activity of Lipopeptides Containing Lysine-Rich Tripeptides
Self-Assembly and Antimicrobial Activity of Lipopeptides Containing Lysine-Rich Tripeptides
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DOI：
10.1021/acs.biomac.3c01184
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发表时间：
2024-01-11
影响因子：
6.2
通讯作者：
Hamley，Ian W.
中科院分区：
文献类型：
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作者：
Adak，Anindyasundar;Castelletto，Valeria;Hamley，Ian W.
采用光谱学、低温透射电镜（cro - tem）和小角x射线散射（SAXS）相结合的方法研究了两对模型脂化三肽在水溶液中的构象和自组装。棕榈酰化脂肽包括C16-YKK或C16-WKK（具有双赖氨酸残基）或它们各自含有d-赖氨酸(k)的衍生物，即C16-YKK和C16-WKK。这四种分子自组装成球形胶束，由于水溶液中胶束间的堆积，在SAXS剖面中表现出结构因子效应。与胶束结构一致，冠状中的三肽具有很大程度上的无序构象，用光谱方法探测。在足够低的浓度下，发现这些分子与成纤维细胞具有良好的细胞相容性，尽管在检测的最高浓度下（高于荧光染料探针测定的脂肽的临界聚集浓度）会注意到细胞活力的一些丧失。初步试验还显示对革兰氏阴性菌和革兰氏阳性菌均有抗菌活性。
The conformation and self-assembly of two pairs of model lipidated tripeptides in aqueous solution are probed using a combination of spectroscopic methods along with cryogenic-transmission electron microscopy (cryo-TEM) and small-angle X-ray scattering (SAXS). The palmitoylated lipopeptides comprise C16-YKK or C16-WKK (with twol-lysine residues) or their respective derivatives containingd-lysine (k), i.e., C16-Ykk and C16-Wkk. All four molecules self-assemble into spherical micelles which show structure factor effects in SAXS profiles due to intermicellar packing in aqueous solution. Consistent with micellar structures, the tripeptides in the coronas have a largely unordered conformation, as probed using spectroscopic methods. The molecules are found to have good cytocompatibility with fibroblasts at sufficiently low concentrations, although some loss of cell viability is noted at the highest concentrations examined (above the critical aggregation concentration of the lipopeptides, determined from fluorescence dye probe measurements). Preliminary tests also showed antimicrobial activity against both Gram-negative and Gram-positive bacteria.