Structure-activity relationships and action mechanisms of collagen-like antimicrobial peptides.
Structure-activity relationships and action mechanisms of collagen-like antimicrobial peptides.
复制标题
类胶原抗菌肽的构效关系及作用机制。
作者：
Masuda R;Dazai Y;Mima T;Koide T
抗微生物三螺旋肽R3先前从胶原样组合肽文库获得。本研究基于R3的构效关系研究，开发了一种活性更强的多肽RR 4，其净电荷和电荷密度均比R3高，对革兰氏阴性和革兰氏阳性细菌菌株（包括多重耐药菌株）均具有抗菌活性。它的作用可以归因于进入细胞并与细胞间分子如DNA/RNA相互作用，抑制细胞分裂，而不是增加细菌膜的渗透性。RR 4在血清中具有良好的稳定性和较低的细胞毒性。
An antimicrobial triple‐helical peptide,R3, was previously obtained from a collagen‐like combinatorial peptide library. In this research, based on structure–activity relationship studies ofR3, a more potent peptide,RR4, with increased positive net charge and charge density relative toR3, was developed.RR4exhibited antimicrobial activity against both Gram‐negative and Gram‐positive bacterial strains, including multidrug‐resistant strains. Its action could be attributed to entry into cells and interactions with intercellular molecules such as DNA/RNA that inhibited cell division rather than increasing bacterial membrane permeability. Furthermore,RR4exhibited remarkable stability in serum and low cytotoxicity.