Rational design of novel amphipathic antimicrobial peptides focused on the distribution of cationic amino acid residues

以阳离子氨基酸残基的分布为重点的新型两亲性抗菌肽的合理设计

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作者:Takashi Misawa, Chihiro Goto, Norihito Shibata, Motoharu Hirano, Yutaka Kikuchi, Mikihiko Naito, Yosuke Demizu

Abstract

Antimicrobial peptides (AMPs) have garnered much attention as novel therapeutic agents against infectious diseases. They exhibit antimicrobial activity through microbial membrane disruption based on their amphipathic properties. In this study, we rationally designed and synthesized a series of novel AMPs Block, Stripe, and Random, and revealed that Stripe exhibits potent antimicrobial activity against Gram-positive and Gram-negative microbes. Moreover, we also demonstrated that Stripe disrupts both Gram-positive and Gram-negative mimetic bacterial membranes. Finally, we investigated the hemolytic activity and cytotoxicity in human blood cells and human cell lines, and found that Stripe exhibited neither. These data indicated that Stripe is a promising antimicrobial reagent that does not display significant cytotoxicity.

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