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


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.

SUBMITTER: Misawa T 

PROVIDER: S-EPMC6590335 | biostudies-literature | 2019 Jun

REPOSITORIES: biostudies-literature

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

Misawa Takashi T   Goto Chihiro C   Shibata Norihito N   Hirano Motoharu M   Kikuchi Yutaka Y   Naito Mikihiko M   Demizu Yosuke Y  

MedChemComm 20190404 6


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 <b>Block</b>, <b>Stripe</b>, and <b>Random</b>, and revealed that <b>Stripe</b> exhibits potent antimicrobial activity against Gram-positive and Gram-negative microbes. Moreover, we also demonst  ...[more]

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