European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences · 2020
Decanoic acid modification enhances the antibacterial activity of PMAP-23RI-Dec.
СтатьяНазвание и аннотация: Перевод пока не подготовлен
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Shen Tengfei, Chen Liangliang, Liu Yongqing, Shi Shuaibing, Liu Zhixin, Cai Kairui, Liao Chengshui, Wang Chen
Аннотация
Antimicrobial peptides are a new type of antibacterial drugs with a broad antibacterial spectrum. Based on our previous research, PMAP-23RI-Dec was designed by modifying the C-terminal of PMAP-23RI with decanoic acid. In this study, we measured the antibacterial activity, stability, hemolysis, and cytotoxicity of PMAP-23RI-Dec. The mechanism of PMAP-23RI-Dec on biofilm and cell membranes were also studied. The results show that PMAP-23RI-Dec exhibited high antibacterial activity and stability, but the hemolytic activity and cytotoxicity of PMAP-23RI-Dec were not enhanced. Moreover, PMAP-23RI-Dec could inhibit biofilm formation at low concentrations, and enhance the killing effect on bacteria by changing the permeability of their cell membranes. Finally, PMAP-23RI-Dec reduced Pseudomonas aeruginosa GIM1.551 and Staphylococcus aureus ATCC25923 damage to organs, and showed superior efficacy against peritonitis. PMAP-23RI-Dec also reduced the scope of abscess and alleviated wound infections. Our research indicated that PMAP-23RI-Dec is a new antibacterial agent with potential clinical application.