癸酸修饰增强 PMAP-23RI-Dec 的抗菌活性。
Decanoic acid modification enhances the antibacterial activity of PMAP-23RI-Dec.
机构信息
The Key Lab of Veterinary Biological Products, Henan University of Science and Technology, Luoyang, Henan 471000, China.
The Key Lab of Veterinary Biological Products, Henan University of Science and Technology, Luoyang, Henan 471000, China; Henan Provincial Open Laboratory of Key Disciplines in Environmental and Animal Products Safety, Henan University of Science and Technology, Luoyang, Henan 471000, China.
出版信息
Eur J Pharm Sci. 2021 Feb 1;157:105609. doi: 10.1016/j.ejps.2020.105609. Epub 2020 Oct 22.
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.
抗菌肽是一种新型的抗菌药物，具有广谱抗菌作用。基于我们之前的研究，通过在 PMAP-23RI 的 C 末端修饰癸酸设计了 PMAP-23RI-Dec。在本研究中，我们测量了 PMAP-23RI-Dec 的抗菌活性、稳定性、溶血活性和细胞毒性。还研究了 PMAP-23RI-Dec 对生物膜和细胞膜的作用机制。结果表明，PMAp-23RI-Dec 表现出高抗菌活性和稳定性，但 PMAP-23RI-Dec 的溶血活性和细胞毒性没有增强。此外，PMAp-23RI-Dec 可以在低浓度下抑制生物膜的形成，并通过改变其细胞膜的通透性增强对细菌的杀伤作用。最后，PMAp-23RI-Dec 减少了铜绿假单胞菌 GIM1.551 和金黄色葡萄球菌 ATCC25923 对器官的损伤，并显示出对腹膜炎的优异疗效。PMAp-23RI-Dec 还减少了脓肿范围并缓解了伤口感染。我们的研究表明，PMAp-23RI-Dec 是一种具有潜在临床应用的新型抗菌剂。
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