School of Basic Medical Sciences, Henan University of Science and Technology, Luoyang, 471003, China.
School of Basic Medical Sciences, Henan University of Science and Technology, Luoyang, 471003, China.
Toxicon. 2022 Apr 15;209:1-9. doi: 10.1016/j.toxicon.2022.01.012. Epub 2022 Feb 1.
Antimicrobial peptides are widely acknowledged as an alternative class of antimicrobial agents. In this study, a lysine-rich scorpion peptide derivative Pacavin-5K was designed, which showed an improved antibacterial spectrum, significantly higher antibacterial activity, and lower toxicity compared to the native peptide. It also showed an improved thermal and serum stability. Notably, Pacavin-5K significantly decreased the bacterial counts in the wounded region in the mouse cutaneous infection model caused by Staphylococcus aureus and Pseudomonas aeruginosa. Moreover, Pacavin-5K did not induce bacterial resistance associated with its antibacterial mechanism disrupting the membrane. Furthermore, Pacavin-5K could kill the S. aureus cells at the biofilm state. Overall, Pacavin-5K could be a potential alternative antibacterial agent against skin infection caused by S. aureus and P. aeruginosa.
抗菌肽被广泛认为是一类替代的抗菌药物。在这项研究中，设计了一种富含赖氨酸的蝎子肽衍生物 Pacavin-5K，与天然肽相比，它显示出了改善的抗菌谱、更高的抗菌活性和更低的毒性。它还表现出了改善的热稳定性和血清稳定性。值得注意的是，Pacavin-5K 显著降低了金黄色葡萄球菌和铜绿假单胞菌引起的小鼠皮肤感染模型中创伤区域的细菌计数。此外，Pacavin-5K 不会诱导与破坏膜的抗菌机制相关的细菌耐药性。此外，Pacavin-5K 可以杀死生物膜状态下的金黄色葡萄球菌细胞。总体而言，Pacavin-5K 可能是一种对抗金黄色葡萄球菌和铜绿假单胞菌引起的皮肤感染的潜在替代抗菌药物。
