Animal Biosciences, University of Guelph, Guelph, ON N1G 2W1, Canada.
Biomolecules. 2020 Jul 8;10(7):1014. doi: 10.3390/biom10071014.
Multi-drug resistant (MDR) bacteria and their biofilms are a concern in veterinary and human medicine. Protegrin-1 (PG-1), a potent antimicrobial peptide (AMP) with antimicrobial and immunomodulatory properties, is considered a potential alternative for conventional antibiotics. AMPs are less stable and lose activity in the presence of physiological fluids, such as serum. To improve stability of PG-1, a hybrid peptide, SynPG-1, was designed. The antimicrobial and antibiofilm properties of PG-1 and the PG-1 hybrid against MDR pathogens was analyzed, and activity after incubation with physiological fluids was compared. The effects of these peptides on the IPEC-J2 cell line was also investigated. While PG-1 maintained some activity in 25% serum for 2 h, SynPG-1 was able to retain activity in the same condition for up to 24 h, representing a 12-fold increase in stability. Both peptides had some antibiofilm activity against and . While both peptides prevented biofilm formation of methicillin-resistant (MRSA), neither could destroy MRSA's pre-formed biofilms. Both peptides maintained activity after incubation with trypsin and porcine gastric fluid, but not intestinal fluid, and stimulated IPEC-J2 cell migration. These findings suggest that SynPG-1 has much better serum stability while maintaining the same antimicrobial potency as PG-1.
多药耐药（MDR）细菌及其生物膜是兽医和人类医学关注的问题。Protegrin-1（PG-1）是一种具有抗菌和免疫调节特性的强效抗菌肽（AMP），被认为是传统抗生素的潜在替代品。AMP 在存在生理液（如血清）时不太稳定并且失去活性。为了提高 PG-1 的稳定性，设计了一种杂合肽 SynPG-1。分析了 PG-1 和 PG-1 杂合肽对 MDR 病原体的抗菌和抗生物膜特性，并比较了在与生理液孵育后的活性。还研究了这些肽对 IPEC-J2 细胞系的影响。虽然 PG-1 在 25%血清中 2 小时保持一定活性，但 SynPG-1 能够在相同条件下保持活性长达 24 小时，稳定性提高了 12 倍。两种肽都对 和 具有一定的抗生物膜活性。虽然两种肽都能阻止耐甲氧西林金黄色葡萄球菌（MRSA）的生物膜形成，但都不能破坏 MRSA 已形成的生物膜。两种肽在与胰蛋白酶和猪胃液孵育后仍保持活性，但与肠液孵育后则没有活性，并刺激了 IPEC-J2 细胞迁移。这些发现表明，SynPG-1 具有更好的血清稳定性，同时保持与 PG-1 相同的抗菌效力。
