School of Pharmaceutical Sciences, Southern Medical University, 1838 Guangzhou Avenue North, Guangzhou 510515, PR China.
School of Pharmaceutical Sciences, Southern Medical University, 1838 Guangzhou Avenue North, Guangzhou 510515, PR China.
Eur J Med Chem. 2014 Aug 18;83:36-44. doi: 10.1016/j.ejmech.2014.06.003. Epub 2014 Jun 4.
Tryptophan and arginine rich antimicrobial peptides (AMPs) possess high potencies against both gram positive and gram negative bacteria, while lipopeptides represent another family of promising antimicrobial agents to combat invading pathogens. In the present study, we have synthesized a series of very short arginine, lysine and tryptophan containing lipopeptides and evaluated their antimicrobial activities against a panel of pathogenic microorganisms including Staphylococcus aureus, Escherichia coli, and Candida albicans. The results showed that most of these peptides were effective against tested strains with MIC values ranging from 3.9 to 62.5 μg/mL. In addition to the small size, potent bactericidal activity, low to moderate hemolytic toxicity and membrane disruption ability, several peptides such as C10-RIKWWK and C10-RKWWK apparently retarded the migration of DNA on agarose gel in the DNA-binding assay, which implied the multiple modes of action in their bacteria-killing mechanism. These peptides revealed a promising therapeutic potential to develop as new antimicrobial agents.
色氨酸和精氨酸丰富的抗菌肽（AMPs）对革兰氏阳性菌和革兰氏阴性菌均具有高活性，而脂肽则是另一种有前途的抗菌剂家族，可以对抗入侵的病原体。在本研究中，我们合成了一系列含有精氨酸、赖氨酸和色氨酸的非常短的脂肽，并评估了它们对包括金黄色葡萄球菌、大肠杆菌和白色念珠菌在内的一系列致病微生物的抗菌活性。结果表明，这些肽中的大多数对测试菌株有效，MIC 值范围为 3.9 至 62.5μg/mL。除了体积小、杀菌活性强、溶血毒性低到中度和破坏膜的能力外，一些肽，如 C10-RIKWWK 和 C10-RKWWK，在 DNA 结合试验中明显减缓了琼脂糖凝胶上 DNA 的迁移，这表明它们在杀菌机制中有多种作用模式。这些肽显示出作为新型抗菌剂开发的有希望的治疗潜力。
