期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 61, 期 9, 页码 3889-3907出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.7b01729
关键词
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资金
- National Natural Science Foundation of China [31272453, 31472104, 31672434]
- China Agriculture Research System [CARS 36]
- Program for Universities in Heilongjiang Province [1254CGZH22]
Antimicrobial peptides are an important weapon against invading pathogens and are potential candidates as novel antibacterial agents, but their antifungal activities are not fully developed. In this study, a set of imperfectly amphipathic peptides was developed based on the imperfectly amphipathic palindromic structure R-n(XRXXXRX))R-n (n = 1, 2; X represents L, I, F, or W), and the engineered peptides exhibited high antimicrobial activities against all fungi and bacteria tested (including fluconazole-resistant Candida albicans), with geometric mean (GM) MICs ranging from 2.2 to 6.62 mu M. Of such peptides, 13 (16) (RRIRIIIRIRR-NH2) that was Ile rich in its hydrophobic face had the highest antifungal activity (GM(fungi) = 1.64 mu M) while showing low toxicity and high salt and serum tolerance. It also had dramatic LPS-neutralizing propensity and a potent membrane-disruptive mechanism against microbial cells. In summary, these findings were useful for short AMPs design to combat the growing threat of drug-resistant fungal and bacterial infections.
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