Nylon-3 Polymers with Selective Antifungal Activity

被引:122
作者
Liu, Runhui [1 ,2 ]
Chen, Xinyu [1 ]
Hayouka, Zvi [1 ]
Chakraborty, Saswata [1 ]
Falk, Shaun P. [3 ]
Weisblum, Bernard [3 ]
Masters, Kristyn S. [2 ]
Gellman, Samuel H. [1 ]
机构
[1] Univ Wisconsin, Dept Chem, Madison, WI 53706 USA
[2] Univ Wisconsin, Dept Biomed Engn, Madison, WI 53706 USA
[3] Univ Wisconsin, Dept Med, Madison, WI 53706 USA
关键词
HOST-DEFENSE PEPTIDES; DE-NOVO DESIGN; ANTIMICROBIAL BETA-PEPTIDES; RING-OPENING POLYMERIZATION; ANIONIC-POLYMERIZATION; ANTIBACTERIAL ACTIVITY; HEMOLYTIC ACTIVITIES; RANDOM COPOLYMERS; PEPTOID MIMICS; LYTIC PEPTIDES;
D O I
10.1021/ja4006404
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Host-defense peptides inhibit bacterial growth but show little toxicity toward mammalian cells. A variety of synthetic polymers have been reported to mimic this antibacterial selectivity; however, achieving comparable selectivity for fungi is more difficult because these pathogens are eukaryotes. Here we report nylon-3 polymers based on a novel subunit that display potent antifungal activity (MIC = 3.1 mu g/mL for Candida albicans) and favorable selectivity (IC10 > 400 mu g/mL for 3T3 fibroblast toxicity; HC10 > 400 mu g/mL for hemolysis).
引用
收藏
页码:5270 / 5273
页数:4
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