抗真菌
细胞内
流出
生物
体内
化学
生物化学
阳离子聚合
戒毒(替代医学)
作用机理
杀菌剂
抗真菌药
铁稳态
细胞膜
抗氧化剂
微生物学
平衡
细胞生物学
细胞壁
抗药性
真菌蛋白
细胞
行动方式
作者
Nan Liu,Mingrui Cheng,Y Tao,Xingchen Sun,Boyi Wu,Wenjing Ma,Xujiao Zhou,Jiaxu Hong,Jingjing Hu,Yiyun Cheng
标识
DOI:10.1073/pnas.2537796123
摘要
Fungal infections pose a growing global health challenge, exacerbated by a scarcity of effective treatments and rising drug resistance. Although cationic polymers emerge as promising antifungal candidates owing to structural tunability, design flexibility, and resistance to proteolytic degradation, their clinical utility has been hampered by nonselective membrane-disruption mechanisms. Herein, we develop a class of polycatechols- termed fungal iron predators (FIPs), exhibit exceptional fungicidal activity and markedly low cytotoxicity. These FIPs can efficiently infiltrate fungal cells, selectively sequester labile iron, and disrupt iron homeostasis and metabolism. The ensuing iron starvation provokes severe mitochondrial dysfunction and energy collapse, culminating in fungal cell death. Through systemic optimization of cationic density and catechol stoichiometry, we obtained an FIP variant demonstrating potent antifungal activity with high selectivity toward fungi over mammalian cells, minimal propensity to induce resistance, and supplementary antioxidant properties. Remarkably, this FIP candidate shows robust therapeutic performance across multiple in vivo models of fungal infection. Critically, this work established a groundbreaking paradigm in polymer design: shifting the antifungal mechanism from traditional nonspecific membrane disruption to targeted intracellular metabolic interference. The general applicability of this strategy across diverse cationic polymer backbones opens avenues for developing next generation of precision antifungal agents.
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