Chang C-W T, Takemoto J Y
Department of Chemistry & Biochemistry, Utah State University, Logan, Utah 84322-0300 U.S.A.
Department of Biology, Utah State University, Logan, Utah 84322-5305 U.S.A.
Medchemcomm. 2014 Aug 1;5(8):1048-1057. doi: 10.1039/C4MD00078A.
The attachment of alkyl and other hydrophobic groups to traditional antibacterial kanamycins and neomycins creates amphiphilic aminoglycosides with altered antimicrobial properties. In this review, we summarize the discovery of amphiphilic kanamycins that are antifungal, but not antibacterial, and that inhibit the growth of fungi by perturbation of plasma membrane functions. With low toxicities against plant and mammalian cells, they appear to specifically target the fungal plasma membrane. These new antifungal agents offer new options for fighting fungal pathogens and are examples of reviving old drugs to confront new therapeutic challenges.
将烷基和其他疏水基团连接到传统抗菌药物卡那霉素和新霉素上，可产生具有改变抗菌特性的两亲性氨基糖苷类药物。在本综述中，我们总结了两亲性卡那霉素的发现，这些卡那霉素具有抗真菌而非抗菌作用，并且通过干扰质膜功能来抑制真菌生长。它们对植物和哺乳动物细胞毒性低，似乎特异性靶向真菌质膜。这些新型抗真菌剂为对抗真菌病原体提供了新选择，是旧药复苏以应对新治疗挑战的范例。
