Histatin 5-Inspired Short-Chain Peptides Selectively Combating Pathogenic Fungi with Multifaceted Mechanisms

Adv Healthc Mater. 2024 Jul;13(17):e2303755. doi: 10.1002/adhm.202303755. Epub 2024 Mar 9.

Abstract

Short-chain antifungal peptides (AFPs) inspired by histatin 5 have been designed to address the problem of antifungal drug resistance. These AFPs demonstrate remarkable antifungal activity, with a minimal inhibitory concentration as low as 2 µg mL-1. Notably, these AFPs display a strong preference for targeting fungi rather than bacteria and mammalian cells. This is achieved by binding the histidine-rich domains of the AFPs to the Ssa1/2 proteins in the fungal cell wall, as well as the reduced membrane-disrupting activity due to their low amphiphilicity. These peptides disrupt the nucleus and mitochondria once inside the cells, leading to reactive oxygen species production and cell damage. In a mouse model of vulvovaginal candidiasis, the AFPs demonstrate not only antifungal activity, but also promote the growth of beneficial Lactobacillus spp. This research provides valuable insights for the development of fungus-specific AFPs and offers a promising strategy for the treatment of fungal infectious diseases.

Keywords: antifungal mechanism; antifungal peptides; commensal bacteria protection; selective antifungal activity; vulvovaginal candidiasis.

MeSH terms

  • Animals
  • Antifungal Agents* / chemistry
  • Antifungal Agents* / pharmacology
  • Candida albicans / drug effects
  • Candidiasis, Vulvovaginal / drug therapy
  • Candidiasis, Vulvovaginal / microbiology
  • Female
  • Fungi / drug effects
  • Histatins* / chemistry
  • Histatins* / pharmacology
  • Humans
  • Mice
  • Microbial Sensitivity Tests
  • Peptides / chemistry
  • Peptides / pharmacology
  • Reactive Oxygen Species / metabolism

Substances

  • Histatins
  • Antifungal Agents
  • HTN3 protein, human
  • Reactive Oxygen Species
  • Peptides