Antibiotics (Aug 2021)

Design, Synthesis and Antifungal Activity of Stapled Aurein1.2 Peptides

  • Mengjun Zheng,
  • Ruina Wang,
  • Si Chen,
  • Yan Zou,
  • Lan Yan,
  • Linjing Zhao,
  • Xiang Li

DOI
https://doi.org/10.3390/antibiotics10080956
Journal volume & issue
Vol. 10, no. 8
p. 956

Abstract

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Aurein1.2 is a 13-residue antimicrobial peptide secreted by the Australian tree frog Litoria aurea. In order to improve its stabilities, the helical contents and corresponding biological activities of Aurein1.2 (a series of stapled analogues) were synthesized, and their potential antifungal activities were evaluated. Not surprisingly, the stapled Aurein1.2 peptides showed higher proteolytic stability and helicity than the linear counterpart. The minimum inhibitory concentration (MIC) of ten stapled peptides against six strains of common pathogenic fungi was determined by the microscale broth dilution method recommended by CLSI. Of them, Sau-1, Sau-2, Sau-5, and Sau-9 exhibited better inhibitory effects on the fungi than the linear peptide. These stapled Aurein1.2 peptides may serve as the leading compounds for further optimization and antifungal therapy.

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