Antifungal activity of analogues of antimicrobial peptides isolated from bee venoms against vulvovaginal Candida spp.
FEMS Yeast Res. 2019 Feb 11
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Candida albicans is the main causative agent of vulvovaginal candidiasis, a common mycosis in women, relapses of which are difficult to manage due to biofilm formation.
This study aimed to develop novel non-toxic compounds active against Candida spp. biofilms. We synthesized analogues of natural antifungal peptides LL-III (LL-III/43) and HAL-2 (peptide VIII) originally isolated from bee venoms and elucidated their structures by nuclear magnetic resonance spectroscopy.
The haemolytic, cytotoxic, antifungal and anti-biofilm activities of LL-III/43 and peptide VIII were then tested. LL-III/43 and VIII showed moderate cytotoxicity to HUVEC-2 cells and had comparable inhibitory activity against C. albicans and non-albicans spp. The lowest minimum inhibitory concentration (MIC90) of LL-III/43 was observed towards C. tropicalis (0.8 µM). That was 8-fold lower than that of antimycotic amphotericin B. Both peptides can be used to inhibit Candida spp. biofilms formation.
Biofilm inhibitory concentrations (BIC50) ranged from 0.9 to 58.6 µM and biofilm eradication concentrations (BEC50) for almost all tested Candida spp. strains ranged from 12.8 to 200 µM.
Also proven were the peptides' abilities to reduce area colonized by biofilm, inhibit hyphae formation and permeabilize cell membranes in biofilm. LL-III/43 and VIII are promising candidates for further development as therapeutics against vulvovaginal candidiasis.
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