Peptide engineering has gained attraction as a source of new cationicity-enhanced analogues with high potential for the design of next-generation antibiotics. In this context, cruzioseptin-1 (CZS-1), a peptide identified from Cruziohyla calcarifer, is recognized for its antimicrobial potency. However, this amidated-peptide is moderately hemolytic. In order to reduce toxicity and increase antimicrobial potency, 3 peptide analogues based on cruzioseptin-1 were designed and evaluated. [K4K15]CZS-1, an analogue with increased cationicity and reduced hydrophobicity, showed antibacterial, antifungal and antiproliferative properties. In addition, [K4K15]CZS-1 is less hemolytic than CZS-1. The in silico and scanning electron microscopy analysis reveal that [K4K15]CZS-1 induces a membranolytic effect on bacteria. Overall, these results confirm the potential of CZS-1 as source of inspiration for design new selective antimicrobial analogues useful for development of new therapeutic agents.
CITATION STYLE
Bermúdez-Puga, S., Morán-Marcillo, G., Espinosa de los Monteros-Silva, N., Naranjo, R. E., Toscano, F., Vizuete, K., … Proaño-Bolaños, C. (2023). Inspiration from cruzioseptin-1: membranolytic analogue with improved antibacterial properties. Amino Acids, 55(1), 113–124. https://doi.org/10.1007/s00726-022-03209-6
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