Inspiration from cruzioseptin-1: membranolytic analogue with improved antibacterial properties

Autor: Sebastián Bermúdez-Puga, Giovanna Morán-Marcillo, Nina Espinosa de los Monteros-Silva, Renato E. Naranjo, Fernanda Toscano, Karla Vizuete, Marbel Torres Arias, José R. Almeida, Carolina Proaño-Bolaños
Rok vydání: 2023
Předmět:
Zdroj: Repositorio Universidad Regional Amazónica
Universidad Regional Amazónica
instacron:IKIAM
ISSN: 1438-2199
0939-4451
Popis: 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.
Databáze: OpenAIRE
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