Inspiration from cruzioseptin-1: membranolytic analogue with improved antibacterial properties
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. Howeve...
| Autores: | , , , , , , , , |
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| Formato: | artículo |
| Estado: | Versión publicada |
| Fecha de publicación: | 2023 |
| País: | Ecuador |
| Recursos: | Universidad Regional Amazónica |
| Repositorio: | Repositorio Universidad Regional Amazónica |
| OAI Identifier: | oai:repositorio.ikiam.edu.ec:RD_IKIAM/646 |
| Acesso em linha: | https://doi.org/10.1007/s00726-022-03209-6 http://repositorio.ikiam.edu.ec/jspui/handle/RD_IKIAM/646 |
| Access Level: | acceso abierto |
| Palavra-chave: | Antimicrobial peptides Cruzioseptin. Membranolytic effect Rational design |
| Resumo: | 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. |
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