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- Title
Inspiration from cruzioseptin-1: membranolytic analogue with improved antibacterial properties.
- Authors
Bermúdez-Puga, Sebastián; Morán-Marcillo, Giovanna; Espinosa de los Monteros-Silva, Nina; Naranjo, Renato E.; Toscano, Fernanda; Vizuete, Karla; Torres Arias, Marbel; Almeida, José R.; Proaño-Bolaños, Carolina
- Abstract
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.
- Subjects
PEPTIDE antibiotics; PEPTIDES; SCANNING electron microscopy; INSPIRATION; ANTIMICROBIAL peptides
- Publication
Amino Acids, 2023, Vol 55, Issue 1, p113
- ISSN
0939-4451
- Publication type
Article
- DOI
10.1007/s00726-022-03209-6