TY - JOUR
T1 - Inspiration from cruzioseptin-1
T2 - membranolytic analogue with improved antibacterial properties
AU - Bermúdez-Puga, Sebastián
AU - Morán-Marcillo, Giovanna
AU - Espinosa de los Monteros-Silva, Nina
AU - Naranjo, Renato E.
AU - Toscano, Fernanda
AU - Vizuete, Karla
AU - Torres Arias, Marbel
AU - Almeida, José R.
AU - Proaño-Bolaños, Carolina
N1 - Publisher Copyright:
© 2023, The Author(s), under exclusive licence to Springer-Verlag GmbH Austria, part of Springer Nature.
PY - 2023/1
Y1 - 2023/1
N2 - 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.
AB - 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.
KW - Antimicrobial peptides
KW - Cruzioseptin
KW - Membranolytic effect
KW - Rational design
UR - https://www.scopus.com/pages/publications/85145731882
U2 - 10.1007/s00726-022-03209-6
DO - 10.1007/s00726-022-03209-6
M3 - Artículo
C2 - 36609571
AN - SCOPUS:85145731882
SN - 0939-4451
VL - 55
SP - 113
EP - 124
JO - Amino Acids
JF - Amino Acids
IS - 1
ER -