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Título : Cruzioseptins, antibacterial peptides from Cruziohyla calcarifer skin, as promising leishmanicidal agents
Autor : Mendes, Bruno
Proaño Bolaños, Carolina
Gadelha, Fernanda R
de Almeida, José R.
Miguel, Danilo C.
Palabras clave : cruzioseptins
Frog skin secretion
Fecha de publicación : 2020
Editorial : Scopus
Citación : Bruno Mendes, Carolina Proaño-Bolaños, Fernanda R Gadelha, José R Almeida, Danilo C Miguel, Cruzioseptins, antibacterial peptides from Cruziohyla calcarifer skin, as promising leishmanicidal agents, Pathogens and Disease, Volume 78, Issue 6, August 2020, ftaa053, doi.org/10.1093/femspd/ftaa053
Resumen : Screenings of natural products have significantly contributed to the discovery of novel leishmanicidal agents. In this study, three known cruzioseptins—antibacterial peptides from Cruziohyla calcarifer skin—were synthesized and evaluated against promastigotes and amastigotes stages of Leishmania (L.) amazonensis and L. (V.) braziliensis. EC50 ranged from 9.17 to 74.82 μM, being cruzioseptin-1 the most active and selective compound, with selectivity index > 10 for both promastigotes and amastigotes of L. (V.) braziliensis. In vitro infections incubated with cruzioseptins at 50 μM showed up to ∼86% reduction in the amastigote number. Cruzioseptins were able to destabilize the parasite's cell membrane, allowing the incorporation of a DNA-fluorescent dye. Our data also demonstrated that hydrophobicity and charge appear to be advantageous features for enhancing parasiticidal activity. Antimicrobial cruzioseptins are suitable candidates and alternative molecules that deserve further in vivo investigation focusing on the development of novel antileishmanial therapies.
URI : https://doi.org/10.1093/femspd/ftaa053
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