Title: Cruzioseptins, antibacterial peptides from Cruziohyla calcarifer skin, as promising leishmanicidal agents
Author: Mendes, Bruno; Proaño-bolaños, Carolina; Gadelha, Fernanda R; Almeida, José R; Miguel, Danilo C
Is part of: Pathogens and Disease, v. 78, p. 1 - 8
Citation: Mendes, Bruno; Proaño-bolaños, Carolina; Gadelha, Fernanda R; Almeida, José R; Miguel, Danilo C; Cruzioseptins, antibacterial peptides from Cruziohyla calcarifer skin, as promising leishmanicidal agents. Pathogens and Disease, v.78, p. 1-8, 2020
Abstract: 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 mu M, 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 mu M showed up to similar 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.
Funding: Results of this work are part of the project 'Conservation of Ecuadorian amphibian diversity and sustainable use of its genetic resources,' which involves MAE, Ikiam-Universidad Regional Amazonica, Queen's University Belfast, Centro Jambatu, Global Environmental Facility (GEF) and 'Programa de las Naciones Unidas para el Desarrollo' (PNUD). B.M. was recipient of a CAPES-DS fellowship (Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior-Programa de Demanda Social). D.C.M. thanks FAEPEX-Pro-Reitoria de Pesquisa (PRP)/UNICAMP for financial support (#519.292).