期刊
PATHOGENS AND DISEASE
卷 78, 期 6, 页码 -出版社
OXFORD UNIV PRESS
DOI: 10.1093/femspd/ftaa053
关键词
cruzioseptins; frog skin secretion; leishmanicidal; peptides
资金
- CAPES-DS fellowship (Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior-Programa de Demanda Social)
- FAEPEX-Pro-Reitoria de Pesquisa (PRP)/UNICAMP [519.292]
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.
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