Voltar
Artigo Acesso aberto Produção Nacional Revisado por pares
BIBTEX RIS

The alkylaminoalkanethiosulfuric acids exhibit in-vitro antileishmanial activity against Leishmania (Viannia) braziliensis : a new perspective for use of these schistosomicidal agents

2019; Oxford University Press; Volume: 71; Issue: 12 Linguagem: Inglês

10.1111/jphp.13163

ISSN

2042-7158

Autores

Gabriane Nascimento Porcino, Luciana Maria Ribeiro Antinarelli, Ana Carolina Ribeiro Gomes Maia, Priscila de Faria Pinto, Alessandro Taunay-Rodrigues, Paulo Marcos Zech Coelho, David Lee Nelson, Marcus L. O. Penido, Elaine Soares Coimbra, Eveline Gomes Vasconcelos,

Tópico(s)

Insect Pest Control Strategies

Resumo

The alkylaminoalkanethiosulfuric acids (AAATs) are amphipathic compounds effective against experimental schistosomiasis, of low toxicity, elevated bioavailability after a single oral dose and prompt tissue absorption.To explore the in-vitro antileishmanial potential of AAATs using five compounds of this series against Leishmania (Viannia) braziliensis.Their effects on promastigotes and axenic amastigotes, and cytotoxicity to macrophages were tested by the MTT method, and on Leishmania-infected macrophages by Giemsa stain. Effects on the mitochondrial membrane potential of promastigotes and axenic amastigotes and DNA of intracellular amastigotes were tested using JC-1 and TUNEL assays, respectively.The 2-(isopropylamino)-1-octanethiosulfuric acid (I) and 2-(sec-butylamino)-1-octanethiosulfuric acid (II) exhibit activity against both promastigotes and intracellular amastigotes (IC50 25-35 µm), being more toxic to intracellular parasites than to the host cell. Compound I induced a loss of viability of axenic amastigotes, significantly reduced (30%) the mitochondrial membrane potential of both promastigotes and axenic amastigotes and promoted selective DNA fragmentation of the nucleus and kinetoplast of intracellular amastigotes.In this previously unpublished study of trypanosomatids, it is shown that AAATs could also exhibit selective antileishmanial activity, a new possibility to be investigated in oral treatment of leishmaniasis.

Referência(s)