Please use this identifier to cite or link to this item: https://www.arca.fiocruz.br/handle/icict/30720
Title: Trypanosoma cruzi: activity of heterocyclic cationic molecules in vitro
Authors: Pacheco, Michele Gabriele de Oliveira
Silva, Cristiane França da
Souza, Elen Mello de
Batista, Marcos Meuser
Silva, Patrícia Bernardino da
Kumar, Arvind
Stephens, Chad E.
Boykin, David W.
Soeiro, Maria de Nazaré C.
Affilliation: Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ. Brasil.
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ. Brasil.
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ. Brasil.
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ. Brasil.
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ. Brasil.
Georgia State University. Department of Chemistry. Atlanta, GA, USA.
Georgia State University. Department of Chemistry. Atlanta, GA, USA.
Georgia State University. Department of Chemistry. Atlanta, GA, USA.
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ. Brasil.
Abstract: Chagas disease remains a serious public health problem in several Latin American countries. New chemotherapy is urgently needed since current drugs are limited in efficacy and exhibit undesirable side effects. Aromatic diamidines and analogs are well known anti-parasitic agents and in this study, we have evaluated the in vitro trypanocidal effect of several different heterocyclic cationic compounds, including diamidines (DB1195, DB1196 and DB1345), a monoamidine (DB824), an arylimidamide (DB613A) and a guanylhydrazone (DB1080) against amastigotes and bloodstream trypomastigotes of Trypanosoma cruzi, the etiological agent of Chagas disease. Our present findings showed that all compounds exerted, at low-micromolar doses, a trypanocidal effect upon both intracellular parasites and bloodstream trypomastigotes of T. cruzi. The activity of DB1195, DB1345, DB824 and DB1080 against bloodstream forms was reduced when these compounds were assayed in the presence of mouse blood possibly due to their association with plasma constituents and/or due to metabolic instability of the compounds. However, trypanocidal effects of DB613A and DB1196 were not affected by plasma constituents, suggesting their potential application in the prophylaxis of banked blood. In addition, potency and selectivity of DB613A, towards intracellular parasites, corroborate previous results that demonstrated the highly promising activity of arylimidamides against this parasite, which justify further studies in experimental models of T. cruzi infection.
Keywords: Trypanosoma cruzi
Chagas Disease
Diamidines
keywords: Trypanosoma cruzi
Diamidinas
Doença de Chagas
Issue Date: 2009
Publisher: Elsevier
Citation: PACHECO, Michele Gabriele de Oliveira; et al. Trypanosoma cruzi: Activity of heterocyclic cationic molecules in vitro. Experimental Parasitology, v.123, p.73-80, 2009.
DOI: 10.1016/j.exppara.2009.06.004
ISSN: 0014-4894
Copyright: restricted access
Appears in Collections:IOC - Artigos de Periódicos

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