Please use this identifier to cite or link to this item: https://www.arca.fiocruz.br/handle/icict/30812
Title: Trypanosoma cruzi: in vitro activity of Epoxy-alpha-Lap, a derivative of alpha-lapachone, on trypomastigote and amastigote forms
Authors: Bourguignon, S. C.
Faria Neto, Hugo Castro C.
Santos, D. O.
Alves, C. R.
Ferreira, V. F.
Gama, I. L.
Silva, F. C.
Seguins, W. S.
Pinho, R. T.
Affilliation: Universidade Federal Fluminense. Departamento de Biologia Geral e Celular. Niterói, RJ, Brasil.
Universidade Federal Fluminense. Departamento de Biologia Geral e Celular. Niterói, RJ, Brasil.
Universidade Federal Fluminense. Departamento de Biologia Geral e Celular. Niterói, RJ, Brasil / Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Imunologia Clínica. Rio de Janeiro, RJ, Brasil.
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Molecular e Doenças Endêmicas. Rio de Janeiro, RJ, Brasil.
Universidade Federal Fluminense. Instituto de Química. Departamento de Química Orgânica. Niterói, RJ, Brasil.
Universidade Federal Fluminense. Instituto de Química. Departamento de Química Orgânica. Niterói, RJ, Brasil.
Universidade Federal Fluminense. Instituto de Química. Departamento de Química Orgânica. Niterói, RJ, Brasil.
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Imunologia Clínica. Rio de Janeiro, RJ, Brasil.
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Imunologia Clínica. Rio de Janeiro, RJ, Brasil.
Abstract: Chagas disease is an endemic parasitic infection caused by Trypanosomacruzi that affects 18-20 million people in Central and South America. Recently we described the Epoxy-alpha-Lap, an oxyran derivative of alpha-lapachone, which presents a low toxicity profile and a high inhibitory activity against T.cruzi epimastigotes forms, the non-infective form of this parasite. In this work we described the trypanocidal effects of Epoxy-alpha-Lap on extracellular (trypomastigote) and intracellular (amastigote) infective forms of two T. cruzi strains (Y and Colombian) known by their different infective profile. Our results showed that Epoxy-alpha-Lap is lethal to trypomastigote Y and Colombian strains (97% and 84%, respectively). Interestingly, Epoxy-alpha-Lap also showed a trypanocidal effect in human macrophage infected with T. cruzi Y (85.6%) and Colombian (71.9%) strains amastigote forms. Similar effects were observed on T. cruzi amastigote infected Vero cells (96.4% and 95.0%, respectively). Our results pointed Epoxy-alpha-Lap as a potential candidate for Chagas disease chemotherapy since it presents trypanocidal activity on all T. cruzi forms with low) toxicity profile.
Keywords: a-Lapachone
Epoxi-a-Lap
Trypanocidad effect
Trypanosoma cruzi
Chagas Disease
keywords: Trypanosoma cruzi
Efeito de tripanocida
Epoxi-a-Lap
a-Lapachone
Doença de Chagas
Issue Date: 2009
Publisher: Elsevier
Citation: BOURGUIGNON, S. C. et al. Trypanosoma cruzi: in vitro activity of Epoxy-a-Lap, a derivative of A-lapachone on trypomastigote and amastigote forms. Experimental Parasitology, v.122, p.91-96, Mar. 2009.
DOI: 10.1016/j.exppara.2009.03.002
ISSN: 0014-4894
Copyright: restricted access
Appears in Collections:IOC - Artigos de Periódicos

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