Please use this identifier to cite or link to this item: https://www.arca.fiocruz.br/handle/icict/15912
Title: The efficacy of novel arylimidamides against Trypanosoma cruzi in vitro
Authors: Silva, Christiane França
Daliry, Anissa
Silva, Patrícia Bernardino da
Akay, Senol
Banerjee, Moloy
Farahat, Abdelbasset A.
Fisher, Mary K.
Hu, Laixing
Kumar, Arvind
Liu, Zongying
Stephens, Chad E.
Boykin, David W.
Soeiro, Maria de Nazaré Correia
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.
Augusta State University. Department of Chemistry. Georgia, USA.
Augusta State University. Department of Chemistry. Georgia, USA.
Augusta State University. Department of Chemistry. Georgia, USA.
Augusta State University. Department of Chemistry and Physics. Georgia, USA.
Augusta State University. Department of Chemistry. Georgia, USA.
Augusta State University. Department of Chemistry. Georgia, USA.
Augusta State University. Department of Chemistry. Georgia, USA.
Augusta State University. Department of Chemistry and Physics. Georgia, USA.
Augusta State University. Department of Chemistry. Georgia, USA.
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil.
Abstract: The present study aimed to determine the in vitro biological efficacy and selectivity of 7 novel AIAs upon bloodstream trypomastigotes and intracellular amastigotes of Trypanosoma cruzi. The biological activity of these aromatic compounds was assayed for 48 and 24 h against intracellular parasites and bloodstream forms of T. cruzi (Y strain), respectively. Additional assays were also performed to determine their potential use in blood banks by treating the bloodstream parasites with the compounds diluted in mouse blood for 24 h at 4 °C. Toxicity against mammalian cells was evaluated using primary cultures of cardiac cells incubated for 24 and 48 h with the AIAs and then cellular death rates were determined by MTT colorimetric assays. Our data demonstrated the outstanding trypanocidal effect of AIAs against T. cruzi, especially DB1853, DB1862, DB1867 and DB1868, giving IC50 values ranging between 16 and 70 nanomolar against both parasite forms. All AIAs presented superior efficacy to benznidazole and some, such as DB1868, also demonstrated promising activity as a candidate agent for blood prophylaxis. The excellent anti-trypanosomal efficacy of these novel AIAs against T. cruzi stimulates furtherin vivo studies and justifies the screening of new analogues with the goal of establishing a useful alternative therapy for Chagas disease.
Keywords: Trypanosoma cruzi
Chagas Disease
Chemotherapy
arylimidamides
keywords: Trypanosoma cruzi
Doença de Chagas
Quimioterapia
arylimidamides
Issue Date: 2011
Publisher: Cambridge University Press
Citation: SILVA, Christiane França da; et al. The efficacy of novel arylimidamides against Trypanosoma cruzi in vitro. Parasitology, v.138, n.14, p.1863-1869, Dec. 2011.
DOI: 10.1017/S0031182011001429
ISSN: 0031-1820
Copyright: restricted access
Appears in Collections:IOC - Artigos de Periódicos

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