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Memórias do Instituto Oswaldo Cruz
Fundação Oswaldo Cruz, Fiocruz
ISSN: 1678-8060
EISSN: 1678-8060
Vol. 105, No. 3, 2010, pp. 239-245
Bioline Code: oc10042
Full paper language: English
Document type: Research Article
Document available free of charge

Memórias do Instituto Oswaldo Cruz, Vol. 105, No. 3, 2010, pp. 239-245

 en The biological in vitro effect and selectivity of aromatic dicationic compounds on Trypanosoma cruzi check for this species in other resources
da Silva, Cristiane França; da Silva, Patrícia Bernadino; Batista, Marcos Meuser; Daliry, Anissa; Tidwell, Richard Ryyy & Soeiro, Maria de Nazaré Correia

Abstract

Trypanosoma cruzi check for this species in other resources is a parasite that causes Chagas disease, which affects millions of individuals in endemic areas of Latin America. One hundred years after the discovery of Chagas disease, it is still considered a neglected illness because the available drugs are unsatisfactory. Aromatic compounds represent an important class of DNA minor groove-binding ligands that exhibit potent antimicrobial activity. This study focused on the in vitro activity of 10 aromatic dicationic compounds against bloodstream trypomastigotes and intracellular forms of T. cruzi. Our data demonstrated that these compounds display trypanocidal effects against both forms of the parasite and that seven out of the 10 compounds presented higher anti-parasitic activity against intracellular parasites compared with the bloodstream forms. Additional assays to determine the potential toxicity to mammalian cells showed that the majority of the dicationic compounds did not considerably decrease cellular viability. Fluorescent microscopy analysis demonstrated that although all compounds were localised to a greater extent within the kinetoplast than the nucleus, no correlation could be found between compound activity and kDNA accumulation. The present results stimulate further investigations of this class of compounds for the rational design of new chemotherapeutic agents for Chagas disease.

Keywords
aromatic compounds, Trypanosoma cruzi, chemotherapy, Chagas disease

 
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