Activity of novel aromatic compounds against Trypanosoma cruzi

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PUCE - Quito
Background: The parasitic hemoflagellate protozoan Trypanosoma cruzi is the causative agent of Chagas Disease (CD), a tropical infection affecting mainly low-income population segments in Latin America, where it is one of the leading parasitic infections. Nifurtimox (NFX) and benznidazole (BNZ) are the only two drugs currently approved to treat infections with T. cruzi; however, they frequently induce serious side effects while their efficacy is unsatisfactory. Therefore, identification of novel compounds displaying specific activity against T. cruzi is of high interest, as a basis for development of new drugs to treat CD. Methods. Seven novel aromatic compounds were evaluated. In vitro activity against the recombinant Tulahuen ß-gal strain of T. cruzi was measured employing colorimetric assays for ß-gal activity. Cytotoxicity against cultured mammalian cells was evaluated via resazurin reduction assays. BNZ was used as a reference drug. Results: All studied compounds presented activity against T. cruzi in vitro; however, five of them also induced significant host-cell damage, suggesting their toxicity is not specific. Compounds 3K and 3L showed no cytotoxicity measurable up to 100 µM concentrations, while displaying IC50 values against T. cruzi of 1.464 and 2.717 µM, respectively. In the same assay, BNZ, displayed an IC50 value of 1.558 µM and no cytotoxicity at concentrations up to 100 µM. Conclusions: Two compounds evaluated in the study are selectively toxic against intracellular T. cruzi amastigotes in vitro and did not display cytotoxic activity against mammalian cells. Their IC50 values are comparable to those obtained for BNZ, the reference drug. Novel compounds with specific anti-T. cruzi activity can be further explored in the search for options for CD treatment.
Enfermedad de Chagas, Compuestos aromáticos, Citotoxicidad, Trypanosoma cruzi, Nifurtimox, Benzinidazol