Abstract

LEAL PINTO, Sandra Milena et al. Activity against Trypanosoma cruzi, Leishmania chagasi and mammalian cells of new N-benzyl (2-furylmethyl) cinnamamides. Rev. Univ. Ind. Santander. Salud [online]. 2009, vol.41, n.3, pp.275-279. ISSN 0121-0807.

Introduction: The chemotherapy against leishmaniasis and Chagas disease is ineffective, a condition that is aggravating the public health problem caused by these tropical diseases. Objective: To determine the activity of new N-benzyl(2-furylmethyl) cinnamamides in the free and intracellular forms of Leishmania chagasi and Trypanosoma cruzi and Vero and THP-1 cells. Materials and methods: The parasites and cells were treated with different concentrations of the compounds and the activity was determined microscopically and MTT colorimetric test in the case of parasites and mammalian cells. Antiparasitic activity of tested compounds was expressed as the concentration that inhibits or destroys 50% or 90% of parasites and cells. Results: The N-arylalkylamides 1, 2 and 5 were active against T. cruzi epimastigotes with a range of activities between IC₅₀ 3.71-38.81 μM and IC₉₀ between 50.87-59.87 μM. The compound 2 was active on intracellular amastigotes of L. chagasi with IC₅₀ 77.76 μM. The tested amides were not toxic to THP-1 cells; just only compound 4 resulted partially toxic on Vero cells (CC₅₀ 65.9 ± 5.71 μM). Conclusions: The low toxicity and the antiparasitic activity showed by the cinnamanide compounds 1, 2 and 5 support the design of new related molecules in order to be evaluated on in vitro and in vivo systems for these parasitic diseases. Salud UIS 2009; 41: 275-279.

Keywords : Leishmaniasis; Chagas disease; intracellular amastigote; cytotoxicity; N-substituted cinnamamides.

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