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We describe herein an evaluation of trypanocidal effects of the natural alkaloid piperine and twelve synthetic derivatives against epimastigote and amastigote forms of the protozoan parasite Trypanosoma cruzi, the causative agent of the incurable human disease, Chagas'' disease. The results obtained point to piperine as a suitable template for the development of new drugs with trypanocidal activity. [Copyright &y& Elsevier]

Abstract: Himatanthus sucuuba (HsL) latex exhibited a potent leishmanicidal activity against intracellular amastigotes of Leishmania amazonensis, a causative agent of cutaneous leishmaniasis. HsL inhibited intracellular amastigote growth in a dose-dependent manner (IC50 =15.7µg/mL). Moreover, HsL increased nitric oxide (NO) and Tumor Nuclear Factor-α (TNF-α) and decreased Transforming Growth Factor-β (TGF-β) production in macrophages. As assessed by plasma membrane integrity and mitochondrial activity, HsL showed low toxicity for host macrophages. HsL in vivo was active by the oral route, reducing the parasite load in established footpad lesions after only five doses. In summary, these findings support HsL as an interesting candidate for further evaluations regarding its potential application as a therapeutical agent against Leishmania. [Copyright &y& Elsevier]