Abstract
Sesquiterpene lactones are naturally occurring compounds mainly found in the Asteraceae family. These types of plant metabolites display a wide range of biological activities, including antiprotozoal activity and are considered interesting structures for drug discovery. Four derivatives were synthesized from estafietin (1), isolated from Stevia alpina (Asteraceae): 11βH,13-dihydroestafietin (2), epoxyestafietin (3a and 3b), 11βH,13-methoxyestafietin, (4) and 11βH,13-cianoestafietin. The antiprotozoal activity against Trypanosoma cruzi and Leishmania braziliensis of these compounds was evaluated. Epoxyestafietin was the most active compound against T. cruzi trypomastigotes and amastigotes (IC50 values of 18.7 and 2.0 µg/mL, respectively). Estafietin (1) and 11βH,13-dihydroestafietin (2) were the most active and selective compounds on L. braziliensis promastigotes (IC50 values of 1.0 and 1.3 μg/mL, respectively). The antiparasitic activity demonstrated by estafietin and some of its derivatives make them promising candidates for the development of effective compounds for the treatment of Chagas disease and leihsmaniasis.
Highlights
Sesquiterpenelactones (STLs) are a family of naturally occurring compounds mainly found in the Astaeraceae family, though not exclusively
On day 6 post-infection, the assays and compounds were added at 0–100 μg/mL in 150 μL medium
Infected untreated mammalian cells were used as 6 h and the optical density was read at 570 nm
Summary
Sesquiterpenelactones (STLs) are a family of naturally occurring compounds mainly found in the Astaeraceae family, though not exclusively. The possibility of introducing structural modifications to improve its pharmacological properties (efficacy, selectivity, solubility, andtoxicity) has radically modified the panorama and has made its therapeutic application feasible [9,10] In this sense, simple modifications made either on the lactone ring (opening, dihydrogenation) or on functional groups (OH, COOH) could be a strategy to improve the biological activities or reduce the toxicity [10,11]. T. cruzi has a complex life cycle with four distinct developmental forms that alternate between the insect vector (epimastigotes and metacyclic trypomastigotes) and the mammalian host (bloodstream trypomastigotes and amastigotes) This parasitosis has a worldwide distribution, with the highest prevalence values occurring in Latin America. Each compound was tested for their cytotoxicity on mammalian cells
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