Activity of Estafietin and Analogues on Trypanosoma cruzi and Leishmania braziliensis
AbstractSesquiterpene 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. View Full-Text
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Sülsen, V.P.; Lizarraga, E.F.; Elso, O.G.; Cerny, N.; Sanchez Alberti, A.; Bivona, A.E.; Malchiodi, E.L.; Cazorla, S.I.; Catalán, C.A.N. Activity of Estafietin and Analogues on Trypanosoma cruzi and Leishmania braziliensis. Molecules 2019, 24, 1209.
Sülsen VP, Lizarraga EF, Elso OG, Cerny N, Sanchez Alberti A, Bivona AE, Malchiodi EL, Cazorla SI, Catalán CAN. Activity of Estafietin and Analogues on Trypanosoma cruzi and Leishmania braziliensis. Molecules. 2019; 24(7):1209.Chicago/Turabian Style
Sülsen, Valeria P.; Lizarraga, Emilio F.; Elso, Orlando G.; Cerny, Natacha; Sanchez Alberti, Andrés; Bivona, Augusto E.; Malchiodi, Emilio L.; Cazorla, Silvia I.; Catalán, César A.N. 2019. "Activity of Estafietin and Analogues on Trypanosoma cruzi and Leishmania braziliensis." Molecules 24, no. 7: 1209.
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