Molecules 2013, 18(1), 1053-1062; doi:10.3390/molecules18011053

Antiprotozoal Activity of Quinonemethide Triterpenes from Maytenus ilicifolia (Celastraceae)

1 Instituto de Quimica, Universidade Estadual Paulista, UNESP, PO BOX 355, Araraquara-SP 14801-970, Brazil 2 Faculdade de Ciencias Farmaceuticas, Universidade Estadual Paulista, UNESP, Araraquara-SP 14801-902, Brazil 3 Instituto de Ciencias Biomedicas, Universidade de São Paulo, São Paulo 05508-000, Brazil 4 Departamento de Biotecnologia Vegetal, Universidade de Ribeirão Preto, Ribeirão Preto-SP 14096-900, Brazil These authors contributed equally to this work.
* Author to whom correspondence should be addressed.
Received: 19 November 2012; in revised form: 18 December 2012 / Accepted: 21 December 2012 / Published: 15 January 2013
(This article belongs to the Special Issue Triterpenes and Triterpenoids)
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Abstract: The present study describes the leishmanicidal and trypanocidal activities of two quinonemethide triterpenes, maytenin (1) and pristimerin (2), isolated from Maytenus ilicifolia root barks (Celastraceae). The compounds were effective against the Trypanosomatidae Leishmania amazonensis and Leishmania chagasi and Trypanosoma cruzi, etiologic agents of leishmaniasis and Chagas’ disease, respectively. The quinonemethide triterpenes 1 and 2 exhibited a marked in vitro leishmanicidal activity against promastigotes and amastigotes with 50% inhibitory concentration (IC50) values of less than 0.88 nM. Both compounds showed IC50 lower than 0.3 nM against Trypanosoma cruzi epimastigotes. The selectivity indexes (SI) based on BALB/c macrophages for L. amazonensis and L. chagasi were 243.65 and 46.61 for (1) and 193.63 and 23.85 for (2) indicating that both compounds presented high selectivity for Leishmania sp. The data here presented suggests that these compounds should be considered in the development of new and more potent drugs for the treatment of leishmaniasis and Chagas’ disease.
Keywords: Celastraceae; Maytenus ilicifolia; leishmanicidal; trypanocidal; quinone-methide triterpenes; maytenin; pristimerin

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MDPI and ACS Style

dos Santos, V.A.F.F.M.; Leite, K.M.; da Costa Siqueira, M.; Regasini, L.O.; Martinez, I.; Nogueira, C.T.; Galuppo, M.K.; Stolf, B.S.; Pereira, A.M.S.; Cicarelli, R.M.B.; Furlan, M.; Graminha, M.A.S. Antiprotozoal Activity of Quinonemethide Triterpenes from Maytenus ilicifolia (Celastraceae). Molecules 2013, 18, 1053-1062.

AMA Style

dos Santos VAFFM, Leite KM, da Costa Siqueira M, Regasini LO, Martinez I, Nogueira CT, Galuppo MK, Stolf BS, Pereira AMS, Cicarelli RMB, Furlan M, Graminha MAS. Antiprotozoal Activity of Quinonemethide Triterpenes from Maytenus ilicifolia (Celastraceae). Molecules. 2013; 18(1):1053-1062.

Chicago/Turabian Style

dos Santos, Vania A.F.F.M.; Leite, Karoline M.; da Costa Siqueira, Mariana; Regasini, Luis O.; Martinez, Isabel; Nogueira, Camila T.; Galuppo, Mariana K.; Stolf, Beatriz S.; Pereira, Ana M.S.; Cicarelli, Regina M.B.; Furlan, Maysa; Graminha, Marcia A.S. 2013. "Antiprotozoal Activity of Quinonemethide Triterpenes from Maytenus ilicifolia (Celastraceae)." Molecules 18, no. 1: 1053-1062.

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