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• dos Santos, VA. F. F. M.
• Leite, KM.
• da Costa Siqueira, M
• Regasini, LO.
• Martinez, I
• Nogueira, CT.
• Galuppo, MKolos
• Stolf, BS.
• Pereira, AMaria Soares
• Cicarelli, RM. B.
• Furlan, M
• Graminha, MA. S.
• [+] on Google Scholar
• dos Santos, VA. F. F. M.
• Leite, KM.
• da Costa Siqueira, M
• Regasini, LO.
• Martinez, I
• Nogueira, CT.
• Galuppo, MKolos
• Stolf, BS.
• Pereira, AMaria Soares
• Cicarelli, RM. B.
• Furlan, M
• Graminha, MA. S.
• [+] on PubMed
• dos Santos, VA. F. F. M.
• Leite, KM.
• da Costa Siqueira, M
• Regasini, LO.
• Martinez, I
• Nogueira, CT.
• Galuppo, MKolos
• Stolf, BS.
• Pereira, AMaria Soares
• Cicarelli, RM. B.
• Furlan, M
• Graminha, MA. S.

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

Article

Antiprotozoal Activity of Quinonemethide Triterpenes from Maytenus ilicifolia (Celastraceae)

Vania A. F. F. M. dos Santos ^1,† , Karoline M. Leite ^2,† , Mariana da Costa Siqueira ² , Luis O. Regasini ¹ , Isabel Martinez ² , Camila T. Nogueira ² , Mariana Kolos Galuppo ³ , Beatriz S. Stolf ³ , Ana Maria Soares Pereira ⁴ , Regina M. B. Cicarelli ² , Maysa Furlan ¹  and Marcia A. S. Graminha ^2,*

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)

Download PDF Full-Text [229 KB, Updated Version, uploaded 23 January 2013 09:43 CET]

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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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