Antiprotozoal Activity of Quinonemethide Triterpenes from Maytenus ilicifolia (Celastraceae)

Molecules

Vania A. F. F. M. dos Santos¹  Karoline M. Leite¹  Mariana da Costa Siqueira¹  Luis O. Regasini¹  Isabel Martinez¹  Camila T. Nogueira¹  Mariana Kolos Galuppo¹  Beatriz S. Stolf¹  Ana Maria Soares Pereira¹  Regina M. B. Cicarelli¹  Maysa Furlan¹ 

[1] ¹Instituto de Quimica, Universidade Estadual Paulista, UNESP, PO BOX 355, Araraquara-SP 14801-970, Brazil

关键词: Celastraceae;    Maytenus ilicifolia;    leishmanicidal;    trypanocidal;    quinone-methide triterpenes;    maytenin;    pristimerin;   

DOI  :  10.3390/molecules18011053

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
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