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Antiprotozoal Activity of Quinonemethide Triterpenes from Maytenus ilicifolia (Celastraceae)
by
Vania A. F. F. M. Dos Santos, Karoline M. Leite, Mariana Da Costa Siqueira, Luis O. Regasini, Isabel Martinez, Camila T. Nogueira, Mariana Kolos Galuppo, Beatriz S. Stolf, Ana Maria Soares Pereira, Regina M. B. Cicarelli, Maysa Furlan and Marcia A. S. Graminha
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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
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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 (IC
50) values of less than 0.88 nM. Both compounds showed IC
50 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.
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