title: Antiprotozoal activity of quinonemethide triterpenes from Maytenus ilicifolia (Celastraceae).
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 (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.
authors: Instituto de Quimica, Universidade Estadual Paulista, UNESP, PO BOX 355, Araraquara-SP 14801-970, Brazil.
authors: Vania A F F M
authors: VA
authors: Dos Santos
authors: Karoline M
authors: KM
authors: Leite
authors: Mariana
authors: M
authors: da Costa Siqueira
authors: Luis O
authors: LO
authors: Regasini
authors: Isabel
authors: I
authors: Martinez
authors: Camila T
authors: CT
authors: Nogueira
authors: Mariana Kolos
authors: MK
authors: Galuppo
authors: Beatriz S
authors: BS
authors: Stolf
authors: Ana Maria Soares
authors: AM
authors: Pereira
authors: Regina M B
authors: RM
authors: Cicarelli
authors: Maysa
authors: M
authors: Furlan
authors: Marcia A S
authors: MA
authors: Graminha
mesh_terms: D000818:Animals; D002478:Cells, Cultured; D020128:Inhibitory Concentration 50; D007891:Leishmania / Q000187:drug effects; D007928:Lethal Dose 50; D008264:Macrophages / Q000187:drug effects / Q000469:parasitology / Q000502:physiology; D029755:Maytenus / Q000737:chemistry*; D051379:Mice; D008807:Mice, Inbred BALB C; D010936:Plant Extracts / Q000494:pharmacology* / Q000633:toxicity; D018517:Plant Roots / Q000737:chemistry; D011809:Quinones / Q000494:pharmacology* / Q000633:toxicity; D014315:Triterpenes / Q000494:pharmacology* / Q000633:toxicity; D014344:Trypanocidal Agents / Q000494:pharmacology* / Q000633:toxicity; D014349:Trypanosoma cruzi / Q000187:drug effects
chemical_list: D010936:Plant Extracts; D011809:Quinones; D014315:Triterpenes; D014344:Trypanocidal Agents