title: Drimanes from Drimys brasiliensis with leishmanicidal and antimalarial activity.
abstract: This paper evaluates CHCl3 and CH3OH extracts of the stem bark, branches and leaves of Drimys brasiliensis and drimane sesquiterpenes isolated from the stem bark against strains of Leishmania amazonensis and Leishmania braziliensis promastigotes and Plasmodium falciparum trophozoites. All of the extracts and compounds were tested in cell lines in comparison with reference standards and cell viability was determined by the XTT method. The CHCl3 and CH3OH extracts from the stem bark and branches yielded promising results against two strains of Leishmania, with 50% inhibitory concentrations (IC50 ) values ranging from 39-100 µg/mL. The CHCl3 extract of the stem bark returned IC50 values of 39 and 40.6 µg/mL for L. amazonensis and L. braziliensis, respectively. The drimanes were relatively effective: 1-β-(p-coumaroyloxy)-polygodial produced IC50 values of 5.55 and 2.52 µM for L. amazonensis and L. braziliensis, respectively, compared with 1-β-(p-methoxycinnamoyl)-polygodial, which produced respective IC50 values of 15.85 and 17.80 µM. The CHCl3 extract demonstrated activity (IC50 of 3.0 µg/mL) against P. falciparum. The IC50 values of 1-β-(p-cumaroyloxyl)-polygodial and 1-β-(p-methoxycinnamoyl)-polygodial were 1.01 and 4.87 µM, respectively, for the trophozoite strain. Therefore, the results suggest that D. brasiliensis is a promising plant from which to obtain new and effective antiparasitic agents.
authors.affiliation: Programa de Mestrado em Ciências Farmacêuticas, Universidade do Vale do Itajaí, Itajaí, SC, Brasil.
authors.forename: Vanessa Duarte
authors.initials: VD
authors.lastname: Claudino
authors.forename: Kesia Caroline
authors.initials: KC
authors.lastname: da Silva
authors.forename: Valdir
authors.initials: V
authors.lastname: Cechinel Filho
authors.forename: Rosendo Augusto
authors.initials: RA
authors.lastname: Yunes
authors.forename: Franco
authors.initials: F
authors.lastname: Delle Monache
authors.forename: Alberto
authors.initials: A
authors.lastname: Giménez
authors.forename: Efrain
authors.initials: E
authors.lastname: Salamanca
authors.forename: David
authors.initials: D
authors.lastname: Gutierrez-Yapu
authors.forename: Angela
authors.initials: A
authors.lastname: Malheiros
mesh_terms: D000962:Antimalarials / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D032424:Drimys / Q000737:chemistry*; D020128:Inhibitory Concentration 50; D007892:Leishmania braziliensis / Q000187:drug effects*; D007894:Leishmania mexicana / Q000187:drug effects*; D021261:Parasitic Sensitivity Tests; D010936:Plant Extracts / Q000494:pharmacology*; D010963:Plasmodium falciparum / Q000187:drug effects*; D000081223:Polycyclic Sesquiterpenes; D012717:Sesquiterpenes / Q000494:pharmacology*
chemical_list: D000962:Antimalarials; D000981:Antiprotozoal Agents; D010936:Plant Extracts; D000081223:Polycyclic Sesquiterpenes; D012717:Sesquiterpenes; C437376:drimane