RESUMEN
Bioguided-fractionation of the methanol extract of the leaves of Careya arborea led to isolation of a triterpenoid saponin, designated arborenin, and characterized as 3-O-beta-D-glucopyranosyl(1-->2)-beta-D-glucopyranosyl-2 alpha,3beta-dihydroxy-taraxast-20-en-28-oic acid (1), together with desacylescin III (2). The structures were determined on the basis of extensive 2D NMR spectroscopic analysis. The saponin showed in vitro antileishmanial activity against Leishmania donovani (strain AG 83).
Asunto(s)
Antiprotozoarios/farmacología , Lecythidaceae/química , Leishmania donovani/efectos de los fármacos , Hojas de la Planta/química , Saponinas/farmacología , Triterpenos/farmacología , Animales , Antiprotozoarios/química , Antiprotozoarios/aislamiento & purificación , Secuencia de Carbohidratos , Espectroscopía de Resonancia Magnética/métodos , Espectroscopía de Resonancia Magnética/normas , Conformación Molecular , Datos de Secuencia Molecular , Pruebas de Sensibilidad Parasitaria , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Estándares de Referencia , Saponinas/química , Saponinas/aislamiento & purificación , Triterpenos/química , Triterpenos/aislamiento & purificaciónRESUMEN
Some novel quinoline derivatives were prepared and tested for antileishmanial activity. 2-(2-Methylquinolin-4-ylamino)-N-phenylacetamide (2) was found to be significantly more active than the standard antileishmanial drug sodium antimony gluconate (SAG) in reducing the parasite load both in the spleen and liver at a much lower concentration in hamster models. The results suggest that the compound could be exploited as an antileishmanial drug.