In vitro evaluation of new terpenoid derivatives against Leishmania infantum and Leishmania braziliensis
Mem. Inst. Oswaldo Cruz
;
107(3): 370-376, May 2012. ilus, graf, tab
Artículo
en Inglés
| LILACS
| ID: lil-624019
ABSTRACT
The activity of five (1-5) abietane phenol derivatives against Leishmania infantum and Leishmania braziliensis was studied using promastigotes and axenic and intracellular amastigotes. Infectivity and cytotoxicity tests were performed with J774.2 macrophage cells using Glucantime as a reference drug. The mechanisms of action were analysed by performing metabolite excretion and transmission electron microscopy ultrastructural studies. Compounds 1-5 were more active and less toxic than Glucantime. The infection rates and mean number of parasites per cell observed in amastigote experiments showed that derivatives 2, 4 and 5 were the most effective against both L. infantum and L. braziliensis. The ultrastructural changes observed in the treated promastigote forms confirmed that the greatest cell damage was caused by the most active compound (4). Only compound 5 caused changes in the nature and amounts of catabolites excreted by the parasites, as measured by ¹H nuclear magnetic resonance spectroscopy. All of the assayed compounds were active against the two Leishmania species in vitro and were less toxic in mammalian cells than the reference drug.
Texto completo:
Disponible
Índice:
LILACS (Américas)
Asunto principal:
Terpenos
/
Leishmania braziliensis
/
Leishmania infantum
/
Macrófagos
/
Antiprotozoarios
Límite:
Animales
País/Región como asunto:
America del Sur
/
Brasil
Idioma:
Inglés
Revista:
Mem. Inst. Oswaldo Cruz
Asunto de la revista:
Medicina Tropical
/
Parasitología
Año:
2012
Tipo del documento:
Artículo
/
Documento de proyecto
País de afiliación:
España
Institución/País de afiliación:
University of Granada/ES
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