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
Artigo
em Inglês
| LILACS
| ID: lil-624019
Biblioteca responsável:
BR1.1
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:
Disponível
Coleções:
Bases de dados internacionais
Contexto em Saúde:
Doenças Negligenciadas
Problema de saúde:
Zoonoses
Base de dados:
LILACS
Assunto principal:
Terpenos
/
Leishmania braziliensis
/
Leishmania infantum
/
Macrófagos
/
Antiprotozoários
Limite:
Animais
País/Região como assunto:
América do Sul
/
Brasil
Idioma:
Inglês
Revista:
Mem. Inst. Oswaldo Cruz
Assunto da revista:
Medicina Tropical
/
Parasitologia
Ano de publicação:
2012
Tipo de documento:
Artigo
/
Documento de projeto
País de afiliação:
Espanha
Instituição/País de afiliação:
University of Granada/ES