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
Article
in English
| 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.
Full text:
Available
Index:
LILACS (Americas)
Main subject:
Terpenes
/
Leishmania braziliensis
/
Leishmania infantum
/
Macrophages
/
Antiprotozoal Agents
Limits:
Animals
Country/Region as subject:
South America
/
Brazil
Language:
English
Journal:
Mem. Inst. Oswaldo Cruz
Journal subject:
Tropical Medicine
/
Parasitology
Year:
2012
Type:
Article
/
Project document
Affiliation country:
Spain
Institution/Affiliation country:
University of Granada/ES
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