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Memórias do Instituto Oswaldo Cruz
Fundação Oswaldo Cruz, Fiocruz
ISSN: 1678-8060
EISSN: 1678-8060
Vol. 107, No. 3, 2012, pp. 370-376
Bioline Code: oc12053
Full paper language: English
Document type: Research Article
Document available free of charge

Memórias do Instituto Oswaldo Cruz, Vol. 107, No. 3, 2012, pp. 370-376

 en In vitro evaluation of new terpenoid derivatives against Leishmania infantum check for this species in other resources and Leishmania braziliensis check for this species in other resources
Ramírez-Macías, Inmaculada; Marín, Clotilde; Chahboun, Rachid; Olmo, Francisco; Messouri, Ibtisam; Huertas, Oscar; Rosales, María Jose; Gutierrez-Sánchez, Ramón; Alvarez-Manzaneda, Enrique & Sánchez-Moreno, Manuel

Abstract

The activity of five (1-5) abietane phenol derivatives against Leishmania infantum check for this species in other resources and Leishmania braziliensis check for this species in other resources 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.

Keywords
abietane phenol compounds - Leishmania infantum - Leishmania braziliensis - biological evaluation of activity - promastigote - amastigote forms

 
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