In vitro evaluation of new terpenoid derivatives against Leishmania infantum and Leishmania braziliensis.


Ramírez-Macías, I; Marín, C; Chahboun, R; Olmo, F; Messouri, I; Huertas, O; Rosales, MJ; Gutierrez-Sánchez, R; Alvarez-Manzaneda, E; Sánchez-Moreno, M; (2012) In vitro evaluation of new terpenoid derivatives against Leishmania infantum and Leishmania braziliensis. Memorias do Instituto Oswaldo Cruz, 107 (3). pp. 370-6. ISSN 0074-0276 DOI: https://doi.org/10.1590/S0074-02762012000300012

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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.

Item Type: Article
Faculty and Department: Faculty of Infectious and Tropical Diseases > Dept of Pathogen Molecular Biology
Research Centre: Neglected Tropical Diseases Network
PubMed ID: 22510833
Web of Science ID: 302933000012
URI: http://researchonline.lshtm.ac.uk/id/eprint/2928918

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