In Vitro and in Vivo Activity of an Organic Tellurium Compound on Leishmania (Leishmania) chagasi

In Vitro and in Vivo Activity of an Organic Tellurium Compound on Leishmania (Leishmania) chagasi

Author Pimentel, Isabella Aparecida Salerno Autor UNIFESP Google Scholar
Paladi, Carolina de Siqueira Autor UNIFESP Google Scholar
Katz, Simone Autor UNIFESP Google Scholar
Judice, Wagner Alves de Souza Autor UNIFESP Google Scholar
Cunha, Rodrigo Luiz Oliveira Rodrigues Autor UNIFESP Google Scholar
Barbieri, Clara Lucia Autor UNIFESP Google Scholar
Institution Universidade Federal de São Paulo (UNIFESP)
Univ Mogi das Cruzes
Universidade Federal do ABC (UFABC)
Abstract Tellurium compounds have shown several biological properties and recently the leishmanicidal effect of one organotellurane was demonstrated. These findings led us to test the effect of the organotellurium compound RF07 on Leishmania (Leishmania) chagasi, the agent of visceral leishmaniasis in Latin America. in vitro assays were performed in L. (L.) chagasi-infected bone marrow derived macrophages treated with different concentrations of RF07. in in vivo experiments Golden hamsters were infected with L. (L.) chagasi and injected intraperitoneally with RF07 whereas control animals received either Glucantime or PBS. the effect of RF07 on cathepsin B activity of L. (L.) chagasi amastigotes was assayed spectrofluorometrically using fluorogenic substrates. the main findings were: 1) RF07 showed significant leishmanicidal activity against intracellular parasites at submicromolar concentrations (IC50 of 529.7+/-26.5 nM), and the drug displayed 10-fold less toxicity to macrophages (CC50 of 5,426+/-272.8 nM); 2) kinetics assays showed an increasing leishmanicidal action of RF07 at longer periods of treatment; 3) one month after intraperitoneal injection of RF07 L. (L.) chagasi-infected hamsters showed a reduction of 99.6% of parasite burden when compared to controls that received PBS; 4) RF07 inhibited the cathepsin B activity of L. (L.) chagasi amastigotes. the present results demonstrated that the tellurium compound RF07 is able to destroy L. (L.) chagasi in vitro and in vivo at concentrations that are non toxic to the host. We believe these findings support further study of the potential of RF07 as a possible alternative for the chemotherapy of visceral leishmaniasis.
Language English
Sponsor Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
Instituto de Pesquisa, Informacao e Tecnologia da Amazonia (IPITAM)
Date 2012-11-07
Published in Plos One. San Francisco: Public Library Science, v. 7, n. 11, 7 p., 2012.
ISSN 1932-6203 (Sherpa/Romeo, impact factor)
Publisher Public Library Science
Extent 7
Access rights Open access Open Access
Type Article
Web of Science ID WOS:000311935800130

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