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

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dc.contributor.author Pimentel, Isabella Aparecida Salerno [UNIFESP]
dc.contributor.author Paladi, Carolina de Siqueira [UNIFESP]
dc.contributor.author Katz, Simone [UNIFESP]
dc.contributor.author Judice, Wagner Alves de Souza [UNIFESP]
dc.contributor.author Cunha, Rodrigo Luiz Oliveira Rodrigues [UNIFESP]
dc.contributor.author Barbieri, Clara Lucia [UNIFESP]
dc.date.accessioned 2016-01-24T14:28:00Z
dc.date.available 2016-01-24T14:28:00Z
dc.date.issued 2012-11-07
dc.identifier http://dx.doi.org/10.1371/journal.pone.0048780
dc.identifier.citation Plos One. San Francisco: Public Library Science, v. 7, n. 11, 7 p., 2012.
dc.identifier.issn 1932-6203
dc.identifier.uri http://repositorio.unifesp.br/handle/11600/35501
dc.description.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. en
dc.description.sponsorship Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorship Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
dc.description.sponsorship Instituto de Pesquisa, Informacao e Tecnologia da Amazonia (IPITAM)
dc.format.extent 7
dc.language.iso eng
dc.publisher Public Library Science
dc.relation.ispartof Plos One
dc.rights Acesso aberto
dc.title In Vitro and in Vivo Activity of an Organic Tellurium Compound on Leishmania (Leishmania) chagasi en
dc.type Artigo
dc.contributor.institution Universidade Federal de São Paulo (UNIFESP)
dc.contributor.institution Univ Mogi das Cruzes
dc.contributor.institution Universidade Federal do ABC (UFABC)
dc.description.affiliation Universidade Federal de São Paulo, Escola Paulista Med, Dept Microbiol Imunol & Parasitol, São Paulo, Brazil
dc.description.affiliation Univ Mogi das Cruzes, Ctr Interdisciplinar Invest Bioquim, São Paulo, Brazil
dc.description.affiliation Univ Fed ABC, Ctr Ciencias Nat & Humanas, São Paulo, Brazil
dc.description.affiliationUnifesp Universidade Federal de São Paulo, Escola Paulista Med, Dept Microbiol Imunol & Parasitol, São Paulo, Brazil
dc.identifier.file WOS000311935800130.pdf
dc.identifier.doi 10.1371/journal.pone.0048780
dc.description.source Web of Science
dc.identifier.wos WOS:000311935800130



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