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dc.contributor.authorPietra, Renata Celi Carvalho de Souza
dc.contributor.authorRodrigues, Lucas Fonseca
dc.contributor.authorTeixeira, Eliane de Moraes
dc.contributor.authorFried, Levi
dc.contributor.authorLefkove, Benjamin
dc.contributor.authorRabello, Ana Lucia Teles
dc.contributor.authorArbiser, Jack
dc.contributor.authorFerreira, Lucas Antônio Miranda
dc.contributor.authorFernandes, Ana Paula
dc.date.accessioned2018-11-21T13:09:45Z
dc.date.available2018-11-21T13:09:45Z
dc.date.issued2013
dc.identifier.citationPIETRA, Renata Celi Carvalho de Souza et al. Triphenylmethane Derivatives Have High In Vitro and In Vivo Activity against the Main Causative Agents of Cutaneous Leishmaniasis. PLoS One, v. 8, n. 1, e51864, 2013
dc.identifier.issn1932-6203
dc.identifier.urihttps://www.arca.fiocruz.br/handle/icict/30120
dc.language.isoeng
dc.publisherPublic Library of Science
dc.rightsopen access
dc.subject.otherdoenças parasitarias
dc.subject.otherleishmaniose
dc.subject.otherPromastigotas
dc.subject.otherMacrofagos
dc.subject.otherAmastigotas
dc.titleTriphenylmethane Derivatives Have High In Vitro and In Vivo Activity against the Main Causative Agents of Cutaneous Leishmaniasis
dc.typeArticle
dc.identifier.doi10.1371/journal.pone.0051864
dc.description.abstractenThe current standard of care for cutaneous leishmaniasis (CL) is organic antimonial compounds, but the administration of these compounds is complicated by a low therapeutic - toxic index, as well as parenteral administration. Thus, there is an urgent need for the development of new and inexpensive therapies for the treatment of CL. In this study, we evaluate the activity of the triphenylmethane (TPM) class of compounds against three species of Leishmania which are pathogenic in humans. The TPM have a history of safe use in humans, dating back to the use of the original member of this class, gentian violet (GV), from the early 20th century. Initially, the in vitro efficacy against Leishmania (Viannia) braziliensis, L. (Leishmania) amazonensis and L. (L.) major of 9 newly synthesized TPM, in addition to GV, was tested. Inhibitory concentrations (IC) IC50 of 0.025 to 0.84 µM had been found in promastigotes in vitro assays. The four most effective compounds were then tested in amastigote intracellular assays, resulting in IC50 of 0.10 to 1.59 µM. A high degree of selectivity of antiparasitic activity over toxicity to mammalian cells was observed. Afterwards, GV and TPM 6 were tested in a topical formulation in mice infected with L. (L.) amazonensis leading to elimination of parasite burdens at the site of lesion/infection. These results demonstrated that TPM present significant anti-leishmanial activities and provide a rationale for human clinical trials of GV and other TPM. TPM are inexpensive and safe, thus using them for treatment of CL may have a major impact on public health.
dc.creator.affilliationUniversidade Federal de Minas Gerais. Departamento de Análises Clínicas e Toxicológicas.Belo Horizonte, MG, Brazil
dc.creator.affilliationUniversidade Federal de Minas Gerais. Departamento de Análises Clínicas e Toxicológicas.Belo Horizonte, MG, Brazil
dc.creator.affilliationFundação Oswaldo Cruz. Instituto René Rachou. Laboratório de Pesquisa Clínica. Belo Horizonte, MG, Brasil.
dc.creator.affilliationDepartment of Dermatology. Emory University School of Medicine. Atlanta, Georgia, United States of America.
dc.creator.affilliationDepartment of Dermatology. Emory University School of Medicine. Atlanta, Georgia, United States of America.
dc.creator.affilliationFundação Oswaldo Cruz. Instituto René Rachou. Laboratório de Pesquisa Clínica. Belo Horizonte, MG, Brasil.
dc.creator.affilliationDepartment of Dermatology. Emory University School of Medicine. Atlanta, Georgia, United States of America.
dc.creator.affilliationUniversidade Federal de Minas Gerais. Departamento de Análises Clínicas e Toxicológicas.Belo Horizonte, MG, Brazil
dc.creator.affilliationUniversidade Federal de Minas Gerais. Departamento de Análises Clínicas e Toxicológicas.Belo Horizonte, MG, Brazil
dc.subject.enParasitic diseases
dc.subject.enLeishmania
dc.subject.enPromastigotes
dc.subject.enMacrophages
dc.subject.enAmastigotes
dc.subject.enCytotoxicity
dc.subject.enLeishmaniasis
dc.subject.enMTT assay
Appears in Collections:MG - IRR - Artigos de Periódicos

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