Please use this identifier to cite or link to this item: https://www.arca.fiocruz.br/handle/icict/15959
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dc.contributor.authorSilva, Cristiane França da
dc.contributor.authorBatista, Denise da Gama Jaen
dc.contributor.authorOliveira, Gabriel Melo
dc.contributor.authorSouza, Elen Mello de
dc.contributor.authorHammer, Erica Ripoll
dc.contributor.authorSilva, Patricia Bernardino da
dc.contributor.authorDaliry, Anissa
dc.contributor.authorAraujo, Julianna Siciliano
dc.contributor.authorBritto, Constança
dc.contributor.authorRodrigues, Ana Carolina Mondaine
dc.contributor.authorLiu, Zongying
dc.contributor.authorFarahat, Abdelbasset A.
dc.contributor.authorKumar, Arvind
dc.contributor.authorBoykin, David W.
dc.contributor.authorSoeiro, Maria de Nazaré Correia
dc.date.accessioned2016-09-27T13:26:45Z
dc.date.available2016-09-27T13:26:45Z
dc.date.issued2012
dc.identifier.citationSILVA, Cristiane França da; et al. In Vitro and In Vivo Investigation of the Efficacy of Arylimidamide DB1831 and Its Mesylated Salt Form - DB1965 - against Trypanosoma cruzi Infection. PLoS One, v.7, n.1, e30356, 8p, Jan. 2012.
dc.identifier.issn1932-6203
dc.identifier.urihttps://www.arca.fiocruz.br/handle/icict/15959
dc.language.isoeng
dc.publisherPublic Library of Science
dc.rightsopen access
dc.subject.otherTrypanosoma cruzi
dc.subject.otherDoença de Chagas
dc.subject.otherArylimidamides
dc.subject.otherTratamento
dc.titleIn vitro and in vivo investigation of the efficacy of arylimidamide DB1831 and its mesylated salt form--DB1965--against Trypanosoma cruzi infection
dc.typeArticle
dc.identifier.doi10.1371/journal.pone.0030356
dc.description.abstractenChagas disease is caused by infection with the intracellular protozoan parasite Trypanosoma cruzi. At present, nifurtimox and benznidazole, both compounds developed empirically over four decades ago, represent the chemotherapeutic arsenal for treating this highly neglected disease. However, both drugs present variable efficacy depending on the geographical area and the occurrence of natural resistance, and are poorly effective against the later chronic stage. As a part of a search for new therapeutic opportunities to treat chagasic patients, pre-clinical studies were performed to characterize the activity of a novel arylimidamide (AIA--DB1831 (hydrochloride salt) and DB1965 (mesylate salt)) against T. cruzi. These AIAs displayed a high trypanocidal effect in vitro against both relevant forms in mammalian hosts, exhibiting a high selectivity index and a very high efficacy (IC(50) value/48 h of 5-40 nM) against intracellular parasites. DB1965 shows high activity in vivo in acute experimental models (mouse) of T. cruzi, showing a similar effect to benznidazole (Bz) when compared under a scheme of 10 daily consecutive doses with 12.5 mg/kg. Although no parasitological cure was observed after treating with 20 daily consecutive doses, a combined dosage of DB1965 (5 mg/kg) with Bz (50 mg/kg) resulted in parasitaemia clearance and 100% animal survival. In summary, our present data confirmed that aryimidamides represent promising new chemical entities against T. cruzi in therapeutic schemes using the AIA alone or in combination with other drugs, like benznidazole.
dc.creator.affilliationFundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil.
dc.creator.affilliationFundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil.
dc.creator.affilliationFundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil.
dc.creator.affilliationFundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil.
dc.creator.affilliationFundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil.
dc.creator.affilliationFundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil.
dc.creator.affilliationFundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil.
dc.creator.affilliationFundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil.
dc.creator.affilliationFundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Molecular e Doenças Endêmicas. Rio de Janeiro, RJ, Brasil.
dc.creator.affilliationFundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Molecular e Doenças Endêmicas. Rio de Janeiro, RJ, Brasil.
dc.creator.affilliationGeorgia State University. Department of Chemistry. Atlanta, GA, USA.
dc.creator.affilliationGeorgia State University. Department of Chemistry. Atlanta, GA, USA.
dc.creator.affilliationGeorgia State University. Department of Chemistry. Atlanta, GA, USA.
dc.creator.affilliationGeorgia State University. Department of Chemistry. Atlanta, GA, USA.
dc.creator.affilliationFundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil.
dc.subject.enTrypanosoma cruzi
dc.subject.enChagas Disease
dc.subject.enaryimidamides
dc.subject.enTherapeutic
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