The efficacy of 2-nitrovinylfuran derivatives against Leishmania in vitro and in vivo
Mem. Inst. Oswaldo Cruz
; 110(2): 166-173, 04/2015. tab, graf
Artigo
em Inglês
| LILACS
| ID: lil-744479
Biblioteca responsável:
BR1.1
ABSTRACT
Despite recent advances in the treatment of some forms of leishmaniasis, the available drugs are still far from ideal due to inefficacy, parasite resistance, toxicity and cost. The wide-spectrum antimicrobial activity of 2-nitrovinylfuran compounds has been described, as has their activity against Trichomonas vaginalis and other protozoa. Thus, the aim of this study was to test the antileishmanial activities of six 2-nitrovinylfurans in vitro and in a murine model of leishmaniasis. Minimum parasiticide concentration (MPC) and 50% inhibitory concentration (IC50) values for these compounds against the promastigotes of Leishmania amazonensis, Leishmania infantum and Leishmania braziliensis were determined, as were the efficacies of two selected compounds in an experimental model of cutaneous leishmaniasis (CL) caused by L. amazonensis in BALB/c mice. All of the compounds were active against the promastigotes of the three Leishmania species tested. IC50 and MPC values were in the ranges of 0.8-4.7 µM and 1.7-32 µM, respectively. The compounds 2-bromo-5-(2-bromo-2-nitrovinyl)-furan (furvina) and 2-bromo-5-(2-methyl-2-nitrovinyl)-furan (UC245) also reduced lesion growth in vivo at a magnitude comparable to or higher than that achieved by amphotericin B treatment. The results demonstrate the potential of this class of compounds as antileishmanial agents and support the clinical testing of Dermofural(r) (a furvina-containing antifungal ointment) for the treatment of CL.
Texto completo:
Disponível
Coleções:
Bases de dados internacionais
Contexto em Saúde:
ODS3 - Saúde e Bem-Estar
/
ODS3 - Meta 3.3 Acabar com as doenças tropicais negligenciadas e combater as doenças transmissíveis
/
ODS3 - Meta 3.4 Reduzir as mortes prematuras devido doenças não transmissíveis
/
ODS3 - Meta 3.2 Reduzir as mortes de recém nascidos e crianças com menos de 5 anos
Problema de saúde:
Meta 3.2: Reduzir as mortes de recém nascidos e crianças com menos de 5 anos
/
Leishmaniose
/
Linfomas e Mieloma Múltiplo
/
Infecções
/
Doenças Não Transmissíveis
/
Nutrição
Base de dados:
LILACS
Assunto principal:
Doença de Hodgkin
/
Protocolos de Quimioterapia Combinada Antineoplásica
Tipo de estudo:
Estudo de etiologia
/
Guia de prática clínica
/
Estudo prognóstico
/
Fatores de risco
Limite:
Humanos
Idioma:
Inglês
Revista:
Mem. Inst. Oswaldo Cruz
Assunto da revista:
Medicina Tropical
/
Parasitologia
Ano de publicação:
2015
Tipo de documento:
Artigo
País de afiliação:
Cuba
Instituição/País de afiliação:
Universidad Central Martha Abreu de Las Villas/CU