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Memórias do Instituto Oswaldo Cruz
Fundação Oswaldo Cruz, Fiocruz
ISSN: 1678-8060
EISSN: 1678-8060
Vol. 110, No. 2, 2015, pp. 166-173
Bioline Code: oc15020
Full paper language: English
Document type: Research Article
Document available free of charge

Memórias do Instituto Oswaldo Cruz, Vol. 110, No. 2, 2015, pp. 166-173

 en The efficacy of 2-nitrovinylfuran derivatives against Leishmania check for this species in other resources in vitro and in vivo
Sifontes-Rodríguez, Sergio; Monzote-Fidalgo, Lianet; Castañedo-Cancio, Nilo; Montalvo-Álvarez, Ana Margarita; López-Hernández, Yamilé; Diogo, Niurka Mollineda; Infante-Bourzac, Juan Francisco; Pérez-Martín, Oliver; Meneses-Marcel, Alfredo; García-Trevijano, José Antonio Escario & Cabrera-Pérez, Miguel Ángel

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 check for this species in other resources , Leishmania infantum check for this species in other resources and Leishmania braziliensis check for this species in other resources 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® (a furvina-containing antifungal ointment) for the treatment of CL.

Keywords
nitrovinylfuran; furvina; UC245; Leishmania; BALB/c; promastigote

 
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