The efficacy of 2-nitrovinylfuran derivatives against Leishmania in vitro and in vivo
| Autor: | Juan Francisco Infante-Bourzac, Niurka Mollineda Diogo, Oliver Pérez-Martín, Yamilé López-Hernández, Ana M. Montalvo-Álvarez, Nilo Castañedo-Cancio, Miguel Ángel Cabrera-Pérez, Lianet Monzote-Fidalgo, Alfredo Meneses-Marcel, José Antonio Escario Garcia-Trevijano, Sergio Sifontes-Rodríguez |
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| Jazyk: | angličtina |
| Rok vydání: | 2015 |
| Předmět: |
Microbiology (medical)
lcsh:Arctic medicine. Tropical medicine Time Factors Vinyl Compounds lcsh:RC955-962 lcsh:QR1-502 UC245 Antiprotozoal Agents Leishmaniasis Cutaneous Pharmacology In Vitro Techniques lcsh:Microbiology KB Cells Inhibitory Concentration 50 Cutaneous leishmaniasis In vivo Amphotericin B medicine Animals Humans Furans nitrovinylfuran Cell Proliferation Leishmania Clinical Trials as Topic Mice Inbred BALB C biology Neglected Diseases Leishmaniasis Articles medicine.disease biology.organism_classification Antimicrobial Leishmania braziliensis promastigote Disease Models Animal furvina Immunology Female Leishmania infantum BALB/c medicine.drug |
| Zdroj: | Memórias do Instituto Oswaldo Cruz Memórias do Instituto Oswaldo Cruz., Vol 110, Iss 2, Pp 166-173 (2015) Memórias do Instituto Oswaldo Cruz, Volume: 110, Issue: 2, Pages: 166-173, Published: 24 MAR 2015 |
| ISSN: | 1678-8060 0074-0276 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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