Nitric oxide inhibitory activity of hydrogenated synthetic analogues of furanonaphthoquinones isolated from Tabebuia spp

Objective: to describe the synthesis of analogues of furanonaphthoquinones isolated from Tabebuia genus and their inhibitory effect on nitric oxide production. Methods: a series of six derivatives were prepared through cycloaddition reactions and the products characterized by spectroscopy methods. The biological activity was evaluated measuring their effect on the pro-inflammatory mediator production in macrophages RAW 264.7 induced with lipopolysaccharides. To prevent compounds from interfering with cellular viability, their cytotoxic effect was determined using methyl tetrazolium assay. Additionally, scavenging effect was in vitro measured. Results: FNQ1, FNQ2, and FNQ5 derivatives showed potent concentration-depending inhibitory effect on nitric oxide production, with an IC50 value lower than 2 µM concentration at which they did not have toxic or scavenging effects. FNQ5 was the most active and selective derivative. Conclusions: this is the first paper concerning the anti-inflammatory potential of tested synthetic compounds. Our results indicated that FNQ5 might be considered as useful potential anti-inflammatory molecule to treat inflammatory diseases related with nitric oxide overproduction(AU)

Objetivo: describir la síntesis de análogos de furanonaftoquinonas aisladas del género Tabebuia y su efecto inhibidor en la producción de óxido nítrico. Métodos: se obtuvo una serie de seis derivados a través de reacciones de cicloadición y se caracterizaron los productos por métodos espectroscópicos. Se evaluó la actividad biológica por su efecto en la producción del mediador proinflamatorio en macrófagos RAW 264.7 activados con lipopolisacárido. Para asegurar que los compuestos no interfirieran con la viabilidad celular, se evaluó su efecto citotóxico empleando el ensayo de metiltetrazolio. Adicionalmente, se evaluó el efecto captador del radical in vitro. Resultados: los derivados FNQ1, FNQ2 y FNQ5 demostraron potente efecto inhibitorio en la producción de óxido nítrico de manera concentración-dependiente, con un valor de CI50 menor que 2 µM, concentración a la que no ejercieron efectos tóxicos o captadores de radicales. FNQ5 resultó el compuesto más activo y selectivo. Conclusiones: este trabajo es el primero que evalúa el potencial antinflamatorio de los compuestos sintetizados. Los resultados indican que FNQ5 puede ser considerada como una molécula de uso potencial para el tratamiento de enfermedades inflamatorias que cursen con sobreproducción de óxido nítrico(AU)

Genus Lantana: chemical aspects and biological activities

Species of the genus Lantana, belonging to the family Verbenaceae, is among the various species studied scientifically. These species are mainly native to the tropical and subtropical regions of the Americas. Currently, they are present in various countries, where they are often grown as ornamental plants. For decades, species of Lantana have been of great interest for phytochemical, biological and pharmacological studies, which have been recently intensified. The components isolated from different species of Lantana cited in the literature constitute the focus of this review. Information ethnopharmacology of Lantana, as well as the activities of their different phytochemicals are discussed. In this review, it was observed that the genus Lantana has been widely studied in relation to its phytochemical components and terpenoids, flavonoids and phenylpropanoids are the more common secondary metabolites in Lantana. All these aspects, considered in this review, allow an evaluation of the ethnopharmacological potential of Lantana for the utilization of the large biomass of these plants.