RESUMEN
2-[(2,6-Dichlorobenzylidene)amino]-5,6-dihydro-4H-cyclopenta[b]thiophene-3-carbonitrile, 5TIO1, is a new 2-aminothiophene derivative with promising pharmacological activities. The aim of this study was to evaluate its antioxidant activity in different areas of mice central nervous system. Male Swiss adult mice were intraperitoneally treated with Tween 80 dissolved in 0.9% saline (control group) and 5TIO1 (0.1, 1, and 10 mg kg(-1)). Brain homogenates-hippocampus, striatum, frontal cortex, and cerebellum-were obtained after 24 h of observation. Superoxide dismutase and catalase activities, lipid peroxidation and nitrite content were measured using spectrophotometrical methods. To clarify the 5TIO1's mechanism on oxidative stress, western blot analysis of superoxide dismutase and catalase was also performed. 5TIO1 decreased lipid peroxidation and nitrite content in all brain areas and increased the antioxidant enzymatic activities, specially, in cerebellum. The data of Western blot analysis did not demonstrate evidence of the upregulation of these enzymes after the administration of this compound. Our findings strongly support that 5TIO1 can protect the brain against neuronal damages regularly observed during neuropathologies.
Asunto(s)
Antioxidantes/farmacología , Encéfalo/metabolismo , Estrés Oxidativo , Bases de Schiff/farmacología , Tiofenos/farmacología , Animales , Antioxidantes/química , Encéfalo/efectos de los fármacos , Catalasa/metabolismo , Cerebelo/enzimología , Cerebelo/metabolismo , Cuerpo Estriado/enzimología , Cuerpo Estriado/metabolismo , Lóbulo Frontal/enzimología , Lóbulo Frontal/metabolismo , Hipocampo/enzimología , Hipocampo/metabolismo , Inyecciones Intraperitoneales , Peroxidación de Lípido , Masculino , Ratones , Nitritos/metabolismo , Estrés Oxidativo/efectos de los fármacos , Bases de Schiff/química , Superóxido Dismutasa/metabolismo , Tiofenos/químicaRESUMEN
We examined the sedative, anxiolytic and antidepressant effects of essential oil (EO) of leaves from Citrus limon, which has been used as one of the most popular compounds in Brazilian traditional herbal medicine. The effects of EO were demonstrated by open-field, elevated-plus-maze, rota rod, pentobarbital-induced sleeping time, and forced swimming tests in mice. In the open-field test, EO at the doses of 50, 100 and 150 mg/kg, after oral administration, significantly decreased the number of crossings, grooming, and rearing. In the elevated-plus-maze (EPM) test, EO increased the time of permanence and the number of entrances in the open arms. On the contrary, the time of permanence and the number of entrances in the closed arms were decreased. In the rota rod test, EO did not alter motor coordination and, thus, was devoid of effects, as related to controls. In the pentobarbital-induced sleeping time test, EO at the same doses significantly increased the animals sleeping time duration. Since EO, at the doses of 50, 100 and 150 mg/kg, did not show a sedative effect in the open field test, these three doses were used in the forced swimming test, producing a decrease in the immobility time, similarly to that of imipramine (positive control). However, the antidepressant effects of EO were not altered by the previous administration of paroxetine. In addition, effects of EO in the forced swimming test were totally blocked by reserpine pretreatment. In conclusion, the present work evidenced sedative and anxiolytic effects of EO that might involve an action on benzodiazepine-type receptors, and also an antidepressant effect where noradrenergic and serotoninergic mechanisms will probably play a role.