RESUMO
The effects of an ethanol extract of the aerial parts of Ruta chalepensis on the central nervous system (CNS) and LD(50) determination were studied in mice. A crude extract was given systemically and its effects were tested on pentylenetetrazole (PTZ)-induced seizures, sodium pentobarbital-induced hypnosis, exploratory activity, anxiety and nociception. Results from the experimental models tested showed: (1) a delay in the onset of seizures and a dose-dependent suppression in the tonic phase and mortality induced by PTZ; (2) a prolongation of the time of sodium pentobarbital-induced hypnosis; (3) a significant attenuation in the anxiety-response and (4) a reduction in the licking time and shaking behavior in the formalin-induced nociception test. The sedative-hypnotic potentiation, anxiolytic, anticonvulsant and antinociceptive effects suggest that Ruta chalepensis induces a depressant activity on the CNS.
Assuntos
Ansiolíticos/farmacologia , Anticonvulsivantes/farmacologia , Depressores do Sistema Nervoso Central/farmacologia , Hipnóticos e Sedativos/farmacologia , Extratos Vegetais/farmacologia , Ruta/química , Animais , Ansiedade/induzido quimicamente , Ansiedade/tratamento farmacológico , Etanol/farmacologia , Comportamento Exploratório/efeitos dos fármacos , Masculino , Camundongos , Medição da Dor , Pentobarbital/toxicidade , Pentilenotetrazol/toxicidade , Fitoterapia , Convulsões/induzido quimicamente , Convulsões/tratamento farmacológicoRESUMO
The activity-guided fractionation of the ethanol extract of leaves of Annona diversifolia Saff., led to the isolation of palmitone (16-hentriacontanone) as the only anticonvulsant active compound. This aliphatic ketone was highly effective to diminish pentylenetetrazole (PTZ)-induced clonic-tonic seizures and toxicity. Also, it produced a prolongation of the latency for onset of seizures and a reduction of the death rate produced by 4-aminopyridine (4-AP) and bicuculline (BIC). However, it was inactive to inhibit the kainic acid (KA)- and strychnine (STC)-induced seizures. Palmitone did not produce motor incoordination and loss of righting reflex which are used as signs of neurological impairment. Palmitone (ED50 = 1.85 mg/kg) proved to be a more potent antiepileptic drug against the PTZ-induced seizures than etosuximide (ED50 = 59.6 mg/kg), sodium valproate (ED50 = 63 mg/kg), and carbamazepine (ED50 > 300 mg/kg) and it was only four-fold less potent than diazepam (ED50 = 0.48 mg/kg). The pharmacological profile of palmitone suggests that this compound could be acting on the GABAergic inhibitory system.
