RESUMO
Dihydroquercetin effects on the tone of isolated segments of the portal vein of rats were studied. Dihydroquercetin did not modify the basal venous tone, but reduced the amplitude of contractions induced by KCl and norepinephrine hydrotartrate.
Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Veia Porta/efeitos dos fármacos , Quercetina/análogos & derivados , Vasoconstrição/efeitos dos fármacos , Animais , Técnicas In Vitro , Masculino , Contração Muscular/efeitos dos fármacos , Músculo Liso Vascular/efeitos dos fármacos , Músculo Liso Vascular/fisiologia , Norepinefrina , Veia Porta/fisiologia , Cloreto de Potássio , Quercetina/farmacologia , Ratos , Ratos WistarRESUMO
The clinical trials on 31 patients with arteriosclerosis and I-II stage discirculatory encephalopathy to assess an ability of Ascovertin to limit hemorheology abnormalities were carried out. In patients with discirculatory encephalopathy was a distinct increase in blood viscosity which was induced by disturbances of cell rheological factors: increase in aggregation of erythrocytes and decrease in their deformability were observed in comparison with indices in the group of healthy volunteers. No difference in plasma viscosity and fibrinogen was found. The treatment with Ascovertin in patients with discirculatory encephalopathy improved their attention, memory, mental performance, normalized sleep, releaved headache, decreased fatiquebility, led to the decrease in blood viscosity values, the reduction of pathological erythrocyte hyper aggregation and the improvement of erythrocyte deformability. We partly connect this clinical effect and hemorheology activity of Ascovertin with its antioxidant property--there was found impressive lipid peroxidation suppression. No significant changes in hemorheological and lipid peroxidation indices were observed in patients without Ascovertin.
Assuntos
Antioxidantes/uso terapêutico , Hemorreologia , Arteriosclerose Intracraniana/tratamento farmacológico , Viscosidade Sanguínea , Artérias Cerebrais/patologia , Agregação Eritrocítica/efeitos dos fármacos , Agregação Eritrocítica/fisiologia , Deformação Eritrocítica/efeitos dos fármacos , Fibrinogênio/metabolismo , Humanos , Arteriosclerose Intracraniana/sangue , Valores de Referência , EscleroseRESUMO
Peroral administration of 70 mg/kg ascovertin and 150 mg/kg Leuzea extract to rats with cerebral ischemia for 5 days prevented destructive changes and decrease in the density of synapses in the cerebral cortex. These preparations activated compensatory and reparative mechanisms underlying plasticity of the synaptic pool, which was realized through hypertrophy and destruction of synaptic contacts. Ascovertin possessed more pronounced cerebroprotective activity than Leuzea extract.
Assuntos
Ácido Ascórbico/farmacologia , Encéfalo/patologia , Isquemia , Extratos Vegetais/farmacologia , Quercetina/análogos & derivados , Quercetina/farmacologia , Sinapses/patologia , Animais , Ácido Ascórbico/metabolismo , Encéfalo/efeitos dos fármacos , Córtex Cerebral/efeitos dos fármacos , Córtex Cerebral/metabolismo , Combinação de Medicamentos , Feminino , Hipertrofia , Isquemia/metabolismo , Masculino , Ratos , Ratos Wistar , Sinapses/efeitos dos fármacosRESUMO
1. The major metabolites of ethacizin (ethyl 10-[3-diethylaminopropionyl]phenothiazine-2-carbamate) have been isolated from human urine by h.p.l.c. and identified by determination of u.v., i.r., n.m.r. and mass spectra and comparison with spectra of synthetic standard compounds. 2. The pathways of metabolism of ethacizin include N-de-ethylation, sulphoxidation, N-10 amide hydrolysis, aromatic hydroxylation and conjugation.
