RESUMO
Gastroprotective mechanism of peganine hydrochloride isolated from Peganum harmala seeds was investigated. Peganine hydrochloride was evaluated against cold restraint (CRU), aspirin (AS), alcohol (AL) and pyloric ligation (PL) induced gastric ulcer models in rats. Potential anti-ulcer activity of peganine was observed against CRU (50.0%), AS (58.5%), AL (89.41%) and PL (62.50%) induced ulcer models. The reference drug omeprazole (10mg/kg, p.o.) showed 77.45% protection against CRU, 49.97% against AS and 69.42% against PL model. Sucralfate, another reference drug (500mg/kg, p.o.) showed 62.50% protection in AL induced ulcer model. Peganine significantly reduced free acidity (33.38%), total acidity (38.09%) and upregulated mucin secretion by 67.91%, respectively. Further, peagnine significantly inhibited H(+) K(+)-ATPase activity in vitro with IC50 of 73.47µg/ml as compared to the IC50 value of omeprazole (30.24µg/ml) confirming its anti-secretory activity.
Assuntos
Alcaloides/uso terapêutico , Antiulcerosos/uso terapêutico , Peganum/química , Extratos Vegetais/uso terapêutico , Quinazolinas/uso terapêutico , Úlcera Gástrica/tratamento farmacológico , Álcoois/farmacologia , Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Animais , Antiulcerosos/isolamento & purificação , Antiulcerosos/farmacologia , Antioxidantes/análise , Antioxidantes/metabolismo , Aspirina/farmacologia , Temperatura Baixa , Modelos Animais de Doenças , ATPase Trocadora de Hidrogênio-Potássio/efeitos dos fármacos , Masculino , Estrutura Molecular , Omeprazol/farmacologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Piloro , Quinazolinas/isolamento & purificação , Quinazolinas/farmacologia , Ratos , Ratos Sprague-Dawley , Sementes/química , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/prevenção & controle , Sucralfato/farmacologia , Sucralfato/uso terapêuticoRESUMO
A new chemical access has been developed to synthesize biaryls from substituted acetophenones, phenylacetones, dihydrochalcone, and 2-acetylnaphthalene in reasonably good yields at room temperature via a domino reaction sequence of AlCl(3) catalyzed cyclization, dehydration, and then oxidation.
