RESUMO
Spiro derivatives of oxindole and isoxazole-5-one were synthesized by using Michael addition reaction, highlighting the regioselective approach towards the synthesis of Michael diadduct followed by condensation of Michael diadduct. The spiro compound 4 showed antitubercular activity against Mycobacterium tuberculosis H37Rv whereas spiro compound 9 possesses pronounced anticancer and antibacterial profile.
Assuntos
Androstenóis/síntese química , Antibacterianos/síntese química , Antineoplásicos/síntese química , Antituberculosos/síntese química , Compostos de Espiro/síntese química , Alquilação , Animais , Antibacterianos/farmacologia , Antibacterianos/toxicidade , Antineoplásicos/farmacologia , Antituberculosos/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Desenho de Fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Indóis/síntese química , Camundongos , Testes de Sensibilidade Microbiana , Compostos de Espiro/farmacologia , Compostos de Espiro/toxicidade , Células Tumorais CultivadasRESUMO
Administration of 70% methanolic extract of Punicagranatum fruit rind (250 mg/kg and 500 mg/kg) shows a percentage of inhibition in 22.37, 74.21 and 21.95, 63.41 in aspirin- and ethanol-induced gastric ulceration, respectively. In treated groups of animals, the in vivo antioxidant levels such as superoxide dismutase (SOD), catalase, glutathione (GSH) and glutathione peroxidase (GPx) levels were increased and found more or less equal to the normal values. The tissue lipid peroxidation level was found to be decreasing in treated groups of animals as compared to the control group. The histopathological examination of the stomach of the ulcerated animals shows severe erosion of gastric mucosa, sub-mucosal edema and neutrophil infiltration. All of these symptoms were found to be normal in treated groups. In general, the results of the present investigation revealed the gastroprotective activity of the extract through antioxidant mechanism.
Assuntos
Antiulcerosos/uso terapêutico , Lythraceae , Fitoterapia , Úlcera Gástrica/tratamento farmacológico , Animais , Antiulcerosos/química , Antioxidantes/química , Antioxidantes/metabolismo , Antioxidantes/uso terapêutico , Aspirina , Etanol , Frutas/química , Mucosa Gástrica/efeitos dos fármacos , Mucosa Gástrica/metabolismo , Mucosa Gástrica/patologia , Peroxidação de Lipídeos , Masculino , Metanol , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Ranitidina/uso terapêutico , Ratos , Ratos Wistar , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/patologiaRESUMO
Antioxidant, antitumor and anticarcinogenic activity of gossypin (3,5,8,3',4'-pentahydroxy-7-O glucosyl flavone) was carried out. The compound needed for 50% inhibition of superoxide, hydroxyl and nitric oxide radicals was 3 microg/ml, 41 microg/ml and 12 microg/ml, respectively. Gossypin also impart 50% inhibition at concentrations 37 microg/ml and 43 microg/ml, respectively for in vitro lipid peroxidation. The compound shows IC50 of 30 microM, 42.5 microM and 45.1 microM concentrations in L 929, HT 29 and K 562 cell lines in 72 hrs MTT assay. The compound shows a zone of inhibition of 8 mm in topo I and topo II inhibition assay in Saccharomyces ceriviseae mutant cultures. It reduces the tumor burden in solid tumor harboring animals (p < 0.001) and effectively inhibits the formation of new blood vessels on tumor mass. 20 mg/kg b.wt of gossypin increase the life span of ascites tumor harboring animals (100%) and (164.7%) respectively by oral and intraperitoneal administration of the drug. Gossypin reduced the incidence of papilloma formation and papilloma/mouse in DMBA/ croton oil induced skin papilloma.
