RESUMO
Concerning the role of antioxidant and anti-inflammatory agents for hepatic fibrosis patients, the current study deals with the development of novel chalcone derivatives 5a-i via efficient synthetic methodology in a two-step reaction involving Claisen-Schmidt condensation. The obtained target analogs were screened for in vitro antioxidant activity by various methods (H2 O2 , DPPH, ferrous reducing power, and nitric oxide), where they exhibit considerable radical scavenging activity. These compounds were also evaluated for inhibitory potency against NF-κB activation induced by LPS for the determination of their anti-inflammatory activity. The inhibition values indicate that the entire set of compounds efficiently inhibits the NF-κB activation provoked by LPS. Among the series, compound 5i was identified as the most potent inhibitor of NF-κB, with a relative NF-κB activity of 1.12 ± 0.53. It also inhibits various inflammatory mediators, such as TNF-α, IL-1ß, IL-6, and PGE2 .
Assuntos
Anti-Inflamatórios não Esteroides/química , Antioxidantes/química , Chalconas/química , NF-kappa B/antagonistas & inibidores , Animais , Anti-Inflamatórios não Esteroides/síntese química , Anti-Inflamatórios não Esteroides/farmacologia , Antioxidantes/síntese química , Antioxidantes/farmacologia , Linhagem Celular , Chalconas/síntese química , Chalconas/farmacologia , Dinoprostona/metabolismo , Sequestradores de Radicais Livres/síntese química , Sequestradores de Radicais Livres/química , Sequestradores de Radicais Livres/farmacologia , Interleucina-1beta/metabolismo , Interleucina-6/metabolismo , Lipopolissacarídeos/farmacologia , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , Simulação de Acoplamento Molecular , NF-kappa B/metabolismo , Estereoisomerismo , Relação Estrutura-Atividade , Fator de Necrose Tumoral alfa/metabolismoAssuntos
Coledocostomia/métodos , Neoplasias do Ducto Colédoco/complicações , Icterícia Obstrutiva/etiologia , Icterícia Obstrutiva/cirurgia , Idoso , Idoso de 80 Anos ou mais , Alanina Transaminase/sangue , Bilirrubina/sangue , Ducto Colédoco/cirurgia , Drenagem , Feminino , Seguimentos , Humanos , Icterícia Obstrutiva/sangue , Jejuno/cirurgia , Masculino , Pessoa de Meia-Idade , Neoplasias Pancreáticas/complicações , Taxa de Sobrevida , gama-Glutamiltransferase/sangueRESUMO
Three kinds of membranes were prepared from suspensions containing polyacrylonitrile, dimethyl sulfoxide, polyethylene glycol and different amount of Fe3O4 by the phase inversion process. The rejection rate and the flux of membrane were investigated in the filtration of pig blood solution. SEM also studied the morphologies of fouled membranes. The permeate flux and the rejection rate decline fast in the initial several minutes and then change slowly. The magnetized membrane has a higher flux and a relative flux than the corresponding non-magnetized membrane. And the magnetized membrane containing about 3 wt% Fe3O4 has a prominent anti-fouling performance with above 52% relative flux. The results indicate that the magnetized ferrosoferric oxide-polyacrylonitrile membranes are promising in the recovery of blood proteins in the slaughterhouse effluents. In addition, the hydraulic resistance model explained results and the fouling mechanism was also given.
