RESUMO
A series of 5,6,7-trimethoxyflavone-6-chlorotacrine hybrids were designed, synthesized and evaluated as multifunctional agents for the treatment of Alzheimer's disease (AD). The results showed that the target compounds exhibited good acetylcholinesterase (AChE) inhibitory potencies, high selectivity toward AChE over butyrylcholinesterase (BuChE), potential antioxidant activities and significant inhibitory potencies of self-induced beta-amyloid peptide (Aß) aggregation. In particular, compound 14c had the strongest AChE inhibitory activity with IC50 value of 12.8 nM, potent inhibition of self-induced Aß1-42 aggregation with inhibition ratio of 33.8% at 25 µM. Moreover, compound 14c acted as an antioxidant, as well as a neuroprotectant. Furthermore, 14c could cross the blood-brain barrier (BBB) in vitro. The results showed that compound 14c might be a potential multifunctional candidate for the treatment of AD.
Assuntos
Doença de Alzheimer/tratamento farmacológico , Antioxidantes/farmacologia , Inibidores da Colinesterase/farmacologia , Desenho de Fármacos , Flavonas/farmacologia , Tacrina/análogos & derivados , Acetilcolinesterase/metabolismo , Animais , Antioxidantes/síntese química , Antioxidantes/química , Butirilcolinesterase/metabolismo , Sobrevivência Celular/efeitos dos fármacos , Inibidores da Colinesterase/síntese química , Inibidores da Colinesterase/química , Relação Dose-Resposta a Droga , Electrophorus , Equidae , Flavonas/síntese química , Flavonas/química , Estrutura Molecular , Células PC12 , Ratos , Relação Estrutura-Atividade , Tacrina/síntese química , Tacrina/química , Tacrina/farmacologiaRESUMO
BACKGROUND AND METHODS: Commercial pure titanium with nanotopography was prepared via a high-energy shot-peening (HESP) technique. The surface characteristics were evaluated, and the preliminary cell responses to the nanotopographical surface were investigated. RESULTS: The nanotopographical surface layer on titanium was successfully processed by HESP. The average nanoscale grains were approximately 60 nm in diameter and they were nonhomogeneously distributed on the surface. MG-63 cells with an osteogenic phenotype were well adhered and well spread on the nanostructured surface. Compared to the original polished control, the nanotopographical surface highly improved the adhesion, viability, and differentiation of MG-63 cells. CONCLUSION: Titanium with nanotopography achieved by HESP has good cytocompatibility and shows promise for dental implant applications.
Assuntos
Nanoestruturas/química , Osteoblastos/efeitos dos fármacos , Titânio/química , Materiais Biocompatíveis/química , Materiais Biocompatíveis/toxicidade , Linhagem Celular Tumoral , Fenômenos Fisiológicos Celulares/efeitos dos fármacos , Humanos , Nanoestruturas/toxicidade , Nanotecnologia , Propriedades de Superfície , Titânio/toxicidadeRESUMO
PURPOSE: To investigate the adequate luting cements for zirconia ceramics to dentin. METHODS: Blocks of sintered zirconia ceramics were randomly divided into 4 groups with 8 slices in each. After saliva immersion,airborne-particle abraded ceramic specimens were cleaned with phosphoric acid gel(containing 35% phosphoric acid) and then bonded to dentin with these four kinds of luting cements. After preserved in 37 degrees centigrade distilled water for 24 hours, the shear bonding strength of these specimens was tested and the data was analyzed with SPSS12.0 software package. RESULTS: The Multilink Automix could attain the highest shear bonding strength and the 3M RelyXTM Unicem AplicapTM could attain higher shear bonding strength, which were both significantly higher than in the Tokuso Ionomer and Shofu Polycarboxylate Cement groups(P<0.05). CONCLUSION: Total etching resin luting cement is an ideal option to the bonding of zirconia ceramics and can provide a strong bonding.
