RESUMO
Some methoxy-, hydroxyl-, pyridyl-, or fluoro-substituted 3,5-bis(arylidene)-4-piperidones (BAPs) could reduce inflammation and promote hepatoma cell apoptosis by inhibiting activation of NF-κB, especially after introduction of trifluoromethyl. Herein, a series of trifluoromethyl-substituted BAPs (4-30) were synthesised and the biological activities were evaluated. We successfully found the most potential 16, which contains three trifluoromethyl substituents and exhibits the best anti-tumour and anti-inflammatory activities. Preliminary mechanism research revealed that 16 could promote HepG2 cell apoptosis in a dose-dependent manner by down-regulating the expression of Bcl-2 and up-regulating the expression of Bax, C-caspase-3. Meanwhile, 16 inhibited activation of NF-κB by directly inhibiting the phosphorylation of p65 and IκBα induced by LPS, together with indirectly inhibiting MAPK pathway, thereby exhibiting both anti-hepatoma and anti-inflammatory activities. Molecular docking confirmed that 16 could bind to the active sites of Bcl-2, p65, and p38 reasonably. The above results suggested that 16 has enormous potential to be developed as a multifunctional agent for the clinical treatment of liver cancers and inflammatory diseases.
Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Antineoplásicos/farmacologia , Carcinoma Hepatocelular/tratamento farmacológico , Neoplasias Hepáticas/tratamento farmacológico , NF-kappa B/antagonistas & inibidores , Piperidonas/farmacologia , Anti-Inflamatórios não Esteroides/síntese química , Anti-Inflamatórios não Esteroides/química , Antineoplásicos/síntese química , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Carcinoma Hepatocelular/metabolismo , Carcinoma Hepatocelular/patologia , Linhagem Celular , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Neoplasias Hepáticas/metabolismo , Neoplasias Hepáticas/patologia , Simulação de Acoplamento Molecular , Estrutura Molecular , NF-kappa B/metabolismo , Fosforilação/efeitos dos fármacos , Piperidonas/síntese química , Piperidonas/química , Relação Estrutura-AtividadeRESUMO
Photocatalytic degradation of pollutants is considered a promising approach for wastewater treatment, but is hampered by low efficiency and limited understanding of degradation pathways. A novel oxygen-doped porous g-C3N4/oxygen vacancies-rich BiOCl (OCN/OVBOC) heterostructure was prepared for photocatalytic degradation of bisphenol A (BPA). The synergistic defect and doping engineering favor the formation of strong bonded interface for S-scheme mechanism. Among them, 0.3 OCN/OVBOC showed the most excellent degradation rate, which was 8 times and 4 times higher than that of pure g-C3N4 and BiOCl, respectively. This excellent performance is mainly attributed to the significantly enhanced charge separation via strong bonded interface and redox capability of the S-scheme heterojunction structure, by tuning the coordination excitation and electron localization of the catalyst via O doping and vacancies. This work provides important insights into the role of synergistic defect and doping engineering in facilitating the formation of strong bonded S-scheme heterojunction and ultimately sheds new light on the design of efficient photocatalysts.
Assuntos
Elétrons , Poluentes Ambientais , Oxigênio , PorosidadeRESUMO
Aerator is an indispensable tool in aquaculture, and China is one of the largest aquaculture countries in the world. So, the intelligent control of the aerator is of great significance to energy conservation and environmental protection and the prevention of the deterioration of dissolved oxygen. There is no intelligent aerator related work in practice and research. In this paper, we mainly study the intelligent aerator control based on deep learning, and propose a dissolved oxygen prediction algorithm with long and short term memory network, referred as DopLSTM. The prediction results are used to the intelligent control design of the aerator. As a result, it is proved that the intelligent control of the aerator can effectively reduce the power consumption and prevent the deterioration of dissolved oxygen.