%0 Journal Article
%T Potential multifunctional agents with anti-hepatoma and anti-inflammation properties by inhibiting NF-抗B activation
%A Chang-Ming Su
%A Cheng Yang
%A Chun-Hua Wang
%A Gui-Ge Hou
%A Hong-Qin Zhang
%A Mei Liu
%A Yun Hou
%J Journal of Enzyme Inhibition and Medicinal Chemistry
%D 2019
%R https://doi.org/10.1080/14756366.2019.1635124
%X Abstract Inhibition of NF-百B signalling has been demonstrated as a therapeutic option in treating inflammatory diseases and cancers. Herein, we synthesized novel dissymmetric 3,5-bis(arylidene)-4-piperidones (BAPs, 83每102) and characterized fully. MTT and ELISA assay were performed to screen the anti-hepatoma and anti-inflammation properties. 96 showed the most potential bioactivity. 96 could promote HepG2 apoptosis through up-regulating the expression of C-Caspase-3 and Bax, down-regulating the expression of Bcl-2, while markedly inhibit LPS or TNF-汐-induced activation of NF-百B through both inhibiting the phosphorylation of I百B汐 and p65, and preventing the p65 nuclear translocation to exhibit both anti-hepatoma and anti-inflammatory activities. Molecular docking verified that simulated 96 can effectively bond to the active site of Bcl-2 and NF-百B/p65 proteins. 96 inhibited xenografts growth by reducing the expression of TNF-汐 and Bcl-2 in the tumour tissue. This study suggested that 96 could be developed as a potential multifunctional agent for treatment of inflammatory diseases and cancers
%U https://www.tandfonline.com/doi/full/10.1080/14756366.2019.1635124