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European journal of medicinal chemistry v.143, 2018년, pp.1768 - 1778   SCI SCIE
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DMXAA-pyranoxanthone hybrids enhance inhibition activities against human cancer cells with multi-target functions

Liu, Jie (Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China ) ; Zhou, Fan (Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China ) ; Zhang, Lei (Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China ) ; Wang, Huailing (School of Food Sciences and Engineering, South China University of Technology, Guangzhou 510641, PR China ) ; Zhang, Jianrun (Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China ) ; Zhang, Cao (Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China ) ; Jiang, Zhenlei (Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China ) ; Li, Yanbing (Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan Universit ) ; Liu, Zhijun ; Chen, Heru ;
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    Abstract Four 5,6-dimethylxanthone-4-acetic acid ( D ) and pyranoxanthone ( P ) hybrids ( D-P-n ) were design-synthesized based on multi-target-addressed strategy. D-P-4 was confirmed as the most active agent against HepG-2 cell line growth with an IC 50 of 0.216 ± 0.031 μM. Apoptosis analysis indicated different contributions of early/late apoptosis/necrosis to cell death for both monomers, the combination ( D + P in 1:1 mol ratio) and D-P-4 . They all arrested more cells on S phase. Western Blot implied that D-P-4 regulated p53/MDM2 to a better healthy state. Moreover, it improved Bax/Bcl-2 signaling pathway to increase cancer cell apoptosis. In all cases studied, D-P-4 showed the best activity and synergistic effect. All the evidences support that D-P-4 is a better anti-cancer therapy with multi-target functions. Highlights D-P-4 hybrid increased the activity against the growth of HepG-2 cancer cells by 460 times compared to DMXAA. D-P-4 regulated p53/MDM2 to a better healthy state than both monomers and the combination. D-P-4 showed better activity in regulating Bax/Bcl-2 to increase HepG-2 cell apoptosis. D-P-4 arrested more cells on S phase compared with any one of the two monomers or the combination. Graphical abstract [DISPLAY OMISSION]


  • 주제어

    Xanthones .   Anti-cancer .   Multi-targets-addressed ligand .   Synergistic effect .   p53/MDM2 .   Bax/Bcl-2.  

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