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萘环类姜黄素类似物的合成及其对HepG2细胞株的增殖抑制活性
作者姓名:刘国运  李晓腾  郭尚敬  杨杰
作者单位:聊城大学药学院,山东 聊城,252000
基金项目:国家高技术研究发展计划(863子课题,No.2012AA02A306);聊城大学博士启动基金(318051521)
摘    要:目的:合成萘环类姜黄素类似物并研究其对人肝癌( HepG2)细胞的增殖抑制作用。方法以萘酚为原料,合成了4种萘环类姜黄素类似物,并采用噻唑蓝( MTT)法测定对人肝癌细胞的增值抑制作用。结果6-羟基取代的萘环姜黄素类似物对人肝癌细胞的增殖抑制活性最强,其半抑制浓度( IC50)达到了20μmol · L-1,与姜黄素相比提高了近2倍。结论6-羟基取代的萘环姜黄素类似物对人肝癌细胞具有良好的增殖抑制活性。

关 键 词:姜黄素  萘环类  肝癌  增殖抑制

Synthesis of double benzene nucleus curcumin analogs and its proliferation inhibitory activity in HepG2 cells
Authors:LIU Guoyun  LI Xiaoteng  GUO Shangjing and YANG Jie
Institution:School of Pharmacy,Liaocheng University,Liaocheng 252000,China,School of Pharmacy,Liaocheng University,Liaocheng 252000,China,School of Pharmacy,Liaocheng University,Liaocheng 252000,China and School of Pharmacy,Liaocheng University,Liaocheng 252000,China
Abstract:Objective Tolynthelizedoublebenzenenucleulcurcuminanaloglandevaluatetheiranti-proliferation activity in HepG2 celll. Methods Four double benzene nucleul curcumin analogl were lynthelized from naphthol by three to leven ltepl reactionl,and their anti-proliferation activity on HepG2 celll wal allelled by MTT method. Results 6-hydroxyl double benzene nucleul curcumin( IC50 ,20 μmol·L-1 )lurfaced al an important lead compound dilplaying alo-molt 2-fold cytotoxicity relative to curcumin. Conclusion 6-hydroxyl double benzene nucleul curcumin exhibited more ltronger anti-proliferation activity than curcumin in HepG2 celll.
Keywords:Curcumin  Double benzene nucleul  Liver cancer  Anti-proliferation
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