Synthesis and biological analysis of a new curcumin analogue for enhanced anti-tumor activity in HepG 2 cells
Synthesis and biological analysis of a new curcumin analogue for enhanced anti-tumor activity in HepG 2 cells
复制标题
增强 HepG 2 细胞抗肿瘤活性的新型姜黄素类似物的合成和生物学分析
DOI：
10.3892/or_00000781
复制
发表时间：
2010-05-01
期刊：
影响因子：
4.2
通讯作者：
Li, Xiaokun
中科院分区：
文献类型：
--
作者：
Xiao, Jian;Chu, Yanhui;Li, Xiaokun
The aim of the present study was to investigate the apoptosis of human hepatocellular carcinoma cell line HepG 2 induced by a new curcumin analogue, GL63. HepG 2 cells were treated with increasing closes of GL63 and curcumin for 48 h. The proliferation of cells was detected with MTT. The apoptosis were examined by flow cytometry. The caspase-3 activity was detected by Western blotting. ER calcium stores were assessed by the fluorescent calcium indicator fura-2/AM. The protein expression of ER stress pathway, GRP78, XBP-1, ATE-4 and CHOP were examined with Western blotting. Growth inhibitory effect was observed for treatment with GL63 in a dose-dependent manner and with more potential than curcumin. GL63 at 20 mu M induced significant apoptosis in HepG 2 cells. Furthermore. GL63 induced the ER stress response, up-regulation of CHOP, XBP-1, ATF-4 and GRP78 expression in a dose-dependent, while curcumin had no effect on ER stress. These results suggest that GL63 has more potent anti-tumor activity than curcumin, which is associated with activation of ER stress and induction of apoptosis in HepG 2 cells.
