Synthesis and biological analysis of a new curcumin analogue for enhanced anti-tumor activity in HepG 2 cells

  • Authors:
    • Jian Xiao
    • Yanhui Chu
    • Keqiong Hu
    • Jin Wan
    • Yi Huang
    • Chengxi Jiang
    • Guang Liang
    • Xiaokun Li
  • View Affiliations

  • Published online on: May 1, 2010     https://doi.org/10.3892/or_00000781
  • Pages: 1435-1441
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Abstract

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 doses 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, ATF-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 µM 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.

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May 2010
Volume 23 Issue 5

Print ISSN: 1021-335X
Online ISSN:1791-2431

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Spandidos Publications style
Xiao J, Chu Y, Hu K, Wan J, Huang Y, Jiang C, Liang G and Li X: Synthesis and biological analysis of a new curcumin analogue for enhanced anti-tumor activity in HepG 2 cells . Oncol Rep 23: 1435-1441, 2010.
APA
Xiao, J., Chu, Y., Hu, K., Wan, J., Huang, Y., Jiang, C. ... Li, X. (2010). Synthesis and biological analysis of a new curcumin analogue for enhanced anti-tumor activity in HepG 2 cells . Oncology Reports, 23, 1435-1441. https://doi.org/10.3892/or_00000781
MLA
Xiao, J., Chu, Y., Hu, K., Wan, J., Huang, Y., Jiang, C., Liang, G., Li, X."Synthesis and biological analysis of a new curcumin analogue for enhanced anti-tumor activity in HepG 2 cells ". Oncology Reports 23.5 (2010): 1435-1441.
Chicago
Xiao, J., Chu, Y., Hu, K., Wan, J., Huang, Y., Jiang, C., Liang, G., Li, X."Synthesis and biological analysis of a new curcumin analogue for enhanced anti-tumor activity in HepG 2 cells ". Oncology Reports 23, no. 5 (2010): 1435-1441. https://doi.org/10.3892/or_00000781