Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 21, Issue 17, Pages 5012-5020Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.06.053
Keywords
Apoptosis; Cell cycle; Colon cancer; Curcumin analogues; EGFR
Funding
- Natural Science Foundation of China [21171154, 91129706]
- Special Fund for Marine Scientific Research in the Public Interest [01005024]
- Program for Science and Technology Development of Shandong Province [2012GSF11912]
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Epidermal growth factor receptor (EGFR) is an effective molecular target of anti-cancer therapies. Curcumin inhibits cancer cell growth in vitro by suppressing gene expression of EGFR and reduces tumor growth in various animal models. To overcome instable and insoluble properties of curcumin as therapeutics, we designed and synthesized six novel pyrimidine-substituted curcumin analogues with or without a hydroxyl group originally present in curcumin. The cell viability tests indicated that IC50 of the analogues containing hydroxyl group were 3 to 8-fold lower than those of the analogues without hydroxyl group in two colon cancer cell lines tested. Western blot analysis indicates the analogues containing hydroxyl group inhibited expression and tyrosine phosphorylation of EGFR. Further protein analyses showed that the analogues had anti-cellular proliferation, pro-apoptosis, and cell cycle arrest properties associated with suppressed EGFR expression. These results indicate that the hydroxyl groups in curcumin and the analogues were critical for observed biological activities. (C) 2013 The Authors. Published by Elsevier Ltd. All rights reserved.
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