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| Title | Novel curcumin analogue hybrids: Synthesis and anticancer activity |
| Publication Type | Journal Article |
| Year of Publication | 2018 |
| Authors | Wang, JQ, Wang, X, Wang, Y, Tang, WJ, Shi, JB, Liu, XH |
| Journal | Eur J Med Chem |
| Volume | 156 |
| Pagination | 493-509 |
| Date Published | Aug 5 |
| ISBN Number | 0223-5234 |
| Accession Number | 30025345 |
| Keywords | Anticancer activity, Antineoplastic Agents/chemical synthesis/*chemistry/*pharmacology, Apoptosis/drug effects, Cell Cycle/drug effects, Cell Line, Tumor, Cell Proliferation/drug effects, Curcumin hybrids, Curcumin/*analogs & derivatives/chemical synthesis/*pharmacology, Humans, Membrane Potential, Mitochondrial/drug effects, Mitochondria/drug effects/metabolism, Neoplasms/*drug therapy/metabolism, Reactive Oxygen Species/metabolism, Signal Transduction/drug effects, Stomach Neoplasms/drug therapy/metabolism, Synthesis, Thioredoxin Reductase 1/antagonists & inhibitors/metabolism, TrxR |
| Abstract | In this study, twenty curcumin analogue hybrids as potential anticancer agents through regulation protein of TrxR were designed and synthesized. Results of anticancer activity showed that 5,7-dimethoxy-3-(3-(2-((1E, 4E)-3-oxo-5-(pyridin-2-yl)penta-1,4-dien-1- yl)phenoxy)propoxy)-2-(3,4,5-trimethoxyphenyl)-4H-chromen-4-one (compound 7d) could induce gastric cancer cells apoptosis by arresting cell cycle, break mitochondria function and inhibit TrxR activity. Meanwhile, western blot revealed that this compound could dramatically up expression of Bax/Bcl-2 ratio and high expression of TrxR oxidation. These results preliminarily show that the important role of ROS mediated activation of ASK1/MAPK signaling pathways by this title compound. |