Novel curcumin analogue hybrids: Synthesis and anticancer activity
| Autor: | Jing Bo Shi, Xiaobin Wang, Wen Jian Tang, Yang Wang, Xin Hua Liu, Jie Quan Wang |
|---|---|
| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
Thioredoxin Reductase 1 Curcumin Antineoplastic Agents Apoptosis Mitochondrion 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Western blot Stomach Neoplasms Cell Line Tumor Neoplasms Drug Discovery medicine Humans ASK1 Cell Proliferation Membrane Potential Mitochondrial Pharmacology medicine.diagnostic_test Chemistry Cell Cycle Organic Chemistry General Medicine Cell cycle Mitochondria 030104 developmental biology Biochemistry 030220 oncology & carcinogenesis Cancer cell Reactive Oxygen Species Function (biology) Signal Transduction |
| Zdroj: | European Journal of Medicinal Chemistry. 156:493-509 |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/j.ejmech.2018.07.013 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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