期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 133, 期 -, 页码 50-61出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2017.03.068
关键词
Xanthones; Anti-cancer; Drug combination; Synergistic effect; p53-MDM2
资金
- Guangdong Provincial Project of Science and Technology [2015A030311012]
- Guangzhou Project of Science and Technology [201607010215]
- Fundamental Research Funds for the Central Universities [11615323]
34 Xanthones were synthesized by microwave assisted technique. Their in vitro inhibition activities against five cell lines growth were evaluated. The SAR has been thoroughly discussed. 7-Bromo-1,3-dihydroxy-9H-xanthen-9-one (3-1) was confirmed as the most active agent against MDA-MB-231 cell line growth with an IC50 of 0.46 +/- 0.03 mu M. Combination of 3-1 and 5,6-dimethylxanthone-4-acetic acid (DMXAA) showed the best synergistic effect. Apoptosis analysis indicated different contributions of early/late apoptosis and necrosis to cell death for both monomers and the combination. Western Blot implied that the combination regulated p53/MDM2 to a better healthy state. Furthermore, 3-1 and DMXAA arrested more cells on G2/M phase; while the combination arrested more cells on S phase. All the evidences support that the 3-1/DMXAA combination is a better anti-cancer therapy. (C) 2017 Elsevier Masson SAS. All rights reserved.
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