Synthesis and Biological Evaluation of Curcumin Derivatives withWater-Soluble Groups as Potential Antitumor Agents: An in Vitro Investigation Using Tumor Cell Lines.
In: Molecules, Jg. 20 (2015-12-01), Heft 12, S. 21501-21514
Online
academicJournal
Zugriff:
Three series of curcumin derivatives including phosphorylated, etherified, and esterified products of curcumin were synthesized, and their anti-tumor activities were assessed against human breast cancerMCF-7, hepatocellular carcinoma Hep-G2, and human cervical carcinoma HeLa cells. Compared with curcumin, compounds 3, 8, and 9 exhibited stronger antitumor cell line growth activities against HeLa cells. Compound 12 also showed higher antitumor cell line growth activities on MCF-7 cells than curcumin. Among them, 4-((1E,6E)-7-(4-Hydroxy-3-methoxyphenyl)-3,5-dioxohepta-1,6-dienyl)-2-methoxyphenyl dihydrogen phosphate(3) showed the strongest activity with an half maximal inhibitory concentration (IC 50 ) of 6.78 µMagainst HeLa cells compared with curcumin with an IC 50 of 17.67 µM. Stabilities of representatives of the three series were tested in rabbit plasma in vitro, and compounds 3 and 4 slowly released curcumin in plasma. The effect of compound 3 onHeLa cell apoptosis was determined by examining morphological changes by DAPI (4',6-diamidino-2-phenylindole) staining as well as Annexin V-FITC/ Propidium Iodide (PI) double staining and flow cytometry. The results showed that 3 induced cellular apoptosis in a dose-dependent manner. Together our findings show that 3 merits further investigation as a new potential antitumor drug candidate. [ABSTRACT FROM AUTHOR]
Copyright of Molecules is the property of MDPI and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)
Titel: |
Synthesis and Biological Evaluation of Curcumin Derivatives withWater-Soluble Groups as Potential Antitumor Agents: An in Vitro Investigation Using Tumor Cell Lines.
|
---|---|
Autor/in / Beteiligte Person: | Ding, Luyang ; Ma, Shuli ; Lou, Hongxiang ; Sun, Longru ; Ji, Mei |
Link: | |
Zeitschrift: | Molecules, Jg. 20 (2015-12-01), Heft 12, S. 21501-21514 |
Veröffentlichung: | 2015 |
Medientyp: | academicJournal |
ISSN: | 1420-3049 (print) |
DOI: | 10.3390/molecules201219772 |
Schlagwort: |
|
Sonstiges: |
|