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Bioorg Chem. 2015 Jun;60:123-9. doi: 10.1016/j.bioorg.2015.04.010. Epub 2015 May 13.

13,14-Dihydroxy groups are critical for the anti-cancer effects of garcinol.

Author information

1
School of Pharmaceutical Engineering & Life Science, Changzhou University, Jiangsu 213164, PR China.
2
Beijing Institute of Dental Research, Beijing Stomatological Hospital, Capital Medical University, Beijing 100050, PR China.
3
Beijing Institute of Dental Research, Beijing Stomatological Hospital, Capital Medical University, Beijing 100050, PR China. Electronic address: xinyanzhangzh@126.com.
4
School of Pharmaceutical Engineering & Life Science, Changzhou University, Jiangsu 213164, PR China. Electronic address: xinchen@cczu.edu.cn.

Abstract

In the presence of K2CO3/Cs2CO3 (molar ratio 10:1), garcinol was subjected to methylation by reaction with iodomethane at room temperature to afford 13,14-dimethoxy garcinol. The methylated garcinol derivative was screened against oral cancer cell line SCC15 for cell proliferation and apoptosis. 13,14-Dimethoxy garcinol showed weaker inhibitory activity on SCC15 cell growth than garcinol, and had little effect on cell cycle and apoptosis of SCC15, whereas garcinol effectively induced cell cycle arrest and cell apoptosis. Meanwhile, the ELISA data showed that the inhibitory effect of garcinol on 5-Lox pathway was more potent than 13,14-dimethoxy garcinol (P<0.05). All these results have confirmed the important role of 13,14-dihydroxy groups for anti-cancer effects of garcinol.

KEYWORDS:

13,14-Dimethoxy garcinol; Anti-cancer; Cell apoptosis; Cell proliferation

PMID:
26000492
DOI:
10.1016/j.bioorg.2015.04.010
[Indexed for MEDLINE]

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