13,14-Dihydroxy groups are critical for the anti-cancer effects of garcinol
13,14-Dihydroxy groups are critical for the anti-cancer effects of garcinol
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13,14-二羟基对于藤黄醇的抗癌作用至关重要
DOI：
10.1016/j.bioorg.2015.04.010
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发表时间：
2015-06-01
影响因子：
5.1
通讯作者：
Chen, Xin
中科院分区：
文献类型：
--
作者：
Han, Chao-Ming;Zhou, Xin-Ying;Chen, Xin
在K2 CO 3/Cs2 CO 3（摩尔比10：1）存在下，Garcinol与碘甲烷在室温下发生甲基化反应，得到13，14-二甲氧基Garcinol。针对口腔癌细胞系SCC 15的细胞增殖和凋亡筛选甲基化Garcinol衍生物。13，14-二甲氧基Garcinol对SCC 15细胞生长的抑制作用弱于Garcinol，对SCC 15细胞周期和凋亡的影响较小，而Garcinol能有效地诱导细胞周期阻滞和细胞凋亡。同时，ELISA结果显示，Garcinol对5-Lox途径的抑制作用强于13，14-二甲氧基Garcinol（P < 0.05）。这些结果证实了13，14-二羟基在Garcinol抗癌作用中的重要作用。(C)2015 Elsevier Inc. All rights reserved.
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. (C) 2015 Elsevier Inc. All rights reserved.