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没食子酸-芒果苷杂合分子的合成及抗肿瘤活性评价

Synthesis and anti-tumor activity evaluation of gallic acid-mangiferin hybrid molecule.

作者信息

Hu Xiang-yu, Deng Jia-gang, Wang Lin, Yuan Ye-fei

机构信息

Luzhou Medical College, Sichuan Luzhou 646000, China.

出版信息

Med Chem. 2013 Dec;9(8):1058-62. doi: 10.2174/1573406411309080007.

Abstract

To improve the anti-tumor effects of gallic acid and mangiferin, a gallic acid-mangiferin hybrid molecule (GAMA) was synthesized from gallic acid with mangiferin in the presence of ionic liquid ChC1(choline chloride)·2SnC12. Chemical and spectroscopic methods, such as (1)H and (13)C NMR spectroscopy, and HR-ESIMS were used for the structure identification of GA-MA. Using the cell counting kit-8 (CCK-8) assay, the in vitro anti-tumor effects were compared between GA-MA, gallic acid and mangiferin on human hepatoma HepG2, human nasopharyngeal carcinoma CNE, human lung cancer NCI-H460, human ovarian cancer SK-OV-3, and human cervical cancer Hela cells. The results showed that the half inhibitory concentration (IC50) of GA-MA on HepG2, CNE, NCI-H460, SK-OV-3, and Hela cells was significantly lower than that of gallic acid or mangiferin. This showed that GA-MA has a better in vitro anti-tumor effect than gallic acid and mangi-ferin.

摘要

为提高没食子酸和芒果苷的抗肿瘤效果,在离子液体氯化胆碱·二氯化锡(ChC1(氯化胆碱)·2SnC12)存在的条件下,由没食子酸与芒果苷合成了一种没食子酸 - 芒果苷杂合分子(GAMA)。采用化学和光谱方法,如(1)H 和(13)C 核磁共振光谱以及高分辨电喷雾电离质谱(HR - ESIMS)对 GA - MA 的结构进行鉴定。使用细胞计数试剂盒 - 8(CCK - 8)检测法,比较了 GA - MA、没食子酸和芒果苷对人肝癌 HepG2 细胞、人鼻咽癌 CNE 细胞、人肺癌 NCI - H460 细胞、人卵巢癌 SK - OV - 3 细胞和人宫颈癌 Hela 细胞的体外抗肿瘤效果。结果表明,GA - MA 对 HepG2、CNE、NCI - H460、SK - OV - 3 和 Hela 细胞的半数抑制浓度(IC50)显著低于没食子酸或芒果苷。这表明 GA - MA 比没食子酸和芒果苷具有更好的体外抗肿瘤效果。

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