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| 藤黄酸衍生物的合成及其抗肿瘤活性 | |
| 作者单位： | ;1.云南民族大学民族药资源化学国家民委-教育部重点实验室;2.云南民族大学化学与环境学院 |
| 摘 要： | 以藤黄酸为原料分别与氨基酸反应,合成了一系列新型的藤黄酸衍生物,其结构经MS、~1H NMR、~(13)C NMR确证.采用磺酰罗丹明B(sulfurhodamine B)法测试目标化合物对人肺癌A549、人黑色素瘤A375、人肝癌HepG2和人胃癌BGC823细胞的体外抗肿瘤活性.结果显示,大多数化合物表现出较强的抗肿瘤活性.其中含非极性小基团侧链的氨基酸衍生物的活性普遍较高,化合物3和4的活性明显高于藤黄酸对照品;部分含极性氨基酸的衍生物的活性下降并且针对不同细胞株体现了不同的选择性. |
| 关 键 词： | 藤黄酸 衍生物 合成 抗肿瘤 |
Synthesis and antitumor activity of gambogic acid derivatives |
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| Affiliation: | ,Key Laboratory of Chemistry in Ethnic Medicinal Resources, State Ethnic Affairs Commission and Ministry of Education of China, Yunnan Minzu University,School of Chemistry and Environment, Yunnan Minzu University |
| Abstract: | A series of new derivatives of gambogic acid were synthesized. We synthesized gambogic acid with amino acids, and the structures were confirmed by MS, ~1H NMR, ~(13)C NMR. The in-vitro antitumor activity of the target compounds against human cancer cells A549(lung cancer), A375(melanoma), HepG2(hepatocellular carcinoma) and BGC823(gastric cancer) was determined by sulfurhodamine B assay. The results showed that most of the compounds showed a strong antitumor activity. The activity of amino acid derivatives containing a non-polar small-group side chain was generally good, and the activity of compound 3 and 4 was significantly higher than that of gambogic acid. The activity of derivatives containing polar amino acids decreased and showed a different selectivity to different cell lines. |
| Keywords: | gambogic acid derivative synthesis antitumor |
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