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[摘要]
目的 研究皂角刺Gleditsiae Spina中黄酮类化学成分及其抗肿瘤活性。方法 采用硅胶柱色谱、Sephadex LH-20柱色谱及半制备HPLC等方法对皂角刺中黄酮类化学成分进行分离纯化,并根据理化性质和波谱学数据分析鉴定化合物结构;采用SRB法测定化合物7~16对人乳腺癌细胞MCF-7的细胞毒活性。结果 从皂角刺醋酸乙酯部位中分离得到16个黄酮类化合物,分别鉴定为tricin(1)、甘草素(2)、7,4'-二羟基-5,3'-二甲氧基黄酮醇(3)、鹰嘴豆醇(4)、7,3',5'-三羟基二氢黄酮(5)、7,4'-二羟基黄酮醇(6)、双氢山柰素(7)、紫铆查耳酮(8)、(2S)-5,7,3',5'-四羟基二氢黄酮(9)、7,3',5'-三羟基-5-甲氧基黄酮醇(10)、槲皮素(11)、黄颜木素(12)、fisetin(13)、leucorobinetinidin(14)、thevetiaflavon(15)、异牡荆素(16);其中化合物8对MCF-7细胞的IC50值为28.53 μmol/L。结论 化合物1~6、8~10、14、15为首次从该属植物中分离得到,化合物8对MCF-7细胞具有明显细胞毒活性。
[Key word]
[Abstract]
Objective To investigate the flavonoids from Gleditsiae Spina (thorns of Gleditsia sinensis) and their antitumor activities. Methods The chemical constituents in the EtOAc fraction from Gleditsiae Spina were isolated and purified by the chromatography on silica gel, Sephadex LH-20 columns, and semi-preparative HPLC. Their structures were identified by various spectroscopic analyses, and the cytotoxicity of compounds 7—16 were evaluated in vitro against MCF-7 cell lines by SRB method. Results Sixteen compounds were isolated from the extracts of Gleditsiae Spina and identified as tricin (1), liquiritigenin (2), 7,4'-dihydroxy-5,3'-dimethoxyflavanonol (3), garbanzol (4), 7,3',5'-trihydroxyflavanone (5), 7,4'-dihydroxyflavonol (6), dihydrokaempferol (7), butein (8), (2S)-5,7,3',5'- tetrahydroxyflavanone (9), 7,3',5'-trihydroxy-5-methoxyflavanonol (10), quercetin (11), fustin (12), fisetin (13), leucorobinetinidin (14), thevetiaflavon (15), and isovitexin (16). Compound 8 showed the inhibitory effect against MCF-7 cells with IC50 value of 28.53 μmol/L. Conclusion Compounds 1—6, 8—10, 14 and 15 are isolated from the plants of Gleditsia L. for the first time, compound 8 shows the significant cytotoxic activity against MCF-7 cells.
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[基金项目]
山东省科学院科学技术发展计划项目(2014QN02);山东省科学院—枣庄产学研联合基金资助项目