皂角刺中黄酮类成分及其抗肿瘤活性研究

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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28.53μmol/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。 Objective To study the flavonoids and their anti-tumor activities in Gleditsiae Spina. Methods The flavonoids were isolated and purified by silica gel column chromatography, Sephadex LH-20 column chromatography and semi-preparative HPLC. The structures of the compounds were identified by physicochemical properties and spectral data analysis. The compounds 7 ~ 16 on human breast cancer cells MCF-7 cytotoxicity. Results Sixteen flavonoids were isolated from the ethyl acetate fraction of the gleditsia sinensis and identified as tricin (1), licorice (2), 7,4’-dihydroxy-5,3’-dimethoxyflavone (4), 7,3 ’, 5’-trihydroxyflavone (5), 7,4’-dihydroxyflavone (6), dihydroabenzoin (8), (2S) -5,7,3 ’, 5’-Tetrahydroxyflavone (9), 7,3’, 5’-trihydroxy-5-methoxy Flavonol (10), quercetin (11), kaempferol (12), fisetin (13), leucorobinetinidin (14), thevetiaflavon (15) and isovitaminin The IC50 value was 28.53 μmol / L. Conclusion Compounds 1-6, 8-10, 14 and 15 were isolated from this genus for the first time. Compound 8 showed obvious cytotoxic activity to MCF-7 cells.
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