皂角刺中3个香豆素类化合物及其细胞毒活性研究  

Investigation of three coumarin components in thorns of Gleditsia sinensis and their cytotoxic activity to tumor cells

作　　者：尹卫平[1] 刘华清[1] 高嘉屿[1] 曹冉冉 

机构地区：[1]河南科技大学化工与制药学院,河南洛阳471023

出　　处：《中草药》2016年第14期2424-2427,共4页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金青年基金(U1504830)

摘　　要：目的研究皂角刺Gleditsiae Spina(皂荚干燥棘刺)的化学成分。方法利用硅胶、Sephadex LH-20等柱色谱法反复进行分离纯化,通过谱学分析和理化性质鉴定表征化合物的结构。细胞毒活性采用四甲偶氮唑盐(MTT)比色法,测定化合物对肝癌(Hep G2)、肺癌(A-549)和食管癌(EC109)细胞株的细胞增殖抑制率。结果从皂角刺90%乙醇提取物的醋酸乙酯部位分离得到3个香豆素类化合物,分别鉴定为滨蒿内酯(1)、异东莨菪内酯(2)和6-氨基-7-甲氧基香豆素(3)。结论化合物3为新的香豆素类化合物,命名为皂角香豆素A。化合物1、2为首次从该植物中分离得到。细胞毒活性研究显示化合物2对肺癌A549细胞有较强的增殖抑制活性,其IC50值为34.47μg/m L。Objective To investigate the chemical constituents from Gleditsiae Spina（the thorns of Gleditsia sinensis）. Methods The compounds were isolated and purified by silica gel, Sephadex LH-20 column chromatographic techniques, and their chemical structures were confirmed on the basis of spectroscopic analysis by the physicochemical properties. Cytotoxic activity using the MTT colorimetry method was performed to measure the inhibitory effect of the compounds on cell proliferation of Hep G2, A-549, and EC109. Results Three coumarins were obtained from the ethyl acetate soluble fraction of the 90% ethanolic extract and their structures were identified as scoparone（1）, isoscopoletin（2）, and 6-amino-7-methoxycoumarin（3）. Conclusion Compound 3 is a novel coumarin named gledisinmarin A. Compounds 1 and 2 are isolated from this plant for the first time. Compound 2 displays the stronger cytotoxicity against A549 cell with an IC50 value of 34.47 μg/m L, while cisplatin with an IC50 value of 11.50 μg/m L as a positive control.

关 键 词：皂角刺 皂角香豆素A 滨蒿内酯 异东莨菪内酯 抗肿瘤活性 

分 类 号：R284.1[医药卫生—中药学]