甘遂的化学成分及其活性研究

Chemical constituents in root tubers of Euphorbia kansui and their activities

目的对甘遂Euphorbia kansui毒性部位的化学成分进行提取分离和鉴定;并对化合物进行细胞毒活性筛选。方法通过硅胶柱色谱、制备型高效液相色谱等方法进行分离纯化,根据波谱数据分析（MS、1H-NMR、13C-NMR）鉴定化合物结构;通过MTT法对单体化合物进行细胞毒活性测试。结果从甘遂乙醇提取物的醋酸乙酯部位分离得到9个化合物,分别鉴定为甘遂萜脂B（1）、3-O-（2,3-二甲基丁酰基）-13-O-十二烷酰基-巨大戟二萜醇（2）、5-O-苯甲酰-20-去氧巨大戟二萜醇（3）、大戟醇（4）、异东莨菪素（5）、腺苷（6）、羟基酪醇（7）、2′,4′,7-三羟基异黄酮（8）、大黄素（9）。其中化合物1为假白榄烷型二萜类化合物,2、3为巨大戟烷型二萜类化合物,4为三萜类化合物。结论化合物6~8为首次从该植物中分离得到的化合物,3和9对肠上皮细胞ICE-6具有较好的抑制作用。

Objective To study the isolation and identification of the chemical constituents in the root tubers of Euphorbia kansui and screen the cytotoxic activity of monomer compounds. Methods The silica gel column chromatography and high performance liquid chromatography（HPLC） methodx were used. The structures were identified by the spectrum data analysis（MS, 1H-NMR, and 13C-NMR）; The cytotoxic activity of monomer compounds was determined by MTT method. Results Nine compounds were identified from the ethyl acetate part, respectively. They were kansuinin B（1）, 3-O-（2, 3-dimethylbutanoyl）-13-O-dodecanoyl-ingenol（2）, 5-O-benzoyl-20-deoxyingenol（3）, euphol（4）, isoscopletin（5）, adenosine（6）, hydroxytyrosol（7）, 2′, 4′, 7-trihydroxy isoflavone（8）, and emodin（9）. Among them compound 1 is jatrophane-type diterpene, compounds 2 and 3 are the ingenane-type diterpenes, compound 4 is triterpene compound. Conclusion Compounds 6-8 are isolated from this plant for the first time. Compounds 1 and 9 have the good inhibition on intestinal epithelial cells ICE-6.