粟米草三萜类化学成分及其活性研究

目的研究粟米草Mollugo pentaphylla中的三萜类化学成分,寻找其中具有细胞毒活性化合物。方法综合运用大孔吸附树脂、硅胶柱色谱、半制备型高效液相及SephadexLH-20凝胶柱色谱等各种色谱技术进行系统化学研究,根据其理化性质和MS、NMR等波谱数据鉴定化合物结构,同时对所得的三萜皂苷进行细胞毒活性测试。结果从粟米草干燥地上部分醇提取物中共分离得到6个三萜类化合物,分别鉴定为粟米草苷E(1)、3-O-α-L-rhamnopyranosy1(1→2)-α-L-arabinopyranosyl]-28-O-β-D-glucopyranosyl (1→6)-β-D-glucopyranosyl] oleanolic acid(2)、竹节香附皂苷R8(3)、竹节香附素A(4)、mollugogenolsA(5)、齐墩果酸(6)。细胞毒活性显示,化合物1~5对人前列腺癌DU145细胞、人宫颈癌HeLa细胞及人早幼粒白血病HL-60细胞均显示一定的抑制作用,尤其是对人早幼粒急性白血病HL-60细胞,其IC50分别为10.21、38.43、40.28、20.59、83.16μmol/L。结论化合物1为新的齐墩果酸型三萜皂苷,2~4为首次从该植物中分离得到。细胞毒活性显示,化合物1~5对人前列腺癌DU145细胞、人宫颈癌HeLa细胞及人早幼粒白血病HL-60细胞均显示一定的抑制作用。

Chemical compositions and anticancer activity of Mollugo pentaphylla

Objective To investigate the chemical compositions and anticancer activity of Mollugo pentaphylla. Methods These compounds were isolated by various technologies, such as silica gel, Sephadex LH-20 and high performance liquid chromatography. Their structures were elucidated on the basis of physicochemical properties and spectroscopic data. The cytotoxic activities of compounds 1-5 against five cancer cell lines were tested by MTT. Results Six compounds were isolated from this plant and identified as mollugoside E(1), 3-O-α-L-rhamnopyranosy1(1→2)-α-L-arabinopyranosyl]-28-O-β-D-glucopyranosyl(1→6)-β-Dglucopyranosyl]oleanolic acid(2), raddeanoside R8(3), raddeanin A(4), mollugogenol A(5), and oleanolic acid(6). The cytotoxic activities results showed that compounds 1-5 had certain inhibitory effects on human prostate cancer DU145 cell lines, cervical cancer Hela cell lines and early-juvenile leukemia HL 60 cell lines, especially on HL 60 cells with IC50 value of 10.21, 38.43, 40.28, 20.59, and 83.16 μmol/L, respectively. Conclusion Compound 1 is a new triterpenoid saponin and compounds 2-4 are isolated first time from M. pentaphylla. The cytotoxic activities results showed that compounds 1-5 had certain inhibitory effects on DU145, Hela and HL 60 cell lines.