狼毒大戟的化学成分及细胞毒活性研究

Chemical constituents and cytotoxic activity of Euphorbia fischeriana Steud

目的研究大戟科植物狼毒大戟的化学成分及其细胞毒活性。方法采用硅胶柱色谱等术分离纯化狼毒大戟中的化学成分,根据化合物的理化性质和波谱数据分析鉴定化合物的结构。采用噻唑蓝比色法探究9个化合物对肝癌细胞株和乳腺癌细胞株的细胞毒活性。结果共从狼毒大戟饮片中分离得到9个化合物,分别鉴定为岩大戟内酯B(1)、ebracteolatain A(2)、3,3'-二乙酰基-2,4'-二甲氧基-2',4,6,6'-四羟基-二苯基甲烷(3)、β-香树脂醇乙酸酯(4)、狼毒乙素(5)、β-谷甾醇(6)、euphebracteolatain A(7)、fischeria A(8)、岩大戟内酯A(9)。细胞毒活性研究发现,化合物1~9对肝癌细胞株HepG2无显著活性;化合物2对乳腺癌细胞株MCF-7、MDA-MB-231、Sum149、ZR-75-1、SKBr3、BT474的IC_(50)分别为(5.73±0.74)、(5.41±0.26)、(5.47±0.17)、(3.49±0.54)、(10.10±1.66)、(2.63±0.59)μmol·L^(-1)。化合物3对乳腺癌细胞株Sum149、ZR-75-1细胞毒活性明显,其IC_(50)分别为(5.23±0.44)、(10.13±1.80)μmol·L^(-1)。结论化合物3是新化合物,化合物7为首次从狼毒大戟中分离得到;化合物2和化合物3对乳腺癌细胞有显著细胞毒活性。

Objective To determine the chemical constituents of Euphorbia fischeriana Steud.and its cytotoxic activity.Methods The chemical constituents were isolated and purified by silica column chromatography,and identified by nuclear magnetic resonance spectrum analysis based on their physical characteristics.MTT was performed to determine the cycotoxic activities of these compounds on hepatoma carcinoma cells and breast cancer cells in vitro.Results Nine compounds were isolated and identified from Euphorbia fischeriana Steud.,including jolkinolide B(1),ebracteolatain A(2),3,3'-diacetyl-2,4'-dimethoxy-2',4,6,6'-tetrahydroxy-diphenyl(3),β-amyrin acetate(4),2,4-dihydroxy-6-methoxy-3-methyl-1-acetophenone(5),β-sitosterol(6),euphebracteolatain A(7),fischeria A(8),and jolkinolide A(9).Theses compounds had no significant cytotoxic activity on hepatocellular carcinoma cell line HepG2.The IC_(50) values of compound 2 for the breast cancer cell lines MCF-7,MDA-MB-231,Sum149,ZR-75-1,SKBr3 and BT474 were(5.73±0.74),(5.41±0.26),(5.47±0.17),(3.49±0.54),(10.10±1.66)and(2.63±0.59)μmol·L^(-1),respectively.The IC_(50) values of compound 3 for the breast cancer cell lines Sum149,and ZR-75-1 were(5.23±0.44),and(10.13±1.80)μmol·L^(-1),respectively.Conclusion Compound 3 is a new compound,and compound 7 has been isolated from Euphorbia fischeriana Steud.for the first time.Compound 2 and Compound 3 show cytotoxic activity on breast cancer cells.