Chemical Constituents in Chloroform Extraction of Tetrastigmatis hemsleyani Diels et. Gilg and Their Antitumor Activities

目的研究三叶青三氯甲烷部位的化学成分及其体外抗肿瘤活性。方法利用硅胶,制备薄层板,lH-20等各种色谱技术分离单体化合物,通过nMr和质谱对化合物进行结构鉴定,并采用气-质联用色谱对三叶青三氯甲烷部位的其他成分进行分析,采用MTT法对分离得到的单体化合物进行抗肿瘤活性评价。结果通过经典色谱法分离得到6个化合物,分析鉴定为β-谷甾醇(1),4-羟基-3-甲氧基苯甲醛(2),齐墩果酸(3),5-羟甲基糠醛(4),壬二酸(5)和香草酸(6),并通过gC-MS指认了22个化合物。结论化合物2~6首次从三叶青中分离得到。化合物1和3对HElA229有较强的细胞毒活性,IC50分别为40.78,25.69μg·M l-1。化合物3对A375有较强的细胞毒活性,IC50为69.87μg·M l-1。三叶青三氯甲烷部位的体外抗肿瘤活性由多种成分共同作用产生。OBJECTIVE To investigate the chemical constituents in chloroform extraction of Tetrastigmatis hemsleyani diels et.Gilg and their antitumor activities.METHODS Various chromatography techniques such as column chromatography on silica gel,Sephadex LH-20 and preparative TLC were used to isolate and purify the compounds.Their structures were identified by1H-NMR,13C-NMR and MS.Their antitumor activities was tested by MTT method.Moreover,the other compounds of chloroform extraction were detected by GC-MS.RESULTS Six compounds were isolated by classic chromatography and identified as β-sitosterol( 1),4-hydroxy-3-methoxybenzaldehyde( 2),oleanolic acid( 3),5-hydroxymethyl furfural( 4),azelaic acid( 5),vanillic acid( 6).Twenty-two compounds were identified by GC-MS.CONCLUSION Compounds 2-6 are isolated from this plant for the first time.Compounds 1 and3 shows strong cytotoxic activities against Hela229 with IC50 values of 40.78,25.69 μg · m L-1,respectively.Compound 3 also showed strong cytotoxic activities against with IC50 values of 69.87 μg·m L-1.The result proved that antitumor activity of chloroform extraction of Tetrastigmatis hemsleyani diels et.Gilg is due to the contribution of multi-components.宁波市自然科学基金资助项目(2012A610181