华泽兰化学成分及其抗肿瘤活性研究

Research on Chemical Constituents and Anti-tumor Activity of Eupatorium chinense

目的：研究华泽兰的化学成分及其抗肿瘤活性。方法：采用正相硅胶柱层析、制备薄层层析及制备型HPLC等方法分离纯化,利用NMR、MS等波谱学方法鉴定化合物结构,利用MTT比色法评价6个化合物的肿瘤细胞毒活性。结果：从华泽兰乙酸乙酯部位分离得到6个化合物,分别鉴定为：eupalinilide G（1）、8β-（4＇-hydroxytigloyloxy）-5-desoxy-8-desacyleuparotin（2）、3-（hydroxymethyl）-1,13,14,15-tetrahydroxy-7,11,15-trimethyl-2,6,10-hexadecatriene（3）、3-（hydroxymethyl）-1,13,15-trihydroxy-7,11,15-trimethyl-2,6,10-hexadecatrien-14-yl acetate（4）、eupafolin（5）、hiyodorilactone B（6）。化合物2对人胃癌HGC-27细胞及小鼠黑色素瘤B16细胞的IC50分别为4.29μg/m L、5.53μg/m L。结论：其中,化合物2~6为首次从华泽兰中分离得到;化合物2对HGC-27细胞有显著的细胞毒活性。

Objective： To study the chemical constituents and their anti-tumor activity of Eupatorium chinense. Methods： The chemical constituents were separated and purified by the normal phase silica gel column chromatography,preparative thin-layer chromatography,and preparative HPLC. Their structures were determined by various spectral data,their antitumor activity in vitro was determined by MTT assay. Results： Six compounds were isolated from the ethyl acetate extract of Eupatorium chinense,and the structures were identified as eupalinilide G（ 1）,8β-（ 4＇-hydroxytigloyloxy）-5-desoxy-8-desacyleuparotin（ 2）,3-（ hydroxymethyl）-1,13,14,15-tetrahydroxy-7,11,15-trimethyl-2,6,10-hexadecatriene（ 3）,3-（ hydroxymethyl）-1,13,15-trihydroxy-7,11,15-trimethyl-2,6,10-hexadecatrien-14-yl acetate（ 4）,eupafolin（ 5） and hiyodorilactone B（ 6）. Compound 2 showed cytotoxicity against HGC-27 and B16 cancer cell lines with IC50 values of 4. 29 μg/m L and 5. 53 μg/m L,respectively. Conclusion： Compounds 2 ~ 5 are isolated from the Eupatorium chinense for the first time,and compound 2 has significant cytotoxic activity against HGC-27 cell line.