转筋草的抗肿瘤迁移化学成分研究

目的研究转筋草Pachysandra terminalis中抗肿瘤迁移活性成分。方法综合运用硅胶柱色谱、凝胶柱色谱、HPLC制备色谱等多种色谱法对转筋草提取物中的活性部位进行分离纯化;采用NMR等波谱学方法鉴定化合物结构;通过趋化实验和伤口愈合实验评价单体化合物的抗肿瘤迁移活性。结果从转筋草中分离得到6个化合物,分别为粉蕊黄杨二醇A(1)、(+)-(20S)-20-dimethylamino-3-(3α-methylsenecioylamino)-5α-pregn-12β-ol(2)、2,4-二羟基苯乙酮(3)、香草酸(4)、epipachysamine D(5)、β-谷甾醇(6)。抗肿瘤迁移实验结果表明:化合物2、5在浓度为10μg·m L-1时趋化抑制率分别为74.1%、82.5%。结论化合物1⁴均为首次从该植物中分离得到;化合物2、5有抗肿瘤迁移活性。

Anti-tumor metastatic constituents from Pachysandra terminalis Sieb. Zucc

Objective To study the anti-tumor metastatic constituents from Pachysandra terminalis Sieb. Zucc. MethodsConstituent isolation and purification were carried by repetitive column chromatography（silica gel, Toyopearl HW-40 and preparative HPLC）. Their structures were elucidated on the basis of spectral data analysis. Anti-tumor metastasis assay and wound healing migration assay were used to evaluate the isolated compounds of their activities. Results Six compounds（1- 6） were isolated and identified as follows： pachysandiol A（1）;（ ＋）-（20S）-20-dimethylamino-3-（3α-methylsenecioylamino）-5α-pregn-12β-ol（2）; 2, 4-dihydroxy-phenylethanone（3）; vanillic acid（4）; epipachysamine D（5） and β-sitosterol（6）. At 10 μg·mL^- 1, compound 2 and 5 revealed positive anti-tumor metastatic activities with an inhibition rate of 74.1% and 82.5%. Conclusion Compound 1- 4 have been isolated from Pachysandra terminalisSieb. Zucc for the first time. Compound 2 and 5 show positive anti-tumor metastatic activities.