目的研究绿升麻中具有抗肿瘤活性的化学成分。方法以硅胶柱色谱、凝胶色谱等多种柱色谱分离,制备高效液相色谱纯化,得到单体化合物,以各有机波谱鉴定化合物结构。结果分离得到7个环菠萝蜜烷型三萜类化合物,鉴定为25-脱水升麻醇-3-O-β-D-木糖苷(25-anhydrocimigenol-3-O-β-D-xylopyranoside,Ⅰ)、25-乙酰升麻醇-3-O-β-D-木糖苷(25-O-acetylcimicigenol-3-O-β-D-xylopyranoside,Ⅱ)、升麻醇-3-O-α-L-阿拉伯糖苷(cimigenol-3-O-α-L-arabinopyranoside,Ⅲ)、升麻醇-3-O-β-D-木糖苷(cimigenol-3-O-β-D-xylopyranoside,Ⅳ)、3′-乙酰升麻醇-3-O-β-D-木糖苷(3′-O-acetylcimigenol-3-O-β-D-xylopyranoside,Ⅴ)、24-乙酰升麻醇-3-O-β-D-木糖苷[24-O-acetyl-shengmanol-3-O-β-D-xylopyranoside(23R,24R),Ⅵ]、24-O-acetylisodahurinol-3-O-β-D-xylopyranoside(Ⅶ)。结论化合物Ⅰ~Ⅶ首次从绿升麻中分离得到,抗肿瘤药理实验显示化合物Ⅰ、Ⅱ在质量浓度30μg/mL时对宫颈癌细胞(HeLa)和小鼠成纤维细胞(L929)具有较强细胞毒作用。

Objective To isolate and elucidate the antitumor constituents from the rhizoma of Actaea asiatica. Methods Chemical constituents were isolated by repeated column chromatography (Toyopearl HW-40C and HPLC) and their structures were elucidated on the basis of spectral data analysis. Results Seven cycloartane triterpeniods were isolated and identified to be 25-anhydrocimigenol-3-O-β-D-xylopyranoside (Ⅰ), 25-O-acetyl cimicigenol-3-O-β-D-xylopyranoside (Ⅱ), cimigenol-3-O-α-L-arabinopyranoside (Ⅲ), cimigenol-3-O-β-D-xylopyranoside (Ⅳ), 3′-O-acetyl cimigenol-3-O-β-D-xylopyranoside (Ⅴ), 24-O-acetyl shengmanol-3-O-β-D-xylopyranoside (23R, 24R) (Ⅵ), 24-O-acetyl isodahurinol-3-O-β-D-xylopyranoside (Ⅶ), respectively. Conclusion Compounds Ⅰ-Ⅶ are isolated from A. asiatica for the first time. Compounds Ⅰ and Ⅱ show significant inhibitory effects on HeLa and L929 cell lines of mice at the concentration of 30 μg/mL.

天津医科大学科研基金资助(2004xk32)