摘要
目的阐明民间用于癌症治疗的长叶水麻Debregeasialongifolia(Burm f )Wedd 的化学成分及其抗肿瘤活性。方法用小鼠乳腺癌tsFT2 10细胞的流式细胞术筛选模型 ,确定抗肿瘤活性部位 ;利用大孔树脂HP - 2 0、SephadexLH - 2 0、硅胶等柱色谱和制备HPLC色谱等技术 ,分离精制活性部位的化学成分 ;根据理化性质和波谱数据鉴定化合物的化学结构 ,用流式细胞术评价其抗肿瘤活性。结果与结论从长叶水麻活性部位分离鉴定了没食子酸 (1)、3,5 二甲氧基没食子酸 4 O β D 吡喃葡萄糖苷 (2 )和 (- ) 表儿茶素 (3)等 3个酚酸类化合物 ,其中 ,化合物 1具有细胞周期G2 /M期抑制活性。化合物 1和 2系首次从长叶水麻中分离得到 ,1为该植物抗肿瘤活性成分的首例报道。
Aim To clarify the antitumor constituents of Debregeasia longifolia (Burm.f.)Wedd.,a Chinese folk medicine was used for the treatment of cancers.Methods A bioactive fraction was obtained from the crude extract of D.longifolia through a bioassay-guided fractionation,and the chemical constituents of the fraction were examined to obtain pure compounds by the use of column chromatography over HP-20,Sephadex LH-20 and silica gel,preparative HPLC over reversed phase C18 and recrystallization.The structures of the compounds obtained were elucidated by the spectroscopic method and the antitumor activity was assayed by the flow cytometry using a mouse tsFT210 cells.Results Three phenolics-derived compounds were isolated from the bioactive fraction of the crude extract of D.longifolia .Their structures were identified as gallic acid(1 ),3,5-dimethoxygallic acid-4- O-β-D -glucopyranoside(2 )and(-)-epicatechin(3 ),respectively.Among them,1 inhibited the cell cycle progression of the tsFT210 cells at the G2/M phase with the MIC value of 12.5 μg/mL,coinciding with the same effect reported in the literature [5] ,while 2 and 3 showed no effect on the present bioassay.Conclusion Compounds 1 and 2 were isolated from D.longifolia for the first time,and 1 provides the first example of antitumor constituents of the same plant,which possesses cell cycle inhibitory activity.
出处
《中国药物化学杂志》
CAS
CSCD
2004年第4期193-196,共4页
Chinese Journal of Medicinal Chemistry
基金
国家重点基础研究发展规划项目 (G19980 5 1113)
国家杰出青年科学基金项目 (3982 5 12 6 )
国家教育部长江学者奖励计划资助项目
关键词
药物化学
分离
鉴定
色谱分离
长叶水麻
酚酸类
抗肿瘤
medicinal chemistry
isolation
identification
chromatographic isolation
Debregeasia longifolia
gallic acid
3,5-dimethoxygallic acid-4-O-β-D-glucopyranoside
eicatechin
antitumor activity
