山芝麻中化学成分与抗肿瘤活性研究

Studies on chemical constituents and their anti-tumor activities in roots of Helicteres angustifolia

目的研究山芝麻中的化学成分及其抗肿瘤活性。方法采用硅胶柱层析、制备薄层层析等色谱方法,对山芝麻乙醇提取物分离纯化,用波谱和薄层方法进行化合物结构鉴定。鉴定出的化合物,采用四甲基偶氮唑蓝(MTT)法观察化合物对人结肠癌细胞(HT-29)和卵巢癌细胞(OVCA429)的抑制增殖作用。结果分离出的9种化合物分别是葫芦素B(cucurbitacin B)(Ⅰ),葫芦素E(cucurbitacin E)(Ⅱ),迷迭香酸(rosmarinic acid)(Ⅲ),十二硫醇(Dodecanethiol)(Ⅳ),β-谷甾醇(β-sitosterol)(Ⅴ),乌苏酸(Ursolic acid)(Ⅵ),细辛脂素(Asarinin)(Ⅶ),麦角甾醇(Ergosterol)(Ⅷ),2,6-二甲氧基对醌(2,6-dimethoxy-p-quinone)(Ⅸ)。以荷瘤小鼠S180为模型,观察其体内抗肿瘤作用。山芝麻的乙醇提取物在高剂量组抑瘤率为54.73%,表现出较好的抗肿瘤活性。经过MTT分析,化合物Ⅶ的IC50值显示对HT-29细胞显著抗增殖作用,对OVCA429细胞表现出微弱的抑制活性。化合物Ⅴ对HT-29细胞和OVCA429细胞都只有轻中度抑制作用。此外,化合Ⅲ和Ⅳ只对OVCA429细胞表现为轻度抑制活性,其它化合物没有显示针对这两种人癌细胞系的抗增殖作用(IC50>100μmol·L-1)。结论山芝麻具有多种化学成分,部分具有较好的抗肿瘤活性,值得更加深入的研究。

Objective To study the chemical constituents and the anti -tumor activity in roots of Helicteres angustifolia（HA）.Meth-ods Silica gel column chromatography,preparative thin layer chromatography and other chromatographic methods were used to isolate the compounds from HA spectral and thin layer methods were used to identify the compound structures.Effects of these compounds on the proliferations of HT -29 cells and OVCA -429 cells were tested by MTT method.180 mice tumor model was established to observe anti-tumor activity in vivo of HA extracts.Results Cucurbitacin B （I）,cucurbitacin E （II）,rosmarinic acid （III）,dodecanethio （IV）,β-sitosterol（V）,ursolic acid （VI）,asarinin （VII）,ergosterol （VIII）and 2,6 -dimethoxy -p -quinone （IX）were isola-ted from HA.Compound VII showed a significant inhibitory activity on HT -29 cells and a weak inhibitory activity on OVCA429 cells. Compound V showed little inhibitory activity on HT -29 cells and OVCA429.In addition,the compounds IV and III only showed mild inhibitory activity on OVCA429 cells.Conclusion Some of the compounds in HA have significant anti -tumor activity,which is wor-thy of further study.