水溶性海星皂苷的分离纯化及其抗肿瘤活性研究

为利用废弃海星壳资源开发出纯天然抗肿瘤药物,通过AB-8型吸附树脂、常压硅胶与Sephadex LH-20葡聚糖凝胶的柱层析技术,从罗氏海盘车(Asterias rollestoni Bell)壳的水抽提液中分离纯化出水溶性海星皂苷,并对其体内外抑瘤活性进行了研究。分离纯化与性质鉴定的结果显示,所得水溶性海星皂苷的性质隶属于甾体皂苷,其纯化样品的纯度可高达99.6％;体外抑瘤活性检测结果证实,所得皂苷纯品对HeLa宫颈癌细胞、SGC-7901胃癌细胞、A-549肺癌细胞和Bel 7402肝癌细胞均具有显著的抑制活性。50mg／L皂苷对这4种癌细胞的抑制率分别为(92.06±2.60)％、(95.22±2.87)％、(95.04±3.30)％和(91。60±4。30)％,其IC50值分别为7.05、5.28、5.32、6.16mg／L。体内抑瘤活性检测结果证实,灌胃剂量为2、 5、 10μg／g的皂苷纯品对S180实体瘤荷瘤小鼠均具有显著的抑制活性,并具有浓度依赖性,10μg／g皂苷纯品的抑瘤率可高达46.27％,高于10μg／g抗肿瘤药物环磷酰胺(CTX)的抑瘤率(41.04％);同时,2、 5、 10μg／g的皂苷纯品还均能浓度依赖性地显著提高荷瘤小鼠的胸腺指数和脾指数。

Purification and anti-tumor activity examination of water-soluble asterosaponin from Asterias rollestoni Bell

To develop natural anti tumor medicaments from abandoned starfish shells, water soluble asterosaponin from Asterias rollestoni Bell were isolated, purified and their anti tumor bioactivities were examined. After extracted with hot water and purified with macroporous resin column and silica gel column chromatograghy respectively, water soluble asterosaponin with purity of 99.6％ and properties of steroidal saponins was obtained. In vitro anti tumor activity examination showed that the purified asterosaponin had high anti tumor activity on HeLa cells, SGC 7901 gastric cancer cells, A 549 lung cancer cells and Bel 7402 hepatocarcinoma cells. The inhibiting rate of 50 mg／L asterosaponin to the above four kinds of cancer cells was(92.06±2.60)％, (95.22±2.87)％, (95.04±3.30)％ and (91.60±4.30)％, and its corresponding IC50 value to these cells was 7.05, 5.28, 5.32 and 6.16mg／L, respectively. In vivo anti tumor activity examination showed that the purified asterosaponin at the dose of 2.10μg／g bodyweight had obvious inhibiting effect on the S180 solid tumor in mice in a dose dependent manner. And tumor inhibiting rate of 10μg／g asterosaponin was as high as 46.27％, higher than that of 10μg／g cyclophosvnamide (CTX, one kind of anti cancer drugs). Besides, 2.10μg／g asterosaponin could obviously increase the thymus index and spleen index of the tumor-bearing mice.