| 徐蕾,宋清平,杨爽,等.仿刺参(Apostichopus japonicus)中皂苷类成分的分离鉴定及细胞毒活性研究[J].中国海洋药物,2018,37(6):38-46. |
| 仿刺参(Apostichopus japonicus)中皂苷类成分的分离鉴定及细胞毒活性研究 |
| Study on isolation and tumor-cytotoxic activity of triterpene glycosides in Apostichopus japonicas |
| 投稿时间：2018-05-17 修订日期：2018-05-17 |
| DOI： |
| 中文关键词: 仿刺参 海参皂苷 分离鉴定 细胞毒。 |
| English Keywords:Apostichopus japonicas triterpene glycosides isolation and identification tumor-cytotoxic activity. |
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| 中文摘要: |
| 目的 对仿刺参(Apostichopus japonicus)体内皂苷类成分进行分离及结构鉴定,研究纯化皂苷的抗肿瘤细胞毒活性。方法 以鲜仿刺参为原材料,选用60%的乙醇溶液从海参中提取出海参皂苷,然后通过有机溶剂萃取法、大孔树脂法、硅胶柱层析、凝胶柱层析、半制备HPLC分离纯化海参皂苷,采用LTQ Orbitrap XL 质谱、Jeol JNM-ECP 600 核磁技术对得到的海参皂苷进行结构鉴定,以人肺癌细胞(A549)、人结肠癌细胞(HCT116)、人肝癌细胞(BEL-7402)、人肺腺癌细胞(NCI-H1975)和正常肝细胞(L-02)为对象对纯化皂苷抗肿瘤细胞毒活性进行研究。结果 从鲜仿刺参同时得到三种三萜皂苷类化合物,分别为Holotoxin D、Holotoxin B1和Holotoxin A1,产率分别为2.30×10-7、1.86×10-6和3.49×10-6。三种皂苷的细胞毒活性具有一致性,对肿瘤细胞具有良好的抑制率,抑制率均随皂苷单体浓度增大而增大,且到达一定浓度时之后趋于稳定,均呈现弱效抑制作用。结论 首次从鲜仿刺参中同时纯化得到Holotoxin D,Holotoxin B1和Holotoxin A1,比例为1:7.97:14.94。三种皂苷单体具有良好的抗肿瘤活性,Holotoxin D抗肿瘤活性为首次报道,本研究为以后的肿瘤药物的筛选研究奠定了良好的基础。 |
| English Summary: |
| Objective: The triterpene glycosides from the Apostichopus japonicas were isolated and identified, and tumor-cytotoxic activities of the compounds were further determined. Methods: The preparation of triterpene glycosides were extracted from fresh Apostichopus japonicas with 60% aq.ethanol. The triterpene glycosides were separated and purified by organic solvents, macroporous resin, silica gel column chromatography, gel column chromatography and semi preparative HPLC. The structures of them were determined by ESI-MS and NMR, the tumor-cytotoxic activities were studied with A549 cells, HCT116 cells and BEL-7402 cells by the SRB assay. Results: Three kinds of three triterpene glycosides were purified and identified, which were Holotoxin D, Holotoxin B1, Holotoxin A1, respectively. The cytotoxicity of three saponins was consistent, and had a good inhibitory effect on A549, HCT116 and BEL-7402, the inhibition rate of three saponins was the strongest at 12.5 μM and then tended to be stable, showing a weak inhibitory effect. Conclusion: Holotoxin D, Holotoxin B1 and Holotoxin A1 were purified from the Apostichopus japonicas for the first time synchronously, and the ratio was 1:7.97:14.94. The three kinds of saponins had good antitumor activity, and the anti tumor activity of Holotoxin D was the first report. This study laid a good foundation for screening tumor drugs in the future. |
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