本文总结了课题组近年来对10种海洋生物和中药中具有抗肿瘤特别是抗神经胶质瘤作用的皂苷成分的研究成果。对3种海星、5种海参和2种植物中药的皂苷成分进行了系统的提取、分离和结构鉴定，共鉴定了78个皂苷，其中新化合物53个，多数化合物都具有新颖的结构特征。多数皂苷具有显著的体外抗肿瘤特别是抗神经胶质瘤作用，部分皂苷经原位给药(间质化疗)显示显著的体内抗胶质瘤作用并克服了皂苷常见的溶血副作用。抗肿瘤作用机制涉及干预细胞周期、诱导凋亡、微管稳定以及多条信号通路。该研究为进一步开发抗胶质瘤新药提供了有价值的先导化合物和科学依据。皂苷原位给药方式的成功有效克服了限制皂苷成药性的关键瓶颈——溶血性，表明抗神经胶质瘤可能是皂苷类抗癌新药开发的突破口。

This paper reviews our recent progress in studying the saponins possessing antitumor effects, especially anti-glioblastoma effects, extracted from ten species of marine organisms and Traditional Chinese Medicines. Systematic extraction, isolation and structural elucidation have been performed for the saponin constituents from three species of starfishes, five species of sea cucumbers and two species of medicinal plants, resulting in the identification of 78 saponins, among which 53 are new compounds. Most of the new compounds possess relatively rare structural features. Most of the saponins show in vitro cytotoxicity against tumor cells, especially glioblastoma cells. Several saponins exhibit significant anti-glioblastoma effects in vivo by in situ administration (interstitial chemotherapy), and their haemolytic side effects can be avoided in the tests. Multiple mechanisms of action, such as interfering with cell cycle progression, inducing apoptosis, promoting stabilization of microtubule, as well as several signal transduction pathways, are involved in their anticancer effects. Our study may provide leads for developing new anti-glioblastoma drugs, and establish a homebase for the further development of these marine and terrestrial organisms. The success of the approach to administrate saponins in situ has conquered the bottleneck in the development of saponins as new drugs-haemolytic effects. These results indicate that anti-glioblastoma may become the breakthrough point for pursuing new anticancer drugs from saponins.

国家“863”计划项目（2006AA09Z423）：海星和海绵中抗肿瘤先导化合物的发现及活性评价，负责人：林厚文；国家“863”计划项目（2007AA09Z401）：基于化学生态学的海洋苔藓动物次生代谢产物结构多样性及其抗肿瘤活性先导化合物的发现，负责人：汤海峰；国家自然科学基金（20502035）：基于促微管聚合作用的海星皂苷的分离鉴定和抗肿瘤活性研究，负责人：汤海峰；国家自然科学基金（30873402）：新的中药皂苷成份抑制恶性胶质瘤增殖的机制研究及构效关系分析，负责人：程光。