运用结构修饰和构建含氮二萜类似物库的方法挖掘麻疯树植物中抗肿瘤活性成分

项目名称： 运用结构修饰和构建含氮二萜类似物库的方法挖掘麻疯树植物中抗肿瘤活性成分

项目编号： No.81202437

项目类型： 青年科学基金项目

立项/批准年度： 2013

项目学科： 药物学、药理学

项目作者： 刘接卿

作者单位： 中国科学院昆明植物研究所

项目金额： 23万元

中文摘要： 麻疯树（Jatropha curcas L.）又名小桐子，为大戟科（Euphorbiaceae）麻疯树属植物，是国际上研究最多的能源植物之一，到2015年，将在中国种植1500万亩以上。现代药理研究表明其根皮和树皮具有抗肿瘤活性，但未从中开发出具有应用价值的药用成分或药物制剂。为有效开发大面积种植的麻疯树作为能源植物之外的医药用途，从中筛选生物活性特别是抗肿瘤活性的化合物，我们进行以下研究：1）对麻疯树中含量较高、细胞毒活性较好的二萜化合物curcusones A、B、C、D等进行结构修饰，阐明其构效关系，发现高活性化合物，为开发抗肿瘤药物奠定基础；2）从麻疯树根皮和树皮提取物中富集并构建不同极性大小的二萜化合物库，以天然二萜化合物库为底物，分别与含氮试剂如氨水、水合肼、胺等反应引入氮原子，构建含氮二萜类似物库，并从含氮二萜类似物库中筛选抗肿瘤活性或其它生物活性化合物。

中文关键词： 小桐子；抗肿瘤；结构修饰；构效关系；二萜

英文摘要： Jatropha curcas L. (XiaoTongZi), a species jatropha genus of Euphorbiaceae, attacted global attention as a biofuel crop. In China, more than 15 million acres of J. curcas will be cultivated by 2015. Pharmacological researches demonstrated that the root and stem barks of J. curcas possessed antitumor activities. However,neither medicinal preparation nor medicinal ingredients have been developed from J. curcas so far. For full utilization of the abundant resources of J. curcas, it is necessary to explore its bioactive, especially cytotoxic, constituents and its medicinal uses. Consequently, researches were conducted as follows: 1) Structural modification of curcusones A, B, C, and D, all of which are rich in root and stem barks and show slight cytotoxity, could clarify their structure-activity relationship (SAR), discover remarkable cytotoxic compounds, and lay the foundations for developing antitumor drug. 2) Accumulate the different polarity diterpenes from extracts of root and stem barks of J. curcas as the natural diterpene library (NDL). Subsequently, NDL reacted with nitrogenous reagens such as ammonia water，hydrazine hydrate, and amine for building nitrogenous diterpene-likeness library (NDLL), form which bioactive compounds with anticancer activity and other bioactivities were screened and identified.

英文关键词： jatropha curcas；anti-cancer；structural modification；structure-activity relationship；diterpene