二聚单萜吲哚生物碱结构复杂、新颖多样，具有显著的生物活性，是药物筛选和发现的重要源泉。前期工作发现夹竹桃科植物药用狗牙花中的3个二聚单萜吲哚生物碱对五株人癌细胞具有显著的体外生长抑制活性。因此，本项目拟对5-6种云南产夹竹桃科植物的二聚单萜吲哚生物碱先进行富集分离鉴定，然后对其中量大但活性弱或无活性的单分子单萜吲哚生物碱混合物不经纯化直接进行针对性仿生偶联反应，形成新的二聚单萜吲哚生物碱，进行抗肿瘤等活性筛选，探讨构效关系。如此可避免单分子生物碱纯化前的损失，尽量多地得到结构新颖或含量高的二聚单萜吲哚生物碱。这种“分离-改造-分离-活性筛选”的研究模式对快速发现新颖结构的二聚单萜吲哚生物碱、增加其含量或活性等具有重要的意义。预期分离鉴定二聚单萜吲哚生物碱100个，其中1-2个化合物具有显著的活性，为进一步的创新药物研制和合理开发利用资源提供依据。

The structure of monoterpenoid bisindole alkaloids is complex, novel, diverse and has significant biological activity, which is an important source of drug screening and discovery. Our previous study showed that three monoterpenoid bisindole alkaloids from Tabernaemontana bovina (Apocynaceae) had significant inhibitory activity on the growth of five human cancer cells. Therefore, this project intends to first isolate and identify monoterpenoid bisindole alkaloids from 5-6 species of Apocynaceae from Yunnan, and then to form new structures of monoterpenoid bisindole alkaloids by biomimetic assembly of left and mixed monoterpene indole alkaloids with large amounts but weak activity or no activity. The isolated monoterpenoid bisindole alkaloids were assayed for antitumor activity and to explore the structure-activity relationship. The method could provide as much as possible the monoterpenoid bisindole alkaloids of new or high content, while avoiding the loss of monoterpenoid indole alkaloids and trace amounts of monoterpenoid bisindole alkaloids before the isolation and purification. The research model of "separation - transformation - separation - activity screening" is of great significance for the rapid discovery of novel structure of monoterpenoid bisindole alkaloids, increasing their content or activity. It is expected to identify 100 isolates of monoterpenoid bisindole alkaloids, of which 1-2 compounds have significant activity, and provide the basis for further development of innovative drugs and rational exploitation and utilization of resources.