怒江藤黄中酚类化合物抗肿瘤作用机制和构效关系研究

项目名称： 怒江藤黄中酚类化合物抗肿瘤作用机制和构效关系研究

项目编号： No.81202863

项目类型： 青年科学基金项目

立项/批准年度： 2013

项目学科： 医学八处

项目作者： 夏正祥

作者单位： 中国科学院上海有机化学研究所

项目金额： 23万元

中文摘要： 怒江藤黄（Garcinia nujiangensis）为我国特有植物。课题组在进行抗肿瘤活性筛选中，发现怒江藤黄（叶子、枝条和果实）丙酮提取物均有明显抗肿瘤活性。但是未见文献报道该植物的化学和药理研究。本项目在怒江藤黄提取物抗肿瘤实验疗效确切的基础上，拟采用活性导向与化学跟踪相结合，将现代微量、快速、在线等集成的分离分析策略与传统分离、分析技术相结合，对怒江藤黄的化学成分进行深入系统研究；结合前期对怒江藤黄叶子化学和药理研究的相关工作，对酚类成分抗肿瘤构效关系进行分析，力求寻找到不同结构酚类对抗肿瘤活性的影响规律；并且在药理研究的基础上，对特征酚类化合物抗肿瘤作用机理进行探求，阐明该类化合物发挥作用的靶点和通路。研究成果不仅对怒江藤黄资源的综合利用提供理论指导，而且对寻找抗肿瘤的中药具有重要的参考价值，为开发我国具有知识产权的新药奠定良好的基础。

中文关键词： 怒江藤黄；口山酮；多环多异戊烯基间苯三酚；抗肿瘤；细胞毒性

英文摘要： Garcinia nujiangensis is endemic to China. We are screening for anti-tumor constituents from T.C.M. The results showed that the acetone extract from the leaves, twigs and fruits of Garcinia nujiangensis had significant anti-tumor activity. However,Study on chemistry and pharmacology of the title plant have not been reported. So the proposed project is based on bioassay and chemistry-guided fractionation of Garcinia nujiangensis by modern minor, fast, online integration strategy and the traditional separation and analysis techniques, combined with the early work on chemical and pharmacological studies. Determined to analyze the structure-activity relationship of anti-tumor phenolic compounds, to explore the mechanism of the characteristics phenolic compounds on anti-tumor effect, to explain the target and pathway of antitumor compounds. The results not only provide theoretical guidance for the comprehensive utilization of Garcinia nujiangensis, but also has important reference value for finding anti-tumor constituents from traditional Chinese medicine, and lay a good foundation for the development of new drugs with Chinese intellectual property rights.

英文关键词： Garcinia Nujiangensis；xanthone；PPAPS；anti-tumour；cytotoxic