五种西部地区产血桐属植物的化学成分及其抗肿瘤活性研究

Discovery of bioactive lead compounds is crucial step for innovative drug research. Natural products is considered to be one of the important ways of anti-cancer drug research in searching for bioactive lead molecules due to the diversity of their structure and biological activity. Isopentenyl and terpene substituted aromatic compounds has become an important research content in natural drug development for their diversity of skeleton types with novel and unique structures. In the plants of genus Macaranga (Euphorbiaceae family), prenylated derivatives and terpenoids can easily polymerize with aromatic compounds and generated novel natural molecules. Up to now, only few studies have been reported on the chemical constituents of this genus in China. In our previous research, the chemical constituents of 4 species of genus Macaranga and their antitumor activity have been researched and found some unique natural molecules generated by the prenylated and terpenoids substituted lavonoids or stibenes, and some of isolates shows good antitumor activity. This project aims at studying the chemical constituents of 5 species of genus Macaranga in western region of China and their antitumor activity systematically. The research will provide scientific basis the rational utilization of the plant resources of this genus and provide new information for the research and development of new anticancer drug with independent intellectual property of China.

发现有生物活性的先导化合物是创新药物研究的前提基础，天然产物由于具有结构类型及生物活性多样性特点，被认为是抗癌药物研发中寻找活性先导分子的重要途径之一。异戊烯基及萜类取代的芳香化合物由于骨架类型多样、结构新颖独特，已成为天然药物研发中的重要研究内容。大戟科血桐属（Macaranga）中的异戊烯基衍生物及萜类化合物容易与芳香化合物发生聚合而产生一些结构新颖的天然分子，且国内对该属植物的化学成分研究较少，因此项目组对4种血桐属植物进行了初步的化学成分和抗肿瘤活性研究，发现了一些结构独特的异戊烯基及萜类与二苯乙烯和黄酮类化合物的聚合体，并显示出较好的抗肿瘤活性。本项目拟继续对西部地区产的5种血桐属植物的化学成分及抗肿瘤活性进行系统研究，为合理开发利用该属植物资源和研发具我国自主知识产权抗癌新药提供科学依据。

发现有生物活性的先导化合物是创新药物研究的前提基础，天然产物由于具有结构类型及生物活性多样性特点，被认为是抗癌药物研发中寻找活性先导分子的重要途径之一。异戊烯基及萜类取代的芳香化合物由于骨架类型多样、结构新颖独特，已成为天然药物研发中的重要研究内容。大戟科血桐属中的异戊烯基衍生物及萜类化合物容易与芳香化合物发生聚合而产生一些结构新颖的天然分子，且国内对该属植物的化学成分研究较少，本项目完成了中平树（M. denticulata），山中平树(M. hemsleyana Pax et Hoffm)，泡腺血桐（M. pustulata），海南血桐（M. hemsleyana），鼎湖血桐（M. sampsonii）等5种血桐属植物的化学成分和生物活性探讨研究，并为了进一步拓展和丰富本项目所研究的化合物类型的多样性，开展了一种与血桐属植物同为大戟科的大戟属植物泽漆（Euphorbia helioscopia）的化学成分和生物活性研究，从6种植物中共分离得到150个化合物，开展了抗肿瘤活性研究，并拓展性探索了抗炎症和抗病毒活性的初步研究，取得了系列研究结果，如发现了系列新的异戊烯基取代的黄酮类分子和结构新颖的二萜类分子以及发现了活性分子Cirsitakaoside，目前部分结果已经正式发表论文5篇，申请专利1项。研究结果为合理开发利用该属植物资源和研发具我国自主知识产权抗癌新药提供科学依据。