三种枪刀药属植物中新颖二萜结构的发现及其活性研究

Terpenoids with the characteristics of wide distribution in nature, diverse structures, and a variety of biological activities are important source of lead compounds in drug discovery. Hypoestes species have important medicinal value and have been used as folk medicine for the treatment of a variety of ailments. Previous phytochemical investigations on Hypoestes plants had resulted in the isolation of a number of diverse diterpenoids with potent biological activities. Among them, a novel verticillane diterpenoid, hypoestoxide with prominent anti-inflammatory and anti-tumor activities, was isolated from H. rosea growing in Africa, which have attracted increasing attention for pharmacology and organic synthesis. Previously, 25 diterpenoids including one caged and three rearrangement labdane diterpenoids were isolated from H. phyllostachys cv. Pink Splash by the applicant. Therefore, the project will take three Hypoestes genus plants as research. The chemical constituents will be explored by phytochemical methods, and their focused anti-inflammatory and anti-tumor activities, and structure-activity relationships will be conducted by means of chemical and biological methods. The project aims to get some active compounds with further development and utilization value, and at the same time provide the basis for the rational development and utilization of the Hypoestes species..Key words: Hypoestes; Novel diterpenoids; Biological activities; Structure-activity relationships.

萜类化合物在自然界中分布广泛、结构类型多样，具有多种多样的生理功能，是寻找和发现药物先导化合物的重要源泉。枪刀药属(Hypoestes)植物作为民族药或民间草药使用，具有重要的药用价值，研究表明该属植物中富含二萜类成分，其结构新颖多样，活性显著。其中，从非洲产的H. rosea中发现结构新颖的维替生烷二萜hypoestoxide，具有显著地抗炎、抗肿瘤活性，引起药理学和有机合成研究者的广泛关注。申请人前期从红斑枪刀药中发现25个二萜类成分，包括1个具有氧杂笼状结构和3个具有重排半日花烷骨架的新颖结构天然产物。基于此，本项目拟对我国资源丰富的三种枪刀药属植物中二萜类成分展开深入的研究，对所分离得到的化合物重点进行抗炎和抗肿瘤活性筛选，以期获得结构新颖的活性成分，并进行初步的构效关系研究。该项目的研究将对药物先导化合物的发现和枪刀药属植物资源的合理开发利用具有重要意义。

爵床科枪刀药属(Hypoestes)植物多作为民间草药使用，具有重要的药用价值，研究表明该属植物中富含二萜类成分，其结构新颖多样，活性显著。本项目系统开展三种枪刀药属植物红点草（H. phyllostachys）、枪刀药（H. purpurea）、三花枪刀药（H. triflora）的化学成分，从中分离鉴定180个化合物，其中萜类成分150个，包括新结构萜类化合物65个。部分萜类化合物开展血管舒张作用、抗糖尿病、抗肿瘤活性评价，发现2个活性显著具有舒张血管作用的半日花烷二萜和1个体内具有显著抗糖尿病活性化合物。共发表研究论文5篇，包括 SCI论文4篇，中文核心1篇，其中IF>6的论文1篇，申请专利2项，培养研究生1人。通过本项目的实施进一步丰富了枪刀药属植物化学成分和活性的多样性，为从该属植物中寻找药物先导化合物和进一步开发利用奠定坚实化学物质基础。