两种海南榕属植物抗肿瘤活性成分及其作用机制研究

海南岛是我国榕属植物分布的主要区域之一，其物种的多样性和丰富度都很高，国内外对榕属植物进行了较多的研究，但对大果榕和薜荔的抗癌活性成分及作用机制缺乏系统研究。课题组前期针对本地区热带药用植物资源进行抗肿瘤筛选时发现，大果榕的石油醚萃取物具有较强抗肿瘤活性，进一步化学成分分离，目前共完成32个化合物的分离及结构鉴定，包括3个结构新颖的大环内酯lasiodiplodins类似物。本项目拟运用植物化学和药理学相结合的方法，在抗肿瘤活性导向下，利用现代分离手段深入开展海南地区榕属植物大果榕和薜荔中新颖结构化学成分的分离分析研究，并对分离得到的化合物进行体外肿瘤细胞增殖抑制活性测试；以细胞增殖、细胞周期调控、细胞凋亡及胞内钙离子浓度等对活性优良化合物进行作用机制研究，可望优选出结构新颖、活性高、选择性较好的药物先导化合物，为创制自主知识产权的新型抗肿瘤药物奠定基础。

Hainan Island is one of the major regional distribution of Ficus plants in China, where the species diversity and richness are high. There is little systematic study on these medicinal plants of Hainnan region. In the chemical and biological activity studies of a series of Hainan medicinal plants, we found that the petroleum ether fraction of the ethanol extracts of Ficus auriculata showed good anticancer properties. Thirty two compounds have been isolated and identified from this active fraction,including three novel compounds structurally similar to the macrolide compound lasiodiplodin. This project aims to continue to employ phytochemical and pharmacological methods to further understand the chemical composition and the antitumor activity of two endimic species. The mechanisms of action of active constituents on cell morphology、cell cycle、cell apoptosis、intra-cellular calcium ion concentration will also be investigated. Our efforts are expected to lead to the identification of potent and selective anticancer compounds that have novel molecular structures,laying a foundation for developing new antitumor agents with independent intellectual property rights.