三沙永兴岛两种短指软珊瑚中抑制NF-κB活性萜类化合物的发现

项目名称： 三沙永兴岛两种短指软珊瑚中抑制NF-κB活性萜类化合物的发现

项目编号： No.21302198

项目类型： 青年科学基金项目

立项/批准年度： 2014

项目学科： 数理科学和化学

项目作者： 杨斌

作者单位： 中国科学院南海海洋研究所

项目金额： 25万元

中文摘要： 软珊瑚中富含多种结构新颖、活性显著地次生代谢产物，多年来一直是海洋天然产物研究的热点。前期的筛选实验显示，我们采集自三亚东锣岛的短指软珊瑚中萜类化合物种类多样，结构新颖，分离的49个化合物中包括41个萜类化合物，其中新化合物23个，从中筛选到多个萜类化合物具有明显的抑制肿瘤相关因子NF-κB活性。为了筛选和发现我国南海短指软珊瑚中抑制NF-κB的萜类化合物，我们运用现代色谱学的分离手段和波谱学的结构鉴定技术，以萜类化合物核磁氢谱特征峰为导向并结合HPLC分析快速分离采集三沙市永兴岛附近海域的两种短指软珊瑚中萜类化合物，利用HEK-293细胞系上建立的NF-κB结合序列驱动的荧光素酶报告基因的稳转株对得到的萜类化合物进行NF-κB抑制活性检测，以便寻找到具有显著抗肿瘤的萜类化合物，特别是能抑制NF-κB的先导化合物，为新型抗肿瘤药物的研发提供科学依据和物质基础。

中文关键词： 软珊瑚；核因子kB；抗肿瘤；萜类化合物；

英文摘要： Marine organisms are a rich source of novel, bioactive secondary metabolites, and the interest in the marine organisms continues to grow every year, with soft coral being a consistent source of active metabolites. In our previous study on the bioactive constituents of soft coral, 49 compounds, including 41 terpenoids, were isolated from soft coral Sinularia kotanianensis, collected from Dongluo Island, Sanya. Some of these terpenoids showed significant inhibitory activity toward NF-κB. Aim to systematically study the chemical constituents of soft coral in the South China Sea, and to search for novel antitumor terpenoids, we have collected two soft coral Sinularia sp. from the Yongxing Island,Sansha. Guided by 1H-NMR informations and HPLC analysis, we will purify and characterize terpenoids from these soft coral. These compounds will be elucidated by spectroscopic and chemical methods. Using the cell-based HEK293 NF-κB luciferase reporter gene assay, the isolated terpenoids will be evaluated for inhibition of NF-κB activation. This progect is going to find some terpenoids as inhibitors of NF-κB, and provide theoretical basis to further research in a productive manner.

英文关键词： Soft coral；NF-κB；anticancer；terpenoids；