两种陇产五加属药用植物中具有抗肿瘤活性的茋类成分研究

项目名称： 两种陇产五加属药用植物中具有抗肿瘤活性的茋类成分研究

项目编号： No.21462026

项目类型： 地区科学基金项目

立项/批准年度： 2015

项目学科： 环境科学、安全科学

项目作者： 胡浩斌

作者单位： 陇东学院

项目金额： 50万元

中文摘要： 短柄五加（Acanthopanax brachypus）和藤五加（Acanthopanax leucorrhizus）为我国特有的两种五加属药用植物，在甘肃有丰富的资源，其茎皮具有抗炎、抗肿瘤、抗血栓等功效，但至今国内外对其化学成分和生物活性尚缺乏研究。前期研究中，课题组首次从陇产两种植物的茎皮甲醇提取物中发现具有抗肿瘤活性的茋类成分。为此，本项目拟以其甲醇提取物的乙酸乙酯萃取物中的活性组分（ABE6和ALE5）为研究对象，在抗肿瘤活性的跟踪筛选下，采用高速逆流色谱等技术从中分离出约30个茋类成分，利用波谱和化学分析法确定单体结构，并针对其结构特点进行结构改造获得约50个衍生物，经体内外抗肿瘤活性研究和构效关系分析，优选出1-2个结构新颖、活性强、选择性高、毒性低的药物先导物。以阐明两种植物抗肿瘤活性的物质基础和作用机制，也为深入研究进而创制具有我国自主知识产权的新型抗肿瘤药物奠定基础。

中文关键词： 短柄五加；藤五加；抗肿瘤活性；茋类化合物；构效关系

英文摘要： Acanthopanax brachypus and Acanthopanax leucorrhizus, growing abundantly in Gansu province, are two peculiar medicinal plants of Acanthopanax in China. Their stem barks possess antiinflammatory, antitumor and antithrombosis properties, but chemical constituents and bioactivities are lack of research at home and abroad up to now. In preliminary work, we have firstly discovered antitumor stilbenoids from the methanol extract of the stem barks of the above two plants from Gansu province. Therefore, the active subfractions (ABE6 and ALE5) in ethyl acetate fraction from the methanol extracts will be taken as the research object, on the basis of antitumor activity screening,about 30 stilbenoids with novel structure will be isolated and purified from ABE6 and ALE5 by the application of some isolation techniques, especially the application of high-speed counter-current chromatography (HSCCC), and their structures will be elucidated by spectral and chemical analyses, about 50 derivatives will be obtained by structural modification according to the characteristics of structure, 1-2 drug leads with novel structure, strong activity, higher selectivity and low toxicity, will be optimized by the study of antitumor activity in vitro and in vivo and the analysis of structure-activity relationships.These researches will help clarify the substance basis and pharmacological mechanism about the antitumor activity of the above plants, simultaneously also lay the foundation for the deep study and create the new type of antitumor agents with independent intellectual property of China.

英文关键词： Acanthopanax brachypus;Acanthopanax leucorrhizus;antitumor activity;stilbenoid;structure-activity relationship