土木香和冷蒿中倍半萜内酯化合物抑制人乳腺癌细胞增殖活性及构-效关系研究  

Antiproliferative Activity of Sesquiterpenoids from Inula helenium and Artemisia frigida on Human Breast Tumor Cell Lines and Their Structure-Activity Relationship Investigation

作　　者：李明[1] 刘霞[2] 郭书翰[2] 董玫[2] 杜正伦 高鹏志[1] 宋铁鹰[1] 史清文[2] 

机构地区：[1]石家庄市第一医院,石家庄050011 [2]河北医科大学基础医学院法医学系,河北省法医学重点实验室,石家庄050017

出　　处：《天然产物研究与开发》2013年第4期555-557,529,共4页Natural Product Research and Development

基　　金：河北省科技支撑项目(11276103D-89);国家自然科学基金项目(81072551);河北省自然科学基金项目(C2010000489);河北省卫生厅指导性课题(20110550)

摘　　要：利用四唑盐(MTT)比色法检测菊科植物土木香和冷蒿中分离纯化的八种倍半萜内酯化合物对人乳腺癌细胞增殖活性的影响,探讨了倍半萜内酯化合物体外抑制人肿瘤细胞增殖作用以及化合物结构与活性之间的构-效关系。实验结果显示异土木香内酯和去氢-β-姜黄烯对人乳腺癌细胞的增殖均有明显的抑制作用,其他试验用倍半萜内酯即使在100μmol/L的高浓度下,对人乳腺癌肿瘤细胞的增殖不显示抑制活性,倍半萜内酯化合物抑制人肿瘤细胞增殖活性与其直型和角型结构无关,不饱和内酯是抑制肿瘤细胞增殖活性的必需基团。The objective of this study was to detect the antiproliferative effect of eight sesquiterpenoids isolated from In ula helenium and Artemisiafrigida on human breast tumor cancer cells, and to explore the preliminary relationship be tween structure and activity of the tested sesquiterpenoids. The antitumor activities of eight sesquiterpenoids against the MCF7 and KT cell lines were evaluated using MTr assay. Isoalantolactone （3） and dehydrocostuslactone （4） exhibited significant activities against human breast cell lines. The others did not showed activities against tested cell lines. The ex perimental results demonstrated that fivemembered 13unsaturated lactone group was necessary for the antiproliferation of human breast cell lines, the skeleton of these 8 sesquiterpene have little relationship with the activities in the tested cell lines.

关 键 词：土木香 冷蒿 倍半萜内酯化合物 乳腺癌细胞 增殖活性 构-效关系. 

分 类 号：Q946.91[生物学—植物学]