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

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.