新型芳香基苦参碱衍生物的合成及抗肿瘤活性研究

Study on synthesis and anti-tumour activity of matrine derivatives with aryl

摘要:

分别用茴香醛、黎芦醛、3,4,5-三甲氧基苯甲醛、2,3,4-三甲氧基苯甲醛与苦参碱在氢化钠的催化作用下，利用Claisen-Schimidt缩合反应合成4个芳香基苦参碱衍生物；应用正交试验设计优化合成工艺条件。采用MTT法测试目标化合物对人结肠癌细胞株HT-29，人胰腺癌细胞株PANC-1的增殖抑制活性。结果显示：合成的4个芳香基苦参碱衍生物对这两种癌细胞均有明显的增殖抑制作用，较先导化合物苦参碱有更好的抗肿瘤活性。

Abstract:

Four matrine derivatives were synthesized by Claisen-Schimidt condensation in which matrine reacted with anisaldehyde or veratrum aldehyde or 3,4,5-trimethoxy-benzaldehyd or 2,3,4-trimethoxy-benzaldehyd in sodium hydride solution. The most suitable condition for the synthesis was decided by the orthogonal experiment. Inhibitory effects of these compounds were determined by the MTT assay on the growth of HT-29 cells and PANC-1 cells. These compounds exhibited better inhibitory effects than matrine . Four matrine derivatives being synthesized have better anticancer activity than matrine.