藤黄酸胺基醇酯的合成及其抗肿瘤活性

Synthesis and biological evaluation of aminoalcohol gambogate as anti-tumor agents

摘要: 以藤黄酸为原料，与相应的二溴烷烃反应得到藤黄酸溴代烷基酯，再将其与不同的胺反应得到20个藤黄酸胺基醇酯衍生物( 3a ~ 3t )，其结构经IR、MS、¹H NMR确证。采用MTT法测试目标化合物对肝癌细胞Bel-7402、SMMC-7721、Bel-7404、QGY-7701和 HepG2的体外抗肿瘤活性。结果显示，大多数化合物表现出较强的抗肿瘤活性，其中化合物 3c ， 3g ， 3h ， 3p 和 3t 活性强于藤黄酸， 3g 和 3h 的抗肿瘤活性强于紫杉醇。

Abstract: Gambogic acid(GA)was treated with corresponding dibromoalkanes to form brominated compounds, which were coupled with various amines to generate the target compounds 3a - 3t . Their structures were characterized by IR, MS and ¹H NMR. The effects of the target compounds on the proliferation of human HCC Bel-7402, SMMC-7721, Bel-7404, QGY-7701 and HepG2 cells were evaluated in vitro by MTT assay using GA and taxol as positive controls. Most of the GA derivatives( 3c , 3g , 3h , 3p , 3t )displayed more potent activity against liver cancer cells than GA, and the activities of 3g and 3h were even more potent than that of taxol.