2α,3β-二羟基齐墩果烷-12-烯-28β-醛的合成、表征及抗肿瘤活性研究

Synthesis and Characterization of 2α,3β-DihydroxylUrsa-12-en-28β-aldehyde and Preliminary Study on Anti-tumor Activities

以具有一定抗肿瘤活性的齐墩果酸为先导化合物,通过对C-2位、C-3位和C-28位进行结构修饰,得到具有抗肿瘤活性的五环三萜类化合物2α,3β-二羟基齐墩果烷-12-烯-28β-醛。并通过IR、HNMR和13C NMR对其结构进行表征。研究其对MCF-7(人乳腺癌细胞)和Hela(人宫颈癌细胞)的抑制作用。结果表明中间体和目标产物对两种癌细胞抑制作用均优于齐墩果酸。

In order to develop petacyclic triterpenoids with potential anti-tumor activities,we take the natural product oleanolic acid which with anti-tumor activity as the lead compounds for modifying their structures in this paper.2,3-DihydroxylUrsa-12-en-28-aldehyde were synthesized through modification at C-2,C-3 and C-28 of oleanolic acid.The structures of the compounds were confirmed by IR,1H NMR and 13C NMR.Finally,anti-tumor activities comparison among the new derivatives and OA was carried out.The result shows that the activation of target material and one of the intermediate was superior to oleanolic acid in anti-tumor.