齐墩果酸衍生物的合成及抗肿瘤活性的研究

Synthesis and anti-tumor activity of oleanolic acid derivatives

摘要:
以天然产物齐墩果酸为先导化合物, 经过氧化、酯化 (酰化)、水解等反应设计合成了10个齐墩果酸衍生物, 以HeLa、HepG2和BGC-823细胞为靶细胞, 采用MTT法用吉非替尼和依托泊苷作阳性对照, 进行初步的体外抗肿瘤活性筛选。结果表明, 化合物5a对HepG2细胞、化合物7对HeLa细胞的抑制活性明显高于母体齐墩果酸。因此, 化合物5a和7值得进一步研究。

Abstract:
Structural modifications were performed with natural product of oleanolic acid to search for novel anticancer drugs. Ten oleanolic acid derivatives were designed and obtained by the reaction of oxidation, acylation or hydrolyzation, etc. The cytotoxic activity of derivatives was evaluated against HeLa, HepG2 and BGC-823 cells in vitro by MTT assay, gefitinib and etoposide used as a positive control. The results showed that compound 5a was particularly active to inhibit HepG2 cells growth, and anti-tumor activity of compound 7 on HeLa cells was significantly stronger than oleanolic acid. They are worthy to be studied further.