硝酸酯类NO供体型齐墩果酸衍生物的合成及抗肿瘤活性

基金项目: 国家自然科学基金资助项目(No.2097210);江苏省自然科学基金资助项目 (No.BK2009302);天津市应用基础及前沿技术研究计划资助项目(No.JCZDJC21400)

Synthesis and antitumor activity of novel oleanolic acid-nitrate conjugates

摘要: 以齐墩果酸为先导物，将其3位OH通过各种类型的连接基团与硝酸酯类NO供体偶联，合成了10个目标化合物（ 2,4,8a～8c,10,12,15a～15c ）。结构均经IR，MS及¹H NMR确证，并采用MTT法测定了偶联物的细胞毒性。结果显示，化合物 8c 对人肺癌细胞A549、人结肠癌细胞HT-29及人肝癌细胞SMMC-7721均具有较强的抗肿瘤活性，值得进一步研究。
- 齐墩果酸 /
- 硝酸酯 /
- 抗肿瘤活性 /
- NO /
- 合成
Abstract: A series of novel oleanolic acid-nitrate conjugates were synthesized by coupling nitrate with 3-OH of OA via various linkers, and their structures were determined by IR,MS and ¹H NMR. The cytotoxicity of the synthetic derivatives against human cancer cells SMMC-7721,BEL-7402,A549 and HT-29 was evaluated by MTT assay. Preliminary experimental results showed that compound 8c was the most potent one, whose cytotoxicity against A549,HT-29 and SMMC-7721 was stronger than that of the positive control adriamycin. Compound 8c is a promising compound worthy of further study.
- oleanolic acid /
- nitrate /
- antitumor activity /
- NO /
- synthesis