目的 基于药用植物露兜簕Pandanus tectorius中的单体咖啡酰奎宁酸类天然产物3-O-咖啡酰奎宁酸进行结构修饰,并对其结构修饰物进行体外抗流感病毒生物活性研究.方法 以3-O-咖啡酰奎宁酸为原料,通过3条反应路线分别制得目标化合物,利用流感病毒体外感染MDCK细胞模型评价该类衍生物的抗病毒活性.结果 设计并合成13个3-O-咖啡酰奎宁酸类衍生物B1～B13,均经波谱技术确证结构.药理实验结果表明,衍生物B4、B6和B10具有不同程度抑制流感病毒在细胞中复制的活性.结论 化合物B2、B4～B13为未见文献报道的咖啡酰奎宁酸类新化合物,B4具有潜在的抗流感病毒生物活性,值得进一步深入研究.

Objective To modify the structure of natural monomeric compound 3-O-caffeoylquinic acid from medicinal plant Pandanus tectorius, and evaluate the anti-influenza virus activity of the derivatives. Methods Applying 3-O-caffeoylquinic acid as material, the target compounds were prepared by three routes and evaluated for their anti-influenza virus effects by MDCK cells in vitro. Results Thirteen caffeoylquinic acid derivatives B1—B13 were synthesized. The structures of the target compounds were identified by spectrum. Pharmacological results showed that the compounds B4, B6, and B10 had the different potencial inhibition on the replication of influenza virus in cells. Conclusion The new compounds B2 and B4—B13 which show the potential biological activity of anti-influenza virus, have not been reported in any literatures and are worth studying further.

国家自然科学基金资助项目(81302656)