绿原酸酰胺二聚体的合成及体外抗脂质代谢紊乱活性研究.PDFVIP

现代药物与临床 Drugs Clinic 第 30 卷 第 5 期 2015 年 5 月 ·487 · 绿原酸酰胺二聚体的合成及体外抗脂质代谢紊乱活性研究 1 2 1 1 1 1* 田 瑜 ，王文倩 ，李永胜 ，王 丹 ，郭 鹏 ，许旭东 1. 中国医学科学院 北京协和医学院 药用植物研究所，北京 100193 2. 天津药物研究院，天津 300193 摘 要：目的 设计合成绿原酸的酰胺二聚体衍生物，并对其进行体外抗脂质代谢紊乱活性的研究。方法 以绿原酸为起始 原料经 3 步反应制得目标化合物，利用 HepG2 细胞株评价该类化合物的调血脂活性。结果 设计并合成 8 个绿原酸酰胺二 聚体衍生物 CGA-2a～2d 及 CGA-3a～3d，均经波谱技术确证结构。药理实验结果表明，衍生物 CGA-2d 和 CGA-3a～3d 具 有不同程度的调血脂活性。结论 绿原酸二聚体化合物 CGA-2a～2d 及 CGA-3a～3d 均为未见文献报道的新化合物，部分化 合物具有潜在的调脂生物活性，具有深入研究价值。 关键词：绿原酸；酰胺二聚体；调脂 中图分类号：R284.3 ；R285.5 文献标志码：A 文章编号：1674 - 5515(2015)05 - 0487 - 05 DOI: 10.7501/j.issn.1674-5515.2015.05.003 Synthesis of chlorogenic acid amide dimers and their anti-lipid metabolic disorder activities in vitro 1 2 1 1 1 1 TIAN Yu , WANG Wen-qian , LI Yong-sheng , WANG Dan , GUO Peng , XU Xu-dong 1. Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, China 2. Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China Abstract: Objective To design and synthesize the derivatives of chlorogenic acid amide dimers, and to study anti-lipid metabolic disorder activities in vitro. Methods Chlorogenic acid was used as starting material to synthesize the target compounds by three steps. The lipid-regulating activities of the compounds were tested by HepG2 cells. Results Eight chlorogenic acid dimers CGA-2a ～2d and CGA-3a ～ 3d were synthesized. The structures of the target compounds were identified by spectrum. Pharmacological results showed that compounds CGA-2d and CGA-3a～3d had different levels potency of lipid-regulating effects in cells. Conclusion The dimers CGA-2a～2d and CGA-3a～3d are new compounds, some of which have potent