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。

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 potential lipid-regulating biological activities, worthy of further development.

国家自然科学基金资助项目(81302656)