目的 設(shè)計合成綠原酸的酰胺二聚體衍生物,并對其進(jìn)行體外抗脂質(zhì)代謝紊亂活性的研究。方法 以綠原酸為起始原料經(jīng)3步反應(yīng)制得目標(biāo)化合物,利用HepG2細(xì)胞株評價該類化合物的調(diào)血脂活性。結(jié)果 設(shè)計并合成8個綠原酸酰胺二聚體衍生物CGA-2a～2d及CGA-3a～3d,均經(jīng)波譜技術(shù)確證結(jié)構(gòu)。藥理實驗結(jié)果表明,衍生物CGA-2d和CGA-3a～3d具有不同程度的調(diào)血脂活性。結(jié)論 綠原酸二聚體化合物CGA-2a～2d及CGA-3a～3d均為未見文獻(xiàn)報道的新化合物,部分化合物具有潛在的調(diào)脂生物活性,具有深入研究價值。

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.

國家自然科學(xué)基金資助項目(81302656)