Synthesis and lipid-regulating evaluation of caffeic acid amide derivatives / 中草药

ABSTRACT

Objective To evaluate the anti-lipid metabolic disorder activities of these compounds in vitro, the natural caffeic acid amide derivatives were designed and synthesized. Methods Using caffeic acid as start material, BOP as a condensing agent, and the target compounds were sequentially prepared with fourteen amines, and then the lipid-regulating effect was evaluated using HepG2 cells. Results Fourteen caffeic acid amide compounds CA1-CA14 were synthesized. The structures of the target compounds were identified by spectrum. Pharmacological results showed that fourteen derivatives have potency of lipid-regulating in different levels. In particular, compound CA6 showed significant lipid-regulating effects compared to the lead compounds caffeic acid and Simvastatin. Conclusion Compound CA6, CA7, and CA11 had not been reported in any literatures before. Among them, the novel compounds CA6 and CA11 have showed potential of lipid-regulating activities, and deserved further research.