Synthesis of caffeic acid ester derivatives and their bioactivities / 中草药

ABSTRACT

Objective: To design and synthetise the natural products caffeic acid ester derivatives, and to study the lipid metabolic disturbance regulation activity of the derivatives. Methods: Applying caffeic acid as material, the target compounds were prepared by two routes and evaluated for antihyperlipidemic effects in HepG2 cells. Results: Ten caffeic acid ester derivatives were synthesized, and compound C5 has not yet been reported. The structures of the target compounds were identified by spectrum. Pharmacological results showed that eight derivatives had potency of lipid-regulating in different levels. In particular, compounds C3 and C5 showed significant lipid-regulating effects compared to the lead compound caffeic acid and positive drug Simvastatin. Conclusion: Compound C5 is a new caffeic acid ester derivative. The primary structure-activity relationships are discussed in this article.