RESUMO
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.
RESUMO
Hyperlipidemia is a common clinical disease. In recent years, the incidence of hyperlipidemia increased, and patients gradually increased. Hyperlipidemia easily leads to atherosclerosis, coronary heart disease and other cardiovascular and cerebrovascular diseases, and causes crisis to human health. Clinically, Western medicine treatment has a good effect, but also the existence of side effects and even toxic effects, long-term use of drug resistance and other issues. Chinese materia medica (CMM) under the guidance of traditional Chinese medicine theory, with good efficacy and side effects of small features in the clinical dialectical treatment, plays the characteristics of Chinese medicine, and has obvious advantages. In this paper, CMM monomer, single CMM, compound, and integrated traditional Chinese and Western medicine in the treatment of hyperlipidemia were reviewed, and Chinese medicine lipid-lowering development prospects and problems were analyzed.