Synthesis and In Vitro Evaluation of Caffeoylquinic Acid Derivatives as Potential Hypolipidemic Agents
Beijing Key Laboratory of Innovative Drug Discovery of Traditional Chinese Medicine (Natural Medicine) and Translational Medicine; Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Ministry of Education; Key Laboratory of Efficacy Evaluation of Chinese Medicine against Glycolipid Metabolic Disorders, State Administration of Traditional Chinese Medicine; Zhong Guan Cun Open Laboratory of the Research and Development of Natural Medicine and Health Products; Key Laboratory of New Drug Discovery Based on Classic Chinese Medicine Prescription; Key Laboratory of New Drug Discovery Based on Classic Chinese Academy of Medical Sciences; Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100193, China
Center of Research and Development on Life Sciences and Environment Sciences, Harbin University of Commerce, Harbin 150076, China
School of Pharmacy, Hainan Medical University, Haikou 571199, China
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editors: Pavel B. Drasar and Vladimir A. Khripach
Received: 14 January 2019 / Revised: 28 February 2019 / Accepted: 5 March 2019 / Published: 9 March 2019
A series of novel caffeoylquinic acid derivatives of chlorogenic acid have been designed and synthesized. Biological evaluation indicated that several synthesized derivatives exhibited moderate to good lipid-lowering effects on oleic acid-elicited lipid accumulation in HepG2 liver cells. Particularly, derivatives 3d
exhibited more potential lipid-lowering effect than the positive control simvastatin and chlorogenic acid. Further studies on the mechanism of 3d
revealed that the lipid-lowering effects were related to their regulation of TG levels and merit further investigation.
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MDPI and ACS Style
Tian, Y.; Cao, X.-X.; Shang, H.; Wu, C.-M.; Zhang, X.; Guo, P.; Zhang, X.-P.; Xu, X.-D. Synthesis and In Vitro Evaluation of Caffeoylquinic Acid Derivatives as Potential Hypolipidemic Agents. Molecules 2019, 24, 964.
Tian Y, Cao X-X, Shang H, Wu C-M, Zhang X, Guo P, Zhang X-P, Xu X-D. Synthesis and In Vitro Evaluation of Caffeoylquinic Acid Derivatives as Potential Hypolipidemic Agents. Molecules. 2019; 24(5):964.
Tian, Yu; Cao, Xiao-Xue; Shang, Hai; Wu, Chong-Ming; Zhang, Xi; Guo, Peng; Zhang, Xiao-Po; Xu, Xu-Dong. 2019. "Synthesis and In Vitro Evaluation of Caffeoylquinic Acid Derivatives as Potential Hypolipidemic Agents." Molecules 24, no. 5: 964.
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