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Molecules 2019, 24(5), 964; https://doi.org/10.3390/molecules24050964

Synthesis and In Vitro Evaluation of Caffeoylquinic Acid Derivatives as Potential Hypolipidemic Agents

1
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
2
Center of Research and Development on Life Sciences and Environment Sciences, Harbin University of Commerce, Harbin 150076, China
3
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
(This article belongs to the Special Issue Synthesis, Study and Utilization of Natural Products)
Full-Text   |   PDF [2509 KB, uploaded 9 March 2019]   |  

Abstract

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, 3g, 4c and 4d exhibited more potential lipid-lowering effect than the positive control simvastatin and chlorogenic acid. Further studies on the mechanism of 3d, 3g, 4c and 4d revealed that the lipid-lowering effects were related to their regulation of TG levels and merit further investigation. View Full-Text
Keywords: caffeoylquinic acids; chlorogenic acid; derivatives; lipid-lowering effects; oleic acid-elicited; HepG2 cells caffeoylquinic acids; chlorogenic acid; derivatives; lipid-lowering effects; oleic acid-elicited; HepG2 cells
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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.

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