Molecules (Mar 2019)
Synthesis and In Vitro Evaluation of Caffeoylquinic Acid Derivatives as Potential Hypolipidemic Agents
- Yu Tian,
- Xiao-Xue Cao,
- Hai Shang,
- Chong-Ming Wu,
- Xi Zhang,
- Peng Guo,
- Xiao-Po Zhang,
- Xu-Dong Xu
Affiliations
- Yu Tian
- 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
- Xiao-Xue Cao
- 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
- Hai Shang
- 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
- Chong-Ming Wu
- 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
- Xi Zhang
- Center of Research and Development on Life Sciences and Environment Sciences, Harbin University of Commerce, Harbin 150076, China
- Peng Guo
- 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
- Xiao-Po Zhang
- School of Pharmacy, Hainan Medical University, Haikou 571199, China
- Xu-Dong Xu
- 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
- DOI
- https://doi.org/10.3390/molecules24050964
- Journal volume & issue
-
Vol. 24,
no. 5
p. 964
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.
Keywords
- caffeoylquinic acids
- chlorogenic acid
- derivatives
- lipid-lowering effects
- oleic acid-elicited
- HepG2 cells
