title: Metabolism of chicoric acid by rat liver microsomes and bioactivity comparisons of chicoric acid and its metabolites.
abstract: Chicoric acid has recently become a hot research topic due to its potent bioactivities. However, there are few studies relevant to this acid's pharmacokinetic characteristics and the pharmacological activities of its metabolites. To compare the abilities of chicoric acid and its metabolites in scavenging free radicals and their effects on the viability of 3T3-L1 preadipocytes, an in vitro study of the metabolism of chicoric acid in rat liver microsomes was performed using liquid tandem mass spectrometry (HPLC-MS/MS). The results indicated that caffeic acid and caftaric acid were the hepatic phase I metabolites of chicoric acid. These three compounds had strong capacities for scavenging free radicals and had been demonstrated to increase intracellular ROS levels in 3T3-L1 preadipocytes, thereby reducing cell vitality. Finally, the pharmacological activities of chicoric acid were significantly stronger than those of its metabolites within a certain concentration range.
authors.affiliation: College of Food Science and Engineering, Northwest A&F University, Yangling 712100, China. xueboliu@aliyun.com xueboliu@nwsuaf.edu.cn.
authors.forename: Qian
authors.initials: Q
authors.lastname: Liu
authors.forename: Yutang
authors.initials: Y
authors.lastname: Wang
authors.forename: ChunXia
authors.initials: C
authors.lastname: Xiao
authors.forename: Wanqiang
authors.initials: W
authors.lastname: Wu
authors.forename: Xuebo
authors.initials: X
authors.lastname: Liu
mesh_terms: D041721:3T3-L1 Cells; D017667:Adipocytes / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D000818:Animals; D019440:Anti-Obesity Agents / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D000975:Antioxidants / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D002109:Caffeic Acids / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D002851:Chromatography, High Pressure Liquid; D016166:Free Radical Scavengers / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D007700:Kinetics; D050216:Metabolic Detoxication, Phase I; D051379:Mice; D008862:Microsomes, Liver / Q000187:drug effects / Q000378:metabolism*; D015394:Molecular Structure; D010636:Phenols / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D051381:Rats; D017382:Reactive Oxygen Species / Q000819:agonists / Q000378:metabolism; D021241:Spectrometry, Mass, Electrospray Ionization; D013386:Succinates / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D053719:Tandem Mass Spectrometry
chemical_list: D019440:Anti-Obesity Agents; D000975:Antioxidants; D002109:Caffeic Acids; D016166:Free Radical Scavengers; D010636:Phenols; D017382:Reactive Oxygen Species; D013386:Succinates; C100435:chicoric acid; C040048:caffeic acid; C515101:caftaric acid