title: The metabolic profile of acteoside produced by human or rat intestinal bacteria or intestinal enzyme in vitro employed UPLC-Q-TOF-MS.
abstract: Acteoside, the main and representative phenylethanoid glycosides of Herba Cistanches, possesses wide bioactivities but low oral bioavailability. It may serve as the prodrug and be converted into the active forms in gastrointestinal tract, which mainly occurred in intestinal tract composed of intestinal bacteria and intestinal enzyme. Intestinal bacteria, a new drug target, take a significant role on exerting pharmacological effects of drugs by oral administration. In this paper, acteoside was incubated with human or rat intestinal bacteria or rat intestinal enzyme for 36 h to seek metabolites responsible for pharmacodynamics. The samples were analyzed by ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry. Besides the parent compound, 14 metabolites were detected and identified based on their retention times and fragmentation patterns in their MS spectra including 8 degradation metabolites, 2 isomers in intestinal bacteria and intestinal enzyme samples and 4 parent metabolites only found in intestinal enzymes. The metabolic pathway of acteoside was thus proposed. Identification of these metabolites of acteoside by the intestinal bacteria or intestinal enzyme gave an insight to clarify pharmacological mechanism of traditional Chinese medicines and identify the real active molecules.
authors.affiliation: School of Traditional Chinese Medicine, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China.
authors.forename: Qingling
authors.initials: Q
authors.lastname: Cui
authors.affiliation: School of Traditional Chinese Medicine, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China. Electronic address: panyingni@163.com.
authors.forename: Yingni
authors.initials: Y
authors.lastname: Pan
authors.affiliation: School of Traditional Chinese Medicine, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China.
authors.forename: Xiaotong
authors.initials: X
authors.lastname: Xu
authors.affiliation: School of Traditional Chinese Medicine, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China.
authors.forename: Wenjie
authors.initials: W
authors.lastname: Zhang
authors.affiliation: School of Traditional Chinese Medicine, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China.
authors.forename: Xiao
authors.initials: X
authors.lastname: Wu
authors.affiliation: School of Traditional Chinese Medicine, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China.
authors.forename: Shouhe
authors.initials: S
authors.lastname: Qu
authors.affiliation: School of Traditional Chinese Medicine, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China. Electronic address: liuxiaoqiu3388@126.com.
authors.forename: Xiaoqiu
authors.initials: X
authors.lastname: Liu
mesh_terms: D000818:Animals; D001419:Bacteria / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid; D004365:Drugs, Chinese Herbal / Q000493:pharmacokinetics; D005960:Glucosides / Q000493:pharmacokinetics*; D006801:Humans; D007422:Intestines / Q000201:enzymology* / Q000382:microbiology*; D013058:Mass Spectrometry; D015394:Molecular Structure; D010636:Phenols / Q000493:pharmacokinetics*; D051381:Rats; D059808:Polyphenols
chemical_list: D004365:Drugs, Chinese Herbal; D005960:Glucosides; D010636:Phenols; C058956:acteoside; D059808:Polyphenols
keywords: Acteoside; Intestinal bacteria; Intestinal enzyme; Metabolic profile; UPLC-Q-TOF–MS