title: Identification of acteoside and its major metabolites in rat urine by ultra-performance liquid chromatography combined with electrospray ionization quadrupole time-of-flight tandem mass spectrometry.
abstract: In this study, metabolites in the urine samples of rats orally administered with acteoside, a phenylethanoid glycoside compound, were detected and identified using ultra-performance liquid chromatography coupled with electrospray ionization quadrupole time-of-flight tandem mass spectrometry (UPLC/ESI-QTOF-MS) combined with an automated MS(E) technique. Up to 35 metabolites (19 metabolites of the parent drug and 16 metabolites of the degradation products) were observed, including processes of oxidization, glucuronidation, sulfation, and methyl conjugation. According to the metabolic pathways, acteoside mainly functioned as a prodrug and underwent hydrolysis before being absorbed into the blood. The degradation products, especially caffeic acid and hydroxytyrosol, were involved in further metabolism which was responsible for the low oral bioavailability but obvious pharmacological activities of acteoside. In summary, this work provided valuable information on acteoside metabolism through the rapid and reliable UPLC/ESI-QTOF-MS technique, which could be widely used for the investigation of natural product metabolites.
authors.affiliation: The MOE Key Laboratory for Standardization of Chinese Medicines and the SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines, Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, China.
authors.forename: Meng
authors.initials: M
authors.lastname: Qi
authors.forename: Aizhen
authors.initials: A
authors.lastname: Xiong
authors.forename: Pengfei
authors.initials: P
authors.lastname: Li
authors.forename: Qiming
authors.initials: Q
authors.lastname: Yang
authors.forename: Li
authors.initials: L
authors.lastname: Yang
authors.forename: Zhengtao
authors.initials: Z
authors.lastname: Wang
mesh_terms: D000818:Animals; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D005960:Glucosides / Q000737:chemistry / Q000378:metabolism / Q000652:urine*; D008297:Male; D008958:Models, Molecular; D010636:Phenols / Q000737:chemistry / Q000378:metabolism / Q000652:urine*; D051381:Rats; D017207:Rats, Sprague-Dawley; D021241:Spectrometry, Mass, Electrospray Ionization / Q000379:methods; D053719:Tandem Mass Spectrometry / Q000379:methods*; D059808:Polyphenols
chemical_list: D005960:Glucosides; D010636:Phenols; C058956:acteoside; D059808:Polyphenols
keywords: Acteoside; MS(E) technique; Metabolite identification; Prodrug; UPLC/ESI-QTOF-MS