title: Metabolite profiles of icariin in rat plasma by ultra-fast liquid chromatography coupled to triple-quadrupole/time-of-flight mass spectrometry.
abstract: In this work, the metabolite profiles of icariin in rat plasma were qualitatively investigated, and the possible metabolic pathways of icariin were subsequently proposed. After oral administration of icariin, rat plasma samples were collected and pretreated by protein precipitation. Then these pretreated samples were injected into a Venusil ASB-C18 column with mobile phase consisted of 0.1% formic acid water and 0.1% formic acid acetonitrile and detected by Ultra fast liquid chromatography coupled to time-of-flight mass spectrometry (UFLC-TOF/MS). A total of 19 metabolites, namely, icariside I (M1), icaritin (M2), desmethylicaritin and its isomer (M3-M6), icaritin-3-O-gluA (M7), icaritin-7-O-gluA (M8), icariside II and its isomer (M9 and M10), icaritin-3,7-di-O-gluA (M11), 1,3-isoprene alcohol icaritin and its isomer (M12, M13 and M18), 1,3-isoprene alcohol icariside II (M14), allylic alcohol icaritin and its isomer (M15 and M16), 1,3-isoprene icariside II (M17) and icaritin-3-O-rha-7-O-gluA (M19) were detected and tentatively identified, and 9 of them, including M7 and M8 and M12-M18 were reported for the first time. The metabolites profiles in plasma revealed that glucuronide conjugates of isoflavonoids and flavonoid aglycones were the major circulating forms of icariin.
authors.affiliation: Key Laboratory of New Drug Delivery System of Chinese Meteria Medica, Jiangsu Provincial Academy of Chinese Medicine, 100 Shizi Road, Nanjing 210028, Jiangsu Province, China.
authors.forename: Qian
authors.initials: Q
authors.lastname: Qian
authors.forename: Song-Lin
authors.initials: SL
authors.lastname: Li
authors.forename: E
authors.initials: E
authors.lastname: Sun
authors.forename: Ke-Rong
authors.initials: KR
authors.lastname: Zhang
authors.forename: Xiao-Bin
authors.initials: XB
authors.lastname: Tan
authors.forename: Ying-Jie
authors.initials: YJ
authors.lastname: Wei
authors.forename: Hong-Wei
authors.initials: HW
authors.lastname: Fan
authors.forename: Li
authors.initials: L
authors.lastname: Cui
authors.forename: Xiao-Bin
authors.initials: XB
authors.lastname: Jia
mesh_terms: D000284:Administration, Oral; D000818:Animals; D011232:Chemical Precipitation; D002853:Chromatography, Liquid / Q000379:methods*; D005419:Flavonoids / Q000008:administration & dosage / Q000378:metabolism / Q000493:pharmacokinetics*; D020719:Glucuronides; D008297:Male; D013058:Mass Spectrometry / Q000379:methods*; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D005419:Flavonoids; D020719:Glucuronides; C056599:icariin