title: New analytical method for the study of the metabolism of gentiopicroside in rats after oral administration by LC-TOF-MS following picolinoyl derivatization.
abstract: The metabolism of gentiopicroside (GPS) in vivo was studied for the first time by LC-MS following picolinoyl derivatization. Incubation of erythrocentaurin, one of the main in vitro metabolites of GPS by intestinal bacteria, with liver microsome indicated that GPS might be metabolized to a final metabolite 3,4-dihydro-5-(hydroxymethyl)isochroman-1-one (HMIO) in vivo. After hydrolysis with sulfatase, HMIO was successfully detected in rat plasma after oral administration of GPS by LC-MS following picolinoyl derivatization. 4-Methoxyphenyl methanol was used as an internal standard to quantify HMIO in rat plasma. A metabolic pathway of GPS in rats is proposed. The monoterpene compound GPS was found to be metabolized to dihydroisocoumarin, which may be responsible for the pharmacological effect of GPS.
authors.affiliation: National TCM Key Lab of Serum Pharmacochemistry, Department of Pharmaceutical Analysis, Heilongjiang University of Chinese Medicine, Harbin, China; Institute of Natural Medicine, University of Toyama, Toyama, Japan.
authors.forename: Zhigang
authors.initials: Z
authors.lastname: Wang
authors.forename: Shanshan
authors.initials: S
authors.lastname: Wang
authors.forename: Yujia
authors.initials: Y
authors.lastname: Sun
authors.forename: Huiyu
authors.initials: H
authors.lastname: Wang
authors.forename: Guang
authors.initials: G
authors.lastname: Chen
authors.forename: Xijun
authors.initials: X
authors.lastname: Wang
authors.forename: Masao
authors.initials: M
authors.lastname: Hattori
authors.forename: Hailong
authors.initials: H
authors.lastname: Zhang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D005260:Female; D057888:Iridoid Glucosides / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism*; D008297:Male; D013058:Mass Spectrometry / Q000379:methods*; D008862:Microsomes, Liver / Q000737:chemistry / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar
chemical_list: D057888:Iridoid Glucosides; C012997:gentiopicroside
keywords: Derivatization; Gentiopicroside; Iridoid compounds; Metabolism