title: Metabolism of eupatilin in rats using liquid chromatography/electrospray mass spectrometry.
abstract: Eupatilin (5,7-dihydroxy-3',4',6-trimethoxy flavone) is an active ingredient of an ethanol extract of Artemisia asiatica (DA-9601) that is used in the treatment of gastritis. In vitro and in vivo metabolism of eupatilin in the rats has been studied by LC-electrospray mass spectrometry. Rat liver microsomal incubation of eupatilin in the presence of NADPH and UDPGA resulted in the formation of four metabolites (M1-M4). M1, M2, M3 and M4 were tentatively identified as 3'- or 4'-O-demethyl-eupatilin glucuronide, eupatilin glucuronide, 6-O-demethyleupatilin and 3'- or 4'-O-demethyl-eupatilin, respectively. Those metabolites from in vitro study were also characterized in bile, plasma or urine samples after an intravenous administration of eupatilin to rats. In rat bile, plasma and urine samples, eupatilin glucuronide (M2) was a major metabolite, whereas M3, M4 and M4 glucuronide (M1) were the minor metabolites.
authors.affiliation: Drug Metabolism and Bioanalysis Laboratory, College of Pharmacy and Medicinal Resources Research Center, Wonkwang University, Iksan 570-749, Korea.
authors.forename: Hye Young
authors.initials: HY
authors.lastname: Ji
authors.forename: Hye Won
authors.initials: HW
authors.lastname: Lee
authors.forename: Hyun Joo
authors.initials: HJ
authors.lastname: Shim
authors.forename: Soon Hoe
authors.initials: SH
authors.lastname: Kim
authors.forename: Won Bae
authors.initials: WB
authors.lastname: Kim
authors.forename: Hye Suk
authors.initials: HS
authors.lastname: Lee
mesh_terms: D000818:Animals; D002853:Chromatography, Liquid / Q000379:methods*; D004365:Drugs, Chinese Herbal; D005419:Flavonoids / Q000378:metabolism*; D008297:Male; D008862:Microsomes, Liver / Q000378:metabolism; D051381:Rats; D021241:Spectrometry, Mass, Electrospray Ionization / Q000379:methods*
chemical_list: D004365:Drugs, Chinese Herbal; D005419:Flavonoids; C045325:eupatilin