Metabolism of eupatilin in rats using liquid chromatography/electrospray mass spectrometry.
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.
Ji
Hye Young
HY
Drug Metabolism and Bioanalysis Laboratory, College of Pharmacy and Medicinal Resources Research Center, Wonkwang University, Iksan 570-749, Korea.
Lee
Hye Won
HW
Shim
Hyun Joo
HJ
Kim
Soon Hoe
SH
Kim
Won Bae
WB
Lee
Hye Suk
HS
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*
D004365:Drugs, Chinese Herbal; D005419:Flavonoids; C045325:eupatilin