Abstract
Ellagitannin is a common compound in food and herbs, but there are few detailed studies on the metabolism of purified ellagitannins. FR429 is a purified ellagitannin with antitumor potential, which is from Polygonum capitatum Buch.-Ham.ex D. Don. The present study was designed to investigate the metabolic profiles of FR429 in rats in vivo. Using liquid chromatography coupled to ion trap time-of-flight mass spectrometry (LC/MSn-IT-TOF), total eight metabolites were found in rat bile and urine after intravenous administration of FR429, but could not be detected in plasma. These metabolites were ellagic acid, mono-methylated FR429, ellagic acid methyl ether glucuronide, ellagic acid methyl ether diglucuronide, ellagic acid dimethyl ether glucuronide, and ellagic acid dimethyl ether diglucuronide. It was concluded that methylation and subsequent glucuronidation were the major metabolic pathways of FR429 in rats in vivo. This is the first report on the in vivo metabolism of the purified ellagitannin in rats.
Highlights
Ellagitannins (ETs) are the hydrolyzable tannins enriched in fruits and herbs
The fragmentation pattern (Figure 2A) and retention time were the same as those of EA authentic those of EA authentic standard, which confirms that M1 was ellagic acid
Glucuronide (M4), EA dimethyl ether glucuronide and dimethyl diglucuronide (M7), derivatives, as metabolites of FR429, are believed(M5 to be excreted through the ether kidneys into the urine
Summary
Ellagitannins (ETs) are the hydrolyzable tannins enriched in fruits and herbs (especially berries and nuts). Previous studies mainly focused on the pharmacokinetics and metabolism of ETs after oral administration of ET-rich food or extracts since ETs are difficult to be purified. FR429 was metabolized in sulfation rat liver cytosol mainly through inhibited tumor growth in hepatoma-xenografted mice after intraperitoneal administration It is necessary to investigate the metabolic profiles of FR429 to hepatoma determine cells whether vivo antiHowever, its in vitro IC50 value was very high (>100 μM) in [12].the. It in is necessary cancer effects observed in xenografted mice are derived from its metabolites. Profiles of FR429 in plasma, bile, and urine after its intravenous administration in rats in vivo
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