In Vivo Metabolite Profiling of a Purified Ellagitannin Isolated from Polygonum capitatum in Rats

Molecules. 2016 Aug 24;21(9):1110. doi: 10.3390/molecules21091110.

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/MS(n)-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.

Keywords: FR429; LC/MSn-IT-TOF; ellagitannin; metabolite profiling.

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic / chemistry*
  • Antineoplastic Agents, Phytogenic / pharmacokinetics*
  • Hydrolyzable Tannins / chemistry*
  • Hydrolyzable Tannins / pharmacokinetics*
  • Male
  • Mass Spectrometry
  • Polygonum / chemistry*
  • Rats
  • Rats, Sprague-Dawley

Substances

  • Antineoplastic Agents, Phytogenic
  • Hydrolyzable Tannins
  • ellagitannin