Analysis of the pharmacokinetics and metabolism of aloe-emodin following intravenous and oral administrations in rats

Chung Ping Yu, Chi Sheng Shia, Hui Ju Lin, Yow Wen Hsieh, Shiuan Pey Lin*, Yu Chi Hou

*Corresponding author for this work

Research output: Contribution to journalJournal Article peer-review

30 Scopus citations

Abstract

Aloe-emodin, a natural polyphenolic anthraquinone, has shown various beneficial bioactivities in vitro. The aim of this study was to investigate the pharmacokinetics and metabolism of aloe-emodin. Aloe-emodin was intravenously and orally administered to rats. The concentrations of aloe-emodin and rhein, a metabolite of aloe-emodin, were determined by HPLC method prior to and after hydrolysis with β-glucuronidase and sulfatase/β-glucuronidase. The results showed that the systemic exposures of aloe-emodin and its metabolites were ranked as aloe-emodin glucuronides (G) > rhein sulfates (S) > aloe-emodin > rhein and rhein G when aloe-emodin was given intravenously. In contrast, when aloe-emodin was administered orally, the parent form of aloe-emodin was not absorbed per se, and the systemic exposures of its metabolites were ranked as aloe-emodin G > rhein G > rhein. In conclusion, the metabolites of aloe-emodin are more important than the parent form for the bioactivities in vivo.

Original languageEnglish
Pages (from-to)1641-1647
Number of pages7
JournalBiomedical Chromatography
Volume30
Issue number10
DOIs
StatePublished - 01 10 2016
Externally publishedYes

Bibliographical note

Publisher Copyright:
Copyright © 2016 John Wiley & Sons, Ltd.

Keywords

  • LC/MS/MS
  • aloe-emodin
  • metabolism
  • pharmacokinetics
  • rhein

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