PLoS ONE (Jan 2012)

Intestinal absorption and first-pass metabolism of polyphenol compounds in rat and their transport dynamics in Caco-2 cells.

  • Zenghui Teng,
  • Chengjun Yuan,
  • Feng Zhang,
  • Menglei Huan,
  • Weidong Cao,
  • Kangchu Li,
  • Jingyue Yang,
  • Dayong Cao,
  • Siyuan Zhou,
  • Qibing Mei

DOI
https://doi.org/10.1371/journal.pone.0029647
Journal volume & issue
Vol. 7, no. 1
p. e29647

Abstract

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BACKGROUND: Polyphenols, a group of complex naturally occurring compounds, are widely distributed throughout the plant kingdom and are therefore readily consumed by humans. The relationship between their chemical structure and intestinal absorption, transport, and first-pass metabolism remains unresolved, however. METHODS: Here, we investigated the intestinal absorption and first-pass metabolism of four polyphenol compounds, apigenin, resveratrol, emodin and chrysophanol, using the in vitro Caco-2 cell monolayer model system and in situ intestinal perfusion and in vivo pharmacokinetic studies in rats, so as to better understand the relationship between the chemical structure and biological fate of the dietary polyphenols. CONCLUSION: After oral administration, emodin and chrysophanol exhibited different absorptive and metabolic behaviours compared to apigenin and resveratrol. The differences in their chemical structures presumably resulted in differing affinities for drug-metabolizing enzymes, such as glucuronidase and sulphatase, and transporters, such as MRP2, SGLT1, and P-glycoprotein, which are found in intestinal epithelial cells.