title: Intestinal absorption and first-pass metabolism of polyphenol compounds in rat and their transport dynamics in Caco-2 cells.
abstract: 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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Fourth Military Medical University, Xi'an, People's Republic of China.
authors.forename: Zenghui
authors.initials: Z
authors.lastname: Teng
authors.forename: Chengjun
authors.initials: C
authors.lastname: Yuan
authors.forename: Feng
authors.initials: F
authors.lastname: Zhang
authors.forename: Menglei
authors.initials: M
authors.lastname: Huan
authors.forename: Weidong
authors.initials: W
authors.lastname: Cao
authors.forename: Kangchu
authors.initials: K
authors.lastname: Li
authors.forename: Jingyue
authors.initials: J
authors.lastname: Yang
authors.forename: Dayong
authors.initials: D
authors.lastname: Cao
authors.forename: Siyuan
authors.initials: S
authors.lastname: Zhou
authors.forename: Qibing
authors.initials: Q
authors.lastname: Mei
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001692:Biological Transport; D018938:Caco-2 Cells; D002463:Cell Membrane Permeability; D006801:Humans; D007408:Intestinal Absorption; D007421:Intestine, Small / Q000378:metabolism; D008297:Male; D059808:Polyphenols / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism* / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D013997:Time Factors
chemical_list: D059808:Polyphenols