title: Absorption and metabolism characteristics of rutin in Caco-2 cells.
abstract: The intestinal absorption and metabolism characteristics of the potentially beneficial polyphenol rutin were studied by measuring the intracellular accumulation and transport of rutin into Caco-2 cells with the sensitive and reliable analytical method of HPLC-coupled tandem mass spectrometry. Rutin and glucuronidated rutin were absorbed differently by the basolateral and apical membranes, and rutin showed differential permeability through the apical and basolateral sides. Approximately 33% of the rutin was metabolized to glucuronidated rutin, and the intracellular concentration of glucuronidated rutin was much lower than that of parent rutin. P-glycoprotein and multidrug-resistant proteins 2 and 3 were involved in the transmembrane transport and intracellular accumulation of rutin by Caco-2 cells. These results suggest that a specific transport system mediates rutin movement across the apical membrane in Caco-2 cells and that metabolic enzymes are important for this process.
authors.affiliation: Department of Pharmacy, Xijing Hospital, Fourth Military Medical University, Xi'an, Shaan'xi 710032, China.
authors.forename: Xiaofang
authors.initials: X
authors.lastname: Zhang
authors.forename: Jinhui
authors.initials: J
authors.lastname: Song
authors.forename: Xiaopeng
authors.initials: X
authors.lastname: Shi
authors.forename: Shan
authors.initials: S
authors.lastname: Miao
authors.forename: Yan
authors.initials: Y
authors.lastname: Li
authors.forename: Aidong
authors.initials: A
authors.lastname: Wen
mesh_terms: D018938:Caco-2 Cells; D002462:Cell Membrane / Q000378:metabolism*; D006801:Humans; D007408:Intestinal Absorption / Q000502:physiology*; D008657:Metabolic Clearance Rate; D012431:Rutin / Q000378:metabolism / Q000493:pharmacokinetics*
chemical_list: D012431:Rutin