title: Characterization of the intestinal absorption of seven flavonoids from the flowers of Trollius chinensis using the Caco-2 cell monolayer model.
abstract: The human Caco-2 cell monolayer model was used to investigate the absorption property, mechanism, and structure-property relationship of seven representative flavonoids, namely, orientin, vitexin, 2"-O-β-L-galactopyranosylorientin, 2"-O-β-L-galactopyranosylvitexin, isoswertisin, isoswertiajaponin, and 2"-O-(2"'-methylbutanoyl)isoswertisin from the flowers of Trollius chinensis. The results showed that these flavonoids were hardly transported through the Caco-2 cell monolayer. The compounds with 7-OCH3 including isoswertisin, isoswertiajaponin and 2"-O-(2"'-methylbutanoyl)isoswertisin were absorbed in a passive diffusion manner, and their absorbability was increased in the same order as their polarity. The absorption of the remaining compounds with 7-OH including orientin, vitexin, 2"-O-β-L-galactopyranosylorientin, and 2"-O-β-L-galactopyranosylvitexin involved transporter mediated efflux in addition to passive diffusion. Among the four compounds with 7-OH, those with a free hydroxyl group at C-2" such as orientin and vitexin were the substrates of P-glycoprotein (P-gp) and that with a free hydroxyl group at C-2' such as 2"-O-β-L-galactopyranosylorientin was the substrate of multidrug resistance protein 2 (MRP2). The results of this study also implied that the absorbability of the flavonoids should be taken into account when estimating the effective components of T. chinensis.
authors: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, China.
authors: Lijia
authors: L
authors: Liu
authors: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, China.
authors: Lina
authors: L
authors: Guo
authors: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, China.
authors: Can
authors: C
authors: Zhao
authors: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, China.
authors: Xiuwen
authors: X
authors: Wu
authors: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, China.
authors: Rufeng
authors: R
authors: Wang
authors: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, China.
authors: Chen
authors: C
authors: Liu
mesh_terms: D047310:Apigenin / Q000008:administration & dosage; D018938:Caco-2 Cells; D005419:Flavonoids / Q000008:administration & dosage* / Q000737:chemistry; D035264:Flowers / Q000737:chemistry / Q000378:metabolism; D005960:Glucosides / Q000008:administration & dosage; D006027:Glycosides / Q000008:administration & dosage; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects*; D029626:Ranunculaceae / Q000737:chemistry
chemical_list: D005419:Flavonoids; D005960:Glucosides; D006027:Glycosides; C090074:isoswertiajaponin 2''-O-arabinopyranoside; D047310:Apigenin; C032731:vitexin; C065886:orientin