ArticlePharmaceutical research2006
The efflux of flavonoids morin, isorhamnetin-3-O-rutinoside and diosmetin-7-O-beta-D-xylopyranosyl-(1-6) -beta-D-glucopyranoside in the human intestinal cell line caco-2.
Article in Pharmaceutical research, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 42 citations in OpenAlex.
- Flavonoids for gastrointestinal tract local and associated systemic effects: A review of clinical trials and future perspectives.Journal of advanced research · 2025Review
- In Vitro Prebiotic Potential ofMolecules (Basel, Switzerland) · 2025Article
- Hydrogel Delivery System ContainingPharmaceutics · 2020Article
- Encapsulation of epigallocatechin-3-gallate into albumin nanoparticles improves pharmacokinetic and bioavailability in rat model.3 Biotech · 2019Article
- Bioaccessibility, Intestinal Permeability and Plasma Stability of Isorhamnetin Glycosides from Opuntia ficus-indica (L.).International journal of molecular sciences · 2017Article
- MK571 inhibits phase-2 conjugation of flavonols by Caco-2/TC7 cells, but does not specifically inhibit their apical efflux.Biochemical pharmacology · 2015Article
- Isolation and bioactivities of the flavonoids morin and morin-3-O-β-D-glucopyranoside from Acridocarpus orientalis-A wild Arabian medicinal plant.Molecules (Basel, Switzerland) · 2014Article
- The protective effect of diosmin on hepatic ischemia reperfusion injury: an experimental study.Bosnian journal of basic medical sciences · 2013Article
- Highly variable contents of phenolics in St. John's Wort products affect their transport in the human intestinal Caco-2 cell model: pharmaceutical and biopharmaceutical rationale for product standardization.Journal of agricultural and food chemistry · 2010Article
- Bioavailability challenges associated with development of anti-cancer phenolics.Mini reviews in medicinal chemistry · 2010Review
- Subcellular localization of flavonol aglycone in hepatocytes visualized by confocal laser scanning fluorescence microscope.Cytotechnology · 2009Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeIn this study, we chose three of the flavonoids isorhamnetin-3-O-rutinoside(IRR) diosmetin-7-O-beta-D-xylopyranosyl-(1-6)-beta-D-glucopyranoside(DXG) and morin, which showed obvious efflux, to test the hypothesis that a specific efflux transporter is responsible for their transportation.
methodsThe intestinal epithelial membrane transport of the flavonoids were examined using the monolayer of the human Caco-2 cell line grown in Transwells, a common model of intestinal absorption. The flavonoids were measured by high performance liquid chromatography with UV detector.
resultThe efflux of morin, IRR and DXG, across Caco-2 cell monolayers was examined over the concentration range from 2 to 200 microM and showed a saturable process. The depletion of the cellular ATP stores with 5 mM iodoacetamide led to a significant inhibition of the efflux. Fifty micromolar verapamil, a chemical inhibitor of P-glycoprotein, had no effect on the transport of the three flavonoids, while the presence of 50 microM MK-571 and 1 mM probenecid, MRP inhibitors, resulted in an obvious reduction in the efflux. Moreover, inhibition of morin transport by MK-571 demonstrated concentration dependence. The transportation of the three flavonoids was compared with apigenin.
conclusionThese data support a role for MRPs in the intestinal transcellular efflux of morin, IRR, DXG and possibly other hydrophilic flavonoid aglycons and glycosides.
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