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  • Title: Transport mechanisms of flavanone aglycones across Caco-2 cell monolayers and artificial PAMPA membranes.
    Author: Kobayashi S, Nagai T, Konishi Y, Tanabe S, Morimoto K, Ogihara T.
    Journal: J Pharm Pharmacol; 2012 Jan; 64(1):52-60. PubMed ID: 22150672.
    Abstract:
    OBJECTIVES: We recently reported that flavanone aglycones (hesperetin, naringenin and eriodictyol) are efficiently absorbed via proton-coupled active transport, in addition to transcellular passive diffusion, in Caco-2 cells. Here, we aimed to evaluate in detail the absorption mechanisms of these flavanones, as well as homoeriodictyol and sakuranetin. METHODS: We evaluated the absorption mechanisms of the above compounds by means of in vitro studies in Caco-2 cells in parallel with an artificial membrane permeation assay (PAMPA) under pH-gradient and iso-pH conditions. KEY FINDINGS: Comparison of the permeability characteristics of flavanones in Caco-2 cells and in PAMPA under these conditions, as well as a consideration of the physicochemical properties, indicated that hesperetin, naringenin, eriodictyol and homoeriodictyol were efficiently transported by passive diffusion according to the pH-partition hypothesis, except in the case of sakuranetin. However, transport of all flavanones were remarkably temperature-dependent, and was significantly reduced when Caco-2 cells were treated with amino acid-modifying reagents. CONCLUSIONS: Our data confirm that both passive diffusion and an active transport mechanism contribute to flavanone absorption through human intestinal epithelium.
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