Intestinal transport characteristics and metabolism of C-glucosyl dihydrochalcone, aspalathin

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dc.contributor.authorBowles, Sandraen_ZA
dc.contributor.authorJoubert, Elizabethen_ZA
dc.contributor.authorDe Beer, Daleneen_ZA
dc.contributor.authorLouw, Johanen_ZA
dc.contributor.authorBrunschwig, Christelen_ZA
dc.contributor.authorNjoroge, Mathewen_ZA
dc.contributor.authorLawrence, Ninaen_ZA
dc.contributor.authorWiesner, Lubbeen_ZA
dc.contributor.authorChibale, Kellyen_ZA
dc.contributor.authorMuller, Christoen_ZA
dc.date.accessioned2019-02-20T10:26:39Z
dc.date.available2019-02-20T10:26:39Z
dc.date.issued2017
dc.descriptionCITATION: Bowles, S., et al. 2017. Intestinal transport characteristics and metabolism of C-glucosyl dihydrochalcone, aspalathin. Molecules, 22(4):554, doi:10.3390/molecules22040554.
dc.descriptionThe original publication is available at https://www.mdpi.com
dc.description.abstractInsight into the mechanisms of intestinal transport and metabolism of aspalathin will provide important information for dose optimisation, in particular for studies using mouse models. Aspalathin transportation across the intestinal barrier (Caco-2 monolayer) tested at 1–150 µM had an apparent rate of permeability (Papp) typical of poorly absorbed compounds (1.73 × 10⁻⁶cm/s). Major glucose transporters, sodium glucose linked transporter 1 (SGLT1) and glucose transporter 2 (GLUT2), and efflux protein (P-glycoprotein, PgP) (1.84 × 10⁻⁶ cm/s; efflux ratio: 1.1) were excluded as primary transporters, since the Papp of aspalathin was not affected by the presence of specific inhibitors. The Papp of aspalathin was also not affected by constituents of aspalathin-enriched rooibos extracts, but was affected by high glucose concentration (20.5 mM), which decreased the Papp value to 2.9 × 10⁻⁷ cm/s. Aspalathin metabolites (sulphated, glucuronidated and methylated) were found in mouse urine, but not in blood, following an oral dose of 50 mg/kg body weight of the pure compound. Sulphates were the predominant metabolites. These findings suggest that aspalathin is absorbed and metabolised in mice to mostly sulphate conjugates detected in urine. Mechanistically, we showed that aspalathin is not actively transported by the glucose transporters, but presumably passes the monolayer paracellularly.en_ZA
dc.description.urihttps://www.mdpi.com/1420-3049/22/4/554
dc.description.versionPublisher's version
dc.format.extent15 page
dc.identifier.citationBowles, S., et al. 2017. Intestinal transport characteristics and metabolism of C-glucosyl dihydrochalcone, aspalathin. Molecules, 22(4):554, doi:10.3390/molecules22040554
dc.identifier.issn1420-3049 (online)
dc.identifier.otherdoi:10.3390/molecules22040554
dc.identifier.urihttp://hdl.handle.net/10019.1/105445
dc.language.isoen_ZAen_ZA
dc.publisherMDPI
dc.rights.holderAuthors retain copyright
dc.subjectBioavailabilityen_ZA
dc.subjectMetabolismen_ZA
dc.subjectAspalathinen_ZA
dc.titleIntestinal transport characteristics and metabolism of C-glucosyl dihydrochalcone, aspalathinen_ZA
dc.typeArticleen_ZA
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