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Molecules 2017, 22(4), 554;

Intestinal Transport Characteristics and Metabolism of C-Glucosyl Dihydrochalcone, Aspalathin

Biomedical Research and Innovation Platform, South African Medical Research Council, Tygerberg, Cape Town 7130, South Africa
Plant Bioactives Group, Post-Harvest and Wine Technology Division, Agricultural Research Council, Infruitec-Nietvoorbij, Stellenbosch 7600, South Africa
Department of Food Science, Stellenbosch University, Stellenbosch 7600, South Africa
Department of Biochemistry and Microbiology, University of Zululand, Kwa-Dlangezwa 3886, South Africa
Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa
Drug Discovery and Development Centre (H3D), University of Cape Town, Rondebosch 7701, South Africa
Division of Clinical Pharmacology, University of Cape Town, Observatory, Cape Town 7925, South Africa
Institute of Infectious Disease and Molecular Medicine, Faculty of Health Sciences, University of Cape Town, Observatory, Cape Town 7925, South Africa
South African Medical Research Council Drug, Discovery and Development Research Unit, University of Cape Town, Rondebosch 7701, South Africa
Department of Medical Physiology, Stellenbosch University, Tygerberg 7507, South Africa
Author to whom correspondence should be addressed.
Academic Editor: Nancy D. Turner
Received: 14 March 2017 / Accepted: 27 March 2017 / Published: 30 March 2017
(This article belongs to the Collection Bioactive Compounds)
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Insight 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 × 10−6 cm/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. View Full-Text
Keywords: aspalathin; bioavailability; Caco-2; transport; metabolism aspalathin; bioavailability; Caco-2; transport; metabolism

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Bowles, S.; Joubert, E.; De Beer, D.; Louw, J.; Brunschwig, C.; Njoroge, M.; Lawrence, N.; Wiesner, L.; Chibale, K.; Muller, C. Intestinal Transport Characteristics and Metabolism of C-Glucosyl Dihydrochalcone, Aspalathin. Molecules 2017, 22, 554.

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