Next Article in Journal
Chemical Synthesis and Characterization of an Equinatoxin II(1–85) Analogue
Next Article in Special Issue
Phenolic Compounds from the Rhizomes of Smilax china L. and Their Anti-Inflammatory Activity
Previous Article in Journal
Zerumbone Alleviates Neuropathic Pain through the Involvement of l-Arginine-Nitric Oxide-cGMP-K+ ATP Channel Pathways in Chronic Constriction Injury in Mice Model
Previous Article in Special Issue
Assessment of Lipophilicity Indices Derived from Retention Behavior of Antioxidant Compounds in RP-HPLC
Article Menu
Issue 4 (April) cover image

Export Article

Open AccessArticle
Molecules 2017, 22(4), 554; doi:10.3390/molecules22040554

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

1
Biomedical Research and Innovation Platform, South African Medical Research Council, Tygerberg, Cape Town 7130, South Africa
2
Plant Bioactives Group, Post-Harvest and Wine Technology Division, Agricultural Research Council, Infruitec-Nietvoorbij, Stellenbosch 7600, South Africa
3
Department of Food Science, Stellenbosch University, Stellenbosch 7600, South Africa
4
Department of Biochemistry and Microbiology, University of Zululand, Kwa-Dlangezwa 3886, South Africa
5
Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa
6
Drug Discovery and Development Centre (H3D), University of Cape Town, Rondebosch 7701, South Africa
7
Division of Clinical Pharmacology, University of Cape Town, Observatory, Cape Town 7925, South Africa
8
Institute of Infectious Disease and Molecular Medicine, Faculty of Health Sciences, University of Cape Town, Observatory, Cape Town 7925, South Africa
9
South African Medical Research Council Drug, Discovery and Development Research Unit, University of Cape Town, Rondebosch 7701, South Africa
10
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)
View Full-Text   |   Download PDF [842 KB, uploaded 30 March 2017]   |  

Abstract

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
Figures

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).

Supplementary material

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

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.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top