The role of sodium-dependent glucose transporter 1 and glucose transporter 2 in the absorption of cyanidin-3-o-β-glucoside in Caco-2 cells

Anthocyanins have multiple biological activities of benefit to human health. While a few studies have been conducted to evaluate the bioavailability of anthocyanins, the mechanisms of their absorption mechanism remain ill-defined. In the present study, we investigated the absorption mechanism of cya...

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Published in:Nutrients 2014-10, Vol.6 (10), p.4165-4177
Main Authors: Zou, Tang-Bin, Feng, Dan, Song, Gang, Li, Hua-Wen, Tang, Huan-Wen, Ling, Wen-Hua
Format: Article
Language:English
Subjects:
absorption
Anthocyanins - pharmacokinetics
Caco-2 Cells
Cell Line
Cy-3-G
Epithelial Cells - drug effects
Epithelial Cells - metabolism
Glucosides - pharmacokinetics
GLUT2
Humans
Intestinal Absorption - drug effects
Intestinal Mucosa - cytology
Phloretin - pharmacology
Phlorhizin - pharmacology
RNA, Small Interfering - drug effects
SGLT1
siRNA
Sodium-Glucose Transporter 1 - metabolism
Sodium-Glucose Transporter 2 - metabolism
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Summary:Anthocyanins have multiple biological activities of benefit to human health. While a few studies have been conducted to evaluate the bioavailability of anthocyanins, the mechanisms of their absorption mechanism remain ill-defined. In the present study, we investigated the absorption mechanism of cyanidin-3-O-β-glucoside (Cy-3-G) in human intestinal epithelial (Caco-2) cells. Cy-3-G transport was assessed by measuring the absorptive and efflux direction. Inhibition studies were conducted using the pharmacological agents, phloridzin, an inhibitor of sodium-dependent glucose transporter 1 (SGLT1), or phloretin, an inhibitor of glucose transporter 2 (GLUT2). The results showed that phloridzin and phloretin significantly inhibited the absorption of Cy-3-G. In addition, Caco-2 cells transfected with small interfering RNA (siRNA) specific for SGLT1 or GLUT2 showed significantly decreased Cy-3-G absorption. These siRNA transfected cells also showed a significantly decreased rate of transport of Cy-3-G compared with the control group. These findings suggest that Cy-3-G absorption is dependent on the activities of SGLT1 and GLUT2 in the small intestine and that SGLT1 and GLUT2 could be a limiting step for the bioavailability of Cy-3-G.
ISSN:2072-6643
2072-6643
DOI:10.3390/nu6104165