The facilitative glucose transporter, GLUT4, mediates insulin-stimulated glucose uptake in adipocytes and muscles, and the participation of GLUT4 in the pathogenesis of various clinical conditions associated with obesity, visceral fat accumulation and insulin resistance has been proposed. Glucose uptake by some members of the GLUT family, mainly GLUT1, is inhibited by flavonoids, the natural polyphenols present in fruits, vegetables and wine. Therefore it is of interest to establish if these polyphenolic compounds present in the diet, known to be effective antioxidants but also endowed with several other biological activities such as protein-tyrosine kinase inhibition, interfere with GLUT4 function. In the present study, we show that three flavonoids, quercetin, myricetin and catechin-gallate, inhibit the uptake of methylglucose by adipocytes over the concentration range of 10–100 μM. These three flavonoids show a competitive pattern of inhibition, with Ki=16, 33.5 and 90 μM respectively. In contrast, neither catechin nor gallic acid inhibit methylglucose uptake. To obtain a better understanding of the interaction among GLUT4 and flavonoids, we have derived a GLUT4 three-dimensional molecular comparative model, using structural co-ordinates from a GLUT3 comparative model and a mechanosensitive ion channel [PDB (Protein Data Bank) code 1MSL] solved by X-ray diffraction. On the whole, the experimental evidence and computer simulation data favour a transport inhibition mechanism in which flavonoids and GLUT4 interact directly, rather than by a mechanism related to protein-tyrosine kinase and insulin signalling inhibition. Furthermore, the results suggest that GLUT transporters are involved in flavonoid incorporation into cells.
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Research Article|
March 08 2005
Myricetin, quercetin and catechin-gallate inhibit glucose uptake in isolated rat adipocytes
Pablo STROBEL;
Pablo STROBEL
1
*Molecular Nutrition Laboratory, Faculty of Biological Sciences, Universidad Católica de Chile, Casilla 114-D, Santiago, Chile
1To whom correspondences should be addressed (email [email protected]).
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Claudio ALLARD;
Claudio ALLARD
*Molecular Nutrition Laboratory, Faculty of Biological Sciences, Universidad Católica de Chile, Casilla 114-D, Santiago, Chile
†Center for Genomics and Bioinformatics, Faculty of Biological Sciences, Universidad Católica de Chile, Casilla 114-D, Santiago, Chile
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Tomás PEREZ-ACLE;
Tomás PEREZ-ACLE
†Center for Genomics and Bioinformatics, Faculty of Biological Sciences, Universidad Católica de Chile, Casilla 114-D, Santiago, Chile
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Rosario CALDERON;
Rosario CALDERON
*Molecular Nutrition Laboratory, Faculty of Biological Sciences, Universidad Católica de Chile, Casilla 114-D, Santiago, Chile
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Rebeca ALDUNATE;
Rebeca ALDUNATE
*Molecular Nutrition Laboratory, Faculty of Biological Sciences, Universidad Católica de Chile, Casilla 114-D, Santiago, Chile
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Federico LEIGHTON
Federico LEIGHTON
*Molecular Nutrition Laboratory, Faculty of Biological Sciences, Universidad Católica de Chile, Casilla 114-D, Santiago, Chile
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Publisher: Portland Press Ltd
Received:
April 29 2004
Revision Received:
September 27 2004
Accepted:
October 07 2004
Accepted Manuscript online:
October 07 2004
Online ISSN: 1470-8728
Print ISSN: 0264-6021
The Biochemical Society, London
2005
Biochem J (2005) 386 (3): 471–478.
Article history
Received:
April 29 2004
Revision Received:
September 27 2004
Accepted:
October 07 2004
Accepted Manuscript online:
October 07 2004
Citation
Pablo STROBEL, Claudio ALLARD, Tomás PEREZ-ACLE, Rosario CALDERON, Rebeca ALDUNATE, Federico LEIGHTON; Myricetin, quercetin and catechin-gallate inhibit glucose uptake in isolated rat adipocytes. Biochem J 15 March 2005; 386 (3): 471–478. doi: https://doi.org/10.1042/BJ20040703
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