Pharmacokinetic profile of bilberry anthocyanins in rats and the role of glucose transporters : LC-MS/MS and computational studies
Articolo
Data di Pubblicazione:
2017
Citazione:
Pharmacokinetic profile of bilberry anthocyanins in rats and the role of glucose transporters : LC-MS/MS and computational studies / G. Baron, A. Altomare, L. Regazzoni, V. Redaelli, S. De Grandi, A. Riva, P. Morazzoni, A. Mazzolari, M. Carini, G. Vistoli, G. Aldini. - In: JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS. - ISSN 0731-7085. - 144(2017 Sep 10), pp. 112-121.
Abstract:
The aim of the present investigation was to better understand the pharmacokinetic profile of bilberry (Vaccinium Myrtillus) anthocyanins and the role of glucose transporters (sGLT1 and GLUT2) on their absorption. In particular, the absorption of 15 different anthocyanins contained in a standardized bilberry extract (Mirtoselect(®)) was measured in rats by a validated LC-ESI-MS/MS approach. The plasma concentration peak (Cmax) of 11.1ng/mL was reached after 30min and fasting condition significantly increased the bioavailability of anthocyanins by more than 7 fold in respect to fed rats. Glucose co-administration did not interfere with the overall anthocyanin uptake. Bioavailability of each anthocyanin was then estimated by comparing the relative content in plasma vs extract. The 15 anthocyanins behaved differently in term of bioavailability and both the aglycone and the sugar moiety were found to affect the absorption. For instance, arabinoside moiety was detrimental while cyanidin enhanced bioavailability. Computational studies permitted to rationalize such results, highlighting the role of glucose transporters (sGLT1 and GLUT2) in anthocyanins absorption. In particular a significant correlation was found for the 15 anthocyanins between sGLT1 and GLUT2 recognition and absorption.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
Bilberry anthocyanins; Computational studies; Glucose transporters; Mass spectrometry; Pharmacokinetic; Vaccinium myrtillus; sGLT1 and GLUT2
Elenco autori:
G. Baron, A. Altomare, L. Regazzoni, V. Redaelli, S. De Grandi, A. Riva, P. Morazzoni, A. Mazzolari, M. Carini, G. Vistoli, G. Aldini
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