Baron G, Altomare A, Regazzoni L, Redaelli V, Grandi S, Riva A, Morazzoni P, Mazzolari A, Carini M, Vistoli G, Aldini G
Department of Pharmaceutical Sciences, University of Milan, via Mangiagalli 25, 20133, Milan, Italy.
Indena S. p. A., Viale Ortles 12-20139, Milan, Italy.
J Pharm Biomed Anal. 2017 Sep 10;144:112-121. doi: 10.1016/j.jpba.2017.04.042. Epub 2017 Apr 27.
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.
本研究的目的是更好地了解越橘（欧洲越橘）花青素的药代动力学特征以及葡萄糖转运蛋白（sGLT1和GLUT2）在其吸收过程中的作用。具体而言，通过经过验证的LC-ESI-MS/MS方法，在大鼠中测量了标准化越橘提取物（Mirtoselect）中所含15种不同花青素的吸收情况。30分钟后达到血浆浓度峰值（Cmax）为11.1ng/mL，与进食大鼠相比，禁食条件下花青素的生物利用度显著提高了7倍以上。葡萄糖共同给药并未干扰花青素的总体摄取。然后通过比较血浆与提取物中的相对含量来估计每种花青素的生物利用度。这15种花青素在生物利用度方面表现不同，发现糖苷配基和糖部分均会影响吸收。例如，阿拉伯糖苷部分不利，而花青素增强了生物利用度。计算研究有助于解释这些结果，突出了葡萄糖转运蛋白（sGLT1和GLUT2）在花青素吸收中的作用。特别是，发现15种花青素在sGLT1和GLUT2识别与吸收之间存在显著相关性。
