Pharmacokinetic profile of bilberry anthocyanins in rats and the role of glucose transporters: LC-MS/MS and computational studies
Pharmacokinetic profile of bilberry anthocyanins in rats and the role of glucose transporters: LC-MS/MS and computational studies
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DOI：
10.1016/j.jpba.2017.04.042
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发表时间：
2017-09-10
影响因子：
3.4
通讯作者：
Aldini, G.
中科院分区：
文献类型：
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作者：
Baron, G.;Altomare, A.;Aldini, G.
本研究的目的是为了更好地了解越橘（Vaccinium Myrtillus）花青素的药动学特征以及葡萄糖转运体（sGLT1和GLUT2）在其吸收中的作用。特别地，通过验证的LC-ESI-MS/MS方法测量了标准越橘提取物（Mirtoselect (R)）中15种不同花青素在大鼠中的吸收。30min后血药浓度峰值（Cmax）达到11.1 ng/mL，空腹使大鼠体内花青素的生物利用度提高了7倍以上。葡萄糖共给药不干扰整体花青素摄取。然后通过比较血浆和提取物中的相对含量来估计每种花青素的生物利用度。15种花青素在生物利用度方面表现不同，糖苷元和糖段都影响吸收。例如，阿拉伯糖苷部分是有害的，而花青素提高了生物利用度。计算研究使这些结果合理化，强调了葡萄糖转运体（sGLT1和GLUT2）在花青素吸收中的作用。特别是在sGLT1和GLUT2的识别和吸收之间发现了15种花青素的显著相关性。(C) 2017 Elsevier B.V.版权所有
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 (R)) was measured in rats by a validated LC-ESI-MS/MS approach. The plasma concentration peak (Cmax) of 11.1 ng/mL was reached after 30 min 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. (C) 2017 Elsevier B.V. All rights reserved.