Research Center for Nutrition and Food Safety, Institute of Military Preventive Medicine, Third Military Medical University, Chongqing Key Laboratory of Nutrition and Food Safety, Research Center for Medical Nutrition, Chongqing 400038, People's Republic of China.
J Nutr Biochem. 2013 Nov;24(11):1823-9. doi: 10.1016/j.jnutbio.2013.04.003. Epub 2013 Aug 6.
Resveratrol is a natural polyphenol that exerts potent effects to suppress atherosclerosis. However, its low concentration in plasma has placed this role in doubt. Thus, resveratrol effects might be dependent on its transport into vascular endothelium, a question not previously addressed in spite of its obvious and fundamental importance. Via high-performance liquid chromatography and liquid chromatography/mass spectrometry, we found that resveratrol was absorbed by human umbilical vein endothelial cells in a temperature-, concentration- and time-dependent manner, suggesting the involvement of passive diffusion and active transport. As determined by confocal laser scanning microscopy, resveratrol primarily distributed throughout the cytoplasm. Furthermore, resveratrol absorption was modulated by serum proteins and sodium-dependent glucose transporter 1 (SGLT1) yet inhibited by glucose (an SGLT1 substrate) and phlorizin (an SGLT1 selective inhibitor), as well as SGLT1 siRNA transfection. Additionally, Sprague-Dawley rats were intragastrically administrated with 100mg/kg of resveratrol and the concentration of resveratrol in blood vessels declined more slowly up to 24h compared to that in the blood. Our results suggested that resveratrol uptake by vascular endothelial cells involved both passive diffusion and an SGLT1-mediated process, at least partially. Moreover, the intracellular resveratrol pool may be more important than the serum level in vivo. These provide new insights into the cardiovascular benefits of resveratrol.
白藜芦醇是一种天然多酚，具有抑制动脉粥样硬化的强大作用。然而，其在血浆中的低浓度使其作用受到质疑。因此，白藜芦醇的作用可能依赖于其向血管内皮的转运，尽管这一点显然非常重要，但以前尚未对此进行过研究。通过高效液相色谱和液相色谱/质谱分析，我们发现白藜芦醇以温度、浓度和时间依赖的方式被人脐静脉内皮细胞吸收，提示其涉及被动扩散和主动转运。通过共聚焦激光扫描显微镜确定，白藜芦醇主要分布在细胞质中。此外，白藜芦醇的吸收受血清蛋白和钠依赖性葡萄糖转运蛋白 1（SGLT1）调节，但被葡萄糖（SGLT1 底物）和根皮苷（SGLT1 选择性抑制剂）以及 SGLT1 siRNA 转染所抑制。此外，Sprague-Dawley 大鼠经胃内给予 100mg/kg 的白藜芦醇，与血液中的白藜芦醇浓度相比，血管中的白藜芦醇浓度在 24 小时内下降更缓慢。我们的结果表明，血管内皮细胞摄取白藜芦醇涉及被动扩散和 SGLT1 介导的过程，至少部分如此。此外，细胞内白藜芦醇池在体内可能比血清水平更重要。这些为白藜芦醇的心血管益处提供了新的见解。
