Satsu Hideo, Awara Sohei, Unno Tomonori, Shimizu Makoto
a Department of Biotechnology, Faculty of Engineering , Maebashi Institute of Technology , Maebashi , Japan.
b Department of Applied Biological Chemistry, Graduate School of Agricultural and Life Sciences , The University of Tokyo , Tokyo , Japan.
Biosci Biotechnol Biochem. 2018 Apr;82(4):636-646. doi: 10.1080/09168451.2017.1387515. Epub 2017 Dec 1.
Inhibition of excessive fructose intake in the small intestine could alleviate fructose-induced diseases such as hypertension and non-alcoholic fatty liver disease. We examined the effect of phytochemicals on fructose uptake using human intestinal epithelial-like Caco-2 cells which express the fructose transporter, GLUT5. Among 35 phytochemicals tested, five, including nobiletin and epicatechin gallate (ECg), markedly inhibited fructose uptake. Nobiletin and ECg also inhibited the uptake of glucose but not of L-leucine or Gly-Sar, suggesting an inhibitory effect specific to monosaccharide transporters. Kinetic analysis further suggested that this reduction in fructose uptake was associated with a decrease in the apparent number of cell-surface GLUT5 molecules, and not with a change in the affinity of GLUT5 for fructose. Lastly, nobiletin and ECg suppressed the permeation of fructose across Caco-2 cell monolayers. These findings suggest that nobiletin and ECg are good candidates for preventing diseases caused by excessive fructose intake.
抑制小肠中过量的果糖摄入可以缓解果糖诱导的疾病，如高血压和非酒精性脂肪肝病。我们使用表达果糖转运蛋白GLUT5的人肠道上皮样Caco-2细胞，研究了植物化学物质对果糖摄取的影响。在测试的35种植物化学物质中，包括川陈皮素和表儿茶素没食子酸酯（ECg）在内的5种物质显著抑制了果糖摄取。川陈皮素和ECg也抑制了葡萄糖的摄取，但对L-亮氨酸或甘氨酰甘氨酸没有抑制作用，这表明它们对单糖转运蛋白具有特异性抑制作用。动力学分析进一步表明，果糖摄取的减少与细胞表面GLUT5分子的表观数量减少有关，而与GLUT5对果糖的亲和力变化无关。最后，川陈皮素和ECg抑制了果糖跨Caco-2细胞单层的渗透。这些发现表明，川陈皮素和ECg是预防由过量果糖摄入引起的疾病的良好候选物质。
