کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8304134 | 1538381 | 2018 | 26 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Quercetin inhibits glucose transport by binding to an exofacial site on GLUT1
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موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
زیست شیمی
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چکیده انگلیسی
Quercetin, a common dietary flavone, is a competitive inhibitor of glucose uptake and is also thought to be transported into cells by GLUT1. In this study, we confirm that quercetin is a competitive inhibitor of GLUT1 and also demonstrate that newly synthesized compounds, WZB-117 and BAY-876 are robust inhibitors of GLUT1 in L929â¯cells. To measure quercetin interaction with L929â¯cells, we develop a new fluorescent assay using flow cytometry. The binding of quercetin and its inhibitory effects on 2-deoxyglucose (2DG) uptake showed nearly identical dose dependent effects, with both having maximum effects between 50 and 100â¯Î¼M and similar half maximum effects at 8.9 and 8.5â¯Î¼M respectively. The interaction of quercetin was rapid with t1/2 of 54â¯s and the onset and loss of its inhibitory effects on 2DG uptake were equally fast. This suggests that either quercetin is simply binding to surface GLUT1 or its transport in and out of the cell reaches equilibrium very quickly. If quercetin is transported, the co-incubation of quercetin with other glucose inhibitors should block quercetin uptake. However, we observed that WZB-117, an exofacial binding inhibitor of GLUT1 reduced quercetin interaction, while cytochalasin B, an endofacial binding inhibitor, enhanced quercetin interaction, and BAY-876 had no effect on quercetin interaction. Taken together, these data are more consistent with quercetin simply binding to GLUT1, but not actually being transported into L929â¯cells via the glucose channel in GLUT1.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biochimie - Volume 151, August 2018, Pages 107-114
Journal: Biochimie - Volume 151, August 2018, Pages 107-114
نویسندگان
Kathryn E. Hamilton, Janelle F. Rekman, Leesha K. Gunnink, Brianna M. Busscher, Jordan L. Scott, Andrew M. Tidball, Nathan R. Stehouwer, Grace N. Johnecheck, Brendan D. Looyenga, Larry L. Louters,