Carrier-mediated uptake of nobiletin, a citrus polymethoxyflavonoid, in human intestinal Caco-2 cells.
Carrier-mediated uptake of nobiletin, a citrus polymethoxyflavonoid, in human intestinal Caco-2 cells.
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DOI：
10.1016/j.foodchem.2013.12.069
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发表时间：
2014-07
期刊：
影响因子：
8.8
通讯作者：
O. Kimura;C. Ohta;N. Koga;K. Haraguchi;Y. Kato;T. Endo
中科院分区：
文献类型：
--
作者：
O. Kimura;C. Ohta;N. Koga;K. Haraguchi;Y. Kato;T. Endo
用Caco-2细胞研究了川陈皮素（NBL）的肠吸收机制。NBL从Caco-2细胞顶膜的摄取是快速的和温度依赖性的，代谢抑制剂NaN 3和羰基氰对三氟甲氧基苯腙的存在下，没有引起NBL摄取的减少。NBL的初始摄取与其浓度之间的关系是饱和的，这表明载体介导的过程的参与。NBL的K和摄取清除率（Vmax/Km）分别为50.6和168.1 μl/mg蛋白/min。该清除率值约为非饱和摄取清除率值的9倍（Kd：18.5 μl/mg蛋白/min）。结构相似的化合物，如槲皮素和木犀草素的存在下，竞争性抑制NBL摄取。这些结果表明，从Caco-2细胞的顶端膜的NBL的摄取主要是介导的能量不依赖的易化扩散过程。
The mechanism of intestinal absorption of nobiletin (NBL) was investigated using Caco-2 cells. The uptake of NBL from the apical membranes of Caco-2 cells was rapid and temperature-dependent and the presence of metabolic inhibitors, NaN3and carbonylcyanidep-trifluoromethoxyphenylhydrazone, did not cause a decrease in NBL uptake. The relationship between the initial uptake of NBL and its concentration was saturable, suggesting the involvement of a carrier-mediated process. TheKmand uptake clearance (Vmax/Km) values for NBL were 50.6 and 168.1 μl/mg protein/min, respectively. This clearance value was about 9-fold greater than that of the non-saturable uptake clearance (Kd: 18.5 μl/mg protein/min). The presence of structurally similar compounds, such as quercetin and luteolin, competitively inhibited NBL uptake. These results suggest that uptake of NBL from the apical membranes of Caco-2 cells is mainly mediated by an energy-independent facilitated diffusion process.