AIM： To evaluate the inhibitory effects of apigenin and kaempferol on the uptake of several important solute carrier （SLC） transporters.METHODS： Various SLC transporters including the essential human organic anion...AIM： To evaluate the inhibitory effects of apigenin and kaempferol on the uptake of several important solute carrier （SLC） transporters.METHODS： Various SLC transporters including the essential human organic anion transporter 1 （OAT1）, OAT2, OAT3 and OAT4 as well as the important organic cation transporter 1 （OCTN1） and OCTN2, were over-expressed in human embryonic kidney （HEK）-293 cells, a well-established cell model of transporter studies. Transport uptake assay was performed 24 h after the transfection. The transport activity was assessed with the uptake of previously determined transporter model substrates and the inhibitory effect of apigenin and kaempferol was evaluated with the substrate uptake in the presence of 10 μmol/L of each compound. Uptake measurements with varying concentrations of inhibitors （ranged from 0.0001 to 50 μmol/L） were performed to further characterize the inhibitory potency of apigenin and kaempferol. The IC50 value （the concentration that inhibits 50% of the transporter function） of each com-pound was then calculated by the nonlinear regression model of Graphpad Prism 6.0 software.RESULTS： Our data indicated that apigenin could potently inhibit the uptake of estrone-3-sulfate （ES） mediated by the HEK-293 cells expressing OAT2, OAT3 and OAT4 as well as the L-ergothioneine uptake via OCTN1-expressing HEK-293 cells. Among these trans-porters, the most prominent inhibition of apigenin was observed in the case of OAT3. Kaempferol showed sig-nifcant inhibitory effects on the uptake of ES mediated through OAT2 and OAT3. Impaired L-ergothioneine uptake due to the presence of kaempferol was also ob-served in OCTN1-expressing HEK-293 cells. Similar to apigenin, kaempferol showed the most potent inhibito-ry effect on OAT3 as well. To further assess the inhibi-tory potencies of these two compounds on the uptake of ES mediated by OAT3-expressing HEK-293 cells, their IC50 values were then determined. Both chemicals showed pronounced inhibitory potencies on OAT展开更多
本试验旨在研究枯草芽孢杆菌(BS)、蒙脱石(MMT)及其互作对产蛋鸡生产性能、养分表观利用率和肠黏膜养分转运载体基因表达的影响。采用2×2双因子随机试验设计,主效应分别为BS(0、0.5 g/kg)、MMT(0、0.5 g/kg)及二者互作。选择360只2...本试验旨在研究枯草芽孢杆菌(BS)、蒙脱石(MMT)及其互作对产蛋鸡生产性能、养分表观利用率和肠黏膜养分转运载体基因表达的影响。采用2×2双因子随机试验设计,主效应分别为BS(0、0.5 g/kg)、MMT(0、0.5 g/kg)及二者互作。选择360只29周龄健康的罗曼粉壳蛋鸡,随机分为4组(每组6个重复,每个重复15只),分别饲喂基础饲粮(对照组)、基础饲粮+0.5 g/kg BS(BS组)、基础饲粮+0.5 g/kg M M T(M M T组)、基础饲粮+0.5 g/kg M M T+0.5 g/kg BS(M M T+BS组)。预试期7 d,正试期70 d。结果显示:1)与对照组相比,各添加组产蛋鸡产蛋率均显著提高(P<0.05);MMT组和MMT+BS组日产蛋量显著提高(P<0.05);MMT+BS组料蛋比显著降低(P<0.05)。2)饲粮中添加BS显著提高了干物质、粗脂肪、能量和粗蛋白质的表观利用率(P<0.05);BS组和MMT+BS组能量表观利用率显著高于对照组(P<0.05)。3)与对照组相比,各添加组产蛋鸡空肠黏膜碱性氨基酸转运载体1 m RNA表达量均显著提高(P<0.05);BS和M M T互作对产蛋鸡空肠黏膜易化葡萄糖转运载体2和碱性氨基酸转运载体1m RNA表达量有显著影响(P<0.05)。由此可见,饲粮中单独添加BS和M M T及二者联用均能够提高产蛋鸡的产蛋率和日产蛋量;饲粮中添加BS能够提高产蛋鸡对饲粮中干物质、粗脂肪、粗蛋白质和能量的表观利用率;饲粮中单独添加BS和MMT及二者联用均能够上调产蛋鸡肠黏膜碱性氨基酸转运载体1基因的表达。展开更多
AIM:To evaluate the correlation between the level of 18 F-fluoro-2-deoxyglucose (18 F-FDG) uptake and glucose transporter 1 (GLUT1) expression in colorectal adenocarcinoma (CRA).METHODS:Forty four patients with resect...AIM:To evaluate the correlation between the level of 18 F-fluoro-2-deoxyglucose (18 F-FDG) uptake and glucose transporter 1 (GLUT1) expression in colorectal adenocarcinoma (CRA).METHODS:Forty four patients with resected CRA and preoperative 18 F-FDG positron emission tomography computed tomography data were investigated in this study.Comparison of maximum standardized uptake value (SUVmax) of the lesion was made with GLUT1 expression by immunohistochemistry and various clinicopathologic factors including tumor volume,invasion depth,gross finding,and lymph node metastasis.RESULTS:SUVmax was 14.45 ± 7.0 in negative GLUT1 expression cases,15.51 ± 5.7 in weak GLUT1 expression cases,and 16.52 ± 6.8 in strong GLUT1 expression cases,and there was no correlation between between GLUT1 expression and SUVmax.SUVmax was significantly correlated with tumor volume (P < 0.001).However,there was no significant differences in SUVmax and GLUT1 expression among other clinicopathologic factors.CONCLUSION:GLUT1 expression does not correlates significantly with 18 F-FDG uptake in CRA.18 F-FDG uptake was increased with tumor volume,which is statistically significant.展开更多
基金Supported by Internal funding from Faculty of Pharmacy,the University of Sydney,Australia
文摘AIM： To evaluate the inhibitory effects of apigenin and kaempferol on the uptake of several important solute carrier （SLC） transporters.METHODS： Various SLC transporters including the essential human organic anion transporter 1 （OAT1）, OAT2, OAT3 and OAT4 as well as the important organic cation transporter 1 （OCTN1） and OCTN2, were over-expressed in human embryonic kidney （HEK）-293 cells, a well-established cell model of transporter studies. Transport uptake assay was performed 24 h after the transfection. The transport activity was assessed with the uptake of previously determined transporter model substrates and the inhibitory effect of apigenin and kaempferol was evaluated with the substrate uptake in the presence of 10 μmol/L of each compound. Uptake measurements with varying concentrations of inhibitors （ranged from 0.0001 to 50 μmol/L） were performed to further characterize the inhibitory potency of apigenin and kaempferol. The IC50 value （the concentration that inhibits 50% of the transporter function） of each com-pound was then calculated by the nonlinear regression model of Graphpad Prism 6.0 software.RESULTS： Our data indicated that apigenin could potently inhibit the uptake of estrone-3-sulfate （ES） mediated by the HEK-293 cells expressing OAT2, OAT3 and OAT4 as well as the L-ergothioneine uptake via OCTN1-expressing HEK-293 cells. Among these trans-porters, the most prominent inhibition of apigenin was observed in the case of OAT3. Kaempferol showed sig-nifcant inhibitory effects on the uptake of ES mediated through OAT2 and OAT3. Impaired L-ergothioneine uptake due to the presence of kaempferol was also ob-served in OCTN1-expressing HEK-293 cells. Similar to apigenin, kaempferol showed the most potent inhibito-ry effect on OAT3 as well. To further assess the inhibi-tory potencies of these two compounds on the uptake of ES mediated by OAT3-expressing HEK-293 cells, their IC50 values were then determined. Both chemicals showed pronounced inhibitory potencies on OAT
文摘本试验旨在研究枯草芽孢杆菌(BS)、蒙脱石(MMT)及其互作对产蛋鸡生产性能、养分表观利用率和肠黏膜养分转运载体基因表达的影响。采用2×2双因子随机试验设计,主效应分别为BS(0、0.5 g/kg)、MMT(0、0.5 g/kg)及二者互作。选择360只29周龄健康的罗曼粉壳蛋鸡,随机分为4组(每组6个重复,每个重复15只),分别饲喂基础饲粮(对照组)、基础饲粮+0.5 g/kg BS(BS组)、基础饲粮+0.5 g/kg M M T(M M T组)、基础饲粮+0.5 g/kg M M T+0.5 g/kg BS(M M T+BS组)。预试期7 d,正试期70 d。结果显示:1)与对照组相比,各添加组产蛋鸡产蛋率均显著提高(P<0.05);MMT组和MMT+BS组日产蛋量显著提高(P<0.05);MMT+BS组料蛋比显著降低(P<0.05)。2)饲粮中添加BS显著提高了干物质、粗脂肪、能量和粗蛋白质的表观利用率(P<0.05);BS组和MMT+BS组能量表观利用率显著高于对照组(P<0.05)。3)与对照组相比,各添加组产蛋鸡空肠黏膜碱性氨基酸转运载体1 m RNA表达量均显著提高(P<0.05);BS和M M T互作对产蛋鸡空肠黏膜易化葡萄糖转运载体2和碱性氨基酸转运载体1m RNA表达量有显著影响(P<0.05)。由此可见,饲粮中单独添加BS和M M T及二者联用均能够提高产蛋鸡的产蛋率和日产蛋量;饲粮中添加BS能够提高产蛋鸡对饲粮中干物质、粗脂肪、粗蛋白质和能量的表观利用率;饲粮中单独添加BS和MMT及二者联用均能够上调产蛋鸡肠黏膜碱性氨基酸转运载体1基因的表达。
基金Supported by National Research Foundation of Korea Grant funded by the Ministry of Education,Science and Technology through the Research Center for Resistant Cells,No.R13-2003-009
文摘AIM:To evaluate the correlation between the level of 18 F-fluoro-2-deoxyglucose (18 F-FDG) uptake and glucose transporter 1 (GLUT1) expression in colorectal adenocarcinoma (CRA).METHODS:Forty four patients with resected CRA and preoperative 18 F-FDG positron emission tomography computed tomography data were investigated in this study.Comparison of maximum standardized uptake value (SUVmax) of the lesion was made with GLUT1 expression by immunohistochemistry and various clinicopathologic factors including tumor volume,invasion depth,gross finding,and lymph node metastasis.RESULTS:SUVmax was 14.45 ± 7.0 in negative GLUT1 expression cases,15.51 ± 5.7 in weak GLUT1 expression cases,and 16.52 ± 6.8 in strong GLUT1 expression cases,and there was no correlation between between GLUT1 expression and SUVmax.SUVmax was significantly correlated with tumor volume (P < 0.001).However,there was no significant differences in SUVmax and GLUT1 expression among other clinicopathologic factors.CONCLUSION:GLUT1 expression does not correlates significantly with 18 F-FDG uptake in CRA.18 F-FDG uptake was increased with tumor volume,which is statistically significant.
基金This work was supported by grants from the National Natural Science Foundation of China （ No. 81173047 and No. 31371161 ） and the Natural Science Foundation of Hunan （No. 12JJ5068）.
