委陵菜黄酮衍生物促进L6细胞GLUT4的转位活性

Activities of tiliroside derivatives on enhancing GLUT4 translocation in L6 cells

目的：筛选出具有促进骨骼肌细胞L6表面GLUT4转位活性的委陵菜黄酮衍生物。方法：将实验细胞分成空白对照组，胰岛素组（以胰岛素刺激20min）和黄酮衍生物组（加不同衍生物刺激24h），用类ELISA法测定细胞膜上GLUT4的量。结果：对黄酮衍生物1～14影响L6大鼠骨骼肌细胞GLUT4转运的实验结果表明，衍生物1、5、6、8～11在10μg／mL作用浓度下，促进GLUT4转位的量分别为空白对照组的（3．60±0．30）倍、（3．66±0．26）倍、（2．87±0．49）倍、（3．97±0．37）倍、（2．82±0．45）倍、（3．37±0．67）倍、（4．43±0．61）倍（P〈0．05）。化合物6与胰岛素叠加作用为空白对照组的（4．31±0．22）倍（P〈0．05）。结论：委陵菜黄酮衍生物促进GLUT4转位的作用为首次报道。黄酮衍生物1、5、6、8～11有明显地促进L6表面GLUT4转位的作用；化合物6与胰岛素有协同作用。

Objective： To study the effects of tiliroside derivatives on enhancing translocation activity of GLUT4 on the surface of the skeletal muscle cell L6. Methods： Experimental groups included basal group, insulin group and different tiliroside derivatives groups. For the tiliroside derivatives groups, the cells were incubated with the different tiliroside derivatives for 24 h; for the insulin group, the cells were incubated with insulin for 20 min. The amount of GLUT4 on the surface of the skeletal muscle cell L6 was measured by an an- tibody-coupled absorbance assay. Results： In the experiment of tiliroside derivatives 1 -14 on enhancing GLUT4 translocation in L6 cells, the folds of GLUT4 translocation above basal in derivatives 1, 5, 6, and 8-11 （10μg/mL） groups were 3.60 ± 0.30, 3.66 ± 0.26, 2.87 ± 0.49, 3.97 ± 0.37, 2.82 ± 0.45, 3.37 ± 0.67, 4.43 ± 0.61 （P 〈 0.05）, respectively. In derivative 6 with insulin group, the value was 4.31 - 0.22 times of the basal group （P 〈 0.05）. Conclusion： The translocation of GLUT4 is enhanced by tiliroside derivatives 1, 5, 6, and 8-11, and the overlay experiment show that there is a synergism effect on enhancing GLUT4 translocation between insulin and derivative 6.