Farese R V, Ishizuka T, Standaert M L, Cooper D R
Veterans' Administration Hospital, Tampa, FL 33612.
Metabolism. 1991 Feb;40(2):196-200. doi: 10.1016/0026-0495(91)90174-u.
Glyburide and tolbutamide, at concentrations of 20 to 40 mumol/L and 1 to 2 mmol/L, respectively, stimulated glucose transport in rat adipocytes. Concomitantly, protein kinase C was activated, as evidenced by translocation of immunoreactive enzyme from cytosol to membranes. Glucose transport effects of the sulfonylureas were blocked by three inhibitors of protein kinase C (H-7, staurosporine, and sangivamycin), and by phorbol ester-induced down-regulation of protein kinase C. These findings suggest that sulfonylureas may stimulate glucose transport in rat adipocytes through activation of protein kinase C.
格列本脲和甲苯磺丁脲,分别在浓度为20至40微摩尔/升和1至2毫摩尔/升时,刺激大鼠脂肪细胞的葡萄糖转运。与此同时,蛋白激酶C被激活,免疫反应性酶从胞质溶胶转位到细胞膜就证明了这一点。磺酰脲类药物的葡萄糖转运作用被三种蛋白激酶C抑制剂(H-7、星形孢菌素和放线菌素)以及佛波酯诱导的蛋白激酶C下调所阻断。这些发现表明,磺酰脲类药物可能通过激活蛋白激酶C来刺激大鼠脂肪细胞的葡萄糖转运。