Skowroński R, Madrala A, Angielski S
Department of Clinical Biochemistry, Medical Academy, Gdańsk, Poland.
Horm Metab Res. 1988 Feb;20(2):77-81. doi: 10.1055/s-2007-1010757.
The effects of oral hypoglycaemic drugs, SPC-703 (n-/p-toluenesulphonyl/-5-methyl-2-pirazoline-1-carbonami de) and tolbutamide on insulin binding and glucose metabolism by isolated adipocytes were studied. After 10 days of administration of both sulphonylurea derivatives, no differences were observed in insulin concentration between both experimental and the control groups of animals, despite a significant fall in blood glucose level. SPC-703 and tolbutamide in concentrations of 1 mM added in vitro to the suspension of adipocytes had no effect on insulin binding or on basal and insulin simulated glucose metabolism. Daily administration of 300 mg/kg body weight of SPC-703 or tolbutamide for 10 days resulted in 48% and 34% increase of specific binding of insulin by adipocytes, respectively. From the Scatchard plot analysis we noted that the increase of binding resulted from increased affinity of insulin receptors for hormone. Simultaneous increase in basal and insulin stimulated glucose metabolism by adipocytes, as measured by 14CO2 production and 14C incorporation into cellular lipids, was observed. The results indicate that hypoglycaemic action of sulphonylureas may be explained by increased affinity of insulin receptors and the stimulating action of these compounds on peripheral glucose metabolism.
研究了口服降糖药SPC - 703（N - /对甲苯磺酰/- 5 - 甲基 - 2 - 吡唑啉 - 1 - 碳酰胺）和甲苯磺丁脲对分离的脂肪细胞胰岛素结合及葡萄糖代谢的影响。在给予两种磺酰脲衍生物10天后，尽管血糖水平显著下降，但实验组和对照组动物的胰岛素浓度未观察到差异。体外向脂肪细胞悬液中添加1 mM浓度的SPC - 703和甲苯磺丁脲对胰岛素结合或基础及胰岛素刺激的葡萄糖代谢均无影响。每日给予300 mg/kg体重的SPC - 703或甲苯磺丁脲，持续10天，结果脂肪细胞对胰岛素的特异性结合分别增加了48%和34%。通过Scatchard作图分析，我们注意到结合的增加是由于胰岛素受体对激素的亲和力增加所致。同时观察到，通过14CO2产生量和14C掺入细胞脂质来衡量，脂肪细胞基础及胰岛素刺激的葡萄糖代谢同时增加。结果表明，磺酰脲类药物的降糖作用可能是由于胰岛素受体亲和力增加以及这些化合物对周围葡萄糖代谢的刺激作用。
