Matsuda M, Kaku K, Aoki M, Inoue H, Kaneko T
Third Department of Internal Medicine, Yamaguchi University School of Medicine, Ube, Japan.
Horm Metab Res. 1991 May;23(5):209-12. doi: 10.1055/s-2007-1003655.
The effect of sulfonylurea on the activity of acetyl-coenzyme A carboxylase, a rate limiting enzyme of lipogenesis, was investigated using isolated rat adipocytes. Insulin significantly increased the enzyme activity by 170% of the control level, while glucagon and epinephrine decreased the activity of the enzyme by 53% and 64% of the control, respectively. In the presence of tolbutamide (10(-3) M) or glibenclamide (10(-6) M), a significant potentiation of insulin action was found in adipocytes. In addition, sulfonylurea restored the activity of acetyl-CoA carboxylase reduced by glucagon or epinephrine to the control level. Sulfonylurea enhancement of the acetyl-CoA carboxylase activity may offer one possible explanation for a mechanism of antilipolytic action of the drug in adipocytes.
利用分离的大鼠脂肪细胞，研究了磺脲类药物对脂肪生成的限速酶乙酰辅酶A羧化酶活性的影响。胰岛素可使该酶活性显著增加，达到对照水平的170%，而胰高血糖素和肾上腺素则分别使该酶活性降低至对照水平的53%和64%。在存在甲苯磺丁脲（10⁻³ M）或格列本脲（10⁻⁶ M）的情况下，在脂肪细胞中发现胰岛素作用有显著增强。此外，磺脲类药物可将被胰高血糖素或肾上腺素降低的乙酰辅酶A羧化酶活性恢复至对照水平。磺脲类药物增强乙酰辅酶A羧化酶活性可能为该药物在脂肪细胞中的抗脂解作用机制提供一种可能的解释。
