Engfeldt P, Arner P, Ostman J
J Clin Endocrinol Metab. 1983 Mar;56(3):501-6. doi: 10.1210/jcem-56-3-501.
The influence of several agents known to affect the rate of lipolysis or the phosphodiesterase (PDE) activity in rat adipose tissue was studied in human adipose tissue in vitro. Only insulin, catecholamines, prostaglandin E1, and cAMP increased PDE activity in man (by 20-40% over the control values). In dose-response studies, it was found that the ED50 values for insulin and isopropyl noradrenaline were of the same magnitude as the previously observed ED50 values for lipolysis in human adipose tissue. The time course for insulin and isopropyl noradrenaline showed maximum stimulation after 10 min, followed by a decline, with the curve approaching zero at 60 min. In subcellular fractions of adipose tissue, the highest specific PDE activity was found in the particulate fraction, in which the effects of both insulin and isopropyl noradrenaline were most marked. It is concluded that the stimulatory effect of catecholamines on PDE may be one reason for the failure of these agents to produce a sustained increase in the cAMP level and that the effect of insulin on PDE may be one mechanism by which insulin reduces the rate of lipolysis.
在体外人体脂肪组织中研究了几种已知会影响大鼠脂肪组织脂解速率或磷酸二酯酶(PDE)活性的药物的作用。只有胰岛素、儿茶酚胺、前列腺素E1和环磷酸腺苷(cAMP)能增加人体PDE活性(比对照值增加20% - 40%)。在剂量 - 反应研究中,发现胰岛素和异丙去甲肾上腺素的半数有效剂量(ED50)值与先前在人体脂肪组织中观察到的脂解ED50值大小相同。胰岛素和异丙去甲肾上腺素的时间进程显示,10分钟后刺激作用达到最大值,随后下降,60分钟时曲线接近零。在脂肪组织的亚细胞组分中,颗粒组分的特异性PDE活性最高,胰岛素和异丙去甲肾上腺素在该组分中的作用最为显著。得出的结论是,儿茶酚胺对PDE的刺激作用可能是这些药物未能使cAMP水平持续升高的原因之一,而胰岛素对PDE的作用可能是胰岛素降低脂解速率的一种机制。