Mahgoub A, Hirsch P F, Munson P L
Department of Pharmacology, School of Medicine, University of North Carolina, Chapel Hill 27599-7455, USA.
Endocrine. 1997 Jun;6(3):279-83. doi: 10.1007/BF02820504.
The specificity and potency of glucocorticoids to lower serum calcium (Ca) in rats after parathyroidectomy (PTX) and adrenalectomy (ADX) were examined. Rats fasted overnight were given sc injections of various steroids immediately after the operations. The fall in serum calcium 5 h after PTX-ADX in rats given hypocalcemic doses of corticosterone was compared to that after injection of a test steroid. At high doses, progesterone, estradiol, testosterone, and aldosterone were inactive, whereas glucocorticoids were consistently hypocalcemic. These results indicate that the Ca-lowering effect is specific for steroids with glucocorticoid activity. Potency estimates were made by comparing the dose-response of natural and synthetic glucocorticoids to that of corticosterone, the major glucocorticoid in rats. The mean potency of hydrocortisone was 8.2 times that of corticosterone. Prednisolone was about 9.6, triamcinolone 33, betamethasone 109, and dexamethasone 301 times as potent as corticosterone. Thus, the use of the calcium-lowering action as a bioassay has provides a specific and rapid in vivo method to compare potencies of glucocorticoids consistent with those obtained by anti-inflammatory and glycogen deposition assays. The importance of this interesting calcitonin-like action of glucocorticoids in normal physiology of calcium metabolism is not yet established.
研究了糖皮质激素在大鼠甲状旁腺切除(PTX)和肾上腺切除(ADX)后降低血清钙(Ca)的特异性和效力。过夜禁食的大鼠在手术后立即皮下注射各种类固醇。将给予降钙素剂量皮质酮的大鼠PTX - ADX后5小时血清钙的下降与注射测试类固醇后的下降进行比较。在高剂量时,孕酮、雌二醇、睾酮和醛固酮无活性,而糖皮质激素始终具有降钙作用。这些结果表明,降钙作用对具有糖皮质激素活性的类固醇具有特异性。通过比较天然和合成糖皮质激素与大鼠主要糖皮质激素皮质酮的剂量反应来进行效力估计。氢化可的松的平均效力是皮质酮的8.2倍。泼尼松龙约为9.6倍,曲安西龙为33倍,倍他米松为109倍,地塞米松为皮质酮的301倍。因此,利用降钙作用作为生物测定法提供了一种在体内比较糖皮质激素效力的特异性和快速方法,这与通过抗炎和糖原沉积测定法获得的结果一致。糖皮质激素这种有趣的降钙素样作用在钙代谢正常生理中的重要性尚未确定。