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兔体内主要皮质类固醇结合亲和力与代谢清除率之间的相互关系。

Interrelations between binding affinity and metabolic clearance rate for the main corticosteroids in the rabbit.

作者信息

Daniel J Y, Leboulenger F, Vaudry H, Floch H H, Assenmacher I

出版信息

J Steroid Biochem. 1982 Mar;16(3):379-84. doi: 10.1016/0022-4731(82)90049-8.

DOI:10.1016/0022-4731(82)90049-8
PMID:7087466
Abstract

In the rabbit, the metabolic clearance rate (MCR) was found to be higher for corticosterone than for cortisol. At the same time corticosterone, aldosterone and 11-dehydrocorticosterone showed similar MCR while cortisone ranged at intermediate levels between cortisol and corticosterone. The relative binding affinity of transcortin to the corticosteroids, as calculated by an in vitro technique, decreased progressively from cortisol, to cortisone, then to corticosterone, then 11-dehydrocorticosterone and, finally to aldosterone. The occurrence of antibodies in plasma, induced against aldosterone, corticosterone or even cortisone resulted in a marked decrease in the MCR of the corresponding steroid, to the level measured in controls for cortisol. We deduced that, in rabbits: (1) the MCR of a corticosteroid is clearly connected with its binding to a specific protein; (2) in spite of the relatively high binding affinity of transcortin for corticosterone as compared to other species it nevertheless appears unable to significantly protect the steroid against peripheral metabolism; (3) a very effective protection is however, induced, by raising a specific antibody with a high binding affinity for corticosterone.

摘要

在兔子身上,发现皮质酮的代谢清除率(MCR)高于皮质醇。同时,皮质酮、醛固酮和11-脱氢皮质酮的MCR相似,而可的松则介于皮质醇和皮质酮之间的中等水平。通过体外技术计算得出,皮质素与皮质类固醇的相对结合亲和力从皮质醇到可的松,再到皮质酮、11-脱氢皮质酮,最后到醛固酮逐渐降低。血浆中针对醛固酮、皮质酮甚至可的松产生的抗体,会导致相应类固醇的MCR显著降低,降至对照组中皮质醇所测得的水平。我们推断,在兔子中:(1)皮质类固醇的MCR与其与特定蛋白质的结合明显相关;(2)尽管与其他物种相比,皮质素对皮质酮的结合亲和力相对较高,但它似乎无法显著保护该类固醇免受外周代谢的影响;(3)然而,通过产生对皮质酮具有高结合亲和力的特异性抗体,可以诱导出非常有效的保护作用。

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