Chaudhuri G, Steingold K A, Pardridge W M, Judd H L
Department of Obstetrics and Gynecology, School of Medicine, University of California, Los Angeles 90024.
Am J Physiol. 1988 Jan;254(1 Pt 1):E79-83. doi: 10.1152/ajpendo.1988.254.1.E79.
The metabolic clearance rate (MCR) of gonadal or adrenal steroid hormones in rabbits often does not bear the expected inverse relationship with hormone binding to testosterone-binding globulin (TeBG) or corticosteroid-binding globulin (CBG). This suggests TeBG or CBG may not impede steroid hormone delivery to tissues. The effects of rabbit plasma proteins on the influxes of 3H-labeled steroids from the circulation into the rabbit uterus were measured in vivo using a tissue sampling single-injection technique. In the absence of plasma proteins, estradiol (E2) and testosterone (T) were freely diffusible through the uterine microvasculature (i.e., extraction greater than 80%). The extractions of dihydrotestosterone (DHT) and corticosterone (B) ranged from 60 to 72%, while that of cortisol (F) was reduced at 40%. Rabbit serum exerted no inhibition of the influxes of the steroids tested. The influxes of T and B greatly exceeded the rates that would be expected if only the free and albumin-bound fractions estimated in vitro were diffusible in vivo. However, the extraction of [3H]corticosteroid-binding globulin or bovine [3H]albumin were low, consistent with little, if any, extravascular uptake of the plasma proteins. The results indicate both albumin-bound and globulin-bound steroid hormone are available for transport into the uterus in the rabbit in vivo without significant exodus of the plasma protein, per se.
兔体内性腺或肾上腺甾体激素的代谢清除率(MCR)通常与激素和睾酮结合球蛋白(TeBG)或皮质类固醇结合球蛋白(CBG)的结合不存在预期的反比关系。这表明TeBG或CBG可能不会阻碍甾体激素向组织的输送。采用组织采样单次注射技术在体内测量了兔血浆蛋白对3H标记类固醇从循环进入兔子宫的流入量的影响。在没有血浆蛋白的情况下,雌二醇(E2)和睾酮(T)可自由透过子宫微血管(即提取率大于80%)。双氢睾酮(DHT)和皮质酮(B)的提取率在60%至72%之间,而皮质醇(F)的提取率则降至40%。兔血清对所测试类固醇的流入量没有抑制作用。T和B的流入量大大超过了仅根据体外估计的游离和与白蛋白结合部分在体内可扩散的速率。然而,[3H]皮质类固醇结合球蛋白或牛[3H]白蛋白的提取率较低,这表明血浆蛋白几乎没有血管外摄取(如果有的话)。结果表明,在兔体内,与白蛋白结合和与球蛋白结合的甾体激素均可用于转运至子宫,而血浆蛋白本身不会大量外流。