Sakiyama R, Pardridge W M, Musto N A
Department of Medicine, University of California School of Medicine, Los Angeles 90024.
J Clin Endocrinol Metab. 1988 Jul;67(1):98-103. doi: 10.1210/jcem-67-1-98.
The availability of testosterone and estradiol to Sertoli and prostate cells is dependent upon 1) the permeability properties of the blood-tubular barrier (BTB) of the testis or prostate cell membrane, and 2) sex steroid binding to plasma proteins, such as albumin or testosterone-binding globulin (TeBG). Sex steroid influx into these tissues was studied after in vivo arterial bolus injections of [3H]testosterone or [3H]estradiol in anesthetized rats. Both testosterone and estradiol were readily cleared across the BTB or prostate cell membrane in the absence of plasma proteins and in the presence of human pregnancy serum, in which testosterone or estradiol are 80-95% distributed to TeBG. The extravascular extraction of [3H]TeBG across the BTB or prostate plasma membrane [73 +/- 2% (+/- SE) and 92 +/- 9%, respectively] was significantly greater than extraction of [3H]albumin or other plasma space markers and indicative of a rapid first pass clearance of TeBG by Sertoli or prostate cells. In summary, these studies indicate that 1) testosterone and estradiol are readily cleared by Sertoli and prostate cells; 2) albumin- and TeBG-bound sex steroids represent the major circulating pool of bioavailable hormone for testis or prostate; and 3) the TeBG-sex steroid complex may be nearly completely available for influx through the BTB or prostate plasma membrane.
1)睾丸或前列腺细胞膜的血-管屏障(BTB)的通透性;2)性类固醇与血浆蛋白的结合,如白蛋白或睾酮结合球蛋白(TeBG)。在麻醉大鼠体内动脉推注[3H]睾酮或[3H]雌二醇后,研究了性类固醇进入这些组织的情况。在不存在血浆蛋白以及存在人妊娠血清(其中睾酮或雌二醇80%-95%分布于TeBG)的情况下,睾酮和雌二醇均能很容易地穿过BTB或前列腺细胞膜。[3H]TeBG穿过BTB或前列腺质膜的血管外提取率(分别为73±2%(±标准误)和92±9%)显著高于[3H]白蛋白或其他血浆空间标志物的提取率,表明支持细胞或前列腺细胞对TeBG有快速的首过清除作用。总之,这些研究表明:1)支持细胞和前列腺细胞能很容易地清除睾酮和雌二醇;2)与白蛋白和TeBG结合的性类固醇是睾丸或前列腺生物可利用激素的主要循环库;3)TeBG-性类固醇复合物几乎可完全用于穿过BTB或前列腺质膜进入细胞。