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多种甾体对双氢睾酮与人良性前列腺增生中亲雄激素蛋白结合的抑制作用。

Inhibition by various steroids on dihydrotestosterone binding to androphilic protein in human benign prostatic hypertrophy.

作者信息

Kodama T, Honda S, Shimazaki J

出版信息

Endocrinol Jpn. 1978 Oct;25(5):453-60. doi: 10.1507/endocrj1954.25.453.

Abstract

The effect of various steroidal compounds on the binding of the androphilic protein to dihydrotestosterone in the cytosol of tissues of human benign prostatic hypertrophy was examined. Androgens, as well as estrogens and gestagens showed an inhibitory effect on the binding. Non-steroidal anti-androgens were revealed to be weak inhibitors on the binding. Two androphilic proteins were observed in Sephadex G-200 chromatography in fractions eluted at the void volume and in fractions appearing at the site of IgG, and the rate of inhibition on the binding of both fractions by various steroids was compared. The rate of inhibition by various compounds was generally higher in the IgG fraction than in the void volume fraction. When the ligand and inhibitors were incubated with the cytosol prior to fractionation by Sephadex chromatography, rate of inhibition was lower than that obtained when the ligand and inhibitors were reacted with fractions after chromatography. Implications of the difference observed in these two experiments are not clear at this moment. The results obtained by the protamine precipitation experiment were almost the same as those by the experiment using the extract of the unfractionated acetone-dried cytosol, therefore, the protamine procedure does not seem to precipitate the tissue specific androphilic protein specifically.

摘要

研究了各种甾体化合物对人良性前列腺增生组织胞浆中亲雄激素蛋白与双氢睾酮结合的影响。雄激素以及雌激素和孕激素均显示出对该结合的抑制作用。已发现非甾体类抗雄激素是该结合的弱抑制剂。在Sephadex G - 200色谱中,在空体积洗脱的级分和出现在IgG位置的级分中观察到两种亲雄激素蛋白,并比较了各种甾体对这两个级分结合的抑制率。各种化合物在IgG级分中的抑制率通常高于空体积级分。当配体和抑制剂在通过Sephadex色谱分级分离之前与胞浆一起孵育时,抑制率低于配体和抑制剂在色谱分离后与级分反应时获得的抑制率。目前这两个实验中观察到的差异的意义尚不清楚。鱼精蛋白沉淀实验得到的结果与使用未分级的丙酮干燥胞浆提取物的实验结果几乎相同,因此,鱼精蛋白方法似乎不能特异性沉淀组织特异性亲雄激素蛋白。

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Inhibition of testosterone metabolism in the human prostate.抑制人体前列腺中的睾酮代谢。
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