Inhibition by tamoxifen of estrogen-stimulated accumulation of preprolactin messenger ribonucleic acid

Biochimica et Biophysica Acta (BBA) - Nucleic Acids and Protein Synthesis Pub Date : 1981-11-27 DOI:10.1016/0005-2787(81)90025-3

J Spona, H Leibl

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引用次数: 4

Abstract

Estrogens are involved in the stimulation of prolactin synthesis in the rat anterior pituitary. After 5 days of treatment with 17β-estradiol, strong enhancement of [³H]leucine incorporation into prolactin and stimulation of translatable preprolactin mRNA, respectively, were noted. Increase in prolactin synthesis was also found following daily application with estriol and the synthetic estrogen 1,3-dibenzoyloxy-17β-methyl-1,3,5(10)-estratrien-17β-ol (DB-EE2). The antiestrogen tamoxifen (trans-1-(p-β-dimethylaminoethoxyphenyl)-1,2-diphenylbut-1-ene) was demonstrated to inhibit estradiol-stimulated prolactin synthesis. Antagonistic effects of tamoxifen were dose dependent. Low doses of the antiestrogen were already sufficient to suppress 17β-estradiol-enhanced levels of prolactin mRNA. On the other hand, estriol potentiated 17β-estradiol-stimulated levels of serum prolactin and prolactin synthesis. Our results add further information about the transcriptional control by estrogens and demonstrate inhibitory actions of antiestrogens on distinct regulatory levels of protein synthesis in the rat pituitary.

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他莫昔芬抑制雌激素刺激的前催乳素信使核糖核酸积累

雌激素参与刺激大鼠垂体前叶催乳素合成。用17β-雌二醇治疗5天后，我们发现[3H]亮氨酸并入催乳素的能力明显增强，可翻译的泌乳素前mRNA水平明显提高。每日应用雌三醇和合成雌激素1,3-二苯甲酰氧基-17β-甲基-1,3,5(10)-雌二醇-17β-醇(DB-EE2)后，催乳素合成也增加。抗雌激素的他莫昔芬(反式-1-(对-β-二甲胺乙氧基苯基)-1,2-二苯基丁-1-烯)被证明可以抑制雌二醇刺激的催乳素合成。他莫昔芬的拮抗作用呈剂量依赖性。低剂量的抗雌激素已经足以抑制17β-雌二醇增加的催乳素mRNA水平。另一方面，雌三醇增强了17β-雌二醇刺激的血清催乳素水平和催乳素合成。我们的研究结果为雌激素对转录的控制提供了进一步的信息，并证明了抗雌激素对大鼠垂体蛋白合成的不同调节水平的抑制作用。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Biochimica et Biophysica Acta (BBA) - Nucleic Acids and Protein Synthesis

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