Effect of transformed steroid compounds on mRNA synthesis and glucocorticoid-receptor interaction in the thymocytes of adrenalectomized rats.

Endokrinologie Pub Date : 1982-07-01
P P Golikov, A S Bobkova, A V Kamernitzky, I G Reshetova
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Abstract

In tests on a thymocyte culture from adrenalectomized rats, we studied the effect of fifty synthetized transformed steroid compounds, containing delta 4-keto-or delta 5-3-oxygroups in ring A, oxygen containing substituents in ring D, and a superstructured 20-keto side chain, on the glucocorticoid and antiglucocorticoid effects and steroid-receptor interaction. Ten compounds (conc. 10(-6)M) competed with 3H-triamcinolone acetonide for binding the thymocytes over the cytosol glucocorticoid receptor. Steroid compounds containing a delta 4-3-ketogroup (conc. 10(-6)M) suppress inclusion of 3H-uridine in thymocyte RNA more than compounds containing a delta 5-3-oxygroup. An antiglucocorticoid effect on thymocyte function is produced by 16,17 alpha-isopropylidendioxy-21-methylidene-pregn-5-en-3 beta-ol-20-one, 16,17 alpha-isopropylidendioxy-pregn-5-en-3 beta-ol-20-one and 16,17 alpha-isopropylidendioxy-21 a-methyl-21, [21a]-epoxy-21-homopregn-4-en-3, 20-dione at concentration of 10(-6) M.

转化类固醇化合物对去肾上腺大鼠胸腺细胞mRNA合成及糖皮质激素受体相互作用的影响。
在肾上腺切除大鼠的胸腺细胞培养实验中,我们研究了50种合成的转化类固醇化合物对糖皮质激素和抗糖皮质激素作用以及类固醇受体相互作用的影响,这些化合物在a环中含有4-酮或5-3-氧基,在D环中含有氧取代基,在超结构的20-酮侧链中。十种化合物(conc)10(-6)M)与3h -曲安奈德在胞浆糖皮质激素受体上结合胸腺细胞竞争。含有4-3-酮基的甾类化合物。10(-6)M)比含有5-3-氧基的化合物更能抑制胸腺细胞RNA中3h -尿苷的包涵。16,17 α -异丙基二氧基-21-甲基-孕酮-5-en-3 - β -醇-20- 1,16,17 α -异丙基二氧基-孕酮-5-en-3 - β -醇-20- 1和16,17 α -异丙基二氧基-21- a-甲基-21,[21a]-环氧-21-homopregn-4-en- 3,20 -二酮在10(-6)M浓度下对胸腺细胞功能产生抗糖皮质激素作用。
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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