Effect of transformed steroid compounds on mRNA synthesis and glucocorticoid-receptor interaction in thymocytes of adrenalectomized rats
Golikov, P.P.; Bobkova, A.S.; Kamernitskiĭ, A.V.; Reshetova, I.G.
Farmakologiia i Toksikologiia 45(2): 89-93
1982
ISSN/ISBN: 0014-8318 PMID: 7075758 Document Number: 189266
Experiments on thymocyte culture of adrenalectomized rats were made to study the effect of 50 transformed steroid compounds containing delta 4-3-keto or delta 5-3-hydroxygroup in ring A, oxygen-containing substituents in ring D and superstructed 20-keto-side chain on glucocorticoid and antiglucocorticoid effects and steroid-receptor interaction. Ten compounds given in a concentration of 10(6) M competed with 3H-triamcinolon for binding thymocyte cytosol on glucocorticoid receptors. Steroid compounds containing the delta 4-3-ketogroup inhibit more actively the incorporation of 3H-uridine into RNA in a concentration of 10(6) M, as compared with compounds containing the delta 5-3-hydroxygroup. Antiglucocorticoid effect on thymocyte function is also produced by 16,17 alpha-isopropylidenedioxy-pregn-5-en-20-on-3 beta-ol; 16,17 alpha-isopropylidenedioxy-pregna-5,21 (21a)-dien-20-on-3 beta-ol at a concentration of 10(6) M.