Golikov P P, Bobkova A S, Kamernitskiĭ A V, Reshetova I G
Farmakol Toksikol. 1982 Mar-Apr;45(2):89-93.
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.
对肾上腺切除大鼠的胸腺细胞培养进行了实验,以研究50种含有A环上δ4-3-酮基或δ5-3-羟基、D环上含氧取代基以及构建的20-酮侧链的转化甾体化合物对糖皮质激素和抗糖皮质激素作用以及甾体-受体相互作用的影响。10种浓度为10⁻⁶ M的化合物与³H-曲安西龙竞争结合胸腺细胞胞质溶胶中的糖皮质激素受体。与含有δ5-3-羟基的化合物相比,含有δ4-3-酮基的甾体化合物在浓度为10⁻⁶ M时更能有效抑制³H-尿苷掺入RNA。16,17α-异丙叉二氧基-孕-5-烯-20-酮-3β-醇;16,17α-异丙叉二氧基-孕甾-5,21(21a)-二烯-20-酮-3β-醇在浓度为10⁻⁶ M时也对胸腺细胞功能产生抗糖皮质激素作用。