Effect of transformed steroid compounds on mRNA synthesis and glucocorticoid-receptor interaction in the thymocytes of adrenalectomized rats.
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.
D000315:Adrenalectomy; D000818:Animals; D008214:Lymphocytes / Q000187:drug effects* / Q000378:metabolism; D008297:Male; D012333:RNA, Messenger / Q000096:biosynthesis*; D051381:Rats; D011965:Receptors, Glucocorticoid / Q000378:metabolism*; D011987:Receptors, Steroid / Q000378:metabolism*; D013256:Steroids / Q000494:pharmacology*
D012333:RNA, Messenger; D011965:Receptors, Glucocorticoid; D011987:Receptors, Steroid; D013256:Steroids