P P Golikov, A S Bobkova, A V Kamernitzky, I G Reshetova
{"title":"Effect of transformed steroid compounds on mRNA synthesis and glucocorticoid-receptor interaction in the thymocytes of adrenalectomized rats.","authors":"P P Golikov, A S Bobkova, A V Kamernitzky, I G Reshetova","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p>","PeriodicalId":11605,"journal":{"name":"Endokrinologie","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"1982-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Endokrinologie","FirstCategoryId":"1085","ListUrlMain":"","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
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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.
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