Scholarlink

<p>The effect of new progestins of the D′-pentarane series containing an additional three- or six-membered D′ ring in the 16α,17β-positions of the steroid skeleton and oxime groups in the 3- or 6-position on the expression level (amount of mRNA) of genes of progesterone- (mPR, PGRmC1, PR-A, PR-B) and estrogen-steroid (mER, ER<sub>α</sub>, ER<sub>β</sub>) and vitamin D receptors in immunocompetent blood cells of healthy patients was studied. Only pentarane 6(<i>E</i>)-hydroxyimino-16α,17β-cyclohexanopregn-4-en-3β-ol-20-one (K-1044) of the four steroids studied with high progesterone receptor binding did not reduce the level of estrogen receptor ER mRNA, a predictor of the effectiveness of menopausal hormone therapy. The remaining three compounds exhibited pronounced inhibition of ER mRNA expression by 3.5 and 9 times lower than the control values for 6(<i>E</i>)-methoxyimino-16α,17β-cyclohexanopregn-4-en-3-ol-20-one (K-1046) and 16α,17β-cyclopropano-pregn-4-ene-3,20-dione (K-338), respectively, and practically to zero for 3(<i>E</i>)-hydroxyimino-16α,17β-cyclo-hexanopregn-4-ene-3,20-dione (K-993). Also, these four pentaranes not only did not reduce but also increased the expression of vitamin D receptor (VDR) mRNA in peripheral blood mononuclear cells. The effect of pentarane K-1044 was the most significant.</p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Effect of New Progestins of the D′-Pentarane Series on Expression of Estrogen ERβ and Vitamin D Receptor Genes in Immunocompetent Blood Cells

  • 期刊论文

  • 发表日期：

    2026年2月1日

查看全文
  • E. N. Kareva,
  • I. S. Levina,
  • E. V. Krasnoshchok,
  • N. A. Kochina,
  • Yu. V. Kuznetsov,
  • I. V. Zavarzin

摘要

The effect of new progestins of the D′-pentarane series containing an additional three- or six-membered D′ ring in the 16α,17β-positions of the steroid skeleton and oxime groups in the 3- or 6-position on the expression level (amount of mRNA) of genes of progesterone- (mPR, PGRmC1, PR-A, PR-B) and estrogen-steroid (mER, ERα, ERβ) and vitamin D receptors in immunocompetent blood cells of healthy patients was studied. Only pentarane 6(E)-hydroxyimino-16α,17β-cyclohexanopregn-4-en-3β-ol-20-one (K-1044) of the four steroids studied with high progesterone receptor binding did not reduce the level of estrogen receptor ER mRNA, a predictor of the effectiveness of menopausal hormone therapy. The remaining three compounds exhibited pronounced inhibition of ER mRNA expression by 3.5 and 9 times lower than the control values for 6(E)-methoxyimino-16α,17β-cyclohexanopregn-4-en-3-ol-20-one (K-1046) and 16α,17β-cyclopropano-pregn-4-ene-3,20-dione (K-338), respectively, and practically to zero for 3(E)-hydroxyimino-16α,17β-cyclo-hexanopregn-4-ene-3,20-dione (K-993). Also, these four pentaranes not only did not reduce but also increased the expression of vitamin D receptor (VDR) mRNA in peripheral blood mononuclear cells. The effect of pentarane K-1044 was the most significant.