Catecholestrogens are MCF-7 cell estrogen receptor agonists

J Steroid Biochem Mol Biol. 1993 Dec;46(6):781-9. doi: 10.1016/0960-0760(93)90319-r.


Catecholestrogens are important metabolites of estradiol and estrone in the human. Considerable interest has focused on the catecholestrogens 2-hydroxy- and 4-hydroxyestradiol since they bind to the estrogen receptor with an affinity in the range of estradiol. Using the MCF-7 cell line, we analysed the capacity of purified catecholestrogens to transform the estrogen receptor into its high affinity nuclear binding form and to affect receptor-dependent processes such as proliferation and expression of the progesterone receptor (PR). Incubations with 2-hydroxy- and 4-hydroxyestradiol at 10(-8) M for 1 h resulted in tight nuclear binding of the estrogen receptor. During treatment of the cells with catecholestrogens we obtained a marked increase in proliferation rate of 36 and 76% for 2-hydroxy- and 4-hydroxyestradiol, respectively, relative to the inductive effect of estradiol (100%). The PR level, was slightly increased by treatment with 2-hydroxyestradiol (10%), whereas treatment with 4-hydroxyestradiol increased the PR level at 28%, compared to estradiol (100%). From these results we conclude that the 2- and 4-hydroxylated derivatives of estradiol are active hormones and are able to initiate estrogen receptor mediated processes in MCF-7 cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Breast Neoplasms
  • Cell Division / drug effects
  • Cell Nucleus / drug effects
  • Cell Nucleus / metabolism
  • Estradiol / analogs & derivatives*
  • Estradiol / metabolism
  • Estradiol / pharmacology
  • Estrogens, Catechol / pharmacology*
  • Female
  • Humans
  • Kinetics
  • Receptors, Estrogen / drug effects
  • Receptors, Estrogen / metabolism*
  • Receptors, Progesterone / biosynthesis
  • Receptors, Progesterone / drug effects
  • Receptors, Progesterone / metabolism*
  • Tamoxifen / pharmacology
  • Time Factors
  • Tumor Cells, Cultured


  • Estrogens, Catechol
  • Receptors, Estrogen
  • Receptors, Progesterone
  • Tamoxifen
  • Estradiol
  • 2-hydroxyestradiol
  • 4-hydroxyestradiol