Effects of the beta-isomer of hexachlorocyclohexane on estrogen-sensitive human mammary tumor cells

Toxicol Appl Pharmacol. 1989 Nov;101(2):310-8. doi: 10.1016/0041-008x(89)90279-2.


The effects of the beta-isomer of hexachlorocyclohexane (beta-HCH) on the induction of the cytosolic progesterone receptor (PgRc), on the redistribution of the estrogen receptor (ER), and its affinity for ER were investigated in the estrogen-sensitive human mammary tumor cell line MCF-7. The effects of beta-HCH were compared to those of estradiol-17 beta (E2) and 2,4,6-trichlorophenol (TCP), a major urinary metabolite of beta-HCH in rats. beta-HCH in concentrations higher than 1 microM caused induction of PgRc whereas TCP was essentially without effect up to a cytotoxic concentration of 100 microM. Furthermore, beta-HCH (10 microM) caused redistribution of ER, i.e., decrease of cytosolic ER concentration and increase of nuclear ER concentration, in a way similar to E2. In contrast to this, beta-HCH up to a molar excess of 6 X 10(4) (concentration 30 microM) caused no significant displacement of [3H]E2 from ER indicating that beta-HCH has no substantial affinity for ER. It is concluded that beta-HCH has estrogenic properties which are at variance with the failure to demonstrate binding of beta-HCH to ER.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Biotransformation / drug effects
  • Breast Neoplasms / analysis
  • Breast Neoplasms / metabolism*
  • Cell Nucleus / drug effects
  • Cell Nucleus / metabolism
  • Chlorophenols / pharmacology
  • Cytosol / drug effects
  • Cytosol / metabolism
  • Dose-Response Relationship, Drug
  • Estradiol / pharmacology
  • Female
  • Hexachlorocyclohexane / pharmacology*
  • Humans
  • Rats
  • Receptors, Estrogen / metabolism*
  • Receptors, Progesterone / drug effects
  • Receptors, Progesterone / metabolism
  • Tumor Cells, Cultured / drug effects


  • Chlorophenols
  • Receptors, Estrogen
  • Receptors, Progesterone
  • Estradiol
  • Hexachlorocyclohexane
  • 2,4,6-trichlorophenol
  • beta-hexachlorocyclohexane