Androgen receptor or estrogen receptor-beta blockade alters DHEA-, DHT-, and E(2)-induced proliferation and PSA production in human prostate cancer cells

Prostate. 2007 Aug 1;67(11):1152-62. doi: 10.1002/pros.20585.

Abstract

Background: Dehydroepiandrosterone (DHEA) is an endogenous steroid that is metabolized to androgens and/or estrogens in the human prostate. DHEA levels decline with age, and use of DHEA supplements to retard the aging process is of unproved effectiveness and safety. LNCaP and LAPC-4 prostate cancer cells were used to determine whether DHEA-modulated proliferation and prostate specific antigen (PSA) production were mediated via the androgen receptor (AR) and/or ERbeta.

Methods: Cells were treated with DHEA, DHT, or E(2) and antagonists to AR (Casodex-bicalutamide) or ER (ICI 182,780) or siRNA to the respective receptors. Proliferation was assessed by MTT assay and PSA mRNA and protein secretion were measured by quantitative real-time PCR and ELISA. Associations of AR and ERbeta were analyzed by co-immunoprecipitation studies and fluorescent confocal microscopy.

Results: DHEA-, T-, and E(2)-induced proliferation of LNCaP cells was blunted by Casodex but not by ICI treatment. In LNCaP cells, Casodex and ICI suppressed hormone-induced PSA production. In LAPC-4 cells, DHT-stimulated PSA mRNA was inhibited by Casodex and ICI, and the minimal stimulation by DHEA was inhibited by ICI. Use of siRNAs confirmed involvement of AR and ERbeta in hormone-induced PSA production while AR-ERbeta co-association was suggested by immunoprecipitation and nuclear co-localization.

Conclusions: These findings support involvement of both AR and ERbeta in mediating DHEA-, DHT-, and E(2)-induced PSA expression in prostate cancer cells.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, N.I.H., Intramural

MeSH terms

  • Androgen Antagonists / pharmacology
  • Androgen Receptor Antagonists*
  • Anilides / pharmacology
  • Cell Division / drug effects
  • Cell Line, Tumor
  • Dehydroepiandrosterone / pharmacology*
  • Estradiol / analogs & derivatives
  • Estradiol / pharmacology
  • Estrogen Antagonists / pharmacology
  • Estrogen Receptor beta / antagonists & inhibitors*
  • Estrogen Receptor beta / physiology
  • Fulvestrant
  • Gene Expression / drug effects
  • Humans
  • Male
  • Nitriles / pharmacology
  • Prostate-Specific Antigen / biosynthesis*
  • Prostate-Specific Antigen / genetics
  • Prostate-Specific Antigen / metabolism
  • Prostatic Neoplasms / metabolism
  • Prostatic Neoplasms / pathology*
  • RNA, Messenger / analysis
  • RNA, Small Interfering / pharmacology
  • Receptors, Androgen / physiology
  • Testosterone / analogs & derivatives*
  • Testosterone / pharmacology
  • Tosyl Compounds / pharmacology

Substances

  • Androgen Antagonists
  • Androgen Receptor Antagonists
  • Anilides
  • Estrogen Antagonists
  • Estrogen Receptor beta
  • Nitriles
  • RNA, Messenger
  • RNA, Small Interfering
  • Receptors, Androgen
  • Tosyl Compounds
  • Fulvestrant
  • Testosterone
  • Dehydroepiandrosterone
  • Estradiol
  • boldenone
  • bicalutamide
  • Prostate-Specific Antigen