Indole-3-carbinol downregulation of telomerase gene expression requires the inhibition of estrogen receptor-alpha and Sp1 transcription factor interactions within the hTERT promoter and mediates the G1 cell cycle arrest of human breast cancer cells

Carcinogenesis. 2011 Sep;32(9):1315-23. doi: 10.1093/carcin/bgr116. Epub 2011 Jun 21.

Abstract

Indole-3-carbinol (I3C), a naturally occurring hydrolysis product of glucobrassicin from cruciferous vegetables such as broccoli, cabbage and Brussels sprouts, is an anticancer phytochemical that triggers complementary sets of antiproliferative pathways to induce a cell cycle arrest of estrogen-responsive MCF7 breast cancer cells. I3C strongly downregulated transcript expression of the catalytic subunit of the human telomerase (hTERT) gene, which correlated with the dose-dependent indole-mediated G(1) cell cycle arrest without altering the transcript levels of the RNA template (hTR) for telomerase elongation. Exogenous expression of hTERT driven by a constitutive promoter prevented the I3C-induced cell cycle arrest and rescued the I3C inhibition of telomerase enzymatic activity and activation of cellular senescence. Time course studies showed that I3C downregulated expression of estrogen receptor-alpha (ERα) and cyclin-dependent kinase-6 transcripts levels (which is regulated through the Sp1 transcription factor) prior to the downregulation of hTERT suggesting a mechanistic link. Chromatin immunoprecipitation assays demonstrated that I3C disrupted endogenous interactions of both ERα and Sp1 with an estrogen response element-Sp1 composite element within the hTERT promoter. I3C inhibited 17β-estradiol stimulated hTERT expression and stimulated the production of threonine-phosphorylated Sp1, which inhibits Sp1-DNA interactions. Exogenous expression of both ERα and Sp1, but not either alone, in MCF7 cells blocked the I3C-mediated downregulation of hTERT expression. These results demonstrate that I3C disrupts the combined ERα- and Sp1-driven transcription of hTERT gene expression, which plays a significant role in the I3C-induced cell cycle arrest of human breast cancer cells.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anticarcinogenic Agents / pharmacology*
  • Breast Neoplasms / pathology*
  • Cell Line, Tumor
  • Cyclin-Dependent Kinase 6 / genetics
  • Down-Regulation
  • Estrogen Receptor alpha / antagonists & inhibitors
  • Estrogen Receptor alpha / genetics
  • Estrogen Receptor alpha / physiology*
  • Female
  • G1 Phase / drug effects*
  • Gene Expression Regulation
  • Humans
  • Indoles / pharmacology*
  • Phosphorylation
  • Promoter Regions, Genetic*
  • Sp1 Transcription Factor / antagonists & inhibitors
  • Sp1 Transcription Factor / physiology*
  • Telomerase / genetics*

Substances

  • Anticarcinogenic Agents
  • ESR1 protein, human
  • Estrogen Receptor alpha
  • Indoles
  • Sp1 Transcription Factor
  • indole-3-carbinol
  • CDK6 protein, human
  • Cyclin-Dependent Kinase 6
  • TERT protein, human
  • Telomerase