Anti-tumor effect of 4-Amino-2-Trifluoromethyl-Phenyl Retinate on human breast cancer MCF-7 cells via up-regulation of retinoid receptor-induced gene-1

Biomed Pharmacother. 2013 Oct;67(8):687-92. doi: 10.1016/j.biopha.2013.05.001. Epub 2013 Jun 11.

Abstract

4-Amino-2-Trifluoromethyl-Phenyl Retinate (ATPR) is one of the retinoid derivatives designed and synthesized in our team. In this paper, we explored the potential anti-tumor effects of ATPR in breast cancer. Here we found that ATPR showed remarkable anti-proliferative effects in a dose- and time-dependent manner, caused cell cycle arrest in the G0/G1 phase and significantly increased the expression of retinoid receptor-induced gene-1 (RRIG1). ATPR decreased the expression of phosphorylation-ERK (p-ERK) and increased the expression of estrogen receptor β (ERβ) and phosphorylation-p38 (p-p38). Following RRIG1 knockdown by RNAi interference, we found that the changes of ERβ, p-ERK and p-p38 induced by ATPR were both depressed. Our data suggest that ATPR could inhibit the proliferation and induce differentiation of MCF-7 cells via mediating the expression of RRIG1.

Keywords: ATPR; Breast cancer cells; Estrogen receptors; MAPK pathway; RNA interference; Retinoid receptor-induced gene-1.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Blotting, Western
  • Breast Neoplasms* / genetics
  • Breast Neoplasms* / pathology
  • Cell Culture Techniques
  • Cell Cycle Checkpoints / drug effects*
  • Cell Proliferation / drug effects*
  • Dose-Response Relationship, Drug
  • Female
  • Humans
  • MCF-7 Cells
  • Membrane Proteins / genetics*
  • Molecular Structure
  • RNA, Small Interfering / genetics
  • Retinoids / chemistry
  • Retinoids / pharmacology*
  • Reverse Transcriptase Polymerase Chain Reaction
  • Time Factors
  • Tumor Suppressor Proteins / genetics*
  • Up-Regulation

Substances

  • 4-amino-2-trifluoromethyl-phenyl retinate
  • Antineoplastic Agents
  • Membrane Proteins
  • RNA, Small Interfering
  • RRIG1 protein, human
  • Retinoids
  • Tumor Suppressor Proteins