Picropodophyllin inhibits type I endometrial cancer cell proliferation via disruption of the PI3K/Akt pathway

Acta Biochim Biophys Sin (Shanghai). 2019 Jul 10;51(7):753-760. doi: 10.1093/abbs/gmz055.

Abstract

The type-I insulin-like growth factor receptor (IGF-IR) is overexpressed in endometrial cancer. High IGF-IR expression was considered as an important prognostic factor for tumor progression. The purpose of this study was to investigate the role and molecular mechanism of IGF-IR inhibitor picropodophyllin (PPP) in the growth and development of endometrial cancer. High expression of IGF-IR was observed in endometrial cancer tissues, as well as in ECC-1 and KLE cell lines. PPP suppressed the number of clones of ECC-1 and KLE cell lines; however, it had no significant effect on HEC-1-A cell line, which expressed lower IGF-IR than ECC-1 and KLE cell lines. Furthermore, PPP reduced cell proliferation capacity, inhibited the IGF-IR mRNA expression, and suppressed protein phosphorylation of IGF-IR and Akt in the three cell lines. In addition, PPP inhibited the protein expression of survivin in KLE cell line after 1 h of exposure, though this effect did not last for prolonged time. In conclusion, IGF-IR was mostly overexpressed in type I endometrial cancer. High IGF-IR expression was an important prognostic factor of tumor progression. PPP mediated the down-regulation of IGF-IR phosphorylation and inhibited cell proliferation via the PI3K/Akt signal pathway. PPP may have the potential to become a clinical treatment target in endometrial carcinoma.

Keywords: cell proliferation; endometrial cancer; picropodophyllin; tissue chip; type-I insulin-like growth factor receptor.

MeSH terms

  • Cell Line, Tumor
  • Cell Proliferation / drug effects*
  • Cell Proliferation / genetics
  • Endometrial Neoplasms / genetics
  • Endometrial Neoplasms / metabolism*
  • Endometrial Neoplasms / pathology
  • Female
  • Gene Expression Regulation, Neoplastic / drug effects
  • Humans
  • Phosphatidylinositol 3-Kinases / metabolism*
  • Phosphorylation / drug effects
  • Podophyllotoxin / analogs & derivatives*
  • Podophyllotoxin / pharmacology
  • Prognosis
  • Proto-Oncogene Proteins c-akt / metabolism*
  • Receptor, IGF Type 1 / antagonists & inhibitors
  • Receptor, IGF Type 1 / genetics
  • Receptor, IGF Type 1 / metabolism
  • Signal Transduction / drug effects*
  • Survivin / genetics
  • Survivin / metabolism

Substances

  • Survivin
  • picropodophyllin
  • Receptor, IGF Type 1
  • Proto-Oncogene Proteins c-akt
  • Podophyllotoxin