Mifepristone inhibits IGF-1 signaling pathway in the treatment of uterine leiomyomas

Drug Des Devel Ther. 2019 Sep 3:13:3161-3170. doi: 10.2147/DDDT.S212157. eCollection 2019.

Abstract

Purpose: To investigate the role of IGF-1 signaling pathway in the treatment of uterine leiomyomas with mifepristone.

Patients and methods: From October 2015 to December 2018, 50 patients with uterine leiomyoma were included in this study. Overexpression or siRNA of IGF-1 in primary human uterine leiomyoma cells were treated with or without mifepristone. MTT was used to evaluate cell viability in assays of cell proliferation and cytotoxicity. IGF-1 expression in the cells was measured with real-time RT-PCR and Western blotting and manipulated with lentivirus ectopic overexpression or siRNA silencing.

Results: Inhibition of cell viability by mifepristone was found dependent on drug concentration and treatment time. IGF-1 and phosphorylation-ERK1/2 expression were decreased, while phosphorylation-AKT expression was increased after mifepristone treatment. IGF-1 significantly promoted cell growth, while IGF-1 knockdown and mifepristone showed synergistic inhibition effects on cell growth. The overexpression of IGF-1 reversed the inhibition of cell growth and ERK1/2 phosphorylation but showed no effect on AKT phosphorylation.

Conclusion: Our study for the first time demonstrated that IGF-1 signaling via ERK1/2 appears to be an important target of mifepristone in the treatment of uterine leiomyomas, which may provide a new approach to avoid leiomyoma re-growth after cessation of mifepristone.

Keywords: IGF-1; mifepristone; signal pathway; uterine leiomyomas.

MeSH terms

  • Adult
  • Antineoplastic Agents / pharmacology*
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Drug Screening Assays, Antitumor
  • Female
  • Humans
  • Insulin-Like Growth Factor I / antagonists & inhibitors*
  • Insulin-Like Growth Factor I / genetics
  • Insulin-Like Growth Factor I / metabolism
  • Leiomyoma / drug therapy*
  • Leiomyoma / metabolism
  • Leiomyoma / pathology
  • Mifepristone / pharmacology*
  • Signal Transduction / drug effects*
  • Tumor Cells, Cultured
  • Uterine Neoplasms / drug therapy*
  • Uterine Neoplasms / metabolism
  • Uterine Neoplasms / pathology

Substances

  • Antineoplastic Agents
  • IGF1 protein, human
  • Mifepristone
  • Insulin-Like Growth Factor I