[HSP90 Inhibitor 17-AAG Inhibits Multiple Myeloma Cell Proliferation by Down-regulating Wnt/β-Catenin Signaling Pathway]

Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2016 Feb;24(1):117-21. doi: 10.7534/j.issn.1009-2137.2016.01.023.
[Article in Chinese]

Abstract

Objective: To investigate the inhibitory effect of HSP90 inhibitory 17-AAG on proliferation of multiple myeloma cells and its main mechanism.

Methods: The multiple myeloma cells U266 were treated with 17-AAG of different concentrations (200, 400, 600 and 800 nmol/L) for 24, 48, and 72 hours respectively, then the proliferation rate, expression levels of β-catenin and C-MYC protein, as well as cell cycle of U266 cells were treated with 17-AAG and were detected by MTT method, Western blot and flow cytometry, respectively.

Results: The 17-AAG showed inhibitory effect on the proliferation of U266 cells in dose- and time-depetent manners (r = -0.518, P < 0.05 and r = -0.473, P < 0.05), while the culture medium without 17-AAG displayed no inhibitory effect on proliferation of U266 cells (P > 0.05). The result of culturing U266 cells for 72 hours by 17-AAG of different concentrations showed that the more high of 17-AAG concentration, the more low level of β-catenin and C-MYC proteins (P < 0.05); At same time of culture, the more high of 17-AAG concentration, the more high of cell ratio in G1 phase (P < 0.05), at same concentration of 17-AAG, the more long time of culture, the more high of cell ratio in G1 phase (P < 0.05).

Conclusion: The HSP90 inhibitory 17-AAG can inhibit the proliferation of multiple myeloma cells, the down-regulation of Wnt/β-catenin signaling pathway and inhibition of HSP90 expression may be the main mechnisms of 17-AAG effect.

MeSH terms

  • Apoptosis
  • Benzoquinones / pharmacology*
  • Cell Cycle
  • Cell Division
  • Cell Line, Tumor / drug effects
  • Cell Proliferation / drug effects
  • Down-Regulation
  • HSP90 Heat-Shock Proteins / antagonists & inhibitors*
  • Humans
  • Lactams, Macrocyclic / pharmacology*
  • Multiple Myeloma / metabolism
  • Multiple Myeloma / pathology*
  • Proto-Oncogene Proteins c-myc / metabolism
  • Wnt Signaling Pathway / drug effects*
  • beta Catenin / metabolism

Substances

  • Benzoquinones
  • CTNNB1 protein, human
  • HSP90 Heat-Shock Proteins
  • Lactams, Macrocyclic
  • Proto-Oncogene Proteins c-myc
  • beta Catenin
  • tanespimycin