Antitumor effects of the novel quinazolinone MJ-33: inhibition of metastasis through the MAPK, AKT, NF-κB and AP-1 signaling pathways in DU145 human prostate cancer cells

Int J Oncol. 2012 Oct;41(4):1513-9. doi: 10.3892/ijo.2012.1560. Epub 2012 Jul 18.

Abstract

Quinazolinone compounds have been shown to have antitumor activity in many human cancer cell lines. In the present study, we investigated the anti-metastatic activity of MJ-33 (2-(3-ethoxyphenyl)-6-pyrrolidinylquinazolinone), a novel quinazolinone derivate, and the signaling pathway of MJ-33 in human prostate cells. MJ-33 exhibited a growth inhibitory effect on DU145, LNCaP and PC-3 cells by MTT assay. DU145 cells showed greater sensitivity to the growth inhibition of MJ-33 than that of LNCaP and PC-3 cells. MJ-33 also had an inhibitory effect on the invasion, migration and adhesion of DU145 cells using Boyden chamber transwell assays, wound-healing and adhesion assay. In addition, MJ-33 inhibited cell metastasis through the reduction of matrix metalloproteinase-2 (MMP-2), matrix metalloproteinase-9 (MMP-9) and urokinase-type plasminogen activator (u-PA) enzyme activities and protein levels by gelatin zymography assay and western blot analysis, respectively. MJ-33 reduced the protein levels of p-JNK, p-p38, p-ERK, p-AKT and nuclear NF-κB (p65), c-fos and c-Jun protein levels by western blotting. Using electrophoretic mobility-shift assay (EMSA), we demonstrated that MJ-33 blocked the activation of transcription factor AP-1 (activator protein-1) and NF-κB, which led to the inhibition of MMP-2 and MMP-9 expression. Collectively, our data showed that MJ-33 decreased protein levels of MAPKs (mitogen-activated protein kinases), AKT, AP-1 and NF-κB, resulting in the inhibition of matrix metalloproteinases. Downregulation of MMP-2 and MMP-9 reduces the invasion, migration and adhesion activities of DU145 cells. MJ-33 may be a promising agent against prostate cancer metastasis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Adhesion / drug effects
  • Gene Expression Regulation, Neoplastic / drug effects
  • Glycerophosphates / administration & dosage*
  • Humans
  • MAP Kinase Signaling System / drug effects
  • Male
  • Matrix Metalloproteinase 2 / biosynthesis
  • Matrix Metalloproteinase 2 / metabolism
  • Matrix Metalloproteinase 9 / biosynthesis
  • Matrix Metalloproteinase 9 / metabolism
  • NF-kappa B / metabolism
  • Neoplasm Metastasis / drug therapy*
  • Neoplasm Metastasis / pathology
  • Oncogene Protein v-akt / metabolism*
  • Prostatic Neoplasms / drug therapy*
  • Prostatic Neoplasms / pathology
  • Quinazolinones / administration & dosage
  • Signal Transduction / drug effects
  • Transcription Factor AP-1 / metabolism*

Substances

  • Glycerophosphates
  • NF-kappa B
  • Quinazolinones
  • Transcription Factor AP-1
  • 1-hexadecyl-3-trifluoroethylglycero-sn-2-phosphomethanol
  • Oncogene Protein v-akt
  • Matrix Metalloproteinase 2
  • Matrix Metalloproteinase 9