u-PA inhibitor amiloride suppresses peritoneal metastasis in gastric cancer

World J Surg Oncol. 2012 Dec 12:10:270. doi: 10.1186/1477-7819-10-270.

Abstract

Background: Peritoneal metastasis in gastric cancer represents a ubiquitous human health problem but effective therapies with limited side effects are still lacking. Although previous research suggested that u-PA was involved in some tumor metastasis such as lung-specific metastasis, the role of u-PA for peritoneal metastasis in gastric cancer is still unclear. The aim of this study was to explore whether selective pharmacological blockade of u-PA is able to affect the peritoneal metastasis of gastric cancer both in vivo and in vitro.

Methods: In the present study, we evaluated the effects and explored the anti-tumor mechanisms of amiloride, a selective u-PA inhibitor, on a panel of gastric cancer cell lines and in a murine model of human gastric cancer MKN45.

Results: The study showed that amiloride significantly inhibited the tumor growth and prolonged the survival of the tumor-bearing mice. In vitro, compared with controls, amiloride could not only significantly down-regulate the mRNA expression and protein level of u-PA from MKN45 cells with dose dependence but also inhibit the adhesion of HMrSV5 cells, migration and invasion of MKN45 cells.

Conclusions: The findings in our current report provide evidence that selective u-PA inhibitor amiloride has potent effects against peritoneal metastasis in gastric cancer, suggesting its possible therapeutic value for the treatment of gastric cancer.

MeSH terms

  • Acid Sensing Ion Channel Blockers / therapeutic use*
  • Amiloride / therapeutic use*
  • Animals
  • Apoptosis / drug effects
  • Blotting, Western
  • Cell Adhesion / drug effects
  • Cell Movement / drug effects
  • Cell Proliferation / drug effects
  • Humans
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Peritoneal Neoplasms / metabolism
  • Peritoneal Neoplasms / prevention & control*
  • Peritoneal Neoplasms / secondary
  • RNA, Messenger / genetics
  • Real-Time Polymerase Chain Reaction
  • Reverse Transcriptase Polymerase Chain Reaction
  • Stomach Neoplasms / metabolism
  • Stomach Neoplasms / pathology
  • Stomach Neoplasms / prevention & control*
  • Tumor Cells, Cultured
  • Urokinase-Type Plasminogen Activator / antagonists & inhibitors*
  • Urokinase-Type Plasminogen Activator / metabolism

Substances

  • Acid Sensing Ion Channel Blockers
  • RNA, Messenger
  • Amiloride
  • Urokinase-Type Plasminogen Activator