Carbenoxolone disodium suppresses the migration of gastric cancer by targeting HDAC6

Future Med Chem. 2023 Feb;15(4):333-344. doi: 10.4155/fmc-2022-0246. Epub 2023 Mar 22.

Abstract

Aim: Because of the severe morbidity and mortality of gastric cancer, discovering new candidate drugs has been an urgent issue. The close association between histone deacetylase 6 (HDAC6) and gastric cancer makes the development of HDAC6-targeted anti-gastric cancer drugs a viable idea. Methods & results: Carbenoxolone disodium was identified as a novel HDAC6 inhibitor. Cellular thermal shift assay, surface plasmon resonance assay and molecular docking confirmed its binding ability to HDAC6. Cell viability, wound healing and transwell assays as well as animal studies have demonstrated that carbenoxolone disodium could block the proliferation and migration of gastric cancer cells MGC-803 in vitro and in vivo. Conclusion: This is the first report to indicate that carbenoxolone disodium could be an HDAC6 inhibitor with potential for treatment of gastric cancer.

Keywords: HDAC6; carbenoxolone disodium; gastric cancer; migration.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Carbenoxolone
  • Histone Deacetylase 6
  • Histone Deacetylase Inhibitors / chemistry
  • Histone Deacetylase Inhibitors / pharmacology
  • Histone Deacetylases* / metabolism
  • Molecular Docking Simulation
  • Neoplasms*

Substances

  • Histone Deacetylase 6
  • Histone Deacetylases
  • Carbenoxolone
  • Histone Deacetylase Inhibitors