FPHPB inhibits gastric tumor cell proliferation by inducing G2-M cell cycle arrest

Biomed Pharmacother. 2018 Feb:98:694-700. doi: 10.1016/j.biopha.2017.12.106. Epub 2018 Jan 4.

Abstract

Gastric cancer is a common cancer in the world with high morbidity and mortality. Here, we report that FPHPB (4-(4-(2-fluoropyridin-3-yl)phenyl)-N-(4-hydroxyphenyl)), a derivative of CMPD-1/MK2a Inhibitor, had anti-tumor activities by inhibiting gastric tumor SNU-16 and SGC7901 cells. FPHPB dose-dependently inhibited cell proliferation, induced cell apoptosis and arrested SNU-16 and SGC7901 cells in G2-M cell cycle checkpoint. Upon treatment with FPHPB, apoptotic proteins cleaved PARP and cleaved caspase-3 were remarkably increased, and G2-M regulatory molecules, the phosphorylation of Cdc2 and Chk2, were significantly accentuated. Collectively, FPHPB has anti-tumor activities and may be a potential candidate for treating gastric cancers.

Keywords: Apoptosis; Cell cycle; FPHPB; Gastric tumor cells; Proliferation.

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects
  • CDC2 Protein Kinase / metabolism
  • Caspase 3 / metabolism
  • Cell Cycle Checkpoints / drug effects*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects*
  • G2 Phase Cell Cycle Checkpoints / drug effects*
  • Humans
  • Phosphorylation / drug effects
  • Stomach Neoplasms / drug therapy*
  • Stomach Neoplasms / metabolism

Substances

  • Antineoplastic Agents
  • CDC2 Protein Kinase
  • Caspase 3