12-Lipoxygenase inhibition induced apoptosis in human gastric cancer cells

Carcinogenesis. 2001 Sep;22(9):1349-54. doi: 10.1093/carcin/22.9.1349.

Abstract

Arachidonic acid release from membrane phospholipids is essential for tumour cell proliferation. Lipoxygenases constitute a pathway for arachidonate metabolism. The present study investigated the expression of 12-lipoxygenase and its effect on cell proliferation as well as survival in two human gastric cancer cell lines (AGS and MKN-28). RT-PCR and western blots, respectively, showed 12-LOX mRNA and protein expression in both AGS and MKN-28 cell lines. Treatment with a 12-LOX inhibitor, baicalein, significantly inhibited cancer cell proliferation, but a metabolite of 12-LOX activity, 12 hydroxyeicosatetraenoic acid (12-HETE) reversed baicalein-induced growth inhibition. Furthermore, the blockade of the 12-LOX pathway through a 12-LOX inhibitor and antisense induced apoptosis of gastric cancer cell lines. The biochemical characteristics of apoptosis were p53-independent combined with a decrease in bcl-2 expression. Caspase-7 was proteolytically activated and responsible for the apoptosis execution.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 12-Hydroxy-5,8,10,14-eicosatetraenoic Acid / pharmacology
  • Apoptosis / drug effects*
  • Apoptosis / physiology
  • Arachidonate 12-Lipoxygenase / biosynthesis
  • Arachidonate 12-Lipoxygenase / genetics
  • Blood Platelets / enzymology
  • Blotting, Western
  • Caspase 3
  • Caspase 7
  • Caspases / metabolism
  • Cell Division / drug effects
  • Cell Division / physiology
  • Drug Interactions
  • Flavanones*
  • Flavonoids / pharmacology*
  • Gene Expression Regulation, Neoplastic / drug effects
  • Growth Inhibitors / pharmacology
  • Humans
  • Lipoxygenase Inhibitors* / pharmacology*
  • RNA, Messenger / biosynthesis
  • RNA, Messenger / genetics
  • Stomach Neoplasms / enzymology
  • Stomach Neoplasms / pathology*
  • Tumor Cells, Cultured

Substances

  • Flavanones
  • Flavonoids
  • Growth Inhibitors
  • Lipoxygenase Inhibitors
  • RNA, Messenger
  • baicalein
  • 12-Hydroxy-5,8,10,14-eicosatetraenoic Acid
  • Arachidonate 12-Lipoxygenase
  • CASP3 protein, human
  • CASP7 protein, human
  • Caspase 3
  • Caspase 7
  • Caspases