Select dietary phytochemicals function as inhibitors of COX-1 but not COX-2

PLoS One. 2013 Oct 3;8(10):e76452. doi: 10.1371/journal.pone.0076452. eCollection 2013.

Abstract

Recent clinical trials raised concerns regarding the cardiovascular toxicity of selective cyclooxygenase-2 (COX-2) inhibitors. Many active dietary factors are reported to suppress carcinogenesis by targeting COX-2. A major question was accordingly raised: why has the lifelong use of phytochemicals that likely inhibit COX-2 presumably not been associated with adverse cardiovascular side effects. To answer this question, we selected a library of dietary-derived phytochemicals and evaluated their potential cardiovascular toxicity in human umbilical vein endothelial cells. Our data indicated that the possibility of cardiovascular toxicity of these dietary phytochemicals was low. Further mechanistic studies revealed that the actions of these phytochemicals were similar to aspirin in that they mainly inhibited COX-1 rather than COX-2, especially at low doses.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • 6-Ketoprostaglandin F1 alpha / pharmacology
  • Animals
  • Cell Line
  • Cell Survival / drug effects
  • Cyclooxygenase 1 / genetics
  • Cyclooxygenase 1 / metabolism*
  • Cyclooxygenase 2 / genetics
  • Cyclooxygenase 2 / metabolism*
  • Cyclooxygenase Inhibitors / pharmacology*
  • Cyclooxygenase Inhibitors / toxicity
  • Enzyme Activation / drug effects
  • Human Umbilical Vein Endothelial Cells / drug effects
  • Human Umbilical Vein Endothelial Cells / metabolism
  • Humans
  • Inhibitory Concentration 50
  • Mice
  • Mice, Knockout
  • Nitric Oxide / biosynthesis
  • Phytochemicals / pharmacology*
  • Phytochemicals / toxicity
  • Thromboxane B2 / pharmacology

Substances

  • Cyclooxygenase Inhibitors
  • Phytochemicals
  • Nitric Oxide
  • Thromboxane B2
  • 6-Ketoprostaglandin F1 alpha
  • Cyclooxygenase 1
  • Cyclooxygenase 2