Selective inhibition of cyclooxygenase-1 and -2 using intact insect cell assays

Biochem Pharmacol. 1996 Dec 13;52(11):1777-85. doi: 10.1016/s0006-2952(96)00599-0.


We have utilized the baculovirus expression system to develop an in vitro intact cell assay for screening nonsteroidal anti-inflammatory drug (NSAID) inhibition of the two isozymes of human cyclooxygenase (prostaglandin endoperoxidase synthase, EC Infected Spodoptera frugiperda (sf9) cells expressing either human cyclooxygenase-1 (hCOX-1) or human cyclooxygenase-2 (hCOX-2) were harvested 24 hr postinfection, a time point where all cells are viable and hCOX-1 or hCOX-2 are correctly processed. Cells were distributed to a 96-well plate, preincubated with various NSAIDs, and challenged with 10 microM arachidonic acid; then cyclooxygenase activity was assessed indirectly by prostaglandin E2-specific radioimmunoassay. The rank order of potency of NSAID-mediated inhibitions of hCOX-1 and hCOX-2 paralleled those that have been observed in other cell systems. This sf9 cell-based assay can be utilized for the identification of potent and selective inhibitors of hCOX-1 and/or hCOX-2. Compounds that preferentially inhibit hCOX-2 may provide novel NSAIDs that reduce inflammation while sparing the stomach and kidneys of toxic side-effects seen with current nonselective NSAIDs.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Cells, Cultured
  • Cyclooxygenase Inhibitors / pharmacology*
  • Isoenzymes / antagonists & inhibitors*
  • Prostaglandin-Endoperoxide Synthases / biosynthesis
  • Recombinant Proteins / biosynthesis
  • Spodoptera


  • Anti-Inflammatory Agents, Non-Steroidal
  • Cyclooxygenase Inhibitors
  • Isoenzymes
  • Recombinant Proteins
  • Prostaglandin-Endoperoxide Synthases