Figure 4.

Inhibition of COX-1 activity. Human COX-1 was overexpressed in COS-7 cells. Cells were treated in the absence or presence of different concentrations of the compounds 3, 4, 7, 8 and 9 or ibuprofen prior to the addition of 25 μM arachidonic acid as indicated in the method section. PGE₂ was measured in the supernatant by enzyme immunoassay. Results were expressed as percentage of PGE₂ in arachidonic acid treated samples which was attributed a value of 100. Fitting of curves was done using Grafit software. Results correspond to mean ± S.E.M. for 3 experiments. (Insert) Cells were transfected in suspension with pcDNA3-COX-1 plasmid using Fugene® 6 transfection reagent at a ratio of 3:1 (fugene: DNA). Insert represents Western blot analysis of COX-1 using selective monoclonal COX-1 in untransfected and pcDNA3-COX-1transfected cells.