Table 1

Tranilast does not inhibit prostaglandin synthesis by rh-COX enzymes in transfected COS-1 cells

Drug% Product% Inhibition PG Synthesis
COX-INo inhibitor3.1321.1218.830
10 μM flurbiprofen0.60.250.09483
50 μM tranilast3.4221.0719.83−5
200 μM tranilast6.5724.0718.16−8
COX-IINo inhibitor12.7747.1222.730
10 μM flurbiprofen1.573.623.3786
50 μM tranilast12.5547.422.60
200 μM tranilast9.2243.9819.1710

Values given are the percentage of total radiolabeled product generated by COS-1 cells transfected with COX-I or -II after incubation with 10 μM [1-14C]AA. Assays in intact cells were carried out as described under Materials and Methods. Prior to the addition of radiolabeled substrate, the cells were incubated with either vehicle, flurbiprofen (10 μM), or tranilast (50 and 200 μM). Reactions were terminated after 10 min at 37°C and supernatants were extracted and subjected to TLC.