Effects of lysine clonixinate on cyclooxygenase I and II in rat lung and stomach preparations

FRANCHI ANA MARIA; DI GIROLAMO GUILLERMO; DE LOS SANTOS AR; MARTI ML; GIMENO MARTA

PROSTAGLANDINS LEUKOTRIENES AND ESSENTIAL FATTY ACIDS

ELSEVIER SCI LTD

Lugar: Amsterdam; Año: 1998 vol. 58 p. 421 - 424

0952-3278

Lysine clonixinate (LC) is a drug of antiinflammatory antipyretic and analgesic activity that produces minordigestive side-effects. This fact induced us to think that LC is possibly a weak COX-1 inhibitor. In order to investigateour hypothesis we inhibited cyclooxygenase activity with LC or indomethacin (INDO) in rat lung and stomach obtainedfrom rats treated with lipopolysacharide (LPS) and control rats. Rat lung preparations incubated with 14C-arachidonicacid synthesise mainly PGE2. LC at 2.5 and 4.1 x 104 M does not modify the basal production of PGE 2 (probablyCOX-l) but at 6.8 x 10 -2 M significantly inhibited PGE2 production (approximately 48.5% inhibition, P < 0.001). On theother hand, INDO at 104 inhibited the basal production of PGE 2 by around 73%. In LPS-treated rats, the production ofPGE2 was significantly higher than in the lungs of control rats, probably due to the induction of COX-2. The addition ofLC at 2.7 and 4.1 x 10 -2 M recovered the control values of PGE2 inhibiting, probably only from COX-2 activity. LC athigher concentrations (6.8 x 10 -2 M) and INDO 104 M inhibited PGE2 formed by COX-2 and also partly by COX-1 activity.