Inhibiting PLA 2 activity should, in theory, be an effective approach to control the inflammation. Several naturally occurring polyphenolic compounds have been reported as inhibitors of PLA 2 . Among the naturally occurring polyphenols, catechol (1,2-dihydroxybenzene) possesses antiinflammatory activity. Catechol can inhibit cyclooxygenase and lipo-oxygenase. By means of enzyme kinetic study, it was revealed that catechol can inhibit PLA 2 also. Crystal structure showed that catechol binds to PLA 2 at the opening of the active site cleft. This might stop the entry of substrate into the active site. Hence, catechol can be used as a lead compound for the development of novel anti-inflammatory drugs with PLA 2 as the target.