Effect of Dietary Stilbenes on 5-Lipoxygenase and Cyclooxygenases Activities In Vitro

Abstract

Stilbenes contained in various foods are associated with health beneficial effects. In this study six natural and one synthetic stilbene were tested for their potential to regulate the activity of lipoxygenase and cyclooxygenase in vitro. The most potent inhibitor of 5-lipoxygenase was pterostilbene (IC50 = 9.32 μM), whereas the strongest inhibitor of cyclooxygenase-1 and cyclooxygenase-2 was pinostilbene (IC50s = 1.90 and 0.35 μM, respectively). Pterostilbene (IC50s = 11.70 and 27.04 μM for cyclooxygenase-1 and cyclooxygenase-2, respectively) and oxyresveratrol (IC50s = 18.49; 2.79 and 14.71 μM for 5-lipoxygenase, cyclooxygenase-1, and cyclooxygenase-2, respectively) were capable to inhibit catalytic activity of all three tested enzymes. Isorhapontigenin (IC50s = 8.81 and 24.00 μM for cyclooxygenase-1 and cyclooxygenase-2, respectively) and rhapontigenin (IC50s = 24.55 and 36.12 μM for cyclooxygenase-1 and cyclooxygenase-2, respectively) were only moderate or weak inhibitors of both cyclooxygenase forms. In summary, these results indicated that besides the known cyclooxygenase inhibitor resveratrol also other natural stilbenes could be potent inhibitors of the arachidonic acid pathway and deserve further attention as compounds with promising health benefits.