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

Figures & data

TABLE 1 IC₅₀ values of stilbenes and reference inhibitors on COX-1, COX-2, and 5-LO

	IC50 (μM)^a
Compound	COX-1	COX-2	Ratio COX-1/COX-2	IC50 (μM) 5-LO
resveratrol	2.27 ± 1.17	3.40 ± 0.50	0.67	>50
oxyresveratrol	2.79 ± 0.94	14.71 ± 8.07	0.18	18.49 ± 7.79
pinostilbene	1.90 ± 1.61	0.35 ± 0.23	5.42	>50
pterostilbene	11.70 ± 5.56	27.04 ± 15.68	0.43	9.32 ± 3.32
rhapontigenin	24.55 ± 10.38	36.12 ± 10.43	0.68	>50
isorhapontigenin	8.81 ± 3.75	24.00 ± 11.16	0.37	>50
TMS	>50	>50		>50
ibuprofen	13.14 ± 3.84	8.77 ± 2.55	1.49	nt^b
indomethacin	1.61 ± 0.72	10.12 ± 5.66	0.15	nt
zileuton	nt	nt		4.23 ± 3.00

^aMean ± SD of three independent tests with two replicates;

^bnot tested.

FIGURE 1 Structures of tested compounds.

FIGURE 2 Docking pose of pinostilbene in COX-2. Spheres signify hydrophobic interactions with the binding pocket. The arrows pointing from protein structure to pinostilbene signify a hydrogen bond acceptor. The arrows pointing from pinostilbene to protein structure signify hydrogen bond donor interaction.