Cyclooxygenases (COXs) are the key enzymes in the biosynthesis of prostanoids. COX-1 is a constitutive
enzyme while the expression of COX-2 is highly stimulated in the event of inflammatory processes,
leading to the production of large amounts of prostaglandins (PGs), in particular PGE2 and PGI2, which
are pro-inflammatory mediators.
Lipoxygenases (LOXs) are enzymes that produce hydroxy acids and leukotrienes (LTs). 5-LOX
metabolizes arachidonic acid to yield, among other products, LTB4, a potent chemoattractantmediator of
inflammation.
The aim of the present work was to evaluate the anti-inflammatory potential of 2-styrylchromones
(2-SC), a chemical family of oxygen heterocyclic compounds, vinylogues of flavones (2-phenylchromones),
by studying their COX-1 and COX-2 inhibitory capacity as well as their effects on the LTB4
production by stimulated human polymorphonuclear leukocytes (PMNL).
Some of the tested 2-SC were able to inhibit both COX-1 activity and LTB4 production which makes
them dual inhibitors of the COX and 5-LOX pathways. The most effective compounds in this study were
those having structural moieties with proved antioxidant activity (30,40-catechol and 40-phenol
substituted B-rings).
This type of compounds may exhibit anti-inflammatory activity with a wider spectrum than that of
classical non-steroidal anti-inflammatory drugs (NSAIDs) by inhibiting 5-LOX product-mediated
inflammatory reactions, towards which NSAIDs are ineffective.
