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|Title: ||Anti-inflammatory potential of 2-styrylchromones regarding their interference with arachidonic acid metabolic pathways|
|Authors: ||Gomes, Ana|
Santos, Clementina M.M.
Lima, José Costa
|Issue Date: ||2009|
|Citation: ||Gomes, Ana; Fernandes, Eduarda; Silva, Artur; Pinto, Diana; Santos, Clementina; Cavaleiro, José; Costa Lima, José (2009) - Anti-inflammatory potential of 2-styrylchromones regarding their interference with arachidonic acid metabolic pathways. Biochemical Pharmacology. ISSN 0006-2952. 78:2, p. 171-177|
|Abstract: ||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
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
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.|
|Peer Reviewed: ||yes|
|Publisher version: ||http://www.sciencedirect.com/science/journal/00062952|
|Appears in Collections:||PTV - Artigos em Revistas Indexados ao ISI|
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