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Title: Anti-inflammatory potential of 2-styrylchromones regarding their interference with arachidonic acid metabolic pathways
Author: Gomes, Ana
Fernandes, Eduarda
Silva, Artur
Pinto, Diana
Santos, Clementina M.M.
Cavaleiro, José
Lima, José Costa
Keywords: 2-Styrylchromones
Leukotriene B4
Dual inhibitors
Issue Date: 2009
Publisher: Elsevier
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 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.
Peer review: yes
ISSN: 0006-2952
Publisher Version:
Appears in Collections:PTV - Artigos em Revistas Indexados ao ISI/Scopus

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