Anti-inflammatory potential of 2-styrylchromones regarding their interference with arachidonic acid metabolic pathways

• Type: Article in International Scientific Journal
• Date: 2009

Authors

Ana Gomes (Author) Other; Eduarda Fernandes (Author) FFUP; Artur M S Silva (Author) Other; Diana C G A Pinto (Author) Other; Clementina M M Santos (Author) Other; Jose A S Cavaleiro (Author) Other; Jose L F C Lima (Author) FFUP

Journal

Title: Biochemical Pharmacology

Vol. 78 No. 5

Pages: 171-177

ISSN: 0006-2952

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 32 Citations

Scopus - 36 Citations

Scientific classification

FOS: Medical and Health sciences > Basic medicine

Other information

Authenticus ID: P-003-HG0

DOI: 10.1016/j.bcp.2009.03.028

Abstract (EN): 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 PGE(2) and PGI(2), 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, LTB(4), a potent chemoattractant mediator 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 LTB(4) production by stimulated human polymorphonuclear leukocytes (PMNL). Some of the tested 2-SC were able to inhibit both COX-1 activity and LTB(4) 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 (3',4'-catechol and 4'-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.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 7