Publication
Anti-inflammatory potential of 2-styrylchromones regarding their interference with arachidonic acid metabolic pathways
| dc.contributor.author | Gomes, Ana Sara | |
| dc.contributor.author | Fernandes, Eduarda | |
| dc.contributor.author | Silva, Artur | |
| dc.contributor.author | Pinto, Diana | |
| dc.contributor.author | Santos, Clementina M.M. | |
| dc.contributor.author | Cavaleiro, José | |
| dc.contributor.author | Lima, José Costa | |
| dc.date.accessioned | 2011-04-04T11:02:43Z | |
| dc.date.available | 2011-04-04T11:02:43Z | |
| dc.date.issued | 2009 | |
| dc.description.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. | por |
| dc.description.sponsorship | The authors acknowledge FCT and FEDER financial support for the project POCI/QUI/59284/2004 and the Organic Chemistry Research Unit (no. 62; Univ. Aveiro). Ana Gomes acknowledges FCT and FSE her PhD grant (SFRH/BD/23299/2005). | |
| dc.identifier.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 | por |
| dc.identifier.doi | 10.1016/j.bcp.2009.03.028 | |
| dc.identifier.issn | 0006-2952 | |
| dc.identifier.uri | http://hdl.handle.net/10198/3919 | |
| dc.language.iso | eng | por |
| dc.peerreviewed | yes | por |
| dc.publisher | Elsevier | por |
| dc.subject | 2-Styrylchromones | por |
| dc.subject | Cyclooxygenase | por |
| dc.subject | 5-Lipoxigenase | por |
| dc.subject | Leukotriene B4 | por |
| dc.subject | Dual inhibitors | por |
| dc.subject | Inflammation | por |
| dc.title | Anti-inflammatory potential of 2-styrylchromones regarding their interference with arachidonic acid metabolic pathways | por |
| dc.type | journal article | |
| dspace.entity.type | Publication | |
| oaire.awardURI | info:eu-repo/grantAgreement/FCT/POCI/POCI%2FQUI%2F59284%2F2004/PT | |
| oaire.awardURI | info:eu-repo/grantAgreement/FCT/SFRH/SFRH%2FBD%2F23299%2F2005/PT | |
| oaire.citation.endPage | 177 | por |
| oaire.citation.startPage | 171 | por |
| oaire.citation.title | Biochemical Pharmacology | por |
| oaire.fundingStream | POCI | |
| oaire.fundingStream | SFRH | |
| person.familyName | Santos | |
| person.givenName | Clementina M.M. | |
| person.identifier.ciencia-id | 9018-DB9C-C590 | |
| person.identifier.orcid | 0000-0003-4380-7990 | |
| person.identifier.scopus-author-id | 7201458663 | |
| project.funder.identifier | http://doi.org/10.13039/501100001871 | |
| project.funder.identifier | http://doi.org/10.13039/501100001871 | |
| project.funder.name | Fundação para a Ciência e a Tecnologia | |
| project.funder.name | Fundação para a Ciência e a Tecnologia | |
| rcaap.rights | openAccess | por |
| rcaap.type | article | por |
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