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dc.contributor.authorFioravanti, A
dc.contributor.authorTinti, L
dc.contributor.authorPascarelli, NA
dc.contributor.authorDi Capua, A
dc.contributor.authorLamboglia, A
dc.contributor.authorCappelli, A
dc.contributor.authorBiava, M
dc.contributor.authorGiordani, A
dc.contributor.authorNiccolini, S
dc.contributor.authorGaleazzi, M
dc.contributor.authorAnzini, M
dc.date.accessioned2017-08-11T12:30:48Z
dc.date.available2017-08-11T12:30:48Z
dc.date.issued2012
dc.identifier.issn1347-8613
dc.identifier.doi10.1254/jphs.12016FP
dc.identifier.urihttp://hdl.handle.net/10072/343845
dc.description.abstractThe aim of this in vitro study was to examine the possible effect of [2-methyl-5-(4-methylsulphonyl)phenyl-1-phenyl-3-(2-n-propyloxyethyl)]-1H-pyrrole (VA441), a new selective cyclooxygenase (COX)-2 inhibitor, on human osteoarthritic (OA) chondrocyte cultivated in the presence or absence of interleukin-1β (IL-1β). In particular, we assessed the effects of 1 and 10 μM of VA441, celecoxib, and indomethacin on cell viability, COX-2 and inducible nitric oxide synthase (iNOS) gene expression, prostaglandin E2 (PGE2) production, and nitric oxide (NO) and metalloproteinase-3 (MMP-3) release. Furthermore, we carried out morphological assessment by transmission electron microscopy (TEM). The presence of IL-1β led to a significant increase in PGE2, MMP-3, and NO production, as well as a significant increase in gene expression of COX-2 and iNOS. All the drugs tested had a statistically significant inhibitory effect on PGE2 production and gene expression of COX-2 stimulated by IL-1β. VA441 and celecoxib significantly suppressed IL-1β-stimulated MMP-3 and NO and iNOS gene expression in a dose-dependent manner, while indomethacin did not show any significant effect on MMP-3 and NO production or on iNOS gene expression. TEM demonstrated that IL-1β severely alters the structure of chondrocytes; after co-incubation with VA441 or celecoxib, the cells recovered their ultrastructure. Our data suggest that VA441 and celecoxib may have a beneficial effect on chondrocyte metabolism.
dc.description.peerreviewedYes
dc.languageeng
dc.publisherJapanese Pharmacological Society
dc.relation.ispartofpagefrom6
dc.relation.ispartofpageto14
dc.relation.ispartofissue1
dc.relation.ispartofjournalJournal of Pharmacological Sciences
dc.relation.ispartofvolume120
dc.subject.fieldofresearchPharmacology and Pharmaceutical Sciences not elsewhere classified
dc.subject.fieldofresearchPharmacology and Pharmaceutical Sciences
dc.subject.fieldofresearchcode111599
dc.subject.fieldofresearchcode1115
dc.titleIn vitro effects of VA441, a new selective cyclooxygenase-2 inhibitor, on human osteoarthritic chondrocytes exposed to IL-1β
dc.typeJournal article
dc.type.descriptionC1 - Articles
dc.type.codeC - Journal Articles
gro.hasfulltextNo Full Text
gro.griffith.authorDi Capua, Angela


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