title: 5-Arylidene-4-thiazolidinone derivatives active as antidegenerative agents on human chondrocyte cultures.
abstract: 5-Arylidene-2-oxo-4-thiazolidinones and 2-phenylimino analogues were evaluated for their antidegenerative activity on human chondrocyte cultures stimulated by IL-1β and for their inhibitory capability against matrix metalloproteinase- 13. Our results indicated that 5-arylidene-4-thiazolidinone derivatives 1-9 exhibit antidegenerative activity and could block multiple cartilage destruction during the osteoarthritic process. Out of the selected compounds, (5-arylidene- 2,4-dioxothiazolidin-3-yl)acetic acids 7-9 showed significant effectiveness in reducing NO release and restoring normal levels of GAGs in chondrocytes treated with IL-1β. Moreover, benzoic acids 1, 5 and 6 proved to be effective MMP-13 inhibitors and were able to restore normal levels of GAGs.
authors: Dipartimento di Scienze del Farmaco, Faculty of Pharmacy, University of Catania, V.le A. Doria 6, 95125 Catania, Italy.
authors: Annamaria
authors: A
authors: Panico
authors: Rosanna
authors: R
authors: Maccari
authors: Venera
authors: V
authors: Cardile
authors: Lucia
authors: L
authors: Crasci
authors: Simone
authors: S
authors: Ronsisvalle
authors: Rosaria
authors: R
authors: Ottanà
mesh_terms: D001565:Benzoates / Q000737:chemistry / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D019902:Chondrocytes / Q000187:drug effects*; D004789:Enzyme Activation / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D053509:Matrix Metalloproteinase 13 / Q000378:metabolism; D061965:Matrix Metalloproteinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D015394:Molecular Structure; D045162:Thiazolidinediones / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D001565:Benzoates; D061965:Matrix Metalloproteinase Inhibitors; D045162:Thiazolidinediones; D053509:Matrix Metalloproteinase 13