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5-Arylidene-4-Thiazolidinone Derivatives Active as Antidegenerative Agents on Human Chondrocyte Cultures

[ Vol. 9 , Issue. 1 ]

Author(s):

Annamaria Panico, Rosanna Maccari, Venera Cardile, Lucia Crascì, Simone Ronsisvalle and Rosaria Ottanà   Pages 84 - 90 ( 7 )

Abstract:


5-Arylidene-2-oxo-4-thiazolidinones and 2-phenylimino analogues were evaluated for their antidegenerative activity on human chondrocyte cultures stimulated by IL-1 β 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.

Keywords:

Antidegenerative activity, Anti-inflammatory activity, 5-Arylidene-2-phenylimino-4-thiazolidinones, 5-Arylidene- 4-thiazolidinones, Glycosaminoglycans, Human chondrocytes, Matrix metalloproteinase-13, Nitric oxide

Affiliation:

Dipartimento Farmacochimico, Faculty of Pharmacy, University of Messina, Polo Universitario dell’Annunziata, 98168 Messina, Italy



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