In vitro comprehensive analysis of VA692 a new chemical entity for the treatment of osteoarthritis

International Immunopharmacology
Sara CheleschiFrancisco Blanco

Abstract

Selective cyclooxigenase (COX)-2 inhibitors were developed to prevent traditional non-steroidal anti-inflammatory drugs (tNSAIDs) gastro-intestinal adverse effects. VA692, a recently disclosed selective COX-2 inhibitor, structurally related to well-known marketed coxibs, showed anti-inflammatory, and anti-nociceptive properties. The aim of this study was to analyze the anti-inflammatory effect of VA692, in comparison with celecoxib. At this purpose we evaluated the pro-inflammatory cytokines and anti-oxidant enzymes gene expression, apoptosis and ROS production, and PGE2 release in chondrocytes (both primary cultures and immortalized T/C-28a2 cell line) treated with the two drugs. Furthermore, a proteomic analysis has been performed in T/C-28a2 cell line to evaluate modifications in their proteomic profile following drug treatment in presence of IL-1β. Our results demonstrated the anti-inflammatory effect of the novel synthesized VA692, and confirmed those of celecoxib, in counteracting the stimulus of IL-1β in both osteoarthritic (OA) chondrocytes and T/C-28a2 cell line. Furthermore, the data underlined the possible anti-apoptotic and anti-oxidant role of VA692, implying its regulation in superoxide anion production as indicat...Continue Reading

Citations

Oct 23, 2019·International Journal of Molecular Sciences·Sara CheleschiAntonella Fioravanti
Dec 20, 2018·International Journal of Molecular Sciences·Sara CheleschiAntonella Fioravanti
Apr 29, 2020·Drug Design, Development and Therapy·Hui GaoPing Li
May 28, 2020·International Journal of Molecular Sciences·Sara CheleschiAntonella Fioravanti
Feb 22, 2021·Osteoarthritis and Cartilage·M DudekQ-J Meng
Apr 4, 2021·International Journal of Molecular Sciences·Sara CheleschiAntonella Fioravanti

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