LAUSR

Abstract Casticin, an active compound isolated from Vitex rotundifolia L., was reported to possess anti‐inflammatory activity. However, the effect of casticin on inflammatory response in human osteoarthritis (OA) chondrocytes remains unclear. In the current study, we examined the anti‐inflammatory effects of casticin on chondrocytes exposed to interleukin‐1&bgr; (IL‐1&bgr;). Our results demonstrated that casticin treatment significantly improved cell viability in chondrocytes exposed to IL‐1&bgr;. Casticin significantly inhibited IL‐1&bgr;‐induced NO and PGE2 production, and iNOS and COX‐2 expression in human OA chondrocytes. It also suppressed the levels of TNF‐&agr; and IL‐6, as well as decreased production of MMP‐3, MMP‐13, ADAMTS‐4 and ADAMTS‐5 in IL‐1&bgr;‐stimulated chondrocytes. Furthermore, casticin prevented IL‐1&bgr;‐induced NF‐&kgr;B activation in chondrocytes. Taken together, these findings showed that casticin attenuates inflammatory responses in chondrocytes stimulated with IL‐1&bgr;, possibly through the NF‐&kgr;B signaling pathway. Thus, casticin may serve as a potential anti‐inflammatory agent in the treatment of OA.