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The purpose of this study was to investigate the effect of the novelly synthesized coumarin derivative, RKNU026 on pro-inflammatory cytokine inhibitory efficacy. The results demonstrated that RKNU026 could inhibit IL-1β and TNF-α production in a concentration dependent pattern. The half maximal inhibitory concentrations (IC50) of RKNU026 for IL-1β and TNF-α were 0.024 µM and 729 µM, respectively. Compared with dexamethasone at the same final concentration of 1 µM, the efficacy of RKNU026 on IL-1β inhibition was still lower than dexamethasone (70.78% versus 89.53%) while RKNU026 had no efficacy on TNF-α inhibition at this concentration. Our work suggests that RKNU026 has anti-inflammatory efficacy through pro-inflammatory cytokine inhibition. Furthermore, it is considered to be an IL-1β inhibitor rather than a TNF-α inhibitor.
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