Selective mPGES-1 Inhibitor Ameliorated Adjuvant-Induced Arthritis in the Rat Model

Figure 3

Effects of MPO-0144 on mPGES-1, COX-1, and COX-2 enzymes. (a) Inhibitory activity of MPO-0144 against mPGES-1 activity in IL-1β (1 ng/mL)-stimulated RAW 264.7 macrophage cells. MK886 (10 μM) was used as a positive control of mPGES-1 inhibition [17]. (b) The inhibition activity of MPO-0144 against ovine COX-1 enzyme. sc-560 (100 nM) was used as a positive control of COX-1 inhibition. (c) The inhibition activity of MPO-0144 against human recombinant COX-2 enzyme. Dup-697 (100 nM) was used as a positive control of COX-2 inhibition. This IC₅₀ value (IC₅₀ = 0.03 μM) was obtained by the extrapolation method. Values are indicated as the mean ± SEM (n = 3). Statistically significant values were compared using one-way ANOVA and Dunnett’s post hoc test. ^∗P < 0.05; ; vs. the vehicle group. All statistics were performed using GraphPad Prism 5 statistical software (GraphPad Software Inc., CA, USA).

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