Compound 27a moderately inhibits
mPGES-1 within eicosanoid
and docosanoid biosyntheses. (A–G) Effect of 27a on mPGES-1 in microsomal preparations of IL-1β-treated A549
cells (A), 12-LOX (B), and 15-LOX product formation (C) in PMNL treated
with A23187 and AA, isolated ovine COX-1 (D), COX-1-dependent 12-HHT
formation in platelets (E), human recombinant COX-2 (F), and human
recombinant sEH (G). (H) Quantitative illustration of the lipid mediator
network of macrophages (M1) treated with 27a (1 μM)
and stimulated with pathogenic E. coli as compared to the vehicle control. The node size represents the
mean concentration in pg, and the color intensity denotes the fold
change for each lipid mediator. AA, arachidonic acid; DHA, docosahexaenoic
acid; cys-LTs, cysteinyl-LTs; et-LTB4, LTB4 isomers;
EPA, eicosapentaenoic acid; LX, lipoxine; MaR, maresin; 20-OH-LTB4, 20-hydroxy-LTB4; PD, protectin; Rv, resolvin;
TX, thromboxane. Data are expressed as mean (H) + SEM (A-G) from n = 3 independent experiments. *p <
0.05 vs control; RM one-way ANOVA + Tukey’s post hoc test.