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. 2021 Jul 19;64(15):11496–11526. doi: 10.1021/acs.jmedchem.1c00806

Figure 3.

Figure 3

Compound 27a accumulates in innate immune cells and inhibits 5-LOX product formation. (A) Effect of 27a on 5-LOX product formation (LTB4, its isomers, and 5-H(P)ETE) in PMNL treated with Ca2+-ionophore A23187 or A23187 and arachidonic acid (AA). (B) Intracellular uptake of 27a or 12a by PMNL treated with 150 nM of the respective compound for 20 min. Average intracellular concentrations were calculated for spherical PMNL with a diameter of 13 μm. (C) Effect of 27a or 12a on 5-LOX product formation initiated by A23187 and AA in LPS-prestimulated monocytes. (D, E) Effect of 27a on AA release from Escherichia coli-stimulated macrophages (D) and fMLP-induced Ca2+ influx in PMNL (E). (F, G) Effects of 27a or 12a on 5-LOX product formation in human whole blood stimulated with A23187 (F) or LPS and fMLP (G) upon preincubation with the compounds for 10 min (F, G) or 3 h (F). Data are expressed as mean ± SEM (A, C–G) or mean with single values (B) from n = 3 (A–E, F, left panel) and n = 4 (F, right panel, G) independent experiments. *p < 0.05, **p < 0.01, ***p < 0.001 vs control (A, C–G); RM one-way ANOVA + Tukey’s post hoc test (A, C–G).