Analogues of 2-phenyl-ethenesulfonic acid phenyl ester have dual functions of inhibiting expression of inducible nitric oxide synthase and activating peroxisome proliferator-activated receptor γ

We identified a series of 2-phenyl-ethenesulfonic acid phenyl ester analogues as novel dual-function agents that suppressed nitric oxide production in lipopolysaccharide/interferon γ-stimulated RAW264.7 cells and activated peroxisome proliferator-activated receptor γ (PPARγ) in a cell-based transactivation assay. Western blot analysis demonstrated that these compounds inhibit the expression of inducible nitric oxide synthase protein, and scintillation proximity assay validated their ability to bind to PPARγ. Our studies provide the basis for developing these dual-function agents for anti-inflammation and anti-atherosclerosis therapy.

Graphical abstractDual functions of 2-phenyl-ethenesulfonic acid phenyl ester analogues inhibit expression of inducible nitric oxide synthase and activate peroxisome proliferator-activated receptor γ.Figure optionsDownload full-size imageDownload as PowerPoint slide