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 gamma.
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 gamma-stimulated RAW264.7 cells and activated peroxisome proliferator-activated receptor gamma (PPARgamma) 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 PPARgamma. Our studies provide the basis for developing these dual-function agents for anti-inflammation and anti-atherosclerosis therapy.
Lee
Yue-Zhi
YZ
Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County 350, Taiwan, ROC.
Yang
Cheng-Wei
CW
Kang
Iou-Jiun
IJ
Wu
Ssu-Hui
SH
Chao
Yu-Sheng
YS
Chern
Jyh-Haur
JH
Lee
Shiow-Ju
SJ
D000476:Alkanesulfonates / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology; D002460:Cell Line; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D004789:Enzyme Activation; D004952:Esters / Q000737:chemistry*; D020128:Inhibitory Concentration 50; D051379:Mice; D008956:Models, Chemical; D009569:Nitric Oxide / Q000737:chemistry; D052247:Nitric Oxide Synthase Type II / Q000096:biosynthesis*; D047495:PPAR gamma / Q000096:biosynthesis*; D013451:Sulfonic Acids / Q000737:chemistry; D015533:Transcriptional Activation
D000476:Alkanesulfonates; D000893:Anti-Inflammatory Agents; D004952:Esters; D047495:PPAR gamma; D013451:Sulfonic Acids; D009569:Nitric Oxide; D052247:Nitric Oxide Synthase Type II