Isatins inhibit cyclooxygenase-2 and inducible nitric oxide synthase in a mouse macrophage cell line.
Isatin is a versatile compound with a diversity of effects. We designed to investigate the inhibitory effect of isatin derivatives on lipopolysaccharide/interferon-gamma-induced expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) proteins, production of prostaglandin E(2) (PGE(2)), nitric oxide (NO), tumor necrosis factor (TNF-alpha), and their capacity to scavenge NO. Isatins inhibit TNF-alpha production and iNOS and COX-2 protein expression resulting on reduced levels of NO and PGE(2). Our results indicate isatin and it derivatives as inhibitors of iNOS and COX-2 enzymes, which might be used as anti-inflammatory and antitumoral agents.
Matheus
Maria Eline
ME
Department of Basic and Clinical Pharmacology, ICB, Federal University of Rio de Janeiro, Brazil.
Violante
Flávio de Almeida
Fde A
Garden
Simon John
SJ
Pinto
Angelo C
AC
Fernandes
Patricia Dias
PD
D000818:Animals; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D051546:Cyclooxygenase 2 / Q000378:metabolism*; D016861:Cyclooxygenase Inhibitors / Q000494:pharmacology; D007510:Isatin / Q000494:pharmacology*; D008070:Lipopolysaccharides / Q000494:pharmacology; D008264:Macrophages / Q000187:drug effects* / Q000201:enzymology; D051379:Mice; D009569:Nitric Oxide / Q000096:biosynthesis; D052247:Nitric Oxide Synthase Type II / Q000037:antagonists & inhibitors / Q000378:metabolism*
D016861:Cyclooxygenase Inhibitors; D008070:Lipopolysaccharides; D009569:Nitric Oxide; D007510:Isatin; D052247:Nitric Oxide Synthase Type II; D051546:Cyclooxygenase 2