In vitro anti-inflammatory activity of 3-O-methyl-flavones isolated from Siegesbeckia glabrescens

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1511-4. doi: 10.1016/j.bmcl.2007.12.052. Epub 2007 Dec 25.

Abstract

Four flavones, 3,4'-O-dimethylquercetin (1), 3,7-O-dimethylquercetin (2), 3-O-methylquercetin (3) and 3,7,4'-O-trimethylquercetin (4) were isolated as the inhibitors of nitric oxide production in activated microglia (IC(50) values: 11.1, 4.2, 3.8, and 25.1 microM, respectively). They suppressed the expression of protein and mRNA of inducible nitric oxide synthase. Furthermore, compounds 2 and 3 showed scavenging activity of peroxynitrite with SC(50) values of 1.75 and 0.77 microM, respectively.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / isolation & purification*
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Asteraceae / chemistry*
  • Cell Line
  • Dose-Response Relationship, Drug
  • Flavones / isolation & purification
  • Flavones / pharmacology*
  • Lipopolysaccharides / pharmacology
  • Mice
  • Microglia / drug effects
  • Microglia / enzymology
  • Microglia / metabolism
  • Nitric Oxide / antagonists & inhibitors
  • Nitric Oxide / biosynthesis
  • Nitric Oxide Synthase Type II / antagonists & inhibitors
  • Nitric Oxide Synthase Type II / biosynthesis
  • Nitric Oxide Synthase Type II / genetics
  • Nitric Oxide Synthase Type II / metabolism
  • Quercetin / analogs & derivatives*
  • RNA, Messenger / biosynthesis
  • RNA, Messenger / genetics

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Flavones
  • Lipopolysaccharides
  • RNA, Messenger
  • Nitric Oxide
  • Quercetin
  • Nitric Oxide Synthase Type II