Effects of flavonoids on Naja naja and human recombinant synovial phospholipases A2 and inflammatory responses in mice

Life Sci. 1994;54(20):PL333-8. doi: 10.1016/0024-3205(94)90021-3.

Abstract

Six flavonoid derivatives were tested for their influence on Naja naja and human recombinant synovial phospholipase A2. They showed a selectivity for the last enzyme with IC50 = 14.3, 17.6, 12.2 and 28.2 microM for quercetagetin, kaempferol-3-O-galactoside, scutellarein and scutellarein-7-O-glucuronide, respectively, while reduced effects were observed for hispidulin and hibifolin. After topical application all the flavonoids inhibited 12-O-tetradecanoylphorbol-13-acetate-induced ear oedema in mice with a potency comparable to that of indomethacin and they were also able to inhibit carrageenan-induced mouse paw oedema at a dose of 150 mg/kg p.o. The blockade of the free hydroxyl at C-7 or C-6 reduced the anti-inflammatory activity and also the inhibitory effect on human recombinant synovial phospholipase A2. These results are in accordance with the notion that group II phospholipases A2 may play a role in experimental inflammation, although several mechanisms seems to be involved in the anti-inflammatory effect of this group of flavonoids.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Chromones / pharmacology
  • Edema / chemically induced
  • Edema / physiopathology*
  • Edema / prevention & control
  • Flavanones*
  • Flavones*
  • Flavonoids / pharmacology*
  • Galactosides / pharmacology
  • Humans
  • Inflammation / chemically induced
  • Inflammation / physiopathology
  • Inflammation / prevention & control
  • Kaempferols*
  • Male
  • Mice
  • Phospholipases A / metabolism*
  • Phospholipases A2
  • Quercetin / analogs & derivatives
  • Quercetin / pharmacology
  • Recombinant Proteins / metabolism
  • Snakes
  • Tetradecanoylphorbol Acetate / toxicity

Substances

  • Chromones
  • Flavanones
  • Flavones
  • Flavonoids
  • Galactosides
  • Kaempferols
  • Recombinant Proteins
  • kaempferol-3-O-galactoside
  • hibifolin
  • Quercetin
  • Phospholipases A
  • Phospholipases A2
  • hispidulin
  • Tetradecanoylphorbol Acetate
  • scutellarein
  • quercetagetin