Naturally occurring biflavonoid, ochnaflavone, inhibits cyclooxygenases-2 and 5-lipoxygenase in mouse bone marrow-derived mast cells

Arch Pharm Res. 2006 Apr;29(4):282-6. doi: 10.1007/BF02968571.

Abstract

Ochnaflavone is a medicinal herbal product isolated from Lonicera japonica that inhibits cyclooxygenase-2 (COX-2) dependent phases of prostaglandin D2 (PGD2) generation in bone marrow-derived mast cells (BMMC) in a concentration-dependent manner with IC50 values of 0.6 microM. Western blotting probed with specific anti-COX-2 antibodies showed that the decrease in quantity of the PGD2 product was accompanied by a decrease in the COX-2 protein level. In addition, this compound consistently inhibited the production of leukotriene C4 (LTC4) in a dose dependent manner, with an IC50 value of 6.56 microM. These results demonstrate that ochnaflavone has a dual cyclooxygenase-2/5-lipoxygenase inhibitory activity. Furthermore, this compound strongly inhibited degranulation reaction in a dose dependent manner, with an IC50 value of 3.01 microM. Therefore, this compound might provide a basis for novel anti-inflammatory drugs.

Publication types

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

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / isolation & purification
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Arachidonate 5-Lipoxygenase / metabolism
  • Bone Marrow Cells / drug effects
  • Bone Marrow Cells / physiology
  • Cell Degranulation
  • Cyclooxygenase 2 / metabolism
  • Cyclooxygenase 2 Inhibitors / isolation & purification
  • Cyclooxygenase 2 Inhibitors / pharmacology*
  • Dose-Response Relationship, Drug
  • Flavonoids / isolation & purification
  • Flavonoids / pharmacology*
  • Leukotriene C4 / metabolism
  • Lipoxygenase Inhibitors* / isolation & purification
  • Lipoxygenase Inhibitors* / pharmacology*
  • Lonicera* / chemistry
  • Male
  • Mast Cells / drug effects*
  • Mast Cells / physiology
  • Mice
  • Mice, Inbred BALB C
  • Prostaglandin D2 / metabolism

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Cyclooxygenase 2 Inhibitors
  • Flavonoids
  • Lipoxygenase Inhibitors
  • Leukotriene C4
  • ochnaflavone
  • Arachidonate 5-Lipoxygenase
  • Cyclooxygenase 2
  • Prostaglandin D2