Anti-inflammatory activity of 6-hydroxy-2,7-dimethoxy-1,4-henanthraquinone from tuberous roots of yam (Dioscorea batatas) through inhibition of prostaglandin D₂ and leukotriene C₄ production in mouse bone marrow-derived mast cells

Arch Pharm Res. 2011 Sep;34(9):1495-501. doi: 10.1007/s12272-011-0911-8. Epub 2011 Oct 6.

Abstract

6-Hydroxy-2,7-dimethoxy-1,4-phenanthraquinone (PAQ) isolated from the tuberous roots of Yam (Dioscorea batatas) inhibited cyclooxygenase-2 (COX-2) and cyclooxygenase-1 (COX-1) dependent prostaglandin D(2) (PGD(2)) generation in mouse bone marrow-derived mast cells in a concentration-dependent manner with IC(50) values of 0.08 μM and 0.27 μM, respectively. In the Western blotting with specific anti-COX-2 antibodies, the decrease of the quantity of PGD(2) was accompanied by a decrease in the COX-2 protein level. But PAQ did not affect COX-1 protein level. In addition, this compound inhibited 5-lipoxygenase (5-LOX) dependent production of leukotriene C(4) in a dose-dependent manner, with an IC(50) of 0.032 μM. These results demonstrate that PAQ has a dual COX-2/5-LOX inhibitory activity. This compound also inhibited the degranulation reaction in a dose-dependent manner with an IC(50) of 2.7 μM. Thus, these results suggest that PAQ may be useful in regulating mast cell-mediated inflammatory diseases.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Blotting, Western
  • Bone Marrow Cells / cytology*
  • Cell Survival / drug effects
  • Dioscorea / chemistry*
  • Dose-Response Relationship, Drug
  • Electrophoresis, Polyacrylamide Gel
  • Inhibitory Concentration 50
  • Leukotriene C4 / antagonists & inhibitors*
  • Leukotriene C4 / biosynthesis
  • Male
  • Mast Cells / drug effects*
  • Mast Cells / immunology
  • Mice
  • Mice, Inbred BALB C
  • Phenanthrenes / pharmacology*
  • Plant Tubers / chemistry
  • Prostaglandin D2 / antagonists & inhibitors*
  • Prostaglandin D2 / biosynthesis
  • Quinones / pharmacology*

Substances

  • 6-hydroxy-2,7-dimethoxy-1,4-phenanthraquinone
  • Anti-Inflammatory Agents, Non-Steroidal
  • Phenanthrenes
  • Quinones
  • Leukotriene C4
  • Prostaglandin D2