Dual inhibition of cyclooxygenases-2 and 5-lipoxygenase by deoxypodophyllotoxin in mouse bone marrow-derived mast cells
- Dual inhibition of cyclooxygenases-2 and 5-lipoxygenase by deoxypodophyllotoxin in mouse bone marrow-derived mast cells
- Anthriscus sylvestris; deoxypodophyllotoxin; cyclooxygenase-2; 5-lipoxygenase; bone marrow-derived mast cells
- Issue Date
- PHARMACEUTICAL SOC JAPAN
- BIOLOGICAL & PHARMACEUTICAL BULLETIN, v. 27, No. 6, Page. 786-788
- Deoxypodophyllotoxin (Anthricin) is a medicinal herbal product isolated from Anthriscus sylvestris HOFFM.
that inhibits cyclooxygenase-2 (COX-2) and COX-1-dependent phases of prostaglandin D2 (PGD2) generation in
bone marrow-derived mast cells (BMMC) in a concentration-dependent manner with IC50 values of 1.89 mM and
65.3 mM, respectively. This study also found that this compound inhibited COX-1 and 2-dependent conversion of
the exogenous arachidonic acid to PGD2 in a dose-dependent manner with an IC50 values of 0.01 mM and 12.1 mM,
respectively using a COX enzyme assay kit. However, this compound did not inhibit COX-2 protein expression up
to a concentration of 30 mM in the BMMC, indicating that deoxypodophyllotoxin directly inhibits COX-2 activity.
Furthermore, this compound consistently inhibited the production of leukotriene C4 (LTC4) in a dose dependent
manner, with an IC50 value of 0.37 mM. These results demonstrate that deoxypodophyllotoxin has a dual cyclooxygenase-2 selective/5-lipoxygenase inhibitory activity, and therefore this compound might provide a basis for novel
- 0918-6158; 1347-5215
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