Dual Inhibition of Cyclooxygenases-2 and 5-Lipoxygenase by Deoxypodophyllotoxin in Mouse Bone Marrow-Derived Mast Cells(Biochemistry/Molecular Biology)

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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 D_2 (PGD_2) generation in bone marrow-derived mast cells (BMMC) in a concentration-dependent manner with IC_<50> values of 1.89μM and 65.3 μM, respectively. This study also found that this compound inhibited COX-1 and 2-dependent conversion of the exogenous arachidonic acid to PGD_2 in a dose-dependent manner with an IC_<50> values of 0.01 μM and 12.1 μM, respectively using a COX enzyme assay kit. However, this compound did not inhibit COX-2 protein expression up to a concentration of 30 μM. in the BMMC, indicating that deoxypodophyllotoxin directly inhibits COX-2 activity. Furthermore, this compound consistently inhibited the production of leukotriene C_4 (LTC_4) in a dose dependent manner, with an IC_<50> value of 0.37 μM. These results demonstrate that deoxypodophyllotoxin has a dual cyclooxy-genase-2 selective/5-lipoxygenase inhibitory activity, and therefore this compound might provide a basis for novel anti-inflammatory drugs.
社団法人日本薬学会の論文
2004-06-01