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  • 标题:Dual Inhibition of Cyclooxygenases-2 and 5-Lipoxygenase by Deoxypodophyllotoxin in Mouse Bone Marrow-Derived Mast Cells
  • 本地全文:下载
  • 作者:Seung Ho Lee ; Min Jung Son ; Hye Kyung Ju
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2004
  • 卷号:27
  • 期号:6
  • 页码:786-788
  • DOI:10.1248/bpb.27.786
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:Deoxypodophyllotoxin (Anthricin) is a medicinal herbal product isolated from Anthriscus sylvestris H OFFM . 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 μ M and 65.3 μ M , 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 μ M and 12.1 μ M , respectively using a COX enzyme assay kit. However, this compound did not inhibit COX-2 protein expression up to a concentration of 30 μ M 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 μ M . 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 anti-inflammatory drugs.
  • 关键词:Anthriscus sylvestris;deoxypodophyllotoxin;cyclooxygenase-2;5-lipoxygenase;bone marrow-derived mast cells
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