文章基本信息

标题：Ginkgetin, a Biflavone from Ginko biloba Leaves, Inhibits Cyclooxygenases-2 and 5-Lipoxygenase in Mouse Bone Marrow-Derived Mast Cells
本地全文：下载
作者：Jong Keun Son ; Min Jung Son ; Eunkyung Lee 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2005
卷号：28
期号：12
页码：2181-2184
DOI：10.1248/bpb.28.2181
出版社：The Pharmaceutical Society of Japan
摘要：Ginkgetin, a biflavone from Ginkgo biloba leaves, was previously reported to be a phospholipase A₂ inhibitor and this compound showed the potent antiarthritic activity in rat adjuvant-induced arthritis as well as analgesic activity. This investigation was carried out to find effects on cyclooxygenase-2 (COX-2) in vitro effect. Ginkgetin inhibits 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 0.75 μ M . 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 0.33 μ M . These results demonstrate that ginkgetin has a dual cyclooxygenase-2/5-lipoxygenase inhibitory activity. Furthermore, this compound also inhibited degranulation reaction in a dose dependent manner, with an IC₅₀ value of 6.52 μ M . Therefore, this compound might provide a basis for novel anti-inflammatory agents.
关键词：Ginkgo biloba;ginkgetin;biflavonoid;cyclooxygenase-2;5-lipoxygenase;bone marrow-derived mast cell