• Title/Summary/Keyword: human secretory phospholipase $A_2$ arachdidonic acid releasing enzyme

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Inhibitory Activity of Amentoflavone on Arachidonic Acid Releasing Enzyme, Phopholipase $A_2$ and Inhibition of Histamine Release from Mast Cells (Amentoflavone의 아라키돈산 유리효소인 phopholipase $A_2$에 대한 저해활성 및 비만세포에서 histamine 유리 억제효과)

  • Moon, Tae-Chul;Lee, Eun-Kyung;Lee, Sung-Ho;Son, Kun-Ho;Kim, Hyun-Pyo;Kang, Sam-Sik;Chang, Hyeun-Wook
    • Korean Journal of Pharmacognosy
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    • v.33 no.1 s.128
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    • pp.49-52
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    • 2002
  • Amentoflavone, naturally occurring biflavonoid, isolated from the leaves of Ginko biloba, selectively inhibited human seceretory phospholipase $A_2$. This compound potently and irreversibly inhibited human group IIA in a dose dependent manner with an $IC_50$ about $3\;{\mu}M$. Amentoflavone inhibited phospholipase $A_2$ by a noncompetitive manner with the apparent Ki value of $1{\times}10^{-5}M$. In addition, the inhibitory activity of amentoflavone is rather specific against group IIA phospholipase $A_2$ than group IB phospholipase $A_2$. Furthermore, this compound strong inhibit histamine release from $A_{23187}$ treated rat peritoneal mast cells. These results indicate naturally occurring biflavonoid represents a novel anti-inflammatory agent.