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Inhibitory Activity of Amentoflavone on Arachidonic Acid Releasing Enzyme, Phopholipase $A_2$ and Inhibition of Histamine Release from Mast Cells  

Moon, Tae-Chul (College of Pharmacy, Yeungnam University)
Lee, Eun-Kyung (College of Pharmacy, Yeungnam University)
Lee, Sung-Ho (College of Pharmacy, Yeungnam University)
Son, Kun-Ho (Depart. Food & Nutrition, Andong National University)
Kim, Hyun-Pyo (College of Pharmacy, Kangwan National University)
Kang, Sam-Sik (Natural Products Res. Institute. Seoul National University)
Chang, Hyeun-Wook (College of Pharmacy, Yeungnam University)
Publication Information
Korean Journal of Pharmacognosy / v.33, no.1, 2002 , pp. 49-52 More about this Journal
Abstract
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.
Keywords
Amentoflavone; Ginko biloba; human secretory phospholipase $A_2$ arachdidonic acid releasing enzyme; mast cells; histamine; $A_{23187}$;
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