KMID : 0043319940170040218
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Archives of Pharmacal Research 1994 Volume.17 No. 4 p.218 ~ p.222
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Inactivation of human pleural fluid phospholipase A2 by dioscin
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Baek Suk-Hwan
Kim Sung-Hwan Son Kun-Ho Chung Kyu-Charn Chang Hyun-Wook
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Abstract
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The natural product, spirostanol glycoside dioscin, was shown to directly inactivate human pleural fluid phospholipase Inactivation was dose, and time dependent. The was estimated at 18 .mu.M and virtually complete inactivation of the enzyme occurred at 50 .mu.M. Using Michaelis-Menten kinetics, dioscin inactivated the enzyme by a competitive inhibitory manner, the apparent Ki value was . Reversibility was studied directly by dialysis method, the inhibition was reversible. Additioin of excess concentration up to 8 mM did not antagonize the inhibitory activity of dioscin. Inactivation of several kinds of by dioscin is due to interaction with the active site of and may be a useful adjunt in the theraphy of inflammatory diseases.
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KEYWORD
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Phospholipase, Dioscin, Human pleural fluid (HPF)
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