非ステロイド性抗炎症薬の蛋白結合(第2報)サリチル酸の蛋白結合におよぼす種々の薬物の影響

概要

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The effect of five nonsteroidal anti-inflammatory agents and seven sulfonamides on the binding of salicylic acid to bovine serum albumin (BSA, fraction V) was examined by the equilibrium dialysis method at pH 7.4 and 37°. Most of anti-inflammatory agents, which have a high affinity for BSA, strongly displaced salicylic acid. Sulfonamide derivatives also reduced the binding of salicylic acid though their effect of displacement was less than that of anti-inflammatory agents. When the percentage of displacement for salicylic acid was plotted against log (Σnk) which represents a binding ability of the displacing agent itself, a sigmoid curve was obtained. It was suggested that the amount of displacement tends to correspond to the binding ability of the displacing agent and becomes progressively greater as log (Σnk) becomes larger than that of salicylic acid. Furthermore, in the wide range of salicylic acid concentration (0.1-2.5×10^<-3>M) naproxen and flurbiprofen showed patterns of displacement for salicylic acid different from that of other displacing agents. It was assumed that they have binding mechanisms different from the others including salicylic acid.
公益社団法人日本薬学会の論文
1978-11-25