Inhibition of Copper-Containing Amine Oxidase by Oximes

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The inhibitory effects of twelve oxime compounds on the activity of bovine serum monoamine oxidase (copper-containing amine oxidase, E.C. 1.4.3.6) were assayed in vitro. The most potent inhibitor among the compounds examined was 2-butanone oxime, of which the 50% inhibiting concentration in the reaction mixture was 7×10^<-6> M. Acetone oxime, acetoaldehyde oxime, salicylaldehyde oxime and formamide oxime were less potent inhibitors, while 2,3-butanedione monooxime, 2,3-butanedione dioxime, D-camphor oxime, α-furil dioxime, pyridine-2-aldehyde oxime, pyridine-4-aldehyde oxime, syn-2-pyridialdehyde oxime and di-2-pyridiketone oxime exhibited virtually no inhibitory effect on the enzyme activity. The type ofinhibition by 2-butanone oxime was non-competitive, and the inhibitor constant and K_m value with respect to allylamine as the substrate were estimated graphically to be 6.7×10^<-6> and 3.9×10^<-4> M, respectively.
公益社団法人日本薬学会の論文
1988-08-25