Tropolone類似化合物のCatechol-O-methyltransferase阻害作用について

概要

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Inhibitory effects of several hopolone analogs and 2-methoxyphenol (IX) on catechol-O-methyltransferase (COMT) were examined, comparing with those of catechol (I) and pyrogallol (II) as controls, and the following results were obtained. COMT was partially purified by the method of Mavrides et al., and the enzyme activity was measured by the modified method of Pisano, using solvent extraction with isoamyl alcohol instead of chromatographic procedure. The inhibitions of I, tropolone (III), sodium salt of 4-isopropyltropolone (IV), 5-nitrosotropolone (V), 5-aminotropolone (VI), and 2-hydrazino-5-(p-methoxyphenoxy) tropone (VII) were competitive, and those of II and IX were mixed type, and their K_i values were determined. On the other hand, 2-methoxytropone (VIII) had no effect on COMT activity, suggesting that the hydroxyl in III was indispensable for the inhibitory effect. From the fact that VIII as metabolite of III could not be detected in the incubation medium, it was suggested that the mode of inhibition of III was different from those of polyphenols.
社団法人日本薬学会の論文
1967-04-25