Inhibitory Effects of Tropolone Analogues on Catechol-O-methyltransferase

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  • Tropolone類似化合物のCatechol-O-methyltransferase阻害作用について
  • Tropolone ルイジ カゴウブツ ノ Catechol-O-methyltransferase ソガイ サヨウ ニ ツイテ

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Description

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 Ki 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.

Journal

  • YAKUGAKU ZASSHI

    YAKUGAKU ZASSHI 87 (4), 345-350, 1967

    The Pharmaceutical Society of Japan

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