[合成生物抗氧化剂——乙酰胆碱酯酶活性抑制剂]。

F I Braginskaia, O M Zorina, E M Molochkina, G A Nikiforov, E B Burlakova
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引用次数: 0

摘要

研究了合成抗氧化剂(3-氧吡啶、嘧啶和受阻酚)对膜结合乙酰胆碱酯酶(AChE)活性的抑制作用。根据ache反应的动力学特征(KM, Vmax, KI),发现受阻酚化合物对酶的抑制模式为非竞争性或混合型,这取决于抑制剂的结构或所使用的底物乙酰胆碱或乙酰硫代胆碱。通过对受阻酚的水溶性衍生物和脂溶性离子醇的抑制作用的比较研究,可以揭示所研究的合成生物抗氧化剂对膜结合AChE的直接和介导(通过膜微环境)抑制作用的可能贡献。
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[Synthetic bioantioxidants--inhibitors of acetylcholinesterase activity].

The inhibitory effects of synthetic antioxidants (3-oxypyridine, pyrimidine and hindered phenols) on the enzymic activity of membrane-bound acetylcholinesterase (AChE) was studied. In terms of estimated kinetic characteristics of AChE-reaction (KM, Vmax, KI), the pattern of enzyme inhibition by the hindered phenol compounds was found to be of non-competitive or mixed type depending on the inhibitor structure or on the substrate acetylcholine or acetylthiocholine used. The comparative study of the inhibitory action of water-soluble derivatives of hindered phenols and fatty-soluble ionol made it possible to reveal possible contributions to the inhibition of both direct and mediated (by the membrane microsurroundings) effects on the membrane-bound AChE by the studied synthetic bioantioxidants.

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