Braginskaia F I, Zorina O M, Molochkina E M, Nikiforov G A, Burlakova E B
Izv Akad Nauk SSSR Biol. 1992 Sep-Oct(5):690-8.
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.
研究了合成抗氧化剂（3-羟基吡啶、嘧啶和受阻酚）对膜结合乙酰胆碱酯酶（AChE）酶活性的抑制作用。根据AChE反应的估计动力学特征（KM、Vmax、KI），发现受阻酚化合物对酶的抑制模式取决于抑制剂结构或所使用的底物乙酰胆碱或乙酰硫代胆碱，为非竞争性或混合型。对受阻酚的水溶性衍生物和脂溶性离子醇的抑制作用进行比较研究，有助于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。
