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研究了首乌总提取物对乙酰胆碱酯酶(AChE)抑制活性的筛选及抑制动力学。结果表明,首乌乙酸乙酯组分和水组分的抑制能力随着抑制剂浓度的增大而逐渐减弱,甚至表现出一定的增强作用,而水组分没有AChE抑制能力。水饱和正丁醇组分和石油醚组分均对AChE具有显著的抑制能力,两者对AChE的抑制作用类型分别为非竞争型和混合型的可逆抑制,水饱和正丁醇组分对AChE的非竞争型抑制常数Ki、Kis分别为3.2668μm ol/L和4.8194μm ol/L,石油醚组分对AChE的混合型抑制常数Ki、Kis分别为2.6985μm ol/L和4.7192μm ol/L,表明两种组分对游离酶的抑制作用均强于其对于酶-底物复合物的抑制作用,且后者较前者对AChE的抑制作用更强。
The screening of the total inhibitory activity of Radix Polygoni multiflori extract on acetylcholinesterase (AChE) and its inhibition kinetics were studied. The results showed that the inhibitory ability of ethyl acetate fraction and water fraction of Radix Aconiti decadillaris decreased with the increase of inhibitor concentration, and even showed a certain enhancement effect, while the water fraction did not have AChE inhibitory ability. The water-saturated n-butanol fraction and the petroleum ether fraction had significant inhibitory effect on AChE. The inhibitory effects of both AChE and AChE were reversible inhibition of non-competitive and mixed-type respectively. The effect of water-saturated n-butanol on AChE Kis were 3.2668μmol / L and 4.8194μmol / L, respectively. The mixed inhibition constants Ki and Kis of petroleum ether component to AChE were 2.6985μmol / L and 4.7192μmol / L, respectively , Indicating that the inhibitory effect of both components on the free enzyme is stronger than that on the enzyme-substrate complex, and the latter is more effective than the former on inhibiting AChE.