摘要
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 inhibitory activity and kinetics of radix polygonum multiflorum thumb on acetylcholinesterase（AChE） were investigated,and inhibitory activity of radix polygonum multiflorum thumb ethylacetate fractions and water fractions were gradually weakened as the inhibitor concentration increased,and even showed some enhancement,water fractions didn＇t have any inhibitory activity of AChE.Water-saturated n-butyl alcohol fractions and petroleum ether fractions components were significant inhibition activity for AChE.Reversible inhibition of AChE by both of them was observed,and the types of reversible inhibition were non-competitive reversible inhibition and mixed inhibition,respectively.The non-competitive reversible inhibitory constants Ki and Kis were 3.2668μmol/L and 4.8194μmol/L for water-saturated n-butyl alcohol fraction components.The mixed inhibitory constants Ki and Kis were 2.6985μmol/L and 4.7192μmol/L for petroleum ether fraction components,respectively.The inhibitory kinetic results indicated that the inhibition effects of fraction components on free enzyme were stronger than those on enzyme-substrate complex,and the inhibition effects of petroleum ether fraction components were stronger than those of water-saturated n-butyl alcohol fraction components.
出处
《光谱实验室》
CAS
CSCD
2012年第2期745-749,共5页
Chinese Journal of Spectroscopy Laboratory
基金
中南民族大学自然科学青年启动基金(YZQ10008)
关键词
首乌总提取物
乙酰胆碱酯酶
抑制
动力学
Total Extractive of Radix Polygonum Multiflorum Thumb
Acetylcholinesterase
Inhibition
Kinetics
