芫花素对乙酰胆碱酯酶抑制作用研究

The Inhibitory Effect of Genkwanin on Acetylcholinesterase

乙酰胆碱酯酶(AChE)抑制剂是目前治疗阿尔茨海默症(AD)的主要药物。本文应用酶抑制动力学方法研究了芫花素对AChE活性的抑制作用及抑制动力学。研究发现,芫花素能显著地抑制AChE的活性,对AChE酶活力的50%抑制浓度(IC50)为8.96μmol·L^-1。芫花素对AChE的抑制作用表现为混合Ⅰ型可逆抑制,芫花素对乙酰胆碱酯酶的抑制常数KI为5.77×10^-6 mol·L^-1,抑制常数KIS为31.11×10^-6 mol·L^-1,结果表明芫花素对游离酶的抑制作用强于其对酶-底物复合物的抑制作用。

Acetylcholinesterase(AChE)inhibitors are mainly used in the treatment of Alzheimer's disease(AD).The inhibitory effects of genkwanin on the activity of AChE and its inhibition kinetics were studied by enzyme inhibition kinetics.As a result,it revealed that genkwanin significantly inhibited the activity of AChE,and the 50%inhibitory concentration(IC 50)of AChE enzyme activity was 8.96μmol·L^-1.Kinetic analyses showed that the type of reversible inhibition of genkwanin on AChE was mixed inhibition.The mixed inhibition constants K I and K IS were determined to be 5.77×10^-6 mol·L^-1 and 31.11×10^-6 mol·L^-1,respectively.The inhibitory kinetic results indicated that the inhibition effect of genkwanin on free enzyme was stronger than that on enzyme-substrate complex.