研究了2-氯酚(2-CP)及2,4-二氯苯酚(2,4-DCP)对乙酰胆碱酯酶(AChE)活性的抑制作用及抑制动力学.结果表明,两种氯酚均能显著地抑制AChE的活性,2-CP及2,4-DCP对AChE酶活力的50%抑制浓度(IC50)分别为0.68,0.56mmol·L-1.2-CP及2,4-DCP对AChE的抑制作用类型为混合型的可逆抑制,2-CP对AChE的混合型抑制常数Ki,K′i分别为0.42,2.80mmol·L-1,2,4-DCP对AChE的混合型抑制常数Ki,K′i分别为0.37,0.70mmol·L-1,表明两种氯酚对游离酶的抑制作用均强于其对酶-底物复合物的抑制作用,且后者较前者对乙酰胆碱酯酶的抑制作用更强.
The inhibition effect of ortho-chlorophenol(2-CP)and 2,4-dichlorophenol(2,4-DCP)on acetylcholinesterase(AChE)and its kinetics were studied by spectrophotometry.The results show that the activity of AChE can be inhibited obviously by 2-CP and 2,4-DCP,and the 50%inhibitory concentration(IC50)is 0.68mmol·L-1for 2-CP and 0.56mmol·L-1 for 2,4-DCP,respectively.Reversible inhibition of AChE by 2-CP and 2,4-DCP has been observed,and the type of reversible inhibition is mixed inhibition.The mixed inhibitory constants Kiand K'iare 0.42mmol·L-1 and 2.80mmol·L-1for 2-CP,and are 0.37 mmol·L-1 and 0.70mmol·L-1for 2,4-DCP,respectively.The inhibitory kinetic results indicate that the inhibition effect of chlorophenols on free enzyme is stronger than that on enzyme-substrate complex,and the inhibition effect of 2,4-DCP is stronger than that of 2-CP.