用多种方法分析环磷酰胺对大鼠脑乙酰胆碱酯酶抑制作用的数据。

Multiple approaches to analyse the data for rat brain acetylcholinesterase inhibition by cyclophosphamide.

机构信息

Enzymoic, 7 Peterlee Pl., Hebersham, NSW, 2770, Australia.

出版信息

Neurochem Res. 2010 Oct;35(10):1501-9. doi: 10.1007/s11064-010-0199-y. Epub 2010 Jul 21.

PMID:20652634

Abstract

Acetylcholinesterase (AChE) is an externally oriented membrane-bound enzyme and its main physiological role is termination of chemical transmission at cholinergic synapses and secretory organs by rapid hydrolysis of the neurotransmitter acetylcholine (ACh). Nevertheless, it is well known that cyclophosphamide (CP; nitrogen mustard derivative) is an eminent anticancer drug. The present work addresses multiple approaches to analyze an identical data for rat brain AChE inhibition by CP. These different angels of analysis based on two classical (Lineweaver-Burk as well as Dixon) plots, their secondary replots, a new graphical approach and general built-in equations of GOSA. Thus various kinetic constants (K(I), K(s,) K(m), k(sl), V(mao), K(i), k(sli), S(lo), K(maxi), S(K0.5), k(cat) and k(sp)) were estimated and mode of inhibition discussed in the current study.

摘要

乙酰胆碱酯酶 (AChE) 是一种外向型膜结合酶，其主要生理作用是通过快速水解神经递质乙酰胆碱 (ACh) 来终止胆碱能突触和分泌器官的化学传递。然而，众所周知，环磷酰胺 (CP; 氮芥衍生物) 是一种杰出的抗癌药物。本工作采用多种方法分析 CP 对大鼠脑 AChE 抑制的相同数据。这些分析的不同角度基于两种经典方法（Lineweaver-Burk 和 Dixon 作图）、它们的二次重绘图、一种新的图形方法和 GOSA 的内置通用方程。因此，在本研究中估计了各种动力学常数 (K(I)、K(s,)、K(m)、k(sl)、V(mao)、K(i)、k(sli)、S(lo)、K(maxi)、S(K0.5)、k(cat) 和 k(sp))，并讨论了抑制模式。