A graphical kinetic analysis model for the inhibition of acetylcholinesterase by anti-alzheimer's drug, tacrine

الملخص EN

Acetyl cholinesterase (AChE) is an externally oriented crucial membrane-bound enzyme, which exists at cholinergic synapses, and terminates the impulse transmission by very rapid hydrolysis of the neurotransmitter, acetylcholine.

Inhibition of AChE has been the target purpose for pest control and in warfare, from the long time ago but from the past several years, these are one of the most actively investigated classes of compounds for the search for an effective ideal treatment of various brain diseases such as Alzheimer's diseases (AD), Parkinson's diseases and also some other disorders like glaucoma and myasthenia gravis.

In the current study, some modern kinetic parameters of AChE inhibition by terrine (one of the licensed drug for the therapy of AD) have been investigated.

The assay was done with erythrocyte AChE using five different substrate (ASCh) concentrations in the absence and presence of terrine (0.00625 - 0.10 µM).

The change in optical density was monitored for 12 min.

Seven modified kinetic parameters (kmax, kir, Kea, kmltoc, k20rc, Kasich and KdcAcelc) were calculated from these experimental data, which will be fruitful for detail kinetic analysis of the inhibition of various enzymes particularly, AChE by different reversible inhibitors like anti-Alzheimer's therapeutic agents, in vitro.