Three series (series A-C) of coumarin analogues with phenylpiperazine functions as substitution were designed and synthesized for studying their potential for treating Alzheimer's (AD) disease. Their anticholinesterase activities were assayed according to Ellmann's method against freshly prepared acetylcholinesterase (AChE) from Electrophorus electricus using donepezil as the reference compound...

This current study addresses the effect of diazinon on reversible kinetic parameters such as Michaelis-Menten constant (KS) and Vmax of bovine retinal acetylcholinesterase (AChE). The Ks for the hydrolysis of acetylthiocholine iodide by AChE was increased while Vmax was decreased than the control value in the presence of the diazinon. A LineweaverBurk plot, Dixon plot and their secondary replot...

In a bioassay-guided search for acetylcholinesterase (AChE) inhibitors from 180 medicinal plants, an ethyl acetate extract of whole plants of Agrimonia pilosa ledeb yielded tiliroside (1), 3-methoxy quercetin (2), quercitrin (3) and quercetin (4). We report herein for the first time that all four flavonol compounds showed significant inhibitory effects on AChE, particularly quercetin (4), which...

A method for whole animal acetylcholinesterase (AChE) histochemistry was combined with standard S10 plastination. Resultant whole or partial animal specimens prepared in this manner were superior to whole animal specimens processed for AChE histochemistry and stored in formalin. The results compared favorably with those attained with isolated organ or tissue whole mounts while preserving and en...

Quantitative receptor autoradiography was performed on neonatal and adult cat brains. Serial sections through the basal ganglia were assayed for D1- and D2-dopamine receptors and acetylcholinesterase (AChE) staining. The neonatal basal ganglia revealed patches of increased D1-receptor density that frequently overlapped with patches of increased AChE staining, while the D2-receptor distribution ...

The sensitivity of acetylcholinesterases (ACHE) isolated from the plant-parasitic nematodes Meloidogyne arenaria, M. incognita, and Heterodera glycines and the free-living nematode Caenorhabditis elegans to carbamate and organophosphate nematicides was examined. The AChE from plant-parasitic nematode species were more sensitive to carbamate inhibitors than was AChE from C. elegans, but response...

The large amount of pesticide residues in the environment is a threat to global health by inhibition of acetylcholinesterase (AChE). Biosensors for inhibition of AChE have been thus developed for the detection of pesticides. In line with the rapid development of nanotechnology, nanomaterials have attracted great attention and have been intensively studied in biological analysis due to their uni...

Acetylcholinesterase (AChE) remains a highly viable target for the symptomatic improvement in Alzheimer's disease (AD) because cholinergic deficit is a consistent and early finding in AD. The treatment approach of inhibiting peripheral AchE for myasthenia gravis had effectively proven that AchE inhibition was a reachable therapeutic target. Subsequently tacrine, donepezil, rivastigmine, and gal...

Cholinesterases (ChEs) play a vital role in the regulation of cholinergic transmission. The inhibition of ChEs is considered to be involved in increasing acetylcholine level in the brain and thus has been implicated in the treatment of Alzheimer's disease. We have designed and synthesized a series of novel indole derivatives and screened them for inhibition of acetylcholinesterase (AChE) and bu...

Cholinesterases (ChE) acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are capable for hydrolyzing esters. Our previous structure-activity analysis of ChE substrates showed that extended conformation of substrate choline moiety is productive for hydrolysis by AChE and its semi-folded conformation is productive for hydrolysis by BChE. The formation of activated complex between ChE an...