A Robust and Convenient Fluorimetric Assay for Measuring Acetylcholinesterase Activity and Screening Acetylcholinesterase Inhibitors

Isolation and characterization of acetylcholinesterase inhibitors from Piper longum L.

Background and objectives: The cholinergic deficit correlates with the severity of Alzheimer’s disease. The cholinergic function can be improved by AChE inhibitors blocking this key enzyme in the breakdown of acetylcholine. Based on traditional medicine, during two last decades the use of herbal medicinal substances in dementia therapy has been studied. The fruit extract of <em...

Acetylcholinesterase Inhibitors: Pharmacology and Toxicology

Acetylcholinesterase is involved in the termination of impulse transmission by rapid hydrolysis of the neurotransmitter acetylcholine in numerous cholinergic pathways in the central and peripheral nervous systems. The enzyme inactivation, induced by various inhibitors, leads to acetylcholine accumulation, hyperstimulation of nicotinic and muscarinic receptors, and disrupted neurotransmission. H...

Exploring Different Virtual Screening Strategies for Acetylcholinesterase Inhibitors

The virtual screening problems associated with acetylcholinesterase (AChE) inhibitors were explored using multiple shape, and structure-based modeling strategies. The employed strategies include molecular docking, similarity search, and pharmacophore modeling. A subset from directory of useful decoys (DUD) related to AChE inhibitors was considered, which consists of 105 known inhibitors and 373...

Acetylcholinesterase inhibitors attenuate angiogenesis

Donepezil {(RS)-2-[(1-benzyl-4-piperidyl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one} is a reversible acetylcholinesterase inhibitor and used for treatment of patients with AD (Alzheimer's disease). Recent studies showed that treatment with donepezil reduced production of inflammatory cytokines in PBMCs (peripheral blood mononuclear cells). It was also reported that muscle-derived inflammatory...

Inhibitors of Acetylcholinesterase