The X-ray crystallographic structure of Torpedo californica acetylcholinesterase (TcAChE) in complex with the bifunctional inhibitor NF595, a potentially new anti-Alzheimer drug, has been solved. For the first time in TcAChE, a major conformational change in the peripheral-site tryptophan residue is observed upon complexation. The observed conformational flexibility highlights the dynamic natur...

Background and Objective: Alzheimer’s disease (AD) is a multifactorial disease with debilitating consequences and few therapeutic strategies exist for it. With regard to antioxidant capacity and anti-β-amyloid polymerization potential of ellagic acid, this study was conducted to evaluate the effect of this substance on enhanced acetylcholinesterase reactivity in an experimental model of Alzheim...

In this work we consider marketed drugs for Alzheimer disease (AD) including acetylcholinesterase inhibitors (AChE-Is) and antiglutamatergic treatment involving the N-methyl-d-aspartate (NMDA) receptor. We discuss medications and substances available for use as cognitive enhancers that are not approved for AD or cognitive impairment, and other neurotransmitter-related therapies in development o...

In search of potent inhibitors cholinesterase enzymes and antioxidant agents, synthetic derivatives dihydroquinazolin-4(1H)-one 1-38 were evaluated as potential anti-Alzheimer agents through in vitro acetylcholinesterase (AChE) butyrylcholinesterase (BChE) inhibitions radical (DPPH ABTS) scavenging activities. The (SAR) was mainly based on the different substituents at aryl part which showed a ...

Hypertrichosis is the excessive hair growth in any area of the skin surface. Acquired localized hypertrichosis may be secondary to multiple causes and there is a secondary form due to several drugs, which is usually reversible with discontinuation of the causative agent. Rivastigmine is a reversible and competitive inhibitor of acetylcholinesterase and butyrylcholinesterase used for symptomatic...

Acetylcholinesterase inhibition, antioxidant and cytotoxic activities of Hedychium gardnerianum leaf essential oils from S. Miguel Island were determined. All the oils inhibited acetylcholinesterase, with IC(50) values of approximately 1 mg/mL, showing no statistical differences between collection sites. Three oils presented mixed inhibition, whilst one was almost truly competitive. This activi...

The transient opening of a backdoor in the active-site wall of acetylcholinesterase, one of nature's most rapid enzymes, has been suggested to contribute to the efficient traffic of substrates and products. A crystal structure of Torpedo californica acetylcholinesterase in complex with the peripheral-site inhibitor aflatoxin is now presented, in which a tyrosine at the bottom of the active-site...

OBJECTIVES Alzheimer's disease (AD) as progressive cognitive decline and the most common form of dementia is due to degeneration of the cholinergic neurons in the brain. Therefore, administration of the acetylcholinesterase (AChE) inhibitors such as donepezil is the first choice for treatment of the AD. In the present study, we focused on the synthesis and anti-cholinesterase evaluation of new ...

Interest in the biological role of bioactive compounds present in medicinal herbs has increased over the last years. Of particular interest are plants that have an anti-Alzheimer activities. Several plants can be useful for Alzheimer (AD) management. Such as these which have anti-inflammatory activity, acetylcholinesterase (AChE) inhibitory action, antiapoptotic, slow the aggregation of amyloid...

BACKGROUND The therapeutic options to treat Alzheimer-type dementia (ATD) in recent years, have made it increasingly necessary to become familiar with the employment pattern of these new medicinal products. METHODS A cross-sectional observational study of the population with ATD treated with acetylcholinesterase inhibitors and/or memantine in the Gallician Health Service. Databases were compi...