14,474 results match your criteria acetylcholinesterase ache


Acute gene expression changes in the mouse hippocampus following a combined Gulf War toxicant exposure.

Life Sci 2021 Jul 19:119845. Epub 2021 Jul 19.

Laboratory of Molecular Biology, VA New Jersey Health Care System, Research & Development (Mailstop 15), Bldg. 16, Rm. 16-176, 385 Tremont Ave, East Orange, NJ 07018, United States of America; Rutgers School of Graduate Studies, Newark, NJ 07103, United States of America; Laboratory of Molecular Biology, Bay Pines VA Healthcare System, Research and Development, 151, Bldg. 22, Rm. 123, 10000 Bay Pines Blvd, Bay Pines, FL 33744, United States of America; Pharmacology, Physiology, and Neuroscience, Rutgers-New Jersey Medical School, Newark, NJ 07103, United States of America. Electronic address:

Aims: Approximately 30% of the nearly 700,000 Veterans who were deployed to the Gulf War from 1990 to 1991 have reported experiencing a variety of symptoms including difficulties with learning and memory, depression and anxiety, and increased incidence of neurodegenerative diseases. Combined toxicant exposure to acetylcholinesterase (AChE) inhibitors has been studied extensively as a likely risk factor. In this study, we modeled Gulf War exposure in male C57Bl/6J mice with simultaneous administration of three chemicals implicated as exposure hazards for Gulf War Veterans: pyridostigmine bromide, the anti-sarin prophylactic; chlorpyrifos, an organophosphate insecticide; and the repellant N,N-diethyl-m-toluamide (DEET). Read More

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Potential of nafimidone derivatives against co-morbidities of epilepsy: In vitro, in vivo, and in silico investigations.

Drug Dev Res 2021 Jul 22. Epub 2021 Jul 22.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jagiellonian University Medical College, Krakow, Poland.

Nafimidone is known for its clinical antiepileptic effects and alcohol derivatives of nafimidone were reported be potent anticonvulsants. These compounds are structurally similar to miconazole, which is known to inhibit cholinesterases, protect neurons, and ameliorate cognitive decline. Herein, we aimed to reveal the potential of three nafimidone alcohol esters (5 g, 5i, and 5 k), which were previously reported for their anticonvulsant effects, against co-morbidities of epilepsy such as inflammatory and neuropathic pain, cognitive and behavioral deficits, and neuron death, and understand their roles in related pathways such as γ-butyric acid type A (GABA ) receptor and cholinesterases using in vitro, in vivo and in silico methods. Read More

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Synthesis of ellagic acid glucoside using glucansucrase from Leuconostoc and characterization of this glucoside as a functional neuroprotective agent.

AMB Express 2021 Jul 21;11(1):108. Epub 2021 Jul 21.

Institute of Agricultural Science and Technology, Chonnam National University, Gwangju, 61186, South Korea.

Ellagic acid glucoside was synthesized via transglucosylation using sucrose and glucansucrase derived from Leuconostoc mesenteroides B-512 FMCM. After such enzymatic synthesis, the product was purified by 50% ethyl acetate fraction and C18 column chromatography. Modification of ellagic acid glucoside was verified by LC-MS/MS at m/z 485. Read More

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The State of The Art on Acetylcholinesterase Inhibitors in the Treatment of Alzheimer's Disease.

J Cent Nerv Syst Dis 2021 7;13:11795735211029113. Epub 2021 Jul 7.

Institute for Biomedical Research and Innovation of the National Research Council, Catanzaro, Italy.

Alzheimer's disease (AD) is a chronic disabling disease that affects the central nervous system. The main consequences of AD include the decline of cognitive functions and language disorders. One of the causes leading to AD is the decrease of neurotransmitter acetylcholine (ACh) levels in the brain, in part due to a higher activity of acetylcholinesterase (AChE), the enzyme responsible for its degradation. Read More

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An Antidote Screening System for Organophosphorus Poisoning Using Zebrafish Larvae.

ACS Chem Neurosci 2021 Jul 20. Epub 2021 Jul 20.

Department of Life and Health Sciences, INSERM, Maladies Rares: Génétique et Métabolisme (MRGM), U1211, Université de Bordeaux, Pessac, F-33615, France.

Organophosphorus (OP) cholinesterase inhibitors, which include insecticides and chemical warfare nerve agents, are very potent neurotoxicants. Given that the actual treatment has several limitations, the present study provides a general method, called the zebrafish-OP-antidote test (ZOAT), and basic scientific data, to identify new antidotes that are more effective than the reference pyridinium oximes after acute OP poisoning. The reactivation capacity of a chemical compound can be measured using and acetylcholinesterase (AChE) assays. Read More

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Identification of Phenolic Compounds by LC-MS/MS and Evaluation of Bioactive Properties of Two Edible Halophytes: and .

Molecules 2021 Jul 1;26(13). Epub 2021 Jul 1.

Department of Pharmaceutical Botany, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey.

This work aimed to evaluate the phenolic content and antioxidant, antimicrobial and enzyme inhibitory activities of the methanol extracts and their fractions of two edible halophytic species, (LE) and (LS). The total phenolic content resulted about two-fold higher in the ethyl acetate fraction of LE (522.82 ± 5. Read More

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Evaluation of a Newly Synthesized Acetylcholinesterase Inhibitor in a Transgenic Model of Alzheimer's Disease.

Front Neurosci 2021 30;15:691222. Epub 2021 Jun 30.

Division of Molecular Therapeutics and Formulation, School of Pharmacy, The University of Nottingham, University Park, Nottingham, United Kingdom.

Alzheimer's disease is a neurodegenerative disease characterized by disrupted memory, learning functions, reduced life expectancy, and locomotor dysfunction, as a result of the accumulation and aggregation of amyloid peptides that cause neuronal damage in neuronal circuits. In the current study, we exploited a transgenic line, expressing amyloid-β peptides to investigate the efficacy of a newly synthesized acetylcholinesterase inhibitor, named XJP-1, as a potential AD therapy. Behavioral assays and confocal microscopy were used to characterize the drug effect on AD symptomatology and amyloid peptide deposition. Read More

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Synthesis and evaluation of novel arylisoxazoles linked to tacrine moiety: in vitro and in vivo biological activities against Alzheimer's disease.

Mol Divers 2021 Jul 17. Epub 2021 Jul 17.

Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran.

Alzheimer's disease (AD) is now ranked as the third leading cause of death after heart disease and cancer. There is no definite cure for AD due to the multi-factorial nature of the disease, hence, multi-target-directed ligands (MTDLs) have attracted lots of attention. In this work, focusing on the efficient cholinesterase inhibitory activity of tacrine, design and synthesis of novel arylisoxazole-tacrine analogues was developed. Read More

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Amygdalus spinosissima root extract enhanced scopolamine-induced learning and memory impairment in mice.

Metab Brain Dis 2021 Jul 17. Epub 2021 Jul 17.

Faculty of Veterinary Medicine, Universiti Putra Malaysia, 43400 UPM, Serdang, Malaysia.

The Amygdalus spinosissima (Rosaceae) plant has been used in the Iranian folk medicine as a remedy for the burn wound. Hence, in this study, we aimed to determine the possible medicinal potential of the plant focusing on the root part. The bioactive phenolic and flavonoid compounds present in the root extract of the Amygdalus spinosissima plant as well as its antioxidant and anti-inflammatory properties were determined. Read More

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Identification of Compounds for Butyrylcholinesterase Inhibition.

SLAS Discov 2021 Jul 16:24725552211030897. Epub 2021 Jul 16.

Division for Pre-Clinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Rockville, MD, USA.

Butyrylcholinesterase (BChE) is a nonspecific cholinesterase enzyme that hydrolyzes choline-based esters. BChE plays a critical role in maintaining normal cholinergic function like acetylcholinesterase (AChE) through hydrolyzing acetylcholine (ACh). Selective BChE inhibition has been regarded as a viable therapeutic approach in Alzheimer's disease. Read More

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The cytoskeleton as a non-cholinergic target of organophosphate compounds.

Chem Biol Interact 2021 Jul 13;346:109578. Epub 2021 Jul 13.

Department of Toxicology, Center for Research and Advanced Studies of the National Polytechnic Institute. Av. IPN 2508, San Pedro Zacatenco, C.P. 07360, Mexico City, Mexico. Electronic address:

Current organophosphate (OP) toxicity research now considers potential non-cholinergic mechanisms for these compounds, since the inhibition of acetylcholinesterase (AChE) cannot completely explain all the adverse biological effects of OP. Thanks to the development of new strategies for OP detection, some potential molecular targets have been identified. Among these molecules are several cytoskeletal proteins, including actin, tubulin, intermediate filament proteins, and associated proteins, such as motor proteins, microtubule-associated proteins (MAPs), and cofilin. Read More

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Neuroprotective effects of NDEELNK from sea cucumber ovum against scopolamine-induced PC12 cell damage through enhancing energy metabolism and upregulation of the PKA/BDNF/NGF signaling pathway.

Food Funct 2021 Jul 14. Epub 2021 Jul 14.

National Engineering Research Center of Seafood, School of Food Science and Technology, Dalian Polytechnic University, Dalian 116034, P. R. China.

The aim of the study was to evaluate the neuroprotective function of sea cucumber ovum peptide-derived NDEELNK and explore the underlying molecular mechanisms. NDEELNK exerted the neuroprotective effect by improving the acetylcholine (ACh) level and reducing the acetylcholinesterase (AChE) activity in PC12 cells. By molecular docking, we confirmed that the NDEELNK backbone and AChE interacted through hydrophobic and hydrogen bonds in contact with the amino acid residues of the cavity wall. Read More

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Anticholinesterase Activity of Eight Medicinal Plant Species: and Studies in the Search for Therapeutic Agents against Alzheimer's Disease.

Evid Based Complement Alternat Med 2021 25;2021:9995614. Epub 2021 Jun 25.

Department of Science, University of Basilicata, Viale Dell'Ateneo Lucano 10, Potenza 85100, Italy.

Many Bangladeshi medicinal plants have been used to treat Alzheimer's disease and other neurodegenerative diseases. In the present study, the anticholinesterase effects of eight selected Bangladeshi medicinal plant species were investigated. Species were selected based on the traditional uses against CNS-related diseases. Read More

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A highly sensitive acetylcholinesterase electrochemical biosensor based on Au-Tb alloy nanospheres for determining organophosphate pesticides.

Nanotechnology 2021 Jul 13. Epub 2021 Jul 13.

Beihang University, 37 Xueyuan Road, Haidian District, Beijing, Beijing, 100083, CHINA.

Accurately detect the residues of organophosphate pesticides(OPs) in food and environment is critical to our daily lives. In this study, we developed a novel acetylcholinesterase (AChE) biosensor based on Au-Tb alloy nanospheres (NSs) for rapid and sensitive detection of OPs for the first time. Au-Tb alloy nanospheres that with good conductivity and biocompatibility were produced with a mild hydrothermal. Read More

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A subchronic low-dose exposure of a glyphosate-based herbicide induces depressive and anxious-like behavior in mice: quercetin therapeutic approach.

Environ Sci Pollut Res Int 2021 Jul 12. Epub 2021 Jul 12.

Laboratório de Biotecnologia da Reprodução (Biotech), Campus Uruguaiana, Universidade Federal do Pampa (UNIPAMPA), Uruguaiana, RS, CEP 97500-970, Brazil.

In this study, we investigated the possible role of pesticide exposure in contributing to neurological diseases such as depression. Here, we evaluated whether a subchronic low dose of a glyphosate-based herbicide (GBH) could induce alterations in the central nervous system, using the flavonoid quercetin as a therapeutic strategy. Forty mice were divided into four treatment groups: control, GBH, quercetin, and GBH+Quer groups and received 50 mg/kg of GBH solution, 30 mg/kg of quercetin, and/or vehicles for 30 days via gavage. Read More

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Pharmacophore-based drug design of AChE and BChE dual inhibitors as potential anti-Alzheimer's disease agents.

Bioorg Chem 2021 Jul 7;114:105149. Epub 2021 Jul 7.

School of Life Science, Ludong University, Yantai, Shandong 264025, China.

For the Alzheimer's disease (AD) with complex pathogenesis, single target drugs represent one of the most effective therapeutic strategies in clinical. However, the traditional concept of "a disease, a target" is difficult to find very effective drugs, and multi-target drugs have already become new hot spot in drug development for this disease. In our present study, our efforts toward discovering new cholinesterase (ChE) inhibitors aided by computational methods will provide useful information as anti-AD agents in the future. Read More

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Neurological effects of acute exposure to caffeine and organophosphates in mice.

Pol J Vet Sci 2021 Jun;24(2):211-216

Department of Pathophysiology, Medical University of Lublin, Jaczewskiego 8, 20-090 Lublin, Poland.

Organophosphate (OP) pesticides are commonly known for their neurotoxicity. In the current experiments, two OPs used agriculturally, chlorpyrifos and dimethoate, were separately adminis- tered with centrally acting caffeine that is known to affect the pharmacological action of other substances. The aim of this study was to determine whether the combination of OP and caffeine may influence their neurotoxic potential. Read More

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Neuroactive venom compounds obtained from as potential leads for neurodegenerative diseases: insights on their acetylcholinesterase and beta-secretase inhibitory activities .

J Venom Anim Toxins Incl Trop Dis 2021 28;27:e20210009. Epub 2021 Jun 28.

Department of Biochemistry, Faculty of Pharmacy, University of Santo Tomas, Manila, Philippines, 1008.

Background: Spider venom is a rich cocktail of neuroactive compounds designed to prey capture and defense against predators that act on neuronal membrane proteins, in particular, acetylcholinesterases (AChE) that regulate synaptic transmission through acetylcholine (ACh) hydrolysis - an excitatory neurotransmitter - and beta-secretases (BACE) that primarily cleave amyloid precursor proteins (APP), which are, in turn, relevant in the structural integrity of neurons. The present study provides preliminary evidence on the therapeutic potential of venom against neurodegenerative diseases.

Methods: Spider venom was extracted by electrostimulation and fractionated by reverse-phase high-performance liquid chromatography (RP-HPLC) and characterized by matrix-assisted laser desorption ionization-time flight mass spectrometry (MALDI-TOF-MS). Read More

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The chemical diversity, the attractant, anti-acetylcholinesterase, and antifungal activities of metabolites from biocontrol Trichoderma harzianum uncovered by OSMAC strategy.

Bioorg Chem 2021 Jul 6;114:105148. Epub 2021 Jul 6.

Functional Molecules Analysis and Biotransformation Key Laboratory of Universities in Yunnan Province, Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, 2nd Cuihu North Road, Kunming 650091, China. Electronic address:

Eight new compounds (1-8) were discovered from Trichoderma harzianum associated with edible mushroom by the one strain many compounds (OSMAC) strategy. Triharzianin A (1) is the first naturally scaffold characterized by a C-prostaglandin skeleton. The configurations of 1-3, and 5 were determined by the Mosher's method, experimental and calculated ECD spectra, and plausible biosynthesis of stereospecific epoxidation. Read More

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Computational evidence of new putative allosteric sites in the acetylcholinesterase receptor.

J Mol Graph Model 2021 Sep 2;107:107981. Epub 2021 Jul 2.

Department of Bioinformatics, Institute of Biochemistry and Biophysics, University of Tehran, Tehran, Iran.

Acetylcholinesterase (AChE), with a rigid structure and buried active site at the end of a deep narrow gorge, is interesting enough to solve the paradox between high catalytic activity and unavailability of the active site in treatment of Alzheimer's disease (AD). In this way, the blind docking process is performed on an ensemble of AChE structures created with molecular dynamics (MD) simulations to survey the whole space of AChE to find multiple access pathways to the active site and ranking them based on their affinity scores. Our results show that there are other allosteric binding sites in the protein structure whose inhibition, can affect protein function by disrupting the release of the Acetylcholine (AC) degradation products. Read More

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September 2021

Tranilast, a Transient Receptor Potential Vanilloid 2 Channel (TRPV2) Inhibitor Attenuates Amyloid β-Induced Cognitive Impairment: Possible Mechanisms.

Neuromolecular Med 2021 Jul 6. Epub 2021 Jul 6.

Department of Pharmacology and Toxicology, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, S.A.S. Nagar, Mohali, Punjab, 160062, India.

Alzheimer's disease (AD) is associated with the accumulation of β-amyloid and leads to cognitive impairment. Numerous studies have established that neuronal calcium homeostasis is perturbed in AD. Recently, transient receptor potential vanilloid 2 (TRPV2) channels, a non-selective calcium-permeable channel, have been investigated in several diseases. Read More

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Acetylcholinesterase and monoamine oxidase-B inhibitory activities by ellagic acid derivatives isolated from Castanopsis cuspidata var. sieboldii.

Sci Rep 2021 Jul 6;11(1):13953. Epub 2021 Jul 6.

Department of Pharmacy, and Research Institute of Life Pharmaceutical Sciences, Sunchon National University, Suncheon, 57922, Republic of Korea.

Among 276 herbal extracts, a methanol extract of Castanopsis cuspidata var. sieboldii stems was selected as an experimental source for novel acetylcholinesterase (AChE) inhibitors. Five compounds were isolated from the extract by activity-guided screening, and their inhibitory activities against butyrylcholinesterase (BChE), monoamine oxidases (MAOs), and β-site amyloid precursor protein cleaving enzyme 1 (BACE-1) were also evaluated. Read More

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Butyrylcholinesterase as a perioperative complication marker in patients after transcatheter aortic valve implantation: a prospective observational study.

BMJ Open 2021 Jul 6;11(7):e042857. Epub 2021 Jul 6.

Department of Anesthesiology, University Hospital Regensburg, Regensburg, Germany

Objectives: Transcatheter aortic valve implantation (TAVI) is performed in elderly patients with severe aortic valve stenosis and increased operative risks. We tested the hypothesis that acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) have a predictive value for prevalent complications after TAVI and could serve as indicators of systemic inflammation in the early postoperative period.

Design: Prospective observational study. Read More

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Isolation and characterization of chemical constituents from roots and their enzyme inhibitory and antioxidant effects.

Z Naturforsch C J Biosci 2021 Jul 5. Epub 2021 Jul 5.

Department of Chemistry, Faculty of Science, Muğla Sıtkı Koçman University, 48000, Muğla, Turkey.

Isolation and bioactive effects of the roots of L. were firstly investigated herein. Enzyme (acetylcholinesterase, butyrylcholinesterase, urease, α-amylase, α-glucosidase, and tyrosinase) inhibitory effects of root extracts were tested. Read More

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Larvicidal activity and in silico studies of cinnamic acid derivatives against Aedes aegypti (Diptera: Culicidae).

Bioorg Med Chem 2021 Jun 28;44:116299. Epub 2021 Jun 28.

Institute of Chemistry and Biotechnology, Federal University of Alagoas, Avenida Lourival Melo Mota, 57072-970 Maceio, AL, Brazil. Electronic address:

Cinnamic acid derivatives (CAD's) represent a great alternative in the search for insecticides against Aedes aegypti mosquitoes since they have antimicrobial and insecticide properties. Ae. aegypti is responsible for transmitting Dengue, Chikungunya, and Zika viruses, among other arboviruses associated with morbimortality, especially in developing countries. Read More

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Studies on the affinity of 6-[(-(cyclo)aminoalkyl)oxy]-4-chromen-4-ones for sigma 1/2 receptors.

RSC Med Chem 2021 Jun 20;12(6):1000-1004. Epub 2021 May 20.

Laboratory of Medicinal Chemistry, IQOG, CSIC C/Juan de la Cierva 3 28006 Madrid Spain

Sigma (σ) receptors represent attractive targets for the development of potential agents for the treatment of several disorders, including Alzheimer's disease and neuropathic pain. In the search for multitarget small molecules (MSMs) against such disorders, we have re-discovered chromenones as new affine σ/σ ligands. 6-(4-(Piperidin-1-yl)butoxy)-4-chromen-4-one (), a previously identified MSM with potent dual-target activities against acetylcholinesterase and monoamine oxidase B, also exhibited σ/σ affinity. Read More

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Cholinesterase inhibitory activity of tinosporide and 8-hydroxytinosporide isolated from : and studies targeting management of Alzheimer's disease.

Saudi J Biol Sci 2021 Jul 30;28(7):3893-3900. Epub 2021 Mar 30.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Dhaka, Dhaka 1000, Bangladesh.

Tinosporide and 8-hydroxytinosporide isolated from were evaluated for acetylcholinesterase (AChE) and butylcholinesterase (BuChE) inhibitory activities. The structure of the compound was confirmed by spectroscopic analysis, whereas cholinesterase inhibition was investigated by Ellman method using donepezil as standard drug and the data were presented as IC (μg/ml ± SEM). Furthermore, donepezil, tinosporide and 8-hydroxytinosporide were executed for docking analysis. Read More

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Dietary flaxseed's protective effects on body tissues of mice after oral exposure to xylene.

Saudi J Biol Sci 2021 Jul 27;28(7):3789-3798. Epub 2021 Mar 27.

Faculty of Natural Sciences, Constantine the Philosopher University in Nitra, Nábrežie mládeže 91, 949 74 Nitra, Slovak Republic.

Xylene is a common pollutant in the environment that enters the body of animals and humans in various ways, but most often through the respiratory tract and adversely affects their overall health. However, xylene effects after oral exposure have not been sufficiently studied. This study aimed to investigate the effects of xylene exposure on the mouse organism and to identify possible beneficial effects of flaxseed on such exposure. Read More

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2',6'-dihydroxy-4'-methoxy dihydrochalcone improves the cognitive impairment of Alzheimer's disease: a structure-activity relationship study.

Curr Top Med Chem 2021 Jul 1. Epub 2021 Jul 1.

Postgraduate Program in Pharmaceutical Sciences, University of Itajaí Valley, UNIVALI- Itajaí, SC, Brazil.

Background: Chalcones and dihydrochalcones present potent inhibition of acetylcholinesterase, which is currently considered the most efficient approach for symptomatic treatment of Alzheimer's disease.

Objective: The present study aimed to explore the potential benefits of 2',6'-dihydroxy-4'-methoxy dihydrochalcone on the cognitive deficits of animals submitted to the streptozotocin-induced Alzheimer's model, as well as to evaluate the possible mechanisms of action.

Methods: Learning and memory functions of different groups of animals were submitted to the streptozotocin-induced Alzheimer's model (STZ 2. Read More

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Toxicological insights of Spike fragments SARS-CoV-2 by exposure environment: A threat to aquatic health?

J Hazard Mater 2021 Jun 25;419:126463. Epub 2021 Jun 25.

Post-graduation Program in Biotechnology and Biodiversity, Goiano Federal Institution and Federal University of Goiás, GO, Brazil; Biological Research Laboratory, Post-graduation Program in Conservation of Cerrado Natural Resources, Goiano Federal Institute - Urata Campus, GO, Brazil. Electronic address:

The Spike protein (S protein) is a critical component in the infection of the new coronavirus (SARS-CoV-2). The objective of this work was to evaluate whether peptides from S protein could cause negative impact in the aquatic animals. The aquatic toxicity of SARS-CoV-2 Spike protein peptides derivatives has been evaluated in tadpoles (n = 50 tadpoles/5 replicates of 10 animals) from species Physalaemus cuvieri (Leptodactylidae). Read More

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