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acetylcholinesterase

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https://www.readbyqxmd.com/read/28108398/association-between-butyrylcholinesterase-and-cerebrospinal-fluid-biomarkers-in-alzheimer-s-disease-patients
#1
António José Gabriel, Maria Rosário Almeida, Maria Helena Ribeiro, João Durães, Miguel Tábuas-Pereira, Ana Cristina Pinheiro, Rui Pascoal, Isabel Santana, Inês Baldeiras
The deficit of cholinergic activity is one of the main findings in Alzheimer's disease (AD), and is related to the synthesis of acetylcholine, and the hydrolysing enzymes, acetylcholinesterase and butyrylcholinesterase (BuChE). Together with the Apolipoprotein E-ε4 allele (ApoE-ε4), the BuChE-K variant has been proposed to increase AD risk in certain populations. In addition, this polymorphism has been associated with a lower capacity to attenuate β-amyloid aggregation. In the present study we explored the interaction of the BuChE-K variant with its activity in CSF, conventional AD biomarkers and ApoE genotype...
January 17, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28106328/on-the-influence-of-the-protonation-states-of-active-site-residues-on-ache-reactivation-a-qm-mm-approach
#2
Thomas Driant, Florian Nachon, Cyril Ollivier, Pierre-Yves Renard, Etienne Derat
Acetylcholinesterase (AChE) is an enzyme of the serine hydrolase superfamily and a mediator of the signal transmission at cholinergic synapses catalysing acetylcholine cleavage into an acetate and a choline. This enzyme is vulnerable to covalent inhibition by organophosphate compounds (like VX). The covalent inhibition of AChE does not revert spontaneously and in order to restore catalytic activity known reactivator compounds have limited action. Simulations of VX-inhibited AChE reactivation by pralidoxime, a classical reactivator, were performed by QM/MM...
January 19, 2017: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/28104598/pisa-syndrome-due-to-donepezil-pharmacokinetic-interactions-to-blame
#3
David Pollock, Emma Cunningham, Bernadette McGuinness, Anthony Peter Passmore
We report a case of Pisa syndrome (PS) due to the acetylcholinesterase inhibitor donepezil which may have been precipitated by pharmacokinetic interactions with commonly used medications. PS is defined as a reversible lateral bending of the trunk with a tendency to lean to one side. This is a rare but very distressing complication with this commonly used medication which was not initially recognised, leading to increasing disability for the patient and significant carer stress. Cessation of donepezil and modulation of potential interacting medications resulted in complete resolution...
January 18, 2017: Age and Ageing
https://www.readbyqxmd.com/read/28102474/anti-amnestic-effect-of-curcumin-in-combination-with-donepezil-an-anticholinesterase-drug-involvement-of-cholinergic-system
#4
Ayodele Jacob Akinyemi, Ganiyu Oboh, Sunday Idowu Oyeleye, Opeyemi Ogunsuyi
Recently, combination therapy involving cholinesterase (ChE) inhibitor with other neuroprotective agents has shown better desirable effect in the management/prevention of dementia but limited information is available on their effect with dietary polyphenols. Hence, this study sought to assess the combined pretreatment effect of curcumin, the major polyphenolic compound of turmeric (Curcuma longa) rhizomes, with donepezil, a cholinesterase inhibitor, on cognitive function in scopolamine-induced memory impairment in rats...
January 19, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/28101995/cholinergic-signaling-in-myelination
#5
REVIEW
R Douglas Fields, Dipankar J Dutta, Jillian Belgrad, Maya Robnett
There is a long history of research on acetylcholine (ACh) function in myelinating glia, but a resurgence of interest recently as a result of the therapeutic potential of manipulating ACh signaling to promote remyelination, and the broader interest in neurotransmitter signaling in activity-dependent myelination. Myelinating glia express all the major types of muscarinic and nicotinic ACh receptors at different stages of development, and acetylcholinesterase and butyrylcholinesterase are highly expressed in white matter...
January 19, 2017: Glia
https://www.readbyqxmd.com/read/28100726/decreased-intestinal-acetylcholinesterase-in-early-parkinson-disease-an-11c-donepezil-pet-study
#6
Tatyana D Fedorova, Louise B Seidelin, Karoline Knudsen, Anna C Schacht, Jacob Geday, Nicola Pavese, David J Brooks, Per Borghammer
OBJECTIVE: To investigate systemic levels of acetylcholinesterase in early Parkinson disease (PD) with (11)C-donepezil PET, a potential marker of parasympathetic innervation. METHODS: This was a cross-sectional study with 19 patients with early-stage PD (disease duration 1.5 ± 0.6 years) and 16 age-matched controls who had clinical assessments, olfaction tests, and (11)C-donepezil PET to measure acetylcholinesterase density in peripheral organs. RESULTS: The patients with PD showed significantly reduced (11)C-donepezil uptake in the small intestine (-14%, p = 0...
January 18, 2017: Neurology
https://www.readbyqxmd.com/read/28100082/synthesis-and-bioactivity-of-several-new-hetaryl-sulfonamides
#7
Parham Taslimi, Afsun Sujayev, Sevgi Mamedova, Pınar Kalın, İlhami Gulçin, Nastaran Sadeghian, Sukru Beydemir, O Irfan Kufrevioglu, Saleh H Alwasel, Vagif Farzaliyev, Sabir Mamedov
1-(4-Methylsulfonyl)-2-thione-4-aryl-5-Z-6-methyl and oxyalkyl-imidazoles were synthesized from different tetrahydropyrimidinethiones and aryl sulfonyl chloride. These compunds were tested for metal chelating effects and to determine the phrase in which inhibition occured between two physiologically pertinent compunds and carbonic anhydrase (CA) isozymes I and II (hCA I and II), butyrylcholinesterase (BChE) and acetylcholinesterase (AChE). AChE was detected in high concentrations in the brain and red blood cells...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097911/design-synthesis-and-docking-study-of-novel-coumarin-ligands-as-potential-selective-acetylcholinesterase-inhibitors
#8
Fatih Sonmez, Belma Zengin Kurt, Isil Gazioglu, Livia Basile, Aydan Dag, Valentina Cappello, Tiziana Ginex, Mustafa Kucukislamoglu, Salvatore Guccione
New coumaryl-thiazole derivatives with the acetamide moiety as a linker between the alkyl chains and/or the heterocycle nucleus were synthesized and in vitro tested as acetylcholinesterase (AChE) inhibitors. 2-(diethylamino)-N-(4-(2-oxo-2H-chromen-3-yl)thiazol-2-yl)acetamide (6c, IC50 value of 43 nM) was the best AChE inhibitor with a selectivity index of 4151.16 over BuChE. Kinetic study of AChE inhibition revealed that 6c was a mixed-type inhibitor. Moreover, the result of H4IIE hepatoma cell toxicity assay for 6c showed negligible cell death...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097907/the-lignicolous-fungus-trametes-versicolor-l-lloyd-1920-a-promising-natural-source-of-antiradical-and-ache-inhibitory-agents
#9
Ljiljana Janjušević, Maja Karaman, Filip Šibul, Giuseppina Tommonaro, Carmine Iodice, Dragica Jakovljević, Boris Pejin
This study aimed to determine antiradical (DPPH(•) and (•)OH) and acetylcholinesterase (AChE) inhibitory activities along with chemical composition of autochtonous fungal species Trametes versicolor (Serbia). A total of 38 phenolic compounds with notable presence of phenolic acids were identified using HPLC/MS-MS. Its water extract exhibited the highest antiradical activity against (•)OH (3.21 μg/mL), among the rest due to the presence of gallic, p-coumaric and caffeic acids. At the concentration of 100 μg/mL, the same extract displayed a profound AChE inhibitory activity (60...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097466/trachyspermum-ammi-seeds-supplementation-helps-reverse-scopolamine-alprazolam-and-electroshock-induced-amnesia
#10
Kapil Soni, Milind Parle
The present study was designed to explore the beneficial effects of successive 10 days administration of Trachyspermum ammi seed's powder (TASP) along with diet (at the dose of 0.5%, 1.0% and 2.0% w/w) on learning and memory of mice. A total of 306 mice divided in 51 equal groups were employed in the study. Passive avoidance paradigm (PAP) and Object recognition Task (ORT) were employed as exteroceptive models. The brain acetylcholinesterase activity (AChE), serum cholesterol, brain monoaldehyde (MDA), brain reduced glutathione (GSH) and brain nitrite were estimated and Alprazolam, Scopolamine and Electroshock induced amnesia was employed to describe the actions...
January 17, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28096851/acetylcholinesterase-inhibitor-improves-learning-and-memory-impairment-induced-by-toxoplasma-gondii-infection
#11
Hossein Mahmoudvand, Vahid Sheibani, Hossein Keshavarz, Saeedeh Shojaee, Khadijeh Esmaeelpour, Naser Ziaali
BACKGROUND: Here, we established the mouse models of chronic toxoplasmosis by T. gondii Tehran strain to provide a good understanding about defining the possible association between T. gondii exposure and learning and memory impairments. Moreover, as secondary objective of the present study, we hypothesized whether administration of an acetylcholinesterase (AChE) inhibitor could reduce learning and memory impairments induced by T. gondii infection. METHODS: Twenty-four male BALB/c mice were used to establishment of latent toxoplasmosis...
April 2016: Iranian Journal of Parasitology
https://www.readbyqxmd.com/read/28093699/anti-alzheimer-s-disease-activity-of-compounds-from-the-root-bark-of-morus-alba-l
#12
Eun Bi Kuk, A Ra Jo, Seo In Oh, Hee Sook Sohn, Su Hui Seong, Anupom Roy, Jae Sue Choi, Hyun Ah Jung
The inhibition of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein cleaving enzyme 1 (BACE1) plays important roles in prevention and treatment of Alzheimer's disease (AD). Among the individual parts of Morus alba L. including root bark, branches, leaves, and fruits, the root bark showed the most potent enzyme inhibitory activities. Therefore, the aim of this study was to evaluate the anti-AD activity of the M. alba root bark and its isolate compounds, including mulberrofuran G (1), albanol B (2), and kuwanon G (3) via inhibition of AChE, BChE, and BACE1...
January 16, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28091956/does-caffeine-influence-the-anticholinesterase-and-antioxidant-properties-of-donepezil-evidence-from-in-vitro-and-in-vivo-studies
#13
Ganiyu Oboh, Opeyemi Babatunde Ogunsuyi, Oluwaseyi Emmanuel Olonisola
Caffeine is adjudged world's most consumed pharmacologically active food component. With reports of the potential cognitive enhancing properties of caffeine, we sought to investigate if caffeine can influence the anticholinesterase and antioxidant properties of donepezil-a selective acetylcholinesterase (AChE) inhibitor used in the management of Alzheimer's disease (AD). In vitro, we investigated the effect of donepezil (DON), caffeine (CAF) and their various combinations on the activity of AChE in rat brain homogenate, as well as determined their antioxidant properties...
January 13, 2017: Metabolic Brain Disease
https://www.readbyqxmd.com/read/28091410/molecular-mechanisms-of-increased-heart-rate-in-shenxianshengmai-treated-bradycardia-rabbits
#14
Zhou-Ying Liu, Jian Huang, Na-Na Liu, Min Zheng, Tao Zhao, Bu-Chang Zhao, Yi-Min Wang, Jie-Lin Pu
BACKGROUND: The molecular mechanisms of Shenxianshengmai (SXSM), a traditional Chinese medicine, on bradycardia have been incompletely understood. The study tried to investigate the gene expression profile and proteomics of bradycardia rabbits' hearts after SXSM treatment. METHODS: Twenty-four adult rabbits were randomly assigned in four groups: sham, model, model plus SXSM treatment, and sham plus SXSM treatment groups. Heart rate was recorded in all rabbits. Then, total RNA of atria and proteins of ventricle were isolated and quantified, respectively...
2017: Chinese Medical Journal
https://www.readbyqxmd.com/read/28089589/synthesis-anticholinesterase-activity-and-molecular-modeling-study-of-novel-carbamate-substituted-thymol-carvacrol-derivatives
#15
Belma Zengin Kurt, Isil Gazioglu, Aydan Dag, Ramin Ekhteiari Salmas, Gülru Kayık, Serdar Durdagi, Fatih Sonmez
New thymol and carvacrol derivatives with the carbamate moiety were synthesized and their inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were evaluated. 5-isopropyl-2-methylphenyl(3-fluorophenyl)carbamate (29) was found to be the most potent AChE inhibitor with IC50 values of 2.22μM, and 5-isopropyl-2-methylphenyl (4-fluorophenyl)carbamate (30) exhibited the strongest inhibition against BuChE with IC50 value of 0.02μM. Additionally, the result of H4IIE hepatoma cell toxicity assay for compounds 18, 20, 29, 30 and 35 showed negligible cell death at 0...
December 26, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28088901/advanced-structure-activity-relationships-applied-to-mentha-spicata-l-subsp-spicata-essential-oil-compounds-as-ache-and-nmda-ligands-in-comparison-with-donepezil-galantamine-and-memantine-new-approach-in-brain-disorders-pharmacology
#16
Speranta Avram, Mernea Maria, Eyup Bagci, Lucian Hritcu, Livia-Cristina Borcan, Dan Mihailescu
BACKGROUND: Alzheimer's disease (AD) therapy is based on several natural and synthetic compounds that act as acetylcholinesterase (AChE) and N-methyl-D-aspartate receptor (NMDA) ligands that have limited efficiency in relieving AD symptoms. Recent studies show that inhibitors isolated from Mentha spicata L. subsp. spicata are promising for AD therapy. OBJECTIVE: We aimed to identify novel and more potent phytopharmaceutical compounds for AD treatment by taking into account the compounds from Mentha spicata L...
January 13, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28081467/oxidative-stress-and-mrna-expression-of-acetylcholinesterase-in-the-leukocytes-of-ischemic-patients
#17
Mesut Işık, Şükrü Beydemir, Aslan Yılmaz, Muhammet Emin Naldan, Hatice Esra Aslan, İlhami Gülçin
BACKGROUND: Pathogenesis of ischemic brain injury is occurred by crucial metabolic reasons. For instance, oxidative stress from free radical generation is causing to the thrombotic cerebrovascular stroke. In this case, the measurement of the oxidative stress is very important for a better understanding of the stroke pathophysiology. Because, the oxidative stress in stroke is generally assumed as one of the mechanisms taking part in neuronal damage. Thus, oxidative stress has a vital role in the cholinergic system...
January 9, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28078916/in-vivo-protection-studies-of-bis-quaternary-2-hydroxyimino-n-pyridin-3-yl-acetamide-derivatives-hnk-oximes-against-tabun-and-soman-poisoning-in-swiss-albino-mice
#18
P Kumar, D Swami, D P Nagar, K P Singh, J Acharya, H N Karade, R Yadav
The study reports antidotal efficacy of three HNK [ bis quaternary 2-(hydroxyimino)-N-(pyridin-3yl) acetamide derivatives] and pralidoxime (2-PAM), against soman and tabun poisoning in Swiss albino mice. Protection index (PI) was determined (treatment doses: HNK oximes, ×0.20 of their median lethal dose (LD50) and 2-PAM, 30 mg/kg, intramuscularly (im)) together with atropine (10 mg/kg, intraperitoneally). Probit log doses with difference of 0.301 log of LD50 of the nerve agents administered and inhibition of acetylcholinesterase (AChE) activity by 50% (IC50) was calculated at optimized time in brain and serum...
January 1, 2017: Human & Experimental Toxicology
https://www.readbyqxmd.com/read/28078633/benzodiazepine-use-and-risk-of-developing-alzheimer-s-disease-a-case-control-study-based-on-swiss-claims-data
#19
Fabienne A Biétry, Alena M Pfeil, Oliver Reich, Matthias Schwenkglenks, Christoph R Meier
BACKGROUND: A possible association between benzodiazepine use and Alzheimer's disease (AD) has been hypothesized in previous studies. OBJECTIVES: Using claims data from the Helsana Group, a large Swiss health insurance provider, we examined the association between previous benzodiazepine use and the risk of AD. METHODS: We conducted a matched case-control study and identified 1438 incident AD cases between 2013 and 2014 based on recorded first-time use of drugs used to treat AD [i...
January 11, 2017: CNS Drugs
https://www.readbyqxmd.com/read/28078612/ameliorative-effect-of-ginsenoside-rg1-on-lipopolysaccharide-induced-cognitive-impairment-role-of-cholinergic-system
#20
Yang Jin, Jian Peng, Xiaona Wang, Dong Zhang, Tianyin Wang
Bacterial endotoxin lipopolysaccharide (LPS) can induce systemic inflammation, and therefore disrupt learning and memory processes. Ginsenoside Rg1, a major bioactive component of ginseng, is shown to greatly improve cognitive function. The present study was designed to further investigate whether administration of ginsenoside Rg1 can ameliorate LPS-induced cognitive impairment in the Y-maze and Morris water maze (MWM) task, and to explore the underlying mechanisms. Results showed that exposure to LPS (500 μg/kg) significantly impaired working and spatial memory and that repeated treatment with ginsenoside Rg1 (200 mg/kg/day, for 30 days) could effectively alleviate the LPS-induced cognitive decline as indicated by increased working and spatial memory in the Y-maze and MWM tests...
January 11, 2017: Neurochemical Research
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