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acetylcholinesterase

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https://www.readbyqxmd.com/read/27911323/short-term-response-is-not-predictive-of%C3%A2-long-term-response-to%C3%A2-acetylcholinesterase-inhibitors-in-old-age-subjects-with-alzheimer-s-disease-a%C3%A2-real-world-study
#1
Virginia Boccardi, Marta Baroni, Nicoletta Smirne, Alessandra Clodomiro, Sara Ercolani, Annalisa Longo, Carmelinda Ruggiero, Amalia C Bruni, Patrizia Mecocci
BACKGROUND: Most of clinical guidelines recommend discontinuing treatment with cholinesterase inhibitors (ChEIs) in patients with Alzheimer's disease (AD) who do not show an initial response to therapy as evaluated with the Mini-Mental State Examination (MMSE) scale. However, understanding the relationship between the initial response to ChEI treatment and the subsequent course of the disease is extremely important in clinical practice, but evidence is limited, particularly in the old-old population...
November 29, 2016: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/27911294/deleterious-effect-of-butyrylcholinesterase-k-variant-in-donepezil-treatment-of-mild-cognitive-impairment
#2
Sophie Sokolow, Xiaohui Li, Lucia Chen, Kent D Taylor, Jerome I Rotter, Robert A Rissman, Paul S Aisen, Liana G Apostolova
BACKGROUND: Donepezil is an acetylcholinesterase inhibitor frequently prescribed for the treatment of mild cognitive impairment (MCI) though not approved by the Food and Drug Administration for this indication. In Alzheimer's disease, butyrylcholinesterase (BChE) activity increases with disease progression and may replace acetylcholinesterase function. The most frequent polymorphism of BChE is the K-variant, which is associated with lower acetylcholine-hydrolyzing activity. BChE-K polymorphism has been studied in Alzheimer's disease progression and donepezil therapy, and has led to contradictory results...
November 29, 2016: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/27910192/novel-tacrine-based-pyrano-3-4-5-6-pyrano-2-3-b-quinolinones-synthesis-and-cholinesterase-inhibitory-activity
#3
Roshanak Hariri, Zahra Afshar, Mohammad Mahdavi, Maliheh Safavi, Mina Saeedi, Zahra Najafi, Reyhaneh Sabourian, Elahe Karimpour-Razkenari, Najmeh Edraki, Farshad Homayouni Moghadam, Abbas Shafiee, Mahnaz Khanavi, Tahmineh Akbarzadeh
In order to develop effective anti-cholinesterase compounds, a novel series of pyrano[3',4':5,6]pyrano[2,3-b]quinolinones were designed, synthesized, and evaluated in vitro against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). All derivatives showed very good AChE inhibitory (AChEI) activity (IC50  = 0.37-5.62 μM) compared with rivastigmine (IC50  = 11.07 μM). Among them, 11-amino-12-(2,3-dichlorophenyl)-3-methyl-7,8,9,10-tetrahydropyrano[3',4':5,6]pyrano[2,3-b]quinolin-1(12H)-one (6f) displayed the best inhibitory activity...
December 2016: Archiv der Pharmazie
https://www.readbyqxmd.com/read/27908752/n-propargylpiperidines-with-naphthalene-2-carboxamide-or-naphthalene-2-sulfonamide-moieties-potential-multifunctional-anti-alzheimer-s-agents
#4
Urban Košak, Damijan Knez, Nicolas Coquelle, Boris Brus, Anja Pišlar, Florian Nachon, Xavier Brazzolotto, Janko Kos, Jacques-Philippe Colletier, Stanislav Gobec
In the brains of patients with Alzheimer's disease, the enzymatic activities of butyrylcholinesterase (BChE) and monoamine oxidase B (MAO-B) are increased. While BChE is a viable therapeutic target for alleviation of symptoms caused by cholinergic hypofunction, MAO-B is a potential therapeutic target for prevention of neurodegeneration in Alzheimer's disease. Starting with piperidine-based selective human (h)BChE inhibitors and propargylamine-based MAO inhibitors, we have designed, synthesized and biochemically evaluated a series of N-propargylpiperidines...
November 19, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27908719/ultrahigh-pressure-assisted-enzymatic-extraction-maximizes-the-yield-of-longan-pulp-polysaccharides-and-their-acetylcholinesterase-inhibitory-activity-in-vitro
#5
Yajuan Bai, Lei Liu, Ruifen Zhang, Fei Huang, Yuanyuan Deng, Mingwei Zhang
An extraction method employing ultrahigh pressure-assisted enzymatic treatment was developed and optimized by response surface methodology to increase the yield of longan pulp polysaccharides (LP-UE). A maximum polysaccharides yield of 8.55% was obtained under the optimal conditions of 407MPa ultrahigh pressure maintained for 6min with an enzyme to pretreated material ratio of 1:100, an enzymolysis time of 1.7h and a water to pretreated material ratio of 42ml/g. Subsequently, the physicochemical properties and acetylcholinesterase (AChE) inhibitory activity of LP-UE were compared to those of longan pulp polysaccharides (LP) extracted by hot water (LP-H), ultrahigh pressure (LP-U) or enzymatic treatment (LP-E)...
November 28, 2016: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/27906609/glyphosate-adversely-affects-danio-rerio-males-acetylcholinesterase-modulation-and-oxidative-stress
#6
Fernanda Moreira Lopes, Sergiane Souza Caldas, Ednei Gilberto Primel, Carlos Eduardo da Rosa
It has been demonstrated that glyphosate-based herbicides are toxic to animals. In the present study, reactive oxygen species (ROS) generation, antioxidant capacity against peroxyl radicals (ACAP), and lipid peroxidation (LPO), as well as the activity and expression of the acetylcholinesterase (AChE) enzyme, were evaluated in Danio rerio males exposed to 5 or 10 mg/L of glyphosate for 24 and 96 h. An increase in ACAP in gills after 24 h was observed in the animals exposed to 5 mg/L of glyphosate. A decrease in LPO was observed in brain tissue of animals exposed to 10 mg/L after 24 h, while an increase was observed in muscle after 96 h...
December 1, 2016: Zebrafish
https://www.readbyqxmd.com/read/27901474/cerebellar-neurochemical-and-histopathological-changes-in-rat-model-of-parkinson-s-disease-induced-by-intrastriatal-injection-of-rotenone
#7
Yasser A Khadrawy, Iman M Mourad, Haitham S Mohammed, Neveen A Noor, Heba S Aboul Ezz
The aim of the present work was to investigate the neurochemical changes induced in the cerebellum of rat model of Parkinson's disease (PD). Rats were divided into two groups; control and rat model of PD induced by the intrastriatal injection of rotenone. As compared to control, a significant increase in the excitatory amino acid neurotransmitters; glutamate and aspartate together with a significant decrease in the inhibitory amino acids, GABA, glycine and taurine were observed in the cerebellum of rat model of PD...
November 30, 2016: General Physiology and Biophysics
https://www.readbyqxmd.com/read/27901381/effects-of-fisetin-on-hyperhomocysteinemia-induced-experimental-endothelial-dysfunction-and-vascular-dementia
#8
Boyina Hemanth Kumar, Ravula Arun Reddy, Jerald Mahesh Kumar, B Dinesh Kumar, Prakash V Diwan
This study was designed to investigate the effects of fisetin (FST) on hyperhomocysteinemia (HHcy)-induced experimental endothelial dysfunction (ED) and vascular dementia (VaD) in rats. Wistar rats were randomly divided into 8 groups: control, vehicle control, l-methionine, FST (5, 10, and 25 mg/kg, p.o.), FST-per se (25 mg/kg, p.o.), and donepezil (0.1 mg/kg, p.o.). l-Methionine administration (1.7 g/kg, p.o.) for 32 days induced HHcy. ED and VaD induced by HHcy were determined by vascular reactivity measurements, behavioral analysis using Morris water maze and Y-maze, along with a biochemical and histological evaluation of thoracic aorta and brain tissues...
August 11, 2016: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/27900576/time-course-behavioral-safety-and-protective-efficacy-of-centrally-active-reversible-acetylcholinesterase-inhibitors-in-cynomolgus-macaques
#9
Lindsey R Hamilton, Steven C Schachter, Todd M Myers
Galantamine hydrobromide and (-)huperzine A, centrally active reversible acetylcholinesterase inhibitors, are potentially superior to the current standard, pyridostigmine bromide, as a pretreatment for organophosphorus chemical warfare nerve agent intoxication. Galantamine, huperzine, and pyridostigmine were compared for time course of acetylcholinesterase inhibition in 12 cynomolgus macaques. Although both galantamine and huperzine shared a similar time course profile for acetylcholinesterase inhibition, huperzine was 88 times more potent than galantamine...
November 30, 2016: Neurochemical Research
https://www.readbyqxmd.com/read/27899389/high-dose-rivastigmine-in-the-symptom-management-of-lewy-body-dementia
#10
Joseph Marwan Nour, Leonidas Chouliaras, Lilian Hickey
A man presented in late 2004 at the age of 65 with a decline in memory. He was diagnosed with Lewy body dementia and started on 3 mg rivastigmine a day, which made a marked clinical improvement. He lived with the illness for 10 years, over which time the dose of acetylcholinesterase inhibitors (ChEI) he took rose to two 9.5 mg rivastigmine patches and 7.5 mg donepezil, significantly above British National Formulary (BNF) limits. He demonstrated clear clinical response to ChEI and showed improvements in alertness and functioning...
November 29, 2016: BMJ Case Reports
https://www.readbyqxmd.com/read/27899289/protective-propensity-of-bacoside-a-and-bromelain-on-renal-cholinesterases-%C3%AE-aminobutyric-acid-and-serotonin-level-of-mus-musculus-intoxicated-with-dichlorvos
#11
Sonam Agarwal, Bharti Chaudhary, Renu Bist
Current study established a protective action of bacoside A and bromelain against the toxic effects of dichlorvos in kidneys of mice. Experimental design included five groups. The first group was control. Mice of groups II, III and IV were administered doses of dichlorvos, bromelain and bacoside A respectively. In group V, mice were treated with both the antioxidants (bacoside A and bromelain) and dichlorvos. After 21 days of exposure of different doses, levels of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), γ-aminobutyric acid (GABA) and serotonin were measured in renal tissues...
November 26, 2016: Chemico-biological Interactions
https://www.readbyqxmd.com/read/27898990/european-paediatric-surgeons-association-survey-on-the-management-of-hirschsprung-disease
#12
Augusto Zani, Simon Eaton, Francesco Morini, Prem Puri, Risto Rintala, Ernest van Heurn, Marija Lukac, Pietro Bagolan, Joachim F Kuebler, Florian Friedmacher, Rene Wijnen, Juan A Tovar, Michael E Hoellwarth, Agostino Pierro
: Aim This study aims to define patterns of Hirschsprung disease (HD) management. Methods An online questionnaire was sent to all European Paediatric Surgeons' Association (EUPSA) members. Results A total of 294 members (61 countries) answered (response rate: 61%). DIAGNOSIS: All respondents perform rectal biopsies (61% rectal suction [RSBs], 39% open full-thickness), 96% contrast enema, and 31% anorectal manometry. At RSB, 17% take the most distal biopsy 1 cm above the dentate line, 34% take 2 cm, 30% take 3 cm, and 19% take > 3 cm...
November 29, 2016: European Journal of Pediatric Surgery
https://www.readbyqxmd.com/read/27897265/mutations-in-acetylcholinesterase2-ace2-increase-the-insensitivity-of-acetylcholinesterase-to-fosthiazate-in-the-root-knot-nematode-meloidogyne-incognita
#13
Wen-Kun Huang, Qin-Song Wu, Huan Peng, Ling-An Kong, Shi-Ming Liu, Hua-Qun Yin, Ru-Qiang Cui, Li-Ping Zhan, Jiang-Kuan Cui, De-Liang Peng
The root-knot nematode Meloidogyne incognita causes severe damage to continuously cropping vegetables. The control of this nematode relies heavily on organophosphate nematicides in China. Here, we described resistance to the organophosphate nematicide fosthiazate in a greenhouse-collected resistant population (RP) and a laboratory susceptible population (SP) of M. incognita. Fosthiazate was 2.74-fold less toxic to nematodes from RP than that from SP. Quantitative real-time PCR revealed that the acetylcholinesterase2 (ace2) transcription level in the RP was significantly higher than that in the SP...
November 29, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27897077/understanding-the-conformational-flexibility-and-electrostatic-properties-of-curcumin-in-the-active-site-of-rhache-via-molecular-docking-molecular-dynamics-and-charge-density-analysis
#14
Saravanan Kandasamy, Kalaiarasi Chinnasamy, Kumaradhas Poomani
Acetylcholinesterase (AChE) is an important enzyme responsible for Alzheimer disease (AD), as per report, keto-enol form of curcumin inhibits this enzyme. The present study aims to understand the binding mechanism of keto-enol curcumin with the recombinant human Acetylcholinesterase (rhAChE) from its conformational flexibility, intermolecular interactions, charge density distribution and the electrostatic properties at the active site of rhAChE. To accomplish this, a molecular docking analysis of curcumin with the rhAChE was performed, which gives the structure and conformation of curcumin in the active site of rhAChE...
November 29, 2016: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/27895161/the-e-loop-of-the-transmitter-binding-site-is-a-key-determinant-of-the-modulatory-effects-of-physostigmine-on-neuronal-nicotinic-%C3%AE-4%C3%AE-2-receptors
#15
Xiaochun Jin, Megan M McCollum, Allison L Germann, Gustav Akk, Joseph H Steinbach
Physostigmine is a well-known inhibitor of acetylcholinesterase, which can also activate, potentiate and inhibit acetylcholine receptors, including neuronal nicotinic receptors comprising α4 and β2 subunits. We have found that the two stoichiometric forms of this receptor differ in the effects of physostigmine. The form containing 3 copies of α4 and 2 of β2 was potentiated at low concentrations of ACh and physostigmine, while the form containing 2 copies of α4 and 3 of β2 was inhibited. Chimeric constructs of subunits indicated that the presence of inhibition or potentiation depended on the source of the extracellular ligand-binding domain of the subunit...
November 28, 2016: Molecular Pharmacology
https://www.readbyqxmd.com/read/27893738/fenugreek-seed-powder-nullified-aluminium-chloride-induced-memory-loss-biochemical-changes-a%C3%AE-burden-and-apoptosis-via-regulating-akt-gsk3%C3%AE-signaling-pathway
#16
Asokan Prema, Arokiasamy Justin Thenmozhi, Thamilarasan Manivasagam, Musthafa Mohamed Essa, Mohammed D Akbar, Mohammed Akbar
Alzheimer's disease (AD) is the most common form of dementia that mainly affects the cognitive functions of the aged populations. Trigonella foenum-graecum (L.) (fenugreek), a traditionally well utilized medicinal plant ubiquitously used as one of the main food additive worldwide, is known to have numerous beneficial health effects. Fenugreek seed extract could be able to inhibit the activity of acetylcholinesterase (AChE), a key enzyme involved in the pathogenesis of AD, and further shown to have anti-parkinsonic effect...
2016: PloS One
https://www.readbyqxmd.com/read/27890370/acetylcholinesterase-butyrylcholinesterase-and-paraoxonase-1-activities-in-rats-treated-with-cannabis-tramadol-or-both
#17
Omar M E Abdel-Salam, Eman R Youness, Yasser A Khadrawy, Amany A Sleem
OBJECTIVE: To investigate the effect of Cannabis sativa resin and/or tramadol, two commonly drugs of abuse on acetylcholinesterase and butyrylcholinesterase activities as a possible cholinergic biomarkers of neurotoxicity induced by these agents. METHODS: Rats were treated with cannabis resin (5, 10 or 20 mg/kg) (equivalent to the active constituent Δ(9)-tetrahydrocannabinol), tramadol (5, 10 and 20 mg/kg) or tramadol (10 mg/kg) combined with cannabis resin (5, 10 and 20 mg/kg) subcutaneously daily for 6 weeks...
November 2016: Asian Pacific Journal of Tropical Medicine
https://www.readbyqxmd.com/read/27890007/a-current-perspective-on-the-inhibition-of-cholinesterase-by-natural-and-synthetic-inhibitors
#18
Anzer A Shah, Showkat A Ganie, Mohammad A Kamal, Tanveer Ali Dar
Majority of the observed cognitive and behavioral changes in Alzheimer's diseaseare postulated to be due to the deficiencies in cholinergic pathways of the brain. Enhancement of cholinergic transmission may thus stimulate the cholinergic receptors or prolong the availability of acetylcholine in synaptic cleft and hence improve the Alzheimer's disease associated symptoms. Of these two, the inhibition of cholinesterases (Acetylcholinesterase and Butyrylcholinesterase) by cholinesterase inhibitors is suggested to be a promising strategy...
November 23, 2016: Current Drug Metabolism
https://www.readbyqxmd.com/read/27887948/s-allyl-cysteine-ameliorates-cognitive-deficits-in-streptozotocin-diabetic-rats-via-suppression-of-oxidative-stress-inflammation-and-acetylcholinesterase
#19
Tourandokht Baluchnejadmojarad, Zahra Kiasalari, Siamak Afshin-Majd, Zahra Ghasemi, Mehrdad Roghani
Diabetes mellitus (DM) is associated with learning, memory, and cognitive deficits. S-allyl cysteine (SAC) is the main organosulfur bioactive molecule in aged garlic extract with anti-diabetic, antioxidant, anti-inflammatory and nootropic property. This research was conducted to evaluate the efficacy of SAC on alleviation of learning and memory deficits in streptozotocin (STZ)-diabetic rats and to explore involvement of toll-like receptor 4 (TLR4), nuclear factor (erythroid-derived 2)-like 2 (Nrf2), nuclear factor-kappa B (NF-κB), and heme oxygenase 1 (HO-1) signaling cascade...
November 22, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27886567/evaluation-of-8-hydroxy-2-deoxyguanosine-and-nfkb-activation-oxidative-stress-response-acetylcholinesterase-activity-and-histopathological-changes-in-rainbow-trout-brain-exposed-to-linuron
#20
Ahmet Topal, Gonca Alak, Serdar Altun, Hüseyin Serkan Erol, Muhammed Atamanalp
Linuron is a widely used herbicide to control grasses and annual broad leaf weeds. It is known that linuron has toxic effects on different organisms. However, the toxic effects of linuron on aquatic organisms, especially fish, is completely unknown. Thus, we aimed to investigate changes in 8-hydroxy-2-deoxyguanosine (8-OHdG) and nuclear factor kappa B (NFkB) activity, histopathological changes, antioxidant responses and acetylcholinesterase (AChE) activity in rainbow trout brain after exposure to linuron. Fish were exposed to 30μg/L, 120μg/L and 240μg/L concentrations of linuron for twenty-one days...
November 13, 2016: Environmental Toxicology and Pharmacology
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