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acetylcholinesterase

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https://www.readbyqxmd.com/read/28427893/study-of-acetylcholinesterase-activity-and-apoptosis-in-sh-sy5y-cells-and-mice-exposed-to-ethanol
#1
Wenjun Sun, Liangjing Chen, Wei Zheng, Xiaoan Wei, Wenqi Wu, Ellen G Duysen, Wei Jiang
Ethanol is one of the most commonly abused psychotropic substances with deleterious effects on the central nervous system. Ethanol exposure during development results in the loss of neurons in brain regions and when exposed to ethanol cultured cells undergo apoptosis. To date no information is available on whether abnormally high AChE activity is characteristic of apoptosis in animals exposed to ethanol. The aims of the present study were to determine whether induction of AChE activity is associated with ethanol-induced apoptosis and to explore the mechanism of enhanced AChE activity induced by ethanol...
April 17, 2017: Toxicology
https://www.readbyqxmd.com/read/28427041/the-efficacy-of-donepezil-administration-on-acetylcholinesterase-activity-and-altered-redox-homeostasis-in-alzheimer-s-disease
#2
Pinar Atukeren, Mahir Cengiz, Hakan Yavuzer, Remise Gelisgen, Esma Altunoglu, Sena Oner, Fusun Erdenen, Damla Yuceakın, Himmet Derici, Ufuk Cakatay, Hafize Uzun
Alzheimer's disease (AD) is a serious multifactorial disorder with progressive neurodegenerative outcomes related with impaired redox homeostasis. Inhibition of the enzyme acetylcholinesterase (AChE), as one of the major therapeutic strategies, is considered to be offering only symptomatic relief and moderate disease modifying effect. We intended to investigate the effects of acetylcholinesterase inhibition via donepezil on protein carbonyl (PCO), advanced protein oxidation products (AOPP) and ischemia modified albumin (IMA) as protein oxidation markers and ferric reducing antioxidant power (FRAP), prooxidant-antioxidant balance (PAB), total thiol (T-SH), protein thiol (P-SH) as antioxidant status markers and also kynurenine (KYN), N-formyl kynurenine (N-FKYN) and protein bound dityrosine (DT) levels all in one demonstrating the redox homeostasis in Alzheimer patients also correlated with AChE activity...
April 17, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28419991/effect-of-melatonin-and-resveratrol-against-memory-impairment-and-hippocampal-damage-in-a-rat-model-of-vascular-dementia
#3
Dongfang Shen, Xiaoyan Tian, Wenxu Sang, Rongrong Song
OBJECTIVES: This study was intended to investigate whether treatment with resveratrol and melatonin alone or in combination can exert neurorestorative effects in a rat model of vascular dementia. METHODS: Briefly, male Wistar rats were subjected to permanent bilateral common carotid artery occlusion (BCCAO) by surgery. After 4 weeks, the cognitive deficits were assessed using the Morris water maze and novel object recognition tests. The biochemical parameters of oxidative stress and inflammation were also assessed...
April 19, 2017: Neuroimmunomodulation
https://www.readbyqxmd.com/read/28419192/efficacy-and-safety-of-a-novel-acetylcholinesterase-inhibitor-octohydroaminoacridine-in-mild-to-moderate-alzheimer-s-disease-a-phase-ii-multicenter-randomised-controlled-trial
#4
Shifu Xiao, Tao Wang, Xiuqiang Ma, Yingyi Qin, Xia Li, Zhongxin Zhao, Xueyuan Liu, Xiaoping Wang, Hengge Xie, Qinpu Jiang, Li Sun, Benyan Luo, Lan Shang, Weixian Chen, Yan Bai, Muni Tang, Maolin He, Lan Wu, Qilin Ma, Deren Hou, Jia He
Background: inhibition of acetylcholinesterase (AChE) has been a effective treatment for Alzheimer's disease (AD). Octohydroaminoacridine, a new AChE inhibitor, is a potential treatment for AD. Method: we conducted a multicenter, randomised, double blind, placebo-controlled, parallel-group Phase II clinical trial to investigate the effects of octohydroaminoacridine in patients with mild-to-moderate AD. Patients were randomised to receive placebo thrice daily, octohydroaminoacridine 1 mg/thrice daily (TID) (low-dose group), 2 mg/TID (middle-dose group) or 4 mg/TID (high-dose group)...
April 17, 2017: Age and Ageing
https://www.readbyqxmd.com/read/28418831/the-evaluation-of-benefit-of-newly-prepared-reversible-inhibitors-of-acetylcholinesterase-and-commonly-used-pyridostigmine-as-pharmacological-pretreatment-of-soman-poisoned-mice
#5
Jiří Kassa, Jan Korábečný, Eugenie Nepovimová
AIM: The ability of four newly prepared reversible inhibitors of acetylcholinesterase (6-chlorotacrine, 7-phenoxytacrine, compounds 1 and 2) and currently used carbamate pyridostigmine to increase the resistance of mice against soman and the efficacy of antidotal treatment of soman-poisoned mice was evaluated. METHODS: The evaluation of the effect of pharmacological pretreatment is based on the identification of changes of soman-induced toxicity that was evaluated by the assessment of its LD50 value and its 95% confidence limit using probitlogarithmical analysis of death occurring within 24 h after administration of soman...
April 18, 2017: Acta Medica (Hradec Králové)
https://www.readbyqxmd.com/read/28417668/exploring-molecular-structural-requirement-for-ache-inhibition-through-multi-chemometric-and-dynamics-simulation-analyses
#6
Tabassum Hossain, Achintya Saha, Arup Mukherjee
The acetylcholinesterase enzyme (AChE) plays an important role in central and peripheral nervous systems. Acetylcholine (ACh) acts through the regulation of AChE activity, which can play a key role in accelerating senile amyloid β-peptide (Aβ) plaque deposition. Therefore, inhibition of the AChE enzyme can be used as a key principle to prevent ACh depletion. The present study has been emphasized to explore both ligand- and structure-based 3D QSAR, HQSAR, pharmacophore, molecular docking and simulation studies on a set of structurally diverse inhibitors to optimize prime structural features responsible for selective binding to AChE, and vis-à-vis inhibiting enzyme activity...
April 18, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28417590/calcitonin-gene-related-peptide-cgrp-a-novel-target-for-alzheimer-s-disease
#7
REVIEW
Yogendra Singh, Gaurav Gupta, Birendra Shrivastava, Rajiv Dahiya, Juhi Tiwari, Madhu Ashwathanarayana, Rakesh Kumar Sharma, Mohit Agrawal, Anurag Mishra, Kamal Dua
Alzheimer's disease (AD) is leading cause of death among older characterized by neurofibrillary tangles, oxidative stress, progressive neuronal deficits, and increased levels of amyloid-β (Aβ) peptides. Cholinergic treatment could be the best suitable physiological therapy for AD. Calcitonin gene-related peptide (CGRP) is a thirty-seven-amino acid regulatory neuropeptide resulting from different merging of the CGRP gene, which also includes adrenomedullin, amylin, calcitonin, intermedin, and calcitonin receptor-stimulating peptide...
April 17, 2017: CNS Neuroscience & Therapeutics
https://www.readbyqxmd.com/read/28416102/synthesis-biochemical-evaluation-and-molecular-modeling-studies-of-aryl-and-arylalkyl-di-n-butyl-phosphates-effective-butyrylcholinesterase-inhibitors
#8
Kensaku Nakayama, Jason P Schwans, Eric J Sorin, Trina Tran, Jeannette Gonzalez, Elvis Arteaga, Sean McCoy, Walter Alvarado
A series of dialkyl aryl phosphates and dialkyl arylalkyl phosphates were synthesized. Their inhibitory activities were evaluated against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The di-n-butyl phosphate series consistently displayed selective inhibition of BChE over AChE. The most potent inhibitors of butyrylcholinesterase were di-n-butyl-3,5-dimethylphenyl phosphate (4b) [KI=1.0±0.4μM] and di-n-butyl 2-naphthyl phosphate (5b) [KI=1.9±0.4μM]. Molecular modeling was used to uncover three subsites within the active site gorge that accommodate the three substituents attached to the phosphate group...
April 5, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28415036/toxic-effects-of-glyphosate-on-diploid-and-triploid-fin-cell-lines-from-misgurnus-anguillicaudatus
#9
Yanjie Qin, Xia Li, Yang Xiang, Di Wu, Liwen Bai, Zhuangzhuang Li, Yan Liang
We examined the toxic effects of glyphosate on diploid (DIMF) and triploid (TRMF) fin cell lines from the Oriental Weather Loach Misgurnus anguillicaudatus. The LC50 values of glyphosate estimated by methylthiazolyldiphenyl-tetrazolium bromide (MTT) assay were 315.34 and 371.77 mg/L for DIMF and TRMF, respectively. Superoxide dismutase (SOD) and glutathione-S-transferase (GST) activities in DIMF and TRMF cells gradually increased and then decreased with increasing glyphosate concentrations, reaching a maximum at 240 mg/L glyphosate...
March 25, 2017: Chemosphere
https://www.readbyqxmd.com/read/28413513/huperzine-a-inhibits-immediate-addictive-behavior-but-not-behavioral-sensitization-following-repeated-morphine-administration-in-rats
#10
Jinling Sun, Lin Tian, Ruisi Cui, Xinwang Li
Acetylcholinesterase inhibitors are regarded as promising therapeutic agents to treat addiction. The current study aimed to examine the effects of huperzine A, a cholinesterase inhibitor, on behavioral sensitization induced by repeated morphine administration and relapse induced by contextual conditioning. The present study also assessed whether the state-dependency hypothesis may explain the results. Adult rats were divided into four groups (n=8) and intraperitoneally injected with 0.2, 0.3 or 0.4 mg/kg huperzine A or saline (1 ml/kg, control), for 5 days...
April 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28413414/comedication-and-treatment-length-in-users-of-acetylcholinesterase-inhibitors
#11
Anne Sverdrup Efjestad, Hege Ihle-Hansen, Vidar Hjellvik, Hege Salvesen Blix
BACKGROUND/AIMS: Reduced clinical effect on cognitive decline in dementia by acetylcholinesterase inhibitors (AChEIs) may be due to concurrent use of drugs with anticholinergic properties. The aim was to analyze the incidence of AChEI use and comedication with drugs with anticholinergic properties and other potential unfavorable effects. METHODS: A prospective study applying drug use data from the Norwegian Prescription Database. Anticholinergic Drug Scale (ADS) scores were used as a measure of overall anticholinergic burden...
January 2017: Dementia and Geriatric Cognitive Disorders Extra
https://www.readbyqxmd.com/read/28412626/quantification-of-heat-shock-protein-70-and-acetylcholinesterase-over-a-time-course-suggests-environmental-adaptation-in-a-foundational-molluscan-species
#12
Andrew Ravaschiere, Caroline Cutler, Kristi Edleson, Zachery Halem, Henry Magun, Fred Meckler, Rachel Cox
Waterways in urban areas often act as repositories for sewage, industrial waste, and environmental contaminants. In response, inhabitants of these watersheds undergo physiological adaptations specific to their respective environments. Effects of these stressors can be assayed by quantification of various well-documented biomarkers in sentinel species such as the Atlantic Ribbed mussel, Geukensia demissa, a native to the Bronx River Estuary, Bronx, NY, USA. Heat shock protein 70 (Hsp70) is a universally expressed biomarker for an array of environmental stressors including toxins and low dissolved oxygen...
April 13, 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/28411556/hydrogen-peroxide-modifies-both-activity-and-isoforms-of-acetylcholinesterase-in-human-neuroblastoma-sh-sy5y-cells
#13
Alba Garcimartín, M Elvira López-Oliva, M Pilar González, Francisco J Sánchez-Muniz, Juana Benedí
The involvement of cholinergic system and the reactive oxygen species (ROS) in the pathogenesis of some degenerative diseases has been widely reported; however, the specific impact of hydrogen peroxide (H2O2) on the acetylcholinesterase (AChE) activity as well as AChE isoform levels has not been clearly established. Hence, the purpose of present study is to clarify whether H2O2 alters these parameters. Human neuroblastoma SH-SY5Y cells were treated with H2O2 (1-1000µM) for 24h and AChE activity and AChE and cytochrome c levels were evaluated...
April 4, 2017: Redox Biology
https://www.readbyqxmd.com/read/28409416/tributyltin-bioaccumulation-and-toxic-effects-in-freshwater-gastropods-pomacea-canaliculata-after-a-chronic-exposure-field-and-laboratory-studies
#14
María L Martínez, María N Piol, Norma Sbarbati Nudelman, Noemí R Verrengia Guerrero
Freshwater samples and gastropod mollusks (Pomacea canaliculata) were collected at 5 sampling stations located along the lower Río de la Plata basin, Argentina, to assess the extent of tributyltin (TBT) contamination. Determined data revealed the presence of TBT and some of its breakdown products (dibutyltin: DBT, and monobutyltin: MBT) in all freshwater samples and also in soft tissues of P. canaliculata gastropods. Chronic bioassays (6 months) were performed using female gastropods that had been reared under laboratory conditions and exposed to a similar TBT concentration than the value determined in freshwater samples (1 µg L(-1))...
April 13, 2017: Ecotoxicology
https://www.readbyqxmd.com/read/28408800/rutin-protects-against-neuronal-damage-in-vitro-and-ameliorates-doxorubicin-induced-memory-deficits-in-vivo-in-wistar-rats
#15
Grandhi Venkata Ramalingayya, Sri Pragnya Cheruku, Pawan G Nayak, Anoop Kishore, Rekha Shenoy, Chamallamudi Mallikarjuna Rao, Nandakumar Krishnadas
Doxorubicin (DOX) is the most widely used broad-spectrum anticancer agent, either alone or in combination, for most cancers including breast cancer. Long-term use of chemotherapeutic agents to treat breast cancer patients results in cognitive complications with a negative impact on survivors' quality of life. The study objective was to evaluate rutin (RUT) for its neuroprotective effect against DOX in human neuroblastoma (IMR32) cells in vitro and study its potential to ameliorate DOX-induced cognitive dysfunction in Wistar rats...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28407384/point-mutations-in-acetylcholinesterase-1-associated-with-chlorpyrifos-resistance-in-the-brown-planthopper-nilaparvata-lugens-st%C3%A3-l
#16
Y Zhang, B Yang, J Li, M Liu, Z Liu
Insecticide resistance frequently results from target-site insensitivity, such as point mutations in acetylcholinesterases (AChEs) for resistance to organophosphates and carbamates. From a field-originated population of Nilaparvata lugens, a major rice pest, a resistant population (R9) was obtained by nine-generation continuous selection with chlorpyrifos. From the same field population, a relatively susceptible population (S9) was also constructed through rearing without any insecticides. Compared to the susceptible strain, Sus [medium lethal dose (LC50 ) = 0...
April 13, 2017: Insect Molecular Biology
https://www.readbyqxmd.com/read/28406297/binding-analysis-of-some-classical-acetylcholinesterase-inhibitors-insights-for-a-rational-design-using-free-energy-perturbation-method-calculations-with-qm-mm-md-simulations
#17
Érica C M Nascimento, Mónica Oliva, Katarzyna Świderek, João B L Martins, Juan Andrés
In the present study, the binding free energy of some classical inhibitors (DMT, DNP, GNT, HUP, THA) with acetylcholinesterase (AChE) is calculated by means of the free energy perturbation (FEP) method based on hybrid quantum mechanics and molecular mechanics (QM/MM) potentials. The results highlight the key role of the van der Waals interaction for the inhibition process, since the contribution of this term to the binding free energy is almost as decisive as the electrostatic one. The analysis of the geometrical parameters and the interaction energy per residue along the QM/MM molecular dynamics (MD) simulations highlights the most relevant interactions in the different AChE-ligand systems, showing that the charged residues with a more prominent contribution to the interaction energy are Asp72 and Glu199, although the relative importance depends on the molecular size of the ligand...
April 13, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28404526/stereospecific-cholinesterase-inhibition-by-o-s-diethylphenylphosphonothioate
#18
Ahmed Mohammed, Jennifer Sneathen, Sara Glazier Frojen, Louis Kuo, Cynthia M Dupureur
The inhibition kinetics and stereospecificity of the chiral nerve agent derivative O,S-diethylphenylphosphonothioate (DEPP) were examined for two forms of acetylcholinesterase (human and eel) and equine butyrylcholinesterase. Both S- and R-DEPP are poor inhibitors of eel AChE (IC50 150μM), consistent with a large, nondiscriminatory binding interaction in the active site of this enzyme. However, S-DEPP is active against human and equine AChE with low μM IC50s. DEPP stereospecificities (S/R) toward these enzymes are moderate (20) relative to other cholinesterase-organophosphate (OP) systems...
March 30, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28403780/synthesis-of-novel-benzothiazole-piperazine-derivatives-and-their-biological-evaluation-as-acetylcholinesterase-inhibitors-and-cytotoxic-agents
#19
Enise Ece Gurdal, Bengisu Turgutalp, Hayrettin Ozan Gulcan, Tugba Erçetin, Mustafa Fethi Sahin, Irem Durmaz, Rengul Cetin Atalay, Quoc Dat Nguyen, Wolfgang Sippl, Mine Yarim
A new series of benzothiazole-piperazine derivatives were synthesized and a complete chemical characterization of the novel compounds was provided. In vitro cytotoxic activities were screened against colorectal (HCT-116), breast (MCF-7) and hepatocellular (Huh7) cancer cell lines by Sulforhodamine B assay. All compounds showed cytotoxic activity against hepatocellular (Huh7) and breast (MCF-7) cancer cell lines. Dihalo substituted benzylpiperazine derivatives (2a, 2e) had the highest cytotoxic activities in all tested cell lines...
April 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28402435/comparative-effect-of-three-neurotoxic-insecticides-with-different-modes-of-action-on-adult-males-and-females-of-three-tortricid-moth-pests
#20
Miguel A Navarro-Roldán, Jesús Avilla, Dolors Bosch, Joan Valls, César Gemeno
Insecticides are the dominant pest management method in fruit and vegetable crops worldwide owing to their quick effect, low cost, and relatively easy application, but they bear negative effects on human health and the environment. Insecticide mode of action (MoA), target species, and sex are variables that could affect insecticide-induced mortality. We recorded the mortality caused by three neurotoxic insecticides with different modes of action (chlorpyrifos [organophosphate, acetylcholinesterase inhibitor], λ-cyhalothrin [pyrethroid, sodium channel modulator], and thiacloprid [neonicotinoid, nicotinic acetylcholinesterase receptor agonist]) applied topically to adult males and females of three economically important tortricid species [Cydia pomonella (L...
April 11, 2017: Journal of Economic Entomology
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