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Cholinesterase

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https://www.readbyqxmd.com/read/28428009/effect-of-methylparaben-in-artemia-franciscana
#1
Amparo Comeche, María Martín-Villamil, Yolanda Pico, Inma Varó
In this study, the toxicity of methylparaben (MeP) an emerging contaminant, was analyzed in the sexual species Artemia franciscana, due to its presence in coastal areas and marine saltworks in the Mediterranean region. The acute toxicity (24h-LC50) of MeP in nauplii was tested and its chronic effect (9days) evaluated by measuring survival and growth under two sublethal concentrations (0.0085 and 0.017mg/L). Also, the effect on several key enzymes involved in: antioxidant defences (catalase (CAT) and gluthathion-S-transferase (GST)), neural activity (cholinesterase (ChE)) and xenobiotic biotransformation (carboxylesterase (CbE), was assessed after 48h under sublethal exposure...
April 17, 2017: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
https://www.readbyqxmd.com/read/28418778/parkinsonism-signs-and-symptoms-in-agricultural-pesticide-handlers-in-washington-state
#2
Susan Searles Nielsen, Shu-Ching Hu, Harvey Checkoway, Maria Negrete, Pablo Palmández, Theresa Bordianu, Brad A Racette, Christopher D Simpson
OBJECTIVES: Examine associations between pesticide exposure and signs or symptoms of parkinsonism. METHODS: Prior to the 2014 pesticide spray season we examined 38 active pesticide handlers age 35-65 (median 43.5) who participated in the State of Washington's cholinesterase monitoring program in the Yakima Valley, where cholinesterase-inhibiting insecticides are applied in fruit orchards. A movement disorders specialist assessed the workers using the Unified Parkinson's Disease Rating Scale (UPDRS) motor subscore 3 (UPDRS3)...
April 18, 2017: Journal of Agromedicine
https://www.readbyqxmd.com/read/28416036/exploring-dementia-management-attitudes-in-primary-care-a-key-informant-survey-to-primary-care-physicians-in-25-european-countries
#3
Ferdinando Petrazzuoli, Shlomo Vinker, Tuomas H Koskela, Thomas Frese, Nicola Buono, Jean Karl Soler, Jette Ahrensberg, Radost Asenova, Quintí Foguet Boreu, Gülsen Ceyhun Peker, Claire Collins, Miro Hanževački, Kathryn Hoffmann, Claudia Iftode, Donata Kurpas, Jean Yves Le Reste, Bjørn Lichtwarck, Davorina Petek, Daniel Pinto, Diego Schrans, Sven Streit, Eugene Yee Hing Tang, Athina Tatsioni, Péter Torzsa, Pemra C Unalan, Harm van Marwijk, Hans Thulesius
BACKGROUND: Strategies for the involvement of primary care in the management of patients with presumed or diagnosed dementia are heterogeneous across Europe. We wanted to explore attitudes of primary care physicians (PCPs) when managing dementia: (i) the most popular cognitive tests, (ii) who had the right to initiate or continue cholinesterase inhibitor or memantine treatment, and (iii) the relationship between the permissiveness of these rules/guidelines and PCP's approach in the dementia investigations and assessment...
April 18, 2017: International Psychogeriatrics
https://www.readbyqxmd.com/read/28413513/huperzine-a-inhibits-immediate-addictive-behavior-but-not-behavioral-sensitization-following-repeated-morphine-administration-in-rats
#4
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/28406525/an-improved-radiosynthesis-of-o-2-18-f-fluoroethyl-o-p-nitrophenyl-methylphosphonate-a-first-in-class-cholinesterase-pet-tracer
#5
Kiel D Neumann, Charles M Thompson, Joseph E Blecha, John M Gerdes, Henry F VanBrocklin
O-(2-Fluoroethyl)-O-(p-nitrophenyl) methylphosphonate 1 is an organophosphate (OP) cholinesterase inhibitor, which creates a phosphonyl-serine covalent adduct at the enzyme active site blocking cholinesterase activity in vivo. The corresponding radiolabeled O-(2-[(18) F]fluoroethyl)-O-(p-nitrophenyl) methylphosphonate, [(18) F]1, has been previously prepared and found to be an excellent positron emission tomography (PET) imaging tracer for assessment of cholinesterases in live brain, peripheral tissues and blood...
April 12, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28404526/stereospecific-cholinesterase-inhibition-by-o-s-diethylphenylphosphonothioate
#6
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/28400237/cytochrome-p450-binding-studies-of-novel-tacrine-derivatives-predicting-the-risk-of-hepatotoxicity
#7
Alanna McEneny-King, Wesseem Osman, Andrea N Edginton, Praveen P N Rao
The 1,2,3,4-tetrahydroacridine derivative tacrine was the first drug approved to treat Alzheimer's disease (AD). It is known to act as a potent cholinesterase inhibitor. However, tacrine was removed from the market due to its hepatotoxicity concerns as it undergoes metabolism to toxic quinonemethide species through the cytochrome P450 enzyme CYP1A2. Despite these challenges, tacrine serves as a useful template in the development of novel multi-targeting anti-AD agents. In this regard, we sought to evaluate the risk of hepatotoxicity in a series of C9 substituted tacrine derivatives that exhibit cholinesterase inhibition properties...
April 3, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28388521/design-synthesis-and-biological-activity-of-novel-donepezil-derivatives-bearing-n-benzyl-pyridinium-moiety-as-potent-and-dual-binding-site-acetylcholinesterase-inhibitors
#8
Jin-Shuai Lan, Tong Zhang, Yun Liu, Jing Yang, Sai-Sai Xie, Jing Liu, Ze-Yang Miao, Yue Ding
A series of new donepezil derivatives were designed synthesized and evaluated as multifunctional cholinesterase inhibitors against Alzheimer's disease (AD). In vitro studies showed that most of them exhibited significant potency to inhibit acetylcholinesterase and self-induced β-amyloid (Aβ) aggregation, and moderate antioxidant activity. Especially, compound 5b presented the greatest ability to inhibit cholinesterase (IC50, 1.9 nM for eeAChE and 0.8 nM for hAChE), good inhibition of Aβ aggregation (53...
March 23, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28387023/simultaneous-usage-of-dementia-medications-and-anticholinergics-among-asians-and-pacific-islanders
#9
Brian R Schultz, Junji Takeshita, Deborah Goebert, Steven Takeshita, Brett Y Lu, Alexandre Guilloux, Joy Higa
BACKGROUND: The simultaneous use of dementia medications and anticholinergic medications occurs frequently. Cholinesterase inhibitors and anticholinergic medications likely counteract one another, potentially exposing patients to medications with decreased benefit, more adverse effects, and higher cost of care. We identified the rate of concurrent prescriptions of cholinesterase inhibitors/memantine with anticholinergics in an urban hospital setting with a large Asian and Pacific Islander population...
April 7, 2017: Psychogeriatrics: the Official Journal of the Japanese Psychogeriatric Society
https://www.readbyqxmd.com/read/28382676/natural-genomic-amplification-of-cholinesterase-genes-in-animals
#10
REVIEW
Arnaud Chatonnet, Nicolas Lenfant, Pascale Marchot, Murray E Selkirk
Tight control of the concentration of acetylcholine at cholinergic synapses requires precise regulation of the number and state of the acetylcholine receptors, and of the synthesis and degradation of the neurotransmitter. In particular, the cholinesterase activity has to be controlled exquisitely. In the genome of the first experimental models used (man, mouse, zebrafish and drosophila), there are only one or two genes coding for cholinesterases, whereas there are more genes for their closest relatives the carboxylesterases...
April 5, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28375126/tyrosinase-inhibition-anti-acetylcholinesterase-and-antimicrobial-activities-of-the-phytochemicals-from-gynotroches-axillaris-blume
#11
Salam Ahmed Abed, Hasnah Mohd Sirat, Muhammad Taher
The leaves of Gynotroches axillaris were chemically and biologically studied. Sequential extraction of the leaves using petroleum ether, chloroform, and methanol afforded three extracts. Purification of pet. ether extract yielded, squalene and β-amyrin palmitate as the major compounds, together with palmitic acid and myristic acid as the minor components. The methanol extract yielded two flavonoids, quercitrin and epicatechin. The isolated compounds were characterized by MS, IR and NMR (1D and 2D). Anti-acetyl cholinesterase screening using TLC bio-autography assay showed that palmitic acid and myristic acid were the strongest inhibition with detection limit 1...
November 2016: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28373142/aflatoxins-produced-by-aspergillus-parasiticus-present-in-the-diet-of-quails-increase-the-activities-of-cholinesterase-and-adenosine-deaminase
#12
Aleksandro Schafer da Silva, Janio M Santurio, Lenilson F Roza, Nathieli B Bottari, Gabriela M Galli, Vera M Morsch, Maria Rosa C Schetinger, Matheus D Baldissera, Lenita M Stefani, Willian M Radavelli, Thainã Tomasi, Marcel M Boiago
The aim of this study was to evaluate the effects of aflatoxins on cholinesterases (acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), and adenosine deaminase (ADA) activities in quails. For this, twenty male quails were randomly distributed into two groups (n = 10 each): the group A was composed by quails that received feed without aflatoxin (the control group); while the group B was composed by quails that received feed contaminated with 200 ppm/kg of feed of aflatoxin. On day 20, the animals were euthanized to measure the activities of AChE (total blood and brain), BChE (serum) and ADA (serum, liver, and brain), as well as for histopathological analyses (liver and intestine)...
March 31, 2017: Microbial Pathogenesis
https://www.readbyqxmd.com/read/28367983/cholinesterase-like-organocatalysis-by-imidazole-and-imidazole-bearing-molecules
#13
Paola Nieri, Sara Carpi, Stefano Fogli, Beatrice Polini, Maria Cristina Breschi, Adriano Podestà
Organocatalysis, which is mostly explored for its new potential industrial applications, also represents a chemical event involved in endogenous processes. In the present study, we provide the first evidence that imidazole and imidazole derivatives have cholinesterase-like properties since they can accelerate the hydrolysis of acetylthiocholine and propionylthiocholine in a concentration-dependent manner. The natural imidazole-containing molecules as L-histidine and histamine show a catalytic activity, comparable to that of imidazole itself, whereas synthetic molecules, as cimetidine and clonidine, were less active...
April 3, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28367435/effect-of-underlying-renal-disease-on-nutritional-and-metabolic-profile-of-older-adults-with-reduced-renal-function
#14
Silvia Lai, Maria Ida Amabile, Silvia Altieri, Daniela Mastroluca, Carlo Lai, Paola Aceto, Massimiliano Crudo, Anna Rita D'Angelo, Maurizio Muscaritoli, Alessio Molfino
BACKGROUND: Chronic kidney disease is a common condition in the general population, particularly among older adults. Renal impairment is in turn associated with metabolic and nutritional derangements and with increased risk of cardiovascular disease. AIM: To compare the metabolic, nutritional, and cardiovascular impact of reduced kidney function between patients with and without known renal disease. MATERIALS AND METHODS: We enrolled consecutive outpatients (age ≥65 years) with reduced renal function who were divided into two groups: Group A with history of renal disease and Group B with unknown renal disease...
2017: Frontiers in Nutrition
https://www.readbyqxmd.com/read/28364639/the-impacts-of-emergent-pollutants-on-ruditapes-philippinarum-biochemical-responses-to-carbon-nanoparticles-exposure
#15
Lucia De Marchi, Victor Neto, Carlo Pretti, Etelvina Figueira, Federica Chiellini, Amadeu M V M Soares, Rosa Freitas
Multi-walled carbon nanotubes (MWCNTs) are one of the most important carbon Nanoparticles (NPs). The production and use of these NPs are increasing rapidly and, therefore, the need to assess their presence in the environment and associated risks has become of prime importance. Recent studies demonstrated the impacts of different NPs on bivalves, a taxonomic group where species tolerance to anthropogenic stressors, such as pollutants, is widely variable. The Manila clam Ruditapes philippinarum is one of the most commonly used bivalve species in environmental monitoring studies and ecotoxicology tests, however, to our knowledge, no information is available on biochemical alterations on this species due to MWCNTs exposure...
March 18, 2017: Aquatic Toxicology
https://www.readbyqxmd.com/read/28359849/a-review-on-traditional-uses-phytochemistry-pharmacology-pharmacokinetics-and-toxicology-of-the-genus-peganum
#16
REVIEW
Shuping Li, Xuemei Cheng, Changhong Wang
ETHNOPHARMACOLOGICAL RELEVANCE: The plants of the genus Peganum have a long history as a Chinese traditional medicine for the treatment of cough, hypertension, diabetes, asthma, jaundice, colic, lumbago, and many other human ailments. Additionally, the plants can be used as an amulet against evil-eye, dye and so on, which have become increasingly popular in Asia, Iran, Northwest India, and North Africa. AIM OF THE REVIEW: The present paper reviewed the ethnopharmacology, phytochemistry, analytical methods, biological activities, metabolism, pharmacokinetics, toxicology, and drug interaction of the genus Peganum in order to assess the ethnopharmacological use and to explore therapeutic potentials and future opportunities for research...
March 27, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28358738/%C3%AE-7-nicotinic-acetylcholine-receptor-inhibition-by-indinavir-implications-for-cognitive-dysfunction-in-treated-hiv-disease
#17
Sean Ekins, Paul Mathews, Erin K Saito, Natalie Diaz, David Naylor, Julia Chung, Aaron M McMurtray
OBJECTIVE: This study set out to determine if the human immunodeficiency virus (HIV) protease inhibitor, indinavir, alters responsiveness of α7-nicotinic acetylcholine receptors to acetylcholine. DESIGN: Treatment with highly active antiretroviral therapy has dramatically reduced development of HIV associated dementia and more severe forms of cognitive impairment. However, many individuals continue to experience cognitive decline of uncertain etiology. Previous studies have failed to demonstrate significant alterations of functional brain connectivity, structural brain changes, or changes in cerebral blood flow sufficient to explain cognitive decline in virally suppressed individuals...
March 29, 2017: AIDS
https://www.readbyqxmd.com/read/28357095/hepatectomy-combined-with-microwave-ablation-of-the-spleen-for-treatment-of-hepatocellular-carcinoma-complicated-with-splenomegaly-a-retrospective-study
#18
Jian-Bo Han, Feng-Wei Kong, Hai Ding, Yu-Feng Zhang, Jun-Mao Liu, Qiang Wei, Liang Hu, Liang Zhao, Chuan-Jun Xu, Yong-Xiang Yi
The present retrospective study aimed to investigate the mid-term safety and efficacy of hepatectomy combined with microwave ablation of the partial spleen for treatment of liver cancer complicated with hypersplenism. A retrospective analysis was performed on 23 patients who underwent hepatectomy combined with microwave ablation of the partial spleen for liver cancer, complicated with hypersplenism that was secondary to cirrhosis. The splenic and ablated volumes were calculated according to a contrast-enhanced computed tomography scan prior to and 2 weeks after the operation...
February 2017: Molecular and Clinical Oncology
https://www.readbyqxmd.com/read/28356027/natural-polyphenols-in-the-treatment-of-alzheimer-s-disease
#19
Syed Badrul Syarifah Noratiqah, Isa Naina-Mohamed, Mohamed S Zulfarina, H M S Qodriyah
Neurodegenerative disease is an incurable disease which involves the degeneration or death of the nerve cells. Alzheimer's Disease (AD) is a neurodegenerative disease discovered in 1906 by Alois Alzheimer, a German clinical psychiatrist and neuroanatomist. The main pathological hallmarks of this disease are the formation of extracellular amyloid β (Aβ) plaques and intracellular neurofibrillary tangle (NFT). The accumulation of the amyloid protein aggregates in the brain of AD patients leads to oxidative stress and inflammation...
March 28, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28355738/-research-on-risk-factors-of-short-term-outcome-in-aids-patients-with-pneumocystis-pneumonia
#20
A X Li, C Y Huang, H W Zhang, T Zhang, H Wu, W Wang
Objective: To investigate the prognostic risk factors of acquired immunodeficiency syndrome (AIDS) patients with pneumocystis pneumonia (PCP), and to establish risk models for predicting early outcome. Methods: The clinical data of 418 AIDS patients with PCP admitted to Department of Infectious Diseases, Beijing You'an Hospital, Capital Medical University from January 2008 to May 2016 were retrospectively analyzed.The patients were divided into death group and survival group according to clinical outcome during hospitalization...
March 21, 2017: Zhonghua Yi Xue za Zhi [Chinese medical journal]
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