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cholinesterase inhibitor

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https://www.readbyqxmd.com/read/29243208/plasma-cholinesterase-activity-in-female-green-turtles-chelonia-mydas-nesting-in-laguna-de-terminos-mexico-related-to-organochlorine-pesticides-in-their-eggs
#1
Gerardo Rivas-Hernández, Yaneli May-Uc, Elsa Noreña-Barroso, Víctor Cobos-Gasca, Gabriela Rodríguez-Fuentes
The inhibition of cholinesterase (ChE) activity has been used as a biomarker of exposure to organophosphate and carbamate insecticides. ChE of nesting female green turtles (Chelonia mydas) were biochemically characterized using two substrates, acetylthiocholine iodide and butyrylthiocholine iodide, and three ChE inhibitors (eserine sulfate, BW284C51 and iso-OMPA). The results indicated that BChE is the predominant plasma ChE in female C. mydas, but with atypical properties that differ from those found in human BChE...
December 14, 2017: Bulletin of Environmental Contamination and Toxicology
https://www.readbyqxmd.com/read/29243034/application-of-pyridostigmine-in-pediatric-gastrointestinal-motility-disorders-a-case-series
#2
Mhd Louai Manini, Michael Camilleri, Rayna Grothe, Carlo Di Lorenzo
BACKGROUND: Gastrointestinal (GI) motility disorders are common in children. Treatment is challenging with limited medical and surgical options. Pyridostigmine, an acetyl cholinesterase inhibitor, increases acetylcholine at the neuromuscular junction promoting intestinal contractions. Little is known about the role and dosing of pyridostigmine in pediatric GI motility disorders. METHODS: We present a case series of children with GI dysmotility managed with oral pyridostigmine...
December 14, 2017: Paediatric Drugs
https://www.readbyqxmd.com/read/29231138/cholinesterase-inhibitor-6-chlorotacrine-in-vivo-toxicological-profile-and-behavioural-effects
#3
Jan Misik, Eugenie Nepovimova, Jaroslav Pejchal, Jiri Kassa, Jan Korabecny, Ondrej Soukup
BACKGROUND: 6-chlorotacrine is a cholinesterase inhibitor showing good inhibitory potential, even better than parent compound tacrine, in vitro. Despite tacrine scaffold is broadly used for design and synthesis of novel compounds with anti-Alzheimer's potential, no in vivo effects have been investigated so far. Thus, basic toxicological and behavioural evaluation has been carried out throughout this study. METHODS: Maximum tolerated dose (MTD) and median lethal dose (LD50) were assessed in BALB/c mice and Wistar rats...
December 11, 2017: Current Alzheimer Research
https://www.readbyqxmd.com/read/29222591/dementia-with-lewy-bodies-and-parkinson-s-disease-dementia-current-concepts-and-controversies
#4
REVIEW
Kurt A Jellinger
Dementia with Lewy bodies (DLB) and Parkinson's disease-dementia (PDD), although sharing many clinical, neurochemical and morphological features, according to DSM-5, are two entities of major neurocognitive disorders with Lewy bodies of unknown etiology. Despite considerable clinical overlap, their diagnosis is based on an arbitrary distinction between the time of onset of motor and cognitive symptoms: dementia often preceding parkinsonism in DLB and onset of cognitive impairment after onset of motor symptoms in PDD...
December 8, 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/29210284/can-persistence-with-cholinesterase-inhibitor-treatment-lower-mortality-and-health-care-costs-among-patients-with-alzheimer-s-disease-a-population-based-study-in-taiwan
#5
Li-Jung Elizabeth Ku, Chung-Yi Li, Yu Sun
Although cholinesterase inhibitors (ChEIs) have been proved to help reduce cognitive deterioration in patients with Alzheimer's disease (AD), their effects on survival remain inconclusive. This study aims to assess the effects of the persistent use of ChEIs on the risk of mortality in patients with AD. This population-based cohort study included 8614 patients having AD with ChEI prescription from 2002 to 2006 and followed until 2010. Kaplan-Meier curves and hazard ratios (HRs) of mortality were estimated in association with ChEI treatment duration and adherence...
January 1, 2017: American Journal of Alzheimer's Disease and Other Dementias
https://www.readbyqxmd.com/read/29209218/nootropic-and-neuroprotective-effects-of-dichrocephala-integrifolia-on-scopolamine-mouse-model-of-alzheimer-s-disease
#6
Nadège E Kouémou, Germain S Taiwe, Fleur C O Moto, Simon Pale, Gwladys T Ngoupaye, Jacqueline S K Njapdounke, Gisèle C N Nkantchoua, David B Pahaye, Elisabeth Ngo Bum
Alzheimer's disease the most common form of dementia in the elderly is a neurodegenerative disease that affects 44 millions of people worldwide. The first treatments against Alzheimer's disease are acetylcholinesterase inhibitors; however, these medications are associated with many side effects. Dichrocephala integrifolia is a traditional herb widely used by indigenous population of Cameroon to treat and prevent Alzheimer's disease and for memory improvement. In this study, we evaluated the effect of the decoction prepared from leaves of D...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29190477/synthesis-and-biological-evaluation-of-new-oxopyrrolidine-derivatives-as-inhibitors-of-acetyl-cholinesterase-and-%C3%AE-amyloid-protein-as-anti-alzheimer-s-agents
#7
Lamia W Mohamed, Suzan M Abuel-Maaty, Waleed A Mohammed, May A Galal
A new series of oxopyrrolidines was synthesized and evaluated for their effect on Alzheimer's disease by measuring their inhibitory activity against acetyl cholinesterase enzyme and amyloid β 42 protein. Most of the compounds showed good inhibitory activity with ethyl 2-(2-(2, 6-dimethylphenylcarbamoyl)- 5-oxopyrrolidin-1-yl) acetate (V) having the highest activity against acetyl cholinesterase with IC50 value 1.84 ng/g tissue compared to standard donepezil 3.34 ng/g tissue. Furthermore, compound 1-((4-(4-chlorophenyl) piperazin-1-yl) methyl)-N-(2,6-dimethylphenyl)-5- oxopyrrolidine- 2-carboxamide (IIIe) displayed the highest activity against β 42 protein with IC50 value of 11...
November 15, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29183615/rna-interference-of-acetylcholinesterase-in-the-asian-citrus-psyllid-diaphorina-citri-increases-its-susceptibility-to-carbamate-and-organophosphate-insecticides
#8
Abdelaziz Kishk, Faraj Hijaz, Helmy A I Anber, Tsamoh K AbdEl-Raof, AbdEl-Hakeem D El-Sherbeni, Sobhy Hamed, Nabil Killiny
The Asian citrus psyllid, Diaphorina citri Kuwayama (Hemiptera: Lividae) transmits the Candidatus Liberibacter asiaticus, which causes citrus greening disease or Huanglongbing, (HLB). To date, there is no efficient cure for HLB disease and the control of D. citri using insecticides became the most important tools for the management of HLB. However, the extensive use of insecticides could increase D. citri resistance to these insecticides. The objective of this study was to investigate the effect of RNA interference of acetylcholinesterase (AChE) on the mortality and susceptibility of D...
November 2017: Pesticide Biochemistry and Physiology
https://www.readbyqxmd.com/read/29175588/modification-of-bischler-m%C3%A3-hlau-indole-derivatives-through-palladium-catalyzed-suzuki-reaction-as-effective-cholinesterase-inhibitors-their-kinetic-and-molecular-docking-studies
#9
Shaista Parveen, Muhammad Shakil Shah, Sumera Zaib, Tayyaba Gul, Khalid Mohammed Khan, Jamshed Iqbal, Abbas Hassan
Due to the immense importance of aryl indole nucleus, herein we report the palladium-catalyzed arylation of N-substituted 2-aryl indole utilizing Suzuki-Miyaura cross coupling methodology. The biological screening for cholinesterase inhibition of the resulted biaryl indole moieties was carried out to evaluate their pharmacological potential, expecting to involve the development of new therapeutics for various inflammatory, cardiovascular, gastrointestinal and neurological diseases. This research work also involved the use of utilization of microwave-assisted organic synthesis (MAOS) for the synthesis of Bischler-Möhlau indole which is further biarylated via palladium-catalyzed cross coupling reaction...
November 17, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29174877/cholinesterase-inhibitor-discontinuation-the-buck-stops-here
#10
EDITORIAL
Nathan Herrmann
No abstract text is available yet for this article.
October 31, 2017: American Journal of Geriatric Psychiatry
https://www.readbyqxmd.com/read/29171993/prevalence-of-delirium-in-a-population-of%C3%A2-elderly-outpatients-with-dementia-a%C3%A2-retrospective-study
#11
Desirée Addesi, Raffaele Maio, Nicoletta Smirne, Valentina Laganà, Natalia Altomari, Gianfranco Puccio, Rosanna Colao, Chiara Cupidi, Francesco Perticone, Amalia Cecilia Bruni
BACKGROUND: Delirium is a multifactorial geriatric syndrome and often occurs in patients with cognitive impairment. It also remains under-recognized, specifically in elderly outpatients, because signs of delirium might overlap with symptoms of dementia. OBJECTIVE: The aim of the present study is to retrospectively apply the chart-based delirium instrument on a cohort of elderly outpatients with dementia, to assess prevalence and features of delirium in this population...
November 20, 2017: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/29167930/planarian-cholinesterase-molecular-and-functional-characterization-of-an-evolutionarily-ancient-enzyme-to-study-organophosphorus-pesticide-toxicity
#12
Danielle Hagstrom, Siqi Zhang, Alicia Ho, Eileen S Tsai, Zoran Radić, Aryo Jahromi, Kelson J Kaj, Yingtian He, Palmer Taylor, Eva-Maria S Collins
The asexual freshwater planarian Dugesia japonica has emerged as a medium-throughput alternative animal model for neurotoxicology. We have previously shown that D. japonica are sensitive to organophosphorus pesticides (OPs) and characterized the in vitro inhibition profile of planarian cholinesterase (DjChE) activity using irreversible and reversible inhibitors. We found that DjChE has intermediate features of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Here, we identify two candidate genes (Djche1 and Djche2) responsible for DjChE activity...
November 22, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/29167065/a-systematic-review-of-practice-guidelines-and-recommendations-for-discontinuation-of-cholinesterase-inhibitors-in-dementia
#13
REVIEW
Brenna N Renn, Ali Abbas Asghar-Ali, Stephen Thielke, Angela Catic, Sharyl R Martini, Brian G Mitchell, Mark E Kunik
Cholinesterase inhibitors (ChEIs) are the primary pharmacological treatment for symptom management of Alzheimer disease (AD), but they carry known risks during long-term use, and do not guarantee clinical effects over time. The balance of risks and benefits may warrant discontinuation at different points during the disease course. Indeed, although there is limited scientific study of deprescribing ChEIs, clinicians routinely face practical decisions about whether to continue or stop medications. This review examined published practice recommendations for discontinuation of ChEIs in AD...
October 10, 2017: American Journal of Geriatric Psychiatry
https://www.readbyqxmd.com/read/29143695/an-overview-of-systematic-reviews-of-pharmacological-and-non-pharmacological-interventions-for-the-treatment-of-behavioral-and-psychological-symptoms-of-dementia
#14
Suzanne M Dyer, Stephanie L Harrison, Kate Laver, Craig Whitehead, Maria Crotty
BACKGROUND: This systematic overview reports findings from systematic reviews of randomized controlled trials of pharmacological and non-pharmacological interventions for behavioural and psychological symptoms of dementia (BPSD). METHODS: The Cochrane Database of Systematic Reviews, DARE, Medline, EMBASE, and PsycINFO were searched to September 2015. RESULTS: Fifteen systematic reviews of eighteen different interventions were included. A significant improvement in BPSD was seen with: functional analysis-based interventions (GRADE quality of evidence moderate; standardized mean difference (SMD) -0...
November 16, 2017: International Psychogeriatrics
https://www.readbyqxmd.com/read/29142396/antioxidant-and-cholinesterase-inhibitory-activities-of-ethyl-acetate-extract-of-terminalia-chebula-cell-free-in-vitro-and-in-silico-studies
#15
Mohamed Asik Rajmohamed, Suganthy Natarajan, Premkumar Palanisamy, Akbarsha Mohammad Abdulkader, Archunan Govindaraju
Background: Alzheimer's disease (AD) is a progressive neurodegenerative disorder clinically characterized by memory loss and impaired cognitive function. Cholinergic enzyme deficiency and oxidative stress are the two major factors implicated in the pathogenesis of AD. The symptomatic treatment, as of now, is the use of cholinesterase inhibitors toward cholinergic "downturn." Therefore, there is a search for compounds that will be useful in focused therapies. There has been suggestion that Terminalia chebula fruit would be a potential source...
October 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/29135926/proline-based-carbamates-as-cholinesterase-inhibitors
#16
Hana Pizova, Marketa Havelkova, Sarka Stepankova, Andrzej Bak, Tereza Kauerova, Violetta Kozik, Michal Oravec, Ales Imramovsky, Peter Kollar, Pavel Bobal, Josef Jampilek
Series of twenty-five benzyl (2S)-2-(arylcarbamoyl)pyrrolidine-1-carboxylates was prepared and completely characterized. All the compounds were tested for their in vitro ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), and the selectivity of compounds to individual cholinesterases was determined. Screening of the cytotoxicity of all the compounds was performed using a human monocytic leukaemia THP-1 cell line, and the compounds demonstrated insignificant toxicity. All the compounds showed rather moderate inhibitory effect against AChE; benzyl (2S)-2-[(2-chlorophenyl)carbamoyl]pyrrolidine-1-carboxylate (IC50 = 46...
November 14, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29127449/determining-a-threshold-sub-acute-dose-leading-to-minimal-physiological-alterations-following-prolonged-exposure-to-the-nerve-agent-vx-in-rats
#17
E Bloch-Shilderman, I Rabinovitz, I Egoz, G Yacov, N Allon, U Nili
VX, a potent inhibitor of cholinesterase (ChE), is considered as one of the most toxic, persistent and least volatile nerve agents. VX is absorbed in various environmental surfaces and is gradually released long after its initial dispersal. Its toxicity is mainly caused by disrupting central and peripheral cholinergic nervous system activity, leading to potential long-term detrimental effects on health. The primary objective of the present study was to assess the threshold VX dose leading to minimal physiological alterations following prolonged VX exposure...
November 10, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/29126732/2-arylbenzofurans-from-artocarpus-lakoocha-and-methyl-ether-analogs-with-potent-cholinesterase-inhibitory-activity
#18
Umalee Namdaung, Anan Athipornchai, Thongchai Khammee, Mayuso Kuno, Sunit Suksamrarn
In vitro screening for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of the Artocarpus lakoocha root-bark extracts revealed interesting results. Bioassay-guided fractionation resulted in the isolation of two new (1 and 2) and six known 2-arylbenzofurans 3-8, along with one stilbenoid 9 and one flavonoid 10. The structures of the isolated compounds were elucidated by UV, IR, 1D- and 2D-NMR and MS spectroscopic data analysis. Compounds 4, 6 and 7 exhibited more potent AChE inhibitory activity (IC50 = 0...
October 12, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29125188/the-mouse-passive-transfer-model-of-musk-myasthenia-gravis-disrupted-musk-signaling-causes-synapse-failure
#19
REVIEW
Nazanin Ghazanfari, Sofie Trajanovska, Marco Morsch, Simon X Liang, Stephen W Reddel, William D Phillips
While the majority of myasthenia gravis patients express antibodies targeting the acetylcholine receptor, the second most common cohort instead displays autoantibodies against muscle-specific kinase (MuSK). MuSK is a transmembrane tyrosine kinase found in the postsynaptic membrane of the neuromuscular junction. During development, MuSK serves as a signaling hub, coordinating the alignment of the pre- and postsynaptic components of the synapse. Adult mice that received repeated daily injections of IgG from anti-MuSK(+) myasthenia gravis patients developed muscle weakness, associated with neuromuscular transmission failure...
November 10, 2017: Annals of the New York Academy of Sciences
https://www.readbyqxmd.com/read/29116600/recent-progress-in-the-pharmacotherapy-of-alzheimer-s-disease
#20
Rita Khoury, Kush Patel, Jake Gold, Stephanie Hinds, George T Grossberg
Alzheimer's disease is the most common major neurocognitive disorder with substantial social and economic impacts. This article is an update on current pharmacotherapy, advancements in biomarker use, and drugs in the pipeline for this disease. To date, no new drug has qualified to be added to the current therapeutic arsenal comprising cholinesterase inhibitors and the NMDA receptor antagonist memantine. Drugs in the pipeline include symptomatic therapies that are neurotransmitter-based, but mostly disease-modifying therapies...
November 7, 2017: Drugs & Aging
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