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Cholinesterase inhibitors

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https://www.readbyqxmd.com/read/28715142/cholinesterase-inhibition-reduces-arrhythmias-in-asymptomatic-chagas-disease
#1
Renata Rodrigues Teixeira de Castro, Graciema Porphirio, Sergio Salles Xavier, Ruy Silveira Moraes, Elton Luis Ferlin, Jorge Pinto Ribeiro, Antonio Claudio Lucas da Nóbrega
INTRODUCTION: Parasympathetic dysfunction may play a role in the genesis of arrhythmias in Chagas disease. AIM: This study evaluates the acute effects of pyridostigmine (PYR), a reversible cholinesterase inhibitor, on the occurrence of arrhythmias in patients with Chagas cardiac disease. METHOD: Following a double-blind, randomized, placebo-controlled, cross-over protocol, 17 patients (age 50±2 years) with Chagas cardiac disease type B underwent 24-hour Holter recordings after oral administration of either pyridostigmine bromide (45 mg, 3 times/day) or placebo (PLA)...
July 17, 2017: Cardiovascular Therapeutics
https://www.readbyqxmd.com/read/28714881/assessment-of-enzyme-inhibition-a-review-with-examples-from-the-development-of-monoamine-oxidase-and-cholinesterase-inhibitory-drugs
#2
REVIEW
Rona R Ramsay, Keith F Tipton
The actions of many drugs involve enzyme inhibition. This is exemplified by the inhibitors of monoamine oxidases (MAO) and the cholinsterases (ChE) that have been used for several pharmacological purposes. This review describes key principles and approaches for the reliable determination of enzyme activities and inhibition as well as some of the methods that are in current use for such studies with these two enzymes. Their applicability and potential pitfalls arising from their inappropriate use are discussed...
July 15, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28714400/cholinesterase-inhibitory-activity-of-some-semi-rigid-spiro-heterocycles-pom-analyses-and-crystalline-structure-of-pharmacophore-site
#3
Taibi Ben Hadda, Oualid Talhi, Artur S M Silva, Fatma Sezer Senol, Ilkay Erdogan Orhan, Abdur Rauf, Yahia N Mabkhot, Khaldoun Bachari, Ismail Warad, Thoraya A Farghaly, Ismail I Althagafi, Mohammad S Mubarak
Cholinesterase family consists of two sister enzymes; acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) which hydrolyze acetylcholine. Since deficit of acetylcholine has been evidenced in the patients of Alzheimer's disease (AD), cholinesterase inhibitors are currently the most prescribed drug class for the treatment of AD. In the present study, five compounds (2-6) with spiro skeleton have been synthesized and tested for their inhibitory potential in vitro against AChE and BChE using ELISA microtiter plate assays at 25 mg/mL...
July 13, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28711758/assessing-the-binding-of-cholinesterase-inhibitors-by-docking-and-molecular-dynamics-studies
#4
M Rejwan Ali, Mostafa Sadoqi, Simon G Møller, Allal Boutajangout, Mihaly Mezei
In this report we assessed by docking and molecular dynamics the binding mechanisms of three FDA-approved Alzheimer drugs, inhibitors of the enzyme acetylcholinesterase (AChE): donepezil, galantamine and rivastigmine. Dockings by the softwares Autodock-Vina, PatchDock and Plant reproduced the docked conformations of the inhibitor-enzyme complexes within 2Å of RMSD of the X-ray structure. Free-energy scores show strong affinity of the inhibitors for the enzyme binding pocket. Three independent Molecular Dynamics simulation runs indicated general stability of donepezil, galantamine and rivastigmine in their respective enzyme binding pocket (also referred to as gorge) as well as the tendency to form hydrogen bonds with the water molecules...
June 29, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28699213/acetamide-derivatives-of-chromen-2-ones-as-potent-cholinesterase-inhibitors
#5
Suchita Prasad, Bipul Kumar, Shiv Kumar, Karam Chand, Shashank S Kamble, Hemant K Gautam, Sunil K Sharma
Alzheimer's disease (AD), a neurodegenerative disorder, is a serious medical issue worldwide with drastic social consequences. Inhibition of cholinesterase is one of the rational and effective approaches to retard the symptoms of AD and, hence, consistent efforts are being made to develop efficient anti-cholinesterase agents. In pursuit of this, a series of 19 acetamide derivatives of chromen-2-ones were synthesized and evaluated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory potential...
July 12, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28698023/inhibitory-effects-of-serratene-type-triterpenoids-from-lycopodium-complanatum-on-cholinesterases-and-%C3%AE-secretase-1
#6
Van Thu Nguyen, Bing Tian Zhao, Su Hui Seong, Jeong Ah Kim, Mi Hee Woo, Jae Sui Choi, Byung Sun Min
Phytochemical investigation of Lycopodium complanatum whole plants led to the isolation of two new serratene-type triterpenoids (1 and 2) along with eight known triterpenoids (3-10). Their structures were established using 1D and 2D NMR spectroscopic techniques and mass spectrometry. These compounds did not inhibit acetylcholinesterases (AChE) and butyrylcholinesterase (BChE), but did inhibit β-secretase 1 (BACE1). Compounds 1 and 6 showed potent BACE1 inhibition with IC50 values of 2.79 ± 0.28 and 2.49 ± 0...
July 8, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28688279/synthesis-of-novel-5-aroylhydrazinocarbonyl-escitalopram-as-cholinesterase-inhibitors
#7
Mehr-Un Nisa, Munawar A Munawar, Amber Iqbal, Asrar Ahmed, Muhammad Ashraf, Qurra-Tul-Ann A Gardener, Misbahul A Khan
A novel series of 5-(aroylhydrazinocarbonyl)escitalopram (58-84) have been designed, synthesized and tested for their inhibitory potential against cholinesterases. 3-Chlorobenzoyl- (71) was found to be the most potent compound of this series having IC50 1.80 ± 0.11 μM for acetylcholinesterase (AChE) inhibition. For the butyrylcholinesterase (BChE) inhibition, 2-bromobenzoyl- (76) was the most active compound of the series with IC50 2.11 ± 0.31 μM. Structure-activity relationship illustrated that mild electron donating groups enhanced enzyme inhibition while electron withdrawing groups reduced the inhibition except o-NO2...
June 30, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28687725/design-and-development-of-a-novel-chalcone-derivative-as-an-anticholinesterase-inhibitor-for-possible-treatment-of-dementia
#8
Fu-Chun Zhao, Yan Wu, Xiao-Jie Song
BACKGROUND Cognitive decline (e.g., memory loss), which mainly occurs in the elderly, is termed dementia. In the present study, we intended to explore the cholinesterase inhibitory activity of some novel synthesized chalcones, together with their effect on β-amyloid anti-aggregation. MATERIAL AND METHODS A novel class of chalcone derivatives have been synthesized and characterized by FT-IR, ¹H-NMR, ¹³C-NMR, and mass and elemental analysis. These derivatives were later used for the determination of acetylcholinesterase (AChE) inhibitory and b-amyloid anti-aggregation activity...
July 8, 2017: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/28674252/the-long-lasting-enhancing-effect-of-distigmine-on-acetylcholine-induced-contraction-of-guinea-pig-detrusor-smooth-muscle-correlates-with-its-anticholinesterase-activity
#9
Keisuke Obara, Tsukasa Ogawa, Daisuke Chino, Yoshio Tanaka
Distigmine bromide (distigmine), a reversible, long-lasting cholinesterase (ChE) inhibitor, is used for the treatment of underactive bladder in Japan and has been shown to potentiate urinary bladder (UB) contractility. We studied the duration of distigmine's potentiating effects on acetylcholine (ACh)-induced UB contraction and its inhibitory effects on ChE activity, and compared that with those of other ChE inhibitors (neostigmine, pyridostigmine, and ambenonium). The duration of potentiating/inhibitory effects of ChE inhibitors, including distigmine, on ACh-induced guinea pig UB contraction/ChE activity was evaluated for 12 h following washout...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28673719/newly-developed-drugs-for-alzheimer-s-disease-in-relation-to-energy-metabolism-cholinergic-and-monoaminergic-neurotransmission
#10
REVIEW
Jan Korábečný, Eugenie Nepovímová, Tereza Cikánková, Katarína Špilovská, Lucie Vašková, Eva Mezeiová, Kamil Kuča, Jana Hroudová
Current options for Alzheimer's disease (AD) treatment are based on administration of cholinesterase inhibitors (donepezil, rivastigmine, galantamine) and/or memantine, acting as an N-methyl-D-aspartate (NMDA). Therapeutic approaches vary and include novel cholinesterase inhibitors, modulators of NMDA receptors, monoamine oxidase (MAO) inhibitors, immunotherapeutics, modulators of mitochondrial permeability transition pores (mPTP), amyloid-beta binding alcohol dehydrogenase (ABAD) modulators, antioxidant agents, etc...
July 1, 2017: Neuroscience
https://www.readbyqxmd.com/read/28671413/alzheimer-disease-pharmacologic-and-nonpharmacologic-therapies-for-cognitive-and-functional-symptoms
#11
Ted Epperly, Megan A Dunay, Jack L Boice
Alzheimer disease comprises a syndrome of progressive cognitive and functional decline. Treatments should target cognitive and functional symptoms. Cholinesterase inhibitors, memantine, and a combination of a cholinesterase inhibitor and memantine have produced statistically significant but clinically small delays in various domains of cognitive and functional decline in select patients with Alzheimer disease. Vitamin E has been shown to delay functional decline in patients with mild to moderate Alzheimer disease, especially when taken in combination with a cholinesterase inhibitor...
June 15, 2017: American Family Physician
https://www.readbyqxmd.com/read/28670949/preparation-and-optimization-of-rivastigmine-loaded-tocopherol-succinate-based-solid-lipid-nanoparticles
#12
Fariba Malekpour-Galogahi, Ashrafalasadat Hatamian-Zarmi, Fariba Ganji, Bahman Ebrahimi-Hosseinzadeh, Fahimeh Nojoki, Razi Sahraeian, Zahra Beagom Mokhtari-Hosseini
Rivastigmine hydrogen tartrate (RHT) is a pseudo-irreversible inhibitor of cholinesterase, and is used for the treatment of Alzheimer's. However, RHT delivery to the brain is limited by the Blood-Brain Barrier (BBB). The purpose of this study was to improve the brain-targeting delivery of RHT by producing and optimizing rivastigmine hydrogen tartrate-loaded tocopherol succinate-based solid lipid nanoparticles (RHT-SLNs). RHT-SLNs were prepared using the microemulsion technique. The impact of significant variables such as surfactant concentration and drug/lipid ratio on the size of RHT-SLNs and their drug loading and encapsulation efficiency was analyzed using a five-level central composite design (CCD)...
July 2, 2017: Journal of Liposome Research
https://www.readbyqxmd.com/read/28655740/diabetes-in-a-large-dementia-cohort-clinical-characteristics-and-treatment-from-the-swedish-dementia-registry
#13
Juraj Secnik, Pavla Cermakova, Seyed-Mohammad Fereshtehnejad, Pontus Dannberg, Kristina Johnell, Johan Fastbom, Bengt Winblad, Maria Eriksdotter, Dorota Religa
OBJECTIVE: We aimed to investigate the differences in clinical characteristics and pharmacological treatment associated with the presence of diabetes in a large cohort of patients with dementia. RESEARCH DESIGN AND METHODS: A cross-sectional registry-based study was conducted using data from the Swedish Dementia Registry (SveDem). Data on dementia diagnosis, dementia type, and demographic determinants were extracted from SveDem. Data from Swedish Patient Register and Prescribed Drug Register were combined for the diagnosis of diabetes...
June 27, 2017: Diabetes Care
https://www.readbyqxmd.com/read/28650104/alzheimer-s-disease-and-metabolic-syndrome-a-link-from-oxidative-stress-and-inflammation-to-neurodegeneration
#14
REVIEW
Eduardo Rojas-Gutierrez, Guadalupe Muñoz-Arenas, Samuel Treviño, Blanca Espinosa, Raúl Chavez, Karla Rojas, Gonzalo Flores, Alfonso Díaz, Jorge Guevara
Alzheimer's disease (AD) is the most common cause of dementia and one of the most important causes of morbidity and mortality among the aging population. AD diagnosis is made post-mortem, and the two pathologic hallmarks, particularly evident in the end stages of the illness, are amyloid plaques and neurofibrillary tangles (NFT). Currently, there is no curative treatment for AD. Additionally, there is a strong relation between oxidative stress, metabolic syndrome (MetS) and AD. The high levels of circulating lipids and glucose imbalances amplify lipid peroxidation that gradually diminishes the antioxidant systems, causing high levels of oxidative metabolism that affects cell structure, leading to neuronal damage...
June 26, 2017: Synapse
https://www.readbyqxmd.com/read/28646835/association-between-blood-cholinesterase-activity-organophosphate-pesticide-residues-on-hands-and-health-effects-among-chili-farmers-in-ubon-ratchathani-province-northeastern-thailand
#15
Thitirat Nganchamung, Mark G Robson, Wattasit Siriwong
Background: Use of pesticides has been documented to lead to several adverse health effects. Farmers are likely to be exposed to pesticides through dermal exposure as a result of mixing, loading, and spraying. Organophosphate pesticides (OPs) are widely used in most of the agricultural areas throughout Thailand. OPs are cholinesterase inhibitors and blood cholinesterase activity is used as a biomarker of OP effects. Objective: This study aims to determine the association between blood cholinesterase activity and organophosphate pesticide residues on chili farmer’s hands and their adverse health effects...
2017: Roczniki Państwowego Zakładu Higieny
https://www.readbyqxmd.com/read/28638340/neurologically-potent-molecules-from-crataegus-oxyacantha-isolation-anticholinesterase-inhibition-and-molecular-docking
#16
Mumtaz Ali, Sultan Muhammad, Muhammad R Shah, Ajmal Khan, Umer Rashid, Umar Farooq, Farhat Ullah, Abdul Sadiq, Muhammad Ayaz, Majid Ali, Manzoor Ahmad, Abdul Latif
Crataegus oxyacantha is an important herbal supplement and famous for its antioxidant potential. The antioxidant in combination with anticholinesterase activity can be considered as an important target in the management of Alzheimer's disease. The compounds isolated from C. oxyacantha were evaluated for cholinesterases inhibitory activity using Ellman's assay with Galantamine as standard drug. Total of nine (1-9) compounds were isolated. Compounds 1 and 2 were isolated for the first time from natural source...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28631100/co-modulation-of-an-allosteric-modulator-of-nicotinic-receptor-cholinesterase-inhibitor-galantamine-and-a-5-ht4-receptor-agonist-rs-67333-effect-on-scopolamine-induced-memory-deficit-in-the-mouse
#17
Thomas Freret, Véronique Lelong-Boulouard, Pierre Lecouflet, Katia Hamidouche, François Dauphin, Michel Boulouard
AIM: It is widely assumed that the upcoming therapeutics for Alzheimer's disease will require to act on more than one target to be effective. We investigated here whether a combination of the nicotinic receptor allosteric modulator/cholinesterase inhibitor galantamine can act synergistically with the type 4 serotonin receptor (5-HT4R) partial agonist, RS-67333, to counterbalance deficits in short- and long-term memory. To select sub-efficacious doses of both drugs, dose-response studies were first performed on the scopolamine-induced deficits of spontaneous alternation in the Y-maze task and of acquisition and retrieval processes in a passive avoidance task...
June 19, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28629119/cholinesterase-inhibitory-activities-of-adamantyl-based-derivatives-and-their-molecular-docking-studies
#18
Huey Chong Kwong, Siau Hui Mah, Tze Shyang Chia, Ching Kheng Quah, Gin Keat Lim, C S Chidan Kumar
Adamantyl-based compounds are clinically important for the treatments of type 2 diabetes and for their antiviral abilities, while many more are under development for other pharmaceutical uses. This study focused on the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of adamantyl-based ester derivatives with various substituents on the phenyl ring using Ellman's colorimetric method. Compound 2e with a 2,4-dichloro electron-withdrawing substituent on the phenyl ring exhibited the strongest inhibition effect against AChE, with an IC50 value of 77...
June 17, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28626471/early-versus-late-onset-alzheimer-disease-long-term-functional-outcomes-nursing-home-placement-and-risk-factors-for-rate-of-progression
#19
Carina Wattmo, Åsa K Wallin
BACKGROUND/AIMS: Whether age at onset influences functional deterioration in Alzheimer disease (AD) is unclear. We, therefore, investigated risk factors for progression in activities of daily living (ADL) and nursing home placement (NHP) in cholinesterase inhibitor (ChEI)-treated patients with early-onset AD (EOAD) versus late-onset AD (LOAD). METHODS: This 3-year, prospective, observational, multicenter study included 1,017 participants with mild-to-moderate AD; 143 had EOAD (onset <65 years) and 874 LOAD (onset ≥65 years)...
January 2017: Dementia and Geriatric Cognitive Disorders Extra
https://www.readbyqxmd.com/read/28606768/genetic-analysis-of-the-ric3-gene-in-han-chinese-patients-with-parkinson-s-disease
#20
Dan He, Pengzhi Hu, Xiong Deng, Zhi Song, Lamei Yuan, Xiuhong Yuan, Hao Deng
Parkinson's disease (PD) is the second-most common etiologically complex neurodegenerative disease. Genetic abnormalities are thought to play an important role in the development of PD. Recently, mutations in the resistance to inhibitors of cholinesterase 3 gene (RIC3) have been reported to cause autosomal-dominant PD in Indian population. To determine whether RIC3 gene coding variant(s) are associated with PD in Han Chinese population, the RIC3 gene coding region in 218 mainland Han Chinese patients with PD and the identified variants in 242 normal controls were examined using direct sequencing analysis...
July 13, 2017: Neuroscience Letters
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