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cholinesterase inhibitor

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https://www.readbyqxmd.com/read/29034839/pharmacogenetics-of-angiotensin-converting-enzyme-inhibitors-in-patients-with-alzheimer-s-disease-dementia
#1
Fabricio Ferreira de Oliveira, Elizabeth Suchi Chen, Marilia Cardoso Smith, Paulo Henrique Ferreira Bertolucci
BACKGROUND: While the angiotensin-converting enzyme degrades amyloid-β, angiotensin-converting enzyme inhibitors (ACEis) may slow cognitive decline by way of cholinergic effects, by increasing brain substance P and boosting the activity of neprilysin, and by modulating glucose homeostasis and augmenting the secretion of adipokines to enhance insulin sensitivity in patients with Alzheimer's disease dementia (AD). We aimed to investigate whether ACE gene polymorphisms rs1800764 and rs4291 are associated with cognitive and functional change in patients with AD, while also taking APOE haplotypes and anti-hypertensive treatment with ACEis into account for stratification...
October 16, 2017: Current Alzheimer Research
https://www.readbyqxmd.com/read/29033232/design-synthesis-and-biological-evaluation-of-phthalimide-alkylamine-derivatives-as-balanced-multifunctional-cholinesterase-and-monoamine-oxidase-b-inhibitors-for-the-treatment-of-alzheimer-s-disease
#2
Zhipei Sang, Keren Wang, Huifang Wang, Lintao Yu, Huijuan Wang, Qianwen Ma, Mengyao Ye, Xue Han, Wenmin Liu
A series of novel phthalimide-alkylamine derivatives were synthesized and evaluated as multi-functions inhibitors for the treatment of Alzheimer's disease (AD). The results showed that compound TM-9 could be regarded as a balanced multi-targets active molecule. It exhibited potent and balanced inhibitory activities against ChE and MAO-B (huAChE, huBuChE, and huMAO-B with IC50 values of 1.2μM, 3.8μM and 2.6 μM, respectively) with low selectivity. Both kinetic analysis of AChE inhibition and molecular modeling study suggested that TM-9 binds simultaneously to the catalytic active site and peripheral anionic site of AChE...
September 28, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29032750/longitudinal-neuropsychological-outcome-in-taiwanese-alzheimer-s-disease-patients-treated-with-medication
#3
Pi-Shan Sung, Meng-Ni Wu, Ping-Song Chou, Hui-Chen Su, Sheng-Hsiang Lin, Yuan-Han Yang
Background The longitudinal change of neuropsychological tests (NPTs) in treated Alzheimer's disease (AD) is essential to understand the interplay of a therapeutic response from medication and a disease decline due to degenerative processes. The aim of our study is to investigate the annual cognitive progression as measured by commonly used NPTs in treated AD patients and to assess the potential predictors of disease progression. Methods Participants (N=455) diagnosed with AD and treated with cholinesterase inhibitors (ChEIs) or memantine at memory clinics in three hospitals in southern Taiwan from January 2009 to December 2014 were enrolled in this prospectively registered study...
October 10, 2017: Current Alzheimer Research
https://www.readbyqxmd.com/read/29032010/dual-effects-of-insect-nachr-chaperone-ric-3-on-hybrid-receptor-promoting-assembly-on-endoplasmic-reticulum-but-suppressing-transport-to-plasma-membrane-on-xenopus-oocytes
#4
Haibo Bao, Xixia Xu, Wei Liu, Na Yu, Zewen Liu
Resistance to inhibitors of cholinesterase (RIC) -3 promotes the maturation (folding and assembly) of neuronal nicotinic acetylcholine receptors (nAChRs) as a molecular chaperone. The modulation effects of RIC-3 on homomeric α7 nAChRs are always positive, but its effects on heteromeric subtypes are inconsistent among reports. In this study, five RIC-3 isoforms were identified from Locusta migratoria. Four isoforms showed obvious effects on hybrid receptor Locα1/rβ2 expressed in Xenopus oocytes. As a representative, the co-expression of RIC-3v4 exhibited the decreased agonist responses (Imax) on oocytes, lower specific [(3)H]epibatidine binding (Bmax) on plasma membrane protein (PMP), and reduced subunit levels in PMP, which showed that the mature Locα1/rβ2 on the plasma membrane was decreased by the co-expression of RIC-3...
October 11, 2017: Neurochemistry International
https://www.readbyqxmd.com/read/29031067/new-pyridine-derivatives-as-inhibitors-of-acetylcholinesterase-and-amyloid-aggregation
#5
Fabiana Pandolfi, Daniela De Vita, Martina Bortolami, Antonio Coluccia, Roberto Di Santo, Roberta Costi, Vincenza Andrisano, Francesco Alabiso, Christian Bergamini, Romana Fato, Manuela Bartolini, Luigi Scipione
A new series of pyridine derivatives with carbamic or amidic function has been designed and synthesized to act as cholinesterase inhibitors. The synthesized compounds were tested toward EeAChE and hAChE and toward eqBChE and hBChE. The carbamate 8 was the most potent hAChE inhibitor (IC50 = 0.153 ± 0.016 μM) while the carbamate 11 was the most potent inhibitor of hBChE (IC50 = 0.828 ± 0.067 μM). A molecular docking study indicated that the carbamate 8 was able to bind AChE by interacting with both CAS and PAS, in agreement with the mixed inhibition mechanism...
September 18, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29028480/revisiting-the-cholinergic-hypothesis-in-alzheimer-s-disease-emerging-evidence-from-translational-and-clinical-research
#6
Harald Hampel, Marsel M Mesulam, A Claudio Cuello, Ara S Khachaturian, Martin R Farlow, Peter J Snyder, Ezio Giacobini, Zaven S Khachaturian
Scientific evidence collected over the past four decades suggests that a loss of cholinergic innervation in the cerebral cortex of patients with Alzheimer's disease (AD) is an early pathogenic event correlated with cognitive impairment. This evidence led to the formulation of the "cholinergic hypothesis of AD" and the development of cholinesterase inhibitor therapies. Although approved only as symptomatic therapies, recent studies suggest that long-term use of these drugs may also have disease-modifying benefits...
October 10, 2017: Alzheimer's & Dementia: the Journal of the Alzheimer's Association
https://www.readbyqxmd.com/read/29023987/prevalence-of-delusions-in-drug-na%C3%A3-ve-alzheimer-disease-patients-a-meta-analysis
#7
Leo Lai, Philip E Lee, Peter Chan, Mark C Fok, Ging-Yuek R Hsiung, Amir A Sepehry
INTRODUCTION: Neuropsychiatric symptoms (NPS) are common at all stages of Alzheimer disease (AD). Delusions in AD are associated with negative clinical consequences and may signal rapid disease progression. Hence, we sought to determine the prevalence of delusions in drug-naïve (no cholinesterase inhibitor or neuroleptic medications) AD patients. METHODS: In this meta-analysis, a search of the EMBASE, MEDLINE, and PsycINFO databases was performed. We selected studies reporting delusion prevalence measured by the Neuropsychiatric Inventory (NPI) in drug-naïve AD patients...
October 11, 2017: International Journal of Geriatric Psychiatry
https://www.readbyqxmd.com/read/29023733/tonic-inhibition-of-brown-adipose-tissue-sympathetic-nerve-activity-via-muscarinic-acetylcholine-receptors-in-the-rostral-raphe-pallidus
#8
Ellen Paula Santos da Conceição, Christopher J Madden, Shaun F Morrison
We sought to determine if body temperature and energy expenditure are influenced by a cholinergic input to neurons in the rostral raphe pallidus (rRPa), the site of sympathetic premotor neurons controlling brown adipose tissue (BAT) thermogenesis. Nanoinjections of the muscarinic acetylcholine receptor (mAChR) receptor agonist, oxotremorine, or the cholinesterase inhibitor, neostigmine (NEOS), in the rRPa of anaesthetized rats decreased cold-evoked BAT sympathetic nerve activity (SNA, nadirs: -72%, and -95%), BAT temperature (TBAT, -0...
October 10, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28987876/synthesis-and-cholinesterase-inhibitory-activity-study-of-new-piperidone-grafted-spiropyrrolidines
#9
Alireza Basiri, Basma M Abd Razik, Mohammed Oday Ezzat, Yalda Kia, Raju Suresh Kumar, Abdulrahman I Almansour, Natarajan Arumugam, Vikneswaran Murugaiyah
Alzheimer's disease (AD) is a prevalent neurodegenerative disorder, which affected 35 million people in the world. The most practiced approach to improve the life expectancy of AD patients is to increase acetylcholine neurotransmitter level at cholinergic synapses by inhibition of cholinesterase enzymes. A series of unreported piperidone grafted spiropyrrolidines 8(a-p) were synthesized and evaluated in vitro for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities. Therein, compounds 8h and 8l displayed more potent AChE enzyme inhibition than standard drug with IC50 values of 1...
September 29, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28986116/9-substituted-acridine-derivatives-as-acetylcholinesterase-and-butyrylcholinesterase-inhibitors-possessing-antioxidant-activity-for-alzheimer-s-disease-treatment
#10
Galina F Makhaeva, Sofya V Lushchekina, Natalia P Boltneva, Olga G Serebryakova, Elena V Rudakova, Alexey A Ustyugov, Sergey O Bachurin, Alexander V Shchepochkin, Oleg N Chupakhin, Valery N Charushin, Rudy J Richardson
We investigated the inhibitory activity of 4 groups of novel acridine derivatives against acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and carboxylesterase (CaE) using the methods of enzyme kinetics and molecular docking. Antioxidant activity of the compounds was determined using the 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS(+)) radical decolorization assay as their ability to scavenge free radicals. Analysis of the esterase profiles and antiradical activities of the acridine derivatives showed that 9-aryl(heteroaryl)-N-methyl-9,10-dihydroacridines have a high radical-scavenging activity but low potency as AChE and BChE inhibitors, whereas 9-aryl(heteroaryl)-N-methyl-acridinium tetrafluoroborates effectively inhibit cholinesterases but do not exhibit antiradical activity...
September 20, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28973990/versatility-of-7-substituted-coumarin-molecules-as-antimycobacterial-agents-neuronal-enzyme-inhibitors-and-neuroprotective-agents
#11
Erika Kapp, Hanri Visser, Samantha L Sampson, Sarel F Malan, Elizabeth M Streicher, Germaine B Foka, Digby F Warner, Sylvester I Omoruyi, Adaze B Enogieru, Okobi E Ekpo, Frank T Zindo, Jacques Joubert
A medium-throughput screen using Mycobacterium tuberculosis H37Rv was employed to screen an in-house library of structurally diverse compounds for antimycobacterial activity. In this initial screen, eleven 7-substituted coumarin derivatives with confirmed monoamine oxidase-B and cholinesterase inhibitory activities, demonstrated growth inhibition of more than 50% at 50 µM. This prompted further exploration of all the 7-substituted coumarins in our library. Four compounds showed promising MIC99 values of 8...
September 30, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28966245/long-lasting-inhibitory-effects-of-distigmine-on-recombinant-human-acetylcholinesterase-activity
#12
Keisuke Obara, Daisuke Chino, Yoshio Tanaka
To elucidate the mechanism whereby distigmine, an underactive bladder remedy, potentiates urinary bladder contractions long-lastingly, the inhibition of recombinant human acetylcholinesterase (rhAChE) by distigmine was investigated. A centrifugal ultrafiltration device, Nanosep(®) 10K, was used to separate rhAChE and a bound inhibitor from an unbound inhibitor, reaction substrate, and reaction product. This allowed the same aliquot of rhAChE to be repeatedly assayed for up to 48 h to confirm the long-lasting binding of an inhibitor...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28955143/new-drug-research-and-development-for-alzheimer-s-pathology-present-and-prospect
#13
Tao Wang
Cholinesterase inhibitors and N-methyl-D-aspartic receptor antagonists are currently the main treatments for Alzheimer's disease (AD), targeting the clinical symptoms of AD. β-amyloid (Aβ) deposition and the highly-phosphorylated Tau protein-induced neurofibrillary tangles are some of the common pathological features of AD. In the past 20 years, many new drugs that focus on the pathogenesis of Alzheimer's disease have been assessed in clinical trials. Drugs such as β-amyloid monoclonal antibody and gamma-secretase inhibitor target the Aβ pathological pathway...
August 25, 2017: Shanghai Archives of Psychiatry
https://www.readbyqxmd.com/read/28946641/kinetics-and-molecular-docking-studies-of-6-formyl-umbelliferone-isolated-from-angelica-decursiva-as-an-inhibitor-of-cholinesterase-and-bace1
#14
Md Yousof Ali, Su Hui Seong, Machireddy Rajeshkumar Reddy, Sung Yong Seo, Jae Sue Choi, Hyun Ah Jung
Coumarins, which have low toxicity, are present in some natural foods, and are used in various herbal remedies, have attracted interest in recent years because of their potential medicinal properties. In this study, we report the isolation of two natural coumarins, namely umbelliferone (1) and 6-formyl umbelliferone (2), from Angelica decursiva, and the synthesis of 8-formyl umbelliferone (3) from 1. We investigated the anti-Alzheimer disease (anti-AD) potential of these coumarins by assessing their ability to inhibit acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1)...
September 24, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28944565/novel-tetrahydroacridine-derivatives-with-iodobenzoic-acid-moiety-as-multifunctional-acetylcholinesterase-inhibitors
#15
Robert Skibiński, Kamila Czarnecka, Małgorzata Girek, Ireneusz Bilichowski, Nina Chufarova, Elżbieta Mikiciuk-Olasik, Paweł Szymański
New synthesized series of 9-amino-1,2,3,4-tetrahydroacridine derivatives with iodobenzoic acid moiety were studied for their inhibitory activity towards cholinesterase and against β-amyloid aggregation. All novel molecules 3a-3i interacted with both cholinesterases - acetylcholinesterase and butyrylcholinesterase, delivered nanomolar IC50 values. The structure-activity relationship showed that N-butyl moiety derivatives are stronger inhibitors towards AChE and BuChE than N-ethyl and N-propyl moieties compounds...
September 25, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28936936/-treatment-of-dementia
#16
K Blom, G A H van den Elsen, H L Koek, J B Sanders, H C Kruithof, J A H R Claassen
- Treatment options for patients with dementia are limited. This article provides an overview of possible interventions, both pharmaceutical and non-pharmaceutical, for Alzheimer's disease, vascular dementia and mixed dementia.- Pharmaceutical treatment options include cholinesterase inhibitors, memantine and experimental medication. Cholinesterase inhibitors are only recommended for Alzheimer's disease and mixed dementia, not for vascular dementia or mild cognitive impairment. There is no proof of effectiveness for the other pharmaceutical options...
2017: Nederlands Tijdschrift Voor Geneeskunde
https://www.readbyqxmd.com/read/28929747/structure-of-an-insecticide-sequestering-carboxylesterase-from-the-disease-vector-culex-quinquefasciatus-what-makes-an-enzyme-a-good-insecticide-sponge
#17
Davis H Hopkins, Nicholas J Fraser, Peter D Mabbitt, Paul D Carr, John G Oakeshott, Colin J Jackson
Carboxylesterase (CBE)-mediated metabolic resistance to organophosphate and carbamate insecticides is a major problem for the control of insect disease vectors, such as the mosquito. The most common mechanism involves overexpression of CBEs that bind to the insecticide with high affinity, thereby sequestering them before they can interact with their target. However, the absence of any structure for an insecticide-sequestering CBE limits our understanding of the molecular basis for this process. We present the first structure of a CBE involved in sequestration, Cqestβ2(1), from the mosquito disease vector Culex quinquefasciatus...
October 17, 2017: Biochemistry
https://www.readbyqxmd.com/read/28925729/advances-toward-multifunctional-cholinesterase-and-%C3%AE-amyloid-aggregation-inhibitors
#18
Dawid Panek, Tomasz Wichur, Justyna Godyń, Anna Pasieka, Barbara Malawska
The emergence of a multitarget design approach in the development of new potential anti-Alzheimer's disease agents has resulted in the discovery of many multifunctional compounds focusing on various targets. Among them the largest group comprises inhibitors of both cholinesterases, with additional anti-β-amyloid aggregation activity. This review describes recent advances in this research area and presents the most interesting compounds reported over a 2-year span (2015-2016). The majority of hybrids possess heterodimeric structures obtained by linking structurally active fragments interacting with different targets...
September 19, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28922160/memantine-for-alzheimer-s-disease-an-updated-systematic-review-and-meta-analysis
#19
Taro Kishi, Shinji Matsunaga, Kazuto Oya, Ikuo Nomura, Toshikazu Ikuta, Nakao Iwata
BACKGROUND: The clinical benefit of memantine for Alzheimer's disease (AD) remains inconclusive. OBJECTIVE: We performed an updated systematic review and meta-analysis of the efficacy/safety of memantine in AD. METHODS: We included randomized trials of memantine for AD patients. Cognitive function scores (CF), behavioral disturbances scores (BD), and all-cause discontinuation were used as primary measures. Effect size based on a random-effects model was evaluated in the meta-analyses...
2017: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/28917965/the-development-of-a-butyrylcholinesterase-porous-pellet-for-innovative-detection-of-cholinesterase-inhibitors
#20
Jiří Zeman, David Vetchý, Aleš Franc, Sylvie Pavloková, Vladimír Pitschmann, Lukáš Matějovský
The aim of the presented research was the preparation of an innovative carrier with significantly improved properties for the fast and sensitive detection of cholinesterase inhibitors such as nerve agents. This innovative carrier was in the form of spherical pellets containing different amounts of Neusilin. Neusilin is a synthetic and amorphous form of magnesium aluminometasilicate with a high specific surface area, and the immobilized enzyme butyrylcholinesterase with an activity of 50nkat·g(-1). Pellets were prepared by the extrusion-spheronization method and dried in a hot air oven under two conditions - at 30°C for 72h and at 60°C for 24h...
September 13, 2017: European Journal of Pharmaceutical Sciences
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