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https://www.readbyqxmd.com/read/29447949/protective-effects-of-alpinae-oxyphyllae-fructus-extracts-on-lipopolysaccharide-induced-animal-model-of-alzheimer-s-disease
#1
Yunlong Wang, Mengshi Wang, Kaiyue Fan, Tongde Li, Tingxu Yan, Bo Wu, Kaishun Bi, Ying Jia
ETHNOPHARMACOLOGICAL RELEVANCE: Alpinae Oxyphyllae Fructus (AOF) with warming and tonifying the kidney and spleen, anti-salivation, anti-polyuria and anti-diarrhea functions is the dried ripe fruits of Alpinia oxyphylla Miq. (Zingiberaceae). As a traditional Chinese medicine, its application history is very long. AIMS OF THE STUDY: The purpose of our study is to investigate the effects of different solvent extracts from AOF on lipopolysaccharide (LPS)-induced animal model of Alzheimer's disease (AD) to elucidate the traditional medical theories with modern pharmacological methods and provide a reference for further clarifying its active components and mechanisms...
February 12, 2018: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29439368/systemic-administration-of-donepezil-attenuates-the-efficacy-of-environmental-enrichment-on-neurobehavioral-outcome-after-experimental-traumatic-brain-injury
#2
Corina O Bondi, Narayana K Yelleswarapu, Julian Day-Cooney, Kimiya Memarzadeh, Kaitlin A Folweiler, Carine E Bou-Abboud, Jacob B Leary, Jeffrey P Cheng, Roya Tehranian-DePasquale, Anthony E Kline
BACKGROUND: The acetylcholinesterase inhibitor (AChEI) donepezil (DON) is recommended as a potential treatment for cognition after clinical traumatic brain injury (TBI) and therefore may be prescribed as an adjunct therapy during rehabilitation. However, a dose-response study evaluating DON after a controlled cortical impact (CCI) injury in rats did not reveal cognitive benefits. OBJECTIVE: The aim of this study was to determine the effect of DON on behavioral and histological outcome when combined with environmental enrichment (EE), a preclinical model of neurorehabilitation...
2018: Restorative Neurology and Neuroscience
https://www.readbyqxmd.com/read/29439327/stabilized-low-n-amyloid-%C3%AE-oligomers-induce-robust-novel-object-recognition-deficits-associated-with-inflammatory-synaptic-and-gabaergic-dysfunction-in-the-rat
#3
William Watremez, Joshua Jackson, Bushra Almari, Samantha L McLean, Ben Grayson, Joanna C Neill, Nicolas Fischer, Ahmad Allouche, Violette Koziel, Thierry Pillot, Michael K Harte
BACKGROUND: With current treatments for Alzheimer's disease (AD) only providing temporary symptomatic benefits, disease modifying drugs are urgently required. This approach relies on improved understanding of the early pathophysiology of AD. A new hypothesis has emerged, in which early memory loss is considered a synapse failure caused by soluble amyloid-β oligomers (Aβo). These small soluble Aβo, which precede the formation of larger fibrillar assemblies, may be the main cause of early AD pathologies...
2018: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/29434777/effects-of-donepezil-on-cognitive-functions-and-the-expression-level-of-%C3%AE-amyloid-in-peripheral-blood-of-patients-with-alzheimer-s-disease
#4
Yunxia Ma, Jinming Ji, Gang Li, Shuzhen Yang, Shuangshuang Pan
Alzheimer's disease is a degenerative disease affecting the central nervous system for which donepezil is usually prescribed. The aim of the present study was to examine the effects of donepezil on the cognitive functions and expression levels of β-amyloid (Aβ) in the peripheral blood of patients with Alzheimer's disease. In total, 76 patients with cognitive impairment, who visited the Department of Neurology of Binzhou City Center Hospital from June 2015 to September 2016, had memory decline for more than three consecutive months and underwent mini-mental state examination (MMSE) score screening, were selected for the study...
February 2018: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/29427354/simple-determination-of-some-anti-dementia-drugs-in-wastewater-and-human-plasma-samples-by-tandem-dispersive-liquid-liquid-microextraction-followed-by-hplc
#5
Ehsan Mirparizi, Maryam Rajabi, Alireza Asghari
In this work, a simple method, namely, tandem dispersive liquid-liquid microextraction, with a high sample clean-up is applied for the rapid determination of the anti-dementia drugs rivastigmine and donepezil in wastewater and human plasma samples. This method, which is based upon two consecutive dispersive microextractions, is performed in 7 min. In the method, using a fast back-extraction step, the applicability of the dispersive microextraction methods in complicated matrixes is conveniently improved. This step can be performed in less than 2 min, and very simple tools are required for this purpose...
February 10, 2018: Journal of Separation Science
https://www.readbyqxmd.com/read/29421570/design-synthesis-and-pharmacological-evaluation-of-n-benzyl-piperidinyl-aryl-acylhydrazone-derivatives-as-donepezil-hybrids-discovery-of-novel-multi-target-anti-alzheimer-prototype-drug-candidates
#6
Flávia Pereira Dias Viegas, Matheus de Freitas Silva, Miguel Divino da Rocha, Maísa Rosa Castelli, Mariana Máximo Riquiel, Rafael Pereira Machado, Sarah Macedo Vaz, Laís Medeiros Simões de Lima, Karla Cristine Mancini, Patrícia Cruz Marques de Oliveira, Élida Parreira Morais, Vanessa Silva Gontijo, Fernanda Motta R da Silva, Dora D'Alincourt da Fonseca Peçanha, Newton Gonçalves Castro, Gilda A Neves, Alexandre Giusti-Paiva, Fabiana Cardoso Vilela, Lidiane Orlandi, Ihosvany Camps, Márcia Paranho Veloso, Luis Felipe Leomil Coelho, Marisa Ionta, Guilherme Álvaro Ferreira-Silva, Rodrigo Machado Pereira, Laurent E Dardenne, Isabella Alvim Guedes, Wellerson de Oliveira Carneiro Junior, Paula Maria Quaglio Bellozi, Antônio Carlos Pinheiro de Oliveira, Fábio Furlan Ferreira, Letizia Pruccoli, Andrea Tarozzi, Claudio Viegas
A new series of sixteen multifunctional N-benzyl-piperidine-aryl-acylhydrazones hybrid derivatives was synthesized and evaluated for multi-target activities related to Alzheimer's disease (AD). The molecular hybridization approach was based on the combination, in a single molecule, of the pharmacophoric N-benzyl-piperidine subunit of donepezil, the substituted hydroxy-piperidine fragment of the AChE inhibitor LASSBio-767, and an acylhydrazone linker, a privileged structure present in a number of synthetic aryl- and aryl-acylhydrazone derivatives with significant AChE and anti-inflammatory activities...
January 31, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29420357/acetyl-cholinesterase-inhibitors-and-cell-derived-peripheral-inflammatory-cytokines-in-early-stages-of-alzheimer-s-disease
#7
Nikolaos Kokras, Evangelia Stamouli, Ioannis Sotiropoulos, Everina A Katirtzoglou, Kostas T Siarkos, Georgia Dalagiorgou, Krystallenia I Alexandraki, Stavroula Coulocheri, Christina Piperi, Antonios M Politis
BACKGROUND: Clinical and preclinical studies firmly support the involvement of the inflammation in the pathogenesis of Alzheimer's disease (AD). Despite acetylcholinesterase inhibitors (AChEI) being widely used in AD patients, there is no conclusive evidence about their impact on the inflammatory response. METHODS: This study investigates peripheral proinflammatory cytokines (interferon gamma [IFN-γ], tumor necrosis factor alpha [TNF-α], and interleukins 1β [IL-1β] and 6 [IL-6]) by firstly comparing peripheral blood mononuclear cell (PBMC)-derived secretion in drug-naïve and AChEI-treated AD patients versus healthy controls...
February 7, 2018: Journal of Clinical Psychopharmacology
https://www.readbyqxmd.com/read/29413486/oleocanthal-rich-extra-virgin-olive-oil-enhances-donepezil-effect-by-reducing-amyloid-%C3%AE-load-and-related-toxicity-in-a-mouse-model-of-alzheimer-s-disease
#8
Yazan S Batarseh, Amal Kaddoumi
Previous evidence suggested that extra-virgin olive oil (EVOO) is linked to attenuating amyloid-β (Aβ) pathology and improving cognitive function in Alzheimer's disease (AD) mouse models. In addition, we recently reported the beneficial effect of oleocanthal, a phenolic compound in EVOO, against AD pathology. Currently, medications available to target AD pathology are limited. Donepezil is an acetylcholine esterase inhibitor approved for use for all AD stages. Donepezil has been reported to have limited Aβ-targeting mechanisms beside its acetylcholine esterase inhibition...
December 27, 2017: Journal of Nutritional Biochemistry
https://www.readbyqxmd.com/read/29406017/examining-the-effectiveness-of-acetylcholinesterase-inhibitors-and-stimulant-based-medications-for-cognitive-dysfunction-in-multiple-sclerosis-a-systematic-review-and-meta-analysis
#9
REVIEW
Jack Cotter, Nils Muhlert, Anahita Talwar, Kiri Granger
We sought to examine the effectiveness of acetylcholinesterase inhibitors (AChEIs) and stimulant-based medications for improving cognitive performance in patients with multiple sclerosis (MS). An electronic database search was conducted on 25th March 2017. Eligible studies were double-blind, randomised, placebo-controlled trials that examined the efficacy of compounds that act primarily as AChEIs or stimulants (administered daily for ≥1 week) on cognitive outcome measures in patients with MS. Where suitable data was reported, we generated effect sizes and corresponding 95% confidence intervals and performed meta-analyses using random-effects models to investigate the effectiveness of these drug types across cognitive domains...
March 2018: Neuroscience and Biobehavioral Reviews
https://www.readbyqxmd.com/read/29358550/amalaki-rasayana-improved-memory-and-neuronal-metabolic-activity-in-abpp-ps1-mouse-model-of-alzheimer-s-disease
#10
Vivek Tiwari, Kamal Saba, Pandichelvam Veeraiah, Jedy Jose, Subhash C Lakhotia, Anant B Patel
Alzheimer's disease (AD) is the most common neurodegenerative disorder characterized by progressive loss of memory and cognitive function. The cerebral metabolic rate of glucose oxidation has been shown to be reduced in AD. The present study evaluated efficacy of dietary Amalaki Rasayana (AR), an Ayurvedic formulation used in Indian traditional system, in AbPP-PS1 mouse model of AD in ameliorating memory and neurometabolism, and compared with donepezil, a standard FDA approved drug for AD. The memory of mice was measured using Morris Water Maze analysis...
September 2017: Journal of Biosciences
https://www.readbyqxmd.com/read/29350336/brain-over-bladder-a-systematic-review-of-dual-cholinesterase-inhibitor-and-urinary-anticholinergic-use
#11
REVIEW
Laura K Triantafylidis, Jenna S Clemons, Emily P Peron, John Roefaro, Kristin M Zimmerman
BACKGROUND: Case reports have demonstrated that dual use of cholinesterase inhibitors (ChIs) and urinary anticholinergics (UAChs) in older adults may be associated with delusions, aggression, changes in cognition, and anxiety, which typically resolve on drug discontinuation. Despite opposing mechanisms of action, these drugs continue to be co-prescribed. OBJECTIVE: This systematic review evaluates cognitive and functional outcomes of dual use of ChIs and UAChs and describes its prevalence...
January 19, 2018: Drugs & Aging
https://www.readbyqxmd.com/read/29336496/donepezil-reverses-dendritic-spine-morphology-adaptations-and-fmr1-epigenetic-modifications-in-hippocampus-of-adult-rats-after-adolescent-alcohol-exposure
#12
Patrick J Mulholland, Tara L Teppen, Kelsey M Miller, Hannah G Sexton, Subhash C Pandey, H Scott Swartzwelder
BACKGROUND: Adolescent intermittent ethanol (AIE) exposure produces persistent impairments in cholinergic and epigenetic signaling and alters markers of synapses in the hippocampal formation, effects that are thought to drive hippocampal dysfunction in adult rodents. Donepezil (Aricept), a cholinesterase inhibitor, is used clinically to ameliorate memory-related cognitive deficits. Given that donepezil also prevents morphological impairment in preclinical models of neuropsychiatric disorders, we investigated the ability of donepezil to reverse morphological and epigenetic adaptations in the hippocampus of adult rats exposed to AIE...
January 16, 2018: Alcoholism, Clinical and Experimental Research
https://www.readbyqxmd.com/read/29335209/chameleon-like-behavior-of-indolylpiperidines-in-complex-with-cholinesterases-targets-potent-butyrylcholinesterase-inhibitors
#13
Talita P C Chierrito, Susimaire Pedersoli-Mantoani, Carlos Roca, Victor Sebastian-Pérez, Loreto Martínez-Gonzalez, Daniel I Pérez, Concepción Perez, Angeles Canales, F Javier Cañada, Nuria E Campillo, Ivone Carvalho, Ana Martinez
Alzheimer's disease (AD) is the most common form of dementia worldwide with an increasing prevalence for the next years. The multifactorial nature of AD precludes the design of new drugs directed to a single target being probably one of the reasons for recent failures. Therefore, dual binding site acetylcholinesterase (AChE) inhibitors have been revealed as cognitive enhancers and β-amyloid modulators offering an alternative in AD therapy field. Based on the dual ligands NP61 and donepezil, the present study reports the synthesis of a series of indolylpiperidines hybrids to optimize the NP61 structure preserving the indole nucleus, but replacing the tacrine moiety of NP61 by benzyl piperidine core found in donepezil...
January 5, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29334662/aqueous-extracts-of-two-tropical-ethnobotanicals-tetrapleura-tetraptera-and-quassia-undulata-improved-spatial-and-non-spatial-working-memories-in-scopolamine-induced-amnesic-rats-influence-of-neuronal-cholinergic-and-antioxidant-systems
#14
Veronica O Odubanjo, Emmanuel O Ibukun, Ganiyu Oboh, Stephen A Adefegha
BACKGROUND: Tetrapleura tetraptera (TT) and Quassia undulata (QU) are two predominant tropical ethnobotanicals with various medicinal values but are commonly used in folklore for the treatment of mental illness without justifiable mechanisms of action. AIM OF THE STUDY: To investigate the effects of aqueous extracts from TT fruits and QU leaves on the spatial and non-spatial working memory, antioxidant status and activities of neuronal marker enzymes of scopolamine-induced amnesic rats and thus, understand the possible mechanism of action of these plants...
January 11, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29332255/profiling-attention-and-cognition-enhancing-drugs-in-a-rat-touchscreen-based-continuous-performance-test
#15
Zhiyong Ding, Jordan W Brown, Lynne E Rueter, Eric G Mohler
RATIONALE: A novel rodent continuous performance test (CPT) was developed as one of the goals of the NEWMEDS (Novel Methods leading to New Medications in Depression and Schizophrenia) consortium to improve its translatability to the CPT test used in human subjects. OBJECTIVES: The objective of the study is to investigate the effects of attention and cognition enhancing drugs in rodent CPT. METHODS: A single cohort of rats were trained to asymptotic performance in the test...
January 13, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29324339/novel-donepezil-like-n-benzylpyridinium-salt-derivatives-as-ache-inhibitors-and-their-corresponding-dihydropyridine-bio-oxidizable-prodrugs-synthesis-biological-evaluation-and-structure-activity-relationship
#16
Rabah Azzouz, Ludovic Peauger, Vincent Gembus, Mihaela-Liliana Ţînţaş, Jana Sopková-de Oliveira Santos, Cyril Papamicaël, Vincent Levacher
As an extension of our previous work on donepezil-based "bio-oxidizable" prodrug approach, two new classes of N-benzylpyridinium donepezil analogues in tetralone B2 and acetophenone B3 series and a new set of indanone derivatives B1 were investigated along with the corresponding dihydropyridine prodrugs A1-3. A total of fifty one N-benzylpyridinium quaternary donepezil analogues B1-3 and twenty two prodrugs A1-3 were synthesized and evaluated for their inhibitory activities against hAChE and eqBuChE. While most prodrugs A1-3 were demonstrated to be inactive against AChE (IC50 > 10 μM), a large number of the corresponding N-benzylpyridinium salt B1-3 exhibited appealing three-to-one-digit nanomolar hAChE inhibitory activities and even reaching subnanomolar activity (IC50 = 0...
December 27, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29319499/similar-treatment-outcomes-with-ginkgo-biloba-extract-egb-761-and-donepezil-in-alzheimer-s-dementia-in-very-old-age-a-retrospective-observational-study
#17
Michael Rapp, Martin Burkart, Thomas Kohlmann, Jens Bohlken
OBJECTIVE: To provide pilot data for the safety and efficacy of EGb 761 in the oldest-old patients (aged 80 or older). MATERIALS AND METHODS: In a retrospective analysis, we compared treatment outcomes with EGb 761 or donepezil over 12 months in 189 patients aged 80 years or older suffering from Alzheimer's disease (AD). RESULTS: Over 12 months, there was no significant difference in cognitive decline, measured with the mini-mental state examination (MMSE) score, between donepezil and EGb 761 (p = 0...
January 10, 2018: International Journal of Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29318278/effect-of-idalopirdine-as-adjunct-to-cholinesterase-inhibitors-on-change-in-cognition-in-patients-with-alzheimer-disease-three-randomized-clinical-trials
#18
RANDOMIZED CONTROLLED TRIAL
Alireza Atri, Lutz Frölich, Clive Ballard, Pierre N Tariot, José Luis Molinuevo, Neli Boneva, Kristian Windfeld, Lars L Raket, Jeffrey L Cummings
Importance: New therapeutic approaches for Alzheimer disease (AD) are needed. Objective: To assess whether idalopirdine, a selective 5-hydroxytryptamine-6 receptor antagonist, is effective for symptomatic treatment of mild to moderate AD. Design, Setting, and Participants: Three randomized clinical trials that included 2525 patients aged 50 years or older with mild to moderate AD (study 1: n = 933 patients at 119 sites; study 2: n = 858 at 158 sites; and study 3: n = 734 at 126 sites)...
January 9, 2018: JAMA: the Journal of the American Medical Association
https://www.readbyqxmd.com/read/29315246/recent-advances-in-electrochemical-biosensors-based-on-enzyme-inhibition-for-clinical-and-pharmaceutical-applications
#19
REVIEW
Loubna El Harrad, Ilhame Bourais, Hasna Mohammadi, Aziz Amine
A large number of enzyme inhibitors are used as drugs to treat several diseases such as gout, diabetes, AIDS, depression, Parkinson's and Alzheimer's diseases. Electrochemical biosensors based on enzyme inhibition are useful devices for an easy, fast and environment friendly monitoring of inhibitors like drugs. In the last decades, electrochemical biosensors have shown great potentials in the detection of different drugs like neostigmine, ketoconazole, donepezil, allopurinol and many others. They attracted increasing attention due to the advantage of being high sensitive and accurate analytical tools, able to reach low detection limits and the possibility to be performed on real samples...
January 9, 2018: Sensors
https://www.readbyqxmd.com/read/29299992/development-of-a-nasal-donepezil-loaded-microemulsion-for-treatment-of-alzheimer-s-disease-in-vitro-and-ex-vivo-characterization
#20
Lupe Carolina Espinoza, Marisol Vacacela, Beatriz Clares, Maria Luisa Garcia, Maria Jose Fabrega, Ana Cristina Calpena
BACKGROUND: Donepezil (DPZ) is widely prescribed as a specific and reversible acetylcholinesterase inhibitor for the symptomatic treatment of mild to moderate Alzheimer's disease (AD). OBJECTIVE: Considering the therapeutic potential of DPZ and the advantages offered by the intranasal route as an alternative for drug administration, the aim of this study was the development and characterization of a DPZ microemulsion (ME) for nose-to-brain delivery. METHOD: The ME was developed by construction of pseudoternary phase diagrams and characterized by dynamic light scattering and transmission electron microscopy...
January 4, 2018: CNS & Neurological Disorders Drug Targets
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