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Donepezil

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https://www.readbyqxmd.com/read/28521305/bushen-yizhi-formula-ameliorates-cognitive-dysfunction-through-sirt1-er-stress-pathway-in-samp8-mice
#1
Shi-Jie Zhang, Ting-Ting Xu, Lin Li, Yu-Min Xu, Zi-Ling Qu, Xin-Chen Wang, Shui-Qing Huang, Yi Luo, Na-Chuan Luo, Ping Lu, Ya-Fei Shi, Xin Yang, Qi Wang
The Chinese formula Bushen-Yizhi (BSYZ) has been reported to ameliorate cognitive dysfunction. However the mechanism is still unclear. In this study, we employ an aging model, SAMP8 mice, to explore whether BSYZ could protect dementia through SIRT1/endoplasmic reticulum (ER) stress pathway. Morris water maze and the fearing condition test results show that oral administration of BSYZ (1.46 g/kg/d, 2.92 g/kg/d and 5.84 g/kg/d) and donepezil (3 mg/kg/d) shorten the escape latency, increase the crossing times of the original position of the platform and the time spent in the target quadrant, and increase the freezing time...
May 4, 2017: Oncotarget
https://www.readbyqxmd.com/read/28514890/spatial-recognition-test-a-novel-cognition-task-for-assessing-topographical-memory-in-mice
#2
Enes Havolli, Mark Dw Hill, Annie Godley, Pascal Jd Goetghebeur
Dysfunction in topographical memory is a core feature of several neurological disorders. There is a large unmet medical need to address learning and memory deficits as a whole in central nervous system disease. There are considerable efforts to identify pro-cognitive compounds but current methods are either lengthy or labour intensive. Our test used a two chamber apparatus and is based on the preference of rodents to explore novel environments. It was used firstly to assess topographical memory in mice at different retention intervals (RI) and secondly to investigate the effect of three drugs reported to be beneficial for cognitive decline associated with Alzheimer's disease, namely: donepezil, memantine and levetiracetam...
May 1, 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28499726/inhibitory-effect-of-donepezil-on-bradykinin-induced-increase-in-the-intracellular-calcium-concentration-in-cultured-cortical-astrocytes
#3
Kouki Makitani, Shota Nakagawa, Yasuhiko Izumi, Akinori Akaike, Toshiaki Kume
Donepezil is a potent and selective acetylcholinesterase inhibitor developed for the treatment of Alzheimer's disease. In the present study, we investigated the responses of astrocytes to bradykinin, an inflammatory mediator, and the effect of donepezil on these responses using cultured cortical astrocytes. Bradykinin induced a transient increase of intracellular calcium concentration ([Ca(2+)]i) in cultured astrocytes. Bradykinin-induced [Ca(2+)]i increase was inhibited by the exposure to thapsigargin, which depletes Ca(2+) stores on endoplasmic reticulum, but not by the exclusion of extracellular Ca(2+)...
April 24, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28495476/studies-on-diagnostic-biomarkers-and-therapeutic-mechanism-of-alzheimer-s-disease-through-metabolomics-and-hippocampal-proteomics
#4
Weiwei Lin, Jianmei Zhang, Yanmeng Liu, Ruijun Wu, Haisong Yang, Xiaobo Hu, Xiaomei Ling
Alzheimer's disease (AD) is the main cause of dementia, but precise diagnosis and treatment are not sufficient so far. The purpose of this study is to develop biomarkers and therapeutic targets for diagnosis and better understanding of AD. As a result, lysophosphatidylcholine and intermediates of sphingolipid metabolism including sphinganine-1-phosphate, sphingosine-1-phosphate, sphingomyelin, and sphingosine in plasma were annotated as potential biomarkers by using UPLC-Q-TOF-MS and UHPLC-Q-Exactive-MS. Besides, glutathione S-transferases (GSTs) including GstA3, Gstm1, Gstm5, Gstm3, Gstk1 and Gstp1 were significantly enhanced in AD hippocampus by using label free nano-LC-MS/MS...
May 8, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28487125/design-synthesis-and-biological-evaluation-of-3-4-dihydro-2-1h-quinoline-o-alkylamine-derivatives-as-new-multipotent-cholinesterase-monoamine-oxidase-inhibitors-for-the-treatment-of-alzheimer-s-disease
#5
Zhipei Sang, Wanli Pan, Keren Wang, Qinge Ma, Lintao Yu, Wenmin Liu
A new family of multitarget molecules able to interact with acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), as well as with monoamino oxidase (MAO) A and B, has been synthesized. Novel 3,4-dihydro-2(1H)-quinoline-O-alkylamine derivatives have been designed using a conjunctive approach that combines the JMC49 and donepezil. The most promising compound TM-33 showed potent and balance inhibitory activities toward ChE and MAO (eeAChE, eqBuChE, hMAO-A and hMAO-B with IC50 values of 0.56μM, 2.3μM, 0...
April 6, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28458525/rivastigmine-the-advantages-of-dual-inhibition-of-acetylcholinesterase-and-butyrylcholinesterase-and-its-role-in-subcortical-vascular-dementia-and-parkinson-s-disease-dementia
#6
REVIEW
Nagaendran Kandiah, Ming-Chyi Pai, Vorapun Senanarong, Irene Looi, Encarnita Ampil, Kyung Won Park, Ananda Krishna Karanam, Stephen Christopher
Several studies have demonstrated clinical benefits of sustained cholinesterase inhibition with rivastigmine in Alzheimer's disease (AD) and Parkinson's disease dementia (PDD). Unlike donepezil and galantamine that selectively inhibit acetylcholinesterase (AChE; EC 3.1.1.7), rivastigmine is a unique cholinesterase inhibitor with both AChE and butyrylcholinesterase (BuChE; EC 3.1.1.8) inhibitory activity. Rivastigmine is also available as transdermal patch that has been approved by the US Food and Drug Administration for the treatment of mild, moderate, and severe AD as well as mild-to-moderate PDD...
2017: Clinical Interventions in Aging
https://www.readbyqxmd.com/read/28458424/evaluation-of-neuroprotective-effect-of-quercetin-with-donepezil-in-scopolamine-induced-amnesia-in-rats
#7
Laxmi Adiveppa Pattanashetti, Ashok D Taranalli, Vinay Parvatrao, Rohit H Malabade, Dushyant Kumar
OBJECTIVE: The objective of this study was to evaluate the neuroprotective effect of quercetin with donepezil in scopolamine-induced amnesia in rats. MATERIALS AND METHODS: Five groups of adult male Wistar rats (12 months old) weighing 180-200 g (n = 6) were used. The normal control group received normal saline and test group animals were pretreated orally with quercetin (25 mg/kg), donepezil (3 mg/kg), and a combination of quercetin (25 mg/kg) with donepezil (3 mg/kg), respectively, dosed at every 24 h interval for 14 consecutive days, afterward amnesia was induced by scopolamine (3 mg/kg) on the 14(th) day through intraperitoneal route...
January 2017: Indian Journal of Pharmacology
https://www.readbyqxmd.com/read/28454848/design-synthesis-and-evaluation-of-multitarget-directed-ligands-against-alzheimer-s-disease-based-on-the-fusion-of-donepezil-and-curcumin
#8
Jun Yan, Jinhui Hu, Anqiu Liu, Lin He, Xingshu Li, Hui Wei
By fusing donepezil and curcumin, a novel series of compounds were obtained as multitarget-directed ligands against Alzheimer's disease. Among them, compound 11b displayed potent acetylcholinesterase (AChE) inhibition (IC50=187nM) and the highest BuChE/AChE selectivity (66.3). Compound 11b also inhibited 45.3% Aβ1-42 self-aggregation at 20μM and displayed remarkable antioxidant effects. The metal-chelating property of compound 11b was elucidated by determining the 1:1 stoichiometry for the 11b-Cu(II) complex...
April 18, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28442406/anti-amnesic-effect-of-extract-and-alkaloid-fraction-from-aerial-parts-of-peganum-harmala-on-scopolamine-induced-memory-deficits-in-mice
#9
Wei Liu, Yudan Zhu, Yongli Wang, Shenglan Qi, Yuwen Wang, Chao Ma, Shuping Li, Bo Jiang, Xuemei Cheng, Zhengtao Wang, Zhenyu Xuan, Changhong Wang
ETHNOPHARMACOLOGICAL RELEVANCE: Aerial parts of Peganum harmala Linn (APP) is used as traditional medical herb for treatment of forgetfulness in Uighur medicine in China. But, the active ingredients and underlying mechanisms are unclear. AIM OF THE STUDY: The present study was undertaken to investigate the improvement effects of extract and alkaloid fraction from APP on scopolamine-induced cognitive dysfunction and to elucidate their underlying mechanisms of action, and to support its folk use with scientific evidence, and lay a foundation for its further researches...
April 22, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28427041/the-efficacy-of-donepezil-administration-on-acetylcholinesterase-activity-and-altered-redox-homeostasis-in-alzheimer-s-disease
#10
Pinar Atukeren, Mahir Cengiz, Hakan Yavuzer, Remise Gelisgen, Esma Altunoglu, Sena Oner, Fusun Erdenen, Damla Yuceakın, Himmet Derici, Ufuk Cakatay, Hafize Uzun
Alzheimer's disease (AD) is a serious multifactorial disorder with progressive neurodegenerative outcomes related with impaired redox homeostasis. Inhibition of the enzyme acetylcholinesterase (AChE), as one of the major therapeutic strategies, is considered to be offering only symptomatic relief and moderate disease modifying effect. We intended to investigate the effects of acetylcholinesterase inhibition via donepezil on protein carbonyl (PCO), advanced protein oxidation products (AOPP) and ischemia modified albumin (IMA) as protein oxidation markers and ferric reducing antioxidant power (FRAP), prooxidant-antioxidant balance (PAB), total thiol (T-SH), protein thiol (P-SH) as antioxidant status markers and also kynurenine (KYN), N-formyl kynurenine (N-FKYN) and protein bound dityrosine (DT) levels all in one demonstrating the redox homeostasis in Alzheimer patients also correlated with AChE activity...
June 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28421986/all-solid-state-pvc-membrane-and-carbon-paste-ion-selective-electrodes-for-determination-of-donepezil-hydrochloride-in-pharmaceutical-formulation
#11
Nesreen Khamees, Tagreed Abdel-Fattah Mohamed, Abeer Rashad Derar, Azza Aziz
All-solid-state, polyvinyl chloride (PVC) membrane, and carbon paste potentiometric ion-selective electrodes (ISEs) were proposed for the determination of donepezil hydrochloride (DON) in the drug substance and a pharmaceutical formulation. The potentiometric response toward DON was based on the existence of donepezil-tetraphenyl borate (DON-TPB) in a PVC membrane or a carbon paste in the presence of dioctylphthalate. In contrast, the solid-state electrode was prepared by direct incorporation of DON-TPB into a commercial nail varnish without external additives...
April 18, 2017: Journal of AOAC International
https://www.readbyqxmd.com/read/28417590/calcitonin-gene-related-peptide-cgrp-a-novel-target-for-alzheimer-s-disease
#12
REVIEW
Yogendra Singh, Gaurav Gupta, Birendra Shrivastava, Rajiv Dahiya, Juhi Tiwari, Madhu Ashwathanarayana, Rakesh Kumar Sharma, Mohit Agrawal, Anurag Mishra, Kamal Dua
Alzheimer's disease (AD) is leading cause of death among older characterized by neurofibrillary tangles, oxidative stress, progressive neuronal deficits, and increased levels of amyloid-β (Aβ) peptides. Cholinergic treatment could be the best suitable physiological therapy for AD. Calcitonin gene-related peptide (CGRP) is a thirty-seven-amino acid regulatory neuropeptide resulting from different merging of the CGRP gene, which also includes adrenomedullin, amylin, calcitonin, intermedin, and calcitonin receptor-stimulating peptide...
April 17, 2017: CNS Neuroscience & Therapeutics
https://www.readbyqxmd.com/read/28411132/methyl-jasmonate-attenuates-memory-dysfunction-and-decreases-brain-levels-of-biomarkers-of-neuroinflammation-induced-by-lipopolysaccharide-in-mice
#13
Umukoro Solomon, Eduviere Anthony Taghogho
Neuroinflammation plays a central role in the etiology and progression of Alzheimer's disease (AD), a neurodegenerative disorder, characterized by a gradual loss of memory functions. Thus, it has been proposed that agents that could reduce inflammatory processes in AD brains might be useful for the treatment of the disease. Methyl jasmonate (MJ) is a bioactive compound, which has been reported to exhibit anti-amnesic and in vitro anti-inflammatory activities. In this study, we further examine its effects on the brain levels of biomarkers of neuroinflammation in lipopolysaccharide (LPS)-induced memory deficits in mice...
April 12, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/28403780/synthesis-of-novel-benzothiazole-piperazine-derivatives-and-their-biological-evaluation-as-acetylcholinesterase-inhibitors-and-cytotoxic-agents
#14
Enise Ece Gurdal, Bengisu Turgutalp, Hayrettin Ozan Gulcan, Tugba Erçetin, Mustafa Fethi Sahin, Irem Durmaz, Rengul Cetin Atalay, Quoc Dat Nguyen, Wolfgang Sippl, Mine Yarim
A new series of benzothiazole-piperazine derivatives were synthesized and a complete chemical characterization of the novel compounds was provided. In vitro cytotoxic activities were screened against colorectal (HCT-116), breast (MCF-7) and hepatocellular (Huh7) cancer cell lines by Sulforhodamine B assay. All compounds showed cytotoxic activity against hepatocellular (Huh7) and breast (MCF-7) cancer cell lines. Dihalo substituted benzylpiperazine derivatives (2a, 2e) had the highest cytotoxic activities in all tested cell lines...
April 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28402165/statistical-properties-of-continuous-composite-scales-and-implications-for-drug-development
#15
Hong Liu-Seifert, Scott Andersen, Michael Case, JonDavid Sparks, Karen C Holdridge, Alette M Wessels, Suzanne Hendrix, Paul Aisen, Eric Siemers
Little research has been conducted on the statistical properties of composite measures comprising linear combinations of continuous component scales. We assessed the quantitative relationship between the composites and their individual components regarding their abilities to detect treatment effects. In particular, we developed the mathematical derivation of the treatment effect size of a continuous composite in relation to the treatment effect sizes of its components and proved multiple properties of the composite...
April 12, 2017: Journal of Biopharmaceutical Statistics
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
#16
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
#17
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/28381516/randomized-controlled-trials-in-mild-cognitive-impairment-sources-of-variability
#18
Ronald C Petersen, Ronald G Thomas, Paul S Aisen, Richard C Mohs, Maria C Carrillo, Marilyn S Albert
OBJECTIVE: To examine the variability in performance among placebo groups in randomized controlled trials for mild cognitive impairment (MCI). METHODS: Placebo group data were obtained from 2 National Institute on Aging (NIA) MCI randomized controlled trials, the Alzheimer's Disease Cooperative Study (ADCS) MCI trial and the Alzheimer's Disease Neuroimaging Initiative (ADNI), which is a simulated clinical trial, in addition to industry-sponsored clinical trials involving rivastigmine, galantamine, rofecoxib, and donepezil...
May 2, 2017: Neurology
https://www.readbyqxmd.com/read/28378260/effect-of-metformin-on-adult-hippocampal-neurogenesis-comparison-with-donepezil-and-links-to-cognition
#19
Sara Ahmed, Zahra Mahmood, Aneela Javed, Shoaib Naiyer Hashmi, Inga Zerr, Saima Zafar, Saadia Zahid
Recent studies have uncovered evidence suggesting that interference with hippocampal adult neurogenesis contributes to neurodegeneration in Alzheimer's disease (AD). Evidence supporting that AD is a metabolic disease with derangements in brain glucose utilization implies the use of anti-diabetics as an alternate therapeutic strategy. The present study drew comparison between the pro-neurogenic potential of metformin and donepezil in AlCl3-induced mouse model of neurodegeneration. Morris water maze task and subsequent immunohistochemical evaluation for NeuN was conducted...
April 4, 2017: Journal of Molecular Neuroscience: MN
https://www.readbyqxmd.com/read/28377707/cholinergic-potentiation-improves-perceptual-cognitive-training-of-healthy-young-adults-in-three-dimensional-multiple-object-tracking
#20
Mira Chamoun, Frédéric Huppé-Gourgues, Isabelle Legault, Pedro Rosa-Neto, Daniela Dumbrava, Jocelyn Faubert, Elvire Vaucher
A large body of literature supports cognitive enhancement as an effect of cholinergic potentiation. However, it remains elusive whether pharmacological manipulations of cholinergic neurotransmission enhance complex visual processing in healthy individuals. To test this hypothesis, we randomly administered either the cholinergic transmission enhancer donepezil (DPZ; 5 mg P.O.) or placebo (lactose) to young adults (n = 17) 3 h before each session of the three-dimensional (3D) multiple object tracking (3D-MOT) task...
2017: Frontiers in Human Neuroscience
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