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https://www.readbyqxmd.com/read/29665389/application-of-pectin%C3%A2-zinc-oxide-hybrid-nanocomposite-in-the-delivery-of-a-hydrophilic-drug-and-a-study-of-its-isotherm-kinetics-and-release-mechanism
#1
Arun K Kodoth, Vivek M Ghate, Shaila A Lewis, B Vishalakshi
Pectin-based gel and its nanocomposite with zinc oxide have been compared for their capacity to release Donepezil for the possible use as an implantable drug delivery platform for the treatment of Alzheimer's disease. Adsorption capacities of the samples were determined as a function of pH, temperatures, concentrations of the drug, and the mass of the adsorbent. The nanocomposite exhibited significant adsorption compared to the parent gel. Adsorption data for the nanocomposite system fits well with Langmuir model and followed pseudo-first order kinetics, while that of the parent polymeric system followed pseudo-second-order kinetics...
April 14, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29663860/novel-coumarin-derivatives-as-potent-acetylcholinesterase-inhibitors-insight-into-efficacy-mode-and-site-of-inhibition
#2
Prayasee Baruah, Grace Basumatary, Semen O Yesylevskyy, Kripamoy Aguan, Ghanashyam Bez, Sivaprasad Mitra
The inhibitory efficacy of two substituted coumarin derivatives on the activity of neurodegenerative enzyme acetylcholinesterase (AChE) was assessed in aqueous buffer as well as in the presence of human serum albumin (HSA) and compared against standard cholinergic AD drug, Donepezil (DON). The experimental data revealed the inhibition to be of non-competitive type with both the systems showing substantial inhibitory activity on AChE. In fact, one of the tested compounds Chromenyl Coumarate (CC) was found to be better inhibitor (IC50 = 48...
April 17, 2018: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/29651884/kinetic-and-structural-studies-on-the-interactions-of-torpedo-californica-acetylcholinesterase-with-two-donepezil-like-rigid-analogues
#3
Rosanna Caliandro, Alessandro Pesaresi, Luca Cariati, Antonio Procopio, Manuela Oliverio, Doriano Lamba
Acetylcholinesterase inhibitors were introduced for the symptomatic treatment of Alzheimer's disease (AD). Among the currently approved inhibitors, donepezil (DNP) is one of the most preferred choices in AD therapy. The X-ray crystal structures of Torpedo californica AChE in complex with two novel rigid DNP-like analogs, compounds 1 and 2, have been determined. Kinetic studies indicated that compounds 1 and 2 show a mixed-type inhibition against TcAChE, with Ki values of 11.12 ± 2.88 and 29.86 ± 1...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29627618/chemometrics-assisted-spectrophotometric-green-method-for-correcting-interferences-in-biowaiver-studies-application-to-assay-and-dissolution-profiling-study-of-donepezil-hydrochloride-tablets
#4
Mohamed A Korany, Hoda Mahgoub, Rim S Haggag, Marwa A A Ragab, Osama A Elmallah
A green, simple and cost effective chemometric UV-Vis spectrophotometric method has been developed and validated for correcting interferences that arise during conducting biowaiver studies. Chemometric manipulation has been done for enhancing the results of direct absorbance, resulting from very low concentrations (high incidence of background noise interference) of earlier points in the dissolution timing in case of dissolution profile using first and second derivative (D1 & D2) methods and their corresponding Fourier function convoluted methods (D1/FF& D2/FF)...
March 27, 2018: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/29622037/a-phase-2-clinical-trial-of-pf-05212377-sam-760-in-subjects-with-mild-to-moderate-alzheimer-s-disease-with-existing-neuropsychiatric-symptoms-on-a-stable-daily-dose-of-donepezil
#5
Terence Fullerton, Brendon Binneman, William David, Marielle Delnomdedieu, James Kupiec, Peter Lockwood, Jessica Mancuso, Jeffrey Miceli, Joanne Bell
BACKGROUND: Symptomatic benefits have been reported for 5-HT6 receptor antagonists in Alzheimer's disease (AD) trials. SAM-760 is a potent and selective 5-HT6 receptor antagonist that has demonstrated central 5-HT6 receptor saturation in humans at a dose of 30 mg. METHODS: This was a randomized, double-blind, placebo-controlled, parallel-group, multicenter trial evaluating the efficacy and safety of SAM-760 30 mg once daily (QD) for 12 weeks in subjects with AD on a stable regimen of donepezil 5 to 10 mg QD...
April 5, 2018: Alzheimer's Research & Therapy
https://www.readbyqxmd.com/read/29619603/inosine-improves-cognitive-function-and-decreases-aging-induced-oxidative-stress-and-neuroinflammation-in-aged-female-rats
#6
Poonam Ruhal, Dinesh Dhingra
In the present study, the effect of inosine was evaluated on learning and memory of 18 months old aged female rats. Inosine (50, 100 and 200 mg/kg; i.p.) was administered to separate groups of rats for 15 successive days. Donepezil (1 mg/kg; i.p.), an acetylcholinesterase inhibitor, was used as a standard drug. Behavioral models such as Morris water maze and elevated plus maze were used to evaluate the effect of drugs on learning and memory of rats. After behavioral studies, animals were killed and their brain was isolated and further processed for estimation of various biochemical parameters such as acetylcholinesterase activity, oxidative stress markers, proinflammatory marker and histological examinations...
April 4, 2018: Inflammopharmacology
https://www.readbyqxmd.com/read/29611620/synthesis-and-biological-evaluation-of-potential-acetylcholinesterase-inhibitors-based-on-a-benzoxazine-core
#7
Claudio Méndez-Rojas, Gabriel Quiroz, Mario Faúndez, Carlos Gallardo-Garrido, C David Pessoa-Mahana, Hery Chung, Eduardo Gallardo-Toledo, Claudio Saitz-Barría, Ramiro Araya-Maturana, Marcelo J Kogan, María C Zúñiga-López, Patricio Iturriaga-Vásquez, Carla Valenzuela-Gutiérrez, Hernán Pessoa-Mahana
With the purpose of expanding the structural variety of chemical compounds available as pharmacological tools for the treatment of Alzheimer's disease, we synthesized and evaluated a novel series of indole-benzoxazinones (Family I) and benzoxazine-arylpiperazine derivatives (Family II) for potential human acetylcholinesterase (hAChE) inhibitory properties. The most active compounds 7a and 7d demonstrated effective inhibitory profiles with Ki values of 20.3 ± 0.9 μM and 20.2 ± 0.9 μM, respectively...
April 3, 2018: Archiv der Pharmazie
https://www.readbyqxmd.com/read/29611403/effect-of-placenta-derived-mesenchymal-stem-cells-in-a-dementia-rat-model-via-microglial-mediation-a-comparison-between-stem-cell-transplant-methods
#8
Jae Sung Cho, Jihyeon Lee, Da Un Jeong, Han Wool Kim, Won Seok Chang, Jisook Moon, Jin Woo Chang
PURPOSE: Loss of cholinergic neurons in the hippocampus is a hallmark of many dementias. Administration of stem cells as a therapeutic intervention for patients is under active investigation, but the optimal stem cell type and transplantation modality has not yet been established. In this study, we studied the therapeutic effects of human placenta-derived mesenchymal stem cells (pMSCs) in dementia rat model using either intracerebroventricular (ICV) or intravenous (IV) injections and analyzed their mechanisms of therapeutic action...
May 2018: Yonsei Medical Journal
https://www.readbyqxmd.com/read/29605487/association-between-abca1-gene-polymorphisms-and-the-therapeutic-response-to-donepezil-therapy-in-han-chinese-patients-with-alzheimer-s-disease
#9
Jin Lu, Jianliang Fu, Yuan Zhong, Quanjun Yang, Jinlu Huang, Jie Li, Yan Huo, Yuwu Zhao, Lili Wan, Cheng Guo
AIM: It is reported that ABCA1, which plays a key role in cholesterol transport and apolipoprotein E (APOE) metabolism in the brain, is related to Alzheimer's disease. However, few studies have focused on the relationship between the ABCA1 gene and the therapeutic response to donepezil (DNP), which has been shown to be related to reduced sAPP production.This study evaluated the association between the ABCA1 gene polymorphism and the clinical response to donepezil therapy in Han Chinese patients with Alzheimer's disease...
March 29, 2018: Brain Research Bulletin
https://www.readbyqxmd.com/read/29602294/melatonin-ameliorates-brain-oxidative-stress-and-upregulates-senescence-marker-protein-30-and-osteopontin-in-a-rat-model-of-vascular-dementia
#10
I Bin-Jaliah, H F Sakr
The aim of this study was to investigate the effect of melatonin on oxidative stress and senescence marker protein-30 (SMP30) as well as osteopontin (OPN) expression in the hippocampus of rats subjected to vascular dementia (VD). A total of 72 male rats were divided into six groups (n = 12 each) as follows: (i) untreated control (CON), (ii) sham-operated group, (iii) sham-operated + melatonin, (iv) rats exposed to VD induced by permanent bilateral occlusion of the common carotid arteries (BCCAO) leading to chronic cerebral hypoperfusion, (v) rats exposed to VD + melatonin, and (vi) rats exposed to VD + donepezil (DON)...
March 1, 2018: Physiology International
https://www.readbyqxmd.com/read/29567174/protein-mimicking-nanowire-inspired-electro-catalytic-biosensor-for-probing-acetylcholinesterase-activity-and-its-inhibitors
#11
Qingqing Zhang, Yufang Hu, Di Wu, Shaohua Ma, Jiao Wang, Jiajia Rao, Lihua Xu, Huan Xu, Huili Shao, Zhiyong Guo, Sui Wang
A highly sensitive electrochemical biosensor based on the synthetized L-Cysteine-Ag(I) coordination polymer (L-Cys-Ag(I) CP), which looks like a protein-mimicking nanowire, was constructed to detect acetylcholinesterase (AChE) activity and screen its inhibitors. This sensing strategy involves the reaction of acetylcholine chloride (ACh) with acetylcholinesterase (AChE) to form choline that is in turn catalytically oxidized by choline oxidase (ChOx) to produce hydrogen peroxide (H2 O2 ), thus L-Cys-Ag(I) CP possesses the electro-catalytic property to H2 O2 reduction...
June 1, 2018: Talanta
https://www.readbyqxmd.com/read/29564727/tacrine-10-hupyridone-a-dual-binding-acetylcholinesterase-inhibitor-potently-attenuates-scopolamine-induced-impairments-of-cognition-in-mice
#12
Huixin Chen, Siying Xiang, Ling Huang, Jiajia Lin, Shengquan Hu, Shing-Hung Mak, Chuang Wang, Qinwen Wang, Wei Cui, Yifan Han
Tacrine(10)-hupyridone (A10E) was designed as a dual-binding acetylcholinesterase (AChE) inhibitor from the modification of tacrine and a fragment of huperzine A. We have found that A10E effectively inhibited AChE in a mixed competitive manner, with an IC50 of 26.4 nM, which is more potent than those of tacrine and huperzine A. Most importantly, we have shown, for the first time that A10E attenuated scopolamine-induced cognitive impairments without affecting motor function in mice. A10E effectively attenuated impairments of learning and memory to a similar extent as donepezil, an inhibitor of AChE used for treating Alzheimer's disease (AD)...
March 21, 2018: Metabolic Brain Disease
https://www.readbyqxmd.com/read/29560413/effect-of-donepezil-on-transcranial-magnetic-stimulation-parameters-in-alzheimer-s-disease
#13
Yun Tae Hwang, Lorenzo Rocchi, Paul Hammond, Chris Jd Hardy, Jason D Warren, Basil H Ridha, John Rothwell, Martin N Rossor
Introduction: There is a need for a reliable, noninvasive biomarker for Alzheimer's disease (AD). We assessed whether short-latency afferent inhibition (SAI), a transcranial magnetic stimulation paradigm that assesses cholinergic circuits of the brain, could become such a biomarker. Methods: Nineteen patients with AD underwent four SAI testing sessions. The timing of their usual donepezil dose was altered to create different cholinergic states for each session. This was compared to the SAI results from 20 healthy subjects...
2018: Alzheimer's & Dementia: Translational Research & Clinical Interventions
https://www.readbyqxmd.com/read/29560322/pharmacotherapy-prescription-trends-for-cognitive-behavioral-disorder-in-patients-with-brain-injury-in-korea
#14
Sungchul Huh, Tae Wan Kim, Jung Hyun Yang, Myung Hoon Moon, Soo-Yeon Kim, Hyun-Yoon Ko
Objective: To investigate the current status of pharmacotherapy prescribed by physiatrists in Korea for cognitive-behavioral disorder. Methods: A cross-sectional study was performed by mailing questionnaires to 289 physiatrists working at teaching hospitals. Items on the questionnaire evaluated prescribing patterns of 16 drugs related to cognitive-behavioral therapy, the status of combination pharmacotherapy, and tools for assessing target symptoms. Results: Fifty physiatrists (17...
February 2018: Annals of Rehabilitation Medicine
https://www.readbyqxmd.com/read/29553158/cholinergic-medication-for-antipsychotic-induced-tardive-dyskinesia
#15
REVIEW
Irina Tammenmaa-Aho, Rosie Asher, Karla Soares-Weiser, Hanna Bergman
BACKGROUND: Tardive dyskinesia (TD) remains a troublesome adverse effect of conventional antipsychotic (neuroleptic) medication. It has been proposed that TD could have a component of central cholinergic deficiency. Cholinergic drugs have been used to treat TD. OBJECTIVES: To determine the effects of cholinergic drugs (arecoline, choline, deanol, lecithin, meclofenoxate, physostigmine, RS 86, tacrine, metoxytacrine, galantamine, ipidacrine, donepezil, rivastigmine, eptastigmine, metrifonate, xanomeline, cevimeline) for treating antipsychotic-induced TD in people with schizophrenia or other chronic mental illness...
March 19, 2018: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/29543387/design-synthesis-and-evaluation-of-genipin-derivatives-for-the-treatment-of-alzheimer-s-disease
#16
Weijun Huang, Yujun Wang, Jiaming Li, Yanchun Zhang, Xiaodong Ma, Panhu Zhu, Yang Zhang
Twenty two novel genipin derivatives have been designed, synthesized and evaluated for their inhibitory activity against acetylcholinesterase (AChE). As a result, compound 13a bearing ligustrazine moiety displayed the most potent AChE inhibitory activity in this serieswith IC50 value of 218 nM. Besides, MTT assay was performed to investigate the neuroprotection of these compounds against PC12 cells injured by Amyloid β-protein 1-42 (Aβ1-42 ). Among them, 8a showed higher inhibition rate (%Inhibition = 22...
March 15, 2018: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29533663/nnn-pincer-ru-ii-complex-catalyzed-%C3%AE-alkylation-of-ketones-with-alcohols
#17
Xiao-Niu Cao, Xiao-Min Wan, Fa-Liu Yang, Ke Li, Xin-Qi Hao, Tian Shao, Xinju Zhu, Mao-Ping Song
A series of novel ruthenium(II) complexes supported by a symmetrical NNN ligand were prepared and fully characterized. These complexes exhibited good performance in transfer hydrogenation to form new C-C bonds using alcohols as the alkylating agents, generating water as the only byproduct. A broad range of substrates, including (hetero)aryl- or alkyl-ketones and alcohols, were well tolerated under the optimized conditions. Notably, α-substituted methylene ketones were also investigated, which afforded α-branched steric hindrance products...
March 13, 2018: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29529892/profiling-donepezil-template-into-multipotent-hybrids-with-antioxidant-properties
#18
Eva Mezeiova, Katarina Spilovska, Eugenie Nepovimova, Lukas Gorecki, Ondrej Soukup, Rafael Dolezal, David Malinak, Jana Janockova, Daniel Jun, Kamil Kuca, Jan Korabecny
Alzheimer's disease is debilitating neurodegenerative disorder in the elderly. Current therapy relies on administration of acetylcholinesterase inhibitors (AChEIs) -donepezil, rivastigmine, galantamine, and N-methyl-d-aspartate receptor antagonist memantine. However, their therapeutic effect is only short-term and stabilizes cognitive functions for up to 2 years. Given this drawback together with other pathological hallmarks of the disease taken into consideration, novel approaches have recently emerged to better cope with AD onset or its progression...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29522770/therapeutic-evaluation-of-solid-lipid-nanoparticle-of-quercetin-in-pentylenetetrazole-induced-cognitive-impairment-of-zebrafish
#19
Narahari Rishitha, Arunachalam Muthuraman
BACKGROUND: Quercetin is a major flavonoid in various plants. It possesses the multiple pharmacological actions like vascular integrity and regulatory action of the blood-brain barrier. AIMS: The present study is focused on evaluating the role of solid lipid nanoparticle of quercetin in pentylenetetrazole (PTZ) induced cognitive impairment of Danio rerio species. MAIN METHODS: The memory impairment of zebrafish was induced by exposing of PTZ in 7...
March 6, 2018: Life Sciences
https://www.readbyqxmd.com/read/29519323/icariside-ii-ameliorates-ibotenic-acid-induced-cognitive-impairment-and-apoptotic-response-via-modulation-of-mapk-pathway-in-rats
#20
Lianzi He, Yuanyuan Deng, Jianmei Gao, Lingrong Zeng, Qihai Gong
BACKGROUND: Excitotoxicity is extensively recognized as a major pathological process of neuronal death and has been proved to play a key role in Alzheimer's disease (AD). ICS II, a flavonoid compound from Herba Epimedii Maxim, is attracting great interests due to its neuroprotective properties. PURPOSE: The present study was aimed to explore the effects of ICS II on cognitive dysfunction and apoptotic response induced by excitatory neurotoxin ibotenic acid (IBO) injection in rats...
March 1, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
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