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https://www.readbyqxmd.com/read/28103749/clinical-practice-with-anti-dementia-drugs-a-revised-third-consensus-statement-from-the-british-association-for-psychopharmacology
#1
John T O'Brien, Clive Holmes, Matthew Jones, Roy Jones, Gill Livingston, Ian McKeith, Peter Mittler, Peter Passmore, Craig Ritchie, Louise Robinson, Elizabeth L Sampson, John-Paul Taylor, Alan Thomas, Alistair Burns
The British Association for Psychopharmacology coordinated a meeting of experts to review and revise its previous 2011 guidelines for clinical practice with anti-dementia drugs. As before, levels of evidence were rated using accepted standards which were then translated into grades of recommendation A-D, with A having the strongest evidence base (from randomised controlled trials) and D the weakest (case studies or expert opinion). Current clinical diagnostic criteria for dementia have sufficient accuracy to be applied in clinical practice (B) and both structural (computed tomography and magnetic resonance imaging) and functional (positron emission tomography and single photon emission computerised tomography) brain imaging can improve diagnostic accuracy in particular situations (B)...
December 1, 2016: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28102474/anti-amnestic-effect-of-curcumin-in-combination-with-donepezil-an-anticholinesterase-drug-involvement-of-cholinergic-system
#2
Ayodele Jacob Akinyemi, Ganiyu Oboh, Sunday Idowu Oyeleye, Opeyemi Ogunsuyi
Recently, combination therapy involving cholinesterase (ChE) inhibitor with other neuroprotective agents has shown better desirable effect in the management/prevention of dementia but limited information is available on their effect with dietary polyphenols. Hence, this study sought to assess the combined pretreatment effect of curcumin, the major polyphenolic compound of turmeric (Curcuma longa) rhizomes, with donepezil, a cholinesterase inhibitor, on cognitive function in scopolamine-induced memory impairment in rats...
January 19, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/28088312/dementia-in-parkinson-s-disease
#3
REVIEW
Hasmet A Hanagasi, Zeynep Tufekcioglu, Murat Emre
Dementia can occur in a substantial number of patients with Parkinson's disease with a point prevalence close to 30%. The cognitive profile is characterized by predominant deficits in executive, visuospatial functions, attention and memory. Behavioral symptoms are frequent such as apathy, visual hallucinations and delusions. The most prominent associated pathology is Lewy body-type and biochemical deficit is cholinergic. Placebo-controlled randomized trials with cholinesterase inhibitors demonstrated modest but significant benefits in cognition, behavioral symptoms and global functions...
January 5, 2017: Journal of the Neurological Sciences
https://www.readbyqxmd.com/read/28080146/perceptions-vs-evidence-therapeutic-substitutes-for-antipsychotics-in-patients-with-dementia-in-long-term-care
#4
Brianne L Olivieri-Mui, John W Devlin, Aileen Ochoa, Danielle Schenck, Becky Briesacher
OBJECTIVE: To compare differences between clinician perceptions of therapeutic substitutes for antipsychotics prescribed to patients with dementia in long term care (LTC) and published evidence. METHODS: A mixed-methods approach that included a drug information search, online survey of 55 LTC clinicians and a comprehensive literature review was used. For 41 pharmacologic antipsychotic substitute candidates identified, LTC clinicians rated the likelihood they would substitute each for patients with dementia and identified non-pharmacologic antipsychotic substitutes...
January 12, 2017: Aging & Mental Health
https://www.readbyqxmd.com/read/28064079/tacrine-resveratrol-fused-hybrids-as-multi-target-directed-ligands-against-alzheimer-s-disease
#5
Jakub Jeřábek, Elisa Uliassi, Laura Guidotti, Jan Korábečný, Ondřej Soukup, Vendula Sepsova, Martina Hrabinova, Kamil Kuča, Manuela Bartolini, Luis Emiliano Peña-Altamira, Sabrina Petralla, Barbara Monti, Marinella Roberti, Maria Laura Bolognesi
Multi-target drug discovery is one of the most followed approaches in the active central nervous system (CNS) therapeutic area, especially in the search for new drugs against Alzheimer's disease (AD). This is because innovative multi-target-directed ligands (MTDLs) could more adequately address the complexity of this pathological condition. In a continuation of our efforts aimed at a new series of anti-AD MTDLs, we combined the structural features of the cholinesterase inhibitor drug tacrine with that of resveratrol, which is known for its purported antioxidant and anti-neuroinflammatory activities...
December 26, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28063945/calcineurin-inhibitors-improve-memory-loss-and-neuropathological-changes-in-mouse-model-of-dementia
#6
Amit Kumar, Nirmal Singh
AIM: The present study was designed to investigate the potential of Cyclosporine (CsA) and Tacrolimus, the inhibitors of calcineurin (CaN) in cognitive deficits of mice. METHODS: Streptozotocin [STZ, 3mg/kg, injected intracerebroventricular (i.c.v.)] was used to induce memory deficits in NIH mice, while aged mice separately taken served as a natural model of dementia. Morris water maze (MWM) test was employed to evaluate learning and memory of the animals. A battery of biochemical and histopathological studies was also performed...
January 4, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28061415/an-enantiomer-based-virtual-screening-approach-discovery-of-chiral-organophosphates-as-acetyl-cholinesterase-inhibitors
#7
Aiqian Zhang, Yunsong Mu, Fengchang Wu
Chiral organophosphates (OPs) have been used widely around the world, very little is known about binding mechanisms with biological macromolecules. An in-depth understanding of the stereo selectivity of human AChE and discovering bioactive enantiomers of OPs can decrease health risks of these chiral chemicals. In the present study, a flexible molecular docking approach was conducted to investigate different binding modes of twelve phosphorus enantiomers. A pharmacophore model was then developed on basis of the bioactive conformations of these compounds...
January 3, 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/28058292/monoclonal-antibodies-that-recognize-various-folding-states-of-pure-human-butyrylcholinesterase-can-immunopurify-butyrylcholinesterase-from-human-plasma-stored-at-elevated-temperatures
#8
Hong Peng, Thomas A Blake, Rudolph C Johnson, Alicia J Dafferner, Stephen Brimijoin, Oksana Lockridge
Human plasma to be analyzed for exposure to cholinesterase inhibitors is stored at 4 °C or lower to prevent denaturation of human butyrylcholinesterase (HuBChE), the biomarker of exposure. Currently published protocols immunopurify HuBChE using antibodies that bind native HuBChE before analysis by mass spectrometry. It is anticipated that the plasma collected from human casualties may be stored nonideally at elevated temperatures of up to 45 °C for days or maybe weeks. At 45 °C, the plasma loses 50% of its HuBChE activity in 8 days and 95% in 40 days...
December 31, 2016: ACS Omega
https://www.readbyqxmd.com/read/28058207/memory-loss-five-new-things
#9
Ferenc Deak, Nidhi Kapoor, Calin Prodan, Linda A Hershey
PURPOSE OF REVIEW: Memory loss can be due to a wide variety of causes. We provide new information about the biology of common genetic and acquired causes of memory loss in older adults. RECENT FINDINGS: New data are available about the genetics of Alzheimer disease (AD), dementia with Lewy bodies (DLB), and frontotemporal dementia. Amyloid PET, FDG-PET, and MRI have improved our understanding of how mild cognitive impairment evolves to AD. Several studies have shown links between concussion and chronic traumatic encephalopathy...
December 2016: Neurology. Clinical Practice
https://www.readbyqxmd.com/read/28049192/combined-memantine-and-donepezil-treatment-improves-behavioral-and-psychological-symptoms-of-dementia-like-behaviors-in-olfactory-bulbectomized-mice
#10
Yasushi Yabuki, Kazuya Matsuo, Koga Hirano, Yasuharu Shinoda, Shigeki Moriguchi, Kohji Fukunaga
Memantine, an uncompetitive N-methyl-D-aspartate receptor antagonist, and the cholinesterase inhibitor, donepezil, are approved in most countries for treating moderate-to-severe Alzheimer's disease (AD). These drugs have different molecular targets; thus, it is expected that the effects of combined treatment would be synergistic. Some reports do show memantine/donepezil synergy in ameliorating cognition in AD model animals, but their combined effects on behavioral and psychological symptoms of dementia (BPSD)-like behaviors have not been addressed...
January 4, 2017: Pharmacology
https://www.readbyqxmd.com/read/28040595/euphorbia-denticulata-lam-a-promising-source-of-phyto-pharmaceuticals-for-the-development-of-novel-functional-formulations
#11
Gokhan Zengin, Ahmet Uysal, Abdurrahman Aktumsek, Andrei Mocan, Adriano Mollica, Marcello Locatelli, Luisa Custodio, Nuno R Neng, José M F Nogueira, Zaahira Aumeeruddy-Elalfi, M Fawzi Mahomoodally
In this study, Methanolic extracts of Euphorbia denticulata parts (flowers, leaf, stem, and mix of aerial parts) were assessed for a panoply of bioactivities. Inhibitory potential against key enzymes involved in diabetes (α-glucosidase and α-amylase), obesity (pancreatic lipase), neurodegenerative diseases (cholinesterases), and hyperpigmentation (tyrosinase) was evaluated. The antioxidant and antibacterial properties were also assessed. The total phenolic, flavonoid, and phytochemical profile were established using HPLC/DAD and molecular modelling studies on specific target compounds were performed in silico...
December 29, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28035933/frontal-lobe-function-correlates-with%C3%A2-one-year-incidence-of-urinary-incontinence-in-elderly-with-alzheimer-disease
#12
Taiki Sugimoto, Masaki Yoshida, Rei Ono, Shunsuke Murata, Naoki Saji, Shumpei Niida, Kenji Toba, Takashi Sakurai
BACKGROUND: Urinary incontinence (UI) is frequently observed in patients with Alzheimer's disease (AD). Although previous works highlight the association between frontal lobe-related function and UI, causal relationship is unclear. OBJECTS: To clarify the longitudinal association between frontal lobe function and the incidence of UI at 1 year in patients with AD. METHODS: The subjects were 215 continent AD patients who attended the Memory Clinic of the National Center for Geriatrics and Gerontology of Japan during the period from March 2011 to December 2014...
December 30, 2016: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/28035929/the-citicholinage-study-citicoline-plus-cholinesterase-inhibitors-in-aged-patients-affected-with-alzheimer-s-disease-study
#13
Pietro Gareri, Alberto Castagna, Antonino Maria Cotroneo, Daria Putignano, Raffaele Conforti, Francesco Santamaria, Saverio Marino, Salvatore Putignano
BACKGROUND: Citicoline can have beneficial effects both in degenerative and in vascular cognitive decline in a variety of ways (apoptosis inhibition, neuroplasticity potentiation, phospholipid, and acetylcholine (ACh) synthesis). Acetylcholinesterase inhibitors (AChEIs) have been used for treatment of Alzheimer's disease (AD). When co-administered with cholinergic precursors, they are able to increase the intrasynaptic levels of ACh more than when the single drugs given alone. OBJECTIVE: The aim of the present study was to show the effectiveness of oral citicoline plus AChEIs in patients affected with AD...
December 30, 2016: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/28033733/isolation-crystal-structure-determination-and-cholinesterase-inhibitory-potential-of-isotalatizidine-hydrate-from-delphinium-denudatum
#14
Hanif Ahmad, Shujaat Ahmad, Ezzat Khan, Adnan Shahzad, Mumtaz Ali, Muhammad Nawaz Tahir, Farzana Shaheen, Manzoor Ahmad
CONTEXT: Delphinium denudatum Wall (Ranunculaceae) is a rich source of diterpenoid alkaloids and is widely used for the treatment of various neurological disorders such as epilepsy, sciatica and Alzheimer's disease. OBJECTIVE: The present study describes crystal structure determination and cholinesterase inhibitory potential of isotalatazidine hydrate isolated from the aerial part of Delphinium denudatum. MATERIALS AND METHODS: Phytochemical investigation of Delphinium denudatum resulted in the isolation of isotalatazidine hydrate in crystalline form...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/27990564/planarian-cholinesterase-in-vitro-characterization-of-an-evolutionarily-ancient-enzyme-to-study-organophosphorus-pesticide-toxicity-and-reactivation
#15
Danielle Hagstrom, Hideto Hirokawa, Limin Zhang, Zoran Radic, Palmer Taylor, Eva-Maria S Collins
The freshwater planarian Dugesia japonica has recently emerged as an animal model for developmental neurotoxicology and found to be sensitive to organophosphorus (OP) pesticides. While previous activity staining of D. japonica, which possess a discrete cholinergic nervous system, has shown acylthiocholine catalysis, it is unknown whether this is accomplished through an acetylcholinesterase (AChE), butyrylcholinesterase (BChE), or a hybrid esterase and how OP exposure affects esterase activity. Here, we show that the majority of D...
December 18, 2016: Archives of Toxicology
https://www.readbyqxmd.com/read/27984078/anti-inflammatory-and-protective-effects-of-mt-031-a-novel-multitarget-mao-a-and-ache-buche-inhibitor-in-scopolamine-mouse-model-and-inflammatory-cells
#16
Wei Liu, Alon Rabinovich, Yuval Nash, Dan Frenkel, Yuqiang Wang, Moussa B H Youdim, Orly Weinreb
Previous study demonstrated that the novel multitarget compound, MT-031 preserved in one molecule entity the beneficial properties of its parent drugs, rasagiline and rivastigmine, and exerted high dual potencies of monoamine oxidase-A (MAO-A) and cholinesterase (ChE) inhibition in acute-treated mice and neuroprotective effects against H2O2-induced neurotoxicity in human neuroblastoma SH-SY5Y cells. The present study aimed to further investigate the anti-inflammatory and protective effects of MT-031 in scopolamine mouse model and inflammatory cell cultures...
October 28, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27978805/alzheimer-s-disease-a-review-from-the-pathophysiology-to-diagnosis-new-perspectives-for-pharmacological-treatment
#17
Leide Caroline Dos Santos Picanço, Priscilla Farias Ozela, Maiara de Fátima de Brito Brito, Abraão Alves Pinheiro, Elias Carvalho Padilha, Francinaldo Sarges Braga, Carlos Henrique Tomich de Paula da Silva, Cleydson Breno Rodrigues Dos Santos, Joaquín María Campos Rosa, Lorane Izabel da Silva Hage-Melim
Dementia is characterized by the impairment of cognition and behavior of people over 65 years. Alzheimer's disease (AD) is the most prevalent neurodegenerative disorder in the world, as approximately 47 million people are affected by this disease and the tendency is that this number will increased 62% by 2030. Two microscopic features assist in the characterization of the disease, the amyloid plaques and neurofibrillary agglomerates. All these factors are responsible for the slow and gradual deterioration of memory that affect language, personality or cognitive control...
December 12, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27956858/hptlc-fingerprinting-and-cholinesterase-inhibitory-and-metal-chelating-capacity-of-various-citrus-cultivars-and%C3%A2-olea-europaea
#18
Fatma Sezer Senol, Anita Ankli, Eike Reich, Ilkay Erdogan Orhan
Inhibitory activity of thirty-one ethanol extracts obtained from albedo, flavedo, seed and leaf parts of 17 cultivars of Citrus species from Turkey, the bark and leaves of Olea europaea L. from two locations (Turkey and Cyprus) as well as caffeic acid and hesperidin was tested against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), related to the pathogenesis of Alzheimer's disease, using ELISA microtiter assays at 500 µg/mL. Metal-chelating capacity of the extracts was also determined. BChE inhibitory effect of the Citrus sp...
September 2016: Food Technology and Biotechnology
https://www.readbyqxmd.com/read/27951490/2-4-disubstituted-quinazolines-as-amyloid-%C3%AE-aggregation-inhibitors-with-dual-cholinesterase-inhibition-and-antioxidant-properties-development-and-structure-activity-relationship-sar-studies
#19
Tarek Mohamed, Praveen P N Rao
A library of fifty-seven 2,4-disubstituted quinazoline derivatives were designed, synthesized and evaluated as a novel class of multi-targeting agents to treat Alzheimer's disease (AD). The biological assay results demonstrate the ability of several quinazoline derivatives to inhibit both acetyl and butyrylcholinesterase (AChE and BuChE) enzymes (IC50 range = 1.6-30.5 μM), prevent beta-amyloid (Aβ) aggregation (IC50 range 270 nM-16.7 μM) and exhibit antioxidant properties (34-63.4% inhibition at 50 μM)...
December 2, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27940150/cholinesterase-inhibitors-are-compatible-with-psychosocial-intervention-for-alzheimer-disease-patients-suggested-by-neuroimaging-findings
#20
Kenichi Meguro
We previously reported that the frontal lobe was stimulated by psychosocial intervention for dementia patients, and that the parietal lobe was associated with logical judgment. We hypothesized that the combined therapeutic approach with symptomatic drug treatment can directly stimulate not only attention function but also judgment function indirectly to observing other participants' behaviors. Fifty-two patients with Alzheimer disease underwent the group reminiscence approach with reality orientation, as well as the donepezil treatment...
January 30, 2017: Psychiatry Research
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