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https://www.readbyqxmd.com/read/29772299/biophenols-enzymes-%C3%AE-secretase-cholinesterases-histone-deacetylase-and-tyrosinase-inhibitors-from-olive-olea-europaea-l
#1
Syed Haris Omar, Christopher J Scott, Adam S Hamlin, Hassan K Obied
The focus of this study was on inhibition of enzymes involved in the pathogenesis Alzheimer's disease (AD) including prime amyloid beta (Aβ) producing enzyme (β-secretase: BACE-1) and disease progression enzymes including acetylcholinesterase (AChE), butyrylcholinesterase (BChE), histone deacetylase (HDAC), and tyrosinase along with the catecholamine L-DOPA, by using olive biophenols. Here we report the strongest inhibition of BACE-1 from rutin (IC50 : 3.8 nM) followed by verbascoside (IC50 : 6.3 nM) and olive fruit extract (IC50 : 18 ng), respectively...
May 14, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29772289/nose-to-brain-drug-delivery-an-update-on-clinical-challenges-and-progress-towards-approval-of-anti-alzheimer-drugs
#2
REVIEW
Mukta Agrawal, Swarnlata Saraf, Shailendra Saraf, Sophia G Antimisiaris, Mahavir Chougule, Sunday A Shoyele, Amit Alexander
According to the Alzheimer Association Report (2017), Alzheimer's disease (AD) is the 6th primary cause of death in the USA, which affects nearly 5.5 million people. In the year 2017 itself, the cost of AD treatment in the USA has been reported to rise to $259 billion. This statistic shows the severity of the disease in the USA which is very much similar across the globe. On the other hand, the treatment remains limited to a few conventional oral medications (approved by FDA). These are mainly acting superficially from mild to the moderate AD...
May 14, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29768996/a-systematic-review-on-donepezil-based-derivatives-as-potential-cholinesterase-inhibitors-for-alzheimer-s-disease
#3
Jan Korabecny, Katarina Spilovska, Eva Mezeiova, Ondrej Benek, Radomir Juza, Daniel Kaping, Ondrej Soukup
Alzheimer's disease (AD) is a multifactorial progressive neurodegenerative disorder characterized by memory loss, disorientation, and gradual deterioration of intellectual capacity. Its etiology has not been elucidated yet. To date, only one therapeutic approach has been approved for the treatment of AD. The pharmacotherapy of AD has relied on non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist - memantine, and acetylcholinesterase (AChE) inhibitors (AChEIs) - tacrine, donepezil, rivastigmine and galantamine...
May 16, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29762677/anti-dementia-drugs-for-psychopathology-and-cognitive-impairment-in-schizophrenia-a-systematic-review-and-meta-analysis
#4
Taro Kishi, Toshikazu Ikuta, Kazuto Oya, Shinji Matsunaga, Yuki Matsuda, Nakao Iwata
Background: We conducted a systematic review and meta-analysis of double-blind, randomized, placebo-controlled trials of anti-dementia drugs plus antipsychotics (ADD+AP) for schizophrenia. Methods: Primary outcomes of efficacy and safety included improving overall symptoms (Positive and Negative Syndrome Scale and Brief Psychiatric Rating Scale scores) and all-cause discontinuation, respectively. Other outcomes included psychopathology subscales (positive, negative, general, and anxiety/depressive symptoms), cognitive function (attention/vigilance, reasoning/problem solving, social cognition, speed of processing, verbal learning, visual learning, working memory, and cognitive control/executive function), Mini-Mental State Examination (MMSE) scores, treatment discontinuation due to adverse events and inefficacy, and individual adverse events...
May 14, 2018: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29756568/aporphines-and-alzheimer-s-disease-towards-a-medical-approach-facing-the-future
#5
Seyed Mohammad Nabavi, Eugenio Uriarte, Luca Rastrelli, Eduardo Sobarzo-Sanchez
Alzheimer's disease (AD) is a neurodegenerative disease that is reducing progressively the part cognitive inside the Central Nervous System (CNS) and that affects the memories and emotions of the patients who endure this disease. Many drugs have been assessed in patients with different evolutionary grades of the disease, having diverse results, depending on the used compound. Some of them afford dependence and many others with side effects that affect the emotional part and the economic cost of the treatment...
May 13, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29752082/pvc-membrane-coated-wire-and-carbon-paste-ion-selective-electrodes-for-potentiometric-determination-of-galantamine-hydrobromide-in-physiological-fluids
#6
Fatehy M Abdel-Haleem, Mohamed Saad, Ahmed Barhoum, Mikhael Bechelany, Mahmoud S Rizk
We report on highly-sensitive ion-selective electrodes (ISEs) for potentiometric determining of galantamine hydrobromide (GB) in physiological fluids. Galantamine hydrobromide (GB) was selected for this study due to its previous medical importance for treating Alzheimer's disease. Three different types of ISEs were investigated: PVC membrane electrode (PVCE), carbon-paste electrode (CPE), and coated-wire electrode (CWE). In the construction of these electrodes, galantaminium-reineckate (GR) ion-pair was used as a sensing species for GB in solutions...
August 1, 2018: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/29742314/benzofuran-and-indole-a-promising-scaffold-for-drug-development-in-alzheimer-s-disease
#7
Deepti Goyal, Amandeep Kaur, Bhupesh Goyal
Alzheimer's disease (AD) is a progressive neurodegenerative disease with no clinically accepted treatment to cure or halt its progression. The Food and Drug Administration (FDA) approved drugs (rivastigmine, donepezil, galantamine and memantine) at best provide marginal benefits thus emphasize the urgent need to explore other molecular entities as future drug candidates for AD. Looking at the wide pharmaceutical applications of heterocyclic compounds and particularly those containing benzofuran and indole ring system; these molecular frameworks draw special attention of the medicinal chemists for further evaluation in numerous diseases...
May 9, 2018: ChemMedChem
https://www.readbyqxmd.com/read/29735100/multidirectional-investigations-on-different-parts-of-allium-scorodoprasum-l-subsp-rotundum-l-stearn-phenolic-components-in-vitro-biological-and-in-silico-propensities
#8
Adriano Mollica, Gokhan Zengin, Marcello Locatelli, Carene Marie Nancy Picot-Allain, Mohamad Fawzi Mahomoodally
Allium species have been widely used for culinary and medicinal purposes. This study attempts for the first time to investigate into the enzyme inhibitory potential of different plant parts of Allium scorodoprasum L. subsp. rotundum (L.) Stearn, also known as wild garlic or leek in Turkey. The antioxidant and enzyme inhibitory potential of the flower, stem, and bulb extracts of A. scorodoprasum were assessed using in vitro bio-assays. The phenolic composition of the different plant parts was also established...
June 2018: Food Research International
https://www.readbyqxmd.com/read/29726619/development-and-validation-of-a-uplc-ms-method-for-the-determination-of-galantamine-in-guinea-pig-plasma-and-its-application-to-a-pre-clinical-bioavailability-study-of-novel-galantamine-formulations
#9
Jiang Wang, Naresh Pavurala, Xiaoming Xu, Yellela S R Krishnaiah, Patrick J Faustino
To evaluate the bioavailability and pharmacokinetic profiles of two novel galantamine formulations as medical countermeasure products, an ultra-performance liquid chromatography-single quadrupole mass spectrometry (UPLC-MS) method was developed and validated for quantifying galantamine in guinea pig plasma using solid phase extraction with a mixed mode strong cation exchange reversed phase cartridge. Chromatographic separation was achieved on a Waters Acquity UPLC BEH C18 column maintained at 40 °C. The mobile phases were solution-A acetonitrile-water (5:95, v/v) and solution-B acetonitrile-water (90:10, v/v), which both contain 2 mM ammonium formate and 0...
May 4, 2018: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29717478/monotherapy-is-good-enough-for-patients-with-mild-to-moderate-alzheimer-s-disease-a-network-meta-analysis-of-76-randomized-controlled-trials
#10
Kelvin Kf Tsoi, Joyce Yc Chan, Felix Ch Chan, Hoyee W Hirai, Timothy Cy Kwok, Samuel Ys Wong
Memantine and the Acetylcholinesterase inhibitors (AChEIs) are two classes of drugs that are used to treat patients with Alzheimer's disease. We conducted a network meta-analysis of randomized controlled trials to compare the treatment effectiveness of monotherapy or combination therapy A total of 23,707 AD patients in 76 randomized trials were identified. In patients with mild-to-moderate AD, monotherapy with donepezil, galantamine or rivastigmine were superior to placebo in enhancing cognitive functions and activities of daily living (ADL), whereas monotherapy with donepezil or memantine were superior to placebo in improving behavioral symptoms...
May 1, 2018: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29697300/cooperative-hydrogen-bonds-and-mobility-of-the-non-aromatic-ring-as-selectivity-determinants-for-human-acetylcholinesterase-to-similar-anti-alzheimer-s-galantaminics-a-computational-study
#11
Rafael E O Rocha, Leonardo H F de Lima
Galantamine (Gnt) is a natural alkaloid inhibitor of acetylcholinesterase and is presently one of the most used drugs in the treatment against Alzheimer's disease during both the initial and intermediate stages. Among several natural Gnt derivatives, sanguinine (Sng) and lycoramine (Lyc) attract attention because of the way their subtle chemical differences from Gnt lead to drastic and opposite distinctions in inhibitory effects. However, to date there is no solved structure for these natural derivatives. In the present study, we applied computational modeling and free energy calculation methods to better elucidate the molecular basis of the subtle distinctions between these derivatives and Gnt...
April 26, 2018: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/29670547/medications-used-for-cognitive-enhancement-in-patients-with-schizophrenia-bipolar-disorder-alzheimer-s-disease-and-parkinson-s-disease
#12
REVIEW
Wen-Yu Hsu, Hsien-Yuan Lane, Chieh-Hsin Lin
Background/aims: Cognitive impairment, which frequently occurs in patients with schizophrenia, bipolar disorder, Alzheimer's disease, and Parkinson's disease, has a significant impact on the daily lives of both patients and their family. Furthermore, since the medications used for cognitive enhancement have limited efficacy, the issue of cognitive enhancement still remains a clinically unsolved challenge. Sampling and methods: We reviewed the clinical studies (published between 2007 and 2017) that focused on the efficacy of medications used for enhancing cognition in patients with schizophrenia, bipolar disorder, Alzheimer's disease, and Parkinson's disease...
2018: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/29669582/galantamine-improves-cognition-hippocampal-inflammation-and-synaptic-plasticity-impairments-induced-by-lipopolysaccharide-in-mice
#13
Yi Liu, Yuyun Zhang, Xian Zheng, Tongyong Fang, Xia Yang, Xuan Luo, Anlei Guo, Kelly A Newell, Xu-Feng Huang, Yinghua Yu
BACKGROUND: Neuroinflammation plays an important role in the onset and progression of neurodegenerative diseases such as Alzheimer's disease. Lipopolysaccharide (LPS, endotoxin) levels are higher in the brains of Alzheimer's disease patients and are associated with neuroinflammation and cognitive decline, while neural cholinergic signaling controls inflammation. This study aimed to examine the efficacy of galantamine, a clinically approved cholinergic agent, in alleviating LPS-induced neuroinflammation and cognitive decline as well as the associated mechanism...
April 18, 2018: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/29669164/galantamine-is-not-a-positive-allosteric-modulator-of-human-%C3%AE-4%C3%AE-2-or-%C3%AE-7-nicotinic-acetylcholine-receptors
#14
Natalia M Kowal, Philip K Ahring, Vivian W Y Liao, Dinesh C Indurti, Benjamin S Harvey, Susan M O'Connor, Mary Chebib, Elin S Olafsdottir, Thomas Balle
BACKGROUND AND PURPOSE: The alkaloid galantamine was originally isolated from the green snowdrop Galanthus woronowii and is currently marketed as a drug for treatment of mild to moderate dementia in Alzheimer's disease patients. In addition to a well-documented proficiency of inhibiting the acetylcholinesterase enzyme, galantamine has been reported to increase neuronal nicotinic acetylcholine (nACh) receptor function by acting as a positive allosteric modulator. Yet, there remains controversy regarding these findings in the literature...
April 18, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29653432/in-vitro-evaluation-and-in-silico-studies-applied-on-newly-synthesized-amide-derivatives-of-n-phthaloylglycine-as-butyrylcholinesterase-bche-inhibitors
#15
Samreen Begum, Shaikh Sirajuddin Nizami, Uzma Mahmood, Summyia Masood, Sahar Iftikhar, Summayya Saied
Amide derivatives of N-phthaloylglycine were synthesized under Schotten Baumann reaction condition. The structures of synthesized compounds (4a-d) were characterized by using FTIR, 1 HNMR and EI-MS. The compounds were evaluated for their in-vitro Butyrylcholinesterase inhibition and all of them exhibited good activity against this enzyme. Compound 4a (IC50  = 6.5 ± 0.1) was found to be most potent compared with the reference compound Galantamine (IC50  = 6.6 ± 0.00038) and the other compounds (4b,4c,4d) were also possess that activity and hence can be employed for the discovery of lead compounds against Alzheimer's disease...
April 7, 2018: Computational Biology and Chemistry
https://www.readbyqxmd.com/read/29572553/galantamine-anti-colitic-effect-role-of-alpha-7-nicotinic-acetylcholine-receptor-in-modulating-jak-stat3-nf-%C3%AE%C2%BAb-hmgb1-rage-and-p-akt-bcl-2-pathways
#16
Shakeeb A Wazea, Walaa Wadie, Ashraf K Bahgat, Hanan S El-Abhar
Vagal stimulation controls systemic inflammation and modulates the immune response in different inflammatory conditions, including inflammatory bowel diseases (IBD). The released acetylcholine binds to alpha-7 nicotinic acetylcholine receptor (α7 nAChR) to suppress pro-inflammatory cytokines. This provides a new range of potential therapeutic approaches for controlling inflammatory responses. The present study aimed to assess whether galantamine (Galan) anti-inflammatory action involves α7 nAChR in a 2,4,6-trinitrobenzene sulfonic acid (TNBS) model of colitis and to estimate its possible molecular pathways...
March 23, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29570959/galantamine-memantine-combination-for-cognitive-impairments-due-to-electroconvulsive-therapy-traumatic-brain-injury-and-neurologic-and-psychiatric-disorders-kynurenic-acid-and-mismatch-negativity-target-engagement
#17
Maju Mathew Koola
Cognitive impairments due to electroconvulsive therapy (ECT), traumatic brain injury (TBI), and neurologic and psychiatric disorders are prevalent. Cholinergic and glutamatergic pathways, α-7 nicotinic acetylcholine (α-7nACh) receptor, and N-methyl-d-aspartate (NMDA) receptor are potential pathophysiologic mechanisms in all of these conditions. Galantamine not only is an acetylcholinesterase inhibitor but has a dual mode of action as a α-7nACh receptor modulator as well. Memantine is a noncompetitive NMDA receptor antagonist...
March 1, 2018: Primary Care Companion to CNS Disorders
https://www.readbyqxmd.com/read/29559423/symptomatic-treatment-of-vascular-cognitive-impairment-stream-vci-protocol-for-a-cross-over-trial
#18
Jolien Fleur Leijenaar, Geert Jan Groeneveld, Wiesje Maria van der Flier, Philip Scheltens, Erica Surya Klaassen, Henry Chanoch Weinstein, Geert Jan Biessels, Frederik Barkhof, Niels Daniël Prins
BACKGROUND: People with vascular cognitive impairment (VCI) constitute a clinically heterogeneous group, but previous symptomatic drug trials in VCI did not take this clinical heterogeneity into account. Executive dysfunction and memory impairment are the cognitive domains that are most frequently impaired in VCI, and these impairments are likely to reflect vascular damage to specific neurotransmitter systems, which opens the possibility for targeted symptomatic treatment directed at specific neurotransmitters...
March 20, 2018: JMIR Research Protocols
https://www.readbyqxmd.com/read/29553158/cholinergic-medication-for-antipsychotic-induced-tardive-dyskinesia
#19
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/29552507/galantamine-memantine-combination-effective-in-dementia-translate-to-dementia-praecox
#20
Maju Mathew Koola, Ajay K Parsaik
No abstract text is available yet for this article.
June 2018: Schizophrenia Research. Cognition
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