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https://www.readbyqxmd.com/read/28797788/novel-dehydroabietylamine-derivatives-as-potent-inhibitors-of-acetylcholinesterase
#1
Jana Wiemann, Anne Loesche, René Csuk
Nowadays, the inhibition of acetylcholinesterase is one of the main pharmacological strategies for the treatment of Alzheimer's disease. Therefore, a set of thirty-four derivatives of the diterpenoid dehydroabietylamine has been synthesized and screened in colorimetric Ellman's assays to determine their ability to inhibit the enzymes acetylcholinesterase (AChE, from electric eel) and butyrylcholinesterase (BChE, from equine serum). A systematic variation of the substitution of dehydroabietylamides enabled an approach to analogs showing a remarkable inhibition potency for AChE...
August 1, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28780468/design-and-synthesis-of-2-6-di-substituted-phenyl-thiazolo-3-2-b-1-2-4-triazoles-as-%C3%AE-glucosidase-and-%C3%AE-amylase-inhibitors-co-relative-pharmacokinetics-and-3d-qsar-and-risk-analysis
#2
Pervaiz Ali Channar, Aamer Saeed, Fayaz Ali Larik, Sajid Rashid, Qaiser Iqbal, Maryam Rozi, Saima Younis, Jamaluddin Mahar
Ten fused heterocyclic derivatives bearing the 2,6-di(subsituted phenyl)thiazolo[3,2-b]-1,2,4-triazoles as central rings were synthesized and structures of the compounds were established by analytical and spectral data using FTIR, EI-MS, (1)H NMR and (13)C NMR techniques. In vitro inhibitory activities of synthesized compounds on α-amylase, α-glucosidase and α-burylcholinesterase (α-BuChE) were evaluated using a purified enzyme assays. Compound 5c demonstrated strong and selective α-amylase inhibitory activity (IC50=1...
August 3, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28761423/galantamine-protects-against-beta-amyloid-peptide-induced-dna-damage-in-a-model-for-alzheimer-s-disease
#3
Willian O Castillo, Andres Felipe Aristizabal-Pachon
No abstract text is available yet for this article.
June 2017: Neural Regeneration Research
https://www.readbyqxmd.com/read/28760642/galantamine-administration-reduces-reactive-astrogliosis-and-upregulates-the-anti-oxidant-enzyme-catalase-in-rats-submitted-to-neonatal-hypoxia-ischemia
#4
F K Odorcyk, F Nicola, L E Duran-Carabali, F Figueiró, J Kolling, A Vizuete, E L Konrath, C A Gonçalves, A T S Wyse, C A Netto
Neonatal hypoxia ischemia (HI) plays a role in the etiology of several neurological pathologies and causes severe sequelae. Acetylcholine is a neurotransmitter in the central nervous system and cholinesterase inhibitors have demonstrated a positive action over HI induced deficits. In order to evaluate the effects of pre and post-hypoxia administrations of galantamine, a cholinesterase inhibitor, in a model of perinatal HI, Wistar rats in the post-natal day 7 (PND7) were subjected to a combination of unilateral occlusion of the right carotid artery with the exposure to a 1h hypoxia...
July 29, 2017: International Journal of Developmental Neuroscience
https://www.readbyqxmd.com/read/28724799/galantamine-alleviates-inflammation-and-insulin-resistance-in-patients-with-metabolic-syndrome-in-a-randomized-trial
#5
Fernanda M Consolim-Colombo, Carine T Sangaleti, Fernando O Costa, Tercio L Morais, Heno F Lopes, Josiane M Motta, Maria C Irigoyen, Luiz A Bortoloto, Carlos Eduardo Rochitte, Yael Tobi Harris, Sanjaya K Satapathy, Peder S Olofsson, Meredith Akerman, Sangeeta S Chavan, Meggan MacKay, Douglas P Barnaby, Martin L Lesser, Jesse Roth, Kevin J Tracey, Valentin A Pavlov
BACKGROUND: Metabolic syndrome (MetS) is an obesity-driven condition of pandemic proportions that increases the risk of type 2 diabetes and cardiovascular disease. Pathophysiological mechanisms are poorly understood, though inflammation has been implicated in MetS pathogenesis. The aim of this study was to assess the effects of galantamine, a centrally acting acetylcholinesterase inhibitor with antiinflammatory properties, on markers of inflammation implicated in insulin resistance and cardiovascular risk, and other metabolic and cardiovascular indices in subjects with MetS...
July 20, 2017: JCI Insight
https://www.readbyqxmd.com/read/28711758/assessing-the-binding-of-cholinesterase-inhibitors-by-docking-and-molecular-dynamics-studies
#6
M Rejwan Ali, Mostafa Sadoqi, Simon G Møller, Allal Boutajangout, Mihaly Mezei
In this report we assessed by docking and molecular dynamics the binding mechanisms of three FDA-approved Alzheimer drugs, inhibitors of the enzyme acetylcholinesterase (AChE): donepezil, galantamine and rivastigmine. Dockings by the softwares Autodock-Vina, PatchDock and Plant reproduced the docked conformations of the inhibitor-enzyme complexes within 2Å of RMSD of the X-ray structure. Free-energy scores show strong affinity of the inhibitors for the enzyme binding pocket. Three independent Molecular Dynamics simulation runs indicated general stability of donepezil, galantamine and rivastigmine in their respective enzyme binding pocket (also referred to as gorge) as well as the tendency to form hydrogen bonds with the water molecules...
June 29, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28705297/the-diagnosis-and-treatment-of-behavioral-disorders-in-dementia
#7
Torsten Kratz
BACKGROUND: Behavioral disorders such as aggressiveness, agitation, delusions, disinhibition, affect lability, and apathy arise in more than 90% of patients with dementia. Behavioral disorders are a major challenge and the greatest stress factor in everyday life for nursing personnel and for family members caring for the patient. METHODS: This review is based on relevant publications retrieved by a selective literature search in the PubMed, Cochrane Library, and German S3 guideline databases with the search terms "behavioral disorders," "non-cognitive disorders," and "challenging behavior," in conjunction with "dementia" and "behavioral and psychological symptoms of dementia...
June 30, 2017: Deutsches Ärzteblatt International
https://www.readbyqxmd.com/read/28684359/significance-of-the-nicotinic-alpha7-receptor-in-cognition-and-antipsychotic-like-behavior-in-the-rat
#8
Marie-Louise G Wadenberg, Dina Manetti, Maria Novella Romanelli, Hugo R Arias
Schizophrenic (SCH) patients show cognitive impairment in attentional performance. Positive allosteric modulators (PAMs) of α7 nicotinic acetylcholine receptors (nAChRs) such as the Alzheimer's drug galantamine (GAL) and PAM-2 are documented to have pro-cognitive properties. However, it is not well established if these properties would be lost, or may hamper antipsychotic efficacy, when given as an adjunct to an antipsychotic which is needed for managing psychotic symptoms. Using adult male Wistar rats, we here investigated the effects of: a) GAL, alone or co-administered with the antipsychotic risperidone (RISP), on acute phencyclidine (PCP)-induced deficits in the attentional set-shifting (ASST) test; b) PAM-2, alone and co-administered with RISP, in the conditioned avoidance response (CAR) test for antipsychotic activity...
July 3, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28678552/acetylcholinesterase-inhibitors-for-treating-dementia-symptoms-a-safety-evaluation
#9
Dana Mohammad, Parco Chan, Janelle Bradley, Krista Lanctôt, Nathan Herrmann
The prevalence of Alzheimer's disease (AD) continues to rise, while treatment options for cognitive impairment are limited. Acetylcholinesterase inhibitors (AChEIs) aim to provide symptomatic benefit for cognitive decline, however these drugs are not without adverse events (AEs). The safety profile of each drug must be taken carefully into consideration before being prescribed, as new dosages and formulations have recently been approved. Areas Covered: Donepezil, galantamine and rivastigmine are the three AChEIs approved for the treatment of varying stages of AD...
July 5, 2017: Expert Opinion on Drug Safety
https://www.readbyqxmd.com/read/28673719/newly-developed-drugs-for-alzheimer-s-disease-in-relation-to-energy-metabolism-cholinergic-and-monoaminergic-neurotransmission
#10
REVIEW
Jan Korábečný, Eugenie Nepovimová, Tereza Cikánková, Katarína Špilovská, Lucie Vašková, Eva Mezeiová, Kamil Kuča, Jana Hroudová
Current options for Alzheimer's disease (AD) treatment are based on administration of cholinesterase inhibitors (donepezil, rivastigmine, galantamine) and/or memantine, acting as an N-methyl-D-aspartate (NMDA). Therapeutic approaches vary and include novel cholinesterase inhibitors, modulators of NMDA receptors, monoamine oxidase (MAO) inhibitors, immunotherapeutics, modulators of mitochondrial permeability transition pores (mPTP), amyloid-beta binding alcohol dehydrogenase (ABAD) modulators, antioxidant agents, etc...
July 1, 2017: Neuroscience
https://www.readbyqxmd.com/read/28645134/-arterial-hyper-and-hypotension-associated-with-psychiatric-medications-a-risk-assessment-based-on-the-summaries-of-product-characteristics-smpcs
#11
Roland W Freudenmann, Ninja Freudenmann, Bartosz Zurowski, Carlos Schönfeldt-Lecuona, Ludwig Maier, Roland E Schmieder, Christian Lange-Asschenfeldt, Maximilian Gahr
Introduction Psychiatric medications are well-known triggers of clinically relevant blood pressure changes. Therefore, we aimed at creating ranking lists for their risk of causing arterial hyper- or hypotension. Methods We analyzed 784 Summaries of Product characteristics (SmPCs, available online from "Rote Liste" or "Gelbe Liste" websites) from 105 psychiatric medications registered in adult psychiatry in Germany and extracted the standardized reported risks of increasing or decreasing arterial blood pressure...
August 2017: Deutsche Medizinische Wochenschrift
https://www.readbyqxmd.com/read/28638340/neurologically-potent-molecules-from-crataegus-oxyacantha-isolation-anticholinesterase-inhibition-and-molecular-docking
#12
Mumtaz Ali, Sultan Muhammad, Muhammad R Shah, Ajmal Khan, Umer Rashid, Umar Farooq, Farhat Ullah, Abdul Sadiq, Muhammad Ayaz, Majid Ali, Manzoor Ahmad, Abdul Latif
Crataegus oxyacantha is an important herbal supplement and famous for its antioxidant potential. The antioxidant in combination with anticholinesterase activity can be considered as an important target in the management of Alzheimer's disease. The compounds isolated from C. oxyacantha were evaluated for cholinesterases inhibitory activity using Ellman's assay with Galantamine as standard drug. Total of nine (1-9) compounds were isolated. Compounds 1 and 2 were isolated for the first time from natural source...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28631100/co-modulation-of-an-allosteric-modulator-of-nicotinic-receptor-cholinesterase-inhibitor-galantamine-and-a-5-ht4-receptor-agonist-rs-67333-effect-on-scopolamine-induced-memory-deficit-in-the-mouse
#13
Thomas Freret, Véronique Lelong-Boulouard, Pierre Lecouflet, Katia Hamidouche, François Dauphin, Michel Boulouard
AIM: It is widely assumed that the upcoming therapeutics for Alzheimer's disease will require to act on more than one target to be effective. We investigated here whether a combination of the nicotinic receptor allosteric modulator/cholinesterase inhibitor galantamine can act synergistically with the type 4 serotonin receptor (5-HT4R) partial agonist, RS-67333, to counterbalance deficits in short- and long-term memory. To select sub-efficacious doses of both drugs, dose-response studies were first performed on the scopolamine-induced deficits of spontaneous alternation in the Y-maze task and of acquisition and retrieval processes in a passive avoidance task...
June 19, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28625836/molecular-interaction-studies-of-acetylcholinesterase-with-potential-acetylcholinesterase-inhibitors-from-the-root-of-rhodiola-crenulata-using-molecular-docking-and-isothermal-titration-calorimetry-methods
#14
Fa-Jie Li, Yuan Liu, Yuan Yuan, Bin Yang, Zhen-Ming Liu, Lu-Qi Huang
(-)-Epicatechin gallate ((-)-ECG), 1,2,3,4,6-O-pentagalloylglucose (PGG), rhodionin, herbacetin and rhodiosin isolated from the root of Rhodiola crenulata exhibited potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50±5.83 to 2.43±0.34μg/mL. With the aim of explaining the differences in activity of these active ingredients and clarifying how they inhibit AChE, the AChE-inhibitor interactions were further explored using molecular docking and isothermal titration calorimetry (ITC) methods in the present study...
June 16, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28621397/new-bioactive-heteroleptic-copper-ii-carboxylates-structure-enzymatic-and-dna-binding-studies
#15
Afifa Mushtaq, Saqib Ali, Muhammad Tahir, Hammad Ismail, Bushra Mirza, Muhammad Saadiq, Muhammad Haleem, Muhammad Iqbal
Two new binuclear O-bridged copper(II) carboxylates with chemical formulas [Cu2(3-ClC6H4CH2COO)4(phen)2] (1) and [Cu2(3-ClC6H4CH2COO)4(bipy)2] (2) where phen = 1,10-phenanthroline and bipy = 2,2'-bipyridine have been synthesized and characterized by FT-IR, UV-Visible spectroscopy, CHN analysis and single crystal XRD. The results revealed distorted square pyramidal geometry around each copper atom of 1 and 2. The DNA interaction studies showed strong binding with Kb = 5.07 × 103 and 4.62 × 103 M-1 for 1 and 2, respectively...
June 2017: Acta Chimica Slovenica
https://www.readbyqxmd.com/read/28590362/a-randomized-clinical-trial-of-oxytocin-or-galantamine-for-the-treatment-of-negative-symptoms-and-cognitive-impairments-in-people-with-schizophrenia
#16
Robert W Buchanan, Deanna L Kelly, Elaine Weiner, James M Gold, Gregory P Strauss, Maju M Koola, Robert P McMahon, William T Carpenter
PURPOSE/BACKGROUND: Negative symptoms and cognitive impairments tend to co-occur in people with schizophrenia. If their association with each other is due, in part, to shared pathophysiology, then this suggests that a single drug could potentially be effective for both domains. The current study was designed to examine this hypothesis. METHODS/PROCEDURES: Fifty-eight participants with either Diagnostic and Statistical Manual of Mental Disorders, Fourth Edition, Text Revision schizophrenia or schizoaffective disorder entered into a 6-week double-blind, placebo-controlled, double-dummy, randomized clinical trial of intranasal oxytocin and galantamine...
August 2017: Journal of Clinical Psychopharmacology
https://www.readbyqxmd.com/read/28588366/neurocognitive-effect-of-nootropic-drug-brahmi-bacopa-monnieri-in-alzheimer-s-disease
#17
REVIEW
Kaustubh S Chaudhari, Nishant R Tiwari, Rakesh R Tiwari, Rohan S Sharma
Alzheimer's disease (AD) is a progressive neurodegenerative disease of the elderly. The rapid increase in its incidence has necessitated development of newer drugs. Ayurvedic herbal medications are increasingly researched due to their biosafety profile and usefulness in cognitive impairment. In this article, we critically reviewed one such Medhya Rasayana (nootropic drug) Brahmi-derived from extract of Bacopa monnieri (EBm). Studies have shown that EBm promotes free radical scavenger mechanisms and protects cells in prefrontal cortex, hippocampus, and striatum against cytotoxicity and DNA damage implicated in AD...
May 2017: Annals of Neurosciences
https://www.readbyqxmd.com/read/28554861/galantamine-alleviates-senescence-of-u87-cells-induced-by-beta-amyloid-through-decreasing-ros-production
#18
Yan Zhang, Lingling Zhao, Zhaoxuan Wu, Xinxin Chen, Tong Ma
Galantamine, which is currently used in the treatment of Alzheimer's disease (AD), has been shown to exert a neuroprotective effect against beta-amyloid (Aβ) peptide-induced toxicity, a critical component involved in the pathogenesis of AD. The aim of this study was to examine the effects of galantamine on proliferation, senescence and ROS production in a U87 cell line treated with Aβ. With the use of a Cell Counting Kit-8 and β galactosidase staining assay, we observed that galantamine (0.3μM) pretreatment significantly prevented Aβ1-40-induced cell degradation and senescence...
July 13, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28458553/long-term-effect-of-galantamine-on-cognitive-function-in-patients-with-alzheimer-s-disease-versus-a-simulated-disease-trajectory-an-observational-study-in-the-clinical-setting
#19
Ryoko Nakagawa, Takashi Ohnishi, Hisanori Kobayashi, Toshio Yamaoka, Tsutomu Yajima, Ai Tanimura, Toshiya Kato, Kazutake Yoshizawa
BACKGROUND: Long-term maintenance of cognitive function is an important goal of treatment for Alzheimer's disease (AD), but evidence about the long-term efficacy of cholinesterase inhibitors is sparse. To evaluate the long-term efficacy and safety of galantamine for AD in routine clinical practice, we conducted a 72-week post-marketing surveillance study. The effect of galantamine on cognitive function was estimated in comparison with a simulated disease trajectory. PATIENTS AND METHODS: Patients with mild-to-moderate AD received flexible dosing of galantamine (16-24 mg/day) during this study...
2017: Neuropsychiatric Disease and Treatment
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
#20
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
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