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Physostigmine

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https://www.readbyqxmd.com/read/29173156/identification-of-human-acetylcholine-esterase-inhibitors-from-the-constituents-of-egb761-by-modeling-docking-and-molecular-dynamics-simulations
#1
Lihu Zhang, Dongdong Li, Fuliang Cao, Wei Xiao, Linguo Zhao, Zhenzhong Wang, Gang Ding
EGb761, a standardized and well-defined product extract of Ginkgo biloba leaves, has beneficial effects on the treatment of multiple diseases, particularly Alzheimer's disease (AD). Identification of natural acetylcholine esterase (AChE) inhibitors from EGb761 would provide a novel therapeutic approach against the Alzheimer's disease. A series of 21 kinds of promising EGB761 compounds were selected, and subsequently evaluated for their potential ability to bind AChE enzyme by molecular docking and a deep analysis of protein surface pocket features...
November 23, 2017: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/29167930/planarian-cholinesterase-molecular-and-functional-characterization-of-an-evolutionarily-ancient-enzyme-to-study-organophosphorus-pesticide-toxicity
#2
Danielle Hagstrom, Siqi Zhang, Alicia Ho, Eileen S Tsai, Zoran Radić, Aryo Jahromi, Kelson J Kaj, Yingtian He, Palmer Taylor, Eva-Maria S Collins
The asexual freshwater planarian Dugesia japonica has emerged as a medium-throughput alternative animal model for neurotoxicology. We have previously shown that D. japonica are sensitive to organophosphorus pesticides (OPs) and characterized the in vitro inhibition profile of planarian cholinesterase (DjChE) activity using irreversible and reversible inhibitors. We found that DjChE has intermediate features of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Here, we identify two candidate genes (Djche1 and Djche2) responsible for DjChE activity...
November 22, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/29136766/behavioral-and-biochemical-evidences-for-nootropic-activity-of-boldine-in-young-and-aged-mice
#3
Dinesh Dhingra, Kapil Soni
Boldine, a bioactive compound, has been reported to be neuroprotective, but its effect on learning and memory has not been explored. So, the present study was aimed to study the effect of boldine on the learning and memory of the Swiss albino male young and aged mice. Boldine (1.5, 3 and 6mg/kg, po) and physostigmine salicylate (0.1mg/kg, ip) were administered to separate groups of mice for 7 successive days. Morris water maze was utilized as a behavioural model to study the effect of drugs on learning and memory of mice...
November 6, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29126416/adjunctive-use-of-physostigmine-salicylate-anticholium%C3%A2-in-perioperative-sepsis-and-septic-shock-study-protocol-for-a-randomized-double-blind-placebo-controlled-monocentric-trial-anticholium%C3%A2-per-se
#4
Johannes B Zimmermann, Nadine Pinder, Thomas Bruckner, Monika Lehmann, Johann Motsch, Thorsten Brenner, Torsten Hoppe-Tichy, Stefanie Swoboda, Markus A Weigand, Stefan Hofer
BACKGROUND: Severe sepsis and septic shock remain a major challenge, even in modern intensive care. In Germany, about 68,000 patients die annually because of septic diseases, characterized by a complex systemic inflammatory response. Causal treatment of the underlying infection is essential for successful management of sepsis, but the course can be positively influenced by supportive and adjuvant measures. The cholinergic anti-inflammatory pathway (CAP) represents a new approach to adjunctive therapy of septic diseases and can be pharmacologically activated by the acetylcholinesterase inhibitor physostigmine (Anticholium®)...
November 10, 2017: Trials
https://www.readbyqxmd.com/read/29122691/sexually-diergic-hypothalamic-pituitary-adrenal-axis-responses-to-selective-and-non-selective-muscarinic-antagonists-prior-to-cholinergic-stimulation-by-physostigmine-in-rats
#5
Marissa A Smail, Jessica L Soles, Tracy E Karwoski, Robert T Rubin, Michael E Rhodes
Central cholinergic systems regulate the hypothalamic-pituitary-adrenal (HPA) axis differentially in males and females (sexual diergism). We previously investigated the role of muscarinic receptors in this regulation by administering physostigmine (PHYSO), an acetylcholinesterase inhibitor, to male and female rats pretreated with scopolamine (SCOP), a nonselective muscarinic antagonist. SCOP pretreatment enhanced adrenocorticotropic hormone (ACTH) and corticosterone (CORT) responses in both sexes; males had greater ACTH responses while females had greater CORT responses...
November 7, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/29119218/odor-cueing-during-slow-wave-sleep-benefits-memory-independently-of-low-cholinergic-tone
#6
Jens G Klinzing, Sabine Kugler, Surjo R Soekadar, Björn Rasch, Jan Born, Susanne Diekelmann
RATIONALE: Sleep-dependent memory consolidation depends on the concerted reactivation of memories in the hippocampo-neocortical system. The communication of reactivated information from the hippocampus to the neocortex is assumed to be enabled by low levels of acetylcholine, particularly during slow-wave sleep (SWS). Recent studies suggest that the reactivation of memories does not only occur spontaneously but can also be externally triggered by re-presenting learning-associated cues during sleep...
November 8, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/29081821/flavonoid-composition-and-biological-activities-of-ethanol-extracts-of-caryocar-coriaceum-wittm-a-native-plant-from-caatinga-biome
#7
Daniela Ribeiro Alves, Selene Maia de Morais, Fernanda Tomiotto-Pellissier, Milena Menegazzo Miranda-Sapla, Fábio Roger Vasconcelos, Isaac Neto Goes da Silva, Halisson Araujo de Sousa, João Paulo Assolini, Ivete Conchon-Costa, Wander Rogério Pavanelli, Francisco das Chagas Oliveira Freire
Caryocar coriaceum fruits, found in Brazilian Cerrado and Caatinga, are commonly used as food and in folk medicine, as anti-inflammatory, bactericide, fungicide, leishmanicide, and nematicide. Due to the biological potential of this plant, this study focuses on the evaluation of antifungal and antileishmanial activities, including anticholinesterase and antioxidant tests, correlating with total phenols and flavonoids content. Peel extracts contain higher yield of phenols and flavonoids as analyzed by spectrophotometric methods...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/29073764/retraction-of-an-expeditious-route-to-both-enantiomers-of-all-carbon-quaternary-stereocenters-at-c-3-carbon-of-lactams-via-3-3-sigmatropic-rearrangement-total-synthesis-of-physostigmine
#8
Ganesh Pandey, Jagadish Khamrai, Akash Mishra
No abstract text is available yet for this article.
November 17, 2017: Organic Letters
https://www.readbyqxmd.com/read/28963050/seizure-susceptibility-in-the-app-ps1-mouse-model-of-alzheimer-s-disease-and-relationship-with-amyloid-%C3%AE-plaques
#9
Karen E Reyes-Marin, Angel Nuñez
Alzheimer's disease is a common age associated neurodegenerative disorder associated with an elevated risk of seizures that may be fundamentally connected to cognitive dysfunction. We used 4-9month-old mice of the APP/PS1 mouse model of Alzheimer's disease to study the presence of epileptiform-like discharges and to establish if the amyloid-β plaques affect their generation. The EEG of the APP/PS1 transgenic mice revealed a higher incidence of epileptiform-like discharges i.e. seizure events (interictal spikes, sharp waves, or polyspikes) than in the controls...
December 15, 2017: Brain Research
https://www.readbyqxmd.com/read/28756934/postoperative-anticholinergic-poisoning-concealed-complications-of-a-commonly-used-medication
#10
Xiao Chi Zhang, Natalija Farrell, Thomas Haronian, Jason Hack
BACKGROUND: Scopolamine is a potent anticholinergic compound used commonly for the prevention of postoperative nausea and vomiting. Scopolamine can cause atypical anticholinergic syndromes due to its prominent central antimuscarinic effects. CASE REPORT: A 47-year-old female presented to the emergency department (ED) 20 h after hospital discharge for a right-knee meniscectomy, with altered mental status (AMS) and dystonic extremity movements that began 12 h after her procedure...
October 2017: Journal of Emergency Medicine
https://www.readbyqxmd.com/read/28718647/fecl3-catalyzed-allylation-reactions-onto-3-hydroxy-2-oxindoles-formal-total-syntheses-of-bis-cyclotryptamine-alkaloids-%C3%A2-chimonanthine-and-%C3%A2-folicanthine
#11
Lakshmana K Kinthada, Sai Raghavendra Medisetty, Amarchand Parida, K Naresh Babu, Alakesh Bisai
An FeCl3-catalyzed efficient strategy for the allylation reactions of 3-hydroxy-2-oxindoles with allyltrimethylsilane has been developed. The reaction affords a variety of 2-oxindoles having quaternary center at the pseudobenzylic position in an operationally simple and inexpensive procedure. Control experiments using enantioenriched 3-hydroxy-2-oxindole show that the reaction proceeds through in situ generated 2H-indol-2-one (8). The methodology presents an efficient and concise access to the pyrroloindoline alkaloids (±)-deoxyeseroline (1a), (±)-esermethole (1b), (±)-physostigmine (1c), (±)-phenserine (1d), and (±)-physovenine (1e)...
August 7, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28703024/safety-and-effectiveness-of-physostigmine-a-10-year-retrospective-review
#12
Ann M Arens, Krishna Shah, Suad Al-Abri, Kent R Olson, Tom Kearney
BACKGROUND: Physostigmine has long been recognized as an antidote to reverse anticholinergic delirium. However, its effectiveness, safety profile, and dosing have been disputed. OBJECTIVES: To describe effectiveness, adverse events, and dosing associated with the use of physostigmine to reverse anticholinergic delirium. METHODS: A retrospective cohort study of hospitalized patients reported to a regional poison center system between 2003 and 2012 who received physostigmine to reverse an anticholinergic toxidrome...
July 13, 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28630263/determination-of-the-residues-in-the-extracellular-domain-of-the-nicotinic-%C3%AE-subunit-required-for-the-actions-of-physostigmine-on-neuronal-nicotinic-receptors
#13
Xiaochun Jin, Allison L Germann, Daniel J Shin, Gustav Akk, Joe Henry Steinbach
Physostigmine can potentiate and inhibit neuronal nicotinic receptors, in addition to inhibiting the activity of acetylcholinesterase. We found that receptors containing three copies of the α2 subunit are inhibited by low concentrations of physostigmine in contrast to receptors containing three copies of the α4 subunit that are potentiated. We exploited this observation to determine the regions required for the actions of physostigmine. Chimeric constructs of the α2 and α4 subunits located two regions in the extracellular amino-terminal domain of the subunit: the E loop (a loop of the transmitter-binding domain) and a region closer to the amino-terminus that collectively could completely determine the different effects of physostigmine...
September 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28615883/clinicobiochemical-changes-in-ivermectin-toxicity-in-doberman-pinscher-pups
#14
Sahadeb Dey, Nitin P Kurade, Kishore Lal Khurana, Ananya Dan
This study is based on naturally intoxicated Doberman pinscher pups. Six Doberman pinscher pups were overdosed 50 times of recommended ivermectin dose by the pet owner and presented to Referral Veterinary Polyclinic section of this institute in a state of coma. The pups were unable to hold their head up and had no pupillary reflex. The pups were examined clinically and samples of blood were taken for haemato-biochemical studies, before and after treatment. During intoxication there was marked haemoconcentration, increase in values of serum creatinine phosphokinase, gamma glutamyl transpeptidase but decrease in serum glucose levels...
June 2017: Journal of Parasitic Diseases: Official Organ of the Indian Society for Parasitology
https://www.readbyqxmd.com/read/28571775/critical-role-of-ca1-muscarinic-receptors-on-memory-acquisition-deficit-induced-by-total-tsd-and-rem-sleep-deprivation-rsd
#15
Bibi-Zahra Javad-Moosavi, Gholamhassan Vaezi, Mohammad Nasehi, Seyed-Ali Haeri-Rouhani, Mohammad-Reza Zarrindast
AIM: Despite different theories regarding sleep physiological function, an overall census indicates that sleep is useful for neural plasticity which eventually strengthens cognition and brain performance. Different studies show that sleep deprivation (SD) leads to impaired learning and hippocampus dependent memory. According to some studies, cholinergic system plays an important role in sleep (particularly REM sleep), learning, memory, and its retrieval. So this study has been designed to investigate the effect of CA1 Cholinergic Muscarinic Receptors on memory acquisition deficit induced by total sleep deprivation (TSD) and REM sleep deprivation (RSD)...
October 3, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28500787/corticosterone-primes-the-neuroinflammatory-response-to-gulf-war-illness-relevant-organophosphates-independently-of-acetylcholinesterase-inhibition
#16
Alicia R Locker, Lindsay T Michalovicz, Kimberly A Kelly, Julie V Miller, Diane B Miller, James P O'Callaghan
Gulf War Illness (GWI) is a chronic multi-symptom disorder affecting veterans of the 1991 Gulf War. Among the symptoms of GWI are those associated with sickness behavior, observations suggestive of underlying neuroinflammation. We have shown that exposure of mice to the stress hormone, corticosterone (CORT), and to diisopropyl fluorophosphate (DFP), as a nerve agent mimic, results in marked neuroinflammation, findings consistent with a stress/neuroimmune basis of GWI. Here, we examined the contribution of irreversible and reversible acetylcholinesterase (AChE) inhibitors to neuroinflammation in our mouse model of GWI...
August 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28499986/n-acetylcysteine-treatment-attenuates-the-cognitive-impairment-and-synaptic-plasticity-loss-induced-by-streptozotocin
#17
Michael da Costa, Jamile Bernardi, Lidiane Costa, Tiago Fiuza, Ricardo Brandão, Maria F Ribeiro, Joana D Amaral, Cecília M P Rodrigues, Maria E Pereira
Alzheimer's disease (AD) is a neurodegenerative disorder pathologically characterized by severe neuronal and glial structural changes and progressive cognitive decline. N-acetylcysteine (NAC) is a well-known pharmacological agent with pro-neurogenic properties and neuroprotective effects. In this study, we evaluated NAC protective effects on cognitive impairment and associated pathological markers in a streptozotocin (STZ)-induced sporadic dementia of AD type mice model. Animals were divided into six groups: I) Sham, II) NAC, III) physostigmine (PHY), IV) STZ, V) NAC + STZ and VI) PHY + NAC...
June 25, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28445778/the-impact-of-bilateral-vagotomy-on-the-physostigmine-induced-airway-constriction-in-ferrets
#18
Burim Neziri, Armond Daci, Shaip Krasniqi, Ramadan Sopi, Musa A Haxhiu
Vagal innervations have a great role in the respiratory function and are the main route of signal transmission from respiratory neural centers into the trachea and others conducting airways. We have investigated the role of central mechanisms related to vagal neural pathways and the cholinergic outflow in tracheobronchial smooth muscle tone and lung mechanics parameters. Parameters of lung mechanics such as lung resistance (RL), dynamic compliance (Cdyn) and pressure in bypassed tracheal segment (Ptseg) were measured before and after vagotomy and asphyxia test...
August 2017: Respiratory Physiology & Neurobiology
https://www.readbyqxmd.com/read/28373858/enhanced-cholinergic-activity-improves-cerebral-blood-flow-during-orthostatic-stress
#19
Jorge M Serrador, Roy Freeman
Cerebral blood flow (CBF) and consequently orthostatic tolerance when upright depends on dilation of the cerebral vasculature in the face of reduced perfusion pressure associated with the hydrostatic gradient. However, it is still unclear if cholinergic activation plays a role in this dilation. To determine if enhancing central cholinergic activity with the centrally acting acetylcholinesterase inhibitor, physostigmine would increase CBF when upright compared to the peripherally acting acetylcholinesterase inhibitor, neostigmine, or saline...
2017: Frontiers in Neurology
https://www.readbyqxmd.com/read/28294544/identification-of-acetylcholinesterase-inhibitors-using-homogenous-cell-based-assays-in-quantitative-high-throughput-screening-platforms
#20
Shuaizhang Li, Ruili Huang, Samuel Solomon, Yitong Liu, Bin Zhao, Michael F Santillo, Menghang Xia
Acetylcholinesterase (AChE) is an enzyme responsible for metabolism of acetylcholine, a neurotransmitter associated with muscle movement, cognition, and other neurobiological processes. Inhibition of AChE activity can serve as a therapeutic mechanism, but also cause adverse health effects and neurotoxicity. In order to efficiently identify AChE inhibitors from large compound libraries, homogenous cell-based assays in high-throughput screening platforms are needed. In this study, a fluorescent method using Amplex Red (10-acetyl-3,7-dihydroxyphenoxazine) and the Ellman absorbance method were both developed in a homogenous format using a human neuroblastoma cell line (SH-SY5Y)...
May 2017: Biotechnology Journal
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