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acetylcholinesterase

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https://www.readbyqxmd.com/read/29667149/three-dimensional-reconstructed-eccrine-sweat-glands-with-vascularization-and-cholinergic-and-adrenergic-innervation
#1
Mingjun Zhang, Haihong Li, Liyun Chen, Shuhua Fang, Sitian Xie, Changmin Lin
Functional integrity of the regenerated tissues requires not only structural integrity but also vascularization and innervation. We previously demonstrated that the three-dimensional (3D) reconstructed eccrine sweat glands had similar structures as those of the native ones did, but whether the 3D reconstructed glands possessing vascularization and innervation was still unknown. In the study, Matrigel-embedded eccrine sweat gland cells were implanted under the inguinal skin. Ten weeks post-implantation, the vascularization, and innervation in the 10-week reconstructed eccrine sweat glands and native human eccrine sweat glands were detected by immunofluorescence staining...
April 17, 2018: Journal of Molecular Histology
https://www.readbyqxmd.com/read/29667118/acmt-position-statement-alternative-or-contingency-countermeasures-for-acetylcholinesterase-inhibiting-agents
#2
Andrew Stolbach, Vikhyat Bebarta, Michael Beuhler, Shaun Carstairs, Lewis Nelson, Michael Wahl, Paul M Wax, Charles McKay
First responders and health care providers must prepare to provide care for patients poisoned by acetylcholinesterase (AchE) inhibitor chemical warfare agents or pesticides. However, pre-deployed medical countermeasures (MCMs) may not be sufficient due to production and delivery interruption, rapid depletion of contents during a response, expiration of MCM components, or lack of local availability of approved MCMs. To augment supplies of community-based and forward-deployed nerve agent countermeasures, the American College of Medical Toxicology (ACMT) supports several strategies: (1) The use of expired atropine, diazepam, and pralidoxime auto-injectors and vials if non-expired drugs are unavailable; and (2) Investigation, development, and identification of alternative countermeasures-commonly stocked drugs that are not approved for nerve agent poisoning but are in the same therapeutic class as approved drugs...
April 17, 2018: Journal of Medical Toxicology: Official Journal of the American College of Medical Toxicology
https://www.readbyqxmd.com/read/29666099/collapse-in-the-elderly-rivastigmine-induced-heart-block-and-a-literature-review-of-the-pharmacology-of-acetylcholinesterase-inhibitors-used-in-alzheimer-s-disease
#3
Olushola Alonge, Fahad Mujtaba Iqbal, Elzbieta Cifonelli
Falls resulting in neck of femur fractures are common in the elderly. Often multiple comorbidities can make management and diagnosis of such a polyfactorial condition difficult, particularly with Alzheimer's dementia (AD). Indeed, poorly managed AD may contribute to falls. We present our management of an 87-year-old woman, on rivastigmine for AD, who presented with a collapse episode-attributed to rivastigmine-resulting in a neck of femur fracture. Furthermore, we perform a literature review of the pharmacology of acetylcholinesterase inhibitors and how their use in AD may contribute to bradyarrhythmias...
April 17, 2018: BMJ Case Reports
https://www.readbyqxmd.com/read/29665406/sn56-neuronal-cell-death-after-24-h-and-14-days-chlorpyrifos-exposure-through-glutamate-transmission-dysfunction-increase-of-gsk-3%C3%AE-enzyme-%C3%AE-amyloid-and-tau-protein-levels
#4
Paula Moyano, María Teresa Frejo, María José Anadon, José Manuel García, María Jesús Díaz, Margarita Lobo, Emma Sola, Jimena García, Javier Del Pino
Chlorpyrifos (CPF) is an organophosphate insecticide described to induce cognitive disorders, both after acute and repeated administration. However, the mechanisms through which it induces these effects are unknown. CPF has been reported to produce basal forebrain cholinergic neuronal cell death, involved on learning and memory regulation, which could be the cause of such cognitive disorders. Neuronal cell death was partially mediated by oxidative stress generation, P75NTR and α7 -nAChRs gene expression alteration triggered through acetylcholinesterase (AChE) variants disruption, suggesting other mechanisms are involved...
April 14, 2018: Toxicology
https://www.readbyqxmd.com/read/29664277/nerve-agents-what-they-are-how-they-work-how-to-counter-them
#5
Stefano Costanzi, John-Hanson Machado, Moriah Mitchell
Nerve agents are organophosphorus chemical warfare agents that exert their action through the irreversible inhibition of acetylcholinesterase, with a consequent overstimulation of cholinergic transmission followed by its shutdown. Beyond warfare, they have notoriously been employed in acts of terrorism as well as high profile assassinations. After a brief historical introduction on the development and deployment of nerve agents, this review provides a survey of their chemistry, the way they affect cholinergic transmission, the available treatment options, and the current directions for their improvement...
April 17, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29663860/novel-coumarin-derivatives-as-potent-acetylcholinesterase-inhibitors-insight-into-efficacy-mode-and-site-of-inhibition
#6
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/29660899/plasma-exosome-levels-in-non-small-cell-lung-cancer-correlation-with-clinicopathological-features-and-prognostic-implications
#7
Qingyun Liu, Ying Xiang, Shuai Yuan, Weijia Xie, Chengying Li, Zeyao Hu, Ying Xiang, Na Wu, Long Wu, Zubin Yu, Li Bai, Yafei Li
BACKGROUND: Biomarker studies revealed important clinical significance of exosome for cancer patients. However, there is currently no consensus on exosome quantification methods. METHODS: Bicinchoninic acid (BCA) method, acetylcholinesterase (AChE) method and nanoparticle tracking analysis (NTA) were utilized to quantify 20 plasma exosome samples, and interrelations between these three methods were explored. Associations of plasma exosome levels with characteristics and prognosis of 208 non-small-cell lung cancer (NSCLC) patients were investigated...
April 3, 2018: Cancer Biomarkers: Section A of Disease Markers
https://www.readbyqxmd.com/read/29660616/intestinal-damage-neurotoxicity-and-biochemical-responses-caused-by-tris-2-chloroethyl-phosphate-and-tricresyl-phosphate-on-earthworm
#8
Yang Yang, Yao Xiao, Yeqian Chang, Yibin Cui, Göran Klobučar, Mei Li
Organophosphate esters (OPEs) draw growing concern about characterizing the potential risk on environmental health due to its wide usage and distribution. Two typical types of organophosphate esters (OPEs): tris (2-chloroethyl) phosphate (TCEP) and tricresyl phosphate (TCP) were selected to evaluate toxicity of OPEs to the soil organism like earthworm (Eisenia fetida). Histopathological examination (H&E), oxidative stress, DNA damage and RT-qPCR was used to identify the effects and potential mechanism of their toxicity...
April 13, 2018: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/29660615/biochemical-and-molecular-alterations-in-freshwater-mollusks-as-biomarkers-for-petroleum-product-domestic-heating-oil
#9
Ali Abdulhamza Al-Fanharawi, Adel M Rabaa, Ayad M J Al-Mamoori
To investigate the effect one of the oil products, domestic heating oil (DHO), on freshwater mollusks, Unio tigridis and Viviparous bengalensis were exposed to three DHO concentrations for each species (5.8, 8.7, and 17.4 ml L-1 for mussels; 6.5, 9.7, and 19.5 mlL-1 for snails, respectively). Antioxidant enzymes (superoxide dismutase, catalase), malondialdehyde, acetylcholinesterase and DNA damage in both species tissues were monitored over 21 days. The results showed that both antioxidant enzymes concentration (SOD and CAT) increased in the lowest DHO concentrations (5...
April 13, 2018: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/29660609/aflatoxin-b-1-contaminated-diet-disrupts-the-blood-brain-barrier-and-affects-fish-behavior-involvement-of-neurotransmitters-in-brain-synaptosomes
#10
Matheus D Baldissera, Carine F Souza, Carla Cristina Zeppenfeld, Sharine N Descovi, Karen Luise S Moreira, Maria Izabel U M da Rocha, Marcelo L da Veiga, Aleksandro S da Silva, Bernardo Baldisserotto
It is known that the cytotoxic effects of aflatoxin B1 (AFB1 ) in endothelial cells of the blood-brain barrier (BBB) are associated with behavioral dysfunction. However, the effects of a diet contaminated with AFB1 on the behavior of silver catfish remain unknown. Thus, the aim of this study was to evaluate whether an AFB1 -contaminated diet (1177 ppb kg feed-1 ) impaired silver catfish behavior, as well as whether disruption of the BBB and alteration of neurotransmitters in brain synaptosomes are involved...
April 4, 2018: Environmental Toxicology and Pharmacology
https://www.readbyqxmd.com/read/29658111/architectonic-characteristics-of-the-visual-thalamus-and-superior-colliculus-in-titi-monkeys
#11
Mary Kl Baldwin, Leah Krubitzer
Titi monkeys are arboreal, diurnal New World monkeys whose ancestors were the first surviving branch of the New World radiation. In the current study, we use cytoarchtectonic and immunohistochemical characteristics to compare subcortical structures associated with visual processing with those of other well-studied primates. Our goal was to appreciate features that are similar across all New World monkeys, and primates in general, versus those features that are unique to titi monkeys and other primate taxa. We examined tissue stained for Nissl substance, cytochrome oxidase (CO), acetylcholinesterase (AChE), calbindin (Cb), parvalbumin (Pv), and vesicular glutamate transporter 2 (VGLUT2) to characterize the superior colliculus, lateral geniculate nucleus, and visual pulvinar...
April 15, 2018: Journal of Comparative Neurology
https://www.readbyqxmd.com/read/29656653/derivatization-molecular-docking-and-in-vitro-acetylcholinesterase-inhibitory-activity-of-glycyrrhizin-as-a-selective-anti-alzheimer-agent
#12
Fatma M Abdel Bar, Diaaeldin M Elimam, Amira S Mira, Fardous F El-Senduny, Farid A Badria
Acetylcholinesterase inhibitors (AChE-Is) increase both level and duration of action of acetylcholine (ACh); thus, alleviate symptoms of Alzheimer's disease (AD). Glycyrrhizin, is the main active compound in liquorice root. Its aglycone, glycyrrhetinic acid, has shown several beneficial pharmacological activities. This study reports the synthesis and screening of a series of glycyrrhetinic acid analogs as AChE-Is. Fourteen derivatives were prepared, of which five derivatives are recorded as new viz., 3-phenyl-carbamoyl-18β-glycyrrhetinic acid (J9), 3-acetyl-18β-glycyrrhetinic-30-anilinamide (J10), 3-acetyl-18β-glycyrrhetinic-30-ethanolamide (J11), 3-acetyl-18β-glycyrrhetinic-30-n-butylamide (J12) and 18β-glycyrrhetinic acid-30-prenyl ester (J14), in addition to nine known derivatives (J1-J8 & J13)...
April 16, 2018: Natural Product Research
https://www.readbyqxmd.com/read/29655693/molecular-modeling-and-in-vitro-approaches-towards-cholinesterase-inhibitory-effect-of-some-natural-xanthohumol-naringenin-and-acyl-phloroglucinol-derivatives
#13
Ilkay Erdogan Orhan, Dariusz Jedrejek, F Sezer Senol, Ramin Ekhteiari Salmas, Serdar Durdagi, Iwona Kowalska, Lukasz Pecio, Wieslaw Oleszek
BACKGROUND: Many natural products, particularly phenolic compounds, have been reported to have a strong inhibition against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), the key enzymes in the pathology of Alzheimer's disease (AD). HYPOTHESIS: Therefore, we hypothesized that some xanthahumol, naringenin, and acyl phloroglucinol derivatives (1-14) isolated from Humulus lupulus L. (hops) may have an inhibitory potential against AChE and BChE. METHODS: Inhibitory potential of compounds 1-14 were tested against AChE and BChE using ELISA microtiter assay...
March 15, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/29655452/treatment-of-myasthenia-gravis
#14
REVIEW
Constantine Farmakidis, Mamatha Pasnoor, Mazen M Dimachkie, Richard J Barohn
With specialized care, patients with myasthenia gravis can have very good outcomes. The mainstays of treatment are acetylcholinesterase inhibitors, and immunosuppressive and immunomodulatory therapies. There is good evidence thymectomy is beneficial in thymomatous and nonthymomatous disease. Nearly all of the drugs used for MG are considered "off-label." The 2 exceptions are acetylcholinesterase inhibitors and complement inhibition with eculizumab, which was recently approved by the US Food and Drug Administration for myasthenia gravis...
May 2018: Neurologic Clinics
https://www.readbyqxmd.com/read/29653427/potential-of-portuguese-vine-shoot-wastes-as-natural-resources-of-bioactive-compounds
#15
Manuela M Moreira, M Fátima Barroso, João Vasconcellos Porto, M J Ramalhosa, Jaroslava Švarc-Gajić, Letícia Estevinho, Simone Morais, Cristina Delerue-Matos
Since annually a high amount of wastes is produced in vine pruning, the aim of this study was to evaluate the potential of vine shoots from two Portuguese grape varieties (Touriga Nacional - TN and Tinta Roriz - TR) to be used as a natural source of phenolic compounds. To reach this goal, three techniques were explored, namely microwave-assisted extraction (MAE), subcritical water extraction (SWE) and conventional extraction (CE). The phenolic composition of the extracts, antioxidant and biological activities were evaluated by spectrophotometry and chromatography...
April 10, 2018: Science of the Total Environment
https://www.readbyqxmd.com/read/29652789/terpenoids-from-the-soft-coral-sinularia-sp-collected-in-yongxing-island
#16
Guo-Fei Qin, Xu-Li Tang, Yan-Ting Sun, Xiang-Chao Luo, Jing Zhang, Leen van Ofwegen, Ping-Jyun Sung, Ping-Lin Li, Guo-Qiang Li
Three new sesquiterpenoids (sinuketal ( 1 ), sinulins A and B ( 2 and 3 )) and two new cembranoids (sinulins C and D ( 4 and 5 )), as well as eight known sesquiterpenoids ( 6–13 ) and eight known cembranoids ( 14–21 ), were isolated from the Xisha soft coral Sinularia sp. Their structures were elucidated by extensive spectroscopic analysis. Compound 1 possesses an unprecedented isopropyl-branched bicyclo [6.3.0] undecane carbon skeleton with unique endoperoxide moiety, and a plausible biosynthetic pathway of it was postulated...
April 13, 2018: Marine Drugs
https://www.readbyqxmd.com/read/29652477/targeted-nanoparticles-for-selective-marking-of-neuromuscular-junctions-and-ex-vivo-monitoring-of-endogenous-acetylcholine-hydrolysis
#17
Alsu R Mukhametshina, Svetlana V Fedorenko, Alexey M Petrov, Guzel F Zakyrjanova, Konstantin A Petrov, Leniz F Nurullin, Irek R Nizameev, Asiya R Mustafina, Oleg G Sinyashin
The present work for the first time introduces nanosensors for luminescent monitoring of acetylcholinesterase (AChE)-catalyzed hydrolysis of endogenous acetylcholine (AСh) released in neuromuscular junctions of isolated muscles. The sensing function results from the quenching of Tb(III)-centered luminescence due to proton-induced degradation of luminescent Tb(III) complexes doped into silica nanoparticles (SNs, 23 nm), when acetic acid is produced from the enzymatic hydrolysis of ACh. The targeting of the silica nanoparticles by α-bungarotoxin was used for selective staining of the synaptic space in the isolated muscles by the nanosensors...
April 13, 2018: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/29652131/thioflavin-t-interaction-with-acetylcholinesterase-new-evidence-of-1-1-binding-stoichiometry-obtained-with-samples-prepared-by-equilibrium-microdialysis
#18
Anna I Sulatskaya, Georgy N Rychkov, Maksim I Sulatsky, Natalia P Rodina, Irina M Kuznetsova, Konstantin K Turoverov
The aim of the present work was investigation of the fluorescent dye thioflavin T (ThT) binding to acetylcholinesterase (AChE). ThT is an effectively used test for the protease activity, as well as a probe for amyloid fibril formation. Despite the extended and active investigation of the ThT - AChE binding, there is still no common view on the stoichiometry of this interaction. In particular, there is a hypothesis explaining the spectral properties of the bound to AChE dye and high quantum yield of its fluorescence by formation of dimers or excimers of ThT...
April 13, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29651948/therapeutic-potential-of-multifunctional-tacrine-analogues
#19
Maja Przybylowska, Szymon Kowalski, Krystyna Dzierzbicka, Iwona Inkielewicz-Stepniak
Tacrine is a potent inhibitor of cholinesterases (acetylcholinesterase and butyrylcholinesterase) that shows limiting clinical application by liver toxicity. In spite of this, analogues of tacrine are considered as model inhibitor of cholinesterases in the therapy of Alzheimer's disease. The interest in these compounds is mainly related to a high variety of their structure and biological properties. In the present review, we have described the role of cholinergic transmission and treatment strategies in Alzheimer's disease as well as the synthesis and biological activity of several recently developed classes of multifunctional tacrine analogues and hybrids, which consist a new paradigm to treat Alzheimer's disease...
April 11, 2018: Current Neuropharmacology
https://www.readbyqxmd.com/read/29651884/kinetic-and-structural-studies-on-the-interactions-of-torpedo-californica-acetylcholinesterase-with-two-donepezil-like-rigid-analogues
#20
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
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