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acetylcholinesterase

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https://www.readbyqxmd.com/read/28728120/cadmium-and-high-temperature-effects-on-brain-and-behaviour-of-lymantria-dispar-l-caterpillars-originating-from-polluted-and-less-polluted-forests
#1
Vesna Perić-Mataruga, Branka Petković, Larisa Ilijin, Marija Mrdaković, Slađana Dronjak Čučaković, Dajana Todorović, Milena Vlahović
Insects brain as a part of nervous system is the first-line of fast stress response that integrate stress signals to regulate all aspects of insect physiology and behaviour. The cadmium (Cd) bioaccumulation factor (BF), activity of the neurotoxicity biomarker acetylcholinesterase (AChE), dopamine content, expression and amount of Hsp70 in the brain and locomotor activity were evaluated in the 4th instar of Lymantria dispar L. caterpillars fed a Cd supplemented diet and reared in an optimal temperature regime (23 °C) and/or exposed to high temperature (28 °C)...
July 11, 2017: Chemosphere
https://www.readbyqxmd.com/read/28728106/multipotent-ache-and-bace-1-inhibitors-for-the-treatment-of-alzheimer-s-disease-design-synthesis-and-bio-analysis-of-7-amino-1-4-dihydro-2h-isoquilin-3-one-derivates
#2
Xiong-Jie Zhao, Da-Min Gong, Yu-Ren Jiang, Dong Guo, Yao Zhu, You-Chao Deng
In this paper, the preparation of a new class of multi-target-directed ligands (MTDLs) based on a 7-amino-1,4-dihydro-2H-isoquilin-3-one, whose lead (compound I) showed promising properties in acetylcholinesterase (AChE) inhibitory activity [1], is described. The results of in vitro activities and molecular docking demonstrated that the target molecule (compounds 10a-n) with three parts of aromatic moieties and appropriate structural length can interact with aromatic residues in catalytic active site (CAS), peripheral anionic site (PAS) and the channel of AChE...
July 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28727975/appendicular-biopsy-in-total-colonic-aganglionosis-a-histologically-challenging-and-inadvisable-practice
#3
Suravi Mohanty, Usha Kini, Kanishka Das, Divya Puttegowda, Lokendra Yadav, Manjally Kunjipapu Babu, Kiran Mahadevappa, Prasanna Kumar, Shubha Attibele Mahadevaiah, Mainak Deb
Background The reliability of intraoperative evaluation of ganglion cells in the appendix as a guide to a diagnosis of total colonic aganglionosis is unclear. Objective To evaluate the diagnostic utility of appendicular innervation in colonic Hirschsprung disease (HD) and TCA. Methods Prospective, systematic study of ganglion cells and the neural plexii in appendices from cases (HD and TCA) and age matched controls with frozen and paraffin sections, rapid acetylcholinesterase (AChE) and immunohistochemistry...
July 2017: Pediatric and Developmental Pathology
https://www.readbyqxmd.com/read/28726179/methionine-and-or-methionine-sulfoxide-alter-ectoenzymes-activities-in-lymphocytes-and-inflammatory-parameters-in-serum-from-young-rats-acute-and-chronic-effects
#4
Mayara Sandrielly Pereira Soares, Marcelo Zanusso Costa, Tatiane Morgana da Silva, Marta Gazal, Carlus Augustu Tavares do Couto, Gabriela Nogueira Debom, Rodrigo Rodrigues, Juliana Hofstätter Azambuja, Emerson André Casali, Cesar Eduardo Jacintho Moritz, Marta Frescura Duarte, Elizandra Braganhol, Francieli Moro Stefanello, Roselia Maria Spanevello
In this study we investigated the effect of acute and chronic treatment with Met and/or methionine sulfoxide (MetO) on ectonucleotidases and cholinesterases activities from lymphocytes and purine derivatives compounds, C-protein reactive, interleukin-10, interleukin-6, and tumor necrosis factor-α levels in serum of young rats. Adenosine triphosphate hydrolysis was decreased in lymphocytes 1 h after treatment by MetO and Met + MetO. However, adenosine triphosphate and adenosine diphosphate hydrolysis in lymphocytes was increased in the groups MetO and Met + MetO and adenosine deaminase activity was increased in MetO 3 h after the treatment...
July 19, 2017: Cell Biochemistry and Biophysics
https://www.readbyqxmd.com/read/28726034/mentally-stimulating-activities-associate-with-better-cognitive-performance-in-parkinson-disease
#5
Jeffrey L B Bohnen, Martijn L T M Müller, Jacob Haugen, Nicolaas I Bohnen
Subjects at risk of dementia benefit from participation in mentally stimulating activities, but no prior studies have investigated similar associations in Parkinson disease (PD). The aim of this study was to investigate the relationship between times spent engaging in mentally stimulating activities and cognitive functions in PD while accounting for the degree of primary neurodegenerations. PD patients (N = 41, 33 males; age 68.5 ± 7.2; Hoehn and Yahr stage 2.6 ± 0.6) completed the Community Health Activities Model Program for Seniors questionnaire, mini-mental state examination (MMSE), and [(11)C]dihydrotetrabenazine dopaminergic and [(11)C]piperidinyl propionate acetylcholinesterase PET imaging...
July 19, 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/28725146/lc-esi-ms-ms-profiling-of-phenolics-from-eleutherococcus-spp-inflorescences-structure-activity-relationship-as-antioxidants-inhibitors-of-hyaluronidase-and-acetylcholinesterase
#6
Daniel Załuski, Marta Olech, Rafał Kuźniewski, Robert Verpoorte, Renata Nowak, Helena D Smolarz
Nature is a source of many plant-based molecules used as pro- or drugs. Eleutherococcus species are native to Asia and the North Russia, and are traditionally used to treat various diseases. In turn, neither secondary metabolites of the species cultivated in the West Europe nor the bioactivity is known. No differences in the phenols and flavonoids content in the inflorescences were found. The richest in polyphenols was E. giraldii (5.18 mg/g), while in flavonoids it was E. gracilistylus (1.80 mg/g). Using LC-ESI-MS/MS, protocatechuic and trans-caffeic acids have been identified as the most abundant compounds in E...
July 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28724799/galantamine-alleviates-inflammation-and-insulin-resistance-in-patients-with-metabolic-syndrome-in-a-randomized-trial
#7
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/28724203/huprine-x-attenuates-the-neurotoxicity-induced-by-kainic-acid-especially-brain-inflammation
#8
J Relat, B Pérez, P Camps, D Muñoz-Torrero, A Badia, M V Clos
Huprine X (HX) is a synthetic anticholinesterasic compound that exerts a potent inhibitory action on acetylcholinesterase (AChE) activity, an agonist effect on cholinergic receptors, neuroprotective activity in different neurotoxicity models in vivo and in vitro and cognition enhancing effects in non-transgenic (C57BL/6) and transgenic (3xTg-AD, APPswe) mice. In the present study, we assessed the ability of HX (0.8 mg/kg, 21 days) to prevent the damage induced by kainic acid (KA; 28 mg/kg) regarding apoptosis, glia reactivity and neurogenesis in mouse brain...
July 19, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28723617/small-molecular-floribundiquinone-b-derived-from-medicinal-plants-inhibits-acetylcholinesterase-activity
#9
Bing Niu, Mengying Zhang, Pu Du, Li Jiang, Rui Qin, Qiang Su, Fuxue Chen, Dongshu Du, Yilai Shu, Kuo-Chen Chou
Being a neurodegenerative disorder, Alzheimer's disease (AD) is the one of the most terrible diseases. And acetylcholinesterase (AChE) is considered as an important target for treating AD. Acetylcholinesterase inhibitors (AChEI) are considered to be one of the effective drugs for the treatment of AD. The aim of this study is to find a novel potential AChEI as a drug for the treatment of AD. In this study, instead of using the synthetic compounds, we used those extracted from plants to investigate the interaction between floribundiquinone B (FB) and AChE by means of both the experimental approach such as fluorescence spectra, ultraviolet-visible (UV-vis) absorption spectrometry, circular dichroism (CD) and the theoretical approaches such as molecular docking...
July 11, 2017: Oncotarget
https://www.readbyqxmd.com/read/28723196/label-free-homogeneous-electroanalytical-platform-for-pesticide-detection-based-on-acetylcholinesterase-mediated-dna-conformational-switch-integrated-with-rolling-circle-amplification
#10
Xiaojuan Liu, Mengmeng Song, Ting Hou, Feng Li
This study addresses the need for sensitive pesticide assay by reporting a new label-free and immobilization-free homogeneous electroanalytical strategy, which combines acetylcholinesterase (AChE)-catalyzed hydrolysis product-mediated DNA conformational switch and rolling circle amplification (RCA) to detect organophosphorous and carbamate pesticides in a "signal-on" mode. When target pesticides were present, AChE activity was inhibited and could not trigger the following DNA conformational change and the RCA reaction, which results in numerous methylene blue (MB) molecules in a free state, generating a strong electrochemical response...
April 28, 2017: ACS Sensors
https://www.readbyqxmd.com/read/28722471/simulated-annealing-molecular-dynamics-and-ligand-receptor-contacts-analysis-for-pharmacophore-modeling
#11
Ma'mon M Hatmal, Mutasem O Taha
AIM: Ligand-based pharmacophore modeling requires long list of inhibitors, while pharmacophores based on single ligand-receptor crystallographic structure can be too restricted or promiscuous. METHODOLOGY: This prompted us to combine simulated annealing molecular dynamics (SAMD) with ligand-receptor contacts analysis as means to construct pharmacophore model(s) from single ligand-receptor complex. Ligand-receptor contacts that survive numerous heating-cooling SAMD cycles are considered critical and are used to guide pharmacophore development...
July 19, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28721486/modulatory-effect-of-lycopene-against-carbofuran-toxicity-in-african-catfish-clarias-gariepinus
#12
Heba S Hamed, Alaa G M Osman
In the current study, African catfish, Clarias gariepinus, was exposed to a sublethal concentration of carbofuran (CF) to investigate its negative effects on biochemical and oxidative stress biomarkers. Also, the putative role of lycopene (LYC) administration in alleviating these negative effects was evaluated. Fish were divided into six groups in triplicates as follows: group I was without treatment, group II was orally administered corn oil, group III was orally administered 18 mg LYC/kg body weight, group IV was exposed to 0...
July 18, 2017: Fish Physiology and Biochemistry
https://www.readbyqxmd.com/read/28720101/drug-candidates-in-clinical-trials-for-alzheimer-s-disease
#13
REVIEW
Shih-Ya Hung, Wen-Mei Fu
Alzheimer's disease (AD) is a major form of senile dementia, characterized by progressive memory and neuronal loss combined with cognitive impairment. AD is the most common neurodegenerative disease worldwide, affecting one-fifth of those aged over 85 years. Recent therapeutic approaches have been strongly influenced by five neuropathological hallmarks of AD: acetylcholine deficiency, glutamate excitotoxicity, extracellular deposition of amyloid-β (Aβ plague), formation of intraneuronal neurofibrillary tangles (NTFs), and neuroinflammation...
July 19, 2017: Journal of Biomedical Science
https://www.readbyqxmd.com/read/28719874/combined-effects-of-temperature-and-clomazone-gamit-%C3%A2-on-oxidative-stress-responses-and-b-esterase-activity-of-physalaemus-nattereri-leiuperidae-and-rhinella-schneideri-bufonidae-tadpoles
#14
Juliane Silberschmidt Freitas, Andreia Arantes Felício, Fabrício Barreto Teresa, Eduardo Alves de Almeida
Temperature is an important factor influencing the toxicity of chemicals in aquatic environments. Neotropical tadpoles experience large temperature fluctuations in their habitats and many species are distributed in areas impacted by agriculture. This study evaluated the effects caused by the exposure to clomazone (Gamit(®)) at different temperatures (28, 32 and 36 °C) on biochemical stress responses and esterase activities in Physalaemus nattereri and Rhinella schneideri tadpoles. Results evidenced that temperature modulates the effects of clomazone on biochemical response of tadpoles...
July 14, 2017: Chemosphere
https://www.readbyqxmd.com/read/28718019/neonatal-placental-and-umbilical-cord-blood-parameters-in-pregnant-women-residing-in-areas-with-intensive-pesticide-application
#15
María Martha Quintana, Berta Vera, Gladis Magnarelli, Natalia Guiñazú, María Gabriela Rovedatti
In rural populations, the proximity to areas with intensive pesticide application represents a risk factor of xenobiotic exposure. Here, we investigated whether newborns born to mothers residing in an area with intensive pesticide application show alterations in placental and neonatal morphometric standards, umbilical cord blood (UCB) biochemical parameters, and/or biomarkers related to oxidative stress and oxidative damage. Samples were collected from 151 healthy pregnant women residing in a rural area (rural group; RG) during the pesticide spraying (SS) and nonspraying (NSS) seasons, as well as from women from an urban population (control group; CG), and grouped according to the delivery type (vaginal or cesarean)...
July 17, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28716085/the-protective-effect-of-fermented-curcuma-longa-l-on-memory-dysfunction-in-oxidative-stress-induced-c6-gliomal-cells-proinflammatory-activated-bv2-microglial-cells-and-scopolamine-induced-amnesia-model-in-mice
#16
Cheong-Su Eun, Jong-Soon Lim, Jihye Lee, Sam-Pin Lee, Seun-Ah Yang
BACKGROUND: Curcuma longa L. is a well-known medicinal plant that has been used for its anti-cancer, neuroprotective, and hepatoprotective effects. However, the neuroprotective effect of fermented C. longa (FCL) has not been reported. Therefore, in this study, the effectiveness of FCL for the regulation of memory dysfunction was investigated in two brain cell lines (rat glioma C6 and murine microglia BV2) and scopolamine-treated mice. METHODS: C. longa powder was fermented by 5% Lactobacillus plantarum K154 containing 2% (w/v) yeast extract at 30 °C for 72 h followed by sterilization at 121 °C for 15 min...
July 17, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28715867/therapeutic-impact-of-grape-leaves-polyphenols-on-certain-biochemical-and-neurological-markers-in-alcl3-induced-alzheimer-s-disease
#17
Ibrahim H Borai, Magda K Ezz, Maha Z Rizk, Hanan F Aly, Mahmoud El-Sherbiny, Azza A Matloub, Ghadha I Fouad
Alzheimer's disease (AD) is a grave and prevailing neurodegenerative disease, characterized by slow and progressive neurodegeneration in different brain regions. Aluminum (Al) is a potent and widely distributed neurotoxic metal, implicated in the neuropathogenesis of AD. This study aimed to evaluate the possible neurorestorative potential of Vitis vinifera Leaves Polyphenolic (VLP) extract in alleviating aluminum chloride (AlCl3)-induced neurotoxicity in male rats. AlCl3 neurotoxicity induced a significant decrease in brain/serum acetylcholine (ACh) contents and serum dopamine (DA) levels, along with a significant increment of brain/serum acetylcholinesterase (AChE) activities...
July 13, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28714400/cholinesterase-inhibitory-activity-of-some-semi-rigid-spiro-heterocycles-pom-analyses-and-crystalline-structure-of-pharmacophore-site
#18
Taibi Ben Hadda, Oualid Talhi, Artur S M Silva, Fatma Sezer Senol, Ilkay Erdogan Orhan, Abdur Rauf, Yahia N Mabkhot, Khaldoun Bachari, Ismail Warad, Thoraya A Farghaly, Ismail I Althagafi, Mohammad S Mubarak
Cholinesterase family consists of two sister enzymes; acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) which hydrolyze acetylcholine. Since deficit of acetylcholine has been evidenced in the patients of Alzheimer's disease (AD), cholinesterase inhibitors are currently the most prescribed drug class for the treatment of AD. In the present study, five compounds (2-6) with spiro skeleton have been synthesized and tested for their inhibitory potential in vitro against AChE and BChE using ELISA microtiter plate assays at 25 mg/mL...
July 13, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28714263/enhancing-methyl-parathion-degradation-by-the-immobilization-of-burkholderia-sp-isolated-from-agricultural-soils
#19
Maikel Gilberto Fernández-López, Carolina Popoca-Ursino, Enrique Sánchez-Salinas, Raunel Tinoco-Valencia, Jorge Luis Folch-Mallol, Edgar Dantán-González, Ma Laura Ortiz-Hernández
Organophosphate pesticides are of great interest for research because they are currently the most commonly used pesticides. In this study, a bacterial strain capable of completely degrading methyl parathion (MP) was isolated from agricultural soils in central Mexico. This strain was designated strain S5-2 and was identified as Burkholderia cenocepacia. To increase degradation yields, cells were immobilized on three different supports: powdered zeolite and Opuntia sp. and Agave sp. fibers. The results indicated a significant increase in MP hydrolysis and p-nitrophenol (PNP) degradation with immobilized cells compared to free cell cultures...
July 17, 2017: MicrobiologyOpen
https://www.readbyqxmd.com/read/28713915/concurrent-administration-of-thyroxine-and-donepezil-induces-plastic-changes-in-the-prefrontal-cortex-of-adult-hypothyroid-rats
#20
Fen Wang, Zhangbi Wu, Xiaoxue Zha, Yaojun Cai, Bo Wu, Xuemei Jia, Defa Zhu
The aim of the present study was to observe the effects of the concurrent administration of thyroxine (T4) and an acetylcholinesterase (AChE) inhibitor, donepezil (DON), on the hypothyroidism‑induced ultrastructural changes of the prefrontal cortex (PFC) in adult rats. The acetylcholine (ACh) content and AChE activity was assessed, as well as the expressions of synaptotagmin‑1 (syt‑1) and SNAP‑25 were analyzed in the rats. Adding 0.05% propylthiouracil to rats' drinking water induced a hypothyroid rat model...
July 14, 2017: Molecular Medicine Reports
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