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https://www.readbyqxmd.com/read/28640711/effects-of-season-and-postmortem-changes-on-blood-analytes-in-pyrenean-chamois-rupicapra-pyrenaica
#1
Asta Tvarijonaviciute, Ignasi Marco, Rafaela Cuenca, Santiago Lavín, Josep Pastor
Our objectives were to evaluate the effects of the 1) season, and 2) postmortem changes on serum biochemistries related with metabolism in Pyrenean chamois (Rupicapra pyrenaica pyrenaica). Serum samples from 98 animals obtained from 2009 to 2012 were included. To investigate seasonal influences on blood parameters, the Pyrenean chamois were captured in drive-nets during the feed abundant (FA; n=32) and food deficient (FD; n=35) seasons. To evaluate the possible differences in biochemistry analytes when sampling live or dead animals, we used serum samples from 32 captured animals and 31 dead animals (obtained during controlled hunting) in the FA season...
June 22, 2017: Journal of Wildlife Diseases
https://www.readbyqxmd.com/read/28632446/multitarget-drug-design-strategy-in-alzheimer-s-disease-focus-on-cholinergic-transmission-and-amyloid-%C3%AE-aggregation
#2
Elena Simoni, Manuela Bartolini, Izuddin F Abu, Alix Blockley, Cecilia Gotti, Giovanni Bottegoni, Roberta Caporaso, Christian Bergamini, Vincenza Andrisano, Andrea Cavalli, Ian R Mellor, Anna Minarini, Michela Rosini
AIM: Alzheimer pathogenesis has been associated with a network of processes working simultaneously and synergistically. Over time, much interest has been focused on cholinergic transmission and its mutual interconnections with other active players of the disease. Besides the cholinesterase mainstay, the multifaceted interplay between nicotinic receptors and amyloid is actually considered to have a central role in neuroprotection. Thus, the multitarget drug-design strategy has emerged as a chance to face the disease network...
June 20, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28632402/3-benzyloxy-1-5-18-f-fluoropentyl-5-nitro-1h-indazole-a-pet-radiotracer-to-measure-acetylcholinesterase-in-brain
#3
Soledad Fernández, Javier Giglio, Ana Laura Reyes, Andrés Damián, Concepción Pérez, Daniel I Pérez, Mercedes González, Patricia Oliver, Ana Rey, Henry Engler, Hugo Cerecetto
AIM: Noninvasive studies of the acetylcholinesterase (AChE) level in Alzheimer's disease (AD) patients can contribute to a better understanding of the disease and its therapeutic. We propose 3-(benzyloxy)-1-(5-[(18)F]fluoropentyl)-5-nitro-1H-indazole, [(18)F]-IND1, structurally related to the AChE-inhibitor CP126,998, as a new positron emission tomography-radiotracer. EXPERIMENTAL: Radiosynthesis, with 18F, stability, lipophilicity and protein binding of [18F]-IND1 were studied...
June 20, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28632395/design-synthesis-and-multitarget-biological-profiling-of-second-generation-anti-alzheimer-rhein-huprine-hybrids
#4
Francisco Javier Pérez-Areales, Nibal Betari, Antonio Viayna, Caterina Pont, Alba Espargaró, Manuela Bartolini, Angela De Simone, José Fernando Rinaldi Alvarenga, Belén Pérez, Raimon Sabate, Rosa Maria Lamuela-Raventós, Vincenza Andrisano, Francisco Javier Luque, Diego Muñoz-Torrero
AIM: Simultaneous modulation of several key targets of the pathological network of Alzheimer's disease (AD) is being increasingly pursued as a promising option to fill the critical gap of efficacious drugs against this condition. MATERIALS & METHODS: A short series of compounds purported to hit multiple targets of relevance in AD has been designed, on the basis of their distinct basicities estimated from high-level quantum mechanical computations, synthesized, and subjected to assays of inhibition of cholinesterases, BACE-1, and Aβ42 and tau aggregation, of antioxidant activity, and of brain permeation...
June 20, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28631839/natural-variability-of-biochemical-biomarkers-in-the-macro-zoobenthos-dependence-on-life-stage-and-environmental-factors
#5
Lucia Scarduelli, Roberto Giacchini, Paolo Parenti, Sonia Migliorati, Agnese Maria Di Brisco, Marco Vighi
Biomarkers are widely used in ecotoxicology as indicators of exposure to toxicants. However, their ability to provide ecologically relevant information remains controversial. One of the major problems is understanding if the measured responses are determined by stress factors or lie within the natural variability range. In a previous work, the natural variability of enzymatic levels in invertebrates sampled in pristine rivers was proved to be relevant across both space and time. In this work, the experimental design was improved by considering different life stages of the selected taxa and by measuring more environmental parameters...
June 20, 2017: Environmental Toxicology and Chemistry
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
#6
Xiaochun Jin, Allison L Germann, Daniel J Shin, Gustav Akk, Joseph H Steinbach
Physostigmine can potentiate and inhibit neuronal nicotinic receptors, in addition to inhibiting the activity of acetylcholinesterase. We found that receptors containing 3 copies of the α2 subunit are inhibited by low concentrations of physostigmine in contrast to receptors containing 3 copies of the α4 subunit that are potentiated. We exploited this observation to determine 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...
June 19, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28629287/anti-acetylcholinesterase-activity-and-antioxidant-properties-of-extracts-and-fractions-of-carpolobia-lutea
#7
Lucky Legbosi Nwidu, Ekramy Elmorsy, Jack Thornton, Buddhika Wijamunige, Anusha Wijesekara, Rebecca Tarbox, Averil Warren, Wayne Grant Carter
CONTEXT: There is an unmet need to discover new treatments for Alzheimer's disease. This study determined the anti-acetylcholinesterase (AChE) activity, DPPH free radical scavenging and antioxidant properties of Carpolobia lutea G. Don (Polygalaceae). OBJECTIVE: The objective of this study is to quantify C. lutea anti-AChE, DPPH free radical scavenging, and antioxidant activities and cell cytotoxicity. MATERIALS AND METHODS: Plant stem, leaves and roots were subjected to sequential solvent extractions, and screened for anti-AChE activity across a concentration range of 0...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28629119/cholinesterase-inhibitory-activities-of-adamantyl-based-derivatives-and-their-molecular-docking-studies
#8
Huey Chong Kwong, Siau Hui Mah, Tze Shyang Chia, Ching Kheng Quah, Gin Keat Lim, C S Chidan Kumar
Adamantyl-based compounds are clinically important for the treatments of type 2 diabetes and for their antiviral abilities, while many more are under development for other pharmaceutical uses. This study focused on the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of adamantyl-based ester derivatives with various substituents on the phenyl ring using Ellman's colorimetric method. Compound 2e with a 2,4-dichloro electron-withdrawing substituent on the phenyl ring exhibited the strongest inhibition effect against AChE, with an IC50 value of 77...
June 17, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28626522/study-of-para-quinone-methide-precursors-toward-the-realkylation-of-aged-acetylcholinesterase
#9
Ryan J Yoder, Qinggeng Zhuang, Jeremy M Beck, Andrew Franjesevic, Travis G Blanton, Sydney Sillart, Tyler Secor, Leah Guerra, Jason D Brown, Carolyn Reid, Craig A McElroy, Özlem Doğan Ekici, Christopher S Callam, Christopher M Hadad
Acetylcholinesterase (AChE) is an essential enzyme that can be targeted by organophosphorus (OP) compounds, including nerve agents. Following exposure to OPs, AChE becomes phosphylated (inhibited) and undergoes a subsequent aging process where the OP-AChE adduct is dealkylated. The aged AChE is unable to hydrolyze acetylcholine, resulting in accumulation of the neurotransmitter in the central nervous system (CNS) and elsewhere. Current therapeutics are only capable of reactivating inhibited AChE. There are no known therapeutic agents to reverse the aging process or treat aged AChE...
June 8, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28625948/anticholinesterase-activity-and-identification-of-huperzine-a-in-three-mexican-lycopods-huperzia-cuernavacensis-huperzia-dichotoma-and-huperzia-linifolia-lycopodiaceae
#10
Mariana Vázquez García, Gilsane Lino von Poser, Miriam Apel, Rosa Cerros Tlatilpa, Aniceto Mendoza-Ruiz, María Luisa Villarreal, Amelia Teresinha Henriques, Alexandre Cardoso Taketa
Huperzine A (Hup A), the alkaloid produced by the Chinese medicinal plant Huperzia serrata, has been documented to be a promising agent for the treatment of Alzheimer's disease due to its potent acetylcholinesterase inhibitory (AChEI) activity. The search for anticholinesterase natural products, as well as for alternative sources of Hup A in Mexican lycopods, prompted us to investigate these plants. The action of methanolic and alkaloidal extracts of three Huperzia species (H. cuernavacensis, H. dichotoma, and H...
January 2017: Pakistan Journal of Pharmaceutical Sciences
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
#11
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 15, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28624507/effect-of-pyridostigmine-on-in-vivo-and-in-vitro-respiratory-muscle-of-mdx-mice
#12
Gabriela de Cássia Sousa Amancio, Andrea Grabe-Guimarães, Dridi Haikel, Johan Moreau, Neila Marcia Silva Barcellos, Alain Lacampagne, Stefan Matecki, Olivier Cazorla
The current work was conducted to verify the contribution of neuromuscular transmission defects at the neuromuscular junction to Duchenne Muscular Dystrophy disease progression and respiratory dysfunction. We tested pyridostigmine and pyridostigmine encapsulated in liposomes (liposomal PYR), an acetylcholinesterase inhibitor to improve muscular contraction on respiratory muscle function in mdx mice at different ages. We evaluated in vivo with the whole-body plethysmography, the ventilatory response to hypercapnia, and measured in vitro diaphragm strength in each group...
June 14, 2017: Respiratory Physiology & Neurobiology
https://www.readbyqxmd.com/read/28621747/novel-tacrine-scutellarin-hybrids-as-multipotent-anti-alzheimer-s-agents-design-synthesis-and-biological-evaluation
#13
Katarina Spilovska, Jan Korabecny, Vendula Sepsova, Daniel Jun, Martina Hrabinova, Petr Jost, Lubica Muckova, Ondrej Soukup, Jana Janockova, Tomas Kucera, Rafael Dolezal, Eva Mezeiova, Daniel Kaping, Kamil Kuca
A novel series of 6-chlorotacrine-scutellarin hybrids was designed, synthesized and the biological activity as potential anti-Alzheimer's agents was assessed. Their inhibitory activity towards human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBChE), antioxidant activity, ability to cross the blood-brain barrier (BBB) and hepatotoxic profile were evaluated in vitro. Among these compounds, hybrid K1383, bearing two methylene tether between two basic scaffolds, was found to be very potent hAChE inhibitor (IC50 = 1...
June 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28621503/ph-responsive-fluorescence-enhancement-in-graphene-oxide-naphthalimide-nanoconjugates-a-fluorescence-turn-on-sensor-for-acetylcholine
#14
Sreejith Mangalath, Silja Abraham, Joshy Joseph
A pH sensitive, fluorescence 'turn on' sensor based on a graphene oxide-naphthalimide nanoconjugate (GO-NI) for the detection of acetylcholine (ACh) by monitoring the enzymatic activity of acetylcholinesterase (AChE) in aqueous solution is reported. These nanoconjugates were synthesized by covalently anchoring picolyl substituted naphthalimide derivatives on GO/rGO surface via EDC-NHS coupling strategy and the morphological and photophysical properties were studied in detail. Synergistic effects of - interactions between GO and naphthalimide chromophore, and efficient photoinduced electron and energy transfer processes are responsible for the strong quenching of fluorescence of these nanoconjugates, which gets perturbed at acidic pH conditions leading to significant enhancement of fluorescence emission...
June 16, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28620187/discovery-and-identification-of-o-o-diethyl-o-4-5-phenyl-4-5-dihydroisoxazol-3-yl-phenyl-phosphorothioate-xp-1408-as-a-novel-mode-of-action-of-organophosphorus-insecticides
#15
Zhigang Zeng, Ying Yan, Bingfeng Wang, Niu Liu, Hanhong Xu
Organophosphorus (OP) insecticides play an important role in pest control. Many OP insecticides have been removed from the market because of their high toxicity to humans. We designed and synthesized a new OP insecticide with the goal of providing a low cost, and less toxic insecticide. The mode of action of O, O-diethyl O-(4-(5-phenyl-4, 5-dihydroisoxazol-3-yl) phenyl) phosphorothioate (XP-1408) was studied in Drosophila melanogaster. Bioassays showed that XP-1408 at a concentration of 50 mg/L delayed larval development...
June 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28619612/improving-the-acetylcholinesterase-inhibitory-effect-of-illigera-henryi-by-solid-state-fermentation-with-clonostachys-rogersoniana
#16
Xue-Jiao Li, Jian-Wei Dong, Le Cai, Rui-Feng Mei, Zhong-Tao Ding
Illigera henryi, an endemic traditional Chinese medicine, contains abundant aporphine alkaloids that possess various bioactivities. In the present study, tubers of I. henryi were fermented by several fungi, and the acetylcholinesterase (AChE) inhibitory activities of non-fermented and fermented I. henryi were measured. The results showed that the fermentation of I. henryi with Clonostachys rogersoniana 828H2 is effective for improving the AChE inhibitory activity. A key biotransformation was found during the C...
June 13, 2017: Journal of Bioscience and Bioengineering
https://www.readbyqxmd.com/read/28619513/myricetin-ameliorates-scopolamine-induced-memory-impairment-in-mice-via-inhibiting-acetylcholinesterase-and-down-regulating-brain-iron
#17
Beiyun Wang, Yuan Zhong, Chengjie Gao, Jingbo Li
The aim of our study was to investigate to investigate the effect of myricetin on Alzheimer's disease (AD) and its underlying mechanisms. In our study, Myricetin effectively attenuated Fe(2+)-induced cell death in SH-SY5Y cells in vitro. In a mouse model of AD, myricetin treatment significantly reversed scopolamine-induced cognitive deficits deriving from a novel action of inhibiting acetylcholinesterase (AChE) and down-regulating brain iron. Furthermore, Myricetin treatment reduced oxidative damage and increased antioxidant enzymes activity in mice...
June 12, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28618655/eugenia-uniflora-fruit-red-type-standardized-extract-a-potential-pharmacological-tool-to-diet-induced-metabolic-syndrome-damage-management
#18
Pathise Souto Oliveira, Vitor Clasen Chaves, Natália Pontes Bona, Mayara Sandrielly Pereira Soares, Juliane de Souza Cardoso, Flávia Aleixo Vasconcellos, Rejane Giacomelli Tavares, Marcia Vizzotto, Luísa Mariano Cerqueira da Silva, Fabiane Borelli Grecco, Giovana Duzzo Gamaro, Roselia Maria Spanevello, Claiton Leoneti Lencina, Flávio Henrique Reginatto, Francieli Moro Stefanello
The aim of this study was to investigate the effect of Eugenia uniflora fruit (red type) extract on metabolic status, as well as on neurochemical and behavioral parameters in an animal model of metabolic syndrome induced by a highly palatable diet (HPD). Rats were treated for 150days and divided into 4 experimental groups: standard chow (SC) and water orally, SC and E. uniflora extract (200mg/kg daily, p.o), HPD and water orally, HPD and extract. Our data showed that HPD caused glucose intolerance, increased visceral fat, weight gain, as well as serum glucose, triacylglycerol, total cholesterol and LDL cholesterol; however, E...
June 10, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28618650/anti-amnesic-effects-of-ganoderma-species-a-possible-cholinergic-and-antioxidant-mechanism
#19
Ravneet Kaur, Varinder Singh, Richa Shri
Mushrooms are valued for their nutritional as well as medicinal properties. Ganoderma species are used traditionally to treat neurological disorders but scientific evidence for this is insufficient. The present study was designed to systematically evaluate the anti-amnesic effect of selected Ganoderma species i.e. G. mediosinense and G. ramosissimum. Extracts of selected mushroom species were evaluated for their antioxidant activity and acetylcholinesterase (AChE) inhibition using in-vitro assays (DPPH and Ellman tests respectively)...
June 10, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28618362/exposure-of-larvae-to-thiamethoxam-affects-the-survival-and-physiology-of-the-honey-bee-at-post-embryonic-stages
#20
Daiana Antonia Tavares, Claudia Dussaubat, André Kretzschmar, Stephan Malfitano Carvalho, Elaine C M Silva-Zacarin, Osmar Malaspina, Géraldine Bérail, Jean-Luc Brunet, Luc P Belzunces
Under laboratory conditions, the effects of thiamethoxam were investigated in larvae, pupae and emerging honey bees after exposure at larval stages with different concentrations in the food (0.00001 ng/μL, 0.001 ng/μL and 1.44 ng/μL). Thiamethoxam reduced the survival of larvae and pupae and consequently decreased the percentage of emerging honey bees. Thiamethoxam induced important physiological disturbances. It increased acetylcholinesterase (AChE) activity at all developmental stages and increased glutathione-S-transferase (GST) and carboxylesterase para (CaEp) activities at the pupal stages...
June 12, 2017: Environmental Pollution
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