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D Cupic Miladinovic, S Borozan, S Ivanovic
Chlorpyrifos is a widely used organophosphate pesticide (OP). In birds and mammals OP exhibits a toxic effect via inhibition of cholinesterases [acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)] and through oxidative/nitrosative stress. In this study, the influence of chlorpyrifos on cholinesterase activity, parameters of oxidative stress [malondialdehyde (MDA); glutathione (GSH); superoxide dismutase (SOD); nitrite concentration (NO2-); hydrogen peroxide (H2O2)], and inflammatory parameter [activity of myeloperoxidase (MPO)] in the brain of Japanese quail (Coturnix japanica) was examined...
February 19, 2018: Poultry Science
Kamil Kuca, Kamil Musilek, Daniel Jun, Jana Zdarova-Karasova, Eugenie Nepovimova, Ondrej Soukup, Martina Hrabinova, John Mikler, Tanos C C Franca, Elaine F F Da Cunha, Alexandre A De Castro, Martin Valis, Teodorico C Ramalho
BACKGROUND: Based on in vitro and in vivo rat experiments, the newly developed acetylcholinesterase (AChE) reactivator, K203, appears to be much more effective in the treatment of tabun poisonings than currently fielded oximes. METHODS: To determine if this reactivating efficacy would extend to humans, studies were conducted in vitro using human brain homogenate as the source of AChE. The efficacy of K203 was compared with commercially available oximes; pralidoxime, obidoxime and asoxime (HI-6)...
February 21, 2018: BMC Pharmacology & Toxicology
Guoliang Li, Ge Hong, Xinyu Li, Yan Zhang, Zengping Xu, Lina Mao, Xizeng Feng, Tianjun Liu
A series of novel tacrine-phenolic acid dihybrids and tacrine-phenolic acid-ligustrazine trihybrids were synthesized, characterized and screened as novel potential anti-Alzheimer drug candidates. These compounds showed potent inhibition activity towards cholinesterases (ChEs), among of them, 9i was the most potent one towards acetylcholinesterase (eeAChE, IC50  = 3.9 nM; hAChE, IC50  = 65.2 nM). 9i could also effectively block β-amyloid (Aβ) self-aggregation with an inhibition ratio of 47% at 20 μM...
February 13, 2018: European Journal of Medicinal Chemistry
Young-Jun Choi, Hyemin Kim, Ji-Woo Kim, Seokjoo Yoon, Han-Jin Park
OBJECTIVES: The aim of the study is to generate a spherical three-dimensional (3D) aggregate of hepatocyte-like cells (HLCs) differentiated from human embryonic stem cells and to investigate the effect of the 3D environment on hepatic maturation and drug metabolism. RESULTS: Quantitative real-time PCR analysis indicated that gene expression of mature hepatocyte markers, drug-metabolizing enzymes, and hepatic transporters was significantly higher in HLCs cultured in the 3D system than in those cultured in a two-dimensional system (p < 0...
February 20, 2018: Biotechnology Letters
Paula Rayane de Souza, Kelma Sirleide de Souza, Caio Rodrigo Dias de Assis, Marlyete Chagas de Araújo, Kaline Catiely Campos Silva, Juliett de Fátima Xavier da Silva, Andreia Cybelle Marques Ferreira, Valdir Luna da Silva, Mônica Lúcia Adam, Luiz Bezerra de Carvalho, Ranilson de Souza Bezerra
Enzyme biomarkers from several aquatic organisms have been used for assessing the exposure to contaminants at sublethal levels. Amongst them, the cholinesterases are commonly extracted from several organisms to evaluate/measure organophosphate and carbamate neurotoxic effects. Acetylcholinesterase (AChE; EC is an enzyme of the group of serine esterases that acts on the hydrolysis of the neurotransmitter acetylcholine allowing the intermittence of the nerve impulses responsible for the neuronal communication...
February 12, 2018: Aquatic Toxicology
Esther E Nwanna, Adeniyi A Adebayo, Ganiyu Oboh, Opeyemi B Ogunsuyi, Ayokunle O Ademosun
Most alkaloids are produced by plants as a defense mechanism against herbivores. Since alkaloids are known to possess pharmacological effects, this study sought to investigate the in vitro modulatory effect of alkaloid obtained from two commonly consumed vegetables in southern Nigeria, Lasianthera africana (editan) and Gongronema latifolium (utazi), on some enzyme activities relevant to neurodegeneration. Effects of the alkaloids on cholinesterases (acetylcholinesterase [AChE] and butyrylcholinesterase [BChE]) and monoamine oxidase (MAO) activities were determined in vitro...
February 16, 2018: Journal of Dietary Supplements
Cintia E Citterio, Yoshiaki Morishita, Nada Dakka, Balaji Veluswamy, Peter Arvan
Thyroglobulin (TG) is the most abundant thyroid gland protein, a dimeric iodoglycoprotein (660 kDa). TG serves as the protein precursor in the synthesis of thyroid hormones tetraiodothyronine (T4) and triiodothyronine (T3). The primary site for T3 synthesis in TG involves an iodotyrosine acceptor at the antepenultimate Tyr residue (at the extreme carboxyl-terminus of the protein). The carboxyl-terminal region of TG is comprised of the CholinEsterase-Like (ChEL) domain followed by a short unique tail sequence...
February 12, 2018: Journal of Biological Chemistry
Javier E Ortiz, Adriana Garro, Natalia B Pigni, María Belén Agüero, German Roitman, Alberto Slanis, Ricardo D Enriz, Gabriela E Feresin, Jaume Bastida, Alejandro Tapia
BACKGROUND: In Argentina, the Amaryllidaceae family (59 species) comprises a wide variety of genera, only a few species have been investigated as a potential source of cholinesterases inhibitors to treat Alzheimer disease (AD). PURPOSE: To study the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of the basic dichloromethane extracts (E) from Hieronymiella aurea, H. caletensis, H. clidanthoides, H. marginata, and H. speciosa species, as well as the isolated compounds from these plant extracts...
January 15, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Archana S Gurjar, Mrunali N Darekar, Keng Yoon Yeong, Luyi Ooi
Alzheimer's disease (AD) is a progressive neurodegenerative disorder with multiple factors associated with its pathogenesis. Our strategy against AD involves design of multi-targeted 2-substituted-4,5-diphenyl-1H-imidazole analogues which can interact and inhibit AChE, thereby, increasing the synaptic availability of ACh, inhibit BuChE, relieve induced oxidative stress and confer a neuroprotective role. Molecular docking was employed to study interactions within the AChE active site. In silico ADME study was performed to estimate pharmacokinetic parameters...
February 2, 2018: Bioorganic & Medicinal Chemistry
Valeria Cavallaro, Yanina F Moglie, Ana P Murray, Gabriel E Radivoy
A series of thirty-three alkynyl and β-ketophosphonates were evaluated for their in vitro acetyl- and butyryl-cholinesterase (AChE and BChE) inhibitory activities using Ellman's spectrophotometric method. None of the examined compounds inhibited AChE activity at tested concentrations while twenty-nine of them showed significant and selective inhibition of BChE with IC50 values between 38.60 µM and 0.04 µM. In addition, structure-activity relationships were discussed. The most effective inhibitors were the dibutyl o-methoxyphenyl alkynylphosphonate 3dc and dibutyl o-methoxyphenyl β-ketophosphonate 4dc...
February 7, 2018: Bioorganic Chemistry
Oľga Otrubová, Ladislav Turecký, Oľga Uličná, Pavol Janega, Ján Luha, Jana Muchová
N-acetyl-L-cysteine (NAC) is a drug routinely used in several health problems, e.g. liver damage. There is some information emerged on its negative effects in certain situations. The aim of our study was to examine its ability to influence liver damage induced by long-term burden. We induced liver damage by CCl4 (10 weeks) and monitored the impact of parallel NAC administration (daily 150 mg/kg of b.w.) on liver morphology and some biochemical parameters (triacylglycerols, cholesterol, alanine aminotransferase (ALT), aspartate aminotransferase (AST), bilirubin, bile acids, proteins, albumins and cholinesterase)...
January 2018: General Physiology and Biophysics
Fahimeh Vafadarnejad, Mohammad Mahdavi, Elahe Karimpour-Razkenari, Najmeh Edraki, Bilqees Sameem, Mahnaz Khanavi, Mina Saeedi, Tahmineh Akbarzadeh
A novel series of coumarin-pyridinium hybrids were synthesized and evaluated as inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) using Ellman's method. Among synthesized compounds, 1-(3-fluorobenzyl)-4-((2-oxo-2H-chromene-3-carboxamido)methyl)pyridinium bromide (7l) was found to be the most active compound toward AChE (IC50 = 10.14 µM), 1-(3-chlorobenzyl)-3-((2-oxo-2H-chromene-3-carboxamido)methyl)pyridinium bromide (7g) and 1-(2,3-dichlorobenzyl)-3-((2-oxo-2H-chromene-3-carboxamido)methyl)pyridinium chloride (7h) depicted the best BChE inhibitory activity (IC50s = 0...
January 27, 2018: Bioorganic Chemistry
Raju Suresh Kumar, Abdulrahman I Almansour, Natarajan Arumugam, Dhaifeallah Mohammed Qaide Althomili, Mohammed Altaf, Alireza Basiri, Kotresha D, Thota Sai Manohar, Venketesh S
A small library of novel spiropyrrolidine heterocyclic hybrids has been prepared regioselectively in 1-butyl-3-methylimidazoliumbromide ([bmim]Br) with good to excellent yields using a [3+2] cycloaddition reaction. These synthesized compounds were evaluated as potential agents for treating Alzheimer's disease. Compound 4b showed the most potent activity, with an IC50 of 7.9 ± 0.25 µM against acetylcholinesterase (AChE). The inhibition mechanisms for the most active compounds on AChE and butyrylcholinesterase (BChE) receptors were elucidated using molecular docking simulations...
February 2, 2018: Bioorganic Chemistry
Nikolaos Kokras, Evangelia Stamouli, Ioannis Sotiropoulos, Everina A Katirtzoglou, Kostas T Siarkos, Georgia Dalagiorgou, Krystallenia I Alexandraki, Stavroula Coulocheri, Christina Piperi, Antonios M Politis
BACKGROUND: Clinical and preclinical studies firmly support the involvement of the inflammation in the pathogenesis of Alzheimer's disease (AD). Despite acetylcholinesterase inhibitors (AChEI) being widely used in AD patients, there is no conclusive evidence about their impact on the inflammatory response. METHODS: This study investigates peripheral proinflammatory cytokines (interferon gamma [IFN-γ], tumor necrosis factor alpha [TNF-α], and interleukins 1β [IL-1β] and 6 [IL-6]) by firstly comparing peripheral blood mononuclear cell (PBMC)-derived secretion in drug-naïve and AChEI-treated AD patients versus healthy controls...
February 7, 2018: Journal of Clinical Psychopharmacology
Dawid Panek, Anna Więckowska, Anna Pasieka, Justyna Godyń, Jakub Jończyk, Marek Bajda, Damijan Knez, Stanislav Gobec, Barbara Malawska
The complex nature of Alzheimer's disease calls for multidirectional treatment. Consequently, the search for multi-target-directed ligands may lead to potential drug candidates. The aim of the present study is to seek multifunctional compounds with expected activity against disease-modifying and symptomatic targets. A series of 15 drug-like various substituted derivatives of 2-(benzylamino-2-hydroxyalkyl)isoindoline-1,3-diones was designed by modification of cholinesterase inhibitors toward β-secretase inhibition...
February 7, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Nahid Ahmadi, Ali Mandegary, Akram Jamshidzadeh, Mohaddeseh Mohammadi-Sardoo, Mohammadreza Mohammadi-Sardo, Elham Salari, Leyla Pourgholi
The widespread use of pesticides in agriculture represents a threat to the human populations exposed to them. In this cross-sectional study, the hematological and biochemical parameters, plasma cholinesterase (PChE) activity, oxidative stress, genotoxicity, and NAD(P)H: quinone oxidoreductase 1 (NQO1) C609T polymorphism were measured in 100 greenhouse workers occupationally exposed to pesticide mixture and 104 normal healthy controls. There was a decrease in erythrocytes (5.45%, p = 0.026) and hemoglobin (3...
February 7, 2018: Toxics
Carey N Pope, Stephen Brimijoin
Acetylcholinesterase (AChE, EC and butyrylcholinesterase (BChE, EC are related enzymes found across the animal kingdom. The critical role of acetylcholinesterase in neurotransmission has been known for almost a century, but a physiological role for butyrylcholinesterase is just now emerging. The cholinesterases have been deliberately targeted for both therapy and toxicity, with cholinesterase inhibitors being used in the clinic for a variety of disorders and conversely for their toxic potential as pesticides and chemical weapons...
January 30, 2018: Biochemical Pharmacology
Sengul Uysal, Abdurrahman Aktumsek, Carene M N Picot, Hamiyet Unuvar, Adriano Mollica, Milen I Georgiev, Gokhan Zengin, Mohamad Fawzi Mahomoodally
Extracts (methanol, ethyl acetate, and water) from Dianthus calocephalus Boiss. prepared by different extraction techniques (maceration, Soxhlet, and ultrasonication) were studied for possible inhibitory action against key enzymes (α-amylase, α-glucosidase, acetyl cholinesterase, butyryl cholinesterase, and tyrosinase). Antioxidant potential was established using a battery of assays and phenolic compounds profiled by RP-HPLC. Binding pose of tyrosinase with rutin was studied by means of molecular docking...
January 30, 2018: Food and Chemical Toxicology
Jie Zhu, Hongyu Yang, Yao Chen, Hongzhi Lin, Qi Li, Jun Mo, Yaoyao Bian, Yuqiong Pei, Haopeng Sun
The cholinergic hypothesis has long been a "polar star" in drug discovery for Alzheimer's disease (AD), resulting in many small molecules and biological drug candidates. Most of the drugs marketed for AD are cholinergic. Herein, we report our efforts in the discovery of cholinesterases inhibitors (ChEIs) as multi-target-directed ligands. A series of tacrine-ferulic acid hybrids have been designed and synthesised. All these compounds showed potent acetyl-(AChE) and butyryl cholinesterase(BuChE) inhibition. Among them, the optimal compound 10g, was the most potent inhibitor against AChE (electrophorus electricus (eeAChE) half maximal inhibitory concentration (IC50) = 37...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
Dimple Popli, Vishaka Anil, Akshatha B Subramanyam, Namratha M N, Ranjitha V R, Saroja N Rao, Ravishankar V Rai, Melappa Govindappa
This research study is to develop an easy and eco-friendly method for the synthesis of AgNPs using aqueous extract of endophytic fungi, Cladosporium species (CsAgNPs) and investigated the effects of antioxidant, anti-diabetic and anti-acetylcholinesterase (AChE), anti-butyrylcholinesterase (BChE) activity. Cladosporium species-mediated silver nanoparticles were characterized by UV-Vis spectrophotometer, Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD) and energy dispersive X-ray spectroscopy (EDX)...
February 5, 2018: Artificial Cells, Nanomedicine, and Biotechnology
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