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Hiroyuki Ohbe, Taisuke Jo, Hiroki Matsui, Kiyohide Fushimi, Hideo Yasunaga
INTRODUCTION: In contrast to information on the effects of organophosphate, pesticide, or environmental exposures, data on cholinergic crisis caused by pharmaceutical cholinesterase inhibitors are sparse. The present study aimed to describe the characteristics, demographics, and mortality of patients with cholinergic crisis caused by pharmaceutical cholinesterase inhibitors using a nationwide inpatient database in Japan. METHODS: We identified patients diagnosed with cholinergic crisis as a result of taking cholinesterase inhibitor medications in the Japanese Diagnosis Procedure Combination inpatient database from July 2010 to March 2016...
June 15, 2018: Journal of Medical Toxicology: Official Journal of the American College of Medical Toxicology
Danping Liu, Jian Li, Wei Lu, Yanbing Wang, Xinlan Zhou, Dan Huang, Xiufen Li, Rongrong Ding, Zhanqing Zhang
OBJECTIVE: To evaluate the performance of a new mathematical model gamma- glutamyl transpeptidase to cholinesterase and platelet ratio (GCPR) versus gamma- glutamyl transpeptidase to platelet ratio (GPR) in predicting significant fibrosis and cirrhosis of chronic hepatitis B (CHB). METHODS: A complete cohort of 2343 patients was divided into early and late cohort depending on the time of liver biopsy. With reference to the Scheuer standard, liver pathological stage ≥S2 and ≥S4 were defined as significant fibrosis and cirrhosis, respectively...
June 12, 2018: Clinical Microbiology and Infection
Rafael Blesa, Kazuhiro Toriyama, Kengo Ueda, Sean Knox, George Grossberg
INTRODUCTION: Alzheimer's disease (AD) is the most common cause of dementia, characterized by a progressive decline in cognition and function. Current treatment options for AD include the cholinesterase inhibitors (ChEIs) donepezil, galantamine, and rivastigmine, as well as the N-methyl-D-aspartate receptor antagonist memantine. Treatment guidelines recommend the use of ChEIs as standard of care first-line therapy. Several randomized clinical studies have demonstrated the benefits of ChEIs on cognition, global function, behavior and activities of daily living...
June 12, 2018: Current Alzheimer Research
Giacobini Ezio, Pepeu Giancarlo
This review has two aims. First, to examine whether or not sex and gender may influence the brain cholinergic system in animals and in humans. Second, to examine the available evidence of sexually dimorphic response to the therapeutic and toxic effects of cholinesterase inhibitors. Animal research reveals no marked difference in the general morphology of the brain cholinergic system but subtle functional gender differences have been reported. In humans, gender differences in nucleus basalis of Meynert (NBM) exist...
June 12, 2018: Current Alzheimer Research
Xiaoran Duan, Yongli Yang, Sihua Wang, Xiaolei Feng, Tuanwei Wang, Pengpeng Wang, Wu Yao, Liuxin Cui, Wei Wang
Cholinesterase activity (ChA), the effective biomarker for organophosphate pesticide exposure, is possibly affected by single nucleotide polymorphisms (SNPs) in cell-cycle-related genes. One hundred and eighty workers with long-term exposure to omethoate and 115 healthy controls were recruited to explore the gene-gene and gene-environment interactions. The acetylthiocholine and dithio-bis-(nitrobenzoic acid) method was used to detect the cholinesterase activities in whole blood, erythrocytes and plasma. Genetic polymorphisms were determined by the PCR-RFLP and direct PCR electrophoresis methods...
May 2018: Royal Society Open Science
Rafael J Buralli, Helena Ribeiro, Thais Mauad, Luís F Amato-Lourenço, João M Salge, Fredi A Diaz-Quijano, Renata S Leão, Rejane C Marques, Daniele S Silva, Jean Remy Davée Guimarães
Pesticide exposure is a growing public health concern. Although Brazil is the world’s largest consumer of pesticides, only a few studies have addressed the health effects among farmers. This study aimed to evaluate whether pesticide exposure is associated with respiratory outcomes among rural workers and relatives in Brazil during the crop and off-seasons. Family farmers (82) were interviewed about occupational history and respiratory symptoms, and cholinesterase tests were conducted in the crop-season...
June 8, 2018: International Journal of Environmental Research and Public Health
Lúcia Guilhermino, Luís R Vieira, Diogo Ribeiro, Ana Sofia Tavares, Vera Cardoso, Anabela Alves, José Manuel Almeida
Microplastics and antimicrobials are widely spread environmental contaminants and more research on their toxicity is needed. The uptake and effects of the antimicrobial florfenicol, microplastics, and their mixtures on Corbicula fluminea were investigated. Bivalves were exposed for 96h to florfenicol (1.8 and 7.1mg/l), microplastics (0.2 and 0.7mg/l), or mixtures of the two substances. After 96h, all bivalves exposed to antimicrobial treatments had florfenicol in their body (e.g. 2±1μg/g). Microplastics were found in the gut, lumen of the digestive gland, connective tissue, hemolymphatic sinuses, and gills surface of animals...
May 1, 2018: Science of the Total Environment
Chamseddine Derabli, Imen Boualia, Ahmed B Abdelwahab, Raouf Boulcina, Chawki Bensouici, Gilbert Kirsch, Abdelmadjid Debache
In this work, we describe the preparation of some new Tacrine analogues modified with a pyranopyrazole moiety. A one-pot multicomponent reaction of 3-methyl-1H-pyrazol-5(4H)-one, aryl(or hetero)aldehydes, malononitrile and cyclohexanone involving a Friedländer condensation led to the title compounds. The synthesized heterocyclic analogues of this molecule were evaluated in vitro for their AChE and BChE inhibitory activities in search for potent cholinesterase enzyme inhibitors. Most of the synthesized compounds displayed remarkable AChE inhibitory activities with IC50 values ranging from 0...
June 1, 2018: Bioorganic & Medicinal Chemistry Letters
Ehsan Ullah Mughal, Asif Javid, Amina Sadiq, Shahzad Murtaza, Muhammad Naveed Zafar, Bilal Ahmad Khan, Sajjad Hussain Sumra, Muhammad Nawaz Tahir, Kanwal, Khalid Mohammed Khan
The prime objective of this research work is to prepare readily soluble synthetic analogues of naturally occurring 3-O-flavonol glycosides and then investigate the influence of various substituents on biological properties of synthetic compounds. In this context, a series of varyingly substituted 3-O-flavonol glycosides have been designed, synthesized and characterized efficiently. The structures of synthetic molecules were unambiguously corroborated by IR, 1 H, 13 C NMR and ESI-MS spectroscopic techniques...
June 1, 2018: Bioorganic & Medicinal Chemistry
Lucia De Marchi, Victor Neto, Carlo Pretti, Etelvina Figueira, Federica Chiellini, Andrea Morelli, Amadeu M V M Soares, Rosa Freitas
Salinity shifts in estuarine and coastal areas are becoming a topic of concern and are one of the main factors influencing nanoparticles behaviour in the environment. For this reason, the impacts of multi-walled carbon nanotubes (MWCNTs) under different seawater salinity conditions were evaluated on the common ragworm Hediste diversicolor, a polychaete species widely used as bioindicator of estuarine environmental quality. An innovative method to assess the presence of MWCNT aggregates in the sediments was used for the first time...
June 5, 2018: Scientific Reports
Sukesh Kumar Gupta, Manoj Kumar Mesharam, Sairam Krishnamurthy
Electromagnetic radiation (EMR) can induce or modulate several neurobehavioral disorders. Duration and frequency of exposure of EMR is critical to develop cognitive disorders. Even though EMR-2450 is widely used, its effects on cognition in relation to mitochondrial function and apoptosis would provide better understanding of its pathophysiological effects. Therefore, a comparative study of different frequencies of EMR exposure would give valuable information on effects of discrete frequencies of EMR on cognition...
June 2018: Journal of Biosciences
Hsiao Shan Cho, Li Kai Huang, Yao Tung Lee, Lung Chan, Chien Tai Hong
Objectives: Cholinesterase inhibitors (ChEIs) are the mainstream treatment for delaying cognitive decline in Alzheimer's disease (AD). Low vitamin B12 is associated with cognitive dysfunction, and its supplementation has been applied as the treatment for certain types of reversible dementia. The present study hypothesized that baseline serum vitamin B12 is associated with the deterioration of cognitive function in people with AD undergoing ChEI treatment. Materials and methods: Between 2009 and 2016, medical records from 165 Taiwanese with mild to moderate AD who underwent ChEI treatment for at least 2 years were reviewed...
2018: Frontiers in Neurology
Manizheh Mostofi, Ghodsi Mohammadi Ziarani, Negar Lashgari
A series of bezofuran appended 1,5-benzothiazepine compounds 7a-v was designed, synthesized and evaluated as cholinesterase inhibitors. The biological assay experiments showed that most of the compounds displayed a clearly selective inhibition for butyrylcholinesterase (BChE), while a weak or no effect towards acetylcholinesterase (AChE) was detected. All analogs exhibited varied BChE inhibitory activity with IC50 value ranging between 1.0 ± 0.01 and 72 ± 2.8 μM when compared with the standard donepezil (IC50 , 2...
March 1, 2018: Bioorganic & Medicinal Chemistry
Onur Bender, Eulogio J Llorent-Martínez, Gokhan Zengin, Adriano Mollica, Ramazan Ceylan, Lucia Molina-García, Maria Luisa Fernández-de Córdova, Arzu Atalay
The genus Hypericum is one of the most popular genera in both traditional medicine and scientific platform. This study is designed to provide conceptual insights on the biological potential and chemical characterization of H. salsugineum, which is endemic to Turkey. The qualitative and quantitative phenolic content of the extracts was characterized by HPLC-ESI-MSn. Biological efficiency was investigated by enzyme inhibitory assays (cholinesterases, tyrosinase, amylase, and glucosidase) and anti-cancer efficacy tests (anti-proliferative activities with the iCELLigence technology, colony formation and wound healing scratch assays)...
2018: PloS One
Luciana R Tallini, Laura Torras-Claveria, Warley de Souza Borges, Marcel Kaiser, Francesc Viladomat, José Angelo S Zuanazzi, Jaume Bastida
Natural products play an important role in the development of new drugs. In this context, the Amaryllidaceae alkaloids have attracted considerable attention in view of their unique structural features and various biological activities. In this study, twenty-three alkaloids were identified from Crinum amabile by GC-MS and two new structures (augustine N -oxide and buphanisine N -oxide) were structurally elucidated by NMR. Anti-parasitic and cholinesterase (AChE and BuChE) inhibitory activities of six alkaloids isolated from this species, including the two new compounds, are described herein...
May 26, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Sudhakar R Subramaniam, Iddo Magen, Nicholas Bove, Chunni Zhu, Vincent Lemesre, Garima Dutta, Chris Jean Elias, Henry A Lester, Marie-Francoise Chesselet
In addition to dopaminergic and motor deficits, patients with Parkinson's disease (PD) suffer from non-motor symptoms, including early cognitive and social impairment, that do not respond well to dopaminergic therapy. Cholinergic deficits may contribute to these problems, but cholinesterase inhibitors have limited efficacy. Mice over-expressing α-synuclein, a protein critically associated with PD, show deficits in cognitive and social interaction tests, as well as a decrease in cortical acetylcholine. We have evaluated the effects of chronic administration of nicotine in mice over-expressing wild type human α-synuclein under the Thy1-promoter (Thy1-aSyn mice)...
May 31, 2018: Neurobiology of Disease
Junyi Li, Di Rao, Robert B Gibbs
Cholinergic projections have been shown to interact with estrogens in ways that influence synaptic plasticity and cognitive performance. The mechanisms are not well understood. The goal of this study was to investigate whether cholinergic projections influence brain estrogen production by affecting aromatase (ARO), or influence estrogen signaling by affecting estrogen receptor expression. In the first experiment, ovariectomized rats received intraseptal injection of the selective immunotoxin 192IgG-saporin to destroy cholinergic inputs to the hippocampus...
May 28, 2018: Neuroscience
Ahmet Turan Isik, Pinar Soysal, Brendon Stubbs, Marco Solmi, Cristina Basso, Stefania Maggi, Patricia Schofield, Nicola Veronese, Christoph Mueller
OBJECTIVES: To evaluate the cardiovascular (CV) effects of acetylcholinesterase inhibitors (AChEIs) in individuals with dementia DESIGN: Systematic review and meta-analysis. SETTING: Two authors independently searched major electronic databases from inception until June 17, 2017, for longitudinal (without a control group) and cohort (with a control group) studies reporting CV outcomes in relation to AChEIs. Randomized controlled trials were excluded because they included relatively healthy subjects...
May 30, 2018: Journal of the American Geriatrics Society
Harald Hampel, M-Marsel Mesulam, A Claudio Cuello, Martin R Farlow, Ezio Giacobini, George T Grossberg, Ara S Khachaturian, Andrea Vergallo, Enrica Cavedo, Peter J Snyder, Zaven S Khachaturian
Cholinergic synapses are ubiquitous in the human central nervous system. Their high density in the thalamus, striatum, limbic system, and neocortex suggest that cholinergic transmission is likely to be critically important for memory, learning, attention and other higher brain functions. Several lines of research suggest additional roles for cholinergic systems in overall brain homeostasis and plasticity. As such, the brain's cholinergic system occupies a central role in ongoing research related to normal cognition and age-related cognitive decline, including dementias such as Alzheimer's disease...
May 29, 2018: Brain: a Journal of Neurology
Adam Kostelnik, Miroslav Pohanka
Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are two enzymes sensitive to various chemical compounds having ability to bind to crucial parts of these enzymes. Boldine is a natural alkaloid and it was mentioned in some older works that it can inhibit some kinds of AChE. We reinvestigated this effect on AChE and also on BChE using acetyl (butyryl) thiocholine and Ellman's reagents as standard substances for spectrophotometric assay. We found out IC50 of AChE equal to 372  μ mol/l and a similar level to BChE, 321  μ mol/l...
2018: BioMed Research International
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