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Cholinesterase

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https://www.readbyqxmd.com/read/28544873/3d-qsar-studies-of-some-reversible-acetyl-cholinesterase-inhibitors-based-on-comfa-and-ligand-protein-interaction-fingerprints-using-pc-ls-svm-and-pls-ls-svm
#1
Hamidreza Ghafouri, Mohsen Ranjbar, Amirhossein Sakhteman
A great challenge in medicinal chemistry is to develop different methods for structural design based on the pattern of the previously synthesized compounds. In this study two different QSAR methods were established and compared for a series of piperidine acetylcholinesterase inhibitors. In one novel approach, PC-LS-SVM and PLS-LS-SVM was used for modeling 3D interaction descriptors, and in the other method the same nonlinear techniques were used to build QSAR equations based on field descriptors. Different validation methods were used to evaluate the models and the results revealed the more applicability and predictive ability of the model generated by field descriptors (Q(2)LOO-CV=1, R(2)ext=0...
May 10, 2017: Computational Biology and Chemistry
https://www.readbyqxmd.com/read/28544619/design-and-synthesis-of-some-acridine-piperazine-hybrids-for-the-improvement-of-cognitive-dysfunction
#2
Anuradha Sharma, Poonam Piplani
A novel series of hybrid molecules (5a-5m) was designed, synthesized and evaluated as multifunctional cholinesterase (ChE) inhibitors against cognitive dysfunction. Heterocyclic moieties acridine and piperazine were conjugated with suitable linkers in a single scaffold and the structures of the target compounds were confirmed by IR, (1) H NMR, (13) C NMR and LC-MS analysis. The pharmacological activity of synthesized compounds was evaluated using behavioral models of amnesia viz. step down passive avoidance and elevated plus maze at a dose 0...
May 25, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28544328/acetylcholine-related-proteins-in-non-neoplastic-appearing-colonic-mucosa-from-patients-with-colorectal-neoplasia
#3
Morten Matthiesen Bach Damm, Thorbjørn Søren Rønn Jensen, Badar Mahmood, Morten Lundh, Steen Seier Poulsen, Niels Bindslev, Mark Berner Hansen
The pathogenesis of colorectal neoplasia (CRN) has been associated with altered non-neuronal acetylcholine (ACh) metabolism. The aim of this study was to characterize expression, function and cellular location of ACh-related proteins in biopsies obtained from endoscopic normal appearing sigmoid colon in patients with and without CRN. Messenger-RNA (mRNA) levels of 17 ACh-related proteins were quantified by rt-qPCR. Functional responses to ACh, measured as electrogenic transepithelial short circuit current (SCC), were recorded using the Ussing chamber technique...
May 23, 2017: Molecular Carcinogenesis
https://www.readbyqxmd.com/read/28542985/cholinesterase-reactivators-and-bioscavengers-for-pre-and-post-exposure-treatments-of-organophosphorus-poisoning
#4
REVIEW
Patrick Masson, Florian Nachon
Organophosphorus agents (OPs) irreversibly inhibit acetylcholinesterase (AChE) causing a major cholinergic syndrome. The medical counter-measures of OP poisoning have not evolved for the last 30 years with carbamates for pretreatment, pyridinium oximes-based AChE reactivators, antimuscarinic drugs and neuroprotective benzodiazepines for post-exposure treatment. These drugs ensure protection of peripheral nervous system and mitigate acute effects of OP lethal doses. However, they have significant limitations...
May 21, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28535697/identification-of-peptides-present-in-sour-milk-whey-that-ameliorate-scopolamine-induced-memory-impairment-in-mice
#5
Kazuhito Ohsawa, Naoto Uchida, Kohji Ohki, Hidehiko Yokogoshi
Cognitive impairment is treated with cholinesterase inhibitors that slow cognitive decline but cause significant adverse effects. Functional foods that improve memory without such effects would therefore be valuable. We reported that unidentified components of sour milk whey produced by fermentations using Lactobacillus helveticus and Saccharomyces cerevisiae improved memory in a mouse model of scopolamine-induced memory impairment. Here, we show that casein-derived peptides were the most active components of orally administered fractions of this milk product...
May 23, 2017: International Journal of Food Sciences and Nutrition
https://www.readbyqxmd.com/read/28534003/new-pharmacological-approaches-to-treating-non-motor-symptoms-of-parkinson-s-disease
#6
Michael A Kelberman, Elena M Vazey
PURPOSE OF REVIEW: Non-motor symptoms in patients with Parkinson's Disease (PD) are better predictors of quality of life changes, caregiver burden, and mortality than motor symptoms. Levodopa has limited, and sometimes detrimental, effects on these symptoms. In this review we discuss recent evidence on pharmacological treatments for non-motor symptoms. RECENT FINDINGS: Breakthroughs have been made in the treatment of psychosis and sleep dysfunction. Pimavanserin has become the first FDA approved drug for PD psychosis...
December 2016: Current Pharmacology Reports
https://www.readbyqxmd.com/read/28527279/-cases-of-acute-pesticide-poisoning-in-colonia-puerto-pirap%C3%A3-itap%C3%A3%C2%BAa-paraguay-february-2014
#7
María Esther Pedrozo, Sandra Ocampos, Rosa Galeano, Andrea Ojeda, Agueda Cabello, Dalva De Assis
In Paraguay, pesticides are the causative agent in 13.7% of poisonings, especially organophosphorus compounds. Such poisoning produces the inhibition of acetylcholinesterase generating three possible clinical conditions: acute poisoning, intermediate syndrome or late neurotoxicity. We present 15 cases of acute poisoning, ten women and five men from a rural community between 5 and 67 years of age, whose symptoms began after using water contaminated by pesticides from the community network. The most common symptoms were nausea and vomiting, followed by abdominal pain, headache, fever, itching, red eyes and sweating...
June 1, 2017: Biomédica: Revista del Instituto Nacional de Salud
https://www.readbyqxmd.com/read/28524136/-clinical-evaluation-of-the-effectiveness-of-cholinesterase-inhibition-with-neuromidin-in-the-treatment-of-primary-glaucoma-patients
#8
I A Zakharova, R V Avdeev, V A Pristavka, S N Surnin, V Yu Makhmutov, I I Savrasova
AIM: to investigate neuromidin effectiveness in the treatment of patients with primary glaucoma and compensated intraocular pressure (IOP). MATERIAL AND METHODS: A total of 40 patients (80 eyes) were examined. Of them, 10 eyes with early glaucoma, 36 eyes with moderate-stage glaucoma, 33 eyes with advanced glaucoma, and 1 eye with end-stage glaucoma. In 19 eyes, IOP was controlled through beta-blockers, in 11 eyes - through carbonic anhydrase inhibitors, in 10 eyes - through prostaglandin analogues, and in 39 eyes - through combination drugs...
2017: Vestnik Oftalmologii
https://www.readbyqxmd.com/read/28516254/use-of-muscular-cholinesterase-of-astyanax-bifasciatus-teleostei-characidae-as-a-biomarker-in-biomonitoring-of-rural-streams
#9
Jardel Nimet, Ana Tereza Bittencourt Guimarães, Rosilene Luciana Delariva
Cholinesterase (ChE) activity was measured in Astyanax bifasciatus maintained in controlled conditions. Muscle ChE activity of individuals collected in field conditions in two seasons was compared among specimens collected in seven streams (forest and rural) of the lower Iguaçu river basin in association with physical, chemical, pesticides and biological factors. Significant differences in muscle ChE activity between control fish and fish collected in streams in both seasons were found, with higher activity in natural conditions...
May 17, 2017: Bulletin of Environmental Contamination and Toxicology
https://www.readbyqxmd.com/read/28514891/synergistic-effect-of-rapamycin-and-metformin-against-age-dependent-oxidative-stress-in-rat-erythrocyte
#10
Abhishek Kumar Singh, Geetika Garg, Sandeep Singh, Syed Ibrahim Rizvi
Erythrocytes are particularly vulnerable towards age-dependent oxidative stress mediated damage. Caloric restriction mimetics (CRMs) may provide a novel strategy for the maintenance of redox balance as well as effective treatment of age associated diseases. Herein, we have investigated the beneficial effect of co-treatment of CRM-candidate drugs, rapamycin (an immunosuppressant drug and inhibitor of mammalian target of rapamycin) and metformin (an anti-diabetic biguanide and activator of adenosine monophosphate kinase) against aging-induced oxidative stress in erythrocytes and plasma of aging rats...
May 17, 2017: Rejuvenation Research
https://www.readbyqxmd.com/read/28511871/effect-of-distigmine-on-the-contractile-response-of-guinea-pig-urinary-bladder-to-electrical-field-stimulation
#11
Keisuke Obara, Yurina Kobayashi, Daisuke Chino, Yoshio Tanaka
Distigmine bromide (distigmine) is a reversible carbamate group cholinesterase (ChE) inhibitor. Although mainly used clinically for the treatment of myasthenia gravis, distigmine is also indicated for detrusor underactivity in Japan. According to the pharmacological classification of distigmine, its therapeutic effect against detrusor underactivity appears to be produced by enhanced urinary bladder smooth muscle (UBSM) contractility due to an increased concentration of acetylcholine between parasympathetic nerve endings and UBSM cells...
May 13, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28510502/the-impact-of-steroidal-glycoalkaloids-on-the-physiology-of-phytophthora-infestans-the-causative-agent-of-potato-late-blight
#12
Paul Dahlin, Marion C Müller, Sophia Ekengren, Lauren S McKee, Vincent Bulone
Steroidal glycoalkaloids (SGAs) are plant secondary metabolites known to be toxic to animals and humans and that have putative roles in defense against pests. The proposed mechanisms of SGA toxicity are sterol-mediated disruption of membranes and inhibition of cholinesterase activity in neurons. It has been suggested that phytopathogenic microorganisms can overcome SGA toxicity by enzymatic deglycosylation of SGAs. Here, we have explored SGA-mediated toxicity toward the invasive oomycete Phytophthora infestans, the causative agent of the late blight disease in potato and tomato, as well as the potential for SGA deglycosylation by this species...
May 16, 2017: Molecular Plant-microbe Interactions: MPMI
https://www.readbyqxmd.com/read/28508250/a-real-world-analysis-of-treatment-patterns-for-cholinesterase-inhibitors-and-memantine-among-newly-diagnosed-alzheimer-s-disease-patients
#13
Nawal Bent-Ennakhil, Florence Coste, Lin Xie, Myrlene Sanon Aigbogun, Yuexi Wang, Furaha Kariburyo, Ann Hartry, Onur Baser, Peter Neumann, Howard Fillit
INTRODUCTION: Alzheimer's disease (AD) is the most common neurodegenerative form of dementia. Pharmacological therapies for symptomatic treatment, such as acetylcholinesterase inhibitors (AChEIs) and memantine, have been available in the USA since 2000. Over the past decade, few studies have analyzed real-world anti-dementia treatment patterns in the USA. This study evaluated monotherapy AChEIs and memantine treatment patterns among newly diagnosed AD patients. METHODS: A retrospective cohort study was conducted using Medicare data and the Minimum Data Set from 2008 to 2012...
May 15, 2017: Neurology and Therapy
https://www.readbyqxmd.com/read/28505534/discorhabdin-alkaloids-from-antarctic-latrunculia-spp-sponges-as-a-new-class-of-cholinesterase-inhibitors
#14
Tanja Botić, Andrea Defant, Pietro Zanini, Monika Cecilija Žužek, Robert Frangež, Dorte Janussen, Daniel Kersken, Željko Knez, Ines Mancini, Kristina Sepčić
The brominated pyrroloiminoquinone alkaloids discorhabdins B, L and G and 3-dihydro-7,8- dehydrodiscorhabdin C, isolated from methanol extracts of two specimens of Latrunculia sp. sponges collected near the Antarctic Peninsula, are here demonstrated for the first time to be reversible competitive inhibitors of cholinesterases. They showed Ki for electric eel acetylcholinesterase of 1.6-15.0 μM, for recombinant human acetylcholinesterase of 22.8-98.0 μM, and for horse serum butyrylcholinesterase of 5.0-76...
May 6, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28504912/synthesis-and-biological-assessment-of-racemic-benzochromenopyrimidinetriones-as-promising-agents-for-alzheimer-s-disease-therapy
#15
Youssef Dgachi, Helène Martin, Alexandre Bonet, Mourad Chioua, Isabel Iriepa, Ignacio Moraleda, Fakher Chabchoub, José Marco-Contelles, Lhassane Ismaili
AIM: Due to the complex nature of Alzheimer's disease, there is a renewed search for multitarget directed drugs. RESULTS: This paper describes the synthesis and in vitro biological evaluation of six racemic 13-aryl-2,3,4,13-tetrahydro-1H,12H-benzo[6,7]chromeno[2,3-d]pyrido[1,2-a]pyrimidine-7,12,14-triones (1a-6a), and six racemic 15-aryl-8,9,10,11,12,15-hexahydro-14H-benzo[6',7']chromeno[2',3:4,5] pyr-imido [1,2-a]azepine-5,14,16-triones (1b-6b), showing antioxidant and cholinesterase inhibitory capacity...
May 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28504893/dual-inhibitors-of-cholinesterases-and-monoamine-oxidases-for-alzheimer-s-disease
#16
Damijan Knez, Matej Sova, Urban Košak, Stanislav Gobec
Accumulating evidence indicates a solid relationship between several enzymes and Alzheimer's disease. Cholinesterases and monoamine oxidases are closely associated with the disease symptomatology and progression and have been tackled simultaneously using several multifunctional ligands. This design strategy offers great chances to alter the course of Alzheimer's disease, in addition to alleviation of the symptoms. More than 15 years of research has led to the identification of various dual cholinesterase/monoamine oxidase inhibitors, while some showing positive outcomes in clinical trials, thus giving rise to additional research efforts in the field...
May 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28503953/effect-of-deltamethrin-and-fluoride-co-exposure-on-the-brain-antioxidant-status-and-cholinesterase-activity-in-wistar-rats
#17
Adil Mehraj Khan, Rajinder Raina, Nitin Dubey, Pawan Kumar Verma
The study evaluated the effect of commercial preparation of deltamethrin, Butox(®), and fluoride (F(-)) co-exposure on the brain antioxidant status and cholinesterase activity in rats. Group A was untreated. Group B was gavaged Butox(®), providing deltamethrin at the dose rate of 1.28 mg per kg body weight per day. Group C was administered F(-), as NaF, in drinking water providing 20 ppm F(-). Group D received both deltamethrin and F(-) at the same dosages as groups B and C, respectively. Although, glutathione S-transferase activity was induced only in Butox(®) alone treated group, the activities of superoxide dismutase and catalase were inhibited in all treatment groups when compared to the control group...
May 15, 2017: Drug and Chemical Toxicology
https://www.readbyqxmd.com/read/28501648/tetrahydroacridine-derivatives-with-fluorobenzoic-acid-moiety-as-multifunctional-agents-for-alzheimer-s-disease-treatment
#18
Kamila Czarnecka, Paweł Szymański, Małgorzata Girek, Elżbieta Mikiciuk-Olasik, Robert Skibiński, Jacek Kabziński, Ireneusz Majsterek, Barbara Malawska, Jakub Jończyk, Marek Bajda
A novel series of 9-amino-1,2,3,4-tetrahydroacridine derivatives with 2-fluorobenzoic acid or 3-fluorobenzoic acid moiety were designed, synthesized and evaluated as inhibitors of cholinesterases and aggregation of β-amyloid. In the study target compounds were very potent inhibitors of AChE and BChE. The most promising agents had higher inhibitory potency than the reference drugs which was tacrine. Ultimately, the kinetic assay shows the most active target compound 3c against AChE. Almost all of them were more potent against BChE than AChE...
May 5, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28501487/inhibition-on-cholinesterase-and-tyrosinase-by-alkaloids-and-phenolics-from-aristotelia-chilensis-leaves
#19
Carlos L Cespedes, Cristian Balbontin, Jose G Avila, Mariana Dominguez, Julio Alarcon, Cristian Paz, Viviana Burgos, Leandro Ortiz, Ignacio Peñaloza-Castro, David S Seigler, Isao Kubo
It is reported in this study the effect of isolates from leaves of Aristotelia chilensis as inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and tyrosinase enzymes. The aim of the paper was to evaluate the activity of A. chilensis towards different enzymes. In addition to pure compounds, extracts rich in alkaloids and phenolics were tested. The most active F5 inhibited AChE (79.5% and 89.8% at 10.0 and 20.0 μg/mL) and against BChE (89.5% and 97.8% at 10.0 and 20.0 μg/mL), showing a strong mixed-type inhibition against AChE and BChE...
May 10, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28500971/assessment-of-the-oxidative-and-neurotoxic-effects-of-glyphosate-pesticide-on-the-larvae-of-rhamdia-quelen-fish
#20
Thaís Maylin Sobjak, Silvia Romão, Cristian Zwetzch do Nascimento, Andrey Felipe Potulski Dos Santos, Lucas Vogel, Ana Tereza Bittencourt Guimarães
The aim of this work was to investigate the effects of glyphosate on the antioxidant system, as well as the neurotoxic effects on the larvae of Rhamdia quelen. A completely randomized design was implemented with the eggs of silver catfish distributed in 48 containers with 300 mL of water, which were subdivided randomly into two groups: control and treated with 6.5 mg L of glyphosate. These groups were evaluated at four time points (12 h, 24 h, 48 h, and 72 h), each with six replications. The survival rate of eggs/larvae (%) was evaluated, and samples were collected for antioxidant system analysis (catalase - CAT, glutathione transferase - GST, glutathione reductase - GR, and lipoperoxidation - LPO), and neurotoxic evaluation (cholinesterase - ChE)...
May 5, 2017: Chemosphere
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