keyword
MENU ▼
Read by QxMD icon Read
search

cholinesterase inhibitor

keyword
https://www.readbyqxmd.com/read/29655693/molecular-modeling-and-in-vitro-approaches-towards-cholinesterase-inhibitory-effect-of-some-natural-xanthohumol-naringenin-and-acyl-phloroglucinol-derivatives
#1
Ilkay Erdogan Orhan, Dariusz Jedrejek, F Sezer Senol, Ramin Ekhteiari Salmas, Serdar Durdagi, Iwona Kowalska, Lukasz Pecio, Wieslaw Oleszek
BACKGROUND: Many natural products, particularly phenolic compounds, have been reported to have a strong inhibition against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), the key enzymes in the pathology of Alzheimer's disease (AD). HYPOTHESIS: Therefore, we hypothesized that some xanthahumol, naringenin, and acyl phloroglucinol derivatives (1-14) isolated from Humulus lupulus L. (hops) may have an inhibitory potential against AChE and BChE. METHODS: Inhibitory potential of compounds 1-14 were tested against AChE and BChE using ELISA microtiter assay...
March 15, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/29655451/muscle-specific-tyrosine-kinase-and-myasthenia-gravis-owing-to-other-antibodies
#2
REVIEW
Michael H Rivner, Mamatha Pasnoor, Mazen M Dimachkie, Richard J Barohn, Lin Mei
Around 20% of patients with myasthenia gravis are acetylcholine receptor antibody negative; muscle-specific tyrosine kinase antibodies (MuSK) were identified as the cause of myasthenia gravis in 30% to 40% of these cases. Anti MuSK myasthenia gravis is associated with specific clinical phenotypes. One is a bulbar form with fewer ocular symptoms. Others show an isolated head drop or symptoms indistinguishable from acetylcholine receptor-positive myasthenia gravis. These patients usually respond well to immunosuppressive therapy, but not as well to cholinesterase inhibitors...
May 2018: Neurologic Clinics
https://www.readbyqxmd.com/read/29651948/therapeutic-potential-of-multifunctional-tacrine-analogues
#3
Maja Przybylowska, Szymon Kowalski, Krystyna Dzierzbicka, Iwona Inkielewicz-Stepniak
Tacrine is a potent inhibitor of cholinesterases (acetylcholinesterase and butyrylcholinesterase) that shows limiting clinical application by liver toxicity. In spite of this, analogues of tacrine are considered as model inhibitor of cholinesterases in the therapy of Alzheimer's disease. The interest in these compounds is mainly related to a high variety of their structure and biological properties. In the present review, we have described the role of cholinergic transmission and treatment strategies in Alzheimer's disease as well as the synthesis and biological activity of several recently developed classes of multifunctional tacrine analogues and hybrids, which consist a new paradigm to treat Alzheimer's disease...
April 11, 2018: Current Neuropharmacology
https://www.readbyqxmd.com/read/29642720/use-of-potentially-inappropriate-medications-in-people-with-dementia-in-vietnam-and-its-associated-factors
#4
Tuan Anh Nguyen, Thang Pham, Huyen Thi Thanh Vu, Thanh Xuan Nguyen, Trinh Thi Vu, Binh Thi Thanh Nguyen, Ngoc Quynh Nguyen, Binh Thanh Nguyen, Binh Thanh Nguyen, Tam Ngoc Nguyen, Sinh Viet Phan, Anh Trung Nguyen, Tuan Le Pham, Ha Thu Dang, Lisa Kalisch-Ellett, Marianne Gillam, Nicole Pratt, Sun Qiang, Haipeng Wang, Tipaporn Kanjanarach, Mohamed Azmi Ahmad Hassali, Zaheer-Ud-Din Babar, Asrenee Ab Razak, Dujrudee Chinwong, Elizabeth E Roughead
This study examined the use of potentially inappropriate medicines that may affect cognition (PIMcog) in people with dementia and its associated factors. Medical records of all outpatients with dementia attending a tertiary hospital in Vietnam between January 1, 2015, and December 31, 2016, were examined. Medicine use was assessed against a list of PIMcog. Variables associated with having a PIMcog were assessed using a multiple logistic regression. Of the 128 patients, 41% used a PIMcog, 39.1% used cholinesterase inhibitors (CEIs) concomitantly with anticholinergics, and 18% used antipsychotics...
January 1, 2018: American Journal of Alzheimer's Disease and Other Dementias
https://www.readbyqxmd.com/read/29625258/chemical-characterization-with-in-vitro-biological-activities-of-gypsophila-species
#5
Dimitrina Zheleva-Dimitrova, Gokhan Zengin, Vessela Balabanova, Yulian Voynikov, Valentin Lozanov, Irina Lazarova, Reneta Gevrenova
Methanol-aqueous extracts from the aerial parts of Gypsophila glomerata (GGE), G. trichotoma (GTE) and G. perfoliata (GPE) were investigated for antioxidant potential using different in vitro models, as well as for phenolic and flavonoid contents. The possible anti-cholinesterase, anti-tyrosinase, anti-amylase and anti-glucosidase activities were also tested. The flavonoid variability was analyzed using ultra high-performance liquid chromatography (UHPLC) coupled with hybrid quadrupole-Orbitrap high resolution mass spectrometry (HRMS)...
March 21, 2018: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29621640/synthesis-and-characterization-of-new-inhibitors-of-cholinesterases-based-on-n-phenylcarbamates-in-vitro-study-of-inhibitory-effect-type-of-inhibition-lipophilicity-and-molecular-docking
#6
Katarína Vorčáková, Magdaléna Májeková, Eva Horáková, Pavel Drabina, Miloš Sedlák, Šárka Štěpánková
Based on current treatment of Alzheimer's disease, where the carbamate inhibitor Rivastigmine is used, two series of carbamate derivatives were prepared: (i) N-phenylcarbamates with additional carbamate group (1-12) and (ii) N-phenylcarbamates with monosaccharide moiety (13-24). All compounds were tested for the inhibitory effect on both of the cholinesterases, electric eel acetylcholinesterase (eeAChE) and butyrylcholinesterase from equine serum (eqBChE) and the inhibitory activity (expressed as IC50 values) was compared with that of the established drugs Galanthamine and Rivastigmine...
March 28, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29614668/a-study-of-a-supplement-containing-huperzine-a-and-curcumin-in-dementia-patients-and-individuals-with-mild-cognitive-impairment
#7
Takeshi Tabira, Nobutoshi Kawamura
Extracts from Huperzia serrata (HS) function as a cholinesterase inhibitor and a glutamic acid receptor antagonist. We tested a supplement containing HS extracts, curcumin, and others in dementia patients and individuals with mild cognitive impairment (MCI) in an open label study. Most patients with Alzheimer's disease, dementia with Lewy bodies, and MCI individuals exhibited improvements in cognitive functions, as assessed by the Alzheimer's Disease Assessment Scale-cognitive subscale Japanese version. The scores were significantly improved at 6-12 weeks compared with baseline scores (p = 0...
March 29, 2018: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/29605586/a-protective-role-of-autophagy-in-tdcipp-induced-developmental-neurotoxicity-in-zebrafish-larvae
#8
Ruiwen Li, Ling Zhang, Qipeng Shi, Yongyong Guo, Wei Zhang, Bingsheng Zhou
Tris (1, 3-dichloro-2-propyl) phosphate (TDCIPP), an extensively used organophosphorus flame retardant, is frequently detected in various environmental media and biota, and has been demonstrated as neurotoxic. Autophagy has been proposed as a protective mechanism against toxicant-induced neurotoxicity. The purpose of the present study was to investigate the effect of TDCIPP exposure on autophagy, and its role in TDCIPP-induced developmental neurotoxicity. Zebrafish embryos (2-120 h post-fertilization [hpf]) were exposed to TDCIPP (0, 5, 50 and 500 μg/l) and a model neurotoxic chemical, chlorpyrifos (CPF, 100 μg/l)...
March 15, 2018: Aquatic Toxicology
https://www.readbyqxmd.com/read/29600750/terpenes-phenylpropanoids-sulfur-and-other-essential-oil-constituents-as-inhibitors-of-cholinesterases
#9
Olivera Politeo, Franko Burcul, Ivica Blazevic, Mila Radan
Essential oils constituents are a diverse family of low molecular weight organic compounds with comprehensive biological activity. According to their chemical structure these active compounds can be divided into four major groups: terpenes, terpenoids, phenylpropenes, and "others". In addition, they may contain diverse functional groups according to which they can be classified as hydrocarbons (monoterpenes, sesquiterpenes, and aliphatic hydrocarbons); oxygenated compounds (monoterpene and sesquiterpene alcohols, aldehydes, ketones, esters, and other oxygenated compounds); and sulfur and/or nitrogen sulfur-containing compounds (thioesters, sulfides, isothiocyantes, nitriles, and others)...
March 29, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29597336/comparative-evaluation-of-the-antioxidant-and-anti-alzheimer-s-disease-potential-of-coumestrol-and-puerarol-isolated-from-pueraria-lobata-using-molecular-modeling-studies
#10
Prashamsa Koirala, Su Hui Seong, Hyun Ah Jung, Jae Sue Choi
The current study assesses the antioxidant effects of two similar isoflavonoids isolated from Pueraria lobata , coumestrol and puerarol, along with the cholinergic and amyloid-cascade pathways to mitigate Alzheimer's disease (AD). Antioxidant activity was evaluated via 1,1-diphenyl-2-picryhydrazyl (DPPH) and peroxynitrite (ONOO- ) scavenging ability further screened via ONOO- -mediated nitrotyrosine. Similarly, acetyl- and butyrylcholinesterase (AChE/BChE) and β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitory activities were assessed together with docking and kinetic studies...
March 28, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29593539/optimization-of-cholinesterase-based-catalytic-bioscavengers-against-organophosphorus-agents
#11
Sofya V Lushchekina, Lawrence M Schopfer, Bella L Grigorenko, Alexander V Nemukhin, Sergei D Varfolomeev, Oksana Lockridge, Patrick Masson
Organophosphorus agents (OPs) are irreversible inhibitors of acetylcholinesterase (AChE). OP poisoning causes major cholinergic syndrome. Current medical counter-measures mitigate the acute effects but have limited action against OP-induced brain damage. Bioscavengers are appealing alternative therapeutic approach because they neutralize OPs in bloodstream before they reach physiological targets. First generation bioscavengers are stoichiometric bioscavengers. However, stoichiometric neutralization requires administration of huge doses of enzyme...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29563775/development-of-small-bisquaternary-cholinesterase-inhibitors-as-drugs-for-pre-treatment-of-nerve-agent-poisonings
#12
Kamil Kuca, Jana Zdarova Karasova, Ondrej Soukup, Jiri Kassa, Eva Novotna, Vendula Sepsova, Anna Horova, Jaroslav Pejchal, Martina Hrabinova, Eva Vodakova, Daniel Jun, Eugenie Nepovimova, Martin Valis, Kamil Musilek
Background: Intoxication by nerve agents could be prevented by using small acetylcholinesterase inhibitors (eg, pyridostigmine) for potentially exposed personnel. However, the serious side effects of currently used drugs led to research of novel potent molecules for prophylaxis of organophosphorus intoxication. Methods: The molecular design, molecular docking, chemical synthesis, in vitro methods (enzyme inhibition, cytotoxicity, and nicotinic receptors modulation), and in vivo methods (acute toxicity and prophylactic effect) were used to study bispyridinium, bisquinolinium, bisisoquinolinium, and pyridinium-quinolinium/isoquinolinium molecules presented in this study...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29559029/use-of-fda-approved-medications-for-alzheimer-s-disease-in-mild-dementia-is-associated-with-reduced-informal-costs-of-care
#13
Stephanie Behrens, Gail B Rattinger, Sarah Schwartz, Joshua Matyi, Chelsea Sanders, M Scott DeBerard, Constantine G Lyketsos, JoAnn T Tschanz
BACKGROUND: The use of FDA approved medications for Alzheimer's disease [AD; FDAAMAD; (cholinesterase inhibitors and N-methyl-D-aspartate receptor antagonists)] has been associated with symptomatic benefit with a reduction in formal (paid services) and total costs of care (formal and informal costs). We examined the use of these medications and their association with informal costs in persons with dementia. METHOD: Two hundred eighty participants (53% female, 72% AD) from the longitudinal, population-based Dementia Progression Study in Cache County, Utah (USA) were followed up to ten years...
March 21, 2018: International Psychogeriatrics
https://www.readbyqxmd.com/read/29557685/magnesium-sulfate-and-calcium-channel-blocking-drugs-as-antidotes-for-acute-organophosphorus-insecticide-poisoning-a-systematic-review-and-meta-analysis
#14
Miran Brvar, Ming Yin Chan, Andrew H Dawson, Richard R Ribchester, Michael Eddleston
INTRODUCTION: Treatment of acute organophosphorus or carbamate insecticide self-poisoning is often ineffective, with tens of thousands of deaths occurring every year. Researchers have recommended the addition of magnesium sulfate or calcium channel blocking drugs to standard care to reduce acetylcholine release at cholinergic synapses. OBJECTIVE: We aimed to review systematically the evidence from preclinical studies in animals exposed to organophosphorus or carbamate insecticides concerning the efficacy of magnesium sulfate and calcium channel blocking drugs as therapy compared with placebo in reducing mortality or clinical features of poisoning...
March 20, 2018: Clinical Toxicology
https://www.readbyqxmd.com/read/29550345/an-improved-immobilized-enzyme-reactor-mass-spectrometry-based-label-free-assay-for-butyrylcholinesterase-ligand-screening
#15
Adriana Ferreira Lopes Vilela, Cláudia Seidl, Juliana Maria Lima, Carmen Lúcia Cardoso
Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are key cholinesterase enzymes responsible for the hydrolysis of acetylcholine into choline and acetic acid, an essential process for the restoration of the cholinergic neuron. The loss of cholinergic function in the central nervous system contributes to the cognitive decline associated with advanced age and Alzheimer's disease (AD). Inhibitions assays represent a significant role in the drug discovery process. Herein, we describe an improved label free method to screen and characterize new BChE ligands...
March 14, 2018: Analytical Biochemistry
https://www.readbyqxmd.com/read/29537978/a-randomized-trial-of-oral-and-transdermal-rivastigmine-for-postural-instability-in-parkinson-disease-dementia
#16
Jaime McDonald, Emmanuelle Pourcher, Alexandra Nadeau, Philippe Corbeil
OBJECTIVES: The objective of this study was to compare the efficacy and safety of oral and transdermal rivastigmine for postural instability in patients with Parkinson disease dementia (PDD) who were candidates for a cholinesterase inhibitor. The primary outcome was the change in mean velocity of the center of pressure (CoP) after 6 months. Secondary outcomes included structural parameters of dynamic posturography, clinical rating scales, and adverse events requiring dose reduction. METHODS: Patients with PDD were randomized in a 1:1 ratio to oral or transdermal rivastigmine with target doses of 6 mg twice daily and 9...
March 13, 2018: Clinical Neuropharmacology
https://www.readbyqxmd.com/read/29535608/genistein-a-phytoestrogen-in-soybean-induces-the-expression-of-acetylcholinesterase-via-g-protein-coupled-receptor-30-in-pc12-cells
#17
Etta Y L Liu, Miranda L Xu, Yan Jin, Qiyun Wu, Tina T X Dong, Karl W K Tsim
Genistein, 4',5,7-trihydroxyisoflavone, is a major isoflavone in soybean, which is known as phytestrogen having known benefit to brain functions. Being a common phytestrogen, the possible role of genistein in the brain protection needs to be further explored. In cultured PC12 cells, application of genistein significantly induced the expression of neurofilaments (NFs), markers for neuronal differentiation. In parallel, the expression of tetrameric form of proline-rich membrane anchor (PRiMA)-linked acetyl-cholinesterase (G4 AChE), a key enzyme to hydrolyze acetylcholine in cholinergic synapses, was induced in a dose-dependent manner: this induction included the associated protein PRiMA...
2018: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/29533874/the-concept-of-hybrid-molecules-of-tacrine-and-benzyl-quinolone-carboxylic-acid-bqca-as-multifunctional-agents-for-alzheimer-s-disease
#18
V Hepnarova, J Korabecny, L Matouskova, P Jost, L Muckova, M Hrabinova, N Vykoukalova, M Kerhartova, T Kucera, R Dolezal, E Nepovimova, K Spilovska, E Mezeiova, N L Pham, D Jun, F Staud, D Kaping, K Kuca, O Soukup
Novel tacrine-benzyl quinolone carboxylic acid (tacrine-BQCA) hybrids were designed based on multi-target directed ligands (MTLDs) paradigm, synthesized and evaluated in vitro as inhibitors of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBChE). Tacrine moiety is represented herein as 7-methoxytacrine, 6-chlorotacrine or unsubstituted tacrine forming three different families of seven members, i.e. 21 compounds in overall. Introducing BQCA, a positive modulator of M1 muscarinic acetylcholine receptors (mAChRs), the action of novel compounds on M1 mAChRs was evaluated via Fluo-4 NW assay on the Chinese hamster ovarian (CHO-M1WT2) cell line...
March 2, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29529892/profiling-donepezil-template-into-multipotent-hybrids-with-antioxidant-properties
#19
Eva Mezeiova, Katarina Spilovska, Eugenie Nepovimova, Lukas Gorecki, Ondrej Soukup, Rafael Dolezal, David Malinak, Jana Janockova, Daniel Jun, Kamil Kuca, Jan Korabecny
Alzheimer's disease is debilitating neurodegenerative disorder in the elderly. Current therapy relies on administration of acetylcholinesterase inhibitors (AChEIs) -donepezil, rivastigmine, galantamine, and N-methyl-d-aspartate receptor antagonist memantine. However, their therapeutic effect is only short-term and stabilizes cognitive functions for up to 2 years. Given this drawback together with other pathological hallmarks of the disease taken into consideration, novel approaches have recently emerged to better cope with AD onset or its progression...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29527733/synthesis-biological-evaluation-and-docking-studies-of-some-5-chloro-2-3h-benzoxazolone-mannich-bases-derivatives-as-cholinesterase-inhibitors
#20
Sirin Uysal, Sulunay Parlar, Ayse H Tarikogullari, Fadime Aydin Kose, Vildan Alptuzun, Zeynep Soyer
A series of N-substituted-5-chloro-2(3H)-benzoxazolone derivatives were synthesized and evaluated for their acetylcholinesterase (AChE), butyrylcholinesterase (BuChE) inhibitory, and antioxidant activities. The structures of the title compounds were confirmed by spectral and elemental analyses. The cholinesterase (ChE) inhibitory activity studies were carried out using Ellman's colorimetric method. The free radical scavenging activity was also determined by in vitro ABTS (2,2-azinobis(3-ethylbenzothiazoline-6-sulfonic acid)) assay...
March 12, 2018: Archiv der Pharmazie
keyword
keyword
34622
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"