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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
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
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
Gholam Hassan Danaei, Bahram Memar, Ramin Ataee, Mohammad Karami
Several studies have shown that oxidative stress and cell damage can occur at very early stages of diazinon (DZN) exposure. The present study was designed to determine the beneficial effect of thymoquinone (Thy), the main component of Nigella sativa (black seed or black cumin), against DZN cardio-toxicity in rats. In the present experimental study, 48 male Wistar rats were randomly divided into six groups: control (corn oil gavages), DZN gavages (20 mg/kg/day), Thy gavages (10 mg/kg/day) and Thy + DVN gavages (2...
April 12, 2018: Drug and Chemical Toxicology
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
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
Danica Sabolová, Pavol Kristian, Mária Kožurková
This review describes the synthesis of a wide range of novel tetrahydroacridine derivatives (tiocyanates, selenocyanates, ureas, selenoureas, thioureas, isothioureas, disulfides, diselenides and several tacrine homo- and hetro-hybrids). These tacrine congeners exhibit significant anticholinesterase and cytotoxic properties and may therefore be of considerable potential for the development of new drugs for the treatment of Alzheimer's disease.
April 6, 2018: Journal of Applied Toxicology: JAT
A S M Ali Reza, Mohammad Shahadat Hossain, Sharmin Akhter, Md Rezanur Rahman, Mst Samima Nasrin, Md Josim Uddin, Golam Sadik, A H M Khurshid Alam
BACKGROUND: Alzheimer's disease (AD), one of the major causes of dementia, is an overwhelming neurodegenerative disease that particularly affects the brain, leading to memory loss and impairment of language and judgment capacity. The aim of the present study was to investigate the antioxidant and anticholinesterase properties of the leaves of Elatostema papillosum (EPL) and correlate with their phytochemical profiles, which are relevant to the treatment of AD. METHODS: The dried coarse powder of EPL was extracted with 80% methanol (EPL-M80) by cold extraction method...
April 5, 2018: BMC Complementary and Alternative Medicine
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
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
Arif Mermer, Neslihan Demirbaş, Yakup Şirin, Harun Uslu, Zeynep Özdemir, Ahmet Demirbaş
The synthesis of ethyl 4-oxo-1,4-dihydroquinoline-3-carboxylates (4, 5) was performed via the reaction of corresponding anilines with diethyl ethoxymethylenemalonate under conventional and also microwave promoted conditions. The treatment of 4 and 5 afforded the corresponding hydrazides (6 and 7). These hydrazides were converted to the corresponding carbo(thio)amides (9a-f and 10a-e) which were then subjected to an intramolecular cyclisation leading to the formation of quinolone-triazole hybrids (11a-f and 12a-e)...
March 20, 2018: Bioorganic Chemistry
Jacqueline Cotton, John Edwards, Muhammad Aziz Rahman, Susan Brumby
BACKGROUND: Australian farmers are routinely exposed to a wide variety of agrichemicals, including herbicides and insecticides. Organophosphate (OP) insecticides are widely used for agricultural production, horticulture and animal husbandry practices. Symptoms of OP toxicity are the results of inhibition of the enzyme acetylcholinesterase (AChE) which is found in many types of conducting tissue in human bodies such as nerve and muscle, central and peripheral tissues, motor and sensory fibres...
April 2, 2018: Environmental Health: a Global Access Science Source
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
Jinliang Du, Rui Jia, Li-Ping Cao, Weidong Ding, Pao Xu, Guojun Yin
Fatty liver is an increasingly serious disease of fish in aquaculture. However, the mechanisms responsible for the occurrence of fatty liver remain unclear, and no effective methods for the prevention and treatment of this disease have yet been found. In the present study, we aimed to develop an in vitro model of hepatocyte injury using oleic acid as hepatotoxicant and evaluate the protective effects of Rhizoma Alismatis extract (RAE) in Jian carp using this model. Primary hepatocytes from Jian carp were isolated and purified and cultured in vitro...
March 30, 2018: Fish Physiology and Biochemistry
Akina Nara, Chiho Yamada, Takanori Kodama, Kanju Saka, Tetsuya Takagi
Organophosphates are widely used as pesticides. However, organophosphates are occasionally orally ingested to commit suicide. In this case, a man in his late 80s committed suicide by ingesting both dichlorvos and phenthoate. Autopsy findings revealed a characteristic volatile odor from his mouth, stomach, lungs, liver, and kidneys. The esophageal mucosa was denatured and had lost elasticity. Serum cholinesterase activity was 9 IU/L. Toxicological analyses performed using high-performance liquid chromatography-tandem mass spectrometry revealed that dichlorvos concentrations in the left and right cardiac blood samples were 11...
March 30, 2018: Journal of Forensic Sciences
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
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
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
A M Kolesnikov, M A Yuidin, A S Nikiforov, I M Ivanov, N G Vengerovich, A S Makacheev
The efficiency of different reactivators of cholinesterase (toxogonin, dipiroxime, pralidoxime, carboxim, HI-6, and methoxime) at inhibition of butyrylcholinesterase and human acetylcholinesterase by organophosphate insecticide malathion was evaluated in in vitro experiments. Most reactivators increased inhibition of butyrylcholinesterase in comparison with the control, but HI-6 in a concentration of 10-3 mol/liter partially (10%) restored activity of the enzyme. Oxime-induced reactivation of acetylcholinesterase was most pronounced in dipyroxime and toxogonin: parameters of the kinetics of reduction of the phosphorylated enzyme differed by more than 2 times from the values received with the use of other reactivators...
March 26, 2018: Bulletin of Experimental Biology and Medicine
Amara Mumtaz, Muhammad Shoaib, Sumera Zaib, Muhammad Shakil Shah, Huma Aslam Bhatti, Aamer Saeed, Izhar Hussain, Jamshed Iqbal
Alzheimer is a neurodegenerative disease and requires the development of new scaffold to treat it. In this regard, thiazoles derivative are playing their significant role. In the current research paper we have focused our attention for the development of tetrasubstituted thiazole (3a-h) derivatives using domino synthesis by mixing the thiourea as a precursor, with acetophenone in the presence of iodine and tosic acid in DMSO and refluxed for 12-22 h. The structures of the newly synthesized compounds were confirmed by FTIR,1 H NMR,13 C NMR and EIMS analysis...
March 9, 2018: Bioorganic Chemistry
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