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Jin Young Lee
O-ethyl S-2-diisopropylaminoethyl methyl phosphonothiolate (VX) is a highly toxic chemical warfare agent because it inhibits cholinesterase (ChE) activity in the nervous system. Inhibition of butyrylcholinesterase (BChE) activity by VX is due to formation of a phosphorylated BChE adduct; this adduct in human plasma can serve as a biomarker of exposure to nerve agents. We compared purification efficiency between the procainamide affinity gel method and immunomagnetic separation (IMS) for the nerve agent adduct of BChE in plasma and then optimized the sample preparation by purifying BChE to measure biomarkers of human exposure to organophosphorus nerve agents...
December 13, 2017: Journal of Chromatographic Science
Gerardo Rivas-Hernández, Yaneli May-Uc, Elsa Noreña-Barroso, Víctor Cobos-Gasca, Gabriela Rodríguez-Fuentes
The inhibition of cholinesterase (ChE) activity has been used as a biomarker of exposure to organophosphate and carbamate insecticides. ChE of nesting female green turtles (Chelonia mydas) were biochemically characterized using two substrates, acetylthiocholine iodide and butyrylthiocholine iodide, and three ChE inhibitors (eserine sulfate, BW284C51 and iso-OMPA). The results indicated that BChE is the predominant plasma ChE in female C. mydas, but with atypical properties that differ from those found in human BChE...
December 14, 2017: Bulletin of Environmental Contamination and Toxicology
Mhd Louai Manini, Michael Camilleri, Rayna Grothe, Carlo Di Lorenzo
BACKGROUND: Gastrointestinal (GI) motility disorders are common in children. Treatment is challenging with limited medical and surgical options. Pyridostigmine, an acetyl cholinesterase inhibitor, increases acetylcholine at the neuromuscular junction promoting intestinal contractions. Little is known about the role and dosing of pyridostigmine in pediatric GI motility disorders. METHODS: We present a case series of children with GI dysmotility managed with oral pyridostigmine...
December 14, 2017: Paediatric Drugs
Akimasa Kawai, Hideo Matsumoto, Youko Endou, Yui Honda, Hisako Kubota, Masaharu Higashida, Toshihiro Hirai
BACKGROUND/AIMS: Carnitine plays an important role in the metabolism of fatty acids. It has also been reported that the administration of anticancer drugs may lead to reductions in serum carnitine levels due to decreased activity of organic cation transporter novel 2, which plays a role in the reabsorption of carnitine in the tubules of the kidney. We therefore studied the change in carnitine levels when chemotherapy was administered repeatedly to patients with gastric cancer. METHODS: Ten patients with upper gastrointestinal cancer were enrolled in this study between December 2014 and August 2015...
December 13, 2017: Annals of Nutrition & Metabolism
Luciana R Tallini, Edison H Osorio, Vanessa Dias Dos Santos, Warley de Souza Borges, Marcel Kaiser, Francesc Viladomat, José Angelo S Zuanazzi, Jaume Bastida
The Amaryllidaceae family has proven to be a rich source of active compounds, which are characterized by unique skeleton arrangements and a broad spectrum of biological activities. The aim of this work was to perform the first detailed study of the alkaloid constituents of Hippeastrum reticulatum (Amaryllidaceae) and to determine the anti-parasitological and cholinesterase (AChE and BuChE) inhibitory activities of the epimers (6α-hydroxymaritidine and 6β-hydroxymaritidine). Twelve alkaloids were identified in H...
December 9, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Jan Misik, Eugenie Nepovimova, Jaroslav Pejchal, Jiri Kassa, Jan Korabecny, Ondrej Soukup
BACKGROUND: 6-chlorotacrine is a cholinesterase inhibitor showing good inhibitory potential, even better than parent compound tacrine, in vitro. Despite tacrine scaffold is broadly used for design and synthesis of novel compounds with anti-Alzheimer's potential, no in vivo effects have been investigated so far. Thus, basic toxicological and behavioural evaluation has been carried out throughout this study. METHODS: Maximum tolerated dose (MTD) and median lethal dose (LD50) were assessed in BALB/c mice and Wistar rats...
December 11, 2017: Current Alzheimer Research
Dinesh Neupane, Erik Jørs, Lars Peter Andreas Brandt
Background: Farmers in developing countries use highly toxic organophosphate pesticides. Thus, the aim of this study was to compare plasma cholinesterase (PChE) enzyme activity before and after exposure to organophosphate pesticides in a real-life setting. Methods: This was a prospective study conducted on 25 farmers spraying organophosphate pesticide in their farm. The PChE level was measured and clinical signs and symptoms of toxicity were asked before and immediately after spraying...
2017: Environmental Health Insights
Agung Nugroho, Jong-Hyuk Park, Jae Sue Choi, Kyoung-Sik Park, Joon-Pyo Hong, Hee-Juhn Park
Three acacetin triglycosides (compounds 1, 2 and 3) were isolated from the herbs of Elsholtzia ciliata (Labiatae). The structure were identified as 7-O-β-D-glucopyranosyl-(1 → 2)[α-L-rhamnopyranosyl-(1 → 6)]-β-D-glucopyranoside (compound 1), 7-O-(6-O-acetyl)-β-D-glucopyranosyl-(1 → 2)[α-L-rhamnopyranosyl-(1 → 6)]-β-D-glucopyranoside (compound 2) and 7-O-(6-O-acetyl)-β-D-glucopyranosyl-(1 → 2)[(4-O-acetyl)-α-L-rhamnopyranosyl-(1 → 6)]-β-D-glucopyranoside (compound 3) of acacetin...
December 11, 2017: Natural Product Research
Weiwei Sang, Benji Lv, Ke Li, Yan Lu
BACKGROUND AND OBJECTIVE: Mesenchymal stem cells transfusion has been considered as a promising option for liver cirrhosis (LC). The aim of this study was to systematically evaluate the efficacy and safety of umbilical cord mesenchymal stem cells (UMSC) combined with traditional supportive therapy (TST) for the treatment of patients with LC. METHODS: Data was extracted from clinical trials published on Web of Science, PubMed, EMBASE, Cochrane Library, Wanfang and CNKI database...
December 6, 2017: Clinics and Research in Hepatology and Gastroenterology
Kurt A Jellinger
Dementia with Lewy bodies (DLB) and Parkinson's disease-dementia (PDD), although sharing many clinical, neurochemical and morphological features, according to DSM-5, are two entities of major neurocognitive disorders with Lewy bodies of unknown etiology. Despite considerable clinical overlap, their diagnosis is based on an arbitrary distinction between the time of onset of motor and cognitive symptoms: dementia often preceding parkinsonism in DLB and onset of cognitive impairment after onset of motor symptoms in PDD...
December 8, 2017: Journal of Neural Transmission
Li-Jung Elizabeth Ku, Chung-Yi Li, Yu Sun
Although cholinesterase inhibitors (ChEIs) have been proved to help reduce cognitive deterioration in patients with Alzheimer's disease (AD), their effects on survival remain inconclusive. This study aims to assess the effects of the persistent use of ChEIs on the risk of mortality in patients with AD. This population-based cohort study included 8614 patients having AD with ChEI prescription from 2002 to 2006 and followed until 2010. Kaplan-Meier curves and hazard ratios (HRs) of mortality were estimated in association with ChEI treatment duration and adherence...
January 1, 2017: American Journal of Alzheimer's Disease and Other Dementias
Nadège E Kouémou, Germain S Taiwe, Fleur C O Moto, Simon Pale, Gwladys T Ngoupaye, Jacqueline S K Njapdounke, Gisèle C N Nkantchoua, David B Pahaye, Elisabeth Ngo Bum
Alzheimer's disease the most common form of dementia in the elderly is a neurodegenerative disease that affects 44 millions of people worldwide. The first treatments against Alzheimer's disease are acetylcholinesterase inhibitors; however, these medications are associated with many side effects. Dichrocephala integrifolia is a traditional herb widely used by indigenous population of Cameroon to treat and prevent Alzheimer's disease and for memory improvement. In this study, we evaluated the effect of the decoction prepared from leaves of D...
2017: Frontiers in Pharmacology
Yiming Zhou, Beibei Yan, Shen Zhao, Xiaoli Zhou, Ying Xiao
The aim of the study was to investigate toxicity of the synthesized roast duck flavor through animal experiment (mice feeding with the flavor for 35 days), and the major toxic compounds (acrylamide and 3,4-benzopyrene) were detected by high performance liquid chromatography. Compared with the control group, the blood biochemical indexes including protein content, bilirubin content, activity of alkaline phosphatase, activity of aspartate transaminase (AST) and alanine transaminase (ALT), cholesterol content, high density lipoprotein (HDL) and low density lipoprotein (LDL) content, triglycerides content, activity of creatine kinase (CK) and CK-MB, activity of cholinesterase (CHE) and lactate dehydrogenase (LDH), total bile acid (TBA) in high dose feeding group were significantly different...
December 2, 2017: Food and Chemical Toxicology
Shu Peng, Yu-Chen Pan, Yaling Wang, Zhe Xu, Chao Chen, Dan Ding, Yongjian Wang, Dong-Sheng Guo
The introduction of controlled self-assembly into living organisms opens up desired biomedical applications in wide areas including bioimaging/assays, drug delivery, and tissue engineering. Besides the enzyme-activated examples reported before, controlled self-assembly under integrated stimuli, especially in the form of sequential input, is unprecedented and ultimately challenging. This study reports a programmable self-assembling strategy in living cells under sequentially integrated control of both endogenous and exogenous stimuli...
November 2017: Advanced Science (Weinheim, Baden-Wurttemberg, Germany)
Samina Afzal, Bashir Ahmad Chaudhry, Ashfaq Ahmad, Muhammad Uzair, Khurram Afzal
Background: Corchorus depressus (Cd) commonly known as Boa-phalee belonging to the family Tiliaceae having 50 genera and 450 species. Cd is not among the studied medicinal agent despite its potential in ethnopharmacology. Objectives: The present study investigated antioxidant, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and α-glucosidase inhibitory activities of Cd. The dichloromethane and methanolic extracts of the Cd were evaluated for biological activities such as antioxidant and enzyme inhibitory activities of AChE, BChE, and α-glucosidase...
October 2017: Pharmacognosy Magazine
Kazufumi Kitagaki, Michio Nakanishi, Rei Ono, Kazuya Yamamoto, Yuji Suzuki, Noriyuki Fukui, Hidetoshi Yanagi, Harumi Konishi, Masanobu Yanase, Norihide Fukushima
PURPOSE: Although cardiac rehabilitation is recommended for patients early after heart transplantation (HTx), adequate exercise effect cannot always be obtained, partly because in patients with chronic heart failure, exercise capacity is reduced due to malnutrition during waiting for HTx. This study aimed to investigate the relationships between exercise capacity and clinical variables, including nutritional indicators, early after HTx. PATIENTS AND METHODS: Forty three HTx recipients were studied...
December 1, 2017: Clinical Transplantation
Lamia W Mohamed, Suzan M Abuel-Maaty, Waleed A Mohammed, May A Galal
A new series of oxopyrrolidines was synthesized and evaluated for their effect on Alzheimer's disease by measuring their inhibitory activity against acetyl cholinesterase enzyme and amyloid β 42 protein. Most of the compounds showed good inhibitory activity with ethyl 2-(2-(2, 6-dimethylphenylcarbamoyl)- 5-oxopyrrolidin-1-yl) acetate (V) having the highest activity against acetyl cholinesterase with IC50 value 1.84 ng/g tissue compared to standard donepezil 3.34 ng/g tissue. Furthermore, compound 1-((4-(4-chlorophenyl) piperazin-1-yl) methyl)-N-(2,6-dimethylphenyl)-5- oxopyrrolidine- 2-carboxamide (IIIe) displayed the highest activity against β 42 protein with IC50 value of 11...
November 15, 2017: Bioorganic Chemistry
Abdelaziz Kishk, Faraj Hijaz, Helmy A I Anber, Tsamoh K AbdEl-Raof, AbdEl-Hakeem D El-Sherbeni, Sobhy Hamed, Nabil Killiny
The Asian citrus psyllid, Diaphorina citri Kuwayama (Hemiptera: Lividae) transmits the Candidatus Liberibacter asiaticus, which causes citrus greening disease or Huanglongbing, (HLB). To date, there is no efficient cure for HLB disease and the control of D. citri using insecticides became the most important tools for the management of HLB. However, the extensive use of insecticides could increase D. citri resistance to these insecticides. The objective of this study was to investigate the effect of RNA interference of acetylcholinesterase (AChE) on the mortality and susceptibility of D...
November 2017: Pesticide Biochemistry and Physiology
Aleksandar R Zivkovic, Kevin M Tourelle, Thorsten Brenner, Markus A Weigand, Stefan Hofer, Karsten Schmidt
BACKGROUND: Sterile inflammation is an immediate and well-coordinated immune response to surgical injury. The cholinergic system plays a pivotal role in the inflammatory response. Induced inflammation stimulates the vagus nerve, which in turn activates anti-inflammatory nonneuronal processes. Serum cholinesterase (butyrylcholinesterase [BChE]) is an enzyme that hydrolyzes acetylcholine. Measuring the activity of the BChE in blood might indicate the level of the nonneuronal cholinergic activity...
December 2017: Journal of Surgical Research
Shaista Parveen, Muhammad Shakil Shah, Sumera Zaib, Tayyaba Gul, Khalid Mohammed Khan, Jamshed Iqbal, Abbas Hassan
Due to the immense importance of aryl indole nucleus, herein we report the palladium-catalyzed arylation of N-substituted 2-aryl indole utilizing Suzuki-Miyaura cross coupling methodology. The biological screening for cholinesterase inhibition of the resulted biaryl indole moieties was carried out to evaluate their pharmacological potential, expecting to involve the development of new therapeutics for various inflammatory, cardiovascular, gastrointestinal and neurological diseases. This research work also involved the use of utilization of microwave-assisted organic synthesis (MAOS) for the synthesis of Bischler-Möhlau indole which is further biarylated via palladium-catalyzed cross coupling reaction...
November 17, 2017: Bioorganic Chemistry
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