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https://www.readbyqxmd.com/read/28820005/inhibition-of-endocannabinoid-metabolizing-enzymes-in-peripheral-tissues-following-developmental-chlorpyrifos-exposure-in-rats
#1
Robert W Buntyn, Navatha Alugubelly, Rachel L Hybart, Afzaal N Mohammed, Carole A Nail, Greta C Parker, Matthew K Ross, Russell L Carr
Repeated developmental exposure to the organophosphate (OP) insecticide chlorpyrifos (CPF) inhibits brain fatty acid amide hydrolase (FAAH) activity at low levels, whereas at higher levels, it inhibits brain monoacylglycerol lipase (MAGL) activity. FAAH and MAGL hydrolyze the endocannabinoids anandamide (AEA) and 2-arachidonylglycerol (2-AG), respectively. Peripherally, AEA and 2-AG have physiological roles in the regulation of lipid metabolism and immune function, and altering the normal levels of these lipid mediators can negatively affect these processes...
January 1, 2017: International Journal of Toxicology
https://www.readbyqxmd.com/read/28817822/predictors-of-postoperative-non-chylous-massive-discharge-after-pancreaticoduodenectomy-for-pancreatic-ductal-adenocarcinoma
#2
Kyoji Ito, Yoshikuni Kawaguchi, Yoshihiro Sakamoto, Junichi Arita, Kiyoshi Hasegawa, Norihiro Kokudo
BACKGROUND: Pancreaticoduodenectomy (PD) is performed for pancreatic ductal adenocarcinoma (PDA) located at the pancreas head/body. Non-chylous massive discharge after PD is frequently encountered and can cause a vicious cycle of complications associated with severe dehydration and protein loss. METHODS: From August 2008 to June 2015, 102 patients who underwent PD for PDA were retrospectively reviewed. High non-chylous discharge was defined as postoperative daily serous discharge exceeding 10 mL/kg...
August 18, 2017: Digestive Surgery
https://www.readbyqxmd.com/read/28815802/prophylactic-effects-of-ellagic-acid-and-rosmarinic-acid-on-doxorubicin-induced-neurotoxicity-in-rats
#3
Hanan A Rizk, Marwa A Masoud, Omar W Maher
Doxorubicin (DOX) is a chemotherapeutic agent widely used in human malignancies. Its long-term use cause neurobiological side effects. The aim of the present study was to investigate the prophylactic effect exerted by daily administration of ellagic acid (EA) and rosmarinic acid (RA) on DOX-induced neurotoxicity in rats. Our data showed that DOX-induced significant elevation of brain malondialdehyde, tumor necrosis factor-alpha (TNF-α), inducible nitric oxide synthase (iNOS), caspase-3, and cholinesterase associated with significant reduction in reduced glutathione, monoamines namely serotonin, dopamine, as well as norepinephrine...
August 16, 2017: Journal of Biochemical and Molecular Toxicology
https://www.readbyqxmd.com/read/28814827/anticholinesterase-constituents-from-the-leaves-of-spondias-mombin-l-anacardiaceae
#4
Taiwo Olayemi Elufioye, Efere M Obuotor, Joseph M Agbedahunsi, Saburi A Adesanya
Spondias mombin has been used in traditional medicine for the management of several diseases, including memory loss. This study aimed to evaluate the cholinesterase inhibitory activity of the methanol extract of the leaves and its derived fractions, as well as carry out detailed phytochemical investigations leading to the isolation and characterization of bioactive compounds from the plant. The acetyl cholinesterase (AChE) and butyryl cholinesterase (BUChE) inhibitory activities were evaluated by colorimetric and thin-layer chromatography bioautographic assay techniques...
2017: Biologics: Targets & Therapy
https://www.readbyqxmd.com/read/28804856/toxic-effects-of-copper-on-liver-and-cholinesterase-of-clarias-gariepinus
#5
Siti Nadzirah Padrilah, Siti Aqlima Ahmad, Nur Adeela Yasid, Mohd Khalizan Sabullah, Hassan Mohd Daud, Ariff Khalid, Mohd Yunus Shukor
The release of pollutants, especially heavy metals, into the aquatic environment is known to have detrimental effects on such an environment and on living organisms including humans when those pollutants are allowed to enter the food chain. The aim of this study is to analyse the damage to Clarias gariepinus' liver caused by exposure to different concentrations of copper. In the present study, samples of C. gariepinus were exposed to sub-lethal copper sulphate (CuSO4) concentrations (from 0.2 to 20.0 mg/L) for 96 h...
August 13, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28801274/mannich-base-approach-to-5-methoxyisatin-3-4-isopropylphenyl-hydrazone-a-water-soluble-prodrug-for-a-multitarget-inhibition-of-cholinesterases-beta-amyloid-fibrillization-and-oligomer-induced-cytotoxicity
#6
Leonardo Pisani, Annalisa De Palma, Nicola Giangregorio, Daniela V Miniero, Paolo Pesce, Orazio Nicolotti, Francesco Campagna, Cosimo D Altomare, Marco Catto
Targeting protein aggregation for the therapy of neurodegenerative diseases remains elusive for medicinal chemists, despite a number of small molecules known to interfere in amyloidogenesis, particularly of amyloid beta (Aβ) protein. Starting from previous findings in the antiaggregating activity of a class of indolin-2-ones inhibiting Aβ fibrillization, 5-methoxyisatin 3-(4-isopropylphenyl)hydrazone 1 was identified as a multitarget inhibitor of Aβ aggregation and cholinesterases with IC50s in the low μM range...
August 8, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28799487/dementia-etiologies-and-remedies-in-traditional-persian-medicine-a-review-of-medicinal-plants-and-phytochemistry
#7
Laila Shirbeigi, Behnam Dalfardi, Zohre Abolhasanzade, Fatemeh Nejatbakhsh
BACKGROUND: Dementia is a chronic neurodegenerative disease causing progressive and gradual impairment of different brain's cognitive functions. The prevalence of dementia is about 3 to 7% in different parts of the world. OBJECTIVE: The aim of this study was to determine the etiologies of dementia according to the Traditional Persian Medicine scientists' viewpoint and introduce their recommended herbal remedies for this disease. METHOD: The authors explored six main Traditional Persian Medicine textbooks for the disease of dementia, its etiologies and related recommended herbal treatments...
August 10, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28797651/biological-effects-and-chemical-characterization-of-iris-schachtii-markgr-extracts-a-new-source-of-bioactive-constituents
#8
Andrei Mocan, Gokhan Zengin, Adriano Mollica, Ahmet Uysal, Erdogan Gunes, Gianina Crișan, Abdurrahman Aktumsek
This study gathers information about the effects of different extracts (methanol and water) from rhizomes and aerial parts of Iris schachtii on selected enzymes (cholinesterases, alpha-amylase and alpha-glucosidase, tyrosinase and lipase) as well as on their antioxidant capacities and antimutagenic properties in relation with their phenolic composition. The chemical composition was assessed by determining total phenolic and flavonoid content as well as individual phenolic compounds by HPLC-DAD. Moreover, antioxidant abilities of the investigated extracts were tested by using different assays including free radical scavenging (DPPH and ABTS), reducing power (CUPRAC and FRAP), phosphomolybdenum and metal chelating, overall rhizomes being indicated as a superior source of antioxidant compounds...
August 7, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28791707/preface-cholinergic-mechanisms
#9
Marco A M Prado, Pascale Marchot, Israel Silman
This special issue is a companion to the meeting 'XVth International Symposium on Cholinergic Mechanisms', and is edited by Israel Silman, Marco Prado and Pascale Marchot. In the review articles, renowned researchers in the field capture key mechanisms of cholinergic neurotransmission, from genomic amplification of cholinesterase genes, splicing and post-translational modifications; features of the neuromuscular junction, implications of cholinergic circuitry that are relevant to addiction, anxiety and mood, to preclinical models, protein biomarkers, and clinical findings that are relevant to pathology, for example, developmental neurotoxicity...
August 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28790827/the-effects-of-memantine-on-behavioral-disturbances-in-patients-with-alzheimer-s-disease-a-meta-analysis
#10
Taro Kishi, Shinji Matsunaga, Nakao Iwata
BACKGROUND: Memantine is effective in the treatment of behavioral disturbances in patients with Alzheimer's disease. It has not yet been fully determined which behavioral disturbances respond best to memantine. METHODS: We conducted a meta-analysis of memantine vs control (placebo or usual care) for the treatment of individual behavioral disturbances (delusion, hallucination, agitation/aggression, dysphoria, anxiety/phobia, euphoria, apathy, disinhibition, irritability/lability, aberrant motor activity/activity disturbances, nighttime disturbance/diurnal rhythm disturbances, and eating disturbances)...
2017: Neuropsychiatric Disease and Treatment
https://www.readbyqxmd.com/read/28782481/rational-approaches-design-strategies-structure-activity-relationship-and-mechanistic-insights-for-esterase-inhibitors
#11
Harbinder Singh, Jatinder Vir Singh, Navdeep Kaur, Mohit Sanduja, Gurpreet Singh, Preet Mohinder Singh Bedi, Sahil Sharma
BACKGROUND: Esterase is an enzyme that splits esters into an acid and alcohol. Varieties of esterases are present in human body to control diverse set of cellular processes and execute their specific functions. It can be seen that any increase in metabolites produced by these enzymes lead to severe pathological conditions like Alzheimer disease, hypercholesterolemia etc. OBJECTIVE: Numerous esterase inhibitors have been developed and reported by the researchers around the globe, but not systematically summarized yet...
August 7, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28770024/metformin-and-its-sulfenamide-prodrugs-inhibit-human-cholinesterase-activity
#12
Magdalena Markowicz-Piasecka, Joanna Sikora, Łukasz Mateusiak, Elżbieta Mikiciuk-Olasik, Kristiina M Huttunen
The results of epidemiological and pathophysiological studies suggest that type 2 diabetes mellitus (T2DM) may predispose to Alzheimer's disease (AD). The two conditions present similar glucose levels, insulin resistance, and biochemical etiologies such as inflammation and oxidative stress. The diabetic state also contributes to increased acetylcholinesterase (AChE) activity, which is one of the factors leading to neurodegeneration in AD. The aim of this study was to assess in vitro the effects of metformin, phenformin, and metformin sulfenamide prodrugs on the activity of human AChE and butyrylcholinesterase (BuChE) and establish the type of inhibition...
2017: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/28766165/chagas-disease-modulation-of-the-inflammatory-response-by-acetylcholinesterase-in-hematological-cells-and-brain-tissue
#13
Aniélen D Silva, Nathieli B Bottari, Guilherme M do Carmo, Matheus D Baldissera, Carine F Souza, Vanessa S Machado, Vera M Morsch, Maria Rosa C Schetinger, Ricardo E Mendes, Silvia G Monteiro, Aleksandro S Da Silva
Chagas disease is an acute or chronic illness that causes severe inflammatory response, and consequently, it may activate the inflammatory cholinergic pathway, which is regulated by cholinesterases, including the acetylcholinesterase. This enzyme is responsible for the regulation of acetylcholine levels, an anti-inflammatory molecule linked to the inflammatory response during parasitic diseases. Thus, the aim of this study was to investigate whether Trypanosoma cruzi infection can alter the activity of acetylcholinesterase and acetylcholine levels in mice, and whether these alterations are linked to the inflammatory cholinergic signaling pathway...
August 1, 2017: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/28766156/a-primer-on-nerve-agents-what-the-emergency-responder-anesthesiologist-and-intensivist-needs-to-know
#14
Keith Candiotti
PURPOSE: The purpose of this review article is to familiarize first responders, anesthesiologists, and intensivists with the medical management of patients exposed to nerve agents. SOURCE: This review is based on the current medical literature available to the general medical community. PRINCIPAL FINDINGS: Nerve agents are some of the deadliest substances known to humanity. Though they kill primarily via muscle paralysis, which leads to respiratory arrest, these agents affect virtually every organ system in the body...
August 1, 2017: Canadian Journal of Anaesthesia, Journal Canadien D'anesthésie
https://www.readbyqxmd.com/read/28762049/biogenic-synthesis-of-gold-nanoparticles-from-terminalia-arjuna-bark-extract-assessment-of-safety-aspects-and-neuroprotective-potential-via-antioxidant-anticholinesterase-and-antiamyloidogenic-effects
#15
Natarajan Suganthy, Vijayan Sri Ramkumar, Arivalagan Pugazhendhi, Giovanni Benelli, Govindaraju Archunan
The development of neuroprotective drugs through eco-friendly production routes is a major challenge for current pharmacology. The present study was carried out to synthesize gold nanoparticles (AuNPs) through biogenic route using ethanolic bark extract of Terminalia arjuna, a plant of high interest in Asian traditional medicine, and to evaluate its neuroprotective effects. The synthesized AuNPs were characterized by UV-Vis spectroscopy, FTIR spectroscopy, XRD, FESEM, EDX, HRTEM, DLS, and zeta potential analyses...
July 31, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28760642/galantamine-administration-reduces-reactive-astrogliosis-and-upregulates-the-anti-oxidant-enzyme-catalase-in-rats-submitted-to-neonatal-hypoxia-ischemia
#16
F K Odorcyk, F Nicola, L E Duran-Carabali, F Figueiró, J Kolling, A Vizuete, E L Konrath, C A Gonçalves, A T S Wyse, C A Netto
Neonatal hypoxia ischemia (HI) plays a role in the etiology of several neurological pathologies and causes severe sequelae. Acetylcholine is a neurotransmitter in the central nervous system and cholinesterase inhibitors have demonstrated a positive action over HI induced deficits. In order to evaluate the effects of pre and post-hypoxia administrations of galantamine, a cholinesterase inhibitor, in a model of perinatal HI, Wistar rats in the post-natal day 7 (PND7) were subjected to a combination of unilateral occlusion of the right carotid artery with the exposure to a 1h hypoxia...
July 29, 2017: International Journal of Developmental Neuroscience
https://www.readbyqxmd.com/read/28757214/vulnerability-of-marsh-frog-pelophylax-ridibundus-to-the-typical-wastewater-effluents-ibuprofen-triclosan-and-estrone-detected-by-multi-biomarker-approach
#17
Halina I Falfushynska, Lesya L Gnatyshyna, Oksana Horyn, Oksana B Stoliar
Pharmaceutical and personal care products (PPCPs) are the environmental pollutants of growing concern. The aim of this study was to indicate the effects of typical PPCPs on the marsh frog Pelophylax ridibundus. We treated male frogs with waterborne ibuprofen (IBU, 250ng·L(-1)), triclosan (TCS, 500ng·L(-1)), or estrone (E1, 100ng·L(-1)) for 14days. Common vulnerability of the frogs was detected from dramatic decrease of Zn, total and metalated metallothionein (MT) concentrations, Zn/Cu ratio, the elevation of activity of glutathione-S-transferase, cathepsin D and DNA instability in the liver, the depletion of cholinesterase in the brain and cortisol in the blood plasma in all exposures...
July 27, 2017: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
https://www.readbyqxmd.com/read/28756012/design-synthesis-and-pharmacological-evaluation-of-a-novel-series-of-hormone-sensitive-lipase-inhibitor
#18
Tomoko Ogiyama, Mitsuhiro Yamaguchi, Nobuya Kurikawa, Shoko Honzumi, Koji Terayama, Nobumi Nagaoka, Yuka Yamamoto, Takako Kimura, Daisuke Sugiyama, Shin-Ichi Inoue
HSL inhibition is a promising approach to the treatment of dyslipidemia. As a result of re-optimization of lead compound 2, we identified novel compound 25a exhibiting potent inhibitory activity against HSL enzyme and cell with high selectivity for cholinesterases (AChE and BuChE). Reflecting its potent in vitro activity, compound 25a exhibited antilipolytic effect in rats at 1mg/kg p.o., which indicated that this novel compound is the most potent orally active HSL inhibitor. Moreover, compound 25a did not show bioactivation liability...
July 17, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28752503/trends-in-drug-prescription-rates-for-dementia-an-observational-population-based-study-in-france-2006-2014
#19
Mathilde François, Jonathan Sicsic, Alexis Elbaz, Nathalie Pelletier Fleury
BACKGROUND: Since the 2011 French guidance updates, cholinesterase inhibitors and memantine are considered optional in the management of dementia and leave physicians free to prescribe based on their clinical expertise. OBJECTIVES: The aims of this study were to analyze the influence of these recent guidance updates on the prescription rates of these drugs and to quantify the impact of potential changes on healthcare expenditures. METHODS: Patients over 65 years old from a representative sample of a national administrative claims database, the French national health insurance database, were retrospectively included from 2006 to 2014...
July 27, 2017: Drugs & Aging
https://www.readbyqxmd.com/read/28751142/design-synthesis-and-biological-evaluation-of-dual-acetylcholinesterase-and-phosphodiesterase-5a-inhibitors-in-treatment-for-alzheimer-s-disease
#20
Li-Yun Zhou, Yao Zhu, Yu-Ren Jiang, Xiong-Jie Zhao, Dong Guo
With the recent research advances in molecular biology and technology, multiple credible hypotheses about the progress of Alzheimer's disease (AD) have been proposed; multi-target drugs have emerged as an innovative therapeutic approach for AD. Current clinical therapy for AD patients is mainly palliative treatment targeting acetylcholinesterase (AChE). Inhibition of phosphodiesterase 5A (PDE5A) has recently been validated as a potentially novel therapeutic approach for Alzheimer's disease (AD). In this work, series of new compounds were designed, synthesized and evaluated as dual cholinesterase and PDE5A inhibitor...
July 4, 2017: Bioorganic & Medicinal Chemistry Letters
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