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https://www.readbyqxmd.com/read/29040957/molecular-docking-and-antiamnesic-effects-of-nepitrin-isolated-from-rosmarinus-officinalis-on-scopolamine-induced-memory-impairment-in-mice
#1
Nasiara Karim, Imran Khan, Abeer Abdelhalim, Heba Abdel-Halim, Jane R Hanrahan
Rosmarinus officinalis has long been known as the herb of remembrance. The present study was undertaken to investigate the anti-amnesic effects of nepitrin isolated from Rosmarinus officinalis using in-vivo models of Y-maze and novel object recognition test (NORT) along with in vitro antioxidant and acetylcholinesterase (AChE) and buterylcholinesterase (BuChE) inhibition potential. Nepitrin showed a concentration dependent inhibition of AChE and BuChE enzymes with IC50 values of 65 and 72μg/mL, respectively and antioxidant activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2, 2'-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) with IC50 values 270 and 210μg/mL, respectively...
October 14, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29034738/chemodiversity-of-nepeta-menthoides-boiss-bohse-essential-oil-from-iran-and-antimicrobial-acetylcholinesterase-inhibitory-and-cytotoxic-properties-of-1-8-cineole-chemotype
#2
Niloofar Kahkeshani, Abbas Hadjiakhoondi, Latifeh Navidpour, Tahmineh Akbarzadeh, Malihe Safavi, Elahe Karimpour-Razkenari, Mahnaz Khanavi
The essential oil of Nepeta menthoides Boiss. & Bohse., from Iran, was analysed by GC/MS. Two types of multivariate analyses were done based on the chemical composition of the investigated sample in this study and 12 other samples reported in the literature to show the chemodiversity in essential oil composition. Antimicrobial, acetylcholinesterase inhibitory and cytotoxic activities of the essential oil and its major component were assessed. Twenty-one compounds were identified, representing 96.81% of the total oil and the major constituent was 1,8-cineole (70...
October 15, 2017: Natural Product Research
https://www.readbyqxmd.com/read/29033787/a-novel-ex-vivo-model-to-investigate-the-underlying-mechanisms-in-alzheimer-s-disease
#3
Emanuele Brai, Skye Stuart, Antoine-Scott Badin, Susan A Greenfield
Currently there is no widely accepted animal model reproducing the full pathological profile of Alzheimer's disease (AD), since the basic mechanisms of neurodegeneration are still poorly understood. We have proposed that the interaction between the α7 nicotinic acetylcholine receptor (α7-nAChR) and a recently discovered toxic peptide, cleaved from the acetylcholinesterase (AChE) C-terminus, could account for the aberrant processes occurring in AD. In this article we describe a new application on ex vivo model procedure, which combines the advantages of both in vivo and in vitro preparations, to study the effects of the AChE-derived peptide on the rat basal forebrain (BF)...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/29031972/selective-two-dimensional-effect-directed-analysis-with-thin-layer-chromatography
#4
Lena Stütz, Stefan C Weiss, Wolfgang Schulz, Wolfgang Schwack, Rudi Winzenbacher
There are thousands of organic trace substances in the environment that are not fully characterized, and evaluation of their relevance to the ecosystem is difficult. Effect-directed analysis (EDA) is a suitable tool to assess the effects of a substance via in-vitro bioassays, which can provide information about the relevance of the substance. High-performance thin-layer chromatography (HPTLC) has been shown to be a good method for fractionation. Environmental samples, however, often have high complexity, which is why the peak capacity of HPTLC is not sufficient...
October 6, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/29031576/acute-and-long-term-effects-of-trophic-exposure-to-silver-nanospheres-in-the-central-nervous-system-of-a-neotropical-fish-hoplias-intermedius
#5
T Klingelfus, J R Lirola, L F Oya Silva, G R Disner, M Vicentini, M J B Nadaline, J C Z Robles, L M Trein, C L Voigt, H C Silva de Assis, M Mela, D M Leme, M M Cestari
Nanotechnologies are at the center of societal interest, due to their broad spectrum of application in different industrial products. The current concern about nanomaterials (NMs) is the potential risks they carry for human health and the environment. Considering that NMs can reach bodies of water, there is a need for studying the toxic effects of NMs on aquatic organisms. Among the NMs' toxic effects on fish, the interactions between NMs and the nervous system are yet to be understood. For this reason, our goal was to assess the neurotoxicity of polyvinylpyrrolidone coated silver nanospheres [AgNS (PVP coated)] and compare their effects in relation to silver ions (Ag(+)) in carnivorous Hoplias intermedius fish after acute and subchronic trophic exposure through the analysis of morphological (retina), biochemical (brain) and genetic biomarkers (brain and blood)...
October 11, 2017: Neurotoxicology
https://www.readbyqxmd.com/read/29031067/new-pyridine-derivatives-as-inhibitors-of-acetylcholinesterase-and-amyloid-aggregation
#6
Fabiana Pandolfi, Daniela De Vita, Martina Bortolami, Antonio Coluccia, Roberto Di Santo, Roberta Costi, Vincenza Andrisano, Francesco Alabiso, Christian Bergamini, Romana Fato, Manuela Bartolini, Luigi Scipione
A new series of pyridine derivatives with carbamic or amidic function has been designed and synthesized to act as cholinesterase inhibitors. The synthesized compounds were tested toward EeAChE and hAChE and toward eqBChE and hBChE. The carbamate 8 was the most potent hAChE inhibitor (IC50 = 0.153 ± 0.016 μM) while the carbamate 11 was the most potent inhibitor of hBChE (IC50 = 0.828 ± 0.067 μM). A molecular docking study indicated that the carbamate 8 was able to bind AChE by interacting with both CAS and PAS, in agreement with the mixed inhibition mechanism...
September 18, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29030875/protection-of-grain-products-from-sitophilus-oryzae-l-contamination-by-anti-insect-pest-repellent-sachet-containing-allyl-mercaptan-microcapsule
#7
Yoonjee Chang, Soo-Hyun Lee, Ja Hyun Na, Pahn-Shick Chang, Jaejoon Han
The purpose of this study was to develop an anti-insect pest repellent sachet to prevent Sitophilus oryzae (L.) (Coleoptera: Curculionidae) contamination in grain packaging. The anti-insect pest activities of essential oils (EOs) from garlic (Allium Sativum), ginger (Zingiber Officinalis), black pepper (Piper nigrum), onion (Allium cepa), and fennel (Foeniculum vulgare) as well as major compounds (allyl disulfide, AD; allyl mercaptan, AM) isolated from of garlic and onion (AD and AM) were measured against S...
October 14, 2017: Journal of Food Science
https://www.readbyqxmd.com/read/29030431/distinctive-modulation-of-dopamine-release-in-the-nucleus-accumbens-shell-mediated-by-dopamine-and-acetylcholine-receptors
#8
Jung Hoon Shin, Martin F Adrover, Veronica A Alvarez
Nucleus accumbens (NAc) shell shows unique dopamine (DA) signals in vivo and plays a unique role in DA dependent behaviors, such as reward-motivated learning and the response to drugs of abuse. A di-synaptic mechanism for DA release was reported and shown to require synchronized firing of cholinergic interneurons (CINs) and activation of nicotinic acetylcholine (ACh) receptors (nAChRs) in DA neuron (DAN) axons. The properties of this di-synaptic mechanism of DA transmission is not well understood in the NAc shell...
October 13, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29029320/insecticidal-mechanism-of-wintergreen-oil-against-the-health-pest-paederus-fuscipes-coleoptera-staphylinidae
#9
Zhiping Liu, Qiang Zhang, Xuan Wu, Wei Yu, Shengquan Guo
Paederus fuscipes, a health pest, causes dermatitis linearis in humans. Wintergreen oil exhibits optimal insecticidal activity against P. fuscipes. However, the insecticidal mechanism remains unclear not only in P. fuscipes but also in other pests. In this study, we explored the insecticidal mechanism of wintergreen oil in terms of its effect on the activity of acetylcholinesterase (AChE) enzyme and detoxifying enzymes (carboxylesterase, glutathione-S-transferase, and mixed function oxidase); such effect was studied by fumigation both in vivo and in vitro in P...
October 4, 2017: Journal of Medical Entomology
https://www.readbyqxmd.com/read/29027091/walnut-supplementation-reverses-the-scopolamine-induced-memory-impairment-by-restoration-of-cholinergic-function-via-mitigating-oxidative-stress-in-rats-a-potential-therapeutic-intervention-for-age-related-neurodegenerative-disorders
#10
Saida Haider, Zehra Batool, Saara Ahmad, Rafat Ali Siddiqui, Darakhshan Jabeen Haleem
The brain is highly susceptible to the damaging effects of oxidative reactive species. The free radicals which are produced as a consequence of aerobic respiration can cause cumulative oxygen damage which may lead to age-related neurodegeneration. Scopolamine, the anti-muscarinic agent induces amnesia and oxidative stress similar to that observed in the older age. Studies suggest that antioxidants derived from plant products may provide protection against oxidative stress. Therefore, the present study was designed to investigate the attenuation of scopolamine-induced memory impairment and oxidative stress by walnut supplementation in rats...
October 12, 2017: Metabolic Brain Disease
https://www.readbyqxmd.com/read/29026987/acetylcholinesterase-activity-and-time-after-a-peak-pesticide-use-period-among-ecuadorian-children
#11
Jose Ricardo Suarez-Lopez, Cheyenne R Butcher, Sheila Gahagan, Harvey Checkoway, Bruce H Alexander, Wael K Al-Delaimy
PURPOSE: Mother's Day (May) is a holiday with substantial demand for flowers, associated with heightened flower production and escalated pesticide use. The effect of spray seasons on pesticide exposures of children living in agricultural communities but who do not work in agriculture is poorly understood. In this study, we estimated the association of time after Mother's Day harvest with children's acetylcholinesterase (AChE) activity. AChE is a physiological marker of organophosphate/carbamate pesticide exposures that may take up to 3 months to normalize after its inhibition...
October 13, 2017: International Archives of Occupational and Environmental Health
https://www.readbyqxmd.com/read/29026496/the-effects-of-gestational-and-lactational-exposure-to-nonylphenol-on-c-jun-and-c-fos-expression-and-learning-and-memory-in-hippocampus-of-male-f1-rat
#12
Yu Jie, Wang Pan, Yan Wenxia, Gao Feng, He Liting, Li Wenmei, Xu Jie
OBJECTIVES: To investigate the effects of Nonylphenol (NP) in pups from dams exposed during gestational and lactational periods on immediate early genes (c-jun, c-fos) in hippocampus and the learning and memory of F1 rats. MATERIALS AND METHODS: Twenty eight pregnant dams, stratified by pregnancy date, were randomly assigned into 4 groups, which were gavaged with NP at the doses of 50 mg/kg/day, 100 mg/kg/day, 200 mg/kg/day and groundnut oil, respectively. Step-down avoidance test, and learning and memory effects of NP were evaluated on 8-weeks-old pups...
April 2017: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/29024789/in-vitro-pharmacological-characterization-of-the-bispyridinium-non-oxime-compound-mb327-and-its-2-and-3-regioisomers
#13
K V Niessen, T Seeger, S Rappenglück, T Wein, G Höfner, K T Wanner, H Thiermann, F Worek
The primary toxic mechanism of organophosphorus compounds, i.e. nerve agents or pesticides, is based on the irreversible inhibition of acetylcholinesterase. In consequence of the impaired hydrolysis, the neurotransmitter acetylcholine accumulates in cholinergic synapses and disturbs functional activity of nicotinic and muscarinic acetylcholine receptors by overstimulation and subsequent desensitization. The resulting cholinergic syndrome will become acute life-threatening, if not treated adequately. The current standard treatment, consisting of administration of a competitive mAChR antagonist (e...
October 9, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/29023806/the-percutaneous-toxicokinetics-of-vx-in-a-damaged-skin-porcine-model-and-the-evaluation-of-woundstat%C3%A2-as-a-topical-decontaminant
#14
Helen Lydon, Charlotte Hall, Hazem Matar, Christopher Dalton, J Kevin Chipman, John S Graham, Robert P Chilcott
This study used a damaged skin, porcine model to evaluate the in vivo efficacy of WoundStat™ for the decontamination of superficial, nerve agent-contaminated wounds. Anaesthetized animals were randomly assigned to either control (n = 7), no decontamination (n = 12) or WoundStat™ (n = 12) treatment groups. Pigs were exposed to a 5× LD50 dose of neat, radiolabelled S-[2-(diisopropylamino)ethyl]-O-ethyl methyl-phosphonothioate (VX; or equivalent volume of sterile saline for the control group) via an area of superficially damaged skin on the ear...
October 10, 2017: Journal of Applied Toxicology: JAT
https://www.readbyqxmd.com/read/29022183/in-search-of-a-comprehensible-set-of-endpoints-for-the-routine-monitoring-of-neurotoxicity-in-vertebrates-sensory-perception-and-nerve-transmission-in-zebrafish-danio-rerio-embryos
#15
Daniel Stengel, Sarah Wahby, Thomas Braunbeck
In order to develop a test battery based on a variety of neurological systems in fish, three sensory systems (vision, olfaction, and lateral line) as well as nerve transmission (acetylcholine esterase) were analyzed in zebrafish (Danio rerio) embryos with respect to their suitability as a model for the screening of neurotoxic trace substances in aquatic ecosystems. As a selection of known or putative neurotoxic compounds, amidotrizoic acid, caffeine, cypermethrin, dichlorvos, 2,4-dinitrotoluene, 2,4-dichlorophenol, 4-nonylphenol, perfluorooctanoic acid, and perfluorooctane sulfonic acid were tested in the fish embryo test (OECD test guideline 236) to determine EC10 values, which were then used as maximum test concentration in subsequent neurotoxicity tests...
October 12, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/29019446/the-role-of-the-oximes-hi-6-and-hs-6-inside-human-acetylcholinesterase-inhibited-with-nerve-agents-a-computational-study
#16
Teobaldo Cuya, Arlan da Silva Gonçalves, Jorge Alberto Valle da Silva, Teodorico C Ramalho, Kamil Kuca, Tanos C C França
Abstracts The oximes 4-carbamoyl-1-[({2-[(E)-(hydroxyimino) methyl] pyridinium-1-yl} methoxy) methyl] pyridinium (known as HI-6) and 3-carbamoyl-1-[({2-[(E)-(hydroxyimino) methyl] pyridinium-1-yl} methoxy) methyl] pyridinium (known as HS-6) are isomers differing from each other only by the position of the carbamoyl group on the pyridine ring. However this slight difference was verified to be responsible for big differences in the percentual of reactivation of acetylcholinesterase (AChE) inhibited by the nerve agents tabun, sarin, cyclosarin and VX...
October 11, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/29019394/studies-on-16-17-pyrazoline-substituted-heterosteroids-as-anti-alzheimer-and-anti-parkinsonian-agents-using-lps-induced-neuroinflammation-models-of-mice-and-rats
#17
Ranjit Singh, Sridhar Thota, Ranju Bansal
Alzheimer's disease (AD) and Parkinson's disease (PD) are the most common forms of neurodegenerative disorders. Dehydroepiandrosterone (DHEA) has been reported as a neuroprotective steroid useful in the therapeutic management of neurodegenerative disorders such as AD and PD. Herein we report the synthesis and evaluation of a new series of 16,17-pyrazolinyl DHEA analogues 2-4a-d as neuroprotective agents using LPS-induced neuroinflammation animal models. Treatment with the pyrazoline substituted steroids considerably improved the LPS-induced learning, memory and movement deficits in animal models...
October 11, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29017403/protective-effect-of-zizyphus-lotus-jujube-fruits-against-cypermethrin-induced-oxidative-stress-and-neurotoxicity-in-mice
#18
Khazri Abdelhafidh, Lazher Mhadhbi, Ali Mezni, Sellami Badreddine, Hamouda Beyrem, Ezzeddine Mahmoudi
CONTEXT: Cypermethrin (CYP) is a synthetic pyrethroid insecticide used worldwide in agriculture, home pest control. The toxicity of CYP is well studied in many organisms Objective: The aim of present study was to investigate the protective effect of Zizyphus lotus (Zizyp) fruit against neurotoxicity and oxidative stress induced by CYP in mice. MATERIALS AND METHODS: Mice were divided into four groups of six each: groups I and II were used as control and CYP control (20mg/kg body weight)...
October 11, 2017: Biomarkers: Biochemical Indicators of Exposure, Response, and Susceptibility to Chemicals
https://www.readbyqxmd.com/read/29017096/enhancing-mir-132-expression-by-aryl-hydrocarbon-receptor-attenuates-tumorigenesis-associated-with-chronic-colitis
#19
Abdullah M Alzahrani, Hamza Hanieh, Hairul-Islam Mohamed Ibrahim, Omar Mohafez, Tamer Shehata, Mohammad Bani Ismail, Manal Alfwuaires
BACKGROUND: Chronic inflammation in ulcerative colitis (UC) patients is the major risk factor for colitis-associated colon cancer (CAC). Recent evidences have shown that microRNAs (miRNAs) are implicated in CAC pathogenesis. However, the interaction of miRNAs with the transcription factors that alleviate CAC has not been reported. METHODS: 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) or 3,3'-diindolylmethane (DIM) were used to activate aryl hydrocarbon receptor (Ahr) in azoxymethane (AOM)/dextran sodium sulfate (DSS)-induced CAC in mice...
October 7, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/29017007/dmso-a-mixed-competitive-inhibitor-of-human-acetylcholinesterase
#20
Amit Kumar, Taher Darreh-Shori
Dimethyl sulfoxide (DMSO) is the most common organic solvent used in biochemical and cellular assays during drug discovery programs. Despite its wide use, the effect of DMSO on several enzyme classes, which are crucial targets of the new therapeutic agents, are still unexplored. Here, we report the detailed biochemical analysis of the effects of DMSO on the human acetylcholine-degrading enzyme, acetylcholinesterase (AChE), the primary target of current Alzheimer's therapeutics. Our analysis showed that DMSO is a considerably potent and highly selective irreversible mixed-competitive inhibitor of human AChE with IC50 values in the lower millimolar range, corresponding to 0...
October 16, 2017: ACS Chemical Neuroscience
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