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N-acyl or cannabinoid or NAPE

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https://www.readbyqxmd.com/read/28230380/effects-of-6-hydroxyceramides-on-the-thermotropic-phase-behavior-and-permeability-of-model-skin-lipid-membranes
#1
Andrej Kovacik, Michaela Silarova, Petra Pullmannová, Jaroslav Maixner, Katerina Vavrova
Ceramides (Cer) based on 6-hydroxysphingosine are important components of the human skin barrier, the stratum corneum. Although diminished concentrations of 6-hydroxyCer have been detected in skin diseases such as atopic dermatitis, our knowledge of these unusual sphingolipids, which have only been found in the skin, is limited. In this work, we investigate the biophysical behavior of N-lignoceroyl 6-hydroxysphingosine (Cer NH) in multilamellar lipid membranes composed of Cer/free fatty acids (C16-C24)/cholesterol/cholesteryl sulfate...
February 23, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/28229493/issues-with-monitoring-the-safety-of-psychoactive-products-under-a-legal-regulated-market-for-new-psychoactive-substances-legal-highs-in-new-zealand
#2
Marta Rychert, Chris Wilkins, Karen Witten
INTRODUCTION: New Zealand's Psychoactive Substances Act (2013) established the world's first regulated market for 'low risk' psychoactive products ('legal highs'). Under an interim PSA regime, 47 existing products were permitted to be continued to be sold. AIM: To explore issues with the implementation of regulatory systems to monitor the safety of products on the legal market under the interim Psychoactive Substances Act regime. METHODS: Semi-structured interviews with 30 key stakeholders, including industry, government agency, health and drug service professionals were conducted, transcribed and analysed thematically...
February 23, 2017: Drug and Alcohol Review
https://www.readbyqxmd.com/read/28226397/innate-lymphoid-cells-in-asthma-cannabinoids-on-the-balance
#3
EDITORIAL
Kayluz Frias Boligan, Stephan von Gunten
The network of cells and soluble mediators implicated in the pathogenesis of asthma and allergic disorders is complex. Deciphering details of the crosstalk between its components is essential for the identification of novel drug targets and for advances in patient management and precision medicine (1, 2). There is increasing evidence that innate lymphoid cells (ILCs) contribute to allergic responses (3). This article is protected by copyright. All rights reserved.
February 22, 2017: Allergy
https://www.readbyqxmd.com/read/28225877/synthetic-cannabinoids-in-the-kidneys
#4
Alper Alp, Hakan Akdam, Banu Yılmaz Avcıoğlu, Sibel Ersan
Acute kidney injury is an important cause of mortality and morbidity today and can occur due to several reasons. As time, geographic regions, and living conditions change, various etiological agents arise with nephrotoxic effects. Awareness of such nephrotoxic effects has been raised with the increasing frequency of addictive substance use, especially among young people in society.
January 1, 2017: Revista da Associação Médica Brasileira
https://www.readbyqxmd.com/read/28225111/cubr-tbhp-mediated-synthesis-of-n-acyl-sulfonimidamides-via-the-oxidative-cross-coupling-of-sulfonimidamides-and-aldehydes
#5
Ganesh Chandra Nandi, Cijil Raju
N-Acyl sulfonimidamides were synthesized via a Cu-catalyzed double C-H/N-H activation protocol. The imino end of sulfonimidamides was acylated using aldehyde as the acylating agent and t-butyl hydrogen peroxide (TBHP) as the oxidant in acetonitrile (MeCN) at 82 °C. The mild reaction conditions afforded low-to-moderate yields of N-acyl sulfonimidamides with high structural diversity.
February 22, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28225085/aidp-a-novel-n-acyl-homoserine-lactonase-gene-from-antarctic-planococcus-sp
#6
Wah Seng See-Too, Robson Ee, Yan-Lue Lim, Peter Convey, David A Pearce, Wai-Fong Yin, Kok-Gan Chan
Planococcus is a Gram-positive halotolerant bacterial genus in the phylum Firmicutes, commonly found in various habitats in Antarctica. Quorum quenching (QQ) is the disruption of bacterial cell-to-cell communication (known as quorum sensing), which has previously been described in mesophilic bacteria. This study demonstrated the QQ activity of a psychrotolerant strain, Planococcus versutus strain L10.15(T), isolated from a soil sample obtained near an elephant seal wallow in Antarctica. Whole genome analysis of this bacterial strain revealed the presence of an N-acyl homoserine lactonase, an enzyme that hydrolyzes the ester bond of the homoserine lactone of N-acyl homoserine lactone (AHLs)...
February 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28223925/effects-of-intermittent-alcohol-exposure-on-emotion-and-cognition-a-potential-role-for-the-endogenous-cannabinoid-system-and-neuroinflammation
#7
Laura Sanchez-Marin, Francisco J Pavon, Juan Decara, Juan Suarez, Ana Gavito, Estela Castilla-Ortega, Fernando Rodriguez de Fonseca, Antonia Serrano
Intermittent alcohol exposure is a common pattern of adolescent alcohol use that can lead to binge drinking episodes. Alcohol use is known to modulate the endocannabinoid system (ECS), which is involved in neuronal communication, neuroplasticity, neuroinflammation and behavior. Adolescent male Wistar rats were exposed to 4-week intermittent alcohol intoxication (3 g/kg injections for 4 days/week) or saline (N = 12 per group). After alcohol deprivation, adult rats were assessed for emotionality and cognition and the gene expression of the ECS and other factors related to behavior and neuroinflammation was examined in the brain...
2017: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/28222356/extinction-of-avoidance-behavior-by-safety-learning-depends-on-endocannabinoid-signaling-in-the-hippocampus
#8
Vincenzo Micale, Jens Stepan, Angela Jurik, Fabricio A Pamplona, Rudolph Marsch, Filippo Drago, Matthias Eder, Carsten T Wotjak
The development of exaggerated avoidance behavior is largely responsible for the decreased quality of life in patients suffering from anxiety disorders. Studies using animal models have contributed to the understanding of the neural mechanisms underlying the acquisition of avoidance responses. However, much less is known about its extinction. Here we provide evidence in mice that learning about the safety of an environment (i.e., safety learning) rather than repeated execution of the avoided response in absence of negative consequences (i...
February 3, 2017: Journal of Psychiatric Research
https://www.readbyqxmd.com/read/28221034/regioselective-1-4-conjugate-addition-of-grignard-reagents-to-%C3%AE-%C3%AE-%C3%AE-%C3%AE-dienones-and-%C3%AE-%C3%AE-%C3%AE-%C3%AE-dienyl-thiol-esters
#9
Emmanuel Amoah, R Karl Dieter
Alkyl Grignard reagents (Et, nBu, iPr, cyclohexyl), with the exception of tBuMgCl, undergo exclusive or exceptionally highly regioselective 1,4-addition reactions to α,β-γ,δ-unsaturated ketones, while aryl and heteroaryl Grignard reagents give mixed results ranging from exclusive 1,4-addition (1-naphthyl, 2-N-methylpyrrolyl) to regioselective 1,2-addition (2-furyl, 2:1). All alkyl, aryl, and heteroaryl Grignard reagents examined gave exclusive 1,4-addition reactions with α,β-γ,δ-unsaturated thiol esters, with the exception of tBuMgCl which gave an 80:20 mixture of 1,4-:1,6-addition products...
February 21, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28220706/human-cannabinoid-receptor-2-ligand-interaction-motif-transmembrane-helix-2-cysteine-c2-59-89-as-determinant-of-classical-cannabinoid-agonist-activity-and-binding-pose
#10
Han Zhou, Yan Peng, Aneetha Halikhedkar, Pusheng Fan, David R Janero, Ganesh A Thakur, Richard Warren Mercier, Xin Sun, Xiaoyu Ma, Alexandros Makriyannis
Cannabinoid receptor 2 (CB2R)-dependent signaling is implicated in neuronal physiology and immune surveillance by brain microglia. Selective CB2R agonists hold therapeutic promise for inflammatory and other neurological disorders. Information on human CB2R (hCB2R) ligand-binding and functional domains is needed to inform the rational design and optimization of candidate drug-like hCB2R agonists. Prior demonstration that hCB2R transmembrane helix 2 (TMH2) cysteine C2.59(89) reacts with small-molecule methanethiosulfonates showed that this cysteine residue is accessible to sulfhydryl derivatization reagents...
February 21, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28220074/involvement-of-cannabinoid-signaling-in-vincristine-induced-gastrointestinal-dysmotility-in-the-rat
#11
Gema Vera, Ana E López-Pérez, José A Uranga, Rocío Girón, Ma Isabel Martín-Fontelles, Raquel Abalo
Background: In different models of paralytic ileus, cannabinoid receptors are overexpressed and endogenous cannabinoids are massively released, contributing to gastrointestinal dysmotility. The antitumoral drug vincristine depresses gastrointestinal motility and a similar mechanism could participate in this effect. Therefore, our aim was to determine, using CB1 and CB2 antagonists, whether an increased endocannabinoid tone is involved in vincristine-induced gastrointestinal ileus. Methods: First, we confirmed the effects of vincristine on the gut mucosa, by conventional histological techniques, and characterized its effects on motility, by radiographic means...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28220044/pregnenolone-blocks-cannabinoid-induced-acute-psychotic-like-states-in-mice
#12
A Busquets-Garcia, E Soria-Gómez, B Redon, Y Mackenbach, M Vallée, F Chaouloff, M Varilh, G Ferreira, P-V Piazza, G Marsicano
Cannabis-induced acute psychotic-like states (CIAPS) represent a growing health issue, but their underlying neurobiological mechanisms are poorly understood. The use of antipsychotics and benzodiazepines against CIAPS is limited by side effects and/or by their ability to tackle only certain aspects of psychosis. Thus, safer wide-spectrum treatments are currently needed. Although the blockade of cannabinoid type-1 receptor (CB1) had been suggested as a therapeutical means against CIAPS, the use of orthosteric CB1 receptor full antagonists is strongly limited by undesired side effects and low efficacy...
February 21, 2017: Molecular Psychiatry
https://www.readbyqxmd.com/read/28219782/characterization-of-phospholipid-nitroxidation-by-lc-ms-in-biomimetic-models-and-in-h9c2-myoblast-using-a-lipidomic-approach
#13
Tânia Melo, Pedro Domingues, Teresa M Ribeiro-Rodrigues, Henrique Girão, Marcela A Segundo, M Rosário M Domingues
Under nitroxidative stress conditions, lipids are prone to be modified by reaction with reactive nitrogen species (RNS) and different modifications were reported to occur in fatty acids. However, in the case of phospholipids (PL) studied under nitroxidative stress conditions, only nitroalkene derivatives of phosphatidylcholine (PC) and phosphatidylethanolamine (PE), were reported when using both in vitro biomimetic conditions and in vivo model system of type 1 diabetes mellitus. Therefore, in order to further explore other nitroxidative modifications of PL, a biomimetic model of nitroxidation combined with liquid chromatography mass spectrometry (MS) and MS/MS approaches were used to characterize the nitrated and nitroxidized derivatives of PCs and PEs...
February 17, 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28219717/effects-of-tetrahydrocannabinol-on-glucose-uptake-in-the-rat-brain
#14
I Miederer, K Uebbing, J Röhrich, S Maus, N Bausbacher, K Krauter, V Weyer-Elberich, B Lutz, M Schreckenberger, R Urban
Δ(9)-Tetrahydrocannabinol (THC) is the psychoactive component of the plant Cannabis sativa and acts as a partial agonist at cannabinoid type 1 and type 2 receptors in the brain. The goal of this study was to assess the effect of THC on the cerebral glucose uptake in the rat brain. 21 male Sprague Dawley rats (12-13 w) were examined and received five different doses of THC ranging from 0.01 to 1 mg/kg. For data acquisition a Focus 120 small animal PET scanner was used and 24.1-28.0 MBq of [(18)F]-fluoro-2-deoxy-d-glucose were injected...
February 17, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28219703/immunomodulatory-properties-of-1-2-dihydro-4-hydroxy-2-oxo-1-8-naphthyridine-3-carboxamide-derivative-vl15
#15
Anna Maria Malfitano, Chiara Laezza, Simone Bertini, Daniela Marasco, Tiziano Tuccinardi, Maurizio Bifulco, Clementina Manera
1,2-dihydro-4-hydroxy-2-oxo-1,8-naphthyridine-3-carboxamide derivative VL15 has been recently developed as a selective cannabinoid CB2 receptor compound. Given the high selectivity of this compound at the cannabinoid CB2 receptor and the well-known protective function of this receptor in neurological disorders with autoimmune component like multiple sclerosis, we assessed the immunomodulatory properties of VL15. We assessed on activated peripheral blood mononuclear cells (PBMC), proliferation and viability, cell cycle progression and measured activation markers and the expression of phosphorylated proteins...
February 17, 2017: Biochimie
https://www.readbyqxmd.com/read/28219487/evidence-for-the-risks-and-consequences-of-adolescent-cannabis-exposure
#16
REVIEW
Amir Levine, Kelly Clemenza, Moira Rynn, Jeffrey Lieberman
OBJECTIVE: This review of the scientific literature examines the potential adult sequelae of exposure to cannabis and related synthetic cannabinoids in adolescence. We examine the four neuropsychiatric outcomes that are likely most vulnerable to alteration by early cannabinoid use, as identified within both the clinical and preclinical research: cognition, emotional functioning, risk for psychosis, and addiction. METHOD: A literature search was conducted through PubMed, PsychInfo, and Google Scholar with no publication date restrictions...
March 2017: Journal of the American Academy of Child and Adolescent Psychiatry
https://www.readbyqxmd.com/read/28218780/microrna-139-modulates-alzheimer-s-associated-pathogenesis-in-samp8-mice-by-targeting-cannabinoid-receptor-type-2
#17
Y Tang, J S Bao, J H Su, W Huang
Alzheimer's disease (AD) is a neurodegenerative disorder, and is the most common type of dementia in the elderly population. Growing evidence indicates that microRNAs (miRNAs) play a crucial role in neuroinflammation associated with AD progression. In this study, we analyzed the expression of microRNA-139 (miR-139) as well as the learning and memory function in AD. We observed that the miR-139 expression was significantly higher in the hippocampus of aged senescence accelerated mouse prone 8 (SAMP8) mice (2...
February 16, 2017: Genetics and Molecular Research: GMR
https://www.readbyqxmd.com/read/28218648/expression-purification-and-monitoring-of-conformational-changes-of-hcb2-tmh67h8-in-different-membrane-mimetic-lipid-mixtures-using-circular-dichroism-and-nmr-techniques
#18
Elvis K Tiburu, Jianqin Zhuang, Heidimarie N A Fleischer, Patrick K Arthur, Gordon A Awandare
This work was intended to develop self-assembly lipids for incorporating G-protein coupled receptors (GPCRs) in order to improve the success rate for nuclear magnetic resonance spectroscopy (NMR) structural elucidation. We hereby report the expression and purification of uniformly (15)N-labeled human cannabinoid receptor-2 domain in insect cell media. The domain was refolded by screening several membrane mimetic environments. Different q ratios of isotropic bicelles were screened for solubilizing transmembrane helix 6, 7 and 8 (TMH67H8)...
February 17, 2017: Membranes
https://www.readbyqxmd.com/read/28215997/cannabinoids-and-epilepsy-introduction
#19
EDITORIAL
Jerzy P Szaflarski, Orrin Devinsky
No abstract text is available yet for this article.
February 16, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28215162/gut-brain-axis-role-of-lipids-in-the-regulation-of-inflammation-pain-and-cns-diseases
#20
Roberto Russo, Claudia Cristiano, Carmen Avagliano, Carmen De Caro, Giovanna La Rana, Giuseppina Mattace Raso, Roberto Berni Canani, Rosaria Meli, Antonio Calignano
The human gut is a composite anaerobic environment with a large, diverse and dynamic enteric microbiota, represented by more than 100 trillion microorganisms, including at least 1000 distinct species. The discovery that a different microbial composition can influence behavior and cognition, and in turn the nervous system can indirectly influence enteric microbiota composition, has significantly contributed to establish the well-accepted concept of gut-brain axis. This hypothesis is supported by several evidence showing mutual mechanisms, which involve the vague nerve, the immune system, the hypothalamic-pituitary-adrenal (HPA) axis modulation and the bacteria-derived metabolites...
February 16, 2017: Current Medicinal Chemistry
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