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N-acyl or cannabinoid or NAPE

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https://www.readbyqxmd.com/read/27909709/synthesis-of-a-fluorescent-photoaffinity-probe-of-osw-1-by-site-selective-acylation-of-an-inactive-congener-and-biological-evaluation
#1
K Sakurai, M Hiraizumi, N Isogai, R Komatsu, T Shibata, Y Ohta
A novel fluorescent photoaffinity probe of OSW-1 was prepared in two steps from a naturally occurring inactive congener by a sequential site-selective acylation strategy using Me2SnCl2. It displayed highly potent anticancer activity and a similar intracellular localization property to that of a fluorescently-tagged OSW-1, thereby demonstrating its potential utility in live cell studies.
December 2, 2016: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/27909432/volatile-mediated-effects-predominate-in-paraburkholderia-phytofirmans-growth-promotion-and-salt-stress-tolerance-of-arabidopsis-thaliana
#2
Thomas Ledger, Sandy Rojas, Tania Timmermann, Ignacio Pinedo, María J Poupin, Tatiana Garrido, Pablo Richter, Javier Tamayo, Raúl Donoso
Abiotic stress has a growing impact on plant growth and agricultural activity worldwide. Specific plant growth promoting rhizobacteria have been reported to stimulate growth and tolerance to abiotic stress in plants, and molecular mechanisms like phytohormone synthesis and 1-aminocyclopropane-1-carboxylate deamination are usual candidates proposed to mediate these bacterial effects. Paraburkholderia phytofirmans PsJN is able to promote growth of several plant hosts, and improve their tolerance to chilling, drought and salinity...
2016: Frontiers in Microbiology
https://www.readbyqxmd.com/read/27909319/the-cannabinoid-receptor-1-as-a-key-mediator-of-adolescent-behavior
#3
Rainer Spanagel, Falk Kiefer
No abstract text is available yet for this article.
January 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27909291/engineering-of-a-thermostable-esterase-est816-to-improve-its-quorum-quenching-activity-and-the-underlying-structural-basis
#4
Xiwen Liu, Li-Chuang Cao, Xin-Jiong Fan, Yu-Huan Liu, Wei Xie
N-acyl-homoserine lactones (AHLs) are small diffusible molecules called autoinducers that mediate cell-to-cell communications. Enzymatic degradation of AHLs is a promising bio-control strategy known as quorum-quenching. To improve the quorum-quenching activity of a thermostable esterase Est816, which had been previously cloned, we have engineered the enzyme by random mutagenesis. One of the mutants M2 with double amino acid substitutions (A216V/K238N) showed 3-fold improvement on catalytic efficiency. Based on the crystal structure determined at 2...
December 2, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27908729/structural-and-biochemical-characterization-of-fabk-from-thermotoga-maritima
#5
Byung Hak Ha, Sang Chul Shin, Jin Ho Moon, Gyochang Keum, Chan-Wha Kim, Eunice EunKyeong Kim
TM0800 from Thermotoga maritima is one of the hypothetical proteins with unknown function. The crystal structure determined at 2.3 Å resolution reveals a two domain structure: the N-terminal domain forming a barrel and the C-terminal forming a lid. One FMN is bound between the two domains with the phosphate making intricate hydrogen bonds with protein and three tightly bound water molecules, and the isoalloxazine ring packed against the side chains of Met22 and Met276. The structure is almost identical to that of FabK (enoyl-acyl carrier protein (ACP) reductase, ENR II), a key enzyme in bacterial type II fatty-acid biosynthesis that catalyzes the final step in each elongation cycle; and the enzymatic activity confirms that TM0800 is an ENR...
November 28, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27905022/neurophysiology-of-space-travel-energetic-solar-particles-cause-cell-type-specific-plasticity-of-neurotransmission
#6
Sang-Hun Lee, Barna Dudok, Vipan K Parihar, Kwang-Mook Jung, Miklós Zöldi, Young-Jin Kang, Mattia Maroso, Allyson L Alexander, Gregory A Nelson, Daniele Piomelli, István Katona, Charles L Limoli, Ivan Soltesz
In the not too distant future, humankind will embark on one of its greatest adventures, the travel to distant planets. However, deep space travel is associated with an inevitable exposure to radiation fields. Space-relevant doses of protons elicit persistent disruptions in cognition and neuronal structure. However, whether space-relevant irradiation alters neurotransmission is unknown. Within the hippocampus, a brain region crucial for cognition, perisomatic inhibitory control of pyramidal cells (PCs) is supplied by two distinct cell types, the cannabinoid type 1 receptor (CB1)-expressing basket cells (CB1BCs) and parvalbumin (PV)-expressing interneurons (PVINs)...
November 30, 2016: Brain Structure & Function
https://www.readbyqxmd.com/read/27903654/carbon-and-acyl-chain-flux-during-stress-induced-triglyceride-accumulation-by-stable-isotopic-labeling-of-the-polar-microalga-coccomyxa-subellipsoidea-c169
#7
James W Allen, Concetta C DiRusso, Paul N Black
Deriving biofuels and other lipoid products from algae is a promising future technology directly addressing global issues of atmospheric CO2 balance. To better understand the metabolism of triglyceride synthesis in algae, we examined their metabolic origins in the model species, Coccomyxa subellipsoidea C169, using stable isotopic labeling. Labeling patterns arising from (13)C-U-glucose, (13)CO2, or D2O supplementation were analyzed by GC-MS and/or LC-MS over time courses during nitrogen (N) starvation to address the roles of catabolic carbon (C) recycling, acyl chain redistribution, and de novo fatty acid (FA) synthesis during the expansion of the lipid bodies...
November 30, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27903642/behavioral-characterization-of-kappa-opioid-receptor-agonist-spiradoline-and-cannabinoid-receptor-agonist-cp55940-mixtures-in-rats
#8
Vanessa Minervini, Sujata S Dahal, Charles France
Pain is a significant clinical problem and there is a need for more effective treatments with reduced adverse effects that currently limit the use of mu opioid receptor agonists. Synthetic kappa opioid receptor agonists have no abuse liability and well-documented antinociceptive effects; however, adverse effects (diuresis, dysphoria) preclude their use in the clinic. Combining kappa opioids with non-opioid drugs (cannabinoid receptor agonists) allows for smaller doses of each drug to produce antinociception...
November 30, 2016: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27903595/lifelong-imbalanced-linoleic-alpha-linolenic-acid-intake-impairs-emotional-and-cognitive-behavior-in-adult-rats-via-changes-in-brain-endocannabinoid-system
#9
Erica Zamberletti, Fabiana Piscitelli, Valentina De Castro, Elisabetta Murru, Marina Gabaglio, Paola Colucci, Chiara Fanali, Pamela Prini, Tiziana Bisogno, Mauro Maccarrone, Patrizia Campolongo, Sebastiano Banni, Tiziana Rubino, Daniela Parolaro
Imbalanced dietary n-3 and n-6 PUFA content has been associated with a number of neurological conditions. Endocannabinoids are n-6 PUFA derivatives, whose brain concentrations are sensitive to modifications of fatty acid composition of the diet, and play a central role in the regulation of mood and cognition. As such, the endocannabinoid system appears to be an ideal candidate for mediating the effects of dietary fatty acids on mood and cognition. Lifelong administration of isocaloric alpha linolenic acid (ALA) deficient and enriched diets induced short-term memory deficits, whereas only dietary ALA enrichment altered emotional reactivity in adult male rats compared to animals fed a standard diet, balanced in ALA/linoleic (LA) ratio...
November 30, 2016: Journal of Lipid Research
https://www.readbyqxmd.com/read/27900697/screening-for-n-ahsl-based-signaling-interfering-enzymes
#10
Stéphane Uroz, Phil M Oger
Quorum sensing (QS)-based signaling is a widespread pathway used by bacteria for the regulation of functions involved in their relation to the environment or their host. QS relies upon the production, accumulation and perception of small diffusable molecules by the bacterial population, hence linking high gene expression with high cell population densities. Among the different QS signal molecules, an important class of signal molecules is the N-acyl homoserine lactone (N-AHSL). In pathogens such as Erwinia or Pseudomonas, N-AHSL based QS is crucial to overcome the host defenses and ensure a successful infection...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/27900531/accidental-cannabis-poisoning-in-the-elderly
#11
Anja Zupan Mežnar, Miran Brvar, Gregor Kralj, Dragan Kovačič
There are two main varieties of Cannabis sativa plant, namely, hemp which is cultivated for fiber and seeds and contains low amounts of psychoactive cannabinoids and the other which is cultivated for the drug cannabis or marijuana. Increasing popularity of hemp food products and alleged beneficial effects of cannabinoids in the drug variety of cannabis might lead to confusion in the lay population and unintentional ingestion of marijuana, as described in this case report. During a workshop on the use of hemp for medicinal purposes, there was a degustation of various hemp food products including also cookies that were brought by one of the attendees...
November 29, 2016: Wiener Klinische Wochenschrift
https://www.readbyqxmd.com/read/27900439/non-ribosomal-peptide-synthases-from-pseudomonas-aeruginosa-play-a-role-in-cyclodipeptide-biosynthesis-quorum-sensing-regulation-and-root-development-in-a-plant-host
#12
Omar González, Randy Ortíz-Castro, César Díaz-Pérez, Alma L Díaz-Pérez, Viridiana Magaña-Dueñas, José López-Bucio, Jesús Campos-García
Diverse molecules mediate cross-kingdom communication between bacteria and their eukaryotic partners and determine pathogenic or symbiotic relationships. N-acyl-L-homoserine lactone-dependent quorum-sensing signaling represses the biosynthesis of bacterial cyclodipeptides (CDPs) that act as auxin signal mimics in the host plant Arabidopsis thaliana. In this work, we performed bioinformatics, biochemical, and plant growth analyses to identify non-ribosomal peptide synthase (NRPS) proteins of Pseudomonas aeruginosa, which are involved in CDP synthesis...
November 30, 2016: Microbial Ecology
https://www.readbyqxmd.com/read/27900261/targeting-the-endocannabinoid-cb1-receptor-system-for-treating-obesity-in-prader-willi-syndrome
#13
Ibrahim Knani, Brian J Earley, Shiran Udi, Alina Nemirovski, Rivka Hadar, Asaad Gammal, Resat Cinar, Harry J Hirsch, Yehuda Pollak, Itai Gross, Talia Eldar-Geva, Daniela P Reyes-Capo, Joan C Han, Andrea M Haqq, Varda Gross-Tsur, Rachel Wevrick, Joseph Tam
OBJECTIVE: Extreme obesity is a core phenotypic feature of Prader-Willi syndrome (PWS). Among numerous metabolic regulators, the endocannabinoid (eCB) system is critically involved in controlling feeding, body weight, and energy metabolism, and a globally acting cannabinoid-1 receptor (CB1R) blockade reverses obesity both in animals and humans. The first-in-class CB1R antagonist rimonabant proved effective in inducing weight loss in adults with PWS. However, it is no longer available for clinical use because of its centrally mediated, neuropsychiatric, adverse effects...
December 2016: Molecular Metabolism
https://www.readbyqxmd.com/read/27899885/interacting-cannabinoid-and-opioid-receptors-in-the-nucleus-accumbens-core-control-adolescent-social-play
#14
Antonia Manduca, Olivier Lassalle, Marja Sepers, Patrizia Campolongo, Vincenzo Cuomo, Giovanni Marsicano, Brigitte Kieffer, Louk J M J Vanderschuren, Viviana Trezza, Olivier J J Manzoni
Social play behavior is a highly rewarding, developmentally important form of social interaction in young mammals. However, its neurobiological underpinnings remain incompletely understood. Previous work has suggested that opioid and endocannabinoid neurotransmission interact in the modulation of social play. Therefore, we combined behavioral, pharmacological, electrophysiological, and genetic approaches to elucidate the role of the endocannabinoid 2-arachidonoylglycerol (2-AG) in social play, and how cannabinoid and opioid neurotransmission interact to control social behavior in adolescent rodents...
2016: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/27899748/cannabinoid-type-2-receptor-drives-neurogenesis-and-improves-functional-outcome-after-stroke
#15
Isabel Bravo-Ferrer, María I Cuartero, Juan G Zarruk, Jesús M Pradillo, Olivia Hurtado, Víctor G Romera, Javier Díaz-Alonso, Juan M García-Segura, Manuel Guzmán, Ignacio Lizasoain, Ismael Galve-Roperh, María A Moro
BACKGROUND AND PURPOSE: Stroke is a leading cause of adult disability characterized by physical, cognitive, and emotional disturbances. Unfortunately, pharmacological options are scarce. The cannabinoid type-2 receptor (CB2R) is neuroprotective in acute experimental stroke by anti-inflammatory mechanisms. However, its role in chronic stroke is still unknown. METHODS: Stroke was induced by permanent middle cerebral artery occlusion in mice; CB2R modulation was assessed by administering the CB2R agonist JWH133 ((6aR,10aR)-3-(1,1-dimethylbutyl)-6a,7,10,10a-tetrahydro-6,6,9-trimethyl-6H-dibenzo[b,d]pyran) or the CB2R antagonist SR144528 (N-[(1S)-endo-1,3,3-trimethylbicyclo-[2...
November 29, 2016: Stroke; a Journal of Cerebral Circulation
https://www.readbyqxmd.com/read/27899456/free-and-glucuronide-whole-blood-cannabinoids-pharmacokinetics-after-controlled-smoked-vaporized-and-oral-cannabis-administration-in-frequent-and-occasional-cannabis-users-identification-of-recent-cannabis-intake
#16
Matthew N Newmeyer, Madeleine J Swortwood, Allan J Barnes, Osama A Abulseoud, Karl B Scheidweiler, Marilyn A Huestis
BACKGROUND: There is increasing interest in markers of recent cannabis use because following frequent cannabis intake, Δ(9)-tetrahydrocannabinol (THC) may be detected in blood for up to 30 days. The minor cannabinoids cannabidiol, cannabinol (CBN), and THC-glucuronide were previously detected for ≤2.1 h in frequent and occasional smokers' blood after cannabis smoking. Cannabigerol (CBG), Δ(9)-tetrahydrocannabivarin (THCV), and 11-nor-9-carboxy-THCV might also be recent use markers, but their blood pharmacokinetics have not been investigated...
December 2016: Clinical Chemistry
https://www.readbyqxmd.com/read/27899449/deficiency-of-a-retinal-dystrophy-protein-acbd5-impairs-peroxisomal-%C3%AE-oxidation-of-very-long-chain-fatty-acids
#17
Yuichi Yagita, Kyoko Shinohara, Yuichi Abe, Keiko Nakagawa, Mohammed Al-Owain, Fowzan S Alkuraya, Yukio Fujiki
Acyl-CoA binding domain containing 5 (ACBD5) is a peroxisomal protein that carries an acyl-CoA binding domain (ACBD) at its N-terminal region. The recent identification of a mutation in the ACBD5 gene in patients with a syndromic form of retinal dystrophy highlights the physiological importance of ACBD5 in humans. However, the underlying pathogenic mechanisms and the precise function of ACBD5 remain unclear. We herein report that ACBD5 is a peroxisomal tail-anchored membrane protein exposing its ACBD to the cytosol...
November 29, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27899300/role-of-the-endocannabinoid-system-in-the-control-of-mouse-myometrium-contractility-during-the-menstrual-cycle
#18
Ester Pagano, Pierangelo Orlando, Stefania Finizio, Antonietta Rossi, Lorena Buono, Fabio Arturo Iannotti, Fabiana Piscitelli, Angelo A Izzo, Vincenzo Di Marzo, Francesca Borrelli
Cannabis and cannabinoids are known to affect female reproduction. However, the role of the endocannabinoid system in mouse uterine contractility in the dioestrus and oestrus phases has not been previously investigated. The present study aimed at filling this gap. Endocannabinoid (anandamide and 2-arachidonoylglycerol) levels were measured in mouse uterus at dioestrus and oestrus phases by liquid chromatography-mass spectrometry; quantitative reverse transcription-PCR measured mRNA expression of cannabinoid receptors and enzymes involved in the metabolism of endocannabinoids...
November 26, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/27898071/are-adolescents-more-vulnerable-to-the-harmful-effects-of-cannabis-than-adults-a-placebo-controlled-study-in-human-males
#19
C Mokrysz, T P Freeman, S Korkki, K Griffiths, H V Curran
Preclinical research demonstrates that cannabinoids have differing effects in adolescent and adult animals. Whether these findings translate to humans has not yet been investigated. Here we believe we conducted the first study to compare the acute effects of cannabis in human adolescent (n=20; 16-17 years old) and adult (n=20; 24-28 years old) male cannabis users, in a placebo-controlled, double-blind cross-over design. After inhaling vaporized active or placebo cannabis, participants completed tasks assessing spatial working memory, episodic memory and response inhibition, alongside measures of blood pressure and heart rate, psychotomimetic symptoms and subjective drug effects (for example, 'stoned', 'want to have cannabis')...
November 29, 2016: Translational Psychiatry
https://www.readbyqxmd.com/read/27897367/bifunctionality-of-activ-as-a-cyclase-thioesterase-revealed-by-in-vitro-reconstitution-of-actinorhodin-biosynthesis-in-streptomyces-coelicolor-a3-2
#20
Takaaki Taguchi, Takayoshi Awakawa, Yukitaka Nishihara, Michiho Kawamura, Yasuo Ohnishi, Koji Ichinose
Type II polyketide synthase (PKS) iteratively generates a nascent polyketide thioester of acyl carrier protein (ACP), which is structurally modified to produce an ACP-free intermediate towards its final metabolite. However, the timing of ACP off-loading is not well defined due to the lack of an apparent thioesterase (TE) among relevant biosynthetic enzymes. Here, ActIV, which had been assigned as a second ring cyclase (CYC) in actinorhodin (ACT) biosynthesis, was shown to possess a TE activity in vitro with a model substrate, anthraquinone-2-carboxylic acid-N-acetylcysteamine...
November 29, 2016: Chembiochem: a European Journal of Chemical Biology
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