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palmitoylethanolamide

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https://www.readbyqxmd.com/read/29054595/the-n-acylethanolamine-acid-amidase-inhibitor-arn077-suppresses-inflammation-and-pruritus-in-a-mouse-model-of-allergic-dermatitis
#1
O Sasso, M Summa, A Armirotti, S Pontis, C De Mei, D Piomelli
N-acylethanolamine acid amidase (NAAA), a cysteine hydrolase highly expressed in macrophages and B-lymphocytes, catalyzes the degradation of palmitoylethanolamide (PEA). PEA is an agonist of peroxisome proliferator-activated receptor-α (PPAR-α) and an important regulator of pain and innate immunity. In the present study, we investigated the properties of the NAAA inhibitor, ARN077, in a mouse model of allergic contact dermatitis. Acute topical applications of ARN077 attenuated key signs of DNFB-induced dermatitis in a dose-dependent manner...
October 17, 2017: Journal of Investigative Dermatology
https://www.readbyqxmd.com/read/29046777/effect-of-palmitoylethanolamide-on-inflammatory-and-neuropathic-pain-in-rats
#2
Tai-Kyung Seol, Wonho Lee, Sunah Park, Kyu Nam Kim, Tae Yeon Kim, You Na Oh, Jong Hun Jun
BACKGROUND: A growing body of evidence suggests that neuroinflammation, which is characterized by infiltration of immune cells, activation of mast cells and glial cells, and production of inflammatory mediators in the peripheral and central nervous systems, plays an important role in the induction and maintenance of chronic pain. Palmitoylethanolamide (PEA), which is a type of N-acylethanolamide and a lipid, has an anti-inflammatory effect. Relative to the anti-inflammatory effect, little is known about its analgesic effect in chronic pain...
October 2017: Korean Journal of Anesthesiology
https://www.readbyqxmd.com/read/29045169/use-of-topical-cannabinomimetic-palmitoylethanolamide-in-ocular-surface-disease-associated-with-antiglaucoma-medications
#3
Antonio Di Zazzo, Gloria Roberti, Alireza Mashaghi, Tulio Batista Abud, Daniela Pavese, Stefano Bonini
PURPOSE: Chronic use of topical hypotensive therapies in glaucoma patients leads to chronic inflammation of the ocular surface, which decreases the success rate of long-term glaucoma management. The aim of this study is to evaluate the effect of topical palmitoylethanolamide (PEA) (Defluxa(©)), a well-known anti-inflammatory and analgesic agent, in suppressing the ocular surface inflammation associated with the use of hypotensive eye drops. METHODS: In a pilot clinical trial, we enrolled 15 glaucomatous patients who received topical PEA (Defluxa) in addition to the current antiglaucoma drugs, while 15 glaucomatous patients did not receive any additional treatment...
November 2017: Journal of Ocular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29032410/relationship-between-circulating-fatty-acids-and-fatty-acid-ethanolamide-levels-after-a-single-2-h-dietary-fat-feeding-in-male-sprague-dawley-rats-elevated-levels-of-oleoylethanolamide-palmitoylethanolamide-linoleoylethanolamide-arachidonoylethanolamide-and
#4
Anthonia O Olatinsu, Jyoti Sihag, Peter J H Jones
Previous studies show that long term variations in dietary fat consumption impact circulating fatty acid ethanolamide (FAE) concentrations, however, few studies have investigated short term effects of dietary fat feeding on FAE levels. The trial's objective was to explore the effect of acute feeding of varying amounts of dietary n-9 and n-3 fatty acids on plasma and organ levels of FAE. Sixty-four rats were assigned to four groups fed meals containing 40% of energy as either safflower oil (control), canola oil (CO), or DHA rich oil (DRO), each consumed as a bolus within a 2-h window...
November 2017: Lipids
https://www.readbyqxmd.com/read/28954820/cannabidiol-and-palmitoylethanolamide-are-anti-inflammatory-in-the-acutely-inflamed-human-colon
#5
Daniel G Couch, Chris Tasker, Elena Theophilidou, Jonathan N Lund, Saoirse E O'Sullivan
OBJECTIVE: We sought to quantify the anti-inflammatory effects of two cannabinoid drugs, cannabidiol (CBD) and palmitoylethanolamide (PEA), in cultured cell lines and compared this effect with experimentally inflamed explant human colonic tissue. These effects were explored in acutely and chronically inflamed colon, using inflammatory bowel disease and appendicitis explants. DESIGN: Caco-2 cells and human colonic explants collected from elective bowel cancer, inflammatory bowel disease (IBD) or acute appendicitis resections, and were treated with the following drug treatments: vehicle, an inflammatory protocol of interferon γ (IFNγ) and tumour necrosis factor α (TNFα; 10 ng/ml), inflammation and PEA (10 µM), inflammation and CBD (10 µM), and PEA or CBD alone, CBD or vehicle were added simultaneously with IFNγ...
November 1, 2017: Clinical Science (1979-)
https://www.readbyqxmd.com/read/28939905/expression-and-differential-responsiveness-of-central-nervous-system-glial-cell-populations-to-the-acute-phase-protein-serum-amyloid-a
#6
Massimo Barbierato, Mila Borri, Laura Facci, Morena Zusso, Stephen D Skaper, Pietro Giusti
Acute-phase response is a systemic reaction to environmental/inflammatory insults and involves hepatic production of acute-phase proteins, including serum amyloid A (SAA). Extrahepatically, SAA immunoreactivity is found in axonal myelin sheaths of cortex in Alzheimer's disease and multiple sclerosis (MS), although its cellular origin is unclear. We examined the responses of cultured rat cortical astrocytes, microglia and oligodendrocyte precursor cells (OPCs) to master pro-inflammatory cytokine tumour necrosis factor (TNF)-α and lipopolysaccaride (LPS)...
September 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28931663/targeting-fatty-acid-amide-hydrolase-as-a-therapeutic-strategy-for-antitussive-therapy
#7
Michael A Wortley, John J Adcock, Eric D Dubuis, Sarah A Maher, Sara J Bonvini, Isabelle Delescluse, Ross Kinloch, Gordon McMurray, Christelle Perros-Huguet, Marianthi Papakosta, Mark A Birrell, Maria G Belvisi
Cough is the most common reason to visit a primary care physician, yet it remains an unmet medical need. Fatty acid amide hydrolase (FAAH) is an enzyme that breaks down endocannabinoids, and inhibition of FAAH produces analgesic and anti-inflammatory effects. Cannabinoids inhibit vagal sensory nerve activation and the cough reflex, so it was hypothesised that FAAH inhibition would produce antitussive activity via elevation of endocannabinoids.Primary vagal ganglia neurons, tissue bioassay, in vivo electrophysiology and a conscious guinea pig cough model were utilised to investigate a role for fatty acid amides in modulating sensory nerve activation in vagal afferents...
September 2017: European Respiratory Journal: Official Journal of the European Society for Clinical Respiratory Physiology
https://www.readbyqxmd.com/read/28875041/palmitoylethanolamide-in-the-treatment-of-failed-back-surgery-syndrome
#8
Antonella Paladini, Giustino Varrassi, Giuseppe Bentivegna, Sandro Carletti, Alba Piroli, Stefano Coaccioli
INTRODUCTION: This observational study was designed to evaluate the efficacy of ultramicronized palmitoylethanolamide (um-PEA) (Normast®) administration, as add-on therapy for chronic pain, in the management of pain-resistant patients affected by failed back surgery syndrome. METHODS: A total of 35 patients were treated with tapentadol (TPD) and pregabalin (PGB). One month after the start of standard treatment, um-PEA was added for the next two months. Pain was evaluated by the Visual Analogue Scale (VAS) at the time of enrollment (T0) and after one (T1), two (T2), and three (T3) months...
2017: Pain Research and Treatment
https://www.readbyqxmd.com/read/28861512/identification-of-a-widespread-palmitoylethanolamide-contamination-in-standard-laboratory-glassware
#9
Roberto Angelini, Donovan A Argueta, Daniele Piomelli, Nicholas V DiPatrizio
Introduction: Fatty acid ethanolamides (FAEs) are a family of lipid mediators that participate in a host of biological functions. Procedures for the quantitative analysis of FAEs include organic solvent extraction from biological matrices (e.g., blood), followed by purification and subsequent quantitation by liquid chromatography-mass spectrometry (LC/MS) or gas chromatography-mass spectrometry. During the validation process of a new method for LC/MS analysis of FAEs in biological samples, we observed unusually high levels of the FAE, palmitoylethanolamide (PEA), in blank samples that did not contain any biological material...
2017: Cannabis and Cannabinoid Research
https://www.readbyqxmd.com/read/28861501/palmitoylethanolamide-modulates-gpr55-receptor-signaling-in-the-ventral-hippocampus-to-regulate-mesolimbic-dopamine-activity-social-interaction-and-memory-processing
#10
Cecilia Kramar, Michael Loureiro, Justine Renard, Steven R Laviolette
Introduction: The GPR55 receptor has been identified as an atypical cannabinoid receptor and is implicated in various physiological processes. However, its functional role in the central nervous system is not currently understood. The presence of GPR55 receptor in neural regions such as the ventral hippocampus (vHipp), which is critical for cognition, recognition memory, and affective processing, led us to hypothesize that intra-vHipp GPR55 transmission may modulate mesolimbic activity states and related behavioral phenomena...
2017: Cannabis and Cannabinoid Research
https://www.readbyqxmd.com/read/28843504/mammalian-enzymes-responsible-for-the-biosynthesis-of-n-acylethanolamines
#11
REVIEW
Zahir Hussain, Toru Uyama, Kazuhito Tsuboi, Natsuo Ueda
Bioactive N-acylethanolamines (NAEs) are ethanolamides of long-chain fatty acids, including palmitoylethanolamide, oleoylethanolamide and anandamide. In animal tissues, NAEs are biosynthesized from membrane phospholipids. The classical "transacylation-phosphodiesterase" pathway proceeds via N-acyl-phosphatidylethanolamine (NAPE), which involves the actions of two enzymes, NAPE-generating Ca(2+)-dependent N-acyltransferase (Ca-NAT) and NAPE-hydrolyzing phospholipase D (NAPE-PLD). Recent identification of Ca-NAT as Ɛ isoform of cytosolic phospholipase A2 enabled the further molecular biological approaches toward this enzyme...
December 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28826538/the-role-of-nuclear-hormone-receptors-in-cannabinoid-function
#12
Marco Pistis, Saoirse E O'Sullivan
Since the early 2000s, evidence has been accumulating that most cannabinoid compounds interact with the nuclear hormone family peroxisome proliferator-activated receptors (PPARs). This can be through direct binding of these compounds to PPARs, metabolism of cannabinoid to other PPAR-activating chemicals, or indirect activation of PPAR through cell signaling pathways. Delivery of cannabinoids to the nucleus may be facilitated by fatty acid-binding proteins and carrier proteins. All PPAR isoforms appear to be activated by cannabinoids, but the majority of evidence is for PPARα and γ...
2017: Advances in Pharmacology
https://www.readbyqxmd.com/read/28822061/co-ultramicronized-palmitoylethanolamide-luteolin-facilitates-the-development-of-differentiating-and-undifferentiated-rat-oligodendrocyte-progenitor-cells
#13
Stephen D Skaper, Massimo Barbierato, Laura Facci, Mila Borri, Gabriella Contarini, Morena Zusso, Pietro Giusti
Oligodendrocytes, the myelin-producing cells of the central nervous system (CNS), have limited capability to bring about repair in chronic CNS neuroinflammatory demyelinating disorders such as multiple sclerosis (MS). MS lesions are characterized by a compromised pool of undifferentiated oligodendrocyte progenitor cells (OPCs) unable to mature into myelin-producing oligodendrocytes. An attractive strategy may be to replace lost OLs and/or promote their maturation. N-palmitoylethanolamine (PEA) is an endogenous fatty acid amide signaling molecule with anti-inflammatory and neuroprotective actions...
August 18, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28805944/suppression-of-acute-and-anticipatory-nausea-by-peripherally-restricted-fatty-acid-amide-hydrolase-inhibitor-in-animal-models-role-of-ppar%C3%AE-and-cb1-receptors
#14
Erin M Rock, Guillermo Moreno-Sanz, Cheryl L Limebeer, Gavin N Petrie, Roberto Angelini, Daniele Piomelli, Linda A Parker
BACKGROUND AND PURPOSE: Effective treatments of nausea are limited. In this study we evaluated the ability of the peripherally restricted fatty acid amide hydrolase (FAAH) inhibitor, URB937, to suppress acute and anticipatory nausea in rats and examined the pharmacological mechanism of this effect. EXPERIMENTAL APPROACH: We investigated the potential of URB937 (administered i.p.) to reduce the establishment of lithium chloride-induced conditioned gaping (model of acute nausea) and to reduce the expression of contextually-elicited conditioned gaping (model of anticipatory nausea) in rats...
November 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28802121/identification-of-highly-potent-n-acylethanolamine-acid-amidase-naaa-inhibitors-optimization-of-the-terminal-phenyl-moiety-of-oxazolidone-derivatives
#15
Yuhang Li, Qi Chen, Longhe Yang, Yanting Li, Yang Zhang, Yan Qiu, Jie Ren, Canzhong Lu
N-acylethanolamine acid amidase (NAAA) is a cysteine hydrolase that participates in the deactivation of fatty acid ethanolamides, such as palmitoylethanolamide (PEA). NAAA inhibition may provide a potential therapeutic strategy for the treatment of diseases in which higher PEA level is desired. In the present study, we reported the structure-activity relationship (SAR) studies for oxazolidone derivatives as NAAA inhibitors. A series of substituents or alkyl replacements for the terminal phenyl ring of oxazolidone derivatives were examined...
October 20, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28768536/a-novel-composite-formulation-of-palmitoylethanolamide-and-quercetin-decreases-inflammation-and-relieves-pain-in-inflammatory-and-osteoarthritic-pain-models
#16
Domenico Britti, Rosalia Crupi, Daniela Impellizzeri, Enrico Gugliandolo, Roberta Fusco, Carlo Schievano, Valeria Maria Morittu, Maurizio Evangelista, Rosanna Di Paola, Salvatore Cuzzocrea
BACKGROUND: Osteoarthritis (OA) is a common progressive joint disease in dogs and cats. The goal of OA treatment is to reduce inflammation, minimize pain, and maintain joint function. Currently, non-steroidal anti-inflammatory drugs (e.g., meloxicam) are the cornerstone of treatment for OA pain, but side effects with long-term use pose important challenges to veterinary practitioners when dealing with OA pain. Palmitoylethanolamide (PEA) is a naturally-occurring fatty acid amide, locally produced on demand by tissues in response to stress...
August 2, 2017: BMC Veterinary Research
https://www.readbyqxmd.com/read/28727699/efficacy-of-palmitoylethanolamide-for-pain-a-meta-analysis
#17
Bekir Berker Artukoglu, Chad Beyer, Adi Zuloff-Shani, Ephraim Brener, Michael Howard Bloch
BACKGROUND: Palmitoylethanolamide (PEA) is a cannabimimetic compound that has been investigated as an analgesic agent in animal models and clinical trials. OBJECTIVES: We conducted a meta-analysis to examine the efficacy of PEA for treating pain in randomized, controlled trials. STUDY DESIGN: Systematic review and meta-analysis. SETTING: This meta-analysis examined all randomized, controlled trials involving the effect of PEA on pain score...
July 2017: Pain Physician
https://www.readbyqxmd.com/read/28676456/palmitoylethanolamide-and-polydatin-combination-reduces-inflammation-and-oxidative-stress-in-vascular-injury
#18
Enrico Gugliandolo, Roberta Fusco, Flavia Biundo, Ramona D'Amico, Filippo Benedetto, Rosanna Di Paola, Salvatore Cuzzocrea
Acute and chronic inflammation responses are important risk factors for vascular remodeling processes such as in atherosclerosis, arteriosclerosis and restenosis. Inflammation and oxidative stress in the intimal region after vascular damage are a key event in the development of neointimal hyperplasia. In this study, we used this model of vascular damage, which involves the complete ligature of the left carotid artery for 14days, to observe the role of N-palmitoylethanolamine in combination with Polydatin at the dose of 30mg/kg, on regulation of inflammatory process, and oxidative stress...
July 1, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28665150/association-between-plasma-n-acylethanolamides-and-high-hemoglobin-concentration-in-southern-peruvian-highlanders
#19
Dulce E Alarcón-Yaquetto, Lidia Caballero, Gustavo F Gonzales
Alarcón-Yaquetto, Dulce E., Lidia Caballero, and Gustavo F. Gonzales. Association between plasma N-acylethanolamides and high hemoglobin concentration in Southern Peruvian highlanders. High Alt Med Biol 00:000-000, 2017.-High-altitude (HA) hypoxia is a stressful condition endured by organisms through different mechanisms. Failing to adapt to chronic HA exposure leads to a disease called chronic mountain sickness (CMS) characterized by excessive erythrocytosis (hemoglobin [Hb] ≥19 g/dL for women and ≥21 g/dL for men)...
June 30, 2017: High Altitude Medicine & Biology
https://www.readbyqxmd.com/read/28659728/hedonic-eating-in-prader-willi-syndrome-is-associated-with-blunted-pyy-secretion
#20
A E Rigamonti, S Bini, F Piscitelli, A Lauritano, V Di Marzo, C Vanetti, F Agosti, A De Col, E Lucchetti, G Grugni, A Sartorio
Hedonic and homeostatic hunger represent two different forms of eating: just for pleasure or following energy deprivation, respectively. Consumption of food for pleasure was reported to be associated with increased circulating levels of both the orexigenic peptide ghrelin and some specific endocannabinoids in normal-weight subjects and patients with morbid obesity. To date, the effects of palatable food on these mediators in Prader-Willi syndrome (PWS) are still unknown. To explore the role of some gastrointestinal orexigenic and anorexigenic peptides and endocannabinoids (and some related congeners) in chocolate consumption, we measured changes in circulating levels of ghrelin, cholecystokinin (CCK), peptide YY (PYY), anandamide (AEA), 2-arachidonoyl-glycerol (2-AG), palmitoylethanolamide (PEA) and oleoylethanolamide (OEA) in eight satiated adult PWS patients after consumption of chocolate and, on a separate day, of a non-palatable isocaloric food with the same macronutrient composition...
2017: Food & Nutrition Research
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