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J M Keppel Hesselink, D J Kopsky, N Sajben
Topical treatments of localized neuropathic pain syndromes in general are mostly neglected, mainly due to the fact that most pain physicians expect that a topical formulation needs to result in a transdermal delivery of the active compounds. On the basis of the practical experience, this study brings forth a new, somewhat neglected element of the vulvodynia pathogenesis: the cross talk between the nerve endings of nociceptors, the adjacent immunocompetent cells, and vaginal epithelial cells. Insight into this cross talk during a pathogenic condition supports the treatment of vulvodynia with topical (compounded) creams...
2016: Journal of Pain Research
Oscar Prospéro-García, Octavio Amancio-Belmont, Alline L Becerril Meléndez, Alejandra E Ruiz-Contreras, Mónica Méndez-Díaz
Sleep is regulated by several brain structures, neurotransmitters and neuromodulators. Endocannabinoids (eCBs) are a group of lipids with modulatory activity in the brain and bind mainly to cannabinoid receptors CB1R and CB2R, thereby modulating several brain functions, (memory, mood, food intake, pain perception). Oleoylethanolamide and palmitoylethanolamide belong to the N-acylethanolamides (NAEs) family, another type of active endogenous lipids. They bind to the peroxisome proliferator-activated receptor α but not to CB1R, thereby modulating food satiety, inflammation and pain...
October 15, 2016: Neuroscience and Biobehavioral Reviews
Jan M Keppel Hesselink, Flavia Chiosi, Ciro Costagliola
Resolvins are a novel class of lipid-derived endogenous molecules (autacoids) with potent immunomodulating properties, which regulate the resolution phase of an active immune response. These modulating factors are locally produced, influencing the function of cells and/or tissues, which are produced on demand and subsequently metabolized in the same cells and/or tissues. This review is focused on certain lipid autacoids with putative relevance for ophthalmology in general and for dry eye more specifically. We also briefly investigate the concept of aliamides and the role of palmitoylethanolamide in ophthalmology, and analyze in more detail the putative role and the preclinical and clinical development of resolvins as emerging treatments for dry eye and related disorders, with a focus on one of the lead resolvin derivatives - RX-10045...
2016: Drug Design, Development and Therapy
Massimo Vaia, Stefania Petrosino, Daniele De Filippis, Luana Negro, Andrea Guarino, Rosa Carnuccio, Vincenzo Di Marzo, Teresa Iuvone
In mice, 2,4-dinitrofluorobenzene (DNFB) induces contact allergic dermatitis (CAD), which, in a late phase, is characterized by mast cell (MC) infiltration and angiogenesis. Palmitoylethanolamide (PEA), an endogenous anti-inflammatory molecule, acts by down-modulating MCs following activation of the cannabinoid CB2 receptor and peroxisome proliferator-activated receptor-α (PPAR-α). We have previously reported the anti-inflammatory effect of PEA in the early stage of CAD. Here, we examined whether PEA reduces the features of the late stage of CAD including MC activation, angiogenesis and itching...
October 5, 2016: European Journal of Pharmacology
Bartolomeo Bertolino, Rosalia Crupi, Daniela Impellizzeri, Giuseppe Bruschetta, Marika Cordaro, Rosalba Siracusa, Emanuela Esposito, Salvatore Cuzzocrea
AIMS: Autism spectrum disorder (ASD) is a condition defined by social communication deficits and repetitive restrictive behaviors. Association of the fatty acid amide palmitoylethanolamide (PEA) with the flavonoid luteolin displays neuroprotective and antiinflammatory actions in different models of central nervous system pathologies. We hypothesized that association of PEA with luteolin might have therapeutic utility in ASD, and we employed a well-recognized autism animal model, namely sodium valproate administration, to evaluate cognitive and motor deficits...
October 4, 2016: CNS Neuroscience & Therapeutics
Yuma Sakura, Kazuhito Tsuboi, Toru Uyama, Xia Zhang, Rikiya Taoka, Mikio Sugimoto, Yoshiyuki Kakehi, Natsuo Ueda
N-Acylethanolamine acid amidase (NAAA) is a lysosomal enzyme, hydrolyzing various bioactive N-acylethanolamines with a preference for palmitoylethanolamide. Human NAAA mRNA was previously reported to consist of multiple 3'-end splice variants. However, their tissue distributions and roles have not been examined yet. In the present study, we first identified four major splice variants (tentatively referred to as a1, a2, b2, and c2) in a human prostate cancer cell line LNCaP, which were composed of exons 1-11, exons 1-10 and 12, exons 1-9 and 12, and exons 1-8 and 12, respectively...
October 5, 2016: Biochimica et Biophysica Acta
Bright N Okine, Manish K Madasu, Fiona McGowan, Charles Prendergast, Jessica C Gaspar, Brendan Harhen, Michelle Roche, David P Finn
The neural substrates and mechanisms mediating the antinociceptive effects of the endogenous bioactive lipid, N-palmitoylethanolamide (PEA), require further investigation. We investigated the effects of exogenous PEA administration into the anterior cingulate cortex (ACC), an important brain region linked with cognitive and affective modulation of pain, on formalin-evoked nociceptive behaviour in rats. Potential involvement of peroxisome proliferator-activated receptor isoforms (PPAR) α and γ or endocannabinoid-mediated entourage effects at cannabinoid1 (CB1) receptors or transient receptor potential subfamily V member 1 (TRPV1) in mediating the effects of PEA was also investigated...
August 16, 2016: Pain
Iffat Ara Sonia Rahman, Kazuhito Tsuboi, Zahir Hussain, Ryouhei Yamashita, Yoko Okamoto, Toru Uyama, Naoshi Yamazaki, Tamotsu Tanaka, Akira Tokumura, Natsuo Ueda
N-Acylethanolamines form a class of lipid mediators and include an endocannabinoid arachidonoylethanolamide (anandamide), analgesic and anti-inflammatory palmitoylethanolamide, and appetite-suppressing oleoylethanolamide. In animal tissues, N-acylethanolamines are synthesized from N-acylated ethanolamine phospholipids directly by N-acylphosphatidylethanolamine-hydrolyzing phospholipase D or through multi-step pathways via N-acylethanolamine lysophospholipids. We previously reported that glycerophosphodiesterase (GDE) 4, a member of the GDE family, has lysophospholipase D (lysoPLD) activity hydrolyzing N-acylethanolamine lysophospholipids to N-acylethanolamines...
September 13, 2016: Biochimica et Biophysica Acta
Marika Cordaro, Daniela Impellizzeri, Enrico Gugliandolo, Rosalba Siracusa, Rosalia Crupi, Emanuela Esposito, Salvatore Cuzzocrea
Leukocyte infiltration, improved levels of intercellular adhesion molecule 1 (ICAM-1), and oxidative stress in the colon are the principal factors in inflammatory bowel disease. The goal of the current study was to explore the effects of adelmidrol, an analog of the anti-inflammatory fatty acid amide signaling molecule palmitoylethanolamide, in mice subjected to experimental colitis. Additionally, to clarify whether the protective action of adelmidrol is dependent on the activation of peroxisome proliferator-activated receptors (PPARs), we investigated the effects of a PPARγ antagonist, GW9662, on adelmidrol action...
November 2016: Molecular Pharmacology
Carmen Avagliano, Roberto Russo, Carmen De Caro, Claudia Cristiano, Giovanna La Rana, Giuseppe Piegari, Orlando Paciello, Rita Citraro, Emilio Russo, Giovambattista De Sarro, Rosaria Meli, Giuseppina Mattace Raso, Antonio Calignano
Several pathogenetic factors have been involved in the onset and progression of Parkinson's disease (PD), including inflammation, oxidative stress, unfolded protein accumulation, and apoptosis. Palmitoylethanolamide (PEA), an endogenous N-acylethanolamine, has been shown to be a neuroprotective and anti-inflammatory molecule, acting as a peroxisome proliferator activated receptor (PPAR)-α agonist. In this study we investigated the effects of PEA on behavioral alterations and the underlying pathogenic mechanisms in the 6-hydroxydopamine (6-OHDA)-induced model of PD in male mice...
September 8, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Giulia Donvito, Jenny L Wilkerson, M Imad Damaj, Aron H Lichtman
Chemotherapy-induced peripheral neuropathy (CIPN) represents a serious complication associated with anticancer drugs. Although there are no medications available that effectively prevent CIPN, many classes of drugs have been used to treat this condition, including anticonvulsants, serotonin and noradrenaline reuptake inhibitors, and opioids. However, these theraputic options yielded inconclusive results in CIPN clincal trials and produce assorted side effects with their prolonged use. Thus, there is an urgent need to develop efficacious and safe treatments for CIPN...
September 8, 2016: Journal of Pharmacology and Experimental Therapeutics
Daniela Impellizzeri, Rosanna Di Paola, Marika Cordaro, Enrico Gugliandolo, Giovanna Casili, Valeria Maria Morittu, Domenico Britti, Emanuela Esposito, Salvatore Cuzzocrea
The aim of study was to examine the anti-inflammatory and analgesic effects of adelmidrol, an analogue of palmitoylethanolamide (PEA), in animal models of acute and chronic inflammation [carrageenan-induced paw edema (CAR) and collagen-induced arthritis (CIA)]. In order to elucidate whether the action of adelmidrol is related to activation of peroxisome proliferator-activated receptors (PPAR-α or PPAR-γ), we investigated the effects of PPAR-γ antagonist, GW9662 on adelmidrol mechanism. CAR induced paw edema, hyperalgesia and the activation of pro-inflammatory NF-κB pathway were markedly reduced by treatment with adelmidrol...
November 1, 2016: Biochemical Pharmacology
Eleonora Margheritis, Beatrice Castellani, Paola Magotti, Sara Peruzzi, Elisa Romeo, Francesca Natali, Serena Mostarda, Antimo Gioiello, Daniele Piomelli, Gianpiero Garau
The membrane-associated enzyme NAPE-PLD (N-acyl phosphatidylethanolamine specific-phospholipase D) generates the endogenous cannabinoid arachidonylethanolamide and other lipid signaling amides, including oleoylethanolamide and palmitoylethanolamide. These bioactive molecules play important roles in several physiological pathways including stress and pain response, appetite and lifespan. Recently, we reported the crystal structure of human NAPE-PLD and discovered specific binding sites for the bile acid deoxycholic acid...
August 29, 2016: ACS Chemical Biology
Owein Guillemot-Legris, Julien Masquelier, Amandine Everard, Patrice D Cani, Mireille Alhouayek, Giulio G Muccioli
BACKGROUND: Obesity and its associated disorders are becoming a major health issue in many countries. The resulting low-grade inflammation not only affects the periphery but also the central nervous system. We set out to study, in a time-dependent manner, the effects of a high-fat diet on different regions of the central nervous system with regard to the inflammatory tone. METHODS: We used a diet-induced obesity model and compared at several time-points (1, 2, 4, 6, 8, and 16 weeks) a group of mice fed a high-fat diet with its respective control group fed a standard diet...
2016: Journal of Neuroinflammation
D Petrini, M Di Giuseppe, G Deli, C De Caro Carella
A 14-month-old intact male Syrian hamster was admitted for lethargy and hematuria. A total body radiographic image and abdominal ultrasonography showed the presence of a vesical calculus. During cystotomy, a sterile urine sample was obtained and sent to the diagnostic laboratory along with the urolith for analysis. Urine culture was found negative for bacterial growth, and the urolith was identified as a calcium-oxalate stone. Diet supplementation with palmitoylethanolamide, glucosamine and hesperidin was adopted the day after discharge...
2016: Open veterinary journal
Stefania Petrosino, Vincenzo Di Marzo
Palmitoylethanolamide (PEA) has emerged as a potential nutraceutical, since this compound is naturally produced in many plant and animal food sources, as well as in cells and tissues of mammals, and it is endowed with important neuroprotective, anti-inflammatory and analgesic actions. Several efforts have been made to identify the molecular mechanism of action of PEA, and explain its multiple effects both in the central and the peripheral nervous system. Here, we provide an overview of the pharmacology, efficacy and safety of PEA in neurodegenerative disorders, pain perception and inflammatory diseases...
August 19, 2016: British Journal of Pharmacology
Niclas Stensson, Bijar Ghafouri, Nazdar Ghafouri, Björn Gerdle
Although chronic widespread musculoskeletal pain is a significant health problem, the molecular mechanisms involved in developing and maintaining chronic widespread musculoskeletal pain are poorly understood. Central sensitization mechanisms maintained by stimuli from peripheral tissues such as muscle have been suggested. Lipid mediators with anti-inflammatory characteristics such as endogenous ligands of peroxisome proliferator activating receptor-α, oleoylethanolamide, and palmitoylethanolamide are suggested to regulate nociceptive transmission from peripheral locations on route towards the central nervous system...
2016: Molecular Pain
Domenico Chirchiglia, Attilio Della Torre, Francesco Signorelli, Giorgio Volpentesta, Giusy Guzzi, Carmelino Angelo Stroscio, Federica Deodato, Donatella Gabriele, Angelo Lavano
Nummular headache has been recently described as a primary disorder characterized by head pain exclusively felt in a small rounded area typically 2-6 cm in diameter, not attributed to another disorder. Both size and shape of the painful area remain constant since the onset of symptoms. A 57-year-old woman presented with a history of focal episodic pain in a circumscribed area on the right parietal region. The administration of standard oral doses of palmitoylethanolamide and topiramate in combination showed an improvement in pain symptoms and on pain measuring scales...
2016: International Medical Case Reports Journal
Maura Marcucci, Federico Germini, Anna Coerezza, Luca Andreinetti, Lorenzo Bellintani, Alessandro Nobili, Paolo Dionigi Rossi, Daniela Mari
BACKGROUND: Chronic pain in older people is highly prevalent, often underestimated, and associated with adverse outcomes. Most available analgesic drugs are often either ineffective or not tolerated, with many side effects. Palmitoylethanolamide (PEA) is an endogenous widely distributed N-acylethanolamina involved in neuroinflammation and pain-generating processes. Formulations containing ultra-micronized palmitoylethanolamide (um-PEA) are available but their effectiveness on chronic pain in highly heterogeneous geriatric patients is not clear and probably not generalizable...
2016: Trials
Edoardo Parrella, Vanessa Porrini, Rosa Iorio, Marina Benarese, Annamaria Lanzillotta, Mariana Mota, Mariella Fusco, Paolo Tonin, PierFranco Spano, Marina Pizzi
The combination of palmitoylethanolamide (PEA), an endogenous fatty acid amide belonging to the family of the N-acylethanolamines, and the flavonoid luteolin has been found to exert neuroprotective activities in a variety of mouse models of neurological disorders, including brain ischemia. Indirect findings suggest that the two molecules can reduce the activation of mastocytes in brain ischemia, thus modulating crucial cells that trigger the inflammatory cascade. Though, no evidence exists about a direct effect of PEA and luteolin on mast cells in experimental models of brain ischemia, either used separately or in combination...
October 1, 2016: Brain Research
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