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https://www.readbyqxmd.com/read/29772784/capsaicin-in-metabolic-syndrome
#1
REVIEW
Sunil K Panchal, Edward Bliss, Lindsay Brown
Capsaicin, the major active constituent of chilli, is an agonist on transient receptor potential vanilloid channel 1 (TRPV1). TRPV1 is present on many metabolically active tissues, making it a potentially relevant target for metabolic interventions. Insulin resistance and obesity, being the major components of metabolic syndrome, increase the risk for the development of cardiovascular disease, type 2 diabetes, and non-alcoholic fatty liver disease. In vitro and pre-clinical studies have established the effectiveness of low-dose dietary capsaicin in attenuating metabolic disorders...
May 17, 2018: Nutrients
https://www.readbyqxmd.com/read/29765535/effects-of-cb2-and-trpv1-receptors-stimulation-in-pediatric-acute-t-lymphoblastic-leukemia
#2
Francesca Punzo, Iolanda Manzo, Chiara Tortora, Elvira Pota, Velia D' Angelo, Giulia Bellini, Alessandra Di Paola, Federica Verace, Fiorina Casale, Francesca Rossi
T-Acute Lymphoblastic Leukemia (T-ALL) is less frequent than B-ALL, but it has poorer outcome. For this reason new therapeutic approaches are needed to treat this malignancy. The Endocannabinoid/Endovanilloid (EC/EV) system has been proposed as possible target to treat several malignancies, including lymphoblastic diseases. The EC/EV system is composed of two G-Protein Coupled Receptors (CB1 and CB2), the Transient Potential Vanilloid 1 (TRPV1) channel, their endogenous and exogenous ligands and enzymes. CB1 is expressed mainly in central nervous system while CB2 predominantly on immune and peripheral cells, therefore we chose to selectively stimulate CB2 and TRPV1...
April 20, 2018: Oncotarget
https://www.readbyqxmd.com/read/29740093/differential-contributions-of-peripheral-and-central-mechanisms-to-pain-in-a-rodent-model-of-osteoarthritis
#3
Adrian R Haywood, Gareth J Hathway, Victoria Chapman
The mechanisms underlying the transition from acute nociceptive pain to centrally maintained chronic pain are not clear. We have studied the contributions of the peripheral and central nervous systems during the development of osteoarthritis (OA) pain. Male Sprague-Dawley rats received unilateral intra-articular injections of monosodium iodoacetate (MIA 1 mg) or saline, and weight-bearing (WB) asymmetry and distal allodynia measured. Subgroups of rats received intra-articular injections of, QX-314 (membrane impermeable local anaesthetic) + capsaicin, QX-314, capsaicin or vehicle on days 7, 14 or 28 post-MIA and WB and PWT remeasured...
May 8, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29730242/potentiation-of-capsaicin-induced-neurogenic-inflammation-by-5-ht7-receptors-in-the-rat-hind-paw-involvement-of-calcitonin-gen-related-peptide
#4
Luis D Arreola-Peralta, Frida Altamirano-Reyna, Deni M Galindo-González, Jessica G Solis-Anguiano, Enza Lacivita, Marcello Leopoldo, José A Terrón
A decrease in the activation threshold of primary sensory neurons to transient receptor potential V1 (TRPV1) stimulation by serotonin 5-HT7 receptors has been reported but no confirmation if this might translate into facilitation of neurogenic inflammation has been provided. We analysed the modulation of capsaicin (CAP)-induced neurogenic inflammation in the rat hind paw by the selective 5-HT7 receptor agonist, LP-44, and the involvement of calcitonin gen-related peptide (CGRP) in this effect. Animals received intra-plantar injections (30 μl) of vehicle, CAP (0...
May 3, 2018: Peptides
https://www.readbyqxmd.com/read/29722529/targeting-transient-receptor-potential-vanilloid-1-trpv1-channel-softly-the-discovery-of-passerini-adducts-as-a-topical-treatment-for-inflammatory-skin-disorders
#5
Marta Serafini, Alessia Griglio, Silvio Aprile, Fabio Seiti, Cristina Travelli, Franco Pattarino, Giorgio Grosa, Giovanni Sorba, Armando A Genazzani, Sara Gonzales-Rodriguez, Laura Butron, Isabel Devesa, Asia Fernández-Carvajal, Tracey Pirali, Antonio Ferrer-Montiel
Despite being an old molecule, capsaicin is still a hot topic in scientific community and the development of new capsaicinoids is a promising pharmacological approach in the management of skin disorders related to inflammation and pruritus. Here we report the synthesis and the evaluation of capsaicin soft drugs that undergo deactivation by the hydrolyzing activity of skin esterases. The implanting of an ester group in the lipophilic moiety of capsaicinoids by the Passerini multicomponent reaction affords both agonists and antagonists that retain transient receptor potential vanilloid 1 channel (TRPV1) modulating activity and, at the same time, are susceptible to hydrolysis...
May 3, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29715454/-effect-of-polygodial-and-its-direct-derivatives-on-the-mammalian-na-k-atpase-activity
#6
Diogo Gomes Garcia, Cassiano Felippe Gonçalves-de-Albuquerque, Camila Ignácio da Silva, Robert Kiss, Ramesh Dasari, Sunena Chandra, Alexander Kornienko, Patricia Burth
The sesquiterpene polygodial is an agonist of the transient receptor potential vanilloid 1 (TRPV1). Our group recently reported the synthesis and anticancer effects of polygodial and its derivatives, and showed that these compounds retain activity against apoptosis- and multidrug-resistant cancer cells. Herein, we tested the inhibitory effect of these compounds on the activity of the enzyme Na+ /K+ -ATPase (NKA) from kidney (α1 isoform) and brain (α2 and α3 isoforms) guinea pig extracts. Polygodial (1) displayed a dose-dependent inhibition of both kidney and brain purified NKA preparations, with higher sensitivity for the cerebral isoforms...
April 28, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29697532/chemokine-c-c-motif-receptor-2-mediates-mechanical-and-cold-hypersensitivity-in-sickle-cell-disease-mice
#7
Katelyn E Sadler, Katherine J Zappia, Crystal L O'Hara, Sarah N Langer, Andy D Weyer, Cheryl A Hillery, Cheryl L Stucky
Approximately one third of individuals with sickle cell disease (SCD) develop chronic pain. This debilitating pain is inadequately treated because the underlying mechanisms driving the pain are poorly understood. In addition to persistent pain, SCD patients are also in a tonically pro-inflammatory state. Previous studies have revealed that there are elevated plasma levels of many inflammatory mediators including chemokine (c-c motif) ligand 2 (CCL2) in individuals with SCD. Using a transgenic mouse model of SCD, we investigated the contributions of CCL2 signaling to SCD-related pain...
April 23, 2018: Pain
https://www.readbyqxmd.com/read/29679953/antinociception-by-the-anti-oxidized-phospholipid-antibody-e06
#8
Milad Mohammadi, Beatrice Oehler, Jan Kloka, Corinna Martin, Alexander Brack, Robert Blum, Heike L Rittner
BACKGROUND AND PURPOSE: Reactive oxygen species (ROS) and their downstream molecules such as oxidized phospholipids (OxPL) and 4-hydroxynonenal (4-HNE) activate transient receptor potential ankyrin 1 (TRPA1) and vanilloid 1 (TRPV1) ion channels in vivo and in vitro shaping thermal and mechanical hypersensitivity in inflammatory pain. E06/T15 is a monoclonal autoantibody against oxidized phosphatidylcholine (OxPC) used in diagnostics in arteriosclerosis. Recently, we provided evidence that E06 also ameliorates inflammatory pain...
April 21, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29662945/metabotropic-glutamate-receptor-2-3-mglur2-3-activation-suppresses-trpv1-sensitization-in-mouse-but-not-human-sensory-neurons
#9
Tayler D Sheahan, Manouela V Valtcheva, Lisa A McIlvried, Melanie Y Pullen, David A A Baranger, Robert W Gereau
The use of human tissue to validate putative analgesic targets identified in rodents is a promising strategy for improving the historically poor translational record of preclinical pain research. We recently demonstrated that in mouse and human sensory neurons, agonists for metabotropic glutamate receptors 2 and 3 (mGluR2/3) reduce membrane hyperexcitability produced by the inflammatory mediator prostaglandin E2 (PGE2 ). Previous rodent studies indicate that mGluR2/3 can also reduce peripheral sensitization by suppressing inflammation-induced sensitization of TRPV1...
March 2018: ENeuro
https://www.readbyqxmd.com/read/29661478/chronic-adriamycin-treatment-impairs-cgrp-mediated-functions-of-meningeal-sensory-nerves
#10
Éva Deák, Judit Rosta, Krisztina Boros, Gyöngyi Kis, Péter Sántha, Karl Messlinger, Gábor Jancsó, Mária Dux
Adriamycin is a potent anthracycline-type antitumor agent, but it also exerts potentially serious side effects due to its cardiotoxic and neurotoxic propensity. Multiple impairments in sensory nerve functions have been recently reported in various rat models. The present experiments were initiated in an attempt to reveal adriamycin-induced changes in sensory effector functions of chemosensitive meningeal afferents. Meningeal blood flow was measured with laser Doppler flowmetry in the parietal dura mater of adult male Wistar rats...
April 10, 2018: Neuropeptides
https://www.readbyqxmd.com/read/29660342/investigation-of-trpv1-loss-of-function-phenotypes-in-trpv1-leu206stop-mice-generated-by-n-ethyl-n-nitrosourea-mutagenesis
#11
Thomas Christoph, Babette Kögel, Klaus Schiene, Thomas Peters, Wolfgang Schröder
N-ethyl-N-nitrosourea (ENU) random mutagenesis was used to generate a mouse model for the analysis of the transient receptor potential vanilloid 1 (TRPV1) cation channel. A transversion from T→A in exon 4 led to a Leu206Stop mutation generating a loss-of-function mutant. The TRPV1 agonist capsaicin was used to analyze functional and nociceptive parameters in vitro and in vivo in TRPV1 Leu206Stop mice and congenic C3HeB/FeJ controls. Capsaicin-induced [Ca2+ ]i changes in small diameter DRG neurons were significantly diminished in TRPV1 Leu206Stop mice and administration of capsaicin induced neither hypothermia nor nocifensive behaviour in vivo...
April 13, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29596901/periaqueductal-gray-glutamatergic-cannabinoid-and-vanilloid-receptor-interplay-in-defensive-behavior-and-aversive-memory-formation
#12
Franklin P Back, Antonio P Carobrez
Stimulation of the midbrain periaqueductal gray matter (PAG) in humans elicits sensations of fear and impending terror, and mediates predator defensive responses in rodents. In rats, pharmacological stimulation of the dorsolateral portion of the PAG (dlPAG) with N-Methyl-d-Aspartate (NMDA) induces aversive conditioning that acts as an unconditioned stimulus (US). In the present work, we investigated the interplay between the vanilloid TRPV1 and cannabinoid CB1 receptors in the NMDA-dlPAG defensive response and in subsequent aversive learning...
March 26, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29581825/novel-inhibitor-candidates-of-trpv2-prevent-damage-of-dystrophic-myocytes-and-ameliorate-against-dilated-cardiomyopathy-in-a-hamster-model
#13
Yuko Iwata, Yoshimi Katayama, Yasushi Okuno, Shigeo Wakabayashi
Transient receptor potential cation channel, subfamily V, member 2 (TRPV2) is a principal candidate for abnormal Ca2+ -entry pathways, which is a potential target for therapy of muscular dystrophy and cardiomyopathy. Here, an in silico drug screening and the following cell-based screening to measure the TRPV2 activation were carried out in HEK293 cells expressing TRPV2 using lead compounds (tranilast or SKF96365) and off-patent drug stocks. We identified 4 chemical compounds containing amino-benzoyl groups and 1 compound (lumin) containing an ethylquinolinium group as candidate TRPV2 inhibitors...
March 6, 2018: Oncotarget
https://www.readbyqxmd.com/read/29580951/modality-specific-peripheral-antinociceptive-effects-of-%C3%AE-opioid-agonists-on-heat-and-mechanical-stimuli-contribution-of-sigma-1-receptors
#14
Ángeles Montilla-García, Gloria Perazzoli, Miguel Á Tejada, Rafael González-Cano, Cristina Sánchez-Fernández, Enrique J Cobos, José M Baeyens
Morphine induces peripherally μ-opioid-mediated antinociception to heat but not to mechanical stimulation. Peripheral sigma-1 receptors tonically inhibit μ-opioid antinociception to mechanical stimuli, but it is unknown whether they modulate μ-opioid heat antinociception. We hypothesized that sigma-1 receptors might play a role in the modality-specific peripheral antinociceptive effects of morphine and other clinically relevant μ-opioid agonists. Mechanical nociception was assessed in mice with the paw pressure test (450 g), and heat nociception with the unilateral hot plate (55 °C) test...
March 23, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29578059/the-effect-of-the-electrophilic-fatty-acid-nitro-oleic-acid-on-trp-channel-function-in-sensory-neurons
#15
REVIEW
Jonathan M Beckel, William C de Groat
Nitro-oleic acid (NO2 -OA) and related nitroalkenes are electrophilic fatty acid derivatives that are present in normal tissues at nanomolar concentrations and can increase significantly during inflammation. These substances can suppress multiple intracellular signaling pathways contributing to inflammation by reversible Michael addition reactions with nucleophilic residues such as cysteine and histidine leading to post-translational modification of proteins. NO2 -OA also can influence inflammation and pain by acting on transient receptor potential (TRP) channels in primary sensory neurons...
March 22, 2018: Nitric Oxide: Biology and Chemistry
https://www.readbyqxmd.com/read/29577893/participation-of-transient-receptor-potential-vanilloid-1-in-paclitaxel-induced-acute-visceral-and-peripheral-nociception-in-rodents
#16
Mateus Fortes Rossato, Flavia Karine Rigo, Sara Marchesan Oliveira, Gustavo Petri Guerra, Cássia Regina Silva, Thiago Mattar Cunha, Marcus Vinícius Gomez, Juliano Ferreira, Gabriela Trevisan
The clinical use of paclitaxel as a chemotherapeutic agent is limited by the severe acute and chronic hypersensitivity caused when it is administered via intraperitoneal or intravenous routes. Thus far, evidence has suggested that transient receptor potential vanilloid-1 (TRPV1) has a key role in the chronic neuropathy induced by paclitaxel. Despite this, the role of TRPV1 in paclitaxel -related acute nociception, especially the development of visceral nociception, has not been evaluated. Thus, the goal of this study was to evaluate the participation of TRPV1 in a model of acute nociception induced by paclitaxel in rats and mice...
March 22, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29553496/establishing-a-mouse-model-of-a-pure-small-fiber-neuropathy-with-the-ultrapotent-agonist-of-transient-receptor-potential-vanilloid-type-1
#17
Yi-Chen Lee, Shui-Chin Lu, Yu-Lin Hsieh
Patients with diabetes mellitus (DM) or those experiencing the neurotoxic effects of chemotherapeutic agents may develop sensation disorders due to degeneration and injury of small-diameter sensory neurons, referred to as small fiber neuropathy. Present animal models of small fiber neuropathy affect both large- and small-diameter sensory fibers and thus create a neuropathology too complex to properly assess the effects of injured small-diameter sensory fibers. Therefore, it is necessary to develop an experimental model of pure small fiber neuropathy to adequately examine these issues...
February 13, 2018: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/29543451/analyses-of-synthetic-n-acyl-dopamine-derivatives-revealing-different-structural-requirements-for-their-anti-inflammatory-and-transient-receptor-potential-channel-of-the-vanilloid-receptor-subfamily-subtype-1-trpv1-activating-properties
#18
Prama Pallavi, Marc Pretze, Julio Caballero, Yingchun Li, Björn B Hofmann, Eleni Stamellou, Sarah Klotz, Carmen Wängler, Björn Wängler, Ralf Loesel, Steffen Roth, Bastian Theisinger, Handan Moerz, Uta Binzen, Wolfgang Greffrath, Rolf-Detlef Treede, Martin C Harmsen, Bernhard K Krämer, Mathias Hafner, Benito A Yard, Anna-Isabelle Kälsch
We studied the chemical entities within N-octanoyl dopamine (NOD) responsible for the activation of transient-receptor-potential channels of the vanilloid-receptor subtype 1 (TRPV1) and inhibition of inflammation. The potency of NOD in activating TRPV1 was significantly higher compared with those of variants in which the ortho-dihydroxy groups were acetylated, one of the hydroxy groups was omitted ( N-octanoyl tyramine), or the ester functionality consisted of a bulky fatty acid ( N-pivaloyl dopamine). Shortening of the amide linker (ΔNOD) slightly increased its potency, which was further increased when the carbonyl and amide groups (ΔNODR) were interchanged...
April 12, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29520110/capsaicin-upregulates-hdac2-via-trpv1-and-impairs-neuronal-maturation-in-mice
#19
Sung Eun Wang, Seung Yeon Ko, Yong-Seok Kim, Sungsin Jo, Seung Hoon Lee, Sung Jun Jung, Hyeon Son
Transient receptor potential vanilloid 1 (TRPV1) affects mood and neuroplasticity in the brain, where its role is poorly understood. In the present study we investigated whether capsaicin (8-methyl-N-vanillyl-trans-6-nonenamide), an agonist of TRPV1, induced chromatin remodeling and thereby altered gene expression related to synaptic plasticity. We found that capsaicin treatment resulted in upregulation of histone deacetylase 2 (HDAC2) in the mouse hippocampus and HDAC2 was enriched at Psd95, synaptophysin, GLUR1, GLUR2 promoters...
March 9, 2018: Experimental & Molecular Medicine
https://www.readbyqxmd.com/read/29518656/copper-induced-activation-of-trp-channels-promotes-extracellular-calcium-entry-and-activation-of-camk-pka-pkc-pkg-and-cblpk-leading-to-increased-expression-of-antioxidant-enzymes-in-ectocarpus-siliculosus
#20
Alberto González, Claudio A Sáez, Bernardo Morales, Alejandra Moenne
The existence of functional Transient Receptor Potential (TRP) channels was analyzed in Ectocarpus siliculosus using agonists of human TRPs and specific antagonists of TRPA1, TRPC5, TRPM8 and TRPV; intracellular calcium was detected for 60 min. Increases in intracellular calcium were observed at 13, 29, 39 and 50-52 min, which appeared to be mediated by the activation of TRPM8/V1 at 13 min, TRPV1 at 29 min, TRPA1/V1 at 39 min and TRPA1/C5 at 50-52 min. In addition, intracellular calcium increases appear to be due to extracellular calcium entry, not requiring protein kinase activation...
May 2018: Plant Physiology and Biochemistry: PPB
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