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https://www.readbyqxmd.com/read/29048662/capsaicin-inhibits-proliferation-and-induces-apoptosis-in-osteosarcoma-cell-lines-via-the-mitogen%C3%A2-activated-protein-kinase-pathway
#1
Yuan Zhang, Xu Deng, Tao Lei, Chang Yu, Yang Wang, Guosheng Zhao, Xiaoji Luo, Ke Tang, Zhengxue Quan, Dianming Jiang
Capsaicin, a pungent molecular compound present in many hot peppers, exerts anticancer activities against various human cancer cell lines by inducing apoptosis. However, the effects of capsaicin on human osteosarcoma (OS) as well as the related mechanisms remain to be fully elucidated. In the present study, the anticancer effects of capsaicin on 3 human OS cell lines (MG63, 143B and HOS) were investigated. Various concentrations of capsaicin (50-300 µM) effectively decreased cell viability in all 3 OS cell lines in a dose-dependent manner...
September 18, 2017: Oncology Reports
https://www.readbyqxmd.com/read/29046638/blockade-of-cannabinoid-cb1-receptors-in-the-dorsal-periaqueductal-gray-unmasks-the-antinociceptive-effect-of-local-injections-of-anandamide-in-mice
#2
Diego C Mascarenhas, Karina S Gomes, Tatiani Sorregotti, Ricardo L Nunes-de-Souza
Divergent results in pain management account for the growing number of studies aiming at elucidating the pharmacology of the endocannabinoid/endovanilloid anandamide (AEA) within several pain-related brain structures. For instance, the stimulation of both Transient Receptor Potential Vanilloid type 1 (TRPV1) and Cannabinoid type 1 (CB1) receptors led to paradoxical effects on nociception. Here, we attempted to propose a clear and reproducible methodology to achieve the antinociceptive effect of exogenous AEA within the dorsal periaqueductal gray (dPAG) of mice exposed to the tail-flick test...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29042318/mechanisms-of-%C3%AE-opioid-receptor-inhibition-of-nmda-receptor-induced-substance-p-release-in-the-rat-spinal-cord
#3
Wenling Chen, Helena S Ennes, James A McRoberts, Juan Carlos Marvizon
The interaction between NMDA receptors and μ-opioid receptors in primary afferent terminals was studied by using NMDA to induce substance P release, measured as neurokinin 1 receptor internalization. In rat spinal cord slices, the μ-opioid receptor agonists morphine, DAMGO and endomorphin-2 inhibited NMDA-induced substance P release, whereas the antagonist CTAP right-shifted the concentration response of DAMGO. In vivo, substance P release induced by intrathecal NMDA after priming with BDNF was inhibited by DAMGO...
October 14, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29035821/neuronal-nitric-oxide-synthase-is-involved-in-cb-trpv1-signalling-focus-on-control-of-hippocampal-hyperexcitability
#4
Fabio Carletti, Giuditta Gambino, Valerio Rizzo, Giuseppe Ferraro, Pierangelo Sardo
Cannabinoids (CB), transient receptors potential vanilloid type 1 (TRPV1) and nitric oxide (NO) were found to be interlinked in regulating some neuronal functions such as membrane excitability and synaptic transmission. TRPV1 play a fundamental role since it represents a synaptic target for CB that triggers several downstream cellular pathways. In this regard, recent evidence report that TRPV1 could influence NO production by modulating neuronal NO synthase (nNOS) activity. In the present research, we pointed to manipulate nNOS function to assess its role on TRPV1 signalling in hyperexcitability conditions elicited in the dentate gyrus of hippocampal formation...
October 3, 2017: Epilepsy Research
https://www.readbyqxmd.com/read/29035314/animal-toxins-providing-insights-into-trpv1-activation-mechanism
#5
REVIEW
Matan Geron, Adina Hazan, Avi Priel
Beyond providing evolutionary advantages, venoms offer unique research tools, as they were developed to target functionally important proteins and pathways. As a key pain receptor in the nociceptive pathway, transient receptor potential vanilloid 1 (TRPV1) of the TRP superfamily has been shown to be a target for several toxins, as a way of producing pain to deter predators. Importantly, TRPV1 is involved in thermoregulation, inflammation, and acute nociception. As such, toxins provide tools to understand TRPV1 activation and modulation, a critical step in advancing pain research and the development of novel analgesics...
October 16, 2017: Toxins
https://www.readbyqxmd.com/read/29024230/%C3%AE-aminobutyric-acid-gaba-oral-rinse-reduces-capsaicin-induced-burning-mouth-pain-sensation-an-experimental-quantitative-sensory-testing-study-in-healthy-subjects
#6
Y Zhang, K Wang, L Arendt-Nielsen, B E Cairns
BACKGROUND: In burning mouth patients, analgesia after oral administration of clonazepam may result from modulation of peripheral γ-aminobutyric acid (GABA) receptors. METHODS: The effect of oral administration of test solutions (water, 0.5 mol/L or 0.05 mol/L GABA, 1% lidocaine) was investigated for the amelioration of pain and sensitivity induced by application of capsaicin (1%, 2 min) to the tongue of thirty healthy male and female subjects in this four-session, randomized, placebo-controlled, double-blinded, cross-over study...
October 11, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/29023749/preparative-isolation-and-purification-of-capsaicin-and-dihydrocapsaicin-from-capsici-fructus-using-supercritical-fluid-extraction-combined-with-high-speed-countercurrent-chromatography
#7
Rongwei Yan, Leilei Zhao, Junfei Tao, Yong Zou, Xinjun Xu
BACKGROUND: Supercritical fluid extraction with CO2 (SFE-CO2 ) was utilized for extraction of capsaicin (CA) and dihydrocapsaicin (DHCA) from Capsici Fructus, and then a two-step enrichment method about separating capsaicinoids from SFE-CO2 extracts was developed. The process involved extraction with aqueous methanol and crystallization by alkali-extraction and acid-precipitation. Finally, a consecutive high speed countercurrent chromatography (HSCCC) separation method was successfully applied in the purification of CA and DHCA from capsaicinoids crystal...
October 11, 2017: Journal of the Science of Food and Agriculture
https://www.readbyqxmd.com/read/29017758/in-vitro-and-in-vivo-pharmacological-characterization-of-asp8477-a-novel-highly-selective-fatty-acid-amide-hydrolase-inhibitor
#8
Tomonari Watabiki, Noriko Tsuji, Tetsuo Kiso, Tohru Ozawa, Fumie Narazaki, Shuichiro Kakimoto
Although exogenous agonists for cannabinoid (CB) receptors are clinically effective for treating chronic pain, global activation of brain CB receptors causes frequent central nervous system (CNS) side-effects. Fatty acid amide hydrolase (FAAH) is a primary catabolic enzyme for anandamide (AEA), an endogenous CB. Recently, we discovered a novel FAAH inhibitor, 3-pyridyl 4-(phenylcarbamoyl)piperidine-1-carboxylate (ASP8477). In vitro studies demonstrated that ASP8477 inhibited human FAAH-1, FAAH-1 (P129T) and FAAH-2 activity with IC50 values of 3...
October 7, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28994767/effects-of-exposure-of-formaldehyde-to-a-rat-model-of-atopic-dermatitis-induced-by-neonatal-capsaicin-treatment
#9
Rafael Taeho Han, Seung Keun Back, JaeHee Lee, Hye Young Kim, Hee Jin Kim, Heung Sik Na
Atopic dermatitis is chronically relapsing pruritic eczema and prevails around the world especially in developed countries. Complex interactions between genetic and environmental factors are known to play an important role in the pathophysiology of atopic dermatitis. However, we still lack a detailed picture of the pathogenesis of this disease. Thus, it is of importance to develop appropriate animal models for elucidating the progression of atopic dermatitis. Moreover, investigating the effect of environmental factors such as air pollutants on atopic dermatitis expands understanding of the disease...
September 27, 2017: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/28992455/-1-h-nmr-studies-of-molecular-interaction-of-d-glucosamine-and-n-acetyl-d-glucosamine-with-capsaicin-in-aqueous-and-non-aqueous-media
#10
Inocencio Higuera-Ciapara, Claudia Virués, Marcela Jiménez-Chávez, Evelin Martínez-Benavidez, Javier Hernández, Zaira Domínguez, Roberto López-Rendón, Enrique F Velázquez, Motomichi Inoue
Complex formation of D-glucosamine (Gl) and N-acetyl-D-glucosamine (AGl) with capsaicin (Cp) were studied by (1)H NMR titrations in H2O-d2 and DMSO-d6; capsaicin is the major bioactive component of chili peppers. Every titration curve has been interpreted by formulating a suitable model for the reaction equilibrium, to elucidate intermolecular interactions. In DMSO, glucosamine cations associate with each other to yield linear aggregates, and undergo pseudo-1:1-complexation with capsaicin, the formation constant being ca...
September 29, 2017: Carbohydrate Research
https://www.readbyqxmd.com/read/28988851/ablation-of-c-fibers-decreases-quantal-size-of-gabaergic-synaptic-transmission-in-the-insular-cortex
#11
Shota Murayama, Kiyofumi Yamamoto, Mari Kaneko, Bunnai Ogiso, Masayuki Kobayashi
The primary sensory cortex exhibits neuroplastic changes responding to sensory disturbances, and GABAergic synaptic transmission plays a critical role in the regulation of plasticity. The insular cortex (IC) integrates orofacial nociceptive signals conveyed via myelinated Aδ- and unmyelinated C-fibers. However, it has been unknown whether a disturbance of nociceptive inputs, such as a deletion of the peripheral nerves, alters GABAergic local circuit in IC. The present study elucidated GABAergic synaptic transmission in the model rat whose C-fibers were ablated by capsaicin injection 1-2 days after birth...
October 6, 2017: Neuroscience
https://www.readbyqxmd.com/read/28986540/reactive-metabolites-of-acetaminophen-activate-and-sensitize-the-capsaicin-receptor-trpv1
#12
Mirjam J Eberhardt, Florian Schillers, Esther M Eberhardt, Linus Risser, Jeanne de la Roche, Christine Herzog, Frank Echtermeyer, Andreas Leffler
The irritant receptor TRPA1 was suggested to mediate analgesic, antipyretic but also pro-inflammatory effects of the non-opioid analgesic acetaminophen, presumably due to channel activation by the reactive metabolites parabenzoquinone (pBQ) and N-acetyl-parabenzoquinonimine (NAPQI). Here we explored the effects of these metabolites on the capsaicin receptor TRPV1, another redox-sensitive ion channel expressed in sensory neurons. Both pBQ and NAPQI, but not acetaminophen irreversibly activated and sensitized recombinant human and rodent TRPV1 channels expressed in HEK 293 cells...
October 6, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28984399/characterization-of-a-novel-capsaicin-heat-ongoing-pain-model
#13
R C Price, W Gandhi, C Nadeau, R Tarnavskiy, A Qu, E Fahey, L Stone, P Schweinhardt
BACKGROUND: Human experimental pain models provide an important translational link between pre-clinical models and clinical pain. Using topical capsaicin and continuous heat application, the novel capsaicin/heat ongoing pain (CHOP) model induces long-lasting experimental pain of which the perceived intensity can be individually adjusted. METHODS: In the CHOP model, capsaicin or control cream is applied to a 10 × 10 cm skin area and a heating pad is applied over the area after cream removal...
October 6, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28982207/transient-receptor-potential-vanilloid-1-inhibitors-block-laparotomy-and-opioid-induced-infarct-size-reduction-in-rats
#14
Helen M Heymann, Yun Wu, Yao Lu, Nir Qvit, Garrett J Gross, Eric R Gross
BACKGROUND AND PURPOSE: In light of the opioid epidemic, physicians are increasingly prescribing non-opioid analgesics to surgical patients. Transient receptor potential vanilloid 1 (TRPV1) inhibitors are potentially alternative pain therapeutics for surgery. Here we examined in rodents whether cardioprotection conferred by two occurrences during surgery, a laparotomy or morphine delivery, is mediated by TRPV1. We further tested whether an experimental analgesic peptide (known as P5) targeted against the TRPV1 C-terminus region interferes with laparotomy- or morphine-induced cardioprotection...
October 5, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28982197/distinct-and-common-expression-of-receptors-for-inflammatory-mediators-in-vagal-nodose-versus-jugular-capsaicin-sensitive-trpv1-positive-neurons-detected-by-low-input-rna-sequencing
#15
Jingya Wang, Marian Kollarik, Fei Ru, Hui Sun, Benjamin McNeil, Xinzhong Dong, Geoffrey Stephens, Susana Korolevich, Philip Brohawn, Roland Kolbeck, Bradley Undem
Capsaicin-sensitive sensory C-fibers derived from vagal ganglia innervate the visceral organs, and respond to inflammatory mediators and noxious stimuli. These neurons play an important role in maintenance of visceral homeostasis, and contribute to the symptoms of visceral inflammatory diseases. Vagal sensory neurons are located in two ganglia, the jugular ganglia (derived from the neural crest), and the nodose ganglia (from the epibranchial placodes). The functional difference, especially in response to immune mediators, between jugular and nodose neurons is not fully understood...
2017: PloS One
https://www.readbyqxmd.com/read/28981081/influence-of-gaba-b-agonist-baclofen-on-capsaicin-induced-excitation-of-secondary-peristalsis-in-humans
#16
Wei-Yi Lei, Jui-Sheng Hung, Tso-Tsai Liu, Chih-Hsun Yi, Chien-Lin Chen
OBJECTIVES: Esophageal instillation of capsaicin enhances secondary peristalsis, but the γ-aminobutyric acid receptor type B (GABA-B) agonist baclofen inhibits secondary peristalsis. This study aimed to investigate whether baclofen could influence heartburn perception and secondary peristalsis subsequent to capsaicin infusion in healthy adults. METHODS: Secondary peristalsis was performed by slow and rapid mid-esophagus air injections in 15 healthy subjects. Two different sessions including esophageal infusion of capsaicin-containing red pepper sauce (0...
October 5, 2017: Clinical and Translational Gastroenterology
https://www.readbyqxmd.com/read/28977586/estradiol-sensitizes-the-transient-receptor-potential-vanilloid-1-receptor-in-pain-responses
#17
Maja Payrits, Éva Sághy, Kata Cseko, Krisztina Pohóczky, Kata Bölcskei, Dávid Ernszt, Klaudia Barabás, János Szolcsányi, István M Ábrahám, Zsuzsanna Helyes, Éva Szoke
Sex differences exist in chronic pain pathologies, and gonadal estradiol (E2) alters the pain sensation. The nocisensor transient receptor potential vanilloid 1 (TRPV1) receptor plays a critical role in triggering pain. Here we examined the impact of E2 on the function of TRPV1 receptor in mice sensory neurons in vitro and in vivo. Both mechano- and thermonociceptive thresholds of the plantar surface of the paw of female mice were significantly lower in proestrus compared with the estrus phase. These thresholds were higher in ovariectomized (OVX) mice and significantly lower in sham-operated mice in proestrus compared with the sham-operated mice in estrus phase...
October 1, 2017: Endocrinology
https://www.readbyqxmd.com/read/28970017/role-of-ventrolateral-orbital-cortex-muscarinic-and-nicotinic-receptors-in-modulation-of-capsaicin-induced-orofacial-pain-related-behaviors-in-rats
#18
Esmaeal Tamaddonfard, Amir Erfanparast, Amir Abbas Farshid, Fatmeh Delkhosh-Kasmaie
Acetylcholine, as a major neurotransmitter, mediates many brain functions such as pain. This study was aimed to investigate the effects of microinjection of muscarinic and nicotinic acetylcholine receptor antagonists and agonists into the ventrolateral orbital cortex (VLOC) on capsaicin-induced orofacial nociception and subsequent hyperalgesia. The right side of VLOC was surgically implanted with a guide cannula in anaesthetized rats. Orofacial pain-related behaviors were induced by subcutaneous injection of a capsaicin solution (1...
September 29, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28957441/diversity-amongst-trigeminal-neurons-revealed-by-high-throughput-single-cell-sequencing
#19
Minh Q Nguyen, Youmei Wu, Lauren S Bonilla, Lars J von Buchholtz, Nicholas J P Ryba
The trigeminal ganglion contains somatosensory neurons that detect a range of thermal, mechanical and chemical cues and innervate unique sensory compartments in the head and neck including the eyes, nose, mouth, meninges and vibrissae. We used single-cell sequencing and in situ hybridization to examine the cellular diversity of the trigeminal ganglion in mice, defining thirteen clusters of neurons. We show that clusters are well conserved in dorsal root ganglia suggesting they represent distinct functional classes of somatosensory neurons and not specialization associated with their sensory targets...
2017: PloS One
https://www.readbyqxmd.com/read/28956064/nature-is-the-best-source-of-anti-inflammatory-drugs-indexing-natural-products-for-their-anti-inflammatory-bioactivity
#20
Miran Aswad, Mahmoud Rayan, Saleh Abu-Lafi, Mizied Falah, Jamal Raiyn, Ziyad Abdallah, Anwar Rayan
OBJECTIVES: The aim was to index natural products for less expensive preventive or curative anti-inflammatory therapeutic drugs. MATERIALS: A set of 441 anti-inflammatory drugs representing the active domain and 2892 natural products representing the inactive domain was used to construct a predictive model for bioactivity-indexing purposes. METHOD: The model for indexing the natural products for potential anti-inflammatory activity was constructed using the iterative stochastic elimination algorithm (ISE)...
September 27, 2017: Inflammation Research: Official Journal of the European Histamine Research Society ... [et Al.]
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