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https://www.readbyqxmd.com/read/29153839/asymmetry-between-activation-and-deactivation-during-a-transcriptional-pulse
#1
Lee S S Dunham, Hiroshi Momiji, Claire V Harper, Polly J Downton, Kirsty Hey, Anne McNamara, Karen Featherstone, David G Spiller, David A Rand, Bärbel Finkenstädt, Michael R H White, Julian R E Davis
Transcription in eukaryotic cells occurs in gene-specific bursts or pulses of activity. Recent studies identified a spectrum of transcriptionally active "on-states," interspersed with periods of inactivity, but these "off-states" and the process of transcriptional deactivation are poorly understood. To examine what occurs during deactivation, we investigate the dynamics of switching between variable rates. We measured live single-cell expression of luciferase reporters from human growth hormone or human prolactin promoters in a pituitary cell line...
November 13, 2017: Cell Systems
https://www.readbyqxmd.com/read/29151076/modulation-of-the-endocannabinoid-system-by-the-fatty-acid-amide-hydrolase-monoacylglycerol-and-diacylglycerol-lipase-inhibitors-as-an-attractive-target-for-secretory-diarrhoea-therapy
#2
A Wasilewski, A Misicka, M Sacharczuk, J Fichna
Secretory diarrhoea is a leading cause of mortality and morbidity worldwide. Our aim was to characterize the effect of inhibition of selected enzymes involved in the synthesis or degradation of endocannabinoids on electrolyte equilibrium in the mouse colonic tissue. The aim of this study was to evaluate the effects of PF-3845, JZL-184 and RHC-80267, as inhibitors of fatty acid amide hydrolase (FAAH), monoacylglycerol (MAGL) and diacylglycerol lipase (DAGL), respectively on epithelial ion transport in isolated mouse colon stimulated by forskolin (FSK), veratridine (VER) and bethanechol (BET)...
August 2017: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
https://www.readbyqxmd.com/read/29146864/acute-hypoxia-reoxygenation-and-vascular-oxygen-sensing-in-the-chicken-embryo
#3
Riazuddin Mohammed, Carlos E Salinas, Dino A Giussani, Carlos E Blanco, Angel L Cogolludo, Eduardo Villamor
Fetal/perinatal hypoxia is one of the most common causes of perinatal morbidity and mortality and is frequently accompannied by vascular dysfunction. However, the mechanisms involved have not been fully delineated. We hypothesized that exposure to acute hypoxia-reoxygenation induces alterations in vascular O2 sensing/signaling as well as in endothelial function in the chicken embryo pulmonary artery (PA), mesenteric artery (MA), femoral artery (FA), and ductus arteriosus (DA). Noninternally pipped 19-day embryos were exposed to 10% O2 for 30 min followed by reoxygenation with 21% O2 or 80% O2 Another group was constantly maintained at 21% O2 or at 21% O2 for 30 min and then exposed to 80% O2 Following treatment, responses of isolated blood vessels to hypoxia as well as endothelium-dependent (acetylcholine) and -independent (sodium nitroprusside and forskolin) relaxation were investigated in a wire myograph...
November 2017: Physiological Reports
https://www.readbyqxmd.com/read/29142291/resveratrol-modulates-cocaine-induced-inhibitory-synaptic-plasticity-in-vta-dopamine-neurons-by-inhibiting-phosphodiesterases-pdes
#4
Yan Li, Laikang Yu, Li Zhao, Fanxing Zeng, Qing-Song Liu
Resveratrol is a natural phytoalexin synthesized by plants, including grapes. It displays a wide range of neuroprotective benefits associated with anti-aging. Recent studies have shown that resveratrol regulates dopaminergic transmission and behavioral effects of drugs of abuse. The goal of the present study is to investigate whether and how resveratrol alters basal inhibitory synaptic transmission and cocaine-induced inhibitory synaptic plasticity in dopamine neurons of the ventral tegmental area (VTA). We report that resveratrol elevated cAMP levels by itself and further potentiated a forskolin-induced increase in cAMP levels in midbrain slices, consistent with reported effects of inhibition of phosphodiesterases (PDEs)...
November 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29138698/soluble-epoxide-hydrolase-inhibitor-and-14-15-epoxyeicosatrienoic-acid-facilitated-long-term-potentiation-through-camp-and-camkii-in-the-hippocampus
#5
Han-Fang Wu, Yi-Ju Chen, Su-Zhen Wu, Chi-Wei Lee, I-Tuan Chen, Yi-Chao Lee, Chi-Chen Huang, Chung-Hsi Hsing, Chih-Wei Tang, Hui-Ching Lin
Epoxyeicosatrienoic acids (EETs) are derived from arachidonic acid and metabolized by soluble epoxide hydrolase (sEH). The role of EETs in synaptic function in the central nervous system is still largely unknown. We found that pharmacological inhibition of sEH to stabilize endogenous EETs and exogenous 14,15-EET significantly increased the field excitatory postsynaptic potential (fEPSP) response in the CA1 area of the hippocampus, while additionally enhancing high-frequency stimulation- (HFS-) induced long-term potentiation (LTP) and forskolin- (FSK-) induced LTP...
2017: Neural Plasticity
https://www.readbyqxmd.com/read/29133260/expression-of-fshr-in-chondrocytes-and-the-effect-of-fsh-on-chondrocytes
#6
Dehuan Kong, Qingbo Guan, Guandong Li, Wei Xin, Xiaoyi Qi, Yanjing Guo, Jiajun Zhao, Jin Xu, Shui Sun, Ling Gao
OBJECTIVE: Chondrocytes express many kinds of hormone receptors. The function of Follicle stimulating hormone (FSH) in the ovary is mediated by FSH receptor (FSHR). FSH receptor (FSHR) is found in many non-ovarian tissues, however it has been unclear if chondrocytes express FSHR. The purpose of this study is to determine it. METHODS: Mouse primary chondrocytes and human articular cartilage tissues were examined. The expression and sequence of FSHR mRNA by reverse transcription polymerase chain reaction (RT-PCR) and sequenced, respectively, and its protein expression was tested using western blotting and location was observed under immunofluorescence microscopy...
November 10, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29127599/cb1-receptors-mediated-inhibition-of-atp-induced-ca-2-i-increase-in-cultured-rat-spinal-dorsal-horn-neurons
#7
Jingdong Long, Xiaolu Lei, Meiyun Chen, Shulei Yang, Tao Sun, Junwei Zeng, Deqian Yu, Hong Tian, Xiaohong Liu
Spinal cannabinoid receptor 1 (CB1R) and purinergic P2X receptors (P2XR) play a critical role in the process of pathological pain. Both CB1R and P2XR are expressed in spinal dorsal horn (DH) neurons. It is not clear whether CB1 receptor activation modulates the function of P2X receptor channels within dorsal horn. For this reason, we observed the effect of CP55940 (cannabinoid receptor agonist) on ATP-induced Ca(2+) mobilization in cultured rat DH neurons. The changes of intracellular calcium concentration ([Ca(2+)]i) were detected with confocal laser scanning microscopy using fluo-4/AM as a calcium fluorescent indicator...
November 10, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/29125193/exposure-to-a-specific-time-varying-electromagnetic-field-inhibits-cell-proliferation-via-camp-and-erk-signaling-in-cancer-cells
#8
Carly A Buckner, Alison L Buckner, Stan A Koren, Michael A Persinger, Robert M Lafrenie
Exposure to specific electromagnetic field (EMF) patterns can affect a variety of biological systems. We have shown that exposure to Thomas-EMF, a low-intensity, frequency-modulated (25-6 Hz) EMF pattern, inhibited growth and altered cell signaling in malignant cells. Exposure to Thomas-EMF for 1 h/day inhibited the growth of malignant cells including B16-BL6 mouse melanoma cells, MDA-MB-231, MDA-MB-468, BT-20, and MCF-7 human breast cancer and HeLa cervical cancer cells but did not affect non-malignant cells...
November 10, 2017: Bioelectromagnetics
https://www.readbyqxmd.com/read/29109685/binding-and-signaling-studies-disclose-a-potential-allosteric-site-for-cannabidiol-in-cannabinoid-cb2-receptors
#9
Eva Martínez-Pinilla, Katia Varani, Irene Reyes-Resina, Edgar Angelats, Fabrizio Vincenzi, Carlos Ferreiro-Vera, Julen Oyarzabal, Enric I Canela, José L Lanciego, Xavier Nadal, Gemma Navarro, Pier Andrea Borea, Rafael Franco
The mechanism of action of cannabidiol (CBD), the main non-psychotropic component of Cannabis sativa L., is not completely understood. First assumed that the compound was acting via cannabinoid CB2 receptors (CB2Rs) it is now suggested that it interacts with non-cannabinoid G-protein-coupled receptors (GPCRs); however, CBD does not bind with high affinity to the orthosteric site of any GPCR. To search for alternative explanations, we tested CBD as a potential allosteric ligand of CB2R. Radioligand and non-radioactive homogeneous binding, intracellular cAMP determination and ERK1/2 phosphorylation assays were undertaken in heterologous systems expressing the human version of CB2R...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29108990/laminin-1-induces-endocytosis-of-67kda-laminin-receptor-and-protects-neuroscreen-1-cells-against-death-induced-by-serum-withdrawal
#10
Rayudu Gopalakrishna, Usha Gundimeda, Sarah Zhou, Helena Bui, Andrew Davis, Thomas McNeill, William Mack
Although the function of laminin in the basement membrane is known, the function of soluble "neuronal" laminin is unknown. Since laminin is neuroprotective, we determined whether the soluble laminin-1 induces signaling for neuroprotection via its 67KDa laminin-1 receptor (67LR). Treatment of Neuroscreen-1 (NS-1) cells with laminin-1 or YIGSR peptide, which corresponds to a sequence in laminin-1 β1 chain that binds to 67LR, induced a decrease in the cell-surface expression of 67LR and caused its internalization...
November 8, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29103957/basolateral-cholesterol-depletion-alters-aquaporin-2-post-translational-modifications-and-disrupts-apical-plasma-membrane-targeting
#11
Hanne B Moeller, Cecilia Hvitfeldt Fuglsang, Cecilie Nøhr Pedersen, Robert A Fenton
Apical plasma membrane accumulation of the water channel Aquaporin-2 (AQP2) in kidney collecting duct principal cells is critical for body water homeostasis. Posttranslational modification (PTM) of AQP2 is important for regulating AQP2 trafficking. The aim of this study was to determine the role of cholesterol in regulation of AQP2 PTM and in apical plasma membrane targeting of AQP2. Cholesterol depletion from the basolateral plasma membrane of a collecting duct cell line (mpkCCD14) using methyl-beta-cyclodextrin (MBCD) increased AQP2 ubiquitylation...
November 2, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29101175/loss-of-caveolin-3-dependent-regulation-of-ica-in-rat-ventricular-myocytes-in-heart-failure
#12
Simon M Bryant, Cherrie H T Kong, Mark B Cannell, Clive H Orchard, Andrew F James
β2-adrenoceptors and the L-type Ca current (ICa) redistribute from the t-tubules to the surface membrane of ventricular myocytes from failing hearts. The present study investigated the role of changes in caveolin-3 (Cav-3) and protein kinase A (PKA) signaling, both of which have previously been implicated in this redistribution. ICa was recorded using the whole cell patch clamp technique from ventricular myocytes isolated from the hearts of rats that had undergone either coronary artery ligation (CAL) or equivalent Sham operation 18 weeks earlier...
November 3, 2017: American Journal of Physiology. Heart and Circulatory Physiology
https://www.readbyqxmd.com/read/29097424/the-free-fatty-acid-receptor-1-promotes-airway-smooth-muscle-cell-proliferation-through-mek-erk-and-pi3k-akt-signaling-pathways
#13
Atsuko Matoba, Nao Matsuyama, Sumire Shibata, Eiji Masaki, Charles W Emala, Kentaro Mizuta
Obesity is a risk factor for asthma and influences airway hyperresponsiveness, which is in part modulated by airway smooth muscle proliferative remodeling. Plasma free fatty acids (FFAs) levels are elevated in obese individuals, and long-chain FFAs act as endogenous ligands for the free fatty acid receptor 1 (FFAR1), which couples to both Gq and Gi proteins. We examined whether stimulation of FFAR1 induces airway smooth muscle cell proliferation through classical MEK/ERK and/or PI3K/Akt signaling pathways. The long-chain FFAs (oleic acid and linoleic acid) and a FFAR1 agonist (GW9508) induced human airway smooth muscle (HASM) cell proliferation, which was inhibited by the MEK inhibitor U0126 and the PI3K inhibitor LY294002...
November 2, 2017: American Journal of Physiology. Lung Cellular and Molecular Physiology
https://www.readbyqxmd.com/read/29081032/prolonged-morphine-treatment-alters-expression-and-plasma-membrane-distribution-of-%C3%AE-adrenergic-receptors-and-some-other-components-of-their-signaling-system-in-rat-cerebral-cortex
#14
Lucie Hejnova, Jitka Skrabalova, Jiri Novotny
β-Adrenergic signaling plays an important role in regulating diverse brain functions and alterations in this signaling have been observed in different neuropathological conditions. In this study, we investigated the effect of a 10-day treatment with high doses of morphine (10 mg/kg per day) on major components and functional state of the β-adrenergic receptor (β-AR) signaling system in the rat cerebral cortex. β-ARs were characterized by radioligand binding assays and amounts of various G protein subunits, adenylyl cyclase (AC) isoforms, G protein-coupled receptor kinases (GRKs), and β-arrestin were examined by Western blot analysis...
October 28, 2017: Journal of Molecular Neuroscience: MN
https://www.readbyqxmd.com/read/29078739/effects-of-a-new%C3%A2-combination-of%C3%A2-plant-extracts-plus-d-mannose-for-the-management-of-uncomplicated-recurrent-urinary-tract-infections
#15
Carlo Genovese, Sergio Davinelli, Katia Mangano, Gianna Tempera, Daria Nicolosi, Salvatore Corsello, Franca Vergalito, Edoardo Tartaglia, Giovanni Scapagnini, Roberto Di Marco
Urinary tract infections (UTIs) are an economic burden for public health. The increasing prevalence of resistant bacteria which cause UTIs may be related to the inappropriate prescription of antibiotics. The aim of this preliminary study was to evaluate whether three different combinations of plant extracts plus d-mannose are effective in preventing the recurrence of UTIs. Three groups of patients received three combinations of plant extracts in conjunction with d-mannose. These were: berberine, arbutin and birch (group A); berberine, arbutin, birch and forskolin (group B); and proanthocyanidins (group C)...
October 27, 2017: Journal of Chemotherapy
https://www.readbyqxmd.com/read/29068160/the-effect-of-fluoride-on-the-structure-function-and-proteome-of-intestinal-epithelia
#16
Flávia Amadeu de Oliveira, Lesley J MacVinish, Simran Amin, Duleni Herath, Pia Jeggle, Ioanna Mela, Maria Pieri, Chetanya Sharma, Gavin E Jarvis, Flávia M Levy, Mariana R Santesso, Zohaib N Khan, Aline L Leite, Rodrigo C Oliveira, Marília A R Buzalaf, J Michael Edwardson
Fluoride exposure is widespread, with drinking water commonly containing natural and artificially added sources of the ion. Ingested fluoride undergoes absorption across the gastric and intestinal epithelia. Previous studies have reported adverse gastrointestinal effects with high levels of fluoride exposure. Here, we examined the effects of fluoride on the transepithelial ion transport and resistance of three intestinal epithelia. We used the Caco-2 cell line as a model of human intestinal epithelium, and rat and mouse colonic epithelia for purposes of comparison...
October 25, 2017: Environmental Toxicology
https://www.readbyqxmd.com/read/29066718/hyperlipidemia-induced-cholesterol-crystal-production-by-endothelial-cells-promotes-atherogenesis
#17
Yvonne Baumer, Sara McCurdy, Tina M Weatherby, Nehal N Mehta, Stefan Halbherr, Pascal Halbherr, Noboru Yamazaki, William A Boisvert
Endothelial cells (EC) play a key role in atherosclerosis. Although EC are in constant contact with low density lipoproteins (LDL), how EC process LDL and whether this influences atherogenesis, is unclear. Here we show that EC take up and metabolize LDL, and when overburdened with intracellular cholesterol, generate cholesterol crystals (CC). The CC are deposited on the basolateral side, and compromise endothelial function. When hyperlipidemic mice are given a high fat diet, CC appear in aortic sinus within 1 week...
October 24, 2017: Nature Communications
https://www.readbyqxmd.com/read/29050254/rgs19-upregulates-nm23-h1-2-metastasis-suppressors-by-transcriptional-activation-via-the-camp-pka-creb-pathway
#18
Yuanjun Li, Jiaxing Song, Yao Tong, Sookja Kim Chung, Yung H Wong
The Nm23 metastasis suppressor family is involved in physiological and pathological processes including tumorigenesis and metastasis. Although the inverse correlation of Nm23 level with tumor metastasis potential has been widely observed, the mechanisms that regulate the expression of Nm23 remain poorly understood. Our previous studies have revealed that Nm23-H1/2 isoforms are upregulated by RGS19, a regulator of G protein signaling (RGS) protein which accelerates the termination of Gi signals. Here, we examined the ability of RGS19 to stimulate transcriptional regulation of Nm23 by screening a panel of luciferase reporter genes...
September 19, 2017: Oncotarget
https://www.readbyqxmd.com/read/29033832/cyclotides-isolated-from-an-ipecac-root-extract-antagonize-the-corticotropin-releasing-factor-type-1-receptor
#19
Mohsen Fahradpour, Peter Keov, Carlotta Tognola, Estela Perez-Santamarina, Peter J McCormick, Alireza Ghassempour, Christian W Gruber
Cyclotides are plant derived, cystine-knot stabilized peptides characterized by their natural abundance, sequence variability and structural plasticity. They are abundantly expressed in Rubiaceae, Psychotrieae in particular. Previously the cyclotide kalata B7 was identified to modulate the human oxytocin and vasopressin G protein-coupled receptors (GPCRs), providing molecular validation of the plants' uterotonic properties and further establishing cyclotides as valuable source for GPCR ligand design. In this study we screened a cyclotide extract derived from the root powder of the South American medicinal plant ipecac (Carapichea ipecacuanha) for its GPCR modulating activity of the corticotropin-releasing factor type 1 receptor (CRF1R)...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29032334/anti-hypersensitivity-effects-of-the-phthalimide-derivative-n-4methyl-phenyl-4-methylphthalimide-in-different-pain-models-in-mice
#20
Gislaine Francieli da Silva, Mariana Ferreira Dos Anjos, Lilian Wunsch Rocha, Luiz Felipe Gomes Rebello Ferreira, Dorimar Serafim Stiz, Rogério Corrêa, Jose Roberto Santin, Valdir Cechinel Filho, Marcelo Zaldini Hernandes, Nara Lins Meira Quintão
The treatment of chronic pain remains a challenge for clinicians worldwide, independent of its pathogenesis. It motivates several studies attempting to discover strategies to treat the disease. The in silico analysis using molecular docking approach demonstrated that the phthalimide N-(4methyl-phenyl)-4-methylphthalimide (MPMPH-1) presented high affinity to adenylyl-cyclase enzyme (AC). It also prominently reduced the mechanical hypersensitivity of mice challenged by Forskolin, an AC activator. This effect lasted for up to 48h after Forskolin injection, presenting activity longer than MDL-12330A (AC inhibitor)...
October 12, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
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