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chloride channel activators

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https://www.readbyqxmd.com/read/27932986/role-of-quercetin-in-modulating-chloride-transport-in-the-intestine
#1
Bo Yu, Yu Jiang, Lingling Jin, Tonghui Ma, Hong Yang
Epithelial chloride channels provide the pathways for fluid secretion in the intestine. Cystic fibrosis transmembrane conductance regulator (CFTR) and calcium-activated chloride channels (CaCCs) are the main chloride channels in the luminal membrane of enterocytes. These transmembrane proteins play important roles in many physiological processes. In this study, we have identified a flavonoid quercetin as a modulator of CaCC chloride channel activity. Fluorescence quenching assay showed that quercetin activated Cl(-) transport in a dose-dependent manner, with EC50 ~37 μM...
2016: Frontiers in Physiology
https://www.readbyqxmd.com/read/27927103/mechanism-of-action-of-relaxant-effect-of-agastache-mexicana-ssp-mexicana-essential-oil-in-guinea-pig-trachea-smooth-muscle
#2
Andrés Navarrete, Natalia Ávila-Rosas, Mateo Majín-León, José Luis Balderas-López, Alejandro Alfaro-Romero, José Carlos Tavares-Carvalho
CONTEXT: Agastache mexicana ssp. mexicana (Kunth) Lint & Epling (Lamiaceae), popularly known as 'toronjil morado', is used in Mexican traditional medicine for the treatment of several diseases such as hypertension, anxiety and respiratory disorders. OBJECTIVE: This study investigates the relaxant action mechanism of A. mexicana ssp. mexicana essential oil (AMEO) in guinea-pig isolated trachea model. MATERIALS AND METHOD: AMEO was analyzed by GC/MS...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/27921211/helix-o-modulates-voltage-dependency-of-clc-1
#3
Ju Yong Seong, Kotdaji Ha, Chansik Hong, Jongyun Myeong, Hyun-Ho Lim, Dongki Yang, Insuk So
The chloride channel (CLC) family of proteins consists of channels and transporters that share similarities in architecture and play essential roles in physiological functions. Among the CLC family, CLC-1 channels have the representative homodimeric double-barreled structure carrying two gating processes. One is protopore gating that acts on each pore independently by glutamate residue (Eext). The other is common gating that closes both pores simultaneously in association with large conformational changes across each subunit...
December 5, 2016: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/27917283/protective-effects-of-nimodipine-and-lithium-against-aluminum-induced-cell-death-and-oxidative-stress-in-pc12-cells
#4
Jamileh Saberzadeh, Mehdi Omrani, Mohammad Ali Takhshid
OBJECTIVES: The role of aluminum (Al) in the pathogenesis of neurodegenerative diseases has been implicated in several studies. However, the exact mechanisms of cytotoxic effects of Al have not been elucidated yet. The aim of this study was to investigate the effect of L-type calcium channel antagonist, nimodipine (NM), and lithium chloride (LiCl) on Al-induced toxicity in PC12 cells. MATERIALS AND METHODS: PC12 cells were treated with Al-maltolate (Almal) in the presence and absence of different concentrations of NM (50-150 μm) and/or LiCl (0...
November 2016: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/27913277/specific-stabilization-of-cftr-by-phosphatidylserine
#5
Ellen Hildebrandt, Netaly Khazanov, John C Kappes, Qun Dai, Hanoch Senderowitz, Ina L Urbatsch
The Cystic Fibrosis Transmembrane Conductance Regulator (CFTR, ABCC7) is a plasma membrane chloride ion channel in the ABC transporter superfamily. CFTR is a key target for cystic fibrosis drug development, and its structural elucidation would advance those efforts. However, the limited in vivo and in vitro stability of the protein, particularly its nucleotide binding domains, has made structural studies challenging. Here we demonstrate that phosphatidylserine uniquely stimulates and thermally stabilizes the ATP hydrolysis function of purified human CFTR...
November 29, 2016: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/27895116/correctors-and-potentiators-rescue-function-of-the-truncated-w1282x-cftr-translation-product
#6
Peter M Haggie, Puay-Wah Phuan, Joseph-Anthony Tan, Haijin Xu, Radu G Avramescu, Doranda Perdomo, Lorna Zlock, Dennis W Nielson, Walter E Finkbeiner, Gergely L Lukacs, Alan S Verkman
W1282X is the fifth most common CFTR mutation that causes cystic fibrosis. Here, we investigated the utility of a small molecule corrector / potentiator strategy, as used for ΔF508-CFTR, to produce functional rescue of the truncated translation product of the W1282X mutation, CFTR1281, without the need for read-through. In transfected cell systems, certain potentiators and correctors including VX-809 and VX-770 increased CFTR1281 activity. To identify novel correctors and potentiators with potentially greater efficacy on CFTR1281, functional screens were done of ~30,000 synthetic small molecules and drugs/nutraceuticals in CFTR1281-transfected cells...
November 28, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27888566/functional-expression-of-g-protein-coupled-receptor-30-in-immature-rat-epididymal-epithelium
#7
Xiaonian Cao, Jiehong Huang, Geng Zhang, Wulin Zuo, Chongfeng Lan, Qing Sun, Dengliang Yang, Dongdong Gao, Christopher H K Cheng, Wen-Liang Zhou
The aim of this study is to investigate the functional role of G protein-coupled receptor 30 (GPR30) in the epididymis. We found that GPR30 is expressed in the epithelium of the immature rat epididymis and is involved in chloride secretion into the caudal epididymis lumen. The short-circuit current (Isc) experiments showed that in primary cultured caudal epididymis epithelium, activation of GPR30 by its specific agonist G1 induced a mono-phasic current increase, and G15, the specific antagonist of GPR30, could completely inhibit the current induced by G1...
November 26, 2016: Cell Biology International
https://www.readbyqxmd.com/read/27881775/a-biophysical-model-for-cytotoxic-cell-swelling
#8
Koen Dijkstra, Jeannette Hofmeijer, Stephan A van Gils, Michel J A M van Putten
: We present a dynamic biophysical model to explain neuronal swelling underlying cytotoxic edema in conditions of low energy supply, as observed in cerebral ischemia. Our model contains Hodgkin-Huxley-type ion currents, a recently discovered voltage-gated chloride flux through the ion exchanger SLC26A11, active KCC2-mediated chloride extrusion, and ATP-dependent pumps. The model predicts changes in ion gradients and cell swelling during ischemia of various severity or channel blockage with realistic timescales...
November 23, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/27871896/gastroprotective-and-ulcer-healing-effects-of-hydroethanolic-extract-of-leaves-of-caryocar-coriaceum-mechanisms-involved-in-the-gastroprotective-activity
#9
Luis Jardelino de Lacerda Neto, Andreza Guedes Barbosa Ramos, Valterlucio Santos Sales, Severino Denicio Gonçalves de Souza, Antonia Thassya Lucas Dos Santos, Larissa Rolim de Oliveira, Marta Regina Kerntopf, Thais Rodrigues de Albuquerque, Henrique Douglas Melo Coutinho, Lucindo Jose Quintans-Júnior, Almir Gonçalves Wanderley, Irwin Rose Alencar de Menezes
This work aimed to determine the chemical fingerprint of hydroethanolic extract of leaves of Caryocar coriaceum (HELCC) and the gastroprotective activity. The chemical fingerprint of HELCC was analyzed by HPLC-DAD, to quantify total phenols and flavonoids were carried out by Folin-Ciocalteu reagent and aluminum chloride assay, while in vitro antioxidant activity was evaluated by the DPPH method. The methods used to determine pharmacological activity were: gastroprotective screening test in classical models of induced acute and chronic gastric lesions and physical barrier test...
November 18, 2016: Chemico-biological Interactions
https://www.readbyqxmd.com/read/27871064/benzopyrimido-pyrrolo-oxazine-dione-cftr-inhibitor-r-bpo-27-for-anti-secretory-therapy-of-diarrheas-caused-by-bacterial-enterotoxins
#10
Onur Cil, Puay-Wah Phuan, Anne Marie Gillespie, Sujin Lee, Lukmanee Tradtrantip, Jianyi Yin, Ming Tse, Nicholas C Zachos, Ruxian Lin, Mark Donowitz, Alan S Verkman
Secretory diarrheas caused by bacterial enterotoxins, including cholera and traveler's diarrhea, remain a major global health problem. Inappropriate activation of the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel occurs in these diarrheas. We previously reported that the benzopyrimido-pyrrolo-oxazinedione (R)-BPO-27 inhibits CFTR chloride conductance with low-nanomolar potency. Here, we demonstrate using experimental mouse models and human enterocyte cultures the potential utility of (R)-BPO-27 for treatment of secretory diarrheas caused by cholera and Escherichia coli enterotoxins...
November 8, 2016: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/27866192/dietary-genistein-rescues-reduced-basal-chloride-secretion-in-diabetic-jejunum-via-sex-dependent-mechanisms
#11
Shawn Catmull, Faisal Masood, Sydney Schacht, Robert Dolan, Daniel Stegman, Lana Leung, Layla Al-Nakkash
BACKGROUND/AIMS: The goal of this study was to determine the effect of dietary genistein (naturally occurring phytoestrogen) on jejunal secretory function in a clinically relevant model of diabetes and obesity, the leptin-defIcient ob/ob mouse. METHODS: We measured transepithelial short circuit current (Isc), across freshly isolated segments of jejunum from 12-week old male and female ob/ob and lean C57Bl/6J mice fed a genistein diet (600 mg genistein/kg diet) for 4-weeks...
2016: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/27861612/clic1-inhibition-attenuates-vascular-inflammation-oxidative-stress-and-endothelial-injury
#12
Yingling Xu, Ji Zhu, Xiao Hu, Cui Wang, Dezhao Lu, Chenxue Gong, Jinhuan Yang, Lei Zong
Endothelial dysfunction, which includes endothelial oxidative damage and vascular inflammation, is a key initiating step in the pathogenesis of atherosclerosis (AS) and an independent risk factor for this disorder. Intracellular chloride channel 1 (CLIC1), a novel metamorphic protein, acts as a sensor of cell oxidation and is involved in inflammation. In this study, we hypothesize that CLIC1 plays an important role in AS. Apolipoprotein E-deficient mice were supplied with a normal diet or a high-fat and high-cholesterol diet for 8 weeks...
2016: PloS One
https://www.readbyqxmd.com/read/27860832/anoctamins-tmem16-proteins-chloride-channels-flirting-with-lipids-and-extracellular-vesicles
#13
Jarred M Whitlock, H Criss Hartzell
Anoctamin/TMEM16 proteins exhibit diverse functions in cells throughout the body and are implicated in several human diseases. Although the founding members ANO1 (TMEM16A) and ANO2 (TMEM16B) are Ca(2+)-activated Cl(-) channels, most ANO paralogs are Ca(2+)-dependent phospholipid scramblases that serve as channels facilitating the movement (scrambling) of phospholipids between leaflets of the membrane bilayer. Phospholipid scrambling significantly alters the physical properties of the membrane and its landscape and has vast downstream signaling consequences...
November 16, 2016: Annual Review of Physiology
https://www.readbyqxmd.com/read/27859594/glutamate-transporter-associated-anion-channels-adjust-intracellular-chloride-concentrations-during-glial-maturation
#14
Verena Untiet, Peter Kovermann, Niklas J Gerkau, Thomas Gensch, Christine R Rose, Christoph Fahlke
Astrocytic volume regulation and neurotransmitter uptake are critically dependent on the intracellular anion concentration, but little is known about the mechanisms controlling internal anion homeostasis in these cells. Here we used fluorescence lifetime imaging microscopy (FLIM) with the chloride-sensitive dye MQAE to measure intracellular chloride concentrations in murine Bergmann glial cells in acute cerebellar slices. We found Bergmann glial [Cl(-) ]int to be controlled by two opposing transport processes: chloride is actively accumulated by the Na(+) -K(+) -2Cl(-) cotransporter NKCC1, and chloride efflux through anion channels associated with excitatory amino acid transporters (EAATs) reduces [Cl(-) ]int to values that vary upon changes in expression levels or activity of these channels...
November 18, 2016: Glia
https://www.readbyqxmd.com/read/27859335/extracellular-protons-enable-activation-of-the-calcium-dependent-chloride-channel-tmem16a-ano1
#15
Silvia Cruz-Rangel, José J De Jesus-Pérez, Iván A Aréchiga-Figueroa, Aldo A Rodríguez-Menchaca, Patricia Pérez-Cornejo, H Criss Hartzell, Jorge Arreola
TMEM16A (ANO1), the pore forming subunit of a Ca(2+) -dependent Cl(-) channel (CaCC), is activated by direct, voltage-dependent, binding of intracellular Ca(2+) . Endogenous CaCCs are regulated by extracellular protons; however, the molecular basis of such regulation remains unidentified. Here, we evaluated the effects of different extracellular proton concentrations ([H(+) ]o ) on mouse TMEM16A expressed in HEK-293 cells using whole-cell and inside-out patch clamp recordings. We found that increasing the [H(+) ]o from 10(-10) to 10(-5...
November 17, 2016: Journal of Physiology
https://www.readbyqxmd.com/read/27853135/cl-out-is-a-novel-cooperative-optogenetic-tool-for-extruding-chloride-from-neurons
#16
Hannah Alfonsa, Jeremy H Lakey, Robert N Lightowlers, Andrew J Trevelyan
Chloride regulation affects brain function in many ways, for instance, by dictating the GABAergic reversal potential, and thereby influencing neuronal excitability and spike timing. Consistent with this, there is increasing evidence implicating chloride in a range of neurological conditions. Investigations about these conditions, though, are made difficult by the limited range of tools available to manipulate chloride levels. In particular, there has been no way to actively remove chloride from neurons; we now describe an optogenetic strategy, 'Cl-out', to do exactly this...
November 17, 2016: Nature Communications
https://www.readbyqxmd.com/read/27852936/the-vasorelaxant-mechanisms-of-methanol-on-isolated-rat-aortic-rings-involvement-of-ion-channels-and-signal-transduction-pathways
#17
Y Bai, Q Zhang, Z Yang, Z Meng, Q Zhao
It is reported that methanol is generally used as an industrial solvent, antifreeze, windshield washer fluid, cooking fuel and perfume. Methanol ingestion can lead to severe metabolic disturbances, blindness, or even death. So far, few studies about its negative effects on cardiovascular system have been reported. The purpose of this study was to determine the vasoactive effect of methanol and roles of ion channels and signal transduction pathways on isolated rat aorta. The results suggested that the mechanism of methanol-induced vasorelaxation at low concentrations (<500 mM) was mediated by ATP-sensitive K(+) (KATP) and L-type Ca(2+) channels, but the mechanism at high concentrations (>600 mM) was related to KATP, voltage-dependent K(+), big-conductance Ca(2+)-activated K(+), L-type Ca(2+) channels as well as prostacyclin, protein kinase C, β-adrenoceptors pathways...
November 16, 2016: Human & Experimental Toxicology
https://www.readbyqxmd.com/read/27849367/fetal-exposure-to-low-levels-of-the-plasticizer-dehp-predisposes-the-adult-male-adrenal-gland-for-endocrine-disruption
#18
S Lee, D B Martinez-Arguelles, E Campioli, V Papadopoulos
In utero exposure to endocrine disrupting chemicals (EDCs) may affect adult health. Di-(2-ethylhexyl) phthalate (DEHP) is an EDC widely used in the production of polyvinyl chloride products and an ubiquitous environmental contaminant. Previously, we used a rat model system to show that fetal exposure to DEHP decreased levels of major steroid hormones in adulthood and that environmentally-relevant levels of DEHP affected both gene expression and epigenomic loci that were affected by exposure to high levels. In the adrenal gland, we reported that the peroxisome proliferator-activated receptor (PPAR) and cholesterol biosynthesis pathways were sensitive targets of DEHP...
November 16, 2016: Endocrinology
https://www.readbyqxmd.com/read/27844056/hyperpolarization-activated-currents-and-subthreshold-resonance-in-granule-cells-of-the-olfactory-bulb
#19
Ruilong Hu, Katie A Ferguson, Christina B Whiteus, Dimphna H Meijer, Ricardo C Araneda
An important contribution to neural circuit oscillatory dynamics is the ongoing activation and inactivation of hyperpolarization-activated currents (Ih). Network synchrony dynamics play an important role in the initial processing of odor signals by the main olfactory bulb (MOB) and accessory olfactory bulb (AOB). In the mouse olfactory bulb, we show that Ih is present in granule cells (GCs), the most prominent inhibitory neuron in the olfactory bulb, and that Ih underlies subthreshold resonance in GCs. In accord with the properties of Ih, the currents exhibited sensitivity to changes in extracellular K(+) concentration and ZD7288 (4-ethylphenylamino-1,2-dimethyl-6-methylaminopyrimidin chloride), a blocker of Ih...
September 2016: ENeuro
https://www.readbyqxmd.com/read/27835719/adjunctive-taurine-in-first-episode-psychosis-a-phase-2-double-blind-randomized-placebo-controlled-study
#20
Colin P O'Donnell, Kelly A Allott, Brendan P Murphy, Hok Pan Yuen, Tina-Marie Proffitt, Alicia Papas, Jennifer Moral, Tee Pham, Michaela K O'Regan, Christina Phassouliotis, Raelene Simpson, Patrick D McGorry
OBJECTIVE: Taurine is an inhibitory neuromodulatory amino acid in the central nervous system that activates the GABA- and glycine-insensitive chloride channel and inhibits the N-methyl-d-aspartate receptor. It also functions as a neuroprotective agent and has a role in neural development and neurogenesis. The aim of this study was to determine the efficacy of adjunctive taurine in improving symptomatology and cognition among patients with a DSM-IV first-episode psychotic disorder. METHODS: 121 patients with first-episode psychosis, aged 18-25 years, attending early intervention services consented to participate in this randomized, double-blind, placebo-controlled trial conducted from January 2007 to May 2009...
November 8, 2016: Journal of Clinical Psychiatry
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