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https://www.readbyqxmd.com/read/28926059/br%C3%A3-nsted-acidity-in-deep-eutectic-solvents-and-ionic-liquids
#1
Andrew P Abbott, Sahar S M Alabdullah, Azhar Y M Al-Murshedi, Karl S Ryder
Despite the importance of ionic liquids in a variety of fields, little is understood about the behaviour of protons in these media. The main difficulty arises due to the unknown activity of protons in non-aqueous solvents. This study presents acid dissociation constants for nine organic acids in deep eutectic solvents (DESs) using standard pH indicator solutes. The pKIn value for bromophenol blue was found by titrating the DES with triflic acid. The experimental method was developed to understand the acid-base properties of deep eutectic solvents, and through this study it was found that the organic acids studied were slightly less dissociated in the DES than in water with pKa values between 0...
September 19, 2017: Faraday Discussions
https://www.readbyqxmd.com/read/28924693/phosphodiesterase-4-inhibition-affects-both-the-direct-and-indirect-pathway-an-electrophysiological-study-examining-the-tri-phasic-response-in-the-substantia-nigra-pars-reticulata
#2
P R A Heckman, J V Schweimer, T Sharp, J Prickaerts, A Blokland
Fronto-striatal circuits constitute the neurobiological basis of many neuropsychiatric disorders. Part of the intracellular signaling within these circuits, including its dopaminergic modulation, is regulated by the cyclic adenosine monophosphate (cAMP)/protein kinase A (PKA) signaling cascade. Based on the overall expression in human fronto-striatal circuitry, we tested the effects of a cAMP selective phosphodiesterase 4 (PDE4) inhibitor on the tri-phasic response in the dorsomedial substantia nigra pars reticulata (SNr) upon stimulation of the infralimbic cortex in rats...
September 18, 2017: Brain Structure & Function
https://www.readbyqxmd.com/read/28924458/control-of-nuclear-cytoplasmic-shuttling-of-ankrd54-by-pkc%C3%AE
#3
Amy L Samuels, Alison Louw, Reza Zareie, Evan Ingley
AIM: To identify and characterize the effect of phosphorylation on the subcellular localization of Ankrd54. METHODS: HEK293T cells were treated with calyculin A, staurosporin or phorbol 12-myristate 13-acetate (PMA). Cells were transfected with eGFP-tagged Ankrd54 with or without Lyn tyrosine kinase (wild-type, Y397F mutant, or Y508F mutant). The subcellular localization was assessed by immunofluorescence imaging of cells, immunoblotting of subcellular fractionations...
August 26, 2017: World Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28921568/neuronal-activity-dependent-local-activation-of-dendritic-unfolded-protein-response-promotes-expression-of-brain-derived-neurotrophic-factor-in-cell-soma
#4
Atsushi Saito, Longjie Cai, Koji Matsuhisa, Yosuke Ohtake, Masayuki Kaneko, Soshi Kanemoto, Rie Asada, Kazunori Imaizumi
Unfolded protein response (UPR) has roles not only in resolving the accumulation of unfolded proteins owing to endoplasmic reticulum (ER) stress, but also in regulation of cellular physiological functions. ER stress transducers providing the branches of UPR signaling are known to localize in distal dendritic ER of neurons. These reports suggest that local activation of UPR branches may produce integrated outputs for distant communication, and allow regulation of local events in highly polarized neurons. Here, we demonstrated that synaptic activity- and brain-derived neurotrophic factor (BDNF)-dependent local activation of UPR signaling could be associated with dendritic functions through retrograde signal propagation by using murine neuroblastoma cell line, Neuro-2A and primary cultured hippocampal neurons derived from postnatal day 0 litter C57BL/6 mice...
September 16, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28920604/a-ratiometric-fluorescent-ph-probe-based-on-keto-enol-tautomerization-for-imaging-of-living-cells-in-extreme-acidity
#5
Zong-Xuan Tong, Wei Liu, Hui Huang, Hong-Zong Chen, Xian-Jun Liu, Yong-Qing Kuang, Jian-Hui Jiang
6-(Diethylamino)-2,3-dihydro-1H-xanthene-4-carbaldehyde (DDXC), a reported synthetic intermediate for near-infrared fluorescent dyes, was developed into a fluorescent pH probe for extreme acidity. The unique sensing mechanism of DDXC for pH is based on the reversible protonation of the carbonyl oxygen followed by keto-enol tautomerization. The probe displays a linear ratiometric fluorescence response (I512/I580) to H(+) over the extremely acidic range of pH 2.0-4.0 with a pKa of 3.11, and features high fluorescence quantum yield (Φ = 0...
September 18, 2017: Analyst
https://www.readbyqxmd.com/read/28920464/absorption-sites-of-orally-administered-drugs-in-the-small-intestine
#6
Teruo Murakami
In pharmacotherapy, drugs are mostly taken orally to be absorbed systemically from the small intestine, and some drugs are known to have preferential absorption sites in the small intestine. It would therefore be valuable to know the absorption sites of orally administered drugs and the influencing factors. Areas covered:In this review, the author summarizes the reported absorption sites of orally administered drugs, as well as, influencing factors and experimental techniques. Information on the main absorption sites and influencing factors can help to develop ideal drug delivery systems and more effective pharmacotherapies...
September 17, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28919478/atorvastatin-reduces-lipid-accumulation-in-the-liver-by-activating-protein-kinase-a-mediated-phosphorylation-of-perilipin-5
#7
Xing Gao, Yang Nan, Yuanlin Zhao, Yuan Yuan, Bincheng Ren, Chao Sun, Kaiyu Cao, Ming Yu, Xuyang Feng, Jing Ye
Statins have been proven to be effective in treating non-alcoholic fatty liver disease (NAFLD). Recently, it was reported that statins decreased the hepatic expression of perilipin 5 (Plin5), a lipid droplet (LD)-associated protein, which plays critical roles in regulating lipid accumulation and lipolysis in liver. However, the function and regulation mechanism of Plin5 have not yet been well-established in NAFLD treatment with statins. In this study, we observed that atorvastatin moderately reduced the expression of Plin5 in livers without changing the protein level of Plin5 in the hepatic LD fraction of mice fed with high-fat diet (HFD)...
September 12, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28919123/liraglutide-a-glucagon-like-peptide-1-receptor-agonist-facilitates-osteogenic-proliferation-and-differentiation-in-mc3t3-e1-cells-through-phosphoinositide-3-kinase-pi3k-protein-kinase-b-akt-extracellular-signal-related-kinase-erk-1-2-and-camp-protein-kinase
#8
Xuelun Wu, Shilun Li, Peng Xue, Yukun Li
Previous studies have proven that Glucagon-like peptide-1 (GLP-1) and its receptor agonist exert favorable anabolic effects on skeletal metabolism. However, whether GLP-1could directly impact osteoblast-mediated bone forming is still controversial, and the underlying molecular mechanism remains to be elucidated. Thus in this paper, we investigated the effects of liraglutide, a glucagon-like peptide-1 (GLP-1) receptor agonist, on murine MC3T3-E1 preosteoblasts proliferation and differentiation and explored the potential cellular basis...
September 14, 2017: Experimental Cell Research
https://www.readbyqxmd.com/read/28918839/prostaglandin-e2-induces-prorenin-dependent-activation-of-pro-renin-receptor-and-upregulation-of-cyclooxygenase-2-in-collecting-duct-cells
#9
Nicolás Salinas-Parra, Cristian Reyes-Martínez, Minolfa C Prieto, Alexis A Gonzalez
BACKGROUND: Prostaglandin E2 (PGE2) regulates renin expression in renal juxtaglomerular cells. PGE2 acts through E-prostanoid (EP) receptors in the renal collecting duct (CD) to regulate sodium and water balance. CD cells express EP1 and EP4, which are linked to protein kinase C (PKC) and PKA downstream pathways, respectively. Previous studies showed that the presence of renin in the CD, and that of PKC and PKA pathways, activate its expression. The (pro)renin receptor (PRR) is also expressed in CD cells, and its activation enhances cyclooxygenase-2 (COX-2) through extracellular signal-regulated kinase (ERK)...
September 2017: American Journal of the Medical Sciences
https://www.readbyqxmd.com/read/28918155/the-binding-of-orally-dosed-hydrophobic-active-pharmaceutical-ingredients-to-casein-micelles-in-milk
#10
M Cheema, A N Hristov, F M Harte
Casein proteins (αS1-, αS2-, β- and κ-casein) account for 80% of the total protein content in bovine milk and form casein micelles ( D¯11 = 130 nm, approximately 10(15) micelles/mL). The affinity of native casein micelles with the 3 hydrophobic active pharmaceutical ingredients (API), meloxicam [351.4 g/mol; log P = 3.43; acid dissociation constant (pKa) = 4.08], flunixin (296.2 g/mol; log P = 4.1; pKa = 5.82), and thiabendazole (201.2 g/mol; log P = 2.92; pKa = 4.64), was evaluated in bovine milk collected from dosed Holstein cows...
September 13, 2017: Journal of Dairy Science
https://www.readbyqxmd.com/read/28917975/the-memory-ameliorating-effects-of-dhp1402-an-herbal-mixture-on-cholinergic-blockade-induced-cognitive-dysfunction-in-mice
#11
Haneul Kim, Hyung Eun Lee, In Ho Jung, Se Jin Jeon, Jiabao Zhang, Yubeen Kwon, Dae Sik Jang, Jong Hoon Ryu
ETHNOPHARMACOLOGICAL RELEVANCE: Ziziphus jujuba var. spinosa (Bunge) Hu ex H.F Chow (rhamnaceae) and Codonopsis lanceolata (Siedbold & Zucc.) Benth. & Hook.f. ex Trautv. (campanulaceae), compositions of DHP1402, have long been used for treating anti-dementia or hypomnesia as folk medicine. AIM OF THE STUDY: It has been reported that Z. jujuba var. spinosa and C. lanceolata are effective on cognitive function with different mechanism of action. Therefore, in the present study, we evaluated the synergistic effects of Ziziphus jujuba var...
September 13, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28917800/%C3%AE-cyclodextrins-incorporated-multi-walled-carbon-nanotubes-modified-electrode-for-the-voltammetric-determination-of-the-pesticide-dichlorophen
#12
Karolina Sipa, Mariola Brycht, Andrzej Leniart, Paweł Urbaniak, Agnieszka Nosal-Wiercińska, Bartłomiej Pałecz, Sławomira Skrzypek
In this work, a glassy carbon electrode modified with β-cyclodextrins and multi-walled carbon nanotubes (β-CDs/MWCNTs/GCE) was constructed and applied for the square-wave adsorptive stripping voltammetric (SWAdSV) determination of the pesticide dichlorophen (Dcp). For the first time, this compound was electrochemically investigated. The voltammetric measurements were conducted in phosphate buffer (PBS) at pH 6.5 as a supporting electrolyte, and SWAdSV technique parameters were optimized. A linear calibration curve in the wide concentration range from 5...
January 1, 2018: Talanta
https://www.readbyqxmd.com/read/28917447/cell-penetrating-peptides-to-dissect-host-pathogen-protein-protein-interactions-in-theileria-transformed-leukocytes
#13
REVIEW
Malak Haidar, Perle Latré de Laté, Eileen J Kennedy, Gordon Langsley
One powerful application of cell penetrating peptides is the delivery into cells of molecules that function as specific competitors or inhibitors of protein-protein interactions. Ablating defined protein-protein interactions is a refined way to explore their contribution to a particular cellular phenotype in a given disease context. Cell-penetrating peptides can be synthetically constrained through various chemical modifications that stabilize a given structural fold with the potential to improve competitive binding to specific targets...
September 7, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28917150/efficient-delivery-of-signal-responsive-gene-carriers-for-disease-specific-gene-expression-via-bubble-liposomes-and-sonoporation
#14
Akira Tsuchiya, Jeong-Hun Kang, Takeshi Mori, Yuki Naritomi, Satoshi Kushio, Takuro Niidome, Katsuro Tachibana, Yoko Takahashi, Yoichi Negishi, Yusuke Oda, Ryo Suzuki, Kazuo Maruyama, Yoshiki Katayama
Sonoporation is a promising method to intracellularly deliver synthetic gene carriers that have lower endocytotic uptake than viral carriers. Here, we applied sonoporation to deliver genes via polyethylene glycol (PEG)-grafted polymeric carriers that specifically respond to hyperactivated protein kinase A (PKA). PEG-grafted polymeric carrier/DNA polyplexes were not efficiently delivered into cells via the endocytotic pathway because of the hydrophilic PEG layer surrounding the polyplexes. However, the delivery of polyplexes into cells was significantly increased by sonoporation...
September 9, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28917116/thermal-and-photo-induced-degradation-of-perfluorinated-carboxylic-acids-kinetics-and-mechanism
#15
Jiaoqin Liu, Ruijuan Qu, Zunyao Wang, Itza Mendoza-Sanchez, Virender K Sharma
Perfluorinated carboxylic acids (PFCAs) of different carbon chain lengths are chemicals of concern to human health and their removal, using conventional remediation technologies, is challenging. The present paper pursuits thermal and photo-induced degradation of PFCAs (F(CF2)nCOOH, n = 1-9) under various concentrations of four different acids (HNO3, H2SO4, HCl, and H3PO4) covering a range of strong acidic to basic pH. For thermal-induced experiments, the temperature was set at 40 °C, 60 °C, and 80 °C at acid strengths of 0...
September 6, 2017: Water Research
https://www.readbyqxmd.com/read/28916831/the-melanocortin-signaling-camp-axis-accelerates-repair-and-reduces-mutagenesis-of-platinum-induced-dna-damage
#16
Stuart G Jarrett, Katharine M Carter, Brent J Shelton, John A D'Orazio
Using primary melanocytes and HEK293 cells, we found that cAMP signaling accelerates repair of bi- and mono-functional platinum-induced DNA damage. Elevating cAMP signaling either by the agonistic MC1R ligand melanocyte stimulating hormone (MSH) or by pharmacologic cAMP induction by forskolin enhanced clearance of intrastrand cisplatin-adducts in melanocytes or MC1R-transfected HEK293 cells. MC1R antagonists human beta-defensin 3 and agouti signaling protein blocked MSH- but not forskolin-mediated enhancement of platinum-induced DNA damage...
September 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28916818/identification-of-4-phenylquinolin-2-1h-one-as-a-specific-allosteric-inhibitor-of-akt
#17
Bill X Huang, Kenny Newcomer, Karl Kevala, Elena Barnaeva, Wei Zheng, Xin Hu, Samarjit Patnaik, Noel Southall, Juan Marugan, Marc Ferrer, Hee-Yong Kim
Akt plays a major role in tumorigenesis and the development of specific Akt inhibitors as effective cancer therapeutics has been challenging. Here, we report the identification of a highly specific allosteric inhibitor of Akt through a FRET-based high-throughput screening, and characterization of its inhibitory mechanism. Out of 373,868 compounds screened, 4-phenylquinolin-2(1H)-one specifically decreased Akt phosphorylation at both T308 and S473, and inhibited Akt kinase activity (IC50 = 6 µM) and downstream signaling...
September 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28915043/proton-network-flexibility-enables-robustness-and-large-electric-fields-in-the-ketosteroid-isomerase-active-site
#18
Lu Wang, Stephen D Fried, Thomas E Markland
Hydrogen bond networks play vital roles in biological functions ranging from protein folding to enzyme catalysis. Here we combine electronic structure calculations and ab initio path integral molecular dynamics simulations, which incorporate both nuclear and electronic quantum effects, to show why the network of short hydrogen bonds in the active site of ketosteroid isomerase is remarkably robust to mutations along the network and how this gives rise to large local electric fields. We demonstrate that these properties arise from the network's ability to respond to a perturbation by shifting proton positions and redistributing electronic charge density...
September 15, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28915030/radical-enhanced-acidity-why-bicarbonate-carboxyl-hydroperoxyl-and-related-radicals-are-so-acidic
#19
John C Walton
Comparison of accepted pKa values of bicarbonate, carboxyl and hydroperoxyl radicals, with those of models having the unpaired electron replaced by H-atoms, implied the acidity of the radicals was greatly increased. A DFT computational method of estimating pKas was developed and applied to a set of radicals designed to probe the phenomenon of Radical-Enhanced Deprotonation (RED-shift) and its underlying causes. Comparison of the computed pKa values of twelve acid radicals to those of the corresponding model acids confirmed the intensified acidity of the title radicals and also pin-pointed the carboxy-ethynyl (HO2CCC•) and the carboxy-aminyl (HO2CNH•) radicals as having enhanced acidity...
September 15, 2017: Journal of Physical Chemistry. A
https://www.readbyqxmd.com/read/28912160/dopamine-d2-receptors-modulate-pyramidal-neurons-in-mouse-medial-prefrontal-cortex-through-a-stimulatory-g-protein-pathway
#20
Sarah E Robinson, Vikaas S Sohal
Dopaminergic modulation of prefrontal cortex is believed to play key roles in many cognitive functions and to be disrupted in pathological conditions such as schizophrenia. We have previously described a phenomenon whereby dopamine D2 receptor (D2R) activation elicits afterdepolarizations (ADPs) in subcortically-projecting (SC) pyramidal neurons within L5 of the prefrontal cortex. These D2R-induced ADPs only occur following synaptic input which activates NMDA receptors (NMDARs) even when the delay between the synaptic input and afterdepolarizations is relatively long, e...
September 14, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
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