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https://www.readbyqxmd.com/read/29353375/comparative-effects-of-hydrogen-sulfide-releasing-compounds-on-3h-d-aspartate-release-from-bovine-isolated-retinae
#1
Pratik Bankhele, Ankita Salvi, Jamal Jamil, Fatou Njie-Mbye, Sunny Ohia, Catherine A Opere
We investigated the pharmacological actions of a slow-releasing H2S donor, GYY 4137; a substrate for the biosynthesis of H2S, L-cysteine and its precursor, N-acetylcysteine on potassium (K+; 50 mM)-evoked [3H]D-aspartate release from bovine isolated retinae using the Superfusion Method. GYY 4137 (10 nM-10 µM), L-cysteine (100 nM-10 µM) and N-acetylcysteine (10 µM-1 mM) elicited a concentration-dependent decrease in K+-evoked [3H]D-aspartate release from isolated bovine retinae without affecting basal tritium efflux...
January 20, 2018: Neurochemical Research
https://www.readbyqxmd.com/read/29353349/daclatasvir-a-review-of-preclinical-and-clinical-pharmacokinetics
#2
REVIEW
Yash Gandhi, Timothy Eley, Aberra Fura, Wenying Li, Richard J Bertz, Tushar Garimella
Daclatasvir is a first-in-class, highly selective, hepatitis C virus, non-structural protein 5a polymerase replication complex inhibitor with picomolar potency and broad genotypic coverage in vitro. Daclatasvir undergoes rapid absorption, with a time to reach maximum plasma concentration of 1-2 h and an elimination half-life of ~ 10 to 14 h observed in single-ascending dose studies. Steady state was achieved by day 4 in multiple-ascending dose studies. Daclatasvir can be administered without regard to food or pH modifiers...
January 20, 2018: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/29353319/management-strategies-for-noncardiac-surgery-following-a-coronary-artery-event
#3
REVIEW
Thomas F Whayne, Sibu P Saha
PURPOSE OF REVIEW: Coronary artery event includes acute coronary syndrome (ACS), percutaneous coronary intervention (PCI), and coronary artery bypass graft (CABG) surgery. Following such an event, risk of noncardiac surgery is increased. Of major concern is what can make this surgery safer? RECENT FINDINGS: High functional capacity improves cardiovascular (CV) risk; at least 4.0 metabolic equivalents (METs) on stress test are favorable. Risk scores can suggest need for further evaluation...
January 20, 2018: Current Cardiology Reports
https://www.readbyqxmd.com/read/29353189/synthesis-of-cross-linked-protein-metal-hybrid-nanoflowers-and-its-application-in-repeated-batch-decolorization-of-synthetic-dyes
#4
Sanjay K S Patel, Sachin V Otari, Jinglin Li, Dong Rip Kim, Sun Chang Kim, Byung-Kwan Cho, Vipin C Kalia, Yun Chan Kang, Jung-Kul Lee
Herein, we report the preparation of a cross-linked protein-metal hybrid nanoflower (NF) system for laccase immobilization. The immobilized laccase showed effective encapsulation yield and activity recovery of 78.1% and 204%, respectively. The catalytic efficiency (kcatVmax-1) of cross-linked NF (CL-NF) was 2.2-fold more than that of free laccase. The CL-NF also exhibited significantly higher stability towards pH and temperature changes. It exhibited excellent storage stability and tolerance towards solvents and inhibitors as compared with the free enzyme...
January 4, 2018: Journal of Hazardous Materials
https://www.readbyqxmd.com/read/29353037/curcumin-protects-cortical-neurons-against-oxygen-and-glucose-deprivation-reoxygenation-injury-through-flotillin-1-and-extracellular-signal-regulated-kinase1-2-pathway
#5
Zhengyu Lu, Yanping Liu, Yang Shi, Xinjie Shi, Xin Wang, Chuan Xu, Hong Zhao, Qiang Dong
In this study, we provided evidence that curcumin could be a promising therapeutic agent for ischemic stroke by activating neuroprotective signaling pathways. Post oxygen and glucose deprivation/reoxygenation (OGD/R), primary mouse cortical neurons treated with curcumin exhibited a significant decrease in cell death, LDH release and enzyme caspase-3 activity under OGD/R circumstances, which were abolished by flotillin-1 downregulation or extracellular signal-regulated kinase (ERK) inhibitor. Moreover, flotillin-1 knockdown led to suppression of curcumin-mediated ERK phosphorylation under OGD/R condition...
January 15, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29352819/dietary-fibre-intake-in-relation-to-the-risk-of-incident-chronic-kidney-disease
#6
Parvin Mirmiran, Emad Yuzbashian, Golaleh Asghari, Shaghayegh Sarverzadeh, Fereidoun Azizi
The purpose of this study was primarily to evaluate the association of total fibre intake with the risk of incident chronic kidney disease (CKD). We also evaluated the association of dietary fibre from fruits, vegetables, cereals and legumes with the incidence of CKD in a population-based prospective study. We followed up 1630 participants of the Tehran Lipid and Glucose Study for 6·1 years, who were initially free of CKD. Baseline diet was assessed by a valid and reliable FFQ. Estimated glomerular filtration rate (eGFR) was calculated, using the Modification of Diet in Renal Disease Study equation, and CKD was defined as eGFR <60 ml/min per 1·73 m2...
January 21, 2018: British Journal of Nutrition
https://www.readbyqxmd.com/read/29352755/a-mos1-transposase-in-vivo-assay-to-screen-new-hiv-1-integrase-inhibitors
#7
Mariana Cancian, Elgion L S Loreto
The integrase and transposase enzymes of retrovirus and transposons, respectively, share the catalytic DDE domain. In vitro assays showed that inhibitors of HIV-1 integrase generally inhibit the mariner Mos1 transposase. Using a Drosophila strain in which the mobilisation of the mariner element can be quantified by mosaic eyes, we showed that flies maintained in medium containing 210 µM to 4 mM of raltegravir, or 1 or 2 mM of dolutegravir, which are HIV-1 integrase inhibitor used in AIDS treatment, have 23-33% less somatic mobilisation in mosaic eyes when treated with raltegravir and 28-32% when treated with dolutegravir...
January 19, 2018: Genetica
https://www.readbyqxmd.com/read/29352744/crystal-structure-of-adp-dependent-glucokinase-from-methanocaldococcus-jannaschii-in-complex-with-5-iodotubercidin-reveals-phosphoryl-transfer-mechanism
#8
Piotr Tokarz, Magdalena Wiśniewska, Marcin M Kamiński, Grzegorz Dubin, Przemysław Grudnik
ADP-dependent glucokinase (ADPGK) is an alternative novel glucose phosphorylating enzyme in a modified glycolysis pathway of hyperthermophilic Archaea. In contrast to classical ATP-dependent hexokinases, ADPGK utilizes ADP as a phosphoryl group donor. Here we present a crystal structure of archaeal ADPGK from Methanocaldococcus jannaschii in complex with an inhibitor, 5-iodotubercidin, D-glucose, inorganic phosphate and a magnesium ion. Detailed analysis of the architecture of the active site allowed for confirmation of the previously proposed phosphorylation mechanism and the crucial role of the invariant arginine residue (Arg197)...
January 20, 2018: Protein Science: a Publication of the Protein Society
https://www.readbyqxmd.com/read/29352168/epigenetic-control-of-influenza-virus-role-of-h3k79-methylation-in-interferon-induced-antiviral-response
#9
Laura Marcos-Villar, Juan Díaz-Colunga, Juan Sandoval, Noelia Zamarreño, Sara Landeras-Bueno, Manel Esteller, Ana Falcón, Amelia Nieto
Influenza virus stablishes a network of virus-host functional interactions, which depends on chromatin dynamic and therefore on epigenetic modifications. Using an unbiased search, we analyzed the epigenetic changes at DNA methylation and post-translational histone modification levels induced by the infection. DNA methylation was unaltered, while we found a general decrease on histone acetylation, which correlates with transcriptional inactivation and may cooperate with the impairment of cellular transcription that causes influenza virus infection...
January 19, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29352107/mycolyltransferase-from-mycobacterium-tuberculosis-in-covalent-complex-with-tetrahydrolipstatin-provides-insights-into-antigen-85-catalysis
#10
Christopher M Goins, Steven Dajnowicz, Micholas D Smith, Jerry M Parks, Donald R Ronning
Mycobacterium tuberculosis Antigen 85 enzymes (Ag85s) catalyze the transfer of mycolic acid (MA) from trehalose monomycolate to produce the mycolyl arabinogalactan (mAG) or trehalose dimycolate (TDM). These lipids define the protective mycomembrane of Mycobacteria. The current model of substrate binding within the active sites of Ag85s for the production of TDM is not sterically and geometrically feasible; additionally, this model does not account for the production of mAG. Furthermore, this model does not address how Ag85s limit the hydrolysis of the acyl-enzyme intermediate while catalyzing acyl transfer...
January 19, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29352103/dynamic-cycling-of-t-snare-acylation-regulates-platelet-exocytosis
#11
Jinchao Zhang, Yunjie Huang, Jing Chen, Haining Zhu, Sidney W Whiteheart
Platelets regulate vascular integrity by secreting a host of molecules that promote hemostasis and its sequelae. Given the importance of platelet exocytosis, it is critical to understand how it is controlled. The t-SNAREs, SNAP-23 and syntaxin-11, lack classical transmembrane domains (TMDs), yet both are associated with platelet membranes and redistributed into cholesterol-dependent, lipid rafts when platelets were activated. Using metabolic labeling and hydroxylamine/HCl (HA) treatment, we showed that both contain thioester-linked acyl groups...
January 19, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29352069/identification-of-ketene-reactive-intermediate-of-erlotinib-possibly-responsible-for-inactivation-of-p450-enzymes
#12
Huimin Zhao, Siyuan Li, Zixin Yang, Ying Peng, Xiaohui Chen, Jiang Zheng
Erlotinib (ELT), a tyrosine kinase inhibitor, is widely used for the treatment of non-small-cell lung cancer in clinic. Unfortunately, severe drug-induced liver injury and other adverse effects occurred during the treatment. Meanwhile, ELT has been reported to be a mechanism-based inactivator of CYPs 3A4 and 3A5. The objectives of this study were to identify ketene intermediate of ELT and investigate the association of the acetylenic bioactivation with the enzyme inactivation caused by ELT. A ketene intermediate was detected in human microsomal incubations of ELT, using 4-bromobenzylamine as a trapping agent...
January 19, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29351747/combination-of-pelargonium-sidoides-and-coptis-chinensis-root-inhibits-nuclear-factor-kappa-b-mediated-inflammatory-response-in-vitro-and-in-vivo
#13
Sang Mi Park, Byung-Gu Min, Ji Yun Jung, Kyung Hwan Jegal, Chul Won Lee, Kwang Youn Kim, Young Woo Kim, Youn-Woong Choi, Il Je Cho, Sae Kwang Ku, Sang Chan Kim
BACKGROUND: Pelargonium sidoides (PS) and Coptis chinensis root (CR) have traditionally been used to treat various diseases, including respiratory and gastrointestinal infections, dysmenorrhea, and hepatic disorders. The present study was conducted to evaluate the anti-inflammatory effects of a combination of PS and CR in vitro and in vivo. METHODS: The in vitro effects of PS + CR on the induction of inflammation-related proteins were evaluated in lipopolysaccharide (LPS)-stimulated RAW 264...
January 19, 2018: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/29351724/the-role-of-extracellular-matrix-components-in-angiogenesis-and-fibrosis-possible-implication-for-systemic-sclerosis
#14
Vasiliki Liakouli, Paola Cipriani, Paola Di Benedetto, Piero Ruscitti, Francesco Carubbi, Onorina Berardicurti, Noemi Panzera, Roberto Giacomelli
Extracellular matrix (ECM) plays a crucial role in the regulation of both physiological and pathological angiogenesis. ECM homeostasis and function is ensuring by the tightly regulation of the different ECM components including, collagens, proteoglycans and a variety of different glycoproteins. An altered expression of the above ECM molecules as well as an imbalance between the action of matrix remodeling enzymes and their tissue inhibitors is known to be responsible for impaired angiogenesis and fibrosis. Systemic Sclerosis (SSc) is an autoimmune disease characterized by micro-angiopathy, failure of reparative angiogenesis and excessive fibrosis of the skin and various internal organs, dues to an increased production of ECM...
January 19, 2018: Modern Rheumatology
https://www.readbyqxmd.com/read/29351216/in-silico-and-in-vitro-study-of-the-bromelain-phytochemical-complex-inhibition-of-phospholipase-a2-pla2
#15
Fatahiya Mohamed Tap, Fadzilah Adibah Abd Majid, Hassan Fahmi Ismail, Tet Soon Wong, Kamyar Shameli, Mikio Miyake, Nurul Bahiyah Ahmad Khairudin
Phospholipase A2 (Pla2) is an enzyme that induces inflammation, making Pla2 activity an effective approach to reduce inflammation. Therefore, investigating natural compounds for this Pla2 inhibitory activity has important therapeutic potential. The objective of this study was to investigate the potential in bromelain-phytochemical complex inhibitors via a combination of in silico and in vitro methods. Bromelain-amenthoflavone displays antagonistic effects on Pla2. Bromelian-asiaticoside and bromelain-diosgenin displayed synergistic effects at high concentrations of the combined compounds, with inhibition percentages of more than 70% and 90%, respectively, and antagonistic effects at low concentrations...
January 19, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29350442/role-of-ethylene-and-related-gene-expression-in-the-interaction-between-strawberry-plants-and-the-plant-growth-promoting-bacterium-azospirillum-brasilense
#16
J M Elías, M F Guerrero-Molina, M G Martínez-Zamora, J C Díaz-Ricci, R O Pedraza
• The induced systemic resistance (ISR) is one of the indirect mechanisms of growth promotion exerted by plant growth-promoting bacteria, and can be mediated by ethylene (ET). We assessed the ET production and the expression of related genes in the Azospirillum-strawberry plant interaction. • ET production was evaluated by gas chromatography in plants inoculated or not with A. brasilense REC3. Also, plants were treated with AgNO3 , an inhibitor of ET biosynthesis; with 1-aminocyclopropane-1-carboxylic-acid (ACC), a precursor of ET biosynthesis; and with indole acetic acid (IAA)...
January 19, 2018: Plant Biology
https://www.readbyqxmd.com/read/29350062/telotristat-ethyl-a-novel-agent-for-the-therapy-of-carcinoid-syndrome-diarrhea
#17
Joseph S Dillon, Chandrikha Chandrasekharan
Carcinoid syndrome (CS), characterized by diarrhea and flushing, is present in 20% of patients with neuroendocrine tumors at diagnosis and becomes more frequent with progression. The diarrhea of CS is caused mainly by tumoral secretion of serotonin. It may not be fully controlled by somatostatin analogs, the currently indicated drugs for symptomatic relief. Telotristat ethyl is a novel inhibitor of tryptophan hydroxylase, the rate-limiting enzyme in serotonin biosynthesis. Administration of the drug decreases diarrhea in patients with CS...
January 19, 2018: Future Oncology
https://www.readbyqxmd.com/read/29349667/comparison-of-enalapril-candesartan-and-intralesional-triamcinolone-in-reducing-hypertrophic-scar-development-an-experimental-study
#18
Canser Yilmaz Demir, Muhammet Eren Ersoz, Remzi Erten, Omer Faruk Kocak, Yilmaz Sultanoglu, Yildiray Basbugan
BACKGROUND: The purpose of this study was to compare the effects of oral enalapril, an angiotensin-converting enzyme inhibitor (ACE-I), oral candesartan, an angiotensin receptor blocker (ARB), and intralesional corticosteroid treatments in reducing scar formation. METHODS: Twenty male rabbits were divided into five study groups: A (sham), B (control), C (ACE-I), D (ARB) and E (intralesional corticosteroid). The rabbit ear hypertrophic scar model was used. The hypertrophic scars were photographed and analyzed with the program ImageJ quantitatively to determine the degree of collagen fibers...
January 18, 2018: Aesthetic Plastic Surgery
https://www.readbyqxmd.com/read/29349663/ibandronate-metal-complexes-solution-behavior-and-antiparasitic-activity
#19
Bruno Demoro, Santiago Rostán, Mauricio Moncada, Zhu-Hong Li, Roberto Docampo, Claudio Olea Azar, Juan Diego Maya, Julia Torres, Dinorah Gambino, Lucía Otero
To face the high costs of developing new drugs, researchers in both industry and academy are looking for ways to repurpose old drugs for new uses. In this sense, bisphosphonates that are clinically used for bone diseases have been studied as agents against Trypanosoma cruzi, causative parasite of Chagas disease. In this work, the development of first row transition metal complexes (M = Co2+, Mn2+, Ni2+) with the bisphosphonate ibandronate (iba, H4iba representing the neutral form) is presented. The in-solution behavior of the systems containing iba and the selected 3d metal ions was studied by potentiometry...
January 18, 2018: Journal of Biological Inorganic Chemistry: JBIC
https://www.readbyqxmd.com/read/29348884/alpha-1-antitrypsin-functions-as-a-protective-factor-in-preeclampsia-through-activating-smad2-and-inhibitor-of-dna-binding-4
#20
Yaling Feng, Nan Wang, Jianjuan Xu, Jinfang Zou, Xi Liang, Huan Liu, Ying Chen
Pre-eclampsia (PE) is one of the most common reason for high morbidity and mortality of maternal and prenatal infants. Production from oxidative stress results in maternal ROS system and anti-oxidation defense system imbalance to promote tissue ischemia and hypoxia, and ultimately impairs the maternal organs and placenta. Our previous study showed that exogenous Alpha-1-antitrypsin (AAT) and overexpression of AAT in umbilical vein cell (HUVEC) hypoxia-reoxygenation model could increase the activity of antioxidant enzymes, and played a protective role in preeclampsia animal model...
December 22, 2017: Oncotarget
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