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https://www.readbyqxmd.com/read/29783099/leveraging-the-cruzain-s3-subsite-to-increase-affinity-for-reversible-covalent-inhibitors
#1
Lorenzo Cianni, Geraldo Sartori, Fabiana Rosini, Daniela De Vita, Gabriel Pires, Bianca Rebelo Lopes, Andrei Leitão, Antonio C B Burtoloso, Carlos A Montanari
Cruzain is the major cysteine protease of Trypanosoma cruzi, the etiological agent of Chagas disease. Reversible covalent cruzain inhibitors can block the steps of cell differentiation in the parasite and kill the organism. To this end, the description of how inhibitors modified at the P2/P3 positions lead to analogs with greater cruzain affinity to the S2/S3 subsites is of fundamental importance. Albeit many efforts are being employed in the characterization of the interaction processes with S2 subsite, little is known about the cruzain S3 subsite...
April 26, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29782963/bet-inhibition-by-jq1-alleviates-streptozotocin-induced-diabetic-cardiomyopathy
#2
Miao Guo, Hong-Xia Wang, Wen-Jun Chen
Diabetic cardiomyopathy is a cascade of complex events leading to eventual heart failure in diabetes. JQ1, one of Bromodomain and extra-terminal domain (BET) protein inhibitors, has exerted therapeutic effects on cancer proliferation, inflammation and cardiovascular disease. Recently, JQ1 was reported to protect mice from bleomycin-induced lung fibrosis and reverse the fibrotic response in carbon tetrachloride-induced liver fibrosis. However, its role in diabetic cardiomyopathy remains to be clarified. Our results indicated that JQ1 treatment suppressed cardiac fibrosis and improved cardiac function in a STZ-induced diabetic mouse model...
May 18, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29782957/the-role-of-monoamines-in-the-development-of-alzheimer-s-disease-and-neuroprotective-effect-of-a-proline-rich-polypeptide
#3
Konstantin Yenkoyan, Katarine Fereshetyan, Senik Matinyan, Vergine Chavushyan, Michail Aghajanov
INTRODUCTION: We have analyzed the alterations in the brain monoaminergic system using the rat model of AD-like pathology. In addition, we have investigated potential neuroprotective effects of the hypothalamic proline-rich polypeptide (PRP-1). METHODS: Histochemical staining, HPLC, chemiluminescent and bioluminescence assays. RESULTS: The levels of monoamines in the target AD brain structures were found elevated, except serotonin, which was unaffected in both hippocampus and brainstem and decreased in frontal cortex...
May 18, 2018: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/29782496/development-of-a-toolkit-for-piggybac-mediated-integrative-transfection-of-the-human-filarial-parasite-brugia-malayi
#4
Canhui Liu, Amruta S Mhashilkar, Johan Chabanon, Shulin Xu, Sara Lustigman, John H Adams, Thomas R Unnasch
BACKGROUND: The human filarial parasites cause diseases that are among the most important causes of morbidity in the developing world. The elimination programs targeting these infections rely on a limited number of drugs, making the identification of new chemotherapeutic agents a high priority. The study of these parasites has lagged due to the lack of reverse genetic methods. METHODOLOGY/PRINCIPAL FINDINGS: We report a novel co-culture method that results in developmentally competent infective larvae of one of the human filarial parasites (Brugia malayi) and describe a method to efficiently transfect the larval stages of this parasite...
May 21, 2018: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/29782237/effect-of-porins-and-bla-kpc-expression-on-activity-of-imipenem-with-relebactam-in-klebsiella-pneumoniae-can-antibiotic-combinations-overcome-resistance
#5
Gregory Balabanian, Michael Rose, Nyla Manning, David Landman, John Quale
Imipenem with relebactam is a novel β-lactam-β-lactamase inhibitor that has activity against most KPC-producing Enterobacteriaceae. Using 10 isolates of KPC-possessing Klebsiella pneumoniae, we assessed the relationship between imipenem-relebactam minimum inhibitory concentrations (MICs) and mechanisms known to contribute to antimicrobial resistance. The effect of adding a second agent was assessed by time-kill experiments. Mutations affecting the genes encoding porins ompK35 and ompK36 and identification of β-lactamases were assessed by PCR...
May 21, 2018: Microbial Drug Resistance: MDR: Mechanisms, Epidemiology, and Disease
https://www.readbyqxmd.com/read/29781773/a-comparison-of-total-inward-leakage-measured-using-sodium-chloride-nacl-and-corn-oil-aerosol-methods-for-air-purifying-respirators
#6
Samy Rengasamy, Ziqing Zhuang, George Niezgoda, Gary Walbert, Robert Lawrence, Brenda Boutin, Judith Hudnall, William P Monaghan, Michael Bergman, Colleen Miller, James Harris, Christopher Coffey
The International Organization for Standardization (ISO) standard 16900-1:2014 specifies the use of sodium chloride (NaCl) and corn oil aerosols, and sulfur hexafluoride gas for measuring total inward leakage (TIL). However, a comparison of TIL between different agents is lacking. The objective of this study was to measure and compare TIL for respirators using corn oil and NaCl aerosols. TIL was measured with 10 subjects donning two models of filtering facepiece respirators (FFRs) including FFP1, N95, P100, and elastomeric half-mask respirators (ERs) in NaCl and corn oil aerosol test chambers, using continuous sampling methods...
May 21, 2018: Journal of Occupational and Environmental Hygiene
https://www.readbyqxmd.com/read/29781354/effects-and-possible-mechanisms-of-alpinia-officinarum-ethanol-extract-on-indomethacin-induced-gastric-injury-in-rats
#7
Jingwen Gong, Zhong Zhang, Xuguang Zhang, Feng Chen, Yinfeng Tan, Hailong Li, Jie Jiang, Junqing Zhang
CONTEXT: Alpinia officinarum Hance (Zingiberoside) has a long history in treating gastrointestinal diseases, but its mechanisms of action are not yet known. OBJECTIVE: To investigate the effects and underlying mechanisms of the ethanol extract of A. officinarum rhizomes in an indomethacin-induced gastric injury rat model. MATERIAL AND METHODS: Indomethacin (0.3 g/kg) was orally administered to Sprague-Dawley rats to induce gastric damage; after 7 h, the rats were treated with 0...
December 2018: Pharmaceutical Biology
https://www.readbyqxmd.com/read/29780548/reversible-dispersion-and-release-of-carbon-nanotubes-via-cooperative-clamping-interactions-with-hydrogen-bonded-nanorings
#8
Raquel Chamorro, Leire de Juan-Fernández, Belén Nieto-Ortega, Maria J Mayoral, Santiago Casado, Luisa Ruiz-González, Emilio M Pérez, David González-Rodríguez
Due to their outstanding electronic and mechanical properties, single-walled carbon nanotubes (SWCNTs) are promising nanomaterials for the future generation of optoelectronic devices and composites. However, their scarce solubility limits their application in many technologies that demand solution-processing of high-purity SWCNT samples. Although some non-covalent functionalization approaches have demonstrated their utility in extracting SWCNTs into different media, many of them produce short-lived dispersions or ultimately suffer from contamination by the dispersing agent...
May 7, 2018: Chemical Science
https://www.readbyqxmd.com/read/29780536/thermoreversible-crystallization-driven-aggregation-of-diblock-copolymer-nanoparticles-in-mineral-oil
#9
Matthew J Derry, Oleksandr O Mykhaylyk, Anthony J Ryan, Steven P Armes
A poly(behenyl methacrylate)37 (PBeMA37 ) macromolecular chain transfer agent is utilized for the reversible addition-fragmentation chain transfer (RAFT) dispersion polymerization of benzyl methacrylate (BzMA) directly in mineral oil at 90 °C. Polymerization-induced self-assembly (PISA) occurs under these conditions, yielding a series of sterically-stabilized PBeMA37 -PBzMA x diblock copolymer spheres of tunable diameter as confirmed by dynamic light scattering (DLS) and transmission electron microscopy (TEM) studies...
May 7, 2018: Chemical Science
https://www.readbyqxmd.com/read/29780498/direct-and-indirect-hyperpolarisation-of-amines-using-para-hydrogen
#10
Wissam Iali, Peter J Rayner, Adel Alshehri, A Jonathan Holmes, Amy J Ruddlesden, Simon B Duckett
Nuclear Magnetic Resonance (NMR) and Magnetic Resonance Imaging (MRI) are two widely used techniques for the study of molecules and materials. Hyperpolarisation methods, such as Signal Amplification By Reversible Exchange (SABRE), turn typically weak magnetic resonance responses into strong signals. In this article we detail how it is possible to hyperpolarise the 1 H, 13 C and 15 N nuclei of a range of amines. This involved showing how primary amines form stable but labile complexes of the type [Ir(H)2 (IMes)(amine)3 ]Cl that allow para hydrogen to relay its latent polarisation into the amine...
April 21, 2018: Chemical Science
https://www.readbyqxmd.com/read/29779385/nutritional-available-seleno-amino-acid-derivative-antagonizes-cisplatin-induced-nephrotoxicity-through-inhibition-of-ros-mediated-signaling-pathways
#11
Xiaoling Li, Haobin Zhang, Leung Chan, Chang Liu, Tianfeng Chen
Discovery of nutritionally available agents that could antagonize cisplatin-induced nephrotoxicity is of great significance and clinical application potential. 3,3'-Diselenodipropionic acid (DSePA) is a seleno-amino acid derivative that exhibits strong antioxidant activity. Therefore, this study aimed to examine the protective effects of DSePA on cisplatin-induced nephrotoxicity as well as the molecular mechanisms. The results revealed that DSePA effectively inhibited cell apoptosis induced by cisplatin, through suppressing the caspases activation and PARP cleavage...
May 20, 2018: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/29779246/regulation-of-plasminogen-activation-on-cell-surfaces-and-fibrin
#12
REVIEW
Tetsumei Urano, Francis J Castellino, Yuko Suzuki
The fibrinolytic system dissolves fibrin and maintains vascular patency. Recent advances in imaging analyses allowed visualization of the spatiotemporal regulatory mechanism of fibrinolysis, as well as its regulation by other plasma haemostasis cofactors. Vascular endothelial cells (VECs) retain tissue-type plasminogen activator (tPA) after secretion and maintain high plasminogen (plg) activation potential on their surfaces. As in plasma, the serpin, plasminogen activator inhibitor type 1 (PAI-1), regulates fibrinolytic potential via inhibition of the VEC surface-bound plg activator, tPA...
May 20, 2018: Journal of Thrombosis and Haemostasis: JTH
https://www.readbyqxmd.com/read/29779175/anthocyanins-improve-hippocampus-dependent-memory-function-and-prevent-neurodegeneration-via-jnk-akt-gsk3%C3%AE-signaling-in-lps-treated-adult-mice
#13
Muhammad Sohail Khan, Tahir Ali, Min Woo Kim, Myeung Hoon Jo, Jong Il Chung, Myeong Ok Kim
Microglia plays a critical role in the brain and protects neuronal cells from toxins. However, over-activation of microglia leads to deleterious effects. Lipopolysaccharide (LPS) has been reported to affect neuronal cells via activation of microglia as well as directly to initiate neuroinflammation. In the present study, we evaluated the anti-inflammatory and anti-oxidative effect of anthocyanins against LPS-induced neurotoxicity in an animal model and in cell cultures. Intraperitoneal injections of LPS (250 μg/kg/day for 1 week) induce ROS production and promote neuroinflammation and neurodegeneration which ultimately leads to memory impairment...
May 19, 2018: Molecular Neurobiology
https://www.readbyqxmd.com/read/29777370/analysis-of-genetic-variability-of-respiratory-syncytial-virus-groups-a-and-b-in-kuwait
#14
Nada Madi, Wassim Chehadeh, Mohammed Asadzadeh, Mariam Al-Turab, Anfal Al-Adwani
Respiratory syncytial virus (RSV) is the most frequently identified viral agent in infants, children, and elderly people with acute respiratory tract infections (ARTIs). This study is the only one of its kind in Kuwait, and its purpose was to investigate the genetic variability of the G protein gene in RSV strains prevalent in Kuwait. Respiratory samples were collected from patients with ARTIs in various hospitals in Kuwait and subjected to reverse transcription PCR (RT-PCR) amplifying a fragment of the G gene of RSV...
May 19, 2018: Archives of Virology
https://www.readbyqxmd.com/read/29777330/down-regulating-il-6-gp130-targets-improved-the-anti-tumor-effects-of-5-fluorouracil-in-colon-cancer
#15
Sanhong Li, Jilai Tian, Hongming Zhang, Shoubing Zhou, Xiyong Wang, Lei Zhang, Jiapeng Yang, Zhigang Zhang, Zhenling Ji
Recent studies have confirmed that IL-6/GP130 targets are closely associated with tumor growth, metastasis and drug resistance. 5-Fluorouracil (5-FU) is the most common chemotherapeutic agent for colon cancer but is limited due to chemoresistance and high cytotoxicity. Bazedoxifene (BZA), a third-generation selective estrogen receptor modulator, was discovered by multiple ligand simultaneous docking and drug repositioning approaches to have a novel function as an IL-6/GP130 target inhibitor. Thus, we speculated that in colon cancer, the anti-tumor efficacy of 5-FU might be increased in combination with IL-6/GP130 inhibitors...
May 18, 2018: Apoptosis: An International Journal on Programmed Cell Death
https://www.readbyqxmd.com/read/29776830/pharmacological-modulation-of-radiation-induced-oral-mucosal-complications
#16
S Bockel, A Vallard, A Lévy, S François, M Bourdis, C Le Gallic, D Riccobono, P Annede, M Drouet, Y Tao, P Blanchard, É Deutsch, N Magné, C Chargari
Radiation-induced mucositis is a common toxicity, especially in patients with head and neck cancers. Despite recent technological advances in radiation therapy, such as intensity-modulated radiotherapy, radiation-induced mucositis is still causing treatment disruptions, negatively affecting patients' long and short term quality of life, and impacting medical resources use with economic consequences. The objective of this article was to review the latest updates in the management of radiation-induced mucositis, with a focus on pharmaceutical strategies for the prevention or treatment of mucositis...
May 15, 2018: Cancer Radiothérapie: Journal de la Société Française de Radiothérapie Oncologique
https://www.readbyqxmd.com/read/29776034/derivation-of-markov-processes-that-violate-detailed-balance
#17
Julian Lee
Time-reversal symmetry of the microscopic laws dictates that the equilibrium distribution of a stochastic process must obey the condition of detailed balance. However, cyclic Markov processes that do not admit equilibrium distributions with detailed balance are often used to model systems driven out of equilibrium by external agents. I show that for a Markov model without detailed balance, an extended Markov model can be constructed, which explicitly includes the degrees of freedom for the driving agent and satisfies the detailed balance condition...
March 2018: Physical Review. E
https://www.readbyqxmd.com/read/29775071/strategy-for-overcoming-full-reversibility-of-intermolecular-radical-addition-to-aldehydes-tandem-c-h-and-c-o-bonds-cleaving-cyclization-of-phenoxymethyl-arenes-with-carbonyls-to-benzofurans
#18
Hong-Xing Zheng, Xiang-Huan Shan, Jian-Ping Qu, Yan-Biao Kang
An intermolecular addition of carbon radicals enabled by a cascade radical coupling strategy is developed. It includes an intermolecular alkyl radical addition to a carbonyl group followed by an intramolecular alkoxy radical addition to haloarenes and produces substituted benzofurans in high yields. The radical nature of this reaction is explored by radical trapping experiments and EPR analysis. The mechanism is investigated by KIE experiments and control experiments. This method could provide rapid and practical access to the key intermediate of TAM-16, a safe and potent antibacterial agent for treating tuberculosis, and, therefore, is of great importance for organic synthesis and the pharmaceutical industry...
May 18, 2018: Organic Letters
https://www.readbyqxmd.com/read/29773183/cytosolic-increased-labile-zn-2-contributes-to-arrhythmogenic-action-potentials-in-left-ventricular-cardiomyocytes-through-protein-thiol-oxidation-and-cellular-atp-depletion
#19
Sinan Degirmenci, Yusuf Olgar, Aysegul Durak, Erkan Tuncay, Belma Turan
Intracellular labile (free) Zn2+ -level ([Zn2+ ]i ) is low and increases markedly under pathophysiological conditions in cardiomyocytes. High [Zn2+ ]i is associated with alterations in excitability and ionic-conductances while exact mechanisms are not clarified yet. Therefore, we examined the elevated-[Zn2+ ]i on some sarcolemmal ionic-mechanisms, which can mediate cardiomyocyte dysfunction. High-[Zn2+ ]i induced significant changes in action potential (AP) parameters, including depolarization in resting membrane-potential and prolongations in AP-repolarizing phases...
July 2018: Journal of Trace Elements in Medicine and Biology
https://www.readbyqxmd.com/read/29772998/partially-purified-aqueous-fraction-of-desmodium-gyrans-dc-improves-reverse-cholesterol-transport-and-lipoprotein-metabolism-in-wistar-rats-fed-with-high-fat-diet
#20
M S Indu, Jose Padikkala, Achuthan C Raghavamenon
Apart from the conventional hypolipidemic therapy, plaque regression through enhanced reverse cholesterol transport (RCT) has emerged as novel approach in atherosclerotic drug development. High-density lipoprotein (HDL) mimetics as well as agents that augment the functional HDL and RCT pathways are under intense exploration. Desmodium gyrans (Fabacea) has been shown to have hypolipidemic efficacy, with an HDL-enhancing property. In this study, a chromatographically purified active fraction of D. gyrans (DGMAF) significantly decreased the serum and lipid profiles as well as lipotoxicity in liver in Wistar rats fed with high-fat diet (HFD)...
2018: Journal of Environmental Pathology, Toxicology and Oncology
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