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https://www.readbyqxmd.com/read/28527421/a-phase-iii-randomized-multi-center-double-blind-placebo-controlled-study-of-safety-and-efficacy-of-lofexidine-for-relief-of-symptoms-in-individuals-undergoing-inpatient-opioid-withdrawal
#1
Charles W Gorodetzky, Sharon L Walsh, Peter R Martin, Andrew J Saxon, Kristen L Gullo, Kousick Biswas
BACKGROUND: Lofexidine is an alpha-2-adrenergic receptor agonist approved in the United Kingdom (UK) for the treatment of opioid withdrawal symptoms. Lofexidine has demonstrated better efficacy than placebo for reducing opioid withdrawal symptoms in patients undergoing opioid withdrawal with less reported hypotension than clonidine. METHODS: Designed as an FDA registration trial, this 8-day, randomized, double-blind, placebo-controlled, parallel-group study in 264 patients dependent on short-acting opioids evaluated the efficacy of lofexidine hydrochloride in reducing withdrawal symptoms in patients undergoing opioid withdrawal...
May 10, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28527406/the-relevance-of-ki-calculation-for-bi-substrate-enzymes-illustrated-by-kinetic-evaluation-of-a-novel-lysine-k-acetyltransferase-8-inhibitor
#2
Hannah Wapenaar, Thea van den Bosch, Niek G J Leus, Petra E van der Wouden, Nikolaos Eleftheriadis, Jos Hermans, Gebremedhin Solomon Hailu, Dante Rotili, Antonello Mai, Alexander Dömling, Rainer Bischoff, Hidde J Haisma, Frank J Dekker
Histone acetyltransferases (HATs) are important mediators of epigenetic post-translational modifications of histones that play important roles in health and disease. A disturbance of these modifications can result in disease states, such as cancer or inflammatory diseases. Inhibitors of HATs (HATi) such as lysine (K) acetyltransferase 8 (KAT8), could be used to study the epigenetic processes in diseases related to these enzymes or to investigate HATs as therapeutic targets. However, the development of HATi is challenged by the difficulties in kinetic characterization of HAT enzymes and their inhibitors to enable calculation of a reproducible inhibitory potency...
May 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28527405/synthesis-and-structure-activity-relationships-of-novel-fused-ring-analogues-of-q203-as-antitubercular-agents
#3
Sunhee Kang, Young Mi Kim, Heekyung Jeon, Sejin Park, Min Jung Seo, Saeyeon Lee, Dongsik Park, Jiyeon Nam, Seokwoo Lee, Kiyean Nam, Sanghee Kim, Jaeseung Kim
A set of fused ring analogues of a new antitubercular agent, Q203, was designed and synthesized. To reduce the lipophilicity of Q203 caused by linearly extended side chains, shorter and heteroatoms containing fused rings were introduced into the side chain region. Antitubercular activity was tested against H37Rv-GFP replicating in liquid broth culture medium (extracellular) and within macrophages (intracellular). Many analogues showed potent extracellular activities as well as intracellular activities without cytotoxicity...
May 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28527400/effects-of-combretastatin-a-4-phosphate-on-canine-normal-and-tumor-tissue-derived-endothelial-cells
#4
Yusuke Izumi, Keisuke Aoshima, Yuki Hoshino, Satoshi Takagi
Combretastatin A-4 phosphate (CA4P) selectively blocks tumor blood flow. However, the detailed mechanisms through which CA4P specifically affects tumor blood vessels are not well understood. Recent reports revealed that tumor tissue-derived endothelial cells (TECs) have various specific features in comparison with normal tissue-derived endothelial cells (NECs). Thus, abnormalities in TECs may be involved in the selective vascular blockade mechanism of CA4P. In this study, we evaluated the effects of CA4P on canine NECs and TECs using confocal microscopy...
May 13, 2017: Research in Veterinary Science
https://www.readbyqxmd.com/read/28527398/quantitative-comparison-between-real-space-and-bloch-wave-methods-in-image-simulation
#5
Yi Yang, Qibin Yang, Jianyu Huang, Canying Cai, Jianguo Lin
Both Bloch wave (BW) and real space multislice (RS-MS) methods are based on the Schrödinger equation. The BW method is considered to be the most accurate and popular simulation method used in various simulations, and it has solved many crystallographic problems. In this paper, we verified that the aforementioned two methods are similar to each other with minor difference. First, the RS-MS method is implemented in the real space, while the BW method is carried out in the reciprocal space. Furthermore, by quantitatively calculating exit wavefunctions of four crystals, i...
April 27, 2017: Micron: the International Research and Review Journal for Microscopy
https://www.readbyqxmd.com/read/28527393/a-combination-of-platelet-features-allows-detection-of-early-stage-cancer
#6
Siamack Sabrkhany, Marijke J E Kuijpers, Sander M J van Kuijk, Linda Sanders, Sharo Pineda, Steven W M Olde Damink, Anne-Marie C Dingemans, Arjan W Griffioen, Mirjam G A Oude Egbrink
BACKGROUND: Detection of early-stage cancer significantly improves patient survival. As platelets play an important role in cancer progression, we aimed to investigate whether platelets can be used for the discovery of early-stage cancer. METHODS: Patients with lung (n = 86) or head of pancreas (n = 42) cancer were included, as were healthy sex- and age-matched controls (n = 92). Blood was collected before initiation of treatment. Platelet count, volume and activation status were quantified in whole blood...
May 17, 2017: European Journal of Cancer
https://www.readbyqxmd.com/read/28527390/on-filter-direct-amplification-of-legionella-pneumophila-for-rapid-assessment-of-its-abundance-and-viability
#7
Farag A Samhan, Tiffany M Stedtfeld, Hassan Waseem, Maggie R Williams, Robert D Stedtfeld, Syed A Hashsham
Guidelines and regulations to control Legionella pneumophila in cooling water systems of large buildings are evolving due to the increasing number of outbreaks. Rapid, on-site, simple, and sensitive quantification methods that are also able to assess viability may be extremely useful in monitoring and control. Culture-based methods for measuring L. pneumophila may take 4-10 days and qPCR-based methods are also slow, requiring at least a day from sample to result, albeit mainly due to the need for sample transport to a centralized laboratory...
May 13, 2017: Water Research
https://www.readbyqxmd.com/read/28527388/abiotic-transformation-of-hexabromocyclododecane-by-sulfidated-nanoscale-zerovalent-iron-kinetics-mechanism-and-influencing-factors
#8
Dan Li, Xifen Zhu, Yin Zhong, Weilin Huang, Ping'an Peng
Recent studies showed that sulfidated nanoscale zerovalent iron (S-nZVI) is a better reducing agent than nanoscale zerovalen iron (nZVI) alone for reductive dechlorination of several organic solvents such as trichloroethylene (TCE) due to the catalytic role of iron sulfide (FeS). We measured the rates of transformation of hexabromocyclododecane (HBCD) by S-nZVI and compared them to those by FeS, nZVI, and reduced sulfur species. The results showed that: i) HBCD (20 mg L(-1)) was almost completely transformed by S-nZVI (0...
May 9, 2017: Water Research
https://www.readbyqxmd.com/read/28527383/tributyltin-and-triphenyltin-exposure-promotes-in-vitro-adipogenic-differentiation-but-alters-the-adipocyte-phenotype-in-rainbow-trout
#9
Esmail Lutfi, Natàlia Riera-Heredia, Marlon Córdoba, Cinta Porte, Joaquim Gutiérrez, Encarnación Capilla, Isabel Navarro
Numerous environmental pollutants have been identified as potential obesogenic compounds affecting endocrine signaling and lipid homeostasis. Among them, well-known organotins such as tributyltin (TBT) and triphenyltin (TPT), can be found in significant concentrations in aquatic environments. The aim of the present study was to investigate in vitro the effects of TBT and TPT on the development and lipid metabolism of rainbow trout (Onchorynchus mykiss) primary cultured adipocytes. Results showed that TBT and TPT induced lipid accumulation and slightly enhanced peroxisome proliferator-activated receptor gamma (PPARγ) and CCAAT enhancer binding protein alpha (C/EBPα) protein expression when compared to a control, both in the presence or absence of lipid mixture...
May 8, 2017: Aquatic Toxicology
https://www.readbyqxmd.com/read/28527380/measurement-differences-between-turbidity-instruments-and-their-implications-for-suspended-sediment-concentration-and-load-calculations-a-sensor-inter-comparison-study
#10
A Rymszewicz, J J O'Sullivan, M Bruen, J N Turner, D M Lawler, E Conroy, M Kelly-Quinn
The use of turbidity for indicating environmentally detrimental levels of suspended and colloidal matter in freshwater systems, and for defining acceptable water quality standards in national and European drinking water regulations, is well established. Turbidity is therefore frequently adopted as a surrogate for suspended sediment concentrations (SSC), or as a relative and objective measure of water clarity in monitoring programmes. Through systematic, controlled experimentation, we tested the response of 12 commercially available turbidity sensors, of various designs, to gauge their measurement consistency when benchmarked against pre-prepared sediment suspensions of known SSC...
May 17, 2017: Journal of Environmental Management
https://www.readbyqxmd.com/read/28527360/liposomes-coated-with-hydrophobically-modified-hydroxyethyl-cellulose-influence-of-hydrophobic-chain-length-and-degree-of-modification
#11
Gro Smistad, Bo Nyström, Kaizheng Zhu, Marthe Karoline Grønvold, Anne Røv-Johnsen, Marianne Hiorth
Nanoparticulate systems with an uncharged hydrophilic surface may have a great potential in mucosal drug delivery. In the present study liposomes were coated with hydrophobically modified hydroxyethyl cellulose (HM-HEC) to create a sterically stabilized liposomal system with an uncharged surface. The aim was to clarify the influence of the amount of hydrophobic modification of HEC and the length of the hydrophobic moiety, on the stability of the system and on the release properties. HM-HEC with different degrees of hydrophobic modification (1 and 2mol%) and hydrophobic groups with different chain lengths (C8, C12, C16) were included in the study, as well as fluid phase and gel phase liposomes...
May 1, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28527355/antimycotic-activity-of-fengycin-c-biosurfactant-and-its-interaction-with-phosphatidylcholine-model-membranes
#12
Lina María González-Jaramillo, Francisco José Aranda, José Antonio Teruel, Valeska Villegas-Escobar, Antonio Ortiz
Lipopeptide biosurfactants constitute one of the most promising groups of compounds for the treatment and prevention of fungal diseases in plants. Bacillus subtilis strain EA-CB0015 produces iturin A, fengycin C and surfactin and it has been proven useful for the treatment of black Sigatoka disease in banana plants, an important pathology caused by the fungus Mycosphaerella fijiensis (Morelet). We have found that B. subtilis EA-CB0015 cell free supernatants and purified fractions inhibit M. fijiensis cellular growth...
May 10, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28527351/permutation-entropy-analysis-of-heart-rate-variability-for-the-assessment-of-cardiovascular-autonomic-neuropathy-in-type-1-diabetes-mellitus
#13
Claudia Carricarte Naranjo, Lazaro M Sanchez-Rodriguez, Marta Brown Martínez, Mario Estévez Báez, Andrés Machado García
Heart rate variability (HRV) analysis is a relevant tool for the diagnosis of cardiovascular autonomic neuropathy (CAN). To our knowledge, no previous investigation on CAN has assessed the complexity of HRV from an ordinal perspective. Therefore, the aim of this work is to explore the potential of permutation entropy (PE) analysis of HRV complexity for the assessment of CAN. For this purpose, we performed a short-term PE analysis of HRV in healthy subjects and type 1 diabetes mellitus patients, including patients with CAN...
May 8, 2017: Computers in Biology and Medicine
https://www.readbyqxmd.com/read/28527336/title-potassium-application-regulates-nitrogen-metabolism-and-osmotic-adjustment-in-cotton-gossypium-hirsutum-l-functional-leaf-under-drought-stress
#14
Rizwan Zahoor, Wenqing Zhao, Muhammad Abid, Haoran Dong, Zhiguo Zhou
To evaluate the role of potassium (K) in maintaining nitrogen metabolism and osmotic adjustment development of cotton functional leaves to sustain growth under soil drought and rewatering conditions, the plants of two cotton cultivars Siza 3 (low-K sensitive) and Simian 3 (low-K tolerant), were grown under three different K rates (K0, K1, and K2; 0, 150, and 300kgK2Oha(-1), respectively) and exposed to drought stress with 40±5% soil relative water content (SRWC). The drought stress was applied at flowering stage by withholding water for eight days followed by rewatering to a well-watered level (75±5% SRWC)...
May 4, 2017: Journal of Plant Physiology
https://www.readbyqxmd.com/read/28527333/transcriptome-wide-analysis-of-jasmonate-treated-by-2-cells-reveals-new-transcriptional-regulators-associated-with-alkaloid-formation-in-tobacco
#15
Yuping Yang, Pengcheng Yan, Che Yi, Wenzheng Li, Yuhui Chai, Lingling Fei, Ping Gao, Heping Zhao, Yingdian Wang, Michael P Timko, Bingwu Wang, Shengcheng Han
Jasmonates (JAs) are well-known regulators of stress, defence, and secondary metabolism in plants, with JA perception triggering extensive transcriptional reprogramming, including both activation and/or repression of entire metabolic pathways. We performed RNA sequencing based transcriptomic profiling of tobacco BY-2 cells before and after treatment with methyl jasmonate (MeJA) to identify novel transcriptional regulators associated with alkaloid formation. A total of 107,140 unigenes were obtained through de novo assembly, and at least 33,213 transcripts (31%) encode proteins, in which 3419 transcription factors (TFs) were identified, representing 72 gene families, as well as 840 transcriptional regulators (TRs) distributed among 19 gene families...
May 4, 2017: Journal of Plant Physiology
https://www.readbyqxmd.com/read/28527325/dyslipidemia-management-update
#16
REVIEW
Yingzi Chang, Jacques Robidoux
Association of hypercholesterolemia and atherosclerotic cardiovascular disease (ASCVD) is well established. Reducing low-density lipoprotein-cholesterol (LDL-C) and raising high-density lipoprotein-cholesterol (HDL-C) have been the therapeutic targets to reduce the risk of ASCVD. Cholesterol-lowering medications have been used to provide both primary and secondary prevention of ASCVD for many years by reducing the absorption and reabsorption, promoting excretion, or decreasing the synthesis of cholesterol. Within the past five years, several new classes of cholesterol-lowering drugs have been tested and approved for patients with hypercholesterolemia that are not well controlled by conventional therapy (ezetimibe, bile-acid sequestrants, and statins)...
May 17, 2017: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/28527302/aortic-adventitial-fibroblast-sensitivity-to-mitogen-activated-protein-kinase-inhibitors-depends-on-substrate-stiffness
#17
Rebecca A Scott, Prathamesh M Kharkar, Kristi L Kiick, Robert E Akins
Adventitial fibroblasts (AFs) are key determinants of arterial function and critical mediators of arterial disease progression. The effects of altered stiffness, particularly those observed across individuals during normal vascular function, and the mechanisms by which AFs respond to altered stiffness, are not well understood. To study the effects of matrix stiffness on AF phenotype, cytokine production, and the regulatory pathways utilized to interpret basic cell-matrix interactions, human aortic AFs were grown in 5%, 7...
May 10, 2017: Biomaterials
https://www.readbyqxmd.com/read/28527298/enhanced-adsorption-performance-of-mos2-nanosheet-coated-mil-101-hybrids-for-the-removal-of-aqueous-rhodamine-b
#18
Cao Yang, Jianhua Cheng, Yuancai Chen, Yongyou Hu
A MoS2 nanosheet-coated chromium terephthalate MIL-101 octahedron hybrid (denoted as MoS2/MIL-101) was prepared via a simple hydrothermal reaction. The obtained MoS2/MIL-101 hybrid exhibited a significantly enhanced adsorption ability toward rhodamine B (RhB) as compared with pure MoS2, MIL-101, and the physical mixture of the two. The results demonstrate that the MoS2/MIL-101 hybrid had a high uptake capacity (Qm ≈ 344.8mgg(-1)) and fast adsorption rate for the removal of aqueous RhB. The excellent adsorption performance is likely related to the synergism of hydrogen bonding, π-π stacking interactions, and direct coordination between the MIL-101 substrate and RhB, as well as electrostatic interactions between MoS2 nanosheets and RhB...
May 10, 2017: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28527297/hyaluronic-acid-nanogels-prepared-via-ortho-ester-linkages-show-ph-triggered-behavior-enhanced-penetration-and-antitumor-efficacy-in-3-d-tumor-spheroids
#19
Guanqing Yang, Shengxiang Fu, Weijing Yao, Xin Wang, Qian Zha, Rupei Tang
A new type of pH-triggered hyaluronic acid nanogel system (HA-NGs) was successfully developed for tumor-targeted delivery of drugs. HA-NGs were obtained by copolymerization between methacrylate HA and a new cross-linker containing ortho ester groups in an aqueous solution. The therapeutic drug (DOX) was loaded into the HA-NGs (DOX@HA-NGs) and exhibited appropriate loading of about 17.3% with a size of around 200nm. Such new pH-triggered HA-NGs are found to be highly desirable for targeted cancer therapy because it could significantly minimize the amount of premature drug release in neutral pH, and also provide a sufficient amount of drug to effectively kill the cancer cells caused by the degradation of ortho ester groups at acid pH values...
May 12, 2017: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28527294/activation-of-hypoxia-signaling-in-stromal-progenitors-impairs-kidney-development
#20
Katharina Gerl, Dominik Steppan, Michaela Fuchs, Charlotte Wagner, Carsten Willam, Armin Kurtz, Birgül Kurt
Intrauterine hypoxia is a reason for impaired kidney development. The cellular and molecular pathways along which hypoxia exerts effects on nephrogenesis are not well understood. They are likely triggered by hypoxia-inducible transcription factors (HIFs), and their effects appear to be dependent on the cell compartment contributing to kidney formation. In this study, we investigated the effects of HIF activation in the developing renal stroma, which also essentially modulates nephron development from the metanephric mesenchyme...
May 17, 2017: American Journal of Pathology
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