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https://www.readbyqxmd.com/read/28918449/immunochemical-study-of-the-effect-of-f2glc-on-glycogen-synthase-translocation-and-glycogen-synthesis-in-isolated-rat-hepatocytes
#1
J M Fernández-Novell, M Díaz-Lobo
The compound 2-deoxy-2-fluoro-α-D-glucopyranosyl fluoride (F2Glc), which is a nonmetabolized superior glucose analogue, is a potent inhibitor of glycogen phosphorylase and pharmacological properties are reported. Glycogen phosphorylase (GP) and glycogen synthase (GS) are responsible of the degradation and synthesis, respectively, of glycogen which is a polymer of glucose units that provides a readily available source of energy in mammals. GP and GS are two key enzymes that modulate cellular glucose and glycogen levels; therefore, these proteins are suggested as potential targets for the treatment of diseases related to glycogen metabolism disorders...
September 16, 2017: Applied Biochemistry and Biotechnology
https://www.readbyqxmd.com/read/28918407/burden-of-non-adherence-to-latent-tuberculosis-infection-drug-therapy-and-the-potential-cost-effectiveness-of-adherence-interventions-in-canada-a-simulation-study
#2
Anik R Patel, Jonathon R Campbell, Mohsen Sadatsafavi, Fawziah Marra, James C Johnston, Kirsten Smillie, Richard T Lester
OBJECTIVE: Pharmaceutical treatment of latent tuberculosis infection (LTBI) reduces the risk of progression to active tuberculosis (TB); however, poor adherence tempers the protective effect. We aimed to estimate the health burden of non-adherence, the maximum allowable cost of hypothetical new adherence interventions to be cost-effective and the potential value of existing adherence interventions for patients with low-risk LTBI in Canada. DESIGN: A microsimulation model of LTBI progression over 25 years...
September 15, 2017: BMJ Open
https://www.readbyqxmd.com/read/28918098/identifying-novel-factor-xiia-inhibitors-with-pca-ga-svm-developed-vhts-models
#3
Jonathan Jun Feng Chen, Donald P Visco
There currently is renewed interest in blood clotting Factor XII as a potential target for thrombosis inhibition. Historically untargeted, there is little drug information with which to start drug candidate searches. Typical high-throughput screening can identify potential drug candidates, but is inefficient. Virtual high-throughput screening can be used to raise efficiency by focusing experimental efforts on compounds predicted to be active and is applied here to identify new Factor XIIa inhibitors. We combine principal component analysis, genetic algorithm and support vector machine to create the models used in the virtual high-throughput screening...
September 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28918031/anti-adenoviral-artificial-micrornas-expressed-from-aav9-vectors-inhibit-human-adenovirus-infection-in-immunosuppressed-syrian-hamsters
#4
Katrin Schaar, Anja Geisler, Milena Kraus, Sandra Pinkert, Markian Pryshliak, Jacqueline F Spencer, Ann E Tollefson, Baoling Ying, Jens Kurreck, William S Wold, Robert Klopfleisch, Karoly Toth, Henry Fechner
Infections of immunocompromised patients with human adenoviruses (hAd) can develop into life-threatening conditions, whereas drugs with anti-adenoviral efficiency are not clinically approved and have limited efficacy. Small double-stranded RNAs that induce RNAi represent a new class of promising anti-adenoviral therapeutics. However, as yet, their efficiency to treat hAd5 infections has only been investigated in vitro. In this study, we analyzed artificial microRNAs (amiRs) delivered by self-complementary adeno-associated virus (scAAV) vectors for treatment of hAd5 infections in immunosuppressed Syrian hamsters...
September 15, 2017: Molecular Therapy. Nucleic Acids
https://www.readbyqxmd.com/read/28918016/therapeutic-mirna-and-sirna-moving-from-bench-to-clinic-as-next-generation-medicine
#5
REVIEW
Chiranjib Chakraborty, Ashish Ranjan Sharma, Garima Sharma, C George Priya Doss, Sang-Soo Lee
In the past few years, therapeutic microRNA (miRNA) and small interfering RNA (siRNA) are some of the most important biopharmaceuticals that are in commercial space as future medicines. This review summarizes the patents of miRNA- and siRNA-based new drugs, and also provides a snapshot about significant biopharmaceutical companies that are investing for the therapeutic development of miRNA and siRNA molecules. An insightful view about individual siRNA and miRNA drugs has been depicted with their present status, which is gaining attention in the therapeutic landscape...
September 15, 2017: Molecular Therapy. Nucleic Acids
https://www.readbyqxmd.com/read/28917985/the-effect-of-particle-shape-on-cellular-interaction-and-drug-delivery-applications-of-micro-and-nanoparticles
#6
REVIEW
Anil B Jindal
Encapsulation of therapeutic agents in nanoparticles offers several benefits including improved bioavailability, site specific delivery, reduced toxicity and in vivo stability of proteins and nucleotides over conventional delivery options. These benefits are consequence of distinct in vivo pharmacokinetic and biodistribution profile of nanoparticles, which is dictated by the complex interplay of size, surface charge and surface hydrophobicity. Recently, particle shape has been identified as a new physical parameter which has exerted tremendous impact on cellular uptake and biodistribution, thereby in vivo performance of nanoparticles...
September 13, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28917978/sen1500-a-novel-oral-amyloid-%C3%AE-aggregation-inhibitor-attenuates-brain-pathology-in-a-mouse-model-of-alzheimer-s-disease
#7
D Brunner, S Flunkert, J Neddens, S Duller, D I C Scopes, J M Treherne, B Hutter-Paier
INTRODUCTION: Amyloid-β (Aβ) aggregation is thought to be a major pathogenic event underlying the neuropathology of Alzheimer's disease (AD). The development of new drugs inhibiting the Aβ aggregation process is, therefore, important. SEN1500, an orally bioavailable and CNS-penetrant Aβ aggregation inhibitor, has previously been shown to reduce spatial learning and memory deficits in an APP transgenic mouse model. To verify that the pharmacological properties of SEN1500 are not unique to this model, we investigated brain Aβ pathology, neuroinflammation, as well as memory in a different mouse model of AD expressing the human amyloid precursor protein with Swedish and London mutations (APPSL)...
September 13, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28917974/cross-cultural-analysis-of-medicinal-plants-commonly-used-in-ethnoveterinary-practices-at-south-waziristan-agency-and-bajaur-agency-federally-administrated-tribal-areas-fata-pakistan
#8
Muhammad Abdul Aziz, Muhammad Adnan, Amir Hasan Khan, Muhammad Sufyan, Shahid Niaz Khan
ETHNOPHARMACOLOGICAL RELEVANCE: In remote areas, medicinal plants have an imperative role in curing various livestock's ailments. In Pakistan, people residing in remote areas including South Waziristan Agency and Bajaur Agency depend on traditional herbal remedies for treating their domestic animals. Medicinal plants are an important part of the medical system in these Agencies. The prime goal of the current study is to explore the ethnoveterinary practices in the two regions and discuss cross-cultural consensus on the use of medicinal plants...
September 13, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28917964/phenazopyridine-phthalimide-nano-cocrystal-release-rate-and-oral-bioavailability-enhancement
#9
Yu Huang, Jin-Mei Li, Zhi-Hui Lai, Jun Wu, Tong-Bu Lu, Jia-Mei Chen
Both cocrystal and nanocrystal technologies have been widely used in the pharmaceutical development for poorly soluble drugs. However, the synergistic effects due to the integration of these two technologies have not been well investigated. The aim of this study is to develop a nano-sized cocrystal of phenazopyridine (PAP) with phthalimide (PI) to enhance the release rate and oral bioavailability of PAP. A PAP-PI nano-cocrystal with particle diameter of 21.4±0.1nm was successfully prepared via a sonochemical approach and characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and dynamic light scattering (DLS) analysis...
September 13, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28917952/identification-of-potential-allosteric-communication-pathways-between-functional-sites-of-the-bacterial-ribosome-by-graph-and-elastic-network-models
#10
Pelin Guzel, Ozge Kurkcuoglu
BACKGROUND: Accumulated evidence indicates that bacterial ribosome employs allostery throughout its structure for protein synthesis. The nature of the allosteric communication between remote functional sites remains unclear, but the contact topology and dynamics of residues may play role in transmission of a perturbation to distant sites. METHODS/RESULTS: We employ two computationally efficient approaches - graph and elastic network modeling to gain insights about the allosteric communication in ribosome...
September 13, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28917926/bioadhesive-and-biocompatible-films-as-wound-dressing-materials-based-on-a-novel-dendronized-chitosan-loaded-with-ciprofloxacin
#11
Mónica C García, Ana A Aldana, Luis I Tártara, Fabiana Alovero, Miriam C Strumia, Rubén H Manzo, Marisa Martinelli, Alvaro F Jimenez-Kairuz
The bioadhesive polymeric films as topical drug delivery systems are interesting alternatives to improve the pharmacotherapy and patient compliances. New derivate biomaterials based on weisocyanate- dendronized PVP- crosslinked chitosan and loaded with ciprofloxacin (CIP), as model drug, were used to prepare bioadhesive films. Relevant in vitro/in vivo attributes to define main physicochemical and biopharmaceutical characteristics for topical wound-healing applications were evaluated. A high proportion of CIP, uniformly dispersed along throughout the film, was loaded...
November 1, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28917874/alginate-modified-with-maleimide-terminated-peg-as-drug-carriers-with-enhanced-mucoadhesion
#12
Yarden Shtenberg, Mor Goldfeder, Avi Schroeder, Havazelet Bianco-Peled
The goal of this study was to generate a new mucoadhesive carbohydrate-based delivery system composed of alginate (Alg) backbone covalently attached to polyethylene glycol (PEG) modified with a unique functional end-group (maleimide). The immobilization of PEG-maleimide chains significantly improved the mucoadhesion properties attributed to thioether bonds creation via Michael-type addition and hydrogen bonding with the mucus glycoproteins. Mucoadhesion studies using tensile and rotating cylinder assays revealed a 3...
November 1, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28917801/development-of-a-quantitative-approach-in-blood-plasma-for-low-dosed-hallucinogens-and-opioids-using-lc-high-resolution-mass-spectrometry
#13
Achim T Caspar, Andreas B Kollas, Hans H Maurer, Markus R Meyer
The WHO annually reports an increasing abuse of new psychoactive substances (NPS), which are a heterogeneous group of synthetic drugs and are consumed as substitute for controlled drugs of abuse. In this work, we focused on highly potent derivatives such those of phenethylamine (2C), N-2-methoxybenzyl phenethylamine (NBOMes), lysergic acid diethylamide (LSD), and fentanyl. Severe to fatal intoxications were described due to their high potency. Therefore, they have to be taken at very low doses resulting in low blood concentration in the low ng/mL range, which is a challenge for reliable analytical detection and quantification...
January 1, 2018: Talanta
https://www.readbyqxmd.com/read/28917574/-apparent-worsening-of-psoriasis-lesions-revealing-methotrexate-overdosage
#14
R Haber, B Baroudjian, M Battistella, M Bagot, A Petit
BACKGROUND: Methotrexate (MTX) is an antimetabolite drug used in the treatment of cancers and autoimmune diseases and frequently in dermatology for cutaneous and/or arthritic psoriasis. Toxicities due to MTX overdosage are mainly cutaneous, hepatic and hematologic. Herein, we report a case of MTX overdosage presenting as an erosive and an inflammatory flare of preexisting psoriatic plaques and with new palmar lesions. PATIENTS AND METHODS: A 51-year-old male with a 6-year history of plaque psoriasis resistant to topical corticosteroids was started for the first time on MTX 20mg weekly...
September 13, 2017: Annales de Dermatologie et de Vénéréologie
https://www.readbyqxmd.com/read/28917501/personalized-translational-epilepsy-research-novel-approaches-and-future-perspectives-part-i-clinical-and-network-analysis-approaches
#15
REVIEW
Felix Rosenow, Natascha van Alphen, Albert Becker, Andreas Chiocchetti, Ralf Deichmann, Thomas Deller, Thomas Freiman, Christine M Freitag, Johannes Gehrig, Anke M Hermsen, Peter Jedlicka, Christian Kell, Karl Martin Klein, Susanne Knake, Dimitri M Kullmann, Stefan Liebner, Braxton A Norwood, Diana Omigie, Karlheinz Plate, Andreas Reif, Philipp S Reif, Yvonne Reiss, Jochen Roeper, Michael W Ronellenfitsch, Stephanie Schorge, Gerhard Schratt, Stephan W Schwarzacher, Joachim P Steinbach, Adam Strzelczyk, Jochen Triesch, Marlies Wagner, Matthew C Walker, Frederic von Wegner, Sebastian Bauer
Despite the availability of more than 15 new "antiepileptic drugs", the proportion of patients with pharmacoresistant epilepsy has remained constant at about 20-30%. Furthermore, no disease-modifying treatments shown to prevent the development of epilepsy following an initial precipitating brain injury or to reverse established epilepsy have been identified to date. This is likely in part due to the polyetiologic nature of epilepsy, which in turn requires personalized medicine approaches. Recent advances in imaging, pathology, genetics and epigenetics have led to new pathophysiological concepts and the identification of monogenic causes of epilepsy...
September 13, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28917498/personalized-translational-epilepsy-research-novel-approaches-and-future-perspectives-part-ii-experimental-and-translational-approaches
#16
REVIEW
Sebastian Bauer, Natascha van Alphen, Albert Becker, Andreas Chiocchetti, Ralf Deichmann, Thomas Deller, Thomas Freiman, Christine M Freitag, Johannes Gehrig, Anke M Hermsen, Peter Jedlicka, Christian Kell, Karl Martin Klein, Susanne Knake, Dimitri M Kullmann, Stefan Liebner, Braxton A Norwood, Diana Omigie, Karlheinz Plate, Andreas Reif, Philipp S Reif, Yvonne Reiss, Jochen Roeper, Michael W Ronellenfitsch, Stephanie Schorge, Gerhard Schratt, Stephan W Schwarzacher, Joachim P Steinbach, Adam Strzelczyk, Jochen Triesch, Marlies Wagner, Matthew C Walker, Frederic von Wegner, Felix Rosenow
Despite the availability of more than 15 new "antiepileptic drugs", the proportion of patients with pharmacoresistant epilepsy has remained constant at about 20-30%. Furthermore, no disease-modifying treatments shown to prevent the development of epilepsy following an initial precipitating brain injury or to reverse established epilepsy have been identified to date. This is likely in part due to the polyetiologic nature of epilepsy, which in turn requires personalized medicine approaches. Recent advances in imaging, pathology, genetics, and epigenetics have led to new pathophysiological concepts and the identification of monogenic causes of epilepsy...
September 13, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28917310/screening-of-a-small-well-curated-natural-product-based-library-identifies-two-rotenoids-with-potent-nematocidal-activity-against-haemonchus-contortus
#17
H M P Dilrukshi Herath, Sarah Preston, Andreas Hofmann, Rohan A Davis, Anson V Koehler, Bill C H Chang, Abdul Jabbar, Robin B Gasser
The control of parasitic roundworms (nematodes) is heavily reliant on the use of a limited number of anthelmintic drugs. However, drug resistance is now very widespread and no vaccines are available, such that the discovery of new chemical entities is crucial. Within this context, we screened a library of pure natural products (n=400) against exsheathed third-stage (xL3) larvae of the parasitic nematode Haemonchus contortus using a whole-organism screening method. We identified two plant-derived rotenoids, deguelin and rotenone, with inhibitory activity on xL3 motility...
September 15, 2017: Veterinary Parasitology
https://www.readbyqxmd.com/read/28917086/kostchyienones-a-and-b-new-antiplasmodial-and-cytotoxicity-of-limonoids-from-the-roots-of-pseudocedrela-kotschyi-schweinf-harms
#18
Lazare S Sidjui, Yves O D Nganso, Rufin M K Toghueo, Brussine N K Wakeu, Joel T Dameue, Pierre Mkounga, Achyut Adhikari, Mehreen Lateef, Gabriel N Folefoc, Muhammad S Ali
Two new limonoids, kostchyienones A (1) and B (2), along with 12 known compounds 3-14 were isolated from the roots of Pseudocedrela kostchyi. Compound (7) was isolated for the first time from a natural source. Their structures were elucidated on the basis of spectroscopic evidence. Compounds 1-6 and 13-14 gave IC50 values ranging from 0.75 to 5.62 μg/mL for antiplasmodial activity against chloroquine-sensitive (Pf3D7) and chloroquine-resistant (PfINDO) strains of Plasmodium falciparum. Compound 5 showed moderate potential cytotoxicity against the HEK239T cell line with an IC50 value of 22...
September 16, 2017: Zeitschrift Für Naturforschung. C, A Journal of Biosciences
https://www.readbyqxmd.com/read/28916931/physical-exercise-prescription-in-metabolic-chronic-disease
#19
Laura Stefani, Giorgio Galanti
Metabolic syndrome as a consequence of the association to overweight, hypertension, and diabetes is at high risk of coronary events. Regular physical training has been recently promoted to reduce cardiovascular risks factors, by the improved lifestyle and also by the "anti-inflammatory effectiveness." A positive impact has been shown in case of cancer survived patients either with or without comorbidities and especially in those subjects where the inflammatory process is globally represented. The American College of Sports Medicine (ACSM) guidelines and more recently a new Italian model both support the role of "exercise as therapy" at moderate level of energy expenditure...
2017: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/28916900/were-all-carbapenemases-created-equal-treatment-of-ndm-producing-extensively-drug-resistant-enterobacteriaceae-a-case-report-and-literature-review
#20
REVIEW
Vindana Chibabhai, Trusha Nana, Norma Bosman, Teena Thomas, Warren Lowman
PURPOSE: There is currently a paucity of published literature focused on the treatment of infections caused by NDM-producing organisms. METHODS: We describe a case of a bacteraemia caused by an extensively drug-resistant (XDR) New Delhi metallo-β-lactamase (NDM)-producing Serratia marcescens and review the treatment options for XDR NDM-producing Enterobacteriaceae. RESULTS: Infections caused by New Delhi beta-lactamase (NDM)-producing Enterobacteriaceae are becoming increasingly prevalent worldwide...
September 15, 2017: Infection
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