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https://www.readbyqxmd.com/read/28544960/anti-biofilm-effect-of-dihydromyricetin-loaded-nanocapsules-on-urinary-catheter-infected-by-pseudomonas-aeruginosa
#1
A J F Dalcin, C G Santos, S S Gündel, I Roggia, R P Raffin, A F Ourique, R C V Santos, P Gomes
Nosocomial infections associated with biofilm formation on urinary catheters are among the leading causes of complications due to biofilm characteristics and high antimicrobial resistance. An interesting alternative are natural products, such as Dihydromyricetin (DMY), a flavonoid which presents several pharmacological properties, including strong antimicrobial activity against various microorganisms. However, DMY, has low aqueous solubility and consequently low bioavailability. Nanoencapsulation can contribute to the improvement of characteristics of some drugs, by increasing the apparent solubility and sustained release has been reported among other advantages...
May 15, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28544930/neural-oscillations-demonstrate-that-general-anesthesia-and-sedative-states-are-neurophysiologically-distinct-from-sleep
#2
REVIEW
Oluwaseun Akeju, Emery N Brown
General anesthesia is a man-made neurophysiological state comprised of unconsciousness, amnesia, analgesia, and immobility along with maintenance of physiological stability. Growing evidence suggests that anesthetic-induced neural oscillations are a primary mechanism of anesthetic action. Each anesthetic drug class produces distinct oscillatory dynamics that can be related to the circuit mechanisms of drug action. Sleep is a naturally occurring state of decreased arousal that is essential for normal health...
May 22, 2017: Current Opinion in Neurobiology
https://www.readbyqxmd.com/read/28543443/structural-review-of-ppar%C3%AE-in-complex-with-ligands-cartesian-and-dihedral-angle-principal-component-analyses-of-x-ray-crystallographic-data
#3
Åsmund Kaupang, Tuomo Laitinen, Antti Poso, Trond Vidar Hansen
Two decades of research into the ligand-dependent modulation of the activity of the peroxisome proliferator-activated receptor γ (PPARγ) have demonstrated the heterogeneous modes of action of PPARγ ligands, in terms of their interaction surfaces in the ligand-binding pocket, binding stoichiometry and ability to interact with functionally important parts of the receptor, through both direct and allosteric mechanisms. These findings signal the complex mechanistic bases of the distinct biological effects of different classes of PPARγ ligands...
May 24, 2017: Proteins
https://www.readbyqxmd.com/read/28543407/assessing-bipolar-disorder-in-the-older-adult-the-geri-bd-toolbox
#4
Patricia Marino, Herbert C Schulberg, Ariel G Gildengers, Benoit H Mulsant, Martha Sajatovic, Laszlo Gyulai, Rayan K Aljurdi, Laurie Davan Evans, Samprit Banerjee, Ruben C Gur, Robert C Young
INTRODUCTION: The evidence base regarding characteristics of older adults with bipolar disorder (BD) remains limited. The NIH-funded multicenter study Acute Pharmacotherapy of Late-Life Mania (GERI-BD) assessed various clinical domains before and during mood stabilizer treatment in older adults participating in a 9-week, double-blind randomized controlled trial. We describe the rationale for selecting these instruments. METHODS: Domains and instruments were selected on the basis of the study design and the participants...
May 22, 2017: International Journal of Geriatric Psychiatry
https://www.readbyqxmd.com/read/28542146/the-role-of-extracellular-histone-in-organ-injury
#5
REVIEW
Eleanor Silk, Hailin Zhao, Hao Weng, Daqing Ma
Histones are intra-nuclear cationic proteins that are present in all eukaryotic cells and are highly conserved across species. Within the nucleus, they provide structural stability to chromatin and regulate gene expression. Histone may be released into the extracellular space in three forms: freely, as a DNA-bound nucleosome or as part of neutrophil extracellular traps, and all three can be detected in serum after significant cellular death such as sepsis, trauma, ischaemia/reperfusion injury and autoimmune disease...
May 25, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28541524/metal-bound-clamp-tag-inhibits-proteolytic-cleavage
#6
Michaela L McNiff, Jennifer S Chadwick
Biologics can be an improvement to small molecule drugs, providing high specificity for an identified target, lowering toxicity and limiting side effects. To achieve effective delivery, the biologic must have sufficient time to reach the target tissue. A prolonged half-life in the circulating environment is desired, but often serum stability is limited by proteases. Proteolysis in the serum causes degradation and inactivation as the biologic is fragmented and more rapidly cleared from the body. To improve the circulating half-life, large, hydrophilic polymers may be conjugated or stable fusion tags may be engineered to increase the effective size of the peptide and to hinder degradation by proteases...
May 25, 2017: Protein Engineering, Design & Selection: PEDS
https://www.readbyqxmd.com/read/28541292/long-range-allosteric-regulation-of-the-human-26s-proteasome-by-20s-proteasome-targeting-cancer-drugs
#7
David Haselbach, Jil Schrader, Felix Lambrecht, Fabian Henneberg, Ashwin Chari, Holger Stark
The proteasome holoenzyme is the major non-lysosomal protease; its proteolytic activity is essential for cellular homeostasis. Thus, it is an attractive target for the development of chemotherapeutics. While the structural basis of core particle (CP) inhibitors is largely understood, their structural impact on the proteasome holoenzyme remains entirely elusive. Here, we determined the structure of the 26S proteasome with and without the inhibitor Oprozomib. Drug binding modifies the energy landscape of conformational motion in the proteasome regulatory particle (RP)...
May 25, 2017: Nature Communications
https://www.readbyqxmd.com/read/28541029/homochiral-mof-as-circular-dichroism-sensor-for-enantioselective-recognition-on-nature-and-chirality-of-unmodified-amino-acids
#8
Yan-Wu Zhao, Yan Wang, Xian-Ming Zhang
Self-assembly of zinc salt with rationally designed chiral ligand, (1R,2R)-2-(pyridine-4-yl carbamoyl) cyclohexanecarboxylic acid (RR-PCCH) generated 2D homochiral metal-organic framework [Zn(RR-PCCHC)2] (HMOF-1) that is composed of DNA-like right-handed double-helix structure. HMOF-1 shows high solvent and thermal stability and is also stable in neutral, weak acidic and weak basic aqueous solution. Emulsified HMOF-1 shows strong inherent circular dichroism (CD) signal in aqueous solution, which can show regular intensity change by induction of amino acids...
May 25, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28540656/nalmefene-in-alcohol-use-disorder-subjects-with-psychiatric-comorbidity-a-naturalistic-study
#9
Marco Di Nicola, Sergio De Filippis, Giovanni Martinotti, Luisa De Risio, Mauro Pettorruso, Simone De Persis, Angelo Giovanni Icro Maremmani, Icro Maremmani, Massimo di Giannantonio, Luigi Janiri
INTRODUCTION: Nalmefene is the first drug to be approved for reducing alcohol consumption in alcohol use disorder (AUD) patients at high drinking risk. In real-world settings, there is a high prevalence of concurrent psychiatric disorders in AUD subjects, with associated increased morbidity and worse prognosis. This study evaluated the use of nalmefene in AUD patients with stabilized psychiatric comorbidity previously treated unsuccessfully for alcohol dependence, and assessed craving reduction and safety...
May 24, 2017: Advances in Therapy
https://www.readbyqxmd.com/read/28540352/dataset-on-galanin-receptor-3-mutants-that-improve-recombinant-receptor-expression-and-stability-in-an-agonist-and-antagonist-bound-form
#10
Thao T Ho, Jasmine T Nguyen, Juping Liu, Pawel Stanczak, Aaron A Thompson, Yingzhuo G Yan, Jasmine Chen, Charles K Allerston, Charles L Dillard, Hao Xu, Nicholas J Shoger, Jill S Cameron, Mark E Massari, Kathleen Aertgeerts
Galanin Receptor 3 (GALR3) is a G-protein-coupled receptor with a widespread distribution in the brain and plays a role in a variety of physiologic processes including cognition/memory, sensory/pain processing, hormone secretion, and feeding behavior. Therefore, GALR3 is considered an attractive CNS drug target (Freimann et al., 2015) [1]. This dataset contains GALR3 point mutants that improve recombinant protein expression and thermal stability of the receptor contained in virus-like particles (VLPs) or obtained by detergent-purification of baculovirus-infected insect cells...
June 2017: Data in Brief
https://www.readbyqxmd.com/read/28539620/a-core-extended-naphtalene-diimide-g-quadruplex-ligand-potently-inhibits-herpes-simplex-virus-1-replication
#11
Sara Callegaro, Rosalba Perrone, Matteo Scalabrin, Filippo Doria, Giorgio Palù, Sara N Richter
G-quadruplexes (G4s) are nucleic acids secondary structures, epigenetic regulators in cells and viruses. In herpes simplex virus 1 (HSV-1)-infected cells, G4s are massively present during viral replication. We here aimed at investigating the possibility to target the HSV-1 G4s by a core extended naphtalene diimide (c-exNDI) G4 ligand. Biophysical and biomolecular analysis proved that c-exNDI stabilized the HSV-1 G4s in a concentration dependent manner. In MS competition assays, c-exNDI preferentially recognized HSV-1 G4s over cellular telomeric G4s, the most represented G4s within cells; other less abundant cellular G4s were also recognized...
May 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28539444/improved-prefusion-stability-optimized-codon-usage-and-augmented-virion-packaging-enhance-the-immunogenicity-of-respiratory-syncytial-virus-rsv-fusion-protein-in-a-vectored-vaccine-candidate
#12
Bo Liang, Joan O Ngwuta, Sonja Surman, Barbora Kabatova, Xiang Liu, Matthias Lingemann, Xueqiao Liu, Lijuan Yang, Richard Herbert, Joanna Swerczek, Man Chen, Syed M Moin, Azad Kumar, Jason S McLellan, Peter D Kwong, Barney S Graham, Peter L Collins, Shirin Munir
Respiratory syncytial virus (RSV) is the most important viral agent of severe pediatric respiratory tract disease worldwide, but lacks a licensed vaccine or suitable antiviral drug. A live-attenuated chimeric bovine/human parainfluenza virus type-3 (rB/HPIV3) was developed previously as a vector expressing RSV fusion (F) protein to confer bivalent protection against RSV and HPIV3. In a previous clinical trial in virus-naïve children, rB/HPIV3 was well-tolerated but the immunogenicity of wildtype RSV F was unsatisfactory...
May 24, 2017: Journal of Virology
https://www.readbyqxmd.com/read/28539272/selenium-nanoparticles-as-versatile-carriers-for-oral-delivery-of-insulin-insight-into-the-synergic-antidiabetic-effect-and-mechanism
#13
Wenji Deng, Qian Xie, Huan Wang, Zhiguo Ma, Baojian Wu, Xingwang Zhang
Oral insulin delivery has been plagued by limited bioavailability. This work reports selenium nanoparticles (SeNPs) for oral insulin delivery to overcome the absorption barrier. Insulin-loaded SeNPs (INS-SeNPs) were fabricated by ionic cross-linking/in situ reduction and characterized by particle size and drug entrapment. The resultant INS-SeNPs were 120nm around in particle size with high drug loading. INS-SeNPs exhibited controllable insulin release and outstanding stability in the digestive fluids. INS-SeNPs caused a significant hypoglycemic effect in both normal and diabetic rats...
May 21, 2017: Nanomedicine: Nanotechnology, Biology, and Medicine
https://www.readbyqxmd.com/read/28539250/target-residence-time-guided-optimization-on-ttk-kinase-results-in-inhibitors-with-potent-anti-proliferative-activity
#14
Joost C M Uitdehaag, Jos de Man, Nicole Willemsen-Seegers, Martine B W Prinsen, Marion A A Libouban, Jan Gerard Sterrenburg, Joeri J P de Wit, Judith R F de Vetter, Jeroen A D M de Roos, Rogier C Buijsman, Guido J R Zaman
The protein kinase TTK (Mps1) is a critical component of the spindle assembly checkpoint and a promising drug target for treatment of aggressive cancers, such as triple negative breast cancer. While the first TTK inhibitors have entered clinical trials, little is known about how the inhibition of TTK with small molecule compounds affects cellular activity. We studied the selective TTK inhibitor NTRC 0066-0, which was developed in our own laboratory, together with eleven TTK inhibitors developed by other companies, including Mps-BAY2b, BAY 1161909, BAY 1217389 (Bayer), TC-Mps1-12 (Shionogi), and MPI-0479605 (Myrexis)...
May 21, 2017: Journal of Molecular Biology
https://www.readbyqxmd.com/read/28538693/preparation-characterization-and-antioxidant-activity-evaluation-of-liposomes-containing-water-soluble-hydroxytyrosol-from-olive
#15
Jiao-Jiao Yuan, Frank G F Qin, Jun-Ling Tu, Bing Li
Due to the multiple hydroxyl groups in its structure, hydroxytyrosol (HT) is very sensitive to air and light and has very strong instability and hydrophilicity that affect its biological activity. This study attempted to prepare liposomes containing water-soluble HT to improve the bioavailability and biocompatibility of the target drug. The preparation process factors (temperature, mass ratio of phospholipid (PL) and cholesterol (CH), Tween-80 volume, HT mass) were studied and response surface methodology (RSM) was applied to optimize the conditions...
May 24, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28536795/exploration-of-alginates-as-potential-stabilizers-of-nanosuspension
#16
Jian Guan, Yeli Zhang, Qiaoyu Liu, Xin Zhang, Rina Chokshi, Shirui Mao
The objective of this study was to explore the feasibility of using alginate as a potential stabilizer of nanosuspension and elaborate the corresponding stabilization mechanism. Using lovastatin as a Biopharmaceutics Classification System (BCS) II drug model, alginate-stabilized nanosuspension was fabricated by the high-pressure homogenization method. The particle size, zeta potential, short-term stability, and dissolution behavior of the nanosuspension were characterized. Thereafter, the surface morphology, crystallinity, redispersability, and stability of the spray-dried nanosuspension were investigated...
May 23, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28536655/supporting-looked-after-children-and-care-leavers-in-decreasing-drugs-and-alcohol-solid-protocol-for-a-pilot-feasibility-randomised-controlled-trial-of-interventions-to-decrease-risky-substance-use-drugs-and-alcohol-and-improve-mental-health-of-looked-after
#17
Hayley Alderson, Ruth McGovern, Rebecca Brown, Denise Howel, Frauke Becker, Louise Carr, Alex Copello, Tony Fouweather, Eileen Kaner, Paul McArdle, Elaine McColl, Janet Shucksmith, Alison Steele, Luke Vale, Raghu Lingam
BACKGROUND: Looked after children (LAC) and care leavers are young people who have been placed under the legal care of local authorities, in many instances due to a history of abuse and/or neglect. These young people have a significantly increased risk of substance use and mental disorder compared to their peers. The aim of the SOLID study is to assess the feasibility and acceptability of a definitive three-arm multi-centre randomised controlled trial (RCT) that compares the effectiveness of two interventions that aim to reduce risky drug and alcohol use and improve mental health among LAC aged 12 to 20 years with usual care...
2017: Pilot and Feasibility Studies
https://www.readbyqxmd.com/read/28536462/surface-pegylation-of-mesoporous-silica-nanorods-msnr-effect-on-loading-release-and-delivery-of-mitoxantrone-in-hypoxic-cancer-cells
#18
Amit Wani, Galbokka H Layan Savithra, Ayat Abyad, Shrey Kanvinde, Jing Li, Stephanie Brock, David Oupický
Mesoporous silica nanomaterials show great potential to deliver chemotherapeutics for cancer treatment. The key challenges in the development of injectable mesoporous silica formulations are colloidal instability, hemolysis and inefficient drug loading and release. In this study, we evaluated the effect of PEGylation of mesoporous silica nanorods (MSNR) on hemolysis, colloidal stability, mitoxantrone (MTX) loading, in vitro MTX release, and cellular MTX delivery under hypoxic conditions. We found that PEGylation prevented dose-dependent hemolysis in the concentrations studied (0-10 mg/ml) and improved colloidal stability of MSNR...
May 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28536446/preparation-characterization-and-pharmacokinetics-of-cyadox-nanosuspension
#19
Adeel Sattar, Dongmei Chen, Lishun Jiang, Yuanhu Pan, Yanfei Tao, Lingli Huang, Zhenli Liu, Shuyu Xie, Zonghui Yuan
An increase in number of newly developed synthetic drugs displays bioavailability constraints because of poor water solubility. Nanosuspensions formulation may help to overwhelm these problems by increasing dissolution velocity and saturation solubility. In the present study, cyadox (Cyx) nanosuspension was successfully prepared by recrystallization based on acid-base neutralization combined with high pressure homogenization method using Polyvinylpyrrolidone K30 (PVP) as stabilizer. The nanosuspension had uniform particle distribution, excellent sedimentation rate and redispersibility...
May 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28536023/development-of-long-circulating-docetaxel-loaded-poly-3-hydroxybutyrate-co-3-hydroxyvalerate-nanoparticles-optimization-pharmacokinetic-cytotoxicity-and-in-vivo-assessments
#20
Harsh Vardhan, Pooja Mittal, Sandeep K Reddy Adena, Mansi Upadhyay, Brahmeshwar Mishra
Long-circulating Nanoparticles (NPs) are promising drug delivery vehicles which target solid tumors via enhanced permeation and retention effect. Plackett-Burman (PBD) and Box-Behnken (BBD) designs were adopted to study the effects of factors viz. polymer concentration, surfactant concentration, homogenizer speed, homogenization time and ultrasonication time on responses. A graphical and numerical optimization technique was used to obtain predicted value of the response. The drug entrapment efficiency was approximately 39±0...
May 20, 2017: International Journal of Biological Macromolecules
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