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https://www.readbyqxmd.com/read/28528314/development-of-a-macroporous-ceramic-passive-sampler-for-the-monitoring-of-cytostatic-drugs-in-water
#1
Helena Franquet-Griell, Victor Pueyo, Jorge Silva, Victor M Orera, Silvia Lacorte
The aim of this study was to develop and calibrate a macroporous ceramic passive sampler (MCPS) for the monitoring of anticancer drugs in wastewater. This system was designed by the Spanish Research Council (CSIC) and consists in a porous ceramic tube to allow a high diffusion of contaminants. The MCPS has been calibrated for 16 cytostatic drugs over time periods up to 9 d in spiked water under controlled laboratory conditions. Optimal uptake was accomplished for 7 compounds, namely ifosfamide, cyclophosphamide, capecitabine, prednisone, megestrol, cyproterone and mycophenolic acid, whereas cytarabine was not adsorbed in the receiving phase and the rest were hydrolyzed over the deployment period...
May 11, 2017: Chemosphere
https://www.readbyqxmd.com/read/28528286/assessing-the-stable-conformations-of-ibuprofen-in-solution-by-means-of-residual-dipolar-couplings
#2
Maria Enrica Di Pietro, Giorgio Celebre, Christie Aroulanda, Denis Merlet, Giuseppina De Luca
Detailing the conformational equilibria between global and local minimum energy structures of anti-inflammatory α-arylpropionic acids directly in solution is of the utmost importance for a better understanding of the structure-activity relationships, hence providing valuable clues for rational structure-based drug design studies. Here the conformational preferences of the widely used pharmaceutical ibuprofen were investigated in solution by NMR spectroscopy in weakly ordering phases. A thorough theoretical treatment of the anisotropic interactions that are relevant for NMR spectra led to a conformational model characterized by six pairs of symmetry-related conformers, in particular four couples of gauche structures, with a total probability of 93%, and 2 couples of trans structures, counting for the remaining 7%...
May 17, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28528258/epidemiology-and-management-of-chronic-thromboembolic-pulmonary-hypertension-experience-from-two-expert-centers
#3
Maria Anna Bazmpani, Alexandra Arvanitaki, Maria Toumpourleka, Georgia Pitsiou, Evaggelia Panagiotidou, Sophia Anastasia Mouratoglou, Georgios Sianos, Stavros Hadjimiltiades, Antonios Pitsis, Eckhard Mayer, Ioannis Stanopoulos, Haralambos Karvounis, George Giannakoulas
BACKGROUND: Chronic thromboembolic pulmonary hypertension (CTEPH) is a rare, distinct pulmonary vascular disease, and, therefore, there is lack of data regarding its clinical presentation, diagnosis and management at a national basis. Our objective was to describe the demographics and management of CTEPH patients in Northern Greece. METHODS: We conducted a retrospective, observational study with a joint collaboration from two pulmonary hypertension expert centers in Greece and included patients diagnosed with CTEPH...
May 17, 2017: Hellenic Journal of Cardiology: HJC, Hellēnikē Kardiologikē Epitheōrēsē
https://www.readbyqxmd.com/read/28528134/enhancing-tumor-cell-response-to-multidrug-resistance-with-ph-sensitive-quercetin-and-doxorubicin-conjugated-multifunctional-nanoparticles
#4
Cenk Daglioglu
Classical chemotherapy uses chemotherapeutic agents as a mainstay of anticancer treatment. However, the development of multidrug resistance to chemotherapy limits the effectiveness of current cancer treatment. Nanosized bioconjugates combining a chemotherapeutic agent with a pharmacological approach may improve the curative effect of chemotherapeutic agents. Herein I addressed this issue by describing the synthesis, and testing of, pH-responsive Fe3O4@SiO2(FITC)-BTN/QUR/DOX multifunctional nanoparticles. The particles were designed to modulate resistance-mediating factors and to potentiate the efficacy of DOX against chemoresistance...
May 10, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28527736/the-effects-of-non-invasive-radiofrequency-electric-field-hyperthermia-on-biotransport-and-biodistribution-of-fluorescent-60-fullerene-derivative-in-a-murine-orthotopic-model-of-breast-adenocarcinoma
#5
Norman A Lapin, Martyna Krzykawska-Serda, Sean Dilliard, Yuri Mackeyev, Maciej Serda, Lon J Wilson, Steven A Curley, Stuart J Corr
The aim of this study is to understand the combined and differential biokinetic effects of radiofrequency (RF) electric-field hyperthermia as an adjunctive therapy to [60]fullerene nanoparticle-based drug delivery systems in targeting the micro-vasculature and micro-environments of breast cancer tumors. Intravital microscopy (IVM) is an ideal tool to provide the spatial and temporal resolution needed for quantification in this investigation. The water-soluble and fluorescent [60]fullerene derivative (C60-serPF) was designed to be an amphiphilic nanostructure, which is able to cross several biological membranes and accumulate in tumor tissues by passing through abnormally leaky tumor blood vessels...
May 17, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28527735/advances-in-combination-therapy-of-lung-cancer-rationales-delivery-technologies-and-dosage-regimens
#6
REVIEW
Lan Wu, Donglei Leng, Dongmei Cun, Camilla Foged, Mingshi Yang
Lung cancer is a complex disease caused by a multitude of genetic and environmental factors. The progression of lung cancer involves dynamic changes in the genome and a complex network of interactions between cancer cells with multiple, distinct cell types that form tumors. Combination therapy using different pharmaceuticals has been proven highly effective due to the ability to affect multiple cellular pathways involved in the disease progression. However, the currently used drug combination designs are primarily based on empirical clinical studies, and little attention has been given to dosage regimens, i...
May 17, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28527581/nuclear-receptors-in-skeletal-homeostasis
#7
Hao Zuo, Yihong Wan
Nuclear receptors are a family of transcription factors that can be activated by lipophilic ligands. They are fundamental regulators of development, reproduction, and energy metabolism. In bone, nuclear receptors enable bone cells, including osteoblasts, osteoclasts, and osteocytes, to sense their dynamic microenvironment and maintain normal bone development and remodeling. Our views of the molecular mechanisms in this process have advanced greatly in the past decade. Drugs targeting nuclear receptors are widely used in the clinic for treating patients with bone disorders such as osteoporosis by modulating bone formation and resorption rates...
2017: Current Topics in Developmental Biology
https://www.readbyqxmd.com/read/28527405/synthesis-and-structure-activity-relationships-of-novel-fused-ring-analogues-of-q203-as-antitubercular-agents
#8
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/28527243/-synthesis-of-antibiotic-loaded-polylactic-acid-nanoparticles-and-their-antibacterial-activity-against-escherichia-coli-o157-h7-and-methicillin-resistant-staphylococcus-aureus
#9
Mónica Tatiana Herrera, Jhon Jhamilton Artunduaga, Claudia Cristina Ortiz, Rodrigo Gonzalo Torres
INTRODUCTION: Polymeric nanoparticles are promising nanotechnology tools to fight pathogenic bacteria resistant to conventional antibiotics. OBJECTIVE: To synthesize polylactic acid nanoparticles loaded with ofloxacin and vancomycin, and to determine their antibacterial activity against Escherichia coli O157:H7 and methicillin-resistant Staphylococcus aureus (MRSA). MATERIALS AND METHODS: We synthesized ofloxacin or vancomycin loaded polylactic acid nanoparticles by the emulsification-solvent evaporation method, and characterized them by dynamic light scattering, laser Doppler electrophoresis and scanning electron microscopy...
January 24, 2017: Biomédica: Revista del Instituto Nacional de Salud
https://www.readbyqxmd.com/read/28527032/methylone-and-mdpv-activate-autophagy-in-human-dopaminergic-sh-sy5y-cells-a-new-insight-into-the-context-of-%C3%AE-keto-amphetamines-related-neurotoxicity
#10
Maria João Valente, Cristina Amaral, Georgina Correia-da-Silva, José Alberto Duarte, Maria de Lourdes Bastos, Félix Carvalho, Paula Guedes de Pinho, Márcia Carvalho
Autophagy has an essential role in neuronal homeostasis and its dysregulation has been recently linked to neurotoxic effects of a growing list of psychoactive drugs, including amphetamines. However, the role of autophagy in β-keto amphetamine (β-KA) designer drugs-induced neurotoxicity has hitherto not been investigated. In the present study, we show that two commonly abused cathinone derivatives, 3,4-methylenedioxymethcathinone (methylone) and 3,4-methylenedioxypyrovalerone (MDPV), elicit morphological changes consistent with autophagy and neurodegeneration, including formation of autophagic vacuoles and neurite retraction in dopaminergic SH-SY5Y cells...
May 19, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/28526943/a-global-reference-comparator-for-biosimilar-development
#11
Christopher J Webster, Gillian R Woollett
Major drug regulators have indicated in guidance their flexibility to accept some development data for biosimilars generated with reference product versions licensed outside their own jurisdictions, but most authorities require new bridging studies between these versions and the versions of them licensed locally. The costs of these studies are not trivial in absolute terms and, due to the multiplier effect of required repetition by each biosimilar sponsor, their collective costs are substantial. Yet versions of biologics licensed in different jurisdictions usually share the same development data, and any manufacturing changes between versions have been justified by a rigorous comparability process...
May 19, 2017: BioDrugs: Clinical Immunotherapeutics, Biopharmaceuticals and Gene Therapy
https://www.readbyqxmd.com/read/28526884/combined-use-of-metformin-and-atorvastatin-attenuates-atherosclerosis-in-rabbits-fed-a-high-cholesterol-diet
#12
Fei Luo, Yuan Guo, Gui-Yun Ruan, Jun-Ke Long, Xi-Long Zheng, Qin Xia, Shui-Ping Zhao, Dao-Quan Peng, Zhen-Fei Fang, Xiang-Ping Li
Statins are widely used to reduce cardiovascular risk. Unfortunately, some patients still experience cardiovascular events though prescribed with high-intensity statins. Metformin, an anti-diabetic drug, was reported to possess anti-atherosclerotic effects. Therefore, the experiments were designed to evaluate whether combined use of metformin and atorvastatin can achieve additional benefits. In rabbits fed a high-cholesterol diet, we evaluated the effects of the combination therapy on atherosclerotic plaques, lipid profiles, blood glucose levels, liver and kidney functions...
May 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28526744/combining-properties-of-different-classes-of-pi3k%C3%AE-inhibitors-to-understand-molecular-features-that-confer-selectivity
#13
Grace Q Gong, Jackie D Kendall, James Mj Dickson, Gordon W Rewcastle, Christina M Buchanan, William A Denny, Peter R Shepherd, Jack U Flanagan
Phosphoinositide 3-kinases (PI3K) are major regulators of many cellular functions, and hyperactivation of PI3K cell signalling pathways is a major target for anticancer drug discovery. PI3Kα is the isoform most implicated in cancer, and our aim is to selectively inhibit this isoform, which may be more beneficial than concurrent inhibition of all Class I PI3Ks. We have used structure-guided design to merge high selectivity and high affinity characteristics found in existing compounds. Molecular docking including the prediction of water-mediated interactions, was used to model interactions between the ligands and the PI3Kα affinity pocket...
May 19, 2017: Biochemical Journal
https://www.readbyqxmd.com/read/28526743/systematic-identification-of-functional-residues-of-artemisia-annua-amorpha-4-11-diene-synthase
#14
Xin Fang, Jian-Xu Li, Jin-Quan Huang, You-Li Xiao, Peng Zhang, Xiao-Ya Chen
Terpene synthases (TPSs) are responsible for the extremely diversified and complex structure of terpenoids. Amorpha-4,11-diene synthase (ADS) has a high (90%) fidelity in generating the sesquiterpene precursor for biosynthesis of artemisinin, an antimalarial drug, however, little is known about how active site residues of ADS involved in the carbocation rearrangement and cyclization reactions. Here, we identify seven residues that are key to most of the catalytic steps in ADS. By structural modeling and amino acid sequence alignments of ADS with two functionally relevant sesquiterpene synthases from Artemisia annua, we performed site-directed mutagenesis and found that a single substitution, T296V, impaired the ring closure activity almost completely, and tetra-substitutions (L374Y/L404V/L405I/G439S) led to an enzyme generating 80% monocyclic bisabolyl-type sesquiterpenes, whereas a double mutant (T399L/T447G) showed compromised activity in regioselective deprotonation to yield 34...
May 19, 2017: Biochemical Journal
https://www.readbyqxmd.com/read/28526591/macrophage-based-therapeutic-strategies-in-regenerative-medicine
#15
Kara L Spiller, Timothy J Koh
Mounting evidence suggests that therapeutic cell and drug delivery strategies designed to actively harness the regenerative potential of the inflammatory response have great potential in regenerative medicine. In particular, macrophages have emerged as a primary target because of their critical roles in regulating multiple phases of tissue repair through their unique ability to rapidly shift phenotypes. Herein, we review macrophage-based therapies, focusing on the translational potential for cell delivery of ex vivo-activated macrophages and delivery of molecules and biomaterials to modulate accumulation and phenotype of endogenous macrophages...
May 16, 2017: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/28526350/designing-novel-bioconjugates-of-hydroxyethylcellulose-and-salicylates-for-potential-pharmaceutical-and-pharmacological-applications
#16
Khawar Abbas, Muhammad Amin, Muhammad Ajaz Hussain, Muhammad Sher, Syed Nasir Abbas Bukhari, Ibrahim Jantan, Kevin J Edgar
The present study deals with fabrication of macromolecular prodrugs (MPDs) of salicylic acid (SA) and aspirin (ASP) based on a hydrophilic cellulose ether, hydroxyethylcellulose (HEC). Degrees of substitution (DS) of SA and ASP per HEC repeating unit (HEC-RU) were achieved ranging from 0.60-2.18 and 0.53-1.50, respectively. The amphiphilic HEC-SA conjugate 2 assembled into nanowire-like structures, while HEC-ASP conjugate 6 formed nanoparticles (diameter 300-700nm) at a water/DMSO interface. After oral administration in rabbit models, conjugates 2 and 6 showed plasma half-life of 6...
May 16, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28526046/balloon-versus-stenting-in-severe-ischaemia-of-the-leg-3-basil-3-study-protocol-for-a-randomised-controlled-trial
#17
Benjamin D Hunt, Matthew A Popplewell, Huw Davies, Lewis Meecham, Hugh Jarrett, Gareth Bate, Margaret Grant, Smitaa Patel, Catherine Hewitt, Lazaros Andronis, Jonathan J Deeks, Andrew Bradbury
BACKGROUND: Severe limb ischaemia (SLI) is defined as the presence of rest pain and/or tissue loss secondary to lower extremity atherosclerotic peripheral arterial disease. The superficial femoral and popliteal arteries are the most commonly diseased vessels in such patients and are being increasingly treated using endovascular revascularisation techniques. However, it is currently unknown whether drug-eluting stents and drug-coated balloons confer additional clinical benefits over more established techniques using plain balloons and bare metal stents, or whether they represent a cost-effective use of NHS resources...
May 19, 2017: Trials
https://www.readbyqxmd.com/read/28526024/protective-effect-on-the-coronary-microcirculation-of-patients-with-diabetes-by-clopidogrel-or-ticagrelor-predict-study-rationale-and-design-a-randomized-multicenter-clinical-trial-using-intracoronary-multimodal-physiology
#18
Enrico Cerrato, Alicia Quirós, Mauro Echavarría-Pinto, Hernan Mejia-Renteria, Andres Aldazabal, Nicola Ryan, Nieves Gonzalo, Pilar Jimenez-Quevedo, Luis Nombela-Franco, Pablo Salinas, Iván J Núñez-Gil, José Ramón Rumoroso, Antonio Fernández-Ortiz, Carlos Macaya, Javier Escaned
BACKGROUND: In diabetic patients a predisposed coronary microcirculation along with a higher risk of distal particulate embolization during primary percutaneous intervention (PCI) increases the risk of peri-procedural microcirculatory damage. However, new antiplatelet agents, in particular Ticagrelor, may protect the microcirculation through its adenosine-mediated vasodilatory effects. METHODS: PREDICT is an original, prospective, randomized, multicenter controlled study designed to investigate the protective effect of Ticagrelor on the microcirculation during PCI in patient with diabetes mellitus type 2 or pre-diabetic status...
May 19, 2017: Cardiovascular Diabetology
https://www.readbyqxmd.com/read/28525914/cigarette-filter-ventilation-and-its-relationship-to-increasing-rates-of-lung-adenocarcinoma
#19
Min-Ae Song, Neal L Benowitz, Micah Berman, Theodore M Brasky, K Michael Cummings, Dorothy K Hatsukami, Catalin Marian, Richard O'Connor, Vaughan W Rees, Casper Woroszylo, Peter G Shields
The 2014 Surgeon General's Report on smoking and health concluded that changing cigarette designs have caused an increase in lung adenocarcinomas, implicating cigarette filter ventilation that lowers smoking machine tar yields. The Food and Drug Administration (FDA) now has the authority to regulate cigarette design if doing so would improve public health. To support a potential regulatory action, two weight-of-evidence reviews were applied for causally relating filter ventilation to lung adenocarcinoma. Published scientific literature (3284 citations) and internal tobacco company documents contributed to causation analysis evidence blocks and the identification of research gaps...
December 1, 2017: Journal of the National Cancer Institute
https://www.readbyqxmd.com/read/28525838/design-synthesis-and-evaluation-of-azaacridine-derivatives-as-dual-target-egfr-and-src-kinase-inhibitors-for-antitumor-treatment
#20
Zhishan Cui, Shaopeng Chen, Yanwei Wang, Chunmei Gao, Yuzong Chen, Chunyan Tan, Yuyang Jiang
Overexpression of EGFR is often associated with advanced stage disease and poor prognosis. In certain cancers, Src works synergistically with EGFR to promote proliferation, survival, invasion and metastasis. Development of dual-target drugs against EGFR and Src is of therapeutic advantage against these cancers. Based on molecular docking and our previous studies, we rationally designed a new series of azaacridine derivatives as potent EGFR and Src dual inhibitors. Most of the synthesized azaacridines displayed good antiproliferative activity against K562 and A549 cells...
May 11, 2017: European Journal of Medicinal Chemistry
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