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https://www.readbyqxmd.com/read/27914363/new-insights-into-the-sar-and-drug-combination-synergy-of-2-quinolin-4-yloxy-acetamides-against-mycobacterium-tuberculosis
#1
Bruno Couto Giacobbo, Kenia Pissinate, Valnês Rodrigues-Junior, Anne Drumond Villela, Estêvão Silveira Grams, Bruno Lopes Abbadi, Fernanda Teixeira Subtil, Nathalia Sperotto, Rogério Valim Trindade, Davi Fernando Back, Maria Martha Campos, Luiz Augusto Basso, Pablo Machado, Diógenes Santiago Santos
2-(Quinolin-4-yloxy)acetamides have been described as potent and selective in vitro inhibitors of Mycobacterium tuberculosis (Mtb) growth. Herein, a new series of optimized compounds were found to demonstrate highly potent antitubercular activity, with minimum inhibitory concentration (MIC) values against drug-susceptible and drug-resistant Mycobacterium tuberculosis strains in the submicromolar range. Furthermore, the most active compounds had no apparent toxicity to mammalian cells, and they showed intracellular activities similar to those of isoniazid and rifampin in a macrophage model of Mtb infection...
November 23, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27914361/development-of-cxcr4-modulators-by-virtual-hts-of-a-novel-amide-sulfamide-compound-library
#2
Renren Bai, Qi Shi, Zhongxing Liang, Younghyoun Yoon, Yiran Han, Amber Feng, Shuangping Liu, Yoonhyeun Oum, C Chris Yun, Hyunsuk Shim
CXCR4 plays a crucial role in recruitment of inflammatory cells to inflammation sites at the beginning of the disease process. Modulating CXCR4 functions presents a new avenue for anti-inflammatory strategies. However, using CXCR4 antagonists for a long term usage presents potential serious side effect due to their stem cell mobilizing property. We have been developing partial CXCR4 antagonists without such property. A new computer-aided drug design program, the FRESH workflow, was used for anti-CXCR4 lead compound discovery and optimization, which coupled both compound library building and CXCR4 docking screens in one campaign...
November 24, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27914352/searching-for-novel-modes-of-toxic-actions-of-oil-spill-using-e-%C3%A2-coli-live-cell-array-reporter-system-a-hebei-spirit-oil-spill-study
#3
Dawoon Jung, Miao Guan, Sangwoo Lee, Cheolmin Kim, Hyesoo Shin, Seongjin Hong, Un Hyuk Yim, Won Joon Shim, John P Giesy, Jong Seong Khim, Xiaowei Zhang, Kyungho Choi
Oil is a complex mixture of numerous compounds. Therefore, oil spills near shore can cause various adverse effects on coastal ecosystems. However, most toxicological assessments conducted on oil spill sites have focused on limited modes of toxic actions. In the present study, we utilized the Escherichia coli (E. coli) live cell array system (LCA) to identify novel modes of toxicities of the oil spill-affected sediments. For this purpose, sediment samples were collected from an area heavily polluted by Hebei Spirit oil spill (HSOS) incident of 2007...
November 30, 2016: Chemosphere
https://www.readbyqxmd.com/read/27914343/fluorescence-and-drug-loading-properties-of-znse-mn-zns-paclitaxel-sio2-nanocapsules-templated-by-f127-micelles
#4
Tingting Zhao, Xin Liu, Yuebin Li, Mingguang Zhang, Jian He, Xuewen Zhang, Hui Liu, Xingguo Wang, Haoshuang Gu
Hydrophobic ZnSe:Mn/ZnS core-shell fluorescence quantum dots (QDs) and anticancer drug paclitaxel (PTX) have been co-loaded into folate conjugated hybrid silica nanocapsules via F127 micelles based soft-template method in a mild aqueous environment at room temperature. The encapsulation of QDs shows a F127: QDs mass ratio dependent behavior, which impact much on the morphology and optical properties of composite nanocapsules. These as prepared composite nanocapsules also exhibit good photoluminescence stability under the temperature ranges from 19°C to 49°C...
November 23, 2016: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/27914336/thermoresponsive-supramolecular-micellar-drug-delivery-system-based-on-star-linear-pseudo-block-polymer-consisting-of-%C3%AE-cyclodextrin-poly-n-isopropylacrylamide-and-adamantyl-poly-ethylene-glycol
#5
Xia Song, Jing-Ling Zhu, Yuting Wen, Feng Zhao, Zhong-Xing Zhang, Jun Li
Chemotherapy is facing several limitations such as low water solubility of anticancer drugs and multidrug resistance (MDR) in cancer cells. To overcome these limitations, a thermoresponsive micellar drug delivery system formed by a non-covalently connected supramolecular block polymer was developed. The system is based on the host-guest interaction between a well-defined β-cyclodextrin (β-CD) based poly(N-isopropylacrylamide) star host polymer and an adamantyl-containing poly(ethylene glycol) (Ad-PEG) guest polymer...
November 16, 2016: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/27914333/nano-zinc-oxide-incorporated-graphene-oxide-nanocellulose-composite-for-the-adsorption-and-photo-catalytic-degradation-of-ciprofloxacin-hydrochloride-from-aqueous-solutions
#6
T S Anirudhan, J R Deepa
Purpose of this study is to report the synthetic procedure of a novel photo catalyst, nano zinc oxide incorporated graphene oxide/nanocellulose (ZnO-GO/NC) for the effective adsorption and subsequent photo degradation of ciprofloxacin (CF), an antibiotic widely used in the poultry. Self cleaning property in cellulose was achieved by introducing a nano zinc oxide incorporated graphene oxide into nanocellulose (NC) matrix. By incorporating nano zinc oxide (ZnO) in graphene oxide (GO), band gap could be tuned to 2...
November 17, 2016: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/27914328/synthesis-and-stability-of-ir-820-and-fitc-doped-silica-nanoparticles
#7
Atul V Thorat, Tandra Ghoshal, Lan Chen, Justin D Holmes, Michael A Morris
Fluorescent silica nanoparticles (NPs) have potential in biomedical applications as diagnostics and traceable drug delivery agents. In this study, we have synthesized fluorescent dye grafted silica NPs in two step process. First, a stable method to synthesize various sizes of silica NPs ranging from 20 to 52, 95, 210 and 410nm have been successfully demonstrated. Secondly, as-synthesized silica NPs are readily grafted with some fluorescent dyes like IR-820 and fluorescein isothiocyanate (FITC) dyes by simple impregnation method...
November 15, 2016: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/27914325/fabrication-of-metronidazole-loaded-poly-%C3%AE%C2%B5-caprolactone-zein-core-shell-nanofiber-membranes-via-coaxial-electrospinning-for-guided-tissue-regeneration
#8
Min He, Huiyi Jiang, Rui Wang, Yi Xie, Changsheng Zhao
To develop a biologically mimetic guided tissue regeneration (GTR) membrane with localized sustained drug release function to prevent infection, coaxial electrospinning technique was conducted to fabricate metronidazole (MNA)-loaded poly (ε-caprolactone) (PCL)/zein core/shell nanofibers. The nanofibers displayed a uniform bead-free round morphology as observed by scanning electron microscopy (SEM), and a core/shell structure as confirmed by transmission electron microscopy (TEM). X-ray diffraction (XRD) and differential scanning calorimetry (DSC) characterizations demonstrated that the MNA was well dispersed in the nanofibers matrix...
November 19, 2016: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/27914299/the-effects-of-fluorine-substitution-on-the-chemical-properties-and-inhibitory-capacity-of-donepezil-anti-alzheimer-drug-density-functional-theory-and-molecular-docking-calculations
#9
Azita Khosravan, Safora Marani, Mohammad Sadegh Sadeghi Googheri
Drug fluorination has the potential to reproduce useful drugs with decreasing the side effect of them. Identifying the effect of this improvement on the chemical properties and biological interactions of drug symbolizes a meaningful progress in drug design. Here the fluorination of Donepezil as an anti-Alzheimer drug, including 7 fluorinated derivatives of it, was investigated computationally. In the first part of our calculations, the most important chemical properties of drug that affects the drug efficiency were investigated by applying the M06/6-31g (d, p) and M062X/6-31g (d, p) levels of theories...
November 25, 2016: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/27914294/selective-agonism-of-mglu8-receptors-by-s-3-4-dicarboxyphenylglycine-does-not-affect-sleep-stages-in-the-rat
#10
María Cavas, Gianluigi Scesa, Mercedes Martín-López, José Francisco Navarro
BACKGROUND: Metabotropic glutamate receptors (mGlu) play a role in a number of physiological processes and behaviors, as well as in certain pathological conditions and diseases. New drugs targetting mGlu receptors are being developed with treatment purposes. Recent data indicates that glutamate is involved in sleep, and pharmacological manipulation of distinct subtypes of mGlu receptors affect sleep. Here the consequences of selective pharmacological agonism of mGlu8 receptor upon sleep and wakefulness are explored for the first time...
September 22, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27914279/identification-and-quantification-of-4-methylethcathinone-4-mec-and-3-4-methylenedioxypyrovalerone-mdpv-in-hair-by-lc-ms-ms-after-chronic-administration
#11
Jean Claude Alvarez, Isabelle Etting, Emuri Abe, Antoine Villa, Nicolas Fabresse
4-Methylethcathinone (4-MEC) and 3,4-methylenedioxypyrovalerone (MDPV) are synthetic cathinones. The objective of this study was to develop a method in order to measure these compounds in hair of a patient. After decontamination, 20mg of hair were grinded and incubated in phosphate buffer pH 5.0 in presence of 100ng of MDMA-d5 used as internal standard. Double basic liquid-liquid extraction was performed. Samples were separated on a 1.9μm Hypersil GOLD PFP column (100×2.1mm) using gradient elution. Compounds were detected by a LCQ TSQ Vantage XP triple-quadrupole mass spectrometer...
November 24, 2016: Forensic Science International
https://www.readbyqxmd.com/read/27914270/surface-mediated-transfection-of-a-pdna-vector-encoding-short-hairpin-rna-to-downregulate-tgf-%C3%AE-1-expression-for-the-prevention-of-in-stent-restenosis
#12
He Zhang, Ke-Feng Ren, Hao Chang, Jin-Lei Wang, Jian Ji
In-stent restenosis is one of the most serious modes of failure of cardiovascular stent implant. Although drug-eluting stents have been proven to reduce in-stent restenosis, the nonspecific inhibitory effects of anti-proliferative drugs, such as rapamycin, result in delayed re-endothelialization and fatal late stent thrombosis. Although many studies have focused on promoting rapid re-endothelialization, a feasible method of reducing excessive extracellular matrix (ECM) production and cell proliferation might provide a promising way to efficiently inhibit the restenosis in vivo...
November 24, 2016: Biomaterials
https://www.readbyqxmd.com/read/27914269/targeted-hydroxyethyl-starch-prodrug-for-inhibiting-the-growth-and-metastasis-of-prostate-cancer
#13
Kaidong Zhao, Di Li, Weiguo Xu, Jianxun Ding, Weiqian Jiang, Mingqiang Li, Chunxi Wang, Xuesi Chen
Prostate cancer is one of the most prevalent malignancies among men. Although chemotherapy has been an effective therapeutic approach for treating metastatic prostate cancer, serious undesired side effects have hampered its wide application clinically. In this work, a pH-responsive LHRH-conjugated hydroxyethyl starch-doxorubicin (HES-DOX/LHRH) prodrug was facilely synthesized by conjugating oxidized HES (HES-CHO) with DOX and LHRH through an acid-sensitive Schiff base bond. The resulting prodrug spontaneously self-assembled into nanoscopic micelle with a radius of about 55 nm in an aqueous environment...
November 23, 2016: Biomaterials
https://www.readbyqxmd.com/read/27914267/intein-mediated-site-specific-synthesis-of-tumor-targeting-protein-delivery-system-turning-peg-dilemma-into-prodrug-like-feature
#14
Yingzhi Chen, Meng Zhang, Hongyue Jin, Yisi Tang, Huiyuan Wang, Qin Xu, Yaping Li, Feng Li, Yongzhuo Huang
Poor tumor-targeted and cytoplasmic delivery is a bottleneck for protein toxin-based cancer therapy. Ideally, a protein toxin drug should remain stealthy in circulation for prolonged half-life and reduced side toxicity, but turn activated at tumor. PEGylation is a solution to achieve the first goal, but creates a hurdle for the second because PEG rejects interaction between the drugs and tumor cells therein. Such PEG dilemma is an unsolved problem in protein delivery. Herein proposed is a concept of turning PEG dilemma into prodrug-like feature...
November 27, 2016: Biomaterials
https://www.readbyqxmd.com/read/27914266/skin-integrated-with-perfusable-vascular-channels-on-a-chip
#15
Nobuhito Mori, Yuya Morimoto, Shoji Takeuchi
This paper describes a method for fabricating perfusable vascular channels coated with endothelial cells within a cultured skin-equivalent by fixing it to a culture device connected to an external pump and tubes. A histological analysis showed that vascular channels were constructed in the skin-equivalent, which showed a conventional dermal/epidermal morphology, and the endothelial cells formed tight junctions on the vascular channel wall. The barrier function of the skin-equivalent was also confirmed. Cell distribution analysis indicated that the vascular channels supplied nutrition to the skin-equivalent...
November 27, 2016: Biomaterials
https://www.readbyqxmd.com/read/27914264/pattern-based-sensing-of-triple-negative-breast-cancer-cells-with-dual-ligand-cofunctionalized-gold-nanoclusters
#16
Yu Tao, Mingqiang Li, Debra T Auguste
Early detection of breast cancer is a critical component in patient prognosis and establishing effective therapy regimens. Here, we developed an easily accessible yet potentially powerful sensor to detect cancer cell targets by utilizing seven dual-ligand cofunctionalized gold nanoclusters (AuNCs) as both effective cell recognition elements and signal transducers. On the basis of this AuNC multichannel sensor, we have successfully distinguished healthy, cancerous and metastatic human breast cells with excellent reproducibility and high sensitivity...
November 25, 2016: Biomaterials
https://www.readbyqxmd.com/read/27914253/protein-conjugation-with-pamam-nanoparticles-microscopic-and-thermodynamic-analysis
#17
P Chanphai, E Froehlich, J S Mandeville, H A Tajmir-Riahi
PAMAM dendrimers form strong protein conjugates that are used in drug delivery systems. We report the thermodynamic and binding analysis of polyamidoamine (PAMAM-G4) conjugation with human serum albumin (HSA), bovine serum albumin (BSA) and milk beta-lactoglobulin (b-LG) in aqueous solution at physiological pH. Hydrophobicity played a major role in PAMAM-protein interactions with more hydrophobic b-LG forming stronger polymer-protein conjugates. Thermodynamic parameters showed PAMAM-protein bindings occur via hydrophobic and H-bonding contacts for b-LG, while van der waals and H-bonding interactions prevail in HSA and BSA-polymer conjugates...
November 27, 2016: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/27914235/hyaluronan-as-a-promising-excipient-for-ocular-drug-delivery
#18
REVIEW
Michaela Guter, Miriam Breunig
Hyaluronan (HA) is a naturally occurring polysaccharide and well known for its exceptional properties such as high biocompatibility and biodegradability, along with a low immunogenicity. Besides its use for various biomedical applications it recently came into focus as a favorable excipient for the formulation of various ocular therapeutics. This review article summarizes the ocular distribution of HA and its most heavily investigated binding protein "cluster of differentiation 44" (CD44) which is the rationale for the clinical use of HA, primarily as an additive in ocular applications ranging from eye drops to contact lenses...
November 30, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27914234/food-gastrointestinal-ph-and-models-of-oral-drug-absorption
#19
REVIEW
Ahmad Y Abuhelwa, Desmond B Williams, Richard N Upton, David J R Foster
This article reviews the major physiological and physicochemical principles of the effect of food and gastrointestinal (GI) pH on the absorption and bioavailability of oral drugs, and the various absorption models that are used to describe/predict oral drug absorption. The rate and extent of oral drug absorption is determined by a complex interaction between a drug's physicochemical properties, GI physiologic factors, and the nature of the formulation administered. GI pH is an important factor that can markedly affect oral drug absorption and bioavailability as it may have significant influence on drug dissolution & solubility, drug release, drug stability, and intestinal permeability...
November 30, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27914224/a-systematic-review-of-epileptic-seizures-in-adults-with-subdural-haematomas
#20
REVIEW
Sae-Yeon Won, Juergen Konczalla, Daniel Dubinski, Adriano Cattani, Colleen Cuca, Volker Seifert, Felix Rosenow, Adam Strzelczyk, Thomas M Freiman
BACKGROUND: Posttraumatic epileptic seizures (PTS) are a serious complication in patients with subdural haematoma (SDH). However, to date, several studies have shown discordances about SDH-associated seizures in terms of incidence, risk factors and prophylactic antiepileptic treatment. OBJECTIVE: The aim of this study was to analyse the incidence, risk factors of PTS and the role of prophylactic antiepileptic treatment in patients with SDH. DATA SOURCES: A systematic literature review examining PTS in patients with SDH was performed using PubMed gateway, Cochrane Central Register of Controlled Trials, and Excerpta Medica dataBASE between September 1961 and February 2016...
November 25, 2016: Seizure: the Journal of the British Epilepsy Association
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