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Wyniki wyszukiwania dla: DRUG DELIVERY NANOSYSTEM
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Visualizing Carotid Bodies With Doppler Ultrasound Versus CT Angiography: Preliminary Study
PublikacjaOBJECTIVE. The purpose of this article is to evaluate the utility of ultrasound in identifying carotid bodies (CBs) in patients with drug-resistant arterial hypertension. SUBJECTS AND METHODS. We enrolled 13 patients with drug-resistant hypertension into a trial for surgical CB excision. CT angiography (CTA) and Doppler ultrasound (DUS) of the cervical arteries were performed before surgery. CBs were identified in a blind manner...
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Evaluation of the efficiency of the duty cycle of refuse collection vehicle based on real-world data
PublikacjaIn this paper a method of the efficiency evaluation of the duty cycle of Refuse Collection Vehicle is presented. Using real world data, two representative duty cycles were analysed. Total cycle efficiency was calculated, as well as the efficiency of particular cycle phases. Then, energy needed to collect and compact the waste and energy from fuel were compared. Measured and calculated values were shown on the diagrams illustrating...
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Molecular detection of Candida krusei
PublikacjaThe species identification of fungi belonging to genus Candida is an important issue as this genus becomes the emerging problem of nosocomial infections. As Candida krusei presents intrinsicresistance to the fluconazole that is the drug of the first choice in case of invasive candidiasis the PCR identifying the DNA of C. krusei was elaborated. The analytical sensitivity of the assay on spiked blood samples was estimated at 3-5...
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Pathological brain network activity: memory impairment in epilepsy
PublikacjaOur thinking, memory and cognition in general, relies upon precisely timed interactions among neurons forming brain networks that support cognitive processes. The surgical evaluation of drug-resistant epilepsy using intracranial electrodes provides a unique opportunity to record directly from human brain and to investigate the coordinated activity of cognitive networks. In this issue of Neurology®, Kleen and colleagues1 implicate...
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Information-driven network resilience: Research challenges and perspectives
PublikacjaInternet designed over 40 years ago was originally focused on host-to-host message delivery in a best-effort manner. However, introduction of new applications over the years have brought about new requirements related with throughput, scalability, mobility, security, connectivity, and availability among others. Additionally, convergence of telecommunications, media, and information technology was responsible for transformation...
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Molecular mechanism of proton-coupled ligand translocation by the bacterial efflux pump EmrE
PublikacjaThe current surge in bacterial multi-drug resistance (MDR) is one of the largest challenges to public health, threatening to render ineffective many therapies we rely on for treatment of serious infections. Understanding different factors that contribute to MDR is hence crucial from the global “one health” perspective. In this contribution, we focus on the prototypical broad-selectivity proton-coupled antiporter EmrE, one of the...
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Antifungal Activity of Capridine β as a Consequence of Its Biotransformation into Metabolite Affecting Yeast Topoisomerase II Activity
PublikacjaIn the last few years,increasing importance is attached to problems caused by fungal pathogens. Current methods of preventing fungal infections remain unsatisfactory. There are several antifungal compounds whichare highly effective in some cases, however, they have limitations in usage: Nephrotoxicity and other adverse effects. In addition, the frequent use of available fungistatic drugs promotes drug resistance....
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The Substantial Improvement of Amphotericin B Selective Toxicity Upon Modification of Mycosamine with Bulky Substituents
PublikacjaAbstract: Background: It is assumed that the unfavorable selective toxicity of an antifungal drug Amphotericin B (AmB) can be improved upon chemical modification of the antibiotic molecule. Objective: The aim of this study was verification of the hypothesis that introduction of bulky substituents at the amino sugar moiety of the antibiotic may result in diminishment of mammalian vitro toxicity of thus prepared AmB derivatives. Methods:...
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CYP3A4-dependent cellular response does not relate to CYP3A4-catalysed metabolites of C-1748 and C-1305 acridine antitumor agents in HepG2 cells
PublikacjaHigh CYP3A4 expression sensitizes tumor cells to certain antitumor agents while for others it can lower their therapeutic ef fi cacy. We have elucidated the in fl uence of CYP3A4 overexpression on the cellular response induced by antitumor acridine derivatives, C-1305 and C-1748, in two hepatocellular carcinoma (HepG2) cell lines, Hep3A4 stably transfected with CYP3A4 isoenzyme, and HepC34 expressing empty vector. The compounds...
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Imidazoacridinone-dependent lysosomal photodestruction: a pharmacological Trojan horse approach to eradicate multidrug-resistant cancers
PublikacjaMultidrug resistance (MDR) remains a primary hindrance to curative cancer therapy. Thus, introduction of novel strategies to overcome MDR is of paramount therapeutic significance. Sequestration of chemotherapeutics in lysosomes is an established mechanism of drug resistance. Here, we show that MDR cells display a marked increase in lysosome number. We further demonstrate that imidazoacridinones (IAs), which are cytotoxic fluorochromes,...
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Evaluation of possibilities in identification and susceptibility testing for Candida glabrata clinical isolates with the Integral System Yeast Plus (ISYP)
PublikacjaThe aim of this study was to evaluate possibilities of correct identification and susceptibility testing of C. glabrata clinical isolates with Integral System Yeast Plus (ISYP). For species identification, as the reference method, API Candida test and species-specific PCR reactions were used. The potential of antifungal susceptibility testing by the ISYP test was compared with the Sensititre Yeast One. Whilst the reference methods...
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Phase I and phase II metabolism simulation of antitumor-active 2-hydroxyacridinone with electrochemistry coupled on-line with mass spectrometry.
PublikacjaHere, we report the metabolic profile and the results of associated metabolic studies of 2-hydroxyacridinone (2-OH-AC), the reference compound for antitumor-active imidazo- and triazoloacridinones. Electrochemistry coupled with mass spectrometry was applied to simulate the general oxidative metabolism of 2-OH-AC for the first time. The reactivity of 2-OH-AC products to biomolecules was also examined. The usefulness of the electrochemistry...
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Organic solvents aggregating and shaping structural folding of protein, a case study of the protease enzyme
PublikacjaLow solubility of reactants or products in aqueous solutions can result in the enzymatic catalytic reactions that can occur in non-aqueous solutions. In current study we investigated aqueous solutions containing different organic solvents / deep eutectic solvents (DESs) that can influence the protease enzyme's activity, structural, and thermal stabilities. Retroviral aspartic protease enzyme is responsible for the cleavage of the...
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Electrochemical simulation of enzymatic transformations studied for the selected antitumor acridine derivatives
PublikacjaThe elucidation of the metabolic pathways and the biotransformation mechanisms of potential drugs is a crucial point in drug development. It allows to know the activation routes of the new biologically active compounds, especially in respect to their possible toxicity. Generally, in vivo or in vitro experiments with liver microsomes or hepatocytes are performed. However, these testing schemes are tedious, time consuming and of...
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Effects of Addictive Substances During Pregnancy and Infancy and Their Analysis in Biological Materials
PublikacjaThe use of addictive substances during pregnancy is a serious social problem, not only because of effects on the health of the woman and child, but also because drug or alcohol dependency it detracts from childcare and enhances the prospect of child neglect and family breakdown. Developing additive substance abuse treatment programs for pregnant women is socially important and can help ensure the health of babies, prevent subsequent...
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Universal and contextualized public services: Digital public service innovation framework
PublikacjaIn view of the rising social and economic inequalities, public service delivery should be both universal, i.e. independent of the recipients' social or economic status, and contextualized, i.e. able to compensate for different local needs and conditions. Reconciling both properties requires various forms of innovations, chief among them innovations in digital public services. Building upon the four-stage model underpinning the...
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Interline power flow controller - properties and control strategy in dynamic states
PublikacjaHigh-power electronic converter topologies, in such forms as Unified Power Flow Controllers (UPFC), Static Compensators (STATCOM) and Interline Power Flow Controllers (IPFC), have been used to enhance and optimize the use of transmission facilities, under the concept of a flexible ac transmission system (FACTS). In Europe, the anticipated proliferation of distributed-generation (DG) in the near future, driven by governmental initiatives...
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Cell-penetrating peptides – mechanism of transduction and synthesis – short review
PublikacjaPotential antimicrobial agents may be effective if they are delivered efficiently to their site of action. In many cases, lack of permeability through the cell membrane is the main problem. One of the possible solutions could be a novel intracellular delivery system involving cell-penetrating peptides (CPPs), which may improve the efficiency of many new biophar-maceuticals. Among other things, CPPs are capable of trans-porting...
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Disciplines and measures of information resilience
PublikacjaCommunication networks have become a fundamental part of many critical infrastructures, playing an important role in information delivery in various failure scenarios triggered e.g., by forces of nature (including earthquakes, tornados, fires, etc.), technology-related disasters (for instance due to power blackout), or malicious human activities. A number of recovery schemes have been defined in the context of network resilience...
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Urban Freight Transport Demand Modelling and Data Availability Constraints
PublikacjaThe paper provides a review of urban freight transport demand modelling approaches confronted with constrains regarding adequate data provision from a perspective of the local authorities. Demand estimation models has been selected as a reference because they are the most representative in terms of inclusion of urban freight indicators which can be transformed into a decision-support tool for evaluation of freight measures. The...
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Influence of Self-Similar Traffic Type on Performance of QoS Routing Algorithms
PublikacjaProviding a Quality of Services (QoS) into current telecommunication networks based on packet technology is a big challenge nowadays. Network operators have to support a number of new services like voice or video which generate new type of traffic. This traffic serviced with QoS in consequence requires access to appropriate network resources. Additionally, new traffic type is mixed with older one, like best-effort. Analysis of...
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Tailoring the electrochemical degradation of iron protected with polypyrrole films for biodegradable cardiovascular stents
PublikacjaThe degradation of polypyrrole (PPy) coated iron is studied in phosphate buffer saline solution at 37 °C by odd random phase multisine electrochemical impedance spectroscopy (ORP-EIS). PPy is electropolymerized with anti-inflammatory salicylates incorporated in the film, as a drug release system. The modelling of EIS over time provides the quantitative description of the corrosion behaviour of the material. Thus, the reliable...
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Structure–activity relationships study on biological activity of peptides as dipeptidyl peptidase IV inhibitors by chemometric modeling
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Design and characteristics of gellan gum beads for modified release of meloxicam
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Aryl- and heteroaryl-substituted phenylalanines as AMPA receptor ligands
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Short Term Monitor of Photodegradation Processes in Ranitidine Hydrochloride Observed by FTIR and ATR FTIR
PublikacjaThe effects of degradation of ranitidine hydrochloride exposed to UVB radiation (l = 310 nm) and oxygen in a weathering chamber were studied by Fourier Transform Infrared spectroscopy (FTIR) and Attenuated Total Reflectance Fourier Transform Infrared spectroscopy (ATR-FTIR). ATR-FTIR profile indicated that the degradation was spatially heterogeneous. Significant amounts of photoproducts were detected only in a directly...
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CDK9: Therapeutic Perspective in HCC Therapy
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Current Challenges in Targeting Tumor Desmoplasia to Improve the Efficacy of Immunotherapy
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Solubility advantage of sulfanilamide and sulfacetamide in natural deep eutectic systems: experimental and theoretical investigations
PublikacjaObjective: The aim of this study was to explore the possibility of using natural deep eutectic solvents (NADES) as solvation media for enhancement of solubility of sulfonamides, as well as gaining some thermodynamic characteristics of the analyzed systems. Significance: Low solubility of many active pharmaceutical ingredients is a well-recognized difficulty in pharmaceutical industry, hence the need for different strategies addressing...
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Simplified, serine‐rich theta‐defensin analogues as antitumour peptides
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Investigating the disease‐modifying properties of sclerotiorin in Alzheimer's therapy using acetylcholinesterase inhibition
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Preliminary antifungal activity assay of selected chlorine-containing derivatives of xanthone and phenoxyethyl amines
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The Chemometric Evaluation of Antitumor Activity of Novel Benzensulfonamide Derivatives Based on their Physiochemical Properties
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QSAR Analysis of Compounds Exhibiting General Anesthetics’ Properties
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QSAR Analysis of Selected Antimicrobial Structures Belonging to Nitro-derivatives of Heterocyclic Compounds
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Differential scanning calorimetry for authentication of edible fats and oils - What can we learn from the past to face the current challenges?
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Conformational Preferences of Proline Derivatives Incorporated into Vasopressin Analogues: NMR and Molecular Modelling Studies
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Highly Potent Antidiuretic Antagonists: Conformational Studies of Vasopressin Analogues Modified with 1-Naphthylalanine Enantiomers at Position 2
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Synthesis and biological evaluation of N-acylated tyramine sulfamates containing C-F bonds as steroid sulfatase inhibitors
PublikacjaSteroid sulfatase (STS) is responsible for the hydrolysis of biologically inactive sulfated steroids into their active un-sulfated forms and promotes the growth of various hormone-dependent cancers (e.g., breast cancer). Therefore, the STS enzyme is a promising therapeutic target for the treatment of steroid-sensitive cancers. Herein, we report the synthesis and biological evaluation of sulfamate analogs as potential STS inhibitors...
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Synthesis and biological evaluation of fluorinated 3-phenylcoumarin-7-O-sulfamate derivatives as steroid sulfatase inhibitors
PublikacjaIn the present work, we report the initial results of our study on a series of 3-phenylcoumarin sulfamate-based compounds containing C-F bonds as a novel inhibitors of steroid sulfatase (STS). The new compounds are potent STS inhibitors, possessing more than 10 times higher inhibitory potency than coumarin-7-O-sulfamate. In the course of our investigation, compounds 2b and 2c demonstrated the highest inhibitory effect in the enzymatic...
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Effects of an immunosuppressive treatment on the rat prostate
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Novel anticancer strategy aimed at targeting shelterin complexes by the induction of structural changes in telomeric DNA: hitting two birds with one stone.
PublikacjaThe ends of chromosomes in mammals are composed of telomeric DNA containing TTAGGG repeats, which bind specific proteins called shelterins. This telomeric DNA together with shelterins form a cap that protects the ends of chromosomes from being recognized as sites of DNA damage and from chromosomal fusions. Many very successful antitumor drugs used in the treatment of cancer patients bind to DNA, some of them with a prominent sequence...
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Influence of S-Oxidation on Cytotoxic Activity of Oxathiole-Fused Chalcones
PublikacjaSynthesis, in vitro cytotoxic activity, and interaction with tubulin of oxidized, isomeric 1-(5-alkoxybenzo[d] [1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-ones and 1-(6- alkoxybenzo[d][1,3]oxathiol-5-yl)-3-phenylprop-2-en-1- ones are described. Most of the compounds demonstrated cytotoxic activity at submicromolar concentrations. It was found that oxidation of sulfur atom of the oxathiole-fused chalcones strongly influenced activity...
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Structural Factors Affecting Cytotoxic Activity of (E)-1-(Benzo[d ][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one Derivatives
PublikacjaDerivatives of (E)-1-(5-alkoxybenzo[d][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one (1) demonstrated exceptionally high in vitro cytotoxic activity, with IC50 values of the most active derivatives in the nanomolar range. To identify structural fragments necessary for the activity, several analogs deprived of selected fragments were prepared, and their cytotoxic activity was tested. It was found that the activity depends on combined effects...
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Synthesis and biological activity of ester derivatives of mycophenolic acid and acridines/acridones as potential immunosuppressive agents
PublikacjaImproved derivatives of mycophenolic acid (MPA) are necessary to reduce the frequency of adverse effects, this drug exerts in treated patients. In this study, MPA was coupled with N-(x-hydroxyalkyl)-9-acridone-4-carboxamides or N-(x-hydroxyalkyl)acridine-4-carboxamides to give respective ester conjugates upon Yamaguchi protocol. This esterification required protection of phenol group in MPA. Designed conjugates revealed higher...
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Dietary intervention with beetroot juice during doxorubicin cancer chemotherapy in vivo reduces markers of oxidative stress
PublikacjaCancer chemotherapy with doxorubicin, despite high antitumor activity and broad spectrum of this drug, is on decline due to toxic side effects. The clinical efficacy of anthracyclines have continuously prompted the search for new adjuvants to alleviate undesirable side toxicity incurred by this group of cytostatics. The recent approaches involve the application of synthetic or purified natural antioxidants in combination with doxorubicin...
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Intermolecular Interactions as a Measure of Dapsone Solubility in Neat Solvents and Binary Solvent Mixtures
PublikacjaDapsone is an effective antibacterial drug used to treat a variety of conditions. However, the aqueous solubility of this drug is limited, as is its permeability. This study expands the available solubility data pool for dapsone by measuring its solubility in several pure organic solvents: N-methyl-2-pyrrolidone (CAS: 872-50-4), dimethyl sulfoxide (CAS: 67-68-5), 4-formylmorpholine (CAS: 4394-85-8), tetraethylene pentamine (CAS:...
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Activation Energy and Inclination Magnetic Dipole Influences on Carreau Nanofluid Flowing via Cylindrical Channel with an Infinite Shearing Rate
PublikacjaThe infinite shear viscosity model of Carreau fluid characterizes the attitude of fluid flow at a very high/very low shear rate. This model has the capacity for interpretation of fluid at both extreme levels, and an inclined magnetic dipole in fluid mechanics has its valuable applications such as magnetic drug engineering, cold treatments to destroy tumors, drug targeting, bio preservation, cryosurgery, astrophysics, reaction kinetics,...
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Docking simulations, Molecular properties and ADMET studies of novel Chromane6,7diol analogues as potential inhibitors of Mushroom tyrosinase
PublikacjaResearch on inhibition of tyrosinase enzyme has attained significant value, because tyrosinase inhibitors have potential applications in medicine, cosmetics (as whitening agents) and in agriculture (as bioinsecticides). Determination and elucidation of new tyrosinase inhibitors are not only beneficial for medical purposes, but their promising applications in improving food quality and nutritional...
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Cell Density-Dependent Cytological Stage Profile and Its Application for a Screen of Cytostatic Agents Active Toward Leukemic Stem Cells
PublikacjaProliferation and expansion of leukemia is driven by leukemic stem cells (LSCs). Multidrug resistance (MDR) of LSCs is one of the main reasons of failure and relapses in acute myeloid leukemia (AML) treatment. In this study, we show that maintaining HL-60 at low cell culture density or applying a 240-day treatment with anthrapyridazone (BS-121) increased the percentage of primitive cells, which include LSCs determining the overall...