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Wyniki wyszukiwania dla: drug design
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Optical properties of the chemotherapy drugs used in the central nervous system lymphoma therapy: monitoring drug delivery
PublikacjaOur aim is to optically monitor the delivery of the chemotherapy drugs for brain tumours, particularly used in the central nervous system (CNS) lymphoma therapy. In vivo monitoring would help to optimize the treatment and avoiding unnecessary medications. Moreover, it would be beneficial to be able to measure which of the multi-regimen drugs actually do penetrate and how well into the brain tissue. There exist several potential...
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Bioactive silica-based drug delivery systems containing doxorubicin hydrochloride: In vitro studies
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Use of Materials Based on Polymeric Silica as Bone-Targeted Drug Delivery Systems for Metronidazole
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Homoisocitrate dehydrogenase from Candida albicans: properties, inhibition, and targeting by an antifungal pro-drug
PublikacjaThe LYS12 gene from Candida albicans, coding for homoisocitrate dehydrogenase was cloned and expressed as a His-tagged protein in Escherichia coli. The purified gene product catalyzes the Mg2+- and K+-dependent oxidative decarboxylation of homoisocitrate to alpha-ketoadipate. The recombinant enzyme demonstrates strict specificity for homoisocitrate. SDS-PAGE of CaHIcDH revealed its molecular mass of 42.6±1 kDa, while in size-exclusion...
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The modulatory effect of green tea catechin on drug resistance in human ovarian cancer cells
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Acinetobacter baumannii isolated from hospital‐acquired infection: biofilm production and drug susceptibility
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Fulminant hepatic failure in woman with iron and non-steroidal anti-inflammatory drug intoxication
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New Life of an Old Drug: Caffeine as a Modulator of Antibacterial Activity of Commonly Used Antibiotics
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The Current Use of Mass Spectrometry in Combination with Other Separation Techniques in Drug Discovery Arena
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Activity of Phage–Lactoferrin Mixture against Multi Drug Resistant Staphylococcus aureus Biofilms
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ENCAPSULATION OF ROXITHROMYCIN INTO GELLAN GUM MATRICES AND THE IMPACT OF OTHER NATURAL POLYMERS ON DRUG RELEASE
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Drug-Releasing Antibacterial Coating Made from Nano-Hydroxyapatite Using the Sonocoating Method
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Drug transporter expression profiling in chemoresistant variants of the A2780 ovarian cancer cell line
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Microneedle‐Based Generation of Microbubbles in Cancer Tumors to Improve Ultrasound‐Assisted Drug Delivery
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Silver Nanoparticles as Chlorhexidine and Metronidazole Drug Delivery Platforms: Their Potential Use in Treating Periodontitis
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Cisplatin filled multiwalled carbon nanotubes – a novel molecular hybrid of anticancer drug container
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Polysaccharides-Based Hybrid Materials for Bio- and Non-Bio Sectors. Edytorial
PublikacjaThis special edition spotlights the recent research in the design, development, and emerging applications of polysaccharides-based hybrid materials for biotechnological and biomedical purposes. All the articles published in this issue underscore the significance of materials derived from cellulose, alginate, chitosan, starch, and carrageenan for various applications, including enzyme production, encapsulation, targeted drug delivery,...
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Longitudinal drug synergy assessment using convolutional neural network image-decoding of glioblastoma single-spheroid cultures
PublikacjaAbstract Background In recent years, drug combinations have become increasingly popular to improve therapeutic outcomes in various diseases, including difficult to cure cancers such as the brain cancer glioblastoma. Assessing the interaction between drugs over time is critical for predicting drug combination effectiveness and minimizing the risk of therapy resistance. However, as viability readouts of drug combination experiments...
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Glutathione-mediated conjugation of anticancer drugs: an overview of reaction mechanisms and biological significance for drug detoxification and bioactivation.
PublikacjaThe effectiveness of many anticancer drugs depends on the creation of specific metabolites that may alter their therapeutic or toxic properties. One significant route of biotransformation is a conjugation of electrophilic compounds with reduced glutathione, which can be non-enzymatic and/or catalyzed by glutathione-dependent enzymes. Glutathione usually combines with anticancer drugs and/or their metabolites to form more polar...
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Experimental and Machine-Learning-Assisted Design of Pharmaceutically Acceptable Deep Eutectic Solvents for the Solubility Improvement of Non-Selective COX Inhibitors Ibuprofen and Ketoprofen
PublikacjaDeep eutectic solvents (DESs) are commonly used in pharmaceutical applications as excellent solubilizers of active substances. This study investigated the tuning of ibuprofen and ketoprofen solubility utilizing DESs containing choline chloride or betaine as hydrogen bond acceptors and various polyols (ethylene glycol, diethylene glycol, triethylene glycol, glycerol, 1,2-propanediol, 1,3-butanediol) as hydrogen bond donors. Experimental...
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Experimental and Machine-Learning-Assisted Design of Pharmaceutically Acceptable Deep Eutectic Solvents for the Solubility Improvement of Non-Selective COX Inhibitors Ibuprofen and Ketoprofen
PublikacjaDeep eutectic solvents (DESs) are commonly used in pharmaceutical applications as excellent solubilizers of active substances. This study investigated the tuning of ibuprofen and ketoprofen solubility utilizing DESs containing choline chloride or betaine as hydrogen bond acceptors and various polyols (ethylene glycol, diethylene glycol, triethylene glycol, glycerol, 1,2-propanediol, 1,3-butanediol) as hydrogen bond donors. Experimental...
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Design, synthesis, and biological evaluation of tetrahydroquinolinones and tetrahydroquinolines with anticancer activity
PublikacjaColorectal cancer (CRC) is the most commonly diagnosed cancer in Europe and the United States and the second leading cause of cancer related mortality. A therapeutic strategy used for the treatment of CRC involves targeting the intracellular levels of reactive oxygen species (ROS). In this study, we synthesized a series of novel tetrahydroquinolinones and assessed their ability to inhibit CRC growth and proliferation by evoking...
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Electrochemical simulation of metabolism for antitumor-active imidazoacridinone C-1311 and in silico prediction of drug metabolic reactions
PublikacjaThe metabolism of antitumor-active 5-diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311) has been investigated widely over the last decade but some aspects of molecular mechanisms of its metabolic transformation are still not explained. In the current work, we have reported a direct and rapid analytical tool for better prediction of C-1311 metabolism which is based on electrochemistry (EC) coupled on-line with electrospray...
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Utilizing Genome-Wide mRNA Profiling to Identify the Cytotoxic Chemotherapeutic Mechanism of Triazoloacridone C-1305 as Direct Microtubule Stabilization
PublikacjaRational drug design and in vitro pharmacology profiling constitute the gold standard in drug development pipelines. Problems arise, however, because this process is often dicult due to limited information regarding the complete identification of a molecule’s biological activities. The increasing aordability of genome-wide next-generation technologies now provides an excellent opportunity to understand a compound’s diverse eects...
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The Interaction of Heptakis (2,6-di-O-Methyl)-β-Cyclodextrin with Mianserin Hydrochloride and Its Influence on the Drug Toxicity
PublikacjaOne tetracyclic antidepressant, mianserin hydrochloride (MIA), has quite significant side effects on a patients’ health. Cyclodextrins, which are most commonly used to reduce the undesirable features of contained drugs within their hydrophobic interior, also have the potential to alter the toxic behavior of the drug. The present paper contains investigations and the characteristics of interaction mechanisms for MIA and the heptakis...
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From the pills to environment – Prediction and tracking of non-steroidal anti-inflammatory drug concentrations in wastewater
PublikacjaThe extend of environment pollution by pharmaceuticals is in a stage that required more automatic and integrated solutions. The non-steroidal anti-inflammatory drugs (NSAIDs) are one of the most popular pharmaceutical in the world and emerging pollutants of natural waters. The aim of the paper was to check the correlation of the sales data of selected NSAIDs (ibuprofen, naproxen, diclofenac) and their concentration in the WWTP...
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The bioactivity studies of drug-loaded mesoporous silica-polydimethylsiloxane xerogels using FTIR and SEM/XEDS
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Correlation between physicochemical properties of doxorubicin-loaded silica/polydimethylsiloxane xerogel and in vitro release of drug
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Silver Nanoparticles as Chlorhexidine and Metronidazole Drug Delivery Platforms: Their Potential Use in Treating Periodontitis [Corrigendum]
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Novel and effective synthesis protocol of AgNPs functionalized using L-cysteine as a potential drug carrier
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A randomized and controlled study of noninvasive hemodynamic monitoring as a guide to drug treatment of uncontrolled hypertensive patients
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Combinatory Treatment with miR-7-5p and Drug-Loaded Cubosomes Effectively Impairs Cancer Cells
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New amino acid propyl ester ibuprofenates from synthesis to use in drug delivery systems
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Biological effects in photodynamic treatment combined with electropermeabilization in wild and drug resistant breast cancer cells
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Increased Expression of Several Collagen Genes is Associated with Drug Resistance in Ovarian Cancer Cell Lines
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Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties
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Double layer adhesive silicone dressing as a potential dermal drug delivery film in scar treatment
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The Correlation between Physical Crosslinking and Water-Soluble Drug Release from Chitosan-Based Microparticles
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Essentials and Perspectives of Computational Modelling Assistance for CNS-oriented Nanoparticle-based Drug Delivery Systems
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Virulence and Drug-Resistance of Staphylococcus aureus Strains Isolated from Venous Ulcers in Polish Patients
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Evaluation of multiple genetic markers for typing drug-resistant Mycobacterium tuberculosis strains from Poland
PublikacjaW publikacji przedstawiono wyniki genotypowania wielolekoopornych szczepów Mycobacterium tuberculosis izolowanych od pacjentów z Polski.
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Antibiotic-Based Conjugates Containing Antimicrobial HLopt2 Peptide: Design, Synthesis, Antimicrobial and Cytotoxic Activities
PublikacjaRecent studies have shown that modified human lactoferrin 20−31 fragment, named HLopt2, possesses antibacterial and antifungal activity. Thus, we decided to synthesize and evaluate the biological activity of a series of conjugates based on this peptide and one of the antimicrobials with proven antibacterial (ciprofloxacin, CIP, and levofloxacin, LVX) or antifungal (fluconazole, FLC) activity. The drugs were covalently connected...
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Drug-resistant and hospital-associated Enterococcus faecium from wastewater, riverine estuary and anthropogenically impacted marine catchment basin.
PublikacjaEnterococci, ubiquitous colonizers of humans and other animals, play an increasingly important role in health-care associated infections (HAIs). Acquisition of resistance determinants not only seriously limits available therapeutic options but also increases available gene pool for other species. It is believed that the recent evolution of two clinically relevant species, Enterococcus faecalis and Enterococcus faecium occurred...
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Towards Rational Biosurfactant Design—Predicting Solubilization in Rhamnolipid Solutions
PublikacjaThe efficiency of micellar solubilization is dictated inter alia by the properties of the solubilizate, the type of surfactant, and environmental conditions of the process. We, therefore, hypothesized that using the descriptors of the aforementioned features we can predict the solubilization efficiency, expressed as molar solubilization ratio (MSR). In other words, we aimed at creating a model to find the optimal surfactant and...
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Theoretical Encapsulation of Fluorouracil (5-FU) Anti-Cancer Chemotherapy Drug into Carbon Nanotubes (CNT) and Boron Nitride Nanotubes (BNNT)
PublikacjaIntroduction: Chemotherapy with anti-cancer drugs is considered the most common approach for killing cancer cells in the human body. However, some barriers such as toxicity and side effects would limit its usage. In this regard, nano-based drug delivery systems have emerged as cost-effective and efficient for sustained and targeted drug delivery. Nanotubes such as carbon nanotubes (CNT) and boron nitride nanotubes (BNNT) are promising...
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Degradation of cefadroxil drug by newly designed solar light responsive alcoholic template-based lanthanum ferrite nanoparticles
PublikacjaIn this work, lanthanum ferrite nanoparticles were synthesized via a simple co-precipitation method. Two different templates, namely sorbitol and mannitol, were used in this synthesis to tune the optical, structural, morphological, and photocatalytic properties of lanthanum ferrite. The synthesized lanthanum ferrite-sorbitol (LFOCo-So) and lanthanum ferrite-mannitol (LFOCo-Mo) were investigated through Ultraviolet–Visible (UV–Vis),...
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Molecular characterization of drug-resistant Mycobacterium tuberculosis strains from Poland by use of multiple genetic markers
PublikacjaW pracy przedstawiono wyniki genotypowania wielolekoopornych szczepów Mycobacterium tuberculosis, izolowanych od pacjentów z Polski.
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Thromboelastometric Analysis of Anticancer Cerrena unicolor Subfractions Reveal Their Potential as Fibrin Glue Drug Carrier Enhancers
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Controlled Drug Release and Cytotoxicity Studies of Beta-Lapachone and Doxorubicin Loaded into Cyclodextrins Attached to a Polyethyleneimine Matrix
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Discovery of the anticancer drug vinblastine from the endophytic Alternaria alternata and yield improvement by gamma irradiation mutagenesis
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