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Search results for: drug
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N-acylpeptides with glucosamine-6-phosphate synthase inhibitors - synthesisand antifungal activity
PublicationOpracowano syntezę kilku peptydów (di i tripeptydów) zawierających inhibitory syntazy glukozamino-6-fosforanu oraz przeprowadzono je w N-acylopochodne (acetylowe, heksanoilowe, dekanoilowe) oraz zbadano ich aktywność przeciwgrzybową w stosunku do szczepów Candida albicans z opornością wielolekową. Stwierdzono, że N-acylopeptydy wykazują aktywność przeciwgrzybową oraz określono wartości MIC.
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Fatal iatrogenic vinorelbine poisoning
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Two novel nucleoside ester derivatives of chlorambucil as potential antileukemic prodrugs: a preliminary study
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The Combination of Beta-Blockers and ACE Inhibitors Across the Spectrum of Cardiovascular Diseases
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Preclinical toxicological examination of a putative prostate cancer-specific 4-methyl-1-nitroacridine derivative in rodents
PublicationW pracy przedstawiono wyniki przedklinicznych badań toksykologicznych zwiazków C-1748 i C-857 na szczurach Copenhagen i myszach BALB/c, po podaniu dootrzewnowym lub dożylnym. U myszy dawki letalne (LD50) dla C-1748 wynosiły odpowiednio 9 i 13,4 mg/kg w porównaniu z 2,2 i 3 mg/kg dla C-857. U szczurów po podaniu dootrzewnowym lub dożylnym dla C-1748 dawki LD50 wynosiły odpowiednio 4 i 1,3 mg/kg. Nie stwierdzono zmian w liczbie komórek...
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Protective Effect of Black Tea Against Ethanol-Induced Oxidative Modifications of Liver Proteins and Lipids
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Pregabalin for the treatment of social anxiety disorder
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Space BriGade Establishing and conducting joint second degree studies in Space Technologies in Gdansk and Bremen
ProjectsProject realized in Department of Mechanics and Mechatronics
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Katedra Inżynierii Sanitarnej
Research TeamsKatedra realizuje swoje zadania badawcze w takim zakresie jak opracowywanie metody podczyszczania lub oczyszczania ścieków przemysłowych oraz ich pomiary. Drugą gałęzią zainteresowań są modele matematyczne i symulacje procesów oczyszczania ścieków i zagospodarowania osadów, opracowywanie symulacji strategii eksploatacyjnych i działań modernizacyjnych.
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Zespół Katedry Analizy Nieliniowej i Statystyki
Research TeamsW Katedrze prowadzone są badania w trzech wiodących kierunkach. Pierwszy dotyczy zastosowania metod topologicznych i wariacyjnych w układach dynamicznych, w teorii równań różniczkowych zwyczajnych i cząstkowych oraz w teorii bifurkacji. Drugim kierunkiem badań Katedry jest zastosowanie rachunku prawdopodobieństwa i teorii aproksymacji. Ostatnią specjalizacją jest Geometria i Grafika Komputerowa, która istnieje od 2014 roku. Wybór...
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Dr.shazia Farheen Qureshi
PeopleI am Psychiatrist wants to heal and inspire the minds. I did post grdauation from College of Physicians and Surgeons of Bombay, Mumbai, India. I am having 10 years experience in field of Psychiatry in variety of Clinical settings that have included Child, Adolesecent, Geriatric and Forensic Psychiatry and drug deaddiction services also clinical research work.
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Javed Ather Siddiqui DR.
PeopleI AM PSYCHATRIST,WANTS TO BRING SMILE ON THE FACES OF MENTALLY ILL PATIENTS. I LOVE MY PROFESSION AND WANT TO FACE CHALLENGES FOR SAKE OF THE PATIENTS. I EARNED POST GRADUATE DEGREE FROM MUMBAI UNIVERSITY AT G S SRTH MEDICAL COLLEGE AND KEM HOSPITAL, MUMBAI, INDIA. I HAVE OVER 20 YEARS OF MENTAL HEALTH EXPERIENCE. I HAVE WORKED IN VARIETY OF CLINICAL SETTINGS THAT HAVE INCLUDED DRUG DEADDICTION, CHILD, ADOLESCENT, GERIATRIC AND...
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Ahmer Bin Hafeez
PeopleI have experience in Microbiology & Computational Biology, particularly bioinformatics, homology modeling, phylogenetics, structural biology, and drug discovery. Currently, my interest lies in translatable omics studies and drug discovery against novel protein targets involved in cancer and infectious diseases and Host-Pathogen PPIs. My aim involves the use of computational methods for the identification of novel targets and to...
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The effect of anthraquinone derivatives (C1-C9) on telomerase activity
Open Research DataThe data set contains images of the PCR products obtained from the Telomerase Repeated Amplification Protocol (TRAP). The effect of anthraquinone derivatives (C-C9) on telomerase activity was analyzed using lysates from drug-treatedcancer cell line.
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The II phase metabolism of endogenous and exogenous compounds, including antitumor chemotherapeutics
PublicationThe II phase metabolism, it is a set of metabolism and excretion pathways of endogenous as well as exogenous compounds including xenobiotics. UDP-glucuronyltransferases (UGTs; EC 2.4.1.17) are the most crucial representatives of II phase enzymes, which are responsible for the transformation of bilirubine and bile acids, steroids and thyroid hormones and lipids. Exogenous compounds, including drugs, carcinogens, environmental pollutants...
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Biopsy needles coated with the antimicrobial coatings
PublicationDrug delivery systems are used to achieve higher therapeutic effects of medicaments in a specific diseased site with minimal toxicological effect. The used of biopolymers in drug delivery systems ensure the biocompatibility, biodegradability and low immunogenicity. Drug delivery systems enhance the drug delivery actively and can be used in different diseases. In this study, two types of polymer coatings were prepared and were...
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Polyacrylamide substrate viscosity impact on temozolomide activity in glioblastoma cells by flow cytometry and rheological measurements
Open Research DataDataset includes raw data on cell lines LN-229 and LN-18 treated with temozolomide measured by flow cytometry, rheometry and cell projections. It also includes calculations necessary for creation of figures and conclusions based on those figures in the publication titiled: "Substrate viscosity impairs temozolomide-mediated inhibition of glioblastoma...
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Pregnane X receptor dependent up-regulation of CYP2C9 and CYP3A4 in tumor cells by antitumor acridine agents, C-1748 and C-1305, selectively diminished under hypoxia
PublicationInduction of proteins involved in drug metabolism and in drug delivery has a significant impact on drug-drug interactions and on the final therapeutic effects. Two antitumor acridine derivatives selected for present studies, C-1748 (9-(2’-hydroxyethylamino)-4-methyl-1-nitroacridine) and C-1305 (5-dimethylaminopropylamino-8-hydroxy-triazoloacridinone), expressed high and low susceptibility to metabolic transformations with liver...
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Screening of predicted synergistic multi-target therapies in glioblastoma identifies new treatment strategies
PublicationAbstract Background IDH-wildtype glioblastoma (GBM) is a highly malignant primary brain tumor with a median survival of 15 months after standard of care, which highlights the need for improved therapy. Personalized combination therapy has shown to be successful in many other tumor types and could be beneficial for GBM patients. Methods We performed the largest drug combination screen to date in GBM, using a high-throughput effort...
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Poloxamer: A versatile tri-block copolymer for biomedical applications
PublicationPoloxamers, also called Pluronic, belong to a unique class of synthetic tri-block copolymers containing central hydrophobic chains of poly(propylene oxide) sandwiched between two hydrophilic chains of poly(ethylene oxide). Some chemical characteristics of poloxamers such as temperature-dependent self-assembly and thermo-reversible behavior along with biocompatibility and physiochemical properties make poloxamer-based biomaterials...
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Mission impossible for cellular internalization: When porphyrin alliance with UiO-66-NH2 MOF gives the cell lines a ride
PublicationIs it possible to accelerate cell internalization by hybridization of nanomaterials? Herein we support the realization of using metal-organic frameworks (MOFs) with the assistance of rigid porphyrin structure (H2TMP) aimed at drug loading, drug release, relative cell viability, and targeted in vitro drug delivery. There are several MOFs, i.e., UiO-66-NH2 (125 ± 12.5 nm), UiO-66-NH2 @H2TMP (160 ± 14 nm), UiO-66-NH2 @H2TMP@DOX, and...
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Pemphigoid - Female, 86 - Tissue image [6160730013048041]
Open Research DataThis is the histopathological image of SKIN tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: Pannoramic 250 3DHistech slide scanner (20x magnification) and saved to DICOM format.
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Voltammetric and biological studies of folate-targeted non-lamellar lipid mesophases
PublicationFolate-targeted lipid nanostructures are promising strategies for the development of biocompatible drug delivery systems. The objective of this study was to evaluate the efficacy of drug delivery to cancer cells by folate-targeted lipid mesophases, cubosomes (CUB) and hexosomes (HEX), loaded with doxorubicin (DOX). Three cancer-derived cell lines (KB, HeLa, T98G) exhibiting different expressional levels of folate receptor protein...
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New oryginal generic technologies: A Polish R&D strategic implementation programme
PublicationPolands's pharmaceutical industry is of great significance to the whole economy. According to Forbs (2 October 2012), the cost of launching a new drug varies from USD 1 to 11 bilion. There is little Chance of a Polish pharmaceutical company developing an original drug due to financial reason.Many research teams in Poland take up research projects aimed at new biologically active compounds. But such an objective has no broader perspective,...
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Topical delivery of pharmaceutical and cosmetic macromolecules using microemulsion systems
PublicationMicroemulsions are transparent, thermodynamically stable colloidal systems. Over the recent years, they have been increasingly investigated due to their potential as skin delivery vehicles for a wide range of drug molecules. The nanoscale particle size and the specificity of microemulsion components are the main features determining the skin permeation process. However, in order to effectively cross the skin barrier, the active...
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Fabrication methods of smart composite coatings - review
PublicationPostoperative bacterial infections are one of the main reasons for unsuccessful implantation of long-term implants. The development of bacterial infection requires antibiotic therapy, in extreme cases a reimplantation procedure is necessary. In order to provide materials for implants with antibacterial properties, they are subjected to modifications to create a coating that will release the drug substance, when the inflammation...
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Increased cytotoxicity of an unusual DNA topoisomerase II inhibitor compound C-1305 toward HeLa cells with downregulated PARP-1 activity results from re-activation of the p53 pathway and modulation of mitotic checkpoints
PublicationOur previous studies have shown that murine fibroblast cells, in which PARP-1 gene was inactivated by gene disruption, are extremely sensitive to triazoloacridone compound C-1305, an inhibitor of DNA topoisomerase II with unusual properties. Here, we show that pharmacological inhibition of PARP-1 activity by its inhibitor compound NU1025, sensitizes human cervical carcinoma HeLa cells to compound C-1305 compared to treatment with...
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Damian Rosiak dr inż.
PeopleEducation 2010–2014: Gdansk University of Technology, Chemical Faculty (Eng.) field of study: biotechnology specialty: drug biotechnology 2014–2015: Gdansk University of Technology, Chemical Faculty (M.Sc.) field of study: biotechnology specialty: drug biotechnology 2015–2020: Gdansk University of Technology, Department of Inorganic Chemistry (Ph.D.) discipline: chemical sciences specialty: inorganic chemistry Scientific...
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Polymer biodegradable coatings as active substance release systems for urological applications
PublicationCatheter-associated urinary tract infections are the result of catheterization of the bladder. The risk of infection is directly proportional to the length of the bladder catheterization. Bacteria cells have the ability to adhere and create the biofilm on the surface of catheter materials. Bacteria’s biofilm is an extremely beneficial environment of existence for microorganisms. Microorganisms that are an integral part of the biofilm...
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Improvement of opipramol base solubility by complexation with β-cyclodextrin
PublicationOpipramol (OPI), a tricyclic antidepressant and anxiolytic compound, is administered orally in the form of a dihydrochloride. Salt form of the drug has a higher solubility in water and hence bioavailability and stability. A similar effect can be achieved by closing the hydrophobic part of the drug molecule in the cyclodextrin cavity. The paper presents opipramol inclusion complexes with beta-cyclodextrin (β-CD) in 1:1 molar ratio....
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Synthesis of green benzamide-decorated UiO-66-NH2 for biomedical applications
PublicationMetal-organic frameworks (MOFs) biocompatible systems can host enzymes/bacteria/viruses. Herein we synthesized a series of fatty acid amide hydrolase (FAAH)-decorated UiO-66-NH2 based on Citrus tangerine leaf extract for drug delivery and biosensor applications. Five chemically manipulated FAAH-like benzamides were localized on the UiO-66-NH2 surface with physical interactions. Comprehensive cellular and molecular analyses were...
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The mechanism of internalization study of QDgreen−CD−FA−C−2028 conjugate at IC80 value to cancer (H460, Du-145, and LNCaP) and normal (MRC-5 and PNT1A) cells
Open Research DataThe influence of different endocytosis inhibitors on the internalization of QDgreen−CD−FA−C−2028 conjugate at IC80 value in cancer (H460, Du-145, and LNCaP) and normal (MRC-5 and PNT1A) cells. First, the cells were preincubated with: drug-free medium (no inhibitor), at 4 °C, 5 µM Cytochalasin D, 30 µM Amiloride, 80 µM Dynasore, 25 µM Pitstop 2 and 1.5...
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Modeling of pharmaceuticals mixtures toxicity with deviation ratio and best-fit functions models
PublicationThe present study deals with assessment of ecotoxicological parameters of 9 drugs (diclofenac (sodium salt), oxytetracycline hydrochloride, fluoxetine hydrochloride, chloramphenicol, ketoprofen, progesterone, estrone, androstenedione and gemfibrozil), present in the environmental compartments at specific concentration levels, and theirmutual combinations by couples against Microtox® and XenoScreen YES/YAS® bioassays. As the quantitative...
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Utilizing Genome-Wide mRNA Profiling to Identify the Cytotoxic Chemotherapeutic Mechanism of Triazoloacridone C-1305 as Direct Microtubule Stabilization
PublicationRational 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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Antibacterial Porous Systems Based on Polylactide Loaded with Amikacin
PublicationThree porous matrices based on poly(lactic acid) are proposed herein for the controlled release of amikacin. The materials were fabricated by the method of spraying a surface liquid. Description is given as to the possibility of employing a modifier, such as a silica nanocarrier, for prolonging the release of amikacin, in addition to using chitosan to improve the properties of the materials, e.g., stability and sorption capacity....
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Influence of the electrosynthesis conditions on the spontaneous release of anti-inflammatory salicylate during degradation of polypyrrole coated iron for biodegradable cardiovascular stent
PublicationIn this work, the spontaneous release of anti-inflammatory salicylate from polypyrrole (PPy) coated iron has been studied during degradation of the material in phosphate buffer saline at 37 C. The sodium salicylate was incorporated into PPy in a one-step electropolymerization process. The influence of the synthesis conditions such as sodium salicylate concentration, pyrrole concentration and deposition charge on drug release profile...
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Cellulose Nanomaterials in Biomedical, Food, and Nutraceutical Applications: A Review
PublicationNanotechnology with bionanomaterials have tremendous potential to enhance and utilize for nutrient and bioactive absorption, drug delivery systems, pharmaceutical, and nutraceutical field through various applications. Cellulose nanomaterials are green materials that are obtained from renewable sources and possess exceptional mechanical strength and biocompatibility. The associated unique physical and chemical properties have made...
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The transition of HIV within and between affected populations in Poland
PublicationThe aim of the paper is the estimation of probabilities that describe the transition of HIV within and between the following three populations: homosexual and bisexual men, injecting drug users and heterosexual persons in Poland in the years 1995-2006
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Stable nanoconjugates of transferrin with alloyed quaternary nanocrystals Ag–In–Zn–S as a biological entity for tumor recognition
PublicationOne way to limit the negative effects of anti-tumor drugs on healthy cells is targeted therapy employing functionalized drug carriers. Here we present a biocompatible and stable nanoconjugate of transferrin anchored to Ag-In-Zn-S quantum dots modified with 11-mercaptoundecanoic acid (Tf-QD) as a drug carrier versus typical anticancer drug, doxorubicin. Detailed investigations of Tf-QD nanoconjugates without and with doxorubicin...
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Electrochemistry meets enzymes: Investigation of the biotransformation pathway of C-1311 based on electrochemical simulation in comparison to in vitro methods.
PublicationThe knowledge of the metabolic pathways and the biotransformation of new drugs is one of the major challenges in pharmaceutical research. It is crucial for elucidation of degradation routes of the new biologically active compounds, especially in the area of possible toxicity. Conventional in vitro drug metabolism studies are based on incubating drug candidate with e.g. hepatocytes or, most importantly, liver cell microsomes and...
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Chemosensitization of multidrug resistant Candida albicans by the oxathiolone fused chalcone derivatives
PublicationThree structurally related oxathiolone fused chalcone derivatives appeared effective chemosensitizers, able to restore in part sensitivity to fluconazole of multidrug-resistant C.albicans strains. Compound 21 effectively chemosensitized cells resistant due to the overexpression of the MDR1 gene, compound 6 reduced resistance of cells overexpressing the ABC-type drug transporters CDR1/CDR2 and derivative 18 partially reversed fluconazole...
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The overexpression of CPR and P450 3A4 in pancreatic cancer cells changes the metabolic profile and increases the cytotoxicity and pro-apoptotic activity of acridine antitumor agent, C-1748
PublicationDrug resistance is one of the major cause of pancreatic cancer treatment failure. Thus, it is still imperative to develop new active compounds and novel approach to improve drug efficacy. Here we present 9-amino-1-nitroacridine antitumor agent, C-1748, developed in our laboratory, as a candidate for pancreatic cancer treatment. We examined (i) the cellular response of pancreatic cancer cell lines: Panc-1, MiaPaCa-2, BxPC-3 and...
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Mechanism of Binding of Antifungal Antibiotic Amphotericin B to Lipid Membranes: An Insight from Combined Single-Membrane Imaging, Microspectroscopy, and Molecular Dynamics
PublicationAmphotericin B is a lifesaving polyene antibiotic used in the treatment of systemic mycoses. Unfortunately, the pharmacological applicability of this drug is limited because of its severe toxic side effects. At the same time, the lack of a well-defined mechanism of selectivity hampers the efforts to rationally design safer derivatives. As the drug primarily targets the biomembranes of both fungi and humans, new insights into the...
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Improved cytotoxicity and preserved level of cell death induced in colon cancer cells by doxorubicin after its conjugation with iron-oxide magnetic nanoparticles
PublicationA promising strategy for overcoming the problem of limited efficacy in antitumor drug delivery and in drug release is the use of a nanoparticle-conjugated drug. Doxorubicin (Dox) anticancer chemotherapeutics has been widely studied in this respect, because of severe cardiotoxic side effects. Here, we investigated the cytotoxic effects, the uptake process, the changes in cell cycle progression and the cell death processes in the...
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The influence of ILs on TiO2 microspheres activity towards 5-FU removal under artificial sunlight irradiation
PublicationIn this work, the effect of various ionic liquids (ILs), namely, choline chloride [Chol][Cl], hexadecylpyridynium chloride [HDPy][Cl], and tributylmethylammonium chloride [TBMA][Cl], on the morphology, surface compo-sition in relation to photocatalytic oxidation of 5-fluorouracil (5-FU) and phenol in the presence of TiO2 pho-tocatalysts under artificial sunlight conditions was investigated. The highest photoactivity towards cytostatic...
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Quantification of unconjugated and total ibuprofen and its metabolites in equine urine samples by gas chromatography–tandem mass spectrometry: Application to the excretion study
PublicationIbuprofen (IBU) is a widely used nonsteroidal anti-inflammatory drug (NSAID) in human and also veterinary medicine. NSAIDs are usually highly metabolized compounds in horses; they are often present in equine urine, mostly in their conjugated forms (glucuronides). Thus, hydrolysis to cleave the glucuronide linkage prior to anti-doping analysis is often necessary for improving detection. In this study, unconjugated and total IBU...
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Comparative molecular modelling of biologically active sterols
PublicationMembrane sterols are targets for a clinically important antifungal agent – amphotericin B. The relatively specific antifungal action of the drug is based on a stronger interaction of amphotericin B with fungal ergosterol than with mammalian cholesterol. Conformational space occupied by six sterols has been defined using the molecular dynamics method to establish if the conformational features correspond to the preferential interaction...
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Synthesis of disubstituted 1,3,4,9-tetrahydropyrano-[3,4-b]indole-1-acetic acids derivatives
Publication1,3,4,9-tetrahydropyrano[3,4-b ]indole-1-acetic acid derivatives are of interest for pharmaceutical research as a core structure for synthesis of biological active substance - Etodolac (selective Cyclooxygenase-2 inhibitor, which belongs to the Non-steroidal Anti-inflammatory Drug, NSAID, that shows a clin-ically effective analgesic and anti-inflammatory activity). Here the way of synthesis of two 1,3,4,9-tetrahydropyrano[3,4-b...
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Graphene Production and Biomedical Applications: A Review
PublicationGraphene is a two-dimensional nanomaterial composed of carbon atoms with sp2 hybrid orbitals. Both graphene and graphene-based composite have gained broad interest among researchers because of their outstanding physiochemical, mechanical, and biological properties. Graphene production techniques are divided into top-down and bottom-up synthesis methods, of which chemical vapor deposition (CVD) is the most popular. The biomedical...
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Results of modeling of pharmaceuticals mixtures toxicity with deviation ratio and best-fit functions models using Aliivibrio fischeri bacterium as model organism
Open Research DataThe research was concerned with verifying the impact of mixtures of nine pharmaceuticals against a selected organism, i.e., the bacterium Aliivibrio fischeri. A. fisheri is used as a model organism in the monitoring of acute toxicity in environmental and reference samples in Microtox® systems. Tested pharmaceuticals, namely: diclofenac (sodium salt),...
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A rapid and sensitive method for the quantitative analysis of ibuprofen and its metabolites in equine urine samples by gas chromatography-tandem mass spectrometry
PublicationIbuprofen is widely used in human and veterinary medicine for the treatment of chronic pain as well as rheumatic and musculoskeletal disorders. However, t he anal- gesic and anti-inflammatory properties of Ibuprofen have contributed to frequent drug abuse in equestr ian s ports. A sensitive and rapid gas chromatography with tandem mass spectrometry based method with a simple liquid-liquid extraction and deriva- tization requiring...
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Quantum Dots as a Good Carriers of Unsymmetrical Bisacridines for Modulating Cellular Uptake and the Biological Response in Lung and Colon Cancer Cells
PublicationNanotechnology-based drug delivery provides a promising area for improving the efficacy of cancer treatments. Therefore, we investigate the potential of using quantum dots (QDs) as drug carriers for antitumor unsymmetrical bisacridine derivatives (UAs) to cancer cells. We examine the influence of QD–UA hybrids on the cellular uptake, internalization (Confocal Laser Scanning Microscope), and the biological response (flow cytometry...
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Thermodynamics aspects of interactions between acridine derivatives and DNA
PublicationDNA is a molecular target for many anticancer and antiviral drugs. Therefore, a clear understanding of the interaction of small molecules with DNA is important in the rational design of ligands that can bind to DNA with high affinity and selectivity. There are several methods to investigate interactions between drug and DNA. Some of them measure changing into DNA structures, such as lengthening and untwisting of helix of DNA. Other...
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Naturally-derived hydrogels for 3D pancreatic tumor models: A short review
PublicationStatistics suggest a high proportion of mortality rate by pancreatic cancer, which is a solid tumor characterized by high heterogeneity and the presence of a complex extracellular matrix. The very low effectiveness of pancreatic cancer treatment roots in the high metastatic potential and drug resistance of this tumor. Therefore, the quest for efficient cellular models enabling precise mimicking in vivo conditions, and anticancer...
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Recent breakthroughs in the stability testing of pharmaceutical compounds
PublicationPharmaceutical development is mostly focused on the research leading to approval of a new and viable active substance. However, there is a number of old generation compounds that are still being used in contemporary medicinal practice. So that new analytical developments should cover not only the safety of newly developed drug substances, which is obvious, but should also be directed into the search of individual stability issues...
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Polysaccharide-based electroconductive hydrogels: Structure, properties and biomedical applications
PublicationArchitecting an appropriate platform for biomedical applications requires setting a balance between simplicity and complexity. Polysaccharides (PSAs) play essential roles in our life in food resources, structural materials, and energy storage capacitors. Moreover, the diversity and abundance of PSAs have made them an indispensable part of food ingredients and cosmetics. PSA-based hydrogels have been extensively reviewed in biomedical...
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In vivoevaluation of the CB1allosteric modulator LDK1258 reveals CB1-receptor independent behavioral effects
PublicationIn the present study, we examined whether LDK1258, which produces strong CB1receptor allosteric effects ininvitroassays, would elicitin vivoeffects consistent with allosteric activity. In initial studies, LDK1258 reducedfood consumption and elicited delayed antinociceptive effects in the chronic constrictive injury of the sciaticnerve (CCI) model of neuropathic pain, which unexpectedly emerged 4 h post-injection. UPLC-MS/MS analysisquantified...
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Synthesis, characterization, and interactions of single-walled carbon nanotubes modified with doxorubicin with Langmuir–Blodgett biomimetic membranes
PublicationThe synthesis, characterization, and the influence of single-walled carbon nanotubes (SWCNTs) modified with an anticancer drug doxorubicin (DOx) on the properties of model biological membrane as well as the comparison of the two modes of modification has been presented. The drug was covalently attached to the nanotubes either preferentially on the sides or at the ends of the nanotubes by the formation of hydrazone bond. The efficiency...
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Electrochemistry/mass spectrometry (EC/MS) for fast generation and identification of novel reactive metabolites of two unsymmetrical bisacridines with anticancer activity.
PublicationThe development of a new drug requires knowledge about its metabolic fate in a living organism, regarding the comprehensive assessment of both drug therapeutic activity and toxicity profiles. Electrochemistry (EC) coupled with mass spectrometry (MS) is an efficient tool for predicting the phase I metabolism of redox-sensitive drugs. In particular, EC/MS represents a clear advantage for the generation of reactive drug transformation...
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Targeting Spike‐ACE2 Interface of SARS‐CoV‐2 and its Omicron Variant: A Comparative Screening of Potential Inhibitors for Existing and Anticipating Variants Using Molecular Modelling Approach
PublicationThe recent COVID pandemic has shown major impact on public health and economic crisis. Despite the development of many vaccines and drugs against the severe acute respiratory syndrome (SARS) coronavirus 2, the pandemic still persists. The continued spread of the virus is largely driven by the emergence of viral variants such as α, β, γ, delta, epsilon spike, omicron and its subvariants (BA.1,2,3) which can evade the current vaccines...
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Self-Association of Amphotericin B: Spontaneous Formation of Molecular Structures Responsible for the Toxic Side Effects of the Antibiotic
PublicationAmphotericin B (AmB) is a lifesaving antibiotic used to treat deep-seated mycotic infections. Both the pharmaceutical activity and highly toxic side effects of the drug rely on its interaction with biomembranes, which is governed by the molecular organization of AmB. In the present work we present detailed analysis of self-assembly of AmB molecules in different environments, interesting from the physiological standpoint, based...
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Determination of bromhexine and its metabolites in equine serum samples by liquid chromatography – Tandem mass spectrometry: Applicability to the elimination study after single oral dose
PublicationBromhexine (BH), expectorant used in the treatment of respiratory disorders associated with viscid or excessive mucus, is not permitted for use in the competing horse by many authorities in horseracing and Olympic disciplines. Metabolic studies are of the great importance in anti-doping field because they allow for updating the selection of the most appropriate markers for prohibited substances, such as metabolites present at higher...
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Highly Conserved Homotrimer Cavity Formed by the SARS-CoV-2 Spike Glycoprotein: A Novel Binding Site
PublicationAn important stage in severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) life cycle is the binding of the spike (S) protein to the angiotensin converting enzyme-2 (ACE2) host cell receptor. Therefore, to explore conserved features in spike protein dynamics and to identify potentially novel regions for drugging, we measured spike protein variability derived from 791 viral genomes and studied its properties by molecular...
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Pharmaceutical applications of surfactants
PublicationIn this study we focused on biological activity of various surfactants. According to our research, they con act both as carriers as well as therapeutic agents. Depending on their concentration, they can create different structures in a solution, which influence their properties. Liposomes have a significant role in drug delivery system. Surfactants in from of bilayer are analogous to natural biological cell membrane.
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Problem of aggregation in dye-DNA interaction, calorimetry studies
PublicationNucleic acids are the biological target for many antimicrobial, antitumor and antiviral drugs. Ligand-DNA interactions can be classified into two major categories: 1. covalent binding, which can provide to intermolecular adducts, 2. physico-chemical interactions, which can be divided into intercalation (e.g. adriamycin) or groove binding (e.g. dystamycin). There are several methods to investigate interactions between drug and DNA....
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Data regarding a new, vector-enzymatic DNA fragment amplification-expression technology for the construction of artificial, concatemeric DNA, RNA and proteins, as well as biological effects of selected polypeptides obtained using this method
PublicationApplications of bioactive peptides and polypeptides are emerging in areas such as drug development and drug delivery systems. These compounds are bioactive, biocompatible and represent a wide range of chemical properties, enabling further adjustments of obtained biomaterials. However, delivering large quantities of peptide derivatives is still challenging. Several methods have been developed for the production of concatemers –...
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Ipertrofan Revisited—The Proposal of the Complete Stereochemistry of Mepartricin A and B
PublicationBeing a methyl ester of partricin, the mepartricin complex is the active substance of a drug called Ipertrofan (Tricandil), which was proven to be useful in treatment of benign prostatic hyperplasia and chronic nonbacterial prostatitis/chronic pelvic pain syndrome. Nevertheless, no direct structural evidence on the stereochemistry of its components has been presented to date. In this contribution, we have conducted detailed, NMR-driven...
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Nowe substancje psychoaktywne CZ. II. SYNTETYCZNE KANNABINOIDY - CHARAKTERYSTYKA, METODY OZNACZANIA I WYZWANIA ANALITYCZNE
PublicationDo nielegalnego obrotu co roku trafiają nowe związki o działaniu psychoaktywnym. Dostęp do takich substancji nie jest trudny, gdyż są one łatwo dostępne w wielu krajach, głównie w sklepach internetowych. Ponadto, organy ścigania i wymiar sprawiedliwości nie nadążają z wprowadzaniem tych substancji na listy substancji zakazanych przez co ich kontrola jest bardzo utrudniona. Syntetyczne kannabinoidy to grupa związków chemicznych,...
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Metabolism of antitumour agent 1-nitroacridine derivative, C-1748 in pancreatic cancer cell lines
PublicationPancreatic cancer has the highest mortality rate of all major cancers because of limited treatment options. Surgical removal of the tumour is possible only in its early stage, nevertheless the asymptomatic development very often makes unable an accurate diagnose. In the case of metastatic pancreatic cancer only chemotherapy, mainly with gemcitabine, can be offered to patients. However, common resistance towards gemcitabine imposes...
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New Unsymmetrical Bisacridine Derivatives Noncovalently Attached to Quaternary Quantum Dots Improve Cancer Therapy by Enhancing Cytotoxicity toward Cancer Cells and Protecting Normal Cells
PublicationThe use of nanoparticles for the controlled drug delivery to cells has emerged as a good alternative to traditional systemic delivery. Quantum dots (QDs) offer potentially invaluable societal benefits such as drug targeting and in vivo biomedical imaging. In contrast, QDs may also pose risks to human health and the environment under certain conditions. Here, we demonstrated that unique combination of nanocrystals core components...
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Impact of inorganic ions and pH variations on toxicity and endocrine potential of selected environmentally relevant pharmaceuticals
PublicationAssessment of the impact of pharmaceutical residues on living organisms is a very complex subject. Apart from taking into account the toxicity of individual compounds, environmental factors should also be taken into account. In this paper, attempts were made to assess the impact of coexisting inorganic ions and changes in pH on the toxicity of ten selected pharmaceuticals. Two bioassays were used to measure the estrogenic and androgenic...
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Detection of propofol concentrations in blood by Raman spectroscopy
PublicationIn this paper we present a proof-of-concept of a Raman spectroscopy-based approach for measuring the content of propofol, a common anesthesia drug, in whole human blood, and plasma, which is intended for use during clinical procedures. This method utilizes the Raman spectroscopy as a chemically–sensitive method for qualitative detection of the presence of a drug and a quantitative determination of its concentration. A number of...
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2D MXene nanocomposites: electrochemical and biomedical applications
PublicationIn recent years, key questions about the interaction of 2D MXene nanomaterials in electrochemical and biomedical applications have been raised. Most research has focused on clarifying the exclusive properties of the materials; however, only limited reports have described the biomedical applications of 2D nanomaterials. 2D MXenes are monolayer atomic nanosheets resulting from MAX phase ceramics. The hydrophilic properties, metallic...
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Nowe substancje psychoaktywne. Cz. I. Współczesna sytuacja narkotykowa
PublicationGwałtowny wzrost liczby substancji wprowadzanych na rynek narkotykowy został zaobserwowany już pod koniec lat dziewięćdziesiątych XX wieku. Każdego roku syntezowane są nowe substancje jako analogi już istniejących, a ich ilość systematycznie rośnie. Niejednokrotnie wprowadzenie niewielkiej zmiany w strukturze związku może spowodować znaczne zmiany ich właściwości fizykochemicznych oraz psychoaktywnych. Nowe substancje psychoaktywne...
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Factors causing degradation of sulfadimetoxine
PublicationSulfadimetoxine is a representative of sulfonamide drugs which presence inhibits growth of activated sludge bacteria, rhat is necessary for the effective mineralization of organic and inorganic contaminants. Therefore factors which con prevent this situation are searched. Aim of this study is selection of conditions causing efficien degradation of the drug- sulfadimetoxine. The impact of such aspects as : the type of oxidizing...
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Thermodynamics and kinetics of amphotericin B self-association in aqueous solution characterized in molecular detail
PublicationAmphotericin B (AmB) is a potent but toxic drug commonly used to treat systemic mycoses. Its efficiency as a therapeutic agent depends on its ability to discriminate between mammalian and fungal cell membranes. The association of AmB monomers in an aqueous environment plays an important role in drug selectivity, as oligomers formed prior to membrane insertion – presumably dimers – are believed to act differently on fungal (ergosterol-rich)...
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Mechanism-based inactivation of human cytochrome P450 1A2 and 3A4 isoenzymes by antitumor triazoloacridinone C-1305.
Publication5-Dimethylaminopropylamino-8-hydroxytriazoloacridinone, C-1305, is a promising antitumor therapeutic agent with high activity against several experimental tumors. It was determined to be a potent and selective inhibitor of liver microsomal and human recombinant cytochrome P450 (CYP) 1A2 and 3A4 isoenzymes. Therefore, C-1305 might modulate the effectiveness of other drugs used in multidrug therapy. The objective of this study was...
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Visualizing Carotid Bodies With Doppler Ultrasound Versus CT Angiography: Preliminary Study
PublicationOBJECTIVE. 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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Alkohol-społeczny problem XXI wieku. Zastosowanie biowskaźników spożywania alkoholu w diagnostyce medycznej.
PublicationAlkohol etylowy jest legalną i ogólnodostępną substancją o działaniu psychoaktywnym. Spożywany w niewielkich ilościach może pozytywnie wpływać na zdrowie, ale jego nadmierna konsumpcja powoduje silne uzależnienie. Może być to przyczyną agresywnych zachowań, przemocy w rodzinie, problemów w kontaktach z ludźmi, problemów z prawem, samobójstw, wypadków samochodowych oraz problemów finansowych. Dlatego też, szybka i jednoznaczna diagnostyka...
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Molecular detection of Candida krusei
PublicationThe 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
PublicationOur 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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Natural Deep Eutectic Solvents as Agents for Improving Solubility, Stability and Delivery of Curcumin
PublicationPurpose Study on curcumin dissolved in natural deep eutectic solvents (NADES) was aimed at exploiting their beneficial properties as drug carriers. Methods The concentration of dissolved curcumin in NADES was measured. Simulated gastrointestinal fluids were used to determine the concentration of curcumin and quantum chemistry computations were performed for clarifying the origin of curcumin solubility enhancement in NADES. Results NADES...
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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
PublicationHigh 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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Evaluation of possibilities in identification and susceptibility testing for Candida glabrata clinical isolates with the Integral System Yeast Plus (ISYP)
PublicationThe 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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The Substantial Improvement of Amphotericin B Selective Toxicity Upon Modification of Mycosamine with Bulky Substituents
PublicationAbstract: 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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Imidazoacridinone-dependent lysosomal photodestruction: a pharmacological Trojan horse approach to eradicate multidrug-resistant cancers
PublicationMultidrug 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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Phase I and phase II metabolism simulation of antitumor-active 2-hydroxyacridinone with electrochemistry coupled on-line with mass spectrometry.
PublicationHere, 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
PublicationLow 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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Foliate-Targeting Quantum Dots-β-Cyclodextrin Nanocarrier for Efficient Delivery of Unsymmetrical Bisacridines to Lung and Prostate Cancer Cells
PublicationTargeted drug delivery by nanocarriers molecules can increase the efficiency of cancer treatment. One of the targeting ligands is folic acid (FA), which has a high affinity for the folic acid receptors, which are overexpressed in many cancers. Herein, we describe the preparation of the nanoconjugates containing quantum dots (QDs) and β-cyclodextrin (β-CD) with foliate-targeting properties for the delivery of anticancer compound...
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Molecular mechanism of proton-coupled ligand translocation by the bacterial efflux pump EmrE
PublicationThe 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
PublicationIn 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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Electrochemical simulation of enzymatic transformations studied for the selected antitumor acridine derivatives
PublicationThe 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
PublicationThe 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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Tailoring the electrochemical degradation of iron protected with polypyrrole films for biodegradable cardiovascular stents
PublicationThe 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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Synthesis and biological activity of ester derivatives of mycophenolic acid and acridines/acridones as potential immunosuppressive agents
PublicationImproved 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
PublicationCancer 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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Docking simulations, Molecular properties and ADMET studies of novel Chromane6,7diol analogues as potential inhibitors of Mushroom tyrosinase
PublicationResearch 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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Intermolecular Interactions as a Measure of Dapsone Solubility in Neat Solvents and Binary Solvent Mixtures
PublicationDapsone 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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Cell Density-Dependent Cytological Stage Profile and Its Application for a Screen of Cytostatic Agents Active Toward Leukemic Stem Cells
PublicationProliferation 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...
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Activation Energy and Inclination Magnetic Dipole Influences on Carreau Nanofluid Flowing via Cylindrical Channel with an Infinite Shearing Rate
PublicationThe 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,...