Search results for: Z-DRUGS
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Nonsteroidal anti-inflammatory drugs modulate cellular glycosaminoglycan synthesis by affecting EGFR and PI3K signaling pathways
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Study of the chromatographic behavior of selected antipsychotic drugs on RP-TLC based on quantitative structure–retention relationships
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Extracting functional groups of ALLINI to design derivatives of FDA‐approved drugs: Inhibition of HIV‐1 integrase
PublicationHIV‐1 integrase (IN) is crucial for integration of viral DNA into the host genome and a promising target in development of antiretroviral inhibitors. In this work, six new compounds were designed by linking the structures of two different class of HIV‐1 IN inhibitors (active site binders and allosteric IN inhibitors (ALLINIs)). Among newly designed compounds, INRAT10b was found most potent HIV‐1 IN inhibitor considering different...
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Removal of nonsteroidal anti-inflammatory drugs and analgesics from wastewater by adsorption on cross-linked β-cyclodextrin
PublicationWe present a method using the material in the form of cross-linked β-cyclodextrin (CD) showing high efficiency in the simultaneous removal of hazardous pollutants from sewage, such as diclofenac (DIC), ibuprofen (IBU), ketoprofen (KETO), naproxen (NAPR), salicylic acid (SALI) and tramadol (TRAM). The material is stable and particularly easy to regenerate. The sorbent probably remembers the shape of the contaminants, which increases...
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Ti/TiO2 nanotubes sensitized PbS quantum dots as photoelectrodes applied for decomposition of anticancer drugs under simulated solar energy
PublicationOne of the challenges in research into photoelectrocatalytic (PEC) degradation of pollutants is finding the appropriate photoanode material, which has a significant impact on the process efficiency. Among all others, photoelectrodes based on an ordered TiO2 nanotube arrays are a promising material due to well-developed surface area and efficient charge separation. To increase the PEC activity of this material, the SILAR method was...
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Current View on Green Tea Catechins Formulations, Their Interactions with Selected Drugs, and Prospective Applications for Various Health Conditions
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Comparison of the Usefulness of SPE Cartridges for the Determination ofβ-Blockers andβ-Agonists (Basic Drugs) in Environmental Aqueous Samples
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Legal and economic identification and assessment of pharmacy substitution in narrow therapeutic index drugs, on the example of epileptic medications in Poland
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Maternal immune activation leads to age-related behavioral and immunological changes in male rat offspring - the effect of antipsychotic drugs
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The role of fluids in high-pressure polymorphism of drugs: different behaviour of β-chlorpropamide in different inert gas and liquid media
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Determination of nonsteroidal antiinflammatory drugs in water samples using liquid chromatography coupled with diode-array detector and mass spectrometry
PublicationOpracowano i zwalidowano metodykę do oznaczania śladowych ilości sześciu różnych związków z grupy niesteroidowych leków przeciwzapalnych w próbkach wodnych. Anality zostały wybrane spośród najczęsciej sprzedawanych leków w Polsce. Sprawdzono kilka różnych kolumienek ekstrakcyjnych i wybrano RP-18 jako najlepsze wypełnienie do wzbogacania oznaczanych związków. Opracowaną metodykę z powodzeniem zastosowano do analizy próbek rzeczywistych.
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Recovery of Nonsteroidal Anti-Inflammatory Drugs from Wastes Using Ionic-Liquid-Based Three-Phase Partitioning Systems
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Evaluation and cellular responses of modulators of TRF1/TRF2 protein’s function as potential anticancer drugs interfering with telomeric shelterin’s function
PublicationA number of proteins that interact with telomeres have been identified in human cells, indicating the high plasticity of human nucleoprotein complex organization. The most important complex is the "shelterin" complex, which consists of six proteins: TRF1, TRF2, TIN2, POT1, TPP1. The TRF1 and TRF2 directly bind to telomeric double-stranded DNA and the TIN2 protein. The TIN2 protein also binds to the TPP1 protein, stabilizing the...
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Systematic review of the effect of D‑mannose with or without other drugs in the treatment of symptoms of urinary tract infections/cystitis (Review)
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Quantitative structure—retention relationship modeling of the retention behavior of selected antipsychotic drugs in normal-phase thin-layer chromatography
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Piperine Targets Different Drug Resistance Mechanisms in Human Ovarian Cancer Cell Lines Leading to Increased Sensitivity to Cytotoxic Drugs
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Is sequential batch reactor an efficient technology to protect recipient against non-steroidal anti-inflammatory drugs and paracetamol in treated wastewater?
PublicationThe tested facility was a wastewater treatment plant (WWTP) in Swarzewo, where the wastewater treatment takes place in aeration chambers with activated sludge using sequential batch reactors (SBRs). The concentration of the following pharmaceuticals: ibuprofen, paracetamol, flurbiprofen, naproxen, diclofenac, and its metabolites 5OH-diclofenac and 4OH-diclofenac was tested in influents and effluents. Simultaneously, the conventional...
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Design, synthesis and biological evaluation of novel N-phosphorylated and O-phosphorylated tacrine derivatives as potential drugs against Alzheimer’s disease
PublicationIn this work, we designed, synthesised and biologically investigated a novel series of 14N- and O-phosphorylated tacrine derivatives as potential anti-Alzheimer’s disease agents. In the reaction of 9-chlorotacrine and corresponding diamines/aminoalkylalcohol we obtained diamino and aminoalkylhydroxy tacrine derivatives. Next, the compounds were acid to give final products 6–13 and 16–21 that were characterised by 1H, 13 C, 31P...
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Iso-Partricin, an Aromatic Analogue of Amphotericin B: How Shining Light on Old Drugs Might Help Create New Ones
PublicationPartricin is a heptaene macrolide antibiotic complex that exhibits exceptional antifungal activity, yet poor selective toxicity, in the pathogen/host system. It consists of two compounds, namely partricin A and B, and both of these molecules incorporate two cis-type bonds within their heptaenic chromophores: 28Z and 30Z. In this contribution, we have proven that partricins are susceptible to a chromophore-straightening photoisomerization...
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Letter to the editor on the article “Alteration of redox status by commonly used antimalarial drugs in the north-western region of Nigeria” by Muhammad A et al.
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A new pH/organic modifier gradient RP HPLC method for convenient determination of lipophilicity and acidity of drugs as applied to established imidazoline agents
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Determination of non-steroidal anti-inflammatory drugs in natural waters using off-line and on-line SPE followed by LC coupled with DAD-MS
PublicationOpisano dwie metody pozwalające na jednoczesne oznaczanie zawartości niesterydowych leków przeciwzapalnych (difluisal, diklofenak, naproksen, tolmetin, fenoprofen, ibuprofen) w próbkach wodnych. Próbki przygotowywano do analizy z użyciem techniki ekstrakcji do fazy stałej (off-line i on-line). Natomiast oznaczeń końcowych dokonano z użyciem LC-DAD-MS. Sprawdzono kilka różnych kolumienek ekstrakcyjnych i wybrano RP-18 jako najlepsze...
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Mirosław Andrusiewicz prof. dr hab. n. med. i n. o zdr.
PeopleDiplomas, degrees conferred in specific areas ̶ Post-doctoral degree in medical sciences (doctor habilitated) (discipline: medical biology) December 4, 2017; Title of academic achievement: "Analysis of selected genes involved in the control of pathological changes in cells derived from internal female reproductive organs"; Poznan University of Medical Sciences, Faculty of Medicine II; re-viewers: Prof. Katarzyna Ziemnicka,...
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A new silylating reagent – dimethyl(3,3,3-trifluoropropyl)silyldiethylamine – for the derivatisation of non-steroidal anti-inflammatory drugs prior to gas chromatography–mass spectrometry analysis
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Discovery of small-molecule regenerative drugs using a model of complex tissue injury in mice. Transcriptomic responses of neurodevelopmental genes during pharmacologically induced regeneration
PublicationDespite significant development in regenerative medicine, there is a deficit of effective therapies for wound healing and tissue regeneration. Research performed using animal wound models allows for a better understanding of this complex process, searching for compounds with pro-regenerative properties, and assessing their efficacy and safety. Unfortunately, the lack of adequate preclinical models proves to be an issue as no animal...
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Jakub Miler dr inż.
PeopleAcademic career: 2000: Master of Science - Gdansk University of Technology, Faculty of Electronics, Telecommunications and Informatics, thesis "Computer system for supporting risk management in a software engineering project", supervisor prof. Janusz Górski 2005: PhD - Gdansk University of Technology, Faculty of Electronics, Telecommunications and Informatics, thesis "A Method of Software Project Risk Identification and Analysis",...
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Enhanced Activity of P4503A4 and UGT1A10 Induced by Acridinone Derivatives C-1305 and C-1311 in MCF-7 and HCT116 Cancer Cells: Consequences for the Drugs’ Cytotoxicity, Metabolism and Cellular Response
PublicationActivity modulation of drug metabolism enzymes can change the biotransformation of chemotherapeutics and cellular responses induced by them. As a result, drug-drug interactions can be modified. Acridinone derivatives, represented here by C-1305 and C-1311, are potent anticancer drugs. Previous studies in non-cellular systems showed that they are mechanism-based inhibitors of cytochrome P4503A4 and undergo glucuronidation via UDP-glucuronosyltranspherase...
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Simultaneous analysis of non-steroidal anti-inflammatory drugs and estrogenic hormones in water and wastewater samples using gas chromatography–mass spectrometry and gas chromatography with electron capture detection
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Anna Toruńska-Sitarz
PeopleAnna Toruńska-Sitarz, Msc in Oceanography, PhD in Earth Sciences. She is a cyanobacteriologist and academic teacher, working in the Division of Marine Biotechnology, University of Gdańsk. Her main scientific interests concern antibacterial compounds from marine organisms, regulation of cyanometabolites production in cyanobacteria and cyanobacterial molecular diversity. Further information
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Sulfonamides with hydroxyphenyl moiety: Synthesis, structure, physicochemical properties, and ability to form complexes with Rh(III) ion
PublicationSulfonamides are the first successfully synthesized antimicrobial drugs. The mechanism of sulfonamides’ antimicrobial action involves competitive inhibition of folic acid synthesis and prevention of the growth and reproduction of bacteria. Even though they have been applied in therapy for more than 75 years, sulfonamides are still the drugs of choice for the treatment of various diseases. The aim of this work was to synthesize...
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Feasibility study of a Raman spectroscopic route to drug detection
PublicationWe present an surface-enhanced Raman spectroscopy (SERS) approach for detection of drugs of abuse in whole human blood. We utilize a near infrared laser with 830 nm excitation wavelength in order to reduce the influence of fluorescence on the spectra of blood. However, regular plasmon resonance peak of plasmonic nanoparticles, such as silver or gold fall in a much lower wavelength regime about 400 nm. Therefore, we have shifted...
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Application of bioassays in studies on the impact of pharmaceuticals on the environment
PublicationDrug interactions are often desirable particularly in medicine, when treatment of a patient requires using a mixture of drugs in specific doses to produce the adequate therapeutic effect. Unfortunately, interactions between drugs in the environment are not as desirable, despite the fact that drugs are present in the environment at low concentration levels [1]. Pharmaceuticals are present in the environment in a mixture of compounds,...
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Natural Products Counteracting Cardiotoxicity during Cancer Chemotherapy: The Special Case of Doxorubicin, a Comprehensive Review
PublicationCardiotoxicity is a frequent undesirable phenomenon observed during oncological treatment that limits the therapeutic dose of antitumor drugs and thus may decrease the effec-‐‑ tiveness of cancer eradication. Almost all antitumor drugs exhibit toxic properties towards cardiac muscle. One of the underlying causes of cardiotoxicity is stimulation of oxidative...
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pH-dependent composite coatings for controlled drug delivery system - Review
PublicationNowadays in case of long-term implants, the most common postoperative complications are bacterial infections, which in consequence may provoke loos- ening of the implants in the primary phase of stabilization. Bacterial infections are currently the most frequent cause of revision surgery of the implants such as hip joint endoprosthesis, knee joint endoprosthesis and dental implants. In order to provide the local and long-term antibacterial...
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Targeting DNA Topoisomerase II in Antifungal Chemotherapy.
PublicationTopoisomerase inhibitors have been in use clinically for the treatment of several diseases for decades. Although those enzymes are significant molecular targets in antibacterial and anticancer chemotherapy very little is known about the possibilities to target fungal topoisomerase II (topo II). Raising concern for the fungal infections, lack of effective drugs and a phenomenon of multidrug resistance underlie a strong need to expand...
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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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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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Approaches Towards Better Immunosuppressive Agents
PublicationSeveral classes of compounds are applied in clinics due to their immunosuppressive properties in transplantology and the treatment of autoimmune diseases. Derivatives of mycophe-nolic acid, corticosteroids and chemotherapeutics bearing heterocyclic moieties like methotrexate, azathioprine, mizoribine, and ruxolitinib are active substances with investigated mechanisms of action. However, improved synthetic approaches of known drugs...
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An Approach to Trust Case Development
PublicationIn the paper we present an approach to the architectural trust case development for DRIVE, the IT infrastructure supporting the processes of drugs distribution and application. The objectives of DRIVE included safer and cheaper drugs distribution and application. A trust case represents an argument supporting the trustworthiness of the system. It is decomposed into claims that postulate some trust related properties. Claims differ...
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Application of GC-MS/MS technique for the determination of benzodiazepines in blood samples
PublicationAbstract Benzodiazepines (BZD) are widely used as pharmaceuticals in medicine. However, due to psychostimulatory effect of BZD, in the last decade, they are more and more often used as drugs of abuse. These compounds produce similar effects to classical illicit drugs and are sold as “legal” alternatives to them as new psychoactive substances (NPS). Currently new BZD, named designer benzodiazepines (DBZD), are synthesized each year...
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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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Determination of 3,4-methylenedioxy-α-pyrrolidinobutiophenone (MDPB) in blood. A case report
PublicationSynthetic drugs, known as ‘‘legal highs’’, are still very popular on black market. The determination of their composition are required in courts of law and also to understand what potential users may be subjected to. The interest of new cathinones, e.g. MDPBP, is in view of psychoactive effects that they cause and that, in many cases, they are not controlled by law. The case outlined here concerns 19 years-old man, who was found...
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VUV photofragmentation of the six-membered heterocyclic molecules containing oxygen
PublicationCancer is a significant public health concern worldwide, which results in millions of deaths each year. The standard cure routine for cancer is surgery, and nowadays, radiotherapy or a hadrontherapy. Depending on the type of cancer, patients may undergo additional treatment, including targeted therapy. A combination of radio- or hadron-therapy with proper drug treatment can inhibit the proliferation of cancer cells and thus can...
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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.
PublicationThe 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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Applications of Raman spectroscopy for detection of selected substances in tissues
PublicationThis dissertation explores the applications of Raman spectroscopy for biological tissue analysis. Basics of Raman and surface-enhanced Raman spectroscopy (SERS) are described, along with an analysis of the literature on biodetection and non-invasive blood analysis with emphasis on glucose detection. Instrumentation for Raman measurements is described. The sources of noise and interferences occurring in biological tissue measurements...
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Analysis of friction ridge evidence for trace amounts of paracetamol in various pharmaceutical industries by Raman spectroscopy
PublicationThe detection of potentially harmful substances presents a multifaceted challenge. On one hand, it can directly save lives, on the other, it can significantly aid and enhance police work, thereby increasing the effectiveness of investigations. The research conducted in this study primarily aims to identify paracetamol in fingerprints, considering situations involving direct contact of a person with paracetamol either chronically...
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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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Radiosensitization of DNA in presence of Pt(II)-based compounds
PublicationX-ray irradiation of plasmid DNA in presence of platinum (II)-based compounds was carried out in order to assess the radiosensitization capabilities of these drugs. In present investigations pBR322 plasmid DNA was used to monitor the effectiveness of chosen compounds in inducing strand breaks. Samples were incubated in the presence of potential radiosensitisers: platinum (II) bromide and cis-diamminedibromoplatinum (II). The results...
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Environmentally Oriented Models and Methods for the Evaluation of Drug x Drug Interaction Effects
PublicationThis detailed review compares known and widely used methods for drug interaction estimation, some of which now have historical significance. Pharmaceutical application has been noted as far back as several thousand years ago. Relatively late in the 20th century, however, researchers became aware that their fate and metabolism, which still remain a great challenge for environmental analysts and risk assessors. For the patient’s...
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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...