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The Effect of PEG Concentration on the Release Rate of Cisplatin from PEG-Modified Silica Xerogels
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Silica-Polyethylene Glycol Matrix Synthesis by Sol-Gel Method and Evaluation for Diclofenac Diethyloammonium Release
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Potential of mucoadhesive chitosan glutamate microparticles as microbicide carriers – antiherpes activity and penetration behavior across the human vaginal epithelium
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Ustalanie konfiguracji absolutnej drugorzędowych alkoholi przy użyciu monosacharydów jako sondy chiralnej
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Does the chemical modification of Nystatin A1 affect the drug's ability to overcome the multidrug resistance of fungi?
PublicationAlthough the contemporary medicine keeps moving forward, disseminated infections caused by fungal pathogens are an emerging challenge. The dramatic rise of fungal diseases, especially the most life-threatening systemic mycoses is associated with a permanently growing number of immunodeficient patients. Undoubted difficulties in the treatment of fungal infections are caused by lack of highly effective and selective antifungal drugs,...
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Drugs and driving
PublicationW referacie przedstawiono we wprowadzeniu pojawienie się nowego zagrożenia, jakim jest kierowanie pojazdów przez osoby będące pod wpływek narkotyków. W drugiej części przedstawiono obecnie obowiązujące sankcje, jakie mogą spotkać kierującego oraz definicję środków odurzających, po zażyciu których nie można prowadzić samochodu. W trzeciej części przedstawiono badania naukowe przeprowadzone w Polsce i Niemczech, które pokazują jak...
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„Ach, te to, książki zbójeckie” – z drugiego obiegu w Gdańsku
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DRUGS
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Mosty stalowe na Wiśle wybrane realizacje drugiego dziesięciolecia XXI wieku
PublicationW artykule przedstawiono ostatnio zrealizowane mosty przez Wisłę z przęsłami stalowymi: Most Północny w Warszawie, Most przez Wisłę w Toruniu, Most przez Wisłę w Połańcu.
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Amphotericin B and Its New Derivatives - Mode of Action
PublicationAmphotericin B (AmB) is a well known antifungal and antiprotozoal antibiotic used in the clinic for several decades. Clinicalapplications of AmB, however, are limited by its nephrotoxicity and many other acute side effects which are not acceptable by patientswhen their life is not threaten. In order to improve the therapeutic index of this drug, lipid formulations have been introduced and manyefforts have been made to obtain less...
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Phosphate and Thiophosphate Biphenyl Analogs as Steroid Sulfatase Inhibitors
PublicationIn the present work, we report convenient methods for the synthesis and biological evaluation of phosphate and thiophosphate biphenyl derivatives exhibiting steroid sulfatase (STS) activity. The described synthesis is based on straightforward preparation of biphenyl-4-ol and 40-hydroxybiphenyl- 4-carboxylic acid ethyl ester modified with various phosphate or thiophosphate moieties. The inhibitory effects of these compounds were...
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In silico design of telomerase inhibitors.
PublicationTelomerase is a reverse transcriptase enzyme involved in DNA synthesis at the end of linear chromosomes. Unlike in most other cells, telomerase is reactivated most cancerous cells and, therefore, has become a promising new anticancer target. Despite extensive research, direct telomerase inhibitors have yet not been introduced to the clinics because of the complexity of this enzyme. Structures of this protein from simple organisms...
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Metabolic transformation of antitumor acridinone C-1305 but not C-1311 via selective cellular expression of UGT1A10 increases cytotoxic response: implications for clinical use.
PublicationThe acridinone derivates C-1305 and C-1311 are promising antitumor agents with high activity against several experimental cellular and tumor models and which are under evaluation in pre-clinical and early phase clinical trials. Recent evidence from our laboratories has indicated that both compounds were conjugated by several UGT isoforms with the most active being extrahepatic UGT1A10. The present studies were designed to test...
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Role of Human UDP-Glucuronosyltransferases in the Biotransformation of the Triazoloacridinone and Imidazoacridinone Antitumor Agents C-1305 and C-1311 : Highly Selective Substrates for UGT1A10
Publication5-Diethylaminoethylamino-8-hydroxyimidazoacridinone, C-1311 (NSC-645809), is an antitumor agent shown to be effective against breast cancer in phase II clinical trials. A similar compound, 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone, C-1305, shows high activity against experimental tumors and is expected to have even more beneficial pharmacological properties than C-1311. Previously published studies showed that these...
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Steroid Sulfatase Inhibitors Based on Phosphate and Thiophosphate Flavone Analogs
PublicationA series of phosphate and thiophosphate flavone derivatives were synthesized and biologically evaluated in vitro for inhibition of steroid sulfatase (STS) activity. The described synthesis includes the straightforward preparation of 7-hydroxy-2-phenyl-4H-chromen-4-one 3a, 2-(4-fluorophenyl)-7-hydroxy-4H-chromen-4-one 3b, 7-hydroxy-2-(4-(trifluoromethyl)phenyl)-4H-chromen-4-one 3c, 7-hydroxy-2-(p-tolyl)-4H-chromen-4-one 3d modified...
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Acridinone antitumor agents: C-1311, C-1330 and C-1305 are metabolized by flavin-containing monooxygenase isoenzymes: FMO1, FMO3 and FMO5 with different rates
PublicationRekombinantowe ludzkie monooksygenazy flawinowe: FMO1, FMO3, FMO5 indukują przemiany metaboliczne wybranych do badań pochodnych akrydonu. Biotransformacja związków C-1311, C-1330 i C-1305 przez FMO prowadzi do jednego produktu o strukturze N-tlenku. Wyniki badań wskazują, że najbardziej podatna na przemiany wobec FMO jest pochodna triazoloakrydonu C-1305. Wydaje się więc, że głównymi enzymami pierwszej fazy przemian metabolicznych...
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Novel steroid sulfatase inhibitors based on N ‐thiophosphorylated 3‐(4‐aminophenyl)‐coumarin‐7‐O‐sulfamates
PublicationIn the present work, we described convenient methods for the synthesis ofN-thiophosphorylated 3-(4-aminophenyl)-coumarin-7-O-sulfamates as steroid sulfatase(STS) inhibitors. To design the structures of the potential STS inhibitors, molecularmodeling techniques were used. A computational docking method was used to deter-mine the binding modes of the synthesized inhibitors as well as to identify potentialinteractions between specified...
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Genotoxicity of selected pharmaceuticals, their binary mixtures, and varying environmental conditions – study with human adenocarcinoma cancer HT29 cell line
PublicationPharmaceutical residues are present in the environment in mixtures and their adverse effects may also result from interactions that occur between compounds. Studies presented in this work focus on genotoxicity of pharmaceuticals from different therapeutic groups in mixtures and in individual solutions impacted with different environmental conditions assessed using comet assay (alkaline approach). Binary mixtures of pharmaceuticals...
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Targeting shelterin proteins for cancer therapy.
PublicationAs a global health challenge, cancer prompts continuous exploration for innovative therapies that are also based on new targets. One promising avenue is targeting the shelterin protein complex, a safeguard for telomeres crucial in preventing DNA damage. The role of shelterin in modulating ataxia- telangiectasia mutated (ATM) and ataxia-telangiectasia and Rad3-related (ATR) kinases, key players in the DNA damage response (DDR),...
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Human carnosinases: A brief history, medicinal relevance, and in silico analyses
PublicationCarnosine, an endogenous dipeptide, has been found to have a plethora of medicinal properties, such as antioxidant, antiageing, and chelating effects, but with one downside: a short half-life. Carnosinases and two hydrolytic enzymes, which remain enigmatic, are responsible for these features. Hence, here we emphasize why research is valuable for better understanding crucial concepts like ageing, neurodegradation, and cancerogenesis,...
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The role of intestine and liver in glucuronidation of the imidazo- and triazoloacridinone antitumor agents, C-1311 and C-1305: High affinity substrates for UGT1A10
PublicationCelem przeprowadzonych badań było określenie roli poszczególnych izoform UDP-glukuronylotransferazy (UGT)oraz mikrosomów jelita(HIM)i wątroby (HLM) wyizolowanych od różnych pacjentów w metabolizmie pochodnych akrydonu, związków C-1311 i C-1305. Wykazano, że rodziną UGT katalizującą przemiany C-1305 i C-1311 jest UGT1A, z najwyższą aktywnością wykazywaną przez pozawątrobowy izoenzym UGT1A10. Rozkład aktywności frakcji mikrosomalnych...
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Biotransformation of abused synthetic cannabinoids, JWH-018 and JWH-073, by human cytochromes P450 and UDP-glucuronosyltransferases
PublicationZwiązki oznaczone symbolami JWH-018 i JWH-073 są syntetycznymi pochodnymi kanabinoidów, obecnymi w preparatach o działaniu psychoaktywnym (K2/Spice). Wcześniejsze badań wykazały, że u osób przyjmujących tzw. ''legalną marihuanę'', głównymi produktami biotransformacji obecnymi w moczu były hydroksylowe pochodne obu związków, jak również ich glukuronidy. W związku z tym celem prowadzonych badań było określenie roli poszczególnych...
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Complexation of Bioelements and Toxic Metals by Polyphenolic Compounds - Implications for Health
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Population analysis to assess the influence of age and body weight on pharmacokinetics and pharmacodynamics of dexmedetomidine in New Zealand White rabbits
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Acute and subacute (28-Day) toxicity studies of ionic liquid, didecyldimethyl ammonium acesulfamate, in rats
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The pharmacokinetics of propofol in ICU patients undergoing long-term sedation
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The quantification of reticulocyte maturation and neocytolysis in normal and erythropoietin stimulated rats
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Potential of Liquid Biopsy in Papillary Thyroid Carcinoma in Context of miRNA, BRAF and p53 Mutation
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Genetic Determinants of Vitamin D-Related Disorders; Focus on Vitamin D Receptor
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Morphine and methadone pre-exposures differently modify brain regional Fos protein expression and locomotor activity responses to morphine challenge in the rat
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<p>Potential effects of microbial air quality on the number of new cases of diabetes type 1 in children in two regions of Poland: a pilot study</p>
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Prolonged Quercetin Administration Diminishes the Etoposide-Induced DNA Damage in Bone Marrow Cells of Rats
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Protective Effect of Aronia Melanocarpa Polyphenols on Cadmium Accumulation in the Body: A Study in a Rat Model of Human Exposure to this Metal
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Aqueous Extracts of Selected Potentilla Species Modulate Biological Activity of Human Normal Colon Cells
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New Insights into Dietary Supplements Used in Sport: Active Substances, Pharmacological and Side Effects
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Antioxidants as a Potential Preventive and Therapeutic Strategy for Cadmium
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Rheological Characteristics of Novel Meloxicam-Loaded Complex Organogels Based on Fumed Silica and Poloxamer
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Current status of liposomal porphyrinoid photosensitizers
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Vitamin D Metabolism Gene Polymorphisms and Their Associated Disorders: A Literature Review
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Preliminary Study on the Antibacterial Activity of Essential Oils Alone and in Combination with Gentamicin Against Extended-Spectrum β-Lactamase-Producing and New Delhi Metallo-β-Lactamase-1-Producing Klebsiella pneumoniae Isolates
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Bacteriophage–Ciprofloxacin Combination Effectiveness Depends on Staphylococcus aureus–Candida albicans Dual-Species Communities’ Growth Model
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Biofilm Formation and Prevalence of Biofilm-Related Genes Among Clinical Strains of Multidrug-Resistant Staphylococcus aureus
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Environmental Phage-Based Cocktail and Antibiotic Combination Effects onAcinetobacter baumanniiBiofilm in a Human Urine Model
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The Effect of Subinhibitory Concentrations of trans-Anethole on Antibacterial and Antibiofilm Activity of Mupirocin Against Mupirocin-Resistant Staphylococcus aureus Strains
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Polyurethanes as a carrier of drugs for gentamicin
PublicationGentamicin is one of the most popular drug and is widely used due to its antibiotic properties. 3% of world production of polyurethanes (PU) is dedicated to biomedical applications, where they can serve are parts of orthopedic prosthesis or artificial organs, disposable medical devices, wound and burn dressing, contact lenses among others. In the study, to obtain drug carriers, a combination of these two materials were prepared...
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Analiza wrażliwości pierwszego i drugiego rzędu w problemach statyki prętów cienkościennych
PublicationAnaliza wrażliwości pierwszego rzędu jest wykorzystywana w wielu zagadnieniach teorii konstrukcji. Pomimo tego, że analiza wrażliwości drugiego rzędu pozwala na znaczną poprawę dokładności uzyskiwanych wyników, jest ona mniej popularna niż analiza pierwszego rzędu. W pracy wyznaczono drugą wariację zmiennych stanu zachowania się konstrukcji. Przyjęto klasyczne założenia teorii prętów cienkościennych. W przykładzie numerycznym wyznaczono...
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Primary degradation of antidiabetic drugs
PublicationType 2 diabetes is a chronic disease affecting a large portion of the world population and is treated by orally administered drugs. Since these drugs are often taken in high doses and are excreted unchanged or partially metabolised many of them are nowadays detected in surface waters or wastewater treatment plants effluents. Unmetabolised antidiabetics or some of their transformation products retain their pharmacological activity,...
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Analiza modalna konstrukcji podpierającej stanowiska badawczego dynamiki małogabarytowych wirników część druga - badania symulacyjne
PublicationCelem niniejszej pracy było przedstawienie badań eksperymentalnych oraz symulacyjnych stanowiska VIBstand. W pracy przedstawiono dokładne wyniki badań symulacyjnych, oraz skrótowo wyniki badań eksperymentalnych w celu porównania wyników. Dokładne wyniki badań eksperymentalnych przedstawione zostały części pierwszej artykułu (Analiza modalna konstrukcji podpierającej stanowiska badawczego dynamiki małogabarytowych wirników. Część...
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Porównanie cystouretrografii mikcyjnej i sonocystografii mikcyjnej z użyciem ultrasonograficznego środka kontrastującego drugiej generacji w badaniu prospektywnym
PublicationThe invasiveness and exposure to radiation in voiding cystourethrography led to the introduction of alternative methods of diagnosis of vesicoureteral reflux, including contrast enhanced voiding urosonography. While there is a limited number of studies comparing these methods using new generation ultrasound contrast agents, none of them compared both methods simultaneously. This study is aimed at assessing agreement between contrast...
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Zakres stabilnej pracy silnika indukcyjnego z obserwatorem prędkości kątowej wału wyznaczony za pomocą drugioej metody Lapunowa.
PublicationZamieszczono analizę stabilności układu regulacji silnika indukcyjnego z obserwatorem prędkości kątowej wału w oparciu o drugą metodę Lapunowa. Na podstawie modelu matematycznego układu silnika z obserwatorem wyznaczono funkcję Lapunowa oraz udowodniono warunki jej poprawności. Dokonano analizy lokalnej dla małych prędkości oraz częściowej analizy globalnej rozważanego układu. Wyniki potwierdzono w symulacji komputerowej z zastosowaniem...