Filters
total: 774
Search results for: drug
-
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...
-
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...
-
Rheological Characteristics of Novel Meloxicam-Loaded Complex Organogels Based on Fumed Silica and Poloxamer
Publication -
Current status of liposomal porphyrinoid photosensitizers
Publication -
Vitamin D Metabolism Gene Polymorphisms and Their Associated Disorders: A Literature Review
Publication -
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,...
-
Prolonged Quercetin Administration Diminishes the Etoposide-Induced DNA Damage in Bone Marrow Cells of Rats
Publication -
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...
-
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...
-
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...
-
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
Publication -
Bacteriophage–Ciprofloxacin Combination Effectiveness Depends on Staphylococcus aureus–Candida albicans Dual-Species Communities’ Growth Model
Publication -
Biofilm Formation and Prevalence of Biofilm-Related Genes Among Clinical Strains of Multidrug-Resistant Staphylococcus aureus
Publication -
Environmental Phage-Based Cocktail and Antibiotic Combination Effects onAcinetobacter baumanniiBiofilm in a Human Urine Model
Publication -
The Effect of Subinhibitory Concentrations of trans-Anethole on Antibacterial and Antibiofilm Activity of Mupirocin Against Mupirocin-Resistant Staphylococcus aureus Strains
Publication -
<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>
Publication -
Potential of Liquid Biopsy in Papillary Thyroid Carcinoma in Context of miRNA, BRAF and p53 Mutation
Publication -
Genetic Determinants of Vitamin D-Related Disorders; Focus on Vitamin D Receptor
Publication -
Morphine and methadone pre-exposures differently modify brain regional Fos protein expression and locomotor activity responses to morphine challenge in the rat
Publication -
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...
-
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...
-
Population analysis to assess the influence of age and body weight on pharmacokinetics and pharmacodynamics of dexmedetomidine in New Zealand White rabbits
Publication -
Acute and subacute (28-Day) toxicity studies of ionic liquid, didecyldimethyl ammonium acesulfamate, in rats
Publication -
The pharmacokinetics of propofol in ICU patients undergoing long-term sedation
Publication -
The quantification of reticulocyte maturation and neocytolysis in normal and erythropoietin stimulated rats
Publication -
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...
-
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...
-
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.
-
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...
-
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,...
-
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...
-
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...
-
Investigating the disease- modifying properties of sclerotiorin in Alzheimer's therapy using acetylcholinesterase inhibition
PublicationAlzheimer's disease (AD) is a progressive neurodegenerative disorder caused due to the damage and loss of neurons in specific brain regions. It is the most common form of dementia observed in older people. The symptoms start with memory loss and gradually cause the inability to speak and do day-to-day activities. The cost of caring for those affected individuals is huge and is probably beyond most developing countries capability....
-
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...
-
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...
-
Structure–activity relationships study on biological activity of peptides as dipeptidyl peptidase IV inhibitors by chemometric modeling
Publication -
Design and characteristics of gellan gum beads for modified release of meloxicam
Publication -
Aryl- and heteroaryl-substituted phenylalanines as AMPA receptor ligands
Publication -
Short Term Monitor of Photodegradation Processes in Ranitidine Hydrochloride Observed by FTIR and ATR FTIR
PublicationThe effects of degradation of ranitidine hydrochloride exposed to UVB radiation (l = 310 nm) and oxygen in a weathering chamber were studied by Fourier Transform Infrared spectroscopy (FTIR) and Attenuated Total Reflectance Fourier Transform Infrared spectroscopy (ATR-FTIR). ATR-FTIR profile indicated that the degradation was spatially heterogeneous. Significant amounts of photoproducts were detected only in a directly...
-
CDK9: Therapeutic Perspective in HCC Therapy
Publication -
Solubility advantage of sulfanilamide and sulfacetamide in natural deep eutectic systems: experimental and theoretical investigations
PublicationObjective: The aim of this study was to explore the possibility of using natural deep eutectic solvents (NADES) as solvation media for enhancement of solubility of sulfonamides, as well as gaining some thermodynamic characteristics of the analyzed systems. Significance: Low solubility of many active pharmaceutical ingredients is a well-recognized difficulty in pharmaceutical industry, hence the need for different strategies addressing...
-
Effects of an immunosuppressive treatment on the rat prostate
Publication -
Current Challenges in Targeting Tumor Desmoplasia to Improve the Efficacy of Immunotherapy
Publication -
Investigating the disease‐modifying properties of sclerotiorin in Alzheimer's therapy using acetylcholinesterase inhibition
Publication -
Current state of a dual behaviour of antimicrobial peptides-Therapeutic agents and promising delivery vectors
Publication -
Preliminary antifungal activity assay of selected chlorine-containing derivatives of xanthone and phenoxyethyl amines
Publication -
Simplified, serine‐rich theta‐defensin analogues as antitumour peptides
Publication -
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...
-
Structural Factors Affecting Cytotoxic Activity of (E)-1-(Benzo[d ][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one Derivatives
PublicationDerivatives of (E)-1-(5-alkoxybenzo[d][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one (1) demonstrated exceptionally high in vitro cytotoxic activity, with IC50 values of the most active derivatives in the nanomolar range. To identify structural fragments necessary for the activity, several analogs deprived of selected fragments were prepared, and their cytotoxic activity was tested. It was found that the activity depends on combined effects...
-
Synthesis and biological evaluation of fluorinated 3-phenylcoumarin-7-O-sulfamate derivatives as steroid sulfatase inhibitors
PublicationIn the present work, we report the initial results of our study on a series of 3-phenylcoumarin sulfamate-based compounds containing C-F bonds as a novel inhibitors of steroid sulfatase (STS). The new compounds are potent STS inhibitors, possessing more than 10 times higher inhibitory potency than coumarin-7-O-sulfamate. In the course of our investigation, compounds 2b and 2c demonstrated the highest inhibitory effect in the enzymatic...