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Search results for: DRUG ABUSE
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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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<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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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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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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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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Prolonged Quercetin Administration Diminishes the Etoposide-Induced DNA Damage in Bone Marrow Cells of Rats
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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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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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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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Complexation of Bioelements and Toxic Metals by Polyphenolic Compounds - Implications for Health
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Antioxidants as a Potential Preventive and Therapeutic Strategy for Cadmium
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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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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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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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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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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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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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Fuzzy Control 2023
e-Learning CoursesKurs do przedmiotu "Fuzzy Control" na sem letni 2023, drugi stopień
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Fuzzy Control 2022
e-Learning CoursesKurs do przedmiotu "Fuzzy Control" na sem letni 2022, drugi stopień
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Sterowanie Rozmyte 2023
e-Learning CoursesKurs do przedmiotu "Sterowanie rozmyte" na sem letni 2023, drugi stopień
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Sterowanie Rozmyte 2022
e-Learning CoursesKurs do przedmiotu "Sterowanie rozmyte" na sem letni 2022, drugi stopień
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Fuzzy Control 2024
e-Learning CoursesKurs do przedmiotu "Fuzzy Control" na sem letni 2024, drugi stopień
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Sterowanie Rozmyte 2024
e-Learning CoursesKurs do przedmiotu "Sterowanie rozmyte" na sem letni 2024, drugi stopień
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Nowe zasady projektowania infrastruktury tramwajowej
PublicationWprowadzone we wrześniu 2022 roku zmiany w zasadach projektowania dróg, zwieńczone nowym Rozporządzeniem Ministra Infrastruktury w sprawie przepisów techniczno-budowlanych dotyczących dróg publicznych spowodowały pojawienie się daleko idących konsekwencji w przypadku projektowania tras tramwajowych.
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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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Ekonomiczne i środowiskowe aspekty budowy dróg
e-Learning CoursesMateriały do kursu Ekonomiczne i środowiskowe aspekty budowy dróg na kierunku budownictwo.
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Detailed results of shaping personnel risk factors in enterprise A
Open Research DataThe data presents the shape of all the researched personnel risk factors in the A enterprise (which was tested by the author). Further considerations should be started with the presentation of the synthesis of the obtained results, which is presented in this research data.
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Results of modeling of pharmaceuticals mixtures toxicity with deviation ratio and best-fit functions models using Saccharomyces cerevisiae yeast as model organism
Open Research DataThe research was concerned with verifying the impact of binary mixtures of nine pharmaceuticals against a selected organism, i.e., the yeast Saccharomyces cerevisiae. S cerevisiae is used as a model organism in the monitoring of endocrine disruptors in environmental and reference samples in Xenometrix® systems - XenoScreen®. Tested pharmaceuticals,...
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Węzły grupy C
PublicationDrogi ogólnodostępne, zazwyczaj dwupasmowe dwukierunkowe, stanowią w Polsce ponad 95% łącznej długości dróg publicznych i ogromna większość punktów przecięć tych dróg to skrzyżowania zwykłe lub skanalizowane. Jednakże niektóre z nich są projektowane jako węzły. Najprostszym i najtańszym rozwiązaniem jest wybudowanie węzła grupy C. Są to takie węzły których główne potoki krzyżują się między sobą bezkolizyjnie, a na każdej z krzyżujących...
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Adam Bolt dr hab. inż.
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Historia filozofii z elementami historii matematyki
e-Learning CoursesHistoria filozofii z elementami historii matematyki. Drugi semestr Matematyki, pierwszego stopnia
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Projekt Zespołowy I 2024
e-Learning CoursesProjekt zespołowy I dla studentów fizyki, drugi stopień, sem I
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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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Krechowicz - nowe obrazy, Nadbałtyckie Centrum Kultury, Galeria NCK, Ratusz Staromiejski, 2-29 lipca 2011r.
PublicationDruk do wystawy malarstwa, która miała miejsce w lipcu 2011 roku w Nadbałtyckim Centrum Kultury w Gdańsku. Druk zawiera tekst krytyczny autorstwa Dominiki Krechowicz i notę biograficzną w języku polskim oraz jedną kolorową reprodukcję pracy. Wydawcą jest Nadbałtyckie Centrum Kultury w Gdańsku.