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Search results for: chiral pharmaceuticals
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Structural Characterization and in Vivo Evaluation of β-Hairpin Peptidomimetics as Specific CXCR4 Imaging Agents
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Reversed-Phase TLC and HPLC Retention Data in Correlation Studies with in Silico Molecular Descriptors and Druglikeness Properties of Newly Synthesized Anticonvulsant Succinimide Derivatives
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99mTc-Galacto-RGD2: A Novel 99mTc-Labeled Cyclic RGD Peptide Dimer Useful for Tumor Imaging
PublicationThis study sought to evaluate [99mTc(HYNIC-Galacto-RGD2)-(tricine)(TPPTS)] (99mTc-Galacto-RGD2: HYNIC = 6-hydrazinonicotinyl; Galacto-RGD2 = Glu[cyclo[Arg-Gly-Asp-D-Phe-Lys(SAA-PEG2-(1,2,3-triazole)-1-yl-4-ethylamide)]]2 (SAA = 7-amino-L-glycero-L-galacto-2,6-anhydro-7-eoxyheptanamide, and PEG2 = 3,6-dioxaoctanoic acid); and TPPTS = trisodium triphenylphosphine-3,3',3''-trisulfonate) as a new radiotracer for tumor imaging. Galacto-RGD2...
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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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Encapsulation of Amikacin into Microparticles Based on Low-Molecular-Weight Poly(lactic acid) and Poly(lactic acid-co-polyethylene glycol)
PublicationThe aim of this study was to fabricate novel microparticles (MPs) for efficient and long-term delivery of amikacin (AMI). The emulsification method proposed for encapsulating AMI employed low-molecular-weight poly(lactic acid) (PLA) and poly(lactic acid-co-polyethylene glycol) (PLA−PEG), both supplemented with poly(vinyl alcohol) (PVA). The diameters of the particles obtained were determined as less than 30 μm. Based on an in-vitro...
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Microemulsion Delivery Systems with Low Surfactant Concentrations: Optimization of Structure and Properties by Glycol Cosurfactants
PublicationExtensive use of microemulsions as delivery systems raises interest in the safe ingredients that can form such systems. Here, we assessed the use of two glycols, i.e., propylene glycol and pentylene glycol, and their mixtures to manipulate the properties and structure of microemulsions. Obtained systems with glycols were extensively characterized in terms of capacity to incorporate water phase, droplet size, polydispersity, structure...
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Ryszard Katulski prof. dr hab. inż.
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Physical and Mechanical Evaluation of Silicone-Based Double-Layer Adhesive Patch Intended for Keloids and Scar Treatment Therapy
PublicationGrowing interest in silicone elastomers for pharmaceutical purposes is due to both theirbeneficial material effect for scar treatment and their potential as drug carriers. Regarding their morphological structure, silicone polymers possess unique properties, which enable a wide range of applicability possibilities. The present study focused on developing a double-layer adhesive silicone film (DLASil) by evaluating its physical...
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Application of vibrational spectroscopy, thermal analyses and X-Ray diffraction in the rapid evaluation of the stability in solid-state of ranitidine, famotidine and cimetidine
PublicationThis paper reports the study on applicability of Fourier transform infrared (FTIR), near-infrared (NIR) and Raman spectroscopy, differential scanning calorimetry (DSC) and X-ray diffraction (XRD) for the estimation of the chemical stability and photostability of histamine H2-receptor antagonist substances. Ranitidine hydrochloride (RAN), famotidine (FAM) and cimetidine (CIM) were tested and differences in sensitivity were measured...
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Phytoremediation—From Environment Cleaning to Energy Generation—Current Status and Future Perspectives
Publication:Phytoremediationis a technology based on the use of green plants to remove, relocate, deactivate, or destroy harmful environmental pollutants such as heavy metals, radionuclides, hydrocarbons, and pharmaceuticals. Under the general term of phytoremediation, several processes with distinctively different mechanisms of action are hidden. In this paper, the most popular modes of phytoremediation are described and discussed. A broad...
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Una egemonia instabile
Publicationil ruolo degli Stati Uniti nell'economia globale e la sfida giapponese e cinese
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The New Chinese Civil Code and its contribution to Sustainable Development
PublicationThe first civil code of the People’s Republic of China in the history was adopted by the 13th National People’s Congress in Beijing on 28 May 2020 and will enter into effect on 1 January 2021. The new civil code puts much more emphasis on the sustainable development and protection of the environment and because of that, the Chinese private law has begun to respond to ecological problems as well. The...
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Dianzi Keji Daxue Xuebao/Journal of the University of Electronic Science and Technology of China
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Huadong Ligong Daxue Xuebao /Journal of East China University of Science and Technology
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Influence of Honing Parameters on the Quality of the Machined Parts and Innovations in Honing Processes
PublicationThe article presents a literature review dealing with the effect of the honing parameters on the quality of the machined parts, as well as with the recent innovations in honing processes. First, an overview about the honing and the plateau-honing processes is presented, considering the main parameters that can be varied during machining. Then, the influence of the honing parameters on surface finish, shape deviation and material...
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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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Quality of limes juices based on the aroma and antioxidant properties
PublicationKaffir (Citrus hystrix) and Key (Citrus aurantifolia) limes juices were investigated and compared. Two dimensional gas chromatography coupled with time-of-flight mass spectrometry (GC×GC-TOF-MS) was applied to assess the botanical origin of Kaffir and Key limes juices, based on volatile substances. The biggest differences in the contents of selected terpenes in Kaffir and Key limes occur in chemical compounds such as Limonene,...
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Experimental and theoretical studies on the Sulfamethazine-Urea and Sulfamethizole-Urea solid-liquid equilibria
PublicationThe miscibility of active pharmaceutical ingredients with excipients is an important aspect in pharmaceutical technology protocols. In this study, the differential scanning calorimetry (DSC) was used for Sulfamethazine-Urea (SI–U) and Sulfamethizole-Urea (SO–U) solid-liquid phase diagrams determination. Both sulfonamides form simple binary eutectics with Urea. The lack of new co-crystal phase formation was confirmed by inspection...
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Effect of Silicone on the Collagen Fibrillogenesis and Stability
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Effect of Glycemic Disorders and Habits on the Concentration of Selected Neurotrophic Factors in Patients with Lumbosacral Intervertebral Disc Degeneration
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QSRR Evaluation of the New Anticancer Sulfonamides in View of the cis-trans Isomerism
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Biological Activity of Compounds Exhibiting Local Anesthetics's Properties Evaluated by QSAR Approach
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Comprehensive Spectroscopic Characterization of Finasteride Polymorphic Forms. Does the Form X Exist?
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Directly compressible formulation of immediate release rosuvastatin calcium tablets stabilized with tribasic calcium phosphate
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Substrate Reduction Therapies for Mucopolysaccharidoses
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Modulation of cellular response to anticancer treatment by caffeine:inhibition of cell cycle checkpoints, DNA repair and more
PublicationKofeina i inne metyloksantyny wywołują bardzo różne efekty fizjologiczne w organizmie człowieka. W pracy przedstawiamy, które z tych efektów mogą wpływać na skuteczność terapii przeciwnowotworowych. Kofeina może bezpośrednio wpływać na transport oraz aktywację metaboliczną cząsteczek leków do komórki, poprzez tworzenie kompleksów z lekami zawierającymi układy poliaromatyczne. Kofeina hamuje aktywność kinaz ATM/ATR co prowadzi do...
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Function and Frustration of Multi-Drug ABC Exporter Protein and Design of Model Proteins for Drug Delivery Using Protein Hydration Thermodynamics
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Synthesis of isomeric, oxathiolone fuded chalcones and comparison of their activity toward various microorganisms and human cancer cell lines
PublicationIzomeryczne oksationolowe sprzężone chalkony otrzymano w wyniku kondensacji odpowiedniego acetylobenzo[1,3]oksatiolo-2-onu z aldehydem benzoesowym w środowisku kwaśnym. Określono aktywność cytotoksyczną otrzymanych związków wobec komórek linii HeLa, przeciwbakteryjną wobec Micrococcus luteus, Staphylococcus aureus, Salmonella typhimurium, Escherichia coli i Proteus vulgaris, przeciwgrzybową wobec Candida albicans i tuberkulostatyczną...
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Future of Protease Activity Assays
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Editorial(Hot Topic: Proteolysis in Health and Disease)
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pH-Induced modification to stratum corneum lipids investigated using thermal, spectroscopic, and chromatographic techniques
PublicationZbadano jakim zmianom jakościowym i ilościowym ulegają indywidualne klasy lipidów w Stratum Corneum (tkanka rogowa skóry) pod wpływem środowiska o zmiennym pH.
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Prediction of Bioactive Peptides From Chicken Feather and Pig Hair Keratins Using In Silico Analysis Based on Fragmentomic Approach
PublicationBackground: Keratin is among the most abundant structural proteins of animal origin, however it remains broadly underutilized. Objective: Bioinformatic investigation was performed to evaluate selected keratins originating from mass-produced waste products, i.e., chicken feathers and pig hair, as potential sources of bioactive peptides. Methods: Pepsin, trypsin, chymotrypsin, papain, and subtilisin were used for in silico keratinolysis...
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Transcriptomic Effects of Estrogen Starvation and Induction in the MCF7 Cells. The Meta-analysis of Microarray Results
PublicationEstrogen is one of the most important signaling molecules which targets a number of genes. Estrogen levels regulate cell proliferation and a plethora of metabolic processes, which may interfere with a range of medical conditions and drug metabolism. The MCF7 breast cancer cell line, expressing the estrogen receptor α, is a well-studied model of cellular answer to estrogen. The aim of this study was to characterize transcriptomic...
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Prophylaxis of Non-communicable Diseases: Why Fruits and Vegetables may be Better Chemopreventive Agents than Dietary Supplements Based on Isolated Phytochemicals?
PublicationThe World Health Organization (WHO) report from 2014 documented that non-communicable socalled civilization diseases such as cardiovascular disease, chronic respiratory diseases, cancer or type 2 diabetes are responsible for over 50% of all premature deaths in the world. Research carried out over the past 20 years has provided data suggesting that diet is an essential factor influencing the risk of development of these diseases....
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Chemical Aspects of Biological Activity of Isothiocyanates and Indoles, the Products of Glucosinolate Decomposition
PublicationThere is growing evidence that cancer chemoprevention employing natural, bioactive compounds may halt or at least slow down the different stages of carcinogenesis. A particularly advantageous effect is attributed to derivatives of sulfur-organic phytochemicals, such as glucosinolates (GLs) synthesized mainly in Brassicaceae plant family. GLs are hydrolysed enzymatically to bioactive isothiocyanates (ITC) and indoles, which exhibit strong...
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Electrochemical and in silico approaches for liver metabolic oxidation of antitumor-active triazoloacridinone C -1305
Publication5-Dimethylaminopropylamino-8-hydroxytriazoloacridinone (C-1305) is a promising antitumor compound developed in our laboratory. A better understanding of its metabolic transformations is still needed to explain the multidirectional mechanism of pharmacological action of triazoloacridinone derivatives at all. Thus, the aim of the current work was to predict oxidative pathways of C-1305 that would reflect its phase I metabolism. The...
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The Role of FLT3 Kinase as an AML Therapy Target
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Novel insights into conjugation of antitumor-active unsymmetrical bisacridine C-2028 with glutathione: characteristics of non-enzymatic and glutathione S-transferase-mediated reactions
PublicationUnsymmetrical bisacridines (UAs) are a novel potent class of antitumor-active therapeutics. A significant route of phase II drug metabolism is conjugation with glutathione (GSH), which can be non-enzymatic and/or catalyzed by GSH-dependent enzymes. The aim of this work was to investigate the GSH-mediated metabolic pathway of a representative UA, C 2028. GSH supplemented incubations of C-2028 with rat, but not with human, liver...
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Methods for Elucidation of DNA-Anticancer Drug Interactions and Their Applications in the Development of New Drugs
PublicationDNA damaging agents including anthracyclines, camptothecins and platinum drugs are among most frequently used drugs in the chemotherapeutic routine. Due to their relatively low selectivity for cancer cells, administration is associated with adverse side effects, whereas the inherent genotoxicity of these drugs is associated with risk of developing secondary cancers. Development of new drugs, which could be spared of these drawbacks...
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Krajobrazy - walory, zagrożenia i kształtowanie. W: [Praca zbiorowa] Mate-riały do monografii przyrodniczej regionu gdańskiego. Gdańsk: Marpress** 2003 s. 167-181 bibliogr. 9 poz. Tom 9 Zaborski Park Krajobrazowy. Problemy trójochrony i współistnienia z Parkiem Narodowym ''Bory Tucholskie''. Zaborski Landscape Park. Problems of Landscape Park. Problems of the triprotection and coexistence with the ''Bo- ry Tucholskie'' National Park. Praca zbiorowa pod redakcją M. Przewoźniaka.
PublicationOmówienie cech krajobrazu Zaborskiego Parku Krajobrazowego pod kątem charat-terystyki kompozycyjnej i wizualnej. Przedstawienie głównych cech i składo-wych krajobrazu ZPK: wnętrz krajobrazowych lądowych, wodnych jezior, wnętrz dolin rzek i strumieni, otwarć widokowych i panoramicznych. Przedstawienie dzisiejszego stanu zagospodarowania kulturowego oraz zagrożeń walorów kompo-zycyjnych i estetycznych krajobrazu ZPK.
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Auksetyczne pianki poliuretanowe
PublicationPrzedmiotem badań były auksetyczne pianki poliuretanowe wytworzone metodą trójosiowej termo-kompresji z konwencjonalnych elastycznych pianek poliuretanowych. Materiały auksetyczne charak-teryzują się ujemnym współczynnikiem Poissona i dzięki swojej strukturze komórkowej charakteryzują się unikalnymi właściwościami fizyko-mechanicznymi. Zbadano wpływ trójosiowej termokompresji na zmianę właściwości mechanicznych oraz struktury otrzymanej...
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NADZOROWANIE WYPOSAŻENIA DO MONITOROWANIA I POMIARÓW WEDŁUG WYMAGAŃ WYBRANYCH NORM ORAZ PRZEPISÓW PRAWNYCH
Publication: Przyrządy pomiarowe stanowią zasadniczy element złożonego systemu oceny jakości wyrobów na wszystkich etapach produkcji. Odpowiednio zaprojektowane procedury opisujące procesy kontrolne i pomiarowe, sprawnie zorganizowane i przeprowadzane operacje monitorowania i pomiarów parametrów procesów i produktów oraz skutecznie funkcjonujący nadzór nad wyposażeniem do monitorowania i pomiarów w organizacji są podstawą do wykazania, że...
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Efficient three-dimensional fluorescence measurements for characterization of binding properties in some plants
PublicationThe main aim of this research was to characterize some plants and to determine their similarities and differences, using spectroscopic methods. The interactions of soluble polyphenols of different plants with human serum albumin (HSA) were investigated by 3D-fluorescence. The obtained fluorescence results allow to classify the investigated plants according to their binding properties. The HSA-binding capacities of these plants...
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New Analogues of Mycophenolic Acid
PublicationMycophenolic acid (MPA) possesses antibacterial, antifungal, antiviral, immunosuppressive and anticancer properties. It is a non-competitive and reversible inhibitor of dehydrogenase inosine-5'-monophosphate (IMPDH). This compound belongs to the immunosuppressive drugs used for the prevention of both acute and chronic transplant rejection. Until now, two derivatives of MPA have been used clinically: mycophenolate mofetil (MMF,...
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Greenness assessment of analytical methods used for antibiotic residues determination in food samples
PublicationFood of animal origin plays an important role in ensuring a healthy and sustainable human diet. However, residues of pharmaceuticals, especially antibiotics, can be the cause of many health problems. To protect consumers and improve food quality, analytical methods used to determine contaminants should be simple, selective, and have high throughput and low detection limits. Recently, greenness metric tools have proven useful in...
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Solubility of dapsone in deep eutectic solvents: Experimental analysis, molecular insights and machine learning predictions
PublicationBackground. Dapsone (DAP) is an anti-inflammatory and antimicrobial active pharmaceutical ingredient used to treat, e.g., AIDS-related diseases. However, low solubility is a feature hampering its efficient use. Objectives. First, deep eutectic solvents...
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Stability and phase transition investigation of olanzapine polymorphs
PublicationWe use electrical embedded-fragment QM method with both DFT/ωB97XD/6-31G* and MP2/6-31G* to investigate the phase transformations of olanzapine. Gibbs free energy calculations predict that form I is always the most stable structure and form II is the least stable one, while form IV is more stable than form III below about 200 K but less stable above this temperature, implying a polymorphic phase transformation. This may account...
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Metody badania struktury triacylogliceroli.
PublicationOmówiono strukturę triacylogliceroli oraz liczbę możliwych kombinacji różnych triacylogliceroli w zależności od ilości występujących w nich kwasów tłuszczowych. Przedstawiono różne metody określania rozmieszczenia kwasów tłuszczowych w poszczególnych pozycjach cząsteczek triacylogliceroli. Pokazano metody enzymatyczne z zastosowaniem lipaz regio - i stereospecyficznych oraz metody wykorzystujące wysokosprawną chromatografię cieczową...
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Huanan Ligong Daxue Xuebao/Journal of South China University of Technology (Natural Science)
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Meconium analysis as a promising diagnostic tool for monitoring fetal exposure to toxic substances: Recent trends and perspectives
PublicationPrenatal exposure to toxic substances is an important public health problem. Many biological specimens obtained from the fetus or mother are used for biomonitoring. Each material reflects exposure in a specific time period and has different advantages and disadvantages in terms of accuracy, time window of detection and cost/benefit ratio. Recently, meconium has become the matrix of choice in toxicology screening for detecting exposure...