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Electrochemical Evaluation of Sustainable Corrosion Inhibitors via Dynamic Electrochemical Impedance Spectroscopy
PublicationFinding suitable measurement methods for the effective management of electrochemical problems is of paramount importance, particularly for improving efficiency in corrosion protection. The need for accurate measurement techniques specific to nonstationary conditions has long been recognized, and promising approaches have emerged. This chapter introduces dynamic electrochemical impedance spectroscopy as a novel advancement in electrochemistry...
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Efficient Extraction of Fermentation Inhibitors by Means of Green Hydrophobic Deep Eutectic Solvents
PublicationThe methods for hydrogen yield efficiency improvements, the gaseous stream purification in gaseous biofuels generation, and the biomass pretreatment are considered as the main trends in research devoted to gaseous biofuel production. The environmental aspect related to the liquid stream purification arises. Moreover, the management of post-fermentation broth with the application of various biorefining techniques gains importance....
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Inhibitors of glucosamine-6-phosphate synthase as potential antimicrobials or antidiabetics – synthesis and properties
PublicationGlucosamine-6-phosphate synthase (GlcN-6-P synthase) is known as a promising target for antimicrobial agents and antidiabetics. Several compounds of natural or synthetic origin have been identified as inhibitors of this enzyme. This set comprises highly selective L-glutamine, amino sugar phosphate or transition state intermediate cis-enolamine analogues. Relatively low antimicrobial activity of these inhibitors, poorly penetrating...
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X-ray Photoelectron Spectroscopy of Carboxylic Acids as Corrosion Inhibitors of Aluminium Alloys
PublicationThe datasets, titled X-ray Photoelectron Spectroscopy studies of citric acid adsorption on aluminium alloy 5754 in alkaline media and X-ray Photoelectron Spectroscopy studies of various carboxylic acids adsorption on aluminium alloys in alkaline media, contain XPS studies of the corrosion inhibitory action of selected dicarboxylic acids towards commercially available aluminium alloy 5754 in alkaline media at pH=11. These datasets...
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Geometry optimization of steroid sulfatase inhibitors - the influence on the free binding energy with STS
PublicationIn the paper we review the application of two techniques (molecular mechanics and quantum mechanics) to study the influence of geometry optimization of the steroid sulfatase inhibitors on the values of descriptors coded their chemical structure and their free binding energy with the STS protein. We selected 22 STS-inhibitors and compared their structures optimized with MM+, PM7 and DFT B3LYP/6–31++G* approaches considering separately...
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PEGylated substrates of NSP4 protease: A tool to study protease specificity
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Influence of sub-inhibitory concentration of selected plant essential oils on the physical and biochemical properties of Pseudomonas orientalis
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Inhibitory Effect of Eugenol and trans‐Anethole Alone and in Combination with Antifungal Medicines on Candida albicans Clinical Isolates
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Chocolate desserts with ricotta hydrolysates: In vitro study of inhibitory activity against angiotensin‐converting enzyme and cholinesterase
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Antiplasmodial Activity of Nitroaromatic Compounds: Correlation with Their Reduction Potential and Inhibitory Action on Plasmodium falciparum Glutathione Reductase
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Inhibitory and antimicrobial activities of OGTI and HV-BBI peptides, fragments and analogs derived from amphibian skin
PublicationA series of linear and cyclic fragments and analogs of two peptides (OGTI and HV-BBI) isolated from skin secretions of frogs were synthesized by the solid-phase method. Their inhibitory activity against several serine proteinases: bovine beta-trypsin, bovine alpha-chymotypsin, human leukocyte elastase and cathepsin G from human neutrophils, was investigated together with evaluation of their antimicrobial activities against Gram-negative...
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New potent STS inhibitors based on fluorinated 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamates
PublicationA series of fluorinated analogs based on the frameworks of 4-(1- phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamates have been synthesized as steroid sulfatase (STS) inhibitors. The design of chemical structures of new potential STS inhibitors was supported by molecular docking techniques to identify potential interactions between inhibitors and amino acid residues located in the STS active site. The STS inhibitory potency was evaluated...
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Tissue Factor and Tissue Factor Pathway Inhibitor in Chronically Inflamed Gallbladder Mucosa
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Peptomeric analogues of trypsin inhibitor SFTI-1 isolated from sunflower seeds
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Inhibition of Human and Yeast 20S Proteasome by Analogues of Trypsin Inhibitor SFTI-1
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Eradication of LIG4-deficient glioblastoma cells by the combination of PARP inhibitor and alkylating agent
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Anticandiadal properties of N-acylpeptides containing inhibitor of glucosamine-6-phosphate synthase
PublicationOtrzymano serię N-acylopeptydów zawierających inhibitor syntazy glukozamino-6-fosforanu i zbadano ich aktywność w stosunku do szczepów Candida albicans. Aktywność przeciwgrzybową skorelowano z właściwościami lipofilowymi otrzymanych peptydów. Peptydy zawierające resztę kwasu dekanowego wykazywały najwyższą aktywność przeciwgrzybową.
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Corrosion hazards and inhibitor protection in the seawater injection system on the Baltic sea rig
PublicationOil extraction efficiency in LOTOS Petrobaltic Company is increased by means of injection of seawater into an oilfield aquifer, which is implemented on the Baltic Beta rig, operating on the Baltic Sea. Operational experience has shown a significant degree of corrosion aggressiveness in the injected water, which necessitates frequent repairs of the seawater injection installation. Evaluation of the corrosion phenomena is crucial...
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Galvanostatic impedance measurements for the efficient adsorption isotherm construction in corrosion inhibitor studies
PublicationWe present an approach towards an accurate and time-efficient adsorption isotherm determination to evaluate the corrosion inhibitor interaction in electrolytic environments. The approach is based on dynamic impedance spectroscopy measurements in galvanostatic mode (g-DEIS). The studied corrosion inhibitor is continuously injected between the secondary cell and the corrosion cell. The efficiency corresponding to instantaneous inhibitor...
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Development Of Dynamic Method For Evaluation Of Corrosion Rate On The Example Of Organic Corrosion İnhibitor
PublicationMeasurements of the corrosion rate belong to the most important aspects of materials science. In order to reduce material loss corrosion inhibitors are used. However selection of proper inhibitor should be based on evaluation of its mechanism and effective concentrations. Mechanism of inhibition usually has dynamic character so physicochemical parameters are changing in time. Most of actually used methods...
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Examination of epigenetic inhibitor zebularine in treatment of skin wounds in healthy and diabetic mice
PublicationDNA methyltransferase inhibitor zebularine was proven to induce regeneration in the ear pinna in mice. We utilized a dorsal skin wound model to further evaluate this epigenetic inhibitor in wound healing. Full-thickness excisional wounds were made on the dorsum of 2 and 10-month-old healthy BALB/c and 3 and 8-month-old diabetic (db/db) mice, followed by topical or intraperitoneal zebularine delivery. Depending on the strain, age,...
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Sławomir Milewski prof. dr hab. inż.
PeopleSławomir Milewski, born in 1955 in Puck, Poland, graduated in 1979 in Chemistry from the Faculty of Chemistry, Gdańsk University of Technology (GUT). In 1984 was employed at the Department of Pharmaceutical Technology and Biochemistry. In 1985 he got his PhD, in 1994 became a DSc (habilitation) and in 2002 got the professorship in chemical sciences. Currently he is a full professor and Head of the Department of Pharmaceutical Technology...
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Aktywność przeciwgrzybowa koniugatów inhibitorów enzymatycznych z nośnikami peptydowymi
PublicationCelem badań przedstawionych w rozprawie było określenie aktywności przeciwgrzybowej szeregu związków będących koniugatami peptydów z inhibitorami enzymatycznymi (FMDP, cispentacyna). Zakres badań obejmował zbadanie aktywności peptydów-FMDP, CPP oraz FMDP-CPP wobec grzybów z rodzaju Candida w różnego typu podłożach, określenie możliwości powstawania oporności na FMDP-CPP i peptydy-FMDP, a także określenie szybkości transportu i...
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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...
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Docking simulations, Molecular properties and ADMET studies of novel Chromane6,7diol analogues as potential inhibitors of Mushroom tyrosinase
PublicationResearch on inhibition of tyrosinase enzyme has attained significant value, because tyrosinase inhibitors have potential applications in medicine, cosmetics (as whitening agents) and in agriculture (as bioinsecticides). Determination and elucidation of new tyrosinase inhibitors are not only beneficial for medical purposes, but their promising applications in improving food quality and nutritional...
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Generation of inhibitory compounds during pre-treatment of lignocellulosic biomass
Open Research DataDataset contains calibration curves and typical resultsa obtained during biomass pre-treatment. Data are converted from digital raw files to xlsx files
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Synthesis of analogues of anthraquinones linked to tuftsin or retro-tuftsin residues as potential topoisomerase inhibitors
PublicationZsyntetyzowano 10 nowych analogów antrachinonów z pochodnymi tuftsyny i retro-tuftsyny jako potencjalne inhibitory topoizomerazy. Substratem wyjściowym były zsyntetyzowane 1,4-, 1,5- i 1,8-bis(tosyloksy)-9,10-antrachinony oraz odpowiednio chronione pochodne tuftsyny i retro-tuftsyny, które otrzymano metodą mieszanych bezwodników z zastosowaniem chloromrówczanu izobutylu i NMM. Reakcje prowadzone były w acetonitrylu pod azotem w...
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A Review of Progress in Histone Deacetylase 6 inhibitors Research: Structural Specificity and Functional Diversity.
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Designing of Substrates and Inhibitors of Bovine α-Chymotrypsin with Synthetic Phenylalanine Analogues in Position P1
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Synthesis of New Hydrazone Derivatives and Evaluation of their Efficacy as Proliferation Inhibitors in Human Cancer Cells
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Application of quartz crystal microbalance and dynamic impedance spectroscopy to the study of copper corrosion inhibitors
PublicationThe study investigates the application of Dynamic Electrochemical Impedance Spectroscopy (DEIS) and Electrochemical Quartz Crystal Microbalance (EQCM) techniques to examine the corrosion inhibition of copper by Benzotriazole and Sodium Folate in a 0.1 M NaCl solution. DEIS, an advanced version of Electrochemical Impedance Spectroscopy (EIS), allows for real-time monitoring of non-stationary electrochemical systems,...
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The Protein Folding Problem
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Adrenal Secretory Protease
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PROTEIN AND PEPTIDE LETTERS
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Dipeptidyl Peptidase IV Inhibitory Peptides Generated in Dry-Cured Pork Loin during Aging and Gastrointestinal Digestion
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Antioxidant potential, mineral composition and inhibitory effects of conifer needle extract on hyaluronidase - prospects of application in functional food
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Synthesis and steroid sulfatase inhibitory activities of N-phosphorylated 3-(4-aminophenyl)-coumarin-7-O-sulfamates
PublicationIn the present work, we report convenient methods for the synthesis and biological evaluation of N-phosphorylated derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as potential steroid sulfatase (STS) inhibitors. Their binding modes were modeled using docking techniques. The inhibitory effects of the synthesized compounds were tested on STS isolated from human placenta. All of the newly synthesised coumarin derivatives were...
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Problematyka implantacji protez piersiowych - przegląd literatury
PublicationOperacje związane z wykorzystaniem implantów piersi są jednymi z najczęściej przeprowadzanych zabiegów chirurgii plastycznej, dlatego istotne jest, aby zminimalizować ryzyko powikłań. Do najczęściej występujących zalicza się: obrzęk, wysięk, krwiaki, problemy z gojeniem ran oraz infekcje. Zakłada się, że infekcja jest głównym czynnikiem prowadzącym do degradacji implantu. Agresywne środowisko gospodarza, ciągłe zmiany pH i temperatury...
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Novel Potential Binding Sites for Selective Inhibitor Design of Human Soluble Epoxide Hydrolase
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Triazoloacridone C-1305 impairs XBP1 splicing by acting as a potential IRE1α endoribonuclease inhibitor
PublicationInositol requiring enzyme 1 alpha (IRE1α) is one of three signaling sensors in the unfolding protein response (UPR) that alleviates endoplasmic reticulum (ER) stress in cells and functions to promote cell survival. During conditions of irrevocable stress, proapoptotic gene expression is induced to promote cell death. One of the three signaling stressors, IRE1α is an serine/threonine-protein kinase/endoribonuclease (RNase) that...
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Implication of the disulfide bridge in trypsin inhibitor SFTI-1 in its interaction with serine proteinases
PublicationFourteen monocyclic analogues of trypsin inhibitor SFTI-1 isolated from sunflower seeds were synthesized by the solid-phase method. The purpose of this work was to establish the role of a disulfide bridge present in inhibitor's side chains of Cys3 and Cys11 in association with serine proteinases. This cyclic fragment was replaced by the disulfide bridges formed by L-pencillamine (Pen), homo-L-cysteine (Hcy), N-sulfanylethylglycine...
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A. Computational analysis by molecular docking of thirty alkaloid compounds from medicinal plants as potent inhibitors of SARS-CoV-2 main protease(2020). Focused on analysis of the Medicinal plants that have potential therapeutic ability against COVID-19.
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CURRENT PROTEIN & PEPTIDE SCIENCE
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Current Protocols in Protein Science
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Influence of Osmolytes on Protein and Water Structure: A Step To Understanding the Mechanism of Protein Stabilization
PublicationResults concerning the thermostability of hen egg white lysozyme in aqueous solutions with stabilizing osmolytes, trimethylamine-N-oxide (TMAO), glycine (Gly), and its N-methyl derivatives, N-methylglycine (NMG), N,N-dimethylglycine (DMG), and N,N,N-trimethylglycine (betaine, TMG), have been presented. The combination of spectroscopic (IR) and calorimetric (DSC) data allowed us to establish a link between osmolytes’ influence on...
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Amino Acid and Peptide‐Based Antiviral Agents
PublicationA significant number of antiviral agents used in clinical practice are amino acids, short peptides, or peptidomimetics. Among them, several HIV protease inhibitors (e. g. lopinavir, atazanavir), HCV protease inhibitors (e. g. grazoprevir, glecaprevir), and HCV NS5A protein inhibitors have contributed to a significant decrease in mortality from AIDS and hepatitis. However, there is an ongoing need for the discovery of new antiviral...
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Fluorescent analogs of trypsin inhibitor SFTI-1 isolated from sunflower seeds-synthesis and applications
PublicationThis article describes the synthesis and enzymatic study of newly synthesized analogs of trypsin inhibitors SFTI-1 that were fluorescent labeled on their N-terminal amino groups. Two fluorescent derivatives of benzoxazole (3-[2-(4-diphenylaminophenyl) benzoxazol-5-yl]-L-alanine[(4NPh(2)) Ph] Box-Ala and 3-[2-(2', 4', 5'-trimethoxyphenyl) benzoxazol-5-yl]-l-alanine-[2,4,5-(OMe)3Ph] Box-Ala) were used as efficient fluorescent labels....
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Synthesis of Cyano-Benzylidene Xanthene Synthons Using a Diprotic Brønsted Acid Catalyst, and Their Application as Efficient Inhibitors of Aluminum Corrosion in Alkaline Solutions
PublicationNovel cyano-benzylidene xanthene derivatives were synthesized using one-pot and condensation reactions. A diprotic Brønsted acid (i.e., oxalic acid) was used as an effective catalyst for the promotion of the synthesis process of the new starting xanthene–aldehyde compound. Different xanthene concentrations (ca. 0.1–2.0 mM) were applied as corrosion inhibitors to control the alkaline uniform corrosion of aluminum. Measurements were...
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Identification of sustainable trypsin active‐site inhibitors from Nigrospora sphaerica strain AVA‐1
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Molecular modeling and evaluation of novel dibenzopyrrole derivatives as telomerase inhibitors and potential drug for cancer therapy
PublicationDuring previous years, many studies on synthesis, as well as on anti-tumor, anti-inflammatory and anti-bacterial activities of the pyrazole derivatives have been described. Certain pyrazole derivatives exhibit important pharmacological activities and have proved to be useful template in drug research. Considering importance of pyrazole template, in current work the series of novel inhibitors were designed by replacing central...