Search results for: DRUGS METABOLIZING ENZYMES
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Theoretical Encapsulation of Fluorouracil (5-FU) Anti-Cancer Chemotherapy Drug into Carbon Nanotubes (CNT) and Boron Nitride Nanotubes (BNNT)
PublicationIntroduction: Chemotherapy with anti-cancer drugs is considered the most common approach for killing cancer cells in the human body. However, some barriers such as toxicity and side effects would limit its usage. In this regard, nano-based drug delivery systems have emerged as cost-effective and efficient for sustained and targeted drug delivery. Nanotubes such as carbon nanotubes (CNT) and boron nitride nanotubes (BNNT) are promising...
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Occurrence and seasonal variations of 25 pharmaceutical residues in wastewater and drinking water treatment plants
PublicationThousands of tons of pharmaceuticals are introduced into the aqueous environment due to their incomplete elimination during treatment process in wastewater treatment plants (WWTPs) and water treat- ment plants (WTPs). The presence of pharmacologically active compounds in the environment is of a great interest because of their potential to cause negative effects. Furthermore, drugs can undergo different pro- cesses leading to the...
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Modulation of CYP1A1, CYP1A2 and CYP1B1 expression by cabbage juices and indoles in human breast cell lines
PublicationEpidemiological studies have shown that consumption of cab- bage and sauerkraut is connected with significant reduction of breast cancer incidences. Estrogens are considered a major breast cancer risk factor and their metabolism by P450 enzymes substan- tially contributes to carcinogenic activity. The aim of this study was to investigate the effect of cabbage and sauerkraut juices of differ- ent origin on the expression profile...
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Near-Infrared III Nanophosphorswith Cr3+Ni2+ Energy Transfer for Bioimaging
Open Research DataIn the biomedical field, the use of fluorescence imaging in the second near-infrared (NIR-II) region is growing rapidly because it imparts the advantages of reduced autofluorescence and low photon scattering. The advantage of reduced scattering is that it increases penetration depth in vivo and improves imaging clarity. Herein, this work uses mesoporous...
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Bisphenols (A, S, and F) affect the basic hormonal activity determined for pharmaceuticals – Study of Saccharomyces cerevisiae
PublicationPharmaceuticals and analogs of bisphenol A (BPA) are increasingly threatening environmental pollutants. In this study, mixtures of selected pharmaceuticals (diclofenac sodium salt, chloramphenicol, oxytetracycline hydrochloride, fluoxetine hydrochloride, estrone, ketoprofen, progesterone, gemfibrozil and androstenedione) were prepared with BPA and its two analogs (namely, bisphenols F and S) at such ratios to reflect environmentally...
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Nowe substancje psychoaktywne. Cz. I. Współczesna sytuacja narkotykowa
PublicationGwałtowny wzrost liczby substancji wprowadzanych na rynek narkotykowy został zaobserwowany już pod koniec lat dziewięćdziesiątych XX wieku. Każdego roku syntezowane są nowe substancje jako analogi już istniejących, a ich ilość systematycznie rośnie. Niejednokrotnie wprowadzenie niewielkiej zmiany w strukturze związku może spowodować znaczne zmiany ich właściwości fizykochemicznych oraz psychoaktywnych. Nowe substancje psychoaktywne...
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Selective Cytostatic and Cytotoxic Anticancer Effects of Bisfunctional Agents: A Strategy for the Design of DNA Binding Agents
PublicationVarious agents have been synthesized and proved useful for the National Cancer Institute's anticancer testing as potential new drugs, but most agents suffer side effects from their limited selectivity against cancer cells over healthy ones. Therefore, this paper attempts to describe drugs in terms of the level of tumor cell selectivity which they possess to define the features of mols. that are essential for useful cytotoxicity....
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Expression of a GDSL esterase from Pseudomonas sp. S9 in Pichiapastoris
PublicationCold active lipolytic enzymes are promising to replace the conventional enzymes processes of biotechnological industries. One of the most important feature of the cold-active lipases and esterases is that they offer economic benefits through energy saving. In general, they exhibit high activity at low temperatures and low thermostability at moderate temperatures. Lipolytic enzyme EstS9 was isolated from Pseudomonas sp. S9. A multiple...
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Novel application of terminal restriction fragments length polymorphism method (t-RFLP) for identification of six clinically important Candida sp.
PublicationTerminal restriction fragments length polymorphism method (t-RFLP) is a modified classical RFLP method. The main difference is based on carrying out PCR using a fluorescently labeled primer or primers. The result of such modification is that after digestion of amplicons only terminal fragments of PCR product (containing fluorescent dye) are visualized. T-RFLP method has found application in environmental microbiology and epidemiology....
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Organic solvents aggregating and shaping structural folding of protein, a case study of the protease enzyme
PublicationLow solubility of reactants or products in aqueous solutions can result in the enzymatic catalytic reactions that can occur in non-aqueous solutions. In current study we investigated aqueous solutions containing different organic solvents / deep eutectic solvents (DESs) that can influence the protease enzyme's activity, structural, and thermal stabilities. Retroviral aspartic protease enzyme is responsible for the cleavage of the...
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Proteases immobilized on nanomaterials for biocatalytic, environmental and biomedical applications: Advantages and drawbacks
PublicationProteases have gained significant scientific and industrial interest due to their unique biocatalytic characteristics and broad-spectrum applications in different industries. The development of robust nanobiocatalytic systems by attaching proteases onto various nanostructured materials as fascinating and novel nanocarriers has demonstrated exceptional biocatalytic performance, substantial stability, and ease of recyclability over...
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Selection of effective cocrystals former for dissolution rate improvement of active pharmaceutical ingredients based on lipoaffinity index
PublicationNew theoretical screening procedure was proposed for appropriate selection of potential cocrystal formers possessing the ability of enhancing dissolution rates of drugs. The procedure relies on the training set comprising 102 positive and 17 negative cases of cocrystals found in the literature. Despite the fact that the only available data were of qualitative character, performed statistical analysis using binary classification...
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Predicting Value of Binding Constants of Organic Ligands to Beta-Cyclodextrin: Application of MARSplines and Descriptors Encoded in SMILES String
PublicationThe quantitative structure–activity relationship (QSPR) model was formulated to quantify values of the binding constant (lnK) of a series of ligands to beta–cyclodextrin (β-CD). For this purpose, the multivariate adaptive regression splines (MARSplines) methodology was adopted with molecular descriptors derived from the simplified molecular input line entry specification (SMILES) strings. This approach allows discovery of regression...
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Factors causing degradation of sulfadimetoxine
PublicationSulfadimetoxine is a representative of sulfonamide drugs which presence inhibits growth of activated sludge bacteria, rhat is necessary for the effective mineralization of organic and inorganic contaminants. Therefore factors which con prevent this situation are searched. Aim of this study is selection of conditions causing efficien degradation of the drug- sulfadimetoxine. The impact of such aspects as : the type of oxidizing...
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Opioid Growth Factor and its Derivatives as Potential Non-toxic Multifunctional Anticancer and Analgesic Compounds
PublicationIn this paper, we review the structure-activity relationship of OGF and its analogues. We highlight also OGF derivatives with analgesic, immunomodulatory activity and the ability to penetrate the blood-brain barrier and may be used as safe agents enhancing chemotherapy efficacy and improving quality of life in cancer patients. The reviewed papers indicate that Met-enkephalin and its analogues are interesting candidates for the...
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Phytoplankton communities of polar regions–Diversity depending on environmental conditions and chemical anthropopressure
PublicationThe polar regions (Arctic and Antarctic) constitute up to 14% of the biosphere and offer some of the coldest and most arid Earth's environments. Nevertheless several oxygenic phototrophs including some higher plants, mosses, lichens, various algal groups and cyanobacteria, survive that harsh climate and create the base of the trophic relationships in fragile ecosystems of polar environments. Ecosystems in polar regions are characterized...
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Microcapsules and their applications in pharmaceutical and food industry.
PublicationMicroencapsulation is a process in which tiny particles or droplets are surrounded by a coating or embedded in a homogeneous or heterogeneous matrix, to generate small capsules in size range from a few to few thousand micrometers. The material inside the microcapsule is referred to as the core, internal phase, or fill, whereas the wall is sometimes called shell, coating, wall material, or membrane. It has found application in...
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Biological and mechanical properties of bone cement with nanoparticles - in vivo and in vitro research
PublicationDespite antibiotics preventive treatment, before and after an implant implementation, risk of infection are real. These infections at the implant surface develop in a few months after applying them into the body. To prevent the development of bacteria and to reduce the risk of infection, implants coated with nanoparticles come into use. The Mechanical Department of the Technical University of Gdańsk carried out a research with...
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Impact of high-pressure processing on the bioactive compounds of milk - A comprehensive review
PublicationHigh-pressure processing (HPP) is a promising alternative to thermal pasteurization. Recent studies highlighted the effectivity of HPP (400–600 MPa and exposure times of 1–5 min) in reducing pathogenic microflora for up to 5 logs. Analysis of modern scientific sources has shown that pressure affects the main components of milk including fat globules, lactose, casein micelles. The behavior of whey proteins under HPP is very important...
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Bee Pollen and Bee Bread as a Source of Bacteria Producing Antimicrobials
PublicationThe principal objective of the study was the isolation and identification of bacteria that are present in mature bee bread (BB) and dried (ready for selling and consumption) bee pollen (BP). Obtained isolates were screened for their potential to inhibit select human pathogenic bacteria and their ability to produce enzymes of particular industrial importance. Four and five samples of BP and BB, respectively, were used for the study....
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Electrochemicalsynthesis of 3D nano-/micro-structured porous polypyrrole
PublicationIn this work, electrosynthesis of electroactive, 3D nano-/micro-structured porous polypyrrole film is presented. The PPy film was synthesized potentiostatically in a one-step process from aqueous solution of pyrrole and lithium perchlorate. The growth mechanism of such structure included: the formation of typical globular PPy film, followed by the formation of the PPy fibers, which then took part in the formation of 3D highly porous...
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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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Structural and dynamic changes adopted by EmrE, multidrug transporter protein—Studies by molecular dynamics simulation
PublicationEmrE protein transports positively charged aromatic drugs (xenobiotics) in exchange for two protons and thus provides bacteria resistance to variety of drugs. In order to understand how this protein may recognize ligands, the monomer and asymmetric apo-form of the EmrE dimer embedded in a heterogeneous phospholipid (POPE + POPG) membrane were studied by molecular dynamics simulations. Dimer is regarded as a functional form of the...
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CHEMOTHERAPY-MEDIATED COMPLICATIONS OF WOUND HEALING. AN UNDERSTUDIED SIDE EFFECT
PublicationSignificance: Chemotherapy is a primary method to treat cancer, but while cytotoxic drugs are designed to target rapidly dividing cancer cells, they can also affect other cell types, including dermal cells and macrophages involved in wound healing, which often leads to the development of chronic wounds. The situation becomes even more severe when chemotherapy is combined with surgical tumor excision. Recent advances: Despite its...
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A review on computer‐aided chemogenomics and drug repositioning for rational COVID ‐19 drug discovery
PublicationApplication of materials capable of energy harvesting to increase the efficiency and environmental adaptability is sometimes reflected in the ability of discovery of some traces in an environment―either experimentally or computationally―to enlarge practical application window. The emergence of computational methods, particularly computer-aided drug discovery (CADD), provides ample opportunities for the rapid discovery and development...
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Functionalized Peptide Fibrils as a Scaffold for Active Substances in Wound Healing
PublicationTechnological developments in the field of biologically active peptide applications in medicine have increased the need for new methods for peptide delivery. The disadvantage of peptides as drugs is their low biological stability. Recently, great attention has been paid to self-assembling peptides that can form fibrils. Such a formulation makes bioactive peptides more resistant to enzymatic degradation and druggable. Peptide fibrils...
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Therapeutic Potential of Carnosine and Its Derivatives in the Treatment of Human Diseases
PublicationDespite significant progress in the pathogenesis, diagnosis, treatment, and prevention of cancer and neurodegenerative diseases, their occurrence and mortality are still high around theworld. The resistance of cancer cells to the drugs remains a significant problem in oncology today,while in the case of neuro-degenerative diseases, therapies reversing the process are still yet to be found. Furthermore, it is important to seek new...
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Biological and mechanical properties of bone cement with nanoarticles - in vitro and in vivo research
PublicationDespite antibiotic preventive treatment both before and after implant implementation, the risks of infection are real. These infections develop at the implant surface a few months after inserting them into the body. To prevent the development of bacteria and reduce the risk of infection, implants coated with nanoparticles are used. The Mechanical Department of the Technical University of Gdansk carries out research into using bone...
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Determination of antibiotic residues in honey
PublicationHoney produced by honeybees is a valuable food product. The presence of xenobiotics in honey may harm its quality and constitute a danger to human health. Antibiotics are commonly applied by beekeepers to eliminate disease among honeybees. Moreover, ubiquitous administration of antibiotics may cause bacteria to become resistant to many drugs and spread antibioticresistant strains of bacteria. Appropriate sample preparation and...
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Novel 1,2,3-Triazole Derivatives as Mimics of Steroidal System—Synthesis, Crystal Structures Determination, Hirshfeld Surfaces Analysis and Molecular Docking
PublicationHerein, we present the synthesis and crystal structures determination of five 4-(1-phenyl-1H-1,2,3-triazol-4-yl)phenol derivatives containing halogen atoms, 6a–e, which may be used as an excellent mimic of steroids in the drug development process. Good quality crystals obtained for all of the synthesized compounds allowed the analysis of their molecular structures. Subsequently, the determined crystal structures were used to calculate...
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Investigation of interaction between xanthene dye rhodamine B and metagenomic-derivated methylthioadenosine phosphorylase RSFP
PublicationIn the previous study we found that the expression of the metagenomic - derived methylthioadenosine phosphorylase gene (rsfp) in E. coli cells and the presence of rhodamine B in the growth medium were crucial for the pink fluorescence of one E. coli colony from Antarctic soil metagenomic library (Cieśliński et al., 2009). In this study, rsfp gene expression was induced by an arabinose promoter in an LMG194 E. coli strain and the...
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Common methods for the chiral determination of amphetamine and related compounds I. Gas, liquid and thin-layer chromatography
PublicationThis article reviews the most common, useful methods for the chiral determination of amphetamine (AM) and AM-deriveddesigner drugs in different of matrix, including blood, hair, urine, medicaments or standard solutions, taking into considerationarticles published in the past 15 years. We consider chromatographic methods (e.g., gas, liquid, high-performance liquid, and thinlayer). We describe several types of chiral derivatization...
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Phospholipids as potential prevention factor in carcinogenesis
PublicationPhospholipids are a group of complex lipids, which can be used in cancer chemoprevention. Glicerophospholipids are composed of fatty acids esterified to a glycerol backbone, a phosphate group and a hydrophilic residue such as: cho- line, ethanoloamine, serine or inositol. In the sn-2 position of glicerophospholipid usually there are unsaturated fatty acids, i.e. linolenic acid, while in the sn-1 position more typi- cal are saturated...
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Results of the effect of mixtures of ketoprofen with three cations on the germination of Sorghum bicolor (sorghum) seeds
Open Research DataThe research data includes an attempt to verify whether the addition of cations (sodium, ammonium and potassium) at levels found in the environment would affect the toxicity of pharmaceuticals to Sorghum Bicolor grain. Ion concentrations were selected based on studies of water samples collected in water bodies receiving wastewater from wastewater treatment...
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Results of the effect of mixtures of ketoprofen with three anions on the germination of Sorghum bicolor (sorghum) seeds
Open Research DataThe research data includes an attempt to verify whether the addition of anions (bromide, chloride and fluoride) at levels found in the environment would affect the toxicity of pharmaceuticals to Sorghum Bicolor grain. Ion concentrations were selected based on studies of water samples collected in water bodies receiving wastewater from wastewater treatment...
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Analytical procedures for determination of cocaine and its metabolites in biological samples
PublicationThe dangerous effects and increased usage of illicit drugs have inspired the development of analytical methodologies. We based our review of analytical procedures for determination of cocaine (COC) and its metabolites on literature from the past two decades. Our main aim was to compare the capabilities of different analytical techniques. The diversity of matrices from which COC is determined (e.g., blood, hair, saliva, plasma,...
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Crystal structures of (E)-3-(4-hydroxybenzylidene)chroman-4-one and (E)-3-(3-hydroxybenzylidene)-2-phenylchroman-4-one
PublicationThe synthesis and crystal structures of (E)-3-(4-hydroxybenzylidene)chroman-4-one, C16H12O3,I, and (E)-3-(3-hydroxybenzylidene)-2-phenylchroman-4-one,C22H16O3,II, are reported. These compounds are of interest with respect to biological activity. Both structures display intermolecular C—H---O and O—H---O hydrogen bonding, forming layers in the crystal lattice. The crystal structure of compound I is consolidated...
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3D polypyrrole structures as a sensing material for glucose detection
PublicationIn this work, 3D polypyrrole (PPy) structures as material for glucose detection is proposed. Polypyrrole was electrochemically polymerized on platinum screen-printed electrode from an aqueous solution of lithium perchlorate and pyrrole. The growth mechanism of such PPy structures was studied by ex-situ scanning electron microscopy. Preliminary studies show that studied here PPy film is a good candidate as a sensing material for...
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RESIDUE ANALYSIS OF ETU AND PTU BY LC/MS
PublicationDithiocarbamates (DTCs) are important organosulfur compounds, which act as inhibitors of metal dependant and sulphydryl enzymes and have a serious consequence on biological systems. They possess variety of applications in agriculture as fungicides, as well as, in the rubber industry as vulcanization accelerators and antioxidants. In this way, DTCs are the main group of fungicides used to control approximately 400 pathogens of more...
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Synthesis and antimicrobial activity of 6-sulfo-6-deoxy-D-glucosamine and its derivatives
Publication6-Sulfo-6-deoxy-D-glucosamine (GlcN6S), 6-sulfo-6-deoxy-D-glucosaminitol (ADGS) and their N-acetyl and methyl ester derivatives have been synthesized and tested as inhibitors of enzymes catalyzing reactions of the UDP-GlcNAc pathway in bacteria and yeasts. GlcN6S and ADGS at micromolar concentrations inhibited glucosamine-6-phosphate (GlcN6P) synthase of microbial origin. The former was also inhibitory towards fungal GlcN6P N-acetyl...
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Biochemistry - Laboratory exercises - Nowy
e-Learning CoursesExerise 1. The ability to accumulate metal cations by edible mushrooms, comparison with edible plants Exercise 2. Measurement of activity of glutathione S-transferases - the detoxifying enzymes present in the cytosol of eukaryotic cells Exercise 3. Cell membranes permeability Exercise 4. Detection of mutagenic substances using Ames test Exercise 5. Gluten content in food products part 1. Exercise 6. Gluten content in food...
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Biochemistry - Laboratory exercises
e-Learning CoursesExerise 1. The ability to accumulate metal cations by edible mushrooms, comparison with edible plants Exercise 2. Measurement of activity of glutathione S-transferases - the detoxifying enzymes present in the cytosol of eukaryotic cells Exercise 3. Cell membranes permeability Exercise 4. Detection of mutagenic substances using Ames test Exercise 5. Gluten content in food products part 1. Exercise 6. Gluten content in food...
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Modulation of CYP3A4 activity and induction of apoptosis, necrosis and senescence by the antitumor imidazoacridinone C-1311 in human hepatoma cells
PublicationThere is increasing evidence that the expression level of drug metabolic enzymes affects the final cellular response following drug treatment. Moreover, anti-tumour agents may modulate enzymatic activity and/or cellular expression of metabolic enzymes in tumour cells. We investigated the influence of CYP3A4 overexpression on the cellular response induced by the anti-tumour agent C-1311 in hepatoma cells. C-1311-mediated CYP3A4...
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Characterization of two aminotransferases from Candida albicans
PublicationAminoadipate aminotransferase (AmAA) is an enzyme of α-aminoadipate pathway (AAP) for l-lysine biosynthesis. AmAA may also participated in biosynthesis or degradation of aromatic amino acids and in d-tryptophan based pigment production. The AAP is unique for fungal microorganisms. Enzymes involved in this pathway have specific structures and properties. These features can be used as potential molecular markers. Enzymes catalyzing...
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New Chalcones Derivatives With Potent Antitumor Activity And Their Metabolism In Vitro
PublicationChalcone derivatives exhibit a broad range of biological activities, with antioxidant and cytotoxic properties among the most studied. Despite numerous reports on chalcones as cytotoxic, and potentially anticancer agents, very little is know on their actual mechanism of activity. Generally, chalcones are considered as antimitotic agents, which interfere with tubulin assembly.We have recently developed a new class of chalcones with...
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Recent developmentsinthesynthesisand biological activityofacridine/acridoneanalogues
PublicationMany people in the world struggle with cancer or bacterial, parasitic, viral, Alzheimer's and other diseases. Therefore, many scientists seek new, more effective, more selective and less toxic drugs. Acridine/acridone derivatives constitute a class of compounds with a broad spectrum of biological activity and are of great interest to scientists. Todate, many acridine/acridone analogues have been obtained,which, inter alia, exhibit...
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Rapid determination of multiple aminoglycoside antibiotics in veterinary formulations by ion-pair chromatography coupled with evaporative light scattering detection
PublicationA fast and simple method for simultaneous determination of eight aminoglycoside antibiotics using ion-pairing liquid chromatography (IPLC) coupled with evaporative light scattering detection (ELSD) has been developed and validated. Separation of amikacin, apramycin, gentamicin (as a sum of gentamicin C1, C2 and C1A), kanamycin A, neomycin B, paromomycin, streptomycin and tobramycin was achieved using C18 column with H2O and MeOH/acetone,...
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Recurrent potential pulse technique for improvement of glucose sensing ability of 3D polypyrrole
PublicationIn this work, a new approach for using a 3D polypyrrole (PPy) conducting polymer as a sensing material for glucose detection is proposed. Polypyrrole is electrochemically polymerized on a platinum screen-printed electrode in an aqueous solution of lithium perchlorate and pyrrole. PPy exhibits a high electroactive surface area and high electrochemical stability, which results in it having excellent electrocatalytic properties. The...
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Nutritional and Pharmaceutical Properties of Bioactive Compounds in Organic and Conventional Growing Kiwifruit
PublicationThe bioactivity of two kiwifruit’s cultivars growing under organic and conventional conditions were studied and compared. The bioactive compounds were extracted with water and ethanol using similar conditions which are applied in pharmaceutical applications and for daily fruit consumption such as tea drink. Antioxidant radical scavenging assays [ferric-reducing/antioxidant power (FRAP); cupric reducing antioxidant capacity (CUPRAC);...
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Recent developments in biological sample testing methods for the confirmation of gestational exposure to tobacco smoke anddrugs of abused
PublicationSubstance use is most prevalent in reproductive-aged people also by women during pregnancy. In national prevalence surveys among women aged 15 to 44 years, 10.8 % of women reported using alcohol during pregnancy, 17 % reported smoking during pregnancy, and 4.4 % reported abusing any illicit substances during pregnancy. Virtually all illegal drugs, such as heroin and cocaine, pose dangers to a pregnant woman. Legal substances, such...