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Search results for: UNIERUCHAMIANIE ENZYMÓW
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Oznaczanie struktury triacylogliceroli metodą Brockerhoffa i metodą ISO
PublicationPorównano metody badania struktury triacylogliceroli na przykładzie dwóch różnych olejów roślinnych: oleju rzepakowego i oleju oliwkowego. Stosowano dwie różne metody: metodą Brockerhoffa i metodę ISO. Stwierdzono, że badanie struktury TAG wg ISO wymagało wprowadzenia istotnych zmian do procedury objętej normą. Dla uzyskania ~20% MAG w produktach lipolizy konieczne było sporządzenie zawiesiny enzymu w roztworze TRIS. Po wprowadzeniu...
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STOMACH, Body of stomach - Male, 44 - Tissue image [12060630017624261]
Open Research DataThis is the histopathological image of STOMACH tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: Pannoramic 250 3DHistech slide scanner (20x magnification) and saved to DICOM format.
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Enzymes of the L-methionine biosynthetic pathway as novel molecular targets for antifungal chemotherapy
ProjectsProject realized in Department of Pharmaceutical Technology and Biochemistry according to UMO-2020/39/B/NZ7/01519 agreement from 2021-07-08
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Substancje o działaniu przeciwdrobnoustrojowym jako składniki biodegradowalnych folii z polimerów naturalnych
PublicationArtykuł stanowi przegląd literatury dotyczący substancji dodawanych do folii wytworzonych z biodegradowalnych polimerów naturalnych, przeznaczonych do pakowania żywności, w celu nadania im właściwości przeciwdrobnoustrojowych. Omówiono czynniki przeciwdrobnoustrojowe będące składnikami folii z naturalnych polimerów, takie jak: kwasy organiczne, enzymy i bakteriocyny a także, dodawane do opakowań otrzymywanych z polimerów syntetycznych,...
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Synthesis of the inosine 5′-monophosphate dehydrogenase (IMPDH) inhibitors
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Antiglycoxidative properties of amantadine – a systematic review and comprehensive in vitro study
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Novel synthesis scheme and in vitro antimicrobial evaluation of a panel of (E)-2-aryl-1-cyano-1-nitroethenes
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Flavonoids as inhibitors of human neutrophil elastase
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Flavonoids as tyrosinase inhibitors in in silico and in vitro models: basic framework of SAR using a statistical modelling approach
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Synthesis and biological activity of ester derivatives of mycophenolic acid and acridines/acridones as potential immunosuppressive agents
PublicationImproved derivatives of mycophenolic acid (MPA) are necessary to reduce the frequency of adverse effects, this drug exerts in treated patients. In this study, MPA was coupled with N-(x-hydroxyalkyl)-9-acridone-4-carboxamides or N-(x-hydroxyalkyl)acridine-4-carboxamides to give respective ester conjugates upon Yamaguchi protocol. This esterification required protection of phenol group in MPA. Designed conjugates revealed higher...
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Synthesis of the inosine 5'-monophosphate dehydrogenase (IMPDH) inhibitors
PublicationIn this review are summrized newly described IMPDH inhibitors. The article concerns both synthetic pathways and biological activities of the most promising compounds.
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The synthesis and biological activity of lipophilic derivatives of bicine conjugated with n3-(4-methoxyfumaroyl)-l-2,3-diaminopropanoic acid(fmdp) - an inhibitor of glucosamine-6-phosphate synthase
PublicationOtrzymano serię pochodnych bicyny połączonych z inhibitorem syntazy glukozamino-6-fosforanu (fmdp)oraz zbadano ich właściwości lipofilowe i aktywność przeciwgrzybową. otrzymane związki charakteryzowały się wyższą llipofilowością niż fmdp. wszystkie otrzymane związki wykazywały także wyższą aktywność przeciwgrzybową niż fmdp.
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Chemical reactivity and antimicrobial activity of N-substituted maleimides
PublicationZsyntezowano kilkanaście N-podstawionych maleimidów, zawierających w swojej strukturze podstawniki o różnej wielkości i polarności.Maleimidy o charakterze obojętnym wykazywały silny efekt przeciwgrzybowy; ich aktywność przeciwbakteryjna była zróżnicowana. Niską aktywność przeciwbakteryjną, ale wysoką aktywność cytostatyczną stwierdzono dla maleimidów o charakterze zasadowym. Reaktywność chemiczna i lipofilowość miały wpływ na aktywność...
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Novel amides of mycophenolic acid and some heterocyclic derivatives as immunosuppressive agents
PublicationThe group of new amide derivatives of mycophenolic acid (MPA) and selected heterocyclic amines was synthesised as potential immunosuppressive agents functioning as inosine-5'-monophosphate dehydrogenase (IMPDH) uncompetitive inhibitors. The synthesis employed uronium-type activating system (TBTU/HOBt/DIPEA) while or phosphonic acid anhydride method (T3P/Py) facilitating amides to be obtained in moderate to excellent yields without...
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9,10-Dioxoanthracenyldithiocarbamates effectively inhibit the proliferation of non-small cell lung cancer by targeting multiple protein tyrosine kinases
PublicationAnthraquinones have attracted considerable interest in the realm of cancer treatment owing to their potent anticancer properties. This study evaluates the potential of a series of new anthraquinone derivatives as anticancer agents for non-small-cell lung cancer (NSCLC). The compounds were subjected to a range of tests to assess their cytotoxic and apoptotic properties, ability to inhibit colony formation, pro-DNA damage functions,...
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Development of potent and effective SARS-CoV-2 main protease inhibitors based on maleimide analogs for the potential treatment of COVID-19
PublicationIn the present work, we report a new series of potent SARS-CoV-2 Main Protease (Mpro) inhibitors based on maleimide derivatives. The inhibitory activities were tested in an enzymatic assay using recombinant Mpro (3CL Protease from coronavirus SARS-CoV-2). Within the set of new Mpro inhibitors, 6e demonstrated the highest activity in the enzymatic assay with an IC50 value of 8.52 ± 0.44 mM. The IC50 value for Nirmatrelvir (PF-07321332,...
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Palindromic carbazole derivatives: unveiling their antiproliferative effect via topoisomerase II catalytic inhibition and apoptosis induction
PublicationHuman DNA topoisomerases are essential for crucial cellular processes, including DNA replication, transcription, chromatin condensation, and maintenance of its structure. One of the significant strategies employed in cancer treatment involves the inhibition of a specific type of topoisomerase, known as topoisomerase II (Topo II). Carbazole derivatives, recognised for their varied biological activities, have recently become a significant...
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Design, synthesis and biological evaluation of novel N-phosphorylated and O-phosphorylated tacrine derivatives as potential drugs against Alzheimer’s disease
PublicationIn this work, we designed, synthesised and biologically investigated a novel series of 14N- and O-phosphorylated tacrine derivatives as potential anti-Alzheimer’s disease agents. In the reaction of 9-chlorotacrine and corresponding diamines/aminoalkylalcohol we obtained diamino and aminoalkylhydroxy tacrine derivatives. Next, the compounds were acid to give final products 6–13 and 16–21 that were characterised by 1H, 13 C, 31P...
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Recent progress in the development of steroid sulfatase inhibitors – examples of the novel and most promising compounds from the last decade
PublicationThe purpose of this review article is to provide an overview of recent achievements in the synthesis of novel steroid sulfatase (STS) inhibitors. STS is a crucial enzyme in the biosynthesis of active hormones (including estrogens and androgens) and, therefore, represents an extremely attractive molecular target for the development of hormone-dependent cancer therapies. The inhibition of STS may effectively reduce the availability...
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New potent steroid sulphatase inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives
PublicationIn the present work, we report a new class of potent steroid sulphatase (STS) inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives. Within the set of new STS inhibitors, 6-(1-(1,2,3-trifluorophenyl)-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate 3L demonstrated the highest activity in the enzymatic assay inhibiting the STS activity to 7.98% at 0.5 µM concentration. Furthermore, to verify...
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The influence of different acids and pepsin on the extractability of collagen from the skin of Baltic cod (Gadus morhua)
PublicationZastosowano 5,0 M roztwory kwasu cytrynowego, mlekowego, octowego oraz 0,115 M roztwór kwasu solnego. Kolagen z całych skór ekstrahowano w 4 st.C odpowiednimi kwasami (1 : 6, w/v) w czasie 24, 48 i 72 h. Stwierdzono, że kwas solny jest najmniej efektywnym rozpuszczalnikiem kolagenu spośród użytych kwasów. W zastosowanych warunkach doświadczeń maksymalnie można wyekstrahować kwasem cytrynowym 60 % kolagenu, kwasem octowym i mlekowym...
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The New LM-PCR/Shifter Method for the Genotyping of Microorganism
PublicationTechniques relies on the ligation of appropriates adapters (LM-PCR) as AFLP, PCR MP and ADSRRS are successfully used for epidemiological studies for prokaryotic and eukaryotic microorganisms. In this study we propose a new method, called the LM-PCR/Shifter, based on the use of a Class IIS restriction enzyme giving restriction fragments with different 4 base 5' overhangs (Shifter) and the ligation of appropriate oligonucleotide...
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A Novel Cryptic Clostridial Peptide That Kills Bacteria by a Cell Membrane Permeabilization Mechanism
PublicationThis work reports detailed characteristics of the antimicrobial peptide Intestinalin (P30), which is derived from the LysC enzyme of Clostridium intestinale strain URNW. The peptide shows a broader antibacterial spectrum than the parental enzyme, showing potent antimicrobial activity against clinical strains of Gram-positive staphylococci and Gram-negative pathogens and causing between 3.04 ± 0.12 log kill for Pseudomonas aeruginosa...
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Targeting Spike‐ACE2 Interface of SARS‐CoV‐2 and its Omicron Variant: A Comparative Screening of Potential Inhibitors for Existing and Anticipating Variants Using Molecular Modelling Approach
PublicationThe recent COVID pandemic has shown major impact on public health and economic crisis. Despite the development of many vaccines and drugs against the severe acute respiratory syndrome (SARS) coronavirus 2, the pandemic still persists. The continued spread of the virus is largely driven by the emergence of viral variants such as α, β, γ, delta, epsilon spike, omicron and its subvariants (BA.1,2,3) which can evade the current vaccines...
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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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Ocena przydatności bakterii Thermus ruber jako źródła termostabilnej alfa-glukozydazy użytecznej do wytwarzania syropów glukozowych
PublicationThermus ruber wytwarza alfa-glukozydazę o maksymalnej aktywności w temperaturze 65 C i przy pH 6,0. Wymieniony enzym zachowuje aktywność w zakresie pH 5,5-8,0 i prawie nie zmniejsza aktywności po 60 min inkubacji w 65 C. Szybkość hydrolizy maltozy, maltotetraozy, maltopentaozy oraz maltoheksaozy maleje wraz ze wzrostem masy cząsteckowej substratu.
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Rtęć w organizmach żywych – źródła i formy występowania, bioakumulacja, metody oznaczania
PublicationRtęć (Hg) jest metalem ciężkim o znanej i szeroko badanej toksyczności. Toksyczność rtęci zależy od formy chemicznej tego pierwiastka. Metylortęć (MeHg) jest uważana za najbardziej toksyczną formę rtęci, która po spożyciu jest bioakumulowana i biomagnifikowana w organizmach znajdujących się na kolejnych, następujących po sobie, ogniwach łańcucha pokarmowego. W ekosystemach wodnych, mikroorganizmy przekształcają nieorganiczne formy...
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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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Hanna Staroszczyk dr hab. inż.
PeopleAbsolwentka Wydziału Inżynierii i Technologii Chemicznej Politechniki Krakowskiej, od 2007 roku pracuje w Katedrze Chemii, Technologii i Biotechnologii Żywności Wydziału Chemicznego Politechniki Gdańskiej. Pracowała w Politechnice Krakowskiej, Akademii Rolniczej w Krakowie, Institute of Food Research w Norwich, Academia Sinica w Tajpej oraz University of Arkansas w Fayetteville. W 2013 roku uzyskała stopień doktora habilitowanego...
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Overproduction of CaMet15p native and His-tag versions.
Open Research DataEnzyme of fungal L-methionine biosynthetic pathway: O-acetylhomoserine sulfhydrylase (Met15p) could be exploited as molecular target for antifungal chemotherapy. The goal of the study was to obtain conditions optimal for protein production with the use of prokaryotic cells. The constructed expression plasmids, designed in three different versions: encoding...
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The electrochemical studies of CB-PLA electrode after surface activation by proteinase K digestion
Open Research DataThe dataset contains the electrochemical studies performed to evaluate surface activation of the CB-PLA 3D printed electrodes by enzymatic hydrolysis in a solution containing proteinase K (72h digestion period). Different enzyme concentrations were evaluated: 0.2, 0.4, 0.6 and 0.8 mg/ml. The studies were performed before surface activation, during and...
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Overproduction of CaStr2p native and His-tag versions.
Open Research DataEnzyme of fungal L-methionine biosynthetic pathway: cystathionine-γ-synthase (CaStr2p) could be exploited as molecular target for antifungal chemotherapy. The goal of the study was to obtain conditions optimal for protein production with the use of prokaryotic cells. The constructed expression plasmids, designed in three different versions: encoding...
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Overproduction of homoserine O-acetyltransferase (CaMet2p) native and His-tag versions.
Open Research DataEnzyme of fungal L-methionine biosynthetic pathway: homoserine O-acetyltransferase (Met2p) could be exploited as molecular target for antifungal chemotherapy. The goal of the study was to obtain conditions optimal for protein production with the use of prokaryotic cells. The constructed expression plasmids, designed in three different versions: encoding...
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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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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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Ocena przydatności bakterii Thermus ruber jako źródła syntazy trehalozy
PublicationWykazano, że termofilna bakteria Thermus ruber jest źródłem syntazy trehalozy,katalizującej wewnątrzcząsteczkową transglikozylację maltozy. Wymieniony enzym przejawia największą aktywność w temp. 65 st. C przy pH 6,5. Najlepszą wydajność syntazy trehalozy uzyskiwano podczas hodowli bakterii w 55 st. C na podłożu zawierającym 0,5% peptonu 0,1% wyciągu drożdżowego i 0,5% maltozy lub skrobi.
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NADPH-Cytochrome P-450 reductase in strongly involved in activating metabolic transformatios of 9-amino-1-nitroacridine antitumor agents
PublicationCelem pracy było wyjaśnienie roli reduktazy cytochromu P-450 jaką odgrywa ten enzym w przemianach metabolicznych dwóch związków przeciwnowotworowych z grupy pochodnych 1-nitroakrydyny. Zastosowano metodę HPLC do rozdziału metabolitów, a badania struktur przeprowadzono stosując metodę ESI-MS. Wykazano, że badana reduktaza jest zaangażowana bardziej w metabolizm aktywacyjny 1-nitroakrydyn niż metabolizm detoksykacyjny.
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Thermostable Pyrococcus woesei beta-D-galactosidase - high level expression, purification and biochemical properties
PublicationGen kodujący termostabilną beta-D-galaktozydazę Pyrococcus woesei zamplifikowano z zastosowaniem techniki PCR i klonowano w komórkach Escherichia coli. Skonstruowany system ekspresji genu pozwolił na uzyskanie znacznej ilości termostabilnego białka w komórkach mezofilnego gospodarza. Enzym oczyszczono z zastosowaniem chromatografii powinowactwa po wcześniejszej denaturacji termicznej białek Escherichia coli i scharakteryzowano...
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DDLMS PCR double digestion Ligation Mediated Suppression PCR - a new technique for bacterial specific differentiation
PublicationA new diagnostic kit for K. oxytoca specific differentiation based on ddLMS PCR (ang. double digest ligation Mediated PCR) technique is shown. As a species-specific DNA fragment pehX gene, encoding the enzyme polygalactouronase, was chosen. The genome sequence of K. oxytoca is digested with two endonucleases: AclI and BclI which cut DNA before and after pehX gene. The polymorphic DNA fragments are ligated with AclI-end-specific...
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Izabela Sinkiewicz dr inż.
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Roman Kotlowski dr hab. inż.
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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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Amino Acid Based Antimicrobial Agents – Synthesis and Properties
PublicationStructures of several dozen of known antibacterial, antifungal or antiprotozoal agents are based on the amino acid scaffold. In most of them, the amino acid skeleton is of a crucial importance for their antimicrobial activity, since very often they are structural analogs of amino acid intermediates of different microbial biosynthetic pathways. Particularly, some aminophosphonate or aminoboronate analogs of protein amino acids are...
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Molecular mechanism of the enzymatic oxidation investigated for imidazoacridinone antitumor drug C-1311.
PublicationPraca miala na celu określenie molekularnego mechanizmu enzymatycznej utleniającej aktywacji wymienionego związku przeciwnowotworowego w takim układzie modelowym, w którym wcześniej wykazano jego kowalencyjne wiązanie się do DNA. Badania struktur chemicznych produktów enzymatycznej aktywacji wykazały, że dwa z nich powstają w wyniku dealkilacji łańcucha bocznego cząsteczki, natomiast dwa inne w wyniku aktywacji pierścienia imidazoakrydonu....
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Enzymatyczne przeestryfikowanie oleju rzepakowego kwasem kaprynowym w układzie reakcyjnym o minimalnej zawartości wody
PublicationOpisano wyniki badań nad wbudowywaniem się kwasu kaprynowego w triacylogli-cerole (TAG) oleju rzepakowego w procesie enzymatycznego przeestryfikowania, prowadzonego w obecności małej ilości wody. Katalizatorem procesu był sn-1,3 specyficzny enzym lipolityczny, Lipozyme IM. Parametrem zmiennym był czas reakcji. Produkty przeestryfikowania analizowano stosując technikę chromatografii kolumnowej, TLC i GLC oraz hydrolizę enzymatyczną...
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Glucosinolates from lepidium peruvianum as potential antiamnestic drugs
PublicationLepidium peruvianum (maca) (Brassicaceae) is a naturally occurring plant mainly in the high Andes of Peru. In recent years, it has been intensively researched in terms of its influence on various diseases and towards health improvement. Alzheimer’s disease is an incurable disease that most often affects adults over the age of 60. As since 2003 the US Food and Drug Administration (FDA) did not approve any new drug for Alzheimer’s...
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A new division of bacterial UvrA homologues
PublicationThe UvrA protein is a DNA-binding and damage-recognition enzyme which participates in the prokaryotic type nucleotide excision repair (NER) pathway. It has recently been noted that some bacterial genomes comprise additional uvrA genes which encode five distinct types of UvrA homologue. We investigated the sequences of over 2400 bacterial genomes and found 130 examples of bacteria containing uvrA 2 genes. The sequence analyses conducted...
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The antioxidative properties of white cabbage (Brassica oleracea var. capitata f. alba) fresh and submitted to culinary processing
PublicationKapusta biała stanowi jeden z podstawowych składników diety w Europie centralnej. W publikacji autorzy skupili się na określeniu właściwościach przeciwutleniających kapusty świeżej, kiszonej i poddanej obróbce termicznej. Te właściwości zostały oszacowane dla soków przy wykorzystaniu systemów pozakomórkowych, w komórkach HT29 pod kątem ochrony przed utlenieniem DNA oraz poprzez symulację GSTs i naprawę DNA. Wszystkie badane soki...