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Wyniki wyszukiwania dla: MYCOPHENOLIC ACID
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New Analogues of Mycophenolic Acid
PublikacjaMycophenolic 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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Modifications of total synthesis of mycophenolic acid
PublikacjaThe total synthesis of mycophenolic acid (MPA), a potent immunosuppressant, was modified. The obtained mycophenolic acid was suitable for further preparation of new prospective immunosuppressants with improved therapeutic properties.
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Synthesis and biological activity of mycophenolic acid-amino acid derivatives
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Synthesis and biological activity of mycophenolic acid-amino acid derivatives
PublikacjaIn search of new immunosuppressants, mycophenolic acid (MPA) was coupled with amino acid methyl esters followed by hydrolysis to analogs bearing free carboxylic groups. The obtained compunds were tested in vitro as growth inhibitors of lymphoid cell line (Jurkat) and human peripheral blood mononuclear cells (PBMC) from healthy donors. According to obtained results recovering of free carboxylic group increased their activity. Additionally,...
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Anticancer Properties of Amino Acid and Peptide Derivatives of Mycophenolic Acid
PublikacjaBackground: Although Mycophenolic Acid (MPA) is applied as prodrugs in clinic as an immunosuppressant, it also possesses anticancer activity. MPA acts as Inosine-5’-Monophosphate Dehydrogenase (IMPDH) inhibitor, where the carboxylic group at the end of the side chain interacts with Ser 276 of the enzyme via hydrogen bonds. Therefore, MPA derivatives with other polar groups indicated high inhibition too. On the other hand, potent...
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Immunosuppressive properties of amino acid and peptide derivatives of mycophenolic acid
PublikacjaMycophenolic acid (MPA) was coupled with amino acids and biologically active peptides including derivatives of tuftsin to modify its immunosuppressive properties. Both amino acid unit in the case of simple MPA amides and modifications within peptide moiety of MPA - tuftsin conjugates influenced the observed activity. Antiproliferative potential of the obtained conjugates was investigated in vitro and MPA amides with threonine methyl...
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New conjugates of mycophenolic acid and their antiproliferative activity
PublikacjaThe new conjugates of mycophenolic acid (MPA) were obtained in the reaction of N6-(ω-aminoalkyl)adenosines with MPA in the presence of EDCI as a coupling reagent. New compounds 4a–h were evaluated on leukemia cell line (Jurkat) and PBMC from healthy donors. Length of the linker influenced observed activity. The compound 4b possessing 1,3-diamine spacer exhibited the most promising results and can be considered to further investigations.
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Synthesis and antimicrobial activity of amino acid and peptide derivatives of mycophenolic acid
PublikacjaThe series of 16 novel amino acid and peptide mycophenolic acid (MPA) derivatives was obtained as potential antibacterial agents. Coupling of MPA with respective amines was optimized with condensing reagents such as EDCI/DMAP and T3P/TEA. Amino acid analogs were received both as methyl esters and also with the free carboxylic group. The biological activity of the products was tested on five references bacterial strains: Klebsiella...
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Novel amides of mycophenolic acid and some heterocyclic derivatives as immunosuppressive agents
PublikacjaThe 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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The Chemistry of Mycophenolic Acid-Synthesis and Modifictions Towards Desired Biological Activity
PublikacjaDokonano przeglądu literatury chemicznej na temat metod syntezy kwasu mykofenolowego oraz jego pochodnych, a także zależności pomiędzy ich strukturą i aktywnością biologiczną.
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Investigations on the immunosuppressive activity of derivatives of mycophenolic acid in immature dendritic cell
PublikacjaThe main activity of mycophenolic acid (MPA) and its analogs is the inhibition of proliferation of T cells. Here, we hypothesized that MPA and its conjugates inhibits also the activity of antigen-presenting cells (APC) including dendritic cells (DCs). We tested the effect of novel amino acid derivatives of MPA and conjugates of MPA with acridines/acridones on DCs by flow cytometry, ELISA and MLR assay. Both acridines/acridone derivatives...
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Synthesis and antiproliferative activity of new mycophenolic acid conjugates with adenosine derivatives
PublikacjaNew conjugates of mycophenolic acid (MPA) and adenosine derivatives were synthesized and assessed as potential immunosuppressants on Jurkat cell line and peripheral blood mononuclear cells (PBMC) from healthy donors. As compared to MPA, all compounds were found to be more active against Jurkat cell line. The antiproliferative activities were compared with MPA and adenosine, in both 2′,3′-O-isopropylidene protected and free hydroxyl...
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Immobilization technique for enhanced production of the immunosuppressant mycophenolic acid by ultraviolet and gamma-irradiated Penicillium roqueforti
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Synthesis and biological activity of novel mycophenolic acid conjugates containing nitro-acridine/acridone derivatives
PublikacjaOpracowano warunki reakcji kwasu mykofenolowego z aminowymi pochodnymi akrydyn i akrydonów. Tak otrzymane koniugaty zostały scharakteryzowane, a następnie przebadane in vitro pod względem aktywności przeciwbiałaczkowej oraz immunosupresyjnej.
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Synthesis and biological activity of ester derivatives of mycophenolic acid and acridines/acridones as potential immunosuppressive agents
PublikacjaImproved 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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Kwas mykofenolowy i jego analogi. Synteza i aktywność biologiczna = Mycophenolic acid (MPA) and its analogues. Synthesis and biological activity
PublikacjaW artykule opisano kwas mykofenolowy (MPA)oraz jego analogi. Kwas MPA został odkryty ponad 100 lat temu i nadal pozostaje atrakcyjnym celem badań biologicznych. Z uwagi na bardzo dużą tendencję do ulegania glukuronidyzacji in vivo, ograniczone są jego możliwości zastosowań jako potencjalnego chemoterapeutyka. Otrzymane dotychczas analogi m.in. zawierające różne cykliczne ugrupowania, monocykliczne fenole i niefenolowe analogi oraz...
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Unlocking the biosynthetic potential of Penicillium roqueforti for hyperproduction of the immunosuppressant mycophenolic acid: Gamma radiation mutagenesis and response surface optimization of fermentation medium
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Agro-industrial byproducts for production of the immunosuppressant mycophenolic acid by Penicillium roqueforti under solid-state fermentation: Enhanced production by ultraviolet and gamma irradiation
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Optimization of submerged fermentation conditions for immunosuppressant mycophenolic acid production by Penicillium roqueforti isolated from blue-molded cheeses: enhanced production by ultraviolet and gamma irradiation
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Matcha Green Tea: Chemical Composition, Phenolic Acids, Caffeine and Fatty Acid Profile
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Bioaccessibility of Phenolic Acids and Flavonoids from Buckwheat Biscuits Prepared from Flours Fermented by Lactic Acid Bacteria
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Hyaluronic acid/tannic acid films for wound healing application
PublikacjaIn this study, thin films based on hyaluronic acid (HA) with tannic acid (TA) were investigated in three different weight ratios (80HA/20TA, 50HA/50TA, 20HA/80TA) for their application as materials for wound healing. Surface free energy, as well as their roughness, mechanical properties, water vapor permeability rate, and antioxidant activity were determined. Moreover, their compatibility with blood and osteoblast cells was investigated....
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Novel Cell Permeable Polymers of N-Substituted L-2,3-Diaminopropionic Acid (DAPEGs) and Cellular Consequences of Their Interactions with Nucleic Acids
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The physicochemical properties of 3D materials based on hyaluronic acid modified by tannic acid addition
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Influence of the Type of Amino Acid on the Permeability and Properties of Ibuprofenates of Isopropyl Amino Acid Esters
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Updates in the Metabolism of Lactic Acid Bacteria
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Structural Analysis of 3,5-Bistrifluoromethylhydrocinnamic Acid
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Lysophosphatidic acid signaling in ovarian cancer
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Amino acid formation by electron irradiation
PublikacjaW artykule zaprezentowano procedurę badania reakcji indukowanych przez niskoenergetyczne elektrony w mieszanych warstwach molekularnych CH3COOD:NH3.
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Equilibrium and kinetic studies on acid dye Acid Red 88 adsorption by magnetic ZnFe2O4 spinel ferrite nanoparticles
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Ultrashort Cationic Lipopeptides–Effect of N-Terminal Amino Acid and Fatty Acid Type on Antimicrobial Activity and Hemolysis
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Elicitation of solid callus cultures of Salvia miltiorrhiza Bunge with salicylic acid and a synthetic auxin (1-naphthaleneacetic acid)
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Constituents of Propolis: Chrysin, Caffeic Acid, p-Coumaric Acid, and Ferulic Acid Induce PRODH/POX-Dependent Apoptosis in Human Tongue Squamous Cell Carcinoma Cell (CAL-27)
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Adsorption Kinetics of Acid Dye Acid Red 88 onto Magnetic Multi‐Walled Carbon Nanotubes‐Fe3C Nanocomposite
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Efficient Diethylzinc/Gallic Acid and Diethylzinc/Gallic Acid Ester Catalytic Systems for the Ring-Opening Polymerization of rac-Lactide
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Microstructural behavior of water-in-oil emulsions stabilized by fatty acid esters of propylene glycol and zinc fatty acid salts
PublikacjaZbadano wpływ składu emulgatorów acylopropylenoglikolowych, modyfikowanych mydłami cynku, na charakter przemian strukturalnych jakim ulegają emulsje W/O stabilizowane przez takie emulgatory. Badano zarówno etap emulgowania jak i mikrostrukturę oraz właściwości reologiczne otrzymanych emulsji.
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Investigation of an elutable N-propylphosphonic acid chitosan derivative composition with a chitosan matrix prepared from carbonic acid solution
PublikacjaPorous chitosan composites using CO2 dissolution procedure and including water soluble N-propylphosphonic chitosan derivative (p-CHI) were obtained and characterized. In contrast to the control material, composites containing modified chitosan distinguished by a rapid moisture absorption and good adhesion to the skin. The FTIR analysis confirmed the presence of propylphosphonic group in the structure of the polymer. The porosity...
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Amino Acid and Peptide‐Based Antiviral Agents
PublikacjaA 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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Phenazine - 2,6-dihydroxybenzoic acid (1/1)
PublikacjaOtrzymano krystaliczny kompleks fenazyny z kwasem 2,6-dihydroksybenzoesowym o stechiometrii 1:1. Badania struktury kompleksu za pomocą metod rentgenograficznych wykazały, że powiązane wiązaniami wodorowymi typu OH...N cząsteczki fenazyny układają się w stosy, które stabilizowane są poprzez oddziaływania typu π-π pierścieni aromatycznych. Cząsteczki kwasu zajmują przestrzenie kanałów tworzonych pomiędzy kolumnami pierścieni aromatycznych...
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The Reason Why HAlCl4 Acid Does Not Exist
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Glycyrrhetinic acid and its derivatives in infectious diseases
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Hydrogen charging of nitrided steel in acid solution
PublikacjaKonstrukcyjną stal, azotowaną w wyładowaniu jarzeniowym w mieszaninie gazów o różnej zawartości N2, H2 i Ar, poddawano katodowemu nawodorowaniu w kwaśnym roztworze, imitującym przepracowany olej maszynowy. W pomiarach szybkości przenikania wodoru i ekstrakcji próżniowej określano wpływ azotowanych warstw, odpowiednio, na transport wodoru i na jego nieodwracalne pułapkowanie. W obecności niezdefektowanej warstwy kompaktowych azotków...
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May dithiophosphoric acid participate in the set process?
PublikacjaZastosowano otrzymane S-tioacyloditiofosforany jako odczynniki tioacylujące do syntezy kwasów tiohydroksamowych. Dla większości N-alkilohydroksyloamin produktem tej reakcji były żądane kwasy tiohydroksamowe. Natomiast gdy substratem jest hydroksyloamina zawierająca duży objętościowo podstawnik na atomie azotu lub gdy posiada dwa podstawniki na atomie azotu w reakcji tej tworzą się wyłącznie odpowiednie O-tioacylohydroksyloaminy....
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The 2:1 cocrystal of benzamide and pentafluororbenzoic acid
PublikacjaKrystaliczna struktura centrosymetrycznej supermolekuły składa się z czterech cząsteczek benzamidu oraz dwóch kwasu karboksylowego, które powiązane są ze sobą za pomocą wiązań wodorowych typu O-H...O oraz N-H...O.
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(S)-N-Nitrosoazetidine-2-carboxylic acid.
PublikacjaAnaliza rentgenograficzna monokryształów kwasu (S)-N-nitozoazetydyno-2-karboksylowego wykazała, że reszta N-nitrozoaminowa przyjmuje konfigurację E. Azetydynowy atom azotu jest nieznacznie piramidalny. Cząsteczki w sieci krystalicznej oddziałują ze sobą poprzez wiązania wodorowe pomiędzy atomem tlenu grupy nitrozowej i atomem wodoru grupy karboksylowej, tworząc polimeryczny łańcuch.
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ASCORBIC ACID IN POLYURETHANE SYSTEMS FOR TISSUE ENGINEERING
PublikacjaThe introduction of the paper was devoted to the main items of tissue engineering (TE) and the way of porous structure obtaining as scaffolds. Furthermore, the significant role of the scaffold design in TE was described. It was shown, that properly designed polyurethanes (PURs) find application in TE due to the proper physicochemical, mechanical and biological properties. Then the use of L-ascorbic acid (L-AA) in PUR systems for...
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Easy formation of acyl-Meldrum's acid anhydride
PublikacjaAcyl Meldrum's acid are usually a good source of ketenes upon definite thermal composition. However we treated acyl-Meldrum's acid with the Lewis acid and we observed formation of 5[[(2,2-dimethyl-4,6-dioxo-1,3-dioxan 5 ylidene)(acyl/arylamino)mathoxy](acyl/arylamino)methylene]-2,2dimethyl-1,3-dioxane-4,6 dione which means acyl-Meldrum's acid anhydride. The chemical properities of acyl-Meldrum's acid anhydride were explored.
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Cytotoxic and Antioxidant Activities of Benzohydroxamic Acid Analogues
Publikacja20 benzohydroxamic acid analogues were synthesized and evaluated for their in vitro cytotoxicities against mouse mammary tumor cells as well as antioxidant activities against DPPH radical and superoxide anion. It was found that benzothiohydroxamic acids exhibit greater cytotoxicities than benzohydroxamic acids and N-isopropyl derivatives are more active than N-methyl ones. On the other hand, benzothiohydroxamic acids show more...
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Dissociative electron attachment to benzoic acid (C7H6O2)
PublikacjaThe dissociative electron attachment (DEA) to benzoic acid (C6H5COOH) has been studied using an experimental crossed beam setup of a quadrupole mass spectrometer and a trochoidal electron monochromator. Relative partial cross sections for the DEA to produce negative ion fragments show the main channels for dissociation. The comparison of the present results with the ultraviolet photoelectron spectrum of benzoic acid [J. Meeks,...
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Encapsulation of Amikacin into Microparticles Based on Low-Molecular-Weight Poly(lactic acid) and Poly(lactic acid-co-polyethylene glycol)
PublikacjaThe 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...