Luminescent polyelectrolytes with antiviral activity.

Radical polymerization was used to synthesize and characterize (co)polymers with sodium styrenesulfonate (NaSS), 4-methacryloylamidosalicylic acid (MASA), and N-vinylpyrrolidone, which have a low cytotoxicity and a high antiviral activity against the human respiratory syncytial virus. The interaction of copolymers with Tb3+ ions was studied. The complexes formed in dilute aqueous solutions at a concentration of MASA units c ⩽ 1 · 10-4 mol L-1 demonstrate a strong luminescence. The luminescence intensity is independent of copolymer composition, but increases when the NaSS units are substituted with uncharged N-vinylpyrrolidone units. The obtained Tb3+ polymer complexes are promising luminescent sensors for the visualization of biological objects interacting with copolymers.

Metal-Polymer Complexes of Gallium/Gallium-68 with Copolymers of N-Vinylpyrrolidonewith N-Vinylformamideand N-Vinyliminodiacetic Acid: A Hint for Radiolabeling of Water-Soluble Synthetic Flexible Chain Macromolecules.

Copolymer of N-vinylpyrrolidone (VP) with vinylformamide (VFA) and N-vinyliminodiacetic acid (VIDA) was synthesized; its metal-polymer complexes (MPCs) with gallium were obtained. The complexes were characterized by size exclusion chromatography, hydrodynamic and optical methods, scanning electron microscopy, and spectral methods (UV, IR, 1Н NMR spectroscopy). It was demonstrated that in going from polymer to complex, hydrodynamic parameters of macromolecules change only slightly, although the polymer contains intramolecular Ga(VIDA)2 fragments in its structure. A new method for preparation of MPCs with gallium and gallium-68 radionuclide was suggested. The obtained metal-polymer complex is stable over a wide range of pH values as well as in the histidine challenge reaction. In vivo distribution experiments in intact animals showed high primary accumulation of thegallium-68 MPC in blood with subsequent excretion via urinary tract.

Study of N-vinylpyrrolidone-N-vinylformamide copolymers labelled with indium-113m.

The procedure of the directed synthesis of N-vinylpyrrolidone-N-vinylformamide (VP-VFA) copolymers with grafted iminodiacetate (IDA) chelating units is presented. The methods for labelling resulting conjugates with indium-113m were developed. The metal-copolymer conjugates were characterized by different physicochemical methods, including IR and NMR, viscometry, light scattering, and exclusion high-performance liquid chromatography. Parameters of radiochemical synthesis of the conjugates labelled with indium-113m were optimized. It was shown that the VP-VFA-IDA copolymer firmly binds indium-113m both in the acid and alkaline solutions, with pH of the reaction mixture having almost no effect on the complexation. VP-VFA-IDA-In conjugates were found to be unstable in histidine challenge reaction.

[The effect of synthetic polycation polyallylamine on adhesion and viability of CHL V-79 RJK Chinese hamster fibroblasts with different heat resistance].

The effects of synthetic polycation polyallylamine (PAA) on adhesion of CHL V-79 RJK fibroblasts and CHL V-79 RJK40 cells resistant to 40 degrees C, and attachment to these cells to polycation immobilized on polystyrene surface were studied. We have also investigated the cytotoxicity of PAA. It was shown that cell adherence to polystyrene plastic coated with PAA was enhanced or decreased in dependence of the PAA concentration used for surface coating and did not depend on heat resistance of investigated cell lines. The effect of PAA on cell adhesion to uncoated polystyrene surface after cell exposure with PAA depended not only on the polycation concentration, but also on the extent of heat resistance of investigated cell lines. Pretreatment of CHL V-79 RJK cells with PAA at the nontoxic concentrations led to inhibition of cell adhesion, and no change in adhesive properties of thermoresistant cells was found under the same conditions. PAA was toxic for CHL V-79 RJK and CHL V-79 RJK40 cells only at concentrations of 100 microg/ml (MTT assay). PAA-induced acute toxicity was accompanied by necrotic-like cell damage. Possible mechanisms of the PAA effect on the behaviour of cells with different structural and metabolic characteristics that are due to the temperature of cell cultivation are discussed.

DNA-polycation complexes: effect of polycation structure on physico-chemical and biological properties.

The purpose of the study was to investigate the influence of cationic polymer structure on the formation of DNA-polycation complexes and their transfection activity. Primary, tertiary, and quaternary polyamines with molecular masses ranging from 8000 to 200,000 were investigated. DNA-cationic polymer interaction was characterized by low gradient viscometry, dynamic light scattering, circular dichroism, UV spectrometry, flow birefringence, DNA electrophoresis, and electron microscopy. Transfection activity of the complexes was evaluated by the expression of reporter gene (beta-galactosidase) and using synthetic FITC-labelled oligonucleotides. Complex formation was found to be dependent on the structure and molecular weight of the polymer and the ionic strength of the solution. Secondary DNA structure in complexes was not disrupted, and DNA was protected from protonation. Cell lines of different origin were used for testing of transfection activity of the complexes. The sensitivity of the cells to transfection was established to be highly dependent on the cell line. DNA-polycation complexes are non-toxic according to MTT. Polyallylamine, and polydimethylaminoethylmethacrylate were found to be the most promising polycations for gene delivery. Transfection efficacy of their complexes with DNA to T-98G cells reaches up to 90-100%. It was found that optimal molecular mass of polydimethylaminoethylmethacrylate is in the range of 8000-50,000 Da.

[A short test for potential carcinogenicity of water soluble synthetic polymers].

The effect of synthetic water-soluble polymer with different structure on the appearance in SZNA mice of carcinogen-protein adducts (CPA) containing endogenous carcinogen, 3-oxyanthranilic acid (3-OAA), was investigated. CPA containing 3-OAA (3-OAA-CPA) were detected during the administration of 24 of 30 investigated polymers. The induction of 3-OAA-CPA and the character of their distribution in the organism (in all investigated tissues: serum, extracts of liver, spleen, lungs and kidneys tissues or in single tissues) depended on the chemical structure of polymers. It is concluded, that synthetic polymers represent potential cancerogenic danger, because their administration causes formation of 3-OAA-CPA in the organism of animals.

[Effect of cationic polymers and surface-active substances on bacterial resistance to kanamycin]. / Izuchenie vliianiia kationnykh polimerov i poverkhnostno-aktivnykh veshchestv na ustoichivost' bakterii k kanamitsinu.

The effect of cationic polymers and surface active substances (SAS) on sensitivity of Klebsiella aerogenes 600, Escherichia coli 154 and Proteus vulgaris 7470 to kanamycin was studied. A decrease in the resistance of the above organisms to kanamycin on its use in combination with cationic polymers and SAS was observed. It was shown that such substances inhibited the activity of the enzymes inactivating kanamycin. Their effect was suggested to be due to changes in the lipid surrounding of the enzymes.