[Glycol and Phosphate Depot Forms of 4- and/or 5-Modified Nucleosides Exhibiting Antibacterial Activity].

Resistance developed to the majority of drugs used to treat infectious diseases warrants the design of new compounds effective against drug-resistant strains of pathogens. Recently, several groups of modified nucleosides have been synthesized and showed significant antibacterial activity in vitro, but their further studies were difficult to undertake because of their low solubility in aqueous solutions. Nevertheless, new compounds, well soluble in water-organic solutions, were synthesized and found to be more effective in inhibiting the growth of Gram-positive bacteria and mycobacteria. The water-soluble forms of modified nucleosides under study were assumed to be their depot forms. To check the assumption, the compounds were tested for hydrolysis in various media and their molecular docking was performed into the active center of the putative target, Mycobacterium tuberculosis flavin-dependent thymidylate synthase ThyX. Computer modelling showed that the water-soluble analogs do not act as ThyX inhibitors, supporting the assumption of their depot nature. The compounds were resistant to chemical hydrolysis but were hydrolyzed when incubated with porcine liver carboxylesterase, human serum, or Staphylococcus aureus 209P. The results demonstrate that the compounds are most likely depot forms of modified nucleosides.

Biomonitoring of selected persistent organic pollutants (PCDD/Fs, PCBs and PBDEs) in Finnish and Russian terrestrial and aquatic animal species.

BACKGROUND: The Finnish and Russian animal species (semi-domesticated reindeer, Finnish wild moose, Baltic grey seal and Baltic herring) samples were biomonitored in terrestrial and aquatic environments for polychlorinated dibenzo-p-dioxins and dibenzofurans (PCDD/Fs), polychlorinated biphenyls (PCBs) and polybrominated diphenylethers (PBDEs). RESULTS: Grey seal (Halichoerus grypus) was clearly the most contaminated species. The mean PBDE concentration in grey seal was 115 ng/g fat, and the highest WHO-PCDD/F-PCB-TEQ (toxic equivalent set by WHO) was 327 pg/g fat. In Finnish, reindeer WHO-PCDD/F-TEQ varied from 0.92 pg/g fat in muscle to 90.8 pg/g fat in liver. WHO-PCDD/F-TEQ in moose liver samples was in the range of 0.7-4.26 pg/g fat, and WHO-PCB-TEQ in the range of 0.42-3.34 pg/g fat. Overall moose had clearly lower PCDD/F and DL-PCB concentrations in their liver than reindeer. CONCLUSIONS: Terrestrial animals generally had low POP concentrations, but in reindeer liver dioxin levels were quite high. All Finnish and Russian reindeer liver samples exceeded the EU maximum level [8] for PCDD/Fs (10 pg/g fat), which is currently set for bovine animals.

Efficiency of recombinant thymosin ß4 in spontaneous mouse model of chronic dermatitis.

The therapeutic efficiency of recombinant thymosin ß4 (rTß4) synthesized by us was studied in vivo on spontaneous CBRB mouse model that is adequate to human chronic dermatitis. Three applications of the drug during a week significantly alleviated symptoms of the disease in female mice, and in complex with subsequent antibacterial and antifungal therapy led to a pronounced and lasting (2 months) therapeutic effect. The results attest to a possibility of using rTß4 in combination with the known treatment protocols for chronic inflammatory diseases of the skin.

[Membrane technologies in medicine and ecology].

The paper considers the state-of-the-art of membrane technologies, as applied to the needs of medicine and ecology, the major benefits of membranes for microfiltration and ultrafiltration, and perspectives for the application of new membranes based on new materials. A number of membranes based on aromatic polyamide imides (PAs) have been investigated using rotavirus models. Due to the good solubility of PAs in amide solvents, their based asymmetric membranes can be formed in one step, by applying a water setting bath. The one-stage procedure developed at the Institute of High Molecular Compounds, Russian Academy of Sciences, for the synthesis of aromatic PAs allows one to prepare polymers with required viscosity and strength characteristics. This gives rise to a membrane as porous films of digitiform morphology and asymmetric porous structure.