[Cephalopods as a Source of New Antimicrobial Substances].

Under the conditions of emergence of microbial strains with new properties, including antibiotic resistance, in human and animal populations the search for new antimicrobial substances with improved pharmacological properties and new mechanisms of action from natural objects, in particular from aquatic organisms, is continued. This review presents extensive data on antibacterial, antiviral and antifungal properties of biologically active substances (BAS) of different chemical nature, recovered from representatives of the class of cephalopods (squid, octopus, cuttlefish, nautilus). Analysis of the literature shows that antibacterial activity of some BAS is not inferior, but in some cases is even superior to that of the available antibiotics. The authors note that the review includes the results, mainly of the in vitro studies. Adequate extrapolation of these data to the in vivo conditions is required, that could serve as foundation for development of new generations of medicinal compounds, functional foods and biologically active food supplements.

Biologically Active Substances from Marine Hydrobionts with Antibacterial Activity in Composition of New Wound Dressings.

The data on the experimental study of the efficacy of the gel wound dressings based on chitosan and calcium alginate containing bioactive substances from marine hydrobionts with complex therapeutic action (sulfated polysaccharides from brown algae, hydrolyzed bivalves, peptides from nerve ganglia of cephalopods) are described. The model of thermal burns complicated by Staphylococcus aureus infection was used. Planimetric and bacteriological investigations revealed pronounced wound healing and antibacterial effects of the gel coating. The gel containing sulfated polysaccharides from brown algae showed the highest wound healing activity.

[Hepatoprotective effects of extracts and polysaccharides from seaweed].

Antioxidants of natural origin are considered as possible agents for prevention and treatment of liver diseases. Marine algae and in particular their extracts and obtained from them sulfated polysaccharides are significant sources of natural antioxidants. The recent data on the effect of the extracts and sulfated polysaccharides of seaweed on the functional activity of the liver with injuries induced by CCl4, some drugs (paracetamol, diclofenac), N-nitrosocompounds, aflatoxin are presented in the review. Particular attention is paid to the effect of sulfated polysaccharides and in particular fucoidans on the functional activity of the liver in patients with chronic viral hepatitis C. Fucoidan is highly safe and active not only as an antioxidant but also as an inhibitor of HCV replication, has antiinflammatory and immunomodulating effects. The data of the review allow to conclude that seaweed extracts and sulfated polysaccharides may be a basis for development of new generation drugs in the future for the treatment and prevention of liver diseases.

[Cholinesterase activity in tissues of some crab species from the Japan Sea].

The comparative study of the cholinesterase activity in some crab species was carried out for the first time with use of a set of thiocholine substrates. The substrate specificity was studied in stellar nerve, heart, and hemolymph of three crab species. The crab hemolymph was shown to be characterized by the highest enzyme activity. The enzyme from various crab organs has different structure o substrate specificity. Properties of crab enzymes was compared with acetylcholinesterase (AChE) of human blood erythrocytes, butyrylcholinesterase (BuChE) of horse blood serum, enzyme o squids and bivalve molluscs. The obtained data allow the conclusion to be made on differences in properties of enzymes both at the interspecies and at the tissue levels.

[Adaptation of the cholinergic system of Crenomytilus grayanus (Bivalvia, Mytilidae) to the impact of natural and anthropogenic conditions].

The effects of environmental conditions on cholinesterase activity and kinetic parameters of substrate hydrolysis in the hemolymph of the mussel Crenomytilus grayanus were studied. Under seasonal upwellings, the cholinergic system efficiency is provided for by a wide range of efficient concentrations of the substrate, i.e., under such conditions the mussels at the molecular level have a quantitative adaptation strategy of the enzyme. In mussels from the stationary upwelling zone (at a steady low temperature of water) for efficiency of the cholinergic system, the quantitative strategy of enzyme adaptation is realized. In mussels from a highly contaminated site, irreversible damages to the cholinergic process were observed. The affinity of the substrate to the enzyme is highly informative and an appropriate biomarker for the load level and the adaptation capacity of the organism. The affinity of the substrate to the enzyme is recommended as a new biomarker.

[Brain cholinesterases in marine mammals].

Substrate properties of brain cholinesterases were studied in ringed seal and beluga. Kinetic parameters of hydrolysis of thiocholine esters of carboxylic acids were determined. According to the substrate specificity, the enzyme from the brain of marine mammals can be assigned to acetylcholinesterases. Specific properties of the enzyme from the brain of marine mammals were demonstrated in comparison with land animals. The revealed differences in kinetic parameters of the brain enzyme activity are considered in terms of different biochemical adaptation in ringed seal and beluga.

[Substrate specificity of brain cholinesterase activity of evolutionary old species of fishes]. / Substratnaia spetsifichnost' kholinésteraznoi aktivnosti tkani mozga évoliutsionno drevnikh vidov ryb.

An analysis of brain cholinesterase properties in 3 species of cartilaginous fishes and 1 species of chondrostei, was conducted for the first time. The skates brain enzymes, as to substrate specificity, are shown to be referred to acetylcholinesterases, and the shark brain cholinesterase - to atypical acetylcholinesterase. Kaluga brain cholinesterase, as to its substrate specificity, differes from brain enzymes of cartilaginous fishes. The differences in properties of the nervous tissue cholinestarase of the investigated fish species are the parameters of evolutionary divergence of species.

[Optimization of the process of culturing yeast in the presence of the dispersed mineral palygorskite]. / Optimizatsiia protsessa kul'tivirovaniia drozhzhei v prisutstvii dispersnogo minerala palygorskita.

A positive effect from introduction of the highly dispersed mineral palygorskite in the nutrient medium for aerobic batch cultivation of the yeast Saccharomyces cerevisiae, the Kyivsky strain, used in production of champagne has been established experimentally. An adequate mathematical model describing the process of growth has been constructed. Optimal cultivation conditions have been determined which provided for the achievement of such yeast cell concentration in the culture fluid as 116 mln/ml, palygorskite concentration in the nutrient medium being 0.37 g/l and sucrose 2.0 +/- 0.2%. The yeast obtained possess higher fermentation activity.

[Effects of biologically-active dietary supplement from marine biology on cholinesterase activity and blood lipid peroxidation in humans]. / Vliianie biologicheski aktivnoi pishchevoi dobavki iz morskikh gidrobiontov na kholinésteraznuiu aktivnost' i perekisnoe okislenie lipidov syvorotki krovi cheloveka.

Influence of dietary supplement Tinrostim-C on cholinesterase (ChE) activity and serum lipids peroxidation (LP) in patients whose work connects with emotional stress was examined. Activity of ChE was measured by Ellman calorimetric method (with acetylthiocholin as substrate), LP--by fluorimetric method with malone dialdehyde. Tinrostim-C was given three times a day in 0.5 g. On the 10th day of taking the preparation an activity of serum ChE increased 23.5% higher and had been staying higher during the whole period of observation. In vitro experiments showed an activating effect of Tinrostim-C and piracetam for serum ChE. The level of LP being initially higher was decreasing to values close to normal and had been staying at decreased level during the whole period of observation.

[Certain features of culturing Saccharomyces cerevisiae (Kiev strain) in a wine medium]. / Nekotorye osobennosti kul'tirovaniia Saccharomyces cerevisiae (shtamm kievskii) na vinnoi srede.

The growth of yeast Saccharomyces cerevisiae Kyivsky strain, used in production of champagne, has been studied as affected by a number of factors. The optimum values of saccharose concentration and partial pressure of oxygen dissolved in the medium under which the carbohydrate source use efficiency achieved 9 mln cells/mg of saccharose have been established. The strain growth on the nutrient medium with 2% of saccharose traditionally used in the champagne production has been investigated under the conditions of periodic cultivation. It has been shown that at the beginning of cultivation the low values of the economic coefficient were determined by the Crabtree effect. The saccharose concentration in the culture liquid being decreased to 1%, the carbohydrate utilization efficiency decreases considerably. A chemostatic method of the strain cultivation under growth limitation has been proposed to achieve high concentrations of yeast. Under periodical cultivation the saccharose concentration in the culture liquid would be supported at the level of 0.5-1.0% by its fractional introduction to the fermenter.

[The interaction of organosilicon bisammonium compounds with the cholinesterases of Far-Eastern squids and vertebrates. The comparative enzymological, kinetic and conformational aspects]. / Vzaimodeistvie kremniiorganicheskikh bisammonievykh soedinenii s kholinésterazami dal'nevostochnykh kalmarov i nekotorykh pozvonochnykh. Sravnitel'no-énzimologicheskie, kineticheskie i konformatsionnye aspekty.

The research of interaction of cholinesterases from human erythrocytes, horse blood serum, brain of the frog Rana temporaria, optical ganglia of the Pacific squid Todarodes pacificus, as well as optical ganglia of specimens of the Comandor squid Berryteuthis magister from different areas in the Bering sea with 13 organosilicon bis (trimethylammonium) compounds (silane and siloxane rows) as reversible cholinesterase inhibitors have been first studied and generalized. Calculations of the effector structure using the method of theoretical conformational analysis showed higher rigidity of interonium chain of siloxane derivatives and gave grounds to accept the asymmetry of hydrate envelope for these compounds. The data of conformational and kinetic analysis allowed to propose that specificity of antienzymic effect of organosilicon compounds was mainly due to conformational flexibility of interonium chain and the nature of hydration of effector molecule. The new information on the mechanism of catalytic reactions effected by cholinesterases from animals at different evolutionary stages was obtained.

[The interaction of hexamethonium derivatives with the cholinesterases of vertebrates and invertebrates. The physicochemical and conformational aspects]. / Vzaimodeistvie proizvodnykh geksametoniia s kholinésterazami nekotorykh pozvonochnykh i bespozvonochnykh. Fiziko-khimicheskie i konformatsionnye aspekty.

Conformational and geometrical properties of the hexamethylenebis(trimethylammonium) (CH3)3N+-(CH2)6)-N+(CH3)3 (hexamethonium) and its derivatives with various degree of conformational flexibility of interonion chain having disulfide or two dimethylsilane groups or difluoromethylene chain instead of cholinesterase reversible inhibitors have been determined using molecular mechanics methods. Conformation-activity relationships between these inhibitors and different cholinesterases (human erythrocyte acetylcholinesterase, horse plasma butyrylcholinesterase, cholinesterase from the brain of the grass frog Rana temporaria and optical ganglia from the Pacific squid Todarodes pacificus and Comandor squids Berryteuthis magister from various areas) were investigated. Hypothesis of complex influence of conformational and geometrical properties (if molecules on anticholinesterase efficiency of compounds under investigation was formulated.