[Mechanism of prolonged hypocoagulation appearing after intratracheal administration of heparin]. / Mekhanizm prolongirovannoi gipokoaguliatsii, voznikaiushchei pri intratrakheal'nom vvedenii geparina.

The comparative study of intratracheal and intravenous effect of administration of heparin on blood clotting and mast cell population condition was carried out in experiments. Unlike intravenous bolus injection of heparin, which induced fast short-time inactivation of all enzyme clotting factors, a single intratracheal injection inactivated "internal" rout of thrombin production. It was shown, that long-term hypocoagulability effect and inhibition of factors of blood coagulation after intratracheal administration of heparin correlated with accumulation of heparin in mast cell.

[The reaction of the mast cell population to the intratracheal administration of heparin and fucoidan]. / Reaktsiia tuchno-kletochnoi populiatsii na intratrakheal'noe vvedenie geparina i fukoidana.

Mast cell population of rat after single intratracheal injection of heparin and fukoidan was investigated with cytofluorometry and cytochemical methods. These polysaccharides have great differences in the molecular weight nevertheless they both were found to include in mast cells.

[The anticoagulant and lipolysis-stimulating activity of polysaccharides from marine brown algae]. / Antikoguliantnaia i stimuliruiushchaia lipoliz aktivnost' polisakharidov iz burykh morskikh vodoroslei.

The search for the compounds inducing release of lipoprotein lipase in the blood flow was made in the series of sulfated polysaccharides of brown sea algae of the Japanese Sea--fucoidanes. The effects of the substances on the blood coagulability were studied. Single intravenous injections of the substances were followed by the combined but independent anticoagulant and lipolysis-stimulating effects. Fucoidane isolated from Pelvetia wrightii possessed the greatest lipolysis-stimulating activity along with a weak anticoagulant effect. The degree of the pharmacological effects of the studied compounds did not depend on the degree of sulfation of macromolecules of the polysaccharides. In contrast to heparin fucoidanes exhibited the maximum effect on lipolysis later, 120-180 minutes after the intravenous injection.

[Nucleic acid synthesis and spatial organization of DNA in the presence of heparin and the quaternary ammonium salt of the conidin oligomer-25]. / Sintez nukleinovykh kislot i prostranstvennaia organizatsiiaDNK v prisutstvii geparina i chetvertichnoi ammoniinoi soli oligomera-25 konidina.

A comparative study of polyconidin effects in the replicative and transcription activity of hepatocyte DNA in intact animals, and on peculiarities of spatial organization DNA in the DNA complex with oligomer-25 conidin was carried out. It was shown that polyconidin binding to DNA results in "cross-linking". This process is accompanied by formation of liquid-crystalline dispersion without abnormal optical activity. Liquid crystals possess high density packing of DNA molecules complexed with quaternary ammonium salt of oligomer-25 conidin. The addition of heparin to liquid-crystalline dispersions or phases, destroys the structure of the DNA complex with quaternary ammonium salt of oligomer-25 conidin. As a result "free" DNA molecules appear, they form the cholesteric liquid-crystalline phase. An increase in transcription activity and synchronization of DNA synthesis in hepatocyte was demonstrated. A correlation between chromatin modification and biological activity of chromatin after formation of the DNA--oligomer-25 conidin complex is proposed.

[The dynamics of the body distribution of heparin and its antagonist, the quaternary ammonium salt of conidine oligomer-25, when administered via the lungs]. / Issledovanie dinamiki raspredeleniia v organizme geparina i ego antagonista--chetvertichnoi ammoniinoi soli oligomera-25 konidina, vvedennykh cherez legkie.

The distribution in the organism of radioactivity after intratracheal administration of labelled heparin and its quarterly ammonium salt oligomer-25 conidine was studied. Within 25 hours the preservation of a high level of radioactivity in plasma, its decrease in other investigated organs and the accumulation in mast cells of the peritoneal cavity were observed. The involvement of the lymphatic system in heparin metabolism was shown. A positively charged oligomer conidine administered intratracheally, in contrast to heparin, was not detected in blood plasma in the studied time. The accumulation of the drug in the lung tissue, lymph nodes and excretory organs was noted.

[A comparative study of the antiheparin activity and acute toxicity of stellins]. / Sravnitel'noe issledovanie antigeparinovoi aktivnosti i ostroi toksichnosti stellinov.

The comparative study of the antiheparin activity and acute toxicity of the commercial preparation stellin and its homogeneous fractions was carried out. The summary preparation stellin along with a low antiheparin activity possessed a high toxicity explained by the content of ballast proteins of the nonprotamin nature. One of the homogeneous fractions--stellin B had the best antiheparin properties (heparin neutralizing ratio of 8:1 w:w) and a low toxicity due to a high content of arginine residues and a rigid macromolecular structure facilitating the interpolymer interaction with heparin.

[Effect of intratracheal administration of heparin on the status of the mast cell population in the rat]. / Vliianie intratrakheal'nogo vvedeniia heparina na sostoianie tuchnokletochnoi populiatsii u krys.

The relationship between the blood coagulation changes after intratracheal injection of heparin and the mast cell population condition was studied. A single intratracheal injection of heparin (3500 U/kg) was found to induce a long-term hypocoagulability effect developing parallel to heparin accumulation by mast cells of the peritoneal and pleural cavities.

[Study of the mechanism of the anticoagulant action of fucoidans]. / Izuchenie mekhanizma antikoaguliantnogo deistviia fukoidanov.

The comparative study of the anticoagulant activity of fucoidans, sulphated polysaccharides of brown sea algae was carried out in experiments in vivo. It was shown that compounds of this class possess the anticoagulant activity comparable with that of heparin but with a different mechanism of action. The anticoagulant effect of fucoidans is determined by inhibition of the activity of the blood coagulation "internal" route factors - XI, XII and VIII, the activity of the prothrombin complex factors - II, V and X not changing significantly. It was established that a reduction of the activity of the factors belonging to serine proteases occurs mainly without involvement of antithrombin III.

[Heparin and its antagonist--a quaternary ammonium salt of oligomer-25-conidine: distribution in subcellular organelles, effect on DNA synthesis in the regenerating rat liver]. / Geparin i ego antagonist--chetvertichnaia ammoniinaia sol' oligomera-25-konidina: raspredelenie po subkletochnym organellam, vliianie na sintez DNK v regeneriruiushchei pecheni krys.

Dynamics of distribution in subcellular organelles as well as effects on DNA synthesis of heparin, polycanidine (ChAS oligomer of 25 canidine) and their complexes were studied in regenerating rat liver tissue after partial hepatectomy. Polycanidine and heparin penetrated from circulation into hepatocyte cells, nuclei and mitochondria. After consecutive administration of polyelectrolytes polycanidine increased 2-2.5-fold the amount of heparin entering into cells. Polycanidine formed stable complexes with DNP in nuclei. Heparin and its complexes with polycanidine decreased the DNA synthesis within first day. Heparin appears to be responsible for the inhibitory effect, whereas administration of polycanidine only into animals caused a slight increase in 3H-thymidine incorporation into DNA as compared with controls.

[The effect of normobaric hypoxic stimulation on the aggregation properties of blood cells in an irradiated host]. / Vliianie normobaricheskoi gipoksicheskoi stimuliatsii na aggregatsionnye svoistva kletok krovi obluchennogo organizma.

The influence of a short-term intermittent stimulation by hypoxia on the aggregative properties of platelets and erythrocytes of irradiated body has been investigated. The results show a favourable effect of hypoxic stimulation on some platelet aggregation indices.

[Comparative study of the anticoagulant activity of sulfated polysaccharides from marine brown algae]. / Sravnitel'noe issledovanie antikoaguliantnoi aktivnosti sul'fatirovannykh polisakharidov burykh morskikh vodoroslei.

A comparative study of the anticoagulant activity of fucoidan, sulfated polysaccharides of brown sea algae, was carried out during in vitro and in vivo experiments. Among the compounds of this class of nonlinear polyanions of sea algae there were detected the substances possessing a low toxicity and anticoagulant activity comparable with that of heparin. However the mechanism of action of the studied compounds differs from that of heparin.

[Effect of the synthetic heparin antagonist, conidine oligomer 25, on the synthesis of nucleic acids in regenerating liver cells]. / Vliianie sinteticheskogo antagonista geparina oligomera-25 konidina na sintez nukleinovykh kislot v kletkakh regeneriruiushchei pecheni.

Localization of 14C-conidine oligomer (the synthetic antagonist of heparin) and of polyelectrolyte complex heparin-conidine oligomer 25 was studied in cells of regenerating liver tissue within 20 hrs after partial hepatectomy in rats. Effects of heparin, conidine oligomer 25 and of their polyelectrolyte complex on synthesis of nucleic acids were studied. Conidine oligomer 25 penetrated from circulation into hepatocytes and subcellular organelles of regenerating liver cells and was localized mainly in cytosol (75-88%). In nuclei and mitochondria of the hepatocytes 14C-conidine oligomer 25 was mostly found in the fraction of low density of the organelles. Polyanion heparin, polycation conidine oligomer 25 and their polymeric complex impaired replication and transcription processes.

[Comparative study of the anticoagulant activity of sulfated polysaccharides from red marine algae]. / Sravnitel'noe issledovanie antikoaguliantnoi aktivnosti sul'fatirovannykh polisakharidov krasnykh morskikh vodoroslei.

Experiments in vitro and in vivo were made to study and compare anticoagulant activity and acute toxicity of a great number of sulfate polysaccharides isolated from red sea algae. Polysaccharides were identified, producing an appreciable anticoagulant effect similar to that of heparin. The heparin-like effect of polysaccharides from red sea algae depends on the structure of the carbohydrate chain and the degree of macromolecule sulfation.

[Effect of regulating blood clotting with heparin and its antagonists on mast cells]. / Vliianie reguliatsii svertyvaniia krovi geparinom i ego antagonistami na tuchnye kletki.

The paper concerns the effect of heparin and its antagonists, protamine and 2,5-ionen, on mast cell population from the standpoint of its potential action on blood coagulation. It has been established that intravenous administration of heparin is accompanied by its deposition in mast cells, that gives rise to rapid excretion of the anticoagulant from the blood flow. It has been also shown that protamine sulfate and 2,5-ionen produce degranulation of mast cells, but the synthetic polycation is superior over protamine sulfate in binding heparin of extracellular granules. Retaining of the increased saturation of mast cells with heparin on neutralization of the anticoagulant effect with protamine forms a structural basis for the origination of recurrent heparinemia. Study of blood coagulation has shown that 2,5-ionen is a more efficacious heparin antagonist than protamine sulfate.

[Morphometric analysis of a mast cell population]. / Morfometricheskii analiz populiatsii tuchnykh kletok.

A composite morphometric approach to the analysis of mast cell population is proposed including 4 criteria: the cytogram, the index of heparin saturation, degranulation index, a relative rate of degranulation form. The sensitivity and informative capacity of the composite morphometric analysis were tested in two experimental models: inoculation of heparin and inoculation of its antagonists. Subtle differences in the effect of mast cell degranulaton were found after inoculation of protamine sulphate and a synthetic polycation, 2.5-ionen. Important information on the consumption of exogenous heparin by mast cells was obtained. The simplicity of the analysis as well as the possibility of using its simplified version make the method available for both clinical and experimental pathology.