Hemorrhagic Activity of Cationic Starch Conjugates with Sterically Hindered Phenol after Intravenous Administration to Guinea Pigs.

Intravenous injection of cationic starch conjugated with sterically hindered phenol (terpenophenol) to guinea pigs did not increase hemorrhagic activity (in doses of 2 and 4 mg/kg) and plasma clotting time in activated partial thromboplastin time and prothrombin time tests (in a dose of 4 mg/kg) in comparison with administration of physiological saline. Intravenous injection of the cationic starch conjugate with the highest content of terpenophenol fragments (4.1%wt) in a dose of 2 mg/kg to guinea pigs leads to a decrease in hemorrhagic activity by 4 times in comparison with the control.

Formation of gallic acid layer on γ-AlOOH nanoparticles surface and their antioxidant and membrane-protective activity.

In the reported study we prepared gallic acid modified γ-AlOOH nanoparticles. We proposed mechanism of phenolic compounds binding on the alumina, suggesting covalent and electrostatic interactions. Most of the properties of alumina nanoparticles (NPs) are unchanged, but there is partial reduction of surface charge. Prepared samples are colloidally stable hydrosols. It allowed us to perform biological studies on cellular and non-cellular models, which showed nontoxicity of both pure and hybrid γ-AlOOH nanoparticles. Furthermore, pure alumina NPs exhibit antioxidant properties, which are enhanced after gallic acid immobilization on their surface. Also, hybrid alumina-gallic acid NPs showed membrane-protective activity.

Nanochitin/manganese oxide-biodegradable hybrid sorbent for heavy metal ions.

The article presents the results of the synthesis and research of a new biodegradable hybrid nanosized polymer-inorganic system possessing the double nature of heavy metal ions extraction from solutions. Firstly, the sorption of metal ions takes place by the ion-exchange properties of porous manganese oxide and, secondly, due to specific interaction and chelating with functional groups of polysaccharides in terms of nanochitin (ChNC). The synthesis is based on the colloid-chemical processes of interaction between polysaccharide and manganese oxide nanosized particles. Using the mathematical model of the Derjaguin, Landau, Verwey, and Overbeek (DLVO) theory, it has been shown that this interaction occurs due to the formation of hydrogen bonds and electrostatic interactions of oppositely charged particles. Hybrid sorbents were characterised by X-ray diffraction, Fourier transform infrared spectroscopy, Transmission electron and Atomic force microscopy. The highest value of sorption capacity for hybrid materials was obtained for Ni2+ extraction and reached 114.0 ± 1.1 mg/g. It was shown that biodegradation of hybrid sorbents increases with the concentration of manganese oxide nanoparticles and almost complete degradation of the organic part can be performed within 6 days. The obtained biodegradable sorbents were designed to address ecological problems connected with the pollution of natural waters by toxic metallic ions.

Neuroprotective Activity of D-HES in Transient Global Cerebral Ischemia in Rats.

We studied the effect of O-((((4-hydroxy-3,5-di(1,7,7-trimethylbicyclo[2.2.1]hept-exo-2-yl) benzyl)oxy)ethyl)-O-(2-hydroxyethyl)-(1→4)-α-D-glucan (D-HES, 80 mg/kg, intravenously) and reference preparation ethylmethylhydroxypyridine succinate (EMHP-S, 50 mg/kg, intravenously) on rat survival and neurological deficit in 24 h after transient global cerebral ischemia in Wistar rats. Intravenous administration of D-HES and EMHP-S significantly increased the number of survivors by 68 and 78%, respectively, in comparison with the control group. In groups treated with D-HES and EMHP-S, the number of animals with severe neurological deficit was significantly lower and the number of animals moderate or mild neurological deficit was significantly higher than in the control group.

Effect of Nanocrystalline Particles of Chitin on Blood Components in Humans and Experimental Animals.

Nanocrystalline particles of chitin in the form of hydrosol in a concentration of 0.63 mg/ml have no effect on aggregation of human platelets and clotting time of platelet-poor plasma in coagulation tests. ADP-induced aggregation of human platelets was inhibited by these nanoparticles in concentrations of 0.63 and 1.00 mg/ml in comparison with the control. Intravenous administration of nanoparticles in a dose of 1 mg/kg to guinea pigs produced no anticoagulant effect. The nanocrystalline particles of chitin can be of interest as potential drug delivery systems.

Biosorbents based on esterified starch carrying immobilized oil-degrading microorganisms.

The complex sorbents based on hydrophobized starch, which contain oil-degrading microorganisms, have been proposed for effective sorption and utilization of petroleum-related pollutants. The sorbents were made on the base of benzoic, lauric and stearic acid esters of starch with degrees of substitution of 0.4-1.1. The esterification of starch was carried out by the reaction with acyl chlorides of the corresponding acids in an aqueous-organic medium. The structure of the esters was studied by SEM, IR and NMR spectroscopy. As a result of porous hydrophobic structure, these sorbents are capable of binding and retention of petroleum products on the water surface, and keeping the flotation for at least 30days after the petroleum products sorption. The test of biodegradability of the obtained samples revealed that the modified starches can be degraded by microscopic fungi, therefore they do not cause secondary pollution. The cultures of yeast Rhodotorula glutinis VKM Y-2993D and bacteria Pseudomonas libanensis VKM B-3041D immobilized on the sorbent facilitate the rapid utilization of accumulated petroleum products.

Regulation of structure, rheological and surface properties of chitin nanocrystal dispersions.

The hydrosols of chitin nanocrystals (ChN) are promising as modifiers of properties, drug delivery systems, and media. The purpose of this work is to clarify the mechanisms for regulating processes of stability and structure formation occurring in the ChN hydrosols under the influence of varying ionic strength. ChN were isolated from the crab shell; ChN hydrosols are obtained with different concentrations of the dispersed phase. The structure and morphology of the particles was studied by atomic force microscopy and X-ray diffraction. Hydrosols were studied by rotational viscometry, dynamic light scattering, and photometry in the presence of KCl with concentration up to 200mM. The experimental results of finding the rapid coagulation threshold are compared with calculated ones performed with the use of the modified DLVO theory. It is established that in the range of electrolyte concentrations 30∼75mM, the optical and rheological properties of the ChN hydrosols undergo crucial changes. At an electrolyte concentration of 20∼150mM, particles coagulate at a secondary potential minimum; the parallel orientation of the particles is energetically more advantageous. In systems with a higher concentration of electrolyte, there is no potential barrier; rapid barrier-free coagulation is observed, with the formation of stronger coagulation contacts and the formation of stable gels.

Effect of Sulfation and Molecular Weight on Anticoagulant Activity of Dextran.

Sulfation (to 2.8) of dextrans with molecular weight of 150 and 20 kDa was followed by the appearance of anticoagulant activity that increased with decreasing their molecular weight and did not depend on antithrombin, plasma inhibitor of serine proteases of the blood coagulation system. Antithrombin activity of dextran sulfate with a molecular weight of 20 kDa reached 12.6-15.3 U/mg. Dextran sulfates with molecular weights of 20 and 150 kDa did not potentiate ADP-induced human platelet aggregation.

[Antioxidant properties of conjugates of polyethylene glycols, having a terpenophenolic fragments].

A series of water-soluble conjugates has been synthesized from polyethylene glycols of various lengths and 4-bromomethyl-2,6-diisobornylphenol. Evaluation of membrane protective and antioxidant activity of synthesized products on the model of H2O2-induced hemolysis of blood erythrocytes showed that conjugates have considerable antioxidant activity. A significant membrane protective effect was showed in conjugates with 0.2 and 0.8 mass. % of 2,6-diisobornyl-4-methylene fragments.

[Relationship between the anticoagulant activity of sulfated plant polysaccharides and the area of their precipitation with polycations during biospecific electrophoresis].

Polyanions (in an amount within 1.5 - 6.0 mg), including cellulose sulfates (excreted from Gossipium hirsutum L., molecular weight 22.0 kDa, degree of sulfation within 0.8 - 1.8), inulin sulfates (excreted from Helianthus tuberosus, molecular weight 8.0 kDa, degree of sulfation within 0.6 - 1.6), pectin sulfates (excreted from Abies sibirica L., molecular weight 24.0 kDa, degree of sulfation within 0.8 - 1.1), give rise to peaks of precipitation with polycations of protamine sulfate. Only cellulose sulfates (in amount within 0.38 - 6.00 mg) give the peaks of precipitation with chitosan polycations (molecular weight 10 kDa, degree of deacetylation 85%) during horizontal biospecific electrophoresis. The height of the peak of precipitation with protamin sulfate was found to grow with increasing antithrombin activity of cellulose sulfates and pectin sulfate (for polyanions in an amount within 1.5 - 6 mg). The size of the area of precipitation with chitosan was found to decrease with increasing antithrombin activity of cellulose sulfates.

[Dependence of the anticoagulant activity of starch and inulin on their degree of sulfonation].

We have studied a relationship between the degree of sulfonation and anticoagulant activity of starch from Solanum tuberosum (molecular weight, 25000-30000 Da; sulfonation degree, 0.4-2.5) and inulin from Helianthus tuberosus (molecular weight, 7000-8000 Da; sulfonation degree, 0.6-1.6). Starch and inulin sulfates (i) increased the time of appearance of fibrin clots in plasma in coagulometric tests and (ii) reduced (via antithrombin) the rate of thrombin-induced hydrolysis of a chromogen substrate. The antithrombin (aIIa) activity of starch sulfates reached 16.8-70.0 IU/mg and the activity against factor Xa (aXa activity) was 2.3-16.6 IU/mg. The antithrombin activity of inulin sulfates was within 5.5-11.4 IU/mg and the activity against factor Xa (aXa activity) was within 0-1.4 IU/mg. An increase in the degree of sulfonation led to a growth in the anticoagulant activity of starch sulfates. The anticoagulant activity of starch sulfates and inulin sulfate with sulfonation degree 1.0 is mediated by antithrombin, which is the plasma inhibitor of serine proteases.

[Ionic conjugates of sulfate carboxymethyl cellulose with dialkylaminomethyl derivatives of 2-isobornyl-4-methylphenol: synthesis and study of anti-inflammatory and analgesic activity].

Water-soluble sulfate polysalts of carboxymethyl cellulose and tertiary aminomethyl derivatives of 2-isobornyl-4-methylphenol was obtained. For the synthesized conjugates investigated in vivo anti-inflammatory activity in the test of acute formalin inflammation and analgesic activity in tests the "hot plate" and "vinegar cramps".

Sulfated cellulose derivatives inhibit activities of thrombin and activated factor X.

Sulfated derivatives based on powdered cellulose were obtained, including those containing additional (carboxymethyl, ethyl amide or phosphate) groups, and their activity against blood clotting factors (thrombin and Xa) was studied. Maximum antithrombin activity of the test compounds, measured using a coagulation test, was 144±11 U/mg.