Comparative Analysis of Cytotoxic Activity of New Nitrosyl Iron-Sulfur Complexes in Human Tumor Cells In Vitro.

We studied cytotoxic activity of new tetranitrosyl NO-generating binuclear iron-sulfur [Fe-S] complexes containing different ligands in the molecule against tumor cells in vitro. Cytotoxic activity of the most active complex with cysteamine (CysAm) was compared with that of antitumor drug cisplatin. Caspase activation and morphological changes in cells were visualized by fluorescence microscopy.

[Synthesis and cytotoxicity of allobetulin derivatives].

The synthesis and screening of antitumor activity in vitro (cytotoxicity) of various oxygen, nitrogen, sulfur and platinum-containing derivatives of allobetulin, including different arrangements of the double bonds in the A and B rings, penta- and hexacyclic ring A, 21-acetyl-20,28-epoxy-18α,19βH-ursane-isomeric cycle E, was carry out. (3R,5R)-19β,28-Epoxy-4,5-seco-18α-olean-3(5)-ozonide and 2,3-indolo-21β-acetyl-20β,28-epoxy-18α, H-19β-ursane showed significant cytotoxic activity against melanoma MeWo and Leukemia SR cells, appropriately. (3S,5S)-Diastereomer of the first compound showed no cytotoxicity.

[N6-dipeptide derivatives of the N12-ribosyl-indolo[2,3-a]carbazole].

N6-derivatives of N12-ribosyl-indolo[2,3-a]pirrolo[3,4-c]carbazole-5,7-dione are synthesized as potential antitumor agents, in which an atom of N6-pyrrole part of heterocycle is included into the dipeptide residual of the general formula >N6-(CH2)n-CO-Ala/βAla-OMe (n = 2 or 3). These compounds are derived by reacting of 13-methyl-12-(2,3,4-three-O-acetyl-β-D-ribopyranosyl)indolo[2,3-a]furano[3,4-c] carbazole-5,7-dione with dipeptides, having an unreplaced N-amino end-group, in DMF at 130°C, wherein the nitrogen atom of peptide amino group replaces oxygen O6 in furan ring of heterocycle and is embedded in imide nitrogen atom of pyrrole N6. The ability of the obtained compounds to inhibit growth of SKOV3 human ovarian carcinoma cells was studied, only derivative with radical >N6-(CH2)3-CO-L-Ala-OMe showed cytotoxic activity with an inhibitory concentration of IC50 = 8 μM.

In vitro effect of Knotolan, a new lignan from Abies sibirica, on the growth of hormone-dependent breast cancer cells.

Here we present antiestrogenic effects of Knotolan, a new dietary lignan from Abies sibirica raw material. Knotolan abolished growth-stimulating effects of 17β-estradiol on hormone-dependent MCF-7 cells.

[Toll-like receptor-mediated functional activity of mononuclear cells in children with neutropenia].

Aim: To study the Toll-like receptor (TLR)-mediated functional activity of peripheral blood mononuclear cells (PBMC) from children with different forms of neutropenia.

Materials And Methods: TLR-mediated functional activity of PBMC was evaluated by production of proinflammatory cytokines--TNF alpha and IFN alpha. Ligands for TLR1/2, TLR 2/6, TLR4, TLR5, and TLR9 were used to stimulate TNF alpha production by PBMC from healthy children and children with neutropenia.

[The physicochemical and biological properties of the bovine hemoglobin polymer].

A study was made of bovine hemoglobin polymer obtained by a new method: intraerythrocytic polymerization of hemoglobin followed by isolation of hemoglobin polymer. The polymer obtained had weighted mean and numerical average molecular mass of 388 kD and 134 kD, respectively, P 32 mm Hg, arteriovenous difference 5.1 vol%, Hill's coefficient 2.

[Isolation of factor IX concentrate from cryosupernatant of donor's plasma].

Soviet anion-exchangers were comparatively studied to specify an optimal carrier useful for isolation of factor ix of the blood coagulation system from donor's blood cryosupernatant. The main criteria of gel selection were the yield and purification degree of factor IX, as well as its specific activity and concentration in eluates. It has been shown that DEAE-agarose 6B-CL, possessing pronounced activity with respect to specific sorption of factor IX, meets these requirements to the greatest degree.

[Study of functional properties of chemically-modified hemoglobin during circulation in the blood channel].

Functional activity of the solutions of chemically modified hemoglobins (Hb) with different structure had been investigated during the replacement of acute fatal blood loss in dogs. It was found the correlation between polymerization degree of Hb derivatives and alterations of its oxygen-carrying characteristics in the process of circulation. It was shown that decline of functional activity at the prolonged terms of circulation was more expressed for macromolecular Hb derivatives with heterogeneous structure.

[The structuro-functional heterogeneity of an artificial oxygen carrier based on hemoglobin].

Pyridoxylated polymerized hemoglobin (PP-Hb) was fractionated by the method of high pressure liquid chromatography, Molecular weight distribution, oxygen carrying capacity and antigenic characteristics of separated fractions have been investigated. It was demonstrated that a fraction may be separated from the crude PP-Hb, which is greatly homogeneous if structural and functional characteristics are concerned, and also optimal according to the parameters investigated. So, by a corresponding fractionation method it is possible to overcome the main limitation for use of PP-Hb as an artificial oxygen carrier--its heterogeneity.

[Effect of lowered relative humidity of the air on the accumulation of plutonium-239 in the body and its biological effectiveness].

The experiments on rats show that the 4-month elevated air dryness has no impact on body accumulation of 239Pu but causes more distinct forms of bronchitis and interstitial pneumonia combined with the strain in medullary hemopoiesis and reactivity intensification of pulmonary and B-system immunity. Under prolonged effect of both factors a breakdown in fully adequate immune response can occur.

[Distribution of plutonium-239 in the body of dogs 7 days after the intravenous administration of a citrate complex of the metal].

In experiments with 12 dogs of both sexes it was found that 7 days after intravenous injection of the citrate (2%) complex the concentration of plutonium in the organs and tissues, which are considered noncritical, is lower than in the skeleton by one or two orders of magnitude. No substantial differences were found in plutonium levels in the endocrine glands, (0.7-4.

[Biochemical properties of intramolecularly cross-linked hemoglobin].

The chemical modification of hemoglobin was conducted with the help of bifunctional crosslinking agent--glutaraldehyde. By SDS-polyacrylamide gel electrophoresis and gel-filtration it was shown that the final product contained 70% of modified protein which consisted of non-dissociating hemoglobin dimers and tetramers. It was also shown that the chemical modification didn't produce significant changes in the oxygen-transporting properties of the starting hemoglobin, but had influence on the character of the interaction with the allosteric regulator of reversible oxygenation (pyridoxal-5'-phosphate).

[Changes in the mucous membrane of the trachea and bronchi in dogs based on bronchoscopic data for the combined action of 239Pu and gamma-radiation as compared with the individual actions].

It was established that under conditions of combined exposure of dogs to external gamma- and internal alpha-radiation, a preirradiation with 51.6 mC/kg gamma-rays prevents the development of the signs of endobronchitis which are typical for endobronchitis induced by inhalation of submicron 239Pu dioxide and manifested by hyperemia of trachea and bronchus mucosa, edema, and the presence of mucopurulent exudate.

[Oxygen-dissociation properties and the regulation of the oxygen affinity of a hemoglobin polymer in the bull].

Oxygen-dissociation properties and some aspects of allosteric regulation of bovine hemoglobin (Hb) and its polymerized form (HbP) have been examined. It has been shown that bovine HbP as well as bovine Hb does not require the presence of organic phosphates for normal functioning and has gas transport characteristics which are similar to those of the whole human blood. Pyridoxal-5'-phosphate (PP) works as an allosteric regulator of bovine HbP only in the absence of Cl- ions and vice versa.

[Comparative study of the gas transport characteristics of models of an extraerythrocyte oxygen carrier].

It was shown that coupling of the 2,3-DPH functional analog, pyridoxal-5'-phosphate (PP) to hemoglobin (Hb) and its polymer (HbP) enables one to obtain an artificial oxygen carrier with gas transport characteristics similar to those of freshly prepared donor's blood. Coupling of PP to HB and HbP also intensifies their interaction with other physiologically important ligands (H+ and CO2) and changes the pattern of the relationship of P50 to the hemoprotein concentration in a solution.