[Estrogenic and contraceptive activity of 17-R-hydroximino derivatives of 9alpha-hydroxy-11beta-nitroxyestrones]. / Estrogennaia i kontratseptivnaia aktivnost' 17-R-oksiminoproizvodnykh 9alpha-oksi-11beta-nitroksiéstronov.

The estrogenic or uterotropic (UA) and contraceptive (CA) activity of two modified steroids representing 17-R-oximino-9 alpha-oxy-11 beta-nitroxyestrone derivatives (compounds I and II) was experimentally studied by oral administration in female rats in comparison to ethynylestradiol (EED) and mestranol. Compounds I and II showed significant UA (about half that of EED and mestranol) and a pronounced contraceptive effect (exceeding that of mestranol). The dissociation of the drug effects for CA is also indicated by the index of contraception (IC) or the CA/UA ratio. The administration of compounds I and II did not lead to a loss of animals in the acute toxicity tests on female mice.

Glycopeptidolipids--a new class of artificial antigens with carbohydrate determinants. Synthesis of artificial antigen with type-specific oligosaccharide hapten from Neisseria meningitidis group B.

Synthetic lipopeptide N-palmitoyltyrosyl-seryl-seryl-asparaginyl-alanine, an analogue of B-mitogenic tripalmitoyl-pentapeptide from Escherichia coli lipoprotein, was coupled with an oligosaccharide hapten from Neisseria meningitidis lipooligosaccharide to give a glycopeptidolipid conjugate--the artificial antigen of a new type processing the type-specific microbial determinant.

[Isolation and primary characteristics of the common species-specific outer membrane protein of Rickettsia prowazekii]. / Vydelenie i pervichnaia kharakteristika obshchevidovogo belka naruzhnoi membrany Rickettsia prowazekii.

Common species-specific protein is isolated for the first time in the chromatographically pure state from the outer membrane of Rickettsia prowazekii, and its amino acid composition is determined. As revealed by chromatofocusing technique, the protein possesses pI 4.18 +/- 0.03. Three basic ninhydrin-positive compounds, differing from usual amino acids, were discovered in the protein hydrolyzate. Data suggesting the subunit structure of the isolated protein are presented.

[Antigenic polysaccharides of bacteria of the genus Shigella. The structure of the polysaccharide chain of Shigella boydii type 14]. / Antigennye polisakhridy bakterii roda Shigella. Struktura polisakharidnoi tsepi lipopolisakharida Shigella boydii, tip 14.

A specific acidic polysaccharide has been isolated from the Shigella boydii type 14 antigenic lipopolysaccharide after mild hydrolysis followed by chromatography on Sephadex G-50. The polysaccharide consists of the D-glucuronic acid, 2-acetamido-2-deoxy-D-glucose and D-galactose residues in the ratio 1:1:3. From the results of methylation analysis and partial acid hydrolysis, the structure of the repeating unit of the specific polysaccharide was deduced as follows: (-6DGalp alpha 1-4DGlcAp beta 1-6DGalp beta 1-4DGalp beta 1-4DGlcNAcp beta 1-)n. The 13C NMR spectra of native and carboxyl-reduced polysaccharides, as well as of oligosaccharides produced by partial acid hydrolysis fully confirmed the proposed structure. The approach was suggested to determine the type of substitution of uronic acid moieties in polysaccharide chain by use of chromato-mass-spectrometry of acetylated methyl esters of partially methylated aldonic acids. Serological characteristics of Sh. boydii LPS type 14 and its modified derivatives are discussed.

[Molecular nature of the Brucella polysaccharide antigen (poly-B)]. / Molekuliarnaia priroda polisakharidnogo antigena brutsell (poli-B).

Cyclic (1----2)-beta-D-glucan was isolated from killed cells of pathogenic Brucella melitensis 16M. Its structure was deduced mainly from the acid hydrolysis, methylation analysis and 13C-NMR spectroscopy data. The cycloglucan and demicellated lipopolysaccharide of B. melitensis 16M form a stable complex identical, by immunodiffusion test, to the earlier described polysaccharide B antigen.

[Somatic antigens of Shigella and Escherichia coli. Determination of the structure of O-specific polysaccharide from Shigella boydii type 12 and its serological properties compared with the O-specific polysaccharide from Escherichia coli]. / Somaticheskie antigeny Shigella i Escherichia coli. Ustanovlenie stroeniia O-spetsificheskogo polisakharida iz Shigella boydii, tip 12, i izuchenie ego serologicheskikh svoistv v sravnenii s O-spetsificheskim polisakharidom iz Escherichia coli.

The structure of the O-specific polysaccharide of the somatic antigen (lipopolysaccharide) of Shigella boydii, type 12, was established by 1H- and 13C-NMR, methylation analysis and partial acid hydrolysis methods. The polysaccharide consists of pentasaccharide repeating units of the following structure: (formula; see text) The amount of O-acetyl groups was far less than stoichiometric, only about 2 for 3-4 repeating units. Nevertheless, the results of serological studies revealed 3-O-acetyl-alpha-L-rhamnose residue to be the major immunodominant group. In spite of the presence of similar trisaccharide fragments, the lipopolysaccharide and polysaccharide from Shigella boydii type 12 gave no crossreaction with lipopolysaccharide and polysaccharide from Escherichia coli 07. The possible reasons of the absence of serological relatedness between the Sh. boydii, type 12, and E. coli 07 cells were discussed.

[Effect of nutrient medium perfusion on the secretory activity of rat hepatocytes and pancreatic islet cells]. / Vliianie perfuzii pitatel'noi sredoi na sekretornuiu aktivnost' gepatotsitov i ostrovkovykh kletok podzheludochnoi zhelezy krys.

The data are reported on albumin secretion by rat hepatocytes and insulin secretion by pancreatic beta-cells of newborn rats during cell cultivation on flat synthetic membrane in conditions of continuous medium perfusion. Albumin and insulin secretion by the appropriate cultures was higher in continuous medium perfusion than in the control. Enhanced sensitivity of pancreatic beta-cells to glucose, as compared to the control was revealed. It is concluded that continuous medium perfusion of hepatocytes and pancreatic beta-cells in the primary culture had a favourable effect on albumin and insulin secretion by the appropriate cultures.

[Properties of (Ala5, Orn9)-somatostatin. The inhibition of pancreatic and hypophyseal hormone secretion in cell culture]. / Izuchenie svoistv (Ala5, Orn9)-somatostatina. Ingibirovanie sekretsii pankreaticheskikh i gipofizarnykh gormonov v kul'ture kletok.

Ability of Ala5, Orn9-somatostatin to inhibit the secretion of insulin, glucagon, somatotropic hormone (STH) and prolactin was tested on the model of primary monolayer culture of isolated insular pancreatic and adenohypophyseal cells. Chemical substitution performed between positions 5 and 9 in somatostatin molecule failed to change essentially hormone's biologic activity in suppression of insulin and glucagon in the culture of pancreatic insular cells isolated from newborn rats. Somatostatin analog revealed its natural hormonal ability to inhibit STH secretion but failed to affect that of prolactin. The results are suggestive of the principal possibility to produce somatostatin biologically active analog through lyzine residue substitution in position 9 with obligatory simultaneous substitution amino acid residue in position 5.

[Detection of hormonally dependent albumin secretion by primary cultures of rat hepatocytes using an homologous system of radioimmunological analysis]. / Vyiavlenie gormonal'no-zavisimoi sekretsii al'bumina pervichnymi kul'turami gepatotsitov krys s pomoshch'iu gomologichnoi sistemy radioimmunologicheskogo analiza.

A homologous radioimmunoassay to determine rat serum albumin is described in detail. Using this technique one was able to estimate albumin basal secretion by initial rat hepatocyte cultures in a serum-free medium and to detect protein secretion changes caused by various hormones. The stimulating dose-dependent affects of insulin and growth hormone as well as the inhibitory effect of estradiol with regard to albumin production by cultivated hepatocytes were demonstrated. The time of incubation with hepatic cells which was necessary to reach a maximum expression of the effect, was different for various hormones. The preliminary results provide an opportunity to create models for in vitro studies on various dyshormonal states of the body on the basis of a quantitative estimation of hormone-dependent albumin secretion by initial hepatocyte cultures.

[Effect of thyroliberin on pancreatic islet cell function in rats]. / Vliianie tiroliberina na funktsiiu ostrovkovykh kletok podzheludochnoi zhelezy krys.

A study was made of the TRH effect on insulin and glucagon secretory function of a 4-day neonatal rat pancreatic islet cell culture. The TRH effect was determined in the range of 10-1000 ng/ml concentrations within 30 min and 3 h of cell cultivation with the hormone. TRH stimulated insulin and glucagon secretion within the range of the above doses. No dose dependence was revealed in the TRH stimulation of insulin and glucagon secretion. The data obtained suggest that TRH produces an direct effect on islet cell function stimulating insulin and glucagon secretion.

[Function of hormone-secreting cells cultured under continuous perfusion with nutrient medium]. / Funktsiia gormonsekretiruiushchikh kletok, kul'tiviruemykh v usloviiakh nepreryvnoi perfuzii pitatel'noi sredoi.

The data are presented as to prolactin and ACTH secretion by rat adenohypophysis cells and insulin secretion by pancreatic beta-cells of the newborn rats during cell cultivation on flat synthetic membranes with pores differing in diameter under continuous medium perfusion. The cultured cells were discovered to be viable and to possess secretory activity. Secretion of prolactin and ACTH and that of insulin in the appropriate cultures increases in the course of long-term incubation under continuous medium perfusion. It is concluded that application of the porous membranes enables a selective study of the release of one or another hormone into the medium. It is believed that cultivation of hormone-secreting and hormone-susceptible cells under closed- and unclosed-type nutrient medium perfusion is fairly promising.

[Procedure for producing a monolayer primary culture af rat hepatocytes and evaluation of its functional activity]. / Sposob polucheniia monosloinoi pervichnoi kul'tury gepatotsitov krys i otsenka ee funktsional'noi aktivnosti.

A simple method for isolating hepatocytes from the liver with the aid of trypsin and their cultivation is described. The functional activity of the primary monolayer culture of hepatocytes was evaluated from the rate of albumin synthesis and secretion. The basal rate of albumin synthesis was fairly high during the first 10 minutes but after 2 hours decreased and reached plateau. On the contrary, the basal rate of albumin secretion rose with time and after 2 hours attained the rate of albumin synthesis. Human growth hormone (500 ng/ml) stimulated albumin output within 3 hours of incubation with hormonal stimulation in the cells from hypophysectomized rats being more pronounced as compared to that seen in hepatocytes from intact animals. A conclusion is made that the hepatocyte culture prepared by the method described can produce a release albumin and retains sensitivity to the hormonal regulator.

[Effect of growth hormone on polynucleotide phosphorylase activity in a primary monolayer culture of rat hepatocytes]. / Vliianie gormona rosta na aktivnost' polinukleotidfosforilazy v pervichnoi monosloinoi kul'ture gepatotsitov krys.

Growth hormone (1 microgram/ml) inoculated into the primary culture of rat hepatocytes and incubated for 3 hours at 37 degrees C decreases 2-fold the activity of polynucleotide phosphorylase (PNPase). In the culture of hepatocytes from hypophysectomized rats, the basal activity of PNPase is significantly higher as compared with that in the culture of hepatocytes from intact animals. The most pronounced inhibitory effect of growth hormone on PNPase was seen in the culture of hepatocytes from hypophysectomized animals.

[Biological properties of synthetic somatostatin]. / Issledovanie biologicheskikh svoistv sinteticheskogo somatostatina.

Complex work on the assessment of biological properties of somatostatin synthesized according to a new original method was carried out. Its inhibitory action on the TTH, growth hormone and insulin secretion was demonstrated in vivo and in vitro. As a rule, somatostatin effect was expressed against the background of stimulated hormone secretion, although basal secretion inhibition was observed with respect to insulin, The inhibitory action of somatostatin on the hormonal secretion was direct, not mediated through any regulating factors.

[Functional activity of rat adenohypophysis cells in a primary monolayer culture and the effect of several regulators on it]. / Funktsional'naia aktivnost' kletok adenogipofiza krys v pervichnoi monosloinoi kul'ture i vliianie na nee nekotorykh reguliatorov.

Some peculiarities of labeled growth hormone (GH) and prolactin (PL) secretion in the 5-day monolayer culture of the rat adenohypophysis was studied. The hormones from the culture medium were obtained by electrophoresis on polyacrylamide gel. Natrium-dibutyril of cyclic adenosine-3',5'-monophosphate and theophylline, stimulated the GH and PL secretion. Thyrotropin-releasing hormone (TRH) increased the incorporation of 14C-1-leucine into the cell protein, stimulated PL secretion, but did not act on the GH release. Somatostatin completely abolished the GH secretion mediated by theophyllin, but not that of PL. Some peculiarities in the formation of labeled GH and PL pool in the cells and secretion of these hormones into the culture medium are discussed.

[The functional activity of rat fetus adrenal cortex in monolayer tissue culture]. / Issledovanie funktsional'noi aktivnosti kory nadpochechnikov plodov krys v monosloinoi kul'ture tkani

A study was made of the functional activity of the adrenal cortex in 15 1/2-, 18 1/2-, and 21 1/2-day rat fetuses and neonates. Adrenal tissue was incubated after its preliminary trypsinization at 37 degrees C for over 2 weeks with and without ACTH addition into the culture medium, in the amount of 0.1 U/ml. The corticosterone level was determined in the culture medium fluorimetrically. The activity of 3 beta-oxysteroid dehydrogenase was determined histochemically. Corticosterone was revealed in the culture medium. The activity of 3 beta-oxysteroid dehydrogenase was found in the cells of the cultivated adrenal glands. Addition of ACTH into the culture medium considerably increased the corticosterone level and elevated the activity of 3 beta-oxysteroid dehydrogenase. It can be considered on the basis of the aforesaid that cells of the primary culture of the adrenal cortex of rat fetuses aged 15 1/2-, 18 1/2-, and 21 1/2-days and of neonates could form, in the process of incubation, corticosterone from the endogenous substrates in the course of 11, 16, 8 and 13 cultivation days, respectively. The presence of ACTH in the culture medium for the adrenal glands of rat fetuses (of all the gestation periods under study) and of neonates intensified the steroidogenesis.