Pleiotropic effect of thyroid hormones on gene expression in fish as exemplified from the blue bream Ballerus ballerus (Cyprinidae): Results of transcriptomic analysis.

A pronounced pleiotropic effect of thyroid hormones on the regulation of gene expression in fish in postembryogenesis was demonstrated for the first time using larvae and juveniles of the blue bream Ballerus ballerus as an example. Genome-wide transcriptome sequencing (RNA-seq) identified 1212 differentially expressed genes in the brain and liver of fish kept in triiodothyronine solution (0.25 ng/mL). Our data show that the regulation of gene expression by thyroid hormones is widespread in nature: it involves not only the structural genes but also the regulatory genes. A significant number of genes under the control of thyroid hormones are involved in the determination of morphological traits.

[The etiopathogenetic aspects of sensorineural impairment of hearing].

The author presents a review of the Russian- and foreign-language literature concerning etiology and pathogenesis of sensorineural hearing impairment with the opinions of domestic and foreign researches on this issue.

Application of the Dynamic Gastric Model to evaluate the effect of food on the drug release characteristics of a hydrophilic matrix formulation.

Characterisation of the effect of food on the bio-performance of modified and extended release dosage forms can be very challenging due to the need to replicate the dynamic biochemical conditions of the human gut as well as the complex physical processing modalities under fed state. Classical compendial methods are useful for testing the quality of pharmaceutical dosage forms but typically have limitations in the accurate prediction of food-effect in-vivo. Preliminary evaluation of the Dynamic Gastric Model (DGM) shows that it can provide substantially more detailed mechanistic information on dosage form properties compared to conventional compendial testing. The potential effect of food on the drug release and physical properties of a hydrophilic matrix formulation containing a model drug, hydrochlorothiazide, was studied using compendial methods, bio-relevant media and the DGM (in combination with an off-line intestinal model). Whilst the compendial methods with biorelevant media provided good correlation with the dissolution rates observed using the DGM/intestinal model under simulated fasted state, the quantification of simulated fed state performance changes was much more challenging using the compendial methods. Classical compendial studies using biorelevant FeSSIF and FaSSIF media could not readily discern differences in dissolution performance under fasted and fed states; however, the DGM could detect significant changes in both physical properties as well as drug release performance under fed state processing.

[A novel enzyme immunoassay system for the detection of HIV-1 p24 antigen with a sensitivity of 0.5 pg/ml].

A "DS-EIA-HIV-AG-Screen" enzyme immunoassay system has been devised to detect HIV-1 p24 antigen with a sensitivity of 0.5 pg/ml the use of which permits reduction of a seronegative window phase as compared with the tests showing a lower sensitivity threshold. The "DS-EIA-HIV-AG-Screen" system developed may be used to screen donor blood and to examine risk-group individuals for the early diagnosis of HIV infection.

[Comparative study of the effect of Ladasten, Sydnocarb and their combination on physical work ability of laboratory animals].

The action of Ladasten, Sydnocarb and their combination used at doses of 10 and 20 mg/kg, produce on working ability of mice was evaluated in the swimming test. It was shown that single doses of tested drugs as compared to their combination produce more pronounced and prolonged positive action on physical work ability of animals used in the experiments.

[Thermoprotector properties of a combination of sydnocarb with ladasten].

Thermoprotector properties of a 1 : 1 combination of sydnocarb and ladasten (both in a dose of 10 or 20 mg/kg) along with its effect on the hemodynamics and respiration in experimental animals were studied. The combination of sydnocarb (20 mg/kg) and ladasten (20 mg/kg) produced a significant thermoprotector effect, enhanced the regional and local cerebral flow, and increased the respiration rate.

Psychotropic effects of sidnocarb and ladasten in inbred mice with different reaction to emotional stress.

Dose-dependent relationship of the effects of sidnocarb and Ladasten on open field behavior and free motor activity was studied in inbred C57Bl/6 and BALB/c mice differing by emotional stress reaction phenotype. Ladasten in a dose of 10 mg/kg produced activating and anxiolytic effects on BALB/c mice in the open field test. Combined injection of Ladasten (10 mg/kg) and sidnocarb (6 or 12 mg/kg) activated animal behavior in both tests.

The effect of ultrasonic vibration on the compaction characteristics of paracetamol.

An ultrasonic (US) compaction rig has been developed that is capable of providing compaction pressure together with high-power ultrasonic vibrations of 20 kHz to a powder or granular material in a die. The rig has been used to investigate the effect of US on the compaction properties of paracetamol, a drug that produces tablets that are weak and frequently exhibit capping. It was found that coherent paracetamol tablets could be prepared by US-assisted compaction at pressures as low as 20 to 30 MPa. Application of US before and after compaction was not found to be as effective as US applied during compaction. The breaking forces of the tablets produced with US applied during compaction were found to be consistently significantly higher than when compaction was performed conventionally or with US applied before or after compaction. The application of US during compaction made it possible to increase tablet breaking force, typically by a factor of 2 to 5. It was concluded that pressure should be applied together with US to achieve a better acoustical contact, which is required to transmit vibrations from the horn to the material and also to bond the surfaces of the particles. US application during compaction also resulted in an increase in apparent density, in relation to the apparent density of conventionally prepared paracetamol tablets, of up to 12.8%. US appears to improve particle rearrangement and provide energy for partial melting of particle asperities and subsequent fusion of particle surfaces, thus increasing interparticulate bonding. Development of solid bridges between the particles during US-assisted compaction was observed on scanning electron photomicrographs. Solid bridge formation was thought to result in a reduction of void space, which in turn reduced the rate of water penetration into the compacts and consequently increased tablet disintegration and drug dissolution times. It was found that the results of US-assisted compaction are influenced by formulation and US time. An increase in binder (polyvinylpyrrolidone) concentration and/or US time resulted in a significant increase in the breaking forces of paracetamol tablets produced with US. When paracetamol was mixed with a second material, such as dicalcium phosphate dihydrate and microcrystalline cellulose, stronger compacts were prepared by US-assisted compaction compared with the tablets containing no filler. Positive interactions were considered to have occurred as a result of US-induced bonding between the two materials. Overall, the application of US was found to significantly improve the compaction properties of paracetamol.

Principles and application of ultrasound in pharmaceutical powder compression.

The use of ultrasound during the tableting of pharmaceutical powders is a new concept. However, in the metallurgy, plastic, and ceramic industries, ultrasound-assisted compression of materials has been known for some years. Ultrasound improves the characteristics of the compression process leading to optimized mechanical strength of the compacts without applying excessive compression force. Therefore, problems associated with high-pressure compression in tableting can be overcome and tablets may be manufactured more economically and consistently with the aid of ultrasound compared to conventional pressure processes. Although great progress in the theoretical understanding of the ultrasound-assisted powder compression process has been made since the late 1960s, the need for further research in the area of ultrasound application during pharmaceutical powder compression is essential. Further investigations on a wide range of drugs and excipients, to expand the usefulness and scope of the ultrasound-assisted technique, and to understand the complex phenomena involved in the process, are needed. In this article the principles, advantages, and limitations of the application of ultrasonic vibrations during pharmaceutical powder compression is reviewed with the hope that this article can contribute to, and stimulate research in the area.

[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.

[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.

[The systemic-functional analysis of the principles of organization of vertebrate behavior]. / Sistemno-funktsional'nyi analiz printsipov organizatsii povedeniia pozvonochnykh.

The classification of systemic principles in animals' behaviour organization is revealed and based by means of functional triad method. The methodical basis for structure and function relationship in behaviour formation is given.

[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.

[Adaptive reactions of algal populations to exposure to toxic substances]. / Adaptivnye reaktsii populiatsii vodoroslei na vozdeistvie toksicheskikh veshchestv.

The adaptative reactions of alga populations to the toxic effect have been investigated by the functional triad method. The role of phenotypic and genotypic adaptation and the dynamics of their correlation during the alga adaptation to the toxic media has been revealed.

[Pigmentation of the outer cornea after removal of the eye from Rana lessonae Camerano larvae]. / Pigmentatsiia naruzhnoi rogovitsy posle udaleniia glaza u lichinok Rana lessonae Camerano.

Dynamics and morphological peculiarities of pigmentation in the external cornea after removal of the eye in larvae of Rana lessonae Camerano have been studied in situ depending on the developmental stage during prometamorphosis. The results are compared with the previously obtained data for tadpoles of Rana temporaria (D. V. Popov, Sokolova Z. A., Kalistratova E. N. et al., 1982). The process of pigmentation in the cornea does not depend on the developmental stage, proceeds with a constant rate and accomplishes before the beginning of the metamorphous climax. In the Rana lessonae tadpoles the dermal chromatomorphous units differentiate earlier than in the Rana temporaria larvae. The period of metamorphosis in the R. lessonae is 2 times as long as in the R. temporaria. At the same time, transplantation of the epidermal melanophores during the process of the cornea pigmentation in these species is realized with the same rate. Thus, in this case, the phenomena occurring at the cellular and organism levels are rather autonomous. The differences revealed between the cornea pigmentation in the R. lessonae and R. temporaria larvae are explained as the phenomenon of interlevel heterochrony in ontogenesis.