Svetlana A. Luzhnova

According to WHO data, cardiovascular diseases occupy a leading position in terms of the number per share of the population, both in Russia and in other countries. A prerequisite for the development of these pathologies is atherosclerosis. It is now recognized that drug therapy is leading in curbing the development of atherosclerosis and subsequent complications. In this regard, the urgency of the search for new lipid-lowering drugs aimed at the treatment of this disease is increasing. Recent studies have shown the promise of using the benzothiophene backbone for the synthesis of new effective drugs, since this core has various biological and pharmacological activities, which makes it possible to obtain effective antimicrobial, anticancer, anti-inflammatory, antioxidant, anti-tuberculosis, antidiabetic, anticonvulsant and other drugs on its basis.The purpose of this study was to study the lipid-lowering effect of the azomethine derivative 2-amino-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide, a substance under the laboratory code BF-10, on some indicators of lipid metabolism in healthy rats and under pathological conditions with experimental hyperlipidemia. Atorvastatin was chosen as the reference drug. Determination of biochemical parameters of lipid metabolism in the blood serum and in the liver homogenate (the content of cholesterol, triglycerides, total lipids, LDL, VLDL and HDL) was determined by unified biochemical methods using standard Olvex Diagnosticum kits on a Dixion Torus 120 analyzer. Based on the analysis of the obtained data on the effect of the BF-10 substance on lipid metabolism, it can be concluded that they are comparable with the action of the highly effective reference drug atorvastatin, which allows us to expand information on the spectrum of biological activity of azomethine derivatives and consider the compound under the laboratory code BF-10 promising for further development.

One of the ways to solve the problem of drug resistance in the therapy of infectious diseases is to develop herbal preparations with high antibacterial activity, which have a good drug safety profile, is extremely significant for long-term therapy, the use of which could complement and improve the used combination therapy regimens. The aim of our study was to study the anti-leprosy activity of lofant anise extract obtained by supercritical fluid extraction using CO2 containing phenolic compounds such as gallic acid, coumarin, umbelliferon, luteolin, quercetin, taxifolin, rutin. Materials and methods. The anti-leprosy activity had been studied on Shepard's model. Blood parameters were examined on a SYSMEX XT – 2000i hematological analyzer (Japan). Conclusion. Lofant anise extract, obtained by supercritical fluid extraction using CO2, has a bacteriostatic effect on M. leprae, which is not only comparable to the effect of dapsone, but also with a more prolonged course exceeding it. Unlike the drug of choice (dapsone), the extract, when administered for 30 days, does not cause changes in red blood parameters and does not cause neutropenia. The identified effects actualize further research of the extract for the development of dosage forms based on it for practical health care.

The effects of triphenylantimony(V) catecholate Ph₃Sb(Cat) (1) and its spiroendoperoxide Ph₃Sb(L‐O₂) (2) (Cat = 3,6‐di‐tert‐butyl‐4,5‐dimethoxycatecholate) on lipid peroxidation (LP) in vitro and in vivo were examined in BALB/c line mice. A comparative study of the impact of compounds 1 and 2 on LP under similar conditions was made by measuring the formation of thiobarbituric acid reactive substances (TBARS). The anti‐ or pro‐oxidant action of complexes 1 and 2 may be caused by the different redox level of the ligand acting as radical scavenger and/or by the bound molecular oxygen promoting the oxidation process. Biological experiments (in vitro and in vivo) were performed using mouse tissue homogenates. Decreasing TBARS concentration was observed in all examined tissues and blood serum (in vitro as well as in vivo) for catecholate 1. These results indicate inhibition of LP in the presence of complex 1. In contrast to 1, spiroendoperoxide 2 increases the level of TBARS in tissue homogenates. Minor fluctuations of TBARS concentration in erythrocytes and in blood serum indicate the absence of an obvious anti/pro‐oxidant influence of 2 on the LP process in vivo. The role of catecholate fragment was found to be essential in explaining antioxidant properties. Copyright © 2014 John Wiley & Sons, Ltd.

In Wistar rats, psycho-immune-modulating properties of phenotropyl succinate were studied under conditions of informational-physical stress. The effect ofphenotropyl succinate on the organism specific and unspecific resistance was studied. The data obtained indicate the phenotropyl succinate ability to release neuroimmune disturbances developing under conditions of informational-physical stress.

Behaviour and immune responses of rats and mice following cyclophosphamide administration were investigated. The psycho-immunomodulating effect of the GABAergic compounds was revealed. Phenibut (25 mg/kg) and Baclophen (10 mg/kg) restored functional activity of immune system and corrected disturbances of the behavioural responses. The GABAergic agents restored horizontal and direction investigation activities in the rats and mice, decreased grooming and increased number of passages through central zones in the "Suok" test.