Vol 27, No 9 (2024)

Relevance. The leaves of the Plantago major are a pharmacopeic medicinal plant raw materials, quite well studied in relation to the chemical composition and spectrum of medical use, but the list of drugs based on them today is limited. In this regard, it seemed to be relevant to study the possibility of developing a drug in the form of a medicinal pencil containing an extraction complex of Plantago major leaves, enriched with flavonoids. To solve this problem, it was necessary to choose an extragent that selectively extracts the biologically active substances of the Plantago major leaves, with a predominance of flavonoids.

The aim of the work was a comparative study of the chemical composition and immunotropic effects of the in vitro heteropoly fractions of the leaves of the Plantago major leaves.

Material and methods. The object of research was the leaves of the Plantago major. The content of extractive substances in the raw materials was determined by the pharmacopeic method of single extraction using extractants of various polarity: purified water, 40 %, 70 % and 95 % of ethyl alcohol. The content of the amount of flavonoids in extracts in terms of cinaroside was carried out by differential spectrophotomeria. Heteropoly fractions were obtained by the method of reperculation in a battery from 3 laboratory percolators with subsequent condensation and drying. The assessment of the phagocytic and microbicidal function of neutrophilic granulocytes carried out in vitro on the samples of peripheral blood of conditionally fast-ash persons.

Results. It was revealed that the content of extractive substances was reduced with a decrease in the polarity of the extractant, while the content of the extracted amount of flavonoids increased. comparative immunological studies included the extracts of Plantago major leaves, obtained with the use of 70 % and 95 % of ethyl alcohol. An analysis of their immunotropic effects showed that the fraction extracted by 70% alcohol, statistically significantly increased the indicators of the phagocytic number, phagocytic index and the relative number of neutrophilic granulocytes that absorb bacteria. In addition, in its presence, the digestive ability of neutrophilic granulocytes and the digestion index relative to indicators of the control group increased, the activity of NADPH-oxidase and the number of formsan-positive neutrophil granulocytes increased.

Conclusions. A comparative assessment of the effect of heteropoly fractions of Plantago major leaves on the phagocytic and microbicidal functions of neutrophilic granulocytes showed that the most pronounced positive immunotropic effect was demonstrated by the fraction extracted with 70% ethanol.

Introduction. Naphthyphine hydrochloride is an antifungal and antibacterial drug; a representative of the chemical group of allylamins. The widespread use of Naphthyphine hydrochloride is limited by its low solubility in water, which causes technological difficulties in the production of drugs based on it, and low bioavailability indicators. To increase solubility and increase the release of most active substances from a number of solid and soft dosage forms, the modern method of obtaining their solid dispersions can be used successfully.

Objective. Study the effect of the solid dispersion method obtained using polyvinylpyrrolidone with a molar mass of 10000 g/mol (PVP-10000) on the solubility of Naphthyphine hydrochloride.

Material and methods. A substance of Naphthyphine hydrochloride was used. PVP-10000 was used as a solid dispersion carrier. The solid dispersion of Naphthyphinе hydrochloride with PVP-10000 was obtained with the help of the solvent removal method.

Results. It has been found that the production of solid dispersions increases the solubility and the rate of dissolving of Naphthyphine hydrochloride. The solubility of Naphthyphine hydrochloride from solid dispersion is increased by 2. 2 times compared to the original substance. The combination of physico-chemical analysis methods, such as UV spectroscopy and microcrystalloscopy, makes it highly likely to suggest that the observed increase in the solubility of Naphthyphine hydrochloride from the tested solid dispersions is due to the loss of the active substance's crystallinity and the transition of the effective substance into the solid state in the PVP-10000 matrix, and is also due to solubilization under the action of the polymer, resulting in the formation of the colloidal solutions of Naphthythine hydochloride when dissolved in the water itself of the dispersion.

Conclusion. Obtaining solid dispersions with PVP-10000 improves the water solubility of Naphthyphine hydrochloride. The authors plan to use the results presented in the article in the further development of the composition and technology of rapidly soluble solid forms of Naphthypine hydrochloride tablets and granules, having accelerated (less than 5 minutes) the release of the active substance and increased bioavailability. This will help to approach the treatment of fungal infections in a comprehensive way.

Introdution. Cancer is the second leading cause of death in Russia and the world after cardiovascular diseases. Chemotherapy remains the main line of treatment, but tumor cells can become resistant to drugs. Researchers are working on new effective drugs, including secondary metabolites of plants that have antitumor effects through various mechanisms.

The aim of this study was to investigate the cytotoxic properties of three compounds: alkaloid P1, terpenoid P2, and flavonoid V1 against pancreatic cancer cell line AsPC-1 and non-small cell lung cancer H1299.

Material and methods. Secondary metabolites of Petasites hybrydicus (L.) G. Gaertn., B. Mey. & Scherb. and Viscum album L. were extracted using tetrachloroethylene. For identification of the isolated compounds, high-performance liquid chromatography with mass detection and nuclear magnetic resonance method were used. Non-small cell lung cancer cell line H1299 and pancreatic cancer AsPC-1 were grown in RPMI1640 medium (Gibco, USA) supplemented with 10% FBS (HyClone, USA) and 1% glutamine (Biolot, Russia) under standard conditions. Cell sensitivity to the studied compounds was determined by MTT test.

Results. All three compounds demonstrated antitumor activity against the studied cell lines. Compound V1 increased signs of mesenchymal cells morphology and apoptosis, with IC₅₀ values of 234. 24±21. 56 μM (AsPC-1) and 565. 62±84. 31 μM (H1299). Compound P1 promoted multinucleated cell formation in H1299 culture. Half-inhibitory doses for P1 were 652. 54±56. 12 μM (AsPC-1) and 157. 85±48. 62 μM (H1299). Compound P2 induces cell apoptosis and necrosis and probably affects membrane rigidity. The IC₅₀ values for P2 were 802. 34±121. 02 μM (AsPC-1) and 415. 71±75. 05 μM (H1299).

Conclusions. These compounds can be considered promising antitumor agents for lung cancer and pancreatic cancer.

Introduction. S-nitrosoglutathione is an S-nitrosylated derivative of glutathione and is considered an important mediator of the signaling effects of nitric oxide (II). In turn, nitric oxide can exhibit both regulatory and toxic effects due to the formation of active forms of nitrogen and nitrosylation of intracellular components, which can lead to the development of apoptosis. The role of nitric oxide in the regulation of apoptosis is dual, and therefore requires further study.

The aim of the work was to study the possibility of the development of nitrosative stress and apoptosis under the action of the NO donor – S-nitrosoglutathione.

Material and methods. The study was performed on a HepG2 cell culture. S-nitrosoglutathione was added to the cells at concentrations of 1, 10, 50, 100 μМ and incubated for 3 and 24 hours. Water (S-nitrosoglutathione solvent) was added to the control cells in an equivalent volume. Photometric methods were used to determine cell viability (MTT test), the concentration of nitric oxide and peroxynitrite metabolites. Expression of 3-nitrothyrosine, Bcl2 and Fas were detected by Western blot.

Results. S-nitrosoglutathione at a concentration of 100 μМ (24 h) decreased cell viability and increased concentration of peroxynitrite. The level of nitric oxide metabolites increased under the action of S-nitrosoglutathione at concentrations of 1–100 μМ and exposure periods of 3 and 24 hours, which led to an increase the expression of 3-nitrothyrosine. S-nitrosoglutathione with incubation for 3 hours and concentrations of 1–50 μM increased the level of Bcl2, at concentrations of 50–100 μM it decreased the content of Fas; when incubated for 24 hours and concentrations of 1-100 µM it decreased the level of Bcl2 and Fas.

Conclusion. Thus, in this study, it was found that S-nitrosoglutathione at concentrations of 1–50 μM and an exposure period of 3 hours has a signaling effect in HepG2 cells. S-nitrosoglutathione at a concentration of 100 μМ during incubation of 3 and 24 hours causes the development of nitrosative stress, which leads to the development of apoptosis and decreased cell viability.

Introduction. The development of safe and effective natural antioxidant drugs is an important task in the prevention and treatment of cardiovascular diseases, which are a serious public health problem.

Work Objective is a study of the antioxidant, hypoglycemic and hypolipidemic activities of the herbal extract of hill-growing saltwort (Salsola collina) in comparison with the effect of a standard antioxidant agent.

Material and methods. The object of the study was a "Hepatosol" biologically active food supplement based on a dry concentrated aqueous extract of the Salsola collina herb in capsules.

The patients under observation were matched groups of obese women and men of comparable age with risk factors for cardiovascular diseases. During the study, tolerability and possible adverse events were recorded and vital signs were monitored. The results of a biochemical blood test, lipid profile, oxidative stress and body composition analysis of patients were also evaluated and interpreted.

Results. It has been found out that the parameters of the lipid profile and antioxidant status in patients with obesity and a risk of cardiovascular complications taking the herbal extract of hill-growing saltwort for 3 months returned to normal. A hypoglycemic positive effect of the herbal extract of hill-growing saltwort on reducing the body weight of patients has been recorded. The safety and good tolerability of the study drug have been confirmed.

Conclusions. The results of studies show that a biologically active food supplement "Hepatosol" based on the extract of the Salsola collina herb has antioxidant, hypoglycemic and hypolipidemic activities. Due to these properties, the drugs based on a dry concentrated aqueous extract of the Salsola collina herb are favorable for diet therapy of patients with diabetes mellitus, for weight loss and use in the prevention and complex therapy of cardiovascular diseases.