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Vol 27, No 9 (2024)

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Pharmaceutical chemistry

Comparative study of the composition And immunotropic properties of heteropoly fractions of the leaves of the Plantago major

Nikiforova E.B., Chudilova G.A., Mizina P.G., Сhapurina V.N., Matveeva A.V., Shevchenko A.I., Bikova O.A.

Abstract

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.

Problems of Biological Medical and Pharmaceutical Chemistry. 2024;27(9):3-9
pages 3-9 views

Secondary metabolites of Cuscuta campestris Yunck

Adzhiakhmetova S.L., Pozdnyakov D.I., Dibizheva N.M., Oganesyan E.T.

Abstract

Introduction. In the North Caucasus Cuscuta campestris Yunck. is widespread, which parasitizes crops, vegetable gardens, and flower beds. The main classes of biologically active substances of parasites of the genus Cuscuta L. are polyphenolic compounds.

The purpose of this work was to study some secondary metabolites of C. campestris stems collected from different host plants.

Material and methods. Objects of study: stems of C. campestris collected in the village. Novkus-Artesian of the Neftekumsky district of the Stavropol Territory with Alhagi pseudalhagi (M. Bieb.) Desv., Beta vulgaris L., Leucanthemum vulgare Lam. The determination of the total content of antioxidants in the analyzed extracts was carried out using a TsvetYauza-01-AA device with amperometric detection. Determination of the total content of phenolic compounds using the Folin-Ciocalteu reagent was carried out by the spectrophotometric method on an SF-102 spectrophotometer.

Results. In the extracts studied, the Shinoda test using magnesium showed a red color due to the formation of anthocyanidins, and a yellow-green color due to the reaction with iron (III) salts. The maximum content of the sum of phenolic compounds and the sum of flavonoids is observed in the extract from the stems of C. campestris, collected from A. pseudalhagi, during extraction with 70% ethyl alcohol and amounts to 10,18±0,47% and 5,71±0,25%, respectively. When determining the total content of antioxidants, the optimal extractant is purified water: the maximum content in the aqueous extract obtained from the stems of C. campestris collected from A. pseudalhagi is, in terms of quercetin and gallic acid, 2,02±0,08 mg/g, 1,31±0,05 mg/g, respectively.

Conclusions. In the analyzed extracts, patterns were revealed between the nature of the extractant, the total content of polyphenolic compounds and host plants. It was found that the extracts obtained by extraction with 70% ethyl alcohol from the stems of C. campestris collected from A. pseudalhagi exhibited the maximum total content of polyphenolic compounds and flavonoids.comparable results were obtained when determining the total content of antioxidants and flavonoids in extracts from the stems of C. campestris collected from B. vulgaris and L. vulgare.

Problems of Biological Medical and Pharmaceutical Chemistry. 2024;27(9):10-18
pages 10-18 views

Effect of solid dispersion method on the solubility of naphthifin hydrochloride

Kosenkova S.I., Krasniuk I.I., Krasniuk I.I., Zubareva I.M., Belyatskaya A.V., Stepanova O.I.

Abstract

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.

Problems of Biological Medical and Pharmaceutical Chemistry. 2024;27(9):19-25
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Preparation of the active pharmaceutical substance "Sodium chlorine E6" in the technology of production of drugs for the treatment of malignant neoplasms using a new type of vegetable raw materials

Pogartseva Y.A., Kauhova I.E.

Abstract

Introduction. Already at the beginning of the twentieth century, it was discovered that a cancer cell is able to accumulate and retain colored substances for a certain time. The raw material for the production of the substance for the above photosensitizer is methylpheophorbide a, which is produced from the biomass of the green microalgae Spirulina Platensis, native to Japan and California. In this regard, there is an urgent question of replacing imported intermediates with more affordable ones. For this purpose, Sosnovsky's hogweed was chosen. Given the presence of cytotoxic properties in hogweed, a promising area of research into the pharmacological properties of extracts from Heraculum Sosnowskyi may be the assessment of their cytostatic activity against tumor cell lines.

The purpose of this study was to obtain and standardize the quality of the active pharmaceutical substance "Sodium chlorine E6" synthesized using a new type of plant raw materials.

Material and methods. Three series of active pharmaceutical substance "Sodium chlorine E6" were obtained from methylpheophorbide a isolated from the dried leaves of borscht Sosnowski (Heracleum Sosnowskyi), prepared in June 2023. The quality indicators of sodium chlorine E6 were determined by the following methods in accordance with the State Pharmacopoeia XIV and XV editions.

The following reagents were used in the synthesis: Acetone C₃H₆O ("HIMMED", Russia), Methanol CH₃OH ("HIMMED", Russia), methylene chlorine CH₂Cl₂ (Scharlau, Spain), Hexane C₆H₁₄ (Sisco Research Laboratories, India), Chloroform CHCl₃ (Sisco Research Laboratories, India), Sodium hydroxide NaOH hç (Pan Reac AppliChem, Spain), Methylpheophorbide A, Hydrochloric acid concentrated HCl (OOO "SIGMA Tek", Russia).

Results. The synthesis of the active pharmaceutical substance "Sodium chlorine E6" from methylpheophorbide a, obtained from the leaves of borscht Sosnowski, was carried out. Standardization of the obtained substance has been carried out. The possibility of using Sosnovsky hogweed as a vegetable raw material for obtaining an intermediate in the production of substances based on E6 chlorine derivatives is evaluated.

Conclusion. In the course of the study, the technology of the active pharmaceutical substance "Sodium chlorine E6" was implemented in the processing of Sosnovsky hogweed. Standardization of the produced substance has been carried out.

Problems of Biological Medical and Pharmaceutical Chemistry. 2024;27(9):26-31
pages 26-31 views

Some plant secondary metabolites as promising candidates for the treatment of lung cancer and pancreatic cancer

Mezhevova I.V., Filippova S.Y., Chembarova T.V., Gnennaya N.V., Zlatnik E.Y., Novikova I.A., Enin Y.S., Burov O.N.

Abstract

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.

Problems of Biological Medical and Pharmaceutical Chemistry. 2024;27(9):32-40
pages 32-40 views

Succinate-receptor system of bone and cartilage tissue in patients with metabolic phenotype of osteoarthritis

Shodiev D.R., Zvyagina V.I., Ryabova M.N., Marsyanova Y.A.

Abstract

Introduction. Melatonin, by inducing the expression of antioxidant enzymes and signaling proteins, enhances the effects in the development of pathological processes occurring against the background of oxidative stress, therefore the stabilization of the protective principles of melatonin is a relevant area of research, allowing us to identify new ways of development and treatment of osteoarthritis.

The aim. To study the effect of melatonin on the succinate receptor system of chondrocytes in osteoarthritis under conditions of oxidative stress in vitro.

Materials and methods. The in vitro study was carried out on chondrocyte cell cultures. Melatonin was added to chondrocytes to obtain final concentrations of 100 μM and 500 μM; and hydrogen peroxide (H₂O₂) – 200 µM. The duration of exposure was 24 hours for melatonin and 12 hours for H₂O₂. Succinate levels and expression of its receptor (SUCNR1) were determined in mitochondria and chondrocyte lysates.

Results. It was found that the addition of H₂O₂ at a dose of 200 μM to the nutrient medium for 12 hours led to a fold increase in the level of succinate and SUCNR1 expression in chondrocyte cells. Pre-incubation of chondrocyte cells with melatonin at concentrations of 100 µM and 500 µM, followed by modeling of oxidative stress (H₂O₂ 200 µM) led to a decrease in the expression of the succinate receptor system.

Conclusion. When H₂O₂ is added to the cellular environment of chondrocytes, high expression of SUCNR1 and an increase in succinate levels are observed. Melatonin treatment limits H₂O₂-induced succinate accumulation and reduces SUCNR1 expression in human chondrocyte cells of the metabolic phenotype of osteoarthritis.

Problems of Biological Medical and Pharmaceutical Chemistry. 2024;27(9):41-49
pages 41-49 views

Biological chemistry

S-nitrosoglutationin as an inducer of nitrosative stress and apoptosis

Suchkova O.N., Abalenikhina Y.V., Shchulkin A.V., Kostyukova E.V., Kochanova P.D., Gadzhieva F.T., Yakusheva E.N., Uzbekov M.G.

Abstract

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.

Problems of Biological Medical and Pharmaceutical Chemistry. 2024;27(9):50-56
pages 50-56 views

Medical chemistry

Assessment of antioxidant, hypoglycemic and hypolypidemic activities of the herbal extract of hill-growing saltwort (Salsola collina)

Korotchenko N.V., Sergun V.P., Ivanov A.A., Burkova V.N., Samoylova Y.G.

Abstract

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.

Problems of Biological Medical and Pharmaceutical Chemistry. 2024;27(9):57-64
pages 57-64 views

Anniversaries and dates

On the 70ₜₕ anniversary of the birth of N.E. Kushlinskii

Problems of Biological Medical and Pharmaceutical Chemistry. 2024;27(9):65-67
pages 65-67 views

On the 100ₜₕ anniversary of the birth of V.M. Mulevich

Problems of Biological Medical and Pharmaceutical Chemistry. 2024;27(9):68-69
pages 68-69 views

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