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卷 28, 编号 5 (2025)
Articles
Using squalene to develop effective medicines
摘要
Squalene is a natural organic compound obtained from various sources, for example, deep-sea shark liver oil, vegetable raw materials and oils. It is contained in the human body, being a precursor for the cholesterol synthesis, as well as in plants, being an intermediate in the synthesis of sterols, which are important for maintaining the cell membranes. Recently, the significant raise of interest in relation to this compound has been shown due to its properties and various ways of utilization in medicine.
This article summarizes the numerous features of squalene, examines the potential manners of using squalene as the component of effective medicines.
One of the main advantages of squalene is its antioxidant properties, which help to protect the cells from damage caused by reactive oxygen species, which plays a significant role in the prevention of various diseases, including cardiovascular and oncological ones. In addition, squalene is able to reduce inflammation in the organism because it has an influence on the inflammatory reactions. Its moisturizing properties make it to be a promising component for dermatological medications, squalene is used to treat skin diseases such as eczema and psoriasis, it helps to alleviate symptoms and restore the protective skin functions. Some studies have examined the potential of squalene as an immunostimulant that helps the organism struggle infections and inflammation more effectively. In addition to this, squalene possesses antibacterial properties, which has been demonstrated by several types of microorganisms in various works.
Nowadays, squalene is commercially used only as an adjuvant for vaccines and as an active component for some cosmetic products, however, the prospects for its use as a substance for antitumor medicines are carefully studied, also squalene can be the constituent of the delivering systems for active substances and it can be considered as an excipient ingredient for increasing bioavailability in preparations for topical and external application.
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Modern possibilities of using Chamerion Angustifolium L. (review)
摘要
In recent years, there has been an increasing interest in the utilization of plants, particularly medicinal plants, for purposes beyond merely treating and preventing diseases. These plants are also being used to supplement daily diets and correct dietary habits in order to enhance overall human health.
The aim of this study is to review and synthesize the available literature on the research into the use of Chamerion angustifolium L. and to explore the current possibilities for its application in different industries, including the food and pharmaceutical sectors.
The paper discusses the research and utilization of Chamerion angustifolium, commonly known as willowherb (fireweed), as a potential food crop and valuable medicinal plant. The study examines the possibilities of utilizing both processed and unprocessed forms of this plant, highlighting the benefits of using both native and fermented materials. The paper identifies the various industries in which fireweed can be utilized, including pharmaceutical, food processing, and agriculture. It also analyzes domestic and international literature sources, drawing on publicly available data to discuss the biological characteristics, chemical composition, and methods of utilization of Chamerion angustifolium. In preparing the paper, the authors utilized several electronic databases, including PubMed, e-Library, Cyberleninka, and the Google Scholar search engine, to ensure the accuracy and relevance of their findings.
Currently, fermented willowherb tea is most commonly used as a replacement for traditional tea. To produce a high-quality product, it is essential to define and standardize key stages, including raw material preparation, fermentation, and post-fermentation processing. The parameters for the fermentation process have been determined, and the main and supplementary stages required for product production have been identified. The available techniques for raw material fermentation and the characteristics of post-fermentation treatments have been analyzed, and the impact of the final stages on product quality has been assessed. The advantages and drawbacks of the fermentation method have been considered in relation to the organoleptic properties of the products and the concentration of biologically active compounds in the resulting aqueous extracts. Examples of the practical application of Chamerion angustifolium in the production of nutraceuticals and potential uses of willowherb as a pharmaceutical raw material are provided.
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Improvement of methods for standardization of styphnolobium japonicum fruits
摘要
Introduction. The search for natural sources of active compounds and the development of effective and safe drugs for the prevention and treatment of various diseases is one of the priority areas for the development of the pharmaceutical industry.
A promising object of research is the Styphnolobium japonicum fruits. Currently, due to the receipt of new data on the chemical composition of this raw material, new opportunities are opening up in its use for obtaining various substances and their practical application, as a means of correcting metabolic disorders during menopause, as well as neuroprotective drugs. This circumstance requires a revision of the quality requirements for the fruits of Styphnolobium japonicum.
Objective of the work – Clarification of the description of raw materials, diagnostic elements of the anatomical structure, norms of numerical indicators, as well as the development of a method for quantitative determination of the content of active substances for the preparation of a new edition of the pharmacopoeial article.
Material and methods. The object of the study was dried Styphnolobium japonicum fruits, harvested in 2016-2021 in the Republic of Crimea. The following equipment was used in the work: biological microscope BIO 2 LED (Altami, Russia); spectrophotometer UV-1800 (Shimadzu, Japan); HPLC-UV Prominence-i LC-2030C 3D (Shimadzu, Japan); HPLC-UV-MS/MS LCMC-8040 (Shimadzu, Japan).
Results. The results of the study of medicinal plant materials – Styphnolobium japonicum fruits are presented. The criteria of authenticity (morphological and anatomical and diagnostic features) and quality indicators (nomenclature of numerical indicators) of this type of raw material have been clarified. To confirm the authenticity of the raw materials, a thin-layer chromatography (TLC) technique has been developed. A technique for quantitative determination of the content of active substances has been developed. The proposed quality criteria are included in the new edition of the pharmacopoeial monograph.
Conclusions. As a result of the conducted studies, the diagnostic features of the raw materials were identified and supplemented, a method for confirming authenticity by TLC with a standard sample of sophoricoside was developed, and a nomenclature of numerical indicators and their norms was determined. For the quantitative assessment of biologically active substances, a method for determining the amount of phenolic compounds in terms of genistein was developed and validated.
Based on the data obtained, a pharmacopoeial monograph «Styphnolobium japonicum fruits» FS.2.5.0130 was developed and approved, which is included in the State Pharmacopoeia of the Russian Federation, XV edition.
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Validation of the methods of quantitative analysis of ascorbic acid and rutoside in chewing lozenges
摘要
Introduction. Chewable lozenges are a relatively new dosage form with advantages such as ease of use, high bioavailability of active ingredients and the ability to control dosage. The development of new compositions with vitamins and vitamin-like substances is an urgent task, for which it is necessary to have validated methods for analyzing their quality. For the composition of lozenges with ascorbic acid and rutoside, titrimetric methods and spectrophotometry have been proposed.
The purpose of the work is to validate methods for the quantitative determination of ascorbic acid and rutoside in chewable lozenges intended for use as therapeutic and preventive vitamin products.
Material and methods. The developed methods for the quantitative determination of ascorbic acid and rutoside in chewing lozenges were validated according to the following indicators: specificity, linearity, analytical range, accuracy and precision (repeatability and intra-laboratory precision) in accordance with the requirements of the GPM.1.1.0012 "Validation of analytical methods" of the State Pharmacopoeia of the Russian Federation XV edition.
Results. Based on the conducted validation, it was confirmed that all applied methods meet the necessary acceptance criteria, which guarantees the reliability and accuracy of the results of quantitative determination of ascorbic acid and rutoside in chewable lozenges.
Conclusions. As a result of the conducted research, it was found that the spectrophotometric determination of rutoside in chewing lozenges is optimally carried out at a wavelength of 360 nm; ascorbic acid by iodometry (basic) and iodometry (alternative). The obtained data will be used in the development of regulatory documentation for the vitamin product.
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Influence of a new biostimulant and hydrothermal conditions on the dynamics of phyloquinone accumulation in leaves of Urtica Dioica L.
摘要
Introduction. In connection with the development of agricultural and medicinal plant growing, the search for effective biostimulants is relevant. The results of long-term research by the authors showed that the product of paracetamol biodegradation, obtained from paracetamol waste by biotechnological means, is an active stimulator of plant growth and an inducer of accumulation of biologically active substances in them.
The aim of this study is to investigate the effect of paracetamol biodegradation product and hydrothermal conditions of vegetation periods of different years on the dynamics of phylloquinone (vitamin K1) accumulation in leaves of Urtica dioica L.
Material and methods. The work used the biodegradation product of paracetamol as a biostimulator, and the plant growth stimulator drug "Zircon" as a reference when conducting field experiments in places of natural growth of nettles in the Perm Territory in 2022 and 2023. In the plant raw materials collected from the experimental and control sites at the beginning and end of the vegetation phase, the phylloquinone content was determined by high-performance liquid chromatography. The hydrothermal coefficient was used to assess the effect of hydrothermal conditions of the growing season on the accumulation of phylloquinone.
Results. Under the influence of the biostimulator used in the work, the phylloquinone content in nettle leaves at the beginning of the 2022 vegetation phase increased by 12.0% compared to the control, by 26.6% at the end of the phase, and by 2.6% and 9.1%, respectively, when treated with Zircon. The increase in phylloquinone content at the beginning and at the end of the 2023 vegetation phase under the influence of PBP was 1.5% and 6.5%, and when treated with Zircon – 0.4% and 0.6%, respectively. More favorable hydrothermal conditions compared to 2023 contributed to greater accumulation of phylloquinone in the control and experimental samples of 2022.
Conclusion. The product of paracetamol biodegradation showed properties of an inducer of phylloquinone accumulation in stinging nettle leaves. A significant effect of hydrothermal conditions of the growing environment on the accumulation of phylloquinone by this plant in the vegetation periods of different years was shown.
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The amino acid composition of Haplophyllum Dauricum (l.) G. Don
摘要
Introduction. Haplophyllum dauricum, a well-known source of lignans, is widely used in traditional medicine. Additionally, data on its chemical composition includes information on alkaloids, terpenoids, coumarins, flavonoids, and the macro- and microelement content. However, no information is available regarding the amino acid profile of this plant.
The aim of the study is to determine qualitative and quantitative composition of amino acids in herbs and roots of H. dauricum.
Material and methods. The objects of the study were the herbs and roots of H. dauricum native to the Republic of Buryatia. Samples were collected during the flowering and fruiting periods in 2022 and 2023. The amino acid composition and content were determined using the capillary electrophoresis system "Kapel-105". Statistical analysis of the obtained data was performed using the principal component analysis (PCA) method with the Sirius version 6.0 (Pattern Recognition Systems, a/s, Norway).
Results. Twenty amino acids were found in the herbs and roots parts of H. dauricum, with nonessential amino acids predominating (up to 80.81% of the total). Glutamic acid, glutamine, aspartic acid, and asparagine have the highest content, while proline, arginine, methionine, and serine also have high levels. A change in the quantity of diaminocarboxylic and heterocyclic amino acids was observed in response to abiotic stress.
Conclusions. This is the first study of the qualitative composition and quantitative content of amino acids in H. dauricum. Eight essential amino acids were identified, with glutamic acid, glutamine, aspartic acid, and asparagine being dominant. The data suggest potential for further research on this species and its potential as a source of valuable bioactive compounds.
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The ambiguous role of the matricellular protein tenascin-C in skin wound healing
摘要
Traditional methods for treating extensive skin injuries have certain limitations regarding; therefore, the search for innovative materials and approaches to optimize wound regeneration processes continues to require particular attention. One of the less-studied extracellular matrix proteins in the context of skin wound healing is Tenascin-C (TN-C). At present, its role as a biomarker in tumor processes has been studied in considerable detail, while data on its regenerative properties remain limited. This article examines the mechanisms of action of TN-C, its interactions with cellular structures and signaling pathways, and summarizes the findings of existing studies that highlight its therapeutic potential in stimulating tissue regeneration and improving healing outcomes. TN-C exhibits a multidomain structure, with each domain interacting with specific ligands. This paper presents a deeper understanding of the functional characteristics of each domain, yielding updated information on the properties of TN-C. The review also aims to identify gaps in current knowledge and to determine directions for future research in the field of regenerative medicine. The aim of the study is a comprehensive analysis of current data on the protein Tenascin-C and its potential role as an active component in the process of skin wound healing. The informational and analytical search was conducted through the examination and synthesis of contemporary scientific data available on electronic resources such as PubMed, Web of Science, ScienceDirect, Scopus, Google Scholar, and eLibrary. The literature search was performed using the following keywords: Tenascin-C, wound healing, matricellular proteins, and cell proliferation. Articles published over the past 20 years were analyzed. Based on the results of the literature review, it can be concluded that additional preclinical studies of the investigated protein TN-C as a wound regeneration stimulator are warranted, specifically during the inflammatory and proliferative phases. In the remodeling phase, it may be more appropriate to utilize inhibitors of TN-C expression to avoid the formation of hypertrophic scars.
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Soluble form of podoplanin in patients with bone neoplasms
摘要
Introduction. Podoplanin is a mucin-type transmembrane protein involved in the processes of cell migration, angio- and lymphangiogenesis, embryonic development and metastasis. Its biological activity is realized through interaction with partner proteins (CLEC-2, CD44, galectin-8, etc.). Podoplanin expression is detected in various types of normal cells (lymphatic endothelium, podocytes, follicular dendritic cells), and its increase is associated with a number of malignant neoplasms. Of particular interest is the role of podoplanin in the tumor microenvironment and its potential value as a marker for noninvasive diagnostics. The aim of this work is to study the level of soluble podoplanin in the blood serum of patients with primary bone tumors.
Material and methods. The analysis of podoplanin content in the blood serum was performed in 83 patients with malignant bone tumors (MBT), 24 with benign bone tumors (BBT) and 23 healthy donors of the control group. The total group of patients with malignant bone tumors consisted of 19 children aged 6 to 16 years (median 13 years) and 64 adults aged 19 to 76 years (median 50 years). The serum podoplanin level was measured by enzyme immunoassay using the Human Podoplanin Elisa Kit (RayBiotech, USA) according to the manufacturer's instructions. The obtained data were processed using GraphPad Prizm 10.4 software. When comparing the indicators and analyzing their relationships, the nonparametric Mann–Whitney and Kruskal–Wallis tests were used. Differences and correlations were considered statistically significant at p < 0.05.
Results. The podoplanin level in the control group of children was significantly higher than the level in adults (median 219.6 ng/ml versus 12.8 ng/ml). In patients with MBT, the podoplanin level was lower compared to the control (especially in children), but the differences did not reach statistical significance. In the group of adults, a statistically significant decrease in podoplanin was noted in MBT compared to BBT (p = 0.039). ROC analysis showed low diagnostic value of the studied parameter (AUC=0.514 in adults and AUC=0.645 in children). Among patients over 18 years of age, higher podoplanin levels were associated with age under 50 years (p = 0.011). Podoplanin levels were higher in patients with osteosarcoma than with chondrosarcoma (p = 0.071), but the insignificant differences identified were probably due to the age of the patients. In children, no significant correlations were found between podoplanin levels and clinical and morphological parameters.
Conclusions. Measurement of soluble podoplanin levels in serum has no diagnostic value in patients with MBT. The obtained data highlight the limitations of the use of this marker outside the context of tissue expression and indicate the need for further research in this area. The changes in the content of the soluble form of podoplanin that we described depending on age undoubtedly require further study.
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Disturbance of the night melatonin secretion in patients with the metabolic phenotype of osteoarthritis
摘要
Introduction. The high prevalence of obesity increases the importance of understanding the control of disease progression and associated metabolic abnormalities. Recent studies have revealed melatonin as a cause of degenerative joint diseases and a molecular link between sleep disorders and metabolic diseases, due to its powerful biological functions that have a specific effect on the metabolism of osteochondral tissue. Thus, melatonin plays an important role in the regulation of the sleep/wake cycle, adaptation to environmental changes and is considered a key mediator of pathological processes such as osteoarthritis.
Aim – to assess the severity of somnological disorders and the level of nocturnal secretion of the pineal hormone melatonin in patients with the metabolic phenotype of osteoarthritis.
Material and Methods. 80 patients has took part in the study. Participants were divided into 2 groups: group 1 – patients without joint pathology and normal body mass index; group 2 - patients with the metabolic phenotype of osteoarthritis. The subjects underwent a collection of complaints, anamnesis, as well as a general clinical and orthopedic examination. Serum melatonin levels were determined.
Results. Patients with the metabolic phenotype of osteoarthritis showed dysfunction in scores on the subcomponents of sleep quality and quantity. Patients demonstrated a tendency to daytime sleepiness, dissatisfaction with sleep duration, and frequent awakenings at night, which may be due to pain and symptoms of osteoarthritis. It was found that patients with the metabolic phenotype of osteoarthritis showed a decrease in nocturnal excretion of the pineal gland hormone melatonin in comparison with patients in group 1.
Conclusions. The findings support the growing evidence of a significant interaction between melatonin secretion and metabolically associated diseases.
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Lipid-lowering activity of Phacelia Tanacetifolia Benth. Extract in an experimental model of alcoholic liver damage
摘要
Introduction. Expansion of the domestic raw material base is necessary and expedient due to the study of new plants, including foreign plants. Earlier it was established that the thick extract of the herb of phacelia tanacetifolia has hypolipidemic effect. Evaluation of the effectiveness of this plant substance in this aspect has an important medical and social significance, because lipid metabolism disorders and elevated cholesterol levels are the main risk factors for the development of cerebral ischemia.
The aim of the study is study of hypolipidemic activity of thick extract of phacelia tanacetifolia in conditions of experimental hyperlipidemia induced by ethanol.
Material and methods. The research of hypolipidemic activity was carried out on 20 white Wistar rats weighting 250–270 g. Researched extract was introduced in the form of an aqueous suspension. On the 10th day animals were injected intragastrically once with ethyl alcohol in the form of 40% aqueous solution at a dose of 5 g/kg (in terms of absolute ethanol). Nicotinic acid (Pharmstandard OJSC-UfaVita; Russia) at a dose of 25 mg/kg by the oral route of administration was used as a comparison drug, taking into account the conversion of the maximum daily dose of human to rat using an interspecies coefficient of 5.9. Triglycerides and cholesterol were analyzed on a biochemical analyzer RAL GLIMA MC-15 using reagents from DiaSys, manufactured in Germany.
Results. The introduction of the extract at a dose of 300 mg/kg reduced the content of triglycerides in rat serum by 46%, which may be due to inhibition of their synthesis in the liver; the comparison drug at a dose of 25 mg/kg reduced in serum by 54% and in liver by 68%. Regarding cholesterol, a reduction of 25% in serum and 27% in liver was observed when the extract was administered at a dose of 300 mg/kg and 33% and 20% when the comparison drug was administered. It was also found that under the influence of the extract there was a complete normalization of active thiobarbituric acid products in blood and liver, and liver diene conjugates.
Conclusions. Preventive use of extract in a model of acute hyperlipidemia induced by ethanol demonstrates a hypolipidemic effect due to a decrease in triglycerides and total cholesterol in serum and liver homogenate. An essential role in the prevention of hyperlipidemia plays antioxidant activity of the extract, manifested in the reduction of thiobarbituric acid active products in the liver and serum and diene conjugates in the liver, and increase in the redox potential of the glutathione system.
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The content of neuropeptides in the blood plasma of Wistar rats after subchronic low-dose exposure to mercury acetate
摘要
Introduction. Mercury poisoning has a cumulative effect. Mercury gradually accumulates in tissues and organs, which negatively affects the functions of all body systems, especially the brain.
The aim of this study was to investigate the neuropeptides content in the blood plasma of Wistar rats after subchronic low-dose mercury acetate poisoning.
Material and methods. During the study, rats was intragastrically administered mercury acetate at a dose of 4 mg/kg for 30 days. On days 30 and 44, the blood plasma of rats was tested for the levels of calcium-binding protein (S100), glial fibrillary acidic protein (GFAP), neuron-specific enolase (NSE), pigment epithelial-derived factor (PEDF), myelin basic protein (MBP).
Results. The concentration of S100 protein in the blood plasma of the experimental group of rats decreased by 43,9%, and the concentration of MBP increased by 172,6%. Fourteen days after the end of the toxicant administration, the concentration of protein S100 in the blood plasma of poisoned animals was significantly lower by 132,7% compared to the control group. The content of MBP increased by 59,4% and neuron-specific enolase increased by 44,6%, the concentration of neuropeptides PEDF and GFAP changed insignificantly.
Conclusions. The results obtained demonstrate that even low concentrations of mercury acetate, entering the body for a long time, affect the concentration of neuropeptides in blood plasma, which indicates negative changes in the central nervous system of rats.
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