News of Pharmacy

The growing role of pharmacists in society and prospects for their professional activities

L. O. Hala, K. L. Kosyachenko, Zh. M. Polova, L. V. Konoshevych — Wed, 27 Nov 2024 00:00:00 +0200

Aim. To analyze the changes in the professional functions of pharmacists because of the growing social burden on pharmacies, as well as the prospects for this profession.

Materials and methods. The objects of the study were regulatory legal acts on the regulation of pharmaceutical activities; modern approaches to the organization of pharmaceutical care and services to the population in Ukraine. To achieve this goal, the following methods were used: bibliographic, historical, content analysis, analytical-comparative, systematization and generalization.

Results and discussion. Analyzed the legal acts of the period of Ukraine's independence aimed at forming a patient-oriented model of pharmacy functioning, in particular, the introduction of international quality standards, intensification of state policy to ensure the availability of medicines for the population, and elaboration of the requirements of good pharmacy practice at the present stage. It is proposed that the classical functions of pharmacy institutions (trade, production, information and social), due to the increasing content of the professional roles of pharmacists with the social component of their activities, should be outlined by complex conceptual categories formed from two fundamental activities – socio-economic, trade and production, information and communication, and social and humanitarian. The article considers the prospects for a pharmacist who, at the level of secondary specialization, can acquire new competencies in accordance with the professional standard and further apply for the position of a healthcare professional. As an example, the author characterizes the pharmacist's participation in the pharmacovigilance system – notifying the patient about the possibility of adverse reactions and the algorithm of actions in such a situation, collecting information on adverse drug reactions and health risks, filling out a card-notification of adverse reaction and/or lack of effectiveness of therapy.

Conclusions. The expansion of the content of the professional functions of pharmacists and the growth of their role in society due to the increase in social burden contributes to the formation of a patient-oriented model of pharmacy functioning, but requires the implementation of the requirements of good pharmacy practice and the revision of related regulations to ensure the conditions for the quality provision of pharmaceutical care and services.

The current state and prospects of peptides use in cosmeceuticals

Wed, 27 Nov 2024 00:00:00 +0200

Aim. To analyze the range of peptides in cosmeceuticals.

Materials and methods. The study materials were publications in scientific periodicals. The study used methods of content analysis, comparative, logical, analytical methods and generalization of information.

Results. The analysis of scientific literature data has shown that bioactive peptides of various origins are widely used as active ingredients in cosmeceuticals. In 2022, the global market for the synthesis of cosmetic peptides was estimated in 195.3 million USD. The market is expanding due to the growing consumer demand for skin care and anti-ageing products. Consumers are shifting towards a holistic approach to beauty, appreciating products that not only provide instant results, but also support the skin’s natural processes. Peptides, with their various benefits, perfectly match this approach by promoting skin elasticity from the inside, providing a long-lasting positive result. Peptides can be used to address specific skin problems, such as hyperpigmentation, acne and inflammation. According to the mechanism of action, biologically active peptides are classified as carrier peptides, signal peptides, neurotransmitter inhibitor peptides and enzyme inhibitor peptides. Carrier peptides facilitate the transport of cofactors, such as copper and manganese, across the skin barrier. Both cofactors are essential for enzymatic reactions involved in preventing aging and wound healing. Copper tripeptide-1 and manganese tripeptide-1 are examples of carrier peptides that have been successfully used to reduce fine lines, wrinkles and hyperpigmentation associated with photoaging. Signal peptides or matrikines are derived from extracellular matrix proteins, such as collagen, elastin and fibronectin. Matrikines interact with specific receptors that stimulate the synthesis, repair and remodeling of the extracellular matrix. These peptides also regulate the activity of certain key enzymes involved in the aging process, such as collagenase, elastase, tyrosinase and hyaluronidase. Neurotransmitter inhibitor peptides are the latest cosmeceutical peptides. Similar to botulinum toxins, these peptides prevent the release of acetylcholine, a neurotransmitter responsible for muscle contraction. Inhibiting this process relaxes facial muscles, preventing the formation of fine lines and wrinkles. Neurotransmitter inhibitor peptides are a safer alternative to traditional botulinum toxin treatment with fewer potential side effects. Enzyme inhibitor peptides have become popular active ingredients in anti-ageing cosmetics. This class of peptides inhibits the activity of certain enzymes involved in various biochemical processes of the skin. Their application in cosmeceuticals is to control or inhibit those processes that cause skin damage, aging or loss of elasticity.

Conclusions. The study of peptides for use in cosmeceuticals has opened new prospects in skin care and aesthetic medicine. Bioactive peptides of various origins – from plants, animals, marine organisms, and edible insects – exhibit a wide range of properties, including antiaging, antioxidant, anti-inflammatory, and antimicrobial effects. Peptides open new horizons in the creation of innovative cosmeceuticals, especially when combined with other active components, such as antioxidants or retinoids. Their safety, ability to biodegrade and spot impact make peptides an attractive ingredient for solving various dermatological problems without the side effects of more aggressive skin correction methods.

The synthesis, antimicrobial activity and theoretical calculations of 4-(4,5-diphenyl-1-(4-(phenyldiazenyl)phenyl)-1H-imidazol-2-yl)-N,N-dimethylaniline

Wed, 27 Nov 2024 00:00:00 +0200

Aim. To synthesize 4-(4,5-diphenyl-1-(4-(phenyldiazenyl)phenyl)-1H-imidazol-2-yl)-N,N-dimethylaniline, as well as make theoretical calculations of its structure and study its antimicrobial properties.

Materials and methods. The synthesis procedures were performed in the presence of ionic liquid catalysts and under microwave conditions. The catalysts included 1-butyl-3-methylimidazolehydrosulfate, N-methylpyrrolidone perchlorate, and 1,4-dimethylpiperazinedihydrosulfate ionic liquids. Benzyl, ammonium acetate, p-aminoazobenzene and 4-(dimethylamino)benzaldehyde were taken as reagents. Ethanol was used as a solvent.

Results. The results of the conditions were compared and it was determined that the 1,4-dimethylpiperazinedihydrosulfate catalyst reacted under microwave conditions in a shorter time (19 min) with a higher yield (78.1 %). The structure of the compound synthesized was analyzed by ¹H, ¹³C NMR and IR spectroscopy. The theoretical calculations of the compound were determined using the density functional theory (DFT/B3LYP) method with a basic set of 6-31G(d,p). The geometry of the structure was optimized, bond lengths, angle degrees were given, and important quantum chemical parameters, such as HOMO, LUMO orbitals, reactivity, stability, electrophilicity, electronegativity, chemical softness, chemical hardness were calculated. It was found that the compound had a high stability (∆E = 2.359 eV) and a high biological activity (ω = 5.754 eV). The antimicrobial activity of the sample against bacteria of S. aureus, E. coli, P. aeruginosa, K. pneumoniae, B. anthracoides and C. albicans fungus was studied.

Conclusions. In this work, 4-(4,5-diphenyl-1-(4-(phenyldiazenyl)phenyl)-1H-imidazol-2-yl)-N,N-dimethylaniline has been synthesized from benzyl, ammonium acetate, p-aminoazobenzene and 4-(dimethylamino)benzaldehyde in the presence of microwave and ionic liquid catalysts. It has been determined that 1,4-dimethylpiperazinedihydrosulfate catalyst reacts under microwave conditions in a shorter time (19 min) with a higher yield (78.1 %). The compound has been tested as an antimicrobial agent against bacteria of S. aureus, E. coli, P. aeruginosa, K. pneumoniae, B. anthracoides and C. albicans fungus, showing moderate and higher activity.

The analysis of recombinant insulin production technologies

O. S. Kaliuzhnaia, N. V. Khokhlenkova, M. V. Panenko — Wed, 27 Nov 2024 00:00:00 +0200

Aim. To analyze current trends in insulin production and expression systems used to obtain recombinant proteins.

Materials and methods. The specified goal was achieved using the methods of content analysis, comparative, logical, analytical and generalization of information. The research materials were publications in scientific periodicals, official websites of manufacturing companies.

Results. It has been found that the following expression systems are traditionally used for the commercial production of recombinant human insulins: bacterial – Escherichia coli, and yeast – Saccharomyces cerevisiae. But to meet the global need for insulin, it is necessary to develop new effective expression systems. Therefore, the use of other eukaryotic insulin expression systems that would be suitable for large-scale production is currently being studied. Among such systems, transgenic plants, which are characterized by the absence of potential human pathogens and the presence of post-translational protein modification mechanisms similar to human ones, are promising for introduction into insulin production. Currently, studies using Arabidopsis thaliana, tobacco, lettuce and strawberry plants are successful. Stem cells – embryonic, mesenchymal and induced pluripotent are also considered promising. The methods used in the large-scale production of recombinant insulin based on the synthesis of proinsulin and the two-chain method have been characterized. The technological flowcharts of both technologies have been drawn up, the advantages and disadvantages of each are given.

Conclusions. The analysis of data from the scientific literature has shown that the main methods of producing insulin preparations since the 1980s remain pro-insulin and two-chain methods, which are based on recombinant DNA technologies. The pro-insulin method is considered more efficient and cost-effective compared to the two-chain method since this technology consists of working with a single recombinant strain. The choice between these two methods depends on the specific needs of the manufacturer: for some cases a fast method with proinsulin synthesis is rational, for others – a more accurate and controlled two-chain method. The bacteria – Escherichia coli and yeast – Saccharomyces cerevisiae remain the expression systems used in the existing large-scale production technologies. But using E. coli, insulin precursors are produced in inclusion bodies, and fully functional polypeptides are obtained by solubilization and refolding steps. The yeast-based system yields a soluble insulin precursor that is secreted into the culture fluid, but requires prior humanization due to the risks of an immune response in humans. Thus, current production technologies cannot meet the growing demand for available insulin due to limited production capacity and high production costs, so research is being conducted to find new efficient expression systems, such as plant and mammalian cells, including Arabidopsis thaliana, tobacco, lettuce, strawberry, stem cells.

Substantiation of the composition of sublingual tablets for the treatment of CNS disorders

I. O. Davydova, O. A. Ruban, H. D. Slipchenko , I. V Zupanets, O. I. Ivaniuk — Wed, 27 Nov 2024 00:00:00 +0200

Aim. To develop the composition of sublingual tablets with L-tryptophan, glycine and a dry peony extract.

Materials and methods. L-tryptophan, glycine and a dry peony extract were used as active pharmaceutical ingredients; Lactose GranuLac 200, MCC 102, HPMC methocel K4M CR Premium, HPMC methocel E4M CR Premium, aspartame, maltodextrin, sorbitol, sucralose, Mint cloroph FLV PDR, Strawberry FLV PDR, Apple FLV PDR, Plasdone K-25, crospovidone XL-10, nonessylin and calcium stearate were used as excipients. The pharmacotechnological studies were conducted in accordance with the methods of the State Pharmacopoeia of Ukraine.

Results and discussion. The studies of the pharmacotechnological properties of APIs showed unsatisfactory results (poor fluidity, poor cohesive properties; high hygroscopicity of the peony extract), so it was decided to improve the technological properties of the active substances by wet granulation. Plasdone K-25 (15% aqueous solution) was chosen as a binder. The next step was to select a flour adhesive to improve the bioavailability of the active ingredients. According to the literature, HPMC was included in the composition of the test samples: HPMC methocel E4M CR Premium and HPMC methocel K4M CR Premium. According to the research results, HPMC methocel K4M CR Premium was included in the composition. The tablets developed had a bitter taste due to the presence of tryptophan and the peony extract. To correct the taste and odor, aspartame and Mint cloroph FLV PDR were used. Their optimal content in the formulation was experimentally determined.

Conclusions. As a result of the studies conducted, the following substances have been selected: the binder for granulating the tablet mixture – Plasdone K-25; the flour adhesive to improve bioavailability – HPMC methocel K4M CR Premium; flavors for taste and odor to mask the bitter taste of sublingual tablets – aspartame and Mint cloroph FLV PDR.

The development of the technology of a thick extract for the treatment of cheilitis

Wed, 27 Nov 2024 00:00:00 +0200

Aim. To substantiate the parameters of the technological process for obtaining an aqueous thick extract based on the medicinal plant raw material for the treatment of cheilitis.

Materials and methods. The study objects were experimental samples of a phytocomplex (large burdock root: oak bark: pot marigold flower buds 5: 1: 1.5) and an aqueous thick extract obtained on its basis. During the development of the technology for obtaining a thick extract and its standardization, organoleptic, physicochemical and pharmacotechnological research methods were used in accordance with the methods and recommendations given in the SPhU 2.0. The results of the research were statistically processed in accordance with the requirements of monograph 5.3 of the SPhU 2.3.

Results. The pharmacotechnological properties of the phytocomplex for the prevention and treatment of cheilitis – large burdock root: oak bark: pot marigold flower buds (5: 1: 1.5, respectively) were experimentally studied. The optimal conditions for extraction of the complex with purified water were determined; they were: temperature – 95-100 ºС; three-stage remaceration method; the total ratio of the raw material: finished extract (1:10). The technological parameters were worked out; the technological flowsheet of the process for obtaining an intermediate product – an aqueous thick extract under the conditional name “Phytol” was developed.

Conclusions. Based on the studies conducted, the technological parameters of the extraction process for the phytocomplex proposed have been determined; the technology for obtaining an aqueous thick extract has been substantiated step-by-step, and its technological flowsheet has been drawn up.

Organizational and economic studies of the turnover of anthelmintic drugs in the domestic pharmaceutical market in modern conditions

Wed, 27 Nov 2024 00:00:00 +0200

Aim. To conduct organizational and economic studies of the peculiarities of the turnover of anthelmintic drugs in the domestic pharmaceutical market in modern conditions under the influence of high risks and uncertainties.

Materials and methods are based on open access information for professional use by doctors and pharmacists, materials from scientific publications and monographic editions of domestic and foreign scientists, the results of personal research using Google forms. For the survey, 90 pharmacy specialists were involved as respondents. The results were processed and verified using licensed Microsoft Excel software products.

Results and discussion. The list of anthelmintic drugs, which are in circulation in the domestic pharmaceutical market in modern conditions, has been determined. The organizational and economic features of each of them, such as the level of demand and cost indicators, have been outlined. It has been found that there are 24 names of such anthelmintic drugs, including 11 based on the active substance albendazole, 7 based on pyrantel, 2 based on mebendazole, 3 based on levomizole and one herbal tea based on tansy flowers. The most popular anthelmintic drugs in modern conditions, the level of demand for which exceeds 70.0 % (7 items), have been determined. Certain features of the actions of pharmacy specialists when dispensing anthelmintic drugs from pharmacies, which can contribute to the formation of demand for them, have been studied, including 18 questions according to the respondents’ rating.

Conclusions. The results of the study conducted have allowed determining the peculiarities of the turnover of anthelmintic drugs in the domestic pharmaceutical market in modern conditions under the influence of high risks and uncertainties. Their list, level of demand and cost indicators have been defined, as well as certain recommended actions of the pharmacy specialists when dispensing from pharmacies.

The study of the antiviral effect of a soft dosage form

S. D. Zahorodnia, M. V. Yaromiy, L. O. Artiukh, N. P. Polovko — Wed, 27 Nov 2024 00:00:00 +0200

Aim. To study the antiviral activity of a soft medicine with mangiferin against the herpes simplex virus.

Materials and methods. The studies used samples of the soft dosage form developed with mangiferin, a xanthone belonging to the class of polyphenols. Mangiferin is a light yellow fine crystalline powder obtained from the leaves of the mango tree (Mangifera indica), (manufacturer Shaanxi, China). The substance contains 98.5 % of mangiferin.

The antiviral activity was studied on Vero kidney cells of an African green monkey obtained from the Cell Bank of the Institute of Experimental Pathology, Oncology and Radiobiology named after R. E. Kavetsky of the National Academy of Sciences of Ukraine. The cell cultivation was performed according to standard methods. The cultivation and accumulation of the virus was carried out on Vero cell culture. The infectious titer of the virus was 7.4 log₁₀ TCD _50/ml. The MTT modification analysis was used to study the cell viability. The antiviral activity was studied according to standard methods. The virulicidal activity against HSV-1 was determined by decreasing the cytopathic effect of the virus on cells and the virus titer using the MTT method.

Results and discussion. The determination of the direct effect of the test sample on the extracellular herpes virus (virucidal effect) of an undiluted sample and samples in a dilution of 1:2.5 and 1:5 showed their ability to exhibit a significant virucidal effect against HSV-1 regardless of the dilution used and the exposure time with the virus. It was found that the decrease in the titer of the herpes virus was within 1.7-2.2 log₁₀. When studying the ability of the test sample to influence the development of the cytopathic effect of the herpes virus on cells, it was determined that in dilutions (1:20-1:320), the sample inhibited the reproduction of the virus and the development of HSV-1 on Vero cells compared to the control virus. The greatest efficiency was found when using the sample in dilutions of 1:80-1:320; the reduction in the development of the cytopathic effect of the virus on cells was in the range of 59-64 %. When studying the infectious titer of the herpes virus synthesized de novo after the treatment with various dilutions of the test sample, it was shown that the test sample in the dilutions used did not significantly affect the synthesis of the infectious progeny of the virus, the decrease in the viral titer did not exceed 1.1 log₁₀. Cytotoxicity assays showed that in the dilutions of 1:40 or more, the maximum reduction in cell viability was 18 %, indicating low toxicity of the sample.

Conclusions. According to the results of the study, the ability of the test sample containing 5 % mangiferin to effectively inactivate the extracellular herpes simplex virus Type 1 and significantly inhibit the development of the cytopathic effect of the virus on cells has been found.

The methodology for developing modified release granules based on phytoextracts for the treatment of mastopathy

P. V. Palyvoda, S. S. Zuykina — Wed, 27 Nov 2024 00:00:00 +0200

Aim. To substantiate the scientific and methodological approach to the development of the composition and technology of granules based on phytoextracts with modified release of active substances for the complex treatment of mastopathy.

Materials and methods. The research was conducted by processing electronic and paper sources of information on the etiopathogenetic factors of mastopathy, the concept of developing medicinal products with modified release of active pharmaceutical ingredients (APIs), the market analysis of medicines and dietary supplements (DS) for the treatment of mastopathy.

Results. An information search has been conducted to study the etiology, pathogenesis, clinical manifestations and pharmacotherapy of breast diseases. The article presents and substantiates the stages of experimental research on the development of a medicinal product in the form of granules based on phytoextracts with a modified release of active substances, including marketing and statistical research methods of electronic and paper sources of information on the prevalence and consequences of mastopathy, development of granules based on phytoextracts with a modified release of APIs, standardization, preclinical studies of the medicinal product developed.

Conclusions. The scientific and methodical approach to the development of the composition and technology of granules based on phytoextracts with a modified API release for the complex pharmacocorrection of mastopathy and prevention of the appearance of malignant neoplasms in breast tissues has been substantiated.

The experimental substantiation of the main parameters of the extraction of gaillardia herb (Gaillardia pulchella L.)

M. V. Buryak, L. I. Vyshnevska — Wed, 27 Nov 2024 00:00:00 +0200

In the structure of the pharmaceutical market, the share of drugs based on the medicinal plant raw material (MPRM) is growing. Therefore, it is relevant to create a standardized domestic substance of natural origin – a liquid extract of gaillardia herb (Gaillardia pulchela L.) and develop new medicines based on it.

Aim. To obtain a liquid extract by experimentally substantiating the main parameters of gaillardia herb extraction.

Materials and methods. The study object was the raw material of gaillardia herb collected in the flowering phase at the Botanical Garden of the Poltava National Pedagogical University named after V. G. Korolenko (Poltava) in July and August 2022-2023, dried by the air-shade method and crushed by the rolling method. The crushed raw material was sifted through a sieve with a hole size of 10 mm. The millet was used for further research. The study of pharmaco-technological indicators was carried out according to the standard methods of the SPhU.

Results and discussion. Since the complex of active substances of gaillardia herb was mainly represented by water-soluble BAS, it was necessary to choose a solvent that would remove this group of substances from the raw material as completely as possible. The experimental data obtained show that the ability to extract the BAS complex from gaillardia herb is preferred by purified water, which provides the maximum yield of extractive substances. The next stage of our research was to study the determination of the multiplicity of extraction, based on the determination of the maximum yield of extractive substances. Each of the extracts was selected fractionally with a step of DER 1:1 (drug extract ratio – the ratio of the starting material to the resulting extract). According to the data obtained, the amount of extractives passing during the extraction into the hood increases gradually up to 5 samples. Analyzing extracts from 6 to 10, it can be seen that the amount of extractives and a dry residue varies slightly; percolation with the extraction of more than 5 will lead to an increase in the consumption of the extractant and a decrease in the yield of active substances for the entire volume of the extractant.

Conclusions. Based on the results of the studies conducted, the technological parameters of gaillardia herb have been determined (the volume mass – 0.453 ± 0.016 g/cm³; the bulk mass – 0.071 ± 0.001 g/cm³, the specific gravity – 1.214 ± 0.032 g/cm³, the water absorption coefficient – 1.68 ± 0.08). It has been experimentally proven that when extracting with purified water, the maximum yield of extractive substances is observed in the second volume, the yield of extractive substances is smooth, without sharp fluctuations in concentrations (in contrast to 40 and 70% ethanol). Therefore, the studies have determined an effective extractant for obtaining the extract, namely purified water. As a result of the pharmaco-technological tests conducted, the effective multiplicity of gaillardia herb extraction has been determined, which is equal to 5. The data will be taken into account when developing the technology of a liquid extract from gaillardia herb and choosing equipment for its production.

The study of the toxicological profile of dry extracts of narrow-leaved lavender herb

O. O. Bogatyrova, O. I. Naboka — Fri, 01 Nov 2024 00:00:00 +0200

Aim. To study the acute toxicity of narrow-leaved lavender (Lavandula angustifolia) herb dry extracts of Ukrainian origin.

Materials and methods. The study objects were experimental test samples: test sample No. 1 ‒ a dry extract of narrow-leaved lavender herb obtained by extraction with purified water; test sample No. 2 ‒ a dry extract of narrow-leaved lavender herb obtained by extraction with a water‒ethanol solution (40 % ethanol); test sample No. 3 ‒ a dry extract of narrow-leaved lavender herb obtained by extraction with a water‒ethanol solution (70 % ethanol). To reproduce the clinic of acute poisoning and determine LD₅₀, the acute toxicity of test samples was studied on sexually mature white mice weighing 19-21 g under the conditions of a single intragastric administration. The animals were observed for 2 weeks, which made it possible to assess the toxic effect of the lavender extracts studied on the body of experimental animals. The weight (initial data, 3, 7 and 14 days), the behavior of animals after the introduction of test samples (appearance, respiration, salivation, urination, excreta, feed consumption by animals) were monitored by daily feed and water consumption ‒ on days 7 and 14. The macroscopic examination included the external examination of animals, the examination of internal organs of the chest (heart, lungs, thymus) and abdominal cavities (liver, spleen, kidneys, adrenal glands, testes/ovaries). For statistical processing of the data obtained (body weight), the arithmetic average value and its standard error were used; the reliability of discrepancies between samples was assessed using ANOVA RM and the Dunnet criterion. Comparisons were made with the negative control group. Indicators of the mass coefficients of internal organs were presented in the form of the median, upper and lower quartiles. The reliability of discrepancies between samples was assessed using the Kruskal-Wallis test and the Mann-Whitney test compared to the negative control group.

Results and discussion. It was experimentally proven that intragastric administration of dry extracts from lavender herb in the dose of 5000 mg/kg did not lead to lethality and did not affect the general trophic processes of animals. The macroscopic examination of internal organs and analysis of their mass coefficients confirmed that a single intragastric administration of test samples of lavender extracts did not lead to pathological changes in both males and females. The organ mass coefficients were within the normal range and had no statistically significant differences compared to animals in the negative control group.

Conclusions. The results of the study have demonstrated that a single intragastric administration of test samples of lavender in the dose of 5000 mg/kg does not lead to pathological changes in the physiological state of mice, which allows to attribute the extracts studied to class V of practically non-toxic substances (LD₅₀> 5000 mg/kg).

The effect of a new phytocomposition based on the cranberry leaf extract and amino acids on the pancreas and liver of rats in the model of diabetes mellitus type 2

N.M. Kononenko, M.S. Anisimova — Wed, 27 Nov 2024 00:00:00 +0200

In pharmacotherapy of diabetes mellitus type 2 and metabolic syndrome, medicinal plants and amino acids are used as an important preventive and therapeutic supplement to correct disorders that develop against the background of insulin resistance, which determines the relevance of developing new domestic combined antidiabetic herbal medicines.

Aim. To study the effect of a phytocomposition based on the polyphenol extract from large-fruited cranberry leaves and amino acids (L-arginine, taurine, glycine) on the state of the liver and pancreas of rats in an experimental model of diabetes mellitus type 2.

Materials and methods. Diabetes mellitus type 2 was reproduced by a single injection of rats with a streptozotocin solution in the dose of 65 mg/kg, intraperitoneally with the previous (15 min) intraperitoneal administration of nicotinamide in the dose of 230 mg/kg against the background of obesity (keeping rats on a high-calorie diet for 12 weeks). The pancreatic and hepatoprotective effect of the phytocomposition was studied according to the morphofunctional state of pancreatic β-cells, the content of glycogen and neutral fats in the liver and morphometric indices in the pancreas.

Results. The phytocomposition studied had a stimulating effect on regenerative processes in the insulin-producing apparatus of the rat pancreas – the severity of proliferation of small β-cells in pancreatic islets significantly increased compared to the control pathology. The phytocomposition at the morphological level showed hepatoprotective properties considerably reducing the manifestations of the toxic-dystrophic action of diabetogens, significantly restoring fat and carbohydrate metabolism in hepatocytes.

Conclusions. The results obtained substantiate the feasibility of further study of the phytocomposition as a promising antidiabetic agent.

The study of the total antioxidant capacity of St. John’s Wort (Hypericum perforatum L.) herb

O. Yu. Maslov, M. A. Komisarenko , S. V. Kolisnyk — Wed, 27 Nov 2024 00:00:00 +0200

Aim. To determine the total antioxidant capacity of St. John’s Wort herb.

Materials and methods. The content of phenolic compounds, anthraquinone derivatives, flavonoids, and derivatives of hydroxycinnamic acids was determined by the spectrophotometric analysis, while organic acids were identified by the alkalimetric method; the antioxidant activity of extracts obtained was evaluated by the potentiometric method.

Results and discussion. The total antioxidant capacity of St. John’s Wort herb was 91.35 mmol-equiv/m _{dry weight}, the total content of phenolic compounds was 22.70 mg of gallic acid/mL, anthraquinone derivatives – 0.46 mg of hyperecin/mL, flavonoids – 8.10 mg of rutin/mL, derivatives of hydroxycinnamic acids – 7.90 mg of chlorogenic acid/mL and organic acids – 10.80 mg of citric acid/mL in St. John’s Wort herb extracts obtained during the sequential exhaustive extraction. The correlation analysis showed a very high positive correlation between the antioxidant activity and the total content of phenolic compounds, flavonoids, hydroxycinnamic acid derivatives in St. John’s Wort herb extracts.

Conclusions. The total antioxidant capacity of H. perforatum herb was 91.35 mmol-equiv./m _{dry weight}. The results of the analysis of the BAS content and the antioxidant activity of H. perforatum herb extracts revealed that the aqueous extract had a significant content of phenolic compounds, flavonoids, hydroxycinnamic acids, organic acids and the antioxidant activity, while anthraquinone derivatives dominated in 96 and 60 % EtOH extracts. The quantitative analysis showed that flavonoids and hydroxycinnamic acids dominated among phenolic compounds. The results can be applied in developing optimal technologies for obtaining drugs based on the extract of H. perforatum herb.

A comparative microbiological study of the essential oils from the genus Rosa L.

Fri, 01 Nov 2024 00:00:00 +0200

The medicinal plant raw material containing essential oils always attract the attention of scientists from various countries worldwide. The search for new sources of the plant raw material rich in biologically active substances, particularly volatile compounds, remains a relevant task in modern pharmaceutical science. Our focus has been drawn to Rosa damascena Mill. of the “Veselka” (“Rainbow”) variety grown in the natural environment of Zaporizhzhia; its essential oil exhibits anti-inflammatory, antimicrobial, and antiseptic effects. To obtain a valuable medicinal plant raw material from Rosa damascena with a high content of essential oil, it was introduced into in vitro culture to produce aseptic regenerants, followed by their reintroduction into the natural environment.

Aim. To conduct a comparative microbiological study of essential oils from Rosa damascena of the “Veselka” variety grown via clonal micropropagation in in vitro culture and in the natural environment of Zaporizhzhia.

Materials and methods. The study objects were essential oils obtained by water distillation from rose petals cultivated using the method of clonal micropropagation in in vitro culture (at the premises of the Educational and Scientific Medical Laboratory Center with a vivarium) and the natural environment of Zaporizhzhia. The study of the antimicrobial activity was conducted in the microbiological laboratory of the Department of Microbiology, Virology, and Immunology at Zaporizhzhia State Medical and Pharmaceutical University.

Results and discussion. The essential oils from Rosa damascena grown via clonal micropropagation in in vitro culture and under natural conditions in Zaporizhzhia effectively inhibited the growth of E. coli (21.3 mm and 12.0 mm, respectively) and S. aureus (11.3 mm and 10.2 mm, respectively). The results of the study on C. albicans indicate a high antifungal activity in both essential oils; the mean inhibition zone diameter in the experiments using the oil from Rosa damascena cultivated in in vitro culture is less: 33.3 mm compared to 40 mm in the experiments with the oil from roses grown in the natural environment of Zaporizhzhia.

Conclusions. The method of clonal micropropagation of Rosa damascena of the “Veselka” variety is effective for obtaining a large amount of planting material in a short time with the subsequent reintroduction into the natural environment to expand the raw material base of valuable medicinal plants with a high content of essential oils. The results of the study of the antimicrobial activity of the essential oil of Rosa damascena of the “Veselka” variety cultivated through clonal micropropagation in in vitro culture have exhibited a high antimicrobial activity and moderate antifungal activity compared to the essential oil from Rosa damascena grown in the natural environment of Zaporizhzhia. Therefore, Rosa damascena Mill. of the “Veselka” variety cultivated under in vitro conditions is a promising source of essential oil with a high antibacterial effect in order to create new herbal formulations.

The effect of a new product based on quercetin and a thick extract of carrot seed root on the histological state of the rat cardiac muscle in the adrenaline-hydrocortisone-induced myocardial infarction

T. R. Kononenko, V. V. Chikitkina — Wed, 27 Nov 2024 00:00:00 +0200

Aim. To study the effect of tablets with a thick extract of carrot seed root and quercetin on the histological state of the rat cardiac muscle in the experimental adrenaline-hydrocortisone-induced myocardial infarction.

Materials and methods. The cardioprotective effect of tablets with a thick extract of carrot seed root and quercetin was studied on the model of acute adrenaline-hydrocortisone-induced myocardial infarction caused by subcutaneous administration of 0.1 % adrenaline hydrochloride solution in the dose of 1 mg/kg and 2.5 % hydrocortisone acetate emulsion in the dose of 12.5 mg/kg of the animal weight twice daily for a week. The tablets under research in the dose of 200 mg/kg and the reference drugs – “Thiotriazolin” and “Cratal” tablets were administered for 14 days – 7 days before the infarction modeling and 7 days of the myocardial infarction development, after which their effect on the histological state of the rat heart muscle was studied.

Results. Modeling of the adrenaline-hydrocortisone-induced myocardial infarction in rats is accompanied by the appearance of focal necrotic changes in muscle cells, which in some cases are accompanied by initial regenerative manifestations in the form of granuloma formation; dystrophic processes of cardiomyocytes. The therapeutic and prophylactic administration of tablets from a thick extract of carrot seed root and quercetin on the model of the adrenaline-hydrocortisone-induced myocardial infarction has the cardioprotective effect, reducing the severity of necrotic and dystrophic changes in the cardiac muscle.

Conclusions. As a result of modeling of the adrenaline-hydrocortisone-induced myocardial infarction in rats, focal necrotic changes in muscle cells were observed, sometimes accompanied by the initial formation of a matrix consisting of young fibroblasts; dystrophic processes of cardiomyocytes, in particular myocytolysis, fluctuations in the size of nuclei. The therapeutic and preventive administration of the tablets studied on the model of the adrenaline-hydrocortisone-induced myocardial infarction has the cardioprotective effect, reduces the severity of necrotic and dystrophic changes in the cardiac muscle. By the cardioprotective effect expressiveness, tablets with a thick extract of carrot seed root and quercetin on the model of the adrenaline-hydrocortisone-induced myocardial infarction are not inferior to the reference drugs – “Thiotriazolin” and “Cratal” tablets. The results experimentally substantiate the feasibility of creating a new combined drug from a thick extract of carrot seed root and quercetin for the prevention and pharmacocorrection of a cardiovascular pathology.