The aim of the work. 1,2,4-triazole derivatives possess a wide range of pharmacological activity, so they are used for the development of drugs and active pharmaceutical ingredients. Due to the reactivity of 1,2,4-triazoles there are many options for their further structural modification on different reaction centers. Therefore, the aim of the work was to obtain new S-substituted derivatives of 1,2,4-triazole-3-thiols, study physicochemical parameters of the substances synthesized, evaluate the antimicrobial activity of new S-derivatives of the 4-R1-5-((3-(pyridin-4-yl)-1H-1,2,4-triazol-5-yl)thio)methyl)-4H-1,2,4-triazole-3-thiol series, and study some regularities of the “structure – biological activity” relationship for the synthesized compounds as well. Materials and methods. The subject of the study was new S-substituted 1,2,4-triazoles containing 2-oxopropan-1-yl and 2-aryl-2-oxoethan-1-yl substituents. The antimicrobial activity was studied by double serial dilutions on test cultures of Staphylococcus aureus (ATCC 25923), Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853), and Candida albicans (ATCC 885-653). The results of the biological screening showed that at a concentration of 125 g/mL, all synthesized substances showed activity (MIC – in the range of 31.25 - 62.5 μg/mL, MBCK - in the range of 62.5–125 μg/mL) against strains of Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Candida albicans. Variation of substituents on the sulfur atom did not lead to a significant change in antimicrobial and antifungal activities among derivatives of 4-R1-5-((3-(pyridin-4-yl)-1H-1,2,4-triazole-5-yl) thio)methyl)-4H-1,2,4-triazole-3-thiols. Conclusions. Biological screening data indicate the prospects for the search for new antimicrobial substances among the abovementioned derivatives of 1,2,4-triazoles. The most active compounds were 1-((4-ethyl-5-((3-(pyridin-4-yl)-1H-1,2,4-triazol-5-yl)thio)methyl)-4H-1,2,4-triazol-3-yl)thio)propan-2-one and 1-(4-methoxyphenyl)-2-(4-ethyl-5-(((3-(pyridin-4-yl)-1H)-1,2,4-triazol-5-yl)thio)methyl)-4H-1,2,4-triazol-3-yl)thio)ethanone, which showed the most pronounced antimicrobial activity against the Pseudomonas aeruginosa strain (MIC – 31.25 μg/mL, MBcK - 62.5 μg/mL)

Damask rose of the Veselka variety is an important industrial rose variety used to obtain essential oil. It is widely used in modern cosmetology, perfumery, and aromatherapy. In addition, the essential oil of Damask rose has a whole spectrum of pharmacological properties. The scientific innovation of this research lies in its foundation on cultivating and acquiring planting materials of the Damask rose in vitro. This approach guarantees controlled conditions for plant growth, the production of robust seedlings, and an enhancement in the precision and credibility of the research outcomes. Moreover, the study has scientific novelty in that it explores to assess both the quantitative and qualitative constituents of the essential oil in the acquired plant material of the Damask rose. This assessment takes place within the context of cultivating regenerative plants in an outdoor environment. Such an approach acknowledges the potential distinctions in the oil's component composition acquired from plants propagated through this method in comparison to traditional vegetative reproduction. Lastly, the research has scientific novelty in investigating the potential antimicrobial properties of Damask rose essential oil, which could have significant practical implications in the development of new drugs and combatting infectious diseases. The purpose of the study was to establish the component composition of the essential oil of Rosa damascena Mill., which was grown in vitro, and to determine its antimicrobial effect. Methods. The object of the study was the essential oil of Damask rose of the Veselka variety, which was grown by the method of clonal micropropagation in vitro. The essential oil was extracted from fresh petals collected during dry weather conditions prior to sunrise by hydrodistillation. Determination of the qualitative composition and quantitative content of volatile substances was carried out by the GC-MS method using an Agilent 7890B chromatograph. Antimicrobial activity was studied in vitro using the disk diffusion method with reference test strains of microorganisms Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, Staphylococcus aureus ATCC 25923, Candida albicans ATCC 885-653. Results. According to the results of the chromato-mass spectrometric study, 41 compounds (6 of which were in the isomeric state) were identified, which was belong to 13 different classes of chemicals. Dominant compounds among terpenoid substances were shown: geraniol – 30.96 %, citronellol – 27.08 %, alkanes: nonadecane – 17.29 %, and heneicosene – 5.46 %. It was established that the essential oil of Damask rose had a significant antimicrobial effect against strains of C. albicans and E. coli, the diameters of which growth retardation zones ranged from 32-35 mm and 20-23 mm, respectively. In studies with P. aeruginosa and S. aureus, the essential oil showed moderate antibacterial activity: the diameters of the growth retardation zone of these microorganisms ranged from 13 to 15 mm and 11 to 12 mm, respectively. Conclusion. For the first time, the qualitative composition and quantitative content of volatile substances in the essential oil extracted from the petals of Rosa damascena Mill., Veselka variety, cultivated through the clonal micropropagation in vitro, were explored by chromatography-mass spectrometry techniques. The results of the study of antimicrobial activity showed that the studied essential oil exhibits significant fungicidal effects against Candida microorganisms, along with moderate bactericidal effects on gram-negative (E. coli, P. aeruginosa) and gram-positive (S. Aureus) bacteria. These results highlight the potential of this essential oil for further investigation in the realm of developing novel medicines and herbal preparations. Further clinical studies are needed to assess this potential.

The main problem of modern phytotherapy is the medicinal plants that have a sufficient raw material base and contain a large number of biologically active substances. Treatment of diseases with synthetic drugs leads to the development of resistance to pathogenic microflora and the appearance of allergic reactions. Therefore, to solve this problem, it is necessary to find new plant-based antimicrobials that are safe for long-term use and have a wide spectrum of action. The aim of the work was to study the antibacterial and fungicidal activity of the essential oil of Thymus x citriodorus (Pers.) Schreb. var. “Silver Queen”. Materials and methods. The essential oil of Thymus x citriodorus (Pers.) Schreb. var. “Silver Queen” was used for the experimental part. To test the antimicrobial and antifungal action of the essential oil, reference test strains, gram-positive and gram-negative bacteria, as well as yeast-like fungi of the genus Candida were selected. The studies were performed in vitro using the disco-diffusion method. Results. Studies have shown that the essential oil of Thymus x citriodorus (Pers.) Schreb. var. “Silver Queen” has a significant antibacterial effect against S. aureus ATCC 25923 (diameters of growth inhibition were 14.60 ± 1.52 mm) and fungicidal effect Candida albicans ATCC 885-6530 (29.30 ± 2.82 mm). Antibacterial activity of the essential oil was detected in relation to E. coli (19.60 ± 1.85 mm). It was experimentally proven that the essential oil had no bactericidal effect on the test strain of P. aeruginosa. Conclusions. It was found that the essential oil of the studied hybrid species Thymus x citriodorus (Pers.) Schreb. var. “Silver Queen” shows a significant antibacterial activity and is promising for further research.

Мониторинг циркуляции возбудителей гнойно-септических инфекций (ГСИ) в условиях стационара и изучение антибиотикочувствительности выделенных штаммов микроорганизмов позволяет установить изменения в структуре патогенов и тенденции развития антибиотикорезистентности, а следовательно дает возможность определиться с тактикой антибактериальной терапии и разработать соответствующие профилактические мероприятия. Цель работы – ретроспективный анализ результатов микробиологического мониторинга за возбудителями ГСИ ортопедо-травматологического отделения (ОТО) КНП «Городская больница экстренной и скорой медицинской помощи» за 2017–2020 гг. для определения основных антибактериальных препаратов для проведения эмпирической терапии. Материалы и методы. Проанализировали результаты бактериологических исследований 664 образцов клинического материала от больных ОТО с использованием статистической отчётности по бактериологическим исследованиям и аналитических данных компьютерного программного обеспечения WHONET 5.6. Результаты. Основные возбудители ГСИ в ОТО – микроорганизмы группы ESKAPE: E. coli (3,56 %), S. aureus (18,38 %), K. pneumoniaе (7,71 %), A. baumannii (12,65 %), E. faecalis (12,45 %), P. aeruginosa (9,09 %), – а также S. epidermidis (10,87 %), P. mirabilis (2,4 %), C. amycolatum (2,6 %). Культуры E. faecalis показали чувствительность к ванкомицину, линезолиду, S. aureus – к линезолиду, тигециклину, нетилмицину, A. baumannii – к тигециклину. Штаммы P. aeruginosa, E. coli и K. pneumoniaе были резистентны к большинству антибиотиков. Все псевдомонады были устойчивы к тикарциллину/клавуланату, цефепиму, хлорамфениколу, имипенему, меропенему, азтреонаму, ципрофлоксацину, 71 % штаммов проявили устойчивость к пиперациллину/тазобактаму, 89 % – к левофлоксацину; чувствительными к гентамицину были 46 % изолятов, к амикацину – 59 %. E. coli и K. pneumoniaе резистентны к ампициллину, тикарциллину/клавуланату, азтреонаму, цефтриаксону, цефепиму; количество штаммов, чувствительных к пиперациллину/тазобактаму, карбапенемам, левофлоксацину, гентамицину, амикацину, хлорамфениколу, – 37–65 %. Выводы. В структуре возбудителей ГСИ ортопедо-травматологического отделения запорожской КНП «ГБЭ и СМП» важную роль играют E. coli, S. aureus, K. pneumoniaе, A. baumannii, E. faecalis, P. aeruginosa, S. epidermidis, P. mirabilis, C. amycolatum. Препараты выбора для антибактериальной эмпирической терапии энтерококковых инфекций – ванкомицин, линезолид, стафилококковых – ванкомицин, линезолид, тигециклин, нетилмицин. Постоянный процесс изменения резистентности возбудителей ГСИ делает крайне важным мониторинг антибиотикочувствительности микроорганизмов, циркулирующих в условиях ОТО.

The aim. To study the expression of mRNA of the NLRP3 inflammasome and proinflammatory cytokine IL-1β in the inflamed colon of rats with experimental oxazolone-induced colitis and against the background of the introduction of simvastatin and antagonist of interleukin-1 receptors. Materials and methods. Experiments were carried out on male Wistar rats aged 8 months (body mass 120–150 g). Tissue samples were obtained from rats with experimental oxazolone-induced colitis (n = 20), rats with oxazolone-induced colitis treated with simvastatin (n = 20); rats with oxazolone-induced colitis treated with interleukin-1 receptor antagonist (n = 20) and control animals (n = 10). Clinical signs of colitis were evaluated by the clinical index of disease activity on the following parameters: weight loss, stool consistency and animal behavior. For macroscopic assessment of the development of colitis areas of inflammation and ulceration were investigated. For histological evaluation of lesions, sections of the intestine were stained with hematoxylin and eosin and cellular inflammatory infiltrates, epithelial hyperplasia, ulceration and loss of intestinal glands were studied. IL-1β and NLRP3 inflammasome mRNA expression was analyzed by real-time reverse transcriptase-polymerase chain reaction. Results. Animals treated with oxazolone rapidly developed colitis marked by weight loss and diarrhea peaking by day 2 after oxazolone administration and leading to death of 40 % of the rats by day 4. The histological observation showed inflammatory cell infiltration, including polymorphonuclear leukocytes and multiple erosive lesions in the large intestine. We determined that the expression level of the proinflammatory cytokine IL-1β is increased in colon samples of rats with oxazolone-induced colitis. IL-1β expression is increased 3.5‐fold in inflamed colon compared to uninflamed tissue. Administration of simvastatin and an interleukin-1 receptor antagonist to rats with oxazolone-induced colitis resulted in a 30 % and 2-fold decrease expression of IL-1β in colon samples. In addition, we examined NLRP3 expression in these tissues. RT‐PCR analysis demonstrates a 71‐fold increased expression of NLRP3 mRNA expression in colon samples tested. Administration of simvastatin and an interleukin-1 receptor antagonist to rats with oxazolone-induced colitis resulted in a 2.5- to 3.0-fold decrease expression of NLRP3 mRNA in colon samples. Conclusions. IL-1β and NLRP3 mRNA expression levels were elevated in the inflamed colon of rats with experimental oxazolone-induced colitis. Administration of simvastatin and an interleukin-1 receptor antagonist against the background of colitis caused a decrease in the expression levels of IL-1β and NLRP3 mRNA in the tissues of the intestine. Detection of abnormal expression of IL-1β and NLRP3 mRNA could provide insights into pathogenesis of Crohn's disease, and may help to identify future potential targets for therapeutic strategies in people with inflammatory bowel disease.