Current issues in pharmacy and medicine: science and practice最新文献

{"title":"Age dynamics of strain differences in the morphofunctional state of pancreatic beta- and amylin-producing cells in SHR and Wistar rats","authors":"B. T. A. Hrekova A, Ye. V. Kadzharian, Т. А. Грекова, О. В. Мельнікова, Єлизавета Віталіївна Каджарян","doi":"10.14739/2409-2932.2023.3.286820","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.3.286820","url":null,"abstract":"Large-scale epidemiological studies have shown that cardiac pathology and progressive atherosclerosis in patients with diabetes mellitus occurred already at the stage of prediabetes. Obesity and insulin resistance affect cardiometabolic health due to pleiotropic effects of insulin. Despite the vast range of research, some aspects remain hidden links in the overall pathogenesis of metabolic and hemodynamic disorders. The aim of the work was to study the morphofunctional state of pancreatic islets (PIs), beta- and amylin-producing cells in male rats of Wistar strain (normotensive) and SHR (with spontaneous development of hypertension) in age dynamics. Materials and methods. The study was carried out using 38 male Wistar rats and SHRs aged 7 and 24 months. Non-invasive blood pressure (BP) detection procedures were done using the BP-2000 Blood Pressure Analysis System. The morphofunctional state of PIs was examined in serial 5-μm thick pancreatic tissue sections. Beta- and amylin-producing cells were detected after histological preprocessing and the use of monoclonal FITC-conjugated antibodies. Image file processing was done via ImageJ software (National Institutes of Health, USA). Levels of glycemia were monitored with a SUPER GLUCOCARD-II glucometer. Results. SHRs were hyperglycemic both at 7 and at 24 months, 8.41 ± 0.15 mmol/l and 8.90 ± 0.14 mmol/l, respectively, with elevated BP, 155 ± 5 / 80 ± 5 mm Hg and 165 ± 5 / 90 ± 5 mm, respectively. Old SHRs developed PI hypertrophy mainly associated with the increased number and percentage of beta-cells, apparently in response to hyperglycemia. Both in the PIs of adult and old SHRs, the number of amylin-producing cells was lower while the content of amylin was higher than those in the age-matched Wistar rats. Conclusions. Male SHRs are characterized by a persistent increase in blood pressure and abnormalities of carbohydrate metabolism already at adult age, one of the manifestations of which is hyperglycemia worsening with age. Chronic hyperglycemia in SHRs due to the higher insulin requirement finds its expression in low content of this hormone in the islets at adult age and decreased its content in beta-cells in old animals.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"78 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-11-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139289637","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"External reference pricing for medicines in Ukraine: latest trends","authors":"L. Kucherenko, EF I. V. Nizhenkovska A, EF N. V. Sholoiko A, CE L. O. Hala A, CE N. O. Datsiuk A, Л. І. Кучеренко, І. В. Ніженковська, Н. В. Шолойко, Л. О. Гала, Н. О. Дацюк","doi":"10.14739/2409-2932.2023.3.287758","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.3.287758","url":null,"abstract":"Compared to the previous year, the share of healthcare expenditure in the state budget of Ukraine has decreased, which is associated with increased funding for the security and defense sector. In terms of gross domestic product, healthcare spending has reduced to 2.8 %, which corresponds to the figures for 2019. These circumstances indicate the importance of proper budget utilization, including effectively regulating medicine prices. One of the key elements of rational healthcare budget usage is the development and implementation of external reference pricing (ERP). A well-formulated and implemented ERP policy for pharmaceuticals contributes to improving patient access to essential medicines (EMs). The aim of this study is to analyze the current status of ERP implementation in Ukraine and provide recommendations for improving this policy. Materials and methods. During the research process, an analysis of the ERP’s current regulatory framework was conducted, and ERP implementation in Ukraine was assessed according to adherence to the 14 best practice principles of ERP proposed by Sullivan, Kanavos & Kalo in 2015. Results. In Ukraine, ERP has been introduced for medicines from the National Essential Medicine Lists (NEML) and the “Affordable Medicines” program. The Ministry of Health (MoH) of Ukraine has approved a Register of marginal wholesale prices for medicines purchased with state budget funds and subject to price regulation. Currently, the register includes 1239 medicinal products, of which 1233 are from NEML and 6 have undergone Health Technology Assessment (HTA). Approximately 58 % of medicines have a set price through ERP, 24 % are regulated by internal reference pricing (IRP), and nearly 18 % have declared prices. This indicates a lack of uniformity in approaches to price regulation for medicines and requires further improvements. According to the latest update of the Register of medicines for reimbursement under the state medical guarantees program, there are 486 medicines, including 72 insulins and 21 immunosuppressive medicines (184 medicines are provided with co-payment). Different approaches, including different reference countries and price calculation algorithms, are applied for the price regulation of medicines in NEML and the “Affordable Medicines” program. An assessment of the implementation of the ERP system in Ukraine based on the 14 best practice principles of ERP proposed by Sullivan, Kanavos & Kalo in 2015 showed that the current policy does not adhere to all principles. Conclusions. The analysis revealed different approaches to pricing for medicines NEML and the “Affordable Medicines” program, indicating the need for harmonizing pricing policies for different lists. The adoption of a unified positive list can contribute to improving pricing policies and efficient resource utilization. Collecting, disseminating, and exchanging data on drug prices is crucial to support transparency in pricing and its control. Regular monitor","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"111 19 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-11-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139289795","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Justification of the choice of excipients during the development of the composition of “Pastinocard” tablets","authors":"N. А. Symonenko, O. Shpychak, O. Kukhtenko, Ye. A. Bezrukavyi, H. B. Yurieva","doi":"10.14739/2409-2932.2023.3.287001","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.3.287001","url":null,"abstract":"The aim of the work is to justify the choice of excipients as components for the cardioprotective medicine “Pastinocard” tablets based on the domestic raw material of cultivated parsnip herb thick extract (CPHTE). Materials and methods. Experimental test samples of mixtures of the plant substance of domestic origin CPHTE with groups of excipients, approved for medical use, were used as the object of research. Results. We conducted experimental research by a mathematical planning method called the Greek–Latin square. In this study, we investigated how 16 different auxiliary substances affected the pharmacotechnological properties of tableting masses and tablets made from PPTEG with cardioprotective properties. Our goal was to determine the optimal composition and manufacturing process for a medication, specifically “Pastinocard” tablets. We also developed project plans for manufacturing regulations and quality control methods, which we successfully tested in the industrial production setting at Pharmaceutical Company “Zdorovye”, LTD in Kharkiv. Conclusions. The formulation for cardioprotective tablets, designated as “Pastinocard”, has been both theoretically justified and experimentally developed by domestic CPHTE raw materials. These research findings have been instrumental in crafting the regulatory documentation for quality control and the production processes of the resulting tablet medication.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"182 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-11-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139289928","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"On the issue of criminal liability in the national pharmaceutical sector: theoretical foundations and practical aspects","authors":"O. H. Aleksieiev","doi":"10.14739/2409-2932.2023.3.285957","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.3.285957","url":null,"abstract":"A separate segment in the activity of streamlining, stability, and protection of relations arising in the pharmaceutical sphere should be noted the state’s reaction to criminal offenses and, accordingly, the assessment of the actions of persons who commit such offenses. The aim of the work – is to study the current issues of regulatory and legal support of criminal liability in the pharmaceutical sector. Results. The theoretical nature of the criminal responsibility of pharmaceutical workers is revealed from not only legal but also social and moral positions. The legal basis for the status of pharmaceutical workers as distinct subjects of criminal activity is underscored. It has been proven that the object of crimes committed by pharmaceutical workers as a special subject is, first of all, social relations arising in the sphere of human life and health protection; public health (public health); relations arising during the circulation of narcotic drugs, psychotropic substances, and precursors. Differences in terminology defining the object of pharmaceutical crimes are emphasized. Conclusions. The main aspects determining the problem of the qualification of crimes committed in the pharmaceutical sector of the healthcare industry were analyzed. From the standpoint of criminal law theory, the object, subject, objective, and subjective sides of pharmaceutical crimes were characterized.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"239 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-11-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139290034","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development of a method of quantitative determination of the active substance in Angiolin eye drops by the method of high-performance liquid chromatography","authors":"L. Kucherenko, R. R. Akopian, O. Portna, O. Khromylova, I. Pavliuk","doi":"10.14739/2409-2932.2023.3.288356","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.3.288356","url":null,"abstract":"One of the most common eye diseases is a burn injury. Hence, one of the pressing challenges in the field of pharmacy today is the development of new ophthalmic medications, specifically eye drops. Researchers from the Department of Pharmaceutical, Organic, and Bioorganic Chemistry at Zaporizhzhia State Medical and Pharmaceutical University, led by Professor I. A. Mazur, have successfully synthesized a novel compound. This compound is a derivative of 1,2,4-triazole, specifically (S)-2,6-diaminohexanoic acid 3-methyl-1,2,4-triazolyl-5-thioacetate. Notably, this compound demonstrates anti-inflammatory, wound-healing, and reparative activities. The aim of the work is to develop a method of quantitative determination of the active substance in Angiolin eye drops by the method of high-performance liquid chromatography. Materials and methods. The research employed a liquid chromatograph equipped with a UV detector. A column Hypersil ODS C-18 measuring 250 by 4.6 millimeters with a particle size of 5 microns was used. Results. It was determined that the angiolin content in the 1 % eye drops in series 1 falls within the range of 0.985 to 1.010 grams. This indicates that, in terms of the active substance content, the studied series complies with the requirements of the State Pharmacopoeia of Ukraine. Conclusions. As a result of the conducted research, a method for quantitatively determining the active substance in Angiolin eye drops using high-performance liquid chromatography was developed.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"48 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-11-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139289927","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The influence of new 1,2,3-triazolo-1,4-benzodiazepine derivatives on the muscle tone of rodents","authors":"I. V. Botsula, I. Kireyev, O. Koshovyi, V. Chebanov","doi":"10.14739/2409-2932.2023.3.287999","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.3.287999","url":null,"abstract":"Anxiety disorders represent one of the most prevalent categories of psychiatric illnesses, affecting individuals regardless of gender, age, or social standing. They result in substantial personal and societal costs. The pursuit of novel pharmacological approaches for treating these disorders is driven by the increasing medical necessity to enhance the effectiveness and safety profiles of anxiolytic medications. Due to the fact that benzodiazepines and their derivatives have anti-anxiety, hypnotic-sedative, antidepressant, anticonvulsant, and muscle relaxant properties, they occupy a leading place in the treatment of anxiety disorders. An essential aspect of investigating the pharmacological activity of new triazolobenziazepine derivatives is assessing their impact on rodent muscle tone and coordination of movements. The aim of the work is to find out the influence of new 1,2,3-triazolo-1,4-benzodiazepine derivatives on the muscle tone of rodents in the “vertical grid” test and coordination of movements using the rotarod test. Materials and methods. The objects of the study were 5 new derivatives of 1,2,3-triazolo-1,4-benzodiazepines. Before conducting in vivo experiments, these derivatives were mixed with lactose at a ratio of 1:1000. The “vertical grid” test and rotarod test (rotating rod test) were used to reproduce the model of motor behavior of rodents. Results. The presence of a tendency to the manifestation of a myorelaxant effect in the “vertical grid” test was established. The indicator of the total duration of detention at the facilities was similar and did not differ significantly in the control and experimental groups at doses of 0.50 mg/kg and 0.75 mg/kg. Derivatives MA-252, MA-253 and MA-254 at a dose of 1 mg/kg reduced the total duration of retention on the vertical grid, which indicates their mild muscle relaxant effect. In the rotating rod test, MA-253 derivative at a dose of 1 mg/kg increased the retention time on the rotarod, which demonstrates greater physical endurance of the animals of these experimental groups. Conclusions. The study’s findings indicated that the 1,2,3-triazolo-1,4-benzodiazepine derivatives did not exhibit an adverse impact on movement coordination. Some of these derivatives demonstrated a mild muscle relaxant effect. These results support the need for further research into their influence on spontaneous motor activity. Additionally, there’s a necessity to determine the dosage regimen, establish an effective dose, and adapt it for human use.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"2 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-11-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139290110","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The role and place of the pharmacist-cosmetologist in the choosing and implementation of a cosmetology procedure for hair removal","authors":"N. Tkachenko, T. Mahanova, H. I. Makurina, N. V. Hrinivetska","doi":"10.14739/2409-2932.2023.3.286688","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.3.286688","url":null,"abstract":"In modern cosmetology, the issue of the availability of highly qualified specialists in accordance with the needs of the industry and the implementation of effective cosmetology procedures is acute, which actualizes research on the formation of a patient-centered model of providing medical and pharmaceutical assistance of aesthetic cosmetology. The aim of the work is to substantiate the role and place of the pharmacist-cosmetologist in the selection and provision of a cosmetology procedure for hair removal (CPHR) based on a conjoint analysis of consumer preferences for the specified service. Materials and methods. The main research material for this study included publications by both domestic and foreign scientists concerning aesthetic cosmetology services, consumer behavior regarding cosmetology procedures, professional competencies expected of a pharmacist-cosmetologist, as well as the results of a sociological survey conducted by the CPHR. The research methods employed in this study encompassed information search, synthesis, generalization, formalization, modeling, questionnaires, and regular conjoint analysis. Results. The most attractive methods of epilation were determined – electro epilation, elos epilation and laser epilation. It was established that the majority of consumers do not need a preliminary cosmetologist consultation, but want a consultation after. An algorithm for accompanying CPHR by a pharmacist-cosmetologist was developed. The relevant aspects of pharmaceutical care of CPHR were defined. Conclusions. The conducted conjoint analysis indicates that women are primarily focused on the effectiveness of CPHR (electro epilation, elos epilation, and laser epilation are considered the most effective) and its cost, and then – on the supporting component of the service. The specialist can offer the client (patient) the choice of a method and directly carry out the procedure, having knowledge and experience in diagnosing the condition of the skin and its appendages and understanding the specifics of CPHR against the background of the pharmacoeconomic analysis. The modern Ukrainian model of pharmacist-cosmetologist training allows marketing requirements and accompanying the customer at CPHR. Prospects for further research – formation of an information array and development of pharmaceutical care (assistance) protocols for a pharmacist-cosmetologist in various cosmetic procedures.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"185 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-11-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139289765","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthesis and analgesic activity of new pyrazole-containing derivatives of 1,2,4-triazole-3-thiol","authors":"S. Fedotov, A. S. Hotsulia, Y. Karpenko","doi":"10.14739/2409-2932.2023.3.288364","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.3.288364","url":null,"abstract":"Pain represents a primary symptom of numerous diseases and conditions, affecting millions of people worldwide. Effective analgesic medications can alleviate or eliminate pain, thereby enhancing patients’ quality of life and assisting them in resuming normal physical and social activities. However, several existing analgesics may carry unwanted side effects, such as ulcers, blood clotting issues, drowsiness, and more. The development of new analgesics is focused on creating drugs that are both effective and associated with fewer adverse effects. Considering the continuous rise in the number of patients dealing with neurological, oncological, and other conditions accompanied by chronic pain, there is a growing demand for innovative methods of treatment and pain management. The combination of two different heterocyclic fragments within one molecule makes it possible to use the possibilities of influencing such a molecule on various mechanisms of occurrence and development of various pathological conditions, including those accompanied by pain. Chemical modifications of pyrazole and 1,2,4-triazole structures, involving their incorporation into a single molecule, have the potential, as suggested by in silico predictions, to yield biologically active compounds with analgesic properties. The aim of this work was to determine the optimal conditions for the chemical transformation and properties of 4-amino-5-(3-methylpyrazol-5-yl)-1,2,4-triazole-3-thiol, 4-amino-5-(3-(3-fluorophenyl)pyrazol-5-yl)-1,2,4-triazole-3-thiol and their derivatives for the preparation of bioactive systems with analgesic activity. Materials and methods. The creation of a target series of compounds was implemented by consistently using well-known methods of organic synthesis. 4-Amino-5-(3-methylpyrazole-5-yl)-1,2,4-triazole-3-thiol and 4-amino-5-(3-(3-fluorophenyl)pyrazole-5-yl)-1,2,4-triazole-3-thiol were resynthesized as starting materials using acetone or 1-(3-fluorophenyl)ethane-1-one, diethyloxalate, and sodium methylate using step-by-step hydrazinolysis and carbon disulfide involvement in an alkaline medium. Further targeted functionalization involved the introduction of a 2,6-dichlorophenyl substitute, alkane acid residues, and esters based on them into the structure of the target compounds. The structure of all synthesized substances was determined by IR spectrophotometry, 1H NMR spectroscopy, and elemental analysis. The individuality of the compounds was confirmed by high-performance liquid chromatography-mass spectrometry. The analgesic properties were studied on two models: the “acetic acid-induced writhing test” and a formalin model of pain inflammation. Pharmacokinetic parameters were predictably calculated using the SwissADME online platform. Results. Based on the results of the synthetic part of the work, the structure of 4-amino-5-(3-methylpyrazole-5-yl)-1,2,4-triazole-3-thiol and 4-amino-5-(3-(3-fluorophenyl)pyrazole-5-yl)-1,2,4-triazole-3-thiol, as well as their d","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"300 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-11-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139290028","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Antioxidant, antimicrobial and antifungal activity of the obtained “Cachisept” tablets for resorption in the oral cavity for the treatment and prevention of dental caries","authors":"O. Maslov, BD M. A. Komisarenko A, BD S. V. Ponomarenko A, BD V. Kolisnyk A, F. T. P. O. E, F. T. A. K. E, Yu. S. Kolisnyk, V. Moroz, О. Ю. Маслов, М. А. Комісаренко, С. В. Пономаренко, С. В. Колісник, Т. П. Осолодченко, Т. А. Костіна, Ю. С. Колісник, В. П. Мороз","doi":"10.14739/2409-2932.2023.3.285425","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.3.285425","url":null,"abstract":"Dental caries stands as a highly common chronic ailment affecting individuals globally, with susceptibility to this condition spanning their entire lifespan. Consequently, the search for novel medications aimed at treating and preventing dental caries holds significant importance in the field of pharmacy. The aim of the work was to study the antioxidant, antimicrobial, and antifungal activity of the obtained oral tablets “Сaсhisept” for resorption in the oral cavity for the treatment and prevention of dental caries. Materials and methods. The obtained tablets “Сaсhisept” with green tea leaf extract were the object of investigation. Antioxidant activity was established by the potentiometric method, and antimicrobial and antifungal activity was assessed by the agar well diffusion method. Results. The level of antioxidant activity for tablets “Сaсhisept” was 110.00 ± 2.20 mmol-eqv./mdry res, the obtained tablets had a high level of antioxidant activity according to Maslov’s conditional classification. Staphylococcus aureus (25.33 ± 0.50 mm), Baсillus subtilis (25.33 ± 0.50 mm) and Streptococcus mutans (25.33 ± 0.50 mm) were the most sensitive to the obtained “Сaсhisept” tablets, and the least – Proteus vulgaris (20.67 ± 0.50 mm), and it was observed strong growth inhibition in relation to the fungus Candida albicans (20.00 ± 0.50 mm). Conclusions. The presented study has found that “Сaсhisept” tablets have a high level of antioxidant activity, and also have a high antimicrobial and antifungal effect against all investigated Gram-positive, Gram-negative bacteria, and the Candida albicans fungus. Thus, “Сaсhisept” tablets can be recommended for the treatment and prevention of dental caries.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"154 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-11-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139289656","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"In silico evaluation of the pharmacodynamic component of the interaction of S-alkyl derivatives of 5-methyl-4-(p-tolyl)-1,2,4-triazole-3-thiol with some biological targets","authors":"O. Panasenko, V. M. Odyntsova, A. S. Hotsulia","doi":"10.14739/2409-2932.2023.3.287510","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.3.287510","url":null,"abstract":"Derivatives of 1,2,4-triazole open wide opportunities for modern and progressive scientists in the development of innovative medicines. These compounds are known for their variability and structural flexibility, which allows scientists to experiment and create new molecules with unique properties. The use of 1,2,4-triazole derivatives in the creation of drugs is based on their ability to interact with biological systems and molecular targets. These compounds can be aimed at regulating physiological processes, reducing manifestations of pathological conditions or enhancing necessary biological reactions. Directed modification of the structure of 1,2,4-triazole derivatives allows to create biologically active compounds with improved properties. The aim of the work was to study in silico and to evaluate the possible interaction of a virtual series of S-alkyl derivatives of 5-methyl-4-(p-tolyl)-1,2,4-triazole-3-thiol with some enzyme systems. Materials and methods. A computer method (molecular docking) for predicting and evaluating the interaction between a ligand molecule and a target protein structure. Ligand preparation was performed using MarvinSketch 6.3.0, Hyper Chem 8, and AutoDockTools-1.5.6 programs. Enzyme preparation involved the use of Discovery Studio 4.0 and AutoDockTools-1.5.6 software packages. Direct molecular docking was performed using the Vina program. Results. A virtual series of S-alkyl derivatives of 5-methyl-4-(p-tolyl)-1,2,4-triazole-3-thiol with the potential possibility of creating a biologically active substance has been constructed. Using the Vina software tool, the nature and number of amino acid residues of the active centers of model enzymes, with which the proposed ligands coordinate and bind, were determined. According to the results of docking studies, the predicted affinity for lanosterol-14α-demethylase was determined. The effect on the receptor tyrosine kinase of anaplastic lymphoma is somewhat inferior in terms of qualitative and quantitative indicators. Conclusions. Using the method of molecular docking, it was established that S-alkyl derivatives of 5-methyl-4-(p-tolyl)-1,2,4-triazole-3-thiol have a fairly significant potential for the manifestation of antifungal activity, which justifies the further synthesis of these compounds and more in-depth study of fungistatic and fungicidal properties. Docking results for anaplastic lymphoma kinase show little promise in the development of anticancer agents.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-11-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139289791","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}