{"title":"Features of the planimetric organization of the endocrine part of the pancreas in hypertensive rats of the SHR line","authors":"T. Ivanenko","doi":"10.14739/2409-2932.2022.3.259868","DOIUrl":"https://doi.org/10.14739/2409-2932.2022.3.259868","url":null,"abstract":"Analysis of the endocrine structure of the pancreas and assessment of its degree of heterogeneity is key to assessing such important physiological parameters as islet endocrinocyte mass in healthy people or functional reserve of β-cells in patients with type 1 and type 2 diabetes.\u0000The aim of the study is to perform a comparative planimetric analysis of pancreatic islets of normotensive Wistar rats and hypertensive SHR rats, using the method of double immunofluorescent staining of endocrinocytes.\u0000Materials and methods. The study was performed on the pancreas of SHR and Wistar rats. Insulin and glucagon in the islets of the pancreas were determined by immunofluorescence. The immunofluorescence reaction was studied with an AxioImager-M2 fluorescent microscope.\u0000Results. Planimetric analysis showed the presence of pancreatic islets of all types in the pancreatic tissue of SHR and Wistar rats. The number of single endocrinocytes in SHR hypertensive animals was 2.3 times higher (P < 0.001), and the number of giant islets was 34.2 % higher (P < 0.001), than in normotensive Wistar rats. The presence of regions in some endocrinocytes, that show immunoreactivity to both hormones at once – insulin and glucagon. Such areas were present in islets of all types of both rat lines, however, the total rates in hypertensive rats of the SHR line were 21.8 % lower (P < 0.001), than in normotensive rats of the Wistar line.\u0000Conclusions. Planimetric analysis showed, that the pancreatic islets in normotensive Wistar rats and hypertensive SHR rats occupy 1.4 % of the cross-sectional area of the pancreas. In hypertensive rats the SHR line in the gland by 16.9 % larger total area of the material immunoreactive to insulin. In contrast to Wistar rats, the number of single α-endocrinocytes in the pancreas of hypertensive SHR rats was significantly increased.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"800 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78880685","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 renal function in men with hypertension in conditions of purine and carbohydrate metabolism disorders","authors":"O. Dudko, M. Kolesnyk","doi":"10.14739/2409-2932.2022.3.266580","DOIUrl":"https://doi.org/10.14739/2409-2932.2022.3.266580","url":null,"abstract":"Aim. To assess the condition of renal function in hypertensive men in conditions of disorders of purine and carbohydrate metabolism\u0000Material and methods. 60 male patients (aged from 18 to 65 years) with stage I–II of arterial hypertension (AH) and purine and carbohydrate metabolism disorders were examined. In these patients, the level of uric acid (UA) in daily urine, fractional excretion of UA, creatinine in daily urine, microalbumin in urine and the cystatin C level were determined. Hemodynamics was studied by daily blood pressure monitoring. Assessment of kinetics and deformation of the myocardium in offline mode using the Xstrain software package integrated into the ultrasound device (Esaote, Italy) was made. Patients were divided into 2 clinical groups – 1 group of AH with hyperuricemia, 2 – AH without uricemia. Statistical analysis of the results was performed using the Statistica 13.0 software package (Statsoft, USA).\u0000Results. Correlation analysis in group 1 showed a positive correlation of cystatin C with the average daytime systolic blood pressure (SBP) (r = 0.408) and the variability of diastolic blood pressure (DBP) at night (r = 0.405), urinary microalbumin with the average SBP at night (r = 0.390) and average pulse blood pressure (r = 0.402), LV posterior wall thickness (r = 0.438), LV myocardial mass index (r = 0.621), end-diastolic index (EDI) (r = 0.492), end-systolic index (ESI) (r = 0.426), LV anterior-posterior size (r = 0.385). A negative correlation was established between blood serum SC and ejection fraction (EF) of the LV (r = -0.410), urinary microalbumin with cardiac index (SI) (r = -0.555) and the speed of movement of the lateral (e’ lat) part of the annulus fibrosus mitral valve (r = -0.453).\u0000Conclusions. As a result of the studies, the negative influence of hyperuricemia and hyperglycemia in patients with AH on renal function was established. These changes were evidenced by an increase in microalbuminuria level, a decrease in the fractional excretion of UA, an increasing the serum UA level, remodeling of the myocardium, and worsening of the heart systolic function, worsening of the daily blood pressure profile.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"46 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86522181","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}
T. Brytanova, T. P. Zarichna, A. S. Hotsulia, Yuliia Shostak
{"title":"Study of the preferences of doctors and pharmacists regarding medicines for the treatment of diseases of the peripheral nervous system","authors":"T. Brytanova, T. P. Zarichna, A. S. Hotsulia, Yuliia Shostak","doi":"10.14739/2409-2932.2022.3.263550","DOIUrl":"https://doi.org/10.14739/2409-2932.2022.3.263550","url":null,"abstract":"The aim of the work is to assess the preferences of doctors and pharmaceutical workers regarding drugs for the treatment of diseases of the peripheral nervous system in order to optimize the medical supply of the population.\u0000Materials and methods. Data from the State Register of Medicines of Ukraine, Compendium-online, questionnaires of neurologists and pharmaceutical workers were used in this research. The search systematic, analytical, qualimetric, comparative, statistical analyses were used in the work.\u0000Results. The results of a survey of neurologists revealed that for the treatment of diseases of the peripheral nervous system (radiculopathy, radiculalgia) the most effective treatment regimen is that, which includes “Nucleo CMF Forte”, “Celtican” and “Myelofan”. The effectiveness and safety of the studied drugs were confirmed by qualimetric analysis. However, the results of consumer surveys showed that the latter prefer a treatment regimen that contains “Dicloberl”, “Ketanov” and “Dexalgin”. These drugs are the most irrational in terms of side effects and contraindications. For consumers, the importance of the pharmacological effect outweighs the effects on the body from the side effects of drugs.\u0000Conclusions. The study of the preferences of doctors and pharmacists regarding medicines for the treatment of radiculopathy and radiculalgia was conducted. The most rational treatment regimens are identified, the effectiveness of which is confirmed by the method of qualitative analysis.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"91 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86082401","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}
O. Grechana, A. Serbin, O. O. Salii, A. Rudnyk, I. Shevchenko, L. Fukleva
{"title":"Pharmacognostic studies of Trifolium fragiferum L. flora of Southern Ukraine","authors":"O. Grechana, A. Serbin, O. O. Salii, A. Rudnyk, I. Shevchenko, L. Fukleva","doi":"10.14739/2409-2932.2022.3.259400","DOIUrl":"https://doi.org/10.14739/2409-2932.2022.3.259400","url":null,"abstract":"The work is devoted to the study of herbs of the representative genus Clover Trifolium fragiferum L. from the south Ukrainian flora.\u0000The aim of this research is to investigate the representative of Southern Ukraine flora Trifolium fragiferum L. which has a sufficient raw material base and use in folk medicine.\u0000Materials and methods. Samples were grown in the suburbs of Zaporizhzhia and harvested during full flowering (May – June). Microscopic analysis was performed with temporary preparations of leaves and stems. Plant extracts were analyzed chromatographically using an Agilent Technologies 6890 gas chromatograph with mass spectrometric detection.\u0000Results. The leaf is covered with parenchymal cells with slightly thickened membranes with anocytic stomata. The main parenchyma is composed of rounded toxoid cells. Stem rounded, covered with elongated parenchymal cells with thin membranes with almost no stomata and pubescence. Central axial cylinder is of beam type. Beams are open collateral, large. Above the phloem of the bundles is a multilayered sclerenchyma. The core is partially filled, hollow in the center. 63 compounds were found in the native extract, of which 37 were identified: coumarins, fatty acids, diterpene alcohols, oxygenated hydrocarbons of terpenoid nature, higher hydrocarbons, representatives of phytosterols, and phytosterols. After acid hydrolysis with sulfuric acid, 58 compounds were found, of which 49 were identified: coumarins, alcohols and phenols, aldehydes and ketones, compounds of diterpene nature.\u0000Conclusions. Pharmacognostic analysis of the genus Clover Trifolium fragiferum L. revealed diagnostic microscopic signs of leaves and stems. The components of the native extract are compared, and after its acid hydrolysis. Certain regularities in the distribution of classes of substances that characterized certain types of extracts were revealed: monoterpenoids, aromatic, heterocyclic compounds characterized the hydrolyzed product. Sesquiterpenes and steroid compounds are found only in the native extract of strawberry clover herb. Alcohols, aldehydes, and ketones were the majority in the hydrolyzed extract, and hydrocarbons were observed more in the native. Only 5 components were identified in both extracts: nonacosan, 2-phenoxyethanol, loliolide, dihydroactinidiolide and coumarin with significant differences in amounts.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"78 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73438157","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 results of determining the indicators of the morphological composition of the blood of animals and individual biochemical indicators using a potential drug with a mixture of two active compounds: 4-((5-(decylthio)-4-methyl-4H-1,2,4-triazole-3-yl)methyl)morpholine and 5-(2-fluorophenyl)-4-((4-bro","authors":"M. V. Ohloblina, I. V. Bushuieva, V. Parchenko","doi":"10.14739/2409-2932.2022.3.263015","DOIUrl":"https://doi.org/10.14739/2409-2932.2022.3.263015","url":null,"abstract":"The introduction of new domestic highly effective and safe medicines into medical and veterinary practice is an important task of modern pharmaceutical science. Continuation of the search and conduct of research to bring the biological activity of 1,2,4-triazole derivatives is one of the promising areas of such activity. At this stage of research, it is known that such 1,2,4-triazole derivatives as 4-((5-(decylthio)-4-methyl-4H-1,2,4-triazole-3-yl)methyl)morpholine and 5-(2-fluorophenyl)-4-((4-bromophenyl)ylidene)amino-1,2,4-triazole-3-thiol have a wide spectrum of biological activity. Interest for further thorough research is precisely the antimicrobial and antifungal effects. The introduction into medical and veterinary practice of newly created drugs for the treatment of fungal diseases on the skin of animals requires further studies of the properties of these compounds and their mixtures.\u0000The aim of the work was to determine the indicators of the morphological composition of the blood of animals and individual biochemical indicators when using a preparation with a mixture of two active compounds: 4-((5-(decylthio)-4-methyl-4H-1,2,4-triazole-3-yl)methyl)morpholine and 5-(2-fluorophenyl)-4-((4-bromophenyl)ylidene)amino-1,2,4-triazole-3-thiol in thistle seed oil.\u0000Materials and methods. The material for laboratory research was serum and blood plasma, stabilized by adding trilon-B, tissue biopsy. Indicators were determined in healthy animals and experimentally diseased animals on the third and tenth days after the onset of the disease according to the generally accepted method. During the research, in the course of treatment, general clinical examinations and local examinations of purulent wounds were carried out, as well as blood samples taken from each head of the sheep in the experimental and control groups before the beginning and on the third and tenth days of the experiment. The purulent-inflammatory process was caused by injuring the soft tissues in the groin area on the left side, with the help of a specially made template, followed by dilation of the muscle tissue with an angiotrip and implantation of aerobic-anaerobic surgical infection cultures taken from the bed. The resulting wounds had the following dimensions: 10 cm in length, 1 cm in width, and 2 cm in depth. As early as 24 hours after induction of experimental purulent inflammation, characteristic clinical signs appeared in sheep. The general condition of all 12 animals was somewhat depressed, the appetite was normal. The body temperature was in the range of 38.6–40.3 °C, the pulse was 76–82 beats, and the frequency of respiratory movements was 16–18 per minute. The frequency of scar contractions was 3–6 times in 2 minutes. During the examination, slight swelling was also found in the area of the wound and its edges. There was a small amount of serous-bloody exudate on the surface of the wound. On the 3rd day, the maximum manifestation of clinical signs of acute purulent inflammat","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"63 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84684365","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 and validation method for the determination of related substances in nimesulide granules for oral suspension","authors":"K. Tarapon, O. Tryhubchak","doi":"10.14739/2409-2932.2022.3.259472","DOIUrl":"https://doi.org/10.14739/2409-2932.2022.3.259472","url":null,"abstract":"One of the key stages of pharmaceutical development is the development of analytical methods for quality control of medicines. The critical quality indicator is the content of related impurities, which may increase during shelf life of the product due to the degradation of the active substance, which in turn affects the quality of the product.\u0000The aim of the work is to develop and validate the method for the determination of related impurities in nimesulide granules for oral suspension by HPLC method; to set the specification of finished product for related impurities.\u0000Materials and methods. Sample of finish product Nimesulide, granules for oral suspension, 100 mg/2 g, it was manufactured by JSC “Farmak”. The study was performed using Agilent 1260 liquid chromatograph with UV detector. 2-phenoxyaniline from Sigma-Aldrich, reference standards of nimesulide impurity D EP CRS and LGC, Nimesulide for peak identification EP CRS were used for preparation of standard impurity solutions. Acetonitrile and ammonium dihydrogen phosphate from Sigma-Aldrich were used for chromatographic analysis.\u0000Results. When developing method, the concentrations of solutions, the method of dissolving granules, filters were selected. The chromatographic column was selected, the requirements for the chromatographic system suitability were set. The effect of placebo components has been studied and considered. During the validation the characteristics were studied: specificity, linearity, LOD, LOQ, precision, accuracy, robustness. The limits of the impurity content were established in accordance with the requirements of ICH Q3B guideline, taking into account the data of stress studies, stability and impurities of the substance.\u0000Conclusions. The analytical method for the determination of related substances in finish product nimesulide granules for oral suspension was developed. The validation results showed that the method is suitable for analysis. The specification limits of finished product for related impurities were set.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"55 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89684509","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 properties of 3-(ethylthio)-9-methyl-6-(alkylthio)pyrazolo[1,5-d][1,2,4]triazolo[3,4-f][1,2,4]triazines","authors":"S. Fedotov, C. A. S. Hotsulia A","doi":"10.14739/2409-2932.2022.3.263994","DOIUrl":"https://doi.org/10.14739/2409-2932.2022.3.263994","url":null,"abstract":"The combination of pyrazole and 1,2,4-triazole fragments in one structure makes it possible to achieve some success in creating potential biologically active compounds. Various factors contribute to this process. Among them, we can note the significant possibilities of chemical transformation involving these cycles, the simplicity, and reliability of methods, the creation of molecules with a certain level of bioavailability and the ability to influence a number of biochemical processes. Taking into account the presented facts, the creation of new compounds in a number of pyrazolo-triazole condensed systems is scientifically attractive with endowed features of practical significance and relevance.\u0000The aim of the work was to identify optimal conditions for the production of 3-(ethylthio)-9-methyl-6-(alkylthio)pyrazolo[1,5-d][1,2,4]triazolo[3,4-f][1,2,4]triazines and to study the properties of the target reaction products.\u0000Materials and methods. The chemical part of the work involved the step-by-step creation of target reaction products in the form of 3-(ethylthio)-9-methyl-6-(alkylthio)pyrazolo[1,5-d][1,2,4]triazolo[3,4-f][1,2,4]triazines. The first stage was aimed at conducting the interaction of diethyloxalate with acetone with the participation of sodium methylate in a methanol medium. Ethyl-2,4-dioxopentanoate was used in the conversion process to 3-methylpyrazole-5-carbohydrazide with the participation of hydrazine hydrate. Further modification of the molecule consisted of the gradual formation of the structure of 4-amino-5-(3-methylpyrazol-5-yl)-1,2,4-triazole-3-thiol. The next step involved the synthesis of 3-ethylthio-5-(3-methylpyrazol-5-yl)-1,2,4-triazole-4-amine. Further conversion included the production of potassium 3-ethylthio-9-methylpyrazolo[1,5-d][1,2,4]triazolo[3,4-f][1,2,4]triazine-6-thiolate and its S-alkyl derivatives along the triazine fragment. Cyclooxygenase-2, lanosterol-14α-demethylase and receptor tyrosine kinase were selected as model enzymes for docking, the crystal structure of which was loaded from the Protein Data Bank.\u0000Results. The synthesis of 3-(ethylthio)-9-methyl-6-(alkylthio)-pyrazolo[1,5-d][1,2,4]triazolo[3,4-f][1,2,4]triazines were carried out and the optimal conditions for the production of these substances were determined. The structure of the chemical transformation products was proved and the results of the study of the main physical properties were recorded. The results of virtual studies provided an opportunity to substantiate the prospects of the selected chemical transformation vector, which ultimately made it possible to determine the biological potential of the obtained compounds.\u0000Conclusions. Based on the results of the study, information was obtained that gives a certain idea of the possible level of influence of synthesized compounds on the activity of lanosterol-14α-demethylase, which makes it advisable to further search for substances with fungistatic and fungicidal effects.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"49 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86925636","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}
I. V. Bushuieva, K. Petrova, B. Kyrychko, V. Parchenko
{"title":"Study of mutagenic effects with predicted carcinogenicity of 4-((5-decylthio)-4-methyl-4-H-1,2,4-triazole-3-yl)methyl)morpholine for further research in order to create a new drug with antifungal activity","authors":"I. V. Bushuieva, K. Petrova, B. Kyrychko, V. Parchenko","doi":"10.14739/2409-2932.2022.3.261790","DOIUrl":"https://doi.org/10.14739/2409-2932.2022.3.261790","url":null,"abstract":"The development of effective and safe therapeutic agents using 1,2,4-triazole derivatives is gaining momentum in today’s conditions. The value of such drugs is determined by the rapid and prolonged biological action, which is not accompanied by abrupt changes in homeostasis and pronounced side effects, which are characteristic of most pharmacological drugs of synthetic origin. In the context of a limited range of domestic antimicrobial and antifungal veterinary drugs on the national pharmaceutical market, one of the directions for solving this problem is the search, study, research, and development of drugs with antimicrobial and antifungal activity.\u0000The aim of this work was to study the mutagenic effects with the prediction of carcinogenicity of 4-((5-decylthio)-4-methyl-4-H-1,2,4-triazole-3-yl)methyl)morpholine with the prospect of further creation of new dosage forms for the treatment fungal pathologies of the skin.\u0000Materials and methods. Staph was used to study the effect of 4-((5-decylthio)-4-methyl-4-H-1,2,4-triazol-3-yl)methyl)morpholine in vitro Staphylococcus aureus, strain 209, its UV-2, UV-3 mutants and primary cell cultures. Accounting for gene mutations of microorganisms in the system of metabolic activation (Ames test) was carried out according to the method of L. M. Fonshtein in accordance with the requirements of “Methodological recommendations for assessing the mutagenic properties of new medicinal products” (Kyiv, 1996), supplemented by the methodology according to the recommendations of “Preclinical research of veterinary medicinal products” (edited by I. Ya. Kotsiumbas).\u0000Results. The results of studying the activity of 4-((5-decylthio)-4-methyl-4-H-1,2,4-triazole-3-yl)methyl)morpholine on a model of culture of tumor ascetic cells showed that at concentrations of 1.4 mg/ml, 0.8 mg/ml, 0.3 mg/ml, 0.015 mg/ml it was led to the regression of tumor cells of Ehrlich’s carcinoma and C-37 sarcoma. In experiments with the Nk/L y strain, the same concentrations of 4-((5-decylthio)-4-methyl-4-H-1,2,4-triazole-3-yl)methyl)morpholine significantly slowed down cell growth. The results of the studies indicate a pronounced cytogenetic effect of thiophosfamide and sarcolysin, which suggests their metabolic activation in the body, as evidenced by a pronounced aberration of chromosomes. When comparing the cytogenetic effect of equimolar concentrations, the absence of cytogenetic activity of 4-((5-decylthio)-4-methyl-4-H-1,2,4-triazole-3-yl)methyl)morpholine was revealed.\u0000Conclusions. The positive results of studying the specific activity of 4-((5-decylthio)-4-methyl-4-Н-1,2,4-triazole-3-yl)methyl)morpholine in experiments in vitro were obtained which indicates the expediency of its extensive study in experimental animal tumors. In addition, according to these studies, no mutagenic effect was found at the doses that were used to predict carcinogenicity. Thus, it can be concluded that there is no cytogenetic effect.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"65 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79877888","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}
V. Odyntsova, Yu. I. Korniievskyi, D. Skoryna, V. Н. Korniievska
{"title":"Chromato-mass spectroscopy of tinctures from the underground part of Valerian plants growing in Zaporizhzhia region","authors":"V. Odyntsova, Yu. I. Korniievskyi, D. Skoryna, V. Н. Korniievska","doi":"10.14739/2409-2932.2022.3.261819","DOIUrl":"https://doi.org/10.14739/2409-2932.2022.3.261819","url":null,"abstract":"Modern sedatives used in medical practice can be of both synthetic and natural origin. It is known that the best phytosedative is valerian. In the 18th century, valerian was included in all European pharmacopeias. High efficiency, good tolerability, and virtually no side effects ensure the widespread use of valerian and its phytopreparations in medical practice, especially for the treatment of geriatric patients. Despite this, valerian remains understudied due to its extreme polymorphism.\u0000The aim of the work is to determine the component composition of valerian tinctures made from rhizomes with valerian roots of different species growing in the Zaporizhzhia region by gas chromatography and to carry out their comparative analysis.\u0000Materials and methods. Samples of rhizomes with valerian roots made from medicinal plant raw materials of valerian according to the traditional production recipe (Tinctura Rhizomata cum radicibus Valerianae (1:5)) from different species of valerian growing in the Zaporizhzhia region were selected for experimental studies: Valerian stolonifera Czern. – Kantserivska Balka, Zaporizhzhia district, Zaporizhzhia region; V. exaltata Mikan. – Shyroke village, Vasylivskyi district, Zaporizhzhia region; V. tuberosa L. – Khortytsia Island, Zaporizhzhia; V. collina Wallr. – right bank of the Dnieper River, Zaporizhzhia. The component composition of valerian tinctures was studied using an Agilent 7890B gas chromatograph with a mass spectrometric detector 5977B.\u0000Results. The component composition of tinctures from the underground part of valerian plants growing in the Zaporizhzhia region was identified and analyzed with chromato-mass spectrometry.\u0000Conclusions. 55 components in valerian tincture from underground raw materials of Valeriana stolonifera Czern. were identified with gas chromatography: V. exaltata Mikan. – 48, V. tuberosa L. – 54, V. collina Wallr. – 51. Analyzing the obtained data, we can conclude that valerian tinctures differ in both quantitative and qualitative composition. Only compounds 7 and 9 coincide in tinctures from underground parts of all four types of valerian. Since the tinctures were made following the standard technology, the content of components in medicinal plant raw materials depends on the type, place of growth, environmental conditions, time of collection, drying of raw materials. The results of the study confirm the prospects of using the underground part of the studied plants of the genus Valerian to create new drugs and phytopreparations on their basis. However, given the extreme polymorphism of valerian for the introduction into the culture of promising species that grow in Ukraine, it is necessary to conduct more in-depth pharmacognostic and pharmacological studies of plants of this genus.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"55 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90683170","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":"DFT-analysis of protolytic equivalents of 5-(aryl)-4-(methyl,amino)-1,2,4-triazole-3(2H)-thione","authors":"O. A. Bihdan, N. A. Alk Khalaf","doi":"10.14739/2409-2932.2022.2.254474","DOIUrl":"https://doi.org/10.14739/2409-2932.2022.2.254474","url":null,"abstract":"The use of modern computer methods in aspects of quantum chemistry and systematic analysis of their results give an idea of the reactivity of organic compounds, as well as to understand the essence of known experimental data, correct predictions, and quantitative estimates. Undoubtedly, theoretical calculations are useful in solving such an urgent problem of modern chemistry as prototropic equilibria and properties of substances in the gas phase, solutions, and solid-state.\u0000The aim of the work – until recently assigned to a theoretical vivification in the infusion of solvents on tautomeric equilibrium and acid-base powers і know more broadly practical stasis in the pharmaceutical industry.\u0000Materials and methods. The effect of solvation effects on tautomerism and antitropic properties of 1,2,4-triazole derivatives was studied on the example of model compounds. All calculations were performed using the Gauss-View 6.0.1 molecular link visualization program and Gaussian 98, Gaussian 03 software packages and the use of default convergence criteria. After optimizing the geometry, frequency calculations followed. Thus, the stationary structures are confirmed by checking that all ground states have only real frequencies, and all transition states have only one imaginary frequency. The same method and established basis were used to optimize the geometry. Solvation calculations were performed in the framework of continuous models (D-PCM, C-PCM, IEF-PCM, IPCM, SCIPCM) of discrete and combined models using the Hartree–Fock constraint method, the method of density functional theory B3LYP with basic sets 6-31G (d), 6-31G (d,p), 6-31G++ (d,p), cc-pVDZ, as well as semi-empirical methods in the MOPAC6 package.\u0000Results. For the first time, various quantum chemical calculations of solvated model compounds using different approaches and models, variation of the basis in non-empirical calculations, identification of the role of electronic correlation effects, method of geometry optimization, etc. were carried out within the theory of self-consistent reaction field. The main stage of this study was to compare trends in the equilibrium change in the relative stability of tautomeric forms of thione-thiol tautomerism of 1,2,4-triazole-2(3H)-thions in the gas phase and different prototropic solvents due to the possibility of using different models and calculation methods for quality predictions of the effect of solvation on the position of tautomeric equilibrium in compounds of this class. It was found that the selected various solvents according to all used quantum chemical methods and models (D-PCM, C-PCM. IEF-PCM, IPCM, SCIPCM) reduce the difference in the stability of tautomeric forms of the investigated compounds in comparison with the gas phase, while the greatest stabilizing effect is observed in the solvation of NH-tautomers derived from 1,2,4-triazole-2(3H)-thiones. Using all energy parameters (∆Etot, ∆E0, ∆H298, ∆G298) allowed to determine the effect of complexa","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"84 46 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90816059","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}