Pub Date : 2024-02-02DOI: 10.29296/25877313-2024-02-03
S. S. Kataev, O. Dvorskaya, M. Gofenberg, A.A. Pospelova, E.Yu. Tumilovich
The purpose of the study is to study the metabolic profile of the cannabimimetic 4F-MDMB-BICA in the urine of consumers and to identify markers of 4F-MDMB-BICA use using gas chromatography with a mass spectrometric detector (GC-MS) and liquid chromatography with tandem mass spec-trometry (LC-MS/ MS) in the urine of consumers of psychoactive substances, for chemical-toxicological and forensic chemical analysis. Material and methods. The study of urine samples of 4F-MDMB-BICA cannabimimetic users using enzymatic hydrolysis in combination with solid-phase extraction and gas chromatography with mass spectrometric detection showed that the 4F-MDMB-BICA marker and, in some cases, its nor-metabolite are detected in the urine of consumers. The 4F-MDMB-BICA nor-metabolite is a common biotransformation product for the cannabimimetics 4F-MDMB-BICA and 5F-MDMB-PICA, resulting from the hydrolysis of the ester bond and N-dealkylation of the heterocyclic core. Results. 35 compounds were identified by liquid chromatography with tandem mass spectrometry, including the original parent 4F-MDMB-BICA, 31 metabolites of biotransformation phases I and II, and 3 metabolite artifacts; it was found that the latter are the product of intramolecular cyclization of 4F-MDMB-BICA metabolites. 16 previously undescribed compounds, including 15 metabolites and one artifact were identified. The putative structures, mass spectra and some characteristics of the identified compounds are given, including retention time, MRM transitions, and relative peak area of the substance. Conclusion. From the presented data, it can be seen that the main pathways of 4F-MDMB-BICA metabolism in the human body are hydrolysis of the ester group, hydroxylation of alkyl radicals and the heterocyclic core, oxidative defluorination, and N-dealkylation. The hydrolysis products of the ester bond and hydroxyl derivatives are subsequently conjugated with glucuronic acid.
{"title":"METABOLIC PROFILE OF 4F-MDMB-BICA IN HUMAN URINE","authors":"S. S. Kataev, O. Dvorskaya, M. Gofenberg, A.A. Pospelova, E.Yu. Tumilovich","doi":"10.29296/25877313-2024-02-03","DOIUrl":"https://doi.org/10.29296/25877313-2024-02-03","url":null,"abstract":"The purpose of the study is to study the metabolic profile of the cannabimimetic 4F-MDMB-BICA in the urine of consumers and to identify markers of 4F-MDMB-BICA use using gas chromatography with a mass spectrometric detector (GC-MS) and liquid chromatography with tandem mass spec-trometry (LC-MS/ MS) in the urine of consumers of psychoactive substances, for chemical-toxicological and forensic chemical analysis. Material and methods. The study of urine samples of 4F-MDMB-BICA cannabimimetic users using enzymatic hydrolysis in combination with solid-phase extraction and gas chromatography with mass spectrometric detection showed that the 4F-MDMB-BICA marker and, in some cases, its nor-metabolite are detected in the urine of consumers. The 4F-MDMB-BICA nor-metabolite is a common biotransformation product for the cannabimimetics 4F-MDMB-BICA and 5F-MDMB-PICA, resulting from the hydrolysis of the ester bond and N-dealkylation of the heterocyclic core. Results. 35 compounds were identified by liquid chromatography with tandem mass spectrometry, including the original parent 4F-MDMB-BICA, 31 metabolites of biotransformation phases I and II, and 3 metabolite artifacts; it was found that the latter are the product of intramolecular cyclization of 4F-MDMB-BICA metabolites. 16 previously undescribed compounds, including 15 metabolites and one artifact were identified. The putative structures, mass spectra and some characteristics of the identified compounds are given, including retention time, MRM transitions, and relative peak area of the substance. Conclusion. From the presented data, it can be seen that the main pathways of 4F-MDMB-BICA metabolism in the human body are hydrolysis of the ester group, hydroxylation of alkyl radicals and the heterocyclic core, oxidative defluorination, and N-dealkylation. The hydrolysis products of the ester bond and hydroxyl derivatives are subsequently conjugated with glucuronic acid.","PeriodicalId":20508,"journal":{"name":"Problems Of Biological, Medical And Pharmaceutical Chemistry","volume":"90 8","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140462629","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}
Pub Date : 2024-02-02DOI: 10.29296/25877313-2024-02-06
A. Sheremetyeva, L. V. Karavaeva, N. Durnova, O. Shapoval, N. Mukhamadiev, G. Rabbimova, M. H. Nazirbekov
Introduction. Plant essential oils are natural sources of the different compounds, the action of which in the macroorganism is determined by their chemical composition, depending on environmental factors, including plant species. Aim. The aim of the study was to compare the chemical composition of essential oils, obtained from the aerial parts of Thymus serpyllum L. and Thymus marschallianus Willd. (Lamiaceae). Material and methods. The plant raw materials of Thymus marschallianus were collected in the flowering phase in the Saratov region in June, the plant raw materials of Thymus serpyllum were purchased in the pharmacy network. The essential oils were obtained by Ginsberg’s steam hydrodistillation method. Analysis of their chemical composition was performed by gas-liquid chromatography with mass spectrometry detection. Results. The main components of both types of the essential oils were represented by thymol and its isomers, their mass fraction in the essential oil of T. marschallianus is 38.4, in the essential oil of T. serpyllum is 44%. The comparative analysis was carried out using the non-parametric Mann-Whitney criterion. Statistically significant differences with 95% probability were established for tricyclic sesquiterpene alkenes, the total content of which in the essential oil of T. marschallianus is 4.73%, in the essential oil of T. serpyllum – 3.59%. Conclusion. According to their chemical composition the essential oils of the mentioned plant species belong to phenolic chemotype and are similar in the major compounds.
引言植物精油是不同化合物的天然来源,它们对大型生物的作用取决于其化学成分,取决于环境因素,包括植物种类。研究目的本研究旨在比较从 Thymus serpyllum L. 和 Thymus marschallianus Willd.(唇形科植物)气生部分提取的精油的化学成分。材料和方法百里香(Thymus marschallianus)的植物原料是六月在萨拉托夫州的开花期采集的,百里香(Thymus serpyllum)的植物原料是在药房网络购买的。精油是通过金斯伯格水蒸气蒸馏法获得的。化学成分分析采用气液色谱法和质谱检测法进行。结果显示两种精油的主要成分都是百里酚及其异构体,它们在 T. marschallianus 精油中的质量分数为 38.4%,在 T. serpyllum 精油中的质量分数为 44%。比较分析采用非参数 Mann-Whitney 标准。三环倍半萜烯的总含量在 T. marschallianus 精油中为 4.73%,在 T. serpyllum 精油中为 3.59%。结论。根据化学成分,上述植物物种的精油属于酚类化学类型,主要化合物相似。
{"title":"COMPARATIVE ANALYSIS OF CHEMICAL COMPOSITION OF THYMUS SERPYLLUM L. AND THYMUS MARSCHALLIANUS WILLD. ESSENTIAL OILS BY GAS-LIQUID CHROMATOGRAPHY WITH MASS SPECTROMETRY DETECTION","authors":"A. Sheremetyeva, L. V. Karavaeva, N. Durnova, O. Shapoval, N. Mukhamadiev, G. Rabbimova, M. H. Nazirbekov","doi":"10.29296/25877313-2024-02-06","DOIUrl":"https://doi.org/10.29296/25877313-2024-02-06","url":null,"abstract":"Introduction. Plant essential oils are natural sources of the different compounds, the action of which in the macroorganism is determined by their chemical composition, depending on environmental factors, including plant species. Aim. The aim of the study was to compare the chemical composition of essential oils, obtained from the aerial parts of Thymus serpyllum L. and Thymus marschallianus Willd. (Lamiaceae). Material and methods. The plant raw materials of Thymus marschallianus were collected in the flowering phase in the Saratov region in June, the plant raw materials of Thymus serpyllum were purchased in the pharmacy network. The essential oils were obtained by Ginsberg’s steam hydrodistillation method. Analysis of their chemical composition was performed by gas-liquid chromatography with mass spectrometry detection. Results. The main components of both types of the essential oils were represented by thymol and its isomers, their mass fraction in the essential oil of T. marschallianus is 38.4, in the essential oil of T. serpyllum is 44%. The comparative analysis was carried out using the non-parametric Mann-Whitney criterion. Statistically significant differences with 95% probability were established for tricyclic sesquiterpene alkenes, the total content of which in the essential oil of T. marschallianus is 4.73%, in the essential oil of T. serpyllum – 3.59%. Conclusion. According to their chemical composition the essential oils of the mentioned plant species belong to phenolic chemotype and are similar in the major compounds.","PeriodicalId":20508,"journal":{"name":"Problems Of Biological, Medical And Pharmaceutical Chemistry","volume":"83 3","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140462506","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}
Pub Date : 2024-02-02DOI: 10.29296/25877313-2024-02-02
A. V. Logatkina, V.S. Nikiforov, I. Terekhov
Introduction. Coronary heart disease (CHD), leading among the causes of death in adulthood and old age, is an urgent medical and social problem. The pathogenesis of most forms of coronary heart disease is based on stenosing atherosclerosis of the coronary arteries, which develops against the background of dyslipidemia and arterial hypertension and is accompanied by the activation of immunocompetent cells (ICCs) of the vascular wall with the development of a subclinical inflammatory reaction, as well as the production of pro-inflammatory factors such as interleukins, chemokines, growth factors and etc. In turn, ICC activity is determined by the state of their intracellular molecular cascades, which transmit signals into the cell and ensure its reactivity to various external stimuli, such as mitogens, cytokines, pathogen components, etcIt has been shown that the central nervous system plays an important role in the regulation of ICC activity due to the production of neurohumoral molecules, such as melatonin, endorphin, sero-tonin, etc., which ensure the coordination of immune responses and their control by the central nervous system. The aim of this study was to study the relationship between melatonin production and intracellular factors that regulate the pro-inflammatory activi-ty of whole blood mononuclear cells and their metabolism in patients with coronary artery disease. Material and methods. As part of the cohort study, 58 patients of both sexes with coronary artery disease aged 49 to 67 years and 20 practically healthy individuals of both sexes were examined. In accordance with the purpose of the study, the concentration of focal adhesion protein kinase (FAK), 5'AMP-activated protein kinase (AMPK), AKT1 protein kinase, signal transducers and transcription activators (STAT) was determined in nuclear cy-toplasmic lysates of whole blood mononuclear cells: STAT3, STAT5A and STAT6, c-Jun N-terminal protein kinase 1 and 2 isoforms (JNK), mitogen-activated protein kinase p38 (p38), extracellular growth kinase 1 and 2 isoforms (ERK), Janus kinase type 2 (JAK2), nuclear transcription factor NF -kB, caspase-1, cyclooxygenase-2 (COX-2), p70-S6K1 protein kinase, p53, p27, p21 proteins. In addition, the concentration of cyclic adenosine monophos-phate (cAMP) and cyclic guanosine monophosphate (cGMP) was determined in cell supernatants. Melatonin concentration was determined in blood se-rum. The material for the study was venous blood taken from the cubital vein in the morning from 6.00 to 6.15. Results. The analysis showed that in patients with coronary artery disease, in comparison with practically healthy individuals, in MNCs of whole blood, there was an increased level of protein kinases FAK, AKT, JNK, ERK, p70-S6K1, factor STAT6, protein p21, against which there was a decrease in the content of STAT3, STAT5A, JAK2, transcription factor NF-kB and caspase-1. These changes were accompanied by increased levels of cGMP and cAMP. Against this background,
{"title":"FEATURES OF RELATIONS OF MELATONIN WITH THE STATE OF INTRACELLULAR REGULATORSOF THE FUNCTIONAL ACTIVITY OF WHOLE BLOOD MONONUCLEAR CELLS IN CORONARY HEART DISEASE","authors":"A. V. Logatkina, V.S. Nikiforov, I. Terekhov","doi":"10.29296/25877313-2024-02-02","DOIUrl":"https://doi.org/10.29296/25877313-2024-02-02","url":null,"abstract":"Introduction. Coronary heart disease (CHD), leading among the causes of death in adulthood and old age, is an urgent medical and social problem. The pathogenesis of most forms of coronary heart disease is based on stenosing atherosclerosis of the coronary arteries, which develops against the background of dyslipidemia and arterial hypertension and is accompanied by the activation of immunocompetent cells (ICCs) of the vascular wall with the development of a subclinical inflammatory reaction, as well as the production of pro-inflammatory factors such as interleukins, chemokines, growth factors and etc. In turn, ICC activity is determined by the state of their intracellular molecular cascades, which transmit signals into the cell and ensure its reactivity to various external stimuli, such as mitogens, cytokines, pathogen components, etcIt has been shown that the central nervous system plays an important role in the regulation of ICC activity due to the production of neurohumoral molecules, such as melatonin, endorphin, sero-tonin, etc., which ensure the coordination of immune responses and their control by the central nervous system. The aim of this study was to study the relationship between melatonin production and intracellular factors that regulate the pro-inflammatory activi-ty of whole blood mononuclear cells and their metabolism in patients with coronary artery disease. Material and methods. As part of the cohort study, 58 patients of both sexes with coronary artery disease aged 49 to 67 years and 20 practically healthy individuals of both sexes were examined. In accordance with the purpose of the study, the concentration of focal adhesion protein kinase (FAK), 5'AMP-activated protein kinase (AMPK), AKT1 protein kinase, signal transducers and transcription activators (STAT) was determined in nuclear cy-toplasmic lysates of whole blood mononuclear cells: STAT3, STAT5A and STAT6, c-Jun N-terminal protein kinase 1 and 2 isoforms (JNK), mitogen-activated protein kinase p38 (p38), extracellular growth kinase 1 and 2 isoforms (ERK), Janus kinase type 2 (JAK2), nuclear transcription factor NF -kB, caspase-1, cyclooxygenase-2 (COX-2), p70-S6K1 protein kinase, p53, p27, p21 proteins. In addition, the concentration of cyclic adenosine monophos-phate (cAMP) and cyclic guanosine monophosphate (cGMP) was determined in cell supernatants. Melatonin concentration was determined in blood se-rum. The material for the study was venous blood taken from the cubital vein in the morning from 6.00 to 6.15. Results. The analysis showed that in patients with coronary artery disease, in comparison with practically healthy individuals, in MNCs of whole blood, there was an increased level of protein kinases FAK, AKT, JNK, ERK, p70-S6K1, factor STAT6, protein p21, against which there was a decrease in the content of STAT3, STAT5A, JAK2, transcription factor NF-kB and caspase-1. These changes were accompanied by increased levels of cGMP and cAMP. Against this background, ","PeriodicalId":20508,"journal":{"name":"Problems Of Biological, Medical And Pharmaceutical Chemistry","volume":"86 15","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140462488","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}
Pub Date : 2024-02-02DOI: 10.29296/25877313-2024-02-08
T.V. Fateeva, P. G. Mizina, L. Krepkova, A. N. Babenko
The biographical sketch is dedicated to Serafima Alexandrovna Vichkanova (1924–2017), Doctor of Biological Sciences, Professor, Honored Scientist of the Russian Federation, who worked in the laboratory of antimicrobial and antiviral agents at the All–Russian Research Institute of Medicinal and Aro-matic Plants (Moscow). The main life stages, the scientific directions being developed and the contribution to the formation and development of the field of studying the antimicrobial properties of plants and substances from them in order to create new effective chemotherapeutic agents for the treatment of viral, bacterial, fungal and other infections, as well as a list of the main scientific works are presented in the article
{"title":"ON THE 100TH ANNIVERSARY OF THE BIRTH OF SERAFIMA ALEXANDROVNA VICHKANOVA (1924‒2017)","authors":"T.V. Fateeva, P. G. Mizina, L. Krepkova, A. N. Babenko","doi":"10.29296/25877313-2024-02-08","DOIUrl":"https://doi.org/10.29296/25877313-2024-02-08","url":null,"abstract":"The biographical sketch is dedicated to Serafima Alexandrovna Vichkanova (1924–2017), Doctor of Biological Sciences, Professor, Honored Scientist of the Russian Federation, who worked in the laboratory of antimicrobial and antiviral agents at the All–Russian Research Institute of Medicinal and Aro-matic Plants (Moscow). The main life stages, the scientific directions being developed and the contribution to the formation and development of the field of studying the antimicrobial properties of plants and substances from them in order to create new effective chemotherapeutic agents for the treatment of viral, bacterial, fungal and other infections, as well as a list of the main scientific works are presented in the article","PeriodicalId":20508,"journal":{"name":"Problems Of Biological, Medical And Pharmaceutical Chemistry","volume":"53 2","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140462405","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}
Pub Date : 2024-02-02DOI: 10.29296/25877313-2024-02-05
D. I. Pozdnyakov, A. A. Vikhor, V. Rukovitsina, E. T. Oganesyan, A. P. Pleten, A. A. Prokopov, T. Tatarenko-Kozmina
Introduction. Alzheimer's disease is one of the most common forms of dementia, the pathogenesis of which is based on the accumulation of β–amyloid plaques in brain structures and the development of cholinergic deficiency. The aim of the study was to evaluate the effect of chalcone analogues on the change in acetylcholinesterase activity and the process of β-amyloid aggregation in vitro. Material and methods. The tested compounds were six bis-substituted chalcone analogues, which were dissolved in dimethylsulfoxide during the analysis to obtain double dilutions. The effect of the studied substances on the activity of acetylcholinesterase was evaluated by the modified Ellman method. The change in the aggregation process of β-amyloid particles was determined in reaction with congo red after 3, 6 and 9 days of incubation. Based on the obtained results of the «% inhibition- concentration» relationships, the IC50 index was calculated, which was expressed in mmol/ml. Results. In the course of the study, it was shown that the analyzed chalcone analogues inhibit the aggregation of β-amyloid particles starting from the 6th day of incubation with a maximum on the 9th day. At the same time, the compounds that showed the highest level of activity were trimethoxy-substituted substances under the codes AZBAX4 and AZBAX6, whose IC50 on the 9th day of the study was 21.4±0.928 mmol/ml and 32.4±0.456 mmol/ml, respectively. Also, a high level of anticholinesterase properties was established for these compounds with IC50 of 35.9±0.991mmol/ml and 25.1±0.261 mmol/ml, respectively. The rest of the tested compounds showed a lower level of activity. Conclusion. The study showed that chalcone analogues under the codes AZBAX4 and AZBAX6 inhibit the activity of acetylcholinesterase and the pro-cess of aggregation of β-amyloid in vitro, which makes these compounds promising for further study in order to develop medicines for the pathogenet-ic treatment of Alzheimer's disease.
{"title":"CHALCONE ANALOGUES AS POTENTIAL MEDICINES OF PATHOGENETIC THERAPY OF ALZHEIMER'S DISEASE: IN VITRO SCREENING","authors":"D. I. Pozdnyakov, A. A. Vikhor, V. Rukovitsina, E. T. Oganesyan, A. P. Pleten, A. A. Prokopov, T. Tatarenko-Kozmina","doi":"10.29296/25877313-2024-02-05","DOIUrl":"https://doi.org/10.29296/25877313-2024-02-05","url":null,"abstract":"Introduction. Alzheimer's disease is one of the most common forms of dementia, the pathogenesis of which is based on the accumulation of β–amyloid plaques in brain structures and the development of cholinergic deficiency. The aim of the study was to evaluate the effect of chalcone analogues on the change in acetylcholinesterase activity and the process of β-amyloid aggregation in vitro. Material and methods. The tested compounds were six bis-substituted chalcone analogues, which were dissolved in dimethylsulfoxide during the analysis to obtain double dilutions. The effect of the studied substances on the activity of acetylcholinesterase was evaluated by the modified Ellman method. The change in the aggregation process of β-amyloid particles was determined in reaction with congo red after 3, 6 and 9 days of incubation. Based on the obtained results of the «% inhibition- concentration» relationships, the IC50 index was calculated, which was expressed in mmol/ml. Results. In the course of the study, it was shown that the analyzed chalcone analogues inhibit the aggregation of β-amyloid particles starting from the 6th day of incubation with a maximum on the 9th day. At the same time, the compounds that showed the highest level of activity were trimethoxy-substituted substances under the codes AZBAX4 and AZBAX6, whose IC50 on the 9th day of the study was 21.4±0.928 mmol/ml and 32.4±0.456 mmol/ml, respectively. Also, a high level of anticholinesterase properties was established for these compounds with IC50 of 35.9±0.991mmol/ml and 25.1±0.261 mmol/ml, respectively. The rest of the tested compounds showed a lower level of activity. Conclusion. The study showed that chalcone analogues under the codes AZBAX4 and AZBAX6 inhibit the activity of acetylcholinesterase and the pro-cess of aggregation of β-amyloid in vitro, which makes these compounds promising for further study in order to develop medicines for the pathogenet-ic treatment of Alzheimer's disease.","PeriodicalId":20508,"journal":{"name":"Problems Of Biological, Medical And Pharmaceutical Chemistry","volume":"174 ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140462313","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}
Pub Date : 2024-02-02DOI: 10.29296/25877313-2024-02-01
I.A. Obraztsova, S. S. Popov, A. N. Verevkin, A.A. Pashkova, E. D. Kryl'skii, T.N. Popova
Relevance. In many countries plants have long been used in folk medicine as a source of medicines, as they are well tolerated, gradual development of therapeutic effect and a mild effect on the body. Due to these features such medicines are being safely used in the treatment and prevention of exacerbations of chronic diseases: of cardiovascular system, respiratory system, digestive system, pathologies of the urinary tract, etc., and also as a rehabilitation therapy after past diseases. The purpose of the study is to systematize and generalize the data of world literature concerning the general health-improving and tonic properties study of plants growing in the Republic of Buryatia. Material and methods. In this work used publication materials from the PubMed and е-library databases, search.rsl. The keyword search: restorative, tonic effect, herbal medicines, medicinal plants of Buryatia, biologically active substances, Astragalus membranaceus, Saposhnikovia divaricatа, Scutellaria baicalensis, Sedum roseum, Crataegus sangunea. The survey comprises the data of foreign and national articles, published on the topic during last 20 years. Conclusions. All the plants listed in this review are used for thousands of years in the Tibetan medicine. Based on the analysis of the presented literature data, their range of medicinal use is much wider, then the applications in modern clinical practice. The information reported in this review may be the basis for the development of new herbal medicines, including officinal mixture, with specified pharmacological properties.
{"title":"APOPTOTIC AND PROINFLAMMATORY PROCESSES ESTIMATION IN PATIENTS WITH DIABETIC NEUROPATHY","authors":"I.A. Obraztsova, S. S. Popov, A. N. Verevkin, A.A. Pashkova, E. D. Kryl'skii, T.N. Popova","doi":"10.29296/25877313-2024-02-01","DOIUrl":"https://doi.org/10.29296/25877313-2024-02-01","url":null,"abstract":"Relevance. In many countries plants have long been used in folk medicine as a source of medicines, as they are well tolerated, gradual development of therapeutic effect and a mild effect on the body. Due to these features such medicines are being safely used in the treatment and prevention of exacerbations of chronic diseases: of cardiovascular system, respiratory system, digestive system, pathologies of the urinary tract, etc., and also as a rehabilitation therapy after past diseases.\u0000The purpose of the study is to systematize and generalize the data of world literature concerning the general health-improving and tonic properties study of plants growing in the Republic of Buryatia.\u0000Material and methods. In this work used publication materials from the PubMed and е-library databases, search.rsl. The keyword search: restorative, tonic effect, herbal medicines, medicinal plants of Buryatia, biologically active substances, Astragalus membranaceus, Saposhnikovia divaricatа, Scutellaria baicalensis, Sedum roseum, Crataegus sangunea. The survey comprises the data of foreign and national articles, published on the topic during last 20 years.\u0000Conclusions. All the plants listed in this review are used for thousands of years in the Tibetan medicine. Based on the analysis of the presented literature data, their range of medicinal use is much wider, then the applications in modern clinical practice. The information reported in this review may be the basis for the development of new herbal medicines, including officinal mixture, with specified pharmacological properties.","PeriodicalId":20508,"journal":{"name":"Problems Of Biological, Medical And Pharmaceutical Chemistry","volume":"154 ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140462479","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}
Pub Date : 2024-02-02DOI: 10.29296/25877313-2024-02-04
A.I. Israpilova, A. A. Adieva, A.M. Jafarova, G.M. Abakarov, I. V. Amirkhanova
Introduction. Antimicrobial resistance in bacteria has become a global challenge for public health systems. Bacteria that pose the greatest threat to human health due to their increasing resistance to antibiotics include Escherichia coli, Staphylococcus aureus and Salmonella spp. The purpose of the work is to study the antibacterial properties of three tellurium derivatives against infections caused by Staphylococcus, Escherichia coli and Salmonella. Material and methods. The object of study is heterocyclic tellurium derivatives. A comparative analysis of the antibacterial properties of the syn-thesized tellurium derivatives on bacterial strains of Staphylococcus, Escherichia coli and Salmonella was carried out. To determine the antibacterial properties, the serial dilution method was used. The sensitivity of bacteria to the test tellurium derivatives and to antibiotics was assessed using the disk- diffusion method. Results. The study of three tellurium derivatives in different concentrations made it possible to determine the minimum inhibitory concentration (MIC) for organotellurium compounds, which were 1.35, 0.12 and 0.2 μg of the substance per 1 disk, respectively. For dioxysirocyclo-[4-methylphenyl] tellu-rochloride against E. coli and S. aureus, the minimum inhibitory concentrations (MIC50) were determined to be 16.4 and 18.6 μg of the substance per 1 disk, respectively. Conclusions. The effect of organotellurium substances in relatively low concentrations on strains of bacteria Staphylococcus, Escherichia coli and Salmonella indicates the prospects for further study of the biological properties of tellurium derivatives containing various groups.
{"title":"ANTIBACTERIAL PROPERTIES OF ORGANOTELLURIUM COMPOUNDS","authors":"A.I. Israpilova, A. A. Adieva, A.M. Jafarova, G.M. Abakarov, I. V. Amirkhanova","doi":"10.29296/25877313-2024-02-04","DOIUrl":"https://doi.org/10.29296/25877313-2024-02-04","url":null,"abstract":"Introduction. Antimicrobial resistance in bacteria has become a global challenge for public health systems. Bacteria that pose the greatest threat to human health due to their increasing resistance to antibiotics include Escherichia coli, Staphylococcus aureus and Salmonella spp. The purpose of the work is to study the antibacterial properties of three tellurium derivatives against infections caused by Staphylococcus, Escherichia coli and Salmonella. Material and methods. The object of study is heterocyclic tellurium derivatives. A comparative analysis of the antibacterial properties of the syn-thesized tellurium derivatives on bacterial strains of Staphylococcus, Escherichia coli and Salmonella was carried out. To determine the antibacterial properties, the serial dilution method was used. The sensitivity of bacteria to the test tellurium derivatives and to antibiotics was assessed using the disk- diffusion method. Results. The study of three tellurium derivatives in different concentrations made it possible to determine the minimum inhibitory concentration (MIC) for organotellurium compounds, which were 1.35, 0.12 and 0.2 μg of the substance per 1 disk, respectively. For dioxysirocyclo-[4-methylphenyl] tellu-rochloride against E. coli and S. aureus, the minimum inhibitory concentrations (MIC50) were determined to be 16.4 and 18.6 μg of the substance per 1 disk, respectively. Conclusions. The effect of organotellurium substances in relatively low concentrations on strains of bacteria Staphylococcus, Escherichia coli and Salmonella indicates the prospects for further study of the biological properties of tellurium derivatives containing various groups.","PeriodicalId":20508,"journal":{"name":"Problems Of Biological, Medical And Pharmaceutical Chemistry","volume":"86 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140462497","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}
Pub Date : 2024-02-02DOI: 10.29296/25877313-2024-02-07
A.V. Zykova, D.A. Isakov, S.V. Krivoshchekov
Introduction. The object of increased attention of researchers is calamus (Acorus calamus L.), for the components of which a wide range of pharma-cological activities have been identified – immunomodulatory, anti-inflammatory, analgesic, antioxidant, neuroprotective, hypolipidemic, antitumor. Ac-cording to previous studies, it was found that α(1,2)-L-rhamno-α(1,4)-D-galactopyranosyluronan, isolated from the rhizomes of Acorus calamus L., has antimetastatic, antiblastoma, and immunomodulatory properties. The substance can also reduce the toxic effect on the hematopoietic system and in-crease the effectiveness of chemotherapy. Based on it, a finished dosage form was obtained - a solution for intravenous administration of 10 mg/ml, which requires the development of valid quality control methods for inclusion in the draft regulatory document on the quality and registration of a new drug. The aim of the study was to determine the metrological characteristics of the chromatographic technique for the quantitative determination of α(1,2)-L-rhamno-α(1,4)-D-galactopyranosyluronan in the finished dosage form. Material and methods. The object of the study was the finished dosage form - a solution for intravenous administration of α(1,2)-L-rhamno-α(1,4)-D-galactopyranosyluronan Acorus calamus L. 10 mg/ml, produced on the basis of the educational establishment of the Technology Implementation Cen-ter of the Federal State Budgetary Educational Institution of Higher Education of the Siberian State Medical University of the Ministry of Health Russia. Quantitative determination was carried out using a Dionex Ultimate 3000 liquid chromatograph (Thermo, Germany) with a refractometric detector RI-101. Validation assessment was carried out according to the following indicators: linearity, accuracy, precision under repeatability conditions. Results. Linear regression analysis of the obtained results using the least squares method showed that the technique is linear in the concentration range of 80–120%. When determining the accuracy, the openability for concentrations of 80, 100 and 120% varied in the range of 99.68–101.96%. The values of the relative standard deviation did not exceed the permissible values when assessing precision 0.82–4.51%. Conclusions. The methodology is valid for the studied indicators and can be recommended for inclusion in the draft regulatory document on quality. The work was carried out within the framework of applied scientific research 720000F.99.1.BN62AB30000 within the framework of state assignment No. 056-00116-23-01.
{"title":"VALIDATION EVALUATION OF THE METHOD OF QUANTITATIVE DETERMINATION OF α(1,2)-L-RHAMNO-α(1,4)-D-GALACTOPYRANOSYLURONANE ACORUS CALAMUS L. IN DOSAGE FORM","authors":"A.V. Zykova, D.A. Isakov, S.V. Krivoshchekov","doi":"10.29296/25877313-2024-02-07","DOIUrl":"https://doi.org/10.29296/25877313-2024-02-07","url":null,"abstract":"Introduction. The object of increased attention of researchers is calamus (Acorus calamus L.), for the components of which a wide range of pharma-cological activities have been identified – immunomodulatory, anti-inflammatory, analgesic, antioxidant, neuroprotective, hypolipidemic, antitumor. Ac-cording to previous studies, it was found that α(1,2)-L-rhamno-α(1,4)-D-galactopyranosyluronan, isolated from the rhizomes of Acorus calamus L., has antimetastatic, antiblastoma, and immunomodulatory properties. The substance can also reduce the toxic effect on the hematopoietic system and in-crease the effectiveness of chemotherapy. Based on it, a finished dosage form was obtained - a solution for intravenous administration of 10 mg/ml, which requires the development of valid quality control methods for inclusion in the draft regulatory document on the quality and registration of a new drug. The aim of the study was to determine the metrological characteristics of the chromatographic technique for the quantitative determination of α(1,2)-L-rhamno-α(1,4)-D-galactopyranosyluronan in the finished dosage form. Material and methods. The object of the study was the finished dosage form - a solution for intravenous administration of α(1,2)-L-rhamno-α(1,4)-D-galactopyranosyluronan Acorus calamus L. 10 mg/ml, produced on the basis of the educational establishment of the Technology Implementation Cen-ter of the Federal State Budgetary Educational Institution of Higher Education of the Siberian State Medical University of the Ministry of Health Russia. Quantitative determination was carried out using a Dionex Ultimate 3000 liquid chromatograph (Thermo, Germany) with a refractometric detector RI-101. Validation assessment was carried out according to the following indicators: linearity, accuracy, precision under repeatability conditions. Results. Linear regression analysis of the obtained results using the least squares method showed that the technique is linear in the concentration range of 80–120%. When determining the accuracy, the openability for concentrations of 80, 100 and 120% varied in the range of 99.68–101.96%. The values of the relative standard deviation did not exceed the permissible values when assessing precision 0.82–4.51%. Conclusions. The methodology is valid for the studied indicators and can be recommended for inclusion in the draft regulatory document on quality. The work was carried out within the framework of applied scientific research 720000F.99.1.BN62AB30000 within the framework of state assignment No. 056-00116-23-01.","PeriodicalId":20508,"journal":{"name":"Problems Of Biological, Medical And Pharmaceutical Chemistry","volume":"84 6","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140462342","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}
Pub Date : 2024-01-31DOI: 10.29296/25877313-2024-01-09
P.A. Sheykhmagomedova, E.O. Sergeeva, I.L. Abisalova, L.A. Sajaya, O.I. Popova, I. V. Popov
Introduction. The use of phenolic compounds as agents for preventing the risk of developing various cardiovascular diseases, as well as the prospect of creating new modern highly effective drugs based on them, is of current practical interest. The aim of the study is to identify the hypolipidemic activity of the phytocomplex of the herb Phacelia tanacetifolia Benth., and the possibility of its use in herbal preparations for the treatment of diseases of the cardiovascular system. Material and methods. The object of research was a herb of phacelia tanacetifolia, grown in the Neftekumsky region. The herb was collected during flowering and dried by air-shadowing method. The study of hypolipidemic activity was carried out on 24 white female Wistar rats weighing 270290 g. In the experiment, a Tween model of hyperlipidemia was created and used: a single intraperitoneal injection of Tween-80 at a dose of 250 mg / 100 g of body weight. Lipid profile analysis was carried out on a biochemical analyzer RAL CLIMA MC-15 using reagents from DiaSys, manufactured in Germa-ny. Results. Based on the level of triglycerides and very low density lipoproteins, it was found that the phytocomplex significantly exceeded the values of the reference drug (fenofibrate-canon). Conclusions. In conditions of twin hyperlipidemia, therapeutic and prophylactic administration of the Phacelia tanacetifolia phytocomplex at a dose of 300 mg/kg helps to normalize blood serum lipid metabolism.
{"title":"HYPOLIPIDEMIC ACTIVITY OF THE PHYTOCOMPLEX \u0000OF THE HERB PHACELIA TANACETIFOLIA BENTH.","authors":"P.A. Sheykhmagomedova, E.O. Sergeeva, I.L. Abisalova, L.A. Sajaya, O.I. Popova, I. V. Popov","doi":"10.29296/25877313-2024-01-09","DOIUrl":"https://doi.org/10.29296/25877313-2024-01-09","url":null,"abstract":"Introduction. The use of phenolic compounds as agents for preventing the risk of developing various cardiovascular diseases, as well as the prospect of creating new modern highly effective drugs based on them, is of current practical interest. \u0000The aim of the study is to identify the hypolipidemic activity of the phytocomplex of the herb Phacelia tanacetifolia Benth., and the possibility of its use in herbal preparations for the treatment of diseases of the cardiovascular system.\u0000Material and methods. The object of research was a herb of phacelia tanacetifolia, grown in the Neftekumsky region. The herb was collected during flowering and dried by air-shadowing method. The study of hypolipidemic activity was carried out on 24 white female Wistar rats weighing 270290 g. In the experiment, a Tween model of hyperlipidemia was created and used: a single intraperitoneal injection of Tween-80 at a dose of 250 mg / 100 g of body weight. Lipid profile analysis was carried out on a biochemical analyzer RAL CLIMA MC-15 using reagents from DiaSys, manufactured in Germa-ny. \u0000Results. Based on the level of triglycerides and very low density lipoproteins, it was found that the phytocomplex significantly exceeded the values of the reference drug (fenofibrate-canon).\u0000Conclusions. In conditions of twin hyperlipidemia, therapeutic and prophylactic administration of the Phacelia tanacetifolia phytocomplex at a dose of 300 mg/kg helps to normalize blood serum lipid metabolism.","PeriodicalId":20508,"journal":{"name":"Problems Of Biological, Medical And Pharmaceutical Chemistry","volume":"493 ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140471266","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}