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METABOLIC PROFILE OF 4F-MDMB-BICA IN HUMAN URINE 人体尿液中 4f-mdmb-bica 的代谢概况
Pub Date : 2024-02-02 DOI: 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.
本研究的目的是研究消费者尿液中大麻拟物 4F-MDMB-BICA 的代谢概况,并使用带质谱检测器的气相色谱法(GC-MS)和带串联质谱检测器的液相色谱法(LC-MS/MS)鉴定精神活性物质消费者尿液中使用 4F-MDMB-BICA 的标记物,以便进行化学毒理学和法医化学分析。材料和方法使用酶水解法结合固相萃取和气相色谱法与质谱检测法对 4F-MDMB-BICA 大麻 拟亚胺类药物使用者的尿液样本进行的研究表明,在服用者的尿液中检测到 4F-MDMB-BICA 标记物,在某些情况下还检测到其非代谢物。4F-MDMB-BICA 非代谢物是大麻拟物 4F-MDMB-BICA 和 5F-MDMB-PICA 的常见生物转化产物,由酯键水解和杂环核心的 N-脱烷基化产生。研究结果通过液相色谱-串联质谱法鉴定出 35 种化合物,包括原始母体 4F-MDMB-BICA、31 种生物转化 I 期和 II 期的代谢物以及 3 种代谢物伪品;发现后者是 4F-MDMB-BICA 代谢物分子内环化的产物。共鉴定出 16 种以前未曾描述过的化合物,包括 15 种代谢物和 1 种人工产物。文中给出了已鉴定化合物的推定结构、质谱和一些特征,包括保留时间、MRM 过渡和物质的相对峰面积。结论从所提供的数据可以看出,4F-MDMB-BICA 在人体内代谢的主要途径是酯基的水解、烷基和杂环核心的羟基化、氧化脱氟和 N-脱烷基化。酯键和羟基衍生物的水解产物随后与葡萄糖醛酸共轭。
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引用次数: 0
COMPARATIVE ANALYSIS OF CHEMICAL COMPOSITION OF THYMUS SERPYLLUM L. AND THYMUS MARSCHALLIANUS WILLD. ESSENTIAL OILS BY GAS-LIQUID CHROMATOGRAPHY WITH MASS SPECTROMETRY DETECTION 用气液相色谱-质谱检测法比较分析胸腺蛇床子和胸腺马钱子精油的化学成分精油化学成分的比较分析
Pub Date : 2024-02-02 DOI: 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。
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引用次数: 0
FEATURES OF RELATIONS OF MELATONIN WITH THE STATE OF INTRACELLULAR REGULATORSOF THE FUNCTIONAL ACTIVITY OF WHOLE BLOOD MONONUCLEAR CELLS IN CORONARY HEART DISEASE 褪黑激素与冠心病患者全血单核细胞功能活动细胞内调节器状态关系的特点
Pub Date : 2024-02-02 DOI: 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,
导言。冠心病(CHD)是导致成年和老年死亡的主要原因之一,是一个紧迫的医学和社会问题。大多数冠心病的发病机理是在血脂异常和动脉高血压的背景下发生的冠状动脉狭窄性动脉粥样硬化,同时伴随着血管壁免疫功能细胞(ICC)的活化和亚临床炎症反应的发展,以及白细胞介素、趋化因子、生长因子等促炎因子的产生。反过来,ICC 的活性又取决于其细胞内分子级联的状态,细胞内分子级联向细胞内传递信号,确保细胞对各种外部刺激(如有丝分裂原、细胞因子、病原体成分等)的反应性。本研究旨在研究褪黑激素的产生与调节冠心病患者全血单核细胞促炎活性及其代谢的细胞内因子之间的关系。材料和方法作为队列研究的一部分,对 58 名年龄在 49 至 67 岁之间的男女冠心病患者和 20 名身体健康的男女个体进行了研究。根据研究目的,测定了全血单核细胞核细胞质裂解液中局灶粘附蛋白激酶(FAK)、5'AMP激活蛋白激酶(AMPK)、AKT1蛋白激酶、信号转导和转录激活因子(STAT)的浓度:STAT3、STAT5A 和 STAT6、c-Jun N 端蛋白激酶 1 和 2 异构体(JNK)、丝裂原活化蛋白激酶 p38(p38)、细胞外生长激酶 1 和 2 异构体(ERK)、Janus 激酶 2 型(JAK2)、核转录因子 NF-kB、caspase-1、环氧化酶-2(COX-2)、p70-S6K1 蛋白激酶、p53、p27、p21 蛋白。此外,还测定了细胞上清液中环磷酸腺苷(cAMP)和环磷酸鸟苷(cGMP)的浓度。测定血清中褪黑激素的浓度。研究材料为早晨 6:00 至 6:15 从肘静脉采集的静脉血。结果显示分析表明,与健康人相比,冠心病患者全血 MNC 中蛋白激酶 FAK、AKT、JNK、ERK、p70-S6K1、因子 STAT6、蛋白 p21 的含量增加,而 STAT3、STAT5A、JAK2、转录因子 NF-kB 和 caspase-1 的含量减少。这些变化伴随着 cGMP 和 cAMP 含量的增加。在此背景下,MNC 中的因子含量有所下降。CAD 患者体内的高浓度褪黑激素与 MNC 中蛋白激酶 AMPK、AKT、Jak2、ERK1、蛋白 p21、caspase-1 和 cAMP 含量的减少有关,这是在蛋白 p27 和核因子 NF-kB 水平增加的背景下观察到的。相关性分析结果表明,根据冠心病患者褪黑激素产生的特点,褪黑激素水平与caspase-1、蛋白激酶ERK、JAK2以及转录因子NF-kB和p21蛋白等因子之间的关系呈现出不同的性质。结论在冠心病患者中,褪黑素对ICCs的能量平衡及其新陈代谢具有调节作用,有助于通过限制MNCs中MAPK/SAPK信号通路的功能活性来限制促炎活性。
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引用次数: 0
ON THE 100TH ANNIVERSARY OF THE BIRTH OF SERAFIMA ALEXANDROVNA VICHKANOVA (1924‒2017) 谢拉菲玛-亚历山德罗芙娜-维奇卡诺娃(1924--2017 年)诞辰 100 周年
Pub Date : 2024-02-02 DOI: 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
本传记献给生物科学博士、教授、俄罗斯联邦荣誉科学家谢拉菲玛-亚历山德罗芙娜-维奇卡诺娃(Serafima Alexandrovna Vichkanova,1924-2017 年),她曾在全俄药用植物和芳香植物研究所(莫斯科)抗菌剂和抗病毒剂实验室工作。文章介绍了他的主要人生阶段、正在发展的科学方向、对植物抗菌特性研究领域的形成和发展所做的贡献,以及为治疗病毒、细菌、真菌和其他感染创造新的有效化疗药物所做的贡献,并列出了主要科学著作清单。
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引用次数: 0
CHALCONE ANALOGUES AS POTENTIAL MEDICINES OF PATHOGENETIC THERAPY OF ALZHEIMER'S DISEASE: IN VITRO SCREENING 作为阿尔茨海默病病因治疗潜在药物的查尔酮类似物:体外筛选
Pub Date : 2024-02-02 DOI: 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.
引言阿尔茨海默病是最常见的痴呆症之一,其发病机制是大脑结构中β-淀粉样蛋白斑块的积累和胆碱能缺乏症的发展。本研究旨在评估查尔酮类似物对乙酰胆碱酯酶活性变化和体外β-淀粉样蛋白聚集过程的影响。材料与方法受测化合物为六种双取代查尔酮类似物,分析时将其溶解在二甲基亚砜中以获得双倍稀释液。研究物质对乙酰胆碱酯酶活性的影响采用改进的埃尔曼法进行评估。在培养 3、6 和 9 天后,测定了与刚果红反应的 β 淀粉样蛋白颗粒聚集过程的变化。根据 "抑制率-浓度 "关系的结果,计算出 IC50 指数,以毫摩尔/毫升为单位。研究结果研究结果表明,所分析的查尔酮类似物从培养的第 6 天开始就能抑制 β 淀粉样蛋白颗粒的聚集,并在第 9 天达到最大值。同时,活性最高的化合物是代号为 AZBAX4 和 AZBAX6 的三甲氧基取代物质,其第 9 天的 IC50 分别为 21.4±0.928 mmol/ml 和 32.4±0.456 mmol/ml。此外,这些化合物还具有较高的抗胆碱酯酶特性,其 IC50 分别为 35.9±0.991 mmol/ml 和 25.1±0.261 mmol/ml。其余受测化合物的活性水平较低。结论研究表明,代号为 AZBAX4 和 AZBAX6 的查尔酮类似物在体外能抑制乙酰胆碱酯酶的活性和 β 淀粉样蛋白的聚集过程,这使得这些化合物有望得到进一步研究,从而开发出治疗阿尔茨海默病的药物。
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引用次数: 0
APOPTOTIC AND PROINFLAMMATORY PROCESSES ESTIMATION IN PATIENTS WITH DIABETIC NEUROPATHY 估计糖尿病神经病变患者的凋亡和促炎过程
Pub Date : 2024-02-02 DOI: 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.
相关性。在许多国家,由于植物具有良好的耐受性、治疗效果逐渐显现且对身体影响温和,因此长期以来一直被民间医学用作药物来源。由于这些特点,这些药物被安全地用于治疗和预防慢性疾病的恶化:心血管系统、呼吸系统、消化系统、泌尿系统病变等,还可作为既往疾病后的康复疗法。本研究的目的是系统整理和归纳世界文献中有关布里亚特共和国生长的植物的一般健康改善和滋补特性研究的数据。这项工作使用了 PubMed 和 е-library 数据库、search.rsl 中的出版物资料。关键词搜索:恢复、滋补作用、草药、布里亚特药用植物、生物活性物质、黄芪、Saposhnikovia divaricatа、黄芩、景天、山楂。调查包括过去 20 年间发表的有关该主题的国内外文章数据。本综述中列出的所有植物在藏医药中已有数千年的使用历史。根据对所提供文献数据的分析,这些植物的药用范围要比现代临床实践中的应用广泛得多。本综述所提供的信息可作为开发具有特定药理特性的新草药(包括药用混合物)的基础。
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引用次数: 0
ANTIBACTERIAL PROPERTIES OF ORGANOTELLURIUM COMPOUNDS 有机碲化合物的抗菌特性
Pub Date : 2024-02-02 DOI: 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.
导言。细菌的抗药性已成为公共卫生系统面临的全球性挑战。由于对抗生素的耐药性不断增加,对人类健康构成最大威胁的细菌包括大肠杆菌、金黄色葡萄球菌和沙门氏菌。 本研究的目的是研究三种碲衍生物对葡萄球菌、大肠杆菌和沙门氏菌引起的感染的抗菌特性。材料和方法。研究对象是杂环碲衍生物。对合成的碲衍生物对葡萄球菌、大肠杆菌和沙门氏菌等细菌菌株的抗菌特性进行了比较分析。为确定抗菌特性,采用了系列稀释法。使用磁盘扩散法评估了细菌对测试碲衍生物和抗生素的敏感性。研究结果通过对不同浓度的三种碲衍生物的研究,确定了有机碲化合物的最低抑菌浓度(MIC),分别为每 1 盘 1.35、0.12 和 0.2 微克。二氧代环-[4-甲基苯基] tellu-rochloride 对大肠杆菌和金黄色葡萄球菌的最小抑菌浓度(MIC50)分别为每 1 盘 16.4 和 18.6 微克。结论相对低浓度的有机碲物质对葡萄球菌、大肠杆菌和沙门氏菌菌株的影响表明,进一步研究含有各种基团的碲衍生物的生物特性具有广阔的前景。
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引用次数: 0
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 定量测定α(1,2)-L-RHAMNO-α(1,4)-D-GALACTOPYRANOSYLURONANE ACORUS CALAMUS L. 剂型方法的验证评价
Pub Date : 2024-02-02 DOI: 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.
简介。石菖蒲(Acorus calamus L.)是研究人员日益关注的对象,其成分具有广泛的药理活性--免疫调节、抗炎、镇痛、抗氧化、神经保护、降血脂、抗肿瘤。根据以往的研究,从石菖蒲根茎中分离出的α(1,2)-L-鼠李糖-α(1,4)-D-吡喃半乳糖醛酸具有抗转移、抗肿瘤和免疫调节的特性。该物质还能减少对造血系统的毒性作用,提高化疗的效果。在此基础上,我们获得了一种成品剂型--10 毫克/毫升的静脉注射溶液,这需要制定有效的质量控制方法,以便纳入新药质量和注册监管文件草案。本研究旨在确定色谱技术的计量学特征,以定量测定成品剂型中的α(1,2)-L-鼠李糖-α(1,4)-D-吡喃半乳糖醛酸。材料和方法研究对象是成品剂型--α(1,2)-L-鼠李糖-α(1,4)-D-吡喃半乳糖醛酸菖蒲 10 mg/ml 静脉注射溶液,该溶液由俄罗斯卫生部西伯利亚国立医科大学联邦国家预算高等教育机构技术实施中心的教育机构生产。使用 Dionex Ultimate 3000 液相色谱仪(德国 Thermo 公司)和 RI-101 折光检测器进行定量检测。根据以下指标进行了验证评估:线性、准确度、重复性条件下的精确度。结果使用最小二乘法对所得结果进行线性回归分析表明,该技术在 80-120% 的浓度范围内呈线性关系。在确定准确度时,浓度为 80%、100% 和 120% 的开放性变化范围为 99.68%-101.96%。在评估精确度 0.82-4.51% 时,相对标准偏差值未超过允许值。结论该方法对所研究的指标有效,建议将其纳入质量监管文件草案。这项工作是在应用科学研究 720000F.99.1.BN62AB30000(国家任务编号 056-00116-23-01)的框架内进行的。
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引用次数: 0
HYPOLIPIDEMIC ACTIVITY OF THE PHYTOCOMPLEX OF THE HERB PHACELIA TANACETIFOLIA BENTH. 蕨类草本植物复合物的降血脂活性
Pub Date : 2024-01-31 DOI: 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 270290 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.
导言。使用酚类化合物作为预防各种心血管疾病风险的药物,以及在此基础上开发新的现代高效药物的前景,是当前人们感兴趣的实际问题。本研究的目的是确定草本植物 Phacelia tanacetifolia Benth.的植物复合物的降血脂活性,以及将其用于治疗心血管系统疾病的草药制剂的可能性。研究对象是生长在内夫特库姆斯基地区的一株昙花草。草药在开花期采集,并通过空气阴影法进行干燥。对 24 只体重为 270290 克的白色雌性 Wistar 大鼠进行了降血脂活性研究。在实验中,建立并使用了吐温高脂血症模型:以 250 毫克/100 克体重的剂量一次性腹腔注射吐温-80。使用德国 DiaSys 公司生产的试剂在 RAL CLIMA MC-15 生化分析仪上进行血脂分析。结果。根据甘油三酯和极低密度脂蛋白的水平,发现植物复合物明显超过了参考药物(非诺贝特-卡农)的值。在孪生高脂血症的情况下,以 300 毫克/千克的剂量服用和预防性服用 Phacelia tanacetifolia 植物复方制剂有助于血清脂质代谢的正常化。
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引用次数: 0
MAIN METHODS OF QUALITY CONTROL OF BЕТА-BLOCKER DRUGS AND APPLICATION OF SPECTROPHOTOMETRY IN THE ANALYSIS OF ANTIANGIOGENIC OINTMENTS ON TIZOL GEL (REVIEW) bета-受体阻滞剂药物质量控制的主要方法以及分光光度法在蒂唑凝胶抗血管生成软膏分析中的应用(综述)
Pub Date : 2024-01-31 DOI: 10.29296/25877313-2024-01-06
M.I. Popova
Over th past decade, beta-blockers have shown their promise in the therapy of skin hemangiomas. Infantile hemangiomas are the most common soft tissue tumors occurring in 4-10% of children under the age of 1 year. Various methods are used to treat the disease: laser therapy, surgical exci-sion, cryodestruction, sclerosing, as well as conservative treatment with systemic glucocorticosteroids and beta-blockers administered enterally, topi-cally, and externally. Pharmacotherapy with the use of application dosage forms of beta-receptor antagonists is considered to be the most effective and safe method. This approach to treatment has several advantages over the oral method of administration: first, the convenience and painlessness of use, and secondly, the local effect on the pathological process, hence reducing the risk of systemic side effects (bradycardia, hypotension, bron-chospasm, insomnia). All these advantages emphasize the relevance of the development of soft dosage forms of beta-blockers. The patent RU 2471500 C2 “Use of beta-blocker for preparing drug for treating hemangiomas” proposes atenolol, betaxolol, bisoprolol, carvediol, metoprolol, nebivolol, propranolol and sotalol as antiangiogenic agents. The creation of soft dosage forms of beta-blockers with domestic transcutaneous enhancer Tizol gel is a solution to the problem of targeted delivery of active substances to the lesion site. For the development of new drugs, one of the most fundamen-tal areas of pharmaceutical science, pharmaceutical analysis, is of fundamental importance. The main objectives of pharmaceutical analysis are to determine the qualitative and quantitative characteristics of medicines. This article provides a review of the main methods for the analysis of beta-blockers used for the effective quality control of medicines, as well as methods for identifying, quantifying, and biopharmaceutically analyzing new ointments based on Tizol gel.
在过去十年中,β-受体阻滞剂在治疗皮肤血管瘤方面显示出了良好的前景。婴幼儿血管瘤是最常见的软组织肿瘤,在 1 岁以下的儿童中发病率为 4-10%。治疗方法多种多样:激光治疗、手术切除、冷冻、硬化剂注射,以及全身性糖皮质激素和β-受体阻滞剂的保守治疗,包括肠道给药、局部给药和外部给药。使用β受体拮抗剂的应用剂型进行药物治疗被认为是最有效、最安全的方法。与口服给药方法相比,这种治疗方法有几个优点:首先,使用方便、无痛苦;其次,对病理过程有局部作用,从而降低了全身副作用(心动过缓、低血压、支气管痉挛、失眠)的风险。所有这些优点都强调了开发β-受体阻滞剂软剂型的重要性。RU 2471500 C2 号专利 "使用β-受体阻滞剂配制治疗血管瘤的药物 "提出阿替洛尔、倍他洛尔、比索洛尔、卡维迪奥尔、美托洛尔、奈比洛尔、普萘洛尔和索他洛尔作为抗血管生成剂。用国产经皮增强剂 Tizol 凝胶制作β-受体阻滞剂的软剂型,可以解决将活性物质定向输送到病变部位的问题。对于新药开发而言,制药科学最基础的领域之一--药物分析至关重要。药物分析的主要目的是确定药物的定性和定量特征。本文综述了用于有效控制药品质量的 β-受体阻滞剂的主要分析方法,以及基于 Tizol 凝胶的新型软膏的鉴定、定量和生物制药分析方法。
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引用次数: 0
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Problems Of Biological, Medical And Pharmaceutical Chemistry
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