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Hexokinase and glycolysis: Between brain cells life and death 己糖激酶和糖酵解:脑细胞生死之间
Pub Date : 2023-05-10 DOI: 10.2174/2212796817666230510095530
M. de Cerqueira César, Larissa Rodrigues Souza da Mata, Lais Damásio dos Santos
Hexokinase catalyses the first regulatory step of the glycolytic pathway. We can say without any exaggeration that both hexokinase and glycolysis are involved in the control of brain cells' lifeand death. To perform these pivotal roles, hexokinase occurs in four different isoforms in mammaliancells. Type I isozyme is best suited for energy generation, introducing glucose in glycolysis. In contrast, Type II and Type III isoforms product is directed to generation of NADPH through the pentosephosphate pathway, utilized in biosynthetic processes. Nevertheless, hexokinase has another uniqueproperty to accomplish its multiple functions: the capacity for mitochondrial binding. Linked to itsrole in apoptosis control, the binding of hexokinase inhibits the action of apoptosis inducers, such asBax, from initiating the release of intramitochondrial proteins. Akt mediates HKII binding to mitochondria. Overexpression of the phosphatase SHIP2 reduces Akt activity and enhances apoptosis, emphasizing the role of hexokinase in cell death. Furthermore, hexokinase also participates in cellularsignaling and functional regulation. Adding complexity to this multidimensional enzyme´s attributes,glycolysis occurs in aerobic or anaerobic situations. “Aerobic glycolysis” participates in the control ofcell excitability, in synapse formation and neurite growth. Here we provide an overview of the multiple roles of hexokinase and glycolysis in neuronal metabolic association with astrocytes, oligodendrocytes, and microglia. We also provide an update on the role of hexokinase and glycolysis in microgliaactivation and in brain aging and neurodegenerative diseases.
己糖激酶催化糖酵解途径的第一个调控步骤。我们可以毫不夸张地说,己糖激酶和糖酵解都参与控制脑细胞的生死。为了发挥这些关键作用,己糖激酶在哺乳动物细胞中有四种不同的亚型。I型同工酶最适合产生能量,在糖酵解过程中引入葡萄糖。相比之下,II型和III型同工异构体的产物通过戊二磷酸途径产生NADPH,用于生物合成过程。然而,己糖激酶有另一个独特的特性来完成它的多种功能:线粒体结合的能力。与其在细胞凋亡控制中的作用有关,己糖激酶的结合抑制了细胞凋亡诱导剂(如bax)的作用,使其无法启动线粒体内蛋白的释放。Akt介导HKII与线粒体的结合。磷酸酶SHIP2过表达降低Akt活性,促进细胞凋亡,强调己糖激酶在细胞死亡中的作用。此外,己糖激酶还参与细胞信号传导和功能调节。糖酵解在有氧或无氧情况下发生,使这种多维酶的属性更加复杂。“需氧糖酵解”参与控制细胞兴奋性、突触形成和神经突生长。在这里,我们概述了己糖激酶和糖酵解在星形胶质细胞、少突胶质细胞和小胶质细胞的神经元代谢关联中的多种作用。我们还提供了己糖激酶和糖酵解在小胶质细胞激活、脑老化和神经退行性疾病中的作用的最新进展。
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引用次数: 0
Medicinal, pharmacological and biochemical progress on the study of genus Helianthemum: A review 菊花属植物的药用、药理和生化研究进展综述
Pub Date : 2023-02-27 DOI: 10.2174/2212796817666230227112835
Soumia Mouffouk, Chaima Mouffouk, Sara Mouffouk, Hamada Haba
The genus Helianthemum from the Cistaceae family includes about 110 plants, which are well known for their wide therapeutic uses and interesting pharmacological activities. To the best of our knowledge, there are no previous comprehensive and critical reviews on the therapeutic applications, chemical composition, and biological properties of this genus.In this context, the present paper describes a systematic mini-review on the traditional use, phytochemical composition, and pharmacological properties of species belonging to the genus Helianthemum.For this, more than 75 papers covering the period from 1970 to 2022 were collected and analyzed to achieve this review.From 110 species of the genus Helianthemum, only 22 species were studied. Helianthemum species are widely used in folk medicine for the treatment of respiratory, hepatic, renal, psychiatric, and inflammatory diseases. According to the collected information, species from this genus have several pharmacological properties linked to their rich chemical composition, particularly in phenolic compounds and flavonoids. In fact, Helianthemum plants have antioxidant, antimicrobial, anti-inflammatory, analgesic, antidiabetic, insecticide, anticancer, antiulcer, larvicide, chemo, and hepatoprotective activities, justifying their various uses in traditional medicine.Despite the intense use of Helianthemum species in traditional human and veterinary medicine, few studies were conducted on the phytochemical composition and pharmacological activities of the plants constituting this genus. In fact, until now, the emphasis has only been on twenty-two species and the work carried out was not explanatory, especially for certain species. So it will be interesting to broaden the spectrum of the tested biological activities, especially for endemic species in order to understand the possible modes of action and to confirm the toxicity of certain species.
菊花属(Helianthemum)是蓟科植物,约有110种,以其广泛的治疗用途和有趣的药理活性而闻名。据我们所知,在此之前没有对该属的治疗应用、化学成分和生物学特性进行全面和批判性的综述。在此背景下,本文对菊花属植物的传统用途、植物化学成分和药理特性进行了系统的综述。为此,我们收集和分析了1970年至2022年期间的75多篇论文,以实现这一综述。在110种菊花属植物中,只研究了22种。菊花在民间医学中被广泛用于治疗呼吸、肝脏、肾脏、精神和炎症疾病。根据收集到的信息,该属植物具有多种药理特性,这与它们丰富的化学成分有关,特别是酚类化合物和类黄酮。事实上,菊花具有抗氧化、抗菌、抗炎、镇痛、抗糖尿病、杀虫、抗癌、抗溃疡、杀幼虫、化疗和保护肝脏的活性,这证明了它们在传统医学中的各种用途。尽管菊花在传统的人兽医学中被广泛使用,但对其植物化学成分和药理活性的研究却很少。事实上,到目前为止,重点只放在22个物种上,所开展的工作并没有解释,特别是对某些物种。因此,拓宽测试生物活性的范围,特别是针对特有物种,以了解可能的作用模式并确认某些物种的毒性,将是一件有趣的事情。
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引用次数: 0
Efficacy and Biomedical Roles of Unsaturated Fatty Acids as Bioactive Food Components 不饱和脂肪酸作为生物活性食品成分的功效和生物医学作用
Pub Date : 2023-02-22 DOI: 10.2174/2212796817666230222103441
Morteza Vaezi
Unsaturated fatty acids (UFAs) as bioactive compounds possess a wide range of biomedical functions and a lack or shortage of them may cause serious harm to human body health. Biochemically, UFAs have attracted growing interest, and this attention arises not only from biomedical reasons but also economic ones. Among these fatty acids, omega-3 and omega-6 fatty acids are considered the most efficient and safe compounds which can be used for expanding and identification of novel functionalities. They are considered essential membrane components and are associated with a variety of biological processes. For example, eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) as polyunsaturated fatty acids (PUFAs) play a central role in the proper functioning of the nervous system like anti-atherogenic properties and improve the functioning of the cardiovascular system. Briefly, understanding the relationship between these properties and potential biomedical applications of UFAs may help to elucidate and facilitate the development of novel pathogenesis strategies regarding their disorders in human health and diseases. This review provides the most suitable functional roles and potential mechanisms of UFAs associated with human health and nutrition.
不饱和脂肪酸作为一种生物活性化合物,具有广泛的生物医学功能,缺乏不饱和脂肪酸会对人体健康造成严重危害。生物化学方面,ufa引起了越来越多的兴趣,这种关注不仅来自生物医学原因,而且来自经济原因。在这些脂肪酸中,omega-3和omega-6脂肪酸被认为是最有效和安全的化合物,可用于扩展和鉴定新的功能。它们被认为是必不可少的膜成分,并与多种生物过程有关。例如,二十碳五烯酸(EPA)和二十二碳六烯酸(DHA)作为多不饱和脂肪酸(PUFAs)在神经系统的正常功能中发挥着核心作用,如抗动脉粥样硬化特性和改善心血管系统的功能。简而言之,了解这些特性与ufa潜在的生物医学应用之间的关系可能有助于阐明和促进有关其在人类健康和疾病中的失调的新发病策略的发展。本文综述了不饱和脂肪酸与人体健康和营养相关的最合适的功能作用和可能的机制。
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引用次数: 0
Hydroalcoholic Extract of Achillea Wilhelmsii Decreases the Expressions of Hippo Signaling Pathway-Associated Oncogenes In the A549 Lung Cancer Cell Line 水醇提取物降低A549肺癌细胞系中Hippo信号通路相关癌基因的表达
Pub Date : 2023-02-14 DOI: 10.2174/2212796817666230214100146
M. Ashtiani, Fariba Nabatchian, M. Davoudi, Negin Davoudi, Reza Afrisham
this study aimed to evaluate the effect of the hydroalcoholic extract of this plant on viability and mRNA expression of some Hippo signaling pathway-associated oncogenes and suppressors in A549 lung cancer cell lines.Evidence suggests that the Hippo pathway, which regulates organ size, is altered in a few conditions like lung cancer. Achillea wilhelmsii that used in the traditional Iranian medicine to treat a variety of disorders has been proven to contribute to some signaling pathways in cancers. In this regards, this study aimed to evaluate the effect of the hydroalcoholic extract of this plant on viability and mRNA expression of some Hippo signaling pathway-associated oncogenes and suppressors in A549 lung cancer cell lines.this study aimed to evaluate the effect of the hydroalcoholic extract of this plant on viability and mRNA expression of some Hippo signaling pathway-associated oncogenes and suppressors in A549 lung cancer cell lines.Hydroalcoholic extract was prepared using a Soxhlet extractor and its antiproliferative activity was studied by MTT assay. Then, the mRNA expressions of large tumour suppressor kinases 1 and 2 (LATS1 and LATS2), Yes1 Associated Transcriptional Regulator (YAP1), and Transcriptional co‑activator with PDZ‑binding motif (TAZ) were measured using real-time PCR.According to MTT, the viability was decreased significantly after 24 hours treatment with A. wilhelmsii at concentrations of 200-1000 µg/ml and after 48 hours treatment at a concentration of 100-1000 µg/ml. While the mRNA levels of LATS1, TAZ, and YAP1 decreased significantly compared to untreated cells, the mRNA expression of LATS2 did not change (P˂ 0.05).Hydroalcoholic extract of A. wilhelmsii might inhibit proliferation of lung cancer cells as well as it could decrease the expression of both oncogenes in them. However, it had suppressing effects on LATS1, which should be considered in further studies.none
本研究旨在评估该植物水酒精提取物对A549肺癌细胞株中Hippo信号通路相关癌基因和抑制基因mRNA表达的影响。有证据表明,在肺癌等少数疾病中,调节器官大小的河马通路发生了改变。在伊朗传统医学中用于治疗各种疾病的阿基里斯已经被证明有助于癌症的一些信号通路。因此,本研究旨在评价该植物水酒精提取物对A549肺癌细胞株中Hippo信号通路相关癌基因和抑制基因mRNA表达的影响。本研究旨在评估该植物水酒精提取物对A549肺癌细胞株中Hippo信号通路相关癌基因和抑制基因mRNA表达的影响。采用索氏提取法制备了水酒精提取物,并采用MTT法研究了其抗增殖活性。然后,利用实时荧光定量PCR检测大肿瘤抑制激酶1和2 (LATS1和LATS2)、Yes1相关转录调控因子(YAP1)和PDZ结合基序转录辅激活因子(TAZ)的mRNA表达。MTT结果显示,200 ~ 1000µg/ml的浓度处理24 h, 100 ~ 1000µg/ml的浓度处理48 h后,细胞活力显著降低。与未处理的细胞相比,LATS1、TAZ和YAP1的mRNA表达量显著降低,而LATS2的mRNA表达量没有变化(P小于0.05)。水醇提取物对肺癌细胞的增殖有抑制作用,并能降低肺癌细胞中两种致癌基因的表达。但其对LATS1有抑制作用,应在进一步研究中加以考虑
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引用次数: 0
Traditional use, phytochemistry and pharmacological properties of the genus Onopordum 牛孔草属植物的传统用途、植物化学和药理性质
Pub Date : 2023-01-02 DOI: 10.2174/2212796817666230102092008
Chaima Mouffouk, Soumia Mouffouk, Sara Mouffouk, Hamada Haba
The genus Onopordum (Asteraceae), with about 40 species, is composed ofperennials and spermatophyte plants, which are widely used in popular medicine for the treatment ofseveral human diseases. Plants of this genus constitute an interesting source of bioactive moleculeswith a wide range of pharmacological applications.In this context, the current study describes a critical review of traditional uses, phytochemistry, and pharmacological effects of the genus Onopordum in order to establish a valuable databasefor future ethnopharmacological surveys on this genus.For this, all bibliographic data covering the period of 1970 to 2022 were collected and analyzed.Only 19 species from the genus Onopordum were studied. They are traditionally used to treatgastric, renal, respiratory, urinary, and gynecological diseases and in the food industry for cheese production. Indeed, it was found that Onopordum species are rich in flavonoids, phenolic compounds,terpenoids, alkaloids, tannins, and steroids. These plants exhibit several interesting biological activities including: antioxidant, antimicrobial, antiproliferative, apoptotic, cytotoxic, antitumor, anticholinergic, larvicidal, analgesic and antipyretic, hypotensive, antiepileptic, and anticonvulsant activities.Furthermore, their hemostatic, anti-inflammatory, and moisturizing properties, increase their usefulness in the cosmetic field.According to the present study, Onoporadum species constitute an important naturalsource of secondary metabolites with potential therapeutic, cosmetic, and nutritional applications.However, the focus has been only on 19 species and the publications were not very explanatory,Therefore, in-depth pharmacological and phytochemical studies are needed to fully exploit the therapeutic potential and the chemical composition of Onopordum species.
Onopordum属(Asteraceae)由多年生植物和精子植物组成,约有40种,被广泛用于治疗几种人类疾病的常用药物中。本属植物是一种有趣的生物活性分子来源,具有广泛的药理应用。在此背景下,本研究对蛇孔草属的传统用途、植物化学和药理作用进行了综述,以便为该属的未来民族药理学调查建立一个有价值的数据库。为此,收集和分析了1970年至2022年期间的所有书目数据。本文只研究了蛇孔属的19种。它们传统上用于治疗胃、肾、呼吸、泌尿和妇科疾病,并在食品工业中用于奶酪生产。事实上,人们发现Onopordum物种富含类黄酮、酚类化合物、萜类、生物碱、单宁和类固醇。这些植物具有抗氧化、抗菌、抗增殖、细胞凋亡、细胞毒性、抗肿瘤、抗胆碱能、杀幼虫、镇痛解热、降压、抗癫痫和抗惊厥等生物活性。此外,它们的止血、消炎和保湿特性,增加了它们在化妆品领域的用途。根据目前的研究,Onoporadum是次生代谢物的重要天然来源,具有潜在的治疗、美容和营养用途。然而,目前研究的重点仅局限于19种,文献解释也不够充分。因此,需要深入的药理和植物化学研究,以充分挖掘其治疗潜力和化学成分。
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引用次数: 0
Insights Into Resveratrol as an Inhibitor Against Aβ1-42 Peptide Aggregation: A Molecu-lar Dynamics Simulation Study 白藜芦醇作为A - β1-42肽聚集抑制剂的见解:分子动力学模拟研究
Pub Date : 2022-12-21 DOI: 10.2174/2212796817666221221151713
V. S. Mattaparthi, P. Borah
Resveratrol (RSV), a polyphenolic compound, is reported to have anti-aggregation properties against Amyloid-beta peptides. It is, therefore, significant to understand the mechanism of inhibition of Aβ1-42 peptide aggregation by the RSV at the molecular level. We have used Molecular docking along with Molecular dynamics (MD) simulation techniques to address the role of RSV in the inhibition of Aβ1-42 pep-tide aggregation.To understand the role of Resveratrol on the Aβ1-42 peptide aggregation.In this computational study, we have docked the RSV to Aβ1-42 peptide using Molecular Docking software and then performed MD simulation for the Aβ1-42 peptide monomer Aβ1-42 peptide-RSV complex using the AMBER force field. From the analysis of MD trajectories, we obtained salient structural features and determined the Binding Free Energy(BFE) and Per-residue Energy Decomposition Analysis (PRED) using MM-PBSA/GBSA method.The secondary structure and the conformational analysis obtained from MD trajectories show that the binding of RSV with the Aβ1-42 peptide monomer causes an increase in the helical content in the structure of the Aβ1-42 peptide. The BFE and PRED results show a high binding affinity (GBtotal=-11.07 kcal mol-1; PBtotal= -1.82 kcal mol-1) of RSV with Aβ1-42 peptide. Also, we found the RSV to interact with cru-cial residues (Asp 23 and Lys 28) of the Aβ1-42 peptide. These residues play a signif-icant role in facilitating the formation of toxic amyloid oligomers and amyloid fibrils. The salt bridge interaction between these residues D23–K28 was found to be destabi-lized in the Aβ1-42 peptide when it is complexed with RSV.In summary, it can be concluded that Resveratrol greatly aids the preven-tion of Aβ1-42 peptide aggregation. Therefore, it can be considered a possible drug candidate for therapeutic strategies for Alzheimer’s disease.
白藜芦醇(Resveratrol, RSV)是一种多酚类化合物,据报道具有抗淀粉样蛋白- β肽聚集的特性。因此,从分子水平上了解RSV对a - β1-42肽聚集的抑制机制具有重要意义。我们使用分子对接和分子动力学(MD)模拟技术来解决RSV在抑制a - β1-42肽聚集中的作用。了解白藜芦醇在a - β1-42肽聚集中的作用。在本计算研究中,我们利用分子对接软件将RSV与Aβ1-42肽对接,然后利用AMBER力场对Aβ1-42肽单体Aβ1-42肽-RSV复合物进行MD模拟。利用MM-PBSA/GBSA方法测定了结合自由能(Binding Free Energy, BFE)和每残基能量分解分析(Per-residue Energy Decomposition analysis, PRED)。二级结构和MD轨迹的构象分析表明,RSV与a - β1-42肽单体结合导致a - β1-42肽结构中的螺旋含量增加。BFE和PRED结果显示出较高的结合亲和力(GBtotal=-11.07 kcal mol-1;PBtotal= -1.82 kcal mol-1)。此外,我们发现RSV与a - β1-42肽的关键残基(Asp 23和Lys 28)相互作用。这些残基在促进有毒淀粉样蛋白低聚物和淀粉样蛋白原纤维的形成中起着重要作用。当a - β1-42肽与RSV络合时,这些残基D23-K28之间的盐桥相互作用被发现是不稳定的。综上所述,白藜芦醇对a - β1-42肽聚集具有显著的抑制作用。因此,它可以被认为是阿尔茨海默病治疗策略的可能候选药物。
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引用次数: 0
Benzeneseleninic acid promoting the selenofunctionalization of 2-naphthol derivatives: Synthesis and antioxidant activity of 1-organoselanyl-naphthalen-2-ols 苯亚硒酸促进2-萘酚衍生物的硒化:1-有机塞拉烷-萘-2-醇的合成及其抗氧化活性
Pub Date : 2022-12-20 DOI: 10.2174/2212796817666221220100340
G. Perin, Daniela H. Mailahn, D. R. Araújo, P. Nobre, C. A. Fonseca, Filipe Penteado, E. Lenardão, C. Luchese, E. A. Wilhelm
We report the synthesis and antioxidant evaluation of 1-organoselanyl-naphthalen-2-ols. The title compounds were selectively prepared through the selenofunctionalization of 2-naphthol derivatives using benzeneseleninic acids as a selenium source.We aimed at synthesizing 1-organoselanyl-naphthalen-2-ol by functionalizing 2-naphthol with arylseleninic acids using glycerol as the solvent and further evaluating the pharmacological activity.The products were synthesized at 70 °C using glycerol as a solvent in an oil bath. Reactive species (RS) tests, DPPH radical scavenging activity assay, and ABTS+ radical scavenging activity assay were performed. A statistical analysis of the data was performed.A total of fifteen 1-organoselanyl-naphthalen-2-ols were selectively obtained in yields of 58-95% in 0.25-48 h of reaction. Additionally, all the synthesized seleno-derivatives exhibited antioxidant activity, as revealed by their ability to scavenge DPPH and ABTS+ radicals and reduce the reactive species (RS) levels.The synthesis of 1-arylselanyl-naphthalen-2-ols was developed under mild reaction conditions using benzeneseleninic acid derivatives in reactions with 2-naphthol. All synthesized 2-naphthol derivatives exhibited antioxidant activity, as revealed by their DPPH and ABTS+ radical scavenging activity and reduced RS levels.
本文报道了1-有机塞拉基萘-2-醇的合成及其抗氧化性评价。以苯硒酸为硒源,通过2-萘酚衍生物的硒功能化选择性制备了标题化合物。以丙三醇为溶剂,用芳基亚硒酸对2-萘酚进行功能化,合成1-有机塞拉基-萘-2-醇,并进一步评价其药理活性。产物以甘油为溶剂,在70℃油浴中合成。进行活性物质(RS)测定、DPPH自由基清除活性测定和ABTS+自由基清除活性测定。对数据进行统计分析。在0.25 ~ 48 h的反应时间内,选择性地得到了15种1-有机塞拉烷-萘-2-醇,收率为58 ~ 95%。此外,所有合成的硒衍生物都具有抗氧化活性,可以清除DPPH和ABTS+自由基,降低活性物质(RS)水平。以苯乙烯酸衍生物与2-萘酚为原料,在温和反应条件下合成了1-芳基selanyl-萘-2-醇。所有合成的2-萘酚衍生物均具有抗氧化活性,表明其具有清除DPPH和ABTS+自由基的活性,并降低了RS水平。
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引用次数: 1
A Systematic Review Study on the Effectiveness of Medicinal Plants against Acinetobacter baumannii 药用植物抗鲍曼不动杆菌效果的系统综述研究
Pub Date : 2022-12-08 DOI: 10.2174/2212796817666221208115047
P. Shakib, A. Manouchehri, A. Marzban, H. Esmaeil Lashgarian, A. Alhameedawi
Acinetobacter baumannii is an opportunistic bacterium capable of causing nosocomial infections resistant to a wide range of antibiotics. Herbal medicines could become the source of novel therapies for antibiotic-resistant bacteria. This review paper aimed to survey the effectiveness of medicinal plants in treating infections caused by A. baumannii.The relevant data was obtained by systematically searching PubMed, ISI Web of Science, Scopus, Science Direct, and Google Scholar databases with the specific keywords of medicinal plants (including extracts and essential oils) and bacterial infections (including A. baumannii).The present review identified 23 studies published between 2009 and 2021 that discussed the effectiveness of medicinal plants in inhibiting the growth of A. baumannii. In these studies, 28 medicinal plants were found effective against infection caused by A. baumannii in vivo.The results of this review indicated that to develop a therapeutic strategy for treating bacterial infections, especially A. baumannii, based on medicinal plants, extensive studies were required to determine their cytotoxicity and therapeutic dosage before they could be used as an alternative to antibiotics.
鲍曼不动杆菌是一种机会性细菌,能够引起对多种抗生素耐药的医院感染。草药可能成为治疗耐抗生素细菌的新疗法的来源。本文综述了药用植物对鲍曼不动杆菌感染的治疗效果。通过系统检索PubMed、ISI Web of Science、Scopus、Science Direct、谷歌Scholar等数据库,以药用植物(包括提取物和精油)和细菌感染(包括鲍曼不对称杆菌)为特定关键词获取相关数据。本综述确定了2009年至2021年间发表的23项研究,这些研究讨论了药用植物抑制鲍曼不整虫生长的有效性。在这些研究中,发现28种药用植物在体内对鲍曼不动杆菌感染有效。本综述的结果表明,为了开发一种基于药用植物治疗细菌感染的治疗策略,特别是鲍曼不动杆菌,在将其作为抗生素的替代品之前,需要进行广泛的研究,以确定其细胞毒性和治疗剂量。
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引用次数: 0
Adaptogenic Properties of 1-(Germatran-1-il)-Oxyethylamine 1-(日耳曼-1-il)-氧乙胺的适应性
Pub Date : 2022-12-05 DOI: 10.2174/2212796817666221205164816
I. Zhigacheva, Natalya I. Kricunova, M. Rasulov
Germanium is a biologically active trace element, and it is present in almost all or-gans and tissues. Its biological activity was revealed in the 20th century. However, the study on the possibility of using germanium for medical purposes was first undertaken by the Japanese sci-entist Dr. Kazuhiko Asai in 1940. In 1965, academician M.G.Voronkov and colleagues synthe-sized tricyclic esters of triethanolamine germanium with the general formula XGe(OCH2CH2)3N and studied their biological activity. However, the adaptogenic properties of these compounds have not been sufficiently studied. In this regard, there is an urgent need to study the adaptogen-ic properties of these drugs.As the resistance of the organism to stress factors primarily depends on energy metabolism, the aim of our work was to study the influence of stress and 1- (germatran-1-il) –oxyethylamine (GM) on the functional state of mitochondria.The functional state of mitochondria was studied as per the rate of mitochon-dria respiration by the level of lipid peroxidation and fatty acid composition of mitochondrial membranes by chromatography technique.It was shown that the drug in concentrations of 10-5, 10-6, and 10-11M reduced the intensity of LPO in the membranes of "aged" mitochondria. This can serve as evidence re-garding the presence of anti-stress properties in the drug. Injection of GM at a dose of 10-5 mol/kg to rats prevented the activation of LPO in the membranes of the liver mitochondria in conditions of acute hypobaric hypoxia. To restrict lipid peroxidation, GM prevented changes in the content of C18 and C22 fatty acids in mitochondrial membranes, which probably contributed to maintaining the bioenergetic characteristics of mitochondria at the control level.It is assumed that the anti-stress activity of the drug is associated with its antioxidant properties and its effect on the complex I of the mitochondrial respiratory chain.
锗是一种具有生物活性的微量元素,它几乎存在于所有的器官和组织中。它的生物活性在20世纪被发现。然而,关于将锗用于医疗目的的可能性的研究是由日本科学家浅井和彦博士于1940年首先进行的。1965年,m.g.w oronkov院士等以通式XGe(OCH2CH2)3N合成了三乙醇胺锗三环酯,并对其生物活性进行了研究。然而,这些化合物的适应性还没有得到充分的研究。因此,迫切需要对这些药物的适应原特性进行研究。由于机体对应激因子的抵抗主要依赖于能量代谢,我们的工作目的是研究应激和1- (germatran-1-il) -氧乙胺(GM)对线粒体功能状态的影响。用层析法测定线粒体膜脂质过氧化水平和脂肪酸组成,根据线粒体呼吸速率研究线粒体功能状态。结果表明,10-5、10-6和10-11M浓度的药物可降低“衰老”线粒体膜上LPO的强度。这可以作为药物中抗应激特性存在的证据。大鼠注射10-5 mol/kg剂量的GM可阻止急性低压缺氧条件下肝线粒体膜LPO的活化。为了限制脂质过氧化,转基因抑制了线粒体膜中C18和C22脂肪酸含量的变化,这可能有助于将线粒体的生物能特性维持在控制水平。据推测,该药物的抗应激活性与其抗氧化特性及其对线粒体呼吸链复合体I的影响有关。
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引用次数: 0
Tellurium-containing thiol-peroxidase-like antioxidants and their catalytic mechanism 含碲硫醇过氧化物酶类抗氧化剂及其催化机理
Pub Date : 2022-11-21 DOI: 10.2174/2212796817666221121155138
D. Tanini, A. Capperucci
The development of novel small molecules with effective catalytic antioxidant properties is highly sought after. A wide array of structurally diverse selenium- and tellurium-containing glutathione peroxidase mimics have been studied over the past two decades. Within this arena, organotellurium compounds generally exhibit higher catalytic properties with respect to selenium-containing analogues. Different mechanisms accounting for the thiol-peroxidase-like activity of various classes of organotellurium derivatives have been proposed. This review document develops this area and provides an overview of the catalytic mechanisms proposed for the various classes of tellurium-containing thiol-peroxidase-like-catalysts.
具有有效催化抗氧化性能的新型小分子材料的开发备受关注。在过去的二十年里,人们对一系列结构多样的含硒和含碲谷胱甘肽过氧化物酶模拟物进行了研究。在这一领域,有机碲化合物通常比含硒类似物表现出更高的催化性能。不同类型的有机碲衍生物具有巯基过氧化物酶样活性的机理已被提出。本文综述了这一领域的发展,并对各类含碲硫醇过氧化物酶类催化剂的催化机理进行了综述。
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引用次数: 0
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Current Chemical Biology
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