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SYNTHESIS AND ANTIOXIDANT ACTIVITY OF SOME AMINOADAMANTANE DERIVATIVES 一些氨基金刚烷衍生物的合成和抗氧化活性
Q3 Engineering Pub Date : 2024-07-05 DOI: 10.59957/jctm.v59.i4.2024.15
Antoniya Stoymirska, R. Chayrov, A. Georgieva, E. Tsvetanova, A. Alexandrova, I. Stankova
Chronic fatigue syndrome (CFS) and neurocognitive deficits are a major problem of modern society. The etiology of CFS remains unclear, however, a large number of recent studies have shown oxidative stress may be involved in its pathogenesis. Fatigue is frequent and important in the lives of Parkinson’s disease (PD) patients. 1-amino-adamantane (amantadine and memantine) derivatives has been proposed to be useful in the treatment of Parkinson’s and Alzheimer’s diseases. Its beneficial effect has been related to its novel properties as an N-methyl-D-aspartate receptor (NMDAR) blocker which can neutralize the effect of glutamate at striatal and subthalamic levels. We synthesized and evaluated the antioxidant activity of eleven new aminoadamantane derivatives. Their antioxidant activity has been evaluated using different (superoxide anion, hydroxyl) radical generating systems. The compoundwith s highest anti-oxidative capacity contain 2-(Benzhydrylsulfinyl) substituent.
慢性疲劳综合征(CFS)和神经认知缺陷是现代社会的一个主要问题。慢性疲劳综合征的病因尚不清楚,但最近的大量研究表明,氧化应激可能与慢性疲劳综合征的发病机制有关。疲劳是帕金森病(PD)患者生活中经常出现的重要症状。1-氨基金刚烷(金刚烷胺和美金刚)衍生物被认为可用于治疗帕金森病和阿尔茨海默病。其有益效果与其作为 N-甲基-D-天冬氨酸受体(NMDAR)阻断剂的新特性有关,该阻断剂可中和谷氨酸在纹状体和丘脑下水平的作用。我们合成并评估了 11 种新的氨基金刚烷衍生物的抗氧化活性。我们使用不同的(超氧阴离子、羟基)自由基生成系统对它们的抗氧化活性进行了评估。抗氧化能力最强的化合物含有 2-(二苯甲基亚磺酰基)取代基。
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引用次数: 0
STRUCTURAL REQUIREMENTS OF ANGIOTENSIN RECEPTOR: PREFERRED MODIFICATIONS FOR ANTAGONIST DESIGN 血管紧张素受体的结构要求:拮抗剂设计的首选修饰
Q3 Engineering Pub Date : 2024-07-05 DOI: 10.59957/jctm.v59.i4.2024.16
T. Dzimbova, Atanas Chapkanov
Blood pressure and fluid balance are regulated hormonally by renin-angiotensin system (RAS). Influence on this system could be achieved by different compounds that act as angiotensin-converting enzyme inhibitors (ACE inhibitors), angiotensin receptor blockers and renin inhibitors. The purpose of the present study is to predict the structures of the potent ACE inhibitors on the base of His-Leu peptide structural element of angiotensine I using computational methods. Different modifications were made in the structure of this dipeptide and the energy of binding with the enzyme were calculated. The docking results were analyzed and it was found that along with the important amino acid residue of the receptor molecule Arg167, the Tyr residues (35, 87, 88 and 92) as well as Cys180 areextremely important for the strong binding to the receptor and, accordingly, the manifestation of antagonistic action by the analogues. To block the receptor, the ligand molecule must have an intact terminal carboxyl group and an imidazole nucleus to participate in appropriate interactions. The inclusion of functional groups in the side chains of the amino acid residues of the dipeptide create an additional site for binding to the receptor. With the help of docking, the ligand molecule can be optimized, and this process is fast,  aving the synthesis of many compounds and their biological testing. And finally, the most potent analogues will be synthesized and biologically tested. 
血压和体液平衡受肾素-血管紧张素系统(RAS)的激素调节。不同的化合物可作为血管紧张素转换酶抑制剂(ACE 抑制剂)、血管紧张素受体阻滞剂和肾素抑制剂对该系统产生影响。本研究的目的是以血管紧张素 I 的 His-Leu 肽结构元素为基础,利用计算方法预测强效 ACE 抑制剂的结构。对该二肽的结构进行了不同的修饰,并计算了与酶结合的能量。对对接结果进行分析后发现,除了受体分子的重要氨基酸残基 Arg167 外,Tyr 残基(35、87、88 和 92)以及 Cys180 对于与受体的强结合以及类似物的拮抗作用的表现也极为重要。要阻断受体,配体分子必须具有完整的末端羧基和咪唑核,才能参与适当的相互作用。在二肽的氨基酸残基侧链中加入功能基团,可为与受体的结合创造一个额外的位点。在对接的帮助下,配体分子可以得到优化,这一过程非常迅速,可以合成许多化合物并对其进行生物测试。最后,将合成最有效的类似物并进行生物测试。
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引用次数: 0
COMPUTATIONAL MODELING OF COMPOUNDS THAT INTERACT WITH OPIOID AND CANNABINOID RECEPTORS 与阿片和大麻素受体相互作用的化合物的计算建模
Q3 Engineering Pub Date : 2024-07-05 DOI: 10.59957/jctm.v59.i4.2024.17
Fatima Sapundzhi, T. Dzimbova
The present study was designed to investigate the structure-activity relationship between cannabinoid and opioid ligands with models of cannabinoid and opioid receptors. There are differences in the mechanisms of pain control for these two types of receptors, but targeting the creation of compounds that bind to both opioid and cannabinoid receptors lead to more effective solving of this problem. This will lead to the development of new and improved strategies to prevent opiate addiction and its consequences.
本研究旨在利用大麻素受体和阿片受体模型研究大麻素配体和阿片配体之间的结构-活性关系。这两类受体的疼痛控制机制存在差异,但针对同时与阿片类受体和大麻素受体结合的化合物的研究将更有效地解决这一问题。这将有助于开发新的改良策略,预防阿片类药物成瘾及其后果。
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引用次数: 0
BENZYDAMINE HYDROCHLORIDE IMMOBILIZATION IN MULTILAYER STRUCTURES BASED ON LYOPHILIZED COMPOSITE POLYLACTIC ACID / POLY(Ε-CAPROLACTONE) SUBSTRATES 基于冻干复合聚乳酸/聚(ε-己内酯)基底的多层结构中盐酸苄达明的固定作用
Q3 Engineering Pub Date : 2024-07-05 DOI: 10.59957/jctm.v59.i4.2024.10
A. Viraneva, M. Marudova, A. Grigorov, T. Yovcheva
In the present paper the polyelectrolyte multilayers (PEMs) deposited on lyophilized composite polylactic acid / poly(ε-caprolactone) substrates were investigated. The substrates were charged under positive corona discharge for 1 min with 5 kV voltage applied to the corona electrode and 1 kV voltage of the same polarity applied to the grid. The dependences on the time of storage of the normalized surface potential of the charged substrates (positive) were investigated. Solutions of 1 % casein in phosphate buffer (pH 8) and 0.1 % chitosan in acetate buffer (pH 5) with added benzydamine hydrochloride were prepared. The creation of the multilayers was carried out by utilizing the technique Layer-by-Layer (LbL). The first built-up layer always possesses an electric charge opposite to that of the substrate. The loading efficiency and drug release kinetics of the chosen model drug were carried out spectrophotometrically.
本文研究了沉积在冻干复合聚乳酸/聚(ε-己内酯)基底上的聚电解质多层膜(PEMs)。基底在正电晕放电条件下充电 1 分钟,在电晕电极上施加 5 kV 电压,在栅极上施加相同极性的 1 kV 电压。研究了带电基底(正极)的归一化表面电位与存储时间的关系。制备了磷酸缓冲液(pH 值为 8)中的 1 % 酪蛋白溶液和醋酸盐缓冲液(pH 值为 5)中的 0.1 % 壳聚糖溶液,并添加了盐酸苄达明。多层膜是通过逐层叠加(LbL)技术制成的。第一层形成的多层总是带有与基底相反的电荷。用分光光度法测定了所选模型药物的负载效率和药物释放动力学。
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引用次数: 0
EVALUATION OF ANTIOXIDANT PROPERTIES AND PHYTOCHEMICAL COMPOSITION IN VARIETAL HONEYS 评价各种蜂蜜的抗氧化特性和植物化学成分
Q3 Engineering Pub Date : 2024-07-05 DOI: 10.59957/jctm.v59.i4.2024.4
Petranka Petrova, J. Mrmošanin, Stefan Petrović, M. Chochkova, Vesna Stankov Jovanović
A total of fourteen honey samples, including monofloral, polyfloral, and honeydew honeys, collected from Bulgaria, Turkiye, and Morocco were analyzed with the aim to investigate the influence of floral origin on the biological properties of honey.The antioxidant activities of the samples were estimated using the DPPH, ABTS, FRAP, and CUPRAC methods, as well as analyzing their phytochemical composition by measuring the total phenolic content through the Folin-Ciocalteu method and individual polyphenols by HPLC.The results demonstrated that honeydew honey exhibited the highest total phenolic content and antioxidant activity among all the samples tested. It was followed by linden and forest honeys, which also demonstrated significant biological activity. In contrast, acacia and ziziphus honeys displayed the lowest levels of phenolic content and antioxidant properties among the samples.Our results indicated that while the botanical origin of honey had a significant influence on its biological properties, other factors such as geographical location also played a role in determining its quality. The observed variations among the honey samples from the same botanical origin could be attributed to factors such as specific landscape conditions, including whether the honey was sourced from an urban or rural area, the timing of harvest, beekeeping practices, and storage conditions.
研究人员分析了从保加利亚、土耳其和摩洛哥采集的 14 种蜂蜜样品,包括单花蜜、多花蜜和蜜露蜜,目的是研究花源对蜂蜜生物特性的影响。采用 DPPH、ABTS、FRAP 和 CUPRAC 方法估算了样品的抗氧化活性,并通过 Folin-Ciocalteu 方法测定了总酚含量,采用 HPLC 方法测定了单个多酚含量,从而分析了它们的植物化学成分。结果表明,在所有测试样品中,蜜露蜂蜜的总酚类物质含量和抗氧化活性最高,其次是椴树蜂蜜和森林蜂蜜,它们也表现出了显著的生物活性。我们的研究结果表明,虽然蜂蜜的植物来源对其生物特性有重要影响,但地理位置等其他因素也对其质量起着决定作用。在同一植物产地的蜂蜜样品中观察到的差异可归因于特定的地理条件,包括蜂蜜是来自城市还是农村地区、收获时间、养蜂方法和储存条件等因素。
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引用次数: 0
SEARCH FOR DECAY OF THE 7Be NUCLEUS IN 8B NUCLEUS DISSOCIATION 寻找 8B 核素分解中 7Be 核素的衰变情况
Q3 Engineering Pub Date : 2024-07-05 DOI: 10.59957/jctm.v59.i4.2024.28
R. Stanoeva, S. Kolev, Тatyana Koutzarova
The fragmentation of light relativistic nuclei can be studied in detail by the technique of nuclear track emulsions. The registration of all charged particles and their identification enable one to explore the isotopic composition of fragments and the projectile fragmentation channels. In the present paper results of an analysis of decay of the 7Be nucleus in dissociation of 8B nuclei are presented and a comparative analysis of the experimental data with the Monte Carlo model calculations is made. The paper is illustrated with characteristic images, obtained by means of a microscope, equipped with a CCD camera.
轻相对论原子核的碎裂可以通过核轨道乳化技术进行详细研究。对所有带电粒子的登记和识别使我们能够探索碎片的同位素组成和射弹的碎裂通道。本文介绍了在 8B 核解离过程中 7Be 核衰变的分析结果,并对实验数据和蒙特卡罗模型计算结果进行了比较分析。本文使用配备 CCD 摄像机的显微镜获得的特征图像进行说明。
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引用次数: 0
LASER SYNTHESIS AND PROCESSING OF COMPOSITE NANOSTRUCTURES 激光合成和加工复合纳米结构
Q3 Engineering Pub Date : 2024-07-05 DOI: 10.59957/jctm.v59.i4.2024.11
M. Koleva, Anna Dikovska, N. Nedyalkov, Tsanislava Genova, G. Atanasova
The present work reports the fabrication of porous composite ZnO/noble metal (Ag, Au) nanostructures using ps-pulsed laser deposition at atmospheric pressure. The PLD grown samples are ns-laser annealed, which led to a surface modification and formation of nanoparticles and NP’s aggregates. The effect of laser annealing procedure on the morphology, structure and optical properties of composite nanostructures is studied. The experimental results indicate that the laser annealing changes the plasmon resonance absorption mostly in the silver-doped samples. The laser modification plays a key role in tuning the PL performance for all samples by different mechanisms. Along with the increase in UV emission, there is a corresponding decrease in the broadband defect emission with the laser modification of composite nanostructures. The plasmon resonance absorption contributes to the enhancement of photoluminescence band-edge UV emission of the silver doped samples, while the PL performance of nanostructured ZnO/Au samples is attributed to the surface-plasmon-mediated sequential transfer of defect energy from ZnO to Au and electron transfer from excited Au to ZnO.
本研究报告介绍了在大气压力下利用ps脉冲激光沉积技术制造多孔复合氧化锌/贵金属(银、金)纳米结构的情况。PLD 生长的样品经 ns 激光退火后,表面发生了改性,并形成了纳米颗粒和 NP 聚集体。研究了激光退火过程对复合纳米结构的形态、结构和光学特性的影响。实验结果表明,激光退火主要改变了掺银样品的等离子体共振吸收。激光改性通过不同的机制在调整所有样品的等离子体共振性能方面发挥了关键作用。随着紫外发射的增加,复合纳米结构的宽带缺陷发射也相应减少。等离子体共振吸收有助于增强掺银样品的光致发光带边紫外发射,而纳米结构 ZnO/Au 样品的聚光性能则归因于表面等离子体介导的缺陷能量从 ZnO 到 Au 的顺序转移以及电子从激发的 Au 到 ZnO 的转移。
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引用次数: 0
ASSESSMENT OF HEAVY METAL CONTAMINANTS IN GROUNDWATER AROUND MINING AREA BY USING METAL POLLUTION INDICES MULTIVARIATE ANALYSIS AND GIS TECHNIQUE 利用金属污染指数多元分析和地理信息系统技术评估矿区周围地下水中的重金属污染物
Q3 Engineering Pub Date : 2024-07-05 DOI: 10.59957/jctm.v59.i4.2024.20
Vijayendra Pratap Dheeraj, C. S. Singh, A. K. Sonkar, Saurabh Kumar Barman
An opencast and underground coal mining each have the potential to have a negative impact on the groundwater table in terms of both its quantity and quality. Leachates from overburden dumps and industrial waste are another issue worldwide; they infiltrate into the groundwater and have a negative impact on the quality of it. A concern is that groundwater will become contaminated with heavy metals. Therefore, in the current study, the groundwater sample have been collected systematically from different sources of water in pre monsoon season (May) of 2022 around Korba coalfield (KCF). The collected water samples were examined for 9 different heavy metals by using ICP-MS (Inductively Coupled Plasma Mass Spectrometer-Perkin Elmer, Optima 4300 DV) instrument. In general,the concentrations of few metals such as Aluminium, Cadmium, Copper, Iron, Lead, and Zinc were found to be well below the acceptable limits of World Health Organization (WHO) and Bureau of Indian Standards (BIS) standard, however Manganese, Barium, and Nickel concentrations were observed to be above to desirable limits of WHO and BIS standard at a few sites which is similar to the results obtained by previous studies. These laboratory data were applied for the calculation of heavy metal pollution indices such as Heavy Metal Pollution Index (HPI), Heavy Metal Evaluation Index (HEI), and Contamination Index (Cd). The multiple approach used to evaluate the metal indices identifies that 80 % of HPI, 85 % of HEI, and 95 % of Cd for groundwater samples mostly classified as “lowto medium” class. The spatial diagram of these different indices showed a higher value in the south east part of the region suggesting that the heavy metal leaching from mining activities has little impact on the groundwater in the south east of the examined area. Multivariate statistical studies, like principal component analysis (PCA) analysis reveals that Fe, Pb, and Zn originate from anthropogenic sources like coal mining, while Al and Cd originate from both lithogenic and anthropogenic sources.
露天和地下采煤都有可能对地下水的水量和水质产生负面影响。覆土堆和工业废物的沥滤液是世界范围内的另一个问题;它们渗入地下水,对地下水的质量产生负面影响。人们担心地下水会受到重金属污染。因此,在本研究中,我们在 2022 年季风季节(5 月)前从科尔巴煤田(KCF)附近的不同水源处系统地采集了地下水样本。利用 ICP-MS(电感耦合等离子体质谱仪-珀金埃尔默 Optima 4300 DV)仪器对采集的水样进行了 9 种不同重金属的检测。总体而言,铝、镉、铜、铁、铅和锌等几种金属的浓度远低于世界卫生组织(WHO)和印度标准局(BIS)标准的可接受范围,但在几个地点观察到锰、钡和镍的浓度高于世界卫生组织和印度标准局标准的理想范围,这与之前研究得出的结果相似。这些实验室数据被用于计算重金属污染指数,如重金属污染指数 (HPI)、重金属评估指数 (HEI) 和污染指数 (Cd)。采用多重方法评估金属指数后发现,地下水样本中 80% 的 HPI、85% 的 HEI 和 95% 的 Cd 大都属于 "中低 "级别。这些不同指数的空间图显示,该地区东南部的指数值较高,表明采矿活动造成的重金属沥滤对考察区东南部的地下水影响较小。多变量统计研究,如主成分分析 (PCA) 显示,铁、铅和锌的来源是人为的,如煤矿开采,而铝和镉的来源既有岩石来源,也有人为来源。
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引用次数: 0
EVALUATION OF SOME CHEMICAL CHARACTERISTICS OF SPIRULINA FROM DIFFERENT MANUFACTURERS 评估不同厂家生产的螺旋藻的一些化学特性
Q3 Engineering Pub Date : 2024-07-05 DOI: 10.59957/jctm.v59.i4.2024.7
Krastena Nikolova, Nadezhda Petkova, G. Antova, Z. Petkova, G. Gentscheva, Anelia Gerasimova, Irina Karadjova
Some chemical characteristics of Spirulina from different countries (the USA, China, Belgium, and Bulgaria) were investigated. The study includes a comparative analysis of the content of some elements, tocopherols, and fatty acids in spirulina. The total lipids of the examined sample varied from 1.9 % (China) to 6.1 % (Belgium). Gas chromatography was used to determine the fatty acid composition of glyceride oil isolated from spirulina of different origins. Inductively coupled plasma-optical emission spectrometry and liquid chromatography were used to determine the elemental composition and tocopherol content. The fat content of Spirulina from Bulgaria approaches that of China and the USA, while that of Belgium is almost three times higher. It was found that palmitic acid is the main saturated fatty acid in all samples, and for spirulina from Bulgaria, it reaches 81.2 %. The content of unsaturatedfatty acids is highest in that originating in the USA.
研究调查了不同国家(美国、中国、比利时和保加利亚)螺旋藻的一些化学特征。研究包括对螺旋藻中某些元素、生育酚和脂肪酸含量的比较分析。样本中的总脂含量从 1.9%(中国)到 6.1%(比利时)不等。气相色谱法用于测定从不同产地的螺旋藻中分离出来的甘油脂肪酸组成。电感耦合等离子体-光发射光谱法和液相色谱法用于测定元素组成和生育酚含量。保加利亚螺旋藻的脂肪含量接近中国和美国,而比利时螺旋藻的脂肪含量几乎是中国和美国的三倍。研究发现,棕榈酸是所有样本中的主要饱和脂肪酸,保加利亚螺旋藻的这一比例达到 81.2%。不饱和脂肪酸含量最高的是产自美国的螺旋藻。
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引用次数: 0
SYNTHESIS OF NOVEL BOLDINE AMIDES AND THEIR IN VITRO INHIBITORY EFFECTS ON A MUSHROOM TYROSINASE 新型粗碱酰胺的合成及其对蘑菇酪氨酸酶的体外抑制作用
Q3 Engineering Pub Date : 2024-07-05 DOI: 10.59957/jctm.v59.i4.2024.14
M. Chochkova, B. Stoykova, Petranka Petrova, M. Štícha, Galya Ivanova
Boldine ((S)-2,9-dihydroxy-1,10-dimethoxy-aporphine) has been defined as the major alkaloid in Chilean boldo tree. Besides its diverse pharmacological activities, e.g. neuroprotective, cytoprotective, anti-inflammatory activities, boldine also exhibits tyrosinase-inhibiting effect. Tyrosinase [EC 1.14.18.1] is well known as a bifunctional enzyme that is responsible for the melanin biosynthesis. Considering the diphenolic structural feature of the alkaloid, which is associated with its tyrosinase inhibitory properties, herein we first modified the boldine core and then linked it with the natural phenolic antioxidants such as: caffeic-, ferulic- and sinapic acids. Furthermore, the newly amides were tested in vitro on the mushroom tyrosinase. Our results indicated, that amongst the tested boldine derivatives, caffeoyl- and feruloylamides have shown the anti-tyrosinase activity closely correlated with a hydroquinone, used as a standard.
波尔定((S)-2,9-二羟基-1,10-二甲氧基-阿朴啡)被定义为智利波尔多树的主要生物碱。除了具有神经保护、细胞保护、抗炎等多种药理活性外,波尔多碱还具有抑制酪氨酸酶的作用。众所周知,酪氨酸酶 [EC 1.14.18.1] 是一种双功能酶,负责黑色素的生物合成。考虑到生物碱的二酚结构特征与其抑制酪氨酸酶的特性有关,我们首先对粗碱核心进行了修饰,然后将其与天然酚类抗氧化剂(如咖啡酸、阿魏酸和山奈酸)连接起来。此外,我们还在体外测试了这些新酰胺对蘑菇酪氨酸酶的抑制作用。结果表明,在所测试的粗碱衍生物中,咖啡酰和阿魏酰酰胺的抗酪氨酸酶活性与作为标准的对苯二酚密切相关。
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引用次数: 0
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Journal of Chemical Technology and Metallurgy
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