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Glycoprotein Levels and Oxidative Stomach Damage in Diabetes and Prostate Cancer Model: Protective Effect of Metformin. 糖尿病和前列腺癌模型中的糖蛋白水平和氧化性胃损伤:二甲双胍的保护作用
IF 1.2 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-11-13 DOI: 10.17344/acsi.2023.8198
Onur Ertik, Pinar Koroglu Aydin, Omur Karabulut Bulan, Refiye Yanardag

Men with diabetes have a higher risk of prostate cancer and people with prostate cancer are prone to stomach metastases. Therefore, researchers are continuing in order to find new approaches in the treatment of individuals with both diseases at the same time. The protective effect of metformin (which is used in the treatment of diabetes) on cancer continues to be supported by studies. The present study aimed that the protective effect of metformin in the stomach tissue of diabetic and/or prostate cancer rats was investigated through biochemical parameters. In the study, it was determined that the biochemical parameters studied showed a protective effect on stomach tissues with the administration of metformin to cancer and diabetic+cancer groups, and as a result of the principal component analysis, it was determined that the biochemical parameters studied in the stomach tissue showed a correlation.

男性糖尿病患者罹患前列腺癌的风险较高,而前列腺癌患者则容易发生胃转移。因此,研究人员正在继续寻找同时治疗这两种疾病的新方法。二甲双胍(用于治疗糖尿病)对癌症的保护作用继续得到研究的支持。本研究旨在通过生化指标来调查二甲双胍对糖尿病和/或前列腺癌大鼠胃组织的保护作用。研究结果表明,在癌症组和糖尿病+癌症组服用二甲双胍后,所研究的生化指标对胃组织有保护作用,主成分分析结果表明,所研究的胃组织生化指标显示出相关性。
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引用次数: 0
Synthesis, Characterization and X-Ray Crystal Structures of Oxidovanadium(V) Complexes Derived from N'-(2-Hydroxy-5-methylbenzylidene)-4-methylbenzohydrazide with Antibacterial Activity. 具有抗菌活性的 N'-(2-羟基-5-甲基亚苄基)-4-甲基苯甲酰肼衍生氧化钒(V)配合物的合成、表征和 X 射线晶体结构。
IF 1.2 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-11-10 DOI: 10.17344/acsi.2023.8347
Xue-Rong Tan, Wei Li, Meng-Meng Duan, Zhonglu You

A dinuclear oxidovanadium(V) complex [V2O2L2(OMe)2] (1) was synthesized from N'-(2-hydroxy-5-methylbenzylidene)-4-methylbenzohydrazide (H2L) and VO(acac)2 in MeOH. Reaction of complex 1 with 3-hydroxy-2-methyl-4-pyrone (HL') afforded a mononuclear oxidovanadium(V) complex [VOLL'] (2). The hydrazone and both complexes were characterized by IR, UV and 1H NMR spectroscopy, as well as X-ray single crystal determination. X-ray powder diffraction of the complexes was performed. The V atoms in the two complexes are in octahedral coordination. The molecules of complex 2 are linked through non-classical hydrogen bonds of type C-H∙∙∙O to form one-dimensional chains running along the a axis. The biological assay indicates that the complexes have good antimicrobial activities on the bacteria strains P. aeroginosa, S. aureus, B. subtilis and E. coli.

一种双核氧化钒(V)络合物[V2O2L2(OMe)2](1)是由 N'-(2-羟基-5-甲基亚苄基)-4-甲基苯甲酰肼(H2L)和 VO(acac)2 在 MeOH 中合成的。络合物 1 与 3-羟基-2-甲基-4-吡喃酮(HL')反应,得到单核氧化钒(V)络合物 [VOLL'](2)。通过红外光谱、紫外光谱和 1H NMR 光谱以及 X 射线单晶测定,对腙和两种络合物进行了表征。对复合物进行了 X 射线粉末衍射。这两种络合物中的 V 原子呈八面体配位。络合物 2 的分子通过 C-H∙∙∙O 类型的非经典氢键连接,形成沿 a 轴运行的一维链。生物检测表明,复合物对铜绿假单胞菌、金黄色葡萄球菌、枯草杆菌和大肠杆菌具有良好的抗菌活性。
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引用次数: 0
Synthesis of New of 4-Thiazolidinone and Thiazole Derivatives Containing Coumarin Moiety with Antimicrobial Activity. 具有抗菌活性的含香豆素分子的新 4-噻唑烷酮和噻唑衍生物的合成。
IF 1.2 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-11-09 DOI: 10.17344/acsi.2023.8281
Reem Al-Harbi, Marwa El-Sharief, Samir Abbas

Synthesizing hybrid molecules is one the best manner to achieve novel promising agents. Consequently, series of new thiazoles having coumarin nucleus were synthesized from 3-acetylcoumarin thiosemicarbazones. Cyclization of thiosemicarbazone derivatives with ethyl 2-chloroacetate, 1-chloropropan-2-one and 2-bromo-1-phenylethanone afforded the corresponding 4-thiazolidinones, 4-methylthiazoles and 4-phenylthiazoles, respectively. The expected antimicrobial propriety for the synthesized thiosemicarbazone and thiazole derivatives were investigated. The thiosemicarbazones and thiazolidin-4-ones showed moderate activities against G +ve and G -ve bacteria.

合成杂化分子是获得新型药物的最佳途径之一。因此,我们从 3-乙酰香豆素硫代氨基脲中合成了一系列具有香豆素核的新噻唑。硫代氨基羰基衍生物与 2-氯乙酸乙酯、1-氯丙-2-酮和 2-溴-1-苯乙酮环化后,分别得到了相应的 4-噻唑烷酮、4-甲基噻唑和 4-苯基噻唑。研究人员对合成的硫代氨基羰基和噻唑衍生物的预期抗菌性进行了调查。硫代氨基羰基和噻唑烷-4-酮对 G +ve 和 G -ve 细菌表现出中等程度的活性。
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引用次数: 0
Copper(II) and Nickel(II) Complexes Derived from Isostructural Bromo- and Fluoro-Containing Bis-Schiff Bases: Syntheses, Crystal Structures and Antimicrobial Activity. 铜(II)和镍(II)配合物衍生自含溴和含氟双施氏碱的异构体:合成、晶体结构和抗菌活性。
IF 1.2 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-11-07 DOI: 10.17344/acsi.2023.8359
Ke-Sheng Cao, Ling-Wei Xue, Qiao-Ru Liu

A mononuclear copper(II) complex [CuLa] (1), and three mononuclear nickel(II) complexes [NiLa] (2), [NiLa]·CH3OH (2·CH3OH) and [NiLb] (3), where La and Lb are the dianionic form of N,N'-bis(4-bromosalicylidene)-1,2-cyclohexanediamine (H2La) and N,N'-bis(4-fluorosalicylidene)-1,2-cyclohexanediamine (H2Lb), respectively, were prepared and structurally characterized by spectroscopy method and elemental analyses. The detailed structures were determined by X-ray single crystal diffraction. All the copper and nickel complexes are mononuclear compounds. The metal ions in the complexes are in square planar coordination, with the two phenolate oxygens and two imine nitrogens of the Schiff base ligands. The biological effect of the four complexes were assayed on the bacteria strains Staphylococcus aureus, Escherichia coli and Candida albicans.

一种单核铜(II)络合物[CuLa](1)和三种单核镍(II)络合物[NiLa](2)、[NiLa]-CH3OH (2-CH3OH)和[NiLb](3),其中 La 和 Lb 是 N,N'-双(4-溴代水杨醛基)-1、制备了 N,N'-双(4-溴代水杨醛基)-1,2-环己二胺(H2La)和 N,N'-双(4-氟代水杨醛基)-1,2-环己二胺(H2Lb)。详细结构由 X 射线单晶衍射确定。所有铜和镍络合物都是单核化合物。配合物中的金属离子与希夫碱配体的两个苯酚氧原子和两个亚胺硝基呈正方形配位。四种络合物对金黄色葡萄球菌、大肠杆菌和白色念珠菌菌株的生物效应进行了检测。
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引用次数: 0
A novel nickel(II) complex with N,S donor Schiff base: Structural characterisation, DFT, TD-DFT study and catalytic investigation. 带有 N、S 给体希夫碱的新型镍(II)配合物:结构特征、DFT、TD-DFT 研究和催化调查。
IF 1.2 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-11-04 DOI: 10.17344/acsi.2023.8136
Manas Chowdhury, Niladri Biswas, Sandeepta Saha, Ennio Zangrando, Nayim Sepay, Chirantan Roy Choudhury

One new mononuclear nickel(II) thiosemicarbazone complex (1), has been synthesised from the Schiff base ligand derived from p-anisaldehyde and thiosemicarbazide. Complex 1 is characterized by using different spectroscopic techniques and single crystal X-ray structure analysis. Time dependent density functional theory (TD-DFT) was performed to simulate the electronic spectra of the complex 1 with the help of Polarizable Continuum Model (PCM) model. Complex 1 acts as functional models. The catalytic property has been evaluated from Lineweaver-Burk plot using the Michaelis-Menten approach of enzyme catalysis with a kcat value of the order of 708 h-1.

由对甲氧基苯甲醛和硫代氨基甲酰肼衍生的希夫碱配体合成了一种新的单核镍(II)硫代氨基甲酰肼络合物(1)。利用不同的光谱技术和单晶 X 射线结构分析对配合物 1 进行了表征。在可极化连续模型(PCM)模型的帮助下,进行了时相依密度泛函理论(TD-DFT)来模拟复合物 1 的电子光谱。复合物 1 充当了功能模型。利用酶催化的 Michaelis-Menten 方法,从 Lineweaver-Burk 图中评估了其催化特性,其 kcat 值为 708 h-1。
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引用次数: 0
Synthesis and Cholinesterase Inhibitory Activity of Selected Indole-Based Compounds. 精选吲哚类化合物的合成和胆碱酯酶抑制活性。
IF 1.2 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-11-02 DOI: 10.17344/acsi.2023.8460
Uroš Grošelj, Marija Gršič, Anže Meden, Damijan Knez, Marko Jukič, Jurij Svete, Stanislav Gobec

Synthesis and anticholinesterase activity of 18 previously unpublished indole- and tryptophan-derived compounds are disclosed. These sp3-rich compounds containing an indole structural unit exhibit selective submicromolar inhibition of human butyrylcholinesterase (hBChE). The structures of the newly synthesized compounds were confirmed by 1H and 13C NMR, IR spectroscopy, and high-resolution mass spectrometry.

本研究公开了 18 种以前未发表过的吲哚和色氨酸衍生化合物的合成和抗胆碱酯酶活性。这些富含 sp3 的化合物含有一个吲哚结构单元,对人丁酰胆碱酯酶(hBChE)具有选择性亚摩尔抑制作用。新合成化合物的结构通过 1H 和 13C NMR、红外光谱以及高分辨率质谱法得到了证实。
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引用次数: 0
Comparison of deep eutectic solvent-based ultrasound- and heat-assisted extraction of bioactive compounds from Withania somnifera and process optimization using response surface methodology. 基于深共晶溶剂的薇甘菊生物活性化合物超声提取与热辅助提取的比较,以及利用响应面方法优化工艺。
IF 1.2 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-11-02 DOI: 10.17344/acsi.2023.8419
Faizan Sohail, Dildar Ahmed

Extraction of bioactive compounds from Withania somnifera roots was studied using sodium acetate-glycerol deep eutectic solvent (DES) and two techniques ultrasound-assisted extraction (UAE) and heat-assisted extraction (HAE) under response surface methodology (RSM). For UAE and HAE, total phenolic content (TPC, mg gallic acid equivalents per g dry weight (mg GAE g-1 DW)), total flavonoid content (TFC, mg rutin equivalents g-1 DW (mg RE g-1 DW)), radical scavenging activity (RSA, mg AAE (ascorbic acid equivalents) g-1 DW), and iron chelating activity (ICA, mg EDTAE (ethylenediaminetetraacetate equivalents) g-1 DW%) were 6.51, 6.08, 12.56, and 3.57, respectively, and 3.33, 3.98. 6.57 and 2.48, respectively. For UAE, the optimal conditions were a DES concentration of 50 %, temperature of 60 °C, and time of 20 min, and for HAE, a DES concentration of 60 %, temperature of 60 °C, and time of 75 min. The discovered models were strongly supported by the validation experiments. UAE was more efficient and less time-consuming for extracting phytoconstituents of the W. somnifera than HAE.

采用醋酸钠-甘油深共晶溶剂(DES)以及响应面方法(RSM)下的超声辅助萃取(UAE)和热辅助萃取(HAE)两种技术,研究了从薇甘菊根中萃取生物活性化合物的方法。在超声辅助萃取和热辅助萃取中,总酚含量(TPC,毫克没食子酸当量/克干重(mg GAE g-1 DW))、总黄酮含量(TFC,毫克芦丁当量/克干重(mg RE g-1 DW))、自由基清除活性(RSA,毫克抗坏血酸当量/克干重(mg AAE g-1 DW))和铁螯合活性(ICA,毫克乙二胺四乙酸当量/克干重(mg EDTAE g-1 DW%))分别为 6.51、6.08、12.56 和 3.57,以及 3.33、3.98、6.57 和 2.48。6.57 和 2.48。对于 UAE,最佳条件是 DES 浓度为 50%、温度为 60 ℃、时间为 20 分钟;对于 HAE,最佳条件是 DES 浓度为 60%、温度为 60 ℃、时间为 75 分钟。所发现的模型得到了验证实验的有力支持。与 HAE 相比,UAE 提取植物成分的效率更高,耗时更短。
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引用次数: 0
Rise of gold nanoparticles as carriers of therapeutic agents. 金纳米粒子作为治疗剂载体的兴起。
IF 1.2 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-11-02 DOI: 10.17344/acsi.2023.8216
Satyanarayan Pattnaik, Chandrashekar Thalluri, Kalpana Swain

A nanoparticle is the simplest structural component due to its nanometer-sized diameter. Nanoparticles are typically atoms or molecules that generate a radius (or diameter) of less than 100 nm when bonded collectively. The latest developments in nanotechnology provide a wide range of methods for studying and monitoring various medical and biological processes at the nanoscale. Nanoparticles can help diagnose and treat diseases, such as cancer, by carrying drugs directly to cancer cells. They can also be used to detect disease biomarkers in the body, helping to provide early diagnosis. It is likely that the data will have a positive effect on biology and medicine. It is plausible that nanoparticles could be used in theranostic applications and targeted drug delivery. This could significantly improve patient outcomes and reduce the amount of time, effort, and money needed to diagnose and treat diseases. It could also reduce the side effects of treatments, providing more precise and effective treatments. Nanoparticles for biomedical applications include polymeric and metal nanoparticles; liposomes and micelles; dendrimers and quantum dots; etc. Among the nanoparticles, gold nanoparticles have emerged as a promising platform for drug delivery applications. Gold nanoparticles are highly advantageous for drug delivery applications due to their excellent biocompatibility, stability, and tunable physical and chemical properties. The present review provides an in-depth discussion of the various approaches to gold nanoparticle synthesis and drug delivery applications.

纳米粒子的直径只有纳米大小,因此是最简单的结构组件。纳米粒子通常是原子或分子,它们结合在一起时产生的半径(或直径)小于 100 纳米。纳米技术的最新发展为在纳米尺度上研究和监测各种医学和生物过程提供了广泛的方法。纳米粒子可直接将药物带入癌细胞,从而帮助诊断和治疗癌症等疾病。它们还可用于检测体内的疾病生物标志物,帮助进行早期诊断。这些数据很可能会对生物学和医学产生积极影响。纳米粒子有可能被用于治疗学应用和靶向给药。这将大大改善患者的治疗效果,减少诊断和治疗疾病所需的时间、精力和金钱。它还可以减少治疗的副作用,提供更精确、更有效的治疗。生物医学应用的纳米粒子包括聚合物和金属纳米粒子、脂质体和胶束、树枝状分子和量子点等。在这些纳米粒子中,金纳米粒子已成为一种前景广阔的药物输送应用平台。金纳米粒子具有良好的生物相容性、稳定性以及可调的物理和化学特性,因此在药物递送应用中具有很大的优势。本综述深入探讨了金纳米粒子合成和给药应用的各种方法。
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引用次数: 0
X-ray Powder Diffraction and Supervised Self-Ogranizing Maps as Tools for Forensic Classification of Soils. 作为土壤法医分类工具的 X 射线粉末衍射和监督自粒化图。
IF 1.2 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-11-02 DOI: 10.17344/acsi.2023.8221
Hirijete Idrizi, Mile Markoski, Metodija Najdoski, Igor Kuzmanovski

Due to its transferability, the soil has been commonly used as evidence in criminal investigations. In this work, 172 soil samples taken from five urban parks from the town of Tetovo (North Macedonia) and from additional four rural locations in its vicinity. The soil samples were examined using X-ray powder diffraction. The collected diffractograms were used for development of classification models based on supervised self-organizing maps. The examination generalization performances of the developed models showed that they were able to correctly classify between 95.6 and 97.8% of the samples from the independent test set. The influence of the weather and the seasonal changes on the composition of the soil was also examined. For this purpose, three years after the initial soil samples were collected, additional 28 samples were analyzed from different location. The best models presented in this work were able to successfully classify 27 of these additional samples.

由于其可转移性,土壤通常被用作刑事调查的证据。在这项工作中,172 份土壤样本取自泰托沃镇(北马其顿)的五个城市公园及其附近的四个农村地区。使用 X 射线粉末衍射法对土壤样本进行了检测。收集到的衍射图用于开发基于监督自组织图的分类模型。对所开发模型的泛化性能进行的测试表明,这些模型能够对独立测试集中 95.6% 至 97.8% 的样本进行正确分类。此外,还考察了天气和季节变化对土壤成分的影响。为此,在采集了最初的土壤样本三年后,又对来自不同地点的 28 个样本进行了分析。这项工作中提出的最佳模型能够成功地对其中的 27 个额外样本进行分类。
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引用次数: 0
Syntheses, Characterization, Crystal Structures and Xanthine Oxidase Inhibitory Activity of Hydrazones. 肼类化合物的合成、表征、晶体结构和黄嘌呤氧化酶抑制活性。
IF 1.2 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-11-02 DOI: 10.17344/acsi.2023.8370
Xiao-Jun Zhao, Ling-Wei Xue, Qiao-Ru Liu

Four new fluoro-containing hydrazones were synthesized from 4-fluorobenzaldehyde with chloro- and nitro-substituted benzohydrazides. They are 3-chloro-N'-(4-fluorobenzylidene)benzohydrazide (1), 2-chloro-N'-(4-fluorobenzylidene)benzohydrazide (2), N'-(4-fluorobenzylidene)-4-nitrobenzohydrazide (3), and N'-(4-fluorobenzylidene)-3-nitrobenzohydrazide (4). The compounds have been characterized by IR and 1H NMR spectra, as well as X-ray single crystal determination. Xanthine oxidase (XO) inhibitory activity indicated that the nitro substituted compounds 3 and 4 have effective activity. Docking simulation was performed to insert the compounds into the crystal structure of xanthine oxidase at the active site to investigate the probable binding modes.

由 4-氟苯甲醛与氯代和硝代苯甲酰肼合成了四种新的含氟酰肼。它们分别是 3-氯-N'-(4-氟亚苄基)苯酰肼 (1)、2-氯-N'-(4-氟亚苄基)苯酰肼 (2)、N'-(4-氟亚苄基)-4-硝基苯酰肼 (3) 和 N'-(4-氟亚苄基)-3-硝基苯酰肼 (4)。这些化合物通过红外光谱和 1H NMR 光谱以及 X 射线单晶测定进行了表征。黄嘌呤氧化酶(XO)抑制活性表明,硝基取代的化合物 3 和 4 具有有效的活性。通过对接模拟将化合物插入黄嘌呤氧化酶活性位点的晶体结构中,以研究其可能的结合模式。
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引用次数: 0
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Acta Chimica Slovenica
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