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1.
Oxana Kazakova Irina Smirnova Elena Tretyakova Ren Csuk Sophie Hoenke Lucie Fischer 《International journal of molecular sciences》2021,22(4)
Semi-synthetic triterpenoids, holding an amino substituted seven-membered A-ring (azepano-ring), which could be synthesized from triterpenic oximes through a Beckmann type rearrangement followed by a reduction of lactame fragment, are considered to be novel promising agents exhibiting anti-microbial, alpha-glucosidase, and butyrylcholinesterase inhibitory activities. In this study, in an attempt to develop new antitumor candidates, a series of A-ring azepano- and 3-amino-3,4-seco-derivatives of betulin, oleanolic, ursolic, and glycyrrhetinic acids were evaluated for their cytotoxic activity against five human cancer cell lines and non-malignant mouse fibroblasts by means of a colorimetric sulforhodamine assay. Azepanoallobetulinic acid amide derivative 11 was the most cytotoxic compound of this series but showed little selectivity between the different human tumor cell lines. Flow cytometry experiments showed compound 11 to act mainly by apoptosis (44.3%) and late apoptosis (21.4%). The compounds were further screened at the National Cancer Institute towards a panel of 60 cancer cell lines. It was found that compounds 3, 4, 7, 8, 9, 11, 15, 16, 19, and 20 showed growth inhibitory (GI50) against the most sensitive cell lines at submicromolar concentrations (0.20–0.94 μM), and their cytotoxic activity (LC50) was also high (1–6 μM). Derivatives 3, 8, 11, 15, and 16 demonstrated a certain selectivity profile at GI50 level from 5.16 to 9.56 towards K-562, CCRF-CEM, HL-60(TB), and RPMI-8226 (Leukemia), HT29 (Colon cancer), and OVCAR-4 (Ovarian cancer) cell lines. Selectivity indexes of azepanoerythrodiol 3 at TGI level ranged from 5.93 (CNS cancer cell lines SF-539, SNB-19 and SNB-75) to 14.89 for HCT-116 (colon cancer) with SI 9.56 at GI50 level for the leukemia cell line K-562. The present study highlighted the importance of A-azepano-ring in the triterpenic core for the development of novel antitumor agents, and a future aim to increase the selectivity profile will thus lie in the area of modifications of azepano-triterpenic acids at their carboxyl group. 相似文献
2.
This paper demonstrates a novel approach for a computer-based course assessment. A test is introduced in which computers are deployed. This significantly contributes to the enhancement of the marking consistency, individual performance distinction and feedbacks, and widen the questions range for computer-based modules. The proposed test method, for the first time, uses the simulation files marking for individualised evaluation purposes. The methodology has successfully been implemented in practice for three modules including Process Simulation (CE2105), Advanced Process Simulation (CE4023), and Process Computation (CE3021) at Aston University (UK) over three academic years, from 2016 to 2019. The effectiveness of the proposed approach has been evaluated using several factors, including final marks, consistency multiple academic years, and mark distribution. In contrast to the common teamwork assessments, individualised feedback became possible. While ASPEN has been used for CE4023 and CE2105 tests, MATLAB has been applied as the computation platform for CE3021 module. This reveals the applicability of different software in proposed methodology. The number of students in the cohorts studied was from 52 to 204, demonstrating the applicability of the method for various cohort sizes. Even though the methodology has been demonstrated based on the chemical engineering discipline modules, it allows digitalising the delivery and assessment of a wide range of simulation techniques in many disciplines. 相似文献
3.
Karolina Storesund Francine Amon Anne Steen‐Hansen Shayesteh Haghighatpanah Ida Larsson 《火与材料》2021,45(1):181-190
The aim of this exploratory study has been to investigate the fire properties and environmental aspects of different upholstery material combinations, mainly for domestic applications. An analysis of the sustainability and circularity of selected textiles, along with lifecycle assessment, is used to qualitatively evaluate materials from an environmental perspective. The cone calorimeter was the primary tool used to screen 20 different material combinations from a fire performance perspective. It was found that textile covers of conventional fibres such as wool, cotton and polyester, can be improved by blending them with fire resistant speciality fibres. A new three‐dimensional web structure has been examined as an alternative padding material, showing preliminary promising fire properties with regard to ignition time, heat release rates and smoke production. 相似文献
4.
5.
目的:研究抗坏血酸(ascorbic acid,AsA)-还原型谷胱甘肽(reduced glutathione,GSH)循环代谢在水杨酸处理采后甜瓜诱导的过量H2O2清除过程中的作用。方法:用4 mmol/L水杨酸浸泡‘玉金香’厚皮甜瓜10 min,测定处理后果实常温贮藏过程中丙二醛(malondialdehyde,MDA)含量,分析活性氧的积累水平、超氧化物歧化酶(superoxide dismutase,SOD)和过氧化氢酶(catalase,CAT)活力,以及AsA-GSH循环过程相关酶活力及产物和底物含量。结果:水杨酸处理降低了果实MDA含量,第10天处理组MDA含量较对照组降低14.6%;显著提高了果实O2-·的产生速率和H2O2含量(P<0.05),其中处理后第2天O2-·的产生速率高出同期对照组的1.9 倍,第6天H2O2含量高出对照组果实29.7%;提高了果实SOD活力,但抑制了CAT活力,说明H2O2的清除可能是依赖于除酶促系统外的其他系统。此外,水杨酸处理提高了果实抗坏血酸过氧化物酶、单脱氢抗坏血酸过氧化物酶、脱氢抗坏血酸还原酶和谷胱甘肽还原酶的活力,增加了AsA和氧化型谷胱甘肽的含量,降低了脱氢抗坏血酸和GSH的含量。结论:水杨酸处理诱导了厚皮甜瓜果实的氧爆,抑制了MDA产生,由水杨酸诱导产生的过量H2O2主要依靠AsA-GSH循环系统清除。 相似文献
6.
Smartphones are a promising tool as student response systems (SRS) for interactive teaching due to their widespread diffusion. Here, the main purpose is to assess the efficacy of smartphone-based SRS in large classroom settings of undergraduate Thermodynamics, as representative of engineering courses requiring high-level cognitive skills for problem solving. Four sets of multiple-choice questions were presented during the course. Overall, the results refer to 1055 students between control and SRS classes, each corresponding to a3 years period.One of the main results of this work is the strong linear correlation between the average questionnaire score and the final exam grade (R2 = 0.91). A similar correlation, although with a lower value of R2, is already found in the first questionnaire, thus showing the SRS high predictive power of class performance. The results of this study provide guidance for a quantitative use of smartphone-based SRS in teaching basic disciplines. The SRS monitoring capability allows early detection of struggling students, thus paving the way to personalized tutoring and improved student engagement in active learning practices. This approach is especially important in emergency situations, such as the SARS-Cov-2 pandemic, when distance learning is widely adopted, and remote interactive tools are highly needed. 相似文献
7.
《International Journal of Hydrogen Energy》2022,47(2):1083-1091
α-Ni(OH)2 is a promising candidate of the currently commercialized β-Ni(OH)2 due to its higher theoretical discharge capacity in alkaline solution; however, its instability and poor conductivity plague the practical application. Herein, we propose α-Ni(OH)2 with Co doping and spherical structure to strengthen the stability and enhance the conductivity and use it as the cathode for nickel-metal hydride batteries. Studies show that proper Co doping promotes the electrochemical reaction between the active materials and the electrolyte due to the spherical α-Ni(OH)2 with enlarged interlayer distance and abundant hole channels, as well as high conductivity of Co, therefore, the obtained spherical α-Ni(OH)2 with 7 mol% Co doping delivers significantly improved discharge capability, which is 384.6 mAh g?1 at 70 mA g?1 (0.2 C), increased by 54.3 mAh g?1 compared with pure α-Ni(OH)2, and at a high current of 5 C, it still gives 269.4 mAh g?1, in contrast 218.5 mA g?1 for the pure α-Ni(OH)2. Besides, the cycling stability of the α-Ni(OH)2 with 7 mol% Co doping maintains 340 cycles at a capacity retention of 80% (1C), which is extended 110 cycles in contrast to the pure α-Ni(OH)2. These results provide the underpinning platform of α-Ni(OH)2 for battery applications with high discharge ability and cycle life. 相似文献
8.
为了提高配电网差异化节能降耗效果,解决现有潜力评估方法存在的应用性能差的问题,提出碳中和背景下配电网差异化节能降耗潜力优化评估方法。根据配电网的空间结构,构建相应的等值电路模型。在该模型下,从设备损耗和运行附加损耗2个方面计算配电网的损耗量。根据损耗量计算结果,确定配电网差异化碳中和节能降耗方式。从静态和动态2个角度设置潜力评估指标,通过指标数据处理、指标权重求解等步骤,得出配电网差异化节能降耗潜力的综合量化评估结果。将设计潜力评估方法应用到配电网的差异化节能降耗改造工作中,能够有效降低配电网的实际线损量、降低区域损耗费用,并具有较高的应用价值。 相似文献
9.
中国考古出土的蚕业实物及蚕的艺术形象比较丰富,蚕的艺术形象如蚕纹、陶蚕蛹、牙雕蚕、玉石蚕、铜蚕、金蚕等,可统称为"蚕的模拟形态"。对蚕的模拟形态的功用,已有的诸多解释都有待完善。研究表明,蚕的模拟形态或艺术形象表达的功用或为饰品,或为装饰图案,或有待进一步考究。但无论哪种功用,用"蚕"这一形象都蕴含了特有的用意。通过对中国古代生命观的考察,文章认为蚕的艺术形象折射出相应的中国古代哲学生命观,即中国古人追求的死而复生、生生不息、羽化成仙、长乐无极等观念。 相似文献
10.
《International Journal of Hydrogen Energy》2022,47(11):7432-7442
The durability of metal plate proton exchange membrane fuel cell (PEMFC) stack is still an important factor that hinders its large-scale commercial application. In this paper, we have conducted a 1000 h durability test on a 1 kW metal plate PEMFC stack, and explored the degradation of the core components. After 1000 h of dynamic load cycles, the voltage decay percentage of the stack under the current densities of 1000 mA cm?2 is 5.67%. By analyzing the scanning electron microscopy (SEM) images, the surfaces of the metal plates are contaminated locally by organic matter precipitated from the membrane electrode assembly (MEA). The SEM images of the catalyst coated membrane (CCM) cross section indicate that the MEA has undergone severe degradation, including the agglomeration of the catalyst layer, and the thinning and perforation of the PEM. These are the main factors that cause the rapid increase in hydrogen crossover flow rate and performance decay of the PEMFC stack. 相似文献