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1.
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.
Different aspects of the reciprocal regulatory influence on the development of gonadotropin-releasing hormone (GnRH)-producing- and immune systems in the perinatal ontogenesis and their functioning in adults in normal and pathological conditions are discussed. The influence of GnRH on the development of the immune system, on the one hand, and the influence of proinflammatory cytokines on the development of the hypothalamic-pituitary-gonadal system, on the other hand, and their functioning in adult offspring are analyzed. We have focused on the effects of GnRH on the formation and functional activity of the thymus, as the central organ of the immune system, in the perinatal period. The main mechanisms of reciprocal regulation of these systems are discussed. The reproductive health of an individual is programmed by the establishment and development of physiological systems during critical periods. Regulatory epigenetic mechanisms of development are not strictly genetically controlled. These processes are characterized by a high sensitivity to various regulatory factors, which provides possible corrections for disorders.  相似文献   
3.
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.
杨乾  范存斐  王毅  任亚琳  毕阳 《食品科学》2021,42(1):243-249
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   
5.
针对突发扩频信号用户资源扩大、终端功率降低、系统容量提升等需求,提出了一种低载噪比突发扩频信号的快速捕获硬件实现方法。采用分段匹配滤波器加多普勒并行相干积累的方法,基于硬件实现从算法到工程进行全流程优化设计,最终实现最优的捕获性能。应用结果表明,该硬件设计实现方案的快速捕获性能优越,设计方案正确、可行,已成功应用于工程建设中。  相似文献   
6.
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   
7.
Single-cell RNA-sequencing (scRNA-seq) is a rapidly increasing research area in biomedical signal processing. However, the high complexity of single-cell data makes efficient and accurate analysis difficult. To improve the performance of single-cell RNA data processing, two single-cell features calculation method and corresponding dual-input neural network structures are proposed. In this feature extraction and fusion scheme, the features at the cluster level are extracted by hierarchical clustering and differential gene analysis, and the features at the cell level are extracted by the calculation of gene frequency and cross cell frequency. Our experiments on COVID-19 data demonstrate that the combined use of these two feature achieves great results and high robustness for classification tasks.  相似文献   
8.
《Ceramics International》2022,48(11):15252-15260
The Co3O4, as a potential anode of lithium-ion batteries, has gained considerable attention because of high theoretical capacity. However, the Co3O4 is suffering from serious structure deterioration and rapid capacity fading due to its bulky volume change during cyclic charge/discharge process. Herein, to stabilize the lithium storage performance of the Co3O4 nanoparticles, a characteristic carbon scaffold (HPC) integrating hollow and porous structures has been fabricated by a well-designed method for the first time. The ultrafine Co3O4 nanoparticles are cleverly anchored on the HPC (HPC@Co3O4) and hence achieve significantly improved electrochemical properties including high capacity, improved reaction kinetics and outstanding cycle stability, showing high capacity of 1084.7 mAh g-1 after 200 cycles at 200 mA g-1 as well as 681.4 mAh g-1 after 300 cycles at 1000 mA g-1. The HPC@Co3O4 therefore shows good promising for application in advanced lithium-ion battery anodes. The results of the systematically material and electrochemical characterizations indicate that the synergistic effects of ultrafine Co3O4 nanoparticles and well-designed HPC scaffolds are responsible for the outstand performance of the HPC@Co3O4 anode. Moreover, this work can enrich the understanding and development of stable and high-performance metal oxide-based lithium-ion battery anodes for advanced lithium storage.  相似文献   
9.
In this paper, a salinity gradient solar pond (SGSP) is used to harness the solar energy for hydrogen production through two cycles. The first cycle includes an absorption power cycle (APC), a proton exchange membrane (PEM) electrolyzer, and a thermoelectric generator (TEG) unit; in the second one, an organic Rankine cycle (ORC) with the zeotropic mixture is used instead of APC. The cycles are analyzed through the thermoeconomic vantage point to discover the effect of key decision variables on the cycles’ performance. Finally, NSGA-II is used to optimize both cycles. The results indicate that employing ORC with zeotropic mixture leads to a better performance in comparison to utilizing APC. For the base mode, unit cost product (UCP), exergy, and energy efficiency when APC is employed are 59.9 $/GJ, 23.73%, and 3.84%, respectively. These amounts are 47.27 $/GJ, 29.48%, and 5.86% if ORC with the zeotropic mixture is utilized. The APC and ORC generators have the highest exergy destruction rate which is equal to 6.18 and 10.91 kW. In both cycles, the highest investment cost is related to the turbine and is 0.8275 $/h and 0.976 $/h for the first and second cycles, respectively. In the optimum state the energy efficiency, exergy efficiency, UCP, and H2 production rate of the system enhances 42.44%, 27.54%,15.95%, and 38.24% when ORC with the zeotropic mixture is used. The maximum H2 production is 0.47 kg/h, and is obtained when the mass fraction of R142b, LCZ temperature, pumps pressure ratio, generator bubble point temperature are 0.603, 364.35 K, 2.12, 337.67 K, respectively.  相似文献   
10.
In this present work, the effect of lanthanum oxides (La2O3) on the thermal cycle behavior of TBC coatings and mechanical properties such as adhesion strength and microhardness of 8% Yttria Stabilized Zirconia (8YSZ) TBCs were investigated. CoNiCrAlY and aluminium alloy (Al–13%Si) were used as bond coat and substrate materials. 8YSZ and different wt % of La2O3 (10, 20, and 30%) top coatings were applied using the atmospheric plasma spray (APS) method. The thermal cycling test for TBC coated samples were conducted at 800 °C in the electric furnace. The XRD pattern shows that the La2O3 doped 8YSZ material transformed to cubic pyrochloric structured La2Zr2O7 during thermal cycling. Further, the Taguchi-based grey relation analysis (GRA) method was applied to optimize the TBC coating parameters to achieve better mechanical properties such as adhesion strength and microhardness. And the optimized La2O3/8YSZ TBC coating was coated on CRDI engine combustion chamber components. The engine was tested with microalgae biodiesel and hydrogen, and the results were promising for the TBC-coated engine. The engine performance increased while using La2O3/8YSZ coated components, and the emissions from engine exhaust gas such as CO, HC, and smoke reduced considerably. It was found that there was no separation crack and spallation of the coating layer in the microstructure. Ultimately, the microstructural analysis of the optimized TBC coated piston sample after 50 h of running in the diesel engine confirmed that the developed coating had a superior thermal insulation effect and longer life.  相似文献   
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