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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   
44.
Cell encapsulation within hydrogel droplets is transforming what is feasible in multiple fields of biomedical science such as tissue engineering and regenerative medicine, in vitro modeling, and cell-based therapies. Recent advances have allowed researchers to miniaturize material encapsulation complexes down to single-cell scales, where each complex, termed a single-cell microgel, contains only one cell surrounded by a hydrogel matrix while remaining <100 μm in size. With this achievement, studies requiring single-cell resolution are now possible, similar to those done using liquid droplet encapsulation. Of particular note, applications involving long-term in vitro cultures, modular bioinks, high-throughput screenings, and formation of 3D cellular microenvironments can be tuned independently to suit the needs of individual cells and experimental goals. In this progress report, an overview of established materials and techniques used to fabricate single-cell microgels, as well as insight into potential alternatives is provided. This focused review is concluded by discussing applications that have already benefited from single-cell microgel technologies, as well as prospective applications on the cusp of achieving important new capabilities.  相似文献   
45.
Since the inception of blockchain-related technologies over a decade ago, investors’ uptake of the technologies has grown rapidly. But even with the advancement in standing from conceptual beginnings to real-world experimentation, mainstream adoption of the technologies in either organizational or individual contexts has yet to eventuate. To resolve this paradox, we examine progression of the technologies’ diffusion instead, and in the process, seek to uncover the underlying dynamics of sentiments at play. Diffusion involves multiple actions by different parties, with social discourses via diverse media playing an essential role. In demonstrating the interplay of support to resistance via media framing and the diffusion of innovation theory, findings from our paper contribute to the technology adoption literature. Understanding resistant behavior toward a new technology area could help resolve potential issues that may arise. This would hopefully lead to better technological implementation outcomes in future.  相似文献   
46.
共同购买网络的推荐系统应用越加广泛,仅基于网络内生结构变量研究其共同购买链接的经济意义已有局限,故加入网络口碑这一外生变量,进行更全面的分析。采用了社会网络方法中指数随机图模型进行建模,主要围绕产品销售量、产品入度、差评率和评论数4个方面因素,探究其对共同购买网络中共同购买链接形成的影响。结果显示,销售量、产品入度和评论数对共同购买链接形成的影响呈正比关系,而差评率则会显著地降低产品共同购买的几率。该指数随机图构建出的共同购买网络为在线电商平台管理网络口碑和推荐系统优化设计提供有益参考。  相似文献   
47.
《Ceramics International》2022,48(18):26147-26167
The failure and fragmentation of monolithic bare alumina 99.5% ceramic target and energy dissipation of steel 4340 projectile have been studied in a series of ballistic experiments carried out, with the incidence velocities in a range, 122–290 m/s. The velocity drop and energy dissipation increased with incidence velocity for 10 mm thick target with damage zone extended upon the whole area of rear face at higher velocities. The ballistic results obtained with the 10 mm thick target have been compared with the ballistic performance of the 5 mm thick target used in a previous study to explore the effects of target thickness on the failure mechanism. A model for the residual velocity of projectile after perforation of the single layered ceramic target has been developed based on the Lambert Jonas model by using the experimental data available for 5 mm and 10 mm thick alumina 99.5% target against 10.9 mm projectile. The residual velocities and damage patterns were reproduced with a reasonable amount of accuracy by a three-dimensional finite element model developed on commercial ABAQUS/CAE. The effect of obliquity and projectile diameter to target thickness ratio (D/T) on ballistic performance has been determined by the numerical simulation model with impact velocity in a range of 300–500 m/s. A spatial variation of ejected fragments velocity at different time steps was plotted to develop a velocity profile for the ceramic fragments coming out of the target. A semi-empirical model has been proposed for residual velocity after perforation of a monolithic ceramic target, relating to the incidence velocity and projectile diameter to target thickness ratio. The monolithic ceramic targets have been investigated for a comparative assessment of energy dissipation by the ceramic layer to eventually design an efficient front layer of a ceramic based composite armour in future studies.  相似文献   
48.
Edge Computing is one of the radically evolving systems through generations as it is able to effectively meet the data saving standards of consumers, providers and the workers. Requisition for Edge Computing based items have been increasing tremendously. Apart from the advantages it holds, there remain lots of objections and restrictions, which hinders it from accomplishing the need of consumers all around the world. Some of the limitations are constraints on computing and hardware, functions and accessibility, remote administration and connectivity. There is also a backlog in security due to its inability to create a trust between devices involved in encryption and decryption. This is because security of data greatly depends upon faster encryption and decryption in order to transfer it. In addition, its devices are considerably exposed to side channel attacks, including Power Analysis attacks that are capable of overturning the process. Constrained space and the ability of it is one of the most challenging tasks. To prevail over from this issue we are proposing a Cryptographic Lightweight Encryption Algorithm with Dimensionality Reduction in Edge Computing. The t-Distributed Stochastic Neighbor Embedding is one of the efficient dimensionality reduction technique that greatly decreases the size of the non-linear data. The three dimensional image data obtained from the system, which are connected with it, are dimensionally reduced, and then lightweight encryption algorithm is employed. Hence, the security backlog can be solved effectively using this method.  相似文献   
49.
《Ceramics International》2022,48(1):769-775
Brittle materials generally exhibit size effects, and the mechanical properties of these materials degrade significantly with an increase in size. However, the mathematical law governing the attenuation degree of mechanical properties with the increase in size is still unknown. In this study, maximum loads of differently sized ceramic test strips were subjected to three point bending tests under two working conditions of equal spans and span amplifications, respectively. Subsequently, the theoretical maximum loads of materials were calculated using the finite element method (FEM). By calculating the difference between the calculated values and the actual maximum loads, the attenuation of mechanical properties of ceramic samples were observed. The results show that the theoretical mechanical properties and the performance attenuation caused by the size effect tend to increase according to the following equation: y=ax3+bx2+cx+d. Therefore, mechanical properties and performance attenuation of any sample exhibiting a size within the experimental range can be predicted by a mathematical law, which was obtained through mechanical tests results of four samples with different sizes. The obtained mathematical law holds great significance for predicting the mechanical properties of materials under size effects.  相似文献   
50.
The capture of particles by charged droplets was simulated by considering the electrostatic interactions of droplet-droplet and droplet-particle. The results indicate that the electrostatic repulsion between droplets leads to a dynamic accumulation mode of particles. However, the droplet spacing has an insignificant effect on the capture efficiency when the electrostatic deposition predominates. The increase of droplet charge remarkably improves the capture efficiency, in which the capture of fine particles accounts for the largest proportion. Compared to the droplet charge, the droplet size shows a limited improvement in the capture efficiency. Reducing the droplet velocity prolongs the capture time instead of enhancing the capture capacity per unit time, thereby improving capture efficiency.  相似文献   
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