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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.
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   
48.
为研究渗流作用下新型装配重力式挡土墙应力变化及墙体排水通道对墙后土体固结的影响,采用ABAQUS进行有限元分析,有限元分析结果与模型试验结果相吻合,证明该模型的合理性。在此基础上研究渗流作用下墙体应力变化趋势及墙体排水通道对墙后土体固结效果的影响。研究结果表明:横向排水通道对墙后土体固结效果的影响优于纵向排水通道对土体固结效果的影响,墙体底部横向排水通道的影响作用最显著;渗流作用下墙体应力由上往下呈先增大后减小的趋势,墙体下部所受最大水平剪应力最大。  相似文献   
49.
Heat treatment will affect the nutritional properties and potential bioactivity of food materials. The aim of this work was to evaluate the effect of different thermal treatment (4, 56, 65 and 100 ℃) and in vitro gastrointestinal digestion on the antioxidant activity of egg white hydrolysate. The results demonstrated that egg white hydrolysate treated at 65 ℃ exhibited the highest antioxidant. Remarkably, the simulated digestion significantly increased antioxidant activity of egg white hydrolysate. Furthermore, we identified twenty-four potential antioxidant peptides by performing mass spectrometry and bioinformatic analysis. Six peptides were selected based on the activity prediction score of the online tool. The results showed that P6 (ACPECPK) possessed the most outstanding antioxidant properties and had low cytotoxicity and allergenicity. Bioinformatics technology combined with biochemical assays may offer a way for discovering novel antioxidant peptides from different kinds of food under various heat treatment conditions.  相似文献   
50.
《Ceramics International》2022,48(3):3536-3543
We investigated the optical and electrical properties of Ta2O5/Ag/Ta2O5 films as functions of the thicknesses of the Ta2O5 and Ag layers. It was found that with an increase in the thicknesses of the Ta2O5 and Ag layers from 10 to 40 nm and from 12 to 24 nm, respectively, the sheet resistance, carrier concentration, electron mobility, and resistivity of the Ta2O5/Ag/Ta2O5 film varied from 2.02 to 8.95 Ω/sq, 5.74 × 1021 to 2.92 × 1022 cm–3, from 13.21 to 24.07 cm2/V·s, and from 8.89 × 10-6 to 8.24 × 10-5 Ω cm, respectively. The average transmittance (Tav) of the multilayer samples ranged from 57.18% to 93.99%, and it depended on the Ta2O5 and Ag layer thicknesses. The highest Tav of 93.99% was observed for the film with 35 nm thick Ta2O5 and 18 nm thick Ag layers, and the peak Haacke's figure of merit (157.04 × 10–3 Ω–1) was obtained for 20 nm thick Ta2O5 and 21 nm thick Ag layers. Ta2O5 (100 nm) and Ta2O5/Ag/Ta2O5 (20 nm/21 nm/20 nm) samples had optical bandgaps of 4.70 and 4.45 eV, respectively. Film Wizard simulations were conducted to understand the dependence of the transmittance of the multilayer on the thicknesses of the Ta2O5 and Ag layers, and phasor analyses were performed to determine how the transmittance of the Ta2O5/Ag/Ta2O5 (20 nm/21 nm/20 nm) film depended on the Ta2O5 layer's thickness.  相似文献   
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