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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.
To benefit from recent advances in modeling and computational algorithms,as well as the availability of new covariance data,sensitivity and uncertainty analyses are needed to quantify the impact of uncertain sources on the design parameters of small prismatic high-temperature gas-cooled reactors(HTGRs).In particular,the contribution of nuclear data to the keff uncertainty is an important part of the uncertainty analysis of small-sized HTGR physical calculations.In this study,a small-sized HTGR designed by China Nuclear Power Engineering Co.,Ltd.was selected for keff uncertainty analysis during full lifetime burnup calculations.Models of the cold zero power(CZP)condition and full lifetime burnup process were constructed using the Reactor Monte Carlo Code RMC for neutron transport calculation,depletion calculation,and sensitivity and uncertainty analysis.For the sensitivity analysis,the Contribution-Linked eigenvalue sensitivity/Uncertainty estimation via Track length importance Characterization(CLUTCH)method was applied to obtain sensitive infor-mation,and the"sandwich"method was used to quantify the keff uncertainty.We also compared the keff uncertainties to other typical reactors.Our results show that 235U is the largest contributor to keff uncertainty for both the CZP and depletion conditions,while the contribution of 239Pu is not very significant because of the design of low discharge burnup.It is worth noting that the radioactive capture reaction of 28Si significantly contributes to the keff uncer-tainty owing to its specific fuel design.However,the keff uncertainty during the full lifetime depletion process was relatively stable,only increasing by 1.12%owing to the low discharge burnup design of small-sized HTGRs.These numerical results are beneficial for neutronics design and core parameters optimization in further uncertainty prop-agation and quantification study for small-sized HTGR.  相似文献   
3.
文婷  李波 《机械与电子》2021,39(2):21-24
对IEC 60870-5-104协议的调度命令进行了研究,提出了一种基于现有IEC 60870-5-104协议的调度命令发送新方法。此技术充分利用了IEC 60870-5-104协议的文件发送功能,通过远程终端单元(RTU)向电厂发送包含调度命令的文本文件。考虑到调度命令在电力系统和电力市场结算系统安全方面的重要性,将该方法应用在电网调度自动化 SCADA 系统中,可以实现交换数据的更高可用性。  相似文献   
4.
This paper analyses the perception of Artificial Intelligence (AI) by individuals in Spain and the factors associated with it. It uses data from 6308 individuals from a 2018 Spanish survey. A binary logit regression model is formulated and estimated for the attitude towards robots and AI and its possible determinants. As main results are that a gender gap is detected, and that people have a negative attitude if they are not interested in scientific discoveries and technological developments and if AI and robots are not useful at work.  相似文献   
5.
梯度分层铝合金蜂窝板是一种有效的吸能结构,本工作在梯度铝蜂窝结构的基础上根据梯度率的概念,通过改变蜂窝芯层的胞壁长度,设计了4种质量相同、梯度率不同的铝蜂窝夹芯结构。通过准静态压缩实验,并结合非线性有限元模拟准静态及冲击态下梯度铝蜂窝夹芯结构的变形情况及其力学性能,分析对比了相同质量下梯度铝蜂窝夹芯结构在准静态下的变形模式以及冲击载荷下分层均质蜂窝结构和不同梯度率的分层梯度蜂窝结构的动态响应和能量吸收特性。结果表明:在准静态压缩过程中,铝蜂窝梯度夹芯板的变形具有明显的局部化特征,蜂窝芯的变形为低密度优先变形直至密实,层级之间的密实化应变差随芯层密度的增大而逐渐减小;在高速冲击下,梯度蜂窝板并非严格按照准静态过程中逐级变形直至密实,而是在锤头冲击惯性及芯层密度的相互作用下整体发生的线弹性变形、弹性屈曲、塑性坍塌及密实化;另外,在本工作所设计的梯度率中,当梯度率为γ1=0.0276时,梯度蜂窝夹芯板的吸能性达到最好,相较于同等质量下的均质蜂窝夹芯板,能量吸收提高了10.63%。  相似文献   
6.
7.
The ways in which environmental priorities are framed are varied and influenced by political forces. One technological advance--the proliferation of government open data portals (ODPs)--has the potential to improve governance through facilitating access to data. Yet it is also known that the data hosted on ODPs may simply reflect the goals and interests of multiple levels of political power. In this article, I use traditional statistical correlation and regression techniques along with newer natural language processing and machine learning algorithms to analyze the corpus of datasets hosted on government ODPs (total: 49,066) to extract patterns that relate scales of governance and political liberalism/conservatism to the priorities and meaning attached to environmental issues. I find that state-level and municipal-level ODPs host different categories of environmental datasets, with municipal-level ODPs generally hosting more datasets pertaining to services and amenities and state-level ODPs hosting more datasets pertaining to resource protection and extraction. Stronger trends were observed for the influences of political conservatism/liberalism among state-level ODPs than for municipal-level ODPs.  相似文献   
8.
9.
针对现有基于视频监控的人流量统计方案成本高、算法复杂且不利于个人隐私保护的局限性,利用毫米波雷达体积小、成本低、分辨率高的特点,提出了一种基于双时间点检测的人流量监测方法。该方法先获取人体目标散射点位置和多普勒频移信息来构成点云数据,然后根据多普勒频移正负来判断人体的运动方向,并筛选具有高多普勒频移值的点云数据以降低干扰点对聚类结果的影响;在双时间点对特定区域内人员数量进行统计,并根据双时间点之间所获取的点云数据聚类结果对所统计人员数据进行修正。实验结果表明,该方法能够用匿名的方式以较高的正确率统计人员进出。  相似文献   
10.
文猛  张释如 《包装工程》2022,43(21):162-168
目的 为了解决目前三维数据隐藏算法不能兼顾无失真和盲提取的问题,提出一种新的完全无失真的三维网格模型数据隐藏盲算法。方法 首先使用混沌逻辑映射选择嵌入与提取模式,保证数据的安全性。然后利用面元素重排,完全不会造成三维模型失真的性质,通过不同嵌入模式规则对三角面元素进行重排,以嵌入秘密数据。接收端则可根据相应的提取模式规则提取秘密数据。结果 仿真结果与分析表明,该算法不会对三维模型造成任何失真,嵌入容量为每顶点2比特,且能抵抗仿射变换攻击、噪声攻击和平滑攻击等。结论 这种三维数据隐藏盲算法无失真,容量大、安全性高、鲁棒性强,适用于三维载体不容修改的情形,如军事、医学、秘密通信和版权保护等。  相似文献   
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