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951.
Dr. Zhichao Du Dr. Guolong Li Dr. Haixia Ge Xiaoyang Zhou Prof. Jian Zhang 《ChemMedChem》2021,16(9):1488-1498
To systematically evaluate the impact of neoglycosylation upon the anticancer activities and selectivity of steroids, four series of neoglycosides of diosgenin, pregnenolone, dehydroepiandrosterone and estrone were designed and synthesized according to the neoglycosylation approach. The structures of all the products were elucidated by NMR analysis, and the stereochemistry of C20-MeON-pregnenolone was confirmed by crystal X-ray diffraction. The compounds′ cytotoxicity on five human cancer cell lines was evaluated using a Cell Counting Kit-8 assay, and structure–activity relationships (SAR) are discussed. 2-deoxy-d -glucoside 5 k displayed the most potent antiproliferative activities against HepG2 cells with an IC50 value of 1.5 μM. Further pharmacological experiments on compound 5 k on HepG2 cells revealed that it could cause morphological changes and cell-cycle arrest at the G0/G1 phase and then induced the apoptosis, which might be associated with the enhanced expression of high-mobility group Box 1 (HMGB1). Taken together, these findings prove that the neoglycosylation of steroids could be a promising strategy for the discovery of potential antiproliferative agents. 相似文献
952.
Prof. Ren-Xiao Wang Mi Zhou Hui-Lai Ma Prof. Yuan-Biao Qiao Prof. Qing-Shan Li 《ChemMedChem》2021,16(10):1576-1592
Chronic inflammation represents a long-term reaction of the body's immune system to noxious stimuli. Such a sustained inflammatory response sometimes results in lasting damage to healthy tissues and organs. In fact, chronic inflammation is implicated in the development and progression of various diseases, including cardiovascular diseases, respiratory diseases, metabolic diseases, neurodegenerative diseases, and even cancers. Targeting nonresolving inflammation thus provides new opportunities for treating relevant diseases. In this review, we will go over several chronic inflammation-associated diseases first with emphasis on the role of inflammation in their pathogenesis. Then, we will summarize a number of natural products that exhibit therapeutic effects against those diseases by acting on different markers in the inflammatory response. We envision that natural products will remain a rich resource for the discovery of new drugs treating diseases associated with chronic inflammation. 相似文献
953.
Xu Yunfei He Liang Lei Qi Luo Hongzhi Zhou Cheng Mao Wei Cheng Xiaojuan Li Jianmin Zou Guifu 《SILICON》2021,13(5):1641-1646
Silicon - Nowadays, casted multicrystalline silicon is the most important material in photovoltaic industry. In order to reduce the cost of silicon ingots, the recycle of silicon ingot tailings is... 相似文献
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956.
多自由度电机可以实现空间中的复杂运动,且具有结构简单、精确度高等优势,在机器人仿生关节、机械手臂及工业制造业上具有广阔的应用前景。对多自由度电机的背景、基本原理及技术优势进行了相关叙述。按照驱动机理的不同将多自由度电机进行分类,并对当前多自由度电机的国内外研究现状进行了总结。此外,基于多自由度电机的运动特点,对电机控制过程中的位置检测技术和运动控制策略进行了相关分析。最后,从多自由度电机的结构、控制体系、材料及制造工艺等方面进行了相关的叙述,对多自由度电机的发展趋势进行预测。通过对多自由度电机的研究与分析,为其未来的发展提供参考。 相似文献
957.
By the virtue of their olfactory, physicochemical, and biological characteristics, essential oils (EOs) have drawn wide attention as additives in daily chemicals like perfume or personal care products. Nevertheless, they are physicochemically unstable and susceptible to degradation or loss. Microencapsulation offers a feasible strategy to stabilize and prolong release of EO. This review summarizes the recognized benefits and functional properties of various preparation and characterization methods, wherein innovative fabrication strategies and their formation mechanisms are especially emphasized. Progress in combining detecting/measuring technologies with kinetic modelling are discussed, to give an integral approach of controlling the dynamic release of encapsulated EOs. Moreover, new development trends of EOs capsules are also highlighted. 相似文献
958.
为了探究热氧老化后乙丙橡胶电缆绝缘的局部放电特性及劣化机理,文中通过典型柱–板电极对不同老化程度的乙丙橡胶试样进行了局部放电试验,并对其放电发展特性和材料理化性质进行了分析。结果表明:放电起始电压和闪络电压均随绝缘老化程度的提高而降低;根据放电过程中放电特征量的变化规律,可将放电过程划分为4个阶段:起始阶段、发展阶段、持续阶段、预闪络阶段,且不同老化程度试样的PRPD谱图在各阶段呈现出特定形状;老化后的试样表面气化或气体解吸附、内部添加剂成分析出导致试样表面出现"沟壑区"、白色块状物和"微孔",分子结构中的羰基等含氧基团、聚乙烯和聚丙烯等自由基数量的增加是乙丙橡胶绝缘在热氧老化后更易出现局部放电的关键原因。 相似文献
959.
为了实现油浸式变压器油中溶解气体的预测,进而达到变压器状态预警、降低事故发生率的目的,本文将自适应粒子群优化算法(IDP SO)和最小二乘支持向量机(LSSVM)相结合,建立变压器油中溶解气体预测模型.利用IDP SO算法基于种群的并行搜索策略特点来自适应迭代搜索最优的目标函数值,寻找LSSVM模型中的参数ξ、C和σ的最优取值,克服了应用传统支持向量机算法进行预测时凭主观经验选择参数对模型泛化能力和预测性能的影响.利用国网陕西省电力公司某变电站采集变压器油色谱数据进行实例验证,结果表明基于IDP SO优化的LSSVM算法具有较好的模式跟踪性能,且能够有效提高变压器油中溶解气体预测的预测精度. 相似文献
960.
Junyang Xu Yanjun Jiang Liya Zhou Li Ma Zhihong Huang Jiafu Shi Jing Gao Ying He 《中国化学工程学报》2021,38(10):237-246
Immobilization is an effective method to promote the application of enzyme industry for improving the stability and realizing recovery of enzyme.To some extent,the performance of immobilized enzyme depends on the choice of carrier material.Therefore,the development of new carrier materials has been one of the key issues concerned by enzyme immobilization researchers.In this work,a novel organic-inorganic hybrid material,nickel-carnosine complex (NiCar),was synthesized for the first time by solvothermal method.The obtained NiCar exhibits spherical morphology,hierarchical porosity and abun-dant unsaturated coordination nickel ions,which provide excellent anchoring sites for the immobiliza-tion of proteins.His-tagged organophosphate-degrading enzyme (OpdA) and ω-transaminase (ω-TA)were used as model enzymes to evaluate the performance of NiCar as a carrier.By a simple adsorption process,the enzyme molecules can be fixed on the particles of NiCar,and the stability and reusability are significantly improved.The analysis of protein adsorption on NiCar verified that the affinity adsorp-tion between the imidazole functional group on the protein and the unsaturated coordination nickel ions on NiCar was the main force in the immobilization process,which provided an idea way for the develop-ment of new enzyme immobilization carriers. 相似文献