Synthesis and Pharmacological In Vitro Investigations of Novel Shikonin Derivatives with a Special Focus on Cyclopropane Bearing Derivatives

Melanoma is the deadliest form of skin cancer and accounts for about three quarters of all skin cancer deaths. Especially at an advanced stage, its treatment is challenging, and survival rates are very low. In previous studies, we showed that the constituents of the roots of Onosma paniculata as well as a synthetic derivative of the most active constituent showed promising results in metastatic melanoma cell lines. In the current study, we address the question whether we can generate further derivatives with optimized activity by synthesis. Therefore, we prepared 31, mainly novel shikonin derivatives and screened them in different melanoma cell lines (WM9, WM164, and MUG-Mel2 cells) using the XTT viability assay. We identified (R)-1-(1,4-dihydro-5,8-dihydroxy-1,4-dioxonaphthalen-2-yl)-4-methylpent-3-enyl 2-cyclopropyl-2-oxoacetate as a novel derivative with even higher activity. Furthermore, pharmacological investigations including the ApoToxGlo^TM Triplex assay, LDH assay, and cell cycle measurements revealed that this compound induced apoptosis and reduced cells in the G1 phase accompanied by an increase of cells in the G2/M phase. Moreover, it showed hardly any effects on the cell membrane integrity. However, it also exhibited cytotoxicity against non-tumorigenic cells. Nevertheless, in summary, we could show that shikonin derivatives might be promising drug leads in the treatment of melanoma.     

焊接构造对T型接头超低周疲劳性能的影响

为了研究焊接细节对钢结构超低周疲劳性能的影响,以T型接头为对象,在通用有限元程序Abaqus平台上,开发基于Arlequin算法的结构多尺度计算程序. 利用多尺度算法,开展焊接接头的局部弹塑性有限元分析. 比较焊趾半径、厚钢板未熔透长度及焊趾表面凹凸对局部塑性应变履历的影响,利用Coffin-Manson模型对T型接头的超低周疲劳特性进行定性讨论. 数值计算结果表明,焊趾位置是焊接接头的超低周疲劳易损位置,厚钢板的未熔透长度对焊接部位局部塑性应变的影响不大;焊趾半径对焊趾局部塑性应变有较大的影响,增大焊趾半径可以有效提升钢结构在循环荷载下的超低周疲劳性能;焊趾表面的平整性是影响焊趾局部塑性应变履历的重要因素,尖锐的凹坑会明显降低焊接接头的超低周疲劳性能,磨平的焊趾表面可以减少局部塑性应变,提高接头的超低周疲劳强度.     

教育盛衰与王朝周期律

教育发展周期比王朝盛衰周期长。在同一教育发展周期内，王朝的衰落带来教育发展的小幅波动，新王朝创立之后能在较短的时间内修复原有的教育结构。而当教育结构自身开始坍塌的时候，王朝的衰落则明显加快这一坍塌的过程。教育结构的重建一般需要几个世纪，这一时期内王朝频繁更替，教育与王朝政治处于两衰的恶性循环中。教育与王朝政治的依存关系形成于春秋战国，巩固于西汉。僵硬的教育结构与人的创造力构成持续的冲突，最终导致教育结构的坍塌。     

不可逆量子斯特林热泵循环性能分析与优化

建立了以一维无限深势阱中极端相对论粒子为工质的不可逆量子斯特林热泵循环模型。考虑高低温热源之间的热漏,导出了循环的性能系数与无量纲泵热率的表达式。分析了循环性能与各性能参数之间的关系。研究发现,热泵的性能系数与无量纲泵热率都随粒子在状态1进处于激收态上的占有几度单调递减,性能系数与无量纲泵热率都是势阱宽度比的凸单调函数。无量纲泵热率关于性能系数的关系曲线为回原点的扭叶型,并确定了该不可逆量子斯特林热泵的最优运行区间。     

Effect of supports on the redox performance of pyrite cinder in chemical looping combustion

Chemical looping combustion (CLC) is a clean and efficient flame-free combustion technology,which combust the fuels by lattice oxygen from a solid oxygen carrier with inherent CO2 capture.The develop-ment of oxygen carriers with low cost and high redox performance is crucial to the whole efficiency of CLC process.As the solid by-product from the sulfuric acid production,pyrite cinder presented excellent redox performance as an oxygen carrier in CLC process.The main components in pyrite cinder are Fe2O3,CaSO4,Al2O3 and SiO2 in which Fe2O3 is the active component to provide lattice oxygen.In order to sys-tematic investigate the functions of supports (CaSO4,Al2O3 and SiO2) in pyrite cinder,three oxygen car-riers (Fe2O3-CaSO4,Fe2O3-Al2O3 and Fe2O3-SiO2) were prepared and evaluated in this study.The results showed that Fe2O3-CaSO4 displayed high redox activity and cycling stability in the multiple redox cycles.However,both Fe2O3-Al2O3 and Fe2O3-SiO2 experienced serious deactivation during redox reactions.It indicated that the inert Fe-Si solid solution (Fe2SiO4) was formed in the spent Fe2O3-SiO2 sample,which decreased the oxygen carrying capacity of this sample.The XPS results showed that the oxygen species on the surface of Fe2O3-CaSO4 could be fully recovered after the 20 redox cycles.It can be concluded that CaSO4 is the key to the high redox activity and cycling stability of pyrite cinder.     

Simulated Microgravity Inhibits the Proliferation of Chang Liver Cells by Attenuation of the Major Cell Cycle Regulators and Cytoskeletal Proteins

Simulated microgravity (SMG) induced the changes in cell proliferation and cytoskeleton organization, which plays an important factor in various cellular processes. The inhibition in cell cycle progression has been considered to be one of the main causes of proliferation inhibition in cells under SMG, but their mechanisms are still not fully understood. This study aimed to evaluate the effects of SMG on the proliferative ability and cytoskeleton changes of Chang Liver Cells (CCL-13). CCL-13 cells were induced SMG by 3D clinostat for 72 h, while the control group were treated in normal gravity at the same time. The results showed that SMG reduced CCL-13 cell proliferation by an increase in the number of CCL-13 cells in G0/G1 phase. This cell cycle phase arrest of CCL-13 cells was due to a downregulation of cell cycle-related proteins, such as cyclin A1 and A2, cyclin D1, and cyclin-dependent kinase 6 (Cdk6). SMG-exposed CCL-13 cells also exhibited a downregulation of α-tubulin 3 and β-actin which induced the cytoskeleton reorganization. These results suggested that the inhibited proliferation of SMG-exposed CCL-13 cells could be associate with the attenuation of major cell cycle regulators and main cytoskeletal proteins.     

快淬工艺对无钴AB5型贮氢合金循环稳定性的影响

研究了快淬工艺对无钴AB5型LaxMm1-x(NiMnSiAlFe)4.9(x=0,0.45,0.75,1.0)合金微观结构及电化学循环稳定性的影响.结果表明快淬处理显著改善合金的成分均匀性,使晶粒细化,并显著提高合金的循环稳定性.当淬速从0m/s增加到28 m/s时,经300次充放循环后,x=0.45合金的容量衰减率D从0.28 mAh/g·c-1(c代表一次循环)下降到0.13mAh/g·c-1;x=1.0合金的容量衰减率D从0.3mAh/g·c-1下降到0.14mAh/g·c-1.     

Fe替代Co对AB5型贮氢合金循环稳定性的影响

用铸造及快淬的方法制备了稀土基AB5型Mm（NiMnSiAl）4．3Co0.6-xFex（x=0，0．1，0．2，0．3，0．4，0．5，0．6）贮氢合金，用XRD。TEM及SEM观测了铸态及快淬态的微观结构，测试了合金在铸态及快淬态下的电化学循环稳定性。研究了Fe替代Co对铸态及快淬态贮氢合金微观结构及循环稳定性的影响。研究结果表明，Fe替代Co对铸态及快淬态合金的相结构没有明显影响，但对合金的循环稳定性产生显著影响。Fe替代Co能不同程度地改善铸态及快淬态合金的循环稳定性，但对快淬态合金循环寿命的改善更加显著，导致这一结果的主要原因是Fe替代Co使快淬态合金的微观组织显著细化。     

High cycle fatigue behaviour of Ti–6Al–4V alloy at elevated temperatures

High cycle fatigue behaviour of Ti–6Al–4V alloy was studied at 623 K and 723 K. Fatigue strength decreased at elevated temperatures compared with at ambient temperature. In the short life regime, fatigue strength was lower at 723 K than at 623 K, but in the long life regime it was nearly the same at both temperatures. At elevated temperatures, cracks were generated earlier at applied stresses below the fatigue limit at ambient temperature, indicating lowered crack initiation resistance. Small cracks grew faster at elevated temperatures than at ambient temperature, which became more noticeable with increasing temperature. After allowing for the elastic modulus, small cracks still grew faster at elevated temperatures.     

九江大化肥Shell之碳黑回收技术探讨

对九江大化肥厂Shell渣油气化碳黑闭路循环和石脑油萃取碳黑的成熟可靠性等技术问题进行了探讨。