Design,Synthesis, and in vitro Evaluation of Tubulin-Targeting Dibenzothiazines with Antiproliferative Activity as a Novel Heterocycle Building Block

We prepared a series of free NH and N-substituted dibenzonthiazines with potential anti-tumor activity from N-aryl-benzenesulfonamides. A biological test of synthesized compounds (59 samples) was performed in vitro measuring their antiproliferative activity against a panel of six human solid tumor cell lines and its tubulin inhibitory activity. We identified 6-(phenylsulfonyl)-6H-dibenzo[c,e][1,2]thiazine 5,5-dioxide and 6-tosyl-6H-dibenzo[c,e][1,2]thiazine 5,5-dioxide as the best compounds with promising values of activity (overall range of 2–5.4 μM). Herein, we report the dibenzothiazine core as a novel building block with antiproliferative activity, targeting tubulin dynamics.     

Flow conditioning system for tri-sonic high pressure aerothermal testing

Blowdown testing offers a cost-effective experimental tool to replicate the aerothermal conditions in numerous high speed systems. The wind tunnel must replicate the inlet operating conditions, while the spatial and time dependent inlet flow conditions should be assessed carefully. This paper provides a design methodology and rules that ensure adequate flow conditioning in high inlet pressure wind tunnels suitable for subsonic and supersonic operation with mass-flow limits ranging from 1 kg/s to 25 kg/s, Reynolds numbers from 10³ (1/m) to 4x10⁷ (1/m), and Mach numbers from 0.01 up to 6. The quality of the proposed flow conditioning system was evaluated using stereo PIV measurements combined with hotwire, Pitot probe, and total flow temperature traverses.     

尽善尽美——儒家思想对中国设计的启示

经过几千年的发展和接受,儒家逐步确立了在中国主流意识形态中的“正典”地位。但应该承认,我们对于儒家的接受并不是不加批判全盘照搬的。在这两千多年的时间里,社会生活和意识形态领域所发生的重大变化我们不可能视而不见,而儒家思想恰恰有很大一部分是属于社会学科范畴之内的,在今天明显已经失去积极的意义(比如一些封建宗法),对此当然不能过分坚持,否定发展。因此,对于当今海外的“新儒家”的一些做法,可以欣赏他们对于中国传统文化的热忱,但必须承认那只是一部分知识分子的精英心态,从社会学的眼光看,的确过于保守,不利于文化的创造,特别是不能适应于现代艺术和设计的发展。本文希望区分出儒家思想中具有时代性和永恒性两个方面的内容,在对其已没有价值的社会伦理思想自觉进行发展的同时,对其永恒的东西进行一种当代的阐释。     

Systematic optimization of corrosion,bioactivity, and biocompatibility behaviors of calcium-phosphate plasma electrolytic oxidation (PEO) coatings on titanium substrates

To optimize the corrosion, bioactivity, and biocompatibility behaviors of plasma electrolytic oxidation (PEO) coatings on titanium substrates, the effects of five process variables including frequency, current density, duty cycle, treatment time, and electrolyte Ca/P ratio were evaluated. In our systematic study, a Taguchi design of experimental based on an L16 orthogonal array was used. For this, the coatings characteristics such as the surface roughness, wettability, rutile to anatase and Ca/P ratios, and corrosion polarization resistance were investigated. After determining the optimum process variables for each response, the apatite forming ability in SBF (bioactivity behavior) and MG63 cell attachment and flattening (biocompatibility behavior) for two groups of coatings were examined. The first group was optimized based on the maximum corrosion polarization resistance and the variables were set as the frequency of 2000 Hz, the current density of 5 A/dm², the duty cycle of 30%, the treatment time of 5 min, and the Ca/P ratio of 0.65 at. % in the electrolyte. For the second group, the maximum surface roughness, greatest Ca/P ratio, and highest wettability as well as the minimum rutile to anatase ratio in coatings, could be obtained when the variables were set as the frequency of 10 Hz, the current density of 12.5 A/dm², the duty cycle of 50%, the treatment time of 12.5 min, and the Ca/P ratio of 1.70 at. % in the electrolyte. The results showed that while both groups of coatings indicated a significant apatite forming ability and can serve as bioactive coatings, a proper attachment and flattening of cells and consequently, the favorable biocompatibility properties were seen only in the first group.     

中国抗中子辐照钢的抗辐照设计与验证

聚变堆等未来先进核能系统要求材料在强流高能中子辐照下长期保持良好的结构稳定性和机械性能。为适应未来先进核能技术发展的需要，中国科学院核能安全技术研究所•凤麟团队牵头研发了具有我国自主知识产权的中国抗中子辐照钢--CLAM钢。CLAM钢的设计考虑了未来核能清洁性的要求，以及苛刻服役环境中材料抗辐照、耐高温、耐腐蚀等性能要求。通过中子学计算分析设计了低活化成分范围，基于选择性纳米相析出进行了抗辐照、耐高温性能优化设计。针对材料的抗辐照性能，利用国内外中子、离子、电子及等离子体辐照设施开展了系列辐照考验研究，通过多角度表征辐照前后材料的微观结构和宏观性能，综合评估了材料的辐照性能，并与国际上同类材料在相近或相同条件下的辐照性能进行了对比分析，结果表明CLAM钢具有良好的抗辐照性能。     

Dependence of grip strength on shoulder position and its implications for ergonomics practice

Grip strength (GS) variability due to positional changes in the upper extremity joints is of importance while designing workstations and work methods. This study was conducted to analyze the GS variations due to positional changes at shoulder joint when some important variables were under control. The GSs of dominant and nondominant hands were measured in eight shoulder (0°, 45°, 90°, and 135° of flexion and abduction) and standard test positions (STP). One hundred and thirteen subjects 20–30 years old completed the study. At the dominant side, no significant difference was observed in the pairwise comparisons between STP and the others. Maximum and minimum GSs were obtained in 0° abduction and 45° flexion and abduction, respectively. At the nondominant side, GSs were significantly lower (p < 0.001) in the corresponding test positions and demonstrated more variability. The findings of this study can contribute to the available knowledge to guide occupational ergonomists in their practices.     

Taxonomy of digital community currency platforms*

ABSTRACT

Community currencies are used to pay for products or services within specific groups defined by geographical boundaries or specific common interests. Financial crises, social emergence in developing countries, and increased access to digital devices have stimulated a growing number of communities worldwide to develop digital currency projects. These projects use technologies ranging from traditional plastic cards to mobile phones and blockchain technologies. Following the design science research approach, this paper analyzes digital community currencies (DCCs) by developing a taxonomy based on platform architecture, governance, transactionality and virtuality. By investigating 22 DCC platforms around the world, 4 groups were distinguished: local, proprietary, commons and cyber. The identification of these four different groups of digital community currencies allows us to better discuss the potentials and limitations of each one of them. The presented taxonomy can be useful to researchers and practitioners both to explain and to design DCC platforms. Discussing each of the emerging categories from the proposed taxonomy helps us to provide insights into DCCs, offering a new theoretical frame for investigating the particular case of digital payment platforms.     

Solid lipid nanoparticles of Annona muricata fruit extract: formulation,optimization and in vitro cytotoxicity studies

The present study was aimed to develop Annona muricata fruit extract loaded solid lipid nanoparticles (SLNs) and explore its cytotoxic potential in vitro model of breast cancers. Extract loaded SLNs were successfully prepared by high-pressure homogenization followed by ultrasonication method and optimized using 2³ full factorial design. The extract loaded SLNs were characterized using different parameters such as particle size (PS), % entrapment efficiency (EE), zeta potential (ZP) and % cumulative drug release (CDR). The SLNs formulation was optimized on the basis of software analysis with an overall desirability factor. The PS and %EE of the optimized formulation were found to be 134.8?nm and 83.26%, respectively. The optimized formulation showed a CDR of 79.83% up to 48?h. In vitro cytotoxicity efficacy of extract loaded SLNs was determined using MTT and Apoptosis assay and compared to that of a free extract. The SLNs showed a notable apoptotic effect and better efficacy to kill MCF7 cancer cells as compared to free extract. Thus, extract loaded SLNs could be an alternative dosage form which possibly controls therapeutic action with reducing side effect.     

Synthesis of Benzophenones and in vitro Evaluation of Their Anticancer Potential in Breast and Prostate Cancer Cells

Breast and prostate cancers are frequently treated with chemotherapy. Several novel chemicals are being reported for this purpose, particularly synthetic and natural benzophenones. This work reports the synthesis of substituted 2-hydroxybenzophenones through 1,4-conjugate addition/intramolecular cycloaddition/dehydration of nitromethane on key intermediate chromones. Structures were extensively studied by means of 2D NMR spectroscopy and single-crystal XRD. Their cytotoxicity was evaluated in vitro in two breast cancer cell lines (MDA-MB-231 and T47-D) and one prostate cancer cell line (PC3). The most potent compound exhibited good cytotoxic effects against the three cancer cell lines (IC₅₀ values ranging from 12.09 to 26.49 μm ) and induced cell-cycle retardation only on prostate cancer cells, which suggested that it might exert cell-type-specific effects.