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A series of (trifluoromethyl)cyclopropanes (TFCPs) tolerating a broad range of functional groups, known as tert-butyl bioisosteres, have been obtained from the cyclization reaction between nitromethane­ and 5-[β-(trifluoromethyl)styryl]isoxazoles in 70–94% yields and 75:25 to 90:10 dr. This method offers practical access to this cyclopropyl moiety of pharmacological interest, employing an inorganic base under phase-transfer conditions.

Purpose In this study, pH-sensitive poly(2-ethyl-2-oxazoline)-poly(lactic acid)-poly(β-amino ester) (PEOz-PLA-PBAE) triblock copolymers were synthesized and were conjugated with an antimalaria drug artesunate (ART), for inhibition of a colon cancer xenograft model. Methods The as-prepared polymer prodrugs are tended to self-assemble into polymeric micelles in aqueous milieu, with PEOz segment as hydrophilic shell and PLA-PBAE segment as hydrophobic core. Results The pH sensitivity of the as-prepared copolymers was confirmed by acid-base titration with pKb values around 6.5. The drug-conjugated polymer micelles showed high stability for at least 96 h in PBS and 37°C, respectively. The as-prepared copolymer prodrugs showed high drug loading content, with 9.57%±1.24% of drug loading for PEOz-PLA-PBAE-ART4. The conjugated ART could be released in a sustained and pH-dependent manner, with 92% of released drug at pH 6.0 and 57% of drug released at pH 7.4, respectively. In addition, in vitro experiments showed higher inhibitory effect of the prodrugs on rodent CT-26 cells than that of free ART. Animal studies also demonstrated the enhanced inhibitory efficacy of PEOz-PLA-PBAE-ART2 micelles on the growth of rodent xenograft tumor. Conclusion The pH-responsive artesunate polymer prodrugs are promising candidates for colon cancer adjuvant therapy.

Traditional Chinese multi-herb-combined prescriptions usually show better performance than a single agent since a group of effective compounds interfere multiple disease-relevant targets simultaneously. Huang-Lian-Jie-Du decoction is a remedy made of four herbs that are widely used to treat oral ulcers, gingivitis, and periodontitis. However, the active ingredients and underlying mechanisms are not clear. To address these questions, we prepared a water extract solution of Huang-Lian-Jie-Du decoction (HLJDD), called it as WEH (Water Extract Solution of HLJDD), and used it to treat LPS-induced systemic inflammation in mice. We observed that WEH attenuated inflammatory responses including reducing production of cytokines, chemokines and interferons (IFNs), further attenuating emergency myelopoiesis, and preventing mice septic lethality. Upon LPS stimulation, mice pretreated with WEH increased circulating Ly6C- patrolling and splenic Ly6C+ inflammatory monocytes. The acute myelopoiesis related transcriptional factor profile was rearranged by WEH. Mechanistically we confirmed that WEH interrupted LPS/TLR4/CD14 signaling-mediated downstream signaling pathways through its nine principal ingredients, which blocked LPS stimulated divergent signaling cascades, such as activation of NF-κB, p38 MAPK, and ERK1/2. We conclude that the old remedy blunts LPS-induced "danger" signal recognition and transduction process at multiple sites. To translate our findings into clinical applications, we refined the crude extract into a pure multicomponent drug by directly mixing these nine chemical entities, which completely reproduced the effect of protecting mice from lethal septic shock. Finally, we reduced a large number of compounds within a multi-herb water extract to seven-chemical combination that exhibited superior therapeutic efficacy compared with WEH.

The relationship between the specific surface area (SSA) of rust and the electrochemical behavior of rusted steel under wet–dry acid corrosion conditions was investigated. The results showed that the corrosion current density first increased and then decreased with increasing SSA of the rust during the corrosion process. The structure of the rust changed from single-layer to double-layer, and the γ-FeOOH content decreased in the inner layer of the rust with increasing corrosion time; by contrast, the γ-FeOOH content in the outer layer was constant. When the SSA of the rust was lower than the critical SSA corresponding to the relative humidity during the drying period, condensed water in the micropores of the rust could evaporate, which prompted the diffusion of O2 into the rust and the following formation process of γ-FeOOH, leading to an increase of corrosion current density with increasing corrosion time. However, when the SSA of the rust reached or exceeded the critical SSA, condensate water in the micro-pores of the inner layer of the rust could not evaporate which inhibited the diffusion of O2 and decreased the γ-FeOOH content in the inner rust, leading to a decrease of corrosion current density with increasing corrosion time.

A novel unsupervised change detection for synthetic aperture radar (SAR) images using robust semi-non-negative matrix factorisation (NMF) with total variation (TV) is proposed. In order to effectively handle the noise and outliers as well as consider spatial contextual information, correntropy induced metric and TV regularisation are simultaneously integrated into semi-NMF to build a robust semi-NMF with TV model. Subsequently, the update solutions of the model are optimised by the Karush-Kuhn-Tucker condition and fast gradient projection algorithm. The experimental results demonstrate the effectiveness of the proposed method both visually and quantitatively.

Two rare N-β-D-glucopyranosyl-1H-indole-3-acetic acid conjugates, N-[2-(1-β-D-glucopyranosyl)-1H-indol-3-yl)acetyl]-L-glutamic acid (1) and N-[2-(1-β-D-glucopyranosyl)-1H-indol-3-yl)acetyl]-L-aspartic acid (2) were isolated from Ginkgo biloba. The structures were elucidated by analyses of HRMS and NMR spectroscopic data. In addition, a simplified and efficient synthetic route for compounds 1 and 2 is also disclosed to determine the absolute configurations of them. This concise syntheses of compounds 1 and 2 may facilitate studies of the biology of this type alkaloids. Compounds 1 and 2 were also tested for their cytotoxic and anti-inflammatory activities. The biological evaluation showed that compounds 1 and 2 led to the decrease of interleukin (IL)-6, nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2 at mRNA level in lipopolysaccharide (LPS)-stimulated murine macrophage RAW264.7 cells.

Docetaxel-loaded nanomicelles were prepared in this study to improve the solubility and tumor targeting effect of docetaxel(DTX),and further evaluate their anticancer effects in vitro. PBAE-DTX nanomicelles were prepared by film-hydration method with amphiphilic block copolymer polyethyleneglycol methoxy-polylactide(PELA) and pH sensitive triblock copolymer polyethyleneglycol methoxy-polylactide-poly-β-aminoester(PBAE) were used respectively to prepare PELA-DTX nanomicelles and PBAE-DTX nanomicelles. The nanomicelles were characterized by physicochemical properties and the activity of mice Lewis lung cancer cells was studied. The results of particle size measurement showed that the blank micelles and drug-loaded micelles had similar particle sizes, ranging from 10 to 100 nm. The particle size of PBAE micelles was changed under weak acidic conditions, with good pH response. The encapsulation efficiency of the above two types of DTX-loaded nanomicelles determined by HPLC was(93.8±1.70)% and(87.2±4.10)%, and the drug loading amount was(5.3±0.10)% and(4.9±0.05)%,respectively. Furthermore,the DTX micelles also showed significant inhibitory effects on Lewis lung cancer cells by MTT assay, and pH-sensitive PBAE-DTX showed better cytotoxicity. The results of flow cytometry indicated that,the apoptosis rate of lung cancer Lewis cells was(20.72±1.47)%,(29.71±2.38)%,and(40.91±1.90)%(P0.05) at 48 h after treatment in DTX,PELA-DTX,and PBAE-DTX groups. The results showed that different docetaxel preparations could promote the apoptosis of Lewis cells, and PBAE-DTX had stronger apoptotic-promoting effect. The pH-sensitive DTX-loaded micelles are promising candidates in developing stimuli triggered drug delivery systems in acidic tumor micro-environments with improved inhibitory effects of tumor growth on Lewis lung cancer.

Effect of small content of chromium (Cr) on wet–dry acid corrosion behavior of low alloy steels has been investigated. The results show that the corrosion resistance of the steels increased with increasing Cr content from 0.10 to 0.50 wt%. Higher content of Cr promotes initial corrosion and accelerates the formation of dense and protective rust in long-term corrosion. The enhanced protectiveness of the rust is closely related to its composition. High content of Cr increases the content of amorphous phases and decreases the content of γ-FeOOH in the rust, resulting in the high compactness of the rust and low electrochemical activity in acid condition. Cr dopes in rust and depresses the transformation from amorphous phases to α-FeOOH, as well as the growth process of FeOOH particles, which is responsible for the enhanced compactness of rust in long-term corrosion.

The corrosion behavior of corrosion resistant steel (CRS) in a simulated wet–dry acid humid environment was investigated and compared with carbon steel (CS) using corrosion loss, polarization curves, X-ray diffraction (XRD), scanning electron microscopy (SEM), electron probe micro-analysis (EPMA), N2 adsorption, and X-ray photoelectron spectroscopy (XPS). The results show that the corrosion kinetics of both steels were closely related to the composition and compactness of the rust, and the electrochemical properties of rusted steel. Small amounts of Cu, Cr, and Ni in CRS increased the amount of amorphous phases and decreased the content of γ-FeOOH in the rust, resulting in higher compactness and electrochemical stability of the CRS rust. The elements Cu, Cr, and Ni were uniformly distributed in the CRS rust and formed CuFeO2, Cu2O, CrOOH, NiFe2O4, and Ni2O3, which enhanced the corrosion resistance of CRS in the wet–dry acid humid environment.

Effects of W and Mo additions on wet-dry acid corrosion behavior of low-alloy steels under different O2 concentrations were investigated. The results showed that W and Mo-containing steels presented excellent wet-dry corrosion resistance under O2 concentrations of both 1 and 5%. The roles of W and Mo played in increasing corrosion resistance of the steels were different. W could improve the thermodynamic stability of the steel substrate, while Mo could promote the formation of protective rust. Interaction between W, Mo and O2 concentration greatly influenced wet-dry acid corrosion of low-alloy steels. W addition was more effective for depressing charge transfer process at the rust/substrate interface and presented higher enhanced effect on increasing corrosion resistance than Mo under O2 concentration of 1%. Mo was more effective on increasing rust compactness and showed higher enhanced effect on increasing corrosion resistance than W under O2 concentration of 5%.

Corrosion behavior of carbon steel in CO2 aqueous environment containing silty sand was investigated using corrosion mass loss method, scanning electron microscopy (SEM), energy diffraction spectrum (EDS), and various electrochemical measurements. The results show that the corrosion rate of carbon steel was obviously reduced due to the existence of silty sand. Silty sand promoted the rapid heterogeneous nucleation of corrosion product FeCO3 and simultaneously decreased its grains growth. Silty sand mixed with corrosion product to form the outer layer of corrosion scale with high compactness, blocking the transport of ferrous ions and leading to the formation of the inner layer of corrosion scale without silty sand. The existence of silty sand in the outer layer of corrosion scale inhibited anodic and cathodic currents.

Riparian buffer zone is important ecological transitional region between river and upland. Restoring the degraded vegetation system is important for preventing soil erosion, improving ecological environment and helping to achieve the sustainable development of ecosystems. Based on the scenario simulation of vegetation pattern and flow length index, we analyzed the responses of hydrological connectivity to vegetation pattern under different vegetation coverages and slope gradients, and explored the optimal vegetation pattern of soil and water conservation in riparian buffer zone in the lower reaches of the Yellow River. The results showed that the midslope-coarsness-clustered distribution of vegetation configuration, which exhibited the shortest flow length and the weakest hydrological connectivity, being the optimal vegetation pattern for controlling slope runoff generation and flow concentration. For the optimal vegetation pattern, its flow length increased with increasing slope length, namely, the longer slope length the more significant difference of hydrological connectivity between different slope gradients. Meanwhile, flow length of the optimal vegetation pattern decreased with increasing vegetation coverage. The differences between different slope gradients were obvious under low vegetation coverage, while it was unobvious on slope with vegetation coverage of 45%. Compared with the irregular variation trend of flow length on the actual vegetation slope, there was a consistent trend of first increase and then decrease on the simulated slope with the optimal vegetation pattern. Within the pre-set slope gradient range (5°-20°), the optimal vegetation pattern changed the variation of flow length between different slope gradients in the process of coverage change, which highlighted the influence of riparian buffer zone vegetation pattern on hydrological connectivity.河岸缓冲带作为河流-陆地之间重要的生态过渡区,恢复以及优化其退化的植被系统对防止水土流失、改善生态环境及实现该区域生态系统的可持续发展具有重要的现实意义.本文基于植被格局情景模拟和汇流路径长度指数,分析不同植被盖度和坡度下坡面水文连通性对植被格局的响应,探讨黄河下游河岸缓冲带水土保持效应的最优植被格局.结果表明: 坡中格局-粗粒度-集群分布的植被配置方式所产生的汇流路径长度最小、水文连通性最弱,是抑制坡面产流汇流效果最优的植被格局类型.对于最优植被格局,其汇流路径长度随坡长的增加而增加,坡长越长,坡度的作用越明显,水文连通性在各坡度之间的差异越显著;汇流路径长度随植被盖度增加而减小,低盖度时各坡度之间的汇流路径长度差异明显,当盖度达到45%时,各坡度之间的汇流路径长度趋于一致、水文连通性差异较小.实证坡面汇流路径长度随植被盖度增加其降低趋势无规律性,而最优植被格局汇流路径长度随植被盖度增加均呈现出一致的先急剧后平缓下降趋势.在设置的5°～20°坡度范围内,最优植被格局在一定程度上改变了盖度变化过程中不同坡度之间汇流路径长度的差异,突显了河岸缓冲带植被格局对水文连通性的影响.

The influence of Cr on the initial corrosion behavior of low-alloy steels exposed to a CO2–O2–H2S–SO2 wet–dry corrosion environment was investigated using weight-loss measurements, scanning electron microscopy, N2 adsorption tests, X-ray diffraction analysis, and electrochemical impedance spectroscopy. The results show that the corrosion rate increases with increasing Cr content in samples subjected to corrosion for 21 d. However, the rust grain size decreases, its specific surface area increases, and it becomes more compact and denser with increasing Cr content, which indicates the enhanced protectivity of the rust. The results of charge transfer resistance (R ct) calculations indicate that higher Cr contents can accelerate the corrosion during the first 7 d and promote the formation of the enhanced protective inner rust after 14 d; the formed protective inner rust is responsible for the greater corrosion resistance during long-term exposure.

The transmembrane transport of drug loaded micelles to intracellular compartment is quite crucial for efficient drug delivery. In the current study, we investigated the cellular internalization and anticancer activity of doxorubicin loaded micelles with folate modified stealthy PEOz corona. Folate-decorated micelles incorporating doxorubicin were characterized for particle size, degree of folate decoration, drug loading content and encapsulation efficiency, morphology, and surface charge. The targeting capability and cell viability were assessed using HeLa, KB, A549 and MCF-7/ADR cell lines. In vitro study clearly illustrated the folate receptor (FR) mediated targeting of FA modified micelles to FR-positive human HeLa, KB and MCF-7/ADR cells, while specific delivery to FR-negative A549 cells was not apparently increased at the same experimental conditions. Cytotoxicity assay showed 60% and 58% decrease in IC50 values for HeLa and KB cells, while only a slight decrease for A549 cells, following treatment with folate modified formulations. The enhanced intracellular delivery of FA modified micelles in MCF-7/ADR cells was also observed. In vivo antitumor tests revealed DOX entrapped FA-PEOz-PCL micelles effectively inhibited the tumor growth and reduced the toxicity to mice compared with free DOX. The current study showed that the targeted nano-vector improved cytotoxicity of DOX and suggested that this novel PEOz endowed stealthy micelle system held great promise in tumor targeted therapy.

Soil and vegetation are the foundation of maintaining riparian ecosystem services, and their spatial distribution and variations can determine the effects of ecological functions. In the present study, selecting the typical reach of the middle and lower reaches of the Yellow River as the study area, the spatial distributions of riparian soil physicochemical properties and their response to environmental factors were analyzed by employing methods of field investigation, experimental analysis, and redundancy analysis (RDA). The results showed that soil particle was composed significantly of silt in the study area, with the increase of riparian buffer distance, soil bulk density increased initially and then decreased, whereas soil moisture showed the opposite pattern. Changes in total soil phosphorus (TP), available phosphorus (AP), total carbon (TC), total organic carbon (TOC), total nitrogen (TN); ammonium nitrogen (NH₄⁺-N) and nitrate nitrogen (NO₃⁻-N) contents under different riparian buffer distance showed no statistically significant differences. The spatial distribution of soil chemical properties was generally insignificantly different through changes between two vegetation types. Pearson correlation analysis showed that there was close relationship between soil physical and chemical properties, therein, TOC content in the study area was positively and significantly related to TN (P0.01), NO₃⁻-N (P0.01, and NH₄⁺-N (P0.05) contents, respectively. Both the TN and TOC contents were significantly negatively related to sand content (P0.01), while was significantly positively related to clay content (P0.01), indicating that high sand content cou ld pormote poro9sity and permeability of soil and then accelerate the degradation rate of organic matters in soils. In addition, the results of RDA indicated that TOC and NH₄⁺-N contents increased with increasing the height and coverage of the tree layer. Soil TP and NO₃⁻-N contents increased with increasing the plant diameter at breast height (DBH) of the tree layer and coverage of the herb layer. Meanwhile, with the increase of elevation gradient, the content of soil NH₄⁺-N presented an increasing trend, indicating that soil properties were significantly influenced by the effects of community structure and elevation gradient in the study area.

In order to prolong the life of inner liner of coke can, the thermal fatigue property of Cr17Mn10Ni3 heat-resisting steel was analyzed and studied from cast metallurgical structure, the morphology of crack surface and cross-section, the injury factor by OM, SEM, photoshop and imagetool software. The results shows, Cr17Mn10Ni3 has a good thermal fatigue property because of the microstructure with good thermal conductivity, austenite matrix and break carbide lying in treelike crystals. It decreases the innerstress and postpones the time of crack formation and extension, during the process with 1100°C and room- temperature water cooling. The cracks mainly appear in the phase interfaces between carbides and matrix, ferrite and austenite, and grain boundaries. The thin and deep cracks with high concentration are beneficial to relax the elastic strain energy. But a single and thick crack easily widens and deepens to be detrimental to the thermal fatigue property.

Taking the surrounding areas of Xiaowan Reservoir in the middle reach of Lancangjiang River as study area, and based on the vegetation investigation at three sites including electricity transmission area (site 1), electricity-transfer substation and roadsides to the substation (site 2), and emigration area (site 3) in 1997 (before dam construction), another investigation was conducted on the vegetation composition, plant coverage, and dominant species at the same sites in 2010 (after dam construction), aimed to evaluate the ecological risk of the dam construction for the terrestrial plant species in middle reach of Lancangjiang River. There was an obvious difference in the summed dominance ratio of dominant species at the three sites before and after the dam construction. According the types of species (dominant and non-dominant species) and the changes of plant dominance, the ecological risk (ER) for the plant species was categorized into 0 to IV, i.e., no or extremely low ecological risk (0), low ecological risk (I), medium ecological risk (II), high ecological risk (III), and extremely high ecological risk (IV). As affected by the dam construction, the majority of the species were at ER III, and a few species were at ER IV. The percentage of the plant species at ER III and ER IV at site 3 was higher than that at sites 1 and 2. The decrease or loss of native plants and the increase of alien or invasive plants were the major ecological risks caused by the dam construction. Effective protection strategies should be adopted to mitigate the ecological risk of the dam construction for the terrestrial plants at species level.

Advancements in the design and synthesis of polymer-based nanoassemblies and nanoparticles, combined with achievements in nanotechnology and medicine, have resulted in remarkable applications of polymer nanosystems in the areas of nanomedicine and pharmaceutical sciences. However, a complete understanding of the absorption, distribution, metabolism, and elimination (ADME) processes of such polymer nanosystems in living systems has not been achieved. The influences of the pharmacokinetic parameters of polymer nanomaterials on the ADME processes are reviewed in this article, with discussions of the absorption and transportation of polymer nanoparticles across biological barriers, the factors affecting the bodily distribution of polymer nanocarriers, the transformation of polymer nanomaterials in vivo, the elimination pathway of polymer nanoparticles from biological systems, and perspectives of future pharmacokinetics and safety investigations of polymer-based nanoassemblies. A full and better understanding of the pharmacokinetic parameters of polymer-based nanomaterials is of vital importance in developing polymer nanosystems with optimal pharmacokinetics and biological safety for applications in nanomedicine and the pharmaceutical industry.

The traditional hardware description languages (VHDL and Verilog) is not suitable for system-level modeling and Hardware Software Codesign, while the SystemC language is more suitable than the traditional HDL language for system-level modeling. This paper describes the packet processing engine(PPE) characteristics of XDNP network processor, analyze the advantage of system-level modeling in SystemC language, and use the SystemC language for the system-level modeling of the packet processing engine. In addition an independent simulation model is built, and the performance of packet processing engine is analyzed and verificated. Compared with the traditional hardware description language model we can obtain about 1.5 times simulation speed as much as that of HDL model.

This paper present a parallel, split bus interconnection scheme for the multi-processor system. The scheme provides a command bus and a set of data bus, each of which works independently. This bus interconnect scheme can greatly improve the bandwidth of data communication within the multi-processor system because of its characteristics of concurrency and separability.