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Accurate knowledge of the distribution characteristics of structural planes in rocks is beneficial in the evaluation of rock mass quality and roadway support decision-making. In this study, in situ monitoring results were used to analyse the deformations and failure characteristics of the rock surrounding the main haulage roadway in the Huahong coal mine to establish a deformation and failure model for the surrounding rock affected by mining. According to an analytic hierarchy process, a comprehensive evaluation index for the degree of fracturing in the rock surrounding the coal seam roadways was proposed. Additionally, a classification method based on the comprehensive widths of the structural planes (CWSPs) inside the complete rock mass was proposed to determine the quality of the surrounding rock. The structures of the rocks surrounding the main haulage roadway in the mine before and after coal mining were observed in situ at monitoring station no. 22. Borehole imaging technology was used to classify the surrounding rock quality using the CWSP-based evaluation method. The results indicated that the roof rock was mildly affected by mining; the corner rock had a large degree of fracturing in the central part of the borehole and a small degree of fracturing at both ends; the rib rock was highly fractured. These evaluation results were consistent with the macroscopic characteristics of the surrounding rocks, indicating the reliability of the deformation and failure model for characterizing the surrounding rocks affected by mining.

BACKGROUND Acute pancreatitis is an inflammatory disease of the pancreas associated with high patient morbidity. Lycium barbarum polysaccharide (LBP), a traditional Chinese medicine with an active component extracted from the goji berry, has previously been reported to have anti-inflammatory effects. This study aimed to investigate the effects of LBP in a mouse model of cerulein-induced acute pancreatitis. MATERIAL AND METHODS Acute pancreatitis was induced by intraperitoneal injection of cerulein in C57BL/6 wild-type mice or nuclear factor erythroid-2-related factor 2 (NRF2) gene knockout mice. LBP or normal saline was administrated by gavage once daily for one week before the induction of acute pancreatitis. At 12 hours after the first intraperitoneal injection of cerulein, the mice were euthanized. Blood and pancreatic tissue were sampled for histology and for the measurement of pro-inflammatory cytokines, serum amylase, and lipase. RESULTS In the untreated mouse model of cerulein-induced acute pancreatitis, amylase and lipase levels were increased, and these levels were reduced by LBP treatment when compared with vehicle treatment. In the untreated mouse model, histology of the pancreas showed edema and inflammation, which were reduced in the LBP-treated mice. In the untreated mouse model, increased levels of tumor necrosis factor-alpha (TNF-alpha) and interleukin-6 (IL-6) were found, which were reduced in the LBP-treated mice. NRF2 gene knockout mice with cerulein-induced acute pancreatitis showed reduced anti-inflammatory effects of LBP treatment. LBP increased the expression of NRF2 and heme oxygenase-1 (HO-1). CONCLUSIONS In a mouse model of cerulein-induced acute pancreatitis, LBP reduced inflammation by upregulating NRF2 and HO-1.

High power supercontinuum (SC) is generated by focusing 800 nm and 400 nm femtosecond laser pulses in fused silica with a microlens array. It is found that the spectrum of the SC is getting broader compared with the case of a single laser pulse, and the spectral energy density between the two fundamental laser wavelengths is getting significantly higher by optimizing the phase matching angle of the BBO. It exceeds μJ/nm over 490 nm range which is from 380 nm to 870 nm, overcoming the disadvantage of relative lower power in the ranges far from the fundamental wavelength.

In this paper, we introduce a new human action recognition framework which consists of feature extract, feature coding, network tuning, and action recognition. Spatial–temporal combined features are designed to represent human actions in both space and time, a method which results in higher accuracy than when individual spatial or temporal features are used. A new layer is added to the Deep Belief Network (DBN), which is used to unify the length of the spatial–temporal features. In the training stage, we suggest some improved methods, including model initialization and a fine-tuning of the DBN’s parameters. We evaluate our framework using the MSR-Action 3D public datasets. Our experiments indicate that spatial–temporal features can achieve an accuracy of 93.4%, an improvement of 1.09% and 11.71% when compared with the uncombined temporal and spatial features, respectively.

It is significant for maintaining public safety to find abnormal behavior among crowd in time and exactly. However, traditional deep learning algorithms still have difficulties to be solved in terms of group abnormal behavior detection, mainly including two aspects. On the one hand, there is a large amount of background redundancy in the monitoring video data, which leads to longer training time and negative effects of the detection accuracy. On the other hand, the abnormal samples in the monitoring video data are relatively low, which will cause the model to generate a higher false alarm rate. Aiming at the above problems, this paper proposes a crowd abnormal behavior detection method based on long short-term memory network (LSTM). First, an improved ViBe image foreground extraction method is proposed to reduce the negative impact of irrelevant background on abnormal behavior detection. Then, use the improved LSTM algorithm of the focal loss function to detect abnormal behavior of the crowd and increase the attention of the LSTM algorithm to abnormal samples, thereby improving the detection accuracy. Finally, the validity of the model is verified on the UMN dataset. Experiments show that the method in this paper can get good results even when the data samples are unbalanced, and the AUC on the UMN datasets reaches 99.83%.

F16 is a mitochondria-targeted, broad-spectrum anticancer agent in the pre-clinic cancer therapy. Here we developed two fluorescent isomers of F16 (o-F16 and m-F16) with entirely different photophysical properties, uncoupling activity, and cytotoxicity by merely modifying the linking orientation of pyridinium and indole units. Individually, o-F16 acted as a strong uncoupler to reduce the mitochondrial respiration efficiency, while m-F16 could hardly uncouple the mitochondrial respiration due to its poor proton dissociation capability. Owing to their intrinsic fluorescence, o-F16 and m-F16 could specifically image mitochondria in the green and red channel, respectively. This work could provide useful information for the development of uncouplers and design of mitochondrial-targeted drugs.

A green Passerini three-component reaction of 2-(4-oxo-4,5,6,7-tetrahydro-1 H -indol-1-yl)acetic acid with alkyl or aryl isocyanides and aldehydes was reported under aqueous conditions at 35 °C for 1 h, and 21 indolone- N -amino acid derivatives were prepared in high yields of 42%–99%. Their structures were characterized by IR, ESI–MS, NMR and elemental analysis, and the possible mechanisms have been also proposed. The highly efficient and eco-friendly method provides a facile access to a library of indolone- N -amino acid derivatives for future research on bioactivity screening.

Protein tyrosine phosphatase 1B (PTP1B) is a key negative regulator of insulin signaling pathway, and more and more studies have shown that it is a potential target for the treatment of type 2 diabetes mellitus (T2DM). In this study, 17 new 4-thiazolinone derivatives were designed and synthesized as novel PTP1B inhibitors, and ADMET prediction confirmed that these compounds were to be drug-like. In vitro enzyme activity experiments were performed on these compounds, and it was found that a plurality of compounds had good inhibitory activity and high selectivity against PTP1B protein. Among them, compound 7p exhibited the best inhibitory activity with an IC50 of 0.92 μM. The binding mode of compound 7p and PTP1B protein was explored, revealing the reason for its high efficiency. In addition, molecular dynamics simulations for the PTP1BWT and PTP1Bcomp#7p systems revealed the effects of compound 7p on PTP1B protein at the molecular level. In summary, the study reported for the first time that 4-thiazolinone derivatives as a novel PTP1B inhibitor had good inhibitory activity and selectivity for the treatment of T2DM, providing more options for the development of PTP1B inhibitors. AbbreviationsBBBblood-brain barrierCDC25Bcell division cycle 25 homolog BCYP2D6Cytochrome P450 2D6 bindingDCCMdynamic cross-correlation mapDSDiscovery StudioH bondhydrogen bondHIAhuman intestinal absorptionLARleukocyte antigen-related phosphataseMDmolecular dynamicsMEG-2maternal-effect germ-cell defective 2MM-PBSAmolecular mechanics Poisson Boltzmann surface area)PCAprincipal component analysisPDBProtein Data BankpNPPp–nitrophenyl phosphatePPBplasma protein bindingPTP1Bprotein tyrosine phosphotase 1BRMSDroot mean square deviationRMSFroot mean square fluctuationSHP-1src homologous phosphatase-1SHP-2src homologous phosphatase-2SPCsingle-point chargeTCPTPT cell protein tyrosine phosphataseT2DMType 2 diabetes mellitusVDWvan der Waals blood-brain barrier cell division cycle 25 homolog B Cytochrome P450 2D6 binding dynamic cross-correlation map Discovery Studio hydrogen bond human intestinal absorption leukocyte antigen-related phosphatase molecular dynamics maternal-effect germ-cell defective 2 molecular mechanics Poisson Boltzmann surface area) principal component analysis Protein Data Bank p–nitrophenyl phosphate plasma protein binding protein tyrosine phosphotase 1B root mean square deviation root mean square fluctuation src homologous phosphatase-1 src homologous phosphatase-2 single-point charge T cell protein tyrosine phosphatase Type 2 diabetes mellitus van der Waals Communicated by Ramaswamy H. Sarma

Underground coal mining inevitably results in land surface subsidence. Acquiring information on land surface subsidence is important in the detection of surface change. However, conventional data acquisition techniques cannot always retrieve information on whole subsidence area. This study focuses on the reconstruction of a digital elevation model (DEM) with terrestrial laser scanning (TLS) point cloud data. Firstly, the methodology of the DEM with terrestrial 3-dimensional laser scanning is introduced. Then, a DEM modeling approach that involves the application of curved non-uniform rational B-splines (NURBS) surface is put forward. Finally, the performance of the DEM modeling approach with different surface inverse methods is demonstrated. The results indicate that the DEM based on the point cloud data and curved NURBS surface can achieve satisfactory accuracy. In addition, the performance of the hyperbolic paraboloid appears to be better than that of the elliptic paraboloid. The reconstructed DEM is continuous and can easily be integrated into other programs. Such features are of great importance in monitoring dynamic ground surface subsidence.

In this paper analysed the forms of heavy metals (Zn Pb Cd and As) of the Smelting Slag for Lead and Zinc,using BCR sequential extraction. Different chemical morphological of heavy metals have different activity and harmfulness. Migration and Utilization of heavy metals were decided by the existent form of heavy metals in the soil,which influenced Bioactivity and Toxicity. The results show that the main forms of Zn and Cd are Oxidizable and Residual fraction, and Pb mainly occurred in Oxidizable and Reducible fraction. however, As mainly occurred in Residual fraction, which the percentage of reachs 99.56%. According to the percentage of fractions extracted in total content (As is 0.44%, Zn is 14.7%, Pb is 85.98%, Cd is 48.86%),the latent ecological risk of heavy metals varied in the descending order of,Pb Cd Zn and As.

According to the effect of vibration on stabilization performance of on-board sighting telescope, a performance test analysis method is built based on the image of sighting telescope. The article mainly studies key algorithms of image pretreatment, median filtering and template matching in the process of image processing. The result indicates that vibration has significant impact on the stabilization performance of sighting telescope, especially for continuous aiming accuracy of different target. This research provides reference for the test and evaluation for the precision of vehicle-mounted sighting telescope stabilization.

α-tocopheryl succinate (α-TOS), a redox-inactive vitamin E analogue, holds great promise for selectively triggering mitochondrial apoptosis in tumor cells. In this paper, in order to better understand the biophysical basis of α-TOS under biological conditions, the effects of α-TOS at high concentrations on the function of mitochondria and its interactions with human blood protein (human serum albumin, HSA) were investigated. We found that α-TOS with high concentration not only caused inhibition of mitochondrial respiration and mitochondrial permeability transition (MPT), but also strongly disturbed the mitochondrial membrane and ultrastructure. These results suggest that mitochondria are organelles that are very sensitive to α-TOS-induced stress, and the mechanism of damage to mitochondria may be due to MPT and impairing of the respiratory chain. In addition, it has been also demonstrated that α-TOS possesses moderate binding affinity to HSA in site I due to the formation of the α-TOS–HSA complex by hydrophobic, van der Waals and hydrogen bond forces. These results will help us learn more about biophysical properties of α-TOS at subcellular (mitochondria) and biomacromolecular (HSA) levels.

Heavy metal (HM) tolerance, effects on maize growth, heavy metal absorption and accumulation by endophytic Peyronellaea from HM-contaminated and uncontaminated sites were studied to evaluate the hypothesis that endophytes from HM-contaminated sites would enhance HM-tolerance in hosts. Although we found that certain endophytes improved tolerance of plants to heavy metals, isolates from the HM-contaminated site were not more tolerant to heavy metals than those from the uncontaminated site. Pot experiments indicated that growth and heavy metal absorption and accumulation by host plants in HM-polluted environments could be affected by inoculation with HM-tolerant endophytic fungi, and isolates showed a high intraspecific variability. However, there was no significant difference in growth between the maize inoculated with the endophytes from the HM-contaminated site and uncontaminated site under lead stress. Similarly, the HM content in the shoots and roots of maize inoculated with the isolates from the HM-contaminated site was not always higher than that in maize inoculated with endophytes from the uncontaminated site. Therefore, based on our experiments it is suggested that HM-tolerance due to endophytes and their effects on host plant growth and heavy metal absorption and accumulation were not correlated with origin of the endophytes.

Corrugated-core sandwich panel, which can combine thermal insulation and bearing function, has been used in the design process of integrated thermal protection system (ITPS). This paper focuses on the heat transfer properties of Corrugated-core sandwich panel during the re-entry process under uncertain environment. The uncertainties come from material properties, geometric dimensions and thermal load environment. Interval variables are introduced to describe these uncertainties due to often only small sample information being obtained from experiment and measurement. Based on the non-probabilistic set theory, we use two interval analysis methods named interval analysis methods based on Taylor expansion and collocation interval analysis methods based on Chebyshev polynomial to observe the propagation of uncertainty in the heat transfer analysis. The results show that the existence of uncertainties has obvious effect for heat transfer analysis results. The safety of ITPS will be improved when consider the heat transfer analysis under uncertain environment.

The feasibility of simultaneous vanadium extraction and phosphorus removal from vanadium-containing hot metal was demonstrated with laboratory experimental investigation. The effect of CaO addition on the distribution behavior of vanadium, phosphorus between basic vanadium slag and semi-steel as well as the influence of basicity on the leaching behavior of vanadium, phosphorus was particularly studied. Results show that vanadium oxidation ratio slightly decreases with the increase of basicity, but phosphorus oxidation ratio rapidly increases with the increase of basicity. The leaching of roasted vanadium slag with various CaO contents indicated that the optimal slag basicity for extracting vanadium was 1.5. The maximum leaching efficiency of vanadium could reach 84.02% and the sequence of vanadium leaching efficiency by using different leaching reagents was: 160 g/L Na2CO3 > 100 g/L NaHCO3 > 400 g/L (NH4)2CO3 > 5% H2SO4.

In this paper, aiming at the trans-membrane transport properties of the different DLCs related with the cytotoxicities, we have studied photophysics of DLCs in RMs. MTT assays indicated that DLC 1 were more cytotoxic than DLC 2 and 3. Steady-state absorption and fluorescence method have been used to characterize the binding model of three DLCs (1, 2, and 3) in RMs and bovine serum albumin (BSA). The progressive red-shift of compound 1 indicated that it can experience the hydrophilic and hydrophobic environment owing to the rigid structure, thus it can more easily cross the double membrane of cell than compounds 2 and 3. In conclusion, we simulated a model of compound 1 in RMs. The present study of F16 derivatives in microenvironment would provide some useful information to the cell membrane simulation and design of DLCs.

A green Passerini three-component reaction of 2-(4-oxo-4,5,6,7-tetrahydro-1 H -indol-1-yl)acetic acid with alkyl or aryl isocyanides and aldehydes was reported under aqueous conditions at 35 °C for 1 h, and 21 indolone- N -amino acid derivatives were prepared in high yields of 42%–99%. Their structures were characterized by IR, ESI–MS, NMR and elemental analysis, and the possible mechanisms have been also proposed. The highly efficient and eco-friendly method provides a facile access to a library of indolone- N -amino acid derivatives for future research on bioactivity screening.

In order to study how the parameters of floating slab track and the speed of the train influence the vehicle-track coupling system，the paper built the vehicle-track coupling dynamic system. In the coupling model, the train is simplified a multi-rigid body system. The rail and the floating slab are considered as Euler beam. The wheel-rail relation is regarded as non-linear Hertz contact. The paper solved the dynamic equation of the vehicle-track coupling dynamic system with prediction-correction Newmark-β numerical integration method. Through numerical simulation, the paper gained the affect of fastener stiffness, slab support stiffness, and the speed of train to the characteristic of the coupling system containing the vehicle acceleration, wheel-rail force, the vibration of the track and the counter-force from the basis. The paper provides a reference for the selection of the track parameters and the speed of vehicle.

5-Fluorouracil (5-FU) has been widely used as a chemotherapy agent in the treatment of many types of solid tumors. Investigation of its antimetabolites led to the development of an entire class of fluorinated pyrimidines. However, the toxicity profile associated with 5-FU is significant and includes diarrhea, mucositis, hand-foot syndrome and myelosuppression. In aiming at reducing of the side effects of 5-FU, we have designed and synthesized delocalized lipophilic cations (DLCs) as a vehicle for the delivery of 5-FU. DLCs accumulate selectively in the mitochondria of cancer cells because of the high mitochondrial transmembrane potential (ΔΨm). Many DLCs exhibited anti-cancer efficacy and were explored as potential anti-cancer drugs based on their selective accumulation in the mitochondria of cancer cells. F16, the DLC we used as a vehicle, is a small molecule that selectively inhibits tumor cell growth and dissipates mitochondrial membrane potential. The binding of the conjugate F16-5-FU to bovine serum albumin (BSA) was investigated using spectroscopic and molecular modeling approaches. Fluorescence quenching constants were determined using the Stern-Volmer equation to provide a measure of the binding affinity between F16-5-FU and BSA. The activation energy of the interaction between F16-5-FU and BSA was calculated and the unusually high value was discussed in terms of the special structural block indicated by the molecular modeling approach. Molecular modeling showed that F16-5-FU binds to human serum albumin in site II, which is consistent with the results of site-competitive replacement experiments. It is suggested that hydrophobic and polar forces played important roles in the binding reaction, in accordance with the results of thermodynamic experiments.

This paper investigates the interactions between human serum albumin (HSA) and CdTe quantum dots (QDs) with nearly identical hydrodynamic size, but capped with four different ligands (MPA, NAC, and GSH are negatively charged; CA is positively charged) under physiological conditions. The investigation was carried out using fluorescence spectroscopy, circular dichroism (CD) spectra, UV–vis spectroscopy, and dynamic light scattering (DLS). The results of fluorescence quenching and UV–vis absorption spectra experiments indicated the formation of the complex of HSA and negatively charged QDs (MPA-CdTe, NAC-CdTe, and GSH-CdTe), which was also reconfirmed by the increasing of the hydrodynamic radius of QDs. The K a values of the three negatively charged QDs are of the same order of magnitude, indicating that the interactions are related to the nanoparticle itself rather than the ligands. Δ H S > 0 implied that the electrostatic interactions play predominant roles in the adsorption process. Furthermore, it was also proven that QDs can induce the conformational changes of HSA from the CD spectra and the three-dimensional fluorescence spectra of HSA. However, our results demonstrate that the interaction mechanism between the positively charged QDs (CA-CdTe) and HSA is significantly different from negatively charged QDs. For CA-CdTe QDs, both the static and dynamic quenching occur within the investigated range of concentrations. According to the DLS results, some large-size agglomeration also emerged.