Potential galactosyltransferase inhibitors were synthesized by replacing the diphosphate moiety in sugar donor with a basic amino acid. Analogues containing tryptophan and histidine showed moderate ...inhibition against mycobacterial GlfT2, which we suggest may arise by mimicking the interaction between the diphosphate metal ion complex with the carboxylate residues present in the active site of the enzyme.
Sugar–amino acid–nucleosides (SAAN) were synthesized to mimic glycosyl nucleotide donors based on the hypothesis that a basic amino acid may interact with carboxylate groups of the enzyme in a manner similar to the diphosphate metal ion complex. C-Glycoside analogues of the d-galactopyranose or l-arabinofuranose ring systems, and four amino acids (lysine, glutamine, tryptophan, and histidine), were chosen for this study. The targets were synthesized and tested against GlfT2, a galactofuranosyltransferase essential for cell wall galactan biosynthesis in Mycobacterium tuberculosis. The inhibition assay showed that analogues containing histidine and tryptophan are moderate inhibitors of GlfT2.
Discriminative correlation filters (DCF) with deep convolutional features have achieved favorable performance in recent tracking benchmarks. However, most of existing DCF trackers only consider ...appearance features of current frame, and hardly benefit from motion and inter-frame information. The lack of temporal information degrades the tracking performance during challenges such as partial occlusion and deformation. In this paper, we propose the FlowTrack, which focuses on making use of the rich flow information in consecutive frames to improve the feature representation and the tracking accuracy. The FlowTrack formulates individual components, including optical flow estimation, feature extraction, aggregation and correlation filters tracking as special layers in network. To the best of our knowledge, this is the first work to jointly train flow and tracking task in deep learning framework. Then the historical feature maps at predefined intervals are warped and aggregated with current ones by the guiding of flow. For adaptive aggregation, we propose a novel spatial-temporal attention mechanism. In experiments, the proposed method achieves leading performance on OTB2013, OTB2015, VOT2015 and VOT2016.
Organ protection is a routine therapy in severe injuries. Our aim was to evaluate the beneficial effects of ulinastatin in experimental rats. Rats were randomly divided into a sham control, a model ...control and an ulinastatin-treated group. Malondialdehyde (MDA) and superoxide dismutase (SOD) levels were determined. Serum amylase, serum aspartate aminotransaminase (AST), lactate dehydrogenase (LDH) and creatine kinase isoenzyme (CKMD) activities, interleukin-8 (IL-8), tumor necrosis factor-α (TNF-α), nitric oxide (NO) and cardiac troponin I (nTnl) levels were examined. Results showed that ulinastatin decreased MDA levels and ameliorated the down-regulation of SOD activity. In addition, ulinastatin pretreatment may decrease serum AST, LDH and CKMD activities, IL-8, TNF-α, and nTnl levels, and enhance NO level. Our results demonstrated that oxidative injury occurred after IR and that ulinastatin exhibits significant protective effects against these effects.
•The effects of abnormal arrivals were eliminated successfully using the analytical localization method.•The temporal and spatial errors caused by premeasured wave velocity were weakened efficiently ...with TD.•An effective collaborative localization method for MS/AE was proposed using analytical and TD methods.•The proposed CLMAI is a beneficial complement for the current localization methods of MS/AE.•The CLMAI is applicable to MS localization in the rockmass structure of dynamic underground mining.
The localization of microseismic sources/acoustic emission in the rockmass structure can provide the basis for determining the potential areas of rockmass instability and rockburst in the underground mining. As the construction environment in deep mining is complex, the abnormal arrivals with different scales of errors may be recorded by the monitoring sensors, which can lead to large errors between the located results and the authentic coordinates. In addition, the average premeasured P-wave velocity through blasting tests (blasts) is widely used in the current localization methods, which are unsuitable for the mining environment with dynamic change of wave velocity in multi-level and multi-stope. To eliminate the effects of abnormal arrivals, the analytical localization method is used to remove abnormal arrivals since it has a stable solution with the high precision when the input data are accurate. To weaken errors induced by the dynamic wave velocity, the iterative solution without the need of premeasured P-wave velocity is used to improve the locating accuracy since it can optimize results using the advantage of multiple sensors. Therefore, a collaborative localization method using analytical and iterative solutions (CLMAI) was proposed, which combined with the arrivals of multi-sensor and inversion of the real-time average wave velocity, to seek the optimal locating results. Firstly, the analytical solutions using 6 sensors in unknown velocity system were resolved. The method to remove abnormal arrivals is developed by solving the logistic probability density function for the analytical solutions of different sensors combinations. Then, the iterative localization method based on the time differences was used to locate source coordinates with clear arrivals. Finally, the CLMAI is verified through locating coordinates of blasts and microseismic events (events) in Kaiyang phosphorous mine. Results show that the CLMAI can not only filter the abnormal arrivals by making use of the characteristic of analytical solutions, but also use the iterative method without premeasured average velocity to improve the locating accuracy significantly. The proposed method is a beneficial complement for the current iterative methods using premeasured velocity, which is applicable to microseismic sources localization under complex abnormal arrivals in the rockmass structure of dynamic underground mining.
High-frequency sensors can monitor water quality with high temporal resolution and without environmental influence. However, sensors for detecting key water quality parameters, such as total ...nitrogen(TN), total phosphorus(TP), and other water environmental parameters, are either not yet available or have attracted limited usage. By using a large number of high-frequency sensor and manual monitoring data, this study establishes regression equations that measure high-frequency sensor and key water quality parameters through multiple regression analysis. Results show that a high-frequency sensor can quickly and accurately estimate dynamic key water quality parameters by evaluating seven water quality parameters. An evaluation of the flux of four chemical parameters further proves that the multi-parameter sensor can efficiently estimate the key water quality parameters. However, due to the different optical properties and ecological bases of these parameters, the high-frequency sensor shows a better prediction performance for chemical parameters than for physical and biological parameters. Nevertheless, these results indicate that combining high-frequency sensor monitoring with regression equations can provide real-time and accurate water quality information that can meet the needs in water environment management and realize early warning functions.
Abstract
Livestock on the Qinghai-Tibetan Plateau are faced with extreme harsh winters and are often in negative energy balance during this period. Dietary supplementation can improve growth ...performance of Tibetan sheep and, consequently, we hypothesized that it would also increase microbial abundance and rumen epithelium development. To test this hypothesis, we examined the effect of feed supplementation during the cold season on rumen microbes, fermentation, epithelium development, and absorptive capability in Tibetan sheep. Eighteen 1-yr-old ewes (BW = 29.4 ± 1.79, kg) were offered oat hay ad libitum for 60 d and divided randomly into three groups: 1) no supplement; control group (CON); 2) urea-molasses lick block supplement (BS); and 3) concentrate feed supplement (CS). The ADG of CS ewes (143.3, g/d) was greater (P < 0.05) than BS ewes (87.9, g/d), which was greater (P < 0.05) than CON ewes (44.5, g/d). Serum concentrations of GH, IGF-1, and IGF-2 in the CS and BS groups were greater than in the CON group (P < 0.05). Greater relative abundance of protozoa, Ruminococcus albus, Fibrobacter succinogenes, Streptococcus bovis, and Ruminobacter amylophilus was observed in the CS and BS groups than in the CON group (P < 0.05), and relative abundances of rumen fungi, Butyrivibrio fibrisolvens, and Prevotella ruminicola in the CS group were greater than in the BS and CON groups (P < 0.05). Ruminal total VFA, ammonia, and microbial protein concentrations in the CS and BS groups were greater than in the CON group (P < 0.05), and in the CS group were greater than in the BS group (P < 0.05). Ruminal papillae width and surface area in the CS and BS groups were greater than in the CON group (P < 0.05), while in the CS group were greater than in the BS group (P < 0.05). The mRNA expressions of IGFBP5, NHE1 (sodium/hydrogen antiporter, isoform 1), DRA (downregulated in adenoma), and Na+/K+-ATPase (sodium/potassium ATPase pump) in ruminal epithelium were greater in the CS and BS groups than in the CON group (P < 0.05), and in the CS group was greater than in the BS group (P < 0.05), while NHE3 (sodium/hydrogen antiporter, isoform 3), MCT1 (monocarboxylate transporter 1), and MCT4 (monocarboxylate transporter 4) mRNA expressions in the CS group were greater than in the BS and CON groups (P < 0.05). It was concluded that supplementing Tibetan sheep during the cold season increases rumen microbial abundance and improves fermentation parameters, rumen epithelium development, and absorptive capability.
With the rapid development of the Internet, the exponential growth of information resources makes it harder for users to retrieve information that is useful to themselves. But the advent of ...personalized recommendation systems has brought the hope and help to users. This paper introduces the background and meaning of the original Slope One static algorithm and the current researches. It thoroughly explores the improvement of Slope One algorithm at home and abroad, and clarifies the advantages and disadvantages of the algorithm. Based on the original Slope One static algorithm, an incremental Slope One algorithm is proposed. The advantage of incremental algorithm is that it can adapt to the instantaneous changes of data. Combined with the easy implementation, easy expansion and high accuracy of Slope One, Slope One incremental algorithm has good practicability.
Chronic myelogenous leukemia (CML) is characterized by the t(9;22) (q34;q11)-associated
fusion gene, which is an essential element of clinical diagnosis. As a traditional Chinese medicine, realgar ...has been widely used for the treatment of various diseases for >1,500 years. Inspired by nano-drug, realgar nanoparticles (NPs) have been prepared with an average particle size of <100 nm in a previous work. Compared with coarse realgar, the realgar NPs have higher bioavailability. As a principal constituent protein of caveolae, caveolin-1 (Cav-1) participates in regulating various cellular physiological and pathological processes including tumorigenesis and tumor development. In previous studies, it was found that realgar NPs can inhibit several types of tumor cell proliferation. However, the therapeutic effect of realgar NPs on CML has not been fully elucidated. In the present paper, it was demonstrated that realgar NPs can inhibit the proliferation of K562 cells and degrade Bcr-Abl fusion protein effectively. Both apoptosis and autophagy were activated in a dose-dependent manner in realgar NPs treated cells, and the induction of autophagy was associated with class I phosphoinositide 3-kinase/protein kinase B/mammalian target of rapamycin pathway. Morphological analysis indicated that realgar NPs induced differentiation effectively in CML cells. Furthermore, it was identified that Cav-1 might play a crucial role in realgar NP therapy. In order to study the effects of Cav-1 on K562 cells during realgar NP treatment, a Cav-1 overexpression cell model was established by using transient transfection. The results indicated that Cav-1 overexpression inhibited K562 cell proliferation, promoted endogenic autophagy, and increased the sensitivity of K562 cells to realgar NPs. Therefore, the results demonstrated that realgar NPs degraded Bcr-Abl oncoprotein, while the underlying mechanism might be related to apoptosis and autophagy, and Cav-1 might be considered as a potential target for clinical comprehensive therapy of CML.
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