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In this paper, we propose a novel stereoscopic image quality assessment (SIQA) method by learning non-negative matrix factorization (NMF)-based color visual characteristics for monocular perception and considering binocular interactions. In training phase, a feature basis matrix is learned based on NMF by considering color information and a feature detector is designed by performing Schmidt orthogonalization on the feature basis matrix. In construction of SIQA phase, for monocular perception, visual saliency regions are selected and parts-based feature similarity indexes of left and right views based on the feature vectors extracted by the feature detector are calculated. For binocular interactions, we calculate cyclopean feature similarity index by considering binocular fusion and rivalry. Finally, support vector regression is used to simulate nonlinear relationship between monocular perception and binocular interactions. Experimental results on LIVE 3D image databases and NBU 3D IQA database demonstrate that the proposed SIQA method is more consistent with human perception. [ABSTRACT FROM AUTHOR]

Researches have demonstrated that trans-fatty acids are related to the progression of atherosclerosis, but the underlying mechanism is not clear till now. In the presented study, two-dimensional electrophoresis based proteomics was used to discover the role of elaidic acid in atherosclerosis. In human umbilical vein endothelial cells (HUVEC), twenty-two and twenty-three differentially expressed proteins were identified in low (50 μmol/L) and high (400 μmol/L) concentration elaidic acid simulated groups, respectively, comparing with the control group. The expressions of some selected proteins (PSME3, XRCC5, GSTP1, and GSTO1) were validated by qRT-PCR analysis. Western blotting analysis further confirmed that elaidic acid downregulated the expression of PSME3 and XRCC5. Moreover, P53, the downstream protein of PSME3, was further investigated. Results demonstrated that a variety of proteins, many of which were related to oxidative stress, apoptosis, and DNA damage, were involved in the elaidic acid induced atherosclerosis. Furthermore, P53 was demonstrated to regulate the atherosclerosis through cell cycle arrest and apoptosis pathway. [ABSTRACT FROM AUTHOR]

Health literacy (HL) has become an important public health issue and is receiving growing attention. However, the HL levels of military college students in China have never been analyzed. This study aimed to investigate the HL and related associate factors in military college students in Chongqing, China. Data was obtained with the “Chinese Citizen Health Literacy Questionnaire (2012 edition)” from 3183 military college students aged 16–28 years at Chongqing in December 2015. A total score of ≥80 points determined adequate HL, and HL level was defined as the proportion of students who had adequate HL out of the total number of participants. Multiple logistic regression analysis with a stepwise forward likelihood ratio (LR) method was used to determine the effects of sociodemographic characteristics, health-related behaviors, and family-related factors on HL level. The mean score of HL was 68.56, and the HL level of military college students was 21.05%; the overall knowledge rate was 71.33%. The independent factors that were associated with HL level were years in college, educational system, time playing online games, annual household income and father's education level. Senior (odds ratio [OR] = 1.229, 95% confidence interval [CI] 1.018∼1.484), undergraduate (OR = 1.509, 95% CI 1.151∼1.978), time played games more than 5 hours each week (OR = 0.638, 95% CI 0.486∼0.837), annual household incomes more than 50,000 yuan (OR = 1.231, 95% CI 1.027∼1.476) and father's education level (high school: OR = 2.327, 95% CI 1.186∼4.565; university: OR = 2.450, 95% CI 1.244∼4.825), were independently associated with higher HL level. HL levels of military college students in Chongqing need to be improved across the board. Our data suggests that special emphasis should be placed on students in junior and those in the specialist educational system. School departments may also benefit from incorporating health literacy into their curricula and helping students manage the time they spend playing online games. [ABSTRACT FROM AUTHOR]

New chemotherapeutic compounds and regimens are needed to combat multidrug-resistant Mycobacterium tuberculosis . Here, we used a series of murine models to assess an antitubercular lead compound SKLB-TB1001. In the Mycobacterium bovis bacillus Calmette-Guérin and the acute M. tuberculosis H37Rv infection mouse models, SKLB-TB1001 significantly attenuated the mycobacterial load in lungs and spleens. The colony forming unit counts and histological examination of lungs from H37Rv infected mice revealed that the benzothiazinethione analogue SKLB-TB1001 as a higher dose level was as effective as isoniazid. Moreover, in a multidrug-resistant (MDR)-TB mouse model, SKLB-TB1001 showed significant activity in a dose-dependent manner and was more effective than streptomycin. These results suggested that SKLB-TB1001 could be an antitubercular drug candidate worth further investigation. [ABSTRACT FROM AUTHOR]

The perceived quality assessment of three-dimensional (3D) images has emerged as a challenging research topic in the field of 3D imaging in recent years. Especially, blind quality assessment of 3D images encounters challenges due to prior information about the original 3D images is not available. In this paper, we propose a blind 3D image quality assessment (IQA) metric that utilizes the self-similarity of binocular features. The primary contribution of this study is that the proposed metric considers the binocular visual property and the local visual structural property for blind 3D-IQA. We calculate the self-similarity of binocular rivalry response as well as binocular orientation selectivity in the distorted 3D image. We then extract the inter- and intra-pixel binocular quality-predictive features from these self-similarity measures. Following feature extraction, we use machine learning based on the support vector regression (SVR) procedure to drive the overall quality score. Our results on publicly accessible 3D databases confirmed that the proposed metric is highly efficient and robust. [ABSTRACT FROM AUTHOR]

The proliferating effects of 3 different simple triglycerides (tristearin, triolein, and trilinolein) on the human umbilical vein smooth muscle cells (HUVSMCs) induced by oxidized-LDL (ox-LDL) were investigated in this study. The protein and mRNA gene expressions of proliferating cell nuclear antigen (PCNA), smooth muscle-α-actin (SM-α-actin), and monocyte chemoattractant protein-1 (MCP-1) in HUVSMCs were measured by Western blotting and real-time quantitative polymerase chain reaction (PCR). It was shown that in tristearin (SSS) treated HUVSMCs, the saturated fatty acid content was increased, and the compositions of polyunsaturated fatty acid (PUFA) and monounsaturated fatty acid were decreased significantly. On the other hand, triolein (OOO) and trilinolein (LLL) significantly increased the levels of some typical PUFA such as arachidonic acid, eicosapentaenoic acid, and docosahexaenoic acid. Moreover, LLL and OOO could upregulate the protein and mRNA expressions of PCNA, MCP-1 as well as downregulate the expression of SM-α-actin. The results also showed that, SSS had significant promotion effects on the proliferation of HUVSMCs induced by ox-LDL. Although both LLL and OOO could inhibit the proliferation of HUVSMCs induced by ox-LDL, and might have certain inhibition of the atherosclerotic process. [ABSTRACT FROM AUTHOR]

ZnO thin films prepared by pulsed laser deposition at low temperature are utilized as the electron transport layer in CH3 NH3PbI3− xCl x-based perovskite solar cells with a planar heterojunction structure. Oxygen pressure greatly influences the transparent and conductive properties of ZnO films, which are extremely important as electron transport layer for the perovskite solar cells. The transparent and conductive properties of the films under different oxygen pressures are studied by ultraviolet-visible spectrophotometer and Hall effect measurement system. Through controlling the oxygen pressure, transparent ZnO films with high conductivity are grown and adopted as electron transport layer for planar perovskite solar cell with a power conversion efficiency of 6.3%. After further surface modification of ZnO electron transport layer with [6,6]-phenyl-C61-butyric acid methyl ester, the efficiency of the planar solar cell increases to 7.5%. [ABSTRACT FROM AUTHOR]

In the field of practical three-dimensional (3D) applications, blind measurement of the perceptual quality of distorted 3D images remains a challenging research topic. In this paper, we propose a completely blind 3D image quality measurement (IQM) metric that utilizes a binocular vision mechanism to better align with human perception. As its primary focus, this study is inspired by the visual processing in the primary visual cortex (V1) and the higher visual areas (V2) of binocular vision to facilitate blind 3D-IQM. Furthermore, the proposed metric does not require distorted samples or human subjective opinion scores for training. More specifically, the binocular quality-predictive features of areas V1 and V2 are first extracted from a corpus of pristine natural 3D images. Subsequently, a pristine multivariate Gaussian (MVG) model is trained from the extracted features. Finally, with the trained MVG model, the quality of distorted 3D images is measured using a Mahalanobis distance. Experimental results using two public benchmark 3D databases show that in comparison with current state-of-the-art IQM metrics, the proposed metric achieves excellent prediction performance. [ABSTRACT FROM AUTHOR]

Mercury ions pollution has threatened people's health. Conventional nano-adsorbents suffer from the aggregation and later separation, novel adsorbent with high adsorption performance and easy recover properties is highly needed. In this study, thiol-functionalized electrospun polyacrylonitrile (PAN) nanofibrous membrane was obtained and used as easy recovery adsorbent for mercury ions. The morphologies and chemical composition were studied using SEM, TEM, ATR-FTIR, XRD and XPS. The results indicated that mercury adsorption performance was pH sensitive and the optimal pH range for mercury ions adsorption was about 5.5–6.0. The adsorption equilibrium reached within 25 min, and the adsorption process can be described using the pseudo-second-order model. Isotherm data fitted well to the Langmuir isotherm model. After adsorption of mercury ions, the thiol-functionalized nanofibrous membranes can be regenerated, and the adsorption efficiency maintained up to 90% after three times of usage. [ABSTRACT FROM AUTHOR]

Background: Although a reductionist approach has sought to understand the roles of individual nutrients and biochemicals in foods, it has become apparent that there can be differences when studying food components in isolation or within the natural matrix of a whole food.Objective: The objective of this study was to determine the ability of whole-food intake to modulate the development of obesity and other metabolic dysfunction in mice fed a high-fat (HF), Western-style obesogenic diet. To test the hypothesis that an n-3 (ω-3) polyunsaturated fatty acid-rich food could synergize with other, largely polyphenol-rich foods by producing greater reductions in metabolic disease conditions, the intake of English walnuts was evaluated in combination with 9 other whole foods.Methods: Eight-week-old male C57Bl/6J mice were fed low-fat (LF; 10% fat) and HF control diets, along with an HF diet with 8.6% (wt:wt) added walnuts for 9 wk. The HF control diet contained 46% fat with added sucrose (10.9%, wt:wt) and cholesterol (1%, wt:wt); the added sucrose and cholesterol were not present in the LF diet. Other groups were provided the walnut diet with a second whole food-raspberries, apples, cranberries, tart cherries, broccoli sprouts, olive oil, soy protein, or green tea. All of the energy-containing whole foods were added at an energy level equivalent to 1.5 servings/d. Body weights, food intake, and glucose tolerance were determined. Postmortem, serum lipids and inflammatory markers, hepatic fat, gene expression, and the relative concentrations of 594 biochemicals were measured.Results: The addition of walnuts with either raspberries, apples, or green tea reduced glucose area under the curve compared with the HF diet alone (-93%, -64%, and -54%, respectively, P < 0.05). Compared with HF-fed mice, mice fed walnuts with either broccoli sprouts or green tea (-49% and -61%, respectively, P < 0.05) had reduced hepatic fat concentrations. There were differences in global gene expression patterns related to whole-food content, with many examples of differences in LF- and HF-fed mice, HF- and walnut-fed mice, and mice fed walnuts and walnuts plus other foods. The mean ± SEM increase in relative hepatic concentrations of the n-3 fatty acids α-linolenic acid, eicosapentanoic acid, and docosapentanoic acid in all walnut-fed groups was 124% ± 13%, 159% ± 11%, and 114% ± 10%, respectively (P < 0.0001), compared with LF- and HF-fed mice not consuming walnuts.Conclusions: In obese male mice, walnut consumption with an HF Western-style diet caused changes in hepatic fat concentrations, gene expression patterns, and fatty acid concentrations. The addition of a second whole food in combination with walnuts produced other changes in metabolite concentrations and gene expression patterns and other physiologic markers. Importantly, these substantial changes occurred in mice fed typical amounts of intake, representing only 1.5 servings each food/d. [ABSTRACT FROM AUTHOR]

Fibrosis is emerging as a hallmark of metabolically dysregulated white adipose tissue (WAT) in obesity. Although adipose tissue fibrosis impairs adipocyte plasticity, little is known about how aberrant extracellular matrix (ECM) remodeling of WAT is initiated during the development of obesity. Here we show that treatment with the antidiabetic drug metformin inhibits excessive ECM deposition in WAT of ob/ob mice and mice with diet-induced obesity, as evidenced by decreased collagen deposition surrounding adipocytes and expression of fibrotic genes including the collagen cross-linking regulator LOX Inhibition of interstitial fibrosis by metformin is likely attributable to the activation of AMPK and the suppression of transforming growth factor-β1 (TGF-β1)/Smad3 signaling, leading to enhanced systemic insulin sensitivity. The ability of metformin to repress TGF-β1-induced fibrogenesis is abolished by the dominant negative AMPK in primary cells from the stromal vascular fraction. TGF-β1-induced insulin resistance is suppressed by AMPK agonists and the constitutively active AMPK in 3T3L1 adipocytes. In omental fat depots of obese humans, interstitial fibrosis is also associated with AMPK inactivation, TGF-β1/Smad3 induction, aberrant ECM production, myofibroblast activation, and adipocyte apoptosis. Collectively, integrated AMPK activation and TGF-β1/Smad3 inhibition may provide a potential therapeutic approach to maintain ECM flexibility and combat chronically uncontrolled adipose tissue expansion in obesity. [ABSTRACT FROM AUTHOR]

The CREDENCE trial testing canagliflozin and the EMPA-REG OUTCOME trial testing empagliflozin suggest different effects on acute kidney injury (AKI). AKI diagnosis was mainly made based on changes of serum creatinine (sCr) although this also reflect mode of action of SGLT-2 inhibitors. We analyzed both compounds in a rat AKI model. The renal ischemia-reperfusion injury (I/R) model was used. Four groups were analyzed: sham, I/R+placebo, I/R+canagliflozin (30 mg/kg/day), I/R+ empagliflozin (10 mg/kg/day). Glucose excretion was comparable in both treatment groups indicating comparable SGLT-2 inhibition. Comparing GFR surrogate markers after I/R (sCr and blood urea nitrogen (BUN)), sCr peaked 24 h after I/R, BUN after 48 h, respectively, in the placebo treated I/R group. At all investigated time points after I/R sCr and BUN was higher in the I/R + canagliflozin group as compared to placebo treated rats, whereas the empagliflozin group did not differ from the placebo group. I/R led to tubular dilatation and necrosis. Empagliflozin was able to reduce that finding whereas canagliflozin had no effect. Treatment with empagliflozin also resulted in a significant reduction in an improved inflammatory score (p = 0.006). Renal expression of kidney injury molecule-1 (KIM-1) increased after I/R and empagliflozin but not canagliflozin significantly alleviated KIM-1 expression. I/R reduced urinary miR-26a excretion. Empagliflozin but not canagliflozin was able to restore normal levels of urinary miR-26a. This study in an AKI model confirmed safety data in the EMPA-REG OUTCOME trial suggesting that empagliflozin might reduce AKI risk. The empagliflozin effects on KIM-1 and miR-26a might indicate beneficial regulation of inflammation. These data should stimulate clinical studies with AKI risk as primary endpoint. [ABSTRACT FROM AUTHOR]

Light-field images provide a spatial and angular description of the light, and they can capture rich visual information in the natural world. In recent years, the research on light-field imaging has achieved many fruitful results. As more and more people are now focusing their attention to light-field imaging, the copyright protection of light-field images has become an urgent problem that needs to be addressed. Digital watermarking can effectively protect the copyright ownership of light-field images. Currently, there exists no light-field image watermarking scheme that can resist various geometric attacks. In this work, relying on geranion theory and polar harmonic Fourier moments (PHFMs), geranion polar harmonic Fourier moments (GPHFMs) are constructed and utilized for light-field image watermarking. The geranion represents a hypercomplex number containing one real part and thirty-one imaginary parts, and the imaginary parts of geranion can be used to encode multiple image color components while maintaining the correlation between each component. GPHFMs are stable image features, with good image reconstruction ability and stability. Essentially, the light-field image watermarking based on GPHFMs offers good imperceptibility and robustness, can resist various attacks, and effectively solves the problem of current watermarking schemes related to their inability of resisting geometric attacks. Furthermore, it is verified through experiments that the proposed scheme is more robust than the previously reported schemes. [ABSTRACT FROM AUTHOR]

Ceria–zirconia solid solution nanoparticulates, Ce 1− x Zr x O 2− δ ( x = 0, 0.2, 0.3, 0.4, 0.6, 0.8 and 1.0), are impregnated into the porous 430L stainless steel scaffolds and evaluated as the anode catalysts for solid oxide fuel cells (SOFCs). Combined analyses of X-ray diffraction and Raman scattering reveal the fluorite cubic ( c ) structure up to x ≤ 0.3 transforms to a mixture of the cubic and metastable tetragonal ( t ″) phases for 0.4 ≤ x ≤ 0.8, with the onset of tetragonal distortions at x = 0.8. Temperature-programmed reduction in H 2 indicates that doping Zr 4+ into the ceria lattice could improve the oxygen storage capacity. Nonetheless, the charge transfer process within the bulk Ce 1− x Zr x O 2− δ or across the interfaces of Ce 1− x Zr x O 2− δ |YSZ becomes increasingly sluggish at x ≥ 0.3. The two opposite effects yield the smallest anode polarization resistances at x = 0.3, e.g. , 0.08 ± 0.01 Ω cm 2 for Ce 0.7 Zr 0.3 O 2− δ versus 0.24 ± 0.02 Ω cm 2 for CeO 2− δ or 0.26 ± 0.04 Ω cm 2 for Ce 0.4 Zr 0.6 O 2− δ at 800 °C. Furthermore, thin YSZ electrolyte fuel cells with impregnated La 0.6 Sr 0.4 Fe 0.9 Sc 0.1 O 3− δ – YSZ cathode supports produce peak power densities of 1.24 W cm −2 at 800 °C for nano-Ce 0.7 Zr 0.3 O 2− δ @430L anodes, approximately 80% higher than 0.67–0.70 W cm −2 on nano-CeO 2− δ @430L or nano-Ce 0.4 Zr 0.6 O 2− δ @430L anodes. [ABSTRACT FROM AUTHOR]

Background: Intake of polyphenols and polyphenol-rich fruit extracts has been shown to reduce markers of inflammation, diabetes, and hepatic complications that result from the consumption of a high-fat (HF) diet.Objective: The objective of this study was to determine whether mice fed polyphenol-rich apple peel extract (AE), cherry extract (CE), and quercetin, a phytochemical abundant in fruits including apples and cherries, would modulate the harmful effects of adiposity on blood glucose regulation, endocrine concentrations, and hepatic metabolism in HF-fed C57BL/6J male mice.Methods: Groups of 8-wk-old mice (n = 8 each) were fed 5 diets for 10 wk, including low-fat (LF; 10% of total energy) and HF (60% of total energy) control diets and 3 HF diets containing polyphenol-rich AE, CE, and quercetin (0.2% wt:wt). Also, an in vitro study used HepG2 cells exposed to quercetin (0-100 μmol/L) to determine whether intracellular lipid accumulation could be modulated by this phytochemical.Results: Mice fed the HF control diet consumed 36% more energy, gained 14 g more body weight, and had ∼50% elevated blood glucose concentrations (all P < 0.05) than did LF-fed mice. Mice fed HF diets containing AE, CE, or quercetin became as obese as HF-fed mice, but had significantly lower blood glucose concentrations after food deprivation (-36%, -22%, -22%, respectively; P < 0.05). Concentrations of serum C-reactive protein were reduced 29% in quercetin-fed mice compared with HF-fed controls (P < 0.05). A qualitative evaluation of liver tissue sections suggested that fruit phytochemicals may reduce hepatic lipid accumulation. A quantitative analysis of lipid accumulation in HepG2 cells demonstrated a dose-dependent decrease in lipid content in cells treated with 0-100 μmol quercetin/L (P < 0.05).Conclusions: In mice, consumption of AE, CE, or quercetin appears to modulate some of the harmful effects associated with the consumption of an obesogenic HF diet. Furthermore, in a cell culture model, quercetin was shown to reduce intracellular lipid accumulation in a dose-dependent fashion. [ABSTRACT FROM AUTHOR]

In the past decade, various fragile digital watermarking techniques have been proposed for monoscopic image authentication and temper detection. In this paper, a novel binocular visual characteristics based pixel-wise fragile watermarking scheme for stereoscopic image authentication and tamper detection is proposed. The scheme consists of two processes: embedding of the stereoscopic image authentication message and tamper detection. In the watermark embedding process, the binocular just noticeable difference (BJND) model is used for guiding watermark embedding, which is convenient for achieving a balanced relationship between watermarking capacity and visual transparency. In the tamper detection process, a probability theory and an algorithm of binocular disparity are employed to improve previously obtained detection results and to enhance authentication accuracy. Moreover, to improve the security of the proposed scheme, MD5 hash function and chaotic map are used. Experimental results reveal that the proposed scheme is not only secure, but also achieves superior tamper detection for different attacks. [ABSTRACT FROM AUTHOR]

There are both diversity and unity in the strength characteristics of different geomaterials and concretes. Based on the generalized nonlinear strength theory, a simple but unified strength criterion (USC) is proposed for various materials, such as soils, gravels, rocks, and concretes. Power function is used as the failure curve of the USC in meridian plane, while the shape of failure curve in π-plane is curved triangle, which is between the SMP and Mises criterion. With only four independent parameters, which are convenient to be determined, the proposed criterion is able to take the effects of friction, cohesion, hydrostatic pressure, and intermediate principal stress into consideration. The proposed criterion is compared with some widely used unified strength criteria, such as the Zienkiewicz-Pande criterion and the Lade criterion, against the experimental results for various soils, gravels, rocks, and concretes. The comparison between the predicted and observed results confirmed the validity of the proposed criterion used as a USC for geomaterials and concretes. [ABSTRACT FROM AUTHOR]

FLT3 inhibitors have been explored as a viable therapy for acute myeloid leukemia (AML). However, the clinical outcomes of these FLT3 inhibitors were underwhelming except AC220. Therefore, the development of novel FLT3 inhibitors with high potency against both FLT3-WT and FLT3-ITD mutants are strongly demanded at the present time. In this study, we designed and synthesized a series of novel N -(5-( tert -butyl)isoxazol-3-yl)- N ′-phenylurea derivatives as FLT3 inhibitors. SAR studies focused on the fused rings led to the discovery of a series of compounds with high potency against FLT3-ITD-bearing MV4-11 cells and significantly inhibitory activity toward FLT3. Among these compounds, N -(5-( tert -butyl)isoxazol-3-yl)- N ′-(4-(7-methoxyimidazo[1,2- a ]pyridin-2-yl)phenyl)urea ( 16i ), displayed acceptable aqueous solubility, desirable pharmacokinetic profile and high cytotoxicity selectivity against MV4-11 cells. This compound can inhibit phosphorylation of FLT3 and induce apoptosis in a concentration-dependent manner. Further in vivo antitumor studies showed that 16i led to complete tumor regression in the MV4-11 xenograft model at a dose of 60 mg/kg/d while without observable body weight loss. This study had provided us a new chemotype of FLT3 inhibitors as novel therapic candidates for AML. [ABSTRACT FROM AUTHOR]

A bispyrene fluorescence probe with the cavitand linkage (compound 1) was synthesized, which was proved to be a versatile platform due to the ability of adopting two spatially well‐defined conformations: a closed vase and an expanded kite. vase‐1 was switched to kite‐1 upon addition of TFA or cooling, whereas kite‐1 was isomerized to vase‐1 in the presence of NEt3 or through heating. The interconversion in this molecular switch was tightly associated with the change of fluorescence as we found that changing the temperature and pH of the system‐ a bispyrene compound 1 and gelator 2 led to the sol ‐ gel transformation and reversible intramolecular excimer emission. Briefly, the results show that the fluorescence decreases in the gelation phase and is enhanced in the solution due to variations in temperature and pH. we thus concluded that 1 could be a useful fluorescence probe to determine the multiple states of organogel. [ABSTRACT FROM AUTHOR]

Examines a novel small organic molecules for a highly enantioselective aldol reaction. Importance of acid proton of proline in the reactivity and stereoselectivity of the proline-catalyzed direct aldol reaction; Role of terminal hydroxyl group in the catalyst in stereodiscrimination; Strategy in the design of organic catalysts for direct asymmetric aldol reactions and related transformations.

microRNA (miRNA) is a group of small non-coding RNA that plays important role in post-transcription of gene expression. With the studies about miRNA increase in sugarcane, the researchers lack an exhaustive resource to achieve the data. To fill this gap, we developed MicroSugar, a database that supported mRNA and miRNA annotation for sugarcane (http://suc.gene-db.com). MicroSugar is an integrated resource developed for 194,528 genes including 80,746 unigenes from long reads of Pacbio platform and 468 miRNAs from 72 samples. Internode elongation (jointing) is the key biological characteristic for the growth of sugarcane tillers into sugarcane stems. The present study combined the sequencing data from the different stages in internode elongation of stem and tiller. In total, the 14,300 3′ untranslated region (UTR) sequences were extracted from the gene sequences and 3019 mRNAs as target of 327 miRNA were identified by miRanda algorithm and Spearman's Rho of expression levels. To determine the gene functions regulated by these miRNAs, the gene ontology enrichment analysis was performed and it confirmed that the over-represented Gene Ontology (GO) terms were associated with organism formation indicating the growth controlling function by miRNAs in sugarcane. Moreover, MicroSugar is a comprehensive and integrated database with a user-friendly responsive template. By browsing, searching and downloading of the nucleotide sequences, expression and miRNA targets, the user can retrieve information promptly. The database provides a valuable resource to facilitate the understanding of miRNA in sugarcane development and growth which will contribute to the study of sugarcane and other plants. • A comprehensive miRNA targets database for sugarcane have been built. • MicroSugar provides miRNA, mRNA and miRNA-mRNA correlation information. • Accessible at http://suc.gene-db.com. [ABSTRACT FROM AUTHOR]

Almost all genomes have orphan genes, the majority of which are not functionally annotated. There is growing evidence showed that orphan genes may play important roles in the environmental stress response of Physcomitrium patens. We identified PpARDT (ABA-responsive drought tolerance) as a moss-specific and ABA-responsive orphan gene in P. patens. PpARDT is mainly expressed during the gametophytic stage of the life cycle, and the expression was induced by different abiotic stresses. A PpARDT knockout (Ppardt) mutant showed reduced dehydration-rehydration tolerance, and the phenotype could be rescued by exogenous ABA. Meanwhile, transgenic Arabidopsis lines exhibiting heterologous expression of PpARDT were more sensitive to exogenous ABA than wild-type (Col-0) plants and showed enhanced drought tolerance. These indicate that PpARDT confers drought tolerance among land plants potentially by enhancing ABA response. Further, we identified genes encoding abscisic acid receptor PYR/PYL family proteins, and ADP-ribosylation factors (Arf) as hub genes associated with the Ppardt phenotype. Given the lineage-specific characteristics of PpARDT, our results provide insights into the roles of orphan gene in shaping lineage-specific adaptation possibly by recruiting common pre-existed pathway components. • We characterized PpARDT as an orphan gene in P. patens, and found that PpARDT confers drought tolerance among land plants potentially by enhancing ABA response. • We identified genes encoding abscisic acid receptor PYR/PYL family proteins, and ADP-ribosylation factors (Arf) as hub genes associated with the Ppardt phenotype. • Our results provide insights into the roles of orphan gene in shaping lineage-specific adaptation possibly by recruiting common pre-existed pathway components. [ABSTRACT FROM AUTHOR]

Phenotypic plasticity is widespread in all organisms. This biological property is particularly important for sessile organisms like plants to cope with the ever-changing environmental conditions. Leymus chinensis is a predominantly clonal grass that adapts to diverse stressful habitats including drought, cold and salinity-alkalinity. Previous studies suggest that the remarkable environmental adaption of L. chinensis is probably due to its high degree of phenotypic plasticity; however, the underlying molecular mechanism remains unexplored. In this study, we grew L. chinensis clonal plants in four soil types that differ in nutrient content, nitrate-nitrogen concentration and pH. We observed plasticity in several phenotypic traits in response to specific edaphic factors. By employing de novo RNA-sequencing assembly, we curated differentially expressed genes (DEGs) under each soil type. We found that DEGs under each edaphic condition were enriched for highly specific as well as common GO or KEGG terms known to be biologically relevant to the respective conditions. Moreover, gene activation or silencing was also highly condition-dependent. Together, our results suggest that the high phenotypic plasticity of L. chinensis is likely rooted in its evolved intrinsic property of expressing specific transcriptome profiles in response to diverse niche conditions. • Diverse soils lead to plastic phenotypes in L. chinensis with flexible and condition-specific gene expression. [ABSTRACT FROM AUTHOR]

Rabies remains a worldwide concern, and dogs are a major vector for rabies virus (RABV) transmission. Vaccination is used in China to control the spread of rabies in dogs, a practice which necessitates effective, efficient, and high-throughput methods to confirm vaccination. The current rapid fluorescent focus inhibition test (RFFIT) method to measure virus-neutralizing antibody titers in the serum involves multiple steps, and more efficient methods are needed to match the increasing demand for this type of monitoring. In this study, based on the parental rRC-HL strain, a recombinant RABV rRV-eGFP expressing enhanced green fluorescent protein (eGFP) fused with RABV P protein was generated by a reverse genetic technique. The rRV-eGFP grew stably and successfully expressed P–eGFP fusion in Neuro-2A (NA) host cells. Furthermore, the P protein was shown to co-localize with eGFP in rRV-eGFP-infected NA cells. Since eGFP is easily detected in infected cells under a fluorescence microscope, rRV-eGFP could be used to establish a more rapid virus-neutralizing antibody titers assay based on RFFIT, designated as the RFFIT-eGFP method. From 69 canine serum samples, the RFFIT-eGFP method was shown to be as specific and as sensitive as the RFFIT method, suggesting that it might represent a faster tool than conventional RFFIT for measuring RABV virus-neutralizing antibody titers in canine sera without sacrificing accuracy. [ABSTRACT FROM AUTHOR]

Tuberculosis (TB) remains a major human health problem. New therapeutic antitubercular agents are urgent needed to control the global tuberculosis pandemic. We synthesized a new series of 4-carbonyl piperazine substituted 1,3-benzothiazin-4-one derivatives and evaluated their anti-mycobacterial activities against Mycobacterium tuberculosis H37Ra as well as their druggabilities. The results showed that most of these derivatives, especially the compounds with simple alkyl side chains, exhibited good antitubercular activities and favorable aqueous solubilities with no obvious cytotoxicity. It suggested that the 4-carbonyl piperazine substituents in benzothiazinone scaffold were well tolerated, in which the compound 8h , with an antitubercular activity of MIC 0.008 μM, exhibited an excellent aqueous solubility of 104 μg/mL, which was 100-fold better than the potent DprE1 inhibitor Comp.1 (BTZ038), also more soluble than PBTZ169 . [ABSTRACT FROM AUTHOR]

Thedesign, synthesis, and SAR studies of novel inhibitors of HCVNS4B based on the imidazo[2,1-b]thiazole scaffoldwere described. Optimization of potency with respect to genotype 1bresulted in the discovery of two potent leads 26f(EC50= 16 nM) and 28g(EC50= 31 nM).The resistance profile studies revealed that 26fand 28gtargeted HCV NS4B, more precisely the second amphipathicα helix of NS4B (4BAH2). Cross-resistance between our 4BAH2inhibitors and other direct-acting antiviral agents targeting NS3/4A,NS5A, and NS5B was not observed. For the first time, the synergismof a series of combinations based on 4BAH2 inhibitors was evaluated.The results demonstrated that our 4BAH2 inhibitor 26fwas synergistic with NS3/4A inhibitor simeprevir, NS5A inhibitordaclatasvir, and NS5B inhibitor sofosbuvir, and it could also reducethe dose of these drugs at almost all effect levels. Our study suggestedthat favorable effects could be achieved by combining 4BAH2 inhibitorssuch as 26fwith these approved drugs and that new all-oralantiviral combinations based on 4BAH2 inhibitors were worth developingto supplement or even replace current treatment regimens for curingHCV infection. [ABSTRACT FROM AUTHOR]

Background: Abnormal activation of PI3K/AKT/mTOR (PAM) pathway, caused by PIK3CA mutation, KRAS mutation, PTEN loss, or AKT1 mutation, is one of the most frequent signaling abnormalities in breast carcinoma. However, distribution and frequencies of mutations in PAM pathway are unclear in breast cancer patients from the mainland of China and the correlation between these mutations and breast cancer outcome remains to be identified. Methods: A total of 288 patients with invasive ductal breast cancer were recruited in this study. Mutations in PIK3CA (exons 4, 9 and 20), KRAS (exon 2) and AKT1 (exon 3) were detected using Sanger sequencing. PTEN loss was measured by immunohistochemistry assay. Correlations between these genetic aberrations and clinicopathological features were analyzed. Results: The frequencies of PIK3CA mutation, KRAS mutation, AKT1 mutation and PTEN loss were 15.6%, 1.8%, 4.4% and 35.3%, respectively. However, except for PTEN loss, which was tied to estrogen receptor (ER) status, these alterations were not associated with other clinicopathological features. Survival analysis demonstrated that PIK3CA mutation, PTEN loss and PAM pathway activation were not associated with disease-free survival (DFS). Subgroup analysis of patients with ER positive tumors revealed that PIK3CA mutation more strongly reduced DFS compared to wild-type PIK3CA (76.2% vs. 54.2%; P = 0.011). PIK3CA mutation was also an independent factor for bad prognosis in ER positive patients. Conclusions: AKT1, KRAS and PIK3CA mutations and PTEN loss all exist in women with breast cancer in the mainland China. PIK3CA mutation may contribute to the poor outcome of ER positive breast carcinomas, providing evidence for the combination of PI3K/AKT/mTOR inhibitors and endocrine therapy. [ABSTRACT FROM AUTHOR]

To address issues of image authenticity verification and integrity protection, a fragile watermarking method for stereo image authentication is proposed with stereo matching technique. According to stereo matching of left and right images, non-overlapping blocks of left image are classified into non-matchable and matchable ones. Right image blocks and non-matchable blocks of left image are categorized into smooth, texture and complex blocks considering their roughness. Then, the corresponding alterable-length watermark is computed based on the results of block classification, and the destroyed blocks are recovered by using the corresponding alterable-length watermark. Besides, matchable tampered blocks of left image are recovered with the matched contents in right image. A detection technique with the part of alterable-length watermark is used to increase accuracy of tamper localization at the receiver. The disparity can be used to recover the tampered matchable block. Therefore, the quality of watermarked images is improved because of low embedding capacity. Additionally, the alterable-capacity watermark provides suitable information for smoother images with fewer bits and we obtain high quality restoration. Experimental results show that the proposed method can not only localize the tampered regions precisely but also recover the tampered regions with higher quality compared with the state-of-the-art methods. [ABSTRACT FROM AUTHOR]

Background: Human rabies cases in the Guangxi province of China decreased from 839 in 1982 to 24 in 1995, but subsequently underwent a sharp increase, and has since maintained a high level. Methodology/Principal Findings: 3,040 brain samples from normal dogs and cats were collected from 14 districts of Guangxi and assessed by RT-PCR. The brain samples showed an average rabies virus (RV) positivity rate of 3.26%, but reached 4.71% for the period Apr 2002 to Dec 2003. A total of 30 isolates were obtained from normal dogs and 28 isolates from rabid animals by the mouse inoculation test (MIT). Six representative group I and II RV isolates showed an LD50 of 10−5.35/ml to 10−6.19/ml. The reactivity of monoclonal antibodies (MAbs) to group I and II RV isolates from the Guangxi major epidemic showed that eight anti-G MAbs showed strong reactivity with isolates of group I and II with titers of ≥10,000; however, the MAbs 9-6, 13-3 and 12-14 showed lower reactivity. Phylogenetic analysis based on the G gene demonstrated that the Guangxi RV isolates have similar topologies with strong bootstrap values and are closely bonded. Alignment of deduced amino acids revealed that the mature G protein has four substitutions A96S, L132F, N436S, and A447I specific to group I, and 13 substitutions T90M, Y168C, S204G, T249I, P253S, S289T, V332I, Q382H, V427I, L474P, R463K Q486H, and T487N specific to group II, coinciding with the phylogenetic analysis of the isolates. Conclusions: Re-emergence of human rabies has mainly occurred in rural areas of Guangxi since 1996. The human rabies incidence rate increased is related with RV positive rate of normal dogs. The Guangxi isolates tested showed a similar pathogenicity and antigenicity. The results of phylogenetic analysis coincide with that of alignment of deduced amino acids. Author Summary: Rabies is a worldwide zoonosis disease and is of considerable public health threat and hazard. The Guangxi province of southern China is a severe rabies epidemic region. Human rabies cases decreased from 839 in 1982 to 24 in 1995 in Guangxi as a result of a dog vaccination campaign. However, the number subsequently underwent a sharp increase, and has since maintained a high level. This study reports the systematic surveillance of rabies in Guangxi over the 30-year period from 1982 to 2012. The data revealed that a re-emergence of human rabies has occurred mainly in rural areas of Guangxi since 1996. Human rabies incidence rate increased follows increased instances of RV positive normal dogs. To further understand this re-emergence of rabies, the biological properties of the rabies virus (RV), including the RV-positive rate of normal dogs, pathogenicity, antigenicity and evolution, have been evaluated. The Guangxi isolates all showed similar pathogenicity and antigenicity. These isolates also exhibited similar topologies with strong bootstrap values in the two groups and were closely bonded. Thus these findings will be helpful to understanding the epidemiological situation for rabies in Guangxi. [ABSTRACT FROM AUTHOR]

Background: Human rabies cases in the Guangxi province of China decreased from 839 in 1982 to 24 in 1995, but subsequently underwent a sharp increase, and has since maintained a high level. Methodology/Principal Findings: 3,040 brain samples from normal dogs and cats were collected from 14 districts of Guangxi and assessed by RT-PCR. The brain samples showed an average rabies virus (RV) positivity rate of 3.26%, but reached 4.71% for the period Apr 2002 to Dec 2003. A total of 30 isolates were obtained from normal dogs and 28 isolates from rabid animals by the mouse inoculation test (MIT). Six representative group I and II RV isolates showed an LD50 of 10−5.35/ml to 10−6.19/ml. The reactivity of monoclonal antibodies (MAbs) to group I and II RV isolates from the Guangxi major epidemic showed that eight anti-G MAbs showed strong reactivity with isolates of group I and II with titers of ≥10,000; however, the MAbs 9-6, 13-3 and 12-14 showed lower reactivity. Phylogenetic analysis based on the G gene demonstrated that the Guangxi RV isolates have similar topologies with strong bootstrap values and are closely bonded. Alignment of deduced amino acids revealed that the mature G protein has four substitutions A96S, L132F, N436S, and A447I specific to group I, and 13 substitutions T90M, Y168C, S204G, T249I, P253S, S289T, V332I, Q382H, V427I, L474P, R463K Q486H, and T487N specific to group II, coinciding with the phylogenetic analysis of the isolates. Conclusions: Re-emergence of human rabies has mainly occurred in rural areas of Guangxi since 1996. The human rabies incidence rate increased is related with RV positive rate of normal dogs. The Guangxi isolates tested showed a similar pathogenicity and antigenicity. The results of phylogenetic analysis coincide with that of alignment of deduced amino acids. [ABSTRACT FROM AUTHOR]

[Display omitted] Due to the main role of removing abasic sites in base-excision repair (BER), the overexpression of human apurinic/apyrimidinic endonuclease 1 (APE1) in tumor cells often induces chemotherapy resistance. APE1 contains an endogenous Mg2+ in the active site, while the displacement by toxic Ni2+ attenuates the effectiveness of BER. In present work, comparative molecular dynamics simulations were performed to reveal the changes in the conformation and motion-mode of APE1 44-318 after the substitution of Mg2+ by Ni2+, based on the calculated force field parameters. The results show that Ni2+ disrupts the functional opening of the loops related to DNA binding, and impairs the flexible transformation ability of metal site to cause the loss of the nucleophilic water. Our study also gives an explanation for the disorder of Mg2+ site. This work explores the influence of Ni2+ on the structure and function of APE1 and proposes a putative mechanism for Ni2+-induced BER cytotoxicity. [ABSTRACT FROM AUTHOR]

To date, the lowest protective SGLT2 inhibitor dose is unknown. We initially performed a dose-response pilot study in normal rats. Based on the results of this pilot study we compared the cardio-renal effects of the SGLT-2 inhibitor empagliflozin, with placebo or telmisartan in rats with 5/6 nephrectomy (5/6 Nx) on a high salt diet (HSD). The experimental set up was as follows: Sham operation (Sham) with normal diet and placebo; 5/6 Nx with 2% HSD and placebo; 5/6 Nx with HSD and empagliflozin (0.6 mg/kg/day, bid); 5/6 Nx with HSD and telmisartan (5 mg/kg/day, qd). Empagliflozin treatment increased urinary glucose excretion, in parallel to empagliflozin plasma levels, in a dose-dependent manner starting at doses of 1 mg/kg in the pilot study. 5/6Nx rats on HSD treated with this low empagliflozin dose showed significantly reduced cardiac (−34.85%; P < 0.05) and renal (−33.68%; P < 0.05) fibrosis in comparison to 5/6Nx rats on HSD treated with placebo. These effects were comparable to the effects observed when implementing the standard dose (5 mg/kg/day) of telmisartan (cardiac fibrosis: −36.37%; P < 0.01; renal fibrosis; −43.96%; P < 0.01). RNA-sequencing followed by confirmatory qRT-PCR revealed that both telmisartan and empagliflozin exert their cardiac effects on genes involved in vascular cell stability and cardiac iron homeostasis, whereas in the kidneys expression of genes involved in endothelial function and oxidative stress were differentially expressed. Urinary adenosine excretion, a surrogate marker of the tubuloglomerular feedback (TGF) mechanism, was not affected. In conclusion, the antifibrotic properties of low dose empagliflozin were comparable to a standard dose of telmisartan. The underlying pathways appear to be TGF independent. [Display omitted] • The clinical use of SGLT2 inhibitors is sometimes limited by side effects such as ketoacidosis or urinary tract infections. The lowest effective dose, however, is yet not established. • In an initial pilot study, we identified the lowest empagliflozin dose increasing urinary glucose excretion indicating efficacy in healthy rats. • The antifibrotic properties of this low dose of 1 mg/kg empagliflozin – about 10 times lower as currently used - were comparable to a standard dose of telmisartan in 5/6 nephrectomies rats on high salt died. • RNA-sequencing revealed that both telmisartan and empagliflozin exert their cardiac effects on genes involved in vascular cell stability and cardiac iron homeostasis, whereas renal effects involved genes important for endothelial function and oxidative stress. [ABSTRACT FROM AUTHOR]

Abstract: Structure stability and electrical conductivity of LaSr2Fe2CrO9-δ were investigated in air and in hydrogen to explore its potential applications as symmetrical electrodes for solid oxide fuel cells. X-Ray diffraction measurements showed that LaSr2Fe2CrO9-δ was essentially stable despite the presence of minor LaSrFeO4 impurities after heat-treated in humidified hydrogen at 800°C. LaSr2Fe2CrO9-δ-based symmetrical fuel cells fabricated on LSGM electrolyte substrates via screen printing achieved a maximum power density of 224 mW cm−2. After using a composite electrode (50 wt% LaSr2Fe2CrO9-δ–50 wt% Gd0.2Ce0.8O2-δ), both the anode and the cathode polarization resistances decreased. The maximum power density of symmetrical fuel cells using LaSr2Fe2CrO9-δ–Gd0.2Ce0.8O2-δ composite electrodes increased to 264 mW/cm2 and the corresponding total cell polarization resistance was 0.454Ω cm2 at 800°C with humidified hydrogen fuels and ambient air oxidants. [Copyright &y& Elsevier]

Specific biopharmaceutics classification investigation and study on phamacokinetic profile of a novel drug candidate (2-methylcarbamoyl-4-{4-[3- (trifluoromethyl) benzamido] phenoxy} pyridinium 4-methylbenzenesulfonate monohydrate, NCE) were carried out. Equilibrium solubility and intrinsic dissolution rate (IDR) of NCE were estimated in different phosphate buffers. Effective intestinal permeability (Peff) of NCE was determined using single-pass intestinal perfusion technique in rat duodenum, jejunum and ileum at three concentrations. Theophylline (high permeability) and ranitidine (low permeability) were also applied to access the permeability of NCE as reference compounds. The bioavailability after intragastrical and intravenous administration was measured in beagle dogs. The solubility of NCE in tested phosphate buffers was quite low with the maximum solubility of 81.73 µg/mL at pH 1.0. The intrinsic dissolution ratio of NCE was 1 × 10-4 mg·min-1·cm-2. The Peff value of NCE in all intestinal segments was more proximate to the high-permeability reference theophylline. Therefore, NCE was classified as class II drug according to Biopharmaceutics Classification System due to its low solubility and high intestinal permeability. In addition, concentration-dependent permeability was not observed in all the segments, indicating that there might be passive transportation for NCE. The absolute oral bioavailability of NCE in beagle dogs was 26.75%. Therefore, dissolution promotion will be crucial for oral formulation development and intravenous administration route will also be suggested for further NCE formulation development. All the data would provide a reference for biopharmaceutics classification research of other novel drug candidates. [ABSTRACT FROM AUTHOR]

This study aimed to investigate the profiles change in proanthocyanidins (PAs) catalyzed by polyphenol oxidase (PPO) from lotus seedpod in a model wine system (MWS). Results showed that PAs from lotus seedpod consisted of dimer (74.00 %) and trimer (22.75 %). PPO could tolerate ethanol concentrations below 20 % (v/v). The optimum temperature of PPO activity was 80 °C, and the optimal pH was 9.0. Its molecular weight was approximately 31 kDa, and its secondary structures were α-helix (59.0 %), β-sheet (4.3 %), turns (14.1 %), and random coils (22.6 %). In the MWS, the trimers gradually increased from 22.55 % at 0 h (control) to 100 % at 10 h incubation, while the dimers decreased from 74.33 % (control) to 0 % at 10 h incubation. Moreover, the composition of the precipitate formed at different incubation time points was approximately 16.54 % of monomers, 21.03 % of dimers, and 62.43 % of trimers at 2 h incubation with PPO. The results from this study have provided in vitro evidence for a possible application of PPO in red wine aging. [ABSTRACT FROM AUTHOR]

Background: AZD4547, a small-molecule inhibitor targeting the tyrosine kinase of Fibroblast Growth Factor Receptors (FGFRs), is currently under phase II clinical study for human subjects having breast cancer, while the underlying mechanism remains elusive. The aim of this study is to explore the potential mechanism by which AZD4547 inhibits breast tumor lung metastases at the level of the tumor microenvironment. Methods: First, through in vitro experiments, we investigated the efficacy of the FGFRs inhibitor AZD4547 on 4T1 tumor cells for their proliferation, apoptosis, migration, and invasion. Second, by in vivo animal experiments, we evaluated the effects of AZD4547 on tumor growth and lung metastases in 4T1 tumor-bearing mice. Finally, we examined the impact of AZD4547 on the infiltration of myeloid-derived suppressor cells (MDSCs) in lung, spleens, peripheral blood and tumor. Results: Through this study we found that AZD4547 could efficiently suppress tumor 4T1 cells through restraining their proliferation, blocking migration and invasion, and inducing apoptosis in vitro. In animal model we also demonstrated that AZD4547 was able to inhibit tumor growth and lung metastases, consistent with the decreased MDSCs accumulation in the tumor and lung tissues, respectively. Moreover, the reduced number of MDSCs in peripheral blood and spleens were also observed in the AZD4547-treated mice. Importantly, through the AZD4547 treatment, the CD4+ and CD8+ T-cells were significantly increased in tumor and spleens. Conclusion: Our studies showed that AZD4547 can inhibit breast cancer cell proliferation, induce its apoptosis and block migration and invasion in vitro and suppress tumor growth and lung metastases by modulating the tumor immunologic microenvironment in vivo. © 2014 S. Karger AG, Basel [ABSTRACT FROM AUTHOR]

Abstract: Current treatment for hepatitis C is barely satisfactory, there is an urgent need to develop novel agents for combating hepatitis C virus infection. This study discovered a new class of thieno[2,3-b]pyridine derivatives as HCV inhibitors. First, a hit compound characterized by a thienopyridine core was identified in a cell-based screening of our privileged small molecule library. And then, structure activity relationship study of the hit compound led to the discovery of several potent compounds without obvious cytotoxicity in vitro (12c, EC50 =3.3μM, SI >30.3, 12b, EC50 =3.5μM, SI >28.6, 10l, EC50 =3.9μM, SI >25.6, 12o, EC50 =4.5μM, SI >22.2, respectively). Although the mechanism of them had not been clearly elucidated, our preliminary optimization of this class of compounds had provided us a start point to develop new anti-HCV agents. [Copyright &y& Elsevier]

The medicinal plants of Huang-qi (Radix Astragali) and Sheng-ma (Cimicifuga foetida) demonstrate significantly better antioxidant effects when used in combination than when used alone. However, the bioactive components and interactional mechanism underlying this synergistic action are still not well understood. In the present study, 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay was employed to investigate the antioxidant capacity of single herbs and their combination with the purpose of screening synergistic antioxidant compounds from them. Chromatographic isolation was performed on silica gel, Sephadex LH-20 columns and HPLC, and consequently to yield formononetin, calycosin, ferulic acid and isoferulic acid, which were identified by their retention time, UV λmax, MS and MS/MS data. The combination of isoferulic acid and calycosin at a dose ratio of 1∶1 resulted in significant synergy in scavenging DPPH radicals and ferric reducing antioxidant power (FRAP) assay. Furthermore, the protective effects of these four potential synergistic compounds were examined using H2O2-induced HepG2 Cells bioassay. Results revealed that the similar synergy was observed in the combination of isoferulic acid and calycosin. These findings might provide some theoretical basis for the purported synergistic efficiency of Huang-qi and Sheng-ma as functional foods, dietary supplements and medicinal drugs. [ABSTRACT FROM AUTHOR]

Actinomycin D (Act D) is a general transcriptional inhibitor that is approved for the treatment of sarcomas, and Wilms, germ cell and trophoblastic tumors. Little is known about the molecular mechanisms that dictate the sensitivity of cancer cells to Act D. In this study, we investigated the effects of Act D on heat shock proteins ( HSPs) and the expression and roles of HSP27 in Act D-induced cancer cell apoptosis. We show that Act D upregulates HSP27 and HSP70 expression in cancer cells, whereas it inhibits HSP90 expression. The upregulation of HSP27 by Act D is not attributable to changes in HSP27 transcription or HSP27 synthesis. HSP27 knockdown leads to an increase in Act D-induced caspase 3 and caspase 7 cleavage, and sensitizes rhabdosarcoma cells and breast cancer cells to Act D-induced apoptosis. We conclude that upregulation of HSP27 represents an adaptive response that compromises the anticancer activity of Act D. [ABSTRACT FROM AUTHOR]

Abstract: N-Alkyl and heterocycle substituted 1,3-benzothiazin-4-one (BTZ) derivatives were synthesized. The anti-mycobacterial activities of these compounds were evaluated by determination of minimal inhibitory concentration (MIC) for Mycobacterium tuberculosis H37Ra and M. tuberculosis H37Rv. It was found that an extended or branched alkyl chain analog could enhance the potency, and activities of N-alkyl substituted BTZs were not affected by either nitro or trifluoromethyl at 6-position. Trifluoromethyl plays an important role in maintaining anti-tubercular activity in the piperazine or piperidine analogs. Compound 8o, which contains an azaspirodithiolane group, showed a MIC of 0.0001μM against M. tuberculosis H37Rv, 20-fold more potent than BTZ043 racemate. These results suggested that the volume and lipophilicity of the substituents were important in maintaining activity. In addition, compound 8o was nontoxic to Vero cells and orally bioavailable in a preliminary pharmacokinetics study. [Copyright &y& Elsevier]

[Display omitted] • A novel heterogeneous electro-Fenton catalyst Fe@Fe 2 O 3 -CeO 2 was synthesized. • Satisfactory performance in degradation of multiple organic pollutants was achieved. • The novel catalyst exhibited good recyclability and stability with low metal leaching. • The associated mechanism and possible tetracycline degradation pathways were proposed. Developing efficient heterogeneous electro-Fenton (EF) catalysts for degradation of organic pollutants remains a challenge. Herein, a novel heterogeneous EF catalyst, core–shell Fe@Fe 2 O 3 -CeO 2 composite, was successfully synthesized in a facile manner for effective degradation of tetracycline (TC) pollutant. The catalytic activity was evaluated by effects of different processes, Fe/Ce molar ratio, catalyst dosage, initial solution pH, applied current and aeration mode. Fe@Fe 2 O 3 -CeO 2 with 2:1 Fe/Ce molar ratio achieved TC removal efficiency of 90.7% within 1 h and mineralization efficiency of 86.9% within 6 h with such excellent performance attributed to the high utilization efficiency of H 2 O 2 and the synergistic effects between Ce4+/Ce3+ and Fe3+/Fe2+. Moreover, this novel catalyst exhibited good recyclability and stability in successive cycles with low metal leaching. Furthermore, the heterogeneous EF process showed satisfactory catalytic activity towards degradation of other organic pollutants (e.g., metronidazole, diclofenac sodium, and chloramphenicol). Based on the experimental results and analysis, the mechanism of the heterogeneous EF process with Fe@Fe 2 O 3 -CeO 2 catalyst and possible TC degradation pathways were proposed, which provides insights into the catalytic reaction process and should be of value in facilitating the application of this method in refractory wastewater treatment. [ABSTRACT FROM AUTHOR]

In this paper, the in-situ Scanning Electron Microscopy (in-situ SEM) technique and three-dimensional (3-D) phase-field simulation were combined to perform a comprehensive study on the kinetics and mechanisms of dewetting (or agglomeration) of a 30 nm NiSi films on Si(100) substrate at 600 °C. The evolution of texture during agglomeration of the polycrystalline NiSi thin film was also studied by ex-situ Electron BackScattered Diffraction (EBSD). The phase-field simulation results showed that abnormal grain growth plays an important role in the dewetting process of polycrystalline films, while the misorientations between the NiSi grains and the Si substrate are the main reason for the agglomeration of NiSi polycrystalline thin film on the monocrystal Si substrate. Moreover, 3-D phase-field simulations coupled with experimental information on misorientation distribution and initial grain size were also performed, and the simulated Ni silicide grain morphology is in good agreement with the in-situ SEM results during agglomeration. In order to slow down or to suppress the agglomeration, it is highly recommended to increase the volume fraction of low angle grains, and/or to decrease the misorientation between the NiSi grain and the Si substrate or between the NiSi grains. [Display omitted] [ABSTRACT FROM AUTHOR]

Our previous study isolated a novel Issatchenkia terricola WJL-G4, which exhibited a potent capability of reducing citric acid. In the current study, I. terricola WJL-G4 was applied to decrease the content of citric acid in red raspberry juice, followed by the red raspberry wine preparation by Saccharomyces cerevisiae fermentation, aiming to investigate the influence of I. terricola WJL-G4 on the physicochemical properties, organic acids, phenolic compounds and antioxidant activities during red raspberry wine processing. The results showed that after being treated with I. terricola WJL-G4, the citric acid contents in red raspberry juice decreased from 19.14 ± 0.09 to 6.62 ± 0.14 g/L, which was further declined to 5.59 ± 0.22 g/L after S. cerevisiae fermentation. Parameters related to CIELab color space, including L*, a*, b*, h°, and ∆E* exhibited the highest levels in samples after I. terricola WJL-G4 fermentation. Compared to the red raspberry wine pretreated without deacidification (RJO-SC), wine pretreated by I. terricola WJL-G4 (RJIT-SC) exhibited significantly decreased contents of gallic acid, cryptochlorogenic acid, and arbutin, while significantly increased contents of caffeic acid, sinapic acid, raspberry ketone, quercitrin, quercetin, baicalein, and rutin. Furthermore, the antioxidant activities including DPPH· and ABTS+· radical scavenging were enhanced in RJIT-SC group as compared to RJO-SC. This work revealed that I. terricola WJL-G4 had a great potential in red raspberry wine fermentation. [ABSTRACT FROM AUTHOR]

The microstructure, physicochemical properties and adsorption capacities of deoiled red raspberry pomace (DRP) and its total dietary fiber (DRPF) were investigated in the study, aiming to evaluate their potential to use as functional food ingredients. The chemical composition showed that both DRP and DRPF were mainly made of lignin. Compared to DRP, DRPF exhibited significantly decreased total contents of sugar, fat, and crude protein, from 13.37%, 5.07% and 2.58% to 1.54%, 1.17% and 1.37%, respectively. The thermal gravity analysis revealed that DRP and DRPF were stable under 162 ° C and 197 ° C, respectively. DRPF showed higher water-holding capacity (8.97 g/g vs. 2.62 g/g in DRP), swelling ability (10.18 mL/g vs. 6.93 g/g in DRP) and water solubility (0.25% vs. 0.07% in DRP). DRP had significantly higher in vitro cholesterol, and glucose adsorption capacities. However, better adsorption capacity of toxic ions was shown in DRPF. Based on chemical composition and characteristics, DRP and DRPF are both ideal supplements for dietary fiber and might be suitable to use as anti-obesity ingredients. Moreover, DRPF may be a better choice for toxic ions removing food. • DRPF is dietary fiber extracted enzymically from DRP. • DRP and DRPF was simultaneously studied for the first time. • DRP had lower water-holding capacity, swelling ability and solubility. • DRP had superior cholesterol, glucose, nitrite ions adsorption capacity in vitro. • DRPF had advantages of higher toxic ions adsorption capacity. [ABSTRACT FROM AUTHOR]

High content of citric acid in lemon juice leads to poor sensory experience. The study aimed to investigate the dynamics changes in organic acids, phenolic compounds, and antioxidant activities of lemon juice fermented with Issatchenkia terricola WJL-G4. The sensory evaluation of fermented lemon juice was conducted as well. Issatchenkia terricola WJL-G4 exhibited a potent capability of reducing the contents of citric acid (from 51.46 ± 0.11 g/L to 8.09 ± 0.05 g/L within 60 h fermentation) and increasing total phenolic level, flavonoid contents, and antioxidant activities compared to those of unfermented lemon juice. A total of 20 bioactive substances, including 10 phenolic acids and 10 flavonoid compounds, were detected both in fermented and unfermented lemon juice. The lemon juice fermented for 48 h had better sensory characteristics. Our findings demonstrated that lemon juice fermented with Issatchenkia terricola exhibited reduced citric acid contents, increased levels of health-promoting phenolic compounds, and enhanced antioxidant activities. [ABSTRACT FROM AUTHOR]

A novel series of N-methylpicolinamide-4-thiol derivatives were synthesized and evaluated on human cancer cell lines. Among them, compound 6p displayed potent and broad-spectrum anti-proliferative activities in vitro on some human cancer cell lines, even better than sorafenib. The advanced kinase inhibitory assays showed that compound 6p could selectively inhibit Aurora-B kinase. The biological results were rationalized by the molecular docking study, which indicated the stable interactions of 6p with the Aurora-B kinase. [ABSTRACT FROM AUTHOR]

An improved synthesis of 6-aryl-3-cyanopyridine-2-(1H)-thiones utilizing enaminones as starting materials catalyzed by 1,4-diazabicyclo[2.2.2]octane (DABCO) was described. Moreover, a convenient one-pot conversion of aryl ketones to 6-aryl-3-cyanopyridine-2-(1H)-thiones was also developed in moderate to good yields (up to 80%). [ABSTRACT FROM AUTHOR]

A series of novel benzothiazole-2-thiol derivatives were synthesized and their structures determined by 1H-NMR, 13C-NMR and HRMS (ESI). The effects of all compounds on a panel of different types of human cancer cell lines were investigated. Among them, pyridinyl-2-amine linked benzothiazole-2-thiol compounds 7d, 7e, 7f and 7i exhibited potent and broad-spectrum inhibitory activities. Compound 7e displayed the most potent anticancer activity on SKRB-3 (IC50 = 1.2 nM), SW620 (IC50 = 4.3 nM), A549 (IC50 = 44 nM) and HepG2 (IC50 = 48 nM) and was found to induce apoptosis in HepG2 cancer cells. [ABSTRACT FROM AUTHOR]