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Verticillium wilt and Fusarium wilt, caused by Verticillium dahliae and Fusarium oxysporum, respectively, severely restricted cotton production. It is difficult to control the damage due to large unknown about the interaction between plants and pathogens. Here, we reported the identification of cotton Bsr-k1, which was also designated as GhBsr-k1. The GhBsr-k1 was expressed in the root, stem and leaf. Silencing of GhBsr-k1 improved plant resistance to both V. dahliae and F. oxysporum. In the GhBsr-k1-silenced plants, the expression of phenylpropanoid metabolism related genes were significantly up-regulated comparing with the control, which resulting the increase of lignin deposition. Moreover, the expression level of PALs exhibited highly negative correlation with GhBsr-k1. Collectively, the results suggested GhBsr-k1 acted as a negative regulator during plant resistance against V. dahliae and F. oxysporum. The potential mechanisms beyond GhBsr-k1 in plant defense may related to the regulation of the transcript of lignin deposition genes (GhPAL2, GhPAL5).

Two novel 3-D Ln(III)–Cu(I) heterometallic coordination polymers, [Ln2Cu2(L3)4(C2O4)2]·H2O (Ln = Sm, Eu; HL3 = 5-aminonicotinic acid), were hydrothermally produced by reacting lanthanide oxide and copper halide with 5-aminonicotinic acid and orotic acid. In the two isostructural complexes, {Ln6}-wheel clusters link each other via edge-sharing mode, constructing honeycomb-like layers which stack in –ABAB– mode. On the whole, the architectures can be described as sandwich framework constructed by {Ln6}-wheel layers pillared by interlamellar [CuOL32] triangle pillars. The electronic structure was theoretically calculated by the density functional theory, confirming the direct transition character. The steady and transient photoluminescent spectra were measured, from which the intensity parameters, radiative lifetime and quantum efficiency were calculated within the framework of the Judd–Ofelt theory. [Eu2Cu2(L3)4(C2O4)2]·H2O can be regarded as a potential candidate for LED applications.

Human activities in cold climates are more and more frequent. But, an efficient strategy to maintain the human body temperature is still a challenging work. In this paper, we propose a photothermal...

Although multivalent glycosidase inhibitors have shown enhanced glycosidase inhibition activities, further applications and research directions need to be developed in the future. In this paper, two positional isomeric perylene bisimide derivatives (PBI-4DNJ-1 and PBI-4DNJ-2) with 1-deoxynojirimycin conjugated were synthesized. Furthermore, PBI-4DNJ-1 and PBI-4DNJ-2 showed positional isomeric effects on the optical properties, self-assembly behaviors, glycosidase inhibition activities, and hypoglycemic effects. Importantly, PBI-4DNJ-1 exhibited potent hypoglycemic effects in mice with 41.33 ± 2.84 and 37.45 ± 3.94% decreases in blood glucose at 15 and 30 min, respectively. The molecular docking results showed that the active fragment of PBI-4DNJ-1 has the highest binding energy (9.649 kcal/mol) and the highest total hydrogen bond energy (62.83 kJ/mol), which were related to the positional isomeric effect on the hypoglycemic effect in mice. This work introduced a new means to develop antihyperglycemic agents in the field of multivalent glycomimetics.

Mammalian sperm is highly susceptible to reactive oxygen species (ROS) during the cryopreservation process. Astaxanthin (AST), a red pigment of the carotenoid family, is recognized as having a variety of beneficial biological activities and effects, including antioxidant, anticancer, anti-diabetic, and anti-inflammatory. The present study aimed to investigate whether the presence of AST protected boar sperm from ROS stress during cryopreservation. Boar sperm was diluted with a freezing medium supplemented with different concentrations of AST (0, 0.5, 1, 2, or 5 μM). The addition of AST, especially at a concentration of 2 μM, exerted positive effects on post-thaw sperm motility parameters. Meanwhile, sperm plasma membrane integrity and acrosome integrity of post-thaw sperm were significantly increased, while lipid peroxidation was inhibited in response to 2 μM AST treatment. Interestingly, compared to the control, supplementation with 2 μM AST increased unsaturated fatty acids (UFAs) levels and decreased saturated fatty acids (SFAs) content in post-thaw sperm, leading to a decreased ratio of SFAs/UFAs in the AST group. In conclusion, the addition of AST to freezing extenders inhibited lipid peroxidation and regulated fatty acid composition of the sperm membrane, improved post-thaw sperm quality, and had no adverse effect on boar sperm in vitro fertilization (IVF) capacity and potential for embryonic development. Our data provide a novel insight into understanding the mechanisms of AST concerning protecting boar sperm quality against ROS damage during cryopreservation.

Taking Jiaozuo mining area as the research background, according to the survey of water samples among the main water-filled aquifers of the mine and water gushing sources due to the exploitation of the No.21 coal seams in Shanxi group, six kinds of water chemical composition were selected as the sample indexes, including Cl-, SO42-, HCO3-, Na++K+, Ca2+, Mg2+, based on the data of groundwater chemical composition, and a principal component analysis was applied to establish the mathematical model by the method of factor analysis. A piper diagram was used to intuitively conduct the synthetical analyses for the general chemical characteristics and water quality types of the water samples. At the same time, via the comparative analysis between the water properties of water exits and that of the main aquifers in the Jiaozuo mining area, discrimination of the hybridization of the multiple water gushing sources due to coal mining was done. Moreover, by dint of the SPSS factor analysis, the water chemical proxies were carried on dimensionality reduction from the six kinds of water chemical composition to the three major factors, which replaced the original variables to participate in the data modeling. The results of the study showed that the combination of the piper diagram and the factor analysis modeling could effectively identify the water gushing sources owing to exploiting the No.21 coal seams of the Shanxi group in the Jiaozuo mining area and rank on the basis of the contributions of each aquifer to the amounts of water bursting in the mine, solving the problems of information superposition and correlations consisted in the identification of water gushing sources, which provides a theoretical basis for the prevention and cure of the mine water disasters.

Reducing the poisoning effect of alkali and heavy metals over ammonia selective catalytic reduction (NH3-SCR) catalysts is still an intractable issue, as the presence of K and Pb in fly ash greatly...

Due to the influences of precursors emissions, meteorology, geography and other factors, ozone formation sensitivity (OFS) is generally spatially and temporally heterogeneous. This study characterized detailed spatial and temporal variations of OFS in Guangdong-Hong Kong-Macao Greater Bay Area (GBA) from 2012 to 2016 based on OMI satellite data, and analyzed the relationships of OFS with precursors emissions, meteorology and land use types (LUTs). From 2012 to 2016, the OFS tended to be NOx-limited in GBA, with the value of FNR (HCHO/NO2) increasing from 2.04 to 2.22. According to the total annual emission statistics of precursors, NOx emissions decreased by 33.1% and VOCs emissions increased by 35.2% from 2012 to 2016, directly resulting in OFS tending to be NOx-limited. The Grey Relation Analysis results show that total column water (TCW), surface net solar radiation (SSR), air temperature at 2 m (T2) and surface pressure (SP) are the top four meteorological factors with the greatest influences on OFS. There are significant positive correlations between FNR and T2, SSR, TCW, and significant negative correlations between FNR and SP. In GBA, the OFS tends to be NOx-limited regime in wet season (higher T2, SSR, TCW and lower SP) and VOCs-limited regime in dry season (lower T2, SSR, TCW and higher SP). The FNR displays obvious gradient variations on different LUTs, with the highest in “Rural areas”, second in “Suburban areas” and lowest in “Urban areas”.

In this work, compared with non-Cu2In nanoalloy counterpart Cu-In/ZrO2 catalysts, Cu1In2Zr4-O catalyst with the structure of Cu2In alloy exhibited an excellent performance for CO2 hydrogenation to ...

Andrographolide is a labdane diterpenoid from Andrographis paniculata and has been used in the clinic for several decades to treat a variety of diseases in east Asia. In the present study, modification of 12-thioether andrographolide was carried out to seek compounds with better antitumor activity and drug-like properties. A series of novel 3,19-modified thioether andrographolide derivatives were synthesized and evaluated for their in vitro anticancer activities against human breast cancer cells. The results are promising and important in the further development of anticancer agents.

A series of heterogeneous catalysts based on phosphomolybdic salts with different metals in counter or substituent positions, LnPMo12O40 (L = Al3+, Fe3+, Cr3+, Ti4+, Zr4+ and Zn2+, abbreviated as LPMo12) and HxPMo11LO39 (L = Zn2+, Cr3+, Fe3+, Al3+, Ti4+, for Ti4+; the amount of O is 40, abbreviated as HPMo11L), were prepared using a simple calcination treatment and were evaluated in aerobic oxidation of glycerol. After calcination at about 250 °C for 4 h, homogeneous LnPMo12O40·nH2O and HxPMo11LO39·mH2O became heterogeneous. Their specific surface areas were also enhanced as well as their activity and reusability. Similar to the homogeneous catalysts, AlPMo12 treated at 400 °C (AlPMo12-400) was found to be the most active catalyst in glycerol oxidation to lactic acid, with 96.1% yield and 98.6% conversion at 60 °C for 5 h with 1 MPa of O2; it gave a turnover number (TON; TON = [LA]/[catalyst]) of 2.4 × 102, higher than that of AlPMo12-250 treated at 250 °C (TON = 2.0 × 102). AlPMo12 behaved as a heterogeneous catalyst in glycerol oxidation and could be reused at least 12 times. AlPMo12-400 also performed well in crude glycerol oxidation, affording lactic acid yields as high as 86.8%.

The steel–plastic compound geogrid has been widely used as a new reinforcement material in geotechnical engineering and other fields. Therefore, it is essential to fully understand the mechanical properties of steel–plastic compound geogrid-reinforced belts to utilize steel–plastic compound geogrids efficiently. In this study, tensile mechanical tests of steel wire, polyethylene geogrid belt, and steel–plastic compound geogrid-reinforced belt were conducted with respect to the tensile mechanical properties of steel–plastic compound geogrid-reinforced belts. In addition, the minimum reinforcement and optimal reinforcement ratios of steel–plastic compound geogrid-reinforced belts were summarized. The results showed that the steel–plastic compound geogrid-reinforced belts possessed an incongruent force of the internal steel wire during the tensile process. The tensile stress–strain curve of the steel–plastic compound geogrid-reinforced belt can be divided into the composite adjustment, steel wire breaking, and residual deformation stages. The tensile strength of the steel–plastic compound geogrid-reinforced belt is proportional to the diameter and number of steel wires in the reinforced belt. The minimum and optimum reinforcement ratios of steel wire in the steel–plastic compound geogrid-reinforced belt were 0.63% and 11.92%, respectively.

Diabetic osteoporosis (DOP) belongs to secondary osteoporosis caused by diabetes; it has the characteristics of high morbidity and high disability. In the present study, we constructed a type 1 diabetic rat model and administered chondroitin sulfate (200 mg/kg) for 10 weeks to observe the preventive effect of chondroitin sulfate on the bone loss of diabetic rats. The results showed that chondroitin sulfate can reduce blood glucose and relieve symptoms of diabetic rats; in addition, it can significantly increase the bone mineral density, improve bone microstructure, and reduce bone marrow adipocyte number in diabetic rats; after 10 weeks of chondroitin sulfate administration, the SOD activity level was upregulated, as well as CAT levels, indicating that chondroitin sulfate can alleviate oxidative stress in diabetic rats. Chondroitin sulfate was also found to reduce the level of serum inflammatory cytokines (TNF-α, IL-1, IL-6, and MCP-1) and alleviate the inflammation in diabetic rats; bone metabolism marker detection results showed that chondroitin sulfate can reduce bone turnover in diabetic rats (decreased RANKL, CTX-1, ALP, and TRACP 5b levels were observed after 10 weeks of chondroitin sulfate administration). At the same time, the bone OPG and RUNX 2 expression levels were higher after chondroitin sulfate treatment, the bone RANKL expression was lowered, and the OPG/RANKL ratio was upregulated. All of the above indicated that chondroitin sulfate could prevent STZ-induced DOP and repair bone microstructure; the main mechanism was through anti-oxidation, anti-inflammatory, and regulating bone metabolism. Chondroitin sulfate could be used to develop anti-DOP functional foods and diet interventions for diabetes.

Glyphosate is a highly effective, low-toxicity, broad-spectrum herbicide, which is extensively used in global agriculture to control weeds and vegetation. However, glyphosate has become a potential threat to human and ecosystem because of its excessive usage and its bio-concentration in soil and water. Herein, a novel turn-on fluorescent probe, N-n-butyl-4-(3-pyridin)ylmethylidenehydrazine-1,8-naphthalimide (NPA), is proposed. It efficiently detected Cu2+ within the limit of detection (LOD) of 0.21 μM and displayed a dramatic turn-off fluorescence response in CH3CN. NPA-Cu2+ complex was employed to selectively and sensitively monitor glyphosate concentrations in real samples accompanied by a fluorescence turn-on mode. A good linear relationship between NPA and Cu2+ of glyphosate was found in the range of 10–100 μM with an LOD of 1.87 μM. Glyphosate exhibited a stronger chelation with Cu2+ than NPA and the system released free NPA through competitive coordination. The proposed method demonstrates great potential in quantitatively detecting glyphosate in tap water, local water from Songhua River, soil, rice, millet, maize, soybean, mung bean, and milk with mild conditions, and is a simple procedure with obvious consequences and no need for large instruments or pretreatment.

Objective: To investigate the effects of “Yingwei Fang” on nitric oxide synthase (eNOS), endothelin-converting enzyme (ECE) and homocysteine (Hey) in patients with type 2 diabetes mellitus. Methods: 39 cases of type 2 diabetes mellitus with different syndromes were observed, including 14 cases of Yin deficiency heat, 10 cases of Qi and Yin deficiency and 15 cases of Yin and Yang deficiency. All patients took “Yingwei Fang” capsules orally, 5 capsules per time, 3 times a day. At the same time, they were combined with conventional treatment such as dialectical TCM dialectical theory of treatment and hypoglycemia. The changes of eNOS, ECE and Hcy were measured after 150 days of treatment and compared with those before treatment. RESULTs: After treatment, there were changes in $e$ NOS, ECE and Hcy in patients with Yin deficiency, Qi and Yin deficiency and Yin and Yang deficiency, among which eNOS, ECE and Hcy were significantly improved (P

The Creep Crack Growth (CCG) of polyethylene pipe directly limits its long-term lifetime. The long-term lifetime estimation of polyethylene pipe was proposed by combining the crack kinetics and Paris-Erdogan crack growth model. According the Full Notch Creep Test (FNCT) to measure the relationship between the crack opening displacement COD and the test time ti of the preformed PE ring notch specimens during creep tension, and the crack growth rate da/dt, stress intensity factor KI can be calculated, then the inherent parameters A, m of PE materials can be obtained through the Paris-Erdogan crack growth model. Finally, the relationship between the crack depth af and the crack growth time tCCG of polyethylene pipes in the long-term use process can be extrapolated. The test result shown that, when the specification of PE pipes were dn110-sdr11, if there was an initial crack with a depth of aini = 0.4mm on the outer wall of the pipe, and under the continuous action of pipe pressure with p = 0.4 MPa, when the depth crack of PE1 and PE2 pipes expanded to 0.8mm, it needed to maintain or replace the defective pipe section, and the lifetime of the pipes were 22.89 and 20.03 years. Respectively, if the pipes were not maintained and replaced in time, and it will exist medium leakage only takes 14.13 and 12.44 years.

Large pore size of fibrous membrane (FM) deteriorates the cycle lifetime and rate capabilities, and the way of obtaining FM with improved electrolyte wettability and decreased pore size is still challenging. Herein, we report a facile method for the fabrication of the polydopamine modification polyacrylonitrile (PDA@PAN) FM via the combination of the spin coating and electrospinning techniques. The PDA coating increases the fiber diameter and the surface roughness of the PAN fibers, thus decreasing the pore size and mitigating the lithium dendrite formation by uniformly distributing Li-ion flux. Meanwhile, PDA modification not only improves the affinity for electrolyte and enhances the ion conductivity (1.39 mS cm−1), but also doubles the stress strength (13.92 MPa) because of the formation of more adhesion structure. Consequently, both the Li/LiFePO4 and Li/Li4Ti5O12 cells involving PDA@PAN FM demonstrate more stable cycle life and better rate capability compared with those of cells based on PAN FM and Celgard membrane. The work also provides a promising separator fabrication strategy for other energy storage systems.

2,5-Diformylfuran (DFF) is a versatile compound that can be used as a precursor in the synthesis of various value-added products, which can be obtained from aerobic oxidation of 5-hydroxymethylfurfural (HMF). However, aerobic oxidation of 5-HMF gives rise to several pathways and products containing DFF, 2,5-furandicarboxylic acid (FDCA), or maleic anhydride (MA). To date, both homogeneous and heterogeneous metal catalysts have been explored for the oxidation of HMF to DFF with various oxidants. It was found that materials containing vanadium showed higher efficiency with conversions ranging from 84% to 100% and DFF yields of 82%−99.9% at 120−140°C for 3−11 h in dimethyl sulfoxide (DMSO). Selective oxidation of 5-HMF depended on the nature of the catalysts and supports. Polyoxometalates (POMs) are widely applied in catalysis especially in catalytic transformation of biomass. Especially, POMs containing vanadium had been found to be potential for oxidation of HMF to produce a series of products including DFF and MA. The diversity in structure and components allows POMs to be most active in acidic and redox catalysis. Compared to their homogeneous catalysis, heterogeneous systems showed more favorable in easy separation and reuse, introduction of special active sites belonging to supports, enhancement in surface area. Under such circumstances, heterogeneous POM catalysts are developed using microporous, mesoporous and macroporous SiO2, TiO2 and ZrO2 as supports. Compared to powdered mesoporous materials, electrospun nanofibers are good candidates because of their high surface-to-volume ratios. Herein, trifunctional H5PMo10V2O40/meso-ZrO2(f) had been synthesized using combined electrospinning and surfactant pore-forming technology, which were characterized by IR, 31P MAS NMR, XRD, SEM, TEM, and N2 adsorption-desorption measurement. Combination of IR, 31P MAS NMR, XRD, BET surface areas, SEM and TEM could confirm that POM molecules were loaded on ZrO2 nanofibers (200−400 nm) with mesoporous structure. It was found that decorating ZrO2 nanofibers by H5PMo10V2O40 generated enhanced catalytic activity by emerging their unique individual properties of redox ability, Bronsted acidity, Lewis acidity, and nanofiber structure with higher surface area. H5PMo10V2O40/meso-ZrO2(f) materials were evaluated in aerobic oxidation of 5-HMF to DFF. The conversion of HMF followed the order: HPMoV/meso-ZrO2(5-f) (0.17 mmol g−1, 60.1%) (0.22 mmol g−1, 79.8%) (0.36 mmol g−1, 92.3%) (0.41 mmol g−1, 94.2%) (0.47 mmol g−1, 95.6%) (0.51 mmol g−1, 96.4%) (2.66 mmol g−1, 99.9%), which followed the increase of HPMoV loading hence the Bronsted acidity. The DFF yields depended on their Lewis acidity as HPMoV/meso-ZrO2(35-f) (B/L=0.04:1, yield=74.6%) 7 h. The mechanism study showed that the generated O2 was the active site in this aerobic oxidation being catalyzed by H5PMo10V2O40. Moreover, H5PMo10V2O40/meso-ZrO2(f) showed good stability and duration for being reused at least ten times without leaching of POMs from ZrO2 nanofibers.

The objective of the present analysis was to determine whether changes in Brief Pain Inventory (BPI) average pain scores by patient global impression of improvement (PGI‐I) category and the cut‐off for clinically important difference (CID) were different between Asian and Caucasian patients with chronic pain due to osteoarthritis. This analysis used data from 3 (Caucasian) and 2 (Asian) randomized, placebo‐controlled, 10‐ to 14‐week duloxetine studies for the treatment of patients ≥40 years of age with osteoarthritis pain. The receiver operating characteristic (ROC) analysis was used to characterize the association between changes in BPI average pain scores and PGI‐I levels at study endpoint. The CID was characterized by PGI‐I, and the cut‐off point for CID in BPI average pain scores was determined by the intersection of a 45‐degree tangent line with each ROC curve. Data from 668 Asian and 868 Caucasian patients were available for analysis. Baseline BPI average pain ratings including worst and least pain were comparable between Asians and Caucasians. Ratings for percentage change from baseline to endpoint for BPI average pain scores in Asian patients and Caucasian patients were similar across the 7 PGI‐I categories, regardless of age, gender, study, and treatment. The ROC analysis results of cut‐off points in BPI average pain scores demonstrated the raw change cut‐off was −3.0, and percentage change cut‐off was −40% for both Asian and Caucasian patients. Overall, the present analysis concludes changes in BPI average pain scores by PGI‐I category and the cut‐off for CID were similar for Asian and Caucasian patients with chronic pain due to osteoarthritis.

Histamine H1 receptor (H1R) and histamine H4 receptor (H4R) are essential in allergic inflammation. The roles of H4R have been characterized in T cell subsets, whereas the functional properties of H4R in monocytes remain unclear. In the current study, the responses of H4R in peripheral monocytes from patients with allergic rhinitis (AR) were investigated. The results confirmed that H4R has the functional effects of mediating cytokine production (i.e., down-regulating IFN-γ and up-regulating IL-6) in cells from a monocyte cell line following challenge with histamine. We demonstrated that when monocytes from AR patients were stimulated with allergen extracts of house dust mite (HDM), IFN-γ secretion was dependent on H4R activity, but IL-6 secretion was based on H1R activity. Furthermore, a combination of H1R and H4R antagonists was more effective at blocking the inflammatory response in monocytes than treatment with either type of antagonist alone.

Two new lignan derivatives, jatrolignan A (1) and B (2), were isolated from the aerial parts of Jatropha curcas. Their structures were elucidated by spectroscopic methods, including extensive 1D and 2D NMR experiments, as well as high-resolution ESI mass analysis.

In this paper, a long-period waveguide grating was fabricated in x-cut lithium niobate substrate by patterned annealed proton exchange waveguide fabrication process. The waveguide mode characteristic was evaluated using a charge-coupled device (CCD) camera. It shows that the waveguide is single mode transmission at a wavelength of 1 550 nm. The transmission spectra of the long period waveguide gratings were measured by optical spectrum analyzer (OSA) and show an extinction ratio of ~17 dB and a 3 dB bandwidth of ~10 nm at the resonant wavelength. The resonant wavelength moves toward to the long wavelength direction as the waveguide width-difference increases in the same period, and also shifts toward to the long wavelength direction with the increase of the period in the case of the same waveguide width-difference. The method of fabricating a long period waveguide grating based on a patterned annealed proton exchange technique simplifies the fabrication process, and at the same time, reduces the fabrication cost.

BACKGROUND Retinoblastoma is a rare malignancy arising from the immature cells of the retina, generally in children up to the age of 3 years. Here, we assessed the anticancer effects of a natural sesquiterpene lactone - 8-deoxylactucin - on the growth of the retinoblastoma RB355 and normal RPE cells. MATERIAL AND METHODS Cell viability was assessed by 3-(4,5-dimethylthiazol-2-Yl)-2,5-diphenyltetrazolium bromide (MTT) assay, and apoptosis was assessed by DAPI staining and annexin V/propidium iodide (PI) assay. Reactive oxygen species (ROS) levels were determined by fluorescence microscopy. Flow cytometry was used to determine the cell cycle distribution. Protein expression was determined by Western blot analysis. RESULTS The results showed that 8-deoxylactucin exerted selective and potent anticancer effects on the RB355 cells and exhibited an IC50 of 25 µM. Nonetheless, the cytotoxic effects of 8-deoxylactucin on the normal RPF cells were comparatively lower, as evident from the IC₅₀ of 65 µM. 8-Deoxylactucin increased the production of ROS and triggering apoptosis of RB355 cells. The induction of 8-deoxylactucin-induced apoptosis was also accompanied with increased cleavage of caspase 3, upregulation of Bax, and downregulation of Bcl-2. The 8-deoxylactucin-induced cell cycle arrest of RB355 cells was also associated with inhibition of cyclin A and B1 expression, as well as the inhibition of Cdc2 phosphorylation. CONCLUSIONS 8-Deoxylactucin inhibits the growth of RB355 cells by apoptosis, cell cycle arrest, and increased production of ROS.

Background The objectives of this study were to assess the maintenance of effect of duloxetine 60 mg once-daily (QD) in Chinese patients with chronic pain due to osteoarthritis (OA) of the knee or hip and to provide additional long-term safety data. Methods This was an open-label, extension phase of a randomized, double-blind, placebo-controlled clinical trial. Eligible patients were outpatients who met the American College of Rheumatology clinical and radiographic criteria for OA with a rating ≥4 on Brief Pain Inventory (BPI) 24-h average pain. After completing the 13-week placebo-controlled phase, patients originally assigned to placebo were titrated to duloxetine 60 mg QD (PLA_DLX), whereas patients originally assigned to duloxetine 60 mg QD remained on the same dose of duloxetine (DLX_DLX) for another 13 weeks. The maintenance effect of duloxetine 60 mg QD during the extension phase was evaluated by a 1-sided 97.5% confidence interval (CI) of the baseline-to-endpoint change in the extension phase for patients who took duloxetine and reported ≥30% reduction in BPI average pain at the end of placebo-controlled phase (placebo-controlled phase duloxetine responders). Other BPI severity and interference items, as well as safety and tolerability, were assessed. Results Of 342 patients entering the extension phase, 162 (97.6%) DLX_DLX-treated patients and 157 (89.2%) PLA_DLX-treated patients completed this phase. Most patients (76.0%) were female. Mean age was 60.6 years. Mean BPI average pain was 5.5 at baseline of the placebo-controlled phase. Among 113 placebo-controlled phase duloxetine responders, mean change in BPI average pain during the extension phase was − 0.59 (from 2.47 to 1.88); the upper bound of the 1-sided 97.5% CI was − 0.31 and less than the pre-specified non-inferiority margin of a 1.5-point increase (p

Background The NAC (NAM, ATAF1/ATAF2, and CUC2) transcription factors belong to a large family of plant-specific transcription factors in monocot and dicot species. These transcription factors regulate the expression of stress tolerance-related genes that protect plants from various abiotic stresses, including drought, salinity, and low temperatures. Results In this study, we identified the CaNAC46 transcription factor gene in Capsicum annuum. Its open reading frame was revealed to comprise 921 bp, encoding a protein consisting of 306 amino acids, with an isoelectric point of 6.96. A phylogenetic analysis indicated that CaNAC46 belongs to the ATAF subfamily. The expression of CaNAC46 was induced by heat, cold, high salt, drought, abscisic acid, salicylic acid, and methyl jasmonate treatments. Thus, CaNAC46 may be important for the resistance of dry pepper to abiotic stresses. A subcellular localization analysis confirmed that CaNAC46 is localized in the nucleus. The overexpression of CaNAC46 improved the tolerance of transgenic Arabidopsis thaliana plants to drought and salt stresses. The CaNAC46-overexpressing lines had longer roots and more lateral roots than wild-type lines under prolonged drought and high salt stress conditions. Additionally, CaNAC46 affected the accumulation of reactive oxygen species (ROS). Moreover, CaNAC46 promoted the expression of SOD, POD, RD29B, RD20, LDB18, ABI, IAA4, and P5CS. The malondialdehyde contents were higher in TRV2-CaNAC46 lines than in wild-type plants in response to drought and salt stresses. Furthermore, the expression levels of stress-responsive genes, such as ABA2, P5CS, DREB, RD22, CAT, and POD, were down-regulated in TRV2-CaNAC46 plants. Conclusions Under saline and drought conditions, CaNAC46 is a positive regulator that activates ROS-scavenging enzymes and enhances root formation. The results of our study indicate CaNAC46 is a transcriptional regulator responsible for salinity and drought tolerance and suggest the abiotic stress-related gene regulatory mechanisms controlling this NAC transcription factor are conserved between A. thaliana and pepper.

The hydrolysis properties of lipase in castor was evaluated using two different substrate forms (tripalmitic glycerides and trioleic glycerides) to catalyze the reaction under different operational conditions. RcLipase was obtained from castor seeds and results show that RcLipase is a conservative serine lipase with a conserved catalytic center (SDH) and a conserved pentapeptide (GXSXG). This enzyme exhibited the greatest activity and tolerance to chloroform and toluene when it was expressed in Pichia pastoris GS115 at 40 ℃ and pH 8.0. Zn and Cu ions exerted obvious inhibitory effects on the enzyme, and displayed good hydrolytic activity for long-chain natural and synthetic lipids. HPLC analysis showed that this enzyme has 1,3 regioselectivity when glycerol tripalmitate and oleic acid are used as substrates. The fatty acid composition in the reaction product was 21.3% oleic acid and 79.1% sn-2 palmitic acid.

A pyrimidine moiety exhibiting a wide range of pharmacological activities has been employed in the design of privileged structures in medicinal chemistry. To prepare libraries of novel heterocyclic compounds with potential biological activities, a series of novel 2-(pyridin-2-yl) pyrimidine derivatives were designed, synthesized and their biological activities were evaluated against immortalized rat hepatic stellate cells (HSC-T6). Fourteen compounds were found to present better anti-fibrotic activities than Pirfenidone and Bipy55&prime, DC. Among them, compounds ethyl 6-(5-(p-tolylcarbamoyl)pyrimidin-2-yl)nicotinate (12m) and ethyl 6-(5-((3,4-difluorophenyl)carbamoyl)pyrimidin-2-yl)nicotinate (12q) show the best activities with IC50 values of 45.69 &mu, M and 45.81 &mu, M, respectively. Furthermore, the study of anti-fibrosis activity was evaluated by Picro-Sirius red staining, hydroxyproline assay and ELISA detection of Collagen type I alpha 1 (COL1A1) protein expression. Our study showed that compounds 12m and 12q effectively inhibited the expression of collagen, and the content of hydroxyproline in cell culture medium in vitro, indicating that compounds 12m and 12q might be developed the novel anti-fibrotic drugs.

Sulfur-Doped graphene has attracted significant attention because of its potential uses in sensors, catalysts, and energy storage applications. In conventional approaches, the sulfur-doped graphene is fabricated with graphene oxide and sulfur-containing compounds through thermal annealing or hydrothermal process, which generally involves special equipment and heat treatment, and requires additional stabilizers to make it solution-processable. In this work, we report a facile one-step approach to synthesize water-dispersible sulfur-doped reduced graphene oxide (S-rGO). Graphene oxide (GO) could be readily reduced and converted to S-rGO simultaneously by directly mixing GO dispersion with hydrosulfide hydrate (NaSH·xH2O) at room temperature. The sulfur doping is confirmed by high resolution S 2p XPS spectrum and element mapping. The colloidal dispersion state of S-rGO is confirmed by the investigation of Tyndall effect, the zeta potential and particle size distribution measurement. Compared with previously reported strategies, NaSH can initiate the reduction and sulfur doping at room temperature, demand no heat treatment, require no equipment and form stable aqueous S-rGO dispersion without using any stabilizer. These advantages will facilitate large-scale production of water-dispersible (sulfur doped) graphene and further boost their applications in sensors, catalysts and energy storage devices.

Bio-based adhesives have low water resistance and they are less durable than synthetic adhesives, which limits their exterior applications. In this study, a bio adhesive was developed from soybean meal and larch tannin that was designed for exterior use. Phenol hydroxymethylated tannin oligomer (PHTO) was synthesized and then mixed with soybean meal flour in order to obtain a soybean meal-based adhesive (SPA). The results showed that the moisture absorption rate, residual rate, and solid content of SPA with 10 wt % PHTO (mass ratio with respect to the entire adhesive) were improved by 22.8%, 11.6%, and 6.8%, respectively, as compared with that of pure SPA. The wet shear strength of plywood with SPA with 10 wt % PHTO (boiling in 100 &deg, C water for 3 h) was 1.04 MPa when compared with 0 MPa of pure SPA. This met the bond strength requirement of exterior-use plywood (GB/T 9846.3-2004). This improved adhesive performance was mainly due to the formation of a crosslinked structure between the PHTO and the protein and also PHTO self-crosslinking. The formaldehyde emission of the resulting plywood was the same as that of solid wood. The PHTO-modified SPA can potentially extend the applications of SPAs from interior to exterior plywood.

Background CYP3A29 is crucial for drug metabolism in pigs and an important research model of human CYP3A4. Recent studies have shown that some probiotics can regulate the expression of CYP3A in mammals, but the mechanisms underlying their action are unclear. This study explored whether Enterococcus faecium HDRsEf1 could modulate the expression of CYP3A29 in pig intestine and potential mechanisms. Results we found that HDRsEf1 significantly reduced CYP3A29 expression in pig intestinal tissues and epithelial cells, dependent on cell-cell contact. In IPEC-J2 cells, HDRsEf1 treatment decreased the transcription activity of the CYP3A29 promoter, RXR-α expression and abrogated or mitigated the RXR-α or PXR over-expression-increased CYP3A29 expression. Both RXR-α/PXR over-expression synergistically increased CYP3A29 expression while RXR-α or PXR silencing reduced CYP3A29 expression. Co-immunoprecipitation revealed that RXR-α directly interacted with PXR. HDRsEf1, like a NF-kB inhibitor, significantly decreased the NF-kBp65 activation, RXR-α and CYP3A29 expression, which were abrogated by RXR-α silencing. The down-regulated CYP3A29 expression by HDRsEf1 was associated with increased A20 expression, which were abrogated by TLR1/2 silencing. Conclusions HDRsEf1 inhibits the expression of CYP3A29 through the TLR1/2-induced A20 to attenuate the NF-κB/RXR-α signaling in pig intestinal tissues. Our findings may provide new insights into the mechanisms by which probiotics regulate the expression of CYP450s, and suggest potential risks in the clinical application of probiotics

Contrast-induced acute kidney injury (CI-AKI) is a severe complication caused by intravascular applied radial contrast media (CM). Pyroptosis is a lytic type of cell death inherently associated with inflammation response and the secretion of pro-inflammatory cytokines following caspase-1 activation. The aim of the present study was to investigate the protective effects of acetylbritannilactone (ABL) on iopromide (IOP)-induced acute renal failure and reveal the underlying mechanism. In vivo and in vitro, IOP treatment caused renal damage and elevated the caspase-1 (+) propidium iodide (PI) (+) cell count, interleukin (IL)-1β and IL-18 levels, lactate dehydrogenase (LDH) release, and the relative expression of nucleotide-binding domain, leucine-rich repeat containing protein 3 (NLRP3), apoptosis-associated speck-like protein (ASC), and gasdermin D (GSDMD), suggesting that IOP induces AKI via the activation of pyroptosis. Furthermore, the pretreatment of ABL partly mitigated the CI-AKI, development of pyroptosis, and subsequent kidney inflammation. These data revealed that ABL partially prevents renal dysfunction and reduces pyroptosis in CI-AKI, which may provide a therapeutic target for the treatment of CM-induced AKI.

Schiff bases are generally utilized to detect and quantitatively analyze metallic cations and anions. However, pesticide detection based on Schiff base structure has not been reported so far. Mesotrione is a kind of triketone 4-hydroxy-phenyl-pyruvate-dioxygenase (HPPD) inhibitor whereas excessive use of mesotrione produces residues causing a negative impact on the environment. Herein, we report a Schiff base type probe 6-(2-hydroxybenzylidene)-N-n-butyl-naphthalimide (HNA) which can switch on in a fluorescence mode in response to mesotrione efficiently, enabling the quantification of testing sample. It is worth mentioning that the simple and direct cleavage of the targeted carbon–nitrogen double bond of Schiff base in probe is proved to be triggered by acetophenyl unit in mesotrione which may be ascribed from the competition equilibrium between the intramolecular and intermolecular hydrogen bonds. As a result, the non-fluorescent probe with photo-induced electron transfer process is converted to the precursor of the probe with strong fluorescence. Further results reveal that the strong electronegativity of carbonyl carbon atom in acetophenone group is capable of improving the detection capability of probe. Aided by the switch-on change of fluorescence, the quantitative determination of mesotrione is realized with the limit of detection (LOD) of 0.16 μM with potentials of quantitative sensing in real water samples. Moreover, two other probes bearing pyrene and Schiff base structure are synthesized and exhibit the feasibility of mesotrione detection with LODs of 0.43 μM and 3.20 μM, respectively. The present work provides a novel and convenient method for the detection of mesotrione with high sensitivity and easy operation based on the probe with general C = N of Schiff base structure, which greatly benefit for the future research regarding to the acetophenone-type herbicide sensing.

Silver and carbon coated NaTi2(PO4)3 is synthesized via a facile sol-gel method, with polyvinyl alcohol as carbon source and silver nitrate as Ag source. NaTi2(PO4)3@C/Ag is characterized by XRD, SEM, TEM, EDS and XPS. It can be found that C/Ag composite layer is uniformly coated on the surface of NaTi2(PO4)3. Compared with the pure NaTi2(PO4)3, NaTi2(PO4)3@C/Ag material demonstrates significantly higher rate capability and cycling stability. It can deliver an initial discharge capacity of 126.5 mA h g−1 at a current rate of 2 C with the capacity retention of 94.5% after 100 cycles. It can still deliver an initial discharge capacity of 97.5 mA h g−1 at a current rate of 5 C with a substantial capacity retention of 83.8% after 400 cycles. It is worth mentioning that NaTi2(PO4)3@C/Ag also exhibits pretty good rate capacity. When the current density ranges from 1 C, 2 C, 5 C, 10 C and finally back to 1 C, NaTi2(PO4)3@C/Ag electrode still retains a discharge capacity of 84.6 mAh g−1 after 200 cycles at 5 C corresponding to a capacity retention ratio of 83.5%.

KxCu1−xO1−γ (0 ≤ x ≤ 0.12) and K0.08Cu0.92O1−γ anode materials are synthesized via a simple ethylene glycol assisted sol-gel method and characterized by X-ray diffraction, Scanning Electron Microscopy, High-resolution/Transmission Electron Microscopy, Energy Dispersive Spectroscopy and Select Area Electron Diffraction. The introduction of potassium element improves the electro-chemical performance of CuO greatly, especially for x = 0.08. After Ag coating, K0.08Cu0.92O1−γ@Ag anode displays superior electro-chemical performance with excellent reversible capacity, cyclic performance and rate capability. It delivers a capacity of 804.3 mA h g−1 even at the 50th cycle. The role played by the K element doping and Ag coating are fully discussed.

The perovskite type oxide Ca1-xLixMnO3-δ (x = 0, 0.02, 0.05, 0.1, 0.2) was prepared by a simple citric acid assisted sol-gel method and was investigated as a possible lithium ion anode material. XRD confirmed that up to 10% calcium element in the CaMnO3 lattice can be replaced by lithium without the obvious corruption of lattice symmetry or the appearance of the secondary phase. Although pure CaMnO3 exhibited poor electro-chemical performance, the introduction of lithium has greatly improved the electrochemical performance of Ca1-xLixMnO3-δ. Without carbon coating, the specific capacity of Ca0.95Li0.05MnO3-δ within the initial 10 cycles were maintained at ca. 480 mA h g−1, and after 50 cycles of rate capability testing it was estimated to be around 350 mA h g−1. The rate capability was also improved significantly. The detailed structural analysis of lithium doping CaMnO3 revealed that this improvement in the electro-chemical performance mostly likely originated from the extra lithium diffusion path between two 8c sites mediated by the 36 f oxygen vacancy in between. Further EIS and CV tests demonstrated that the lithium doping reduced the charge transfer resistance effectively and increased the lithium ion diffusion coefficient accordingly. Although the performance of lithium doping CaMnO3 was still inferior to the frequently investigated anode material like Si series or metal oxide series, the further improvement of the material was still possible by further modification of perovskite CaMnO3.

Multisubstituted indoles were synthesized via a one-pot tandem copper-catalyzed Ullmann-type C-N bond formation/intramolecular cross-dehydrogenative coupling process at 130 °C in DMSO. The methodology allows practical and modular assembly of indoles in good to excellent yields from readily available aryl iodides and enamines.

Well-dispersed bimetallic RuCo alloy nanoparticles (NPs) were successfully immobilized on the multi-porous, water-tolerant metal organic frameworks MIL-53(Al) by a facile solvent impregnation method. Among the RuCo@MIL-53(Al) with different Ru/Co molar ratios, the Ru1Co1@MIL-53(Al) performed better and was superior to Ru@MIL-53(Al) and single RuCo NPs for the hydrolysis of ammonia borane (AB, NH3BH3), owing to the synergistic effect caused by the electronic and geometric interactions between Ru and Co atoms and bi-functional effect generated between the RuCo NPs and the MIL-53(Al) support. Compared with bimetallic Ru1Ni1 and Ru1Cu1 counterparts loadings, the Ru1Co1@MIL-53(Al) also showed better catalytic activity for the hydrolysis of AB. Moreover, the Ru1Co1@ MIL-53(Al) presented good durability and reusability in the catalytic reaction, and the activation energy (Ea) and turnover frequency values (TOF) were 34.32 kJ mol−1 and 87.24 mol H2 min−1 (mol Ru)−1, respectively.

A novel Schiff-base (HL) based on rhodamine B derivative was designed and synthesized as a highly selective and sensitive “turn-on” fluorescent probe for M 3+ (Cr 3+ , Fe 3+ , and Al 3+ ) in methanol. Upon addition of M 3+ , the spirolactam ring (colorless and nonfluorescent) of HL was opened to the ring-open forms (pink and orange-yellow fluorescence). These results indicated that HL could be used as a colorimetric and fluorescent probe for the detection of M 3+ with low detection limit of 0.63 μM (Cr 3+ ), 0.14 μM (Fe 3+ ), and 0.22 μM (Al 3+ ). The binding constant (Ka) of M 3+ binding to HL were calculated to be 0.87 × 10 4 M −1 (Cr 3+ ), 1.14 × 10 4 M −1 (Fe 3+ ), and 4.48 × 10 4 M −1 (Al 3+ ), respectively from a Benesi-Hildebrand plot. The binding stoichiometry between HL and M 3+ was determined from the Job’s plot (fluorescent spectrum) and ESI–MS spectrum data to be 1:1. Furthermore, the recognition process of the probe for M 3+ was chemically reversible on the addition of fluorinion (F − ).

To develop strong and tough bio-based composite films as replacements for synthetic polymer films is challenging. Based on the strong adhesion of the comb-like structure of geckos’ feet or pressure-sensitive resins on substrates, a comb-like polymer-aminated dialdehyde starch (A-DAS) was designed and prepared from polyamide polyamine polymer and dialdehyde starch via a Schiff-based reaction, and then combined with soy protein isolate (SPI) to develop a protein-based film. The comb-like A-DAS exhibited strong adhesion with SPI molecules by forming multiple hydrogen bonds, which created a noncovalent network that improved both the strength and toughness of the resultant film. The results showed that after integrating A-DAS (SPI:A-DAS weight ratio of 2:1), the tensile strength of the film dramatically increased by 1072.2% to 25.09 MPa, which is markedly better than that of other reported protein-based films. The toughness of the SPI/A-DAS film increased to 16.74 MJ/m3. Notably, the modified film could block 100% of the ultraviolet transmittance (

The main protection mechanism of anti-corrosion coatings was to shield and hinder corrosive media. When inorganic flake fillers were added to improve the anti-corrosion performance of the coatings, it was necessary to solve the problem of inorganic-organic compatibility. This paper combined the barrier properties of flaky and chemically inert basalt scales with the corrosion inhibition of aniline trimers, and prepared aniline trimers modified basalt scales to improve the anticorrosion performance of the coatings. Aniline trimer was conducive to the compatibility and dispersion of basalt flakes in epoxy resin. The enhancement of shielding and anti-corrosion performance of the coatings was attributed to the dispersed distribution of basalt flakes, which reduced the water content and diffusion rate in coatings. Aniline trimer acted as the corrosion inhibitor. When corrosive media penetrated the coatings, it adsorbed on the metal surface and formed protective films, thereby enhancing the corrosion resistance of the coatings. The aniline trimer modified basalt flakes increased the anti-corrosion resistance of epoxy coatings by two orders of magnitude, and its optimal mass content was about 10%.

By an effective energy model in the device under laser single event effects (SEE) test, a two-photon absorption (TPA) of pulsed laser energy transmission mechanism model vs heavy ion linear energy transfer (LET) for SEE have been established. Based on 4H Silicon Carbide (4H-SiC) diodes material parameters which should be considered for SEE) irradiated by TPA of pulsed laser, model for TPA of pulsed laser front-side SEE testing is built. Testing results show that model can give effective SEE laser energies. Meanwhile, relationship between effective laser energy and equivalent LET (ELET) has been validated. Single event transient (SET), permanent damage, and single event burnt-out (SEB) of 4H-SiC diode can be triggered by TPA of pulsed laser, and equivalent LET of pulsed laser energy is consistent with heavy ion LET.

Polyunsaturated fatty acid (PUFA) is important for the development of the fetal brain, and the retina. Gestational diabetes mellitus (GDM) may influence maternal and fetal fatty acid metabolism, in turn affecting fetal growth and development. In several studies, maternal and fetal PUFA metabolic differences have been reported between mothers with and without GDM, but not in other studies. Thus, the aim of this meta-analysis (registration number: CRD42020220448) was to compare levels of linoleic acid (LA), α-linolenic acid (ALA), arachidonic acid (AA), docosahexaenoic acid (DHA), and total n-3 and n-6 PUFA between mothers with and without GMD and their fetuses.We performed a meta-analysis of observational studies on maternal and fetal fatty acid metabolism, published until May 2021. In addition, we performed subgroup analysis depending on the analyzed tissues (plasma/serum, erythrocyte membrane, or placenta) and the expression modes of fatty acids (concentration or percentage).We included 24 observational studies involving 4335 maternal datasets and 12 studies involving 1675 fetal datasets in the meta-analysis. Levels of AA, DHA, and n-6 and n-3 PUFA were lower in the cord blood of mothers with GDM than in controls (P 0.05). Compared to that in controls, in erythrocyte membranes, the percentages of AA, DHA, and n-6 and n-3 PUFA in total fatty acid were lower in mothers with GDM (P 0.05), but in plasma/serum, the percentages of AA, DHA, and n-6 PUFA in total fatty acid were higher in mothers with GDM (P 0.05).GDM appears to influence the transfer of PUFAs from mothers to fetuses. The percentage of PUFAs in maternal plasma/serum was higher, and that in erythrocyte membranes was lower in mothers with GDM compared to those with normal glucose tolerance.

Boride-based ultra-high temperature ceramics have been extensively utilized as high temperature thermal protection materials due to its excellent physical and mechanical properties. Yet, the synthesis of boride-based ceramic powder with high purity, ultra-fine structure and excellent dispersity remains a great challenge to reach. In this work, zirconium diboride (ZrB2) ultra-high temperature ceramic powder with high purity and ultra-fine structure (size of hundreds of nanometers) was prepared by carbothermal reaction combined with sol-gel method. Various dispersants including oleic acid (OA), polyethylene glycol (PEG) and polyvinyl pyrrolidone (PVP) were employed during the preparation procedure to tune the physicochemical properties of the resultant ZrB2. According to the X-ray diffraction and microscopy characterizations, it was revealed that the OA turned up as the most effective dispersant to obtain the ZrB2 powder with hundreds-nanometer-scale and high purity. Besides, the thermogravimetry-differential thermal analysis and Fourier transformed infrared spectroscopy analysis were performed, unveiling the function of OA in enhancing the dispersity of the ZrB2. Such a work on the effect of dispersant on the preparation of ultra-high temperature ceramic powder could shed some important light for the development of high temperature resistant materials.

Listeria monocytogenes (L. monocytogenes), a psychrophilic and fatal foodborne zoonotic pathogen, with being one of the most common contaminants in foods, demands rapid and reliable detection techniques. Herein, we present a phosphatase (ALP)-mediated magnetic relaxation DNA biosensor enabling the rapid and sensitive analysis for L. monocytogenes in ham samples. The DNA probes were initially designed to specifically hybridize with targeted region of bacterial genomic DNA in L. monocytogenes, and the amount of ALP is related to the concentration of L. monocytogenes through DNA hybridization. Under enzyme-catalyzed reaction, ALP can induce Mn(VII) to convert into Mn(II). The valence state variation from Mn(VII) to Mn(II) results in a significant change of transverse relaxation time (T2) of surrounding water molecules, which can be used as an out-put of magnetic signal. Without any DNA amplification step, this magnetic biosensor could exhibit high sensitivity for L. monocytogenes detection with a linear range from 2 × 102 to 2 × 107 CFU mL−1, as well as a low detection limit (LOD) of 102 CFU mL−1. The constructed DNA biosensor, therefore, could offer an ideal candidate for the detection of food-borne pathogens with simple and reliable analytical performance.

Zn1-xCoxO (0 ≤ x ≤ 0.15) anode material was prepared by an easy polyacrylamide assisted sol-gel route. The successful replacement of Zinc by Cobalt within Cobalt content x ≤ 0.09 was confirmed by structural characterization. The introduction of Cobalt element greatly improved the electro-chemical performances of the matrix Zinc oxide. Without carbon coating, at the 20th cycle, Zn0.91Co0.09O anode still preserved a capacity a little bit more than 1000 mA h g−1 and a capacity more than 600 mA h g−1 was retained at the end of the 50th cycle. Better rate capability was also witnessed. The SEM, EIS at OCV, CV and in situ XRD were further carried out to elucidate the lithiation mechanism. The role Cobalt doping played can be summarized as follows: the stabilization of the Li2Zn phase, the minimization of charge transfer resistance and the enhanced reversibility of the reduction from metal oxide to metal.

High expression of glutaminyl cyclase (QC) contributes to the initiation of Alzheimer's disease (AD) by catalyzing the generation of neurotoxic pyroglutamate (pE)-modified β-amyloid (Aβ) peptides. Preventing the generation of pE-Aβs by QC inhibition has been suggested as a novel approach to a disease-modifying therapy for AD. In this work, a series of diphenyl conjugated imidazole derivatives (DPCIs) was rationally designed and synthesized. Analogues with this scaffold exhibited potent inhibitory activity against human QC (hQC) and good in vitro blood-brain barrier (BBB) permeability. Further assessments corroborated that the selected hQC inhibitor 28 inhibits the activity of hQC, dramatically reduces the generation of pE-Aβs in cultured cells and in vivo, and improves the behavior of AD mice.

Summary Objective We assessed the efficacy and safety of duloxetine (60 mg, once daily), compared with placebo, during a 13-week treatment period in Chinese patients with chronic pain due to osteoarthritis (OA). Design Patients were at least 40 years old (male or female) who met American College of Rheumatology clinical and radiographic criteria for the diagnosis of OA of the knee or hip. The primary efficacy measure in this phase 3, randomized, double-blind, placebo-controlled clinical trial was assessment of pain severity by the Brief Pain Inventory (BPI) 24-h Average Pain rating. The clinical trial was conducted at 17 study centers. Statistical approaches included mixed-effects model repeated measures and analysis of covariance. A Fisher exact test was applied to categorical variables. Results Of 407 patients randomized (duloxetine: N = 205; placebo: N = 202), 166 (81.0%) patients from the duloxetine group and 176 (87.1%) patients from the placebo group completed the 13-week treatment phase. The majority (76.4%) of patients was female; mean age was 60.5 years. Duloxetine-treated patients reported significant pain reduction, compared with placebo treatment, on the BPI 24-h Average Pain rating (least-squares mean (LS Mean) change from baseline to endpoint [95% confidence interval (CI)], duloxetine: −2.23; placebo: −1.73; difference = −0.50 [−0.80, −0.20]; P = 0.001). The incidence of discontinuations due to adverse events was 9.0% in duloxetine-treated patients and 4.5% in placebo-treated patients ( P = 0.109). Conclusions This study demonstrated the efficacy of duloxetine in Chinese patients with chronic pain due to OA. The safety profile of duloxetine observed in this study was consistent with that in previous duloxetine trials. This trial is registered with ClinicalTrials.gov (NCT01931475).

Herein three novel cobalt metal–organic frameworks (Co-MOFs) with similar ingredients, [Co(bib)(o-bdc)]∞ (1), [Co2(bib)2(m-bdc)2]∞ (2), and {[Co(bib)(p-bdc)(H2O)](H2O)0.5}∞ (3), have been synthesized from the reaction of cobalt nitrate with 1,4-bis(imidazol-1-yl)benzene (bib) and structure-related aromatic acids (1,2-benzenedicarboxylic acid = o-bdc, 1,3-benzenedicarboxylic acid = m-bdc, and 1,4-benzenedicarboxylic acid = p-bdc) by the solvothermal method. It is aimed to perform systematic research on the relationship among the conformation of benzoate acid, lattice dimension of Co-MOF, and pore diameter of MOF-derived carbon composite. Through the precursor strategy, Co-MOFs 1–3 have been utilized to synthesize porous cobalt@carbon nanotube composites (Co@CNTs). After the in situ gas-sulfurization, secondary composites CoS2@CNTs were successfully obtained, which kept similar morphologies of corresponding Co@CNTs without destroying previous highly dispersed structures. Co-MOFs and two series of composites...

Characteristics of ethanol solution’s vacuum flash under adsorption condition were investigated experimentally. The temperature of cooling medium, ethanol solution flow velocity, and ethanol solution concentration were varied as experimental parameters. Explore the effects of these parameters on ice making process via controlling a single parameter. As results showed, adsorption condition can effectively reduce the peak pressure of ice slurry generator at initial flash moment. This peak pressure just reaches the minimum (800 Pa) when the cooling medium temperature in adsorption chamber is at 30 °C. The larger ethanol solution velocity of flow, the higher pressure when the whole system is stable in the same ethanol solution concentration. When the ethanol solution flow rate (velocity of flow) is at 5 L/h, the ethanol solution temperature can be reduced to −9 °C, which is more conducive to the production of ice crystals, but it may have ice blocking phenomenon. Ethanol additives can promote the solution to cool the temperature below 0 °C, and the higher the concentration is, the lower the temperature is. But for this ice preparation system, when the solution concentration is at 5%, it is more favorable to produce ice crystals. Through the analysis of all experimental conditions, 10 L/h of ethanol solution flow rate with ethanol concentration of 5% is the best ice production condition under the adsorption conditions.