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In order to explore the effect of alloying on the microstructures and mechanical properties of AlCoCrFeNi2.1 eutectic high-entropy alloys (EHEAs), 0.1, 0.2, and 0.3 at.% V, Mo, and B were added to the AlCoCrFeNi2.1 alloy in this work. The effects of the elements and contents on the phase composition, microstructures, mechanical properties, and fracture mechanism were investigated. The results showed that the crystal structures of the AlCoCrFeNi2.1 EHEAs remained unchanged, and the alloys were still composed of FCC and BCC structures, whose content varied with the addition of alloying elements. After alloying, the aggregation of Co, Cr, Al, and Ni elements remained unchanged, and the V and Mo were distributed in both dendritic and interdendritic phases. The tensile strengths of the alloys all exceeded 1000 MPa when the V and Mo elements were added, and the Mo0.2 alloy had the highest tensile strength, of 1346.3 MPa, and fracture elongation, of 24.6%. The alloys with the addition of V and Mo elements showed a mixed ductile and brittle fracture, while the B-containing alloy presented a cleavage fracture. The fracture mechanism of Mo0.2 alloy is mainly crack propagation in the BCC lamellae, and the FCC dendritic lamellae exhibit the characteristics of plastic deformation. [ABSTRACT FROM AUTHOR]

In order to analyze the shear mechanism of the steel-fiber high-strength concrete corbels, a calculation model for the shear bearing capacity of steel-fiber-reinforced high-strength concrete corbels was proposed based on the modified compression field theory. Considering the existence of residual tensile stress in steel-fiber-reinforced concrete at crack locations, the cracked steel-fiber-reinforced concrete was treated as a continuous material. The constitutive relation of cracked steel-fiber-reinforced concrete and the local stress equilibrium equation were modified. It was compared with the results of 34 steel-fiber high-strength concrete corbels, including those in this paper. The predicted results were compared with the experimental values and the predictions of the Fattuhi model, Campione model, and Russo model to validate the rationality of the proposed model. The results revealed that the mean value between the experimental values and the predicted results of the proposed model is 1.104, with a variance of 0.003, showing good agreement. The proposed model can accurately predict the shear bearing capacity of steel-fiber-reinforced high-strength concrete corbels. [ABSTRACT FROM AUTHOR]

As a transfer member at the discontinuous place of vertical load, the deep beam has a complex stress mechanism and many influencing factors, such as compressive strength of concrete, shear span ratio, and reinforcement ratio. At the same time, the stress analysis principle of traditional shallow beams is no longer applicable to the design and calculation of deep-beam structure. The main purpose of this paper was to use the strut-and-tie model to analyze its stress mechanism, and to verify the applicability of the model. Nine high-strength concrete deep-beam specimens with longitudinal reinforcement with an anchor plate of the same size were tested by two-point concentrated loading method. The effects of shear span ratio (0.3, 0.6, and 0.9), longitudinal reinforcement ratio (0.67%, 1.05%, and 1.25%), horizontal reinforcement ratio (0.33%, 0.45%, and 0.50%), and stirrup reinforcement ratio (0.25%, 0.33%, and 0.50%) on the failure mode, deflection curve, characteristic load, crack width, steel bar, and concrete strain of the specimens were analyzed. The results showed that the failure mode of deep-beam specimens was diagonal compression failure. The normal section cracking load was about 15 to 20% of the ultimate load, and the inclined section cracking load was about 30~40% of the ultimate load. The shear span ratio increased from 0.3 to 0.9, and the bearing capacity decreased by 32.9%. When the longitudinal reinforcement ratio increased from 0.67% to 1.25%, the ultimate load increased by 42.6%. The shear span ratio and longitudinal reinforcement ratio have a significant effect on the bearing capacity of the high-strength concrete deep beams with longitudinal reinforcement with an anchor plate. The shear capacity of nine high-strength concrete deep-beam specimens with longitudinal reinforcement with an anchor plate was calculated by national standards, and the results were compared with the calculation results of the Tan–Tang model, the Tan–Cheng model, SSTM, and SSSTM. The analysis showed that the softened strut-and-tie model takes into account the softening effect of compressive concrete, and is a more accurate mechanical model, which can be applied to predict the shear capacity of high-strength concrete deep-beam members with longitudinal reinforcement with an anchor plate. [ABSTRACT FROM AUTHOR]

According to the shear capacity test results of six steel-fiber-reinforced high-strength concrete (SFHSC) corbels with welded-anchorage longitudinal reinforcement under concentrated load, the effects of shear span ratio and steel fiber volume fraction on the failure mode, cracking load and ultimate load of corbel specimens were analyzed. On the basis of experimental research, the shear transfer mechanism of corbel structure was discussed. Then, a modified softened strut-and-tie model (MSSTM), composed of the diagonal and horizontal mechanisms, was proposed, for steel-fiber-reinforced high-strength concrete corbels. The contributions of concrete, steel fiber and horizontal stirrups to the shear bearing capacity of the corbels were clarified. A calculation method for the shear bearing capacity of steel-fiber-reinforced high-strength concrete corbels was established and was simplified on this basis. The calculation results of the model were compared with the test values and calculation results of the GB50010-2010 code, the ACI318-19 code, the EN 1992-1-1 code and the CSA A23.3-19 code. The results showed that the concrete corbel with small shear span ratio mainly has two typical failure modes: shear failure and diagonal compression failure. With the increase in shear span ratio, the shear capacity of corbels decreases. Steel fiber can improve the ductility of a reinforced concrete corbel, but has little effect on the failure mode of the diagonal section. The calculated values of the national codes were lower than the experimental values, and the results were conservative. The theoretical calculation values of the shear capacity calculation model of the corbels were close to the experimental results. In addition, the model has a clear mechanical concept considering the tensile properties of steel-fiber-reinforced high-strength concrete and the influence of horizontal stirrups, which can reasonably reflect the shear transfer mechanism of corbels. [ABSTRACT FROM AUTHOR]

As short cantilever members, corbels are mainly used to transfer eccentric loads to columns. Because of the discontinuity of load and geometric structure, corbels cannot be analyzed and designed using the method based on beam theory. Nine steel-fiber-reinforced high-strength concrete (SFRHSC) corbels were tested. The width of the corbels was 200 mm, the cross-section height of the corbel column was 450 mm, and the cantilever end height was 200 mm. The shear span/depth ratios considered were 0.2, 0.3, and 0.4; the longitudinal reinforcement ratios were 0.55%, 0.75%, and 0.98%; the stirrup reinforcement ratios were 0.39%, 0.52%, and 0.785%; and the steel fiber volume ratios were 0, 0.75%, and 1.5%. According to the test results, this paper discusses the failure process and failure mode of corbel specimens with a small shear span/depth ratio and analyzes the effects of variables such as shear span/depth ratio, longitudinal reinforcement ratio, stirrup reinforcement ratio, and steel fiber volume content on the shear capacity of corbels. The shear capacity of corbels is significantly affected by the shear span/depth ratio, followed by the longitudinal reinforcement ratio and the stirrup reinforcement ratio. Moreover, it is shown that steel fibers have little impact on the failure mode and ultimate load of corbels, but can enhance the crack resistance of corbels. In addition, the bearing capacities of these corbels were calculated by Chinese code GB 50010-2010 and further compared with ACI 318-19 code, EN 1992-1-1:2004 code, and CSA A23.3-19 code, which adopt the strut-and-tie model. The results indicate that the calculation results by the empirical formula in the Chinese code are close to the corresponding test results, while the calculation method based on the strut-and-tie model of a clear mechanical concept yields conservative results, and hence the related parameter values must be further modified. [ABSTRACT FROM AUTHOR]

On the basis of the test results of nine steel-fiber high-strength concrete corbel specimens subjected to a vertical load, the influence of the steel fiber content on the shear performance of corbels was analyzed. The softened strut-and-tie model (SSTM) was used to analyze the shear strength of steel-fiber high-strength concrete corbels, taking into consideration the shear contribution of steel fibers. A calculation model for the shear strength of steel-fiber high-strength concrete corbels is proposed, and a database for 26 steel-fiber high-strength concrete corbels was created by using the model. The results obtained according to the codes ACI318-19, EC2, CSA A23.3-19 and the softened strut-and-tie model were compared with the experimental values to verify the rationality of the model. The findings showed that steel fiber can effectively limit the crack width and improve the crack morphology. The overall average value of the ratio between the experimental and the predicted strengths of the model was 1.082, and the variance was 0.004. The values predicted with the proposed calculation model were closer to the experimental values than those calculated according to the codes. This study provides a definite mechanical model that can reveal the shear mechanism of steel-fiber high-strength concrete. It can reasonably predict the shear strength of steel-fiber high-strength concrete corbels. [ABSTRACT FROM AUTHOR]

This study aimed to investigate the effects of perfluorooctanesulfonic acid (PFOS) exposure on glucose-stimulated insulin secretion (GSIS) of rat insulinoma (INS-1) cells and the potential protective effects of procyanidins (PC). The effects of PFOS and/or PC on GSIS of INS-1 cells were investigated after 48 h of exposure (protein level: insulin; gene level: glucose transporter 2 (Glut2), glucokinase (Gck), and insulin). Subsequently, the effects of exposure on the intracellular reactive oxygen species (ROS) activity were measured. Compared to the control group, PFOS exposure (12.5, 25, and 50 μM) for 48 h had no significant effect on the viability of INS-1 cells. PFOS exposure (50 μM) could reduce the level of insulin secretion and reduce the relative mRNA expression levels of Glut2, Gck, and insulin. It is worth noting that PC could partially reverse the damaging effect caused by PFOS. Significantly, there was an increase in ROS after exposure to PFOS and a decline after PC intervention. PFOS could affect the normal physiological function of GSIS in INS-1 cells. PC, a plant natural product, could effectively alleviate the damage caused by PFOS by inhibiting ROS activity. [ABSTRACT FROM AUTHOR]

Standardized treatment guidelines and effective drugs are not available for human triple-negative breast cancer (TNBC). Many efforts have recently been exerted to investigate the efficacy of natural compounds as anticancer agents owing to their low toxicity. However, no study has examined the effects of isobavachalcone (IBC) on the programmed cell death (PCD) of human triple-negative breast MDA-MB-231 cancer cells. In this study, IBC substantially inhibited the proliferation of MDA-MB-231 cells in concentration- and time-dependent manners. In addition, we found that IBC induced multiple cell death processes, such as apoptosis, necroptosis, and autophagy in MDA-MB-231 cells. The initial mechanism of IBC-mediated cell death in MDA-MB-231 cells involves the downregulation of Akt and p-Akt-473, an increase in the Bax/Bcl-2 ratio, and cleaved caspases-3 induced apoptosis; the upregulation of RIP3, p-RIP3 and MLKL induced necroptosis; as well as a simultaneous increase in LC3-II/I ratio induced autophagy. In addition, we observed that IBC induced mitochondrial dysfunction, thereby decreasing cellular ATP levels and increasing reactive oxygen species accumulation to induce PCD. These results suggest that IBC is a promising lead compound with anti-TNBC activity. [ABSTRACT FROM AUTHOR]

A series of bakuchiol derivatives were synthesized and evaluated for their anti-proliferative and the inhibitory activities on SMMC7721 cell line migration using PX-478 as a positive control. The results showed (S,E)-4-(7-methoxy-3,7-dimethyl-3-vinyloct-1-en-1-yl)phenol (10) to have the best activity among the tested compounds, which included PX-478. In addition, compound 10 showed greater inhibitory activity than that of bakuchiol in the transwell migration and invasion assays at every dose. In western blotting tests, compound 10 showed a promising ability to downregulate the expression of HIF-1α and its associated downstream proteins MMP-2 and MMP-9. Moreover, this effect was dose-dependent and could represent a possible mechanism of action for the anticancer activity of compound 10. [ABSTRACT FROM AUTHOR]

Ginkgo biloba L. has been used in traditional Chinese medicine (TCM) for thousands of years. However, the anti-cancer properties of ginkgolic acids (GAS) isolated from G. biloba have not been investigated in human nasopharyngeal carcinoma cells. In this study, GAS exhibited an inhibitory effect on the ATPase activity of heat shock protein 90 (Hsp90) and anti-proliferative activities against four human cancer cell lines, with IC50 values ranging from 14.91 to 23.81 μg·mL−1. In vivo experiments confirmed that GAS inhibited tumor growth in CNE-2Z cell-xenografted nude mice with low hepatotoxicity. We further demonstrated that GAS suppressed migration and invasion and induced the apoptosis of CNE-2Z cells by inducing the degradation of Hsp90 client proteins (MMP-2, MMP-9, Her-2, c-Raf, Akt, and Bcl-2). Together, GAS are new Hsp90 inhibitors by binding to Hsp90 (hydrogen bond and hydrophobic interaction). Thus, GAS from G. biloba might represent promising Hsp90 inhibitors for the development of anti-nasopharyngeal carcinoma agents. [ABSTRACT FROM AUTHOR]

The morbidity and mortality caused by the globally prevalent human respiratory pathogen respiratory syncytial virus (RSV) approaches that world-wide of influenza. We previously demonstrated that the RSV matrix (M) protein shuttles, in signal-dependent fashion, between host cell nucleus and cytoplasm, and that this trafficking is central to RSV replication and assembly. Here we analyze in detail the nuclear role of M for the first time using a range of novel approaches, including quantitative analysis of de novo cell transcription in situ in the presence or absence of RSV infection or M ectopic expression, as well as in situ DNA binding. We show that M, dependent on amino acids 110–183, inhibits host cell transcription in RSV-infected cells as well as cells transfected to express M, with a clear correlation between nuclear levels of M and the degree of transcriptional inhibition. Analysis of bacterially expressed M protein and derivatives thereof mutated in key residues within M's RNA binding domain indicates that M can bind to DNA as well as RNA in a cell-free system. Parallel results for point-mutated M derivatives implicate arginine 170 and lysine 172, in contrast to other basic residues such as lysine 121 and 130, as critically important residues for inhibition of transcription and DNA binding both in situ and in vitro. Importantly, recombinant RSV carrying arginine 170/lysine 172 mutations shows attenuated infectivity in cultured cells and in an animal model, concomitant with altered inflammatory responses. These findings define an RSV M-chromatin interface critical for host transcriptional inhibition in infection, with important implications for anti-RSV therapeutic development. [ABSTRACT FROM AUTHOR]

Magnolol (MAG), a biphenolic neolignan, has various biological activities including antitumor effects. In this study, 15 MAG derivatives were semi-synthesized and evaluated for their in vitro anticancer activities. From these derivatives, compound 6a exhibited the best cytotoxic activity against four human cancer cell lines, with IC50 values ranging from 20.43 to 28.27 μM. Wound-healing and transwell assays showed that compound 6a significantly inhibited the migration and invasion of MDA-MB-231 cells. In addition, Western blotting experiments, performed using various concentrations of 6a, demonstrated that it downregulates the expression of HIF-1α, MMP-2, and MMP-9 in a concentration-dependent manner. Overall, these results suggest that substituting a benzyl group having F atoms substituted at the C2 position on MAG is a viable strategy for the structural optimization of MAG derivatives as anticancer agents. [ABSTRACT FROM AUTHOR]

A new series of mollugin-1,2,3-triazole derivatives were synthesized using a copper(I)-catalyzed Huisgen 1,3-dipolar cycloaddition reaction of corresponding O-propargylated mollugin with aryl azides. All the compounds were evaluated for their cytotoxicity on five human cancer cell lines (HL-60, A549, SMMC-7721, SW480, and MCF-7) using MTS assays. Among the synthesized series, most of them showed cytotoxicity and most of all, compounds 14 and 17 exhibited significant cytotoxicity of all five cancer cell lines. [ABSTRACT FROM AUTHOR]

Nasopharyngeal carcinoma (NPC) is a common malignant head and neck tumor. Drug resistance and distant metastasis are the predominant cause of treatment failure in NPC patients. Hispidulin is a flavonoid extracted from the bioassay-guided separation of the EtOH extract of Salvia plebeia with strong anti-proliferative activity in nasopharyngeal carcinoma cells (CNE-2Z). In this study, the effects of hispidulin on proliferation, invasion, migration, and apoptosis were investigated in CNE-2Z cells. The [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] (MTT) assay and the colony formation assay revealed that hispidulin could inhibit CNE-2Z cell proliferation. Hispidulin (25, 50, 100 μM) also induced apoptosis in a dose-dependent manner in CNE-2Z cells. The expression of Akt was reduced, and the expression of the ratio of Bax/Bcl-2 was increased. In addition, scratch wound and transwell assays proved that hispidulin (6.25, 12.5, 25 μM) could inhibited the migration and invasion in CNE-2Z cells. The expressions of HIF-1α, MMP-9, and MMP-2 were decreased, while the MMPs inhibitor TIMP1 was enhanced by hispidulin. Moreover, hispidulin exhibited potent suppression tumor growth and low toxicity in CNE-2Z cancer-bearing mice at a dosage of 20 mg/kg/day. Thus, hispidulin appears to be a potentially effective agent for NPC treatment. [ABSTRACT FROM AUTHOR]

The goal of this study was to determine the rat lens aldose reductase-inhibitory effects of 95% ethanol extracts from the leaves of C. esculenta and, its organic solvent soluble fractions, including the dichloromethane (CH2Cl2), ethyl acetate (EtOAc), n-butanol (BuOH) and water (H2O) layers, using dl-glyceraldehyde as a substrate. Ten compounds, namely tryptophan (1), orientin (2), isoorientin (3), vitexin (4), isovitexin (5), luteolin-7-O-glucoside (6), luteolin-7-O-rutinoside (7), rosmarinic acid (8), 1-O-feruloyl-d-glucoside (9) and 1-O-caffeoyl-d-glucoside (10) were isolated from the EtOAc and BuOH fractions of C. esculenta. The structures of compounds 1-10 were elucidated by spectroscopic methods and comparison with previous reports. All the isolates were subjected to an in vitro bioassay to evaluate their inhibitory activity against rat lens aldose reductase. Among tested compounds, compounds 2 and 3 significantly inhibited rat lens aldose reductase, with IC50 values of 1.65 and 1.92 μM, respectively. Notably, the inhibitory activity of orientin was 3.9 times greater than that of the positive control, quercetin (4.12 μM). However, the isolated compounds showed only moderate ABTS+ [2,29-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid)] activity. These results suggest that flavonoid derivatives from Colocasia esculenta (L.) Schott represent potential compounds for the prevention and/or treatment of diabetic complications.

A method combining hydrophilic interaction chromatography (HILIC) and electrospray ionization mass spectrometry (ESI-MS) was developed for the characterization and determination of natural Cordyceps. Separation was achieved on a Waters Xbridge Amide column with gradient elution. Identification of 15 target nucleosides and nucleobases was based on retention time, UV spectra and mass measurements of the protonated molecules ([M+H]⁺) and main fragment ions (ESI-TOF/MS). Eight non-target compounds were tentatively identified by ESI-TOF/MS. The 15 target compounds were quantified by HILIC-ESI-MS/MS using time-programmed selective ion monitoring or multiple reaction monitoring in positive-ion mode under optimized mass conditions. This technique showed good linearity, repeatability and recovery. This approach was also successfully implemented in the analysis of nucleosides and nucleobases in 12 batches of natural Cordyceps samples that were collected from different regions in China. The developed HILIC-ESI-MS method exhibited clear advantages in identifying and determining highly polar bioactive components in Cordyceps, as well as their quality control.

A new triphenylphosphine adduct of cyclopalladated ferrocenylpyridazine containing a chloride anion, 2a, has been synthesized from the reaction of the chloride-bridged palladacyclic dimer 1a with triphenylphosphine. The corresponding adducts 3a,b containing iodide anion have been readily prepared through anion exchange reactions of 2a,b with NaI in acetone. These complexes were characterized by elemental analysis, IR and 1H-NMR. Additionally, their crystal structures have been determined by X-ray diffraction and intermolecular C-H···X (Cl, Br, I) bonds were found in the crystals. The use of these palladacycles as catalysts for the Suzuki and Sonogashira reactions was examined. The complexes 2a,b exhibited higher catalytic activity than the corresponding 3a,b in the Suzuki reaction. However, the order of activity of adducts with varying halogen anions is 3a~3b > 2a~>2b in the Sonogashira reaction.