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Allergic rhinitis (AR) is a noninfectious inflammatory disease seriously affecting the quality of life. This study aimed to assess the efficacy of the Tuomin Zhiti decoction in allergic rhinitis and to provide a reference for clinical treatment. One hundred patients with AR treated in the Department of Otolaryngology of our hospital from January 2019 to December 2020 were recruited and assigned via a random number table method (1 : 1) to receive either oral loratadine and mometasone nasal spray (control group) or the Tuomin Zhiti decoction plus oral loratadine and mometasone nasal spray (study group). The total clinical efficacy was 86% (43/50) in the study group, which was significantly higher than that of 64% (32/50) in the control group. After treatment, the Total Nasal Symptoms Scores (TNSS) and Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ) scores between the two groups were similar, but 12 weeks after treatment, the study group had significantly lower TNSS and RQLQ scores than the control group. After treatment, the study group obtained lower levels of interleukin (IL)-4 and higher levels of interferon-γ (IFN-γ) than the control group. Significantly lower post-treatment peripheral blood eosinophil count (EOS) and eosinophil cationic protein (ECP) levels were observed in the study group in contrast to those of the control group. The Tuomin Zhiti decoction for the treatment of AR patients alleviates their clinical symptoms, reduces the inflammatory responses, enhances the immune function of patients by regulating IL-4 and IFN-γ, and lowers the long-term recurrence rate. [ABSTRACT FROM AUTHOR]

A series of novel 2-amino-4-aryl-pyrimidine derivatives of ursolic acid were designed, synthesized, and evaluated for their anticancer activities against four cancer cell lines (MCF-7, HeLa, HepG2, and A549) and a human hepatocyte cell line (LO2) via MTT assay. Among these derivatives, compound 7b exhibited potent cytotoxic activity against MCF-7 and HeLa cells with IC50 values of 0.48 ± 0.11 and 0.74 ± 0.13 μM, respectively, and substantially lower cytotoxicity to LO2 cells. Further cellular mechanism studies in MCF-7 cells elucidated that compound 7b could inhibit cell migration, induce cell cycle arrest at S phase and trigger mitochondrial-related apoptosis by increasing the generation of intracellular ROS and decreasing the mitochondrial membrane potential (MMP), which was associated with upregulation of the protein expression level of Bax and downregulation the level of Bcl-2 and the activation of caspase cascade. Western blot analyses also revealed that compound 7b could simultaneously suppress RAS/Raf/MEK/ERK and PI3K/AKT/mTOR signaling pathways, which could be responsible for the induction of apoptosis. Molecular docking study revealed that MEK1 kinase could be one of the possible targets of the title compounds. These results offered a promising scaffold for the investigation of novel targeted anticancer agents. [ABSTRACT FROM AUTHOR]

Aqueous zinc ion batteries (ZIBs) are considered as promising energy storage devices in the post-lithium-ion era, due to their high energy density, low cost, high safety, and environmental benignity, however their commercialization is hindered by the sluggish diffusion kinetics of cathode materials due to the large hydrate Zn2+ radius. In this work, we propose a unique structure inheritance strategy for preparing Bi2S3 micro-straws in which a metal–organic framework (MOF) denoted as Bi-PYDC (PYDC2− = 3,5-pyridinedicarboxylate) with a string of [Bi2O2]2+ chains is judiciously selected as the structure-directing template to induce the formation of micro-straws based on a topochemical reaction. The distinctive hollow structure significantly enhances the ionic storage kinetics. Impressively, the obtained battery exhibits an ultra-long cycle life of more than 10 000 cycles at a current density of 1 A g−1 while maintaining a capacity of more than 153.4 mA h g−1. In addition, the Zn2+ insertion/extraction mechanism of Bi2S3 micro-straws is also investigated by multiple analytical methods, revealing the involvement of Zn2+ rather than H+ in the electrochemical storage process. This work may lead a new direction for constructing high performance cathodes of Zn-ion batteries through a MOF-based structure-directing template. [ABSTRACT FROM AUTHOR]

Polymeric dielectric composites have wide applications in many fields ranging from wearable devices, sensors to energy storage. In this work, a novel kind of hybrid particles with ‘core-shell’-like structure were fabricated via the polydopamine-assisted deposition technology, in which the tetra-pod zinc oxide whisker (T-ZnOw) was the ‘core’ and the two-dimensional graphene oxide (GO) was the ‘shell’, while polydopamine (PDA) was the adhesion layer between T-ZnOw and GO. With the aid of PDA adhesion layer, the ‘core-shell’-like structure of the hybrid GO/PDA@T-ZnOw particles could be maintained in the poly(vinylidene fluoride) (PVDF) composites. Dielectric property measurements showed that the hybrid particles could be an excellent candidate to prepare the dielectric composites with excellent dielectric properties. There was a critical particle content (2.0–2.5 wt%) at which the composites exhibited the maximum dielectric constant and relatively low dielectric loss. Further results showed that GO and PDA@T-ZnOw particles had tremendous synergistic effect in enhancing the dielectric properties of the composites. The mechanisms for the largely enhanced dielectric constant were mainly related to the multiple interfaces in the composites, including the interfaces between GO and PVDF, between GO and PDA and between PDA and T-ZnOw, which provided more probability for interfacial polarization of the composites in the electrical field. This work presents a guideline to design high-performance dielectric composites with construction of the multiple interfaces. [ABSTRACT FROM AUTHOR]

Cerebral ischemia-reperfusion injury (CIRI) is associated with a poor neurological prognosis in patients who have experienced cardiac arrest (CA) and cardiopulmonary resuscitation (CPR). The aim of the current study was to investigate the potential role of a calpain inhibitor in CIRI using a rat model of CA. CA was induced in adult male Sprague-Dawley rats, and MDL28170 (a calpain inhibitor) was administered to the rats within 30 min after the return of spontaneous circulation. Differences between groups were evaluated by measuring survival rate, CPR duration and neurological deficit score. Hematoxylin-eosin staining and Nissl staining were performed to assess cerebral injury, and microstructure and autophagy were assessed by transmission electron microscopy. The levels of calpain-1, calpain-2, calpastatin, interleukin (IL)-1β, tumor necrosis factor (TNF)-α, P62, beclin-1 and LC3 in the brain tissues were determined using western blotting and double immunofluorescence staining. There was no significant difference in CPR duration or survival rate among the groups. At 24 h after CPR, the CA group demonstrated damaged tissue morphology; decreased neurological deficit scores, and P62 expression; and upregulated calpain-2, IL-1βp17, TNF-α, beclin-1 and LC3 levels in the cortex. However, MDL28170 improved neuronal function and suppressed inflammation and autophagy by inhibiting calpain-2 level, but there were no differences in the calpain-1 and calpastatin levels. These results suggest that calpain-2, inflammation and autophagy are involved in CA-induced CIRI. MDL28170 inhibited calpain-2 expression, inflammation and autophagy, which suggests its potential efficacy in treating post-CA nerve damage. [ABSTRACT FROM AUTHOR]

3D Bi2S3 materials were prepared by the trisodium citrate (Na3Cit)-assisted solvothermal method and applied to aqueous zinc ion batteries (AZIBs) to explore the effect of the electrode material morphology on the electrochemical performance. As the concentration of Na3Cit increases, the 3D assembly morphology evolves from coral-like to sphere-like to snowflake-like structures. The electrochemical test results show that the electrode materials of various morphologies possess excellent cycle life, but the specific capacity varies greatly depending on the morphology. Impressively, the Bi2S3-1.2 electrode has the best electrochemical performance, with a capacity of 203.5 mA h g−1 after 4000 charge/discharge cycles at 0.5 A g−1. Furthermore, the Bi2S3-1.2 electrode delivers an ultralong lifetime of over 10 000 cycles with a capacity of 150.2 mA h g−1 at 1 A g−1. This work demonstrates a feasible route to prepare ultra-long cycle life AZIBs. [ABSTRACT FROM AUTHOR]

The aggregation of anaerobic ammonium oxidation (anammox) bacteria is important for the start-up and biomass retention of anammox processes. However, it is unclear whether it is beneficial to the activity, growth and reproduction of anammox bacteria. In this study, four reactor systems were developed to explore the effects of aggregation on anammox activity, growth and reproduction, after excluding the contribution of aggregation to sludge settling and retention. Results demonstrated that (i) compared with free-living planktonic bacteria, the aggregated bacteria had a higher volumetric nitrogen removal rate (0.75 kg-N/(m³·d)) and specific nitrogen removal activity (1.097 kg-N/VSS/d). And after 67 days cultivation, it had the higher sludge concentration and relative abundance (92.4%); (ii) compared with acidic polysaccharides and α- d -glucopyranose polysaccharides, β- d -glucopyranose polysaccharide play more essential roles of anammox aggregation; (iii) norspermidine triggered the secretion of α- d -glucopyranose polysaccharides to combat the toxicity, and inhibited biomass growth rate; (iv) immobilization in polyvinyl alcohol (10%) or sodium alginate (2%) gel beads was better than sodium alginate-chitosan gel beads and norspermidine (biofilm inhibitor) for the cultivation of free-living planktonic anammox bacteria. This is the first comparative study of three methods for cultivating free-living anammox bacteria. In conclusion, we found that the aggregation of anammox sludge not only facilitates biomass retention but also enhances the bioactivity, relative abundance, growth, and reproduction rate of anammox bacteria. The work is helpful to understand the formation of anammox granular sludge and contribute to the fast start-up and stable operation in anammox application. [Display omitted] • Activity and growth of planktonic and aggregated anammox bacteria examined. • ACA and PVA-SA are compared for the first time for immobilizing anammox bacteria. • Roles of alkaline and acidic polysaccharides in anammox aggregation are elucidated. • β- d -glucopyranose polysaccharides play an essential role in anammox aggregation. • Norspermidine is proven to trigger secretion of α- d -glucopyranose polysaccharides. [ABSTRACT FROM AUTHOR]

Abstract: To study pharmacokinetic properties of puerarin poly(amido amine) (PAMAM) dendrimer complex, a sensitive liquid chromatography tandem mass spectrometry method (LC-MS/MS) was developed and validated to determine puerarin in rabbit aqueous humor using microdialysis sampling. Astilbin was used as the internal standard. The linear range for puerarin was from 2 to 1000ng/mL (r =0.9986) based on 20μL of aqueous humor. The coefficients of variations for intra-day and inter-day precisions were less than 10.0%, and the relative error of accuracy was within ±6.3%. The mean extraction recovery of puerarin varied from 80.4% to 85.5%. Microdialysis provides a complete concentration versus time profile. A significant difference was observed in main pharmacokinetic parameters of C max, AUC and t 1/2 between puerarin solution and puerarin PAMAM dendrimer complex. Complex formation resulted in an obvious increase in bioavailability of puerarin after topical administration to rabbit according to the above LC-MS/MS assay method. [Copyright &y& Elsevier]

Abstract: Field experimental studies on surge flow irrigation with sediment-laden water in northwestern China showed that a sealing layer was formed on the soil surface as a result of the sediments in the irrigation water going through a ‘trapping’, ‘settling’ and ‘sealing’ processes in the irrigated field. The sealing layer reduced the surface roughness and intake rate of the surface soil, and thus sped up the flow advance. Therefore, higher irrigation efficiency can be achieved with less irrigation water requirement. Analytical studies on water saving efficiencies indicated that the water saving effect of surge irrigation with sediment-laden water was achieved by an interactive impact of sediment content and the intermittent feature of surge flow, but the sediments effect was more pronounced. [Copyright &y& Elsevier]

[Display omitted] • A self-supported framework of GNPs and CNFs has been constructed. • The framework is well maintained in the epoxy composites. • Largely enhanced thermal conductivities in different directions are achieved. • The composites exhibit excellent friction performance. Thermally conductive epoxy composites have a broad range of applications in many fields relating to microelectronic devices and encapsulating materials of high-power electrical appliance. However, it is still a challenge to effectively fabricate thermally conductive epoxy composite materials that have various excellent comprehensive properties. In this work, a simple suction filtration method is developed to construct the self-supported framework of graphene nanoplatelets (GNPs) and carbon nanofibers (CNFs), and then epoxy is impregnated into the framework to prepare the composites. The morphological characterizations show that one dimensional CNFs exhibit the "supporting" effect between the parallelly arranged GNP layers in axial direction and the "bridging" effect between adjacent GNP aggregates in radial direction, and the self-supported framework is maintained in the epoxy composites. The highest thermal conductivities are 3.74 W/m·K in radial direction and 3.28 W/m·K in axial direction, at filler contents of 13.09 and 14.49 wt%, respectively, which are 1770% and 1540% higher than that of the pure epoxy. Further results show that the composite samples have high storage modulus, enhanced thermal resistance, and improved anti-friction performance, all of them ensure that the epoxy composites can be used as the materials of the components and parts of the electrical appliance toward continuous loading, vibration, and large heat dissipation. [ABSTRACT FROM AUTHOR]

[Display omitted] • A series of novel indolequinone derivatives of ursolic acid were synthesized. • Compound 6t exhibited the most potent antiproliferative activity. • Compound 6t inhibited cell migration and induced the apoptosis of MCF-7 cells. • Compound 6t inhibited PI3K/AKT/m-TOR signaling pathway in MCF-7 cells. A series of novel indolequinone derivatives of ursolic acid bearing ester, hydrazide, or amide moieties were designed, synthesized, and screened for their in vitro antiproliferative activities against three cancer cell lines (MCF-7, HeLa, and HepG2) and a normal gastric mucosal cell line (Ges-1). A number of compounds showed significant activity against tested cancer cell lines. Among them, compound 6t exhibited the most potent activity against three cancer cell lines with IC 50 values of 1.66 ± 0.21, 3.16 ± 0.24, and 10.35 ± 1.63 µM, respectively, and considerably lower cytotoxicity to Ges-1 cells. Especially, compound 6t could arrest cell cycle at S phase, suppress the migration of MCF-7 cells, elevate intracellular reactive oxygen species (ROS) level, and decrease mitochondrial membrane potential. Western blot analysis showed that compound 6t upregulated Bax, cleaved caspase-3/9, cleaved PARP levels and downregulated Bcl-2 level of MCF-7 cells. All these results indicated that compound 6t could significantly induce the apoptosis of MCF-7 cells. Meanwhile, compound 6t markedly decreased p-AKT and p-mTOR expression, which revealed that compound 6t probably exerted its cytotoxicity through targeting PI3K/AKT/mTOR signaling pathway. Therefore, compound 6t could be a promising lead for the discovery of novel anticancer agents. [ABSTRACT FROM AUTHOR]

• ERK and calpain-2 are activated in cerebral ischemia–reperfusion injury cases. • Neuroinflammation and necroptosis are involved in CIRI induced by CA/CPR. • PD98059 and MDL28170 can inhibit the ERK/calpain-2 pathway. • Inhibition of ERK/calpain-2 can reduce neuroinflammation and necroptosis after CIRI. Cerebral ischemia–reperfusion injury (CIRI) is the leading cause of poor neurological prognosis after cardiopulmonary resuscitation (CPR). We previously reported that the extracellular signal-regulated kinase (ERK) activation mediates CIRI. Here, we explored the potential ERK/calpain-2 pathway role in CIRI using a rat model of cardiac arrest (CA). Adult male Sprague-Dawley rats suffered from CA/CPR-induced CIRI, received saline, DMSO, PD98059 (ERK1/2 inhibitor, 0.3 mg/kg), or MDL28170 (calpain inhibitor, 3.0 mg/kg) after spontaneous circulation recovery. The survival rate and the neurological deficit score (NDS) were utilized to assess the brain function. Hematoxylin stain, Nissl staining, and transmission electron microscopy were used to evaluate the neuron injury. The expression levels of p-ERK, ERK, calpain-2, neuroinflammation-related markers (GFAP, Iba1, IL-1β, TNF-α), and necroptosis proteins (TNFR1, RIPK1, RIPK3, p-MLKL, and MLKL) in the brain tissues were determined by western blotting and immunohistochemistry. Fluorescent multiplex immunohistochemistry was used to analyze the p-ERK, calpain-2, and RIPK3 co-expression in neurons, and RIPK3 expression levels in microglia or astrocytes. At 24 h after CA/CPR, the rats in the saline-treated and DMSO groups presented with injury tissue morphology, low NDS, ERK/calpain-2 pathway activation, and inflammatory cytokine and necroptosis protein over-expression in the brain tissue. After PD98059 and MDL28170 treatment, the brain function was improved, while inflammatory response and necroptosis were suppressed by ERK/calpain-2 pathway inhibition. Inflammation activation and necroptosis involved in CA/CPR-induced CIRI were regulated by the ERK/calpain-2 signaling pathway. Inhibition of that pathway can reduce neuroinflammation and necroptosis after CIRI in the CA model rats. [ABSTRACT FROM AUTHOR]

In order to improve the fe rrous ion-dependent ni trate r emoval (FeNiR) process, hexametaphosphate chelated ferrous ion was used as substrate to replace the free ferrous ion. With hexametaphosphate chelated ferrous ion as substrate, the influent pH was adjusted to 6.8, and as a result a higher effluent pH (7.2) was detected. The v olumetric r emoval r ate (VRR) of nitrate kept at 0.42 ± 0.03 kg-N/(m3∙d) for 48 days and the corresponding nitrogen removal efficiency was 94.39 ± 4.57%. After 88 days of cultivation, FeNiR granules became small because of the oligotrophic substrate. The transmission electron microscope (TEM) analysis showed that less iron encrustation was formed on the surface or in the periplasm of FeNiR cells. The linear curve of the living cell percentage versus time showed that the death rate of FeNiR cells with chelated ferrous ion as substrate was much lower than that with free ferrous ion as substrate (0.4210 vs 0.9221). Without iron encrustation, both the FeNiR activity and al kaline p hosphatase (ALP) activity of FeNiR cells kept at high level and thus the efficiency of the FeNiR reactor kept stable and high. With hexametaphosphate chelated ferrous ion as substrate, the pH in bulk liquid was high (pH = 7.2) resulting in the high FeNiR rate, and less iron encrustation was formed around cells ensuring the stability of high FeNiR rate. Therefore, using hexametaphosphate chelated ferrous ion as substrate was an efficient way to improve the FeNiR process. Image 1 • With chelating Fe(II) as substrate the FeNiR rate kept at 0.42 kg-N/(m3∙d) for 48 days. • Chelating Fe(II) allowed a high pH (7.2) in reactor thus resulted in the high FeNiR rate. • Chelating Fe(II) caused few iron encrustation thus the high FeNiR rate kept stable. [ABSTRACT FROM AUTHOR]

In this paper, a turn-on fluorescent probe (DBE) was designed and synthesized for probing bisulfite (HSO3−) by coupling dehydroabietic acid-based benzimidazole derivatives with ethyl cyanoacetate moiety. The structure of the compound was characterized using its UV-Vis, 1H-NMR, 13C-NMR and HRMS spectra. The probe showed significant selectivity and sensitivity towards HSO3− compared to other analytes in DMF/PBS buffer (3/7, v/v, 10 mM, pH = 7.4), and exhibited a detection limit at the nanomolar level (3.2 nM), fast response time (140 s) and good pH stability (6–10) in living systems. Furthermore, this probe was successfully utilized for the fluorescence imaging of HSO3− in living zebrafish and MCF-7 cells with remarkable lysosome-targeting properties. [ABSTRACT FROM AUTHOR]

With the expectation of finding new and effective antitumor drugs, a series of novel N‐(1H‐benzo[d]imidazole‐2‐yl)‐benzamide/benzenesulfonamide derivatives of dehydroabietic acid were synthesized and evaluated for cytotoxic activity against three human cancer cell lines (MCF‐7, HeLa, and HepG2 cells) and one human normal hepatocyte cell line (LO2). As a result, a number of derivatives showed moderate to good antitumor activities. Among them, compound 8h exhibited the most potent activities against three cancer cell lines with IC50 values of 0.87 ± 0.18, 9.39 ± 0.72, and 8.31 ± 0.64 μM, respectively, and was less active to normal hepatocyte LO2 cells. Further mechanism studies revealed that compound 8h could arrest the cell cycle of MCF‐7 cells at S phase and induce the apoptosis of MCF‐7 cells in ROS‐mediated mitochondrial pathway. [ABSTRACT FROM AUTHOR]

Cell elongation and secondary wall deposition are two consecutive stages during cotton fiber development. The mechanisms controlling the progression of these two developmental phases remain largely unknown. Here, we report the functional characterization of the actin-bundling protein GhFIM2 in cotton fiber. Overexpression of GhFIM2 increased the abundance of actin bundles, which was accompanied with accelerated fiber growth at the fast-elongating stage. Meanwhile, overexpression of GhFIM2 could propel the onset of secondary cell wall biogenesis. These results indicate that the dynamic rearrangement of actin higher structures involving GhFIM2 plays an important role in the development of cotton fiber cells. [ABSTRACT FROM AUTHOR]

Sugars are involved in plant growth, fruit quality, and signaling perception. Therefore, understanding the mechanisms involved in soluble sugar accumulation is essential to understand fruit development. Here, we report that MdPFPβ, a pyrophosphate‐dependent phosphofructokinase gene, regulates soluble sugar accumulation by enhancing the photosynthetic performance and sugar‐metabolizing enzyme activities in apple (Malus domestica Borkh.). Biochemical analysis revealed that a basic helix‐loop‐helix (bHLH) transcription factor, MdbHLH3, binds to the MdPFPβ promoter and activates its expression, thus promoting soluble sugar accumulation in apple fruit. In addition, MdPFPβ overexpression in tomato influenced photosynthesis and carbon metabolism in the plant. Furthermore, we determined that MdbHLH3 increases photosynthetic rates and soluble sugar accumulation in apple by activating MdPFPβ expression. Our results thus shed light on the mechanism of soluble sugar accumulation in apple leaves and fruit: MdbHLH3 regulates soluble sugar accumulation by activating MdPFPβ gene expression and coordinating carbohydrate allocation. [ABSTRACT FROM AUTHOR]

The solubility of β-HMX in acetone + water mixed solvents was measured using a synthetic method. The laser monitoring observation technique was used to determine the disappearance of the solid phase in a solid + liquid mixture. All data were measured at atmospheric pressure and at temperatures ranging from (293.15 to 313.15) K. The effects of solvent composition and temperature on the solubility are discussed. The experimental data were correlated with an empirical equation. [ABSTRACT FROM AUTHOR]

A Mn18Cr2 steel containing TiN precipitates was fabricated by vacuum induction melting. The morphology of TiN precipitates and the interface orientation relationship between TiN and γ-Fe were characterized by means of SEM, TEM and SAED, and the formation mechanism of TiN precipitates in Mn18Cr2 steel was clarified. Results show that the TiN precipitates are more likely to exhibit a cubic-shaped morphology and form both within the grain and at the grain boundary of γ-Fe. The interface orientation relationship between TiN and γ-Fe is determined as follows: . Because of the smallest interfacial misfit, the secondary close-packed lane {100} of TiN preferentially combines with the close-packed plane {111} of γ-Fe during the precipitation in order to minimize the interface energy. After nucleation, the TiN precipitates exhibit cubic appearance due to the fact that the TiN has a FCC structure with rock salt type structure. This study provides reference for the material design of the austenitic high-manganese steels with excellent yield strength. [ABSTRACT FROM AUTHOR]

The NLR family pyrin domain-containing 3 (NLRP3) inflammasome, which is composed of NLRP3, apoptosis-associated speck-like protein containing a CARD (ASC) and pro-caspase-1 protein complexes, is activated by the reactive oxygen species (ROS) that are associated with ischemia-reperfusion (I/R) and are involved in brain damage. Pomelo peel oil (PPO) exhibits antioxidant activity. However, it is unclear whether PPO is able to attenuate NLRP3 inflammasome-induced inflammation and pyroptosis. Healthy male Sprague-Dawley rats were subjected to 7 min of cardiac arrest via trans-esophageal electrical stimulation, followed by cardiopulmonary resuscitation (CPR). The rats were then treated with PPO prior to reperfusion for 24 h. Hematoxylin and eosin staining was used to evaluate brain tissue and cell damage. In the brain tissues, reactive oxygen species (ROS) were assayed, immunofluorescence was used to analyze the expression of NLRP3 and western blotting was performed to determine the expression levels of neuroenolase (NSE), NF-κB, interleukin-1β (IL-1β), gasdermin D (GSDMD) and the NLRP3 inflammasome. Treatment of the rats with PPO significantly decreased the pathological damage of the brain tissue and reduced the expression of NSE, production of ROS and secretion of NF-κB, NLRP3, IL-1β and GSDMD. In conclusion, these results demonstrate the ability of PPO to protect the brain against I/R injury in rats after CPR by a mechanism involving inhibition of the inflammation and pyroptosis mediated by NLRP3 inflammasome activation. [ABSTRACT FROM AUTHOR]

• Dehydroabietate-based fluorescent probe for Hg2+ and Fe3+ was synthesized and characterized. • Detection limits of the sensor were 31.0 nM and 31.2 nM for Hg2+ and Fe3+ ions, respectively. • The sensor have a wide pH range for ion detection (5 ~ 12), and a short response time (10 s). • Fluorescent imaging experiments using MCF-7 and SMCC-7721 cell were carried out successfully. A novel dehydroabietic acid-based fluorescent probe (DBH) containing 2,4-diarylbenzimidazole moiety was designed and synthesized, and the compound was characterized by its UV–Vis, FT-IR, 1H NMR, 13C NMR and ESI-MS spectra. DBH could be used for the detection of Fe3+ and Hg2+ through the selective fluorescence quenching in EtOH/H 2 O solution. The probe DBH showed excellent selectivity and sensitivity towards Fe3+ and Hg2+ over other metal ions. The limits of detection were calculated as 3.12 × 10−8 M and 3.10 × 10−8 M, respectively. Especially, DBH have a wide pH range for ion detection (5 ~ 12), and a short response time (10 s). Job's plot method in combination with ESI-MS and FT-IR spectra was used to determine the stoichiometry of DBH -Fe3+/Hg2+ complexes as both 2:1. Moreover, DBH exhibited low cytotoxicity to MCF-7 and SMCC-7721 cells (IC 50 > 100 μM). In the fluorescent cell imaging experiments, DBH could be used as a prominent intracellular probe for the detection of Fe3+ and Hg2+ in living cells. [ABSTRACT FROM AUTHOR]

Tuning the magnetic anisotropy of metal ions remains highly interesting in the design of improved single‐molecule magnets (SMMs). We herein report synthetic, structural, magnetic, and computational studies of four mononuclear CoII complexes, namely [Co(hfac)2(MeCN)2] (1), [Co(hfac)2(Spy)2] (2), [Co(hfac)2(MBIm)2] (3), and [Co(hfac)2(DMF)2] (4) (MeCN=acetonitrile, hfac=hexafluoroacetylacetone, Spy=4‐styrylpyridine, MbIm=5,6‐dimethylbenzimidazole, DMF=N,N‐dimethylformamide), with distorted octahedral geometry constructed from hexafluoroacetylacetone (hfac) and various axial ligands. By a building block approach, complexes 2–4 were synthesized by recrystallization of the starting material of 1 from various ligands containing solution. Magnetic and theoretical studies reveal that 1–4 possess large positive D values and relative small E parameters, indicating easy‐plane magnetic anisotropy with significant rhombic anisotropy in 1–4. Dynamic alternative current (ac) magnetic susceptibility measurements indicate that these complexes exhibit slow magnetic relaxation under external fields, suggesting field‐induced single‐ion magnets (SIMs) of 1–4. These results provide a promising platform to achieve fine tuning of magnetic anisotropy through varying the axial ligands based on Co(II) bis(hexafluoroacetylacetonate) complexes. [ABSTRACT FROM AUTHOR]

In this paper, a series of novel 1H-dibenzo[a,c]carbazole derivatives of dehydroabietic acid bearing different N-(piperazin-1-yl)alkyl side chains were designed, synthesised and evaluated for their in vitro anticancer activities against three human hepatocarcinoma cell lines (SMMC-7721, HepG2 and Hep3B). Among them, compound 10g exhibited the most potent activity against three cancer cell lines with IC50 values of 1.39 ± 0.13, 0.51 ± 0.09 and 0.73 ± 0.08 µM, respectively. In the kinase inhibition assay, compound 10g could significantly inhibit MEK1 kinase activity with IC50 of 0.11 ± 0.02 µM, which was confirmed by western blot analysis and molecular docking study. In addition, compound 10g could elevate the intracellular ROS levels, decrease mitochondrial membrane potential, destroy the cell membrane integrity, and finally lead to the oncosis and apoptosis of HepG2 cells. Therefore, compound 10g could be a potent MEK inhibitor and a promising anticancer agent worthy of further investigations. [ABSTRACT FROM AUTHOR]

In this article, a series of novel quinoline derivatives of ursolic acid (UA) bearing hydrazide, oxadiazole, or thiadiazole moieties were designed, synthesised, and screened for their in vitro antiproliferative activities against three cancer cell lines (MDA-MB-231, HeLa, and SMMC-7721). A number of compounds showed significant activity against at least one cell line. Among them, compound 4d exhibited the most potent activity against three cancer cell lines with IC50 values of 0.12 ± 0.01, 0.08 ± 0.01, and 0.34 ± 0.03 μM, respectively. In particular, compound 4d could induce the apoptosis of HeLa cells, arrest cell cycle at the G0/G1 phase, elevate intracellular reactive oxygen species level, and decrease mitochondrial membrane potential. In addition, compound 4d could significantly inhibit MEK1 kinase activity and impede Ras/Raf/MEK/ERK transduction pathway. Therefore, compound 4d may be a potential anticancer agent and a promising lead worthy of further investigation. [ABSTRACT FROM AUTHOR]

Using dicyanamides, three two-dimensional coordination polymers (CPs) [CuII(valdmpn)LnIII(μ-1,5-dca)3]n (LnIII = Gd (1), Tb (2) and Dy (3)) were synthesized and characterized. Compounds 1–3 are two-dimensional coordination polymers bridged with μ-1,5-dca connecting the [CuII(valdmpn)LnIII]3+ units. In compounds 1–3, the Cu atom was pentacoordinated with an elongated square pyramidal (C4v) geometry, while the Ln (Gd, Tb and Dy) atom was nine-coordinated with a muffin (Cs) geometry. Detailed direct current (dc) magnetic measurements and simulated data demonstrated the existence of a ferromagnetic CuII–GdIII interaction for compound 1. Alternating current (ac) magnetic measurements revealed that compound 2 exhibited a slow magnetic relaxation behavior under a zero dc field. A hysteresis loop at 1.8 K was observed in compound 2, characteristic of typical single-molecule magnets (SMMs). However, compound 3 showed a slow magnetic relaxation behavior under a dc field. This system provides a good opportunity to determine the character of the Ln(III) ions incorporated and/or the origin of the slow magnetic relaxation behavior. [ABSTRACT FROM AUTHOR]

Ferrous ion can be used as electron donor for denitrification in the ferrous ion-dependent nitrate removal (FeNiR). To prevent the FeNiR performance decrease caused by iron encrustation, a modified FeNiR process with batch sludge replacement was developed. Based on the decay kinetics of sludge mass and sludge activity, the sludge retention time (SRT) was determined as 40 days in the modified FeNiR process. To keep the FeNiR rate at 0.70 kg-N/(m3·d), the sludge replacement amount was 25% of total sludge every 10 days. The FeNiR efficiency stabilized around 70%. The batch sludge replacement could be an effective method to offset the active sludge decay caused by iron encrustation, and therefore led to the good FeNiR performance. The wasted FeNiR sludge was found to adsorb phosphate at a rate of 0.9 mg-P/(g VS min). The modified FeNiR process was proposed to be coupled with phosphate removal, achieving the co-removal of nitrate and phosphate. The coupled technology is promising due to the less consumption of resources and energy, as well as the less production of excessive sludge. Unlabelled Image • The FeNiR rate kept at 0.70 kg-N/(m3·d) with 25% sludge replacement per 10 days. • The batch sludge replacement offset the sludge decay leading to the stable FeNiR. • A coupled and cost-effective technology of N- and P-removal was proposed. [ABSTRACT FROM AUTHOR]

In this study, a series of new indole derivatives of ursolic acid bearing different N-(aminoalkyl)carboxamide side chains were designed, synthesized, and evaluated for their in vitro cytotoxic activities against two human hepatocarcinoma cell lines (SMMC-7721 and HepG2) and normal hepatocyte cell line (LO2) via MTT assay. Among them, compound 5f exhibited the most potent activity against SMMC-7721 and HepG2 cells with IC50 values of 0.56 ± 0.08 μM and 0.91 ± 0.13 μM, respectively, and substantially lower cytotoxicity to LO2 cells. A follow-up enzyme inhibition assay and molecular docking study indicated that compound 5f can significantly inhibit the activity of Topoisomerase IIα. Further mechanistic studies performed in SMMC-7721 cells revealed that compound 5f can elevate the intracellular ROS levels, decrease mitochondrial membrane potential, and finally lead to the apoptosis of SMMC-7721 cells. Collectively, compound 5f is a promising Topoisomerase II (Topo II) inhibitor, which exhibited the potential as a lead compound for the discovery of novel anticancer agents. [ABSTRACT FROM AUTHOR]

Abstract A few carbon nanotubes (CNTs) and 1,2,3,4-bis(3,4-dimethylbenzylidene sorbitol (DMDBS) were incorporated into polypropylene/ethylene-propylene-diene terpolymer (PP/EPDM) (85/15, wt/wt) blends. It was found that DMDBS exhibited excellent nucleation effect on the crystallization of PP matrix, while its nucleation effect was weakened to a certain extent in the samples containing CNTs. Slightly changed localization state of CNTs from EPDM component to the blend interface was induced by DMDBS. Mechanical property measurements showed that compared with the low impact strength of the binary PP/EPDM (13.5 kJ/m2), greatly enhanced impact strength (51.2 kJ/m2) was achieved for the sample containing 1 wt% CNTs and 0.2 wt% DMDBS, which was also different from the slight enhancement of impact strength induced by adding only CNTs (18.8 kJ/m2) or DMDBS (16.3 kJ/m2). The synergistic toughening mechanisms of CNTs and DMDBS are attributed to the much reduced PP spherulites and the bridging effect of CNTs at the blend interface, which both facilitate the stress transferring from EPDM particles to PP matrix. Highlights • Largely reduced PP spherulites are achieved for the PP/EPDM blends containing DMDBS. • More CNTs locate at the blend interface. • The synergistic toughening efficiency is as high as 460%. • Both the largely reduced PP spherulites and the bridging effect of CNTs facilitate the stress transfer. [ABSTRACT FROM AUTHOR]

The apoplast serves as the first battlefield between the plant hosts and invading microbes; therefore, work on plant-pathogen interactions has increasingly focused on apoplastic immunity. In this study, we identified three proteins in the apoplast of cotton (Gossypium sp) root cells during interaction of the plant with the fungal pathogen Verticillium dahliae. Among these proteins, cotton host cells secrete chitinase 28 (Chi28) and the Cys-rich repeat protein 1 (CRR1), while the pathogen releases the protease VdSSEP1. Biochemical analysis demonstrated that VdSSEP1 hydrolyzed Chi28, but CRR1 protected Chi28 from cleavage by Verticillium dahliae secretory Ser protease 1 (VdSSEP1). In accordance with the in vitro results, CRR1 interacted with Chi28 in yeast and plant cells and attenuated the observed decrease in Chi28 level that occurred in the apoplast of plant cells upon pathogen attack. Knockdown of CRR1 or Chi28 in cotton plants resulted in higher susceptibility to V. dahliae infection, and overexpression of CRR1 increased plant resistance to V. dahliae , the fungus Botrytis cinerea , and the oomycete Phytophthora parasitica var nicotianae. By contrast, knockout of VdSSEP1 in V. dahliae destroyed the pathogenicity of this fungus. Together, our results provide compelling evidence for a multilayered interplay of factors in cotton apoplastic immunity. [ABSTRACT FROM AUTHOR]

Left ventricular hypertrophy (LVH) is a common abnormality in hemodialysis (HD) patients. Mitochondrial dysfunction contributes to the progression of LVH. As an inner mitochondrial membrane structural protein, mitofilin plays a key role in maintaining mitochondrial structure and function. The aim of this study was to investigate the relationship between mitofilin and LVH in HD patients. A total of 98 HD patients and 32 healthy controls were included in the study. Serum N-terminal proBNP (NT-proBNP), endothelin-1 (ET-1), and atrial natriuretic peptide (ANP) were examined. The protein level of mitofilin and the mitochondrial DNA (mtDNA) copy number were estimated in peripheral blood mononuclear cells (PBMCs). The left ventricle mass index (LVMI) was evaluated in all participants, and the interaction between these variables and the LVMI was assessed. The LVMI was positively correlated with the NT-proBNP, ET-1, and ANP levels, and it was negatively correlated with mtDNA copy number and mitofilin levels. Multiple regression analysis showed that the NT-proBNP, ET-1, and ANP levels as well as mitofilin levels and mtDNA copy number were associated with the LVMI. Although further research of these associations is needed, this result suggests that LVH may affect the levels of mitofilin in HD patients. [ABSTRACT FROM AUTHOR]

Summary: Salicylic acid (SA) signalling plays an essential role in plant innate immunity. In this study, we identified a component in the SA signaling pathway in potato (Solanum tuberosum), the transcription factor StbZIP61, and characterized its function in defence against Phytophthora infestans. Expression of StbZIP61 was induced upon P. infestans infection and following exposure to the defense signaling hormones SA, ethylene and jasmonic acid. Overexpression of StbZIP61 increased the tolerance of potato plants to P. infestans while RNA interference (RNAi) increased susceptibility. Yeast two‐hybrid and pull down experiments revealed that StbZIP61 could interact with an NPR3‐like protein (StNPR3L) that inhibited its DNA‐binding and transcriptional activation activities. Moreover, StNPR3L interacted with StbZIP61 in an SA‐dependent manner. Among candidate genes involved in SA‐regulated defense responses, StbZIP61 had a significant impact on expression of StICS1, which encodes a key enzyme for SA biosynthesis. StICS1 transcription was induced upon P. infestans infection and this responsive expression to the pathogen was reduced in StbZIP61 RNAi plants. Accordingly, StICS1 expression was remarkably enhanced in StbZIP61‐overexpressing plants. Together, our data demonstrate that StbZIP61 functions in concert with StNPR3L to regulate the temporal activation of SA biosynthesis, which contributes to SA‐mediated immunity against P. infestans infection in potato. [ABSTRACT FROM AUTHOR]

Three push-pull chromophores comprising a triphenylamine (TPA) as electron-donating moiety and functionalized β-diketones as electron acceptor units are studied by various spectroscopic techniques. The time-correlated single-photon counting data shows that increasing the number of electron acceptor units accelerates photoluminescence relaxation rate of compounds. Transient spectra data shows that intramolecular charge transfer (ICT) takes place from TPA units to β-diketones units after photo-excitation. Increasing the number of electron acceptor units would prolong the generation process of ICT state, and accelerate the excited molecule reorganization process and the relaxation process of ICT state. [ABSTRACT FROM AUTHOR]

Through comparing the linear and nonlinear optical property of two pull-push chromophores, which are composed of difluoroboron β-diketonate functionalized with carbazole and tert-butyl carbazole, the role of tert-butyl in chromosphere has been discussed in detail. The tert-butyl unit would lead to the absorption and fluorescence peak red shift and accelerate the fluorescence relaxation rate of chromophores. Moreover, the tert-butyl unit would affect obviously the two-photon optical property of chromophore according to the Z-scan test. The transient absorption (TA) data shows that these two pull-push chromopphores both own intramolecular charge transfer (ICT) characteristics and the tert-butyl unit accelerate the dynamic rate of ICT generation and relaxation process, which may be responsible for the variance of fluorescence property. [ABSTRACT FROM AUTHOR]

Two push-pull compounds, which are comprised of triphenylamine (TPA) (electron donor units) and functionalized β-diketones difluorboron complexes (electron acceptor units) are probed by many spectroscopies, which offers the relationship between electron acceptor and the intrinsic excited state properties of push–pull chromophores. We found that the photoluminescence (PL) intensity would enhance with the number of electron acceptor. Transient absorption (TA) data shows that intramolecular charge transfer (ICT) process really exists in the two molecules after photoexcitation and this process would be prolonged through increasing the electron-acceptor, which would be responsible for the improvement of PL property. [ABSTRACT FROM AUTHOR]

The direct analysis of drug distribution of rotigotine-loaded microspheres (RoMS) from tissue sections by liquid extraction surface analysis (LESA) coupled with tandem mass spectrometry (MS/MS) was demonstrated. The RoMS distribution in rat tissues assessed by the ambient LESA-MS/MS approach without extensive or tedious sample pretreatment was compared with that obtained by a conventional liquid chromatography tandem mass spectrometry (LC-MS/MS) method in which organ excision and subsequent solvent extraction were commonly employed before analysis. Results obtained from the two were well correlated for a majority of the organs, such as muscle, liver, stomach, and hippocampus. The distribution of RoMS in the brain, however, was found to be mainly focused in the hippocampus and striatum regions as shown by the LESA-imaged profiles. The LESA approach we developed is sensitive enough, with an estimated LLOQ at 0.05 ng/mL of rotigotine in brain tissue, and information-rich with minimal sample preparation, suitable, and promising in assisting the development of new drug delivery systems for controlled drug release and protection. [ABSTRACT FROM AUTHOR]

Lung cancer is the leading cause of cancer-related death worldwide. The development of epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) and immune checkpoint inhibitors (ICIs) has brought favorable survival benefits to patients with non–small-cell lung cancer (NSCLC); unfortunately, acquired drug resistance remains a major barrier to the treatment of NSCLC. Recent studies have demonstrated that the transcriptional co-activator with a PDZ-binding motif (TAZ, also called WWTR1) induces tumor immune evasion by directly modulating the expression of programmed death ligand 1 (PD-L1), a key therapeutic target for checkpoint immunotherapy. Moreover, aberrant activation of TAZ is also a major mechanism of acquired resistance to EGFR-TKIs in NSCLC. Therefore, TAZ signaling blockade might be an effective strategy to overcome resistance to ICIs and EGFR-TKIs in NSCLC. In this study, we showed for the first time that artesunate effectively reduced TAZ and PD-L1 expression in NSCLC. We further demonstrated that artesunate suppressed TAZ/PD-L1–induced T-cell growth inhibition in vitro and enhanced anti-tumor immunity by recruiting infiltrating CD8 + T-cells in syngeneic mouse models. Artesunate also inhibited the stem cell–like properties of NSCLC cells and suppressed tumor growth in xenografts bearing gefitinib-resistant tumors. In addition, our results of molecular docking and cellular thermal shift assay analysis suggested that artesunate might directly target the TAZ–TEAD complex and induce proteasome-dependent TAZ degradation in NSCLC cells. These results suggest that artesunate enhanced anti-tumor immunity and overcame EGFR-TKI resistance in NSCLC at least in part by suppressing TAZ/PD-L1 signaling. [Display omitted] • Artesunate inhibited the expression of TAZ and PD-L1 in NSCLC. • Artesunate suppressed TAZ/PD-L1-induced T-cell growth inhibition. • Artesunate enhanced anti-tumor immunity by recruiting infiltrating CD8+ T-cells. • Artesunate overcame EGFR-TKI resistance in NSCLC. • Artesunate promoted TAZ degradation in a proteasome-dependent manner. [ABSTRACT FROM AUTHOR]

Abstract: Protein–DNA interactions are involved in many biological processes essential for gene expression and regulation. To understand the molecular mechanisms of protein–DNA recognition, it is crucial to analyze and identify DNA-binding residues of protein–DNA complexes. Here, we proposed a novel descriptor shape string and another two related features shape string PSSM and shape string pair composition to characterize DNA-binding residues. We employed the new features and the position-specific scoring matrix (PSSM) for modeling and prediction. The results of a benchmark dataset showed that our approach significantly improved the accuracy of the predictor. The overall accuracy of our approach reached 85.86% with 85.02% sensitivity and 86.02% specificity. The results also demonstrated that shape string is a powerful descriptor for the prediction of DNA-binding residues. The additional two related features enhanced the predictive value. [Copyright &y& Elsevier]

Background: Ovarian cancer is known as one of the most common cancers in the world among women. ST6GALNAC1 is highly expressed in cancer stem cells (CSCs), which correlates to high tumor-initiating, self-renewal and differentiation abilities. This present study aims to investigate how ST6GALNAC1 affects ovarian cancer stem cells (OCSCs). Methods: In order to identify the differentially expressed genes related to ovarian cancer, microarray-based gene expression profiling of ovarian cancer was used, and ST6GALANC1 was one of the identified targets. After that, levels of ST6GALNAC1 in OCSCs and ovarian cancer cells were examined. Subsequently, an Akt signaling pathway inhibitor LY294002 was introduced into the cluster of differentiation 90+ (CD90+) stem cells, and cell proliferation, migration and invasion, levels of CXCL16, EGFR, CD44, Nanog and Oct4, as well as tumorigenicity of OCSCs were examined. Results: By using a comprehensive microarray analysis, it was determined that ST6GALNAC1 was highly expressed in ovarian cancer and it regulated the Akt signaling pathway. High levels of ST6GALNAC1 were observed in OCSCs and ovarian cancer cells. Silencing ST6GALNAC1 was shown to be able to reduce cell proliferation, migration, invasion, self-renewal ability, tumorigenicity of OCSCs. In accordance with these results, the effects of ST6GALNAC1 in OCSCs were dependent on the Akt signaling pathway. Conclusions: When taken together, our findings defined the potential stimulative roles of ST6GALNAC1 in ovarian cancer and OCSCs, which relied on the Akt signaling pathway. [ABSTRACT FROM AUTHOR]