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Carbon aerogels with nanoporous structure are attractive for thermal insulation under extreme conditions, but their practical applications are usually plagued by the inherent brittleness and easy-oxidation characteristic at high temperature. Herein, silica-modified carbon aerogels (SCAs) with extraordinarily high strength are prepared via a facile sol-gel polymerization of phenolic resin and siloxane, followed by ambient pressure drying and carbonization. The resulting SCAs possess medium-high density of ∼ 0.5 g·cm-3 and mesoporous structure with the mean pore size of 33 nm. During carbonization process, the siloxane could be gradually transformed into the amorphous SiO2 particles and crystalline SiC particles, which are coated on the surface of carbon nanoparticle and consequently improve the oxidation-resistance of carbon aerogels. Due to the density-porosity trade-off, the SCAs have high compressive strength of 10.0 MPa and satisfied thermal conductivities of 0.118 W·m-1·K-1 at 25 °C and 0.263 W·m-1·K-1 at 1000 °C. Furthermore, needled carbon fiber-reinforced SCAs (CF-SCAs) with ultrahigh compressive strength of 210.5 MPa are prepared, which exhibit good thermal conductivities of 0.207 W·m-1·K-1 at 25 °C and 0.407 W·m-1·K-1 at 1000 °C. The ultrahigh mechanical strength, good oxidation-resistance, good thermal insulation as well as the facile preparation make the SACs great promising in high-temperature insulations especially under harsh conditions.

In this work, a pH-tunable multicolor luminescent lanthanide-based hydrogel (CS/DEX/CP) was prepared based on lanthanide coordination polymer (CP), dextran aldehyde (DEX) and chitosan (CS). The CP was obtained by the self-assembly of guanosine acid (GMP), ciprofloxacin (CIP), Eu3+, and Tb3+. As-prepared CS/DEX/CP hydrogel could emit blue, green, and red luminescence of CIP, Tb3+, and Eu3+, respectively. It was also found that the luminescence of CS/DEX/CP hydrogel exhibited visual color change in the pH range of 5.5 to 8. Such pH-sensitive hydrogel was multicolor-responsive to protons produced by bacterial growth, therefore, it could provide early warning of bacterial infection by Naked-eye. In addition, the increased acidity resulted in not only the degradation of acid-labile Schiff base linkages between DEX and CS, but also the fracture of coordination between CIP and lanthanide ions. As a result, the released CIP and CS showed significantly antibacterial activity against both S.aureus and E. coli.

Carbon dioxide (CO2) assisted synthesis of water-soluble silver nanoparticle with a narrow particle size distribution is reported here based on the phase-inversion procedure. Bio-derived chitosan (CS) is used to stabilize the metal nanoparticles according to its abundant functional groups. Formic acid is employed as both a solvent (for the polymer) and a reductant for in-situ reducing the silver precursor along with the solvent evaporation. CO2 is utilized to combine with the amino groups of CS, reducing the viscosity of chitosan/formic acid solution and limiting the formation of hydrogen bonds. This promotes the stabilization and reduction efficiency of silver nanoparticles. In particular, 100% of Ag metal nanoparticles with the size of 7.5 ± 2.3 nm is successfully synthesized with the assistance of CO2. Interestingly, the synthesized CS/Ag nanocomposites are water-soluble owing to the formation of carbamate groups. This water-soluble silver nanoparticle presents an exceptional performance in the selective reduction of 4-nitrophenol, where the turnover frequency (TOF = 599 h−1) is even double with respect to the CO2 free system.

A hydrothermal process was proposed to prepare BiVO4/ diatomite composite photocatalysts, where BiVO4 was grown from a precursor solution containing diatomite, and EDTA used as a chelating agent to prevent the precipitation of precursor solution compositions on diatomite before hydrothermal treatment. The effect of some processing parameters like diatomite percentage and Ag-loaded amount on their photocatalytic performance were also investigated in detail by X-ray diffraction (XRD), X-ray photoelectron spectroscopy (XPS), BET, and UV‐Vis spectroscopy. The results show that BiVO4/ diatomite composite photocatalysts can be successfully prepared at 160 °C for the duration of 3h by the hydrothermal process. The diatomite has two significant impacts on their photocatalytic performance: (1) enhancing the dispersion of BiVO4 crystallites due to its high porosity and specific surface area to favor their photocatalytic performance, and (2) having a light screening effect to incident visible light to decrease their photocatalytic activity. Appropriately incorporating diatomite could improve their photocatalytic performance, but the overuse of diatomite would reduce that. Similarly, depositing Ag could effectively improve their photocatalytic activity because of its good light absorption and photosensitive characteristics, but excessive addition would result in their decrease since the overuse of Ag would also promote the electron-hole recombination.

Plastid terminal oxidase (PTOX) accepts electrons from plastoquinol to reduce molecular oxygen to water. We introduced the gene encoding Chlamydomonas reinhardtii (Cr)PTOX2 into the Arabidopsis (Arabidopsis thaliana) wild-type (WT) and proton gradient regulation5 (pgr5) mutant defective in cyclic electron transport around photosystem I (PSI). The accumulation of CrPTOX2 only mildly affected photosynthetic electron transport in the WT background during steady-state photosynthesis but partly complemented the induction of nonphotochemical quenching (NPQ) in the pgr5 background. During the induction of photosynthesis by actinic light (AL) of 130 µmol photons m−2 s−1, the high level of PSII yield (Y(II)) was induced immediately after the onset of AL in WT plants accumulating CrPTOX2. NPQ was more rapidly induced in the transgenic plants than in WT plants. P700 was also oxidized immediately after the onset of AL. Although CrPTOX2 does not directly induce a proton concentration gradient (ΔpH) across the thylakoid membrane, the coupled reaction of PSII generated ΔpH to induce NPQ and the downregulation of the cytochrome b6f complex. Rapid induction of Y(II) and NPQ was also observed in the pgr5 plants accumulating CrPTOX2. In contrast to the WT background, P700 was not oxidized in the pgr5 background. Although the thylakoid lumen was acidified by CrPTOX2, PGR5 was essential for oxidizing P700. In addition to acidification of the thylakoid lumen to downregulate the cytochrome b6f complex (donor-side regulation), PGR5 may be required for draining electrons from PSI by transferring them to the plastoquinone pool. We propose a reevaluation of the contribution of this acceptor-side regulation by PGR5 in the photoprotection of PSI.

Cancer stemness represents a major source of development and progression of colorectal cancer (CRC). c-Met critically contributes to CRC stemness, but how c-Met is activated in CRC remains elusive. We previously identified the lipolytic factor ABHD5 as an important tumour suppressor gene in CRC. Here, we show that loss of ABHD5 promotes c-Met activation to sustain CRC stemness in a non-canonical manner. Mechanistically, we demonstrate that ABHD5 interacts in the cytoplasm with the core subunit of the SET1A methyltransferase complex, DPY30, thereby inhibiting the nuclear translocation of DPY30 and activity of SET1A. In the absence of ABHD5, DPY30 translocates to the nucleus and supports SET1A-mediated methylation of YAP and histone H3, which sequesters YAP in the nucleus and increases chromatin accessibility to synergistically promote YAP-induced transcription of c-Met, thus promoting the stemness of CRC cells. This study reveals a novel role of ABHD5 in regulating histone/non-histone methylation and CRC stemness., This study reveals an unrecognized role of ABHD5 in regulating colon cancer stemness via controlling YAP methylation and nuclear localization, further explaining the molecular mechanism through which ABHD5 functions as a tumour suppressor gene in colon cancer.

Periodontitis is a chronic inflammation of periodontal tissue, and programmed cell death plays an important role in chronic periodontitis induced by P. gingivalis. Studies have shown that the increased expression of pyroptosis-related NLRP3 inflammasome and the pro-inflammatory cytokines IL-1β and IL-18 in gingivitis, invasive periodontitis, and chronic periodontitis patients. The present study aimed to investigate whether the inhibition of pyroptosis could protect porphyromonas gingival lipopolysaccharide (pg-LPS)-induced human periodontal ligament stem cells (hPDLSCs) injury and inflammation. The hPDLSCs were treated with pg-LPS and ATP in the presence of caspase1/4 inhibitor VX765. The cell proliferation and survival were assessed by CCK-8, the osteogenic differentiation capacity was evaluated by Alkaline Phosphatase (ALP) assay and alizarin red staining. Then, cell apoptosis, cleavage of gasdermin D (GSDMD) and generation of inflammatory cytokines were estimated. Lastly, western blotting was used to detect the expression of potential target proteins. Results showed that the treatment of pg-LPS plus ATP significantly inhibited the proliferation, survival and osteogenic differentiation of hPDLSCs, while inducing cell apoptosis, pyroptosis and inflammation. However, the presence of VX765 partially recovered the cell proliferation, survival and osteogenic differentiation. At the same time, VX765 inhibited cell apoptosis, cleavage of GSDMD and generation of inflammatory cytokines. Besides, the expression of related proteins including Bax, Bcl-2, cleaved (c)-caspase3, c-caspase4, c-caspase1, Toll Like Receptor 4, High Mobility Group Box 1 (HMGB1) and NLRP3 was all rescued by VX765. In conclusion, our results revealed that the blocking of cell pyroptosis could protect hPDLSCs from pg-LPS-induced injury. Therefore, the application of pyroptosis inhibitor may be a valuable therapeutic approach for treating periodontitis.

Supplemental digital content is available in the text., Objective The intestinal barrier injury caused by severe acute pancreatitis (SAP) can induce enterogenous infection, further aggravating the inflammatory reactions and immune responses. This study aimed to test the hypothesis that emodin protects the intestinal function and is involved in the immune response in SAP. Methods The network pharmacology was established using the Swiss target prediction and pathway enrichment analysis. The SAP mice model was induced by cerulein (50 μg/kg) and lipopolysaccharide (10 mg/kg) hyperstimulation. The pharmacological effect of emodin in treating SAP was evaluated at mRNA and protein levels by various methods. Results The network analysis provided the connectivity between the targets of emodin and the intestinal barrier–associated proteins and predicted the BAX/Bcl-2/caspase 3 signaling pathway. Emodin alleviated the pathological damages to the pancreas and intestine and reduced the high concentrations of serum amylase and cytokines in vivo. Emodin increased the expression of intestinal barrier–related proteins and reversed the changes in the apoptosis-related proteins in the intestine. Simultaneously, emodin regulated the ratio of T helper type 1 (TH1), TH2, TH17, γδ T cells, and interferon γ/interleukin 17 producing γδ T cells. Conclusions These findings partly verified the mechanism underlying the regulation of the intestinal barrier and immune response by emodin.

Background Retinal biomarkers of Alzheimer’s disease (AD) have been extensively investigated in recent decades. Retinal nervous and vascular parameters can reflect brain conditions, and they can facilitate early diagnosis of AD. Objective Our study aimed to evaluate the difference in retinal neuro-layer thickness and vascular parameters of patients with AD and healthy controls (HCs). Methods Non-invasive optical coherence tomography angiography (OCTA) was used to determine the combined thickness of the retinal nerve fiber layer (RNFL) and ganglion cell layer (GCL), as well as the full retinal thickness (FRT). The vascular branching (VB), vascular curvature (VC), and vascular density (VD) for AD and HC groups were also obtained. The Mini-Mental State Examination (MMSE) was used to evaluate the cognitive performance of all the participants. After obtaining all the parameters, two-way analysis of variance (ANOVA) was used to compare the mean values of all the retinal parameters of the patients with AD and the HCs. Pearson's correlation was used to test the association between retinal parameters, MMSE scores, and vascular parameters. Results Seventy-eight eyes from 39 participants (19 AD and 20 HC; male, 52.6% in AD and 45.0% in HC; mean [standard deviation] age of 73.79 [7.22] years in AD and 74.35 [6.07] years in HC) were included for the analysis. The average RNFL + GCL thickness (106.32 ± 7.34 μm), FRTs of the four quadrants (290.35 ± 13.05 μm of inferior quadrant, 294.68 ± 9.37 μm of superior quadrant, 302.97 ± 6.52 μm of nasal quadrant, 286.02 ± 13.74 μm of temporal quadrant), and retinal VD (0.0148 ± 0.003) of patients with AD, compared with the HCs, were significantly reduced (p p r2 = 0.2146, p Conclusion Our study suggested that the patients with AD, compared with age-matched HCs, had significantly reduced RNFL + GCL thickness and vascular density. These reductions correlated with the cognitive performance of the participants. By combining nerve and vessel parameters, the diagnosis of AD can be improved using OCTA technology. Trail registration Name of the registry: Chinese Clinical Trail Registry, Trial registration number: ChiCTR2000035243, Date of registration: Aug. 5, 2020. URL of trial registry record: http://www.chictr.org.cn/index.aspx

The involvement of zinc (Zn) in terms of aroma formation has been rarely investigated. This study shows that the regulation of 2-acetyl-1-pyrroline (2AP) biosynthesis was evaluated in two different rice cultivars under foliar Zn application. The results showed that the 2AP and Zn contents in leaves and grains were improved substantially under foliar Zn application. The 2AP content was positively related to the expression P5CS2 gene, contents of proline, 1-pyrroline, and Δ1-pyrroline-5-carboxylate (P5C), and the activity of pyrroline-5-carboxylate synthase (P5CS) under Zn application in fragrant rice. Multiple transcription factors (TFs) were differently expressed, such as bZIPs, NACs, and MYBs, to play a role under Zn treatments in fragrant rice, suggesting the crucial role of 46 differently expressed TFs in 2AP improvements in fragrant rice. Furthermore, this study showed that the optimal foliar Zn application at a concentration of 30 mg L-1 could increase the 2AP content of aromatic rice and keep the yield stable or increase the yield. TFs were involved in regulating to promote the 2AP formation in aromatic rice under the foliar Zn application. However, the relationship between 2AP biosynthesis pathway genes and TFs in fragrant rice remains to be further studied.

A new tyramine derivative, glycosamide A (1), together with two known amide alkaloids, N-benzoyltyramine methyl ether (2) and aurantiamide acetate (3), was isolated from the branches and leaves of Glycosmis craibii Tanaka. Their structures were elucidated through extensive 1D and 2D NMR and HR-ESI-MS spectroscopic analyses. All known compounds were isolated from the genus Glycosmis for the first time. Furthermore, the antiproliferative activities of all isolated alkaloids in vitro were evaluated. Compound 2 displayed weak antiproliferative activities against five human cancer cell lines, HL-60, SMMC-7721, A-549, MCF-7, and SW480.

Two new aldoximes A–B (1−2), and two known analogues (3−4), were identified from ethanolic extracts of Glycosmis craibii. The structures of new compounds 1−2 were unambiguously elucidated based on spectroscopic methods. All isolated aldoximes were evaluated for their anti-inflammatory activity in vivo. Compounds 1−4 displayed remarkable inhibitory effects against nitric oxide (NO) production stimulated by lipopolysaccharide in mouse macrophage RAW 264.7 cells with the IC50 values ranging from 2.38 ± 0.08–8.43 ± 0.21 μM.

Endometrial cancer is generally one of the most evident malignant tumours of the female reproductive system, and the mechanisms underlying its cell proliferation and apoptosis are key to research in gynaecological oncology. In the paper, the in-depth molecular mechanism by which DJ-1 protein regulates the proliferation and apoptosis of Ishikawa cells was investigated. DJ-1 knockdown and overexpressing Ishikawa stable cell lines were established by lentiviral transduction. The levels of DJ-1 and noncanonical NF-κB signaling proteins were evaluated by Western blotting. Cell counting kit-8 (CCK-8) and flow cytometry were applied to analyze the cell viability and apoptosis. Co-immunoprecipitation experiment was utilized to assess the DJ-1-Cezanne interaction. The results showed that DJ-1 overexpression conferred apoptosis resistance and high proliferation on Ishikawa cells, while DJ-1 knockdown in Ishikawa cells produced the opposite results. These findings again suggested that DJ-1 inhibits the apoptosis and promotes the proliferation of Ishikawa cells. More crucially, further data showed that the noncanonical NF-κB activation was required for the regulation of Ishikawa cell proliferation and apoptosis by DJ-1. Meanwhile, it was found that noncanonical NF-κB pathway may be activated by DJ-1 interacting with and negatively regulating Cezanne in Ishikawa cells. Overall, this work revealed that DJ-1 associates with and negatively regulates Cezanne and consequently triggers the noncanonical NF-κB activation, thereby regulating Ishikawa cell proliferation and apoptosis.

The outbreak of novel coronavirus pneumonia (COVID-19), defined as a worldwide pandemic, has been a public health emergency of international concern. Pudilanxiaoyan oral liquid (PDL), an effective drug of Traditional Chinese Medicine (TCM), is considered to be an effective and alternative means for clinical prevention of COVID-19. The purpose of this study was to identify potential active constituents of PDL, and explore its underlying anti-COVID-19 mechanism using network pharmacology. Integration of target prediction (SwissTargetPrediction and STITCH database) was used to elucidate the active components of PDL. Protein–protein interaction network analyses, gene ontology, Kyoto Encyclopedia of Genes and Genomes pathway enrichment analyses, network construction, and molecular docking were applied to analyze the prospective mechanisms of the predicted target genes. Our results showed that the key active ingredients in PDL were luteolin, apigenin, esculetin, chrysin, baicalein, oroxylin A, baicalin, wogonin, cymaroside, and gallic acid. A majority of the predicted targets were mainly involved in the pathways related to viral infection, lung injury, and inflammatory responses. An in vitro study further inferred that inhibiting the activity of nuclear factor (NF)-кB signaling pathway was a key mechanism by which PDL exerted anti-COVID-19 effects. This study not only provides chemical basis and pharmacology of PDL but also the rationale for strategies to exploring future TCM for COVID-19 therapy.

A high-performance quasi-vertical GaN Schottky barrier diode (SBD) was successfully fabricated by using a high-quality n−-GaN drift layer with a precisely-controlled n-type doping. A high current on/off ratio of 1010, an ideality factor of 1.03, a low specific on-resistance of 1.41 $\text{m}\Omega \cdot $ cm2, and a relatively high breakdown voltage (BV) of 250 V have been achieved for the SBD without edge termination. Furthermore, with an Argon-implanted termination, the as-fabricated GaN-on-Si SBD shows a record high BV of 405 V, yielding a critical electric field of ~ 2 MV/cm, while the forward conduction characteristics are well maintained.

The supported 40 wt% (NH4)3HPMo11VO40 (APMV) catalysts over two different types of supports, supports-I (Cs3PMo12O40, Cs2.5H0.5PMo12O40, Cs4PMo11VO40 and Cs3HPMo11VO40) and supports-II (CeO2, WO3/ZrO2 and S-1 molecular sieve), were synthesized by deposition–precipitation method and further evaluated in the partial oxidation of isobutane to methacrylic acid (MAA) at 340 °C under atmospheric pressure. The fresh and used catalysts were characterized by N2 adsorption/desorption, TG/DTG, XRD, FT-IR, Raman spectroscopy, pyridine- adsorption FT-IR and NH3-TPD to investigate their structure, stability and surface acidity. The better results were obtained by impregnating 40 wt% active APMV phase onto the supports-I phase with same/similar Keggin structure, and it is believed that the formation of coherent interfaces between two structural well-matched phases with the same/similar Keggin anions greatly promotes interfacial transfer abilities of electrons and lattice oxygen, which is responsible for the efficient oxygen insertion to maximize MAA selectivity and conversion of isobutane. The current work provides a concept of phase synergy to design a promising catalyst for selective oxidation of isobutane.

A full elucidation of chemisorbed donor behavior is of fundamental importance for tailoring the active species but has not yet been achieved for Ziegler–Natta catalysts. Herein, by exploiting the s...

Hydrosilylation is one of the most important reactions in synthetic chemistry and ranks as a fundamental method to access organosilicon compounds in industrial and academic processes. However, the enantioselective construction of chiral-at-silicon compounds via catalytic asymmetric hydrosilylation remained limited and difficult. Here we report a highly enantioselective hydrosilylation of ynones, a type of carbonyl-activated alkynes, using a palladium catalyst with a chiral binaphthyl phosphoramidite ligand. The stereospecific hydrosilylation of ynones affords a series of silicon-stereogenic silylenones with up to 94% yield, >20:1 regioselectivity and 98:2 enantioselectivity. The density functional theory (DFT) calculations were conducted to elucidate the reaction mechanism and origin of high degree of stereoselectivity, in which the powerful potential of aromatic interaction in this reaction is highlighted by the multiple C-H-π interaction and aromatic cavity-oriented enantioselectivity-determining step during desymmetric functionalization of Si-H bond.

Camellia oil is a popular edible oil in China as a result of its nutritional properties. However, the key odorants of camellia oil remain unclear. In this study, the volatiles of virgin camellia oil (VCO) were extracted by solvent-assisted and non-solvent-assisted methods. A total of 66 volatile compounds were identified using gas chromatography-mass spectrometry-olfactometry, with flavor dilution factors ranging from 1 to 729 via aroma extraction dilution analysis. Among them, 10 odorants were identified for the first time in VCO. Moreover, 41 volatiles were confirmed as aroma-active compounds with odor activity values greater than 1. Aroma recombination and omission studies demonstrated that aldehydes, esters, acids, and heterocyclic compounds significantly contribute to the aroma profiles of VCO. Hexanal, octanal, (E,E)-2,4-heptadienal, (E,E)-2,4-nonadienal, decyl acetate, ethyl benzoate, ethyl 2-methylbutanoate, 2-methylbutyl (Z)-2-methyl-2-butenoate, 2-methylbutanoic acid, hexanoic acid, 2-pentylfuran, and 2-methyl-3-furanthiol could impart roasted-like, nut-like, fat-like, fruit-like, grass-like, and sweat-like odors and were the key odorants in VCO. The lipoxygenase pathway was possibly responsible for the formation of key odorants in VCO. This work provides an extract aroma consistent for virgin camellia oil.

The interfacial bonding and structure at the nanoscale in the polymer–clay nanocomposites are essential for obtaining desirable material and structure properties. Layered nanocomposite films of cellulose nanofibrils (CNFs)/montmorillonite (MTM) were prepared from the water suspensions of either CNFs bearing quaternary ammonium cations (Q-CNF) or CNFs bearing carboxylate groups (TO-CNF) with MTM nanoplatelets carrying net surface negative charges by using vacuum filtration followed by compressive drying. The effect of the ionic interaction between cationic or anionic charged CNFs and MTM nanoplatelets on the structure, mechanical properties, and flame retardant performance of the TO-CNF/MTM and Q-CNF/MTM nanocomposite films were studied and compared. The MTM nanoplatelets were well dispersed in the network of TO-CNFs in the form of nanoscale tactoids with the MTM content in the range of 5–70 wt %, while an intercalated structure was observed in the Q-CNF/MTM nanocomposites. The resulting TO-CNF/MTM nanocomposite films had a better flame retardant performance as compared to the Q-CNF/MTM films with the same MTM content. In addition, the effective modulus of MTM for the TO-CNF/MTM nanocomposites was as high as 129.9 GPa, 3.5 times higher than that for Q-CNF/MTM (37.1 GPa). On the other hand, the Q-CNF/MTM nanocomposites showed a synergistic enhancement in the modulus and tensile strength together with strain-to-failure and demonstrated a much better toughness as compared to the TO-CNF/MTM nanocomposites.

We have established dual paclitaxel (PTX)/superparamagnetic iron oxide (SPIO)-loaded PLGA-based nanoparticles for theranostic purposes. The fabricated nanoparticles exhibited a spherical morphology with a size of ∼240 nm. The PTX and iron loading were 1.84 ± 0.4 and 10.4 ± 1.93 mg/100 mg, respectively. The relaxometry studies and phantom magnetic resonance imaging demonstrated their efficacy as T2 contrast agents. A significant cellular uptake of nanoparticles by the endometrial Ishikawa cells was demonstrated using confocal laser scanning microscopy. While SPIO did not show any toxicity in endometrial Ishikawa cells, PTX-loaded nanoparticles indicated cytotoxic activity. Together, these advantages of multifunctional nanoparticles may be considered as future nanomedicines for simultaneous molecular imaging, drug delivery, and real-time monitoring of therapeutic response.

Gut bacterial β-glucuronidases (GUS) play an important role in deconjugation of various O-glucuronides, which are tightly linked with the drug-induced intestinal toxicity. Increasing evidence has indicated that inhibition of bacterial GUS could alleviate GUS-associated intestinal toxicity, but the potent and broad-spectrum inhibitors against multiple bacterial GUS have been rarely reported. This study aimed to find potent and broad-spectrum GUS inhibitors from Ginkgo biloba. It was found that amentoflavone displayed relatively strong inhibition on three GUS including CpGUS, SpasGUS and EcGUS. Further investigations demonstrated that amentoflavone could inhibit GUS-mediated PNPG hydrolysis in a dose-dependent manner with IC50 values of 2.36 μM, 2.88 μM and 3.43 μM for CpGUS, SpasGUS and EcGUS, respectively. Inhibition kinetic studies showed that amentoflavone functioned as a non-competitive inhibitor against all tested GUS with Ki values of less than 2 μM. Docking simulations indicated that amentoflavone could tightly bind on allosteric sites of three GUS mainly via hydrogen bonding interactions, and the number of hydroxyl groups of amentoflavone played crucial roles in these interactions. Collectively, our findings suggested that amentoflavone was a potent broad-spectrum inhibitor against bacterial GUS, which can be used as a promising lead compound for developing novel agents to alleviate GUS-associated intestinal toxicity.

Novel multicompartment self-assemblies of triblock copolymer polystyrene–polyisoprene–poly(2-vinylpyridine) (PS-PI-P2VP) for drug delivery are demonstrated. The triblock copolymer assemblies in dilute solutions in a common solvent (tetrahydrofuran) undergo transformations from core-shell-corona micelles to multicompartment micelles by adding P2VP-selective solvent (water). The effects of water content and pH on the assembled structures were systematically investigated. Multicompartment micelles are also obtained by adding a surfactant, 4-biphenylcarboxylic acid, into the solution. Such multicompartment self-assemblies are used as carriers for encapsulation and release of an anticancer drug doxorubicin hydrochloride (DOX). The drug loading content and drug loading efficiency of DOX were evaluated. The DOX release experiments were performed at 37°C under pH 5.5 and pH 7.4. The DOX release rate was improved as pH decreased from pH 7.4 to 5.0, with 45.6% release of DOX in 32 h.

In this article, a dynamic charge storage mechanism is proposed for designing the p-GaN gate dynamic charge storage high-electron-mobility transistor (DCS-HEMT) with ultralow switching loss. The device features a p-doped DCS layer in AlGaN buffer. When the DCS-HEMT is turning off, the net negative charges in the DCS layer significantly contribute to the depletion of 2-D-electron-gas (2DEG) channel, leading to low turn-off loss ( ${E} _{OFF}$ ). During turn-on process, reduction of the negative charges amount could accelerate the formation of electrons at the 2DEG channel, which results in low turn-on loss ( ${E} _{ON}$ ). Verified by the calibrated simulation, total switching loss ( ${E} _{\text {SW}} \boldsymbol = {E}_{OFF} +{E}_{ON}$ ) of the designed DCS-HEMT is 61% lower than that of the conventional p-GaN gate HEMT (C-HEMT). The improved performance makes the DCS-HEMT a competitive candidate for low switching loss power applications.

Surface modification of oxygen evolution reaction (OER) cocatalysts is a promising approach to improve PEC water oxidation activity by accelerating the surface charge injection efficiency and catalytic reaction kinetics. However, the PEC performance is still restricted by inefficient charge transfer at the semiconductor/cocatalyst interface. In this study, ultrathin Ti3C2 nanosheets, serving as a highly efficient hole transport layer, were introduced into the Fe2O3/CoAl-layered double hydroxide (LDH) interface. The obtained Fe2O3–Ti3C2–CoAl photoanodes exhibited a significantly improved photocurrent density of 2.1 mA cm−2 at 1.23 V versus the reversible hydrogen electrode (RHE) under AM 1.5G illumination. In this system, the Ti3C2 nanolayer not only suppresses the interfacial recombination of photogenerated carriers but also facilitates efficient hole transfer from Fe2O3 to the OER cocatalyst, thus promoting the PEC performance. This study provides a new guideline for optimizing the charge transfer at the semiconductor/cocatalyst interface.

We herein report an extended gate-type organic thin-film transistor (OTFT)-based polyamine sensor and its application in pattern recognition. The extended-gate electrode was functionalized with a complex of copper(II) ions and 2-carboxymethylthio-5-mercapto-1,3,4-thiadiazole, which enabled the OTFT to respond to polyamines in an aqueous solution. Moreover, the responses of the OTFT-based sensor exhibited a cross-reactivity, implying its capability to detect multi-analytes. Thus, we performed pattern recognition against nine target polyamines (spermine, spermidine, trimethylenediamine, ethylenediamine, histamine, tryptamine, putrescine, cadaverine and 1,6-diaminohexane) in combination with linear discriminant analysis and successfully discriminated the analytes. Moreover, we achieved the quantification of spermine in a diluted fruit juice by using a support vector machine with high accuracy. Overall, the demonstration using the OTFT-based chemical sensor with pattern recognition revealed its potential for sensing polyamines in real samples.

Catalytic asymmetric variants for functional group transformations based on carbon-carbon bond activation still remain elusive. Herein we present an unprecedented palladium-catalyzed (3 + 2) spiro-annulation merging C(sp2)-C(sp2) σ bond activation and click desymmetrization to form synthetically versatile and value-added oxaspiro products. The operationally straightforward and enantioselective palladium-catalyzed atom-economic annulation process exploits a TADDOL-derived bulky P-ligand bearing a large cavity to control enantioselective spiro-annulation that converts cyclopropenones and cyclic 1,3-diketones into chiral oxaspiro cyclopentenone-lactone scaffolds with good diastereo- and enantio-selectivity. The click-like reaction is a successful methodology with a facile construction of two vicinal carbon quaternary stereocenters and can be used to deliver additional stereocenters during late-state functionalization for the synthesis of highly functionalized or more complex molecules.

Oxidative stress and apoptosis of vascular smooth muscle cells (VSMCs) are key to vascular calcification in patients with chronic kidney disease (CKD). The mitochondria-targeted antioxidant, mitoquinone (MitoQ), which reduces oxidative stress and apoptosis, has a protective effect in acute models of renal injury but whether MitoQ can attenuate vascular calcification in CKD patients is unknown. This study was conducted to investigate whether MitoQ can prevent calcification, both in vitro and in vivo. Adenine was used to induce calcification in rats, and inorganic phosphate was used to induce calcification in VSMCs. To elucidate the underlying molecular mechanism, a specific inhibitor of Nrf2, ML385, was used 1 h before MitoQ administration. Histological staining, ELISA, flow cytometry, alizarin red staining and western blotting were used to test this hypothesis. Administration of MitoQ alleviated calcification and oxidative stress. The anti-apoptotic effect of MitoQ was associated with upregulation of Bcl-2, downregulation of Bax, and increased Nrf2 expression. The effects of MitoQ were reversed by treatment with ML385. This study offers evidence that MitoQ attenuates vascular calcification by suppressing oxidative stress and apoptosis of VSMCs through the Keap1/Nrf2 pathway. MitoQ should be further investigated as a potential therapy to prevent vascular calcification in CKD patients.

Background To establish the co-delivery liposomes of gefitinib (GFT) and curcumin (CUR) via oral administration with the goals of improving the synergistic effect and reducing acquired drug resistance. Methods We prepared liposomes (LPs) which can embed the anticancer compound GFT and CUR and investigated whether they could enhance the antitumor effects of anticancer drugs against MDR. The LPs system was characterized by transmission electron microscopy (TEM), particle size, encapsulation efficiency, cellular uptake and cell viability. In addition, the release characteristics and pharmacodynamics of the LPs were also studied in detail. Results The results showed that GFT/CUR LPs were characterized by small particle size of about 130 nm and negative zeta potential of about −22.2 mV, and the drug controlled to release slowly on a biphasic pattern. Compared with control groups, GFT/CUR LPs showed a higher cellular uptake and cell inhibition rates. Through pharmacodynamics analysis, we found that two compounds (GFT and CUR) were incorporated into one LPs carrier, which played a good role in synergistic effect. Conclusion Co-delivery of GFT and CUR has the potential to improve cancer treatment efficacy and overcome acquired resistance, especially towards GFT-resistant cells.

Fragrant Brassica species seed oils (FBO) produced in China are mainly obtained from rapeseed (Brassica napus: B. napus) and mustard seeds (Brassica juncea: B. juncea). The characterization and differences of aroma profiles between those two species remain unclear. In this study, the volatile compounds in FBOs were systemically extracted by headspace solid-phase microextraction and solvent-assisted flavor evaporation combined with ultrasound and identified by comprehensive two-dimensional gas chromatography and time-of-flight mass spectrometry (GC×GC-TOFMS) and gas chromatography-olfactometry (GC-O). Ninety-three odorants were identified as aroma-active compounds with flavor dilution (FD) factors ranging from 1 to 6561. Moreover, 63 key compounds exhibited their odor activity values (OAVs) to be greater than 1. The oils of the two species were successfully recombinated with their key odorants. B. juncea oils presented stronger pungent-like, pickled-like, and fishy like notes compared to B. napus oils. The key odor differences were primarily attributed to the concentration of 3-butenenitrile, 4-(methylsulfanyl)butanenitrile, 5-(methylsulfanyl)pentanenitrile, 3-isothiocyanato-1-propene, 3-methyl-3-butenenitrile, isothiocyanatocyclopropane, (methylsulfanyl)acetonitrile, dimethyl sulfide, dimethyl trisulfide, and 3-(methyldisulfanyl)-1-propene. This work provides a guide for the selection of raw materials and odor markers in fragrant B. napus and B. juncea oils.

Background: The retinal microvasculature within the macula in glaucomatous eyes is not clear. Objectives: To detect macular vessel density (MVD) changes in primary angle-closure glaucoma (PACG). Methods: Twenty-two PACG patients who had an episode of acute primary angle closure were included. Structural optical coherence tomography (OCT) scans were conducted to measure the thickness of the peripapillary retinal nerve fiber layer and macular ganglion cell complex (GCC). The MVD was measured with OCT angiography. Results: A weakened macular microvascular network that had an expanded fovea avascular zone was observed in the case group. Compared with the control group, the case group had a lower MVD ( p < 0.001). Single correlation analysis revealed a significant correlation of the MVD with best-corrected visual acuity (BCVA) ( r = −0.65, p = 0.001), GCC ( r = 0.50, p = 0.018), and the visual field mean deviation ( r = −0.54, p = 0.009) in the case group. Moreover, in the mixed-effect models, the MVD was found to be positively correlated with GCC ( p = 0.017) and negatively correlated with LogMar BCVA ( p < 0.001). Conclusions: After an acute angle-closure attack, the macular microvascular network is attenuated, and the MVD decreases significantly.

Background Multiple sclerosis (MS) is an immune-mediated demyelinated disease of the central nervous system. Activation of microglia is involved in the pathogenesis of myelin loss. Objective This study is focused on the role of Hv1 in regulating demyelination and microglial activation through reactive oxygen species (ROS) production after lysophosphatidylcholine (LPC)-mediated demyelination. We also explored autophagy in this process. Methods A model of demyelination using two-point LPC injection into the corpus callosum was established. LFB staining, immunofluorescence, Western blot, and electron microscopy were used to study the severity of demyelination. Microglial phenotype and autophagy were detected by immunofluorescence and Western blot. Morris water maze was used to test spatial learning and memory ability. Results We have identified that LPC-mediated myelin damage was reduced by Hv1 deficiency. Furthermore, we found that ROS and autophagy of microglia increased in the demyelination region, which was also inhibited by Hv1 knockout. Conclusion These results suggested that microglial Hv1 deficiency ameliorates demyelination through inhibition of ROS-mediated autophagy and microglial phenotypic transformation.

The experimental speeds of sound for the binary system of ethanol (1) + n-heptane (2) with the mole fractions of ethanol being (0.100, 0.300, 0.500, 0.700, and 0.900) were measured by Rayleigh-Bril...

Purpose This study aims to reveal the mechanism underlying baicalin-suppressing ovarian cancer stemness. Methods OVCAR-3 and the primary ovarian cancer cells were used for cell model. The ovarian cancer stem cells were isolated by suspension culture. Cell viability and clonogenicity were examined by CCK-8 assay and colony formation assay. The self-renewal of the cells was evaluated by the determination of sphere-forming capacity and the frequency of in vitro sphere-forming and in vivo tumor-initiating cells. The mRNA and protein levels were relatively quantified by qRT-PCR and Western blot. The transcription regulation of target genes was tested by luciferase reporter assay and a modified nuclear rn-on qRT-PCR assay. Results Treatment with a non-toxic dose of baicalin significantly inhibited the spherogenicity of ovarian cancer cells. Moreover, a non-toxic dose of baicalin treatment suppressed the frequency of sphere-forming and tumor-initiating ovarian cancer cells. Furthermore, the expression of ovarian cancer stem cell markers (CD133 and ALDH1A1) was inhibited by a non-toxic dose of baicalin treatment. Baicalin inhibits YAP activity and suppresses RASSF6, a positive regulator of YAP, at the transcriptional level. Overexpression of both YAP and RASSF6 abolished the inhibitory effect of baicalin on the proliferation and stemness of ovarian cancer cells. Conclusion The results in this study demonstrated that baicalin suppresses the stemness of ovarian cancer cells by attenuating YAP activity via inhibiting RASSF6 at the transcriptional level. This finding revealed baicalin as a novel YAP inhibitor that could serve as an anti-cancer drug for eradicating ovarian cancer stem cells.

AIM: To identify proangiogenic factors engaged in neovascular age-related macular degeneration (AMD) except vascular endothelial growth factor (VEGF) from human retinal pigment epithelial (hRPE) cells and investigate the underlying mechanisms. METHODS: VEGF receptor 2 (VEGFR2) in ARPE-19 cells was depleted by siRNA transfection or overexpressed through adenovirus infection. The mRNA and the protein levels of interleukin-8 (IL-8) in ARPE-19 cells were measured by quantitative real-time polymerase chain reaction and enzyme-linked immunosorbent assay respectively. The protein levels of AKT, p-AKT, MEK, p-MEK, ERK1/2, p-ERK1/2, JNK, p-JNK, p38 and p-p38 were detected by Western blotting. A selective chemical inhibitor, LY3214996, was employed to inhibit phosphorylation of ERK1/2. Cell viability was determined by MTT assay. RESULTS: Knockdown of VEGFR2 in ARPE-19 cells robustly augmented IL-8 production at both the mRNA and the protein levels. Silencing VEGFR2 substantially enhanced phosphorylation of MEK and ERK1/2 while exerted no effects on phosphorylation of AKT, JNK and p38. Inhibiting ERK1/2 phosphorylation by LY3214996 reversed changes in VEGFR2 knockdown-induced IL-8 upregulation at the mRNA and the protein levels with no effects on cell viability. VEGFR2 overexpression significantly reduced IL-8 generation at the mRNA and the protein levels. CONCLUSION: Blockade of VEGF signaling augments IL-8 secretion via MEK/ERK1/2 axis and overactivation of VEGF pathway decreases IL-8 production in hRPE cells. Upregulated IL-8 expression after VEGF signaling inhibition in hRPE cells may be responsible for being incompletely responsive to anti-VEGF remedy in neovascular AMD, and IL-8 may serve as an alternative therapeutic target for neovascular AMD.

Abstract Mangiferin is a compound with many pharmacological activities and exists in many natural products. Anhydrous and hydrate of mangiferin have been reported separately in two literatures, but the polymorphism of this compound has not been realized until this paper. In this study, polymorph screening of mangiferin has been carried out and five forms have been obtained including three new forms never reported. Several solid state characterization methods, such as powder X-ray diffraction, differential scanning calorimetry and thermogravimetry, are used to identify and characterize all of mangiferin forms. The comparison of the crystallographic data and hirshfeld surface analysis were first reported for mangiferin anhydrous and hydrate. Furthermore, the studies on stability, transformation and solubility have been undertaken, the results prompt that form V can be used as the dominant polymorph for the development of innovative pharmaceuticals. Graphic Abstract

In this work, an optical waveguide in the chalcogenide glass (80GeS2–15Ga2S3–5Sb2S3) is fabricated for the first time and its optical properties are investigated. A one-dimensional chalcogenide waveguide structure has been formed by 550 keV He+ ion implantation with a dose of 4 × 1016 ions/cm2 at room temperature. The effective refractive indices of the guided modes at the wavelength of 632.8 nm were measured with the aid of the Model 2010 Prism Coupler system. The refractive index profile, a critical factor in the analysis of waveguide structure, was reconstructed by the reflectivity calculation method. It was found that a positive change of refractive index occurred in the waveguide region, and an optical barrier with decreased refractive index was built at the end of the ion trajectory, i.e., producing a type of “well + barrier” structure. The SRIM 2013 program was utilized to display the profile of the energy loss versus the penetrated depth when the incident ion beam implanted. The near-field intensity distribution for the fundamental mode along the TE polarization was simulated through the finite-difference beam propagation method. From our experiments, these data provide a great deal of useful information about the manufacture of the chalcogenide waveguide structure.

The present research investigates the use of biocolorants (Anthocyanin and chlorophyll) extracted from Cinnamomum camphora waste/fallen leaves to develop natural and beautiful shades on wool fibers...

Lipid metabolic deficiencies are associated with many genetic disorders. Bietti crystalline dystrophy (BCD), a blindness-causing inherited disorder with changed lipid profiles, is more common in Chinese and Japanese than other populations. Our results reveal that mouse models lacking Cyp4v3 have less physiological and functional changes than those of BCD patients with this gene defect. After the administration of a high-fat diet (HFD), the occurrence of retinal lesions were both accelerated and aggregated in the Cyp4v3−/− mouse models, implying that changed lipid levels were not only associated factors but also risk factors to BCD patients. Facilitated by the results, we found that the reduced electroretinography waveforms and retinal thickness observed in the HFD-induced mouse models were effectively recovered after subretinal delivery of a human CYP4V2 gene carried by an adeno-associated virus vector, which demonstrates the potential curability of BCD by gene therapy.

Omeprazole is a commonly used drug in patients with ulcerative colitis (UC). This study investigated the pharmacokinetics of omeprazole in rats with UC induced by dextran sulfate sodium (DSS). The pharmacokinetics of intravenously administered omeprazole (20 mg/kg) was investigated in normal and UC rats using LC-MS/MS. The formation of 5-OH omeprazole, a main metabolite of omeprazole, in rat liver microsomes (RLMs) from normal and UC rats was compared. The protein levels of CYP1A2, CYP2D1, and CYP3A1 in the liver were measured by Western blot. Compared with normal rats, UC rats had increased plasma concentrations of omeprazole, resulting in an increased AUC0–240 min and decreased CL. DSS treatment decreased the formation rate of 5-OH omeprazole in RLMs but did not change the affinity of the enzymes. The Vmax and CLint of RLMs from UC rats were 62% and 48% those of RLMs from normal rats, respectively. The hepatic CYP1A2 and CYP3A1 protein levels in UC rats were 42.6 and 45.2% lower than those in normal rats, respectively; however, the protein levels of CYP2D1 in the two groups were similar. The activity and expression of some hepatic CYP450 isoforms were decreased by UC, leading to changes in the pharmacokinetics of omeprazole.

An increasing number of studies have shown that Alzheimer’s disease (AD) is a systemic disease characterized by brain dysfunction. In this study, we aimed to investigate the effects of curcumin on the liver, an important metabolic organ, and on the brain in APPswe/PS1dE9 (APP/PS1) mice, and the interaction between these effects. Curcumin was administered to 5-month-old APP/PS1 transgenic mice for 7 consecutive days using the intragastric (ig) and intracerebroventricular (icv) administration routes, respectively. The object recognition test (ORT) and open field test (OFT) were conducted to evaluate long-term recognition memory and anxiety after curcumin administration. Levels of β-amyloid (Aβ), Aβ42, and interleukin-1β (IL-1β) in the brain and liver were measured. In the ig group, curcumin ameliorated anxiety-like behavior and suppressed the level of Aβ42 in the liver and the total Aβ in the brain. In the icv group, curcumin treatment affected the distribution of Aβ42 and IL-1β in the brain compared to the liver. There was a significant treatment–region interaction in Aβ42 level for the icv group (F(1, 24) = 17.7, p

The experimental speeds of sound combined with Brillouin frequency shifts of ethyl laurate at temperatures from 294.97 to 572.89 K along six isobaric lines from 0.1 to 10.0 MPa were measured by Ray...

Light is a vital environmental factor that can affect the synthesis of volatile organic compounds (VOCs) in grape berries. However, the mechanism through which light affects the synthesis of VOCs is still unclear for wine grapes. In our study, fruit bags with light transmittances of 50%, 15%, 5%, and 0% were used to bag the ‘Marselan’ clusters 45 days after flowering, and these treatments were named A, B, C, and D, respectively. The non-bagged clusters were used as controls (CK). The types and contents of VOCs were determined using a gas chromatography–mass spectrometer (GC–MS) with the berries 35 days before harvest (S1), 25 days before harvest (S2), and at the harvest stage (S3). RNA-seq analysis was performed on S2 and S3 samples. The results showed that the types and total contents of VOCs synthesized by fatty acid metabolic and isoprene metabolic pathways decreased with a decrease in light intensity in berries at S3. The types of VOCs synthesized by the amino acid metabolic pathway were reduced under complete shading conditions, which was consistent with results of other treatments and in the CK. The total content of VOCs was significantly reduced in shaded berries. The components of VOCs were also significantly decreased in shaded berries, except for 2-heptanol, cis-7-decenal, and trans-2-hexenal. Furthermore, RNA-seq analysis revealed that the pathway related to VOC synthesis was the alpha-linolenic acid metabolic pathway, which contained 10 differentially expressed genes from the LOXO, HPL, and ADH gene families. Correlation analysis between metabolites and differentially expressed genes of this pathway showed that the synthesis of most VOCs was highly correlated with the expression levels of LOXOs (VIT_09s0002g01080, VIT_06s0004g01450), HPL (VIT_12s0059g01060), and ADHs (VIT_04s0044g01110, VIT_18s0001g15450, VIT_18s0001g15410) (r > 0.95, p 0.95, p

An ultrasensitive detection and effective removal material was successfully developed by using a pillar[n]arene-based supramolecular polymer gel (MTP5⊃HB). The MTP5⊃HB can ultrasensitively recognize Cu2+ and Fe3+, and the limits of detection (LODs) for Cu2+ and Fe3+ are 1.55 and 2.68 nmol/L, respectively. Additionally, the in-situ generated metallogel MTP5⊃HB-Cu can exclusively detect CN−, and the LOD for CN− is 1.13 nmol/L. Noticeably, the xerogel of MTP5⊃HB-Cu can effectively remove CN− from aqueous solution with 94.40% removal rate. Test kit based on MTP5⊃HB-Cu is also prepared for convenient detection of CN−.

Aim Mesenchymal stem cell (MSC)-based therapy is being explored in treating osteoarthritis (OA). Human umbilical cord-derived mesenchymal stem cells (hUC-MSCs) are least reported. In this study, we investigated the effects of single intra-articular injections of hUC-MSCs on a rat OA model. Method hUC-MSCs were isolated from the Wharton's jelly of the human umbilical cord and identified. Eighteen Sprague-Dawley rats were used for the OA model. All rats were divided into 3 groups: hyaluronic acid (HA)+MSCs (n = 6), HA (n = 6), and control group (n = 6). One by 106 hUC-MSCs in 100 μL HA, 100 μL HA or 100 μL saline were injected into the knee joint 4 weeks post-surgery as a single dose. Cartilage degeneration was evaluated at 6 and 12 weeks after treatment with macroscopic examination, micro-computed tomography analysis, behavioral analysis, and histology. Results At 6 weeks, the HA + MSCs group had a significantly better International Cartilage Repair Society score in the femoral condyle compared to the HA and control groups. Histological analysis also showed more proteoglycan and less cartilage loss, with lower modified Mankin score in the HA + MSCs group. However, at 12 weeks there were no significant differences between groups from macroscopic examination and histological analysis. Subchondral bone sclerosis of the medial femoral condyle and behavioral tests showed no significant differences between groups at 6 and 12 weeks. Conclusion These findings indicate that single injection of hUC-MSCs can have temporary effects on decelerating the progression of cartilage degeneration in OA rats, but may not inhibit OA progression in the long-term.