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Based on previous research, this study synthesized 24 compounds by splicing the substructures of the indolyl group and the isothiocyanate group. Alternaria alternata , Phytophthora capsici , Botrytis cinerea, and Valsa mali were used to test the activity of the target compounds. At 100 μg/mL, compounds 8 , 13 , 14 , and 17 exhibited excellent inhibitory effects of more than 80% on P. capsici , B. cinerea, and V. mail . The EC 50 values of compounds 13 and 14 were 0.64 and 2.08 μg/mL, respectively. Potted antifungal activity demonstrated that compounds 13 and 14 had a protective effect of around 80% against B. cinerea at 200 μg/mL. Further physiological and biochemical studies on B. cinerea revealed that compound 13 thickened cell walls and caused mitochondrial vacuolization. Moreover, theoretical calculations indicated that the charge distribution of indolyl isothiocyanate compounds played a crucial role in the observed fungicidal activity. In summary, this study provided fundamental reference data for the derivative synthesis of these indolyl isothiocyanate compounds.

The discovery of interfacial superconductivity in monolayer FeSe/oxides has spurred intensive research interest. Here we not only extend the FeSe/FeO x superconducting interface to FeSe/NdFeO 3 but also establish robust interface-enhanced superconductivity at a very low doping level. Specifically, well-annealed FeSe/NdFeO 3 exhibits a low doping level of 0.038-0.046 e - /Fe with a larger superconducting pairing gap without a nematic gap, indicating an enhancement of the enhanced superconducting pairing strength and suppression of nematicity by the FeSe/FeO x interface compared with those of thick FeSe films. These results improve our understanding of the roles of the oxide interface in the low-electron-doped regime.

Radiochemical yields (RCYs) of isotope exchange-based 18 F-fluorination of non-carbon-centered substrates in water are rationally enhanced by adding surfactants, which increases both the rate constant k and local reactant concentrations. Among 12 surfactants, the cationic surfactant cetrimonium bromide (CTAB) and two nonionic surfactants (Tween 20 and Tween 80) were selected for their superior catalytic effects, namely, electrostatic effects or solubilization effects. For a model substrate, bis(4-methoxyphenyl)phosphinic fluoride, the 18 F-fluorination rate constant ( k ) increased up to 7-fold, while its saturation concentration rose up to 15-fold due to micelle formation, encapsulating 70-94% of the substrate. With 30.0 mmol/L CTAB, the required 18 F-labeling temperature of a typical organofluorosilicon prosthesis ([ 18 F]SiFA) decreased from 95 °C to room temperature, achieving an RCY of 22%. For an E[c(RGDyK)] 2 -derived peptide tracer with an organofluorophosphine prosthesis, the RCY in water at 90 °C achieved 25%, correspondingly increasing the molar activity (A m ). After high-performance liquid chromatography (HPLC) or solid-phase purification, the residual selected surfactant concentrations in the tracer injections were well below the FDA DII (Inactive Ingredient Database) limits or the LD50 in mice.

The reported specific positron emission tomography (PET) probes for the diagnosis of highly metastatic hepatocellular carcinoma (HCC) suffer from excessively high background uptake and fast blood clearance. Herein, five 68 Ga-labeled polyethylene glycol (PEG)-modified derivatives of the TMTP1 peptide were synthesized. The log D values decreased from -1.70 (non-PEGylated) to -1.97 to -2.94 corresponding to the increase of PEG chain length. Subnanomolar and nanomolar affinities comparable to the non-PEGylated TMTP1 derivative were revealed by the IC 50 values in SMMC-7721 cells. [ 68 Ga]Ga-NOTA-PEG 2 -TMTP1 presented a significantly higher tumor/liver ratio (4.19 ± 0.54, at 30 min post intravenous injection) and tumor/muscle ratio (2.14 ± 0.17) compared to the others and the previously radiolabeled TMTP1 derivatives. Small HCC lesions (<2 mm) in situ were detected with high tumor/liver ratio and low tumor/muscle ratio. The improved pharmacokinetics and blood clearance rate of 68 Ga-labeled TMTP1 derivatives indicated that moderate hydrophilicity due to PEGylation contributed to high-contrast PET of HCC.

A two-dimensional silicon nanosheet (2D Si NS) is promising as a lithium-ion battery anode. However, insufficient cycling life at high current density hampers its practical applications due to its easy fragileness. Rationally engineering the Si micro/nanostructure is promising to address this issue. Unfortunately, the precise construction of a dedicated micro/nanostructure into 2D Si NS meets serious challenges. Herein, a facile strategy is developed to synthesize a sandwich-like honeycomb Si NS/solid Si NS/honeycomb Si NS (h/s/h-Si NS) anode through self-assembled preparation of a sandwich-like honeycomb SiO 2 NS/solid SiO 2 NS/honeycomb SiO 2 NS template, followed by magnesiothermic reduction. This unique structure effectively enhances the mechanical strength, enlarges the specific surface area, and reserves sufficient space to accommodate the anode volume change. A conductive carbon layer is further coated on the h/s/h-Si NS (h/s/h-Si@C NS) to construct a stable electrode/electrolyte interface. The optimal h/s/h-Si@C NS displays outstanding performance with high initial Coulombic efficiency (86%), high reversible capacity (1624 mAh g -1 after 100 cycles at 1000 mA g -1 ), good rate capability (over 1000 mAh g -1 at 4000 mA g -1 ), and long cycling life even at 4000 mA g -1 (93% retained capacity after 1000 cycles). This work provides a new strategy for constructing high-performance Si electrodes for lithium-ion battery applications.

A series of lanthanide-containing water-resistant nitrates, namely RE(OH) 2 NO 3 (RE = Tb( 1 ), Dy( 2 ), Ho( 3 ), and Er( 4 )), was obtained through the hydrothermal process. As possible nonlinear optical materials, they feature a layered isomorph composed of an [REO 3 (OH) 6 ] polyhedron and an [NO 3 ] triangle, and the synergistic arrangement of the [REO 3 (OH) 6 ] and [NO 3 ] groups in their structures leads to their obvious second-order nonlinear optical effect. Nevertheless, the unique optical absorption caused by the electronic transitions on 4f-4f orbitals of lanthanides results in their second harmonic generation responses of different strengths, with 1 exhibiting 5.07 times that of KDP, but 2 - 4 showing less than half of KDP. In addition, 1 possesses an outstanding water-resistant capacity and a transparent cut-off edge around 300 nm, foreshadowing its potential value as a nonlinear optical crystal. Moreover, 1 is found to emit characteristic green fluorescence due to the typical 5 D 4 → 7 F 5 transitions of the excited Tb 3+ ions.

Our recent study showed that glutamate can inhibit dopamine oxidation via chelating copper. l-Theanine is an amino acid analogue of glutamate, whereas tea (-)-epigallocatechin-3-gallate (EGCG) is similar to dopamine in avidly undergoing oxidation. We thus hypothesized that l-theanine could also restrain EGCG oxidation via chelating copper. The current study scrutinized influences of l-theanine on EGCG oxidation in vitro and in vivo. The in vitro results showed that l-theanine and copper formed an l-theanine-copper complex with impaired redox activity of copper. Accordingly, l-theanine effectively suppressed copper-facilitated EGCG oxidation, hydroxyl radical production, and DNA damage; inhibited EGCG autoxidation which in essence involves catalysis of transition metals such as copper; and reduced EGCG oxidation-associated formation of a quinone adduct with proteins known as quinoproteins. Consistently, l-theanine significantly increased hepatic EGCG levels and reduced hepatic quinoprotein levels and liver injury in mice treated with EGCG. These lines of evidence together suggest that tea l-theanine can protect against tea catechin oxidation.

As part of continuing efforts to deepen the understanding of photo-induced mass transport in azo-containing polymers, we compared the diffraction efficiency (DE) during surface-relief grating (SRG) inscription, photo-induced molecular orientation (< P 2 >), and thermal stability in two sets of supramolecular azopolymer complexes, namely, hydrogen-bonded (H-bonded) and ionically bonded (i-bonded) complexes, both as a function of the polymer degree of polymerization (DP). To that end, poly(4-vinylpyridine) (P4VP) polymers with DPs of 41, 480, and 1900 were H-bonded at an equimolar ratio with 4-hydroxy-4'-dimethylaminoazobenzene (azoOH), and the fully quaternized derivatives of the three P4VPs (P4VPMe) were i-bonded via ion exchange to sodium 4-[(4-dimethylamino)-phenylazo]benzene sulfonate (azoSO 3 ), also known as methyl orange, where the OH functionality of azoOH is replaced by a sulfonate group. The i-bonded complexes show much better DE performances and < P 2 > levels than those of H-bonded complexes, which we relate to the liquid crystal structure of the former complexes. Fitting the < P 2 > curves by a biexponential equation leads to two parameters associated with a fast trans-cis or angular hole burning (AHB) process and a slow angular redistribution (AR) process of the azo, respectively. It is found that AHB is predominant in the H-bonded complexes, whereas the AR contribution is much greater in the i-bonded complexes, assuring their superior SRG efficiency that is enabled by the anisotropic free volume created mainly by the AR process. In each set of complexes, the SRG efficiency is much better for the lowest DP complex, while the AR contribution is constant (and low) for the H-bonded complexes and increases roughly linearly with the decrease in DP for the i-bonded complexes. The latter difference might be related to the presence of entanglements in the complexes with DPs 480 and 1900, which slow down the macroscopic movement during SRG inscription but not the molecular-scale movement in photo-orientation.

In the current era of global climate change, environmental stresses, especially drought and salt, have impaired the growth and productivity of crops, e.g., cotton. Understanding the mechanisms of plants' adaptation to these abiotic stresses is crucial to breed stress-tolerant crop species. In the present study, integrated metabolomics, lipidomics, and mass spectrometry imaging (MSI) were used to discover the spatial distribution of differential metabolites and lipids in two cottonseed cultivars with contrasting drought and salt tolerance properties. Seventeen differential metabolites and 125 differential lipids were identified. Their possible roles in augmenting stress tolerance were illustrated, which were involved in reactive oxygen species scavenging, osmotic adjustment, and cell membrane structure reconstruction. MSI analysis provided a visualization of nine differential lipids and four differential metabolites in cottonseeds with varied abundances and distributions. The results may help understand cottonseeds' convictive metabolic and lipidomic regulatory networks in coping with salinity and drought stresses and give new insights into the stress-tolerance traits relevant to other crops.

Fine particulate matter (PM 2.5 ) has been reported to be associated with neurological disorders. However, the effects of PM 2.5 on changes in metabolic and lipid profile of the brain are unclear. In this study, global metabolomics and lipidomics in mice cortex were investigated from the analyses by ultraperformance liquid chromatography-Orbitrap mass spectrometry. The partial least-squares discriminant analysis showed that the metabolite and lipid profiles were significantly altered by PM 2.5 exposure. The changed metabolic pathways including alanine, aspartate, and glutamate metabolism, carnitine metabolism, and glycerophospholipid remodeling pathway were found to be associated with a neurodegenerative process according to their corresponding molecular mechanisms. Our results indicated that PM 2.5 exposure could induce neurological damage.

Bletilla striata is widely used for stanching bleeding. In this study, polysaccharides from B. striata (BSP) were extracted by hot water. Four polysaccharides named BSP-1-BSP-4 were fractionated using DEAE-52 cellulose. BSP fractions contained sulfate, and the degrees of substitution of BSP-3 and BSP-4 were 1.59 and 1.70, respectively. Analysis of monosaccharide composition showed that four polysaccharides were mainly composed of mannan and glucose. The in vitro results showed that BSP-1-BSP-4 elicited pro-coagulant capacities by shortening the activating partial thromboplastin time, prothrombin time, and thrombin time and elevating the fibrinogen content. Immunomodulatory activity was evaluated by MTT assay, the pinocytic capacity and NO production. Although BSP fractions did not affect RAW 264.7 cell viability, they, especially BSP-2, enhanced the immunomodulatory activity by increasing the pinocytic capacity and NO production. Overall, BSP may be developed as a potential coagulant with immunomodulatory effects., Competing Interests: The authors declare no competing financial interest., (© 2020 The Authors. Published by American Chemical Society.)

Chalcogenide phase-change materials show strikingly contrasting optical and electrical properties, which has led to their extensive implementation in various memory devices. By performing spin-, time-, and angle-resolved photoemission spectroscopy combined with the first-principles calculation, we report the experimental results that the crystalline phase of GeSb 2 Te 4 is topologically nontrivial in the vicinity of the Dirac semimetal phase. The resulting linearly dispersive bulk Dirac-like bands that cross the Fermi level and are thus responsible for conductivity in the stable crystalline phase of GeSb 2 Te 4 can be viewed as a 3D analogue of graphene. Our finding provides us with the possibility of realizing inertia-free Dirac currents in phase-change materials.

Redox-active metal oxide nanoparticles show varying oxidizing capacities and injury potentials toward biological systems. Here, two metal oxide libraries including transition-metal-doped Co 3 O 4 and PdO-Co 3 O 4 with strong chemical contacts were design-synthesized and used to investigate their biological injury potential and mechanisms using zebrafish as a model organism. Among different dopants, Cu significantly increased the oxidizing capacity of Co 3 O 4 . An increased amount of PdO resulted in higher density of heterojunctions, which also led to higher oxidizing capacity. The oxidizing capacity of these nanoparticles was positively correlated with higher mortality of dechorionated embryos and severe larval skin injury upon exposure. Using transgenic zebrafish Tg ( LysC :eGFP), we show in real time that the redox-active nanoparticles induced skin injury and activated the infiltration of immune cells. Such inflammatory response was confirmed by the increased mRNA expression level of Nrf2a, HO-1 , IL-1β , and IL-6 genes. Although the exposure to the nanoparticles alone was not lethal, the skin injury did lower the tolerance level against other environmental contaminants. More importantly, after withdrawing from the nanoparticle exposure, larvae with skin injury could recover within 24 h in uncontaminated medium, indicating such injury was transient and recoverable.

Near-infrared (NIR) light-responsive, injectable hydrogels are among the most promising drug delivery systems for localized anticancer therapy owing to its minimally invasive administration and remote-controlled manner. However, most currently reported NIR-responsive hydrogels were usually generated through physical mixing of thermosensitive polymers and photothermal conversion agents. In this study, a novel type of dynamic-covalent hydrogel (GelPV-DOX-DBNP) with NIR light-triggered drug release behavior was rationally designed for chemo-photothermal combination treatment of tumors. Concretely, this NIR-responsive hydrogel was formed by specific benzoxaborole-carbohydrate interactions between benzoxaborole (BOB)-modified hyaluronic acid (BOB-HA) and fructose-based glycopolymer (PolyFru), where photosensitizer perylene diimide zwitterionic polymer (PDS), reductant ascorbic acid (Vc), anticancer drug doxorubicin (DOX) as well as photothermal nanoparticles (DB-NPs) were encapsulated, simultaneously. Upon 660 nm light irradiation, both PDS and Vc within the designed hydrogel can convert oxygen into hydrogen peroxide, which could make hydrogel be degraded through the breakage of dynamic covalent bonds based on benzoxaborole-carbohydrate interactions, leading to NIR light-activatable release of DOX and DB-NPs from GelPV-DOX-DBNP. Furthermore, the released DB-NPs can convert 915 nm light irradiation into heat, enabling the application of GelPV-DOX-DBNP as a NIR-responsive drug delivery platform for both chemotherapy and photothermal therapy (PTT). In vivo results prove that GelPV-DOX-DBNP exhibited a markedly enhanced chemo-photothermal synergistic therapy for 4T1 tumor model mice, compared to chemotherapy alone or PTT. This work presents a new strategy to construct NIR light-responsive hydrogel as one alternative drug delivery system for anticancer applications.

The silkworm genome has been deeply sequenced and assembled, but accurate genome annotation, which is important for modern biological research, remains far from complete. To improve silkworm genome annotation, we carried out a proteogenomics analysis using 9.8 million mass spectra collected from different tissues and developmental stages of the silkworm. The results confirmed the translational products of 4307 existing gene models and identified 1701 novel genome search-specific peptides (GSSPs). Using these GSSPs, 74 novel gene-coding sequences were identified, and 121 existing gene models were corrected. We also identified 1182 novel junction peptides based on an exon-skipping database that resulted in the identification of 973 alternative splicing sites. Furthermore, we performed RNA-seq analysis to improve silkworm genome annotation at the transcriptional level. A total of 1704 new transcripts and 1136 new exons were identified, 2581 untranslated regions (UTRs) were revised, and 1301 alternative splicing (AS) genes were identified. The transcriptomics results were integrated with the proteomics data to further complement and verify the new annotations. In addition, 14 incorrect genes and 10 skipped exons were verified using the two analysis methods. Altogether, we identified 1838 new transcripts and 1593 AS genes and revised 5074 existing genes using proteogenomics and transcriptome analyses. Data are available via ProteomeXchange with identifier PXD009672. The large-scale proteogenomics and transcriptome analyses in this study will greatly improve silkworm genome annotation and contribute to future studies.

Poly(3-hexylthiophene) (P3HT)-based organic solar cells (OSCs) have been extensively studied due to unique advantages of P3HT such as roll-to-roll and large-area printing fabrication, but a poor short-circuit current density greatly limits the enhancement of power conversion efficiency (PCE). Herein, via the thiophene-fused aromatic heterocycle as a "π-bridge", two "A-π-D-π-A"-type acceptors have been designed and synthesized for P3HT-based OSCs. The aromaticity of the fused thiophene ring has effectively stabilized the quinoid population, thus strengthening the intramolecular charge transfer and further improving the current density. Owing to the weaker electron-withdrawing ability of the thiophene-fused benzotriazole unit in JC2 than the thiophene-fused benzothiadiazole unit in JC1 , a blue-shifted absorption occurs for JC2 to show a better complementarity with P3HT to improve the light-harvesting efficiency and current density of the derived OSCs, and an uplifted lowest unoccupied molecular orbital energy level is also achieved for JC2 to obtain higher voltages. Thus, the P3HT: JC2 -based device exhibits a PCE of 6.24% with a high J SC of 13.96 mA cm -2 and a V OC of 0.71 V, significantly exceeding those of the P3HT: JC1 device with a PCE of 2.80%, a J SC of 10.66 mA cm -2 , and a V OC of 0.48 V. This indicates that the fusion of a thiophene ring onto a benzotriazole unit is an effective strategy to balance the V OC and J SC of P3HT-based OSCs to achieve excellent photovoltaic performances.

This study aimed to investigate the efficacy of polydopamine nanoparticles (Pdop-NPs) as a subcutaneous antigen delivery vehicle in antitumor therapy. The nanoparticles were prepared by self-polymerization of dopamine in an aerobic and weak alkaline solution, and the tumor model antigen-ovalbumin (OVA) was grafted onto the nanoparticles to form OVA@Pdop nanoparticles (OVA@Pdop-NPs). The particle size of OVA@Pdop-NPs was 232.8 nm with a zeta potential of -23.4 mV, and the loading capacity of OVA protein was 754 μg mg -1 . OVA@Pdop-NPs were essentially noncytotoxic and even demonstrated a slightly viability effect on bone-marrow-derived dendritic cells (BMDCs). As compared to free OVA, OVA@Pdop-NPs exhibited higher cellular uptake and were easier to migrate to lymph nodes in vivo. Both in vitro and in vivo experiments showed that OVA@Pdop-NPs promoted the maturation of DCs with up-regulated expression of major histocompatibility complex (MHC), costimulatory molecules, and cytokines. When used to treat the mice bearing OVA-MC38 colon tumor, OVA@Pdop-NPs could effectively activate OVA-specific cytotoxic CD8 + T cells and induce the production of memory CD4 + and CD8 + T cells and thus led to significantly suppressed tumor growth. All the preliminary data demonstrated the application potential of OVA@Pdop-NPs as a vaccine vector in cancer immunotherapy.

Herein, we fabricated a new yolk-shell-structured mesoporous silica nanoparticle (YMSN) with multifunctionalities of fluorescence imaging, photothermal therapy (PTT), and drug delivery by using a fluorescein isothiocyanate-doped silica nanoparticle partially covered by patchy gold as the core. Different from the conventional selective etching procedure, the multifunctional silica core is left intact, and the alkali etching mainly occurs in a hexadecyl trimethyl ammonium bromide/silica hybrid layer, which leads to the formation of the void space in YMSNs. In addition, the utilization of patchy gold as the PTT agent can avoid the shield against the outer irradiation on the core. Results show that the as-prepared YMSNs have a good biocompatibility in the concentration of 0-1000 μg·mL -1 and a high doxorubicin-loading capability (8.04 wt %). In vitro and in vivo antitumor experiments reveal that the resulting YMSNs can be utilized for chemo- and photothermic combination therapy as well as optical imaging.

Theanine, a unique bioactive constituent from tea ( Camellia sinensis) leaves, is widely used as a functional ingredient and dietary supplement. To evaluate the anti-inflammatory and hepatoprotective effects of theanine and its molecular mechanism, the lipopolysaccharide (LPS)-induced inflammation mouse model was employed in this study. The survival rate of mice in the theanine-treated group increased significantly compared with that of LPS-only group mice. Furthermore, ICR male mice were randomly divided into three or four groups: control, LPS (LPS treatment only), LPS + theanine (20 mg/kg/day), and theanine (theanine treatment only). The results showed that compared with the LPS group, the liver damage and oxidative stress of the theanine-treated group decreased significantly, based on plasma alanine aminotransferase (ALT) and aspartate aminotransferase (AST) concentrations, hepatic total superoxide dismutase (T-SOD), and malondialdehyde (MDA) levels, and histological scores and apoptosis [terminal deoxynucleotide transferase-mediated deoxyuridine triphosphate nick end-labeling (TUNEL) staining and caspase-3 activity] in the liver tissues. Furthermore, compared with no treatment, pretreatment with theanine significantly decreased the release of interleukin (IL)-1β and tumor necrosis factor (TNF)-α, inhibited the expression of several inflammatory factors (including IL-1β, TNF-α, and IL-6), and increased the IL-10/interferon (IFN)-γ ratio in the hepatic tissues. In the LPS-induced inflammation model, theanine inhibited the expression of proinflammatory mediators involved in the nuclear factor-kappa B (NF-κB) pathway, such as inducible nitric oxide synthase (iNOS) and matrix metalloproteinase-3 (MMP-3), and attenuated the phosphorylation of NF-κB in the hepatic tissues. Moreover, theanine suppressed the acute-phase response (elevated nitric oxide and C-reactive protein levels). Furthermore, theanine suppressed the LPS-induced inflammatory state by normalizing hypothalamic-pituitary-adrenal (HPA) axis hyperactivity. Taken together, the results suggest that theanine potentially ameliorates LPS-induced inflammation and acute liver injury; molecular mechanism of action may involve normalization of HPA axis hyperactivity and inactivation of the NF-κB signaling pathway.

A new microporous metal-organic framework (MOF) with formula {Co 2 (oba) 4 (3-bpdh) 2 }4H 2 O [oba = 4,4'-oxybis(benzoic acid); 3-bpdh = N, N'-bis-(1-pyridine-3-yl-ethylidene)-hydrazine] was assembled, and its morphology was found to undergo a microrod-to-nanosphere transformation with temperature variation. Core-shell Au@Pd functional nanoparticles (NPs) were successfully encapsulated in the center of the monodisperse nanospheres, and Pt NPs were well-dispersed and fully immobilized on the surface of Au@Pd@1Co to build the Pt/Au@Pd@1Co composites, which exhibited NPs catalytic activity for the reverse water gas shift reaction. The core-shell Au@Pd NPs in MOF significantly enchanced the CO selectivity of the catalyst, and the Pt NP loading on the surface of the nanosphere afforded a desirable CO 2 conversion.