Visible-Light-Promoted Cyanoalkylation/Cyclization Cascade Reaction to Assemble Polyheterocycles in Continuous Flow.

This study describes a visible-light-induced cascade reaction for preparing cyanoalkyl-containing polyheterocycles initiated by the photoinduced radical cascade addition of N-arylacrylamide derivatives using cyclic oxime esters as radical sources followed by cyanoalkyl-mediated cyclization. This protocol features outstanding functional group compatibility, providing a variety of desired phenanthridine derivatives in moderate to good yields. Moreover, the application of a microflow technique enhanced these reactions compared with the equivalent batch reaction, significantly reducing reaction times to 10 min.

A lysosome-targetable fluorescent probe for the ratiometric detection of formaldehyde in living cells and in vivo.

Inspired by the synthetic method of benzoxazine derivatives and our previous research, a fluorescent probe (SWJT-6) was designed for formaldehyde (FA) detection based on the cyclization reaction. The synthetic SWJT-6 showed excellent colorimetric and ratiometric response to formaldehyde, and could be perfectly used as test strips to detect formaldehyde. It also showed a fast detection time (3 min), low detection limit (5.65 µM) and high selectivity for formaldehyde within various interfering analytes. In addition, SWJT-6 has been successfully applied in bioimaging of intracellular and lysosomal formaldehyde in both HeLa cells and zebrafish.

Novel Sulfonamide Derivatives Containing a Piperidine Moiety as New Bactericide Leads for Managing Plant Bacterial Diseases.

Plant bacterial diseases are an intractable problem due to the fact that phytopathogens have acquired strong resistances for traditional pesticides, resulting in restricting the quality and yield of agricultural products around the world. To develop new agrochemical alternatives, we prepared a novel series of sulfanilamide derivatives containing piperidine fragments and assessed their antibacterial potency. The bioassay results revealed that most molecules displayed excellent in vitro antibacterial potency towards Xanthomonas oryzae pv. oryzae (Xoo) and Xanthomonas axonopodis pv. citri (Xac). In particular, molecule C4 exhibited outstanding inhibitory activity toward Xoo with EC50 value of 2.02 µg mL-1, which was significantly better than those of the commercial agents bismerthiazol (EC50 = 42.38 µg mL-1) and thiodiazole copper (EC50 = 64.50 µg mL-1). A series of biochemical assays confirmed that compound C4 interacted with dihydropteroate synthase, and irreversibly damaged the cell membrane. In vivo assays showed that the molecule C4 presented acceptable curative and protection activities of 34.78% and 39.83%, respectively, at 200 µg mL-1, which were greater than those of thiodiazole and bismerthiazol. This study highlights the valuable insights for the excavation and development of new bactericides that can concurrently target dihydropteroate synthase and bacterial cell membranes.

Research on Diffusible Signal Factor-Mediated Quorum Sensing in Xanthomonas: A Mini-Review.

Xanthomonas spp. are important plant pathogens that seriously endanger crop yields and food security. RpfF is a key enzyme that is involved in the synthesis of diffusible signal factor (DSF) signals and predominates in the signaling pathway regulating quorum sensing (QS) in Xanthomonas. Currently, novel RpfF enzyme-based quorum sensing agents have been proposed as a promising strategy for the development of new pesticides. However, few reports are available that comprehensively summarize the progress in this field. Therefore, we provide a comprehensive review of the recent advances in DSF-mediated QS and recently reported inhibitors that are proposed as bactericide candidates to target the RpfF enzyme and control plant bacterial diseases.

Electrochemical Tri- and Difluoromethylation-Triggered Cyclization Accompanied by the Oxidative Cleavage of Indole Derivatives.

Considering their unique roles in organic synthesis, and pharmaceutical and agrochemical applications, the development of fluoroalkylation, cyclization, and indole oxidative cleavage are important topics. Herein, an unprecedented electrochemical tri- and difluoromethylation/cyclization/indole oxidative cleavage process occurring in an undivided cell is presented. The protocol employs a readily prepared Langlois reagent as the fluoroalkyl source, affording a series of tri- or difluoromethylated 2-(2-acetylphenyl)isoquinoline-1,3-diones in good yields with excellent stereoselectivity. It is worth noting that this new methodology merges the fluoroalkylation/cyclization of N-substituted acrylamide alkenes with the oxidative cleavage of an indole C(2)=C(3) bond under external oxidant-free conditions.

Visual detection of S2- with a paper-based fluorescence sensor coated with CdTe quantum dots via headspace sampling.

A simple method was developed in this work for facile and visual detection of S2- using a paper-based fluorescence (FL) sensor coated with CdTe quantum dots (QDs) by headspace sampling. With the addition of hydrochloric acid, the target S2- in the liquid phase would transform to H2 S, which was released to headspace and quenched the FL of CdTe QDs in a linear manner through a gas-solid reaction, with any possible liquid-phase interference avoided. The regular quenching caused by S2- in analyte solution with increased concentration could be easily observed by the naked eye, and the limit of detection (LOD) for this method was 0.13 µM and 0.93 µM for FL and visual sensing, respectively, comparable or not to that by other sensing probes. A relative standard deviation of 1.2% was accomplished from seven replicated measurements, implying the high reproducibility, and the recovery for the spiked water samples ranging from 94 to 103%, and illustrating the satisfactory reliability of this method. Moreover, the preparation of this paper sensor was facile and did not require any complicated or time-consuming procedures for additional modification or functionalization as for other probes previously reported.

Low Power, Low Temperature and Atmospheric Pressure Plasma-Induced Polymerization: Facile Synthesis and Crystal Regulation of Covalent Organic Frameworks.

Low temperature and atmospheric pressure plasma-induced polymerization was demonstrated as a fast and facile strategy for tailoring of packing phase of COF-1 as well as preparing diverse covalent organic frameworks (COFs) including both two-dimensional (2D) COFs and three-dimensional (3D) COFs. By regulating the solvents, the fast construction of well-ordered AB staggered COF-1 and AA eclipsed COF-1 was facilely realized in minutes. The plasma approach presented here led to the rapid preparation of eight classical 2D COFs, including boronate ester-linkage (COF-5, COF-8 and COF-10), azine-linkage (NUS-2), ß-ketoenamine-linkage (TpPa, TPBD), imine-linkage (ILCOF-1, Py-COF), and 3D-COF-102 (boroxine linkage) in less than 1 hour. Different from conventional methods, the proposed methodology required much less time, lower power, no extra heating, inert-gas protection and pressure. The fast nucleation and growth of COFs with good crystallinity, morphology and thermal stability can be achieved under mild conditions.

Single Bimetallic Lanthanide-Based Metal-Organic Frameworks for Visual Decoding of a Broad Spectrum of Molecules.

Distinguishing the delicate structural differences among molecules is a critical and challenging task in biological/chemical analysis. A molecular decoding strategy has recently become promising to differentiate similar molecules, which is advantageous over the common sensing methods mostly used for detecting a single target. However, the design of an ideal molecular decoder is still strictly hindered by the tailored preparation of probes for particular molecules and the severe lack of widespread feasibility. We herein for the first time proposed to use single bimetallic lanthanide-based metal-organic frameworks (Ln-MOFs) as a powerful, versatile probe for fast and facile decoding of homologues, isomers, enantiomers, and even deuterated isotopomers, based on the unique host-guest interaction of a specific target with the Ln-MOF which could provide an according visual output based on the modulated energy transfer process.

Titanium Incorporation into Zr-Porphyrinic Metal-Organic Frameworks with Enhanced Antibacterial Activity against Multidrug-Resistant Pathogens.

This study uses metal-organic frameworks (MOFs) alone without any added antibacterial ingredients as the nonantibiotic agent for photodynamic therapy (PDT) of chronic wounds infected by multidrug-resistant (MDR) bacteria. Nanoparticles (NPs) of MOFs (PCN-224) are incorporated with titanium through a facile cation exchange strategy. The obtained bimetallic PCN-224(Zr/Ti) shows greatly enhanced photocatalytic performance for the generation of reactive oxygen species under visible light, which is responsible for the effective antibacterial activities. The PCN-224(Zr/Ti) NPs are loaded onto lactic-co-glycolic acid nanofibers to prepare a wound dressing, which shows high biocompatibility and minimal cytotoxicity. The wound dressing is efficient for PDT-based in vivo healing of the chronic wound infected by MDR bacteria. Most importantly, this work does not involve any additional antibacterial agents, which is facile, low cost, and in particular, greatly explores the potential of MOFs as a powerful nonantibiotic agent in PDT.

Childhood Neglect and Psychological Distress Among Pregnant Women: The Chain Multiple Mediation Effect of Perceived Social Support and Positive Coping.

This study aimed to investigate the association between childhood neglect and psychological distress in pregnant women and to assess whether perceived social support and coping styles mediated this association. Pregnant women (N = 276) recruited from the prenatal clinic of a comprehensive hospital in China participated in this study. Participants reported their experiences of childhood neglect and abuse, depression, anxiety, perceived social support, and coping styles. Childhood neglect was positively associated with psychological distress. Perceived social support mediated the relationship between childhood neglect and psychological distress. Perceived social support and positive coping acted as chain mediators between childhood neglect and psychological distress. Childhood neglect is a risk factor for psychological distress during pregnancy independent of childhood abuse; perceived social support and positive coping can influence this relationship.

Estimation of Temporal Gait Parameters Using a Wearable Microphone-Sensor-Based System.

Most existing wearable gait analysis methods focus on the analysis of data obtained from inertial sensors. This paper proposes a novel, low-cost, wireless and wearable gait analysis system which uses microphone sensors to collect footstep sound signals during walking. This is the first time a microphone sensor is used as a wearable gait analysis device as far as we know. Based on this system, a gait analysis algorithm for estimating the temporal parameters of gait is presented. The algorithm fully uses the fusion of two feet footstep sound signals and includes three stages: footstep detection, heel-strike event and toe-on event detection, and calculation of gait temporal parameters. Experimental results show that with a total of 240 data sequences and 1732 steps collected using three different gait data collection strategies from 15 healthy subjects, the proposed system achieves an average 0.955 F1-measure for footstep detection, an average 94.52% accuracy rate for heel-strike detection and 94.25% accuracy rate for toe-on detection. Using these detection results, nine temporal related gait parameters are calculated and these parameters are consistent with their corresponding normal gait temporal parameters and labeled data calculation results. The results verify the effectiveness of our proposed system and algorithm for temporal gait parameter estimation.

Test of the stress sensitization model in adolescents following the pipeline explosion.

PURPOSE: The stress sensitization model states that early traumatic experiences increase vulnerability to the adverse effects of subsequent stressful life events. This study examined the effect of stress sensitization on development of posttraumatic stress disorder (PTSD) symptoms in Chinese adolescents who experienced the pipeline explosion. METHODS: A total of 670 participants completed self-administered questionnaires on demographic characteristics and degree of explosion exposure, the Childhood Trauma Questionnaire (CTQ), and the Posttraumatic Stress Disorder Checklist-Civilian Version (PCL-C). Associations among the variables were explored using MANOVA, and main effects and interactions were analyzed. RESULTS: Overall MANOVA tests with the PCL-C indicated significant differences for gender (F=6.86, p=.000), emotional abuse (F=6.79, p=.000), and explosion exposure (F=22.40, p=.000). There were significant interactions between emotional abuse and explosion exposure (F=3.98, p=.008) and gender and explosion exposure (F=2.93, p=.033). CONCLUSIONS: Being female, childhood emotional abuse, and a high explosion exposure were associated with high PTSD symptom levels. Childhood emotional abuse moderated the effect of explosion exposure on PTSD symptoms. Thus, stress sensitization influenced the development of PTSD symptoms in Chinese adolescents who experienced the pipeline explosion as predicted by the model.

Two-dimensional MoS2 nanosheets as a capillary GC stationary phase for highly effective molecular screening.

Stable layered MoS2 nanosheets were employed as a stationary phase in gas chromatography. A wide range of different analytes were screened with excellent separation efficiency.

RNA m5C methylation: a potential modulator of innate immune pathways in hepatocellular carcinoma.

RNA 5-methylcytosine (m5C) methylation plays a crucial role in hepatocellular carcinoma (HCC). As reported, aberrant m5C methylation is closely associated with the progression, therapeutic efficacy, and prognosis of HCC. The innate immune system functions as the primary defense mechanism in the body against pathogenic infections and tumors since it can activate innate immune pathways through pattern recognition receptors to exert anti-infection and anti-tumor effects. Recently, m5C methylation has been demonstrated to affect the activation of innate immune pathways including TLR, cGAS-STING, and RIG-I pathways by modulating RNA function, unveiling new mechanisms underlying the regulation of innate immune responses by tumor cells. However, research on m5C methylation and its interplay with innate immune pathways is still in its infancy. Therefore, this review details the biological significance of RNA m5C methylation in HCC and discusses its potential regulatory relationship with TLR, cGAS-STING, and RIG-I pathways, thereby providing fresh insights into the role of RNA methylation in the innate immune mechanisms and treatment of HCC.

Expanding the Structural Diversity of Tubulin-Targeting Agents: Development of Highly Potent Benzimidazoles for Treating Fungal Diseases.

Benzimidazoles, the representative pharmacophore of fungicides, have excellent antifungal potency, but their simple structure and single site of action have hindered their wider application in agriculture. In order to extend the structural diversity of tubulin-targeted benzimidazoles, novel benzimidazole derivatives were prepared by introducing the attractive pyrimidine pharmacophore. 2-((6-(4-(trifluoromethyl)phenoxy)pyrimidin-4-yl)thio)-1H-benzo[d]imidazole (A25) exhibited optimal antifungal activity against Sclerotinia sclerotiorum (S. s.), affording an excellent half-maximal effective concentration (EC50) of 0.158 µg/mL, which was higher than that of the reference agent carbendazim (EC50 = 0.594 µg/mL). Pot experiments revealed that compound A25 (200 µg/mL) had acceptable protective activity (84.7%) and curative activity (78.1%), which were comparable with that of carbendazim (protective activity: 90.8%; curative activity: 69.9%). Molecular docking displayed that multiple hydrogen bonds and π-π interactions could be formed between A25 and ß-tubulin, resulting in a stronger bonding effect than carbendazim. Fluorescence imaging revealed that the structure of intracellular microtubules can be changed significantly after A25 treatment. Overall, these remarkable antifungal profiles of constructed novel benzimidazole derivatives could facilitate the application of novel microtubule-targeting agents.

LncRNA LINC01232 Enhances Proliferation, Angiogenesis, Migration and Invasion of Colon Adenocarcinoma Cells by Downregulating miR-181a-5p.

LncRNAs play crucial roles in the progression of colon adenocarcinoma (COAD), but the role of LINC01232 in COAD has not received much attention. The present study was designed to explore the related mechanisms of LINC01232 in the progression of COAD. LINC01232, miR-181a-5p, p53, c-myc, Bcl-2, cyclin D1, p16, Bax, VEGF, E-cadherin, vimentin, N-cadherin and SDAD1 expressions were determined by western blot and qRT-PCR. CCK-8, tubule formation, and Transwell assays were employed to detect proliferation, angiogenesis, and migration/invasion of COAD cells, respectively. The relationship between LINC01232 and miR-181a-5p was predicted by LncBase Predicted v.2, and then verified through dual luciferase reporter gene assay. According to the results, LINC01232 was highly expressed in COAD cells and enhanced proliferation, angiogenesis, migration, and invasion of COAD cells. Downregulated LINC01232 promoted expression of p53 and p16, and inhibited c-myc, Bcl-2 and cyclin D1 expressions in COAD cells, while upregulation of LINC01232 generated the opposite effects. LINC01232 was negatively correlated with miR-181a-5p while downregulated miR-181a-5p could reverse the effects of siLINC01232 on cell proliferation, angiogenesis, migration, and invasion. Similarly, miR-181a-5p mimic could also offset the effect of LINC01232 overexpression. SiLINC01232 increased the expressions of Bax and E-cadherin, and decreased the expressions of VEGF, vimentin, N-cadherin and SDAD1, which were partially attenuated by miR-181a-5p inhibitor. Collectively, LINC01232 enhances the proliferation, migration, invasion, and angiogenesis of COAD cells by decreasing miR-181a-5p expression.

Multi-color fluorescence sensing platform for visual determination of norfloxacin based on a terbium (Ш) functionalized covalent organic framework.

Sensitive and visual determination of fluoroquinolone antibiotics (FQs) is of great significance since their abuse and inappropriate handling can be problematic. Herein, we propose a lanthanide covalent organic framework fluorescence sensing system (Tb@COF-Ru) with visualization capability to determine the FQs level, where Tb@COF was employed as the sensing probe, while the red-emitting Ru(bpy)32+ serves as a constant red fluorescent background. With increasing norfloxacin concentration, the green fluorescence of Tb3+ is gradually enhanced, finally realizing the multicolor fluorescence change from red to green. With a smartphone for RGB analysis, visual monitoring and quantitative analysis were realized without any sophisticated instrument. Limits of detection for the fluorescence quantitative and visual mode for norfloxacin were 0.33 nM and 7.3 µM, respectively. This method was rapid (1 min) and visualized, providing a simple analysis of various food matrices (honey, milk, egg and beef) and water samples for trace FQs.

Novel Benzothiazole Derivatives as Potential Anti-Quorum Sensing Agents for Managing Plant Bacterial Diseases: Synthesis, Antibacterial Activity Assessment, and SAR Study.

As quorum sensing (QS) regulates bacterial pathogenicity, antiquorum sensing agents have powerful application potential for controlling bacterial infections and overcoming pesticide/drug resistance. Identifying anti-QS agents thus represents a promising approach in agrochemical development. In this study, the anti-QS potency of 53 newly prepared benzothiazole derivatives containing an isopropanolamine moiety was analyzed, and structure-activity relationships were examined. Compound D3 exhibited the strongest antibacterial activity, with an in vitro EC50 of 1.54 µg mL-1 against Xanthomonas oryzae pv oryzae (Xoo). Compound D3 suppressed QS-regulated virulence factors (e.g., biofilm, extracellular polysaccharides, extracellular enzymes, and flagella) to inhibit bacterial infection. In vivo anti-Xoo assays indicated good control efficiency (curative activity, 47.8%; protective activity, 48.7%) at 200 µg mL-1. Greater control efficiency was achieved with addition of 0.1% organic silicone or orange peel essential oil. The remarkable anti-QS potency of these benzothiazole derivatives could facilitate further novel bactericidal compound development.

Construction of a Ceramic Appearance Design System Based on Technology for Internet of Things.

The planning and design of intelligent storage systems in ceramic parks based on the industrial Internet of Things technology are proposed. Based on the analysis of the storage demand of ceramic parks, information transformation is carried out according to the original manual operation mode. The RFID technology is applied to the overall planning of the warehouse area and the deployment of the software; it is applied to the overall planning of the RFID system, the hardware deployment of the two-dimensional warehouse system, and the integration of the RFID technology and the software deployment of the two-dimensional warehouse system. It realizes the close cooperation between the information system and hardware equipment, optimizes the system process, and improves the level of warehouse management.In addition, smart terminal ceramics refer to those with fine ceramic appearances or functionalities in smart terminal products, such as smartphones, smart watches, and other wearable devices, in the field of consumer electronics, including ceramic back plates, middle frames, buttons, fingerprint recognition sheets on mobile phones and ceramic cases, bracelets, and back covers on smart watches. Aside the excellent performance and aesthetic properties of ceramic materials, they can also be adapted to the trends in 5G and wireless communication technology. From the perspective of high strength, high toughness, and colorful nano-zirconia ceramics, this article was aimed to review the development process and industrialization application process.

Design, Synthesis, and Biological Profiles of Novel 1,3,4-Oxadiazole-2-carbohydrazides with Molecular Diversity.

To unceasingly expand the molecular diversity of 1,3,4-oxadiazole-2-carbohydrazides, herein, small fragments (including -CH2-, -OCH2-, and -SCH2-) were incorporated into the target compounds to screen out the potential succinate dehydrogenase inhibitors (SDHIs). The bioassay results showed that the antifungal effects (expressed by EC50) against Sclerotinia sclerotiorum, Botryosphaeria dothidea, Fusarium oxysporum, and Colletotrichun higginsianum could reach 1.29 (10a), 0.63 (8h), 1.50 (10i), and 2.09 (10i) µg/mL, respectively, which were slightly lower than those of carbendazim (EC50 were 0.69, 0.13, 0.55, and 0.80 µg/mL, respectively). Especially, compound 10h was extremely bioactive against Gibberella zeae (G. z.) with an EC50 value of 0.45 µg/mL. This outcome was better than that of fluopyram (3.76 µg/mL) and was similar to prochloraz (0.47 µg/mL). In vivo trials against the corn scab (infected by G. z.) showed that compound 10h had control activity of 86.8% at 200 µg/mL, which was better than that of boscalid (79.6%). Further investigations found that compound 10h could inhibit the enzymatic activity of SDH in the G. z. strain with an IC50 value of 3.67 µM, indicating that potential SDHIs might be developed. Additionally, the other biological activities of these molecules were screened simultaneously. The anti-oomycete activity toward Phytophthora infestans afforded a minimal EC50 value of 3.22 µg/mL (10h); compound 4d could strongly suppress the growth of bacterial strains Xanthomonas axonopodis pv. citri and Xanthomonas oryzae pv. oryzae with EC50 values of 3.79 and 11.4 µg/mL, respectively; and compound 10a displayed some insecticidal activity toward Plutella xylostella. Given their multipurpose features, these frameworks could be actively studied as potential pesticide leads.