RESUMO
A rapid photoelectrochemical (PEC) sensor was constructed for nitrite detection in food based on the one-step chemical etching strategy of BiOCl/Zn0.5Cd0.5S (BOC/ZCS) nanocomposites by nitrite. BOC/ZCS heterojunction was prepared by a simple coprecipitation method, and it was found that BOC/ZCS showed significant photoelectrochemical (PEC) activity. The results of this study confirmed that the decrease in the photocurrent of the sensor was linked to the etching of ZCS by nitrite under acidic conditions. Under optimized conditions, the BOC/ZCS-based PEC sensor showed good analytical properties for detecting nitrite, with linear ranges of 1-100 µM and 100-600 µM. The detection limit of the sensor was 0.41 µM (S/N = 3). Excellent repeatability, reproducibility, low background noise, and immunity to interference were demonstrated using the proposed system, and satisfactory results were achieved for the nitrite assay using real samples. These results demonstrate a new method for nitrite detection developed using the proposed PEC sensor.
Assuntos
Técnicas Eletroquímicas , Limite de Detecção , Nitritos , Nitritos/análise , Técnicas Eletroquímicas/instrumentação , Bismuto/química , Zinco/química , Zinco/análise , Nanocompostos/química , Processos Fotoquímicos , Contaminação de Alimentos/análiseRESUMO
Induction of autophagic death in cancer cells is one of the promising strategies for the development of anti-cancer therapeutics. In the present study, we designed and synthesized a series of isatin Schiff base derivatives containing thioether structures. After discovering the highly active target compound H13 (IC50 = 4.83 µM) based on in vitro antiproliferation, we also found it had a high safety against normal cells HEK293 with CC50 of 69.01 µM, indicating a sufficient therapeutic window. In addition, to provide reference for subsequent studies, a model was successfully constructed by Sybyl software. Preliminary mechanistic studies suggested that H13-induced apoptosis may be closely related to ROS accumulation and mitochondrial dysfunction. Subsequent studies revealed that H13 inhibited cell proliferation by inducing cellular autophagy mainly through blocking signal of the PI3K/AKT/mTOR pathway. Altogether, these results suggested that H13 was potentially valuable as a lead compound.
RESUMO
BACKGROUND: Non-small-cell lung cancer is a prevalent malignancy associated with significant morbidity and mortality rates. Tryptanthrin and its derivatives have exhibited potent antitumor activity. OBJECTIVE: This study aims to investigate the inhibitory effect of a novel synthesized tryptanthrin derivative D6 on proliferation and the possible mechanism of human non-small cell lung cancer cell lines (A549) in vitro. METHODS: In this study, MTT assay, cell migration, colony formation assay, cell cycle analysis, cell apoptosis, JC- 1 staining assay, reactive oxygen species analysis, proteomics, western blotting, high content screening and absorption titrations analysis were performed. RESULTS: We found that D6 inhibited both the proliferation and migration, induced cell cycle arrest in the G2/M phase, increased levels of ROS, decreased mitochondrial membrane potential, and promoted apoptosis in A549 cells. Further mechanistic studies found that D6 reduced EGFR expression in A549 cells and inhibited the EGFR pathway by decreasing phosphorylation levels of EGFR, Stat3, AKT and Erk1/2. Moreover, DNA damage induced by D6 involved an increase in p53/MDM2 ratio and concentration-dependent accumulation of micronuclei. CONCLUSION: D6 demonstrated significant antitumor activity against A549 cells by inhibiting the EGFR signaling pathway, inducing DNA damage, and subsequently leading to oxidative stress, apoptosis, and cell cycle arrest. Our findings suggest that D6 exhibits potential as an NSCLC drug, owing to its attributes such as antiproliferative activity and ability to induce apoptosis by attenuating the EGFR-mediated signaling pathway.
Assuntos
Antineoplásicos , Apoptose , Carcinoma Pulmonar de Células não Pequenas , Proliferação de Células , Dano ao DNA , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Receptores ErbB , Neoplasias Pulmonares , Quinazolinas , Humanos , Apoptose/efeitos dos fármacos , Dano ao DNA/efeitos dos fármacos , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Carcinoma Pulmonar de Células não Pequenas/patologia , Carcinoma Pulmonar de Células não Pequenas/metabolismo , Receptores ErbB/metabolismo , Receptores ErbB/antagonistas & inibidores , Neoplasias Pulmonares/tratamento farmacológico , Neoplasias Pulmonares/patologia , Neoplasias Pulmonares/metabolismo , Proliferação de Células/efeitos dos fármacos , Quinazolinas/farmacologia , Quinazolinas/química , Quinazolinas/síntese química , Antineoplásicos/farmacologia , Antineoplásicos/química , Antineoplásicos/síntese química , Estrutura Molecular , Relação Estrutura-Atividade , Células Tumorais CultivadasRESUMO
The in-depth mechanisms of microRNA regulation of premature ovarian failure (POF) remain unclear. Crispr-cas9 technology was used to construct transgenic mice. The qPCR and Western blot was used to detect the expression level of genes. H&E staining were used to detect ovarian pathological phenotypes. We found that the expression levels of microRNA-3061 were significantly higher in ovarian granulosa cells (OGCs) of POF mouse models than in controls. The miR-3061+/-/AMH-Cre+/- transgenic mice manifested symptoms of POF. RNA-Seq and luciferase reporter assay confirmed that the PAX7 was one of the target genes negatively regulated by microRNA-3061 (miR-3061-5p). Moreover, PAX7 mediated the expression of non-canonical Wnt/Ca2+ signalling pathway by binding to the motifs of promoters to stimulate the transcriptional activation of Wnt5a and CamK2a. In contrast, specific knock-in of microRNA-3061 in OGCs significantly downregulated the expression levels of PAX7 and inhibited the expression of downstream Wnt/Ca2+ signalling pathway. We also discerned a correlation between the expression levels of mRNAs of the Wnt/Ca2+ signalling pathway and the levels of E2 and FSH in POF patients by examining gene expression in the follicular fluid-derived exosomes of women. We confirmed that overexpression of microRNA-3061 induced proliferative inhibition of OGCs and ultimately induced POF in mice by suppressing the transcription factor PAX7 and downregulating expression levels of its downstream Wnt/Ca2+ signalling pathway genes.
Assuntos
Regulação para Baixo , Células da Granulosa , Camundongos Transgênicos , MicroRNAs , Fator de Transcrição PAX7 , Insuficiência Ovariana Primária , Via de Sinalização Wnt , Animais , Feminino , MicroRNAs/genética , MicroRNAs/metabolismo , Insuficiência Ovariana Primária/genética , Insuficiência Ovariana Primária/metabolismo , Camundongos , Células da Granulosa/metabolismo , Fator de Transcrição PAX7/metabolismo , Fator de Transcrição PAX7/genética , Sinalização do Cálcio/genética , HumanosRESUMO
Monolithic distributed Bragg reflector (DBR) cavity which directly integrates fiber Bragg gratings (FBGs) into the photosensitive RE-doped fibers is a promising configuration in constructing compact and efficient single frequency fiber lasers (SFFLs). Yet, the doping level of rare-earth (RE) ions has generally to be sacrificed in the classical Ge-photosensitized RE-doped silica fibers because of the dramatic refractive index increase caused by the introduction of Ge. Here, we demonstrate an approach to realize the trade-off between photosensitivity and RE doping concentration. We validate that the addition of a small amount of cerium (0.37wt.%) instead of Ge could photosensitize Yb3+-doped silica fiber (YDF), while maintaining fiber numerical aperture (NA) at 0.12 under a high 2.5-wt.% Yb doping level. Based on the short monolithic DBR cavity constructed by this germanium-free photosensitive highly YDF, a 1064â nm fiber laser with a 48.6% slope efficiency and an over 200â mW power on two orthogonally polarized modes could be realized. Further stable and linear-polarized 1064â nm SFFL is also demonstrated in a designed monolithic polarization maintaining cavity with an output power of 119â mW and an efficiency of 26.4%. Our results provide an alternative way to develop photosensitive highly RE-doped fibers towards monolithic laser cavity application.
RESUMO
Organic-inorganic hybrid metal halides have unique optical and electronic properties, which are advantageous in the study of nonlinear optical materials. To investigate the effect of stereoactive lone pair electrons and the induction of organic cations on the structure of hybrid antimony(III) halides on nonlinear optics, we synthesize two noncentrosymmetric hybrid antimony(III)-based halide single crystals (TMA)3Sb2X9 (TMA = NH(CH3)3+, X = Cl, Br) by a room-temperature slow evaporation method, and their single-crystal structures, phase transition, X-ray photoelectron spectroscopy, and energy-band structure calculations are studied. More importantly, second-harmonic generation results of (TMA)3Sb2X9 (X = Cl, Br) are about 0.7 and 0.8 × KH2PO4(KDP), respectively. Interestingly, (TMA)3Sb2Cl9 single crystals undergo a reversible structural transition from Pc (No. 7) at room temperature to P21/c (No. 14) at 400 K, while the (TMA)3Sb2Br9 single crystals belong to the noncentrosymmetric space group R3c (No. 161), which clarifies the previous results. This work not only deepens the understanding of the role in lone pair electrons and organic cations in the structural induction in antimony-based halide perovskite materials but also provides guidance for subsequent nonlinear optical explorations.
RESUMO
BACKGROUND: Xanthomonas oryzae pv. oryzae (Xoo) is often considered one of the most destructive bacterial pathogens causing bacterial leaf blight (BLB), resulting in significant yield and cost losses in rice. In this study, a series of novel derivatives containing the isopropanolamine moiety linked to various substituted phenols and piperazines were designed, synthesized and screened. RESULTS: Antibacterial activity results showed that most compounds had good inhibitory effects on Xoo, among which compound W2 (EC50 = 2.74 µg mL-1) exhibited the most excellent inhibitory activity, and W2 also had a certain curative effect (35.89%) on rice compared to thiodiazole copper (TC) (21.57%). Scanning electron microscopy (SEM) results indicated that compound W2 could cause rupture of the Xoo cell membrane. Subsequently, proteomics and quantitative real-time polymerase chain reaction revealed that compound W2 affected the physiological processes of Xoo and may exert antibacterial activity by targeting the two-component system pathway. Interestingly, W2 upregulated Xoo's methyltransferase to impact on its pathogenicity. CONCLUSION: The present study offers a promising phenolic-piperazine-sopropanolamine compound as an innovative antibacterial strategy by specifically targeting the two-component system pathway and inducing upregulation of methyltransferase to effectively impact Xoo's pathogenicity. © 2024 Society of Chemical Industry.
Assuntos
Antibacterianos , Xanthomonas , Xanthomonas/efeitos dos fármacos , Antibacterianos/farmacologia , Antibacterianos/síntese química , Antibacterianos/química , Fenóis/farmacologia , Fenóis/química , Desenho de Fármacos , Piperazinas/farmacologia , Piperazinas/química , Piperazinas/síntese química , Oryza/microbiologia , Doenças das Plantas/microbiologiaRESUMO
Rare-earth-doped silica-based composite glasses (Re-SCGs) are widely used as high-quality laser gain media in defense, aerospace, energy, power, and medical applications. The variable regional chemical environments of Re-SCGs can induce new photoluminescence properties of rare-earth ions but can cause the selective aggregation of rare-earth ions, limiting the application of Re-SCGs in the field of high-power lasers. Here, topological engineering is proposed to adjust the degree of cross-linking of phase-separation network chains in Re-SCGs. A combination of experimental and theoretical characterization techniques suggested that the selective aggregation of rare-earth ions originates from the formation of phase-separated structures in glasses. The decomposition of nanoscale phase separation structures to the sub-nanometer scale, enabled by incorporating Al3+ ions, not only maintains the high luminescence efficiency of rare earth ions but also increases light transmittance and reduces light scattering. Furthermore, our investigation encompassed the exploration of the inhibitory mechanism of Al3+ ions on phase-separation structures, as well as their influence on the spectral characteristics of Re-SCGs. This work provides a new design concept for composite glass materials doped with rare-earth ions and could broaden their application in the field of high-power lasers.
RESUMO
BACKGROUND: Plant bacterial infections and plant viruses seriously affect the yield and quality of crops. Based on the various activities of tryptanthrin, a series of tryptanthrin analogues bearing F and piperazine moieties were designed, synthesized, and evaluated for their biological activities against three plant bacteria and tobacco mosaic virus (TMV). RESULTS: Bioassay results indicated that compounds 6a-6l displayed excellent antibacterial activities in vitro and 6a-6c and 6g exhibited better antiviral activities against TMV than commercial ribavirin. In particular, 6b showed the most effect on Xanthomonas oryzae pv. oryzae (Xoo) with a half-maximal effective concentration (EC50 ) of 1.26 µg mL-1 , compared with the commercial pesticide bismerthiazol (BT; EC50 = 34.3 µg mL-1 ) and thiodiazole copper (TC; EC50 = 73.3 µg mL-1 ). Meanwhile, 6a also had the best antiviral activity at 500 µg mL-1 for curative, protection, and inactivation purposes, compared with ribavirin in vivo. CONCLUSION: Compound 6b could cause changes in bacterial morphology, induce the accumulation of reactive oxygen species, promote apoptosis of bacterial cells, inhibit the formation of biofilm, and block the growth of Xoo cells. Proteomic analysis revealed major differences in the bacterial secretory system pathways T2SS and T6SS, which inhibited membrane transport. Molecular docking revealed that 6a and 6g could interact with TMV coat protein preventing virus assembly. These results suggest that tryptanthrin analogues bearing F and piperazine moieties could be promising candidate agents for antibacterial and antiviral use in agricultural production. © 2023 Society of Chemical Industry.
Assuntos
Oryza , Quinazolinas , Vírus do Mosaico do Tabaco , Xanthomonas , Ribavirina/metabolismo , Ribavirina/farmacologia , Simulação de Acoplamento Molecular , Piperazina/metabolismo , Piperazina/farmacologia , Proteômica , Testes de Sensibilidade Microbiana , Antibacterianos/farmacologia , Antivirais/farmacologia , Doenças das Plantas , Relação Estrutura-AtividadeRESUMO
Mn(II)-based hybrid halides have attracted great attention from the optoelectronic fields due to their nontoxicity, special luminescent properties, and structural diversity. Here, two novel organic-inorganic hybrid Mn(II)-based halide single crystals (1-mpip)MnCl4·3H2O and (1-mpip)2MnCl6 (1-mpip = 1-methylpiperazinium, C5H14N2+) were grown by a slow evaporation method in ambient atmosphere. Interestingly, (1-mpip)2MnCl6 single crystals exhibit the green emission with a PL peak at 522 nm and photoluminescence quantum yields (PLQYs) of ≈5.4%, whereas (1-mpip)MnCl4·3H2O single crystals exhibit no emission characteristics. More importantly, there exists a thermal-induced phase transformation from (1-mpip)MnCl4·3H2O to emissive (1-mpip)2MnCl6 at 372 K. Moreover, a reversible luminescent conversion between (1-mpip)MnCl4·3H2O and (1-mpip)2MnCl6 was simply achieved when heated to 383 K and placed in a humid environment or sprayed with water. This work not only deepens the understanding of the thermal-induced phase transformation and humidity-sensitive luminescent conversion of hybrid Mn(II)-based halides, but also provides a guidance for thermal and humidity sensing and anticounterfeiting applications of these hybrid materials.
RESUMO
Taking inspiration from the use of natural product-derived bactericide candidates in drug discovery, a series of novel 9-aliphatic amine tryptanthrin derivatives were designed, synthesized, and evaluated for their biological activity against three plant bacteria. The majority of these compounds exhibited excellent antibacterial activity in vitro. Compound 7c exhibited a significantly superior bacteriostatic effect against Xanthomonas axonopodis pv Citri (Xac), Xanthomonas oryzae pv Oryzae (Xoo), and Pseudomonas syringae pv Actinidiae (Psa) with final corrected EC50 values of 0.769, 1.29, and 15.5 µg/mL, respectively, compared to the commercial pesticide thiodiazole copper which had EC50 values of 58.8, 70.9, and 91.9 µg/mL. Preliminary mechanism studies have demonstrated that 7c is capable of altering bacterial morphology, inducing reactive oxygen species accumulation, promoting bacterial cell apoptosis, inhibiting normal cell growth, and affecting cell membrane permeability. Moreover, in vivo experiments have substantiated the effectiveness of 7c as a therapeutic and defensive agent against the citrus canker. The proteomic analysis has unveiled that the major disparities are located within the bacterial secretion system pathway, which hinders membrane transportation. These discoveries imply that 7c could be an auspicious prototype for developing antiphytopathogenic bacterial agents.
Assuntos
Oryza , Xanthomonas , Proteômica , Oxidiazóis/farmacologia , Doenças das Plantas/microbiologia , Testes de Sensibilidade Microbiana , Antibacterianos/farmacologia , Bactérias , Oryza/microbiologiaRESUMO
Nd3+-doped three-level (4F3/2-4I9/2) fiber lasers with wavelengths in the range of 850-950â nm are of considerable interest in applications such as bio-medical imaging and blue and ultraviolet laser generation. Although the design of a suitable fiber geometry has enhanced the laser performance by suppressing the competitive four-level (4F3/2-4I11/2) transition at â¼1 µm, efficient operation of Nd3+-doped three-level fiber lasers still remains a challenge. In this study, taking a developed Nd3+-doped silicate glass single-mode fiber as gain medium, we demonstrate efficient three-level continuous-wave lasers and passively mode-locked lasers with a gigahertz (GHz) fundamental repetition rate. The fiber is designed using the rod-in-tube method and has a core diameter of 4 µm with a numerical aperture of 0.14. In a short 4.5-cm-long Nd3+-doped silicate fiber, all-fiber CW lasing in the range of 890 to 915â nm with a signal-to-noise ratio (SNR) greater than 49â dB is achieved. Especially, the laser slope efficiency reaches 31.7% at 910â nm. Furthermore, a centimeter-scale ultrashort passively mode-locked laser cavity is constructed and ultrashort pulse at 920â nm with a highest GHz fundamental repetition is successfully demonstrated. Our results confirm that Nd3+-doped silicate fiber could be an alternative gain medium for efficient three-level laser operation.
RESUMO
The natural alkaloids of tryptanthrin and their derivatives have a wide range of biological activities. In this research, four series of azatryptanthrin derivatives containing 4-aza/3-aza/2-aza/1-aza tryptanthrin were prepared by condensation cyclization reaction against plant pathogens to develop a new natural product-based bacterial pesticide. Compound 4Aza-8 displayed a remarkable growth inhibitory effect on pathogenic bacteria of Xanthomonas axonopodis pv. citri (Xac), Xanthomonas oryzae pv. Oryzae (Xoo), and Pseudomonas syringae pv. actinidiae (Psa) with the final corrected EC50 values of 0.312, 1.91, and 18.0 µg/mL, respectively, which were greatly superior than that of tryptanthrin (Tryp). Moreover, 4Aza-8 also showed effective therapeutic and protective activities in vivo on citrus canker. Further mechanism studies on Xac elucidated that compound 4Aza-8 was able to affect the growth curve of Xac and the formation of biofilm, cause severe shrinkage in bacterial morphology, increase reactive oxygen species levels, and induce apoptosis in bacterial cells. Quantitative analysis of differential protein profiles found that the major differences were mainly concentrated on the endometrial protein in the bacterial secretion system pathway, which blocked the membrane transport and affected the transfer of DNA to the host cell. In summary, these research results suggest that 4Aza-8 represents a promising anti-phytopathogenic-bacteria agent, which is worth being further investigated as a bactericide candidate.
Assuntos
Citrus , Oryza , Xanthomonas , Antibacterianos/farmacologia , Citrus/microbiologia , Bactérias , Biofilmes , Doenças das Plantas/microbiologia , Oryza/microbiologia , Testes de Sensibilidade MicrobianaRESUMO
A series of 1,4-naphthoquinone derivatives containing were synthesized as anti-cancer agents and the crystal structure of compound 5a was confirmed by X-ray diffraction. In addition, the inhibitory activities against four cancer cell lines (HepG2, A549, K562, and PC-3) were tested, respectively, and compound 5i showed significant cytotoxicity on the A549 cell line with the IC50 of 6.15 µM. Surprisingly, in the following preliminary biological experiments, we found that compound 5i induced autophagy by promoting the recycling of EGFR and signal transduction in the A549 cell, resulting in the activation of the EGFR signal pathway. The potential binding pattern between compound 5i and EGFR tyrosine kinase (PDB ID: 1M17) was also identified by molecular docking. Our research paves the way for further studies and the development of novel and powerful anti-cancer drugs.
Assuntos
Antineoplásicos , Naftoquinonas , Humanos , Células A549 , Linhagem Celular Tumoral , Proliferação de Células , Simulação de Acoplamento Molecular , Naftoquinonas/farmacologia , Antineoplásicos/farmacologia , Antineoplásicos/química , Morte Celular , Receptores ErbB/metabolismo , Autofagia , Ensaios de Seleção de Medicamentos Antitumorais , Relação Estrutura-AtividadeRESUMO
Plant bacterial illnesses are common and cause dramatic damage to agricultural goods all over the world, yet there are few efficient bactericides to alleviate them at present. To discover novel antibacterial agents, two series of quinazolinone derivatives with novel structures were synthesized and their bioactivity against plant bacteria was tested. Combining CoMFA model search and the antibacterial bioactivity assay, D32 was identified as a potent antibacterial inhibitor against Xanthomonas oryzae pv. Oryzae (Xoo), with an EC50 value of 1.5 µg/mL, much better in inhibitory capacity compared to bismerthiazol (BT) and thiodiazole copper (TC) (31.9 and 74.2 µg/mL). The activities of compound D32 against rice bacterial leaf blight in vivo were 46.7% (protective activities) and 43.9% (curative activities), better than commercial drug thiodiazole copper (29.3% protective activities and 30.6% curative activities). Flow cytometry, proteomics, reactive oxygen species, and key defense enzymes were used to further investigate the relevant mechanisms of action of D32. The identification of D32 as an antibacterial inhibitor and revelation of its recognition mechanism not only open the possibility of developing new therapeutic strategies for treatment of Xoo but also provide clues for elucidation of the acting mechanism of quinazolinone derivative D32, which is a possible clinical candidate worth in-depth study.
Assuntos
Oryza , Xanthomonas , Relação Quantitativa Estrutura-Atividade , Cobre/farmacologia , Oxidiazóis/farmacologia , Testes de Sensibilidade Microbiana , Doenças das Plantas/microbiologia , Antibacterianos/química , Oryza/microbiologia , Relação Estrutura-AtividadeRESUMO
In this study, a series of novel tryptanthrin derivatives were synthesized and their inhibitory activities against selected human cancer cell lines, namely, lung (A549), chronic myeloid leukemia (K562), prostate (PC3), and live (HepG2), were evaluated using a methyl thiazolyl tetrazolium colorimetric (MTT) assay. Among the tested compounds, compound C1 exhibited a promising inhibitory effect on the A549 cell line with an IC50 value of 0.55 ± 0.33 µM. The observation of the cell morphological result showed that treatment with C1 could significantly inhibit the migration of A549 cells through the cell migration assay. Moreover, after treatment with C1, the A549 cells exhibited a typical apoptotic morphology and obvious autophagy. In addition, the detection of apoptosis and the mitochondrial membrane potential indicated that C1 induced A549 cell apoptosis via modulating the levels of Bcl2 family members and disrupted the mitochondrial membrane potential. Compound C1 also suppressed the expression of cyclin D1 and increased the expression of p21 in the A549 cells, inducing cell cycle arrest in the G2/M phase in a dose dependent manner. The further mechanism study found that C1 markedly increased the transformation from LC3-I to LC3-II. Taken together, our results suggest that C1 is capable of inhibiting the proliferation of non-small cell lung cancer (NSCLC) cells, inducing cell apoptosis, and triggering autophagy.
Assuntos
Carcinoma Pulmonar de Células não Pequenas , Neoplasias Pulmonares , Humanos , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Neoplasias Pulmonares/tratamento farmacológico , Apoptose , Autofagia , Proliferação de Células , Linhagem Celular TumoralRESUMO
Herein, a new series of 2-chloro-N-(5-(2-oxoindolin-3-yl)-4H-pyrazol-3-yl) acetamide derivatives containing 1,3,4-thiadiazole (10a-i) and 4H-1,2,4-triazol-4-amine (11a-r) moiety was designed, synthesised as novel anticancer agents. The antiproliferative activity values indicated that compound 10 b stood as the most potent derivative with IC50 values of 12.0 nM and 10 nM against A549 and K562 cells, respectively. Mechanism investigation and docking studies of 10 b indicated that it possessed good apoptosis characteristic and dose-dependent growth arrest of A549 and K562 cells, blocked cell cycle into G2/M phase. Interestingly, 10 b suppressed the growth of A549 and K562 cells via modulation of EGFR and p53-MDM2 mediated pathway.
Assuntos
Antineoplásicos , Rubiaceae , Humanos , Células K562 , Ensaios de Seleção de Medicamentos Antitumorais , Indóis/farmacologia , Rubiaceae/metabolismo , Proliferação de Células , Apoptose , Relação Estrutura-Atividade , Linhagem Celular Tumoral , Simulação de Acoplamento Molecular , Estrutura MolecularRESUMO
BACKGROUND: Plant bacterial diseases have seriously affected the yield and quality of crops, among which rice bacterial leaf blight (BLB), caused by Xanthomonas oryzae pv. oryzae has seriously affected the yield of rice. As plant-pathogenic bacteria gradually become resistant to existing bactericides, it is necessary to find effective bactericides with novel structures. RESULTS: Herein, a series of compounds containing quinazolin-4(3H)-one and disulfide moieties were designed and synthesized using a facile synthetic method. The bioassay results revealed that most target compounds possessed noticeable antibacterial activity against Xanthomonas oryzae pv. oryzae. Particularly, compound 2-(butyldisulfanyl) quinazolin-4(3H)-one (1) exhibited remarkable antibacterial activity with the half effective concentration (EC50 ) of 0.52 µg mL-1 . Additionally, compound 1 was confirmed to inhibit the growth of the bacteria, change the bacterial morphology, and increase the level of reactive oxygen species. Proteomics, and RT-qPCR analysis results indicated that compound 1 could downregulate the expression of Pil-Chp histidine kinase chpA encoded by the pilL gene, and the potting experiments proved that compound 1 exhibits significant protective activity against BLB. CONCLUSIONS: Compound 1 may weaken the pathogenicity of Xanthomonas oryzae pv. oryzae by inhibiting the bacterial growth and blocking the pili-mediated twitching motility without inducing the bacterial apoptosis. This study indicates that such derivatives could be a promising scaffold to develop a bacteriostat to control BLB. © 2022 Society of Chemical Industry.
Assuntos
Oryza , Xanthomonas , Tiram/farmacologia , Antibacterianos/farmacologia , Antibacterianos/química , Dissulfetos/farmacologia , Doenças das Plantas/prevenção & controle , Doenças das Plantas/microbiologiaRESUMO
OBJECTIVE: To study the clinical features and power spectral entropy (PSE) of electroencephalography signals in Wilson's disease (WD) patients with dystonia. METHODS: Several scale evaluations were performed to assess the clinical features of WD patients. Demographic information and electroencephalography signals were obtained in all subjects. RESULTS: 34 WD patients with dystonia were recruited in the case group and 24 patients without dystonia were recruited in the control group. 20 healthy individuals were included in the healthy control group. The mean body mass index (BMI) in the case group was significantly lower than that in the controls (p < .05). The case group had significantly higher SAS, SDS, and Bucco-Facial-Apraxia Assessment scores (p < .05). Total BADS scores in the case group were lower than those in the control group (p < .01). Note that 94.11% of the case group presented with dysarthria and 70.59% of them suffered from dysphagia. Dysphagia was mainly related to the oral preparatory stage and oral stage. Mean power spectral entropy (PSE) values in the case group were significantly different (p < .05) from those in the control group and the healthy group across the different tasks. CONCLUSIONS: The patients with dystonia were usually accompanied with low BMI, anxiety, depression, apraxia, executive dysfunction, dysarthria and dysphagia. The cortical activities of the WD patients with dystonia seemed to be more chaotic during the eyes-closed and reading tasks but lower during the swallowing stages than those in the control group.
Assuntos
Distonia , Degeneração Hepatolenticular , Humanos , Apraxias/diagnóstico , Transtornos de Deglutição/diagnóstico , Disartria/diagnóstico , Distonia/complicações , Distonia/fisiopatologia , Eletroencefalografia , Entropia , Degeneração Hepatolenticular/complicações , Degeneração Hepatolenticular/fisiopatologia , Estudos de Casos e ControlesRESUMO
A novel and effective method to improve scintillation properties of glass-ceramics, such as intensity enhancement and decay-time shortening, is reported in this work. Compared with crystal scintillators, glass scintillators always have the problems of low efficiency and long decay; how to solve them has always been a scientific puzzle in the field of scintillation glass-ceramics. The plasma enhancement effect can be predicted to solve the above problems. Ag+ ions were diffused into glasses by ion exchange, and then Ag nanoparticles and CsPbBr3 quantum dots were formed by heat treatment. The structure of the CsPbBr3 perovskite consists of a series of shared corner PbBr6 octahedra with Cs ions occupying the cuboctahedral cavities. By using Ag and the plasma resonance effect, the photoluminescence intensity of CsPbBr3 quantum dot glasses was enhanced by 3 times, its radioluminescence intensity increased by 6.25 times, and its decay time was reduced by a factor of more than one. Moreover, the mechanism of photoluminescence and radioluminescence enhanced by Ag and plasma was discussed based on the experimental results and finite-difference time-domain method. We concluded that the increase in radioluminescence intensity was related to plasma enhancements and the energy exchange between Ag nanoclusters and CsPbBr3 quantum dots. Doping Ag is a valid means to improve the scintillation luminescence of CsPbBr3 quantum dot glasses, which can be applied in the field of scintillation.