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A rare-earth salt Yb(OTf)3-catalyzed regioselective hydroamination of ynamides with anilines and p-toluenesulfonamide has been developed. This protocol provided facile access to a diverse range of amidines with good functional group tolerance in moderate to high yields.

A direct and straightforward thiocyanation of enamides with NH4SCN under metal-free conditions has been accomplished. A variety of (E)-β-thiocyanoenamides are readily produced in a regio- and stereo-selective manner. The protocol features mild reaction conditions, good functional group tolerance and operational simplicity. The potential utility of this strategy was further demonstrated by transformation of thiocyanate into thiotetrazole-containing compounds and a Pd-catalyzed cross-coupling reaction to afford six- or seven-membered sulfur-containing heterocycles. Mechanistic insights into the reaction indicate that the reaction may proceed via a radical mechanism.

Inflammatory bowel disease (IBD) is a chronic intestinal disease, which was commonly found in westerners whereas is increasingly prevalent in Asia because of the changing eating habits. In previous research, we found that a water-soluble polysaccharide isolated from Auricularia auricular-judae (Bull.)-a kind of edible mushroom (Aap)-is composed of β-1,3 glycosidic bonds, which is regarded as therapeutic or protective substance in enteritis. We therefore aimed to find the preventing effect of Aap on IBD. Here, we reported that pre-administration of Aap not only ameliorated weight loss, colon damage, and mucosal inflammation in colitis mice, but also prevented the damage of intestinal barrier by reducing the D-lactic acid and diamine oxidase level in plasma. Through high-throughput sequencing, we found that Aap changed gut microbiota composition. Furthermore, the preventing effect was transmissible via horizontal feces transfer from Aap-treated mice to normal mice. Our results indicated that oral administration of Aap is a promising protective substance of IBD. PRACTICAL APPLICATION: Our study proved that Auricularia auricula polysaccharide had substantial preventing effect on DSS-induced colitis in mice. This research might lay the theoretical foundation and technical support for the development of related functional foods. People could also enhance their gut immunity by eating Auricularia auricular in their daily life. Auricularia auricular as a highly nutritious agricultural product showed the broad significance in nutrition and food function.

By adding one-step memory to enrich the model of discrete-time quantum walk on the Caylay graph of the dihedral group, the model of quantum walk with memory on the Cayley graph of the dihedral group is constructed. The Fourier Transform is used to analyze the walk, and a formula for probability distribution and time-average probability distribution is given. According to the one-to-one correspondence between quantum walk with memory on a regular graph and quantum walk without memory on the corresponding line digraph, the diagrammatic counterpart of quantum walk with one-step memory on the Cayley graph of the dihedral group is presented. Moreover, basic probabilistic properties of the proposed model are further studied using numerical simulation method. Furthermore, the similarities and differences are discussed in comparison to the memoryless model.

Introduction: COVID-19 is a coronavirus-based infectious illness that was first detected at the end of 2019 in Wuhan, China. The novel virus induces severe acute respiratory syndrome (SARS-CoV-2) and has spread globally, resulting in an ongoing pandemic. There is still a lack of evidence for direct comparison of favipiravir therapy. Network meta-analysis (NMA), may incorporate direct and indirect comparisons in a pooled computation while depending on strong assumptions and premises. This study provides evidence-based recommendations on the safety of currently used clinical pharmacological treatments compared to favipiravir for COVID-19 patients. Methodology: We conducted a systematic review and Bayesian NMA. We searched the primary databases and clinical trials center for reports of short-term, randomized controlled trials (RCTs) of favipiravir for COVID-19 treatment. The primary endpoints here considered were any adverse events observed or reported during the treatment cycle with estimates of odds ratio (OR) and 95% confidence interval (CI), until November 6, 2021. Results: Between January 2020 and July 2021, 908 individuals were randomly assigned to one of the seven active prescription medication regimens or placebo in this study, generating seven direct comparisons on 12 data points. The safety of favipiravir over the four clinically efficacious monotherapies or combinations including tocilizumab, arbidol, lopinavir + ritonavir, and chloroquine remained unknown due to the lack of a significant difference and the limited sample size. Conclusions: Overall, comparative rankings could assist doctors and guideline developers in decision-making. We have also concluded that the safety of favipiravir requires further attention.

Removal of low concentration NO in enclosed space by a new combined process incorporating vacuum ultraviolet (VUV)-induced oxidation and wet absorption process at room temperature was studi...

Since of their adjustable pore structure and variety of metal sites, MOFs materials have infinite possibilities, but their low intrinsic activity hinders them from being employed in electrolytic water. The sulfurization and oxidation of MOFs has proven to be a feasible technique for producing highly active catalytic materials. Here, the MOFs are completely converted to hydroxide by treatment with alkaline solutions only. Electron microscopy demonstrates that hydroxides generated from various MOFs retain the complete profile of the precursor and contain a two-dimensional lamellar or mesoporous structure. Fe-MIL-88(A)-OH, a two-dimensional structural transformation product generated from Fe-MIL-88(A), demonstrates significant OER performance increase. At the same 300 mV overpotential, Fe-MIL-88(A)-OH delivers 83 times the current density of Fe-MIL-88(A) and 16 times that of commercial IrO

Pulmonary fibrosis, a severe condition that can progress to respiratory failure and death, is characterized by aberrant activation/proliferation of fibroblasts and excessive extracellular matrix (ECM) deposition and has limited therapeutic options. Identifying novel mediators of pulmonary fibrosis is currently needed to facilitate the development of more effective therapeutic strategies targeting pulmonary fibrosis. The present study was designed to investigate whether transforming growth factor-β (TGF-β) induced protein (TGFBI), an extracellular matrix protein, regulates pulmonary fibrosis in vitro and in vivo and the possible mechanism of actions. It was found that protein expressions of TGFBI were significantly upregulated and G-protein signaling modulator 2 (GPSM2) expression downregulated in fibrotic lung tissues from bleomycin (BLM)-induced rats and TGF-β1-stimulated human lung IMR-90 fibroblasts. Either silencing TGFBI with specific siRNA or treatment with the TGF-β signaling inhibitor SB431542 significantly inhibited TGF-β1-induced fibrotic effects and dysregulation of GPSM2 and Snail expressions in IMR-90 fibroblasts. Moreover, GPSM2 overexpression also inhibited TGF-β1-induced fibrotic effects and Snail upregulation in IMR-90 fibroblasts. Silencing Snail with specific siRNA attenuated TGF-β1-induced fibrotic effects. Therefore, our findings suggest that the extracellular matrix protein TGFBI mediates pulmonary fibrosis through regulation of the GPSM2/Snail axis, which identifies TGFBI as a novel mediator of pulmonary fibrosis and may be a potential therapeutic target for the treatment of pulmonary fibrosis.

Cells reprogram their transcriptomes to adapt to external conditions. The SAGA (Spt-Ada-Gcn5 acetyltransferase) complex is a highly conserved transcriptional coactivator that plays essential roles in cell growth and development, in part by acetylating histones. Here, we uncover an autoregulatory mechanism of the Saccharomyces cerevisiae SAGA complex in response to environmental changes. Specifically, the SAGA complex acetylates its Ada3 subunit at three sites (lysines 8, 14 and 182) that are dynamically deacetylated by Rpd3. The acetylated Ada3 lysine residues are bound by bromodomains within SAGA subunits Gcn5 and Spt7 that synergistically facilitate formation of SAGA homo-dimers. Ada3-mediated dimerization is enhanced when cells are grown under sucrose or under phosphate-starvation conditions. Once dimerized, SAGA efficiently acetylates nucleosomes, promotes gene transcription and enhances cell resistance to stress. Collectively, our work reveals a mechanism for regulation of SAGA structure and activity and provides insights into how cells adapt to environmental conditions.

Understanding the functional dynamics of neural oscillations in the sensory thalamus is essential for elucidating the perception and modulation of neuropathic pain. Local field potentials were recorded from the sensory thalamus of twelve neuropathic pain patients. Single and combinational neural states were defined by the activity state of a single or paired oscillations. Relationships between the duration or occurrence rate of neural state and pre-operative pain level or pain relief induced by deep brain stimulation were evaluated. Results showed that the occurrence rate of the single neural state of low-beta oscillation was significantly correlated with pain relief. The duration and occurrence rate of combinational neural states of the paired low-beta with delta, theta, alpha, high-beta or low-gamma oscillations were more significantly correlated with pain relief than the single neural states. Moreover, these significant combinational neural states formed a local oscillatory network with low-beta oscillation as a key node. The results also showed correlations between measures of combinational neural states and subjective pain level as well. The duration of combinational neural states of paired alpha with delta or theta oscillations and the occurrence rate of neural states of the paired delta with low-beta or low-gamma oscillations were significantly correlated with pre-operative pain level. In conclusion, this study revealed that the integration of oscillations and the functional dynamics of neural states were differentially involved in modulation and perception of neuropathic pain. The functional dynamics could be biomarkers for developing neural state-dependent deep brain stimulation for neuropathic pain.

To investigate the efficacy of propranolol and metoprolol on unstable angina pectoris patients and their effects on high-sensitivity C-reactive protein and lipoprotein associated phospholipase A2. Altogether 138 unstable angina pectoris patients admitted to our hospital were considered and enrolled into two groups in view of the treatment methods. Among them, 62 patients in the control group were treated with propranolol and 76 cases in the observation group were treated with metoprolol. The efficacy and incidence of adverse reactions of patients after treatment in both groups were recorded, and their seizure frequency and duration of angina pectoris were compared. The cardiac functions of both groups before and after treatment were compared: left ventricular ejection fraction, left ventricular end diastolic volume and left ventricular end systolic volume. Enzyme-linked immunosorbent assay was employed to examine the concentration of inflammatory factors in serum before and after treatment: serum high-sensitivity C-reactive protein and serum lipoprotein-associated phospholipase A2. The risk factors affecting their efficacy were assessed through logistic regression analysis. The expression of cardiac function in the observation group after treatment was dramatically better than that in the control group. The seizure frequency, duration and inflammatory factor level in the observation group after treatment were dramatically lower than those in the control group. The clinical efficacy in the observation group was obviously higher than that in the control group. There was no marked difference in incidence of adverse reactions between both groups. Multivariate logistic regression analysis identified that gender, history of diabetes, hypertension, levels of high-sensitivity C-reactive protein, lipoprotein associated phospholipase A2 before treatment and treatment methods were independent risk factors affecting their efficacy. Compared with propranolol, metoprolol can dramatically improve the cardiac function of unstable angina pectoris patients, control the seizure frequency and duration of angina pectoris and reduce the level of inflammatory factors.

The finite dihedral group generated by one rotation and one reflection is the simplest case of the non-abelian group. Cayley graphs are diagrammatic counterparts of groups. In this paper, much attention is given to the Cayley graph of the dihedral group. Considering the characteristics of the elements in the dihedral group, we propose a model of three-state discrete-time quantum walk (DTQW) on the Caylay graph of the dihedral group with Grover coin. We derive analytic expressions for the the position probability distribution and the long-time limit of the return probability starting from the origin. It is shown that the localization effect is governed by the size of the underlying dihedral group, coin operator and initial state. We also numerically investigate the properties of the proposed model via the probability distribution and the time-averaged probability at the designated position. The abundant phenomena of three-state Grover DTQW on the Caylay graph of the dihedral group can help the community to better understand and to develop new quantum algorithms.

Pulmonary fibrosis is a severe condition with limited therapeutic options and characterized by increased fibroblast activation and progressive accumulation of extracellular matrix. Ghrelin, a gastrointestinal hormone, has been reported to possess protective roles in lung diseases including pulmonary fibrosis. However, the precise mechanisms underlying the protective effects of ghrelin remain unknown. The present study was designed to investigate the effects of ghrelin on transforming growth factor-β1 (TGF-β1)-induced pulmonary fibrosis in vitro and in vivo and the possible mechanism of action. It was found that ghrelin significantly attenuated TGF-β1-induced fibrotic responses in human lung fibroblast (IMR-90) cells and bleomycin (BLM)-induced fibrotic lung tissues. Meanwhile, ghrelin decreased the expressions of miR-125a-5p and phosphorylated smad2/3 and increased protein expressions of Kruppel-like factor 13 (KLF13) in vivo and in vitro. Ghrelin–induced anti-fibrotic effects and smad2/3 downregulation in TGF-β1-stimulated IMR-90 cells were markedly reversed by miR-125a-5p mimics and KLF13 siRNA. Furthermore, miR-125a-5p directly targeted KLF13 in IMR-90 cells. Our findings suggest that ghrelin attenuates TGF-β1-induced pulmonary fibrosis via the miR-125a-5p/KLF13 axis, which supports ghrelin as a new therapeutic agent against pulmonary fibrosis by antagonizing the TGF-β1 signaling pathway.

High-efficiency removal of chloramphenicol (CAP) drug from waste water still faces a large challenge up to date. Herein, we report the first metal-organic framework-based adsorbent (PCN-222) for CAP and effective removal was achieved. PCN-222 exhibits a large adsorption capacity of 370 mg g−1, superior to some other MOFs and various reported adsorbents; and more importantly, the adsorption equilibrium can be quickly obtained at only 58 s. Besides, ∼99.0% of CAP can be removed from water in the low concentrations (including the concentrations found in real water). Further investigation indicates that H-bond interaction, electrostatic interaction and the special pore structure of PCN-222 all play important effects on the high-efficiency removal of CAP. Therefore, our work may provide a novel perspective for removing CAP or other antibiotic drugs from contaminated water.

Idiopathic pulmonary fibrosis (IPF) is a progressive interstitial lung disease with increasing occurrence, high death rates and unfavorable treatment regimens. In the current study, we identified the expression of microRNA-9 (miR-9) and anoctamin-1 (ANO1) in IPF mouse models induced by bleomycin, and their effects on inflammation and fibroblast proliferation through the transforming growth factor-β (TGF-β)-Smad3 pathway. To verify the targeting relationship between miR-9 and ANO1, we used bioinformatics prediction and conducted a dual-luciferase reporter gene assay. The underlying regulatory mechanisms of miR-9 and the target gene ANO1 were investigated mainly with the treatment of miR-9 mimic, miR-9 inhibitor, or siRNA against ANO1 in fibroblasts isolated from IPF mice. Enzyme-linked immunosorbent assay was performed to investigate the effect of miR-9 or ANO1 on inflammatory factors. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay and flow cytometry were used to detect fibroblast proliferation and apoptosis. Reverse transcription quantitative polymerase chain reaction and western blot analysis were applied to measure the expression of the TGF-β-Smad3 pathway-related genes. The determination of luciferase activity suggested that miR-9 targets ANO1. Upregulation of miR-9 or silencing of ANO1 intensified inflammation in IPF, promoted proliferation and inhibited apoptotic ability of lung fibroblasts. MiR-9 negatively modulated ANO1, and thus activated the TGF-β-Smad3 pathway. These findings suggest that miR-9 can indirectly activate the TGF-β-Smad3 pathway by inhibiting the expression of ANO1, thereby aggravating inflammation, promotes proliferation and suppressing apoptosis of lung fibroblasts in mice models of IPF.

The present study aimed to investigate the effect of various concentrations of etoposide (VP-16) on the E3 ubiquitin-protein ligase Mdm2 (Mdm2)-retinoblastoma (Rb) signaling pathway in the cellular senescence of A549 lung adenocarcinoma cells. A549 cells were randomly divided into the following four groups: Control group (no treatment), group 1 (1 µmol/l VP-16), group 2 (5 µmol/l VP-16) and group 3 (25 µmol/l VP-16). Each group was cultured for 48 h after treatment prior to observation of the alterations to cellular morphology. The cell cycle distribution of each group was also detected by flow cytometry. In addition, the activity of cellular senescence-associated β-galactosidase, and the expression of Mdm2 and phosphorylated (p-) Rb protein, was measured. The percentage of senescent cells was significantly higher following VP-16 treatment compared with the control group. The percentage of G1 phase cells, and p-Rb protein and Mdm2 protein expression were also significantly different following VP-16 treatment compared with the control group. VP-16 increased the activity of β-galactosidase in the A459 cells. VP-16 also decreased the expression level of Mdm2 and p-Rb protein and inhibited cell cycle progression in G1. These results indicate that VP-16 induces the cellular senescence of A549 cells via the Mdm2-Rb signaling pathway. However, further investigations are required to validate the mechanisms underlying these effects of VP-16.

A highly crystalline covalent organic frameworks (COFs) formed by condensation reaction between 1, 3, 5-tris (4-aminophenyl) benzene and 4, 4′-biphenyldicarboxaldehyde is utilized as a sensing platform for water in organic solvent over a broad concentration range. The resulting COFs exhibits brilliant fluorescence in various organic solvents such as methanol, DMF, acetonitrile and ethanol, moreover its fluorescence intensity has a significant and rapid response to the content of water in organic solvent over a broad concentration range. The broadest sensing range is achieved over 7%–70% (v/v) for water in DMF, and the lowest limit of detection is 0.042% (v/v) for water in methanol among the investigated organic solvents. The superior properties of the sensing platform expand the application ranges of COFs and endow the resulting COFs with a great prospect in practical applications for highly efficient detecting water in organic solvent.

Introduction Lung cancer is the malignant tumor with the fastest increase in morbidity and mortality and the greatest threat to human health and life. Long non-coding RNA (lncRNA) is emerging as an important regulator in many cancers. Recently, it was found that lncRNA prostate cancer associated transcript 1 (PCAT-1) was up-regulated in lung cancer, playing oncogenic roles. However, the underlying regulatory mechanism of PCAT-1 remains unknown. Material and methods The expression levels of PCAT-1 and miR-324-5p were analyzed by real-time PCR, and RAP1A expression was determined by western blotting. RNA pull-down, luciferase and western blotting assays were used to examine the target relationship between PCAT-1 and miR-324-5p or that between miR-324-5p and RAP1A. The functional effects of PCAT-1 and miR-324-5p were examined using cell viability and cell apoptosis assays. Results PCAT-1 overexpression remarkably promoted cell proliferation and suppressed cell apoptosis. Mechanistic investigations demonstrated that PCAT-1 can interact with miR-324-5p and repress its expression, thereby increasing the expression of its target RAP1A. Additionally, rescue experiments revealed that PCAT-1 served as an oncogene partly through sponging miR-324-5p and upregulating RAP1A in lung cancer cells. Conclusions Our findings demonstrate that on account of the dual function of pro-proliferation and anti-apoptosis, PCAT-1/miR-324-5p/RAP1A may be novel candidates for application in the diagnosis, prognosis and therapy of lung cancer.

The finite dihedral group generated by one rotation and one flip is the simplest case of the non-abelian group. Cayley graphs are diagrammatic counterparts of groups. In this paper, much attention is given to the Cayley graph of the dihedral group. Considering the characteristics of the elements in the dihedral group, we conduct the model of discrete-time quantum walk on the Cayley graph of the dihedral group by special coding mode. This construction makes Fourier transformation can be used to carry out spectral analysis of the dihedral quantum walk, i.e. the non-abelian case. Furthermore, the relation between quantum walk without memory on the Cayley graph of the dihedral group and quantum walk with memory on a cycle is discussed, so that we can explore the potential of quantum walks without and with memory. Here, the numerical simulation is carried out to verify the theoretical analysis results and other properties of the proposed model are further studied., 21 pages, 6 figures