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A novel gold(i)/Brønsted acid relay catalysis enabling azofuran activation to induce annulative rearrangement from 3-yne-1,2-diols is reported, producing a series of furan-2-yl-substituted pyrrol-2-ones with good yields.

In this paper, A new gold self-relay catalysis enabling intramolecular annulation and intermolecular Michael addition of 3-yne-1,2-diols with aurone-derived azadienes (or para-quinone methides) is reported, efficiently furnishing a range of unsymmetrical furanized triarylmethanes with substituent diversity in good yields. The overall process was governed by the π- and σ-Lewis acid capability of gold complexes, providing a catalytic strategy for constructing triarylmethane skeletons.

Background To evaluate the activity of hydrogen in endometrial cancer and elucidate its underlying molecular mechanisms. Methods Ishikawa, HEC1A and AN3CA cells were incubated in DMEM medium with or without hydrogen. RNA sequencing was used to explore the association of hydrogen treatment with signaling pathways and functional genes in endometrial cancer cells. The apoptotic rates of the three endometrial cancer cells were evaluated by fluorescein isothiocyanate (FITC) Annexin V and Annexin V-allophycocyanin (APC)/propidium iodide double staining. Results RNA sequencing analysis revealed that hydrogen induced TNF/NF-κB and apoptosis pathways in endometrial cancer cells. The gene sets between hydrogen treatment groups and non-treated groups were mapped in accordance with Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway and Gene Ontology (GO) terms. Hydrogen treatment significantly increased the apoptotic rates of endometrial cancer cells. Conclusions Taken together, our data indicate that hydrogen can serve as a therapeutic target for endometrial cancer via TNF/NF-κB pathway and apoptosis induction.

A sustainable and efficient visible-light-induced Ir(III)-catalyzed annulation of 1,7-diynes with ICF2CO2Et is reported under mild neutral-redox conditions, furnishing a wide range of difluoromethyl-containing (1E,2E)-tetrahydronaphthalen-1-ols bearing two exocyclic double carbon–carbon bonds as major stereoisomers in good yields with high stereoselectivity. Notably, the high stereoselectivity could be observed in most cases. The photocyclization protocol has attractive characteristics of complete atom economy, good compatibility with different types of substituents, and the efficient control of stereochemistry.

Tikhonov regularization (TR) method has played a very important role in the gravity data and magnetic data process. In this paper, the Tikhonov regularization method with respect to the inversion of gravity data is discussed. and the extrapolated TR method (EXTR) is introduced to improve the fitting error. Furthermore, the effect of the parameters in the EXTR method on the fitting error, number of iterations, and inversion results are discussed in details. The computation results using a synthetic model with the same and different densities indicated that. compared with the TR method, the EXTR method not only achieves the a priori fitting error level set by the interpreter but also increases the fitting precision, although it increases the computation time and number of iterations. And the EXTR inversion results are more compact than the TR inversion results, which are more divergent. The range of the inversion data is closer to the default range of the model parameters, and the model features and default model density distribution agree well.

A series of pyrano-fused pyrazolo[3,4-b]pyridine derivatives with an aryl group presenting the 2-position of the pyridine nucleus have been synthesized by microwave-assisted three-component reactions of aldehydes, tetrahydropyran-4-one, and 3-methyl-1-phenyl-1H-pyrazol-5-amine in HOAc. This method is very efficient because of short reaction times and easy work-up, and it provides an efficient and promising synthetic strategy for the construction of the tricyclic pyrano-fused pyrazolo[3,4-b]pyridine skeleton.

A novel and efficient access to 2-(argio(3-methyl-5-oxo-1-phenyl-4,5-dihydro-1H-pyrazol-4-yl)methyl)-3-hydroxynaphthalene-1,4-dione derivatives from readily available substrates in neat water is described with aid of microwave irradiation. The results of our study provide a green, simple and practical one-pot approach to the synthesis of 3-hydroxynaphthalene-1,4-dione analogs in excellent yields without further purification.

A series of new functionalized thiopyrano-, pyrano[4,3-d]pyrimidine derivatives with benzyl group residing in 8-position of fused pyrimidine nucleus were synthesized through multicomponent reactions of aromatic aldehydes, tetrahydrothiopyran-4-one(tetrahydropyran-4-one), and aryl amidines using t-BuOK as a base under microwave heating. The procedure is facile, avoiding time-consuming and costly syntheses, tedious work-up, and purifications of precursors as well as protection/deprotection of functional groups. This method is very efficient due to short reaction times and easy work up and provides a four-component strategy for the construction of the thiopyrano-, and pyrano[4,3-d] pyrimidine skeletons.

A series of new functionalized pyrazolopyridine derivatives with different substituted patterns were synthesized via microwave-assisted multi-component divergent reactions of aldehydes, 5-aminopyrazoles, and cycloketones by controlling the reaction condition. The procedures are facile, avoiding time-consuming and costly syntheses, tedious work-up, and purifications of precursors as well as protection/deprotection of functional groups. This chemistry provides an efficient and promising synthetic strategy to construction of the pyrazolopyridine skeleton.

Entrapped and pooled dense non-aqueous phase liquid (DNAPL) often persists in aquifers and serves as a long-term source of groundwater contamination. Despite vigorous research efforts over the last two decades, all current DNAPL pool remediation strategies suffer from a combination of inefficiency, enhanced risk of contaminant spreading due to uncontrolled mobilization, and or high treatment costs. In the present contribution, we report a novel strategy that makes the density of the representative DNAPL of trichloroethene (TCE) reduction utilizing colloidal liquid aphrons (CLAs) in the remediation process. The effects of the electrolyte (AlCl3) concentrations, the volume fraction of the dispersed oil phase (n-octane) and temperature on the demulsification behavior of CLA dispersion were discussed. Steady-state flow and dynamic viscoelasticity were measured by using a controlled stress rheometer HAAKE RS 6000 with cone-plate geometry in an attempt to reveal the rheological properties of CLAs. A series of batch experiments was conducted to evaluate the recovery efficiency of DNAPL from sand pack under different volumes, flow rates of CLAs and surfactant (Tergitol 15-S-9) flushing solutions. Experimental results suggest that CLAs can be destabilized by a low concentration of Al3+ in the continuous phase. The flow behavior of CLAs presents the typical non-Newtonian liquids with strong shear thinning properties and it could be well described by the Hershel–Bulkley model. Above the phase volume ratio (PVR = Vorg/Vaq) of 8, the systems display viscoelastic behavior. Relative to water, the density reversal of TCE occurs at an electrolyte concentration of 0.05 M, which effectively prevents TCE downward migration during surfactant flushing. As much as 94% of the TCE entrapped in the sand column is removed under the conditions of amounts of 1 PV (pore volume) for CLAs, 4 PV and 1.5 mL/min for Tergitol solution. This approach holds great promise for manipulating DNAPL densities prior to or during remediation processes.

A series of new functionalized macrocyclane-fused pyrazolo[3,4-b]pyridine derivatives with an aryl group at the 2-position of the pyridine nucleus have been synthesized by microwave-assisted three-component reactions of aldehydes, aminopyrazole and cycloketones in HOAc using 1.0 equiv. of TFA as a promoter. The procedure is facile, avoiding time-consuming and costly syntheses, tedious work-ups and purifications of precursors as well as protection/deprotection of functional groups. This method is very efficient due to short reaction times and easy work-up and provides an efficient and promising synthetic strategy for the construction of the macrocyclane-fused pyrazolo[3,4-b]pyridine skeleton.

When nanofibers could be made last century, its filtration potential was expected in a lot of professional fields, such as building industry, medical industry and Environmental protection industry. In the present study, in order to prove and explain its performances, nanofibrous membrane with given thickness was electrospun with 8% PVA solution on conventional cotton scaffold. Then by means of special air filtration test system, the filtration performances between PVA nanofibrous membrane and conventional fibrous filters were confirmed and compared. Besides, the filtration efficiencies of particles distribution 0.3-5um were attained, and at the same time, another important parameter, pressure-drops, could be observed, too. Through data analysis, the differences of filtration performances were verified. Despite the fact that nanofibrous membrane had higher pressure-drops, its filtration efficiency could reach startlingly 99% for some given particles. In succession, SEM was used to observe the particles distribution in filter, and the different filtration mechanisms were analyzed and discussed with SEMS images. Furthermore, we found that the direct inception and the inertial impact improved nanofiber filtration efficiency, while too small diameter of nanofiber induced higher pressure-drops. In general, nanofibers have huge value in air filtration application.

The traditional open pit mine slope deformation monitoring system can not use the monitoring information coming from many monitoring points at the same time, can only using the monitoring data coming from a key monitoring point, and that is to say it can only handle one-dimensional time series. Given this shortage in the monitoring, the multi-sensor information fusion in the state estimation techniques would be introduced to the slope deformation monitoring system, and by the dynamic characteristics of deformation slope, the open pit slope would be regarded as a dynamic goal, the condition monitoring of which would be regarded as a dynamic target tracking. Distributed Information fusion technology with feedback was used to process the monitoring data and on this basis Klman filtering algorithms was introduced, and the simulation examples was used to prove its effectivenes.

A Web-based knowledge database and computing platform for nonlinear differential equations is presented, which could provide computing and graphing based on symbolic computing system Maple and some of its built-in packages. Users can not only calculate specific types of analytical solutions of nonlinear differential systems by calling the packages, but also carry out any symbolic computations associated with equations and other kinds of simple computations in an interactive mode with visual output. The knowledge database of differential equations has all functions of the general database. Furthermore, each equation has a web page to show its properties and research results. In addition, each mathematica formula is stored in its infix form in the knowledge database and can be displayed visually.

Background Mesenchymal stromal cells (MSCs) are proven to have immunosuppressive functions via various mechanisms. These mechanisms were demonstrated by administering bone marrow derived human MSCs (hMSCs) to graft versus host disease (GVHD) murine models. Methods BALB/c host mice were irradiated prior to receiving C57BL/6 donor T cell depleted bone marrow (TCDBM) cells (negative control) and donor CD4+ T lymphocyte with (treatment group) or without hMSCs (positive control). The presence of hMSCs in target tissues and lymphoid organs was documented by using in vivo imaging and measuring the expression of EphB2 and ephrin-B2 by RTqPCR. Survival rate and GVHD score were also monitored. Tissue sections were obtained for histopathologic analysis. Flow cytometry was used to document donor T cell alloreactivity and expression of CCR5, CXCR3 and CCR7. ELISA was utilized to determine levels of proinflammatory cytokines, RANTES (CCL5) and phosphorylated STAT 5A/B. RTqPCR was performed to quantify expression of CCL3 and CXCL9. Western blotting was performed to qualitatively measure iNOS expression. Results Survival rate and GVHD score improved with hMSC treatment. Pathologic changes of GVHD were abrogated. Documentation of suppression of RANTES, CCL3, CXCL9, CCR5 and CXCR3 with simultaneous decrease of donor T cell alloreactivity was demonstrated 6 days after transplantation, along with reduction of levels of inflammatory cytokines, suppression of STAT 5A/B phosphorylation, increased expression of CCR7 and increased production of nitrous oxide by hMSCs. Documentation of homing of hMSCs to lymphoid organs and target tissues was also performed. Conclusions These mechanisms contribute to the current understanding of MSC mechanisms of immunosuppression and forms a comprehensive picture of how they exert immunosuppression in an in vivo model of immune dysregulation. Electronic supplementary material The online version of this article (doi:10.1186/s40164-015-0007-0) contains supplementary material, which is available to authorized users.

A series of pyrano-fused pyrazolo[3,4-b]pyridine derivatives with an aryl group presenting the 2-position of the pyridine nucleus have been synthesized by microwave-assisted three-component reactions of aldehydes, tetrahydropyran-4-one, and 3-methyl-1-phenyl-1H-pyrazol-5-amine in HOAc. This method is very efficient because of short reaction times and easy work-up, and it provides an efficient and promising synthetic strategy for the construction of the tricyclic pyrano-fused pyrazolo[3,4-b]pyridine skeleton.

The shortage of effective antibiotics against multidrug-resistant Acinetobacter baumannii (MDR-Ab) has posed great threat to the public health. But the advent of tigecycline gives us new hope. The goal of our research was to assess the clinical efficacy of tigecycline at different doses by using a pharmacokinetic/pharmacodynamic (PK/PD) model which can incorporate pharmacokinetic data of tigecycline from patients with pneumonia and MICs of MDR-Ab from a tertiary hospital. A 10000-patient Monte-Carlo Simulation based on the PK/PD model was conducted to calculate the probability of target attainment (PTA) and the cumulative fraction of response (CFR) of tigecycline. 97% isolates displayed susceptibility and 3% were tigecycline-intermediate strains and the values of MIC ranged from 0.125 to 4 μ g/ml. A CFR of 61.62% was predicted for tigecycline at current dosage (50 mg q12h). When the dosage was increased, the predicted CFRs for 75 mg q12h, 100 mg q12h, 125 mg q12h, 150 mg q12h were 81.00%, 89.86%, and 94.57%, 96.77%, respectively. Despite presented higher susceptibility, the CFR obtained was not optimal at current dosage. A higher CFR indicating a better clinical efficacy can be gained by the increased dosage.

To investigate contamination levels of polychlorinated dibenzo-p-dioxins and dibenzofurans (PCDD/Fs) and dioxin-like polychlorinated biphenyls (dl-PCBs) in human breast milk from Beijing residents, and evaluate the human body burden of PCDD/Fs and dl-PCBs of general population.A total of 110 human milk samples were collected from 11 regions in Beijing in 2007. After 11 pooled samples were made, concentrations of PCDD/Fs and dl-PCBs in breast milk pooled samples were measured by a high resolution gas chromatography - high resolution mass spectrometry (HRCG-HRMS) with isotope dilution.For congeners of PCDD/Fs and dl-PCBs in human breast milk from Beijing, the highest content of congeners was octachlorodibenzo-p-dioxin (OCDD), polychlorinated biphenyl (PCB)-118, and PCB-105 with the median of 20.6 pg/g fat, 4.07 ng/g fat and 1.63 ng/g fat, respectively. The concentration median of total dioxins in 11 pooled human milk samples from Beijing was 7.4 pg TEQ/g fat. The highest was 13.5 pg TEQ/g fat from Tongzhou, and the lowest was 4.3 pg TEQ/g fat from Pinggu.The contamination level of PCDD/Fs and dl-PCBs in human milk from Beijing is relatively low. However, with the rapid industrialization in China, the human body burden of PCDD/Fs and dl-PCBs will be likely to rise. Thus, further studies should be conducted to continuously monitor the trend of contamination level.

A series of new functionalized pyrazolopyridine derivatives with different substituted patterns were synthesized via microwave-assisted multi-component divergent reactions of aldehydes, 5-aminopyrazoles, and cycloketones by controlling the reaction condition. The procedures are facile, avoiding time-consuming and costly syntheses, tedious work-up, and purifications of precursors as well as protection/deprotection of functional groups. This chemistry provides an efficient and promising synthetic strategy to construction of the pyrazolopyridine skeleton.

A novel pseudo four-component reaction of 4-pyranones or thiones with aromatic aldehydes and arylamidines is established to provide the anellated pyrimidines regioselectively.

A series of new functionalized macrocyclane-fused pyrazolo[3,4-b]pyridine derivatives with an aryl group at the 2-position of the pyridine nucleus have been synthesized by microwave-assisted three-component reactions of aldehydes, aminopyrazole and cycloketones in HOAc using 1.0 equiv. of TFA as a promoter. The procedure is facile, avoiding time-consuming and costly syntheses, tedious work-ups and purifications of precursors as well as protection/deprotection of functional groups. This method is very efficient due to short reaction times and easy work-up and provides an efficient and promising synthetic strategy for the construction of the macrocyclane-fused pyrazolo[3,4-b]pyridine skeleton.

A new one-pot two-step tandem synthesis of highly functionalized benzo[a]pyrano[2,3-c]phenazine derivatives via microwave-assisted multicomponent reactions of 2-hydroxynaphthalene-1,4-dione, diamines, aldehydes, and malononitrile is reported. The procedures are facile, avoiding time-consuming and costly syntheses, tedious workup, and purifications of precursors, as well as protection/deprotection of functional groups. The method is expected to find application in the combinatorial synthesis of biologically active compounds, since phenazine and chromene motifs have a broad spectrum of biological activities.

This article reports the applicability of online gel permeation chromatography (GPC)-GC/MS for the determination of seven predominant polybrominated diphenyl ethers (PBDEs) in eggs to effectively eliminate matrix interference. Selective pressurized liquid extraction using acidic alumina as a fat retainer was used for cleanup of the PBDEs in eggs. It was selected because of its advantages: simpler operation, minimum time spent on sample handing to get fat-free extracts, and low volume of solvent consumption. After concentration, the extract was directly injected for online GC/MS operated in the negative ion chemical ionization mode with a 15 m capillary column. Recoveries of spiked samples were between 75.1 and 102.0%, with RSDs (n=3) ranging from 3.69-11.47% when spiked at levels of 2 and 20 ng/g, dry mass. The LOD varied from 0.25-34 ng/g, dry mass. The proposed method was proven to be rapid, efficient, and reliable for the trace determination of PBDEs in eggs.

The goal of this study was to compare the ability of donor naive and alloantigen-primed effector memory T cells to induce graft-vs-host disease after bone marrow transplantation in MHC-mismatched irradiated host mice. Purified CD4+ naive (CD62LhighCD44low) T cells and CD4+ effector memory (CD62LlowCD44high) T cells obtained from unprimed donors and donors primed to host alloantigens, respectively, were injected into host mice, and the rapidity, severity, and pattern of tissue injury of graft-vs-host disease was assessed. Unexpectedly, the naive T cells induced a more acute and severe colitis than the primed memory cells. Whereas the naive T cells expressing CD62L and CCR7 lymph node homing receptors vigorously expanded in mesenteric lymph nodes and colon by day 6 after transplantation, the primed memory T cells without these receptors had 20- to 100-fold lower accumulation at this early time point. These differences were reflected in the significantly more rapid decline in survival and weight loss induced by naive T cells. The primed memory T cells had a greater capacity to induce chronic colitis and liver injury and secrete IL-2 and IFN-γ in response to alloantigenic stimulation compared with memory T cells from unprimed donors. Nevertheless, the expected increase in potency as compared with naive T cells was not observed due to differences in the pattern and kinetics of tissue injury.

To evaluate the clinical effects of Forsus appliance in treatment of patients with mandibular retrusion after the growth spurts.15 cases of Class II malocclusion with small lower jaw were treated with Forsus appliance. Cephalogram pre-and post-treatment was taken,the width of dental arch was measured, and questionnaire were collected from the patients. SPSS10.0 software package was used for paired t test.SNB increased 1.42 degrees, ANB reduced 1.65 degrees, and Forsus appliance brought about 2.12 degrees reduction of the facial soft tissue profile convexity. The width of dental arch was extended. Overbite reduced and overjet went down 4.98 mm.Forsus appliance can improve sagittal discrepancy and soft tissue profile convexity of patients with Class II malocclusion.

Conditioning with total lymphoid irradiation plus antithymocyte serum protects mice against acute graft-versus-host disease (GVHD) after hematopoietic-cell transplantation. We tested this strategy in humans.Thirty-seven patients with lymphoid malignant diseases or acute leukemia underwent an experimental conditioning regimen with 10 doses of total lymphoid irradiation (80 cGy each) plus antithymocyte globulin, followed by an infusion of HLA-matched peripheral-blood mononuclear cells from related or unrelated donors who received granulocyte colony-stimulating factor.Of the 37 transplant recipients, only 2 had acute GVHD after hematopoietic-cell transplantation. Potent antitumor effects in patients with lymphoid malignant diseases were shown by the change from partial to complete remission. In the transplant recipients who underwent conditioning with total lymphoid irradiation and antithymocyte globulin, the fraction of donor CD4+ T cells that produced interleukin-4 after in vitro stimulation increased by a factor of five, and the proliferative response to alloantigens in vitro was reduced, as compared with normal control subjects and control subjects who underwent conditioning with a single dose of total-body irradiation (200 cGy).A regimen of total lymphoid irradiation plus antithymocyte globulin decreases the incidence of acute GVHD and allows graft antitumor activity in patients with lymphoid malignant diseases or acute leukemia treated with hematopoietic-cell transplantation.

The homing receptors L-selectin and α4β7 integrin facilitate entry of T cells into the gut-associated organized lymphoid tissues such as the mesenteric lymph nodes and Peyer patches. We studied the impact of inactivation of genes encoding these receptors on the ability of purified donor CD4+ T cells to induce acute lethal graft-versus-host disease (GVHD) associated with severe colitis in irradiated major histocompatibility complex (MHC)–mismatched mice. Whereas lack of expression of a single receptor had no significant impact on the severity of colitis and GVHD, the lack of expression of both receptors markedly ameliorated colitis and early deaths observed with wild-type (WT) T cells. The changes in colitis and GVHD were reflected in a marked reduction in the early accumulation of donor T cells in the mesenteric lymph nodes and subsequently in the colon. The purified WT donor CD4+ T cells did not accumulate early in the Peyer patches and failed to induce acute injury to the small intestine. In conclusion, the combination of CD62L and β7 integrin is required to induce acute colitis and facilitate entry of CD4+ donor T cells in the mesenteric nodes associated with lethal GVHD in allogeneic hosts.

In this paper, the homotopy analysis method is employed to decompose the classical boundary-value problem of nonlinear composite media into an infinite number of linear partial differential equations, solving each linear partial differential equation by separating variables together with the method of undetermined coefficients. Although the calculation is rather complicated, the solutions obtained in this paper have much higher precision than those known ones. We also investigate the effective conductivity of nonlinear composite media, and obtain an approximate expression for it.