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This study examined the application of slim-hole nuclear magnetic resonance (NMR) tools to estimate hydraulic conductivity (K

This article is to explore the antidepressant mechanism of Shugan Lipi recipe in regulating tryptophan metabolism,and to find out their common pharmacodynamic substances. UPLC-Q-TOF-MS technology was used to establish fingerprints of Shugan Lipi recipe,and 124 components were identified. The depressed mouse model was replicated by triple-one multiple stress method. Chaihu Shugan Powder,Sini Powder and Xiaoyao Powder were administered in groups to observe the changes in body weight and behavior of the mice. The results showed that compared with the model group,the body weight,sucrose preference percentage and autonomous activity behavior of each administration group were improved. Among them,the effect of Chaihu Shugan Powder was better than that of Sini Powder and Xiaoyao Powder. LC-MS/MS method was used to determine the contents of 5-hydroxytryptamine( 5-HT),kynurenine( KYN) and tryptophan( TPP) in blood,liver,brain,colon and other tissues,as well as TDO enzyme activity in liver. Western blot and RT-PCR were used to detect the protein and gene expression of TDO enzyme,respectively. It was found that the three prescriptions increased the ratio of 5-HT/KYN in different degrees,decreased the ratio of KYN/TRP in liver,colon and brain,and decreased the expression level and activity of TDO enzyme in liver. The order of their ability to regulate tryptophan metabolism was Chaihu Shugan Powdergt;Sini Powdergt;Xiaoyao Powder. In addition,the correlation between the chromatographic peaks in the fingerprints of Shugan Lipi recipes and the pharmacodynamic indexes of tryptophan metabolism was analyzed by the grey relation analysis. The grey relation analysis found that the chemical components with the highest correlation with tryptophan metabolism were mainly from Paeoniae Radix Alba,Citri Reticulatae Pericarpium,Aurantii Fructus Immaturus and Aurantii Fructus. UPLC-Q-TOF-MS was used to analyze the migration components in the plasma of mice after administration of Shugan Lipi recipe,and to verify the common pharmacodynamic substances of Shugan Lipi recipe. The migration of these detected components in plasma was studied,and a total of 18 prototype components and 36 metabolites were identified. Therefore,it was believed that Chaihu Shugan Powder,Sini Powder and Xiaoyao Powder could play an antidepressant role by reducing the expression of TDO enzyme in the liver and regulating the metabolism of tryptophan.The components contained in Paeoniae Radix Alba,Citri Reticulatae Pericarpium,Aurantii Fructus Immaturus and Aurantii Fructus were the common pharmacodynamic substances of Shugan Lipi recipe,which played an important role in regulating tryptophan metabolism.

Pd-catalyzed direct C2-alkenylation of azole derivatives proceeds efficiently under mild conditions, and the reaction of substituted benzoxazoles, oxazole and benzothiazole occurred even at room temperature. The substrate scope of the reaction was turned out to include mono-, di- and trisubstituted alkenyl bromides. To validate the scalability of this method, 5-Methyl-2-(prop-1-en-2-yl)benzoxazole (3c) was prepared on one-gram scale at room temperature.

In the present investigation, we carried a phytochemical study of an ethanol-soluble extract from the root barks of Aspidistra typica Baill., a traditional food and herb medicine, leading to the isolation of four different kinds of compounds, including one benzene substituted coumarin, two organic phosphonic compounds, and one xanthone. The novel benzene substituted coumarin typicacoumarin A (1) was a new type of coumarin, and the two new organic phosphonic compounds, typicalphosphine A (2) and typicalphosphine B (3) were isolated for the first time, and their structures were elucidated by spectral techniques, viz.1D, 2D NMR spectra and HR-ESI-MS. The xanthone compound typicaxanthone A (4) was discovered from nature for the first time. The two new organic phosphonic chlorides (2, 3) showed stronger antibacterial activities, which were comparable to berberine hydrochloride. And typicaxanthone A (4) showed much stronger antibacterial activity against Escherichia coli ATCC-25922 bacterial strain, while typicacoumarin A (1) showed moderate antibacterial activities, weaker than berberine hydrochloride.

Objective: Percutaneous transluminal balloon angioplasty (PTA) is recommended as the first choice to treat stenosis of Brescia-Cimino arteriovenous fistulas (B-C AVFs). The ability to predict which B-C AVFs are at risk for recurrent stenosis post-PTA would allow closer monitoring of patients, and possibly result in surgical intervention rather than repeat PTA. The purpose of this study was to identify predictive factors of primary patency after PTA in B-C AVFs. Methods: Patients diagnosed with B-C AVF primary stenosis and treated by PTA between November 2013 and March 2018 were included in the study. Patient and stenotic lesion characteristics and PTA procedure factors were included in the analysis. The Kaplan–Meier method was used to analyze the primary patency rate. Cox proportional hazard regression analysis was used to identify factors predictive of decreased primary patency. Results: 74 patients (35 males, 39 females) with a mean age of 61.68 ± 11.44 years (range, 36–84 years) were included in the study. The mean B-C AVF age was 16.34 ± 12.93 months (range, 2–84 months), and the median primary patency time was 7.79 ± 0.48 months. Cox proportional hazard regression analysis revealed stenosis location at the inflow artery [hazard ratio (HR)=3.83, 95% confidence interval (CI): 1.46–10.09] or anastomosis (HR = 1.90, 95% CI: 1.09–3.32), dilation >2 times during PTA (HR = 2.30, 95% CI: 1.22–4.34), and residual stenosis >30% (HR = 2.42, 95% CI: 1.26–4.63) were significantly associated with decreased patency. Conclusion: In conclusion, the primary patency rate of PTA for B-C AVF dysfunction is reduced by dilation >2 times, residual stenosis >30%, and stenosis located at the inflow artery or anastomosis. These results may help in tailoring surveillance programs, multiple PTA, or a proximal re-anastomosis surgery in patients with AVF dysfunction. Advances in knowledge: A number of studies have been conducted to examine the predictors of primary patency after PTA, however, no definitive conclusions have been reached. Our study revealed that stenosis location at the inflow artery or anastomosis, dilation >2 times during PTA, and residual stenosis >30% were the predictors of primary patency after PTA, which may help in tailoring surveillance programs, multiple PTA, or a proximal re-anastomosis surgery in patients with arteriovenous fistulas dysfunction.

2-aryl-N-alkylbenzimidazole derivatives synthesized by CuI/PPh3 promoted direct coupling of N-alkylbenzimidazoles with aryl bromides. In vitro neurotoxicities of 20 compounds were evaluated, and the neuroprotective abilities of low-neurotoxic compounds (3b, 3g, 3h, 3i, 3j, 3k, 3o, 3q, 3s and 3t) were investigated against toxicity induced by 1-methyl-4-phenylpyridinium ion (MPP+) in SH-SY5Y neuronal cells. In silico studies revealed that compound 3g could have molecule docking with the following proteins: the bone morphogenetic protein receptor type 1B (BMPR1B), human cytochrome P450 1B1(CYP1B1), Metabotropic glutamate receptor 7 (GRM7), histone deacetylase 6 (HDAC6), 5-hydroxytryptamine receptor 5A (HTR5A), human topoisomerase II beta (TOP2B). A molecular docking simulation of model compound 3g and model protein CYP1B1 has been shown.

Based on previous studies about microflora regulation and immunity enhancement activities of polysaccharides from Codonopsis pilosula Nannf. var. modesta (Nannf.) L. T. Shen (CPP), there is little study on intestinal mucosal immunity, which is a possible medium for contacting microflora and immunity. In the present study, the BALB/c mice were divided into five groups (eight mice in each group), including a normal group (Con), a model control group (Model), and model groups that were administered CPP (50, 100, 200 mg/kg/d) orally each day for seven days after intraperitoneal injection of 60 mg/kg BW/d cyclophosphamide (CP) for three days. CPP recovered the spleen index and restored the levels of IFN-γ, IL-2, IL-10, as well as serum IgG. In addition, it elevated ileum secretory immunoglobulin A (sIgA), the number of Lactobacillus and acetic acid content in cecum. These results indicated that CPP plays an important role in the protection against immunosuppression, especially mucosa immune damage, and the inhibition of pathogenic bacteria colonization, which could be considered a potential natural source of immunoregulator.

The lead-free ceramics 0.92Na0.5Bi0.5TiO3-0.06BaTiO3-0.02K0.5Na0.5NbO3 and 0.92Na0.5Bi0.5TiO3-0.06BaTiO3-0.02K0.5Na0.5NbO3 with the addition of 0.2 wt% Co2O3 were prepared by using a solid state reaction method. The ceramics were sintered in O2 and N2 atmospheres, respectively. The rhombohedral-tetragonal morphotropic phase boundary exists in all samples, with the relative amount of tetragonal phase varying with the sintering atmospheres which does not affect grain size of the ceramics. In the dielectric constant-temperature curves for all samples, two dielectric anomalies appear. The phase transition temperatures and maximum values of dielectric constant are closely related to the sintering atmospheres. The mechanism was also discussed.

(1 − x )(0.93Na 0.5 Bi 0.5 TiO 3 –0.07BaTiO 3 )– x BiAlO 3 (BNBT- x BA, x = 0, 0.01, 0.02, 0.06) lead-free ceramics were synthesized via a conventional solid state reaction method. Crystallite structure, microstructure, dielectric and ferroelectric properties of the BNBT– x BA ceramics were studied in detail. X-ray diffraction results show that all ceramics exhibit typical diffraction peaks of ABO 3 perovskite structure. Scanning electron microscope images show that all samples have fine microstructures. Both Curie temperature and maximum dielectric constant vary with the change in the BiAlO 3 amounts. The values of hysteresis loop squareness were calculated to be 1.26, 0.81, 0.51 and 0.36 for the ceramics with x = 0, 0.01, 0.02 and 0.06, respectively, indicating a decreased switching behavior of polarization. The changes in dielectric and ferroelectric properties of the ceramics are also discussed.

An efficient room-temperature Pd-catalyzed Suzuki–Miyaura cross-coupling reaction of aryl-boronic acids with aryl chlorides is communicated here. The Pd(OAc)2/NiXantphos catalyst system enables the coupling reaction at room temperature in good to excellent yields (average yield >90%).

Zhi-xiang Yuan,1,* Lu Jia,2,* Lee Yong Lim,3 Ju-chun Lin,1 Gang Shu,1 Ling Zhao,1 Gang Ye,1 Xiao-xia Liang,1 Hongming Ji,2 Hua-lin Fu1 1Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan, 2Department of Neurosurgery, Shanxi Provincial People’ Hospital, Taiyuan, China; 3Pharmacy, Centre for Optimization of Medicines, School of Allied Health, The University of Western Australia, Crawley, Australia *These authors contributed equally to this work Abstract: Previously, 3,5-dipentadecyloxybenzamidine hydrochloride (TRX-20)-modified liposomes were reported to specifically target mesangial cells (MCs) in glomeruli. To further gain a better understanding of the characteristics and potential application for glomerular diseases of TRX-20-modified liposomes, we synthesized TRX-20 and prepared TRX-20-modified liposomes (TRX-LPs) with different molar ratios – 6% (6%-TRX-LP), 11% (11%-TRX-LP), and 14% (14%-TRX-LP) – of TRX-20 to total lipid in the present study. All TRX-LPs exhibited concentration-dependent toxicity against the MCs at a lipid concentration ranging from 0.01 to 1.0 mg/mL with IC50 values of 3.45, 1.13, and 0.55 mg/mL, respectively. Comparison of the cell viability of TRX-LPs indicated that high levels of TRX-20 caused severe cell mortality, with 11%-TRX-LP showing the higher cytoplasmic accumulation in the MCs. Triptolide (TP) as a model drug was first loaded into 11%-TRX-LP and the liposomes were further modified with PEG5000 (PEG-TRX-TP-LP) in an attempt to prolong their circulation in blood and enhance TP-mediated immune suppression. Due to specific binding to MCs, PEG-TRX-TP-LP undoubtedly showed better anti-inflammatory action in vitro, evidenced by the inhibition of release of nitric oxide (NO) and tumor necrosis factor-α from lipopolysaccharide-stimulated MCs, compared with free TP at the same dose. In vivo, the PEG-TRX-TP-LP effectively attenuated the symptoms of membranous nephropathic (MN) rats and improved biochemical markers including proteinuria, serum cholesterol, and albumin. Therefore, it can be concluded that the TRX-modified liposome is an effective platform to target the delivery of TP to glomeruli for the treatment of MN. Keywords: triptolide, pegylated liposomes, TRX-20, renal targeting, mesangial cells

(Na0.47Bi0.46Ba0.06K0.01)(Nb0.02Ti0.98-xZrx)O3 lead-free ceramics (BNBKT-xZr, x = 0, 0.01, 0.02, 0.04) were synthesized via conventional solid state reaction method. Crystallite structure of the ceramics was studied using X-ray diffraction. The rhombohedral phase and tetragonal phase coexist in the BNBKT-xZr ceramics. The doping of Zr4+ into BNBKT lattice increases the percentage of the tetragonal phase. The size and shape of grains in the ceramics were affected by the doping of Zr4+ ions. For all the unpoled ceramics, two dielectric anomalies are observed in the dielectric constant-temperature curves. The maximum values of dielectric constant and corresponding temperatures change with the variation of Zr4+ amount. The doping of Zr4+ ions causes a decrease in the ferroelectric properties.

In an attempt to obtain dense lead metaniobate-based ceramics with improved dielectric and piezoelectric properties, the (Pb1.06−xBax)(Nb0.94Ti0.06)2O6 (x = 0, 0.04, 0.08, 0.12) piezoelectric ceramics were prepared separately from the two kinds of calcined powders, i.e., the powders with the rhombohedral phase and orthorhombic phase. For obtaining the calcined powders with the different phases, two different calcination temperatures of 900 °C and 1250 °C were chosen. The calcined powders were characterized using X-ray diffraction, scanning electron microscope, laser particle size analyzer and differential scanning calorimetry. Effects of the phase structures of the calcined powders on crystallite structure, microstructure, dielectric and piezoelectric properties of the ceramics were studied in detail. The lattice parameters and grain size of the ceramics are related to the phase structures of the calcined powders. The doping of Ba2+ has an influence on the dielectric and piezoelectric properties of the ceramics. The ceramics with x = 0.08 fabricated from the calcined powders with the orthorhombic phase demonstrate the optimum dielectric and piezoelectric properties.

Based on the collected data to carry on the analysis, found that the CNC system in the CNC grinding machine fault rate, a large part of the station, the reliability growth of CNC system is studied in the paper, CNC system parameter selecting principles of reliability growth are particularly discussed. CNC system reliability ideal growth curve is settled to CNC system reliability, Thus increasing CNC system to improve the reliability of CNC grinder machine reliability is of great significance.

The regioselective demethylations of two C19-diterpenoid alkaloids, 2 and 3, have been achieved with HBr–HOAc, trimethylsilyl iodide, or BBr3. It was observed that HBr–HOAc is an optimal demethylating agent for these two C19-diterpenoid alkaloids because it could provide different O-demethylation products by using different reaction temperature and reaction time. Especially, 1-O-methyl group in 2 and 3, one of the most difficult ones to be demethylated, could be removed by the treatment with HBr–HOAc at an elevated temperature and a prolonged reaction time.

The ColR – ColS two-component signal transduction system was originally characterized as a regulatory system involved in the capacity of root-colonizing biocontrol bacterium Pseudomonas fluorescens to colonize plant roots. There are three pairs of putative colR – colS two-component regulatory systems annotated in the phytopathogen Xanthomonas campestris pathovar campestris . Mutational studies revealed that one of them, named colR XC1049 and colS XC1050 , is a global regulatory system involved in various cellular processes, including virulence, hypersensitive response and stress tolerance. Growth rate determination showed that, although the colR XC1049 and colS XC1050 mutants are not auxotrophic, colR XC1049 and colS XC1050 are required for the pathogen to proliferate well in standard media and host plants. Assays of β-glucuronidase activities of plasmid-driven promoter- gusA reporters and/or semi-quantitative RT-PCR demonstrated that colR XC1049 and colS XC1050 positively regulate expression of hrpC and hrpE operons, and that expression of colR XC1049 and colS XC1050 is not controlled by key hrp regulators HrpG and HrpX.

RsmA is an RNA-binding protein functioning as a global post-transcriptional regulator of various cellular processes in bacteria and has been demonstrated to be an important virulence regulator in many animal bacterial pathogens. However, its function in other phytopathogenic bacteria is unclear, except for the Erwinia carotovora RsmA, which acts as a negative virulence regulator. In this work, we investigated the function of the rsmA-like gene, named rsmAXcc, of the phytopathogen Xanthomonas campestris pv. campestris. Deletion of rsmAXcc resulted in complete loss of virulence on the host plant Chinese radish, hypersensitive response on the nonhost plant pepper ECW-10R, and motility on the surface of an agar plate. The rsmAXcc mutant displayed a significant reduction in the production of extracellular amylase, endoglucanase, and polysaccharide, but a significant increase in intracellular glycogen accumulation and an enhanced bacterial aggregation and cell adhesion. Microarray hybridization and semiquantitative reverse-transcription polymerase chain reaction analysis showed that deletion of rsmAXcc led to significantly reduced expression of genes encoding the type III secretion system (T3SS), T3SS-effectors, and the bacterial aggregate dispersing enzyme endo-β-1,4-mannanase. These results suggest that rsmAXcc is involved in the control of various cellular processes, including pathogenesis of X. campestris pv. campestris.

It is well known that the type III secretion system (T3SS) and type III (T3) effectors are essential for the pathogenicity of most bacterial phytopathogens and that the expression of T3SS and T3 effectors is suppressed in rich media but induced in minimal media and plants. To facilitate in-depth studies on T3SS and T3 effectors, it is crucial to establish a medium for T3 effector expression and secretion. Xanthomonas campestris pv. campestris (Xcc) is a model bacterium for studying plant-pathogen interactions. To date no medium for Xcc T3 effector secretion has been defined. Here, we compared four minimal media (MME, MMX, XVM2, and XOM2) which are reported for T3 expression induction in Xanthomonas spp. and found that MME is most efficient for expression and secretion of Xcc T3 effectors. By optimization of carbon and nitrogen sources and pH value based on MME, we established XCM1 medium, which is about 3 times stronger than MME for Xcc T3 effectors secretion. We further optimized the concentration of phosphate, calcium, and magnesium in XCM1 and found that XCM1 with a lower concentration of magnesium (renamed as XCM2) is about 10 times as efficient as XCM1 (meanwhile, about 30 times stronger than MME). Thus, we established an inducing medium XCM2 which is preferred for T3 effector secretion in Xcc.

Eighteen schizandrin A derivatives, possessing an acyl group at 7-OH and/or halogen(s) at C-4 and C-11, were designed and synthesized for evaluation of their in vitro ability to inhibit multidrug resistance (MDR). They exhibit weak ability to restore the intracellular Rhodamine 123 in human hepatocarcinoma MDR cell lines Bel7402 and HCT8 relative to the reference drug verapamil.

To collect the researching documents of recent years about the pharmacodynamics research and modem clinic application of Huangqintang and its relative prescription, and to discuss the current general situation of the pharmacodynamics research and clinic application. Huangqintang has the pharmacodynamics effect such as resist bacteria and inflammation, adjust immune system, ease pain, protect the liver, lower the index of aminotransferase, anti-cancer and virus, lower the physical temperature, and calm down the emotion. The original and relative prescription can be commonly used in curing intestines disease such as diarrhea, acute enteritis and gastritis, ameba diarrhea, etc. It can also be used in internal medicine, gynecology, dermatology, etc.

Five new C18-diterpenoid alkaloids, anthriscifolcines A (1), B (2), C (3), D (4), and E (5), together with a known C19-diterpenoid alkaloid delcorine (6), were isolated from the whole herb of Delphinium anthriscifolium var. savatieri. The structures of these new alkaloids were established on the basis of spectral data (1D- and 2D-NMR, HR-ESI-MS).

A new conversional synthesis of the ABC ring system of taxoids from the C19-diterpenoid alkaloid lycoctonine was developed in 6 steps with 2% overall yield. The distinctive features of the conversion include pinacol rearrangement, enlargement of ring B, and opening of a four-membered ring.

Construction of a microarray based on the genome of Xanthomonas campestris pv.campestris (Xcc), and its use to analyse 18 other virulent Xcc strains, revealed insights into the genetic diversity and determinants of host specificity of Xcc strains., Background Xanthomonas campestris pathovar campestris (Xcc) is the causal agent of black rot disease of crucifers worldwide. The molecular genetic diversity and host specificity of Xcc are poorly understood. Results We constructed a microarray based on the complete genome sequence of Xcc strain 8004 and investigated the genetic diversity and host specificity of Xcc by array-based comparative genome hybridization analyses of 18 virulent strains. The results demonstrate that a genetic core comprising 3,405 of the 4,186 coding sequences (CDSs) spotted on the array are conserved and a flexible gene pool with 730 CDSs is absent/highly divergent (AHD). The results also revealed that 258 of the 304 proved/presumed pathogenicity genes are conserved and 46 are AHD. The conserved pathogenicity genes include mainly the genes involved in type I, II and III secretion systems, the quorum sensing system, extracellular enzymes and polysaccharide production, as well as many other proved pathogenicity genes, while the AHD CDSs contain the genes encoding type IV secretion system (T4SS) and type III-effectors. A Xcc T4SS-deletion mutant displayed the same virulence as wild type. Furthermore, three avirulence genes (avrXccC, avrXccE1 and avrBs1) were identified. avrXccC and avrXccE1 conferred avirulence on the hosts mustard cultivar Guangtou and Chinese cabbage cultivar Zhongbai-83, respectively, and avrBs1 conferred hypersensitive response on the nonhost pepper ECW10R. Conclusion About 80% of the Xcc CDSs, including 258 proved/presumed pathogenicity genes, is conserved in different strains. Xcc T4SS is not involved in pathogenicity. An efficient strategy to identify avr genes determining host specificity from the AHD genes was developed.