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Phytochemical investigations on the dry leaves of Illicium dunnianum have led to the isolation of 24 lignans. Illiciumlignans G–K (1–5) were five undescribed benzofuran lignans, illiciumlignan L (6) was one undescribed ditetrahydrofuran lignan, illiciumlignans M–O (7–9) were three new sesquilignans, and compounds 10, 12, 13, 15, and 18–21 were firstly isolated from the genus Illicium. Their structures were elucidated by detailed spectroscopic analyses (UV, IR, HR-ESI-MS, and NMR) and CD experiments. All isolates were evaluated by measuring their inhibitory effects on PGE2, and NO production in LPS-stimulated RAW 264.7 macrophages.

Objective To study the antipyretic and anti-inflammatory constituents from the active fraction of Reduning (RDN) Injection. Methods In this study, the active fraction of RDN Injection was screened by the LPS-induced mouse endotoxin shock model. The chemical constituents were isolated by chromatography on HP-20 macroporous adsorptive resins, silica gel, ODS columns and reverse phase MPLC and HPLC repeatedly, and their structures were elucidated based on spectroscopic analysis (HR-ESI-MS, NMR, ECD) and chemical methods. Meanwhile, we evaluated the anti-inflammatory activities of the isolates by measuring their inhibitory effects on TNF-α production in LPS stimulated RAW 264.7 macrophages. Results The 95% ethanol eluate of RDN Injection by the macroporous adsorption resin column was proved to be the antipyretic and anti-inflammatory active fraction of this injection. A novel iridoid, named jasminoide A (1), and a new guaiane sesquiterpenoid, named (1R,7R,8S,10R)-7,8,11-trihydroxy-4-guaien-3-one (2), were isolated from Reduning injection, and compound 2 can inhibit TNF-α production with IC50 values of 72.24 µmol/L. Conclusion In this study, two new terpenoids were isolated from Reduning Injection, and compound 2 showed inhibitory activity against LPS-activated TNF-α production in RAW 264.7 cells in vitro.

As recognized as the most economical and effective measure to increase carbonate oil and gas well production, matrix acidising is widely used. The main feature of acidising and the key influence factor of increasing production is what kind of acid etched wormholes can be formed. The actual etched wormholes grow in disorder and randomly, that's why it is extremely difficult to describe by classical mathematical methods. Due to the lack of a quantitative calculation model for the growth law of acid-etched wormholes, penetration depth, competition and distribution patterns among different etched wormholes, an effective method for acidising parameters optimization cannot be formed. The stimulated production of different wells vary greatly. In order to establish the corresponding quantitative calculation model for geometric size of acid etched wormholes, three-dimensional competitive distribution of different wormholes, and production prediction, also to achieve the quantitative optimization of treatment parameters for different wells and improve oil and gas production, firstly, we designed and completed indoor core etched experiments and CT scanning technology to obtain the true three-dimensional morphology of linear acid etched wormholes. Besides, the radial wormholes in 14 cubic feet of super large cores were proven to meet the requirement of fractal. The fractal dimensions of these two wormhole types were also obtained. Furthermore, a quantitative calculation model for the wormhole length expansion was established. Secondly, according to the mathematical model of extending competition among different acid etched wormholes, the fractal distribution law of the length of wormholes in the vertical direction is obtained. Combined with the fractal wormhole length calculation model, a method to solve the dual fractal model by calculating the maximum wormhole length is given. Finally, the classic acidised production rate calculation model was revised. The influence of the three-dimensional expansion length and distribution of wormholes on the skin factor was considered in detail. The sensitivity of key acidising parameters, such as acid strength and pumping rate, was also analyzed. The results show that both the linear wormholes obtained from conventional cores and the radial wormholes obtained from super-large cores can be described by fractal geometry. The fractal dimension corresponding to the optimal pumping rate is 1.46-1.63. Considering the dual-fractal distribution of acid-etched wormholes, the skin factor is larger than that of the conventional equalization model. This is mainly due to the fact that the equalization model only uses the maximum length of the wormholes. This also explains why wells or layers with negative skin factors can still increase production rate after uniform acidising. At the same time, for a specific layer, there is a better acid strength and pumping rate. With these parameters, the acid consumption and predicted production rate are better, which provides a theoretical basis for the quantitative optimization of acidising treatment parameters.

Jin-hong tablets (JHT), a well-known Traditional Chinese Patent Medicine (TCPM), has been effectively used for the treatment of chronic superficial gastritis (CSG) in clinic. The metabolic profile of TCPMs is the key part of discovering their bioactive components. In this study, a five-step strategy based on ultra-performance liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry (UPLC-Q/TOF-MS) and metabolynxTM software combined with mass defect filter (MDF) technique was developed to delineate the metabolic profile of JHT in vivo. As a result, a total of 163 JHT-related xenobiotics (38 prototypes and 125 metabolites) were identified or tentatively characterized in rat biological samples, and the phase I and II metabolism process mainly included demethylation, hydroxylation, sulfation and glucuronidation. In addition, after oral administration of JHT, a large amount of alkaloids-related ingredients were detected in rat plasma samples, indicating that alkaloids may play an important role in the treatment of CSG with JHT. This study is beneficial for understanding of JHT's in vivo metabolic profiles and characteristics, which helps to reveal its in vivo effective components and provides a solid basis for further studies on its functional mechanism.

Zanazour Oilfield has the typical characteristics of large perforation interval span, large number of perforation intervals, large differences in physical properties between different layers, and uneven fluid production profile. In order to achieve uniform acidification requirements, improve fluid production profile, and increase the use of low permeability layers, a multifunctional diverting acid fluid system suitable for the characteristics of the Zanazour oilfield was developed. The system has the characteristics of temporary blocking and diverting, selective acidification, and energy-assisted flowing back and so on. Based on the reservoir and fluid characteristics, lithology and physical properties of the oilfield, three acid liquid systems with good compatibility and temporary plugging, diverting, deep acidification, and energy-enhancing flowing back were developed, and their properties were tested with laboratory tests. At the same time, in order to give full play to the advantages of different functional acid liquid systems and achieve the purpose of synergistic enhancement, selective foamed acid systems and technologies, as well as emulsified self-diverting acid systems and technology have been formed. The pilot implementation of the field experiments, through high construction success rate and significant better production increasing effect than that of conventional liquids, indicated that the multifunctional diverting acid system and synergistic acidification technology have better adaptability in the oil field.

A cylindrical drift chamber (CDC) has been developed for the COMET Phase-I experiment. To search for the muon-to-electron conversion with a sensitivity of $3 \times 10^{-15}$, the CDC is required to have momentum resolution of 200 keV/$c$ for 100-MeV/$c$ electrons. In order to reduce the multiple scattering, we have selected a chamber gas mixture of 90% helium with 10% isobutane. Construction of the CDC was successfully conducted, and performance evaluation is being carried out. We have confirmed stable operation without a magnetic field thus far based on cosmic-ray tests. In this paper, the motivation, design, construction, and commissioning status of the CDC are presented.

Chronic superficial gastritis (CSG) is a common disease of the digestive system that possesses a serious pathogenesis. Jinhong tablet (JHT), a traditional Chinese medicine (TCM) prescription, exerts therapeutic effects against CSG. However, the molecular basis of its therapeutic effect has not been clarified. Herein, we employed UPLC-Q/TOF-MS-based chemical profile identification to determine the chemical components in JHT. Further, we applied network pharmacology to illustrate its molecular mechanisms. A total of 96 chemical constituents were identified in JHT, 31 of which were confirmed using reference standards. Based on the bioinformatics analysis performed using the symptom-guided pharmacological networks of “chi,” “blood,” “pain,” and “inflammation,” and a target screening based on the interaction probabilities between compounds and targets, MMP2, DRD2, and AKR1B1 were identified as key targets in the therapeutic effect exhibited by JHT against CSG. Moreover, according to the inhibitory activities presented in the literature and binding mode analysis, the structural types of alkaloids, flavonoids, organic acids, including chlorogenic acid (10), caffeic acid (13), (-)-corydalmine (33), (-)-isocorypalmine (36), isochlorogenic acid C (38), isochlorogenic acid A (41), quercetin-3-O-α-L-rhamnoside (42), isochlorogenic acid B (47), quercetin (63), and kaempferol (70) tended to show remarkable activities against CSG. Owing to the above findings, we systematically identified the chemical components of JHT and revealed its molecular mechanisms based on the symptoms associated with CSG.

Three unusual sesquiterpenoid dimers, nardochinoids A–C (1–3), were isolated from Nardostachys chinensis Batal. Compound 1 features a rare fused 3,8-dioxatricyclo[7.2.1.01,6]dodecane-11-one ring system, compound 2 is the first nitrogen-containing nornardosinane–aristolane sesquiterpene conjugate, and compound 3 represents the first example of the dimer of a nornardosinane and a nardosinane sesquiterpene. Their structures were characterized by NMR spectroscopic methods and X-ray single-crystal diffraction analysis. Compound 3 showed significant anti-inflammatory activities.

Four previously unreported sesquiterpenoid diasteromers, arteannoides U–X (1–4), together with one new norsesquiterpenoid 5 (arteannoide Y) and one undescribed rearranged cadinene sesquiterpenoid 6 (arteannoide Z) were obtained from the dried aerial parts of Artemisia annua (Qinghao). Notably, arteannoides U–X (1–4) are four stereoisomers that possess the same molecules and the same planar connectivity, but differ from each other in configuration at a certain stereocenter. Their accurate structures were unambiguously identified and distinguished by extensive spectroscopic analyses, NMR calculations with DP4+ analysis, electronic circular dichroism (ECD) calculations and X-ray diffraction analyses. Compounds 1, 3, and 4 showed inhibitory activities against the production of inflammatory cytokines (PGE2, NO, IL-6 and TNF-α) in lipopolysaccharide (LPS)-induced RAW 264.7 macrophages.

The reoxidation of molten steel by oxidising slag directly affects the molten steel cleanliness. There is a good relationship between molten steel cleanliness and the defect sources of cold rolled sheets. The results show that there is a direct relationship of the slag composition to steel cleanliness and the rate of surface defects on the final products. The thermodynamic calculations show that the activity of iron oxide decreases with the increase of w(CaO)/w(Al2O3) specifically when the content of T.Fe in slag remains at lower levels. In order to enhance the absorption ability of the slag to Al2O3 inclusions, w(CaO)/w(Al2O3) should be controlled in the range of 1.0–1.4 in the liquid region of slag when T.Fe content in RH final slag is less than 6 mass%. By reasonable control of T.Fe content and w(CaO)/w(Al2O3) in the slag, the defect content of sheets significantly declines.

Cryoprotective saccharides are widely accepted additives that reduce thawing loss, maintain texture, and retard protein denaturation in the frozen seafood. The present study aimed to investigate the roles of trehalose and alginate oligosaccharides on cryoprotection of frozen shrimp, primarily focusing on the interactions between myosin and saccharide molecules using a molecular dynamics (MD) simulation analysis. The results indicated that soaking in the trehalose and alginate oligosaccharides solutions markedly reduced thawing and cooking losses in frozen shrimp, with respective values decreasing to 6.02%, 8.14%, and 5.99%, 8.19% after 9weeks of storage, which were significantly lower than that of fresh water treatment (9.75% and 15.09%). Our assumption was that water replacement played a leading role in cryoprotection, as shown in previous experimental results and reports. Furthermore, homology modeling and MD simulations confirmed that trehalose and alginate oligosaccharides substituted the water molecules around the myosin surface by forming hydrogen bonds with polar residues of amino acids, thereby stabilizing the structures in the absence of water during frozen storage. These conditions affected the flexibility of particular amino acid residues, enhanced the residue cross correlations within the two chains of myosin, and also increased the total interaction energy between myosin and water/saccharide molecules, thereby leading to an increase in protein stability. Finally, by comparing the experimental results to that of MD simulation, significant positive correlation existed between saccharides and the stabilization of myosin in shrimp muscle. The findings of the present study may help better understand the cryoprotective mechanisms of saccharides in frozen shrimp, and the two saccharides may be potentially used as alternative additives in seafood to maintain better quality during frozen storage.

A series of [1,2,4]triazolo[4,3-b][1,2,4,5]tetrazine derivatives have been synthesized and their structures were confirmed by single-crystal X-ray diffraction. Compared to some reported structures of 1,6-dihydro-1,2,4,5-tetrazine, these compounds can't be considered as having homoaromaticity. Their antiproliferative activities were evaluated against MCF-7, Bewo and HL-60 cells in vitro. Two compounds were highly effective against MCF-7, Bewo and HL-60 cells with IC50 values in 0.63-13.12μM. Three-dimensional quantitative structure-activity relationship (3D-QSAR) studies of comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) were carried out on 51 [1,2,4]triazolo[4,3-b][1,2,4,5]tetrazine derivatives with antiproliferative activity against MCF-7 cell. Models with good predictive abilities were generated with the cross validated q(2) values for CoMFA and CoMSIA being 0.716 and 0.723, respectively. Conventional r(2) values were 0.985 and 0.976, respectively. The results provide the tool for guiding the design and synthesis of novel and more potent tetrazine derivatives.

With complex fractured-vuggy heterogeneous structures, water has to be injected to facilitate oil production. However, the effect of different water injection modes on oil recovery varies. The limitation of existing numerical simulation methods in representing fractured-vuggy carbonate reservoirs makes numerical simulation difficult to characterize the fluid flow in these reservoirs. In this paper, based on a geological example unit in the Tahe Oilfield, a three-dimensional physical model was designed and constructed to simulate fluid flow in a fractured-vuggy reservoir according to similarity criteria. The model was validated by simulating a bottom water drive reservoir, and then subsequent water injection modes were optimized. These were continuous (constant rate), intermittent, and pulsed injection of water. Experimental results reveal that due to the unbalanced formation pressure caused by pulsed water injection, the swept volume was expanded and consequently the highest oil recovery increment was achieved. Similar to continuous water injection, intermittent injection was influenced by factors including the connectivity of the fractured-vuggy reservoir, well depth, and the injection–production relationship, which led to a relative low oil recovery. This study may provide a constructive guide to field production and for the development of the commercial numerical models specialized for fractured-vuggy carbonate reservoirs.

Arteannoide A (1), an unusual cadinane dimer featuring a rare fused 6,8-dioxabicyclo[3.2.l]octan-7-one ring system, arteannoides B and C (2 and 3), two novel heterodimers incorporating a rearranged cadinene sesquiterpenoid and a phenylpropanoid, together with two new rearranged cadinene sesquiterpenoids 4 and 5, were isolated from Artemisia annua L. Their structures were determined by a combination of NMR spectroscopy, electronic circular dichroism calculations, and X-ray diffraction analyses. Compounds 2 and 3 showed inhibition of nitric oxide production in lipopolysaccharide-induced RAW 264.7 mouse macrophage cell lines with IC50 values of 4.5 and 2.9 μM, respectively.

A new dimeric secoiridoids derivative, named japonicaside E, together with six known compounds were isolated from the flower buds of Lonicera japonica. The structures of these compounds were elucidated by the analyses of mass spectrometry and NMR spectroscopy. All compounds were evaluated for anti-inflammatory activity in vitro.

Two new labdane diterpenoids, Leojaponin E (1) and F (2), together with three known compounds were isolated from the dried herb of Leonurus japonicus Houtt., Lamiaceae. Their structures were determined based on extensive spectroscopic analyses. The absolute configurations of 1 and 2 were elucidated on the basis of experimental and calculated electronic circular dichroism spectra. In addition, compounds 1 and 2 exerted inhibition of LPS-induced PGE2 production in a dose-dependent manner at concentrations ranging from 5 to 20 μM.

A reliable and sensitive liquid chromatography-ion trap-time of flight tandem mass spectrometric assay (LCMS-IT-TOF) coupled with accelerated solvent extraction (ASE) was developed to identify and quantify six typical heterocyclic aromatic amines (HCAs), including 2-amino-3-methylimidazo[4,5-f]quinoline (IQ), 2-amino-3,4-dimethylimidazo[4,5-f]quinoline (MeIQ), 2-amino-3,8-dimethylimidazo[4,5-f]quinoxaline (MeIQx), 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP), 2-amino-9H-pyrido[2,3-b]indole (AαC) and 2-amino-3-methyl-9H-pyrido[2,3-b]indole (MeAαC) in cooked meat products. The effects of various experimental factors on separation and detection were investigated, and the fragmentation patterns of six HCAs were discussed. The method has shown high reproducibility with intra-day and inter-day precision (RSD, %) less than 6.16% across three quality control levels for the six analytes. The assay was linear over the concentration range of 10 to 1000 μg L−1 for IQ, MeIQ and 5 to 500 μg L−1 for MeIQx, PhIP, AαC and MeAαC (r2 ≥ 0.996). The experimental results showed that the proposed method can be used successfully to identify and determine six typical HCAs at ultra-trace levels (μg kg−1) in cooked meat products.

To evaluate the protective effects of Reduning Injection (热毒宁注射液, RDN), a patent Chinese medicine, on lipopolysaccharide (LPS)-induced acute lung injury (ALI) in rats and its underlying mechanisms of action. Sixty male Sprague-Dawley rats were randomly divided into 6 groups, including normal control, model, dexamethasone (DEX, 5 mg/kg), RDN-H (720 mg/kg), RDN-M (360 mg/kg) and RDN-L (180 mg/kg) groups, with 10 rats in each group. Rats were challenged with intravenous injection of LPS 1 h after intraperitoneal treatment with RDN or DEX. At 6 h after LPS challenge, lung tissues and bronchoalveolar lavage fluid (BALF) were collected, and the number of inflammatory cells was determined. The right lungs were collected for histopathologic examination, measurement of gene and protein expressions, superoxide dismutase (SOD) and myeloperoxidase (MPO) activities. In vivo pretreatment of RDN (360, 720 mg/kg) significantly reduced the weight of wet to dry (W/D) ratio of lung, protein content in BALF, and led to remarkable attenuation of LPS-induced histopathological changes in the lungs. Meanwhile, RDN enormously decreased BALF total inflammatory cells, especially neutrophil and macrophage cell numbers. Moreover, RDN increased SOD activity, inhibited MPO activity, alleviated LPS-induced tumor neurosis factor-α (TNF-α) and inducible nitric oxide synthase (iNOS) expression in lung tissues. Furthermore, RDN (720 mg/kg) efficiently weakened nuclear factorkappa B (NF-κB) gene and protein expression. Anti-inflammatory effects of RDN was demonstrated to be preventing pulmonary neutrophil infiltration, lowering MPO activity, TNF-α and iNOS gene expression by inhibiting NF-κB activity in LPS-induced ALI.

Six new monoterpene glycosides, named 6'-O-nicotinoylalbiflorin (1), 4'-O-vanillylalbiflorin (2), paeonidanin L (3), paeoniflorigenin-1-O-β-d-xyloside (4), 6'-(2-hydroxypropanoyl)-paeoniflorin (5), oxylactiflorin (6), together with 16known ones (7-22) were isolated from the 70% ethanol extract of Paeoniae Radix. Their structures were elucidated based on spectroscopic analysis (1D and 2D NMR, HRESIMS, IR and UV), chemical evidences and comparison with literatures. The inhibitory effects of all the isolates were evaluated against lipopolysaccharide (LPS) stimulated PGE2 production in RAW 264.7 macrophages.

A series of xanthone analogues modified from vadimezan 6 with carboxyl substitution were synthesized as esters, amides, arylidene hydrazides, diacylhydrazides and acyl thiosemicarbazides, and their structures were confirmed by IR, 1H NMR, MS, HRMS or elemental analysis. The in vitro anticancer activities were evaluated by the MTT method. It was found that compounds 8f, 8g and 10e were effective against A549 with an IC50 at 10.8 μM, 9.4 μM and 11.5 μM respectively, and that 8e was effective against HL-60 with an IC50 at 4.6 μM. Compounds 8f–h showed a significant inhibitory effect on HUVEC growth and migration in vitro, among which 8h inhibited HUVEC growth with an IC50 at 6.4 μM and HUVEC migration by 67.6% and 89.7% at 2.5 μg mL−1 and 10 μg mL−1 respectively. More spectacularly, docking study indicated that compound 8h might target the ATP binding site of VEGFR2. In addition, compounds 8a, 8f–h exhibited moderate in vivo antitumor efficacy against the S180 xenograft in ICR mice by 22.4–29.6% tumor weight inhibition.

A series of novel 5-alkyl(aryl)-3-[(3-trifluoromethyl)anilino]-4,5-dihydro-1H-pyrazolo[4,3-d]pyrimidin-4-imines were designed and synthesized by the multistep reactions. 1 reacted with 3-(trifluoromethyl)aniline to obtain N,S-acetals 2 in the presence of 10 mol% DBU. 2 reacted with hydrazine to form 5-amino-3-[(3-trifluoromethyl)anilino]-1H-pyrazol-4- nitrile 3, the target compounds 5a, 5b, 5c, 5d, 5e, 5f, 5g, 5h, 5i, 5j, 5k, 5l, 5m were obtained by the reaction of 3 with triethyl orthoformate followed by the cyclization of 4 with various amines. Their structures were confirmed by IR, 1H NMR, EI-MS, and elemental analyses. The preliminary bioassay indicated that some of them displayed moderate herbicidal activity against dicotyledonous weed Brassica campestris L at the concentration of 100 mg/L. For example, compounds 5f, 5g, 5h, and 5j possessed 60.1%, 63.4%, 67.1%, and 61.3% inhibition against Brassica campestris L at the concentration of 100 mg/L.

1-Acyl-3,6-diphenyl-1,4-dihydro-1,2,4,5-tetrazines were prepared by treatment of 3,6-diphenyl-1,4- (or 1,2)-dihydro-1,2,4,5-tetrazine and an equimolar amount of an acyl chloride. Further reaction with another equivalent of an acyl chloride yielded 1,4(or 1,2)-diacyl-3,6-diphenyl-1,4(or 1,2)-dihydro-1,2,4,5-tetrazines. Their structures are confirmed by 1H NMR, IR, and mass spectra and by elemental analysis and X-ray diffraction. The experimental results are also validated by calculation of molecular stabilisation energies with the DFT calculations (B3LPY method). It can be shown that when alkanoyl chlorides are used, the products are the 1,4-dihydro-1,2,4,5-tetrazines, whereas acylation with aroyl chlorides affords 1,2-dihydro-1,2,4,5-tetrazines.

Ethnopharmacological relevance Cuscuta chinensis ( C. chinensis ) is a well-known traditional Chinese herb that has been used to treat heart disease, diabetes, liver injury, cancer, and aging. Materials and methods Murine osteoblastic MC3T3-E1 cells were treated with various concentrations of C. chinensis water extraction at different time intervals. The antioxidant effect of C. chinensis on MC3T3-E1 cells was evaluated using MTT and TUNEL assays. The effect of C. chinensis on cell cycle was analyzed by flow cytometry with propidium iodide. Lipid peroxidation was measured by the HPLC method. The cellular redox status was determined from the reduced glutathione to oxidized glutathione ratio (GSH/GSSG) and the enzymes involved in glutathione metabolism, including glutathione reductase (GR), Glutathione S-transferase (GST), and Glucose-6-phosphate dehydrogenase (G6PD). The changes in relative mitochondrial transmembrane potential (Δ Ψm ) in the MC3T3-E1 cells were analyzed with rhodamine 123 staining. Western blot analysis was used to evaluate the levels of cytochrome c (cyto c ), Bax, Bcl-2, caspase 3, Sirt3, and IDH2 expressions. Results The C. chinensis water extraction protects tertiary butyl hydroperoxide (TBHP)-treated MC3T3-E1 cells from death in a dose-dependent manner. C. chinensis treatment significantly inhibited the reactive oxygen species (ROS) generation, malondialdehyde (MDA) production, and increased the activity of superoxide dismutase (SOD), GR, GST, and G6PD. The release of cyto c from mitochondria was reduced by C. chinensis , which increased the expression of antiapoptotic IDH2, Sirt3, and Bcl-2 and decreased the expression of Bax, cyto c , and caspase 3. Conclusions C. chinensis modulated the oxidative stress-induced apoptosis in MC3T3-E1 cells, probably due to its antioxidant activity and functioning via mitochondria-dependent pathways.

The aim of this study was to investigate the therapeutic efficacies and treatment effects of absolute ethanol and bleomycin for the treatment of venous malformation (VM) in children. A total of 138 children with VM were randomly divided into two groups; 75 patients were treated with absolute ethanol, while a further 63 were treated with bleomycin under general anesthesia between February 2009 and February 2012. The treatment outcome and complications were observed in the two groups and the treatment efficacy was classified as one of four categories: cured, markedly effective, effective and ineffective. The curative effect was analyzed 6–24 months after treatment, with a mean of 15 months. Absolute ethanol was effective (cured, markedly effective or effective) in 71 cases and bleomycin was effective in 41 cases, and the difference between the effective rates was considered to be statistically significant (χ2=19.6, P

This study was designed to investigate the antifebrile effect and mechanisms of Bai-Hu decoction (BHD), a traditional Chinese medical (TCM) prescription. The rabbits used in this study received an intravenous injection of lipopolysaccharide (LPS) after being orally administered with BHD, ibuprofen, or saline, and their rectal temperatures were monitored by a copper–constantan thermocouple. Concentrations of interleukin-1 beta (IL-1β) and tumor necrosis factor alpha (TNF-α) in serum and hypothalamus were assayed using the commercially available rabbit IL-1β and TNF-α enzyme-linked immunosorbent assay kits following the manufacturer’s instructions. The BHD treatment group exhibited a significant fall in body temperature in both peaks compared with the LPS group (p

A rare hetero dimeric terpenoid derivative, named japonicaside C, together with five known secoiridoid gloucosides were isolated from the flower buds of Lonicera japonica. The structures of these compounds were established on the basis of spectroscopic analyses. Japonicaside C is the first representative of a novel type of hetero dimeric terpenoid, biogenetically originated from a guaiane-type sesquiterpenoid and a secoiridoid glucoside. Anti-virus activity of the isolated compounds was evaluated in vitro.

Nine fungal strains, previously isolated from produced wastewater in Liaohe oilfield in China, were screened for the study on the biodegradation ability of heavy oil in a batch of shake-flask culture. Among them, fungi F1, F4, F5 and F7 showed relatively higher abilities for the biodegradation of heavy oil. Heavy oil removal rates after 56 days by the above four strains were 57.82 %, 63.30 %, 36.46 % and 45.63 %, respectively. In addition, the biodegradation process followed the first- order kinetics, and the half- life of heavy oil from long to short order was F5>F7>F1>F4. By contrast, fungus F4 was the highest effective strain for heavy oil degradation. Degradation rates of petroleum fractions by different fungal strains varied significantly. And the highest degradation rates of alkanes was 42.99 % by F5, and correspondingly, that of aromatics with 37.87 % by F1, and that of colloids and asphaltenes with 46.42 % by F4.

For high grade pipeline steel, elimination of Al2O3 inclusions can improve the susceptibility of hydrogen-induced cracking (HIC) and stress corrosion cracking (SCC). In the present work, the transformation of Al2O3 inclusions with slag-metal reaction was studied by controlling ladle slag and relative technologies in LF-RH refining process. It is found that Al2O3 inclusions decrease with increasing refining time, and no pure Al2O3 inclusions exist in molten steel at the end of secondary refining; the remained inclusions in molten steel are liquid calcium aluminates and semi-liquid CaO-MgO-Al2O3 complex inclusions. The analysis of thermodynamic equilibrium proves that CaO and MgO in slag can be reduced by aluminum in molten steel, which is the source of calcium and magnesium in molten steel.

The aim of this article is to investigate the mechanism of vitexin-4''-O-glucoside (VOG) protecting ECV-304 cells against tertbutyl hydroperoxide (TBHP)-induced injury. ECV-304 cell viability was measured by MTT assay. Apoptosis was determined by terminal deoxynucleotidyl transferase-mediated dUTP nick end-labelling (TUNEL) assay. Cellular morphological changes were observed using phase contrast microscopy. The change of relative mitochondrial transmembrane potential in the ECV-304 cells was analysed with rhodamine 123 staining. Lipid peroxidation was measured by the HPLC method. The results showed that 128 µmol L(-1) VOG could effectively protect ECV-304 cells against cytotoxicity induced by TBHP. VOG protected TBHP-treated ECV-304 cells from death, significantly decreased MDA production, and increased superoxide dismutase (SOD) activity and mitochondrial membrane potential (ΔΨ). Taken together, VOG protects against TBHP-induced ECV-304 cell injury partially through resuming mitochondrial function.

Aim Accumulating evidence has indicated that Panax notoginseng saponins (PNS), the major ingredients in Panax notoginseng ( Burk. ) F.H. Chen which could be found widely in Asia, can attenuate atherogenesis in vivo . This study was designed to examine the relationship of PNS with cholesterol ester in foam cells sourced from macrophages and the effect of PNS on the expression of ATP-binding cassette transporter A1 (ABCA1). Materials and methods Foam cells sourced from macrophages were cultured with PNS. The content of cholesterol ester in foam cells was analyzed and expressions of ABCA1 and liver X receptor α (LXRα) in foam cells were measured by real-time PCR and western blotting methods. Results The results showed that PNS could significantly decrease the level of cholesterol ester in foam cells at middle and high dosages. The real-time PCR and western blotting assays indicated that the expression of ABCA1 was up-regulated by PNS in a dose-dependent manner. Analysis based on these results showed that the cholesterol ester level was negatively correlated with ABCA1 expression. Conclusions As a result, we conclude that by up-regulating the expression of ABCA1, PNS could lower the cholesterol ester level, which resulted in the attenuation of the foam cell formation. This bioactivity might be associated with the special chemical structures of PNS that are similar to the natural agonist of LXRα.

A lab-incubation experiment was conducted to investigate the effects of different forms of nitrogen application (ammonium, NH4+-N; nitrate, NO3−-N; and amide-N, NH2-N) and different concentrations (40, 200 and 800 mg L−1) on N2O emission from the fluvo-aquic soil subjected to a freezing-thawing cycling. N2O emission sharply decreased at the start of soil freezing, and then showed a smooth line with soil freezing. In subject to soil thawing, N2O emission increased and reached a peak at the initial thawing stage. The average N2O emissions with addition of NH4+-N, NO3−-N and NH2-N are 119.01, 611.61 and 148. 22 μg m−2 h−1, respectively, at the concentration of 40 mg L−1; 205.28, 1 084.40 and 106.13 μg m−2 h−1 at the concentration of 200 mg L−1; and 693.95, 1820.02 and 49.74 μg m−2 h−1 at the concentration of 800 mg L−1. The control is only 100.35 μg m−2 h−1. N2O emissions with addition of NH4+-N and NO3−-N increased with increasing concentration, by ranging from 17.49 to 425.67% for NH4+-N, and from 563.38 to 1 458.6% for NO3−-N compared with control. There was a timelag for N2O emission to reach a steady state with an increase of concentration. In contrast, by adding NH2-N to soil, N2O emission decreased with increasing concentration. In sum, NH4+-N or NO3−-N fertilizer incorporated in soil enhanced the cumulative N2O emission from the fluvo-aquic soil relative to amide-N. This study suggested that ammonium and nitrate concentration in overwintering water should be less than 200 and 40 mg L−1 in order to reduce N2O emissions from soil, regardless of amide-N.

Dissolved organic matter (DOM) influences many aspects of drinking water treatment, including the formation of harmful disinfection by-products (DBPs) when disinfectants are applied. DOM was isolated and fractionated using membrane ultra-filtration (UF) and reverse osmosis (RO) to eight individual fractions based on molecular weight cut-offs from a conventional surface water treatment plant (WTP) in Guangzhou of PR China. Molecular weights of these eight fractions were further calibrated using high performance size exclusion chromatography (HPSEC) and they ranged from 0.36 to 182.6 kDa. Fractions with molecular weight

To discover the new medicinal activity, the structure of diflunisal has been modified. Forty amide derivatives of diflunisal were synthesized starting from diflunisal in three steps. Their inhibition growth rate of human lung cancer cell (A549) and human endometrial adenocarcinoma cell (Ishikawa) in vitro was evaluated. The preliminary assay results showed that compounds 6j, 7o and 8c exhibited good anti-tumor activities and excellent selectivity for the Ishikawa cell, may be potential anti-tumor agents.

A simple high-performance liquid chromatographic (HPLC) assay using the internal standard method is developed for the simultaneous determination of eight polyphenols. The analyzed compounds isolated from the leaves of Crataegus pinnatifida Bge. var. major include chlorogenic acid, vitexin-4"-O-glucoside, vitexin-2"-O-rhamnoside, vitexin, rutin, hyperoside, isoquercitrin, and quercetin. HPLC analysis is performed on a Diamonsil C18 analytical column (150 x 4.6 mm, i.d., 5-microm) using solvent (A) acetonitrile-tetrahydrofuran (95:5, v/v) and (B) 1% aqueous phosphoric acid as the mobile phase with UV absorption at 270 nm. The calibration curves of the eight polyphenols are linear (r(2) > 0.9992) over the concentration range of 0.0894-120.0 microg/mL. The mean recoveries are 95.4% to 98.1%. The results indicate that the HPLC method developed can easily be applied to the determination of eight polyphenols in the leaves of Crataegus pinnatifida Bge. var. major.

To investigate the antioxidant effect of vitexin-4''-O-glucoside, a flavone glycoside, isolated from the leaves of Crataegus pinnatifida Bge. var. major, we developed a simple and sensitive high-performance liquid chromatography (HPLC) method to determine levels of malondialdehyde (MDA) in ECV304 cell culture medium after induction by tert-butyl-hydroperoxide (TBHP). The preparation of analyzed samples involved a one-step derivatization with thiobarbituric acid (TBA). HPLC analysis was performed on a Synergi Hydro-RP, a polar end-capped C18 column (250 x 4.6 mm, 4 mum), using an acetonitrile-ammonium acetate aqueous solution (10 mM, pH 6.8) as the mobile phase under linear gradient conditions with UV detection at 532 nm. The calibration curve was linear over 0.0125-1.25 microM MDA (r = 0.9951). Relative standard deviations (RSDs) of intra-day and inter-day precision were less than 6.1% and 5.0%, respectively. The mean recovery was 96.9 +/- 1.6%. The lower limit of quantification (LLOQ) of MDA was 0.0125 microM. This chromatographic method was successfully applied to investigating the in vitro antioxidant effect of vitexin-4''-O-glucoside. Vitexin-4''-O-glucoside (120 M) protected ECV304 cells from peroxidation induced by TBHP.

We have reported that the protective effect of Magnolol on TBHP-induced injury in human nonsmall lung cancer H460 cells is partially via a p53 dependent mechanism. In this study, we found that Magnolol displayed a stimulatory effect at low concentrations (or = 20 microM) whilst inhibitory effect at high concentrations (or = 40 microM) in H460 cells. To investigate the mechanism of inducing the biphasic effect in H460 cells with Magnolol, we showed that Magnolol stimulated DNA synthesis at low concentrations and displayed an inhibition effect at high concentrations in H460 cells. More importantly, the inhibition of DNA synthesis was accompanied by the S phase cell cycle arrest and the appearance of intense intracytoplasmic vacuoles. These vacuoles can be labeled by autophagic marker monodansylcadaverin (MDC), 3-methyladenine (3-MA), an inhibitor of autophagy, was able to inhibit the occurrence of autophagy. The results of the LDH activity assay and TUNEL assay also showed that Magnolol at high concentrations inhibiting H460 cell growth was not via apoptotic pathway. Furthermore, accompanied by the occurrence of autophagy, the expression of phospho-Akt was down-regulated but PTEN significantly was up-regulated. In conclusion, Magnolol induces H460 cells death by autophagy but not apoptotic pathway. Blockade of PI3K/PTEN/Akt pathway is maybe related to Magnolol-induced autophagy. Autophagic cells death induction by Magnolol underlines the potential utility of its induction as a new cancer treatment modality.

Problem The relationship between genital infection and two sperm parameters, namely, concentrations of nitric oxide (NO) and cytokines [e.g., interleukin (IL)-17 and IL-18], in the semen of infertile males remains undetermined. Method of study Semen samples from 81 infertile (with or without Ureaplasma urealyticum infection) and normal males were subjected to semen analysis. Results Nitric oxide concentration in the semen of infertile males with genital infection was higher than those of infertile males without genital infection and of normal males (P < 0.05). Sperm density, pH, percentage of forward, movement of sperm, sperm activation rate, sperm survival rate, and normal rate of the sperm morphology of infertile males with U. urealyticum infection were significantly lower than those of infertile males without genital infection and of normal males (P < 0.05). NO concentrations were also positively correlated with IL-17 and IL-18 concentrations in the semen of infertile males. Conclusion Increased NO concentration and abnormal IL-17 and IL-18 expression were induced by genital infection and induced damage to male reproductive capacity, thereby causing male infertility.

River water sample was collected from Guangzhou section of the Pearl River to investigate soluble organic fractions and formation of trihalomethane (THMs) after chlorine and chlorine dioxide treatments. The water sample was passed through Amicon® YC-05, YM-1, YM-3, YM-10, YM-30, YM-100 and ZM-500 series membranes after a pre-treatment. The molecular weight distribution and the specific ultra-violet absorbance (SUVA254) of each fraction obtained from membrane were analyzed, and these fractions were further disinfected with chlorine and chlorine dioxide. The results showed that reverse osmosis (RO) fraction contained mainly dissolved organic matter (DOM) from the water sample, suggesting that the water has been highly contaminated by anthropogenic activities. Meanwhile, the THMs concentration and SUVA254 increased gradually as the molecular weight of the obtained fractions reduced, indicating that the low molecular weight DOM was the major THMs precursor in the disinfection process with chlorine and chlorine dioxide. The results suggest that THMs in source water of Pearl River could be effectively reduced when pollution of human activity is greatly controlled. Between the two disinfection processes tested, chlorine dioxide produced less THMs than chlorine in this study.

A series of novel 5-alkyl(aryl)-3-[(3-trifluoromethyl)anilino]-4,5-dihydro-1H-pyrazolo[4,3-d]pyrimidin-4-imines were designed and synthesized by the multistep reactions. 1 reacted with 3-(trifluoromethyl)aniline to obtain N,S-acetals 2 in the presence of 10 mol% DBU. 2 reacted with hydrazine to form 5-amino-3-[(3-trifluoromethyl)anilino]-1H-pyrazol-4- nitrile 3, the target compounds 5a, 5b, 5c, 5d, 5e, 5f, 5g, 5h, 5i, 5j, 5k, 5l, 5m were obtained by the reaction of 3 with triethyl orthoformate followed by the cyclization of 4 with various amines. Their structures were confirmed by IR, 1H NMR, EI-MS, and elemental analyses. The preliminary bioassay indicated that some of them displayed moderate herbicidal activity against dicotyledonous weed Brassica campestris L at the concentration of 100 mg/L. For example, compounds 5f, 5g, 5h, and 5j possessed 60.1%, 63.4%, 67.1%, and 61.3% inhibition against Brassica campestris L at the concentration of 100 mg/L.

Three new iridoid glucosides, 6″-O-trans-feruloylgenipin gentiobioside (1), 2'-O-trans-caffeoylgardoside (2), jasmigeniposide A (3), and one new bis-iridoid glucoside, jasmigeniposide B (4), along with six known analogues (5-10), were isolated from the fruit of Gardenia jasminoides. Their structures were established on the basis of spectroscopic analyses and chemical methods. Anti-virus activity of isolated compounds were evaluated in vitro and only compound 9 showed moderate inhibitory activity against H1N1 with 50% effective concentration (EC50) value of 104.36 μM, and selective index (SI) value greater than 4.79.

In the title compound, C22H19Cl2N5S, the thiazole and pyrimidine rings are almost co-planar, making a dihedral angle of 6.48 (7)°. In the crystal, intermolecular N—H...N hydrogen bonds link pairs of molecules into centrosymmetric dimers..

A series of novel compounds 7-43 were prepared via the condensation of enaminones 4a-h and the guanidines carbonate 6a-f. The structures of these newly synthesized compounds were confirmed by (1) H-NMR, MS, EA and IR. All the compounds were tested for their cytotoxic activity in vitro against human cancer cell lines including Ishikawa, A549, BEL-7404, SPC-A-01 and SGC-7901. Most of them showed moderate cytotoxic against the tested cell lines. Among them, the most potent compounds 9 and 30 exhibited more efficient activity against Ishikawa, A549.

International audience; Natural rubber (poly(1,4-cis-isoprene), NR) is a polymer of considerable industrial importance due to its exceptional properties. It is mostly produced from the cultivation of Hevea brasiliensis, and to a limited extent from Parthenium argentatum. Till date none of the synthetic equivalent of NR exists. Recently we suggested that the mechanism of NR biosynthesis is based on carbocationic polymerization, similarly to that of natural oligoisoprenoids forming by enzyme-catalyzed prenylation. In this article we present proof of concept of a new bio-inspired synthetic route towards the synthesis of polyisoprenes based on carbocationic polymerization initiated by dimethyl allyl bromide (DMABr)/TiCl4. It is shown that using this strategy, 1,4-oligoisoprene carrying a dimethyl allyl head group is produced in both cis and trans configurations, together with cyclized sequences

A series of caffeic acid amide derivatives 2-cyano-(3-substituted phenyl)acrylamides were synthesized via Knoevenogal condensation of substituted benzaldehydes with cyanoacetamides. The structure of compound 1f was determined as E-isomer by X-ray diffractive analysis. The biological screening tests in vitro showed that compound 1b has obvious inhibitory activities against human gastric carcinoma cell line BGC-823, human nasopharyngeal carcinoma cell line KB and human hepatoma cell line BEL-7402 with IC(50) values of 5.6 microg/mL, 13.1 microg/mL and 12.5 microg/mL, respectively. Some preliminary structure-activity relationships (SAR) were also proposed which may provide a direction for further study.

Ligularia is mainly distributed in the western regions of China. Most of the species have been traditionally used in folk medicine for the treatment of hepatitis B, asthma, hemoptysis and pulmonary tuberculosis. In our continuation of research on antiviral components from traditional Chinese medicine, Ligularia atroviolacea was tested for inhibitory effects on hepatitis B virus (HBV). A bioassay-guided phytochemical examination of L. atroviolacea disclosed that its ethyl acetate extract, which was made up of two eremophilenolides, showed suppressive activity on the expression of HBV surface antigen (HBsAg) in the HepG2.2.15 cell line. Then a simple and effective preparative high-speed counter-current chromatography method was successfully developed for the isolation and purification of two main active metabolites, 8beta-hydroxyeremophil-3,7(11)-dien-12,8alpha;15,6alpha-diolide and 8beta-methoxyeremophil-3,7(11)-dien-12,8alpha;15,6alpha-diolide from the ethyl acetate extract of L. atroviolacea by a one-step separation using a two-phase solvent system composed of light petroleum (60-90 degrees C)-ethyl acetate-methanol-water (9:1:8:2, v/v/v). The chemical structures of the two eremophilenolides were identified by ESI-MS, (1)H-NMR and (13)C-NMR analysis. The anti-HBV activity of the two purified compounds was measured; both of them showed suppressive activity on the expression of HBsAg in the HepG2.2.15 cell line. The results support the continued and expanded exploitation and utilization of L. atroviolacea.

The aim is to investigate the effect of Magnolol preserved H460 cells from an oxidative agent tert-butylhydroperoxide (TBHP)-induced cell death. Magnolol augmented cell survival ratio after TBHP challenged. The protective action of this drug was more efficacious than that of N-acetylcysteine (NAC) which is a putative antioxidant. DNA damage, detected by the comet assay, was diminished after treatment of Magnolol. The cells viability decreased after treatment with 0.15 mM TBHP for 24 h, accompanied by inducing apoptotic death of the cells. Cytotoxicity and apoptosis induced by TBHP were significantly inhibited or attenuated after pretreatment with 20 microM Magnolol. Magnolol contributes to the cells survival through downregulated the p53 phosphorylation and PTEN expression, and upregulated Akt phosphorylation. Taken together, Magnolol was effective against DNA single strand breaks (SSB) formation, cytotoxicity and lipid peroxidation induced by TBHP, and its effects on p53 phosphorylation, PTEN and Akt phosphorylation were due to its antioxidative function, and partially via a p53 dependent mechanism in this protective effects.

The aim of the present study was to investigate the mechanism of hyperoside protecting ECV-304 cells against tertbutyl hydroperoxide (TBHP)-induced injury. ECV-304 cell viability was measured by MTT assay. Cellular morphologic changes were observed using phase contrast microscopy. The genotoxic effects of TBHP and the protective ability of hyperoside were assessed by the Comet test. Lipid peroxidation was measured by HPLC method. The cellular redox status was determined from GSH/GSSG ratios. Apoptosis was detected by terminal deoxynucleotidyl transferase-mediated dUTP nick end-labeling (TUNEL) assay. Western blot analysis was used to evaluate the levels of cytochrome c, p53, SIRT1, Bax and Bcl-2 expression. The results showed that 128 µmol/l hyperoside could effectively protect TBHP-treated ECV-304 cells from death, increase superoxide dismutase activity and significantly decrease malondialdehyde production. Hyperoside was effective in protecting against the induction of oxidized DNA bases and redox state alterations induced by TBHP. Furthermore, the release of proapoptotic cytochrome c from mitochondria was reduced by hyperoside, which increased the expression of antiapoptotic SIRT1 and inhibited the translocation of Bax from cytoplasm to mitochondria. Taken together, these results indicate that hyperoside is effective in protecting against the oxidative damage induced by TBHP. The mechanism of hyperoside protecting against ECV-304 cell apoptosis by TBHP is related with resuming mitochondrial function and regulating the expression of SIRT1 and Bcl-2 family members.

In the title compound, C23H23N5S, the thiazole ring and pyrimidine ring are almost coplanar, making a dihedral angle of 4.02 (9)°. in the crystal, weak intermolecular N—H...N interactions link pairs of molecules into centrosymmetric dimers.

The asymmetric unit of the title compound, C23H23N5OS, contains two independent molecules. In one molecule, the thiazole and pyrimidine rings are almost co-planar, making a dihedral angle of 2.48 (8)°. In the other molecule, the corresponding dihedral angle is 12.82 (8)°. The crystal structure is stabilized by weak intermolecular N—H...N and C—H...O interactions that extend along the b axis.