Search

Liriogerphines A-D (

Four unprecedented cycloheptanone-containing and some related known bioactive polyketides were isolated from an endophytic fungus associated with the critically endangered conifer Abies beshanzuensis.

The aim of the present study was to discuss the design of a microfluidic chip consisting of columns, and its use for the enrichment of nasopharyngeal cancer (NPC) cells. A microfluidic chip experiment was simulated using FLUENT software. Within the microfluidic chip, aptamers were bound to the reaction chamber (consisting of columns) using a biotin-avidin system. Cell suspension was introduced into the reaction chamber to capture NPC cells. NPC cells were subsequently eluted, and the capture rate of the cells was calculated. The modified aptamer-bound microfluidic chip was able to capture NPC cells with a capture rate of ~90%. The modified aptamer-bound microfluidic chip has a wide range of potential applications for the diagnosis of NPC.

Based on molecular simulation, the etravirine-VRX-480773 hybrids previously disclosed by our group were optimized to yield novel pyrimidine sulfonylacetanilides 8 with improved activity against a panel of seven clinically relevant single and double mutant strains of HIV-1. The improvement in potency in this in vitro model of HIV RNA replication partly validates the mechanism by which this class of allosteric pyrimidine derivatives inhibits the reverse transcriptase (RT), and represents a remarkable step forward in the development of anti-HIV drugs.

Black pepper extracts reportedly inhibit food spoilage and food pathogenic bacteria. This study explored the antimicrobial activity of black pepper chloroform extract (BPCE) against Escherichia coli and Staphylococcus aureus. The antibacterial mechanism of BPCE was elucidated by analyzing the cell morphology, respiratory metabolism, pyruvic acid content, and ATP levels of the target bacteria. Scanning electron micrographs showed that the bacterial cells were destroyed and that plasmolysis was induced. BPCE inhibited the tricarboxylic acid pathway of the bacteria. The extract significantly increased pyruvic acid concentration in bacterial solutions and reduced ATP level in bacterial cells. BPCE destroyed the permeability of the cell membrane, which consequently caused metabolic dysfunction, inhibited energy synthesis, and triggered cell death.

A series of new DAPY-DPEs hybrids, combined the important pharmacophores of DAPYs and DPEs, has been synthesized and biologically evaluated for their anti-HIV activities against wild-type HIV-1 strain IIIB, double RT mutant (K103N+Y181C) strain RES056 and HIV-2 strain ROD in MT-4 cell cultures. Many promising candidates with potent inhibitory activity (wild-type) within the EC50 range from 0.16 to 0.013 μM were obtained. In particular, 3c, 3p, 3r and 3s displayed low nM level EC50 values (35, 13, 50 and 17 nM, respectively) and high selectivity (9342, 25131, 2890 and 11338, respectively), which were much more potent than NVP (EC50=0.31 μM, SI=48), 3TC (EC50=2.24 μM, SI>39), DDI (EC50=23.20 μM, SI>9) and DLV (EC50=0.65 μM, SI>67), and comparable to AZT (EC50=0.0071 μM, SI>13144) and EFV (EC50=0.0062 μM, SI>1014). The HIV-1 reverse transcriptase inhibitory assay confirmed that these DAPY-DPEs hybrids targeted HIV-1 RT. Molecular simulation was performed to investigate the potential binding mode of the newly synthesized compounds. And reasonable explanation for the activity results was discussed with docking method.

A new series of 29 diarylpyrimidine analogues featuring a cyclopropylamino group between the pyrimidine scaffold and the aryl wing have been synthesized. All of the new compounds have been characterized by spectra analysis. The target molecules were evaluated for their in vitro anti-HIV activity with FDA-approved drugs as references. Some of the compounds exhibited moderate to potent activities against wild-type HIV-1. The compound 4-((4-((cyclopropylamino)(2,5-difluorophenyl)methyl)pyrimidin-2-yl)amino)benzonitrile (1e) displayed potent anti-HIV-1 activity against WT HIV-1 with an IC50 of 0.099 μM and a selectivity index of 2302. The preliminary structure-activity relationship (SAR) of this new series of compounds was also investigated.

A series of new diarylpyrimidines (DAPYs) characterized by a halogen atom on the methylene linker between wing I and the central pyrimidine ring was synthesized and evaluated for their anti-HIV activity in MT-4 cell cultures. The two most promising compounds 7f and 7g showed excellent activity against wild-type HIV-1 with low nanomolar EC 50 values of 0.005 and 0.009 μM, respectively, which were comparable to or more potent than all the reference drugs zidovudine (AZT), lamivudine (3TC), nevirapine (NEV), efavirenz (EFV), delaviridine (DLV) and etravirine (ETV). In particular, 7g also displayed strong activity against the double mutant strain 103N + 181C with an EC 50 value of 8.2 μM. The preliminary structure–activity relationship (SAR) and molecular docking analysis of this new series of CHX-DAPYs were also investigated.

Here we report the asymmetric amination of 3-(2-oxoindolin-3-ylidene)butanoates catalyzed by a cinchona-derived alkaloid, yielding products with an N-containing stereocenter in high yields and moderate enantioselectivity. The developed process could be an attractive approach for the synthesis of chiral amino acids.

The main aim of the present work was to optimize mead production using Response Surface Methodology. The effects of pH (X1:4–6), diammonium phosphate concentration (X2: 90–150g/hL), and temperature(X3: 24–32°C) on mead quality, concerning the final ethanol, was studied. The results showed that regression equation fit well with experimental data and the optimum extraction conditions determined in order to maximize the combined responses were pH value of 6.5, diammonium phosphate concentration of 150g/hL, temperature of 28°C. The mead produced under these conditions had the following characteristics: ethanol concentration of 9.3% and good flavor.

A series of C6-rigid S-DABO analogs characterized by a substituted benzoyl group at C6 position of the pyrimidine ring has been synthesized and biological evaluation as NNRTIs against wild-type HIV-1 strain IIIB, double RT mutant (K103N + Y181C) strain RES056 as well as HIV-2 strain ROD in MT-4 cell cultures. Most of the compounds exhibited moderate antiviral activities. Among them, compound 7q displayed the highest anti-HIV-1 activity with an EC50 value of 0.26 μM and a selectivity index (SI) of 541. The preliminary structure–activity relationship (SAR) of these new S-DABOs was investigated, the target RT was confirmed and docking study was performed.

Substances from Fructus Alpinia Oxyphylla (AOF) were extracted by using solvent extraction. In accordance with central composited design of response surface methodology system, the extracts were analyzed for the index which is the criteria formula of multiplying OD value by the yield. The optimum conditions obtained were extraction temperature of 60°C, liquid-solid ratio of 9mL/g, and solvent density of 80%. According to Ficks second law of diffusion, experimental parameters of K (rate constant), Ea (activation energy), Gs (effective diffusion coefficient) were gained, which represents a good agreement between the model simulation and the results of the actual process. The results can provide the valuable theory basis for the technical design and further research of extraction process. Antibacterial activities of the extraction were shown through MIC of which represents a significant effect.

A short and cyanide-free enantioselective synthesis of atorvastatin calcium has been achieved starting from a commercially available highly substituted 1,4-diketone in an overall yield of 40%. The key step in this approach is the asymmetric aldol reaction of an aldehyde with diketene in the presence of Ti(O-i-Pr)4–Schiff base complex to create the (5R)-stereochemistry of atorvastatin calcium.

In order to investigate the effect of magnetic field on the antibacterial substances from black pepper, we used shaking and ultrasonic-assisted ethanol extraction with Escherichia coli, Staphylococcus aureus, Bacillus anthracis and Aspergillus niger as indicator bacteria respectively. Meanwhile, extraction rate and diameter of inhibition zone were regarded as the activity monitoring parameters. The results showed the existence of magnetic field can make a difference. It weakened the antibacterial activity of black pepper by shaking extraction. However, the antibacterial activity of substances to Aspergillus niger was proportional to the intensity of the applied magnetic field by ultrasonic-assisted ethanol extraction.

The aim of this work was to optimize extraction procedure of antibacterial compounds from amomum tsao-ko and verify antibacterial ability of yields. Two methods were carried out and compared. One is ethanol reflux extraction, and the other is ultrasonic-assisted ethanol extraction which selected due to better antibacterial efficiency of the extract obtained. In order to improve extraction rate and antibacterial activity which both varied with ultrasonic-assisted extraction conditions, Box-Behnken design was employed. Studies showed that the optimum conditions for extraction antibacterial substances from amomum tsao-ko were determined to be: ethanol density 100%, soaking time 4h, extraction time 120min.

In this paper, the entangled strength of the subsystem of the Jaynes-Cummings model (JCM) is studied. Both the field and the atom are in thermal state. The expression of the entanglement (negativity) and its numerical analysis are shown. The numerical results show that there exists a critical temperature and frequency, the entanglement oscillates with time above a critical temperature and below a critical frequency; the entanglement is different in different subspace and decreases exponentially with the increase of the photon number of the subspace. One can control the entanglement through changing temperature, field frequency and different subspace.

The aim of this work was to optimize a simultaneous distillation-extraction (SDE) procedure for the volatile compounds of black pepper (Piper Nigrum L.). Several variables that could potentially affect the extraction efficiency, namely, the liquid: solid ratio (volume per mass), soaking time and simultaneous distillation-extraction time have been optimized by means of response surface methodology (RSM). The optimum technology conditions have been attained by RSM as follows: the ratio of liquid to solid 25:1, simultaneous distillation-extraction time 3h and the soaking time 1.5h, under the optimum operating conditions, the extraction yield was 1.458%.

In this study, the volatile compounds of pepper (Piper Nigrum L.) were extracted and analyzed by simultaneous distillation-extraction (SDE) and gas chromatography-mass spectrometry (GC-MS). The differences in volatile compounds were observed by GC-MS data sets. Results showed vinyl compounds were the most dominant volatiles in pepper by simultaneous distillation-extraction (SDE) and GC-MS, and 22 volatile compounds in the white pepper and black pepper were the same.

By employing the tensor analysis technique, we propose three schemes of controlled teleportation: series controlled, circular controlled and network controlled teleportation. We discuss the necessary and sufficient condition for realizing these schemes, in which we use a general two-qubit entangled state instead of the GHZ state as the communication channel. This enables successful implementation of teleportation without using the Hadamard operation.

The microstructures, wettabilities and mechanical properties of Sn–9Zn–xAg (x = 0, 0.1, 0.3, 0.5, 1 wt%) lead-free solders were investigated, respectively in this paper. Results show that, when the quantity of Ag added to the solder is 0.3 wt%, the microstructure of the solder becomes finer and more uniform than Sn–9Zn, and when the quantity of Ag is exceeded 0.3 wt% (upto 0.5–1 wt%), the AgZn3 intermetallic compounds appear in the solder. In particular, adding 0.3 wt% Ag improves the wettability due to the better oxidation resistance of the Sn–9Zn–0.3Ag solder. Results also indicate that adding 0.3 wt% Ag to the solder enhances mechanical property of soldered joint, at which the fracture micrographs show that plenty of small and uniform dimples could be observed on the Sn–9Zn–0.3Ag soldered joints fractures. When the content of Ag is upto 1 wt%, some Cu–Zn and Ag–Zn intermetallic compounds appear on the bottom of dimples, and the mechanical property of the soldered joint decreases.

In order to investigate the turbulent flow and mass transfer in primary settling tanks, numerical simulations are conducted by using a modified k−e two-layer model based Boussinesq’s approximation to model the Reynolds stress in primary settling tanks, and solving the governing equations using a hybrid finite analytic method (HFAM). The simulation results obtained using the mathematical model are compared with the experimental data and simulation results available in the literature, and the results of comparison indicate that the profiles of the primary velocity field are in line with the experimental results and the flow-through curve obtained using the mathematical model are in good agreement with the curves based on experimental data. It is therefore concluded that the HFAM approach can be used to simulate the turbulent flow and mass transfer in a primary settling tank, and the modified k−e two-layer model can be used to establish the velocity field distribution at the bottom of a primary settling tank.

Earlier we reported the identification of diarylpyrimidine-quinolone hybrids as a new class of HIV-1 NNRTIs. A few of these hybrids displayed moderate inhibitory activity against wt HIV-1 replication at submicromolar level, however, all of them lacked inhibitory activity against the double mutant virus (K103N/Y181C), which is the most prevalent NNRTI resistant-associated double mutant observed in the clinic. In the present study, we designed and synthesized a new series of diarylpyrimidine-quinolone hybrids featuring a halogen group at C-6' position of quinolone ring. The biological results indicated that most of these hybrids could inhibit wt HIV-1 replication at nanomolar level ranging from 0.088 to 0.0096 μM. The most promising hybrid 5c displayed a significant EC 50 value of 0.0096 μM against HIV-1 III B and of 0.98 μM against K103N/Y181C. Further docking studies revealed that these hybrids could be well located in the hydrophobic NNIBP of HIV-1 RT despite the bulky and polar properties of a quinolone 3-carboxylic acid scaffold in the molecules. These promising results suggested a high potential to further develop these hybrids as next-generation NNRTIs with improved antiviral efficacy and resistance profile.

To investigate the lysophosphatidic acid (LPA) receptors expression situation and their biological significance in human ovarian cancer cell lines and in human epithelial ovarian neoplasms.The reverse transcription-polymerase chain reaction (RT-PCR) and Western blotting were employed to measure the expression levels of LPA(1), LPA(2) and LPA(3) mRNA, LPA(2) and LPA(3) protein expression in cultured human ovarian cancer cell lines (3AO, SKOV3 and OVCAR3) and in human epithelial ovarian neoplasms. The immunocytochemical method was used to detect LPA(2) and LPA(3) protein expression in cultured human ovarian cancer cell lines.RT-PCR revealed that all ovarian cancer cell lines expressed LPA(1), LPA(2) and LPA(3) mRNA. The positive rates (100%; 86.4%; 88.2%) of LPA(1) mRNA in normal ovarian tissue, benign tumor and ovarian cancer were no significant difference (p0.05). The expression level of LPA(1) mRNA was significantly higher in normal ovarian tissue compared with that in benign tumor and in ovarian cancer tissue (p0.01). LPA(1) expression level was no significant difference in both benign tumor and ovarian cancer tissue (p0.05). LPA(2) mRNA-positive rates (92.6%) and expression level were significantly higher in ovarian cancer compared with that in benign tumor (31.8%) and in normal ovarian tissue (31.3%) (p0.01); LPA(2) mRNA-positive rates and expression level were no significant difference in both benign tumor and normal ovarian tissue (p0.05). LPA(3) mRNA-positive rates (92.6%) and expression level were significantly higher in ovarian cancer compared with that in benign tumor (31.8%) and in normal ovarian tissue (31.3%) (p0.01), LPA(3) mRNA-positive rates and expression level were no significant difference in both benign tumor and normal ovarian tissue (p0.05). LPA(1) mRNA expression level was significantly decreased compared with that of LPA(2) and LPA(3) in ovarian cancer (p0.01); Western blotting clearly revealed that all ovarian cancer cell lines showed LPA(2) and LPA(3) protein. The positive rates and expression level of LPA(2) and LPA(3) protein were significantly increased in ovarian cancer (92.6%; 92.6%) compared with that in benign tumor (45.5%; 45.5%) and that in normal ovarian tissue (43.8%; 43.8%) (p0.01); LPA(2) and LPA(3) protein-positive rates and expression level were no significant difference in both benign tumor and normal ovarian tissue (p0.05). Correlation of clinicopathological parameters showed that LPA receptors mRNA and protein expression were associated with FIGO stage and histological grade, except pathologic types and age. The mRNA and protein expression of LPA(2) and LPA(3) in stages III and IV was significantly higher than that in stages I and II epithelial ovarian cancer (p0.05). The mRNA and protein expression of pathologic grade G(3) was significantly higher compared with grade G(1) (p0.05).LPA(1), LPA(2) and LPA(3) mRNA and protein expressed widely in human epithelial ovarian neoplasms. LPA(2) and LPA(3) may be involved in the development and progression of human ovarian cancer. There was a significant correlation between LPA(2), LPA(3) and invasion and metastasis of epithelial ovarian cancer. LPA(2) and LPA(3) may be a prognostic indicator in patients with epithelial ovarian cancer.

To study hypoglycemic effect and mechanism of the total flavonoids of Propolis (TFP) in the STZ diabetic rats.The model of type 2 diabetic rats was induced by high-fat diet feeding for 4 weeks combined with intraperitoneal injection of streptozotocin (STZ). Then the rats without above-mentioned treatment were selected as the normal control group,the diabetic rats were randomly divided into four groups by blood glucose, the model control group, high doses (240 mg/kg), medium doses (120 mg/kg) and low doses (60 mg/kg) TFP groups. The TFP preparation was intragastric administration given to rats in TFP groups. The model control rats were treated intragastric administration with 0.5% sodium carboxymethyl cellulose (CMC-Na) for 4 weeks. The rats were fed with high fat diet during treatment. 12 hours after the last administration, glucose (GLU), total cholesterol (TC), triglyceride (TG), high density lipoprotein( HDL-C), low density lipoprotein LDL-C), glycated hemoglobin (GHb), serum insulin INS), C-peptide (C-P), superoxide dismutase( SOD), malondialdehyde (MDA), glutathione (GSH), tumor necrosis factor-alpha (TNF-alpha), free fatty acid (FFA), nitric oxide (NO), and hepatic glycogen were determined.Compared with the normal group, the levels of GLU, TC, TG, HDL-C, FFA, TNF-alpha, NO, MDA and GHb in serum were increased significantly in the model control group (P0.05-P0.001), the levels of HDL-C, INS, C-P, SOD and GSH in serum and hepatic glycogen in hepatic tissue were decreased significantly (P0.01 or P0.001). The levels of all above indexes of high and medium doses groups were improved significantly compared with the model control group (P0.05-P0.01).TFP can significantly decrease the level of blood glucose,improve the glucose and lipid metabolism and inhibit insulin resistance in STZ diabetic rats.

Self-mixing interferometry (SMI) based on nanometer fringes and polarization flipping is realized. The interferometer comprises a single-mode He-Ne laser and a high-amplitude reflectivity feedback mirror. The nanometer fringes are obtained by tilting the external feedback mirror. The fringe density is 35 times higher than that derived with conventional two-beam interference, and each fringe corresponds to a λ/70 displacement in external cavity length. Moreover, polarization flipping occurs when the external feedback mirror moves in the opposite direction. Such movement can be used to easily distinguish displacement direction. Experimental results show an optical resolution of displacement measurement of 9.04 nm with a range of 100 µm. The proposed SMI presents promising application prospects in precisely measuring displacement and calibrating other micro-displacement sensors because of its optical wavelength traceability.

A molecular hybridization approach is a powerful tool in the design of new molecules with improved affinity and efficacy. In this context, a series of diarylpyrimidine–quinolone hybrids were synthesized and evaluated against both wt HIV-1 and mutant viral strains. The most active hybrid 5a displayed an EC 50 value of 0.28 ± 0.07 μM against HIV-1 III B . A couple of enzyme-based assays clearly pinpoint a RT-targeted mechanism of action. Docking studies revealed that these hybrids could be well located in the NNIBP of HIV-1 RT despite the bulky and polar properties of a quinolone 3-carboxylic acid moiety in the molecules.

In this Letter, we have calculated the concurrence of the pairwise thermal entanglement for the four-qubit and five-qubit Heisenberg XX chain. It is found that there is a great difference between the even-qubit and the odd-qubit chain in the aspect of the critical temperature and of the existence of the entanglement for the case of the qubit number n no more than 5.

We studied the influence of the impurity to the entanglement in three-qubit Heisenberg XX chain and got the analytical expression of the concurrence C, go a step further, for fixed J , we discussed the concrete effect of the impurity parameter J1 to the concurrence. At the condition T → 0, when |J1 |�| J |, the concurrence C = (2 √ 2 − 1)/4; when J1 →− J and J →∞

To explore therapeutic effects of bone setting manipulation for the treatment of over degree II supination-eversion fractures of ankle,and analyze manipulative reduction mechanism.From 2005 to 2008, 95 patients with over degree II supination-eversion fractures of ankle were treated respectively by manipulation and operation. There were 43 cases [11 males and 32 females with an average age of (44.95 +/- 12.65) years] in manipulation group, and 2 cases were degree II, 11 cases were degree III, and 30 cases were degree IV. There were 52 cases [21 males and 31 females with an average age of (39.96 +/- 13.28) years] in operative group,and 6 cases were degree II, 18 cases were degree III, and 28 cases were degree IV. Bone setting manipulation and hard splint external fixation were applied to manipulative group. Operative reduction internal fixation was performed in operative group. X-ray was used to evaluate reduction of fracture before and after treatment, 2 months after treatment. Ankle joint function was evaluated according to Olerud-Molander scoring system after 6 months treatment.All patients were followed up with good reduction. Three cases occurred wound complication in operative group, but not in manipulative group. In manipulation group, 19 cases got excellent results, 20 cases good and 4 cases fair; while in operative group, 30 cases got excellent results, 20 cases good and 2 cases poor. There were no significant differences in fracture reduction and ankle joint function recovery between two groups (P0.05). Efficacy of operative treatment was better than that of manipulative treatment at degree IV fracture (P0.05).Bone setting manipulation is a good method for treating supination-eversion ankle joint fractures, which has advantages of simple and safe operation, reliable efficacy. For ankle join fracture at degree IV, manipulative reduction should be adopted earlier, and operative treatment also necessary

This article reports the design, synthesis and antiviral evaluation of a new series of non-nucleoside reverse transcriptase inhibitors (NNRTIs). The basic skeleton of these target 18 molecules is diarylpyrimidine featuring a substituted amino group between the pyrimidine scaffold and the aryl wing. All of the new compounds have been characterized by spectra analysis. The entire target molecules were evaluated for their in vitro anti-HIV activity with controlling group of FDA approved drugs. Most of them showed good to potent activities against wild-type (WT) HIV-1 with IC50 values in the range of 0.0175–69.21 μM. 2-(4-Cyanophenylamino)-4-(2-cyanovinylphenylhydrazonomethyl)pyrimidine (1d) displayed potent anti-HIV-1 activity against WT HIV-1 with a selectivity index (SI) of 106367 and an IC50 value of 1.75 nM, which was 47 fold lower than that of AZT. Compound 1d also showed a broad-spectrum inhibitory activity, with an IC50 value of 5.33 μM and 5.05 μM against both HIV-1 double-mutated (K103N/Y181C) strain and HIV-2 strain, respectively. The preliminary structure–activity relationship (SAR) was also investigated. The binding modes with HIV-1 RT for both the wild type and mutant type have also been discussed.

A series of CR 2 (OH)-diarylpyrimidine derivatives (CR 2 (OH)-DAPYs) featuring a hydrophobic group at CH(OH) linker between wing I and the central pyrimidine were synthesized and evaluated for their anti-HIV activity in MT-4 cell cultures. All the target compounds except for compound 3k displayed inhibitory activity against HIV-1 wild-type with EC 50 values ranging from 7.21 ± 1.99 to 0.067 ± 0.006 μM. Among them, compound 3d showed the most potent anti-HIV-1 activity (EC 50 = 0.067 ± 0.006 μM, SI > 592), which was approximately 2-fold more potent than the reference drugs nevirapine (NVP) and delaviridine (DLV) in the same assay. In addition, the binding modes with HIV-1 RT and the preliminary SAR studies of these new derivatives were also investigated.

To explore the clinical effects and safty of manipulative reduction with percutaneous poking K-wire fixation for the treatment of the calcaneus fractures and analyze the indication of the minimal invasion.From December 2008 to December 2011,135 closed calcaneal fractures cases were divided randomly into poking group and plate group, treated respectively by percutaneous poking reduction and operative reduction. In poking group, there were 69 cases (82 feet) including 60 males and 9 females, with an average age of (43.29+/-10.46) years ranging from 18 to 64 years; 30 cases of left, 26 cases of right and 13 cases of double; 54 feet of Essex-Lopresti classification tongue form, 28 feet of joint compression; 33 feet of Sanders type II ,49 of type III. In plate group, there were 66 cases (75 feet) including 58 males and 8 females,with an average age of (46.00+/-2.42) years ranging from 21 to 63 years; 31 cases of left, 26 cases of right and 9 cases of double; 48 feet of Essex-Lopresti classification tongue form, 27 feet of joint compression; 28 feet of Sanders type II, 47 of type III. According to Kerr scoring standard,clinical effects and complications were evaluated combining with Sanders and Essex-Lopresti classification.All 135 cases were followed up after 24 weeks. Fractures were recoveried in 8 to 12 weeks (means 10.2 weeks). In poking group, there were 2 cases of infection, 5 cases of wire movement; in plate group,18 cases of wound local skin necrosis, 5 cases of calf intestines nerve injured; there were statistical significant (P0.05). Postoperative evaluation of Sanders type II after 24 weeks, the proportion of excellent results was above 70%,and there were no significant differences on effects of tongue form and compressing form of calcaneus fractures with percutaneous poking and operative redution (P0.05). In the caes of Sanders type III, there were no significant differences on effects of tongue form fractures with percutaneous poking and operative reduction (P0.05). There were significant differences on effects and complications of compressing form fractures (P0.01), operative reduction better than percutaneous poking. Pain, walking,Kerr scoring of tongue form fractures of Sanders II , III with poking reduction were better than compression fractures. In compression fractures of Sanders Ill, plate internal fixation was better than poking redution in working and walking function, there were significant difference (P0.05).For tongue form or compressing form of Sanders type II and tongue form of Sanders type III, manipulative reduction with percutaneous poking K-wire fixation has advantages of minimal invasion, minimized complications. Compressing form of Sanders type III fracture should be treated with operative redution.

Nowadays, following an accident in coalmines, what affects emergent rescue efficiency is mainly attributable to the uncertain positions and physiological state of coalmine ersonnel. In view of such problem, the wireless communication network and its node structure were designed for coalmines with the aid of the emerging ZigBee technique. With this system, the information on the coalmine personnel is collected by the portable terminal node placed in the miners' lamp cap. Then, the data is transmitted via the underground wireless network to the emergency rescue center on the surface, which helps to reaLize positioning of personnel and monitoring of emergency state and provide assistance for effectively conducting emergency rescue.

The chemical structure and stereochemistry of 12 intermediates in the total synthesis of (+)-biotin starting from D-mannose as chiral pool were completely assigned using one- and two-dimensional NMR experiments, including 1D selective NOE, DEPT, COSY, HSQC and HMBC.

To explore the feasibility of the adenosine triphosphate-tumor chemosensitivity assay (ATP-TCA) in human cervical cancer chemosensitivity testing and to analyze the relationship between the three drug resistance-associated proteins: P-glycoprotein (P-gp); glutathione S-transferase-pi (GST-pi); thymidylate synthase (TS) and ATP-TCA.ATP-TCA was used to detect the sensitivity of 35 specimens of fresh cervical cancer to six cytotoxic drugs as follows: paclitaxel (TAX), cisplatin (DDP), bleomycin (BLM), gemcitabine (GEM), 5-fluorouracil (5-FU), irinotecan (CPT-11). Consecutive sections from 35 cases of cervical cancer were assessed immunohistochemically for expression of P-gp, GST-pi and TS proteins.(1) Thirty-two of 35 assays were completed successfully, with an evaluability rate of ATP-TCA at 91% (32/35). There was a marked heterogeneity of chemosensitivity in cervical cancer. The ex vivo sensitive rate of TAX was 88% (28/32), of 5-FU 72% (23/32), of GEM 62% (20/32), of DDP 19% (6/32), of BLM 16% (5/32), and of CPT-11 12% (4/32). (2) The expression of GST-pi and TS protein in cervical cancer was 66% (21/32) and 44% (14/32), which was associated with the resistance to DDP and 5-FU ex vivo (P=0.011, P=0.022), respectively; but the expression of P-gp protein was not associated with any resistance to TAX, 5-FU, GEM, DDP, BLM or CPT-11 ex vivo (P0.05).ATP-TCA could be used to individualize chemotherapy by selecting agents for particular patients of cervical cancer. The expression of GST-pi and TS protein might be useful biomarkers to predict the resistance to DDP and 5-FU in patients with cervical cancer.

To investigate the expression and correlation of KiSS-1, matrix metalloproteinase-9 (MMP-9) and nuclear factor (NF)-kappaBp65 proteins in primary epithelial ovarian tumors.Expression of KiSS-1, MMP-9, NF-kappaBp65 proteins in primary ovarian epithelial tumors (malignant n = 50, borderline tumor n = 20, benign adenoma n = 20, normal tissue n = 10) was evaluated by immunohistochemical staining.Expression of metastin protein in primary epithelial ovarian cancers was significantly higher than that in ovarian benign adenoma (P0.05) and normal tissues (P0.05). Expression of metastin protein in ovarian borderline tumors was significantly higher than that in normal tissues (P0.05). Expression of metastin protein in ovarian cancer was significantly correlated with node metastasis (P0.05). However, Metastin protein expression was not correlated with different histological classifications (P0.05), differentiation grade (P0.05) and International Federation of Gynecology and Obstetrics (FIGO) stage (P0.05). MMP-9 protein was positive in 68% (34/50) of the epithelial ovarian cancers, significantly higher than that in normal tissues (20%, 2/10; P0.05). NF-kappaBp65 protein was positive in 72% (36/50) of the epithelial ovarian cancers, significantly higher than that in ovarian benign adenoma (30%, 6/20; P0.05) and normal tissues (10%, 1/10; P0.05). The expression of MMP-9 protein in epithelial ovarian cancer was significantly correlated with FIGO stage (P0.05) and lymph node metastasis (P0.05). However, MMP-9 protein expression was not correlated with different histological classifications (P0.05) and differentiation grade (P0.05). The expression of NF-kappaBp65 protein in epithelial ovarian cancer was significantly correlated with FIGO stage (P0.05), differentiation grade (P0.05) and lymph node metastasis (P0.05). However, NF-kappaBp65 protein expression was not correlated with different histological classifications (P0.05). There was obviously negative correlation between KiSS-1 and MMP-9 expression in ovarian cancer (rs = -0.547, P0.05), as well as between KiSS-1 and NF-kappaBp65 expression in ovarian cancer (rs = -0.414, P0.05), while there was obviously positive correlation between MMP-9 and NF-kappaBp65 expression in ovarian cancer (rs = 0.695, P0.05).The results indicate that KiSS-1 plays some role in suppression of the metastasis of ovarian epithelial cancers, which may be through inhibiting the expression of MMP-9 and NF-kappaBp65.

Quantum correlations are essential for quantum information processing (QIP). Measurement-induced nonlocality (MIN) is a good measure of quantum correlation, and is favored for its conceptual implication and potential application. We investigated here the particular behaviors of the geometric and entropic measures of MIN in the two-qubit Heisenberg XY model and revealed the effects of anisotropic parameter γ and the external magnetic field B on them. Our results showed that both γ and B can serve as efficient controlling parameters for tuning MIN in the XY model.

To investigate the expressions of lysophosphatidic acid (LPA) receptors at both mRNA and protein levels and their biological significance in different human ovarian cancer cell lines.Reverse transcription-polymerase chain reaction (RT-PCR), streptovidin peroxidase-conjugated (SP) immunohistochemical assay and Western blotting were employed to measure the expression levels of LPA(1), LPA(2) and LPA(3) mRNA and LPA(2) and LPA(3) protein in cultured human ovarian cancer cell lines 3AO.SKOV3, and OVCAR3.All the ovarian cancer cell lines expressed LPA(1), LPA(2) and LPA(3) mRNAs and LPA(2) and LPA(3) proteins.LPA(1), LPA(2) and LPA(3) expressions occur extensively in human epithelial ovarian cancer cell lines, and LPA(2) and LPA(3) may be involved in the development and progression of human ovarian cancer.

A series of conformationally restricted dihydro-alkylthio-benzyl- oxopyrimidine (S-DABO) hybrids, which combined the structural features of C6-α-methylbenzyl-thio-DABOs (α-methyl-S-DABOs) and C6-α-cyanobenzyl-thio-DABOs (CN-S-DABOs), has been synthesized and biologically evaluated for their anti-HIV activity against wild-type HIV-1 strain IIIB, double RT mutant (K103N + Y181C) strain RES056 and HIV-2 strain ROD in MT-4 cell cultures. Most of these compounds exhibited inhibitory activity (wild-type) within the range of EC50 values from micromolar to nanomolar. Among them, compound 1s displayed the highest anti-HIV-1 activity with an EC50 value of 91 nM and a selectivity index (SI) of 548, which was more potent than zalcitabine and comparable to nevirapine and delavirdine in the same assay. The HIV-1 reverse transcriptase inhibitory (RT) assay confirmed that these conformationally restricted S-DABO hybrids targeted HIV-1 RT. The preliminary structure-activity relationship (SAR) and molecular docking analysis of this new series of conformationally constrained CN-S-DABO hybrids were also investigated. © 2014 the Partner Organisations. ispartof: Medicinal Chemistry Communications vol:5 issue:4 pages:468-473 status: published

In this paper, we propose a semi-classical theory to successfully explain the polarization flipping in a single frequency laser. An experimental setup is built to verify this theory. The observed experimental phenomena are consistent with the theoretical analysis. We perform phase retardation measurements of birefringent components using this experimental system. The results show that the measurement repeatability is 0.12° and the measurement accuracy is 0.22°.

Two new tetranuclear iron(III) complexes, [Fe4(TBA)4(μ-O)2(μ4-Suc)](ClO4)4(OH)2·1.5CH3CN·2C2H5OH·6H2O (1) and [Fe4(TBA)4(μ-O)2(μ4-Tp)](ClO4)6·3C2H5OH·6H2O (2) (Suc = succinate, Tp = terephthalate, TBA = tris(2-benzimidazolylmethyl)amine) have been prepared and characterized by various physicochemical techniques. X-Ray crystallography reveals complex 1 contains equivalent two μ-oxo-μ-carboxylate diiron(III) centers bridged by a succinate acting as a tetradentate ligand linked to four iron atoms, forming a tetranuclear core [Fe4(TBA)4(O)2(Suc)]6+, in which each iron atom has an N4O2 donor set with distorted octahedral geometry and each of the two diiron(III) centers contains two iron atoms with a distinct coordination environment. Magnetic behaviors indicate the presence of a stongly antiferromagnetic coupling in the two complexes with the exchange coupling constants J = −114.27(8) cm−1 for 1 and J = −119.52(6) cm−1 for 2. The NMR spectra imply that the structures in the solid state are retained in solution. The two tetranuclear complexes exhibit similar cyclic voltammograms, i.e. there are three irreversible two-electron redox peaks at Ec = 0.247, −0.233 V; Ea = 0.354 V for 1 and Ec = 0.307, −0.166 V; Ea = 0.526 V for 2. The preliminary study on the hydrolysis of adenosine 5′-triphosphate (ATP) followed by 31P NMR spectroscopy shows that the two complexes can catalyze the hydrolysis of ATP.