[Effect of Xinling Wan in treatment of stable angina pectoris: a randomized, double-blinded, placebo parallel-controlled, multicenter trial].

To evaluate the effectiveness and safety of Xinling Wan on patients with stable angina pectoris, a randomized, double-blinded, placebo parallel-controlled, multicenter clinical trial was conducted. A total of 232 subjects were enrolled and randomly divided into experiment group and placebo group. The experiment group was treated with Xinling Wan (two pills each time, three times daily) for 4 weeks, and the placebo group was treated with placebo. The effectiveness evaluation showed that Xinling Wan could significantly increase the total duration of treadmill exercise among patients with stable angina pectoris. FAS analysis showed that the difference value of the total exercise duration was between experiment group (72.11±139.32) s and placebo group (31.25±108.32) s. Xinling Wan could remarkably increase the total effective rate of angina pectoris symptom score, and the analysis showed that the total effective rate was 78.95% in experiment group and 42.61% in placebo group. The reduction of nitroglycerin dose was (2.45±2.41) tablets in experiment group and (0.50±2.24) tablets in placebo group on the basis of FAS analysis. The decrease of symptom integral was (4.68±3.49) in experiment group and (3.19±3.31) in placebo group based on FAS analysis. Besides, Xinling Wan could decrease the weekly attack time and the duration of angina pectoris. PPS analysis results were similar to those of FAS analysis. In conclusion, Xinling Wan has an obvious therapeutic effect in treating stable angina pectoris, with a good safety and a low incidence of adverse event and adverse reaction in experiment group.

The mechanism of improved intracellular organic selenium and glutathione contents in selenium-enriched Candida utilis by acid stress.

Batch culture of Candida utilis CCTCC M 209298 for the preparation of selenium (Se)-enriched yeast was carried out under different pH conditions, and maximal intracellular organic Se and glutathione (GSH) contents were obtained in a moderate acid stress environment (pH 3.5). In order to elucidate the physiological mechanism of improved performance of Se-enriched yeast by acid stress, assays of the key enzymes involved in GSH biosynthesis and determinations of energy supply and regeneration were performed. The results indicated that moderate acid stress increased the activity of γ-glutamylcysteine synthetase and the ratios of NADH/NAD+ and ATP/ADP, although no significant changes in intracellular pH were observed. In addition, the molecular mechanism of moderate acid stress favoring the improvement of Se-yeast performance was revealed by comparing whole transcriptomes of yeast cells cultured at pH 3.5 and 5.5. Comparative analysis of RNA-Seq data indicated that 882 genes were significantly up-regulated by moderate acid stress. Functional annotation of the up-regulated genes based on gene ontology and the Kyoto Encyclopedia of Genes and Genome (KEGG) pathway showed that these genes are involved in ATP synthesis and sulfur metabolism, including the biosynthesis of methionine, cysteine, and GSH in yeast cells. Increased intracellular ATP supply and more amounts of sulfur-containing substances in turn contributed to Na2SeO3 assimilation and biotransformation, which ultimately improved the performance of the Se-enriched C. utilis.

Design, synthesis and biological activity evaluation of desloratadine analogues as H1 receptor antagonists.

A series of N-substituted desloratadine analogues were designed and synthesized. They were tested for H1 antihistamine activity by inhibiting histamine-induced contraction of isolated ileum muscles of guinea-pigs in vitro and inhibiting histamine-induced asthmatic reaction in guinea-pigs in vivo. All the evaluated compounds exhibited significant antihistamine activity compared with desloratadine. Five active compounds induced no sedative effects on mouse and four of them exhibited lower anticholinergic side effects than desloratadine. Among these analogues, compound 10, (1S,4S)-4-chlorocyclohexyl desloratadine displayed the highest activity and best safety profile. And it was believed to be a potential candidate as the 3rd generation antihistamine.

Synthesis and antihistamine evaluations of novel loratadine analogues.

A series of loratadine analogues containing hydroxyl group and chiral center were synthesized. The effect of the synthesized compounds on the histamine-induced contractions of guinea-pig ileum muscles was studied. In addition, the in vivo asthma-relieving effect of the analogues in the histamine induced asthmatic reaction in guinea-pigs was determined. Most of the compounds exhibited definite H(1) antihistamine activity. The S-enantiomers, compounds 2, 4 and 8, are more potent than the R-enantiomers, compounds 1, 3 and 7. Compound 6 was the most active one among the eight synthesized compounds.

Diagnostic and Prognostic Value of TAT, PIC, TM, and t-PAIC in Malignant Tumor Patients With Venous Thrombosis.

BACKGROUND: Venous thromboembolism (VTE) is an important complication in patients with malignant tumors. Its exact diagnosis and treatment are still lacking. We used a high-sensitive chemiluminescence method to detect thrombin-antithrombin III complex (TAT), plasmin-α2-plasmininhibitor complex (PIC), thrombomodulin (TM), and tissue plasminogen activator-inhibitor complex(t-PAIC) in combination with D-dimer and fibrin degradation product (FDP) to analyze their diagnostic and prognostic value in patients with malignant tumors. METHODS: In total, 870 patients with confirmed malignant tumors were included, 82 of whom had diagnosed VTE; 200 healthy individuals were classified as the control group. The TAT, PIC, TM, and t-PAIC were detected using Sysmex HISCL5000 automated analyzers, whereas FDP and D-dimer were detected using Sysmex CS5100 coagulation analyzer. Receiver operating characteristic (ROC) curves were used to evaluate the diagnostic efficiency. Survival probabilities were determined using Kaplan-Meier analysis, and multivariate analyses were performed using a Cox regression model. RESULTS: Compared with healthy controls, patients with malignant tumors showed significantly elevated TAT, PIC, TM, t-PAIC, D-dimer, and FDP. Similarly, compared with patients in the non-thrombosis group, those in the thrombosis group showed significantly elevated levels of the above mentioned markers. Logistic regression analysis showed that TAT, PIC, TM, t-PAIC, D-Dimer, and FDP were all associated with VTE. ROC analysis showed that "TAT+PIC+TM+t-PAIC+D-dimer+FDP"showed the highest sensitivity and specificity. Patients with elevated TAT, PIC, TM, and t-PAIC had a significantly shorter survival. Multivariate Cox survival analysis showed that TM and t-PAIC were significantly associated with poor prognosis. In addition, the incidence of VTE was significantly lower in patients with malignant tumors who were treated with low-molecular-weight heparin (LMWH), and their survival period was significantly longer than that of patients with malignant tumors who were not treated with LMWH. CONCLUSION: TAT, PIC, TM, and t-PAIC combined with D-dimer and FDP were better than the application of a single marker in the diagnosis of VTE in patients with malignant tumors. TAT and PIC can be used as sensitive markers in the diagnosis of VTE but not as prognostic markers. TM and t-PAIC might be independent prognostic indicators in patients with malignant tumors, regardless of the state of thrombus.

Diagnostic value of contrast-enhanced ultrasound in papillary thyroid microcarcinoma.

The aim of the present study was to explore the value and characteristics of contrast-enhanced ultrasound (CEUS) in the diagnosis of papillary thyroid microcarcinoma (PTMC). By analyzing CEUS information of 130 nodules obtained from 106 patients with PTMC, who had been diagnosed by surgery and pathological analysis, CEUS characteristics of PTMC nodules were concluded. Based on the results, the PTMC nodules were divided into three groups as follows: 32 nodules (24.62%) were found to be enhanced earlier than the surrounding normal thyroid tissue, 95 nodules (73.08%) were enhanced at the same time as the normal thyroid tissue and 3 nodules (2.30%) were enhanced later than the normal thyroid tissue. The results also demonstrated that the peak enhancement intensity of the 130 nodules was lower compared with the irregular intensity of the normal parenchyma in corresponding thyroids, and that PTMC enhancement washed out faster than in normal thyroid parenchyma. In conclusion, the PTMC characteristics that CEUS can detect may improve the diagnostic accuracy and provide valuable information for the treatment of the disease.

Design, synthesis and antihistamine evaluations of several N-hydroxyalkyl desloratadine analogues.

Several N-hydroxyalkyl desloratadines and N-methoxyl ethyl desloratadine were prepared and evaluated for H1 antihistamine activity. The effects on isolated ileum smooth muscle tension in guinea pigs in vitro and asthma-relieving effects on the histamine-induced asthmatic reaction in guinea-pigs in vivo were examined. Most of them exhibited satisfactory H1 antihistamine activity and were obviously more potent than loratadine. Among these, Compound 3, N-(3-hydroxy)propyl desloratadine was the most active one. And it was chosen as a candidate for evaluation of acute toxicity (LD(50)= 0.876(0.784-0.980) g/kg), significantly superior to that of desloratadine (LD(50)=0.353 g/kg). Meanwhile, the experimental results demonstrated that the oxygen atom in the side carbon chain is crucial for enhancing the antihistamine activities.

Avoiding Loss of Catalytic Activity of Pd Nanoparticles Partially Embedded in Nanoditches in SiC Nanowires.

Nanoditches from selective etching of periodically twinned SiC nanowires were employed to hinder the migration and coalescence of Pd nanoparticles supported on the nanowires, and thus to improve their catalytic stability for total combustion of methane. The results show that the etched Pd/SiC catalyst can keep the methane conversion of almost 100% while the unetched one has an obvious decline in the catalytic activity from 100 to 82% after ten repeated reaction cycles. The excellent catalytic stability originates from the limitation of the nanoditches to the migration and growth of Pd nanoparticles.

Spectrofluorimetric determination of trace nitrite with a novel fluorescent probe.

A simple, sensitive and selective fluorimetric determination for trace nitrites was developed using an unsymmetrical rhodamine with a high fluorescence quantum yield and large Stokes shift. The method is based on the reaction of the unsymmetrical rhodamine with nitrite in an acidic medium to form a nitroso product, which has much lower fluorescence because the electron-withdrawing effect of the nitroso group influences the system of p-pi conjugation between N atom and benzene ring. Under optimum conditions, the fluorescence quenching intensity is linear over a nitrite concentration range of 1.0 x 10(-8) to 3.5 x 10(-7)M. The detection limit is 2.0 x 10(-10)M (S/N=3). The method was applied to the determination of nitrite in tap water and lake water with satisfactory results. The mechanism for the reaction is also reported.

Periodically twinned SiC nanowires.

Twinning has been recognized to be an important microstructural defect in nanoscale materials. Periodically twinned SiC nanowires were largely synthesized by the carbothermal reduction of a carbonaceous silica xerogel prepared from tetraethoxysilane and biphenyl with iron nitrate as an additive. The twinned ß-SiC nanowires, with a hexagonal cross section, a diameter of 50-300 nm and a length of tens to hundreds of micrometers, feature a zigzag arrangement of periodically twinned segments with a rather uniform thickness along the entire growth length. Computer simulation has been used to generate three-dimensional atomic structures of the zigzag columnar twin structure by the stacking of hexagonal discs of {111} planes of SiC. A minimum surface energy and strain energy argument is proposed to explain the formation of periodic twins in the SiC nanowires. The thickness of the periodic twinned segments is found to be linearly proportional to the nanowire diameter, and a constant volume model is proposed to explain the relation.

[The role of ERK1/2 in leptin promoting the proliferation of human endometrial cancer cell line Ishikawa].

BACKGROUND & OBJECTIVE: Epidemiologic studies showed that leptin is closely related to the tumorigenesis of endometrial cancer, but the mechanism is unclear. As a mitogenic agent, leptin can promote the proliferation of many kinds of cells. This study was to explore the role of extracellular signal-regulated kinase 1/2 (ERK1/2) in leptin promoting the proliferation of human endometrial cancer cell line Ishikawa. METHODS: The expression of leptin receptor OB-Rb in Ishikawa cells was detected by fluoroimmunoassay. Ishikawa cells were treated by leptin at various concentrations (0, 10, 50, 100, and 150 ng/ml) for different time (6, 12, and 24 h). Cell proliferation was examined by MTT assay. Meanwhile, the effect of PD98059, selective inhibitor of ERK1/2, on the proliferation of Ishikawa cells induced by leptin was also studied. Ishikawa cells were treated with 100 ng/ml leptin for different time (20, 40, and 60 min), then the levels of phosphorylated ERK1/2 (p-ERK1/2) and ERK1/2 were examined by Western blot. RESULTS: Fluoroimmunoassay showed the presence of OB-Rb in Ishikawa cells. Leptin stimulated the proliferation of Ishikawa cells. This effect was maximal at 100 ng/ml after 24-hour treatment, and there was no significant difference between 100 ng/ml group and 150 ng/ml group (P=0.129). Blocking ERK1/2 phosphorylation by PD98059 significantly reduced the proliferation of Ishikawa cells stimulated by leptin. When treated with 100 ng/ml Leptin and 100 micromol/L PD98059 for 24 h, cell proliferation rate was (6.88+/-0.86)%. ERK1/2 phosphorylation was enhanced significantly in Ishikawa cells after treatment of 100 ng/ml leptin. CONCLUSION: Leptin may promote the proliferation of endometrial cancer Ishikawa cells by activating ERK1/2 signaling pathway.