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When infected by Helicobacter pylori, it often causes gastritis, gastric ulcer, or gastric cancer. Antibiotics are used to treat H. pylori infection, as they inhibit or kill H. pylori often ex-tending to reduce the incidences of gastric adenoma and cancer. However, H. pylori has developed drug resistance to many clinically used antibiotics over the years, thereby providing no warranty of successful treatment whenever H. pylori infection befalls. We report here that fucoidan from Sargassumhemiphyllum can effectively reduce infection of H. pylori without development of drug resistance. Fucoidan demonstrated a strong anti-inflammation activity in RAW264.7 cell model. Using AGS cell model, fucoidan decreased H. pylori adhesion to host cells and thus reduced its infection rate, especially in post-treatment where the infection rate was reduced to 40%. Mechanistically, fucoidan intervenes the proper functions of adhesion molecules BabA and AlpA of H. pylori. Moreover, fucoidan is able to significantly lower the total count of H. pylori and the levels of IL-6 and TNF-α in vivo. Added together, these convergent results suggest that fucoidan is an effective agent in a position to protect stomach from H. pylori infection by reducing its total count and induced inflammation.

The purpose of this work was to study and further clarify the anti-wear and anti-friction mechanism of ultrafine SiO2/MoS2 powders in the complex calcium sulfonate grease. In this paper, 15nm nanoSiO2, 1μm MoS2 and commercial NLGI Grade No.2 complex calcium sulfonate grease were used as the research objects, SEM, EDS and XPS were used to study the morphology, composition and film chemical constitution of the long friction wear spots of grease containing single nanoSiO2 powder, ultrafine MoS2 powder and the two compound powders, which formed in the process of four ball long friction. The results show that nanoSiO the grease plays a role in filling the undercut, ball bearings and polishing and forming high hardness Ca3Fe2(SiO4)3 and part of Fe2O3 anti-wear films in the process of long friction. The ultrafine MoS2 powder has a self-repairing effect to fill the grooves,forming the MoS2, MoO3 anti-friction films and Fe2(SO4)3 anti-wear film. The two powders in the composite grease have a synergistic effect, acting on the friction pair together, and simultaneously forming self-repairing anti-friction and anti-wear films, thereby further improving the tribological performance of the base grease.

For the development of complex calcium sulfonate grease containing ultrafine SiO2/MoS2 powders with self-reparing performance. On the basis of the dispersion of the nanoSiO2 particles, the effects of particle size,addition amount,load and the mass ratio of nanoSiO2 to ultrafine MoS2 powders on the tribological properties of commercial No.2 complex calcium sulfonate grease were systematically studied by four ball friction and wear tester. The results show that suitable particle size and addition amount of single SiO2 and MoS2 powders can significantly reduce the coefficient of friction (COF) and the wear scar diameter (WSD) of the grease. The composite of nanoSiO2 and MoS2 powder can broaden the load range of base grease and further improve the tribological properties of complex calcium sulfonate grease. When the mass ratio of nanoSiO2 powder to MoS2 powder is 3:7 and the total addition amount is 0.8wt%, the COF and the WSD of the grease are decreased by 53.64% and 27.08%, respectively, compared with the base grease. The two powders in the composite grease have synergy effect for improving the tribological performance and the friction stability of the grease during the process of long friction.

The globo-series glycosphingolipids (GSLs) SSEA3, SSEA4, and Globo-H specifically expressed on cancer cells are found to correlate with tumor progression and metastasis, but the functional roles of these GSLs and the key enzyme β1,3-galactosyltransferase V (β3GalT5) that converts Gb4 to SSEA3 remain largely unclear. Here we show that the expression of β3GalT5 significantly correlates with tumor progression and poor survival in patients, and the globo-series GSLs in breast cancer cells form a complex in membrane lipid raft with caveolin-1 (CAV1) and focal adhesion kinase (FAK) which then interact with AKT and receptor-interacting protein kinase (RIP), respectively. Knockdown of β3GalT5 disrupts the complex and induces apoptosis through dissociation of RIP from the complex to interact with the Fas death domain (FADD) and trigger the Fas-dependent pathway. This finding provides a link between SSEA3/SSEA4/Globo-H and the FAK/CAV1/AKT/RIP complex in tumor progression and apoptosis and suggests a direction for the treatment of breast cancer, as demonstrated by the combined use of antibodies against Globo-H and SSEA4.

Atopic dermatitis (AD) is a long-term allergic skin disorder that occurs most frequently in children. Currently, the common treatment of AD is corticosteroids; however, the drugs cause serious side effects. Therefore, there are many patients who seek complementary and alternative treatments such as healthy food. We report that fucoidan from Cladosiphon okamuranus (COP) exhibit exceptional immuno-modulatory effects significantly improving atopic dermatitis (AD) at both in vitro and in vivo levels: First, we performed the P815 cell degranulation assay, of which the results revealed that COP possesses anti-degranulation activity suggesting COP is very conducive to relieving allergic reactions of AD. Next, we performed the animal model examination, of which AD was significantly improved, suggesting COP can focally and globally modulate the immune systems of animals. The systemic improvements were manifested clearly by decreased epidermal hyperplasia, reduced infiltration of eosinophils, and decreased expression of AD-associated cytokines. Notably, COP reduced epidermal hyperplasia by downregulating the expression of IL-22. COP displayed therapeutic effects, which is comparable to corticosteroids but lack corticosteroid side effects, such as weight loss in our animal study. COP is multitudinous immunomodulatory abilities to serve as a healthy food supplement at the current stage, not least beneficial to atopic dermatitis.

Aberrant composition of glycans in the tumor microenvironment (TME) and abnormal expression of extracellular matrix proteins are hallmarks of hepatocellular carcinoma (HCC), however, the mechanisms responsible for establishing the TME remain unclear. We demonstrate that the chondroitin polymerizing factor (CHPF), an enzyme that mediates the elongation of chondroitin sulfate (CS), is a critical elicitor of the malignant characteristics of HCC as it modifies the potent tumor suppressor, decorin (DCN). CHPF expression is frequently downregulated in HCC tumors, which is associated with the poor overall survival of HCC patients. We observed that restoring CHPF expression suppressed HCC cell growth, migration, and invasion in vitro and in vivo. Mechanistic investigations revealed that TGF-β signaling is associated with CHPF-induced phenotype changes. We found that DCN, as a TGF-β regulator, is modified by CHPF, and that it affects the distribution of DCN on the surface of HCC cells. Importantly, our results confirm that CHPF and DCN expression levels are positively correlated in primary HCC tissues. Taken together, our results suggest that CHPF dysregulation contributes to the malignancy of HCC cells, and our study provides novel insights into the significance of CS, which affects DCN expression in the TME.

This study was aimed to develop a simple, fast, and reliable technique to detect fluoroquinolones (FQs)-conjugated bovine serum albumin (BSA). Four tested FQs, enrofloxacin, ofloxacin, danofloxacin, and orbifloxacin, were conjugated with BSA by following the N-hydroxysuccinimide ester method. The technique was designed according to the different absorption characteristics of the FQs and BSA; FQs can be detected by both UV and fluorescence detectors, but BSA can only be detected by UV. The results demonstrated that the developed method was efficient in detecting FQs-BSA conjugates. In addition, the method not only trace the FQs and BSA conjugation responses but also can be used to estimate the level of FQs-BSA conjugation. Therefore, this technique is a valuable tool for the detection drug-carrier-conjugated antigens, especially for FQs-BSA-conjugates during the production of anti-FQs monoclonal antibodies.

We analyzed the residual of oxolinic acid in the serum and muscle of the Chinese mitten crab by high-performance liquid chromatography (HPLC) coupled with a fluorescence detector. A standard solution of oxolinic acid was prepared by dilution with 0.05 M phosphate buffered saline (PBS) (pH 7.4). Serum and muscle samples were completely homogenized prior to addition of oxolinic acid. Samples were then transferred into an ultrasonic water bath and centrifuged. The supernatants of serum and water layer of hexane defatted muscle were passed through C-18 solid phase extraction columns. Finally, oxolinic acid in the column was eluted with methanol/NH4OH (75:25 v/v), and then was evaporated to dry by nitrogen gas. Extracted oxolinic acid was determined by HPLC with a fluorescence detector (excitation/emission=335 nm/378 nm) and a Cosmosil 5C18-MS reverse phase column (5 μm, 4.6×150 mm i.d.). A mixture of acetonitrile and 0.02 M PBS pH 3.0 (25:75) was used as the mobile phase at a flow rate of 1.0 mL/min. A peak with retention time around 8 min was observed. With the addition of 100 μg L^(-1) oxolinic acid treatments, the mean recoveries from serum and muscle were 92% and 82%, respectively. The detection limit was 1 ppb and standard curves spiked at different levels showed a good linear correlation coefficient (R(superscript 2)＞0.999 for oxolinic acid). Because residual oxolinic acid could not be detected in all tested crabs initially, five crabs were fed with oxolinic acid for 7 days by oral administration on purpose and the residual oxolinic acid in both sera and muscle were measured, respectively. The results showed that the residual oxoilinic acid in both sera and muscle could be quantified by this method. Therefore, our developed technique may be employed as a practical method for detection of residual oxolinic acid residue in Chinese mitten crabs or other aquaculture products.

A method of high-heating-rate thermal reduction is used to produce porous graphene nanosheets (PGNSs). This material is characterized by a unique holey structure, which is suitable for ionic liquid (IL) electrolyte. To study the effects of electrolyte anion, 1-ethyl-3-methylimidazolium bis(trifluoromethylsulfony)imide (EMI-TFSI) and 1-ethyl-3-methylimidazolium bis(fluorosulfonyl)imide (EMI-FSI) ILs are used. Due to the smaller size of FSI−, EMI-FSI shows a higher conductivity and lower viscosity than those of EMI-TFSI. The specific capacitances of PGNS electrodes are 90 and 260 F g−1, respectively, measured in EMI-TFSI and EMI-FSI ILs at a potential scan rate of 50 mV s−1. The PGNS symmetric cell with EMI-FSI electrolyte is able to deliver a maximum energy and power densities of 110 Wh kg−1 and 101 kW kg−1, respectively, with a cell voltage of 3.5 V. In addition, 85% of the initial capacity can be retained after 2000 charge–discharge cycles.

Quantum dots (QDs) are used in the bio-medical area because of their excellent optical properties. Their biomedical utilization has remained a serious biosecurity concern. Cytotoxicity experiments have shown that QD toxicity is connected to the properties of the QDs. In this paper, the toxicity of QDs was studied from the aspect of surface functional groups at the mitochondrial level. Three types of ligands, thioglycollic acid (TGA), mercaptoethylamine (MEA) and l-cysteine (l-Cys), which have similar structures but different functional groups were used to coat CdTe QDs. The effects of the three types of CdTe QDs on mitochondria were then observed. The experimental results showed the three types of CdTe QDs could impair mitochondrial respiration, destroy membrane potential and induce mitochondrial swelling. Interestingly, MEA-CdTe QDs showed similar effects on membrane potential and mitochondrial swelling as did l-Cys-CdTe QDs, while TGA-CdTe QDs showed stronger effects than that of the two other QDs. Moreover, the three types of CdTe QDs showed significantly different effects on mitochondrial membrane fluidity. MEA-CdTe QDs decreased mitochondrial membrane fluidity, l-Cys-CdTe QDs showed no obvious influence on mitochondrial membrane fluidity and TGA-CdTe QDs increased mitochondrial membrane fluidity. The interaction mechanism of CdTe QDs on mitochondrial permeability transition (MPT) pores as well as Cd(2+) release by CdTe QDs were checked to determine the reason for their different effects on mitochondria. The results showed that the impact of the three types of CdTe QDs on mitochondria was not only related to the released metal ion, but also to their interaction with MPT pore proteins. This work emphasizes the importance of surface functional groups in the behavior of CdTe QDs at the sub-cellular level.

Atopic dermatitis (AD) is a T helper (Th) 2 cell-mediated allergic disease, which features increased number of immunocytes and level of Th2-associated cytokines. Fucoidan is well known a naturally occurring agent effectively ameliorating many AD symptoms. Though these alleviative effects are exhilarating, the mechanisms behind, however, are still rather limited. In this study, we report that fucoidan derived from Cladosiphon okamuranus (FT) inhibits nitric oxide (NO) production by exerting its anti-inflammatory ability. Topical application on animals show that FT promotes skin repair, reduces immunocyte proliferation, and decreases serum IgE level. In histological analysis, FT favorably reduces epidermal hyperplasia and eosinophilic infiltration. The pharmacodynamics mechanism of FT is determined by means of down-regulating AD-associated cytokines (IL-4, IL-5, IL-22, IL-33, and TSLP) and up-regulating TGF-β1 level. Moreover, FT can regulate systemic immunity by enhancing tolerogenic dendritic cells (Tol-DCs) to activate regulatory T cells (Treg) differentiation and to decrease the population of Th22 and memory B cells. Overall, topical application of FT is able to enhance Treg secreting TGF-β1 and to down-regulate Th2 cell-mediated immunity so that AD symptoms are significantly alleviated. Thereby, FT is an ideal drug candidate potentially replacing or complementing corticosteroids to be developed and used as a therapeutic agent to treat AD.

The potential toxicity of Quantum dots (QDs) should be assessed comprehensively for their fast spreading applications. Many studies have shown the toxicity of QDs is associated with their surface ligands. In this work, two analog ligands with one carbon difference, 2-mercaptoacetic acid (TGA) and 3-mercaptopropionic acid (MPA) were used as coating materials in the syntheses of two types of CdTe QDs with similar physicochemical properties. Then the biological effects of QDs on isolated mitochondria were studied. It was found that the two types of QDs could impair mitochondrial respiration and induce mitochondrial permeability transition (MPT). However, as compared with TGA-CdTe QDs, MPA-CdTe QDs had a stronger effect on MPT. The weaker effect of TGA-CdTe QDs on MPT might be owing to their better stability and thus less amount of released Cd2+, which could be further explained by the stronger affinity between the ligand (TGA) and the cadmium complexes in the crystal growth of QDs. These results highlighted the importance of ligands responsible for the toxicity of QDs at the sub-cellular level.

PT-peptide is derived from the anti-lipopolysaccharide factor of the swimming crab Portunus trituberculatus. The peptide, consisting of 34 amino acids, contains a lipopolysaccharide binding domain. In this study, we investigated the effect of PT-peptide encapsulated in raw milk-derived extracellular vesicles (EVs), designated as EVs-PT peptide, on immune regulation. The results showed that raw milk-derived EVs efficaciously delivered the PT-peptide into monocytes and elevated immune activity, including reactive oxygen species level, superoxide anion production, and phagocytosis. PT-peptide and EVs-PT peptide also elevated the secretion of cytokines, such as interferon-&gamma, interleukin-6, and tumor necrosis factor-&alpha, in human monocytic THP-1 cells. These results suggest that the PT-peptide could be developed as an immune stimulator.

The hyperactivity of the lateral habenula (LHb) is closely associated with depression. At present, it is unknown how GABA transporter (GAT) in the LHb affects depressive-like behaviors, particularly in Parkinson's disease (PD)-related depression. In this study, unilateral 6-hydroxydopamine lesions of the substantia nigra pars compacta (SNc) in rats induced depressive-like behaviors and led to hyperactivity of LHb neurons compared to sham-lesioned rats. Intra-LHb injection of GAT-1 inhibitor NO-711 produced antidepressant-like responses, decreased firing rate of LHb neurons, and increased levels of LHb extracellular GABA in sham-lesioned and the lesioned rats. Further, the dose producing behavioral effects in the lesioned rats was lower than that of sham-lesioned rats. In the lesioned rats, the duration of inhibitory effect on the firing rate and increased levels of the GABA induced by NO-711 was longer than those in sham-lesioned rats, respectively. Intra-LHb injection of GAT-3 inhibitor SNAP-5114 improved depressive-like behaviors and decreased firing rate of LHb neurons in the lesioned rats, but not in sham-lesioned rats. SNAP-5114 increased LHb GABA levels in the lesioned rats, whereas did not alter that in sham-lesioned rats. These changes were involved in the down-regulated expression of LHb GAT-1 and GAT-3 after lesioning the SNc. These findings suggest that GAT-1 plays a major role in transporting LHb GABA under physiological conditions, and depletion of dopamine increases the transport capacity of GAT-3 in the LHb. Further, the study provides evidence that GAT-1 and GAT-3 in the LHb are involved in the regulation of PD-related depression.

2-Benzylisoquinolin-1(2H)-ones has been proposed as vasodilative agents on the basis of scaffold hopping. In the present study, a series of 2-benzylisoquinolin-1(2H)-ones were synthesized. Their vasodilative effects were evaluated by wire myograph on isolated rat mesenteric arterial ring induced contraction with 60mM KCl. The structure-activity relationships of target compounds were discussed. Among these compounds, C7 and C8 displayed potent vasodilative effects and significantly inhibited the contraction of rat mesenteric arterial rings induced by phenylephrine. The antihypertensive effects of compounds C7 and C8 on SHR were further evaluated. The results indicated that oral administrational C7 and C8 can significantly reduce both diastolic and systolic blood pressure in a dose-dependent manner. Moreover, C7 maintained the effects for 4h at a dosage of 4.0mg/kg. These findings suggest that the title compounds can serve as novel vasodilative agents and promising antihypertensive agents.

Bioactive glass (BG) was made by the sol&ndash, gel method and doped with boron (B) to increase its bioactivity. Microstructures of BG and B-doped BG were observed by scanning electron microscopy, and phase identification was performed using an X-ray diffraction diffractometer. The ion concentrations released after soaking in simulated body fluid (SBF) for 1, 4, and 7 days were measured by inductively coupled plasma mass spectrometry, and the pH value of the SBF was measured after soaking samples to determine the variation in the environment. Brunauer&ndash, Emmett&ndash, Teller (BET) analysis was performed to further verify the characteristics of mesoporous structures. High performance liquid chromatography was used to evaluate the drug delivery ability of teicoplanin. Results demonstrated that B-doped BG performed significantly better than BG in parameters assessed by the BET analysis. B-doped BG has nanopores and more rough structures, which is advantageous for drug delivery as there are more porous structures available for drug adsorption. Moreover, B-doped BG was shown to be effective for keeping pH values stable and releasing B ions during soaking in SBF. The cumulative release of teicoplanin from BG and B-doped BG reached 20.09% and 3.17% on the first day, respectively. The drug release gradually slowed, reaching 29.43% and 4.83% after 7 days, respectively. The results demonstrate that the proposed bioactive glass has potential as a drug delivery system.

In the present study, a series of m-(4-morpholinoquinazolin-2-yl)benzamides were designed, synthesized and characterized. The antiproliferative activities of the synthesized compounds were evaluated against two human cell lines (HCT-116 and MCF-7). Compounds with IC50 values below 4 μM were further evaluated against U-87 MG and A549 cell lines. Among these evaluated compounds, compound T10 displayed a remarkable antiproliferative effect in vitro. The hoechst staining assay showed that compound T10 caused morphological changes. The cell cycle and apoptosis assay further indicated that compound T10 can arrest HCT-116 cells in G2/M and G0/G1 phase and induce apoptosis. PI3K enzyme assays indicated that compounds T7 and T10 selectively inhibit PI3Kα. A Western bolt assay further suggested that compound T10 can block the PI3K/Akt/mTOR pathway. Moreover, compound T10 inhibited tumor growth on a mice S180 homograft model. These findings directly identify m-(4-morpholinoquinazolin-2-yl)benzamide derivatives as novel anticancer agents.

Mitochondrial function is applied as oxidative stress and neuronal damage index. In this study, d-galactose was used to induce free radicals production and neuronal damage in HN-h cells, and the effect of novel 43 kDa protein isolated from oyster on anti-mitochondrial dysfunction and zinc-binding ability were evaluated. Crystal violet stain results indicated zinc-binding protein of oyster (ZPO) attenuated neuronal cell death induced by 100 mM of d-galactose on HN-h cells in a dose-dependent manner. ZPO alleviated mitochondrial inactivation, mitochondrial membrane potential decreasing, oxidative stress, and fusion/fission state in non-cytotoxic concentration of d-galactose (50 mM)-treated HN-h cells. ZPO treatment recovered metallathionein-3 (MT-3) decrease and inhibited β- and γ-secretase as well as amyloid beta (Aβ) accumulation in HN-h cells caused by d-galactose induction. These results suggest ZPO could avoid oxidative stress and is a functional protein for zinc concentration maintainability, which has potential for development of functional foods for neuronal protection.

Six 2-(2-acylaminobenzothiazol-6-yl)isoquinoline-1,3(2H,4H)-diones (1a–1f) and five 2-arylisoquinoline-1,3(2H,4H)-diones (1g–1k) were synthesized by refluxing homophthalic anhydrides with 2-acylaminobenzothiazolyl-6-amine or substituted aniline in glacial acetic acid. The cytotoxic activities of 1a–1k were evaluated via MTT method against A431, A549, and PC3. Compound 1b relatively displayed a higher cytotoxic activity than the others. The antitumor effect of 1b were evaluated in established nude mice PANC-1 xenograft model. The results suggest that compound 1b could potentially inhibit tumor growth.

The silicon-wire, surrounded by bimetallic layers of silver and gold, demonstrates surface plasmon interference with TM/TE enhanced sensitivity of 2873-nm per refractive-index-unit, 6 times and 15% better than the top gold film and an additional silicon layer embedded in silicon, respectively.

A magnetically separable photocatalyst silver vanadates@SiO2/Fe3O4 was prepared by hydrothermal process. The prepared sample was composed of mixed phases of a–Ag3VO4 and Ag4V2O4, and the main phase was a–Ag3VO4. The bandgap of the synthesized sample was 2.2 eV. In the degradation of methyl orange (MO) solution under the visible light (l>420 nm), the silver vanadates@SiO2/Fe3O4 showed high photocatalytic activity in two-cycle photocatalytic test.

A new approach to the benzo[a]quinolizidine alkaloid was described. Total synthesis of (±)-protoemetinol (1) was reported.

A convenient method for the preparation of 4- or 5-substituted 3-sulfonyl-δ-lactams via regioselective reduction of N-alkyl-3-sulfonyl glutarimides is described. Formal synthesis of (±)-paroxetine and (±)-tacamonine is also reported.

A formal synthesis of (±)-isodihydronepetalactone (1) from cyclobutenone 5 was de scribed. Baeyer-Villiger lactonization of cyclobutanone 8 followed by decholorination led to lactone 4, which under went a series of functional group trans formations, furnished cyclopentanone derivative 15. Shapiro reaction on hydrazone derivative in the presence of excess dry ice gave lactone 2. Lactone 2 had previously been converted to isodihydronepetalactone (1).

NO production catalysed by eNOS (endothelial nitric-oxide synthase) plays an important role in the cardiovascular system. A variety of agonists activate eNOS through the Ser1177 phosphorylation concomitant with Thr495 dephosphorylation, resulting in increased ·NO production with a basal level of calcium. To date, the underlying mechanism remains unclear. We have previously demonstrated that perturbation of the AIE (autoinhibitory element) in the FMN-binding subdomain can also lead to eNOS activation with a basal level of calcium, implying that the AIE might regulate eNOS activation through modulating phosphorylation at Thr495 and Ser1177. Here we generated stable clones in HEK-293 (human embryonic kidney 293) cells with a series of deletion mutants in both the AIE (Δ594–604, Δ605–612 and Δ626–634) and the C-terminal tail (Δ14; deletion of 1164–1177). The expression of Δ594–604 and Δ605–612 mutants in non-stimulated HEK-293 cells substantially increased nitrate/nitrite release into the culture medium; the other two mutants, Δ626–634 and Δ1164–1177, displayed no significant difference when compared with WTeNOS (wild-type eNOS). Intriguingly, mutant Δ594–604 showed close correlation between Ser1177 phosphorylation and Thr495 dephosphorylation, and NO production. Our results have indicated that N-terminal portion of AIE (residues 594–604) regulates eNOS activity through coordinated phosphorylation on Ser1177 and Thr495., Our findings demonstrate for the first time that AIE insert exerts its regulatory function by coordinate phosphorylation on eNOS Ser1177 and Thr495, highlighting the importance of AIE in regulating agonist-induced eNOS activation.

A formal [3+3] cycloaddition strategy to substituted glutarimides was studied. N -Benzyl α-sulfonylacetamides and various α,β-unsaturated esters were used as starting materials.

2-Aryl-8-hydroxy (or methoxy)-isoquinolin-1(2H)-one has been proposed as a novel scaffold of EGFR inhibitor based on scaffold hoping. In the present study, a series of 2-aryl-8-hydroxy (or methoxy)-isoquinolin-1(2H)-one derivatives were synthesized. Their antiproliferative activities in vitro were evaluated via MTT assay against two human cancer cell lines, including A431 and A549. The SAR of the title compounds was preliminarily discussed. The compounds with ideal inhibition were evaluated through ELISA-based EGFR-TK assay. Compound 6c showed the best activity against A431 and EGFR tyrosine kinase. These findings suggest that title compounds are EGFR inhibitors with novel structures.

Electroluminescence (EL) is observed from the Au/Si-rich SiO2 film/p-Si diodes, in which the Si-rich SiO2 films are scored deliberately by a diamond tip. The EL intensity of the scored diode annealed at 800 degreesC is about 6 times of that of the unscored counterpart. The EL spectrum of the unscored diode could be decomposed into two Gaussian luminescence bands with peaks at about 1.83 and 2.23eV, while for the EL spectrum of the scored diode, an additional Gaussian band at about 3.0eV appears, and the 1.83-eV peak increases significantly in intensity. The photoluminescence (PL) spectrum of an unscored Si-rich SiO2 film has only one band peaking at about 1.48eV, whereas the PL spectrum of the scored one has two bands at about 1.48 and 1.97eV. We consider that the high-density defect regions produced by the scoring provide new luminescence centres and become some types of nonradiative centres in the Si oxide layer, which thus result in changes of the EL and PL spectra.

An anisotropic EPR signal was observed in porous Si. According to its symmetry andg value, the EPR signal can be attributed to silicon dangling bonds located on the surface of a porous Si skeleton. The evolution of the EPR signal at room temperature in air was measured. The annealing temperature dependence of the EPR and the PL of porous Si in oxygen and the effects of gamma irradiation on the EPR and the PL spectra of porous Si were studied. The changes of the EPR signal and the PL intensity induced in atmosphere by ethyl alcohol and acetone were discovered. The dangling bond is only one of the factors which affect the PL.

Treatment of N-alkyl-3-sulfonyl glutarimides (1) with sodium hydride and then lithium aluminum hydride could give regioselective reduced hydroxy piperidones (5) which were further dehydrated to 3,4-dihydro-3-tosylpyridin-2-ones (6) in the presence of boron trifluoride.

γ-Substituted α,β-unsaturated δ-lactams 1 was synthesized from α-sulfinyl acetamides 3 in three steps. Formal synthesis of (±)-protoemetinol was also reported.

Treatment of N-alkyl-3-sulfonyl glutarimides (1) with sodium hydride and then lithium aluminum hydride could give regioselective reduced hydroxy piperidones (5) which were further dehydrated to 3,4-dihydro-3-tosylpyridin-2-ones (6) in the presence of boron trifluoride.

γ-Substituted α,β-unsaturated δ-lactams 1 was synthesized from α-sulfinyl acetamides 3 in three steps. Formal synthesis of (±)-protoemetinol was also reported.

Recent studies have shown that use of nonsteroidal anti-inflammatory drugs (NSAIDs) is associated with an increased risk of myocardial infarction. To explore whether NSAIDs may induce endothelial apoptosis and thereby enhance atherothrombosis, we treated human umbilical vein endothelial cells (HUVECs) with sulindac sulfide (SUL), indomethacin (IND), aspirin (ASA), or sodium salicylate (NaS), and we analyzed apoptosis. SUL and/or IND significantly increased annexin V-positive cells, cleaved poly(ADP-ribose) polymerase (PARP) and caspase-3. ASA and NaS at 1 mM did not induce PARP cleavage or caspase-3 and at 5 mM, ASA but not NaS increased apoptosis. Because peroxisome proliferator-activated receptor delta-mediated 14-3-3epsilon up-regulation was reported to play a crucial role in protecting against apoptosis, we determined whether NSAIDs suppress this transcriptional pathway. SUL, IND, and ASA (5 mM) suppressed PPARdelta and 14-3-3 proteins in a manner parallel to PARP cleavage. Neither ASA nor NaS at 1 mM interfered with PPARdelta or 14-3-3epsilon expression. SUL inhibited PPARdelta promoter activity, which correlated with 14-3-3epsilon promoter suppression. Suppression of 14-3-3epsilon was associated with increased Bad translocation to mitochondria. Neither carbaprostacylin nor 4-(3-(2-propyl-3-hydroxy-4-acetyl)-phenoxy)propyloxyphenoxy acetic acid (L-165041) prevented HUVECs from SUL-induced apoptosis. Because of suppression of ectopic PPARdelta by sulindac, adenoviral PPARdelta transduction failed to restore 14-3-3epsilon or prevent PPAR cleavage. Our findings suggest that NSAIDs, but not aspirin (

A formal [3+3] cycloaddition strategy to substituted glutarimides was studied. N -Benzyl α-sulfonylacetamides and various α,β-unsaturated esters were used as starting materials.

Room temperature photoluminescence (PL) has been observed from Er doped silicon rich silicon oxide films grown by magnetron sputtering. For all kinds of silicon rich silicon oxide films grown with different excess Si contents, each PL spectrum has two peaks at 1.54 and 1.38μm, which originate from Er3+ and a certain kind of defects, respectively, in the silicon rich silicon oxide. It was found that 1.54 and 1.38μm PL peak intensities are correlated with each other. The PL intensity-dependence on the excess-Si content and annealing temperature was studied in detail.

The photoluminescence (PL) intensity of porous silicon in H2O2 under illtimina-tion increases first, and then decreases with increasing processing time, and the PL intensity reaches its maximum when the processing time is one minute. Under illumination in air, the PL degradation of porous silicon without processing is substa-ntia1, but that for the processed porous silicon gets much smaller. The Fourier-transform infrared (FTIR) absorption shows that the localized vibration related to oxygen increases greatly but all kinds of Si-H bonds decrease obviously. Contrasting the variation of the FTIR with that of the PL in the processes, we conclude that the luminescence does not come from the Si-H bonds on the surfaces of porous silicon.