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Docosahexaenoic acid (DHA) plays an essential role in brain, and its status is dependent on dietary intakes. School-aged children in rural China, who consume diets low in omega-3 polyunsaturated fatty acids, may benefit from DHA supplementation. Therefore, this trial was performed to examine the effect of 6-month DHA supplementation on executive functions (EFs) among healthy school-aged children in rural China. A randomized, double-blind, placebo-controlled trial was conducted among 106 primary school children aged 7–12 years in rural China. Participants were randomized to receive either 300 mg/d DHA or placebo for 6 months. EFs including working memory and cognitive flexibility were evaluated at baseline, at 3 months and at 6 months, using Digit Span Backwards and Wisconsin card sorting test, respectively. Socio-demographic data were collected at baseline, and erythrocyte membrane fatty acids and serum neurotransmitters were measured at baseline and after 6-month intervention. Ninety-four children (88.7%) completed the study according to the protocol. Changes in erythrocyte membrane fatty acids indicated good compliance of the participants. There was no significant intervention effect on serum neurotransmitters. In two-factor ANCOVA, both groups showed a significant improvement in the Digit Span Backwards and the Wisconsin card sorting test from baseline to endpoint. However, no significant intervention effect was found on any EF scores. Linear regression analysis suggested no significant association between changes in erythrocyte DHA level with changes in any EF scores. Supplementation with 300 mg/d DHA for 6 months had no benefit on EFs including working memory and cognitive flexibility among healthy school-aged children. This trial was registered at clinicaltrials.gov as NCT02308930 on December 5, 2014.

Starches from sixteen cassava germplasms harvested at the same time in the Hainan region were evaluated for their physicochemical and structural properties. The granule morphology of all the isolated cassava starch samples showed round, bell or oval shapes and exhibited the same A-type crystalline pattern. The crystallinity range was 26.6–30.8%. The selected cassava germplasms showed a wide variation in granule size distribution: The D[4,3] (the average particle size) ranged from 13.49 μm to 306.27 μm. The water absorption capacity (192.6–226.7%), oil absorption capacity (185.0–216.9%) and transparency (6.8–16.5%) indices varied significantly among the cassava germplasms. However, the retrogradation rates of the cassava starch pastes increased rapidly during the first 1 h and then stabilized. The solubility of starch increased with the temperature. In addition, the FTIR (Fourier Transform Infrared Spectrometer) ratios of 1045/1022 cm−1 and 1022/995 cm−1 of the sixteen cassava starches varied in the range of 1.06–1.78 and 0.78–1.04, respectively. These results indicated that the granule size, relative crystallinity, degree of short-range order, water and oil absorption capacities, solubility and transparency of the cassava starches were greatly influenced by the variety of cassava, which could help in determining the advantages of these starches for applications in different food and nonfood industries.

Activin A, a member of the transforming growth factor-beta superfamily, plays a neuroprotective role in multiple neurological diseases. Endoplasmic reticulum (ER) stress-mediated apoptotic and autophagic cell death is implicated in a wide range of diseases, including cerebral ischemia and neurodegenerative diseases. Thapsigargin was used to induce PC12 cell death, and Activin A was used for intervention. Our results showed that Activin A significantly inhibited morphological changes in thapsigargin-induced apoptotic cells, and the expression of apoptosis-associated proteins [cleaved-caspase-12, C/EBP homologous protein (CHOP) and cleaved-caspase-3] and biomarkers of autophagy (Beclin-1 and light chain 3), and downregulated the expression of thapsigargin-induced ER stress-associated proteins [inositol requiring enzyme-1 (IRE1), tumor necrosis factor receptor-associated factor 2 (TRAF2), apoptosis signal-regulating kinase 1 (ASK1), c-Jun N-terminal kinase (JNK) and p38]. The inhibition of thapsigargin-induced cell death was concentration-dependent. These findings suggest that administration of Activin A protects PC12 cells against ER stress-mediated apoptotic and autophagic cell death by inhibiting the activation of the IRE1-TRAF2-ASK1-JNK/p38 cascade.

Previous studies have demonstrated that betaine supplements increase lean body mass in livestock and improve muscle performance in human beings, but evidence for its effect on human lean mass is limited. Our study assessed the association of circulating betaine with lean mass and its composition in Chinese adults. A community-based study was conducted on 1996 Guangzhou residents (weight/mass: 1381/615) aged 50–75 years between 2008 and 2010. An interviewer-administered questionnaire was used to collect general baseline information. Fasting serum betaine was assessed using HPLC-MS. A total of 1590 participants completed the body composition analysis performed using dual-energy X-ray absorptiometry during a mean of 3·2 years of follow-up. After adjustment for age, regression analyses demonstrated a positive association of serum betaine with percentage of lean mass (LM%) of the entire body, trunk and limbs in men (all PP=0·016). Each sd increase in serum betaine was associated with increases in LM% of 0·609 (whole body), 0·811 (trunk), 0·422 (limbs), 0·632 (arms) and 0·346 (legs) in men and 0·350 (trunk) in women. Multiple logistic regression analysis revealed that the prevalence of lower LM% decreased by 17 % (whole body) and 14 % (trunk) in women and 23 % (whole body), 28 % (trunk), 22 % (arms) and 26 % (percentage skeletal muscle index) in men with each sd increment in serum betaine. Elevated circulating betaine was associated with a higher LM% and lower prevalence of lower LM% in middle-aged and elderly Chinese adults, particularly men.

Macrophages can be alternatively activated by TGF-β1 and high-ambient glucose, in which the role of Smad2 and the crosstalk between ERK and Smad2 pathways are not fully understood. The activation of ERK and Smad2 pathways and the expression of arginase-1 were detected by Western blot. The role of Smad2 and the relationship between ERK and Smad2 pathways were investigated by using biochemical inhibitors. The protein of arginase-1 was significantly overexpressed in RAW264.7 cells stimulated by TGF-β1 and high-ambient glucose, which can be partially blocked by not only U0126 (ERK inhibitor) but also SB431542 (Smad2 inhibitor). Furthermore, simply inhibiting one pathway had no effect on the other pathway. In conclusion, both ERK and Smad2 signal pathways are involved in the activation of macrophages induced by TGF-β1 and high-ambient glucose, while there is no crosstalk shown in the process.

Aiming to be applied in silicon gyroscope, a three-order single loop feedforward modulator with three-bit quantizer and local feedback is designed in this paper. Signal band is 200 KHz, sampling rate is 25.6 MHz, OSR is 64. Ideal modulator is then designed and simulated in MATLAB, getting SNR 125dB. Non-ideal factors are also added to ideal model, DWA technology is adopted to restrain the nonlinearity of multi-bit quantizer, getting SNR 104dB. Finally, transistor-level full-difference modulator is designed and simulated in Cadence, fetting SNR 101.3dB.

The dietary intake of methyl donors is favorably associated with many diseases, but the findings regarding primary liver cancer (PLC) risk are limited. This study investigated the association between the intake of choline, betaine and methionine and PLC risk in adults. This 1:1 matched case-control study enrolled 644 hospital-based PLC patients and 644 community-based controls who were matched by sex and age, in Guangzhou, China. An interviewer-administered questionnaire and a food-frequency questionnaire were used to collect general information and dietary intake information. Conditional logistic regression showed a significantly inverse association between total choline and betaine intakes and PLC risk. The multivariable-adjusted odds ratios (ORs) and their 95% confidence intervals (CIs) for PLC for the top (vs. bottom) tertile were 0.34 (0.24–0.49; P -trend P -trend = 0.011) for betaine. No significant association was observed between the intake of methionine and PLC risk (P > 0.05). For individual choline compounds, higher consumptions of free choline, glycerophosphocholine, phosphocholine, phosphatidylcholine and sphingomyelin were associated with a lower PLC risk (all P-trend P-interactions: 0.488–0.890). Our findings suggest that higher choline and betaine intakes may be associated with a lower risk of PLC.

The QTLs associated with cassava yield traits were detected by two-QTL model (unconditional and conditional QTLs) approaches after planting for 90 d, 180 d and 270 d in the present study. A genetic linkage map was constructed with a segregating F1population derived from a cross of 2 heterozygous parental plants from the cultivars South China 6 and Mianbao, and analysed with 39 SSR markers. The constructed linkage map of cassava consisted of 12 linkage groups covering a total length of 694.59 cM with a mean distance of 17.81 cM between two markers. The F1 population was evaluated for components of yield including fresh root yield (FRY), harvest index (HI), and starch content in dry root weight (SC) at 90 d, 180 d and 270 d. The identification of QTLs for yield traits at three growth periods explained 56.4% for FRY, 16.3% for HI and 27.3% for SC, suggesting characterization of yield components. The work made a step closer to understand the persistence of quantitative genetic variations of cassava in different development periods.

In order to exploit the induced female 2n gametes for cassava (Manihot esculenta) breeding, a detailed histological observation of female gametogenesis was conducted to correlate with the morphological characteristics of inflorescences and female flower buds. The SC5 gynoecia at the stage of prophase I were selected for unreduced megaspores induction with 0.3 % colchicine and 1 % dimethyl sulfoxide-soaked cotton plugs for 2 days. The resulted female cyathia were artificially pollinated with ploidy-level mixed pollens of SC10. Out of 250 hybrid progenies, two plants which exhibited morphological variations were confirmed as sexual tetraploids by flow cytometry and chromosome counting. Our results demonstrated that induction of 2n gametes combined with hybridization can be an effective approach for sexual tetraploid production for cassava.

Fe3O4 nanoparticles were prepared, and catalyzed the reaction of H2O2-methyl orange. In pH 1.42 HCl-NaAc buffer solution, methyl orange has two absorption peaks at 331nm and 506 nm. When Fe3O4 nanoparticles was added, it can catalyzed H2O2 oxidizing methyl orange to result in the absorption value decreased at 506 nm. The decreased absorption value is linear with the concentration of H2O2 in the range of 3.5-33 μmol/L. Based on this, a new colorimetric assay has been proposed for the determination of H2O2 in the water sample, with satisfactory results.

We studied the effects of surface oxidation on the kinetics of deuterium (D 2 ) absorption by Sc. A Sieverts apparatus was used to measure the D 2 absorption kinetics and X-ray photoelectron spectroscopy (XPS) was used to determine the surface oxidation state during heat treatments in ultra-high vacuum. In the as-received condition, the bulk Sc sample was covered by an Sc 2 O 3 film. However, the Sc 2 O 3 phase decomposed dramatically at 573 K due to the fast diffusion of oxygen from the surface to the bulk. The initial surface of Sc was cleaned of most oxygen by heating up to 873 K whereas the obtained fresh surface at temperatures over 873 K was contaminated by oxygen again when cooled down to room temperature. Due to fresh surfaces available for D 2 absorption, the sample at temperatures over 873 K started to absorb D 2 as soon as it was introduced. The absorption rate at these temperatures appears to be governed by D diffusion in the Sc bulk. However, the sample deuterated at room temperature presented an incubation time before the absorption was observed. And this stage was followed by a surface controlled process that changed gradually to a stage related to deuterium diffusion into the bulk.

Adult cardiomyocytes (CMs) have very limited capacity to regenerate. Therefore, there is a great interest in developing strategies to treat infarcted CMs that are able to regenerate cardiac tissue and promote revascularization of infarcted zones in the heart. Recently, stem cell transplantation has been proposed to replace infarcted CMs and to restore the function of the affected tissue. This area of research has become very active in recent years due to the huge clinical need to improve the efficacy of currently available therapies. Slingshot (SSH) is a family of protein phosphatases, which can specifically dephosphorylate and reactivate cofilin and inhibit the polymerization of actin filaments and actively involved in cytoskeleton rearrangement. In this study, we found that SSH1L promoted morphology changes of microfilaments during differentiation but was inhibited by the inhibitors of actin polymerization such as cytochalasin D. Overexpression of SSH1L could promote cardiac-specific protein and genes expression. 5-Aza can induce the differentiation of hMSCs into cardiomyocyte-like cells in vitro. We also observed that SSH1L efficiently promotes hMSCs differentiation into cardiomyocyte-like cells through regulation and rearrangement of cytoskeleton. Our work provides evidence that supports the positive role of SSH1L in the mechanism of stem cell differentiation into cardiomyocyte-like cells.

In this paper, a novel structure named as quasidouble silicon-on-insulator metal-oxide-semiconductor transistor (SOI MOSFET) is proposed. Compared with the structure of normal SOI MOSFET, ultrathin oxide layers and p+ wells are added under the source and drain regions, which successfully isolate the source and drain from the buried oxide (BOX). The ultrathin oxide layers prevent the leakage current of the back gate and enhance its reliability. And the P+ wells acting as body ties suppress the floating body effect, but also decrease the resistance of the body contact. Transfer characteristic curve, output characteristic curve and the reliability of this structure are simulated by Sentaurus TCAD, and we compared the simulation results with that of the normal SOI MOSFET.

Dietary intake of vitamin A (VA) and carotenes has shown beneficial effects for decreasing the risk of some types of cancer, but findings on the risk of primary liver cancer (PLC) are inconsistent. This case–control study explored the associations between the dietary intake of VA and carotenes and the risk of PLC. We recruited 644 incident PLC patients (diagnosed within one month of each other) and 644 age- and gender-matched controls in Guangzhou, China. A food frequency questionnaire was used to assess habitual dietary intake. Logistic regression analyses found that higher intakes of VA and carotenes were independently associated with decreased PLC risk (all P-trend < 0.001). The multivariable-adjusted ORs (95% CI) of PLC for the highest (vs. lowest) quartile were 0.34 (0.24–0.48) for vitamin A and 0.35 (0.25–0.49) for carotenes. The associations were not significantly modified by smoking, alcohol, or tea drinking (P-interactions: 0.062–0.912). Dose–response analysis showed a U-shaped VA–PLC relationship, with sharply decreased risks at the intakes of about 1000 μg retinol equivalent (RE)/day, and then slowly went down toward the flat-bottomed risks with the lowest risk at 2300 μg RE/day. Our findings suggest that greater intake of retinol, carotenes, and total VA may decrease PLC risk among the Chinese population at an intake of 1000 μg RE/day or greater from food sources.

Activin A (Act A), a member of the transforming growth factor-beta (TGF-β), reduces neuronal apoptosis during cerebral ischemia through Act A/Smads signaling pathway. However, little is known about the effect of Act A/Smads pathway on autophagy in neurons. Here, we found that oxygen-glucose deprivation (OGD)-induced autophagy was suppressed by exogenous Act A in a concentration-dependent manner and enhanced by Act A/Smads pathway inhibitor (ActRIIA-Ab) in neuronal PC12 cells. These results indicate that Act A/Smads pathway negatively regulates autophagy in OGD-treated PC12 cells. In addition, we found that c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein (MAP) kinase pathways are involved in the OGD-induced autophagy. The activation of JNK and p38 MAPK pathways in OGD-treated PC12 cells was suppressed by exogenous Act A and enhanced by ActRIIA-Ab. Together, our results suggest that Act A/Smads signaling pathway negatively regulates OGD-induced autophagy via suppression of JNK and p38 MAPK pathways in neuronal PC12 cells.

Here we describe a potent tool to investigate arginine rhamnosylation and develop novel antibiotics., A previously discovered posttranslational modification strategy – arginine rhamnosylation – is essential for elongation factor P (EF-P) dependent rescue of polyproline stalled ribosomes in clinically relevant species such as Pseudomonas aeruginosa and Neisseria meningitidis. However, almost nothing is known about this new type of N-linked glycosylation. In the present study we used NMR spectroscopy to show for the first time that the α anomer of rhamnose is attached to Arg32 of EF-P, demonstrating that the corresponding glycosyltransferase EarP inverts the sugar of its cognate substrate dTDP-β-l-rhamnose. Based on this finding we describe the synthesis of an α-rhamnosylated arginine containing peptide antigen in order to raise the first anti-rhamnosyl arginine specific antibody (anti-ArgRha). Using ELISA and Western Blot analyses we demonstrated both its high affinity and specificity without any cross-reactivity to other N-glycosylated proteins. Having the anti-ArgRha at hand we were able to visualize endogenously produced rhamnosylated EF-P. Thus, we expect the antibody to be not only important to monitor EF-P rhamnosylation in diverse bacteria but also to identify further rhamnosyl arginine containing proteins. As EF-P rhamnosylation is essential for pathogenicity, our antibody might also be a powerful tool in drug discovery.

In this paper, LaNi4.7Al0.3 alloy samples were obtained via melting in middle frequency influence fire .In addition, The alloy pellets were milled for absorbing and desorbing Hydrogen ability study, The P-V-T measurement provided us with poisonous effect on the oxidation of LaNi4.7Al0.3.To understand the poisoning mechanism of O2 on LaNi4.7Al0.3, the X-ray photoelectron spectroscopy (XPS) was introduced to analyzed the process of poisoning of LaNi4.7Al0.3 alloy, Which revealed the changes of the valence of the elements of the alloy LaNi4.7Al0.3 poisoned by O2.

Bacteriophage 29 (Phi29) packaging RNA (pRNA) is one of the key components in the viral DNA-packaging motor. It contains two functional domains facilitating the translocation of DNA into the viral capsid by interacting with other elements in the motor and promoting adenosine triphosphates hydrolysis. Through the connection between interlocking loops in adjacent pRNA monomers, pRNA functions in the form of multimer ring in the motor. Previous studies have addressed the unique structure and conformation of pRNA. However, there are different DNA-packaging models proposed for the viral genome transportation mechanism. The DNA-packaging ability and the unique features of pRNA have been attracting efforts to study its potential applications in nanotechnology. The pRNA has been proved to be a promising tool for delivering nucleic acid-based therapeutic molecules by covalent linkage with ribozymes, small interfering RNAs, aptamers, and artificial microRNAs. The flexibility in constructing dimers, trimers, and hexamers enables the assembly of polyvalent nanoparticles to carry drug molecules for therapeutic purposes, cell ligands for target delivery, image detector for drug entry monitoring, and endosome disrupter for drug release. Besides these fascinating pharmacological advantages, pRNA-based drug delivery has also been demonstrated to prolong the drug half life with minimal induction of immune response and toxicity.

The present study investigated the neuroprotective effects of aucubin on hydrogen peroxide (H2O2)-induced apoptosis in PC12 cells. Exposure of PC12 cells to 0.25 mm H2O2 induced a leakage of lactate dehydrogenase and decreased cell viability, as shown by 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide assay. In a dose over 0.1 mm, aucubin increased PC12 cellular viability and markedly attenuated H2O2-induced apoptotic cell death. Quantitation of apoptosis by flow cytometry indicated that aucubin inhibited H2O2-induced apoptosis in PC12 cells. Nuclear damage was alleviated by aucubin, as shown by Hoechst staining. In addition, the levels of malondialdehyde were reduced and the activity of superoxide dismutase, catalase and glutathione peroxidase was augmented in these cells. These results indicated that aucubin inhibited H2O2-induced apoptosis in PC12 cells through regulation of the endogenous oxidant–antioxidant balance. Our results suggest that aucubin is a potential protective agent for the treatment of oxidative-stress-induced neurodegenerative disease. Copyright © 2011 John Wiley & Sons, Ltd.

The first synthesis of the naturally occurring cyclic peptide euryjanicin B has been achieved. A general method was described to synthesize the cyclic peptide by a two-step solid-phase/solution synthesis strategy. All the amino acids in this study are L -configuration, The linear heptapeptide was assembled by standard Fmoc chemistry on solid-phase and subsequently cyclization was carried out by solution method.

Based on the active site of lanosterol 14α-demethylase of azole antifungal agents, sixteen 1-(1H-1,2,4-triazole-1-yl)- 2-(2,4-difluorophenyl)-3-(N-n-butyl-N-1-substitutedbenzyl-4-methylene-1H-1,2,3-triazole)-2-propanols have been designed, synthesized and evaluated as antifungal agents. Results of preliminary antifungal tests against eight human pathogenic fungi in vitro showed that some of the compounds exhibited excellent activities with broad spectrum.

In this study, the effect of aucubin on H(2)O(2)-induced apoptosis was studied by using a rat pheochromocytoma (PC12) cell line. We have analyzed the apoptosis of H(2)O(2)-induced PC12 cells, H(2)O(2)-induced apoptosis appeared to correlate with lower Bcl-2 expression, higher Bax expression and sequential activation of caspase-3 leading to cleavage of poly-ADP-ribose polymerase (PARP). Aucubin not only inhibited lower Bcl-2 expression, high Bax expression, but also modulated caspase-3 activation, PARP cleavage, and eventually protected against H(2)O(2)-induced apoptosis. These results indicated that aucubin can obstruct H(2)O(2)-induced apoptosis by regulating of the expression of Bcl-2 and Bax, as well as suppression of caspases cascade activation.

A series of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-(N-isoproyl-N-substituted-amino)-2-propanols have been designed and synthesized on the basis of the active site of lanosterol 14a-demethylase (CYP51). Their structures were confirmed by MS and 1H NMR. In vitro antifungal activities of these synthesized compounds were evaluated against eight human pathogenic fungi. The results showed that all title compounds exhibited activity against fungi tested to some extent. Compounds 3c, 3d, 7a, 7b and 7c exhibited more potent antifungal activities against nearly all fungi tested except Aspergillus fumigatus than fluconazole.

Excess production of reactive oxygen species by macrophages has been implicated in many inflammatory diseases. The present study investigated the inhibitory effect of the stem bark extract of Acanthopanax senticosus on the production of superoxide anion and hydrogen peroxide in mouse peritoneal macrophages in vitro and in vivo. Exposure of mouse peritoneal macrophages to A. senticosus extract significantly suppressed superoxide anion production induced by zymosan in a dose-dependent manner. Similarly, exposure of mouse peritoneal macrophages to A. senticosus extract significantly inhibited hydrogen peroxide production induced by phorbol 12-myristate 13-acetate (PMA) in a dose-dependent manner. Intraperitoneal administration of A. senticosus extract to KM mice reduced the ex vivo production of zymosan induced-superoxide anion and PMA-induced hydrogen peroxide by their peritoneal macrophages. Exposure to A. senticosus extract did not affect the cell viability or systemic toxicity. A. senticosus inhibited reactive oxygen species production by mouse peritoneal macrophages in vitro and in vivo and may be partly responsible for the antiinflammatory function.

The effects of MgO promoter on the physicochemical properties and catalytic performance of Ni/Al2O3 catalysts for the partial oxidation of methane to syngas were studied by means of BET, XRD, H2-TPR, TEM and performance evaluation. It was found that the MgO promoter benefited from the uniformity of nickel species in the catalysts, inhibited the formation of NiAl2O4 spinel and improved the interaction between nickel species and support. These results were related to the formation of NiO-MgO solid solution and MgAl2O4 spinel. Moreover, for the catalysts with a proper amount of MgO promoter, the nickel dispersiveness was enhanced, therefore making their catalytic performance in methane partial oxidation improved. However, the excessive MgO promoter exerted a negative effect on the catalytic performance. Meanwhile, the basicity of MgO promoted the reversed water-gas shift reaction, which led to an increase in CO selectivity and a decrease in H2 selectivity. The suitable content of MgO promoter in Ni/Al2O3 catalyst was ∼7 wt-%.

Excess nitric oxide (NO) production has been implicated in inflammatory diseases. The present study investigated the inhibitory effect of the stem bark extract of Acanthopanax senticosus (A. senticosus) on NO production in murine macrophages in vitro and in vivo. In vitro exposure of RAW264.7 cells to 1, 10, 50, 100, 250, 500 and 1000 µg/mL of A. senticosus extract significantly suppressed NO production induced by lipopolysaccharide (LPS) and interferon gamma (IFN-γ) in a dose-dependent manner. In vitro exposure of mouse resident peritoneal macrophages to 1, 10, 100 and 1000 µg/mL of A. senticosus extract significantly suppressed NO production induced by LPS and IFN-γ in a dose-dependent manner. In vivo administration of A. senticosus extract (50, 100 and 200 mg/kg) to KM mice dose-dependently inhibited LPS and IFN-γ induced production of NO in isolated mouse peritoneal macrophages ex vivo. Exposure to A. senticosus extract had no effect on cell viability and systemic toxicity. The results demonstrated that the stem bark extract of A. senticosus extract inhibits NO production in murine macrophages in vitro and in vivo. Copyright © 2007 John Wiley & Sons, Ltd.

[1,2,4]-Triazole-[4,3-a]-quinoxaline is an important component of many drugs. The yield of the reported methods for triazole cyclization step was usually as low as 20%. In this article, the triazole cyclization step was successfully done by using microwave method with a high yield of 75% for the first time.

Twenty-three 1-(1H-1, 2, 4-thazole-1-yl)-2-(2, 4-difluorophenyl)-3-(N-cycloproyl-N-substituted-amino)-2-propanols were designed and synthesized on the basis of the active site of lanosterol 14α-demethylase. In vitro antifungal activities showed that some of the title compounds had higher antifungal activity and broader antifungal spectrum than fluconazole.

Since the 1990s, a number of terminal alkynyl residue-containing cyclic/acyclic peptides have been identified from marine organisms, especially cyanobacteria and marine mollusks. This review has presented 66 peptides, which covers over 90% marine peptides with terminal alkynyl fatty acyl units. In fact, more than 90% of these peptides described in the literature are of cyanobacterial origin. Interestingly, all the linear peptides featured with terminal alkyne were solely discovered from marine cyanobacteria. The objective of this article is to provide an overview on the types, structural characterization of these unusual terminal alkynyl fatty acyl units, as well as the sources and biological functions of their composed peptides. Many of these peptides have a variety of biological activities, including antitumor, antibacterial, antimalarial, etc. Further, we have also discussed the evident biosynthetic origin responsible for formation of terminal alkynes of natural PKS (polyketide synthase)/NRPS (nonribosome peptide synthetase) hybrids.

Copper is known to be a critical factor in Alzheimer's disease (AD) pathogenesis, as it is involved in amyloid-β (Aβ) peptide related toxicity. However, the relationship between neurotoxicity and Aβ peptide in the presence of copper remains unclear. The effect of copper has not been clearly differentiated between Aβ42 and Aβ40, and it is still debated whether copper-mediated neurotoxicity is due to reactive oxygen species (ROS) accumulation or other molecular mechanisms. Here, we describe that copper dramatically affects Aβ42 aggregation and enhances Aβ42 cytotoxicity while it shows no significant effects on Aβ40. These phenomena are mainly because that the strong interactions between copper and Aβ42 lead to great conformation changes, and stabilize Aβ42 aggregates at highly toxic nanoscale oligomer stage, whereas copper shows no similar impact on Aβ40. We also propose a possible molecular mechanism that copper enhances Aβ42 cytotoxicity via perturbing membrane structure. Moreover, we test the effect of an analogue of copper, nickel, on Aβ aggregation and cytotoxicity, finding that nickel also enhances cytotoxicity via Aβ42 nanoscale oligomer formation. These results clarify that the copper-induced Aβ42 nanoscale oligomer formation is the key process for Aβ neurotoxicity, and suggest that disrupting the interactions between copper and Aβ42 peptide to inhibit nanoscale oligomerization process, deserves more attention in AD drug development.

Seedlings of O. violaceus were cultured on MS media and treated at low temperature. Cold treatment at 5–7 °C for more than 7 days was needed for flower induction of seedlings in vitro originated from germinated seeds. When cultured on MS media supplemented with 2.5 mg l−1 zeatin and 2 mg l−1 gibberellin (GA3), seedlings in vitro did initiate flowers without cold treatment. When MS media was used with a reduced amount of NH4NO3, flower induction of seedlings in vitro could be accelerated.

[1,2,4]-Triazole-[4,3-a]-quinoxaline is an important component of many drugs. The yield of the reported methods for triazole cyclization step was usually as low as 20%. In this article, the triazole cyclization step was successfully done by using microwave method with a high yield of 75% for the first time.

Oligo-microarray can be fabricated on modified surface of glass slides involving immobilization of oligonucleotides. In this study, glass slides were modified with acrylic acid-co-acrylamide copolymer and EDC (1-ethyl-3(3-dimethylaminopropyl)-carbodiimide)/NHS (N-hydroxysuccinimide) by covalent linkage method, and covalent immobilization of unmodified oligonucleotide on the glass surface was achieved. The platform with binding of stable and sensitive oligonucleotides was prepared for oligo-microarray fabrication. An optimum concentration of 0.5 g/L was used for spotting. The lengths of 26 to 70 mer oligonucleotides were immobilized on the surface efficiently. The spots were ∼160 nm in diameter and their mean value of fluorescent intensity was measured in the range of 3.2 × 104 to 7.3 × 104 after hybridization. The modified glass surface was scanned by SEM and the dendritic structure was observed. Results showed that the process of preparation of the modified glass surface was simple and cost effective, and the modified surface can be used for the oligo-microarray fabrication and also attachment of protein, PNA etc. © 2008 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater, 2008

Aim of the study In this study, we evaluated protective effect of Acanthopanax senticosus extract (ASE) and a possible signaling pathway involved during endotoxic shock induced by intraperitoneal injection lipopolysaccharide (LPS) and D-galactosamine (D-GalN) in BALB/c mice. Materials and methods Mice were intraperitoneal administrated with ASE (100, 200 or 400 mg/kg) prior to injection of 50 μg/kg LPS and 1 g/kg D-GalN. The levels of tumor necrosis-alpha (TNF-α) and interleukin-10 (IL-10) in serum and liver. Nitric oxide (NO) production in serum and inducible nitric oxide synthase (iNOS) protein level were investigated. Nuclear factor-kappa B (NF-κB) activation in liver was determined. Furthermore, we evaluated the effect of ASE pretreatment on infiltration of inflammatory cells into the heart, liver and lung of mice. Results Treatment of mice with ASE prior to LPS/D-GalN injection significantly improved the survival rate. ASE pretreatment inhibited the elevation of TNF-α in serum and liver. ASE also decreased iNOS level in liver and the overproduction of nitric oxide (NO) in serum. In addition, IL-10 levels in serum and liver were markedly enhanced. ASE pretreatment inhibited NF-κB activation in liver of mice. Moreover, infiltration of inflammatory cells into the heart, liver and lung of mice was also attenuated by ASE pretreatment. Conclusions These results suggested that ASE protected mice against LPS/D-GalN-induced endotoxic shock involving inhibition of NF-κB activation, which caused down-regulation of TNF-α and involved up-regulation of IL-10. Acanthopanax senticosus may thus prove beneficial in the prevention of endotoxic shock.

Aim of the study The herb Acanthopanax senticosus (Siberian ginseng) has long been used as a traditional medicine. However, little is known about anti-inflammatory effects and its mechanisms of action. Excess production of nitric oxide (NO) is one of the characteristics of inflammation. In this study we examined the effects of A. senticosus extract (ASE) on NO production and inducible nitric oxide synthase (iNOS) gene expression in lipopolysaccharide (LPS) plus interferon-gamma (IFN-γ)-stimulated RAW264.7 macrophages and investigated its mechanisms of anti-inflammatory activity. Materials and methods RAW264.7 macrophages were treated with 10 μg/ml LPS plus 20 U/ml IFN-γ in the presence or absence of ASE. NO production and iNOS gene expression were investigated. We further evaluated the effect of ASE on oxidative stress-sensitive transcription nuclear factor-kappa B (NF-κB) activation. Results ASE significantly suppressed NO production and iNOS gene expression in a dose-dependent manner. ASE also reduced DNA-binding activity of NF-κB in LPS plus IFN-γ stimulated RAW264.7 macrophages. Further studies indicated that LPS plus IFN-γ-induced inhibitory factor-kappa B alpha (I-κBα) degradation and p65 nuclear translocation were inhibited in RAW264.7 macrophages exposed to ASE. Moreover, ASE inhibited the LPS plus IFN-γ mediated increase in intracellular peroxides production. Conclusions These results suggest ASE suppresses iNOS gene expression through the inhibition of intracellular peroxides production, which has been implicated in the activation of NF-κB.

In the title compound, [Cd(C(14)H(8)O(4))(C(12)H(8)N(2))](n), the Cd(II) ion is seven-coordinated in a distorted penta-gonal-bipyramidal coordination geometry by five O atoms from bridging biphenyl-3,3'-dicarboylate (dpda) ligands and two N atoms from a 1,10-phenanthroline (1,10-phen) ligand. In the crystal, dinuclear units with a Cd⋯Cd separation of 3.8208 (7) Å are observed. Each of these dinuclear units is bridged via 3,3'-bpda in a chelating/chelating and bridging fashion, generating a zigzag chain along the c axis. Neighboring chains are further packed via weak π-π inter-actions between inter-chain parallel 1,10-phen rings [centroid-centroid distance = 3.5197 (9) Å] into a three-dimensional supra-molecular architecture.