Input: Plant breeders and biotechnologists have attempted to manipulate HKT gene expression through genetic engineering and more conventional plant breeding methods to improve the salinity tolerance of commercially important crop plants.


Input: Successful manipulation of a biological trait is more likely to be effective after a thorough understanding of how the trait, genes and proteins are interconnected at the whole plant level.


Input: This article examines the current structural and functional knowledge relating to plant HKTs and how their structural features may explain their transport selectivity.


Input: We also highlight specific areas where new knowledge of plant HKT transporters is needed.


Input: Our goal is to present how knowledge of the structure of HKT proteins is helpful in understanding their function and how this understanding can be an invaluable experimental tool.


Input: As such, we assert that accurate structural information of plant IMPs will greatly inform functional studies and will lead to a deeper understanding of plant nutrition, signalling and stress tolerance, all of which represent factors that can be manipulated to improve agricultural productivity.


Input: Sphingomyelin in high-density lipoproteins: structural role and biological function.

Sphingomyelin


Input: High-density lipoprotein (HDL) levels are an inverse risk factor for cardiovascular diseases, and sphingomyelin (SM) is the second most abundant phospholipid component and the major sphingolipid in HDL.

sphingomyelin

sphingolipid


Input: Considering the marked presence of SM, the present review has focused on the current knowledge about this phospholipid by addressing its variable distribution among HDL lipoparticles, how they acquire this phospholipid, and the important role that SM plays in regulating their fluidity and cholesterol efflux from different cells.

cholesterol


Input: In addition, plasma enzymes involved in HDL metabolism such as lecithin-cholesterol acyltransferase or phospholipid transfer protein are inhibited by HDL SM content.

cholesterol


Input: Likewise, HDL SM levels are influenced by dietary maneuvers (source of protein or fat), drugs (statins or diuretics) and modified in diseases such as diabetes, renal failure or Niemann-Pick disease.


Input: Furthermore, increased levels of HDL SM have been shown to be an inverse risk factor for coronary heart disease.


Input: The complexity of SM species, described using new lipidomic methodologies, and their distribution in different HDL particles under many experimental conditions are promising avenues for further research in the future.


Input: Bioinspired design and macroscopic assembly of poly (vinyl alcohol)-coated graphene into kilometers-long fibers.

poly (vinyl alcohol)

graphene


Input: Nacre is characterized by its excellent mechanical performance due to the well-recognized " brick and mortar " structure.


Input: Many efforts have been applied to make nacre-mimicking materials, but it is still a big challenge to realize their continuous production.


Input: Here, we prepared sandwich-like building blocks of poly (vinyl alcohol) (PVA)-coated graphene, and achieved high-nanofiller-content kilometers-long fibers by continuous wet-spinning assembly technology.

poly (vinyl alcohol)

PVA

graphene


Input: The fibers have a strict " brick and mortar " layered structure, with graphene sheet as rigid brick and PVA as soft mortar.

graphene

PVA


Input: The mortar thickness can be precisely tuned from 2. 01 to 3. 31 nm by the weight feed ratio of PVA to graphene, as demonstrated by both atomic force microscopy and X-ray diffraction measurements.

graphene


Input: The mechanical strength of the nacre-mimicking fibers increases with increasing the content of PVA, and it rises gradually from 81 MPa for the fiber with 53. 1 wt% PVA to 161 MPa for the fiber with 65. 8 wt% PVA.

PVA

PVA

PVA


Input: The mechanical performance of our fibers was independent of the molecular weight (MW) of PVA in the wide range of 2-100 kDa, indicating that low MW polymers can also be used to make strong nanocomposites.

PVA


Input: The tensile stress of fibers immersed in PVA 5 wt% solution reached ca.

PVA


Input: 200 MPa, surpassing the values of nacre and most of other nacre-mimicking materials.


Input: The nacre-mimicking fibers are highly electrically conductive (~ 350 S m (-1)) after immersing in hydroiodic acid, enabling them to connect a circuit to illuminate an LED lamp.

hydroiodic acid


Input: A capture approach for supercoiled plasmid DNA using a triplex-forming oligonucleotide.


Input: Proteins that recognize and bind specific sites in DNA are essential for regulation of numerous biological functions.


Input: Such proteins often require a negative supercoiled DNA topology to function correctly.


Input: In current research, short linear DNA is often used to study DNA-protein interactions.


Input: Although linear DNA can easily be modified, for capture on a surface, its relaxed topology does not accurately resemble the natural situation in which DNA is generally negatively supercoiled.


Input: Moreover, specific binding sequences are flanked by large stretches of non-target sequence in vivo.


Input: Here, we present a straightforward method for capturing negatively supercoiled plasmid DNA on a streptavidin surface.


Input: It relies on the formation of a temporary parallel triplex, using a triple helix forming oligonucleotide containing locked nucleic acid nucleotides.

nucleotides


Input: All materials required for this method are commercially available.


Input: Lac repressor binding to its operator was used as model system.


Input: Although the dissociation constants for both the linear and plasmid-based operator are in the range of 4 nM, the association and dissociation rates of Lac repressor binding to the plasmid-based operator are ~ 18 times slower than on a linear fragment.


Input: This difference underscores the importance of using a physiologically relevant DNA topology for studying DNA-protein interactions.


Input: Clinical Pharmacology and the Catalysis of Regulatory Science: Opportunities for the Advancement of Drug Development and Evaluation.


Input: The " regulatory paradox " is a tension between aversion to uncertainty and willingness to accept unknowns about a drug before its approval.


Input: Finding the right balance may mean the difference between fostering and stifling innovation.


Input: Clinical pharmacology applied in the drug development and regulatory contexts can bridge mechanistic reasoning and empiricism to help reconcile the regulatory paradox.


Input: Here, we propose that the discipline of clinical pharmacology, in the regulatory setting, is well positioned to build on its past successes in the advancement and acceleration of drug development. Clinical Pharmacology & Therapeutics (2013); advance online publication 10 April 2013. doi: 10. 1038/clpt. 2013. 32.


Input: Generic Development of Topical Dermatologic Products, Part II: Quality by Design for Topical Semisolid Products.


Input: The emergence of quality by design as a relatively new systematic science and risk-based approach has added a new dimension to pharmaceutical development and manufacturing.


Input: This review attempts to discuss the quality by design elements and concepts applied for topical semisolid products.


Input: Quality by design begins with defining a quality target product profile as well as critical quality attributes.


Input: Subsequently, this is followed by risk identification/risk analysis/risk evaluation to recognize critical material attributes and critical process parameters, in conjunction with design of experiments or other appropriate methods to establish control strategies for the drug product.


Input: Several design-of-experiment examples are included as practical strategies for the development and optimization of formulation and process for topical drug products.


Input: Hypermethylation of P15, P16, and E-cadherin genes in ovarian cancer.


Input: Both p16 and p15 proteins are inhibitors of cyclin-dependent kinases that prevent the cell going through the G1/S phase transaction.


Input: E-cadherin is a transmembrane glycoprotein that mediates calcium-dependent interactions between adjacent epithelial cells.

calcium


Input: Two groups of patients were selected: the first group suffered from epithelial serous ovarian tumors and the second group suffered from benign ovarian lesions; ovarian tissue samples from all the subjects (benign and malignant) were subjected to methylation-specific polymerase chain reaction for methylated and unmethylated alleles of the genes (E-cadherin, p15, and p16).


Input: Results obtained showed that aberrant methylation of p15 and p16 genes were detected in 64. 29 and 50% of ovarian cancer patients, while E-cadherin hypermethylation was detected in 78. 57% of ovarian cancer patients.


Input: Methylation of E-cadherin was significantly correlated with different stage of disease (p < 0. 05).


Input: It was found that the risk of E-cadherin hypermethylation was 1. 347-fold, while risk of p15 hypermethylation was 1. 543-fold and p16 was 1. 2-fold among patients with ovarian cancer than that among patients with benign ovarian lesions.


Input: In conclusion, Dysfunction of the cell cycle and/or the cell-cell adhesion molecule plays a role in the pathogenesis of ovarian cancer and that the analysis of the methylation of p15 and E-cadherin genes can provide clinically important evidence on which to base the treatment.


Input: Physiological and biochemical mechanisms of allelopathy mediated by the allelochemical extracts of Phytolacca latbenia (Moq.) H.


Input: Walter.


Input: In allelopathy, one plant suppresses the growth and development of other plant/plants by negatively affecting a variety of physiological and biochemical reactions.


Input: We checked the effects of methanolic extracts (allelochemical extracts) of Phytolacca latbenia (Moq.) H.


Input: Walter on antioxidant enzyme activities such as peroxidases (PODs), super oxide dismutases (SODs) and catalase (CAT) and on total protein contents (TPC), cellular injury (CI), and malondialdehyde (MDA) in the germinating seeds of Brassica napus L.

super oxide

malondialdehyde

MDA


Input: (dicot) and Triticum aestivum L.


Input: (monocot).


Input: Both the crude methanolic extract root (CMER) and crude methanolic extract aerial (CMEA) of P. latbenia at 10000 ppm significantly reduced the POD activity in both the test seeds.


Input: The activity of SODs was significantly decreased by both CMER and CMEA in B. napus germinating seeds.


Input: A linear increase in the activity of CAT, CI, and MDA contents was found in both the test seeds with the increasing concentrations of CMEA and CMER, while TPC of the germinating seeds was found decreased.

MDA


Input: It is inferred that both the CMEA and CMER inhibited/delayed the seed germination, reduced the seedling growth by affecting a variety of biochemical and physiological attributes, and also caused cellular membrane injury in the germinating seeds of both the monocot and dicot seeds.


Input: Ultrasonic synthesis, characterization of beta-aminoketones by bismuth (III) triflate and determination of antigenotoxic properties.

beta-aminoketones

bismuth (III) triflate


Input: Direct-type catalytic Mannich reaction for the synthesis of beta-aminoketones from cyclohexanone, substituted aromatic amines and aromatic or hetero-aromatic aldehydes has been applied in water with bismuth triflate under ultrasound.

beta-aminoketones

cyclohexanone

aromatic amines and aromatic or hetero-aromatic aldehydes

bismuth triflate


Input: Good yields of the expected beta-aminoketones were obtained from available substrates, at room temperature in 1-2 hours.

beta-aminoketones


Input: This study was designed to evaluate the mutagenic and antimutagenic potential of synthesized beta-aminoketones compounds using Ames/Salmonella and Escherichia coli WP2 bacterial reverse mutation assay systems.

beta-aminoketones


Input: Ameliorative effect of lycopene against 2, 3, 7, 8-tetrachlorodibenzo-pdioxin-induced rat liver microsomal toxicity: An in vitro study.

lycopene

2, 3, 7, 8-tetrachlorodibenzo-pdioxin


Input: The objective of the current study was to investigate the potential oxidative damage of 2, 3, 7, 8-tetrachlorodibenzo-p-dioxin (TCDD) in hepatic microsomal fractions in vitro and to further elucidate the potential modulatory effect of lycopene.

2, 3, 7, 8-tetrachlorodibenzo-p-dioxin

TCDD

lycopene


Input: Rat liver microsomes were divided into four groups.


Input: Group I served as a control and is incubated with vehicle (toluene).

toluene


Input: Groups II and IV were incubated with 20 micro M lycopene for 1 h before further incubating; groups III and IV with 15 nM of TCDD for further 1 h.

lycopene

TCDD


Input: Hydrogen peroxide (H2O2) production, lipid peroxidation (LPO), protein carbonyl content and activities of uridine 5'-diphospho-glucuronyltransferase (UDPGT) and P450 were significantly increased.

Hydrogen peroxide

carbonyl

uridine 5'-diphospho


Input: Moreover, the activity of antioxidant enzymes superoxide dismutase, glutathione peroxidase, catalse, glutathione-S-transferase and glutathione reductase as well as the microsomal thiol content were significantly decreased.

glutathione

glutathione

S

glutathione


Input: Incubation with lycopene (group IV) maintained near normal activities of the enzymes, normalized thiol and carbonyl content and significantly reduced LPO and H2O2 production.

lycopene

thiol

carbonyl


Input: In conclusion, the findings of the study indicate that TCDD induces a significant oxidative stress in liver microsomes as manifested by increased LPO, H2O2 production, protein carbonyl content and activities of UDPGT and P450 and decreased antioxidant enzymes activities and thiol content.

TCDD

carbonyl

thiol


Input: By the reversal of biochemical and oxidative markers toward normalcy, the protective role of lycopene is illuminated in rat liver microsomal toxicity.

lycopene


Input: Circulating glucagon to ghrelin ratio as a determinant of insulin resistance in hyperthyroidism.


Input: Due to stimulated overall metabolism, a state of nutritional inadequacy often ensues, during thyrotoxicosis.


Input: We aimed to investigate circulating levels of some major components of the system that regulates energy stores, glucose, and fat metabolism, during thyrotoxicosis compared to euthyroidism.

glucose


Input: Fasting serum ghrelin, leptin, adiponectin, insulin, glucagon, glucose, as well as body fat composition were analyzed during thyrotoxicosis in 40 hyperthyroid patients (50. 5 +/- 15. 2 years old, 22 females, 31 with Graves disease, and 9 with toxic nodular goiter).

glucose


Input: The same measurements were repeated an average 3 months later, when all patients achieved euthyroidism.


Input: Compared to euthyroidism, in thyrotoxicosis, patients had lower ghrelin and fat mass; had comparable insulin, HOMA-IR, glucagon, and leptin levels; higher levels of circulating adiponectin.


Input: Fasting serum glucose tended to be higher during thyrotoxicosis.

glucose


Input: The unique correlation of HOMA-IR was with the-glucagon to ghrelin ratio-(r = 0. 801, p < 0. 001) in hyperthyrodism, and with glucagon itself in euthyroidism (r =-0. 844, p < 0. 001).


Input: Circulating levels of ghrelin are decreased; leptin, insulin, glucagon are unchanged; adiponectin are increased during hyperthyroidism.


Input: The fasting HOMA-IR tends to be higher, despite the decreased adiposity in hyperthyroidism.


Input: The-glucagon to ghrelin ratio-strongly correlates with fasting HOMA-IR in hyperthyroidism.


Input: Clinical strategies to enhance the efficacy of nicotine replacement therapy for smoking cessation: a review of the literature.

nicotine


Input: A number of smoking cessation pharmacotherapies have led to increases in quitting and thus to significant benefits to public health.


Input: Among existing medications, nicotine replacement therapy (NRT) has been available the longest, has the largest literature base in support, and is the only option for over-the-counter access.

nicotine


Input: While the short-term efficacy of NRT is well documented in clinical trials, long-term abstinence rates associated with using NRT are modest, as most smokers will relapse.


Input: This literature review examines emerging clinical strategies to improve NRT efficacy.


Input: After an initial overview of NRT and its FDA-approved indications for use, we review randomized trials in which clinical delivery of NRT was manipulated and tested, in an attempt to enhance efficacy, through (1) duration of use (pre-quit and extended use), (2) amount of use (high-dose and combination NRT), (3) tailoring to specific smoker groups (genotype and phenotype), or (4) use of NRT for novel purposes (relapse prevention, temporary abstinence, cessation induction).


Input: Outcomes vary within and across topic area, and we highlight areas that offer stronger promise.


Input: Combination NRT likely represents the most promising strategy moving forward; other clinical strategies offer conflicting evidence but deserve further testing (pre-quit NRT or tailored treatment) or offer potential utility but are in need of further, direct tests.


Input: Some areas, though based on a limited set of studies, do not offer great promise (high-dose and extended treatment NRT).


Input: We conclude with a brief discussion of emergent NRT products (e. g., oral nicotine spray, among others), which may ultimately offer greater efficacy than current formulations.

nicotine


Input: In order to further lower the prevalence of smoking, novel strategies designed to optimize NRT efficacy are needed.


Input: Optimal management of metastatic renal cell carcinoma: current status.


Input: The armamentarium for the systemic therapy of advanced renal cell carcinoma (RCC) has undergone dramatic changes over the past 6 years.


Input: While high-dose interleukin (IL)-2 remains an option for highly selected good and intermediate risk patients with clear-cell histology because of durable complete responses in a small fraction of patients, cytokine-based therapy including interferon (IFN) has been supplanted by vascular-endothelial growth factor (VEGF) and mammalian target of rapamycin (mTOR) inhibitors.

rapamycin


Input: Treatment decision is initially based on prognostication of the disease.


Input: As metastatic RCC (mRCC) is commonly an indolent disease, a period of observation should always been considered.


Input: For good and intermediate risk disease, pazopanib, sunitinib or the combination of bevacizumab plus IFN are considered.

pazopanib

sunitinib


Input: Notably, recent data suggest non-inferiority for the efficacy of pazopanib compared to sunitinib coupled with a better toxicity profile.

pazopanib

sunitinib


Input: A novel VEGF receptor inhibitor, tivozanib, is expected to be approved based on improvement in PFS when compared to sorafenib in the first-line setting.

tivozanib

sorafenib


Input: The use of temsirolimus for poor risk disease is supported by a phase III trial dedicated to this group of patients.

temsirolimus


Input: The role of cytoreductive nephrectomy in the context of VEGF and mTOR inhibitors is being studied in randomized trials.


Input: Selected patients with solitary or oligometastatic disease may be eligible for metastatectomy.


Input: Following first-line VEGF inhibitors, second-line therapy with everolimus and axitinib have demonstrated benefits in progression-free survival (PFS).

everolimus

axitinib


Input: One phase III trial comparing sorafenib and temsirolimus in the post-sunitinib setting showed no difference in PFS, the primary endpoint, but did show a superior overall survival for sorafenib.

sorafenib

temsirolimus

sunitinib

sorafenib


Input: Sorafenib, pazopanib and axitinib have all demonstrated clinical benefit following cytokines.

Sorafenib

pazopanib

axitinib


Input: Therapy following first-line mTOR inhibitors remains undefined, although VEGF inhibitors have demonstrated activity in this setting.


Input: Optimal sequencing of agents and individualized therapy based on biomarkers is undergoing investigation.


Input: Today, the choice of therapy is based on patient and physician decision, which is a function of comorbidities, toxicity profiles and costs.


Input: Clinical trials evaluating novel agents and combinations should be preferred when available since agents in the current therapeutic arsenal have not yielded cures despite extending median survival to greater than 2 years.


Input: One noteworthy new class of agents that has yielded durable responses is programmed death (PD)-1 inhibitors, which target a T-lymphocyte checkpoint and are heralding a resurgence of immunotherapy.


Input: Finally, optimal therapy for non-clear cell RCC remains to be delineated, although sunitinib, everolimus and other VEGFR-TKI or mTOR inhibitors have all demonstrated modest benefit.

sunitinib

everolimus


Input: Multiple gene polymorphisms can improve prediction of non-vertebral fracture in postmenopausal women.


Input: Clinical risk factors (CRFs), with or without bone mineral density (BMD), are used to determine the risk of osteoporotic fracture (OF), which has a heritable component.


Input: This study investigated whether genetic profiling can additionally improve the ability to predict OF.


Input: Using 1, 229 unrelated Korean postmenopausal women, 39 single-nucleotide polymorphisms (SNPs) in 30 human genomic loci were tested for association with osteoporosis-related traits, such as BMD, osteoporosis, vertebral fracture (VF), non-vertebral fracture (NVF), and any fracture.


Input: To estimate the effects of genetic profiling, the genetic risk score (GRS) was calculated using five prediction models: (model I) GRSs only; (model II) BMD only; (model III) CRFs only; (model IV) CRFs and BMD; and (model V) CRFs, BMD and GRS.


Input: A total of 21 SNPs within 19 genes associated with one or more osteoporosis-related traits and were included for GRS calculation.


Input: GRS associated with BMD before and after adjustment for CRFs (P = < 0. 001 to 0. 018).


Input: GRS associated with NVF before and after adjustment for CRFs and BMD (P = 0. 017 to 0. 045), and with any fracture after adjustment for CRFs and femur neck BMD (P = 0. 049).


Input: In terms of predicting NVF, the area under the receptor-operator characteristics curve (AUC) for model I was 0. 55, which was lower than the AUCs of models II (0. 60), III (0. 64), and IV (0. 65).


Input: Adding GRS to model IV (in model V) increased the AUC to 0. 67, and improved the accuracy of NVF classification by 11. 5% (P = 0. 014).


Input: In terms of predicting any fracture, the AUC of model V (0. 68) was similar to that of model IV (0. 68), and model V did not significantly improve the accuracy of any fracture classification (P = 0. 39).


Input: Thus, genetic profiling may enhance the accuracy of NVF predictions and help to delineate the intervention threshold.


Input: Design and in vitro evaluation of a novel polymeric excipient for buccal applications.


Input: Background: The objective of this study was to develop and evaluate a more effective mucoadhesive thiomer for buccal drug-delivery systems.


Input: Methods: 2-iminothiolane was covalently attached to a chitosan backbone.


Input: A preactivation step followed, mediated by 6, 6' dithionicotinamide, thiol groups were modified by disulfide bonds formation.

6, 6' dithionicotinamide

thiol

disulfide


Input: Mucoadhesion studies were performed on buccal mucosa.


Input: In addition, water-uptake capacity, disintegration, release and cytotoxicity studies were completed.


Input: Results: The obtained chitosan-thiobutylamidine conjugate displayed 647. 4 +/- 85. 23 micro mol/g immobilized thiol groups.

thiobutylamidine


Input: Due to the preactivation, approximately 60% of thiol groups were modified by formation of disulfide bonds.

disulfide


Input: Chitosan-thiobutylamidine-mercaptonicotinamide displayed 1. 8-fold higher stability and 1. 6-fold higher mucoadhesive properties, respectively.

thiobutylamidine

mercaptonicotinamide


Input: The release study demonstrated a 1. 4-fold more prolonged drug release compared with corresponding thiomers.


Input: Conclusion: According to these results, preactivated thiomers demonstrate an improved stability and increased mucoadhesive properties.


Input: Therefore, they seem to be advantageous for buccal administration over corresponding thiomers and chitosan.


Input: Present and future approaches to screening of G-protein-coupled receptors.


Input: As G-protein-coupled receptors (GPCRs) mediate a multitude of cellular signal transduction events, affecting more or less all human disease areas, it is, therefore, no surprise that they comprise the largest family of current drug targets.


Input: Screening of compounds interacting with GPCRs has developed during the past decade from receptor binding assays, to various functional determination of coupling to G-proteins, and, more recently, G-protein-independent signal transduction events.


Input: Additional opportunities have been presented in drug discovery through novel pharmacological properties obtained for receptor dimers and by identification of ligands for orphan GPCRs.


Input: Furthermore, high-throughput formats and automation has substantially facilitated and accelerated the screening process providing powerful tools in improving modern drug discovery.


Input: Organic Solvent-Based Graphene Oxide Liquid Crystals: A Facile Route toward the Next Generation of Self-Assembled Layer-by-Layer Multifunctional 3D Architectures.

Graphene Oxide


Input: We introduce soft self-assembly of ultralarge liquid crystalline (LC) graphene oxide (GO) sheets in a wide range of organic solvents overcoming the practical limitations imposed on LC GO processing in water.

graphene oxide


Input: This expands the number of known solvents which can support amphiphilic self-assembly to ethanol, acetone, tetrahydrofuran, N-dimethylformamide, N-cyclohexyl-2-pyrrolidone, and a number of other organic solvents, many of which were not known to afford solvophobic self-assembly prior to this report.

ethanol

acetone

tetrahydrofuran

N-dimethylformamide


Input: The LC behavior of the as-prepared GO sheets in organic solvents has enabled us to disperse and organize substantial amounts of aggregate-free single-walled carbon nanotubes (SWNTs, up to 10 wt%) without compromise in LC properties.

carbon


Input: The as-prepared LC GO-SWNT dispersions were employed to achieve self-assembled layer-by-layer multifunctional 3D hybrid architectures comprising SWNTs and GO with unrivalled superior mechanical properties (Young' s modulus in excess of 50 GPa and tensile strength of more than 500 MPa).


Input: Helicity as a Steric Force: Stabilization and Helicity-Dependent Reversion of Colored o-Quinonoid Intermediates of Helical Chromenes.

o-Quinonoid


Input: Photolysis of regioisomeric helical chromenes 1 and 2 leads to colored reactive intermediates.


Input: While the latter generally decay quite rapidly, they are found to be longer lived in 1 and highly persistent in 2.


Input: The remarkable stability of the otherwise fleeting transient in 2 allowed isolation and structural characterization by X-ray crystallography.


Input: The structural analyses revealed that steric force inherent to the helical scaffold is the origin of stability as well as differentiation in the persistence of the intermediates of 1 and 2 (1Q and 2Q).


Input: The structure further shows that diphenylvinyl moiety in the TT isomer of 2Q gets splayed over the helical scaffold such that it is fraught with a huge steric strain to undergo required bond rotations to regenerate the precursor chromene.

diphenylvinyl


Input: Otherwise, reversion of 2Q was found to occur at higher temperatures.


Input: Aazahelical chromenes 3 and 4 with varying magnitudes of helicity were designed in pursuit of o-quinonoid intermediates with graded activation barriers.

o-quinonoid


Input: Their photogenerated intermediates 3Q and 4Q were also isolated and structurally characterized.


Input: The activation barriers for thermal reversion of 2Q-4Q, as determined from Arrhenius and Eyring plots, are found to correlate nicely with the helical turn, which decisively determines the steric force.


Input: The exploitation of helicity is thus demonstrated to develop a novel set of photoresponsive helicenes 2-4 that lead to colored intermediates exhibiting graded stability.


Input: It is further shown that the photochromism of 2-4 in conjunction with response of 2Q-4Q to external stimuli (acid, heat, and visible radiation) permits development of molecular logic gates with INHIBIT function.


Input: Screening and Structural Analysis of Flavones Inhibiting Tankyrases.

Flavones


Input: Flavonoids are known for their beneficial effects on human health, and therefore the therapeutic potential of these compounds have been extensively studied.

Flavonoids


Input: Flavone has been previously identified as a tankyrase inhibitor, and to further elucidate whether tankyrases would be inhibited by other flavonoids, we performed a systematic screening of tankyrase 2 inhibitory activity using 500 natural and naturally derived flavonoids covering nine different flavonoid classes.

Flavone

flavonoids

flavonoids

flavonoid


Input: All identified tankyrase inhibitors were flavones.

flavones


Input: We report crystal structures of all the hit compounds in complex with the catalytic domain of human tankyrase 2.


Input: Flavone derivatives in all 10 crystal structures bind to the nicotinamide binding site of tankyrase 2.

Flavone

nicotinamide


Input: Potencies of the active flavones toward tankyrases vary between 50 nM and 1. 1 mu M, and flavones show up to 200-fold selectivity for tankyrases over ARTD1.

flavones

flavones


Input: The molecular details of the interactions revealed by cocrystal structures efficiently describe the properties of potent flavone derivatives inhibiting tankyrases.

flavone


Input: Alexander b o hm (1971-2012).


Input: On November 28, 2012 Alexander (Alex) B o hm, a bacterial geneticist, died at age 41, only a few months after taking up a position as an assistant professor at the LOEWE Center for Synthetic Microbiology in Marburg, Germany.


Input: Earlier in 2012 Alex had been diagnosed with an aggressive form of thyroid cancer that left him little time to live his scientific and personal dreams.


Input: Water-Mediated Interactions Influence the Binding of Thapsigargin to Sarco/Endoplasmic Reticulum Calcium Adenosinetriphosphatase.

Thapsigargin

Calcium


Input: A crystal structure suggests four water molecules are present in the binding cavity of thapsigargin in sarco/endoplasmic reticulum calcium ATPase (SERCA).

thapsigargin

calcium


Input: Computational chemistry indicates that three of these water molecules mediate an extensive hydrogen-bonding network between thapsigargin and the backbone of SERCA.

hydrogen

thapsigargin


Input: The orientation of the thapsigargin molecule in SERCA is crucially dependent on these interactions.

thapsigargin


Input: The hypothesis has been verified by measuring the affinity of newly synthesized model compounds, which are prevented from participating in such water-mediated interactions as hydrogen-bond donors.

hydrogen


Input: Water-Soluble Polymer Exfoliated Graphene: As Catalyst Support and Sensor.

Graphene


Input: In this paper, we obtained various water-soluble polymer functionalized graphene in dimethyl sulfoxide under ultrasonication.

graphene

dimethyl sulfoxide


Input: The atomic force microscope analysis and control experiment shows the water-soluble polymer is the crucial part to help solvent molecules separate interlayer.


Input: Such polymer/graphene exhibits high conductivity and tunable surface property, as confirmed by the selected area electron diffraction and Raman and electrochemical impedance spectroscopy.

graphene


Input: As a result, a catalyst based on polyvinyl pyrrolidone (PVP)/graphene shows better methanol oxidation performance than that based on PVP/reduced graphene oxide.

polyvinyl pyrrolidone

PVP

graphene

methanol

PVP

graphene oxide


Input: By changing to another polymer, poly (4-vinylpyridine)/graphene shows a stable and reversible response to pH, and demonstrates its potential for sensor application.

poly (4-vinylpyridine)

graphene


Input: Detection of Nitrogen-Protonated Nitrous Oxide (HNNO (+)) by Rotational Spectroscopy.

Nitrogen

Protonated Nitrous Oxide

HNNO (+)


Input: The rotational spectrum of nitrogen-protonated nitrous oxide (HNNO (+)), an isomer whose existence was first inferred from kinetic studies more than 30 years ago, has now been detected by Fourier transform microwave spectroscopy, guided by new high-level coupled-cluster calculations of its molecular structure.

nitrogen

protonated nitrous oxide

HNNO (+)


Input: From high-resolution measurements of the hyperfine splitting in its fundamental rotational transition, the rotational constant (B + C)/2 and the quadrupole tensor element chi aa (N) for both nitrogen atoms have been precisely determined.

N

nitrogen


Input: The derived constants agree well with quantum-chemical calculations here and others in the literature.


Input: The chi aa (N) values for the two isomers of protonated nitrous oxide are qualitatively consistent with the valence bond description of H-N = N (+) = O for the electronic structure of the nitrogen-protonated form and N = N (+)-O-H for the oxygen-protonated form.

N

protonated nitrous oxide

H-N = N (+) = O

nitrogen

N = N (+)-O-H

oxygen


Input: HNNO (+) is found to be 2-4 times less abundant than NNOH (+) under a range of experimental conditions, as might be expected because this metastable isomer is known to be only ~ 6 kcal mol (-1) less stable than ground-state NNOH (+) from kinetic measurements by Ferguson and co-workers.

HNNO (+)

NNOH (+)

NNOH (+)


Input: Immunopathology of rheumatoid arthritis.


Input: Rheumatoid arthritis (RA) is one of the most common autoimmune diseases.


Input: Genetic and epidemiologic studies point to a relevant role of adaptive T-cell response interactions with environmental factors such as smoking in the immunopathogenesis of the disease.


Input: These interactions result in a specific systemic autoantibody response that seems to contribute to the synovial inflammatory process.


Input: The reasons for specific localization of the autoimmune proinflammatory process to synovial tissue remain poorly known, but relevant local effector mechanisms have been recently unveiled and successfully targeted by new specific therapies.


Input: A relevant role for cytokine networks, where TNF-alpha displays a pivotal role, has been confirmed.


Input: The local pathology is hallmarked by immune cell accumulation and expansion of resident stromal and vascular cells.


Input: Crosstalk between these elements generates an aggressive environment that leads to cartilage and bone destruction. RA provides represents a model for systemic T-cell mediated systemic autoimmunity leading to local cellular and autoantibody mediated chronic inflammation.


Input: Whereas targeting of these elements with specific antagonists may interfere with the disease process, reestablishing tolerance and preventing further synovial inflammation has not been achieved.


Input: Safety evaluation of desloratadine in allergic rhinitis.

desloratadine


Input: Introduction: Desloratadine is a biologically active metabolite of second-generation antihistamine loratadine.

Desloratadine

loratadine


Input: It is also indicated for the treatment of allergic diseases, including allergic rhinitis.


Input: Areas covered: A Medline search was conducted to identify preclinical and clinical studies of desloratadine.

desloratadine


Input: This was supplemented with additional articles obtained from online sources.


Input: The focus of this review is on the safety profile of desloratadine.

desloratadine


Input: Expert opinion: The review of these data indicates that the safety profile of desloratadine is similar to other second-generation antihistamines.

desloratadine


Input: Desloratadine is highly selective for histamine H1-receptors, does not cross the blood-brain barrier (BBB), and has minimal adverse events (very low sedation rate), with a better safety and tolerability than first-generation antihistamines.

Desloratadine

histamine


Input: Desloratadine is safe and well tolerated without having central nervous system (CNS) or cardiovascular effects and with low drug interaction.

Desloratadine


Input: Proposed diagnostic criteria for subclinical Cushing' s syndrome associated with adrenal incidentaloma.


Input: Subclinical Cushing' s syndrome (SCS) associated with adrenal incidentaloma is usually characterized by autonomous cortisol secretion without overt symptoms of Cushing' s syndrome (CS).

cortisol


Input: Although the diagnostic criteria for SCS differ among countries, the 1 mg dexamethasone suppression test (DST) is essential to confirm the presence and the extent of cortisol overproduction.

dexamethasone

cortisol


Input: Since 1995, SCS has been diagnosed in Japan based on serum cortisol levels >= 3 mu g/dl (measured by radioimmunoassay [RIA]) after a 1 mg DST.

cortisol


Input: However, the increasing use of enzyme immunoassays (EIA) instead of RIA has hindered the diagnosis of SCS because of the differing sensitivities of commercially available assays, particularly for serum cortisol levels of around 3 mu g/dl.

cortisol


Input: One way to overcome this problem is to lower the cortisol threshold level after a 1 mg DST.

cortisol


Input: In the present study, we examined the clinical applicability of lowering the cortisol threshold to 1. 8 mu g/dl, similar to the American Endocrine Society' s guidelines for CS, by reanalyzing 119 patients with adrenal incidentaloma.

cortisol


Input: Our findings indicate that serum cortisol levels >= 1. 8 mu g/dl after 1 mg DST are useful to confirm the diagnosis of SCS if both of the following criteria are met: (1) basal ACTH level < 10 pg/ml (or poor plasma ACTH response to corticotrophin-releasing hormone) and (2) serum cortisol >= 5 mu g/dl at 21: 00 to 23: 00 h.

cortisol

cortisol


Input: If only one of (1) and (2) are met, we recommend that other clinical features are considered in the diagnosis of SCS, including serum dehydroepiandrosterone sulfate levels, urine free cortisol levels, adrenal scintigraphy, and clinical manifestation.

dehydroepiandrosterone sulfate

cortisol


Input: Synthesis, Antidepressant Evaluation and Docking Studies of Long-Chain Alkylnitroquipazines as Serotonin Transporter Inhibitors.

Alkylnitroquipazines

Serotonin


Input: Twelve alkyl analogues (1-12) of the high-affinity serotonin transporter (SERT) inhibitor 6-nitroquipazine (6-NQ) were synthesized and studied using in vitro radioligand competition binding assays to determine their binding affinity (Ki).

alkyl

serotonin


Input: The putative antidepressant activity of five of the binders with the highest SERT binding affinities was studied by the forced swim and locomotor activity mouse tests.


Input: The three-dimensional (3D) structures of 8 and 9 were determined using NOE NMR technique.


Input: Flexible docking of the compounds was undertaken to illustrate the binding of the compounds in the SERT model.


Input: Our results showed that several of the 6-NQ analogues are high-affinity SERT inhibitors and indicated that the octyl (8), decyl (10) and dodecyl (12) 6-NQ analogues exhibit moderate antidepressant activity.

octyl

decyl

dodecyl


Input: Vortex domain structures of an epitaxial ferroelectric nanodot and its temperature-misfit strain phase diagram.


Input: Phase field simulations were conducted to investigate the effect of misfit strain on the vortex domain structure (VDS) in a BaTiO3 nanodot.


Input: Taking into account the effect of inhomogeneous eletromechanical fields, ambient temperature and surface effects, our calculations demonstrate a strong effect of misfit strain on the orientation and magnitude of the polarization dipoles.


Input: As a consequence, fruitful equilibrium vortex domain patterns can be obtained by adjusting the epitaxial misfit strain between the substrate and the nanodot.


Input: While the nanodot exhibits a single transition from a paraelectric to a near-rhombohedral vortex state at zero misfit strain with the decrease of temperature, complicated transformations of vortex domain patterns are found under nonzero misfit strain.


Input: Typically, orthorhombic, tetragonal and several unreported vortex domain patterns (e. g., with zero toroidal moment) are found.


Input: Moreover, misfit strain-induced transformations into these domain patterns are also predicted for a ferroelectric nanodot with initial near-rhombohedral vortex state.


Input: Combining effects of the ambient temperature and misfit strain, a " temperature-misfit strain " phase-diagram depicting the fruitful vortex domain patterns of the nanodot was obtained.


Input: Our simulations indicate promising application of strain engineering in controlling the VDS in ferroelectric nanostructures.


Input: Metabolomics reveals trichloroacetate as a major contributor to trichloroethylene-induced metabolic alterations in mouse urine and serum.

trichloroacetate

trichloroethylene


Input: Trichloroethylene (TCE)-induced liver toxicity and carcinogenesis is believed to be mediated in part by activation of the peroxisome proliferator-activated receptor alpha (PPAR alpha).

Trichloroethylene

TCE


Input: However, the contribution of the two TCE metabolites, dichloroacetate (DCA) and trichloroacetate (TCA) to the toxicity of TCE, remains unclear.

TCE

dichloroacetate

DCA

trichloroacetate

TCA

TCE


Input: The aim of the present study was to determine the metabolite profiles in serum and urine upon exposure of mice to TCE, to aid in determining the metabolic response to TCE exposure and the contribution of DCA and TCA to TCE toxicity.

TCE

TCE

DCA

TCA

TCE


Input: C57BL/6 mice were administered TCE, TCA, or DCA, and urine and serum subjected to ultra-performance liquid chromatography coupled with electrospray ionization quadrupole time-of-flight mass spectrometry (UPLC-ESI-QTOFMS)-based global metabolomics analysis.

TCE

TCA

DCA


Input: The ions were identified through searching metabolomics databases and by comparison with authentic standards, and quantitated using multiple reactions monitoring.


Input: Quantitative polymerase chain reaction of mRNA, biochemical analysis, and liver histology were also performed.


Input: TCE exposure resulted in a decrease in urine of metabolites involved in fatty acid metabolism, resulting from altered expression of PPAR alpha target genes.

TCE

fatty acid


Input: TCE treatment also induced altered phospholipid homeostasis in serum, as revealed by increased serum lysophosphatidylcholine 18: 0 and 18: 1, and phosphatidylcholine metabolites.

TCE

lysophosphatidylcholine 18: 0 and 18: 1

phosphatidylcholine


Input: TCA administration revealed similar metabolite profiles in urine and serum upon TCE exposure, which correlated with a more robust induction of PPAR alpha target gene expression associated with TCA than DCA treatment.

TCA

TCE

TCA

DCA


Input: These data show the metabolic response to TCE exposure and demonstrate that TCA is the major contributor to TCE-induced metabolite alterations observed in urine and serum.

TCE

TCA

TCE


Input: Boron Enhances Odontogenic and Osteogenic Differentiation of Human Tooth Germ Stem Cells (hTGSCs) In Vitro.

Boron


Input: Stem cell technology has been a great hope for the treatment of many common problems such as Parkinson' s disease, Alzheimer' s disease, diabetes, cancer, and tissue regeneration.


Input: Therefore, the main challenge in hard tissue engineering is to make a successful combination of stem cells and efficient inductors in the concept of stem cell differentiation into odontogenic and osteogenic cell types.


Input: Although some boron derivatives have been reported to promote bone and teeth growth in vivo, the molecular mechanism of bone formation has not been elucidated yet.

boron


Input: Different concentrations of sodium pentaborate pentahydrate (NaB) were prepared for the analysis of cell toxicity and differentiation evaluations.

sodium pentaborate pentahydrate

NaB


Input: The odontogenic, osteogenic differentiation and biomineralization of human tooth germ stem cells (hTGSCs) were evaluated by analyzing the mRNA expression levels, odontogenic and osteogenic protein expressions, alkaline phosphatase (ALP) activity, mineralization, and calcium deposits.

calcium


Input: The NaB-treated group displayed the highest ALP activity and expression of osteo-and odontogenic-related genes and proteins compared to the other groups and baseline.

NaB


Input: In the current study, increased in vitro odontogenic and osteogenic differentiation capacity of hTGSCs by NaB application has been shown for the first time.

NaB


Input: The study offers considerable promise for the development of new scaffold systems combined with NaB in both functional bone and tooth tissue engineering.

NaB


Input: Cryptococcal infections: changing epidemiology and implications for therapy.


Input: Although the incidence of HIV-associated cryptococcosis has decreased in developed countries since the introduction of antiretroviral therapy, this disease continues to cause significant morbidity and mortality in sub-Saharan Africa among patients with AIDS.


Input: Important strides have been made in an attempt to decrease the burden of disease, particularly the development of the lateral flow assay cryptococcal antigen (LFA CrAg) as a diagnostic tool in resource-limited settings, coupled with the introduction of pre-emptive treatment with fluconazole for HIV-positive patients at risk for cryptococcosis with a positive LFA CrAg.

fluconazole


Input: Among solid organ transplant recipients, recent prospective studies have identified cryptococcosis as the third most common invasive fungal infection, and progress is being made toward earlier diagnosis and more effective therapy.


Input: Finally, the Cryptococcus gattii outbreak in British Columbia, Canada and the US Pacific Northwest is providing important new insights into the emergence of this pathogen in geographic areas previously considered low risk for acquisition of infection.


Input: Understanding the similarities and differences among C. gattii and C. neoformans infections will provide critical insights into the behavior of these organisms in the human host.


Input: Both pathogens affect immunocompetent and immunosuppressed hosts, causing pulmonary, central nervous system and widely disseminated infections.


Input: Treatment recommendations in the future will necessarily take into account the site of infection, clinical severity of the infection, Cryptococcus species, host immune status and economic resources.


Input: Protective effects of green tea on antioxidative biomarkers in chemical laboratory workers.


Input: Chemical materials are environmental contaminants, are extensively used in laboratories, and may cause various forms of health hazards in laboratory workers.


Input: Therefore, this toxicity most likely is a result of the oxidative metabolism of chemical to reactive products.


Input: As green tea (GT) possesses antioxidant effects, the objective of this study was to examine any amelioration oxidative stress in chemical laboratory workers drinking one cup (3 g/300 ml water) of freshly prepared tea once daily.


Input: Baseline characteristics including age, sex, smoking, fruit consumption, and duration of exposure were recorded via questionnaire to the subjects.


Input: Saliva level oxidative stress parameters such as total antioxidant capacity (TAC), glutathione peroxidase (GPx), catalase (CAT), and superoxide dismutase (SOD) were estimated before and after consumption of GT in these workers.

glutathione

superoxide


Input: Treatment of subjects with GT induced a significant reduction in saliva GPx activity (406. 61 +/- 22. 07 vs. 238. 96 +/- 16. 26 U/l p = 0. 001) and induction in TAC (0. 46 +/- 0. 029 mu mol/ml vs. 0. 56 +/- 0. 031, p = 0. 016).


Input: No statistically significant alteration was found for saliva SOD (0. 080 +/- 0. 0019 vs. 0. 079 +/- 0. 0014, p > 0. 05) and CAT (20. 36 +/- 0. 69 vs. 19. 78 +/- 0. 71, p > 0. 05) after 28 days treatment by GT.


Input: These results demonstrate that drinking GT during chemical exposure can reduce several parameters indicative of oxidative stress.


Input: In conclusion, using GT as a dietary supplement can be a rational protocol to control source of hazards in chemical laboratory workers.


Input: Attenuation of Gouty Arthritis by Emodinol in Monosodium Urate Crystal-Treated Mice.

Emodinol

Monosodium Urate


Input: A series of studies have recently demonstrated that the release of interleukin 1 beta induced by monosodium urate crystals is central to the experimental gouty arthritis.

monosodium urate


Input: Elaeagnus pungens has been traditionally used for the treatment of gouty arthritis in China for more than thousands years.


Input: However, there is still little known about the active ingredients and mechanisms of E. pungens against gouty arthritis.


Input: Emodinol, as a major triterpene compound in E. pungens, has been seldom reported to have an effect on gouty arthritis.

Emodinol

triterpene


Input: Therefore, the potential beneficial effects and mechanisms of emodinol on gouty arthritis were investigated in this study.

emodinol


Input: Results showed that it significantly ameliorated the hyperalgesia, inflammation, and levels of multiple proinflammatory cytokines in monosodium urate crystals-treated mice.

monosodium urate


Input: These findings elucidate that emodinol exhibits a prominent effect on improving symptoms of acute gouty arthritis induced by monosodium urate crystals through inhibiting the generation of proinflammatory cytokines.

emodinol

monosodium urate


Input: Dioecy in Plants-Is It an Important Factor for Phytochemists to Consider?


Input: Plants with separate male and female flowers are termed dioecious.


Input: Dioecy is not rare, yet is a characteristic that could potentially impact the phytochemical and subsequent pharmacological properties of a species.


Input: This is a brief insight which highlights why the sex of the plant might be an important factor to consider for researchers within phytochemistry related fields.


Input: Scanning protein analysis of electrofocusing gels using X-ray fluorescence.


Input: Recently, " metallomics, " in addition to genomics and proteomics, has become a focus as a novel approach to identify sensitive fluctuations in homeostasis that accompany metabolic processes, such as stress responses, differentiation, and proliferation.


Input: Cellular elements and associated protein behavior provide important clues for understanding cellular and disease mechanism (s).


Input: It is important to develop a system for measuring the native status of the protein.


Input: In this study, we developed an original freeze-dried electrofocusing native gel over polyimide film (native-gel film) for scanning protein analysis using synchrotron radiation excited X-ray fluorescence (SPAX).

polyimide


Input: To our knowledge, this is the first report detailing the successful mapping of metal-associated proteins of electrofocusing gels using X-ray fluorescence.


Input: SPAX can provide detection sensitivity equivalent to that of LA-ICP-MS.


Input: In addition to this increased sensitivity, SPAX has the potential to be combined with other X-ray spectroscopies.


Input: Our system is useful for further applications in proteomics investigating cellular element-associated protein behaviors and disease mechanisms.


Input: Simultaneous two and three photon resonant enhancement of third-order NLO susceptibility in an azo-dye functionalized polymer film.

azo


Input: We report the observation of simultaneous two and three photon resonances, enhancing the third-order NLO susceptibility in a thin film of an azo-dye polymer.

azo


Input: The possibility of 2-3 orders of magnitude increase in chi ((3)) susceptibility is sustained by quantum mechanical calculations.


Input: This improves the applications of azo-polymers in all optical signal processing as well as in nonlinear optical imaging.

azo


Input: The lifetime and efficiency of triplet-triplet fluorescence from the excited state of a TMM biradical determined using transient emission spectroscopy by two-color two-laser flash photolysis.

TMM


Input: The single laser flash photolysis (FP) of 2-(4-benzoylphenyl)-2-phenyl-1-methylenecyclopropane gave rise to a ground state trimethylenemethane (TMM) biradical with absorption bands at 362 and 545 nm and an excited state of this biradical that displays triplet-triplet fluorescence at 580 nm.

2-(4-benzoylphenyl)-2-phenyl-1-methylenecyclopropane

trimethylenemethane

TMM


Input: The excited biradical is likely formed via an expected two-photon process as well as an unexpected one-photon process.


Input: The fluorescence quantum yield of the excited biradical, 0. 021, was successfully determined by employing a two-color two-laser FP technique.


Input: The PIM Family of Serine/Threonine Kinases in Cancer.

Serine

Threonine


Input: The proviral insertion site in Moloney murine leukemia virus, or PIM proteins, are a family of serine/threonine kinases composed of three different isoforms (PIM1, PIM2, and PIM3) that are highly evolutionarily conserved.

serine

threonine


Input: These proteins are regulated primarily by transcription and stability through pathways that are controlled by Janus kinase/Signal transducer and activator of transcription, JAK/STAT, transcription factors.


Input: The PIM family proteins have been found to be overexpressed in hematological malignancies and solid tumors, and their roles in these tumors were confirmed in mouse tumor models.


Input: Furthermore, the PIM family proteins have been implicated in the regulation of apoptosis, metabolism, cell cycle, and homing and migration, which has led to the postulation of these proteins as interesting targets for anticancer drug discovery.


Input: In the present work, we review the importance of PIM kinases in tumor growth and as drug targets.


Input: Congruence of Phytochemical and Morphological Profiles along an Altitudinal Gradient in Origanum vulgare ssp. vulgare from Venetian Region (NE Italy).


Input: Plants of Origanum vulgare L. ssp.


Input: vulgare from the Veneto region (NE Italy) were selected to study the variability of the essential-oil composition from leaves and inflorescences throughout an elevation gradient.


Input: We investigated also the morphology of non-glandular and glandular trichomes, their distribution on the vegetative and reproductive organs, as well as the histochemistry of the secreted products, with special focus on the terpenoidic fraction.


Input: Since glandular trichomes are prerequisite for the essential-oil synthesis, the second objective was to establish whether its production is related to glandular hair number, and density.


Input: Essential-oil contents decline with increasing altitude, and the micromorphological observations revealed a decrease in trichome density along the same direction.


Input: Moreover, GC/MS analysis together with principal component analysis (PCA) showed that the three investigated populations were significantly different in chemical composition.


Input: Therefore, an important interpopulation variability for low-, mid-, and high-altitude sites was established, suggesting the likely occurrence of different biotypes associated with altitudinal levels.


Input: Hence, the involvement of abiotic factors such as temperature and drought in the chemical polymorphism of O. vulgare associated with elevation is briefly discussed.


Input: Configurational Assignment of Secondary Hydroxyl Groups and Methyl Branches in Polyketide Natural Products through Bioinformatic Analysis of the Ketoreductase Domain.

Hydroxyl

Methyl


Input: Profile hidden Markov models (HMMs) were used to predict the configuration of secondary alcohols and alpha-methyl branches of modular polyketides.

secondary alcohols

alpha-methyl


Input: Based on the configurations of two chiral centers in these polyketides, 78 ketoreductases were classified into four different types of polyketide producers.


Input: The identification of positions that discriminate between these protein families was followed by fitting six profile HMMs to the data set and the corresponding subsets, to model the conserved regions of the protein types.


Input: Ultimately, the profile HMMs described herein predict protein subtypes based on the complete information-rich region; consequently, slight changes in a multiple sequence alignment do not significantly alter the outcome of this classification method.


Input: Additionally, Viterbi scores can be used to assess the reliability of the classification.


Input: Identification and Characterization of a Cellulose Binding Heptapeptide Revealed by Phage Display.

Heptapeptide


Input: Cellulose nanowhiskers (CNWs) were used in conjunction with phage display technology to identify polypeptides which bind the crystalline region of cellulose.


Input: A consensus peptide WHWTYYW was identified to efficiently bind the CNWs.


Input: The binding affinities of specific phage particles were assessed using biopanning assays and enzyme-linked immunosorbent assay (ELISA).


Input: The WHWTYYW peptide was synthesized and isothermal titration calorimetry (ITC) analysis showed that the peptide exhibited a binding constant of ~ 10 (5) M (-1) toward the crystalline CNWs.


Input: In order to understand how the affinity of this peptide differs for non-crystalline cellulose, binding properties were characterized using cello-oligosaccharides as substrates.


Input: Binding analysis was performed using UV spectroscopy and fluorescence quenching experiments.


Input: The specific molecular interactions of the WHWTYYW peptide with cellohexaose were examined using nuclear magnetic resonance (NMR).

cellohexaose


Input: Interactions of this peptide with crystalline cellulose were also investigated using computational molecular modeling (MM) studies.


Input: The MM and NMR experiments indicate that the WHWTYYW peptide exhibits a bent structure when bound, allowing the Y5 amino acid to form a CH/pi stacking interaction and H-bond with the glucose ring of cellulose.

amino acid

CH

H

glucose


Input: Probing the Mechanism of TBAF-Catalyzed Deacylation of Cellulose Esters.

TBAF

Esters


Input: The mechanism of the recently discovered, unusual tetrabutylammonium fluoride (TBAF) deacylation of cellulose esters has been investigated by methods including kinetic isotope effect (KIE) studies.

tetrabutylammonium fluoride

TBAF


Input: The secondary KIE (kH/kD = 1. 26 +/- 0. 04) measured for deacylation at C-2/3 suggests a mechanism involving a ketene intermediate for those positions.


Input: An inverse KIE (kH/kD = 0. 87 +/- 0. 03) for the deacylation at C-6 indicates the involvement of a tetrahedral intermediate in the mechanism.


Input: Additional studies suggest the possibility that TBAF chelation by neighboring acyl groups may account for the unexpected regioselectivity at the secondary alcohol esters that is observed in the TBAF deacylation of cellulose esters.

TBAF

acyl

secondary alcohol esters

TBAF

esters


Input: Liquid/Gas and Liquid/Liquid Phase Equilibria of the System Water/Bovine Serum Albumin.


Input: The thermodynamic behavior of the system H2O/BSA was studied at 25 degrees C within the entire composition range: vapor pressure measurements via head space sampling gas chromatography demonstrate that the attainment of equilibria takes more than one week.


Input: A miscibility gap was detected via turbidity and the coexisting phases were analyzed.


Input: At 6 degrees C the two phase region extends from ca.


Input: 34 to 40 wt% BSA; it shrinks upon heating.


Input: The polymer rich phase is locally ordered, as can be seen under the optical microscope using crossed polarizers.


Input: The Flory-Huggins theory turns out to be inappropriate for the modeling of experimental results.


Input: A phenomenological expression is employed which uses three adjustable parameters and describes the vapor pressures quantitatively; it also forecasts the existence of a miscibility gap.


Input: Monitoring Controlled Release of Payload from Gold Nanocages Using Surface Enhanced Raman Scattering.


Input: Novel organic and inorganic nanostructures for localized and externally triggered delivery of therapeutic agents at a target site have received immense attention over the past decade owing to their enormous potential in treating complex diseases such as cancer.


Input: Gold nanocages, a novel class of hollow plasmonic nanostructures, have been recently demonstrated to serve as carriers for the delivery of payload with external trigger such as light or ultrasound.


Input: In this article, we demonstrate that surface enhanced Raman spectroscopy (SERS) can be employed to noninvasively monitor the release of payload from these hollow plasmonic nanostructures.


Input: The large enhancement of electromagnetic (EM) field at the interior surface of these nanostructures enables us to monitor the controlled release of Raman-active cargo from nanocages.


Input: Considering that SERS can be excited and collected in near-infrared (NIR) therapeutic window, this technique can serve as a powerful tool to monitor the drug release in vivo, providing additional control over externally triggered drug administration.


Input: Carcinogenicity Prediction of Noncongeneric Chemicals by a Support Vector Machine.


Input: The ability to identify carcinogenic compounds is of fundamental importance to the safe application of chemicals.


Input: In this study, we generated an array of in silico models allowing the classification of compounds into carcinogenic and noncarcinogenic agents based on a data set of 852 noncongeneric chemicals collected from the Carcinogenic Potency Database (CPDBAS).


Input: Twenty-four molecular descriptors were selected by Pearson correlation, F-score, and stepwise regression analysis.


Input: These descriptors cover a range of physicochemical properties, including electrophilicity, geometry, molecular weight, size, and solubility.


Input: The descriptor mutagenic showed the highest correlation coefficient with carcinogenicity.


Input: On the basis of these descriptors, a support vector machine-based (SVM) classification model was developed and fine-tuned by a 10-fold cross-validation approach.


Input: Both the SVM model (Model A1) and the best model from the 10-fold cross-validation (Model B3) runs gave good results on the test set with prediction accuracy over 80%, sensitivity over 76%, and specificity over 82%.


Input: In addition, extended connectivity fingerprints (ECFPs) and the Toxtree software were used to analyze the functional groups and substructures linked to carcinogenicity.


Input: It was found that the results of both methods are in good agreement.


Input: Natural Products Containing a Nitrogen-Nitrogen Bond.

Nitrogen

Nitrogen


Input: As of early 2013, over 200 natural products are known to contain a nitrogen-nitrogen (N-N) bond.

nitrogen

nitrogen

N-N


Input: This report categorizes these compounds by structural class and details their isolation and biological activity.


Input: Synthesis and Self-assembly of Amphiphilic Homoglycopolypeptide.


Input: The synthesis of the amphiphilic homoglycopolypeptide was carried out by a combination of NCA polymerization and click chemistry to yield a well-defined polypeptide having an amphiphilic carbohydrate on its side chain.

carbohydrate


Input: The amphiphilicity of the carbohydrate was achieved by incorporation of an alkyl chain at the C-6 position of the carbohydrate thus also rendering the homoglycopolypeptide amphiphilic.

carbohydrate

alkyl

carbohydrate


Input: The homoglycopolypeptide formed multimicellar aggregates in water above a critical concentration of 0. 9 mu M due to phase separation.


Input: The multimicellar aggregates were characterized by DLS, TEM, and AFM.


Input: It is proposed that hydrophobic interactions of the aliphatic chains at the 6-position of the sugar moieties drives the assembly of these rod-like homoglycopolypeptide into large spherical aggregates.

sugar


Input: These multimicellar aggregates encapsulate both hydrophilic as well as hydrophobic dye as was confirmed by confocal microscopy.


Input: Finally, amphiphilic random polypeptides containing 10% and 20% alpha-d-mannose in addition to glucose containing a hydrophobic alkyl chain at its 6 position were synthesized by our methodology, and these polymers were also found to assemble into spherical nanostructures.

alpha-d-mannose

glucose

alkyl


Input: The spherical assemblies of amphiphilic random glycopolypeptides containing 10% and 20% mannose were found to be surface bioactive and were found to interact with the lectin Con-A.

mannose


Input: The time point of beta-catenin knockout in hepatocytes determines their response to xenobiotic activation of the constitutive androstane receptor.

androstane


Input: The constitutive androstane receptor (CAR) controls the expression of drug-metabolizing enzymes and regulates hepatocyte proliferation.

androstane


Input: Studies with transgenic mice with an early postnatal conditional hepatocyte-specific knockout of the beta-catenin gene Ctnnb1 revealed that beta-catenin deficiency decreases the magnitude of induction of drug-metabolizing enzymes by CAR activators, abrogates zonal differences in the hepatocytes' susceptibility to these compounds, and impacts on hepatocyte proliferation.


Input: These data, however, do not allow distinguishing between effects caused by beta-catenin deficiency during postnatal liver development and acute effects of beta-catenin deficiency in the adult animal at the time point of CAR activation.


Input: Therefore, CAR activation was now studied in a different mouse model allowing for the hepatocyte-specific knockout of beta-catenin in adult mice.


Input: Treatment of these mice with 3mg/kg body weight of the model CAR activator 1, 4-bis-[2-(3, 5-dichloropyridyloxy)] benzene (TCPOBOP) confirmed previous findings related to the coordinate regulation of drug metabolism by beta-catenin and CAR.

1, 4-bis-[2-(3, 5-dichloropyridyloxy)] benzene

TCPOBOP


Input: More importantly, the present study clarified that the impact of beta-catenin signaling on CAR-mediated enzyme induction in the liver is not merely due to developmental defects caused by a postnatal lack of beta-catenin, but depends on the presence of beta-catenin at the time point of xenobiotic treatment.


Input: The study also revealed interesting differences between the two mouse models: hepatic zonation of TCPOBOP-dependent induction of drug-metabolizing enzymes was restored in mice with late knockout of beta-catenin, and the strong proliferative response of female mice was exclusively abolished when using animals with a late beta-catenin knockout.

TCPOBOP


Input: This suggests a beta-catenin-dependent postnatal priming of hepatocytes during postnatal liver development, later affecting the proliferative response of adult animals to CAR-activating xenobiotics.


Input: Glutathione conjugation attenuates biological activities of 6-dehydroshogaol from ginger.

Glutathione


Input: 6-Dehydroshogaol (6-DHSG) is a bioactive alpha, beta-unsaturated carbonyl compound isolated from fresh ginger with anti-inflammatory and phase II enzyme inducing activities.

alpha, beta-unsaturated carbonyl


Input: Here we describe the glutathione (GSH)-dependent metabolism and the effect of this metabolic transformation on the biological activities of 6-DHSG.

glutathione

GSH


Input: Compared with other ginger compounds, such as 6-gingerol and 6-shogaol, 6-DHSG showed the most potent anti-inflammatory effect in lipopolysaccharide (LPS)-stimulated RAW 264. 7 cells.


Input: The biological activities of 6-DHSG were attenuated by sulfhydryl antioxidants such as glutathione (GSH) or N-acetyl cysteine (NAC), but not ascorbic acid (ASC).

sulfhydryl

glutathione

GSH

N-acetyl cysteine

NAC

ascorbic acid

ASC


Input: 6-DHSG was metabolised by GSH to form a GSH conjugate (GS-6-DHSG) in RAW 264. 7 cells, via a potential mechanism involving the catalytic activity of glutathione-S-transferase (GST).

GSH

GSH

glutathione

S


Input: GS-6-DHSG showed reduced biological activities compared with 6-DHSG in multiple biological assays.


Input: Together, these results indicate that GSH conjugation attenuates the biological activities of 6-DHSG and other alpha, beta-unsaturated carbonyl compounds.

GSH

alpha, beta-unsaturated carbonyl


Input: Beneficial effects of noni (Morinda citrifolia L.) juice on livers of high-fat dietary hamsters.


Input: Polyphenols in noni juice (NJ) are mainly composed of phenolic acids, mainly gentisic, p-hydroxybenoic, and chlorogenic acids.

Polyphenols

phenolic acids

gentisic, p-hydroxybenoic, and chlorogenic acids


Input: To investigate the beneficial effects of NJ on the liver, hamsters were fed with two diets, normal-fat and high-fat diets.


Input: Furthermore, high-fat dietary hamsters were received distilled water, and 3, 6, and 9mL NJ/kg BW, respectively.


Input: After a 6-week feeding period, the increased (p < 0. 05) sizes of liver and visceral fat in high-fat dietary hamsters compared to the control hamsters were ameliorated (p < 0. 05) by NJ supplementation.


Input: NJ also decreased (p < 0. 05) serum/liver lipids but enhanced (p < 0. 05) daily faecal lipid/bile acid outputs in the high-fat dietary hamsters.

bile acid


Input: High-fat dietary hamsters supplemented with NJ had higher (p < 0. 05) liver antioxidant capacities but lowered (p < 0. 05) liver iNOS, COX-2, TNF-alpha, and IL-1 beta expressions, gelatinolytic levels of MMP9, and serum ALT values compared to those without NJ.


Input: Hence, NJ protects liver against a high-fat dietary habit via regulations of antioxidative and anti-inflammatory responses.


Input: Proposal of mechanism of the freeze-thaw fractionation of 7S and 11S globulins in soymilk.


Input: The mechanism underlying the freeze-thaw fractionation of 7S and 11S globulins in soymilk was investigated.


Input: Freeze-thawed soymilk demonstrated an increased particle size compared with raw soymilk.


Input: Further, when defatted raw soymilk was freeze-thawed, it was fractionated into 7S (supernatant) and 11S (precipitate) globulins, similar to what is found with freeze-thaw of raw soymilk.


Input: When raw soymilk samples with different ratios of 11S/7S were freeze-thawed, the 11S-deficient variety showed no precipitate.


Input: The addition of sodium sulphite or sodium dodecyl sulphate also inhibited precipitate formation after freeze-thawing, resulting in no fractionation.

sodium sulphite

sodium dodecyl sulphate


Input: These results suggest that the fractionation is due to selective precipitation of aggregates of 11S globulins and/or 11S globulins and lipid complexes, in which the protein molecules interact through disulphide bonds and/or hydrophobic interactions.

disulphide


Input: Novel water-resistant UV-activated oxygen indicator for intelligent food packaging.

oxygen


Input: For the first time, alginate polymer has been applied to prevent dyes from leaching out of colorimetric oxygen indicator films, which enable people to notice the presence of oxygen in the package in an economic and simple manner.

oxygen

oxygen


Input: The dye-based oxygen indicator film suffers from dye leaching upon contact with water.

oxygen


Input: In this work, UV-activated visual oxygen indicator films were fabricated using thionine, glycerol, P25 TiO2, and zein as a redox dye, a sacrificial electron donor, UV-absorbing semiconducting photocatalyst, and an encapsulation polymer, respectively.

oxygen

thionine

glycerol

P25 TiO2


Input: When this zein-coated film was immersed in water for 24h, the dye leakage was as high as 80. 80 +/- 0. 45%.


Input: However, introduction of alginate (1. 25%) as the coating polymer considerably diminished the dye leaching to only 5. 80 +/- 0. 06%.


Input: This is because the ion-binding ability of alginate could prevent the cation dye from leaching into water.


Input: This novel water-resistant UV-activated oxygen indicator was also successfully photo-bleached and regained colour fast in the presence of oxygen.

oxygen

oxygen


Input: Influence of phenolic compounds on the sensorial perception and volatility of red wine esters in model solution: An insight at the molecular level.

phenolic

esters


Input: Impact of (+)-catechin and gallic acid on sensory perception and volatility of isoamyl acetate, ethyl isobutyrate, ethyl butyrate and ethyl octanoate was investigated in model solutions, by means of triangle tests, detection threshold determination and HS-GC-MS analyses.

(+)-catechin

gallic acid

isoamyl acetate

ethyl isobutyrate

ethyl butyrate

ethyl octanoate


Input: Catechin significantly altered the sensory perception of most esters (ethyl isobutyrate, ethyl butyrate and ethyl octanoate) while gallic acid displayed no impact.

Catechin

esters

ethyl isobutyrate

ethyl butyrate

ethyl octanoate

gallic acid


Input: Ethyl butyrate and ethyl octanoate odour thresholds doubled or tripled in the presence of catechin, underlining a retention impact of phenolic compounds in liquid matrix.

Ethyl butyrate

ethyl octanoate

catechin

phenolic


Input: The headspace analyses displayed a decrease only in ethyl octanoate volatility in presence of catechin, whereas no significant difference in other esters concentrations was observed.

ethyl octanoate

catechin

esters


Input: This study indicated that phenolic compounds have a variable impact on aroma compounds' volatility and their sensory perception.

phenolic


Input: The polarity of phenolic and volatile compounds as well as their spatial conformation also appeared to influence the interaction strength.

phenolic


Input: Fast determination of sulfonamides from egg samples using magnetic multiwalled carbon nanotubes as adsorbents followed by liquid chromatography-tandem mass spectrometry.

sulfonamides

carbon


Input: A simple and effective method based on magnetic separation has been developed for the extraction of sulfonamides (SAs) from egg samples using magnetic multiwalled carbon nanotubes (MMWCNTs) as an adsorbent.

sulfonamides

SAs

carbon


Input: The MMWCNTs were simply prepared by depositing Fe3O4 onto MWCNTs that had been previously oxidised.


Input: The extraction procedure was carried out in a single step by blending and subsequently stirring the mixture of MMWCNTs and aqueous egg samples.


Input: The SAs were first extracted as described above, adsorbed onto the MMWCNTs directly and finally analysed by liquid chromatography-tandem mass spectrometry.

SAs


Input: The limits of detection obtained are in the range of 1. 4-2. 8ngg (-1).


Input: The proposed method was successfully applied in determining SAs in the eggs obtained from laying hens fed with SA standards, and compared to eggs purchased from local markets.

SAs


Input: The results demonstrate that SAs were detectable in the incurred egg samples.

SAs


Input: Investigation of tocotrienol biosynthesis in rice (Oryza sativa L.).

tocotrienol


Input: Rice tocotrienol (T3) has gained attention due to its physiological activities (e. g., antiangiogenesis).

tocotrienol


Input: However, the biosynthetic pathway for T3 production in rice grain has not been well studied.


Input: We hypothesized that T3 biosynthesis enzymes and/or precursors play an important role in T3 production in whole grain.


Input: This proposal was evaluated in rice (Oryza sativa L.) by PCR and HPLC techniques.


Input: Grain tocopherol as well as flag leaf vitamin E levels were also investigated for comparison.

tocopherol

vitamin E


Input: For rice samples 14days after flowering, grain was abundant in T3, but not in flag leaf.


Input: Expression of a gene encoding homogentisate geranylgeranyltransferase (HGGT, which has long been believed to be important for T3 production) differed significantly between grain and flag leaf.


Input: We then investigated rice samples during the grain maturation period, and found that grain T3 and HGGT levels increased in the early stage and then reached a plateau.


Input: T3 precursors such as homogentisate and geranylgeranyl pyrophosphate decreased during maturation.

geranylgeranyl pyrophosphate


Input: No increase in grain T3 from the middle to late stages of maturation and a decrease in T3 precursors during maturation suggest that HGGT would be an essential, but not limiting factor for T3 biosynthesis, and T3 precursors could regulate the T3 level in grain.


Input: The results of this study would be useful for nutraceutical purposes (e. g., development of T3-overproducing rice for the prevention of angiogenic disorders).


Input: Thermal analysis of some natural polysaccharide materials by isoconversional method.


Input: Isoconversional thermal analysis of some important polysaccharides from functional foods is reported.


Input: Various thermal parameters including apparent activation energy (Ea), pre-exponential factor (A) were worked out, and the fitness of data to different models describing the degradation kinetics of polysaccharides was studied.


Input: The polysaccharides from Mimosa pudica (MP), Plantago ovata (PO), Argyreia speciosa (AS), Acacia nilotica (AN), P. ovata husk (HK) and Acacia modesta (AM) exhibited multistep degradation while those from Astragalus gummifer (AG), Salvia aegyptiaca (SA) and Ocimum basicilicum (OB) degraded mainly in single step.


Input: Generally, the degradation was exothermal.


Input: The average Ea values as determined by Flynn-Wall-Ozawa method were found to be in the range 132-187kJmol (-1).


Input: The mean comprehensive index of thermal stability (ITS) fell in the range 0. 33-0. 43.


Input: All the materials under investigation except those from SA and AS appear to be as stable as some of the important commercial materials used as pharmaceutical ingredients.


Input: Model-fitting analysis revealed that the major degradation step follows first-order kinetics.


Input: Determination of alpha-keto acids in pork meat and Iberian ham via tandem mass spectrometry.

alpha-keto acids


Input: An analytical method which offers accurate determination and identification of eight alpha-keto acids (alpha-ketoglutaric acid, pyruvic acid, 4-hydroxyphenylpyruvic acid, 3-methyl-2-oxobutyric acid, alpha-keto-gamma-methylthiobutyric acid, 4-methyl-2-oxovaleric acid, 3-methyl-2-oxovaleric acid, and phenylpyruvic acid) in pork meat and Iberian ham samples is reported.

alpha-keto acids

alpha-ketoglutaric acid

pyruvic acid

4-hydroxyphenylpyruvic acid

3-methyl-2-oxobutyric acid

alpha-keto-gamma-methylthiobutyric acid

4-methyl-2-oxovaleric acid

3-methyl-2-oxovaleric acid

phenylpyruvic acid


Input: The method utilises a highly selective and sensitive method of multiple reaction monitoring (MRM) by mass spectrometry.


Input: The analytical method is simple (although the chemical derivatisation of the alpha-keto acids with dansylhydrazine is required), precise (< 18% RSD), accurate (90-110%), sensitive (0. 01-0. 34mg/kg of defatted and freeze-dried meat depending on the alpha-keto acid) and linear (R > 0. 99) over several orders of magnitude (until 0. 01-146. 1mg/kg of defatted and freeze-dried meat depending on the alpha-keto acid).

alpha-keto acids

dansylhydrazine

alpha-keto acid

alpha-keto acid


Input: Using this methodology, alpha-keto acids were found to be present in pork meat to a low extent, and their concentration increased when they were determined in Iberian ham.

alpha-keto acids


Input: This is the first report of the presence of alpha-keto acids in both pork meats and Iberian hams.

alpha-keto acids


Input: Amino acid profiles and quantitative structure-property relationship models as markers for Merlot and Torront e s wines.

Amino acid


Input: Quantitative structure-property relationships (QSPRs) were applied to the aminograms obtained by HPLC in our laboratories for Torront e s and Merlot wines.


Input: Dragon theoretical descriptors were derived for a set of optimized amino acid structures with the purpose of establishing QSPR models.

amino acid


Input: The statistical Replacement Method was used for designing the best multi-parametric linear regression models, which included structural features selected from a pool containing 1497 constitutional, topological, geometrical or electronic molecular descriptors.


Input: Predicted QSPR results were in good agreement with experimental amino acid profiles.

amino acid


Input: The developed QSPR approach showed to be of practical value for distinguishing each wine varietal, and for calculating experimentally non-available amino acid concentrations of Torront e s and Merlot wines.

amino acid


Input: It was also useful for assessing wine authenticity; the models were especially suitable for Merlot and Torront e s wines.


Input: Prooxidative and antioxidative properties of beta-carotene in chlorophyll and riboflavin photosensitized oil-in-water emulsions.

beta-carotene

chlorophyll

riboflavin


Input: Effects of beta-carotene on the oxidative stability of chlorophyll or riboflavin photosensitized oil-in-water (O/W) emulsions were determined by analysing the depleted headspace oxygen content, lipid hydroperoxides, fluorescence intensity, and headspace volatiles.

beta-carotene

chlorophyll

riboflavin

oxygen

hydroperoxides


Input: As the concentration of beta-carotene increased from 0 to 10, 100, and 1000 mu M, the oxidative stability of samples containing chlorophylls decreased in a concentration-dependent manner under light, indicating that beta-carotene acted as a prooxidant.

beta-carotene

chlorophylls

beta-carotene


Input: However, in riboflavin photosensitized O/W emulsions, 100 and 1000 mu M beta-carotene inhibited lipid oxidation.

riboflavin

beta-carotene


Input: Although beta-carotene protected both photosensitisers in O/W emulsions, beta-carotene displayed antioxidative or prooxidative properties, which depended on the polarity of the photosensitisers.

beta-carotene

beta-carotene


Input: The development of t-2-heptenal and 1-octen-3-ol increased greatly in chlorophyll sensitised O/W emulsions with an increase in beta-carotene concentration, implying that more singlet oxygen oxidation occurred due to the higher levels of remaining chlorophylls.

chlorophyll

beta-carotene

oxygen

chlorophylls


Input: However, the content of t-2-heptenal and 1-octen-3-ol in the riboflavin sensitised O/W emulsions was not significantly correlated with the beta-carotene concentration, which indicates that beta-carotene in the lipid particles effectively quenched singlet oxygen.

riboflavin

beta-carotene

beta-carotene

oxygen


Input: Conjugated linoleic acid and calcium co-supplementation improves bone health in ovariectomised mice.

linoleic acid

calcium


Input: Osteoporosis is a significant health concern for the elderly; conjugated linoleic acid (CLA) has been shown to improve overall bone mass when calcium is included as a co-supplement.

linoleic acid

calcium


Input: However, potential effects of CLA and calcium on bone mass during a period of bone loss have not been reported.

calcium


Input: The purpose of this study was to determine how dietary calcium modulates the effects of conjugated linoleic acid (CLA) in preventing bone loss, using an ovariectomised mouse model.

calcium

linoleic acid


Input: CLA supplementation significantly prevented ovariectomy-associated weight and fat mass gain, compared to non-supplemented controls.


Input: CLA significantly increased bone markers without major changes in bone mineral composition in the femur compared to respective controls.


Input: CLA treatment increased serum parathyroid hormone (PTH) significantly (p = 0. 0172), while serum 1, 25-dihydroxyvitamin D3 concentration was not changed by CLA.

1, 25-dihydroxyvitamin D3


Input: Meanwhile, CLA significantly reduced femur tartrate resistant acid phosphatase (TRAP) activity, suggesting potential reduction of osteoclastogenesis.


Input: The data suggest that CLA, along with dietary calcium, has great potential to be used to prevent bone loss and weight gain associated with menopause.

calcium


Input: The oestrogenic and anti-platelet activities of dihydrobenzofuroisocoumarins and homoisoflavonoids from Liriope platyphylla roots.

dihydrobenzofuroisocoumarins

homoisoflavonoids


Input: The ethanolic extract of Liriope platyphylla (Liliaceae) roots showed potential oestrogenic and anti-platelet activities.


Input: Twenty-six compounds were isolated and classified as 10 skeletons, including two unusual new dihydrobenzofuroisocoumarins, (+)-platyphyllarin A (1) and B (2), one new butanoate, ethyltributanoate (3), and two new homoisoflavanones, (-)-liriopein A (4) and B (5), along with 21 known compounds, including six homoisoflavonoids, one chalcone, six amides, one lignan, one fatty acid derivative, one alkaloid, three benzenoids, and two steroids.

dihydrobenzofuroisocoumarins

(+)-platyphyllarin A (1) and B

butanoate

ethyltributanoate

homoisoflavanones

(-)-liriopein A (4) and B

homoisoflavonoids

chalcone

amides

lignan

fatty acid

benzenoids

steroids


Input: The biosynthetic pathway of compounds 1 and 2 was proposed in the current investigation.


Input: The oestrogenic activity of the isolates was evaluated utilising the pER8: GUS reporter assay system in transgenic Arabidopsis plant as well as the SEAP reporter assay system in MCF-7 breast cancer cell-line; the anti-platelet activity was evaluated using the anti-platelet aggregation assay.


Input: Several components exhibited significant oestrogenic and anti-platelet activities; demonstrating for the first time the potential use of L. platyphylla as a nutritional supplement for cardiovascular and endocrine diseases.


Input: Investigation on the role of Spirulina platensis in ameliorating behavioural changes, thyroid dysfunction and oxidative stress in offspring of pregnant rats exposed to fluoride.


Input: The study investigated the role of Spirulina platensis in reversing sodium fluoride-induced thyroid, neurodevelopment and oxidative alterations in offspring of pregnant rats.

sodium fluoride


Input: The total antioxidant activity, phycocyanins, and beta carotene content were quantified in Spirulina.

beta carotene


Input: Thirty female pregnant rats were allocated to six groups and treatment initiated orally from embryonic day (ED) 6 to postnatal day (PND) 15.


Input: Treatment groups included control, Spirulina alone, sodium fluoride (20mg/kg) alone, and sodium fluoride along with Spirulina (250 and 500mg/kg).

sodium fluoride

sodium fluoride


Input: Serum fluoride levels were determined on ED 20 and PND 11.

fluoride


Input: Offspring were subjected to behavioural testing, estimation of thyroid levels, oxidative measurements in brain mitochondrial fraction and histological evaluation of the cerebellum.


Input: Fluoride-induced alterations in thyroid hormones, behaviour and increased oxidative stress.

Fluoride


Input: Spirulina augmented the displacement of fluoride, facilitated antioxidant formation, improved behaviour and protected Purkinje cells.

fluoride


Input: Supplementing Spirulina during pregnancy could reduce the risk of fluoride toxicity in offspring.

fluoride


Input: Impact of blanching on polyphenol stability and antioxidant capacity of innovative coriander (Coriandrum sativum L.) pastes.

polyphenol


Input: Fresh coriander leaves were steam-and water-blanched at 100 degrees C and at 90 and 100 degrees C, respectively, for 1-10min, and subsequently comminuted to form a paste.


Input: Pasty products obtained from coriander fruits were processed after water-blanching applying the same time-temperature regimes.


Input: Among the 11 phenolics characterised in leaves by high-performance liquid chromatography coupled to mass spectrometric detection, several caffeic acid derivatives, 5-feruloylquinic and 5-p-coumaroylquinic acids were tentatively identified for the first time.

phenolics

caffeic acid

5-feruloylquinic and 5-p-coumaroylquinic acids


Input: In fruits, 10 phenolics were detected, whereas rutin, a dicaffeic acid derivative and two feruloylquinic and caffeoylquinic acid isomers were newly detected.

phenolics

rutin

dicaffeic acid

feruloylquinic and caffeoylquinic acid


Input: Upon steam-blanching for 1min, phenolic contents and antioxidant capacities remained virtually unchanged.

phenolic


Input: In contrast, water-blanching and extended steam-blanching even yielded increased levels compared to the unheated control, whereas short-time water-blanching resulted in higher values than prolonged heat treatment.


Input: Thus, short-time water-blanching is recommended as the initial unit in the processing of coriander leaves and fruits into novel pasty products.


Input: Synthesis and evaluation of carbamoylmethylene linked prodrugs of BMS-582949, a clinical p38 alpha inhibitor.

carbamoylmethylene


Input: A series of carbamoylmethylene linked prodrugs of 1 (BMS-582949), a clinical p38 alpha inhibitor, were synthesized and evaluated.

carbamoylmethylene


Input: Though the phosphoryloxymethylene carbamates (3, 4, and 5) and alpha-aminoacyloxymethylene carbamates (22, 23, and 26) were found unstable at neutral pH values, fumaric acid derived acyloxymethylene carbamates (2, 28, and 31) were highly stable under both acidic and neutral conditions.

phosphoryloxymethylene carbamates

alpha-aminoacyloxymethylene carbamates

fumaric acid

acyloxymethylene carbamates


Input: Prodrugs 2 and 31 were also highly soluble at both acidic and neutral pH values.


Input: At a solution dose of 14. 2mpk (equivalent to 10mpk of 1), 2 gave essentially the same exposure of 1 compared to dosing 10mpk of 1 itself.


Input: At a suspension dose of 142mpk (equivalent to 100mpk of 1), 2 demonstrated that it could overcome the solubility issue associated with 1 and provide a much higher exposure of 1.


Input: To our knowledge, the unique type of prodrugs like 2, 28, and 31 was not reported in the past and could represent a novel prodrug approach for secondary amides, a class of molecules frequently identified as drug candidates.

secondary amides


Input: Conformationally restricted homotryptamines.

homotryptamines


Input: Part 6: Indole-5-cycloalkyl methylamines as selective serotonin reuptake inhibitors.

Indole-5-cycloalkyl methylamines

serotonin


Input: Racemic 5-(trans-2-aminomethylcyclopropyl) indoles, 5-(trans-2-aminomethylcyclopentyl) indoles, and 5-(cis-2-aminomethylcyclopentyl) indoles were synthesized and evaluated as selective serotonin reuptake inhibitors.

Racemic 5-(trans-2-aminomethylcyclopropyl) indoles

5-(trans-2-aminomethylcyclopentyl) indoles

5-(cis-2-aminomethylcyclopentyl) indoles

serotonin


Input: These analogs followed SAR trends similar to those previously reported for 3-cycloalkyl substituted indoles.

3-cycloalkyl substituted indoles


Input: The most potent analogs exhibited single digit nanomolar inhibition at the human serotonin transporter but were 10-fold less active than the previously reported compounds.


Input: Biodegradable microparticles for strictly regulating the release of neurotrophic factors.


Input: A lot of research has been carried out in the last decade to find a cure for neurodegenerative diseases especially Parkinson' s disease but to little avail.


Input: In this study we have demonstrated the use of poly (lactic acid-co-glycolic acid) (PLGA)/collagen biodegradable microparticles formed using water-in-oil-in-water (W/O/W) double emulsion method, as a neurotrophic factor delivery vehicle.

poly (lactic acid-co-glycolic acid)

PLGA


Input: The microparticles were encapsulated with glial cell-derived neurotrophic factor (GDNF) fused with collagen binding peptide (CBP) immobilized to the inner collagen phase.


Input: The novelty lies in the strict regulation of release of GDNF-CBP from the microparticles as compared to a burst release from standard microparticles.


Input: The microparticles were demonstrated to be non-cytotoxic till 300 mu g/2 x 10 (5) cells and revealed a maximum release of 250ng GDNF-CBP/mg microparticles in 0. 3% collagenase.


Input: Differentiation of neural progenitor cells (NPCs) into mature neurons was demonstrated by co-culturing microparticles with cells in a medium containing collagenase which enabled the release of encapsulated GDNF-CBP, signaling the differentiation of NPCs into microtubule-associated protein 2 (MAP2)-expressing neurons.


Input: The successful ability of these microparticles to deliver neurotrophic factors and allow differentiation of NPCs into mature neurons provides some scope in its use for the treatment of Parkinson' s disease and other neurodegenerative diseases.


Input: Cell biology: notch recycling is numbed.


Input: During asymmetric cell division, the Notch regulator Numb segregates unequally to establish different cell fates in the two daughter cells.


Input: Numb is thought to act as an endocytic protein.


Input: Two new studies show that Numb antagonizes Notch signaling by also regulating recycling of Sanpodo-Notch complexes via AP-1.


Input: Monoacylglycerol lipase inhibition-induced changes in plasma corticosterone levels, anxiety and locomotor activity in male CD1 mice.

Monoacylglycerol

corticosterone


Input: The hypothalamus-pituitary-adrenal-axis is strongly controlled by the endocannabinoid system.


Input: The specific impact of enhanced 2-arachidonoylglycerol signaling on corticosterone plasma levels, however, was not investigated so far.

corticosterone


Input: Here we studied the effects of the recently developed monoacylglycerol lipase inhibitor JZL184 on basal and stress-induced corticosterone levels in male CD1 mice, and found that this compound dramatically increased basal levels without affecting stress responses.

monoacylglycerol

corticosterone


Input: Since acute changes in corticosterone levels can affect behavior, JZL184 was administered concurrently with the corticosterone synthesis inhibitor metyrapone, to investigate whether the previously shown behavioral effects of JZL184 are dependent on corticosterone.

corticosterone

corticosterone

metyrapone

corticosterone


Input: We found that in the elevated plus-maze, the effects of JZL184 on " classical " anxiety-related measures were abolished by corticosterone synthesis blockade.

corticosterone


Input: By contrast, effects on the " ethological " measures of anxiety (i. e. risk assessment) were not affected by metyrapone.

metyrapone


Input: In the open-field, the locomotion-enhancing effects of the compound were not changed either.


Input: These findings show that monoacylglycerol lipase inhibition dramatically increases basal levels of corticosterone.

monoacylglycerol

corticosterone


Input: This endocrine effect partly affects the anxiolytic, but not the locomotion-enhancing effects of monoacylglycerol lipase blockade.

monoacylglycerol


Input: Effect of N-acetyl cysteine (NAC), an organosulfur compound from Allium plants, on experimentally induced hepatic prefibrogenic events in wistar rat.

N-acetyl cysteine

NAC

organosulfur


Input: Aim of present study was to investigate the effect of NAC on experimental chronic hepatotoxicity models induced by carbon tetrachloride (CCl4) and thioacetamide (TAA).

NAC

carbon tetrachloride

thioacetamide

TAA


Input: CCl4 toxicity was induced by administering 200 mu l CCl4 (diluted 2: 3 in coconut oil)/100g body weight, p. o., twice weekly for 8 weeks.


Input: TAA toxicity was induced by administering 150mg/kg b.

TAA


Input: wt. of TAA i. p., twice weekly for 8 weeks.

TAA


Input: NAC treatment was started along with toxicants (CCl4 and TAA) for 8 weeks and continued for further 4 weeks.

NAC

TAA


Input: Self reversal group was kept without any treatment for 4 weeks after completion of toxicant treatments.


Input: Alanine aminotransferase (ALT), Aspartate aminotransferase (AST), Alkaline phosphatase (ALP), Bilirubin were measured in serum.

Alanine

Aspartate

Bilirubin


Input: Hydroxyproline (HP), lipid peroxidation (LPO), catalase (CAT), Glutathione peroxidase (GPx) and Glutathione (GSH) were determined in liver samples by colorimetric methods.

Hydroxyproline

Glutathione

Glutathione

GSH


Input: Cytochrome P450 2E1 (CYP 450 2E1), activity was determined as hydroxylation of aniline in liver microsomes.

aniline


Input: General examination and histological analysis were also performed.


Input: Serum markers of liver damage (AST, ALT, ALP and Bilirubin) were increased by CCl4 and TAA intoxication (p < 0. 001), whereas co-treatment with NAC reversed such changes (p < 0. 001).

Bilirubin

TAA

NAC


Input: HP was enhanced in toxicant groups (p < 0. 001 in CCl4 and TAA), but inhibited by NAC (p < 0. 001).

TAA

NAC


Input: LPO was increased while as GSH, CAT and GPx decreased by the administration of CCl4 and TAA (p < 0. 001); co-administration of NAC restored these liver markers to normal levels (p < 0. 001).

GSH

NAC


Input: Biochemical determinations were corroborated by general and histological findings.


Input: Keeping in view the biochemical and histopathological studies, it was concluded that CCl4 and TAA are strong hepatotoxic agents that produce liver fibrosis with close proximity to human etiology (micronodular cirrhosis) and NAC has a significant protective activity against CCl4 and TAA.

TAA

NAC

TAA


Input: NAC has also been validated as a model against oxidative burden in chronic liver pathology.

NAC


Input: Pancreatic beta-cell response to increased metabolic demand and to pharmacologic secretagogues requires EPAC2A.


Input: Incretin hormone action on beta-cells stimulates in parallel two different intracellular cyclic AMP-dependent signaling branches mediated by PKA and EPAC2A.

cyclic AMP


Input: Both pathways contribute towards potentiation of glucose-stimulated insulin secretion (GSIS).

glucose


Input: However, the overall functional role of EPAC2A in beta-cells as it relates to in vivo glucose homeostasis remains incompletely understood.

glucose


Input: Therefore, we have examined in vivo GSIS in global EPAC2A knockout mice.


Input: Additionally, we have conducted in vitro studies of GSIS and calcium dynamics in isolated EPAC2A-deficient islets.

calcium


Input: EPAC2A deficiency does not impact glucose-stimulated insulin secretion in mice under basal conditions.

glucose