Input: The maximum permissible limits for Pb and Cd determined by WHO/FAO are 10. 0ppm and 0. 3ppm respectively.

Pb

Cd


Input: Thus, random assessment on the safety of some ready-to-use aqueous based anti-malaria herbal products on the market is necessary to prevent public health hazards associated with consuming these plant extracts.


Input: Although lead and cadmium concentration in the anti-malaria herbal products were below the maximum permissible limits, their cumulative effect on the health of an individual which consume recommended volume of not less than 1000 mL for effective malaria parasite clearance cannot be ignored.

cadmium


Input: Enzymatic catalyzed palm oil hydrolysis under ultrasound irradiation: diacylglycerol synthesis.

diacylglycerol


Input: Diacylglycerol (DAG) rich oils have an organoleptic property like that of regular edible oils, but these oils do not tend to be accumulated as fat.

Diacylglycerol

DAG


Input: Palm oil ranks first in the world in terms of edible oil production owing to its low cost.


Input: The aim of this study was to propose a new methodology to produce diacylglycerol by hydrolysis of palm oil using Lipozyme RM IM commercial lipase as a catalyst under ultrasound irradiation.

diacylglycerol


Input: The reactions were carried out at 55 degrees C with two different methods.


Input: First, the reaction system was exposed to ultrasonic waves for the whole reaction time, which led to enzymatic inactivation and water evaporation.


Input: Ultrasound was then used to promote emulsification of the water/oil system before the hydrolysis reaction, avoiding contact between the probe and the enzymes.


Input: An experimental design was used to optimize the ultrasound-related parameters and maximize the hydrolysis rate, and in these conditions, with a change in equilibrium, DAG production was evaluated.

DAG


Input: Better reaction conditions were achieved for the second method: 11. 20 wt.% (water + oil mass) water content, 1. 36 wt.% (water + oil mass) enzyme load, 12 h of reaction time, 1. 2 min and 200 W of exposure to ultrasound.


Input: In these conditions diacylglycerol yield was 34. 17 wt.%.

diacylglycerol


Input: Clearance and bioavailability study through arterio-venous drug concentrations relationship.


Input: Venous plasma drug concentrations are routinely monitored in order to determine pharmacokinetic parameters or to establish relationships with drug pharmacodynamic and clinical effects.


Input: Arterial drug concentration is higher than the respective venous concentration during the period where drug input of the substance predominates, whereas venous drug concentration is higher during the long period where drug elimination becomes the main process.


Input: This arterial-venous difference responds to current bioavailability and clearance of the drug-individual systems.


Input: Following the vein/artery plasma drug concentration ratio at a non-eliminating organ it is possible to monitor both parameters time by time.


Input: This way of following up the pharmacokinetic systems allows us to detect any changes in drug absorption or disposition more efficiently, without the need of a long period of time and regardless the duration of such system modification.


Input: Spray-dried casein-based micelles as a vehicle for solubilization and controlled delivery of flutamide: Formulation, characterization, and in vivo pharmacokinetics.

flutamide


Input: Novel casein (CAS)-based micelles loaded with the poorly soluble anti-cancer drug, flutamide (FLT), were successfully developed in a powdered form via spray-drying technique.

flutamide

FLT


Input: Genipin (GNP) was used to crosslink CAS micelles as demonstrated by color variation of the micelles.

Genipin

GNP


Input: Drug solubilization was enhanced by incorporation within the hydrophobic micellar core which was confirmed by solubility study and UV spectra.


Input: Spherical core-shell micelles were obtained with a particle size below 100nm and zeta potential around-30mV.


Input: At low drug loading, FLT was totally incorporated within micellar core as revealed by thermal analysis.

FLT


Input: However, at higher loading, excess non-incorporated drug at micelle surface caused a significant reduction in the surface charge density.


Input: Turbidity measurements demonstrated the high physical stability of micelles for 2weeks dependent on GNP-crosslinking degree.

GNP


Input: In a dry powdered form, the micelles were stable for 6months with no significant changes in drug content or particle size.


Input: A sustained drug release from CAS micelles up to 5days was observed.


Input: After i. v. administration into rats, CAS micelles exhibited a prolonged plasma circulation of FLT compared to drug solution.

FLT


Input: Furthermore, a more prolonged drug systemic circulation was observed for GNP-crosslinked micelles.

GNP


Input: Overall, this study reports the application of spray-dried natural protein-based micelles for i. v. delivery of hydrophobic anti-cancer drugs such as FLT.

FLT


Input: Neuroprotective effects of mercaptoethylleonurine and mercaptoethylguanidine analogs on hydrogen peroxide-induced apoptosis in human neuronal SH-SY5Y cells.

mercaptoethylleonurine

mercaptoethylguanidine

hydrogen peroxide


Input: A series of mercaptoethylleonurine and mercaptoethylguanidine derivatives were designed and synthesized.

mercaptoethylleonurine

mercaptoethylguanidine


Input: Their neuroprotective effects toward H2O2-induced apoptosis were investigated in human SH-SY5Y cells.


Input: The results from these studies identified several potent compounds, with compound 8k emerging as the most effective.


Input: Further investigation demonstrated that 8k reduced H2O2-induced activation of mitochondrial apoptosis by inhibiting the expression of Bax and elevating the expression of Bcl-2.


Input: Moreover, the molecular mechanism underlying the observed neuroprotective effects of 8k was exerted via the Akt and JNK pathways.


Input: Compound 8k can be a lead compound for further discovery of neuroprotective medicine.


Input: Paeoniflorin protects human EA. hy926 endothelial cells against gamma-radiation induced oxidative injury by activating the NF-E2-related factor 2/heme oxygenase-1 pathway.

Paeoniflorin

heme


Input: Pulmonary endothelial cells have been demonstrated to have a critical role in the pathogenesis of radiation-induced lung injury.


Input: Our preliminary experiments indicated that Paeoniflorin protected human EA. hy926 endothelial cells from radiation-induced oxidative injury.

Paeoniflorin


Input: This study was designed to confirm the protective effect of Paeoniflorin against radiation-induced endothelial cellular damage and to elucidate the underlying mechanisms.

Paeoniflorin


Input: Preincubation of EA. hy926 cells with Paeoniflorin before gamma-radiation resulted in significant inhibition of apoptosis, a decrease in mitochondrial membrane potential and enhanced cell viability.

Paeoniflorin


Input: In particular, we showed that Paeoniflorin significantly reduced the formation of intracellular reactive oxygen species (ROS), the level of malondialdehyde (MDA) and lactate dehydrogenase (LDH) leakage, and enhanced production of the endogenous antioxidants, glutathione (GSH) and superoxide dismutase (SOD) in EA. hy926 cells.

Paeoniflorin

oxygen

malondialdehyde

MDA

lactate

glutathione

GSH

superoxide


Input: Treatment of these cells with Paeoniflorin significantly induced HO-1 expression.

Paeoniflorin


Input: Moreover, Paeoniflorin promoted the nuclear translocation of nuclear factor erythroid 2 related factor-2 (Nrf-2).

Paeoniflorin


Input: The Paeoniflorin-induced HO-1 expression was abrogated by Nrf2 siRNA.

Paeoniflorin


Input: Furthermore, inhibition of HO-1 with zinc protoporphyrin IX (ZNPP) significantly reversed the protective effect of Paeoniflorin against radiation-induced damage in EA. hy926 cells.

zinc protoporphyrin IX

ZNPP

Paeoniflorin


Input: Our findings confirmed that Paeoniflorin protected EA. hy926 cells against radiation-induced injury through the Nrf2/HO-1 pathway.

Paeoniflorin


Input: Stimuli-responsive copolymer solution and surface assemblies for biomedical applications.


Input: Stimuli-responsive polymeric materials is one of the fastest growing fields of the 21st century, with the annual number of papers published more than quadrupling in the last ten years.


Input: The responsiveness of polymer solution assemblies and surfaces to biological stimuli (e. g. pH, reduction-oxidation, enzymes, glucose) and externally applied triggers (e. g. temperature, light, solvent quality) shows particular promise for various biomedical applications including drug delivery, tissue engineering, medical diagnostics, and bioseparations.

glucose


Input: Furthermore, the integration of copolymer architectures into stimuli-responsive materials design enables exquisite control over the locations of responsive sites within self-assembled nanostructures.


Input: The combination of new synthesis techniques and well-defined copolymer self-assembly has facilitated substantial developments in stimuli-responsive materials in recent years.


Input: In this tutorial review, we discuss several methods that have been employed to synthesize self-assembling and stimuli-responsive copolymers for biomedical applications, and we identify common themes in the response mechanisms among the targeted stimuli.


Input: Additionally, we highlight parallels between the chemistries used for generating solution assemblies and those employed for creating copolymer surfaces.


Input: Anatomical connection strength predicts dopaminergic drug effects on fronto-striatal function.


Input: RATIONALE: The neurotransmitter dopamine plays a key role in cognitive functions that are associated with fronto-striatal circuitry and has been implicated in many neuropsychiatric disorders.

dopamine


Input: However, there is a large variability in the direction and extent of dopaminergic drug effects across individuals.


Input: OBJECTIVES: We investigated whether individual differences in dopaminergic drug effects on human fronto-striatal functioning are associated with individual differences in white matter tracts.


Input: METHODS: The effects of the dopamine receptor agonist bromocriptine were assessed using functional magnetic resonance imaging in 22 healthy volunteers in a placebo-controlled, double-blind, within-subject design.

dopamine

bromocriptine


Input: Human psychopharmacology and functional neuroimaging were combined with functional connectivity analyses and structural connectivity analyses to establish a link between dopaminergic drug effects on fronto-striatal function and fronto-striatal anatomy.


Input: RESULTS: We demonstrate that bromocriptine alters functional signals associated with attention switching in the basal ganglia.

bromocriptine


Input: Crucially, individual differences in the drug' s effect on these signals could be predicted from individual differences in fronto-striato-thalamic white matter tracts, as indexed by diffusion tensor imaging.


Input: Anatomical fronto-striatal connectivity also predicted drug effects on switch-related functional connectivity between the basal ganglia and the prefrontal cortex.


Input: CONCLUSIONS: These data reinforce the link between dopamine, cognition and the basal ganglia and have implications for the individual tailoring of dopaminergic drug therapy based on anatomical fronto-striatal connection strength.

dopamine


Input: Management of chemotherapy-induced nausea and vomiting: focus on newer agents and new uses for older agents.


Input: Chemotherapy-induced nausea and vomiting (CINV) is associated with a significant deterioration in quality of life.


Input: The emetogenicity of the chemotherapeutic agents, repeated chemotherapy cycles, and patient risk factors significantly influence CINV.


Input: The use of a combination of a serotonin 5-HT3 receptor antagonist, dexamethasone and a neurokinin 1 (NK1) receptor antagonist has significantly improved the control of acute and delayed emesis in single-day chemotherapy.

serotonin

dexamethasone


Input: Palonosetron, a second-generation 5-HT3 receptor antagonist with a different half-life, a different binding capacity and a different mechanism of action than the first-generation 5-HT3 receptor antagonists appears to be the most effective agent in its class.

Palonosetron


Input: Aprepitant, the first and only agent clinically available in the NK1 receptor antagonist drug class has been used effectively as an additive agent to the 5-HT3 receptor antagonists and dexamethasone to control CINV.

Aprepitant

dexamethasone


Input: Rolapitant and netupitant are other NK1 receptor antagonists that are currently in phase III clinical trials.

Rolapitant

netupitant


Input: Despite the control of emesis, nausea has not been well controlled by current agents.


Input: Olanzapine, a US-FDA approved antipsychotic, has emerged in recent trials as an effective preventative agent for CINV, as well as a very effective agent for the treatment of breakthrough emesis and nausea.

Olanzapine


Input: Clinical trials using gabapentin, cannabinoids and ginger have not been definitive regarding their efficacy in the prevention of CINV.

gabapentin


Input: Additional studies are necessary for the control of nausea and for the control of CINV in the clinical settings of multiple-day chemotherapy and bone marrow transplantation.


Input: Predicting the Optimal Basal Insulin Infusion Pattern in Children and Adolescents on Insulin Pumps.


Input: OBJECTIVEWe aimed at developing and cross-validating a mathematical prediction model for an optimal basal insulin infusion pattern for children with type 1 diabetes on continuous subcutaneous insulin infusion therapy (CSII). RESEARCH DESIGN AND METHODSWe used the German/Austrian DPV-Wiss database for quality control and scientific surveys in pediatric diabetology and retrieved all CSII patients < 20 years of age (November 2009).


Input: A total of 1, 248 individuals from our previous study were excluded (dataset 1), resulting in 6, 063 CSII patients (dataset 2) (mean age 10. 6 +/- 4. 3 years).


Input: Only the most recent basal insulin infusion rates (BRs) were considered.


Input: BR patterns were identified and corresponding patients sorted by unsupervised clustering.


Input: Logistic regression analysis was applied to calculate the probabilities for each BR pattern.


Input: Equations were based on both independent datasets separately, and probabilities for BR patterns were cross-validated using typical test patients. RESULTSOf the 6, 063 children, 5, 903 clustered in one of four major circadian BR patterns, confirming our previous study.


Input: The oldest age-group (mean age 12. 8 years) was represented by 2, 490 patients (42. 18%) with a biphasic dawn-dusk pattern (BC).


Input: A broad single insulin maximum at 9-10 p. m.


Input: (F) was unveiled by 853 patients (14. 45%) (mean age 6. 3 years).


Input: Logistic regression analysis revealed that age, to a lesser extent duration of diabetes, and partly sex predicted BR patterns.


Input: Cross-validation revealed almost identical probabilities for BR patterns BC and F in the two datasets but some variation in the remaining two BR patterns. CONCLUSIONSReconfirmation of four key BR patterns in two very large independent cohorts supports that these patterns are realistic approximations of the circadian distribution of insulin needs in children with type 1 diabetes.


Input: Prediction of an optimal pattern a priori can improve initiation and clinical follow-up of CSII in children and adolescents.


Input: In addition, these BR patterns represent valuable information for insulin-infusion algorithms in closed-loop CSII.


Input: Metabolism-Dependent Inhibition of CYP3A4 by Lapatinib: Evidence for Formation of a Metabolic Intermediate Complex with a Nitroso/Oxime Metabolite Formed via a Nitrone Intermediate.

Lapatinib

Nitroso

Oxime

Nitrone


Input: Metabolism-dependent inhibition (MDI) of cytochrome P450 (P450) enzymes has the potential to cause clinically relevant drug-drug interactions.


Input: In the case of several alkylamine drugs, MDI of P450 involves formation of a metabolite that binds quasi-irreversibly to the ferrous heme iron to form a metabolic intermediate (MI) complex.

alkylamine

ferrous heme iron


Input: The specific metabolites coordinately bound to ferrous iron and the pathways leading to MI complex formation are the subject of debate.

ferrous iron


Input: We describe an approach combining heme iron oxidation with potassium ferricyanide and metabolite profiling to probe the mechanism of MI complex-based CYP3A4 inactivation by the secondary alkylamine drug lapatinib.

heme iron

potassium ferricyanide

secondary alkylamine

lapatinib


Input: Ten metabolites formed from lapatinib by CYP3A4-mediated heteroatom dealkylation, C-hydroxylation, N-oxygenation with or without further oxidation, or a combination thereof, were detected by accurate mass spectrometry.

lapatinib

N


Input: The abundance of one metabolite, the N-dealkylated nitroso/oxime lapatinib metabolite (M9), correlated directly with the prevalence or the disruption of the MI complex with CYP3A4.

N

nitroso

oxime lapatinib


Input: Nitroso/oxime metabolite formation from secondary alkylamines has been proposed to occur through two possible pathways: (1) sequential N-dealkylation, N-hydroxylation, and dehydrogenation (primary hydroxylamine pathway) or (2) N-hydroxylation with dehydrogenation to yield a nitrone followed by N-dealkylation (secondary hydroxylamine pathway).

Nitroso

oxime

alkylamines

N

N

primary hydroxylamine

N

nitrone

N

secondary hydroxylamine


Input: All intermediates for the secondary hydroxylamine pathway were detected but the primary N-hydroxylamine intermediate of the primary hydroxylamine pathway was not.

secondary hydroxylamine

N

hydroxylamine

primary hydroxylamine


Input: Our findings support the mechanism of lapatinib CYP3A4 inactivation as MI complex formation with the nitroso metabolite formed through the secondary hydroxylamine and nitrone pathway, rather than by N-dealkylation to the primary amine followed by N-hydroxylation and dehydrogenation as is usually assumed.

lapatinib

nitroso

secondary hydroxylamine

nitrone

N

primary amine

N


Input: Interpretation of optoelectronic transient and charge extraction measurements in dye-sensitized solar cells.


Input: Tools that assess the limitations of dye sensitized solar cells (DSSCs) made with new materials are critical for progress.


Input: Measuring the transient electrical signals (voltage or current) after optically perturbing a DSSC is an approach which can give information about electron concentration, transport and recombination.


Input: Here we describe the theory and practice of this class of optoelectronic measurements, illustrated with numerous examples.


Input: The measurements are interpreted with the multiple trapping continuum model which describes electrons in a semiconductor with an exponential distribution of trapping states.


Input: We review standard small perturbation photocurrent and photovoltage transients, and introduce the photovoltage time of flight measurement which allows the simultaneous derivation of both effective diffusion and recombination coefficients.


Input: We then consider the utility of large perturbation measurements such as charge extraction and the current interrupt technique for finding the internal charge and voltage within a device.


Input: Combining these measurements allows differences between DSSCs to be understood in terms such as electron collection efficiency, semiconductor conduction band edge shifts and recombination kinetics.


Input: Functional UDP-glucuronyltransferase 2B15 polymorphism and bisphenol A concentrations in blood: results from physiologically based kinetic modelling.

UDP

bisphenol A


Input: Bisphenol A (BPA) is a chemical in widespread use that is under scientific discussion due to its endocrine activity.

Bisphenol A

BPA


Input: Controversies exist about how to interpret reportedly high blood concentrations measured in uncontrolled situations.


Input: Physiologically based pharmaco-/toxicokinetic modelling resulted in 10-100-fold lower blood concentrations than those reported.


Input: Moreover, in controlled situations, BPA did not exceed the level of detection (< 0. 3 ng/ml) in human blood or urine.

BPA


Input: Using a validated human PBK model, this study investigated the influence of functionally relevant polymorphic UGT2B15, the enzyme mediating BPA metabolism, on the BPA concentration-time profile in human blood.

BPA

BPA


Input: Maximum concentrations (C (max)) and areas under the curves (AUCs) in blood from high and low metabolisers differed by a factor of 4. 7 and 4. 6, respectively (doses: 1 and 0. 05 mu g/kg/day).


Input: Low metabolisers excreted a greater proportion of BPA via the sulphate pathway compared to high metabolisers.

BPA

sulphate


Input: This finding explains why C (max) and AUC increased to a smaller extent, as predicted from in vitro data obtained with transfected cells possessing only the UGT2B15 variants.


Input: The highest C (max) value calculated in the subject with the lowest metabolic clearance was roughly 40 pg/ml, which is far lower than reported high blood concentrations, which in turn cannot be explained by genetically impaired UGT2B15 activity.


Input: From the risk assessment perspective, our results indicate that the traditional uncertainty factor is sufficient to account for the variability in the polymorphic glucuronidation of BPA.

BPA


Input: Current-use pesticides in stream water and suspended particles following runoff: Exposure, effects, and mitigation requirements.


Input: The European Union' s directive for sustainable use of pesticides requires implementing risk mitigation measures at streams threatened by pesticide entries.


Input: The need for mitigation measures was investigated at 10 stream sites within an intensively used arable region in central Germany by characterizing pesticide exposure following edge-of-field runoff and effects on the aquatic macroinvertebrates.


Input: Moreover, the influence of riparian buffer strip width (as a mitigation measure) at the sampling sites was considered.


Input: Generally, invertebrate fauna was dominated by pesticide-tolerant species, suggesting a high pesticide exposure at almost all sites.


Input: This result is also reflected by the elevated levels of suspended particle contamination in terms of toxic units (logTUMax >-2), corresponding to one-hundredth of the median lethal concentration (LC50) to Daphnia magna.


Input: At two sites that received high aqueous-phase entries of the pyrethroid lambda-cyhalothrin (logTUMax >-0. 6), the abundance and number of sensitive species in terms of the species at risk index decreased during the pesticide application period.

lambda-cyhalothrin


Input: In contrast, no acute significant negative effects on macroinvertebrates were observed at sites characterised by low water-phase toxicity (logTUMax <-3. 5).


Input: An influence of riparian buffer strip width on pesticide exposure was not observed, supposedly because of the presence of erosion rills and ephemeral ditches.


Input: In conclusion, results show that mitigation measures (such as the improvement of currently present riparian buffer strips) are needed in the study area.


Input: Environ Toxicol Chem 2013; 32: 1254-1263.


Input: (c) 2013 SETAC.


Input: ERK-mediated phosphorylation of fibroblast growth factor receptor 1 on Ser777 inhibits signaling.


Input: Fibroblast growth factor 1 (FGF1) controls cellular activities through the activation of specific cell-surface FGF receptors (FGFRs).


Input: Transphosphorylation of tyrosine residues in the kinase domain of FGFRs leads to activation of intracellular signaling cascades, including those mediated by mitogen-activated protein kinases (MAPKs).

tyrosine


Input: FGFRs also contain a serine-rich C-terminal tail.

serine

C


Input: We identified a regulatory mechanism of FGFR signaling involving phosphorylation of Ser (777) in the C-terminal region of FGFR1 by the MAPKs extracellular signal-regulated kinase 1 (ERK1) and ERK2.

Ser

C


Input: Prevention of the phosphorylation of Ser (777) in FGFR1 or mutation of Ser (777) to alanine enhanced FGF-stimulated receptor tyrosine phosphorylation and increased cell proliferation, cell migration, and axonal growth.

Ser

Ser

alanine

tyrosine


Input: A form of FGFR1 with a phosphomimetic mutation at Ser (777) exhibited reduced signaling.

Ser


Input: Activation of MAPKs by other receptor tyrosine kinases also resulted in phosphorylation of Ser (777) in FGFR1, thereby enabling crosstalk regulation of FGFR activity by other signaling pathways.

tyrosine

Ser


Input: Our data reveal a negative feedback mechanism that controls FGF signaling and thereby protects the cell from excessive activation of FGFR.


Input: Indolizine derivatives as HIV-1 VIF-ElonginC interaction inhibitors.

Indolizine


Input: Compound 1 (VEC-5) was identified as a potent small molecular HIV-1 VIF inhibitor that targets the VIF-ElonginC interaction.


Input: A structure-activity relationship study was carried out to develop compounds with improved efficacy against HIV-1 and 49 indolizine derivatives of three categories were designed and synthesized.

indolizine


Input: We found that 5 compounds exhibited promising anti-HIV-1 activity and the most active compound 2g had an IC (50) value of 11. 0 mu M.


Input: These results provide new information to develop highly potent small-molecule HIV-1 VIF inhibitors.


Input: (c) 2013 John Wiley & Sons A/S.


Input: Solution structure and in silico binding of a cyclic peptide with hepatitis B surface antigen.


Input: A specific ligand targeting the immunodominant region of hepatitis B virus (HBV) is desired in neutralizing the infectivity of the virus.


Input: In a previous study, a disulfide constrained cyclic peptide cyclo S (1), S (9) Cys-Glu-Thr-Gly-Ala-Lys-Pro-His-Cys (S (1), S (9)-cyclo-CETGAKPHC) was isolated from a phage displayed cyclic peptide library using an affinity selection method against HBV surface antigen (HBsAg).

disulfide

cyclo S (1), S (9) Cys-Glu-Thr-Gly-Ala-Lys-Pro-His-Cys


Input: The cyclic peptide binds tightly to HBsAg with a relative dissociation constant (K (D) (rel)) of 2. 9 nM.


Input: The binding site of the peptide was located at the immunodominant region on HBsAg.


Input: Consequently, this study was aimed to elucidate the structure of the cyclic peptide and its interaction with HBsAg in silico.


Input: The solution structure of this cyclic peptide was solved using (1) H, (13) C and (15) N NMR spectroscopy and molecular dynamics (MD) simulations with NMR-derived distance and torsion angle restraints.

(1) H

(13) C

(15) N


Input: The cyclic peptide adopted two distinct conformations due to the isomerization of the Pro residue with one structured region in the ETGA sequence.

Pro


Input: Docking studies of the peptide ensemble with a model structure of HBsAg revealed that the cyclic peptide can potentially be developed as a therapeutic drug that inhibits the virus-host interactions.


Input: (c) 2013 John Wiley & Sons A/S.


Input: Adsorption of model perfumes at the air-solution interface by coadsorption with an anionic surfactant.


Input: The adsorption of the model perfumes phenyl ethanol, PE, and linalool, LL, at the air-solution interface by coadsorption with the anionic surfactant sodium dodecyl 6-benezene sulfonate, LAS-6, has been studied primarily by neutron reflectivity, NR.

phenyl ethanol

linalool

sodium dodecyl 6-benezene sulfonate


Input: The variation in the mixed surface adsorption with solution composition is highly nonideal, and the more hydrophobic LL is more surface active.


Input: At a LAS-6 concentration of 0. 5 mM the adsorption of PE and LL is broadly similar but with the LL systematically more surface active, and at 2 mM the LL completes more effectively for the surface than the PE.


Input: The variation in surface composition with solution composition and concentration reflect the greater hydrophobicity and hence surface activity of LL, and the greater solubility of PE in aqueous solution.


Input: Changing the geometry of the LAS isomer, from the symmetrical LAS-6 geometry to the more asymmetrical LAS-4, results in the LL competing more effectively for the surface due to changes in the packing constraints associated with the hydrophobic region.

LAS


Input: The results provide insights into the factors that affect coadsorption that can be more broadly applied to the surface delivery of a wide range of molecules other than perfumes.


Input: In vitro polyphenolics erythrocyte model and in vivo chicken embryo model revealed gallic acid to be a potential hemorrhage inducer: physicochemical action mechanisms.

polyphenolics

gallic acid


Input: The in vivo chicken embryo model (CEM) demonstrated that gallic acid (GA) induced dysvascularization and hypoxia.

gallic acid


Input: Inflammatory edema, Zenker' s necrosis, hemolysis, and liposis of cervical muscles were the common symptoms.


Input: Levels of the gene hif-1 alpha, HIF-1 alpha, TNF-alpha, IL-6, and NF kappa B in cervical muscles were all significantly upregulated, while the vascular endothelial growth factor (VEGF) was downregulated in a dose-responsive manner.


Input: Consequently, the cervical muscle inflammation and hemolysis could have been stimulated en route to the tissue TNF-alpha-canonical and the atypical pathways.


Input: We hypothesized that GA could deplete the dissolved oxygen (DO) at the expense of semiquinone and quinone formation, favoring the reactive oxygen species (ROS) production to induce RBC disruption and Fe (2 +) ion release.

oxygen

semiquinone

quinone

oxygen

Fe (2 +)


Input: To explore this, the in vitro polyphenolics-erythrocyte model (PEM) was established.

polyphenolics


Input: PEM revealed that the DO was rapidly depleted, leading to the release of a huge amount of Fe (II) ions and hydrogen peroxide (HPO) in a two-phase kinetic pattern.

Fe (II)

hydrogen peroxide

HPO


Input: The kinetic coefficients for Fe (II) ion release ranged from 0. 347 h (-1) to 0. 774 h (-1); and those for Fe (III) ion production were from 6. 66 x 10 (-3) h (-1) to 8. 93 x 10 (-3) h (-1).

Fe (II)

Fe (III)


Input: For phase I HPO production, they ranged from 0. 236 h (-1) to 0. 774 h (-1) and for phase II HPO production from 0. 764 h (-1) to 2. 560 h (-1) at GA within 6 mu M to 14 mu M.

HPO

HPO


Input: Thus, evidence obtained from PEM could strongly support the phenomena of CEM.


Input: To conclude, GA tends to elicit hypoxia-related inflammation and hemolysis in chicken cervical muscles through its extremely high prooxidant activity.


Input: A genetically encoded and gate for cell-targeted metabolic labeling of proteins.


Input: We describe a genetic AND gate for cell-targeted metabolic labeling and proteomic analysis in complex cellular systems.


Input: The centerpiece of the AND gate is a bisected methionyl-tRNA synthetase (MetRS) that charges the Met surrogate azidonorleucine (Anl) to tRNA (Met).

methionyl

MetRS

azidonorleucine

Anl

Met


Input: Cellular protein labeling occurs only upon activation of two different promoters that drive expression of the N-and C-terminal fragments of the bisected MetRS.

N

C


Input: Anl-labeled proteins can be tagged with fluorescent dyes or affinity reagents via either copper-catalyzed or strain-promoted azide-alkyne cycloaddition.

Anl

copper


Input: Protein labeling is apparent within 5 min after addition of Anl to bacterial cells in which the AND gate has been activated.

Anl


Input: This method allows spatial and temporal control of proteomic labeling and identification of proteins made in specific cellular subpopulations.


Input: The approach is demonstrated by selective labeling of proteins in bacterial cells immobilized in the center of a laminar-flow microfluidic channel, where they are exposed to overlapping, opposed gradients of inducers of the N-and C-terminal MetRS fragments.

N

C


Input: The observed labeling profile is predicted accurately from the strengths of the individual input signals.


Input: Improving the second-order nonlinear optical response of fluorescent proteins: the symmetry argument.


Input: We have successfully designed and expressed a new fluorescent protein with improved second-order nonlinear optical properties.


Input: It is the first time that a fluorescent protein has been rationally altered for this particular characteristic.


Input: On the basis of the specific noncentrosymmetry requirements for second-order nonlinear optical effects, we had hypothesized that the surprisingly low first hyperpolarizability (beta) of the enhanced yellow fluorescent protein (eYFP) could be explained by centrosymmetric stacking of the chromophoric Tyr66 and the neighboring Tyr203 residue.


Input: The inversion center was removed by mutating Tyr203 into Phe203, with minor changes in the linear optical properties and even an improved fluorescence quantum yield.


Input: Structure determination by X-ray crystallography as well as linear optical characterization corroborate a correct folding and maturation.


Input: Measurement of beta by means of hyper-Rayleigh scattering (HRS) as well as their analysis using quantum chemistry calculations validate our hypothesis.


Input: This observation can eventually lead to improved red fluorescent proteins for even better performance.


Input: On the basis of the specific function (second-harmonic generation), the color of its emission, and in analogy with the " fruit " names, we propose SHardonnay as the name for this Tyr203Phe mutant of eYFP.


Input: Raman spectra of interchanging beta-lactamase inhibitor intermediates on the millisecond time scale.


Input: Rapid mix-rapid freeze is a powerful method to study the mechanisms of enzyme-substrate reactions in solution.


Input: Here we report a protocol that combines this method with normal (non-resonance) Raman microscopy to enable us to define molecular details of intermediates at early time points.


Input: With this combined method, SHV-1, a class A beta-lactamase, and tazobactam, a commercially available beta-lactamase inhibitor, were rapidly mixed on the millisecond time scale and then were flash-frozen by injection into an isopentane solution surrounded by liquid nitrogen.

tazobactam

isopentane

nitrogen


Input: The " ice " was finally freeze-dried and characterized by Raman microscopy.


Input: We found that the reaction is almost complete in solution at 25 ms, giving rise to a major population composed of the trans-enamine intermediate.

trans-enamine


Input: Between 25 and 500 ms, minor populations of protonated imine are detected that have previously been postulated to precede enamine intermediates.

imine

enamine


Input: However, within 1 s, the imines are converted entirely to enamines.

imines

enamines


Input: Interestingly, with this method, we can measure directly the turnover number of SHV-1 and tazobactam.

tazobactam


Input: The enzyme is completely inhibited at 1: 4 ratio (enzyme: inhibitor) or greater, a number that agrees with the turnover number derived from steady-state kinetic methods.


Input: This application, employing non-intensity-enhanced Raman spectroscopy, provides a general and effective route to study the early events in enzyme-substrate reactions.


Input: Preparation of lipase-coated, stabilized, hydrophobic magnetic particles for reversible conjugation of biomacromolecules.


Input: This Communication presents the development of a novel strategy for the easy conjugation of biomolecules to hydrophobic magnetic microparticles via reversible coating with previously functionalized lipase molecules.


Input: First, the ability of lipase to be strongly adsorbed onto hydrophobic surfaces was exploited for the stabilization of microparticles in aqueous medium by the creation of a hydrophilic surface.


Input: Second, the surface amino acids of lipase can be tailored to suit biomolecule conjugation.

amino acids


Input: This approach has been demonstrated by amino-epoxy activation of lipase, enabling the conjugation of different biomolecules to the magnetic particle' s surface.

amino

epoxy


Input: For example, it was possible to immobilize 70% of Escherichia coli proteins on the recovered particles.


Input: Furthermore, this strategy could be extended to other lipase chemical modification protocols, enabling fine control of biomolecule coupling.


Input: These conjugation techniques constitute a modular methodology that also permits the recycling of the magnetic carrier following use.


Input: Exposure to lambda-cyhalothrin, a synthetic pyrethroid, increases reactive oxygen species production and induces genotoxicity in rat peripheral blood.

lambda-cyhalothrin

pyrethroid

oxygen


Input: Lambda-cyhalothrin (LTC) is a synthetic pyrethroid with a broad spectrum of insecticidal and acaricidal activities used to control a wide range of insect pests in a variety of applications.

Lambda-cyhalothrin

LTC

pyrethroid


Input: However, there is little known about its adverse effects, in particular those related to its genotoxicity in humans.


Input: To elucidate the genotoxicity mechanisms of LTC, the micronuclei (MN) frequencies, the levels of reactive oxygen species (ROS), erythrocyte osmotic fragility, nitrite (NO) formation, protein carbonyl (PCO) levels and malondialdehyde (MDA) production were evaluated for a period of 7, 14 and 21 days.

LTC

oxygen

nitrite

NO

carbonyl

malondialdehyde

MDA


Input: Our results show that exposure rat to LTC (1/10DL50 = 6. 23 mg/kg) for a period of 7, 14 and 21 days induced a noticeable genotoxic effect in rat peripheral blood evidenced by a significant increase in the frequency of MN only at day 21 of treatment.

LTC


Input: Significant differences between the two groups were observed in erythrocyte osmotic fragility.


Input: Further, a significant (p < 0. 01) increase in ROS contents, NO formation, PCO levels and lipid peroxidation in erythrocytes were observed at different times of treatments, suggesting the implication of oxidative stress in its toxicity.

NO


Input: These results confirm the genotoxic and the pro-oxidant effects of LTC in rat peripheral blood.

LTC


Input: The periodontal health of lead-exposed children living in a shipyard industrial area.


Input: In a cross-sectional design, 292 schoolchildren living around a shipyard area, known to be contaminated with lead from shipyard industry, were examined to verify the association between lead exposure and periodontal health.


Input: The probing pocket depth (PD), bleeding on probing, plaque and calculus, and the presence of Aggregatibacter actinomycetemcomitans (Aa) in subgingival crevices were recorded.


Input: Gingival inflammation was the most common (98%) among children in the area.


Input: No significant difference in gingival inflammation was observed between high blood lead (PbB) and low PbB children.


Input: The prevalence rate of probing PD of >= 5 mm was 14%.


Input: The high PbB group showed more deep pockets at tooth 16 (upper right first permanent molar) and tooth 46 (lower right first permanent molar) than the low PbB group.


Input: The odds ratios (ORs) for having probing PD >= 5 mm after adjusting for other factors were 3. 63 (95% confidence interval (CI), 1. 24-10. 61; p = 0. 02) for tooth 16 and 3. 93 (95% CI, 1. 18-13. 00; p = 0. 02) for tooth 46.


Input: The presence of Aa was observed in 17% of the children and it significantly increased in high PbB compared with low PbB children at tooth 46 (OR = 5. 53, 95% CI: 1. 68-18. 15; p = 0. 005).


Input: This study may suggest no association between lead exposure and gingival inflammation, yet there was the involvement of deeper periodontal tissue in lead-exposed children.


Input: Protective role of L-carnitine and vitamin E on the testis of atherosclerotic rats.

L-carnitine

vitamin E


Input: Atherosclerosis is a condition caused by lipid build-up and inflammation in the arteries, so hyperlipidemia is the major reason for atherosclerosis.


Input: Testis was found to be negatively affected by hyperlipidemia which leads to its impaired functions.


Input: Vitamin E and < sc > l </sc >-carnitine have well-known lipid-lowering and antioxidative activities.

Vitamin E

< sc > l </sc >-carnitine


Input: Triton WR 1339 is a non-ionic detergent, which induces severe hyperlipidemia by inhibition of lipoprotein lipase.

Triton WR 1339


Input: The present study evaluates the protective role of vitamin E and < sc > l </sc >-carnitine on the testis in atherosclerosis and detects the most effective choice for protection against atherosclerosis; vitamin E, < sc > l </sc >-carnitine or a combination of both.

vitamin E

< sc > l </sc >-carnitine

vitamin E

< sc > l </sc >-carnitine


Input: A total of 80 albino male rats were divided into eight groups (10 rats for each group): control (G (1)), triton (G (2)), < sc > l </sc >-carnitine (G (3)), triton + < sc > l </sc >-carnitine (G (4)), vitamin E (G (5)), triton + vitamin E (G (6)), < sc > l </sc >-carnitine + vitamin E (G (7)) and triton + < sc > l </sc >-carnitine + vitamin E (G (8)).

triton

< sc > l </sc >-carnitine

triton

< sc > l </sc >-carnitine

vitamin E

triton

vitamin E

< sc > l </sc >-carnitine

vitamin E

triton

< sc > l </sc >-carnitine

vitamin E


Input: Data showed a significant increase in the levels of total cholesterol (TC), triglycerides (TGs), low-density lipoprotein cholesterol (LDL-C), 17 beta hydroxysteroid dehydrogenase (17 beta HSD), testicular catalase and malondialdehyde (MDA) in G (2) when compared with G (1), whereas high-density lipoprotein cholesterol (HDL-C), serum testosterone, testicular 17 ketosteroid reductase (17 KSR), total thiol and glutathione-S-transferase (GST) data showed a significant decrease in G (2) when compared with G (1).

cholesterol

triglycerides

cholesterol

17 beta hydroxysteroid

malondialdehyde

MDA

cholesterol

testosterone

ketosteroid

thiol

glutathione

S


Input: Treatment with < sc > l </sc >-carnitine or/and vitamin E helps in improving the adverse effect of triton; also the histological changes confirm this finding.

< sc > l </sc >-carnitine

vitamin E

triton


Input: So the present study recommends all people to include < sc > l </sc >-carnitine and vitamin E in their diet to be protected against atherosclerosis.

< sc > l </sc >-carnitine

vitamin E


Input: Critical parameters in exfoliating graphite into graphene.

graphite

graphene


Input: Dispersing graphite into few-layers graphene sheets (GS) in water is very appealing as an environmental-friendly, low-cost, low-energy method of obtaining graphene.

graphite

graphene

graphene


Input: Very high GS concentrations in water (0. 7 mg mL (-1)) were obtained by optimizing the nature of dispersant and the type of ultra-sonic generator.


Input: We find that a multi-step sonication procedure involving both tip and bath sources considerably enhances the yield of exfoliated GS.


Input: Raman and transmission electron microscopy indicate few-layers graphene patches with typical size of ~ 0. 65 mu m in one dimension and ~ 0. 35 mu m in the other.

graphene


Input: These were further employed in combination with water-dispersed CNTs to fabricate conductive transparent electrodes for a molecularly-controlled solar-cell with an open-circuit voltage of 0. 53 V.


Input: The CRF (1) receptor antagonist SSR125543 prevents stress-induced cognitive deficit associated with hippocampal dysfunction: Comparison with paroxetine and D-cycloserine.

paroxetine

D-cycloserine


Input: RATIONALE: The selective CRF (1) (corticotropin releasing factor type 1) receptor antagonist SSR125543 has been previously shown to attenuate the long-term cognitive deficit produced by traumatic stress exposure.


Input: Memory disturbances described in post-traumatic stress disorder (PTSD) patients are believed to be associated with changes in neuronal activity, in particular at the level of the hippocampus.


Input: OBJECTIVES: The present study aims at investigating whether the effects of SSR125543 (10 mg/kg/day for 2 weeks) on cognitive impairment induced by traumatic stress exposure are associated with changes in hippocampal excitability.


Input: Effects of SSR125543 were compared to those of the 5-HT reuptake inhibitor, paroxetine (10 mg/kg/day), and the partial N-methyl-D-aspartate (NMDA) receptor agonist, D-cycloserine (10 mg/kg/day), two compounds which have demonstrated clinical efficacy against PTSD.

paroxetine

N-methyl-D-aspartate

NMDA

D-cycloserine


Input: METHODS: Mice received two unavoidable electric foot-shocks.


Input: Then, 1 or 16 days after stress, they were tested for their memory performance using the object recognition test.


Input: Neuronal excitability was recorded during the third week post-stress in the CA1 area of the hippocampus.


Input: Drugs were administered from day 1 post-stress to the day preceding the electrophysiological study.


Input: RESULTS: Application of electric shocks produced cognitive impairment 16, but not 1 day after stress, an effect which was associated with a decrease in hippocampal neuronal excitability.


Input: Both stress-induced effects were prevented by repeated administration of SSR125543, paroxetine and D-cycloserine.

paroxetine

D-cycloserine


Input: CONCLUSIONS: These findings confirm that the CRF (1) receptor antagonist SSR125543 is able to attenuate the behavioral effects of traumatic stress exposure and indicate that these effects are associated with a normalization of hippocampal neuronal excitability impaired by stress.


Input: Lupenone from Erica multiflora leaf extract stimulates melanogenesis in B16 murine melanoma cells through the inhibition of ERK1/2 activation.

Lupenone


Input: Hypopigmentation diseases are usually managed using UVB light which increases the patients' risk for skin cancer.


Input: Here, we evaluated the melanogenesis stimulatory effects of leaf extracts of Erica multiflora, a medicinal plant from the Mediterranean region, and its active component, lup-20 (29)-en-3-one, as possible therapeutic agents to address hypopigmentation disorders.

lup-20 (29)-en-3-one


Input: B16 murine melanoma cells were treated with E. multiflora extracts or its active component lupenone to evaluate their effects on melanin biosynthesis.

lupenone


Input: The mechanism underlying the observed effects was also determined.


Input: Bioactivity-guided fractionation of fifteen ethyl acetate fractions identified fraction 2 to have melanogenesis stimulatory effects due to its ability to decrease mitogen-activated protein kinase phosphorylated extracellular signal-regulated kinases 1 and 2 activation.

ethyl acetate


Input: Preparative TLC of ethyl acetate fraction 2 revealed the presence of lup-20 (29)-en-3-one as the major bioactive component.

ethyl acetate

lup-20 (29)-en-3-one


Input: B16 cells treated with lup-20 (29)-en-3-one increased melanin content without cytotoxicity.

lup-20 (29)-en-3-one


Input: To determine the mechanism for the observed effects of lup-20 (29)-en-3-one, the tyrosinase enzyme activity, the tyrosinase protein expression, and the activation of phosphorylated extracellular signal-regulated kinases 1 and 2 were determined.

lup-20 (29)-en-3-one


Input: In addition, the expression of the tyrosinase mRNA was quantified using real-time PCR.


Input: Results showed that lup-20 (29)-en-3-one has no effect on the tyrosinase enzyme activity but can increase tyrosinase expression at both the transcriptional and translational levels.

lup-20 (29)-en-3-one


Input: The increase in the tyrosinase mRNA expression was most likely due to the inhibited mitogen-activated protein kinase phosphorylated extracellular signal-regulated kinases 1 and 2 activation.


Input: We report for the first time that E. multiflora ethyl acetate extract and its active compound lup-20 (29)-en-3-one stimulate melanogenesis by increasing the tyrosinase enzyme expression via mitogen-activated protein kinase phosphorylated extracellular signal-regulated kinases 1 and 2 phosphorylation inhibition, making it a possible treatment for hypopigmentation diseases.

ethyl acetate

lup-20 (29)-en-3-one


Input: Peptide based macrocycles: selective histone deacetylase inhibitors with antiproliferative activity.


Input: Histone deacetylase inhibitors (HDACi) have been enthusiastically investigated as a novel generation of chemotherapeutics for cancers usually called as epigenetic therapeutics.


Input: Histone deacetylases have been found to influence cellular function by catalyzing the removal of acetyl groups from epsilon-N-acetylated lysine residues of several protein substrates including histones, transcription factors, alpha-tubulin, and nuclear importers.

epsilon-N-acetylated lysine


Input: Cyclic peptides represent the most structurally complicated and diverse class of histone deacetylase inhibitors.


Input: Each subtype of the Histone Deacetylase (HDAC) family perform a distinct role in the gene expression and cyclic peptides with their plentiful set of surface contacts, zinc binding group and macrocyclic cap, can target enzyme precisely through adequate modulation of the amino acid configurational and structural assortment.

zinc

amino acid


Input: The present article summarizes current status of different peptide based macrocyclic compounds being developed as HDACi for the treatment of cancer.


Input: Targeting multiplicity: the key factor for anti-cancer nanoparticles.


Input: In this mini-review, we focus on different strategies to bring nanotools specifically to cancer cells.


Input: We discuss about a better targeting of tumor, combining the characteristics of tumor environment, the increase in nanoparticles life time, the biomarkers overexpressed on cancer cells and different physical methods for non invasive therapies.


Input: Here we detail the necessity of a synergy between passive and active targeting for an actual specificity of cancer cells.


Input: Computational models for predicting interactions with membrane transporters.


Input: Membrane transporters, including two members: ATP-binding cassette (ABC) transporters and solute carrier (SLC) transporters are proteins that play important roles to facilitate molecules into and out of cells.

ATP


Input: Consequently, these transporters can be major determinants of the therapeutic efficacy, toxicity and pharmacokinetics of a variety of drugs.


Input: Considering the time and expense of bio-experiments taking, research should be driven by evaluation of efficacy and safety.


Input: Computational methods arise to be a complementary choice.


Input: In this article, we provide an overview of the contribution that computational methods made in transporters field in the past decades.


Input: At the beginning, we present a brief introduction about the structure and function of major members of two families in transporters.


Input: In the second part, we focus on widely used computational methods in different aspects of transporters research.


Input: In the absence of a high-resolution structure of most of transporters, homology modeling is a useful tool to interpret experimental data and potentially guide experimental studies.


Input: We summarize reported homology modeling in this review.


Input: Researches in computational methods cover major members of transporters and a variety of topics including the classification of substrates and/or inhibitors, prediction of protein-ligand interactions, constitution of binding pocket, phenotype of non-synonymous single-nucleotide polymorphisms, and the conformation analysis that try to explain the mechanism of action.


Input: As an example, one of the most important transporters P-gp is elaborated to explain the differences and advantages of various computational models.


Input: In the third part, the challenges of developing computational methods to get reliable prediction, as well as the potential future directions in transporter related modeling are discussed.


Input: Index of refraction, density, and solubility of ammonium iodide solutions at high pressure.

ammonium iodide


Input: An asymmetric moissanite anvil cell is used to study aqueous solutions of ammonium iodide at pressures up to 10 kbar.

moissanite

ammonium iodide


Input: The index of refraction is measured using the rotating Fabry-Perot technique, with an accuracy of approximately 1%.


Input: The mass density and molar volume of the solutions are estimated using the measured index values, and the molar volume is used to predict the pressure dependence of the solubility.


Input: The solubility derived from the index of refraction measurements is shown to agree with that which is determined by direct observation of the onset of crystallization.


Input: Antimalarial activities of 6-iodouridine and its prodrugs and potential for combination therapy.


Input: Resistance by Plasmodium falciparum to almost all clinically used antimalarial drugs requires the development of new classes of antimalarials.


Input: 6-Iodouridine (15), a novel and potent inhibitor of orotidine 5'-monophosphate decarboxylase (ODCase), exhibited efficacy in a mouse model infected by P. chabaudi chabaudi.

orotidine 5'-monophosphate


Input: Compound 15 exhibited promising antimalarial activity against P. falciparum, including drug-resistant isolates, and no rapid drug-resistant populations of the parasite were observed when challenged with 15.


Input: Uridine provided options to overcome any toxicity in the host but still suppressing the parasite load when treated with 15.

Uridine


Input: In drug combination studies, compound 15 showed good efficacy in vivo with artemisinin and azithromycin.

artemisinin

azithromycin


Input: The propionyl ester of 15 exhibited superior antimalarial efficacy.

propionyl ester


Input: Antimalarial activities of 15 and its prodrugs and potential for combination therapy are discussed in the context of novel strategies.


Input: Solution effect on diazonium-modified Au (111): reactions and structures.

diazonium

Au (111)


Input: Surface modifications of a Au (111) electrode with 4-bromobenzenediazonium tetrafluoroborate (BBD) in acetonitrile (ACN) and 0. 1 M HClO4 have been characterized by scanning tunneling microscopy (STM).

Au (111)

4-bromobenzenediazonium tetrafluoroborate

BBD

acetonitrile

ACN


Input: In ACN, STM results reveal the formation of disordered thin organic films.

ACN


Input: The involvement of the radical as an intermediate is evidenced by the negative effect of radical scavengers on organic thin film formation.


Input: In contrast, the 4, 4'-dibromobiphenyl monolayer is observed when the aqueous solution is used as a medium to carry out the grafting experiment.

4, 4'-dibromobiphenyl


Input: The biphenyl compound is considered to be generated by a radical-radical coupling reaction.

biphenyl


Input: Genome-wide integrated analyses of androgen receptor signaling in prostate cancer based on high-throughput technology.

androgen


Input: The androgen receptor (AR) is a steroid hormone receptor that functions as a ligand-dependent transcriptional factor, which plays a key role in the development and progression of prostate cancer.

androgen

steroid


Input: Recent advancement in high throughput technologies including microarrays and deep-sequencing provides unbiased genome-wide knowledge on the AR signaling including datasets for androgen-regulated gene expression and genomic binding sites for AR.

androgen


Input: In the present review, we will briefly summarize the main features of the AR signaling as well as the individual AR target genes identified by the integration of multiple datasets in prostate cancer.


Input: Cap analysis gene expression (CAGE) is also featured as a unique transcriptome method, which particularly determines the androgen-dependent transcription start points in prostate cancer.

androgen


Input: Recurrent rearrangements in prostate cancer: causes and therapeutic potential.


Input: DNA damage and genetic rearrangements are hallmarks of cancer.


Input: However, gene fusions as driver mutations in cancer have classically been a distinction in leukemia and other rare instances until recently with the discovery of gene fusion events occurring in 50 to 75% of prostate cancer patients.


Input: The discovery of the TMPRSS2-ERG fusion sparked an onslaught of discovery and innovation resulting in a delineation of prostate cancer via a molecular signature of gene fusion events.


Input: The increased commonality of high-throughput sequencing data coupled with improved bioinformatics approaches not only elucidated the molecular underpinnings of prostate cancer progression, but the mechanisms of gene fusion biogenesis.


Input: Interestingly, the androgen receptor (AR), already known to play a significant role in prostate cancer tumorigenesis, has recently been implicated in the processes resulting in gene fusions by inducing the spatial proximity of genes involved in rearrangements, promoting the formation of double-strand DNA breaks (DSB), and facilitating the recruitment of proteins for non-homologous end-joining (NHEJ).

androgen


Input: Our increased understanding of the mechanisms inducing genomic instability may lead to improved diagnostic and therapeutic strategies.


Input: To date, the majority of prostate cancer patients can be molecularly stratified based on their gene fusion status thereby increasing the potential for tailoring more specific and effective therapies.


Input: Targeting the akt kinase to modulate survival, invasiveness and drug resistance of cancer cells.


Input: The deregulation of oncogenic signaling pathways which provide survival advantages to tumor cells is mediated by multiple cellular networks.


Input: Among them, the PI3K-Akt-mTOR axis, in particular the serine/threonine kinase Akt, is recognized as a key player.

serine

threonine


Input: The kinase is hyperactivated due to a variety of mechanisms including loss of PTEN, mutations in the PI3K catalytic subunit, receptor tyrosine kinase and Ras activation.

tyrosine


Input: Indeed, inappropriate activation of the Akt kinase is a common event in human tumors and Akt appears to be a critical player in cell survival that may also account for the therapeutic resistance and the invasive phenotype of tumors.


Input: Inhibition of Akt signalling results in apoptosis and growth inhibition of tumour cells with elevated Akt activity.


Input: A functional role in drug resistance is supported by evidence that tumor cells with acquired resistance to antitumor agents may display increased Akt activation and that treatment with molecularly targeted agents can activate feed-back loops involving Akt.


Input: This serine/threonine kinase may therefore represent an amenable target for modulation of sensitivity to compounds with different molecular features due to its pleiotropic role in cell survival.

serine

threonine


Input: Different types of Akt inhibitors [i. e., ATP mimetics and pleckstrin-homology (PH) domain binders] have been generated and some of them have reached the clinical setting.

ATP


Input: The present review focuses on the i) mechanisms implicating Akt in increased survival and invasive potential of tumor cells of different tumor types and ii) on the development of Akt inhibitors as modulators of drug resistance.


Input: Emerging Role of Colloidal Drug Delivery Systems (CDDS) in NSAID Topical Administration.


Input: NSAIDs are the most commonly prescribed category of drugs for the treatment of musculoskeletal pain and inflammation associated with many conditions.


Input: Topical administration of these drugs is always the best choice since adverse effects occur commonly with systemic NSAID therapy.


Input: Colloidal drug delivery systems (CDDS) are interesting systems, which are able to improve the duration of drug residence in the skin and to allow an achievable drug sustained and controlled release compared to conventional topical formulations. This review focuses on micro and nanoemulsions, vesicular carriers and nanoparticles as novel high efficiency delivery systems of NSAIDs in topical applications.


Input: Rationally designed multi-targeted agents against neurodegenerative diseases.


Input: Neurodegenerative diseases are complex disorders with several pathoetiological pathways leading to cell death.


Input: Rationally designed multi-targeted agents, or " multi-targeted designed drugs " (MTDD) show significant promise in preclinical studies as neuroprotective and disease-modifying agents.


Input: In this review, we highlight the use of chemical scaffolds that lend themselves exquisitely to the development of MTDDs in neurodegeneration.


Input: Notably, synthetic polycyclic cage compounds have served as scaffolds for novel voltage-gated calcium channel blockers, NMDA receptor antagonists, and sigma-receptor ligands-attractive targets in neurodegeneration.

calcium

NMDA


Input: In an entirely different approach, compounds containing the thiazolidinedione moiety (referred to as glitazones) alter mitochondrial function through the mitochondrial protein mitoNEET, an attractive new drug target for the treatment of neurodegenerative diseases.

thiazolidinedione

glitazones


Input: The design strategy for yet another agent, ladostigil, employed the amalgamation of active chemical moieties of the AChE inhibitor rivastigmine, and the monoamine oxidase-B (MAO-B) inhibitor rasagiline, leading to a single compound that targets both enzymes simultaneously.

ladostigil

rivastigmine

monoamine

rasagiline


Input: Natural products have also served as design templates for several MTDD design studies.


Input: In particular, the stilbene scaffold has become popular in particular due to the neuroprotective effects of the non-flavonoid natural product resveratrol.

stilbene

flavonoid

resveratrol


Input: Recently, stilbene scaffold-based compounds were developed to reduce-through chelation with metal ions that interact with beta-amyloid-both metal-induced beta-amyloid protein aggregation, and ROS generated from this aggregate.

stilbene


Input: Other subtle modifications of the stilbene motif led to the creation of reversible, non-competitive MAO inhibitors.

stilbene


Input: Finally, compounds derived from the xanthine scaffold afford neuroprotection in Parkinson' s disease through mechanisms that include dual adenosine A2A receptor antagonism and MAO-B inhibition.

xanthine

adenosine


Input: Human disease and drug pharmacology, complex as real life.


Input: In the past decades drug discovery practice has escaped from the complexity of the formerly used phenotypic screening in animals to focus on assessing drug effects on isolated protein targets in the search for drugs that exclusively and potently hit one selected target, thought to be critical for a given disease, while not affecting at all any other target to avoid the occurrence of side-effects.


Input: However, reality does not conform to these expectations, and, conversely, this approach has been concurrent with increased attrition figures in late-stage clinical trials, precisely due to lack of efficacy and safety.


Input: In this context, a network biology perspective of human disease and treatment has burst into the drug discovery scenario to bring it back to the consideration of the complexity of living organisms and particularly of the (patho) physiological environment where protein targets are (mal) functioning and where drugs have to exert their restoring action.


Input: Under this perspective, it has been found that usually there is not one but several disease-causing genes and, therefore, not one but several relevant protein targets to be hit, which do not work on isolation but in a highly interconnected manner, and that most known drugs are inherently promiscuous.


Input: In this light, the rationale behind the currently prevailing single-target-based drug discovery approach might even seem a Utopia, while, conversely, the notion that the complexity of human disease must be tackled with complex polypharmacological therapeutic interventions constitutes a difficult-torefuse argument that is spurring the development of multitarget therapies.


Input: Photothermal tautomerization of a UV sunscreen (4-tert-butyl-4'-methoxydibenzoylmethane) in acetonitrile studied by steady-state and laser flash photolysis.

acetonitrile


Input: The photothermal tautomerization processes between enol and keto forms of 4-tert-butyl-4'-methoxydibenzoylmethane (trade name, Avobenzone) in acetonitrile have been studied by steady-state and laser flash photolysis.

enol

keto

Avobenzone

acetonitrile


Input: The keto form is produced upon photolysis of the enol in only acetonitrile with a quantum yield of 0. 014.

keto

enol

acetonitrile


Input: The molar absorptivity of the keto form was determined.

keto


Input: Phototautomerization from the keto to the enol form was not seen.

keto

enol


Input: Laser flash photolysis of the keto form recognized the formation of the triplet state.

keto


Input: In the dark, the keto form underwent thermal tautomerization to the enol with a lifetime of 5. 1 h at 295 K.

keto

enol


Input: The enolization rate in acetonitrile was not accelerated by the presence of alcohols and/or water but increased with increasing temperature and followed the Arrhenius expression.

acetonitrile

alcohols


Input: The activation energy and the frequency factor were determined for the enolization process from the keto to the enol form.

keto

enol


Input: On the basis of the energy states of the tautomers and isomers as estimated by DFT calculations, a schematic energy diagram was determined for the photothermal tautomerization processes in acetonitrile.

acetonitrile


Input: Newly observed spontaneous activation of ethephon as a butyrylcholinesterase inhibitor.

ethephon


Input: The plant growth regulator ethephon (2-chloroethylphosphonic acid) inhibits human butyrylcholinesterase (BChE) by making a covalent adduct on the active site serine 198.

ethephon

2-chloroethylphosphonic acid

serine


Input: Our goal was to extend earlier studies on ethephon inhibition.

ethephon


Input: Addition of freshly prepared ethephon to BChE in buffered medium, at pH 7. 0 and 22 degrees C, resulted in no inhibition initially.

ethephon


Input: However, inhibition developed progressively over 60 min of incubation.


Input: Preincubation of ethephon in pH 7-9 buffers increased its initial inhibitory potency.

ethephon


Input: These observations indicated that ethephon itself was not the inhibitor.

ethephon


Input: About 3% of the initial ethephon could be trapped as a BChE adduct.

ethephon


Input: Mass spectral analysis of the active site peptide from inhibited BChE showed that the inhibitor added a mass of 108 Da to the active site serine on peptide FGES198AGAAS.

serine


Input: This result rules out a previous hypothesis that ethephon adds HPO3 to BChE (added mass of 80 Da).

ethephon


Input: To accommodate these observations, we propose that in aqueous media at neutral to slightly alkaline pH about 3% of the ethephon is converted (t1/2 = 9. 9 h at pH 7. 0) into a cyclic oxaphosphetane which is the actual BChE inhibitor forming the 2-hydroxyethylphosphonate adduct on BChE at Ser198 while about 97% of the ethephon breaks down to ethylene (t1/2 = 11-48 h at pH 7. 0) which is responsible for plant growth regulation.

ethephon

cyclic oxaphosphetane

ethephon

ethylene


Input: Neural stem/progenitor cells display a low requirement for oxidative metabolism independent of hypoxia inducible factor-1alpha expression.


Input: Neural stem/progenitor cells (NSPCs) are multipotent cells within the embryonic and adult brain that give rise to both neuronal and glial cell lineages.


Input: Maintenance of NSPC multipotency is promoted by low oxygen tension, although the metabolic underpinnings of this trait have not been described.

oxygen


Input: In this study, we investigated the metabolic state of undifferentiated NSPCs in culture, and tested their relative reliance on oxidative versus glycolytic metabolism for survival, as well as their dependence on hypoxia inducible factor-1alpha (HIF-1 alpha) expression for maintenance of metabolic phenotype.


Input: Unlike primary neurons, NSPCs from embryonic and adult mice survived prolonged hypoxia in culture.


Input: In addition, NSPCs displayed greater susceptibility to glycolytic inhibition compared with primary neurons, even in the presence of alternative mitochondrial TCA substrates.

TCA


Input: NSPCs were also more resistant than neurons to mitochondrial cyanide toxicity, less capable of utilizing galactose as an alternative substrate to glucose, and more susceptible to pharmacological inhibition of the pentose phosphate pathway by 6-aminonicotinamide.

cyanide

galactose

glucose

pentose phosphate


Input: Inducible deletion of exon 1 of the Hif1a gene improved the ability of NSPCs to utilize pyruvate during glycolytic inhibition, but did not alter other parameters of metabolism, including their ability to withstand prolonged hypoxia.

pyruvate


Input: Taken together, these data indicate that NSPCs have a relatively low requirement for oxidative metabolism for their survival and that hypoxic resistance is not dependent upon HIF-1 alpha signaling.


Input: The in vitro and in vivo effects of nicotine on bone, bone cells and fracture repair.

nicotine


Input: INTRODUCTION: Cigarette smoke has negative effects on bone metabolism and fracture repair.


Input: However, no study has reviewed effects of nicotine on bone and fracture repair independent of other constituents of cigarette smoke.

nicotine


Input: The authors review the existing evidence of the effect of nicotine on' bone' and' bone cells' and fracture repair, drawing conclusions relevant to clinical practice and future research.

nicotine


Input: AREAS COVERED: A literature review was conducted using PRISMA guidelines and PubMed, Cochrane, MEDLINE/OVID, EMBASE, NHS Evidence and Google scholar databases.


Input: Articles were included if they specifically investigated the effects of nicotine on' bone' or fracture repair in animal or human models or in vitro effects on' bone cells'.

nicotine


Input: A total of 64 papers were included in this review, of which 15 were human in vitro studies and 49 animal studies wherein 9 were in vitro and 40 in vivo.


Input: In vivo studies of the effects of nicotine in animals demonstrated widespread effects on bone including osteoneogenesis, osseointegration, steady-state skeletal bone and genes and cytokines relevant to bone cell physiology and bone homeostasis.

nicotine


Input: In these studies, nicotine' s effects are predominately negative, inhibiting bone cell metabolism and fracture repair, whereas most in vitro studies reported biphasic responses in all bone cells except osteoclastic cells.

nicotine


Input: EXPERT OPINION: The review suggests that nicotine has effects on osteoneogenesis, osseointegration and steady-state skeletal bone in animal in vivo models, as well as effects on all' bone cells', via several mechanisms in both animal and human cell in vitro studies.

nicotine


Input: The effect of nicotine is dose-dependent, with higher concentrations having predominantly negative effects, whereas at low concentrations a stimulatory effect is seen.

nicotine


Input: Stimulatory effects on certain cells may indicate a possible, limited therapeutic role; advice regarding smoking cessation perioperatively should remain due to the other harmful components of cigarette smoke, but there may be scope for allowing the use of nicotine patches instead of complete abstention.

nicotine


Input: Further research into clinical outcomes is required before the exact response of bone and fracture repair in humans to nicotine is known.

nicotine


Input: Benchmark dose for estimation of cadmium reference level for osteoporosis in a Chinese female population.

cadmium


Input: In this study, the reference level of cadmium in urine and blood related with bone damage was assessed using benchmark dose in a Chinese female population.

cadmium


Input: Total of 338 women was recruited, and urine and blood samples were collected from each individual for determination of cadmium in urine (UCd) and blood (BCd).

cadmium


Input: Bone mineral density was measured by dual energy X-ray absorptiometry.


Input: BMD and BMDL were calculated corresponding to additional risk of 5% and 10%.


Input: With benchmark response (BMR) of 5%/10%, the BMD of BCd, UCd related with osteoporosis was 1. 88 mu g/L/3. 23 mu g/L and 5. 30 mu g/g crea/9. 06 mu g/g crea, and the BMDL-05 was 1. 39 mu g/L/2. 38 mu g/L and 3. 78 mu g/g crea/6. 36 mu g/g crea; the BMD of BCd, UCd related with low bone mass was 0. 95 mu g/L/3. 12 mu g/L and 3. 12 mu g/g crea/5. 87 mu g/g crea, and the BMDL-05 was 0. 72 mu g/L/1. 35 mu g/L and 2. 14 mu g/g crea/3. 99 mu g/g crea.


Input: The BMD of UCd in people over 60years old was much lower than that of people less than 60years old.


Input: BMD value was related with ages and effects biomarkers.


Input: Our data showed that BMD of UCd associated with osteoporosis was lower than that previously estimated.


Input: DNA damage and oxidative stress in human B lymphoblastoid cells after combined exposure to hexavalent chromium and nickel compounds.

hexavalent chromium

nickel


Input: In the present study, human B lymphoblastoid cells were exposed to potassium dichromate and/or nickel chloride for 24h or 48h.

potassium dichromate

nickel chloride


Input: The cell viability and DNA damage induced by these compounds was measured with the CCK-8 assay and Comet assay, respectively.


Input: In addition, the generation of reactive oxygen species (ROS) and the levels of malondialdehyde (MDA) were measured using commercially available kits.

oxygen

malondialdehyde

MDA


Input: Our results indicated that potassium dichromate could decrease cell viability and induce DNA damage in human B lymphoblastoid cells in a time-and concentration-dependent manner, but the toxicity of nickel chloride was not so obvious at concentrations used in our study.

potassium dichromate

nickel chloride


Input: The results of ROS showed that both two compounds could only induce weak elevation of ROS level, but MDA levels were significantly enhanced.

MDA


Input: Antagonistic effects of cytotoxicity were mainly found between Cr (VI) and Ni (II), and synergistic effects of DNA damage and oxidative stress were partially found between these two compounds.

Cr (VI)

Ni (II)


Input: Moreover, there were good correlations between the results of comet assay and the results of oxidative stress assays.


Input: It is suggested that synergistic DNA damage induced by simultaneously exposure of hexavalent chromium and nickel compounds is possibly related to oxidative stress.

hexavalent chromium

nickel


Input: Spiro heterocycles as potential inhibitors of SIRT1: Pd/C-mediated synthesis of novel N-indolylmethyl spiroindoline-3, 2'-quinazolines.

Pd

C

N-indolylmethyl spiroindoline-3, 2'-quinazolines


Input: Novel N-indolylmethyl substituted spiroindoline-3, 2'-quinazolines were designed as potential inhibitiors of SIRT1.

N-indolylmethyl substituted spiroindoline-3, 2'-quinazolines


Input: These compounds were synthesized in good yields by using Pd/C-Cu mediated coupling-cyclization strategy as a key step involving the reaction of 1-(prop-2-ynyl)-1' H-spiro [indoline-3, 2'-quinazoline]-2, 4' (3' H)-dione with 2-iodoanilides.

Pd

C-Cu

1-(prop-2-ynyl)-1' H-spiro [indoline-3, 2'-quinazoline]-2, 4' (3' H)-dione


Input: Some of the compounds synthesized have shown encouraging inhibition of Sir 2 protein (a yeast homologue of mammalian SIRT1) in vitro and three of them showed dose dependent inhibition of Sir 2.


Input: The docking results suggested that the benzene ring of 1, 2, 3, 4-tetrahydroquinazolin ring system of these molecules occupied the deep hydrophobic pocket of the protein and one of the NH along with the sulfonyl group participated in strong H-bonding interaction with the amino acid residues.

benzene

1, 2, 3, 4-tetrahydroquinazolin

NH

sulfonyl

H

amino acid


Input: Effects of salinomycin on human bone marrow-derived mesenchymal stem cells in vitro.

salinomycin


Input: Various hypotheses on the origin of cancer stem cells (CSCs) exist, including that CSCs develop from transformed human bone marrow mesenchymal stem cells (hBMSC).


Input: Since the polyether antibiotic salinomycin selectively kills CSCs, the present study aims to elucidate the effects of salinomycin on normal hBMSC.

salinomycin

salinomycin


Input: The immunophenotype of hBMSC after salinomycin exposure was observed by flow cytometry.

salinomycin


Input: The multi-differentiation capacity of hBMSC was evaluated by Oil Red O and van Kossa staining.

Oil Red O


Input: Cytotoxic effects of salinomycin were monitored by the [3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide] (MTT) assay.

salinomycin

3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide

MTT


Input: Furthermore, spheroid formation and migration capacity were assessed.


Input: There were no differences in the immunophenotype and multi-differentiation capacity of hBMSC induced by salinomycin treatment.

salinomycin


Input: Cytotoxic effects were observed at concentrations of 30 mu M and above.


Input: Neither the migration capability nor the ability to form spheroids was affected.


Input: Essential functional properties of hBMSC were unaffected by salinomycin.

salinomycin


Input: However, dose-dependent cytotoxicity effects could be observed.


Input: Overall, low dose salinomycin showed no negative effects on hBMSC.

salinomycin


Input: Since mesenchymal stem cells from various sources respond differently, further in vitro studies are needed to clarify the effect of salinomycin on tissue-specific stem cells.

salinomycin


Input: Regulatory decisions on endocrine disrupting chemicals should be based on the principles of endocrinology.


Input: For years, scientists from various disciplines have studied the effects of endocrine disrupting chemicals (EDCs) on the health and wellbeing of humans and wildlife.


Input: Some studies have specifically focused on the effects of low doses, i. e. those in the range that are thought to be safe for humans and/or animals.


Input: Others have focused on the existence of non-monotonic dose-response curves.


Input: These concepts challenge the way that chemical risk assessment is performed for EDCs.


Input: Continued discussions have clarified exactly what controversies and challenges remain.


Input: We address several of these issues, including why the study and regulation of EDCs should incorporate endocrine principles; what level of consensus there is for low dose effects; challenges to our understanding of non-monotonicity; and whether EDCs have been demonstrated to produce adverse effects.


Input: This discussion should result in a better understanding of these issues, and allow for additional dialog on their impact on risk assessment.


Input: Net analyte signal standard addition method for simultaneous determination of sulphadiazine and trimethoprim in bovine milk and veterinary medicines.

sulphadiazine

trimethoprim


Input: Net analyte signal standard addition method has been used for the simultaneous determination of sulphadiazine and trimethoprim by spectrophotometry in some bovine milk and veterinary medicines.

sulphadiazine

trimethoprim


Input: The method combines the advantages of standard addition method with the net analyte signal concept which enables the extraction of information concerning a certain analyte from spectra of multi-component mixtures.


Input: This method has some advantages such as the use of a full spectrum realisation, therefore it does not require calibration and prediction step and only a few measurements require for the determination.


Input: Cloud point extraction based on the phenomenon of solubilisation used for extraction of sulphadiazine and trimethoprim in bovine milk.

sulphadiazine

trimethoprim


Input: It is based on the induction of micellar organised media by using Triton X-100 as an extraction solvent.

Triton X-100


Input: At the optimum conditions, the norm of NAS vectors increased linearly with concentrations in the range of 1. 0-150. 0 mu molL (-1) for both sulphadiazine and trimethoprim.

sulphadiazine

trimethoprim


Input: The limits of detection (LOD) for sulphadiazine and trimethoprim were 0. 86 and 0. 92 mu molL (-1), respectively.

sulphadiazine

trimethoprim


Input: Anti-inflammatory effects of an aqueous extract of Welsh onion green leaves in mice.


Input: The anti-inflammatory effects of an aqueous extract of Welsh onion green leaves (WOE) in mice was investigated.


Input: Administration of WOE, in the range of 0. 25-1g/kg, showed a concentration dependent inhibition on paw edema development after carrageenan treatment in mice.


Input: The anti-inflammatory effects of WOE were closely attributed to decreased levels of tissue NO and tumor necrosis factor-alpha (TNF-alpha).

NO


Input: Further evidence for WOE' s protection is shown in the reduction of lipid oxidation and the increase of antioxidant enzyme activities, including catalase (CAT), superoxide dismutase (SOD), and glutathione peroxidase (GPX) in vivo.

superoxide

glutathione


Input: Further, WOE also decreased the number of acetic acid-induced writhing responses and formalin-induced pain in the late phase in mice.

acetic acid

formalin


Input: Overall, the results showed that WOE might serve as a natural source of anti-inflammatory compounds.


Input: Apple polyphenols suppress antigen presentation of ovalbumin by THP-1-derived dendritic cells.

polyphenols


Input: Apple polyphenol extract (AP) and procyanidin contained in AP were investigated for their immunomodulatory effects using THP-1-derived human dendritic cells (TDDCs).

polyphenol

procyanidin


Input: The expression levels of HLA-DR (MHC class II) and CD86 (costimulatory molecule) were measured as an indicator of antigen presentation in TDDCs.


Input: A significant decrease in HLA-DR expression was observed in the AP and fractionated procyanidin-treated cells in the presence of ovalbumin (OVA), but no effect on CD86 expression was observed.

procyanidin


Input: The uptake of OVA was not inhibited by AP treatment, and the gene expression of membrane-associated RING-CH ubiquitin E3 ligase, MARCH1, was up-regulated by AP treatment.


Input: It can therefore be presumed that AP suppresses HLA-DR expression via the ubiquitin-proteasome pathway.


Input: Furthermore, the up-regulation of IL-12 and TNF-alpha was found in the procyanidin trimers-treated cells in the presence of OVA.

procyanidin


Input: These results suggest that apple polyphenols would be an effective factor for the development of immunomodulatory agents with suppressive effects of antigen presentation.

polyphenols


Input: Comparison of extraction induced by emulsion breaking, ultrasonic extraction and wet digestion procedures for determination of metals in edible oil samples in Turkey using ICP-OES.


Input: The content of elements (Cd, Cr, Cu, Fe, Mn, Ni, Pb and Zn) in edible oils (sunflower, hazelnut, canola, corn and olive oils) from Turkey was determined using inductively coupled plasma optical emission spectrometry (ICP-OES) after ultrasonic extraction, wet digestion, and extraction induced by emulsion breaking procedures (EIEB).

Cd

Cr

Cu

Fe

Mn

Ni

Pb

Zn


Input: In order to evaluate the best sample preparation procedure, EIEB procedure was compared by ultrasonic extraction and wet digestion procedures.


Input: The results in the samples (minimum-maximum in mgkg (-1)) were: 0. 022-0. 058, Cr 0. 126-7. 106, Cu 0. 570-4. 504, Fe 8. 004-12. 588, Mn 0. 035-0. 054, Ni 0. 908-2. 182, Pb 0. 099-0. 134 and Zn 2. 206-8. 982.

Cr

Cu

Fe

Mn

Ni

Pb

Zn


Input: The EIEB procedure was found to be fast, reliable, simple, and excellent in comparison with the other studied procedures.


Input: The recovery test was performed by spiking the samples with known amounts of the metals in the form of organometallic standards and applying the EIEB procedure.


Input: The recoveries were in the range of 96-109%.


Input: Reduction of abdominal fat accumulation in rats by 8-week ingestion of a newly developed sweetener made from high fructose corn syrup.

fructose


Input: Many studies have shown that ingestion of high-fructose corn syrup (HFCS) may cause an increase in body weight and abdominal fat.

fructose


Input: We recently developed a new sweetener containing rare sugars (rare sugar syrup; RSS) by slight isomerization of HFCS.

sugars

sugar


Input: Here, the functional effects of RSS on body weight and abdominal fat, and biochemical parameters in Wistar rats were examined.


Input: Rats (n = 30) were randomly divided into three groups and maintained for 8-weeks on starch, starch + HFCS (50: 50), and starch + RSS (50: 50) diets.


Input: Rats in the Starch and HFCS groups gained significantly more body weight and abdominal fat than the RSS group.


Input: Fasting serum insulin in the RSS group was significantly lower than in the Starch and HFCS groups, although serum glucose in the HFCS and RSS groups was significantly lower than that in the Starch group.

glucose


Input: Thus, the substitution of HFCS with RSS prevents obesity induced by the consumption of HFCS.


Input: Analysis of the blackening of green pepper (Piper nigrum Linnaeus) berries.


Input: This paper investigates polyphenol oxidase (PPO) activity, reduced weight percentage after sun drying, and the changes in colour and appearance of green pepper (Piper nigrum Linnaeus) berries after blanching and sun drying.

polyphenol


Input: The results show that the degree of reduced weight percentage and browning in green pepper berries after blanching for 10 min is greater at 100 degrees C than at 90 and 80 degrees C.


Input: Moreover, the samples blanched at 100 degrees C for 10 min had the fastest water loss, but the lowest PPO activity.


Input: Thus, the PPO enzymatic oxidation of polyphenols might not be the only reason for the browning of green pepper berries.

polyphenols


Input: This result is significantly different from that of Variyar, Pendharkar, Banerjeea, and Bandyopadhyay (1988) and therefore deserves further study.


Input: Nutritional value and antioxidant activity of honeys produced in a European Atlantic area.


Input: One hundred eighty-seven honey samples from an Atlantic European area were studied to determine their nutritional compositions and antioxidant capacities, as well as the relationships between them.


Input: The results showed that heather, polyfloral, blackberry, and eucalyptus honeys had the highest carbohydrate contents, whereas honeydew and chestnut honeys had the lowest.

carbohydrate


Input: There were some important differences among the honey types, which were related to the presence of minor components.


Input: The protein contents were significantly higher in honeydew and chestnut honeys, and the same results were obtained for mineral contents.


Input: Related to the presence of several antioxidant compounds, heather honey had the highest phenolic content, whereas honeydew and chestnut honeys had the highest flavonoid contents.

flavonoid


Input: Multivariate analysis showed that some variables, such as the amounts of flavonoids, minerals, proteins, and phenols, were significantly correlated with antioxidant activity.

flavonoids

phenols


Input: The regression analysis produced a significant model (R (2) = 0. 716; F = 154. 680; P < 0. 001) that related the antioxidant activity and the flavonoids, K, and P contents.

flavonoids

K

P


Input: Assessment of antimicrobial and antiprotozoal activity of the olive oil macerate samples of Hypericum perforatum and their LC-DAD-MS analyses.


Input: Twenty-one samples of traditionally-prepared (home-made) and ready-made (commercial) St.


Input: John' s Wort olive oil macerates were profiled for their in vitro antimicrobial and antiprotozoal activity.


Input: Their cytotoxic potential was evaluated on MRC-5 fibroblasts.


Input: In the antiprotozoal assays, ten of the oils inhibited Trypanosoma brucei rhodesiense (IC (50) 15. 9-64. 5 mu g/mL), while only one oil exerted antimicrobial activity towards Staphylococcus aureus (IC (50) = 88. 7 mu g/mL).


Input: LC-DAD-MS data revealed the presence of pseudohypericin (0. 135-3. 280 mu g/g) and hypericin (0. 277-6. 634 mu g/g) in all the oils, whereas chlorogenic acid (1. 063 mu g/g) was detected only in one oil sample.

pseudohypericin

hypericin

chlorogenic acid


Input: Hyperforin was detected in four (0. 977-2. 399 mu g/g) and adhyperforin in six samples (0. 005-3. 165 mu g/g).

Hyperforin

adhyperforin


Input: Hypericin and pseudohypericin were common in the active oils, whereas hyperforin, adhyperforin, and chlorogenic acid were absent in these samples.

Hypericin

pseudohypericin

hyperforin

adhyperforin

chlorogenic acid


Input: Our results indicated that if the correct plant material is used, the infused oils from Hypericum perforatum may contain active components.


Input: Classification of Spanish extra virgin olive oils by data fusion of visible spectroscopic fingerprints and chemical descriptors.


Input: The potential of visible fingerprints and physical-chemical parameters in combination with multivariate data analysis was examined to classify extra virgin olive oils (EVOOs) from different Spanish regions according to their geographical origin.


Input: Firstly, spectral and quality parameters matrices were processed separately and subsequently were joined to evaluate the effect of synergy on the information obtained from the different methodologies.


Input: Linear discriminant analysis (LDA) and partial least squares discriminant analysis (PLS-DA) were performed as classification methods.


Input: The results revealed a perfect discrimination between the defined categories after performing PLS-DA on the Fused matrix, reaching 100% of correct classifications and showed a clear improvement in the overall prediction rates (92. 5%), so that the effect of synergy was confirmed.


Input: These accurate results emphasise the feasibility of the proposed strategy and encourage the development of similar approaches based on visible spectroscopy in olive oil quality and traceability determination.


Input: Anti-inflammatory effects of phenolic crude extracts from five fractions of Corchorus Olitorius L.


Input: Corchorus olitorius L.


Input: is grown in Taiwan during summer.


Input: Tender leaves are crushed and washed by running water before eating.


Input: Five fractions including crude phenolic extracts (using 80 per cent aqueous acetone) of whole plant, leaf, stem, washed leaf (WL) and dried water washing material (WW) were used in this study.

acetone


Input: Linoleic acid autoxidation inhibitions on all fractions were higher than that on alpha-tocopherol.

Linoleic acid

alpha-tocopherol


Input: Except for WL and WW, other fractions also showed DPPH radical scavenging efficiency.

DPPH


Input: The effect of all fractions on the regulation of inflammatory responses in lipopolysaccharide (LPS)-stimulated J774A. 1 macrophage cells was investigated.


Input: All fractions diminished LPS-induced protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase 2 (COX-2).

nitric oxide


Input: Nitric oxide (NO) and prostaglandin E2 (PGE (2)), downstream products, were also suppressed in dose-dependent manners, except for WL and WW.

Nitric oxide

NO

prostaglandin E2

PGE (2)


Input: Oxidative modification and loss of leaf phenolics after kneading and washing greatly affected DPPH radical scavenging and inflammatory responses.

phenolics

DPPH


Input: Storage stability of hen egg white powders in three protein/water dough model systems.


Input: In recent years, due to the specific health benefits associated with bioactive peptides and the reduction of protein allergenicity by enzymatic hydrolysis, the utilisation of protein hydrolysates in the intermediate-moisture food (IMF) market, such as high protein nutrition bars (HPNB), has significantly increased.


Input: Currently, no reported study is related to the storage stability of dried hen egg white (DEW) and its hydrolysates (HEW) in an IMF matrix.


Input: Therefore, three DEW/HEW dough model systems (100% HEW + 0% DEW, 75% HEW + 25% DEW and 50% HEW + 50% DEW) were established using two commercial spray-dried egg white powders to study the effect of temperature and fraction of HEW on these IMF models (water activity (a (w)): ~ 0. 8).


Input: During storage at three different temperatures (23, 35 and 45 degrees C) for 70 days, the selected physicochemical properties of the dough systems were compared.


Input: Overall, kinetic analysis showed an apparent zero-order model fit for the change in the colour (L (*)), fluorescence intensity (FI) and hardness, as a function of time, for different dough model systems.


Input: As expected, the L (*), FI and hardness increased as a function of time mainly due to the Maillard reaction.


Input: The amount of free amino groups decreased, with an increase in rate of loss, as temperature increased in the 100% HEW + 0% DEW model.

amino


Input: When DEW was substituted for some HEW, the regeneration of the free amino groups after loss was observed as a function of time.

amino


Input: Furthermore, when the percentage of HEW was decreased, the incidence of mouldy samples occurred sooner, which indicates that HEW has some antimicrobial ability, especially in the 100% HEW + 0% DEW system where mould growth did not occur.


Input: Investigation of isotope dilution mass spectrometric (ID-MS) method to determine niacin in infant formula, breakfast cereals and multivitamins.

niacin


Input: An isotope dilution LC/mass spectrometric (ID-LC/MS) method was developed as a candidate reference method for the accurate determination of niacin in infant formula, breakfast cereals and multivitamin.

niacin


Input: After spiking nicotinamide-d (4) as an internal standard, infant formula and breakfast cereal samples were hydrolysed under alkaline condition.

nicotinamide-d (4)


Input: Samples were then analysed in SRM mode to detect nicotinic acid and nicotinic acid-d (4) at m/z 124 --> 80 and 127 --> 84, respectively.

nicotinic acid

nicotinic acid-d (4)


Input: In the case of multivitamin sample that contains mainly free nicotinamide, LC/MS monitored nicotinamide and nicotinamide-d (4) at their SRM channels of m/z 123 --> 80 and m/z 127 --> 84, respectively, after simple extraction.

nicotinamide

nicotinamide

nicotinamide-d (4)


Input: The repeatability and reproducibility were tested for the validation of the developed ID/LC-MS method.


Input: Additionally, the developed analytical method was applied to determine total niacin contents in homogenised infant formula, homogenised multivitamin, and commercially available products including different types of infant formula, breakfast cereals, and multivitamin tablets.

niacin


Input: Hypolipidemic and antioxidant activities of thymoquinone and limonene in atherogenic suspension fed rats.

thymoquinone

limonene


Input: The hypolipidemic and antioxidant actions of thymoquinone (TQ) and limonene (LMN) were investigated by giving 1 ml of 10mg TQ or 200mg LMN suspension, by gavage in two equal doses (morning and evening) of 0. 5 ml each for 30 days, in rats, fed an atherogenic suspension.

thymoquinone

limonene

LMN

LMN


Input: These compounds effectively ameliorated all the altered cardiovascular risk parameters via a reduction in HMG-CoA reductase activity, along with an increase in arylesterase activity.

HMG-CoA


Input: The compounds significantly blocked the shift in buoyancy from less atherogenic lb-LDL to highly atherogenic sd-LDL, restoring the percent distribution of LDL-C and apoB into sd-LDL and lb-LDL to near normal levels.


Input: These compounds also blocked basal and maximal formation of CD and malondialdehyde, and lengthened the lag times of LDL, sd-LDL and lb-LDL in the order TQ > LMN.

malondialdehyde

LMN


Input: Our results strongly suggest an important therapeutic use of test compounds, especially TQ, in the prevention of cardiovascular disease risks parameters.


Input: Effects of sodium caseinate concentration and storage conditions on the oxidative stability of oil-in-water emulsions.

sodium


Input: The oxidative stability of various oils (sunflower, camelina and fish) and 20% oil-in-water (O/W) emulsions, were examined.


Input: The mean particle size decreased from 1179 to 325 nm as sodium caseinate (emulsifier) concentration was increased from 0. 25% to 3% in O/W emulsions (P < 0. 05).

sodium


Input: Increasing the microfluidisation pressure from 21 to 138 MPa, resulted in a particle size decrease from 289 to 194 nm (P < 0. 05).


Input: Emulsified oils had lower detectable lipid hydroperoxide and p-Anisidine values than their corresponding bulk oils (P < 0. 05).

hydroperoxide

p-Anisidine


Input: The lipid hydroperoxide and p-Anisidine values of emulsions generally decreased as sodium caseinate concentration increased, and similarly decreased as microfluidisation pressure increased (P < 0. 05).

hydroperoxide

p-Anisidine

sodium


Input: Increasing storage temperature of the emulsions from 5 to 60 degrees C, resulted in lower detectable lipid oxidation products during storage (P < 0. 05).


Input: Antioxidant activity and nutritional quality of traditional red-grained rice varieties containing proanthocyanidins.

proanthocyanidins


Input: Proanthocyanidin-containing rice varieties have been rarely reported.

Proanthocyanidin


Input: Antioxidant capacity, major antioxidant components, and nutritional parameters of eight traditional red-grained rice varieties containing proanthocyanidins grown in Sri Lanka were investigated.

proanthocyanidins


Input: The tested traditional red varieties, on the average, had over sevenfold higher both total antioxidant capacity and phenolic content than three light brown-grained new-improved rice varieties.


Input: Major antioxidant phenolic compounds identified in this study included proanthocyanidins, phenolic acids and gamma-oryzanols (ferulic acid derivatives).

phenolic

proanthocyanidins

phenolic acids

gamma-oryzanols

ferulic acid


Input: Proanthocyanidins were detected only in the traditional red varieties, but not found in new-improved ones.

Proanthocyanidins


Input: Most traditional red varieties also contained significantly higher levels of protein with well balanced amino acids and higher contents of fat, fibre and vitamin E (tocopherols and tocotrienols) than the new-improved ones.

amino acids

vitamin E

tocopherols

tocotrienols