Input: The efficiency of biotransformation in detoxification depended on the microorganism and steroid substrate used.

steroid


Input: Biotransformation was a relatively slow process as it also depended on the growth phase of the fungus.


Input: In addition to biotransformation, steroid extrusion out of the cells contributed to the lowering of the active intracellular steroid concentration.

steroid

steroid


Input: Plasma membrane Pdr5 transporter was found to be the most effective, followed by Snq2 transporter and vacuolar transporters Ybt1 and Ycf1.


Input: Proteins Aus1 and Dan1 were not found to be involved in steroid import.

steroid


Input: The research of possible targets of steroid hormone action in fungi suggests that steroid hormones inhibit ergosterol biosynthesis in S. cerevisiae and H. werneckii.

steroid

steroid

ergosterol


Input: Results of this inhibition caused changes in the sterol content of the cellular membrane.

sterol


Input: The presence of steroid hormones most probably causes the degradation of the Tat2 permease and impairment of tryptophan import.

steroid

tryptophan


Input: ADX71743, a potent and selective negative allosteric modulator of metabotropic glutamate receptor 7: in vitro and in vivo characterization.

glutamate


Input: Metabotropic glutamate receptor 7 (mGlu (7)) has been suggested to be a promising novel target for treatment of a range of disorders, including anxiety, post-traumatic stress disorder, depression, drug abuse, and schizophrenia.

glutamate


Input: Here we characterized a potent and selective mGlu (7) negative allosteric modulator (NAM) (+)-6-(2, 4-dimethylphenyl)-2-ethyl-6, 7-dihydrobenzo [d] oxazol-4 (5H)-one (ADX71743).

(+)-6-(2, 4-dimethylphenyl)-2-ethyl-6, 7-dihydrobenzo [d] oxazol-4 (5H)-one


Input: In vitro, Schild plot analysis and reversibility tests at the target confirmed the NAM properties of the compound and attenuation of L-(+)-2-amino-4-phosphonobutyric acid-induced synaptic depression confirmed activity at the native receptor.

L-(+)-2-amino-4-phosphonobutyric acid


Input: The pharmacokinetic analysis of ADX71743 in mice and rats revealed that it is bioavailable after s. c. administration and is brain penetrant (cerebrospinal fluid concentration/total plasma concentration ratio at C (max) = 5. 3%).


Input: In vivo, ADX71743 (50, 100, 150 mg/kg, s. c.) caused no impairment of locomotor activity in rats and mice or activity on rotarod in mice.


Input: ADX71743 had an anxiolytic-like profile in the marble burying and elevated plus maze tests, dose-dependently reducing the number of buried marbles and increasing open arm exploration, respectively.


Input: Whereas ADX71743 caused a small reduction in amphetamine-induced hyperactivity in mice, it was inactive in the mouse 2, 5-dimethoxy-4-iodoamphetamine-induced head twitch and the rat conditioned avoidance response tests.

amphetamine

2, 5-dimethoxy-4-iodoamphetamine


Input: In addition, the compound was inactive in the mouse forced swim test.


Input: These data suggest that ADX71743 is a suitable compound to help unravel the physiologic role of mGlu (7) and to better understand its implication in central nervous system diseases.


Input: Our in vivo tests using ADX71743, reported here, suggest that pharmacological inhibition of mGlu (7) is a valid approach for developing novel pharmacotherapies to treat anxiety disorders, but may not be suitable for treatment of depression or psychosis.


Input: Synthesis of substituted 6-amino-4-(2, 4-dimethoxyphenyl)-[1, 2] dithiolo [4, 3-b] pyrrol-5-ones and their raising leukocyte count activities.

6-amino-4-(2, 4-dimethoxyphenyl)-[1, 2] dithiolo [4, 3-b] pyrrol-5-ones


Input: The design and synthesis of a series of substituted 6-amino-4-(2, 4-dimethoxyphenyl)-[1, 2] dithiolo [4, 3-b] pyrrol-5-ones are described.

6-amino-4-(2, 4-dimethoxyphenyl)-[1, 2] dithiolo [4, 3-b] pyrrol-5-ones


Input: All the synthesized compounds were evaluated for raising leukocyte count activities in normal mice.


Input: Four compounds (8a, b, d, h) exhibited raising leukocyte count activities close or higher than positive control recombinant human granulocyte colony stimulating factor (rhG-CSF), and some (8e-g, k, p, r) had a moderate effect.


Input: Among them, the most potent compound 8a was evaluated for its antileukopenia activity in cyclophosphamide (CTX) treated mice.

cyclophosphamide


Input: Interestingly, 8a exhibited significant antileukopenia activity as compared to rhG-CSF.


Input: The results suggest that this kind of compounds might be utilized for the development of new candidate for treatment of leukocytopenia.


Input: Characterization of steroidogenic enzyme expression in aldosterone-producing adenoma: a comparison with various human adrenal tumors.

aldosterone


Input: We analyzed the expression profiles of several steroidogenic enzymes in normal adrenals, aldosterone-producing adenomas (APA), cortisol-producing adenomas combined with Cushing' s syndrome (CPA) or with subclinical Cushing' s syndrome (SCPA), and nonfunctioning adrenal adenomas (NFA) to clarify the nature and characteristics of steroidogenesis in APA.

aldosterone

cortisol


Input: Clinical data were collected for all subjects.


Input: In resected adrenal glands (normal adrenals, APA, CPA, SCPA, and NFA), the mRNA expression levels of the CYP17, HSD3B2, CYP11B1, and CYP11B2 genes were studied using real-time quantitative PCR and immunohistochemistry.


Input: The CYP11B2 mRNA level in APA was significantly higher than that in other groups.


Input: The CYP17/HSD3B2 ratio for mRNA in APA was significantly lower than those in the other groups.


Input: Low ratio of CYP17/HSD3B2 with high expression of CYP11B2 seems to explain steroidogenic characteristics of APA.


Input: A theoretical analysis of the effect of the hydrogenation of graphene to graphane on its mechanical properties.

graphene

graphane


Input: We investigated the effect of the hydrogenation of graphene to graphane on its mechanical properties using first-principles calculations based on density-functional theory.

graphene

graphane


Input: The hydrogenation reduces the ultimate strengths in all three tested deformation modes--armchair, zigzag, and biaxial--and the in-plane stiffness by 1/3.


Input: The Poisson ratio was reduced from 0. 178 to 0. 078, a 56% decrease.


Input: However, the ultimate strain in zigzag deformation was increased by 8. 7%.


Input: The shear mode elastic constants are more sensitive than longitudinal ones to hydrogenation.


Input: The fourth and fifth order longitudinal mode elastic constants are inert to the hydrogenation, in contrast to a large decrease of those in second and third order.


Input: The hydrogenation does not change the monotonic decrement of the Poisson ratio with increasing pressure, but the rate is tripled.


Input: Our results indicate that graphene-graphane systems could be used for hydrogen storage with high speed of charge-discharge of hydrogen.

graphene

graphane

hydrogen

hydrogen


Input: (4, 4')-Bipyridine in vacuo and in solvents: a quantum chemical study of a prototypical floppy molecule from a molecular transport perspective.

(4, 4')-Bipyridine


Input: We report results of quantum chemical calculations for the neutral and anionic species of (4, 4')-bipyridine (44BPY), a prototypical molecule with a floppy degree of freedom, placed in vacuo and in solvents.

(4, 4')-bipyridine


Input: In addition to equilibrium geometries and vibrational frequencies and spectra, we present adiabatic energy curves for the vibrational modes with significant intramolecular reorganization upon charge transfer.


Input: Special attention is paid to the floppy strongly anharmonic degree of freedom of 44BPY, which is related to the most salient structural feature, namely the twist angle theta between the two pyridine rings.

pyridine


Input: The relevance of the present results for molecular transport will be emphasized.


Input: We show that the solvent acts as a selective gate electrode and propose a scissor operator to account for solvent effects on molecular transport.


Input: Our result on the conductance G vs. cos (2) theta is consistent with a significant transmission in perpendicular conformation indicated by previous microscopic analysis.


Input: Detailed mechanism for the orthogonal polarization switching of gold nanorod plasmons.


Input: In this work, we describe an electro-optic material capable of orthogonally switching the polarization of the localized surface plasmon resonance scattering of single gold nanorods, independent of their orientation.


Input: Liquid crystal samples are prepared in a sandwich configuration with electrodes arranged so that an applied voltage induces alignment-switching of the liquid crystal molecules covering individual gold nanorods.


Input: Due to the birefringence of the nematic liquid crystal, the reorientation in the nematic director alignment causes a change in the output polarization of the scattered light.


Input: We propose the underlying mechanism to be based on a homogeneous nematic to twisted nematic phase transition and provide support for it via Jones calculus by modelling the effect of ideally aligned homogeneous nematic and twisted nematic phases on polarized light transmitted through the sample.


Input: In the model, we include the effects of sample thickness and surface plasmon resonance wavelength, expressed in terms of the phase retardation, chi, on the observed output polarization.


Input: We find four distinctively different trends for the output polarization as a function of the incident polarization as chi is varied.


Input: Two of these cases provide reproducible orthogonal polarization switching of the surface plasmon resonance while maintaining a high degree of polarization.


Input: These results are verified experimentally with liquid crystal cells of different thicknesses.


Input: The deviation of the experimental samples from ideal behaviour can be explained by the inherent variations in the surface plasmon resonance maximum and local cell thickness.


Input: 5-cholesten-3 beta, 25-diol 3-sulfate decreases lipid accumulation in diet-induced nonalcoholic fatty liver disease mouse model.

5-cholesten-3 beta, 25-diol 3-sulfate


Input: Sterol regulatory element-binding protein-1c (SREBP-1c) increases lipogenesis at the transcriptional level, and its expression is upregulated by liver X receptor alpha (LXR alpha).


Input: The LXR alpha/SREBP-1c signaling may play a crucial role in the pathogenesis of nonalcoholic fatty liver disease (NAFLD).


Input: We previously reported that a cholesterol metabolite, 5-cholesten-3 beta, 25-diol 3-sulfate (25HC3S), inhibits the LXR alpha signaling and reduces lipogenesis by decreasing SREBP-1c expression in primary hepatocytes.

cholesterol

5-cholesten-3 beta, 25-diol 3-sulfate


Input: The present study aims to investigate the effects of 25HC3S on lipid homeostasis in diet-induced NAFLD mouse models.


Input: NAFLD was induced by feeding a high-fat diet (HFD) in C57BL/6J mice.


Input: The effects of 25HC3S on lipid homeostasis, inflammatory responses, and insulin sensitivity were evaluated after acute treatments or long-term treatments.


Input: Acute treatments with 25HC3S decreased serum lipid levels, and long-term treatments decreased hepatic lipid accumulation in the NAFLD mice.


Input: Gene expression analysis showed that 25HC3S significantly suppressed the SREBP-1c signaling pathway that was associated with the suppression of the key enzymes involved in lipogenesis: fatty acid synthase, acetyl-CoA carboxylase 1, and glycerol-3-phosphate acyltransferase.

fatty acid

acetyl-CoA


Input: In addition, 25HC3S significantly reduced HFD-induced hepatic inflammation as evidenced by decreasing tumor necrosis factor and interleukin 1 alpha/beta mRNA levels.


Input: A glucose tolerance test and insulin tolerance test showed that 25HC3S administration improved HFD-induced insulin resistance.

glucose


Input: The present results indicate that 25HC3S as a potent endogenous regulator decreases lipogenesis, and oxysterol sulfation can be a key protective regulatory pathway against lipid accumulation and lipid-induced inflammation in vivo.


Input: From the bottom up: dimensional control and characterization in molecular monolayers.


Input: Self-assembled monolayers are a unique class of nanostructured materials, with properties determined by their molecular lattice structures, as well as the interfaces with their substrates and environments.


Input: As with other nanostructured materials, defects and dimensionality play important roles in the physical, chemical, and biological properties of the monolayers.


Input: In this review, we discuss monolayer structures ranging from surfaces (two-dimensional) down to single molecules (zero-dimensional), with a focus on applications of each type of structure, and on techniques that enable characterization of monolayer physical properties down to the single-molecule scale.


Input: Oxygen tracer diffusion along interfaces of strained Y2O3/YSZ multilayers.

Oxygen

YSZ


Input: Heterophase boundaries can offer fast transport paths in solid electrolyte materials.


Input: In recent studies an enhancement of the ionic conductivity was indeed observed in micro-/nanoscaled Y (2) O (3)-stabilised ZrO (2) (YSZ) composites and hetero multilayers of thin films.

Y (2) O (3)

ZrO (2)

YSZ


Input: As space charge regions can be neglected due to high charger carrier concentrations, we assume that strain and microstructural changes at the heterophase boundaries are responsible for the observed conductivity effects.


Input: In order to obtain independent information on the role of heterophase boundaries for fast transport in strained solid electrolytes, systematic measurements of the (18) O-tracer diffusion coefficient in nanoscaled YSZ/Y (2) O (3) multilayers were performed.

(18) O

YSZ

Y (2) O (3)


Input: Multilayer samples were prepared by Pulsed Laser Deposition (PLD) on (0001) Al (2) O (3) substrates and characterised by X-Ray Diffraction (XRD), Scanning Electron Microscopy (HRSEM) and Time-of-Flight Secondary Ion Mass Spectrometry (ToF-SIMS).

Al (2) O (3)


Input: To separate interface and bulk transport from the total oxygen diffusivity of the multilayer system, the (average) thickness of the YSZ-layers in the multilayers was varied from 45 nm to 12 nm.

oxygen

YSZ


Input: Upon decreasing the thickness of the YSZ layers, respectively increasing the density of parallel interfaces, the total diffusion coefficient of the multilayer system is increased by a factor of 2 compared to bulk YSZ.

YSZ

YSZ


Input: The experimental results agree well with formerly published data for ionic conductivity measurements.


Input: They also support a negligible contribution of partial electronic conductivity in the multilayer.


Input: Oral exposure to industrial effluent with exceptionally high levels of drugs does not indicate acute toxic effects in rats.


Input: The Patancheru area near Hyderabad in India is recognized as a key link in the global supply chain for many bulk drugs.


Input: A central treatment plant receives wastewater from approximately 90 different manufacturers, and the resulting complex effluent has contaminated surface, ground, and drinking water in the region.


Input: Ecotoxicological testing of the effluent has shown adverse effects for several organisms, including aquatic vertebrates, at high dilutions.


Input: In addition, a recent study of microbial communities in river sediment indicated that the contamination of antibiotic substances might contribute to the emergence and spread of antibiotic resistance genes.


Input: In an attempt to start investigating how exposure to effluent-contaminated water may directly affect humans and other terrestrial vertebrates, rats were tube-fed effluent.


Input: Several pharmaceuticals present in the effluent could be detected in rat blood serum at low concentrations.


Input: However, results from exploratory microarray and quantitative polymerase chain reaction assays indicated no marked effects on hepatic gene transcription after 5 d of exposure.


Input: Clinical analysis of blood serum constituents, used as biomarkers for human disease did not reveal any significant changes, nor was there an effect on weight gain.


Input: The authors could not find evidence for any acute toxicity in the rat; however, the authors cannot rule out that was there an effect on weight gain higher doses of effluent or a longer exposure time may still be associated with risks for terrestrial vertebrates.


Input: Iron L-edge X-ray absorption spectroscopy of oxy-picket fence porphyrin: experimental insight into Fe-O2 bonding.

Iron

porphyrin

Fe


Input: The electronic structure of the Fe-O (2) center in oxy-hemoglobin and oxy-myoglobin is a long-standing issue in the field of bioinorganic chemistry.

Fe

O (2)


Input: Spectroscopic studies have been complicated by the highly delocalized nature of the porphyrin, and calculations require interpretation of multideterminant wave functions for a highly covalent metal site.

porphyrin


Input: Here, iron L-edge X-ray absorption spectroscopy, interpreted using a valence bond configuration interaction multiplet model, is applied to directly probe the electronic structure of the iron in the biomimetic Fe-O (2) heme complex [Fe (pfp) (1-MeIm) O (2)] (pfp (" picket fence porphyrin ") = meso-tetra (alpha, alpha, alpha, alpha-o-pivalamidophenyl) porphyrin or TpivPP).

iron

iron

Fe

O (2) heme

[Fe (pfp) (1-MeIm) O (2)]

pfp

picket fence porphyrin

meso-tetra (alpha, alpha, alpha, alpha-o-pivalamidophenyl) porphyrin

TpivPP


Input: This method allows separate estimates of sigma-donor, pi-donor, and pi-acceptor interactions through ligand-to-metal charge transfer and metal-to-ligand charge transfer mixing pathways.


Input: The L-edge spectrum of [Fe (pfp) (1-MeIm) O (2)] is further compared to those of [Fe (II) (pfp) (1-MeIm) (2)], [Fe (II) (pfp)], and [Fe (III) (tpp) (ImH) (2)] Cl (tpp = meso-tetraphenylporphyrin) which have Fe (II) S = 0, Fe (II) S = 1, and Fe (III) S = 1/2 ground states, respectively.

[Fe (pfp) (1-MeIm) O (2)]

[Fe (II) (pfp) (1-MeIm) (2)]

[Fe (II) (pfp)]

[Fe (III) (tpp) (ImH) (2)] Cl

tpp

meso-tetraphenylporphyrin

Fe (II)

Fe (II)

Fe (III)


Input: These serve as references for the three possible contributions to the ground state of oxy-pfp.

oxy-pfp


Input: The Fe-O (2) pfp site is experimentally determined to have both significant sigma-donation and a strong pi-interaction of the O (2) with the iron, with the latter having implications with respect to the spin polarization of the ground state.

Fe

O (2) pfp

O (2)

iron


Input: Probing the Bonding and Electronic Structure of Single Atom Dopants in Graphene with Electron Energy Loss Spectroscopy.

Graphene


Input: A combination of scanning transmission electron microscopy, electron energy loss spectroscopy, and ab initio calculations reveal striking electronic structure differences between two distinct single substitutional Si defect geometries in graphene.

Si

graphene


Input: Optimised acquisition conditions allow for exceptional signal-to-noise levels in the spectroscopic data.


Input: The near-edge fine structure can be compared with great accuracy to simulations and reveal either an sp (3)-like configuration for a trivalent Si or a more complicated hybridized structure for a tetravalent Si impurity.

Si

Si


Input: Controlling the pulsed-laser-induced size reduction of Au and Ag nanoparticles via changes in the external pressure, laser intensity, and excitation wavelength.

Au

Ag


Input: The laser-induced size reduction of aqueous noble metal nanoparticles has been the subject of intensive research, because of the mechanistic interest in the light-nanoparticle interactions and its potential application to size control.


Input: The photothermal evaporation hypothesis has gained solid support.


Input: However, the polydispersity of the final products is considered as an inherent drawback of the method.


Input: It is likely that the polydispersity arises from the uncontrolled heat dissipation caused by vapor bubble formation in the ambient atmosphere.


Input: To overcome this problem, we applied high pressures of 30-100 MPa.


Input: The particle size was regulated by adjusting three parameters: the pressure, laser intensity, and excitation wavelength.


Input: For example, starting from a colloidal solution of 100 nm diameter gold nanoparticles, highly monodisperse (+/- 3-5%) spheres with various diameters ranging from 90 to 30 nm were fabricated by tuning the laser intensity at 100 MPa, using an excitation wavelength of 532 nm.


Input: Further size reduction of the diameter to 20 nm was achieved by reducing the pressure and switching the excitation wavelength to 355 nm.


Input: It was found that the application of high pressures led to the heat loss-controlled size-reduction of the gold nanoparticles.


Input: More complicated results were obtained for 100 nm silver nanoparticles, possibly because of the different size-dependent light-absorbing nature of these particles.

silver


Input: Based on our extensive experimental studies, a detailed picture was developed for the nanosecond laser-induced fabrication of gold and silver nanoparticles, leading to unprecedented size control.

silver


Input: Multimode multidrop serial coalescence effects during condensation on hierarchical superhydrophobic surfaces.


Input: The prospect of enhancing the condensation rate by decreasing the maximum drop departure diameter significantly below the capillary length through spontaneous drop motion has generated significant interest in condensation on superhydrophobic surfaces (SHS).


Input: The mobile coalescence leading to spontaneous drop motion was initially reported to occur only on hierarchical SHS, consisting of both nanoscale and microscale topological features.


Input: However, subsequent studies have shown that mobile coalescence also occurs on solely nanostructured SHS.


Input: Thus, recent focus has been on understanding the condensation process on nanostructured surfaces rather than on hierarchical SHS.


Input: In this work, we investigate the impact of microscale topography of hierarchical SHS on the droplet coalescence dynamics and wetting states during the condensation process.


Input: We show that isolated mobile and immobile coalescence between two drops, almost exclusively focused on in previous studies, are rare.


Input: We identify several new droplet shedding modes, which are aided by tangential propulsion of mobile drops.


Input: These droplet shedding modes comprise of multiple droplets merging during serial coalescence events, which culminate in formation of a drop that either departs or remains anchored to the surface.


Input: We directly relate postmerging drop adhesion to formation of drops in nanoscale as well as microscale Wenzel and Cassie-Baxter wetting states.


Input: We identify the optimal microscale feature spacing of the hierarchical SHS, which promotes departure of the highest number of microdroplets.


Input: This optimal surface architecture consists of microscale features spaced close enough to enable transition of larger droplets into micro-Cassie state yet, at the same time, provides sufficient spacing in-between the features for occurrence of mobile coalescence.


Input: Novel strategy for preparation of graphene-Pd, Pt composite, and its enhanced electrocatalytic activity for alcohol oxidation.

graphene

Pd

Pt

alcohol


Input: As advanced electrodes for direct alcohol fuel cells, graphene-Pd and graphene-Pt composites with a trace of SnO (2) have been successfully synthesized by a modified electroless plating technique.

alcohol

graphene

Pd

graphene

Pt

SnO (2)


Input: The surface of graphene oxide is first sensitized by Sn (2 +) ions, and subsequently, Pd or Pt nanoparticles are deposited on the surface of graphene oxide.

graphene oxide

Sn (2 +)

Pd

Pt

graphene oxide


Input: Finally, graphene oxide was reduced to graphene by further adding NaBH (4).

graphene oxide

graphene

NaBH (4)


Input: Compared to other carbon-(e. g., Vulcan XC-72R) supported Pd and Pt, the resultant graphene-Pd and Pt composites exhibit better electrocatalytic activity and long-term stability toward alcohol electrooxidation.

carbon

Vulcan XC-72R

Pd

Pt

graphene

Pd

Pt

alcohol


Input: Additionally, a trace amount of SnO (2) formed around active catalysts may also be beneficial to the enhancement of electrochemical activity.

SnO (2)


Input: Simple strategy to functionalize polymeric substrates via surface-initiated ATRP for biomedical applications.


Input: The functionalization of polymer surfaces via surface-initiated atom transfer radical polymerization (ATRP) is of crucial importance to prepare various functional materials.


Input: It is generally complicated to conduct ATRP on different organic material surfaces.


Input: In this work, a facile photoinduced one-step method was first developed for the covalent immobilization of ATRP initiators on the C-H group-containing substrates such as biaxially oriented polypropylene (BOPP).

C-H

polypropylene


Input: The C-H bonds of precise location of inert polymer surfaces were readily transferred to bromoalkyl initiator, followed by ATRP of 2-(dimethylamino) ethyl methacrylate (DMAEMA) and glycidyl methacrylate (GMA), respectively, to produce the resultant patterned BOPP-g-P (DMAEMA) and BOPP-g-P (GMA) films.

C-H

bromoalkyl

2-(dimethylamino) ethyl methacrylate

DMAEMA

glycidyl methacrylate

GMA

P (DMAEMA)

P (GMA)


Input: The epoxy groups of the P (GMA) microdomains can be aminated for covalently coupling IgG, while the P (DMAEMA) microdomains were used for immobilizing IgG via electronic interactions.

epoxy

P (GMA)

P (DMAEMA)


Input: The resultant IgG-coupled microdomains could interact with the corresponding target proteins, anti-IgG.


Input: Selective inhibitors and tailored activity probes for lipoprotein-associated phospholipase A (2).


Input: Lipoprotein-associated phospholipase A (2) (Lp-PLA (2) or PLA (2) G7) binds to low-density lipoprotein (LDL) particles, where it is thought to hydrolyze oxidatively truncated phospholipids.


Input: Lp-PLA (2) has also been implicated as a pro-tumorigenic enzyme in human prostate cancer.


Input: Several inhibitors of Lp-PLA (2) have been described, including darapladib, which is currently in phase 3 clinical development for the treatment of atherosclerosis.

darapladib


Input: The selectivity that darapladib and other Lp-PLA (2) inhibitors display across the larger serine hydrolase family has not, however, been reported.

darapladib

serine


Input: Here, we describe the use of both general and tailored activity-based probes for profiling Lp-PLA (2) and inhibitors of this enzyme in native biological systems.


Input: We show that both darapladib and a novel class of structurally distinct carbamate inhibitors inactivate Lp-PLA (2) in mouse tissues and human cell lines with high selectivity.

darapladib

carbamate


Input: Our findings thus identify both inhibitors and chemoproteomic probes that are suitable for investigating Lp-PLA (2) function in biological systems.


Input: Identification of benzofuran central cores for the inhibition of leukotriene A (4) hydrolase.

benzofuran

leukotriene A (4)


Input: Leukotrienes (LT' s) are known to play a physiological role in inflammatory immune response.

Leukotrienes


Input: Leukotriene A (4) hydrolase (LTA (4) H) is a cystolic enzyme that stereospecifically catalyzes the transformation of LTA (4) to LTB (4).

Leukotriene A (4)

LTA (4)

LTB (4)


Input: LTB (4) is a known pro-inflammatory mediator.

LTB (4)


Input: This paper describes the identification and synthesis of substituted benzofurans as LTH (4) H inhibitors.

benzofurans


Input: The benzofuran series demonstrated reduced mouse and human whole blood LTB (4) levels in vitro and led to the identification one analog for advanced profiling.

benzofuran

LTB (4)


Input: Benzofuran 28 showed dose responsive target engagement and provides a useful tool to explore a LTA (4) H inhibitor for the treatment of inflammatory diseases, such as asthma and inflammatory bowel disease (IBD).

Benzofuran


Input: Cell-cycle and DNA damage regulation of the DNA mismatch repair protein Msh2 occurs at the transcriptional and post-transcriptional level.


Input: DNA mismatch repair during replication is a conserved process essential for maintaining genomic stability.


Input: Mismatch repair is also implicated in cell-cycle arrest and apoptosis after DNA damage.


Input: Because yeast and human mismatch repair systems are well conserved, we have employed the budding yeast Saccharomyces cerevisiae to understand the regulation and function of the mismatch repair gene MSH2.


Input: Using a luciferase-based transcriptional reporter, we defined a 218-bp region upstream of MSH2 that contains cell-cycle and DNA damage responsive elements.


Input: The 5' end of the MSH2 transcript was mapped by primer extension and was found to encode a small upstream open reading frame (uORF).


Input: Mutagenesis of the uORF start codon or of the uORF stop codon, which creates a continuous reading frame with MSH2, increased Msh2 steady-state protein levels ~ 2-fold.


Input: Furthermore, we found that the cell-cycle transcription factors Swi6, Swi4, and Mbp1-along with SCB/MCB cell-cycle binding sites upstream of MSH2-are all required for full basal expression of MSH2.


Input: Mutagenesis of the cell-cycle boxes resulted in a minor reduction in basal Msh2 levels and a 3-fold defect in mismatch repair.


Input: Disruption of the cell-cycle boxes also affected growth in a DNA polymerase-defective strain background where mismatch repair is essential, particularly in the presence of the DNA damaging agent methyl methane sulfonate (MMS).

methyl methane sulfonate

MMS


Input: Promoter replacements conferring constitutive expression of MSH2 revealed that the transcriptional induction in response to MMS is required to maintain induced levels of Msh2.

MMS


Input: Turnover experiments confirmed an elevated rate of degradation in the presence of MMS.

MMS


Input: Taken together, the data show that the DNA damage regulation of Msh2 occurs at the transcriptional and post-transcriptional levels.


Input: The transcriptional and translational control elements identified are conserved in mammalian cells, underscoring the use of yeast as a model system to examine the regulation of MSH2.


Input: 3, 4-Methylenedioxy-methamphetamine induces in vivo regional up-regulation of central nicotinic receptors in rats and potentiates the regulatory effects of nicotine on these receptors.

3, 4-Methylenedioxy-methamphetamine

nicotine


Input: Nicotine (NIC), the main psychostimulant compound of smoked tobacco, exerts its effects through activation of central nicotinic acetylcholine receptors (nAChR), which become up-regulated after chronic administration.

Nicotine

NIC

acetylcholine


Input: Recent work has demonstrated that the recreational drug 3, 4-methylenedioxy-methamphetamine (MDMA) has affinity for nAChR and also induces up-regulation of nAChR in PC 12 cells.

3, 4-methylenedioxy-methamphetamine

MDMA


Input: Tobacco and MDMA are often consumed together.

MDMA


Input: In the present work we studied the in vivo effect of a classic chronic dosing schedule of MDMA in rats, alone or combined with a chronic schedule of NIC, on the density of nAChR and on serotonin reuptake transporters.

MDMA

NIC

serotonin


Input: MDMA induced significant decreases in [(3) H] paroxetine binding in the cortex and hippocampus measured 24h after the last dose and these decreases were not modified by the association with NIC.

MDMA

[(3) H] paroxetine

NIC


Input: In the prefrontal cortex, NIC and MDMA each induced significant increases in [(3) H] epibatidine binding (29. 5 and 34. 6%, respectively) with respect to saline-treated rats, and these increases were significantly potentiated (up to 72. 1%) when the two drugs were associated.

NIC

MDMA

[(3) H] epibatidine


Input: Also in this area, [(3) H] methyllycaconitine binding was increased a 42. 1% with NIC + MDMA but not when they were given alone.

[(3) H] methyllycaconitine

NIC

MDMA


Input: In the hippocampus, MDMA potentiated the alpha 7 regulatory effects of NIC (raising a 25. 5% increase to 52. 5%) but alone was devoid of effect.

MDMA

NIC


Input: MDMA had no effect on heteromeric nAChR in striatum and a coronal section of the midbrain containing superior colliculi, geniculate nuclei, substantia nigra and ventral tegmental area.

MDMA


Input: Specific immunoprecipitation of solubilised receptors suggests that the up-regulated heteromeric nAChRs contain alpha 4 and beta 2 subunits.


Input: Western blots with specific alpha 4 and alpha 7 antibodies showed no significant differences between the groups, indicating that, as reported for nicotine, up-regulation caused by MDMA is due to post-translational events rather than increased receptor synthesis.

nicotine

MDMA


Input: Cloning, expression and analysis of the olfactory glutathione S-transferases in coho salmon.

glutathione S


Input: The glutathione S-transferases (GSTs) provide cellular protection by detoxifying xenobiotics, maintaining redox status, and modulating secondary messengers, all of which are critical to maintaining olfaction in salmonids.

glutathione S


Input: Here, we characterized the major coho salmon olfactory GSTs (OlfGSTs), namely omega, pi, and rho subclasses.


Input: OlfGST omega contained an open reading frame of 720bp and encoded a protein of 239 amino acids.

amino acids


Input: OlfGST pi and OlfGST rho contained open reading frames of 627 and 681nt, respectively, and encoded proteins of 208 and 226 amino acids.

amino acids


Input: Whole-protein mass spectrometry yielded molecular weights of 29, 950, 23, 354, and 26, 655Da, respectively, for the GST omega, pi, and rho subunits.


Input: Homology modeling using four protein-structure prediction algorithms suggest that the active sites in all three OlfGST isoforms resembled counterparts in other species.


Input: The olfactory GSTs conjugated prototypical GST substrates, but only OlfGST rho catalyzed the demethylation of the pesticide methyl parathion.

methyl parathion


Input: OlfGST pi and rho exhibited thiol oxidoreductase activity toward 2-hydroxyethyl disulfide (2-HEDS) and conjugated 4-hydroxynonenal (HNE), a toxic aldehyde with neurodegenerative properties.

thiol

2-hydroxyethyl disulfide

HNE

aldehyde


Input: The kinetic parameters for OlfGST pi conjugation of HNE were K (M) = 0. 16 +/- 0. 06mM and V (max) = 0. 5 +/- 0. 1 mu molmin-(1) mg-(1), whereas OlfGST rho was more efficient at catalyzing HNE conjugation (K (M) = 0. 022 +/- 0. 008 mM and V (max) = 0. 47 +/- 0. 05 mu molmin-(1) mg-(1)).

HNE

HNE


Input: Our findings indicate that the peripheral olfactory system of coho expresses GST isoforms that detoxify certain electrophiles and pesticides and that help maintain redox status and signal transduction.


Input: Salsolinol induced apoptotic changes in neural stem cells: amelioration by neurotrophin support.

Salsolinol


Input: Salsolinol (SAL), a catechol isoquinoline has invited considerable attention due to its structural similarity with dopaminergic neurotoxin 1-methyl-4-phenyl-1, 2, 3, 6-tetrahydropyridine (MPTP).

Salsolinol

SAL

catechol isoquinoline

1-methyl-4-phenyl-1, 2, 3, 6-tetrahydropyridine

MPTP


Input: Its high endogenous presence in Parkinsonian brain implicated its possible association with the disease process.


Input: SAL is also present in alcohol beverages and certain food materials and can get access to brain especially in conditions of immature or impaired BBB.

SAL


Input: Besides this, the effect of SAL on neural stem cells (NSCs) which are potential candidates for adult neurogenesis and transplantation mediated rejuvenating attempts for Parkinson' s disease (PD) brain has not been known so far.

SAL


Input: NSCs in both the cases have to overcome suppressive cues of diseased brain for their survival and function.


Input: In this study we explored the toxicity of SAL toward NSCs focusing on apoptosis and status of PI3K survival signaling.

SAL


Input: NSCs cultured from embryonic day 11 rat fetal brain including those differentiated to TH (+ ve) colonies, when challenged with SAL (1-100 mu M), elicited a concentration and time dependent cell death/loss of mitochondrial viability.

SAL


Input: 10 mu M SAL on which significant mitochondrial impairment initiated was further used to study mechanism of toxicity.

SAL


Input: Morphological impairment, enhanced TUNEL positivity, cleaved caspase-3 and decreased Bcl-2: Bax suggested apoptosis.


Input: Sal toxicity coincided with reduced pAkt level and its downstream effectors: pCREB, pGSK-3 beta, Bcl-2 and neurotrophins GDNF, BDNF suggesting repressed PI3K/Akt signaling.

Sal


Input: Multiple neurotrophic factor support in the form of Olfactory Ensheathing Cell' s Conditioned Media (OEC CM) potentially protected NSCs against SAL through activating PI3K/Akt pathway.

SAL


Input: This was confirmed on adding LY294002 the PI3K inhibitor which abolished the protection.


Input: We inferred that SAL exerts substantial toxicity toward NSCs.

SAL


Input: These findings will lead to better understanding of endogenous threats that might affect the fate of transplanted NSCs and their probable antidotes.


Input: Assessment of an automated in vitro basal cytotoxicity test system based on metabolically-competent cells.


Input: When in vitro test systems are evaluated for assessment of the toxicity of chemical compounds, particular efforts are made to mimic the in vivo reality as close as possible.


Input: Cellular models with appropriate metabolic competence, i. e. with the potency to biotransform chemical compounds, are considered crucial since some metabolites have a different toxicity than their parent compounds.


Input: In this study a cell based in vitro test system is proposed to investigate the basal cytotoxicity of several reference chemicals.


Input: Both metabolic competent HepaRG cells and cells with no or low hepatic enzyme activity (undifferentiated HepaRG and proliferating HepG2) were used.


Input: The classic Neutral Red Uptake (NRU) assay proved to be robust and reliable to be applied as viability assay.

Neutral Red


Input: The test was performed on a robotic platform, which enabled fully automated and simultaneous screening of the compounds.


Input: The outcome of these tests grouped the tested compounds in three categories following their detoxification effect (benzo (a) pyrene, valproic acid), their bio-activation effect (aflatoxin B1) and their specific effect on inhibition of cell proliferation (cycloheximide, sodium lauryl sulphate, atropine sulphate monohydrate, acetylsalicylic acid).

benzo (a) pyrene

valproic acid

aflatoxin B1

cycloheximide

sodium lauryl sulphate

atropine sulphate monohydrate

acetylsalicylic acid


Input: Data management in large-scale collaborative toxicity studies: How to file experimental data for automated statistical analysis.


Input: High-throughput screening approaches are carried out for the toxicity assessment of a large number of chemical compounds.


Input: In such large-scale in vitro toxicity studies several hundred or thousand concentration-response experiments are conducted.


Input: The automated evaluation of concentration-response data using statistical analysis scripts saves time and yields more consistent results in comparison to data analysis performed by the use of menu-driven statistical software.


Input: Automated statistical analysis requires that concentration-response data are available in a standardised data format across all compounds.


Input: To obtain consistent data formats, a standardised data management workflow must be established, including guidelines for data storage, data handling and data extraction.


Input: In this paper two procedures for data management within large-scale toxicological projects are proposed.


Input: Both procedures are based on Microsoft Excel files as the researcher' s primary data format and use a computer programme to automate the handling of data files.


Input: The first procedure assumes that data collection has not yet started whereas the second procedure can be used when data files already exist.


Input: Successful implementation of the two approaches into the European project ACuteTox is illustrated.


Input: Thirteen week rodent feeding study with grain from molecular stacked trait lepidopteran and coleopteran protected (DP-O O 4114-3) maize.


Input: The results from a subchronic feeding study conducted in Sprague-Dawley rats fed with diets containing grain from 4114 (OECD unique identifier: DP-O O 4114-3) maize that was untreated (4114) or sprayed in field with glufosinate ammonium (4114GLU) in a design similar to previous studies are reported.

glufosinate ammonium


Input: The test material, 4114 maize, is a hybrid maize produced by transformation with a DNA construct encoding 4 different transgenic proteins for resistance to lepidopteran pests, coleopteran pests, and tolerance to the herbicidal active ingredient glufosinate ammonium.

glufosinate ammonium


Input: There were a total of 144 rats divided into 12 groups of 12 rats/sex/group.


Input: All experimental diets were formulated by Purina Mills, LLC (St. Louis, MO) in accordance with the standards of Purina Mills Labdiet (R) Certified Rodent LabDiet (R) 5002.


Input: The incorporation rate of maize grain in all diets was 32% (wt/wt).


Input: No biologically significant, treatment related differences in body weight, food consumption, clinical pathology parameters (hematology, blood chemistry, urinalysis, or organ weight) were observed in rats consuming the diets containing 4114 maize grain compared with rats fed conventional maize diets.


Input: A number of histologic observations were noted in this study but were background lesions and representative of what would be expected for rats of this age and strain.


Input: An independent panel of experts determined certain observations to be spontaneous and not related to the test diet.


Input: Accordingly, these results support the conclusion that 4114 maize grain is as safe and nutritious as conventional maize grain.


Input: Olive oil oleuropein has anti-breast cancer properties with higher efficiency on ER-negative cells.

oleuropein


Input: Breast cancer constitutes a major health problem for women worldwide.


Input: However, its incidence varies between populations and geographical locations.


Input: These variations could be diet-related, since there are several carcinogenic compounds in the modern diet, while natural products contain various anti-cancer elements.


Input: Several lines of evidence indicate that, in addition to their clear preventive effect, these compounds could also be used as therapeutic agents.


Input: In the present report we have shown that oleuropein, a pharmacologically safe natural product of olive leaf, has potent anti-breast cancer properties.

oleuropein


Input: Indeed, oleuropein exhibits specific cytotoxicity against breast cancer cells, with higher effect on the basal-like MDA-MB-231 cells than on the luminal MCF-7 cells.

oleuropein


Input: This effect is mediated through the induction of apoptosis via the mitochondrial pathway.


Input: Moreover, oleuropein inhibits cell proliferation by delaying the cell cycle at S phase and up-regulated the cyclin-dependent inhibitor p21.

oleuropein


Input: Furthermore, oleuropein inhibited the anti-apoptosis and pro-proliferation protein NF-kappa B and its main oncogenic target cyclin D1.

oleuropein


Input: This inhibition could explain the great effect of oleuropein on cell proliferation and cell death of breast cancer cells.

oleuropein


Input: Therefore, oleuropein warrants further investigations to prove its utility in preventing/treating breast cancer, especially the less-responsive basal-like type.

oleuropein


Input: Monotropein isolated from the roots of Morinda officinalis ameliorates proinflammatory mediators in RAW 264. 7 macrophages and dextran sulfate sodium (DSS)-induced colitis via NF-kappa B inactivation.

Monotropein

sodium


Input: We previously demonstrated that monotropein isolated from the roots of Morinda officinalis (Rubiaceae) has anti-inflammatory effects in vivo.

monotropein


Input: In the present study, we investigated the molecular mechanisms underlying the anti-inflammatory effects of monotropein in lipopolysaccharide (LPS)-induced RAW 264. 7 macrophages and dextran sulfate sodium (DSS)-induced colitis mouse model.

monotropein

sodium


Input: Monotropein was found to inhibit the expressions of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), tumor necrosis factor-alpha (TNF-alpha), and interleukin-1 beta (IL-1 beta) mRNA in LPS-induced RAW 264. 7 macrophages.

Monotropein

nitric oxide


Input: Treatment with monotropein decreased the DNA binding activity of nuclear factor-kappa B (NF-kappa B).

monotropein


Input: Consistent with these findings, monotropein also suppressed phosphorylation and degradation of inhibitory kappa B-alpha (I kappa B-alpha), and consequently the translocations of NF-kappa B.

monotropein


Input: In the DSS-induced colitis model, monotropein reduced disease activity index (DAI), myeloperoxidase (MPO) activity, and inflammation-related protein expressions by suppressing NF-kappa B activation in colon mucosa.

monotropein


Input: Taken together, these findings suggest that the anti-inflammatory effects of monotropein are mainly related to the inhibition of the expressions of inflammatory mediators via NF-kappa B inactivation, and support its possible therapeutic role in colitis.

monotropein


Input: Increased urinary excretion of albumin, hemopexin, transferrin and VDBP correlates with chronic sensitization to gentamicin nephrotoxicity in rats.

gentamicin


Input: Drug nephrotoxicity is a serious health and economic problem worldwide.


Input: Rats can be acutely sensitized to acute kidney injury (AKI) by subnephrotoxic treatments with potentially nephrotoxic drugs.


Input: Acquired sensitization to AKI poses a silent risk impossible to diagnose pre-emptively with the technology available at the clinical level.


Input: Herein, we hypothesized whether a chronic, subnephrotoxic insult to the kidneys might result in chronically acquired sensitization to AKI, and whether chronic sensitization might be detected through specific urinary markers.


Input: To this end, rats were treated with a subtoxic dosage of the experimental nephrotoxin uranyl nitrate (UN) in the drinking water for 21 weeks, or plain water (as control), and then with low-dose gentamicin for 7 days.

nitrate

gentamicin


Input: Renal function and renal tissue damage were evaluated through the experiment.


Input: The mild renal damage caused by gentamicin was markedly magnified in rats having received UN chronically, which was evident both at the functional and histological level.

gentamicin


Input: Four proteins, namely albumin, hemopexin, transferrin and vitamin D binding protein were increased in the urine in temporal association with the appearance of chronic predisposition.

vitamin D


Input: Although further studies are necessary, our results suggest that these proteins might be potentially used as markers of hidden, chronic predisposition to gentamicin nephrotoxicity, in order to appropriately and pre-emptively stratify and handle individuals according to their specific risk in the long term, and to conveniently optimize their life conditions or additional clinical procedures or treatments that might trigger the disease.

gentamicin


Input: This might reduce AKI incidence and severity and the associated costs.


Input: Chemokine expression is upregulated in chondrocytes in diabetic fracture healing.


Input: Chemokines are thought to play an important role in several aspects of bone metabolism including the recruitment of leukocytes and the formation of osteoclasts.


Input: We investigated the impact of diabetes on chemokine expression in normal and diabetic fracture healing.


Input: Fracture of the femur was performed in streptozotocin-induced diabetic and matched normoglycemic control mice.

streptozotocin


Input: Microarray analysis was carried out and chemokine mRNA levels in vivo were assessed.


Input: CCL4 were examined in fracture calluses by immunohistochemistry and the role of TNF in diabetes-enhanced expression was investigated by treatment of animals with the TNF-specific inhibitor, pegsunercept.


Input: In vitro studies were conducted with ATDC5 chondrocytes.


Input: Diabetes significantly upregulated mRNA levels of several chemokines in vivo including CCL4, CCL8, CCL6, CCL11, CCL20, CCL24, CXCL2, CXCL5 and chemokine receptors CCR5 and CXCR4.


Input: Chondrocytes were identified as a significant source of CCL4 and its expression in diabetic fractures was dependent on TNF (P < 0. 05).


Input: TNF-alpha significantly increased mRNA levels of several chemokines in vitro which were knocked down with FOXO1 siRNA (P < 0. 05).


Input: CCL4 expression at the mRNA and proteins levels was induced by FOXO1 over-expression and reduced by FOXO1 knockdown.


Input: The current studies point to the importance of TNF-alpha as a mechanism for diabetes enhanced chemokine expression by chondrocytes, which may contribute to the accelerated loss of cartilage observed in diabetic fracture healing.


Input: Moreover, in vitro results point to FOXO1 as a potentially important transcription factor in mediating this effect.


Input: Synthesis, crystal structure and antidiabetic activity of substituted (E)-3-(Benzo [d] thiazol-2-ylamino) phenylprop-2-en-1-one.

(E)-3-(Benzo [d] thiazol-2-ylamino) phenylprop-2-en-1-one


Input: A novel series of substituted (E)-3-(Benzo [d] thiazol-2-ylamino) phenylprop-2-en-1-onewere synthesized starting from 2-aminobenzothiazole and 1-aryl-3, 3-bis-(methylsulfanyl)-2-propen-1-onesin the presence of a catalytic amount of sodium hydride in THF.

(E)-3-(Benzo [d] thiazol-2-ylamino) phenylprop-2-en-1-onewere

1-aryl-3, 3-bis-(methylsulfanyl)-2-propen-1-onesin

sodium hydride

THF


Input: The synthesised compounds' structures were confirmed by IR, Mass spectrometry, (1) H NMR, (13) C NMR and HRMS spectral data.

(1) H

(13) C


Input: These compounds were evaluated for their antidiabetic activity, and most of the derivatives of (E)-3-(Benzo [d] thiazol-2-ylamino) phenylprop-2-en-1-one displayed significant antidiabetic activity.

(E)-3-(Benzo [d] thiazol-2-ylamino) phenylprop-2-en-1-one


Input: Water soluble polymer films for intravascular drug delivery of antithrombotic biomolecules.


Input: Over the past 10years, the number of percutaneous coronary intervention (PCI) procedures performed in the United States has increased by 33%; however, restenosis, which inhibits complete functional recovery of the vessel wall, remains a complication of this procedure.


Input: To traverse the complications associated with PCI, the investigation of therapeutic delivery has become an integral topic in modern research.


Input: One such therapeutic, a mimic of the proteoglycan decorin, termed DS-SILY, can mask exposed collagen and thereby effectively decrease platelet activation, has recently been developed by our lab.


Input: Drawing inspiration from coating technologies developed by the pharmaceutical industry, a fast-dissolving polymer film has been developed to deliver active therapeutic agents from a balloon catheter during PCI.


Input: This research investigates the release of DS-SILY from fast-dissolving polymer films composed of poly (vinyl alcohol) (PVA) and poly (ethylene glycol) (PEG).

poly (vinyl alcohol)

PVA

poly (ethylene glycol)

PEG


Input: Thin, uniform polymer films were produced via spin coating technique.


Input: The dissolution speed of the polymer films was found to be dependent on the concentration of polymer solution, where at least 65% of the films were shown to dissolve into nanometer sized polymer fragments within 2min.


Input: DS-SILY, up to 6. 26 mu g/cm (2), was loaded into the films and functional release of the mimic was demonstrated by its successful binding to collagen upon release.


Input: Furthermore, DS-SILY released from films resulted in increased platelet inhibition.


Input: These results indicate that use of fast-dissolving polymer films allow for the successful release of biomolecules and further investigation of their use for localized drug delivery during PCI procedures is warranted.


Input: Sequential delivery of TAT-HSP27 and VEGF using microsphere/hydrogel hybrid systems for therapeutic angiogenesis.


Input: Ischemic disease is associated with high mortality and morbidity rates, and therapeutic angiogenesis via systemic or local delivery of protein drugs is one potential approach to treat the disease.


Input: In this study, we hypothesized that combined delivery of TAT-HSP27 (HSP27 fused with transcriptional activator) and VEGF could enhance the therapeutic efficacy in an ischemic mouse model, and that sequential release could be critical in therapeutic angiogenesis.


Input: Alginate hydrogels containing TAT-HSP27 as an anti-apoptotic agent were prepared, and porous PLGA microspheres loaded with VEGF as an angiogenic agent were incorporated into the hydrogels to prepare microsphere/hydrogel hybrid delivery systems.


Input: Sequential in vitro release of TAT-HSP27 and VEGF was achieved by the hybrid systems.


Input: TAT-HSP27 was depleted from alginate gels in 7 days, while VEGF was continually released for 28 days.


Input: The release rate of VEGF was attenuated by varying the porous structures of PLGA microspheres.


Input: Sequential delivery of TAT-HSP27 and VEGF was critical to protect against muscle degeneration and fibrosis, as well as to promote new blood vessel formation in the ischemic site of a mouse model.


Input: This approach to controlling the sequential release behaviors of multiple drugs could be useful in the design of novel drug delivery systems for therapeutic angiogenesis.


Input: Synthesis and evaluation of a backbone biodegradable multiblock HPMA copolymer nanocarrier for the systemic delivery of paclitaxel.

HPMA

paclitaxel


Input: The performance and safety of current antineoplastic agents, particularly water-insoluble drugs, are still far from satisfactory.


Input: For example, the currently widely used Cremophor EL (R)-based paclitaxel (PTX) formulation exhibits pharmacokinetic concerns and severe side effects.

paclitaxel

PTX


Input: Thus, the concept of a biodegradable polymeric drug-delivery system, which can significantly improve therapeutic efficacy and reduce side effects is advocated.


Input: The present work aims to develop a new-generation of long-circulating, biodegradable carriers for effective delivery of PTX.

PTX


Input: First, a multiblock backbone biodegradable N-(2-hydroxypropyl) methacrylamide (HPMA) copolymer-PTX conjugate (mP-PTX) with molecular weight (Mw) of 335 kDa was synthesized by RAFT (reversible addition-fragmentation chain transfer) copolymerization, followed by chain extension.

N-(2-hydroxypropyl) methacrylamide

HPMA

PTX

PTX


Input: In vitro studies on human ovarian carcinoma A2780 cells were carried out to investigate the cytotoxicity of free PTX, HPMA copolymer-PTX conjugate with Mw of 48 kDa (P-PTX), and mP-PTX.

PTX

HPMA

PTX

PTX

PTX


Input: The experiments demonstrated that mP-PTX has a similar cytotoxic effect against A2780 cells as free PTX and P-PTX.

PTX

PTX

PTX


Input: To further compare the behavior of this new biodegradable conjugate (mP-PTX) with free PTX and P-PTX in vivo evaluation was performed using female nu/nu mice bearing orthotopic A2780 ovarian tumors.

PTX

PTX

PTX


Input: Pharmacokinetics study showed that high Mw mP-PTX was cleared more slowly from the blood than commercial PTX formulation and low Mw P-PTX.

PTX

PTX

PTX


Input: SPECT/CT imaging and biodistribution studies demonstrated biodegradability as well as elimination of mP-PTX from the body.

PTX


Input: The tumors in the mP-PTX treated group grew more slowly than those treated with saline, free PTX, and P-PTX (single dose at 20 mg PTX/kg equivalent).

PTX

PTX

PTX

PTX


Input: Moreover, mice treated with mP-PTX had no obvious ascites and body-weight loss.

PTX


Input: Histological analysis indicated that mP-PTX had no toxicity in liver and spleen, but induced massive cell death in the tumor.

PTX


Input: In summary, this biodegradable drug delivery system has a great potential to improve performance and safety of current antineoplastic agents.


Input: C (22)-steroidal lactone glycosides from stems and leaves of Paris polyphylla var. yunnanensis.

C (22)-steroidal lactone glycosides


Input: Further phytochemical investigation on the stems and leaves of Paris polyphylla var. yunnanensis has led to the isolation of three C (22)-steroidal lactone glycosides.

C (22)-steroidal lactone glycosides


Input: Two of these are new compounds, designated as chonglouoside SL-7 (1) and chonglouoside SL-8 (2).

chonglouoside SL-7

chonglouoside SL-8


Input: Their structures were elucidated on the basis of extensive spectroscopic analysis, as well as comparison with the reported spectroscopic data.


Input: This is the first report of C (22)-steroidal lactone glycosides isolated from the Paris genus.

C (22)-steroidal lactone glycosides


Input: Compounds 1 and 3 showed moderate antimicrobic activity against Propionibacterium acnes with MIC values of 31. 3 and 3. 9 mu g/mL, respectively.


Input: Caffeine-induced inhibition of the activity of glutamate transporter type 3 expressed in Xenopus oocytes.

Caffeine

glutamate


Input: Caffeine has been known to trigger seizures, however, the precise mechanism about the proconvulsive effect of caffeine remains unclear.

Caffeine

caffeine


Input: Glutamate transporters play an important role to maintain the homeostasis of glutamate concentration in the brain tissue.

Glutamate

glutamate


Input: Especially, dysfunction of excitatory amino acid transporter type 3 (EAAT3) can lead to seizures.

amino acid


Input: We investigated the effects of caffeine on the activity of EAAT3 and the involvement of protein kinase C (PKC) and phosphatidylinositol 3-kinase (PI3K).

caffeine


Input: Rat EAAT3 was expressed in Xenopus oocytes by injecting EAAT3 mRNA.


Input: l-Glutamate (30 mu M)-induced inward currents were recorded via the two-electrode voltage clamp method.

l-Glutamate


Input: Caffeine decreased EAAT3 activity in a dose-dependent manner.

Caffeine


Input: Caffeine (30 mu M for 3min) significantly reduced V (max), but did not alter K (m) value of EAAT3 for glutamate.

Caffeine

glutamate


Input: When preincubated oocytes with phorbol-12-myristate-13-acetate (PMA, a PKC activator) were exposed to caffeine, PMA-induced increase in EAAT3 activity was abolished.

PMA

caffeine

PMA


Input: Two PKC inhibitors (chelerythrine and staurosporine) significantly reduced basal EAAT3 activity.

chelerythrine

staurosporine


Input: Whereas, there were no significant differences among the PKC inhibitors, caffeine, and PKC inhibitors + caffeine groups.

caffeine

caffeine


Input: In similarly fashion, wortmannin (a PI3K inhibitor) significantly decreased EAAT3 activity, however no statistical differences were observed among the wortmannin, caffeine, and wortmannin + caffeine groups.

wortmannin

wortmannin

caffeine

wortmannin

caffeine


Input: Our results demonstrate that caffeine attenuates EAAT3 activity and this reducing effect of caffeine seems to be mediated by PKC and PI3K.

caffeine

caffeine


Input: The electroreduction of benzoic acid: voltammetric observation of adsorbed hydrogen at a platinum microelectrode in room temperature ionic liquids.

benzoic acid

hydrogen

platinum


Input: The electrochemical reduction of benzoic acid in the presence and absence of hydrogen (H (2)) has been investigated using a 10 mu m diameter platinum microelectrode in four different room temperature ionic liquids (RTILs), namely [C (4) mim] [NTf (2)], [C (4) mpyrr] [NTf (2)], [C (4) mim] [OTf] and [C (4) mim] [BF (4)], versus Ag/Ag (+).

benzoic acid

hydrogen

H (2)

platinum

[C (4) mim] [NTf (2)]

[C (4) mpyrr] [NTf (2)]

[C (4) mim] [OTf]

[C (4) mim] [BF (4)]

Ag

Ag (+)


Input: In all cases, reductive voltammetry is observed, and is suggested to occur via a CE mechanism in which dissociation of benzoic acid is followed by electron transfer to H (+) ultimately forming adsorbed hydrogen.

benzoic acid

H (+)

hydrogen


Input: Furthermore, the adsorbed H atoms, formed from the reduction of benzoic acid, could be used to achieve the rapid hydrogenolysis of the organic compound (bis (benzyloxycarbonyl)-l-lysine) on the timescale of the voltammetric technique under moderate conditions (25 degrees C).

H

benzoic acid

bis (benzyloxycarbonyl)-l-lysine


Input: Rational design of the survivin/CDK4 complex by combining protein-protein docking and molecular dynamics simulations.


Input: Survivin, the smallest inhibitor of apoptosis protein (IAP), is a valid target for cancer research.


Input: It mediates both the apoptosis pathway and the cell cycle and has been proposed to form a complex with the cyclin-dependent kinase protein CDK4.


Input: The resulting complex transports CDK4 from the cytosol to the nucleus, where CDK4 participates in cell division.


Input: Survivin has been recognized as a node protein that interacts with several partners; disruption of the formed complexes can lead to new anticancer compounds.


Input: We propose a rational model of the survivin/CDK4 complex that fulfills the experimental evidence and that can be used for structure-based design of inhibitors modifying its interface recognition.


Input: In particular, the suggested complex involves the alpha helical domain of survivin and resembles the mode of binding of survivin in the survivin/borealin X-ray structure.


Input: The proposed model has been obtained by combining protein-protein docking, fractal-based shape complementarity, electrostatics studies and extensive molecular dynamics simulations.


Input: Probing the structural, electronic and magnetic properties of multicenter Fe 2 S 2 0/-, Fe 3 S 4 0/-and Fe 4 S 4 0/-clusters.

Fe 2 S 2

Fe 3 S 4

Fe 4 S 4


Input: The structural, electronic and magnetic properties of neutral and anion Fe2S2, Fe3S4 and Fe4S4 have been investigated with the aid of previous photoelectron spectroscopy and density functional theory calculations.


Input: Theoretical electron detachment energies (both vertical and adiabatic) of anion clusters for the lowest energy structure were computed and compared with the experimental results to verify the ground states.


Input: The optimized structures show that the ground state structures of Fe2S2 (0/-), Fe3S4 (0/-) and Fe4S4 (0/-) favor high spin state and are similar to their structures in proteins.


Input: The electron delocalization pattern for all the clusters and the nature of bonding between Fe and S atoms were studied by analyzing molecular orbitals.

Fe

S


Input: Natural population analysis demonstrates that Fe atoms act as an electron donor in all clusters, and the electron density difference map clearly shows the direction of the electron flow over the whole complex.

Fe


Input: Furthermore, the investigated magnetism shows that the Fe atoms carried most of the magnetic moments, which is due mainly to the 3d state, while only very small magnetic moments are found on S atoms.

Fe

S


Input: Methylation-controlled J-protein MCJ acts in the import of proteins into human mitochondria.


Input: Loss of expression of the methylation-controlled J gene, MCJ (DNAJC15), is observed in cases of several tumors and plays a crucial role in the chemoresistance of ovarian cancer cells.


Input: Aside from the pathophysiological effects, almost nothing is known about the cellular function of MCJ.


Input: Here, we provide the first evidence that MCJ acts in the biogenesis of mitochondria.


Input: Our results demonstrate that MCJ is located in mitochondria.


Input: It is anchored in the mitochondrial inner membrane with the C-terminal J domain facing the matrix space.

C


Input: We show that MCJ forms a stable subcomplex with a component of the mitochondrial import motor, MAGMAS, a protein overexpressed in cells treated with granulocyte-macrophage colony-stimulating factor and in prostate carcinomas.


Input: In addition, MCJ and MAGMAS interact with the core components of the TIM23 pre-protein translocase.


Input: We demonstrate that the recombinant soluble MCJ domain stimulates the ATPase activity of the human mtHsp70 chaperone, mortalin, the central component of the import motor of the TIM23 translocase.


Input: This stimulation is counteracted by MAGMAS.


Input: Moreover, pre-protein import into mitochondria is impaired in the absence of MCJ.


Input: Interestingly, MCJ is able to take over the function of Tim14, the essential J co-chaperone of the mitochondrial protein import motor in yeast.


Input: In summary, our results show that MCJ functions as J co-chaperone of the human TIM23 pre-protein translocase, suggesting a link between mitochondrial pre-protein import and tumorigenesis.


Input: The yeast eukaryotic translation initiation factor 2B translation initiation complex interacts with the fatty acid synthesis enzyme YBR159W and endoplasmic reticulum membranes.

fatty acid


Input: Using affinity purifications coupled with mass spectrometry and yeast two-hybrid assays, we show the Saccharomyces cerevisiae translation initiation factor complex eukaryotic translation initiation factor 2B (eIF2B) and the very-long-chain fatty acid (VLCFA) synthesis keto-reductase enzyme YBR159W physically interact.

fatty acid


Input: The data show that the interaction is specifically between YBR159W and eIF2B and not between other members of the translation initiation or VLCFA pathways.


Input: A ybr159w Delta null strain has a slow-growth phenotype and a reduced translation rate but a normal GCN4 response to amino acid starvation.

amino acid


Input: Although YBR159W localizes to the endoplasmic reticulum membrane, subcellular fractionation experiments show that a fraction of eIF2B cofractionates with lipid membranes in a YBR159W-independent manner.


Input: We show that a ybr159w Delta yeast strain and other strains with null mutations in the VLCFA pathway cause eIF2B to appear as numerous foci throughout the cytoplasm.


Input: The response of soil organism communities to the application of the insecticide lindane in terrestrial model ecosystems.

lindane


Input: The EU plant protection regulation 1107/2009/EC defines the requirements for active ingredients to be approved, specifically including the assessment of effects on biodiversity and ecosystems.


Input: According to that, semi-field methods are expected to be more important in the near future.


Input: Therefore, a higher-tier experiment suitable to assess the risk for soil organisms was conducted to further develop the TME (terrestrial model ecosystems) methodology in a dose-response design with the persistent insecticidal model compound lindane (gamma-HCH).

lindane

gamma-HCH


Input: The effects of lindane on soil communities such as collembolans, oribatid mites, nematodes, soil fungi and plant biomass were determined in 42 TME.

lindane


Input: Intact TME-soil cores (diameter 300 mm, height 400 mm) from undisturbed grassland were stored outdoor under natural climatic conditions.


Input: Lindane was applied in five concentrations between 0. 032 mg active ingredients (ai)/kg dry soil and 3. 2 mg ai/kg dry weight soil, six-fold replicated each.

Lindane


Input: Twelve TME served as untreated controls.


Input: Abundance and community structures of oribatids, collembolans, enchytraeids, nematodes and fungi were recorded.


Input: Oribatid mites' community responded 3 months after treatment, although they were not significantly affected by the overall treatment regimen.


Input: Collembolans in total and species-specific abundance as well as the community endpoints (principal response curves, diversity measures) were adversely affected by moderate dosages of lindane.


Input: Effects were transient between 3 and 5 months after treatment with a recovery within 1 year.


Input: No significant effects could be detected for enchytraeids, nematodes and fungi.


Input: The study design and the obtained results allow for calculations of no observed effect concentrations below the highest treatment level for populations and for soil communities as defined entities, as well as effective concentrations.


Input: The paper discusses the limits of effect detection in the light of achievable coefficients of variation and by means of minimum detectable differences.


Input: Outdoor TME are useful to analyze and assess functional and structural endpoints in soil organisms' communities and their possible recovery after pesticide treatment within 1 year.


Input: Significance of peptide transporter 1 in the intestinal permeability of valacyclovir in wild-type and PepT1 knockout mice.

valacyclovir


Input: The purpose of this study was to quantitatively determine the contribution of PepT1 [peptide transporter 1 (SLC15A1)] to the intestinal permeability of valacyclovir, an ester prodrug of the antiviral drug acyclovir.

valacyclovir

acyclovir


Input: In situ single-pass intestinal perfusions were employed (pH 6. 5 x 90 minutes) to assess the effective permeability (P (eff)) of 100 mu M [(3) H] valacyclovir in wild-type and PepT1 knockout mice.

[(3) H] valacyclovir


Input: Acyclovir pharmacokinetics was also evaluated after oral administration of 25 nmol/g valacyclovir.

Acyclovir

valacyclovir


Input: In wild-type mice, jejunal uptake of valacyclovir was best described by both saturable (K (m) = 10. 2 mM) and nonsaturable components where the saturable pathway accounted for 82% of total transport.

valacyclovir


Input: Valacyclovir P (eff) was 2. 4 x 10 (-4) cm/s in duodenum, 1. 7 x 10 (-4) cm/s in jejunum, 2. 1 x 10 (-4) cm/s in ileum, and 0. 27 x 10 (-4) cm/s in colon.

Valacyclovir


Input: In Pept1 knockout mice, P (eff) values were about 10% of that in wild-type animals for these small intestinal segments.


Input: Valacyclovir P (eff) was similar in the colon of both genotypes.

Valacyclovir


Input: There were no differences in valacyclovir P (eff) between any of the intestinal segments of PepT1 knockout mice.

valacyclovir


Input: Valacyclovir P (eff) was significantly reduced by the dipeptide glycylsarcosine and the aminocephalosporin cefadroxil, but not by the amino acids l-valine or l-histidine, the organic acid p-aminohippurate, or the organic base tetraethylammonium (all at 25 mM).

Valacyclovir

glycylsarcosine

aminocephalosporin cefadroxil

amino acids l-valine

l-histidine

p-aminohippurate

tetraethylammonium


Input: PepT1 ablation resulted in 3-to 5-fold reductions in the in vivo rate and extent of valacyclovir absorption.

valacyclovir


Input: Our findings conclusively demonstrate, using in situ and in vivo validations in genetically modified mice, that PepT1 has a major influence in improving the oral absorption of valacyclovir.

valacyclovir


Input: Mammalian frataxin controls sulfur production and iron entry during de novo Fe4S4 cluster assembly.

sulfur

iron


Input: Iron-sulfur (Fe-S) cluster-containing proteins are essential components of cells.

Iron-sulfur

Fe-S


Input: In eukaryotes, Fe-S clusters are synthesized by the mitochondrial iron-sulfur cluster (ISC) machinery and the cytosolic iron-sulfur assembly (CIA) system.

Fe-S

iron-sulfur

iron-sulfur


Input: In the mammalian ISC machinery, preassembly of the Fe-S cluster on the scaffold protein (ISCU) involves a cysteine desulfurase complex (NFS1/ISD11) and frataxin (FXN), the protein deficient in Friedreich' s ataxia.

Fe-S

cysteine


Input: Here, by comparing the biochemical and spectroscopic properties of quaternary (ISCU/NFS1/ISD11/FXN) and ternary (ISCU/NFS1/ISD11) complexes, we show that FXN stabilizes the quaternary complex and controls iron entry to the complex through activation of cysteine desulfurization.

iron

cysteine


Input: Furthermore, we show for the first time that in the presence of iron and L-cysteine, an [Fe (4) S (4)] cluster is formed within the quaternary complex that can be transferred to mammalian aconitase (mACO2) to generate an active enzyme.

iron

L-cysteine

Fe (4) S (4)


Input: In the absence of FXN, although the ternary complex can assemble an Fe-S cluster, the cluster is inefficiently transferred to ACO2.

Fe-S


Input: Taken together, these data help to unravel further the Fe-S cluster assembly process and the molecular basis of Friedreich' s ataxia.

Fe-S


Input: Dynamic behavior of water droplet impact on microtextured surfaces: the effect of geometrical parameters on anisotropic wetting and the maximum spreading diameter.


Input: Textured silicon surfaces decorated by square arrays of pillars with adjustable pitch were fabricated.

silicon


Input: The wetting behavior, especially for direction-dependent water contact angles on textured silicon surfaces after silanization, was investigated by incorporating the contact line fraction into a modified Wenzel model.

silicon


Input: Also, the effect of geometrical parameters on the anisotropic wetting behavior of water was examined with respect to water droplet impact on the textured surface.


Input: Moreover, the maximum spreading factor was studied theoretically in terms of energy conservation, allowing for surface topography and viscous friction of the liquid flowing among the arrays of the posts.


Input: Theoretical models were found to be in good agreement with experimental data.


Input: Mineral and sensory profile of seasoned cracked olives packed in diverse salt mixtures.


Input: This work studies the effect of packing cracked seasoned olives with NaCl, KCl, and CaCl (2) mixture brines on their mineral nutrients and sensory attributes, using RSM methodology.

NaCl

KCl

CaCl (2)


Input: The Na, K, Ca, and residual natural Mn contents in flesh as well as saltiness, bitterness and fibrousness were significantly related to the initial concentrations of salts in the packing solution.

K

Ca

Mn


Input: This new process led to table olives with a significantly lower sodium content (about 31%) than the traditional product but fortified in K and Ca.

sodium

K

Ca


Input: High levels of Na and Ca in the flesh led to high scores of acidity and saltiness (the first descriptor) and bitterness (the second) while the K content was unrelated to any sensory descriptor.

Ca

K


Input: The new presentations using moderate proportions of alternative salts will therefore have improved nutritional value and healthier characteristics but only a slightly modified sensory profile.


Input: Direct potentiometric determination of starch using a platinum redox sensor.

platinum


Input: Here, we describe the development of a platinum redox sensor for the direct potentiometric quantification of starch in solution.

platinum


Input: The sensor measures the decrease in free triiodide ion after it complexes with starch to form a starch-triiodide complex.

triiodide

triiodide


Input: This decrease was, therefore, correlated with starch concentration, and the composition and stability of the potassium triiodide solution were optimised.

potassium triiodide


Input: The starch-triiodide complex was characterized potentiometrically at variable starch and triiodide concentrations.

triiodide

triiodide


Input: We also propose a response mechanism for the platinum redox sensor towards starch and an appropriate theoretical model.

platinum


Input: The optimised method exhibited satisfactory accuracy and precision and was in good agreement with a standard spectrophotometric method.


Input: The sensor was tested over a range of 0. 4-9 mg starch, with recoveries ranging from 97. 8% to 103. 4% and a detection limit of 0. 01 mg starch.


Input: Rapid detection and quantification of milk adulteration using infrared microspectroscopy and chemometrics analysis.


Input: The application of attenuated total reflectance mid-infrared microspectroscopy (MIR-microspectroscopy) was evaluated as a rapid method for detection and quantification of milk adulteration.


Input: Milk samples were purchased from local grocery stores (Columbus, OH, USA) and spiked at different concentrations of whey, hydrogen peroxide, synthetic urine, urea and synthetic milk.

hydrogen peroxide

urea


Input: Samples were place on a 192-well microarray slide, air-dried and spectra were collected by using MIR-microspectroscopy.


Input: Pattern recognition analysis by Soft Independent Modeling of Class Analogy (SIMCA) showed tight and well-separated clusters allowing discrimination of control samples from adulterated milk.


Input: Partial Least Squares Regression (PLSR) showed standard error of prediction (SEP) ~ 2. 33, 0. 06, 0. 41, 0. 30 and 0. 014 g/L for estimation of levels of adulteration with whey, synthetic milk, synthetic urine, urea and hydrogen peroxide, respectively.

urea

hydrogen peroxide


Input: Results showed that MIR-microspectroscopy can provide an alternative methodology to the dairy industry for screening potential fraudulent practice for economic adulteration of cow' s milk.


Input: Cashew apple (Anacardium occidentale L.) extract from by-product of juice processing: a focus on carotenoids.


Input: Cashew apple fibrous residue is a by-product of the cashew juice industry.


Input: After pressing using a helical type continuous press followed by crossflow microfiltration, an aqueous extract was obtained from these cashew apple fibres.


Input: It was characterised by an intense yellow colour due to carotenoid pigments.


Input: Carotenoids were identified and quantified in the cashew apple before extraction, in its aqueous extract and in the concentrate obtained by microfiltration.


Input: Cashew apple aqueous extract and its concentrate presented a carotenoid profile with 11 carotenoids, most of them were tentatively identified by HPLC-DAD-MS and are xanthophylls present under an esterified form.


Input: Auroxanthin and beta-cryptoxanthin represented around 50% of total carotenoids.

beta-cryptoxanthin


Input: Concentration of the extract by microfiltration led to epoxy-furanoxy rearrangement of violaxanthin and antheraxanthin.

epoxy

furanoxy

violaxanthin

antheraxanthin


Input: The process allowed an increase of 10 times total carotenoid content compared with initial cashew apple.


Input: Total carotenoid content of the final concentrated extract reached 54 mg/kg.


Input: Inhibition effects and induction of apoptosis of flavonoids on the prostate cancer cell line PC-3 in vitro.

flavonoids


Input: Myricetin and myricitrin are naturally occurring flavonoids have been suggested to play a role in inhibition of proliferation and transformation of carcinogenic cell.

Myricetin

myricitrin

flavonoids


Input: However, the underlying molecular mechanisms of their activity have not yet to be revealed.


Input: The aim of the present study was to clarify the molecular mechanisms of apoptosis cell on the prostate cancer induced by myricetin, myricitrin, quercetin and quercitrin.

myricetin

myricitrin

quercetin

quercitrin


Input: The MTT assay confirmed that myricetin had the strongest inhibitory effect on human prostate cancer cell line PC-3, myricitrin was second, and quercitrin was the weakest.

MTT

myricetin

myricitrin

quercitrin


Input: A noticeable synergistic effect was observed with the inhibition of cell proliferation when myricetin was used in combination with myricitrin.

myricetin

myricitrin


Input: In the concentration range of 37. 5-300 mu mol/L, the inhibitory effects of these flavonoids were enhanced with increasing dose and treatment time.

flavonoids


Input: The acridine orange analysis and annexin V-FITC/PI double-staining results confirmed that myricetin and myricitrin were effective in inducing PC-3 cell apoptosis.

acridine orange

FITC

myricetin

myricitrin


Input: The results showed that myricetin was more effective than myricitrin in inducing cell apoptosis.

myricetin

myricitrin


Input: The apoptosis rate increased with increasing flavonoid concentration in a dose dependent manner.

flavonoid


Input: A synergistic effect was observed on the apoptosis rate when myricetin was used in combination with myricitrin.

myricetin

myricitrin


Input: Assessment of DFG-S19 method for the determination of common endocrine disruptor pesticides in wine samples with an estimation of the uncertainty of the analytical results.


Input: A gas chromatographic method for the determination of endocrine disruptor pesticides (Chlorpyrifos, Penconazole, Procymidone, Iprodione, Bromopropylate and Lambda-Cyhalothrin) in wine samples is described.

Chlorpyrifos

Penconazole

Procymidone

Iprodione

Bromopropylate

Lambda-Cyhalothrin


Input: A general DFG-S19 method for residual pesticide determination in all kind of food stuff was investigated to simplify and adopt for wine samples in this work.


Input: Alternative sample preparation routes were elucidated and compared according to their recovery values.


Input: Four different separation techniques were tested and the method employing florosil column after a LLE procedure was applied for wine samples with satisfactory recovery ratios (72-97%).

florosil


Input: The pesticides were extracted from the sample by cyclohexane-ethyl acetate mixture (1: 1 v/v) and cleaned up by florosil column.

cyclohexane

ethyl acetate

florosil


Input: The regression coefficients were at least 0. 99 and relative standard deviations were no higher than 16%.


Input: Detection limits were in the range of 0. 6-2. 9 ng/mL and the relative expanded measurement uncertainties were calculated in the 7-22% range.


Input: Quality of bread supplemented with mushroom mycelia.


Input: Mushroom mycelia of Antrodia camphorata, Agaricus blazei, Hericium erinaceus and Phellinus linteus were used to substitute 5% of wheat flour to make bread.


Input: Bread quality, including specific volume, colour property, equivalent umami concentration (EUC), texture profile analysis, sensory evaluation and functional components, was analysed.


Input: Mycelium-supplemented bread was smaller in loaf volume and coloured, and had lower lightness and white index values.


Input: White bread contained the lowest amounts of free umami amino acids and umami 5'-nucleotides and showed the lowest EUC value.

amino acids

nucleotides


Input: Incorporating 5% mushroom mycelia into the bread formula did not adversely affect the texture profile of the bread.


Input: However, incorporating 5% mushroom mycelia into the bread formula did lower bread' s acceptability.


Input: After baking, mycelium-supplemented bread still contained substantial amounts of gamma-aminobutyric acid and ergothioneine (0. 23-0. 86 and 0. 79-2. 10 mg/g dry matter, respectively).

gamma-aminobutyric acid

ergothioneine


Input: Overall, mushroom mycelium could be incorporated into bread to provide its beneficial health effects.


Input: Natural occurrence of deoxynivalenol in wheat from Paran a State, Brazil and estimated daily intake by wheat products.

deoxynivalenol


Input: The occurrence of deoxynivalenol (DON) was evaluated in 113 wheat samples from the northern and central/southwestern regions of Paran a State, Brazil during the 2008 and 2009 growing seasons, and this rate of occurrence was used to estimate the DON dietary exposure.

deoxynivalenol

DON

DON


Input: The DON determination was carried out by an indirect competitive enzyme-linked immunosorbent assay.

DON


Input: DON was detected in 66. 4% samples at levels ranging from 206. 3 to 4732. 3 mu g/kg (mean 1894. 9 mu g/kg).

DON


Input: The estimated daily intake (EDI) of DON through bread and pasta was evaluated in the inhabitants of Londrina City in northern Paran a State, Brazil.

DON


Input: The average intake of these inhabitants was 0. 79 mu g/kg body weight (b. w.) for bread and 0. 35 mu g/kg b. w. for pasta.


Input: The total EDI was 1. 13 mu g/kg, which is above the Provisional Tolerable Daily Maximum Intake (PTDMI) of 1 mu g/kg b. w.


Input: To our knowledge, this is the first report on natural DON occurrence in wheat and DON dietary exposure estimation from Paran a, Brazil.

DON

DON


Input: Hepatoprotective effect of 2, 3-dehydrosilybin on carbon tetrachloride-induced liver injury in rats.

2, 3-dehydrosilybin

carbon tetrachloride


Input: The aim of this study was to investigate the protective effect of 2, 3-dehydrosilybin (DHS) against carbon tetrachloride (CCl (4))-induced liver injury in rats.

2, 3-dehydrosilybin

DHS

carbon tetrachloride

CCl (4)


Input: Administration of DHS significantly attenuated the levels of serum aspartate aminotransferase, alanine aminotransferase, and liver lipid peroxidation in CCl (4)-treated rats.

DHS

aspartate

alanine

CCl (4)


Input: Moreover, we showed that DHS prevented DNA damage and decreased the protein levels of gamma-H2AX, which is a specific DNA damage marker, in CCl (4)-treated rat livers.

DHS

CCl (4)


Input: DHS also markedly increased the activity of antioxidant enzymes, such as superoxide dismutase, catalase, glutathione peroxidase, and glutathione reductase in CCl (4)-treated rat livers.

superoxide

glutathione

CCl (4)


Input: Furthermore, we found that DHS significantly inhibited the production of serum nitric oxide as well as the levels of serum IL-6, IFN-gamma, and TNF-alpha in CCl (4)-treated rats.

DHS

nitric oxide

CCl (4)


Input: Additionally, DHS significantly suppressed iNOS expression on the protein levels in CCl (4)-treated rat livers.

DHS

CCl (4)


Input: Collectively, the present study suggests that DHS protects the liver from CCl (4)-induced hepatic damage via antioxidant and anti-inflammatory mechanisms.

DHS

CCl (4)


Input: Development of a rapid and simple voltammetric method to determine total antioxidative capacity of edible oils.


Input: In this work we report on a new, rapid and simple voltammetric method to determine the total antioxidant capacity (TAC) of the edible oils.


Input: The method explores the ABTS radical (2, 2'-azinobis (3-ethylbenzothiazoline-6-sulphonic acid)) assay as a redox probe and it relays on measuring catalytic voltammetric currents.

ABTS

2, 2'-azinobis (3-ethylbenzothiazoline-6-sulphonic acid)


Input: The electrocatalysis comprises redox regeneration of the electrochemically created ABTS (+) radical either by Trolox (6-hydroxy-2, 5, 7, 8-tetramethychroman-2-carboxylic acid) or by antioxidants present in studied oils.

ABTS (+)

Trolox

6-hydroxy-2, 5, 7, 8-tetramethychroman-2-carboxylic acid


Input: The detection limit of the method is determined to be 0. 5 mg/L of Trolox equivalent, being a slightly lower than the corresponding UV-VIS spectrophotometric method.

Trolox


Input: Applying the proposed voltammetric method the total antioxidant capacity of three types of commercially available cold-pressed edible oils are determined, and the results are found to be in a very good agreement with those obtained by UV-VIS spectrophotometry.


Input: The reported voltammetric method is cheap, rapid and simple, and it can be used as a sustainable alternative to the UV-VIS methods for the determination of total antioxidant capacitance of oils and other liquid lipophilic nutrients.


Input: Potent antioxidant capacity of studied oils was also confirmed by electron paramagnetic resonance spectroscopy of superoxide anion produced by macrophages.

superoxide


Input: Effect of the genistein metabolite on leptin secretion in murine adipocytes in vitro.

genistein


Input: Soy isoflavonoids have many useful properties.

isoflavonoids


Input: However, they are metabolized in vivo, including in humans.


Input: The effect of the metabolism of soy isoflavonoids on their properties is not fully understood.

isoflavonoids


Input: We have isolated the bacterial strain SY8519, which has been shown to metabolize daidzein to O-desmethylangolensin and to produce 2-(4-hydroxyphenyl) propionic acid from genistein.

daidzein

O-desmethylangolensin

2-(4-hydroxyphenyl) propionic acid

genistein


Input: According to chiral HPLC analysis, the 2-(4-hydroxyphenyl) propionic acid obtained from the bacterium was optically active.

2-(4-hydroxyphenyl) propionic acid


Input: To determine the absolute stereochemistry of the microbial product, we prepared (S)-2-(4-hydroxyphenyl) propionic acid from (S)-2-phenylpropionic and concluded that the microbial product had an R-configuration by chiral HPLC analysis.

(S)-2-(4-hydroxyphenyl) propionic acid


Input: We also applied the metabolite to mouse adipocytes and found that 2-HPPA was less effective at reducing leptin secretion than the parent compound genistein.

genistein


Input: Our results suggested that' O-desmethylangolensin-production' attenuates the effect of soy isoflavonoids by reducing not only the activity of daidzein but also that of genistein.

O-desmethylangolensin

isoflavonoids

daidzein

genistein


Input: Simultaneous detection of flavonoids and phenolic acids in Herba Lysimachiae and Herba Desmodii Styracifolii using liquid chromatography tandem mass spectrometry.

flavonoids

phenolic acids


Input: A sensitive liquid chromatography and tandem mass spectrometry (LC-MS/MS) method was developed and validated for the simultaneous analysis of 15 flavonoids and 3 phenolic acids in Herba Lysimachiae and Herba Desmodii Styracifolii.

flavonoids

phenolic acids


Input: Separation was performed using a Diamonsil C (18) column, which was eluted with methanol (A) and 0. 1 /1000 acetic acid (B).

methanol

acetic acid


Input: The gradient condition was as follows: 0-34 min, 20-34% A; 34-38 min, 34-95% A; maintained 95% A for the next 4 min.


Input: Analytes were detected using a hybrid quadrupole linear ion trap mass spectrometer that was equipped with an electrospray ionisation source in the negative ion and multiple-reaction monitoring modes.


Input: A full validation of the method was performed, including the linearity, precision, and accuracy, as well as limits of detection and quantification.


Input: The results indicated that the developed method was simple, sensitive and reliable.


Input: Furthermore, the method was successfully applied to differentiate 16 batches of Herba Lysimachiae and 21 batches of Herba Desmodii Styracifolii.


Input: Differentiation of Sparidae species by DNA sequence analysis, PCR-SSCP and IEF of sarcoplasmic proteins.


Input: The increasing global trade of fishery and aquaculture products makes it necessary to develop methods for species identification in case of fish fillets or other highly processed seafood with external morphological characteristics (e. g. gills, fins) of the original fish being removed.


Input: Species identification methods based on DNA-or protein-analysis, like DNA sequencing of PCR products, PCR-SSCP (polymerase chain reaction-single strand conformation polymorphism), and isoelectric focusing (IEF) of water-soluble proteins of fish fillet were applied successfully to distinguish between various sparid species including Sparus aurata, Spondyliosoma cantharus, Boops boops, Acanthopagrus bifasciatus, Argyrops spinifer, Pagellus bogaraveo and Lithognathus mormyrus of the family Sparidae available on European markets.


Input: Indication of the presence of parvalbumins in light muscle of all of the studied species is presented by the location of heat-stable proteins in the anodic range of the IEF gels.


Input: Exploration of Vanilla pompona from the Peruvian Amazon as a potential source of vanilla essence: quantification of phenolics by HPLC-DAD.

phenolics


Input: This study provides the first chemical investigation of wild-harvested fruits of Vanilla pompona ssp. grandiflora (Lindl.) Soto-Arenas developed in their natural habitat in the Peruvian Amazon.


Input: Flowers were hand-pollinated and the resulting fruits were analysed at different developmental stages using an HPLC-DAD method validated for the quantification of glucovanillin and seven other compounds.

glucovanillin


Input: The method showed satisfactory linearity (r (2) > 0. 9969), precision (coefficient of variation < 2%), recoveries (70-100%), limit of detection (0. 008-0. 212 mu g/ml), and limit of quantification (0. 027-0. 707 mu g/ml).


Input: The evaluation of crude and enzyme-hydrolyzed Soxhlet-extracted samples confirmed the leading role of glucosides in fruit development.


Input: LC-ESI-MS studies corroborated the identities of four glucosides and seven aglycones, among them vanillin (5. 7/100 g), 4-hydroxybenzyl alcohol (3. 6/100 g), and anisyl alcohol (7. 1/100 g) were found in high concentrations.

vanillin

4-hydroxybenzyl alcohol

anisyl alcohol


Input: The attractive flavor/aroma profile exhibited by wild V. pompona fruits supports studies focused on the development of this species as a specialty crop.


Input: Nutritive value of masau (Ziziphus mauritiana) fruits from Zambezi Valley in Zimbabwe.


Input: Ziziphus mauritiana (masau) fruits are consumed by many people in Zimbabwe.


Input: The fruits contribute significantly to people' s diet when they are in season.


Input: The objective of this study was to determine the nutritional content of the fruits and, hence, quantify their contribution to the diet.


Input: Samples of masau were collected in two seasons (August 2006 and August 2007).


Input: Both macronutrients and micronutrients were determined using standard AOAC methods of analysis.


Input: Dry matter content ranged from 21. 1 +/- 0. 2 to 24. 1 +/- 0. 3 g 100 g (-1) of edible portion of the sweet and sour fruits, and 84. 8 +/- 0. 2 to 87. 2 +/- 0. 2 g 100 g (-1) for the dried fruit.


Input: Crude protein per 100g edible portion of dry weight ranged between 7. 9 +/- 0. 0 and 8. 7 +/- 0. 0 g, crude fat from 0. 8 +/- 0. 0 to 1. 5 +/- 0. 0 g, crude fibre from 4. 9 +/- 0. 0 to 7. 3 +/- 0. 0 g, ash between 3. 0 +/- 0. 0 and 4. 3 +/- 0. 0 g and carbohydrate between 79. 5 +/- 0. 0 and 83. 2 +/- 0. 0 g.

carbohydrate


Input: The fruits were rich in vitamin C (15. 0 +/- 0. 0-43. 8 +/- 0. 02 mg 100 g (-1)) and the energy values ranged between 1516. 0 +/- 1. 73 and 1575. 0 +/- 2. 3 kJ 100 g (-1).

vitamin C


Input: Furthermore, the fruits contained (mg 100 g (-1) of dry weight) potassium from 1865. 0 +/- 1. 3 to 2441. 0 +/- 1. 1, calcium from 160. 0 +/- 0. 3 to 254. 0 +/- 0. 1, sodium between 185. 0 +/- 0. 1 and 223. 0 +/- 0. 2, magnesium between 83. 0 +/- 0. 0 and 150. 0 +/- 0. 13 and phosphorous from 87. 0 +/- 0. 1 to 148. 0 +/- 0. 5.

potassium

calcium

sodium

magnesium

phosphorous


Input: Manganese and copper contents ranged between 0. 7 +/- 0. 03 and 1. 6 +/- 0. 03, while iron and zinc ranged between 2. 1 +/- 0. 43 and 4. 3 +/- 0. 1, and 0. 6 +/- 0. 0-0. 9 +/- 0. 0 mg 100 g (-1) of dry weight, respectively.

Manganese

copper

iron

zinc


Input: The masau fruit is therefore a good potential source of carbohydrates, proteins and micronutrients, such as calcium, potassium, sodium, phosphorous, copper, iron, Vitamin C and zinc.

carbohydrates

calcium

potassium

sodium

phosphorous

copper

iron

Vitamin C

zinc


Input: Development of sample preparation method for isoliquiritigenin, liquiritin, and glycyrrhizic acid analysis in licorice by ionic liquids-ultrasound based extraction and high-performance liquid chromatography detection.

isoliquiritigenin

liquiritin

glycyrrhizic acid


Input: An ionic liquid-based ultrasonic-assisted extraction (ILUAE) method had been used for the effective extraction of isoliquiritigenin (IQ), liquiritin (LQ) and glycyrrhizic acid (GA) from licorice.

isoliquiritigenin

liquiritin

glycyrrhizic acid


Input: The ionic liquids with different cations and anions were investigated in this work and 0. 5 M 1-butyl-3-methylimidazolium bromide solution was selected as solvent.

1-butyl-3-methylimidazolium bromide


Input: In addition, the technical parameters including soaking time, solid-liquid ratio, ultrasonic power and time were optimized.


Input: Compared with the conventional solvent extraction, the proposed approach exhibited higher efficiency, which indicated the ILUAE was an efficient, rapid and simple sample preparation technique.


Input: There was no degradation of the target analytes had been observed at the optimum conditions which was evidenced by the stability studies performed with standard of IQ, LQ and GA.


Input: The proposed method also showed high reproducibility and was environmental friendly.


Input: Comparative formation of 2-amino-1-methyl-6-phenylimidazo [4, 5-b] pyridine (PhIP) in creatinine/phenylalanine and creatinine/phenylalanine/4-oxo-2-nonenal reaction mixtures.

2-amino-1-methyl-6-phenylimidazo [4, 5-b] pyridine

PhIP

creatinine

phenylalanine

creatinine

phenylalanine


Input: The comparative formation of the heterocyclic aromatic amine 2-amino-1-methyl-6-phenylimidazo [4, 5-b] pyridine (PhIP) in both creatinine/phenylalanine (CRN/Phe) and creatinine/phenylalanine/4-oxo-2-nonenal (CRN/Phe/ON) systems was studied to analyse the ability of lipid-derived reactive carbonyls to promote PhIP formation.

2-amino-1-methyl-6-phenylimidazo [4, 5-b] pyridine

PhIP

creatinine

phenylalanine

CRN

Phe

creatinine

phenylalanine

CRN

Phe

carbonyls

PhIP


Input: Although PhIP was produced to some extent in the CRN/Phe system, the presence of the oxidized lipid increased considerably the amount of PhIP produced.

PhIP

CRN

Phe

PhIP


Input: This increase seemed to be a consequence of the decrease in the E (a) of the reaction when the lipid was present, which diminished from 112. 9 to 80. 9 kJ/mol.


Input: On the other hand, the addition of the lipid did not seem to produce PhIP by an alternative mechanism because PhIP was formed analogously in both CRN/Phe and CRN/Phe/ON systems as a function of pH, creatinine concentration, phenylalanine concentration, time, temperature, oxygen concentration in the reaction atmosphere, and the addition of different amounts of ammonia.

PhIP

PhIP

CRN

Phe

CRN

Phe

creatinine

phenylalanine

oxygen

ammonia


Input: All these results suggest that the ability of lipid oxidation products to produce PhIP is related to their capacity to induce the Strecker degradation of phenylalanine to phenylacetaldehyde.

PhIP

phenylalanine

phenylacetaldehyde


Input: Therefore, any other reactive carbonyl compound that can produce the Strecker degradation of phenylalanine should also be considered as a potential inducer of PhIP formation under appropriate conditions.

carbonyl

phenylalanine

PhIP


Input: Rapid detecting total acid content and classifying different types of vinegar based on near infrared spectroscopy and least-squares support vector machine.


Input: More than 3. 2 million litres of vinegar is consumed every day in China.