Input: In this study, 30 Wistar rats were randomly divided into three groups: a control group, a sodium fluoride (NaF) + EGb group, and a NaF group.

sodium fluoride

NaF

NaF


Input: The rats were administered 0. 5 ml water containing NaF (100 mg/l) and EGb (120 mg/kg) per day via gavage.

NaF


Input: After 3 months, the rats' capacity for learning and memory was tested using a Y-maze.


Input: Damage to hippocampal neurons was evaluated by histological examination of the CA3 area.


Input: Superoxide dismutase (SOD) activity and the levels of glutathione peroxidase (GSH-Px) and malondialdehyde (MDA) were measured.

Superoxide

glutathione

GSH

malondialdehyde

MDA


Input: Furthermore, the expression levels of Bcl-2 and Bax and the levels of cleaved Caspase3 in the hippocampus were evaluated by RT-PCR and Western blotting.


Input: The results showed that EGb could improve learning and memory abilities, enhance the activities of SOD and GSH-Px, attenuate the level of MDA, upregulate the ratio of Bcl-2/Bax, and downregulate the level of cleaved Caspase3.

GSH


Input: Effects of High Iron and Glucose Concentrations over the Relative Expression of Bcl2, Bax, and Mfn2 in MIN6 Cells.

Iron

Glucose


Input: Type 2 diabetes is characterized by hyperglycemia and oxidative stress.


Input: Hyperglycemia is linked to mitochondrial dysfunction and reduced beta-cell mass due to the reduced expression of genes such as Mfn2 as well as the participation of the Bcl2 gene family, responsible for increased apoptosis.


Input: The purpose of this study was to describe the effect of different iron and/or glucose concentrations over Mfn2, Bax, and Bcl2 expressions in a beta-pancreatic cell line (MIN6 cells).

iron

glucose


Input: MIN6 cells were pre-incubated with different iron and/or glucose concentrations, and the relative mRNA abundance of the Bcl2/Bax ratio and of Mfn2 genes was measured by qRT-PCR.

iron

glucose


Input: Heme oxygenase (HO) activity, iron uptake, superoxide dismutase activity, and glutathione content were also determined.

iron

superoxide

glutathione


Input: The Bcl2/Bax ratio increased and Mfn2 expression decreased in MIN6 cells after glucose stimulation.

glucose


Input: These effects were higher when glucose and iron were incubated together.

glucose

iron


Input: Additionally, treatment with glucose/iron showed a higher HO activity.

glucose

iron


Input: Our study revealed that high glucose/Fe concentrations in MIN6 cells induced an increase of the Bcl2/Bax ratio, an indicator of increased cell apoptosis.

glucose

Fe


Input: Ospemifene: first global approval.

Ospemifene


Input: Ospemifene (Osphena (TM)) is an oral selective estrogen receptor modulator (SERM), with tissue-specific estrogenic agonist/antagonist effects.

Ospemifene

Osphena

estrogen


Input: QuatRx Pharmaceuticals conducted the global development of the agent before licensing it to Shionogi for regulatory filing and commercialization worldwide.


Input: Ospemifene is the first non-estrogen treatment approved for moderate to severe dyspareunia in women with menopause-related vulvar and vaginal atrophy.

Ospemifene

estrogen


Input: The drug is approved in the USA, and application for EU regulatory approval is underway.


Input: This article summarizes the milestones in the development of ospemifene leading to this first approval for moderate to severe dyspareunia, a symptom of postmenopausal vulvar and vaginal atrophy.

ospemifene


Input: Pasireotide: A Review of Its Use in Cushing' s Disease.

Pasireotide


Input: Pasireotide (Signifor ((R))) is a new subcutaneous somatostatin analogue that acts via somatostatin receptors to inhibit the secretion of corticotropin from the pituitary adenoma in patients with Cushing' s disease.

Pasireotide

Signifor

somatostatin

somatostatin


Input: Pasireotide has a receptor binding profile that is distinct from that of other somatostatin analogues, binding with high affinity to somatostatin receptor subtype 5, which is strongly over expressed in corticotroph adenoma cells.

Pasireotide

somatostatin

somatostatin


Input: Pasireotide is the first pituitary-directed agent to be approved for use in Cushing' s disease.

Pasireotide


Input: In a phase III clinical trial in patients with Cushing' s disease, twice-daily pasireotide 600 or 900 mu g for 6 months led to normalization of urinary free cortisol (UFC) levels in up to a quarter of all patients (primary endpoint) and significantly reduced mean UFC levels.

pasireotide

cortisol


Input: The reduction in UFC levels is rapid (within one to two months) and sustained (up to 24 months).


Input: Most patients who do not have an early response to pasireotide do not respond at a later time point.

pasireotide


Input: Decreases in UFC levels achieved during pasireotide treatment are accompanied by decreases in serum and salivary cortisol levels, as well as improvements in clinical signs and symptoms, including body weight, blood pressure and health-related quality-of-life.

pasireotide

cortisol


Input: Pasireotide has a generally similar tolerability profile to that of other somatostatin analogues, but is associated with a relatively high incidence of hyperglycaemia, requiring the addition or intensification of glucose-lowering medication in a substantial proportion of patients.

Pasireotide

somatostatin

glucose


Input: Thus, pasireotide, together with on-going patient monitoring, provides a promising new option for the medical management of Cushing' s disease.

pasireotide


Input: Bicyclic Derivatives of L-Idonojirimycin as Pharmacological Chaperones for Neuronopathic Forms of Gaucher Disease.

L-Idonojirimycin


Input: New human beta-glucocerebrosidase (GCase) ligands with rigid 1, 6-anhydro-beta-L-idonojirimycin cores have been designed with the aid of molecular modeling.

1, 6-anhydro-beta-L-idonojirimycin


Input: Efficient pharmacological chaperones for the L444P (trafficking-incompetent) mutant GCase enzyme associated with type 2 and 3 Gaucher disease (GD) were identified.


Input: Proteomic identification of the candidate target proteins of 15-deoxy-delta (12, 14)-prostaglandin J2.

15-deoxy-delta (12, 14)-prostaglandin J2


Input: 15-deoxy-delta12, 14-prostaglandin J2 (15d-PGJ2) is an endogenous anti-inflammatory lipid derived from PGD2.

15-deoxy-delta12, 14-prostaglandin J2


Input: One potential mechanism for its activity is the covalent modification of cellular proteins, via a reactive alpha, beta-unsaturated carbonyl group in its cyclopentenone ring, which in turn alters protein function.

alpha, beta-unsaturated carbonyl

cyclopentenone


Input: In order to identify the candidate target proteins covalently modified by 15d-PGJ2 in human aortic endothelial cell (EC), EC were treated with biotinylated-15d-PGJ2, the modified proteins extracted by Neutravidin affinity-purification and the proteins identified by LTQ Orbitrap mass spectrometer.


Input: Classification of the 358 identified proteins was performed using PANTHER classification system (www. pantherdb. org), showing that the proteins mapped to metabolic process, cellular process and transport activity.


Input: This protein data set highlights the potential for 15d-PGJ2 to covalently modify cellular proteins and provides a source of data that will aid further studies on the mechanism of action of this endogenous regulator of inflammation.


Input: This article is protected by copyright.


Input: All rights reserved.


Input: Emergent Renal Dysfunction with Colistin Pharmacotherapy.

Colistin


Input: STUDY OBJECTIVE: To evaluate the association between the administration of intravenous (IV) colistin and the emergence of renal dysfunction.

colistin


Input: DESIGN: A retrospective medical record review.


Input: SETTING: A tertiary care academic medical center.


Input: PATIENTS: A total of 174 critically ill patients who received at least one dose of IV colistin between 2004 and 2007.

colistin


Input: MEASUREMENTS AND MAIN RESULTS: The primary outcome was development of renal dysfunction, defined as an increase in serum creatinine of 50% or more during therapy or the initiation of renal replacement therapy (RRT), in patients who received at least one dose of colistin and were not already on RRT.

creatinine

colistin


Input: The severity of renal dysfunction was further categorized by the RIFLE criteria.


Input: Demographic and clinical characteristics were analyzed by logistic regression for association with new renal dysfunction.


Input: A total of 174 patients were evaluated for renal dysfunction.


Input: Of these patients, 84 (48%) experienced renal dysfunction on colistin.

colistin


Input: On multivariate analysis, age in years (odds ratio [OR] 1. 03, 95% confidence interval [CI] 1. 01-1. 05) and receipt of concurrent nephrotoxin (s) (OR 3. 35, 95% CI 1. 34-8. 36) significantly increased the risk of developing renal dysfunction.


Input: CONCLUSION: In this critically ill population, renal dysfunction occurred frequently and was associated with older age and receipt of nephrotoxins.


Input: Patterning Surfaces for Controlled Platelet Adhesion and Detection of Dysfunctional Platelets.


Input: Platelets play a fundamental role in thrombus formation and in the pathogenesis of arterial thrombosis.


Input: Patterning surfaces for controlled platelet adhesion paves the way for adhesion and activation mechanisms in platelets and detection of platelet functional defects.


Input: Here, a new and simple method based on controlled polymerization of 2-methacryloyloxyethyl phosphorylcholine (MPC) on the surface of styrene-block-(ethylene-co-butylene)-block-styrene (SEBS) is shown.

2-methacryloyloxyethyl phosphorylcholine

MPC

styrene-block-(ethylene-co-butylene)-block-styrene

SEBS


Input: The competition between polymerization and degradation enables platelet adhesion on SEBS to be switched on and off.

SEBS


Input: The adhesive sites of the platelets can be down to single cell level, and the dysfunctional platelets can be quantitatively detected.


Input: Thermal and Electrical Transport in Ultralow Density Single-Walled Carbon Nanotube Networks.

Carbon


Input: The thermal, electrical, and thermoelectric properties of aerogels of single-walled carbon nanotubes are characterized.

carbon


Input: Their ultralow density enables the transport properties of the junctions to be distinguished from those of the nanotubes themselves.


Input: Junction thermal and electrical conductances are found to be orders of magnitude larger than those found in typical dense SWCNT networks.


Input: In particular, the average junction thermal conductance is close to the theoretical maximum for a van der Waals bonded SWCNT junction.


Input: A Tunable Spherical Cap Microfluidic Electrically Small Antenna.


Input: A highly efficient microfluidic 3D electrically small antenna is created using a simple fabrication technique.


Input: It is easy to construct simply by pneumatically inflating a planar microfluidic antenna into a spherical cap.


Input: It has premium performance around its hemispherical shape, combining a wide working band with high efficiency.


Input: Receptor-Specific Delivery of Protein Antigen to Dendritic Cells by a Nanoemulsion Formed Using Top-Down Non-Covalent Click Self-Assembly.


Input: A new class of targeted and immune-evading nanocarrier made using only biological components and facile processes is assembled in a bottom-up fashion.


Input: Simple top-down sequential addition of immune-evading or receptor-specific antibody elements conjugated to biosurfactant protein DAMP4 promotes self-assembly at an interface previously formed in the presence of peptide surfactant AM1, leading to a functional display at the interface through non-covalent molecular self-assembly.


Input: A Dual Enzyme Microgel with High Antioxidant Ability Based on Engineered Seleno-Ferritin and Artificial Superoxide Dismutase.

Superoxide


Input: An antioxidant microgel with both glutathione peroxidase (GPx) and superoxide dismutase (SOD) activities is reported.

glutathione

superoxide


Input: Using computational design and genetic engineering methods, the main catalytic components of GPx are fabricated onto the surface of ferritin.


Input: The resulting seleno-ferritin (Se-Fn) monomers can self-assemble into nanocomposites that exhibit remarkable GPx activity due to the well organized multi-GPx catalytic centers.

Se


Input: Subsequently, a porphyrin derivative is synthesized as an SOD mimic, and is employed to construct a synergistic dual enzyme system by crosslinking Se-Fn nanocomposites into a microgel.

porphyrin

Se


Input: Significantly, this dual enzyme microgel is demonstrated to display better antioxidant ability than single GPx or SOD mimics in protecting cells from oxidative damage.


Input: A Model-Based Approach to Predict Longitudinal HbA1c, Using Early Phase Glucose Data From Type 2 Diabetes Mellitus Patients After Anti-Diabetic Treatment.

Glucose


Input: Predicting late phase outcomes from early-phase findings can help inform decisions in drug development.


Input: If the measurements in early-phase differ from those in late phase, forecasting is more challenging.


Input: In this paper, we present a model-based approach for predicting glycosylated hemoglobin (HbA1c) in late phase using glucose and insulin concentrations from an early-phase study, investigating an anti-diabetic treatment.

glucose


Input: Two previously published models were used; an integrated glucose and insulin (IGI) model for meal tolerance tests and an integrated glucose-red blood cell-HbA1c (IGRH) model predicting the formation of HbA1c from the average glucose concentration (Cg, av).

glucose

glucose

glucose


Input: Output from the IGI model was used as input to the IGRH model.


Input: Parameters of the IGI model and drug effects were estimated using data from a phase1 study in 59 diabetic patients receiving various doses of a glucokinase activator.


Input: Cg, av values were simulated according to a Phase 2 study design and used in the IGRH model for predictions of HbA1c.


Input: The performance of the model-based approach was assessed by comparing the predicted to the actual outcome of the Phase 2 study.


Input: We have shown that this approach well predicts the longitudinal HbA1c response in a 12-week study using only information from a 1-week study where glucose and insulin concentrations were measured.

glucose


Input: Transient, Biocompatible Electronics and Energy Harvesters Based on ZnO.

ZnO


Input: The combined use of ZnO, Mg, MgO, and silk provides routes to classes of thin-film transistors and mechanical energy harvesters that are soluble in water and biofluids.

ZnO

Mg

MgO


Input: Experimental and theoretical studies of the operational aspects and dissolution properties of this type of transient electronics technology illustrate its various capabilities.


Input: Application opportunities range from resorbable biomedical implants, to environmentally dissolvable sensors, and degradable consumer electronics.


Input: Cell Surface Receptor Targeted Biomimetic Apatite Nanocrystals for Cancer Therapy.

Apatite


Input: Nanosized drug carriers functionalized with moieties specifically targeting tumor cells are promising tools in cancer therapy, due to their ability to circulate in the bloodstream for longer periods and their selectivity for tumor cells, enabling the sparing of healthy tissues.


Input: Because of its biocompatibility, high bioresorbability, and responsiveness to pH changes, synthetic biomimetic nanocrystalline apatites are used as nanocarriers to produce multifunctional nanoparticles, by coupling them with the chemotherapeutic drug doxorubicin (DOXO) and the DO-24 monoclonal antibody (mAb) directed against the Met/Hepatocyte Growth Factor receptor (Met/HGFR), which is over-expressed on different types of carcinomas and thus represents a useful tumor target.

apatites

doxorubicin

DOXO


Input: The chemical-physical features of the nanoparticles are fully investigated and their interaction with cells expressing (GTL-16 gastric carcinoma line) or not expressing (NIH-3T3 fibroblasts) the Met/HGFR is analyzed.


Input: Functionalized nanoparticles specifically bind to and are internalized in cells expressing the receptor (GTL-16) but not in the ones that do not express it (NIH-3T3).


Input: Moreover they discharge DOXO in the targeted GTL-16 cells that reach the nucleus and display cytotoxicity as assessed in an MTT assay.

DOXO

MTT


Input: Two different types of ternary nanoparticles are prepared, differing for the sequence of the functionalization steps (adsorption of DOXO first and then mAb or vice versa), and it is found that the ones in which mAb is adsorbed first are more efficient under all the examined aspects (binding, internalization, cytotoxicity), possibly because of a better mAb orientation on the nanoparticle surface.

DOXO


Input: These multifunctional nanoparticles could thus be useful instruments for targeted local or systemic drug delivery, allowing a reduction in the therapeutic dose of the drug and thus adverse side effects.


Input: Moreover, this work opens new perspectives in the use of nanocrystalline apatites as a new platform for theranostic applications in nanomedicine.

apatites


Input: Facile Preparation of Ordered Porous Graphene-Metal Oxide @C Binder-Free Electrodes with High Li Storage Performance.

Graphene

Metal Oxide

Li


Input: A facile and general method is reported to prepare ordered porous graphene-based binder-free electrodes on a large scale.

graphene


Input: This preparation process allows the easy adjustment of the selected components, weight ratio of componets, and the thickness of the electrodes.


Input: Such ordered porous electrodes demonstrate superior Li storage properties; for example, graphene-Fe3 O4 @C depicts high capacities of 1123. 8 and 505 mAh g (-1) at current densities of 0. 5 and 10 A g (-1), respectively.

Li

graphene

Fe3 O4


Input: On the association between Hashimoto' s thyroiditis and papillary thyroid carcinoma.


Input: Looking 100 years back and, hopefully, fewer years ahead to sort out this association.


Input: NOT required for a LETTER TO THE EDITOR.


Input: The Relationship between Charge Density and Polyelectrolyte Brush Profile Using Simultaneous Neutron Reflectivity and In Situ Attenuated Total Internal Reflection FTIR.


Input: We report on a novel experimental study of a pH-responsive polyelectrolyte brush at the silicon/D2O interface.

silicon


Input: A poly [2-(diethylamino) ethyl methacrylate] brush was grown on a large silicon crystal which acted as both a substrate for a neutron reflectivity solid/liquid experiment but also as an FTIR-ATR spectroscopy crystal.

poly [2-(diethylamino) ethyl methacrylate]

silicon


Input: This arrangement has allowed for both neutron reflectivities and FTIR spectroscopic information to be measured in parallel.


Input: The chosen polybase brush shows strong IR bands which can be assigned to the N-D (+) stretch, D2O, and a carbonyl group.

carbonyl


Input: From such FTIR data, we are able to closely monitor the degree of protonation along the polymer chain as well as revealing information concerning the D2O concentration at the interface.


Input: The neutron reflectivity data allows us to determine the physical brush profile normal to the solid/liquid interface along with the corresponding degree of hydration.


Input: This combined approach makes it possible to quantify the charge on a polymer brush alongside the morphology adopted by the polymer chains.


Input: Total Synthesis of the Marine Cyclic Depsipeptide Viequeamide A.

Viequeamide A


Input: The first total synthesis of viequeamide A, a natural cyclic depsipeptide isolated from a marine button cyanobacterium, was achieved with the N-Me-Val-Thr peptide bond as the final macrocyclization site.

viequeamide A

N-Me-Val-Thr


Input: The synthetic product gave nearly identical spectroscopic data to that reported for the natural product.


Input: Molecular Binoculars: How to Spatially Resolve Environmental Fluctuations by Following Two or More Single-Molecule Spectral Trails at a Time.


Input: We propose a novel type of spectral diffusion experiment that enables one to decouple spatial characteristics of the environmental fluctuations, such as their concentration, from the interaction with the chromophore.


Input: Traditional hole broadening experiments do not allow for such decoupling in the common case when the chromophore-environment interaction is scale invariant.


Input: Here we propose to simultaneously follow the spectral trails of a small number of nearby chromophores---two or more---which thereby sense a highly overlapping set of the fluctuations.


Input: To this end, we estimate the combined probability distribution for the frequencies of a set of chromophores contained within the {\em same} sample.


Input: The present setup introduces a new length scale, i. e., the inter-chromophore distance, which breaks the aforementioned scale invariance and enables one to determine independently the concentration of the environmental fluctuations and their coupling to the chromophores, by monitoring the time after which spectral diffusion of distinct chromophores becomes uncorrelated.


Input: We illustrate these results with structural excitations in low temperature glasses.


Input: Plasmonic resonances in self-assembled reduced symmetry gold nanorod structures.


Input: Self-assembled plasmonic Dolmen structures consisting of small gold nanorods (length = 50 nm and diameter = 20 nm) with a few nanometer gaps are observed to show coherent effects of super-radiance and characteristics of Fano resonance due to the significantly reduced symmetry of the structure.


Input: Relative to previous larger structures from top-down electron-beam lithography, the single crystallinity and atomically smooth surfaces of these self-assembled plasmonic structures result in 50% narrower resonances, and the small gaps with associated strong coupling enable observation of multiple dark and bright modes.


Input: By tilting the cap monomer with respect to the base dimer an order of magnitude increase in E-field enhancement at the Fano dip is obtained.


Input: In addition, a spectrally broad mode is observed indicating the strong impact of the geometry of the structure on the nature of coupled modes.


Input: The highly localized electric near-fields in the gaps will enable strong light matter interactions and the narrow resonances will be useful for improved figure of merits in inexpensive chemical and biosensing.


Input: Insight into the Structure of Single Antheraea pernyi Silkworm Fibers Using Synchrotron FTIR Microspectroscopy.


Input: Synchrotron FTIR (S-FTIR) microspectroscopy was used to monitor both protein secondary structures (conformations) and their orientations in single cocoon silk fibers of the Chinese Tussah silk moth (Antheraea pernyi).


Input: In addition, to understand further the relationship between structure and properties of single silk fibers, we studied the changes of orientation and content of different secondary structures in single A. pernyi silk fibers when subjected to different strains.


Input: The results showed that the content and orientation of beta-sheet was almost unchanged for strains from 0 to 0. 3.


Input: However, the orientation of alpha-helix and random coil improved progressively with increasing strain, with a parallel decrease in alpha-helix content and an increase in random coil.


Input: This clearly indicates that most of the deformation upon stretching of the single fiber is due to the change of orientation in the amorphous regions coupled with a conversion of some of the alpha-helix to random coil.


Input: These observations provide an explanation for the supercontraction behavior of certain animal silks and are likely to facilitate understanding and optimization of postdrawing used in the conjunction with the wet-spinning of silk fibers from regenerated silk solutions.


Input: Thus, our work demonstrates the power of S-FTIR microspectroscopy for studying biopolymers.


Input: Statins Protect Human Endothelial Cells from TNF-induced Inflammation via ERK5 Activation.


Input: 3-Hydroxy-3-methylglutaryl coenzyme A reductase inhibitors (statins) exert pleiotropic effects on the cardiovascular system, in part through a decrease in reactive oxygen species (ROS) formation and reduction of vascular inflammation.

3-Hydroxy-3-methylglutaryl coenzyme A

oxygen


Input: To elucidate the molecular mechanisms involved in these effects, we investigated the effect of statins on TNF-alpha-induced ROS production, vascular cell adhesion molecule-1 (VCAM-1) and intercellular adhesion molecule-1 (ICAM-1) expression in human aortic endothelial cells (HAECs).


Input: Exposure of HAECs to TNF-alpha caused production of ROS via Rac-1 membrane translocation and activation.


Input: The Rac-1 activation and ROS liberation mediated TNF-stimulated NF-kappa B activation and the subsequent VCAM-1 and ICAM-1 expression.


Input: Extracellular-signal-regulated kinase 5 (ERK5) plays a central role in inhibiting endothelial inflammation.


Input: Immune complex kinase assay of protein extracts from HAECs treated with atorvastatin revealed increased ERK5 activity in a time-and dose-dependent manner.

atorvastatin


Input: In addition, pretreatment with atorvastatin inhibited TNF-alpha-induced ROS production and VCAM-1 and ICAM-1 expression.

atorvastatin


Input: Chemical or genetic inhibition of ERK5 ablated the statins inhibition of Rac-1 activation, ROS formation, NF-kappa B, VCAM-1 and ICAM-1 expression induced by TNF-alpha.


Input: Taken together, statins, via ERK5 activation, suppress TNF-stimulated Rac-1 activation, ROS generation, NF-kappa B activation and VCAM-1 and ICAM-1 expression in human ECs, which provides a novel explanation for the pleiotropic effects of statins that benefit the cardiovascular system.


Input: Protective effect of ethyl acetate fraction of Acacia ferruginea DC. against ethanol-induced gastric ulcer in rats.

ethyl acetate

ethanol


Input: ETHNOPHARMACOLOGICAL RELEVANCE: In traditional systems of medicine, stem bark of Acacia ferruginea DC.


Input: is used for the treatment of itching, leucoderma, ulcers, stomatitis and diseases of the blood.


Input: In the present study, we determined antioxidant and anti-ulcerogenic activities of Acacia ferruginea stem bark.


Input: MATERIALS AND METHODS: Acetone extract and its sub-fractions of Acacia ferruginea stem bark were subjected to assess their antioxidant potential using various in vitro systems such as DPPH (*), ABTS (* +) scavenging, FRAP and phosphomolybdenum reduction activities.

Acetone

DPPH (*)

ABTS (* +)

phosphomolybdenum


Input: Based on the antioxidant potential, the ethyl acetate fraction was used to evaluate the protective effect of ethanol-induced gastric damage in rat model.

ethanol


Input: Enzyme activities such as superoxide dismutase, glutathione, catalase and lipid peroxidation were also determined in the stomach tissues.

superoxide

glutathione


Input: RESULTS: Ethyl acetate fraction (AFE) of Acacia ferruginea stem bark registered higher antioxidant and free radical scavenging activities than the crude acetone extract and other fractions.

Ethyl acetate

acetone


Input: In addition, AFE exhibited that the IC50 values of DPPH (2. 5 micro g/ml) and ABTS (1. 8 micro g/ml) were lower when compared to the standard quercetin (12. 4 micro g/ml and 4. 7 micro g/ml, respectively).

DPPH

ABTS

quercetin


Input: In ethanol induced gastric ulcer, administration of AFE at doses of 10mg/kg, 50mg/kg and 100mg/kg body weight prior to ethanol ingestion significantly protected the stomach ulceration.

ethanol

ethanol


Input: Consequently significant changes were observed in enzyme activities such as SOD, CAT, GSH and LPO in the stomach tissues when compared with ethanol control group.

GSH

ethanol


Input: CONCLUSION: It is concluded that the ethyl acetate fraction of Acacia ferruginea stem bark possessed higher antioxidant and anti-ulcerogenic activities.

ethyl acetate


Input: Based on the results we suggest that Acacia ferruginea stem bark has potential to provide a therapeutic approach to ethanol mediated ulcer as an effective anti-ulcer agent.

ethanol


Input: Botany, traditional uses, phytochemistry and pharmacology of Waltheria indica L.


Input: (syn. Waltheria americana): A review.


Input: ETHNOPHARMACOLOGICAL RELEVANCE: Waltheria indica L.


Input: (syn. Waltheria americana) is commonly used in traditional medicine in Africa, South America and Hawaii, mainly against pain, inflammation, conditions of inflammation, diarrhea, dysentery, conjunctivitis, wounds, abscess, epilepsy, convulsions, anemia, erectile dysfunctions, bladder ailments and asthma.


Input: AIM OF THE REVIEW: To provide an up-to-date overview of the botany, phytochemistry, traditional uses, pharmacological activities and toxicity data of Waltheria indica.


Input: Additionally, studies providing an evidence for local and traditional uses of Waltheria indica are discussed.


Input: Further phytochemical and pharmacological potential of this species are suggested for future investigations.


Input: MATERIALS AND METHODS: The information was collected from scientific journals, books, theses and reports via academic libraries and electronic search.


Input: These sources include Pubmed, Web of Science, Portal de Portales-Latindex, Science Research. com and Google scholar.


Input: These studies about the medical botanical, traditional uses, chemical, pharmacological and toxicological data on Waltheria indica were published in English, Portuguese, Spanish, German and French.


Input: RESULTS: Crude extracts and isolated compounds from Waltheria indica were investigated and showed analgesic, anti-inflammatory, antibacterial, antifungal, antimalarial, anti-anemic, anti-oxidant, sedative and anticonvulsant activities.


Input: The phytochemical investigations showed the presence of cyclopeptid alkaloids, flavonoids (e. g., (-)-epicatechin, quercetin, kaempferol, kaempferol-3-O-beta-d-(6''-E-p-coumaryl)-glucopyranoside), tannins, sterols, terpenes, saponins, anthraquinones.

cyclopeptid alkaloids

flavonoids

(-)-epicatechin

quercetin

kaempferol

kaempferol-3-O-beta-d-(6''-E-p-coumaryl)-glucopyranoside)

tannins

sterols

terpenes

saponins

anthraquinones


Input: Studies of acute toxicity in animal indicated that Waltheria indica can be toxic.


Input: CONCLUSION: Waltheria indica possess therapeutic potential in the treatment of inflammation, malaria, infectious diseases (e. g., lungs infection due to Klebsiella pneumoniae, diarrhea due to Candida albicans or Escherichia coli) and prevention of oxidative stress.


Input: Further studies are necessary to explore pure compounds responsible for the pharmacological effects and the mechanisms of action.


Input: Further investigations are also needed to provide an evidence base for traditional uses of this species against pain, anemia, convulsions and epilepsy.


Input: In addition, there is a pressing need to investigate the other traditional uses such as dysentery, syphilis, erectile dysfunctions and asthma.


Input: beta-estradiol 17-valerate affects embryonic development and sexual differentiation in Japanese medaka (Oryzias latipes).

beta-estradiol 17-valerate


Input: beta-estradiol 17-valerate (EV) is a synthetic estrogen widely used in combination with other steroid hormones in hormone replacement therapy drugs and is detected in natural waters.

beta-estradiol 17-valerate

estrogen

steroid hormones


Input: Although EV is known as an estrogenic chemical, there is still a lack of data on its developmental and reproductive toxicities in fish following exposure to EV during embryo-larval-, juvenile-and adult-life stages in Japanese medaka (Oryzias latipes).


Input: At the early life stage, the fertilized eggs of medaka were exposed to 1, 10, 100 and 1000ng/L EV for 15 days, and hatched larval fish were continually exposed to the same concentration range for an additional 15 days.


Input: The results showed that exposure to 10ng/L or above resulted in adverse effects on hatchability and time to hatching, and the number of hatched females was twice that of males at 10ng/L or above.


Input: When the hatched fish were continually exposed to 1, 10 and 100ng/L of EV for another 40 days, the hepatosomatic index (HSI) was increased in both males and females, and the gonadosomatic index (GSI) was decreased in females, and increased in males.


Input: Sex reversal was found in fish exposed to 1ng/L and above.


Input: Quantitative real-time RT-PCR showed that mRNA levels of estrogen receptor alpha (ER-alpha) and vitellogenin-I (VTG-I) in the liver of females were significantly down-regulated, while those of vitellogenin-I (VTG-I) in the liver of males were significantly up-regulated at all concentrations.

estrogen


Input: These findings suggest that EV is a reproductive toxicant and estrogenic chemical in both male and female fish.


Input: Estradiol replacement enhances cocaine-stimulated locomotion in female C57BL/6 mice through estrogen receptor alpha.

Estradiol

cocaine

estrogen


Input: Psychostimulant effects are enhanced by ovarian hormones in women and female rodents.


Input: Estradiol increases behavioral responses to psychostimulants in women and female rats, although the underlying mechanism is unknown.

Estradiol


Input: This study utilized mice to investigate the time frame and receptor mediation of estradiol' s enhancement of cocaine-induced behavior as mice enable parallel use of genetic, surgical and pharmacological methods.

estradiol

cocaine


Input: The spontaneous behavior of Sham and Ovariectomized (Ovx) female wildtype (WT) mice was determined during habituation to a novel environment and after cocaine administration.

cocaine


Input: Ovx mice were replaced with vehicle (sesame oil) or 17 beta-estradiol (E2) for 2 days or 30 min prior to a cocaine challenge to investigate the time course of E2' s effects.

17 beta-estradiol

cocaine


Input: To examine receptor mediation of estradiol effects, Ovx mice replaced for 2 days with either the ER alpha-selective agonist PPT or the ER beta-selective agonist DPN were compared to Sham mice, and mice lacking either ER alpha (alpha ERKO) or ER beta (beta ERKO) were compared to WT littermates.

estradiol

PPT

DPN


Input: Ovx mice exhibited fewer ambulations during habituation than Sham females.


Input: Cocaine-induced increases in behavioral ratings were greater in Sham than in Ovx mice.

Cocaine


Input: Two days but not 30 min of E2 replacement in Ovx mice increased cocaine responses to Sham levels.

cocaine


Input: PPT replacement also increased the cocaine response relative to vehicle-or DPN-treated Ovx mice.

PPT

cocaine

DPN


Input: alpha ERKO mice displayed modestly attenuated behavioral responses to novelty and cocaine compared to alpha WT littermates, but no behavioral differences were found between beta ERKO and beta WT mice.

cocaine


Input: These results suggest that E2 enhances cocaine-stimulated locomotion in mice predominantly through ER alpha.

cocaine


Input: Discovery of natural estrogen receptor modulators with structure-based virtual screening.

estrogen


Input: Eleven compounds were identified as estrogen receptor modulators from an in-house natural product database (NPD) by structure-based virtual screening for ER alpha and ER beta.

estrogen


Input: Among them, 3 compounds were confirmed as ER agonists and 8 compounds were confirmed as ER antagonists by yeast two-hybrid (Y2H) assay, with EC50 values ranging from several micromolar to 100 micromolar.


Input: In this study, a novel series of cycloartane triterpenoids isolated from Schisandra glaucescens Diels was found to have ER antagonistic effect, the most potent antagonist of which exhibited activity with EC50 value of 2. 55 and 4. 68 mu M for ER alpha and ER beta, respectively.

cycloartane triterpenoids


Input: Moreover, the types of modulation and subtype selectivity were also investigated through molecular docking simulation.


Input: Designing degradable hydrogels for orthogonal control of cell microenvironments.


Input: Degradable and cell-compatible hydrogels can be designed to mimic the physical and biochemical characteristics of native extracellular matrices and provide tunability of degradation rates and related properties under physiological conditions.


Input: Hence, such hydrogels are finding widespread application in many bioengineering fields, including controlled bioactive molecule delivery, cell encapsulation for controlled three-dimensional culture, and tissue engineering.


Input: Cellular processes, such as adhesion, proliferation, spreading, migration, and differentiation, can be controlled within degradable, cell-compatible hydrogels with temporal tuning of biochemical or biophysical cues, such as growth factor presentation or hydrogel stiffness.


Input: However, thoughtful selection of hydrogel base materials, formation chemistries, and degradable moieties is necessary to achieve the appropriate level of property control and desired cellular response.


Input: In this review, hydrogel design considerations and materials for hydrogel preparation, ranging from natural polymers to synthetic polymers, are overviewed.


Input: Recent advances in chemical and physical methods to crosslink hydrogels are highlighted, as well as recent developments in controlling hydrogel degradation rates and modes of degradation.


Input: Special attention is given to spatial or temporal presentation of various biochemical and biophysical cues to modulate cell response in static (i. e., non-degradable) or dynamic (i. e., degradable) microenvironments.


Input: This review provides insight into the design of new cell-compatible, degradable hydrogels to understand and modulate cellular processes for various biomedical applications.


Input: Phytoestrogenic Potential of Cyclopia Extracts and Polyphenols.

Polyphenols


Input: Cyclopia Vent. species, commonly known as honeybush, are endemic to Southern Africa.


Input: The plant is traditionally used as an herbal tea but several health benefits have recently been recorded.


Input: This minireview presents an overview of polyphenols found in Cyclopia and focusses on the phytoestrogenic potential of selected polyphenols and of extracts prepared from the plant.

polyphenols

polyphenols


Input: Large lateral movement of transmembrane helix S5 is not required for substrate access to the active site of rhomboid intramembrane protease.


Input: Rhomboids represent an evolutionarily ancient protease family.


Input: Unlike most other proteases, they are polytopic membrane proteins, and specialize in cleaving transmembrane protein substrates.


Input: Rhomboid protease' s polar active site is embedded in the membrane, and normally closed.


Input: For bacterial rhomboid GlpG, it has been proposed that one of the protease' s transmembrane helices (S5) can rotate to open a lateral gate, enabling substrate to enter the protease from inside the membrane.


Input: Here we study GlpG' s conformational change by solving the cocrystal structure of the protease with a mechanism-based inhibitor.


Input: We also examine the lateral gating model by crosslinking S5 to a neighboring helix (S2).


Input: The crystal structure shows that inhibitor binding displaces a capping loop (L5) from the active site, but causes only minor shifts of the transmembrane helices.


Input: Crosslinking S5 and S2, which not only restricts S5' s lateral movement, but also prevents substrate from passing between the two helices, does not hinder the protease' s ability to cleave a membrane protein substrate in detergent solution and in reconstituted membrane vesicles.


Input: Taken together, these data suggest that a large lateral movement of S5 helix is not required for substrate access to rhomboid protease' s active site.


Input: Resumption of menstruation and pituitary response to gonadotropin-releasing hormone in functional hypothalamic amenorrhea undertaking estrogen replacement therapy.

gonadotropin-releasing hormone

estrogen


Input: Background: Functional hypothalamic amenorrhea (FHA) refers to a functional menstrual disorder with various causes and presentations.


Input: Recovery of menstrual cyclicity is common in long-term follow-up but the affecting factors remain unknown.


Input: Aim: To explore factors affecting the menstrual resumption and to evaluate the pituitary response to gonadotropin-releasing hormone (GnRH) in FHA.

gonadotropin-releasing hormone

GnRH


Input: Materials and Methods: Thirty cases with FHA were recruited.


Input: All subjects were put on continuous 1mg/day estradiol valerate orally and followed up monthly.

estradiol valerate


Input: Recovery was defined as the occurrence of at least three consecutive regular cycles.


Input: Responder referred to those who recovered within two years of therapy.


Input: Gonadotropin response to the 50 microgram GnRH challenge was tested every three months.

GnRH


Input: Results: Nineteen (63. 3%) subjects recovered with a mean time to recovery of 26. 8 months.


Input: Time to recovery was negatively correlated with body mass index (BMI) before and by amenorrhea.


Input: Twenty-one cases had undertaken therapy for more than two years and ten of them recovered.


Input: BMI before and by amenorrhea were negatively correlated with the recovery.


Input: Significant increase of serum luteinizing hormone (LH) and LH response to GnRH were noted after recovery.

GnRH


Input: Conclusions: Menstrual resumption was common in FHA undertaking ERT.


Input: The likelihood of recovery was affected by their BMI before and by amenorrhea but not by the weight gain during therapy.


Input: Low serum LH and attenuated LH response to GnRH were the main features of pituitary deficiency in FHA.

GnRH


Input: The menstrual resumption in FHA was accompanied by the recovery of serum LH and the LH response to GnRH.

GnRH


Input: CHRONIC IDIOPATIC URTICARIA AND GRAVES' DISEASE.


Input: Chronic urticaria is a common condition characterized by recurrent episodes of mast cell-driven wheal and flare-type skin reactions lasting for more than 6 weeks.


Input: In about 75% of cases, the underlying causes remain unknown, and the term chronic idiopathic urticaria (CIU) is used to emphasize that wheals develop independently of identified external stimuli.


Input: Although CIU affects about 1. 0% of the general population, its etiopathogenesis is not yet well understood.


Input: It is now widely accepted that in many cases CIU should be regarded as an autoimmune disorder caused by circulating and functionally active IgG autoantibodies specific for the IgE receptor (FceRI) present on mast cells and basophils or for IgE itself.


Input: The well-known association of CIU with other autoimmune processes/diseases represents further indirect evidence of its autoimmune origin.


Input: Autoimmune thyroid diseases, especially autoimmune thyroiditis, represent the most frequently investigated diseases in association with CIU.


Input: Here we review this topic with particular regard to the association between Graves' disease and CIU.


Input: The possible pathogenetic mechanisms and the clinical implications of such an association are discussed.


Input: The Beneficial Effect of Total Glucosides of Paeony on Psoriatic Arthritis Links to Circulating Tregs and Th1 Cell Function.


Input: Total glycosides of peony (TGP) is a natural immuno-modulatory drug extracted from traditional Chinese herb peony.


Input: It has been approved by State Food and Drug Administration for the treatment of rheumatoid arthritis.


Input: However, data of TGP effect on psoriatic arthritis (PsA) is still scarce.


Input: In this study, 19 patients with PsA received 12-week treatment of TGP, and clinical efficacy in joint manifestations was evaluated by DAS28 at weeks 0, 4, 8 and 12.


Input: Peripheral percentages of Tregs, Th1, Th2 and NK cells were analyzed, and serum Th1-type cytokines (IL-12, IFN-gamma and TNF-alpha), Th2-type cytokines (IL-4, IL-5 and IL-10) as well as pro-inflammatory factors (IL-2, IL-6 and IL-8) were concomitantly examined.


Input: Six patients (32%) exhibited >= 25% decrease of DAS28 (responders).


Input: Interestingly, all responders displayed a continuous decrease in Treg and Th1 numbers during TGP treatment, concomitant with significant decreases in Th1-type cytokine levels.


Input: Serum IL-6 also showed a significant decline in responders.


Input: Non-responders lacked these sequential alterations.


Input: Thus, TGP merits further consideration as a promising therapeutic option for PsA.


Input: The result indicated that recovery of Tregs and Th1 may serve as prognostic markers to assess responsiveness to TGP treatment in PsA.


Input: Copyright (c) 2013 John Wiley & Sons, Ltd.


Input: Amphiphilic Polypeptides as a Bifunctional Template in the Mineralization of Calcium Carbonate at the Air/Water Interface.

Calcium Carbonate


Input: A well-defined amphiphilic polypeptide, poly (glutamic acid) 22-block-poly (alanine) 8 (PGlu22-b-PAla8), which plays the roles of both soluble (functional) additive and insoluble (structural) matrix, is employed to mediate the mineralization of CaCO3 at the air/water interface.

poly (glutamic acid) 22-block-poly (alanine) 8


Input: X-ray diffraction (XRD) and Raman spectroscopy, for example, show that the polymorph of CaCO3 particles obtained is calcite.

calcite


Input: The observations from SEM and TEM suggest that PGlu22-b-PAla8 initiates the amorphous precursor phase and heterogeneous nucleation of CaCO3 at the air/water interface, while temporarily stabilizes the gelatinous precursors as a process-directing agent; nevertheless, the initial concentration of Ca (2 +) controls the procedure of crystallization and the final morphology of CaCO3 particles.

Ca (2 +)


Input: Such " bifunctional " amphiphilic-polypeptide-regulated mineralization at the air/water interface may be applied to the synthesis of many kinds of symmetrical inorganic/organic hybrids.


Input: Very Low Calorie Diet Mimics the Early Beneficial Effect of Roux-en-Y Gastric Bypass on Insulin Sensitivity and Beta-Cell Function in Type 2 Diabetic Patients.


Input: Marked improvement in glycemic control occurs in patients with type 2 diabetes (T2DM) shortly after Roux-en-Y gastric bypass surgery (RYGB) and before there is major weight loss.


Input: The objective of this study was to determine if the magnitude of this change is primarily due to caloric restriction or is unique to the surgical procedure.


Input: We studied eleven subjects who underwent RYGB and fourteen subjects mean-matched for BMI, HbA1c and diabetes duration who were admitted to our inpatient research unit and given a very low calorie diet (VLCD) of 500 kcal/day with a macronutrient content similar to that consumed by patients after RYGB.


Input: Frequently sampled intravenous glucose tolerance tests were performed before and after interventions.

glucose


Input: Both groups lost an equivalent amount of weight over a mean study period of 21 days.


Input: Insulin sensitivity, acute insulin secretion after intravenous glucose administration and beta-cell function as determined by disposition index improved to a similar extent in both groups.

glucose


Input: Likewise, changes in fasting glucose and fructosamine levels were similar.

glucose

fructosamine


Input: Based on these data, VLCD improves insulin sensitivity and beta-cell function just as well as RYGB in the short term.


Input: This study was registered in ClinicalTrials. gov NCT00627484.


Input: Central Pulse Pressure and Its Hemodynamic Determinants in Middle-Aged Adults With Impaired Fasting Glucose and Diabetes: The Asklepios study.

Glucose


Input: OBJECTIVEPulse pressure (PP), a strong predictor of cardiovascular events in type 2 diabetes, is a composite measure affected by several hemodynamic factors.


Input: Little is known about the hemodynamic determinants of central PP in type 2 diabetes or whether abnormalities in central pulsatile hemodynamics are already present in individuals with impaired fasting glucose (IFG).

glucose


Input: In a population-based study, we aimed to compare central PP and its hemodynamic determinants among adults with normal fasting glucose (n = 1654), IFG (n = 240), and type 2 diabetes (n = 33). RESEARCH DESIGN AND METHODSWe measured carotid pressure, left ventricular outflow, aortic root diameter, carotid artery flow, and distension in order to measure various structural and hemodynamic arterial parameters. RESULTSIFG was associated with a greater mean arterial pressure (MAP) but was not associated with intrinsic aortic stiffening or abnormal aortic pulsatile indices after adjustment for MAP.

glucose


Input: After adjustment for age, sex, and MAP, type 2 diabetes was associated with a higher aortic root characteristic impedance (Zc), aortic root elastance-thickness product (Eh), and aortic root pulse wave velocity (but not aortic root diameter), a greater carotid-femoral pulse wave velocity, and lower total arterial compliance and wave reflection magnitude.


Input: Carotid size, Zc, distensibility, or Eh did not significantly differ between the groups. CONCLUSIONSType 2 diabetes, but not IFG, is associated with greater large artery stiffness, without abnormalities in aortic root diameter or carotid stiffness.


Input: Subjects with type 2 diabetes demonstrate a decreased reflection magnitude, which may indicate an increased penetration of pulsatile energy to distal vascular beds.


Input: Genetics of mineralocorticoid excess: an update for clinicians.


Input: Aldosterone plays a major role in regulating sodium and potassium homeostasis, and blood pressure.

Aldosterone

sodium

potassium


Input: More recently aldosterone has emerged as a key hormone in mediating end organ damage.

aldosterone


Input: In extreme cases, dysregulated aldosterone production leads to primary aldosteronism, the most common form of secondary hypertension.

aldosterone


Input: However, even within the physiological range, high levels of aldosterone are associated with an increased risk of developing hypertension over time.

aldosterone


Input: Primary aldosteronism represents the most common and curable form of hypertension, with a prevalence that increases with the severity of hypertension.


Input: Although genetic causes underlying glucocorticoid remediable aldosteronism, one of the three Mendelian forms of primary aldosteronism, were established some time ago, somatic and inherited mutations in the potassium channel GIRK4 have only recently been implicated in the formation of aldosterone producing adenoma and in familial hyperaldosteronism type 3.

potassium

aldosterone


Input: Moreover, recent findings have identified somatic mutations in two additional genes, involved in maintaining intracellular ionic homeostasis and cell membrane potential, in a subset of aldosterone producing adenoma. This review summarizes our current knowledge on the genetic determinants that contribute to variations in plasma aldosterone and renin levels in the general population, and the genetics of familial and sporadic primary aldosteronism.

aldosterone

aldosterone


Input: Various animal models that have significantly improved our understanding of the pathophysiology of excess aldosterone production will also be discussed.

aldosterone


Input: Finally, we will outline the cardiovascular, renal and metabolic consequences of mineralocorticoid excess beyond blood pressure regulation.


Input: Synthesis of Atactic and Isotactic Poly (1, 2-glycerol carbonate) s: Degradable Polymers for Biomedical and Pharmaceutical Applications.

Poly (1, 2-glycerol carbonate) s


Input: The synthesis and characterization of atactic and isotactic linear poly (benzyl 1, 2-glycerol carbonate) s are reported.

poly (benzyl 1, 2-glycerol carbonate) s


Input: The poly (benzyl 1, 2-glycerol carbonate) s were obtained via the ring-opening copolymerization of rac-/(R)-benzyl glycidyl ether with CO2 using [SalcyCo (III) X] complexes with high carbonate linkage selectivity and polymer/cyclic carbonate selectivity (> 99%).

poly (benzyl 1, 2-glycerol carbonate) s

rac-/(R)-benzyl glycidyl ether

[SalcyCo (III) X]

carbonate

carbonate


Input: Deprotection of the resultant polymers afforded poly (1, 2-glycerol carbonate) s with a functionalizable pendant primary hydroxyl group.

poly (1, 2-glycerol carbonate) s

primary hydroxyl


Input: Poly (1, 2-glycerol carbonate) showed a remarkable increase in degradation rate compared to poly (1, 3-glycerol carbonate) with a t1/2 =~ 2-3 days.

Poly (1, 2-glycerol carbonate)

poly (1, 3-glycerol carbonate)


Input: These polymers fulfill an unmet need for a readily degradable biocompatible polycarbonate.

polycarbonate


Input: A New Face for Old Antibiotics: Tetracyclines in Treatment of Amyloidoses.

Tetracyclines


Input: The use of tetracyclines has declined because of the appearance of resistant bacterial strains.

tetracyclines


Input: However, the indications of nonantimicrobial activities of these drugs have considerably raised interest and triggered clinical trials for a number of different pathologies.


Input: About 10 years ago we first reported that tetracyclines inhibited the aggregation of prion protein fragments and Alzheimer' s beta peptides, destabilizing their aggregates and promoting their degradation by proteases.

tetracyclines


Input: On the basis of these observations, the antiamyloidogenic effects of tetracyclines on a variety of amyloidogenic proteins were studied and confirmed by independent research groups.

tetracyclines


Input: In this review we comment on the data available on their antiamyloidogenic activity in preclinical and clinical studies.


Input: We also put forward that the beneficial effects of these drugs are a result of a peculiar pleiotropic action, comprising their interaction with oligomers and disruption of fibrils, as well as their antioxidant, anti-inflammatory, antiapoptotic, and matrix metalloproteinase inhibitory activities.


Input: Physicochemical characterization of nimodipine-polyethylene glycol solid dispersion systems.

nimodipine

polyethylene glycol


Input: Abstract This study investigates the solid-solid interactions between nimodipine (NIM) and polyethylene glycol (PEG) of different mean molecular weights (PEG 2000, 4000 and 6000), in solid dispersion systems, applying differential scanning calorimetry (DSC), Fourier-Transform infrared spectroscopy, powder X-ray diffraction (PXRD), hot stage microscopy (HSM) and theoretical modeling by the Flory-Huggins (FH) solution theory.

nimodipine

NIM

polyethylene glycol

PEG

PEG 2000, 4000 and 6000


Input: Phase diagrams constructed with the aid of DSC and FH solution theory showed sensitivity on the estimated values of the FH interaction parameter (chi).


Input: When chi is considered a constant number (chi = alpha, alpha != 0), formation of a eutectic mixture is predicted in the 70-80% w/w PEG concentration region, while when chi was considered as a function of concentration and temperature (chi = f (phi, Tau)), the model predicts the formation of monotectic systems.

PEG


Input: Construction of more precise phase diagrams by HSM to the aid of Kofler' s " contact preparation " method confirmed the monotectic nature of the examined systems.


Input: Studies on NIM' s re-crystallization process in the solid dispersions revealed a strong dependence of the crystallization rate, as well as the resulting crystal form, on the mean molecular weight and concentration of PEG: NIM crystallization rates decrease as PEG' s MW increases, while NIM mod II crystals predominate in dispersions prepared at temperatures above NIM' s liquidus and growth of NIM mod I prevailing in PEG-rich samples.

NIM

PEG

NIM

PEG

NIM

NIM

NIM

PEG


Input: Discovery of a New Class of Natural Product-Inspired Quinazolinone Hybrid as Potent Antileishmanial agents.

Quinazolinone


Input: The high potential of quinazolinone containing natural products and their derivatives in medicinal chemistry led us to discover four novel series of 53 compounds of quinazolinone based on the concept of molecular hybridization.

quinazolinone

quinazolinone


Input: Most of the synthesized analogues exhibited potent leishmanicidal activity against intracellular amastigotes (IC50 from 0. 65 +/- 0. 2 to 7. 76 +/- 2. 1 mu M) as compared to miltefosine (IC50 = 8. 4 +/- 2. 1 mu M) and nontoxic toward the J-774A. 1 cell line and Vero cells.

miltefosine


Input: Moreover, activation of Th1 type and suppression of Th2 type immune responses and induction in nitric oxide generation proved that 8a and 8g induce murine macrophages to prevent survival of parasites.

nitric oxide


Input: Compounds 8a and 8g exhibited significant in vivo inhibition of parasite 73. 15 +/- 12. 69% and 80. 93 +/- 10. 50% against Leishmania donovani/hamster model.


Input: Our results indicate that compounds 8a, 8g, and 9f represent a new structural lead for this serious and neglected disease.


Input: A road map for molecular ecology.


Input: The discipline of molecular ecology has undergone enormous changes since the journal bearing its name was launched approximately two decades ago.


Input: The field has seen great strides in analytical methods development, made groundbreaking discoveries and experienced a revolution in genotyping technology.


Input: Here, we provide brief perspectives on the main subdisciplines of molecular ecology, describe key questions and goals, discuss common challenges, predict future research directions and suggest research priorities for the next 20 years.


Input: New trifluoromethyl quinolone derivatives: Synthesis and investigation of antimicrobial properties.

trifluoromethyl quinolone


Input: A series of quinolone derivatives, containing different heterocyclic amines were prepared.

quinolone

heterocyclic amines


Input: Synthesized compounds were evaluated for their in vitro antimicrobial activities against two Gram-positive bacteria, three Gram-negative bacteria as well as four fungi.


Input: All the derivatives showed good activity towards Gram-positive bacteria and less activity towards Gram-negative bacteria.


Input: They also showed moderate to comparable activity against Aspergillus niger and Candida albicans and low to moderate antifungal activity against Aspergillus fumigatus and Aspergillus flavus.


Input: In vitro antiproliferative effect of a water-soluble Laminaria japonica polysaccharide on human melanoma cell line A375.


Input: A water-soluble polysaccharide WPS-2-1, purified from Laminaria japonica, has been found to have antitumor activity.


Input: In this study, WPS-2-1 exhibited high anti-proliferative activity on A375 cells in a dosedependent manner.


Input: Further investigation indicated that WPS-2-1 induced A375 cells apoptosis.


Input: Moreover, WPS-2-1-induced apoptosis was associated with the alteration in expressions of Bcl-2 family proteins.


Input: Mitochonadrial apoptotic pathway was involved in WPS-2-1-induced apoptosis, which included the loss of mitochondrial membrane and activation of caspase-3/9.


Input: The results in this study suggested that WPS-2-1 could effectively inhibit proliferation of A375 cells in vitro and induce apoptosis via mitochondrial apoptotic pathway.


Input: It might serve as a potential anti-tumor agent.


Input: Body composition assessment for the definition of cardiometabolic risk.


Input: Obesity is associated with a major prevalence of cardiovascular risk factors and high risk of cardiovascular events and contributes to the increase in cardiovascular morbidity and mortality worldwide.


Input: Beyond the fat mass per se, the pattern of fat distribution has a profound influence on cardiometabolic risk.


Input: The increase in abdominal adipose tissue confers an independent risk, while the amount of gluteofemoral body fat is thought to be protective.


Input: Changes in the capacity of different depots to store and release fatty acids and to produce adipocytokines are important determinants of fat distribution and its metabolic consequences.

fatty acids


Input: Because of the complexity of the assessment of body fat with imaging techniques, great attention has been paid to other measures of adiposity, such as waist circumference (WC), waist-to-hip ratio (WHR) and waist-to-height ratio (WHtR), which provide information on body fat distribution, although BMI is the established clinical measure to estimate the cardiovascular risk disease associated with excessive body weight.


Input: Abdominal obesity is a main predictive factor of the Metabolic Syndrome, so it is certain that it represents a better marker of cardiovascular risk than BMI.


Input: Visceral adiposity index (VAI) has recently proven to be a marker of visceral adipose distribution and function, associated with insulin sensitivity in patients at metabolic risk; however, the evidence needs to be further confirmed.


Input: In summary, BMI, WC, WHR, WHtR and VAI are all useful tools for assessing adiposity/obesity in clinical practice, and should be evaluated along with other cardiometabolic risk factors to define cardiovascular risk stratification.


Input: Unusual glycosaminoglycans from a deep sea hydrothermal bacterium improve fibrillar collagen structuring and fibroblast activities in engineered connective tissues.


Input: Biopolymers produced by marine organisms can offer useful tools for regenerative medicine.


Input: Particularly, HE800 exopolysaccharide (HE800 EPS) secreted by a deep-sea hydrothermal bacterium displays an interesting glycosaminoglycan-like feature resembling hyaluronan.


Input: Previous studies demonstrated its effectiveness to enhance in vivo bone regeneration and to support osteoblastic cell metabolism in culture.


Input: Thus, in order to assess the usefulness of this high-molecular weight polymer in tissue engineering and tissue repair, in vitro reconstructed connective tissues containing HE800 EPS were performed.


Input: We showed that this polysaccharide promotes both collagen structuring and extracellular matrix settle by dermal fibroblasts.


Input: Furthermore, from the native HE800 EPS, a low-molecular weight sulfated derivative (HE800 DROS) displaying chemical analogy with heparan-sulfate, was designed.

sulfated


Input: Thus, it was demonstrated that HE800 DROS mimics some properties of heparan-sulfate, such as promotion of fibroblast proliferation and inhibition of matrix metalloproteinase (MMP) secretion.

sulfate


Input: Therefore, we suggest that the HE800EPS family can be considered as an innovative biotechnological source of glycosaminoglycan-like compounds useful to design biomaterials and drugs for tissue engineering and repair.


Input: Antiprotozoal screening and cytotoxicity of extracts and fractions from the leaves, stem bark and root bark of Alstonia congensis.


Input: ETHNOPHARMACOLOGICAL RELEVANCE: To evaluate the antiprotozoal activity and cytotoxicity of extracts and fractions from the leaves, root bark and stem bark of Alstonia congensis (Apocynaceae), used in traditional medicine against parasitic diseases.


Input: MATERIALS AND METHODS: The aqueous and 80% MeOH extracts, and a series of fractions and subfractions from the leaves, stem and root bark of Alstonia congensis were tested in vitro for their antiprotozoal activity against Trypanosoma brucei brucei, Trypanosoma cruzi, Lesihamania infantum and the chloroquine and pyrimethamine-resitant K1 strain of Plasmodium falciparum.

MeOH

chloroquine

pyrimethamine


Input: Their cytotoxicity on MRC-5 cells (human lung fibroblasts) was evaluated as well.


Input: RESULTS: The aqueous and 80% MeOH extracts and a series of subfractions of each plant part exhibited pronounced antiprotozoal activity against the K1 strain of Plasmodium falciparum with IC50 values ranging from 2 to 5 micro g/ml, and good activity against Trypanosoma brucei brucei and Trypanosoma cruzi with IC50 values ranging between 5 and 10 micro g/ml.

MeOH


Input: The residual 80% MeOH extract from the leaves, and the total alkaloid extract from stem and root bark were the only subfractions active against Leishmania infantum with IC50 values < 10 micro g/ml.

MeOH


Input: None of the samples from the root bark was cytotoxic against MRC-cell lines (CC50 > 64 micro g/ml).


Input: In general, the aqueous extracts (traditional decoctions) showed the highest selectivity, especially against Plasmodium falciparum.


Input: CONCLUSION: These results can partly support and justify the traditional use of these plant parts of Alstonina congensis as raw materials for the preparation of traditional remedies to treat parasitic diseases such as malaria and trypanosomiasis.


Input: Structure of hydrated cobalt ions confined in the nanospace of single-walled carbon nanotubes.

cobalt

carbon


Input: The structure of hydrated Co ions confined in the nanospace of single-walled carbon nanotubes (SWNTs) has been studied using the X-ray absorption fine structure (XAFS) technique.

Co

carbon


Input: Water adsorption isotherms on Co-impregnated SWNTs indicate a high affinity of Co ions to water molecules.

Co

Co


Input: The results of XAFS analysis provided the information on the proportion of dissolved species in nanospaces against the total amount of cobalt ions adsorbed on the open-pored SWNT.

cobalt


Input: The structural information of the first shell around a Co ion was expressed in terms of the hydration number, Co-O distance and Debye-Waller factor.

Co

Co-O


Input: The actual coordination number and the interatomic distance of Co-O for the dissolved species were remarkably reduced compared to the bulk aqueous solution indicating the dehydration of water molecules from Co ions and a compact hydrated structure in the micropore of SWNTs.

Co-O

Co


Input: Comparative phosphoproteomic analysis of checkpoint recovery identifies new regulators of the DNA damage response.


Input: How cells recover from a DNA damage-induced arrest is currently poorly understood.


Input: We performed large-scale quantitative phosphoproteomics to identify changes in protein phosphorylation that occurred during recovery from arrest in the G2 phase of the cell cycle caused by DNA damage.


Input: We identified 154 proteins that were differentially phosphorylated, and systematic depletion of each of these differentially phosphorylated proteins by small interfering RNA (siRNA) identified at least 10 potential regulators of recovery.


Input: Astrin, a protein associated with the mitotic spindle, was among the potential regulators of recovery.

Astrin


Input: We found that astrin controlled the abundance of the cell cycle regulator p53 during DNA damage-induced arrest.


Input: Cells in which astrin was depleted had decreased murine double minute 2 (MDM2) abundance and increased p53 at the later stages of the DNA damage response.

astrin


Input: Astrin was required for continued expression of genes encoding proteins that promote cell cycle progression in arrested cells.

Astrin


Input: Thus, by controlling p53 abundance in cells recovering from DNA damage, astrin maintains the cells in a state competent to resume the cell cycle.


Input: A molecular mechanism for therapeutic effects of cGMP-elevating agents in pulmonary arterial hypertension.

cGMP


Input: Pulmonary arterial hypertension (PAH) 5 is a progressive, usually fatal disease with abnormal vascular remodeling.


Input: Pulmonary artery smooth muscle cells (PASMCs) from PAH patients are hyper-proliferative and apoptosis-resistant, and demonstrate decreased signaling in response to bone morphogenetic proteins (BMPs).


Input: Cyclic GMP-elevating agents are beneficial in PAH, but their mechanism (s) of action are incompletely understood.

Cyclic GMP


Input: Here we show that BMP signaling via Smad1/5/8 requires cGMP-dependent protein kinase isotype I (PKGI) to maintain PASMCs in a differentiated, low-proliferative state.

cGMP


Input: BMP cooperation with cGMP/PKGI was crucial for transcription of contractile genes, and suppression of pro-proliferative and anti-apoptotic genes.

cGMP


Input: Lungs from mice with low or absent PKGI (Prkg1 +/-and Prkg1-/-mice) exhibited impaired BMP signaling, decreased contractile gene expression, and abnormal vascular remodeling.


Input: Conversely, cGMP stimulation of PKGI restored defective BMP signaling in rats with hypoxia-induced PAH, consistent with cGMP-elevating agents reversing vascular remodeling in this PAH model.

cGMP

cGMP


Input: Our results provide a mechanism for the therapeutic effects of cGMP-elevating agents in PAH, and suggest that combining them with BMP mimetics may provide a novel, disease-modifying approach to PAH therapy.

cGMP


Input: The in vivo TRPV6 protein starts at a non-AUG triplet decoded as methionine upstream the canonical initiation at AUG.

methionine


Input: TRPV6 channels function as epithelial Ca2 + entry pathways in the epididymis, prostate and placenta.

Ca2 +


Input: However, like of most proteins the identity of the endogenous TRPV6 protein relies on predicted gene coding regions and is only known to a certain level of approximation.


Input: We show that in vivo the TRPV6 protein has an extended N-terminus.

N


Input: Translation initiates at a non-AUG codon, at ACG, which is decoded by methionine and which is upstream of the annotated AUG which is not used for initiation.

methionine


Input: The in vitro properties of channels formed by the extended full length TRPV6 proteins and the so far annotated and shorter TRPV6 are similar, but the extended N-terminus increases trafficking to the plasma membrane and represents an additional scaffold for channel assembly.

N


Input: The increased translation of the shorter TRPV6 cDNA version may overestimate the in vivo situation where translation efficiency may represent an additional mechanism to tightly control the TRPV6-mediated Ca2 + entry in order to prevent deleterious Ca2 + overload.

Ca2 +

Ca2 +


Input: One-Pot in Situ Mixed Film Formation by Azo Coupling and Diazonium Salt Electrografting.

Azo

Diazonium Salt


Input: So simple: The in situ synthesis of an aryldiazonium salt and an azo-aryldiazonium salt by azo coupling from sulfanilic acid and aniline is reported.

aryldiazonium salt

azo-aryldiazonium salt

azo

sulfanilic acid

aniline


Input: Formation of a mixed organic layer is monitored by cyclic voltammetry and atomic force microscopy.


Input: A compact mixed layer is obtained with a global roughness of 0. 4 nm and 10-15% vertical extension in the range 1. 5-6 nm.


Input: Comparative Study of Metals Accumulation in Cultured In Vitro Mycelium and Naturally Grown Fruiting Bodies of Boletus badius and Cantharellus cibarius.


Input: Cantharellus cibarius Fr.


Input: (chanterelle) and Boletus badius Pers.


Input: (bay bolete) harvested from natural sites in Poland were used to derive in vitro cultures.


Input: The optimal medium composition for cultures was developed.


Input: Concentrations of the chosen elements (Zn, Cu, Fe, Mg, Ni, and Cd) in mycelium samples were measured by means of atomic absorption spectrometry.

Zn

Cu

Fe

Mg

Ni

Cd


Input: Fe concentration in the analyzed mushroom materials was in the range 215. 4-680. 3 mu g/g dry weight.

Fe


Input: Mean values of Mg were respectively (in micrograms per gram dry weight) 541. 8 for mycelium of C. cibarius cultured in vitro and 1, 004. 1 for C. cibarius fruiting bodies and 928. 9 for the mycelium of B. badius cultured in vitro and 906. 4 for B. badius fruiting bodies.

Mg


Input: The mean concentrations of Zn were 442. 7 mu g/g dry weight in mycelium from in vitro cultures of B. badius and 172. 1 in B. badius fruiting bodies and 131. 9 in the case of C. cibarius in mycelium from in vitro cultures and 95. 5 for the C. cibarius fruiting bodies.

Zn


Input: Cu exhibited a reversal tendency, i. e., the element concentrations in naturally grown mushrooms were significantly higher (43. 57 mu g/g dry weight for C. cibarius and 43. 54 mu g/g for B. badius) than in cultured in vitro mycelium (12. 47 mu g/g for C. cibarius and 4. 17 mu g/g for B. badius).

Cu


Input: Ni was found in lowest concentrations ranging from 0. 33 to 1. 88 mu g/g dry weight.

Ni


Input: Toxic metal Cd was found in relatively high concentrations in naturally grown species (0. 79 mu g/g dry weight-1. 02).

Cd


Input: The lowest was the concentration of Cd in C. cibarius mycelium from in vitro culture-0. 06 mu g/g dry weight-a bit higher than it was in the B. badius mycelium (0. 21 mu g/g).

Cd


Input: Biodegradable Polysilsesquioxane Nanoparticles as Efficient Contrast Agents for Magnetic Resonance Imaging.

Polysilsesquioxane


Input: Polysilsesquioxane (PSQ) nanoparticles are crosslinked homopolymers formed by condensation of functionalized trialkoxysilanes, and provide an interesting platform for developing biologically and biomedically relevant nanomaterials.

Polysilsesquioxane

PSQ

trialkoxysilanes


Input: In this work, the design and synthesis of biodegradable PSQ particles with extremely high payloads of paramagnetic Gd (III) centers is explored, for use as efficient contrast agents for magnetic resonance imaging (MRI).

PSQ

Gd (III)


Input: Two new bis (trialkoxysilyl) derivatives of Gd (III) diethylenetriamine pentaacetate (Gd-DTPA) containing disulfide linkages are synthesized and used to form biodegradable Gd-PSQ particles by base-catalyzed condensation reactions in reverse microemulsions.

bis (trialkoxysilyl)

Gd (III) diethylenetriamine pentaacetate

Gd-DTPA

disulfide

Gd-PSQ


Input: The Gd-PSQ particles, PSQ-1 and PSQ-2, carry 53. 8 wt% and 49. 3 wt% of Gd-DTPA derivatives, respectively.

Gd-PSQ

Gd-DTPA


Input: In addition, the surface carboxy groups on the PSQ-2 particles can be modified with polyethylene glycol (PEG) and the anisamide (AA) ligand to enhance biocompatibility and cell uptake, respectively.


Input: The Gd-PSQ particles are readily degradable to release the constituent Gd (III) chelates in the presence of endogenous reducing agents such as cysteine and glutathione.

Gd-PSQ

Gd (III)

cysteine

glutathione


Input: The MR relaxivities of the Gd-PSQ particles are determined using a 3T MR scanner, with r1 values ranging from 5. 9 to 17. 8 mMs (-1) on a per-Gd basis.

Gd-PSQ

Gd


Input: Finally, the high sensitivity of the Gd-PSQ particles as T1-weighted MR contrast agents is demonstrated with in vitro MR imaging of human lung and pancreatic cancer cells.

Gd-PSQ


Input: The enhanced efficiency of the anisamide-functionalized PSQ-2 particles as a contrast agent is corroborated by both confocal laser scanning microscopy imaging and ICP-MS analysis of Gd content in vitro.

anisamide

Gd


Input: Diaion HP-2MG modified with 2-(2, 6-dichlorobenzylideneamino) benzenethiol as new adsorbent for solid phase extraction and flame atomic absorption spectrometric determination of metal ions.

2-(2, 6-dichlorobenzylideneamino) benzenethiol


Input: A solid phase extraction method for enrichment-separation and the determination of cobalt (Co (2 +)), copper (Cu (2 +)), nickel (Ni (2 +)), zinc (Zn (2 +)) and lead (Pb (2 +)) ions in real samples has been proposed.

cobalt

Co (2 +)

copper

Cu (2 +)

nickel

Ni (2 +)

zinc

Zn (2 +)

Pb (2 +)


Input: The influences of some analytical parameters like pH, flow rate, eluent type and interference of matrix ions on recoveries of analytes were optimized.


Input: The limits of detection were found in the range of 1. 6-3. 9 micro g L (-1), while preconcentration factor for all understudy metal ions were found to be 166 with loading half time (t 1/2) less than 10 min.


Input: The procedure was applied for the enrichment-separation of analyte ions in environmental samples with recoveries higher than 94. 8% and relative SD < 4. 9% (N = 5).


Input: Grb10-mediated Negative Regulation of IGF1R-Activated Signalling Pathway Results in Cognitive Disorder in Diabetic Rats.


Input: Growth factor receptor-bound protein 10 (Grb10) is a Src homology 2 (SH2) domain-containing protein and one of the binding partners for several trans-membrane tyrosine-kinase receptors, including insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF1-R).

tyrosine


Input: The hippocampus, which is critical for cognitive functions, is one of the main distribution areas of Grb10 in the central nervous system.


Input: In recent years, diabetic encephalopathy has been defined as a third type of diabetes and the IGF1-IR pathway has been shown to be critical for the neuropathogenic process of cognitive disorder in diabetes.


Input: However, the role of endogenous Grb10 in regulating the IGF1-IR pathway and neurobehavioral changes is not explicit.


Input: The objective of this study was to determine the in vivo function of endogenous Grb10 in diabetic encephalopathy and the underlying mechanisms.


Input: Using stereotaxic surgical techniques and lentiviral vectors expressing specific short hairpin RNA (shRNA), we could steadily knock down Grb10 expression in the hippocampus.


Input: More importantly, we demonstrated that hippocampus-specific modulation of Grb10 protein levels led to a prominent remission of cognitive disorder, including improvements in both ultrastructural pathology and abnormal neurobehavioural changes.


Input: Our findings indicate that endogenous overexpression of Grb10 functions as a suppressor of the IGF1-IR pathway, which may represent an important mechanism that regulates cognitive disorder in diabetes.


Input: This article is protected by copyright.


Input: All rights reserved.


Input: A new ent-kaurane diterpenoid glycoside from Isodon japonica var. glaucocalyx.

ent-kaurane diterpenoid glycoside


Input: A new ent-kaurane diterpenoid glycoside (1), named glaucocalyxin G, has been isolated from the n-butanol-soluble fraction of the dried whole plants of Isodon japonica var. glaucocalyx along with two known compounds, namely arjunglucoside (2) and kaempferol-3-O-rutinoside (3).

ent-kaurane diterpenoid glycoside

glaucocalyxin G

n-butanol

arjunglucoside


Input: The structures of the isolated compounds were assigned on the basis of their (1) H and (13) C NMR spectra including two-dimensional NMR techniques such as HMQC, HMBC, and NOESY experiments and comparison with the literature data.

(1) H

(13) C


Input: Potential role of CYP2D6 in the central nervous system.


Input: Abstract 1.


Input: Cytochrome P450 2D6 (CYP2D6) is a pivotal enzyme responsible for a major drug oxidation polymorphism in human populations.


Input: Distribution of CYP2D6 in brain and its role in serotonin metabolism suggest that CYP2D6 may have a function in the central nervous system.

serotonin


Input: To establish an efficient and accurate platform for the study of CYP2D6 in vivo, a human CYP2D6 (Tg-2D6) model was generated by transgenesis in wild-type (WT) C57BL/6 mice using a P1 phage artificial chromosome clone containing the complete human CYP2D locus, including the CYP2D6 gene and 5'-and 3'-flanking sequences.


Input: Human CYP2D6 was expressed not only in the liver but also in the brain.


Input: The abundance of serotonin and 5-hydroxyindoleacetic acid in brain of Tg-2D6 is higher than in WT mice, either basal levels or after harmaline induction.

serotonin

5-hydroxyindoleacetic acid

harmaline


Input: Metabolomics of brain homogenate and cerebrospinal fluid revealed a significant up-regulation of L-carnitine, acetyl-L-carnitine, pantothenic acid, 2'-deoxycytidine diphosphate (dCDP), anandamide, N-acetylglucosaminylamine and a down-regulation of stearoyl-L-carnitine in Tg-2D6 mice compared with WT mice.

L-carnitine

acetyl-L-carnitine

pantothenic acid

2'-deoxycytidine diphosphate

dCDP

anandamide

N-acetylglucosaminylamine

stearoyl-L-carnitine


Input: Anxiety tests indicate Tg-2D6 mice have a higher capability to adapt to anxiety.


Input: Overall, these findings indicate that the Tg-2D6 mouse model may serve as a valuable in vivo tool to determine CYP2D6-involved neurophysiological metabolism and function.


Input: Two Substrate-Confined Sol-Gel Coassembled Ordered Macroporous Silica Structures with an Open Surface.

Silica


Input: A sol-gel cooperative assembly method was demonstrated for the fabrication of inverse opal films with an open surface.


Input: In this method, a sol-gel silicate precursor was cooperatively assembled into the interstitial spaces of microspheres at the same time when polystyrene templates formed in between two desired substrates.

silicate


Input: Silica inverse opals with a three-dimensional ordered macroporous (3DOM) structure were obtained after selective removing the colloidal templates by calcination.

Silica


Input: The open surfaces with a high degree of interconnected porosity and extremely uniform pore size were characterized by scanning electron microscope (SEM).


Input: Optical transmission spectra reveals the existence of considerable deep band gaps of up to 70% and steep band edges of up to 6%/nm in the [111] directions of the 3DOM silica samples.

silica


Input: A little shrinkage confirmed by transmission spectra is not larger than 3%, in consistent with the results measured by SEM, which revealing the sufficient and compact infiltration into the interstitial spaces by our confined sol-gel coassembly method.


Input: With different incidence angles, the positions of pseudogaps can be easily tuned in the wide range from 720 nm to 887 nm, agreed well with the calculated values by the Bragg law.


Input: All the results prove that the sol-gel coassembly method with two substrates confinement is a simple, low cost, convenient and versatile method for the fabrication of silica inverse opals without overlayers in large domains.

silica


Input: Toxicological impact of inhaled electric mosquito-repellent liquid on the rat: a hematological, cytokine indications, oxidative stress and tumor markers.


Input: Abstract Context: High malaria burden has led to the increased use of insecticides in the tropics and subtropics.


Input: This study thus aimed at assessing the hematological effects alteration of pyrethroid insecticide exposure using the experimental animal model.

pyrethroid


Input: Objective: A commonly available Electric Mosquito-Repellent Liquid pyrethroid insecticide containing prallethrin 1. 6% w/w is widely used for mosquito control in Saudi Arabia.

pyrethroid

prallethrin


Input: The immunotoxic effects after inhalation exposures to the preparation for a continuous period of 24, 48, and 72 h were investigated in rats.


Input: Methods and materials: Rats were exposed to prallethrin 1. 6% w/w by inhalation for 72 consecutive hours.

prallethrin


Input: Total blood count, blood indices of creatine kinase (CK), gamma-glutamyltranspeptidase (gamma-GT), superoxide dismutase (SOD), nitric oxide (NO), malondialdehyde (MDA), interleukin (IL)-2, tumor necrosis factors (TNF) alpha, alpha-fetoprotein (AFP), carbohydrate antigen (CA) 19. 9 and carcinoembrionic antigen (CEA) were assayed.

creatine

superoxide

nitric oxide

NO

malondialdehyde

MDA

carbohydrate


Input: Results: The administration of prallethrin 1. 6% w/w created significant increased changes in the levels of total WBC, lymphocytes, RBC, hemoglobin, packed cell volume, platelets, mean corpuscular volume, and mean corpuscular hemoglobin in rats after 24, 48, and 72 h of continuous inhalation; however, there was a significant reduction in neutrophils at transient reduction in the monocytes after 24 and 48 h to return to normal after 72 h.

prallethrin


Input: Significant increases in the levels of CK, gamma-GT, SOD, NO, MDA, AFP, IL-2, and TNF alpha were recorded.

NO

MDA


Input: CA and CEA did not exhibit any change.


Input: Conclusions: Continuous inhalation to prallethrin 1. 6% insecticides poses toxicity on hematological variables.

prallethrin


Input: It is also concluded that pyrethroid group of insecticide may cause hematological, biochemical, cytokine disturbances and possible mutagenic damage to the tissues.

pyrethroid


Input: Identification of novel Gyrase B inhibitors as potential anti-TB drugs: Homology modeling, hybrid virtual screening and molecular dynamics simulations.


Input: Using an integrated computational approach involving homology modeling, Pharmacophore/Structure-Based virtual screening, molecular dynamics simulations and per-residue energy contribution, ten compounds were proposed as potential TB inhibitors.


Input: Via validated docking calculations, binding free energy calculations showed that the proposed compounds presented better binding affinity with DNA Gyrase B when compared to Novobiocin.

Novobiocin


Input: The compiled in-silico approach employed in this study may serve as a useful tool in the process of the design and development of drugs, not only against TB, but also for a wide range of biological systems.


Input: This article is protected by copyright.


Input: All rights reserved.


Input: Vitamin C forestalls cigarette smoke induced NF-kappa B activation in alveolar epithelial cells.

Vitamin C


Input: Cigarette smoking causes cellular oxidative stress resulting in inflammatory diseases of lung wherein transcription factor NF-kappa B plays an important role.


Input: It is possible that vitamin C, an antioxidant, may prevent cigarette smoke (CS)-induced NF-kappa B activation that involves degradation of I-kappa B epsilon and nuclear translocation of c-Rel/p50 in alveolar epithelial cells.

vitamin C


Input: Therefore, to examine the hypothesis, we verified the effect of vitamin C on CS-induced expression of NF-kappa B driven luciferase reporter and NF-kappa B binding at its target DNA by EMSA in alveolar epithelial A549 cells.

vitamin C


Input: We also examined the level of I-kappa B epsilon and sub-cellular distribution of c-Rel by western blotting and immunofluorescence respectively in CSE-treated A549 cells with or without vitamin C pretreatment.

vitamin C


Input: We observed a significant reduction in CSE induced luciferase expression, NF-kappa B DNA binding, I-kappa B epsilon degradation and c-Rel nuclear translocation in cells pretreated with vitamin C.

vitamin C


Input: To further validate the result, we examined sub-cellular distribution of c-Rel in lungs of CS-exposed guinea pigs treated or untreated with vitamin C.

vitamin C


Input: Result showed that vitamin C treatment resulted in markedly reduced c-Rel nuclear translocation.

vitamin C


Input: All these results demonstrate that vitamin C prevents CS (E)-induced NF-kappa B activation and thus it could be used for the prevention of CS-induced inflammatory diseases.

vitamin C


Input: Screening for polyphenols, antioxidant and antimicrobial activitiesof extracts from eleven Helianthemum taxa (Cistaceae) used in folk medicine in south-eastern Spain.

polyphenols


Input: ETHNOPHARMACOLOGICAL RELEVANCE: The Helianthemum genus contains approximately one hundred taxa.


Input: Some of them are important medicinal plants used in several countries for many different purposes.


Input: However, studies addressing the phytochemistry of many of these species or their biological activities are currently nonexistent.


Input: AIM OF THE STUDY: To perform a comparative analysis of the qualitative composition of secondary metabolites and biological activities of the leaves of the most commonly distributed and used Spanish Helianthemum taxa in order to find a relationship between chemotype, biological activity and uses.


Input: MATERIALS AND METHODS: water and 80% methanolic extracts derived from 11 different Helianthemum taxa were analyzed for their phytochemical composition using standard methods.


Input: Furthermore, HPLC analysis was performed for the estimation of gallic acid, ellagic acid, tannins and flavonols as marker compounds.

gallic acid

ellagic acid

tannins

flavonols


Input: The antioxidant activity was measured by employing the scavenging activity on DPPH (2, 2-diphenyl-1-picrylhydrazyl) and ABTS (2, 2'-azinobis-3-ethylbenzothiazoline-6-sulfonate) radicals.

DPPH

2, 2-diphenyl-1-picrylhydrazyl

ABTS

2, 2'-azinobis-3-ethylbenzothiazoline-6-sulfonate


Input: The 80% methanolic extracts were evaluated for antibacterial (Gram-positive Staphylococcus aureus, Enterococcus faecalis and Listeria monocytogenes and Gram-negative Escherichia coli and Salmonella enterica) activity using the micro dilution technique.


Input: RESULTS: The total polyphenolic content and antioxidant capabilities differed significantly among the Helianthemum leaf extracts.


Input: A strong correlation between total phenolic content, antioxidant properties and antimicrobial activity was found.


Input: The polyphenolic profile was specific for each taxon.


Input: Whereas Helianthemum alypoides, Helianthemum cinereum subsp. rotundifolium, Helianthemum hirtum, Helianthemum asperum, and Helianthemum marifolium subsp. marifolium were characterized by the presence of gallic acid, egallic derivatives and ellagitannins; the polyphenolic profile of Helianthemum apenninum subsp. cavanillesianum, Helianthemum syriacum and Helianthemum polygonoides was mostly based on flavonoids.

gallic acid

egallic

flavonoids


Input: Helianthemum cinereum, Helianthemum alypoides and Helianthemum marifolium consistently presented the strongest radical scavenging activity (in water extracts EC50 ranges from 29. 88 to 38. 1 against DPPH and from 8. 11 to 20. 8 against ABTS, and in 80% MeOH extracts from 25. 3 to 31. 8 against DPPH and from 6. 15 to 8. 6 against ABTS), total phenol content (> 117mg GAE/l) and antimicrobial activities.

DPPH

ABTS

MeOH

DPPH

ABTS


Input: CONCLUSION: The Helianthemum taxa used in folk medicine did not cluster in a unique section, being equally distributed in two out of the four sections analysed.


Input: There was not a clear relationship between the chemotype, based on the polyphenolic composition of the taxa, and their taxonomical classification.


Input: However, the composition of the methanolic and water extracts from the leaves of plants belonging to the Helianthemum genus was strongly related to their medicinal uses.


Input: Caffeic Acid Phenethyl Ester Suppresses Proliferation and Survival of TW2. 6 Human Oral Cancer Cells via Inhibition of Akt Signaling.

Caffeic Acid Phenethyl Ester


Input: Caffeic acid phenethyl ester (CAPE) is a bioactive component extracted from honeybee hive propolis.

Caffeic acid phenethyl ester

CAPE


Input: Our observations indicated that CAPE treatment suppressed cell proliferation and colony formation of TW2. 6 human oral squamous cell carcinoma (OSCC) cells dose-dependently.

CAPE


Input: CAPE treatment decreased G1 phase cell population, increased G2/M phase cell population, and induced apoptosis in TW2. 6 cells.

CAPE


Input: Treatment with CAPE decreased protein abundance of Akt, Akt1, Akt2, Akt3, phospho-Akt Ser473, phospho-Akt Thr 308, GSK3 beta, FOXO1, FOXO3a, phospho-FOXO1 Thr24, phospho-FoxO3a Thr32, NF-kappa B, phospho-NF-kappa B Ser536, Rb, phospho-Rb Ser807/811, Skp2, and cyclin D1, but increased cell cycle inhibitor p27Kip.

CAPE

phospho

phospho

phospho

phospho

phospho

phospho


Input: Overexpression of Akt1 or Akt2 in TW2. 6 cells rescued growth inhibition caused by CAPE treatment.

CAPE


Input: Co-treating TW2. 6 cells with CAPE and 5-fluorouracil, a commonly used chemotherapeutic drug for oral cancers, exhibited additive cell proliferation inhibition.

CAPE


Input: Our study suggested that administration of CAPE is a potential adjuvant therapy for patients with OSCC oral cancer.

CAPE


Input: Assessment of genotoxic effects of flumorph by the comet assay in mice organs.

flumorph


Input: The present study investigated the genotoxic effects of flumorph in various organs (brain, liver, spleen, kidney and sperm) of mice.

flumorph


Input: The DNA damage, measured as comet tail length (micro m), was determined using the alkaline comet assay.


Input: The comet assay is a sensitive assay for the detection of genotoxicity caused by flumorph using mice as a model.

flumorph


Input: Statistically significant increases in comet assay for both dose-dependent and duration-dependent DNA damage were observed in all the organs assessed.


Input: The organs exhibited the maximum DNA damage in 96 h at 54 mg/kg body weight.


Input: Brain showed maximum DNA damage followed by spleen > kidney > liver > sperm.


Input: Our data demonstrated that flumorph had induced systemic genotoxicity in mammals as it caused DNA damage in all tested vital organs, especially in brain and spleen.

flumorph


Input: Role of central metabolism in the osmoadaptation of the halophilic bacterium Chromohalobacter salexigens.


Input: Bacterial osmoadaptation involves the cytoplasmic accumulation of compatible solutes in order to counteract extracellular osmolarity.


Input: The halophilic and highly halotolerant bacterium Chromohalobacter salexigens is able to grow up to 3 M NaCl in a minimal medium due to the de novo synthesis of ectoines.

NaCl

ectoines


Input: This is an osmoregulated pathway that burdens central metabolic routes by quantitatively drawing off TCA cycle intermediaries.

TCA


Input: Consequently, metabolism in C. salexigens has adapted to support this biosynthetic route.


Input: Metabolism of C. salexigens is more efficient at high salinity than at low salinity, as reflected by lower glucose consumption, lower metabolite overflow and higher biomass yield.

glucose


Input: At low salinity, by-products (mainly gluconate, pyruvate and acetate) accumulate extracellularly.

gluconate

pyruvate

acetate


Input: Using [1-13C]-, [2-13C]-, [6-13C]-and [U-13C6]-glucose as carbon sources, we were able to determine the main central metabolic pathways involved in ectoines biosynthesis from glucose.

[1-13C]-, [2-13C]-, [6-13C]-and [U-13C6]-glucose

carbon

ectoines

glucose


Input: C. salexigens uses the Entner-Doudoroff pathway rather than the standard glycolytic pathway for glucose catabolism, and anaplerotic activity is high to replenish the TCA cycle with the intermediaries withdrawn for ectoines biosynthesis.

glucose

TCA

ectoines


Input: Metabolic flux ratios at low and high salinity were similar, revealing a certain metabolic rigidity, probably due to its specialization to support high biosynthetic fluxes and partially explaining why metabolic yields are so highly affected by salinity.


Input: This work represents an im-portant contribution to the elucidation of specific metabolic adaptations in compatible solute accumulating halophilic bacteria.


Input: Selective Bisubstrate Inhibitors with Sub-nanomolar Affinity for Protein Kinase Pim-1.


Input: Potent and selective: The unique nature of the ATP binding pocket structure of Pim family protein kinases (PKs) was used for the development of bisubstrate inhibitors and a fluorescent probe with sub-nanomolar affinity.

ATP


Input: Conjugates of arginine-rich peptides with two ATP mimetic scaffolds were synthesized and tested as inhibitors of Pim-1.

arginine

ATP


Input: Against a panel of 124 protein kinases, a novel ARC-PIM conjugate selectively inhibited PKs of the Pim family.


Input: Side effects associated with psychotropic medications in patients with bipolar disorder: evidence from two independent samples.


Input: Available evidence concerning the side effects experienced by bipolar disorder (BD) patients under naturalistic conditions has been poorly investigated.


Input: The aim of this study was therefore to investigate side effects related to major psychotropic drugs in two independent samples of BD patients naturalistically treated with mood stabilizers, antidepressants, antipsychotics and/or anxiolytics.


Input: Overall, 3654 patients from the Systematic Treatment Enhancement Program for Bipolar Disorder (STEP-BD) sample and 282 patients from the Clinical Outcome and Psycho-Education for Bipolar Disorder (COPE-BD) sample were included.


Input: The primary outcome measure was the influence of each class of psychotropic drugs under investigation on the emergence of any side effect, as measured with the monitoring form in the STEP-BD study and the Udvalg for Kliniske Unders o gelser Side Effect Rating Scale in the COPE-BD study.


Input: Secondary outcome measures included the effects of such drugs on psychic, neurologic, autonomic and other side effects.


Input: Mood stabilizers and antipsychotics were associated with high rates of side effects in both samples.


Input: Furthermore, antipsychotics were specifically associated with psychic side effects, whereas mood stabilizers were specifically associated with neurologic side effects.


Input: Our results largely confirm in a naturalistic setting results previously observed in randomized controlled trials focusing on BD patients.


Input: In Vitro Activity of Paclitaxel-Loaded Polymeric Expansile Nanoparticles in Breast Cancer Cells.

Paclitaxel


Input: Through a series of in vitro studies, the essential steps for intracellular drug delivery of paclitaxel using a pH-responsive nanoparticle system have been investigated in breast cancer cells.

paclitaxel


Input: We successfully encapsulated paclitaxel within polymeric expansile nanoparticles (Pax-eNPs) at 5% loading via a miniemulsion polymerization procedure.

paclitaxel

Pax


Input: Fluorescently tagged eNPs were readily taken up by MDA-MB-231 breast cancer cells grown in culture as confirmed by confocal microscopy and flow cytometry.


Input: The ability of the encapsulated paclitaxel to reach the cytoplasm was also observed using confocal microscopy and fluorescently labeled paclitaxel.

paclitaxel

paclitaxel


Input: Pax-eNPs were shown to be efficacious against three in vitro human breast adenocarcinoma cell lines (MDA-MB-231, MCF-7 and SK-BR-3) as well as cells isolated from the pleural effusions of two different breast cancer patients.

Pax


Input: Lastly, macropinocytosis was identified as the major cellular pathway responsible for eNP uptake, as confirmed using temperature-sensitive metabolic reduction, pharmacologic inhibitors, and fluid-phase marker co-localization.


Input: LiGen: a High Performance workflow for chemistry driven de novo design.


Input: Tools for molecular de novo design are actively sought incorporating sets of chemical rules for fast and efficient identification of structurally new chemotypes endowed with a desired set of biological properties.


Input: In this paper, we present LiGen, a suite of programs which can be used sequentially or as stand-alone tools for specific purposes.


Input: In its standard application, LiGen modules are used to define input constraints, either structure-based, through active site identification, or ligand-based, through pharmacophore definition, to docking and to de novo generation.


Input: Alternatively, individual modules can be combined in a user-defined manner to generate project-centric workflows.