Input: The reaction is followed spectrophotometrically by measuring the change in absorbance (Delta A) at 420 nm using a fixed time method (70 s).


Input: The reaction variables were optimised in order to achieve the highest sensitivity.


Input: The thirty six criterion detection limit was 0. 3 ng/mL, and the relative standard deviation for ten replicate measurements of 30 ng/mL of tartrazine was 0. 98% (n = 10).

tartrazine


Input: The method was successfully applied to the determination of tartrazine in lemon, and papaya-flavoured gelatin, candy, and in fruit syrup.

tartrazine


Input: Root tubers of Lactuca tuberosa as a source of antioxidant phenolic compounds and new furofuran lignans.

phenolic

furofuran lignans


Input: From the root tubers of Lactuca tuberosa, a wild edible plant species, nine phenolic compounds were isolated, including two new furofuran lignan glucosides, named lactuberin A and lactuberin B.

phenolic

furofuran lignan glucosides

lactuberin A

lactuberin B


Input: Their structures were elucidated by spectroscopic methods, especially HRESIMS and 2D NMR techniques.


Input: This is the first time that compounds belonging to the epi series of 2, 6-diaryl-3, 7-dioxabicyclo [3. 3. 0] octane type furofuran lignans have been found in Lactuca species.

2, 6-diaryl-3, 7-dioxabicyclo [3. 3. 0] octane

furofuran lignans


Input: The total phenolic content of the root tuber extract was evaluated and its major phenolic constituents, caffeic acid, chlorogenic acid and 3, 5 dicaffeoylquinic acid, known to possess antioxidant activity, were quantified.

phenolic

caffeic acid

chlorogenic acid

3, 5 dicaffeoylquinic acid


Input: Additionally, the root tuber extract showed DPPH radical scavenging activity implying its potential as functional food.

DPPH


Input: Compositional characterisation of soluble apple polysaccharides, and their antioxidant and hepatoprotective effects on acute CCl4-caused liver damage in mice.


Input: Water-soluble apple peel polysaccharides (APP) and apple flesh polysaccharides (AFP) were isolated from Pink Lady fruits, and their in vitro antioxidant capacities were characterised by DPPH (), HO (), and O (2) (-) systems, and ferric-reducing antioxidant power assay.

DPPH

HO

O (2) (-)

ferric


Input: Oral administration of APP at 250 and 500 mg/kg bw in mice was shown to be as effective as AFP in lowering the CCl (4)-caused increases of serum alanine aminotransferase, aspartate aminotransferase and lactic dehydrogenase activities, and hepatic malondialdehyde level, and antagonising the decreases in antioxidant superoxide dismutase and glutathione peroxidase activities caused by CCl (4) (p < 0. 05).

CCl (4)

alanine

aspartate

malondialdehyde

superoxide

glutathione

CCl (4)


Input: Histopathological examinations further confirmed that both APP and AFP could protect the liver from CCl (4)-induced histological alteration.

CCl (4)


Input: HPLC analysis also showed similar profiles of monosaccharide composition for APP and AFP with arabinose, galactose and galacturonic acid being main component monosaccharides.

arabinose

galactose

galacturonic acid


Input: All of these findings demonstrate that the extracts of both APP and AFP possess antioxidant and hepatoprotective potential.


Input: Modelling the interactions between free phenols, L-ascorbic acid, apple polyphenoloxidase and oxygen during a thermal treatment.

phenols

L-ascorbic acid

oxygen


Input: The kinetics of degradation of chlorogenic acid (CG), (-) epicatechin (EPI), L-ascorbic acid (AA) and polyphenoloxidase (PPO) activity from Marie-M e nard apple in pH 3. 8 solutions at 20 and 50 degrees C were investigated to provide information on the impact of the presence of CG, EPI and/or AA on PPO thermostability.

chlorogenic acid

(-) epicatechin

EPI

L-ascorbic acid

EPI


Input: The effect of the heat treatment on their degradation by enzymatic and/or nonenzymatic ways was also studied.


Input: Stoechiokinetic reactions on the basis of experimental data and literature and determination of the kinetic constants (k) at 20 and 50 degrees C were elaborated before modelling the interaction among reactants, by fitting the reaction curves to predictive model.


Input: Apple PPO was thermolabile, denaturing after 10min at 70 degrees C.


Input: Losses of PPO activity were favoured by the presence of EPI in model solutions, compared with CG, due to the formation of o-quinones of EPI (QEPI) lowering PPO stability.

EPI

o-quinones

EPI


Input: Temperature quickened both enzymatic phenol oxidations before PPO deteriorated and the whole set of the chemical reactions, including the production of secondary oxidation products and CG or EPI regeneration.

phenol

EPI


Input: Results also confirmed that AA in excess induced a fast regeneration of CG and EPI from the corresponding o-quinones formed enzymatically via redox chemical reactions.

EPI

o-quinones


Input: Evaluation of antioxidant activities and chemical characterisation of staghorn sumac fruit (Rhus hirta L.).


Input: Staghorn sumac (Rhus hirta L.) is a native tree in Eastern Canada whose fruit has been used by aboriginal peoples to treat various illnesses, and has recently been found to be a good source of antioxidants.


Input: However, the phytochemical composition of R. hirta is not known.


Input: In this study, we used Four highly accepted assays and confirmed its FRAP, ORAC, beta-CLAMS and PCL values to be 79. 95 mu mol AAE/g DW, 1544 mu mol TE/g DW, RAA 129% and 4513 mu mol TE/g DW, respectively.


Input: The antioxidant activities correlated positively to the total polyphenols content, which was higher in the ethanolic extract (81. 6 mg GAE/g DW) compared to the water extract (46. 3mg GAE/g DW), suggesting polyphenols play an important role.

polyphenols

polyphenols


Input: Quantitative data from UHPLC and qualitative studies using HPLC-DAD-MS showed that in addition to commonly found phenolic acids, flavonoids and anthocyanins, R. hirta fruit contained a novel group of unique anthocyanins with aglycones (anthocyanidins) at 449, 419 and 433 Da.

phenolic acids

flavonoids

anthocyanins

anthocyanins

anthocyanidins


Input: Further studies on the identification and their health beneficial effects are being conducted.


Input: Relationships between the evolution of the percentage in weight of polar compounds and that of the molar percentage of acyl groups of edible oils submitted to frying temperature.

acyl


Input: The evolution of the molar percentage of several kinds of acyl groups of extra virgin olive, sunflower and virgin linseed oils was monitored throughout heating at frying temperature by means of (1) H nuclear magnetic resonance.

acyl

(1) H


Input: Likewise, the evolution of the percentage in weight of the polar compounds of the same oils under the same heating conditions was also determined.


Input: Relationships between both sets of parameters, in each oil and in the oils as a group, were studied.


Input: An equation which is able to accurately predict the percentage in weight of the polar compounds, throughout the heating at frying temperature, of any one of these three oils, from the molar percentage of triunsaturated, diunsaturated and monounsaturated acyl groups, was obtained.

acyl


Input: In this way both molar percentage of acyl groups and percentage in weight of polar compounds can be obtained in a few minutes that registration of the (1) H NMR spectrum of the oil takes, in addition to the rest of information provided by this technique.

acyl

(1) H


Input: The study reveals the close relationships between percentage in weight of polar compounds and the composition expressed in terms of molar percentages of acyl groups in edible oils heated at frying temperature.

acyl


Input: Evaluation of sea bream (Sparus aurata) shelf life using an optoelectronic nose.


Input: A new optoelectronic nose for the shelf-life assessment of fresh sea bream in cold storage has been developed.


Input: The chromogenic array used eight sensing materials (based on aluminium oxide and silica gel) containing pH indicators, Lewis acids and an oxidation-reduction indicator.

aluminium oxide

silica gel

Lewis acids


Input: The colour changes of the sensor array were characteristic of sea bream spoilage.


Input: Colour modulations were measured on day 0 and for the samples held in cold storage for 2, 4, 7, 9 and 11 days.


Input: Determination of moisture content, pH, total volatile basic nitrogen (TVB-N), drip loss, ATP-related compounds and K (1)-value and microbial (mesophilic bacteria and Enterobacteriaceae) analyses were carried out on the same days.

nitrogen

N

ATP


Input: The changes in the chromogenic arrays data were processed by statistical analysis (PCA).


Input: Moreover, PLS statistical studies allowed the creation of models to correlate the chromogenic data with concentrations of mesophilic and Enterobacteriaceae.


Input: The results suggest the feasibility of this system to help develop optoelectronic noses for fish freshness monitoring.


Input: A water-alcohol extract of Citrus grandis whole fruits has beneficial metabolic effects in the obese Zucker rats fed with high fat/high cholesterol diet.

alcohol

cholesterol


Input: Epidemiological studies suggest that citrus fruits and compounds such as flavonoids, limonoids and pectins have health promoting effects.

flavonoids


Input: Our aim was to study the effects of Citrus grandis (L.) Osbeck var. tomentosa hort. fruit extract on the energy metabolism.


Input: A whole fruit powder from dry water and alcohol extracts of C. grandis containing 19% naringin flavonoid was prepared.

alcohol

naringin


Input: The effects of the citrus extract were followed in the obese Zucker rats fed with the HFD.


Input: The circulatory levels of GLP-1 decreased significantly by the extract in comparison to the HFD group, whereas the decreased ghrelin levels were reversed.


Input: The levels of PYY were decreased in all HFD groups.


Input: The leptin amounts decreased but not significantly whereas insulin and amylin were unchanged.


Input: The cholesterol and glucose levels were somewhat but not systematically improved in the HFD fed rats.

cholesterol

glucose


Input: Further studies are needed to identify the active compounds and their mechanisms.


Input: Effect of incorporating hydrothermal, kilned and defatted oats on antioxidant and chapatti making properties of wheat flour.


Input: Oats were subjected to treatments like defatting, hydrothermal cooking and kilning, milled into flour and then the control and treated flours were incorporated into wheat flour at 25% and 50% levels and chapatti making behaviour and antioxidant properties were studied.


Input: The treatments significantly affected the antioxidant properties of oats.


Input: Incorporating oat flours to wheat increased total phenolic content but lowered the antioxidant activity however both were decreased significantly upon baking.


Input: The reducing power of the oat blended flour was higher than the wheat flours and ranged from 8. 0 to 15. 5 mu mol AAE/g and was further increased upon baking.


Input: The metal chelating activity of flour blends varied from 62. 0% to 73. 8% and further increased upon baking.


Input: After baking the total flavonoid content was lowered and ranged from 308 to 389 mu g CE/g.

flavonoid


Input: The non-enzymatic browning index significantly increased up to 27. 6% upon baking.


Input: Piceatannol, a potent bioactive stilbene, as major phenolic component in Rhodomyrtus tomentosa.

Piceatannol

stilbene

phenolic


Input: The sim fruit (Rhodomyrtus tomentosa) has long been used in folk medicine to treat diarrhoea, dysentery, and to boost the immune system.


Input: The purpose of this work was to determine its phenolic profile and to evaluate the changes of content during maturation, as well as the variations induced by environmental conditions.


Input: Using HPLC-ESI-HR-MS, 19 phenolic compounds (PCs) were tentatively characterised and included stilbenes and ellagitannins as major components, followed by anthocyanins, flavonols, and gallic acid.

phenolic

stilbenes

anthocyanins

flavonols

gallic acid


Input: PCs were then further quantified by HPLC-DAD.


Input: Piceatannol, a promising health-promoting stilbene component, was the major PC in the fruit with a concentration of 2. 3mg/g dry weight at full maturity stage.

Piceatannol

stilbene


Input: This concentration is 1000-2000 times higher than that of red grapes, a major source of stilbene in the human diet.

stilbene


Input: During maturation, the contents in piceatannol and other stilbenes, ellagitannins, and flavonols decreased while the anthocyanin content increased.

piceatannol

stilbenes

flavonols

anthocyanin


Input: Shade-grown sim fruits showed significantly higher piceatannol levels than sun-exposed fruits.

piceatannol


Input: Taken together, these findings highlight the potential of sim, an under-utilised plant species from South-East Asia, as a source of health-promoting fruits.


Input: Comparative study on hypocholesterolemic and antioxidant activities of various extracts of fenugreek seeds.


Input: The hypocholesterolemic and antioxidant activities of various extracts (water, methanol, ethyl acetate, hexane, dichloro-methane) of fenugreek seeds were investigated in cholesterol-fed rats.

methanol

ethyl acetate

hexane

dichloro-methane

cholesterol


Input: Only the ethyl acetate extract reduced total cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) and increased high-density lipoprotein cholesterol (HDL-C) compared with those of rats fed a cholesterol-rich diet (HCD).

ethyl acetate

cholesterol

triglycerides

cholesterol

cholesterol

cholesterol


Input: Furthermore, the content of thiobarbituric acid-reactive substances (TBARS), and catalase and superoxide dismutase (SOD) in liver, heart and kidney decreased significantly after oral administration of the ethyl acetate extract, compared with those of HCD-fed rats.

thiobarbituric acid

superoxide

ethyl acetate


Input: The phenolic and flavono i d contents were highest in the methanol and the ethyl acetate extracts.

phenolic

flavono i d

methanol

ethyl acetate


Input: These results showed that the ethyl acetate extract of the fenugreek seeds had a significant hypocholesterolemic effect and antioxidant activity in cholesterol-fed rats, whether this is partly due to the presence of flavono i ds in the extract needs further study.

ethyl acetate

flavono i ds


Input: Structural elucidation and antioxidant activity of a water-soluble polysaccharide from the fruit bodies of Bulgaria inquinans (Fries).


Input: The non-lichenized ascomycete Bulgaria inquinans (Fries), growing in the Changbai Mountain of China, has been used as medicinal diet for many years.


Input: In a previous study, we have reported that a heteropolysaccharide BIWS-4b from the fruit bodies of B. inquinans (Fries) exhibited markedly antimalarial and immunostimulating activities.


Input: In this paper, the structural features and antioxidant activity of BIWS-4b were investigated.


Input: The results showed that BIWS-4b contains an alpha-(1 --> 2), (1 --> 6)-mannan core to which the glucogalactan chains are attached.


Input: The glucogalactan chains were composed of (1 --> 6)-, (1 --> 5)-and (1 --> 5, 6)-linked beta-Galf, (1 --> 4)-linked and non-reducing terminal beta-Glcp units, and might be attached to the mannan core at the O-2 positions of alpha-Manp units.

beta-Galf

beta-Glcp

alpha-Manp


Input: The antioxidant assays showed that BIWS-4b exhibited good activities, including free radicals scavenging effects, ferrous ion-chelating ability and reducing power.

ferrous


Input: Thus, BIWS-4b could be used as a natural antioxidant agent for food and pharmaceutical industries.


Input: Effects of different freezing treatments on the biogenic amine and quality changes of bighead carp (Aristichthys nobilis) heads during ice storage.

amine


Input: The effects of different freezing treatments on the quality changes of bighead carp heads were evaluated in terms of pH value, TBARS, TVB-N, K-value, biogenic amine, total aerobic counts (TACs), drip loss, cooking loss and electrical conductivity (EC) during ice storage.

amine


Input: Fish heads were stored at-40 degrees C (T1),-40 degrees C for 12h and then-18 degrees C (T2),-18 degrees C (T3) for 3months prior to ice storage.


Input: No significant differences were observed among T1, T2 and T3 for drip loss, cooking loss and EC (p > 0. 05).


Input: T2 showed lower TACs, pH value, TBARS and TVB-N than T3 did.


Input: Significant lower value of spermine and spermidine were observed in T1, T2 and T3 than those of control group (fresh) from 9th to 18th day (p < 0. 05).

spermine

spermidine


Input: Drip loss was significantly correlated with TBARS, pH value, TVB-N, and TACs in groups T1, T2 and T3 (p < 0. 05).


Input: Isomerisation of carrot beta-carotene in presence of oil during thermal and combined thermal/high pressure processing.

beta-carotene


Input: The effect of thermal processing (85-130 degrees C) and combined thermal/high pressure processing (100 degrees C combined with 0. 1 to 700 MPa and 700 MPa combined with 85-115 degrees C) on beta-carotene isomerisation in an olive oil/carrot emulsion and pure olive oil phase enriched with carrot beta-carotene was investigated.

beta-carotene

beta-carotene


Input: Thermal processing always resulted in an increase in the contribution of the cis-isomers, with the increase being more pronounced at higher temperatures.


Input: In the oil/carrot emulsion, less beta-carotene isomerisation was observed during combined thermal/high pressure processing compared to thermal processing.

beta-carotene


Input: This effect was attributed to strengthening of the carrot cell walls under high pressure, thereby hindering the transfer of beta-carotene to the oil phase and lowering its susceptibility to isomerisation.

beta-carotene


Input: In an oil phase enriched with beta-carotene, beta-carotene isomerisation was not influenced by the applied pressure at 100 degrees C and became almost temperature insensitive at 700 MPa.

beta-carotene

beta-carotene


Input: Inhibitory activity of Filipendula ulmaria constituents on recombinant human histidine decarboxylase.

histidine


Input: Histidine decarboxylase (HDC) catalyses the formation of histamine, a bioactive amine.

Histidine

histamine

amine


Input: Agents that control HDC activity are beneficial for treating histamine-mediated symptoms, such as allergies and stomach ulceration.

histamine


Input: We searched for inhibitors of HDC from the ethyl acetate extract of the petal of Filipendula ulmaria, also called meadowsweet.

ethyl acetate


Input: Rugosin D, rugosin A, rugosin A methyl ester (a novel compound), and tellimagrandin II were the main components; these 4 ellagitannins exhibited a non-competitive type of inhibition, with K (i) values of approximately 0. 35-1 mu M.

Rugosin D

rugosin A

rugosin A methyl ester

tellimagrandin II


Input: These K (i) values are nearly equal to that of histidine methyl ester (K (i) = 0. 46 mu M), an existing substrate analogue inhibitor.

histidine methyl ester


Input: Our results show that food products contain potent HDC inhibitors and that these active food constituents might be useful for designing clinically available HDC inhibitors.


Input: Antioxidant properties of different edible mushroom species and increased bioconversion efficiency of Pleurotus eryngii using locally available casing materials.


Input: Total phenolics, radical scavenging activity (RSA) on DPPH, ascorbic acid content and chelating activity on Fe (2 +) of Pleurotus citrinopileatus, Pleurotus djamor, Pleurotus eryngii, Pleurotus flabellatus, Pleurotus florida, Pleurotus ostreatus, Pleurotus sajor-caju and Hypsizygus ulmarius have been evaluated.

phenolics

DPPH

ascorbic acid

Fe (2 +)


Input: The assayed mushrooms contained 3. 94-21. 67 mg TAE of phenolics, 13. 63-69. 67% DPPH scavenging activity, 3. 76-6. 76 mg ascorbic acid and 60. 25-82. 7% chelating activity.

phenolics

DPPH

ascorbic acid


Input: Principal Component Analysis (PCA) revealed that significantly higher total phenolics, RSA on DPPH and growth/day was present in P. eryngii whereas P. citrinopileatus showed higher ascorbic acid and chelating activity.

phenolics

DPPH

ascorbic acid


Input: Agglomerative hierarchical clustering analysis revealed that studied mushroom species fall into two clusters; Cluster I included P. djamor, P. eryngii and P. flabellatus, while Cluster II included H. ulmarius, P. sajor-caju, P. citrinopileatus, P. ostreatus and P. florida.


Input: Enhanced yield of P. eryngii was achieved on spent compost casing material.


Input: Use of casing materials enhanced yield by 21-107% over non-cased substrate.


Input: Interaction between lysozyme and procyanidin: multilevel structural nature and effect of carbohydrates.

procyanidin

carbohydrates


Input: The interaction of procyanidins with proteins has aroused extensive attention due to its important relationship with the bioavailability and astringent property of polyphenols.

procyanidins

polyphenols


Input: In the present work, we have investigated the interactions of lysozyme with procyanidin dimer (B3) using various biophysical approaches, which aims to provide insights into the mechanism of protein/polyphenol aggregation.

procyanidin

polyphenol


Input: Procyanidin B3 spontaneously binds lysozyme, inducing the multilevel structural changes in lysozyme and the formation of insoluble complexes.

Procyanidin B3


Input: The relationship between lysozyme aggregation and the loss of enzymatic activity was monitored using dynamic light scattering and fluorescence quenching.


Input: The influences of two carbohydrates (gum arabic and sucrose) on lysozyme/B3 aggregation were also studied.

carbohydrates

sucrose


Input: Gum arabic effectively inhibited the formation of insoluble aggregates, but was unable to restore the fluorescence and activity of lysozyme.


Input: However, sucrose concomitantly decreased the aggregate size with the recovery of fluorescence and lysozyme activity.


Input: These results proposed two probable mechanisms by which these two carbohydrates inhibit protein/polyphenol aggregation.

carbohydrates

polyphenol


Input: The protein interactions and rheological properties of skim milk heated in the presence of low levels of reducing agent.


Input: Skim milk with low levels of added beta-mercaptoethanol (SM-ME) and untreated skim milk (SM) were heated and then made into acid gels.

beta-mercaptoethanol


Input: Acid gels prepared from heated SM-ME had markedly higher firmness and contained more protein connections than acid gels prepared from heated SM.


Input: Electrophoretic analyses of the milks showed that the levels of beta-lactoglobulin and alpha-lactalbumin associated with the casein micelles increased with increasing beta-ME concentration.


Input: The levels of disulphide-linked whey proteins were higher in SM-ME than in SM.

disulphide


Input: This suggested that there may be higher levels of initiators for thiol-disulphide exchange reactions, resulting in an increase in the rate of the reactions and the formation of greater numbers of small aggregates, in SM-ME than in SM.

thiol

disulphide


Input: Consequently, acid gels made from SM-ME may have more bonds and more particles participating in the network, resulting in firmer gels, than acid gels made from SM.


Input: A novel colloidal gold-based lateral flow immunoassay for rapid simultaneous detection of cyromazine and melamine in foods of animal origin.

cyromazine

melamine


Input: A rapid and sensitive lateral flow immunoassay (LFIA) based on competitive format was developed and validated for simultaneous detection of cyromazine (CA) and melamine (MA) in foods of animal origin.

cyromazine

melamine


Input: With this method, the cut-off value for the two test lines were achieved at 25 ng/g, which was lower than the maximum residue levels (MRLs) established for CA and MA.


Input: At three fortified levels (50, 100, and 150 ng/g), the recoveries for CA and MA ranged from 73. 9% to 104. 2% with the relative standard deviation (RSD) less than 11. 9%, based on within day and interday analysis.


Input: The lower detection limit for CA and MA in matrix sample were 0. 22 ng/ml and 0. 26 ng/ml, respectively, which were lower than those of published literatures.


Input: A parallel analysis of CA and MA in real samples conducted by HPLC showed comparable results to those obtained from LFIA.


Input: The results of LFIA were in good agreement with those of high performance liquid chromatography (HPLC) in the analysis of CA and MA in foods of animal origin, demonstrating the practical applicability of the developed assay in real samples.


Input: Overall, to our knowledge, this is the first report of quantitative or semi-quantitative simultaneous detection for CA and MA by immunochromatographic assay.


Input: Total amino acid profiles of heat-processed fresh Elaeis guineensis and Raphia hookeri wines.

amino acid


Input: Total amino acid (AA) profiles of heat-processed fresh Elaeis guineensis and Raphia hookeri wines were studied.

amino acid


Input: Heating their fresh wines to 85 degrees C, cooling and diluting to original volumes distilled off ethanol, but did not change their moisture and nitrogen contents.

ethanol

nitrogen


Input: R. hookeri wine contained more (p < 0. 05) Phe, Val, Ala, Gly, Pro, Asp, Asn, His and Lys than E. guineensis wine which contained more (p < 0. 05) Met, Cys, Glu, Gln, Ser and Arg.

Phe

Val

Ala

Gly

Pro

Asp

Asn

His

Lys

Met

Cys

Glu

Gln

Ser

Arg


Input: Tyrosine, Leu, Ile and Thr contents did not vary (p > 0. 05).

Tyrosine

Leu

Ile

Thr


Input: Glycine and Pro contents were low suggesting high globular protein concentrations.

Glycine

Pro


Input: sum basic AA/sum acidic AA ratios were > 1 suggesting high basic protein contents.


Input: The E. guineensis and R. hookeri wines contained 58. 25 +/- 0. 56% and 56. 79 +/- 0. 4% essential AAs, respectively.

AAs


Input: Essential AA scores suggested Leu as their limiting AA.

Leu


Input: In conclusion, the wines can adequately meet daily nitrogen and essential AA needs when a 70 kg adult drinks 1425. 45 ml.

nitrogen


Input: Quality and antioxidant properties of breads enriched with dry onion (Allium cepa L.) skin.


Input: The aim of the study was to investigate the effect on the antioxidant properties and sensory value of bread of adding ground onion skin (OS).


Input: For a determination of bioaccessibility and bioavailability in vitro the human gastrointestinal tract model was used.


Input: OS contained mastication-extractable quercetin (4. 6 mg/g).

quercetin


Input: Quercetin from OS was highly bioaccessible during in vitro conditions, but only approximately 4% of quercetin released during simulated digestion was bioavailable in vitro.

Quercetin

quercetin


Input: The antioxidant potential of bread with OS was significantly higher than the activity noted in the control.


Input: In particular, OS addition significantly fortificated bread with bioaccessible lipid oxidation preventers and compounds with reducing and chelating abilities.


Input: The 2-3% OS addition caused significant improvement of antioxidant abilities (further increases in the OS supplement did not increase the activity of bread).


Input: Sensory evaluation showed that replacement of wheat flour in bread with up to 3% OS powder gave satisfactory consumer acceptability.


Input: Determination of total iron in food samples after flow injection preconcentration on polyurethane foam functionalized with N, N-bis (salicylidene)-1, 3-propanediamine.

iron

polyurethane

N, N-bis (salicylidene)-1, 3-propanediamine


Input: A highly selective flow injection sorption system was developed for the fast determination of total iron in food samples.

iron


Input: Iron (III) was reduced to iron (II) by ascorbic acid and preconcentrated on a mini-column packed with polyurethane foam (PUF) functionalized with N, N-bis (salicylidene)-1, 3-propanediamine (SPDA).

Iron (III)

iron (II)

ascorbic acid

polyurethane

N, N-bis (salicylidene)-1, 3-propanediamine

SPDA


Input: The retained Fe (II) was eluted with hydrochloric acid and subsequently reacted to 2, 4, 6-tri (2'-pyridyl)-1, 3, 5-triazine (TPTZ) then measured at 593 nm.

Fe (II)

hydrochloric acid

2, 4, 6-tri (2'-pyridyl)-1, 3, 5-triazine

TPTZ


Input: The procedure has resulted preconcentration factor 36, sample frequency 20 h (-1) and detection limit 18 mu g L (-1).


Input: The precision (RSD) was found to be 5. 7% and 3. 1% at concentration levels 0. 1 and 5. 0 mu g mL (-1) iron (II), respectively.

iron (II)


Input: Finally, the method was successfully applied to determination of total iron in reference material and food samples.

iron


Input: Effects of blanching on polyphenol stability of innovative paste-like parsley (Petroselinum crispum (Mill.) Nym ex A. W. Hill) and marjoram (Origanum majorana L.) products.

polyphenol


Input: Fresh herbs were water-and steam-blanched at 90-100 degrees C and 100 degrees C, respectively, for 1-10 min and 30 s to 7 min for parsley and marjoram, respectively, and subsequently minced to obtain a paste.


Input: For the first time, phenolic compounds of unheated marjoram were characterised by high-performance liquid chromatography coupled to mass spectrometry (HPLC-MS).

phenolic


Input: Hereby, 10 phenolics were detected.

phenolics


Input: Among them, apigenin-glucuronide, lucenin-2 and lithospermic acid were tentatively identified for the first time.

apigenin-glucuronide

lithospermic acid


Input: In unheated parsley, apart from the major compound apiin, 10 further phenolics were characterised including several p-coumaric acid derivatives which were newly detected.

apiin

phenolics

p-coumaric acid


Input: Except for apiin, short-time steam-and water-blanching (1 min), respectively, did not cause significant losses of phenolic compounds, and thus proved to be the most suitable measures to ensure polyphenol retention.

apiin

phenolic

polyphenol


Input: Consequently, blanching is a recommendable initial operation in the processing of parsley and marjoram into novel paste-like products.


Input: Phenolic compounds and antioxidant activities of selected species of seaweeds from Danish coast.

Phenolic


Input: Water and ethanolic extracts of 16 species of seaweeds collected along the Danish coasts were screened for antioxidant activities using four in vitro antioxidant assays (2, 2-diphenyl-1-picrylhydrazyl radical scavenging activity, reducing power, ferrous ion-chelating and liposome model system).

2, 2-diphenyl-1-picrylhydrazyl

ferrous


Input: Furthermore their effectiveness in retarding lipid peroxidation in fish oil was evaluated by an accelerated stability test.


Input: Significant differences were observed in total and individual phenolic content and the antioxidant activities of seaweed species evaluated.


Input: Ethanol was more efficient for polyphenol extraction than water.

Ethanol

polyphenol


Input: Polysiphonia fucoides and all the Fucus species tested showed highest radical scavenging activity, reducing power, inhibition of oxidation in liposome model system and in fish oil and were high in phenolic content.


Input: These seaweeds could be potential rich sources of natural antioxidants for protection of foods against oxidation.


Input: In general, the various antioxidative assays correlated well with the total phenolic content, indicating that algal polyphenols are active components in these extracts.

polyphenols


Input: However, in some of the antioxidative assays some species with low total phenolic content also showed good antioxidative effects indicating that some other co-extracted active compounds such as pigments and tocopherols in ethanolic extracts and sulphated polysaccharides, proteins or peptides in water extracts may also contribute to the overall antioxidant properties and this needs further investigation.

tocopherols


Input: Relationships between harvest time and wine composition in Vitis vinifera L.


Input: cv.


Input: Cabernet Sauvignon 1.


Input: Grape and wine chemistry.


Input: The study aimed to quantify the effects of grape maturity on wine alcohol, phenolics, flavour compounds and polysaccharides in Vitis vinifera L.

phenolics


Input: cv Cabernet Sauvignon.


Input: Grapes were harvested at juice soluble solids from 20 to 26 degrees Brix which corresponded to a range of wine ethanol concentrations between 12% and 15. 5%.

ethanol


Input: Grape anthocyanin and skin tannin concentration increased as ripening progressed, while seed tannin declined.

anthocyanin

tannin

tannin


Input: In the corresponding wines, monomeric anthocyanin and wine tannin concentration increased with harvest date, consistent with an enhanced extraction of skin-derived phenolics.

anthocyanin

tannin

phenolics


Input: In wines, there was an observed increase in yeast-derived metabolites, including volatile esters, dimethyl sulfide, glycerol and mannoproteins with harvest date.

esters

dimethyl sulfide

glycerol


Input: Wine volatiles which were significantly influenced by harvest date were isobutyl methoxypyrazine, C (6) alcohols and hexyl acetate, all of which decreased as ripening progressed.

isobutyl methoxypyrazine

alcohols

hexyl acetate


Input: The implications of harvest date for wine composition is discussed in terms of both grape composition and yeast metabolism.


Input: D/H exchange in C-H bonds of fatty acids: implication for geographical discrimination of food materials.

D

H

C-H

fatty acids


Input: The stable isotope analysis of non-exchangeable hydrogen in food materials has been believed as a powerful tool for tracing geographical origins and delivery of the materials.

hydrogen


Input: However, little information is available for the D/H exchanges even in hydrophobic molecules, which leads to potential uncertainty on the observed results.

D

H


Input: To further evaluate the reliability of hydrogen isotopes of organic molecules, we examined the isotope exchangeability in fatty acids within phospholipid bilayers exposed to D (2) O for 12h.

hydrogen

fatty acids

D (2) O


Input: The results indicate that the isotope ratio is clearly increased during all examines (e. g., 93-328 /1000 in 50% D (2) O), in which its magnitude depends on type of fatty acids and state of bilayers.

D (2) O

fatty acids


Input: However, these results also indicate very clearly that the observed exchange rate is negligible if samples are exposed to natural abundance of deuterium (0. 0156%) in natural and laboratory environments before/during analysis.

deuterium


Input: The potential to intensify sulforaphane formation in cooked broccoli (Brassica oleracea var. italica) using mustard seeds (Sinapis alba).

sulforaphane


Input: Sulforaphane, a naturally occurring cancer chemopreventive, is the hydrolysis product of glucoraphanin, the main glucosinolate in broccoli.

Sulforaphane

glucoraphanin

glucosinolate


Input: The hydrolysis requires myrosinase isoenzyme to be present in sufficient activity; however, processing leads to its denaturation and hence reduced hydrolysis.


Input: In this study, the effect of adding mustard seeds, which contain a more resilient isoform of myrosinase, to processed broccoli was investigated with a view to intensify the formation of sulforaphane.

sulforaphane


Input: Thermal inactivation of myrosinase from both broccoli and mustard seeds was studied.


Input: Thermal degradation of broccoli glucoraphanin was investigated in addition to the effects of thermal processing on the formation of sulforaphane and sulforaphane nitrile.

glucoraphanin

sulforaphane

sulforaphane nitrile


Input: Limited thermal degradation of glucoraphanin (less than 12%) was observed when broccoli was placed in vacuum sealed bag (sous vide) and cooked in a water bath at 100 degrees C for 8 and 12 min.

glucoraphanin


Input: Boiling broccoli in water prevented the formation of any significant levels of sulforaphane due to inactivated myrosinase.

sulforaphane


Input: However, addition of powdered mustard seeds to the heat processed broccoli significantly increased the formation of sulforaphane.

sulforaphane


Input: Effect of thermal heating on some lignans in flax seeds, sesame seeds and rye.

lignans


Input: Consumption of lignan rich food is presumed to have positive effects on human health.

lignan


Input: As numerous foods are consumed mainly in processed form it is important to investigate the changes of the lignan content during processing.

lignan


Input: To this end, unheated and heated sesame seeds, sesame products, rye grains, rye flour, rye bread and flax seeds were extracted by sonication with ethanol/water (70: 30, v: v) or sodium methoxide.

ethanol

sodium methoxide


Input: The extracts were additionally hydrolysed enzymatically (beta-glucuronidase/arylsulphatase, cellulase), the compounds separated on a reversed phase column by gradient elution and detected by UV/ESI-MS in the negative ionisation multiple reaction monitoring mode (MRM).


Input: Secoisolariciresinol, lariciresinol, pinoresinol, 7-hydroxymatairesinol, syringaresinol, isolariciresinol, secoisolariciresinol diglycoside, lariciresinol monoglycoside, pinoresinol mono-, di-and triglycoside, sesaminol, sesaminol triglycoside, sesamolinol and sesamolinol diglycoside were identified.

Secoisolariciresinol

lariciresinol

pinoresinol

syringaresinol

isolariciresinol

secoisolariciresinol diglycoside

lariciresinol monoglycoside

pinoresinol mono-, di-and triglycoside

sesaminol

sesaminol triglycoside

sesamolinol

sesamolinol diglycoside


Input: Moderate heating at 100 degrees C did not degrade the lignan aglycones and glycosides in dry foods.


Input: In contrast, heating was responsible for the better extractability of the lignans.

lignans


Input: If samples with high moisture content were heated, the degradation of the lignans in sesame seeds and rye was observed already at 100 degrees C.

lignans


Input: Higher roasting temperatures caused degradation of aglycones and glycosides.


Input: Especially at 250 degrees C, lignans were degraded rapidly in sesame seeds and rye but not in flax seeds.


Input: Dung-shen (Codonopsis pilosula) attenuated the cardiac-impaired insulin-like growth factor II receptor pathway on myocardial cells.


Input: Previous studies from our lab showed that increase in AngII in H9c2 cells causes elevated IGFII and IGFIIR through MEK and JNK, leading to rise in intracellular calcium, calcineurin activation by PLC-beta 3 via G alpha q, insertion into mitochondrial membranes of Bad, and apoptosis via caspases 9 and 3.

calcium


Input: Codonopsis pilosula is traditionally used to lower blood pressure.


Input: The purpose of our study is to investigate if C. pilosula attenuates AngII plus Leu (27)-IGFII-induced calcium influx and apoptosis in H9c2 cardiomyoblasts.

Leu

calcium


Input: C. pilosula significantly attenuated AngII induced IGFIIR promoter activity.


Input: Leu (27)-IGFII was applied to enhance the AngII effect.

Leu


Input: C. pilosula also reversed Ca (2 +) influx, MOMP and apoptosis increased by AngII plus Leu (27)-IGFII.

Ca (2 +)

Leu


Input: Molecular markers in IGFIIR apoptotic pathway (IGFIIR, calcineurin, etc.) and IGFIIR-G alpha q association were downregulated by C. pilosula.


Input: However, p-Bad (Ser136) and Bcl-2 were increased.


Input: Therefore, C. pilosula suppresses AngII plus Leu (27)-IGFII-induced IGFII/IGFIIR pathway in myocardial cells.

Leu


Input: Characterization and identification of gamma-irradiated sauces by electron spin resonance spectroscopy using different sample pretreatments.


Input: Tomato ketchup, barbeque sauce, sweet chili sauce, and spaghetti sauce were gamma irradiated at 0, 1, 5, and 10 kGy.


Input: Electron spin resonance (ESR) technique was used to characterize the irradiated sauces, targeting radiation-induced cellulose radicals and using a modified sample pretreatment method.


Input: The samples were first washed with water, and then the residues were extracted with alcohol.

alcohol


Input: The non-irradiated sauces exhibited the single central signal, whose intensity showed a significant increase on irradiation.


Input: The ESR spectra from the radiation-induced cellulose radicals, with two side peaks (g = 2. 02012 and g = 1. 98516) equally spaced (+/- 3 mT) from the central signal, were also observed in the irradiated sauces.


Input: The improvements in the central (natural) and radiation-induced (two side peaks corresponding to the cellulose radicals) signal intensities were obvious, when compared with routine freeze-drying and alcoholic-extraction techniques.


Input: Near infrared reflectance spectroscopy for determination of the geographical origin of wheat.


Input: The feasibility of using near infrared reflectance (NIR) spectroscopy combined with chemometrics was investigated to discriminate wheat geographical origins.


Input: A total of 240 wheat samples from two growing years from four major wheat producing regions in China were analyzed.


Input: After spectral data pre-treatment to wheat kernel and whole wheat flour, linear discriminant analysis (LDA) based on principal component scores and discriminant partial least squares analysis (DPLS) were applied to classify origins of samples excluding water spectrum.


Input: The results showed that there were significant differences among wheat NIR spectra from different regions.


Input: Wheat could be classified based on geographical origins with chemometrics.


Input: DPLS were better than LDA for wheat origin determination.


Input: In conclusion, NIRS combined with chemometrics is a promising method for identifying wheat according to geographical origin, but the effectiveness should be verified further.


Input: Determination of tartrazine in beverage samples by stopped-flow analysis and three-way multivariate calibration of non-linear kinetic-spectrophotometric data.

tartrazine


Input: The performance of MCR-ALS was studied in the modeling of non-linear kinetic-spectrophotometric data acquired by a stopped-flow system for the quantitation of tartrazine in the presence of brilliant blue and sunset yellow FCF as possible interferents.

tartrazine

brilliant blue and sunset yellow FCF


Input: In the present work, MCR-ALS and U-PCA/RBL were firstly applied to remove the contribution of unexpected components not included in the calibration set.


Input: Secondly, a polynomial function was used to model the non-linear data obtained by the implementation of the algorithms.


Input: MCR-ALS was the only strategy that allowed the determination of tartrazine in test samples accurately.

tartrazine


Input: Therefore, it was applied for the analysis of tartrazine in beverage samples with minimum sample preparation and short analysis time.

tartrazine


Input: The proposed method was validated by comparison with a chromatographic procedure published in the literature.


Input: Mean recovery values between 98% and 100% and relative errors of prediction values between 4% and 9% were indicative of the good performance of the method.


Input: Effect of ferrous sulfate fortification in germinated brown rice on seed iron concentration and bioavailability.

ferrous sulfate

iron


Input: The present study evaluated the effectiveness of germination and iron fortification on iron concentration and bioavailability of brown rice.

iron

iron


Input: Iron fortification during germination process with 0. 05-2 g/L ferrous sulfate increased the iron concentration in germinated brown rice from 1. 1 to 15. 6 times than those in raw brown rice.

Iron

ferrous sulfate

iron


Input: Based on the recommended dietary allowance of iron, maximum germination rate and gamma-aminobutyric acid, we recommend the brown rice fortified with 0. 25 g/L FeSO (4) as a suitable fortification level to use in germination process.

iron

gamma-aminobutyric acid

FeSO (4)


Input: Iron fortification during the germination process has a positive effect on iron concentration and bioavailability.

Iron

iron


Input: A significant difference was observed among the cultivars in respect to the capacity for iron accumulation and bioavailability.

iron


Input: Germination alone could improve in vitro iron solubility, but had no effect on iron bioavailability in Caco-2 cell, the additional fortification process should be combined to get high amount of bioavailable iron from the brown rice.

iron

iron

iron


Input: Apoptosis of human breast cancer cells induced by microencapsulated betulinic acid from sour jujube fruits through the mitochondria transduction pathway.

betulinic acid


Input: Betulinic acid (BA), a natural pentacyclic triterpenoid, was isolated from sour jujube fruits for the first time.

Betulinic acid

pentacyclic triterpenoid


Input: An inclusion complex comprising BA and beta-cyclodextrin (beta-CD) was formed to improve the dissolution of BA, but little is known about its anticancer effect.

beta-cyclodextrin

beta-CD


Input: In this study, the anti-proliferative and apoptosis mechanisms of BA-beta-CD on human breast cancer MCF-7 cells were further investigated.

BA-beta-CD


Input: Experimental results confirmed that the complexation model inhibited the growth of MCF-7 cells in a dose-dependent manner, arrested cell cycle in the G2/M phase and induced apoptosis via the mitochondria transduction pathway.


Input: Gene and protein analyses showed that the complexation model significantly inhibited Bcl-2 expression and promoted Bax expression, causing caspase-3 and caspase-9 cascade activation.


Input: These findings corroborated evidence on microencapsulated BA as an apoptosis inducer in MCF-7 cells.


Input: Thus, sour jujube fruits may have potential use as a breast cancer chemotherapeutic agent.


Input: Transglycosylation of stevioside to improve the edulcorant quality by lower substitution using cornstarch hydrolyzate and CGTase.

stevioside


Input: Stevioside is an abundant sweetener extracted from Stevia rebaudiana leaf with a bitter aftertaste.

Stevioside


Input: Enzymatic transglycosylation of stevioside is a solution to improve the edulcorant quality of stevioside, but highly derivatised stevioside coming with high conversion of stevioside is undesired.

stevioside

stevioside

stevioside

stevioside


Input: In this experiment, the transglycosylation of stevioside was investigated by using a commercial cyclodextrin glucanotransferase and cornstarch hydrolyzate.

stevioside


Input: With controlled parameters, the product was mainly composed of mono-and di-glucosylated stevioside while the highest stevioside conversion reached 77. 11%.

mono-and di-glucosylated stevioside

stevioside


Input: Neither kinetic nor thermodynamic factor stimulated the formation of high substituted steviosides.

steviosides


Input: The simultaneous hydrolysis in the reaction might inhibit the yield of highly substituted steviosides.

steviosides


Input: Effects of oil exposure and dispersant use upon environmental adaptation performance and fitness in the European sea bass, Dicentrarchus labrax.


Input: The worldwide increasing recourse to chemical dispersants to deal with oil spills in marine coastal ecosystems is a controversial issue.


Input: Yet, there exists no adequate methodology that can provide reliable predictions of how oil and dispersant-treated oil can affect relevant organism or population-level performance.


Input: The primary objective of the present study was to examine and compare the effects of exposure to untreated oil (weathered Arabian light crude oil), chemically dispersed oil (Finasol, TOTAL-Fluides) or dispersant alone, upon the ability of fish for environmental adaptation.


Input: To reach that goal, we implemented high-throughput, non-lethal challenge tests to estimate individual hypoxia and heat tolerance as surrogate measures of their capacity to face natural contingencies.


Input: Experimental populations were then transferred into semi-natural tidal ponds and correlates of individuals' fitness (growth and survival) were monitored over a period of 6 months.


Input: In accordance with our stated objectives, the contamination conditions tested corresponded to those observed under an oil slick drifting in shallow waters.


Input: Our results revealed that the response of control fish to both challenges was variable among individuals and temporally stable (repeatable) over a 2-month period.


Input: Exposure to chemical dispersant did not affect the repeatability of fish performance.


Input: However, exposure to oil or to a mixture of oil plus dispersant affected the repeatability of individuals' responses to the experimental challenge tests.


Input: At population level, no difference between contamination treatments was observed in the distribution of individual responses to the hypoxia and temperature challenge tests.


Input: Moreover, no correlation between hypoxia tolerance and heat tolerance was noticed.


Input: During the field experiment, hypoxia tolerance and heat tolerance were found to be determinants of survivorship.


Input: Moreover, experimental groups exposed to oil or to dispersant-treated oil displayed significantly lower survival than control or dispersant-exposed groups.


Input: Finally, from the four experimental populations tested, the one exposed to chemically dispersed oil presented the lowest growth rate.


Input: High serum vitamin D levels reduce the risk for nonalcoholic fatty liver disease in healthy men independent of metabolic syndrome.

vitamin D


Input: Recent studies suggest an association of vitamin D with obesity, diabetes and cardiovascular diseases.

vitamin D


Input: We analyzed the association of serum vitamin D level assessed by 25-hydroxyvitamin D (3) {25 (OH) D (3)} with nonalcoholic fatty liver disease (NAFLD) in apparently healthy men.

vitamin D

25-hydroxyvitamin D (3)

25 (OH) D (3)


Input: We performed a cross-sectional study of 6, 567 Korean men who participated in a health screening program, evaluating the association of serum 25 (OH) D (3) levels with the risk of NAFLD assessed by abdominal ultrasonogram.

25 (OH) D (3)


Input: Of the participants, 43. 6% had NAFLD and 21. 1% had metabolic syndrome.


Input: Age, serum calcium, and aspartate aminotransferase levels showed weak but significant positive correlations with 25 (OH) D (3) level; total cholesterol, triglycerides, low-density lipoprotein cholesterol and fasting insulin level showed weak but significant negative correlations with 25 (OH) D (3) level.

calcium

aspartate

25 (OH) D (3)

cholesterol

triglycerides

cholesterol

25 (OH) D (3)


Input: The mean 25 (OH) D (3) level was significantly lower in participants with NAFLD than in those without (38. 7 +/- 9. 0 vs. 39. 7 +/- 9. 7 nmol/L, p < 0. 001).

25 (OH) D (3)


Input: When participants were divided into tertiles based on mean 25 (OH) D (3) level, the proportion with NAFLD significantly increased as mean 25 (OH) D (3) level decreased (40. 0, 45. 0 and 45. 9%, p for linear trend < 0. 001).

25 (OH) D (3)

25 (OH) D (3)


Input: Multiple logistic regression analyses with NAFLD as the dependent variable showed that the tertiles with lower 25 (OH) D (3) levels had a significantly increased risk for NAFLD compared with the highest tertile, even after adjusting for body mass index and metabolic syndrome (OR 1. 247 and 1. 408 vs. the highest tertile, p < 0. 001).

25 (OH) D (3)


Input: Thus, participants with higher serum 25 (OH) D (3) showed a significantly reduced risk for NAFLD compared with the low 25 (OH) D (3) groups, independent of obesity and metabolic syndrome.

25 (OH) D (3)

25 (OH) D (3)


Input: Peer influences on drug self-administration: an econometric analysis in socially housed rats.


Input: Social-learning theories of substance use propose that members of peer groups influence the drug use of other members by selectively modeling, reinforcing, and punishing either abstinence-related or drug-related behaviors.


Input: The objective of the present study was to examine the social influences on cocaine self-administration in isolated and socially housed rats, under conditions where the socially housed rats were tested simultaneously with their partner in the same chamber.

cocaine


Input: To this end, male rats were obtained at weaning and housed in isolated or pair-housed conditions for 6 weeks.


Input: Rats were then implanted with intravenous catheters and cocaine self-administration was examined in custom-built operant conditioning chambers that allowed two rats to be tested simultaneously.

cocaine


Input: For some socially housed subjects, both rats had simultaneous access to cocaine; for others, only one rat of the pair had access to cocaine.

cocaine

cocaine


Input: An econometric analysis was applied to the data, and the reinforcing strength of cocaine was measured by examining consumption (i. e. quantity demanded) and elasticity of demand as a function of price, which was manipulated by varying the dose and ratio requirements on a fixed ratio schedule of reinforcement.

cocaine


Input: Cocaine consumption decreased as a function of price in all groups.

Cocaine


Input: Elasticity of demand did not vary across groups, but consumption was significantly lower in socially housed rats paired with a rat without access to cocaine.

cocaine


Input: These data suggest that the presence of an abstaining peer decreases the reinforcing strength of cocaine, thus supporting the development of social interventions in drug abuse prevention and treatment programs.

cocaine


Input: Inhibition of G beta gamma-subunit signaling potentiates morphine-induced antinociception but not respiratory depression, constipation, locomotion, and reward.

morphine


Input: Inhibition of G beta gamma-subunit signaling to phospholipase C beta 3 has been shown to potentiate morphine-mediated antinociception while attenuating the development of tolerance and dependence in mice.

morphine


Input: The objective of this study was to determine the effect of G beta gamma-subunit inhibition on antinociception and other pharmacological effects, such as respiratory depression, constipation, and hyperlocomotion, mediated by the mu-opioid receptor.


Input: The G beta gamma-subunit inhibitor, gallein, was administered to C57BL/6J mice by intraperitoneal injection before morphine, and data were compared with mice treated with vehicle, morphine, or gallein alone.

gallein

morphine

morphine

gallein


Input: Morphine-induced antinociception was measured using the 55 degrees C warm-water tail-withdrawal test.

Morphine


Input: Pretreatment with gallein produced a dose-dependent potentiation of morphine-mediated antinociception, producing up to a 10-fold leftward shift in the morphine dose-response curve and extending the duration of antinociception induced by a single dose of morphine.

gallein

morphine

morphine

morphine


Input: Gallein pretreatment also prevented acute antinociceptive tolerance induced by morphine.

Gallein

morphine


Input: In contrast, the dose-dependent respiratory depression and hyperlocomotion induced by morphine were not potentiated by gallein pretreatment.

morphine

gallein


Input: Similarly, gallein pretreatment did not potentiate morphine-conditioned place preference responses or morphine-induced constipation, as measured as a reduction in excreta.

gallein

morphine

morphine


Input: These results suggest that selectively inhibiting G beta gamma-mediated signaling may selectively increase mu-opioid receptor-mediated antinociception without matching increases in adverse physiological effects.


Input: Cyclodextrin alleviates neuronal storage of cholesterol in Niemann-Pick C disease without evidence of detectable blood-brain barrier permeability.

cholesterol


Input: Niemann-Pick type C disease is an inherited autosomal recessive neurodegenerative disorder characterised by the accumulation of unesterified cholesterol and sphingolipids within the endosomal/lysosomal compartments.

cholesterol

sphingolipids


Input: It has been observed that the administration of hydroxypropyl-beta-cyclodextrin (HPBCD) delays onset of clinical symptoms and reduces accumulation of cholesterol and gangliosides within neuronal cells.

hydroxypropyl-beta-cyclodextrin

HPBCD

cholesterol

gangliosides


Input: It was assumed that HPBCD exerts its action by readily entering the CNS and directly interacting with neurones and other brain cells to facilitate removal of stored cholesterol from the late endosomal/lysosomal compartment.

HPBCD

cholesterol


Input: Here, we present evidence that refutes this hypothesis.


Input: We use two well established techniques for accurately measuring brain uptake of solutes from blood and show that there is no significant crossing of HPBCD into the brain.

HPBCD


Input: The two techniques are brain in situ perfusion and intraperitoneal injection followed by multi-time-point regression analysis.


Input: Neither study demonstrates significant, time-dependent uptake of HPBCD in either adult or neonatal mice.

HPBCD


Input: However, the volume of distribution available to HPBCD (0. 113 +/- 0. 010 ml/g) exceeds the accepted values for plasma and vascular volume of the brain.

HPBCD


Input: In fact, it is nearly three times larger than that for sucrose (0. 039 +/- 0. 006 ml/g).

sucrose


Input: We propose that this indicates cell surface binding of HPBCD to the endothelium of the cerebral vasculature and may provide a mechanism for the mobilisation and clearance of cholesterol from the CNS.

HPBCD

cholesterol


Input: Differential gene expression in ER alpha-positive and ER alpha-negative breast cancer cells upon leptin stimulation.


Input: In postmenopausal women, adipositas represents a serious risk factor for cancer development and progression.


Input: White adipose tissue secretes the 16 kDa hormone leptin which plays a key role in the regulation of appetite and metabolism.


Input: An increasing number of reports indicate that leptin also interferes with signal transduction pathways implicated in the development of breast cancer.


Input: In our previous study, we identified the estrogen receptor alpha (ER alpha) as a relevant enhancer of leptin-induced signal transduction leading to transactivation of signal transducer and activator of transcription 3 (Stat3).

estrogen


Input: The purpose of this study is the investigation of specific target gene expression in response to leptin-mediated Stat3 signaling.


Input: We performed a comprehensive microarray analysis of ER alpha-positive and ER alpha-negative MDA-MB-231 cells upon leptin treatment and identified 49 genes which showed a significant ER alpha-dependent regulation in leptin-treated MDA-MB-231 cells.


Input: There was no intersection with genes which were merely up-or downregulated by ER alpha expression and only 9 and 11 genes overlapping targets which were regulated by leptin stimulation either in ER alpha-expressing or ER alpha-negative MDA-MB-231 cells, respectively.


Input: To demonstrate the specificity, expression of three target genes was validated by quantitative real-time PCR.


Input: In conclusion, these data imply that leptin can induce a different set of target genes dependent on ER alpha expression, which might contribute to the development and progression of cancer diseases.


Input: Phosphorus-doped silicon nanocrystals exhibiting mid-infrared localized surface plasmon resonance.

Phosphorus

silicon


Input: Localized surface plasmon resonances (LSPRs) enable tailoring of the optical response of nanomaterials through their free carrier concentration, morphology, and dielectric environment.


Input: Recent efforts to expand the spectral range of usable LSPR frequencies into the infrared successfully demonstrated LSPRs in doped semiconductor nanocrystals.


Input: Despite silicon' s importance for electronic and photonic applications, no LSPRs have been reported for doped silicon nanocrystals.

silicon

silicon


Input: Here we demonstrate doped silicon nanocrystals synthesized via a nonthermal plasma technique that exhibits tunable LSPRs in the energy range of 0. 07-0. 3 eV or mid-infrared wavenumbers of 600-2500 cm (-1).

silicon


Input: Immunosensor based on immobilization of antigenic peptide NS5A-1 from HCV and silk fibroin in nanostructured films.


Input: The peptide NS5A-1 (PPLLESWKDPDYVPPWHG), derived from hepatitis C virus (HCV) NS5A protein, was immobilized into layer-by-layer (LbL) silk fibroin (SF) films.


Input: Deposition was monitored by UV-vis absorption measurements at each bilayer deposited.


Input: The interaction SF/peptide film induced secondary structure in NS5A-1 as indicated by fluorescence and circular dichroism (CD) measurements.


Input: Voltammetric sensor (SF/NS5A-1) properties were observed when the composite film was tested in the presence of anti-HCV.


Input: The peptide-silk fibroin interaction studied here showed new architectures for immunosensors based on antigenic peptides and SF as a suitable immobilization matrix.


Input: Developing the potential ophthalmic applications of pilocarpine entrapped into polyvinylpyrrolidone-poly (acrylic acid) nanogel dispersions prepared by gamma radiation.

pilocarpine

polyvinylpyrrolidone

poly (acrylic acid)


Input: The aim of this study was to improve the stability and bioavailability of pilocarpine in order to maintain an adequate concentration of the pilocarpine at the site of action for prolonged period of time.

pilocarpine

pilocarpine


Input: Thus, pH-sensitive polyvinylpyrrolidone-poly (acrylic acid) (PVP/PAAc) nanogels prepared by gamma radiation-induced polymerization of acrylic acid (AAc) in an aqueous solution of polyvinylpyrrolidone (PVP) as a template polymer were used to encapsulate pilocarpine.

polyvinylpyrrolidone

poly (acrylic acid)

PVP

PAAc

acrylic acid

AAc

polyvinylpyrrolidone

PVP

pilocarpine


Input: Factors affecting size and encapsulation efficiency were optimized to obtain nanogel suitable for entrapping drug efficiently.


Input: The PVP/PAAc nanogel particles were characterized by dynamic light scattering (DLS), zeta potential, Fourier transform infrared spectroscopy (FTIR), and transmission electron microscopy (TEM), and their size can be controlled by the feed composition and concentration as well as the irradiation dose.

PVP

PAAc


Input: Pilocarpine was loaded into the nanogel particles through electrostatic interactions where the AAc-rich nanogels exhibited the highest loading efficiency.

Pilocarpine

AAc


Input: The transmittance, mucoadhesion, and rheological characteristics of the nanogel particles were studied to evaluate their ocular applicability.


Input: The in vitro release study conducted in simulated tear fluid showed a relatively long sustained release of pilocarpine from the prepared PVP/PAAc nanogel particles if compared with pilocarpine in solution.

pilocarpine

PVP

PAAc

pilocarpine


Input: High-Performance Surface Acoustic Wave Immunosensing System on a PEG/Aptamer Hybridized Surface.

PEG


Input: Label-free immunoassay systems have the advantages of procedural simplicity and a low construction cost of surfaces for immunosensing.


Input: When label-free immunoassay systems are considered, the nonspecific adsorption of unwanted materials should be eliminated unless it aids in the detection of error.


Input: PEG is well-known as a blocking agent for the prevention of the adsorption of nonspecific binding materials when coimmobilized with ligands for targets such as antibodies and oligonucleotides.

PEG


Input: The construction strategy for PEG/ligand coimmobilized surfaces is an important point in the preparation of a high-performance assays because the physiological condition of the ligand depends strongly on its interaction with the PEG chain.

PEG

PEG


Input: In this report, we investigate the interaction between thrombin and a thrombin-binding aptamer (TBA) on a PEG/TBA coimmobilized surface by using a shear horizontal surface acoustic wave (SAW) sensor.

PEG


Input: The thrombin-TBA binding property shows remarkable differences with changes in the PEG density and the distance from the gold surface to the aptamer.

PEG


Input: Influence of the bifunctional chelator on the pharmacokinetic properties of 99mTc (CO) 3-labeled cyclic alpha-melanocyte stimulating hormone analog.

99mTc (CO) 3

cyclic alpha-melanocyte stimulating hormone


Input: Aiming at the design of specific melanocortin-1 receptor (MC1R) targeted imaging probes, we report on the effect of different azolyl-ring substitution patterns (carboxylate at the 4-position and/or methyl groups at the 3, 5 positions) of pyrazolyl-diamine bifunctional chelators (Pz (2)-Pz (4)) on the pharmacokinetic profile of the (99m) Tc (CO) 3-labeled lactam bridge-cyclized alpha-melanocyte stimulating hormone derivative, beta AlaNleCycMSH (hex).

azolyl

carboxylate

methyl

pyrazolyl-diamine

(99m) Tc (CO) 3

lactam

cyclized alpha-melanocyte stimulating hormone

beta AlaNleCycMSH (hex)


Input: Three pyrazolyl-diamine-containing chelators were conjugated to beta AlaNleCycMSHhex, with the resulting peptide conjugates displaying subnanomolar MC1R binding affinity.

pyrazolyl-diamine

beta AlaNleCycMSHhex


Input: Biodistribution studies in B16F1 melanoma-bearing mice show that all radiopeptides present a good melanoma uptake.


Input: The introduction of a carboxylate group in the azolyl-ring leads to a remarkable reduction of the kidney (> 89%) and liver (> 91%) accumulation for (99m) Tc (CO) 3-Pz (3)-beta AlaNleCycMSH (hex) and (99m) Tc (CO) 3-Pz (4)-beta AlaNleCycMSH (hex) when compared to the radiopeptide (99m) Tc (CO) 3-Pz (1)-beta AlaNleCycMSH (hex), where that group is absent.

carboxylate

azolyl

(99m) Tc (CO) 3-Pz (3)-beta AlaNleCycMSH (hex)

(99m) Tc (CO) 3-Pz (4)-beta AlaNleCycMSH (hex)

(99m) Tc (CO) 3-Pz (1)-beta AlaNleCycMSH (hex)


Input: The good tumor uptake and favorable tumor-to-nontarget-organs ratios of (99m) Tc (CO) 3-Pz (3)-beta AlaNleCycMSH (hex) and (99m) Tc (CO) 3-Pz (4)-beta AlaNleCycMSH (hex) highlights the potential of both compounds as melanoma imaging agents.

(99m) Tc (CO) 3-Pz (3)-beta AlaNleCycMSH (hex)

(99m) Tc (CO) 3-Pz (4)-beta AlaNleCycMSH (hex)


Input: Vegfrecine, an Inhibitor of VEGF Receptor Tyrosine Kinases Isolated from the Culture Broth of Streptomyces sp.

Vegfrecine

Tyrosine


Input: A new inhibitor of VEGF receptor tyrosine kinases, vegfrecine (1), was isolated from the culture broth of Streptomyces sp.

tyrosine

vegfrecine


Input: The molecular structure of 1 was determined by NMR and MS analysis combined with synthesis.


Input: Compound 1 showed potent inhibitory activity against vascular endothelial growth factor receptor (VEGFR) tyrosine kinases in in vitro enzyme assays, but platelet-derived growth factor receptors (PDGFRs), fibroblast growth factor receptor (FGFR), and epidermal growth factor receptor (EGFR) responded only weakly.


Input: Compound 1 is a promising new selective VEGFR inhibitor for investigating new treatments of cancer and inflammatory diseases.


Input: Reduction of dimethylarsinic acid to the highly toxic dimethylarsinous acid by rats and rat liver cytosol.

dimethylarsinic acid

dimethylarsinous acid


Input: Dimethylarsinic acid (DMAs (V)), the major urinary metabolite of inorganic arsenic, is weakly cytotoxic, whereas its reduced form, dimethylarsinous acid (DMAs (III)), is highly toxic.

Dimethylarsinic acid

DMAs (V)

arsenic

dimethylarsinous acid

DMAs (III)


Input: Although glutathione S-transferase omega 1 (GSTO1) and arsenic methyltransferase have been shown or thought to catalyze DMAs (V) reduction, their role in DMAs (V) reduction in vivo, or in cell extracts is uncertain.

glutathione S

arsenic

DMAs (V)

DMAs (V)


Input: Therefore, the reduction of DMAs (V) to DMAs (III) in rats and in rat liver cytosol was studied to better understand its mechanism.

DMAs (V)

DMAs (III)


Input: To assess DMAs (V) reduction in rats, a novel procedure was devised based on following the accumulation of red blood cell (RBC)-bound dimethylarsenic (DMAs), which represents DMAs (III), in the blood of DMAs (V)-injected anesthetized rats.

DMAs (V)

dimethylarsenic

DMAs

DMAs (III)

DMAs (V)


Input: These studies indicated that rats reduced DMAs (V) to DMAs (III) to a significant extent, as in 90 min 31% of the injected 50 mu mol/kg DMAs (V) dose was converted to DMAs (III) that was sequestered by the circulating erythrocytes.

DMAs (V)

DMAs (III)

DMAs (V)

DMAs (III)


Input: Pretreatment of rats with glutathione (GSH) depletors (phorone or BSO) delayed the elimination of DMAs (V) and the accumulation of RBC-bound DMAs, whereas the indirect methyltransferase inhibitor periodate-oxidized adenosine was without effect.

glutathione

GSH

phorone

BSO

DMAs (V)

DMAs

periodate

adenosine


Input: Assessment of DMAs (V)-reducing activity of rat liver cytosol revealed that reduction of DMAs (V) required cytosolic protein and GSH and was inhibited by thiol reagents, GSSG and dehydroascorbate.

DMAs (V)

DMAs (V)

GSH

thiol

GSSG

dehydroascorbate


Input: Although thioredoxin reductase (TRR) inhibitors (aurothioglucose and Sb (III)) inhibited cytosolic DMAs (V) reduction, recombinant rat TRR plus NADPH, alone or when added to the cytosol, failed to support DMAs (V) reduction.

aurothioglucose

Sb (III)

DMAs (V)

NADPH

DMAs (V)


Input: On ultrafiltration of the cytosol through a 3 kDa filter, the reducing activity in the retentate was lost but was largely restored by NADPH.

NADPH


Input: Such experiments also suggested that the reducing enzyme was larger than 100 kDa and was not GSTO1.


Input: In summary, reduction of DMAs (V) to the highly toxic DMAs (III) in rats and rat liver cytosol is a GSH-dependent enzymatic process, yet its mechanism remains uncertain.

DMAs (V)

DMAs (III)

GSH


Input: Embryonic and induced pluripotent stem cells: understanding, creating, and exploiting the nano-niche for regenerative medicine.


Input: Embryonic stem cells (ESCs) and induced pluripotent stem cells (iPSCs) have the capacity to differentiate into any specialized cell type of the human body, and therefore, ESC/iPSC-derived cell types offer great potential for regenerative medicine.


Input: However, key to realizing this potential requires a strong understanding of stem cell biology, techniques to maintain stem cells, and strategies to manipulate cells to efficiently direct cell differentiation toward a desired cell type.


Input: As nanoscale science and engineering continues to produce novel nanotechnology platforms, which inform, infiltrate, and impinge on many aspects of everyday life, it is no surprise that stem cell research is turning toward developments in nanotechnology to answer research questions and to overcome obstacles in regenerative medicine.


Input: Here we discuss recent advances in ESC and iPSC manipulation using nanomaterials and highlight future challenges within this area of research.


Input: Large-scale spinning assembly of neat, morphology-defined, graphene-based hollow fibers.

graphene


Input: Large-scale assembly of graphenes in a well-controlled macroscopic fashion is important for practical applications.

graphenes


Input: We have developed a facile and straightforward approach for continuous fabrication of neat, morphology-defined, graphene-based hollow fibers (HFs) via a coaxial two-capillary spinning strategy.

graphene


Input: With a high throughput, HFs and necklace-like HFs of graphene oxide have been well-controlled produced with the ease of functionalization and conversion to graphene HFs via simply thermal or chemical reduction.

graphene oxide

graphene


Input: This work paves the way toward the mass production of graphene-based HFs with desirable functionalities and morphologies for many of important applications in fluidics, catalysis, purification, separation, and sensing.

graphene


Input: Kisspeptin as a link between metabolism and reproduction: Evidences from rodent and primate studies.


Input: Changes in metabolic status gate reproductive activity by still incompletely deciphered mechanisms.


Input: Many neuropeptides have been shown to be involved in restraining hypothalamic gonadotropin releasing hormone (GnRH) release under conditions of negative energy balance.


Input: Broadly, on the basis of their effect on feeding, these can be grouped as orexigenic and anorexigenic neuropeptides.


Input: Reciprocally correlated, in response to changes in systemic concentrations of metabolic hormones, the secretion of orexigenic neuropeptides increases while that of anorexigenic neuropeptides decreases during conditions of food restriction.


Input: Recently, kisspeptin signaling in hypothalamus has appeared as a pivotal regulator of the GnRH pulse generator.


Input: Kisspeptin apparently does not affect feeding, but in light of accumulating data, it has emerged as one of the major conduits in relaying body metabolic status information to GnRH neurons.


Input: The present review examines such data obtained from rodent and primate models, which suggest kisspeptin-Kiss1r signaling as a possible pathway providing a link between metabolism and reproduction.


Input: Discovery of novel 7-membered cyclic amide derivatives that inhibit 11beta-hydroxysteroid dehydrogenase type 1.

7-membered cyclic amide


Input: A series of novel 5-trans-hydroxyadamantan-2-yl-5, 6, 7, 8-tetrahydropyrazolo [4, 3-c] azepin-4 (1H)-ones that inhibit 11beta-hydroxysteroid dehydrogenase type 1 are described.

5-trans-hydroxyadamantan-2-yl-5, 6, 7, 8-tetrahydropyrazolo [4, 3-c] azepin-4 (1H)-ones


Input: We discovered these 7-membered cyclic amide derivatives by introducing a distinctive linker through pharmacophore analysis of known ligands included in X-ray co-crystal structures.

7-membered cyclic amide


Input: Further optimization using docking studies led to highly potent inhibitors 15b and 27, which furthermore showed the potent efficacy in in vivo studies.


Input: Chemical tagging of a drug target using 5-sulfonyl tetrazole.

5-sulfonyl tetrazole


Input: Irreversible modification is one of the most promising strategies to identify cellular receptors of bioactive small molecules.


Input: Here we report that receptor proteins can be chemically tagged using a 5-sulfonyl tetrazole probe.

5-sulfonyl tetrazole


Input: 5-Sulfonyl tetrazole easily accepted nucleophilic attack of thiol groups, while 5-sulfinyl tetrazole did not.

5-Sulfonyl tetrazole

thiol

5-sulfinyl tetrazole


Input: These functional groups were introduced into probe molecules of a natural product.


Input: Cyclosporine A, an immunosuppressant produced by a microbe, was derivatized to possess 5-sulfonyl tetrazole and a tag group, which enabled chemical tagging of cyclophilin A, the cellular receptor of cyclosporine A.

Cyclosporine A

5-sulfonyl tetrazole

cyclosporine A


Input: Cyclosporine A derivative possessing 5-sulfinyl tetrazole could not tag cyclophilin A.

Cyclosporine A

5-sulfinyl tetrazole


Input: This technique will allow efficient identification of cellular receptors of bioactive small molecules.


Input: Anion inhibition studies of the alpha-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae.


Input: An alpha-carbonic anhydrase (CA, EC 4. 2. 1. 1) has been recently cloned and characterized in the human pathogenic bacterium Vibrio cholerae, denominated VchCA (Del Prete et al. J. Med. Chem. 2012, 55, 10742).


Input: This enzyme shows a good catalytic activity for the CO2 hydration reaction, comparable to that of the human (h) isoform hCA I.


Input: Many inorganic anions and several small molecules were investigated as VchCA inhibitors.


Input: Inorganic anions such as cyanate, cyanide, hydrogen sulfide, hydrogen sulfite, and trithiocarbonate were effective VchCA inhibitors with inhibition constants in the range of 33-88 mu M.

cyanate

cyanide

hydrogen sulfide

hydrogen sulfite

trithiocarbonate


Input: Other effective inhibitors were diethyldithiocarbamate, sulfamide, sulfamate, phenylboronic acid and phenylarsonic acid, with KIs of 7-43 mu M.

diethyldithiocarbamate

sulfamide

sulfamate

phenylboronic acid

phenylarsonic acid


Input: Halides (bromide, iodide), bicarbonate and carbonate were much less effective VchCA inhibitors, with KIs in the range of 4. 64-28. 0mM.

Halides

bromide

iodide

bicarbonate

carbonate


Input: The resistance of VchCA to bicarbonate inhibition may represent an evolutionary adaptation of this enzyme to living in an environment rich in this ion, such as the gastrointestinal tract, as bicarbonate is a virulence enhancer of this bacterium.

bicarbonate

bicarbonate


Input: Synthesis of tetrazole analogues of phosphonohydroxamic acids: an attempt to improve the inhibitory activity against the DXR.

phosphonohydroxamic acids


Input: This work is focused on the design of new antimicrobial drugs and on the development of lipophilic inhibitors of the DXR, the second enzyme of the MEP pathway for the biosynthesis of isoprene units in most bacteria, by replacing the phosphonate group of fosmidomycin derivatives by a tetrazoyl moiety capable of multiple hydrogen bonding.

isoprene

phosphonate

fosmidomycin

tetrazoyl

hydrogen


Input: The N-and C-substituted tetrazole analogues of phosphonohydroxamate inhibitors were synthesized and tested on the DXR of Escherichia coli.

N

C

tetrazole

phosphonohydroxamate


Input: This work points out the hypothesis that the phosphonate/phosphate recognition site might be too rigid to accommodate other functional groups.

phosphonate

phosphate


Input: 3D-QSAR and docking studies of pentacycloundecylamines at the sigma-1 (sigma 1) receptor.

pentacycloundecylamines


Input: Pentacycloundecylamine (PCU) derived compounds have been shown to be promising lead structures for the development of novel drug candidates aimed at a variety of neurodegenerative and psychiatric diseases.

Pentacycloundecylamine

PCU


Input: Here we show for the first time a 3D quantitative structure-activity relationship (3D-QSAR) for a series of aza-PCU-derived compounds with activity at the sigma-1 (sigma 1) receptor.

aza-PCU


Input: A comparative molecular field analysis (CoMFA) model was developed with a partial least squares cross validated (q (2)) regression value of 0. 6, and a non-cross validated r (2) of 0. 9.


Input: The CoMFA model was effective at predicting the sigma-1 activities of a test set with an r (2) > 0. 7.


Input: We also describe here the docking of the PCU-derived compounds into a homology model of the sigma-1 (sigma 1) receptor, which was developed to gain insight into binding of these cage compounds to the receptor.

PCU


Input: Based on docking studies we evaluated in a [(3) H] pentazocine binding assay an oxa-PCU, NGP1-01 (IC50 = 1. 78 mu M) and its phenethyl derivative (IC50 = 1. 54 mu M).

[(3) H] pentazocine

oxa-PCU

phenethyl


Input: Results from these studies can be used to develop new compounds with specific affinity for the sigma-1 (sigma 1) receptor.


Input: Investigation of antibacterial mode of action for traditional and amphiphilic aminoglycosides.

aminoglycosides


Input: Aminoglycoside represents a class of versatile and broad spectrum antibacterial agents.

Aminoglycoside


Input: In an effort to revive the antibacterial activity against aminoglycoside resistant bacteria, our laboratory has developed two new classes of aminoglycoside, pyranmycin and amphiphilic neomycin (NEOF004).

aminoglycoside

aminoglycoside

pyranmycin

neomycin


Input: The former resembles the traditional aminoglycoside, neomycin.

aminoglycoside

neomycin


Input: The latter, albeit derived from neomycin, appears to exert antibacterial action via a different mode of action.

neomycin


Input: In order to discern that these aminoglycoside derivatives have distinct antibacterial mode of action, RNA-binding affinity and fluorogenic dye were employed.

aminoglycoside


Input: These studies, together with our previous investigation, confirm that pyranmycin exhibit the traditional antibacterial mode of action of aminoglycosides by binding toward the bacterial rRNA.

aminoglycosides


Input: On the other hand, the amphiphilic neomycin, NEOF004 disrupts the bacterial cell wall.

neomycin


Input: In a broader perspective, it verifies that structurally modified neomycin can exert different antibacterial mode of action leading to the revival of activity against aminoglycoside resistant bacteria.

neomycin

aminoglycoside


Input: Structure-based discovery of cellular-active allosteric inhibitors of FAK.


Input: In order to develop potent and selective focal adhesion kinase (FAK) inhibitors, synthetic studies on pyrazolo [4, 3-c] [2, 1] benzothiazines targeted for the FAK allosteric site were carried out.

pyrazolo [4, 3-c] [2, 1] benzothiazines


Input: Based on the X-ray structural analysis of the co-crystal of the lead compound, 8-(4-ethylphenyl)-5-methyl-1, 5-dihydropyrazolo [4, 3-c] [2, 1] benzothiazine 4, 4-dioxide 1 with FAK, we designed and prepared 1, 5-dimethyl-1, 5-dihydropyrazolo [4, 3-c] [2, 1] benzothiazin derivatives which selectively inhibited kinase activity of FAK without affecting seven other kinases.

8-(4-ethylphenyl)-5-methyl-1, 5-dihydropyrazolo [4, 3-c] [2, 1] benzothiazine 4, 4-dioxide

1, 5-dimethyl-1, 5-dihydropyrazolo [4, 3-c] [2, 1] benzothiazin


Input: The optimized compound, N-(4-tert-butylbenzyl)-1, 5-dimethyl-1, 5-dihydropyrazolo [4, 3-c] [2, 1] benzothiazin-8-amine 4, 4-dioxide 30 possessed significant FAK kinase inhibitory activities both in cell-free (IC50 = 0. 64 mu M) and in cellular assays (IC50 = 7. 1 mu M).

N-(4-tert-butylbenzyl)-1, 5-dimethyl-1, 5-dihydropyrazolo [4, 3-c] [2, 1] benzothiazin-8-amine 4, 4-dioxide


Input: These results clearly demonstrated a potential of FAK allosteric inhibitors as antitumor agents.


Input: Stability of black cohosh triterpene glycosides and polyphenols: Potential clinical relevance.

triterpene glycosides

polyphenols


Input: Concurrent to a clinical trial of black cohosh for menopausal hot flashes, the long-term stability of the black cohosh, over the duration of the clinical trial, was examined.


Input: Analytical results showed that the major constituents, both triterpene glycosides and polyphenols, were stable over the 3-year period of testing.

triterpene glycosides

polyphenols


Input: These results indicate that a black cohosh product stored for several years in a controlled environment does not undergo significant changes in its major constituents.


Input: These results have implications not only for clinical research in natural products, but for basic science, as well as the dietary supplements industry.


Input: Evidence-based review and assessment of botulinum neurotoxin for the treatment of urologic conditions.


Input: Botulinum neurotoxin (BoNT) can be injected to achieve therapeutic benefit across a large range of clinical conditions.


Input: To assess the efficacy and safety of BoNT injections for the treatment of certain urologic conditions, including detrusor sphincter dyssynergia (DSD), lower urinary tract symptoms due to benign prostatic hyperplasia (BPH), and detrusor overactivity (both neurogenic [NDO] and idiopathic [IDO]), an expert panel reviewed evidence from the published literature.


Input: Data sources included English-language studies identified via MEDLINE, EMBASE, CINAHL, Current Contents, and the Cochrane Central Register of Controlled Trials.


Input: Evidence tables generated in the 2008 Report of the Therapeutics and Technology Assessment Subcommittee of the American Academy of Neurology (AAN) review of the use of BoNT for autonomic disorders were also reviewed and updated.


Input: The panel evaluated evidence at several levels, supporting BoNT as a class, for the serotypes BoNT-A and BoNT-B, as well as for the four individual commercially available formulations: abobotulinumtoxinA (A/Abo), onabotulinumtoxinA (A/Ona), incobotulinumtoxinA (A/Inco), and rimabotulinumtoxinB (B/Rima).


Input: The panel ultimately made recommendations on the use of BoNT for the management of these urologic conditions based upon the strength of clinical evidence and following the AAN classification scale.


Input: For the treatment of DSD, the evidence supported a Level B recommendation for the use of A/Ona; A/Abo, A/Inco, and B/Rima received a Level U recommendation.


Input: For the treatment of NDO, there was sufficient clinical evidence to support a Level A recommendation for BoNT-A as well as for both A/Ona and A/Abo; no published data were identified for either A/Inco or B/Rima (Level U).


Input: For the treatment of IDO, the evidence supported a Level A recommendation for A/Ona; A/Inco, A/Abo, and B/Rima received a Level U recommendation.


Input: For the management of BPH, the evidence supported a Level B recommendation for BoNT and A/Ona; no published studies were identified for A/Abo, A/Inco, or B/Rima, warranting a Level U recommendation for these three formulations.


Input: Further studies are needed to evaluate the efficacy and safety of BoNT for the management of urologic conditions.


Input: Metabolism of profenofos to 4-bromo-2-chlorophenol, a specific and sensitive exposure biomarker.

profenofos


Input: Profenofos is a direct acting phosphorothioate organophosphorus (OP) pesticide capable of inhibiting beta-esterases such as acetylcholinesterase, butyrylcholinesterase, and carboxylesterase.

Profenofos

phosphorothioate organophosphorus


Input: Profenofos is known to be detoxified to the biologically inactive metabolite, 4-bromo-2-chlorophenol (BCP); however, limited data are available regarding the use of urinary BCP as an exposure biomarker in humans.

Profenofos

BCP

BCP


Input: A pilot study conducted in Egyptian agriculture workers, demonstrated that urinary BCP levels prior to application (3. 3-30. 0 mu g/g creatinine) were elevated to 34. 5-3566 mu g/g creatinine during the time workers were applying profenofos to cotton fields.

BCP

creatinine

creatinine

profenofos


Input: Subsequently, the in vitro enzymatic formation of BCP was examined using pooled human liver microsomes and recombinant human cytochrome P-450s (CYPs) incubated with profenofos.

BCP

profenofos


Input: Of the nine human CYPs studied, only CYPs 3A4, 2B6, and 2C19 were able to metabolize profenofos to BCP.

profenofos

BCP


Input: Kinetic studies indicated that CYP 2C19 has the lowest Km, 0. 516 mu M followed by 2B6 (Km = 1. 02 mu M) and 3A4 (Km = 18. 9 mu M).


Input: The Vmax for BCP formation was 47. 9, 25. 1, and 19. 2nmol/min/nmol CYP for CYP2B6, 2C19, and 3A4, respectively.

BCP


Input: Intrinsic clearance (Vmax/Km) values of 48. 8, 46. 9, and 1. 02ml/min/nmol CYP 2C19, 2B6, and 3A4, respectively, indicate that CYP2C19 and CYP2B6 are primarily responsible for the detoxification of profenofos.

profenofos


Input: These findings support the use of urinary BCP as a biomarker of exposure to profenofos in humans and suggest polymorphisms in CYP 2C19 and CYP 2B6 as potential biomarkers of susceptibility.

BCP

profenofos


Input: Signaling of an allosteric, nanomolar potent, low molecular weight agonist for the follicle-stimulating hormone receptor.


Input: Follicle-stimulating hormone (FSH) activates FSH receptors (FSHR) in granulosa cells to induce follicle differentiation, growth and estradiol production.

estradiol


Input: FSH is used clinically to treat female infertility and is administered by injection.


Input: To increase patient convenience and compliance, compound homogeneity and composition, low molecular weight (LMW), orally bioavailable, FSHR agonists are now being developed to replace FSH.


Input: In this study, we present the signaling mechanisms of a newly developed LMW dihydropyridine agonist of the FSHR, Org 214444-0.

dihydropyridine

Org 214444-0


Input: Org 214444-0 is shown to be a stereoselective, nanomolar potent FSHR agonist and selective over the structurally related LHR and TSHR.

Org 214444-0


Input: Org 214444-0 is an allosteric agonist interacting with the transmembrane region of the FSHR.

Org 214444-0


Input: When co-incubated with FSH, Org 214444-0 augments FSH' s potency in binding (6. 5-fold) and adenylyl cyclase/cAMP activation (3. 5-fold) in a concentration-dependent manner.

Org 214444-0

cAMP


Input: Like FSH, Org 214444-0 induces FSHR internalization and is only marginally effective in stimulating phospholipase C.

Org 214444-0


Input: Moreover, Org 214444-0 stimulates cAMP and estradiol production in human granulosa cells in culture and supports the follicular phase in mature female rats.

Org 214444-0

cAMP

estradiol


Input: We conclude that Org 214444-0 is a bonafide FSHR agonist.

Org 214444-0


Input: A high-throughput-compatible, fluorescence anisotropy-based assay for ATP-dependent supercoiled DNA relaxation by human topoisomerase II alpha.

ATP


Input: A novel, high-throughput-compatible assay for the ATP-dependent supercoiled DNA relaxing activity of human topoisomerase II alpha (hTopoII alpha) is described.

ATP


Input: The principle of detection is the preferential binding of the oligodeoxyribonucleotide BODIPY-TMR-5'-TTCTTCTTCT-3' to relaxed double-stranded plasmid containing the triplex forming sequence (TTC) 9 versus the supercoiled plasmid.

BODIPY

TMR


Input: Binding of the oligonucleotide to the plasmid increases the fluorescence anisotropy of the BODIPY-TMR label.

BODIPY

TMR


Input: Optimization of the assay conditions was conducted to maximize the signal and the activity of the topoisomerase.


Input: The multiwell assay plate-based fluorescence anisotropy assay gave the same values for the potencies of several previously reported inhibitors of hTopoII alpha as a gel electrophoresis-based assay of DNA relaxation.


Input: Design and synthesis of bicyclic pyrazinone and pyrimidinone amides as potent TF-FVIIa inhibitors.

bicyclic pyrazinone and pyrimidinone amides


Input: Bicyclic pyrazinone and pyrimidinone amides were designed and synthesized as potent TF-FVIIa inhibitors.

Bicyclic pyrazinone and pyrimidinone amides


Input: SAR demonstrated that the S2 and S3 pockets of FVIIa prefer to bind small, lipophilic groups.


Input: An X-ray crystal structure of optimized compound 9b bound in the active site of FVIIa showed that the bicyclic scaffold provides 5 hydrogen bonding interactions in addition to projecting groups for interactions within the S1, S2 and S3 pockets.

hydrogen


Input: Compound 9b showed excellent FVIIa potency, good selectivity against FIXa, Xa, XIa and chymotrypsin, and good clotting activity.


Input: Efficient synthesis of anacardic acid analogues and their antibacterial activities.

anacardic acid


Input: Anacardic acid derivatives exhibit a broad range of biological activities.

Anacardic acid


Input: In this report, an efficient method for the synthesis of anacardic acid derivatives was explored, and a small set of salicylic acid variants synthesised retaining a constant hydrophobic element (a naphthyl tail).

anacardic acid

salicylic acid

naphthyl


Input: The naphthyl side chain was introduced via Wittig reaction and the aldehyde installed using directed ortho-metalation reaction of the substituted o-anisic acids.

naphthyl

aldehyde

o-anisic acids


Input: The failure of ortho-metalation using unprotected carboxylic acid group compelled us to use directed ortho-metalation in which a tertiary amide was used as a strong ortho-directing group.

carboxylic acid

tertiary amide


Input: In the initial route, tertiary amide cleavage during final step was challenging, but cleaving the tertiary amide before Wittig reaction was beneficial.

tertiary amide

tertiary amide


Input: The Wittig reaction with protected carboxylic group (methyl ester) resulted in side-products whereas using sodium salt resulted in higher yields.

carboxylic

methyl ester

sodium


Input: The novel compounds were screened for antibacterial activity and cytotoxicity.


Input: Although substitution on the salicylic head group enhanced antibacterial activities they also enhanced cytotoxicity.

salicylic


Input: Substituted piperidinyl glycinyl 2-cyano-4, 5-methano pyrrolidines as potent and stable dipeptidyl peptidase IV inhibitors.

piperidinyl glycinyl 2-cyano-4, 5-methano pyrrolidines


Input: Synthesis and structure-activity relationship of a series of substituted piperidinyl glycine 2-cyano-4, 5-methano pyrroline DPP-IV inhibitors are described.

piperidinyl glycine 2-cyano-4, 5-methano pyrroline


Input: Improvement of the inhibitory activity and chemical stability of this series of compounds was respectively achieved by the introduction of bulky groups at the 4-position and 1-position of the piperidinyl glycine, leading to a series of potent and stable DPP-IV inhibitors.

piperidinyl glycine


Input: A multivalent peptide as an activator of hypoxia inducible factor-1 alpha.


Input: Hypoxia inducible factor-1 alpha (HIF-1 alpha) is a transcription factor found in mammalian cells under hypoxia.


Input: While HIF-1 alpha in hypoxia translocates to the nucleus where it transcribes the target genes including vascular endothelial growth factor (VEGF) mRNA, HIF-1 alpha is degraded under normoxia, which involves its proline hydroxylation and subsequent binding to the von Hippel-Lindau protein-Elongin B-Elogin C (VBC) complex.

proline


Input: Previously, peptide inhibitors against this interaction between hydroxylated HIF-1 alpha and VBC have been developed to stabilize the transcriptional activity of HIF-1 alpha by preventing the degradation of the protein even under normoxia.


Input: Despite the specific inhibition by these peptides, their poor inhibition potency needs to be improved for further clinical application.


Input: In this work, we have designed and prepared a streptavidin-based multivalent peptide inhibitor against the HIF-1 alpha-VBC complexation.


Input: We have evaluated the potency of the multivalent peptide in terms of stabilization of HIF-1 alpha and the downstream effect.


Input: As the result, we have found that the inhibitor showed about 13-fold lowered IC50 value compared with that of the corresponding monovalent peptide, thereby activating HIF-1 alpha and leading to up-regulation of VEGF protein at the cellular level.


Input: The alpha 3 beta 4 * nicotinic acetylcholine receptor subtype mediates nicotine reward and physical nicotine withdrawal signs independently of the alpha 5 subunit in the mouse.

acetylcholine

nicotine

nicotine


Input: The 15q25 gene cluster contains genes that code for the alpha 5, alpha 3, and beta 4 nicotinic acetylcholine receptor (nAChRs) subunits, and in human genetic studies, has shown the most robust association with smoking behavior and nicotine dependence to date.

acetylcholine

nicotine


Input: The limited available animal studies implicate a role for the alpha 5 and beta 4 nAChR subunits in nicotine dependence and withdrawal; however studies focusing on the behavioral role of the alpha 3 beta 4 * nAChR receptor subtype in nicotine dependence are lacking.

nicotine

nicotine


Input: Because of the apparent role of the alpha 3 beta 4 * nAChR subtype in nicotine dependence, the goal of the current study was to better evaluate the involvement of this subtype in nicotine mediated behavioral responses.

nicotine

nicotine


Input: Using the selective alpha 3 beta 4 * nAChR antagonist, alpha-conotoxin AuIB, we assessed the role of alpha 3 beta 4 * nAChRs in acute nicotine, nicotine reward, and physical and affective nicotine withdrawal.

nicotine

nicotine

nicotine


Input: Because alpha 5 has also been implicated in nicotine dependence behaviors in mice and can form functional receptors with alpha 3 beta 4 *, we also evaluated the role of the alpha 3 beta 4 alpha 5 * nAChR subtype in nicotine reward and somatic nicotine withdrawal signs by blocking the alpha 3 beta 4 * nAChR subtype in alpha 5 nAChR knockout mice with AuIB.

nicotine

nicotine

nicotine


Input: AuIB had no significant effect on acute nicotine behaviors, but dose-dependently attenuated nicotine reward and physical withdrawal signs, with no significant effect in affective withdrawal measures.

nicotine

nicotine


Input: Interestingly, AuIB also attenuated nicotine reward and somatic signs in alpha 5 nAChR knockout mice.

nicotine


Input: This study shows that alpha 3 beta 4 * nAChRs mediate nicotine reward and physical nicotine withdrawal, but not acute nicotine behaviors or affective nicotine withdrawal signs in mice.

nicotine

nicotine

nicotine

nicotine


Input: The alpha 5 subunit is not required in the receptor assembly to mediate these effects.


Input: Our findings suggest an important role for the alpha 3 beta 4 * nAChR subtype in nicotine reward and physical aspects of the nicotine withdrawal syndrome.

nicotine

nicotine


Input: Human serum albumin-based design of a diflunisal prodrug.

diflunisal


Input: The cyclooxygenase-2 inhibitor, diflunisal, is used in the clinic for its anti-inflammatory activity.

diflunisal


Input: About 99% of a dose of diflunisal is unavailable for reaction with the target enzyme, because diflunisal strongly binds to human serum albumin (HSA).

diflunisal

diflunisal


Input: To reduce the binding affinity of diflunisal to albumin, we designed and synthesized the prodrug acetyldiflunisal.

diflunisal

acetyldiflunisal


Input: The crystal structure of HSA complexed with fatty acid and acetyldiflunisal revealed that acetyldiflunisal binds to the IIA subdomain and that upon binding, it acetylates lysine 199.

fatty acid

acetyldiflunisal

acetyldiflunisal

lysine


Input: Mass spectrometry confirmed that acetyldiflunisal acetylates Lys199.

acetyldiflunisal


Input: The acetylated albumin had twofold weaker binding affinity for diflunisal as demonstrated by fluorescence quenching.

diflunisal


Input: Reduced binding affinity means that diflunisal is more easily released from acetylated albumin into the circulation.

diflunisal


Input: Therefore, lower doses of acetyldiflunisal compared to diflunisal will be required.

acetyldiflunisal

diflunisal


Input: Taken together, our results not only provide a template for design of HSA-based prodrugs, but also pave the way toward more effective use of diflunisal in the clinic.

diflunisal


Input: Antitumor and immunomodulatory activity of a water-soluble low molecular weight polysaccharide from Schisandra chinensis (Turcz.) Baill.


Input: A water-soluble low molecular weight polysaccharide (SCPP11) was extracted and purified using DEAE-cellulose and Sephadex G-100 column from Schisandra chinensis (Turcz.) Baill.


Input: Its in vivo and in vitro antitumor and immunomodulatory activity were investigated.


Input: The results showed that SCPP11 with a molecular weight of 3. 4 x 10 (3) Da exhibited indirect cyctotoxic activity against tumor cells in vitro, but could significantly inhibit the growth of Heps cells in vivo at dose of 50mg/kg, and its inhibition rate is higher than that in the positive group.