Input: High-resolution melting analysis (HRM) and methylation-specific PCR (MSP) were performed to detect gene mutation and methylation, respectively, in cell lines and tissues samples.


Input: Expression of NDRG1 mRNA and protein was downregulated in gastric cancer cell lines and tissues.


Input: Specifically, expression of NDRG1 mRNA and protein was lower in all six gastric cancer cell lines than that of normal gastric cells, while 15 out of 20 cases of gastric cancer tissues had the reduced levels of NDRG1 mRNA and protein.


Input: HRM data showed that there was no mutation in NDRG1 gene, but MSP data showed high levels of NDRG1 gene promoter methylation in the CpG islands in both cell lines and tissue samples.


Input: Moreover, treatment with the DNA methyltransferase inhibitor 5-Aza-2'-deoxycytidine upregulated NDRG1 expression in gastric cancer HGC27 cells, but not in the histone deacetylase inhibitor trichostatin A-treated HGC27 cells.

trichostatin A


Input: In conclusion, this study has shown that expression of NDRG1 mRNA and protein was reduced in gastric cancer cell lines and tissues, which is due to methylation of NDRG1 gene promoter.


Input: Further study will unearth the clinical significance of the reduced NDRG1 protein in gastric cancer.


Input: Influence of dietary carbon on mercury bioaccumulation in streams of the Adirondack Mountains of New York and the Coastal Plain of South Carolina, USA.

carbon

mercury


Input: We studied lower food webs in streams of two mercury-sensitive regions to determine whether variations in consumer foraging strategy and resultant dietary carbon signatures accounted for observed within-site and among-site variations in consumer mercury concentration.

mercury

carbon

mercury


Input: We collected macroinvertebrates (primary consumers and predators) and selected forage fishes from three sites in the Adirondack Mountains of New York, and three sites in the Coastal Plain of South Carolina, for analysis of mercury (Hg) and stable isotopes of carbon (delta (13) C) and nitrogen (delta (15) N).

mercury

Hg

carbon

(13) C

nitrogen

(15) N


Input: Among primary consumers, scrapers and filterers had higher MeHg and more depleted delta (13) C than shredders from the same site.

MeHg

(13) C


Input: Variation in delta (13) C accounted for up to 34% of within-site variation in MeHg among primary consumers, beyond that explained by delta (15) N, an indicator of trophic position.

(13) C

MeHg

(15) N


Input: Consumer delta (13) C accounted for 10% of the variation in Hg among predatory macroinvertebrates and forage fishes across these six sites, after accounting for environmental aqueous methylmercury (MeHg, 5% of variation) and base-N adjusted consumer trophic position (Delta delta (15) N, 22% of variation).

(13) C

Hg

methylmercury

MeHg

N

(15) N


Input: The delta (13) C spatial pattern within consumer taxa groups corresponded to differences in benthic habitat shading among sites.

(13) C


Input: Consumers from relatively more-shaded sites had more enriched delta (13) C that was more similar to typical detrital delta (13) C, while those from the relatively more-open sites had more depleted delta (13) C.

(13) C

(13) C

(13) C


Input: Although we could not clearly attribute these differences strictly to differences in assimilation of carbon from terrestrial or in-channel sources, greater potential for benthic primary production at more open sites might play a role.

carbon


Input: We found significant variation among consumers within and among sites in carbon source; this may be related to within-site differences in diet and foraging habitat, and to among-site differences in environmental conditions that influence primary production.

carbon


Input: These observations suggest that different foraging strategies and habitats influence MeHg bioaccumulation in streams, even at relatively small spatial scales.

MeHg


Input: Such influence must be considered when selecting lower trophic level consumers as sentinels of MeHg bioaccumulation for comparison within and among sites.

MeHg


Input: Enzyme kinetic and molecular docking studies for the inhibitions of miltirone on major human cytochrome P450 isozymes.

miltirone


Input: Previous studies have shown that major tanshinones isolated from Danshen (Salvia miltiorrhiza) inhibited human and rat CYP450 enzymes-mediated metabolism of model probe substrates, with potential in causing herb-drug interactions.

tanshinones


Input: Miltirone, another abietane type-diterpene quinone isolated from Danshen, has been reported for its anti-oxidative, anxiolytic and anti-cancer effects.

Miltirone

abietane

diterpene quinone


Input: The aim of this study was to study the effect of miltirone on the metabolism of model probe substrates of CYP1A2, 2C9, 2D6 and 3A4 in pooled human liver microsomes.

miltirone


Input: Miltirone showed moderate inhibition on CYP1A2 (IC (50) = 1. 73 mu M) and CYP2C9 (IC (50) = 8. 61 mu M), and weak inhibition on CYP2D6 (IC (50) = 30. 20 mu M) and CYP3A4 (IC (50) = 33. 88 mu M).

Miltirone


Input: Enzyme kinetic studies showed that miltirone competitively inhibited CYP2C9 (K (i) = 1. 48 mu M), and displayed mixed type inhibitions on CYP1A2, CYP2D6 and CYP3A4 with K (i) values of 3. 17 mu M, 24. 25 mu M and 35. 09 mu M, respectively.

miltirone


Input: Molecular docking study further confirmed the ligand-binding conformations of miltirone in the active sites of these human CYP450 isoforms, and provided some information on structure-activity relationships for the CYPs inhibition by tanshinones.

miltirone

tanshinones


Input: Taken together, CYPs inhibitions of miltirone were weaker than dihydrotanshinone, but stronger than cryptotanshinone, tanshinone I and tanshinone IIA.

miltirone

dihydrotanshinone

cryptotanshinone

tanshinone I

tanshinone IIA


Input: Social networks, web-based tools and diseases: implications for biomedical research.


Input: Advances in information technology have improved our ability to gather, collect and analyze information from individuals online.


Input: Social networks can be seen as a nonlinear superposition of a multitude of complex connections between people where the nodes represent individuals and the links between them capture a variety of different social interactions.


Input: The emergence of different types of social networks has fostered connections between individuals, thus facilitating data exchange in a variety of fields.


Input: Therefore, the question posed now is " can these same tools be applied to life sciences in order to improve scientific and medical research? " In this article, I will review how social networks and other web-based tools are changing the way we approach and track diseases in biomedical research.


Input: (-)-Carvone: antispasmodic effect and mode of action.

(-)-Carvone


Input: (-)-Carvone is a monoterpene ketone found in spearmint (Mentha spicata var. crispa) essential oil that is widely used as an odor and flavor additive.

(-)-Carvone

monoterpene ketone


Input: An intestinal antispasmodic effect was recently reported for (-)-carvone, and it has been shown to be more potent than its (+)-antipode.

(-)-carvone


Input: The mechanism of (-)-carvone action in the intestines has not been investigated.

(-)-carvone


Input: To gain a better understanding of the (-)-carvone antispasmodic effect, we investigated its pharmacological effects in the guinea pig ileum.

(-)-carvone


Input: Terminal portions of the ileum were mounted for isotonic contraction recordings.


Input: The effect of (-)-carvone was compared with that of the classical calcium channel blocker (CCB) verapamil.

(-)-carvone

calcium

verapamil


Input: In isolated ileal smooth muscle, (-)-carvone did not produce direct contractile or relaxation responses and did not modify electrically elicited contractions or low K (+)-evoked contractions.

(-)-carvone

K (+)


Input: The submaximal contractions induced by histamine (p < 0. 001), BaCl2 (p < 0. 05), and carbachol (p < 0. 01) were significantly reduced by (-)-carvone.

histamine

carbachol

(-)-carvone


Input: The contractile response elicited by high concentrations of carbachol was reduced but not abolished by (-)-carvone.

carbachol

(-)-carvone


Input: No additive action was detected with co-incubation of (-)-carvone and verapamil on carbachol-induced contraction.

(-)-carvone

verapamil

carbachol


Input: (-)-Carvone reduced the contraction induced by high K (+) and was almost 100 times more potent than verapamil.

(-)-Carvone

K (+)

verapamil


Input: Thus, (-)-carvone showed a typical and potent CCB-like action.

(-)-carvone


Input: Many effects described for both (-)-carvone and spearmint oil can be explained as a CCB-like mode of action.

(-)-carvone


Input: Mitochondrial electron transfer chain complexes inhibition by different organochalcogens.

organochalcogens


Input: Mitochondrial dysfunction plays a pivotal role in the cell toxicology and death decision.


Input: The aim of the present study was to investigate the effect of three organocompounds (ebselen [Ebs], diphenyl diselenide [(PhSe) (2)] and diphenyl ditelluride [(PhTe) (2)]) on mitochondrial complexes (I, II, I-III, II-III and IV) activity from rat liver and kidney to determine their potential role as molecular targets of organochalcogens.

diphenyl diselenide

(PhSe) (2)

diphenyl ditelluride

(PhTe) (2)

organochalcogens


Input: All studied organochalcogens caused a statistically significant inhibition of the mitochondrial complex I activity.

organochalcogens


Input: Ebs and (PhTe) (2) caused a statistically significant inhibition of the mitochondrial complex II activity in both hepatic and renal membranes.

(PhTe) (2)


Input: Hepatic mitochondrial complex II activity was practically unchanged by (PhSe) (2), whereas it significantly inhibited renal complex II activity.

(PhSe) (2)


Input: Mitochondrial complex IV activity was practically unchanged by the organochalcogens.

organochalcogens


Input: Furthermore, organochalcogens inhibited the mitochondrial respiration supported by complex I or complex II substrates.

organochalcogens


Input: The inhibitory effect of Ebs, (PhSe) (2) and (PhTe) (2) on mitochondrial complex I was prevented by NADH, but it was not prevented by catalase (CAT) and/or superoxide dismutase (SOD).

(PhSe) (2)

(PhTe) (2)

NADH

superoxide


Input: Additionally, the organochalcogens-induced inhibition of complex I and II was completely reversed by reduced glutathione (GSH).

organochalcogens

reduced glutathione

GSH


Input: In conclusion, Ebs, (PhSe) (2) and (PhTe) (2) were more effective inhibitors of renal and hepatic mitochondrial complex I than complex II, whereas complexes III and IV were little modified by these compounds.

(PhSe) (2)

(PhTe) (2)


Input: Taking into account the presented results, we suggest that organochalcogen-induced mitochondrial complexes I and II inhibition can be mediated by their thiol oxidation activity, i. e., Ebs, (PhSe) (2) and (PhTe) (2) can oxidize critical thiol groups from mitochondrial complexes I and II.

organochalcogen

thiol

(PhSe) (2)

(PhTe) (2)


Input: So, mitochondrial dysfunction can be considered an important factor in the toxicity of Ebs, (PhSe) (2) and (PhTe) (2).

(PhSe) (2)

(PhTe) (2)


Input: Estrogen receptor signaling as a target for novel breast cancer therapeutics.

Estrogen


Input: In breast cancer (BC) epithelial cells, the mitogenic action of estradiol is transduced through binding to two receptors, ER alpha and ER beta, which act as transcription factors.

estradiol


Input: Anti-estrogens (AEs) and aromatase inhibitors (AIs) are used clinically to arrest the estrogen-dependent growth of BC.

estrogens

estrogen


Input: In the case of AE or AI resistance, Herceptin or lapatinib may be used to inhibit growth factors.

lapatinib


Input: Estrogen effects are mediated not only through nuclear ERs but also through cytoplasmic/membrane ERs and G-protein-coupled ERs.

Estrogen


Input: These estrogen-binding systems associate with various proteins that direct cell cycle signaling, proliferation and survival.

estrogen


Input: The partners of nuclear ER include SRC1-3, HDACs and ER beta itself as well as newly identified proteins, such as E6-AP, LKB1, PELP1, PAX-2 and FOXA1.


Input: The partners of extra-nuclear ER alpha include PI3K and the tyrosine kinase Src.

tyrosine


Input: These various factors are all potential targets for therapeutic intervention.


Input: In addition, BC proliferation is enhanced by insulin and EGF, which stimulate signaling through the MAPK and PI3K/AKT pathways by activation of the IGF-1R and EGFR axes, respectively.


Input: These pathways are tightly interconnected with ER-activated signaling, and membrane ER alpha forms complexes with Src and PI3K.


Input: Chemokine-mediated signaling also modulates the estrogen response.

estrogen


Input: Inhibiting these pathways with specific inhibitors or activating some of the pathways by gene manipulation may be therapeutically valuable for arresting BC cell cycle progression and for inducing apoptosis to antagonize hormone-resistance.


Input: Here, we review some newly identified putatively targetable ER partners and highlight the need to develop tumor-targeting drug carrier systems affecting both the tumor cells and the tumor environment.


Input: Cytochrome P450-mediated herb-drug interaction potential of Galgeun-tang.


Input: We evaluated the herb-drug interaction potential of Galgeun-tang (GGT) extracts, mediated by cytochrome P450 (CYP) inhibition/induction.


Input: Further, the effects of fermentation on the CYP-mediated herb-drug interaction potential of GGT extracts were determined.


Input: As measured by LC-ESI/MS/MS, GGT extracts (0-300 mu g/mL) showed no inhibitory activity toward eight CYP isoforms (1A2, 2A6, 2B6, 2C9, 2C19, 2D6, 2E1, and 3A4) in pooled human liver microsomes, suggesting that GGT may have low potential for herb-drug interactions mediated by CYP inhibition.


Input: Hepatic CYP expression and activity in rats treated with GGT extracts twice per day for 1week was examined.


Input: Among the tested CYP isoforms (1A1, 1A2, 1B1, 2B1, 2C11, 2E1, 3A1, 3A2, and 4A1), CYP1B1 and 4A1 were increased by GGT extracts.


Input: Hepatic activities of 7-ethoxyresorufin-O-deethylase, 7-pentoxyresorufin-O-depentylase, and chlorzoxazone 6-hydroxylase, but not midazolam hydroxylase were also elevated.

O

O

chlorzoxazone

midazolam


Input: These results raise the possibility that GGT extracts may increase the toxicity of environmental toxicants through the elevating CYP-dependent metabolic activation.


Input: Interestingly, the increases in CYP1B1 and CYP4A1 levels, and 7-ethoxyresorufin-O-deethylase, 7-pentoxyresorufin-O-depentylase, and chlorzoxazone 6-hydroxylase activities were attenuated by fermentation of GGT extract using Lactobacillus plantarum KFRI 402, but not 144.

chlorzoxazone


Input: Further studies are needed to identify the CYP regulatory component (s) from GGT and determination its metabolism.


Input: Comparative study of equimolar doses of gamma-hydroxybutyrate (GHB), 1, 4-butanediol (1, 4-BD) and gamma-butyrolactone (GBL) on catalepsy after acute and chronic administration.

gamma-hydroxybutyrate

GHB

1, 4-butanediol

1, 4-BD

gamma-butyrolactone

GBL


Input: Gamma-hydroxybutyrate (GHB), and its precursors 1, 4-butanediol (1, 4-BD) and gamma-butyrolactone (GBL) are known drugs of abuse.

Gamma-hydroxybutyrate

GHB

1, 4-butanediol

1, 4-BD

GBL


Input: The ability of acute and chronic administration of equimolar doses of GHB (200mg/kg), 1, 4-BD (174mg/kg) and GBL (166mg/kg) to produce catalepsy in male Swiss Webster mice was examined.

GHB

1, 4-BD

GBL


Input: GHB, 1, 4-BD, GBL produced catalepsy when injected acutely.

GHB

1, 4-BD

GBL


Input: Drug treatment was then continued for 14days.


Input: Tolerance development was determined on days 6, 14, and challenged with a higher dose on day 15 in those chronically pretreated mice, and compared with na i ve mice.


Input: Chronic GHB produced tolerance to catalepsy, as evidenced from area under the curve (AUC) of catalepsy versus time (min-sec) on days 6 (678 +/- 254), 14 (272 +/- 247), which were less than those on day 1 (1923 +/- 269).

GHB


Input: However, less tolerance was seen from GBL or 1, 4-BD, as AUCs on days 6 and 14 were not significantly lower than that of day 1.

GBL

1, 4-BD


Input: In conclusion, although equimolar doses were used, expecting similar levels of GHB in the body, 1, 4-BD and GBL shared only some of the in vivo effects of GHB.

GHB

1, 4-BD

GBL

GHB


Input: The rate of metabolic conversion of 1, 4-BD and GBL into GHB might be responsible for the differences in the tolerance development to these drugs.

1, 4-BD

GBL

GHB


Input: Transient gestational and neonatal hypothyroidism-induced specific changes in androgen receptor expression in skeletal and cardiac muscles of adult rat.

androgen


Input: The present study aims to identify the association between androgen status and metabolic activity in skeletal and cardiac muscles of adult rats with transient gestational/neonatal-onset hypothyroidism.

androgen


Input: Pregnant and lactating rats were made hypothyroid by exposing to 0. 05% methimazole in drinking water; gestational exposure was from embryonic day 9-14 (group II) or 21 (group III), lactational exposure was from postnatal day 1-14 (group IV) or 29 (group V).

methimazole


Input: Serum was collected for hormone assay.


Input: Androgen receptor status, Glu-4 expression, and enzyme activities were assessed in the skeletal and cardiac muscles.

Androgen


Input: Serum testosterone and estradiol levels decreased in adult rats of groups II and III, whereas testosterone remained normal but estradiol increased in group IV and V, when compared to coeval control.

testosterone

estradiol

testosterone

estradiol


Input: Androgen receptor ligand binding activity increased in both muscle phenotypes with a consistent increase in the expression level of its mRNA and protein expressions except in the forelimb of adult rats with transient hypothyroidism (group II-V).

Androgen


Input: Glut-4 expression remained normal in skeletal and cardiac muscle of experimental rats.


Input: Specific activity of hexokinase and lactate dehydrogenase increased in both muscle phenotypes whereas, creatine kinase activity increased in skeletal muscles alone.

lactate

creatine


Input: It is concluded that transient gestational/lactational exposure to methimazole results in hypothyroidism during prepuberal life whereas it increases AR status and glycolytic activity in skeletal and cardiac muscles even at adulthood.

methimazole


Input: Thus, the present study suggests that euthyroid status during prenatal and early postnatal life is essential to have optimal AR status and metabolic activity at adulthood.


Input: Lung inflammatory effects, tumorigenesis, and emphysema development in a long-term inhalation study with cigarette mainstream smoke in mice.


Input: Cigarette smoking is the leading cause of lung cancer and chronic obstructive pulmonary disease, yet there is little mechanistic information available in the literature.


Input: To improve this, laboratory models for cigarette mainstream smoke (MS) inhalation-induced chronic disease development are needed.


Input: The current study investigated the effects of exposing male A/J mice to MS (6h/day, 5 days/week at 150 and 300 mg total particulate matter per cubic meter) for 2. 5, 5, 10, and 18 months in selected combinations with postinhalation periods of 0, 4, 8, and 13 months.


Input: Histopathological examination of step-serial sections of the lungs revealed nodular hyperplasia of the alveolar epithelium and bronchioloalveolar adenoma and adenocarcinoma.


Input: At 18 months, lung tumors were found to be enhanced concentration dependently (up to threefold beyond sham exposure), irrespective of whether MS inhalation had been performed for the complete study duration or was interrupted after 5 or 10 months and followed by postinhalation periods.


Input: Morphometric analysis revealed an increase in the extent of emphysematous changes after 5 months of MS inhalation, which did not significantly change over the following 13 months of study duration, irrespective of whether MS exposure was continued or not.


Input: These changes were found to be accompanied by a complex pattern of transient and sustained pulmonary inflammatory changes that may contribute to the observed pathogeneses.


Input: Data from this study suggest that the A/J mouse model holds considerable promise as a relevant model for investigating smoking-related emphysema and adenocarcinoma development.


Input: Identification of inhibitory scFv antibodies targeting fibroblast activation protein utilizing phage display functional screens.


Input: Fibroblast activation protein (FAP) is a serine protease selectively expressed on tumor stromal fibroblasts in epithelial carcinomas and is important in cancer growth, adhesion, and metastases.

serine


Input: As FAP enzymatic activity is a potent therapeutic target, we aimed to identify inhibitory antibodies.


Input: Using a competitive inhibition strategy, we used phage display techniques to identify 53 single-chain variable fragments (scFvs) after three rounds of panning against FAP.


Input: These scFvs were expressed and characterized for binding to FAP by surface plasmon resonance and flow cytometry.


Input: Functional assessment of these antibodies yielded an inhibitory scFv antibody, named E3, which could attenuate 35% of FAP cleavage of the fluorescent substrate Ala-Pro-7-amido-4-trifluoromethylcoumarin compared with nonfunctional scFv control.

Ala-Pro-7-amido-4-trifluoromethylcoumarin


Input: Furthermore, a mutant E3 scFv was identified by yeast affinity maturation.


Input: It had higher affinity (4-fold) and enhanced inhibitory effect on FAP enzyme activity (3-fold) than E3.


Input: The application of both inhibitory anti-FAP scFvs significantly affected the formation of 3-dimensional FAP-positive cell matrix, as demonstrated by reducing the fibronectin fiber orientation from 41. 18% (negative antibody control) to 34. 06% (E3) and 36. 15% (mutant E3), respectively.


Input: Thus, we have identified and affinity-maturated the first scFv antibody capable of inhibiting FAP function.


Input: This scFv antibody has the potential to disrupt the role of FAP in tumor invasion and metastasis.


Input: The velvet complex governs mycotoxin production and virulence of Fusarium oxysporum on plant and mammalian hosts.


Input: Fungal pathogens provoke devastating losses in agricultural production, contaminate food with mycotoxins and give rise to life-threatening infections in humans.


Input: The soil-borne ascomycete Fusarium oxysporum attacks over 100 different crops and can cause systemic fusariosis in immunocompromised individuals.


Input: Here we functionally characterized VeA, VelB, VelC and LaeA, four components of the velvet protein complex which regulates fungal development and secondary metabolism.


Input: Deletion of veA, velB and to a minor extent velC caused a derepression of conidiation as well as alterations in the shape and size of microconidia.


Input: VeA and LaeA were required for full virulence of F. oxysporum on tomato plants and on immunodepressed mice.


Input: A critical contribution of velvet consists in promoting chromatin accessibility and expression of the biosynthetic gene cluster for beauvericin, a depsipeptide mycotoxin that functions as a virulence determinant.

beauvericin

depsipeptide


Input: These results reveal a conserved role of the velvet complex during fungal infection on plants and mammals.


Input: Chemical constituents of Arisaema franchetianum tubers.


Input: A novel pyrrolidine alkaloid, (2R *, 3S *, 5S *)-N, 2-dimethyl-3-hydroxy-5-(10-phenyldecyl) pyrrolidine (1), and 17 known compounds were isolated from Arisaema franchetianum Engl.

pyrrolidine alkaloid

(2R *, 3S *, 5S *)-N, 2-dimethyl-3-hydroxy-5-(10-phenyldecyl) pyrrolidine


Input: (Araceae) tubers.


Input: The 17 compounds were bergenin (2), emodin (3), caffeic acid (4), nobiletin (5), 3-O-beta-d-galactopyranosyl-hederagenin 28-O-beta-d-xylopyranosyl (1 --> 6)-beta-d-galactopyranosyl ester (6), coniferin (7), qingyangshengenin (8), methylconiferin (9), syringaresinol 4'-O-beta-d-glucopyranoside (10), gagaminine (11), perlolyrine (12), (S)-1-(1'-hydroxyethyl)-beta-carboline (13), 1-(beta-carboline-1-yl)-3, 4, 5-trihydroxy-1-pentanone (14), 1-methoxycarbonyl-beta-carboline (15), indolo [2, 3-alpha] carbazole (16), 4-hydroxycinnamic acid methyl ester (17), and methyl 4-[2-hydroxy-2-(4-hydroxy-3-methoxyphenyl)-1-(hydroxymethyl) ethyl] ferulate (18).

bergenin

emodin

caffeic acid

nobiletin

3-O-beta-d-galactopyranosyl-hederagenin 28-O-beta-d-xylopyranosyl (1 --> 6)-beta-d-galactopyranosyl ester

coniferin

qingyangshengenin

methylconiferin

syringaresinol 4'-O-beta-d-glucopyranoside

gagaminine

perlolyrine

1-(beta-carboline-1-yl)-3, 4, 5-trihydroxy-1-pentanone

indolo [2, 3-alpha] carbazole

4-hydroxycinnamic acid methyl ester

methyl 4-[2-hydroxy-2-(4-hydroxy-3-methoxyphenyl)-1-(hydroxymethyl) ethyl] ferulate


Input: The inhibitory activities of compound 1 and its N-methyl derivative (1a) against porcine respiratory and reproductive syndrome virus (PRRSV), human leukemic K562 cells, and human breast cancer MCF-7 cells were evaluated.

N-methyl


Input: Compounds 1 [50% inhibited concentration (IC (50)) = 12. 5 +/- 0. 6 mu M] and 1a (IC (50) = 15. 7 +/- 0. 9 mu M) were cytotoxic against K562 cells.


Input: Compound 1a also had a weak effect on PRRSV with an IC (50) value of 31. 9 +/- 6. 0 mu M [selectivity index (SI) = 18. 7].


Input: Ameliorative effect of Drynaria quercifolia (L.) J.


Input: Sm., an ethnomedicinal plant, in arthritic animals.


Input: Drynaria quercifolia (L.) J.


Input: Sm., is an ethnomedicinal plant used widely in Tamil Nadu to treat arthritis.


Input: The present study was aimed to evaluate the traditional claim of D. quercifolia rhizome water extract in adjuvant induced arthritic animals.


Input: Anti-arthritic effect was studied by assessing the levels of lysosomal enzymes, protein bound carbohydrates, urinary degradative collagen and serum cytokines on control and adjuvant induced arthritis.

carbohydrates


Input: The paw swelling and body weight were also analyzed.


Input: The levels of ROS and lysosomal enzymes in neutrophils of control and adjuvant induced animals were also estimated.


Input: D. quercifolia rhizome water extract at doses of 100 and 200mg/kg reduced the paw thickness and elevated the mean body weight of arthritic rats.


Input: The treatment with extract showed a significant reduction in the levels of plasma and liver lysosomal enzymes as well as protein bound carbohydrates and urinary degradative collagen levels.


Input: The treatment reduced the levels of ROS and lysosomal enzymes in neutrophils significantly.


Input: The significant reduction in the levels of serum pro-inflammatory cytokines (TNF-alpha and IL-1 beta) and the increment in the levels of anti-inflammatory cytokine (IL-10) were also observed by the treatment.


Input: The present study supports the traditional claim of using D. quercifolia to treat rheumatism.


Input: On the origin of chirality in nanoplasmonic gyroid metamaterials.


Input: Metallic single gyroids, a new class of self-assembled nanoplasmonic metamaterials, are analyzed on the basis of a tri-helical metamaterial model.


Input: The physical mechanisms underlying the chiral optical behavior of the nanoplasmonic single gyroid are identified and it is shown that the optical chirality in this metallic structure is primarily determined by structural chirality and the connectivity of helices along the main cubic axes.


Input: Proximal femoral density distribution and structure in relation to age and hip fracture risk in women.


Input: Hip fracture risk rises exponentially with age, but there is little knowledge about how fracture-related alterations in hip structure differ from those of aging.


Input: We employed computed tomography (CT) imaging to visualize the three-dimensional (3D) spatial distribution of bone mineral density (BMD) in the hip in relation to age and incident hip fracture.


Input: We used intersubject image registration to integrate 3D hip CT images into a statistical atlas comprising women aged 21 to 97 years (n = 349) and a group of women with (n = 74) and without (n = 148) incident hip fracture 4 to 7 years after their imaging session.


Input: Voxel-based morphometry was used to generate Student' s t test statistical maps from the atlas, which indicated regions that were significantly associated with age or with incident hip fracture.


Input: Scaling factors derived from intersubject image registration were employed as measures of bone size.


Input: BMD comparisons of young, middle-aged, and older American women showed preservation of load-bearing cortical and trabecular structures with aging, whereas extensive bone loss was observed in other trabecular and cortical regions.


Input: In contrast, comparisons of older Icelandic fracture women with age-matched controls showed that hip fracture was associated with a global cortical bone deficit, including both the superior cortical margin and the load-bearing inferior cortex.


Input: Bone size comparisons showed larger dimensions in older compared to younger American women and in older Icelandic fracture women compared to controls.


Input: The results indicate that older Icelandic women who sustain incident hip fracture have a structural phenotype that cannot be described as an accelerated pattern of normal age-related loss.


Input: The fracture-related cortical deficit noted in this study may provide a biomarker of increased hip fracture risk that may be translatable to dual-energy X-ray absorptiometry (DXA) and other clinical images.


Input: Microfluidic investigation of BDNF-enhanced neural stem cell chemotaxis in CXCL12 gradients.


Input: In vivo studies have suggested that gradients of CXCL12 (aka stromal cell-derived factor 1 alpha) may be critical for neural stem cell (NSC) migration during brain development and neural tissue regeneration.


Input: However, traditional in vitro chemotaxis tools are limited by unstable concentration gradients and the inability to decouple cell migration directionality and speed.


Input: These limitations have restricted the reproducible and quantitative analysis of neuronal migration, which is required for mechanism-based studies.


Input: Using a microfluidic gradient generator, nestin and Sox-2 positive human embryonic NSC chemotaxis is quantified within a linear and stable CXCL12 gradient.


Input: While untreated NSCs are not able to chemotax within CXCL12 gradients, pre-treatment of the cells with brain-derived neurotrophic factor (BDNF) results in significant chemotactic, directional migration.


Input: BDNF pre-treatment has no effect on cell migration speed, which averages about 1 mu m min (-1).


Input: Quantitative analysis determines that CXCL12 concentrations above 9. 0 nM are above the minimum activation threshold, while concentrations below 14. 7 nM are below the saturation threshold.


Input: Interestingly, although inhibitor studies with AMD 3100 revealed that CXCL12 chemotaxis requires receptor CXCR4 activation, BDNF pre-treatment is found to have no profound effects on the mRNA levels or surface presentation of CXCR4 or the putative CXCR7 scavenger receptor.


Input: The microfluidic study of NSC migration within stable chemokine concentration profiles provides quantitative analysis as well as new insight into the migratory mechanism underlying BDNF-induced chemotaxis towards CXCL12.


Input: Modeling toxicity of binary metal mixtures (Cu (2 +)-Ag (+), Cu (2 +)-Zn (2 +)) to lettuce, Lactuca sativa, with the biotic ligand model.

Cu (2 +)-Ag (+)

Cu (2 +)-Zn (2 +)


Input: The biotic ligand model (BLM) was applied to predict metal toxicity to lettuce, Lactuca sativa.


Input: Cu (2 +) had the lowest median effective activity (EA50 (M)), compared with Ag (+) and Zn (2 +) (EA50 (Cu) = 2. 60 x 10 (-8) M, EA50 (Ag) = 1. 34 x 10 (-7) M, EA50 (Zn) = 1. 06 x 10 (-4) M).

Cu (2 +)

Ag (+)

Zn (2 +)

Cu

Ag

Zn


Input: At the 50% response level, the fraction of the total number of biotic ligands occupied by ions (f50 (M)) was lowest for Ag (+) among the metals (f50 (Ag) = 0. 22, f50 (Cu) = 0. 36, f50 (Zn) = 0. 42).

Ag (+)

Ag

Cu

Zn


Input: Cu (2 +) had the highest affinity for biotic ligands compared with Ag (+) and Zn (2 +), as shown by stability constants of the cation-biotic ligand binding, expressed as log K (MBL) (log K (CuBL) = 7. 40, log K (AgBL) = 6. 39, log K (ZnBL) = 4. 00).

Cu (2 +)

Ag (+)

Zn (2 +)

CuBL

AgBL

ZnBL


Input: Furthermore, the BLM was combined with the toxic equivalency factor approach in predicting toxicity of mixtures of Cu (2 +)-Zn (2 +) and Cu (2 +)-Ag (+).

Cu (2 +)-Zn (2 +)

Cu (2 +)-Ag (+)


Input: The fraction of biotic ligands occupied by ions was used to determine the relative toxic potency of metals and the toxic equivalency quotient (TEQ) of mixtures.


Input: This approach allowed for including interactions in estimating mixture toxicity and showed good predictive power (r (2) = 0. 64-0. 84).


Input: The TEQ at the 50% response level (TEQ50, Cu (2 +) equivalents) for Cu (2 +)-Zn (2 +) mixtures was significantly lower than the value for Cu (2 +)-Ag (+) mixtures.

Cu (2 +)

Cu (2 +)-Zn (2 +)

Cu (2 +)-Ag (+)


Input: Joint toxicity depended on both TEQ and specific composition of the mixture.


Input: The present study supports the use of the accumulation of metal ions at the biotic ligands as a predictor of toxicity of single metals and mixtures.


Input: Enantioselective toxicity and bioaccumulation of fipronil in fathead minnows (Pimephales promelas) following water and sediment exposures.

fipronil


Input: Fipronil is a widely used, broad-spectrum pesticide that is applied as an equal mixture of two enantiomers.

Fipronil


Input: As regulations on older pesticides become more stringent, production and application of fipronil is expected to grow, leading to increased inputs into aquatic environments and complex exposures to biota.

fipronil


Input: To better understand the potential exposures introduced by fipronil contamination, we conducted subchronic toxicity tests with larval fathead minnows (Pimephales promelas) and waterborne fipronil and its enantiomers and exposed juvenile fathead minnows to fipronil-spiked sediment.

fipronil

fipronil

fipronil


Input: Enantioselective toxicity was observed in fish after the 7-d subchronic exposure, with increased toxicity of the racemate and (+) enantiomer observed compared with the (-) enantiomer.


Input: Curiously, toxicities of the racemate and (+) enantiomer were not significantly different, even though the racemate contains 50% of the (+) enantiomer and 50% of the less toxic (-) enantiomer.


Input: During the sediment exposure, racemic fipronil in sediment was transformed primarily to fipronil sulfide, while exposed fish rapidly accumulated fipronil and/or fipronil sulfide and transformed the majority to fipronil sulfone.

fipronil

fipronil sulfide

fipronil

fipronil sulfide

fipronil sulfone


Input: Using the results of the sediment-exposure experiment, the authors explored a mechanism that may contribute to the interesting trends in enantioselective toxicity observed during the waterborne exposures.


Input: In tandem, the aquatic toxicity experiment and the spiked sediment exposure demonstrate the potentially complex behavior of fipronil in sediment and fish.

fipronil


Input: Large-scale production of edge-selectively functionalized graphene nanoplatelets via ball milling and their use as metal-free electrocatalysts for oxygen reduction reaction.

graphene

oxygen


Input: Edge-selectively functionalized graphene nanoplatelets (EFGnPs) with different functional groups were efficiently prepared simply by dry ball milling graphite in the presence of hydrogen, carbon dioxide, sulfur trioxide, or carbon dioxide/sulfur trioxide mixture.

graphene

graphite

hydrogen

carbon dioxide

sulfur trioxide

carbon dioxide

sulfur trioxide


Input: Upon exposure to air moisture, the resultant hydrogen-(HGnP), carboxylic acid-(CGnP), sulfonic acid-(SGnP), and carboxylic acid/sulfonic acid-(CSGnP) functionalized GnPs readily dispersed into various polar solvents, including neutral water.

hydrogen

carboxylic acid

sulfonic acid

carboxylic acid

sulfonic acid


Input: The resultant EFGnPs were then used as electrocatalysts for oxygen reduction reaction (ORR) in an alkaline electrolyte.

oxygen


Input: It was found that the edge polar nature of the newly prepared EFGnPs without heteroatom doping into their basal plane played an important role in regulating the ORR efficiency with the electrocatalytic activity in the order of SGnP > CSGnP > CGnP > HGnP > pristine graphite.

graphite


Input: More importantly, the sulfur-containing SGnP and CSGnP were found to have a superior ORR performance to commercially available platinum-based electrocatalyst.

sulfur

platinum


Input: The conjoint influence of home enriched environment and lead exposure on children' s cognition and behaviour in a Mexican lead smelter community.


Input: A range of studies has been conducted on the detrimental effects of lead in mining and smelting communities.


Input: The neurocognitive and behavioural health effects of lead on children are well known.


Input: This research characterized the conjoint influence of lead exposure and home enriched environment on neurocognitive function and behaviour for first-grade children living in a Mexican lead smelter community.


Input: Structural equation models were used for this analysis with latent outcome variables, Cognition and Behaviour, constructed based on a battery of assessments administered to the first-grade children, their parents, and teachers.


Input: Structural equation modelling was used to describe complex relationships of exposure and health outcomes in a manner that permitted partition of both direct and indirect effects of the factors being measured.


Input: Home Environment (a latent variable constructed from information on mother' s education and support of school work and extracurricular activities), and child blood lead concentration each had a main significant effect on cognition and behaviour.


Input: However, there were no statistically significant moderation relationships between lead and Home Environment on these latent outcomes.


Input: Home Environment had a significant indirect mediation effect between lead and both Cognition and Behaviour (p-value < 0. 001).


Input: The mediation model had a good fit with Root Mean Square Error of Approximation < 0. 0001 and a Weighted Root Mean Square Residual of 0. 895.


Input: These results were highly significant and suggest that Home Environment has a moderate mediation effect with respect to lead effects on Behaviour (beta = 0. 305) and a lower mediation effect on Cognition (beta = 0. 184).


Input: The extent of home enrichment in this study was most highly related to the mother' s support of schoolwork and slightly less by the mother' s support of extracurricular activities or mother' s education.


Input: Further research may be able to develop approaches to support families to make changes within their home and child rearing practices, or advocate for different approaches to support their child' s behaviour to reduce the impact of lead exposure on children' s cognitive and behavioural outcomes.


Input: Analysis of gene expression changes to elucidate the mechanism of chilling injury in precision-cut liver slices.


Input: The exact mechanism of chilling injury (by a decrease of temperature to sub-physiological values), especially in the intact organ, is yet unknown.


Input: Precision-cut liver slices (PCLS), which closely resemble the organ from which they are derived, are an ideal in vitro model to study the mechanism of chilling injury in the intact organ.


Input: In the present study we were able to separate chilling injury from other damaging events such as cryoprotectant toxicity and ice-crystal injury and performed micro-array analysis of regulated genes.


Input: Pathway analysis revealed that different stress responses, lipid/fatty acid and cholesterol biosynthesis and metabolism were affected by chilling.

fatty acid

cholesterol


Input: This indicates that the cell-membrane might be the primary site and sensor for chilling, which may initiate and amplify downstream intracellular signaling events.


Input: Most importantly, we were able to identify gene expression responses from stellate cells and Kupffer cells suggesting the involvement of all liver cell types in the injury.


Input: In conclusion, a broad spectrum of previously unknown gene expression changes induced by chilling was identified in the tissue.


Input: This is the first report of a systematic investigation on the mechanism of chilling injury in integrated tissue by micro-array analysis under conditions in which other sources of injury are minimal.


Input: Syntheses and in vitro evaluations of uncharged reactivators for human acetylcholinesterase inhibited by organophosphorus nerve agents.

organophosphorus


Input: Organophosphorus nerve agents (OPNAs) are highly toxic compounds that represent a threat to both military and civilian populations.

Organophosphorus


Input: They cause an irreversible inhibition of acetylcholinesterase (AChE), by the formation of a covalent P-O bond with the catalytic serine.

P-O

serine


Input: Among the present treatment of nerve agents poisoning, pyridinium and bis-pyridinium aldoximes are used to reactivate this inhibited enzyme but these compounds do not readily cross the blood brain barrier (BBB) due to their permanent cationic charge and thus cannot efficiently reactivate cholinesterases in the central nervous system (CNS).

pyridinium and bis-pyridinium aldoximes


Input: In this study, a series of seven new uncharged oximes reactivators have been synthesized and their in vitro ability to reactivate VX and tabun-inhibited human acetylcholinesterase (hAChE) has been evaluated.

oximes

tabun


Input: The dissociation constant KD of inhibited enzyme-oxime complex, the reactivity rate constant kr and the second order reactivation rate constant kr2 have been determined and have been compared to reference oximes HI-6, Obidoxime and 2-Pralidoxime (2-PAM).

oxime

oximes HI-6

Obidoxime


Input: Regarding the reactivation of VX-inhibited hAChE, all compounds show a better reactivation potency than those of 2-PAM, nevertheless they are less efficient than obidoxime and HI-6.

obidoxime


Input: Moreover, one of seven described compounds presents an ability to reactivate tabun-inhibited hAChE equivalent to those of 2-PAM.


Input: Theoretical investigation of a novel high density cage compound 4, 8, 11, 14, 15-pentanitro-2, 6, 9, 13-tetraoxa-4, 8, 11, 14, 15-pentaazaheptacyclo [5. 5. 1. 1 (3, 11). 1 (5, 9)] pentadecane.

4, 8, 11, 14, 15-pentanitro-2, 6, 9, 13-tetraoxa-4, 8, 11, 14, 15-pentaazaheptacyclo [5. 5. 1. 1 (3, 11). 1 (5, 9)] pentadecane


Input: A novel polynitro cage compound 4, 8, 11, 14, 15-pentanitro-2, 6, 9, 13-tetraoxa-4, 8, 11, 14, 15-pentaazaheptacyclo [5. 5. 1. 1 (3, 11). 1 (5, 9)] pentadecane (PNTOPAHP) has been designed and investigated at the DFT-B3LYP/6-31 (d) level.

4, 8, 11, 14, 15-pentanitro-2, 6, 9, 13-tetraoxa-4, 8, 11, 14, 15-pentaazaheptacyclo [5. 5. 1. 1 (3, 11). 1 (5, 9)] pentadecane

PNTOPAHP


Input: Properties, such as electronic structure, IR spectrum, heat of formation, thermodynamic properties and crystal structure have been predicted.


Input: This compound is most likely to crystallize in C2/c space group, and the corresponding cell parameters are Z = 8, a = 29. 78 A, b = 6. 42 A, c = 32. 69 A, alpha = 90. 00 degrees, beta = 151. 05 degrees, gamma = 90. 00 degrees and rho = 1. 94 g/cm (3).


Input: In addition, the detonation velocity and pressure have also been calculated by the empirical Kamlet-Jacobs equation.


Input: As a result, the detonation velocity and pressure of this compound are 9. 82 km/s, 44. 67 GPa, respectively, a little higher than those of 4, 10-dinitro-2, 6, 8, 12-tetraoxa-4, 10-diazaisowurtzitane (TEX, 9. 28 km/s, 40. 72 GPa).

4, 10-dinitro-2, 6, 8, 12-tetraoxa-4, 10-diazaisowurtzitane

TEX


Input: This compound has a comparable chemical stability to TEX, based on the N-NO (2) trigger bond length analysis.

TEX

N-NO (2)


Input: The bond dissociation energy ranges from 153. 09 kJ mol (-1) to 186. 04 kJ mol (-1), which indicates that this compound meets the thermal stability requirement as an exploitable HEDM.


Input: Benchmarks for 0-0 transitions of aromatic organic molecules: DFT/B3LYP, ADC (2), CC2, SOS-CC2 and SCS-CC2 compared to high-resolution gas-phase data.


Input: In the present study a benchmark set of medium-sized and large aromatic organic molecules with 10-78 atoms is presented.


Input: For this test set 0-0 transition energies measured in supersonic jets are compared to those calculated with DFT and the B3LYP functional, ADC (2), CC2 and the spin-scaled CC2 variants SOS-CC2 and SCS-CC2.


Input: Geometries of the ground and excited states have been optimized with these methods in polarized triple zeta basis sets.


Input: Zero-point vibrational corrections have been calculated with the same methods and basis sets.


Input: In addition the energies have been corrected by single point calculations with a triple zeta basis augmented with diffuse functions, aug-cc-pVTZ.


Input: The deviations of the theoretical results from experimental electronic origins, which have all been measured in the gas phase with high-resolution techniques, were evaluated.


Input: The accuracy of SOS-CC2 is comparable to that of unscaled CC2, whereas ADC (2) has slightly larger errors.


Input: The lowest errors were found for SCS-CC2.


Input: All correlated wave function methods provide significantly better results than DFT with the B3LYP functional.


Input: The effects of the energy corrections from the augmented basis set and the method-consistent calculation of the zero-point vibrational corrections are small.


Input: With this benchmark set reliable reference data for 0-0 transition energies for larger organic chromophores are available that can be used to benchmark the accuracy of other quantum chemical methods such as new DFT functionals or semi-empirical methods for excitation energies and structures and thereby augments available benchmark sets augments present benchmark sets which include mainly smaller molecules.


Input: Emergency do not consume/do not use concentrations for ferric chloride in drinking water.

ferric chloride


Input: The U. S.


Input: Congress [PL 107-188] amended the Safe Drinking Water Act and required each community water system serving more than 3, 000 people to conduct vulnerability assessments.


Input: These assessments address potential circumstances that could compromise the safety and reliability of municipal water.


Input: Ferric chloride is used in coagulation and flocculation, and it is used to treat raw water with high viral loads, elevated dissolved solids or high bromide.

Ferric chloride

bromide


Input: Iron is an essential nutrient, but elevated concentrations of FeCl3 are corrosive as a result of hydrolysis to HCl.

Iron

HCl


Input: Based on a no-observed-adverse effect level (NOAEL) of 0. 5% FeCl3 * 6H2O administered in drinking water to male and female F344 rats for up to 2 years, a do not consume concentration of 200 mg FeCl3/L can be derived.

FeCl3 * 6H2O


Input: Since instillation of 0. 3 M (48. 7 g/L) FeCl3 in saline to rodent vagina failed to elicit damage, a topical do not use concentration of 2000 mg FeCl3/L (600 mg Fe/L) can be assigned.

Fe


Input: The only FeCl3 data available to quantify ocular toxicity involved a pH 1 solution in rabbit eyes, but HCl instillation (pH 2. 5) to rabbit eyes found permanent corneal ulceration after 10 min.

HCl


Input: The pH of FeCl3 in water at the do not use limit (2. 4-2. 6) is near the pH (2. 0) considered corrosive by regulatory agencies.


Input: As direct eye contact with water at pH 4. 5 or below increases complaints of ocular discomfort, emergency response plans that address FeCl3 in drinking water must account for Fe levels and the pH of the affected water.

Fe


Input: Toxicity of cadmium and protective effect of bee honey, vitamins C and B complex.

cadmium

vitamins C and B


Input: The present work aimed to study the toxic effect of cadmium (Cd) on rabbits' blood indices, as well as the therapeutic effect of the antioxidant agents, vitamins C and B complex and bee honey on Cd intoxicated rabbits.

cadmium

Cd

vitamins C and B

Cd


Input: Cadmium chloride (CdCl2) was injected subcutaneously at a dose of 3 mg/kg of body weight.

Cadmium chloride


Input: The results showed a significant increase in serum glucose, triglycerides, cholesterol, total protein, albumin, globulin, urea and creatinine, compared to the control group.

glucose

triglycerides

cholesterol

urea

creatinine


Input: In addition, CdCl2 intoxication increased the levels of uric acid, aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase and bilirubin.

uric acid

aspartate

alanine

bilirubin


Input: Concerning haematological parameters, the more obvious changes were an increase in mean corpuscular volume and a decrease in white blood cells count, platelets, lymphocytes, heamatocrit, haemoglobin and red blood cells count.


Input: Treatment of CdCl2-intoxicated animals with vitamins C and B complex and bee honey showed a decrease in the harmful effects of Cd by restoring haematological and biochemical changes.

vitamins C and B

Cd


Input: Bee honey treatment was the most effective in providing recoveries in the altered blood parameters.


Input: Estimation of BDNF gene polymorphism and predisposition to dependence development for selected psychoactive compounds: genetic aspects of addiction with the selected drugs, amphetamine, tetrahydrocannabinol and opiates.

amphetamine

tetrahydrocannabinol


Input: The etiology of drug addiction, a central nervous system (CNS) disease, is not fully known.


Input: This complex problem is believed to be connected with concurrently affecting genetic, psychological and environmental factors.


Input: The development of addiction is connected with CNS reinforcement system and dopaminergic neurotransmission.


Input: Molecular processes are postulated to be of universal character and allow to presume a similar mechanism of dependence for both ethanol and other substances.

ethanol


Input: Therefore, elements of dopaminergic transmission become excellent candidates for the examination of genetic influence on the development of addiction.


Input: A relationship between alcoholic disease and the presence of TaqIA1 and DRD2 alleles permits to initiate another investigation of gene-coding DRD2 dopamine receptor.


Input: The latest results indicate the importance of brain-derived neurotrophic factor (BDNF) in the regulation of dopaminergic route.


Input: The purpose of this research was to reveal the relationship between the Val66Met BDNF gene polymorphism and dependence of psychoactive agent.


Input: The examinations were performed with the Local Research Ethics Committee approval and patient' s consent.


Input: The study group consisted of 100 patients (88 men and 12 women) aged 18-52 years, qualified for research program according to the International Classification of Diseases, Tenth Revision (ICD-10) requirements, medical examination and detailed questionnaire.


Input: Low cytotoxic elastic niosomes loaded with salmon calcitonin on human skin fibroblasts.


Input: A low cytotoxic elastic niosomal formulation loaded with salmon calcitonin was developed.


Input: The elastic niosomes were prepared from Tween 61 mixed with cholesterol at various concentrations of the edge activators (sodium cholate (NaC) and sodium deoxycholate (NaDC); 0. 25, 0. 5, 2. 5, 5 and 10% mole) or ethanol (10-30% v/v).

Tween 61

cholesterol

sodium cholate

NaC

sodium deoxycholate

NaDC

ethanol


Input: The effects of the niosomal concentrations (5, 10 and 20 mM) and phosphate buffer at pH 7. 0 (5, 10, 20 and 30 mM) on the physical characteristics of niosomes were investigated.

phosphate


Input: The 5 mM elastic niosomes in 5 mM phosphate buffer containing calcitonin 0. 22 mg/mL gave the highest elasticity (deformability index (DI)) at 6. 79 +/- 2. 03 determined by the extrusion method.

phosphate


Input: The blank elastic niosomes comprised 2. 5% mole NaDC, 5% mole NaC or 20% v/v ethanol showed the highest elasticity.

NaDC

NaC

ethanol


Input: The 5% mole NaC elastic niosomes loaded with calcitonin gave the highest DI (21. 59 +/- 0. 91) and percentages of calcitonin entrapment efficiency (60. 11 +/- 4. 98).

NaC


Input: This study has demonstrated that this NaC elastic niosome did not only reduce the cytotoxicity of the loaded calcitonin but also gave superior cell viability to the ethanolic elastic niosome as well.

NaC


Input: Two cases of acute dexmedetomidine withdrawal syndrome following prolonged infusion in the intensive care unit: Report of cases and review of the literature.

dexmedetomidine


Input: Prolonged infusion of dexmedetomidine, an alpha (2)-adrenoreceptor agonist anesthetic used in the intensive care unit, produces a withdrawal syndrome of sympathetic over-activity, characterized by tachycardia, hypertension and agitation, but there is no recommended standard treatment for this syndrome.

dexmedetomidine


Input: We describe two patients with a clinical diagnosis of acute dexmedetomidine withdrawal and its management with oral clonidine.

dexmedetomidine

clonidine


Input: We utilized the principle of managing acute drug withdrawal with longer acting medications.


Input: These two cases demonstrated the benefit of using oral, longer acting clonidine to manage acute withdrawal from shorter-acting, intravenous dexmedetomidine.

clonidine

dexmedetomidine


Input: Effects of hypothermia on the disposition of morphine, midazolam, fentanyl, and propofol in intensive care unit patients.

morphine

midazolam

fentanyl

propofol


Input: Therapeutic hypothermia (TH) may induce pharmacokinetic changes that may affect the level of sedation.


Input: We have compared the disposition of morphine, midazolam, fentanyl, and propofol in TH with normothermia in man.

morphine

midazolam

fentanyl

propofol


Input: Fourteen patients treated with TH following cardiac arrest (33-34 degrees C) were compared with eight matched critically ill patients (36-38 degrees C).


Input: Continuous infusions of morphine and midazolam were stopped and replaced with infusions of fentanyl and propofol to describe elimination and start of infusion pharmacokinetics, respectively.

morphine

midazolam

fentanyl

propofol


Input: Serial serum and urine samples were collected for 6-8 hours for validated quantification and subsequent pharmacokinetic analysis.


Input: During TH, morphine elimination half-life (t (1/2)) was significantly higher, while total clearance (CL (tot)) was significantly lower (median [semi-interquartile range (s-iqr)]): t (1/2), 266 (43) versus 168 (11) minutes, P < 0. 01; CL (tot), 1201 (283) versus 1687 (200) ml/min, P < 0. 01.

morphine


Input: No significant differences were seen for midazolam.

midazolam


Input: CL (tot) of fentanyl and propofol was significantly lower in hypothermic patients [median (s-iqr)]: fentanyl, 726 (230) versus 1331 (678) ml/min, P < 0. 05; propofol, 2046 (305) versus 2665 (223) ml/min, P < 0. 05.

fentanyl

propofol

fentanyl

propofol


Input: Compared with the matched, normothermic intensive care unit patients, t (1/2) of morphine was significantly higher during TH.

morphine


Input: CL (tot) was lower during TH for morphine, fentanyl, and propofol but not for midazolam.

morphine

fentanyl

propofol

midazolam


Input: Reducing the infusion rates of morphine, fentanyl, and propofol during TH is encouraged.

morphine

fentanyl

propofol


Input: STAAR: statistical analysis of aromatic rings.


Input: The statistical analysis of aromatic rings program allows for an automated search for anion-pi interactions between phenylalanine residues and carboxylic acid moieties of neighboring aspartic acid or glutamic acid residues in protein data bank (PDB) structures.

phenylalanine

carboxylic acid

aspartic acid

glutamic acid


Input: The program is written in C + + and is available both as a standalone code and through a web implementation that allows users to upload and analyze biomolecular structures in PDB format.


Input: The program outputs lists of Phe/Glu or Phe/Asp pairs involved in potential anion-pi interactions, together with geometrical (distance and angle between the Phe' s center of mass and Glu or Asp' s center of charge) and energetic (quantum mechanical Kitaura-Morokuma interaction energy between the residues) descriptions of each anion-pi interaction.

Phe

Glu

Phe

Asp

Phe

Glu

Asp


Input: Application of the program on the latest content of the PDB shows that anion-pi interactions are present in thousands of protein structures and can possess strong energies, as low as-8. 72 kcal/mol.


Input: BET bromodomain proteins mediate downstream signaling events following growth factor stimulation in human lung fibroblasts and are involved in bleomycin-induced pulmonary fibrosis.

bleomycin


Input: Epigenetic alterations, such as histone acetylation, regulate the signaling outcomes and phenotypic responses of fibroblasts after growth factor stimulation.


Input: The bromodomain and extra-terminal domain-containing proteins (Brd) bind to acetylated histone residues, resulting in recruitment of components of the transcriptional machinery and subsequent gene transcription.


Input: Given the central importance of fibroblasts in tissue fibrosis, this study sought to determine the role of Brd proteins in human lung fibroblasts (LFs) after growth factor stimulation and in the murine bleomycin model of lung fibrosis.

bleomycin


Input: Using small interfering RNA against human Brd2 and Brd4 and pharmacologic Brd inhibitors, this study found that Brd2 and Brd4 are essential in mediating the phenotypic responses of LFs downstream of multiple growth factor pathways.


Input: Growth factor stimulation of LFs causes increased histone acetylation, association of Brd4 with growth factor-responsive genes, and enhanced transcription of these genes that could be attenuated with pharmacologic Brd inhibitors.


Input: Of note, lung fibrosis induced after intratracheal bleomycin challenge in mice could be prevented by pretreatment of animals with pharmacologic inhibitors of Brd proteins.

bleomycin


Input: This study is the first demonstration of a role for Brd2 and Brd4 proteins in mediating the responses of LFs after growth factor stimulation and in driving the induction of lung fibrosis in mice in response to bleomycin challenge.

bleomycin


Input: Hydrogen sulfide as an allosteric modulator of ATP-sensitive potassium channels in colonic inflammation.

Hydrogen sulfide

ATP

potassium


Input: The ATP-sensitive potassium channel (K (ATP)) in mouse colonic smooth muscle cell is a complex containing a pore-forming subunit (Kir6. 1) and a sulfonylurea receptor subunit (SUR2B).

ATP

potassium

K

ATP

sulfonylurea


Input: These channels contribute to the cellular excitability of smooth muscle cells and hence regulate the motility patterns in the colon.


Input: Whole-cell voltage-clamp techniques were used to study the alterations in K (ATP) channels in smooth muscle cells in experimental colitis.

K

ATP


Input: Colonic inflammation was induced in BALB/C mice after intracolonic administration of trinitrobenzene sulfonic acid.

trinitrobenzene sulfonic acid


Input: K (ATP) currents were measured at a holding potential of-60 mV in high K (+) external solution.

K

ATP

K (+)


Input: The concentration response to levcromakalim (LEVC), a K (ATP) channel opener, was significantly shifted to the left in the inflamed smooth-muscle cells.

levcromakalim

LEVC

K

ATP


Input: Both the potency and maximal currents induced by LEVC were enhanced in inflammation.

LEVC


Input: The EC (50) values in control were 6259 nM (n = 10) and 422 nM (n = 8) in inflamed colon, and the maximal currents were 9. 9 +/- 0. 71 pA/pF (60 mu M) in control and 39. 7 +/- 8. 8 pA/pF (3 mu M) after inflammation.


Input: As was seen with LEVC, the potency and efficacy of sodium hydrogen sulfide (NaHS) (10-1000 mu M) on K (ATP) currents were significantly greater in inflamed colon compared with controls.

LEVC

sodium hydrogen sulfide

NaHS

K

ATP


Input: In control cells, pretreatment with 100 micro M NaHS shifted the EC (50) for LEV-induced currents from 2838 (n = 6) to 154 (n = 8) nM.

NaHS


Input: Sulfhydration of sulfonylurea receptor 2B (SUR2B) was induced by NaHS and colonic inflammation.

sulfonylurea

NaHS


Input: These data suggest that sulfhydration of SUR2B induces allosteric modulation of K (ATP) currents in colonic inflammation.

K

ATP


Input: Stem cell lineage commitment by electrical fields and the potential application in drug discovery.


Input: Stem cells may be applied to improve the efficiency of drug discovery, but more effective protocols are first required to control the differentiation.


Input: Recent researches have revealed that physical stimulation is an important avenue for stem cell lineage commitment, such as electrical field stimulation.


Input: Here, we review literatures about stem cell differentiation by electrical field stimulation.


Input: Various forms of electrical fields with soluble induction factors have shown to produce a synergistic effect in order to enhance the osteogenic commitment.


Input: Moreover, electrical field stimulation alone shows marked effects of pre-commitment to cardiomyocyte and neuron.


Input: However, the related precise molecular regulatory mechanism is unclear.


Input: As cardiomyocyte and neuron are crucial factors in drug development process, electrical field stimulation may be proposed as an effect important for stem cell differentiation, exhibiting a potential application in drug discovery.


Input: In vivo DNA electrotransfer for immunotherapy of cancer and neurodegenerative diseases.


Input: Electroporation is the process commonly referred to the transient increase in the permeability of cell membranes on submission to electric field pulses.


Input: Electroporation has become an increasingly extensive method to enhance in vivo DNA delivery for both gene therapy applications as well as for delivery of DNA vaccines, mostly against cancer.


Input: In vivo gene electrotransfer is of special interest since it is the most efficient non-viral strategy for gene delivery and it is worthy of low manufacturing costs, ease of realization and favorable safety profile.


Input: No adverse findings observed in toxicology and biodistribution/integration studies have been warranted for the evaluation of this approach in humans.


Input: Therefore, gene delivery followed by electroporation is currently being investigated in several clinical trials.


Input: The positive outcomes of early studies suggest that the efficacy of gene delivery and immunogenicity has greatly improved by electroporation.


Input: This review briefly summarizes salient features and recent findings that have contributed to the rapid progress of electroimmunotherapy as well as an overview of advanced clinical studies in oncology.


Input: Translation of in vivo DNA electrovaccination for neurodegenerative diseases as well as future expectations are also discussed.


Input: Multivalent agents: a novel concept and preliminary practice in Anti-HIV drug discovery.


Input: The term multivalency (polyvalency) in the biological science is defined as the simultaneous binding of multiple ligands to one receptor (or multiple receptors to one ligand).


Input: The possibility of gaining potency and selectivity was significantly increased through the use of multivalent ligand as a homo-or hetero-dimer, thus multivalent ligands provided a more attractive strategy to design novel anti-HIV agents with therapeutic applications.


Input: Moreover, similar to phenomenon of multivalency, an alternative strategy is called the " mixed sites inhibitor ", viz.


Input: a single molecule that possesses enough chemical space to maximize interactions with its complementary binding pocket, or to bind simultaneously in more than one regions in a target.


Input: Actually, the addition of a third heterocyclic nucleus to the parent compound resulted in " mixed sites " anti-HIV agents with broad spectrum of activities against the mutant HIV-1 strains.


Input: Based on current representative examples, the present article provided a brief review on the rationale for the design of different classes of multivalency anti-HIV agents and also discussed the advantages over their monomeric counterparts, providing a novel paradigm to facilitate the development of anti-HIV/AIDS therapeutic agents in treatment of HIV infected community.


Input: Rosmarinic acid ameliorates acute liver damage and fibrogenesis in carbon tetrachloride-intoxicated mice.

Rosmarinic acid

carbon tetrachloride


Input: The aim of this study was to investigate the therapeutic potential of rosmarinic acid (RA), a natural phenolic, in the treatment of acute liver toxicity.

rosmarinic acid


Input: RA at 10, 25 and 50mg/kg was administered by gavage once daily for 2 consecutive days, 6h after CCl (4) intoxication.

CCl (4)


Input: CCl (4) intoxication caused hepatic necrosis and increased serum ALT activity.

CCl (4)


Input: In the livers, oxidative/nitrosative stress was evidenced by increased 3-nitrotyrosine (3-NT) and thiobarbituric acid reactive substances (TBARS) formation and a significant decrease in Cu/Zn superoxide dismutase (SOD) activity.

thiobarbituric acid

Cu

Zn superoxide


Input: CCl (4) administration triggered inflammatory response in mice livers by activating nuclear factor-kappaB (NF-kappa B), which coincided with the induction of tumor necrosis factor-alpha (TNF-alpha) and cyclooxygenase-2 (COX-2).

CCl (4)


Input: RA improved histological and serum markers of liver damage and significantly ameliorated oxidative/nitrosative stress and inflammatory response in liver tissue.


Input: Additionally, RA prevented transforming growth factor-beta1 (TGF-beta 1) and alpha-smooth muscle actin (alpha-SMA) expression, suggesting suppression of profibrotic response.


Input: Furthermore, RA significantly inhibited the CCl (4)-induced apoptosis, which was evident from decreased cleavage of caspase-3.

CCl (4)


Input: The hepatoprotective activity of RA coincided with enhanced NF-E2-related factor 2 (Nrf2) and heme oxygenase-1 (HO-1) expression.


Input: The results of this study indicates that RA possesses antioxidant, anti-inflammatory, antiapoptotic and antifibrotic activity against acute liver toxicity.


Input: The relationship between bone marrow characteristics and the clinical prognosis of antithyroid drug-induced agranulocytosis.


Input: This study is aimed to explore the relationship between bone marrow characteristics and clinical prognosis of antithyroid drug (ATD) induced agranulocytosis.


Input: A retrospective study was conducted in the first affiliated hospital of the University of South China.


Input: A total of 33 hospitalized patients diagnosed with ATD-induced agranulocytosis were analyzed.


Input: The bone marrow characteristics were classified into two types.


Input: Type I was characterized by reduction or absence of granulocytic precursors and type II was recognized as hypercellular bone marrow with dysmaturity of granulocytic cells.


Input: Bone marrow of 20 cases (61%) were characterized with type I whereas 13 cases (39%) with type II.


Input: The median duration of neutrophil recovery and high-grade fever were 4. 7 +/- 1. 0 days and 3. 6 +/- 2. 5 days respectively for type II, compared to 8. 0 +/- 2. 8 days and 8. 6 +/- 3. 1 days for type I (p < 0. 01 in both compared groups).


Input: However, there was no significant difference between the two types in terms of age, median duration of drug administration before the diagnosis of agranulocytosis, the amount of neutrophil count on admission and the total administration dose of granulocyte-colony stimulating factor (G-CSF) before bone marrow examination.


Input: Two cases of type I died of complications from infection.


Input: This study showed that the bone marrow characteristics of ATD-induced agranulocytosis could be classifed into two types.


Input: Also, the clinical prognosis was closely related to the bone marrow features.


Input: Type I is the dominant type which is usually associated with worse clinical prognosis compared to type II.


Input: Impact of Charcot neuroarthropathy on metatarsal bone mineral density and geometric strength indices.


Input: Charcot neuroarthropathy (CN), an inflammatory condition characterized by rapid and progressive destruction of pedal bones and joints, often leads to deformity and ulceration in individuals with diabetes mellitus (DM) and peripheral neuropathy (PN).


Input: Repetitive, unperceived joint trauma may trigger initial CN damage, causing a proinflammatory cascade that can result in osteolysis and contribute to subsequent neuropathic fracture.


Input: We aimed to characterize osteolytic changes related to development and progression of CN by measuring bone mineral density (BMD) and geometric strength indices using volumetric quantitative computed tomography.


Input: Twenty individuals with DM + PN were compared to twenty age-, sex-, and race-matched individuals with DM + PN and acute CN.


Input: We hypothesized that individuals with acute CN would have decreased BMD and decreased total area, cortical area, minimum section modulus, and cortical thickness in the diaphysis of the second and fifth metatarsals.


Input: Results showed BMD was lower in both involved and uninvolved feet of CN participants compared to DM + PN participants, with greater reductions in involved CN feet compared to uninvolved CN feet.


Input: There was a non-significant increase in total area and cortical area in the CN metatarsals, which helps explain the finding of similar minimum section modulus in DM + PN and CN subjects despite the CN group' s significantly lower BMD.


Input: Larger cortical area and section modulus are typically considered signs of greater bone strength due to higher resistance to compressive and bending loads, respectively.


Input: In CN metatarsals, however, these findings may reflect periosteal woven bone apposition, i. e., a hypertrophic response to injury rather than increased fracture resistance.


Input: Future research using these techniques will aid further understanding of the inflammation-mediated bony changes associated with development and progression of CN and other diseases.


Input: Orexin-A suppresses postischemic glucose intolerance and neuronal damage through hypothalamic brain-derived neurotrophic factor.

glucose


Input: Orexin-A (a glucose-sensing neuropeptide in the hypothalamus) and brain-derived neurotrophic factor (BDNF; a member of the neurotrophin family) play roles in many physiologic functions, including regulation of glucose metabolism.

glucose

glucose


Input: We previously showed that the development of postischemic glucose intolerance is one of the triggers of ischemic neuronal damage.

glucose


Input: The aim of this study was to determine whether there was an interaction between orexin-A and BDNF functions in the hypothalamus after cerebral ischemic stress.


Input: Male ddY mice were subjected to 2 hours of middle cerebral artery occlusion (MCAO).


Input: Neuronal damage was estimated by histologic and behavioral analyses.


Input: Expression of protein levels was analyzed by Western blot.


Input: Small interfering RNA directed BDNF, orexin-A, and SB334867 [N-(2-methyl-6-benzoxazolyl)-N'-1, 5-naphthyridin-4-yl urea; a specific orexin-1 receptor antagonist] were administered directly into the hypothalamus.

N-(2-methyl-6-benzoxazolyl)-N'-1, 5-naphthyridin-4-yl urea


Input: The level of hypothalamic orexin-A, detected by immunohistochemistry, was decreased on day 1 after MCAO.


Input: Intrahypothalamic administration of orexin-A (1 or 5 pmol/mouse) significantly and dose-dependently suppressed the development of postischemic glucose intolerance on day 1 and development of neuronal damage on day 3.

glucose


Input: The MCAO-induced decrease in insulin receptor levels in the liver and skeletal muscle on day 1 was recovered to control levels by orexin-A, and this effect of orexin-A was reversed by the administration of SB334867 as well as by hypothalamic BDNF knockdown.


Input: These results suggest that suppression of postischemic glucose intolerance by orexin-A assists in the prevention of cerebral ischemic neuronal damage.

glucose


Input: In addition, hypothalamic BDNF may play an important role in this effect of orexin-A.


Input: Role of 5-hydroxytryptamine 1B (5-HT1B) receptors in the regulation of ethanol intake in rodents.

ethanol


Input: Evidence indicates that the serotonergic system is important in mediating dependence on and craving for alcohol.

alcohol


Input: Among serotonin receptors, 5-hydroxytryptamine 1B (5-HT1B) receptors have been associated with drug abuse including alcohol.

serotonin

alcohol


Input: In this review, the neurocircuitry involving 5-HT1B receptors in central reward brain regions related to alcohol intake are discussed in detail.

alcohol


Input: Emphasis has been placed on the pharmacological manipulations of 5-HT1B receptor-mediated alcohol intake.

alcohol


Input: Furthermore, 5-HT1B auto-and hetero-receptors regulate alcohol intake through the regulatory mechanism involving release of 5-HT, gamma-aminobutyric acid (GABA), dopamine, and glutamate is evaluated.

alcohol

gamma-aminobutyric acid

GABA

dopamine

glutamate


Input: Thus, interactions between 5-HT1B receptors and these neurotransmitter systems are suggested to modulate alcohol-drinking behavior.

alcohol


Input: This review on the role of 5-HT1B receptors in neurotransmitter release and consequent alcohol intake provides important information about the potential therapeutic role of 5-HT1B receptors for the treatment of alcohol dependence.

alcohol

alcohol


Input: In vivo and in vitro characterization of naltrindole-derived ligands at the kappa-opioid receptor.

naltrindole


Input: Accumulating evidence supports a role for kappa-opioid receptor antagonists in the treatment of mood disorders.


Input: Standard kappa-antagonists have an unusual pharmacodynamic action, with a single injection blocking receptor signaling for several weeks.


Input: Here, we have characterized the kappa-selective properties of two ligands, 5'-(2-aminomethyl) naltrindole (5'-AMN) and N-((Naltrindol-5-yl) methyl) pentanimidamide (5'-MABN), to identify whether modifications of the naltrindole side chain produces short-acting kappa-antagonists.

5'-(2-aminomethyl) naltrindole

N-((Naltrindol-5-yl) methyl) pentanimidamide

naltrindole


Input: Opioid receptor binding affinity and activity were assessed using [(3) H]-diprenorphine binding, guanosine-5'-O-(3-[35S]-thio) triphosphate ([(35) S]-GTP gamma S) binding and isolated guinea-pig ileum.

[(3) H]-diprenorphine

guanosine-5'-O-(3-[35S]-thio) triphosphate

[(35) S]-GTP gamma S


Input: Pharmacodynamic profiles of 5'-AMN and 5'-MABN (1-10 mg/kg) were investigated using the tail-withdrawal assay and diuresis.


Input: Efficacy was also determined in depression-and anxiety-related behavioral paradigms in CD-1 mice.


Input: Both 5'-AMN and 5'-MABN had high affinity for kappa-receptors (K (i) 1. 36 +/- 0. 98 and 0. 27 +/- 0. 08, respectively) and were revealed as potent kappa-antagonists (pA (2) 7. 43 and 8. 18, respectively) and mu-receptor antagonists (pA (2) 7. 62 and 7. 85, respectively) in the ileum.


Input: Contrary to our hypothesis, in vivo, 5'-AMN and 5'-MABN displayed long-lasting antagonist effects in mice, reducing the antinociceptive actions of U50, 488 (10 mg/kg) at 28 and 21 days post-injection, respectively.

U50, 488


Input: Interestingly, while 5'-AMN and 5'-MABN were not kappa-selective, both compounds did show significant antidepressant-and anxiolytic-like effects at 7-14 days post-injection in mice.


Input: EGR1 is critical for gastrin-dependent upregulation of anion exchanger 2 in gastric cancer cells.


Input: The essential anion exchanger (AE) involved in bicarbonate secretion is AE2/SLC4A2, a membrane protein recognized to be relevant for the regulation of the intracellular pH in several cell types.

bicarbonate


Input: Here we report that gastrin, a major gastrointestinal hormone, upregulates the expression of AE2 mRNA and protein in a cholecystokinin B receptor dependent manner in gastric cancer cells.


Input: The upregulated species of AE2 mRNA originates from the classical upstream promoter of the AE2 gene (here referred to as AE2a1) which provides the binding site for transcription factors early growth response 1 (EGR1) and SP1.


Input: EGR1 upregulated the AE2 expression that can be competitively inhibited by SP1 in co-transfection experiments.


Input: This competitive inhibition was avoided in cells because the SP1 expression was time-staggered to EGR1 in response to gastrin.


Input: Overexpression or knockdown of EGR1 consistently increased or decreased the expression of AE2.


Input: Our data linked a novel signal pathway involved in gastrin-stimulated AE2 expression.


Input: Synthesis and evaluation of a series of 3, 4, 5-trimethoxycinnamic acid derivatives as potential antinarcotic agents.

3, 4, 5-trimethoxycinnamic acid


Input: A series of 3, 4, 5-trimethoxycinnamic acid derivatives was prepared and evaluated for antinarcotic effects on morphine dependence in mice and binding affinities on serotonergic receptors.

3, 4, 5-trimethoxycinnamic acid

morphine


Input: The key synthetic strategies involve generation of ketones 6-7, esters 9-12 through condensation reaction, and amides 13-19 via coupling reaction using 1-hydroxybenzotriazole/ethyl (dimethylaminopropryl) carbodiimide system in high yield.

ketones

esters

amides

ethyl (dimethylaminopropryl) carbodiimide


Input: We found that the naloxone-induced morphine withdrawal syndrome was significantly suppressed by new synthetic 3, 4, 5-trimethoxycinnamic acid derivatives (20 mg/kg/day).

naloxone

morphine

3, 4, 5-trimethoxycinnamic acid


Input: Most of 3, 4, 5-trimethoxycinnamic acid derivatives were found to have high affinity to 5-HT (1A) receptor.

3, 4, 5-trimethoxycinnamic acid


Input: The naloxone-induced morphine withdrawal syndrome was attenuated by (+) 8-OH-DPAT (0. 1 mg/kg/day, i. p.), a 5-HT (1A) receptor agonist.

naloxone

morphine

(+) 8-OH-DPAT


Input: In cortical neuronal cells, (+) 8-OH-DPAT (1 mu M) produced an elevation of the pERK 1/2 expression, and the elevated pERK levels were inhibited by WAY 100635, a 5-HT (1A) receptor-specific antagonist.

(+) 8-OH-DPAT

WAY 100635


Input: Interestingly, the pERK levels were increased by the 3, 4, 5-trimethoxycinnamic acid derivatives and the derivatives-mediated changes in pERK levels were blocked by the WAY 100635.

3, 4, 5-trimethoxycinnamic acid

WAY 100635


Input: These results suggested that new synthetic 3, 4, 5-trimethoxycinnamic acid derivatives have a potential antinarcotic effect through acting as a 5-HT (1A) receptor agonist in mice.

3, 4, 5-trimethoxycinnamic acid


Input: A novel mechanism for the promotion of quercetin glycoside absorption by megalo alpha-1, 6-glucosaccharide in the rat small intestine.

quercetin glycoside


Input: The presence of an alpha-1, 6-glucosaccharide enhances absorption of water-soluble quercetin glycosides, a mixture of quercetin-3-O-beta-d-glucoside (Q3G, 31. 8%), mono (23. 3%), di (20. 3%) and more d-glucose adducts with alpha-1, 4-linkage to a d-glucose moiety of Q3G, in a ligated small intestinal loop of anesthetized rats.

quercetin glycosides

d-glucose

d-glucose


Input: We prepared alpha-1, 6-glucosaccharides with different degrees of polymerization (DP) enzymatically and separated them into a megalo-isomaltosaccharide-containing fraction (M-IM, average DP = 11. 0) and an oligo-isomaltosaccharide-containing fraction (O-IM, average DP = 3. 6).


Input: Luminal injection of either saccharide fraction promoted the absorption of total quercetin-derivatives from the small intestinal segment and this effect was greater for M-IM than O-IM addition.

saccharide

quercetin


Input: M-IM also increased Q3G, but not the quercetin aglycone, concentration in the water-phase of the luminal contents more strongly than O-IM.

quercetin


Input: The enhancement of Q3G solubilization in the luminal contents may be responsible for the increases in the quercetin glucoside absorption promoted by alpha-1, 6-glucosaccharides, especially that by M-IM.

quercetin glucoside


Input: These results suggest that the ingestion of alpha-1, 6-glucosaccharides promotes Q3G bioavailability.


Input: alpha-Glucosidase inhibitor from Buthus martensi Karsch.


Input: A bioassay-guided fractionation of an ethanol extract of Buthus martensi Karsch led to the isolation of a potent alpha-glucosidase inhibitor (compound S).

ethanol


Input: The structure was elucidated as a novel beta-carboline glucoalkaloid, harmanyl beta-d-glucopyranoside, on the basis of spectral data, including (1) H NMR, (13) C NMR, (1) H-(1) H COSY, NOESY, and HMBC.

beta-carboline glucoalkaloid

harmanyl beta-d-glucopyranoside

(1) H

(13) C

(1) H

(1) H


Input: Compound S showed potent inhibitory activity against alpha-glucosidase, with an IC (50) value of 24 mu M.


Input: A Lineweaver-Burk plot indicated that its inhibition of alpha-glucosidase was uncompetitive, with a Ki value of 16. 1 mu M.


Input: Thermal stability of yeast hydrolysate as a novel anti-obesity material.


Input: We examined the thermal stability of yeast hydrolysates before and after ultrafiltration (UF) in vitro, and the anti-obesity activity of yeast hydrolysates before and after heat treatment in vivo.


Input: Yeast hydrolysate after UF showed significantly higher thermal stability than before UF.


Input: Yeast hydrolysates before and after UF showed 3 and 4 thermal transition peaks in their thermograms, respectively, and the total thermal denaturation enthalpies of yeast hydrolysates before and after UF were 69. 5 and 36. 5 J/g, respectively.


Input: For the anti-obesity activity study, yeast hydrolysates before and after heating were administered ad libitum with water to 7-week-old male SD rats.


Input: The administration of yeast hydrolysate (YH-control; no heat treatment, YH-1; heat treatment at 140 degrees C, and YH-2; heat treatment at 160 degrees C) significantly increased mRNA expression of cocaine-and amphetamine-regulated transcript (CART) compared with control rats (saline administration).

cocaine

amphetamine


Input: However, there was no significant difference between the heat-treated groups and YH-control and there was no significant difference in neuropeptide Y expression between the heat-treated groups and YH-control.


Input: These results suggest that yeast hydrolysate can be use an anti-obesity material after heat treatment.


Input: Lipid components prepared from a freshwater Clam (Corbicula fluminea) extract ameliorate hypercholesterolaemia in rats fed high-cholesterol diet.


Input: To explore the hypocholesterolaemic components in the fat fraction of freshwater clam extract (FCE), we further fractionated the fat fraction by silica gel column chromatography into nine fat subfractions.

silica gel


Input: In the present study, we used exogenous hypercholesterolaemic rats induced by feeding a high-cholesterol diet; the doses of the added fat subfractions were equivalent to those in 30% FCE.


Input: Two (FF1, FF2) out of the nine fat subfractions strongly reduced serum cholesterol levels in the rats fed a high-cholesterol diet.

cholesterol

cholesterol


Input: Both FF1 and FF2 up-regulated the hepatic gene expression of cholesterol 7 alpha-hydroxylase, a rate-limiting enzyme of bile acid biosynthesis.

cholesterol

bile acid


Input: Thin-layer chromatography showed that FF1 primarily contained sphingolipids, while FF2 mainly contained triacylglycerols and sterol esters.

sphingolipids

triacylglycerols

sterol esters


Input: These results indicate that fractions containing sphingolipids, triacylglycerols, and sterol esters are possibly responsible for the hypocholesterolaemic action in a novel manner through the up-regulation of the hepatic biosynthesis of bile acids.

sphingolipids

triacylglycerols

sterol esters


Input: Separation and purification of sulforaphene from radish seeds using macroporous resin and preparative high-performance liquid chromatography.

sulforaphene


Input: This present study described a rapid and cost-effective method for the separation and purification of natural sulforaphene from radish seeds by SP-700 macroporous resin and preparative high-performance liquid chromatography (HPLC).

sulforaphene


Input: Sulforaphene with high purity and recovery was obtained by preparative HPLC with a C18 column and 30% methanol in ultra-pure water as the mobile phase.

Sulforaphene

methanol


Input: 12. 5 kg of radish seeds, which contained 87. 5 g of sulforaphene, produced 117. 5 g of sulforaphene-rich extract of 65. 8% sulforaphene after primary separation by SP-700 macroporous resin.

sulforaphene

sulforaphene

sulforaphene


Input: 5. 9 g of 96. 5% sulforaphene was obtained from 9. 5 g of the sulforaphene-rich extract after purification by preparative HPLC.

sulforaphene

sulforaphene


Input: The purified compound was assessed by analytical HPLC and characterised by ESI/MS, (1) H NMR and (13) C NMR.

(1) H

(13) C


Input: Standard curve was developed using the purified sulforaphene to allow quantification of sulforaphene in the extracts of radish seeds by analytical HPLC.

sulforaphene

sulforaphene


Input: Bacillus cereus AR156 induces resistance against Rhizopus rot through priming of defense responses in peach fruit.


Input: The biocontrol effects of Bacillus cereus AR156 on Rhizopus rot caused by Rhizopus stolonifer in postharvest peach fruit and the possible mechanisms were investigated.


Input: The results showed that fruit treated with B. cereus AR156 had significantly lower disease incidence and smaller lesion diameter than the control fruit did.


Input: B. cereus AR156 treatment remarkably enhanced activities of chitinase and beta-1, 3-glucanase, promoted accumulation of H (2) O (2), and improved total phenolic content and 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical-scavenging activity.

H (2) O (2)

2, 2-diphenyl-1-picrylhydrazyl

DPPH


Input: Transcripts of four defense related genes were only significantly enhanced in fruit both treated with B. cereus AR156 and inoculated with R. stolonifer compared with those that were only treated with B. cereus AR156 or inoculated with R. stolonifer.


Input: These results suggest that B. cereus AR156 can effectively inhibit Rhizopus rot caused by R. stolonifer and enhance antioxidant activity in peach fruit through the priming of defense responses.


Input: Discrimination against diacylglycerol ethers in lipase-catalysed ethanolysis of shark liver oil.

diacylglycerol ethers


Input: Lipase-catalysed ethanolysis of squalene-free shark liver oil was investigated.

squalene


Input: The mentioned shark liver oil was comprised mainly of diacylglycerol ether and triacylglycerols.

diacylglycerol ether

triacylglycerols


Input: In order to test discrimination against diacylglycerol ether, up to 10 different lipases were compared.

diacylglycerol ether


Input: The ratio of oil to ethanol and lipase stability were also evaluated.

ethanol


Input: Surprisingly, lipase from Pseudomonas stutzeri was the fastest biocatalyst among all assayed, although poor discrimination against diacylglycerol ether was observed.

diacylglycerol ether


Input: The best results in terms of selectivity and stability were obtained with immobilised lipase from Candida antarctica (Novozym 435).


Input: Ethanolysis reaction after 24h in the presence of Novozym 435 produced total disappearance of triacylglycerol and a final reaction mixture comprised mainly of diacylglycerol ethers (10. 6%), monoacylglycerol ethers (32. 9%) and fatty acid ethyl esters (46. 0%).

triacylglycerol

diacylglycerol ethers

monoacylglycerol ethers

fatty acid ethyl esters


Input: In addition, when an excess of ethanol was used, diacylglycerol ethers completely disappeared after 15 h, giving a final product mainly composed of monoacylglycerol ethers (36. 6%) and fatty acid ethyl esters (46. 4%).

ethanol

diacylglycerol ethers

monoacylglycerol ethers

fatty acid ethyl esters


Input: Sustainable production of pectin from lime peel by high hydrostatic pressure treatment.


Input: The application of high hydrostatic pressure technology for enzymatic extraction of pectin was evaluated.


Input: Cellulase and xylanase under five different combinations (cellulase/xylanase: 50/0, 50/25, 50/50, 25/50, and 0/50 U/g lime peel) at ambient pressure, 100 and 200 MPa were used to extract pectin from dried lime peel.


Input: Extraction yield, galacturonic acid (GalA) content, average molecular weight (M (w, ave)), intrinsic viscosity [eta] (w), and degree of esterification (DE) were compared to those parameters obtained for pectins extracted using acid and aqueous processes.

galacturonic acid

GalA


Input: Pressure level, type and concentration of enzyme significantly (p < 0. 05) influenced yield and DE of pectin.


Input: Enzyme and high pressure extraction resulted in yields which were significantly (p < 0. 05) higher than those using acid and aqueous extraction.


Input: Although pressure-induced enzymatic treatment improves pectin yield, it does not have any significant effect on M (w, ave) and [eta] (w) of pectin extracts indicating the potential of high pressure treatment for enzymatic pectin production as a novel and sustainable process.


Input: Introduction and nutritional evaluation of germinated soy germ.


Input: Germinated soy germ (GSG) were developed and evaluated for their nutritional value.


Input: Separated soy germ was germinated at room temperature for 24h under running water.


Input: As germination progressed, the protein and fibre content of GSG increased slightly, while the lipid and carbon to nitrogen (C/N) ratio decreased; free amino acids including GABA increased considerably while free sugars decreased.

carbon

nitrogen

C

N

amino acids

GABA

sugars


Input: Linoleic and linolenic acid were the most abundant unsaturated fatty acids in soy germ, and slight changes were observed in GSG.

Linoleic and linolenic acid

unsaturated fatty acids


Input: The tocopherol and isoflavone contents showed a rapid increase of 32. 4% and 27. 9%, respectively, during germination.

tocopherol

isoflavone


Input: The abundance of GABA, isoflavones and tocopherols demonstrates the high nutritional value of GSG and suggests that GSG can be utilised as a reasonable and effective source of healthy foods.

GABA

isoflavones

tocopherols


Input: Chemical and sensory effects of the freezing process on the aroma profile of black truffles (Tuber melanosporum).


Input: The aim of this work was to evaluate the effect of freezing black truffles (Tuber melanosporum) on their aroma both in sensory and chemical terms.


Input: The truffles were frozen at temperatures of-20 to-80 degrees C.


Input: Descriptive and discriminative sensory and chemical analyses, based on headspace solid phase microextraction followed by gas chromatography-mass spectrometry analysis (HS-SPME-GC-MS), were carried out after 1, 20, 40 and 60 days.


Input: Fifteen compounds with high aromatic potential in truffles were determined.


Input: Their selective ion peak areas were calculated, summed and expressed as percentage of active odour compound, in order to monitor changes in odour profile.


Input: The aroma of frozen truffles differed significantly from the aroma of fresh truffles.


Input: Volatile composition data revealed that T. melanosporum aromatic profile is deeply modified as a consequence of a freezing process.


Input: These aromatic changes could explain the loss of freshness observed in all frozen truffles.


Input: Methional and some phenols were suggested as markers of freezing time.

Methional

phenols


Input: Interestingly, 1-octen-3-one appeared as a general marker of freezing process.


Input: GC/MS analysis of volatiles obtained by headspace solid-phase microextraction and simultaneous-distillation extraction from Rabdosia serra (MAXIM.) HARA leaf and stem.


Input: Volatiles in Rabdosia serra were investigated by headspace solid phase microextraction (HS-SPME) and simultaneous-distillation extraction (SDE).


Input: The HS-SPME technique was previously evaluated to optimise sampling conditions.


Input: A total of 56 and 48 compounds including alcohols, aldehydes, hydrocarbons, ketones, carboxylic acid, ester, and aromatics were identified in leaf and stem by optimised HS-SPME method (CAR/PDMS fibre; incubation time, 10 min; extraction temperature, 50 degrees C; extraction time, 40 min), respectively.

alcohols

aldehydes

hydrocarbons

ketones

carboxylic acid

ester


Input: 1-Octen-3-ol and (2E)-hexenal had significant contribution to R. serra aroma.


Input: Cluster analysis indicated that leaf and stem exhibited different volatile diversity.


Input: Air drying was favourable for the retention of the volatiles, while freeze-and sun-drying led to the loss of volatiles.


Input: SDE method preferred to the analysis of compounds with low volatility including fatty acids and esters.

fatty acids

esters


Input: HS-SPME was a useful technique for the analysis of readily volatile components for the characteristics of R. serra aroma.


Input: Novel angiotensin I-converting enzyme inhibitory peptides derived from soya milk.


Input: Inhibitors of angiotensin I-converting enzyme (ACE) are useful in treating hypertension, and many have been derived from food products, including soybeans.


Input: Using the industrial protease PROTIN SD-NY10, we developed a processed soya milk (PSM) with enhanced ACE inhibitory activity.


Input: The ACE inhibitory activity of PSM (IC (50) = 0. 26 mu g/ml) was greater than that of regular soya milk (IC (50) = 8. 75 mu g/ml).


Input: Eight novel ACE inhibitory peptides were purified from PSM by reversed-phase chromatography: FFYY (IC (50), 1. 9 mu M), WHP (4. 8 mu M), FVP (10. 1 mu M), LHPGDAQR (10. 3 mu M), IAV (27. 0 mu M), VNP (32. 5 mu M), LEPP (100. 1 mu M), and WNPR (880. 0 mu M).


Input: The IC (50) values of these peptides are comparable to those reported for other ACE inhibitory peptides derived from wheat, chicken, bonito, wine, etc.


Input: Due to the relatively low IC (50) values of several peptides identified in this study, they may serve as ideal base components of food supplements for patients with hypertension.


Input: Non-target screening of Allura Red AC photodegradation products in a beverage through ultra high performance liquid chromatography coupled with hybrid triple quadrupole/linear ion trap mass spectrometry.

Allura Red AC


Input: The study deals with the identification of the degradation products formed by simulated sunlight photoirradiation in a commercial beverage that contains Allura Red AC dye.

Allura Red AC


Input: An UHPLC-MS/MS method, that makes use of hybrid triple quadrupole/linear ion trap, was developed.


Input: In the identification step the software tool information dependent acquisition (IDA) was used to automatically obtain information about the species present and to build a multiple reaction monitoring (MRM) method with the MS/MS fragmentation pattern of the species considered.


Input: The results indicate that the identified degradation products are formed from side-reactions and/or interactions among the dye and other ingredients present in the beverage (ascorbic acid, citric acid, sucrose, aromas, strawberry juice, and extract of chamomile flowers).

ascorbic acid

citric acid

sucrose


Input: The presence of aromatic amine or amide functionalities in the chemical structures proposed for the degradation products might suggest potential hazards to consumer health.

aromatic amine or amide


Input: Maple polyphenols, ginnalins A-C, induce S-and G2/M-cell cycle arrest in colon and breast cancer cells mediated by decreasing cyclins A and D1 levels.

polyphenols

ginnalins A-C


Input: Polyphenols are bioactive compounds found in plant foods.

Polyphenols


Input: Ginnalins A-C are polyphenols present in the sap and other parts of the sugar and red maple species which are used to produce maple syrup.

Ginnalins A-C

polyphenols

sugar


Input: Here we evaluated the antiproliferative effects of ginnalins A-C on colon (HCT-116) and breast (MCF-7) tumourigenic and non-tumourigenic colon (CCD-18Co) cells and investigated whether these effects were mediated through cell cycle arrest and/or apoptosis.

ginnalins A-C


Input: Ginnalins A-C were twofold more effective against the tumourigenic than non-tumourigenic cells.

Ginnalins A-C


Input: Among the polyphenols, ginnalin A (84%, HCT-116; 49%, MCF-7) was more effective than ginnalins B and C (50%, HCT-116; 30%, MCF-7) at 50 mu M concentrations.

polyphenols

ginnalin A

ginnalins B and C


Input: Ginnalin A did not induce apoptosis of the cancer cells but arrested cell cycle (in the S-and G (2)/M-phases) and decreased cyclins A and D1 protein levels.

Ginnalin A


Input: These results suggest that maple polyphenols may have potential cancer chemopreventive effects mediated through cell cycle arrest.

polyphenols


Input: Hair mercury levels and food consumption in residents from the Pearl River Delta: South China.

mercury


Input: The Pearl River Delta (PRD) is located in the Southern part of China and is the main region for fish culture in Guangdong Province.


Input: In order to assess the potential health risks associated with dietary consumption of mercury, hair samples from 91 urban, town and fishing village residents, 37 species of fish, cereal, vegetables, and meat samples were collected.

mercury


Input: The average total mercury (THg) and methylmercury (MeHg) concentrations in hair were 1. 08 +/- 0. 94 and 0. 58 +/- 0. 59 mu g/g, respectively.

mercury

methylmercury

MeHg


Input: Daily Hg intake via fish consumption is significantly correlated with THg and MeHg accumulated in human hair (r = 0. 48, p < 0. 01; r = 0. 43, p < 0. 01).

Hg

MeHg


Input: The estimated daily intake of Hg via different food types showed that both fish and cereal consumption were the two main routes of Hg exposure for residents in the sampling areas.

Hg

Hg