UK PubMed Central (United Kingdom)

Mechanism-based inhibition of cytochrome P450 (CYP) 3A4 is characterized by NADPH-, time-, and concentration-dependent enzyme inactivation, occurring when some drugs are converted by CYPs to reactive...Full Text Available

UK PubMed Central (United Kingdom)

A cDNA encoding a cytochrome P450 enzyme was isolated from a cDNA library of the corpora allata (CA) from reproductively active Diploptera punctata cockroaches. This P450 from the endocrine...Full Text Available

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A cytochrome P450 that hydroxylates lauric acid at the 12 position (P450LA omega) was isolated from liver microsomes of clofibrate treated rats. P450LA omega was immunologically distinct from P450s a,b,c,d,e,f,g,h,j,PB1, and PCN1. Polyclonal antibody against P450LA omega was utilized to screen a gt11 cDNA library. A clone (pP450LA omega), was isolated and its sequence determined. The P450LA omega mRNA is a minimum 2387 nts in length and codes for a P450 of Mr.58,222 daltons. This protein shares less than 35% amino acid similarity with P450s b,c,d,e,f,PB1, and PCN1; however, it does contain a hydrophobic amino ...

International Nuclear Information System (INIS)

Three cDNAs, designated IIA3, IIA3v, and IIA4, coding for P450s in the CYP2A gene subfamily were isolated from a #lambda#gt11 library prepared from human hepatic mRNA. Only three nucleotide differences and a single amino acid difference, Leu"1"6"0#->#His, were found between IIA3 and IIA3v, indicating that they are probably allelic variants. IIA4 displayed 94% amino acid similarity with IIA3 and IIA3v. The three cDNAs were inserted into vaccinia virus, and recombinant viruses were used to infect human hepatoma Hep G2 cells. Only IIA3 was able to produce an enzyme that had a reduced CO-bound spectrum with a #lambda#_m_a_x at 450 nm. This expressed enzyme was able to carry out coumarin 7-hydroxylation and ethoxycoumarin O-deethylation. cDNA-expressed IIA3v and IIA4 failed to incorporate heme and were enzymatically inactive. Analysis of IIA proteins in human liver microsomes, using antibody against rat IIA2, revealed two ...

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Both increased cell proliferation and {open_quotes}altered{close_quotes}CYP gene expression are prominent phenomena associated with liver tumor promotion by nongenotoxic carcinogen treatment. BRDU-labeled parenchymal nuclei were observed primarily in the periportal area of groups of rats, independent of nongenotoxic carcinogen treatment. Treatment with each of the 5 nongenotoxic carcinogens resulted in profound alterations in CPY gene expression at both the transcriptional and translational levels. Expression of CYP1A1, 1A1/2, 3A1, 2B1/2, and 4A immunoproteins demonstrated nongenotoxic carcinogen-specific patterns in both magnitude and zonal distribution. In agreement with the CYP immunoprotein data, treatment with each of the five nongenotoxic carcinogens resulted in a unique composition of mRNAs of CYP2B1, 2B2, 2C6, 2C11, 3A1, 3A2, and 4A1, which were variably ...

UK PubMed Central (United Kingdom)

BackgroundTransposons, i.e. transposable elements (TEs), are the major internal spontaneous mutation agents for the variability of eukaryotic genomes. To address the general issue...Full Text Available

UK PubMed Central (United Kingdom)

Protection afforded by trialkyl phosphorothionates against the lung injury caused by trialkyl phosphorothiolates probably results from the inhibition by the P = S moiety of the thionates, of one or...Full Text Available

UK PubMed Central (United Kingdom)

During the treatment of neonatal apnea, formula-fed infants, compared to breastfed infants, show nearly three-fold increase in clearance of caffeine, a substrate...Full Text Available

UK PubMed Central (United Kingdom)

BackgroundABCA3 transporter (ATP-binding cassette transporter of the A subfamily) is localized to the limiting...Full Text Available

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Estrogen metabolism is suggested to play an important role in estrogen-induced breast carcinogenesis. Epidemiologic studies suggest that diets rich in phytoestrogens are associated with a reduced risk of breast cancer. Phytoestrogens are biologically active plant compounds that structurally mimic 17b-estradiol (E2). We hypothesize that phytoestrogens, may provide protection against breast carcinogenesis by altering the expression of estrogen-metabolizing enzymes cytochrome P450 1A1 (Cyp1A1) and 1B1 (Cyp1B1). Cyp1A1 and Cyp1B1 are responsible for the metabolism of E2 to generate 2-hydroxyestradiol (2-OHE2) and 4-hydroxyestradiol (4-OHE2), respectively. Studies suggest that 2-OHE2 and 2-methoxyestradiol may protect against breast carcinogenesis, while 4-OHE2 is carcinogenic in rodent models....

UK PubMed Central (United Kingdom)

N-Hydroxy-N′-(4-n-butyl-2-methylphenyl)formamidine (HET0016) is a potent inhibitor of 20-hydroxyeicosatetraenoic acid (20-HETE) formation by specific cytochrome P450 (CYP) isoforms....Full Text Available

UK PubMed Central (United Kingdom)

Sensory rhodopsins (SRs) belong to a subfamily of heptahelical transmembrane proteins containing a retinal chromophore. These photoreceptors mediate the cascade of vision in animal eyes and phototaxis...Full Text Available

UK PubMed Central (United Kingdom)

Reversion-induced LIM protein (RIL) is a member of the ALP (actinin-associated LIM protein) subfamily of the PDZ/LIM protein family. RIL serves as an adaptor protein and seems to regulate cytoskeletons....Full Text Available

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Background & AimsMolecular mechanisms underlying alcoholic liver disease (ALD) are still not fully understood. Activating transcription factor-4 (ATF4) is the master coordinator of the integrated stress response (ISR), an adaptive pathway triggered by multiple stressors. which can promote cell death and induce metabolic dysregulation if the stress is intense or prolonged. The aim of this study was to assess the effect of alcohol on the ISR signaling pathway in human liver cells and to define the role of cytochrome P450 2E1 (CYP2E1) in this response. MethodsPrimary cultured human hepatocytes and human HepG2 cells over-expressing CYP2E1 by adenoviral infection were exposed to ethanol (25-100mM) for 8-48h. ResultsEthanol treatment of both liver cells up-regulated ATF4 as well as the pro-survi...

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Upon irradiation of aqueous ethylene glycol/water solutions of native chloroperoxidase (CPO) with {sup 60}Co-gamma rays at 77K one observes the one-electron reduction of the enzyme active site by radiolytically generated thermolyzed electrons. In the present study the first absorption spectrum of a low-spin ferrous form of CPO is reported which has peaks at 438, 532 and 563 nm, similar to those observed previously for cytochrome P-450. All previously described ferrous forms of CPO are high spin. In order to observe the final results of the CPO reaction with electrons, the spectral changes of native enzyme after room temperature-gamma-irradiation have also been investigated. Evidence of changes is also presented probably connected with disruption of the tertiary structure of enzyme, correlated with decrease of enzyme activity.

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4-Methylcoumarins that possess two hydroxyl groups ortho to each other in the benzenoid ring have shown to have excellent antioxidant and radical-scavenging properties in different experimental models. Furthermore, they cannot be metabolized by the liver P450 monoxygenases and thus cannot form 3,4-coumarin epoxides, which are believed to be mutagenic. Herein, we present a study on the structure activity relationship of eight synthetic 4-methylcoumarins, carried out by employing a series of different chemical cell-free tests. These compounds were tested by means of three assays involving one redox reaction with the oxidant (DPPH assay, ABTS+ assay and FRAP). Other assays were employed to evaluate the antioxidant properties of the coumarins under investigation against NO, O2- and HClO, which...

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Although polybrominated naphthalenes (PBNs) are contaminants of the commercial fire retardant fireMaster BP-6, the individual PBN isomers have not been identified. In order to study PBNs possessing an analogous level of bromination to those found in fireMaster BP-6, three synthetic PBN mixtures, averaging 5.0, 5.3, and 5.6 bromines per naphthalene were synthetized and partially characterized. The PBN mixtures were administered to immature male Wistar rats and found to be potent inducers of cytochrome P-450-dependent monooxygenases. At the lowest dose tested, 30 mumol X kg-1, each PBN mixture caused maximal induction of benzo(a)pyrene hydroxylase activity. On the basis of enzyme activities, ligand-binding spectra and sodium dodecyl sulfate-polyacrylamide gel electrophoresis, the PBN mixtures were determined to be 3-methylcholanthrene-type inducers of cytochrome P-450 (P-448), resembling qualitatively the ...

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Sunflower combined shaft unit Rankine cycle turboalternator

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We present the low-temperature physical properties of the polycrystalline perovskite systems La2/3A1/3Mn1-xCoxO3, A=Ca, Sr (0.5x1) including electrical resistance, magnetization, ac and dc susceptibilities. The experimental data suggest the presence of correlated ferromagnetic clusters embedded in some non-ferromagnetic matrix. The systems show semiconducting behavior and negative magnetoresistance.

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Variation for wheat (Triticum aestivum L.) grain yield and its component traits was documented in a `Cheyenne¿ x Cheyenne (`Wichita¿ 3A) recombinant inbred chromosome line population. In the present study, a population of 223 Cheyenne (Wichita 3A) recombinant inbred chromosome lines was used to map ...

International Nuclear Information System (INIS)

An assay for the microsomal hydroxylation of lauric acid (LA), based on HPLC with flow-through radiochemical detection, has been developed. Conditions were optimized for resolution and quantitation of three microsomal metabolites of "1"4C-LA, one of which has not been reported previously as a metabolite of LA in mammalian microsomal incubations. These products, 12-(omega)-hydroxy-LA, 11-(omega-1)-hydroxy-LA, and a novel metabolite, 10-(omega-2)-hydroxy-LA, were isolated by HPLC and identified by gas chromatography/mass spectrometry. In the presence of NADPH, the formation of all three metabolites was linear with time and microsomal protein concentration. Hydrogen peroxide also supported the microsomal metabolism of LA, although the ratio of metabolites was substantially different than that produced by NADPH-supported microsomes. Several biochemical probes (metyrapone, #alpha#-naphthoflavone, 2-diethylaminoethyl-2,2-diphenylvalerate hydrochloride, and 10-undecynoic acid) were used to ...

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Eremostachys laciniata (L) Bunge (family: Lamiaceae alt. Labiatae; subfamily: Lamioideae) is one of the 15 endemic Iranian herbs of the genus Eremostachys. A decoction of the roots and flowers of E. laciniata has traditionally been taken orally for the treatment of allergies, headache and liver diseases. Three antibacterial iridoid glucosides, phloyoside I (1), phlomiol (2) and pulchelloside I (3) have been isolated from the rhizomes of this plant. The structures of these compounds were elucidated unequivocally by a series of 1D and 2D NMR analyses. The antibacterial activity and brine shrimp toxicity of these compounds were assessed using the resazurin microtitre assay and the brine shrimp lethality assay, respectively. All three iridoid glycosides 1-3 exhibited from low to moderate level...

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... PERSONAL AUTHOR(S) ROY A. BROOKS, LTC i3a. ... gave the impression of an immediate increase in the standard ... high rate by German standards. ...

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... of a secondary standard (VCO) locally available. ... phase of the local secondary standards to the 10-min average of the phase of ... I3a - - \\.-e-~--. ...

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... i3a TYPT OF REPORT 13b TIME COVERED 14 DATE OF RF ... automation system when used in conjunction with other standard security measures. ...

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... I3a. -YPE OF REPORT T7b 7,ME COVEE 14 DATE OF REPORT (Year, Month. ... the addition of various materials to the standard flare in order to ...

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... Tactical plays are more than drills or standard operating proc-edures. ... IN * BYPMASS OR BREECH MINEFIELD ON FLANK SIXE (TM I3A C1 10 ...

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... proficiency, most Army personnel must shoot to the same standards required of ... Wild- flecken was to provide this standard range, but its scores ... I3a I] ...

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... 1 I3a TYPE OF REPORT 1 3b TIME COVERED ... Measured by this standard the system provides good results; it ... did not fully meet all the standards or ...

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The DNA sequence motif ATTTGCAT (octamer) or its inverse complement has been identified as an evolutionarily conserved element in the promoter region of immunoglobulin genes. Two major DNA-binding proteins that bind in a sequence-specific manner to the octamer DNA sequence have been identified in mammalian species--a ubiquitously expressed protein (Oct-1) and a lymphoid-specific protein (Oct-2). During characterization of the promoter region of the chicken immunoglobulin light chain gene, the authors identified two homologous octamer-binding proteins in chicken B cells. when the cloning of the human gene for Oct-2 revealed it to be a member of a distinct family of homeobox genes, they sought to determine if the human Oct-2 cDNA could be used to identify homologous chicken homeobox genes. Using a human Oct-2 homeobox-specific DNA probe, they were able to identify 6-10 homeobox-containing genes in the chicken genome, demonstrating that the Oct-2-related subfamily of ...

UK PubMed Central (United Kingdom)

The complete nucleotide sequence of the cap3A gene of Streptococcus pneumoniae, which is directly responsible for the transformation of some unencapsulated, serotype 3 mutants to the encapsulated phenotype,...Full Text Available

International Nuclear Information System (INIS)

Rats or mice acutely exposed to high concentrations of ozone show an immediate and significant weight loss, even when allowed free access to food and water. The mechanisms underlying this systemic response to ozone have not been previously elucidated. We have applied the technique of global gene expression analysis to the livers of C57BL mice acutely exposed to ozone. Mice lost up to 14% of their original body weight, with a 42% decrease in total food consumption. We previously had found significant up-regulation of genes encoding proliferative enzymes, proteins related to acute phase reactions and cytoskeletal functions, and other biomarkers of a cachexia-like inflammatory state in lungs of mice exposed to ozone. These results are consistent with a general up-regulation of different gene families responsive to NF-#kappa#B in the lungs of the exposed mice. In the present study, we observed significant down-regulation of different families of mRNAs in the livers of the exposed mice, ...

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Rice is a very important food staple that feeds more than half the world's population. Two major Asian cultivated rice (Oryza sativa L.) subspecies, japonica and indica, show significant phenotypic variation in their stress responses. However, the molecular mechanisms underlying this phenotypic variation are still largely unknown. A common link among different stresses is that they produce an oxidative burst and result in an increase of reactive oxygen species (ROS). In this study, methyl viologen (MV) as a ROS agent was applied to investigate the rice oxidative stress response. We observed that 93-11 (indica) seedlings exhibited leaf senescence with severe lesions under MV treatment compared to Nipponbare (japonica). Whole-genome microarray experiments were conducted, and 1,062 probe sets were identified with gene expression level polymorphisms between the two rice cultivars in addition to differential expression under MV treatment, which were assigned as Core Intersectional Probesets ...

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This study is aimed at exploring the possible mechanism of hypnosis-enhancing effect of HgS or cinnabar (a traditional Chinese medicine containing more than 95% HgS) in mice treated with pentobarbital. We also examined whether the effect of HgS is different from that of the well-known methyl mercury (MeHg). After a short period (7 days) of oral administration to mice, a nontoxic dose (0.1 g/kg) of HgS not only significantly enhanced pentobarbital-induced hypnosis but also attenuated tolerance induction; while a higher dose (1 g/kg) of HgS or cinnabar exerted an almost irreversible enhancing effect on pentobarbital-hypnosis similar to that of MeHg (2 mg/kg) tested, which was still effective even after 10 or 35 days cessation of administration. To study comparatively the effects of different mercury forms from oral administration of MeHg and HgS on membrane ATPase activities of experimental mice, analysis of the Hg content in the cerebral cortex revealed that correlated with the decrease ...

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Dehydrins, a subfamily of group 2 LEA proteins, are intrinsically unstructured plant proteins that accumulate in the late stages of seed development and in vegetative tissues subjected to water deficit, salinity, low temperature, or abscisic acid treatment. In this study, we isolated and characterized ZmDHN2b, a maize dehydrin gene. The genomic organization of the ZmDHN2b gene and its expression in maize seedlings were analyzed. To investigate the function of ZmDHN2b, we generated transgenic tobacco plants constitutively overexpressing ZmDHN2b. Ectopic expression of ZmDHN2b in tobacco accelerated seed germination and seedling growth at 15?C. Furthermore, ZmDHN2b-overexpressing lines had lower levels of cold-induced malondialdehyde and less electrolyte leakage than wild-type tobacco at 4?C....

International Nuclear Information System (INIS)

Macrophage differentiation antigen associated with complement three receptor function (Mac-1) belongs to #beta#_2 subfamily of integrins that mediate important cell-cell and cell-extracellular matrix interactions. Biochemical studies have indicated that Mac-1 is a constitutive heterodimer in vitro. Here, we detected the heterodimerization of Mac-1 subunits in living cells by means of two fluorescence resonance energy transfer (FRET) techniques (fluorescence microscopy and fluorescence spectroscopy) and our results demonstrated that there is constitutive heterodimerization of the Mac-1 subunits and this constitutive heterodimerization of the Mac-1 subunits is cell-type independent. Through FRET imaging, we found that heterodimers of Mac-1 mainly localized in plasma membrane, perinuclear, and Golgi area in living cells. Furthermore, through analysis of the estimated physical distances between cyan fluorescent protein (CFP) and yellow fluorescent protein (YFP) fused ...

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... Figure 5. Distribution of standard deviation computed from N events Page 18. ... t- OJ o o o to to to o (S99J69P) QI0V 01 3AllV"I3a Hinwizv Page 20. ...

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... protein is abundant in cytosolic portions of malignant epithelial tissue (Fig. 3A). In contrast, the degree of CCTβ staining in normal epithelial tissue (Fig. 3B) or connective tissues was much weaker ......

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The goal of the present work was to determine the impact of N3-methyladenine (3-mA), an important lesion generated by many environmental agents and anticancer drugs, on in vivo DNA replication and in vitro RNA transcription. Due to 3-mA chemical instability, the stable isostere 3-methyl-3-deazaadenine (3-m-c(3)A) was site specifically positioned into an oligodeoxynucleotide. The oligomer was, then incorporated into a vector system that is rapidly converted to ssDNA inside yeast cells and requires DNA replication opposite the lesion for plasmid clonal selection. For control purposes, an adenine or a stable apurinic/apyrimidinic (AP)-lesion was placed at the same site. The presence of each lesion in the oligonucleotide was confirmed by MALDI-TOF analysis. Plasmids were then transfected into yeast cells. While the AP-site dramatically reduced plasmid replication in all strains, the 3-m-c(3)A had a slight ...

Wastenet

...Content 3a LCA Methodology - Characterisation(PDF) 3a1 BRE Response - Characterisation 3b LCA Methodology - Normalisation (PDF) 3b1 BRE Response - Normalisation 3c LCA Methodology - Weighting (PDF) 3c1 Feedback - Weighting 3c2 Weightings Exercise (PDF) 4 Specification (PDF) 4a - Functional Units Spreadsheet (Excel) 4b Specification List (Excel) 5 Energy Model (PDF) 6 Whole Life perfomance 6b Response Note To Briefing Note 6 - Whole Life Performance (PDF) 7 End-of-Life and Waste models (PDF) 7a Waste routes and rates feedback (PDF) 7b Waste Disposal Routes for Industry Consultation 7c Site Wastage Rates for Industry Consultation 8 Existing LCA ...

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1 Candoxin (MW 7334.6), a novel toxin isolated from the venom of the Malayan krait Bungarus candidus, belongs to the poorly characterized subfamily of nonconventional three-finger toxins present in Elapid venoms. The current study details the pharmacological effects of candoxin at the neuromuscular junction. 2 Candoxin produces a novel pattern of neuromuscular blockade in isolated nerve-muscle preparations and the tibialis anterior muscle of anaesthetized rats. In contrast to the virtually irreversible postsynaptic neuromuscular blockade produced by curaremimetic alpha-neurotoxins, the neuromuscular blockade produced by candoxin was rapidly and completely reversed by washing or by the addition of the anticholinesterase neostigmine. 3 Candoxin also produced significant train-of-four fade during the onset of and recovery from neuromuscular blockade, both, in vitro and in vivo. The fade phenomenon has been attributed to a blockade of putative presynaptic nicotinic ...

UK PubMed Central (United Kingdom)

Previous DNA relatedness and enzyme electrophoretic mobility studies indicated heterogeneity among strains of Legionella pneumophila serogroups 1, 4, 5, and Lansing 3 (a new, as yet unnumbered serogroup)....Full Text Available

UK PubMed Central (United Kingdom)

BackgroundHepatitis C virus (HCV) infection is the leading cause of chronic hepatitis which progresses to hepatocellular carcinoma (HCC) afflicting > 170 million people worldwide....Full Text Available

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We hypothesized that I kappa B kinase (IKK)-mediated nuclear factor kappa B and forkhead BoxO3a phosphorylation will be associated with age-related endothelial dysfunction. Endothelium-dependent dilation and aortic protein expression/phosphorylation were determined in young and old male B6D2F1 mice and old mice treated with the IKK inhibitor, salicylate. IKK activation was greater in old mice and was associated with greater nitrotyrosine and cytokines. Endothelium-dependent dilation, nitric oxide (NO), and endothelial NO synthase phosphorylation were lower in old mice. Endothelium-dependent dilation and NO bioavailability were restored by a superoxide dismutase mimetic. Nuclear factor kappa B and forkhead BoxO3a phosphorylation were greater in old and were associated with increased express...

International Nuclear Information System (INIS)

Objective: To determine the optimal contrast injection protocol for 64-MDCT coronary angiography. Materials and methods: One hundred and fifty consecutive patients scheduled to undergo retrospectively electrocardiographically gated 64-MDCT. Each 30 patients were assigned to use a different contrast protocol: group 1: uniphasic protocol (contrast injection without saline flush); group 2: biphasic protocol (contrast injection with saline flush); group 3A, 3B and 3C: triphasic protocol (contrast media + different saline diluted contrast media + saline flush). Image quality scores and artifacts were compared and evaluated on both transaxial and three-dimensional coronary artery images among each contrast protocol. Results: Among the triphasic protocol groups, group 3A (30%:70% contrast media-saline mixture was used in second phase) used the least contrast media and had the least frequency of streak ...

International Nuclear Information System (INIS)

Superplastic deformation behavior in an alpha + beta titanium alloy Ti-3A-4V has been investigated by using the method of cross head speed cycling in the temperature range 750-910 /sup 0/C. On the basis of flow stress-strain rate-strain rate sensitivity data, the alloy was found to be superplastic in the entire temperature range studied. Optimum superplasticity was observed in the strain-rate range 3 x 10/sup -5/ sec./sup -1/ to 6 x 10/sup -5/ and at the highest temperature of 910 deg. C. (author).

International Nuclear Information System (INIS)

The effects of D-amino acids at Asp"2"3 and Ser"2"6 residues on the conformational preference of #beta#-amyloid (A#beta#) peptide fragment (A#beta#_2_0_-_2_9) have been studied using different spectroscopic techniques, namely vibrational circular dichroism (VCD), vibrational absorption, and electronic circular dichroism. To study the structure of the A#beta#_2_0_-_2_9, [D-Asp"2"3]A#beta#_2_0_-_2_9, and [D-Ser"2"6]A#beta#_2_0_-_2_9 peptides under different conditions, the spectra were measured in 10 mM acetate buffer (pH 3) and in 2,2,2-trifluoroethanol (TFE). The spectroscopic results indicated that at pH 3, A#beta#_2_0_-_2_9 peptide takes random coil with #beta#-turn structure, while [D-Ser"2"6]A#beta#_2_0_-_2_9 peptide adopts significant amount of polyproline II (PPII) type structure along with #beta#-turn contribution and D-Asp-substituted peptide ...

Science.gov (United States)

Data are presented demonstrating short-wavelength (approx. <6400 A) continuous (cw) laser operation of p-n diode In/sub 0.5/(Al/sub x/Ga/sub 1-//sub x/)/sub 0.5/P multiple quantum well heterostructure (QWH) lasers grown lattice matched on GaAs substrates using metalorganic chemical vapor deposition. In the range from -30 /sup 0/C to room temperature (RTapprox. =300 K, lambdaapprox. =6395 A) the threshold current density changes from 2.3 x 10/sup 3/ A/cm/sup 2/ (-30 /sup 0/C) to 3.7 x 10/sup 3/ A/cm/sup 2/ (RT, 300 K). The cw 300 K photopumped laser operation of the same quaternary QWH crystal is an order of magnitude lower in threshold (7 x 10/sup 3/ W/cm/sup 2/, J/sub eq/approx.2.9 x 10/sup 3/ A/cm/sup 2/) than previously reported for this crystal system, and agrees with the successful demonstration of cw 300 K laser diodes at this short wavelength.

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In developing new brain imaging agents for single photon emission computed tomography (SPECT), we synthesized eleven radioiodinated phenoxyacetic acid derivatives and investigated the relationship between the chemical structure and in vivo characteristics. Biodistribution studies in mice revealed high initial brain uptake for all the compounds. Blood radioactivity level depended markedly upon the chemical stability of the compound. The alpha,alpha-dimethylester derivative, amide derivatives and diamine derivatives, which were stable to hydrolysis, showed low blood activity levels following intravenous administration. Disappearance of the ester and amide compounds from the brain was rapid. However, the diamine derivatives displayed improved retention in the brain. Compounds 3a and 4 possessed the best combination of high brain uptake and sufficient retention to be useful as potential brain imaging radiopharmaceuticals with SPECT devices.

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Premnalatifolin A (1), a unique icetexane diterpene dimer was isolated from the stem-bark of Indian medicinal plant, Premna latifolia. Its structure and relative stereochemistry were elucidated on the basis of detailed spectroscopic analysis, including HRESIMS and 2D NMR (COSY, HSQC, HMBC, and NOESY) spectra. The compound has dimeric carbon skeleton composed of two icetexane skeletal diterpenes linked via ether bond. Further, premnalatifolin A (1) was also evaluated for its cytotoxicity against cancer cell lines (HT-29, A-431, MCF-7, Hep-G2, PC-3, A-549, B-16 F10, and ACHN), which displayed potent activity against HT-29 and MCF-7 cell lines with the IC50 values of 12.15 and 1.11mg/mL, respectively.

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Samples of Fe78B13Si9 (Metglas 2605 TCA) and Fe77Cr2B16Si5 (Metglas 2605 S3A) were exposed to pulsed excimer laser irradiation at repetition rates of 15, 25 and 50Hz. The occurrence of out-of-plane magnetic anisotropy, changes in the average hyperfine magnetic field and width of the hyperfine field distribution were evidenced by transmission Mossbauer spectroscopy. The variation of the recoilless fraction with laser processing parameters was derived from the simultaneous recording of Mossbauer spectra using a stainless steel etalon as a dual absorber. Conclusions on the onset of long-range magnetic order were formulated.

International Nuclear Information System (INIS)

The purpose of the present study was to compare the effectiveness of MRI, CT and radioimmunoscintigraphy in the staging and detection of bladder cancers in 28 patients. We distinguish two groups: Group I included the tumour stages CIS-T_3_A and the second group the deep infiltrative tumours T_3_B-T_4. MRI was slightly superior to CT in respect of tumour staging (75% correct results as compared to 63%). No understaging occurred with MRI, whereas in 22% of the cases the stage of the tumour was underestimated using CT diagnostics. Overstaging occurred in 25% of the MRI and 15% of the CT-diagnostics, respectively. RIS cannot distinguish the tumour groups, and hence this method is useful only for the detection of the primary tumour and metastases. In 77% of cases the tumour was detected and in 15% the tumour could be safely excluded. (orig.).

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Transparency is essential for normal corneal function. Recent studies suggest that corneal cells express high levels of so-called corneal crystallins, such as aldehyde dehydrogenase (ALDH) and transketolase (TKT) that contribute to maintaining cellular transparency. Stromal injury leads to the appearance of repair phenotype keratocytes, the corneal fibroblast and myofibroblast. Previous studies on keratocytes from species such as bovine and rabbit indicate that the transformation from the normal to repair phenotype is accompanied by a loss of corneal crystallin expression, which may be associated with loss of cellular transparency. Here we investigated if a similar loss occurs with human keratocyte repair phenotypes. Human corneal epithelial cells were collected by scraping and keratocytes...

International Nuclear Information System (INIS)

A new iron phosphate (NH4)4Fe3(OH)2F2[H3(PO4)4] has been synthesized hydrothermally at HF concentrations from 0.5 to 1.2 mL. Single-crystal X-ray diffraction analysis reveals its three-dimensional open-framework structure (monoclinic, space group P21/n (No. 14), a=6.2614(13) A, b=9.844(2) A, c=14.271(3) A, ?=92.11(1)o, V=879.0(3) A3). This structure is built from isolated linear trimers of corner-sharing Fe(III) octahedra, which are linked by (PO4) groups to form ten-membered-ring channels along [1 0 0]. This isolated, linear trimer of corner-sharing Fe(III) octahedra, [(FeO4)3(OH)2F2], is new and adds to the diverse linkages of Fe polyhedra as secondary building units in iron phosphates. The trivalent iron at octahedral sites for the title compound has been confirmed by synchrotron Fe K-edge XANES spectra and magnetic measurements. Magnetic measurements also show that this compound exhibit a strong ...

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The analgesic activity of nine substituted N-pyrrolylcarboxylic acids, previously reported as anti-inflammatory agents, has been evaluated. The effects on nociception were examined in male Wistar rats by the Randall-Selitto paw-pressure test. The compounds were administrated in doses 10, 20, and 40 mg/kg both i.p. and p.o. As a whole, the activities of 3-(N-pyrrolyl)propanoic acids 3e-3h and 2-[3-(ethoxycarbonyl)-2-methyl-5-phenyl-1H-1-pyrrolyl]-3-methylpentanoic acid 3i were comparable with or superior to that of metamizole used as a reference (200 mg/kg, i.p.), whereas only 3a from among the N-pyrrolyl-acetic acids 3a-3d showed analgesic activity on the inflamed paw. The compounds found most promising to increase the pain threshold significantly were the same ones with the higher anti-inflammatory activity registered in our previous study: ...

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A series of thiazolo[3,2-b][1,2,4]triazole incorporating diphenylsulfone moieties were synthesized starting from 5-[4-(4-X-phenylsulfonyl)phenyl]-4H-1,2,4-triazole-3-thioles 3a-c, X=H, Cl, Br. Thus, alkylation of 1,2,4-triazoles 3 with phenacyl bromide or 4-bromophenacyl bromide afforded S-substituted 1,2,4-triazoles 4, 5. These new intermediates 4 and 5, in the presence of H2SO4 (c), were cyclized to 2-[4-(4-X-phenylsulfonyl)phenyl]-6-(4-Y-phenyl)[1,3]thiazolo[3,2-b]-[1, 2,4]-triazoles 6, 7 (I) and not to isomeric thiazolo[2,3-c][1,2,4]-triazoles 6, 7 (II). The newly synthesized compounds were characterized by IR, 1H, 13C NMR and elemental analysis. MS spectra confirmed the formation of thiazolo[3,2-b][1,2,4]triazole 6, 7 (forms I) in detriment of [2,3-c] isomeric compounds (forms II). Th...

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Red mud from HINDALCO (Hindustan Aluminium Corporation) Industries Limited, Renukoot, India, contains significant quantities of alumina, iron oxide and silica. Presence of the said constituents makes it a suitable ingredient for the preparation of special cements. Preparation of three varieties of cements was investigated, namely: (a) aluminoferrite (C{sub 4}AF)-belite ({beta}-C{sub 2}S) using lime + red mud + fly ash; (b) aluminoferrite-ferrite (C{sub 2}F)-aluminates (C{sub 3}A and C{sub 12}A{sub 7}) utilizing lime + red mud + bauxite; and (c) sulfoaluminate (C{sub 4}A{sub 3}{bar S})-aluminoferrite-ferrite using lime + red mud + bauxite + gypsum. The effects of composition (proportions of lime, red mud, fly ash, bauxite and gypsum), firing temperature and duration on the properties of cements produced were studied in detail. Cements made from lime + red mud + bauxite or lime + red mud + bauxite + gypsum exhibit strengths comparable or superior ...

British Library Electronic Table of Contents (United Kingdom)

A variety of platinum(II) complexes of methimazole (2-mercapto-1-methylimidazole; HImS=neutral form and ImS=thiolate form), coordinated in both thione and thiolate forms, have been isolated by reacting methimazole with [PtCl(terpy)]Cl (terpy=2,2prime:6prime,2Prime terpyridine), [PtCl2(bipy)] (bipy=bipyridine), [PtCl2(o-phen)] (o-phen=o-phenanthroline), [PtCl2(CH3CN)2] and [PtCl2(COD)] (COD=1,5-cyclooctadiene). These complexes were characterized by electronic absorption, IR and NMR (1H, 13C, 195Pt) spectroscopies. Molecular structure of [Pt(bipy)(HImS)2]Cl23H2O (3a3H2O) has been established by single crystal X-ray crystallography. Platinum thiolate complex, [Pt(ImS)2(HImS)2] (5), could be obtained by treatment of [Pt(HImS)4]Cl2 with sodium methoxide in methanol. The solution of 5 in organic...

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The primary objective of the project is to investigate the long-term effects of commercially available tangentially-fired low NO{sub x} combustion technologies on NOx emissions and boiler performance on Unit 2 at Gulf Power Company's Plant Lansing Smith located near Lynn Haven, Florida. The project will characterize emissions and performance of a tangentially-fired boiler operating in the following configurations: Baseline as-found'' configuration: Phase 1; retrofitted low NO{sub x} concentric firing system (LNCFS) Level 2 and simulated low NO{sub x} bulk furnace staging (LNBFS): Phase 2; retrofitted low NO{sub x} concentric firing system (LNCFS) Level 3, Phase 3a and simulated LNCFS Level 1, Phase 3b.

CERN Document Server

Data mining is a useful decision support technique that can be used to discover production rules in warehouses or corporate data. Data mining research has made much effort to apply various mining algorithms efficiently on large databases. However, a serious problem in their practical application is the long processing time of such algorithms. Nowadays, one of the key challenges is to integrate data mining methods within the framework of traditional database systems. Indeed, such implementations can take advantage of the efficiency provided by SQL engines. In this paper, we propose an integrating approach for decision trees within a classical database system. In other words, we try to discover knowledge from relational databases, in the form of production rules, via a procedure embedding SQL queries. The obtained decision tree is defined by successive, related relational views. Each view corresponds to a given population in the underlying decision tree. We selected the classical ...

British Library Electronic Table of Contents (United Kingdom)

Genome-wide association studies have linked lung cancer risk with a region of chromosome 15q25.1 containing CHRNA3, CHRNA5 and CHRNB4 encoding a3, a5 and b4 subunits of nicotinic acetylcholine receptors (nAChR), respectively. One of the strongest associations was observed for a non-silent single-nucleotide polymorphism at codon 398 in CHRNA5. Here, we have used pharmacological (antagonists) or genetic (RNA interference) interventions to modulate the activity of CHRNA5 in non-transformed bronchial cells and in lung cancer cell lines. In both cell types, silencing CHRNA5 or inhibiting receptors containing nAChR a5 with a-conotoxin MII exerted a nicotine-like effect, with increased motility and invasiveness in vitro and increasing calcium influx. The effects on motility were enhanced by addit...

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This study was designed to identify abnormalities in the hepatic-arterial/portal-venous scintiangiogram (SA) in alcoholic hepatitis (AH). SA's were performed in 35 patients with acute alcoholic hepatitis (AAH), 8; acute alcoholic hepatitis superimposed on cirrhosis (A/C), 14; and cirrhosis (C), 13. Posterior flows were done with a bolus of 10 mCi Tc-99m sulfur colloid with computer time-activity curves over the liver and left kidney. Curves were analyzed for per cent of hepatic arterial (HA) and portal venous contribution using the slope ratio method. Hepatic arterialization was estimated from the angle of the HA component of the curve. Reversal of the relative contribution of the hepatic and portal components of total flow were seen in all groups. Although quite severe in AH, the degree of reversal could not be used to differentiate among the groups. The average HA angle in AAH was 48.3 +- 8.1, in A/C 41.5 +- 10.6, and in C 30.4 +- 12.1. In reviewing the data of only those in ...

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The simulation of the Auxiliary Charcoal Bed (ACB) Vacuum System was performed to evaluate the original vacuum system design, detect and identify design deficiencies, investigate the effects of proposed corrections on system performance, and generally aid in refining the system design before construction and mockup testing. The simulation was performed by using the Advanced Continuous Simulation Language (ACSL). The vacuum system design goals are to provide approximately 20 SCFM of both booster gas and purge gas through the system and maintain a flow of approximately 40 SCFM with a velocity of 50 to 75 f/sec at the entrance to the cyclone separator. The model results showed that the original system design was incapable of meeting the system performance goals. Further simulations showed that the following modifications to the original vacuum system design were required to make the system performance acceptable; (1) Remove valve PCV4. (2) Modify the flow controllers FTC3 and FTC4 from ...

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A gene designated BRCA1, implicated in the susceptibility to early-onset familial breast cancer, has recently been localized to chromosome 17q12-q21. To date, the order of DNA markers mapped within this region has been based on genetic linkage analysis. The authors report the use of multicolor fluorescence in situ hybridization to establish a physically based map of five polymorphic DNA markers and 10 cloned genes spanning this region. Three cosmid clones and Alu-PCR-Generated products derived from 12 yeast artificial chromosome clones representing each of these markers were used in two-color mapping experiments to determine an initial proximity of markers relative to each other on metaphase chromosomes. Interphase mapping was then employed to determine the order and orientation of closely spaced loci by direct visualization of fluorescent signals following hybridization of three probes, each detected in a different color. Statistical analysis of the combined data suggests that the ...

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Results are presented from a series of studies conducted at the Department of Energy (DOE) Savannah River Plant (SRP) with the NASA Airborne Oceanographic Lidar (AOL). These studies included a topographic survey of a {approximately}1000 acre lake basin (presently designated L Lake) which had been excavated for use as a cooling pond for L Reactor; a study of the movement of discharged cooling water in Pond C and the warm arm of Par Pond using Rhodamine WT dye as a tag; initial baseline studies of the vegetation cover of the Steel Creek corridor (through which the outflow of L Lake is carried to the Savannah River); and a demonstration of potential forestry applications of the AOL. These investigations were conducted over a 3-day period in June 1985. The AOL is an advanced airborne laser system capable of making temporal or time history measurements of laser backscatter (bathymetry mode) or spectral measurements of laser induced fluorescence from waterborne constituents (fluorosensing ...

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The chromosomal region 17q12-q21 contains a gene (BRCA1) conferring susceptibility to early-onset familial breast and ovarian cancer. An 8000-rad radiation-reduced hybrid (RH) panel was constructed to provide a resource for long-range mapping of this region. A large fraction of the hybrids ([approximately]90%) retained detectable human chromosome 17 sequences. The complete panel of 76 hybrids was scored for the presence or absence of 22 markers from this chromosomal region, including 14 cloned genes, seven microsatellite repeats, and one anonymous DNA segment. Statistical analysis of the marker retention data employing multipoint methods provided both comprehensive and framework maps of this chromosomal region, including distance estimates between adjacent markers. The comprehensive RH map includes 17 loci and spans 179 cRays[sub (8000)]. Likelihood ratios of at least 1000:1 support the 10-locus framework order: cen-D17S250-ERBB2-(THRA1, ...

International Nuclear Information System (INIS)

Sr3In0.9Co1.1O6, isostructural to Ca3Co2O6, is revealed by the study of the phase relations in the system SrO-InO1.5-CoOx (1000 oC). The structure of Sr3In0.9Co1.1O6 is refined by the combination of powder X-ray and neutron diffraction. Sr3In0.9Co1.1O6 crystallizes in a trigonal lattice with the cell parameters a=b=9.59438(3) A, c=11.02172(4) A with the space group R-3c. Its structure possesses 1D (In/Co)O3 chains running along the c-axis constructed by alternating face-sharing CoO6 octahedra and (In0.9Co0.1)O6 trigonal prisms. The co-occupation of In3+ and Co3+ at the trigonal prismatic site is evidenced by elementary analysis and determined by the structure refinement. Sr3In0.9Co1.1O6 is paramagnetic, and the susceptibility is consistent with the occupation of Co3+ at 10% of the trigonal prismatic positions in a high spin state (HS, S=2). The HS Co3+ is well separated by diamagnetic CoO6 octahedra and InO6 trigonal prisms and shows a g factor ...