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Sample records for alpha hydroxy-5 cap

  1. Synthesis of tritium or deuterium labelled 19-nor-3. cap alpha. -hydroxy-5. cap alpha. -androstan-17-one from nortestosterone

    Energy Technology Data Exchange (ETDEWEB)

    Protiva, J; Klinotova, E [Karlova Univ., Prague (Czechoslovakia). Prirodovedecka Fakulta; Filip, J [Ustav pro Vyzkum, Vyrobu a Vyuziti Radioisotopu, Prague (Czechoslovakia); Hampl, R [Research Inst. of Endocrinology, Praha (Czechoslovakia)

    1982-10-20

    Tritium and/or deuterium (5-H) labelled 19-nor-3..cap alpha..-hydroxy-5..cap alpha..-androstan-17-one (norandrosterone) was prepared from nortestosterone in view to use it as a radioligand for radioimmunoassay of the main nortestosterone metabolites. Based upon model experiments using testosterone and deuterium labelling, the following four step procedure was established: nortestosterone was oxidized with pyridine chlorochromate and the resulting 19-nor-4-androsten-3,17-dione was tritiated with tritium gas under catalysis with tris(triphenylphosphine)rhodium chloride to give (4,5..cap alpha..-/sup 3/H)19-nor-5..cap alpha..-androstan-3,17-dione. A selective reduction of the latter compound yielded (5-/sup 3/H)19-nor-3..cap alpha..-hydroxy-5..cap alpha..-androstan-17-one of the molar radioactivity 0.3 TBq (8.15 Ci)/mmol.

  2. Increased 5. cap alpha. -reductase activity in idiopathic hirsutism

    Energy Technology Data Exchange (ETDEWEB)

    Serafini, P.; Lobo, R.A.

    1985-01-01

    In vitro, genital skin 5..cap alpha..-reductase activity (5..cap alpha..-RA) was measured in ten hirsute women with normal androgen levels (idiopathic hirsutism (IH)) and in ten hirsute women with elevated androgen levels (polycystic ovary syndrome (PCO)) in order to determine the influence of secreted androgens on 5..cap alpha..-RA. In vitro 5..cap alpha..-RA was assessed by incubations of skin with /sup 14/C-testosterone (T) for 2 hours, after which steroids were separated and the radioactivity of dihydrotestosterone (DHT) and 5..cap alpha..-androstane 3..cap alpha..-17..beta..-estradiol (3..cap alpha..-diol) in specific eluates were determined. All androgens were normal in IH with the exception of higher levels of 3..cap alpha..-diol glucuronide which were similar to the levels of PCO. The conversion ratio (CR) of T to DHT in IH and PCO were similar, yet significantly greater than the CR of control subjects. The CR of T to 3..cap alpha..-diol in IH and PCO were similar, yet higher than in control subjects. Serum androgens showed no correlation with 5..cap alpha..-RA, while the CR of T to DHT showed a significant positive correlation with the Ferriman and Gallwey score. The increased 5..cap alpha..-RA in IH appears to be independent of serum androgen levels and is, therefore, an inherent abnormality. The term idiopathic is a misnomer, because hirsutism in these patients may be explained on the basis of increased skin 5..cap alpha..-RA.

  3. Synthesis and antimicrobial evaluation of new 3-alkyl/aryl-2-[((alpha,alpha-diphenyl-alpha-hydroxy)acetyl)hydrazono]-5-methyl-4-thiazolidinones.

    Science.gov (United States)

    Güzeldemirci, Nuray Ulusoy; Ilhan, Eser; Küçükbasmaci, Omer; Satana, Dilek

    2010-01-01

    New 4-thiazolidinone derivatives of benzilic acid (alpha,alpha-diphenyl-alpha-hydroxyacetic acid) have been synthesized and evaluated for antibacterial and antifungal activities. The reaction of 1- (alpha,alpha-diphenyl-alpha-hydroxy)acetyl-4-alkyl/arylthiosemicarbazides with ethyl 2-bromopropionate gave 3-alkyl/aryl-2-[((alpha,alpha-diphenyl-alpha-hydroxy)acetyl)hydrazono]-5-methyl-4-thiazolidinone derivatives. Their antibacterial and antifungal activities were evaluated against S. aureus ATCC 29213, P. aeruginosa ATCC 27853, E. coli ATCC 25922, C. albicans ATCC 10231, C. parapsilosis ATCC 22019, C. krusei ATCC 6258, T. mentagrophytes var. erinacei NCPF 375, M. gypseum NCPF 580 and T. tonsurans NCPF 245. 3e, 3f, 3g and 3h showed the highest antibacterial activity. Particularly 3a and 3e showed the highest antifungal activities against C. parapsilosis ATCC 22019, T. tonsurans NCPF 245 and M. gypseum NCPF 580.

  4. Anti-pp,. cap alpha cap alpha. and p. cap alpha. elastic scattering at high energies and Chou-Yang conjecture

    Energy Technology Data Exchange (ETDEWEB)

    Saleem, M.; Fazal-e-Aleem; Rifique, M.

    1987-03-01

    The recent experimental measurements for anti-pp and ..cap alpha cap alpha.. elastic scattering at high energies have shown that the Chou-Yang conjecture regarding the relationship between the electromagnetic and the hadronic form factor of a particle is only an approximation. A new ansatz has been proposed to obtain hadronic form factors of proton and the ..cap alpha..-particle. These form factors have been used to explain the various characteristics of anti-pp, ..cap alpha cap alpha.. and p..cap alpha.. elastic scattering at high energies.

  5. Enantioselective conjugate radical addition to alpha'-hydroxy enones.

    Science.gov (United States)

    Lee, Sunggi; Lim, Chae Jo; Kim, Sunggak; Subramaniam, Rajesh; Zimmerman, Jake; Sibi, Mukund P

    2006-09-14

    Enantioselective conjugate radical addition to alpha'-hydroxy alpha,beta-unsaturated ketones, compounds containing bidentate donors, has been investigated. It has been found that radical additions to alpha'-hydroxy alpha,beta-unsaturated ketones in the presence of Mg(NTf2)2 and bisoxazoline ligand 5a proceeded cleanly, yielding the addition products in high chemical yields and good enantiomeric excesses.

  6. /sup 58,60,62/Ni (. cap alpha. ,p) three--nucleon transfer reactions and. cap alpha. optical potential ambiguities

    Energy Technology Data Exchange (ETDEWEB)

    Yuanda, Wang; Xiuming, Bao; Zhiqiang, Mao; Rongfang, Yuan; Keling, Wen; Binyin, Huang; Zhifu, Wang; Shuming, Li; Jianan, Wang; Zuxun, Sun; others, and

    1985-11-01

    The differential cross sections are measured using 26.0 MeV ..cap alpha.. particle for /sup 58,62/Ni(..cap alpha.., ..cap alpha..) /sup 58,62/Ni and /sup 58,62/Ni(..cap alpha..,p) /sup 61,65/Cu reactions as well as 25.4 MeV ..cap alpha.. particle for /sup 60/Ni(..cap alpha.., ..cap alpha..)/sup 69/Ni and /sup 60/Ni(..cap alpha.., p)/sup 63/Cu reactions. Consistent calculations with optical model and ZR DWBA are made for (..cap alpha.., ..cap alpha..) and (..cap alpha.., p) reactions by using of single, two, three and four nucleon optical potential parameters. For elastic scattering due to the ..cap alpha.. optical potential ambiguities, all the above optical potential can reproduce the experimental angular distributions. However, the single, two and three nucleon potential, including the Baird's mass systematics and the Chang's energy systematics of ..cap alpha.. potentials, obviously can not provide a reasonable fitting with the (..cap alpha..,p) reaction experimental data. Only the results from the four nucleon potential is in good agreement with the (..cap alpha..,p) reaction experimental data. This reveals that in the ..cap alpha..-particle induced transfer reactions, the real depth of the ..cap alpha..-nucleus optical potential should be rather deep.

  7. Derivatives of 16alpha-hydroxy-dehydroepiandrosterone with an additional 7-oxo or 7-hydroxy substituent: synthesis and gas chromatography/mass spectrometry analysis.

    Science.gov (United States)

    Pouzar, Vladimír; Cerný, Ivan; Hill, Martin; Bicíková, Marie; Hampl, Richard

    2005-10-01

    Derivatives of 16alpha-hydroxy-dehydroepiandrosterone, which have an additional oxygen substituent at position 7 (oxo or hydroxy group), were synthesized. Firstly, 17,17-dimethoxyandrost-5-ene-3beta,16alpha-diyl diacetate was prepared and then oxidized with a complex of chromium(VI) oxide and 2,5-dimethylpyrazole to the respective 7-oxo derivative. This key intermediate was both deprotected or reduced by l-Selectride or sodium borohydride in the presence of cerium(III) chloride and then deprotected to give 7-oxo, 7alpha-hydroxy and 7beta-hydroxy derivatives of 16alpha-hydroxy-dehydroepiandrosterone. The target compounds were characterized by (1)H and (13)C NMR spectra and in the form of O-methyloxime-trimethylsilyl derivatives, by gas chromatography/mass spectrometry methods.

  8. Alpha Hydroxy Acids

    Science.gov (United States)

    ... or tenderness (8), chemical burns (6), and increased sunburn (3). The frequency of such reports for skin ... bear a statement that conveys the following information: Sunburn Alert: This product contains an alpha hydroxy acid ( ...

  9. /sup 56/Fe (. gamma. ,. cap alpha. /sub 0/) reaction

    Energy Technology Data Exchange (ETDEWEB)

    Tamae, T; Sugawara, M [Tohoku Univ., Sendai (Japan). Lab. of Nuclear Science; Tsubota, H

    1974-12-01

    The reaction cross section of /sup 56/Fe (..gamma.., ..cap alpha../sub 0/) was measured from the electron energy of 15 to 25 MeV. The measured data were compared with the calculated ones based on statistic theory. Both agreed with each other. Therefore, the affirmative result was obtained for the presumption that the reaction of (..gamma.., ..cap alpha../sub 0/) of the nuclei around these energy levels can be explained by the statistical theory. The angular distribution of /sup 56/Fe (..gamma.., ..cap alpha../sub 0/) with 17 MeV electron energy was also measured, and the E2/E1 ratio was obtained. In the measurement of the /sup 56/Fe ( Gamma , ..cap alpha../sub 0/) reaction cross section, a natural target of 2.69 mg/cm/sup 2/ was irradiated with an electron beam with energy from 15 MeV to 25 MeV at intervals of 0.5 MeV, and the emitted ..cap alpha.. particles were detected by a broad band magnetic distribution meter. The measured cross section of the (..gamma.., ..cap alpha../sub 0/) reaction agreed with the calculated one based on statistical theory. If this fact is recognized in many nuclei, the cross section of the (..gamma.., ..cap alpha../sub 0/) reaction on those nuclei has the following characteristics. When the increasing rate of the product of a complex nucleus formation cross section and ..cap alpha../sub 0/ penetration factor is larger than that of the sum of all penetration factors of possible channels, the cross section of the (..gamma.., ..cap alpha../sub 0/) reaction increases, and takes a peak value when the above two increasing rates agree with each other.

  10. Effect of tamoxifen pre-treatment on the retention of tritiated oestradiol and 5. cap alpha. -dihydrotestosterone and on glucose metabolism in human breast carcinomas

    Energy Technology Data Exchange (ETDEWEB)

    Deshpande, N; Mitchell, I [Imperial Cancer Research Fund, London (UK). Labs.; Hughes, D

    1978-05-01

    The effect of pre-treatment with tamoxifen on glucose metabolism and retention of injected oestradiol-17B and 5..cap alpha..-dihydrotestosterone by human breast carcinomas were studied in patients undergoing mastectomy. The following effects were observed: the pretreatment reduced retention of oestradiol-17B whereas a small but statistically significant rise in 5..cap alpha..-dihydrotestosterone accumulation was observed. There was an increase in both phosphofructokinase (PFK) and glucose-6-phosphate dehydrogenase (G6PDH) activities in tumours from treated patients whereas ..cap alpha..-glycerolphosphate dehydrogenase (..cap alpha..-GPDH) activity was significantly reduced in the same tumours. The significance of these findings is discussed and it is argued that these changes in carbohydrate metabolism may not be due to the blocking of hormone receptors.

  11. Radioimmunological determination of 5. cap alpha. -pregnane-3,20-dione in the peripheral venous blood of pregnant women showing pathological estriol values and/or HPL values or gestosis, on the basis of the gestational age. Radioimmunologische Bestimmung des 5. cap alpha. -Pregnan-3,20-dion im peripheren Venenblut schwangerer Frauen einer Gruppe mit pathologischen Oestriol- bzw. HPL-Werten und einer Gestosegruppe in Abhaengigkeit vom Gestationsalter

    Energy Technology Data Exchange (ETDEWEB)

    Klemm-Wolfgramm, E.

    1984-01-01

    A modified method of extraction and radioimmunological determination (iodine-125) is described, designed to monitor the concentrations of 5..cap alpha..-pregnandione (5..cap alpha..-DHP) in patients showing a pathological course of pregnancy and to examine the role of 5..cap alpha..-DHP blood levels in the development of gestosis. In this study, a control group was compared with two patient groups showing either (a) gestosis or (b) reduced levels of estriol and/or HPL. (1) In gestosis, the levels of 5..cap alpha..-DHP showed significant reductions that were proportionate to the degree of the disease, whereas decreases in these hormone levels were only observed to a minor extent in connection with pathological values of estriol and/or HPL. (2) The age of the patient had no influence on the hormone concentrations. (3) The increases in 5..cap alpha..-DHP seen in multiparae were only slight and did not attain any statistical significance. (4) No links were established between the concentrations of HPL and 5..cap alpha..-DHP in the maternal plasma and the development of the fetus. (5) Significantly reduced values of 5..cap alpha..-DHP were determined in mothers showing disorders of fetoplacental function (birth weights between 2500 and 3500 g) or gestosis (birth weights above 3500 g). (6) There were no relationships between the maternal serum levels of estriol, HPL and 5..cap alpha..-DHP and the sex of the fetus. (TRV).

  12. Direct Amination of alpha-Hydroxy Amides

    NARCIS (Netherlands)

    Chandgude, Ajay L.; Dömling, Alexander

    A TiCl4-mediated reaction for the direct amination of alpha-hydroxy amides has been developed. This simple, general, additive/base/ligand-free reaction is mediated by economical TiCl4. The reaction runs under mild conditions. This highly efficient C-N bond formation protocol is valid for diverse

  13. Neutron transition multipole moment for /sup 88/Sr(. cap alpha. ,. cap alpha. ')/sup 88/Sr (2/sup +/, 1. 84 MeV)

    Energy Technology Data Exchange (ETDEWEB)

    Datta, S.K.; Ray, S.; Majumdar, H.; Ghosh, S.K.; Samanta, C.; Dasgupta, P.; Chintalapudi, S.N.; Banerjee, S.R.

    1989-04-01

    The neutron transition multipole moment, M/sub n/, for (0/sup +/..-->..2/sup +/, 1.84 MeV) transition is inferred by measuring the (..cap alpha..,..cap alpha..') angular distribution at E/sub ..cap alpha../ = 50 MeV and comparing it with a microscopic distorted-wave Born approximation calculation. Proton transition densities are taken from electron scattering data. M/sub n//M/sub p/ is found to be substantially less than N/Z in agreement with the (p,p') result.

  14. Radioimmunological determination of. cap alpha. -MSH and ACTH in the rat

    Energy Technology Data Exchange (ETDEWEB)

    Usategui Echeverria, R; Oliver, C; Vaudry, H; Lombardi, G; Rozenberg, I; Vague, J [Centre Hospitalier Universitaire de la Timone, 13 - Marseille (France)

    1975-09-01

    Specific and sensitive radioimmunoassay methods for ..cap alpha..-MSH and ACTH are reported. They make possible specific measurements of each hormone in rat plasma or pituitary extracts. Endogenous ..cap alpha..-MSH and ACTH extracted from plasma or pituitary show the same immunoreactivity than synthetic ..cap alpha..-MSH and ACTH. ..cap alpha..-MSH and ACTH levels vary independently from each other in the following conditions: circadian rythm, corticoid treatment, adrenalectomy, ether stress, haloperidol injection.

  15. PROCESS FOR HYDROGENOLYSIS OF ALPHA-HYDROXY ESTERS OR ACIDS USING A HETEROGENEOUS CATALYST

    DEFF Research Database (Denmark)

    2017-01-01

    The present invention relates to a method for hydrogenolysis of alpha-hydroxy esters or acids, comprising reacting the alpha-hydroxy ester or acid in the presence of a heterogeneous catalyst. The present invention also relates to a method for producing propionic acid ester, and the use of any...

  16. Development of calcium-permeable alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors in cultured neocortical neurons visualized by cobalt staining

    DEFF Research Database (Denmark)

    Jensen, J B; Schousboe, A; Pickering, D S

    1998-01-01

    The developmental expression of calcium (Ca2+)-permeable alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) and kainate receptors in cultured neocortical neurons was evaluated by using cobalt uptake, a histochemical method that identifies cells expressing Ca2+-permeable, non-N-methyl-D-aspartate...

  17. Preparation of radioiodinated insulin and thyroid stimulating hormone using 1,3,4,6-tetrachloro-3. cap alpha. , 6. cap alpha. -diphenylglycouril (iodogen) for radioimmunoassay

    Energy Technology Data Exchange (ETDEWEB)

    Pillai, M R.A.; Gupte, J H; Jyotsna, T; Mani, R S

    1987-11-01

    Radioiodinated insulin and thyroid stimulating hormones were prepared using 1,3,4,6-tetrachloro-3..cap alpha.., 6..cap alpha..-diphenylglycouril (iodogen). Conditions of iodination like concentration of iodogen, reaction time, etc. were optimized to get maximum yield. Stability studies of iodogen coated tubes were carried out over a period of time. The dependence of iodination yield on varying amounts of activity and protein concentration were investigated. Iodination yield over a range of pH was also studied. The radiolabelled hormones prepared by this method were used in radioimmunoassay and compared with tracers prepared by the Chloramine-T method. (author) 16 refs.; 5 tabs.

  18. Reconstruction of spin-tensor of 4. 43 MeV state density matrix of the /sup 12/C nucleus in the /sup 12/C(. cap alpha. ,. cap alpha. sub(1). gamma. sub(4,43))/sup 12/C reaction at Esub(. cap alpha. )=25 MeV

    Energy Technology Data Exchange (ETDEWEB)

    Gurevich, G.S.; Lebedev, V.M.; Orlova, N.V.; Spasskij, A.V.; Teplov, I.B.; Shakhvorostova, G.V.; Belkina, M.R. (Moskovskij Gosudarstvennyj Univ. (USSR). Nauchno-Issledovatel' skij Inst. Yadernoj Fiziki)

    1984-01-01

    The results of measuring double differential cross sections of the reaction of inelastic scattering 24.8 MeV ..cap alpha..-particles sup(12)C(..cap alpha.., ..cap alpha..sub(1)..gamma..sub(4.43))sup(12)C in different planes of ..gamma..-quantum escape relatively to the plane of the reaction phisub(..gamma..)=30, 60 and 90 deg are presented. Non-monochromaticity of the beam made up 1%. Functions of angular correlation of the reaction are measured for four angles THETAsub(..cap alpha..)=21, 39, 59 and 135 deg corresponding to maxima of differential cross section in angular distribution of inelastically scattered ..cap alpha..-particles and for THETAsub(..cap alpha..)=89 deg corresponding to the minimum of angular distribution. The results of measurements permit to reconstruct all the components of irreducible spin-tensors of the matrix of state density 4.43 MeV (2/sup +/) formed in this reaction. The values of populations of substates by the projection of the spin of this state are obtained. The analysis of the obtained results testify to the fact that mechanism of inelastic scattering is not reduced to impulse approximation and mechanisms associated with delay in interaction do not make noticeable contribution for the given angles of ..cap alpha..-particle escape.

  19. Nicotinic cholinergic receptor in brain detected by binding of. cap alpha. -(/sup 3/H)bungarotoxin

    Energy Technology Data Exchange (ETDEWEB)

    Eterovic, V A; Bennett, E L

    1974-01-01

    ..cap alpha..-(/sup 3/H)bungarotoxin was prepared by catalytic reduction of iodinated ..cap alpha..-bungarotoxin with tritium gas. Crude mitochondrial fraction from rat cerebral cortex bound 40 x 10/sup -15/ to 60 x 10/sup -15/ moles of ..cap alpha..-(/sup 3/H)bungarotoxin per mg of protein. This binding was reduced by 50% in the presence of approx. 10/sup -6/ M d-tubocurarine or nicotine, 10/sup -5/ M acetylcholine, 10/sup -4/ M carbamylcholine or decamethonium or 10/sup -3/ M atropine. Hexamethonium and eserine were the least effective of the drugs tested. Crude mitochondrial fraction was separated into myelin, nerve endings, and mitochondria. The highest binding of toxin per mg of protein was found in nerve endings, as well as the greatest inhibition of toxin binding by d-tubocurarine. Binding of ..cap alpha..-(/sup 3/H)bungarotoxin to membranes obtained by osmotic shock of the crude mitochondrial fraction indicates that the receptor for the toxin is membrane bound. /sup 125/I-labeled ..cap alpha..-bungarotoxin, prepared with Na/sup 125/I and chloramine T, was highly specific for the acetylcholine receptor in diaphragm, however, it was less specific and less reliable than ..cap alpha..-(/sup 3/H)bungarotoxin in brain. It is concluded that a nicotinic cholinergic receptor exists in brain, and that ..cap alpha..-(/sup 3/H)bungarotoxin is a suitable probe for this receptor.

  20. Angular correlation between short-range. cap alpha. particles and. gamma. quanta

    Energy Technology Data Exchange (ETDEWEB)

    Kul' chitskii, L A; Latyshev, G D; Bulyginskii, D G

    1949-01-01

    Chang (Phys. Rev. 69, 60(1946); 70, 632(1946)) has found that the intensities of short-range ..cap alpha.. rays of Po and Ra are considerably higher than the values given by the Geiger-Nuttall law. This can be explained by assuming surface vibrations of ..cap alpha..-radioactive nuclei, which produce deformations and corresponding lowerings of the potential barrier in certain directions. In this case an angular correlation should exist between the short-range ..cap alpha.. ray and the accompanying ..gamma.. quantum. The authors checked this conclusion by applying the coincidence method to the ..cap alpha.. and ..gamma.. radiations of a mixture of RdTh (/sup 228/Th) and ThC (/sup 212/Bi). Maxima of coincidence numbers occur at angles 45 and 135 deg., with lesser maxima at 0 and 180 deg. Theoretical considerations show that in cases (like the one investigated) where the nuclear spin before and after the ..cap alpha.. and ..gamma.. emissions is zero, the angular correlations are uniquely determined whatever the deformation caused by the vibration; in other cases, the correlation depends on the kind of deformation. Therefore, it would be interesting to investigate the case of Pa, whose nuclear spin is not zero and the decay exhibits intensive groups of short-range ..cap alpha.. particles.

  1. Evaluation of GABAergic neuroactive steroid 3alpha-hydroxy-5alpha-pregnane-20-one as a neurobiological substrate for the anti-anxiety effect of ethanol in rats.

    Science.gov (United States)

    Hirani, Khemraj; Sharma, Ajay N; Jain, Nishant S; Ugale, Rajesh R; Chopde, Chandrabhan T

    2005-07-01

    Acute systemic ethanol administration is known to elevate plasma and cerebral levels of neuroactive steroid 3alpha-hydroxy-5alpha-pregnane-20-one (3alpha, 5alpha-THP; allopregnanolone) to a concentration sufficient to potentiate GABA(A) receptors. We have earlier demonstrated that 3alpha, 5alpha-THP mediates the antidepressant-like effect of ethanol in Porsolt forced swim test. The aim of the present study is to explain the relationship between endogenous GABAergic neurosteroids and anxiolytic effect of ethanol in Sprague-Dawley rats. The mediation of 3alpha, 5alpha-THP in the anti-anxiety effect of ethanol was assessed by pharmacological interactions of ethanol with various endogenous neurosteroidal modulators and using simulated physiological conditions of altered neurosteroid content in elevated plus maze (EPM) test. Pretreatment of 3alpha, 5alpha-THP (0.5-2.5 mug/rat, i.c.v.) or neurosteroidogenic agents such as 3alpha, 5alpha-THP precursor progesterone (5 or 10 mg/kg, i.p.), 11-beta hydroxylase inhibitor metyrapone (50 or 100 mg/kg, i.p.) or the GABA(A) receptor agonist muscimol (25 ng/rat, i.c.v.) significantly potentiated the anti-anxiety effect of ethanol (1 g/kg, i.p.). On the other hand, the GABAergic antagonistic neurosteroid dehydroepiandrosterone sulphate (DHEAS) (1 mg/kg, i.p.), the GABA(A) receptor blocker bicuculline (1 mg/kg, i.p.), the 5alpha-reductase inhibitor finasteride (50 x 2 mg/kg, s.c.) or the mitochondrial diazepam binding inhibitory receptor antagonist PK11195 (1 mg/kg, i.p.) reduced ethanol-induced preference of time spent and number of entries into open arms. Anti-anxiety effect of ethanol was abolished in adrenalectomized (ADX) rats as compared to sham-operated control. This ADX-induced blockade was restored by prior systemic injection of progesterone, signifying the contribution of peripheral steroidogenesis in ethanol anxiolysis. Socially isolated animals known to exhibit decreased brain 3alpha, 5alpha-THP and GABA(A) receptor

  2. X. cap alpha. method with pseudopotentials

    Energy Technology Data Exchange (ETDEWEB)

    Szasz, L. (Fordham Univ., New York (USA). Dept. of Physics)

    1980-06-01

    The X..cap alpha.. method for an atom or molecule is transformed into an all-electron pseudopotential formalism. The equations of the X..cap alpha.. method are exactly transformed into pseudo-orbital equations and the resulting pseudopotentials are replaced by simple density-dependent potentials derived from Thomas-Fermi model. It is shown that the new formalism satisfies the virial theorem. As the first application, it is shown that the model explains the shell-structure of atoms by the property that the pseudo-orbitals for the (ns), (np), (nd), etc. electrons are, in a very good approximation, the solutions of the same equation and have their maxima at the same point thereby creating the peaks in the radial density characterizing the shell structure.

  3. Physiological basis of tingling paresthesia evoked by hydroxy-alpha-sanshool.

    Science.gov (United States)

    Lennertz, Richard C; Tsunozaki, Makoto; Bautista, Diana M; Stucky, Cheryl L

    2010-03-24

    Hydroxy-alpha-sanshool, the active ingredient in plants of the prickly ash plant family, induces robust tingling paresthesia by activating a subset of somatosensory neurons. However, the subtypes and physiological function of sanshool-sensitive neurons remain unknown. Here we use the ex vivo skin-nerve preparation to examine the pattern and intensity with which the sensory terminals of cutaneous neurons respond to hydroxy-alpha-sanshool. We found that sanshool excites virtually all D-hair afferents, a distinct subset of ultrasensitive light-touch receptors in the skin and targets novel populations of Abeta and C fiber nerve afferents. Thus, sanshool provides a novel pharmacological tool for discriminating functional subtypes of cutaneous mechanoreceptors. The identification of sanshool-sensitive fibers represents an essential first step in identifying the cellular and molecular mechanisms underlying tingling paresthesia that accompanies peripheral neuropathy and injury.

  4. Synthetic. cap alpha. subunit peptide 125-147 of human nicotinic acetylcholine receptor induces antibodies to native receptor

    Energy Technology Data Exchange (ETDEWEB)

    McCormick, D.J.; Griesmann, G.E.; Huang, Z.; Lennon, V.A.

    1986-03-05

    A synthetic peptide corresponding to residues 125-147 of the Torpedo acetylcholine receptor (AChR) ..cap alpha.. subunit proved to be a major antigenic region of the AChR. Rats inoculated with 50 ..mu..g of peptide (T ..cap alpha.. 125-147) developed T cell immunity and antibodies to native AChR and signs of experimental autoimmune myasthenia gravis. They report the synthesis and preliminary testing of a disulfide-looped peptide comprising residues 125-147 of the human AChR ..cap alpha.. subunit. Peptide H ..cap alpha.. 125-147 differs from T ..cap alpha.. 125-147 at residues 139 (Glu for Gln) and 143 (Ser for Thr). In immunoprecipitation assays, antibodies to Torpedo AChR bound /sup 125/I-labelled H..cap alpha.. 125-147 antibody bound H..cap alpha.. 125-147, but monoclonal antibodies to an immunodominant region of native AChR bound neither H..cap alpha.. 125-147 nor T ..cap alpha.. 125-147. Rats immunized with H ..cap alpha.. 125-147 produced anti-mammalian muscle AChR antibodies that induced modulation of AChRs from cultured human myotubes. Thus, region 125-147 of the human AChR ..cap alpha.. subunit is extracellular in muscle, and is both antigenic and immunogenic. It remains to be determined whether or not autoantibodies to this region may in part cause the weakness or myasthenia gravis in man.

  5. Accumulation of glycation products in. cap alpha. -H pig lens crystallin and its bearing to diabetic cataract genesis

    Energy Technology Data Exchange (ETDEWEB)

    Vidal, P; Cabezas-Cerrato, J

    1988-01-01

    The incorporation of /sup 11/C-glucose in native pig crystalline by in vitro incubation was found, after subsequent dialysis, to affect all 5 classes of crystallin separated by Sepharose CL-6B column chromatography. Though the radioactivity of the ..cap alpha..-H fraction was three times greater than that of any of the others, autoradiographs of SDS-PAGE gels showed /sup 11/C-glucose adducts to be present in all soluble protein subunits, without there being any evidence of preferential glycation of the ..cap alpha..-H subunits. The concentration of stable glycation products in the ..cap alpha..-H chromatographic fraction of soluble crystallins is suggested to be due the addition of glycated material to this fraction as result of glycation-induced hyperaggregation, and not because the ..cap alpha..-H subunits were especially susceptible to glycation.

  6. Kinetic properties of /sup 3/H-16. cap alpha. -gitoxin in the isolated guinea-pig atrium

    Energy Technology Data Exchange (ETDEWEB)

    Haustein, K O; Glusa, E [Medizinische Akademie, Erfurt (German Democratic Republic)

    1978-04-01

    The accumulation and the loss of (/sup 3/H)-16..cap alpha..-gitoxin were estimated in correlation with its positive inotropic effect using the isolated spontaneously beating guinea-pig atrium. The properties of 16..cap alpha..-gitoxin were compared with those of (/sup 3/H)-ouabain and (/sup 3/H)-digitoxin. The experiments were performed with positive inotropic equieffective glycoside concentrations. During a 2-hr incubation period, 16..cap alpha..-gitoxin was accumulated to a low extent (2.05 nmoles per g w.w., tissue/medium (T/M) ratio =0.66). Similar results were obtained with ouabain (47.5 pmoles per g w.w.; T/M ratio = 0.51), while digitoxin was accumulated to a high extent (266 pmoles per g w.w.; T/M ratio = 2.98). Wash-out experiments demonstrated that the inotropic effect disappears more rapidly than the loss of tissue radioactivity occurred, the effects of 16..cap alpha..-gitoxin were diminished more easily after wash-out than those of ouabain and digitoxin. In the presence of 1.0 instead of 0.1 vol-% dimethylformamide, both the accumulation of radioactivity (5.0 nmoles per g w.w.; T/M ratio = 1.58) and the positive inotropic effect are enhanced. From the experiments it was concluded: (1) 16..cap alpha..-gitoxin has similar kinetic properties as ouabain. (2) The concentration of dimethylformamide used influences the kinetic behaviour on the tissue level. (3) No correlation exists neither between the extent of the positive inotropic effect and theamount of accumulated glycoside, nor between the loss of tissue radioactivity and the disappearance of positive inotropic effect.

  7. Agonist-induced affinity alterations of a central nervous system. cap alpha. -bungarotoxin receptor

    Energy Technology Data Exchange (ETDEWEB)

    Lukas, R.J.; Bennett, E.L.

    1979-01-01

    The ability of cholinergic agonists to block the specific interaction of ..cap alpha..-bungarotoxin (..cap alpha..-Bgt) with membrane-bound sites derived from rat brain is enhanced when membranes are preincubated with agonist. Thus, pretreatment of ..cap alpha..-Bgt receptors with agonist (but not antagonist) causes transformation of sites to a high-affinity form toward agonist. This change in receptor state occurs with a half-time on the order of minutes, and is fully reversible on dilution of agonist. The results are consistent with the identity of ..cap alpha..-Bgt binding sites as true central nicotinic acetylcholine receptors. Furthermore, this agonist-induced alteration in receptor state may represent an in vitro correlate of physiological desensitization. As determined from the effects of agonist on toxin binding isotherms, and on the rate of toxin binding to specific sites, agonist inhibition of toxin binding to the high-affinity state is non-competitive. This result suggests that there may exist discrete toxin-binding and agonist-binding sites on central toxin receptors.

  8. Effects of local anesthetics on cholinergic agonist binding affinity of central nervous system. cap alpha. -bungarotoxin receptors

    Energy Technology Data Exchange (ETDEWEB)

    Lukas, R.L.; Bennett, E.L.

    1979-12-01

    In general, pharmacological effects of local anesthetics may be attributed to their ability to reversibly block the propagation of nerve and muscle action potentials. At physiologically potent concentrations, local anesthetics (LA) also act as noncompetitive antagonists of the physiological response of post-synaptic nicotinic acetylcholine receptors (nAChR) to cholinergic agonists, and increase agonist binding affinities of nAChR from electric organ. It is postulated that the primary site of LA action on nAChR function is at the receptor-coupled ionophore. Furthermore, LA-nAChR ionophore interactions are thought to accelerate physiological desensitization of nAChR, manifest biochemically as increased affinity of nAChR for agonist. Specific receptors for ..cap alpha..-bungarotoxin (..cap alpha..-Bgt), a potent competitive antagonist at nAChR sites in the periphery, have been detected in rat central nervous system membrane preparations. The affinity of these central ..cap alpha..-Bgt receptors (..cap alpha..-BgtR) for cholinergic agonists is found to increase on exposure to agonist. Nevertheless, on the basis of inconsistent pharmacological and physiological results, uncertainty remains regarding the relationship between ..cap alpha..-BgtR and authentic nAChR in the CNS, despite a wide body of biochemical and histological evidence consistent with their identity. Reasoning that if CNS ..cap alpha..-BgtR are true in nAChR, coupled to functional ion channels, LA might be expected to cause biochemically measurable increases in ..cap alpha..-BgtR affinity for cholinergic agonists, we have undertaken a study of the effects of LA on the ability of acetylcholine (ACh) to inhibit interaction of ..cap alpha..-BgtR with /sup 3/H-labeled ..cap alpha..-Bgt.

  9. MFTF-. cap alpha. + T progress report

    Energy Technology Data Exchange (ETDEWEB)

    Nelson, W.D. (ed.)

    1985-04-01

    Early in FY 1983, several upgrades of the Mirror Fusion Test Facility (MFTF-B) at Lawrence Livermore National Laboratory (LLNL) were proposed to the fusion community. The one most favorably received was designated MFTF-..cap alpha..+T. The engineering design of this device, guided by LLNL, has been a principal activity of the Fusion Engineering Design Center during FY 1983. This interim progress report represents a snapshot of the device design, which was begun in FY 1983 and will continue for several years. The report is organized as a complete design description. Because it is an interim report, some parts are incomplete; they will be supplied as the design study proceeds. As described in this report, MFTF-..cap alpha..+T uses existing facilities, many MFTF-B components, and a number of innovations to improve on the physics parameters of MFTF-B. It burns deuterium-tritium and has a central-cell Q of 2, a wall loading GAMMA/sub n/ of 2 MW/m/sup 2/ (with a central-cell insert module), and an availability of 10%. The machine is fully shielded, allows hands-on maintenance of components outside the vacuum vessel 24 h after shutdown, and has provisions for repair of all operating components.

  10. Identification and subcellular localization of a 21-kilodalton molecule using affinity-purified antibodies against. cap alpha. -transforming growth factor

    Energy Technology Data Exchange (ETDEWEB)

    Hazarika, P.; Pardue, R.L.; Earls, R.; Dedman, J.R.

    1987-04-07

    Monospecific antibodies were generated against each of six different peptide sequences derived from rat and human ..cap alpha..-transforming growth factor (..cap alpha..-TGF). The affinity-purified antibody to the 17 amino acid carboxyl-terminal portion of the molecule proved most useful in detecting ..cap alpha..-TGF. When used in a peptide-based radioimmunoassay, it was possible to measure nanogram quantities of native ..cap alpha..-TGF in conditioned cell culture media. When used to analyze cell lysate, these antibodies specifically recognized a 21-kilodalton protein species. Indirect immunofluorescence localization procedures revealed a high concentration of ..cap alpha..-TCF in a perinuclear ring with a diffuse cytoplasmic distribution. These results suggest that a precursor form of ..cap alpha..-TGF has a cellular role beyond that of an autocrine growth factor.

  11. Involvement of prostaglandins F/sub 2. cap alpha. / and E/sub 1/ with rabbit endometrium

    Energy Technology Data Exchange (ETDEWEB)

    Orlicky, D.J.

    1985-01-01

    Several growth factors and hormones are thought to play a role in the growth control of endometrial cells. The authors have shown that prostaglandin F/sub 2..-->../ (PGF/sub 2..cap alpha../) is a growth factor for primary cultures of rabbit endometrium cultured in chemically-defined serum-free medium and that prostaglandin E/sub 1/ (PGE/sub 1/) antagonizes the PGF/sub 2..-->../ induction of growth. Both (/sup 3/H)PGF/sub 2..cap alpha../ and (/sup 3/H)PGE/sub 1/ bind in a time and temperature dependent, dissociable, saturable and specific manner. The binding of (/sup 3/H)PGF/sub 2..cap alpha../ and (/sup 3/H)PGE/sub 1/ can be both down and up regulated and is enzyme sensitive. PGE /sub 1/ stimulates intracellular cAMP synthesis and accumulation in a time and concentration dependent manner. PGF/sub 2..cap alpha../ probably exerts its effects through an amiloride-sensitive intermediate. Both PGF/sub 2..cap alpha../ and PGE/sub 1/ are constitutively synthesized by these primary cultures, and they have shown this synthesis to be both drug and hormone sensitive. They hypothesize that it is the ratio, rather than the absolute quantities, of PGF/sub 2..cap alpha../ and PGE/sub 1/ which is of more importance in the regulation of endometrial cell growth. Furthermore, they believe this regulation of endometrial growth plays a role in control of proliferation during the decidual response and that a derangement in the ratio of these prostaglandins may lead to either infertility or hyperplasia. The ability of these cultures to synthesize prostaglandins in a hormonally regulatable manner may be of importance in the study of dysmenorrhea and uterine cramping as caused by the myometrial contracting prostaglandin, PGF/sub 2..cap alpha../.

  12. Crystal structure of 5-hydroxy-5-propylbarbituric acid

    Directory of Open Access Journals (Sweden)

    Thomas Gelbrich

    2015-11-01

    Full Text Available Molecules of the title compound, C7H10N2O4, systematic name 5-hydroxy-5-propylpyrimidine-2,4,6(1H,3H,5H-trione, form a hydrogen-bonded framework which is based on three independent hydrogen bonds, N—H...O(carbonyl, N—H...O(hydroxy and O—H...O(carbonyl. This framework has the topology of the 5-connected nov net. Each molecule is linked to five other molecules via six hydrogen bonds, and the descriptor of the hydrogen-bonded structure is F65[44.66-nov]. The crystal packing is isostructural with that of the previously reported 5-hydroxy-5-ethyl analogue.

  13. Scattering of alpha particles from /sup 12/C and the /sup 12/C(. cap alpha. ,. gamma. )/sup 16/O stellar reaction rate

    Energy Technology Data Exchange (ETDEWEB)

    Plaga, R.; Becker, H.W.; Redder, A.; Rolfs, C.; Trautvetter, H.P.; Langanke, K.

    1987-04-06

    The elastic scattering of alpha particles from /sup 12/C has been investigated for 35 angles in the range theta/sub lab/ = 22/sup 0/ to 163/sup 0/ and for 51 energies at E/sub ..cap alpha../ = 1.0 to 6.6 MeV. The extracted phase shifts for l=0 to 6 partial waves have been parametrized in terms of the multilevel R-matrix formalism. Information on the deduced parameters of states in /sup 16/O is reported. The data reveal reduced ..cap alpha..-particle widths for the 6.92 and 7.12 MeV subthreshold states consistent with recent work. The implications for the stellar reaction rate of /sup 12/C(..cap alpha..,..gamma..)/sup 16/O are discussed.

  14. Pilot plant production of glucose from starch with soluble. cap alpha. -amylase and immobilized glucoamylase

    Energy Technology Data Exchange (ETDEWEB)

    Lee, D D; Reilly, P J; Collins, Jr, E V

    1975-01-01

    Pilot plant studies were conducted on cooking and thinning of corn starch with free ..cap alpha..-amylase and the conversion of the resulting dextrin with immobilized glucoamylase adsorbed on porous SiO/sub 2/. Feeds of intermediate DE values gave maximum yields unless the flow rate of low DE feeds was decreased. Final DE values and glucose concentrations after dextrin treated with Thermamyl 60 ..cap alpha..-amylase had been further hydrolyzed in an immobilized glucoamylase column, were slightly lower than they were when free glucoamylase was used. Similar results were obtained when dextrin, thinned with HT-1000 ..cap alpha..-amylase, was hydrolyzed at 38/sup 0/ and pH 4.4 in the immobilized glucoamylase column. Free glucoamylase yielded values of DE and glucose almost identical with dextrin thinned with Thermamyl 60 ..cap alpha..-amylase. Yields with the free glucoamylase were also slightly higher than they were with SiO/sub 2/-bound enzyme.

  15. Martensite. gamma. -->. cap alpha. transformations in various purity Fe-Ni-Mo alloys

    Energy Technology Data Exchange (ETDEWEB)

    Nikitina, I.I.; Rozhkova, A.S. (Tsentral' nyj Nauchno-Issledovatel' skij Inst. Chernoj Metallurgii, Moscow (USSR))

    1982-06-01

    Kinetics of isothermal and athermal ..gamma.. ..-->.. ..cap alpha.. martensitic transitions in the Fe-25.5% Ni-4.5% Mo alloys with different degree of purity is studied. The determinant role of dislocation blocking by interstitials in stabilization of isothermal martensitic transformation is displayed. Presented are the data permitting to consider that the character of martensitic transition kinetics is determined by the ratio of the process moving force and resistance to microplastic deformation.

  16. Purification and physicochemical properties of. cap alpha. -amylase from irradiated wheat

    Energy Technology Data Exchange (ETDEWEB)

    Machaiah, J P; Vakil, U K [Bhabha Atomic Research Centre, Bombay (India). Biochemistry and Food Technology Div.

    1981-06-01

    ..cap alpha..-Amylases from control and gamma-irradiated (at 0.2 and 2.0 kGy dose levels) wheat seedlings were purified to homogeneity and characterized. The molecular weight of the enzyme from a 2 kGy irradiated sample was slightly lower than that of the control; other general and catalytic properties also showed some differences. ..cap alpha..-Amylase from the irradiated (2kGy) sample had a narrow range of pH optimum and was inactivated faster at alkaline pH and by heat treatment than the enzyme from unirradiated wheat. A high apparent Michaelis constant (Ksub(m)) and a low maximal velocity (Vsub(max)) for the hydrolysis of soluble starch catalyzed by the enzyme from irradiated (2kGy) wheat, suggested some modifications in the formation of the substrate ..cap alpha..-amylase complex. Further, of the total number of amino acid residues lost on irradiation, dicarboxylic amino acids constituted the largest percentage; these structural alterations in the enzyme may be responsible for its partial inactivation. The total sugars liberated upon amylolysis of starch with the 2kGy irradiated enzyme were lower than control, and there was accumulation of higher maltodextrins in the place of maltose.

  17. 15 beta-hydroxysteroids (Part IV). Steroids of the human perinatal period: the synthesis of 3 alpha,15 beta,17 alpha-trihydroxy-5 alpha-pregnan-20-one and its A/B-ring configurational isomers.

    Science.gov (United States)

    Reeder, A Y; Joannou, G E

    1995-12-01

    In recent years several 15 beta-hydroxysteroids have emerged pathognomonic of adrenal disorders in human neonates of which 3 alpha,15 beta,17 alpha-trihydroxy-5 beta-pregnan-20-one (2) was the first to be identified in the urine of newborn infants affected with congenital adrenal hyperplasia. In this investigation we report the synthesis of the three remaining 3 xi,5 xi-isomers, namely 3 alpha,15 beta,17 alpha-trihydroxy-5 alpha-pregnan-20-one (3), 3 beta,15 beta,17 alpha-trihydroxy-5 alpha-pregnan-20-one (7) and 3 beta,15 beta,17 alpha-trihydroxy-5 beta-pregnan-20-one (8) for their definitive identification in pathological conditions in human neonates. 3 beta,15 beta-Diacetoxy-17 alpha-hydroxy-5-pregnen-20-one (11), a product of chemical synthesis was converted to the isomeric 3 and 7, while conversion of 15 beta,17 alpha-dihydroxy-4-pregnen-3,20-dione (4), a product of microbiological transformation, resulted in the preparation of 8. In brief, selective acetate hydrolysis of 11 gave 15 beta-acetoxy-3 beta,17 alpha-dihydroxy-5-pregnen-20-one (12) which on catalytic hydrogenation gave 15 beta-acetoxy-3 beta,17 alpha-dihydroxy-5 alpha-pregnan-20-one (13) a common intermediate for the synthesis of the 3 beta(and alpha),5 alpha-isomers. Hydrolysis of the 15 beta-acetate gave 7, whereas oxidation with pyridinium chlorochromate gave 15 beta-acetoxy-17 alpha-hydroxy-5 alpha-pregnan-3,20-dione (14) which on reduction with L-Selectride and hydrolysis of the 15 beta-acetate gave 3. Finally, hydrogenation of 4 gave 15 beta, 17 alpha-dihydroxy-5 beta-pregnan-3,20-dione (10) which on reduction with L-Selectride gave 8.

  18. Synthesis of 3 alpha-deuterated 7 alpha-hydroxy-DHEA and 7-oxo-DHEA and application in LC-MS/MS plasma analysis

    Czech Academy of Sciences Publication Activity Database

    Sosvorova, L.K.; Sarek, J.; Vitku, J.; Kvasnica, Miroslav

    2016-01-01

    Roč. 112, AUG (2016), s. 88-94 ISSN 0039-128X Institutional support: RVO:61389030 Keywords : 7 alpha-Hydroxy-DHEA * 7-Oxo-DHEA * Deuterated standard Subject RIV: CE - Biochemistry Impact factor: 2.282, year: 2016

  19. Increased concentration of. cap alpha. - and. gamma. -endorphin in post mortem hypothalamic tissue of schizophrenic patients

    Energy Technology Data Exchange (ETDEWEB)

    Wiegant, V.M.; Verhoef, C.J.; Burbach, J.P.H.; de Wied, D.

    1988-01-01

    The concentrations of ..cap alpha..-, ..beta..- and ..gamma..-endorphin were determined by radioimmunoassay in HPLC fractionated extracts of post mortem hypothalamic tissue obtained from schizophrenic patients and controls. The hypothalamic concentration of ..cap alpha..- and ..gamma..-endorphin was significantly higher in patients than in controls. No difference was found in the concentration of ..beta..-endorphin, the putative precursor of ..cap alpha..- and ..gamma..-endorphins. These results suggest a deviant metabolism of ..beta..-endorphin in the brain of schizophrenic patients. Whether this phenomenon is related to the psychopathology, or is a consequence of ante mortem farmacotherapy, remains to be established.

  20. Structure of the radio emission from the NGC 1579/LkH. cap alpha. 101 region

    Energy Technology Data Exchange (ETDEWEB)

    Brown, R L [National Radio Astronomy Observatory, Charlottesville, Va. (USA); Broderick, J J; Knapp, G R

    1976-06-01

    Radio-frequency observations at 3.7 and 11 cm of the NGC 1579/LkH..cap alpha..101 region show that the radio emission arises in a compact, < 1'' core concentric with a more extended approximately 1' emission region. At these wavelengths the compact component is optically thick, with a spectrum increasing as ..nu.., whereas the extended region is optically thin and contributes at least 80 per cent of the total flux density. LkH..cap alpha..101 appears to be the source of excitation for all of the radio emission; this result, together with the total infrared luminosity, suggests that an appropriate spectral classification for LkH..cap alpha..101 is B1 IIe.

  1. cap alpha. -bungarotoxin binding properties of a central nervous system nicotinic acetylcholine receptor

    Energy Technology Data Exchange (ETDEWEB)

    Lukasiewicz, R J; Bennett, E L

    1978-01-01

    High-affinity, specific binding of radiolabeled ..cap alpha..-bungarotoxin to particulate fractions derived from rat brain shows saturability (B/sub max/ approx. = 37fmol/mg, K/sub D//sup app/ = 1.7 nM) and insensitivity to ionic strength, and is essentially irreversible (K/sub on/ = 5 x 10/sup 6/ min/sup -1/ x mol/sup -1/; K(displacement) = 1.9 x 10/sup -4/ min/sup -1/, tau/sub 1/2/ = 62 h). Subcellular distribution of specific sites is consistent with their location on synaptic junctional complex and post-synaptic membranes. These membrane-bound binding sites exhibit unique sensitivity to cholinergic ligands; pretreatment of membranes with cholinergic agonists (but not antagonists) induces transformation of ..cap alpha..-bungarotoxin binding sites to a high affinity form toward agonist. The effect is most marked for the natural agonist, acetylcholine. These results strongly support the notion that the entity under study is an authentic nicotinic acetylcholine receptor.

  2. Distribution and excretion of. cap alpha. -naphthylthio-(/sup 14/C)urea in Albino rats

    Energy Technology Data Exchange (ETDEWEB)

    Patil, T N; Radhakrishnamurty, R [Central Food Technological Research Inst., Mysore (India)

    1977-09-01

    ..cap alpha..-naphthylthio-(/sup 14/C) urea was synthesised by allowing potassium (/sup 14/C)thiocyanate to react with ..cap alpha..-naphthylamine. Its distribution and excretion were studied in Albino rats following the administration of this rodenticide. Considerable radioactivity observed in liver and kidney, increased till 8 hr and later decreased. About 80% of the activities present in serum and pleural effusion were found in the respective albumin fractions. Approximately 40% of the dose administered was excreted in urine and less than 1% in faeces in 20 hr. About 36% of the total urinary activity was recovered as unchanged compound and the rest was distributed in three metabolites with low Rsyb(f) values. Decrease in cytochsome P-450 content and activities of N, N-dimethylaniline demethylase, aryl 4-hydroxylase and reduced NAD dehydrogenase were observed in ..cap alpha..-naphthylathiourea-treated rats.

  3. Characterization and application of a radioimmunoassay for reduced, carboxymethylated human luteinizing hormone. cap alpha. -subunit. [/sup 125/I tracer technique

    Energy Technology Data Exchange (ETDEWEB)

    Keutmann, H.T.; Beitins, I.Z.; Johnson, L.; McArthur, J.W.

    1978-12-01

    We have established a double antibody RIA using a rabbit antiserum prepared against reduced, carboxymethylated (RCXM) human LH ..cap alpha..-subunit, with RCXM-..cap alpha.. as tracer and standard. This antiserum did not cross-react with any native gonadotropins or subunit, and reacted only weakly with RCXM-..cap alpha... A tryptic digest of RCXM ..cap alpha..-subunit was completely reactive, while chymotryptic digestion abolished all immunoreactivity. By testing with separate tryptic fragments, the recognition site could be localized to a segment close to the amino-terminus of the peptide chain. When applied to measurement of serum and urine, an immunoreactive species, parallel to RCXM ..cap alpha..-subunit by serial dilution, was found in concentrations of 1-2 ng/ml in serum and 3-4 ng/ml in urine. Similar levels of the immunoreactive component were found in conditions of elevated gonadotropins (e.g. pregnancy) as well as gonadotropin deficiency (panhypopituitarism and Kallmann's syndrome). After stimulation with LHRH, no rise was noted at times up to 6 h despite the fact that both LH and LH-..cap alpha.. were elevated. The data indicate that the sequence-specific antiserum may be detecting an immunoreactive form of ..cap alpha..-subunit of LH whose kinetics of appearance and disappearance differs from those of the native subunit.

  4. Effect of dietary protein on the excretion of. cap alpha. /sub 2u/, the sex-dependent protein of the adult male rat

    Energy Technology Data Exchange (ETDEWEB)

    Neuhaus, O W; Flory, W

    1975-01-01

    Adult male rates were maintained on normal (20 percent casein), protein-free (0 percent casein), high protein (50 percent casein), deficient protein (20 percent zein), and a supplemented, deficient protein (20 percent zein plus L-lysine and L-tryptophan) diets. Rats on a protein-free diet excreted approximately 1 mg ..cap alpha../sub 2u//24 h compared with a normal of 10-15 mg/24 h. Depleted rats placed on the normal diet showed a rapid restoration of the normal ..cap alpha../sub 2u/ excretion as well as total urinary proteins. Accumulation of ..cap alpha../sub 2u/ in the blood serum was measured in nephrectomized rats. Rats on the protein free diet accumulated only 30 percent of the ..cap alpha../sub 2u/ compared to normals. On a 50 precent casein diet, rats excreted 30-50 mg ..cap alpha../sub 2u//24 h. However, the accumulation was normal in the serum of nephrectomized rats. A high protein diet did not stimulate ..cap alpha../sub 2u/ synthesis but probably increased the renal loss of all urinary proteins. The excretion of ..cap alpha../sub 2u/ on a zein diet was reduced to the same degree as with the protein-free diet. Supplementation with lysine and tryptophan restored the capacity to eliminate ..cap alpha../sub 2u/ to near normal levels. Accumulation of ..cap alpha../sub 2u/ in the serum of nephrectomized rats kept on the zein diets showed that the effect was to suppress the synthesis of the ..cap alpha../sub 2u/. Supplementation restored the biosynthesis of ..cap alpha../sub 2u/. It is concluded that the effect of dietary protein on the excretion of urinary proteins in the adult male rat is caused in a large part by an influence on the hepatic biosynthesis of ..cap alpha../sub 2u/. The biosynthesis of this protein, which represents approximately 30 percent of the total urinary proteins, is dependent on an adequate supply of dietary protein.

  5. Application of multi-step direct reaction theory to 14 MeV neutron reaction, 3 (n,. cap alpha. )

    Energy Technology Data Exchange (ETDEWEB)

    Kumabe, I.; Matoba, M.; Fukuda, K. [Kyushu Univ., Fukuoka (Japan). Faculty of Engineering; Ikegami, H.; Muraoka, M [eds.

    1980-01-01

    Multi-step direct-reaction theory proposed by Tamura et al. has been applied to continuous spectra of the 14 MeV (n, ..cap alpha..) reaction with some modifications. Calculated results reproduce well the experimental energy and angular distributions of the 14 MeV (n, ..cap alpha..) reactions.

  6. Reaction /sup 56/Fe (. gamma. ,. cap alpha. /sub 0/) and /sup 56/Fe (. gamma. , p/sub 0/)

    Energy Technology Data Exchange (ETDEWEB)

    Tamae, T; Sugawara, M [Tohoku Univ., Sendai (Japan). Lab. of Nuclear Science; Tsubota, H

    1975-06-01

    Precise analysis was made on the cross section of the /sup 56/Fe (..gamma.., ..cap alpha../sub 0/) reaction and the angular distribution at Esub(e) = 17 MeV, including the systematic error. The (..gamma.., ..cap alpha../sub 0/) reaction cross section was compared with a calculation using the compound nucleus model, utilizing the photon absorption cross section derived from the experimental values of /sup 56/Fe (..gamma.., n) and /sup 56/Fe (..gamma.., p) cross sections. From the (..gamma.., ..cap alpha../sub 0/) reaction cross section data of various nuclei, an empirical formula was obtained for determining the position of a peak in the (..gamma.., ..cap alpha../sub 0/) reaction cross section. The /sup 56/Fe (..gamma.., p/sub 0/) reaction cross section measured at an excitation energy in the range of 14.6--25.0 MeV was compared with the calculated one with the compound nucleus model, but the form and size differ totally.

  7. Synthesis of omega-hydroxy carboxylic acids and alpha,omega-dimethyl ketones using alpha,omega-diols as alkylating agents.

    Science.gov (United States)

    Iuchi, Yosuke; Hyotanishi, Megumi; Miller, Brittany E; Maeda, Kensaku; Obora, Yasushi; Ishii, Yasutaka

    2010-03-05

    Synthesis of omega-hydroxy carboxylic acids and alpha,omega-dimethyl diketones was successfully achieved by using alpha,omega-diols as alkylating agents under the influence of an iridium catalyst. For example, the alkylation of butyl cyanoacetate with 1,13-tridecanediol in the presence of [IrCl(cod)](2) or [IrCl(coe)(2)](2) gave rise to butyl 2-cyano-15-hydroxypentadecanoate in good yield which is easily converted to cyclopentadecanolide (CPDL). In addition, the alkylation of acetone with 1,10-decanediol in the presence of [IrCl(cod)](2) and KOH resulted in an important muscone precursor, 2,15-hexadecanedione (HDDO), in good yield.

  8. A new highly selective metabotropic excitatory amino acid agonist: 2-amino-4-(3-hydroxy-5-methylisoxazol-4-yl)butyric acid

    DEFF Research Database (Denmark)

    Bräuner-Osborne, Hans; Sløk, F A; Skjaerbaek, N

    1996-01-01

    The homologous series of acidic amino acids, ranging from aspartic acid (1) to 2-aminosuberic acid (5), and the corresponding series of 3-isoxazolol bioisosteres of these amino acids, ranging from (RS)-2-amino-2-(3-hydroxy-5-methylisoxazol-4-yl)acetic acid (AMAA, 6) to (RS)-2-amino-6-(3-hydroxy-5......-methylisoxazol-4-yl)hexanoic acid (10), were tested as ligands for metabotropic excitatory amino acid receptors (mGlu1 alpha, mGlu2, mGlu4a, and mGlu6). Whereas AMAA (6) and (RS)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propinoic acid (AMPA, 7) are potent and highly selective agonists at N......-methyl-D-aspartic acid (NMDA) and AMPA receptors, respectively, the higher homologue of AMPA (7), (RS)-2-amino-4-(3-hydroxy-5-methylisoxazol-4-yl)butyric acid (homo-AMPA, 8), is inactive at ionotropic excitatory amino acid receptors. Homo-AMPA (8), which is a 3-isoxazolol bioisostere of 2-aminoadipic acid (3), was...

  9. Identification of a novel bile acid in swans, tree ducks, and geese: 3alpha,7alpha,15alpha-trihydroxy-5beta-cholan-24-oic acid.

    Science.gov (United States)

    Kakiyama, Genta; Iida, Takashi; Goto, Takaaki; Mano, Nariyasu; Goto, Junichi; Nambara, Toshio; Hagey, Lee R; Schteingart, Claudio D; Hofmann, Alan F

    2006-07-01

    By HPLC, a taurine-conjugated bile acid with a retention time different from that of taurocholate was found to be present in the bile of the black-necked swan, Cygnus melanocoryphus. The bile acid was isolated and its structure, established by (1)H and (13)C NMR and mass spectrometry, was that of the taurine N-acyl amidate of 3alpha,7alpha,15alpha-trihydroxy-5beta-cholan-24-oic acid. The compound was shown to have chromatographic and spectroscopic properties that were identical to those of the taurine conjugate of authentic 3alpha,7alpha,15alpha-trihydroxy-5beta-cholan-24-oic acid, previously synthesized by us from ursodeoxycholic acid. By HPLC, the taurine conjugate of 3alpha,7alpha,15alpha-trihydroxy-5beta-cholan-24-oic acid was found to be present in 6 of 6 species in the subfamily Dendrocygninae (tree ducks) and in 10 of 13 species in the subfamily Anserinae (swans and geese) but not in other subfamilies in the Anatidae family. It was also not present in species from the other two families of the order Anseriformes. 3alpha,7alpha,15alpha-Trihydroxy-5beta-cholan-24-oic acid is a new primary bile acid that is present in the biliary bile acids of swans, tree ducks, and geese and may be termed 15alpha-hydroxy-chenodeoxycholic acid.

  10. Synthesis of (19E)-3 beta,7 alpha-dihydroxy-17-oxoandrost-5-en-19-al 19-(O-carboxymethyl)oxime, a new hapten for 7 alpha-hydroxydehydroepiandrosterone (3 beta,7 alpha-dihydroxyandrost-5-en-17-one).

    Science.gov (United States)

    Pouzar, V; Slavíková, T; Cerńy, I

    1998-09-01

    The title compound was prepared in 11 steps from 17,17-ethylenedioxy-19-hydroxyandrost-5-en-3 beta-yl acetate. After tert-butyldimethylsilyl protection of the 19-hydroxyl group, a 7-oxo group was introduced by oxidation with 3,5-dimethylpyrazole-chromium trioxide complex, and then selectively reduced with L-Selectride to give a 7 alpha-hydroxy derivative. This partially protected triol was acetylated and desilylated to 3,7-diacetate. Subsequent oxidation with pyridine-chromium trioxide complex gave 19-aldehyde, which was transformed into the corresponding protected 19-(O-carboxymethyl)oxime. Successive ketal cleavage, deacetylation, and methyl ester splitting gave the final (19E)-3 beta,7 alpha-dihydroxy-17-oxoandrost-5-en-19-al 19-(O-carboxymethyl)oxime, designed as a hapten for 7 alpha-hydroxydehydroepiandrosterone immunoassays.

  11. Ap/sub 4/A interactions with a multiprotein form of DNA polymerase. cap alpha. - primase from HeLa cells

    Energy Technology Data Exchange (ETDEWEB)

    Baril, E F; Owen, M W; Vishwanatha, J K; Zamecnik, P C

    1984-06-01

    In previous studies, it was shown that Ap/sub 4/A can function as a primer for in vitro DNA synthesis by the multiprotein form of DNA polymerase ..cap alpha.. with single-stranded DNA and an octadecamer double-stranded DNA template. In these studies, the authors show that Ap/sub 4/A that is greater than 99% pure by high performance liquid chromatography also stimulates the incorporation of (..cap alpha../sup 32/P)ATP into the 10-15 oligoribonucleotide primer with poly(dT) template by the primase that is resolved from the polymerase ..cap alpha.. core enzyme. Other dinucleotides or dinucleotide polyphosphates (e.g. ApA, Ap/sub 2/A or Ap/sub 3/A) do not enhance the incorporation of (..cap alpha../sup 32/P)ATP in this reaction. The results from phosphate transfer experiments demonstrate a covalent linkage between (/sup 3/H)Ap/sub 4/A and the /sup 32/P-labeled oligoriboadenylate that is synthesized by the primase.

  12. Effects of combined maternal administration with alpha-ketoglutarate (AKG) and β-hydroxy-β-methylbutyrate (HMB) on prenatal programming of skeletal properties in the offspring.

    Science.gov (United States)

    Tatara, Marcin R; Krupski, Witold; Tymczyna, Barbara; Studziński, Tadeusz

    2012-05-11

    Nutritional manipulations during fetal growth may induce long-term metabolic effects in postnatal life. The aim of the study was to test whether combined treatment of pregnant sows with alpha-ketoglutarate and β-hydroxy-β-methylbutyrate induces additive long-term effects on skeletal system properties in the offspring. The study was performed on 290 pigs obtained from 24 sows divided into 4 equal groups and subjected to experimental treatment during two weeks before delivery. The first group consisted of control sows, while the second group received alpha-ketoglutarate. The third group was treated with β-hydroxy-β-methylbutyrate and the fourth group underwent combined administration of alpha-ketoglutarate and β-hydroxy-β-methylbutyrate. Piglets obtained from sows were reared until slaughter age to perform morphometric, densitometric and mechanical analyses of femur. Serum evaluations of growth hormone, insulin-like growth factor-1, bone-specific alkaline phosphatase and osteocalcin were performed in newborns and 90-day old piglets; additionally, plasma amino acid concentration was measured in newborns. Maternal treatment with alpha-ketoglutarate and β-hydroxy-β-methylbutyrate significantly reduced fattening time and increased birth body weight, daily body weight gain, bone weight, volumetric bone mineral density, geometrical parameters and mechanical endurance of femur. These effects were associated with increased serum concentrations of growth hormone, insulin-like growth factor-1, bone-specific alkaline phosphatase and osteocalcin. Furthermore, alpha-ketoglutarate and β-hydroxy-β-methylbutyrate administered solely or in combination significantly increased plasma level of 19 amino acids. Hormonal and amino acid evaluations in pigs indicate additive effects of AKG and HMB on systemic growth and development; however, determination of bone properties has not shown such phenomenon.

  13. Gating at the mouth of the acetylcholine receptor channel: energetic consequences of mutations in the alphaM2-cap.

    Directory of Open Access Journals (Sweden)

    Pallavi A Bafna

    2008-06-01

    Full Text Available Gating of nicotinic acetylcholine receptors from a C(losed to an O(pen conformation is the initial event in the postsynaptic signaling cascade at the vertebrate nerve-muscle junction. Studies of receptor structure and function show that many residues in this large, five-subunit membrane protein contribute to the energy difference between C and O. Of special interest are amino acids located at the two transmitter binding sites and in the narrow region of the channel, where CO gating motions generate a lowhigh change in the affinity for agonists and in the ionic conductance, respectively. We have measured the energy changes and relative timing of gating movements for residues that lie between these two locations, in the C-terminus of the pore-lining M2 helix of the alpha subunit ('alphaM2-cap'. This region contains a binding site for non-competitive inhibitors and a charged ring that influences the conductance of the open pore. alphaM2-cap mutations have large effects on gating but much smaller effects on agonist binding, channel conductance, channel block and desensitization. Three alphaM2-cap residues (alphaI260, alphaP265 and alphaS268 appear to move at the outset of channel-opening, about at the same time as those at the transmitter binding site. The results suggest that the alphaM2-cap changes its secondary structure to link gating motions in the extracellular domain with those in the channel that regulate ionic conductance.

  14. Dynamic. cap alpha. -transfer polarisation potentials and the large angle scattering of /sup 16/O + /sup 28/Si

    Energy Technology Data Exchange (ETDEWEB)

    Hussein, M S; Aleixo, A N; Canto, L F; Carrilho, P; Donangelo, R; Paula, L.S. de

    1987-07-01

    A closed expression is derived for the dynamic ..cap alpha..-transfer polarisation potential for heavy-ion elastic scattering. The back-angle angular distributions for the elastic scattering of /sup 16/O + /sup 28/Si obtained by adding this polarisation potential to the E-18 interaction are shown to be in good agreement with the data if an ..cap alpha..-transfer spectroscopic factor of 0.4 is used.

  15. Catalytic asymmetric epoxidation of alpha,beta-unsaturated amides: efficient synthesis of beta-aryl alpha-hydroxy amides using a one-pot tandem catalytic asymmetric epoxidation-Pd-catalyzed epoxide opening process.

    Science.gov (United States)

    Nemoto, Tetsuhiro; Kakei, Hiroyuki; Gnanadesikan, Vijay; Tosaki, Shin-Ya; Ohshima, Takashi; Shibasaki, Masakatsu

    2002-12-11

    The catalytic asymmetric epoxidation of alpha,beta-unsaturated amides using Sm-BINOL-Ph3As=O complex was succeeded. Using 5-10 mol % of the asymmetric catalyst, a variety of amides were epoxidized efficiently, yielding the corresponding alpha,beta-epoxy amides in up to 99% yield and in more than 99% ee. Moreover, the novel one-pot tandem process, one-pot tandem catalytic asymmetric epoxidation-Pd-catalyzed epoxide opening process, was developed. This method was successfully utilized for the efficient synthesis of beta-aryl alpha-hydroxy amides, including beta-aryllactyl-leucine methyl esters. Interestingly, it was found that beneficial modifications on the Pd catalyst were achieved by the constituents of the first epoxidation, producing a more suitable catalyst for the Pd-catalyzed epoxide opening reaction in terms of chemoselectivity.

  16. Mapping of the mouse actin capping protein {alpha} subunit genes and pseudogenes

    Energy Technology Data Exchange (ETDEWEB)

    Hart, M.C.; Korshunova, Y.O.; Cooper, J.A. [Washington Univ. School of Medicine, St. Louis, MO (United States)

    1997-02-01

    Capping protein (CP), a heterodimer of {alpha} and {beta} subunits, is found in all eukaryotes. CP binds to the barbed ends of actin filaments in vitro and controls actin assembly and cell motility in vivo. Vertebrates have three {alpha} isoforms ({alpha}1, {alpha}2, {alpha}3) produced from different genes, whereas lower organisms have only one gene and one isoform. We isolated genomic clones corresponding to the a subunits of mouse CP and found three {alpha}1 genes, two of which are pseudogenes, and a single gene for both {alpha}2 and {alpha}3. Their chromosomal locations were identified by interspecies backcross mapping. The {alpha}1 gene (Cappa1) mapped to Chromosome 3 between D3Mit11 and D3Mit13. The {alpha}1 pseudogenes (Cappa1-ps1 and Cappa1-ps2) mapped to Chromosomes 1 and 9, respectively. The {alpha}2 gene (Cappa2) mapped to Chromosome 6 near Ptn. The {alpha}3 gene (Cappa3) also mapped to Chromosome 6, approximately 68 cM distal from Cappa2 near Kras2. One mouse mutation, de, maps in the vicinity of the {alpha}1 gene. No known mouse mutations map to regions near the {alpha}2 or {alpha}3 genes. 29 refs., 3 figs., 1 tab.

  17. Coincidence measurement between. cap alpha. -particles and projectile-like fragments in reaction of 82. 7 MeV /sup 16/O on /sup 27/Al

    Energy Technology Data Exchange (ETDEWEB)

    Wen-Qing, Shen; Wen-long, Zhan; Yong-tai, Zhu; Shu-zhi, Yin; Zhong-yan, Guo; Wei-min, Qiao; Guo-ying, Fan; Gen-ming, Jin; Song-ling, Li; Zhen, Zhang; others, and

    1987-01-01

    In the coincidence measurement between ..cap alpha..-particles and projectile-like fragments in the reaction of 82.7 MeV /sup 16/O on /sup 27/Al, the contour plot of the C-..cap alpha.. coincidence in the velocity plane and the coincident angular correlation are obtained. Different mechanisms of ..cap alpha..-particle emission are analysed. A possible reaction mechanism of incomplete DIC is discussed.

  18. Effects of thyroid status on presynaptic. cap alpha. 2-adrenoceptor and. beta. -adrenoceptor binding in the rat brain

    Energy Technology Data Exchange (ETDEWEB)

    Atterwill, C.K.; Bunn, S.J.; Atkinson, D.J. (Development Neurobiology Unit, London (UK). Inst. of Neurology); Smith, S.L.; Heal, D.J. (Radcliffe Infirmary, Oxford (UK))

    1984-01-01

    The effect of thyroid status on noradrenergic synaptic function in the mature brain was examined by measuring presynaptic ..cap alpha..2- and postsynaptic ..beta..-adrenoceptors. Repeated triiodothyronine (T/sub 3/) administration to rats (100..mu..g/kg x 14 days hyperthyroid) caused an 18% increase in striatal ..beta..-adrenoceptors as shown by (/sup 3/H)-dihydroalprenolol binding with no change in membranes from cerebral cortex or hypothalamus. In contrast, hypothyroidism (propylthiouracil, PTU x 14 days) produced significant 12% and 30% reductions in striatal and hypothalamic ..beta..-adrenoceptors respectively with no change in the cerebral cortex. Presynaptic ..cap alpha..2-adrenoceptor function was measured in the two dysthyroid states using the clonidine-induced hypoactivity model. Experimental hyperthyroidism increased the degree of clonidine-induced hypoactivity, and suggests increased presynaptic ..cap alpha..2-adrenoceptor function compared with control rats, whereas hypothyroidism suppressed presynaptic ..cap alpha..2-adrenoceptor function. These results show firstly that changes of thyroid status in the mature rat may produce homeostatic alterations at central noradrenergic synapses as reflected by changes in pre- and postsynaptic adrenoceptor function. Secondly, there appear to be T/sub 3/-induced changes in ..beta..-adrenoceptors in the striatum where changes in dopaminergic neuronal activity have previously been demonstrated.

  19. Quasi-exclusive measurement of /sup 12/C(/sup 12/C, 3. cap alpha. )X at 2. 1 GeV/nucleon

    Energy Technology Data Exchange (ETDEWEB)

    Engelage, J; Baumgartner, M; Greiner, D E; Lindstrom, P J; Olson, D L; Wada, R; Crawford, H J; Webb, M L

    1986-05-29

    A study of the reaction /sup 12/C(/sup 12/C,3..cap alpha..)X at 2.1 GeV/nucleon has been completed. The energy and momentum transferred to the /sup 12/C projectile and the cross section for the dissociation of /sup 12/C into three alpha particles have been measured, 9.7 (+5.0/-2.5) millibarns. It is found that the results from this analysis are inconsistent with the predictions of current theoretical models for peripheral relativistic heavy ion collisions.

  20. Szilard-Chalmers effect in natural. cap alpha. disintegrations

    Energy Technology Data Exchange (ETDEWEB)

    Haissinsky, M; Cottin, M

    1948-11-01

    The Szilard-Chalmers effect resulting from the reaction UI(/sup 238/U) ..-->.. UX1(/sup 234/Th) was investigated. The authors developed a chemical method adapted from a technique of Starke (Naturwissenschaften 30, 577(1942)) to separate UX1 which was formed by ..cap alpha.. emission. The experimental accuracy is insufficient to indicate the influence of the degree of dilution of the chemical solutions used on the efficiency of separation, but it is shown that there is a marked decrease in efficiency when solid compounds are used, which is consistent with a hypothesis of Franck and Rabinowitsch (Trans. Faraday Soc. 30, 120(1934)).

  1. cap alpha. -spectra hyperfine structure resolution by silicon planar detectors

    Energy Technology Data Exchange (ETDEWEB)

    Eremin, V K; Verbitskaya, E M; Strokan, N B; Sukhanov, V L; Malyarenko, A M

    1986-10-01

    The lines with 13 keV step from the main one is ..cap alpha..-spectra of nuclei with an odd number of nucleons take place. Silicon planar detectors n-Si with the operation surface of 10 mm/sup 2/ are developed for resolution of this hyperfine structure. The mechanism of losses in detectors for short-range-path particles is analyzed. The results of measurements from detectors with 10 keV resolution are presented.

  2. Thermodynamics of hydrogen and deuterium solutions in. cap alpha. -zirconium

    Energy Technology Data Exchange (ETDEWEB)

    Vinokurov, Yu V; Mogutnov, B M [Tsentral' nyj Nauchno-Issledovatel' skij Inst. Chernoj Metallurgii, Moscow (USSR)

    1979-09-01

    Interaction of H/sub 2/ and D/sub 2/ with ..cap alpha..-Zr are studied in the 700-890 K temperature range using a high-temperature colorimeter. It is shown that hydrogen and deuterium partial enthalpies in zirconium do not depend on the temperature and concentration and compose -48.9+-1.0 and -46.2+-1.2 kJ/g-at. Calculated is an excess entropy of hydrogen in a solution and analyzed are contributions composing it.

  3. Fine structure of the magnetic spectrum of. cap alpha. -rays of ionium

    Energy Technology Data Exchange (ETDEWEB)

    Rosenblum, S; Valadares, M; Vial, J

    1948-11-22

    Using as source of Io--Th an electrolytic deposit on Pt made in 1945 (27% Io), the authors studied the magnetic spectrum of the ..cap alpha..-radiation of Io from long-exposure photographs (4 to 21 days) submitted to a microscopic counting. From a simultaneously obtained ..cap alpha..-spectrum of ThC a ratio was obtained which permitted the assigning of a value of 4682 +- 10 keV to the energy of the most rapid group of Io. This group is separated from another, of a similar order of intensity, by 69 keV. A still slower group seems to exist at 170 keV from the first one (cf Ward, Proc Cambridge Phil Soc 35 322(1939)). There are indications that the groups are of a complex nature, which points to the possible existence either of a soft gamma spectrum or of a complicated beta spectrum. The presence of Ra accumulated since 1945 is visible on the spectra obtained; in a few years it will be possible to determine directly, by the method used, the half life of Ra.

  4. An antiaging skin care system containing alpha hydroxy acids and vitamins improves the biomechanical parameters of facial skin

    Directory of Open Access Journals (Sweden)

    Tran D

    2014-12-01

    Full Text Available Diana Tran, Joshua P Townley, Tanya M Barnes, Kerryn A Greive Ego Pharmaceuticals, Braeside, Victoria, Australia Background: The demand for antiaging products has dramatically increased in recent years, driven by an aging population seeking to maintain the appearance of youth. This study investigates the effects of an antiaging skin care system containing alpha hydroxy acids (AHAs in conjunction with vitamins B3, C, and E on the biomechanical parameters of facial skin. Methods: Fifty two volunteers followed an antiaging skin care regimen comprising of cleanser, eye cream, day moisturizer, and night moisturizer for 21 days. Wrinkle depth (Ry and skin roughness (Ra were measured by skin surface profilometry of the crow's feet area, and skin elasticity parameters R2 (gross elasticity, R5 (net elasticity, R6 (viscoelastic portion, and R7 (recovery after deformation were determined for facial skin by cutometer, preapplication and after 7, 14, and 21 days. Volunteers also completed a self-assessment questionnaire. Results: Compared to baseline, Ry and Ra significantly improved by 32.5% (P<0.0001 and 42.9% (P<0.0001, respectively, after 21 days of antiaging skin care treatment. These results were observed by the volunteers with 9 out of 10 discerning an improvement in skin texture and smoothness. Compared to baseline, R2 and R5 significantly increased by 15.2% (P<0.0001 and 12.5% (P=0.0449, respectively, while R6 significantly decreased by 17.7% (P<0.0001 after 21 days. R7 increased by 9.7% after 21 days compared to baseline but this was not significant over this time period. Conclusion: An antiaging skin care system containing AHAs and vitamins significantly improves the biomechanical parameters of the skin including wrinkles and skin texture, as well as elasticity without significant adverse effects. Keywords: alpha hydroxy acids, antiaging, nicotinamide, vitamin C, vitamin E, profilometry, cutometer

  5. Nickel doping effect on resistance to movement of edge dislocations in. cap alpha. -Fe

    Energy Technology Data Exchange (ETDEWEB)

    Brovkov, V.A.; Dudarev, E.F. (Tomskij Gosudarstvennyj Univ. (USSR). Sibirskij Fiziko-Tekhnicheskij Inst.)

    1984-03-01

    Microplastic deformation of ..cap alpha..-Fe polycrystals and Fe-Ni solid solutions is studied. Data on the concentration and temperature dependences of resistance to movement of edge dislocation at the expense of elastic interaction with atoms of the doping element are obtained.

  6. A study on the determination of Ca/P molar ratio in calcium-hydroxyapatite by alpha excited x-ray fluorescence spectrometry

    International Nuclear Information System (INIS)

    Mizumoto, Yoshihiko; Iwata, Shiro.

    1979-01-01

    Nondestructive powdery calcium-hydroxyapatite (HAp) target was prepared by electrodeposition method. The powdery HAp was deposited on the copper electrode plate of cathode in the electrodeposition solution such as ethyl alcohol, methyl alcohol, etc. The experiments were carried out as functions of different electrodeposition solution, ethyl alcohol concentration, distance between anode and cathode, electrodeposition time and HAp amount added in bath, and distribution of HAp on the copper electrode plate obtained from each experiment was investigated by alpha excited X-ray fluorescence analysis. Ca/P molar ratio of thin HAp target prepared with this method was determined by alpha excited X-ray fluorescence spectrometry. The nondestructive HAp targets of thickness in the range of 5 mu g/cm 2 to 10 mg/cm 2 were easily prepared with comparatively simple apparatus. The HAp on the copper electrode plate was uniform thickness over 15 x 20 mm copper plate within 5%. The Ca/P molar ratio of HAp was 1.64 +- 0.05, which agreed well with stoichiometric value of 1.67 in HAp within standard deviation. (author)

  7. Effects of x-ray irradiation on the induction of. cap alpha. -amylase synthesis by gibberelic acid in the aleurone system of barley

    Energy Technology Data Exchange (ETDEWEB)

    Zellner, H

    1974-01-01

    The influence of ionizing radiation on a system without DNA replication and cell division was investigated with the aid of GA/sub 3/-induced ..cap alpha..-amylase synthesis in aleurone cells of barley. The reaction of the system was determined by dose effect curves (after irradiation of one half of the endosperms in rest) for the synthesis and secretion of ..cap alpha..-amylase, protein, and reducing sugars. The system proves to be highly radiation-resistant. The course of the synthesis of ..cap alpha..-amylase after X-ray irradiation with varying doses during enzyme synthesis suggests that transcription occurs in the middle of the lag-phase and is the most sensitive stage in enzyme synthesis, while translation alone is less sensitive to radiation.

  8. Antiulcerogenic activity of fractions and 3,15-dioxo-21alpha-hydroxy friedelane isolated from Maytenus robusta (Celastraceae).

    Science.gov (United States)

    de Andrade, Sérgio Faloni; Comunello, Eros; Noldin, Vânia Floriani; Monache, Franco Delle; Cechinel Filho, Valdir; Niero, Rivaldo

    2008-01-01

    The hexane, chloroform, ethyl acetate and aqueous-soluble fractions from leaves of Maytenus robusta (Celastraceae) were evaluated for their protective actions against ethanol-induced gastric lesions in rats. The treatment with all fractions (150 mg/kg) and omeprazol (30 mg/kg) significantly reduced the lesion index, the total lesion area, and the percentage of lesion, in comparison with the control group (p<0.05). Since the ethyl acetate-soluble fraction was found to be most active in the pylorus ligated model, this fraction was further investigated and resulted in the isolation of triterpene 3,15-dioxo-21alpha-hydroxy friedelane. The triterpene was evaluated in the HCl/ethanol-induced ulcer model in mice. In this assay, both the groups treated with 3,15-dioxo-21alpha-hydroxy friedelane and omeprazol, at a dose of 30 mg/kg, presented a significant reduction in lesion index, total lesion area, and in the percentage of the lesion, when compared with the control group (p<0.05). The result suggests that the antiulcer effect observed in the extract and fractions may be attributed, at least in part, to this compound. Further experiments are underway to determine which antiulcer mechanisms involved in gastroprotection.

  9. Synthesis of tritiated 1-alpha-methadol and 1-alpha-acetylmethadol

    Energy Technology Data Exchange (ETDEWEB)

    Thang, D.C.; Nam, N.H.; Pontikis, R. (Institut National de la Sante et de la Recherche Medicale (INSERM), Hopital Fernand Widal, 75 - Paris (France)); Pichat, L. (CEA Centre d' Etudes Nucleaires de Saclay, 91 - Gif-sur-Yvette (France). Service des Molecules Marquees)

    1982-04-01

    dl-Methadone was resolved by crystallization of its ammonium d- ..cap alpha.. -bromocamphor-..pi..-sulfonate salt to give d-methadone. The latter in ethyl acetate solution was reduced with tritium gas to 1-..cap alpha..-methadol /sup 3/H in presence of Adams platinum oxide at normal temperature and pressure. Acetylation of 1-..cap alpha..-carbinol hydrochloride by means of acetyl chloride afforded 1-..cap alpha..-acetylmethadol /sup 3/H, specific activity: 20 Ci/mMole. The positions and extent of tritium labelling were determined by /sup 3/H NMR spectroscopy.

  10. Structure-function relationships in the Na,K-ATPase. cap alpha. subunit: site-directed mutagenesis of glutamine-111 to arginine and asparagine-122 to aspartic acid generates a ouabain-resistant enzyme

    Energy Technology Data Exchange (ETDEWEB)

    Price, E.M.; Lingrel, J.B.

    1988-11-01

    Na,K-ATPases from various species differ greatly in their sensitivity to cardiac glycosides such as ouabain. The sheep and human enzymes are a thousand times more sensitive than the corresponding ones from rat and mouse. To define the region of the ..cap alpha..1 subunit responsible for this differential sensitivity, chimeric cDNAs of sheep and rat were constructed and expressed in ouabain-sensitive HeLa cells. The construct containing the amino-terminal half of the rat ..cap alpha..1 subunit coding region and carboxyl-terminal half of the sheep conferred the ouabain-resistant phenotype to HeLa cells while the reverse construct did not. This indicates that the determinants involved in ouabain sensitivity are located in the amino-terminal half of the Na,K-ATPase ..cap alpha.. subunit. By use of site-directed mutagenesis, the amino acid sequence of the first extracellular domain (H1-H2) of the sheep ..cap alpha..1 subunit was changed to that of the rat. When expressed in HeLa cells, this mutated sheep ..cap alpha..1 construct, like the rat/sheep chimera, was able to confer ouabain resistance to these cells. Furthermore, similar results were observed when HeLa cells were transfected with a sheep ..cap alpha..1 cDNA containing only two amino acid substitutions. The resistant cells, whether transfected with the rat ..cap alpha..1 cDNA, the rat/sheep chimera, or the mutant sheep ..cap alpha..1 cDNAs, exhibited identical biochemical characteristics including ouabain-inhibitable cell growth, /sup 86/Rb/sup +/ uptake, and Na,K-ATPase activity. These results demonstrate that the presence of arginine and aspartic acid on the amino end and carboxyl end, respectively, of the H1-H2 extracellular domain of the Na,K-ATPase ..cap alpha.. subunit together is responsible for the ouabain-resistant character of the rat enzyme and the corresponding residues in the sheep ..cap alpha..1 subunit (glutamine and asparagine) are somehow involved in ouabain binding.

  11. 2-Hydroxy-5-nitrobenzaldehyde

    Directory of Open Access Journals (Sweden)

    Şamil Işık

    2009-12-01

    Full Text Available The title compound, C7H5NO4, is essentially planar, with a maximum deviation from the mean plane of 0.0116 (11 Å for the hydroxy O atom. The molecular and crystal structure are stabilized by intra- and intermolecular interactions. An intramolecular O—H...O hydrogen bond generates a six-membered ring, producing an S(6 ring motif. The C—H...O interactions result in the formation of C(5 chains and R22(8 rings forming an approximately planar network parallel to (10overline{1}. These planes are interconnected through π–π interactions [centroid–centroid distance 3.582 (2 Å].

  12. Primary structure of the. cap alpha. -subunit of Na/sup +/, K/sup +/-ATPase. II. Isolation, reverse transcription, and cloning of messenger RNA

    Energy Technology Data Exchange (ETDEWEB)

    Petrukhin, K.E.; Broude, N.E.; Arsenyan, S.G.; Grishin, A.V.; Dzhandzhugazyan, K.N.; Modyanov, N.N.

    1986-10-01

    The messenger RNA coding the ..cap alpha..-subunit of Na/sup +/,K/sup +/-ATPase has been isolated from the outer medullary layer of porcine kidneys. The mRNA gives a specific hybridization band in the 25S-26S region with three oligonucleotide probes synthesized on the basis of information on the structure of three peptides isolated from a tryptic hydrolyzate of the ..cap alpha..-subunit of Na/sup +/,K/sup +/-ATPase. The translation of the mRNA in Xenopus laevis oocytes followed by immunochemical identification of the products of synthesis confirmed the presence of the mRNA of the ..cap alpha..-subunit of Na/sup +/,K/sup +/-ATPase in an enriched fraction of poly(A/sup +/)-RNA. This preparation has been used for the synthesis of cloning of double-stranded cDNA.

  13. Lifetime of the long-lived isomer of /sup 236/Np from. cap alpha. -,. beta. - and electron-capture decay measurements

    Energy Technology Data Exchange (ETDEWEB)

    Lindner, M.; Dupzyk, R.J.; Hoff, R.W.; Nagle, R.J. (California Univ., Livermore (USA). Lawrence Livermore National Lab.)

    1981-01-01

    The half-life of long-lived /sup 236/Np, due to ..cap alpha.., ..beta.. and electron-capture decay, was found to be 1.55 x 10/sup 5/ yr. Of all decays, 88% populate excited states in /sup 236/U and 12% populate levels in /sup 236/Pu. Lifetimes measured by growth of the ground states of /sup 236/U and /sup 236/Pu agree with values from corresponding ..gamma.. de-excitations in these daughter nuclei. Therefore, nearly all the electron-capture decays populate the 6/sup +/ level of the ground-state band in /sup 236/U. Similarly, essentially all the ..beta../sup -/ decay populates an analogous 6/sup +/ level in /sup 236/Pu, which de-excites through a previously unreported transition of 158.3 keV. If a very week ..gamma..-ray at 894 keV can be ascribed to a level in /sup 232/U populated by ..beta.. decay of /sup 232/Pa, its existence establishes a 0.2% ..cap alpha..-branching decay in /sup 236/Np.

  14. 3-Hydroxy-2-[(4-hydroxy-3,5-dimethoxyphenyl(2-hydroxy-4,4-dimethyl-6-oxocyclohex-1-en-1-ylmethyl]-5,5-dimethylcyclohex-2-en-1-one

    Directory of Open Access Journals (Sweden)

    Xiao-Hui Yang

    2011-02-01

    Full Text Available In the title compound, C25H32O7, the 3-hydroxy-5,5-dimethylcyclohex-2-enone rings adopt slightly distorted envelope conformations with the two planes at the base of the envelope forming dihedral angles of 57.6 (4 and 53.9 (9° with the benzene ring. There is an intramolecular hydroxy–ketone O—H...O interaction between the two substituted cyclohexane rings as well as a short intramolecular phenol–methoxy O—H...O interaction.

  15. Mid-aged and aged wild-type and progestin receptor knockout (PRKO) mice demonstrate rapid progesterone and 3alpha,5alpha-THP-facilitated lordosis.

    Science.gov (United States)

    Frye, C A; Sumida, K; Lydon, J P; O'Malley, B W; Pfaff, D W

    2006-05-01

    Progesterone (P) and its 5alpha-reduced metabolite, 3alpha-hydroxy-5alpha-pregnan-20-one (3alpha,5alpha-THP), facilitate sexual behavior of rodents via agonist-like actions at intracellular progestin receptors (PRs) and membrane GABA(A)/benzodiazepine receptor complexes (GBRs), respectively. Given that ovarian secretion of progestins declines with aging, whether or not senescent mice are responsive to progestins was of interest. Homozygous PR knockout (PRKO) or wild-type mice that were between 10-12 (mid-aged) or 20-24 (aged) months of age were administered P or 3alpha,5alpha-THP, and the effect on lordosis were examined. Effects of a progestin-priming regimen that enhances PR-mediated (experiment 1) or more rapid, PR-independent effects of progestins (experiments 2 and 3) on sexual behavior were examined. Levels of P, 3alpha,5alpha-THP, and muscimol binding were examined in tissues from aged mice (experiment 4). Wild-type, but not PRKO, mice were responsive when primed with 17beta-estradiol (E(2); 0.5 microg) and administered P (500 microg, subcutaneously). Mid-aged wild-type mice demonstrated greater increases in lordosis 6 h later compared to their pre-P, baseline test than did aged wild-type mice (experiment 1). Lordosis of younger and older wild-type, but not PRKO, mice was significantly increased within 5 min of intravenous (IV) administration of P (100 ng), compared with E(2)-priming alone (experiment 2). However, wild-type and PRKO mice demonstrated significant increases in lordosis 5 min after IV administration of 3alpha,5alpha-THP, an effect which was more pronounced in mid-aged than in aged animals (100 ng-experiment 3). In tissues from aged wild-type and PRKO mice, levels of P, 3alpha,5alpha-THP, and muscimol binding were increased by P administration (experiment 4). PR binding was lower in the cortex of PRKO than that of wild-type mice. Mid-aged and aged PRKO and wild-type mice demonstrated rapid P or 3alpha,5alpha-THP-facilitated lordosis that may be

  16. Human placental Na/sup +/, K/sup +/-ATPase. cap alpha. subunit: cDNA cloning, tissue expression, DNA polymorphism, and chromosomal localization

    Energy Technology Data Exchange (ETDEWEB)

    Chehab, F.F.; Kan, Y.W.; Law, M.L.; Hartz, J.; Kao, F.T.; Blostein, R.

    1987-11-01

    A 2.2-kilobase clone comprising a major portion of the coding sequence of the Na/sup +/, K/sup +/-ATPase ..cap alpha.. subunit was cloned from human placenta and its sequence was identical to that encoding the ..cap alpha.. subunit of human kidney and HeLa cells. Transfer blot analysis of the mRNA products of the Na/sup +/, K/sup +/-ATPase gene from various human tissues and cell lines revealed only one band (approx. = 4.7 kilobases) under low and high stringency washing conditions. The levels of expression in the tissues were intestine > placenta > liver > pancreas, and in the cell lines the levels were human erythroleukemia > butyrate-induced colon > colon > brain > HeLa cells. mRNA was undetectable in reticulocytes, consistent with the authors failure to detect positive clones in a size-selected ( > 2 kilobases) lambdagt11 reticulocyte cDNA library. DNA analysis revealed by a polymorphic EcoRI band and chromosome localization by flow sorting and in situ hybridization showed that the ..cap alpha.. subunit is on the short is on the short arm (band p11-p13) of chromosome 1.

  17. Comparative study of G2 delay and survival after /sup 241/Americium-. cap alpha. and /sup 60/Cobalt-. gamma. irradiation

    Energy Technology Data Exchange (ETDEWEB)

    Luecke-Huhle, C.; Comper, W.; Hieber, L.; Pech, M.

    1982-06-01

    Survival and G2 delay following exposure to either /sup 60/Cobalt-..gamma..-rays or /sup 241/Americium-..cap alpha..-particles were studied in eight mammalian cell lines of human and animal origin including human fibroblasts from normal individuals and from patients with Ataxia telangiectasia or Fanconi's anemia. For both endpoints the effectiveness of alpha particle was greater as compared to ..gamma..-rays. RBE values for G2 delay (4.6-9.2) were in general comparable to RBE values derived from initial slopes of survival curves but higher compared to the ratio of mean inactivation doses. Ataxia cells were particularly sensitive to cell killing by ..gamma..-irradiation, however, showed average sensitivity to ..cap alpha..-particles of high LET. With the exception of Ataxia cells, cell killing and G2 delay seem to be related processes if individual cell cycle parameters are taken into account.

  18. (-)-6 alpha hydroxy polyanthellian A - A novel antifouling diterpenoid from the Indian soft coral Cladiella krempfi (Hickson)

    Digital Repository Service at National Institute of Oceanography (India)

    LimnaMol, V.P.; Raveendran, T.V.; Parameswaran, P.S.; Kunnath, R.J.; Rajamohanan, P.R.

    shifts of (-)-6α-hydroxy polyanthellin A and polyanthellin A C- No (-)-6α-hydroxy polyanthellin A Polyanthellin A δ c δ h δ c δ h 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 41... 3 4 5 6 7 8 9 1011 12 13 14 15 16 17 18 19 20 H H O CH 3 CH 3 Fig.3. (-)-6α-hydroxy polyanthellin A A 0 20 40 60 80 100 Control 6.25 12.5 25 50 100 Concentration (μg/ml) % A c t i v i t y B 0 20 40 60 80 100 Control 6.25 12.5 25 50 100...

  19. Radiation-induced changes in production of prostaglandins Fsub(2. cap alpha. ), E, and thromboxane B/sub 2/ in guinea pig parenchymal lung tissues

    Energy Technology Data Exchange (ETDEWEB)

    Steel, L K; Catravas, G N [Armed Forces Radiobiology Research Inst., Bethesda, MD (USA)

    1982-11-01

    At 1 hour to 4 days after unilateral exposure of guinea pigs to a single dose (0.5, 1.5, or 3.0 Gy) of gamma-radiation, changes were detected in prostaglandin and thromboxane concentrations in parenchymal lung tissues. At 1-3 hours after exposure, tissue levels of PGFsub(2..cap alpha..), PGE, and thromboxane B/sub 2/ were significantly elevated in animals receiving 3.0 Gy, with the magnitude of alteration revealing a radiation dose effect. By 24 hours, tissue prostaglandin and thromboxane levels returned to near control values. Lung tissue synthesis of prostaglandins in response to H-1 receptor stimulation by the exogenous addition of histamine revealed similar radiation dose effects. The carboxylic acid ionophore A23187, exogenously applied to lung tissues, revealed a transient peak of increased sensitivity to ionophore stimulation for TxB/sub 2/ synthesis at 24 hours and for PGFsub(2..cap alpha..) at 72 hours post-irradiation. The data suggest that significant alterations in prostaglandin and thromboxane concentrations in parenchymal lung tissues occur following irradiation, in a dose-dependent manner, and that altered responsiveness to H-1 receptor stimulation and divalent cation transport also occur.

  20. Drastic nickel ion removal from aqueous solution by curcumin-capped Ag nanoparticles

    Science.gov (United States)

    Bettini, S.; Pagano, R.; Valli, L.; Giancane, G.

    2014-08-01

    A completely green synthesis protocol has been adopted to obtain silver nanoaggregates capped by the natural compound (1E, 6E)-1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-diene), also known as curcumin. The synthesis has been monitored by infrared, Raman, visible and fluorescence spectroscopies. Characterization confirms that curcumin reduces and caps the nanoparticles, and such a procedure allows its solubility in water and drastically increases curcumin stability. Silver nanoparticles (AgNPs)/curcumin complex has been dispersed in a water solution containing a known nickel ion concentration. After three days, a grey precipitate is observed and nickel concentration in the solution is reduced by about 70%.A completely green synthesis protocol has been adopted to obtain silver nanoaggregates capped by the natural compound (1E, 6E)-1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-diene), also known as curcumin. The synthesis has been monitored by infrared, Raman, visible and fluorescence spectroscopies. Characterization confirms that curcumin reduces and caps the nanoparticles, and such a procedure allows its solubility in water and drastically increases curcumin stability. Silver nanoparticles (AgNPs)/curcumin complex has been dispersed in a water solution containing a known nickel ion concentration. After three days, a grey precipitate is observed and nickel concentration in the solution is reduced by about 70%. Electronic supplementary information (ESI) available. See DOI: 10.1039/c4nr02583k

  1. Method for conversion of .beta.-hydroxy carbonyl compounds

    Science.gov (United States)

    Lilga, Michael A.; White, James F.; Holladay, Johnathan E.; Zacher, Alan H.; Muzatko, Danielle S.; Orth, Rick J.

    2010-03-30

    A process is disclosed for conversion of salts of .beta.-hydroxy carbonyl compounds forming useful conversion products including, e.g., .alpha.,.beta.-unsaturated carbonyl compounds and/or salts of .alpha.,.beta.-unsaturated carbonyl compounds. Conversion products find use, e.g., as feedstock and/or end-use chemicals.

  2. Synthesis of 20-14C 3β-hydroxy-5β-pregnan-20-one

    International Nuclear Information System (INIS)

    Garraffo, H.M.; Gros, E.G.

    1982-01-01

    20 - 14 C 3β-hydroxy-5β-pregnan-20-one was synthesised by condensing 3β-acetoxy-5β-androstan-17-one with potassium 14 C cyanide to produce cyanohydrin. This was dehydrated and the resulting unsaturated nitrile treated with methylmagnesiumiodide to produce hydroxypregnenone. Hydrogenation of this gave 14 C 3β-hydroxy-5β-pregnan-20-one. (U.K.)

  3. 5alphaDH-DOC (5alpha-dihydro-deoxycorticosterone) activates androgen receptor in castration-resistant prostate cancer.

    Science.gov (United States)

    Uemura, Motohide; Honma, Seijiro; Chung, Suyoun; Takata, Ryo; Furihata, Mutsuo; Nishimura, Kazuo; Nonomura, Norio; Nasu, Yasutomo; Miki, Tsuneharu; Shuin, Taro; Fujioka, Tomoaki; Okuyama, Akihiko; Nakamura, Yusuke; Nakagawa, Hidewaki

    2010-08-01

    Prostate cancer often relapses during androgen-depletion therapy, even under the castration condition in which circulating androgens are drastically reduced. High expressions of androgen receptor (AR) and genes involved in androgen metabolism indicate a continued role for AR in castration-resistant prostate cancers (CRPCs). There is increasing evidence that some amounts of 5alpha-dihydrotestosterone (DHT) and other androgens are present sufficiently to activate AR within CRPC tissues, and enzymes involved in the androgen and steroid metabolism, such as 5alpha-steroid reductases, are activated in CRPCs. In this report, we screened eight natural 5alphaDH-steroids to search for novel products of 5alpha-steroid reductases, and identified 11-deoxycorticosterone (DOC) as a novel substrate for 5alpha-steroid reductases in CRPCs. 11-Deoxycorticosterone (DOC) and 5alpha-dihydro-deoxycorticosterone (5alphaDH-DOC) could promote prostate cancer cell proliferation through AR activation, and type 1 5alpha-steroid reductase (SRD5A1) could convert from DOC to 5alphaDH-DOC. Sensitive liquid chromatography-tandem mass spectrometric analysis detected 5alphaDH-DOC in some clinical CRPC tissues. These findings implicated that under an extremely low level of DHT, 5alphaDH-DOC and other products of 5alpha-steroid reductases within CRPC tissues might activate the AR pathway for prostate cancer cell proliferation and survival under castration.

  4. Sleep-inducing N-alkyl-5-[m-(trifluoromethyl)phenyl]-5-hydroxy-2-pyrrolidinones and N-alkyl-3-(trifluoromethyl)cinnamamides.

    Science.gov (United States)

    Houlihan, W J; Gogerty, J H; Ryan, E A; Schmitt, G

    1985-01-01

    A series of N-alkyl-3-[m-(trifluoromethyl)phenyl]-5-hydroxy-2-pyrrolidinones and N-alkyl-3-(trifluoromethyl)-cinnamamides were prepared and screened in a series of tests designed to detect potential sleep inducers. The more active members of the series were evaluated for their ability to induce sleep in Cebus monkeys. The most active compound, N-methyl-5-[m-(trifluoromethyl)phenyl]-5-hydroxy-2-pyrrolidinone, was equal to methaqualone.

  5. Electrochemical determination of 5-dodecylsalicylaldoxime and 2′-hydroxy-5′-nonylacetophenone oxime in commercial extractants

    Directory of Open Access Journals (Sweden)

    Elizalde María P.

    2017-01-01

    Full Text Available A differential pulse voltammetric method using a hanging mercury drop electrode (HMDE was optimized for the determination of 5-dodecylsalicylaldoxime in hydro-alcoholic solutions using factorial and central composite designs. The Taguchi design methodology was used to extend the formerly optimized method to the determination of 2′-hydroxy-5′-nonylacetophenone oxime. The method was successfully applied to quantify 5-dodecylsalicylaldoxime and 2′-hydroxy-5′-nonylacetophenone oxime in samples of commercial extractants over the concentration range 0.05–2.45 and 0.07–0.82 mg L-1, respectively, with detection limits of 0.034 and 0.019 mg L-1, respectively.

  6. 5-Hydroxytryptamine 1A/7 and 4alpha receptors differentially prevent opioid-induced inhibition of brain stem cardiorespiratory function.

    Science.gov (United States)

    Wang, Xin; Dergacheva, Olga; Kamendi, Harriet; Gorini, Christopher; Mendelowitz, David

    2007-08-01

    Opioids evoke respiratory depression, bradycardia, and reduced respiratory sinus arrhythmia, whereas serotonin (5-HT) agonists stimulate respiration and cardiorespiratory interactions. This study tested whether serotonin agonists can prevent the inhibitory effects of opioids on cardiorespiratory function. Spontaneous and rhythmic inspiratory-related activity and gamma-aminobutyric acid (GABA) neurotransmission to premotor parasympathetic cardioinhibitory neurons in the nucleus ambiguus were recorded simultaneously in an in vitro thick slice preparation. The mu-opioid agonist fentanyl inhibited respiratory frequency. The 5-hydroxytryptamine 1A/7 receptor agonist 8-hydroxy-2-(di-n-propylamino)tetralin increased respiratory frequency by itself and also prevented the fentanyl-induced respiratory depression. The 5-hydroxytryptamine 4alpha agonist BIMU-8 did not by itself change inspiratory activity but prevented the mu-opioid-mediated respiratory depression. Both spontaneous and inspiratory-evoked GABAergic neurotransmission to cardiac vagal neurons were inhibited by fentanyl. 8-Hydroxy-2-(di-n-propylamino)tetralin inhibited spontaneous but not inspiratory-evoked GABAergic activity to parasympathetic cardiac neurons. However, 8-hydroxy-2-(di-n-propylamino)tetralin differentially altered the opioid-mediated depression of inspiratory-evoked GABAergic activity but did not change the opioid-induced reduction in spontaneous GABAergic neurotransmission. In contrast, BIMU-8 did not alter GABAergic neurotransmission to cardiac vagal neurons by itself but prevented the fentanyl depression of both spontaneous and inspiratory-elicited GABAergic neurotransmission to cardiac vagal neurons. In the presence of tetrodotoxin, the inhibition of GABAergic inhibitory postsynaptic currents with fentanyl is prevented by coapplication of BIMU-8, indicating that BIMU-8 acts at presynaptic GABAergic terminals to prevent fentanyl-induced depression. These results suggest that activation of 5

  7. The Clinician-Administered PTSD Scale for DSM-5 (CAPS-5): Development and initial psychometric evaluation in military veterans.

    Science.gov (United States)

    Weathers, Frank W; Bovin, Michelle J; Lee, Daniel J; Sloan, Denise M; Schnurr, Paula P; Kaloupek, Danny G; Keane, Terence M; Marx, Brian P

    2018-03-01

    The Clinician-Administered PTSD Scale (CAPS) is an extensively validated and widely used structured diagnostic interview for posttraumatic stress disorder (PTSD). The CAPS was recently revised to correspond with PTSD criteria in the fifth edition of the Diagnostic and Statistical Manual of Mental Disorders (DSM-5; American Psychiatric Association, 2013). This article describes the development of the CAPS for DSM-5 (CAPS-5) and presents the results of an initial psychometric evaluation of CAPS-5 scores in 2 samples of military veterans (Ns = 165 and 207). CAPS-5 diagnosis demonstrated strong interrater reliability (к = .78 to 1.00, depending on the scoring rule) and test-retest reliability (к = .83), as well as strong correspondence with a diagnosis based on the CAPS for DSM-IV (CAPS-IV; к = .84 when optimally calibrated). CAPS-5 total severity score demonstrated high internal consistency (α = .88) and interrater reliability (ICC = .91) and good test-retest reliability (ICC = .78). It also demonstrated good convergent validity with total severity score on the CAPS-IV (r = .83) and PTSD Checklist for DSM-5 (r = .66) and good discriminant validity with measures of anxiety, depression, somatization, functional impairment, psychopathy, and alcohol abuse (rs = .02 to .54). Overall, these results indicate that the CAPS-5 is a psychometrically sound measure of DSM-5 PTSD diagnosis and symptom severity. Importantly, the CAPS-5 strongly corresponds with the CAPS-IV, which suggests that backward compatibility with the CAPS-IV was maintained and that the CAPS-5 provides continuity in evidence-based assessment of PTSD in the transition from DSM-IV to DSM-5 criteria. (PsycINFO Database Record (c) 2018 APA, all rights reserved).

  8. Kinetic tritium isotopic effects in the position 2 for 5'-hydroxy-L-tryptophane

    International Nuclear Information System (INIS)

    Boroda, E.; Kanska, M.

    2006-01-01

    Tryptophanase converts 5'-hydroxy-L-tryptophane to pyrogronic acid and ammonia, however there are known conditions for the reversed reaction. Mechanism of the processes are not known till now. Kinetic isotopic effect (KIE) permits finding the rate determining stage in the multistage process. In presented communication, 5'-hydroxy-[2- 3 H]-L-tryptophane was synthesized and the KIE in the room temperature determined for different reaction stages

  9. Synthesis and evaluation of phytotoxic activity of {alpha}-Santonin derivatives; Sintese e avaliacao da atividade fitotoxica de derivados da {alpha}-Santonina

    Energy Technology Data Exchange (ETDEWEB)

    Alvarenga, Elson S.; Barbosa, Luiz C.A.; Saliba, William A.; Arantes, Francisco F.P.; Demuner, Antonio J. [Universidade Federal de Vicosa (UFV), MG (Brazil). Dept. de Quimica]. E-mail: elson@ufv.br; Silva, Antonio A. [Universidade Federal de Vicosa (UFV), MG (Brazil). Dept. de Fitotecnia

    2009-07-01

    Mixtures of {alpha}-Santonin and various solvents were irradiated by either high or low pressure mercury lamps. The photochemical reactions afforded lumisantonin (11) (76% in acetonitrile), (3 S,3a S,9{beta}S)-3,6,6-trimethyl-3,3a,4,5-tetrahydronafto[1,2-b]furan-2,7({eta}6,9{beta}{eta}) dione (12) (100% in acetonitrile), 10{alpha}-acetoxy-3-oxo-1,7{alpha}H{eta},6,11{alpha}a{eta}-guaia-4-en-6,12-oli= de (8) (26% in acetic acid), 10{alpha}-hydroxy-3-oxo-1,7{alpha}a{eta},6,11{alpha}{eta}-guaia-4-en-6,12-olid= e (10) (32%) and (E)-3-((3 S,3a S,7{alpha}S)-3-methyl-2-oxo-6-(propan-2-ylidene)hexahydrobenzofuran- 7 - (7{alpha}{eta})-ylidene)propanoic acid (9) (44%) (in water/ acetic acid 1:1, v/v). Lactone 12 was also prepared by irradiation of lumisantonin in diethyl ether. Lactones 8 and 10 were converted, respectively, into the 10 {alpha}-acetoxy-3{alpha}-hydroxy-1,7{alpha}H,6,11{alpha}H-guaia-4-en-6,12-olid= e (13) (87%) and 3a,10a-dihydroxy-1,7{alpha}H,6,11{alpha}H-guaia-4-en-6,12-olide (14) (75%) by sodium borohydride reduction. The effects of the compounds on the development of radicle of Sorghum bicolor and Cucumis sativus were evaluated. (author)

  10. Search for aligned structure of /sup 12/C-. cap alpha. -/sup 12/C type at high excitation energy in /sup 28/Si. [46 MeV, J,. pi. , resonance, three-body problem

    Energy Technology Data Exchange (ETDEWEB)

    Burnereau, N

    1975-01-01

    The /sup 16/O+/sup 12/C..-->../sup 12/C+..cap alpha..+/sup 12/C reaction is studied mainly at 46MeV (at this energy a state of /sup 28/Si is presumably formed with a spin value of 14/sup +/; resonance of 19.7MeV c.m.). The motivation is to detect an ..cap alpha.. particle with a negligible energy in the c.m. system. This is the signature of the preformation of three aligned clusters in which the average location of the ..cap alpha.. particle is in between the two /sup 12/C's at the center of symmetry of the system. Such a detection is performed by detecting two /sup 12/C's in coincidence at specific angles. The data are understood by three-body calculations with a coupling of relative angular momenta governed by an unique J value. Experimentally, an ..cap alpha.. energy of 200keV is measured with good statistics, supporting the idea of aligned clusters as /sup 28/Si intrinsic shape, related to some highly excited states.

  11. Study of. cap alpha. -/sup 16/O scattering by orthogonality condition models

    Energy Technology Data Exchange (ETDEWEB)

    Breitschaft, A M; Canto, L F; Schechter, H

    1983-06-01

    The use of approximate microscopic theories in ..cap alpha..-/sup 16/O scattering is investigated. The Orthogonality Condition Model (OCM) with both the direct potential of the Resonating Group Method (RMG) and with an effective local potential, V sub(eff), derived from Kernels of Generator Coordinate Method (GCM) is employed to study collisions at CM energies up to 30 MeV, for all relevant partial waves. Although the predictions of the OCM are consistent with exact RGM results in both cases, the nuclear phase-shifts obtained with the effective potential are better. The presence of ambiguities in the derivation of V sub(eff) is noticed. The nature of such ambiguities is discussed.

  12. Synthesis of 5'-bromo-2'-hydroxy-4,4',6'-trimethoxychalcone from Garcinia nervosa and of its isomer 3'-bromo-2'-hydroxy-4,4',6'- trimethoxychalcone

    Digital Repository Service at National Institute of Oceanography (India)

    Parab, S.J.; Kapdi, S.G.; Naik, C.G.; Kamat, S.P.

    The unambiguous syntheses of the naturally occurring 5'-bromo-2'-hydroxy-4,4',6'-trimethoxychalcone 1, a constituent of Garcinia nervosa, and its positional isomer 3'-bromo-2'-hydroxy-4,4',6'-trimethoxychalcone 6 are described...

  13. Direct fluorination of melatonin and 5-hydroxy-L-tryptophan with [18F]F2

    International Nuclear Information System (INIS)

    Chirakal, R.; Firnau, G.; Garnett, E.S.

    1986-01-01

    In order that melatonin receptors may be studied in man with positron emission tomography, melatonin labelled with a positron emitting isotope is needed. The preparation of 6-fluoro-melatonin labelled with F-18 is described. Using the same fluorination method, 5-hydroxy-6-(F-18)fluorotryptophan and 4-(F-18)fluoro-5-hydroxy-tryptophan were also prepared. (UK)

  14. Novel alpha-hydroxy phosphonic acids via castor oil

    Science.gov (United States)

    Hydroxy fatty acids (HFAs) have found a number of uses in today’s market, with uses ranging from materials to pharmaceuticals. Castor oil has served as a versatile HFA; its principle component, ricinoleic acid, can be isolated from castor oil and has been modified extensively for a number of applica...

  15. Secondary. cap alpha. -deuterium kinetic isotope effects in solvolyses of ferrocenylmethyl acetate and benzoate in ethanol

    Energy Technology Data Exchange (ETDEWEB)

    Sutic, D. (Univ. of Zagreb, Yugoslavia); Asperger, S.; Borcic, S.

    1982-12-17

    Secondary ..cap alpha..-deuterium kinetic isotope effects (KIE) in solvolyses of ferrocenyldideuteriomethyl acetate and benzoate were determined in 96% (v/v) ethanol, at 25/sup 0/C, as k/sub H//k/sub D/ = 1.24 and 1.26, respectively. The KIEs were also determined in the presence of 0.1 mol dm/sup -3/ lithium perchlorate: the k/sub H//k/ sub D/ values were 1.23 and 1.22 for acetate and benzoate complexes, respectively. The maximum KIE for the C-O bond cleavage of a primary substrate is as large as, or larger than, that of secondary derivatives, which is estimated to be 1.23 per deuterium. The measured KIE of about 12% per D therefore represents a strongly reduced effect relative to its maximum. The solvolyses exhibit ''a special salt effect''. This effect indicates the presence of solvent-separated ion pairs and the return to tight pairs. As the maximum KIE is expected in solvolyses involving transformation of one type of ion pair into another, the strongly reduced ..cap alpha..-D KIE supports the structure involving direct participation of electrons that in the ground state are localized at the iron atom. The alkyl-oxygen cleavage is accompanied by 10-15% acyl-oxygen cleavage.

  16. Alpha-heavy-ion angular correlations from /sup 28/Si + /sup 12/C. [84 to 91. 5 MeV

    Energy Technology Data Exchange (ETDEWEB)

    Ost, R; Cole, A J [Institut des Sciences Nucleaires, 38 - Grenoble (France); Clover, M R; Fulton, B R; Sikora, B [Rochester Univ., NY (USA). Nuclear Structure Research Lab.

    1980-06-01

    Alpha particles have been measured in coincidence with heavy recoil nuclei from the /sup 28/Si + /sup 12/C reaction. At Esub(lab) = 87 MeV angular correlations for alphas between 15/sup 0/ and 55/sup 0/ and heavy ions at angles -9/sup 0/, -12/sup 0/ and -15/sup 0/ have been taken. An excitation function of coincidence events with THETAsub(..cap alpha..) = 30/sup 0/ and THETAsub(HI) = -12/sup 0/ has been measured for 84 MeV < Esub(lab) < 91.5 MeV. The results are well described by a statistical-model calculation for compound nucleus decay. No evidence is found for additional processes.

  17. Release of /sup 3/H-. cap alpha. -methyl-m-tyramine from rat striatum in vitro

    Energy Technology Data Exchange (ETDEWEB)

    Dorris, R L [Baylor College of Dentistry, Dallas, Tex. (USA). Dept. of Pharmacology

    1976-01-01

    Release of /sup 3/H-d-..cap alpha..-methyl-m-tyramine (/sup 3/H-MMTA), a false dopaminergic transmitter from rat striatum was studied in vitro. After its initial uptake, /sup 3/H-MMTA was released by high K/sup +/ and by amphetamine. The release requirements were essentially the same as those known to exist for release of dopamine in vitro. These studies indicate that /sup 3/H-MMTA might serve as a useful tool with which to study dopamine release mechanisms in vitro.

  18. Quinolinium 8-hydroxy-7-iodoquinoline-5-sulfonate 0.8-hydrate

    Directory of Open Access Journals (Sweden)

    Graham Smith

    2012-12-01

    Full Text Available In the crystal structure of the title hydrated quinolinium salt of ferron (8-hydroxy-7-iodoquinoline-5-sulfonic acid, C9H7N+·C9H5INO4S−·0.8H2O, the quinolinium cation is fully disordered over two sites (occupancy factors fixed at 0.63 and 0.37 lying essentially within a common plane and with the ferron anions forming π–π-associated stacks down the b axis [minimum ring centroid separation = 3.462 (6 Å]. The cations and anions are linked into chains extending along c through hydroxy O—H...O and quinolinium N—H...O hydrogen bonds to sulfonate O-atom acceptors which are also involved in water O—H...O hydrogen-bonding interactions along b, giving a two-dimensional network.

  19. Bovine serum albumin-catalyzed deprotonation of [1-(13)C]glycolaldehyde: protein reactivity toward deprotonation of the alpha-hydroxy alpha-carbonyl carbon.

    Science.gov (United States)

    Go, Maybelle K; Malabanan, M Merced; Amyes, Tina L; Richard, John P

    2010-09-07

    Bovine serum albumin (BSA) in D(2)O at 25 degrees C and pD 7.0 was found to catalyze the deuterium exchange reactions of [1-(13)C]glycolaldehyde ([1-(13)C]GA) to form [1-(13)C,2-(2)H]GA and [1-(13)C,2,2-di-(2)H]GA. The formation of [1-(13)C,2-(2)H]GA and [1-(13)C,2,2-di-(2)H]GA in a total yield of 51 +/- 3% was observed at early reaction times, and at later times, [1-(13)C,2-(2)H]GA was found to undergo BSA-catalyzed conversion to [1-(13)C,2,2-di-(2)H]GA. The overall second-order rate constant for these deuterium exchange reactions [(k(E))(P)] equals 0.25 M(-1) s(-1). By comparison, (k(E))(P) values of 0.04 M(-1) s(-1) [Go, M. K., Amyes, T. L., and Richard, J. P. (2009) Biochemistry 48, 5769-5778] and 0.06 M(-1) s(-1) [Go, M. K., Koudelka, A., Amyes, T. L., and Richard, J. P. (2010) Biochemistry 49, 5377-5389] have been determined for the wild-type- and K12G mutant TIM-catalyzed deuterium exchange reactions of [1-(13)C]GA, respectively, to form [1-(13)C,2,2-di-(2)H]GA. These data show that TIM and BSA exhibit a modest catalytic activity toward deprotonation of the alpha-hydroxy alpha-carbonyl carbon. We suggest that this activity is intrinsic to many globular proteins, and that it must be enhanced to demonstrate meaningful de novo design of protein catalysts of proton transfer at alpha-carbonyl carbon.

  20. Zeolite-catalysed preparation of alpha-hydroxy carboxylic acids and esters thereof

    DEFF Research Database (Denmark)

    2010-01-01

    A process for the production of lactic acid and 2-hydroxy-3-butenoic acid or esters thereof by conversion of glucose, fructose, sucrose, xylose and glycolaldehyde dissolved in a solvent in presence of a solid Lewis acidic catalyst.......A process for the production of lactic acid and 2-hydroxy-3-butenoic acid or esters thereof by conversion of glucose, fructose, sucrose, xylose and glycolaldehyde dissolved in a solvent in presence of a solid Lewis acidic catalyst....

  1. Efficacy and safety of a new superficial chemical peel using alpha-hydroxy acid, vitamin C and oxygen for melasma.

    Science.gov (United States)

    Kim, Won-Serk

    2013-02-01

    Facial skin pigmentary disorders can be resistant to conventional treatment. Superficial chemical peel is an effective and safe treatment in pigmentary problems including melasma, post-inflammatory hyperpigmentation and aging spots. To assess the efficacy and safety of new superficial chemical peel (Melasma peel, Theraderm®), this is composed of alpha-hydroxy acid (AHAs), vitamin C and oxygen for melasma. Twenty-five ethnic Korean patients (Fitzpatrick skin phototypes IV and V) with moderate to severe melasma were enrolled. The patients underwent four treatments at 1-2-week intervals for 8 weeks. Clinical improvement was evaluated on a 5-point scale by participants and by the same dermatologist, and adverse effects were checked during the study. Improvement in the degree of pigmentation, pores, and evenness were noted. Significant clinical improvement of hyperpigmentation was evident. No adverse effects were reported. New superficial chemical peel using AHAs, vitamin C and oxygen is an effective and very safe treatment for melasma.

  2. Monte Carlo alpha calculation

    Energy Technology Data Exchange (ETDEWEB)

    Brockway, D.; Soran, P.; Whalen, P.

    1985-01-01

    A Monte Carlo algorithm to efficiently calculate static alpha eigenvalues, N = ne/sup ..cap alpha..t/, for supercritical systems has been developed and tested. A direct Monte Carlo approach to calculating a static alpha is to simply follow the buildup in time of neutrons in a supercritical system and evaluate the logarithmic derivative of the neutron population with respect to time. This procedure is expensive, and the solution is very noisy and almost useless for a system near critical. The modified approach is to convert the time-dependent problem to a static ..cap alpha../sup -/eigenvalue problem and regress ..cap alpha.. on solutions of a/sup -/ k/sup -/eigenvalue problem. In practice, this procedure is much more efficient than the direct calculation, and produces much more accurate results. Because the Monte Carlo codes are intrinsically three-dimensional and use elaborate continuous-energy cross sections, this technique is now used as a standard for evaluating other calculational techniques in odd geometries or with group cross sections.

  3. Iridoid glycoside biosynthesis in Penstemon secundiflorus. Another H-5, H-9 trans iridoid glycoside

    DEFF Research Database (Denmark)

    Krull, Robert E.; Stermitz, Frank R.; Franzyk, Henrik

    1998-01-01

    Isolation and characterization of the new iridoid 10-hydroxy-(5 alpha H)-6-epidihydrocornin from Penstemon secundiflorus (Scrophulariaceae) is described. In biosynthetic experiments, deoxyloganic acid was incorporated into the transfused iridoid glycosides (5 alpha H)-6-epidihydrocornin and 10-hy......-hydroxy-(5 alpha H)-6-epidihydrocornin in P. secundiflorus. Formation of the trans-fused compounds is therefore a late event in the biosynthesis and does not occur during iridoid formation by cyclization of the open chain monoterpene precursor. In the same plant, 8-epideoxyloganic acid...

  4. An antiaging skin care system containing alpha hydroxy acids and vitamins improves the biomechanical parameters of facial skin.

    Science.gov (United States)

    Tran, Diana; Townley, Joshua P; Barnes, Tanya M; Greive, Kerryn A

    2015-01-01

    The demand for antiaging products has dramatically increased in recent years, driven by an aging population seeking to maintain the appearance of youth. This study investigates the effects of an antiaging skin care system containing alpha hydroxy acids (AHAs) in conjunction with vitamins B3, C, and E on the biomechanical parameters of facial skin. Fifty two volunteers followed an antiaging skin care regimen comprising of cleanser, eye cream, day moisturizer, and night moisturizer for 21 days. Wrinkle depth (Ry ) and skin roughness (Ra ) were measured by skin surface profilometry of the crow's feet area, and skin elasticity parameters R2 (gross elasticity), R5 (net elasticity), R6 (viscoelastic portion), and R7 (recovery after deformation) were determined for facial skin by cutometer, preapplication and after 7, 14, and 21 days. Volunteers also completed a self-assessment questionnaire. Compared to baseline, Ry and Ra significantly improved by 32.5% (Pskin care treatment. These results were observed by the volunteers with 9 out of 10 discerning an improvement in skin texture and smoothness. Compared to baseline, R2 and R5 significantly increased by 15.2% (Pskin care system containing AHAs and vitamins significantly improves the biomechanical parameters of the skin including wrinkles and skin texture, as well as elasticity without significant adverse effects.

  5. A synthetic chalcone derivative, 2-hydroxy-3',5,5'-trimethoxychalcone (DK-139), suppresses the TNFα-induced invasive capability of MDA-MB-231 human breast cancer cells by inhibiting NF-κB-mediated GROα expression.

    Science.gov (United States)

    Lee, Da Young; Lee, Da Hyun; Jung, Jung You; Koh, Dongsoo; Kim, Geum-Soog; Ahn, Young-Sup; Lee, Young Han; Lim, Yoongho; Shin, Soon Young

    2016-01-01

    2-Hydroxy-3',5,5'-trimenthoxyochalcone (DK-139) is a synthetic chalcone-derived compound. This study evaluated the biological activity of DK-139 on the inhibition of tumor metastasis. Growth-regulated oncogene-alpha (GROα) plays an important role in the progression of tumor development by stimulating angiogenesis and metastasis. In this study, DK-139 inhibited tumor necrosis factor alpha (TNFα)-induced GROα gene promoter activity by inhibiting of IκB kinase (IKK) in MDA-MB231 cells. In addition, DK-139 prevented the TNFα-induced cell migration, F-actin formation, and invasive capability of MDA-MB-231 cells. These findings suggest that DK-139 is a potential drug candidate for the inhibition of tumor cell locomotion and invasion via the suppression of NF-κB-mediated GROα expression. Copyright © 2015 Elsevier Ltd. All rights reserved.

  6. Distribution of alpha3, alpha5 and alpha(v) integrin subunits in mature and immature human oocytes.

    Science.gov (United States)

    Capmany, G; Mart, M; Santaló, J; Bolton, V N

    1998-10-01

    The distribution of three integrin subunits, alpha3, alpha5 and alpha(v), in immature and mature human oocytes has been examined using immunofluorescence and confocal microscopy. The results demonstrate that both alpha5 and alpha(v) are present at the germinal vesicle stage, while alpha3 was only detected in oocytes after germinal vesicle breakdown, in metaphase I and II stage oocytes. The cortical concentration of integrin subunits alpha3 and alpha5 is consistent with their localization in the oolemma. In contrast, the homogeneous distribution of alpha(v) throughout the oocyte suggests the existence of cytoplasmic reservoirs of this protein in the oocyte.

  7. Rhodium(II-Catalysed Intramolecular O-H Insertion of a-Diazo-g-Azido-d-Hydroxy-b-Ketoesters: Evidence for a Novel Sigmatropic Rearrangement of an Allylic Azide Intermediate

    Directory of Open Access Journals (Sweden)

    Padwa Albert

    1999-01-01

    Full Text Available The Rh2(OAc4 catalyzed intramolecular O-H insertion reaction of delta-hydroxy-alpha-diazoesters affords 3(2H-furanone-2-carboxylates in good yield but with moderate selectivity (d.e. ca 60%. The initially formed 2,5-substituted cis-furanones were found to epimerize to the corresponding 2,5-trans isomers when subjected to silica gel chromatography. The Rh2(OAc4 catalyzed decomposition of gamma-azido-delta-hydroxy-alpha-diazoesters also furnished 3(2H-furanone-2-carboxylates. These compounds are derived by a sequential O-H insertion reaction followed by a concerted [3,3]-sigmatropic shift of the allylic azide intermediate.

  8. Synthesis of the omega-brominated alpha-trifluoroacetylcycloalkanones and their isoxazole derivatives

    Directory of Open Access Journals (Sweden)

    Flores Alex F. C.

    2006-01-01

    Full Text Available The reactions of a serie of the 2-trifluoroacetyl-1-methoxy-1-cycloalkenes (1a-1e and 2-trifluoroacetylcycloalkanones (2a-2e with molecular bromine to obtain omega-bromo-alpha-trifluoroacetylcycloalkanones (3a-3e, 4a is reported. Was determined that 2-trifluoroacetyl group have established the C-omega as reactive site. The 2-trifluoroacetylcycloalkanones and omega-bromo-alpha-trifluoroacetylcycloalkanones were reacted with hydroxylamine hydrochloride leading to respective 5-trifluoromethyl-5-hydroxy-4,5-dihydro-3,4-polimethyleneisoxazole derivatives (5c-5e and 6c-6e.

  9. Energy dependence of the zero-range DWBA normalization of the /sup 58/Ni(/sup 3/He,. cap alpha. )/sup 57/Ni reaction. [15 to 205 GeV, finite-range and nonlocality corrections

    Energy Technology Data Exchange (ETDEWEB)

    Shepard, J R; Zimmerman, W R; Kraushaar, J J [Colorado Univ., Boulder (USA). Dept. of Physics and Astrophysics

    1977-01-04

    Strong transitions in the /sup 58/Ni(/sup 3/He,..cap alpha..)/sup 57/Ni reaction were analyzed using both the zero-range and exact finite-range DWBA. Data considered covered a range of bombarding energies from 15 to 205 MeV. The zero-range DWBA described all data well when finite-range and non-locality corrections were included in the local energy approximation. Comparison of zero-range and exact finite-range calculations showed the local energy approximation correction to be very accurate over the entire energy region. Empirically determined D/sub 0/ values showed no energy dependence. A theoretical D/sub 0/ value calculated using an ..cap alpha.. wave function which reproduced the measured ..cap alpha.. rms charge radius and the elastic electron scattering form factor agreed well the empirical values. Comparison was made between these values and D/sub 0/ values quoted previously in the literature.

  10. Hippocampal 3alpha,5alpha-THP may alter depressive behavior of pregnant and lactating rats.

    Science.gov (United States)

    Frye, Cheryl A; Walf, Alicia A

    2004-07-01

    The 5alpha-reduced metabolite of progesterone (P), 5alpha-pregnan-3alpha-ol-20-one (3alpha,5alpha-THP), may mediate progestins' effects to reduce depressive behavior of female rats in part through actions in the hippocampus. To investigate, forced swim test behavior and plasma and hippocampal progestin levels were assessed in groups of rats expected to differ in their 3alpha,5alpha-THP levels due to endogenous differences (pregnant and postpartum), administration of a 5alpha-reductase inhibitor (finasteride; 50 mg/kg sc), and/or gestational stress [prenatal stress (PNS)], an animal model of depression. Pregnant rats had higher plasma and hippocampal 3alpha,5alpha-THP levels and less depressive behavior (decreased immobility, increased struggling and swimming) in the forced swim test than did postpartum rats. Finasteride, compared to vehicle-administration, reduced plasma and hippocampal 3alpha,5alpha-THP levels and increased depressive behavior (increased immobility, decreased struggling and swimming). PNS was associated with lower hippocampal, but not plasma, 3alpha,5alpha-THP levels and increased swimming compared to that observed in control rats. Together, these data suggest that 3alpha,5alpha-THP in the hippocampus may mediate antidepressive behavior of female rats.

  11. Screening alpha-glucosidase and alpha-amylase inhibitors from natural compounds by molecular docking in silico.

    Science.gov (United States)

    Jhong, Chien-Hung; Riyaphan, Jirawat; Lin, Shih-Hung; Chia, Yi-Chen; Weng, Ching-Feng

    2015-01-01

    The alpha-glucosidase inhibitor is a common oral anti-diabetic drug used for controlling carbohydrates normally converted into simple sugars and absorbed by the intestines. However, some adverse clinical effects have been observed. The present study seeks an alternative drug that can regulate the hyperglycemia by down-regulating alpha-glucosidase and alpha-amylase activity by molecular docking approach to screen the hyperglycemia antagonist against alpha-glucosidase and alpha-amylase activities from the 47 natural compounds. The docking data showed that Curcumin, 16-hydroxy-cleroda-3,13-dine-16,15-olide (16-H), Docosanol, Tetracosanol, Antroquinonol, Berberine, Catechin, Quercetin, Actinodaphnine, and Rutin from 47 natural compounds had binding ability towards alpha-amylase and alpha-glucosidase as well. Curcumin had a better biding ability of alpha-amylase than the other natural compounds. Analyzed alpha-glucosidase activity reveals natural compound inhibitors (below 0.5 mM) are Curcumin, Actinodaphnine, 16-H, Quercetin, Berberine, and Catechin when compared to the commercial drug Acarbose (3 mM). A natural compound with alpha-amylase inhibitors (below 0.5 mM) includes Curcumin, Berberine, Docosanol, 16-H, Actinodaphnine/Tetracosanol, Catechin, and Quercetin when compared to Acarbose (1 mM). When taken together, the implication is that molecular docking is a fast and effective way to screen alpha-glucosidase and alpha-amylase inhibitors as lead compounds of natural sources isolated from medicinal plants. © 2015 International Union of Biochemistry and Molecular Biology.

  12. The mechanism and kinetics of the electrochemical cleavage of azo bond of 2-hydroxy-5-sulfophenyl-azo-benzoic acids

    International Nuclear Information System (INIS)

    Mandic, Zoran; Nigovic, Biljana; Simunic, Branimir

    2004-01-01

    The electrochemical reduction of 2-hydroxy-5-[(4-sulfophenyl)azo]benzoic acid, 2-hydroxy-5-[(3-sulfophenyl)azo]benzoic acid, 2-hydroxy-5-[(2-sulfophenyl)azo]benzoic acid and 2-hydroxy-5-azo-benzoic acid has been carried out in aqueous solutions at glassy carbon electrode using cyclic voltammetry and chronoamperometry. The position of sulfo substituent relative to azo bridge as well as pH of the solution have significant impact on the electrochemical behavior of these compounds. It has been proposed that these compounds are reduced predominantly as hydrazone tautomers resulting in corresponding hydrazo compounds. The overall electrochemical reduction follows DISP2 mechanism, ultimately leading to the 5-amino salicylic acid and sulfanilic acid. The rate determining step is the homogenous redox reaction between intermediate hydrazo compound and 5-amino salicylic acid quinoneimine. The mechanism is proposed in which activated complex of 5-amino salicylic acid quinoneimine and intermediate hydrazo compound is formed with the simultaneous loss of one proton

  13. Green synthesis of monodisperse silver nanoparticles using hydroxy propyl methyl cellulose

    Energy Technology Data Exchange (ETDEWEB)

    Dong, Chunfa; Zhang, Xianglin, E-mail: hust_zxl@mail.hust.edu.cn; Cai, Hao

    2014-01-15

    Graphical abstract: -- Highlights: • Synthesis of silver nanoparticles using hydroxy propyl methyl cellulose is reported. • HPMC and glucose are used as capping agent and reducing agent respectively. • It is the first time to use HPMC for synthesis of silver nanoparticles. • The small, spherical and well-dispersed particle is observed in the range of 3–17 nm. • The green method can be extended to other noble metals. -- Abstract: A simple and environmentally friendly method for the synthesis of highly stable and small sized silver nanoparticles with narrow distribution from 3 nm to 17 nm is reported. Silver nitrate, hydroxy propyl methyl cellulose (HPMC) and glucose, were used as silver precursor, capping agents and reducing agents respectively. The formation of silver nanoparticles was observed by change of color from colorless to wine red. The silver nanoparticles were characterized by transmission electron microscopy (TEM), UV–visible spectroscopy (UV–vis), X-ray diffraction (XRD) and Fourier-transform infrared spectroscopy (FT-IR). The results demonstrated that the obtained metallic nanoparticles were single crystalline silver nanoparticles capped with HPMC. The effects of the reaction time, reaction temperature and the concentration of silver ion and reducing agents on the particle size were investigated. A possible formation mechanism was proposed. The method may be extended to other noble metal for other technological applications such as additional medicinal, industrial applications.

  14. Green synthesis of monodisperse silver nanoparticles using hydroxy propyl methyl cellulose

    International Nuclear Information System (INIS)

    Dong, Chunfa; Zhang, Xianglin; Cai, Hao

    2014-01-01

    Graphical abstract: -- Highlights: • Synthesis of silver nanoparticles using hydroxy propyl methyl cellulose is reported. • HPMC and glucose are used as capping agent and reducing agent respectively. • It is the first time to use HPMC for synthesis of silver nanoparticles. • The small, spherical and well-dispersed particle is observed in the range of 3–17 nm. • The green method can be extended to other noble metals. -- Abstract: A simple and environmentally friendly method for the synthesis of highly stable and small sized silver nanoparticles with narrow distribution from 3 nm to 17 nm is reported. Silver nitrate, hydroxy propyl methyl cellulose (HPMC) and glucose, were used as silver precursor, capping agents and reducing agents respectively. The formation of silver nanoparticles was observed by change of color from colorless to wine red. The silver nanoparticles were characterized by transmission electron microscopy (TEM), UV–visible spectroscopy (UV–vis), X-ray diffraction (XRD) and Fourier-transform infrared spectroscopy (FT-IR). The results demonstrated that the obtained metallic nanoparticles were single crystalline silver nanoparticles capped with HPMC. The effects of the reaction time, reaction temperature and the concentration of silver ion and reducing agents on the particle size were investigated. A possible formation mechanism was proposed. The method may be extended to other noble metal for other technological applications such as additional medicinal, industrial applications

  15. Analysis of RNA binding by the dengue virus NS5 RNA capping enzyme.

    Directory of Open Access Journals (Sweden)

    Brittney R Henderson

    Full Text Available Flaviviruses are small, capped positive sense RNA viruses that replicate in the cytoplasm of infected cells. Dengue virus and other related flaviviruses have evolved RNA capping enzymes to form the viral RNA cap structure that protects the viral genome and directs efficient viral polyprotein translation. The N-terminal domain of NS5 possesses the methyltransferase and guanylyltransferase activities necessary for forming mature RNA cap structures. The mechanism for flavivirus guanylyltransferase activity is currently unknown, and how the capping enzyme binds its diphosphorylated RNA substrate is important for deciphering how the flavivirus guanylyltransferase functions. In this report we examine how flavivirus NS5 N-terminal capping enzymes bind to the 5' end of the viral RNA using a fluorescence polarization-based RNA binding assay. We observed that the K(D for RNA binding is approximately 200 nM Dengue, Yellow Fever, and West Nile virus capping enzymes. Removal of one or both of the 5' phosphates reduces binding affinity, indicating that the terminal phosphates contribute significantly to binding. RNA binding affinity is negatively affected by the presence of GTP or ATP and positively affected by S-adensyl methoninine (SAM. Structural superpositioning of the dengue virus capping enzyme with the Vaccinia virus VP39 protein bound to RNA suggests how the flavivirus capping enzyme may bind RNA, and mutagenesis analysis of residues in the putative RNA binding site demonstrate that several basic residues are critical for RNA binding. Several mutants show differential binding to 5' di-, mono-, and un-phosphorylated RNAs. The mode of RNA binding appears similar to that found with other methyltransferase enzymes, and a discussion of diphosphorylated RNA binding is presented.

  16. Proton-transfer compounds of 8-hydroxy-7-iodoquinoline-5-sulfonic acid (ferron) with 4-chloroaniline and 4-bromoaniline.

    Science.gov (United States)

    Smith, Graham; Wermuth, Urs D; Healy, Peter C

    2007-07-01

    The crystal structures of the proton-transfer compounds of ferron (8-hydroxy-7-iodoquinoline-5-sulfonic acid) with 4-chloroaniline and 4-bromoaniline, namely 4-chloroanilinium 8-hydroxy-7-iodoquinoline-5-sulfonate monohydrate, C(6)H(7)ClN(+) x C(9)H(5)INO(4)S(-) x H(2)O, and 4-bromoanilinium 8-hydroxy-7-iodoquinoline-5-sulfonate monohydrate, C(6)H(7)BrN(+) x C(9)H(5)INO(4)S(-) x H(2)O, have been determined. The compounds are isomorphous and comprise sheets of hydrogen-bonded cations, anions and water molecules which are extended into a three-dimensional framework structure through centrosymmetric R(2)(2)(10) O-H...N hydrogen-bonded ferron dimer interactions.

  17. Possibility of studying the activity of rocks by the observation of. cap alpha. -particle tracks in a photographic emulsion

    Energy Technology Data Exchange (ETDEWEB)

    Curie, I

    1946-01-01

    A detailed discussion is presented on the possibility of determining the uranium and thorium content of ordinary rocks by observing ..cap alpha..-particle tracks in a photographic film applied to the rocks' surface. Such determinations can be made only where radioactive equilibrium can be assumed. For the examination of normal granite, exposures of several months are needed. The same method can be used to study the distribution of radioactive elements within the rock.

  18. Quinolinium 8-hy-droxy-7-iodo-quinoline-5-sulfonate 0.8-hydrate.

    Science.gov (United States)

    Smith, Graham

    2012-12-01

    In the crystal structure of the title hydrated quinolinium salt of ferron (8-hy-droxy-7-iodo-quinoline-5-sulfonic acid), C9H7N(+)·C9H5INO4S(-)·0.8H2O, the quinolinium cation is fully disordered over two sites (occupancy factors fixed at 0.63 and 0.37) lying essentially within a common plane and with the ferron anions forming π-π-associated stacks down the b axis [minimum ring centroid separation = 3.462 (6) Å]. The cations and anions are linked into chains extending along c through hy-droxy O-H⋯O and quinolinium N-H⋯O hydrogen bonds to sulfonate O-atom acceptors which are also involved in water O-H⋯O hydrogen-bonding inter-actions along b, giving a two-dimensional network.

  19. The heavy quarkonium spectrum at order $m\\alpha_{s}^{5}\\ln\\alpha_{s}$

    CERN Document Server

    Brambilla, Nora; Soto, Joan; Vairo, Antonio

    1999-01-01

    We compute the complete leading-log terms of the next-to-next-to-next-to-leading-order corrections to potential NRQCD. As a by-product we obtain the leading logs at $O(m\\alpha_s^5)$ in the heavy quarkonium spectrum. These leading logs, when $\\Lambda_{QCD} \\ll m\\alpha_s^2$, give the complete $O(m\\alpha_s^5 \\ln \\alpha_s)$ corrections to the heavy quarkonium spectrum.

  20. 5-[(3-Fluorophenyl(2-hydroxy-6-oxocyclohex-1-en-1-ylmethyl]-6-hydroxy-1,3-dimethylpyrimidine-2,4(1H,3H-dione

    Directory of Open Access Journals (Sweden)

    Assem Barakat

    2016-09-01

    Full Text Available 5-[(3-Fluorophenyl(2-hydroxy-6-oxocyclohex-1-en-1-yl-methyl]-6-hydroxy-1,3-di-methylpyrimidine-2,4(1H,3H-dione 3 was synthesized via a multicomponent reaction. The Aldol–Michael addition reactions of N,N-dimethylbarbituric acid, cyclohexane-1,3-dione, and 3-fluorobenzaldehyde in aqueous solution gave the product in high yield. The molecular structure of the compound was confirmed by spectroscopic methods and X-ray crystallography. The title compound (C19H19FN2O5·H2O crystallizes in the Monoclinic form, P21/c, a = 7.8630 (5 Å, b = 20.0308 (13 Å, c = 11.3987 (8 Å, β = 104.274 (3°, V = 1739.9 (2° Å3, Z = 4, Rint = 0.117, wR(F2 = 0.124, T = 100 K.

  1. Effects of Pauli's principle in the. cap alpha. - /sup 16/O elastic scattering

    Energy Technology Data Exchange (ETDEWEB)

    Schechter, H; Canto, L F; Breitschaft, A M

    1986-03-01

    'Exact' microscopic methods like the RGM (Resonating Group Method) and the GCM (Generator Coordinate Method) and approximate methods like the OCM (Orthogonality Condition Model) are used to study the effects of Pauli's Principle in the ..cap alpha..-/sup 16/O elastic scattering. A method to derive 'exact' effective potentials for the OCM is introduced. These potentials, derived from RGM wave functions, make the OCM identical to the RGM and they have the advantage of being free from poles associated to the forbidden states. Numerical calculations are made with V2 and B1 nucleon-nucleon forces at energies in the range 0-30 MeV. The potentials and the resulting phase-shifts are compared to those obtained from the approximate method suggested by Friedrich and Canto. The problem of searching for local, state independent, potentials for the OCM is discussed.

  2. Spectroscopic study, antimicrobial activity and crystal structures of N-(2-hydroxy-5-nitrobenzalidene)4-aminomorpholine and N-(2-hydroxy-1-naphthylidene)4-aminomorpholine

    Science.gov (United States)

    Yıldız, Mustafa; Ünver, Hüseyin; Dülger, Başaran; Erdener, Diğdem; Ocak, Nazan; Erdönmez, Ahmet; Durlu, Tahsin Nuri

    2005-03-01

    Schiff bases N-(2-hydroxy-3-nitrobenzalidene)4-aminomorpholine ( 1) and N-(2-hydroxy-1-naphthylidene)4-aminomorpholine ( 2) were synthesized from the reaction of 4-aminomorpholine with 2-hydroxy-5-nitrobenzaldehyde and 2-hydroxy-1-naphthaldehyde. Compounds 1 and 2 were characterized by elemental analysis, IR, 1H NMR, 13C NMR and UV-Visible techniques. The UV-Visible spectra of the Schiff bases with OH group in ortho position to the imino group were studied in polar and nonpolar solvents in acidic and basic media. The structures of compounds 1 and 2 have been examined cyrstallographically, for two compounds exist as dominant form of enol-imines in both the solutions and solid state. The title compounds 1 and 2 crystallize in the monoclinic space group P2 1/ c and P2 1/ n with unit cell parameters: a=8.410(1) and 11.911(3), b=6.350(9) and 4.860(9), c=21.728(3) and 22.381(6) Å, β=90.190(1) and 95.6(2)°, V=1160.6(3) and 1289.5(5) Å 3, Dx=1.438 and 1.320 g cm -3, respectively. The crystal structures were solved by direct methods and refined by full-matrix least squares. The antimicrobial activities of compounds 1 and 2 have also been studied. The antimicrobial activities of the ligands have been screened in vitro against the organisms Escherichia coli ATCC 11230, Staphylococcus aureus ATCC 6538, Klebsiella pneumoniae UC57, Micrococcus luteus La 2971, Proteus vulgaris ATCC 8427, Pseudomonas aeruginosa ATCC 27853, Mycobacterium smegmatis CCM 2067, Bacillus cereus ATCC 7064, Listeria monocytogenes ATCC 15313, Candida albicans ATCC 10231, Kluyveromyces fragilis NRRL 2415, Rhodotorula rubra DSM 70403, Debaryomyces hansenii DSM 70238 and Hanseniaspora guilliermondii DSM 3432.

  3. Negligible penetration of incidental amounts of alpha-hydroxy acid from rinse-off personal care products in human skin using an in vitro static diffusion cell model.

    Science.gov (United States)

    Okuda, M; Donahue, D A; Kaufman, L E; Avalos, J; Simion, F A; Story, D C; Sakaguchi, H; Fautz, R; Fuchs, A

    2011-12-01

    Alpha-hydroxy acids (AHAs), primarily glycolic and lactic acids, are widely used in cosmetics to alleviate dyspigmentation, photodamage, and other aging skin conditions and as pH adjusters. Glycolic acid reportedly enhances skin damage after repeated ultraviolet light exposure, e.g., increased sunburn cell formation. This study assessed potential in vitro skin penetration of lactic acid and malic acid incorporated into rinse-off personal care products, compared with rinse-off and leave-on exposures to glycolic acid (10%, pH 3.5) in a reference lotion. Radiolabeled AHA-fortified shampoo, conditioner, and lotion were evenly applied as single doses to human epidermal membranes mounted in static diffusion cells (not occluded). Exposures were 1-3 min (rinse-off) or 24 h (leave-on). Epidermal penetration of malic acid and lactic acid from the rinse-off shampoo and conditioner, respectively, was negligible, with >99% removed by rinsing, a negligible portion remaining in the stratum corneum (≤0.15%), and even less penetrating into the viable epidermis (≤0.04%). Glycolic acid penetration from the leave-on reference lotion was 1.42 μg equiv./cm2/h, with total absorbable dose recovery (receptor fluid plus epidermis) of 2.51%, compared to 0.009%, 0.003%, and 0.04% for the rinse-off reference lotion, shampoo (malic acid), and conditioner (lactic acid) exposures, respectively. Dermal penetration of AHAs into human skin is pH-, concentration-, and time-dependent. Alpha-hydroxy acids in rinse-off shampoos and conditioners are almost entirely removed from the skin within minutes by rinsing (resulting in negligible epidermal penetration). This suggests that ultraviolet radiation-induced skin effects of AHA-containing rinse-off products are negligible. Copyright © 2011 Elsevier Ltd. All rights reserved.

  4. Über die Reaktion von [alpha]- und [beta]-Tetralon mit Kaliumsuperoxid

    OpenAIRE

    Lissel, Manfred

    1984-01-01

    The reaction of [alpha]- and [beta]-tetralone with potassium superoxide is described. In addition to 2-hydroxy-1,4-naphthoquinone [alpha]-naphthol is formed from [alpha]-tetralone and [beta]-naphthol and 2-carboxy-benzenepropionic acid from [beta]-tetralone.

  5. Study of some features of coordination polymerization of. cap alpha. -oxides by the example of forming U(4) alkoxyhalides

    Energy Technology Data Exchange (ETDEWEB)

    Khvostik, G M; Minevich, V Ya; Shupik, A N

    1985-10-01

    The interaction of uranium tetrachloride with ..cap alpha..-oxides in THF has been studied by NMR and conductometry methods. The opening of the oxide cycle under the action of UCl/sub 4/ is shown. The formation of the coordinational bond between the oxygen atom of the polyester clain and the catalytic centre is found to result in retardation of the reactions of the chain propagation. The general scheme of the reactions of interaction of UCl/sub 4/ with oxides is proposed.

  6. cap alpha. -transfer reactions /sup 27/Al(/sup 6/Li, d)/sup 31/P, /sup 29/Si(/sup 6/Li, d)/sup 33/S and /sup 31/P(/sup 6/Li, d)/sup 35/Cl at 36 MeV. [Angular distributions, EFR DWBA, spectroscopic strengths

    Energy Technology Data Exchange (ETDEWEB)

    Eswaran, M A; Gove, H E; Cook, R; Sikora, B [Rochester Univ., NY (USA). Nuclear Structure Research Lab.

    1979-08-13

    The ..cap alpha..-transfer reactions /sup 27/Al(/sup 6/Li,d)/sup 31/P,/sup 29/Si(/sup 6/Li,d) /sup 33/S and /sup 31/P(Li,d)/sup 35/Cl have been studied at a /sup 6/Li energy of 36 MeV. Absolute cross sections and angular distributions have been measured and an exact finite-range distorted-wave Born approximation analysis assuming a direct cluster transfer has been used to extract from the data ..cap alpha..-particle spectroscopic strengths for levels populated in /sup 31/P, /sup 33/S and /sup 35/Cl in three reactions respectively. The results show that in the case of most of the low-lying excited states of /sup 31/P a single value of L of the transferred ..cap alpha..-particle contributes, though a multiplicity of L-values are allowed by angular momentum selection rules. It is also found that the ..cap alpha..-particle spectroscopic strength of the ground state of /sup 31/P is a factor of 2 more than the strengths of the ground states of /sup 33/S and /sup 35/Cl. The ..cap alpha..-spectroscopic strengths of ground states of these, as well as other odd-A s-d shell nuclei, are compared with the presently available shell model calculations.

  7. Formation of 4-hydroxy-2,5-dimethyl-3[2H]-furanone by Zygosaccharomyces rouxii: identification of an intermediate.

    Science.gov (United States)

    Hauck, Tobias; Brühlmann, Fredi; Schwab, Wilfried

    2003-07-01

    The formation of the important flavor compound 4-hydroxy-2,5-dimethyl-3[2H]-furanone (HDMF; Furaneol) from D-fructose-1,6-bisphosphate by the yeast Zygosaccharomyces rouxii was studied with regard to the identification of intermediates present in the culture medium. Addition of o-phenylenediamine, a trapping reagent for alpha-dicarbonyls, to the culture medium and subsequent analysis by high-pressure liquid chromatography with diode array detection revealed the formation of three quinoxaline derivatives derived from D-fructose-1,6-bisphosphate under the applied growth conditions (30 degrees C; pH 4 to 5). Isolation and characterization of these compounds by tandem mass spectrometry and nuclear magnetic resonance spectroscopy led to the identification of phosphoric acid mono-(2,3,4-trihydroxy-4-quinoxaline-2-yl-butyl) ester (Q1), phosphoric acid mono-[2,3-dihydroxy-3-(3-methyl-quinoxaline-2-yl)-propyl] ester (Q2), and phosphoric acid mono-[2-hydroxy-3-(3-methyl-quinoxaline-2-yl)-propyl] ester (Q3). Q1 and Q2 were formed independently of Z. rouxii cells, whereas Q3 was detected only in incubation systems containing the yeast. Identification of Q2 demonstrated for the first time the chemical formation of 1-deoxy-2,3-hexodiulose-6-phosphate in the culture medium, a generally expected but never identified intermediate in the formation pathway of HDMF. Since HDMF was detected only in the presence of Z. rouxii cells, additional enzymatic steps were presumed. Incubation of periplasmic and cytosolic protein extracts obtained from yeast cells with D-fructose-1,6-bisphosphate led to the formation of HDMF, implying the presence of the required enzymes in both extracts.

  8. Chitosan Capped Silver Nanoparticles as Colorimetric Sensor for the Determination of Iron(III

    Directory of Open Access Journals (Sweden)

    Javad Tashkhourian

    2017-12-01

    Full Text Available A selective, simple and low-cost method for the colorimetric determination of Fe3+ ions based on chitosan capped silver nanoparticles (Chit-AgNPs was presented. Chitosan is a cationic polyelectrolyte and possesses amino and hydroxy groups which make it widely used as a capping agent for Ag NPs. The synthesized chitosan capped silver nanoparticles with excellent colloidal stability were characterized by UV–Visible spectrometry, transmission electron microscopy, Fourier transform infrared, X-ray diffraction. Chit-AgNPs exhibit a strong surface plasmon resonance band which disappears in the presence of increasing concentrations of Fe3+ ions. This system showed a visually detectable color change from brownish-yellow to colorless for the selective determination of Fe3+. The method can be applied for the determination of Fe3+ ions in the concentration range of 1.0×10-6 to 5.0×10-4 M. The detection limit was determined from three times the standard deviation of the blank signal (3σ/slope as 5.3 × 10−7 M. The developed method was successfully applied for the determination of Fe3+in real samples

  9. 5 alpha-reductase inhibitors and prostatic disease.

    Science.gov (United States)

    Schröder, F H

    1994-08-01

    5 alpha-Reductase inhibitors are a new class of substances with very specific effects on type I and type II 5 alpha R which may be of use in the treatment of skin disease, such as male pattern baldness, male acne and hirsutism, as well as prostatic hyperplasia and prostate cancer. At least two types of 5 alpha R inhibitors with a different pH optimum have been described. cDNA encoding for both the type I and the type II enzyme has been cloned. Most of the orally effective 5 alpha R inhibitors belong to the class of 4-azasteroids. The radical substituted in the 17 position of the steroid ring seems to be related to species specific variations and to the types of 5 alpha R enzymes in different species and organ systems. 5 alpha R inhibitors lead to a decrease of plasma DHT by about 65% while there is a slight rise in plasma testosterone. The decrease of tissue DHT in the ventral prostate of the intact rat, the dog and in humans is more pronounced and amounts to about 85%. There is a reciprocal rise of tissue T in these systems. The application of an inhibitor of 5 alpha R type II leads to a shrinkage of BPH in men by about 30%. In the rat a similar shrinkage accompanied by a significant decrease of total organ DNA occurs. This decrease, however, is not as pronounced as can be achieved with castration.(ABSTRACT TRUNCATED AT 250 WORDS)

  10. Novel One-Pot Access to 3,3-bis(3-hydroxy-5-substituted-1H-pyrazol-4-yl) indolin-2-ones

    International Nuclear Information System (INIS)

    Lin, Y.; Fu, Z.; Song, Q.; Shen, T.

    2016-01-01

    Sodium bicarbonate was applied as catalyst for the synthesis of 3,3-bis(3-hydroxy-5-substituted-1H-pyrazol-4-yl)indolin-2-ones via the reaction of isatins, hydrazine hydrate and ethyl acetoacetate or ethyl benzoylacetate. This reaction was performed in ethanol at 78 degree C, giving 3,3-bis(3-hydroxy-5-substituted-1H-pyrazol-4-yl)indolin-2-one derivatives in good to excellent yields. The structure of 5-bromo-3,3-bis(3-hydroxy-5-methyl-1H-pyrazol-4-yl) indolin-2-one was unambiguously confirmed by X-ray single crystal structure analysis and a plausible reaction mechanism is also proposed. (author)

  11. PLE CATALYZED HYDROLYZES OF ALPHA-SUBSTITUTED ALPHA-HYDROXY ESTERS - THE INFLUENCE OF THE SUBSTITUENTS

    NARCIS (Netherlands)

    MOORLAG, H; KELLOGG, RM

    1991-01-01

    The enzymatic hydrolyses of a variety of alpha-substituted mandelic and lactic esters using pig liver esterase (PLE) have been investigated. High to moderate enantioselectivity was found for various alpha-substituted mandelic esters, whereas PLE showed low to no enantioselectivity for

  12. 2-Amino-3-(3-hydroxy-1,2,5-thiadiazol-4-yl)propionic acid

    DEFF Research Database (Denmark)

    Johansen, Tommy N; Janin, Yves L; Nielsen, Birgitte

    2002-01-01

    In order to identify new subtype-selective (S)-glutamate (Glu) receptor ligands we have synthesized (RS)-2-amino-3-(3-hydroxy-1,2,5-thiadiazol-4-yl)propionic acid [(RS)-TDPA]. Resolution of (RS)-TDPA by chiral chromatography was performed using a Crownpac CR(+) column affording (R)- and (S......)-TDPA of high enantiomeric purity (enantiomeric excess=99.9%). An X-ray crystallographic analysis revealed that the early eluting enantiomer has R-configuration. Both enantiomers showed high affinity as well as high agonist activity at (RS)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA...... a remarkably low AMPA receptor stereoselectivity, (S)-TDPA showing the highest affinity and (R)-TDPA the most potent agonist activity. In addition, (S)-TDPA was shown to interact with synaptosomal Glu uptake sites displacing [(3)H](R)-aspartic acid (IC(50 ) approximately 390 microM). An enantiospecific...

  13. The effects of DHEA, 3beta-hydroxy-5alpha-androstane-6,17-dione, and 7-amino-DHEA analogues on short term and long term memory in the mouse.

    Science.gov (United States)

    Bazin, Marc-Antoine; El Kihel, Laïla; Boulouard, Michel; Bouët, Valentine; Rault, Sylvain

    2009-11-01

    Neurosteroids have been reported to modulate memory processes in rodents. Three analogues of dehydroepiandrosterone (DHEA), two of them previously described (7beta-aminoDHEA and 7beta-amino-17-ethylenedioxy-DHEA), and a new one (3beta-hydroxy-5alpha-androstane-6,17-dione) were synthesized, and their effects were evaluated on memory. This study examined their effects on long term and short term memory in male (6 weeks old) NMRI mice in comparison with the reference drug. Long term memory was assessed using the passive avoidance task and short term memory (spatial working memory) using the spontaneous alternation task in a Y maze. Moreover, the effects of DHEA and its analogues on spontaneous locomotion were measured. In all tests, DHEA and analogues were injected at three equimolar doses (0.300-1.350-6.075 microM/kg). DHEA and its three analogues administered immediately post-training at the highest doses (6.075 microM/kg, s.c.) improved retention in passive avoidance test. Without effect per se in the spatial working memory task, the four compounds failed to reverse scopolamine (1mg/kg, i.p.)-induced deficit in spontaneous alternation. These data suggested an action of DHEA and analogues in consolidation of long term memory particularly when emotional components are implied. Moreover, data indicated that pharmacological modulation of DHEA as performed in this study provides derivatives giving the same mnemonic profile than reference molecule.

  14. Positron emission tomographic studies on aromatic L-amino acid decarboxylase activity in vivo for L-dopa and 5-hydroxy-L-tryptophan in the monkey brain

    Energy Technology Data Exchange (ETDEWEB)

    Hartvig, P; Tedroff, J; Lindner, K J; Bjurling, P; Chang, C W; Laangstroem, B [Uppsala Univ. (Sweden); Tsukada, H [Central Research Lab., Hamamatsu Photonics Shizuoka, Osaka (Japan); Watanabe, Y [Dept. of Neuroscience, Osaka Bioscience Inst., Osaka (Japan)

    1993-01-01

    The regional brain kinetics following 5-hydroxy-L-([beta]-11 C)tryptophan and L-([beta]-11 C)DOPA intravenous injection was measured in twelve Rhesus monkeys using positron emission tomography (PET). The radiolabelled compounds were also injected together with various doses of unlabelled 5-hydroxy-L-tryptophan or L-DOPA. The radioactivity accumulated in the striatal region and the rate of increased utilization with time was calculated using a graphical method with back of the brain as a reference region. The rate constants for decarboxylation were 0.0070 [+-] 0.0007 (S. D) and 0.0121 [+-] 0.0010 min[sup -1] for 5-hydroxy-L-([beta]-11 C)tryptophan and L-([beta]-11 C)DOPA, respectively. After concomitant injection with unlabelled 5-hydroxy-L-tryptophan, the rate constant of 5-hydroxy-L-([beta]-11 C)tryptophan decreased dose-dependently and a 50 percent reduction was seen with a dose of about 4 mg/kg of unlabelled compound. A decreased utilization rate of L-([beta]-11 C)DOPA was seen only after simultaneous injection of 30 mg/kg of either L-DOPA or 5-hydroxy-L-tryptophan. This capacity limitation was most likely interpreted as different affinity of the striatal aromatic amino acid decarboxylase for L-DOPA and 5-hydroxy-L-tryptophan, respectively.

  15. 5 CFR 550.1409 - Inapplicability of premium pay and aggregate pay caps.

    Science.gov (United States)

    2010-01-01

    ... 5 Administrative Personnel 1 2010-01-01 2010-01-01 false Inapplicability of premium pay and aggregate pay caps. 550.1409 Section 550.1409 Administrative Personnel OFFICE OF PERSONNEL MANAGEMENT CIVIL... Inapplicability of premium pay and aggregate pay caps. Accrued compensatory time off under this subpart is not...

  16. Development of methodology for synthesis of (66alpha66-C)-labeled phenethylamine

    Energy Technology Data Exchange (ETDEWEB)

    Jay, M.; Chaney, J.E.; Digenis, G.A. (Kentucky Univ., Lexington (USA))

    1981-05-01

    A one solvent two-step procedure for the synthesis of (..cap alpha..-C)-labeled phenethylamine is described. The method employs crown ethers to aid in the solubilization of sodium cyanide in tetrahydrofuran (THF) for the formation of phenylacetonitrile from benzyl chloride. Reduction of phenylacetonitrile to phenethylamine was accomplished with borane using the same solvent. The overall yield of phenethylamine was 44.5% based on cyanide. The procedure is amenable to hot cell conditions for eventual (..cap alpha..-/sup 11/C)-labeling of phenethylamine. Dimethylsulfoxide (DMSO) was found to be a less desirable solvent for this reaction due to its participation in the Kornblum oxidation.

  17. An antiaging skin care system containing alpha hydroxy acids and vitamins improves the biomechanical parameters of facial skin

    Science.gov (United States)

    Tran, Diana; Townley, Joshua P; Barnes, Tanya M; Greive, Kerryn A

    2015-01-01

    Background The demand for antiaging products has dramatically increased in recent years, driven by an aging population seeking to maintain the appearance of youth. This study investigates the effects of an antiaging skin care system containing alpha hydroxy acids (AHAs) in conjunction with vitamins B3, C, and E on the biomechanical parameters of facial skin. Methods Fifty two volunteers followed an antiaging skin care regimen comprising of cleanser, eye cream, day moisturizer, and night moisturizer for 21 days. Wrinkle depth (Ry) and skin roughness (Ra) were measured by skin surface profilometry of the crow’s feet area, and skin elasticity parameters R2 (gross elasticity), R5 (net elasticity), R6 (viscoelastic portion), and R7 (recovery after deformation) were determined for facial skin by cutometer, preapplication and after 7, 14, and 21 days. Volunteers also completed a self-assessment questionnaire. Results Compared to baseline, Ry and Ra significantly improved by 32.5% (P<0.0001) and 42.9% (P<0.0001), respectively, after 21 days of antiaging skin care treatment. These results were observed by the volunteers with 9 out of 10 discerning an improvement in skin texture and smoothness. Compared to baseline, R2 and R5 significantly increased by 15.2% (P<0.0001) and 12.5% (P=0.0449), respectively, while R6 significantly decreased by 17.7% (P<0.0001) after 21 days. R7 increased by 9.7% after 21 days compared to baseline but this was not significant over this time period. Conclusion An antiaging skin care system containing AHAs and vitamins significantly improves the biomechanical parameters of the skin including wrinkles and skin texture, as well as elasticity without significant adverse effects. PMID:25552908

  18. Natural 4-Hydroxy-2,5-dimethyl-3(2H)-furanone (Furaneol®)

    OpenAIRE

    Wilfried Schwab

    2013-01-01

    4-Hydroxy-2,5-dimethyl-3(2H)-furanone (HDMF, furaneol®) and its methyl ether 2,5-dimethyl-4-methoxy-3(2H)-furanone (DMMF) are import aroma chemicals and are considered key flavor compounds in many fruit. Due to their attractive sensory properties they are highly appreciated by the food industry. In fruits 2,5-dimethyl-3(2H)-furanones are synthesized by a series of enzymatic steps whereas HDMF is also a product of the Maillard reaction. Numerous methods for the synthetic preparation of these c...

  19. Failure of isolated rat tibial periosteal cells to 5 alpha reduce testosterone to 5 alpha-dihydrotestosterone

    International Nuclear Information System (INIS)

    Turner, R.T.; Bleiberg, B.; Colvard, D.S.; Keeting, P.E.; Evans, G.; Spelsberg, T.C.

    1990-01-01

    Periosteal cells were isolated from tibiae of adult male rats after collagenase treatment. Northern blot analysis of total cytoplasmic RNA extracted from the isolated periosteal cells was positive for expression of genes encoding the osteoblast marker proteins osteocalcin (BGP) and pre-pro-alpha 2(I) chain of type 1 precollagen. The isolated periosteal cells were incubated with 1 nM [3H]testosterone [( 3 H]T) for up to 240 minutes and the reaction products separated by high-performance liquid chromatography. [ 3 H]5 alpha-dihydrotestosterone [( 3 H]DHT) was not detected in extracts of periosteal cell incubations. In contrast, [ 3 H]DHT was produced in a time-dependent manner by cells from seminal vesicles. These results suggest that testosterone 5 alpha-reductase activity is not expressed by osteoblasts in rat tibial periosteum and that the anabolic effects of androgens in this tissue are not mediated by locally produced DHT

  20. O(. cap alpha. sub(S))/sup 2/ calculation of energy-energy correlation in e/sup +/e/sup -/ annihilation and comparison with experimental data

    Energy Technology Data Exchange (ETDEWEB)

    Ali, A [Deutsches Elektronen-Synchrotron (DESY), Hamburg (Germany, F.R.); Barreiro, F [Gesamthochschule Siegen (Germany, F.R.)

    1982-12-02

    We report, in the framework of quantum chromodynamics, an order ..cap alpha..sub(s)/sup 2/ calculation for the energy-energy correlation and the related asymmetry distribution in e/sup +/e/sup -/ annihilation. The normalized distributions are found to be stable and the correction to normalization moderate. The data from PETRA and PEP are analyzed and the QCD scale parameter ..lambda.. is determined. Effects due to the quark and gluon fragmentation are also discussed.

  1. Alpha 1-blockers vs 5 alpha-reductase inhibitors in benign prostatic hyperplasia. A comparative review

    DEFF Research Database (Denmark)

    Andersen, J T

    1995-01-01

    During recent years, pharmacological treatment of symptomatic benign prostatic hyperplasia (BPH) has become the primary treatment choice for an increasing number of patients. The 2 principal drug classes employed are alpha 1-blockers and 5 alpha-reductase inhibitors. Current information from...... of patients who will respond well to alpha 1-blockers have yet to be identified, and data concerning the long term effects of these drugs are not yet available. 5 alpha-Reductase inhibitors have a slow onset of effect, but treatment leads to improvement in symptoms, reduction of the size of the prostate gland...... and improvement in objective parameters for bladder outflow obstruction. Approximately 30 to 50% of patients will respond to treatment with 5 alpha-reductase inhibitors. The definitive role of pharmacological treatment in symptomatic BPH remains to be established, although it seems that patients unfit...

  2. [Monograph for N-Methyl-pyrrolidone (NMP) and human biomonitoring values for the metabolites 5-Hydroxy-NMP and 2-Hydroxy-N-methylsuccinimide].

    Science.gov (United States)

    2015-10-01

    1-Methyl-pyrrolidone (NMP) is used as a solvent in many technical applications. The general population may be exposed to NMP from the use as ingredient in paint and graffiti remover, indoors also from use in paints and carpeting. Because of developmental toxic effects, the use of NMP in consumer products in the EU is regulated. The developmental effects accompanied by weak maternally toxic effects in animal experiments are considered as the critical effects by the German HBM Commission. Based on these effects, HBM-I values of 10 mg/l urine for children and of 15 mg/l for adults, respectively, were derived for the metabolites 5-Hydroxy-NMP and 2-Hydroxy-N-methylsuccinimide. HBM-II-values were set to 30 mg/l urine for children and 50 mg/l for adults, respectively. Because of similar effects of the structural analogue 1-ethyl-2-pyrrolidone (NEP), the possible mixed exposure to both compounds has to be taken into account when evaluating the total burden.

  3. Failure of isolated rat tibial periosteal cells to 5 alpha reduce testosterone to 5 alpha-dihydrotestosterone

    Energy Technology Data Exchange (ETDEWEB)

    Turner, R.T.; Bleiberg, B.; Colvard, D.S.; Keeting, P.E.; Evans, G.; Spelsberg, T.C. (Mayo Clinic, Rochester, MN (USA))

    1990-07-01

    Periosteal cells were isolated from tibiae of adult male rats after collagenase treatment. Northern blot analysis of total cytoplasmic RNA extracted from the isolated periosteal cells was positive for expression of genes encoding the osteoblast marker proteins osteocalcin (BGP) and pre-pro-alpha 2(I) chain of type 1 precollagen. The isolated periosteal cells were incubated with 1 nM (3H)testosterone (({sup 3}H)T) for up to 240 minutes and the reaction products separated by high-performance liquid chromatography. ({sup 3}H)5 alpha-dihydrotestosterone (({sup 3}H)DHT) was not detected in extracts of periosteal cell incubations. In contrast, ({sup 3}H)DHT was produced in a time-dependent manner by cells from seminal vesicles. These results suggest that testosterone 5 alpha-reductase activity is not expressed by osteoblasts in rat tibial periosteum and that the anabolic effects of androgens in this tissue are not mediated by locally produced DHT.

  4. Determination of 5-hydroxy-N-methyl-2-pyrrolidone and 2-hydroxy-N-methylsuccinimide in human plasma and urine using liquid chromatography-electrospray tandem mass spectrometry.

    Science.gov (United States)

    Carnerup, M A; Akesson, B; Jönsson, B A

    2001-09-15

    A method for simultaneous determination of 5-hydroxy-N-methyl-2-pyrrolidone (5-HNMP) and 2-hydroxy-N-methylsuccinimide (2-HMSI) was developed. These compounds are metabolites from N-methyl-2-pyrrolidone (NMP), a powerful and widely used organic solvent. 5-HNMP and 2-HMSI were purified from plasma and urine by solid-phase extraction using Isolute ENV+ columns, and analysed by liquid chromatography coupled to a mass spectrometer fitted with an atmospheric pressure turbo ion spray ionisation interface in the positive ion mode. The method was validated for plasma and urine concentrations from 0.12 to 25 microg/ml. The recoveries for 5-HNMP and 2-HMSI in plasma were 99 and 98%, respectively, and in urine 111 and 106%, respectively. For 5-HNMP and 2-HMSI, the within-day precision in plasma was 1-4 and 3-6%, respectively, and in urine 2-12 and 3-10%, respectively. The corresponding data for the between-day precision was 5 and 3-6%, respectively, and 4-6 and 7-8%, respectively. The detection limit for 5-HNMP was 4 ng/ml in plasma and 120 ng/ml in urine. For 2-HMSI, it was 5 ng/ml in plasma and 85 ng/ml in urine. The method is applicable for analysis of plasma and urine samples from workers exposed to NMP.

  5. Sterol synthesis. A novel reductive rearrangement of an alpha,beta-unsaturated steroidal epoxide; a new chemical synthesis of 5alpha-cholest-8(14)-en-3beta, 15alpha-diol.

    Science.gov (United States)

    Parish, E J; Schroepfer, G J

    1977-04-01

    Reduction of 3beta-benzoyloxy-14alpha,15alpha-epoxy-5alpha-cholest-7-ene with either lithium triethylboro-hydride or lithium aluminum hydride (4 molar excess) gave 5-alpha-cholest-8(14)-en-3beta,15alpha-diol in high yield. Reduction of the epoxy ester with lithium triethylborodeuteride or lithium aluminum deuteride (4 molar excess) gave [7alpha-2-H]-5alpha-cholest-8(14)-en-3beta,15alpha-diol. Reduction of 2beta-benzoyloxy-14alpha,15alpha-epoxy-5alpha-cholest-7-ene with a large excess (24 molar excess) of lithium aluminum hydride gave, in addition to the expected 5alpha-cholest-8(14)-en-3beta,15alpha-diol, a significant yield (33%) of 5alpha-cholest-8(14)-en-3beta-o1. Reduction of the epoxy ester with a large excess (24 molar excess) of lithium aluminum deuteride gave [7alpha-2H]-5alpha-cholest-8(14)-en-3beta,15alpha-diol and 5alpha-cholest-8(14)-en-3beta-o1 which contained two atoms of stably bound deuterium.

  6. L-Cysteine Capped CdSe Quantum Dots Synthesized by Photochemical Route.

    Science.gov (United States)

    Singh, Avinash; Kunwar, Amit; Rath, M C

    2018-05-01

    L-cysteine capped CdSe quantum dots were synthesized via photochemical route in aqueous solution under UV photo-irradiation. The as grown CdSe quantum dots exhibit broad fluorescence at room temperature. The CdSe quantum dots were found to be formed only through the reactions of the precursors, i.e., Cd(NH3)2+4 and SeSO2-3 with the photochemically generated 1-hydroxy-2-propyl radicals, (CH3)2COH radicals, which are formed through the process of H atom abstraction by the photoexcited acetone from 2-propanol. L-Cysteine was found to act as a suitable capping agent for the CdSe quantum dots and increases their biocompatability. Cytotoxicty effects of these quantum dots were evaluated in Chinese Hamster Ovary (CHO) epithelial cells, indicated a significant lower level for the L-cysteine capped CdSe quantum dots as compare to the bare ones.

  7. Human pro. cap alpha. 1)(I) collagen: cDNA sequence for the C-propeptide domain

    Energy Technology Data Exchange (ETDEWEB)

    Maekelae, J K; Raassina, M; Virta, A; Vuorio, E

    1988-01-11

    The authors have previously constructed a cDNA clone pHCAL1, covering most of the C-terminal propeptide domain of human pro..cap alpha..1(I) collagen mRNA,by inserting a 678 bp EcoRI-XhoI fragment of cDNA into pBR322. Since the XhoI/SalI ligation prevented removal of the insert, they used the same strategy to obtain a similar clone in pUC8. RNA was isolated from fetal calvarial bones. The cDNA was digested with EcoRI and XhoI and fractionated on a 1 % agarose gel. Fragments of 650-700 bp were cloned in pUC8 at the polylinker site, which now permits easy removal of the insert. The new clone was named pHCAL1U since the RNA was isolated from another individual. The approach outlined is useful for studies on individual variation which is important to recognize when searching for disease-related mutations in type I collagen.

  8. Hepatoprotective Activity of a Complex Compound of 5-Hydroxy-6-Methyluracil and Succinic Acid in Experimental Peritonitis

    Directory of Open Access Journals (Sweden)

    D. A. Yenikeyev

    2008-01-01

    Full Text Available Objective: to evaluate the hepatoprotective efficacy of a complex compound of 5-hydroxy-6-methyluracil and succinic acid in experimental peritonitis. Materials and methods. Experiments were carried out on 48 male albino rats in which peritonitis was simulated via intraperitoneal administration of 7% fecal suspension in a dose of 0.6 ml per 100 g bodyweight. The rate of free radical oxidation processes, the activity of antioxidative protection, the degree of endogenous intoxication and cytolytic syndrome, and the effect of the test compound on these parameters were estimated in the experiment. Results. With the development of an abdominal inflammatory process, there were increases in rates of endogenous intoxication and free radical oxidation (FRO, a change in the activity of antioxidative protection enzymes, and a reduction in the levels of ceruloplasmin and sulfahydryl groups. The complex compound, that comprised 5-hydroxy-6-methyluracil and succinic acid used as monotherapy, reduced the degree of endogenous intoxication, FRO, and lipid peroxidation-antioxidative defense system imbalance. Conclusion. The experimental data suggest that the use of the complex compound containing succinic acid and 5-hydroxy-6-methy-luracil is pathogenetically warranted. Key words: peritonitis, lipid peroxidation, antioxidants, succinic acid, pyrim-idine derivatives.

  9. Ethyl 4-chloro-2′-fluoro-3-hydroxy-5-methylbiphenyl-2-carboxylate

    Directory of Open Access Journals (Sweden)

    Muhammad Adeel

    2011-09-01

    Full Text Available In the title compound, C16H14ClFO3, the dihedral angle between the mean planes of the two benzene rings is 71.50 (5°. Due to an intramolecular O—H...O hydrogen bond between the hydroxy group and the carbonyl O atom of the ethyl ester group, the ethyl ester group lies within the ring plane. The crystal structure is consolidated by intermolecular C—H...O and C—H...F interactions.

  10. Introduction of potential helix-capping residues into an engineered helical protein.

    Science.gov (United States)

    Parker, M H; Hefford, M A

    1998-08-01

    MB-1 is an engineered protein that was designed to incorporate high percentages of four amino acid residues and to fold into a four-alpha-helix bundle motif. Mutations were made in the putative loop I and III regions of this protein with the aim of increasing the stability of the helix ends. Four variants, MB-3, MB-5, MB-11 and MB-13, have replacements intended to promote formation of an 'N-capping box'. The loop I and III sequences of MB-3 (both GDLST) and MB-11 (GGDST) were designed to cause alphaL C-terminal 'capping' motifs to form in helices I and III. MB-5 has a sequence, GPDST, that places proline in a favourable position for forming beta-turns, whereas MB-13 (GLDST) has the potential to form Schellman C-capping motifs. Size-exclusion chromatography suggested that MB-1, MB-3, MB-5, MB-11 and MB-13 all form dimers, or possibly trimers. Free energies for the unfolding of each of these variants were determined by urea denaturation, with the loss of secondary structure followed by CD spectroscopy. Assuming an equilibrium between folded dimer and unfolded monomer, MB-13 had the highest apparent stability (40.5 kJ/mol, with +/-2.5 kJ/mol 95% confidence limits), followed by MB-11 (39.3+/-5.9 kJ/mol), MB-3 (36.4+/-1.7 kJ/mol), MB-5 (34.7+/-2.1 kJ/mol) and MB-1 (29.3+/-1.3 kJ/mol); the same relative stabilities of the variants were found when a folded trimer to unfolded monomer model was used to calculate stabilities. All of the variants were relatively unstable for dimeric proteins, but were significantly more stable than MB-1. These findings suggest that it might be possible to increase the stability of a protein for which the three-dimensional structure is unknown by placing amino acid residues in positions that have the potential to form helix- and turn-stabilizing motifs.

  11. Synthesis, DNA binding and cytotoxic activity of pyrimido[4',5':4,5]thieno(2,3-b)quinoline with 9-hydroxy-4-(3-diethylaminopropylamino) and 8-methoxy-4-(3-diethylaminopropylamino) substitutions.

    Science.gov (United States)

    KiranKumar, Hulihalli N; RohitKumar, Heggodu G; Advirao, Gopal M

    2018-01-01

    Two new derivatives of pyrimido[4',5';4,5]thieno(2,3-b)quinoline (PTQ), 9-hydroxy-4-(3-diethylaminopropylamino)pyrimido[4',5';4,5]thieno(2,3-b)quinoline (Hydroxy-DPTQ) and 8-methoxy-4-(3-diethylaminopropylamino)pyrimido[4',5';4,5]thieno(2,3-b)quinoline (Methoxy-DPTQ) were synthesized and their DNA binding ability was analyzed using spectroscopy (UV-visible, fluorescence and circular dichroism), ethidium bromide dye displacement assay, melting temperature (T m ) analysis and computational docking studies. The hypochromism in UV-visible spectrum and increased fluorescence emission of Hydroxy-DPTQ and Methoxy-DPTQ in the presence of DNA suggested the molecule-DNA interaction. The association constants calculated from UV-visible and spectral titrations were of the order 10 4 to 10 6 M -1 . Circular dichroism studies corroborated the induced conformational changes in DNA upon addition of molecules. The change in the ellipticity was observed both in negative and positive peak of DNA, thus, suggesting the intercalation of molecules. The observed displacement of ethidium bromide from the DNA and increased T m , upon addition of DNA confirmed the intercalative mode of binding. This was further validated by computational docking, which showed clear intercalation of molecules into the d(GpC)-d(CpG) site of the receptor DNA. Anticancer activities of these molecules are evaluated by using MTT assay. Both molecules showed antiproliferative activity against all the three cancer cells studied, with Hydroxy-DPTQ being more potential molecule among the two. IC 50 value of Hydroxy-DPTQ and Methoxy-DPTQ were in the range of 3-5μM and 130-250μM, respectively. Copyright © 2017 Elsevier B.V. All rights reserved.

  12. Impact of DNA3'pp5'G capping on repair reactions at DNA 3' ends.

    Science.gov (United States)

    Das, Ushati; Chauleau, Mathieu; Ordonez, Heather; Shuman, Stewart

    2014-08-05

    Many biological scenarios generate "dirty" DNA 3'-PO4 ends that cannot be sealed by classic DNA ligases or extended by DNA polymerases. The noncanonical ligase RtcB can "cap" these ends via a unique chemical mechanism entailing transfer of GMP from a covalent RtcB-GMP intermediate to a DNA 3'-PO4 to form DNA3'pp5'G. Here, we show that capping protects DNA 3' ends from resection by Escherichia coli exonucleases I and III and from end-healing by T4 polynucleotide 3' phosphatase. By contrast, the cap is an effective primer for DNA synthesis. E. coli DNA polymerase I and Mycobacterium DinB1 extend the DNAppG primer to form an alkali-labile DNApp(rG)pDNA product. The addition of dNTP depends on pairing of the cap guanine with an opposing cytosine in the template strand. Aprataxin, an enzyme implicated in repair of A5'pp5'DNA ends formed during abortive ligation by classic ligases, is highly effective as a DNA 3' decapping enzyme, converting DNAppG to DNA3'p and GMP. We conclude that the biochemical impact of DNA capping is to prevent resection and healing of a 3'-PO4 end, while permitting DNA synthesis, at the price of embedding a ribonucleotide and a pyrophosphate linkage in the repaired strand. Aprataxin affords a means to counter the impact of DNA capping.

  13. Determination of /sup 240/Pu//sup 239/Pu ratio in the environmental samples based on the measurement of Lx/. cap alpha. -ray activity ratio

    Energy Technology Data Exchange (ETDEWEB)

    Komura, K.; Sakanoue, M.; Yamamoto, M.

    1984-06-01

    The determination of the /sup 240/Pu//sup 239/Pu isotopic ratio in environmental samples has been attempted by the measurement of the Lx/..cap alpha..-ray activity ratio using a Ge-LEPS (low-energy photon spectrometer) and a surface-barrier Si detector. By this method, interesting data were obtained for various samples collected from Thule, Greenland, Bikini Atoll and Nagasaki, as well as for some soils collected from near and off-site locations of atomic power stations.

  14. 1,5-Bis(2-hydroxy-3-methoxybenzylidenecarbonohydrazide methanol 0.47-solvate

    Directory of Open Access Journals (Sweden)

    Mouhamadou Moustapha Sow

    2014-04-01

    Full Text Available In the title compound, C17H18N4O5·0.47CH3OH, the virtually planar (r.m.s. deviation = 0.128 Å carbonohydrazide molecule is located on a twofold axis and conformation of its C=N bonds is E. There are short intramolecular O—H...N hydrogen bonds between the hydroxy groups and hydrazide N atoms. In the crystal, bifurcated N—H...(O,O hydrogen bonds assemble the carbonohydrazide molecules into a three-dimensional network. There are C2 symmetric voids in this network, 47% of which are occupied by disordered methanol molecules.

  15. High temperature study on the thermal properties of few-layer Mo0.5W0.5S2 and effects of capping layers

    Directory of Open Access Journals (Sweden)

    Hong Gu

    Full Text Available We investigated the thermal properties of few-layer Mo0.5W0.5S2 using a series of samples with different kinds of capping layers. Temperature-dependent Raman measurements were conducted in the range of 300–500 K, with power-dependent measurements also carried out. It indicated, for the few-layer Mo0.5W0.5S2, the temperature coefficients of the WS2-like E12g mode, MoS2-like E12g mode and A1g mode were −0.0155 cm−1/K, −0.0146 cm−1/K, and −0.0130 cm−1/K, respectively. And the thermal conductivity was estimated to be 44.8 W/mK. Moreover, the Mo0.5W0.5S2 samples coated with capping layers (ZrO2, HfO2 both showed a better thermal stability and a larger thermal conductivity than the one without. The results revealed that the capping layer should be an important factor in the thermal property. Keywords: Mo0.5W0.5S2, TMDs, Thermal properties, High temperature, Capping layers, Raman

  16. Grafting of 2 (2-hydroxy-5-vinylphenyl) 2H-benzotriazole onto polymers with aliphatic groups. Synthesis and polymerization of 2 (2-hydroxy-5-isopropenylphenyl) 2H-benzotriazole and a new synthesis of 2 (2-hydroxy-5-vinylphenyl) 2H-benzotriazole

    Science.gov (United States)

    Pradellok, W.; Nir, Z.; Vogl, O.

    1981-01-01

    Successful grafting of 2(2-hydroxy-5-vinylphenyl)2H-benzotriazole onto saturated aliphatic C-H groups of polymers has been accomplished. When the grafting reaction was carried out in chlorobenzene at 150 C = 160 C with di-tertiarybutylperoxide as the grafting initiator, grafts as high as 20 percent - 30 percent at a grafting efficiency of 50 percent and 80 percent have readily been obtained. The grafting reaction was carried out in tubes sealed under high vacuum since trace amounts of oxygen cause complete inhibition of the grafting reaction by the phenolic monomer. On a variety of different polymers including atactic polypropylene, ethylene/vinyl acetate copolymer, poly(methyl methacrylate), poly(butyl acrylate), and polycarbonate were used.

  17. Towards novel efficient and stable nuclear import signals: synthesis and properties of trimethylguanosine cap analogs modified within the 5',5'-triphosphate bridge.

    Science.gov (United States)

    Zytek, Malgorzata; Kowalska, Joanna; Lukaszewicz, Maciej; Wojtczak, Blazej A; Zuberek, Joanna; Ferenc-Mrozek, Aleksandra; Darzynkiewicz, Edward; Niedzwiecka, Anna; Jemielity, Jacek

    2014-12-07

    A trimethylguanosine (TMG) cap is present at the 5' end of several small nuclear and nucleolar RNAs. Recently, it has been reported that the TMG cap is a potential nuclear import signal for nucleus-targeting therapeutic nucleic acids and proteins. The import is mediated by recognition of the TMG cap by the snRNA transporting protein, snurportin1. This work describes the synthesis and properties of a series of dinucleotide TMG cap (m3(2,2,7)GpppG) analogs modified in the 5',5'-triphosphate bridge as tools to study TMG cap-dependent biological processes. The bridge was altered at different positions by introducing either bridging (imidodiphosphate, O to NH and methylenebisphosphonate, O to CH2) or non-bridging (phosphorothioate, O to S and boranophosphate, O to BH3) modifications, or by elongation to tetraphosphate. The stability of novel analogs in blood serum was studied to reveal that the α,β-bridging O to NH substitution (m3(2,2,7)GppNHpG) confers the highest resistance. Short RNAs capped with analogs containing α,β-bridging (m3(2,2,7)GppNHpG) or β-non-bridging (m3(2,2,7)GppSpG D2) modifications were resistant to decapping pyrophosphatase, hNudt16. Preliminary studies on binding by human snurportin1 revealed that both O to NH and O to S substitutions support this binding. Due to favorable properties in all three assays, m3(2,2,7)GppNHpG was selected as a promising candidate for further studies on the efficiency of the TMG cap as a nuclear import signal.

  18. Synthesis of the natural product building block 5-(3-bromophenyl)-4-hydroxy-5-methylhexan-2-one and its chiral characterization by using chiroptical spectroscopy.

    Science.gov (United States)

    De Gussem, Ewoud; Cornelus, Jelle; Pieters, Sam; Van den Bossche, Dries; Van der Eycken, Johan; Herrebout, Wouter; Bultinck, Patrick

    2013-10-07

    The absolute configuration of 5-(3-bromophenyl)-4-hydroxy-5-methylhexan-2-one, an intermediate in the synthesis of various natural products, is assigned by using vibrational circular dichroism (VCD), electronic circular dichroism (ECD), and optical rotatory dispersion (ORD). Experimental spectra were compared to density functional theory (DFT) calculations of the molecule with known configuration. These three techniques independently confirm that the absolute configuration is (S)-5-(3-bromophenyl)-4-hydroxy-5-methylhexan-2-one, thus enabling us to assign the absolute configuration with high reliability. The reliability of the VCD analysis was assessed quantitatively by using the CompareVOA program. We found that, in cases in which the agreement between theory and experiment was very good, a value of 10 cm(-1) for the triangular weighting function gave a more-realistic discriminative power between enantiomers than the default value of 20 cm(-1). Copyright © 2013 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim.

  19. 4-{3-[Hydroxy(phenylmethyl]-5-thioxo-4,5-dihydro-1H-1,2,4-triazol-4-yl}benzenesulfonamide

    Directory of Open Access Journals (Sweden)

    Mehmet Akkurt

    2010-04-01

    Full Text Available In the title compound, C15H14N4O3S2, the hydroxy group is disordered over two positions with occupancies of 0.619 (5 and 0.381 (5. The benzene ring attached to the heterocycle makes a dihedral angle of 86.92 (9° with respect to the best plane through the five-membered ring. The crystal packing is stabilized by intermolecular O—H...O, N—H...S, N—H...N, C—H...O and C—H...N hydrogen bonds, and N—H...π and C—H...π interactions.

  20. Lariat capping as a tool to manipulate the 5' end of individual yeast mRNA species in vivo

    DEFF Research Database (Denmark)

    Krogh, Nicolai; Pietschmann, Max; Schmid, Manfred

    2017-01-01

    The 5' cap structure of eukaryotic mRNA is critical for its processing, transport, translation, and stability. The many functions of the cap and the fact that most, if not all, mRNA carries the same type of cap makes it difficult to analyze cap function in vivo at individual steps of gene...... in the budding yeast Saccharomyces cerevisiae presumably without cofactors and that lariat capping occurs cotranscriptionally. The lariat-capped reporter mRNA is efficiently exported to the cytoplasm where it is found to be oligoadenylated and evenly distributed. Both the oligoadenylated form and a lariat......-capped mRNA with a templated poly(A) tail translates poorly, underlining the critical importance of the m(7)G cap in translation. Finally, the lariat-capped RNA exhibits a threefold longer half-life compared to its m(7)G-capped counterpart, consistent with a key role for the m(7)G cap in mRNA turnover. Our...

  1. Facile synthesis of hydroxy-modified MOF-5 for improving the adsorption capacity of hydrogen by lithium doping.

    Science.gov (United States)

    Kubo, Masaru; Hagi, Hayato; Shimojima, Atsushi; Okubo, Tatsuya

    2013-11-01

    A facile synthesis of partially hydroxy-modified MOF-5 and its improved H2-adsorption capacity by lithium doping are reported. The reaction of Zn(NO3)2·6H2O with a mixture of terephthalic acid (H2BDC) and 2-hydroxyterephthalic acid (H2BDC-OH) in DMF gave hydroxy-modified MOF-5 (MOF-5-OH-x), in which the molar fraction (x) of BDC-OH(2-) was up to 0.54 of the whole ligand. The MOF-5-OH-x frameworks had high BET surface areas (about 3300 m(2) g(-1)), which were comparable to that of MOF-5. We suggest that the MOF-5-OH-x frameworks are formed by the secondary growth of BDC(2-)-rich MOF-5 seed crystals, which are nucleated during the early stage of the reaction. Subsequent Li doping into MOF-5-OH-x results in increased H2 uptake at 77 K and 0.1 MPa from 1.23 to 1.39 wt.% and an increased isosteric heat of H2 adsorption from 5.1-4.2 kJ mol(-1) to 5.5-4.4 kJ mol(-1). Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  2. Immunohistochemical and radioimmunological demonstration of alpha/sub 1/-fetoprotein in nonmalignant changes of human gastric mucosa

    Energy Technology Data Exchange (ETDEWEB)

    Falser, N; Lederer, B; Reissigl, H [Innsbruck Univ. (Austria). Pathologisch-Anatomisches Lab.; Innsbruck Univ. (Austria). Gastroenterologisches Lab.)

    1977-07-01

    The occurence of ..cap alpha../sub 1/ fetoprotein in nonmalignant changes of the gastric mucosa was investigated by means of immunohistochemistry and radioimmunonoassay. The investigations were performed in tissue sections, cytological imprint preparations as well as in homogenized tissue samples (obtained by gastroscopy). ..cap alpha../sub 1/ fetoprotein could be demonstrated by immuno-histochemistry in about 90% of the samples originating from the surroundings of gastric ulcer and the region of gastrojejunostomy after B II-resection. The RIA was positive in about 75% of the tissue samples, whereas from gastric juice only 40% of positive results could be obtained. No ..cap alpha../sub 1/ fetoprotein-activity could be demonstrated in serum samples. These investigations indicate that ..cap alpha../sub 1/ fetoprotein is not exclusively synthesized by embryonic or neoplastic tissues and also can be synthesized also by regenerating cell-systems. It may be supposed that this synthesis represents an unspecific answer to growth-stimulation.

  3. Role of spinal cord alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors in complete Freund's adjuvant-induced inflammatory pain

    Directory of Open Access Journals (Sweden)

    Shih Ming-Hung

    2008-12-01

    Full Text Available Abstract Spinal cord α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors (AMPARs mediate acute spinal processing of nociceptive and non-nociceptive information, but whether and how their activation contributes to the central sensitization that underlies persistent inflammatory pain are still unclear. Here, we examined the role of spinal AMPARs in the development and maintenance of complete Freund's adjuvant (CFA-induced persistent inflammatory pain. Intrathecal application of two selective non-competitive AMPAR antagonists, CFM-2 (25 and 50 μg and GYKI 52466 (50 μg, significantly attenuated mechanical and thermal hypersensitivities on the ipsilateral hind paw at 2 and 24 h post-CFA injection. Neither CFM-2 nor GYKI 52466 affected the contralateral basal responses to thermal and mechanical stimuli. Locomotor activity was not altered in any of the drug-treated animals. CFA-induced inflammation did not change total expression or distribution of AMPAR subunits GluR1 and GluR2 in dorsal horn but did alter their subcellular distribution. The amount of GluR2 was markedly increased in the crude cytosolic fraction and decreased in the crude membrane fraction from the ipsilateral L4–5 dorsal horn at 24 h (but not at 2 h post-CFA injection. Conversely, the level of GluR1 was significantly decreased in the crude cytosolic fraction and increased in the crude membrane fraction from the ipsilateral L4–5 dorsal horn at 24 h (but not at 2 h post-CFA injection. These findings suggest that spinal AMPARs might participate in the central spinal mechanism of persistent inflammatory pain.

  4. Direct chemical synthesis of 1 alpha,25-dihydroxy[26,27-3H] vitamin D3 with high specific activity: its use in receptor studies

    International Nuclear Information System (INIS)

    Napoli, J.L.; Mellon, W.S.; Fivizzani, M.A.; Schnoes, H.K.; DeLuca, H.F.

    1980-01-01

    The first direct chemical synthesis of radiolabeled 1 alpha, 25-dihydroxyvitamin D3 is reported. Unlike all previous syntheses, the new approach does not rely on enzymatic 1 alpha-hydroxylation of radiolabeled precursors. Rather, isotope is introduced in the last synthetic step by reaction of [3H] -methylmagnesium bromide with methyl 1 alpha-hydroxy-26,27-dinorvitamin D3-25-carboxylate to give 1 alpha,25-dihydroxy-[26,27-3H] vitamin D3 with a specific activity of 160 Ci/mmol. Mass spectroscopy confirmed that the radiohormone consists of a single isomer with six tritium atoms bound to carbons 26 and 27. Synthetically produced 1 alpha,25-dihydroxy [26,27-3H] vitamin D3 is indistinguishable from 1 alpha,25-dihydroxy-[26,27-3H] vitamin D3 obtained from the enzymatic 1 alpha-hydroxylation of 25-hydroxy[26,27-3H] vitamin D3 (160 Ci/mmol) by high-pressure liquid chromatography analysis and in the competitive binding assay using chick intestinal cytosol as the receptor source. Equilibrium dissociation constant measurements with the high specific activity radiohormone indicate a Kd of 8.2 x 10(-11) M for the chick intestinal cytosol 1 alpha,25-dihydroxyvitamin D3 receptor--a value considerably lower than the constants in the range of (1-5) x 10(-9) M previously reported

  5. A brief history of TRIM5alpha.

    Science.gov (United States)

    Newman, Ruchi M; Johnson, Welkin E

    2007-01-01

    In spite of the fact that the first isolates of HIV-1 became available more than 20 years ago, there is still no robust animal model for HIV-1 replication and pathogenesis. This is largely due to the existence of multiple genetic barriers to HIV-1 replication in most nonhuman primates, including a severe block targeting the early, post-entry phase of the viral replication cycle. It is now known that a protein called TRIM5alpha mediates this early restriction in nonhuman primate cells. Tissue culture experiments, together with genetic association studies involving multiple HIV/AIDS cohorts, indicate that the human orthologue of TRIM5alpha does not have a significant impact on HIV-1 replication. However, most human alleles encode a functional protein that can restrict at least one retrovirus unrelated to HIV-1 (N-tropic murine leukemia virus), although one deleterious mutation (H43Y) is present at high frequency in human populations. Phylogenetic analyses of the TRIM5 locus reveal that prehistoric retroviral epidemics, not unlike the current HIV/AIDS pandemic, played a significant role in the evolutionary history of humans and their primate relatives. The discovery of TRIM5alpha's antiretroviral activity sparked the imaginations of many laboratories, and considerable effort has now been channeled into characterizing the protein and determining its possible mechanism(s) of action. It is hoped that research on TRIM5alpha will contribute to the establishment of new and improved models for HIV replication and AIDS pathogenesis, point the way towards novel therapeutic targets to stem the tide of the human AIDS epidemic, provide an experimental window onto the early, post-entry stages of the retroviral replication cycle, and even inspire the search for other cellular factors that modulate retroviral infection.

  6. Transformation of alpha-tocopherol (vitamin E) and related chromanol model compounds into their phenoxonium ions by chemical oxidation with the nitrosonium cation.

    Science.gov (United States)

    Lee, Stephen B; Lin, Ching Yeh; Gill, Peter M W; Webster, Richard D

    2005-12-09

    [reaction: see text] Alpha-tocopherol (alpha-TOH), the main oil component making up vitamin E, and its nonnatural solid 6-hydroxy-2,2,5,7,8-pentamethylchroman and 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid structurally related analogues were oxidized quantitatively with 2 mol equiv of NO+ SbF6(-) in CH3CN at 233 K to form phenoxonium cations (alpha-TO+ SbF6(-)) in a chemically reversible two-electron/one-proton process. Solution-phase infrared spectroscopy, 1H and 13C NMR spectroscopy, and corresponding theoretical calculations of the spectroscopic data using density-based and wave-function-based models support the identity of the remarkably stable phenoxonium cations. The presence of an oxygen atom in the para position to the hydroxyl group and the chromanol ring structure appear to be important factors in stabilization of the phenoxonium ions, which raises the interesting possibility that the cations play a crucial role in the mode of action of vitamin E in biological systems. Although the phenoxonium cations are reactive toward nucleophiles such as water, they may be moderately stable in the hydrophobic (lipophilic) environment where vitamin E is known to occur naturally.

  7. N-tert-Butyl-3-hydroxy-5-androstene-17-carboxamide monohydrate

    Directory of Open Access Journals (Sweden)

    Jiang-Sheng Li

    2009-07-01

    Full Text Available In the title compound, C24H39NO2·H2O, the A and C rings of the pregnolene derivative sterol adopt chair conformations, with the B ring in a flattened chair conformation and the five-membered ring in an envelope conformation twisted about the C/D ring junction. The N-tert-butylcarboxamide substituent is equatorial. The 3β-hydroxy H atom and one H atom of the water molecule are disordered over two positions with equal occupancies. In the crystal structure, O—H...O hydrogen bonds between the 3β-hydroxy groups of neighbouring molecules form dimers in the bc plane and these dimers are stacked along the a axis by additional O—H...O hydrogen bonds involving the water molecules. The steric effect of the bulky tert-butyl substituent in the carboxamide chain precludes hydrogen-bond formation by the N—H group.

  8. Structural changes of eIF4E upon binding to the mRNA 5' monomethylguanosine and trimethylguanosine Cap.

    Science.gov (United States)

    Rutkowska-Wlodarczyk, Izabela; Stepinski, Janusz; Dadlez, Michal; Darzynkiewicz, Edward; Stolarski, Ryszard; Niedzwiecka, Anna

    2008-03-04

    Recognition of the 5' cap by the eukaryotic initiation factor 4E (eIF4E) is the rate-limiting step in the ribosome recruitment to mRNAs. The regular cap consists of 7-monomethylguanosine (MMG) linked by a 5'-5' triphosphate bridge to the first transcribed nucleoside, while some primitive eukaryotes possess a N (2), N (2),7-trimethylguanosine (TMG) cap structure as a result of trans splicing. Mammalian eIF4E is highly specific to the MMG form of the cap in terms of association constants and thermodynamic driving force. We have investigated conformational changes of eIF4E induced by interaction with two cap analogues, 7-methyl-GTP and N (2), N (2),7-trimethyl-GTP. Hydrogen-deuterium exchange and electrospray mass spectrometry were applied to probe local dynamics of murine eIF4E in the apo and cap-bound forms. The data show that the cap binding induces long-range conformational changes in the protein, not only in the cap-binding pocket but also in a distant region of the 4E-BP/eIF4G binding site. Formation of the complex with 7-methyl-GTP makes the eIF4E structure more compact, while binding of N (2), N (2),7-trimethyl-GTP leads to higher solvent accessibility of the protein backbone in comparison with the apo form. The results suggest that the additional double methylation at the N (2)-amino group of the cap causes sterical effects upon binding to mammalian eIF4E which influence the overall solution dynamics of the protein, thus precluding formation of a tight complex.

  9. Synthesis, physical and chemical properties of 2-((5-(hydroxy(phenylmethyl-4R-4H-1,2,4-triazole-3-ylthioacetic acids and its salts

    Directory of Open Access Journals (Sweden)

    A. M. Rud

    2018-02-01

    Full Text Available Today’s a creation of new domestic medicines is very important problem for pharmacy and medicine. Therefore, it is relevant to synthesize new domestic biologically active compounds. It is known that a large number of new 3-thio and 4-amino derivatives on the basis of 1,2,4-triazole have recently been synthesized, among which compounds with high pharmacological activity have been found. Based on the experience of previous studies and with the aim of creating new original drugs, our goal was to synthesize 2-((5-(hydroxy(phenylmethyl-4-R-4H-1,2,4-triazole-3-ylthioacetic acids series and to obtain salts on its basis, which have high indicators of pharmacological activity based on the literature data. The goal of the work is a targeted synthesis of potential low-toxic and highly effective compounds with a wide spectrum of pharmacological activity among 5-(hydroxy(phenylmethyl-4-R-4H-1,2,4-triazole-3-thione derivatives, confirmation of their individuality and structure, as well as the study of physical-chemical properties, for the further pharmacological screening. Materials and methods. 2-((5-(hydroxy(phenylmethyl-4-R-4H-1,2,4-triazole-3-ylthioacetic acids were prepared by heating 5- (hydroxy(phenylmethyl-4-R-4H-1,2,4-triazol-3-thiones with chloroacetic acid. Subsequently, the synthesized thioacetic acids were subject for modification. Salts of 2-((5-(hydroxy(phenylmethyl-4-R-4H-1,2,4-triazole-3-ylthioacetic acids were obtained by reacting thioacetic acids with equivalents of sodium or potassium hydroxides. To obtain Iron(II, Copper(II or Zinc(II salts, half-molar amounts of the appropriate sulfates were added to the obtained solutions. Salts of 2-((5-(hydroxy(phenylmethyl-4-R-4H-1,2,4-triazole-3-ylthioacetic acids with organic bases were obtained by the reaction of acids with piperidine or morpholine in ethanol medium. Results. During the synthetic studies, 13 previously undescribed new compounds were obtained. The individuality of 2-((5-(hydroxy

  10. Progesterone metabolism by the hypothalamus, pituitary, and uterus of the rat during pregnancy

    International Nuclear Information System (INIS)

    Marrone, B.L.; Karavolas, H.J.

    1981-01-01

    Metabolites of [ 3 H]progesterone were quantitated from incubations of hypothalamus, pituitary, and uterus of rats during different stages of pregnancy. The hypothalamus, anterior pituitary, and a section of uterus from five rats on Days 1, 8, 15, and 21 of pregnancy were incubated individually with [3H]progesterone and analyzed for metabolite formation by reverse isotopic dilution analysis. The radioactive metabolites present were 5 alpha-pregnane-3,20-dione (5 alpha-DHP), 3 alpha-hydroxy-5 alpha-pregnan-20-one, 20 alpha-hydroxy-4-pregnen-3-one, 20 alpha-hydroxy-5 alpha-pregnan-3-one, and 5 alpha-pregnane-3 alpha, 20 alpha-diol. The major metabolite formed by the hypothalamus and pituitary was 5 alpha-DHP. In the pituitary samples, formation of 5 alpha-DHP was decreased on Days 15 and 21 of pregnancy compared to Day 1, and formation of 20 alpha-hydroxy-5 alpha-pregnan-3-one was decreased on Day 21 compared to Day 1. In the uterine samples, 3 alpha-hydroxy-5 alpha-pregnan-20-one was the major metabolite formed at all stages of pregnancy. The formation of all metabolic products of progesterone by the uterus was increased on Day 21 compared to Days 1, 8, and 15 of pregnancy. No changes in the formation of progesterone metabolites were observed in the hypothalamic samples during pregnancy. It is concluded that there are different profiles in the in vitro metabolism of [3H]progesterone by the hypothalamus, pituitary, and uterus of the rat during the course of pregnancy

  11. Mass-fragmentographic determination of 25-hydroxy-vitamin D3 using deuterium labeled internal standard

    International Nuclear Information System (INIS)

    Bjorkhem, I.; Holmberg, I.

    1975-01-01

    25-[26- 2 H 3 ] Hydroxy-vitamin D 3 has been synthesized according to the following route: 3β-acetoxy-27-nor-cholest-5-en-25-one → 3β-acetoxy-27-nor-cholesta-5,7-dien-25-one → [26- 2 H 3 ] cholesta-5,7-diene-3β,25-diol → 25-[26- 2 H 3 ] hydroxy-vitamin D 3 . A fixed amount of 25-[26- 2 H 3 ] hydroxy-vitamin D 3 , usually 250 ng, is added to a fixed amount of serum, usually 2.5 ml, and the mixture is extracted with a chloroform-methanol mixture. The extract is chromatographed on a Sephadex LH-20 column together with a trace amount of 25-[26- 3 H] hydroxy-vitamin D 3 . The chromatographic fraction corresponding to 25-hydroxy-vitamin D 3 is collected and the amount of unlabeled 25-hydroxy-vitamin D 3 is determined from the ratio between the mass fragmentographic recording of m/e 131 (base peak of unlabeled 25-hydroxy-vitamin D 3 ) and m/e 134 (base peak of 25-[26- 2 H 3 ] hydroxy-vitamin D 3 ). The relative standard deviation of the method was about 5%. The mean value for 25-hydroxy-vitamin D 3 obtained from 23 different serum samples from healthy Swedish men and women was 27 ng/ml with a standard deviation of 10 ng/ml

  12. Levels of /sup 209/Tl and /sup 211/Pb populated in the /sup 210/Pb(t,. cap alpha. )/sup 209/Tl and /sup 210/Pb(t,d)/sup 211/Pb reactions. [J,. pi.

    Energy Technology Data Exchange (ETDEWEB)

    Ellegaard, C; Barnes, P D [Carnegie-Mellon Univ., Pittsburgh, Pa. (USA); Flynn, E R [Los Alamos Scientific Lab., N.Mex. (USA)

    1976-03-22

    The reactions /sup 210/Pb(t,..cap alpha..)/sup 209/Tl and /sup 210/Pb(t,d)/sup 211/Pb have been studied with 20 MeV tritons. Seven levels in /sup 209/Tl have been identified in the /sup 210/Pb(t,..cap alpha..)/sup 209/Tl reaction. Level spins have been suggested by comparing the observed spectrum with that of the corresponding reaction on /sup 208/Pb. Nineteen levels in /sup 211/Pb were identified in the /sup 210/Pb(t,d)/sup 211/Pb reaction. Angular distributions were measured and lsub(n) values and spectroscopic factors were extracted by DWBA calculations. In both cases the spectra are very similar to the spectra obtained with /sup 208/Pb as a target. The deviations from these simple spectra would appear to be amenable to a description in terms of a coupling of the extra particle or hole to the /sup 210/Pb core.

  13. Detection of stable isotopes with a (n,. cap alpha. ) nuclear reaction: application to the measurement of unidirectional fluxes of borate in a plant

    Energy Technology Data Exchange (ETDEWEB)

    Duval, Y; Thellier, M; Heurteaux, C; Wissocq, J C [Centre National de la Recherche Scientifique, Mont-Saint-Aignan (France). Lab. ' ' Echanges cellulaires' '

    1980-01-01

    The unidirectional influx of borate has been studied in Lemna minor plants with the aid of purified boron isotopes, /sup 10/B and /sup 11/B. Isotope /sup 10/B was detected specifically by nuclear reaction /sup 10/B(n, ..cap alpha..)/sup 7/Li in the presence of ''homogeneous'' detectors. Despite technical difficulties in performing the /sup 10/B-estimations in the plant samples themselves, the results obtained here were consistent with those of efflux experiments, published previously, where the /sup 10/B-measurements were performed in the external solution. Kinetic parameters of borate transports in Lemna minor have been calculated.

  14. /sup 15/N(p,. cap alpha. )/sup 12/C reaction with polarized protons from 0. 34 to 1. 21 MeV

    Energy Technology Data Exchange (ETDEWEB)

    Pepper, G H; Brown, L [Carnegie Institution of Washington, D.C. (USA). Dept. of Terrestrial Magnetism

    1976-03-29

    A polarized beam was used to measure angular distributions of the analyzing power of the /sup 15/N(p,..cap alpha..)/sup 12/C reaction at 0.34 MeV and at five energies from 0.92 to 1.21 MeV. The analyzing power can be fitted with associated Legendre polynomials, P/sub 1//sup 1/ and P/sub 2//sup 1/ sufficing to describe the results except near 1.2 MeV where P/sub 3//sup 1/ is also required. Polarization excitation functions were measured throughout the entire energy range at angles where the polynomials P/sub 2//sup 1/ and P/sub 3//sup 1/ are zero. A polarization contour map is given.

  15. Evidence that steroid 5alpha-reductase isozyme genes are differentially methylated in human lymphocytes.

    Science.gov (United States)

    Rodríguez-Dorantes, M; Lizano-Soberón, M; Camacho-Arroyo, I; Calzada-León, R; Morimoto, S; Téllez-Ascencio, N; Cerbón, M A

    2002-03-01

    The synthesis of dihydrotestosterone (DHT) is catalyzed by steroid 5alpha-reductase isozymes 1 and 2, and this function determines the development of the male phenotype during embriogenesis and the growth of androgen sensitive tissues during puberty. The aim of this study was to determine the cytosine methylation status of 5alpha-reductase isozymes types 1 and 2 genes in normal and in 5alpha-reductase deficient men. Genomic DNA was obtained from lymphocytes of both normal subjects and patients with primary 5alpha-reductase deficiency due to point mutations in 5alpha-reductase 2 gene. Southern blot analysis of 5alpha-reductase types 1 and 2 genes from DNA samples digested with HpaII presented a different cytosine methylation pattern compared to that observed with its isoschizomer MspI, indicating that both genes are methylated in CCGG sequences. The analysis of 5alpha-reductase 1 gene from DNA samples digested with Sau3AI and its isoschizomer MboI which recognize methylation in GATC sequences showed an identical methylation pattern. In contrast, 5alpha-reductase 2 gene digested with Sau3AI presented a different methylation pattern to that of the samples digested with MboI, indicating that steroid 5alpha-reductase 2 gene possess methylated cytosines in GATC sequences. Analysis of exon 4 of 5alpha-reductase 2 gene after metabisulfite PCR showed that normal and deficient subjects present a different methylation pattern, being more methylated in patients with 5alpha-reductase 2 mutated gene. The overall results suggest that 5alpha-reductase genes 1 and 2 are differentially methylated in lymphocytes from normal and 5alpha-reductase deficient patients. Moreover, the extensive cytosine methylation pattern observed in exon 4 of 5alpha-reductase 2 gene in deficient patients, points out to an increased rate of mutations in this gene.

  16. Modifying the 5'-Cap for Click Reactions of Eukaryotic mRNA and To Tune Translation Efficiency in Living Cells.

    Science.gov (United States)

    Holstein, Josephin M; Anhäuser, Lea; Rentmeister, Andrea

    2016-08-26

    The 5'-cap is a hallmark of eukaryotic mRNAs and plays fundamental roles in RNA metabolism, ranging from quality control to export and translation. Modifying the 5'-cap may thus enable modulation of the underlying processes and investigation or tuning of several biological functions. A straightforward approach is presented for the efficient production of a range of N7-modified caps based on the highly promiscuous methyltransferase Ecm1. We show that these, as well as N(2) -modified 5'-caps, can be used to tune translation of the respective mRNAs both in vitro and in cells. Appropriate modifications allow subsequent bioorthogonal chemistry, as demonstrated by intracellular live-cell labeling of a target mRNA. The efficient and versatile N7 manipulation of the mRNA cap makes mRNAs amenable to both modulation of their biological function and intracellular labeling, and represents a valuable addition to the chemical biology toolbox. © 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  17. 5'-Phospho-RNA Acceptor Specificity of GDP Polyribonucleotidyltransferase of Vesicular Stomatitis Virus in mRNA Capping.

    Science.gov (United States)

    Ogino, Minako; Ogino, Tomoaki

    2017-03-15

    The GDP polyribonucleotidyltransferase (PRNTase) domain of the multifunctional L protein of rhabdoviruses, such as vesicular stomatitis virus (VSV) and rabies virus, catalyzes the transfer of 5'-phospho-RNA (pRNA) from 5'-triphospho-RNA (pppRNA) to GDP via a covalent enzyme-pRNA intermediate to generate a 5'-cap structure (GpppA). Here, using an improved oligo-RNA capping assay with the VSV L protein, we showed that the Michaelis constants for GDP and pppAACAG (VSV mRNA-start sequence) are 0.03 and 0.4 μM, respectively. A competition assay between GDP and GDP analogues in the GpppA formation and pRNA transfer assay using GDP analogues as pRNA acceptors indicated that the PRNTase domain recognizes the C-2-amino group, but not the C-6-oxo group, N-1-hydrogen, or N-7-nitrogen, of GDP for the cap formation. 2,6-Diaminopurine-riboside (DAP), 7-deazaguanosine (7-deaza-G), and 7-methylguanosine (m 7 G) diphosphates efficiently accepted pRNA, resulting in the formation of DAPpppA, 7-deaza-GpppA, and m 7 GpppA (cap 0), respectively. Furthermore, either the 2'- or 3'-hydroxyl group of GDP was found to be required for efficient pRNA transfer. A 5'-diphosphate form of antiviral ribavirin weakly inhibited the GpppA formation but did not act as a pRNA acceptor. These results indicate that the PRNTase domain has a unique guanosine-binding mode different from that of eukaryotic mRNA capping enzyme, guanylyltransferase. IMPORTANCE mRNAs of nonsegmented negative-strand (NNS) RNA viruses, such as VSV, possess a fully methylated cap structure, which is required for mRNA stability, efficient translation, and evasion of antiviral innate immunity in host cells. GDP polyribonucleotidyltransferase (PRNTase) is an unconventional mRNA capping enzyme of NNS RNA viruses that is distinct from the eukaryotic mRNA capping enzyme, guanylyltransferase. In this study, we studied the pRNA acceptor specificity of VSV PRNTase using various GDP analogues and identified chemical groups of GDP as

  18. Synthesis of specifically deuterium-labelled pregnanolone and pregnanediol sulphates for metabolic studies in humans.

    Science.gov (United States)

    Baillie, T A; Sjövall, J; Herz, J E

    1975-10-01

    A synthesis is reported of 3beta-hydroxy-5alpha-pregnan-20-one sulphate and the disulphate and 3-monosulphate of 5alpha-pregnane-3beta,20alpha-diol, labelled specifically with deuterium in high isotopic purity for metabolic studies in humans. Base-catalyzed equilibration of 3beta-hydroxy-5alpha-25R-spirostan-12-one (hemcogenin, II) with deuterium oxide, followed by removal of the 12-keto group and degradation of the sapogenin side-chain afforded 3beta-hydroxy-5alpha-[11,11-2H2]pregn-16-en-20-one (VII). Further deuterium atoms were introduced at the 3alpha and 20beta positions by reductions with sodium borodeuteride and lithium aluminum deuteride, respectively. These reactions led to 3beta-hydroxy-5alpha-[3alpha,11,11-2H3]pregnan-20-one (X; isotopic purity 87.2%) and 5alpha-[3alpha,11,11,20beta-2H4]pregnane-3beta,20alpha-diol (XIV; isotopic purity 83.9%). The 3-sulphate of the pregnanolone and the 3,20-disulphate of the pregnanediol were prepared directly form the free alcohols, while the 3-monosulphate of the pregnanediol was obtained via 5alpha-[3alpha,11,11,20beta-2H4]pregnane-3beta,20alpha-diol 20-acetate (XVII).

  19. Influence of the. cap alpha. -,. beta. -, and. gamma. -subunits of the energy-transducing adenosine triphosphatase from Micrococcus lysodeikticus in the immunochemical properties of the protein and in their reconstitution studied by a radioimmunoassay method

    Energy Technology Data Exchange (ETDEWEB)

    Larraga, V; Mollinedo, F; Rubio, N; Munoz, E [Unidad de Biomembranas, Instituto de Inmunologia y Biologia Microbiana, Madrid (Spain)

    1981-03-01

    A sensitive radioimmunoassay was developed for the energy-transducing adenosine triphosphatase (F/sub 1/-ATPase, EC 3.6.1.3) of Micrococcus lysodeikticus and the assay was extended to the ..cap alpha..-, ..beta..-, and ..gamma..-subunits of the enzyme. These subunits were isolated and cross-reactions studied.

  20. Identification of 4,5-didemethyl-4-O-alpha-D-glucopyranosylsimmondsin and pinitol alpha-D-galactosides in jojoba seed meal (Simmondsia chinensis).

    Science.gov (United States)

    Van Boven, M; Leyssen, T; Busson, R; Holser, R; Cokelaere, M; Flo, G; Decuypere, E

    2001-09-01

    The isolation and identification of two pinitol alpha-D-galactosides from jojoba meal are described. The products were isolated by a combination of preparative HPLC on silica gel and TLC on amino silica gel and were identified by MS, NMR spectroscopy, and chemical derivatization as 5-O-(alpha-D-galactopyranosyl)-3-O-methyl-D-chiro-inositol or 5-alpha-D-galactopyranosyl-D-pinitol and 2-O-(alpha-D-galactopyranosyl)-3-O-methyl-D-chiro-inositol or 2-alpha-D-galactopyranosyl-D-pinitol. The same preparative HPLC method on silica gel allowed a new simmondsin derivative to be isolated and identified as 4,5-didemethyl-4-O-alpha-D-glucopyranosylsimmondsin mainly by NMR spectroscopy and high-resolution mass spectrometry.

  1. Natural 4-hydroxy-2,5-dimethyl-3(2H)-furanone (Furaneol®).

    Science.gov (United States)

    Schwab, Wilfried

    2013-06-13

    4-Hydroxy-2,5-dimethyl-3(2H)-furanone (HDMF, furaneol®) and its methyl ether 2,5-dimethyl-4-methoxy-3(2H)-furanone (DMMF) are import aroma chemicals and are considered key flavor compounds in many fruit. Due to their attractive sensory properties they are highly appreciated by the food industry. In fruits 2,5-dimethyl-3(2H)-furanones are synthesized by a series of enzymatic steps whereas HDMF is also a product of the Maillard reaction. Numerous methods for the synthetic preparation of these compounds have been published and are applied by industry, but for the development of a biotechnological process the knowledge and availability of biosynthetic enzymes are required. During the last years substantial progress has been made in the elucidation of the biological pathway leading to HDMF and DMMF. This review summarizes the latest advances in this field.

  2. Natural 4-Hydroxy-2,5-dimethyl-3(2H-furanone (Furaneol®

    Directory of Open Access Journals (Sweden)

    Wilfried Schwab

    2013-06-01

    Full Text Available 4-Hydroxy-2,5-dimethyl-3(2H-furanone (HDMF, furaneol® and its methyl ether 2,5-dimethyl-4-methoxy-3(2H-furanone (DMMF are import aroma chemicals and are considered key flavor compounds in many fruit. Due to their attractive sensory properties they are highly appreciated by the food industry. In fruits 2,5-dimethyl-3(2H-furanones are synthesized by a series of enzymatic steps whereas HDMF is also a product of the Maillard reaction. Numerous methods for the synthetic preparation of these compounds have been published and are applied by industry, but for the development of a biotechnological process the knowledge and availability of biosynthetic enzymes are required. During the last years substantial progress has been made in the elucidation of the biological pathway leading to HDMF and DMMF. This review summarizes the latest advances in this field.

  3. Improved Synthesis of 2',6'-Dihydroxy-3,4-dimethoxy Chalcone by Grinding Technique to Synthesize 5-Hydroxy-3',4'-dimethoxy Flavone

    Directory of Open Access Journals (Sweden)

    Elfi Susanti VH

    2014-07-01

    Full Text Available 5-hydroxy-3',4'-dimethoxy flavone can be efficiently synthesized in two steps via the formation of 2',6'-dihydroxy-3,4-dimethoxy chalcone with good results. 2',6'-dihydroxy-3,4-dimethoxy chalcone as reactants for synthesis of flavones was prepared through Claisen-Schmidt condensation reaction between 2,6-dihydroxyacetophenones,3,4-dimethoxybenzaldehyde and solid NaOH in mortar for 15 min. The yield of the product (70% is higher than conventional method (65%. This chalcone then oxidatively cyclized with iodine to form 5-hydroxy-3',4'-dimethoxy flavone (yield 62%. Compounds synthesized were characterized by spectroscopic (IR, 1H-NMR, and 13C-NMR.

  4. Application of stable isotope ratio analysis explaining the bioformation of 2,5-dimethyl-4-hydroxy-3(2H)-furanone in plants by a biological Maillard reaction

    International Nuclear Information System (INIS)

    Schwab, W.

    1998-01-01

    [1-13C]-D-Fructose and [U-13C6]-D-fructose were applied to detached ripening strawberry fruits, and the incorporation into 2,5-dimethyl-4-hydroxy-3(2H)-furanone 1, 2,5-dimethyl-4-methoxy-3(2H)-furanone 2, 2,5-dimethyl-4-acetoxy-3(2H)-furanone 3, 2,5-dimethyl-4-hydroxy-3(2H)-furanone beta-D-glucopyranoside 4, and 2,5-dimethyl-4-hydroxy-3(2H)-furanone 6'-O-malonyl beta-D-glucopyranoside 5 was determined by HRGC-MS and HPLC-ESI MS-MS. The data clearly showed the direct conversion of D-fructose to the furanones without cleavage of the carbohydrate prior to the formation of 1-5, as expected for a biological Maillard reaction. Both, the furanone and the D-glucose moiety of 4 and 5 contained the labels. However, the label was primarily incorporated into the furanone moiety, indicating that D-fructose is a more efficient precursor of the furanones than D-glucose

  5. ANTI-ALLERGIC EFFECTS OF 1,5-BIS(4’-HYDROXY-3’-METHOXYPHENYL-1,4-PENTADIENE-3-ONE ON MAST CELL-MEDIATED ALLERGY MODEL

    Directory of Open Access Journals (Sweden)

    AGUNG ENDRO NUGROHO

    2009-01-01

    Full Text Available 1,5-bis(4’-hydroxy-3’-methoxyphenyl-1,4-pentadiene-3-one is a 1,5-diphenyl-1,4-pentadiene-3-one analogue of curcumin that is produced by modifying the middle site of curcumin leading to 1,4-pentadiene-3-ones to maintain the hydroxy moiety at the aromatic rings that are responsible for its biological activities. Curcumin has been reported to have anti-allergic effects and can inhibit the release of histamine from mast cells. In the present study, we evaluated the anti-allergic effects of 1,5-bis(4’-hydroxy-3’-methoxyphenyl-1,4-pentadiene-3-one in a mast cell-mediated allergy mode in order to provide information about a newly synthesised-compound for an alternative allergy drug. The study was performed using (1 a rat basophilic leukaemia (RBL-2H3 cell line, which is a tumour analogue of mast cells, with DNP24-BSA, thapsigargin and ionomycin as inducers for secretory markers from mast cells, and (2 an active cutaneous anaphylaxis (ACA reaction, with ovalbumin as an inductor of mast cell degranulation. Treatment with 1,5-bis(4’-hydroxy-3’-methoxyphenyl-1,4-pentadiene-3-one strongly inhibited the DNP24-BSA, thapsigargin and ionomycin-mediated release of histamine and β-hexosaminidase from the RBL-2H3 cell line. The results indicated that this compound influenced the activation processes of FcεRI by antigen and intracellular Ca2+ signalling events in mast cells. In type 1 allergy model, this compound also inhibited the active cutaneous anaphylactic reaction on rat dorsal skins generated by ovalbumin. We conclude that the compound 1,5-bis(4’-hydroxy-3’-methoxyphenyl-1,4-pentadiene-3-one showed anti-allergic activities mediated by mechanisms related to intracellular signalling events in mast cells.

  6. 5,7-dihydroxy-2-(3-hydroxy-4, 5-dimethoxy-phenyl)-chromen-4-one-a flavone from Bruguiera gymnorrhiza displaying anti-inflammatory properties.

    Science.gov (United States)

    Barik, Rajib; Sarkar, Ratul; Biswas, Prova; Bera, Rammohan; Sharma, Soma; Nath, Suvadeep; Karmakar, Sanmoy; Sen, Tuhinadri

    2016-01-01

    Bruguiera gymnorrhiza (BRG) (L.) Lamk (Rhizophoraceae), a mangrove species, is widely distributed in the Pacific region, eastern Africa, Indian subcontinent, and subtropical Australia. The leaves of this plant are traditionally used for treating burns and inflammatory lesions. This study isolates the bioactive compound from the methanol extract of BRG leaves and evaluates the possible mechanisms of anti-inflammatory activity involved. Bioassay-guided fractionation of BRG was performed to identify the bioactive fraction (displaying inhibition of cyclooxygenase 2 [COX2] - 5-lipoxygenase (5-LOX) activities and tumor necrosis factor-alpha (TNF-α) production at the tested concentrations of 100 and 10 μg/ml). The fractionation was performed by solvent extraction and preparative high-performance liquid chromatography. The bioactive compound was characterized by ultraviolet-visible, liquid chromatography-mass spectrometry and nuclear magnetic resonance spectroscopy. The antioxidant potential was evaluated by electron spin resonance spectrum of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical at 250 μM. The effect of the compound was also studied on TNF-α converting enzyme and nuclear factor kappa B (NF-κB) activities at the concentrations 100, 10 and 1 μg/ml. Bioassay-guided purification of BRG revealed the presence of a flavone (5,7-dihydroxy-2- [3-hydroxy-4,5-dimethoxy-phenyl]-chromen-4-one) of molecular weight 330Da. It demonstrated more than 80% inhibition against COX2, 5-LOX activities and TNF-α production at 100 μg/ml. It also displayed 40% inhibition against DPPH radical at the tested concentration along with 23.1% inhibition of NF-κB activity at 100 μg/ml. The isolated methoxy-flavone may play a predominant role in the anti-inflammatory properties displayed by BRG leaves. Such activity may involve multiple mechanisms, namely (a) modulation of oxidative stress (b) inhibition of arachidonic acid metabolism and (c) downregulation of pro-inflammatory cytokines

  7. Practical synthesis of methyl 7-(3-hydroxy-5-oxocyclopent-1-en-1-yl-heptanoate

    Directory of Open Access Journals (Sweden)

    Xinpeng Jiang

    2017-07-01

    Full Text Available The key intermediate of misoprostol, methyl 7-(3-hydroxy-5-oxocyclopent-1-en-1-yl-heptanoate was prepared from commercially available suberic acid in 40% yield over five steps. The key step involved a ZnCl2 catalyzed Friedel-Crafts reaction between furan and 2,9-oxonanedione. Sulfuric acid catalyzed methylation of 8-(furan-2-yl-8-oxooctanoic acid followed by sequential reduction and ZnCl2 catalyzed Piancatelli rearrangement resulted in the formation of the key intermediate of misoprostol.

  8. N-{(2S-3-Hydroxy-4-[(5-methyl-1,3,4-thiadiazol-2-ylsulfanyl]-1-phenyl-2-butyl}-4-methylbenzenesulfonamide

    Directory of Open Access Journals (Sweden)

    Claudia R. B. Gomes

    2011-09-01

    Full Text Available The thiadiazoyl and sulfonyl-benzene rings in the title compound, C20H23N3O3S3, are aligned to the same side of the molecule, forming a twisted `U' shape [dihedral angle = 77.6 (5°]. The benzyl-benzene ring is orientated in the opposite direction from the molecule but projects approximately along the same axis as the other rings [dihedral angle between benzene rings = 28.2 (5°] so that, overall, the molecule has a flattened shape. The hydroxy and amine groups are almost syn which enables the formation of intermolecular hydroxy-OH...N(thiadiazoyl and amine-H...O(sulfonyl hydrogen bonds leading to a supramolecular chain aligned along the a axis.

  9. Inhibition of translation by 7-methyl guanosine (m7G) nucleotide cap analogs with derivatized 5'-monophosphates

    International Nuclear Information System (INIS)

    Tahara, S.M.; Darzynkiewicz, E.; Ekiel, I.

    1986-01-01

    Recognition of the 5'-m 7 GpppN (cap) structure of eukaryote mRNA is an important step of translation initiation as shown by the potent inhibitory effect of m 7 G nucleotides on this process. A comparison of cap analogs as competitive inhibitors of initiation has allowed the authors to map probable protein-ligand contact points between the cap and cognate cap binding proteins (CBPs). Recently, several new derivatives of m 7 GMP (1) with modified phosphates were synthesized: m 7 G 5'-phosphite (2), m 7 G 5'-phosphoramidate (3), m 7 G 5'-methylphosphonate (4), and m 7 G 5'-phosphate-O-methyl ester (5). In addition, 7,8-dimethyl GMP (6) and 7-methyl 8-amino GMP (7) were synthesized. 6 and7 are primarily syn and anti respectively, relative to the glycosidic bond as shown by solution NMR studies. Inhibition by analogs on total translation in reticulocyte lysate and binding of mRNA to rabbit reticulocyte ribosomes was found to be: 1 = 3 > 5 > 4 > 2. The inhibitory activity of 3 was unexpected since it is isosteric with 4, however it suggested that electron configuration and/or the ability to form a hydrogen bond between protein and the phosphate moiety might be important for ligand binding. 7 was more inhibitory than 6. The latter two are isosteric therefore differences in electron delocalization and/or syn-anti conformation are likely to be the reason(s) for the observed difference

  10. Structural basis for the enzymatic formation of the key strawberry flavor compound 4-hydroxy-2,5-dimethyl-3(2H)-furanone.

    Science.gov (United States)

    Schiefner, André; Sinz, Quirin; Neumaier, Irmgard; Schwab, Wilfried; Skerra, Arne

    2013-06-07

    The last step in the biosynthetic route to the key strawberry flavor compound 4-hydroxy-2,5-dimethyl-3(2H)-furanone (HDMF) is catalyzed by Fragaria x ananassa enone oxidoreductase (FaEO), earlier putatively assigned as quinone oxidoreductase (FaQR). The ripening-induced enzyme catalyzes the reduction of the exocyclic double bond of the highly reactive precursor 4-hydroxy-5-methyl-2-methylene-3(2H)-furanone (HMMF) in a NAD(P)H-dependent manner. To elucidate the molecular mechanism of this peculiar reaction, we determined the crystal structure of FaEO in six different states or complexes at resolutions of ≤1.6 Å, including those with HDMF as well as three distinct substrate analogs. Our crystallographic analysis revealed a monomeric enzyme whose active site is largely determined by the bound NAD(P)H cofactor, which is embedded in a Rossmann-fold. Considering that the quasi-symmetric enolic reaction product HDMF is prone to extensive tautomerization, whereas its precursor HMMF is chemically labile in aqueous solution, we used the asymmetric and more stable surrogate product 2-ethyl-4-hydroxy-5-methyl-3(2H)-furanone (EHMF) and the corresponding substrate (2E)-ethylidene-4-hydroxy-5-methyl-3(2H)-furanone (EDHMF) to study their enzyme complexes as well. Together with deuterium-labeling experiments of EDHMF reduction by [4R-(2)H]NADH and chiral-phase analysis of the reaction product EHMF, our data show that the 4R-hydride of NAD(P)H is transferred to the unsaturated exocyclic C6 carbon of HMMF, resulting in a cyclic achiral enolate intermediate that subsequently becomes protonated, eventually leading to HDMF. Apart from elucidating this important reaction of the plant secondary metabolism our study provides a foundation for protein engineering of enone oxidoreductases and their application in biocatalytic processes.

  11. Imaging of alpha(v)beta(3) expression by a bifunctional chimeric RGD peptide not cross-reacting with alpha(v)beta(5).

    Science.gov (United States)

    Zannetti, Antonella; Del Vecchio, Silvana; Iommelli, Francesca; Del Gatto, Annarita; De Luca, Stefania; Zaccaro, Laura; Papaccioli, Angela; Sommella, Jvana; Panico, Mariarosaria; Speranza, Antonio; Grieco, Paolo; Novellino, Ettore; Saviano, Michele; Pedone, Carlo; Salvatore, Marco

    2009-08-15

    To test whether a novel bifunctional chimeric peptide comprising a cyclic Arg-Gly-Asp pentapeptide covalently bound to an echistatin domain can discriminate alpha(v)beta(3) from alpha(v)beta(5) integrin, thus allowing the in vivo selective visualization of alpha(v)beta(3) expression by single-photon and positron emission tomography (PET) imaging. The chimeric peptide was preliminarily tested for inhibition of alpha(v)beta(3)-dependent cell adhesion and competition of 125I-echistatin binding to membrane of stably transfected K562 cells expressing alpha(v)beta(3) (Kalpha(v)beta(3)) or alpha(v)beta(5) (Kalpha(v)beta(5)) integrin. The chimeric peptide was then conjugated with diethylenetriaminepentaacetic acid and labeled with 111In for single-photon imaging, whereas a one-step procedure was used for labeling the full-length peptide and a truncated derivative, lacking the last five C-terminal amino acids, with 18F for PET imaging. Nude mice bearing tumors from Kalpha(v)beta(3), Kalpha(v)beta(5), U87MG human glioblastoma, and A431 human epidermoid cells were subjected to single-photon and PET imaging. Adhesion and competitive binding assays showed that the novel chimeric peptide selectively binds to alpha(v)beta(3) integrin and does not cross-react with alpha(v)beta(5). In agreement with in vitro findings, single-photon and PET imaging studies showed that the radiolabeled chimeric peptide selectively localizes in tumor xenografts expressing alphavbeta3 and fails to accumulate in those expressing alpha(v)beta(5) integrin. When 18F-labeled truncated derivative was used for PET imaging, alphavbeta3- and alpha(v)beta(5)-expressing tumors were visualized, indicating that the five C-terminal amino acids are required to differentially bind the two integrins. Our findings indicate that the novel chimeric Arg-Gly-Asp peptide, having no cross-reaction with alphavbeta5 integrin, allows highly selective alphavbeta3 expression imaging and monitoring.

  12. Monoclonal antibodies for use in an immunoradiometric assay for. cap alpha. -foetoprotein

    Energy Technology Data Exchange (ETDEWEB)

    Hunter, W.M.; Bennie, J.G. (Medical Research Council, Edinburgh (UK). Immunoassay Team); Brock, D.J.H.; Heyningen, V. van (Western General Hospital, Edinburgh (UK))

    1982-04-29

    The advantages offered by a mouse IgG/sub 1/ monoclonal antibody to human ..cap alpha..-foetoprotein (AFP) for the preparation of (/sup 125/I)antibody for use in an immunoradiometric assay (IRMA) have been investigated. The antibody was isolated from ascites fluid by sodium sulphate precipitation followed by gel filtration on Sephadex G-200. The freeze-dried powder and solutions thereof were stable and were used for iodination to 1 atom /sup 125/I/molecule antibody by the chloramine-T procedure. At high antigen concentrations 70-80% of the added (/sup 125/)Ab was present in the sandwich. Linear response curves in the range 1-100 ..mu..g antigen/l incubate were obtained when (/sup 125/I)Ab was in slight excess. In this region an Ag : Ab ratio 1.9 : 1 was obtained which is consistent with the saturation of a bifunctional antibody. Although non-specific binding (in the absence of antigen) was consistently <0.1% of added (/sup 125/I)Ab, this was the main factor in determining assay detection limits. The serum AFP levels from both non-pregnant and pregnant subjects as measured by the IRMA using the (/sup 125/I)monoclonal Ab and by radioimmunoassay (RIA) using a sheep antiserum to AFP were in excellent agreement. The IRMA was manipulatively simple, employed a shorter incubation time (2h), required shorter counting times than the RIA and gave a much wider working range. The provision of a monoclonal antibody for labelling removes the one major practicability barrier which otherwise limits the development and use of the potentially superior IRMA system.

  13. Long-term treatment with calcium-alpha-ketoglutarate corrects secondary hyperparathyroidism.

    Science.gov (United States)

    Zimmermann, E; Wassmer, S; Steudle, V

    1996-01-01

    Calcium-alpha-ketoglutarate (Ca-ket) is known as a highly effective phosphate (P) binder in hemodialysis (HD) patients. In addition, alpha-ketoglutarate has been shown to improve metabolic alterations. We investigated the effect of long-term P-binding therapy with Ca-ket to determine whether P accumulation is the main reason of secondary hyperparathyroidism (HPT) in HD patients or not. Ca-ket was prescribed to 14 HD patients as a soluble preparation in a mean dosage of 4.5 g/day (0.975 g elemental Ca) for a period of 36 months. Serum P continuously dropped from prestudy 2.6 +/- 0.1 (mean +/- SEM) to 1.9 +/- 0.07 mmol/l (p < 0.001), whereas serum Ca increased from 2.2 +/- 0.1 to 2.47 +/- 0.08 mmol/l (p < 0.05). Thus, Ca/P ratio in serum converted significantly from 0.91 +/- 0.02 (prestudy) to 1.28 +/- 0.01 (p < 0.001). Intact parathyroid hormone (iPTH) continuously normalized in all patients from 29 +/- 5 to 8 +/- 2 pmol/l (p < 0.001). The present data show that long-term treatment with Ca-ket normalizes secondary HPT by simultaneously P binding and correcting Ca/P ratio in serum without vitamin D treatment.

  14. 5′-Phospho-RNA Acceptor Specificity of GDP Polyribonucleotidyltransferase of Vesicular Stomatitis Virus in mRNA Capping

    Science.gov (United States)

    Ogino, Minako

    2017-01-01

    ABSTRACT The GDP polyribonucleotidyltransferase (PRNTase) domain of the multifunctional L protein of rhabdoviruses, such as vesicular stomatitis virus (VSV) and rabies virus, catalyzes the transfer of 5′-phospho-RNA (pRNA) from 5′-triphospho-RNA (pppRNA) to GDP via a covalent enzyme-pRNA intermediate to generate a 5′-cap structure (GpppA). Here, using an improved oligo-RNA capping assay with the VSV L protein, we showed that the Michaelis constants for GDP and pppAACAG (VSV mRNA-start sequence) are 0.03 and 0.4 μM, respectively. A competition assay between GDP and GDP analogues in the GpppA formation and pRNA transfer assay using GDP analogues as pRNA acceptors indicated that the PRNTase domain recognizes the C-2-amino group, but not the C-6-oxo group, N-1-hydrogen, or N-7-nitrogen, of GDP for the cap formation. 2,6-Diaminopurine-riboside (DAP), 7-deazaguanosine (7-deaza-G), and 7-methylguanosine (m7G) diphosphates efficiently accepted pRNA, resulting in the formation of DAPpppA, 7-deaza-GpppA, and m7GpppA (cap 0), respectively. Furthermore, either the 2′- or 3′-hydroxyl group of GDP was found to be required for efficient pRNA transfer. A 5′-diphosphate form of antiviral ribavirin weakly inhibited the GpppA formation but did not act as a pRNA acceptor. These results indicate that the PRNTase domain has a unique guanosine-binding mode different from that of eukaryotic mRNA capping enzyme, guanylyltransferase. IMPORTANCE mRNAs of nonsegmented negative-strand (NNS) RNA viruses, such as VSV, possess a fully methylated cap structure, which is required for mRNA stability, efficient translation, and evasion of antiviral innate immunity in host cells. GDP polyribonucleotidyltransferase (PRNTase) is an unconventional mRNA capping enzyme of NNS RNA viruses that is distinct from the eukaryotic mRNA capping enzyme, guanylyltransferase. In this study, we studied the pRNA acceptor specificity of VSV PRNTase using various GDP analogues and identified chemical groups

  15. Photoaffinity labeling of steroid 5 alpha-reductase of rat liver and prostate microsomes

    International Nuclear Information System (INIS)

    Liang, T.; Cheung, A.H.; Reynolds, G.F.; Rasmusson, G.H.

    1985-01-01

    21-Diazo-4-methyl-4-aza-5 alpha-pregnane-3,20-dione (Diazo-MAPD) inhibits steroid 5 alpha-reductase in liver microsomes of female rats with a K/sub i/ value of 8.7 +/- 1.7 nM, and the inhibition is competitive with testosterone. It also inhibits the binding of a 5 alpha-reductase inhibitor, [ 3 H] 17 beta-N,N-diethylcarbamoyl-4-methyl-4-aza-5 alpha-androstan-3-one ([ 3 H]4-MA), to the enzyme in liver microsomes. The inhibition of 5 alpha-reductase activity and of inhibitor binding activity by diazo-MAPD becomes irreversible upon UV irradiation. [1,2- 3 H]Diazo-MAPD binds to a single high affinity site in liver microsomes of female rats, and this binding requires NADPH. Without UV irradiation, this binding is reversible, and it becomes irreversible upon UV irradiation. Both the initial reversible binding and the subsequent irreversible conjugation after UV irradiation are inhibited by inhibitors (diazo-MAPD and 4-MA) and substrates (progesterone and testosterone) of 5 alpha-reductase, but they are not inhibited by 5 alpha-reduced steroids. Photoaffinity labeled liver microsomes of female rats were solubilized and fractionated by high performance gel filtration. The radioactive conjugate eluted in one major peak at Mr 50,000

  16. Chemical Synthesis of a 5'-Terminal TMG-Capped Triribonucleotide m(3)(2,2,7)G(5)(')pppAmpUmpA of U1 RNA.

    Science.gov (United States)

    Sekine, Mitsuo; Kadokura, Michinori; Satoh, Takahiko; Seio, Kohji; Wada, Takeshi; Fischer, Utz; Sumpter, Vicki; Lührmann, Reinhard

    1996-06-26

    The 5'-terminal TMG-capped triribonucleotide, m(3)(2,2,7)G(5)(')pppAmpUmpA, has been synthesized by condensation of an appropriately protected triribonucleotide derivative of ppAmpUmpA with a new TMG-capping reagent. During this total synthesis, it was found that the regioselective 2'-O-methylation of 3',5'-O-(1,1,3,3-tetraisopropyldisiloxane-1,3-diyl)-N-(4-monomethoxytrityl)adenosine was achieved by use of MeI/Ag(2)O without affecting the base moiety. A new route to 2-N,2-N-dimethylguanosine from guanosine via a three-step reaction has also been developed by reductive methylation using paraformaldehyde and sodium cyanoborohydride. These key intermediates were used as starting materials for the construction of a fully protected derivative of pAmpUmpA and a TMG-capping reagent of Im-pm(3)(2,2,7)G. The target TMG-capped tetramer, m(3)(2,2,7)G(5)(')pppAmpUmpA, was synthesized by condensation of a partially protected triribonucleotide 5'-terminal diphosphate species, ppA(MMTr)mpUmpA, with Im-pm(3)(2,2,7)G followed by treatment with 80% acetic acid. The structure of m(3)(2,2,7)G(5)(')pppAmpUmpA was characterized by (1)H and (31)P NMR spectroscopy as well as enzymatic assay using snake venom phosphodiesterase, calf intestinal phosphatase, and nuclease P1.

  17. Alpha-interferon does not increase the efficacy of 5-fluorouracil in advanced colorectal cancer.

    LENUS (Irish Health Repository)

    Thirion, P

    2001-03-02

    Two meta-analyses were conducted to quantify the benefit of combining alpha-IFN to 5FU in advanced colorectal cancer in terms of tumour response and survival. Analyses were based on a total of 3254 individual patient data provided by principal investigators of each trial. The meta-analysis of 5FU +\\/- LV vs. 5FU +\\/- LV + alpha-IFN combined 12 trials and 1766 patients. The meta-analysis failed to show any statistically significant difference between the two treatment groups in terms of tumour response or survival. Overall tumour response rates were 25% for patients receiving no alpha-IFN vs. 24% for patients receiving alpha-IFN (relative risk, RR = 1.02), and median survivals were 11.4 months for patients receiving no alpha-IFN vs. 11.5 months for patients receiving alpha-IFN (hazard ratio, HR = 0.95). The meta-analysis of 5FU + LV vs. 5FU + alpha-IFN combined 7 trials, and 1488 patients. This meta-analysis showed an advantage for 5FU + LV over 5FU + alpha-IFN which was statistically significant in terms of tumour response (23% vs. 18%; RR = 1.26;P = 0.042), and of a borderline significance for overall survival (HR = 1.11;P = 0.066). Metastases confined to the liver and primary rectal tumours were independent favourable prognostic factors for tumour response, whereas good performance status, metastases confined to the liver or confined to the lung, and primary tumour in the rectum were independent favourable prognostic factors for survival. We conclude that alpha-IFN does not increase the efficacy of 5FU or of 5FU + LV, and that 5FU + alpha-IFN is significantly inferior to 5FU + LV, for patients with advanced colorectal cancer.

  18. Value of a radioimmunological monitoring in cancer patients treated with interferon alpha

    Energy Technology Data Exchange (ETDEWEB)

    Bernier, J.; Franchimont, P. (University of Liege, Institute of Pathology (Belgium)); Reuter, A.; Vrindts-Gevaert, Y. (National Institute of Radioelements, Fleurus (Belgium)); Pouillart, P.; Bretaudeau, B.; Falcoff, E.; Magdelenat, H. (Institut Curie, 75 - Paris (France))

    1984-01-01

    Using a radioimmunoassy for human leukocyte interferon (IFN..cap alpha..), pharmacokinetic studies were carried out in twelve cancer patients given sequential intramuscular injections of Hu IFN..cap alpha../sub 2/. Even though individual monitoring of serum IFN titers emphasized for a given dose, marked quantitative variations of the observed maximum concentrations, their mean values were found to be dose-dependent (358+-167 U/ml at 30.10/sup 6/ U and 1044+-599 U/ml at 100.10/sup 6/ U doses). Comparison with bioassay results showed that IFN activities measured in sera were of the same order of magnitude as those calculated from radioimmunoassay standard curves. Data obtained from this series on observed peak time, half-life value and serum concentrations were consistent with those reported by the other groups using recombinant leukocyte interferon in clinical trial. Therefore, radioimmunoassay is an useful method for routinely assaying IFN..cap alpha.. used either as antitumour or antivirus agent because of its high sensitivity (4 U/ml) and its simplicity.

  19. Regulation of bovine kidney alpha-ketoglutarate dehydrogenase complex by calcium ion and adenine nucleotides. Effects on S0.5 for alpha-ketoglutarate.

    Science.gov (United States)

    Lawlis, V B; Roche, T E

    1981-04-28

    Regulation of bovine kidney alpha-ketoglutarate dehydrogenase complex by energy-linked metabolites was investigated. Ca2+, ADP, or inorganic phosphate markedly enhanced the activity of the complex, and ATP or, to a lesser extent, GTP decreased the activity of the complex. Initial velocity studies with alpha-ketoglutarate as the varied substrate demonstrated that these modulators induced large changes in S0.5 for alpha-ketoglutarate (based on analysis in Hill plots) with no change in the maximum velocity (as determined by double-reciprocal plots). For all conditions studied, the Hill coefficients were significantly less than 1.0 with slopes that were linear over wide ranges of alpha-ketoglutarate concentrations, indicating negative cooperativity that probably resulted from multiple site-site interactions. Ca2+ (maintained at 10 muM by a Ca2+ buffer) decreased the S0.5 for alpha-ketoglutarate 63-fold (from 25 to 0.40 mM); even in the presence of a positive effector, ADP or phosphate, Ca2+ decreased the S0.5 for alpha-ketoglutarate 7.8- or 28-fold, respectively. Consistent with a mechanism of action dependent of Ca2+, ADP (1.60 mM) or phosphate (20 mM) reduced the S0.5 for alpha-ketoglutarate in the presence of Ca2+ (i.e., 4.5- or 1.67-fold, respectively); however, these effectors elicited larger decreases in S0.5 in the absence of Ca2+ (i.e., 37- or 3.7-fold, respectively). ATP (1.6 mM) increased the S0.5 for alpha-ketoglutarate, and Ca2+ appreciably reduced the effect, lowering the S0.5 98-fold from 66 to 0.67 mM. Thus the activity of the kidney alpha-ketoglutarate dehydrogenase complex is poised to increase as the energy potential in mitochondria declines, and Ca2+ has a pronounced modulatory effect. Comparative studies on bovine heart alpha-ketoglutarate dehydrogenase complex and the effects of varying the ADP/ATP ratio in the presence or absence of Ca2+ or phosphate are also described.

  20. Actions of alpha2 adrenoceptor ligands at alpha2A and 5-HT1A receptors: the antagonist, atipamezole, and the agonist, dexmedetomidine, are highly selective for alpha2A adrenoceptors.

    Science.gov (United States)

    Newman-Tancredi, A; Nicolas, J P; Audinot, V; Gavaudan, S; Verrièle, L; Touzard, M; Chaput, C; Richard, N; Millan, M J

    1998-08-01

    This study examined the activity of chemically diverse alpha2 adrenoceptor ligands at recombinant human (h) and native rat (r) alpha2A adrenoceptors compared with 5-HT1A receptors. First, in competition binding experiments at h alpha2A and h5-HT1A receptors expressed in CHO cells, several compounds, including the antagonists 1-(2-pyrimidinyl)piperazine (1-PP), (+/-)-idazoxan, benalfocin (SKF 86466), yohimbine and RX 821,002, displayed preference for h alpha2A versus h5-HT1A receptors of only 1.4-, 3.6-, 4-, 10- and 11-fold, respectively (based on differences in pKi values). Clonidine, brimonidine (UK 14304), the benzopyrrolidine fluparoxan and the guanidines guanfacine and guanabenz exhibited intermediate selectivity (22- to 31-fold) for h alpha2A receptors. Only the antagonist atipamezole and the agonist dexmedetomidine (DMT) displayed high preference for alpha2 adrenoceptors (1290- and 91-fold, respectively). Second, the compounds were tested for their ability to induce h5-HT1A receptor-mediated G-protein activation, as indicated by the stimulation of [35S]GTPgammaS binding. All except atipamezole and RX 821,002 exhibited agonist activity, with potencies which correlated with their affinity for h5-HT1A receptors. Relative efficacies (Emax values) were 25-35% for guanabenz, guanfacine, WB 4101 and benalfocin, 50-65% for 1-PP, (+/-)-idazoxan and clonidine, and over 70% for fluparoxan, oxymetazoline and yohimbine (relative to 5-HT = 100%). Yohimbine-induced [35S]GTPgammaS binding was inhibited by the selective 5-HT1A receptor antagonist WAY 100,635. In contrast, RX 821,002 was the only ligand which exhibited antagonist activity at h5-HT1A receptors, inhibiting 5-HT-stimulated [35S]GTPgammaS binding. Atipamezole, which exhibited negligeable affinity for 5-HT1A receptors, was inactive. Third, the affinities for r alpha2A differed considerably from the affinities for h alpha2A receptors whereas the affinities for r5-HT1A differed much less from the affinities for h5-HT

  1. The First Synthesis and Anti-retroviral Activity of 5',5'-Difluoro-3'-Hydroxy-Apiosyl Nucleoside Cyclomonophosphonic Acid Analogs

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Seyeon; Hong, Joon Hee [Chosun University, Gwangju (Korea, Republic of)

    2016-04-15

    The first synthesis of novel 5',5'-difluoro-30-hydroxy apiose nucleoside cyclomonophosphonic acid analogs was performed as potent anti-retroviral agents. Phosphonation was performed by direct displacement of a triflate intermediate with diethyl(lithiodifluoromethyl) phosphonate to give the corresponding(α, α-difluoroalkyl) phosphonate. Condensation successfully proceeded from a glycosyl donor with persilylated bases to yield the nucleoside phosphonate analogs. Deprotection of diethyl phosphonates provided the target nucleoside cyclomonophosphonic acid analogs. The synthesized nucleoside analogs were subjected to anti-viral screening against the human immunodeficiency virus-1 (HIV-1). Cytosine analogs show significant anti-HIV activity.

  2. VITAMIN C, VITAMIN A AND ALPHA HYDROXY ACID IN BENGKOANG (Pachyrhizus Erosus

    Directory of Open Access Journals (Sweden)

    Ardian Widyatmoko

    2016-04-01

    Full Text Available Bengkoang or Pachyrhizus erosus has been used as a traditional cosmetic material since many years ago. Until now, many cosmetic preparations using bengkoang as a main material have been produced by cosmetic industries, mainly for skin care, whitening and sunscreen preparation. However, content of vitamin A, vitamin C and alpha hydroxyl acid has not been discovered yet. These compounds are essential in skin care process because of their activities in cell regeneration, antioxidant as well as peeling of dead skin cell layer. The aim of this research is to provide information about the content of three compounds in bengkoang. Vitamin A has been analysed by spectrophotometer, vitamin C analysed using titration method and alpha hydroxyl acid analysed using gas chromatography. The result showed that concentrations of vitamin A and vitamin C are 179.21 ± 8.19 ppm and 0.31 ± 0.06 %, respectively. Meanwhile the content of alpha hydroxyl acid was 0.80 ± 0.01% (measured as glycolic acid.

  3. 40 CFR 180.1281 - S-Abscisic Acid, (S)-5-(1-hydroxy-2,6,6-trimethyl-4-oxo-1-cyclohex-2-enyl)-3-methyl-penta-(2Z,4E...

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 23 2010-07-01 2010-07-01 false S-Abscisic Acid, (S)-5-(1-hydroxy-2,6... Exemptions From Tolerances § 180.1281 S-Abscisic Acid, (S)-5-(1-hydroxy-2,6,6-trimethyl-4-oxo-1-cyclohex-2... from the requirement of a tolerance is established for residues of S-Abscisic Acid in or on all food...

  4. Progesterone modulation of alpha5 nAChR subunits influences anxiety-related behavior during estrus cycle.

    Science.gov (United States)

    Gangitano, D; Salas, R; Teng, Y; Perez, E; De Biasi, M

    2009-06-01

    Smokers often report an anxiolytic effect of cigarettes. In addition, stress-related disorders such as anxiety, post-traumatic stress syndrome and depression are often associated with chronic nicotine use. To study the role of the alpha5 nicotinic acetylcholine receptor subunit in anxiety-related responses, control and alpha5 subunit null mice (alpha5(-/-)) were subjected to the open field activity (OFA), light-dark box (LDB) and elevated plus maze (EPM) tests. In the OFA and LDB, alpha5(-/-) behaved like wild-type controls. In the EPM, female alpha5(-/-) mice displayed an anxiolytic-like phenotype, while male alpha5(-/-) mice were undistinguishable from littermate controls. We studied the hypothalamus-pituitary-adrenal axis by measuring plasma corticosterone and hypothalamic corticotropin-releasing factor. Consistent with an anxiolytic-like phenotype, female alpha5(-/-) mice displayed lower basal corticosterone levels. To test whether gonadal steroids regulate the expression of alpha5, we treated cultured NTera 2 cells with progesterone and found that alpha5 protein levels were upregulated. In addition, brain levels of alpha5 mRNA increased upon progesterone injection into ovariectomized wild-type females. Finally, we tested anxiety levels in the EPM during the estrous cycle. The estrus phase (when progesterone levels are low) is anxiolytic-like in wild-type mice, but no cycle-dependent fluctuations in anxiety levels were found in alpha5(-/-) females. Thus, alpha5-containing neuronal nicotinic acetylcholine receptors may be mediators of anxiogenic responses, and progesterone-dependent modulation of alpha5 expression may contribute to fluctuations in anxiety levels during the ovarian cycle.

  5. [Pr2(pdc3(Hpdc(H2O4]n·n(H3hp·8n(H2O, a One-Dimensional Coordination Polymer Containing PrO6N3 Tri-Capped Trigonal Prisms and PrO8N Mono-Capped Square Anti-Prisms (H2pdc = Pyridine 2,6-Dicarboxylic Acid, C7H5NO4; 3hp = 3-Hydroxy Pyridine, C5H5NO

    Directory of Open Access Journals (Sweden)

    Shahzad Sharif

    2012-08-01

    Full Text Available The synthesis, structure and some properties of the one-dimensional coordination polymer, [Pr2(pdc3(Hpdc]n·n(H3hp·8n(H2O, (H2pdc = pyridine 2,6-dicarboxylic acid, C7H5NO4; 3hp = 3-hydroxypyridine, C5H5NO are described. One of the Pr3+ ions is coordinated by two O,N,O-tridentate pdc2− ligands and one tridentate Hpdc− anion to generate a fairly regular PrO6N3 tri-capped trigonal prism, with the N atoms acting as the caps. The second Pr3+ ion is coordinated by one tridentate pdc2− dianion, four water molecules and two monodentate bridging pdc2− ligands to result in a PrO8N coordination polyhedron that approximates to a mono-capped square-anti-prism. The ligands bridge the metal-atom nodes into a chain, which extends in the [100] direction. The H3hp+ cation and uncoordinated water molecules occupy the inter-chain regions and an N–HLO and numerous O–HLO hydrogen bonds consolidate the structure. The H3hp+ species appears to intercalate between pendant pdc rings to consolidate the polymeric structure. Crystal data: 1 (C33H43N5O29Pr2, Mr = 1255.54, triclinic,  (No. 2, Z = 2, a = 13.2567(1 Å, b = 13.6304(2 Å, c = 13.6409(2 Å, α = 89.695(1°, β = 63.049(1°, γ = 86.105(1°, V = 2191.16(5 Å3, R(F = 0.033, wR(F2 = 0.084.

  6. Biotransformation of 5-hydroxy-methylfurfural into 2,5-furan-dicarboxylic acid by bacterial isolate using thermal acid algal hydrolysate.

    Science.gov (United States)

    Yang, Chu-Fang; Huang, Ci-Ruei

    2016-08-01

    Thermal acid hydrolysis is often used to deal with lignocellulosic biomasses, but 5-hydroxy-methylfurfural (5-HMF) formed during hydrolysis deeply influences downstream fermentation. 2,5-Furan-dicarboxylic acid (FDCA), which is in the list of future important biomass platform molecules can be obtained using 5-HMF biotransformation. Based on the connection between 5-HMF removal in acid hydrolysate and FDCA production, the optimum thermal acid hydrolysis condition for macroalgae Chaetomorpha linum was established. Potential microbes capable of transforming 5-HMF into FDCA were isolated and characterized under various parameters and inoculated into algal hydrolysate to perform 5-HMF biotransformation. The optimum hydrolysis condition was to apply 0.5M HCl to treat 3% algal biomass under 121°C for 15min. Isolated Burkholderia cepacia H-2 could transform 2000mg/L 5-HMF at the initial pH of 7 at 28°C and 1276mg/L FDCA was received. Strain B. cepacia H-2 was suitable for treating the algal hydrolysate without dilution, receiving 989.5mg/L FDCA. Copyright © 2016 Elsevier Ltd. All rights reserved.

  7. Computational, spectral and structural studies of a new non linear optical crystal: 2-hydroxy pyridinium 3,5-dinitrobenzoate

    Science.gov (United States)

    Sathya, K.; Dhamodharan, P.; Dhandapani, M.

    2017-02-01

    An organic proton transfer compound, 2-hydroxy pyridinium 3,5-dinitrobenzoate (HPDA) was synthesized from 3,5-dinitro benzoic acid and 2 -hydroxy pyridine using methanol:acetone solvent mixture at room temperature and crystallized by solvent evaporation. UV-Vis, FT-IR, 1H, 13C and DEPT-135 NMR spectroscopic techniques, CHN analysis and TG-DTA were used for characterization. Single crystal XRD analysis was carried out to ascertain the molecular structure. Computational studies that include optimization of molecular geometry, natural bond analysis (NBO), Mulliken population analysis and HOMO-LUMO analysis were performed using Gaussian 09 software by B3LYP method at 6-31g basis set level. Hirshfeld analysis indicate O⋯H/H⋯O interactions are the prominent interactions confirming the presence of Nsbnd H⋯O, Osbnd H⋯O and Csbnd H⋯O hydrogen bonding.The second-order NLO property was assessed by Kurtz-Perry powder technique. Theoretical calculations indicate that hyperpolarizability of the crystal is 38 times greater than urea. The results show that the HPDA may be used for opto-electronic applications.

  8. North Polar Cap

    Science.gov (United States)

    2004-01-01

    [figure removed for brevity, see original site] This week we will be looking at five examples of laminar wind flow on the north polar cap. On Earth, gravity-driven south polar cap winds are termed 'catabatic' winds. Catabatic winds begin over the smooth expanse of the cap interior due to temperature differences between the atmosphere and the surface. Once begun, the winds sweep outward along the surface of the polar cap toward the sea. As the polar surface slopes down toward sealevel, the wind speeds increase. Catabatic wind speeds in the Antartic can reach several hundreds of miles per hour. In the images of the Martian north polar cap we can see these same type of winds. Notice the streamers of dust moving downslope over the darker trough sides, these streamers show the laminar flow regime coming off the cap. Within the trough we see turbulent clouds of dust, kicked up at the trough base as the winds slow down and enter a chaotic flow regime. The horizontal lines in these images are due to framelet overlap and lighting conditions over the bright polar cap. Image information: VIS instrument. Latitude 86.5, Longitude 64.5 East (295.5 West). 40 meter/pixel resolution. Note: this THEMIS visual image has not been radiometrically nor geometrically calibrated for this preliminary release. An empirical correction has been performed to remove instrumental effects. A linear shift has been applied in the cross-track and down-track direction to approximate spacecraft and planetary motion. Fully calibrated and geometrically projected images will be released through the Planetary Data System in accordance with Project policies at a later time. NASA's Jet Propulsion Laboratory manages the 2001 Mars Odyssey mission for NASA's Office of Space Science, Washington, D.C. The Thermal Emission Imaging System (THEMIS) was developed by Arizona State University, Tempe, in collaboration with Raytheon Santa Barbara Remote Sensing. The THEMIS investigation is led by Dr. Philip Christensen

  9. Development, genetic mapping and QTL association of cotton PHYA, PHYB, and HY5-specific CAPS and dCAPS markers

    Science.gov (United States)

    Among SNP markers that become increasingly valuable in molecular breeding of crop plants are the CAP and dCAP markers derived from the genes of interest. To date, the number of such gene-based markers is small in polyploid crop plants such as tetraploid cotton that has A and D subgenomes. The obje...

  10. Skin cancer associated with commonly prescribed drugs: tumor necrosis factor alpha inhibitors (TNF-αIs), angiotensin-receptor blockers (ARBs), phosphodiesterase type 5 inhibitors (PDE5Is) and statins -weighing the evidence.

    Science.gov (United States)

    Nardone, Beatrice; Orrell, Kelsey A; Vakharia, Paras P; West, Dennis P

    2018-02-01

    Skin cancers, including both malignant melanoma (MM) and nonmelanoma skin cancer (NMSC), are the most commonly diagnosed cancers in the US. The incidence of both MM and NMSC continues to rise. Areas covered: Current evidence for an association between four of the most commonly prescribed classes of drugs in the U.S. and risk for MM and NMSC is reported. Medline was searched (January 2000 to May 2017) for each drug in the classes and for 'basal cell carcinoma', 'squamous cell carcinoma', 'non-melanoma skin cancer', 'skin cancer' and 'melanoma'. Skin cancer risk information was reported for: tumor necrosis factor alpha inhibitors (TNF-αIs), angiotensin-receptor blockers (ARBs), phosphodiesterase type 5 inhibitors (PDE5Is) and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA)-reductase inhibitors (statins). Expert opinion: Since skin cancer risk is associated with all four classes of these commonly prescribed drugs that represent nearly 20% of the Top 100 drugs in the U.S., these important findings warrant enhanced education, especially for prescribers and those patients at high risk for skin cancer.

  11. Comparison of hydroxy naphthoquinone from North Qinglongyi with different storage times

    Science.gov (United States)

    Xin, G. S.; Ji, Y. B.; Wei, C.

    2017-12-01

    Objective: To determine the appropriate solvent for the extraction of hydroxy naphthoquinone, and to establish a method for the determination of the content of hydroxy naphthoquinone in the North Qinglongyi, and compare the changes of the content of hydroxy naphthoquinone in North Qinglongyi with different storage times. Methods: According to the nature of hydroxy naphthoquinone in alkaline solution will be discolored, so this experiment for Juglone as the standard reagent, 5% KOH solution as a developer, and the absorbance was measured by UV-spectrophotometry at the wavelength of 515 nm. The content of hydroxy naphthoquinone in North Qinglongyi was determined by colorimetric method, and the contents of hydroxy naphthoquinone in North Qinglongyi of different storage times were compared. Results: The optimum extraction solvent was ethyl acetate. The recoveries were 97.73%±1.11% and the RSD was 1.14% (n = 6). The contents of hydroxy naphthoquinone in the North Qinglunyi were 0.0141%, 0.0104% and 0.0073%, respectively, for one year, two years and three years. The content of hydroxy naphthoquinone decreased with the storage time prolonged. Conclusion This experimental method was stability, high recovery rate, simple and reliable. According to the results of this experiment, we can see that the storage time of North Qinglunyi should not be too long. Should try to choose this year’s North Qinglunyi for experimental research.

  12. Synthesis of carbasugars from aldonolactones, part III - A study on the allylic substitution of (1R,5R,8R)- and (1R,5R,8S)-8-hydroxy-2-oxabicyclo[3.3.0]oct-6-en-3-one derivatives - Preparation of (1S,2R,3R)-9-[2-hydroxy-3-(2-hydroxyethyl)cyclopent-4-en-1-yl]-9H-adenine

    DEFF Research Database (Denmark)

    Johansen, Steen Karsk; Lundt, Inge

    2001-01-01

    The palladium-catalyzed substitution of acylated (1R,5R,8R)- and (1R,SR,8S)-8-hydroxy-2-oxabicyclo[3.3.0] ones has been studied using a number of C- and N-nucleophiles, In all cases, the exo derivatives (8R) were found to be more reactive than the corresponding endo derivatives (8S). The reaction...... with these nucleophiles. Additionally, Mitsunobu substitution of (1R,5R,8R)-8-hydroxy-2-oxabicyclo[3.3.0]oct-B-en-3-one (3) with 6-chloropurine, followed by reduction of the lactone moiety and treatment with Liquid ammonia, gave the carbocyclic nucleoside (1S,2R,3R)-9-[2-hydroxy-3-(2-hydroxyethyl)cyclopent-4-en-1-yl]-9H...

  13. New evidence from the Lyman-alpha forest concerning the formation of galaxies

    Energy Technology Data Exchange (ETDEWEB)

    Wolfe, A M

    1986-12-17

    A new type of survey for galaxies with z > 2 is described. The idea is to search for the spectroscopic imprint that the H1 disc of a foreground galaxy leaves on radiation emitted by a background QSO; namely, a Lyman-..cap alpha.. absorption line broadened by radiation damping. A continuing survey has revealed the presence of 15 damped L..cap alpha.. lines with redshifts between 1.8 and 2.8 in the spectra of 68 QSOs. In comparison, no more than three discs with the properties of nearby galaxies should have been detected. Furthermore, the mean column density of the 15 absorbers, = 1.4 x 10/sup 21/cm/sup -2/, is much larger than expected for the outskirts of H1 discs. The statistical and physical evidence accumulated suggests that the damped L..cap alpha.. systems are a distinct population of absorbers with properties reminiscent of H1 discs. It is concluded that the progenitors of the baryon content of nearby galaxies have been detected. The implications for theories of galaxy formations of the discovery of this damped population of absorbers are explained.

  14. Synthesis and characterization of lanthanum complex (5-choloro-8-hydroxy quinoline) bis (2-2'bipyridine) lanthanum La(Bpy)2(5-Clq)

    Science.gov (United States)

    Kumar, Rahul; Soam, Ankur; Bhargava, Parag

    2017-05-01

    Lanthanum complex, (5-choloro 8-hydroxy quinoline) bis (2-2'bipyridine) has been synthesized and characterized by different techniques. Lanthanum complex, La(Bpy)2(5-Clq) was characterized for structural, thermal and photoluminescence analysis. Structural analysis of this material was done by Fourier transformed infrared spectroscopy (FTIR) and mass spectroscopy. Thermal analysis of this material was done by thermal gravimetric analysis (TGA) and material shows the thermal stability up to 400°C. Absorption and emission spectra of the material was measured by UV-visible spectroscopy and photoluminescence spectroscopy. Solution of this material La(Bpy)2(5-Clq) in ethanol showed absorption peak at 332 nm, which may be attributed due to (π - π*) transitions. The photoluminescence spectra of La(Bpy)2(5-Clq) in ethanol solution showed intense peak at 505 nm.

  15. 75 FR 50884 - 2-(2'-hydroxy-3', 5'-di-tert-amylphenyl) benzotriazole and Phenol, 2-(2H-benzotriazole-2-yl)-6...

    Science.gov (United States)

    2010-08-18

    ... 2-(2'-hydroxy-5'-methylphenyl) benzotriazole in guinea pigs showed skin sensitization; however... pesticide manufacturer. Potentially affected entities may include, but are not limited to: Crop production (NAICS code 111). Animal production (NAICS code 112). Food manufacturing (NAICS code 311). Pesticide...

  16. Synthesis, resolution and radioiodination of S(-)trans-5-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'-propenyl)amino]tet ralin-S(-)trans-5-OH-PIPAT: a new dopamine D2-like receptor ligand

    International Nuclear Information System (INIS)

    Chumpradit, Sumalee; Meiping Kung; Vessotskie, Janet; Kung, H.F.

    1995-01-01

    A new dopamine D2-like receptor ligand, (R,S)trans-5-hydroxy-2-[N-n0propyl-N-(3'-iodo-2'-propeny)amino]tet ralin ((R,S)trans-5-OH-PIPAT,3), based on high affinity dopamine receptor agonist 5-hydroxy-2-[N,N-(di-n-propyl)-2-amino]tetralin (5-OH-DPAT,1), was prepared. The synthesis was achieved by a reductive amination of 5-methoxy-2-tetralone with n-propylamine, followed by N-alkylation, to afford 5-methoxy-N-propyl-N-2'-aminotetralin,7. Reduction of 7 with tributyltin hydride gave the tri-n-butyl tin derivative,8, which was converted to 9 by an iododemetalation reaction. Demethylation of 9 gave the desired compound, (R,S)trans-5-OH-PIPAT,3. The resolved (R) and (S)trans-5-OH-PIPAT,3 were also quantitatively prepared. (author)

  17. 1-[3-(2-Benzyloxy-6-hydroxy-4-methylphenyl-5-[3,5-bis(trifluoromethylphenyl]-4,5-dihydro-1H-pyrazol-1-yl]propane-1-one

    Directory of Open Access Journals (Sweden)

    U. H. Patel

    2013-06-01

    Full Text Available In the title compound, C28H24F6N2O3, the mean plane of the central pyrazoline ring forms dihedral angles of 2.08 (9 and 69.02 (16° with the 2-benzyloxy-6-hydroxy-4-methylphenyl and 3,5-bis(trifluoromethylphenyl rings, respectively. The dihedral angle between the mean planes of the pyrazoline and 3,5-bis(trifluoromethylphenyl rings is 68.97 (9°. An intramolecular O—H...N hydrogen bond is observed, which forms an S(6 graph-set motif. In the crystal, pairs of weak C—H...F halogen interactions link the molecules into inversion dimers while molecular chains along [100] are formed by C—H...O contacts.

  18. The glutamate receptor GluR5 agonist (S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid and the 8-methyl analogue

    DEFF Research Database (Denmark)

    Clausen, Rasmus Prætorius; Naur, Peter; Kristensen, Anders Skov

    2009-01-01

    The design, synthesis, and pharmacological characterization of a highly potent and selective glutamate GluR5 agonist is reported. (S)-2-Amino-3-((RS)-3-hydroxy-8-methyl-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid (5) is the 8-methyl analogue of (S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H......-cyclohepta[d]isoxazol-4-yl)propionic acid ((S)-4-AHCP, 4). Compound 5 displays an improved selectivity profile compared to 4. A versatile stereoselective synthetic route for this class of compounds is presented along with the characterization of the binding affinity of 5 to ionotropic glutamate receptors (i......GluRs). Functional characterization of 5 at cloned iGluRs using a calcium imaging assay and voltage-clamp recordings show a different activation of GluR5 compared to (S)-glutamic acid (Glu), kainic acid (KA, 1), and (S)-2-amino-3-(3-hydroxy-5-tert-butyl-4-isoxazolyl)propionic acid ((S)-ATPA, 3) as previously...

  19. Synthesis and evaluation of a 5-Membered Isoiminosugar as Glycosidase Inhibitor

    DEFF Research Database (Denmark)

    Lundt, Inge; Godskesen, Michael Anders

    1998-01-01

    (3R, 4R)-4-hydroxy-3-hydroxymethylpyrrolidine (6) was prepared from D-xylose and found to be a weak inhibitor of alpha-D-, beta-D-glucosidase and alpha-L-fucosidase. (C) 1998 Published by Elsevier Science Ltd. All rights reserved....

  20. On the formation of C2H5O2+ ions having the structure of hydroxy-protonated acetic acid

    NARCIS (Netherlands)

    Terlouw, J.K.; Koster, C.G. de; Levsen, K.

    1984-01-01

    Experiments are reported which are best explained in terms of the formation of the long-sought hydroxy-protonated acetic acid, CH3C(O)OH2- This C2 H5O2+ species, generated upon dissociative ionization of 2,4-dihydroxy-2-methylpentane (consecutive losses of CH3. and C3H6), is characterized by a

  1. IAA transport in corn roots includes the root cap

    International Nuclear Information System (INIS)

    Hasenstein, K.H.

    1989-01-01

    In earlier reports we concluded that auxin is the growth regulator that controls gravicurvature in roots and that the redistribution of auxin occurs within the root cap. Since other reports did not detect auxin in the root cap, we attempted to confirm the IAA does move through the cap. Agar blocks containing 3 H-IAA were applied to the cut surface of 5 mm long apical segments of primary roots of corn (mo17xB73). After 30 to 120 min radioactivity (RA) of the cap and root tissue was determined. While segments suspended in water-saturated air accumulated very little RA in the cap, application of 0.5 μ1 of dist. water to the cap (=controls) increased RA of the cap dramatically. Application to the cap of 0.5 μ1 of sorbitol or the Ca 2+ chelator EGTA reduced cap RA to 46% and 70% respectively compared to water, without affecting uptake. Control root segments gravireacted faster than non-treated or osmoticum or EGTA treated segments. The data indicate that both the degree of hydration and calcium control the amount of auxin moving through the cap

  2. Investigating Spectrum of Biological Activity of 4- and 5-Chloro-2-hydroxy-N-[2-(arylamino-1-alkyl-2-oxoethyl]benzamides

    Directory of Open Access Journals (Sweden)

    Jirina Stolarikova

    2011-03-01

    Full Text Available In this study, a series of twenty-two 5-chloro-2-hydroxy-N-[2-(arylamino-1-alkyl-2-oxoethyl]benzamides and ten 4-chloro-2-hydroxy-N-[2-(arylamino-1-alkyl-2-oxoethyl]benzamides is described. The compounds were analyzed using RP-HPLC to determine lipophilicity. Primary in vitro screening of the synthesized compounds was performed against mycobacterial, bacterial and fungal strains. They were also evaluated for their activity related to the inhibition of photosynthetic electron transport (PET in spinach (Spinacia oleracea L. chloroplasts. The compounds showed biological activity comparable with or higher than the standards isoniazid, fluconazole, penicillin G or ciprofloxacin. For all the compounds, the relationships between the lipophilicity and the chemical structure of the studied compounds as well as their structure-activity relationships are discussed.

  3. Plasma and milk concentrations of vitamin D3 and 25-hydroxy vitamin D3 following intravenous injection of vitamin D3 or 25-hydroxy vitamin D3.

    OpenAIRE

    Hidiroglou, M; Knipfel, J E

    1984-01-01

    Plasma levels of vitamin D3 or 25-hydroxyvitamin D3 in ewes after administration of a single massive intravenous dose of vitamin D3 (2 X 10(6) IU) or 25-hydroxy vitamin D3 (5 mg) were determined at zero, one, two, three, five, ten and 20 days postinjection. In six ewes injected with vitamin D3 conversion of vitamin D3 to 25-hydroxy vitamin D3 resulted in a six-fold increase in the plasma 25-hydroxy vitamin D3 level within one day. Elevated levels were maintained until day 10 but by day 20 a s...

  4. Cervical Cap

    Science.gov (United States)

    ... Videos for Educators Search English Español The Cervical Cap KidsHealth / For Teens / The Cervical Cap What's in ... Call the Doctor? Print What Is a Cervical Cap? A cervical cap is a small cup made ...

  5. Polyketide family of novel antibacterial 7-O-methyl-5'-hydroxy-3'-heptenoate-macrolactin from seaweed-associated Bacillus subtilis MTCC 10403.

    Science.gov (United States)

    Chakraborty, Kajal; Thilakan, Bini; Raola, Vamshi Krishna

    2014-12-17

    Seaweed-associated heterotrophic bacterial communities were screened to isolate potentially useful antimicrobial strains, which were characterized by phylogenetic analysis. The bacteria were screened for the presence of metabolite genes involved in natural product biosynthetic pathway, and the structural properties of secondary metabolites were correlated with the genes. Bioactivity-guided isolation of polyene antibiotic 7-O-methyl-5'-hydroxy-3'-heptenoate-macrolactin from Bacillus subtilis MTCC10403 associated with seaweed Anthophycus longifolius using mass spectrometry and extensive 2D-NMR studies was carried out. The newly isolated macrolactin compound is a bactericidal antibiotic with broad spectrum activity against human opportunistic clinical pathogens. The biosynthetic pathway of 7-O-methyl-5'-hydroxy-3'-heptenoate-macrolactin by means of a stepwise, decarboxylative condensation pathway established the PKS-assisted biosynthesis of the parent macrolactin and the side-chain 5-hydroxyhept-3-enoate moiety attached to the macrolactin ring system at C-7. Antimicrobial activity analysis combined with the results of amplifying genes encoding for polyketide synthetase and nonribosomal peptide synthetase showed that seaweed-associated bacteria had broad-spectrum antimicrobial activity. The present work may have an impact on the exploitation of macrolactins for pharmaceutical and biotechnological applications.

  6. Effects of gamma radiation on the concentration of 5-hydroxy-L-tryptophan and 5-hydroxytryptamine in presence of radioprotector in Sprague Dawley rats

    International Nuclear Information System (INIS)

    Upadhyay, S.N.; Sharma, Ashok; Nagpal, K.K.; Saini, S.K.

    1997-01-01

    The result of variation of 5-hydroxy-L-tryptophan (HT) and 5-hydroxytryptamine (5-HT) in different tissues of control and gamma-irradiated Sprague Dawley rats with and without a radioprotector β-amino-ethylisothiuronium bromide hydrobromide (AET) combination e.g. (HT+AET) have been studied. The retention of HT, in the tissues studied, decreased after lethal dose (10.5 Gy) but for 5-HT, no such trend was observed after incorporation of HT+AET. A slight tendency of both metabolites to come back to control level was also observed for Sprague Dawley rats. In urine concentration of HT was less compared to 5-HT with a lethal dose (10.5 Gy). After incorporation of HT+AET the turnover rate of HT and 5-HT were found to be maximum when it was injected through intraperitoneal route. (author)

  7. 49 CFR 230.41 - Flexible staybolts with caps.

    Science.gov (United States)

    2010-10-01

    ... 49 Transportation 4 2010-10-01 2010-10-01 false Flexible staybolts with caps. 230.41 Section 230... Appurtenances Staybolts § 230.41 Flexible staybolts with caps. (a) General. Flexible staybolts with caps shall have their caps removed during every 5th annual inspection for the purpose of inspecting the bolts for...

  8. Age-dependent changes in expression of alpha1-adrenergic receptors in rat myocardium

    International Nuclear Information System (INIS)

    Schaffer, W.; Williams, R.S.

    1986-01-01

    The expression of alpha 1 -adrenergic receptors within ventricular myocardium of rats ranging in age from 21 days of fetal life to 24 months after birth was measured from [ 125 I] 2-(β hydroxy phenyl) ethylaminomethyl tetralone binding isotherms. No difference was observed in binding affinity between any of the age groups studied. The number of alpha 1 -adrenergic receptors was found to be 60-120% higher in membranes from fetal or immature rats up to 25 days of age when compared with adult animals. The increased expression of alpha 1 -adrenergic receptors in the developing heart relative to that observed in adult heart is consistent with the hypothesis that alpha 1 -adrenergic receptor stimulation may modulate protein synthesis and growth in mammalian myocardium

  9. Occurrence and metabolism of 7-hydroxy-2-indolinone-3-acetic acid in Zea mays

    Science.gov (United States)

    Lewer, P.; Bandurski, R. S.

    1987-01-01

    7-Hydroxy-2-indolinone-3-acetic acid was identified as a catabolite of indole-3-acetic acid in germinating kernels of Zea mays and found to be present in amounts of ca 3.1 nmol/kernel. 7-Hydroxy-2-indolinone-3-acetic acid was shown to be a biosynthetic intermediate between 2-indolinone-3-acetic acid and 7-hydroxy-2-indolinone-3-acetic acid-7'-O-glucoside in both kernels and roots of Zea mays. Further metabolism of 7-hydroxy-2-[5-3H]-indolinone-3-acetic acid-7'-O-glucoside occurred to yield tritiated water plus, as yet, uncharacterized products.

  10. Spectrophotometric determination of La (III) with sulphamethoxazole based hydroxy triazene

    International Nuclear Information System (INIS)

    Manwani, Sapana; Chauhan, R.S.; Goswami, A.K.

    2015-01-01

    In the present study, 3-hydroxy-3-p-chlorophenyll-1-(4-amino-N-(5-methyl-1,2-oxazole-3- yl) benzenesulphonamide-methane) triazene has been synthesized by coupling of hydroxylamine obtained by reduction of nitro compound with diazonium salt obtained from sulphamethoxazole taking hydroxylamine in excess at temperature between 0-5°C. Chemical structure of the synthesized compound was confirmed by IR, 1 H NMR, MASS and by elemental analysis. The complex of the reagent with La (III) has been studied. 3-hydroxy-3-p-chlorophenyll-1-(4-amino-N-(5-methyl-1,2-oxazole-3-yl) benzenesulphonamide-methane) triazene has been used for spectrophotometric determination of lanthanum (III) at 392 nm, keeping the pH between 8.5 to 8.9

  11. Selective agonists at group II metabotropic glutamate receptors: synthesis, stereochemistry, and molecular pharmacology of (S)- and (R)-2-amino-4-(4-hydroxy[1,2,5]thiadiazol-3-yl)butyric acid

    DEFF Research Database (Denmark)

    Clausen, Rasmus P; Bräuner-Osborne, Hans; Greenwood, Jeremy R

    2002-01-01

    Homologation of analogues of the central excitatory neurotransmitter glutamic acid (Glu), in which the distal carboxy group has been bioisosterically replaced by acidic heterocyclic units, has previously provided subtype selective ligands for metabotropic Glu receptors (mGluRs). The (S......)-form of the 1,2,5-thiadiazol-3-ol Glu analogue, 2-amino-3-(4-hydroxy[1,2,5]thiadiazol-3-yl)propionic acid (TDPA, 6), is an 2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) receptor agonist, which in addition stereospecifically activates group I mGluRs. We have now synthesized the (S)- and (R......)-forms of 2-amino-4-(4-hydroxy[1,2,5]thiadiazol-3-yl)butyric acid (homo-TDPA, 7) and shown that whereas neither enantiomer interacts with AMPA receptors, (S)- and (R)-7 appear to be selective and equipotent agonists at group II mGluRs as represented by the mGluR2 subtype. The activities of (S)- and (R)-7...

  12. Impact of x-ray dose on the response of CR-39 to 1-5.5 MeV alphas

    International Nuclear Information System (INIS)

    Rojas-Herrera, J.; Rinderknecht, H. G.; Zylstra, A. B.; Gatu Johnson, M.; Orozco, D.; Rosenberg, M. J.; Sio, H.; Seguin, F. H.; Frenje, J. A.; Li, C. K.; Petrasso, R. D.

    2015-01-01

    The CR-39 nuclear track detector is used in many nuclear diagnostics fielded at inertial confinement fusion (ICF) facilities. Large x-ray uences generated by ICF experiments may impact the CR-39 response to incident charged particles. To determine the impact of x-ray exposure on the CR-39 response to alpha particles, a thick-target bremsstrahlung x-ray generator was used to expose CR-39 to various doses of 8 keV Cu-K α and K β x-rays. The CR-39 detectors were then exposed to 1-5.5 MeV alphas from an Am-241 source. The regions of the CR-39 exposed to x-rays showed a smaller track diameter than those not exposed to x-rays: for example, a dose of 3.0 ± 0.1 Gy causes a decrease of (19 ± 2)% in the track diameter of a 5.5 MeV alpha particle, while a dose of 60.0 ± 1.3 Gy results in a decrease of (45 ± 5)% in the track diameter. The reduced track diameters were found to be predominantly caused by a comparable reduction in the bulk etch rate of the CR-39 with x-ray dose. A residual effect depending on alpha particle energy is characterized using an empirical formula

  13. Facile synthesis of some novel 2-substituted-4,6-diarylpyrimidines using 4 ' -hydroxy-3 ' ,5 ' -dinitrochalcones and S-benzylthiouronium chloride

    Directory of Open Access Journals (Sweden)

    K. L. Ameta

    2012-01-01

    Full Text Available Various 4'-hydroxy-3',5'-dinitro substituted chalcones 1 and S-benzylthiouronium chloride (SBT 2 in the presence of DMF-organic bases (morpholine/ pyrrolidine/ piperidine gave 4,6-diaryl-2-(4-morpholinyl / 1-pyrrolidinyl /1-piperidinyl- pyrimidines 4, 5 and 6 in a facile one-pot conversion. In an another attempt reactants 1 and 2 yielded intermediate 2-benzylthiopyrimidines 3, in presence of DMF, which on treatment with heterocyclic secondary amines gave products 4, 5 and 6 in an alternate two-step process.

  14. Radioactive decay of sup(91m)Nb

    Energy Technology Data Exchange (ETDEWEB)

    Lakshminarayana, V.; Venkataratnam, S.; Rao, B.V.T.; Narasimham, K.L.; Chintalapudi, S.N.

    1987-08-01

    The radioactive decay of sup(91m)Nb, produced by the reaction /sup 89/Y(..cap alpha.., 2n), is studied using Ge(Li), HPGe and Si(Li) detectors. The K-conversion coefficient, ..cap alpha..sub(K), of the 104.5 keV transition is determined accurately, for the first time, from the Nb Ksub(..cap alpha..) x-ray and 104.5 keV gamma-ray intensities. The experimental value of ..cap alpha..sub(K) thus determined is 115(5), in agreement with the value expected for an M4 transition.

  15. A role for 5alpha-reductase activity in the development of male homosexuality?

    Science.gov (United States)

    Alias, A G

    2004-12-01

    Higher body hair with lower mesmorphism ratings were observed in Caucasian homosexual men compared with the general male population, reflecting elevated 5alpha-reductase (5alphaR) activity, and higher dihydrotestosterone-to-testosterone (DHT-to-T) ratio, in sharp contrast to 46,XY 5alphaR 2 deficiency subjects, who are often born with ambiguous, or female genitalia, but tend to grow up to be muscular, heterosexual men with very little body hair, or beard. One study also showed them scoring around dull normal IQs. A greater prevalence of liberal body hair growth in men with higher IQs and/or educational levels was also observed in several samples. The exceptions to this statistical trend are too unsettling, however. Nevertheless, the results of a number of published studies, including one showing higher DHT-to-T ratio in homosexual men, done with different objectives over a span of 80 years, together strongly support these findings. Furthermore, in an animal model, "cognitive-enhancing effects" of "5alpha-reduced androgen [metabolites]" were recently demonstrated.

  16. Novel 1,5,7-trihydroxy-3-hydroxy methyl anthraquinone isolated from terrestrial Streptomyces sp. (eri-26) with antimicrobial and molecular docking studies.

    Science.gov (United States)

    Duraipandiyan, V; Al-Dhabi, N A; Balachandran, C; Raj, M Karunai; Arasu, M Valan; Ignacimuthu, S

    2014-11-01

    Streptomyces sp. isolate ERI-26 was obtained from the Nilgiris forest soil of Western Ghats, Tamil Nadu, India. Novel anthraquinone compound was isolated from the active fraction 5; it was identified by spectroscopical data using UV, IR, NMR and MASS. The isolated compound 1,5,7-trihydroxy-3-hydroxy methyl anthraquinone was tested against bacteria and fungi at minimum inhibitory concentration level. The compound showed significant antimicrobial activity against bacteria, Staphylococcus aureus at 125 μg/ml, Staphylococcus epidermidis at 62.5 μg/m, Bacillus subtilis at 31.25 μg/ml, fungi; Epidermophyton floccosum at 62.5 μg/ml, Aspergillus niger at 31.25 μg/ml, Aspergiller flavus at 31.25 μg/ml, Trichophyton rubrum at 62.5 μg/ml and Botrytis cinerea at 62.5 μg/ml. The isolated compound was subjected to molecular docking studies for the inhibition of TtgR, topoisomerase IV and AmpC β-lactamase enzymes which are targets for antimicrobials. Docking studies of the compound showed low docking energy indicating its usefulness as antimicrobial agent. 1,5,7-Trihydroxy-3-hydroxy methyl anthraquinone is new, and its antimicrobial and molecular docking properties are reported for the first time.

  17. Facile hydrothermal synthesis of alpha manganese sesquioxide ({alpha}-Mn{sub 2}O{sub 3}) nanodumb-bells: Structural, magnetic, optical and photocatalytic properties

    Energy Technology Data Exchange (ETDEWEB)

    Gnanam, S., E-mail: gnanam.nanoscience@gmail.com [Department of Physics, Presidency College, Chennai 600005, Tamilnadu (India); Rajendran, V. [Department of Physics, Presidency College, Chennai 600005, Tamilnadu (India)

    2013-02-15

    Highlights: Black-Right-Pointing-Pointer {alpha}-Mn{sub 2}O{sub 3} nanoparticles sizes of 35-42 nm have been prepared by hydrothermal process. Black-Right-Pointing-Pointer Shapes of {alpha}-Mn{sub 2}O{sub 3}: Dumb-bell, Cauliflower, spherical with rod, spherical with wires. Black-Right-Pointing-Pointer The strong UV emission can be attributed to high purity and perfect crystallinity. Black-Right-Pointing-Pointer Photocatalytic activity of {alpha}-Mn{sub 2}O{sub 3} was studied by degradation of Remazol red B dye. - Abstract: Nanometer scale cubic bixbyite {alpha}-Mn{sub 2}O{sub 3} has been synthesized by a facile hydrothermal method, at a temperature of 450 Degree-Sign C in the presence of various surfactants. The X-ray diffraction (XRD) analysis shows that the average crystallite size of the sample is {approx}35-42 nm. The shapes of the {alpha}-Mn{sub 2}O{sub 3} nanoparticles include: Dumb-bell-like (anionic surfactant), Cauliflower-like (nonionic surfactant), spherical with rods (cationic surfactant) and spherical with wires (surface modifier). The shapes of {alpha}-Mn{sub 2}O{sub 3} nanoparticles depend on the type of surfactant used in the synthesis. The magnetic property of the anionic surfactant assisted sample was primarily studied, using the vibrating sample magnetometer (VSM). The optical absorption spectra confirmed the effectiveness of the selected capping agents, as the anionic capped {alpha}-Mn{sub 2}O{sub 3} colloids absorbed at shorter wavelength than the other agents, indicating a much smaller crystallite size. The property of strong UV emissions may be attributed to the high purity and perfect crystallinity of the as-prepared {alpha}-Mn{sub 2}O{sub 3}. The surfactants-assisted catalyst was tested for its photocatalytic activity towards the photodegradation of the harmful organic dye Remazol Red B, using a multilamp photo reactor. Possible formation mechanisms have also been proposed for the as-synthesized anionic surfactant assisted samples.

  18. Potency of a novel saw palmetto ethanol extract, SPET-085, for inhibition of 5alpha-reductase II.

    Science.gov (United States)

    Pais, Pilar

    2010-08-01

    The nicotinamide adenine dinucleotide phosphate (NADPH)-dependent membrane protein 5alpha-reductase irreversibly catalyses the conversion of testosterone to the most potent androgen, 5alpha-dihydrotestosterone (DHT). In humans, two 5alpha-reductase isoenyzmes are expressed: type I and type II. Type II is found primarily in prostate tissue. Saw palmetto extract (SPE) has been widely used for the treatment of lower urinary tract symptoms secondary to benign prostatic hyperplasia (BPH). The mechanisms of the pharmacological effects of SPE include the inhibition of 5alpha-reductase, among other actions. Clinical studies of SPE have been equivocal, with some showing significant results and others not. These inconsistent results may be due, in part, to varying bioactivities of the SPE used in the studies. The aim of the present study was to determine the in vitro potency of a novel saw palmetto ethanol extract (SPET-085), an inhibitor of the 5alpha-reductase isoenzyme type II, in a cell-free test system. On the basis of the enzymatic conversion of the substrate androstenedione to the 5alpha-reduced product 5alpha-androstanedione, the inhibitory potency was measured and compared to those of finasteride, an approved 5alpha-reductase inhibitor. SPET-085 concentration-dependently inhibited 5alpha-reductase type II in vitro (IC(50)=2.88+/-0.45 microg/mL). The approved 5alpha-reductase inhibitor, finasteride, tested as positive control, led to 61% inhibition of 5alpha-reductase type II. SPET-085 effectively inhibits the enzyme that has been linked to BPH, and the amount of extract required for activity is very low compared to data reported for other extracts. It can be concluded from data in the literature that SPET-085 is as effective as a hexane extract of saw palmetto that exhibited the highest levels of bioactivity, and is more effective than other SPEs tested. This study confirmed that SPET-085 has prostate health-promoting bioactivity that also corresponds favorably to

  19. Dust Attenuation and H(alpha) Star Formation Rates of Z Approx. 0.5 Galaxies

    Science.gov (United States)

    Ly, Chun; Malkan, Matthew A.; Kashikawa, Nobunari; Ota, Kazuaki; Shimasaku, Kazuhiro; Iye, Masanori; Currie, Thayne

    2012-01-01

    Using deep narrow-band and broad-band imaging, we identify 401 z approximately 0.40 and 249 z approximately 0.49 H-alpha line-emitting galaxies in the Subaru Deep Field. Compared to other H-alpha surveys at similar redshifts, our samples are unique since they probe lower H-alpha luminosities, are augmented with multi-wavelength (rest-frame 1000AA--1.5 microns) coverage, and a large fraction (20%) of our samples has already been spectroscopically confirmed. Our spectra allow us to measure the Balmer decrement for nearly 60 galaxies with H-beta detected above 5-sigma. The Balmer decrements indicate an average extinction of A(H-alpha)=0.7(uparrow){+1.4}_{-0.7} mag. We find that the Balmer decrement systematically increases with higher H-alpha luminosities and with larger stellar masses, in agreement with previous studies with sparser samples. We find that the SFRs estimated from modeling the spectral energy distribution (SED) is reliable---we derived an "intrinsic" H-alpha luminosity which is then reddened assuming the color excess from SED modeling. The SED-predicted H-alpha luminosity agrees with H-alpha narrow-band measurements over 3 dex (rms of 0.25 dex). We then use the SED SFRs to test different statistically-based dust corrections for H-alpha and find that adopting one magnitude of extinction is inappropriate: galaxies with lower luminosities are less reddened. We find that the luminosity-dependent dust correction of Hopkins et al. yields consistent results over 3 dex (rms of 0.3 dex). Our comparisons are only possible by assuming that stellar reddening is roughly half of nebular reddening. The strong correspondence argue that with SED modeling, we can derive reliable intrinsic SFRs even in the absence of H-alpha measurements at z approximately 0.5.

  20. Transparent organic light-emitting diodes with different bi-directional emission colors using color-conversion capping layers

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Jonghee, E-mail: jonghee.lee@etri.re.kr [OLED Research Center, Electronics and Telecommunications Research Institute (ETRI), Daejeon 305-700 (Korea, Republic of); Institut für Angewandte Photophysik, Technische Universität Dresden, George-Bähr-Straße 1, 01062 Dresden (Germany); Koh, Tae-Wook [Department of Electrical Engineering, Korea Advanced Institute of Science and Technology (KAIST), Daejeon 305-701 (Korea, Republic of); Cho, Hyunsu [OLED Research Center, Electronics and Telecommunications Research Institute (ETRI), Daejeon 305-700 (Korea, Republic of); Department of Electrical Engineering, Korea Advanced Institute of Science and Technology (KAIST), Daejeon 305-701 (Korea, Republic of); Schwab, Tobias [Institut für Angewandte Photophysik, Technische Universität Dresden, George-Bähr-Straße 1, 01062 Dresden (Germany); Lee, Jae-Hyun [Department School of Global Convergence Studies, Hanbat National University, San 16-1, Duckmyoung-dong, Daejeon 305-719 (Korea, Republic of); Hofmann, Simone [Institut für Angewandte Photophysik, Technische Universität Dresden, George-Bähr-Straße 1, 01062 Dresden (Germany); Lee, Jeong-Ik [OLED Research Center, Electronics and Telecommunications Research Institute (ETRI), Daejeon 305-700 (Korea, Republic of); Yoo, Seunghyup [Department of Electrical Engineering, Korea Advanced Institute of Science and Technology (KAIST), Daejeon 305-701 (Korea, Republic of); and others

    2015-06-15

    We report a study on transparent organic light-emitting diodes (OLEDs) with different bi-directional emission colors, enabled by color-conversion organic capping layers. Starting from a transparent blue OLED with an uncapped Ag top electrode exhibiting an average transmittance of 33.9%, a 4-(dicyanomethylene)-2-methyl-6-(4-dimethylaminostyryl)-4H-pyran (DCM)-doped tris-(8-hydroxy-quinolinato)-aluminum (Alq3) capping layer is applied to achieve color-conversion from blue to orange-red on the top side while maintaining almost unchanged device transmittance. This color-conversion capping layer does not only change the color of the top side emission, but also enhances the overall device efficiency due to the optical interaction of the capping layer with the primary blue transparent OLED. Top white emission from the transparent bi-directional OLED exhibits a correlated color temperature around 6000–7000 K, with excellent color stability as evidenced by an extremely small variation in color coordinate of Δ(x,y)=(0.002, 0.002) in the forward luminance range of 100–1000 cd m{sup −2}. At the same time, the blue emission color of bottom side is not influenced by the color conversion capping layer, which finally results in different emission colors of the two opposite sides of our transparent OLEDs. - Highlights: • We report transparent organic light-emitting diodes (OLEDs) with different bi-directional emission colors. • Transparent blue OLED with color-conversion organic capping layers (CCL) shows orange top side emission. • Top white emission exhibits a CCT around 7000 K, with excellent color stability on a driving voltage.

  1. Transparent organic light-emitting diodes with different bi-directional emission colors using color-conversion capping layers

    International Nuclear Information System (INIS)

    Lee, Jonghee; Koh, Tae-Wook; Cho, Hyunsu; Schwab, Tobias; Lee, Jae-Hyun; Hofmann, Simone; Lee, Jeong-Ik; Yoo, Seunghyup

    2015-01-01

    We report a study on transparent organic light-emitting diodes (OLEDs) with different bi-directional emission colors, enabled by color-conversion organic capping layers. Starting from a transparent blue OLED with an uncapped Ag top electrode exhibiting an average transmittance of 33.9%, a 4-(dicyanomethylene)-2-methyl-6-(4-dimethylaminostyryl)-4H-pyran (DCM)-doped tris-(8-hydroxy-quinolinato)-aluminum (Alq3) capping layer is applied to achieve color-conversion from blue to orange-red on the top side while maintaining almost unchanged device transmittance. This color-conversion capping layer does not only change the color of the top side emission, but also enhances the overall device efficiency due to the optical interaction of the capping layer with the primary blue transparent OLED. Top white emission from the transparent bi-directional OLED exhibits a correlated color temperature around 6000–7000 K, with excellent color stability as evidenced by an extremely small variation in color coordinate of Δ(x,y)=(0.002, 0.002) in the forward luminance range of 100–1000 cd m −2 . At the same time, the blue emission color of bottom side is not influenced by the color conversion capping layer, which finally results in different emission colors of the two opposite sides of our transparent OLEDs. - Highlights: • We report transparent organic light-emitting diodes (OLEDs) with different bi-directional emission colors. • Transparent blue OLED with color-conversion organic capping layers (CCL) shows orange top side emission. • Top white emission exhibits a CCT around 7000 K, with excellent color stability on a driving voltage

  2. Radiation curable coatings containing hydroxy functional polyethers and polyesters of monoethylenic acids or hydroxy esters thereof

    International Nuclear Information System (INIS)

    Kaufman, M.L.

    1978-01-01

    Relatively water insoluble hydroxy functional monoethylenic polyethers or polyesters of monoethylenic carboxylic acids or hydroxy alkyl esters thereof are formed by adducting the monoethylenic acid or its hydroxy ester with an anhydride selected from monoepoxides, lactones, or mixtures thereof in the presence of a Lewis acid catalyst, such as BF 3 etherate, at a temperature below that at which the unsaturation is consumed, typically about 30 to 70 0 C. These adducts are of low volatility and of low toxicity and can be radiation cured in admixture with polyacrylates to form coatings having improved resistance to elevated temperature exposure

  3. Diagnosis of hepatocellular carcinoma by serial determination of serum alpha-fetoprotein concentration

    Energy Technology Data Exchange (ETDEWEB)

    Yumoto, Y; Namba, T; Tanaka, Y; Taketa, K; Ohta, Y [Okayama Univ. (Japan). School of Medicine

    1976-06-01

    This communication describes the clinical significance of serum ..cap alpha..-fetoprotein (S-AFP) determined by radioimmunoassay (RIA) in the diagnosis of hepatocellular carcinoma (HCC). The sensitivity of the AFP assay with the ..cap alpha..-Feto-125 kit produced by the Dainabot RI laboratories was over 2.5 ng/ml. Reproducibility of the kit was satisfactory; coefficient of variation was 6-10% within assays and 13% between assays. The mean and standard deviation of S-AFP in the sera of 30 healthy controls was 5.6+-2.6 ng/ml. When serum with a high level of S-AFP (2.9x10/sup 5/ ng/ml) was diluted with normal horse serum, the actual concentrations of AFP in the diluted serum were consistent with those determined. Thus, normal horse serum was employed to dilute the sera with high levels of AFP. Levels of S-AFP were over 2000 ng/ml in 75.5% of 49 cases with HCC, in 0.64% of 157 patients with hepatitis and cirrhosis of the liver, and in 3.8% of 52 cases of metastatic gastric cancer to the liver. In 20 patients with HCC, levels of S-AFP ranged widely from 7.5 to 9.5x10/sup 5/ ng/ml. In serial determinations of S-AFP in the clinical courses of patients such as those with S-AFP over 2000 ng/ml, the continuous increase of AFP was strongly suggestive of the presence of HCC. In 4 of 20 cases of HCC, the S-AFP levels remained under 300 ng/ml. Histological examination of these 4 cases of HCC showed Classes I and II, but no III in Edmondson's classification. Other cases of HCC with S-AFP levels over 300 ng/ml showed Edmondson's Classes II and III.

  4. Characterization of cap binding proteins associated with the nucleus

    International Nuclear Information System (INIS)

    Patzelt, E.

    1986-04-01

    Eucaryotic mRNAs a carry 7-methylguanosine triphosphate residue (called cap structure) at their 5' terminus. The cap plays an important role in RNA recognition. Cap binding proteins (CBP) of HeLa cells were identified by photoaffinity labelling using the cap analogue γ-( 32 P)-(4-(benzoyl-phenyl)methylamido)-7-methylguanosine-5'-triphosphate (BP-m 7 GTP). Photoreaction of this cap analogue with HeLa cell initiation factors resulted in specific labelling of two polypeptides of Msub(r) 37000 and 26000. The latter was also labelled in crude initiation factors prepared from reticulocytes and is identical to the cap binding protein CBP I previously identified. These cap binding proteins were also affinity labelled in poliovirus infected cell extracts. Photoaffinity reaction with BP-m 7 GTP of whole HeLa cell homogenate showed three additional polypeptides with Msub(r) 120000, 89000 and 80000. These cap binding proteins were found to be associated with the nucleus and are therefore referred to as nuclear cap binding proteins, i.e. NCBP 1, NCBP 2 and NCBP 3. They were also present in splicing extracts. Photoaffinity labelling in these nuclear extracts was differentially inhibited by various cap analogues and capped mRNAs. Affinity chromatography on immobilized globin mRNA led to a partial separation of the three nuclear cap binding proteins. Chromatography on m 7 GTP-Sepharose resulted in a specific binding of NCBP 3. The different behaviour of the cap binding proteins suggests that they are functionally distinct and that they might be involved in different processes requiring cap recognition. (Author)

  5. Structure of the demesmaekerite, Pb/sub 2/Cu/sub 5/(SeO/sub 3/)/sub 6/(UO/sub 2/)/sub 2/(OH)/sub 6/. 2H/sub 2/O

    Energy Technology Data Exchange (ETDEWEB)

    Ginderow, D [Laboratoire de Mineralogie-Cristallographie, Universite Pierre et Marie Curie, Paris, France; Cesbron, F [Bureau de Recherches Geologiques et Minieres (BRGM), 45 - Orleans (France)

    1938-07-15

    Msub(r) = 2172, triclinic, P1-bar, a = 11.955(5), b = 10.039(4), c = 5.639(2) A, ..cap alpha.. = 89.78(4), ..beta.. = 100.36(4), ..gamma.. = 91.34(4)/sup 0/, Z = 1, V = 666 A/sup 3/, Dsub(x) = 5.42(5), Dsub(m) = 5.28(4) Mg m/sup -3/, ..mu..(Mo K..cap alpha..) = 36.57 mm/sup -1/, F(000) = 1217, T = 295 K. The final R value is 0.060 for 3329 observed reflexions. The crystal structure consists of layers of (Cu(O,OH,H/sub 2/O)/sub 6/) octahedra parallel to (010) and linked to each other by oblique chains which are formed by oxygen bridges linking uranyl and selenium ions.

  6. Cervical Cap

    Science.gov (United States)

    ... giving birth vaginally, which means the cervical cap may not fit as well. Inconsistent or incorrect use of the cervical cap increases your risk of pregnancy. For example, you may get pregnant when using the cervical cap if: ...

  7. Piperidinium 3-hydroxy-2-naphthoate

    Directory of Open Access Journals (Sweden)

    Wen-Zhu Wan

    2008-09-01

    Full Text Available The crystals of the title salt, C5H12N+·C11H7O3−, were obtained from a methanol/water solution of 3-hydroxy-2-naphthoic acid and piperidine at room temperature. In the crystal structure, the piperidinium cations display a chair conformation and link with hydroxynaphthoate anions via N—H...O and C—H...O hydrogen bonds. An intramolecular O—H...O interaction is also present.

  8. Current perspectives on the androgen 5 alpha-dihydrotestosterone (DHT) and 5 alpha-reductases in teleost fishes and amphibians.

    Science.gov (United States)

    Martyniuk, Christopher J; Bissegger, Sonja; Langlois, Valérie S

    2013-12-01

    The androgen 5 alpha-dihydrotestosterone (DHT) is a steroidogenic metabolite that has received little attention in non-mammalian species. DHT is produced by the reduction of the double-bond of testosterone by a group of enzymes called 5 alpha-reductases of which there can be multiple isoforms (i.e., srd5a1, srd5a2, and srd5a3). Data from amphibians suggest that the expression of the srd5a genes occurs in early development, and continues until adulthood; however insufficient data exist in fish species, where DHT is thought to be relatively biologically inactive. Here, we demonstrate that fathead minnow (FHM; Pimephales promelas) developing embryos and adults express srd5a enzyme isoforms. During FHM embryogenesis, both srd5a1 and srd5a3 mRNA levels were significantly correlated in expression levels while srd5a2 showed a more unique pattern of expression. In adult FHMs, males had significantly higher levels of srd5a2 in the liver and gonad compared to females. In the male and female liver, transcript levels for srd5a2 were more abundant compared to srd5a1 and srd5a3, suggesting a prominent role for srd5a2 in this tissue. Interestingly, the ovary expressed higher mRNA levels of srd5a3 than the testis. Thus, data suggest that srd5a isoforms can show sexually dimorphic expression patterns in fish. We also conducted a literature review of the biological effects observed in embryonic and adult fish and amphibians after treatments with DHT and DHT-related compounds. Treatments with DHT in teleost fishes and amphibians have resulted in unexpected biological responses that are characteristic of both androgens and anti-androgens. For example, in fish DHT can induce vitellogenin in vitro from male and female hepatocytes and can increase 17β-estradiol production from the teleost ovary. We propose, that to generate further understanding of the roles of DHT in non-mammals, studies are needed that (1) address how DHT is synthesized within tissues of fish and amphibians; (2

  9. Analytical study of zirconium and hafnium α-hydroxy carboxylates

    International Nuclear Information System (INIS)

    Terra, V.R.

    1991-01-01

    The analytical study of zirconium and hafnium α-hydroxy carboxylates was described. For this purpose dl-mandelic, dl-p-bromo mandelic, dl-2-naphthyl glycolic, and benzilic acids were prepared. These were used in conjunction with glycolic, dl-lactic, dl-2-hydroxy isovaleric, dl-2-hydroxy hexanoic, and dl-2-hydroxy dodecanoic acids in order to synthesize the zirconium(IV) and hafnium(IV) tetrakis(α-hydroxy carboxylates). The compounds were characterized by melting point determination, infrared spectroscopy, thermogravimetric analysis, calcination to oxides and X-ray diffractometry by the powder method. (C.G.C)

  10. Quantitative determination of 5-hydroxy-N-methylpyrrolidone in urine for biological monitoring of N-methylpyrrolidone exposure.

    Science.gov (United States)

    Ligocka, D; Lison, D; Haufroid, V

    2002-10-05

    The aim of this work was to validate a sensitive method for quantitative analysis of 5-hydroxy-N-methylpyrrolidone (5-HNMP) in urine. This compound has been recommended as a marker for biological monitoring of N-methylpyrrolidone (NMP) exposure. Different solvents and alternative methods of extraction including liquid-liquid extraction (LLE) on Chem Elut and solid-phase extraction (SPE) on Oasis HLB columns were tested. The most efficient extraction of 5-HNMP in urine was LLE with Chem Elut columns and dichloromethane as a solvent (consistently 22% of recovery). The urinary extracts were derivatized by bis(trimethylsilyl)trifluoroacetamide and analysed by gas chromatography-mass spectrometry (GC-MS) with tetradeutered 5-HNMP as an internal standard. The detection limit of this method is 0.017 mg/l urine with an intraassay precision of 1.6-2.6%. The proposed method of extraction is simple and reproducible. Four different m/z signal ratios of TMS-5-HNMP and tetralabelled TMS-5-HNMP have been validated and could be indifferently used in case of unexpected impurities from urine matrix. Copyright 2002 Elsevier Science B.V.

  11. Structural studies on Mannich bases of 2-Hydroxy-3,4,5,6-tetrachlorobenzene. An UV, IR, NMR and DFT study. A mini-review

    DEFF Research Database (Denmark)

    Hansen, Poul Erik; Spanget-Larsen, Jens

    2016-01-01

    Mannich bases of 2-Hydroxy-3,4,5,6-tetrachlorobenzene are chosen as an exemplary case for tautomeric Mannich bases. Molecular structures are calculated. OH stretching frequencies are rationalized based on DFT calculations. Intrinsic deuterium isotope effects on 13C chemical shifts in the M-form a...

  12. Spectrophotometric Determination of 4-Hydroxy-2-mercapto-6-methylpyrimidine Based on Aggregation of Colloidal Gold Nanoparticles

    Directory of Open Access Journals (Sweden)

    M.Reza Hormozi-Nezhad

    2014-12-01

    Full Text Available We report herein the development of a highly sensitive colorimetric method for the detection of 4-hydroxy-2-mercapto-6-methylpyrimidine (MTU which acts as an anti-thyroid drug utilizing citrate capped gold nanoparticles (Au-NPs. This thiol-containing molecule exhibits intriguing affinity with Au-NPs. The reactivity involves the displacement of the citrate shell by the thiolate shell followed by intermolecular electrostatic interactions or hydrogen-bonding between the thiolate shells. The interparticle interactions depend on ionic strength, pH and Au-NPs concentration of the solution. The interparticle interactions lead to a small change in the plasmon band around 521 nm and the formation of a new red shifted band. The calibration curve is derived from the ratio of the absorption intensity changes at 650 nm to the changes at 520 nm. It was linear in the concentration range of 5.0 × 10-7-2.75 × 10-6 M. The detection limit (3σ for MTU was found to be 1.9 × 10-7 M.

  13. Mass fragmentography of 25-hydroxy vitamin D3

    International Nuclear Information System (INIS)

    Bjoerkhem, I.; Holmberg, I.

    1978-01-01

    A mass fragmentographic assay of 25-hydroxy vitamin D 3 has been developed. [26- 2 H 3 ]-labelled vitamin D 3 is used as internal standard. A fixed amount of the standard is added to a fixed amount of serum or incubation mixture. 25-Hydroxy vitamin D 3 is extracted and the 3-t -butyldimethylsilyl derivation of 25-hydroxy vitamin D 3 is prepared. The latter is purified by means of thin layer chromatography. A trimethylsilyl group is introduced in position 25 prior to analysis by gas chromatography/mass spectrometry. The molecular ion at m/e 586 for unlabelled and m/e 589 for deuterium labelled 3-t-butyldimethylsilyl/25-trimethylsilyl derivative of 25-hydroxy vitamin D 3 are used in the analysis. The assay is designed to determine a few nanograms of 25-hydroxy vitamin D 3 . It has been used for the determination of 25-hydroxy vitamin D 3 in blood serum. The mean value for 25-hydroxy vitamin D 3 obtained from 12 healthy men and women was 21 ng/ml. The relative standard deviation of the method was about 3 %. The assay has also been used to determine the rate of 25-hydroxylation of vitamin D 3 in mitrochondrial fractions of rat liver. (Auth.)

  14. Impact of x-ray dose on the response of CR-39 to 1–5.5 MeV alphas

    Energy Technology Data Exchange (ETDEWEB)

    Rojas-Herrera, J., E-mail: jimmy06@mit.edu; Rinderknecht, H. G.; Zylstra, A. B.; Gatu Johnson, M.; Orozco, D.; Rosenberg, M. J.; Sio, H.; Seguin, F. H.; Frenje, J. A.; Li, C. K.; Petrasso, R. D. [Plasma Science and Fusion Center, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139 (United States)

    2015-03-15

    The CR-39 nuclear track detector is used in many nuclear diagnostics fielded at inertial confinement fusion (ICF) facilities. Large x-ray fluences generated by ICF experiments may impact the CR-39 response to incident charged particles. To determine the impact of x-ray exposure on the CR-39 response to alpha particles, a thick-target bremsstrahlung x-ray generator was used to expose CR-39 to various doses of 8 keV Cu-K{sub α} and K{sub β} x-rays. The CR-39 detectors were then exposed to 1–5.5 MeV alphas from an Am-241 source. The regions of the CR-39 exposed to x-rays showed a smaller track diameter than those not exposed to x-rays: for example, a dose of 3.0 ± 0.1 Gy causes a decrease of (19 ± 2)% in the track diameter of a 5.5 MeV alpha particle, while a dose of 60.0 ± 1.3 Gy results in a decrease of (45 ± 5)% in the track diameter. The reduced track diameters were found to be predominantly caused by a comparable reduction in the bulk etch rate of the CR-39 with x-ray dose. A residual effect depending on alpha particle energy is characterized using an empirical formula.

  15. Effects of glutamic acid analogues on identifiable giant neurones, sensitive to beta-hydroxy-L-glutamic acid, of an African giant snail (Achatina fulica Férussac).

    Science.gov (United States)

    Nakajima, T.; Nomoto, K.; Ohfune, Y.; Shiratori, Y.; Takemoto, T.; Takeuchi, H.; Watanabe, K.

    1985-01-01

    The effects of the seven glutamic acid analogues, alpha-kainic acid, alpha-allo-kainic acid, domoic acid, erythro-L-tricholomic acid, DL-ibotenic acid, L-quisqualic acid and allo-gamma-hydroxy-L-glutamic acid were examined on six identifiable giant neurones of an African giant snail (Achatina fulica Férussac). The neurones studied were: PON (periodically oscillating neurone), d-RPLN (dorsal-right parietal large neurone), VIN (visceral intermittently firing neurone), RAPN (right anterior pallial neurone), FAN (frequently autoactive neurone) and v-RCDN (ventral-right cerebral distinct neurone). Of these, d-RPLN and RAPN were excited by the two isomers (erythro- and threo-) of beta-hydroxy-L-glutamic acid (L-BHGA), whereas PON, VIN, FAN and v-RCDN were inhibited. L-Glutamic acid (L-Glu) had virtually no effect on these neurones. alpha-Kainic acid and domoic acid showed marked excitatory effects, similar to those of L-BHGA, on d-RPLN and RAPN. Their effective potency quotients (EPQs), relative to the more effective isomer of L-BHGA were: 0.3 for both substances on d-RPLN, and 1 for alpha-kainic acid and 3-1 for domoic acid on RAPN. alpha-Kainic acid also had excitatory effects on FAN and v-RCDN (EPQ for both: 0.3), which were inhibited by L-BHGA but excited by gamma-aminobutyric acid (GABA). Erythro-L-tricholomic acid showed marked effects, similar to those of L-BHGA, on VIN (EPQ: 0.3) and RAPN (EPQ: 3-1), but produced weaker effects on PON and d-RPLN (EPQ: 0.1). DL-Ibotenic acid produced marked effects, similar to those of L-BHGA, on PON, VIN (EPQ for both: 1) and RAPN (EPQ: 1-0.3), but had weak effects on d-RPLN (EPQ: less than 0.1) and FAN (EPQ: 0.1). It had excitatory effects on v-RCDN (EPQ: 0.1). This neurone was inhibited by L-BHGA but excited by GABA. L-Quisqualic acid showed the same effects as L-BHGA on all of the neurones examined (EPQ range 30-0.1). It was the most potent of the compounds tested on RAPN (EPQ: 30-10), FAN (EPQ: 30) and v-RCDN (EPQ: 3). alpha

  16. Total synthesis of ciguatoxin and 51-hydroxyCTX3C.

    Science.gov (United States)

    Inoue, Masayuki; Miyazaki, Keisuke; Ishihara, Yuuki; Tatami, Atsushi; Ohnuma, Yuyu; Kawada, Yuuya; Komano, Kazuo; Yamashita, Shuji; Lee, Nayoung; Hirama, Masahiro

    2006-07-26

    Ciguatoxins, the principal causative toxins of ciguatera seafood poisoning, are large ladder-like polycyclic ethers with the 13 ether rings ranging from five- to nine-membered. In this paper, we describe the total synthesis of the two most toxic members of the ciguatoxin family, ciguatoxin 1 and 51-hydroxyCTX3C 2, based on a unified synthetic strategy. The key features in our syntheses were (i) direct construction of the O,S-acetal from the corresponding left and right wing fragments (3, 4, 14); (ii) stereo- and chemoselective radical reaction of the alpha-oxyradical with pentafluorophenyl acrylate to achieve cyclization of the seven-membered G-ring; (iii) ring-closing metathesis reaction to build the nine-membered F-ring; and (iv) an efficient protective group strategy using the oxidatively removable 2-naphthylmethyl groups.

  17. Crystal structure of (Z-3-benzyloxy-6-[(2-hydroxy-5-methylanilinomethylidene]cyclohexa-2,4-dien-1-one

    Directory of Open Access Journals (Sweden)

    Nadir Ghichi

    2014-09-01

    Full Text Available In the title Schiff base compound, C21H19NO3, the conformation about the C=C bond is Z. The N—H group and carbonyl O atom form an intramolecular N—H...O hydrogen bond with an S(6 ring motif. The benzyloxy ring and the 2-hydroxy-5-methylphenyl ring are inclined to the central six-membered ring by 13.68 (9 and 9.13 (8°, respectively, and to one another by 21.95 (9°. In the crystal, molecules are linked by O—H...O hydrogen bonds, forming helical chains along [010].

  18. Identification of di- and tri-substituted hydroxy and ketone metabolites of delta1-tetrahydrocannabinol in mouse liver.

    Science.gov (United States)

    Harvey, D J; Martin, B R; Paton, W D

    1977-08-01

    In vivo liver metabolites of delta1-tetrahydrocannabinol (delta1-THC) were examined with a gas chromatograph--mass spectrometer--computer system as trimethylsilyl (TMS), [2H9]TMS and methyloxime-TMS derivatives. In addition to the reported monohydroxy, acid, and hydroxyacid metabolites, the following multiply substituted metabolites were identified: 2'',7-, 3'', 7-, and 6beta,7-dihydroxy-delta1-THC; 2'',6alpha,7-, and 3'',6alpha,7-trihydroxy-delta1-THC; 2''-, 3''-, and 7-hydroxy-6-oxo-delta1-THC, and 2'',7- and 3'',7-dihydroxy-6-oxo-delta1-THC. The ketones and hydroxyacids were reduced to common alcohols with lithium aluminium deuteride and the number of deuterium atoms in the product was used to distinguish the metabolic alcohols from those produced by reduction.

  19. 2-[(2-{Bis[2-(2-hydroxy-5-nitrobenzylideneaminoethyl]amino}ethyliminomethyl]-4-nitrophenol acetonitrile monosolvate

    Directory of Open Access Journals (Sweden)

    Kwang Ha

    2010-12-01

    Full Text Available In the title compound, C27H27N7O9·CH3CN, the three nitro groups of the polydentate tripodal Schiff base are located approximately parallel to their respective carrier benzene rings, making dihedral angles of 3.9 (4, 5.0 (4 and 6.3 (4°. Intramolecular O—H...N hydrogen bonds between the hydroxy O atoms and the imine N atoms, with O...N distances in the range 2.607 (3–2.665 (3 Å, form nearly planar six-membered rings. In the crystal, weak intermolecular C—H...O and C—H...N hydrogen bonds occur and several intra- and intermolecular π–π interactions are present between adjacent benzene rings, with a shortest centroid–centroid distance of 3.507 (2 Å.

  20. Urinary excretion of androgen metabolites, comparison with excretion of radioactive metabolites after injection of (4-/sup 14/C)testosterone. Influence of age

    Energy Technology Data Exchange (ETDEWEB)

    Deslypere, J P; Sayed, A; Vermeulen, A [Department of Internal Medicine, Section of Endocrinology, State University Academic Hospital, De Pintelaan, 135, Ghent, Belgium; Wiers, P W [Department of Internal Medicine, Section of Pneumology, State University Academic Hospital, The Netherlands

    1981-01-01

    The influence of age on the metabolic pattern of (4-/sup 14/C)testosterone was studied in 20 young and 8 elderly males and compared to the metabolic pattern of endogenous androgens; the latter was also studied in 16 young and 8 elderly women. In both young and elderly males, androsterone and aetiocholanolone glucuronide represent 65% of (4-/sup 14/C)testosterone metabolites: together with their suephoconjugates as well as with 5..cap alpha..- and 5..beta..-androstane-3..cap alpha.., 17..beta..-diol they represent even more than 75% of total urinary metabolites. The 5..cap alpha../5..beta.. ratio of metabolites of (4-/sup 14/C)testosterone was significantly (P<0.01) correlated with the 5..cap alpha../5..beta.. ratio of the metabolites of the endogenous androgens, mainly dehydroepiandrosterone and androstenedione. The 5..cap alpha../5..beta.. ratio of (4-/sup 14/C)testosterone metabolites was generally higher than the ratio of metabolites of endogenous androgens, suggesting that the transformation of T to ring A saturated metabolites occurs at least partially in another compartment than the transformation of DHEA to these metabolites. For both (4-/sup 14/C)testosterone and endogenous androgen metabolites we observed a statistically significant reduction of the 5..cap alpha../5..beta.. ratio with age, a general phenomenon in both males and females. This reduction concern also 11-OH-androst-4-ene-3.17-dione metabolism. Neither sex hormone levels, nor specific binding seems to determine this age dependent shift; neither is there convincing evidence for latent hypothyroisism or liver dysfunction in the elderly. An age associated primary decrease of the 5..cap alpha..-reductase activity seems the most likely explanation.

  1. Dual Effects of Alpha-Hydroxy Acids on the Skin

    Directory of Open Access Journals (Sweden)

    Sheau-Chung Tang

    2018-04-01

    Full Text Available AHAs are organic acids with one hydroxyl group attached to the alpha position of the acid. AHAs including glycolic acid, lactic acid, malic acid, tartaric acid, and citric acid are often used extensively in cosmetic formulations. AHAs have been used as superficial peeling agents as well as to ameliorate the appearance of keratoses and acne in dermatology. However, caution should be exercised in relation to certain adverse reactions among patients using products with AHAs, including swelling, burning, and pruritus. Whether AHAs enhance or decrease photo damage of the skin remains unclear, compelling us to ask the question, is AHA a friend or a foe of the skin? The aim of this manuscript is to review the various biological effects and mechanisms of AHAs on human keratinocytes and in an animal model. We conclude that whether AHA is a friend or foe of human skin depends on its concentration. These mechanisms of AHAs are currently well understood, aiding the development of novel approaches for the prevention of UV-induced skin damage.

  2. Cap-independent translation of plant viral RNAs.

    Science.gov (United States)

    Kneller, Elizabeth L Pettit; Rakotondrafara, Aurélie M; Miller, W Allen

    2006-07-01

    The RNAs of many plant viruses lack a 5' cap and must be translated by a cap-independent mechanism. Here, we discuss the remarkably diverse cap-independent translation elements that have been identified in members of the Potyviridae, Luteoviridae, and Tombusviridae families, and genus Tobamovirus. Many other plant viruses have uncapped RNAs but their translation control elements are uncharacterized. Cap-independent translation elements of plant viruses differ strikingly from those of animal viruses: they are smaller (translation factors, and speculate on their mechanism of action and their roles in the virus replication cycle. Much remains to be learned about how these elements enable plant viruses to usurp the host translational machinery.

  3. Pyridinium 5-[(1,3-diethyl-6-hydroxy-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl(2-methoxyphenylmethyl]-1,3-diethyl-4,6-dioxo-2-thioxopyrimidin-5-ide

    Directory of Open Access Journals (Sweden)

    Abdullah Mohamed Asiri

    2009-08-01

    Full Text Available 1,3-Diethyl-2-thiobarbituric acid reacts with 2-anisaldehyde to form the Michael addition product 2-anisylbis(1,3-diethyl-2-thiobarbitur-5-ylmethanate, which crystallizes as the title pyridinium salt, C5H6N+·C24H29N4O5S2−, when it reacts with the pyridine used to catalyse the reaction. There are two independent ion pairs in the crystal structure. The anion features a methine C atom connected to three six-membered rings; one of the rings carries a hydroxy group, which engages in hydrogen bonding with the carbonyl group belonging to another ring. The monoclinic unit cell emulates an orthorhombic unit cell, and is a twin with a minor twin component of 35%.

  4. Description of analytical method and clinical utility of measuring serum 7-alpha-hydroxy-4-cholesten-3-one (7aC4) by mass spectrometry.

    Science.gov (United States)

    Donato, Leslie J; Lueke, Alan; Kenyon, Stacy M; Meeusen, Jeffrey W; Camilleri, Michael

    2018-02-01

    Imbalance of bile acids (BA) homeostasis in the gastrointestinal tract can lead to chronic diarrhea or constipation when BA in the colon are in excess or low, respectively. Since both disturbances of bowel function can result from other etiologies, identifying BA imbalance is important to tailor treatment strategies. Serum concentrations of 7-alpha-hydroxy-4-cholesten-3-one (7aC4), a precursor in bile acid synthesis, reflect BA homeostasis. Here we describe a method to accurately measure serum 7aC4 and evaluate the clinical utility in patients with diarrhea or constipation phenotypes. Serum 7aC4 is measured after acetonitrile protein precipitation using C18 liquid chromatography, tandem mass spectrometry, and deuterium-labeled 7aC4 internal standard. Assay performance including linearity, precision, and accuracy was assessed using waste serum samples. The reference interval was established in healthy individuals without BA-altering conditions or medications. Clinical performance was assessed in patients with irritable bowel syndrome. The method precisely and accurately measured 7aC4 in human serum from 1.4-338ng/mL with no ion suppression or interference from related 7-keto-cholesterol. Central 95th percentile reference interval was 2.5-63.2ng/mL. Lower serum 7aC4 was found in patients with constipation with sensitivity/specificity of 79%/55% compared to healthy controls. Higher 7aC4 was found in patients with bile acid diarrhea (BAD) compared to those without BAD with sensitivity/specificity of 82%/53%. We have developed a sensitive and precise assay for measuring the concentration of 7aC4 in serum. The assay can be used to screen for diarrhea caused by bile acid malabsorption. Copyright © 2017 The Canadian Society of Clinical Chemists. Published by Elsevier Inc. All rights reserved.

  5. Effects of rooting and tree growth of selected woodland species on cap integrity in a mineral capped landfill site.

    Science.gov (United States)

    Hutchings, T R; Moffat, A J; Kemp, R A

    2001-06-01

    The above and below ground growth of three tree species (Alnus glutinosa, Pinus nigra var. maritima and Acer pseudoplatanus) was studied on a containment landfill site at Waterford, Hertfordshire, UK. Tree root architecture was studied using soil inspection pits excavated next to 12 trees of each species and mapped in detail. Tree height was related to soil thickness over the compacted mineral cap. No roots entered the cap where soil thickness was 1.3 m, but a few roots, especially of alder, were observed within it when the soil cover was 1.0 m or less. Micromorphological analysis of undisturbed samples of the mineral cap suggested that roots exploited weaknesses in the cap rather than actively causing penetration into it. Alder roots were more tolerant of anaerobic conditions within the cap than the other species examined. The results confirm that mineral caps should be covered by 1.5 m of soil or soil-forming material if tree establishment is intended over a restored landfill site, unless protected by other parts of a composite capping system.

  6. Purification of the labeled cyanogen bromide peptides of the. cap alpha. polypeptide from sodium and potassium ion-activated adenosinetriphosphatase modified with N-(/sup 3/H)ethylmaleimide

    Energy Technology Data Exchange (ETDEWEB)

    Le, D.T.

    1985-01-01

    Sodium and potassium ion-activated adenosinetriphosphatase, isolated from canine kidney, was reacted with N-(/sup 3/H)ethylmaleimide under three different conditions, defined by particular concentrations of ligands for the enzyme, such that after the same amount of time the remaining activity of then enzyme varied from 90% to 30%. The conformation of the enzyme also differed among the three conditions. In all cases, the ..cap alpha..-polypeptide was purified and subjected to cyanogen bromide digestion. Two distinct, radioactive peptides were separated by gel filtration of the cyanogen bromide digest on a column of Sephadex LH-60 equilibrated with 95% ethanol: 88% formic acid:4:1. One of the radioactive peptides was shown to contain the sulfhydryl residue whose reaction with N-ethylmaleimide inactivates the enzyme. The other radioactive peptide contained a sulfhydryl residue that seems to react with N-ethylmaleimide only when the binding site for ATP is not occupied. Alkylation of this residue, however, does not result in inactivation of enzyme. Both peptides were purified further by high-pressure liquid chromatography, and their amino-terminal sequences were determined by the manual dansyl-Edman or solid-phase techniques. The peptide containing the sulfhydryl protected by ATP has, as its amino terminus, the lysine that reacts exclusively with fluorescein-5'-isothiocyanate.

  7. rac-1-[6-Hydroxy-4-(4-methoxyphenyl-3,6-dimethyl-4,5,6,7-tetrahydro-2H-indazol-5-yl]ethanone

    Directory of Open Access Journals (Sweden)

    Konstantin A. Potekhin

    2013-02-01

    Full Text Available The title compound, C18H22N2O3, represents a (4S,5R,6S-stereoisomer, crystallizing as a racemate in a centrosymmetric space group. The six-membered aliphatic ring adopts a half-chair conformation, with the hydroxy- and acetyl-substituted C atoms deviating by 0.458 (2 and −0.366 (2 Å, respectively, from the plane defined by other four ring atoms. The pyrazole ring is essentially planar [r.m.s deviation = 0.004 (2 Å]. In the crystal, the molecules are linked into chains along the b axis by N—H...N hydrogen bonds. The chains are linked by O—H...N hydrogen bonds into layers parallel to the bc plane.

  8. Etiologic related studies of ultraviolet light-mediated carcinogenesis

    Energy Technology Data Exchange (ETDEWEB)

    Black, H S; Chan, J T

    1976-01-01

    Comparisons were made of cholesterol-5..cap alpha.. 6..cap alpha..-epoxide (CAE) levels in skin of hairless mice maintained on a regular or antioxidant supplemented diet and receiving chronic ultraviolet light (UVL) radiation over an 18-week period. Cholesterol-5..cap alpha.., 6..cap alpha..-epoxide levels in skin of animals on antioxidant supplemented diet, while reaching a peak four weeks after that of animals on regular diet, thereafter were consistently higher. Dietary antioxidants nevertheless had an inhibitory effect on UVL-induced tumors. These data are inconsistent with the theory of CAE involvement as an ultimate carcinogen in UVL-mediated carcinogenesis.

  9. Evaluation of management alternatives for LWR hulls and caps

    International Nuclear Information System (INIS)

    Chaudon, L.; Mehling, O.; Cecille, L.; Thiels, G.; Kowa, S.

    1993-01-01

    Hulls and caps resulting from the reprocessing of LWR spent fuels represent one of the major sources of alpha-bearing solid waste generated during the nuclear fuel cycle. The Commission of the European Communities has undertaken considerable R and D efforts on the development of advanced treatment and conditioning methods for this type of waste. In view of the encouraging results achieved, the Commission launched a theoretical assessment study on cladding waste management. Six practical or potential schemes were identified and elaborated: direct cementation, decontamination prior to cementation, rolling before cementation, rolling followed by embedding in graphite, compaction, and melting in a cold crucible. The economic aspects of each management option were also investigated. This included the assessment of the plant (treatment, conditioning and interim storage), transport and disposal costs. Further consideration will be required to define the best management option for 'cap' wastes. Transport and disposal costs will also require further analysis from an industrial standpoint

  10. Cradle Cap (For Parents)

    Science.gov (United States)

    ... Safe Videos for Educators Search English Español Cradle Cap (Infantile Seborrheic Dermatitis) KidsHealth / For Parents / Cradle Cap ( ... many babies develop called cradle cap. About Cradle Cap Cradle cap is the common term for seborrheic ...

  11. Selective inhibition of sheep kidney 11 beta-hydroxysteroid dehydrogenase isoform 2 activity by 5 alpha-reduced (but not 5 beta) derivatives of adrenocorticosteroids.

    Science.gov (United States)

    Latif, S A; Sheff, M F; Ribeiro, C E; Morris, D J

    1997-02-01

    We have previously reported that 5 alpha and 5 beta pathways of steroid metabolism are controlled in vivo by dietary Na+ and glycyrrhetinic acid, see Gorsline et al. 1988; Latif et al. 1990. The present investigations provide evidence supporting the suggestion that endogenous substances may regulate the glucocorticoid inactivating isoenzymes, 11 beta-HSD (hydroxysteroid dehydrogenase) 1 (liver) and 11 beta-HSD2 (kidney). The activity of 11 beta-HSD is impaired in essential hypertension, following licorice ingestion, and in patients with apparent mineralocorticoid excess where 11 beta-HSD2 is particularly affected. In all three conditions, excretion of the less common 5 alpha metabolites is elevated in urine. We now report on the differential abilities of a series of Ring A reduced (5 alpha and 5 beta) adrenocorticosteroid and progesterone metabolites to inhibit these isoenzymes. Using liver microsomes with NADP+ as co-factor (11 beta-HSD1), and sheep kidney microsomes with NAD+ as co-factor (11 beta-HSD2), we have systematically investigated the abilities of a number of adrenocorticosteroids and their derivatives to inhibit the individual isoforms of 11 beta-HSD. A striking feature is the differential sensitivity of the two isoenzymes to inhibition by 5 alpha and 5 beta derivatives. 11 beta-HSD1 is inhibited by both 5 alpha and certain 5 beta derivatives. 11 beta-HSD-2 was selectively inhibited only by 5 alpha derivatives: 5 beta derivatives were without inhibitory activity toward this isoform of 11 beta-HSD. These results indicate the importance of the structural conformation of the A and B Rings in conferring specific inhibitory properties on these compounds. In addition, we discuss the effects of additions or substitutions of other functional groups on the inhibitory potency of these steroid molecules against 11 beta-HSD1 and 11 beta-HSD2.

  12. Inhibition of steroid 5 alpha-reductase by specific aliphatic unsaturated fatty acids.

    Science.gov (United States)

    Liang, T; Liao, S

    1992-01-01

    Human or rat microsomal 5 alpha-reductase activity, as measured by enzymic conversion of testosterone into 5 alpha-dihydrotestosterone or by binding of a competitive inhibitor, [3H]17 beta-NN-diethulcarbamoyl-4-methyl-4-aza-5 alpha-androstan-3-one ([3H]4-MA) to the reductase, is inhibited by low concentrations (less than 10 microM) of certain polyunsaturated fatty acids. The relative inhibitory potencies of unsaturated fatty acids are, in decreasing order: gamma-linolenic acid greater than cis-4,7,10,13,16,19-docosahexaenoic acid = cis-6,9,12,15-octatetraenoic acid = arachidonic acid = alpha-linolenic acid greater than linoleic acid greater than palmitoleic acid greater than oleic acid greater than myristoleic acid. Other unsaturated fatty acids such as undecylenic acid, erucic acid and nervonic acid, are inactive. The methyl esters and alcohol analogues of these compounds, glycerols, phospholipids, saturated fatty acids, retinoids and carotenes were inactive even at 0.2 mM. The results of the binding assay and the enzymic assay correlated well except for elaidic acid and linolelaidic acid, the trans isomers of oleic acid and linoleic acid respectively, which were much less active than their cis isomers in the binding assay but were as potent in the enzymic assay. gamma-Linolenic acid had no effect on the activities of two other rat liver microsomal enzymes: NADH:menadione reductase and glucuronosyl transferase. gamma-Linolenic acid, the most potent inhibitor tested, decreased the Vmax. and increased Km values of substrates, NADPH and testosterone, and promoted dissociation of [3H]4-MA from the microsomal reductase. gamma-Linolenic acid, but not the corresponding saturated fatty acid (stearic acid), inhibited the 5 alpha-reductase activity, but not the 17 beta-dehydrogenase activity, of human prostate cancer cells in culture. These results suggest that unsaturated fatty acids may play an important role in regulating androgen action in target cells. PMID:1637346

  13. Thermogravimetry of alpha, omega-diaminoalkanes used in synthesizing zsm-5

    CSIR Research Space (South Africa)

    Howden, MG

    1993-04-01

    Full Text Available Thermogravimetry was determined on a series of alpha, omega-diaminoalkanes, in which the alkane chain contained from three to eight carbon atoms that were located in zeolite ZSM-5 during synthesis. Of the series, 1, 6-diaminohexane functions best...

  14. Personal computer based system to evaluate J-integral by a single specimen unloading compliance method: Pt. 2. Results on A533B Class I steel and CORONA-5

    Energy Technology Data Exchange (ETDEWEB)

    Narendrnath, K R; Margolin, H; Jung, Y H; Godavarti, P S; Murty, K L

    1988-01-01

    A personal computer based single specimen unloading technique has been demonstrated using a nuclear grade pressure vessel material, A533B Class I steel, and an ..cap alpha..-..beta.. titanium alloy, CORONA-5. Experimental parameters investigated in the case of steel include the effect of test temperature, loading rate and neutron irradiation. Results revealed the effect of dynamic strain aging (DSA) as a drop in the critical crack initiation fracture toughness (Jsub(q)); the minimum in Jsub(q) shifts to higher temperatures at higher test speeds as predicted from DSA models. In CORONA-5, the effects of microstructure and heat treatment for two different sizes of equiaxed ..cap alpha.. morphology in a ..beta..-matrix heat treated to different yield strengths were investigated. It is found that the observed higher values of Jsub(q) and tearing modulus result from a greater tortuosity of the crack path and ease of crack blunting. The largest increase in Jsub(q) occurred in fine equiaxed ..cap alpha.. microstructure aged to a nominal yield strength of 896 MPa. Results reveal potential application of the low cost technique for determining fracture toughness of engineering materials.

  15. (E,Z)-3-(3',5'-Dimethoxy-4'-hydroxy-benzylidene)-2-indolinone blocks mast cell degranulation.

    Science.gov (United States)

    Kiefer, S; Mertz, A C; Koryakina, A; Hamburger, M; Küenzi, P

    2010-05-12

    (E,Z)-3-(3',5'-Dimethoxy-4'-hydroxy-benzylidene)-2-indolinone (indolinone) is an alkaloid that has been identified as a pharmacologically active compound in extracts of the traditional anti-inflammatory herb Isatis tinctoria. Indolinone has been shown to inhibit compound 48/80-induced mast cell degranulation in vitro. Application of indolinone to bone marrow derived mast cells showed that it was uniformly distributed in the cytoplasm and that cellular uptake was terminated within minutes. Pre-treatment of IgE-sensitized mast cells with 100nM indolinone rendered them insensitive against FcvarepsilonRI-receptor dependent degranulation. However, upstream signalling induced by antigen such as activation of PI3-K and MAPK remained unaffected. We conclude that indolinone blocks mast cell degranulation at the level of granule exocitosis with an IC(50) of 54nm.

  16. Effect of Terbuthylazine-2-hydroxy at Environmental Concentrations on Early Life Stages of Common Carp (Cyprinus carpio L.

    Directory of Open Access Journals (Sweden)

    Josef Velisek

    2014-01-01

    Full Text Available The aim of the study was to investigate effects of the triazine’s herbicide terbuthylazine-2-hydroxy on early life stage of common carp (Cyprinus carpio L. through antioxidant indices, mortality, growth, development, and histopathology. Based on accumulated mortality in the experimental groups, lethal concentrations of terbuthylazine-2-hydroxy were estimated at 35-day LC50 = 10.9 mg/L terbuthylazine-2-hydroxy. By day 15, fish were exposed to 3.5 mg/L and by day 26, fish were exposed to 0.0029 mg/L; real environmental concentration in Czech rivers, 0.07 mg/L, 1.4 mg/L, and 3.5 mg/L terbuthylazine-2-hydroxy, showed significantly lower mass and total length compared with controls. Based on inhibition of growth in the experimental groups, lowest observed effect concentration (LOEC = 0.002 mg/L terbuthylazine-2-hydroxy and no observed effect concentration (NOEC = 0.0001 mg/L terbuthylazine-2-hydroxy. No significant negative effects on hatching or embryo viability were demonstrated at the concentrations tested, but significant differences in early ontogeny among groups were noted. Fish from the two highest tested concentrations showed a dose-related delay in development compared with the controls. Total superoxide dismutase (SOD activity was significant lower in all groups testedly for terbuthylazine-2-hydroxy compared with the control group. At concentrations of 1.4 and 3.5 mg/L damage to caudal kidney tubules when compared to control fish was found.

  17. The 5 Alpha-Reductase Isozyme Family: A Review of Basic Biology and Their Role in Human Diseases

    Directory of Open Access Journals (Sweden)

    Faris Azzouni

    2012-01-01

    Full Text Available Despite the discovery of 5 alpha-reduction as an enzymatic step in steroid metabolism in 1951, and the discovery that dihydrotestosterone is more potent than testosterone in 1968, the significance of 5 alpha-reduced steroids in human diseases was not appreciated until the discovery of 5 alpha-reductase type 2 deficiency in 1974. Affected males are born with ambiguous external genitalia, despite normal internal genitalia. The prostate is hypoplastic, nonpalpable on rectal examination and approximately 1/10th the size of age-matched normal glands. Benign prostate hyperplasia or prostate cancer does not develop in these patients. At puberty, the external genitalia virilize partially, however, secondary sexual hair remains sparse and male pattern baldness and acne develop rarely. Several compounds have been developed to inhibit the 5 alpha-reductase isozymes and they play an important role in the prevention and treatment of many common diseases. This review describes the basic biochemical properties, functions, tissue distribution, chromosomal location, and clinical significance of the 5 alpha-reductase isozyme family.

  18. Chemical synthesis of highly size-confined triethylamine-capped ...

    Indian Academy of Sciences (India)

    2018-03-23

    Mar 23, 2018 ... TiO2 nanoparticles and its dye-sensitized solar cell performance .... Figure 5. Formation mechanism of TEA-capped and uncapped TiO2 nanoparticles. ... this research work, synthesized TEA-capped TiO2 nanopar- ticles were ...

  19. Conversion of /sup 3/H-testosterone to dihydrotestosterone in human hypertrophic prostatic tissue

    Energy Technology Data Exchange (ETDEWEB)

    Baranowska, B; Zgliczynski, [Centre of Postgraduate Medical Education, Warsaw (Poland). Clinic of Endocrinology

    1979-12-01

    The aim of the study was to develop a simple method for the determination of the conversion of testosterone to 5..cap alpha..-dihydrotestosterone (5..cap alpha..-DHT) after incubation of human hypertrophic prostatic tissue with /sup 3/H-testosterone. The mean conversion rate of /sup 3/H-testosterone to 5..cap alpha..-DHT in hypertrophic prostatic tissue was found to be higher than in normal and carcinomatous tissue. The results indicate that androgen metabolism in the hypertrophic prostatic gland is enhanced.

  20. Analysis of Prescriptions of Alpha-Blockers and Phosphodiesterase 5 Inhibitors from the Urology Department and Other Departments

    Directory of Open Access Journals (Sweden)

    Dong Hyuk Kang

    2011-12-01

    Full Text Available PurposeWe analyzed the prescriptions of alpha-blockers and phosphodiesterase 5 inhibitors (PDE5Is in the urology department as well as in other departments of the general hospital.MethodsWe investigated the frequency of prescription of alpha-blockers and PDE5Is from 3 general hospitals from January 1, 2007 to December 31, 2009. For alpha-blockers, data were collected from patients to whom alpha-blockers were prescribed from among patients recorded as having benign prostatic hyperplasia according to the 5th Korean Standard Classification of Diseases. For PDE5Is, data were collected from patients to whom PDE5Is were prescribed by the urology department and by other departments. Alpha-blockers were classified into tamsulosin, alfuzosin, doxazosin, and terazosin, whereas PDE5Is were classified into sildenafil, tadalafil, vardenafil, udenafil, and mirodenafil.ResultsAlpha-blockers were prescribed to 11,436 patients in total over 3 years, and the total frequency of prescriptions was 68,565. Among other departments, the nephrology department had the highest frequency of prescription of 3,225 (4.7%, followed by the cardiology (3,101, 4.5%, neurology (2,576, 3.8%, endocrinology (2,400, 3.5%, pulmonology (1,102, 1.6%, and family medicine (915, 1.3% departments in order. PDE5Is were prescribed to 2,854 patients in total over 3 years, and the total frequency of prescriptions was 10,558. The prescription frequency from the urology department was 4,900 (46.4%. Among other departments, the endocrinology department showed the highest prescription frequency of 3,488 (33.0%, followed by the neurology (542, 5.1%, cardiology (467, 4.4%, and family medicine (407, 3.9% departments in order.ConclusionsA high percentage of prescriptions of alpha-blockers and PDE5Is were from other departments. For more specialized medical care by urologists is required in the treatment of lower urinary tract symptoms and erectile dysfunction.

  1. Reprint of "Current perspectives on the androgen 5 alpha-dihydrotestosterone (DHT) and 5 alpha-reductases in teleost fishes and amphibians".

    Science.gov (United States)

    Martyniuk, Christopher J; Bissegger, Sonja; Langlois, Valérie S

    2014-07-01

    The androgen 5 alpha-dihydrotestosterone (DHT) is a steroidogenic metabolite that has received little attention in non-mammalian species. DHT is produced by the reduction of the double-bond of testosterone by a group of enzymes called 5 alpha-reductases of which there can be multiple isoforms (i.e., srd5a1, srd5a2, and srd5a3). Data from amphibians suggest that the expression of the srd5a genes occurs in early development, and continues until adulthood; however insufficient data exist in fish species, where DHT is thought to be relatively biologically inactive. Here, we demonstrate that fathead minnow (FHM; Pimephales promelas) developing embryos and adults express srd5a enzyme isoforms. During FHM embryogenesis, both srd5a1 and srd5a3 mRNA levels were significantly correlated in expression levels while srd5a2 showed a more unique pattern of expression. In adult FHMs, males had significantly higher levels of srd5a2 in the liver and gonad compared to females. In the male and female liver, transcript levels for srd5a2 were more abundant compared to srd5a1 and srd5a3, suggesting a prominent role for srd5a2 in this tissue. Interestingly, the ovary expressed higher mRNA levels of srd5a3 than the testis. Thus, data suggest that srd5a isoforms can show sexually dimorphic expression patterns in fish. We also conducted a literature review of the biological effects observed in embryonic and adult fish and amphibians after treatments with DHT and DHT-related compounds. Treatments with DHT in teleost fishes and amphibians have resulted in unexpected biological responses that are characteristic of both androgens and anti-androgens. For example, in fish DHT can induce vitellogenin in vitro from male and female hepatocytes and can increase 17β-estradiol production from the teleost ovary. We propose, that to generate further understanding of the roles of DHT in non-mammals, studies are needed that (1) address how DHT is synthesized within tissues of fish and amphibians; (2

  2. Cradle Cap: Treatment

    Science.gov (United States)

    Cradle cap Treatment Cradle cap usually doesn't require medical treatment. It clears up on its own within a few months. In the meantime, wash ... tips can help you control and manage cradle cap. Gently rub your baby's scalp with your fingers ...

  3. Synthesis and investigation of solvent effects on the ultraviolet absorption spectra of 5-substituted-4-methyl-3-cyano-6-hydroxy-2-pyridones

    Directory of Open Access Journals (Sweden)

    NATASA V. VALENTIC

    2001-08-01

    Full Text Available A number of 5-substituted-4-methyl-3-cyano-6-hydroxy-2-pyridones from cyanoacetamide and the corresponding alkyl ethyl acetoacetates were synthesized according to modified literature procedures. The alkyl ethyl acetoacetates were obtained by the reaction of C-alkylation of ethyl acetoacetate. An investigation of the reaction conditions for the synthesis of 4-methyl-3-cyano-6-hydroxy-2-pyridone from cyanoacetamide and ethyl acetoacetate in eight different solvents was also performed. The ultraviolet absorption spectra of synthesized pyridones were measured in nine different solvents in the range 200–400 nm. The effects of solvent polarity and hydrogen bonding on the absorption spectra are interpreted by means of linear solvation energy relationships using a general equation of the form n = n0 + sp* + aa + bb, where p* is a measure of the solvent polarity, a is the scale of the solvent hydrogen bond donor acidities and b is the scale of the solvent hydrogen bond acceptor basicities.

  4. Who's (Still) Above the Social Security Payroll Tax Cap?

    OpenAIRE

    Nicole Woo; Janelle Jones; John Schmitt

    2012-01-01

    The Social Security payroll tax cap is the earnings level above which no further Social Security taxes are collected. The cap is currently at $110,100, though legislation has been introduced in Congress to apply the Social Security payroll tax to earnings above $250,000 (but not between the current cap and this level). This issue brief updates earlier work, finding that 5.8 percent of workers would be affected if the Social Security cap were eliminated entirely and 1.4 percent would be affect...

  5. Regional distribution of ventilation and perfusion in patients with obstructive pulmonary disease and alpha/sub 1/-antitrypsin deficiency

    Energy Technology Data Exchange (ETDEWEB)

    Mostafa, A B.M.G.; Tulley, N J; Harding, L K; Stockley, R A

    1983-08-01

    Regional distribution of pulmonary ventilation and perfusion has been determined of 13 patients with chronic obstructive pulmonary disease (COPD). Eight patients had alpha/sub 1/-antitrypsin deficiency (..cap alpha../sub 1/ATD). Ventilation studies were carried out using xenon-133 (/sup 133/Xe) and krypton-81m (sup(81m)Kr) gases. Trapping indices were determined from the wash-out part of the xenon ventilation studies. Results obtained from patients were compared with those of normal controls. Ventilation studies with sup(81m)Kr showed pulmonary changes more clearly than did /sup 133/Xe studies and the trapping of radio-xenon was more extensive in lung bases than in apices whether or not the patients had ..cap alpha../sub 1/ ATD. The distribution of perfusion followed a pattern similar to that of ventilation, but did not differ statistically from that of the normal controls.

  6. Experimental search for second-class currents. Beta-ray angular distributions from aligned nuclei /sup 12/B and /sup 12/N

    Energy Technology Data Exchange (ETDEWEB)

    Sugimoto, K; Minamisono, T; Nojiri, Y; Masuda, Y [Osaka Univ., Toyonaka (Japan). Lab. of Nuclear Studies

    1978-01-01

    The ..beta..-energy dependent angular distributions, W(theta) asymptoticaly equals 1 +- P(1 + ..cap alpha../sub +-/E)P/sub 1/(cos theta) + A..cap alpha../sub +-/EP/sub 2/(cos theta), from the aligned nuclei /sup 12/B and /sup 12/N have been measured. Positive A/sup +/ and negative A/sup -/ alignments were successively produced, by use of NMR, after every other production period of polarized nuclei through nuclear reactions; A/sup +/ - A/sup -/ asymptoticaly equals 0.26 for /sup 12/B and /sup +/A/sup +/ - A/sup - +/ asymptoticaly equals 0.55 for /sup 12/N with p asymptoticaly equals 0. The results are ..cap alpha../sub -/(/sup 12/B) = 0.02/sub 5/ +- 0.03/sub 4/%/MeV, /sup +/..cap alpha../sub +/(/sup 12/N)/sup +/ = 0.27/sub 7/ +- 0.05/sub 2/%/MeV, and ..cap alpha../sub -/ - ..cap alpha../sub +/ = 0.30/sub 2/ +- 0.06/sub 2/%/MeV assuming ..cap alpha../sub +/<0. In comparison with available data for CVC test in the mass-12 triad and theoretical predictions, the present ..cap alpha../sub -/ - ..cap alpha../sub +/ value is consistent within 20% level with predictions of the CVC theory and with absence of second-class induced-tensor currents.

  7. Succinct synthesis of saturated hydroxy fatty acids and

    DEFF Research Database (Denmark)

    Kaspersen, Mads Holmgaard; Jenkins, Laura; Dunlop, Julia

    2017-01-01

    Saturated hydroxy fatty acids make up a class of underexplored lipids with potentially interesting biological activities. We report a succinct and general synthetic route to saturated hydroxy fatty acids hydroxylated at position 6 or higher, and exemplify this with the synthesis of hydroxylauric ...... acids. All regioisomers of hydroxylauric acids were tested on free fatty acid receptors FFA1, FFA4 and GPR84. The results show that the introduction of a hydroxy group and its position have a high impact on receptor activity....

  8. Molecular pharmacology of the AMPA agonist, (S)-2-amino-3-(3-hydroxy-5-phenyl-4-isoxazolyl)propionic acid [(S)-APPA] and the AMPA antagonist, (R)-APPA

    DEFF Research Database (Denmark)

    Ebert, B; Madsen, U; Lund, Trine Meldgaard

    1994-01-01

    )-APPA, whereas (R)-APPA is a non-N-methyl-D-aspartic acid (non-NMDA) receptor antagonist showing preferential AMPA blocking effects. In agreement with classical theories for competitive interaction between agonists and antagonists, the efficacy of depolarizations produced by (S)-APPA in the rat cortical wedge......The heterocyclic analogue of (S)-glutamic acid, (S)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid [(S)-AMPA] is a potent and selective AMPA receptor agonist, whereas the enantiomeric compound, (R)-AMPA, is virtually inactive. We have previously characterized (RS)-2-amino-3-(3-hydroxy-5......-phenyl-4-isoxazolyl)propionic acid [(RS)-APPA] as a partial AMPA receptor agonist showing about 60% of the efficacy of (RS)-AMPA. This partial agonism produced by (RS)-APPA is, however, only apparent, since resolution of (RS)-APPA has now been shown to provide the full AMPA receptor agonist, (S...

  9. Conformational analysis of 2,2'-arylmethylene bis(3-hydroxy-5,5-dimethyl-2-cyclohexene-1-one) by NMR and molecular modeling

    Energy Technology Data Exchange (ETDEWEB)

    Ferreira, Marcelle de S.; Figueroa-Villar, Jose D., E-mail: jdfv2009@gmail.com [Instituto Militar de Engenharia (IME), Rio de Janeiro, RJ (Brazil). Dept. de Quimica. Grupo de Medicina Quimica

    2014-05-15

    2,2'-arylmethylene bis(3-hydroxy-5,5-dimethyl-2-cyclohexene-1-ones) with para and ortho-R groups on the benzene ring were prepared and studied by nuclear magnetic resonance (NMR) and molecular modeling to determine their conformational exchanges. Experimental and calculated results indicated conformational interconversions in these compounds by rotation of benzene ring and slow movement of dimedone rings, leading to intramolecular hydrogen bond length variation. The presence of one R group at the ortho position on the benzene ring modifies conformational exchange, leading to disappearance of one intramolecular hydrogen bond and superposition of diverse NMR signals. The correlation of σ{sub p} values with chemical shifts, angles and atomic charges confirms that para-R groups electronic properties are involved in conformational exchange and chemical shift variance. These results will be used to study the interaction of these compounds with bio-molecules and their use as starting materials for design and synthesis of new bioactive agents. (author)

  10. Extractive and spectrophotometric determination of U (VI) using 5-(3-phenolyl azo)-2-hydroxy-4-ethoxy propiophenone oxime (PHEPO)

    International Nuclear Information System (INIS)

    Subrahmanyam, P.; Krishnapriya, B.; Rekha, D.; Reddy Prasad, P.; Chiranjeevi, P.

    2007-01-01

    A simple spectrophotometric method for the determination of U (VI) using 5-(3-phenolyl azo)-2-hydroxy-4-ethoxy propiophenone oxime (PHEPO) is developed. The reagent PHEPO was synthesized and used for extraction of uranium. At pH 8.5-10.0 uranium forms a purple colored complex with PHEPO which was then quantitatively extracted in chloroform showing maximum absorbance at wavelength of 380nm. The proposed method obeys Beer's law in the range of 1.2-19.0ppm. molar absorptivity and Sandelson's sensitivity of extracted species were calculated to be 1.750 x 104 lmol-1 cm-1 and 8.5 x 10-5 mg cm-2 respectively. The method was applied for the determination of uranium in synthetic and plant samples. It was found that the newly developed method is competent to those of standard methods. (author)

  11. Apical cap

    International Nuclear Information System (INIS)

    McLoud, T.C.; Isler, R.J.; Novelline, R.A.; Putman, C.E.; Simeone, J.; Stark, P.

    1981-01-01

    Apical caps, either unilateral or bilateral, are a common feature of advancing age and are usually the result of subpleural scarring unassociated with other diseases. Pancoast (superior sulcus) tumors are a well recognized cause of unilateral asymmetric apical density. Other lesions arising in the lung, pleura, or extrapleural space may produce unilateral or bilateral apical caps. These include: (1) inflammatory: tuberculosis and extrapleural abscesses extending from the neck; (2) post radiation fibrosis after mantle therapy for Hodgkin disease or supraclavicular radiation in the treatment of breast carcinoma; (3) neoplasm: lymphoma extending from the neck or mediastinum, superior sulcus bronchogenic carcinoma, and metastases; (4) traumatic: extrapleural dissection of blood from a ruptured aorta, fractures of the ribs or spine, or hemorrhage due to subclavian line placement; (5) vascular: coarctation of the aorta with dilated collaterals over the apex, fistula between the subclavian artery and vein; and (6) miscellaneous: mediastinal lipomatosis with subcostal fat extending over the apices

  12. 4 Birds 1 Stone to Inhibit 5androstane-3alpha,17beta-diol Conversion to DHT

    Science.gov (United States)

    2016-09-01

    Award Number: W81XWH-15-1-0409 TITLE: 4 Birds 1 Stone to Inhibit 5androstane-3alpha,17beta-diol Conversion to DHT PRINCIPAL INVESTIGATOR...SUBTITLE 5a. CONTRACT NUMBER 5b. GRANT NUMBER W81XWH-15-1-04094 Birds 1 Stone to Inhibit 5androstane-3alpha,17beta-diol Conversion to DHT 5c...testicular androgens, testosterone or dihydrotestosterone ( DHT ). Men diagnosed with advanced prostate cancer or failure potentially curative therapy are

  13. Reactions of saccharides catalyzed by molybdate ions. XXXIII. Use of. cap alpha. (U-/sup 14/C)glucan for preparation of /sup 14/C-labelled saccharides

    Energy Technology Data Exchange (ETDEWEB)

    Bilik, V; Biely, P [Institute of Chemistry, Centre for Chemical Research, Slovak Academy of Sciences, Bratislava (Czechoslovakia); Kolina, J [Ustav pro Vyzkum, Vyrobu a Vyuziti Radioisotopu, Prague (Czechoslovakia)

    1984-01-01

    D-(U-/sup 14/C)glucose obtained in acid hydrolysis of ..cap alpha..-(U-/sup 14/C)glucan (2 M-HCl) was epimerized under a catalytic action of molybdate ions to D-(U-/sup 14/C)mannose isolated with a 20% yield. Oxidative degradation of 4-nitrophenylhydrazones of D-(U-/sup 14/C)arabinose and D-(U-/sup 14/C)xylose resulted in D-(U-/sup 14/C)erythrose and D-(U-/sup 14/C)threose, respectively, with a 15% yield relative to the starting aldopentoses. Nitromethane synthesis with D-(U-/sup 14/C)lyxose followed by oxidative decomposition of the corresponding nitrohexitols yielded /sup 14/C-labelled D-galactose. Described is also the preparation of D-(U-/sup 14/C)arabinose from D-(U-/sup 14/C)glucose and the conversion of D-(U-/sup 14/C)arabinose to D-(U-/sup 14/C)xylose and D-(U-/sup 14/C)lyxose.

  14. Identification of the molecular switch that regulates access of 5alpha-DHT to the androgen receptor.

    Science.gov (United States)

    Penning, Trevor M; Bauman, David R; Jin, Yi; Rizner, Tea Lanisik

    2007-02-01

    Pairs of hydroxysteroid dehydrogenases (HSDs) govern ligand access to steroid receptors in target tissues and act as molecular switches. By acting as reductases or oxidases, HSDs convert potent ligands into their cognate inactive metabolites or vice versa. This pre-receptor regulation of steroid hormone action may have profound effects on hormonal response. We have identified the HSDs responsible for regulating ligand access to the androgen receptor (AR) in human prostate. Type 3 3alpha-hydroxysteroid dehydrogenase (aldo-keto reductase 1C2) acts solely as a reductase to convert 5alpha-dihydrotestosterone (DHT), a potent ligand for the AR (K(d)=10(-11)M for the AR), to the inactive androgen 3alpha-androstanediol (K(d)=10(-6)M for the AR); while RoDH like 3alpha-HSD (a short-chain dehydrogenase/reductase (SDR)) acts solely as an oxidase to convert 3alpha-androstanediol back to 5alpha-DHT. Our studies suggest that aldo-keto reductase (AKRs) and SDRs function as reductases and oxidases, respectively, to control ligand access to nuclear receptors.

  15. Contribution to the study of the diffusion {alpha}-proton for {alpha} particles of 3,1 and 5,3 MeV; Contribution a l'etude de la diffusion {alpha}-proton pour des particules {alpha} d'energie comprise entre 3,1 et 5,3 MeV

    Energy Technology Data Exchange (ETDEWEB)

    Ruhla, C [Commissariat a l' Energie Atomique, Saclay(France). Centre d' Etudes Nucleaires

    1953-07-01

    The diffusion of the particles has by the light cores that present a weak gate of potential, must permit the survey of the nuclear strengths. Some authors, studying the distribution in energy of the protons given out by a hydrogenated target submitted to a bombardment has variable energy, signal that this distribution has a structure of groups. We tried to reproduce experiences of diffusion {alpha}-proton, in order to verify the existence of the groups of signaled protons in the previous works. However in spite of finer experimental conditions, we had recovered any group structures in the distribution of the protons. This work permits to conclude that there is not a resonance in the {alpha}-proton diffusion for included energies between 3,1 and 5,3 MeV. The absence of resonances confirms the existence of the fundamental level of {sup 5}Li above in the neighborhood of 1,8 MeV {sup 4}He + {sup 1}H. (M.B.) [French] La diffusion des particules a par les noyaux legers qui presentent une faible barriere de potentiel, doit permettre l'etude des forces nucleaires. certains auteurs, etudiant la distribution en energie des protons emis par une cible hydrogenee soumise a un bombardement a d'energie variable, signalent que cette distribution a une structure de groupes. Nous avons essaye de reproduire les experiences du type diffusion {alpha}-proton, afin de verifier l'existence des groupes de protons signales dans les travaux anterieurs. Cependant malgre des conditions experimentales plus fines, nous n'avons retrouve aucunce structure de groupe dans la distribution des protons. Ce travail permet de conclure qu'il n'y a pas de resonance dans la diffusion {alpha}-proton pour des energies comprises entre 3,1 et 5,3 MeV. L'absence de resonances confirme l'existence du niveau fondamental de {sup 5}Li au voisinage de 1,8 MeV au-dessus de {sup 4}He + {sup 1}H. (M.B.)

  16. Internal conversion coefficients of M4 isomeric transitions in /sup 125/ /sup 127/ /sup 129/Te decay

    Energy Technology Data Exchange (ETDEWEB)

    Soni, S K; Kumar, A; Gupta, S L; Pancholi, S C [Delhi Univ. (India). Dept. of Physics and Astrophysics

    1977-01-01

    The internal conversion coefficients have been measured using a high resolution low energy Ge(Li) detector for the following M4 transitions: /sup 125/Te: 109.27 keV transition ..cap alpha..sub(T) = 357 +- 11; RG method, /sup 127/Te: 88,26 keV transition ..cap alpha..sub(K) = 484 +- 23; XPG method, /sup 129/Te: 105.50 keV transition ..cap alpha..sub(K) = 213 +- 10; XPG method. It is observed that these values are lower by 2.5-3.6% as compared with Hager and Seltzer's calculations. A comparison between experimental and theoretical ..cap alpha..sub(K) and ..cap alpha..sub(T) values for eleven M4 transitions shows that the experimental values are systematically lower.

  17. Altered cortisol metabolism in polycystic ovary syndrome: insulin enhances 5alpha-reduction but not the elevated adrenal steroid production rates.

    Science.gov (United States)

    Tsilchorozidou, Tasoula; Honour, John W; Conway, Gerard S

    2003-12-01

    Androgen excess in women with polycystic ovary syndrome (PCOS) may be ovarian and/or adrenal in origin, and one proposed contributing mechanism is altered cortisol metabolism. Increased peripheral metabolism of cortisol may occur by enhanced inactivation of cortisol by 5alpha-reductase (5alpha-R) or impaired reactivation of cortisol from cortisone by 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) resulting in decreased negative feedback suppression of ACTH secretion maintaining normal plasma cortisol concentrations at the expense of androgen excess. We have tested whether any enzyme dysregulation was related to circulating insulin or androgen concentrations in women with PCOS and have sought to clarify their relationship with obesity. First, to avoid obesity-related effects on cortisol metabolism, 18 lean women with PCOS were compared with 19 lean controls who were closely matched for body mass index (BMI). Second, the impact of obesity was studied in a cross-section of 42 PCOS women of a broad range of BMI. We measured 24-h urinary excretion of steroid metabolites by gas chromatography/mass spectrometry and fasting metabolic and hormone profiles. Urinary excretion of androgens [androsterone (P = 0.003), etiocholanolone (P = 0.02), and C19 steroid sulfates (P = 0.009)], cortisone metabolites [tetrahydrocortisone (THE) (P = 0.02), alpha-cortolone (P lean PCOS subjects when compared with controls. A significantly higher 5alpha-tetrahydrocortisol (5alpha-THF)/5beta-THF ratio (P = 0.04) and a significantly lower alpha-THF + THF + alpha-cortol/THE + cortolones ratio (P = 0.01) were found in lean PCOS women compared with lean controls, indicating both enhanced 5alpha-R and reduced 11beta-HSD1 activities. A decreased THE/cortolones ratio (P = 0.03) was also found in lean PCOS women compared with lean controls, indicating increased 20 alpha/beta-HSD activity. In the group of 42 PCOS subjects, measures of 5alpha/5beta reduction were positively correlated with the

  18. X-ray structure, semi-empirical MO calculations and π-electron delocalization of 1-cyanoacetyl-5-trifluoromethyl-5-hydroxy-4,5-dihydro-1 H-pyrazoles

    Science.gov (United States)

    Martins, Marcos A. P.; Moreira, Dayse N.; Frizzo, Clarissa P.; Campos, Patrick T.; Longhi, Kelvis; Marzari, Mara R. B.; Zanatta, Nilo; Bonacorso, Helio G.

    2010-04-01

    The structure of three 1-cyanoacetyl-3-alkyl[aryl]-5-trifluoromethyl-5-hydroxy-4,5-dihydro-1 H-pyrazoles ( 1- 3) has been determined by X-ray diffractometry. The 4,5-dihydro-1 H-pyrazole rings were obtained as almost planar structures showing RMS deviation at a range of 0.0196-0.0736 Å. The data demonstrate that the molecular packing is dependent on the substituent present in each molecule. In addition, a computational investigation using semi-empirical AM1 and RM1 methods was performed in order to investigate the correlation between experimental and calculated geometrical parameters. The data obtained suggest that the structural data furnished by the AM1 method is in better agreement with those experimentally determined for the above compounds. An analysis of the π-electron delocalization by HOMA calculations indicate that there is a hyperconjugation effect in the imine group toward to phenyl group at ring 3-position of compound 2, and that this resonance effect decrease in compounds 1 and 3. In addition, it was showed that bond N(1) and C(6) do not have an amide character. Thus, the O(6)-C(6)-N(1)-N(2)-C(3) fragment is not completely delocalized mainly due to the low π-electron delocalization in N(1)-N(2) bond for all compounds.

  19. Three-Dimensional Conformal Radiotherapy in Prostate Cancer Patients: Rise in Interleukin 6 (IL-6) but not IL-2, IL-4, IL-5, Tumor Necrosis Factor-{alpha}, MIP-1-{alpha}, and LIF Levels

    Energy Technology Data Exchange (ETDEWEB)

    Oliveira Lopes, Carlos [Universidade do Vale do Paraiba, Centro de Oncologia Radioterapica do Vale do Paraiba, Universidade do Vale do Paraiba Instituto de Pesquisa e Desenvolvimento, Universidade do Vale do Paraiba, Sao Jose dos Campos, Sao Paulo (Brazil); Callera, Fernando, E-mail: fcallera@gmail.com [Centro de Hematologia Onco-hematologia e Transplantes de Medula Ossea do Vale do Paraiba, Sao Paulo (Brazil)

    2012-03-15

    Purpose: To investigate the effect of radiotherapy (RT) on serum levels of interleukin-2 (IL-2), IL-4, IL-5, IL-6, tumor necrosis factor alpha (TNF-{alpha}), macrophage inflammatory protein-1-alpha (MIP-1-{alpha}) and leukemia inhibitory factor (LIF) in patients with prostate cancer. Methods and Materials: Forty eight patients with prostate cancer received three-dimensional conformal blocking radiation therapy with a linear accelerator. IL-2, IL-4, IL-5, IL-6, TNF-{alpha}, MIP-1-{alpha}, and LIF levels were measured by the related immunoassay kit 1 day before the beginning of RT and during RT at days 15 and 30. Results: The mean IL-2 values were elevated before and during the RT in contrast with those of IL-4, IL-5, IL-6, TNF-{alpha}, MIP-1-{alpha}, and LIF, which were within the normal range under the same conditions. Regarding markers IL-2, IL-4, IL-5, TNF-{alpha}, MIP-1-{alpha}, and LIF, comparisons among the three groups (before treatment and 15 and 30 days during RT) did not show significant differences. Although values were within the normal range, there was a significant rise in IL-6 levels at day 15 of RT (p = 0.0049) and a decline at day 30 to levels that were similar to those observed before RT. Conclusions: IL-6 appeared to peak after 15 days of RT before returning to pre-RT levels. In contrast, IL-2, IL-4, IL-5, TNF-{alpha}, MIP-1-{alpha}, and LIF levels were not sensitive to irradiation. The increased levels of IL-6 following RT without the concurrent elevation of other cytokines involved in the acute phase reaction did not suggest a classical inflammatory response to radiation exposure. Further studies should be designed to elucidate the role of IL-6 levels in patients with prostate cancer treated with RT.

  20. CAPS Activity in Priming Vesicle Exocytosis Requires CK2 Phosphorylation*

    OpenAIRE

    Nojiri, Mari; Loyet, Kelly M.; Klenchin, Vadim A.; Kabachinski, Gregory; Martin, Thomas F. J.

    2009-01-01

    CAPS (Ca2+-dependent activator protein for secretion) functions in priming Ca2+-dependent vesicle exocytosis, but the regulation of CAPS activity has not been characterized. Here we show that phosphorylation by protein kinase CK2 is required for CAPS activity. Dephosphorylation eliminated CAPS activity in reconstituting Ca2+-dependent vesicle exocytosis in permeable and intact PC12 cells. Ser-5, -6, and -7 and Ser-1281 were identified by mass spectrometry as the major phosphorylation sites in...

  1. Preparation and biological evaluation of 2-amino-6-[{sup 18}F]fluoro-9-(4-hydroxy-3-hydroxy-methylbutyl) purine (6-[{sup 18}F]FPCV) as a novel PET probe for imaging HSV1-tk reporter gene expression

    Energy Technology Data Exchange (ETDEWEB)

    Cai Hancheng [Research Center of Radiopharmaceuticals, Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai 201800 (China); Graduate School of the Chinese Academy of Sciences, Beijing 100049 (China); Yin Duanzhi [Research Center of Radiopharmaceuticals, Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai 201800 (China)], E-mail: chcbati@yahoo.com.cn; Zhang Lan [Research Center of Radiopharmaceuticals, Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai 201800 (China); Zhejiang California International NanoSystems Institute, Hangzhou 310029 (China); Yang, Xiaofeng; Xu Xiaoyan; Liu Weiguo; Zheng Xuesheng [Institute of Brain Medical Science, Second affiliated Hospital, Medicine School of Zhejiang University, Hangzhou 310009 (China); Zhang Hong [Department of Nuclear Medicine, Second Affiliated Hospital, Zhejiang University Medical PET Center, Medicine School of Zhejiang University, Hangzhou 310009 (China); Wang Jing [Department of Nuclear Medicine, Second Affiliated Hospital, Zhejiang University Medical PET Center, Medicine School of Zhejiang University, Hangzhou 310009 (China); Zhejiang California International NanoSystems Institute, Hangzhou 310029 (China); Xu Yuhong [Zhejiang California International NanoSystems Institute, Hangzhou 310029 (China); Cheng Dengfeng; Zheng Mingqiang; Han Yanjiang; Wu Mingxing; Wang Yongxian [Research Center of Radiopharmaceuticals, Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai 201800 (China)

    2007-08-15

    Introduction: 2-Amino-6-[{sup 18}F]fluoro-9-(4-hydroxy-3-hydroxy-methylbutyl) purine (6-[{sup 18}F]FPCV) was prepared via a one-step nucleophilic substitution and evaluated as a novel probe for imaging the expression of herpes simplex virus type 1 thymidine kinase (HSV1-tk) reporter gene. Methods: Log P of 6-[{sup 18}F]FPCV was calculated in octanol/phosphate-buffered saline (PBS). Stability studies were performed in PBS and bovine serum albumin (BSA). Cell uptake was performed at various time points in wild-type cells and transduced cells. For in vivo studies, tumors were grown in nude mice by inoculation with C6 cells, wild type and tk positive. The radiotracer was intravenously injected to animals, and micro-PET imaging was performed. Biodistribution of 6-[{sup 18}F]FPCV was performed on another group of animals at different time points. Results: Log P of 6-[{sup 18}F]FPCV was -0.517. 6-[{sup 18}F]FPCV was fairly stable in PBS and BSA at 6 h. The tracer uptake in C6-tk cells was 5.5-18.8 times higher than that in wild-type cells. The plasma half-life of 6-[{sup 18}F]FPCV was as follows: {alpha} t{sub 1/2}=1.2 min and {beta} t{sub 1/2}=73.7 min. The average ratio of tumor uptake between the transduced tumor and the wild-type tumor was 1.69 at 15 min. Conclusion: Biological evaluation showed that 6-[{sup 18}F]FPCV is a potential probe for imaging HSV1-tk gene expression. However, its in vivo defluorination may limit its application in PET imaging of gene expression.

  2. Comparative carbon-13 nuclear magnetic resonance study at 67. 9 MHz on lysozyme (human and egg-white) and. cap alpha. -lactalbumin (human and bovine) in their native and denatured state

    Energy Technology Data Exchange (ETDEWEB)

    van Binst, G; Biesemans, M [Brussels Univ. (Belgium). Faculte des Sciences

    1975-01-01

    A first detailed comparison of the /sup 13/C spectra at high field of two lysozymes (human and egg-white) and two ..cap alpha..-lactalbumins (human and bovine milk) is presented. Assignments were made on most of the resonance peaks in the aliphatic and aromatic regions of the denatured proteins. The relative peak intensities clearly demonstrate the differences in the amino acid composition of the related proteins. The broadening and the complexity of the spectra of the native proteins reflect the non equivalence of the chemical groups in the folded conformation. The usefulness of /sup 13/C nmr spectroscopy in the study of the interaction between small molecules and proteins was tested on N-acteyl-glucosamine in the presence of lysozyme.

  3. Electron impact ionization mass spectra of 3-substituted-2-hydroxy-4(3H)-quinazolinones

    International Nuclear Information System (INIS)

    El Deen, I. M.; Abd El Fattah, M. E.

    2003-01-01

    2-Amino-2-hydroxy-4(3H)-quinazolinone (3) was prepared via condensation of 1 with hydrazine hydrate. Treatment of 3 with appropriate acid in POCl 3 , ethyl chloroacetate and activated olefinic compounds in DMF yielded the corresponding 3-(substituted)amino-2-hydroxy-4(3H)-quinazolinones 4,5 and 6. The electron impact ionization mass spectra of compounds 3 and 4 show a weak molecular ion peak and a base peak of m/z 146 resulting from a cleavage fragmentation. The compounds 5 and 6 give a characteristics fragmentation pattern with a very stable fragment of benzopyrazolone (m/z 132)

  4. Structures of nitrato-(2-hydroxybenzaldehydo) (2,2 Prime -bipyridyl)copper and nitrato-(2-hydroxy-5-nitrobenzaldehydo)(2,2 Prime -bipyridyl)copper

    Energy Technology Data Exchange (ETDEWEB)

    Chumakov, Yu. M. [Academy of Sciences of Moldova, Institute of Applied Physics (Moldova, Republic of); Paladi, L. G. [Moldova State University (Moldova, Republic of); Antosyak, B. Ya.; Simonov, Yu. A. [Academy of Sciences of Moldova, Institute of Applied Physics (Moldova, Republic of); Tsapkov, V. I., E-mail: vtsapkov@gmail.com [Moldova State University (Moldova, Republic of); Bocelli, G. [Institute of Materials for Electronics and Magnetism (Italy); Gulea, A. P. [Moldova State University (Moldova, Republic of); Ginju, D. [Alexandru Ioan Cuza University of Iasi (Romania); Palomares-Sanchez, S. A. [Autonomous University of San Luis Potosi (Mexico)

    2011-03-15

    Nitrato-(2-hydroxy-5-nitrobenzaldehydo)(2,2 Prime -bipyridyl)copper (I) and nitrato-(2-hydroxybenzaldehydo)(2,2 Prime -bipyridyl)copper (II) were synthesized and characterized by X-ray diffraction. The coordination polyhedron of the central copper atom in complex I can be described as a distorted tetragonal pyramid whose base is formed by the phenol and carbonyl oxygen atoms of the monodeprotonated 2-hydroxy-5nitrobenzaldehyde molecule and the nitrogen atoms of the 2,2 Prime -bipyridyl ligand and whose apex is occupied by the oxygen atom of the nitrato group. In the crystal structure, complexes I are linked by the acido ligands and the NO{sub 2} groups of the aldehyde molecule into infinite chains. In complex II, the central copper atom is coordinated by 2-hydroxybenzaldehyde, 2,2 Prime -bipyridyl, and the nitrato group, resulting in the formation of centrosymmetric dimers. The coordination polyhedron of the central copper atom can be described as a bipyramid (4 + 1 + 1) with the same base as in complex I. The axial vertices of the bipyramid are occupied by the oxygen atom of the nitrato group and the bridging phenol oxygen atom of the adjacent complex related to the initial complex by a center of symmetry. In the crystal structure, complexes II are hydrogen bonded into infinite chains.

  5. Analysis of Hydroxy Fatty Acids from the Pollen of Brassica campestris L. var. oleifera DC. by UPLC-MS/MS

    Directory of Open Access Journals (Sweden)

    Nian-Yun Yang

    2013-01-01

    Full Text Available Ultraperformance liquid chromatography coupled with negative electrospray tandem mass spectrometry (UPLC-ESI-MS/MS was used to determine 7 hydroxy fatty acids in the pollen of Brassica campestris L. var. oleifera DC. All the investigated hydroxy fatty acids showed strong deprotonated molecular ions [M–H]−, which underwent two major fragment pathways of the allyl scission and the β-fission of the alcoholic hydroxyl group. By comparison of their molecular ions and abundant fragment ions with those of reference compounds, they were tentatively assigned as 15,16-dihydroxy-9Z,12Z-octadecadienoic acid (1, 10,11,12-trihydroxy-(7Z,14Z-heptadecadienoic acid (2, 7,15,16-trihydroxy-9Z,12Z-octadecadienoic acid (3, 15,16-dihydroxy-9Z,12Z-octadecadienoic acid (4, 15-hydroxy-6Z,9Z,12Z-octadecatrienoic acid (5, 15-hydroxy-9Z,12Z- octadecadienoic acid (6, and 15-hydroxy-12Z-octadecaenoic acid (7, respectively. Compounds 3, 5, and 7 are reported for the first time.

  6. Differential involvement of 5-HT(1A) and 5-HT(1B/1D) receptors in human interferon-alpha-induced immobility in the mouse forced swimming test.

    Science.gov (United States)

    Zhang, Hongmei; Wang, Wei; Jiang, Zhenzhou; Shang, Jing; Zhang, Luyong

    2010-01-01

    Although Interferon-alpha (IFN-alpha, CAS 9008-11-1) is a powerful drug in treating several viral infections and certain tumors, a considerable amount of neuropsychiatric side-effects such as depression and anxiety are an unavoidable consequence. Combination with the selective serotonin (5-HT) reuptake inhibitor (SSRI) fluoxetine (CAS 56296-78-7) significantly improved the situation. However, the potential 5-HT(1A) receptor- and 5-HT(1B) receptor-signals involved in the antidepressant effects are still unclear. The effects of 5-HT(1A) receptor- and 5-HT(1B) receptor signals were analyzed by using the mouse forced swimming test (FST), a predictive test of antidepressant-like action. The present results indicated that (1) fluoxetine (administrated intragastrically, 30 mg/kg; not subactive dose: 15 mg/kg) significantly reduced IFN-alpha-induced increase of the immobility time in the forced swimming test; (2) 5-HT(1A) receptor- and 5-HT(1B) receptor ligands alone or in combination had no effects on IFN-alpha-induced increase of the immobility time in the FST; (3) surprisingly, WAY 100635 (5-HT(1A) receptor antagonist, 634908-75-1) and 8-OH-DPAT(5-HT(1A) receptor agonist, CAS 78950-78-4) markedly enhanced the antidepressant effect of fluoxetine at the subactive dose (15 mg/kg, i. g.) on the IFN-alpha-treated mice in the FST. Further investigations showed that fluoxetine combined with WAY 100635 and 8-OH-DPAT failed to produce antidepressant effects in the FST. (4) Co-application of CGS 12066A (5-HT(1B) receptor agonist, CAS 109028-09-3) or GR 127935 (5-HT(1B/1D) receptor antagonist, CAS 148642-42-6) with fluoxetine had no synergistic effects on the IFN-alpha-induced increase of immobility time in FST. (5) Interestingly, co-administration of GR 127935, WAY 100635 and fluoxetine significantly reduced the IFN-alpha-induced increase in immobility time of FST, being more effective than co-administration of WAY 100635 and fluoxetine. All results suggest that (1) compared to

  7. Docking Studies and Anti-inflammatory Activity of β-Hydroxy-β-arylpropanoic Acids

    Directory of Open Access Journals (Sweden)

    Ivan O. Juranic

    2008-03-01

    Full Text Available The article describes a two-step synthesis of diastereomeric 3-hydroxy-2-methyl-3-(4-biphenylylbutanoic acids. In the first step an intermediate α-bromo propanoicacid 1-ethoxyethyl ester was synthesized. The second step is a new modified Reformatskyreaction in presence of Zn in tetrahydrofuran (THF at –5 to 10 °C between the previouslysynthesized intermediate and 4-acetylbiphenyl. Synthesis of the other studied β-hydroxy-β-arylpropanoic acids has already been reported. These β-hydroxy-β-arylpropanoic acidsbelong to the arylpropanoic acid class of compounds, structurally similar to the NSAIDssuch as ibuprofen. The anti-inflammatory activity and gastric tolerability of thesynthesized compounds were evaluated. Molecular docking experiments were carried outto identify potential COX-2 inhibitors among the β-hydroxy-β-aryl-alkanoic acids class.The results indicate that all compounds possess significant anti-inflammatory activity afteroral administration and that the compounds 2-(9-(9-hydroxy-fluorenyl-2-methylpropanoic acid (5 and 3-hydroxy-3,3-diphenyl-propanoic acid (3 possess thestrongest anti-inflammatory activity, comparable to that of ibuprofen, a standard NSAID,and that none of tested substances or ibuprofen produced any significant gastric lesions.

  8. The Rabies Virus L Protein Catalyzes mRNA Capping with GDP Polyribonucleotidyltransferase Activity.

    Science.gov (United States)

    Ogino, Minako; Ito, Naoto; Sugiyama, Makoto; Ogino, Tomoaki

    2016-05-21

    The large (L) protein of rabies virus (RABV) plays multiple enzymatic roles in viral RNA synthesis and processing. However, none of its putative enzymatic activities have been directly demonstrated in vitro. In this study, we expressed and purified a recombinant form of the RABV L protein and verified its guanosine 5'-triphosphatase and GDP polyribonucleotidyltransferase (PRNTase) activities, which are essential for viral mRNA cap formation by the unconventional mechanism. The RABV L protein capped 5'-triphosphorylated but not 5'-diphosphorylated RABV mRNA-start sequences, 5'-AACA(C/U), with GDP to generate the 5'-terminal cap structure G(5')ppp(5')A. The 5'-AAC sequence in the substrate RNAs was found to be strictly essential for RNA capping with the RABV L protein. Furthermore, site-directed mutagenesis showed that some conserved amino acid residues (G1112, T1170, W1201, H1241, R1242, F1285, and Q1286) in the PRNTase motifs A to E of the RABV L protein are required for cap formation. These findings suggest that the putative PRNTase domain in the RABV L protein catalyzes the rhabdovirus-specific capping reaction involving covalent catalysis of the pRNA transfer to GDP, thus offering this domain as a target for developing anti-viral agents.

  9. Enzymatic synthesis of RNAs capped with nucleotide analogues reveals the molecular basis for substrate selectivity of RNA capping enzyme: impacts on RNA metabolism.

    Directory of Open Access Journals (Sweden)

    Moheshwarnath Issur

    Full Text Available RNA cap binding proteins have evolved to specifically bind to the N7-methyl guanosine cap structure found at the 5' ends of eukaryotic mRNAs. The specificity of RNA capping enzymes towards GTP for the synthesis of this structure is therefore crucial for mRNA metabolism. The fact that ribavirin triphosphate was described as a substrate of a viral RNA capping enzyme, raised the possibility that RNAs capped with nucleotide analogues could be generated in cellulo. Owing to the fact that this prospect potentially has wide pharmacological implications, we decided to investigate whether the active site of the model Paramecium bursaria Chlorella virus-1 RNA capping enzyme was flexible enough to accommodate various purine analogues. Using this approach, we identified several key structural determinants at each step of the RNA capping reaction and generated RNAs harboring various different cap analogues. Moreover, we monitored the binding affinity of these novel capped RNAs to the eIF4E protein and evaluated their translational properties in cellulo. Overall, this study establishes a molecular rationale for the specific selection of GTP over other NTPs by RNA capping enzyme It also demonstrates that RNAs can be enzymatically capped with certain purine nucleotide analogs, and it also describes the impacts of modified RNA caps on specific steps involved in mRNA metabolism. For instance, our results indicate that the N7-methyl group of the classical N7-methyl guanosine cap is not always indispensable for binding to eIF4E and subsequently for translation when compensatory modifications are present on the capped residue. Overall, these findings have important implications for our understanding of the molecular determinants involved in both RNA capping and RNA metabolism.

  10. Thermodynamics of organic molecule adsorption on sorbents modified with 5-hydroxy-6-methyluracil by inverse gas chromatography.

    Science.gov (United States)

    Gus'kov, Vladimir Yu; Gainullina, Yulia Yu; Ivanov, Sergey P; Kudasheva, Florida Kh

    2014-08-22

    The thermodynamic features of organic molecule adsorption from the gaseous phase of sorbents modified with 5-hydroxy-6-methyluracil (HMU) were studied. Molar internal energy and entropy of adsorption variation analyses showed that with every type surface, except for silica gel, layers of supramolecular structure have cavities equal in size with the ones revealed in HMU crystals by X-ray diffraction. Adsorption thermodynamics on HMU-modified sorbents depended on the amount of impregnated HMU and on the polarity, but not the porosity, of the initial sorbent. Polarity of the modified surface increased as a function of HMU quantity and initial sorbent mean pore size, but become appreciably lower if the initial surface is capable of hydrogen bonding. Copyright © 2014 Elsevier B.V. All rights reserved.

  11. (1S,3S,4S-tert-Butyl N-[1-benzyl-3-hydroxy-5-phenyl-4-(picolinamidopentyl]carbamate

    Directory of Open Access Journals (Sweden)

    Jian-Feng Zheng

    2008-07-01

    Full Text Available The title compound, C29H35N3O4, was obtained by the reaction of (2S,4S,5S-tert-butyl N-(4-amino-1-benzyl-3-hydroxy-5-phenylpentylcarbamate and picolinic acid using oxalyl chloride as a chlorinating reagent to activate the carboxyl group. In the crystal structure there are two molecules in the asymmetric unit, which are aligned edge-to-face. In one molecule, the pyridyl ring forms a dihedral angle of 22.0 (1° with the phenyl ring of the terminal benzyl group and 14.3 (1° with the other phenyl ring; in the other molecule, the corresponding angles are 12.1 (1 and 10.6 (1°, respectively. The packing is stabilized by intermolecular hydrogen bonds and C—H...π interactions.

  12. A reduction in hippocampal GABAA receptor alpha5 subunits disrupts the memory for location of objects in mice.

    Science.gov (United States)

    Prut, L; Prenosil, G; Willadt, S; Vogt, K; Fritschy, J-M; Crestani, F

    2010-07-01

    The memory for location of objects, which binds information about objects to discrete positions or spatial contexts of occurrence, is a form of episodic memory particularly sensitive to hippocampal damage. Its early decline is symptomatic for elderly dementia. Substances that selectively reduce alpha5-GABA(A) receptor function are currently developed as potential cognition enhancers for Alzheimer's syndrome and other dementia, consistent with genetic studies implicating these receptors that are highly expressed in hippocampus in learning performance. Here we explored the consequences of reduced GABA(A)alpha5-subunit contents, as occurring in alpha5(H105R) knock-in mice, on the memory for location of objects. This required the behavioral characterization of alpha5(H105R) and wild-type animals in various tasks examining learning and memory retrieval strategies for objects, locations, contexts and their combinations. In mutants, decreased amounts of alpha5-subunits and retained long-term potentiation in hippocampus were confirmed. They exhibited hyperactivity with conserved circadian rhythm in familiar actimeters, and normal exploration and emotional reactivity in novel places, allocentric spatial guidance, and motor pattern learning acquisition, inhibition and flexibility in T- and eight-arm mazes. Processing of object, position and context memories and object-guided response learning were spared. Genotype difference in object-in-place memory retrieval and in encoding and response learning strategies for object-location combinations manifested as a bias favoring object-based recognition and guidance strategies over spatial processing of objects in the mutants. These findings identify in alpha5(H105R) mice a behavioral-cognitive phenotype affecting basal locomotion and the memory for location of objects indicative of hippocampal dysfunction resulting from moderately decreased alpha5-subunit contents.

  13. Phase transition and intramolecular hydrogen bonding in nitro derivatives of ortho-hydroxy acetophenones

    Science.gov (United States)

    Filarowski, A.; Kochel, A.; Koll, A.; Bator, G.; Mukherjee, S.

    2006-03-01

    The crystal structures of two ortho-hydroxy aryl ketones (5-chloro-3-nitro-2-hydroxyacetophenone, 5-methyl-3-nitro-2-hydroxyacetophenone and the complex 5-chloro-3-nitro-2-hydroxyacetophenone with 2-aminobenzoic acid (anthranilic acid)) were determined by X-ray diffraction. The existence of an intramolecular hydrogen bond of enol character between the hydroxyl and acetyl groups was found by the X-ray method. The enol character was also confirmed by DFT (B3LYP/6-31+G(d,p)) calculations. A phase transition was found at 138 K in 5-chloro-3-nitro-2-hydroxyacetophenone. This phase transition was investigated by differential scanning calorimetry (DSC), dilatometry, and the dielectric method. A study of the nitro-group dynamics in the ortho-hydroxy acetophenones was carried out with DFT (B3LYP/6-31+G(d,p)) calculations.

  14. Development of a radioimmunoassay for 18-hydroxy-corticosterone

    Energy Technology Data Exchange (ETDEWEB)

    Martin, V I

    1980-03-01

    It has been suggested that 18-hydroxy-corticosterone (18-OH-B) is a precursor for aldosterone in the biosynthetic pathway. This steroid had not been measured in peripheral plasma and therefore to evaluate its clinical role a sensitive and specific radioimmunoassay was developed. The assay is described and was applied to measure the levels of 18-hydroxy-corticosterone in normal human subjects on (a) an ad libitum sodium intake whilst lying or standing, (b) on a high or low sodium intake whilst recumbent, (c) before and after treatment with either ACTH, metyrapone or dexamethasone on a high or low sodium intake whilst recumbent (d) after insulin induced hypoglycaemia and (e) after infusions of 18-hydroxy-corticosterone. The levels of 18-hydroxy-corticosterone were also measured in patients with (a) 17chemically bond-hydroxylase deficiency, (b) primary or secondary aldosteronism, (c) Bartter's syndrome, (d) Cushing's syndrome, (e) adrenalectomised patients or patient's with Addison's disease and (f) patients with essential hypertension. (author).

  15. The role of alpha3beta1 integrin in determining the supramolecular organization of laminin-5 in the extracellular matrix of keratinocytes.

    Science.gov (United States)

    deHart, Gregory W; Healy, Kevin E; Jones, Jonathan C R

    2003-02-01

    Analyses of mice with targeted deletions in the genes for alpha3 and beta1 integrin suggest that the alpha3beta1 integrin heterodimer likely determines the organization of the extracellular matrix within the basement membrane of skin. Here we tested this hypothesis using keratinocytes derived from alpha3 integrin-null mice. We have compared the organizational state of laminin-5, a ligand of alpha3beta1 integrin, in the matrix of wild-type keratinocytes with that of laminin-5 in the matrix of alpha3 integrin-null cells. Laminin-5 distributes diffusely in arc structures in the matrix of wild-type mouse keratinocytes, whereas laminin-5 is organized into linear, spike-like arrays by the alpha3 integrin-null cells. The fact that alpha3 integrin-null cells are deficient in their ability to assemble a proper laminin-5 matrix is also shown by their failure to remodel laminin-5 when plated onto surfaces coated with purified laminin-5 protein. In sharp contrast, wild-type keratinocytes organize exogenously added laminin-5 into discrete ring-like organizations. These findings led us next to assess whether differences in laminin-5 organization in the matrix of the wild-type and alpha3 integrin-null cells impact cell behavior. Our results indicate that alpha3 integrin-null cells are more motile than their wild-type counterparts and leave extensive trails of laminin-5 over the surface on which they move. Moreover, HEK 293 cells migrate significantly more on the laminin-5-rich matrix derived from the alpha3 integrin-null cells than on the wild-type keratinocyte laminin-5 matrix. In addition, alpha3 integrin-null cells show low strength of adhesion to surfaces coated with purified laminin-5 compared to wild-type cells although both the wild type and the alpha3 integrin-null keratinocytes adhere equally strongly to laminin-5 that has been organized into arrays by other epithelial cells. These data suggest: (1) that alpha3beta1 integrin plays an important role in determining the

  16. The CAP Theorem Versus Databases with Relaxed ACID properties

    DEFF Research Database (Denmark)

    Frank, Lars; Pedersen, Rasmus Ulslev; Havnø Frank, Christian

    2014-01-01

    data from different locations can have at most two of the three desirable CAP properties [5]. The NoSQL movement has applied the CAP theorem as an argument against tradi- tional ACID (atomicity, consistency, isolation, and durabil- ity) databases, which prioritize consistency and partition- tolerance...

  17. Simultaneous measurement of cholesterol 7 alpha-hydroxylase activity by reverse-phase high-performance liquid chromatography using both endogenous and exogenous [4-14C]cholesterol as substrate

    International Nuclear Information System (INIS)

    Hylemon, P.B.; Studer, E.J.; Pandak, W.M.; Heuman, D.M.; Vlahcevic, Z.R.; Chiang, J.Y.

    1989-01-01

    The HPLC-spectrophotometric method for measuring cholesterol 7 alpha-hydroxylase activity was modified by using a C-18 reverse-phase column to separate 7 alpha-hydroxy-4-cholesten-3-one and 4-cholesten-3-one and by adding 7 beta-hydroxycholesterol to each reaction mixture as an internal recovery standard. With this method, we were able to simultaneously measure cholesterol 7 alpha-hydroxylase activity using endogenous cholesterol and exogenous [4- 14 C]cholesterol as substrate. Rat liver cytosol differentially stimulated (286%) the 7 alpha-hydroxylation of exogenous [4- 14 C]-cholesterol. In contrast, total cholesterol 7 alpha-hydroxylase activity was stimulated only 35% by cytosol. This method should prove useful for studying mechanisms of cholesterol delivery to cholesterol 7 alpha-hydroxylase

  18. On the limiting resolution of silicon detectors for short-range particles

    Energy Technology Data Exchange (ETDEWEB)

    Verbitskaya, E M; Eremin, V K; Malyarenko, A M; Strokan, N B; Sukhanov, V L

    1986-10-20

    The transition to planar tecnology has lead to substantial improvement of energy resolution of Si detectors of strongly ionizing nuclear radiations. For 5 MeV ..cap alpha..-particles the resolution (delta/sub ..cap alpha../) is equal 9.2 keV. The application of the method of local diffusion permitted to attain delta/sub ..cap alpha../=8.1-8.4 keV. The comparison of the new resolution level with the theoretical limit is carried out. It is shown that the combination of partial contributions of fluctuations caused by fundamental mechanisms practically determined delta/sub ..cap alpha../ of obtained detectors.

  19. A study of the possibility of using 3-(3'-5'Dinitro-4' - Hydroxy phenyl) phthalide as an indicator

    International Nuclear Information System (INIS)

    Khalil, A. R.; Al-Hamdany, R.

    1998-01-01

    This paper describes a ur-visible spectroscopic characterization and acid-base equilibrium studies of 3-(3 ' -5 ' -din tro-4 ' - hydroxy phenyl) phthalide (1) for its possible use as an indicator. The ionization constant (K 2 ) has been evaluated by potentiometric titration indicating that the reagent is a weak acid comparable to acetic acid. The (pK 2 ) has been attributed to deprotonation of the compound to give the corresponding anion, which possesses considerable resonance stabilization. The different colour shown by each species involved in equilibrium allows the use of this reagent as an acid-base indicator, placing the transition interval between ph 2.0 (colourless) and 3.0 (yellow). (authors). 11 refs., 1 fig., 2 tabs

  20. The relationship between red meat allergy and sensitization to gelatin and galactose-alpha-1,3-galactose

    Science.gov (United States)

    Mullins, Raymond James; James, Hayley; Platts-Mills, Thomas A.E.; Commins, Scott

    2012-01-01

    Background We have observed patients clinically allergic to red meat and meat-derived gelatin. Objective We describe a prospective evaluation of the clinical significance of gelatin sensitization, the predictive value of a positive test and an examination of the relationship between allergic reactions to red meat and sensitization to gelatin and alpha-Gal. Methods Adult patients evaluated 1997-2011 for suspected allergy/anaphylaxis to medication, insect venom or food were skin tested with gelatin colloid. In vitro (ImmunoCap) testing was undertaken where possible. Results Positive gelatin tests were observed in 40/1335 individuals; 30/40 patients with red meat allergy (12 also clinically allergic to gelatin); 2/2 with gelatin colloid anaphylaxis; 4/172 with idiopathic anaphylaxis (all responded to intravenous gelatin challenge of 0.02 to 0.4g); 4/368 with drug allergy. Testing was negative in all patients with venom allergy (n=241), non-meat food allergy (n=222), and miscellaneous disorders (n=290). ImmunoCap was positive to alpha-Gal in 20/24 meat allergics and in 20/22 with positive gelatin skin tests. The results of gelatin skin testing and anti-alpha-Gal IgE were strongly correlated (r=0.46; Pmeat were sensitized to gelatin and a subset was clinically allergic to both. The detection of alpha-Gal in gelatin and correlation between the results of alpha-Gal and gelatin testing raises the possibility that alpha-Gal IgE may be the target of reactivity to gelatin. The pathogenic relationship between tick bites and sensitization to red meat, alpha-Gal and gelatin (with or without clinical reactivity) remains uncertain. PMID:22480538

  1. The Rabies Virus L Protein Catalyzes mRNA Capping with GDP Polyribonucleotidyltransferase Activity

    Directory of Open Access Journals (Sweden)

    Minako Ogino

    2016-05-01

    Full Text Available The large (L protein of rabies virus (RABV plays multiple enzymatic roles in viral RNA synthesis and processing. However, none of its putative enzymatic activities have been directly demonstrated in vitro. In this study, we expressed and purified a recombinant form of the RABV L protein and verified its guanosine 5′-triphosphatase and GDP polyribonucleotidyltransferase (PRNTase activities, which are essential for viral mRNA cap formation by the unconventional mechanism. The RABV L protein capped 5′-triphosphorylated but not 5′-diphosphorylated RABV mRNA-start sequences, 5′-AACA(C/U, with GDP to generate the 5′-terminal cap structure G(5′ppp(5′A. The 5′-AAC sequence in the substrate RNAs was found to be strictly essential for RNA capping with the RABV L protein. Furthermore, site-directed mutagenesis showed that some conserved amino acid residues (G1112, T1170, W1201, H1241, R1242, F1285, and Q1286 in the PRNTase motifs A to E of the RABV L protein are required for cap formation. These findings suggest that the putative PRNTase domain in the RABV L protein catalyzes the rhabdovirus-specific capping reaction involving covalent catalysis of the pRNA transfer to GDP, thus offering this domain as a target for developing anti-viral agents.

  2. Alpha5beta1 integrin-fibronectin interactions specify liquid to solid phase transition of 3D cellular aggregates.

    Directory of Open Access Journals (Sweden)

    Carlos E Caicedo-Carvajal

    2010-07-01

    Full Text Available Tissue organization during embryonic development and wound healing depends on the ability of cells on the one hand to exchange adhesive bonds during active rearrangement and on the other to become fixed in place as tissue homeostasis is reached. Cells achieve these contradictory tasks by regulating either cell-cell adhesive bonds, mediated by cadherins, or cell-extracellular matrix (ECM connections, regulated by integrins. Integrin alpha5beta1 and soluble fibronectin (sFN are key players in cell-ECM force generation and in ECM polymerization. Here, we explore the interplay between integrin alpha5beta1 and sFN and its influence on tissue mechanical properties and cell sorting behavior.We generated a series of cell lines varying in alpha5beta1 receptor density. We then systematically explored the effects of different sFN concentrations on aggregate biomechanical properties using tissue surface tensiometry. We found previously unreported complex behaviors including the observation that interactions between fibronectin and integrin alpha5beta1 generates biphasic tissue cohesion profiles. Specifically, we show that at constant sFn concentration, aggregate cohesion increases linearly as alpha5beta1 receptor density is increased from low to moderate levels, producing a transition from viscoelastic-liquid to pseudo viscoelastic-solid behavior. However, further increase in receptor density causes an abrupt drop in tissue cohesion and a transition back to viscoelastic-liquid properties. We propose that this may be due to depletion of sFn below a critical value in the aggregate microenvironment at high alpha5beta1 levels. We also show that differential expression of alpha5beta1 integrin can promote phase-separation between cells.The interplay between alpha5-integrin and sFn contributes significantly to tissue cohesion and, depending on their level of expression, can mediate a shift from liquid to elastic behavior. This interplay represents a tunable level

  3. Stability constant for thorium(IV) complexes with aryl bis-(5-hydroxy-3-methyl-1-phenyl-4-pyrazolyl)-methane ligands

    Energy Technology Data Exchange (ETDEWEB)

    Stefan, L.S. [Ain Shams Univ., Cairo (Egypt)

    1995-09-01

    Chelate stability constants of aryl bis(5-hydroxy-3-methyl-1-phenyl-4-pyrazolyl)methane (ABPM) derivatives with thorium(IV) ion were determined by the potentiometric method at 30 C and 0.1 mol dm{sup -3} (KNO{sub 3}) in 75% (v/v) dioxane-water solvent. The computation of the titration data indicated that four kinds of complexes [ThL]{sup 2+}, [ThL(OH)]{sup +}, [ThL{sub 2}] and [ThL(OH){sub 2}] were formed. The appropriate formation constants for all of the 1:1 species and 2:1 complexes have been calculated are probable ligand-banding sites of the complexes were proposed. In addition, the applicability of the Hammett equation for correlation of the stability constants of [Th(IV)-ABPM] complexes was discussed. (author). 19 refs, 5 figs, 1 tab.

  4. Stability constant for thorium(IV) complexes with aryl bis-(5-hydroxy-3-methyl-1-phenyl-4-pyrazolyl)-methane ligands

    International Nuclear Information System (INIS)

    Stefan, L.S.

    1995-01-01

    Chelate stability constants of aryl bis(5-hydroxy-3-methyl-1-phenyl-4-pyrazolyl)methane (ABPM) derivatives with thorium(IV) ion were determined by the potentiometric method at 30 C and 0.1 mol dm -3 (KNO 3 ) in 75% (v/v) dioxane-water solvent. The computation of the titration data indicated that four kinds of complexes [ThL] 2+ , [ThL(OH)] + , [ThL 2 ] and [ThL(OH) 2 ] were formed. The appropriate formation constants for all of the 1:1 species and 2:1 complexes have been calculated are probable ligand-banding sites of the complexes were proposed. In addition, the applicability of the Hammett equation for correlation of the stability constants of [Th(IV)-ABPM] complexes was discussed. (author). 19 refs, 5 figs, 1 tab

  5. The 5'-poly(A leader of poxvirus mRNA confers a translational advantage that can be achieved in cells with impaired cap-dependent translation.

    Directory of Open Access Journals (Sweden)

    Pragyesh Dhungel

    2017-08-01

    Full Text Available The poly(A leader at the 5'-untranslated region (5'-UTR is an unusually striking feature of all poxvirus mRNAs transcribed after viral DNA replication (post-replicative mRNAs. These poly(A leaders are non-templated and of heterogeneous lengths; and their function during poxvirus infection remains a long-standing question. Here, we discovered that a 5'-poly(A leader conferred a selective translational advantage to mRNA in poxvirus-infected cells. A constitutive and uninterrupted 5'-poly(A leader with 12 residues was optimal. Because the most frequent lengths of the 5'-poly(A leaders are 8-12 residues, the result suggests that the poly(A leader has been evolutionarily optimized to boost poxvirus protein production. A 5'-poly(A leader also could increase protein production in the bacteriophage T7 promoter-based expression system of vaccinia virus, the prototypic member of poxviruses. Interestingly, although vaccinia virus post-replicative mRNAs do have 5'- methylated guanosine caps and can use cap-dependent translation, in vaccinia virus-infected cells, mRNA with a 5'-poly(A leader could also be efficiently translated in cells with impaired cap-dependent translation. However, the translation was not mediated through an internal ribosome entry site (IRES. These results point to a fundamental mechanism poxvirus uses to efficiently translate its post-replicative mRNAs.

  6. Improved synthesis with high yield and increased molecular weight of poly(alpha,beta-malic acid) by direct polycondensation.

    Science.gov (United States)

    Kajiyama, Tetsuto; Kobayashi, Hisatoshi; Taguchi, Tetsushi; Kataoka, Kazunori; Tanaka, Junzo

    2004-01-01

    The development of synthetic biodegradable polymers, such as poly(alpha-hydroxy acid), is particularly important for constructing medical devices, including scaffolds and sutures, and has attracted growing interest in the biomedical field. Here, we report a novel approach to preparing high molecular weight poly(malic acid) (HMW--PMA) as a biodegradable and bioabsorbable water-soluble polymer. We investigated in detail the reaction conditions for the simple direct polycondensation of l-malic acid, including the reaction times, temperatures, and catalysts. The molecular weight of synthesized alpha,beta-PMA is dependent on both the reaction temperature and time. The optimum reaction condition to obtain alpha,beta-PMA by direct polycondensation using tin(II) chloride as a catalyst was thus determined to be 110 degrees C for 45 h with a molecular weight of 5300. The method for alpha,beta-PMA synthesis established here will facilitate production of alpha,beta-PMA of various molecular weights, which may have a potential utility as biomaterials.

  7. Molecularly imprinted poly(4-amino-5-hydroxy-2,7-naphthalenedisulfonic acid) modified glassy carbon electrode as an electrochemical theophylline sensor

    International Nuclear Information System (INIS)

    Aswini, K.K.; Vinu Mohan, A.M.; Biju, V.M.

    2016-01-01

    Theophylline is an inexpensive drug employed in asthma and chronic obstructive pulmonary disorder medications and is toxic at higher concentration. The development of a molecularly imprinted polymer based theophylline electrochemical sensor on glassy carbon electrode by the electropolymerization of 4-amino-5-hydroxy-2,7-naphthalenedisulfonic acid is being discussed in this work. The MIP modification enhances the theophylline recognition ability and the electron transfer kinetics of the bare electrode. The parameters, controlling the performance of the imprinted polymer based sensor, like number of electropolymerization cycles, composition of the pre-polymerization mixture, pH and immersion time were investigated and optimized. The interaction energy and the most stable conformation of the template–monomer complex in the pre-polymerization mixture were determined computationally using ab initio calculations based on density functional theory. The amperometric measurements showed that the developed sensor has a method detection limit of 0.32 μM for the dynamic range of 0.4 to 17 μM, at optimized conditions. The transducer possesses appreciable selectivity in the presence of structurally similar interferents such as theobromine, caffeine and doxofylline. The developed sensor showed remarkable stability and reproducibility and was also successfully employed in theophylline detection from commercially available tablets. - Highlights: • Molecularly imprinted polymer based theophylline sensor was developed. • Imprinted poly(4-amino-5-hydroxy-2,7-naphthalenedisulfonic acid) was electrodeposited. • Most stable template-monomer complex was assigned by computational analysis. • Possessed remarkable selectivity in the presence of structurally similar interferents • Employed for theophylline detection from commercially available tablets

  8. Molecularly imprinted poly(4-amino-5-hydroxy-2,7-naphthalenedisulfonic acid) modified glassy carbon electrode as an electrochemical theophylline sensor

    Energy Technology Data Exchange (ETDEWEB)

    Aswini, K.K., E-mail: aswinikk@ymail.com; Vinu Mohan, A.M.; Biju, V.M., E-mail: vmbiju@ymail.com

    2016-08-01

    Theophylline is an inexpensive drug employed in asthma and chronic obstructive pulmonary disorder medications and is toxic at higher concentration. The development of a molecularly imprinted polymer based theophylline electrochemical sensor on glassy carbon electrode by the electropolymerization of 4-amino-5-hydroxy-2,7-naphthalenedisulfonic acid is being discussed in this work. The MIP modification enhances the theophylline recognition ability and the electron transfer kinetics of the bare electrode. The parameters, controlling the performance of the imprinted polymer based sensor, like number of electropolymerization cycles, composition of the pre-polymerization mixture, pH and immersion time were investigated and optimized. The interaction energy and the most stable conformation of the template–monomer complex in the pre-polymerization mixture were determined computationally using ab initio calculations based on density functional theory. The amperometric measurements showed that the developed sensor has a method detection limit of 0.32 μM for the dynamic range of 0.4 to 17 μM, at optimized conditions. The transducer possesses appreciable selectivity in the presence of structurally similar interferents such as theobromine, caffeine and doxofylline. The developed sensor showed remarkable stability and reproducibility and was also successfully employed in theophylline detection from commercially available tablets. - Highlights: • Molecularly imprinted polymer based theophylline sensor was developed. • Imprinted poly(4-amino-5-hydroxy-2,7-naphthalenedisulfonic acid) was electrodeposited. • Most stable template-monomer complex was assigned by computational analysis. • Possessed remarkable selectivity in the presence of structurally similar interferents • Employed for theophylline detection from commercially available tablets.

  9. Novel leads from Heliotropium ovalifolium, 4,7,8-trimethoxy-naphthalene-2-carboxylic acid and 6-hydroxy-5,7-dimethoxy-naphthalene-2-carbaldehyde show specific IL-6 inhibitory activity in THP-1 cells and primary human monocytes.

    Science.gov (United States)

    Kulkarni-Almeida, Asha; Suthar, Ashish; Goswami, Hitesh; Vishwakarma, Ram; Chauhan, Vijay Singh; Balakrishnan, Arun; Sharma, Somesh

    2008-12-01

    From our screening program, we identified the anti-inflammatory effects of the extracts of Heliotropium ovalifolium in its ability to inhibit specific cytokines. The H. ovalifolium extract was found to be moderately active with an IC(50) equaling 10 microg/ml for inhibition of interleukin-6 (IL-6) in a human monocytic cell line. Interleukin-6 is a pleiotropic cytokine with implications in the regulation of the immune response, inflammation and hematopoiesis. This prompted us to examine and identify the active molecules that are responsible for the bioactivity in THP-1 cells. Bioassay guided fractionation identified two compounds 4,7,8-trimethoxy-naphthalene-2-carboxylic acid and 6-hydroxy-5,7-dimethoxy-naphthalene-2-carbaldehyde with an IC(50) of 2.4 and 2.0 microM for IL-6 inhibition and an IC(50) of 15.6 and 7.0 microM for tumor necrosis factor-alpha (TNF-alpha) inhibition in THP-1 cells. The protein expression data were supported by the inhibitory effect on mRNA gene expression. The compounds isolated from H. ovalifolium were also non-toxic in human peripheral blood monocytes from normal donors and the activity profile was similar to that obtained on THP-1 cells. Thus, we believe that these scaffolds may be of interest to develop leads for treating rheumatoid arthritis, psoriasis, ulcerative colitis, Crohn's disease and other inflammatory disorders. However, more detailed investigations need to be carried out to explain the efficacy of these compounds as drugs.

  10. Preparation of ω-hydroxy pelargonic acid

    Science.gov (United States)

    Hadi, Siti Faieza Abd; Salimon, Jumat

    2018-04-01

    Utilization of plant oil as renewable raw material for monomers and polymers in bioplastic industry has a great potential to replace conventional petroleum-based plastic usage especially in packaging and adhesive applications. One of useful monomer is ω-hydroxy pelargonic acid that can be polymerizing as biodegradable polyester. In this study, the aim is to synthesis ω-hydroxy pelargonic acid from oleic acid based on oxidation/ esterification/ saponification and reduction methodology. The yield obtained after aqueous workup is 53% and the compound structure is determined by FT-IR and 1H and 13C NMR.

  11. Oxidation of C18 Hydroxy-Polyunsaturated Fatty Acids to Epoxide or Ketone by Catalase-Related Hemoproteins Activated with Iodosylbenzene.

    Science.gov (United States)

    Teder, Tarvi; Boeglin, William E; Brash, Alan R

    2017-07-01

    Small catalase-related hemoproteins with a facility to react with fatty acid hydroperoxides were examined for their potential mono-oxygenase activity when activated using iodosylbenzene. The proteins tested were a Fusarium graminearum 41 kD catalase hemoprotein (Fg-cat, gene FGSG_02217), a Pseudomonas fluorescens Pfl01 catalase (37.5 kD, accession number WP_011333788.1), and a Mycobacterium avium ssp. paratuberculosis 33 kD catalase (gene MAP-2744c). 13-Hydroxy-octadecenoic acids (which are normally unreactive) were selected as substrates because these enzymes react specifically with the corresponding 13S-hydroperoxides (Pakhomova et al. 18:2559-2568, 5; Teder et al. 1862:706-715, 14). In the presence of iodosylbenzene Fg-cat converted 13S-hydroxy-fatty acids to two products: the 15,16-double bond of 13S-hydroxy α-linolenic acid was oxidized stereospecifically to the 15S,16R-cis-epoxide or the 13-hydroxyl was oxidized to the 13-ketone. Products were identified by UV, HPLC, LC-MS, NMR and by comparison with authentic standards prepared for this study. The Pfl01-cat displayed similar activity. MAP-2744c oxidized 13S-hydroxy-linoleic acid to the 13-ketone, and epoxidized the double bonds to form the 9,10-epoxy-13-hydroxy, 11,12-epoxy-13-hydroxy, and 9,10-epoxy-13-keto derivatives; equivalent transformations occurred with 9S-hydroxy-linoleic acid as substrate. In parallel incubations in the presence of iodosylbenzene, human catalase displayed no activity towards 13S-hydroxy-linoleic acid, as expected from the highly restricted access to its active site. The results indicated that with suitable transformation to Compound I, monooxygenase activity can be demonstrated by these catalase-related hemoproteins with tyrosine as the proximal heme ligand.

  12. A nanobody targeting the F-actin capping protein CapG restrains breast cancer metastasis.

    Science.gov (United States)

    Van Impe, Katrien; Bethuyne, Jonas; Cool, Steven; Impens, Francis; Ruano-Gallego, David; De Wever, Olivier; Vanloo, Berlinda; Van Troys, Marleen; Lambein, Kathleen; Boucherie, Ciska; Martens, Evelien; Zwaenepoel, Olivier; Hassanzadeh-Ghassabeh, Gholamreza; Vandekerckhove, Joël; Gevaert, Kris; Fernández, Luis Ángel; Sanders, Niek N; Gettemans, Jan

    2013-12-13

    Aberrant turnover of the actin cytoskeleton is intimately associated with cancer cell migration and invasion. Frequently however, evidence is circumstantial, and a reliable assessment of the therapeutic significance of a gene product is offset by lack of inhibitors that target biologic properties of a protein, as most conventional drugs do, instead of the corresponding gene. Proteomic studies have demonstrated overexpression of CapG, a constituent of the actin cytoskeleton, in breast cancer. Indirect evidence suggests that CapG is involved in tumor cell dissemination and metastasis. In this study, we used llama-derived CapG single-domain antibodies or nanobodies in a breast cancer metastasis model to address whether inhibition of CapG activity holds therapeutic merit. We raised single-domain antibodies (nanobodies) against human CapG and used these as intrabodies (immunomodulation) after lentiviral transduction of breast cancer cells. Functional characterization of nanobodies was performed to identify which biochemical properties of CapG are perturbed. Orthotopic and tail vein in vivo models of metastasis in nude mice were used to assess cancer cell spreading. With G-actin and F-actin binding assays, we identified a CapG nanobody that binds with nanomolar affinity to the first CapG domain. Consequently, CapG interaction with actin monomers or actin filaments is blocked. Intracellular delocalization experiments demonstrated that the nanobody interacts with CapG in the cytoplasmic environment. Expression of the nanobody in breast cancer cells restrained cell migration and Matrigel invasion. Notably, the nanobody prevented formation of lung metastatic lesions in orthotopic xenograft and tail-vein models of metastasis in immunodeficient mice. We showed that CapG nanobodies can be delivered into cancer cells by using bacteria harboring a type III protein secretion system (T3SS). CapG inhibition strongly reduces breast cancer metastasis. A nanobody-based approach offers

  13. Untersuchungen zur Erdbeerfruchtreifung : Biosynthese von 4-Hydroxy-2,5-dimethyl-3(2H)-furanon und Enzymaktivitäten während des Reifungsprozesses

    OpenAIRE

    Raab, Thomas

    2004-01-01

    Die Fruchtreifung stellt einen hochkomplexen Prozess dar, der durch eine Reihe von biochemischen und physiologischen Veränderungen gekennzeichnet ist. Dies umfasst bedeutende Veränderungen von Textur, Farbe sowie die Bildung von geschmacks- und geruchsaktiven Verbindungen. Die vorliegende Arbeit präsentiert neue Erkenntnisse zur Biosynthese von 4-Hydroxy-2,5-dimethyl-3(2H)-furanon (Furaneol®, HDMF), einer Schlüssel-Aromakomponente der Erdbeere (Fragaria x ananassa). Daneben lieferten die durc...

  14. O-hydroxy-functionalized diamines, polymides, methods of making each, and methods of use

    KAUST Repository

    Ma, Xiaohua; Ghanem, Bader S.; Pinnau, Ingo

    2016-01-01

    Embodiments of the present disclosure provide for an ortho (o)-hydroxy-functionalized diamine, a method of making an o-hydroxy-functionalized diamine, an o-hydroxy-functionalized diamine-based polyimide, a method of making an o-hydroxy-functionalized diamine imide, methods of gas separation, and the like.

  15. O-hydroxy-functionalized diamines, polymides, methods of making each, and methods of use

    KAUST Repository

    Ma, Xiaohua

    2016-01-21

    Embodiments of the present disclosure provide for an ortho (o)-hydroxy-functionalized diamine, a method of making an o-hydroxy-functionalized diamine, an o-hydroxy-functionalized diamine-based polyimide, a method of making an o-hydroxy-functionalized diamine imide, methods of gas separation, and the like.

  16. Characterization of a Novel Nicotine Hydroxylase from Pseudomonas sp. ZZ-5 That Catalyzes the Conversion of 6-Hydroxy-3-Succinoylpyridine into 2,5-Dihydroxypyridine

    Directory of Open Access Journals (Sweden)

    Tao Wei

    2017-08-01

    Full Text Available A novel nicotine hydroxylase was isolated from Pseudomonas sp. ZZ-5 (HSPHZZ. The sequence encoding the enzyme was 1206 nucleotides long, and encoded a protein of 401 amino acids. Recombinant HSPHZZ was functionally overexpressed in Escherichia coli BL21-Codon Plus (DE3-RIL cells and purified to homogeneity after Ni-NTA affinity chromatography. Liquid chromatography-mass spectrometry (LC-MS analyses indicated that the enzyme could efficiently catalyze the conversion of 6-hydroxy-3-succinoylpyridine (HSP into 2,5-dihydroxypyridine (2,5-DHP and succinic acid in the presence of nicotinamide adenine dinucleotide (NADH and flavin adenine dinucleotide (FAD. The kinetic constants (Km, kcat, and kcat/Km of HSPHZZ toward HSP were 0.18 mM, 2.1 s−1, and 11.7 s−1 mM−1, respectively. The optimum temperature, pH, and optimum concentrations of substrate and enzyme for 2,5-DHP production were 30 °C, 8.5, 1.0 mM, and 1.0 μM, respectively. Under optimum conditions, 85.3 mg/L 2,5-DHP was produced in 40 min with a conversion of 74.9%. These results demonstrated that HSPHZZ could be used for the enzymatic production of 2,5-DHP in biotechnology applications.

  17. 21 CFR 582.5477 - Methionine hydroxy analog and its calcium salts.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Methionine hydroxy analog and its calcium salts... Nutrients and/or Dietary Supplements 1 § 582.5477 Methionine hydroxy analog and its calcium salts. (a) Product. Methionine hydroxy analog and its calcium salts. (b) [Reserved] (c) Limitations, restrictions, or...

  18. Buy badges and help finance Cap Loisirs activities!

    CERN Multimedia

    2008-01-01

    Please give a warm welcome to Cap Loisirs’ volunteers who will be manning a stand at the main entrance on Friday 8 February! In honour of St. Valentine’s Day, they will be selling a selection of 5 badges designed by artist Anna Sommer, depicting declarations of love by our friends from the animal kingdom. Price : Frs. 3.- per badge The aim of Fondation Cap Loisirs is to provide leisure activities for mentally handicapped children, adolescents and adults. The Foundation offers a wide range of activities which allow the mentally handicapped to enjoy quality leisure in areas as varied as culture, sport, tourism, travel and artistic expression. Fondation Cap Loisirs Rue de Monthoux 66 – 1201 Geneva – Tel: 022 731 86 00 – CCP Genève 12-5587-5 – caploisirs@caploisirs.ch – http://www.Caploisirs.ch

  19. Contact allergy to 2-hydroxy-5-tert-butyl benzylalcohol and 2,6-bis(hydroxymethyl)-4-tert-butylphenol, components of a phenolic resin used in marking pens

    DEFF Research Database (Denmark)

    Hagdrup, H; Egsgaard, H; Carlsen, L

    1994-01-01

    2-hydroxy-5-tert-butyl benzylalcohol and 2,6-bis(hydroxymethyl)-4-tert-butylphenol were identified as contact allergens in a phenolic resin used as a tackifier in the ink of a marking pen, which, after being used directly on the skin, caused an acute contact dermatitis on the hand of a 13-year...

  20. Studies on the characterization and regulation of alpha-1 adrenergic receptors and [3H]WB4101 binding sites in the central nervous system

    International Nuclear Information System (INIS)

    Morrow, A.L.

    1985-01-01

    The purpose of these studies has been to resolve the anomalous binding characteristics of two alpha adrenergic receptor ligands, [ 3 H]WB4101 and [ 3 H]prazosin and to study the regulation of the receptors labeled by these compounds after surgical denervation and chronic drug treatments. Preliminary studies indicated that [ 3 H]WB4101 binding sites, which were believed to represent alpha-1 adrenergic receptors, were increased in number following removal of the fimbrial afferents to the hippocampus. This increase was not due to removal of the adrenergic input into this structure since destruction of the locus coeruleus or the dorsal noradrenergic bundle did not produce the up-regulation. Characterization of alpha-1 adrenergic receptors using [ 3 H]prazosin and [ 3 H]WB4101 revealed evidence for subtypes of alpha-1 receptors designated alpha-1A and alpha-1B. The nanomolar affinity component of [ 3 H]WB4101 binding is not adrenergic but serotonergic. The serotonergic agonists, serotonin and 8-hydroxy-dipropylaminotetraline have affinities of 1.5 and 3.0 nM for this site, when studied in the presence of a 30 nM prazosin mask of the alpha-1 component of [ 3 H]WB4101 binding. Fimbria transection or 5,7 dihydroxytryptamine injections produced increases in the Bmax of the nanomolar affinity component of [ 3 H]WB4101 binding in the presence of a prazosin mask. The up-regulated site showed identical serotonergic pharmacology compared to control tissue. Thus, the author concluded that serotonergic denervation of the hippocampus produces the increase in serotonergic binding sites labeled by [ 3 H]WB4101

  1. Influence of rete testis fluid deprivation on the kinetic parameters of goat epididymal 5 alpha-reductase.

    Science.gov (United States)

    Kelce, W R; Lubis, A M; Braun, W F; Youngquist, R S; Ganjam, V K

    1990-01-01

    A surgical technique to cannulate the rete testis of the goat was utilized to examine the effects of rete testis fluid (RTF) deprivation on the enzymatic activity of epididymal 5 alpha-reductase. Kinetic techniques were used to determine whether the regional enzymatic effect of RTF deprivation is to decrease the apparent number of 5 alpha-reductase active sites or the catalytic activity of each active site within the epididymal epithelium. Paired comparisons of (Vmax)app and (Km)app values between control and RTF-deprived epididymides indicated that RTF deprivation affected the value of (Vmax)app with no apparent change in the values of (Km)app in caput, corpus, and cauda epididymal regions. We conclude that RTF deprivation in the goat epididymis for 7 days results in a decreased number of apparent 5 alpha-reductase active sites within the epididymal epithelium.

  2. Prooxidant action of furanone compounds: implication of reactive oxygen species in the metal-dependent strand breaks and the formation of 8-hydroxy-2'-deoxyguanosine in DNA.

    Science.gov (United States)

    Murakami, K; Haneda, M; Makino, T; Yoshino, M

    2007-07-01

    Prooxidant properties of furanone compounds including 2,5-furanone (furaneol, 4-hydroxy-2,5-dimethyl-furan-3-one), 4,5-furanone (4,5-dimethyl-3-hydroxy-2(5H)-furanone) (sotolone) and cyclotene (2-hydroxy-3-methyl-2-cyclopenten-1-one) were analyzed in relation to the metal-reducing activity. Only 2.5-furanone known as a "strawberry or pineapple furanone" inactivated aconitase the most sensitive enzyme to active oxygen in the presence of ferrous sulfate, suggesting the furaneol/iron-mediated generation of reactive oxygen species. 2,5-Furanone caused strand scission of pBR322 DNA in the presence of copper. Treatment of calf thymus DNA with 2,5-furanone plus copper produced 8-hydroxy-2'-deoxyguanosine in DNA. 2,5-Furanone showed a potent copper-reducing activity, and thus, DNA strand breaks and the formation of 8-hydroxy-2'-deoxyguanosine by 2,5-furanone can be initiated by the production of superoxide radical through the reduction of cupric ion to cuprous ion, resulting in the conversion to hydrogen peroxide and hydroxyl radical. However, an isomer and analog of 2,5-furanone, 4,5-furanone and cyclotene, respectively, did not show an inactivation of aconitase, DNA injuries including strand breakage and the formation of 8-hydroxy-2'-deoxyguanosine, and copper-reducing activity. Cytotoxic effect of 2,5-furanone with hydroxyketone structure can be explained by its prooxidant properties: furaneol/transition metal complex generates reactive oxygen species causing the inactivation of aconitase and the formation of DNA base damage by hydroxyl radical.

  3. Molecular structure, spectral studies, NBO, HOMO-LUMO profile, MEP and Mulliken analysis of 3β,6β-dichloro-5α-hydroxy-5α-cholestane

    Science.gov (United States)

    Alam, Mahboob; Park, Soonheum

    2018-05-01

    The synthesis of 3β,6β-dichloro-5α-hydroxy-5α-cholestane (in general, steroidal chlorohydrin or steroidal halohydrin) and theoretical study of the structure are reported in this paper. The individuality of chlorohydrin was confirmed by FT-IR, NMR, MS, CHN microanalysis and X-ray crystallography. DFT calculations on the titled molecule have been performed. The molecular structure and spectra explained by Gaussian hybrid computational analysis theory (B3LYP) are found to be in correlation with the experimental data obtained from the various spectrophotometric techniques. The theoretical geometry optimization data were compared with the X-ray data. The vibrational bands appearing in the FT-IR are assigned with accuracy using harmonic frequencies along with intensities and animated modes. Molecular properties like NBO, HOMO-LUMO analysis, chemical reactivity descriptors, MEP mapping and dipole moment have been dealt at same level of theory. The calculated electronic spectrum of chlorohydrin is interpreted on the basis of TD-DFT calculations.

  4. How does the antagonism between capping and anti-capping proteins affect actin network dynamics?

    International Nuclear Information System (INIS)

    Hu Longhua; Papoian, Garegin A

    2011-01-01

    Actin-based cell motility is essential to many biological processes. We built a simplified, three-dimensional computational model and subsequently performed stochastic simulations to study the growth dynamics of lamellipodia-like branched networks. In this work, we shed light on the antagonism between capping and anti-capping proteins in regulating actin dynamics in the filamentous network. We discuss detailed mechanisms by which capping and anti-capping proteins affect the protrusion speed of the actin network and the rate of nucleation of filaments. We computed a phase diagram showing the regimes of motility enhancement and inhibition by these proteins. Our work shows that the effects of capping and anti-capping proteins are mainly transmitted by modulation of the filamentous network density and local availability of monomeric actin. We discovered that the combination of the capping/anti-capping regulatory network with nucleation-promoting proteins introduces robustness and redundancy in cell motility machinery, allowing the cell to easily achieve maximal protrusion speeds under a broader set of conditions. Finally, we discuss distributions of filament lengths under various conditions and speculate on their potential implication for the emergence of filopodia from the lamellipodial network.

  5. 47 CFR 54.623 - Cap.

    Science.gov (United States)

    2010-10-01

    ... 47 Telecommunication 3 2010-10-01 2010-10-01 false Cap. 54.623 Section 54.623 Telecommunication... Universal Service Support for Health Care Providers § 54.623 Cap. (a) Amount of the annual cap. The annual cap on federal universal service support for health care providers shall be $400 million per funding...

  6. 47 CFR 54.507 - Cap.

    Science.gov (United States)

    2010-10-01

    ... 47 Telecommunication 3 2010-10-01 2010-10-01 false Cap. 54.507 Section 54.507 Telecommunication... Universal Service Support for Schools and Libraries § 54.507 Cap. (a) Amount of the annual cap. The annual funding cap on federal universal service support for schools and libraries shall be $2.25 billion per...

  7. Magnetic nanoparticles grafted with β-cyclodextrin for solid-phase extraction of 5-hydroxy-3-indole acetic acid

    International Nuclear Information System (INIS)

    Ahmed, Gaber Hashem Gaber; Laíño, Rosana Badía; Calzón, Josefa Angela García; García, Marta Elena Díaz

    2014-01-01

    We describe the synthesis of β-cyclodextrin modified magnetic nanoparticles (CD-mNPs) as a material for solid-phase extraction of the cancer biomarker 5-hydroxy-indole-3-acetic acid (5-HIAA) from urine. The CD-mNPs were characterized by TEM, FTIR, and XRD, and the kinetics and adsorption isotherms were studied. The strong interaction between the CD-mNPs and 5-HIAA is the main driving force for recognition and extraction, while the magnetic core of the NPs allows their separation from the sample matrix. Recovery of 5-HIAA from the adsorbent using an adequate solvent regenerated the adsorbent for further use. 5-HIAA was then quantified by fluorometry of its complex with β-CD. The method works in the 1 × 10 −7 to 1 × 10 −5 mol L −1 (R 2 0.9982–0.9996) concentration range, and the limits of detection (3σ) and quantification (10 σ) of the method are 1.2 × 10 −8 mol L −1 and 4.01 × 10 −8 mol L −1 5-HIAA, respectively. The recovery of 5-HIAA from urine samples spiked with 5-HIAA in three concentrations (1.4 × 10 −6 , 4.50 × 10 −6 and 1.0 × 10 −5 mol L −1 ) are within 63 ± 3 %. (author)

  8. A thermoelectric cap for seafloor hydrothermal vents

    International Nuclear Information System (INIS)

    Xie, Yu; Wu, Shi-jun; Yang, Can-jun

    2016-01-01

    Highlights: • We developed a thermoelectric cap (TC) to harvest hydrothermal energy. • The TC was deployed at a hydrothermal vent site near Kueishantao islet, Taiwan. • The TC monitored the temperature of the hydrothermal fluids during the field test. • The TC could make the thermal energy of hydrothermal fluids a viable power source. - Abstract: Long-term in situ monitoring is crucial to seafloor scientific investigations. One of the challenges of operating sensors in seabed is the lifespan of the sensors. Such sensors are commonly powered by batteries when other alternatives, such as tidal or solar energy, are unavailable. However, the batteries have a limited lifespan and must be recharged or replaced periodically, which is costly and impractical. A thermoelectric cap, which harvests the thermal energy of hydrothermal fluids through a conduction pipe and converts the heat to electrical energy by using thermoelectric generators, was developed to avoid these inconveniences. The thermoelectric cap was combined with a power and temperature measurement system that enables the thermoelectric cap to power a light-emitting diode lamp, an electronic load (60 Ω), and 16 thermocouples continuously. The thermoelectric cap was field tested at a shallow hydrothermal vent site near Kueishantao islet, which is located offshore of northeastern Taiwan. By using the thermal gradient between hydrothermal fluids and seawater, the thermoelectric cap obtained a sustained power of 0.2–0.5 W during the field test. The thermoelectric cap successfully powered the 16 thermocouples and recorded the temperature of the hydrothermal fluids during the entire field test. Our results show that the thermal energy of hydrothermal fluids can be an alternative renewable power source for oceanographic research.

  9. Traducción independiente de la estructura 5´cap del ARN genómico del virus dengue

    Directory of Open Access Journals (Sweden)

    Mariela Pérez Dominguez

    Full Text Available Objetivos. Analizar la participación de la caperuza metil-guanosín-trifosfato (5´cap y de la región inicial del ARN genómico del virus dengue serotipo 2 (DENV-2 genotipo Americano en la traducción, utilizando un sistema libre de células obtenido de placenta humana. Materiales y métodos. Se preparó el plásmido recombinante pTZ18R-D2 conteniendo el ADN que codifica la 5´UTR y los primeros 201 nucleótidos de la cápside viral. Este plásmido se utilizó para transcribir el ARN correspondiente (ARN-D2, sin la 5´cap. El ARN-D2 fue traducido en un sistema constituido por la fracción posmitocondrial (S-30 de placenta humana y se evaluó la incorporación de [ 14C] aminoácidos en presencia del ARN-D2 y en su ausencia (control. Se diseñaron siete oligonucleótidos antisentido (OAs1-7 dirigidos contra secuencias de las estructuras SLA, SLB y cHP del ARN-D2 y se analizó el efecto de los mismos sobre la traducción ARN-D2. Resultados. El ARN-D2 produjo un incremento significativo (p<0,001 en la incorporación de [14C] aminoácidos, con estimulación del 75% de la actividad traduccional respecto al control. El análisis de los productos de traducción mostró un pico de incorporación correspondiente a péptidos con peso molecular aparente cercano al esperado (7,746 kDa. El OAs5, complementario a una secuencia de la estructura SLB del ARN-D2, inhibió completamente la traducción. Conclusiones. El ARN-D2 fue traducido de manera específica y eficiente, bajo condiciones semejantes a las intracelulares en humanos, por un mecanismo alternativo independiente de la 5´cap, que involucraría a la estructura SLB. Este mecanismo podría considerarse como blanco en el desarrollo de terapias antisentido para inhibir la reproducción del virus.

  10. Structural studies on Mannich bases of 2-Hydroxy-3,4,5,6-tetrachlorobenzene. An UV, IR, NMR and DFT study. A mini-review

    DEFF Research Database (Denmark)

    Hansen, Poul Erik; Spanget-Larsen, Jens

    2016-01-01

    Mannich bases of 2-Hydroxy-3,4,5,6-tetrachlorobenzene are chosen as an exemplary case for tautomeric Mannich bases. Molecular structures are calculated. OH stretching frequencies are rationalized based on DFT calculations. Intrinsic deuterium isotope effects on 13C chemical shifts in the M-form a......-form are estimated based on OH bond lengths. The observed deuterium isotope effects on 13C chemical shifts are demonstrated to be largely of equilibrium type except at ambient temperatures....

  11. Cytotoxic and antibacterial activities of sesquiterpene lactones isolated from Tanacetum praeteritum subsp praeteritum

    NARCIS (Netherlands)

    Goren, N; Woerdenbag, HJ; BozokJohansson, C

    1996-01-01

    Ten sesquiterpene lactones and one sesquiterpene isolated from Tanacetum praeteritum subsp. praeteritum: 1 alpha,6 alpha-dihydroxyisocostic acid methyl ester (2), 1 alpha-hydroxy-1-deoxoarglanine (3), douglanin (5), santamarin (6), reynosin (7), 1-epi-tatridin B (8), ludovicin A (10), armexin (12),

  12. Polyethylene versus cotton cap as an adjunct to body wrap in preterm infants.

    Science.gov (United States)

    Shafie, Hashim; Syed Zakaria, Syed Zulkifli; Adli, Ali; Shareena, Ishak; Rohana, Jaafar

    2017-07-01

    Occlusive body wrap using polyethylene plastic applied immediately after birth had been shown to reduce hypothermia among preterm infants. Various adjunct methods have been studied in an attempt to further reduce the incidence of hypothermia. This study was conducted to determine whether polyethylene cap is more effective than cotton cap as an adjunct to polyethylene occlusive body wrap in reducing hypothermia in preterm infants. The subjects consisted of preterm infants 24-34 weeks' gestation born at Universiti Kebangsaan Malaysia Medical Centre. Infants were randomly assigned to NeoCap or control groups. Infants in both groups were wrapped in polyethylene sheets from the neck downwards immediately after birth without prior drying. Infants in the control group had their heads dried and subsequently covered with cotton caps while infants in the NeoCap group had polyethylene caps put on without drying. Axillary temperature was measured on admission to the neonatal intensive care unit (NICU), and after having been stabilized in the incubator. Among the 80 infants recruited, admission hypothermia (axillary temperature <36.5°C) was present in 37 (92.5%) and in 40 (100%) in the NeoCap and control groups, respectively. There was no significant difference in mean temperature on NICU admission between the two groups (35.3 vs 35.1°C, P = 0.36). Mean post-stabilization temperature, however, was significantly higher in the NeoCap group (36.0 vs 35.5°C, P = 0.01). Combined use of polyethylene body wrap and polyethylene cap was associated with a significantly higher mean post-stabilization temperature compared with polyethylene body wrap and cotton cap. © 2017 Japan Pediatric Society.

  13. Preparation and characterization of highly water-soluble magnetic Fe3O4 nanoparticles via surface double-layered self-assembly method of sodium alpha-olefin sulfonate

    International Nuclear Information System (INIS)

    Li, Honghong; Qin, Li; Feng, Ying; Hu, Lihua; Zhou, Chunhua

    2015-01-01

    A kind of double-layered self-assembly sodium alpha-olefin sulfonate (AOS) capped Fe 3 O 4 magnetic nanoparticles (Fe 3 O 4 -AOS-MN) with highly water-solubility was prepared by a wet co-precipitation method with a pH of 4.8. The resulting Fe 3 O 4 -AOS-MN could be dispersed into water to form stable magnetic fluid without other treatments. The result of X-ray diffraction (XRD) indicated that the Fe 3 O 4 -AOS-MN maintained original crystalline structure and exhibited a diameter of about 7.5 nm. The iron oxide phase of nanoparticles determined by Raman spectroscopy is Fe 3 O 4 . Transmission electron microscopy (TEM) analysis confirmed that the Fe 3 O 4 -AOS-MN with spherical morphology were uniformly dispersed in water. FT-IR spectroscopy (FT-IR) and thermo-gravimetric analysis (TGA) verified the successful preparation of Fe 3 O 4 -AOS-MN capped with double-layered self-assembled AOS. The corresponding capacities of monolayer chemical absorption and the second-layer self-assembly absorption were respectively 4.07 and 14.71 wt% of Fe 3 O 4 -MN, which were much lower than those of other surfactants. Vibrating sample magnetometer (VSM) test result showed Fe 3 O 4 -AOS-MN possessed superparamagnetic behavior with the saturation magnetization value of about 44.45 emu/g. The blocking temperature T B of Fe 3 O 4 -AOS-MN capped with double-layered AOS is 170 K. - Highlights: • Double-layered self-assembly sodium alpha-olefin sulfonate (AOS) capped Fe 3 O 4 magnetic nanoparticles are prepared by a wet co-precipitation method. • Double-layered Fe 3 O 4 -AOS-MN exhibits highly water-solubility. • The iron oxide phase is determined by Raman spectroscopy. • Fe 3 O 4 -AOS-MN capped with double-layered AOS possesses super-paramagnetic behavior. • The blocking temperature T B of Fe 3 O 4 -AOS-MN capped with double-layered AOS is 170 K

  14. The utrophin A 5'-UTR drives cap-independent translation exclusively in skeletal muscles of transgenic mice and interacts with eEF1A2.

    Science.gov (United States)

    Miura, P; Coriati, A; Bélanger, G; De Repentigny, Y; Lee, J; Kothary, R; Holcik, M; Jasmin, B J

    2010-04-01

    The molecular mechanisms regulating expression of utrophin A are of therapeutic interest since upregulating its expression at the sarcolemma can compensate for the lack of dystrophin in animal models of Duchenne Muscular Dystrophy (DMD). The 5'-UTR of utrophin A has been previously shown to drive cap-independent internal ribosome entry site (IRES)-mediated translation in response to muscle regeneration and glucocorticoid treatment. To determine whether the utrophin A IRES displays tissue specific activity, we generated transgenic mice harboring control (CMV/betaGAL/CAT) or utrophin A 5'-UTR (CMV/betaGAL/UtrA/CAT) bicistronic reporter transgenes. Examination of multiple tissues from two CMV/betaGAL/UtrA/CAT lines revealed that the utrophin A 5'-UTR drives cap-independent translation of the reporter gene exclusively in skeletal muscles and no other examined tissues. This expression pattern suggested that skeletal muscle-specific factors are involved in IRES-mediated translation of utrophin A. We performed RNA-affinity chromatography experiments combined with mass spectrometry to identify trans-factors that bind the utrophin A 5'-UTR and identified eukaryotic elongation factor 1A2 (eEF1A2). UV-crosslinking experiments confirmed the specificity of this interaction. Regions of the utrophin A 5'-UTR that bound eEF1A2 also mediated cap-independent translation in C2C12 muscle cells. Cultured cells lacking eEF1A2 had reduced IRES activity compared with cells overexpressing eEF1A2. Together, these results suggest an important role for eEF1A2 in driving cap-independent translation of utrophin A in skeletal muscle. The trans-factors and signaling pathways driving skeletal-muscle specific IRES-mediated translation of utrophin A could provide unique targets for developing pharmacological-based DMD therapies.

  15. The pharmaceutical vial capping process: Container closure systems, capping equipment, regulatory framework, and seal quality tests.

    Science.gov (United States)

    Mathaes, Roman; Mahler, Hanns-Christian; Buettiker, Jean-Pierre; Roehl, Holger; Lam, Philippe; Brown, Helen; Luemkemann, Joerg; Adler, Michael; Huwyler, Joerg; Streubel, Alexander; Mohl, Silke

    2016-02-01

    Parenteral drug products are protected by appropriate primary packaging to protect against environmental factors, including potential microbial contamination during shelf life duration. The most commonly used CCS configuration for parenteral drug products is the glass vial, sealed with a rubber stopper and an aluminum crimp cap. In combination with an adequately designed and controlled aseptic fill/finish processes, a well-designed and characterized capping process is indispensable to ensure product quality and integrity and to minimize rejections during the manufacturing process. In this review, the health authority requirements and expectations related to container closure system quality and container closure integrity are summarized. The pharmaceutical vial, the rubber stopper, and the crimp cap are described. Different capping techniques are critically compared: The most common capping equipment with a rotating capping plate produces the lowest amount of particle. The strength and challenges of methods to control the capping process are discussed. The residual seal force method can characterize the capping process independent of the used capping equipment or CCS. We analyze the root causes of several cosmetic defects associated with the vial capping process. Copyright © 2015 Elsevier B.V. All rights reserved.

  16. Problems connected with the use of oligonucleotide probes with a high degree of degeneracy. Identification of mRNA and of cDNA clones corresponding to the gene of the. cap alpha. -subunit of Na/sup +/, K/sup +/-ATPase

    Energy Technology Data Exchange (ETDEWEB)

    Petrukhin, K.E.; Grishin, A.V.; Arsenyan, S.G.; Broude, N.E.; Grinkevich, V.A.; Filippova, L.Yu.; Severtsova, I.V.; Modyanov, N.N.

    1986-10-01

    To identify and search for nucleotide sequences containing the structural part of the gene of the ..cap alpha..-subunit of Na/sup +/, K/sup +/-ATPase, 17-membered oligonucleotide probes corresponding to the peptide Lys-Asp-Ala-Phe-Gln-Asn have been synthesized. It has been shown that, with a 64-fold degeneracyd, the 17-membered probe is suitable only for the identification of a specific sequence in mRNA. To search for clones containing cDNA fragments, preliminary fractionation of the probes with the aid of HPLC or the resynthesis of groups of oligonucleotides with a lower degeneracy is necessary.

  17. pH-metric studies on the mixed ligand-chelates of oxovanadium(IV) with 2,2'-bipyridyl and dicarboxylic or hydroxy acids

    International Nuclear Information System (INIS)

    Jain, A.K.; Kumari, V.; Chaturvedi, G.K.

    1978-01-01

    The interaction of vanadyl ion with 2,2'-bipyridyl and some dicarboxylic or hydroxy acids (where dicarboxylic acid = oxalic (OX), malonic (MALN), phthalic (PHA), maleic (MAL) acids; hydroxy acids salicylic (SA), 5-sulfosalicylic (5-SSA), mandelic (MAND) and glycollic (HG) acids was studied potentiometrically. pH-titrations of the reaction mixtures containing vanadyl sulphate, 2,2'-bipyridyl and one of the dicarboxylic or hydroxy acids (OX, MALN, PHA, MAL, SA, 5-SSA, MAND and HG acids) in equimolar ratio exhibited the formation of 1:1:1 mixed ligand chelates. The formation constants of the resulting biligand chelates were calculated, at 35 + -1 0 and 45 + -1 0 and also the thermodynamic functions viz. ΔF, ΔH and ΔS (μ=0.1M KNO 3 ) (auth.)

  18. The development of a radioimmunoassay for 18-hydroxy-corticosterone

    International Nuclear Information System (INIS)

    Martin, V.I.

    1980-03-01

    It has been suggested that 18-hydroxy-corticosterone (18-OH-B) is a precursor for aldosterone in the biosynthetic pathway. This steroid had not been measured in peripheral plasma and therefore to evaluate its clinical role a sensitive and specific radioimmunoassay was developed. The assay is described and was applied to measure the levels of 18-hydroxy-corticosterone in normal human subjects on (a) an ad libitum sodium intake whilst lying or standing, (b) on a high or low sodium intake whilst recumbent, (c) before and after treatment with either ACTH, metyrapone or dexamethasone on a high or low sodium intake whilst recumbent (d) after insulin induced hypoglycaemia and (e) after infusions of 18-hydroxy-corticosterone. The levels of 18-hydroxy-corticosterone were also measured in patients with (a) 17α-hydroxylase deficiency, (b) primary or secondary aldosteronism, (c) Bartter's syndrome, (d) Cushing's syndrome, (e) adrenalectomised patients or patient's with Addison's disease and (f) patients with essential hypertension. (author)

  19. Alterations in mGluR5 expression and signaling in Lewy body disease and in transgenic models of alpha-synucleinopathy--implications for excitotoxicity.

    Directory of Open Access Journals (Sweden)

    Diana L Price

    2010-11-01

    Full Text Available Dementia with Lewy bodies (DLB and Parkinson's Disease (PD are neurodegenerative disorders of the aging population characterized by the abnormal accumulation of alpha-synuclein (alpha-syn. Previous studies have suggested that excitotoxicity may contribute to neurodegeneration in these disorders, however the underlying mechanisms and their relationship to alpha-syn remain unclear. For this study we proposed that accumulation of alpha-syn might result in alterations in metabotropic glutamate receptors (mGluR, particularly mGluR5 which has been linked to deficits in murine models of PD. In this context, levels of mGluR5 were analyzed in the brains of PD and DLB human cases and alpha-syn transgenic (tg mice and compared to age-matched, unimpaired controls, we report a 40% increase in the levels of mGluR5 and beta-arrestin immunoreactivity in the frontal cortex, hippocampus and putamen in DLB cases and in the putamen in PD cases. In the hippocampus, mGluR5 was more abundant in the CA3 region and co-localized with alpha-syn aggregates. Similarly, in the hippocampus and basal ganglia of alpha-syn tg mice, levels of mGluR5 were increased and mGluR5 and alpha-syn were co-localized and co-immunoprecipitated, suggesting that alpha-syn interferes with mGluR5 trafficking. The increased levels of mGluR5 were accompanied by a concomitant increase in the activation of downstream signaling components including ERK, Elk-1 and CREB. Consistent with the increased accumulation of alpha-syn and alterations in mGluR5 in cognitive- and motor-associated brain regions, these mice displayed impaired performance in the water maze and pole test, these behavioral alterations were reversed with the mGluR5 antagonist, MPEP. Taken together the results from study suggest that mGluR5 may directly interact with alpha-syn resulting in its over activation and that this over activation may contribute to excitotoxic cell death in select neuronal regions. These results highlight the

  20. Push-pull effect on the geometrical, optical and charge transfer properties of disubstituted derivatives of mer-tris(4-hydroxy-1,5-naphthyridinato aluminum (mer-AlND3

    Directory of Open Access Journals (Sweden)

    Rao Joshi Laxmikanth

    2016-01-01

    Full Text Available To design innovative and novel optical materials with high mobility, two kinds of disubstituted derivatives for mer-tris(4-hydroxy-1,5-naphthyridinato aluminum (mer-AlND3 with push (EDG–pull (EWG substituents have been designed. The structures of mer-tris(8-EDG-2-EWG-4-hydroxy-1,5-naphthyridinato aluminum (type I and mer-tris(8-EWG-2-EDG-4-hydroxy-1,5-naphthyridinato aluminum (type II in the ground and first excited states have been optimized at the B3LYP/6-31G(D and CIS/6-31G(D level of theory, respectively. It can be seen from frontier molecular orbitals analysis, in all these complexes, the highest occupied molecular orbital (HOMO is localized on the pyridine-4-ol ring of A-ligand while lowest unoccupied molecular orbital (LUMO is on the pyridyl ring of B-ligand in ground state irrespective of electron donor/acceptor substitution present on the ligands similar to that of mer-tris(8-hydroxyquinoline aluminum (mer-Alq3 and parent mer-AlND3.The absorption and emission wavelengths have been evaluated at the TD-PBE0/6-31G(D level and it can be see that all the type I derivatives show blue shift while most of the type II derivatives show red shift compared to mer-AlND3. All the disubstituted complexes have showed hypsochromic shifts in both the absorption and emission spectra when compared with the calculated absorption and emission spectra respectively of mer-Alq3. It can be seen that the reorganization energies of some of the disubstituted derivatives are comparable with mer-Alq3 and these derivatives might be good candidates for emitting materials in OLED.

  1. Surface protection of mild steel in acidic chloride solution by 5-Nitro-8-Hydroxy Quinoline

    Directory of Open Access Journals (Sweden)

    R. Ganapathi Sundaram

    2018-03-01

    Full Text Available The effect of commercially available quinoline nucleus based pharmaceutically active compound 5-Nitro-8-Hydroxy Quinoline (NHQ against the corrosion of mild steel (MS in 1 M acidic chloride (HCl solution was investigated by chemical (weight loss – WL and electrochemical (Tafel polarization, Linear polarization and Electrochemical impedance spectroscopy techniques. From all the four methods, it is inferred that the percentage of inhibition efficiency increases with increasing the inhibitor concentration from 50 to 300 ppm. The adsorption behavior of inhibitor obeyed through Langmuir isotherm model. Thermodynamic parameters were also calculated and predict that the process of inhibition is a spontaneous reaction. EIS technique exhibits one capacitive loop indicating that, the corrosion reaction is controlled by charge transfer process. Tafel polarization studies revealed that the investigated inhibitor is mixed type and the mode of adsorption is physical in nature. The surface morphologies were examined by FT-IR, SEM and EDX techniques. Theoretical quantum chemical calculations were performed to confirm the ability of NHQ to adsorb onto mild steel surface. Keywords: Acidic chloride solution, MS, NHQ, WL, SEM, FT-IR

  2. Characterization and evaluation of an oral microemulsion containing the antitumor diterpenoid compound ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid.

    Science.gov (United States)

    Lu, Yingnian; Wu, Kefeng; Li, Li; He, Yuhui; Cui, Liao; Liang, Nianci; Mu, Bozhong

    2013-01-01

    The objective of this study was to develop an oral microemulsion formulation of the antitumor diterpenoid agent, ent-11α-hydroxy-15-oxo-kaur-16-en-19-oic-acid (henceforth referred to as 5F), to enhance its bioavailability and evaluate its hepatotoxicity. Pseudoternary phase diagrams showed that the optimal microemulsion formulation contained 45% water, 10% castor oil as the oil phase, 15% Cremophor EL as the surfactant, and 30% as a cosurfactant mixture of 1,2-propanediol and polyethylene glycol (PEG)-400 (2:1, w/w). The microemulsion preparation was characterized and its droplet diameter was within 50 nm. Release of 5F in vitro from the microemulsion was slightly increased compared with a suspension containing the same amount of active drug. Pharmacokinetic parameters in vivo indicated that bioavailability was markedly improved, with the relative bioavailability being 616.15% higher for the microemulsion than for the suspension. Toxicity tests showed that the microemulsion had no hepatotoxicity in mice. These results suggest the potential for 5F microemulsion to be administered by the oral route.

  3. Catastrophic antiphospholipid syndrome (CAPS): Descriptive analysis of 500 patients from the International CAPS Registry.

    Science.gov (United States)

    Rodríguez-Pintó, Ignasi; Moitinho, Marta; Santacreu, Irene; Shoenfeld, Yehuda; Erkan, Doruk; Espinosa, Gerard; Cervera, Ricard

    2016-12-01

    To analyze the clinical and immunologic manifestations of patients with catastrophic antiphospholipid syndrome (CAPS) from the "CAPS Registry". The demographic, clinical and serological features of 500 patients included in the website-based "CAPS Registry" were analyzed. Frequency distribution and measures of central tendency were used to describe the cohort. Comparison between groups regarding qualitative variables was undertaken by chi-square or Fisher exact test while T-test for independent variables was used to compare groups regarding continuous variables. 500 patients (female: 343 [69%]; mean age 38±17) accounting for 522 episodes of CAPS were included in the analysis. Forty percent of patients had an associated autoimmune disease, mainly systemic lupus erythematosus (SLE) (75%). The majority of CAPS episodes were triggered by a precipitating factor (65%), mostly infections (49%). Clinically, CAPS was characterized by several organ involvement affecting kidneys (73%), lungs (60%), brain (56%), heart (50%), and skin (47%). Lupus anticoagulant, IgG anticardiolipin and IgG anti-β2-glycprotein antibodies were the most often implicated antiphospholipid antibodies (83%, 81% and 78% respectively). Mortality accounted for 37% of episodes of CAPS. Several clinical differences could be observed based on the age of presentation and its association to SLE. Those cases triggered by a malignancy tended to occur in older patients, while CAPS episodes in young patients were associated with an infectious trigger and peripheral vessels involvement. Additionally, CAPS associated with SLE were more likely to have severe cardiac and brain involvement leading to a higher mortality (48%). Although the presentation of CAPS is characterized by multiorgan thrombosis and failure, clinical differences among patients exist based on age and underlying chronic diseases, e.g. malignancy and SLE. Copyright © 2016 Elsevier B.V. All rights reserved.

  4. The 5cap of Tobacco Mosaic Virus (TMV) is required for virion attachment to the actin/ER network during early infection

    DEFF Research Database (Denmark)

    Christensen, Nynne Meyn; Tilsner, Jens; Bell, Karen

    to the motile cortical actin/ER network within minutes of injection. Granule movement on actin/ER was arrested by actin inhibitors indicating actindependent RNA movement. The 5’ methylguanosine TMV cap was shown to be required for vRNA anchoring to the ER. TMV vRNA lacking the 5cap failed to form granules...... the fluorescent vRNA pool nor co-injected GFP left the injected trichome, indicating that the synthesis of unlabelled progeny viral (v)RNA is required to initiate cell-cell movement, and that virus movement is not accompanied by passive plasmodesmatal gating. Cy3-vRNA formed granules that became anchored...... on the same ER-bound granules, indicating that TMV virions may become attached to the ER prior to uncoating of the viral genome....

  5. ST5 Observations of the Imbalance of Region 1 and 2 Field-Aligned Currents and Its Implication to the Cross-Polar Cap Pedersen Currents

    Science.gov (United States)

    Le, Guan; Slavin, J. A.; Strangeway, Robert

    2011-01-01

    In this study, we use the in-situ magnetic field observations from Space Technology 5 mission to quantify the imbalance of Region 1 (R1) and Region 2 (R2) currents. During the three-month duration of the ST5 mission, geomagnetic conditions range from quiet to moderately active. We find that the R1 current intensity is consistently stronger than the R2 current intensity both for the dawnside and the duskside large-scale field-aligned current system. The net currents flowing into (out of) the ionosphere in the dawnside (duskside) are in the order of 5% of the total R1 currents. We also find that the net currents flowing into or out of the ionosphere are controlled by the solar wind-magnetosphere interaction in the same way as the field-aligned currents themselves are. Since the net currents due to the imbalance of the R1 and R2 currents require that their closure currents flow across the polar cap from dawn to dusk as Pedersen currents, our results indicate that the total amount of the cross-polar cap Pedersen currents is in the order of 0.1 MA. This study, although with a very limited dataset, is one of the first attempts to quantify the cross-polar cap Pedersen currents. Given the importance of the Joule heating due to Pedersen currents to the high-latitude ionospheric electrodynamics, quantifying the cross-polar cap Pedersen currents and associated Joule heating is needed for developing models of the magnetosphere-ionosphere coupling.

  6. Evaluation of Zinc-alpha-2-Glycoprotein and Proteasome Subunit beta-Type 6 Expression in Prostate Cancer Using Tissue Microarray Technology.

    LENUS (Irish Health Repository)

    2010-07-23

    Prostate cancer (CaP) is a significant cause of illness and death in males. Current detection strategies do not reliably detect the disease at an early stage and cannot distinguish aggressive versus nonaggressive CaP leading to potential overtreatment of the disease and associated morbidity. Zinc-alpha-2-glycoprotein (ZAG) and proteasome subunit beta-Type 6 (PSMB-6) were found to be up-regulated in the serum of CaP patients with higher grade tumors after 2-dimensional difference gel electrophoresis analysis. The aim of this study was to investigate if ZAG and PSMB-6 were also overexpressed in prostatic tumor tissue of CaP patients. Immunohistochemical analysis was performed on CaP tissue microarrays with samples from 199 patients. Confirmatory gene expression profiling for ZAG and PSMB-6 were performed on 4 cases using Laser Capture Microdissection and TaqMan real-time polymerase chain reaction. ZAG expression in CaP epithelial cells was inversely associated with Gleason grade (benign prostatic hyperplasia>G3>G4\\/G5). PSMB-6 was not expressed in either tumor or benign epithelium. However, strong PSMB-6 expression was noted in stromal and inflammatory cells. Our results indicate ZAG as a possible predictive marker of Gleason grade. The inverse association between grade and tissue expression with a rising serum protein level is similar to that seen with prostate-specific antigen. In addition, the results for both ZAG and PSMB-6 highlight the challenges in trying to associate the protein levels in serum with tissue expression.

  7. Effect of active acidity on the stability of amylolytic enzymes in fermentation of corn mash

    Energy Technology Data Exchange (ETDEWEB)

    Zherebtsov, N A; Mal' tsev, P M

    1957-01-01

    The effect of pH between 6.5 and 3.5 on the activity of ..cap alpha..- and ..beta..-amylases, dextrinase, and on the yield of alcohol in the fermentation of corn mash were investigated. The minimum of unfermented maltose and maximum activity of amylolytic enzymes were found from fermentations between pH 5.5 and 4.9. Under these conditions ..beta..-amylase and dextrinase were unaffected, while ..cap alpha..-amylase activity was reduced to 59.1% initial activity. Considerable inactivation of ..beta..-amylase and dextrinase set in at pH 4.0 and ..cap alpha..-amylase at pH 4.5. The highest yield of alcohol was produced from mash with initial pH 6.0 obtained by addition of sodium hydroxide.

  8. 4-Hydroxy-1-naphthaldehydes: proton transfer or deprotonation

    DEFF Research Database (Denmark)

    Manolova, Y; Kurteva, V; Antonov, L

    2015-01-01

    A series of naphthaldehydes, including a Mannich base, have been investigated by UV-Vis spectroscopy, NMR and theoretical methods to explore their potential tautomerism. In the case of 4-hydroxy-1-naphthaldehyde concentration dependent deprotonation has been detected in methanol and acetonitrile....... For 4-hydroxy-3-(piperidin-1-ylmethyl)-1-naphthaldehyde (a Mannich base) an intramolecular proton transfer involving the OH group and the piperidine nitrogen occurs. In acetonitrile the equilibrium is predominantly at the OH-form, whereas in methanol the proton transferred tautomer is the preferred form....... In chloroform and toluene, the OH form is completely dominant. Both 4-hydroxy-1-naphthaldehyde and 4-methoxy-1-naphthaldehyde (fixed enol form) show dimerization in the investigated solvents and the crystallographic data, obtained for the latter, confirm the existence of a cyclic dimer...

  9. No-carrier-added (NCA) synthesis of 6-[{sup 18}F]fluoro-L-DOPA using 3,5,6,7,8,8a-hexahydro-7,7,8a-trimethyl-[6S-(6{alpha}, 8{alpha}, 8{alpha}{beta})]-6,8-methano-2H-1,4-benzoxazin-2-one

    Energy Technology Data Exchange (ETDEWEB)

    Horti, A. [Yale Univ., New Haven, CT (United States). School of Medicine]|[Yale Univ., West Haven, CT (United States). PET Center; Redmond, D.E. Jr. [Yale Univ., New Haven, CT (United States). School of Medicine; Soufer, R. [Yale Univ., West Haven, CT (United States). PET Center

    1995-12-31

    3,5,6,7,8,8a-Hexahydro-7,7,8a-trimethyl-[6S-(6{alpha},8{alpha} , 8{alpha}{beta})]-6,8-methano-2H-1,4-benzoxazino-2-one (2) was investigated as chiral auxiliary for asymmetric NCA nucleophilic synthesis of 6-[{sup 18}F]Fluoro-L-DOPA. Direct condensation of 3,4-dimethoxy-2-[{sup 18}F]fluorobenzaldehyde (1a) or 6-[{sup 18}F]fluoro-piperonal (1b) in the presence of NaH with 2 gave the corresponding [{sup 18}F]-3-[(2-fluorophenyl)methylene]-3,5,6,7,8,8a-hexahydro-7,7,8 a-trimethyl-[6S-(3Z,3{alpha},6{alpha},8{alpha},8{alpha}{beta})]-6, 8-methano-2H-1,4-benzoxazin-2-one derivative 3a or 3b as a single stereoisomer. L-Selectride promoted hydrogenation of the olefinic double bond of these derivatives, in presence of tertbutyl alcohol, afforded the corresponding [{sup 18}F]-3-[(2-fluorophenyl) methyl]-3,5,6,7,8,8a-hexahydro-7,7,8a-trimethyl-[3S-(3{alpha}, 6{alpha}, 8{alpha}8{alpha}{beta})]-6,8-methano-2H-1,4-benzoxazin-2-one derivatives (4a,b) without affecting the orientation of diasterofacial discrimination. Deprotection of the derivatives 4a,b yielded 6-[{sup 18}F]fluoro-L-DOPA (e.e. >90%, 3% radiochemical yield (EOB), total synthesis time 125 min, specific activity >2000 mCi/{mu}mol). Direct deprotection/reduction of the compounds 3a,b provides the enantiomeric mixture of 6-[{sup 18}F]fluoro-D,L-DOPA (10-12% radiochemical yield) and, after chiral separation, 6-[{sup 18}F]fluoro-L-DOPA (e.e. 98%, 4-5% radiochemical yield). (author).

  10. Synthesis and Antifungal Activities of 5-(o-Hydroxy phenyl-2-[4'aryl-3'chloro-2'azetidinon-1-yl]-1,3,4-thiadiazole

    Directory of Open Access Journals (Sweden)

    Shiv K. Gupta

    2011-01-01

    Full Text Available New series of 5-(o-hydroxy phenyl-2-[4'aryl-3'chloro-2'azetidinon-1-yl]-1,3,4-thiadiazole have been synthesized and the structures of the new compounds were established on the basis of IR, 1H NMR spectral data. In vitro antifungal activity (MIC activity was evaluated and compared with standard drugs of ketoconazole. Compounds 3c in the series has shown interesting antifungal activity against both C. albicans and A. niger fungus. In the gratifying result, most of the compounds were found to have moderate antifungal activity.

  11. Standard and alternative landfill capping design in Germany

    International Nuclear Information System (INIS)

    Simon, Franz-Georg; Mueller, Werner W.

    2004-01-01

    Engineered capping systems are in most cases an indispensable and often the only efficient component required by the long-term safety concept for landfills, mine tailings tips and contaminated land. In Germany the composite liner is the main component of standard landfill cappings for municipal and hazardous waste landfills and the compacted clay liner (CCL) for landfills for inert or low-contamination waste. The composite liner is a technically highly effective but very expensive system. Research and experience has given rise to concern about the proper long-term performance of a conventional single CCL as a landfill capping. Therefore, alternative capping systems are discussed and applied for landfills and for the containment of contaminated sites. This paper gives an overview on various alternative engineered cappings and suitable systems for capping reflecting the state of the art and the expert view in Germany. According to the European Council Directive on the landfill of waste an impermeable mineral layer is recommended for the surface sealing of non-hazardous landfills and a composition of artificial sealing liner and impermeable mineral layer for hazardous landfills. In both cases a drainage layer thickness of at least 0.5 m is suggested. These recommendations should be interpreted flexibly and to some extent modified in the light of the experience and results presented in this paper

  12. Integrins beta 5, beta 3 and alpha v are apically distributed in endometrial epithelium.

    Science.gov (United States)

    Aplin, J D; Spanswick, C; Behzad, F; Kimber, S J; Vićovac, L

    1996-07-01

    Several adhesion molecules have been shown to occur at the surface of endometrial cells. One of these is the integrin alpha v subunit which associates with various beta chains including beta 5. We demonstrate the presence of integrin beta 5 polypeptide in human endometrial epithelial cells throughout the menstrual cycle using immunocytochemistry with monospecific antibodies, and at the mRNA level by thermal amplification from endometrial cDNA. Integrin beta 5 is also found in a population of bone marrow-derived cells. A notable feature of the distribution of the beta 5 subunit in the glandular and luminal epithelium is its apical localization, which may suggest an involvement in implantation. However, no evidence was found for regulated expression of epithelial beta 5. In mouse, the beta 5 subunit is found at both the apical and basal surface of epithelial cells and expression is essentially oestrous cycle-independent. Comparisons are made in both species with the distribution of the alpha v and beta 3 subunits which also localize to the apical epithelium.

  13. The rebirth of the cervical cap.

    Science.gov (United States)

    Cappiello, J D; Grainger-Harrison, M

    1981-01-01

    In an effort to dispel myths surrounding the cervical cap, the historical and political factors affecting the cap's use in the U.S. are described. Clinical aspects of cap fitting are also included. The cervical cap has found only limited acceptance in the U.S. Skepticisms on the part of physicians may be the result of 2 factors: confusion of the cervical cap with intracervical devices used for artificial insemination and confusion with stem pessaries; and the lack of clinical research and statistical evaluation of efficacy rates. The latter factor prompted Tietze et al. to conduct the only U.S. statistical study of the cap in 1953. Of the 143 women studied, the pregnancy rate was 7.6/100 years of use. Of the 28 unplanned pregnancies, 6 were related to faulty technique or omission of a spermicide and 10 were instances of admittedly irregular use. When these failures are omitted, the theoretical effectiveness rate is about 98%. Some practitioners are concerned about an increased incidence of cervical erosion with cap use. Possibly currently conducted studies will show that cap and spermicide users have a lower incidence of cervical erosion than women using no contraceptive method. Study findings suggest that the cervical cap may afford protection without any spermicidal supplement, but the use of spermicides continues to be recommended to clients. Advantages of the cervical cap include the following: it can be left in place longer than a diaphragm without additional applications of spermicide in the vagina; and the insertion of the cap is unrelated to the time of intercourse. Despite research on toleration of the cap for 3 weeks at a time, it is recommended that the cap be worn for only a few days at a time. At this time there are no manufacturers of cervical caps for contraceptive use in the U.S. The cap is now being imported from England and it costs $6.00. A factor that has made the cap unpopular with many physicians is the lengthy time required for fitting. An

  14. Diels-Alder Reactions of 12-Hydroxy-9(10®20-5aH-abeo-abieta-1(10,8(9,12(13-triene-11,14-dione

    Directory of Open Access Journals (Sweden)

    Shougang Hu

    2013-06-01

    Full Text Available 12-Hydroxy-9(10®20-5aH-abeo-abieta-1(10,8(9,12(13-triene-11,14-dione (quinone 2 served as the dienophile in numerous intermolecular Diels-Alder reactions. These cycloadditions were conducted either thermally (including microwave heating or with Lewis acid activation. While most dienes reacted with quinone 2 in good chemical yield, others were incompatible under the experimental conditions used.

  15. (2aR*,5S*,6aS*,8aS*,E-Ethyl 5-hydroxy-7,7,8a-trimethyl-8-oxo-2,2a,6,6a,7,8,8a,8b-octahydro-1H-pentaleno[1,6-bc]oxepine-4-carboxylate

    Directory of Open Access Journals (Sweden)

    Goverdhan Mehta

    2012-12-01

    Full Text Available The title compound, C17H24O5, featuring a 2-carbethoxy-3-oxepanone unit in its intramolecularly O—H...O hydrogen-bonded enol form, was obtained via [(CF3CO22Rh]2-catalysed intramolecular O—H bond insertion in the α-diazo-ω-hydroxy-β-ketoester, ethyl 4-[(1S,3aS,6R,6aS-6-hydroxy-2,2,3a-trimethyl-3-oxo-octahydropentalen-1-yl]-2-diazo-3-oxobutanoate. The seven-membered oxacyclic ring, thus constructed on a cis-fused diquinane platform, was found to adopt a distorted boat–sofa conformation.

  16. Ferroelectric capped magnetization in multiferroic PZT/LSMO tunnel junctions

    Energy Technology Data Exchange (ETDEWEB)

    Kumar, Ashok, E-mail: ashok553@nplindia.org; Shukla, A. K. [National Physical Laboratory (CSIR), Dr. K. S. Krishnan Road, New Delhi-110012 (India); Barrionuevo, D.; Ortega, N.; Katiyar, Ram S. [Department of Physics and Institute of Functional Nanomaterials, University of Puerto Rico, San Juan, Puerto Rico 00931-3343 (United States); Shannigrahi, Santiranjan [Institute of Materials Research and Engineering - IMRE, Agency for Science Technology and Research (A-STAR), 3 Research Link, Singapore 117602 (Singapore); Scott, J. F. [Department of Chemistry and Department of Physics, University of St. Andrews, St. Andrews KY16 ST (United Kingdom)

    2015-03-30

    Self-poled ultra-thin ferroelectric PbZr{sub 0.52}Ti{sub 0.48}O{sub 3} (PZT) (5 and 7 nm) films have been grown by pulsed laser deposition technique on ferromagnetic La{sub 0.67}Sr{sub 0.33}MnO{sub 3} (LSMO) (30 nm) to check the effect of polar capping on magnetization for ferroelectric tunnel junction devices. PZT/LSMO heterostructures with thick polar PZT (7 nm) capping show nearly 100% enhancement in magnetization compared with thin polar PZT (5 nm) films, probably due to excess hole transfer from the ferroelectric to the ferromagnetic layers. Core-level x-ray photoelectron spectroscopy studies revealed the presence of larger Mn 3s exchange splitting and higher Mn{sup 3+}/Mn{sup 4+} ion ratio in the LSMO with 7 nm polar capping.

  17. Unique regional distribution of delta 4-3-ketosteroid-5 alpha-oxidoreductase and associated epididymal morphology in the marsupial, Didelphis virginiana.

    Science.gov (United States)

    Kelce, W R; Krause, W J; Ganjam, V K

    1987-09-01

    The epididymal epithelial ultrastructure has been described in the adult male North American opossum, Didelphis virginiana. Morphological results have suggested that absorptive activity is prominent in the proximal epididymal region by virtue of numerous microvilli, an endocytotic complex, dense granules, and multivesicular bodies in the apical cytoplasm. In contrast, the middle and distal epididymal regions exhibit ultrastructural features indicative of protein synthesis such as large invaginated euchromatic nuclei, large nucleoli, and increased amounts of granular endoplasmic reticulum. It is in the middle and distal epididymal regions where sperm head rotation and sperm pairing take place. Epididymal delta 4-3-ketosteroid-5 alpha-oxidoreductase (5 alpha-reductase) activity also has been measured. It has been found that the level of enzyme activity differs significantly (p less than 0.01) between the proximal, middle, and distal epididymal regions. Enzyme-specific activity has been found to be highest in the middle region (47.6 +/- 5.4 picomoles 5 alpha-reduced androgens formed/b/mg protein), lower in the distal region (18.3 +/- 0.7 picomoles 5 alpha-reduced androgens formed/b/mg protein), with little activity (2.4 +/- 1.2 picomoles 5 alpha-reduced androgens formed/h/mg protein) found in the proximal epididymal region. This regional distribution of enzyme activity differs markedly from that reported for eutherian mammals. Both the suggested epididymal protein synthetic and secretory activity and the level of epididymal 5 alpha-reductase activity appear to correlate regionally with the morphological changes that occur in the opossum spermatozoa as they transit the epididymis.

  18. pH-metric studies on the mixed ligand-chelates of oxovanadium(IV) with 2,2'-bipyridyl and dicarboxylic or hydroxy acids

    Energy Technology Data Exchange (ETDEWEB)

    Jain, A K; Kumari, V; Chaturvedi, G K [Agra Coll. (India)

    1978-12-01

    The interaction of vanadyl ion with 2,2'-bipyridyl and some dicarboxylic or hydroxy acids (where dicarboxylic acid = oxalic (OX), malonic (MALN), phthalic (PHA), maleic (MAL) acids; hydroxy acids salicylic (SA), 5-sulfosalicylic (5-SSA), mandelic (MAND) and glycollic (HG) acids was studied potentiometrically. pH-titrations of the reaction mixtures containing vanadyl sulphate, 2,2'-bipyridyl and one of the dicarboxylic or hydroxy acids (OX, MALN, PHA, MAL, SA, 5-SSA, MAND and HG acids) in equimolar ratio exhibited the formation of 1:1:1 mixed ligand chelates. The formation constants of the resulting biligand chelates were calculated, at 35/sup +/-1/sup 0/ and 45/sup +/-1/sup 0/ and also the thermodynamic functions viz. ..delta..F, ..delta..H and ..delta..S (..mu..=0.1M KNO/sub 3/) (auth.).

  19. From beta-relaxation to alpha-decay: Atomistic picture from molecular dynamics simulations for glass-forming Ni0.5Zr0.5 melt

    Energy Technology Data Exchange (ETDEWEB)

    Teichler, Helmar [Inst. Materialphysik, Univ Goettingen (Germany)

    2013-07-01

    In glass-forming melts the decay of structural fluctuation shows the well known transition from beta-relaxation (von-Schweidler law with exponent b) to alpha-decay (KWW law with exponent beta). Here we present results from molecular dynamics simulations for a metallic glass forming Ni0.5Zr0.5 model aimed at giving an understanding of this transition on the atomistic scale. At the considered temperature below mode coupling Tc, the dynamics of the system can be interpreted by residence of the particles in their neighbour cages and escape from the cages as rare processes. Our analysis yields that the fraction of residing particles is characterized by a hierarchical law in time, with von-Schweidler b explicitly related to the exponent of this law. In the alpha-decay regime the stretching exponent reflects, in addition, floating of the cages due to strain effects of escaped particles. Accordingly, the change from beta-relaxation to alpha-decay indicates the transition from low to large fraction of escaped particles.

  20. Extraction of uranium(VI) by emulsion liquid membrane containing 5,8-diethyl-7-hydroxy-6-dodecanone oxime

    International Nuclear Information System (INIS)

    Akiba, Kenichi; Takahashi, Toshihiko; Kanno, Takuji

    1984-01-01

    Extraction of uranium(VI) by a liquid surfactant membrane has been studied. The stability of water-in-oil (w/o) emulsion dispersed in the continuous aqueous phase increased with an increase in surfactant concentrations and in the fraction of the organic phase in emulsion globules. Uranium(VI) in dilute acid solutions was extracted into (w/o) emulsions containing 5,8-diethyl-7-hydroxy-6-dodecanone oxime (LIX 63) as a mobile carrier and its concentration decreased according to [U]sub(t)=[U]sub(o)exp(-ksub(obsd)t). The apparent rate constants (ksub(obsd)) increased with an increase in carrier concentrations and in external pH values, while they were slightly dependent on the stripping acid concentrations. Uranium was transported and concentrated into the internal aqueous droplets. The final concentration of uranium in the external aqueous phase dropped to about 10 -3 of its initial value. (author)

  1. Redox Control and Hydrogen Production in Sediment Caps Using Carbon Cloth Electrodes

    Science.gov (United States)

    Sun, Mei; Yan, Fei; Zhang, Ruiling; Reible, Danny D.; Lowry, Gregory V.; Gregory, Kelvin B.

    2010-01-01

    Sediment caps that degrade contaminants can improve their ability to contain contaminants relative to sand and sorbent-amended caps, but few methods to enhance contaminant degradation in sediment caps are available. The objective of this study was to determine if, carbon electrodes emplaced within a sediment cap at poised potential could create a redox gradient and provide electron donor for the potential degradation of contaminants. In a simulated sediment cap overlying sediment from the Anacostia River (Washington, DC), electrochemically induced redox gradients were developed within 3 days and maintained over the period of the test (~100 days). Hydrogen and oxygen were produced by water electrolysis at the electrode surfaces and may serve as electron donor and acceptor for contaminant degradation. Electrochemical and geochemical factors that may influence hydrogen production were studied. Hydrogen production displayed zero order kinetics with ~75% coulombic efficiency and rates were proportional to the applied potential between 2.5V to 5V and not greatly affected by pH. Hydrogen production was promoted by increasing ionic strength and in the presence of natural organic matter. Graphite electrode-stimulated degradation of tetrachlorobenzene in a batch reactor was dependent on applied voltage and production of hydrogen to a concentration above the threshold for biological dechlorination. These findings suggest that electrochemical reactive capping can potentially be used to create “reactive” sediments caps capable of promoting chemical or biological transformations of contaminants within the cap. PMID:20879761

  2. Structure and electrical conduction of the system La sub(1-x)Ca sub(x)FeO sub(3-. cap alpha. )

    Energy Technology Data Exchange (ETDEWEB)

    Hombo, Jukichi; Urabe, Noriake [Kumamoto Univ. (Japan). Faculty of Engineering; Hiroshige, Gota; Hamada, Kotaro

    1982-08-01

    Perovskite phases in the system, La sub(1-x)Ca sub(x)FeO sub(3-..cap alpha..) were prepared with La/sub 2/O/sub 3/, CaCO/sub 3/, and Fe/sub 2/O/sub 3/ by firing in air and in vacuo. The compositions of samples fired in vacuo and in air are represented as La sub(1-x)Ca sub(x)FeO sub(3-x 2) and La sub(1-x)Ca sub(x)Fe sub(1-y)sup(3+)Fe sub(y)sup(4+)O sub(3-x/2+y/2), respectively. That is, samples fired in vacuo contain some oxygen vacancies and no tetravalent iron; in contrast, samples fired in air contain both oxygen vacancies and tetravalent iron in the structures. The electrical conductivities of these synthesized oxides depended extensively upon the content of tetravalent iron. For instance, the conductivity of the sample x = 0.6 fired in air was larger by 10/sup 6/ than that of the sample fired in vacuo. In this system, except for the two terminal compositions of x = 0 and x = 1.0, the values of activation energy for conduction are considerably small, and from the results of thermo-electromotive force measurement, the charge carrier was positive. Furthermore, the conductivity increased somewhat with time during the conductivity measurement by the direct-current method. These facts suggest that the electric conduction would not be ionic but electronic. The electrical conduction would then be carried out by the so-called hopping mechanism by which the positive charge is transferred.

  3. Microtubule's conformational cap

    DEFF Research Database (Denmark)

    Flyvbjerg, H.

    1999-01-01

    The molecular mechanisms that allow elongation of the unstable microtubule lattice remain unclear. It is usually thought that the GDP-liganded tubulin lattice is capped by a small layer of GTP- or GDP-P(i)-liganded molecules, the so called "GTP-cap". Here, we point-out that the elastic properties...

  4. Are the brightest Lyman Alpha Emitters at z=5.7 primeval galaxies?

    Science.gov (United States)

    Lidman, Christopher; Jones, Heath; Meisenheimer, Klaus; Pompei, Emanuela; Tapken, Christian; Vanzi, Leonardo; Westra, Eduard

    2008-03-01

    Wide-field, narrow-band surveys have proven to be effective at finding very high redshift galaxies that emit brightly in the Lyman alpha line, the so-called Lyman alpha emitters (LAEs). It was through this technique that the most distant spectroscopically confirmed galaxy, a galaxy at z=6.96, was discovered. Considerable effort is currently being spent on discovering these galaxies at ever higher redshifts by extending this technique into the near-IR. In contrast to this effort, there has been relatively little work on understanding these galaxies. In particular, how do LAEs relate to other high redshift galaxies, such as the galaxies discovered through broad band drop out techniques, and, perhaps, more importantly, what role do LAEs play in re-ionising the universe. We recently discovered two extremely luminous LAEs at z=5.7. These LAEs are among the brightest LAEs ever discovered at this redshift. In a recent paper by Mao et al. the brightest LAEs are associated to the most massive halos. We propose to use the IRAC 3.6 micron imager on Spitzer to measure the rest-frame optical flux of the these LAEs. With additional data from the near-IR (rest-frame UV) and very deep optical spectra around the Lyman alpha line, we propose to make a detailed study of the spectral energy distribution from the Lyman alpha line to the rest frame optical of these exceptional LAEs. These data will enable us to estimate the age and mass of the stellar burst that produces the Lyman alpha line, to estimate the contribution from an older stellar population, if any, and to estimate the fraction of Lyman continuum photons that can escape the galaxy and are thus available to reionise the universe.

  5. 75 FR 49527 - Caps Visual Communications, LLC; Black Dot Group; Formerly Known as Caps Group Acquisition, LLC...

    Science.gov (United States)

    2010-08-13

    ... DEPARTMENT OF LABOR Employment and Training Administration [TA-W-74,195] Caps Visual Communications, LLC; Black Dot Group; Formerly Known as Caps Group Acquisition, LLC Chicago, IL; Amended... of Caps Visual Communications, LLC, Black Dot Group, formerly known as Caps Group Acquisition, LLC...

  6. 40 CFR 721.10063 - Halo substituted hydroxy nitrophenyl amide (generic).

    Science.gov (United States)

    2010-07-01

    ... amide (generic). 721.10063 Section 721.10063 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY... Specific Chemical Substances § 721.10063 Halo substituted hydroxy nitrophenyl amide (generic). (a) Chemical... as halo substituted hydroxy nitrophenyl amide (PMN P-04-792) is subject to reporting under this...

  7. Combined effect of kinetin and radiation treatment on the cap opening of Agaricus bisporus

    International Nuclear Information System (INIS)

    Kovacs, E.

    1982-01-01

    Cultivated mushrooms (Agaricus bisporus) with a cap diameter of 3-5 cm were incubated at 20 deg C during the experimental period (30-72 h). The degree of cap opening was determined and the data were evaluated. It was found that kinetin solutions in the 0 to 32 mg kg -1 range stimulated the opening of the mushroom cap. The shorter the time elapsed between picking and treating the mushrooms, the greater was the effect. A kinetin solution with a concentration of 100 mg kg -1 inhibited the opening of the cap. Cap opening in irradiated mushrooms cannot be induced even with kinetin concentrations that stimulate cap opening. Treatment with 0, 2.5 and 10 kGy doses of radiation the stimulating effect on cap opening decreased as a function of the rising dose. The radiation effects in kinetin solutions and various natural cytokinins (zeatin, 2iP and 2iPA) were studied and it was found that cytokinin solutions lost 50-60% of their activity after a radiation dose of only 1 kGy. (author)

  8. Studies on ligand exchange reaction of functionalized mercaptothiadiazole compounds onto citrate capped gold nanoparticles

    International Nuclear Information System (INIS)

    Kalimuthu, Palraj; John, S. Abraham

    2010-01-01

    Mercaptothiadiazole ligands functionalized with thiol (2,5-dimercapto-1,3,4-thiadiazole (DMT)) and methyl (5-methyl-2-mercapto-1,3,4-thiadiazole (MMT)) groups capped onto citrate capped gold nanoparticles (C-AuNPs) by ligand exchange reaction was investigated by UV-vis spectroscopy, FT-IR spectroscopy and transmission electron microscopy (TEM) techniques. The surface plasmon resonance band at 522 nm for C-AuNPs was shifted to 530 nm after capping with DMT whereas an additional band was observed at 630 nm due to aggregation in addition to a shift in the band at 522 nm after capping of MMT onto C-AuNPs. Thus, capping of DMT onto C-AuNPs leads to the formation of stable AuNPs while capping of MMT leads to the formation of unstable AuNPs. FT-IR studies show that the citrate ions were completely replaced by both DMT and MMT ligands from the AuNPs. TEM images indicate that the size and shape of the AuNPs remain same after capping of these ligands.

  9. Mechanisms of the p(He 6,He 5)d, p(He 6,{alpha})t and p(He 6,t){alpha} reactions

    Energy Technology Data Exchange (ETDEWEB)

    Heiberg-Andersen, Henning

    2002-07-01

    This work was devoted to nucleon induced transfer reactions having the potential to probe the sub-cluster structures of the benchmark halo nucleus He 6, without the question marks the necessarily omitted exchange effects tend to put behind the CRC results when both collision partners are composite systems. Still, the exchange complications entered the analysis in an ironic way: The high Q-value of the p(He 6,{alpha})t and p(He 6, t){alpha} reactions caused sensitivity to the t - {alpha} optical potential at small radii, where the one-nucleon exchange effects are strongest. Since the attempt to throw them out of the extracted tau - {alpha} potential failed, it was necessary to extend the model space to avoid a too difficult modelling of the local equivalent t - {alpha} potential. By this step, all the complications originating from antisymmetrization within a larger model space entered the analysis. However, the persistent failures of the two-channel calculations of this and previous works can hardly be due to incorrect treatment of exchange effects only, so the loss of simplicity is probably illusory. Even at small angles, where the surface processes dominate, none of the two-channel calculations with various choices of t - {alpha} optical potentials managed to reproduce the p(He 6, {alpha})t (p(He 6,t){alpha}) data. This motivated inclusion of sequential transfers through the d + He 5 channel, where the sequential triton transfer process, included just for consistency in the coupling scheme of the four-channel calculation, turned out to be more influent than expected. The satisfactory reproduction of both the p(He 6, He 5)d and the p(He 6,{alpha})t (p(He 6,t){alpha}) data by the four-channel approach and the required re-normalization the real part of the p - He 6 optical potential are strong indications of substantial contributions from sequential transfer of the halo neutrons at this energy. The conclusions that can be drawn from this work are limited by the

  10. Macrophage Capping Protein CapG Is a Putative Oncogene Involved in Migration and Invasiveness in Ovarian Carcinoma

    Directory of Open Access Journals (Sweden)

    J. Glaser

    2014-01-01

    Full Text Available The actin binding protein CapG modulates cell motility by interacting with the cytoskeleton. CapG is associated with tumor progression in different nongynecologic tumor entities and overexpression in breast cancer cell lines correlates with a more invasive phenotype in vitro. Here, we report a significant CapG overexpression in 18/47 (38% of ovarian carcinomas (OC analyzed by qRealTime-PCR analyses. Functional analyses in OC cell lines through siRNA mediated CapG knockdown and CapG overexpression showed CapG-dependent cell migration and invasiveness. A single nucleotide polymorphism rs6886 inside the CapG gene was identified, affecting a CapG phosphorylation site and thus potentially modifying CapG function. The minor allele frequency (MAF of SNP rs6886 (c.1004A/G was higher and the homozygous (A/A, His335 genotype was significantly more prevalent in patients with fallopian tube carcinomas (50% as in controls (10%. With OC being one of the most lethal cancer diseases, the detection of novel biomarkers such as CapG could reveal new diagnostic and therapeutic targets. Moreover, in-depth analyses of SNP rs6886 related to FTC and OC will contribute to a better understanding of carcinogenesis and progression of OC.

  11. Preparation of 5-benzotriazolyl-4-hydroxy-3- sec-butylbenzenesulfonate anion-intercalated layered double hydroxide and its photostabilizing effect on polypropylene

    Science.gov (United States)

    Li, Dianqing; Tuo, Zhenjun; Evans, David G.; Duan, Xue

    2006-10-01

    An organic UV absorber has been intercalated into a layered double hydroxide (LDH) host by ion-exchange method using ZnAl-NO 3-LDH as a precursor with an aqueous solution of the sodium salt of 5-benzotriazolyl-4-hydroxy-3- sec-butylbenzenesulfonic acid (BZO). After intercalation of the UV absorber, the interlayer distance in the LDHs increases from 0.89 to 2.32 nm. Infrared spectra and thermogravimetry and differential thermal analysis (TG-DTA) curves reveal the presence of a complex system of supramolecular host-guest interactions. The thermostability of BZO is markedly enhanced by intercalation in the LDH host. ZnAl-BZO-LDHs/polypropylene composite materials exhibit excellent UV photostability.

  12. 78 FR 22490 - Administrative Practice and Procedure; Postal Service; Review of Price Cap Rules

    Science.gov (United States)

    2013-04-16

    ...] Administrative Practice and Procedure; Postal Service; Review of Price Cap Rules AGENCY: Postal Regulatory Commission. ACTION: Proposed rule. SUMMARY: The Commission is initiating a review of its Price Cap Rules. The... implemented without a price cap calculation. Docket No. R2011-5, Order Approving Market Dominant Price...

  13. 40 CFR 1060.521 - How do I test fuel caps for permeation emissions?

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 32 2010-07-01 2010-07-01 false How do I test fuel caps for permeation... EQUIPMENT Test Procedures § 1060.521 How do I test fuel caps for permeation emissions? If you measure a fuel tank's permeation emissions with a nonpermeable covering in place of the fuel cap under § 1060.520(b)(5...

  14. Structural requirement of carboxyl-terminal globular domains of laminin alpha 3 chain for promotion of rapid cell adhesion and migration by laminin-5.

    Science.gov (United States)

    Hirosaki, T; Mizushima, H; Tsubota, Y; Moriyama, K; Miyazaki, K

    2000-07-21

    The basement membrane protein laminin-5, a heterotrimer of laminin alpha3, beta3, and gamma2 chains, potently promotes cellular adhesion and motility. It has been supposed that the carboxyl-terminal globular region of the alpha3 chain consisting of five distinct domains (G1 to G5) is important for its interaction with integrins. To clarify the function of each G domain, we transfected cDNAs for the full-length (wild type (WT)) and five deletion derivatives (DeltaGs) of the alpha3 chain into human fibrosarcoma cell line HT1080, which expressed and secreted the laminin beta3 and gamma2 chains but not the alpha3 chain. The transfectants with the alpha3 chain cDNAs lacking G5 (DeltaG(5)), G4-5 (DeltaG(4-5)), G3-5 (DeltaG(3-5)), and G2-5 (DeltaG(2-5)) secreted laminin-5 variants at levels comparable to that with WT cDNA. However, the transfectant with the cDNA without any G domains (DeltaG(1-5)) secreted little laminin-5, suggesting that the G domains are essential for the efficient assembly and secretion of the heterotrimer alpha3beta3gamma2. The transfectants with WT, DeltaG(5), and DeltaG(4-5) cDNAs survived in serum-free medium longer than those with DeltaG(3-5), DeltaG(2-5), and DeltaG(1-5) cDNAs. The transfectants with WT, DeltaG(5), and DeltaG(4-5) cDNAs secreted apparently the same size of laminin-5, which lacked G4 and G5 due to proteolytic cleavage between G3 and G4, and these laminin-5 forms potently promoted integrin alpha(3)beta(1)-dependent cell adhesion and migration. However, the laminin-5 forms of DeltaG(3-5) and DeltaG(2-5) hardly promoted the cell adhesion and motility. These findings demonstrate that the G3 domain, but not the G4 and G5 domains, of the alpha3 chain is essential for the potent promotion of cell adhesion and motility by laminin-5.

  15. Eddy intrusion of hot plasma into the polar cap and formation of polar-cap arcs

    International Nuclear Information System (INIS)

    Chiu, Y.T.; Gorney, D.J.

    1983-01-01

    We present plasma and electric field data obtained by the S3-3 satellite over the polar caps. We demonstrate that: (1) plasma signatures in the polar cap arc formation region near 5000 km altitude show clear intrusions of plasma sheet (approx.keV) and magneto sheath (approx.100 eV) plasma into a background of low-energy polar cap plasma; (2) the combined plasma and electric field signatures (electron inverted-V, ion beam and delxE<0) are exactly the same as in the evening discrete arc. We interpret this equivalence of polar cap and evening discrete arc signatures as indication that their formation processes are identical. The spatial structures of polar cap electric fields and the associated plasma signatures are consistent with the hypothesis that plasma intrusion into the polar cap takes the form of multiple cellular eddies. This hypothesis provides a unifying view of arc formation and arc configurations

  16. On the polarization of Herbig Ae/Be star radiation

    Energy Technology Data Exchange (ETDEWEB)

    Petrova, N I; Shevchenko, V S

    1987-08-01

    Results of multicolor UBVRI polarimetry of 14 Herbig Ae/Be stars including 7 stars for which observations of polarization have been made for the first time are presented. 6 bright Herbig Ae/Be stars (As 441, AS 442, LK H..cap alpha..134, LK H..cap alpha..135, Lk H..cap alpha..169 and V517 Cyg) which belong to star formation region connected with IC 5070 show the polarization from 1 to 4.5. per cent with similar theta (approx. 180 deg) (basically of interstellar nature). The polarimetrical variability of BD+46 deg 3471, BD+65 deg 1637, HD 200775 and Lk H..cap alpha..234 is confirmed. Mechanismes of polarization in Herbig Ae/Be stars in circumstellar formations are discussed.

  17. Conformational analysis and vibrational spectroscopy of a paracetamol analogous: 2-Bromo-N-(2-hydroxy-5-methylphenyl)-2-methylpropanamide

    Science.gov (United States)

    Viana, Rommel B.; Quintero, David E.; Viana, Anderson B.; Moreno-Fuquen, Rodolfo

    2017-11-01

    We conducted an experimental and quantum chemical investigation of the electronic properties and vibrational mode couplings of a structure analogous to a paracetamol (acetaminophen): 2-Bromo-N-(2-hydroxy-5-methylphenyl)-2-methylpropanamide. The spectroscopic and electronic properties were carried out with the PBE1PBE functional, and G3MP2 was used to predict the heat of formation. Among the E/Z stereoisomers, we showed that the energy gap ranged from 3 to 10 kcal mol-1; the relative stability among the regioisomers (involving the different positions of the methyl and hydroxyl groups) exhibited energy differences lower than 5 kcal mol-1. A topological analysis using the Quantum Theory of Atoms in Molecules (QTAIM) was performed to determine the intramolecular hydrogen bonds that govern the configuration changes, and the Natural Bond Orbital method was used to estimate the interplay between the steric and electrostatic interactions that stabilized each isomer. It was also estimated the influence of the population methodology in to predict the atomic charge distribution for the title compound.

  18. γ-Dodecelactone production from safflower oil via 10-hydroxy-12(Z)-octadecenoic acid intermediate by whole cells of Candida boidinii and Stenotrophomonas nitritireducens.

    Science.gov (United States)

    Jo, Ye-Seul; An, Jung-Ung; Oh, Deok-Kun

    2014-07-16

    Candida boidinii was selected as a γ-dodecelactone producer because of the highest production of γ-dodecelactone from 10-hydroxy-12(Z)-octadecenoic acid among the 11 yeast strains tested. Under the reaction conditions of pH 5.5 and 25 °C with 5 g/L 10-hydroxy-12(Z)-octadecenoic acid and 30 g/L cells, whole C. boidinii cells produced 2.1 g/L γ-dodecelactone from 5 g/L 10-hydroxy-12(Z)-octadecenoic acid after 6 h, with a conversion yield of 64% (mol/mol) and a volumetric productivity of 350 mg/L/h. The production of γ-dodecelactone from safflower oil was performed by lipase hydrolysis reaction and two-step whole-cell biotransformation using Stenotrophomonas nitritireducens and C. boidinii. γ-Dodecelactone at 1.88 g/L was produced from 7.5 g/L safflower oil via 5 g/L 10-hydroxy-12(Z)-octadecenoic acid intermediate by these reactions after 8 h of reaction time, with a volumetric productivity of 235 mg/L/h and a conversion yield of 25% (w/w). To the best of the authors' knowledge, this is the highest volumetric productivity and conversion yield reported to date for the production of γ-lactone from natural oils.

  19. Pulp-Capping with Mineral Trioxide Aggregate

    Directory of Open Access Journals (Sweden)

    Peycheva Kalina

    2015-11-01

    Full Text Available There are two considerations for direct pulp capping - accidental mechanical pulp exposure and exposure caused by caries. Mineral trioxide aggregate (MTA was used as pulp-capping material to preserve the vitality of the pulpal tissues. Follow-up examinations revealed that treatment was successful in preserving pulpal vitality and continued development of the tooth. On the basis of available information, it appears that MTA is the material of choice for some clinical applications. Material and methods: Cases 18 - 8 teeth with grey MTA, 10 teeth with white MTA; diagnose: Pulpitis chronica ulcerosa, Electro pulpal test (EOD - 30-35 μA, pre-clinical X-ray - without changes in the structures, follow ups for 4 years. Successful treatments: without clinical symptoms and changes in the X-rays: 5 teeth with grey MTA, 8 teeth with white MTA for period of 4 years. Unsuccessful treatments: Clinical symptoms and sometimes changes in the X-ray: 3 with grey MTA, 2 with white MTA. MTA is an appropriate material for pulp-capping and follow-up examinations revealed that the treatment was successful in preserving pulpal vitality.

  20. T-Cap Pull-Off and Bending Behavior for Stitched Structure

    Science.gov (United States)

    Lovejoy, Andrew E.; Leone, Frank A., Jr.

    2016-01-01

    The Pultruded Rod Stitched Efficient Unitized Structure (PRSEUS) is a structural concept that was developed by The Boeing Company to address the complex structural design aspects associated with a pressurized hybrid wing body aircraft configuration. An important design feature required for assembly is the integrally stitched T-cap, which provides connectivity of the corner (orthogonal) joint between adjacent panels. A series of tests were conducted on T-cap test articles, with and without a rod stiffener penetrating the T-cap web, under tension (pull-off) and bending loads. Three designs were tested, including the baseline design used in largescale test articles. The baseline had only the manufacturing stitch row adjacent to the fillet at the base of the T-cap web. Two new designs added stitching rows to the T-cap web at either 0.5- or 1.0-inch spacing along the height of the web. Testing was conducted at NASA Langley Research Center to determine the behavior of the T-cap region resulting from the applied loading. Results show that stitching arrests the initial delamination failures so that the maximum strength capability exceeds the load at which the initial delaminations develop. However, it was seen that the added web stitching had very little effect on the initial delamination failure load, but actually decreased the initial delamination failure load for tension loading of test articles without a stiffener passing through the web. Additionally, the added web stitching only increased the maximum load capability by between 1% and 12.5%. The presence of the stiffener, however, did increase the initial and maximum loads for both tension and bending loading as compared to the stringerless baseline design. Based on the results of the few samples tested, the additional stitching in the T-cap web showed little advantage over the baseline design in terms of structural failure at the T-cap web/skin junction for the current test articles.

  1. Designing Smart Charter School Caps

    Science.gov (United States)

    Dillon, Erin

    2010-01-01

    In 2007, Andrew J. Rotherham proposed a new approach to the contentious issue of charter school caps, the statutory limits on charter school growth in place in several states. Rotherham's proposal, termed "smart charter school caps," called for quality sensitive caps that allow the expansion of high-performing charter schools while also…

  2. Activity of L-alpha-amino acids at the promiscuous goldfish odorant receptor 5.24

    DEFF Research Database (Denmark)

    Christiansen, Bolette; Wellendorph, Petrine; Bräuner-Osborne, Hans

    2006-01-01

    The goldfish odorant receptor 5.24 is a member of family C of G protein-coupled receptors and is closely related to the human receptor GPRC6A. Receptor 5.24 has previously been shown to have binding affinity for L-alpha-amino acids, especially the basic amino acids arginine and lysine. Here we...

  3. Structural, vibrational spectroscopic and nonlinear optical activity studies on 2-hydroxy- 3, 5-dinitropyridine: A DFT approach

    Science.gov (United States)

    Asath, R. Mohamed; Premkumar, S.; Jawahar, A.; Mathavan, T.; Dhas, M. Kumara; Benial, A. Milton Franklin

    2015-06-01

    The conformational analysis was carried out for 2-Hydroxy- 3, 5-dinitropyridine molecule using potential energy surface scan and the most stable optimized conformer was predicted. The vibrational frequencies and Mulliken atomic charge distribution were calculated for the optimized geometry of the molecule using DFT/B3LYP cc-pVQZ basis set by Gaussian 09 Program. The vibrational frequencies were assigned on the basis of potential energy distribution calculation using VEDA 4.0 program. In the Frontier molecular orbitals analysis, the molecular reactivity, kinetic stability, intramolecular charge transfer studies and the calculation of ionization energy, electron affinity, global hardness, chemical potential, electrophilicity index and softness values of the title molecule were carried out. The nonlinear optical activity of the molecule was studied by means of first order hyperpolarizability, which was computed as 7.64 times greater than urea. The natural bond orbital analysis was performed to confirm the nonlinear optical activity of the molecule.

  4. FaQR, required for the biosynthesis of the strawberry flavor compound 4-hydroxy-2,5-dimethyl-3(2H)-furanone, encodes an enone oxidoreductase.

    Science.gov (United States)

    Raab, Thomas; López-Ráez, Juan Antonio; Klein, Dorothée; Caballero, Jose Luis; Moyano, Enriqueta; Schwab, Wilfried; Muñoz-Blanco, Juan

    2006-04-01

    The flavor of strawberry (Fragaria x ananassa) fruit is dominated by an uncommon group of aroma compounds with a 2,5-dimethyl-3(H)-furanone structure. We report the characterization of an enzyme involved in the biosynthesis of 4-hydroxy-2,5-dimethyl-3(2H)-furanone (HDMF; Furaneol), the key flavor compound in strawberries. Protein extracts were partially purified, and the observed distribution of enzymatic activity correlated with the presence of a single polypeptide of approximately 37 kD. Sequence analysis of two peptide fragments showed total identity with the protein sequence of a strongly ripening-induced, auxin-dependent putative quinone oxidoreductase, Fragaria x ananassa quinone oxidoreductase (FaQR). The open reading frame of the FaQR cDNA consists of 969 bp encoding a 322-amino acid protein with a calculated molecular mass of 34.3 kD. Laser capture microdissection followed by RNA extraction and amplification demonstrated the presence of FaQR mRNA in parenchyma tissue of the strawberry fruit. The FaQR protein was functionally expressed in Escherichia coli, and the monomer catalyzed the formation of HDMF. After chemical synthesis and liquid chromatography-tandem mass spectrometry analysis, 4-hydroxy-5-methyl-2-methylene-3(2H)-furanone was confirmed as a substrate of FaQR and the natural precursor of HDMF. This study demonstrates the function of the FaQR enzyme in the biosynthesis of HDMF as enone oxidoreductase and provides a foundation for the improvement of strawberry flavor and the biotechnological production of HDMF.

  5. Protection to glycolysis by a combination of 5-hydroxy-L-tryptophan and 2-aminoethylisothiuronium bromide hydrobromide in lethally irradiated rats

    International Nuclear Information System (INIS)

    Basu, S.K.; Srinivasan, M.N.; Chuttani, K.; George, S.

    1992-01-01

    Rate of glycolysis in vivo at different time intervals following 8 Gy[LDsub(100(30)] whole body gamma radiation (WBGR) was evaluated by estimating liver glycogen, blood sugar, serum lactic dehydrogenase (LDH) and lactic acid concentration in adult male Sprague Dawley rats. Within 1 hr of radiation exposure, a significant fall in liver glycogen was observed in rats fed food and water ad libitum. The glycogen content increased after 24 hr and had returned to control level on 7th day after radiation exposure. Blood sugar, serum LDH and blood lactate levels increased significantly as compared to non irradiated controls. Pretreatment with 5-hydroxy-L-tryptophan (5-HTP;100 mg/kg) + 2-aminoethylisothiuronium bromide hydrobromide (AET;20 mg/kg)ip 30 min before 8 Gy WBGR, modified these values and restored them to normal level on 7th day post-irradiation. (author). 24 refs

  6. Synthesis of 25-hydroxy-[26,27-3H]vitamin D2, 1,25-dihydroxy-[26,27-3H]vitamin D2 and their (24R)-epimers

    International Nuclear Information System (INIS)

    Sicinski, R.R.; Tanaka, Y.; Phelps, M.; Schnoes, H.K.; DeLuca, H.F.

    1987-01-01

    Synthesis of a C-24-epimeric mixture of 25-hydroxy-[26,27- 3 H]vitamin D2 and a C-24-epimeric mixture of 1,25-dihydroxy-[26,27- 3 H]vitamin D2 by the Grignard reaction of the corresponding 25-keto-27-nor-vitamin D2 and 1 alpha-acetoxy-25-keto-27-nor-vitamin D3 with tritiated methyl magnesium bromide is described. Separation of epimers by high-performance liquid chromatography afforded pure radiolabeled vitamins of high specific activity (80 Ci/mmol). The identities and radiochemical purities of 25-hydroxy-[26,27- 3 H[vitamin D2 and 1,25-dihydroxy-[26,27- 3 H]vitamin D2 D2 were established by cochromatography with synthetic 25-hydroxyvitamin D2 or 1,25-dihydroxyvitamin D2. Biological activity of 25-hydroxy-[26,27- 3 H]vitamin D2 was demonstrated by its binding to the rat plasma binding protein for vitamin D compounds, and by its in vitro conversion to 1,25-dihydroxy-[26,27- 3 H]vitamin D2 by kidney homogenate prepared from vitamin D-deficient chickens. The biological activity of 1,25-dihydroxy-[26,27- 3 H]vitamin D2 was demonstrated by its binding to the chick intestinal receptor for 1,25-dihydroxyvitamin D3

  7. Experimental demonstration of optical data links using a hybrid CAP/QAM modulation scheme.

    Science.gov (United States)

    Wei, J L; Ingham, J D; Cheng, Q; Cunningham, D G; Penty, R V; White, I H

    2014-03-15

    The first known experimental demonstrations of a 10  Gb/s hybrid CAP-2/QAM-2 and a 20  Gb/s hybrid CAP-4/QAM-4 transmitter/receiver-based optical data link are performed. Successful transmission over 4.3 km of standard single-mode fiber (SMF) is achieved, with a link power penalty ∼0.4  dBo for CAP-2/QAM-2 and ∼1.5  dBo for CAP-4/QAM-4 at BER=10(-9).

  8. NATURE MANAGEMENT, LANDSCAPE AND THE CAP

    OpenAIRE

    Brouwer, Floor M.; Godeschalk, Frans E.

    2004-01-01

    The integration of nature management, landscape and environmental concerns into the Common Agricultural Policy (CAP) has gained momentum with the CAP reforms adopted in June 2003. The report explores instruments and approaches that contribute to the inte-gration of nature conservation and landscape concerns into the CAP. A broader use of the CAP instruments might help to achieve nature types in the Netherlands.

  9. CAPS Simulation Environment Development

    Science.gov (United States)

    Murphy, Douglas G.; Hoffman, James A.

    2005-01-01

    The final design for an effective Comet/Asteroid Protection System (CAPS) will likely come after a number of competing designs have been simulated and evaluated. Because of the large number of design parameters involved in a system capable of detecting an object, accurately determining its orbit, and diverting the impact threat, a comprehensive simulation environment will be an extremely valuable tool for the CAPS designers. A successful simulation/design tool will aid the user in identifying the critical parameters in the system and eventually allow for automatic optimization of the design once the relationships of the key parameters are understood. A CAPS configuration will consist of space-based detectors whose purpose is to scan the celestial sphere in search of objects likely to make a close approach to Earth and to determine with the greatest possible accuracy the orbits of those objects. Other components of a CAPS configuration may include systems for modifying the orbits of approaching objects, either for the purpose of preventing a collision or for positioning the object into an orbit where it can be studied or used as a mineral resource. The Synergistic Engineering Environment (SEE) is a space-systems design, evaluation, and visualization software tool being leveraged to simulate these aspects of the CAPS study. The long-term goal of the SEE is to provide capabilities to allow the user to build and compare various CAPS designs by running end-to-end simulations that encompass the scanning phase, the orbit determination phase, and the orbit modification phase of a given scenario. Herein, a brief description of the expected simulation phases is provided, the current status and available features of the SEE software system is reported, and examples are shown of how the system is used to build and evaluate a CAPS detection design. Conclusions and the roadmap for future development of the SEE are also presented.

  10. The cervical cap (image)

    Science.gov (United States)

    The cervical cap is a flexible rubber cup-like device that is filled with spermicide and self-inserted over the cervix ... left in place several hours after intercourse. The cap is a prescribed device fitted by a health ...

  11. Hydroxy protons as structural probes to reveal hydrogen bonding properties of polyols in aqueous solution by NMR spectroscopy

    Science.gov (United States)

    Oruc, Gizem; Varnali, Tereza; Bekiroglu, Somer

    2018-05-01

    The solution properties of ethylene glycol (ethane-1,2-diol), glycerol (propane-1,2,3-triol), erythritol ((2R,3S)-butane-1,2,3,4-tetraol), D-xylitol ((2R,3r,4S)-pentane-1,2,3,4,5-pentaol), D-mannitol ((2R,3R,4R,5R)-hexane-1,2,3,4,5,6-hexaol), and D-sorbitol ((2S,3R,4R,5R)-hexane-1,2,3,4,5,6-hexaol), constituting a subgroup of polyalcohols/polyols of maximum six carbon atoms have been investigated using 1H NMR chemical shifts, coupling constants, temperature coefficients, and chemical exchange rates of hydroxy protons in aqueous medium. Relative within a molecule, minimum two-fold difference in rate of exchange values and higher temperature dependence of chemical shifts of the hydroxy protons on terminal carbon atoms confirm that sustainable hydrogen bonding interactions is accentuated for the hydroxyl groups on secondary carbons. Compared to the primary carbons i.e. terminal ones, the hydroxy protons on second and third carbon atoms exhibit much lower rate of exchange and smaller temperature coefficients, indicating that they are further involved in transient hydrogen bonding interactions. Scalar 3JOH,CH-couplings ranging between 3.9 and 7.2 Hz imply that the hydroxyl groups are practically in free rotation regime. Examination of the chemical shift differences with respect to the shift of glycol hydroxy proton reveals that the disparity between terminal and inner hydroxyl groups disclosed by the exchange rates and temperature coefficients is sustained with the exception of 0.003 and 0.053 ppm for O(3)H of mannitol and O(5)H of sorbitol respectively. The experimental findings have been augmented by quantum chemical calculations targeting theoretical NMR chemical shifts, as well as the conformational analysis of the structures.

  12. Pharmacologically relevant receptor binding characteristics and 5alpha-reductase inhibitory activity of free Fatty acids contained in saw palmetto extract.

    Science.gov (United States)

    Abe, Masayuki; Ito, Yoshihiko; Oyunzul, Luvsandorj; Oki-Fujino, Tomomi; Yamada, Shizuo

    2009-04-01

    Saw palmetto extract (SPE), used widely for the treatment of benign prostatic hyperplasia (BPH) has been shown to bind alpha(1)-adrenergic, muscarinic and 1,4-dihydropyridine (1,4-DHP) calcium channel antagonist receptors. Major constituents of SPE are lauric acid, oleic acid, myristic acid, palmitic acid and linoleic acid. The aim of this study was to investigate binding affinities of these fatty acids for pharmacologically relevant (alpha(1)-adrenergic, muscarinic and 1,4-DHP) receptors. The fatty acids inhibited specific [(3)H]prazosin binding in rat brain in a concentration-dependent manner with IC(50) values of 23.8 to 136 microg/ml, and specific (+)-[(3)H]PN 200-110 binding with IC(50) values of 24.5 to 79.5 microg/ml. Also, lauric acid, oleic acid, myristic acid and linoleic acid inhibited specific [(3)H]N-methylscopolamine ([(3)H]NMS) binding in rat brain with IC(50) values of 56.4 to 169 microg/ml. Palmitic acid had no effect on specific [(3)H]NMS binding. The affinity of oleic acid, myristic acid and linoleic acid for each receptor was greater than the affinity of SPE. Scatchard analysis revealed that oleic acid and lauric acid caused a significant decrease in the maximal number of binding sites (B(max)) for [(3)H]prazosin, [(3)H]NMS and (+)-[(3)H]PN 200-110. The results suggest that lauric acid and oleic acid bind noncompetitively to alpha(1)-adrenergic, muscarinic and 1,4-DHP calcium channel antagonist receptors. We developed a novel and convenient method of determining 5alpha-reductase activity using LC/MS. With this method, SPE was shown to inhibit 5alpha-reductase activity in rat liver with an IC(50) of 101 microg/ml. Similarly, all the fatty acids except palmitic acid inhibited 5alpha-reductase activity, with IC(50) values of 42.1 to 67.6 microg/ml. In conclusion, lauric acid, oleic acid, myristic acid, and linoleic acid, major constituents of SPE, exerted binding activities of alpha(1)-adrenergic, muscarinic and 1,4-DHP receptors and inhibited 5

  13. Does uncertainty justify intensity emission caps?

    International Nuclear Information System (INIS)

    Quirion, Philippe

    2005-01-01

    Environmental policies often set 'relative' or 'intensity' emission caps, i.e. emission limits proportional to the polluting firm's output. One of the arguments put forth in favour of relative caps is based on the uncertainty on business-as-usual output: if the firm's production level is higher than expected, so will be business-as-usual emissions, hence reaching a given level of emissions will be more costly than expected. As a consequence, it is argued, a higher emission level should be allowed if the production level is more important than expected. We assess this argument with a stochastic analytical model featuring two random variables: the business-as-usual emission level, proportional to output, and the slope of the marginal abatement cost curve. We compare the relative cap to an absolute cap and to a price instrument, in terms of welfare impact. It turns out that in most plausible cases, either a price instrument or an absolute cap yields a higher expected welfare than a relative cap. Quantitatively, the difference in expected welfare is typically very small between the absolute and the relative cap but may be significant between the relative cap and the price instrument. (author)

  14. Classification of two steroids, prostanozol and methasterone, as Schedule III anabolic steroids under the Controlled Substance Act. Final rule.

    Science.gov (United States)

    2012-07-30

    With the issuance of this Final Rule, the Administrator of the DEA classifies the following two steroids as "anabolic steroids'' under the Controlled Substances Act (CSA): prostanozol (17[beta]-hydroxy-5[alpha]-androstano[3,2-c]pyrazole) and methasterone (2[alpha],17[alpha]-dimethyl-5[alpha]-androstan-17[beta]-ol-3-one). These steroids and their salts, esters, and ethers are Schedule III controlled substances subject to the regulatory control provisions of the CSA.

  15. Selective inhibitory effects of (S)-9-(3-hydroxy-2-phosphonyl-methoxypropyl)adenine and 1-(2'-deoxy-2'-fluoro-ß-D-arabinofuranosyl)-5-iodouracil on seal herpesvirus (Phocid herpesvirus 1) infection in vitro.

    NARCIS (Netherlands)

    A.D.M.E. Osterhaus (Albert); J. Groen (Jan); E. de Clercq

    1987-01-01

    textabstractFrom a selection of 25 antiviral compounds with specific anti-herpes activity or broad-spectrum antiviral properties, two compounds, namely (S)-9-(3-hydroxy-2-phosphonyl-methoxypropyl)adenine and 1-(2'-deoxy-2'-fluoro-beta-D-arabinofuranosyl)-5-iodouracil, appeared particularly effective

  16. Synthesis and luminescent properties of star-burst D-π-A compounds based on 1,3,5-triazine core and carbazole end-capped phenylene ethynylene arms

    Energy Technology Data Exchange (ETDEWEB)

    Zhang, Zheng [Department of Applied Chemistry, Nanjing Tech University, Nanjing 210009 (China); Liu, Rui, E-mail: rui.liu@njtech.edu.cn [Department of Applied Chemistry, Nanjing Tech University, Nanjing 210009 (China); Zhu, Xiaolin [Department of Applied Chemistry, Nanjing Tech University, Nanjing 210009 (China); Li, Yuhao [Department of Chemistry, Fudan University, 220 Handan Road, Shanghai 200433 (China); Chang, Jin [Queensland University of Technology, 2 George St., Brisbane 4000 (Australia); Zhu, Hongjun, E-mail: zhuhjnjut@hotmail.com [Department of Applied Chemistry, Nanjing Tech University, Nanjing 210009 (China); Ma, Liangwei; Lv, Wangjie; Guo, Jun [Department of Applied Chemistry, Nanjing Tech University, Nanjing 210009 (China)

    2014-12-15

    Two new star-burst compounds based on 1,3,5-triazine core and carbazole end-capped phenylene ethynylene arms (1a and 1b) were synthesized and characterized. Their photophysical properties were investigated systematically via spectroscopic and theoretical methods. Both compounds exhibit strong {sup 1}π–π{sup ⁎} transitions in the UV region and intense {sup 1}π–π{sup ⁎}/intramolecular charge transfer ({sup 1}ICT) absorption bands in the UV–vis region. Introducing the carbazole end-capped phenylene ethynylene arm on the 1,3,5-triazine core causes a slight bathochromic shift and enhanced molar extinction coefficient of the {sup 1}π–π{sup ⁎}/{sup 1}ICT transition band. Both compounds are emissive in solution at room temperature and 77 K, which exhibit pronounced positive solvatochromic effect. The emitting state could be ascribed to {sup 1}ICT state in more polar solvent, and {sup 1}π–π{sup ⁎} state in low-polarity solvent. The high emission quantum yields (Φ{sub em}=0.90∼1.0) of 1a and 1b (in hexane and toluene) make them potential candidates as efficient light-emitting materials. The spectroscopic studies and theoretical calculations indicate that the photophysical properties of these compounds can be tuned by the carbazole end-capped phenylene ethynylene arm, which would also be useful for rational design of photofunctional materials. - Highlights: • Star-burst compounds based on 1,3,5-triazine core and carbazole end-capped phenylene ethynylene arms. • Photophysical properties of target compounds were investigated systematically via spectroscopic and theoretical methods. • The relatively high fluorescence quantum yields make them potential candidates as light-emitting materials.

  17. Cryopyrin-Associated Autoinflammatory Syndromes (CAPS) - Juvenile

    Science.gov (United States)

    ... all ethnic groups can be affected. What are CAPS? Cryopyrin-associated autoinflammatory syndromes (CAPS) consist of three ... ears by magnetic resonance imaging (MRI). How is CAPS treated? Medications that target interleukin-1 are very ...

  18. Synthesis of 7-hydroxy-4'-methoxyflavanone and 7-hydroxy-4'-methoxyflavone as a candidate anticancer against cervical (HeLa) cancer cell and colon (WiDr) cancer cell by in vitro

    Science.gov (United States)

    Matsjeh, Sabirin; Anwar, Chairil; Solikhah, Eti Nurwening; Farah, Harra Ismi; Nurfitria, Kurnia

    2017-03-01

    The compound 7-hydroxy-4'-methoxyflavanone and 7-hydroxy-4'-methoxyflavone have been synthesized through cyclization reaction of 2 ', 4'-dihydroxy-4-methoxychalcone (1,3-diphenyl-2-propene-1-one). The 2 ', 4'-dihydroxy-4-methoxychalcone were synthesized through Claisen-Schmidt condensation from 2,4-dihydroxyacetophenone and 4-methoxybenzaldehyde (anisaldehyde) in aqueous KOH as a catalyst in ethanol. The 7-hydroxy-4'-methoxyflavanone has been synthesized through cyclization reaction of 2 ', 4'-dihydroxy-4-methoxychalcone by Oxa-Michael addition reaction with sulfuric acid as a catalyst in ethanol. The 7-hydroxy-4'-methoxyflavone has been synthesized through oxidative cyclization reaction of 2 ', 4'-dihydroxy-4-methoxychalcone using I2 in DMSO as a catalyst with a mole ratio (1: 1) mol. All these producets were characterized by FT-IR, GC-MS, and 1H-NMR and 13C-NMR spectrometer. Both of these compounds were tested citotoxycity activity as an anticancer against cervical and colon cancer cells (HeLa and WiDr cell lines) using MTT assay in vitro. Dose series given test solution concentration on HeLa and WiDr cells starting from 0,78; 1,56; 3,12; 6,25; 12,50; 25; 50 and 100 µg/mL with a long incubation treatment for 24 hours. The results study showed that the 7-hydroxy-4'-methoxyflavanone as bright yellow crystals with a melting point 172-174 ° C and a yield of 56.67% and the 7-hydroxy-4'-methoxyflavone as bright yellow crystals with a yield of 88, 31%, and a melting point of 263-265 ° C. The test results cytotoxic 7-hydroxy-4-methoxyflavone showed active against HeLa cells with IC50 value of 25.73 µg/mL and was quite active in the WiDr cells with IC50 value of 83.75 µg/mL. The result of the activity of 7-hydroxy-4-methoxyflavanone show active cytotoxic activity against HeLa and WiDr cell growth with IC50 value of 40.13 µg/mL and 37.85 µg/mL. IC50 value indicated that 7-hydroxy-4'-methoxyflavone and 7-hydroxy-4'-methoxyflavanone potential as inhibitors in HeLa and

  19. Optical properties, electronic structure and magnetism of alpha '-NaxV2O5

    NARCIS (Netherlands)

    Konstantinovic, MI; Popovic, ZV; Presura, C; Gajic, R; Isobe, M; Ueda, Y; Moshchalkov, VV

    2002-01-01

    The optical properties of sodium-deficient alpha'-NaxV2O5 (0.85 less than or equal to x less than or equal to 1.00) single crystals are analyzed using ellipsometry, and infrared reflectivity techniques. In sodium deficient samples, the optical absorption peak associated to the fundamental electronic

  20. The North Zealand CAP Monitor

    DEFF Research Database (Denmark)

    Nielsen, Minna; Ravn, Pernille; Notander Clausen, Lise

    with CAP. We started with 34 audit variables. Through repeated cycles of testing, feedback and discussions, we reduced the number of indicators to 22 and time per audit from 20 to 10 minutes. Strategy for change To link the monitoring system with our patient pathway for CAP we established an improvement...... Designing a database Designing and testing a dashboard to present indicators in a balanced way Messages for others Auditing patients with a common disease as CAP is useful to identify areas for improvement for a large group of patients. The baseline audit can serve as a basis for a monitoring system......Contect We describe how we developed a monitoring system for community acquired pneumonia (CAP) at North Zealand Regional hospital. We serve 310.000 inhabitants and annually around 3200 patients with CAP are admitted. As part of a program of clinical pathways for common conditions, a pathway...

  1. Pengelolaan Fraktur Dentoalveolar pada Anak-Anak dengan Cap Splint Akrilik

    Directory of Open Access Journals (Sweden)

    Dedy Sigit Nur Cahyo

    2015-12-01

    Management of Dentoalveolar Fractures in Children Using Acrylic Cap Splint. The purpose of fracture treatment in children is basically the same as that in adults with different management, while the choice of treatment method mainly relies on the development of jaws and teeth. It reports two cases of dentoalveolar fractures in children under 5 years old who were treated using acrylic cap splint with circum-mandibular wiring under general anesthetic. Two children, aged 1 year and 3 years old were referred to the emergency department of Dr. Sardjito Hospital with the diagnosis of dentoalveolar fractures. Both cases were treated using cap splint with circum-mandibular wiring-based fixation under general anesthetic. After 3 weeks, the acrylic cap splint and the circum-mandibular wiring were released under sedation. No loose teeth were found in the fracture area. In the following 6 weeks, the teeth were stable with normal occlusion and no infection found. Acrylic cap splint with circum-mandibular wiring is a simple, effective and minimally invasive method for dentoalveolar treatment in children.

  2. Endothelial-monocyte activating polypeptide II alters fibronectin based endothelial cell adhesion and matrix assembly via alpha5 beta1 integrin

    International Nuclear Information System (INIS)

    Schwarz, Margaret A.; Zheng, Hiahua; Liu, Jie; Corbett, Siobhan; Schwarz, Roderich E.

    2005-01-01

    Mature Endothelial-Monocyte Activating Polypeptide (mEMAP) II functions as a potent antiangiogenic peptide. Although the anti-tumor effect of mEMAP II has been described, little is known regarding its mechanism of action. Observations that mEMAP II induced apoptosis only in a subset of migrating and proliferating endothelial cells (EC) suggests a targeted effect on cells engaged in angiogenic activities which are known to rely upon cell adhesion and migration. Indeed, we demonstrate that mEMAP II inhibited fibronectin (FN) dependent microvascular EC (MEC) adhesion and spreading and we show that this depends upon the alpha5 beta1 integrin. Immunofluorescence analysis demonstrated that mEMAP II-dependent blockade of FN-alpha5 beta1 interactions was associated with disassembly of both actin stress fiber networks and FN matrix. These findings suggest that mEMAP II blocks MEC adhesion and spreading on fibronectin, via a direct interaction with the integrin alpha5 beta1, thus implicating that alpha5 integrin may be a mediator of mEMAP II's antiangiogenic function

  3. New catalysts for selective hydrogenation of diene and acetylene hydrocarbons into olefins

    Energy Technology Data Exchange (ETDEWEB)

    Frolov, V.M.; Parenago, O.P.; Shuikina, L.P.

    1978-12-01

    New catalysts for selective hydrogenation of diene and acetylene hydrocarbons into olefins were obtained by reacting aqueous palladium, rhodium, or nickel chloride (0.005-0.05 mole/l.) at 50/sup 0/C, in an argon atmosphere with chelating nitrogen compounds, i.e., o-phenanthroline, ..cap alpha..,..cap alpha..'-dipyridyl, sodium ethylenediaminetetracetate, morpholine, branched polyethylene imines, or amino acids such as glycine, ..cap alpha..-alanine, ..beta..-phenyl-..cap alpha..-alanine, tyrosine, or histidine, and treating the complexes so obtained with sodium borohydride at 1:1-1:5 NaBH/sub 4/-metal ratios, in an aqueous medium. Palladium-based complexes showed the highest activities (20-98Vertical Bar3< conversion) and selectivities (98-100Vertical Bar3<) in heterogeneous hydrogenation of cyclopentadiene, butadiene, 1-hexyne, 1,3-cyclohexadiene, or 1,3-cyclooctadiene at 20/sup 0/-60/sup 0/C and 0.5-15 atm hydrogen, carried out in a kinetic circulation reactor or a metallic autoclave. Thus, a catalytic system based on PdCl/sub 2/ and ..beta..-phenyl-..cap alpha..-alanine converted 98Vertical Bar3< of cyclopentadiene to cyclopentene with 99Vertical Bar3< selectivity. The palladium-based catalyst did not deactivate on the contact with air.

  4. Unexpected ethical dilemmas in sex assignment in 46,XY DSD due to 5-alpha reductase type 2 deficiency.

    Science.gov (United States)

    Byers, Heather M; Mohnach, Lauren H; Fechner, Patricia Y; Chen, Ming; Thomas, Inas H; Ramsdell, Linda A; Shnorhavorian, Margarett; McCauley, Elizabeth A; Amies Oelschlager, Anne-Marie E; Park, John M; Sandberg, David E; Adam, Margaret P; Keegan, Catherine E

    2017-06-01

    Sex assignment at birth remains one of the most clinically challenging and controversial topics in 46,XY disorders of sexual development (DSD). This is particularly challenging in deficiency of 5-alpha reductase type 2 given that external genitalia are typically undervirilized at birth but typically virilize at puberty to a variable degree. Historically, most individuals with 5-alpha reductase deficiency were raised females. However, reports that over half of patients who underwent a virilizing puberty adopted an adult male gender identity have challenged this practice. Consensus guidelines on assignment of sex of rearing at birth are equivocal or favor male assignment in the most virilized cases. While a male sex of rearing assignment may avoid lifelong hormonal therapy and/or allow the potential for fertility, female sex assignment may be more consistent with external anatomy in the most severely undervirilized cases. Herein, we describe five patients with 46,XY DSD due 5-alpha-reductase type 2 deficiency, all with a severe phenotype. An inter-disciplinary DSD medical team at one of two academic centers evaluated each patient. This case series illustrates the complicated decision-making process of assignment of sex of rearing at birth in 5-alpha reductase type 2 deficiency and the challenges that arise when the interests of the child, parental wishes, recommendations of the medical team, and state law collide. © 2017 Wiley Periodicals, Inc.

  5. Synthesis, spectroscopic characterization, theoretical study and anti-hepatic cancer activity study of 4-(1E,3Z,6E)-3-hydroxy-7-(4-hydroxy-3-methoxyphenyl)-5-oxohepta-1,3,6-trien-1-yl)-2-methoxyphenyl 4-nitrobenzoate, a novel curcumin congener

    Science.gov (United States)

    Srivastava, Sangeeta; Gupta, Preeti; Singh, Ranvijay Pratap; Jafri, Asif; Arshad, M.; Banerjee, Monisha

    2017-08-01

    In the present work 4-(1E,3Z,6E)-3-hydroxy-7-(4-hydroxy-3-methoxyphenyl)-5-oxohepta-1,3,6-trien-1-yl)-2-methoxyphenyl 4-nitrobenzoate (2), a novel curcumin ester was synthesized. The molecular structure and spectroscopic analysis were performed using experimental techniques like FT-IR, 1H,13C NMR, mass and UV-visible as well as theoretical calculations. The theoretical calculations were done by DFT level of theory using B3LYP/6-31G (d,p) basis set. The vibrational wavenumbers were calculated using DFT method and assigned with the help of potential energy distribution (PED). The electronic properties such as frontier orbitals and band gap energies have been calculated using time dependent density functional theory (TD-DFT). The strength and nature of weak intramolecular interactions have been studied by AIM approach. Global and local reactivity descriptors have been computed to predict reactivity and reactive sites in the molecule. First hyperpolarizability values have been calculated to describe the nonlinear optical (NLO) property of the synthesized compounds. Molecular electrostatic potential (MEP) analysis has also been carried out. The anti-hepatic cancer activity of compound 2 was also carried out.

  6. Beta-decay asymmetries in polarized /sup 12/B and /sup 12/N and the G-parity non-conservation

    Energy Technology Data Exchange (ETDEWEB)

    Sugimoto, K [Osaka Univ., Toyonaka (Japan). Dept. of Physics

    1976-07-01

    The decay asymmetries (A) in polarized /sup 12/B and /sup 12/N have been measured as a function of ..beta..-ray energies (E). The coefficients ..cap alpha..sub(-+) in A = -+ P(p/E) (1 + ..cap alpha..sub(-+)E)) have been determined to be ..cap alpha..sub(-) (/sup 12/B) = +(0.31+-0.06)%/MeV and ..cap alpha..sub(+) (/sup 12/N) = -(0.21+-0.07)%/MeV. The experimental value, ..cap alpha..sub(-) - ..cap alpha..sub (+) = (0.52+-0.09)%/MeV, is larger than the prediction according to conservation of vector current which includes no second-class current, (..cap alpha..sub(-) - ..cap alpha..sub(+) CVC approximately equal to 0.27%/MeV, and indicates the existence of the second-class induced-tensor current.

  7. Some results for the exponential interaction in two or more dimensions

    Energy Technology Data Exchange (ETDEWEB)

    Albeverio, S; Gallavotti, G; Hoegh-Krohn, R [Bielefeld Univ. (Germany, F.R.). Fakultaet fuer Mathematik; Oslo Univ. (Norway). Matematisk Institutt; Rome Univ. (Italy). Istituto di Matematica)

    1979-12-01

    We show that for the regularized exponential interaction lambda e/sup ..cap alpha..phi/: in d space-time dimensions the Schwinger functions converge to the Schwinger functions for the free field if d > 2 for all ..cap alpha.. or if d = 2 for all ..cap alpha.. such that /..cap alpha../ > ..cap alpha../sub 0/.

  8. Synthesis of new series of 3-hydroxy/acetoxy-2-phenyl-4H-chromen ...

    Indian Academy of Sciences (India)

    Abstract. 3-Hydroxy-2-aryl/heteroaryl-4H-chromones 4(a–n) were synthesized from appropriate chalcones. 3(a–n) and acetylated to afford the corresponding acetoxy derivatives 5(a–n). All compounds were evalu- ated for antimicrobial activity against Staphylococus aureus, Bacillus subtillis, Escherichia coli and Pseu-.

  9. Complete 1H and 13C NMR assignments and anti fungal activity of two 8-hydroxy flavonoids in mixture

    International Nuclear Information System (INIS)

    Johann, Susana; Smania Junior, Artur; Branco, Alexsandro

    2007-01-01

    A mixture of the two new flavonols 8-hydroxy-3, 4', 5, 6, 7-pentamethoxyflavone (1) and 8-hydroxy-3, 3', 4', 5, 6, 7-hexamethoxyflavone (2) was isolated from a commercial sample of Citrus aurantifolia. An array of one- ( 1 H NMR, { 1 H} -13 C NMR, and APT -13 C NMR) and two-dimensional NMR techniques (COSY, NOESY, HMQC and HMBC) was used to achieve the structural elucidation and the complete 1 H and 13 C chemical shift assignments of these natural compounds. In addition, the antifungal activity of these compounds against phytopathogenic and human pathogenic fungi was investigated. (author)

  10. Estimated release from the saltstone landfill effect of landfill caps and landfill-cap/monolith-liner combinations

    International Nuclear Information System (INIS)

    Wilhite, E.L.

    1985-01-01

    The effect of capping the entire saltstone landfill is dependent on the effectiveness of the clay cap in preventing infiltration. A cap that is 99% effective will reduce releases from the saltstone landfill by a factor of 7.7. Several combinations of landfill design alterations will result in meeting ground water standards

  11. Production of hydroxy marilone C as a bioactive compound from

    Directory of Open Access Journals (Sweden)

    Osama H. El Sayed

    2016-06-01

    Full Text Available Hydroxy marilone C is a bioactive metabolite produced from the culture broth of Streptomyces badius isolated from Egyptian soil. Hydroxy marilone C was purified and fractionated by a silica gel column with a gradient mobile phase dichloromethane (DCM:methanol then Sephadex LH-20 column using methanol as a mobile phase. It was subjected to many procedures such as infrared (IR, nuclear magnetic resonance (NMR, Mass spectroscopy (MS and UV spectroscopy for elucidation of its structure. It was evaluated for antioxidant, cytotoxicity against human alveolar basal epithelial cell line (A-549 and human breast adenocarcinoma cell line (MCF-7 and antiviral activities; showed that the maximum antioxidant activity was 78.8% at 3 mg/ml after 90 min. and the IC50 value against DPPH radical found about 1.5 mg/ml after 60 min. Using MTT assay the effect of the pure compound on the proliferation of A-549 cells and MCF-7 cells was 443 μg/ml and 147.9 μg/ml, respectively, while for detection of antiviral activity using Madin–Darby canine kidney (MDCK cells the maximum cytotoxicity was at 27.9% and IC50 was 128.1 μg/ml. The maximum concentration required for protecting 50% of the virus-infected cells against H1N1 viral cytopathogenicity (EC50 was 33.25% for 80 μg/ml. These results indicated that the hydroxy marilone C has potential antitumor and antiviral activities.

  12. [Studies on the flavonoids from Dendranthema lavandulifolium].

    Science.gov (United States)

    Shen, Y X; Quan, L H; Guan, L; Chen, J M

    1997-06-01

    From the whole plant of Dendranthema lavandulifolium, two flavonoides (I, II) and two flavone glycosides (III, IV) were isolated. They were identified as luteolin (I), apigenin (II), 5-hydroxy-4'-methoxy-flavone-7-O-alpha-L-rhamnopyranosyl(1-->6)-beta- D-glucopyranosyl (acaciin III) and 5-hydroxy-4'-methoxy-flavone-7-O-alpha-L-rhamnopyranosyl (1-->6) [2-O-acetyl-beta-D-glucopyranosyl(1-->2)]-beta-D-glucopyranoside (IV) by means of IR, UV, 1H-NMR, 13C-NMR, EI-MS, HRFAB, etc. Among these four compounds, I, II were isolated for the first time from this plant, IV is a new compound.

  13. Structure of a two-CAP-domain protein from the human hookworm parasite Necator americanus

    Energy Technology Data Exchange (ETDEWEB)

    Asojo, Oluwatoyin A., E-mail: oasojo@unmc.edu [Pathology and Microbiology Department, 986495 Nebraska Medical Center, Omaha, NE 68198-6495 (United States)

    2011-05-01

    The first structure of a two-CAP-domain protein, Na-ASP-1, from the major human hookworm parasite N. americanus refined to a resolution limit of 2.2 Å is presented. Major proteins secreted by the infective larval stage hookworms upon host entry include Ancylostoma secreted proteins (ASPs), which are characterized by one or two CAP (cysteine-rich secretory protein/antigen 5/pathogenesis related-1) domains. The CAP domain has been reported in diverse phylogenetically unrelated proteins, but has no confirmed function. The first structure of a two-CAP-domain protein, Na-ASP-1, from the major human hookworm parasite Necator americanus was refined to a resolution limit of 2.2 Å. The structure was solved by molecular replacement (MR) using Na-ASP-2, a one-CAP-domain ASP, as the search model. The correct MR solution could only be obtained by truncating the polyalanine model of Na-ASP-2 and removing several loops. The structure reveals two CAP domains linked by an extended loop. Overall, the carboxyl-terminal CAP domain is more similar to Na-ASP-2 than to the amino-terminal CAP domain. A large central cavity extends from the amino-terminal CAP domain to the carboxyl-terminal CAP domain, encompassing the putative CAP-binding cavity. The putative CAP-binding cavity is a characteristic cavity in the carboxyl-terminal CAP domain that contains a His and Glu pair. These residues are conserved in all single-CAP-domain proteins, but are absent in the amino-terminal CAP domain. The conserved His residues are oriented such that they appear to be capable of directly coordinating a zinc ion as observed for CAP proteins from reptile venoms. This first structure of a two-CAP-domain ASP can serve as a template for homology modeling of other two-CAP-domain proteins.

  14. Structure of a two-CAP-domain protein from the human hookworm parasite Necator americanus

    International Nuclear Information System (INIS)

    Asojo, Oluwatoyin A.

    2011-01-01

    The first structure of a two-CAP-domain protein, Na-ASP-1, from the major human hookworm parasite N. americanus refined to a resolution limit of 2.2 Å is presented. Major proteins secreted by the infective larval stage hookworms upon host entry include Ancylostoma secreted proteins (ASPs), which are characterized by one or two CAP (cysteine-rich secretory protein/antigen 5/pathogenesis related-1) domains. The CAP domain has been reported in diverse phylogenetically unrelated proteins, but has no confirmed function. The first structure of a two-CAP-domain protein, Na-ASP-1, from the major human hookworm parasite Necator americanus was refined to a resolution limit of 2.2 Å. The structure was solved by molecular replacement (MR) using Na-ASP-2, a one-CAP-domain ASP, as the search model. The correct MR solution could only be obtained by truncating the polyalanine model of Na-ASP-2 and removing several loops. The structure reveals two CAP domains linked by an extended loop. Overall, the carboxyl-terminal CAP domain is more similar to Na-ASP-2 than to the amino-terminal CAP domain. A large central cavity extends from the amino-terminal CAP domain to the carboxyl-terminal CAP domain, encompassing the putative CAP-binding cavity. The putative CAP-binding cavity is a characteristic cavity in the carboxyl-terminal CAP domain that contains a His and Glu pair. These residues are conserved in all single-CAP-domain proteins, but are absent in the amino-terminal CAP domain. The conserved His residues are oriented such that they appear to be capable of directly coordinating a zinc ion as observed for CAP proteins from reptile venoms. This first structure of a two-CAP-domain ASP can serve as a template for homology modeling of other two-CAP-domain proteins

  15. Preparation and characterization of highly water-soluble magnetic Fe{sub 3}O{sub 4} nanoparticles via surface double-layered self-assembly method of sodium alpha-olefin sulfonate

    Energy Technology Data Exchange (ETDEWEB)

    Li, Honghong; Qin, Li [School of Chemistry and Chemical Engineering, University of Jinan, Jinan 250022 (China); Feng, Ying [Department of Bridge Engineering, Shanxi Railway Institute, Weinan 714000 (China); Hu, Lihua [School of Chemistry and Chemical Engineering, University of Jinan, Jinan 250022 (China); Zhou, Chunhua, E-mail: chm_zhouch@ujn.edu.cn [School of Chemistry and Chemical Engineering, University of Jinan, Jinan 250022 (China)

    2015-06-15

    A kind of double-layered self-assembly sodium alpha-olefin sulfonate (AOS) capped Fe{sub 3}O{sub 4} magnetic nanoparticles (Fe{sub 3}O{sub 4}-AOS-MN) with highly water-solubility was prepared by a wet co-precipitation method with a pH of 4.8. The resulting Fe{sub 3}O{sub 4}-AOS-MN could be dispersed into water to form stable magnetic fluid without other treatments. The result of X-ray diffraction (XRD) indicated that the Fe{sub 3}O{sub 4}-AOS-MN maintained original crystalline structure and exhibited a diameter of about 7.5 nm. The iron oxide phase of nanoparticles determined by Raman spectroscopy is Fe{sub 3}O{sub 4}. Transmission electron microscopy (TEM) analysis confirmed that the Fe{sub 3}O{sub 4}-AOS-MN with spherical morphology were uniformly dispersed in water. FT-IR spectroscopy (FT-IR) and thermo-gravimetric analysis (TGA) verified the successful preparation of Fe{sub 3}O{sub 4}-AOS-MN capped with double-layered self-assembled AOS. The corresponding capacities of monolayer chemical absorption and the second-layer self-assembly absorption were respectively 4.07 and 14.71 wt% of Fe{sub 3}O{sub 4}-MN, which were much lower than those of other surfactants. Vibrating sample magnetometer (VSM) test result showed Fe{sub 3}O{sub 4}-AOS-MN possessed superparamagnetic behavior with the saturation magnetization value of about 44.45 emu/g. The blocking temperature T{sub B} of Fe{sub 3}O{sub 4}-AOS-MN capped with double-layered AOS is 170 K. - Highlights: • Double-layered self-assembly sodium alpha-olefin sulfonate (AOS) capped Fe{sub 3}O{sub 4} magnetic nanoparticles are prepared by a wet co-precipitation method. • Double-layered Fe{sub 3}O{sub 4}-AOS-MN exhibits highly water-solubility. • The iron oxide phase is determined by Raman spectroscopy. • Fe{sub 3}O{sub 4}-AOS-MN capped with double-layered AOS possesses super-paramagnetic behavior. • The blocking temperature T{sub B} of Fe{sub 3}O{sub 4}-AOS-MN capped with double-layered AOS is 170 K.

  16. Evaluation of accuracy and uncertainty of ELISA assays for the determination of interleukin-4, interleukin-5, interferon-gamma and tumor necrosis factor-alpha

    DEFF Research Database (Denmark)

    Borg, Lone; Kristiansen, Jesper; Christensen, Jytte M

    2002-01-01

    . However, models for establishing the traceability and uncertainty of immunoassay results are lacking. Sandwich enzyme-linked immunosorbent assays (ELISAs) were developed for determination of the human cytokines interleukin-4 (IL-4), interleukin-5 (IL-5), interferon-y (IFN-gamma) and tumor necrosis factor-alpha...... (TNF-alpha). The accuracy of each of the assays was evaluated in the ranges of 1-15 microg/l (IL-4), 0.001-1 microg/l (IL-5), 0.5-2.5 microg/l (IFN-T) and 0.14-2.2 microg/l (TNF-alpha). Other evaluated performance characteristics were the limit of detection (LOD), immunological specificity......) of the assessed ELISAs was found to be in the range of 11-18%, except for IL-5 where RSDA increased at decreasing concentrations. The LOD was 0.12 microg/l, 0.0077 microg/l, 0.0069 microg/l and 0.0063 microg/l for IL-4, IL-5, IFN-gamma and TNF-alpha, respectively. Traceability to the WHO IS was established...

  17. Elevation Changes of Ice Caps in the Canadian Arctic Archipelago

    Science.gov (United States)

    Abdalati, W.; Krabill, W.; Frederick, E.; Manizade, S.; Martin, C.; Sonntag, J.; Swift, R.; Thomas, R.; Yungel, J.; Koerner, R.

    2004-01-01

    Precise repeat airborne laser surveys were conducted over the major ice caps in the Canadian Arctic Archipelago in the spring of 1995 and 2000 in order to measure elevation changes in the region. Our measurements reveal thinning at lower elevations (below 1600 m) on most of the ice caps and glaciers, but either very little change or thickening at higher elevations in the ice cap accumulation zones. Recent increases in precipitation in the area can account for the slight thickening where it was observed, but not for the thinning at lower elevations. For the northern ice caps on the Queen Elizabeth Islands, thinning was generally less than 0.5 m/yr , which is consistent with what would be expected from the warm temperature anomalies in the region for the 5-year period between surveys and appears to be a continuation of a trend that began in the mid 1980s. Further south, however, on the Barnes and Penny ice caps on Baffin Island, this thinning was much more pronounced at over 1 m/yr in the lower elevations. Here temperature anomalies were very small, and the thinning at low elevations far exceeds any associated enhanced ablation. The observations on Barnes, and perhaps Penny are consistent with the idea that the observed thinning is part of a much longer term deglaciation, as has been previously suggested for Barnes Ice Cap. Based on the regional relationships between elevation and elevation-change in our data, the 1995-2000 mass balance for the region is estimated to be 25 cu km/yr of ice, which corresponds to a sea level increase of 0.064 mm/ yr . This places it among the more significant sources of eustatic sea level rise, though not as substantial as Greenland ice sheet, Alaskan glaciers, or the Patagonian ice fields.

  18. Development of a fully automated sequential injection solid-phase extraction procedure coupled to liquid chromatography to determine free 2-hydroxy-4-methoxybenzophenone and 2-hydroxy-4-methoxybenzophenone-5-sulphonic acid in human urine.

    Science.gov (United States)

    León, Zacarías; Chisvert, Alberto; Balaguer, Angel; Salvador, Amparo

    2010-04-07

    2-Hydroxy-4-methoxybenzophenone and 2-hydroxy-4-methoxybenzophenone-5-sulphonic acid, commonly known as benzophenone-3 (BZ3) and benzophenone-4 (BZ4), respectively, are substances widely used as UV filters in cosmetic products in order to absorb UV radiation and protect human skin from direct exposure to the deleterious wavelengths of sunlight. As with other UV filters, there is evidence of their percutaneous absorption. This work describes an analytical method developed to determine trace levels of free BZ3 and BZ4 in human urine. The methodology is based on a solid-phase extraction (SPE) procedure for clean-up and pre-concentration, followed by the monitoring of the UV filters by liquid chromatography-ultraviolet spectrophotometry detection (LC-UV). In order to improve not only the sensitivity and selectivity, but also the precision of the method, the principle of sequential injection analysis was used to automate the SPE process and to transfer the eluates from the SPE to the LC system. The application of a six-channel valve as an interface for the switching arrangements successfully allowed the on-line connection of SPE sample processing with LC analysis. The SPE process for BZ3 and BZ4 was performed using octadecyl (C18) and diethylaminopropyl (DEA) modified silica microcolumns, respectively, in which the analytes were retained and eluted selectively. Due to the matrix effects, the determination was based on standard addition quantification and was fully validated. The relative standard deviations of the results were 13% and 6% for BZ3 and BZ4, respectively, whereas the limits of detection were 60 and 30 ng mL(-1), respectively. The method was satisfactorily applied to determine BZ3 and BZ4 in urine from volunteers that had applied a sunscreen cosmetic containing both UV filters. Copyright 2010 Elsevier B.V. All rights reserved.

  19. Development of a fully automated sequential injection solid-phase extraction procedure coupled to liquid chromatography to determine free 2-hydroxy-4-methoxybenzophenone and 2-hydroxy-4-methoxybenzophenone-5-sulphonic acid in human urine

    International Nuclear Information System (INIS)

    Leon, Zacarias; Chisvert, Alberto; Balaguer, Angel; Salvador, Amparo

    2010-01-01

    2-Hydroxy-4-methoxybenzophenone and 2-hydroxy-4-methoxybenzophenone-5-sulphonic acid, commonly known as benzophenone-3 (BZ3) and benzophenone-4 (BZ4), respectively, are substances widely used as UV filters in cosmetic products in order to absorb UV radiation and protect human skin from direct exposure to the deleterious wavelengths of sunlight. As with other UV filters, there is evidence of their percutaneous absorption. This work describes an analytical method developed to determine trace levels of free BZ3 and BZ4 in human urine. The methodology is based on a solid-phase extraction (SPE) procedure for clean-up and pre-concentration, followed by the monitoring of the UV filters by liquid chromatography-ultraviolet spectrophotometry detection (LC-UV). In order to improve not only the sensitivity and selectivity, but also the precision of the method, the principle of sequential injection analysis was used to automate the SPE process and to transfer the eluates from the SPE to the LC system. The application of a six-channel valve as an interface for the switching arrangements successfully allowed the on-line connection of SPE sample processing with LC analysis. The SPE process for BZ3 and BZ4 was performed using octadecyl (C18) and diethylaminopropyl (DEA) modified silica microcolumns, respectively, in which the analytes were retained and eluted selectively. Due to the matrix effects, the determination was based on standard addition quantification and was fully validated. The relative standard deviations of the results were 13% and 6% for BZ3 and BZ4, respectively, whereas the limits of detection were 60 and 30 ng mL -1 , respectively. The method was satisfactorily applied to determine BZ3 and BZ4 in urine from volunteers that had applied a sunscreen cosmetic containing both UV filters.

  20. Tautomerism of 4-hydroxy-2,5-dimethyl-3(2H)-furanone: evidence for its enantioselective biosynthesis.

    Science.gov (United States)

    Raab, Thomas; Hauck, Tobias; Knecht, Anja; Schmitt, Ulrich; Holzgrabe, Ulrike; Schwab, Wilfried

    2003-08-01

    Chiral natural flavor compounds exhibit characteristic enantiomeric excesses due to stereoselective, enzymatically catalyzed reactions during biogenesis. Although the enzymatic formation of the strawberry key flavor compound 4-hydroxy-2,5-dimethyl-3(2H)-furanone (HDMF; Furaneol(R)) is anticipated, the naturally occurring compound is racemic. As racemization due to keto-enol-tautomerism of HDMF could account for this observation, HDMF was investigated by (1)H-NMR spectroscopy tracing the exchange of the proton bound to the furanone-ring at C2 with deuteron from the medium (D(2)O). In addition, the racemization rate of HDMF was directly determined by cyclodextrin-modified capillary electrophoresis of enantiomerically enriched HDMF stored at different pH values. Tautomerism and the racemization rate of HDMF was lowest at pH values between 4 and 5. However, tautomerism and thus racemization was catalyzed under stronger acidic conditions (pH 2) and especially at pH values greater than 7, the value published for plant cell cytosol. Approximately 50% of the protons at C2 were exchanged with deuteron within 1 h at pH 7.2. Therefore, in order to demonstrate the enzymatic formation of HDMF, incubation experiments with Zygosaccharomyces rouxii as well as strawberry protein extract were carried out under slightly acidic conditions (pH 5), the most suitable pH value for studies on the enantiomeric ratio of HDMF. In both experiments the formation of enantiomerically enriched HDMF could be demonstrated for the first time, whereas incubation experiments under neutral conditions resulted in the detection of racemic HDMF. Copyright 2003 Wiley-Liss, Inc.

  1. Applications of hydroxy acids: classification, mechanisms, and photoactivity

    Directory of Open Access Journals (Sweden)

    Andrija Kornhauser

    2010-11-01

    Full Text Available Andrija Kornhauser1, Sergio G Coelho2, Vincent J Hearing21US Food and Drug Administration [retired], Annandale, VA, USA; 2Laboratory of Cell Biology, National Cancer Institute, National Institutes of Health, Bethesda, MD, USAAbstract: Hydroxy acids (HAs represent a class of compounds which have been widely used in a number of cosmetic and therapeutic formulations in order to achieve a variety of beneficial effects for the skin. We review and discuss the most frequently used classes of these compounds, such as a-hydroxy acids, β-hydroxy acids, polyhydroxy acids, and bionic acids, and describe their applications as cosmetic and therapeutic agents. Special emphasis is devoted to the safety evaluation of these formulations, in particular on the effects of their prolonged use on sun-exposed skin. Furthermore, we summarize the very limited number of studies dealing with the modifications evoked by topical application of products containing HAs on photocarcinogenesis. In spite of the large number of reports on the cosmetic and clinical effects of HAs, their biological mechanism(s of action still require more clarification. Some of these mechanisms are discussed in this article along with important findings on the effect of HAs on melanogenesis and on tanning. We also emphasize the important contribution of cosmetic vehicles in these types of studies. Thus, HAs play an important role in cosmetic formulations, as well as in many dermatologic applications, such as in treating photoaging, acne, ichthyosis, rosacea, pigmentation disorders, and psoriasis.Keywords: hydroxy acids, glycolic acid, salicylic acid, UV, erythema, cosmetics

  2. Biosynthesis of 4-hydroxy-2,5-dimethyl-3(2H)-furanone and derivatives in in vitro grown strawberries.

    Science.gov (United States)

    Pérez, A G; Olías, R; Olías, J M; Sanz, C

    1999-02-01

    The biosynthesis of 2,5-dimethyl-4-hydroxy-3(2H)-furanone (Furaneol) and its methyl ether and glucoside derivatives has been studied in strawberries. An in vitro system was used for growing this fruit, showing that the presence in the incubation medium of sucrose or hydroxyquinoline hemisulfate has no effect on the bioformation of these compounds. Strawberries in vitro grown showed an increase in furanone content with time, especially between the second and fourth days, to the same extent as field-grown fruits but at a higher rate. Among the precursors added to the incubation medium, D-fructose gave rise to an increase in furaneol and its glucoside derivative of 42. 6% and 26.3%, respectively. D-fructose 6-phosphate seems to be the precursor of furaneol in strawberries since, when present in the incubation medium, it produced an average increase of 125% in all furanones contents with respect to control fruits.

  3. Conformational and vibrational analysis of 5-hydroxy 2-nitrobenzaldehyde by AB initio hartree-fock, density functional theory calculations

    International Nuclear Information System (INIS)

    Cinakli, S.; Sert, Y.; Boeyuekata, M.; Ucun, F.

    2010-01-01

    The vibrational spectra of benzaldehyde and its derivatives have been studied earlier. The substitution of a functional group changes the spectra markedly. Recent spectroscopic studies of the benzaldehyde and their derivatives have been motivated because the vibrational spectra are very useful for understanding of specific biological process and in the analysis of relatively complex systems. The optimized molecular structure, vibrational frequencies and corresponding vibrational assignments, the total energy calculations, relative energies, the mean vibrational deviations of the two planar O-cis and O-trans roomers of 5-Hydroxy 2-nitrobenzaldehydes have been calculated using ab initio Hartree Fock (HF) and Density Functional Theory (B3LYP) with 6-311++G(d,p) basis set. All computations have been performed on personal computer using the Gaussian 03 program package. The calculations were adapted to Cs symmetries of all the molecules. The O-trans rotomers with lower energy of all the molecules have been found as preferential rotomers in the ground state.

  4. Human skeletal uptake of natural alpha radioactivity from 210Pb-supported 210Po

    International Nuclear Information System (INIS)

    Oyedepo, A.C.

    1998-06-01

    This thesis contributes to increasing knowledge on the dosimetry of natural alpha-particle radiation in skeletal tissues, particularly in utero, and associated risks of malignancy. Alpha-particle radiation is an established aetiological factor of cancer. In the human body, polonium-210 decayed from skeletal lead-210 ( 210 Pb/ 210 Po) is the predominant natural alpha-emitter. 210 Pb displaces calcium (Ca) in mineral hydroxyapatite, especially during periods of rapid bone growth and remodelling when Ca is laid down. It was therefore necessary to study alpha activity uptake and calcification concurrently within bone. Human studies were undertaken on: fetal vertebrae, 17 - 42 weeks of gestation, 74 samples; adult vertebrae, 40 - 95 years, 40 samples; and adult ribs, 20 - 95 years, 51 samples. Specimens were unconcentrated and weighed 210 Pb/ 210 Po. Alpha track data were resolved by specially written software named SPATS (Selection Program for Analysing Track Structures). Ca and phosphorus (P) were biochemically determined. Results were examined for trends in bone type, gender and chronological ageing in humans. The main research findings were: 1) The Ca content of fetal vertebrae increased linearly at a weekly rate of 0.2g Ca 100 g -1 wet bone (typical values of 2, 4, 6 g 100 g -1 at 16, 26 and 36 weeks). 2) The P concentration also increased with advancing fetal age. 3) The Ca:P bone weight ratio rose from 1.7 to 2.2 by 32 gestational weeks. 4) The overall range in bone 210 Pb/ 210 Po alpha activity was 0.25 - 1.1 Bq kg -1 with correlation between activity concentration and fetal age (0.47 ± 0.05 Bq kg -1 for 17 - 26 weeks, 0.67 ± 0.04 Bq kg -1 for 32 - 42 weeks). 5) The correlation between increased alpha radioactivity and increased Ca concentration approximating to 0.0046 Bq g -1 of Ca. 6) A decreasing Ca content of adult vertebrae with increasing age from 40 - 95 years, from ∼ 14 to 5 g 100 g-1, but no correlation with age for adult rib Ca content of 10 - 30 g

  5. Combination of interferon-alpha and 5-fluorouracil inhibits endothelial cell growth directly and by regulation of angiogenic factors released by tumor cells

    International Nuclear Information System (INIS)

    Wada, Hiroshi; Tanemura, Masahiro; Umeshita, Koji; Doki, Yuichiro; Mori, Masaki; Nagano, Hiroaki; Yamamoto, Hirofumi; Noda, Takehiro; Murakami, Masahiro; Kobayashi, Shogo; Marubashi, Shigeru; Eguchi, Hidetoshi; Takeda, Yutaka

    2009-01-01

    The combination therapy of interferon (IFN)-alpha and 5-fluorouracil (5-FU) improved the prognosis of the patients with hepatocellular carcinoma (HCC). To determine the molecular mechanisms of the anti-tumor and anti-angiogenic effects, we examined the direct anti-proliferative effects on human umbilical vein endothelial cells (HUVEC) and indirect effects by regulating secretion of angiogenic factors from HCC cells. The direct effects on HUVEC were examined by TUNEL, Annexin-V assays and cell cycles analysis. For analysis of the indirect effects, the apoptosis induced by the conditioned medium from HCC cell treated by IFN-alpha/5-FU and expression of angiogenic factors was examined. IFN-alpha and 5-FU alone had anti-proliferative properties on HUVEC and their combination significantly inhibited the growth (compared with control, 5-FU or IFN alone). TUNEL and Annexin-V assays showed no apoptosis. Cell cycle analysis revealed that IFN-alpha and 5-FU delayed cell cycle progression in HUVEC with S-phase accumulation. The conditioned medium from HuH-7 cells after treatment with IFN/5-FU significantly inhibited HUVEC growth and induced apoptosis, and contained high levels of angiopoietin (Ang)-1 and low levels of vascular endothelial growth factor (VEGF) and Ang-2. Knockdown of Ang-1 in HuH-7 cells abrogated the anti-proliferative effects on HUVEC while knockdown of Ang-2 partially rescue the cells. These results suggested that IFN-alpha and 5-FU had direct growth inhibitory effects on endothelial cells, as well as anti-angiogenic effects through regulation of angiogenic factors released from HCC cells. Modulation of VEGF and Angs secretion by IFN-alpha and 5-FU may contribute to their anti-angiogenic and anti-tumor effects on HCC

  6. Alpha-particle emission probabilities of ²³⁶U obtained by alpha spectrometry.

    Science.gov (United States)

    Marouli, M; Pommé, S; Jobbágy, V; Van Ammel, R; Paepen, J; Stroh, H; Benedik, L

    2014-05-01

    High-resolution alpha-particle spectrometry was performed with an ion-implanted silicon detector in vacuum on a homogeneously electrodeposited (236)U source. The source was measured at different solid angles subtended by the detector, varying between 0.8% and 2.4% of 4π sr, to assess the influence of coincidental detection of alpha-particles and conversion electrons on the measured alpha-particle emission probabilities. Additional measurements were performed using a bending magnet to eliminate conversion electrons, the results of which coincide with normal measurements extrapolated to an infinitely small solid angle. The measured alpha emission probabilities for the three main peaks - 74.20 (5)%, 25.68 (5)% and 0.123 (5)%, respectively - are consistent with literature data, but their precision has been improved by at least one order of magnitude in this work. © 2013 Published by Elsevier Ltd.

  7. Central Air-Conditioning Plant (CAP) extension

    International Nuclear Information System (INIS)

    Shetty, P.S.; Kaul, S.K.; Mishra, H.

    2017-01-01

    Central Air-Conditioning Plant (CAP) and its associated chilled water network of BARC is one among the largest central plants in India for such application. The plant was planned in 1960s to cater to the air-conditioning and process water requirements of laboratories, workshops and buildings spread over a distance of 1.5 Km in three directions from CAP through underground network of chilled water pipelines. The plant was designed for a total capacity of 6600 TR. The present installed capacity of the plant is 7250 TR. The connected load at present is 9800 TR. After the XII plan capacity will be augmented to 7650 TR. The connected load is expected to cross 11,000 TR after the commissioning of new Engg. Halls 9, 10 and 11

  8. ATLAS electromagnetic end-cap detector

    CERN Multimedia

    Maximilien Brice

    2003-01-01

    After the insertion of the first end-cap into this cryostat, the team proceed to the wiring operations. Millions of wires are connected to the electromagnetic calorimeter on this end-cap, whch must be carefully fed out from the detector so that data can be read out. The energy of photons, electrons and positrons will be measured as they pass through the end-cap having been created along the line of the beams in the proton-proton collisions.

  9. ATLAS end-cap detector

    CERN Multimedia

    Maximilien Brice

    2003-01-01

    Three scientists from the Institute of Nuclear Phyiscs at Novossibirsk with one of the end-caps of the ATLAS detector. The end-caps will be used to detect particles produced in the proton-proton collisions at the heart of the ATLAS experiment that are travelling close to the axis of the two beams.

  10. Lyman-alpha detector designed for rocket measurements of the direct solar radiation at 121.5 nm

    International Nuclear Information System (INIS)

    Guineva, V.; Tashev, V.; Witt, G.; Gumbel, J.; Khaplanov, M.

    2007-01-01

    Rocket measurements of the direct Lyman-alpha radiation penetrating in the atmosphere were planned during the HotPay I rocket experiment, June 2006, Project ASLAF (Attenuation of the Solar Lyman-Alpha Flux), Andoya Rocket Range (ARR), Norway. The basic goal of ASLAF project was the study of the processes in the summer mesosphere and thermosphere (up to 110 km), at high latitudes using the Lyman-alpha measurements. The resonance transition 2 P- 2 S of the atomic hydrogen (Lyman-alpha emission) is the strongest and most conspicuous feature in the solar EUV spectrum. Due to the favourable circumstance, that the Lyman-alpha wavelength (121.5 nm) coincides with a minimum of the O 2 absorption spectrum, the direct Lyman-alpha radiation penetrates well in the mesosphere. The Lyman-alpha radiation is the basic agent of the NO molecules ionization, thus generating the ionospheric D-layer, and of the water vapour photolysis, being one of the main H 2 O loss processes. The Lyman-alpha radiation transfer depends on the resonance scattering from the hydrogen atoms in the atmosphere and on the O 2 absorption. Since the Lyman-alpha extinction in the atmosphere is a measure for the column density of the oxygen molecules, the atmospheric temperature profile can be calculated thereof. The detector of solar Lyman-alpha radiation was manufactured in the Stara Zagora Department of the Solar-Terrestrial Influences Laboratory (STIL). Its basic part is an ionization chamber, filled in with NO. A 60 V power supply is applied to the chamber. The produced photoelectric current from the sensor is fed to a 2-channels amplifier, providing an analogue signal. The characteristics of the Lyman-alpha detector were studied. It passed successfully all tests and the results showed that the instrument could be used in rocket experiments to measure the Lyman-alpha flux. From the measurements of the detector, the Lyman-alpha vertical profile can be obtained. The forthcoming scientific data analysis will

  11. 4-Hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[4-(trifluoromethylphenyl]-1,2-dihydroquinoline-3-carboxamide

    Directory of Open Access Journals (Sweden)

    Emmanuel S. Akinboye

    2014-03-01

    Full Text Available The title compound, C20H17F3N2O4, named tasquinimod, is a second-generation oral quinoline-3-carboxamide analogue, which is currently in phase III clinical trials for the treatment of metastatic prostate cancer. The quinoline unit is almost planar (r.m.s. deviation of fitted atoms = 0.0075 Å. The carboxamide side chain, substituted at position 3, is tilted by 88.07 (7° to the quinoline plane. Both the methyl and carbonyl groups of this carboxamide side chain are in a syn conformation. The 4-(trifluoromethylphenyl plane is inclined at 50.62 (17° to the plane of the carboxamide side chain, and at 87.14 (4° to the plane of the quinoline ring system. The 4-hydroxy H atom acts as a double proton donor in an intramolecular hydrogen bond to the 5-position methoxy O atom and in an intermolecular contact to the 2-oxo group, generating a chain along [010] in the crystal structure.

  12. Development of a routine method for the determination of mean crystallite dimensions in nuclear materials by X-ray diffraction line broadening. An application example using U/sub 3/O/sub 8/ microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Imakuma, K; Sato, I M; Cretella Neto, J; Costa, M I

    1975-03-01

    A method for mean crystallite size determination by X-ray diffraction line broadening was established. Both step-scanning and methods were extensivly tested and the precision of the data obtained as a function of the crystallite size is discussed. Emphasis is given to our contribution in order to eliminate instrumental effects as well as K sub(..cap alpha../sub 1/)/Ksub(..cap alpha../sub 2/) doublet effect upon line broadening. Instrumental correction was performed with a monocrystalline Si sample having mean crystallite size well above 13,000 A improving the accuracy of experimental data. Ksub(..cap alpha../sub 2/) and Ksub(..cap alpha../sub 2/) peaks determined instead of taking it for granted as 5. The mean crystallite dimension of U/sub 3/O/sub 8/ was calculated and the results show the dependence of this parameter on the quality of the microspheres.

  13. [CAP quality management system in clinical laboratory and its issue].

    Science.gov (United States)

    Tazawa, Hiromitsu

    2004-03-01

    The CAP (College of American Pathologists) was established in 1962 and, at present, CAP-accredited laboratories include about 6000 institutions all over the world, mainly in the U.S. The essential purpose of CAP accreditation is high quality reservation and improvement of clinical laboratory services for patient care, and is based on seven points, listed below. (1) Establishment of a laboratory management program and laboratory techniques to assure accuracy and improve overall quality of laboratory services. (2) Maintenance and improvement of accuracy objectively by centering on a CAP survey. (3) Thoroughness in safety and health administration. (4) Reservation of the performance of laboratory services by personnel and proficiency management. (5) Provision of appropriate information to physicians, and contribution to improved quality of patient care by close communication with physicians (improvement in patient care). (6) Reduction of running costs and personnel costs based on evidence by employing the above-mentioned criteria. (7) Reduction of laboratory error. In the future, accreditation and/or certification by organizations such as CAP, ISO, etc., may become a requirement for providing any clinical laboratory services in Japan. Taking the essence of the CAP and the characteristics of the new international standard, ISO151589, into consideration, it is important to choose the best suited accreditation and/or certification depending of the purpose of clinical laboratory.

  14. The projected demise of Barnes Ice Cap: Evidence of an unusually warm 21st century Arctic

    Science.gov (United States)

    Gilbert, A.; Flowers, G. E.; Miller, G. H.; Refsnider, K. A.; Young, N. E.; Radić, V.

    2017-03-01

    As a remnant of the Laurentide Ice Sheet, Barnes Ice Cap owes its existence and present form in part to the climate of the last glacial period. The ice cap has been sustained in the present interglacial climate by its own topography through the mass balance-elevation feedback. A coupled mass balance and ice-flow model, forced by Coupled Model Intercomparison Project Phase 5 climate model output, projects that the current ice cap will likely disappear in the next 300 years. For greenhouse gas Representative Concentration Pathways of +2.6 to +8.5 Wm-2, the projected ice-cap survival times range from 150 to 530 years. Measured concentrations of cosmogenic radionuclides 10Be, 26Al, and 14C at sites exposed near the ice-cap margin suggest the pending disappearance of Barnes Ice Cap is very unusual in the last million years. The data and models together point to an exceptionally warm 21st century Arctic climate.

  15. Interaction effects between the 5-hydroxy tryptamine transporter-linked polymorphic region (5-HTTLPR) genotype and family conflict on adolescent alcohol use and misuse.

    Science.gov (United States)

    Kim, Jueun; Park, Aesoon; Glatt, Stephen J; Eckert, Tanya L; Vanable, Peter A; Scott-Sheldon, Lori A J; Carey, Kate B; Ewart, Craig K; Carey, Michael P

    2015-02-01

    To investigate whether the effects of family conflict on adolescent drinking differed as a function of 5-hydroxy tryptamine transporter-linked polymorphic region (5-HTTLPR) genotype cross-sectionally and prospectively in two independent samples of adolescents. Path analysis and multi-group analysis of two prospective datasets were conducted. United States and United Kingdom. Sample 1 was 175 adolescents in the United States (mean age = 15 at times 1 and 2 with a 6-month interval); Sample 2 was 4916 adolescents in the United Kingdon (mean age = 12 at time 1 and 15 at time 2). In both samples, demographics, tri-allelic 5-HTTLPR genotype and perceived family conflict were assessed at time 1. Alcohol use (frequency of drinking) and alcohol misuse (frequency of intoxication, frequency of drinking three or more drinks, maximum number of drinks) were assessed at times 1 and 2. A significant gene-environment interaction on alcohol misuse at time 1 was found in both sample 1 (β = 0.57, P = 0.001) and sample 2 (β = 0.19, P = 0.01), indicating that the 5-HTTLPR low-activity allele carriers exposed to higher levels of family conflict were more likely to engage in alcohol misuse than non-carriers. A significant gene-environment interaction effect on change in alcohol misuse over time was found only in sample 1 (β = 0.48, P = 0.04) but not in sample 2. Compared with non-carriers, adolescents carrying the 5-HTTLPR low-activity allele are more susceptible to the effects of family conflict on alcohol misuse. © 2014 Society for the Study of Addiction.

  16. Improvement of RVNRL film properties by adding fumed silica and hydroxy apatite

    Directory of Open Access Journals (Sweden)

    Adul Thiangchanya

    2003-01-01

    Full Text Available The effect of adding fumed silica and hydroxy apatite to Radiation Vulcanized Natural Rubber Latex (RVNRL for improving tear strength, aging properties, degradability and water-soluble protein content of rubber films has been investigated. The addition of fumed silica and hydroxy apatite in RVNRL improves tear strength and aging properties of rubber films, whereas tensile strength and degradability of rubber films were unchanged during storage at room temperature. The water-soluble protein content in rubber films was reduced by immobilization of the fumed silica and hydroxy apatite and enhanced by addition of ZnO. This may reduce allergy problems of natural rubber latex products caused by water-soluble protein. The MST of the RVNRL with fumed silica and hydroxy apatite indicated that the latex must be used within two months after mixing because of its stability.

  17. 21 CFR 884.5250 - Cervical cap.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 8 2010-04-01 2010-04-01 false Cervical cap. 884.5250 Section 884.5250 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) MEDICAL DEVICES... cap. (a) Identification. A cervical cap is a flexible cuplike receptacle that fits over the cervix to...

  18. 21 CFR 888.3000 - Bone cap.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 8 2010-04-01 2010-04-01 false Bone cap. 888.3000 Section 888.3000 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) MEDICAL DEVICES ORTHOPEDIC DEVICES Prosthetic Devices § 888.3000 Bone cap. (a) Identification. A bone cap is a mushroom...

  19. Genetic ablation of root cap cells in Arabidopsis

    OpenAIRE

    Tsugeki, Ryuji; Fedoroff, Nina V.

    1999-01-01

    The root cap is increasingly appreciated as a complex and dynamic plant organ. Root caps sense and transmit environmental signals, synthesize and secrete small molecules and macromolecules, and in some species shed metabolically active cells. However, it is not known whether root caps are essential for normal shoot and root development. We report the identification of a root cap-specific promoter and describe its use to genetically ablate root caps by directing root cap-specific expression of...

  20. CENTRIFUGE END CAP

    Science.gov (United States)

    Beams, J.W.; Snoddy, L.B.

    1960-08-01

    An end cap for ultra-gas centrifuges is designed to impart or remove angular momentum to or from the gas and to bring the entering gas to the temperature of the gas inside the centrifuge. The end cap is provided with slots or fins for adjusting the temperature and the angular momentum of the entering gas to the temperature and momentum of the gas in the centrifuge and is constructed to introduce both the inner and the peripheral stream into the centrifuge.

  1. Testosterone 5alpha-reductase inhibitory active constituents of Piper nigrum leaf.

    Science.gov (United States)

    Hirata, Noriko; Tokunaga, Masashi; Naruto, Shunsuke; Iinuma, Munekazu; Matsuda, Hideaki

    2007-12-01

    Previously we reported that Piper nigrum leaf extract showed a potent stimulation effect on melanogenesis and that (-)-cubebin (1) and (-)-3,4-dimethoxy-3,4-desmethylenedioxycubebin (2) were isolated as active constituents. As a part of our continuous studies on Piper species for the development of cosmetic hair-care agents, testosterone 5alpha-reductase inhibitory activity of aqueous ethanolic extracts obtained from several different parts of six Piper species, namely Piper nigrum, P. methysticum, P. betle, P. kadsura, P. longum, and P. cubeba, were examined. Among them, the extracts of P. nigrum leaf, P. nigrum fruit and P. cubeba fruit showed potent inhibitory activity. Activity-guided fractionation of P. nigrum leaf extract led to the isolation of 1 and 2. Fruits of P. cubeba contain 1 as a major lignan, thus inhibitory activity of the fruit may be attributable to 1. As a result of further assay on other known constituents of the cited Piper species, it was found that piperine, a major alkaloid amide of P. nigrum fruit, showed potent inhibitory activity, thus a part of the inhibitory activity of P. nigrum fruit may depend on piperine. The 5alpha-reductase inhibitory activities of 1 and piperine were found for the first time. In addition, the P. nigrum leaf extract showed in vivo anti-androgenic activity using the hair regrowth assay in testosterone sensitive male C57Black/6CrSlc strain mice.

  2. Formation and persistence of DNA adducts from the carcinogen N-hydroxy-2-acetylaminofluorene in rat mammary gland in vivo

    International Nuclear Information System (INIS)

    Allaben, W.T.; Weis, C.C.; Fullerton, N.F.; Beland, F.A.

    1983-01-01

    The rat mammary carcinogen, N-hydroxy-2-acetylaminofluorene (N-hydroxy-2-AAF), has been proposed to be metabolically activated by mammary cytosolic N,O-acetyltransferase to a DNA binding species. To test this hypothesis, adult female Sprague-Dawley derived CD rats were treated, i.p., with 4.0 mg/kg [ring- 3 H]N-hydroxy-2-AAF. After 4 h, 1, 3, 14, and 28 days, the animals were killed, the mammary epithelium DNA was isolated and the carcinogen-deoxyribonucleoside adducts present were analyzed by high pressure liquid chromatography. At each time, only one adduct was detected and it was chromatographically identical to N-(deoxyguanosin-8-yl)-2-aminofluorene. The level of the adduct was maximal at 4 h (1.5 adducts/10(6) nucleotides) and then decreased, following first order kinetics with a t1/2 of 14.2 days. The detection of a single non-acetylated aminofluorene adduct is consistent with N,O-acyltransferase being involved in the metabolic activation of N-hydroxy-2-AAF in the rat mammary gland

  3. Role of 3-Hydroxy Fatty Acid-Induced Hepatic Lipotoxicity in Acute Fatty Liver of Pregnancy

    Directory of Open Access Journals (Sweden)

    Sathish Kumar Natarajan

    2018-01-01

    Full Text Available Acute fatty liver of pregnancy (AFLP, a catastrophic illness for both the mother and the unborn offspring, develops in the last trimester of pregnancy with significant maternal and perinatal mortality. AFLP is also recognized as an obstetric and medical emergency. Maternal AFLP is highly associated with a fetal homozygous mutation (1528G>C in the gene that encodes for mitochondrial long-chain hydroxy acyl-CoA dehydrogenase (LCHAD. The mutation in LCHAD results in the accumulation of 3-hydroxy fatty acids, such as 3-hydroxy myristic acid, 3-hydroxy palmitic acid and 3-hydroxy dicarboxylic acid in the placenta, which are then shunted to the maternal circulation leading to the development of acute liver injury observed in patients with AFLP. In this review, we will discuss the mechanistic role of increased 3-hydroxy fatty acid in causing lipotoxicity to the liver and in inducing oxidative stress, mitochondrial dysfunction and hepatocyte lipoapoptosis. Further, we also review the role of 3-hydroxy fatty acids in causing placental damage, pancreatic islet β-cell glucolipotoxicity, brain damage, and retinal epithelial cells lipoapoptosis in patients with LCHAD deficiency.

  4. Role of 3-Hydroxy Fatty Acid-Induced Hepatic Lipotoxicity in Acute Fatty Liver of Pregnancy

    Science.gov (United States)

    Ibdah, Jamal A.

    2018-01-01

    Acute fatty liver of pregnancy (AFLP), a catastrophic illness for both the mother and the unborn offspring, develops in the last trimester of pregnancy with significant maternal and perinatal mortality. AFLP is also recognized as an obstetric and medical emergency. Maternal AFLP is highly associated with a fetal homozygous mutation (1528G>C) in the gene that encodes for mitochondrial long-chain hydroxy acyl-CoA dehydrogenase (LCHAD). The mutation in LCHAD results in the accumulation of 3-hydroxy fatty acids, such as 3-hydroxy myristic acid, 3-hydroxy palmitic acid and 3-hydroxy dicarboxylic acid in the placenta, which are then shunted to the maternal circulation leading to the development of acute liver injury observed in patients with AFLP. In this review, we will discuss the mechanistic role of increased 3-hydroxy fatty acid in causing lipotoxicity to the liver and in inducing oxidative stress, mitochondrial dysfunction and hepatocyte lipoapoptosis. Further, we also review the role of 3-hydroxy fatty acids in causing placental damage, pancreatic islet β-cell glucolipotoxicity, brain damage, and retinal epithelial cells lipoapoptosis in patients with LCHAD deficiency. PMID:29361796

  5. THE TURN OF THE MONTH EFFECT CONTINUED: A COMPARISON OF SMALL CAP STOCKS AND LARGE CAP STOCKS

    OpenAIRE

    Ramsundhar, Shamman

    2010-01-01

    The purpose of this paper is to investigate whether the turn of the month effect occurs in small cap and large cap stocks and if it occurs in both categories, to determine whether there is a difference in the magnitude. My research, for the period of 1963-2008, based on the CRSP value weighted index, shows that there is a significant turn of the month effect in small and large cap stocks, however the effect is larger in small cap stocks. Furthermore, this effect is not limited to a short time...

  6. Preparation of 2-(. alpha. -(2-ethoxyphenoxy)benzyl)-(5- sup 14 C)morpholine methanesulfonate (( sup 14 C)reboxetine):a new antidepressant agent

    Energy Technology Data Exchange (ETDEWEB)

    Angiuli, P.; Fontana, E.; Vicario, G.P. (Farmitalia Carlo Erba s.r.l., Milan (Italy))

    1991-05-01

    The labelling with radiocarbon of the new antidepressant agent Reboxetine is described. The preparation has been carried out in a two step procedure using 2-chloro-N-(3-(2-ethoxyphenoxy)-2-hydroxy-3-phenyl)propyl-(1-{sup 14}C)acetamide as starting material. The expected compound was prepared by cyclization of the above halogenoacylamido alcohol to the corresponding morpholone ring followed by reduction to the final (5-{sup 14}C)morpholine derivative 4, 98% radiochemically pure and with specific radioactivity of 988 MBq/mmol. An overall radiochemical yield of 57.5% was achieved. (author).

  7. 40 CFR 721.5252 - 2-Naphthalenecarboxylic acid, 4,4′-methylenebis [3-hydroxy-, zinc salt.

    Science.gov (United States)

    2010-07-01

    ...-methylenebis [3-hydroxy-, zinc salt. 721.5252 Section 721.5252 Protection of Environment ENVIRONMENTAL...′-methylenebis [3-hydroxy-, zinc salt. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified as 2-Naphthalenecarboxylic acid, 4,4′-methylenebis [3-hydroxy-, zinc...

  8. Speciation of a group I intron into a lariat capping ribozyme

    DEFF Research Database (Denmark)

    Meyer, Mélanie; Nielsen, Henrik; Oliéric, Vincent

    2014-01-01

    The lariat-capping (LC) ribozyme is a natural ribozyme isolated from eukaryotic microorganisms. Despite apparent structural similarity to group I introns, the LC ribozyme catalyzes cleavage by a 2',5' branching reaction, leaving the 3' product with a 3-nt lariat cap that functionally substitutes ....... The structures also show how conserved interactions twist residues, forming the lariat to join chemical groups involved in branching....

  9. Steroid withdrawal in the mouse results in anxiogenic effects of 3alpha,5beta-THP: a possible model of premenstrual dysphoric disorder.

    Science.gov (United States)

    Smith, Sheryl S; Ruderman, Yevgeniy; Frye, Cheryl; Homanics, Gregg; Yuan, Maoli

    2006-06-01

    3alpha-OH-5alpha[beta]-pregnan-20-one (THP) is a positive modulator of the GABAA receptor (GABAR), which underlies its reported anxiolytic effect. However, there are conditions such as premenstrual dysphoric disorder (PMDD) where increases in THP levels can be associated with adverse mood. In order to test for conditions where THP might be anxiogenic, we developed a mouse model of THP withdrawal. Because delta-containing GABAR are highly sensitive to THP modulation, results were compared in wild-type and delta knockout mice. Finasteride, a 5alpha-reductase blocker, was administered for 3 days to female wild-type or delta knockout mice. Then, animals were tested in the elevated plus maze, following acute administration of THP, lorazepam, flumazenil, or 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol (THIP), and results compared to vehicle-injected controls. CA1 hippocampal GABAR alpha4 subunit levels were assessed by Western blot. After THP withdrawal, THP produced anxiogenic effects, decreasing open arm entries on the elevated plus maze, following a brief shock, in contrast to its expected anxiolytic effects. As we have shown in rats, THP withdrawal also resulted in increased expression of the alpha4 subunit in mouse CA1 hippocampus. As expected for increases in alpha4-containing GABAR, THP withdrawn mice were relatively insensitive to the benzodiazepine (BDZ) lorazepam and had atypical responses to the BDZ antagonist flumazenil when tested on the plus maze. In contrast, they showed a greater anxiolytic response to THIP, which has greater efficacy at alpha4betadelta than other GABAR. Although THP withdrawal in delta knockout mice also increased the alpha4 GABAR subunit, the anxiogenic effects of THP and the anxiolytic effects of THIP were not observed, implicating alpha4betadelta GABAR in these effects. Based on these behavioral and pharmacological findings, we suggest that THP withdrawal in the mouse may serve as a rodent model of PMDD.

  10. Mixed ligand complexes of some of the rare earths. La(III)-, Pr(III)- or Nd-(III)-CDTA-Hydroxy Acids

    Energy Technology Data Exchange (ETDEWEB)

    Rana, H S; Tandon, J P [Rajasthan Univ., Jaipur (India). Chemical Labs.

    1975-11-01

    Biligand complexes of the 1:1 Ln(III)-1,2-diaminocyclohexane-tetraacetic acid (CDTA) chelate with hydroxy acids (where hydroxy acids = salicylic acid (SA); Sulphosalicylic acid (SSA) and 8-hydroxyquinoline-5-sulphonic acid (HQSA)) have been investigated by potentiometric titration. Their formation constants have been calculated (..mu..=0.1M-KNO/sub 3/; and t=30+-1 deg C) as 4.60 +-0.03, 5.46+-0.03, 5.87+-0.05; 3.12+-0.04, 3.95+-0.05, 4.42+-0.07; 2.73+-0.06, 3.45+-0.05 and 3.90+-0.08 for Ln(III)-CDTA-SA,-SSA, and -HQSA respectively (where Ln=La, Pr or Nd). The value of log Ksub(MAB) follows the order: La(III)

  11. Human skeletal uptake of natural alpha radioactivity from {sup 210}Pb-supported {sup 210}Po

    Energy Technology Data Exchange (ETDEWEB)

    Oyedepo, A.C

    1998-06-01

    This thesis contributes to increasing knowledge on the dosimetry of natural alpha-particle radiation in skeletal tissues, particularly in utero, and associated risks of malignancy. Alpha-particle radiation is an established aetiological factor of cancer. In the human body, polonium-210 decayed from skeletal lead-210 ({sup 210}Pb/{sup 210}Po) is the predominant natural alpha-emitter. {sup 210}Pb displaces calcium (Ca) in mineral hydroxyapatite, especially during periods of rapid bone growth and remodelling when Ca is laid down. It was therefore necessary to study alpha activity uptake and calcification concurrently within bone. Human studies were undertaken on: fetal vertebrae, 17 - 42 weeks of gestation, 74 samples; adult vertebrae, 40 - 95 years, 40 samples; and adult ribs, 20 - 95 years, 51 samples. Specimens were unconcentrated and weighed <5 g each. TASTRAK alpha-particle autoradiography was used to assess the bone activity concentration and spatial microdistribution of {sup 210}Pb/{sup 210}Po. Alpha track data were resolved by specially written software named SPATS (Selection Program for Analysing Track Structures). Ca and phosphorus (P) were biochemically determined. Results were examined for trends in bone type, gender and chronological ageing in humans. The main research findings were: 1) The Ca content of fetal vertebrae increased linearly at a weekly rate of 0.2g Ca 100 g{sup -1} wet bone (typical values of 2, 4, 6 g 100 g{sup -1} at 16, 26 and 36 weeks). 2) The P concentration also increased with advancing fetal age. 3) The Ca:P bone weight ratio rose from 1.7 to 2.2 by 32 gestational weeks. 4) The overall range in bone {sup 210}Pb/{sup 210}Po alpha activity was 0.25 - 1.1 Bq kg{sup -1} with correlation between activity concentration and fetal age (0.47 {+-} 0.05 Bq kg{sup -1} for 17 - 26 weeks, 0.67 {+-} 0.04 Bq kg{sup -1} for 32 - 42 weeks). 5) The correlation between increased alpha radioactivity and increased Ca concentration approximating to 0

  12. Increased virulence and competitive advantage of a/alpha over a/a or alpha/alpha offspring conserves the mating system of Candida albicans.

    Science.gov (United States)

    Lockhart, Shawn R; Wu, Wei; Radke, Joshua B; Zhao, Rui; Soll, David R

    2005-04-01

    The majority of Candida albicans strains in nature are a/alpha and must undergo homozygosis to a/a or alpha/alpha to mate. Here we have used a mouse model for systemic infection to test the hypothesis that a/alpha strains predominate in nature because they have a competitive advantage over a/a and alpha/alpha offspring in colonizing hosts. Single-strain injection experiments revealed that a/alpha strains were far more virulent than either their a/a or alpha/alpha offspring. When equal numbers of parent a/alpha and offspring a/a or alpha/alpha cells were co-injected, a/alpha always exhibited a competitive advantage at the time of extreme host morbidity or death. When equal numbers of an engineered a/a/alpha2 strain and its isogenic a/a parent strain were co-injected, the a/a/alpha2 strain exhibited a competitive advantage at the time of host morbidity or death, suggesting that the genotype of the mating-type (MTL) locus, not associated genes on chromosome 5, provides a competitive advantage. We therefore propose that heterozygosity at the MTL locus not only represses white-opaque switching and genes involved in the mating process, but also affects virulence, providing a competitive advantage to the a/alpha genotype that conserves the mating system of C. albicans in nature.

  13. Mechanistic studies with solubilized rat liver steroid 5 alpha-reductase: Elucidation of the kinetic mechanism

    International Nuclear Information System (INIS)

    Levy, M.A.; Brandt, M.; Greway, A.T.

    1990-01-01

    A solubilized preparation of steroid 5 alpha-reductase from rat liver has been used in studies focused toward an understanding of the kinetic mechanism associated with enzyme catalysis. From the results of analyses with product and dead-end inhibitors, a preferentially ordered binding of substrates and release of products from the surface of the enzyme is proposed. The observations from these experiments were identical with those using the steroid 5 alpha-reductase activity associated with rat liver microsomes. The primary isotope effects on steady-state kinetic parameters when [4S-2H]NADPH was used also were consistent with an ordered kinetic mechanism. Normal isotope effects were observed for all three kinetic parameters (Vm/Km for both testosterone and NADPH and Vm) at all substrate concentrations used experimentally. Upon extrapolation to infinite concentration of testosterone, the isotope effect on Vm/Km for NADPH approached unity, indicating that the nicotinamide dinucleotide phosphate is the first substrate binding to and the second product released from the enzyme. The isotope effects on Vm/Km for testosterone at infinite concentration of cofactor and on Vm were 3.8 +/- 0.5 and 3.3 +/- 0.4, respectively. Data from the pH profiles of these three steady-state parameters and the inhibition constants (1/Ki) of competitive inhibitors versus both substrates indicate that the binding of nicotinamide dinucleotide phosphate involves coordination of its anionic 2'-phosphate to a protonated enzyme-associated base with an apparent pK near 8.0. From these results, relative limits have been placed on several of the internal rate constants used to describe the ordered mechanism of the rat liver steroid 5 alpha-reductase

  14. Use of 5-alpha-reductase inhibitors did not increase the risk of cardiovascular diseases in patients with benign prostate hyperplasia: a five-year follow-up study.

    Directory of Open Access Journals (Sweden)

    Teng-Fu Hsieh

    Full Text Available This nationwide population-based study investigated the risk of cardiovascular diseases after 5-alpha-reductase inhibitor therapy for benign prostate hyperplasia (BPH using the National Health Insurance Research Database (NHIRD in Taiwan.In total, 1,486 adult patients newly diagnosed with BPH and who used 5-alpha-reductase inhibitors were recruited as the study cohort, along with 9,995 subjects who did not use 5-alpha-reductase inhibitors as a comparison cohort from 2003 to 2008. Each patient was monitored for 5 years, and those who subsequently had cardiovascular diseases were identified. A Cox proportional hazards model was used to compare the risk of cardiovascular diseases between the study and comparison cohorts after adjusting for possible confounding risk factors.The patients who received 5-alpha-reductase inhibitor therapy had a lower cumulative rate of cardiovascular diseases than those who did not receive 5-alpha-reductase inhibitor therapy during the 5-year follow-up period (8.4% vs. 11.2%, P=0.003. In subgroup analysis, the 5-year cardiovascular event hazard ratio (HR was lower among the patients older than 65 years with 91 to 365 cumulative defined daily dose (cDDD 5-alpha-reductase inhibitor use (HR=0.63, 95% confidence interval (CI 0.42 to 0.92; P=0.018, however there was no difference among the patients with 28 to 90 and more than 365 cDDD 5-alpha-reductase inhibitor use (HR=1.14, 95% CI 0.77 to 1.68; P=0.518 and HR=0.83, 95% CI 0.57 to 1.20; P=0.310, respectively.5-alpha-reductase inhibitor therapy did not increase the risk of cardiovascular events in the BPH patients in 5 years of follow-up. Further mechanistic research is needed.

  15. Double capping of molecular beam epitaxy grown InAs/InP quantum dots studied by cross-sectional scanning tunneling microscopy

    International Nuclear Information System (INIS)

    Ulloa, J. M.; Koenraad, P. M.; Gapihan, E.; Letoublon, A.; Bertru, N.

    2007-01-01

    Cross-sectional scanning tunneling microscopy was used to study at the atomic scale the double capping process of self-assembled InAs/InP quantum dots (QDs) grown by molecular beam epitaxy on a (311)B substrate. The thickness of the first capping layer is found to play a mayor role in determining the final results of the process. For first capping layers up to 3.5 nm, the height of the QDs correspond to the thickness of the first capping layer. Nevertheless, for thicknesses higher than 3.5 nm, a reduction in the dot height compared to the thickness of the first capping layer is observed. These results are interpreted in terms of a transition from a double capping to a classical capping process when the first capping layer is thick enough to completely cover the dots

  16. The alpha3 laminin subunit, alpha6beta4 and alpha3beta1 integrin coordinately regulate wound healing in cultured epithelial cells and in the skin

    DEFF Research Database (Denmark)

    Goldfinger, L E; Hopkinson, S B; deHart, G W

    1999-01-01

    Previously, we demonstrated that proteolytic processing within the globular domain of the alpha3 subunit of laminin-5 (LN5) converts LN5 from a cell motility-inducing factor to a protein complex that can trigger the formation of hemidesmosomes, certain cell-matrix attachment sites found in epithe......-inhibiting antibodies, we provide evidence that LN5 and its two integrin receptors (alpha6beta4 and alpha3beta1) appear necessary for wound healing to occur in MCF-10A cell culture wounds. We propose a model for healing of wounded epithelial tissues based on these results....... in epithelial cells. We have prepared a monoclonal antibody (12C4) whose epitope is located toward the carboxy terminus of the globular domain of the alpha3 laminin subunit. This epitope is lost from the alpha3 subunit as a consequence of proteolytic processing. Antibody 12C4 stains throughout the matrix...... the wound site. A similar phenomenon is observed in human skin wounds, since we also detect expression of the unprocessed alpha3 laminin subunit at the leading tip of the sheet of epidermal cells that epithelializes skin wounds in vivo. In addition, using alpha3 laminin subunit and integrin function...

  17. A novel GABA(A) alpha 5 receptor inhibitor with therapeutic potential.

    Science.gov (United States)

    Ling, István; Mihalik, Balázs; Etherington, Lori-An; Kapus, Gábor; Pálvölgyi, Adrienn; Gigler, Gábor; Kertész, Szabolcs; Gaál, Attila; Pallagi, Katalin; Kiricsi, Péter; Szabó, Éva; Szénási, Gábor; Papp, Lilla; Hársing, László G; Lévay, György; Spedding, Michael; Lambert, Jeremy J; Belelli, Delia; Barkóczy, József; Volk, Balázs; Simig, Gyula; Gacsályi, István; Antoni, Ferenc A

    2015-10-05

    Novel 2,3-benzodiazepine and related isoquinoline derivatives, substituted at position 1 with a 2-benzothiophenyl moiety, were synthesized to produce compounds that potently inhibited the action of GABA on heterologously expressed GABAA receptors containing the alpha 5 subunit (GABAA α5), with no apparent affinity for the benzodiazepine site. Substitutions of the benzothiophene moiety at position 4 led to compounds with drug-like properties that were putative inhibitors of extra-synaptic GABAA α5 receptors and had substantial blood-brain barrier permeability. Initial characterization in vivo showed that 8-methyl-5-[4-(trifluoromethyl)-1-benzothiophen-2-yl]-1,9-dihydro-2H-[1,3]oxazolo[4,5-h][2,3]benzodiazepin-2-one was devoid of sedative, pro-convulsive or motor side-effects, and enhanced the performance of rats in the object recognition test. In summary, we have discovered a first-in-class GABA-site inhibitor of extra-synaptic GABAA α5 receptors that has promising drug-like properties and warrants further development. Copyright © 2015 Elsevier B.V. All rights reserved.

  18. Labeling of eukaryotic messenger RNA 5' terminus with phosphorus -32: use of tobacco acid pyrophosphatase for removal of cap structures

    International Nuclear Information System (INIS)

    Lockard, R.E.; Rieser, L.; Vournakis, J.N.

    1981-01-01

    In recent years, there has been a growing appreciation of the potential applications of 5'- 32 P-end-labeled mRNA, not only for screening recombinant clones and mapping gene structure, but also for revealing possible nucleotide sequence and structural signals within mRNA molecules themselves, which may be important for eukaryotic mRNA processing and turnover and for controlling differential rates of translational initiation. Three major problems, however, have retarded progress in this area, lack of methods for efficient and reproducible removal of m7G5ppp5'-cap structures, which maintain the integrity of an RNA molecule; inability to generate a sufficient amount of labeled mRNA, owing to the limited availability of most pure mRNA species; and the frequent problem of RNA degradation during in vitro end-labeling owing to RNAse contamination. The procedures presented here permit one to decap and label minute quantities of mRNA, effectively. Tobacco acid pyrophosphatase is relatively efficient in removing cap structures from even nanogram quantities of available mRNA, and enough radioactivity can be easily generated from minute amounts ofintact mRNA with very high-specific-activity [gamma- 32 P]ATP and the inhibition of ribonuclease contamination with diethylpyrocarbonate. These procedures can be modified and applied to almost any other type of RNA molecule as well. In Section III of this volume, we explore in detail how effectively 5'-end-labeled mRNA can be used not only for nucleotide sequence analysis, but also for mapping mRNA secondary structure

  19. Differential expression of 5-alpha reductase isozymes in the prostate and its clinical implications

    Directory of Open Access Journals (Sweden)

    Kai Wang

    2014-04-01

    Full Text Available The development of human benign or malignant prostatic diseases is closely associated with androgens, primarily testosterone (T and dihydrotestosterone (DHT. T is converted to DHT by 5-alpha reductase (5-AR isozymes. Differential expression of 5-AR isozymes is observed in both human benign and malignant prostatic tissues. 5-AR inhibitors (5-ARI are commonly used for the treatment of benign prostatic hyperplasia (BPH and were once promoted as chemopreventive agents for prostate cancer (PCa. This review discusses the role of the differential expression of 5-AR in the normal development of the human prostate and in the pathogenesis and progression of BPH and PCa.

  20. Cyclohex-1-ene carboxylic acids: synthesis and biological evaluation of novel inhibitors of human 5 alpha reductase.

    Science.gov (United States)

    Baston, Eckhard; Salem, Ola I A; Hartmann, Rolf W

    2003-03-01

    In search of novel nonsteroidal mimics of steroidal inhibitors of 5 alpha reductase, 4-(2-phenylethyl)cyclohex-1-ene carboxylic acids 1-5 were synthesized with different substituents in para position of the phenyl ring (1: N, N-diisopropylcarbamoyl, 2: phenyl, 3: phenoxy, 4: benzoyl, and 5: benzyl). The principal synthetic approach for the desired compounds consisted of a Wittig olefination between 1, 4-dioxaspiro [4.5]-decane-8-carbaldehyde (4g and the appropriate phosphonium salts. The compounds were tested for inhibition of human 5 alpha reductase isozymes 1 and 2 using DU 145 cells and preparations from prostatic tissue, respectively. They turned out to be good inhibitors of the prostatic isozyme 2 with compound 1 being the most potent one (IC(50) = 760 nM). Isozyme 1 was only slightly inhibited. It is concluded that the novel structures are appropriate for being further optimized, aiming at the development of a novel drug for the treatment of benign prostatic hyperplasia.

  1. Preparation of 5-benzotriazolyl-4-hydroxy-3-sec-butylbenzenesulfonate anion-intercalated layered double hydroxide and its photostabilizing effect on polypropylene

    International Nuclear Information System (INIS)

    Li Dianqing; Tuo Zhenjun; Evans, David G.; Duan Xue

    2006-01-01

    An organic UV absorber has been intercalated into a layered double hydroxide (LDH) host by ion-exchange method using ZnAl-NO 3 -LDH as a precursor with an aqueous solution of the sodium salt of 5-benzotriazolyl-4-hydroxy-3-sec-butylbenzenesulfonic acid (BZO). After intercalation of the UV absorber, the interlayer distance in the LDHs increases from 0.89 to 2.32 nm. Infrared spectra and thermogravimetry and differential thermal analysis (TG-DTA) curves reveal the presence of a complex system of supramolecular host-guest interactions. The thermostability of BZO is markedly enhanced by intercalation in the LDH host. ZnAl-BZO-LDHs/polypropylene composite materials exhibit excellent UV photostability. - Graphical abstract: Intercalation of an organic UV absorber in a layered double hydroxide host leads to an enhancement of its photo- and thermal stability

  2. Biomodulation with sequential intravenous IFN-alpha2b and 5-fluorouracil as second-line treatment in patients with advanced colorectal cancer.

    Science.gov (United States)

    Pérez, J E; Lacava, J A; Domínguez, M E; Rodríguez, R; Barbieri, M R; Romero Acuña, L A; Romero Acuña, J M; Langhi, M J; Amato, S; Marrone, N; Ortiz, E H; Leone, B A; Vallejo, C T; Machiavelli, M R; Romero, A O

    1998-08-01

    A phase II trial was carried out by the Grupo Oncologico Cooperativo del Sur (G.O.C.S.) to assess the efficacy and toxicity of a biochemical modulation of 5-fluorouracil (5-FU) by i.v. pretreatment with interferon (IFN)-alpha2b in patients with advanced colorectal carcinoma refractory to previous therapy with 5-FU modulated by methotrexate (MTX) or leucovorin (LV) or both. Between January 1993 and October 1995, 34 patients were entered on the study. The treatment was IFN-alpha2b 5 x 10(6)/m2 IU in a 1-h i.v. infusion, followed immediately by 5-FU 600 mg/m2 i.v. bolus injection. Courses were repeated weekly until observation of progressive disease or severe toxicity. One patient could not be assessed for response. Objective regression was observed in 2 of 33 patients (6%, 95% confidence interval, 0%-14%). No patient achieved a complete response. Two patients had partial responses (6%). No change was recorded in 14 patients (41%), and progressive disease occurred in 17 (52%). The median time to treatment failure was 3 months, and the median survival was 5 months. Toxicity was within acceptable limits. The main side effects were mucositis and diarrhea. Four episodes of grade 2 stomatitis were observed, causing dosage modifications. The most frequent toxic effects attributable to IFN-alpha2b were mild fatigue and fever. In conclusion, second-line therapy with i.v. IFN-alpha2b preceding 5-FU has shown an interesting profile of activity in a patient population with clearly unfavorable characteristics. From this perspective, further appropriately designed studies are needed to identify the greatest potential of IFN-alpha2b as a modulator of 5-FU.

  3. Reactor neutron activation analysis for aluminium in the presence of phosphorus and silicon. Contributions of /sup 28/Al activities from /sup 31/P (n,. cap alpha. ) /sup 28/Al and /sup 28/Si (n,p) /sup 28/Al reactions

    Energy Technology Data Exchange (ETDEWEB)

    Mizumoto, Yoshihiko (Kinki Univ., Higashi-Osaka, Osaka (Japan). Faculty of Science and Technology); Iwata, Shiro; Sasajima, Kazuhisa; Yoshimasu, Fumio; Yase, Yoshiro

    1984-01-01

    Reactor neutron activation analysis for aluminium in samples containing phosphorus and silicon was studied. The experiments were performed by using pneumatic tube of the Kyoto University Reactor (KUR). At first, the ratios of the /sup 28/Al activity produced from /sup 27/Al(n, ..gamma..) /sup 28/Al reaction by thermal neutrons to that from /sup 31/P(n, ..cap alpha..)/sup 28/Al reaction by fast neutrons, and to that from /sup 28/Si(n, p)/sup 28/Al reaction were measured by ..gamma..-ray spectrometry. With a ratio of about 5 for the thermal to fast neutron flux of KUR, the ratio of the /sup 28/Al activity from aluminium to that from phosphorus was to be 812 +- 7, and to that from silicon 282 +- 3. Secondly, the contributions of /sup 28/Al activities from phosphorus and silicon and the determination limit of aluminium were calculated for various parameters, such as fast neutron flux, thermal to fast neutron flux ratio, amounts of phosphorus and silicon, etc. Thirdly, on the basis of these results, aluminium contents in spinal cords and brains of amyotrophic lateral sclerosis, Parkinsonism-dementia complex and control cases were determined.

  4. Stereocontrolled reduction of alpha- and beta-keto esters with micro green algae, Chlorella strains.

    Science.gov (United States)

    Ishihara, K; Yamaguchi, H; Adachi, N; Hamada, H; Nakajima, N

    2000-10-01

    The stereocontrolled reduction of alpha- and beta-keto esters using micro green algae was accomplished by a combination of the cultivation method and the introduction of an additive. The reduction of ethyl pyruvate and ethyl benzoylformate by the photoautotrophically cultivated Chlorella sorokiniana gave the corresponding alcohol in high e.e. (>99% e.e. (S) and >99% e.e. (R), respectively). In the presence of glucose as an additive, the reduction of ethyl 3-methyl-2-oxobutanoate by the heterotrophically cultivated C. sorokiniana afforded the corresponding (R)-alcohol. On the other hand, the reduction in the presence of ethyl propionate gave the (S)-alcohol. Ethyl 2-methyl-3-oxobutanoate was reduced in the presence of glycerol by the photoautotrophically cultivated C. sorokiniana or the heterotrophically cultivated C. sorokiniana to the corresponding syn-(2R,3S)-hydroxy ester with high diastereo- and enantiomeric excess (e.e.). Some additives altered the stereochemical course in the reduction of alpha- and beta-keto esters.

  5. Synthesis and nicotinic receptor activity of a hydroxylated tropane

    DEFF Research Database (Denmark)

    Bremner, John B; Godfrey, Colette A; Jensen, Anders A.

    2004-01-01

    (+/-)-3alpha-hydroxy homoepibatidine 4 has been synthesized from the alkaloid scopolamine 5 and its properties as a nicotinic agonist assessed. While still binding strongly, the compound showed reduced agonist potency for the alpha(4)beta(2) nAChR compared with the parent compound epibatidine 1....... Compound 4 also displayed generally similar binding and selectivity profiles at alpha(4)beta(2), alpha(2)beta(4), alpha(3)beta(4), and alpha(4)beta(4) nAChR subtypes to those for nicotine....

  6. Cold atmospheric plasma (CAP changes gene expression of key molecules of the wound healing machinery and improves wound healing in vitro and in vivo.

    Directory of Open Access Journals (Sweden)

    Stephanie Arndt

    Full Text Available Cold atmospheric plasma (CAP has the potential to interact with tissue or cells leading to fast, painless and efficient disinfection and furthermore has positive effects on wound healing and tissue regeneration. For clinical implementation it is necessary to examine how CAP improves wound healing and which molecular changes occur after the CAP treatment. In the present study we used the second generation MicroPlaSter ß® in analogy to the current clinical standard (2 min treatment time in order to determine molecular changes induced by CAP using in vitro cell culture studies with human fibroblasts and an in vivo mouse skin wound healing model. Our in vitro analysis revealed that the CAP treatment induces the expression of important key genes crucial for the wound healing response like IL-6, IL-8, MCP-1, TGF-ß1, TGF-ß2, and promotes the production of collagen type I and alpha-SMA. Scratch wound healing assays showed improved cell migration, whereas cell proliferation analyzed by XTT method, and the apoptotic machinery analyzed by protein array technology, was not altered by CAP in dermal fibroblasts. An in vivo wound healing model confirmed that the CAP treatment affects above mentioned genes involved in wound healing, tissue injury and repair. Additionally, we observed that the CAP treatment improves wound healing in mice, no relevant side effects were detected. We suggest that improved wound healing might be due to the activation of a specified panel of cytokines and growth factors by CAP. In summary, our in vitro human and in vivo animal data suggest that the 2 min treatment with the MicroPlaSter ß® is an effective technique for activating wound healing relevant molecules in dermal fibroblasts leading to improved wound healing, whereas the mechanisms which contribute to these observed effects have to be further investigated.

  7. Quantitative analysis of hydroperoxy-, keto- and hydroxy-dienes in refined vegetable oils.

    Science.gov (United States)

    Morales, Arturo; Marmesat, Susana; Dobarganes, M Carmen; Márquez-Ruiz, Gloria; Velasco, Joaquín

    2012-03-16

    Quantitative analysis of the main oxidation products of linoleic acid - hydroperoxy-, keto- and hydroxy-dienes - in refined oils is proposed in this study. The analytical approach consists of derivatization of TAGs into FAMEs and direct analysis by HPLC-UV. Two transmethylation methods run at room temperature were evaluated. The reactants were KOH in methanol in method 1 and sodium methoxide (NaOMe) in method 2. Method 1 was ruled out because resulted in losses of hydroperoxydienes as high as 90 wt%. Transmethylation with NaOMe resulted to be appropriate as derivatization procedure, although inevitably also gives rise to losses of hydroperoxydienes, which were lower than 10 wt%, and formation of keto- and hydroxy-dienes as a result. An amount of 0.6-2.1 wt% of hydroperoxydienes was transformed into keto- and hydroxy-dienes, being the formation of the former as much as three times higher. The method showed satisfactory sensitivity (quantification limits of 0.3 μg/mL for hydroperoxy- and keto-dienes and 0.6 μg/mL for hydroxydienes), precision (coefficients of variation ≤ 6% for hydroperoxydienes and ≤ 15% for keto- and hydroxy-dienes) and accuracy (recovery values of 85(± 4), 99(± 2) and 97.0(± 0.6) % for hydroperoxy-, keto- and hydroxy-dienes, respectively). The method was applied to samples of high-linoleic (HLSO), high-oleic (HOSO) and high-stearic high-oleic (HSHOSO) sunflower oils oxidized at 40 °C. Results showed that the higher the linoleic-to-oleic ratio, the higher were the levels of hydroperoxy-, keto- and hydroxy-dienes when tocopherols were completely depleted, i.e. at the end of the induction period (IP). Levels of 23.7, 2.7 and 1.1 mg/g oil were found for hydroperoxy-, keto- and hydroxy-dienes, respectively, in the HLSO when tocopherol was practically exhausted. It was estimated that hydroperoxydienes constituted approximately 100, 95 and 60% of total hydroperoxides in the HLSO, HOSO and HSHOSO, respectively, along the IP. Copyright © 2012

  8. Targeted Alpha Therapy: From Alpha to Omega

    International Nuclear Information System (INIS)

    Allen, Barry J; Clarke, Raymond; Huang Chenyu

    2013-01-01

    This review covers the broad spectrum of Targeted Alpha Therapy (TAT) research in Australia; from in vitro and in vivo studies to clinical trials. The principle of tumour anti-vascular alpha therapy (TAVAT) is discussed in terms of its validation by Monte Carlo calculations of vascular models and the potential role of biological dosimetry is examined. Summmary of this review is as follows: 1. The essence of TAT 2. Therapeutic objectives 3. TAVAT and Monte Carlo microdosimetry 4. Biological dosimetry 5. Preclinical studies 6. Clinical trials 7. What next? 8. Obstacles. (author)

  9. Synthesis and antibacterial activity of bis-[2-hydroxy-3-(1,7,8,9,10-pentamethyl-3,5-dioxo-4-aza-tricyclo[5.2.1.0(2,6)]dec-8-en-4-yloxy)-propyl]-dimethyl-ammonium chloride.

    Science.gov (United States)

    Struga, Marta; Kossakowski, Jerzy; Stefańska, Joanna; Zimniak, Andrzej; Koziol, Anna E

    2008-06-01

    A new quaternary ammonium compound, bis-[2-hydroxy-3-(1,7,8,9,10-pentamethyl-3,5-dioxo-4-aza-tricyclo[5.2.1.0(2,6)]dec-8-en-4-yloxy)-propyl]-dimethyl-ammonium chloride (4), was synthesized. The compound was investigated for antibacterial activity, including Gram-positive cocci and Gram-negative rods, and antifungal activity. Compound 4 showed significant inhibition against Staphylococcus aureus. Research was carried out over 4 standard strains and 40 hospital strains. Elementary analysis and/or MS, (1)H NMR and (13)C NMR spectra confirmed the identity of the products. The molecular structure of 3 was determined by an X-ray analysis.

  10. Polar Ice Caps: a Canary for the Greenland Ice Sheet

    Science.gov (United States)

    Honsaker, W.; Lowell, T. V.; Sagredo, E.; Kelly, M. A.; Hall, B. L.

    2010-12-01

    Ice caps are glacier masses that are highly sensitive to climate change. Because of their hypsometry they can have a binary state. When relatively slight changes in the equilibrium line altitude (ELA) either intersect or rise above the land the ice can become established or disappear. Thus these upland ice masses have a fast response time. Here we consider a way to extract the ELA signal from independent ice caps adjacent to the Greenland Ice Sheet margin. It may be that these ice caps are sensitive trackers of climate change that also impact the ice sheet margin. One example is the Istorvet Ice Cap located in Liverpool Land, East Greenland (70.881°N, 22.156°W). The ice cap topography and the underlying bedrock surface dips to the north, with peak elevation of the current ice ranging in elevation from 1050 to 745 m.a.s.l. On the eastern side of the ice mass the outlet glaciers extending down to sea level. The western margin has several small lobes in topographic depressions, with the margin reaching down to 300 m.a.s.l. Topographic highs separate the ice cap into at least 5 main catchments, each having a pair of outlet lobes toward either side of the ice cap. Because of the regional bedrock slope each catchment has its own elevation range. Therefore, as the ELA changes it is possible for some catchments of the ice cap to experience positive mass balance while others have a negative balance. Based on weather observations we estimate the present day ELA to be ~1000 m.a.s.l, meaning mass balance is negative for the majority of the ice cap. By tracking glacier presence/absence in these different catchments, we can reconstruct small changes in the ELA. Another example is the High Ice Cap (informal name) in Milne Land (70.903°N, 25.626°W, 1080 m), East Greenland. Here at least 4 unconformities in ice layers found near the southern margin of the ice cap record changing intervals of accumulation and ablation. Therefore, this location may also be sensitive to slight

  11. Extraction and spectrophotometric determination of vanadium(V) with N-hydroxy-N-m-tolyl-N'-(2-methyl-5-chloro)-phenyl-p-toluamidine hydrochloride in presence of salicylic, anthranilic and phthalic acids

    Energy Technology Data Exchange (ETDEWEB)

    Patel, K S; Deb, K K; Mishra, R [Ravishankar Univ., Raipur (India). Dept. of Chemistry

    1981-02-01

    The present work deals with the solvent extraction and simultaneous spectrophotometric determination of microgram quantities of vanadium(V) as mixed ligand complex with N-hydroxy-N-m-tolyl-N'-(2-methyl-5-chloro)-phenyl-p-toluamidine hydrochloride (HTMCPTH) and six carboxylic acids viz. salicylic, acetylsalicylic (aspirin), sulfosalicylic, anthranilic, N-phenyl-anthranilic and phthalic. The method presented here is simple, rapid, sensitive and reasonably selective.

  12. Extraction and spectrophotometric determination of vanadium(V) with N-hydroxy-N-m-tolyl-N'-(2-methyl-5-chloro)-phenyl-p-toluamidine hydrochloride in presence of salicylic, anthranilic and phthalic acids

    International Nuclear Information System (INIS)

    Patel, K.S.; Deb, K.K.; Mishra, R.

    1981-01-01

    The present work deals with the solvent extraction and simultaneous spectrophotometric determination of microgram quantities of vanadium(V) as mixed ligand complex with N-hydroxy-N-m-tolyl-N'-(2-methyl-5-chloro)-phenyl-p-toluamidine hydrochloride (HTMCPTH) and six carboxylic acids viz. salicylic, acetylsalicylic (aspirin), sulfosalicylic, anthranilic, N-phenyl-anthranilic and phthalic. The method presented here is simple, rapid, sensitive and reasonably selective. (author)

  13. Alpha- and Beta-Cyclodextrin Inclusion Complexes with 5-Fluorouracil: Characterization and Cytotoxic Activity Evaluation

    Directory of Open Access Journals (Sweden)

    Cristina Di Donato

    2016-12-01

    Full Text Available Cyclodextrins are natural macrocyclic oligosaccharides able to form inclusion complexes with a wide variety of guests, affecting their physicochemical and pharmaceutical properties. In order to obtain an improvement of the bioavailability and solubility of 5-fluorouracil, a pyrimidine analogue used as chemotherapeutic agent in the treatment of the colon, liver, and stomac cancers, the drug was complexed with alpha- and beta-cyclodextrin. The inclusion complexes were prepared in the solid state by kneading method and characterized by Fourier transform-infrared (FT-IR spectroscopy and X-ray powder diffractometry. In solution, the 1:1 stoichiometry for all the inclusion complexes was established by the Job plot method and the binding constants were determined at different pHs by UV-VIS titration. Furthermore, the cytotoxic activity of 5-fluorouracil and its complexation products were evaluated using the 3-(4,5-dimethylthiazol-2-yl-2,5-diphenyltetrazolium bromide (MTT assay on MCF-7 (breast cancer cell line, Hep G2 (hepatocyte carcinoma cell line, Caco-2 (colon adenocarcinoma cell line, and A-549 (alveolar basal epithelial carcinoma cell line. The results showed that both inclusion complexes increased the 5-fluorouracil capability of inhibiting cell growth. In particular, 5-fluorouracil complexed with beta-cyclodextrin had the highest cytotoxic activity on MCF-7; with alpha-cyclodextrin the highest cytotoxic activity was observed on A-549. The IC50 values were equal to 31 and 73 µM at 72 h, respectively. Our results underline the possibility of using these inclusion complexes in pharmaceutical formulations for improving 5-fluorouracil therapeutic efficacy.

  14. Symptomatic benign prostatic hyperplasia: the role of 5-alpha-reductase inhibitors in the prevention of acute urinary retention and surgical therapy

    Directory of Open Access Journals (Sweden)

    Norma Marigliano

    2012-01-01

    Full Text Available Benign prostatic hyperplasia (BPH is a disease that affects over 50% of males aged 50 years or older. In men aged >80 years, the incidence is 90%. BPH occurs in 9-25% of males aged 40 to 79 years. Fifty percent of patients with BPH are symptomatic. The symptoms include reduced urinary flow, nocturia, defective bladder emptying, urinary hesitancy, and dysuria. Disease progression can be associated with acute urinary retention (AUR. Prostatic obstruction includes mechanical and dynamic components, the latter mediated by alpha-muscarinic receptors. Treatment with alpha-1-blockers (alfuzosin, doxazosin, tamsulosin, and terazosin leads to rapid amelioration of symptoms and urinary flow, usually within one or two weeks. The 5-alpha reductase inhibitors (5-ARIs are “disease-modifying drugs.” They control the growth of the prostate by blocking the conversion of testosterone into dihydrotestosterone (DHT. Finasteride is a 5–ARI that is selective for type 2 receptors. Dutasteride is a powerful inhibitor of both 5- alpha reductase isoforms (type 1 and 2 and produces more complete suppression of DHT synthesis than finasteride. Dutasteride also has a much longer half-life than finasteride (five weeks versus five to six hours. The authors review the results of clinical trials involving finasteride and dutasteride, with and without alpha-1-blockers, highlighting the important role of dutasteride in improving acute urinary retention and eliminating the need for surgical therapy.

  15. Determination of polycyclic aromatic hydrocarbons and their oxy-, nitro-, and hydroxy-oxidation products

    International Nuclear Information System (INIS)

    Cochran, R.E.; Dongari, N.; Jeong, H.; Beránek, J.; Haddadi, S.; Shipp, J.; Kubátová, A.

    2012-01-01

    Highlights: ► We describe a method for determining PAHs and their oxidation products. ► Solid-phase extraction was used to fractionate PAHs and their oxidation products. ► Gas chromatography–mass spectrometry methods were optimized. ► The developed method was applied to two particulate matter (PM) samples. - Abstract: A sensitive method has been developed for the trace analysis of PAHs and their oxidation products (i.e., nitro-, oxy-, and hydroxy-PAHs) in air particulate matter (PM). Following PM extraction, PAHs, nitro-, oxy-, and hydroxy-PAHs were fractionated using solid phase extraction (SPE) based on their polarities. Gas chromatography–mass spectrometry (GC–MS) conditions were optimized, addressing injection (i.e., splitless time), negative-ion chemical ionization (NICI) parameters, i.e., source temperature and methane flow rate, and MS scanning conditions. Each class of PAH oxidation products was then analyzed using the sample preparation and appropriate ionization conditions (e.g., nitro-PAHs exhibited the greatest sensitivity when analyzed with NICI–MS while hydroxy-PAHs required chemical derivatization prior to GC–MS analysis). The analyses were performed in selected-ion-total-ion (SITI) mode, combining the increased sensitivity of selected-ion monitoring (SIM) with the identification advantages of total-ion current (TIC). The instrumental LODs determined were 6–34 pg for PAHs, 5–36 pg for oxy-PAHs, and 1–21 pg for derivatized hydroxy-PAHs using electron ionization (GC-EI-MS). NICI–MS was found to be a useful tool for confirming the tentative identification of oxy-PAHs. For nitro-PAHs, LODs were 1–10 pg using negative-ion chemical ionization (GC-NICI-MS). The developed method was successfully applied to two types of real-world PM samples, diesel exhaust standard reference material (SRM 2975) and wood smoke PM.

  16. Analyses of hydraulic performance of velocity caps

    DEFF Research Database (Denmark)

    Christensen, Erik Damgaard; Degn Eskesen, Mark Chr.; Buhrkall, Jeppe

    2014-01-01

    The hydraulic performance of a velocity cap has been investigated. Velocity caps are often used in connection with offshore intakes. CFD (computational fluid dynamics) examined the flow through the cap openings and further down into the intake pipes. This was combined with dimension analyses...

  17. Biological roles and therapeutic potential of hydroxy-carboxylic acid receptors

    Directory of Open Access Journals (Sweden)

    Kashan eAhmed

    2011-10-01

    Full Text Available In the recent past, deorphanization studies have described intermediates of energy metabolism to activate G protein-coupled receptors (GPCRs and to thereby regulate metabolic functions. GPR81, GPR109A and GPR109B, formerly known as the nicotinic acid receptor family, are encoded by clustered genes and share a high degree of sequence homology. Recently, hydroxy-carboxylic acids were identified as endogenous ligands of GPR81, GPR109A and GPR109B, and therefore these receptors have been placed into a novel receptor family of hydroxy-carboxylic acid (HCA receptors. The HCA1 receptor (GPR81 is activated by the glycolytic metabolite 2-hydroxy-propionic acid (lactate, the HCA2 receptor is activated by the ketone body 3-hydroxy-butyric acid and the HCA3 receptor (GPR109B is a receptor for the β-oxidation intermediate 3-hydroxy-octanoic acid. While HCA1 and HCA2 receptors are present in most mammalian species, the HCA3 receptor is exclusively found in humans and higher primates. HCA receptors are expressed in adipose tissue and mediate anti-lipolytic effects in adipocytes through Gi-type G-protein-dependent inhibition of adenylyl cyclase. HCA2 and HCA3 inhibit lipolysis during conditions of increased β-oxidation such as prolonged fasting, whereas HCA1 mediates the anti-lipolytic effects of insulin in the fed state. As HCA2 is a receptor for the established anti-dyslipidemic drug nicotinic acid, HCA1 and HCA3 also represent promising drug targets and several synthetic ligands for HCA receptors have been developed. In this article, we will summarize the deorphanization and pharmacological characterization of HCA receptors. Moreover, we will discuss recent progress in elucidating the physiological and pathophysiological role to further evaluate the therapeutic potential of the HCA receptor family for the treatment of metabolic disease.

  18. Studies of Li, B and N in ancient oriental pottery and modern ceramic materials by means of (n,p) and (n,. cap alpha. ) spectrometry

    Energy Technology Data Exchange (ETDEWEB)

    Fink, D. (Hahn-Meitner-Institut fuer Kernforschung Berlin G.m.b.H. (Germany, F.R.)); Riederer, J. (Staatliche Museen Preussischer Kulturbesitz, Berlin (Germany, F.R.). Rathgen-Forschungslabor)

    1981-12-31

    The content of Li, B, and N is examined in ancient and modern pottery and its glazes by means of (n,p) and (n,..cap alpha..) reactions with thermal neutrons. Most samples exhibit a proportionality between B and Li concentrations with preferred values around 0.01 at.%. One group of pottery shows nearly constant Li abundance around 0.1 at.%, the B content varying from 10/sup -4/ at.% to 10 at.%. An explanation is given, and the individual groups of pottery are described in detail. Results for different archaeological sites of Sumerian, Babylonian, Assyrian, Phoenician and Roman provenience are presented. The data scattering of B and Li contents of samples from different places of origin varies considerably, and can be used as a measure of the economical importance of ancient centers. Local urban cultures, such as Ur, exhibit a relative data scattering around 0.2, cities with average trade relations show values around 0.4, and for the famous trade center Palmyra, 0.8 was found. The B/Li ratio of pottery indicates whether the clay used is a fresh water or a marine sediment. The B and Li contents of Euphrates pottery show systematic variations along the river valley. Several samples, found in the Mesopotamian region are highly enriched in nitrogen. This is probably due to salt precipitation in the surrounding soil after the destruction of the irrigation facilities by the Mongols in 1258.

  19. Synthesis of TOPO-capped Nanocrystals of Copper Sulphide from a ...

    African Journals Online (AJOL)

    Nearly mono-dispersed TOPO-capped copper sulphide nanocrystals of ca. 4.5 nm (diameter) have been ... aqueous sols,1 monolayers,2 bilayer lipid membranes,3,4 LB films,5 ... addition of an excess of methanol to the yellow solution a thin.

  20. The respective N-hydroxypyrazole analogues of the classical glutamate receptor ligands ibotenic acid and (RS)-2-amino-2-(3-hydroxy-5-methyl-4-isoxazolyl)acetic acid

    DEFF Research Database (Denmark)

    Clausen, Rasmus P; Hansen, Kasper B; Calí, Patrizia

    2004-01-01

    We have determined the pharmacological activity of N-hydroxypyrazole analogues (3a and 4a) of the classical glutamate receptor ligands ibotenic acid and (RS)-2-amino-2-(3-hydroxy-5-methyl-4-isoxazolyl)acetic acid (AMAA), as well as substituted derivatives of these two compounds. The pharmacological...... partial agonism to antagonism with increasing substituent size, substitution abolishes affinity for mglu1 and mglu4 receptors. Ligand- and receptor-based modelling approaches assist in explaining these pharmacological trends among the metabotropic receptors and suggest a mechanism of partial agonism...