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Sample records for methyl ccnu-14c nsc

  1. Biodistribution of a 14C- and sup(99m)Tc-labeled N-substituted nitrosourea (CCNU) in an animal tumor model

    International Nuclear Information System (INIS)

    Castronovo, F.P.; Potsaid, M.S. Jr.; Kopiwoda, S.; Peterson, M.

    1980-01-01

    One formulation of 14 C labelled and another of sup(99m)Tc labelled 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea (CCNU) were administered i.v. to tumour (glioma) bearing rats. The radiopharmacokinetics of 14 C-CCNU were followed up to 24 hours post injection. On a per organ basis the blood, liver, small bowel, kidney cortex and muscle contained most of the activity. Optimum tumour to organ ratios occurred at 4-12 hours. The sup(99m)Tc-CCNU biodistribution was determined at 4 hours and compared to sup(99m)Tc-NaTcO 4 . Tumour capsule to brain (29.5) and to muscle (10.59) ratios suggest sup(99m)Tc-CCNU to be a potential tumour seeking agent. (author)

  2. Synthesis of [methyl-14C]crotonobetaine from DL-[methyl-14C]carnitine

    International Nuclear Information System (INIS)

    Loester, H.; Seim, H.

    1996-01-01

    The causes of carnitine deficiency syndromes are not completely understood, but decomposition of L-carnitine in vivo is likely to be involved. Carnitine is metabolized to γ-butyrobetaine, and crotonobetaine is probably an intermediate in this pathway. To validate experimentally the precursor-product relationship between the three physiologically occuring γ-betaines - L-carnitine, crotonobetaine, γ-butyrobetaine - labelling with stable or radioactive isotopes became necessary. Methyl-labelled carnitine isomers (L(-)-, D(+)- or DL-) or γ-butyrobetaine can be easily synthesized by methylation of 4-amino-3-hydroxybutyric acid isomers or 4-aminobutyric acid, respectively. Because of problems with the 4-aminocrotonic acid, we synthesized labelled crotonbetaine from labelled carnitine. Thus, DL-[methyl- 14 C]carnitine was dehydrated by reaction with concentrated sulfuric acid. After removal of the latter the products were separated and purified by ion exchange chromatography on DOWEX 50 WX8 (200 - 400 mesh) and gradient elution with hydrochloric acid. In addition to the labelled main product [methyl- 14 C]crotonobetaine (yield about 50 %), [methyl- 14 C]glycine betaine and [methyl- 14 C]acetonyl-trimethylammonium (ATMA) were formed. The end products were identified by combined thin layer chromatography/autoradiography and quantified by liquid scintillation counting. (Author)

  3. Synthesis of DL-adrenaline (methyl C{sup 14}) (1961); Synthese de la DL-adrenaline (methyle {sup 14}C) (1961)

    Energy Technology Data Exchange (ETDEWEB)

    Pichat, L; Audinot, M [Commissariat a l' Energie Atomique, Saclay (France). Centre d' Etudes Nucleaires

    1961-07-01

    The sodium derivative of 5-3-4 dibenzyl oxyphenyl 2-oxazolidinone reacted with methyl iodide {sup 14}C, in stoichiometric quantity, gives rise to the corresponding N-methyl {sup 14}C derivative. The oxazolidinone ring is opened by concentrated hydrochloric acid and the benzyl groups removed by catalytic hydrogenolysis. Adrenaline methyl {sup 14}C is then purified on Dowex 50 X-12 exchange resin. Overall-yield is 45 per cent based upon methyl iodide {sup 14}C. (author) [French] Le derive sode de la (dibenzyloxy-3-4-phenyl)-5 oxazolidinone-2 traite par l'iodure de methyle {sup 14}C, en proportion stoechiometrique, fournit le derive N-methyle {sup 14}C correspondant. Apres ouverture du cycle oxazolidinone par HCL concentre et debenzylation par hydrogenation catalytique, on purifie l'adrenaline (methyle {sup 14}C) par chromatographie sur resine echangeuse Dowex 50 X-12. Le rendement est de 45 pour cent par rapport a l'iodure de methyle {sup 14}C. (auteurs)

  4. Synthesis of DL-adrenaline (methyl C{sup 14}) (1961); Synthese de la DL-adrenaline (methyle {sup 14}C) (1961)

    Energy Technology Data Exchange (ETDEWEB)

    Pichat, L.; Audinot, M. [Commissariat a l' Energie Atomique, Saclay (France). Centre d' Etudes Nucleaires

    1961-07-01

    The sodium derivative of 5-3-4 dibenzyl oxyphenyl 2-oxazolidinone reacted with methyl iodide {sup 14}C, in stoichiometric quantity, gives rise to the corresponding N-methyl {sup 14}C derivative. The oxazolidinone ring is opened by concentrated hydrochloric acid and the benzyl groups removed by catalytic hydrogenolysis. Adrenaline methyl {sup 14}C is then purified on Dowex 50 X-12 exchange resin. Overall-yield is 45 per cent based upon methyl iodide {sup 14}C. (author) [French] Le derive sode de la (dibenzyloxy-3-4-phenyl)-5 oxazolidinone-2 traite par l'iodure de methyle {sup 14}C, en proportion stoechiometrique, fournit le derive N-methyle {sup 14}C correspondant. Apres ouverture du cycle oxazolidinone par HCL concentre et debenzylation par hydrogenation catalytique, on purifie l'adrenaline (methyle {sup 14}C) par chromatographie sur resine echangeuse Dowex 50 X-12. Le rendement est de 45 pour cent par rapport a l'iodure de methyle {sup 14}C. (auteurs)

  5. Synthesis of [methyl-{sup 14}C]crotonobetaine from DL-[methyl-{sup 14}C]carnitine

    Energy Technology Data Exchange (ETDEWEB)

    Loester, H.; Seim, H. [Leipzig Univ. (Germany). Inst. of Clinical Chemistry and Pathobiochemistry

    1996-02-01

    The causes of carnitine deficiency syndromes are not completely understood, but decomposition of L-carnitine in vivo is likely to be involved. Carnitine is metabolized to {gamma}-butyrobetaine, and crotonobetaine is probably an intermediate in this pathway. To validate experimentally the precursor-product relationship between the three physiologically occuring {gamma}-betaines - L-carnitine, crotonobetaine, {gamma}-butyrobetaine - labelling with stable or radioactive isotopes became necessary. Methyl-labelled carnitine isomers (L(-)-, D(+)- or DL-) or {gamma}-butyrobetaine can be easily synthesized by methylation of 4-amino-3-hydroxybutyric acid isomers or 4-aminobutyric acid, respectively. Because of problems with the 4-aminocrotonic acid, we synthesized labelled crotonbetaine from labelled carnitine. Thus, DL-[methyl-{sup 14}C]carnitine was dehydrated by reaction with concentrated sulfuric acid. After removal of the latter the products were separated and purified by ion exchange chromatography on DOWEX 50 WX8 (200 - 400 mesh) and gradient elution with hydrochloric acid. In addition to the labelled main product [methyl-{sup 14}C]crotonobetaine (yield about 50 %), [methyl-{sup 14}C]glycine betaine and [methyl-{sup 14}C]acetonyl-trimethylammonium (ATMA) were formed. The end products were identified by combined thin layer chromatography/autoradiography and quantified by liquid scintillation counting. (Author).

  6. Synthesis of [methyl-[sup 14]C]-N-methylputrescine

    Energy Technology Data Exchange (ETDEWEB)

    Secor, H.V.; Izac, R.R.; Hassam, S.B.; Frisch, A.F. (Philip Morris Research Center, Richmond, VA (United States))

    1994-05-01

    [Methyl-[sup 14]C]-N-methylputrescine was prepared from [[sup 14]C]methylamine hydrochloride in five steps. Reaction of benzaldehyde and [[sup 14]C]methylamine (10 mCi) followed by catalytic hydrogenation yielded [methyl-[sup 14]C]-N-methylbenzylamine. The key step in this process is the alkylation of [methyl-[sup 14]C]-N-methylbenzylamine in aqueous medium with 4-bromobutyronitrile. The radiochemical purity of the final product after two successive catalytic hydrogenations was in excess of 97%. The radiochemical yields in two successive runs were 26 and 38%, based on starting [[sup 14]C]methylamine, with specific activities of 22 and 23 mCi/mmol, respectively. This sequence provides a convenient and efficient regioselective radiosynthesis of [methyl-[sup 14]C]-N-methylputrescine. (author).

  7. Synthesis of 14C-labelled α-methyl tyrosine

    International Nuclear Information System (INIS)

    Rajagopal, S.; Venkatachalam, T.K.; Conway, T.; Diksic, M.

    1992-01-01

    A new route for the preparation of radioactively labelled α-methyl L-tyrosine is described. The labelling at the α position has been successfully achieved with 14 C-, 11 C- (very preliminary, unpublished), and 3 H-labelled methyl iodide. A detailed report on 14 C-labelling at the α position and the hydrolysis of 4-methoxy α-methyl phenylalanine is presented. The alkylation proceeds via the methylation of the carbanion of N-benzylidene 4-methoxy phenylalanine methyl ester 2. Hydrolysis of 4-O methyl tyrosine to tyrosine by HBr and HI were analysed and used in the optimization of the hydrolysis conditions of 4. Enantiomeric purity of the isolated L-isomer has been found to be 99% as judged by HPLC. Pseudo first-order rate constant for the hydrolysis of 14 C-labelled α-methyl 4-methoxy phenyl alanine methyl ester was determined. Preliminary findings of the 3 H- and 11 C-radiolabelled α-methyl tyrosine (methyl labelled) are also mentioned. For the first time it was shown that α-methyl D,L-tyrosine can be separated into enantiomerically pure α-methyl D- and L-tyrosine using a CHIRALPAK WH column. (author)

  8. Anaerobic C1 metabolism of the O-methyl-14C-labeled substituent of vanillate

    International Nuclear Information System (INIS)

    Frazer, A.C.; Young, L.Y.

    1986-01-01

    The O-methyl substituents of aromatic compounds constitute a C 1 growth substrate for a number of taxonomically diverse anaerobic acetogens. In this study, strain TH-001, an O-demethylating obligate anaerobe, was chosen to represent this physiological group, and the carbon flow when cells were grown on O-methyl substituents as a C 1 substrate was determined by 14 C radiotracer techniques. O-[methyl- 14 C]vanillate (4-hydroxy-3-methoxy-benzoate) was used as the labeled C 1 substrate. The data showed that for every O-methyl carbon converted to [ 14 C]acetate, two were oxidized to 14 CO 2 . Quantitation of the carbon recovered in the two products, acetate and CO 2 , indicated that acetate was formed in part by the fixation of unlabeled CO 2 . The specific activity of 14 C in acetate was 70% of that in the O-methyl substrate, suggesting that only one carbon of acetate was derived from the O-methyl group. Thus, it is postulated that the carboxyl carbon of the product acetate is derived from CO 2 and the methyl carbon is derived from the O-methyl substituent of vanillate

  9. Synthesis of methyl-2 O-tolyl-3 quinazolone-4 {sup 14}C-2; Synthese de la methyl-2 O-tolyl-3 quinazolone-4 {sup 14}C-2

    Energy Technology Data Exchange (ETDEWEB)

    Herbert, M; Pichat, L [Commissariat a l' Energie Atomique, Saclay (France).Centre d' Etudes Nucleaires

    1959-07-01

    Description of the preparation of methyl-2 O-tolyl-3 quinazolone-4 {sup 14}C-2 (abbreviated to M.T.Q.), using N-acetyl {sup 14}C-1 anthranilic acid. The overall yield reaches 72 per cent with respect to acetyl chloride {sup 14}C-1. By applying the same method to acetyl chloride {sup 14}C-2, M.T.Q. labelled on the methyl group could be obtained. (author) [French] Description de la preparation de la methyl-2 O-tolyl-3 quinazolone-4 {sup 14}C-2 (abregee en M.T.Q.) par l'intermediaire de l'acide N-acetyl {sup 14}C-1 anthranilique. Le rendement global atteint 72 pour cent par rapport au chlorure d'acetyle {sup 14}C-1. La meme methode appliquee au chlorure d'acetyle {sup 14}C-2 permettrait d'obtenir la M.T.Q. marquee sur le groupement methyle. (auteur)

  10. Synthesis of [5,6-13C2, 1-14C]olivetolic acid, methyl [1'-13C]olivetolate and [5,6-13C2, 1-14C]cannabigerolic acid

    International Nuclear Information System (INIS)

    Porwoll, J.P.; Leete, E.

    1985-01-01

    Potential advanced intermediates in the biosynthesis of delta 9 -tetrahydrocannabinol, the major psychoactive principle of marijuana, have been synthesized labeled with two contiguous 13 C atoms and 14 C. Methyl [5,6- 13 C 2 , 1- 14 C]olivetolate was prepared from lithium [ 13 C 2 ]acetylide and dimethyl [2- 14 C]malonate. Reaction with geranyl bromide afforded methyl [5,6- 13 C 2 , 1- 14 C]cannabigerolate, and hydrolysis of these methyl esters with lithium propyl mercaptide yielded the corresponding labeled acids. The 13 C- 13 C couplings observable in the 13 C NMR spectra of these 13 C-enriched compounds and their synthetic precursors are recorded. Methyl [1'- 14 C]olivetolate was prepared from 13 CO 2 to confirm assignments of the 13 C chemical shifts in the pentyl side chain of these compounds. (author)

  11. Synthesis of specific labelled [methyl-14C]sarin

    International Nuclear Information System (INIS)

    Sin-Ren, A.C.; Riggio, G.; Hopff, W.H.; Waser, P.G.

    1988-01-01

    The synthesis of [methyl- 14 C]sarin ([ 14 C]methylphosphono-fluoridic acid 1-methylethyl ester) was accomplished by another approach as for nonlabelled sarin in a tele-conducted reaction vessel. The purity was estimated by IR, GC, and GC-MS and the stability in different media was examined. (author)

  12. Intravenous elimination and percutaneous absorption of topically applied thioguanine-14c (nsc-752) in yorkshire white pigs. Final report, 22 June-14 October 1977

    International Nuclear Information System (INIS)

    Skierkowski, P.; Murphy, J.C.; Watson, E.S.; Folk, R.M.; Pavkov, K.L.

    1978-01-01

    The distribution and elimination of intravenously administered Thioguanine-14C (NSC-752) was studied in female, weanling, Yorkshire, white pigs. Approximately one-half the radioactivity was eliminated in the urine in the first six hours, and the majority was eliminated by the end of the 24 hours after intravenous administration. After 96 hours (4 days) an average of 84% was eliminated via the urine. This elimination percentage was then utilized to determine the amount of Thioguanine-14C absorbed after topical application. Among the whole organs sampled, kidney, liver and spleen had the highest specific activities of radioactivity. Intestine and bone marrow samples had the highest specific activity levels of the random tissues sampled. The absorption of the Thioguanine-14C after topical application was minimal with approximately 0.77% of the administered dose being absorbed at the end of 192 hours (8 days). Significant levels of radioactivity were also detected in skin surrounding the site of application

  13. Radiation plus adjuvant CCNU (1-[2-chloroethyl]-3-cyclohexyl-1-nitrosourea) vs CCNU, hydroxyurea and vincristine in the treatment of malignant glioma

    International Nuclear Information System (INIS)

    Costanza, M.; Buechler, M.; Munzenreider, J.

    1979-01-01

    Following maximal surgery, 25 patients with malignant glioma were randomized to receive either radiation therapy and CCNU or radiation therapy and CCNU, hydroxyurea, and vincristine. Radiation therapy included 4000 rad to whole brain followed by 1500 rad to the primary. Chemotherapy was either: CCNU alone 130 mg/m 2 PO every 6 weeks or triple drug chemotherapy given in 6 week cycles of CCNU 90 mg/m 2 PO (one dose), vincristine 1 mg/m 2 IV (one dose), and hydroxyurea 1.5 gm/m 2 PO every 3 days x 7 doses. Thirteen patients received CCNU alone. Of these, 8 are dead, 2 are alive with progressive disease and 3 are alive with stable disease at 10, 22, and 23 months. Median survival is 10 months. Twelve patients received CCNU, vincristine and hydroxyurea. Of these, 8 are dead, 1 is alive with progressive disease and 3 are stable. Median survival is 9.5 months +. Toxicity included nausea, which was common, leukopenia < 3000 in 7 patients and thrombocytopenia in 9 patients. There were no episodes of bleeding or infection attributable to chemotherapy. Although toxicity was tolerable, no additional benefit could be demonstrated for triple agent chemotherapy with CCNU, vincristine and hydroxyurea compared to CCNU alone. Median survival for both groups was similar at 42 to 44 weeks

  14. Synthesis of two S-(methyl-3H)-labelled enkephalins and S-(methyl-14C) substance P

    International Nuclear Information System (INIS)

    Naegren, K.; Laangstroem, B.; Franzen, H.M.; Ragnarsson, U.

    1988-01-01

    The synthesis of 3 H-labelled Met-enkephalin and Tyr-D-Ala-Gly-Phe-Met-NH 2 (DALA) and 14 C-labelled Substance P (SP) from previously described, fully protected intermediates is reported. The labelled peptides were prepared by methylation with ( 3 H)- or ( 14 C)methyl iodide of the sulphide anions formed on deprotection of the corresponding S-benzyl-homocysteine precursors with sodium in liquid ammonia. After purification by LC, the labelled peptides were obtained in radiochemical yields in the range of 9 to 24% with a radiochemical purity higher than 97%. The specific radioactivities of the 3 H- and 14 C- labelled products, corresponding to the labelled methyl iodides used, were 80 mCi/μmol and 60 μCi/μmol, respectively. (author)

  15. Uptake and distribution of 14C during and following exposure to [14C]methyl isocyanate

    International Nuclear Information System (INIS)

    Ferguson, J.S.; Kennedy, A.L.; Stock, M.F.; Brown, W.E.; Alarie, Y.

    1988-01-01

    Guinea pigs were exposed to [ 14 C]methyl isocyanate ( 14 CH 3 -NCO, 14 C MIC) for periods of 1 to 6 hr at concentrations of 0.5 to 15 ppm. Arterial blood samples taken during exposure revealed immediate and rapid uptake of 14 C. Clearance of 14 C was then gradual over a period of 3 days. Similarly 14 C was present in urine and bile immediately following exposure, and clearance paralleled that observed in blood. Guinea pigs fitted with a tracheal cannula and exposed while under anesthesia showed a reduced 14 C uptake in blood indicating that most of the 14 C MIC uptake in normal guinea pigs occurred from retention of this agent in the upper respiratory tract passages. In exposed guinea pigs 14 C was distributed to all examined tissues. In pregnant female mice similarly exposed to 14 C MIC, 14 C was observed in all tissues examined following exposure including the uterus, placenta, and fetus. While the form of 14 C distributed in blood and tissues has not yet been identified, these findings may help to explain the toxicity of MIC or MIC reaction products on organs other than the respiratory tract, as noted by several investigators

  16. Mineralization of 14C-Pirimiphos-Methyl in Soil Under Aerobic and Anaerobic Conditions

    International Nuclear Information System (INIS)

    Zayed, S.M.A.D.; Farghly, M.; El-Maghrby, S.

    2006-01-01

    The mineralization of 14 C-ring labelled pirimiphos-methyl in clay loam soil was determined in a three months laboratory incubation period under anaerobic and aerobic conditions. Evolution of 14 CO2 increased with time and reached 9.2% and 12 %, of the initial 14 C-concentration , within 90 days in case of anaerobic and aerobic conditions, respectively, at that time, soil contained about 61.5% of the applied dose as extractable residues under anaerobic conditions and 59% under aerobic conditions. the unextractable pesticide residues gradually increased with time and the highest binding capacity of about 11%-13% was observed after 90 days of incubation. the total 14 C-activity recovered from soil was generally between 82% and 92% of the applied radiocarbon. the nature of methanolic 14 C-residues was determined by chromatographic analysis and the results revealed the presence of pirimiphos- methyl as a main product together with its phenol. the principle of radio-respirometry has been used for evaluating the effect of different application rates of pirimiphos-methyl on soil microbial activity using U- 14 C-glucose as a substrate. At two concentrations used, pirimiphos-methyl showed an inhibition in the rate of 14 Co2 evolution over 14 days of incubation as a result of oxidation of 14 C-glucose by microorganisms especially in case of high concentration

  17. Synthesis of (5,6-/sup 13/C/sub 2/, 1-/sup 14/C)olivetolic acid, methyl (1'-/sup 13/C)olivetolate and (5,6-/sup 13/C/sub 2/, 1-/sup 14/C)cannabigerolic acid

    Energy Technology Data Exchange (ETDEWEB)

    Porwoll, J P; Leete, E [Minnesota Univ., Minneapolis (USA). Dept. of Chemistry

    1985-03-01

    Potential advanced intermediates in the biosynthesis of delta/sup 9/-tetrahydrocannabinol, the major psychoactive principle of marijuana, have been synthesized labeled with two contiguous /sup 13/C atoms and /sup 14/C. Methyl (5,6-/sup 13/C/sub 2/, 1-/sup 14/C)olivetolate was prepared from lithium (/sup 13/C/sub 2/)acetylide and dimethyl (2-/sup 14/C)malonate. Reaction with geranyl bromide afforded methyl (5,6-/sup 13/C/sub 2/, 1-/sup 14/C)cannabigerolate, and hydrolysis of these methyl esters with lithium propyl mercaptide yielded the corresponding labeled acids. The /sup 13/C-/sup 13/C couplings observable in the /sup 13/C NMR spectra of these /sup 13/C-enriched compounds and their synthetic precursors are recorded. Methyl (1'-/sup 14/C)olivetolate was prepared from /sup 13/CO/sub 2/ to confirm assignments of the /sup 13/C chemical shifts in the pentyl side chain of these compounds.

  18. Autoradiographic disposition of [1-methyl-14C]- and [2-14C]caffeine in mice

    International Nuclear Information System (INIS)

    Lachance, M.P.; Marlowe, C.; Waddell, W.J.

    1983-01-01

    Male, C57B1/6J mice received either [1-methyl-14C]caffeine or [2-14C]caffeine via the tail vein at a dose of 0.7 or 11 mg/kg, respectively. At 0.1, 0.33, 1, 3, 9, and 24 hr after treatment, the mice were anesthetized with ether and frozen by immersion in dry ice/hexane. The mice were processed for whole-body autoradiography by the Ullberg technique; this procedure does not allow thawing or contact with solvents. All autoradiographs revealed some retention of radioactivity at early time intervals in the lacrimal glands, seminal vesicle fluid, nasal and olfactory epithelium, and retinal melanocytes. The remaining portion of the animal was densitometrically uniform except for the lower levels noted in the CNS and adipose tissues. Excretion of radioactivity by the liver and kidneys seems to be the major routes of elimination. Localization in the liver at late time intervals was confined principally to the centrilobular region. Late sites of retention, observed only after [1-methyl-14C]caffeine administration, included the pancreas, minor and major salivary glands, splenic red pulp, thymal cortex, bone marrow, and gastrointestinal epithelium. Sites of localization present in both studies included the olfactory epithelium, lacrimal glands, hair follicles, and retinal melanocytes. Further studies are needed to determine whether the localization at these various sites is due to metabolic degradation, active transport, or possibly a specific receptor interaction

  19. Synthesis of (5,6-/sup 13/C/sub 2/, 1-/sup 14/C)olivetolic acid, methyl (1'-/sup 13/C)olivetolate and (5,6-/sup 13/C/sub 2/, 1-/sup 14/C)cannabigerolic acid

    Energy Technology Data Exchange (ETDEWEB)

    Porwoll, J.P.; Leete, E. (Minnesota Univ., Minneapolis (USA). Dept. of Chemistry)

    1985-03-01

    Potential advanced intermediates in the biosynthesis of delta/sup 9/-tetrahydrocannabinol, the major psychoactive principle of marijuana, have been synthesized labeled with two contiguous /sup 13/C atoms and /sup 14/C. Methyl (5,6-/sup 13/C/sub 2/, 1-/sup 14/C)olivetolate was prepared from lithium (/sup 13/C/sub 2/)acetylide and dimethyl (2-/sup 14/C)malonate. Reaction with geranyl bromide afforded methyl (5,6-/sup 13/C/sub 2/, 1-/sup 14/C)cannabigerolate, and hydrolysis of these methyl esters with lithium propyl mercaptide yielded the corresponding labeled acids. The /sup 13/C-/sup 13/C couplings observable in the /sup 13/C NMR spectra of these /sup 13/C-enriched compounds and their synthetic precursors are recorded. Methyl (1'-/sup 14/C)olivetolate was prepared from /sup 13/CO/sub 2/ to confirm assignments of the /sup 13/C chemical shifts in the pentyl side chain of these compounds.

  20. Intravenous elimination and percutaneous absorption of topically applied melphalan-14C (NSC-8806) in Yorkshire white pigs. Final report, 17 August-1 December 1977

    International Nuclear Information System (INIS)

    Skierkowski, P.; Murphy, J.C.; Watson, E.S.; Folk, R.M.; Pavkov, K.L.

    1978-01-01

    The distribution and elimination of intravenously administered Melphalan-14C (NSC-8806) was studied in female, weanling Yorkshire white pigs. A three compartment pharmacokinetic model is indicated with a very slow elimination phase (half life = 214 hours). Assay of tissue samples indicate bone and fat may be acting as depots for the drug. After 8 days an average of 70% was eliminated via the urine. Percutaneous studies showed an average of 4.02% of the applied dose was absorbed after 14 days. Significant levels of radioactivity were also detected in skin surrounding the site of application

  1. Synthesis of 1-(2,3-dihydroxypropyl)-2-nitro-1H-imidazole-2-14C and N-(2-hydroxyethyl)-2-(2-nitro-1H-imidazol-1-YL-2-14C)acetamide

    International Nuclear Information System (INIS)

    Fong, M.T.; Leaffer, M.A.

    1986-01-01

    We have prepared the 14 C-labeled analogs of NSC 261036, 1-(2,3-dihydroxypropyl)-2-nitro-1H-imidazole-2- 14 C, and NSC 301467, N-(2-hydroxyethyl)-2-(2-nitro-1H-imidazol-1-yl-2- 14 C) acetamide, for pharmacological, drug distribution, and mechanisms of action studies. The latter is an analog designed for lower toxicity and improved properties. The former is a metabolite of, and appears to be less toxic than, misonidazole. (author)

  2. Effect of pesticide applications on soil microbial activity and on 14C-methyl parathion dissipation

    International Nuclear Information System (INIS)

    Peres, Terezinha Bonanho

    2000-01-01

    Some crops, as cotton, need different pesticide application to control pests and diseases. These compounds reach soil and may affect the soil microbial activity. As the microorganisms play important role on the nutrient cycling, changes in their activities may affect the soil fertility. The influence of several pesticides on soil microbial activity of the 0-15 cm and 15-30 cm depth of the soil profile, and the 14 C-methyl parathion dissipation was studied under influence of other pesticide applications. The influence of pesticides on the microorganisms was followed in an experimental area of the Instituto Biologico, that was divided in two subareas, both under cotton crop. Columns of PVC was buried in both subareas and a solution of 14 C-methyl parathion diluted in the technical compound was applied on the soil surface of each column. One subarea received all the recommended pesticides for the cotton crop besides the 14 C-methyl parathion. The other subarea received only 14 C-methyl parathion solution on the columns soil surface. The soil microbial activity of both subareas was estimated by measurements of dehydrogenase, arylsulfatase and arginine deaminase enzymes. Further, the availability of total nitrogen in the soil was also measured. The dissipation of 14 C-methyl parathion was studied by radiocarbon recovery in soil extracts and combustion of extracted soil and quantification by radiometric techniques. (author)

  3. A convenient photosynthesis of uniformly [14C]-labelled D-glucose, D-fructose and sucrose, and chemical synthesis of methyl-α-D-glucopyranoside ([U-14C]-glucose)

    International Nuclear Information System (INIS)

    Srinivas, G.; Unny, V.K.P.; Mukkanti, K.; Choudary, B.M.

    2013-01-01

    This paper describes a convenient procedure for the radiochemical preparation of D-[U- 14 C]-glucose, D-[U- 14 C]-fructose and [U- 14 C]-sucrose with high specific activity by photosynthesis using ‘canna indica’ leaf, [ 14 C]-carbon dioxide and water in presence of light in a closed system. The [ 14 C]-sugars formed were extracted, separated and then purified by paper chromatography. Further, the pure D-[U- 14 C]-glucose obtained was converted to methyl-α-D-glucopyranoside ([U- 14 C]-glucose) by glycosidation with methanol using (i) HCl, the conventional Fischer method (ii) heterogeneous organic cation exchange resin (Amberlite IR-120 (H + )) and (iii) heterogeneous inorganic cation exchanged montmorillonites called metal M +n -monts. The results indicated that the latter in the form of Fe +3 -montmorillonite gave a better yield ( 65%) as compared to others (40–56%). The radiochemical purity of the no-carrier added product was more than 98%. The product retained its specific activity as that of the starting material which is in the range of 250–300 mCi/mmole (9.25–11.1 GBq/mmole), suitable for use as a radiotracer in biochemical investigations. - Graphical abstract: A convenient photosynthesis of uniformly [ 14 C]-labelled D-glucose, D-fructose and sucrose, and chemical synthesis of methyl-α-D-glucopyranoside ([U- 14 C]-glucose)/[ 14 C]–AMG, in short. The photosynthesis of D-[U- 14 C]-glucose, and two other [ 14 C]-sugars (fructose and sucrose) with high specific activity using ‘Canna indica’ leaf, 14 CO 2 and water in presence of light is presented in this paper. Further, the D-[U- 14 C]-glucose obtained was converted to methyl-α-D-glucopyranoside ([U- 14 C]-glucose)/[ 14 C]–AMG having 98% radiochemical purity and specific activity in the range of 250–300 mCi/mmole, using montmorillonites (M +n -monts). Highlights: ► Synthesis of methyl α D-glucopyranoside ([U- 14 C] glucose) has not been reported using M +n -monts. ► M +n -monts are

  4. Cytotoxic properties of a 4-nitroimidazole (NSC 38087): a radiosensitizer of hypoxic cells in vitro

    International Nuclear Information System (INIS)

    Stratford, I.J.; Williamson, C.; Hardy, C.

    1981-01-01

    5-Phenoxysulphonyl-1-methyl-4-nitroimidazole (NSC 38087) can act as a sensitizer of hypoxic mammalian cells to radiation in vitro. The degree of sensitization achieved is greater than would be predicted from the drug's electron affinity. Cytotoxicity studies have shown that 5sub(μM) NSC 38087 can reduce the surviving fraction of log-phase V79 cells in air at 37 0 C to 10 -2 after 2 h exposure. This toxicity is considerably increased by small rises in temperature. In contrast to other nitroheterocyclic radiosensitizers, NSC 38087 and related 5-substituted 4-nitroimidazoles show greater toxicity towards aerobic than to hypoxic cells. Log-phase cells show the highest sensitivity to the toxic action of NSC 38087, with plateau-phase cells, cells with a history of chronic hypoxia, and thermotolerant cells showing greater resistance. These toxicity data are compared to those for the 2-nitroimidazole hypoxic-cell sensitizer misonidazole. (author)

  5. Phase I study of the combination of benznidazole and CCNU in man

    International Nuclear Information System (INIS)

    Roberts, J.T.; Bleehen, N.M.; Lee, F.Y.F.; Workman, P.; Walton, M.I.

    1984-01-01

    The 2-nitroimidazole benznidazole (BENZO) has previously been shown to be an effective potentiator of the cytotoxicity of CCNU in mice, at levels which are achievable in man. In this study BENZO has been given to 46 patients in oral doses of 4 mg/kg to 30 mg/kg, and drug concentrations measured in plasma, urine, tumor and normal brain by HPLC. Approximately 60% of the drug was bound to plasma proteins and 6% excreted unchanged in urine. Mean tumor/plasma ratios of 88% for 11 gliomas and 72% for 6 superficially accessible non-brain tumors were obtained while that for normal brain was 69%. Doses of more than 17 mg/kg BENZO produce changes in the plasma pharmacokinetics of CCNU, increasing the half life of active hydroxylated metabolites. In addition, CCNU parent compound is present. This is not seen when CCNU is given alone. Such changes may result in improved response rates as it is possible to achieve in man, plasma and tumor levels of BENZO, which in the mouse model produce effective enhancement of the response to CCNU

  6. Enhanced tumor responses through therapies combining CCNU, MISO and radiation

    International Nuclear Information System (INIS)

    Siemann, D.W.; Hill, S.A.

    1984-01-01

    Studies were performed to determine whether the radiation sensitizer misonidazole (MISO) could enhance the tumor control probability in a treatment strategy combining radiation and the nitrosourea 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea (CCNU). In initial experiments KHT sarcoma-bearing mice were injected with 1.0 mg/g of MISO simultaneously with a 20 mg/kg dose of CCNU 30-40 min prior to irradiation (1500 rad). With this treatment protocol approximately 60% of the mice were found to be tumor-free 100 days post treatment. By comparison all 2 agent combinations led to 0% cures. To evaluate the relative importance of chemopotentiation versus radiosensitization in the 3 agent protocol, tumors were treated with MISO plus one anti-tumor agent (either radiation of CCNU) and then at times ranging from 0 to 24 hr later exposed to the other agent. When the time between treatments was 0 to 6 hr, a 60 to 80% tumor control rate was achieved for both MISO plus radiation followed by CCNU and MISO plus CCNU followed by radiation. However if the time interval was increased to 18 or 24 hr, the cure rate in the former treatment regimen dropped to 10% while that of the latter remained high at 40%. The data therefore indicate that (1) improved tumor responses may be achieved when MISO is added to a radiation-chemotherapy combination and (2) MISO may be more effective in such a protocol when utilized as a chemopotentiator

  7. Studies of pirimiphos-methyl residues in stored rice, using 14C-pirimiphos-methyl

    International Nuclear Information System (INIS)

    Varca, L.M.; Sanchez, T.E.; Gambalan, N.; Magallona, E.D.

    1990-01-01

    The distribution and persistence of pirimiphos-methyl on rice (hulled and unhulled) stored over a period of 6 months at 30 deg. C and about 11% moisture were studied using 14 C labelled insecticide. The procedures used for preparing the labelled formulation, applying the insecticide and for the handling and analysis of the grain samples were similar to those described for fenvalerate, see Varca, Sanchez and Magallona, ''Isotopic tracer aided studies of fenvalerate residues in stored products'', these Proceedings. After applying the pirimiphos-methyl, a concentration equal to 0.87 ppm was found on the hulled rice immediately after application; this concentration declined to 0.60 ppm after 6 months of storage. Over 28% of the residue was present in the seed in the methanol extractable form, and 38% was found on the surface at the end of the storage period. For the unhulled rice, most of the residue was retained in the hull with no decrease in the overall level during the storage period. (author)

  8. Synthesis of methyl 3-O-{alpha}-d-glucopyranosyl-C{sub 6}{sup 14}-{beta}-d-xylopyranoside and methyl 2-O-{alpha}-d-Glucopyranosyl-C{sub 6}{sup 14}-l-noviopyranoside; Synthese de methyl-3-O-alpha-D-glucopyranosyl-C{sup 14}-beta-D-xylophranoside et methyl-2-O-alpha-D-glucopyranosyl-C{sub 6}{sup 14}-L-noviopyranoside; Sintez metil-3-O-{alpha}-D-glyukopiranozila-C{sub 6}{sup 14}-{beta}-D-ksilopiranozid i metil 2-O-{alpha}-D-glyukopiranozil-C{sub 6}{sup 14}-L-noviopiranozid; Sintesis de la metil 3-O-{alpha}-D-glucopiranosil-{sup 14}C{sub 6}-{beta}-D-xilopiranosido y de la metil 2-O-{alpha}-D-glucopiranosil-{sup 14}C{sub 6}-L-noviopiranosido

    Energy Technology Data Exchange (ETDEWEB)

    Barker, S A; Keith, M C; Stacey, M; Stroud, D B.E. [Chemistry Department, University of Birmingham (United Kingdom)

    1962-03-15

    Where difficulty is encountered in the chemical synthesis of a disaccharide glycoside labelled with C{sub 6}{sup 14} specifically in only one of its sugar moieties it is often convenient to resort to a synthesis catalysed by microbial transglycosylases. Two examples of the application of this technique are reported; the syntheses: Maltose-C{sub 12}{sup 14} + Methyl {beta}-d-xylopyranoside Penicillium lilacinum/transglucosylase {yields} Methyl 3-0-{alpha}-d-Glucopyranosyl-C{sub 6}{sup 14}-{beta}-d-xylopyranoside (I) + Glucose-C{sub 6}{sup 14} Maltose-C{sub 12}{sup 14} + Methyl l-noviopyranoside Fusarium moniliforme/transglucosylase Methyl-2-0-{alpha}d-Glucopyranosyl-C{sub 6}{sup 14}-l-noviopyranoside (II) + Glucose-C{sub 6}{sup 14}. In such syntheses, it is predictable that the anomeric character of the glycosidic linkage of the donor disaccharide will be retained in the disaccharide synthezised and that the glycosyl residue transferred will be attached, through its reducing group, to the receptor monosaccharide glycoside. By using either a C{sup 14}-labelled donor disaccharide or a C{sup 14}-labelled receptor glycoside, a disaccharide can be synthesized with only one of its sugar moieties labelled. In the synthesis of II the only hydroxyl group free in the receptor methyl novioside is on C{sub 2} and the transferred glucosyl residue can only be attached here. In the synthesis of I the methyl xyloside has free hydroxyls on C{sub 2}, C{sub 3} and C{sub 4} and the microbial enzyme has been found to transfer the glucosyl residue specifically to the hydroxyl on C{sub 3}. The structures of I and I I have been established by the results of elemental analysis, optical rotation, infrared spectra together with an examination of the products of acid hydrolysis and periodate oxidation. (author) [French] Lorsqu'on se heurte a des difficultes dans la synthese chimique d'un glucoside de disaccharide marque au carbone-14 specifiquement dans un seul des deux sucres qui le

  9. The incorporation of [1-14C] acetate into the methyl ketones that occur in steam-distillates of bovine milk fat.

    Science.gov (United States)

    Lawrence, R C; Hawke, J C

    1966-01-01

    1. The (14)C-labelling of the fatty acids and the methyl ketones in steam-distillates of milk fat from a lactating cow that had been injected intravenously with [1-(14)C]acetate was determined. 2. The labelling patterns of the C(6)-C(16) fatty acids and the corresponding methyl ketones with one fewer carbon atoms were similar, particularly so for the C(5)-C(10) compounds at 9 and 22hr. after the injection of [1-(14)C]acetate. The isolation of (14)C-labelled methyl ketones in the range C(3)-C(15) is evidence that the beta-oxo acid precursors, which are glyceride-bound in the milk fat, are synthesized in the mammary gland from acetate. The absence of heptadecan-2-one in steam-distillates and the extremely low specific radioactivity of stearic acid are further evidence for this biosynthetic pathway. 3. The specific radioactivities of the C(5)-C(15) methyl ketones were higher (with the exception of C(9) methyl ketone in the second milking) than the specific activities of the corresponding fatty acids with one more carbon atom. This is consistent with the methyl ketone precursors' being formed during the biosynthesis of fatty acids rather than being products of beta-oxidation of fatty acids.

  10. Distribution of 14C after oral administration of [U-14C]labeled methyl linoleate hydroperoxides and their secondary oxidation products in rats

    International Nuclear Information System (INIS)

    Oarada, M.; Miyazawa, T.; Kaneda, T.

    1986-01-01

    To study the toxicity of low molecular weight (LMW) compounds formed during the autoxidation of oils, 14 C-labeled primary monomeric compounds (methyl linoleate hydroperoxides) and secondary oxidation products, i.e., polymer and LMW compounds prepared from autoxidized methyl [U- 14 C]linoleate hydroperoxides (MLHPO) were orally administered to rats, and their radioactive distributions in tissues and organs were compared. The polymeric fraction consisted mainly of dimers of MLHPO. For the LMW fraction, 4-hydroxy-2-nonenal, 8-hydroxy methyl octanoate and 10-formyl methyl-9-decenoate were identified as major constituents by gas chromatography-mass spectrometry (GC-MS) after chemical reduction and derivatization. When LMW compounds were administered to rats, 14 CO 2 expiration and the excreted radioactivity in urine in 12 hr were significantly higher than those from polymer or MLHPO administration. Maximum 14 CO 2 expiration appeared 2-4 hr after the dose of LMW compounds. Radioactivity of the upper part of small intestines six hr after the dose of LMW compounds was higher than the values from administered polymer or MLHPO. The remaining radioactivity in the digestive contents and feces 12 hr after administration of LMW compounds was much lower than the values observed from administered polymer or MLHPO. Among internal organs, the liver contained the highest concentration of radioactivities from polymer, MLHPO and LMW fractions, and an especially higher level of radioactivity was found in liver six hr after the administration of LMW compounds. Six hours after the dose of LMW compounds, a relatively higher level of radioactivity also was detected in kidney, brain, heart and lung

  11. The autoradiolytic and the γ-induced demethylation of solid thymine-(methyl-14C)

    International Nuclear Information System (INIS)

    Merwitz, O.

    1980-01-01

    The autoradiolytic and the γ-induced demethylation of solid thymine were measured qualitatively and quantitatively for the first time with specially purified thymine-(methyl- 14 C). Analogous experiments with thymine-(methyl- 3 H) and radio-gaschromatographic analysis provided proof for the formation of molecular hydrogen and methane. Ethane was not detected. The results are discussed in connection with e.s.r.-spectroscopic studies. (author)

  12. Synthesis of [21-14C]-fusarin C by enzymic demethylation and remethylation with [14C]-diazomethane

    International Nuclear Information System (INIS)

    Lu, S.-J.; Li, M.H.

    1989-01-01

    Fusarin C, a potent mutagen isolated from Fusarium moniliforme culture extracts, has been prepared radiolabeled in two steps by enzymic hydrolysis of the 21-methyl ester group, using phenobarbital induced microsomal preparations, followed by remethylation using [ 14 F]-diazomethane. Yields, based upon fusarin C, were essentially quantitative and approximately 10% of the [ 14 C]-methyl-nitrosourea, converted to diazomethane, reacted to yield [ 14 C]-fusarin C. (author)

  13. Syntheses of [6-14C] and [5-carboxy, 6-14C2]nitrendipine

    International Nuclear Information System (INIS)

    Maul, N.; Scherling, D.

    1989-01-01

    [6- 14 C]Nitrendipine synthesis started from barium[ 14 ]carbonate, which was converted to [1- 14 C]acetyl chloride. The acid chloride was condensed with Meldrum's acid (2,2-dimethyl-1,3-dioxane-4,6-dione). The resulting intermediate was treated with boiling methanol to give methyl [3- 14 C]acetoacetate. The reaction with gaseous ammonia in toluene yielded the corresponding methyl 3-amino[3- 14 C]crotonate which was condensed with ethyl 2-(3-nitro-benzylidene) acetoacetate to obtain [6- 14 C]nitrendipine. (author)

  14. Synthesis of pinacolyl [14C]methylphosphonochloridate

    International Nuclear Information System (INIS)

    Horvat, J.; Keglevic, D.; Klaic, B.; Kveder, S.; Ladesic, B.; Cosic, M.; Zupanc, S.

    1982-01-01

    A three-step synthetic route to pinacolyl [ 14 C]methylphosphonochloridate (3) from [ 14 C]methyl iodide is described. Condensation of sodium di-n-butyl phosphite with [ 14 C]methyl iodide gave di-n-butyl [ 14 C]methylphosphonate (1) which was converted into [ 14 C]methylphosphonic dichloride (2) by prolonged refluxing with thionyl chloride. Reaction of 2 with pinacolyl alcohol in the presence of N,N-di-n--propylaniline as the base afforded the title compound 3. The radiochemical yield of redistilled 3 was 34,2% based on 1, and the overall radiochemical yield was 20,0% from [ 14 C]methyl iodide. (author)

  15. Synthesis of 7-[α-(2-amino-[2-14C]thiazol-4-yl)-α-(Z)-methoxyimin oacetamido]-3-(1-methylpyrrolidinio)methyl-3-cephem-4-carboxylate hydrochloride ([14C]cefepime hydrochloride)

    International Nuclear Information System (INIS)

    Standridge, R.T.; Swigor, J.E.

    1993-01-01

    The title compound ([ 14 C]cefepime hydrochloride) was prepared as follows:- [ 14 C]Thiourea was condensed with ethyl 4-bromo-3-oxo-2-methoxyimino-acetate providing ethyl 2-(2-amino-4-[2- 14 C] thiazolyl)-2-methoxyi-minoacetate as the pure Z-isomer. Saponification gave the amino acid this was reacted with 1-hydroxybenzotriazole to give the activated ester. Condensation in situ with 7-amino-3-(1-methylpyrrolidinio) methyl-3-cephem-4-carboxylate yielded the product as the pure sulfate salt. Treatment of the sulfate salt with base provided the zwitterion isolated as the stable N-methyl-2-pyrrolidinone adduct. An aqueous solution of the adduct was converted to the crystalline title compound, [ 14 C]Cefepime hydrochloride hydrate, with hydrochloric acid/acetone. Radiochemical purity was 99.0% and specific activity, 34.2 μCi/mg. Overall yield from [ 14 C]thiourea was 18%. (Author)

  16. Synthesis of [3-14C]- and [phenyl-U-14C] olaquindox

    International Nuclear Information System (INIS)

    Maul, W.; Scherling, D.; Seng, F.

    1981-01-01

    Olaquindox is a new feed additive. [ 14 C]Olaquindox, labelled in different positions, was needed for tracer-studies of pharmacokinetics, biotransformation and residues in several species of animals. 2-[N-(2-hydroxethyl)-carbamoyl]-3-methyl-[3- 14 C]quinoxaline-1,4-dioxide([3- 14 C]Olaquindox) was synthesized from barium[ 14 C]carbonate (22 mmoles; 1.15 Ci) via [1- 14 C]acetic acid, sodium[1- 14 C]acetate, [1- 14 C]acetylchloride, ethyl[3- 14 C]acetoacetate and 2-carbethoxy-3-methyl-[3- 14 C]quinoxaline-1,4-dioxide with an overall yield of 10%, based on barium[ 14 C]carbonate. The radiochemical purity was better than 98% (tlc). The specific activities of three preparations were 10.5, 8.4 and 5.45 μCi/mg respectively. [phenyl-U- 14 C]Olaquindox was synthesized starting from [U- 14 C]aniline (19.8 mmoles; 284.4 mCi). Intermediate products were N-acetyl[U- 14 C]aniline, 2-nitro-N-acetyl[U- 14 C]aniline, 2-nitro[U- 14 C]aniline and [U- 14 C]benzofurazanoxide. The total yield was 50% as calculated for [U- 14 C]aniline. At calibration samples of two preparations showed specific activities of 49.5 and 11.1 μCi/mg respectively. The radiochemical purity was checked by tlc and exceeded 98%. (author)

  17. Stereoselective synthesis of the Halaven C14-C26 fragment from D-quinic acid: crystallization-induced diastereoselective transformation of an α-methyl nitrile.

    Science.gov (United States)

    Belanger, Francis; Chase, Charles E; Endo, Atsushi; Fang, Francis G; Li, Jing; Mathieu, Steven R; Wilcoxen, Annie Z; Zhang, Huiming

    2015-04-20

    Crystallization-induced diastereoselective transformation (CIDT) of an α-methyl nitrile completes an entirely non-chromatographic synthesis of the halichondrin B C14-C26 stereochemical array. The requisite α-methyl nitrile substrate is derived from D-quinic acid through a series of substrate-controlled stereoselective reactions via a number of crystalline intermediates that benefit from a rigid polycyclic template. Therefore, all four stereogenic centers in the Halaven C14-C26 fragment were derived from the single chiral source D-quinic acid. © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  18. Degradation of Triazine-2-(14C Metsulfuron-Methyl in Soil from an Oil Palm Plantation.

    Directory of Open Access Journals (Sweden)

    B S Ismail

    Full Text Available Triazine-2-(14C metsulfuron-methyl is a selective, systemic sulfonylurea herbicide. Degradation studies in soils are essential for the evaluation of the persistence of pesticides and their breakdown products. The purpose of the present study was to investigate the degradation of triazine-2-(14C metsulfuron-methyl in soil under laboratory conditions. A High Performance Liquid Chromatograph (HPLC equipped with an UV detector and an on-line radio-chemical detector, plus a Supelco Discovery column (250 x 4.6 mm, 5 μm, and PRP-1 column (305 x 7.0 mm, 10 μm was used for the HPLC analysis. The radioactivity was determined by a Liquid Scintillation Counter (LSC in scintillation fluid. The soil used was both sterilized and non-sterilized in order to observe the involvement of soil microbes. The estimated DT50 and DT90 values of metsulfuron-methyl in a non-sterile system were observed to be 13 and 44 days, whereas in sterilized soil, the DT50 and DT90 were 31 and 70 days, respectively. The principal degradation product after 60 days was CO2. The higher cumulative amount of (14CO2 in (14C-triazine in the non-sterilized soil compared to that in the sterile system suggests that biological degradation by soil micro-organisms significantly contributes to the dissipation of the compound. The major routes of degradation were O-demethylation, sulfonylurea bridge cleavage and the triazine "ring-opened."

  19. Syntheses of (6- sup 14 C) and (5-carboxy, 6- sup 14 C sub 2 )nitrendipine

    Energy Technology Data Exchange (ETDEWEB)

    Maul, N.; Scherling, D. (Bayer AG, Wuppertal (Germany, F.R.). Inst. fuer Pharmakologie)

    1989-04-01

    (6-{sup 14}C)Nitrendipine synthesis started from barium({sup 14})carbonate, which was converted to (1-{sup 14}C)acetyl chloride. The acid chloride was condensed with Meldrum's acid (2,2-dimethyl-1,3-dioxane-4,6-dione). The resulting intermediate was treated with boiling methanol to give methyl (3-{sup 14}C)acetoacetate. The reaction with gaseous ammonia in toluene yielded the corresponding methyl 3-amino(3-{sup 14}C)crotonate which was condensed with ethyl 2-(3-nitro-benzylidene) acetoacetate to obtain (6-{sup 14}C)nitrendipine. (author).

  20. Characterization of acute biliary hyperplasia in Fisher 344 Rats administered the Indole-3-Carbinol Analog, NSC-743380

    Energy Technology Data Exchange (ETDEWEB)

    Eldridge, Sandy R.; Covey, Joseph; Morris, Joel [Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Rockville, MD, 20892 (United States); Fang, Bingliang [The University of Texas MD Anderson Cancer Center, Houston, TX, 77030 (United States); Horn, Thomas L. [IIT Research Institute, Chicago, IL, 60616 (United States); Elsass, Karen E. [Battelle Columbus, Columbus, OH, 43201 (United States); Hamre, John R. [Investigative Toxicology Laboratory, Leidos Biomedical Research, Inc., Frederick National Laboratory for Cancer Research, Frederick, MD 21702 (United States); McCormick, David L. [IIT Research Institute, Chicago, IL, 60616 (United States); Davis, Myrtle A., E-mail: myrtledavis@mail.nih.gov [Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Rockville, MD, 20892 (United States)

    2014-12-15

    NSC-743380 (1-[(3-chlorophenyl)-methyl]-1H-indole-3-carbinol) is in early stages of development as an anticancer agent. Two metabolites reflect sequential conversion of the carbinol functionality to a carboxaldehyde and the major metabolite, 1-[(3-chlorophenyl)-methyl]-1H-indole-3-carboxylic acid. In an exploratory toxicity study in rats, NSC-743380 induced elevations in liver-associated serum enzymes and biliary hyperplasia. Biliary hyperplasia was observed 2 days after dosing orally for 2 consecutive days at 100 mg/kg/day. Notably, hepatotoxicity and biliary hyperplasia were observed after oral administration of the parent compound, but not when major metabolites were administered. The toxicities of a structurally similar but pharmacologically inactive molecule and a structurally diverse molecule with a similar efficacy profile in killing cancer cells in vitro were compared to NSC-743380 to explore scaffold versus target-mediated toxicity. Following two oral doses of 100 mg/kg/day given once daily on two consecutive days, the structurally unrelated active compound produced hepatic toxicity similar to NSC-743380. The structurally similar inactive compound did not, but, lower exposures were achieved. The weight of evidence implies that the hepatotoxicity associated with NSC-743380 is related to the anticancer activity of the parent molecule. Furthermore, because biliary hyperplasia represents an unmanageable and non-monitorable adverse effect in clinical settings, this model may provide an opportunity for investigators to use a short-duration study design to explore biomarkers of biliary hyperplasia. - Highlights: • NSC-743380 induced biliary hyperplasia in rats. • Toxicity of NSC-743380 appears to be related to its anticancer activity. • The model provides an opportunity to explore biomarkers of biliary hyperplasia.

  1. Emergence of nitrosourea resistant sublines of Lewis lung tumour following MeCCNU treatment in vivo.

    Science.gov (United States)

    Stephens, T. C.; Adams, K.; Peacock, J. H.

    1986-01-01

    Several different drug retreatment protocols were employed to examine the emergence of resistance to MeCCNU in Lewis lung tumours. Previous studies suggested that although the majority of cells in untreated Lewis lung tumours were sensitive to MeCCNU, there was a very small proportion of resistant cells (approximately 0.001%) that limited "tumour cure' with that drug. If such cells were inherently drug resistant then it should be possible to derive highly resistant tumours by repeated drug treatment. In the first experiment tumours were treated with a single high dose of MeCCNU (35 or 40 mgkg-1) and on regrowth, transplanted into fresh mice and tested for drug sensitivity. Using both excision cell survival and growth delay endpoints, only approximately 25% of tumours were significantly resistant to the test dose, suggesting that many tumours resist the effects of the drug for reasons other than the presence of inherently drug resistant cells. One of the tumours (R4), that regrew after the initial treatment and appeared to be resistant to the test treatment, was retreated with a further 30 mgkg-1 MeCCNU and became more resistant. This line, designated R4/1, was cross-resistant to the other nitrosoureas, BCNU and CCNU, but not to cyclophosphamide, melphalan, cis-platinum or ionising radiation. The effect of treatment dose on the kinetics of MeCCNU resistance development was also studied in a retreatment regimen where the tumours were allowed to regrow and then transplanted into fresh hosts for the next treatment. Resistance developed more quickly at an intermediate dose of 15 mgkg-1 than at 7.5 mgkg-1 where the selective pressure was lower, or at 30 mgkg-1 where there was probably extinction of partially resistant cells. Resistance to MeCCNU developed even more quickly when tumours were retreated several times in the same host, although in a similar experiment with cyclophosphamide no resistance occurred. PMID:3954945

  2. [{sup 14}C]Serotonin uptake and [O-methyl-{sup 11}C]venlafaxine kinetics in porcine brain

    Energy Technology Data Exchange (ETDEWEB)

    Smith, D.F. E-mail: dfsmith@inet.uni2.dk; Hansen, S.B.; Oestergaard, L.; Gee, A.D.; Danielsen, E.; Ishizu, K.; Bender, D.; Poulsen, P.H.; Gjedde, A

    2001-08-01

    As part of our program of developing PET tracers for neuroimaging of psychotropic compounds, venlafaxine, an antidepressant drug, was evaluated. First, we measured in vitro rates of serotonin uptake in synaptosomes prepared from selected regions of porcine brain. Then, we determined the pharmacokinetics of venlafaxine, [O-methyl-{sup 11}C]-labeled for PET. Synaptosomal studies showed that the active uptake of [{sup 14}C]5-HT differed markedly between brain regions, with highest rates in hypothalamus, raphe region, and thalamus, and lowest rates in cortex and cerebellum. PET studies showed that the unidirectional rate of uptake of [O-methyl-{sup 11}C]venlafaxine from blood to brain was highest in the hypothalamus, raphe region, thalamus and basal ganglia and lowest in the cortex and cerebellum. Under normal physiological conditions, the capillary permeability-surface area (PS) product for [O-methyl-{sup 11}C]venlafaxine could not be estimated, because of complete flow-limitation of the cerebral uptake. Nevertheless, a correlation occurred between the apparent partition volume of the radiotracer and the rate of active uptake of 5-HT in selected regions of the porcine brain. During hypercapnia, limitations of blood-brain transfer were observed, giving PS-products for water that were only ca. 50% higher than those of venlafaxine. Thus, under normal physiological conditions, the rate of uptake of venlafaxine from blood into brain is completely flow-limited.

  3. Fate of the organophosphorus insecticide methoxy-14 C-Azinphos-methyl in baladi egyptian goats

    International Nuclear Information System (INIS)

    Hamdy, N.A.; Fakhr, I.M.I.; Abdalla, E.A.M.; Fouzy, A.S.M.; Hassan, M.N.A.

    1998-01-01

    Consecutive feeding of lactating goats with methoxy- 14 C-azinphos-methyl fo 4 days at dietary levels of 25 mg and 50 mg/goat per day resulted in the presence 0 the insecticide residues in milk 0.028ppm, 0.068ppm respectively at the end of the administration period. The residue levels were marckedly reduced after a withdrawa period of one week and completely disappeared after two weeks. Analysis of milk an urine residues showed similar metabolites in addition to a very small amount of the parent compound in the milk only. The major part of the residues consisted of mon demethylatedl azinophos-methyl, dimethyl phosphorohthioic, dimethyl phosphoro dithioic acids, dimethyl and mono-methyl phosphates. The animals remaine symptoms-frce during the experimental period

  4. Synthesis of cholesterol 26. C{sup 14} (1961); Synthese du cholesterol {sup 14}C-26 (1961)

    Energy Technology Data Exchange (ETDEWEB)

    Herbert, M; Pichat, L [Commissariat a l' Energie Atomique, Saclay (France). Centre d' Etudes Nucleaires

    1961-07-01

    Cholesterol 26 {sup 14}C is synthesized from methylmagnesium iodide {sup 14}C with a 48 per cent overall yield. Cholesterol is purified by chromatography on alumina. The various intermediates of the synthesis are characterized by thin-layer chromatography according to Stahl. (authors) [French] Le cholesterol {sup 14}C-26 est synthetise a partir d'iodure de methyl magnesium {sup 14}C, avec un rendement de 48 pour cent par rapport a l'iodure de methyl {sup 14}C mis en jeu. Le cholesterol est purifie par chromatographie sur alumine. Les intermediaires de la synthese sont caracterises par chromatographie en couche mince, selon Stahl. (auteurs)

  5. Determination of the quantity of acetyl CoA carboxylase by [14C]methyl avidin binding

    International Nuclear Information System (INIS)

    Roman-Lopez, C.R.; Goodson, J.; Allred, J.B.

    1987-01-01

    Conditions are described under which monomeric [ 14 C]methyl avidin binds to SDS-denatured biotin enzymes and remains bound through polyacrylamide gel electrophoresis. The location of radioactive proteins on the dried gel was determined by fluorography and their identity was established by subunit molecular weight. The relative quantity of bound radioactive avidin, stoichiometrically equivalent to the molar quantity of biotin protein, can be determined by scanning the fluorograph with a soft laser densitometer. To determine the absolute quantity of biotin protein, the radioactive areas of the dried gel were cut out, resolubilized, and assayed for radioactivity. Since the specific radioactivity of the [ 14 C]methyl avidin was known, the quantity of avidin bound and therefore the quantity of biotin enzyme could be calculated. The method is illustrated by the analysis of purified acetyl CoA carboxylase and is applied to the analysis of biotin enzymes in isolated rat liver mitochondria

  6. Degradation of 14C-malathion and 14C-chlorpyrifos-methyl on stored wheat

    International Nuclear Information System (INIS)

    Matthews, W.A.

    1990-01-01

    The degradation of malathion and chlorpyrifos-methyl on wheat stored under laboratory conditions was monitored using radiolabelled compounds. Metabolites of both insecticides were isolated and identified, although the formation of bound residues was the most significant feature in the breakdown pattern in both cases. After 5 months of storage, only 16% of the applied dose of malathion remained intact, the remainder being present as free metabolites (25%) or bound residues (42%). Chlorpyrifos-methyl degraded considerably more slowly than malathion, there being 60% of the applied dose still present after 14 months of storage. The bound residues accounted for 29% of the activity after this time. Attempts to determine the location of the activity within the grain suggested that it was concentrated in the germ by a factor of 10. Unfortunately, it was found not to be feasible to isolate the bran layer where a similar concentration of activity might have been expected. (author). 13 refs, 3 figs, 2 tabs

  7. Synthesis of [14C]-62514, a radiolabelled derivative of erythromycin A, via [2-14C]N,N-dimethylethylenediamine

    International Nuclear Information System (INIS)

    Surber, B.W.; Baker, W.R.; Seif, L.

    1991-01-01

    The synthesis of [ 14 C]A-62514, 11-deoxy-11[carboxy(2-dimethylamino-[1- 14 C]ethyl)amino]-6-0-methyl-e rythromycin A 11,12-(cyclic ester), was performed in five steps. The key intermediate, [2- 14 C]N,N-dimethylethyl-enediamine, was obtained in 80% yield by reacting Eschenmoser's salt with K 14 CN and reducing the resulting [1- 14 C]N,N-dimethylglycinonitrile with H 2 and Raney Ni in methanol and ammonium hydroxide. The final product was obtained 97% radiochemically pure in an overall radiochemical yield of 14%, with a specific activity of 39 mCi/mmol. (author)

  8. Distribution of 14C- labelled methyl parathion in the house sparrow, Passer domesticus L

    International Nuclear Information System (INIS)

    Bhatia, P.; Garg, A.K.; Kochhar, V.

    1994-01-01

    The activity of an insecticide when evaluated on dynamic basis is largely explained by differences in the rate of penetration, distribution and excretion. These mechanisms determine the fate of insecticides in the living system. The distribution of an organophosphorus insecticide i.e. 14 C-methyl parathion, based studies conducted on various aspects of it in relation to house sparrow, is presented. 9 refs., 1 fig

  9. Synthesis of [14C]-labelled AY-30,068

    International Nuclear Information System (INIS)

    Hicks, D.R.; Hangeland, J.J.; Mobilio, D.; DeLange, B.

    1988-01-01

    [ 14 C]AY-30,068 (cis-1,8-diethyl-2,3,4,9-tetrahydro-4-(2-propenyl)-1H-carbazole-1-acetic acid), a potent analgesic agent, was prepared by incorporating [ 14 C]methyl iodide via a Wittig reaction. The intermediate aldehyde was synthesized in six steps from cis-1-ethyl-2-oxo-4-(2-propenyl)cyclohexaneacetic acid methyl ester. Three batches of the [ 14 C]labelled AY-30,068 were produced, giving a combined overall yield of 9% from [ 14 C]methyl iodide sp. act. 51.2, 17.7 and 4.4 μCi/mg; 97.5, 98.3, and 98.6% radiochemical purity, respectively. (author)

  10. Synthesis of 14C analogue of 1,2-diaryl-[2-14C]-pyrroles

    International Nuclear Information System (INIS)

    Saemian, N.; Shirvani, G.; Matloubi, H.

    2007-01-01

    Three 1,2-diaryl pyrroles selective COX-2 inhibitors, 2-(4-fluorophenyl)-5-methyl-1-(4-methylsulfonyl-phenyl)-1H pyrrole, 2-(4-fluorophenyl)-1- [4-(methylsulfonyl) phenyl]-1H-pyrrole and 4-[2-(4-fluorophenyl)-1H-pyrrol-1-yl]benzenesulfon-amide, all three labeled with 14 C in the 2-position were prepared from para-fluoro-benzaldehyde-[carbonyl- 14 C]. (author)

  11. Beneficial effects of spin-labelled nitrosourea on CCNU-induced oxidative stress in rat blood compared with vitamin E.

    Science.gov (United States)

    Gadjeva, V; Kuchukova, D; Tolekova, A; Tanchev, S

    2005-07-01

    This study was carried out to determine the effects of a recently synthesized 1-ethyl-3-[4-(2,2,6,6-tetra-methylpiperidine-1-oxyl)]-1-nitrosourea (SLENU), compared with vitamin E as a positive control, on 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea (CCNU)-induced oxidative stress in rats. We determined plasma malonyl dialdehyde (MDA) levels and the activities of erythrocyte superoxide dismutase (SOD) and catalase (CAT). Forty two white albino healthy rats were treated once daily for 30 days with oral preparations of CCNU (12.5 mg/kg and 25 mg/kg), SLENU (25-200 mg/kg), and combinations of these. The CCNU-induced increase in plasma MDA level and the usual decrease in erythrocyte SOD and CAT activities were reversed by SLENU, but not by vitamin E. We have previously demonstrated that SLENU is a superoxide scavenger. A combination of our present findings with previous results thus leads us to proposing a new chemotherapeutic combination of CCNU and SLENU that is devoid of high toxicity.

  12. Synthesis of 14C-dehydrocorydaline chloride

    International Nuclear Information System (INIS)

    Zhang Rui; Wang Ding

    1988-01-01

    A method for synthesis of 14 C-dehydrocorydaline chloride is described. In the presence of sodium hydroxide, acetonylpalmatine is reacted with 14 C-methyl iodide in sealed glass ampoule to give 14 C-13-methylpalmatine iodide which is then converted to chloride. The radiochemical purity of 14 C-dehydrocorydaline determined by TLC is over 98% and the labelling efficiency is 54%

  13. Toxicological Aspects of Bound 14 C-Pirimiphos - methyl (Actellic) in Stored faba Beans to Experimental Mice

    International Nuclear Information System (INIS)

    TahA, H.

    2006-01-01

    The misuse of the insecticides in the environment always represents a high risk for living organisms. however, to take about hazardous effects of it, there is a need to detect their toxicity in the living organism; so the persistence of bound 14 C-pirimiphos methyl, an organophosphorus insecticide in stored faba beans and its toxicological effects to experimental animals (mice) were investigated. Seeds of faba beans were treated with the 14 C-pirimiphos-methyl insecticide at a dose of 30 mg insecticide/kg seeds and stored for 24 weeks under condition simulating these used locally. the level of the total extractable and bound insecticide represented about 95.5% of the actual dose. feeding experiments on mice for 90 days with a diet containing the bound pesticide at a dose of 1.12 ppm/day/mouse caused significant symptoms of toxicity during the experiment period. the cholinesterase activity of both plasma and red blood cells was decreased during the first 15 days. the hemoglobin concentration, erythrocyte and leucocyte count showed slightly significant differences from control values. A significant increase in both of liver and kidney enzymes was observed at the end of the experiment

  14. [14C]-radiolabeling of {[trans-(8β)]-6-methyl-1-(1-methylethyl) ergoline-8-carboxylic acid, 4-methoxycyclohexyl ester (Z)-2-buteneidioate (1:1)}

    International Nuclear Information System (INIS)

    Marzoni, G.; Wheeler, W.J.; Garbrecht, W.L.

    1988-01-01

    The 5HT 2 -receptor antagonist, [ 14 C]-labeled brace[trans-(8β)]-6-methyl-1-(1-methylethyl)ergoline-8-carboxylic acid, 4-methoxycyclohexyl ester (Z)-2-butenedioate (1:1)brace (LY281067) was synthesized from unlabeled 6-methyl-1-(1-methylethyl)ergoline-8-carboxylic acid. The [ 14 C] label was introduced into the carboxyl group attached to the 8 position of the ergoline nucleus. This site is stable to metabolism. The synthesis involves removal of an unlabeled carboxyl group and subsequent reinsertion of a [ 14 C]-labeled carboxyl group into the same position. The radiolabel is not introduced until near the end of the synthesis which allows for ease of handling and scale-up of intermediates. (author)

  15. Synthesis of C-9-14C-1,8-dihydroxy-3-carboxyanthraquinone

    International Nuclear Information System (INIS)

    De Witte, P.; Lemli, J.

    1988-01-01

    The synthesis of C-9- 14 C-rhein is reported using 14 CO 2 as a 14 C-source. After preparing 14 C-1, 8-dimethoxy-3-methylanthraquinone by a condensation reaction, the product is demethylated and the 3-methyl group converted to the corresponding 3-carboxy group. The radio-active yield of the total synthesis, starting with 1 Ci 14 CO 2 is 6,9% (6, 9 mCi); 352 mg 14 rhein is produced with a specific activity of 55,7 mCi/mmol. (author)

  16. Syntheses of {gamma}-aminobutyric-1-{sup 14}C and of {alpha}-aminoadipic-6-{sup 14}C acid from methoxy-3 chloropropyl-magnesium and marked carbon dioxide; Syntheses de l'acide {gamma}-aminobutyrique{sup 14}C-1 et de l'acide {alpha}-aminoadipique {sup 14}C-6 a partir de methoxy-3 chloropropylmagnesium et d'anhydride carbonique marque

    Energy Technology Data Exchange (ETDEWEB)

    Liem, Phung Nhu [Commissariat a l' Energie Atomique, Saclay (France). Centre d' Etudes Nucleaires, Departement des radioelements, Service des molecules marquees

    1967-04-01

    Carbonation of {gamma}-methoxypropyl-magnesium chloride by CO{sub 2} gives {gamma}-methoxy-butyric carboxylic-{sup 14}C acid with a yield of about 95 per cent. When the latter is treated successively with anhydrous HBr and with diazomethane, methyl carboxylic {gamma}-bromobutyrate-{sup 14}C is formed. This in turn gives {gamma}-amino-butyric carboxylic-{sup 14}C acid with an overall yield of 66 per cent with respect to Ba{sup 14}CO{sub 3}, when it is condensed with potassium phthalimide and hydrolyzed by acid. By reacting methyl-{gamma}-bromobutyrate-{sup 14}C with the sodium derivative of ethyl cyanacetamido-acetate in ethanol, followed by an acid hydrolysis, {alpha}-aminoadipic-6-{sup 14}C acid is obtained with an overall yield of 46 per cent with respect to Ba{sup 14}CO{sub 3}. (author) [French] La carbonatation du chlorure de {gamma}-methoxypropylmagnesium par {sup 14}CO{sub 2} donne l'acide {gamma}-methoxybutyrique carboxyle {sup 14}C avec un rendement d'environ 95 pour cent. Ce dernier traite successivement par HBr anhydre et par le diazomethane conduit au {gamma}-bromobutyrate de methyle carboxyle {sup 14}C. Celui-ci condense avec le phtalimide de potassium suivi d'une hydrolyse acide fournit l'acide {gamma}-aminobutyrique carboxyle {sup 14}C avec un rendement global de 66 pour cent par rapport a Ba{sup 14}CO{sub 3}. L'action du {gamma}-bromobutyrate de methyle {sup 14}C sur le derive sode du cyanacetamidoacetate d'ethyle dans l'ethanol suivie d'hydrolyse acide donne l'acide {alpha}-aminoadipique {sup 14}C-6 avec un rendement global de 46 pour cent par rapport a Ba{sup 14}CO{sub 3}. (auteur)

  17. Prostaglandin E2 facilitates neurite outgrowth in a motor neuron-like cell line, NSC-34

    Directory of Open Access Journals (Sweden)

    Hiroshi Nango

    2017-10-01

    Full Text Available Prostaglandin E2 (PGE2 exerts various biological effects by binding to E-prostanoid receptors (EP1-4. Although recent studies have shown that PGE2 induces cell differentiation in some neuronal cells such as mouse DRG neurons and sensory neuron-like ND7/23 cells, it is unclear whether PGE2 plays a role in differentiation of motor neurons. In the present study, we investigated the mechanism of PGE2-induced differentiation of motor neurons using NSC-34, a mouse motor neuron-like cell line. Exposure of undifferentiated NSC-34 cells to PGE2 and butaprost, an EP2-selective agonist, resulted in a reduction of MTT reduction activity without increase the number of propidium iodide-positive cells and in an increase in the number of neurite-bearing cells. Sulprostone, an EP1/3 agonist, also significantly lowered MTT reduction activity by 20%; however, no increase in the number of neurite-bearing cells was observed within the concentration range tested. PGE2-induced neurite outgrowth was attenuated significantly in the presence of PF-0441848, an EP2-selective antagonist. Treatment of these cells with dibutyryl-cAMP increased the number of neurite-bearing cells with no effect on cell proliferation. These results suggest that PGE2 promotes neurite outgrowth and suppresses cell proliferation by activating the EP2 subtype, and that the cAMP-signaling pathway is involved in PGE2-induced differentiation of NSC-34 cells. Keywords: Prostaglandin E2, E-prostanoid receptors, Motor neuron, Neurite outgrowth, cAMP

  18. Preparation of arginine (guanide 14C)

    International Nuclear Information System (INIS)

    Pichat, L.; Baret, C.

    1960-01-01

    Reaction of anhydrous ammoniac at 800 deg. C on 14 CO 3 Ba gives rise to barium cyanamide 14 C with a yield of about 98 per cent. Addition on H 2 S on cyanamide 14 C leads to thiourea 14 C with a 85 per cent yield, which is quantitatively transformed into S-ethyl-isothiouronium iodide by treatment with methyl iodide. This 14 C-isothiouronium salt is used to introduce 14 C guanide group in α-N-tosyl-ornithine; tosyl group in α-N-tosyl-arginine thus obtained is then removed by hydrolysis with hydrochloric acid. Arginine is separated as flavianic acid salt and is purified on exchange resin Dowex-50. The overall yield based on 14 CO 3 Ba is 25 per cent. (author) [fr

  19. The synthesis of [[sup 2]H],[[sup 3]H], and [[sup 14]C]-labeled 8[beta]-[(methylthio)methyl]-6-propylergoline mesylate (pergolide mesylate), a potent, long-acting dopamine agonist

    Energy Technology Data Exchange (ETDEWEB)

    Wheeler, W.J.; Kau, D.L.K.; Bach, N.J. (Lilly (Eli) and Co., Indianapolis, IN (United States). Lilly Research Labs.)

    1990-03-01

    The [[sup 3]H]- and two[[sup 14]C]-isopomers of 8[beta]-[(methylthio)methyl]-6-propylergoline mesylate (pergolide mesylate) have been synthesized. The [[sup 3]H]-derivative was synthesized by the palladium catalyzed tritiation of the corresponding 6-allyl derivative. Reaction of 8[beta]-[(methylthio)methyl]-ergoline with 1-[[sup 14]C]-1-propyl bromide yielded pergolide labeled in the 6-propyl group. Alternatively, reaction of 8[beta]-mesyloxy-6-propylergoline with [[sup 14]C]-sodium cyanide, followed by base hydrolysis, yielded 8 [beta]-carboxy-6-propylergoline-[[sup 14]C], which was subsequently converted to pergolide mesylate radiolabeled in the 17-position via a four step sequence. (Author).

  20. Dopamine transporter binding in rat striatum: a comparison of [O-methyl-{sup 11}C]{beta}-CFT and [N-methyl-{sup 11}C]{beta}-CFT

    Energy Technology Data Exchange (ETDEWEB)

    Yoder, Karmen K.; Hutchins, Gary D.; Mock, Bruce H.; Fei, Xiangshu; Winkle, Wendy L. [Department of Radiology, Indiana University School of Medicine, L3-208, Indianapolis, IN 46202 (United States); Gitter, Bruce D.; Territo, Paul R. [Lilly Center for Anatomical and Molecular Imaging, Integrative Biology Division, Lilly Research Laboratories, Greenfield, IN 46140 (United States); Zheng Qihuang [Department of Radiology, Indiana University School of Medicine, L3-208, Indianapolis, IN 46202 (United States)], E-mail: qzheng@iupui.edu

    2009-01-15

    Introduction: Positron emission tomography scanning with radiolabeled phenyltropane cocaine analogs is important for quantifying the in vivo density of monoamine transporters, including the dopamine transporter (DAT). [{sup 11}C]{beta}-CFT is useful for studying DAT as a marker of dopaminergic innervation in animal models of psychiatric and neurological disorders. [{sup 11}C]{beta}-CFT is commonly labeled at the N-methyl position. However, labeling of [{sup 11}C]{beta}-CFT at the O-methyl position is a simpler procedure and results in a shorter synthesis time [desirable in small-animal studies, where specific activity (SA) is crucial]. In this study, we sought to validate that the O-methylated form of [{sup 11}C]{beta}-CFT provides equivalent quantitative results to that of the more commonly reported N-methyl form. Methods: Four female Sprague-Dawley rats were scanned twice on the IndyPET II small-animal scanner, once with [N-methyl-{sup 11}C]{beta}-CFT and once with [O-methyl-{sup 11}C]{beta}-CFT. DAT binding potentials (BP{identical_to}B'{sub avail}/K{sub d}) were estimated for right and left striata with a nonlinear least-squares algorithm, using a reference region (cerebellum) as the input function. Results: [N-Methyl-{sup 11}C]{beta}-CFT and [O-methyl-{sup 11}C]{beta}-CFT were synthesized with 40-50% radiochemical yields (HPLC purification). Radiochemical purity was >99%. SA at end of bombardment was 258{+-}30 GBq/{mu}mol. Average BP values for right and left striata with [N-methyl-{sup 11}C]{beta}-CFT were 1.16{+-}0.08 and 1.23{+-}0.14, respectively. BP values for [O-methyl-{sup 11}C]{beta}-CFT were 1.18{+-}0.08 (right) and 1.22{+-}0.16 (left). Paired t tests demonstrated that labeling position did not affect striatal DAT BP. Conclusions: These results suggest that [O-methyl-{sup 11}C]{beta}-CFT is quantitatively equivalent to [N-methyl-{sup 11}C]{beta}-CFT in the rat striatum.

  1. Oxidative stress in NSC-741909-induced apoptosis of cancer cells

    Directory of Open Access Journals (Sweden)

    Huang Peng

    2010-04-01

    Full Text Available Abstract Background NSC-741909 is a novel anticancer agent that can effectively suppress the growth of several cell lines derived from lung, colon, breast, ovarian, and kidney cancers. We recently showed that NSC-741909-induced antitumor activity is associated with sustained Jun N-terminal kinase (JNK activation, resulting from suppression of JNK dephosphorylation associated with decreased protein levels of MAPK phosphatase-1. However, the mechanisms of NSC-741909-induced antitumor activity remain unclear. Because JNK is frequently activated by oxidative stress in cells, we hypothesized that reactive oxygen species (ROS may be involved in the suppression of JNK dephosphorylation and the cytotoxicity of NSC-741909. Methods The generation of ROS was measured by using the cell-permeable nonfluorescent compound H2DCF-DA and flow cytometry analysis. Cell viability was determined by sulforhodamine B assay. Western blot analysis, immunofluorescent staining and flow cytometry assays were used to determine apoptosis and molecular changes induced by NSC-741909. Results Treatment with NSC-741909 induced robust ROS generation and marked MAPK phosphatase-1 and -7 clustering in NSC-741909-sensitive, but not resistant cell lines, in a dose- and time-dependent manner. The generation of ROS was detectable as early as 30 min and ROS levels were as high as 6- to 8-fold above basal levels after treatment. Moreover, the NSC-741909-induced ROS generation could be blocked by pretreatment with antioxidants, such as nordihydroguaiaretic acid, aesculetin, baicalein, and caffeic acid, which in turn, inhibited the NSC-741909-induced JNK activation and apoptosis. Conclusion Our results demonstrate that the increased ROS production was associated with NSC-741909-induced antitumor activity and that ROS generation and subsequent JNK activation is one of the primary mechanisms of NSC-741909-mediated antitumor cell activity.

  2. Autoradiography of [14C]paraquat or [14C]diquat in frogs and mice: accumulation in neuromelanin

    International Nuclear Information System (INIS)

    Lindquist, N.G.; Larsson, B.S.; Lyden-Sokolowski, A.

    1988-01-01

    The herbicide paraquat has been suggested as a causative agent for Parkinson's disease because of its structural similarity to a metabolite of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), which may induce a parkinsonism-like condition. MPTP as well as its metabolite 1-methyl-4-phenylpyridine have melanin affinity, and the parkinsonism-inducing potency of MPTP is much stronger in species with melanin in the nerve cells. Autoradiography of [ 3 H]MPTP in experimental animals has shown accumulation in melanin-containing tissues, including pigmented neurons. In the present whole body autoradiographic study accumulation and retention was seen in neuromelanin in frogs after i.p. injection of [ 14 C]paraquat or[ 14 C]diquat. By means of whole body autoradiography of [ 14 C]diquat in mice (a species with no or very limited amounts of neuromelanin) a low, relatively uniformly distributed level of radioactivity was observed in brain tissue. Accumulation of toxic chemical compounds, such as paraquat, in neuromelanin may ultimately cause lesions in the pigmented nerve cells, leading to Parkinson's disease

  3. Identification of Patients with Recurrent Glioblastoma Who May Benefit from Combined Bevacizumab and CCNU Therapy: A Report from the BELOB Trial.

    Science.gov (United States)

    Erdem-Eraslan, Lale; van den Bent, Martin J; Hoogstrate, Youri; Naz-Khan, Hina; Stubbs, Andrew; van der Spek, Peter; Böttcher, René; Gao, Ya; de Wit, Maurice; Taal, Walter; Oosterkamp, Hendrika M; Walenkamp, Annemiek; Beerepoot, Laurens V; Hanse, Monique C J; Buter, Jan; Honkoop, Aafke H; van der Holt, Bronno; Vernhout, René M; Sillevis Smitt, Peter A E; Kros, Johan M; French, Pim J

    2016-02-01

    The results from the randomized phase II BELOB trial provided evidence for a potential benefit of bevacizumab (beva), a humanized monoclonal antibody against circulating VEGF-A, when added to CCNU chemotherapy in patients with recurrent glioblastoma (GBM). In this study, we performed gene expression profiling (DASL and RNA-seq) of formalin-fixed, paraffin-embedded tumor material from participants of the BELOB trial to identify patients with recurrent GBM who benefitted most from beva+CCNU treatment. We demonstrate that tumors assigned to the IGS-18 or "classical" subtype and treated with beva+CCNU showed a significant benefit in progression-free survival and a trend toward benefit in overall survival, whereas other subtypes did not exhibit such benefit. In particular, expression of FMO4 and OSBPL3 was associated with treatment response. Importantly, the improved outcome in the beva+CCNU treatment arm was not explained by an uneven distribution of prognostically favorable subtypes as all molecular glioma subtypes were evenly distributed along the different study arms. The RNA-seq analysis also highlighted genetic alterations, including mutations, gene fusions, and copy number changes, within this well-defined cohort of tumors that may serve as useful predictive or prognostic biomarkers of patient outcome. Further validation of the identified molecular markers may enable the future stratification of recurrent GBM patients into appropriate treatment regimens. ©2016 American Association for Cancer Research.

  4. Synthesis of carbon-14 analogue of 1,5 diaryl-5-[14C]-1,2,3-triazoles

    International Nuclear Information System (INIS)

    Matloubi, Hojatollah; Shafiee, Abbas; Saemian, Nader; Shirvani, Gholamhossein; Daha, Fariba Johari

    2004-01-01

    Two 1,2,3-triazole anticonvulsants, 1-(4-methylsulfone-phenyl)-5-(4-methyl-phenyl)-1,2,3-triazole and 1-(4-methylsulfone-phenyl)-5-phenyl-1,2,3-triazole, both labeled with carbon-14 in the 5-position were prepared from para-tolunitrile-[cyano- 14 C] and benzonitrile-[cyano- 14 C], respectively

  5. Synthesis of 14C-labeled stepholidine

    International Nuclear Information System (INIS)

    Yang Liu; Zhang Xin

    1988-01-01

    L-Tetrahydroprotoberberine (THPB) alkaloids are dopamine-receptor antagonists. Stepholidine has been shown to possess the strongest pharmacological effects among the THPB alkaloids studied. In order to study its metabolism and the mode of action of the drug, a radiolabeled stepholidine was required. We report here the synthesis of 14 C-labeled stepholidine by Mannich condensation of 7-benzyloxy-1-(4-benzyloxy-3-hydroxy-benzyl)-6-methoxy-1,2,3,4-tetrahydroisoquinoline with ( 14 C)formaldehyde followed by methylation and debensylation in 32% radiochemical yield. (author)

  6. Migratory capabilities of human umbilical cord blood-derived neural stem cells (HUCB-NSC) in vitro.

    Science.gov (United States)

    Janowski, Miroslaw; Lukomska, Barbara; Domanska-Janik, Krystyna

    2011-01-01

    Many types of neural progenitors from various sources have been evaluated for therapy of CNS disorders. Prerequisite for success in cell therapy is the ability for transplanted cells to reach appropriate target such as stroke lesion. We have established neural stem cell line from human umbilical cord blood neural stem (HUCB-NSC). In the present study we evaluated migratory capabilities of cells (HUCB-NSC) and the presence of various migration-related receptors. Immunocytochemical analysis revealed abundant expression of CXCR4, PDGFR-alpha, PDGFR-beta, c-Met, VEGFR, IGF-1R and PSA-NCAM receptors in non-adherent population of HUCB-NSC cultured in serum free (SF) conditions (SF cells). Biological activity of selected receptors was confirmed by HUCB-NSC in vitro migration towards SDF-1 and IGF-1 ligands. Additionally, rat brain-derived homogenates have been assessed for their chemoattractive activity of HUCB-NSC. Our experiments unveiled that brain tissue was more attracted for HUCB-NSC than single ligands with higher potency of injured than intact brain. Moreover, adherent HUCB-NSC cultured in low serum (LS) conditions (LS cells) were employed to investigate an impact of different extracellular matrix (ECM) proteins on cell motility. It turned out that laminin provided most permissive microenvironment for cell migration, followed by fibronectin and gelatin. Unexpected nuclear localization of CXCR4 in SF cells prompted us to characterize intracellular pattern of this expression in relation to developmental stage of cells cultured in different conditions. Continuous culture of LS cells revealed cytoplasmatic pattern of CXCR4 expression while HUCB-NSC cultured in high serum conditions (HS cells) resulted in gradual translocation of CXCR4 from nucleus to cytoplasm and then to arising processes. Terminal differentiation of HUCB-NSC was followed by CXCR4 expression decline.

  7. Synthesis of [14C]ABT-418, a cholinergic channel activator labeled at two sites on the isoxazole ring

    International Nuclear Information System (INIS)

    Surber, B.W.; Thomas, S.B.; Elliott, R.L.; Kopecka, Hana

    1996-01-01

    [ 14 C]ABT-418, (S)-3-[ 14 C]methyl-5-[N-methyl-2-pyrrolidinyl] [4- 14 C]isoxazole hydrochloride, was labeled in two positions at maximum specific activity. Starting with 100 mCi of sodium [2- 14 C]acetate, 14.6 mCi at 105 mCi/mmol was obtained in 8 steps including the formation of [1,3- 14 C]acetone in the pyrolysis of barium [2- 14 C]acetate. The key step was the formation of the dianion of [1,3- 14 C]acetone oxime and its condensation with L-proline methyl ester. (author)

  8. Modified synthesis of 11-[14C]-clozapine

    International Nuclear Information System (INIS)

    Matloubi, Hojatollah; Ghandi, Mehdi; Zarrindast, M.-R.; Saemian, Nader

    2001-01-01

    The reported synthetic pathway of 8-chloro-11-(4-methyl-1-piperazinyl)-11-[ 14 C]-5H-dibenzo[b,e][1,4]diazapine (clozapine) was modified in several steps. The synthetic pathway was shortened by 60% and the total yield was increased from 6% to 23%

  9. Synthesis of /sup 14/C- and /sup 35/S-labelled 2-mercaptobenzimidazoles

    Energy Technology Data Exchange (ETDEWEB)

    Doerge, D R

    1988-09-01

    /sup 14/C- and /sup 35/S-labelled 2-mercaptobenzimidazole and 1-methyl-2-mercaptobenzimidazole were synthesized from /sup 14/C-carbon disulfide, /sup 35/S-thiourea, /sup 14/C-methyl iodide and /sup 35/S-thiourea, respectively, for use in studies on the mechanism of action of antithyroid drugs. The products were purified by chromatography on silica and isolated with radiochemical purities of greater than 98%, yields of 45-77% and specific activities of 2.1-5.3 mCi/mmole.

  10. Distribution of radiolabeled 1-(4-amino-2-methyl-5-pyrimidinyl)methyl-3-(2-chloroethyl)-3-nitrosourea hydrochloride in rat brain tumor: intraarterial versus intravenous administration

    International Nuclear Information System (INIS)

    Yamada, K.; Ushio, Y.; Hayakawa, T.; Arita, N.; Huang, T.Y.; Nagatani, M.; Yamada, N.; Mogami, H.

    1987-01-01

    To assess the rationale of intraarterial (i.a.) 1-(4-amino-2-methyl-5-pyrimidinyl)methyl-3-(2-chloroethyl)-3-nitrosourea chemotherapy, distribution of 14 C-labeled 1-(4-amino-2-methyl-5-pyrimidinyl)methyl-3-(2-chloroethyl)-3-nitrosourea in rat glioma was studied after i.a. or i.v. infusion. Immediately after infusion, the tumor located in the hemisphere of intracarotid infusion received 4.6-fold higher radioactivity than the tumor located contralaterally to intracarotid infusion and 2.8-fold higher radioactivity than i.v. infusion. The difference was kept up to 30 min after i.a. infusion. Autoradiographic observation indicated rather uniform distribution of the tracer in the central portion of i.a. infusion. However, in the periphery of i.a. infusion, distribution of the tracer was nonhomogenous. The results indicate that i.a. 1-(4-amino-2-methyl-5-pyrimidinyl)methyl-3-(2-chloroethyl)-3-nitrosourea chemotherapy is useful when the tumor has high blood flow and is located in the center of an infused area

  11. Synthesis of carbon-14 analogue of 1,5 diaryl-5-[{sup 14}C]-1,2,3-triazoles

    Energy Technology Data Exchange (ETDEWEB)

    Matloubi, Hojatollah E-mail: hmatloubi@aeoi.org.ir; Shafiee, Abbas; Saemian, Nader; Shirvani, Gholamhossein; Daha, Fariba Johari

    2004-05-01

    Two 1,2,3-triazole anticonvulsants, 1-(4-methylsulfone-phenyl)-5-(4-methyl-phenyl)-1,2,3-triazole and 1-(4-methylsulfone-phenyl)-5-phenyl-1,2,3-triazole, both labeled with carbon-14 in the 5-position were prepared from para-tolunitrile-[cyano-{sup 14}C] and benzonitrile-[cyano-{sup 14}C], respectively.

  12. Autoradiography of ( sup 14 C)paraquat or ( sup 14 C)diquat in frogs and mice: accumulation in neuromelanin

    Energy Technology Data Exchange (ETDEWEB)

    Lindquist, N G; Larsson, B S; Lyden-Sokolowski, A [Uppsala Univ., Biomedical Center, (Sweden). Dept. of Toxicology

    1988-10-31

    The herbicide paraquat has been suggested as a causative agent for Parkinson's disease because of its structural similarity to a metabolite of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), which may induce a parkinsonism-like condition. MPTP as well as its metabolite 1-methyl-4-phenylpyridine have melanin affinity, and the parkinsonism-inducing potency of MPTP is much stronger in species with melanin in the nerve cells. Autoradiography of ({sup 3}H)MPTP in experimental animals has shown accumulation in melanin-containing tissues, including pigmented neurons. In the present whole body autoradiographic study accumulation and retention was seen in neuromelanin in frogs after i.p. injection of ({sup 14}C)paraquat or({sup 14}C)diquat. By means of whole body autoradiography of ({sup 14}C)diquat in mice (a species with no or very limited amounts of neuromelanin) a low, relatively uniformly distributed level of radioactivity was observed in brain tissue. Accumulation of toxic chemical compounds, such as paraquat, in neuromelanin may ultimately cause lesions in the pigmented nerve cells, leading to Parkinson's disease.

  13. Synthesis of [{sup 14}C]ABT-418, a cholinergic channel activator labeled at two sites on the isoxazole ring

    Energy Technology Data Exchange (ETDEWEB)

    Surber, B.W.; Thomas, S.B. [Abbott Labs., Drug Metabolism, Abbott Park, IL (United States); Elliott, R.L.; Kopecka, Hana [Abbott Labs., Neuroscience Research, Abbott Park, IL (United States)

    1996-09-01

    [{sup 14}C]ABT-418, (S)-3-[{sup 14}C]methyl-5-[N-methyl-2-pyrrolidinyl] [4-{sup 14}C]isoxazole hydrochloride, was labeled in two positions at maximum specific activity. Starting with 100 mCi of sodium [2-{sup 14}C]acetate, 14.6 mCi at 105 mCi/mmol was obtained in 8 steps including the formation of [1,3-{sup 14}C]acetone in the pyrolysis of barium [2-{sup 14}C]acetate. The key step was the formation of the dianion of [1,3-{sup 14}C]acetone oxime and its condensation with L-proline methyl ester. (author).

  14. 13C and 1H nuclear magnetic resonance of methyl-substituted acetophenones and methyl benzoates: steric hindrance and inhibited conjugation.

    Science.gov (United States)

    Budesínský, Milos; Kulhánek, Jirí; Böhm, Stanislav; Cigler, Petr; Exner, Otto

    2004-10-01

    The 1H and 13C NMR spectra of 14 methyl-substituted acetophenones and 14 methyl-substituted methyl benzoates were assigned and interpreted with respect to the conformation of the C(ar)-C(O) bond. The substituent effects are proportional in the two series and can be divided into polar and steric: each has different effects on the 13C SCS of the individual atoms. In the case of C atoms C(O), C(1) and CH3(CO), the steric effects were quantitatively separated by comparing SCS in the ortho and para positions. The steric effects are proportional for the individual C atoms and also to steric effects estimated from other physical quantities. However, they do not depend simply on the angle of torsion phi of the functional group as anticipated hitherto. A better description distinguishes two classes of compounds: sterically not hindered or slightly hindered planar molecules and strongly sterically hindered, markedly non-planar. In order to confirm this reasoning without empirical correlations, the J(C,C) coupling constants were measured for three acetophenone derivatives labeled with 13C in the acetyl methyl group. The constants confirm unambiguously the conformation of 2-methylacetophenone; their zero values are in accord with the conformation of 2,6-dimethylacetophenone. The zero values in the unsubstituted acetophenone are at variance with previous erroneous report but all J(C,C) values are in accord with calculations at the B3LYP/6-311++G(2d,2p)//B3LYP/6-311+G(d,p) level. Copyright 2004 John Wiley & Sons, Ltd.

  15. Biodegradation mechanism of linear alkylbenzenesulfonate-14C

    International Nuclear Information System (INIS)

    Kubodera, Tadayoshi; Muto, Toshio; Yamamoto, Tatsuo

    1978-01-01

    The biodegradation of linear alkylbenzenesulfonate- 14 C (LAS- 14 C) tagged with 14 C at the linear side chain was studied on activated sludge by tracer method in addition to the methylene blue method which is widely employed in the biodegradation of LAS. It was found that there were three periods of rapid adsorption period, acclimation period, and degradation process. The radiolysis of dodecylbenzenesulfonate was studied on irradiating by 5000 Ci 60 Co source. The decomposition products were identified by GLC and GC-MS spectrometry after desulfonation. 1-Tetralone, 1-indanone, 4-methyl-1-tetralone, naphthalene et al. were found in them. (author)

  16. Modified synthesis of 11-[{sup 14}C]-clozapine

    Energy Technology Data Exchange (ETDEWEB)

    Matloubi, Hojatollah E-mail: hmatloubi@seai.neda.net.ir; Ghandi, Mehdi; Zarrindast, M.-R.; Saemian, Nader

    2001-11-01

    The reported synthetic pathway of 8-chloro-11-(4-methyl-1-piperazinyl)-11-[{sup 14}C]-5H-dibenzo[b,e][1,4]diazapine (clozapine) was modified in several steps. The synthetic pathway was shortened by 60% and the total yield was increased from 6% to 23%.

  17. Chlorozotocin

    Science.gov (United States)

    Panasci, Lawrence C.; Green, Dianna; Schein, Philip S.

    1979-01-01

    Chlorozotocin is a chloroethyl nitrosourea with a glucose carrier that has curative activity for the murine L1210 leukemia, but is nonmyelosuppressive in mice. To determine the mechanism for this unique property of reduced bone marrow toxicity, comparative studies were conducted with chlorozotocin and CCNU, a myelotoxic chloroethyl nitrosourea. Suspensions of L1210 leukemia and murine bone marrow cells were incubated for 2 h with 0.1 mM [14C]-chloroethyl chlorozotocin or CCNU. Chlorozotocin demonstrated a fourfold increased covalent binding of the chloroethyl group to L1210 nuclei when compared to equimolar CCNU. Chlorozotocin alkylation of L1210 cells resulted in the binding of 57 pmol of [14C]ethyl group/mg of DNA, which represented a 2.3-fold increased alkylation when compared to CCNU. In marked contrast, the binding of the chloroethyl group to bone marrow nuclei was equivalent for both drugs. In addition, chlorozotocin alkylation of murine bone marrow DNA, 45 pmol of [14C]ethyl group/mg of DNA, was equivalent to that of CCNU. The ratio of L1210:bone marrow DNA alkylation was 1.3 for chlorozotocin compared to 0.6 for CCNU. The intracellular carbamoylation of L1210 and bone marrow protein by CCNU was 400- to 600-fold greater than that produced by chlorozotocin. After a 2-h exposure to 0.1, 0.05, or 0.01 mM drug, both chlorozotocin and CCNU produced a reduction in the cloning efficiency of L1210 cells that was dose dependent. However, chlorozotocin was significantly more cytotoxic than CCNU at all three molar concentrations (P synthesis to 1% of control by 48 h, in contrast to 16% with equimolar CCNU (P 50% indefinite survivors. In contrast, CCNU at the same molar doses resulted in only a 191% ILS; a CCNU dose of 128 μmol/kg was required for comparable optimal L1210 antitumor activity, 413% ILS. On a molar basis, the dose of chlorozotocin that produced optimal in vivo L1210 antitumor activity was one-third to one-half that of CCNU. Chlorozotocin, unlike CCNU

  18. [Expression of ICAT and Wnt signaling-related proteins in the monocytic differentiation of HL-60 cells induced by a new steroidal drug NSC67657].

    Science.gov (United States)

    Wang, J S; Wang, W J; Wang, T; Zhang, Y

    2016-04-01

    To investigate the expression of mRNA and proteins of β-catenin, TCF-4 (ICAT) and Wnt signaling pathway-related genes in the monocytic differentiation of acute myeloid leukemia HL-60 cells induced by a new steroidal drug NSC67657. Wright's staining and α-NBE staining were used to observe the differentiation of HL-60 cells after 5 days of 10 μmol/L NSC67657 treatment. Flow cytometry (FCM) was used to detect the differentiation and cell cycles. The expressions of mRNA and proteins of ICAT and Wnt signaling pathway-related factors, including β-catenin, TCF-4, c-myc, cyclin D1 and TCF-1 before and after differentiation, were detected by RT-PCR and Western blot. Morphological observation showed that NSC67657 induced monocytic differentiation of HL-60 cells. At 5 days after 10 μmol/L NSC67657 treatment, the number of CD14(+) HL-60 cells was (94.37±2.84)%, significantly higher than the (1.31±0.09)% in control group (Pcells were of (18.76±0.98)%, significantly lower than that of (34.38±2.61) % in the control group (Pprotein, and down-regulated the expression of β-catenin mRNA and protin (Pprotein and nuclear protein in the HL-60 cells (P>0.05 for all). The target genes of Wnt signaling pathway, including c-myc, cyclinD1 and TCF-1 mRNA and proteins in the HL-60 cells were significantly down-regulated after NSC67657 treatment (Pcells, and down-regulates the expression of β-catenin and target genes of Wnt signaling pathway. These results indicate that Wnt signaling pathway may be directly or indirectly involved in the monocytic differentiation process of HL-60 cells.

  19. An improved synthesis of 14C labelled glycerol using sodium borohydride

    International Nuclear Information System (INIS)

    Chander, H.; Ramamurthy, T.V.; Viswanathan, K.V.

    1987-01-01

    [1- 14 C]Glyceric acid has been reduced to [1(3)- 14 C]glycerol in high yields via the methyl ester of [1- 14 C]glyceric acid by sodium borohydride in the presence of t-butyl alcohol and methanol. The importance of the procedure is highlighted in relation to other procedures involving lithium aluminium hydride reduction. (author)

  20. Metabolic kinetics and biological effects of radiocarbon (14C)

    International Nuclear Information System (INIS)

    Vasilenko, I.Ya.; Osipov, V.A.; Lyaginskaya, A.M.; Bugryshev, P.F.; Istomina, A.G.; Turova, V.I.; Dement'ev, S.I.; Zhorova, E.S.; Mart'yanov, B.M.; Shal'nova, G.A.; Kuz'mina, T.D.; Shebenko, V.A.; Pomerantseva, M.D.; Ramajya, L.K.

    1988-01-01

    Radiocarbon 14 C is one of the most widespread radionuclides. Increased concentration of anthropogenic 14 C in the biosphere is a problem of considerable hygienic and ecological significance. The paper presents the results of comprehensive studies for years on biokinetics of the main 14 C compounds, inorganic (Na H 14 CO 3 , Na 2 14 CO 3 , K 2 14 CO 3 , Ca 14 CO 3 ) as well as organic ( 14 C-glucose, 14 C-succinic acid, 14 C-glucosamine, 14 C-glycine, 14 C-tryptophane, 14 C-valine, 14 C-palmitic acid, 14 C-stearic acid, 14 C-ethyl alcohol, 14 C-methyl alcohol, 14 C-urea), of 14 C as food constituent and of elementary radiocarbon. The 14 C toxicity is investigated for both acute and chronic small doses received by animals. The nuclide's genetic efficiency is assessed. Based on research evidence, the accumulation multiple and equilibrium time are estimated for long-term 14 C intake by humans. The data may be used for setting genetic standards and estimating an anthropogenic increase of 14 C concentration in the environment. The hazard of anthropogenic radiocarbon is assessed with allowance for further development of nuclear power industry. (author)

  1. Pharmacokinetics of [14C]methylglyoxal-bis-guanylhydrazone) in patients with leukemia.

    Science.gov (United States)

    Rosenblum, M G; Keating, M J; Yap, B S; Loo, T L

    1981-05-01

    Methylglyoxal-bis(guanylhydrazone) (MGBG; NSC 32946), a competitive inhibitor of S-adenosyl-L-methionine decarboxylase (EC 4.1.1.50), currently being reevaluated for its clinical antileukemic activity. MGBG labeled with 14C in the guanylhydrazone moiety was administered i.v. (150 microCi; specific activity, 1.9 microCi/mumol; 20 mg total) to six patients with leukemia. All patients in the study had normal renal and hepatic function. [14C]MGBG underwent no in vivo metabolism; it disappeared from the plasma with an average terminal t 1/2 of 4.1 hr. The 72-hr cumulative urinary excretion was only 14.5 +/- 2.2% (S.E.M.) of the total radioactive dose. The apparent volume of distribution was 661 ml/kg and the total clearance rate was 21.2 ml/kg/min. The low urinary excretion rate and the relatively rapid plasma clearance suggest that MGBG may be sequestered in the body. Therefore, if MGBG is administered by a frequent treatment schedule, the prolonged biological half-life in humans may significantly contribute to its clinical toxicity.

  2. Measurement of the transverse emittance for the NSC Pelletron

    International Nuclear Information System (INIS)

    Rodriques, G.; Mandal, A.; Chopra, S.; Joshi, R.; Datta, S.K.; Roy, A.

    1998-01-01

    The knowledge of the emittance (transverse and longitudinal) of the NSC pelletron is essential for matching the acceptance of the LINAC which is to be installed to augment the pelletron beam energies. The transverse emittance of NSC pelletron has been measured by employing a focussing element and a down-stream beam profile monitor

  3. Oxidation of propionic acid-3-14C with alkaline permanganate

    International Nuclear Information System (INIS)

    Zielinski, M.

    1981-01-01

    The mechanism of oxidation of propionic acid with permanganate in alkaline medium was reinvestigated using methyl- 14 C labelled propionate. The preferential rupture of the αC-βC bond in propionate in highly concentrated alkaline solutions of NaOH (and KOH) was confirmed and the appearance of 14 C-labelled oxalate explained by the formation of the symmetrical intermediate which decomposes in two different modes. (author)

  4. Targeted inhibition of disheveled PDZ domain via NSC668036 depresses fibrotic process

    Energy Technology Data Exchange (ETDEWEB)

    Wang, Cong, E-mail: wangcongweihai@126.com [Immunology and Reproduction Biology Laboratory, Medical School, Nanjing University, Nanjing, Hankou Road 22, Jiangsu 210093 (China); Jiangsu Key Laboratory of Molecular Medicine, Nanjing University, Nanjing, Jiangsu 210093 (China); State Key Laboratory of Analytical Chemistry for Life Science, Nanjing University, Nanjing, Jiangsu 210093 (China); Dai, Jinghong, E-mail: daijinghongnew@163.com [Department of Respiratory Medicine, Nanjing Drum Tower Hospital Affiliated to Medical School of Nanjing University (China); Sun, Zhaorui, E-mail: lanseyunduan@163.com [Immunology and Reproduction Biology Laboratory, Medical School, Nanjing University, Nanjing, Hankou Road 22, Jiangsu 210093 (China); Jiangsu Key Laboratory of Molecular Medicine, Nanjing University, Nanjing, Jiangsu 210093 (China); State Key Laboratory of Analytical Chemistry for Life Science, Nanjing University, Nanjing, Jiangsu 210093 (China); Department of Emergency, Jinling Hospital, Medical School, Nanjing University, Nanjing, Jiangsu 210093 (China); Shi, Chaowen, E-mail: willscw@live.cn [Immunology and Reproduction Biology Laboratory, Medical School, Nanjing University, Nanjing, Hankou Road 22, Jiangsu 210093 (China); Jiangsu Key Laboratory of Molecular Medicine, Nanjing University, Nanjing, Jiangsu 210093 (China); State Key Laboratory of Analytical Chemistry for Life Science, Nanjing University, Nanjing, Jiangsu 210093 (China); Cao, Honghui, E-mail: caohonghui92@gmail.com [Immunology and Reproduction Biology Laboratory, Medical School, Nanjing University, Nanjing, Hankou Road 22, Jiangsu 210093 (China); Jiangsu Key Laboratory of Molecular Medicine, Nanjing University, Nanjing, Jiangsu 210093 (China); State Key Laboratory of Analytical Chemistry for Life Science, Nanjing University, Nanjing, Jiangsu 210093 (China); and others

    2015-02-01

    In this study, we determined the effects of transforming growth factor-beta (TGF-β) and Wnt/β-catenin signaling on myofibroblast differentiation of NIH/3T3 fibroblasts in vitro and evaluated the therapeutic efficacy of NSC668036 in bleomycin-induced pulmonary fibrosis murine model. In vitro study, NSC668036, a small organic inhibitor of the PDZ domain in Dvl, suppressed β-catenin-driven gene transcription and abolished TGF-β1-induced migration, expression of collagen I and α-smooth muscle actin (α-SMA) in fibroblasts. In vivo study, we found that NSC668036 significantly suppressed accumulation of collagen I, α-SMA, and TGF-β1 but increased the expression of CK19, Occludin and E-cadherin that can inhibit pulmonary fibrogenesis. Because fibrotic lung exhibit aberrant activation of Wnt/β-catenin signaling, these data collectively suggest that inhibition of Wnt/β-catenin signaling at the Dvl level may be an effective approach to the treatment of fibrotic lung diseases. - Highlights: • NSC668036 inhibited the proliferation and migration of NIH/3T3 fibroblasts. • NSC668036 suppressed the Wnt/β-catenin signaling pathway. • TGF-β-induced stimulation of profibrotic responses were inhibited by NSC668036. • NSC668036 can inhibit the development of bleomycin-induced pulmonary fibrosis.

  5. Superconducting linear accelerator system for NSC

    Indian Academy of Sciences (India)

    59, No. 5. — journal of. November 2002 physics pp. 849–858. Superconducting linear accelerator system for NSC ... cryogenics facility, RF electronics development, facilities for fabricating niobium resonators indige- ... Prototype resonator was.

  6. The synthesis of [O-methyl-{sup 11}C]venlafaxine: a non-classical, fast-acting antidepressant

    Energy Technology Data Exchange (ETDEWEB)

    Gee, A.D.; Gjedde, A. [Aarhus Univ. Hospital, PET Center, Aarhus (Denmark); Smith, D.F. [Aarhus Univ. Psychiatric Hospital, Inst. for Biological Psychiatry, Risskov (Denmark)

    1997-01-01

    As part of our program to develop PET tracers for the 5-HT reuptake site, venlafaxine, a non-classical, fast-acting antidepressant, was selected as a candidate for labelling with {sup 11}C for in vivo evaluation. [O-methyl-{sup 11}C]venlafaxine was produced by the alkylation of O-desmethyl venlafaxine with [{sup 11}C]methyl iodide followed by HPLC purification and formulation. Radiochemically pure [O-methyl-{sup 11}C]venlafaxine was obtained in a 30 {+-} 5% decay corrected radiochemical yield and a specific activity > 50 GBq/{mu}mol(1.4 Ci/{mu}mol) at the end of synthesis. For a typical production starting with 46 GBq (1.3 Ci) [{sup 11}C]CO{sub 2}, 5.2 GBq (140 mCi) [O-methyl-{sup 11}C]venlafaxine was obtained as a sterile, formulated solution in a synthesis time of 30 min (counted from EOB). (Author).

  7. DNA methylation regulates expression of VEGF-C, and S-adenosylmethionine is effective for VEGF-C methylation and for inhibiting cancer growth

    Energy Technology Data Exchange (ETDEWEB)

    Da, M.X. [Department of Surgical Oncology, Gansu Provincial Hospital, Lanzhou (China); Zhang, Y.B. [Department of Surgery, Ningxia Medical University, Yinchuan (China); Yao, J.B. [Department of Surgical Oncology, Gansu Provincial Hospital, Lanzhou (China); Duan, Y.X. [Department of Surgery, Ningxia Medical University, Yinchuan (China)

    2014-09-30

    DNA hypomethylation may activate oncogene transcription, thus promoting carcinogenesis and tumor development. S-adenosylmethionine (SAM) is a methyl donor in numerous methylation reactions and acts as an inhibitor of intracellular demethylase activity, which results in hypermethylation of DNA. The main objectives of this study were to determine whether DNA hypomethylation correlated with vascular endothelial growth factor-C (VEGF-C) expression, and the effect of SAM on VEGF-C methylation and gastric cancer growth inhibition. VEGF-C expression was assayed by Western blotting and RT-qPCR in gastric cancer cells, and by immunohistochemistry in tumor xenografts. VEGF-C methylation was assayed by bisulfite DNA sequencing. The effect of SAM on cell apoptosis was assayed by flow cytometry analyses and its effect on cancer growth was assessed in nude mice. The VEGF-C promoters of MGC-803, BGC-823, and SGC-7901 gastric cancer cells, which normally express VEGF-C, were nearly unmethylated. After SAM treatment, the VEGF-C promoters in these cells were highly methylated and VEGF-C expression was downregulated. SAM also significantly inhibited tumor growth in vitro and in vivo. DNA methylation regulates expression of VEGF-C. SAM can effectively induce VEGF-C methylation, reduce the expression of VEGF-C, and inhibit tumor growth. SAM has potential as a drug therapy to silence oncogenes and block the progression of gastric cancer.

  8. Differentiated NSC-34 motoneuron-like cells as experimental model for cholinergic neurodegeneration.

    Science.gov (United States)

    Maier, Oliver; Böhm, Julia; Dahm, Michael; Brück, Stefan; Beyer, Cordian; Johann, Sonja

    2013-06-01

    Alpha-motoneurons appear to be exceedingly affected in neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS). Morphological and physiological degeneration of this neuronal phenotype is typically characterized by a marked decrease of neuronal markers and by alterations of cholinergic metabolism such as reduced choline acetyltransferase (ChAT) expression. The motoneuron-like cell line NSC-34 is a hybrid cell line produced by fusion of neuroblastoma with mouse motoneuron-enriched primary spinal cord cells. In order to further establish this cell line as a valid model system to investigate cholinergic neurodegeneration, NSC-34 cells were differentiated by serum deprivation and additional treatment with all-trans retinoic acid (atRA). Cell maturation was characterized by neurite outgrowth and increased expression of neuronal and cholinergic markers, including MAP2, GAP-43 and ChAT. Subsequently, we used differentiated NSC-34 cells to study early degenerative responses following exposure to various neurotoxins (H2O2, TNF-α, and glutamate). Susceptibility to toxin-induced cell death was determined by means of morphological changes, expression of neuronal marker proteins, and the ratio of pro-(Bax) to anti-(Bcl-2) apoptotic proteins. NSC-34 cells respond to low doses of neurotoxins with increased cell death of remaining undifferentiated cells with no obvious adverse effects on differentiated cells. Thus, the different vulnerability of differentiated and undifferentiated NSC-34 cells to neurotoxins is a key characteristic of NSC-34 cells and has to be considered in neurotoxic studies. Nonetheless, application of atRA induced differentiation of NSC-34 cells and provides a suitable model to investigate molecular events linked to neurodegeneration of differentiated neurons. Copyright © 2013 Elsevier Ltd. All rights reserved.

  9. A simple and efficient method for generating Nurr1-positive neuronal stem cells from human wisdom teeth (tNSC) and the potential of tNSC for stroke therapy.

    Science.gov (United States)

    Yang, Kuo-Liang; Chen, Mei-Fang; Liao, Chia-Hsin; Pang, Cheng-Yoong; Lin, Py-Yu

    2009-01-01

    We have isolated human neuronal stem cells from exfoliated third molars (wisdom teeth) using a simple and efficient method. The cultured neuronal stem cells (designated tNSC) expressed embryonic and adult stem cell markers, markers for chemotatic factor and its corresponding ligand, as well as neuron proteins. The tNSC expressed genes of Nurr1, NF-M and nestin. They were used to treat middle cerebral artery occlusion (MCAO) surgery-inflicted Sprague-Dawley (SD) rats to assess their therapeutic potential for stroke therapy. For each tNSC cell line, a normal human impacted wisdom tooth was collected from a donor with consent. The tooth was cleaned thoroughly with normal saline. The molar was vigorously shaken or vortexed for 30 min in a 50-mL conical tube with 15-20mL normal saline. The mixture of dental pulp was collected by centrifugation and cultured in a 25-cm(2) tissue culture flask with 4-5mL Medium 199 supplemented with 5-10% fetal calf serum. The tNSC harvested from tissue culture, at a concentration of 1-2x10(5), were suspended in 3 microL saline solution and injected into the right dorsolateral striatum of experimental animals inflicted with MCAO. Behavioral measurements of the tNSC-treated SD rats showed a significant recovery from neurologic dysfunction after MCAO treatment. In contrast, a sham group of SD rats failed to recover from the surgery. Immunohistochemistry analysis of brain sections of the tNSC-treated SD rats showed survival of the transplanted cells. These results suggest that adult neuronal stem cells may be procured from third molars, and tNSC thus cultivated have potential for treatment of stroke-inflicted rats.

  10. NSC23925, identified in a high-throughput cell-based screen, reverses multidrug resistance.

    Directory of Open Access Journals (Sweden)

    Zhenfeng Duan

    2009-10-01

    Full Text Available Multidrug resistance (MDR is a major factor which contributes to the failure of cancer chemotherapy, and numerous efforts have been attempted to overcome MDR. To date, none of these attempts have yielded a tolerable and effective therapy to reverse MDR; thus, identification of new agents would be useful both clinically and scientifically.To identify small molecule compounds that can reverse chemoresistance, we developed a 96-well plate high-throughput cell-based screening assay in a paclitaxel resistant ovarian cancer cell line. Coincubating cells with a sublethal concentration of paclitaxel in combination with each of 2,000 small molecule compounds from the National Cancer Institute Diversity Set Library, we identified a previously uncharacterized molecule, NSC23925, that inhibits Pgp1 and reverses MDR1 (Pgp1 but does not inhibit MRP or BCRP-mediated MDR. The cytotoxic activity of NSC23925 was further evaluated using a panel of cancer cell lines expressing Pgp1, MRP, and BCRP. We found that at a concentration of >10 microM NSC23925 moderately inhibits the proliferation of both sensitive and resistant cell lines with almost equal activity, but its inhibitory effect was not altered by co-incubation with the Pgp1 inhibitor, verapamil, suggesting that NSC23925 itself is not a substrate of Pgp1. Additionally, NSC23925 increases the intracellular accumulation of Pgp1 substrates: calcein AM, Rhodamine-123, paclitaxel, mitoxantrone, and doxorubicin. Interestingly, we further observed that, although NSC23925 directly inhibits the function of Pgp1 in a dose-dependent manner without altering the total expression level of Pgp1, NSC23925 actually stimulates ATPase activity of Pgp, a phenomenon seen in other Pgp inhibitors.The ability of NSC23925 to restore sensitivity to the cytotoxic effects of chemotherapy or to prevent resistance could significantly benefit cancer patients.

  11. Chemotherapy of Malignant Melanoma with Dimethyl Triazeno Imidazole Carboxamide (DTIC) and Nitrosourea Derivatives (BCNU, CCNU)

    Science.gov (United States)

    Hill, George J.; Ruess, Robert; Berris, Robert; Philpott, Gordon W.; Parkin, Priscilla

    1974-01-01

    Chemotherapy for metastatic melanoma was performed in 80 consecutive evaluable patients. DTIC, BCNU and CCNU produced responses in 28% of patients, alone or in combination with each other. Three of 62 patients treated with DTIC remain free of tumor, off therapy at 18-36 months following objective regression of metastases. Chemotherapy with commercially available drugs continued to be uniformly unsuccessful. DTIC was used successfully in treatment of extensive extracranial disease, including one patient with metastatic melanoma during pregnancy. Cerebral metastases were the sole or major cause of death in 8/9 patients who relapsed following control with DTIC for nine months or longer, and one patient developed a carcinoma of the breast following therapy with DTIC and BCNU. Remission was induced in two patients with intralesional BCG, after prior attempts to control metastases with DTIC and combination chemotherapy. ImagesFig. 2.Fig. 2b.Fig. 2c. PMID:4601984

  12. The 16-MV pelletron accelerator at NSC

    International Nuclear Information System (INIS)

    Narayanan, M.M.; Chopra, S.; Kanjilal, D.

    1994-01-01

    A 15-UD 16-MV Pelletron accelerator was commissioned at Nuclear Science Centre (NSC) in July 1991. It is a large tandem Van de Graaff type electrostatic accelerator capable of accelerating almost any ion beam from hydrogen to uranium to energies from a few tens of MeV (Million electron Volts) to hundreds of MeV. The availability of the various beams having widely variable energy, good energy resolution and excellent quality makes this accelerator an extremely versatile machine. This gives rise to the possibilities of basic and applied research in various disciplines of science. The principle of operation of a tandem accelerator and the salient features of the accelerator system at NSC are described. (author). 2 refs., 4 figs

  13. Absorption, Translocation and Metabolism of {sup 14}C-Labelled Dichlobenil

    Energy Technology Data Exchange (ETDEWEB)

    Pate, D. A.; Funderburk, Jr., H. H. [Auburn University Agricultural Experiment Station, Auburn, AL (United States)

    1966-05-15

    Autoradiographs of bean (Phaseolus vulgaris L.) and alligatorweed (Alternanthera philoxeroides (Mart.) Griseb.) indicated that {sup 14}C-nitrile-labelled dichlobenil (2,6-dichlorobenzonitrile) was slightly absorbed by the leaf and some translocation occurred following foliar application. Plants with roots submersed in radioactive aqueous solution absorbed and translocated the {sup 14}C throughout the plant. An investigation of some of the chemical and physical properties of {sup 14}C-nitrile-labelled dichlobenil was conducted. Loss because of volatilization from counting planchets was considerably reduced by application of acrylic plastic immediately after the solution dried. The plastic coating also eliminated contamination of counting chambers and windows. Two higher plants (bean and alligatorweed ) and four fungi (Fusarium sp., Geotrichum sp., Penicillium sp., Trichoderma sp.) were selected for metabolism studies. Dichlobenil- {sup 14}C was added to Hoagland and Arnon's nutrient solution containing beans or alligatorweed and to liquid cultures containing the other organisms for 12 to 120 h. Extracts from the plants or fungi were chromatographed on silica gel thin-layers. Autoradiographs of the thin-layer chromatographed aqueous extracts revealed a {sup C}-labelled compound of Rf 0.25 that differed from that of dichlobenil, which was 0.6. After esterification of the extracts, a {sup 14}C-labelled compound was observed at Rf 0.95 on thin-layer chromatograms. Chromatography of the unaltered extracts with 2,6- dichlorobenzoic acid revealed identical Rf-values. The esterified aqueous extracts chromatographed precisely with methyl-2,6-dichlorobenzoate. Gas chromatography of the {sup 14}C-labelled compound with an Rf of 0.95 exhibited a retention time identical to that of methyl-2,6-dichlorobenzoate. The quantity of {sup 14}C-labelled compound that chromatographed as 2,6-dichlorobenzoate increased with time of exposure of the various test organisms to dichlobenil {sup

  14. C-Methylated Flavonoids from Cleistocalyx operculatus and Their Inhibitory Effects on Novel Influenza A (H1N1) Neuraminidase

    DEFF Research Database (Denmark)

    Dao, Trong-Tuan; Tung, Bui-Thanh; Nguyen, Phi-Hung

    2010-01-01

    As part of an ongoing study focused on the discovery of anti-influenza agents from plants, four new (1-4) and 10 known (5-14) C-methylated flavonoids were isolated from a methanol extract of Cleistocalyx operculatus buds using an influenza H1N1 neuraminidase inhibition assay. Compounds 4, 7, 8...... mutant) expressed in 293T cells with IC50 values of 8.15 ± 1.05 and 3.31 ± 1.34 μM, respectively. Compounds 4, 7, 8, and 14 behaved as noncompetitive inhibitors in the kinetic studies. These results indicate that C-methylated flavonoids from C. operculatus have the potential to be developed...

  15. The synthesis of carbon-14 labeled pravastatin

    International Nuclear Information System (INIS)

    Wallace, M.A.; Dean, D.C.; Ellsworth, R.L.; Melillo, D.G.; Marks, T.; White, R.F.

    1993-01-01

    An asymmetric route to [ 14 C]β-hydroxycompactin 1 bearing the (S)-2-methyl-[1- 14 C]butanoate side chain has been developed. Methylation of [N-[1- 14 C]butyryl]-4-(S)-phenylmethyl-2-oxazolidinone 4 afforded a 95:5 mixture of diastereomeric [N-(S,R)-2-methyl-[1- 14 C]butyryl]-4-(S)-phenylmethyl-2-oxazolidi nones 5,6 which were separated by preparative HPLC. Oxidative cleavage of 5 afforded optically pure (S)-2-methyl-[1- 14 C]butanoic acid. Acylation of alcohol 9 with optically pure (S)-2-methyl-[1- 14 C] butyryl chloride afforded ester 10. Removal of the silyl ether produced diastereomerically pure compactin 11. Hydroxylation was carried out by biotransformation with Mucor hiemelus to afford diastereomerically pure [[1- 14 C]butanoate]β-hydroxycompactin, [ 14 C]Pravastatin 1. (Author)

  16. Plans for AMS at the NSC pelletron

    International Nuclear Information System (INIS)

    Narayanan, M.M.; Datta, S.K.; Avasti, D.K.; Madhusoodanan, T.; Mandal, S.

    1996-01-01

    The Nuclear Science Centre (NSC) is equipped with a 15UD Pelletron accelerator. The plans for conducting Accelerator Mass Spectrometry (AMS) experiments without any modifications to the existing system and the initial tests are described

  17. Reaction products from N-methyl-N-nitrosourea and deoxyribonucleic acid containing thymidine residues. Synthesis and identification of a new methylation product, O4-methyl-thymidine

    Science.gov (United States)

    Lawley, P. D.; Orr, D. J.; Shah, S. A.; Farmer, P. B.; Jarman, M.

    1973-01-01

    1. DNA was treated with N-methyl-N-nitrosourea at pH7–8, 37°C, degraded to yield 3- and 7-methylpurines and deoxyribonucleosides and the reaction products were separated by chromatography on ion-exchange resins. The following methods for identification and determination of products were used: with unlabelled N-methyl-N-nitrosourea, u.v. absorption; use of methyl-14C-labelled N-methyl-N-nitrosourea and use of [14C]thymine-labelled DNA. 2. The synthesis of O4-methylthymidine and its identification by u.v. and mass spectroscopy are reported. 3. 3-Methylthymidine and O4-methylthymidine were found as methylation products from N-methyl-N-nitrosourea with thymidine and with DNA, in relatively small yields. Unidentified products containing thymine were found in enzymic digests of N-methyl-N-nitrosourea-treated DNA, which may be phosphotriesters. 4. The possible role of formation of methylthymines in mutagenesis by N-methyl-N-nitrosourea is discussed. PMID:4798180

  18. Impact of long term applications of cotton pesticides on soil biological properties, dissipation of [14C]-methyl parathion and persistence of multi-pesticide residues

    International Nuclear Information System (INIS)

    Andrea, M.M.; Peres, T.B.; Luchini, L.C.; Marcondes, M.A.; Pettinelli, A. Jr.; Nakagawa, L.E.

    2001-01-01

    Biological parameters were followed in soils from a cotton farm (Tatui) where the recommended pesticides have been used for years, and from an experimental field (Sao Paulo) which was subdivided in two areas: one received the recommended pesticides and the other was maintained untreated. The soil bioactivities monitored from 1995 to 1998, after different pesticide applications, were: basal and glucose-induced respiration; anaerobic activity; nitrification rate; activity of the enzymes: dehydrogenase, aryl sulfatase and arginine deaminase; the soil capacity to mineralize an aromatic pesticide molecule ([ 14 C]-2,4-D), fungal and bacterial contributions for soil respiration until the beginning of 1998, and fungal and bacterial numbers from the beginning of 1998. The dissipation of [ 14 C]-methyl parathion - one of the recommended pesticides - was followed by radiometric techniques only in Sao Paulo, but persistence of multi-residues was determined in both soils by gas-liquid chromatography. All the biological parameters varied each sampling time and values also varied among soil samples, being inhibited or stimulated by the different pesticide applications, but they mostly recovered the initially detected activity. Dissipation of methyl parathion was fast and not affected by the other pesticide applications. Pesticide residues varied between the two soils but were mostly low after all applications, which indicates their dissipation. (author)

  19. Micro-syntheses for the use of carbon 13 or carbon 14. Micro-preparations of methyl alcohol, methyl iodide, and sodium acetate labeled in the methyl group; Microsyntheses pour l'emploi de carbone 13 ou de carbone 14. Micropreparations d'alcool methylique, d'iodure de methyle et d'acetate de sodium marque sur le groupement methyle

    Energy Technology Data Exchange (ETDEWEB)

    Baret, C; Pichat, L

    1951-11-01

    Apparatus and technique are described in detail for (1) reduction of CO{sub 2} to CH{sub 3}OH with LiAlH{sub 4}, (2) conversion of the methanol to CH{sub 3}I by HI, (3) formation of the Mg Grignard reagent, and (4) addition of inactive CO{sub 2} to form CH{sub 3}COOH. All these operations have been carried out on 0.005 moles. Methyl-labeled Na acetate has been prepared in 67% yield based on the Ba{sup 14}CO{sub 3} used as starting material. (author) [French] Description detaillee d'une technique deja connue pour la reduction du gaz carbonique en alcool methylique par LiAlH{sub 4}. Conversion du methanol en iodure de methyle. Ce dernier transforme en reactif de Grigard, et carbonate, fournit de l'acide acetique. Toutes ces operations on ete effectuees sur 5 x 10{sup -3} moles. La methode a ete appliquee a la synthese d'acetate de sodium marque par le groupement methyle par {sup 14}C avec un rendement global de 67% base sur le carbonate de baryum radioactif mis en oeuvre. (auteurs)

  20. Metabolism of 14C-diazinon by gypsy moth larvae

    International Nuclear Information System (INIS)

    Ahmad, S.; Forgashi, A.J.

    1975-01-01

    The metabolic fate of diazinon in larvae of Porthetria dispar (L.) was determined using 14 C-ring-labeled material. Following a 4-h ingestion period, 28.7 percent of the total recovered activity was present as diazinon in the larvae and 0.2 percent in the feces at 1 hr; by 12 h these amounts had changed to 1.4 and 15.4 percent, respectively. The major transformation products were 2,isopropyl-4-methyl-6-pyrimidinol greater than diazoxon greater than hydroxydiazinon greater than 2-(2'-hydroxy-2'-propyl)-4-methyl-6-pyrimidinol. Small amounts of 5 additional products were detected but were not identified. Metabolism of topically applied diazinon was the same qualitatively as that of ingested diazinon, based on a comparison of chloroform-extractable metabolites, although quantitative differences were evident. The synergists 2,6-dichlorobenzyl-2-propynyl ether (GA4-282) and piperonyl butoxide (PB) altered the metabolism of diazinon (both ingested and topical doses) by apparently similar actions, resulting in a reduction in the formation of 2-isopropyl-4-methyl-6-pyrimidinol, hydroxydiazinon, and 2-(2'-hydroxy-2'-propyl)-4-methyl-6-pyrimidinol

  1. Methylation of food commodities during fumigation with methyl bromide

    International Nuclear Information System (INIS)

    Starratt, A.N.; Bond, E.J.

    1990-01-01

    Sites of methylation in several commodities (wheat, oatmeal, peanuts, almonds, apples, oranges, maize, alfalfa and potatoes) during fumigation with 14 C-methyl bromide were studied. Differences were observed in levels of the major volatiles: methanol, dimethyl sulphide and methyl mercaptan, products of O- and S-methylation, resulting from treatment of the fumigated materials with 1N sodium hydroxide. In studies of maize and wheat, histidine was the amino acid which underwent the highest level of N-methylation. (author). 24 refs, 3 tabs

  2. Preparation of 14C-labeled 8,9-didehydro-6,8-dimethyl-2-methylthioergoline mesylate, a dopamine antagonist potentially useful in the treatment of schizophrenia

    International Nuclear Information System (INIS)

    Wheeler, W.J.

    1988-01-01

    We have prepared 14 C-labeled 8,9-didehydro-6,8-dimethyl-2-methyl-thioergoline mesylate (LY 170542), a dopamine antagonist potentially useful as an anti-psychotic. The 14 C-label was introduced via a novel application of the Wittig reaction on 1-(4'-toluene-sulfonyl)-8,9-didehydro-6-methyl-ergolin-8-one and subsequent reduction of 1-(4'-toluenesulfonyl)-17-[ 14 C]-lysergene by lithium/ammonia at -33 0 C. The 17-[ 14 C]-agroclavine thus prepared was converted into 17-[ 14 C]-LY 170542 by reaction with methanesulfenyl chloride/methanesulfonic acid. (author)

  3. How low can you go? Assessing minimum concentrations of NSC in carbon limited tree saplings

    Science.gov (United States)

    Hoch, Guenter; Hartmann, Henrik; Schwendener, Andrea

    2016-04-01

    Tissue concentrations of non-structural carbohydrates (NSC) are frequently used to determine the carbon balance of plants. Over the last years, an increasing number of studies have inferred carbon starvation in trees under environmental stress like drought from low tissue NSC concentrations. However, such inferences are limited by the fact that minimum concentrations of NSC required for survival are not known. So far, it was hypothesized that even under lethal carbon starvation, starch and low molecular sugar concentrations cannot be completely depleted and that minimum NSC concentrations at death vary across tissues and species. Here we present results of an experiment that aimed to determine minimum NSC concentrations in different tissues of saplings of two broad-leaved tree species (Acer pseudoplatanus and Quercus petratea) exposed to lethal carbon starvation via continuous darkening. In addition, we investigated recovery rates of NSC concentrations in saplings that had been darkened for different periods of time and were then re-exposed to light. Both species survived continuous darkening for about 12 weeks (confirmed by testing the ability to re-sprout after darkness). In all investigated tissues, starch concentrations declined close to zero within three to six weeks of darkness. Low molecular sugars also decreased strongly within the first weeks of darkness, but seemed to stabilize at low concentrations of 0.5 to 2 % dry matter (depending on tissue and species) almost until death. NSC concentrations recovered surprisingly fast in saplings that were re-exposed to light. After 3 weeks of continuous darkness, tissue NSC concentrations recovered within 6 weeks to levels of unshaded control saplings in all tissues and in both species. To our knowledge, this study represents the first experimental attempt to quantify minimum tissue NSC concentrations at lethal carbon starvation. Most importantly, our results suggest that carbon-starved tree saplings are able to

  4. Mineralization of 14C-labelled aromatic pesticide molecules in Egyptian soils under aerobic and anaerobic conditions

    International Nuclear Information System (INIS)

    Zayed, S.M.A.D.; Earghaly, M.; Mahdy, F.; El-Maghraby, S.; Taha, H.; Soliman, S.M.

    2001-01-01

    The mineralization of 2,4-D, carbofuran and pirimiphos-methyl in Egyptian soils was studied over a period of 90 days. Laboratory studies under aerobic and anaerobic conditions were conducted using 14 C-ring labelled pesticides. Under anaerobic conditions 10-14% of applied ring labelled 2,4-D mineralized during 90 days with no significant variations due to soil type. Under aerobic conditions, 2,4-D mineralized more readily in clay soil to reach 29-34% of applied dose within 90 days. In clay loam soil, 14 C-carbofuran and 14 C-pirimiphos-methyl mineralized at a rather slow rate to reach 12-14% and 12-13% of applied dose in 90 days, respectively under aerobic conditions. Generally, soils repeatedly treated with pesticides gave a slightly lower percentage of mineralization than control soils. In all studies, the soil extractable pesticide residues decreased with time and the bound residues gradually increased. The highest binding affinity of about 26-29% was observed with 2,4-D in clay soil under aerobic conditions in 90 days. Carbofuran, and pirimiphos-methyl, on the other hand, had lower binding capacity that did not exceed 16% of applied radioactivity. (author)

  5. The synthesis of nucleoside bases with 14 C

    International Nuclear Information System (INIS)

    Matloubi, H.; Mehrdad, M.

    1997-01-01

    Labelled organic compounds have been widely and diligently applied to research problems in life science and chemistry. In many laboratories they have lost their novelty and have been become conventional research tools since long time ago. these applications frequently require organic compounds substituted (or labelled) with isotopes, but the isotopes are (with certain exception) extracted in first place in simple inorganic forms. The conversion of these simple form into the more or less complex labelled compounds called for by research workers has become in effect a new branch of practical organic chemistry. The preparation of labelled compounds, carbon-14 is probably more extensively and variously used than any other isotope. It emits only beta-particles. In this project, two kinds of nucleoside bases under the name uracil-2- 14 C and thymine (methyl- 14 C) were prepared.(author). 14 refs., 3 figs., 2 tabs

  6. Effects of cerebrolysin on motor-neuron-like NSC-34 cells

    Energy Technology Data Exchange (ETDEWEB)

    Keilhoff, Gerburg, E-mail: Gerburg.keilhoff@med.ovgu.de [Institute of Biochemistry and Cell Biology, Otto-von-Guericke University Magdeburg, Leipziger Str. 44, D-39120 Magdeburg (Germany); Lucas, Benjamin; Pinkernelle, Josephine; Steiner, Michael [Institute of Biochemistry and Cell Biology, Otto-von-Guericke University Magdeburg, Leipziger Str. 44, D-39120 Magdeburg (Germany); Fansa, Hisham [Department of Plastic, Reconstructive and Aesthetic Surgery, Hand Surgery, Klinikum Bielefeld, Teutoburger Str. 50, D-33604 Bielefeld (Germany)

    2014-10-01

    Although the peripheral nervous system is capable of regeneration, this capability is limited. As a potential means of augmenting nerve regeneration, the effects of cerebrolysin (CL) – a proteolytic peptide fraction – were tested in vitro on the motor-neuron-like NSC-34 cell line and organotypic spinal cord cultures. Therefore, NSC-34 cells were subjected to mechanical stress by changing media and metabolic stress by oxygen glucose deprivation. Afterwards, cell survival/proliferation using MTT and BrdU-labeling (FACS) and neurite sprouting using ImageJ analysis were evaluated. Calpain-1, Src and α-spectrin protein expression were analyzed by Western blot. In organotypic cultures, the effect of CL on motor neuron survival and neurite sprouting was tested by immunohistochemistry. CL had a temporary anti-proliferative but initially neuroprotective effect on OGD-stressed NSC-34 cells. High-dosed or repeatedly applied CL was deleterious for cell survival. CL amplified neurite reconstruction to limited extent, affected calpain-1 protein expression and influenced calpain-mediated spectrin cleavage as a function of Src expression. In organotypic spinal cord slice cultures, CL was not able to support motor neuron survival/neurite sprouting. Moreover, it hampered astroglia and microglia activities. The data suggest that CL may have only isolated positive effects on injured spinal motor neurons. High-dosed or accumulated CL seemed to have adverse effects in treatment of spinal cord injury. Further experiments are required to optimize the conditions for a safe clinical administration of CL in spinal cord injuries. - Highlights: • Cerebrolysin (CL) is anti-proliferative but initially neuroprotective in OGD-stressed NSC-34 cells. • CL amplified neurite reconstruction of NSC-34 cells. • CL affected calpain-1 expression and calpain-mediated spectrin cleavage as function of Src expression. • In organotypic spinal cord cultures, CL hampered motor neuron survival and

  7. Effects of cerebrolysin on motor-neuron-like NSC-34 cells

    International Nuclear Information System (INIS)

    Keilhoff, Gerburg; Lucas, Benjamin; Pinkernelle, Josephine; Steiner, Michael; Fansa, Hisham

    2014-01-01

    Although the peripheral nervous system is capable of regeneration, this capability is limited. As a potential means of augmenting nerve regeneration, the effects of cerebrolysin (CL) – a proteolytic peptide fraction – were tested in vitro on the motor-neuron-like NSC-34 cell line and organotypic spinal cord cultures. Therefore, NSC-34 cells were subjected to mechanical stress by changing media and metabolic stress by oxygen glucose deprivation. Afterwards, cell survival/proliferation using MTT and BrdU-labeling (FACS) and neurite sprouting using ImageJ analysis were evaluated. Calpain-1, Src and α-spectrin protein expression were analyzed by Western blot. In organotypic cultures, the effect of CL on motor neuron survival and neurite sprouting was tested by immunohistochemistry. CL had a temporary anti-proliferative but initially neuroprotective effect on OGD-stressed NSC-34 cells. High-dosed or repeatedly applied CL was deleterious for cell survival. CL amplified neurite reconstruction to limited extent, affected calpain-1 protein expression and influenced calpain-mediated spectrin cleavage as a function of Src expression. In organotypic spinal cord slice cultures, CL was not able to support motor neuron survival/neurite sprouting. Moreover, it hampered astroglia and microglia activities. The data suggest that CL may have only isolated positive effects on injured spinal motor neurons. High-dosed or accumulated CL seemed to have adverse effects in treatment of spinal cord injury. Further experiments are required to optimize the conditions for a safe clinical administration of CL in spinal cord injuries. - Highlights: • Cerebrolysin (CL) is anti-proliferative but initially neuroprotective in OGD-stressed NSC-34 cells. • CL amplified neurite reconstruction of NSC-34 cells. • CL affected calpain-1 expression and calpain-mediated spectrin cleavage as function of Src expression. • In organotypic spinal cord cultures, CL hampered motor neuron survival and

  8. Aberrant DNA methylation of ESR1 and p14ARF genes could be useful as prognostic indicators in osteosarcoma

    Directory of Open Access Journals (Sweden)

    Sonaglio V

    2013-06-01

    Full Text Available Viviane Sonaglio,1 Ana C de Carvalho,2 Silvia R C Toledo,3,4 Carolina Salinas-Souza,3,4 André L Carvalho,5 Antonio S Petrilli,3 Beatriz de Camargo,6 André L Vettore21Pediatrics Department, A C Camargo Hospital, São Paulo, Brazil; 2Biological Science Department, Federal University of São Paulo, Diadema, Brazil; 3Department of Pediatrics, Pediatric Oncology Institute, GRAACC/Federal University of São Paulo, São Paulo, Brazil; 4Department of Morphology and Genetics, Federal University of São Paulo, São Paulo, Brazil; 5Department of Head and Neck Surgery, PIO XII Foundation, Barretos Cancer Hospital, Barretos, São Paulo, Brazil; 6Research Program Pediatric Oncology Program, CPNq, Instituto Nacional do Cancer, Rio de Janeiro, BrazilAbstract: Osteosarcoma (OS is the eighth most common form of childhood and adolescence cancer. Approximately 10%–20% of patients present metastatic disease at diagnosis and the 5-year overall survival remains around 70% for nonmetastatic patients and around 30% for metastatic patients. Metastatic disease at diagnosis and the necrosis grade induced by preoperative treatment are the only well-established prognostic factors for osteosarcoma. The DNA aberrant methylation is a frequent epigenetic alteration in humans and has been described as a molecular marker in different tumor types. This study evaluated the DNA aberrant methylation status of 18 genes in 34 OS samples without previous chemotherapy treatment and in four normal bone specimens and compared the methylation profile with clinicopathological characteristics of the patients. We were able to define a three-gene panel (AIM1, p14ARF, and ESR1 in which methylation was correlated with OS cases. The hypermethylation of p14ARF showed a significant association with the absence of metastases at diagnoses, while ESR1 hypermethylation was marginally associated with worse overall survival. This study demonstrated that aberrant promoter methylation is a common event

  9. Synthesis of N-methyl and N-11C-methyl spiperone by phase transfer catalysis in anhydrous solvent

    International Nuclear Information System (INIS)

    Omokawa, Hiroyoshi; Tanaka, Akira; Iio, Mayumi; Nishihara, Yoshiaki; Inoue, Osamu; Yamazaki, Toshio.

    1985-01-01

    Spiperone, a butyrophenone neuroleptic drug, has been used in binding studies of dopamine receptors. Langstrom et al. developed N- 11 C-methyl spiperone, and, in cooperate with Wagner et al., made it possible to visualize the distribution of dopamine receptors in the human brain in vivo. In this paper, we independently developed another synthetic method of N- 11 C-methyl spiperone using the phase transfer catalyst in an anhydrous solvent. Separation of the product is feasible only by passing the reactant solution through a Millipore filter and injecting it onto high pressure liquid chromatography (HPLC). The time required for the synthesis and purification of N- 11 C-methyl spiperone from 11 C-methyl iodide and spiperone was 20 min. Radiochemical yield exceeded 35 % against 11 C-methyl iodide without correcting decay of the radioactivity. (author)

  10. NSC KIPT's experience in production of absorber materials, composites and products for control mechanisms of various nuclear reactor types

    International Nuclear Information System (INIS)

    Odeychuk, N.P.; Zelensky, V.F.; Gurin, V.A.; Konotop, Yu.F.

    2000-01-01

    Data on NSC KIPT developments of absorber composites B 4 C-PyC and B 4 C-SiC are reported. Results of pre-reactor studies and reactor tests of absorber composites developed are given. It is shown that the B 4 C-PyC composites have a high radiation resistance at temperatures up to 1,250 deg C. (author)

  11. Synthesis and characteristics in tumor-bearing mice of N-[11C]methyl-1-deoxynojirimycin and N-[11C]methyl-1-deoxymannojirimycin

    International Nuclear Information System (INIS)

    Ishiwata, Kiichi; Sasaki, Toru; Ishii, Shin-ichi; Senda, Michio; Seki, Hiroyuki; Kitasato Univ.; Nozaki, Tadashi

    1993-01-01

    N-[ 11 C]Methyl-1-deoxynojirimycin ([ 11 C]MDNM) and N-[ 11 C]methyl-1-deoxymannojirimycin ([ 11 C]MDMM) were prepared by 11 C-methylation of 1-deoxynojirimycin (DNM) and 1-deoxymannojirimycin (DMM), which are specific inhibitors of glucosidase and mannosidase, respectively. In mice bearing Ehrich ascitic tumor, the highest uptake of the [ 11 C]MDNM was observed in the kidney, followed by the liver and small intestine, while the tumour uptake was moderate. By MDNM loading, saturable uptake was observed in these tissues. In homogenates of the kidney and tumor tissues, a considerable amount of radioactivity was detected in a high-molecular weight fraction. These results demonstrate that the [ 11 C]MDNM has a potential for imaging the glucosidase activity by positron emission tomography. On the other hand, [ 11 C]MDMM showed lower uptake than [ 11 C]MDNM in the kidney, liver and small intestine and no effect of carrier DMM, suggesting that the [ 11 C]MDMM would not reflect mannosidase activity. (Author)

  12. Distribution and mixing of old and new nonstructural carbon in two temperate trees.

    Science.gov (United States)

    Richardson, Andrew D; Carbone, Mariah S; Huggett, Brett A; Furze, Morgan E; Czimczik, Claudia I; Walker, Jennifer C; Xu, Xiaomei; Schaberg, Paul G; Murakami, Paula

    2015-04-01

    We know surprisingly little about whole-tree nonstructural carbon (NSC; primarily sugars and starch) budgets. Even less well understood is the mixing between recent photosynthetic assimilates (new NSC) and previously stored reserves. And, NSC turnover times are poorly constrained. We characterized the distribution of NSC in the stemwood, branches, and roots of two temperate trees, and we used the continuous label offered by the radiocarbon (carbon-14, (14) C) bomb spike to estimate the mean age of NSC in different tissues. NSC in branches and the outermost stemwood growth rings had the (14) C signature of the current growing season. However, NSC in older aboveground and belowground tissues was enriched in (14) C, indicating that it was produced from older assimilates. Radial patterns of (14) C in stemwood NSC showed strong mixing of NSC across the youngest growth rings, with limited 'mixing in' of younger NSC to older rings. Sugars in the outermost five growth rings, accounting for two-thirds of the stemwood pool, had a mean age  5 yr. Our results are thus consistent with a previously-hypothesized two-pool ('fast' and 'slow' cycling NSC) model structure. These pools appear to be physically distinct. © 2015 The Authors. New Phytologist © 2015 New Phytologist Trust.

  13. Studies onthe behaviour of the insecticide 14C-Pirimiphos-Methyl in aquatic species: tilapia nilotica and potamogeton crispus plant

    International Nuclear Information System (INIS)

    Afifi, L.M.; Kamel, H.A.; Aly, M.A.S.

    2003-01-01

    The bioaccumulation and depletion of 1 4C-labelled pirimiphos-methyl (O-2- diethyl amino-6-methyl pyrimidine-4-gamma l O,O-dimethyl phosphorothioa) were monitored for 6 days following a single application at 7.5 ppm to 2 aquatic species: Bolti fish (Tilapia nilotica) and a rapid growing plant (Potamogeton crispus). The bioconcentration factor (BCF) for fish was relatively low with a maximum reached at 24 hours 122 and 55 in the absence and presence of the weed respectively. Depuration of the insecticide and/or its metabolites in clear water was readily fast. Feeding the treated dried fish to rat, the substance residues were found to be bioavailable where, 75.7% of the given amount was excreted in the urine and 15.3% in the feces. TLC analysis of the urine revealed the presence of 4 metabolites: Desethyl pirimiphos-methyl, 2-diethyl amino-4-hydroxy-6-methylpyrimidine, 2-ethyl amino-4-hydroxy-6-methyl-pyrimidine and 2-amino -4-hydroxy-6- methyl- pyrimidine

  14. Synthesis of 'no-carrier-added' sup(11)C-labelled nitrosoureas

    International Nuclear Information System (INIS)

    Diksic, M.; Farrokhzad, S.; Yamamoto, Y.L.; Feindel, W.

    1985-01-01

    Syntheses for sup(11)C-labelled chemotherapeutic drugs CCNU, BFNU and CFNU (analogs of BCNU) as well as an improved synthesis for sup(11)C-BCNU are described. The procedures for the separation of dual isomers in the case of sup(11)C-labelled CCNU and CFNU are discussed. The specific activity of these 'no-carrier-added' radiopharmaceuticals was approximately 10sup(4) lower than expected for a carrier-free product. The syntheses were normally finished 20-25 min after the end of the collection of sup(11)C-COClsub(2). Chemical and radiochemical purity of the final products as determined by HPLC and TLRC, respectively, was at least 98%. The syntheses yielded 10-25 mCi of nitrosourea ready for use in PET studies. (author)

  15. Development of Plasma Technologies at IPP NSC KIPT

    International Nuclear Information System (INIS)

    Tereshin, V.I.; Chebotarev, V.V.; Garkusha, I.E.; Lapshin, V.I.; Shvets, O.M.; Taran, V.S.

    2001-01-01

    Plasma Technologies in Institute of Plasma Physics of the NSC KIPT are recently developed in the following directions. Material surfaces modification under their irradiation with pulsed plasma streams of different working gases. Besides traditional analysis of improvements of tribological characteristics and structural-phase changes of the modified layers recently we started investigations of material corrosions characteristic improvement under influence of pulsed plasma on the material surfaces. As to the surface coatings in arc discharges of Bulat type devices, new trends are related with multi-layers coatings, using Ti-AI-N coatings in cutting tools, using high frequency discharges or combined HF- and arc discharges for increasing the nomenclature of goods to be coated. Development of ozonators is respectively new area for IPP NSC KIPT. On the base of barrier high-frequency discharge there were developed a number of high efficiency ozonators with ozone production up to 100 G/hour. (author)

  16. Behaviors of 14C-butachlor, 14C-chlorpyrifos and 14C-DDT in Rana japonica japonica Guenther

    International Nuclear Information System (INIS)

    Zhang Yiqiang; Zhong Chuangguang; Zhao Xiaokui; Chen Shunhua

    2002-01-01

    The research on the behaviors of 14 C-butachlor, 14 C-chlorpyrifos and 14 C-DDT in the frog Rana japonica japonica Guenther was carried out. After administrated per os to the frogs in doses of 380, 347, 363 Bq/g, 14 C-butachlor, 14 C-chlorpyrifos and 14 C-DDT, were distributed respectively to various organs within 24 h with specific accumulating organs as gallbladder, intestine and intestine, relevantly to the pesticides described. Compared to that in gallbladder and intestine, the radioactivity of many organs was extremely low, and this might due to the characters of the pesticides. Analysis of the metabolites of 14 C-DDT in frog at 24 th hr demonstrated that DDT was difficult to be degraded. Most 14 C-butachlor, 14 C-chlorpyrifos 14 C-DDT in liver and fat or ovary of frog was extractable with acetone. However, there were some differences between the pesticides, and the organs as well. And 14 C-butachlor, 14 C-chlorpyrifos or 14 C-DDT were better bound in liver than in fat

  17. Automation of 15 UD pelletron operation at NSC

    International Nuclear Information System (INIS)

    Ojha, S.; Sota, M.; Gargari, S.; Joshi, R.; Chopra, S.; Datta, S.K.

    2003-01-01

    15 UD Pelletron accelerator facility at NSC has been operational over last 12 years. The control system of accelerator runs on an network of computers under LINUX operating system running a distributed client server system. A description of the implemented software development is given

  18. Fate of [14C]xanthotoxin (8-methoxypsoralen) in a goat and in bovine ruminal fluid

    International Nuclear Information System (INIS)

    Ivie, G.W.; Beier, R.C.; Bull, D.L.; Oertli, E.H.

    1986-01-01

    A lactating Nubian goat was treated with [ 14 C]xanthotoxin, a photosensitizing psoralen that occurs naturally in some phototoxic range plants, as a single oral dose equivalent to 10.0 mg of xanthotoxin/kg of body weight. The radiochemical was rapidly absorbed, metabolized, and excreted. Although expired air was not monitored for the presence of volatile radiocarbon, the data indicated that greater than 50% of the administered [ 14 C]xanthotoxin was metabolized by cleavage of the O-[ 14 C]methyl moiety, with subsequent loss of the label as, presumably, [ 14 C]CO 2 . Studies with bovine ruminal fluid in vitro indicated that cleavage of the O-methyl moiety of xanthotoxin could occur rapidly in the rumen. In the goat, nonmetabolized xanthotoxin was not excreted in urine, and of several metabolites in urine extracts, 3 were identified as resulting from opening of the furan or lactone ring. Only about 2% of the dose was recovered in the feces, and this consisted mainly of unmetabolized xanthotoxin. Although appreciable amounts of radiocarbon were secreted into milk, this radiocarbon was not in the form of xanthotoxin or any identifiable metabolites. The radiocarbon in milk likely resulted from the biosynthetic incorporation of [ 14 C]CO 2 into normal milk components

  19. N-[11C]methyl-3,4-methylenedioxyamphetamine (Ecstasy) and 2-methyl-N-[11C]methyl-4,5-methylenedioxyamphetamine. Synthesis and biodistribution studies

    International Nuclear Information System (INIS)

    Patt, M.; Machulla, H.J.; Guendisch, D.; Kovar, K.A.; Wuellner, U.; Blocher, A.

    1999-01-01

    In order to evaluate the neurobiological mechanism causing the psychogenic effects of methylenedioxy-derivatives of amphetamine, the carbon-11 labeled analogues of 3,4-methylenedioxymethamphetamine (MDMA), 2 and 2,N-dimethyl-4,5-methylenedioxyamphetamine (MADAM-6) 4 were prepared for application in in-vivo PET studies by methylation of 3,4-methylenedioxyamphetamine (MDA) 1 and 2-methyl-4,5-methylenedioxyamphetamine 3 with [ 11 C]CH 3 I. The radiochemical yield was determined in dependence on time, temperature and amount of precursor. The best conditions for a fast labeling reaction with carbon-11 on a preparative scale were found to be a reaction time of 10 min using 1 mg of the corresponding dimethyl-precursors 1 or 3, thus obtaining radiochemical yields of 60% (based on produced [ 11 C]CH 3 I). Biodistribution studies were performed in rats, a high brain to blood ratio of 7.5 was observed for [ 11 C]MDMA in contrast to a ratio of 3.7 for [ 11 C]MADAM-6. (author)

  20. Notch2 Signaling Maintains NSC Quiescence in the Murine Ventricular-Subventricular Zone

    Directory of Open Access Journals (Sweden)

    Anna Engler

    2018-01-01

    Full Text Available Neurogenesis continues in the ventricular-subventricular zone (V-SVZ of the adult forebrain from quiescent neural stem cells (NSCs. V-SVZ NSCs are a reservoir for new olfactory bulb (OB neurons that migrate through the rostral migratory stream (RMS. To generate neurons, V-SVZ NSCs need to activate and enter the cell cycle. The mechanisms underlying NSC transition from quiescence to activity are poorly understood. We show that Notch2, but not Notch1, signaling conveys quiescence to V-SVZ NSCs by repressing cell-cycle-related genes and neurogenesis. Loss of Notch2 activates quiescent NSCs, which proliferate and generate new neurons of the OB lineage. Notch2 deficiency results in accelerated V-SVZ NSC exhaustion and an aging-like phenotype. Simultaneous loss of Notch1 and Notch2 resembled the total loss of Rbpj-mediated canonical Notch signaling; thus, Notch2 functions are not compensated in NSCs, and Notch2 is indispensable for the maintenance of NSC quiescence in the adult V-SVZ.

  1. Methyl bromide residues in fumigated cocoa beans

    International Nuclear Information System (INIS)

    Adomako, D.

    1975-01-01

    The 14 C activity in unroasted [ 14 C]-methyl bromide fumigated cocoa beans was used to study the fate and persistence of CH 3 Br in the stored beans. About 70% of the residues occurred in the shells. Unchanged CH 3 Br could not be detected, all the sorbed CH 3 Br having reacted with bean constituents apparently to form 14 C-methylated derivatives and inorganic bromide. No 14 C activity was found in the lipid fraction. Roasting decreased the bound (non-volatile) residues, with corresponding changes in the activities and amounts of free sugars, free and protein amino acids. Roasted nibs and shells showed a two-fold increase in the volatile fraction of the 14 C residue. This fraction may be related to the volatile aroma compounds formed by Maillard-type reactions. (author)

  2. Introduction of antineoplastic drug NSC631570 in an inpatient and outpatient setting: Comparative evaluation of biological effects

    Directory of Open Access Journals (Sweden)

    Mariia Rudyk

    2016-04-01

    Full Text Available The aim of this study is to evaluate the effect of moderate physical exercise and treatment time on the organism's response to NSC631570. The sensitivity of circulating phagocytes to the drug at different times of day was estimated in in vitro experiments. NSC631570 was administered intravenously to healthy volunteers (eleven men, 23 ± 2 years in a single therapeutic dose in an inpatient and an outpatient setting. Blood samples were obtained before the drug administration, 30 min after the drug injection and every fourth hour throughout the 24 hour period. Biochemical parameters were determined using the hematological analyzer. Flow cytometry was used to evaluate phagocyte metabolism. Treatment of circulating phagocytes with NSC631570 in vitro resulted in an increase in ROS production along with a decrease in their phagocytic activity, most expressed in the morning time. Drug injection to sedentary persons resulted in pro-inflammatory metabolic polarization of circulating phagocytes. Introduction of NSC631570 to active persons was accompanied by a significant increase in phagocyte endocytosis along with a decrease in the daily mean of ROS generation. Significant oscillation (but in the normal ranges of urea, creatinine, alanine aminotransferase and aspartate aminotransferase after NSC631570 introduction in the outpatient setting was shown during the day. Physical activity interferes with immunomodulatory action of NSC631570 and abrogates pro-inflammatory shift of circulating phagocytes. Biochemical parameters of blood from patients treated with NSC631570 in the outpatient setting must be interpreted cautiously considering the effect of physical activity on some metabolic biomarkers.

  3. Synthesis of 'no-carrier-added' sup(11)C-labelled nitrosoureas

    Energy Technology Data Exchange (ETDEWEB)

    Diksic, M.; Farrokhzad, S.; Yamamoto, Y.L.; Feindel, W. (Montreal Neurological Inst., Quebec (Canada))

    1985-03-01

    Syntheses for sup(11)C-labelled chemotherapeutic drugs CCNU, BFNU and CFNU (analogs of BCNU) as well as an improved synthesis for sup(11)C-BCNU are described. The procedures for the separation of dual isomers in the case of sup(11)C-labelled CCNU and CFNU are discussed. The specific activity of these 'no-carrier-added' radiopharmaceuticals was approximately 10sup(4) lower than expected for a carrier-free product. The syntheses were normally finished 20-25 min after the end of the collection of sup(11)C-COClsub(2). Chemical and radiochemical purity of the final products as determined by HPLC and TLRC, respectively, was at least 98%. The syntheses yielded 10-25 mCi of nitrosourea ready for use in PET studies.

  4. Methylation pathways in schizophrenia

    International Nuclear Information System (INIS)

    Sargent, T.W. III.

    1982-01-01

    Research on the biochemical causes of human psychosis concentrates on investigating whether schizophremia is linked to abnormalities in the metabolism of methyl carbon groups in the body. The metabolism of C-14 labeled methyl groups in methionine is studied in animals, normal subjects and patient volunteers

  5. WRN-targeted therapy using inhibitors NSC 19630 and NSC 617145 induce apoptosis in HTLV-1-transformed adult T-cell leukemia cells

    Directory of Open Access Journals (Sweden)

    R. Moles

    2016-11-01

    Full Text Available Abstract Background Human T-cell leukemia virus type 1 (HTLV-1 infection is associated with adult T-cell leukemia/lymphoma (ATLL, a lymphoproliferative malignancy with a dismal prognosis and limited therapeutic options. Recent evidence shows that HTLV-1-transformed cells present defects in both DNA replication and DNA repair, suggesting that these cells might be particularly sensitive to treatment with a small helicase inhibitor. Because the “Werner syndrome ATP-dependent helicase” encoded by the WRN gene plays important roles in both cellular proliferation and DNA repair, we hypothesized that inhibition of WRN activity could be used as a new strategy to target ATLL cells. Methods Our analysis demonstrates an apoptotic effect induced by the WRN helicase inhibitor in HTLV-1-transformed cells in vitro and ATL-derived cell lines. Inhibition of cellular proliferation and induction of apoptosis were demonstrated with cell cycle analysis, XTT proliferation assay, clonogenic assay, annexin V staining, and measurement of mitochondrial transmembrane potential. Results Targeted inhibition of the WRN helicase induced cell cycle arrest and apoptosis in HTLV-1-transformed leukemia cells. Treatment with NSC 19630 (WRN inhibitor induces S-phase cell cycle arrest, disruption of the mitochondrial membrane potential, and decreased expression of anti-apoptotic factor Bcl-2. These events were associated with activation of caspase-3-dependent apoptosis in ATL cells. We identified some ATL cells, ATL-55T and LMY1, less sensitive to NSC 19630 but sensitive to another WRN inhibitor, NSC 617145. Conclusions WRN is essential for survival of ATL cells. Our studies suggest that targeting the WRN helicase with small inhibitors is a novel promising strategy to target HTLV-1-transformed ATL cells.

  6. Studies on 14C-extractable residue, 14C-bound residue and mineralization of 14C-labeled chlorsulfuron in soils

    International Nuclear Information System (INIS)

    Ye Qingfu; Sun Jinhe; Qi Wenyuan; Wu Jianmin

    2003-01-01

    The purpose of the present study was to investigate 14 C-extractable residue ( 14 C-ER), 14 C-bound residue ( 14 C-BR) and mineralization of 14 C-labeled chlorsulfuron in soils by using isotope technique. The main factors affecting 14 C-BR formation and the distribution pattern of 14 C-BR in humus were also discussed in details. The results were as follows: (1) The 14 C-ER content of 14 C-chlorsulfuron in seven kinds of soil was positively related to soil pH and negatively related to clay content and organic matter content significantly. Moreover. the decrease rate of 14 C-chlorsulfuron parent compound derived from 14 C-ER in soils followed the first order rate reaction, the half-life in Soil 1-Soil 7 were 13.0, 13.1, 17.7, 133.3, 21.8, 22.1, 33.2 days, respectively. It was concluded that soil pH was the main factor affecting the degradation of 14 C-chlorsulfuron. (2) The 14 C-BR content of 14 C-chlorsulfuron in soils increased sharply with the incubation time during the initial 20 days, then changed slowly with time. However, 14 C-BR content during the whole incubation depended on soil types. The order of 14 C-BR content followed Soil 1 > Soil 2, Soil 5 and Soil 6 > Soil 3 > Soil 7 > Soil 4. The maximum values of 14 C-BR content of 14 C-chlorsulfuron in Soil 1-Soil 7 were 53.3%, 40.9%, 37.8%, 16.4%, 42.5%, 41.0% and 31.3% of applied amount. In addition, the 14 C-BR content of 14 C-chlorsulfuron in soils was negatively related to soil pH significantly, and positively related to the clay content. The soil pH was found to be the main factor affecting BR formation of 14 C-chlorsulfuron among the basic properties of soil. (3) During the whole periods of the incubation, the 14 C-BR of 14 C-chlorsulfuron in soils was mainly distributed in fulvic acid and humin. The relative percent of 14 C-BR in fulvic acid was higher than in humin. While the relative percentage of the 14 C-BR in humic acid only account for 2%. It was suggested that fulvic acid played an important role

  7. Single-gap multi-harmonic buncher for NSC Pelletron

    International Nuclear Information System (INIS)

    Sarkar, A.; Ghosh, S.; Barua, P.

    1998-01-01

    A single gap multi harmonic buncher has been installed in the pre-acceleration region of the NSC pelletron. For the operation of the booster LINAC, presently under construction, a pre-tandem buncher is required with higher efficiency and producing beam bunches of smaller time spread. The multi harmonic buncher meets all these requirements

  8. C-11 production with MC-50 cyclotron and synthesis of L-[11C-methyl] methionine

    International Nuclear Information System (INIS)

    Kim, Sang Wook; Hur, Min Goo; Yang, Seung Dae; Ahn, Soon Hyuk; Chun, Kweon Soo

    2003-01-01

    L-[ 11 C-methyl] methionine was prepared via no-carrier-added(nca) fast S-alkylation of L-homocysteine with [ 11 C]CH 3 I using solid support (Al 2 O 3 /KF)at room temperature in ethanol. The radiochemical yield of methylation was 90.2%. After reaction, no radiochemical impurity was detected but traces of L-homocysteine precursor were monitored by UV detector. The purification was archived by passing successively through a C 18 and alumina sep-pak. the radiochemical purity of L-[ 11 C-methyl] methionine was over 98% after purification and total elapsed time to prepare was 10min from [ 11 C]CH 3 I delivery

  9. Free and proteic aminoacids from acetate 14C metabolism in detached leaves of coffee plant

    International Nuclear Information System (INIS)

    Brasil, O.G.; Crocomo, O.J.

    1981-01-01

    The acetate 14 C was studied as the forerunner of proteic and free aminoacids in detached leaves of coffee (coffea arabica L.cv. Mundo Novo). The detached leaves were incubated with acetate -1- 14 C and -2- 14 C during several times (15, 30, 45, 60, 90, 120, 150 and 180 minutes), out of luminosity. The ethanol 80% soluble fraction gave origin to free aminoacid after ion - exchange chromatography. The insoluble fraction through acid hydrolisis furnished proteic aminoacids. The data showed that the acetate molecules contributed for the aminoacids molecules structure, methylic carbon being more incorporated than the carboxylic carbon. (Author) [pt

  10. Synthesis of substituted bromobenzene derivatives via bromoanilines. A moderately selective ortho-bromination of [14C]-aniline

    International Nuclear Information System (INIS)

    Weller, P.E.; Hanzlik, R.P.

    1988-01-01

    The synthesis of [ 14 C]-labeled bromobenzene, 2-bromophenol, 4-bromophenol, 1,2-dibromobenzene, 2-bromobenzonitrile, 2-bromotoluene, and 2-bromoanisole are reported. [ 14 C]-Aniline is selectively monobrominated to ortho- and para-bromoanilines in 5 to 3 ratio. The separated bromoanilines are diazotized and either reduced, hydrolyzed, coupled to bromide, coupled to cyanide, or coupled to carbon. 2-Bromophenol is O-methylated to 2-bromoanisole. (author)

  11. Bioconversion of α-[14C]Zearalenol and β-[14C]Zearalenol into [14C]Zearalenone by Fusarium roseum Gibbosum

    International Nuclear Information System (INIS)

    Richardson, K.E.; Hagler, W.M. Jr.; Hamilton, P.B.

    1984-01-01

    Cultures of Fusarium roseum Gibbosum on rice were treated with [ 14 C]zearalenone, α-[ 14 C]zearalenol, or β-[ 14 C]zearalenol to determine whether a precursor-product relationship exists among these closely related fungal metabolites. Culture extracts were purified by silica gel column chromatography and fractionated by high-pressure liquid chromatography, and the level of radioactivity was determined. Within 7 days, the β-[ 14 C]zearalenol was converted to zearalenone, and no residual β-[ 14 C]zearalenol was detectable. Most of the α-[ 14 C]zearalenol added was also converted into zearalenone within 14 days. In cultures treated with [ 14 C]zearalenone, no radioactivity was noted in any other components

  12. pKa-critical Interpretations of Solubility–pH Profiles: PG 300995 and NSC-639829 Case Studies

    Directory of Open Access Journals (Sweden)

    George Butcher

    2015-07-01

    Full Text Available Two weak bases, PG-300995 (anti-HIV agent and NSC-639829 (anti-tumor agent, whose log S – pH profiles had been previously published, but whose pKa values had not been reported, were analyzed using a method which can determine pKa values from log S – pH data. This “SpH-pKa” technique, although often practiced, can result in inaccurate pKa values, for a variety of reasons. The operational SpH-pKa values were compared to those predicted by MarvinSketch (ChemAxon, ADMET Predictor (Simulation Plus, and ACD/Percepta (ACD/Labs. The agreement for the sparingly-soluble PG-300995 was reasonably good. However, a substantial difference was found for the practically-insoluble NSC-639829. To probe this further, the pKa of NSC‑639829 was measured by an independent spectrophotometric cosolvent technique. The log S - pH profile of NSC-639829 was then re‑analyzed with the independently-measured pKa. It was found that the equilibrium model which best fit the solubility data is consistent with the presence of a monocationic NSC-639829 dimeric species below pH 4. This illustrates that an independently-determined accurate pKa is critical to mechanistic interpretations of solubility-pH data. Apparently, the Henderson-Hasselbalch equation holds for PG-300995, but not NSC-639829.

  13. Formation of 14C-asparagine from 14C-precursor in mulberry leaves

    International Nuclear Information System (INIS)

    Yamashita, Tadaaki

    1981-01-01

    Since a remarkable accumulation of asparagine in the young leaves of mulberry has been observed, the formation of 14 C-asparagine from 14 C-labeled substrates in young leaves was examined in comparison with that in the mature leaves. 14 C-aspartic acid and 14 C-succinic acid expected as active precursors for asparagine biosynthesis, and 14 C-sucrose as respiratory substrates were fed respectively to the disks of young or mature leaves of mulberry. Although 14 C-succinic acid was actively converted to 14 C-asparagine, no significant amount of 14 C-asparagine was formed from 14 C-aspartic acid in two hours of feeding period. The rate of formation of 14 C-asparagine from 14 C-succinic acid in the mature leaves was slightly higher than that in the young leaves. Amino acids other than asparagine acquired 14 C from 14 C-labeled substrates were mainly aspartic acid, glutamic acid, alanine and ν-amino butyric acid in both of the leaves. Intending to accelerate the formation of asparagine in the leaves, ammonium ion was supplied to culturing solution as only source of nitrogen and plants were grown for two weeks in that solution before 14 C-labeled substrates feeding experiments. Supplying of ammonium ion brought about enhanced accumulation of asparagine in the young leaves, and caused remarkable formation of 14 C-asparagine from 14 C-aspartic acid in both of the leaves. However, the rate of 14 C-asparagine formation from 14 C-aspartic acid in the young leaves did not exceed that in the mature leaves. (author)

  14. Synthesis of deleobuvir, a potent hepatitis C virus polymerase inhibitor, and its major metabolites labeled with carbon-13 and carbon-14.

    Science.gov (United States)

    Latli, Bachir; Hrapchak, Matt; Chevliakov, Maxim; Li, Guisheng; Campbell, Scot; Busacca, Carl A; Senanayake, Chris H

    2015-05-30

    Deleobuvir, (2E)-3-(2-{1-[2-(5-bromopyrimidin-2-yl)-3-cyclopentyl-1-methyl-1H-indole-6-carboxamido]cyclobutyl}-1-methyl-1H-benzimidazol-6-yl)prop-2-enoic acid (1), is a non-nucleoside, potent, and selective inhibitor of hepatitis C virus NS5B polymerase. Herein, we describe the detailed synthesis of this compound labeled with carbon-13 and carbon-14. The synthesis of its three major metabolites, namely, the reduced double bond metabolite (2) and the acyl glucuronide derivatives of (1) and (2), is also reported. Aniline-(13) C6 was the starting material to prepare butyl (E)-3-(3-methylamino-4-nitrophenyl-(13) C6 )acrylate [(13) C6 ]-(11) in six steps. This intermediate was then used to obtain [(13) C6 ]-(1) and [(13) C6 ]-(2) in five and four more steps, respectively. For the radioactive synthesis, potassium cyanide-(14) C was used to prepare 1-cylobutylaminoacid [(14) C]-(23) via Buchrer-Bergs reaction. The carbonyl chloride of this acid was then used to access both [(14) C]-(1) and [(14) C]-(2) in four steps. The acyl glucuronide derivatives [(13) C6 ]-(3), [(13) C6 ]-(4) and [(14) C]-(3) were synthesized in three steps from the acids [(13) C6 ]-(1), [(13) C6 ]-(2) and [(14) C]-(1) using known procedures. Copyright © 2015 John Wiley & Sons, Ltd.

  15. Study of the reaction 14 C (p,p) 14 C

    International Nuclear Information System (INIS)

    Murillo, G.; Ramirez, J.; Avila, O.; Fernandez, M.; Darden, S.E.; Prior, R.P.; Sen, S.

    1991-04-01

    The study of the elastic scattering of polarized protons in 14 C, it has been very limited. Some angular distributions exists to low energy, as well as measures of excitation functions to several angles for the differential section and the vectorial analyzer power. A detailed study of the elastic scattering of protons by 14 C, it give us experimental information of the excited states in 15 N. The study of these states, is since of considerable interest it is not very easy to obtain a target of 14 C also in a reaction 14 C (p,p) 14 C is possible to obtain information of levels in 15 N to an excitation energy E X >14.95 MeV. (Author)

  16. Synthesis of [14α-methyl-3H]-24,25-dihydrolanosterol

    International Nuclear Information System (INIS)

    DeKeczer, S.; Kertesz, D.; Parnes, H.

    1993-01-01

    We describe the first synthesis of isomerically pure title compound (6) at high specific activity. This required the development of a convenient, regiospecific synthesis of the δ 8(9) -15-ketone and subsequent alkylation with methyl-[ 3 H 3 ]iodide. A key step in our procedure was the use of an electrochemical reduction of the intermediate [14α-methyl- 3 H]-15-oxo-dihydrolanosterol. This process was effected cleanly and in high yield to give (6), an important assay tool in the search for cholesterol lowering agents. This approach was found to be significantly superior to the Wolff-Kishner reduction of the corresponding 3-benzoate. (Author)

  17. Dual DNA methylation patterns in the CNS reveal developmentally poised chromatin and monoallelic expression of critical genes.

    Directory of Open Access Journals (Sweden)

    Jinhui Wang

    Full Text Available As a first step towards discovery of genes expressed from only one allele in the CNS, we used a tiling array assay for DNA sequences that are both methylated and unmethylated (the MAUD assay. We analyzed regulatory regions of the entire mouse brain transcriptome, and found that approximately 10% of the genes assayed showed dual DNA methylation patterns. They include a large subset of genes that display marks of both active and silent, i.e., poised, chromatin during development, consistent with a link between differential DNA methylation and lineage-specific differentiation within the CNS. Sixty-five of the MAUD hits and 57 other genes whose function is of relevance to CNS development and/or disorders were tested for allele-specific expression in F(1 hybrid clonal neural stem cell (NSC lines. Eight MAUD hits and one additional gene showed such expression. They include Lgi1, which causes a subtype of inherited epilepsy that displays autosomal dominance with incomplete penetrance; Gfra2, a receptor for glial cell line-derived neurotrophic factor GDNF that has been linked to kindling epilepsy; Unc5a, a netrin-1 receptor important in neurodevelopment; and Cspg4, a membrane chondroitin sulfate proteoglycan associated with malignant melanoma and astrocytoma in human. Three of the genes, Camk2a, Kcnc4, and Unc5a, show preferential expression of the same allele in all clonal NSC lines tested. The other six genes show a stochastic pattern of monoallelic expression in some NSC lines and bi-allelic expression in others. These results support the estimate that 1-2% of genes expressed in the CNS may be subject to allelic exclusion, and demonstrate that the group includes genes implicated in major disorders of the CNS as well as neurodevelopment.

  18. Convenient synthesis of [2-14C]-methylglyoxal bis(guanylhydrazone), [14C]-mitoguazone

    International Nuclear Information System (INIS)

    Burgos, A.; Ellames, G.J.

    1995-01-01

    [2- 14 C]-Methylglyoxal bis(guanylhydrazone) dihydrochloride, [ 14 C]-mitoguazone has been prepared in three steps from potassium[1- 14 C]-acetate in an overall radiochemical yield of 16%. The key steps in this procedure are the formation of the sodium salt of[acetone-2- 14 C]-methylsulfinylacetone, and Pummerer rearrangement to the [ 14 C] labelled hermithioacetal, which is trapped with two equivalents of aminoguanidine to afford the desired [ 14 C]-mitoguazone. (Author)

  19. Identification of a Bis-guanylhydrazone [4,4'-Diacetyldiphenylurea-bis(guanylhydrazone); NSC 109555] as a novel chemotype for inhibition of Chk2 kinase.

    Science.gov (United States)

    Jobson, Andrew G; Cardellina, John H; Scudiero, Dominic; Kondapaka, Sudhir; Zhang, Hongliang; Kim, Hijoo; Shoemaker, Robert; Pommier, Yves

    2007-10-01

    Chk2 is a protein kinase involved in the ATM-dependent checkpoint pathway (http://discover.nci.nih.gov/mim). This pathway is activated by genomic instability and DNA damage and results in either cell cycle arrest, to allow DNA repair to occur, or cell death (apoptosis). Chk2 is activated by ATM-mediated phosphorylation and autophosphorylation and in turn phosphorylates its downstream targets (Cdc25A, Cdc25C, BRCA1, p53, Hdmx, E2F1, PP2A, and PML). Inhibition of Chk2 has been proposed to sensitize p53-deficient cells as well as protect normal tissue after exposure to DNA-damaging agents. We have developed a drug-screening program for specific Chk2 inhibitors using a fluorescence polarization assay, immobilized metal ion affinity-based fluorescence polarization (IMAP). This assay detects the degree of phosphorylation of a fluorescently linked substrate by Chk2. From a screen of over 100,000 compounds from the NCI Developmental Therapeutics Program, we identified a bis-guanylhydrazone [4,4'-diacetyldiphenylureabis(guanylhydrazone); NSC 109555] as a lead compound. In vitro data show the specific inhibition of Chk2 kinase activity by NSC 109555 using in vitro kinase assays and kinase-profiling experiments. NSC 109555 was shown to be a competitive inhibitor of Chk2 with respect to ATP, which was supported by docking of NSC 109555 into the ATP binding pocket of the Chk2 catalytic domain. The potency of NSC 109555 was comparable with that of other known Chk2 inhibitors, such as debromohymenialdisine and 2-arylbenzimidazole. These data define a novel chemotype for the development of potent and selective inhibitors of Chk2. This class of drugs may ultimately be useful in combination with current DNA-damaging agents used in the clinic.

  20. Difference in effect of single immunosuppressive agents (cyclophosphamide, CCNU, 5-FU) on peripheral blood immune cell parameters and central nervous system immunoglobulin synthesis rate in patients with multiple sclerosis.

    Science.gov (United States)

    Shih, W W; Baumhefner, R W; Tourtellotte, W W; Haskell, C M; Korn, E L; Fahey, J L

    1983-01-01

    Cyclophosphamide (CY), 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea (CCNU) and 5-fluorouracil (5-FU) were given in single course schedules to chronic progressive multiple sclerosis (MS) patients clinically stable for 6 months. The following peripheral immune cellular parameters were measured before, during and after each drug administration: white blood count (WBC), polymorphonuclear count (PMN), lymphocyte count, percentage of T cells, T cell response to phytohaemagglutinin (PHA), percentage of B cells, percentage of cells bearing receptors for the Fc portion of immunoglobulin (% FcR cells), killer (K) cell activity defined by antibody-dependent cellular cytotoxicity (ADCC), and natural killer (NK) cell activity. Central nervous system (CNS) immunoglobulin G (IgG) synthesis was also measured. The patients were followed carefully by both quantitative and qualitative methods for any change in their neurologic condition. Selective reduction in NK activity was observed with CY and 5-FU while no significant alteration was seen in %FcR cells and K activity. CY differed from 5-FU in reducing lymphocyte count and B cell percentage while 5-FU decreased the percentage of T cells. CCNU, but not the other drugs, reduced T cell proliferative response to PHA. In addition, CCNU, which is known to penetrate well into the nervous system, caused a modest reduction in CNS IgG synthesis, while 5-FU had an uncertain effect. Clinically the patients were unchanged or continued to progress in their disability. The results suggest an independence of the CNS immune from the systemic immune system in MS in response to many immunosuppressive drugs. PMID:6603303

  1. Evaluation of radiation dose resulting from the ingestion of [3H]-and [14C]thymidine in the rat

    International Nuclear Information System (INIS)

    Takeda, H.; Iwakura, T.

    1987-01-01

    Average doses to rat tissues from the ingestion of 2-[ 14 C]thymidine were compared with those from methyl-[ 3 H]thymidine or 6-[ 3 H]thymidine. [ 14 C]thymidine gave the highest dose to spleen and small intestine. Doses to other tissues from [ 14 ]thymidine were almost the same or lower compared with those from [ 3 H]thymidine, irrespective of the 9 times higher β-ray energy of 14 C than that of 3 H. In the case of [ 14 C]thymidine, most of the dose was given by radioactivity incorporated into the organic tissue constituents (non-volatile radioactivity). In the case of [ 3 H]thymidine, the dose contributions by non-volatile radioactivity were very small and major contributions were rather from volatile radioactivity ( 3 HHO), formed by degradation of [ 3 H]thymidine. No significant difference in their total doses was found between the two [ 3 H]precursors, but the dose from non-volatile radioactivity alone was 2-3 times higher with methyl-[ 3 H]thymidine than with 6-[ 3 H]thymidine. Estimates of dose to cell nuclei in various tissues after ingestion of [ 3 H]thymidine were also made in order to predict more precisely possible radiation hazards. (author)

  2. Oxidation of 2-methyl-1-naphthol to 2-methyl-1,4-naphthoquinone using interphase catalysis in the presence of vanadomolybdophosphoric heteropolyacids

    International Nuclear Information System (INIS)

    Matveev, K.I.; Zhizhina, E.G.; Odyakov, V.F.; Parmon, V.N.

    1994-01-01

    2-Methyl-1-naphthol is oxidized by air to 2-methyl-1,4-naphthoquinone (menadione) in the presence of vanadomolybdophosphoric heteropolyacids or their acid salts. This reaction proceeds in a two-phase system with the yield of up to 85 %. The influence of heteropolyacid composition on the reaction rate and its selectivity has been studied and the reaction mechanism has been proposed. 7 refs.; 1 fig.; 1 tab

  3. Metabolic fate of the beta-blocker 14C-bupranolol in humans, dogs, and rhesus monkeys

    International Nuclear Information System (INIS)

    Waller, A.R.; Chasseaud, L.F.; Bonn, R.; Taylor, T.; Darragh, A.; Girkin, R.; Down, W.H.; Doyle, E.

    1982-01-01

    An oral dose of 14 C-bupranolol hydrochloride was well absorbed by humans (100 mg), dogs (1 mg/kg), and rhesus monkeys (1 mg/kg). These species excreted 87.8 and 3.5%, 81.1 and 13.6%, and 92.9 ad 5.0% of the 14 C-dose in urine and feces, respectively, mainly in 12 or 24 hr. Mean plasma levels of 14 C, which appeared to be almost entirely associated with a single metabolite, peaked at 1 hr in humans (1.6 micrograms-equiv./ml) and dogs (1.6 micrograms-/ml) and at 2 hr in monkeys (0.8 micrograms-equiv./ml). Concentrations initially declined with similar half-lives (about 1.5 hr) in all three species. Biliary excretion of 14 C occurred in the animal species in which also peak plasma 14 C levels exceeded those in most tissues. Unchanged bupranolol was not detected in plasma; the peak plasma and urinary 14 C was mainly associated (greater than 90% in humans) with a metabolite produced by oxidation of the aromatic ring methyl group of bupranolol to a carboxyl group

  4. Use of [2-14C]mevalonate and saponin-bound [14C]-3-hydroxy-3-methylglutaric acid for the biosynthesis of terpenoids in leaves of Dioscorea deltoidea

    International Nuclear Information System (INIS)

    Gurielidze, K.G.; Paseshnichenko, V.A.; Vasil'eva, I.S.

    1986-01-01

    After the introduction of [2- 14 C]acetate into leaves of Dioscorea deltoidea, a radioactive furonanalog of deltafolin - protodeltofolin, containing two-thirds of the label in the 3-hydroxy-3-methylglutaryl portion - was isolated from them. Radioactive β-careotene and sterols were isolated from cut young leaves of Dioscorea 24 h after the introduction of [ 14 C] protodeltofolin into them, using chromatography on a column of silica gel and precipitation of sterols in the form of digitonins for this purpose. The incorporation of radioactivity from [ 14 C]-3-hydroxy-3-methyl-glutaric acid, bound in the form of a saponin, and β-carotene came to 0.18-0.80%, while incorporation into sterols came to 0.07-2.86% of the radioactivity of the alcohol extract. Thereby it was shown that 3-hydroxyl-3-methylglutaric acid, bound in the form of the saponin, can be used to form terpenoids in Dioscorea leaves. It was suggested that the binding of hydroxymethylglutaric acid to saponin represents one of the mechanisms of regulation of the rate of terpenoid biosynthesis in Dioscorea leaves

  5. Semi-automated preparation of a 11C-labelled antibiotic - [N-methyl-11C]erythromycin A lactobionate

    International Nuclear Information System (INIS)

    Pike, V.W.; Palmer, A.J.; Horlock, P.L.; Liss, R.H.

    1984-01-01

    A fast semi-automated method is described for labelling the antibiotic, erythromycin A (1), with the short-lived positron-emitting radionuclide, 11 C(tsub(1/2)=20.4 min), in order to permit the non-invasive study of its tissue uptake in vivo. Labelling was achieved by the fast reductive methylation of N-demethylerythromycin A (2) with [ 11 C]formaldehyde, itself prepared from cyclotron-produced [ 11 C]-carbon dioxide. Rapid chemical and radiochemical purification of the [N-methyl- 11 C]erythromycin A (3) were achieved by HPLC and verified by TLC with autoradiography. The purified material was formulated for human i.v. injection as a sterile apyrogenic solution of the lactobionate salt. The preparation takes 42 min from the end of radionuclide production and from [ 11 C]carbon dioxide produces [N-methyl- 11 C]erythromycin A lactobionate in 4-12% radiochemical yield, corrected for radioactive decay. (author)

  6. Donor age and C1orf132/MIR29B2C determine age-related methylation signature of blood after allogeneic hematopoietic stem cell transplantation.

    Science.gov (United States)

    Spólnicka, Magdalena; Piekarska, Renata Zbieć; Jaskuła, Emilia; Basak, Grzegorz W; Jacewicz, Renata; Pięta, Agnieszka; Makowska, Żanetta; Jedrzejczyk, Maciej; Wierzbowska, Agnieszka; Pluta, Agnieszka; Robak, Tadeusz; Berent, Jarosław; Branicki, Wojciech; Jędrzejczak, Wiesław; Lange, Andrzej; Płoski, Rafał

    2016-01-01

    Our recent study demonstrated that DNA methylation status in a set of CpGs located in ELOVL2, C1orf132, TRIM59, KLF14, and FHL2 can accurately predict calendar age in blood. In the present work, we used these markers to evaluate the effect of allogeneic hematopoietic stem cell transplantation (HSCT) on the age-related methylation signature of human blood. DNA methylation in 32 CpGs was investigated in 16 donor-recipient pairs using pyrosequencing. DNA was isolated from the whole blood collected from recipients 27-360 days (mean 126) after HSCT and from the donors shortly before the HSCT. It was found that in the recipients, the predicted age did not correlate with their calendar age but was correlated with the calendar age (r = 0.94, p = 4 × 10(-8)) and predicted age (r = 0.97, p = 5 × 10(-10)) of a respective donor. Despite this strong correlation, the predicted age of a recipient was consistently lower than the predicted age of a donor by 3.7 years (p = 7.8 × 10(-4)). This shift was caused by hypermethylation of the C1orf132 CpGs, for C1orf132 CpG_1. Intriguingly, the recipient-donor methylation difference correlated with calendar age of the donor (r = 0.76, p = 6 × 10(-4)). This finding could not trivially be explained by shifts of the major cellular factions of blood. We confirm the single previous report that after HSCT, the age of the donor is the major determinant of age-specific methylation signature in recipient's blood. A novel finding is the unique methylation dynamics of C1orf132 which encodes MIR29B2C implicated in the self-renewing of hematopoietic stem cells. This observation suggests that C1orf132 could influence graft function after HSCT.

  7. NSC30049 inhibits Chk1 pathway in 5-FU-resistant CRC bulk and stem cell populations.

    Science.gov (United States)

    Narayan, Satya; Jaiswal, Aruna S; Sharma, Ritika; Nawab, Akbar; Duckworth, Lizette Vila; Law, Brian K; Zajac-Kaye, Maria; George, Thomas J; Sharma, Jay; Sharma, Arun K; Hromas, Robert A

    2017-08-22

    The 5-fluorouracil (5-FU) treatment induces DNA damage and stalling of DNA replication forks. These stalled replication forks then collapse to form one sided double-strand breaks, leading to apoptosis. However, colorectal cancer (CRC) stem cells rapidly repair the stalled/collapsed replication forks and overcome treatment effects. Recent evidence suggests a critical role of checkpoint kinase 1 (Chk1) in preventing the replicative stress. Therefore, Chk1 kinase has been a target for developing mono or combination therapeutic agents. In the present study, we have identified a novel orphan molecule NSC30049 (NSC49L) that is effective alone, and in combination potentiates 5-FU-mediated growth inhibition of CRC heterogeneous bulk and FOLFOX-resistant cell lines in culture with minimal effect on normal colonic epithelial cells. It also inhibits the sphere forming activity of CRC stem cells, and decreases the expression levels of mRNAs of CRC stem cell marker genes. Results showed that NSC49L induces 5-FU-mediated S-phase cell cycle arrest due to increased load of DNA damage and increased γ-H2AX staining as a mechanism of cytotoxicity. The pharmacokinetic analysis showed a higher bioavailability of this compound, however, with a short plasma half-life. The drug is highly tolerated by animals with no pathological aberrations. Furthermore, NSC49L showed very potent activity in a HDTX model of CRC stem cell tumors either alone or in combination with 5-FU. Thus, NSC49L as a single agent or combined with 5-FU can be developed as a therapeutic agent by targeting the Chk1 pathway in 5-FU-resistant CRC heterogeneous bulk and CRC stem cell populations.

  8. Microbiology and biogeochemistry of sediments and rhizosphere of mangroves: bacterial production, sulphate-reduction and methylation of mercury with methodological focus on incubation-extraction of 14C-leucine

    International Nuclear Information System (INIS)

    Feijo, Issabella Vitoria Abduche

    2015-01-01

    Mangroves are one of the most important ecosystems when it comes to cycling of various elements, including carbon and mercury. Microbiological processes that occur in sediment are essential for carbon mineralization, its conversion into biomass and for availability of mercury to the food chain. Sulfate-reducing bacteria are one of the main groups responsible for degradation of organic compounds in marine sediments and mercury methylation, especially in the rhizosphere of macrophyte. The aim of this study was to evaluate bacterial production (BP) over different sedimentary profiles as well as mercury methylation (% MeHg), sulfate reduction rates (SRR) and bacterial production in the rhizosphere of a ubiquitous mangrove tree. Radiochemical approaches were used to access bacterial production ( 14 C-leucine), sulfate reduction ( 35 SO 4 ) and mercury methylation ( 203 Hg). Study area was located at Coroa Grande (Sepetiba bay) and Jequia mangrove (Guanabara bay). Methodological studies using 14 C-leucine as a tool to assess bacterial production in mangrove sediment were not found. In this context, we tested two leucine uptake methodologies for measuring bacterial production in mangrove sediments according to Baath et al. (2001) Soil Biol. Biochem., v.33,p. 1571-1574 and Fischer and Pusch (1999) Appl. Environ. Microbiol., v.6, p.4411-4418. Our results suggest that an adaptation of both techniques were suitable to measure BP in mangrove sediment. We also provided underlying parameters of the method such as saturation level and linearity of leucine incorporation that can be used as guidance for future studies in mangrove. Once the methodology was established, we accessed BP along a shallow sedimentary profile in three physiographic mangroves types: basin, fringe and riverine. BP was highly heterogeneous in different physiographic types of mangroves and along the sediment profiles.The mangrove located at Guanabara bay presented BP which was 50 times higher than tho one

  9. Alterations to DNA methylation and expression of CXCL14 are associated with suboptimal birth outcomes.

    Science.gov (United States)

    Cheong, Clara Y; Chng, Keefe; Lim, Mei Kee; Amrithraj, Ajith I; Joseph, Roy; Sukarieh, Rami; Chee Tan, Yong; Chan, Louiza; Tan, Jun Hao; Chen, Li; Pan, Hong; Holbrook, Joanna D; Meaney, Michael J; Seng Chong, Yap; Gluckman, Peter D; Stünkel, Walter

    2014-09-01

    CXCL14 is a chemokine that has previously been implicated in insulin resistance in mice. In humans, the role of CXCL14 in metabolic processes is not well established, and we sought to determine whether CXCL14 is a risk susceptibility gene important in fetal programming of metabolic disease. For this purpose, we investigated whether CXCL14 is differentially regulated in human umbilical cords of infants with varying birth weights. We found an elevated expression of CXCL14 in human low birth weight (LBW) cords, as well as in cords from nutritionally restricted Macaca fascicularis macaques. To further analyze the regulatory mechanisms underlying the expression of CXCL14, we examined CXCL14 in umbilical cord-derived mesenchymal stem cells (MSCs) that provide an in vitro cell-based system amenable to experimental manipulation. Using both whole frozen cords and MSCs, we determined that site-specific CpG methylation in the CXCL14 promoter is associated with altered expression, and that changes in methylation are evident in LBW infant-derived umbilical cords that may indicate future metabolic compromise through CXCL14.

  10. Effect of aldicarb on growth and radio-carbon (14C) and radio-phosphorus (32P) assimilation by Rhizobium japonicum

    International Nuclear Information System (INIS)

    Balasubramanian, A.; Nilakantan, Gita

    1976-01-01

    In vitro studies on the effect of aldicarb (2-methyl-2-(methyl thio) propionaldehde-o-methyl carbamoyl oxime), a soil applied systemic insecticide, on Rhizobium japonicum revealed that the chemical (at 1,2 and 5 ppm levels) stimulated the growth of the organism initially upto 48 hr which declined thereafter upto 72 hr. The incorporation of 14 C-glucose by the cells considerably reduced due to the insecticide treatment. The production of extracellular, water-soluble slime (polysacchardes) was also reduced considerably with increased concentrations of the chemical. However, the incorporation of 14 C-radio-activity in the extracellular slime generally enhanced due to the treatment, upto 6 hr after injection of the radioactivity, which declined significantly later at 15 hr, indicating a qualitative difference in the extracellular polysaccharides produced by the insecticide treated cells. The insecticide treatment drastically reduced the incorporation of 32 P-disodium hydrogen phosphate into Rhizobium cells, but enhanced the specific activity of the extracellular polysacchrides. (author)

  11. Ferrocene Compounds. XXVI. C- and O-Ferrocenylalkylation of Methyl Salicylate

    OpenAIRE

    Kovač, Veronika; Rapić, Vladimir; Alagić, Jasmina; Barišić, Lidija

    1999-01-01

    Reaction of equimolar amounts of methyl salicylate, sodium and N,N,N-trimethylferrocylammonium iodide (1a) in ethanol gave 55% of ethyl 1-ferrocenylethyl ether (4). By refluxing a solution of 9 mmol sodium and 3 mmol of FcCHRNMe3I (1a, R = H; 1b, R = Me; 1c, R = Ph) in a large excess of methyl salicylate for 2-3 hours, the corresponding methyl 5-ferrocylsalicylates (5) (10-23%) and methyl-3-ferrocylsalicylates (6) (12-20%) were obtained. During conversion of salt 1b, besides of 5b and 6b, 20%...

  12. A novel compound NSC745885 exerts an anti-tumor effect on tongue cancer SAS cells in vitro and in vivo.

    Directory of Open Access Journals (Sweden)

    Yuan-Wu Chen

    Full Text Available Oral squamous cell carcinoma (OSCC is a prevalent cancer, especially in developing countries. Anthracyclines and their anthraquinone derivatives, such as doxorubicin, exhibit a cell growth inhibitory effect and have been used as anti-cancer drugs for many years. However, the cardiotoxicity of anthracycline antibiotics is a major concern in their clinical application. NSC745885 is a novel compound synthesized from 1,2-diaminoanthraquinone, which subsequently reacts with thionyl chloride and triethylamine. The present study aimed to investigate the anti-oral cancer potential and the safety of NSC745885.We investigated the anti-cancer potential of NSC745885 in oral squamous carcinoma cell lines and in an in vivo oral cancer xenograft mouse model. The expression of apoptotic related genes were evaluated by real-time RT-PCR and western bloting, and the in vivo assessment of apoptotic marker were measured by immunohistochemical staining. The anti-tumor efficiency and safety between doxorubicin and NSC745885 were also compared.Our results demonstrated that NSC745885 exhibits anti-oral cancer activity through the induction of apoptosis in cancer cells and in tumor-bearing mice, and this treatment did not induce marked toxicity in experimental mice. This compound also exhibits a comparable anti-tumor efficiency and a higher safety in experimental mice when compared to doxorubicin.The data of this study provide evidence for NSC745885 as a potential novel therapeutic drug for the treatment of human OSCC.

  13. NSC23766, a Known Inhibitor of Tiam1-Rac1 Signaling Module, Prevents the Onset of Type 1 Diabetes in the NOD Mouse Model

    Directory of Open Access Journals (Sweden)

    Rajakrishnan Veluthakal

    2016-07-01

    Full Text Available Background/Aims: Type 1 diabetes (T1D is characterized by absolute insulin deficiency due to destruction of pancreatic β-cells by cytokines (e.g., interleukin-1β; IL-1β released by invading immune cells. The mechanisms by which these cytokines induce β-cell dysfunction remain poorly understood. Recent evidence suggests that excessive generation of reactive oxygen species (ROS by the phagocyte-like NADPH oxidase2 (Nox2, along with significantly low levels of antioxidants in β-cells, drive them toward oxidative damage. Rac1, a small G-protein, is one of the members of Nox2 holoenzyme. We recently reported that NSC23766, a known inhibitor of Rac1, significantly attenuated cytokine-induced Nox2 activation and ROS generation in pancreatic islet β-cells in vitro. Herein, we determined the effects of NSC23766 (2.5 mg/kg/day, i.p/daily on the development of diabetes in the NOD mouse, a model for T1D. Methods: Two groups of experimental animals (Balb/c and NOD mice received NSC23766, while the two control groups received equal volume of saline. Body weights and blood glucose were measured every week for 34 weeks. Rac1 activation in pancreatic islets was measured by GLISA activation assay. Rac1 and CHOP expression was determined by Western Blotting. Results: Our findings indicate that administration of NSC23766 significantly prevented the development of spontaneous diabetes in the NOD mice. Furthermore, NSC23766 markedly suppressed Rac1 expression and activity and the endoplasmic reticulum stress (CHOP expression in NOD islets. Conclusions: Our findings provide the first evidence implicating the role of Tiam1-Rac1-Nox2 signaling pathway in the onset of spontaneous diabetes in the NOD mouse model.

  14. Human metabolism of [1-methyl-14C]- and [2-14C]caffeine after oral administration

    International Nuclear Information System (INIS)

    Callahan, M.M.; Robertson, R.S.; Arnaud, M.J.; Branfman, A.R.; McComish, M.F.; Yesair, D.W.

    1982-01-01

    Radiolabeled caffeine was administered orally at 5 mg/kg to adult, male volunteers. Blood, saliva, expired CO2, urine, and feces were collected and analyzed for total radiolabeled equivalents, caffeine, and its metabolites. High-performance liquid chromatography (HPLC) was the principal technique used to separate caffeine and the various metabolites with quantitation by liquid-scintillation counting. The half-life of caffeine in both serum and saliva was approximately 3 hr, with the concentration of caffeine in the saliva samples ranging from 65 to 85% of that found in the serum samples. The major metabolites found in serum and saliva were the dimethylxanthines. In the course of separating the urinary metabolites, our HPLC system partially resolved two unidentified polar metabolites arising from radiolabeled caffeine. The major component corresponded to 5-acetylamino-6-amino-3-methyluracil and in our subjects ranged from 7 to 35% of the administered dose. The other principal urinary metabolites were 1-methylxanthine at approximately 18% of the administered dose and 1-methyluric acid at 15%. The fecal samples contained approximately 5% of the dose, mainly as uric acid compounds which retained the 1-methyl group. In this study we accounted for approximately 90% of the administered radiolabeled dose and identified greater than 95% of the urinary radioactivity as specific metabolites

  15. Synthesis of the mevalonic acid labelled with "1"4C, "1"3C and "3H

    International Nuclear Information System (INIS)

    Rousseau, Bernard

    1982-01-01

    This thesis describes five new methods of synthesis of the (R,S) mevalonic acid adapted to the labelling with "1"4C and "1"3C in positions 4,5 or 5 or 3', or with tritium in position 3'. Three of them use the tri-oxa-2,4,10 adamantyl group as masked carboxyl function. The two others take benefit from the regioselectivity of the bis-hydro-boration of terminal acetylenics by the 9-borabicyclo [3-3-1]nonane. The acylation of the bis-trimethylsilyl lithiomalonate, and the chemistry of dithiannes are also involved. Acetylene and methyl iodide labelled with isotopes are used as cheap base products [fr

  16. A convenient synthesis of sup 14 C-cotinine from sup 14 C-nicotine

    Energy Technology Data Exchange (ETDEWEB)

    Desai, D.H.; Djordjevic, M.V.; Amin, S. (American Health Foundation, Valhalla, NY (USA). Naylor Dana Inst. for Disease Prevention)

    1991-03-01

    A convenient synthesis with analytical monitoring of {sup 14}C-cotinine is reported. {sup 14}C-Nicotine was converted into {sup 14}C-dibromocotinine hydrobromide perbromide. Debromination, achieved by using Zn dust/acetic acid, resulted in high yields (71%) of {sup 14}C-cotinine. (author).

  17. Synthesis of some 11C-labelled alkaloids

    International Nuclear Information System (INIS)

    Laangstroem, B.; Antoni, G.; Halldin, H.; Svaerd, H.; Bergson, G.

    1982-01-01

    Using ( 11 C)-methyl iodide in N-alkylation reactions in dimethylformamide (DMF), the alkaloids N-( 11 C-methyl)-morphine, N-( 11 C-methyl)-codeine, 6-N(methyl)-9, 10-dihydroergotamine, 6-N-( 11 C-methyl)-bromocriptine and N-( 11 C-methyl)-nicotine have been synthesized in radiochemical yields of 50-95%, within 5-10 min of introducing ( 11 C)-methyl iodide into the reaction vial. ( 11 C)-Methyl iodide was obtained within 4-7 min from ( 11 C)-carbon dioxide prepared by the 14 N(p,α) 11 C reaction. (Authors)

  18. Synthesis of methyl ((chloro-2 ethyl)-3 nitroso-3 Ureido)-3 Didesoxy-2,3. alpha. -D-Arabino-hexopyrannoside labelled with carbon-14 or carbon-13 (CY 233 - SR 90008). Synthese du methyl ((chloro-2 ethyl)-3 nitroso-3 Ureido)-3 Didesoxy-2,3. alpha. -D-Arabino-hexopyrannoside marque au carbone-14 ou carbone-13 (CY 233 - SR 90008)

    Energy Technology Data Exchange (ETDEWEB)

    Sion, R.; Schumer, A.; Durme, E. van (Sanofi Recherche, Brussels (Belgium)); Gouyette, A. (Centre de Lutte Contre le Cancer Gustave-Roussy, 94 - Villejuif (France)); Geslin, M.; Fournier, J.P.; Roger, P. (Sanofi Recherche, Montrouge (France). Inst. Choay); Berger, Y. (Sanofi Recherche, Montpellier (France))

    1990-06-01

    CY 233 (Ecomustine or SR 90098) is a new antitumour nitrosourea: it is characterized by a 2-chloroethylnitrosourea substituent on a dideoxycarbohydrate. It has been labelled with {sup 14}C on (a) the carbonyl group of the urea in four stages starting with {sup 14}COCl{sub 2}, (b) the second carbon of the chloroethyl group in four stages starting with ({sup 14}C) ethanolamine, and (c) on the methyl group on the anomeric centre of the carbohydrate in three stages starting with {sup 14}CH{sub 3}OH. The final position was also labelled with {sup 13}C starting with {sup 13}CH{sub 3}OH. These differently labelled compounds are suitable for mechanistic studies of antitumour activity. (author).

  19. Simple automated system for simultaneous production of 11C-labeled tracers by solid supported methylation

    International Nuclear Information System (INIS)

    Quincoces, Gemma; Penuelas, Ivan; Valero, Marta; Serra, Patricia; Collantes, Maria; Marti-Climent, Josep; Arbizu, Javier; Jose Garcia-Velloso, Maria; Angel Richter, Jose

    2006-01-01

    We herein describe a simple setup for the automated simultaneous synthesis of L-[methyl- 11 C]methionine and N-[methyl- 11 C]choline by solid-supported methylation . The setup is extremely simple and easy to adapt to other automated systems and due to its versatility, the method can be utilized for the production of other radiopharmaceuticals requiring a simple [ 11 C]methylation step. Furthermore, it can be used for multiple simultaneous synthesis

  20. Synthesis of no-carrier-added alpha-[11C]methyl-L-tryptophan

    International Nuclear Information System (INIS)

    Chaly, T.; Diksic, M.

    1988-01-01

    Described here is a synthesis of no-carrier-added alpha-[ 11 C]methyl-L-tryptophan based on alkylation with 11 CH 3 I of an anion generated by reacting the Schiff base of L-tryptophan methyl ester with di-isopropylamine. The synthesis requires approximately 30 min after the end of 11 CO 2 collection and gives alpha-[ 11 C]methyl-L-tryptophan in a 20-25% radiochemical yield calculated at the end of the synthesis and without correction for radioactive decay. The specific activity of the final radiopharmaceutical, measured at the end of the synthesis, was around 2000 Ci/mmol. Data confirming the stereospecificity of the synthesis are also presented

  1. Convenient synthesis of [2-{sup 14}C]-methylglyoxal bis(guanylhydrazone), [{sup 14}C]-mitoguazone

    Energy Technology Data Exchange (ETDEWEB)

    Burgos, A.; Ellames, G.J. [Sterling Winthrop Research Centre, Alnwick (United Kingdom). Pharmaceuticals Research Div.

    1995-01-01

    [2-{sup 14}C]-Methylglyoxal bis(guanylhydrazone) dihydrochloride, [{sup 14}C]-mitoguazone has been prepared in three steps from potassium[1-{sup 14}C]-acetate in an overall radiochemical yield of 16%. The key steps in this procedure are the formation of the sodium salt of[acetone-2-{sup 14}C]-methylsulfinylacetone, and Pummerer rearrangement to the [{sup 14}C] labelled hermithioacetal, which is trapped with two equivalents of aminoguanidine to afford the desired [{sup 14}C]-mitoguazone. (Author).

  2. Methyl bromide residues in fumigated cocoa beans with particular reference to inorganic bromide

    International Nuclear Information System (INIS)

    Adomako, D.

    1976-01-01

    Inorganic bromide residues and 14 C-labelled methylated products (expressed as CH 3 Br equivalent) in cocoa beans fumigated with [ 14 C]-methyl bromide have been determined by radiometric and chemical methods. Determination of 14 C by direct combustion in an oxygen chamber followed by liquid scintillation counting confirmed previous findings with respect to the magnitude, distribution and chemical nature of the residues. Although recovery of added bromide was good, the values of total bromide obtained by the chemical method were only half of those estimated from the total residual 14 C-activity. This is attributed to loss of organic (presumably, protein-bound) bromide. In agreement with the total 14 C-labelled residue contents, total bromide in shells was 20 times greater than that in nibs. The low levels of residues in the nib (12ppm as CH 3 Br equivalent, 10ppm Br) and the further reduction of organic residues by roasting suggest that no toxicological and nutritional hazards may be expected from fumigation of cocoa beans with methyl bromide. (author)

  3. Synthesis of 14C- and 3H-labeled fluoxetine, a selective serotonin uptake inhibitor

    International Nuclear Information System (INIS)

    Robertson, D.W.; Krushinski, J.H.; Wong, D.T.; Kau, D.

    1987-01-01

    Fluoxetine (N-methyl-γ-(4-(trifluoromethyl)phenoxy) benzenepropanamine) is a potent, highly selective serotonin uptake inhibitor that is useful in treating a variety of major psychiatric derangements. We have synthesized this compound in 14 C- and 3 H-labeled forms. The tritium label was introduced in the final step by catalytic dehalogenation of the brominated fluoxetine precursor. Reaction conditions could be controlled such that catalytic hydrogenolysis of the labile C-O benzylic bond was minimized. Following HPLC purification, [ 3 H]-fluoxetine was obtained in a state of high radiochemical purity (98%) and specific activity (20.4 Ci/mmol). The 14 C-label was introduced in the final step via a nucleophilic aromatic substitution reaction between the sodium salt of α-(2-(methylamino)ethyl)benzenemethanol and uniformly ring-labeled p-chlorobenzotrifluoride. Following purification by flash chromatography, [ 14 C]-fluoxetine was obtained in 98.3% radiochemical purity with a specific activity of 5.52 mCi/mmol. (author)

  4. 11C-labelling of the analgesic Tramadol and its major metabolites by selective O- and N-methylation

    International Nuclear Information System (INIS)

    Gail, R.; Coenen, H.H.; Hamacher, K.; Stoecklin, G.

    1992-01-01

    For in vivo pharmacokinetic studies with PET, the analgesic Tramadol(1-(3-methoxyphenyl)-2-dimethylaminomethyl-cyclohexan-1-ol) and its major O- and N-desmethylated metabolites M1 and M2 were labelled with carbon-11. Starting with the corresponding desmethyl precursors, [O-methyl- 11 C]Tramadol and racemic[N-methyl- 11 C]Tramadol were prepared by methylation with n.c.a. [ 11 C]methyl iodide in DMSO with radiochemical yields of 85 and 90%, respectively. Specific n.c.a. N-methylation of bis-desmethyl-Tramadol (M5) was achieved with 90% radiochemical yield. However, a selective O-methylation of M5 was not possible even with an excess of NaOH, and only 70% of [O-methyl- 11 C]M2 was obtained. Quaternization of Tramadol or M1 was >15 times slower than O-methylation, and was only observed in the presence of added CH 3 I carrier. (author)

  5. Methods for measuring specific rates of mercury methylation and degradation and their use in determining factors controlling net rates of mercury methylation

    International Nuclear Information System (INIS)

    Ramlal, P.S.; Rudd, J.W.M.; Hecky, R.E.

    1986-01-01

    A method was developed to estimate specific rates of demethylation of methyl mercury in aquatic samples by measuring the volatile 14 C end products of 14 CH 3 HgI demethylation. This method was used in conjuction with a 203 Hg 2+ radiochemical method which determines specific rates of mercury methylation. Together, these methods enabled us to examine some factors controlling the net rate of mercury methylation. The methodologies were field tested, using lake sediment samples from a recently flooded reservoir in the Southern Indian Lake system which had developed a mercury contamination problem in fish. Ratios of the specific rates of methylation/demethylation were calculated. The highest ratios of methylation/demethylation were calculated. The highest ratios of methylation/demethylation occurred in the flooded shorelines of Southern Indian Lake. These results provide an explanation for the observed increases in the methyl mercury concentrations in fish after flooding

  6. Preparation of 14c- amd 180-labeled 2-[2-methoxy-4-(methylsulfinyl)phenyl]-1H-imidazo[4,5-c]-pyridine hydrochloride (LY175326), a cardiotonic with inotropic and vasodilator activities

    International Nuclear Information System (INIS)

    Kau, Don; Krushinski, J.H.; Robertson, D.W.

    1985-01-01

    Two different forms of 14 C-labeled 2-methoxy-4-(methyl-thio)benzoic acid were prepared and employed in the synthesis of 14 C-labeled 2-:2-methoxy-4-(methylsulfinyl)phenyl:-1H-imidazo-[4,5-c]pyridine hydrochloride (LY175326), a cardiotonic with inotropic and vasodilator activities that is currently in clinical trials. The synthetic procedures described in this report allowed the introduction of the 14 C-label in the antepenultimate step. Additionally, an 18 0-labeled form of LY175326 was synthesized to facilitate kinetic analysis of the formation of its sulfide and sulfone metabolites. (author)

  7. One column method to prepare 11C-labelled methyl iodide

    International Nuclear Information System (INIS)

    Kovacs, Z.; Priboczki, E.

    1999-01-01

    A new method in which the [ 11 C]methyl iodide is prepared on one alumina column is presented. A high specific surface alumina column, previously impregnated with lithium aluminium hydride solution, was used for direct trapping from the target gas and reduction into radiocomplex. The complex was then reacted on this column with HI to form [ 11 C]methyl iodide. The use of one alumina column, instead of a freezing trap, reaction vessel and separate unit for iodination, simplifies the apparatus, shortens the synthesis time and is well suitable for automation. (K.A.)

  8. Synthesis of 11-14C-quetiapine, 11-14C-isoclotiapine and 10-(4-methylpiperazin-1-yl)pyrido[4,3-b][1,4]benzothiazepine[10-14C

    International Nuclear Information System (INIS)

    Naghi Saadatjoo; Mohsen Javaheri; Nuclear Science and Technology Research Institute, Tehran; Nader Saemian; Mohsen Amini

    2016-01-01

    Quetiapine is one of the most widely used antipsychotic drug which acts as an antagonist for multiple neurotransmitter receptor sites. 2-[2-(4-(Dibenzo[b,f][1,4]thiazepin-11-yl)piperazin-1-yl)ethoxy]ethanol (quetiapine) labeled with carbon-14 in 11-position has been synthesized as part of a 5-step sequence from anthranilic acid-[carboxy- 14 C]. We have presented a convenient synthetic pathway for labeling of quetiapine with carbon-14 by using one-pot procedures from a key thiazepin-11(10H)-one-[11- 14 C] by good radiochemical yield. And also isoclotiapine[11- 14 C], and 10-(4-methylpiperazin-1-yl)pyrido[4,3-b][1,4]benzothiazepine[10- 14 C], synthesized according to this route. (author)

  9. Distributed control system for NSC tandem-LINAC

    International Nuclear Information System (INIS)

    Ajith Kumar, B.P.; Subrahmaniam, E.T.; Singh, Kundan

    2001-01-01

    The new control system for the tandem-LINAC accelerator system at Nuclear Science Centre (NSC), runs on a network of Pentiums under the LINUX operating system. Some of the computers are interfaced to the devices of the accelerator, using CAMAC, and run a server program. On the same network there are machines providing the operator interface, by running the client program. The client computers use the x-window graphics and shaft encoder knobs interfaced to them to provide the operator interface. The system supports the monitoring and controlling of all the accelerator parameters including the beam profile monitors, from any of the clients. (author)

  10. Pediatric brain stem tumors: analysis of 25 cases

    International Nuclear Information System (INIS)

    Pinel, M.I.S.; Kalifa, C.; Sarrazin, D.; Lemerle, J.

    1985-01-01

    The charts of 25 pediatric patients with brain stem tumors have been reviewed. The use of computed tomography was found to have been valuable in diagnosis and follow-up, as well as in the design of radiation therapy portals. Radiotherapy and combination chemotherapy with VM-26 (4'-1 demethyl-epipodophyllo toxin B-D-thenylidene glucoside) and CCNU(1-2-chloroethyl-methyl-3-Cyclohexyl-1-nitrosourea) were the treatment employed. (M.A.C.) [pt

  11. NSC KIPT Linux cluster for computing within the CMS physics program

    International Nuclear Information System (INIS)

    Levchuk, L.G.; Sorokin, P.V.; Soroka, D.V.

    2002-01-01

    The architecture of the NSC KIPT specialized Linux cluster constructed for carrying out work on CMS physics simulations and data processing is described. The configuration of the portable batch system (PBS) on the cluster is outlined. Capabilities of the cluster in its current configuration to perform CMS physics simulations are pointed out

  12. Synthesis of N-[methyl-11C]hydromorphone by using multivariate strategies for optimization of radiochemical yields

    International Nuclear Information System (INIS)

    Rimland, Annika; Bergson, Goeran; Obenius, Ulf; Sjoeberg, Stefan; Langstroem, Bengt

    1987-01-01

    The synthesis of N-[methyl- 11 C]hydromorphone has been performed by using [ 11 C]methyl iodide and desmethyl hydromorphone in a mixture of dimethylsulphoxide and dimethylformamide as solvent. Optimization of the radiochemical yield by varying the reaction conditions was performed by using multivariate strategies. The labelled hydromorphone was obtained in 72% radiochemical yield in the alkylation reaction with [ 11 C]-methyl iodide, counted from the end of the [ 11 C]methyl iodide synthesis. N-[Methyl- 11 C]hydromorphone was obtained as a ready injectable pharmaceutical solution with a total synthesis time of 40 min and in a 10% total radiochemical yield, with a radiochemical purity > 99.5%, according to HPLC analysis. (author)

  13. Synthesis of methyl [(chloro-2 ethyl)-3 nitroso-3 Ureido]-3 Didesoxy-2,3 α-D-Arabino-hexopyrannoside labelled with carbon-14 or carbon-13 (CY 233 - SR 90008)

    International Nuclear Information System (INIS)

    Sion, R.; Schumer, A.; Durme, E. van; Gouyette, A.; Geslin, M.; Fournier, J.P.; Roger, P.

    1990-01-01

    CY 233 (Ecomustine or SR 90098) is a new antitumour nitrosourea: it is characterized by a 2-chloroethylnitrosourea substituent on a dideoxycarbohydrate. It has been labelled with 14 C on a) the carbonyl group of the urea in four stages starting with 14 COCl 2 , b) the second carbon of the chloroethyl group in four stages starting with [ 14 C] ethanolamine, and c) on the methyl group on the anomeric centre of the carbohydrate in three stages starting with 14 CH 3 OH. The final position was also labelled with 13 C starting with 13 CH 3 OH. These differently labelled compounds are suitable for mechanistic studies of antitumour activity. (author)

  14. SNP rs16906252C>T is an expression and methylation quantitative trait locus associated with an increased risk of developing MGMT-methylated colorectal cancer

    Science.gov (United States)

    Kuroiwa-Trzmielina, Joice; Wang, Fan; Rapkins, Robert W.; Ward, Robyn L.; Buchanan, Daniel D.; Win, Aung Ko; Clendenning, Mark; Rosty, Christophe; Southey, Melissa C.; Winship, Ingrid M.; Hopper, John L.; Jenkins, Mark A.; Olivier, Jake; Hawkins, Nicholas J.; Hitchins, Megan P.

    2016-01-01

    Purpose Methylation of the MGMT promoter is the major cause of O6-methylguanine methyltransferase deficiency in cancer and has been associated with the T variant of the promoter-enhancer SNP rs16906252C>T. We sought evidence for an association between the rs16906252C>T genotype and increased risk of developing a subtype of colorectal cancer (CRC) featuring MGMT methylation, mediated by genotype-dependent epigenetic silencing within normal tissues. Experimental design By applying a molecular pathological epidemiology case-control study design, associations between rs16906252C>T and risk for CRC overall, and CRC stratified by MGMT methylation status, were estimated using multinomial logistic regression in two independent retrospective series of CRC cases and controls. The test sample comprised 1054 CRC cases and 451 controls from Sydney, Australia. The validation sample comprised 612 CRC cases and 245 controls from the Australasian Colon Cancer Family Registry (ACCFR). To determine if rs16906252C>T was linked to a constitutively altered epigenetic state, quantitative allelic expression and methylation analyses were performed in normal tissues. Results An association between rs16906252C>T and increased risk of developing MGMT-methylated CRC in the Sydney sample was observed (OR 3.3; 95%CI=2.0–5.3; PT represents an expression and methylation quantitative trait locus. Conclusions We provide evidence that rs16906252C>T is associated with elevated risk for MGMT-methylated CRC, likely mediated by constitutive epigenetic repression of the T allele. PMID:27267851

  15. Radiosynthesis of dimethyl-2-[{sup 18}F]-(fluoromethyl)-6-methyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate for L-type calcium channel imaging

    Energy Technology Data Exchange (ETDEWEB)

    Sadeghpour, H. [Nuclear Medicine Research Group, Agricultural, Medical and Industrial Research School (AMIRS), Karaj (Iran); Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran Univ. of Medical Sciences, Tehran (Iran); Jalilian, A.R.; Akhlaghi, M.; Mirzaei, M. [Nuclear Medicine Research Group, Agricultural, Medical and Industrial Research School (AMIRS), Karaj (Iran); Shafiee, A. [Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran Univ. of Medical Sciences, Tehran (Iran); Miri, R. [Medicinal and Natural Products Chemistry Research Center, Shiraz Univ. of Medical Sciences, Shiraz (Iran)

    2008-07-01

    Dimethyl 2-(fluoromethyl)-6-methyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate 4a, a fluorinated nifedipine analog, has been shown to elicit significant calcium channel blocker activity using a guinea pig ileal longitudinal smooth muscle model. In order to perform biological studies for detection of L-type calcium channel distribution, we decided to prepare the [{sup 18}F]-labeled compound. The latter compound was prepared in no-carrier-added (n.c.a.) form from dimethyl 2-(bromomethyl)-6-methyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate 2 in one step at 80 C in Kryptofix[222]/K[{sup 18}F]F and acetonitrile as a solvent in 15 min. Column chromatography afforded the radiochemically pure compound in 20 min. Radiochemical purity of the {sup 18}F-nifedipine was determined by RTLC and HPLC (> 98%) and specific activity of 21-48 GBq/{mu}mol (EOB). (orig.)

  16. Effect of aldicarb on growth and radio-carbon (/sup 14/C) and radio-phosphorus (/sup 32/P) assimilation by Rhizobium japonicum

    Energy Technology Data Exchange (ETDEWEB)

    Balasubramanian, A; Nilakantan, G [University of Agricultural Sciences, Bangalore (India). Radiotracer Lab.

    1976-01-01

    In vitro studies on the effect of aldicarb (2-methyl-2-(methyl thio) propionaldehde-o-methyl carbamoyl oxime), a soil applied systemic insecticide, on Rhizobium japonicum revealed that the chemical (at 1,2 and 5 ppm levels) stimulated the growth of the organism initially upto 48 hr which declined thereafter upto 72 hr. The incorporation of /sup 14/C-glucose by the cells considerably reduced due to the insecticide treatment. The production of extracellular, water-soluble slime (polysacchardes) was also reduced considerably with increased concentrations of the chemical. However, the incorporation of /sup 14/C-radio-activity in the extracellular slime generally enhanced due to the treatment, upto 6 hr after injection of the radioactivity, which declined significantly later at 15 hr, indicating a qualitative difference in the extracellular polysaccharides produced by the insecticide treated cells. The insecticide treatment drastically reduced the incorporation of /sup 32/P-disodium hydrogen phosphate into Rhizobium cells, but enhanced the specific activity of the extracellular polysacchrides.

  17. (E-2-Methyl-6-{[(5-methylpyridin-2-ylimino]methyl}phenol

    Directory of Open Access Journals (Sweden)

    Md. Azharul Arafath

    2017-01-01

    Full Text Available In the title compound, C14H14N2O, the dihedral angle between the aromatic rings is 5.54 (9°. The conformation is reinforced by an intramolecular O—H...N hydrogen bond, which closes an S(6 ring. The pyridine N atom and methyl group lie to opposite sides of the molecule. In the crystal, the molecules are linked into a zigzag chain propagating in [0-11] by weak C—H...O hydrogen bonds.

  18. The Human Tyrosyl-DNA Phosphodiesterase 1 (hTdp1) Inhibitor NSC120686 as an Exploratory Tool to Investigate Plant Tdp1 Genes.

    Science.gov (United States)

    Macovei, Anca; Pagano, Andrea; Sabatini, Maria Elisa; Grandi, Sofia; Balestrazzi, Alma

    2018-03-28

    The hTdp1 (human tyrosyl-DNA phosphodiesterase 1) inhibitor NSC120686 has been used, along with topoisomerase inhibitors, as a pharmacophoric model to restrain the Tdp1 activity as part of a synergistic treatment for cancer. While this compound has an end-point application in medical research, in plants, its application has not been considered so far. The originality of our study consists in the use of hTdp1 inhibitor in Medicago truncatula cells, which, unlike human cells, contain two Tdp1 genes. Hence, the purpose of this study was to test the hTdp1 inhibitor NSC120686 as an exploratory tool to investigate the plant Tdp1 genes, since their characterization is still in incipient phases. To do so, M. truncatula calli were exposed to increasing (75, 150, 300 μM) concentrations of NSC120686. The levels of cell mortality and DNA damage, measured via diffusion assay and comet assay, respectively, were significantly increased when the highest doses were used, indicative of a cytotoxic and genotoxic threshold. In addition, the NSC120686-treated calli and untreated MtTdp1α -depleted calli shared a similar response in terms of programmed cell death (PCD)/necrosis and DNA damage. Interestingly, the expression profiles of MtTdp1α and MtTdp1β genes were differently affected by the NSC120686 treatment, as MtTdp1α was upregulated while MtTdp1β was downregulated. The NSC120686 treatment affected not only the MtTdp1 genes but also other genes with roles in alternative DNA repair pathways. Since the expression patterns of these genes were different than what was observed in the MtTdp1α -depleted plants, it could be hypothesized that the NSC120686 treatment exerts a different influence compared to that resulting from the lack of the MtTdp1α gene function.

  19. 1,1′-{1,4-Phenylene bis[3-(6-chloro-2-methyl-4-phenylquinolin-3-yl-4,5-dihydro-1H-pyrazole-5,1-diyl]}dibutan-1-one

    Directory of Open Access Journals (Sweden)

    Allaoua Kedjadja

    2015-10-01

    Full Text Available A new polycyclic compound, 1,1′-{1,4-phenylene bis[3-(6-chloro-2-methyl-4-phenylquinolin-3-yl-4,5-dihydro-1H-pyrazole-5,1-diyl]}dibutan-1-one (3 has been synthesized by cyclocondensation of (2E,2′E-1,1′-bis(6-chloro-2-methyl-4-phenylquinolin-3-yl-3,3′-(1,4-phenylenediprop-2-en-1-one (2 and hydrazine hydrate in butanoic acid. The structure of this compound was established by elemental analysis, 1H-NMR, 13C-NMR, mass and IR spectroscopy.

  20. New bioactive motifs and their use in functionalized self-assembling peptides for NSC differentiation and neural tissue engineering

    Science.gov (United States)

    Gelain, F.; Cigognini, D.; Caprini, A.; Silva, D.; Colleoni, B.; Donegá, M.; Antonini, S.; Cohen, B. E.; Vescovi, A.

    2012-04-01

    discovery of novel functional motifs fostering transplanted stem cell engraftment and nervous fiber regeneration. Using phage display technology we have discovered new peptide sequences that bind to murine neural stem cell (NSC)-derived neural precursor cells (NPCs), and promote their viability and differentiation in vitro when linked to LDLK12 self-assembling peptide (SAPeptide). We characterized the newly functionalized LDLK12 SAPeptides via atomic force microscopy, circular dichroism and rheology, obtaining nanostructured hydrogels that support human and murine NSC proliferation and differentiation in vitro. One functionalized SAPeptide (Ac-FAQ), showing the highest stem cell viability and neural differentiation in vitro, was finally tested in acute contusive spinal cord injury in rats, where it fostered nervous tissue regrowth and improved locomotor recovery. Interestingly, animals treated with the non-functionalized LDLK12 had an axon sprouting/regeneration intermediate between Ac-FAQ-treated animals and controls. These results suggest that hydrogels functionalized with phage-derived peptides may constitute promising biomimetic scaffolds for in vitro NSC differentiation, as well as regenerative therapy of the injured nervous system. Moreover, this multi-disciplinary approach can be used to customize SAPeptides for other specific tissue engineering applications. Electronic supplementary information (ESI) available: Supporting methods and data about CD spectral analysis of SAPeptide solutions (Fig. S1), neural differentiation of murine and human NSCs (Fig. S2) on SAPeptide scaffolds, and their statistical analysis (Table S1). See DOI: 10.1039/c2nr30220a

  1. Synthesis of [2-13C, 2-14C] 2-aminoethanol, [1-13C, 1-14C] 2-chloroethylamine, N,N'-bis([1-13C, 1-14C] 2-chloroethyl)-N-nitrosourea(BCNU) and N-([1-13C, 1-14C] 2-chloroethyl)-N-nitrosourea(CNU)

    International Nuclear Information System (INIS)

    Narayan, R.; Chang, C-j.

    1982-01-01

    [2- 13 C, 2- 14 C]2-Aminoethanol hydrochloride was prepared in good yield from Na*CN in a two step sequence by first converting the Na*CN to OHCH 2 *CN and then reducing the nitrile directly with a solution of borane-tetrahydrofuran complex. The reaction procedure was simple and the pure product could be obtained readily. Using this specifically labelled precursor, the synthesis of [1- 13 C, 1- 14 C]2-chloroethylamine hydrochloride, N-([1- 13 C, 1- 14 C]2-chloroethyl)-N-nitrosourea(CNU) and N,N'-bis([1- 13 C, 1- 14 C]2-chloroethyl)-N-nitrosourea(BCNU) in good yield without isotope scrambling was also reported. (author)

  2. Candida Rugosa Lipase-catalyzed Kinetic Resolution of 3-(Isobutyryloxy)methyl 4-[2-(Difluoromethoxy)phenyl]-2-methyl-5,5-dioxo-1,4-dihydrobenzothieno[3,2-b]pyridine-3-carboxylate

    NARCIS (Netherlands)

    Sobolev, A.; Zhalubovskis, R.; Franssen, M.C.R.; Vigante, B.; Chekavichus, B.; Duburs, G.; Groot, de Æ.

    2004-01-01

    The lipase-catalyzed kinetic resolution of 3-(isobutyryloxy)methyl 4-[2-(difluoromethoxy)phenyl]-2-methyl-5,5-dioxo-1,4-dihydrobenzothieno[3,2-b]pyridine-3-carboxylate has been performed. The most enantioselective reaction (E = 28) was transesterification with n-butanol in water-saturated toluene at

  3. The synthesis of the carbonyl-14C analog of zatosetron maleate, a potent, long acting, orally effective 5-HT3 receptor antagonist

    International Nuclear Information System (INIS)

    O'Bannon, D.D.; Wheeler, W.J.

    1991-01-01

    5-chloro-2,3-dihydro-2,2-dimethyl-N-(8-methyl-8-azabicyclo-[3.2.1.]-oct-3-yl-7-benzofurancarboxamide-[carbonyl- 14 C] (Z)-2-butenedioate (zatosetron-[ 14 C] maleate,1), has been prepared from 5-chloro-7-bromo-2,3-dihydro-2,2-dimethylbenzofuran (5) in four radiochemical steps with the reaction of 5 with K 14 CN/CuCN as the key step. The synthesis of 5 from 2-bromo-4-chlorophenol is also outlined. (author)

  4. Dynamic acetylation of all lysine 4-methylated histone H3 in the mouse nucleus: analysis at c-fos and c-jun.

    Directory of Open Access Journals (Sweden)

    Catherine A Hazzalin

    2005-12-01

    Full Text Available A major focus of current research into gene induction relates to chromatin and nucleosomal regulation, especially the significance of multiple histone modifications such as phosphorylation, acetylation, and methylation during this process. We have discovered a novel physiological characteristic of all lysine 4 (K4-methylated histone H3 in the mouse nucleus, distinguishing it from lysine 9-methylated H3. K4-methylated histone H3 is subject to continuous dynamic turnover of acetylation, whereas lysine 9-methylated H3 is not. We have previously reported dynamic histone H3 phosphorylation and acetylation as a key characteristic of the inducible proto-oncogenes c-fos and c-jun. We show here that dynamically acetylated histone H3 at these genes is also K4-methylated. Although all three modifications are proven to co-exist on the same nucleosome at these genes, phosphorylation and acetylation appear transiently during gene induction, whereas K4 methylation remains detectable throughout this process. Finally, we address the functional significance of the turnover of histone acetylation on the process of gene induction. We find that inhibition of turnover, despite causing enhanced histone acetylation at these genes, produces immediate inhibition of gene induction. These data show that all K4-methylated histone H3 is subject to the continuous action of HATs and HDACs, and indicates that at c-fos and c-jun, contrary to the predominant model, turnover and not stably enhanced acetylation is relevant for efficient gene induction.

  5. The synthesis of (-)-4-methyl-8-chloro-trans-1,2,3,4,4a,5,6,10b-octahydrobenzo-[f]-quinolin-3-one-[3-14C] (LY300502-[14C]) via a circuitous route

    International Nuclear Information System (INIS)

    Fengjiun Kuo; Wheeler, W.J.

    1994-01-01

    The synthesis of the C-14 labeled isotopomer of LY300502, a potent 5α-reductase inhibitor has been accomplished in four radiochemical steps. The route involves the synthesis of LY300502-[ 14 C] from LY300502 via a circuitous route; the label was introduced with ethyl chloroformate-[carbonyl- 14 C]. (author)

  6. Synthesis of bisaramil labelled with carbon-14 and deuterium

    International Nuclear Information System (INIS)

    Szammer, J.; Simon-Trompler, E.; Mlinko, S.

    1994-01-01

    [6,8- 14 C 2 ]-Bisaramil: 3-methyl-7-ethyl-9α-(4-chlorobenzoyloxy)-3,7-diazabicyclo/3. 3.1./nonane-[6,8- 14 C 2 ] monohydrochloride and [7-N-D 5 -ethyl]-Bisaramil: 3-methyl-7-[D 5 -ethyl]-9α-(4-chlorobenzoyloxy)-3,7-diazabicy clo/3.3.1./nonane monohydrochloride were synthesized in four steps from 14 CO 2 (6% overall yield) and in six steps from [D 6 ]-ethanol (4% overall yield), respectively. (Author)

  7. Nature of the C2-methylation effect on the properties of imidazolium ionic liquids.

    Science.gov (United States)

    Rodrigues, Ana S M C; Lima, Carlos F R A C; Coutinho, João A P; Santos, Luís M N B F

    2017-02-15

    Methylation at the C2 position of 1,3-disubstituted imidazolium-based ionic liquids (ILs) is one of the structural features that has gained attention due to its drastic impact on thermophysical and transport properties. Several hypotheses have been proposed to explain this effect but there is still much discrepancy. Aiming for the rationalization of the effects of these structural features on the properties of imidazolium ILs, we present a thermodynamic and computational study of two methylated ILs at the C2 position of imidazolium, [ 1 C 4 2 C 1 3 C 1 im][NTf 2 ] and [ 1 C 3 2 C 1 3 C 1 im][NTf 2 ]. The phase behaviour (glass transition and vaporization equilibrium) and computational studies of the anion rotation around the cation and ion pair interaction energies for both ILs were explored. The results have shown that C2-methylation has no impact on the enthalpy of vaporization. However, it decreases the entropy of vaporization, which is a consequence of the change in the ion pair dynamics that affects both the liquid and gas phases. In addition, the more hindered dynamics of the ion pair are also reflected in the increase in the glass transition temperature, T g . The entropic contribution of anion-around-cation rotation in the imidazolium [NTf 2 ] ILs was quantified experimentally by the comparative analysis of the entropy of vaporization, and computationally by the calculation of the entropies of hindered internal rotation. The global results exclude the existence of significant H-bonding in the C2-protonated (non-methylated) ILs and explain the C2-methylation effect in terms of reduced entropy of the ion pair in the liquid and gas phases. In light of these results, the C2-methylation effect is intrinsically entropic and originates from the more hindered anion-around-cation rotation as a consequence of the substitution of the -H with a bulkier -CH 3 group.

  8. Myo-inositol-14C, phytic acid-14C and ferric phytate-14C metabolism through microbian action in an andosol soil

    International Nuclear Information System (INIS)

    Gonzalez I, J.

    1977-01-01

    The myo-inositol- 14 C, phytic acid- 14 C and ferric phytate- 14 C compounds were incubated in an andosol soil at 70% of the field capacity and at 36.5 deg C during twelve days. These compounds suffered a microbian oxidation at 14 CO 2 of 61.0, 1.9 and 0% respectively. The fixation of the phytic acid- 14 C was observed through the fast decrease in the metabolism, due to the formation of complexes with the Fe and Al (phytates). The myo-inositol- 14 C metabolism was reduced by a factor of nine at the second incubation day. The following mechanisms were observed in the myo-inositol metabolism: (i) adsorption of the inositol by the soil minerals, (ii) adsorption by humic acids, (iii) myo-inositol phosphorylation and (iv) epimerization of myo-inositol to chiro-inositol. It was found that the (i) and (ii) formation depends on the soil microbian activity. The (i), (ii) and (iii) interactions were considered as possible mechanisms for the inhibition of the myo-inositol microbian oxidation. The inhibition of the myo-inositol oxidation through adsorption or phosphorylation is considered as a chemical blockade for the hydroaxial group, avoiding this way a microbian oxidation stereospecific of this hydroxil group. (author)

  9. Age, allocation and availability of nonstructural carbon in mature red maple trees.

    Science.gov (United States)

    Carbone, Mariah S; Czimczik, Claudia I; Keenan, Trevor F; Murakami, Paula F; Pederson, Neil; Schaberg, Paul G; Xu, Xiaomei; Richardson, Andrew D

    2013-12-01

    The allocation of nonstructural carbon (NSC) to growth, metabolism and storage remains poorly understood, but is critical for the prediction of stress tolerance and mortality. We used the radiocarbon ((14) C) 'bomb spike' as a tracer of substrate and age of carbon in stemwood NSC, CO2 emitted by stems, tree ring cellulose and stump sprouts regenerated following harvesting in mature red maple trees. We addressed the following questions: which factors influence the age of stemwood NSC?; to what extent is stored vs new NSC used for metabolism and growth?; and, is older, stored NSC available for use? The mean age of extracted stemwood NSC was 10 yr. More vigorous trees had both larger and younger stemwood NSC pools. NSC used to support metabolism (stem CO2 ) was 1-2 yr old in spring before leaves emerged, but reflected current-year photosynthetic products in late summer. The tree ring cellulose (14) C age was 0.9 yr older than direct ring counts. Stump sprouts were formed from NSC up to 17 yr old. Thus, younger NSC is preferentially used for growth and day-to-day metabolic demands. More recently stored NSC contributes to annual ring growth and metabolism in the dormant season, yet decade-old and older NSC is accessible for regrowth. © 2013 The Authors. New Phytologist © 2013 New Phytologist Trust.

  10. Influence of pesticide applications on degradation of the herbicide 14C - 2,4-D in different soils

    International Nuclear Information System (INIS)

    Marcondes, Marcilio Amaral

    2001-01-01

    Despite the importance of pesticide usage for the food production, its indiscriminate use may cause changes in the soil fertility, because pesticides influence soil microorganisms which are important for the biogeochemical cycles. The influence of applications of several pesticides, as recommended for cotton culture, was studied on the bioactivity of different soils (from Sao Paulo and Tatui, SP) by using radiometric techniques and a closed system for detection of bio mineralization of ''1 4 C-2,4-D ( 14 C-2,4-dichlorophenoxyacetic acid) and production of 14 C-volatile compounds. The 14 C-2,4-D dissipation under influence of other pesticide applications was also studied by determination of 14 C-extractable residues, 14 C-bound residues and qualitative and quantitative analysis of the 14 C-extractable residues by high pressure liquid chromatography (HPLC) and thin layer chromatography (TLC). 14 C-volatile compounds were never detected but increases and decreases of bio mineralization were detected in both soils after different treatments. The mixture of deltamethrin + methyl parathion increased significantly the bioactivity in both soils; nevertheless, monocrotophos did not have any influence. The applications of different pesticides have also influenced the 14 C-2,4-D dissipation, because the radiocarbon recovered as 14 C-extractable residues differed between the treated and untreated samples of both soils. On the other hand, the pesticide applications did not influence the production of 14 C-bound residues. This 14 C-residue was produced in larger amounts by the richest in organic matter soil (Sao Paulo). Although radiocarbon had been detected not only as 14 'C-2,4-D but also as a 14 C-metabolite, in both soils and treatments, results indicate that the ' 14 C-2,4-D dissipation varied in the two studied soils and was influenced by treatments with others pesticides. (author)

  11. Synthesis of radioactively methyl-labelled (1)-carnitine

    International Nuclear Information System (INIS)

    Ingalls, S.T.; Hoppel, C.L.; Turkaly, J.S.

    1982-01-01

    Commercial (l)-carnitine chloride was N-demethylated by the action of sodium benzenemercaptide in warm N,N-dimethylformamide. The product 4-(N,N-dimethylammonio)-3-hydroxybutanoic acid chloride salt was isolated in good yield by ion exchange chromatography. Methylation of the product by 14 C -iodomethane in dry methanol produced biologically active 4-N-Me- 14 C -(l)-carnitine chloride of high specific activity in excellent yield. (author)

  12. Adsorption and leaching of novel fungicide pyraoxystrobin on soils by 14C tracing method.

    Science.gov (United States)

    Liu, Xunyue; Wu, Huiming; Hu, Tingting; Chen, Xia; Ding, Xingcheng

    2018-01-19

    Pyraoxystrobin, (E)-2-(2-((3-(4-chlorophenyl)-1-methyl-1H-pyrazole-5-yloxy)methyl)phenyl)-3-methoxyacrylate, is a newly developed strobilurin fungicide with high antifungal efficiency. It has high potential to enter soil environments that might subsequently impact surface and groundwater. Therefore, 14 C-labeled pyraoxystrobin was used as a tracer to study the adsorption/desorption and migration behavior of this compound under laboratory conditions in three typical agricultural soils. The adsorption isotherms conformed with the Freundlich equation. Single factor analysis showed that organic matter content was the most important factor influencing the adsorption. The highest adsorption level was measured in soil with low pH and high organic carbon content. Once adsorbed, only 2.54 to 6.41% of the adsorbed compound could be desorbed. In addition, the mobility results from thin-layer chromatography and column leaching studies showed that it might be safe to use pyraoxystrobin as a fungicide without causing groundwater pollution from both runoff and leaching, which might be attributed to its strong hydrophobicity. High organic matter content enhanced pyraoxystrobin adsorption and desorption because of the rule of similarity (lipid solubility). In the column leaching study, 95.02% (minimum value) of the applied 14 C remained within the upper 4.0-cm layer after 60 days.

  13. Synthesis of /sup 14/C- and /sup 3/H-labeled fluoxetine, a selective serotonin uptake inhibitor

    Energy Technology Data Exchange (ETDEWEB)

    Robertson, D.W.; Krushinski, J.H.; Wong, D.T.; Kau, D.

    1987-11-01

    Fluoxetine (N-methyl-..gamma..-(4-(trifluoromethyl)phenoxy) benzenepropanamine) is a potent, highly selective serotonin uptake inhibitor that is useful in treating a variety of major psychiatric derangements. We have synthesized this compound in /sup 14/C- and /sup 3/H-labeled forms. The tritium label was introduced in the final step by catalytic dehalogenation of the brominated fluoxetine precursor. Reaction conditions could be controlled such that catalytic hydrogenolysis of the labile C-O benzylic bond was minimized. Following HPLC purification, (/sup 3/H)-fluoxetine was obtained in a state of high radiochemical purity (98%) and specific activity (20.4 Ci/mmol). The /sup 14/C-label was introduced in the final step via a nucleophilic aromatic substitution reaction between the sodium salt of ..cap alpha..-(2-(methylamino)ethyl)benzenemethanol and uniformly ring-labeled p-chlorobenzotrifluoride. Following purification by flash chromatography, (/sup 14/C)-fluoxetine was obtained in 98.3% radiochemical purity with a specific activity of 5.52 mCi/mmol.

  14. Effect of cooking on14 C-tetrachlorvinphos residues in faba beans

    International Nuclear Information System (INIS)

    Farghaly, M.; Zayed, S.M.A.D.

    1986-01-01

    The effect of cooking on 14 C-tetrachlorvinphos in stored vicia faba beans was studied. The results indicated that over 50% of the dose originally present inside the grains (37 ppm), could be recovered in the aqueous extract of the cooked grains. Considerable portion of radioactivity (About 22%) was associated with the grains in a non-extractable from. Residues in cooked beans included, in addition to a small amount of the parent insecticide, desmethyl tetrachlorvinphos, mono methyl phosphate and dimethyl phosphate. The results obtained indicate that tetrachlorvinphos residues are not appreciably affected by cooking. 1 tab

  15. Control of box C/D snoRNP assembly by N6-methylation of adenine.

    Science.gov (United States)

    Huang, Lin; Ashraf, Saira; Wang, Jia; Lilley, David Mj

    2017-09-01

    N 6 -methyladenine is the most widespread mRNA modification. A subset of human box C/D snoRNA species have target GAC sequences that lead to formation of N 6 -methyladenine at a key trans Hoogsteen-sugar A·G base pair, of which half are methylated in vivo The GAC target is conserved only in those that are methylated. Methylation prevents binding of the 15.5-kDa protein and the induced folding of the RNA Thus, the assembly of the box C/D snoRNP could in principle be regulated by RNA methylation at its critical first stage. Crystallography reveals that N 6 -methylation of adenine prevents the formation of trans Hoogsteen-sugar A·G base pairs, explaining why the box C/D RNA cannot adopt its kinked conformation. More generally, our data indicate that sheared A·G base pairs (but not Watson-Crick base pairs) are more susceptible to disruption by N 6 mA methylation and are therefore possible regulatory sites. The human signal recognition particle RNA and many related Alu retrotransposon RNA species are also methylated at N6 of an adenine that forms a sheared base pair with guanine and mediates a key tertiary interaction. © 2017 The Authors. Published under the terms of the CC BY 4.0 license.

  16. Bee Venom Protects against Rotenone-Induced Cell Death in NSC34 Motor Neuron Cells

    Directory of Open Access Journals (Sweden)

    So Young Jung

    2015-09-01

    Full Text Available Rotenone, an inhibitor of mitochondrial complex I of the mitochondrial respiratory chain, is known to elevate mitochondrial reactive oxygen species and induce apoptosis via activation of the caspase-3 pathway. Bee venom (BV extracted from honey bees has been widely used in oriental medicine and contains melittin, apamin, adolapin, mast cell-degranulating peptide, and phospholipase A2. In this study, we tested the effects of BV on neuronal cell death by examining rotenone-induced mitochondrial dysfunction. NSC34 motor neuron cells were pretreated with 2.5 μg/mL BV and stimulated with 10 μM rotenone to induce cell toxicity. We assessed cell death by Western blotting using specific antibodies, such as phospho-ERK1/2, phospho-JNK, and cleaved capase-3 and performed an MTT assay for evaluation of cell death and mitochondria staining. Pretreatment with 2.5 μg/mL BV had a neuroprotective effect against 10 μM rotenone-induced cell death in NSC34 motor neuron cells. Pre-treatment with BV significantly enhanced cell viability and ameliorated mitochondrial impairment in rotenone-treated cellular model. Moreover, BV treatment inhibited the activation of JNK signaling and cleaved caspase-3 related to cell death and increased ERK phosphorylation involved in cell survival in rotenone-treated NSC34 motor neuron cells. Taken together, we suggest that BV treatment can be useful for protection of neurons against oxidative stress or neurotoxin-induced cell death.

  17. Immortalization of human neural stem cells with the c-myc mutant T58A.

    Directory of Open Access Journals (Sweden)

    Lidia De Filippis

    Full Text Available Human neural stem cells (hNSC represent an essential source of renewable brain cells for both experimental studies and cell replacement therapies. Their relatively slow rate of proliferation and physiological senescence in culture make their use cumbersome under some experimental and pre-clinical settings. The immortalization of hNSC with the v-myc gene (v-IhNSC has been shown to generate stem cells endowed with enhanced proliferative capacity, which greatly facilitates the study of hNSCs, both in vitro and in vivo. Despite the excellent safety properties displayed by v-IhNSCs--which do not transform in vitro and are not tumorigenic in vivo--the v-myc gene contains several mutations and recombination elements, whose role(s and effects remains to be elucidated, yielding unresolved safety concerns. To address this issue, we used a c-myc T58A retroviral vector to establish an immortal cell line (T-IhNSC from the same hNSCs used to generate the original v-IhNSCs and compared their characteristics with the latter, with hNSC and with hNSC immortalized using c-myc wt (c-IhNSC. T-IhNSCs displayed an enhanced self-renewal ability, with their proliferative capacity and clonogenic potential being remarkably comparable to those of v-IhNSC and higher than wild type hNSCs and c-IhNSCs. Upon growth factors removal, T-IhNSC promptly gave rise to well-differentiated neurons, astrocytes and most importantly, to a heretofore undocumented high percentage of human oligodendrocytes (up to 23%. Persistent growth-factor dependence, steady functional properties, lack of ability to generate colonies in soft-agar colony-forming assay and to establish tumors upon orthotopic transplantation, point to the fact that immortalization by c-myc T58A does not bring about tumorigenicity in hNSCs. Hence, this work describes a novel and continuous cell line of immortalized human multipotent neural stem cells, in which the immortalizing agent is represented by a single gene which, in

  18. Bioconcentration of haloxyfop-methyl in bluegill (Lepomis macrochirus Rafinesque)

    International Nuclear Information System (INIS)

    Murphy, P.G.; Lutenske, N.E.

    1990-01-01

    Bluegill (Lepomis macrochirus Rafinesque) were exposed to a 14 C haloxyfop-methyl [methyl 2-(4-((3-chloro-5-(trifluoromethyl)-2-pyridinyl)oxy)phenoxy)propanoate] concentration averaging 0.29 μg/L under flow-through conditions for 28 days. At the end of 28 days, the fish were transferred to clean water for a 4-day flow-through clearance period. Bluegill were found to rapidly absorb the ester from water which was then biotransformed at an extremely fast rate within the fish, such that essentially no haloxyfop-methyl was detected in the fish. The estimated bioconcentration factor for haloxyfop-methyl in whole fish was 14 C residue within whole fish was haloxyfop acid [2-(4-((3-chloro-5-(trifluoromethyl)-2-pyridinyl)oxy)phenoxy)propanoic acid] which accounted for an average of about 60% of the total radioactivity. The high rate of biotransformation of the parent compound within the fish demonstrates the importance of basing the bioconcentration factor upon the actual concentration of parent material within the organism rather than the total radioactive residue levels for bioconcentration studies with radiolabeled compounds

  19. A new C-methylated flavonoid glycoside from Pinus densiflora.

    Science.gov (United States)

    Jung, M J; Choi, J H; Chung, H Y; Jung, J H; Choi, J S

    2001-12-01

    A new C-methyl flavonol glycoside, 5,7,8,4'-tetrahydroxy-3-methoxy-6-methylflavone 8-O-beta-D-glucopyranoside (1), has been isolated from the needles of Pinus densiflora, together with kaempferol 3-O-beta-(6"-acetyl)-galactopyranoside.

  20. One-electron reduction of 2- and 6-methyl-1,4-naphthoquinone bioreductive alkylating agents

    International Nuclear Information System (INIS)

    Wilson, I.; Wardman, P.; Lin, T.S.; Sartorelli, A.C.

    1986-01-01

    The semiquinones, Q.-, of derivatives of 2- and 6-methyl-1,4-naphthoquinones, some incorporating leaving groups with substituents such as CH 2 Br or CH 2 OCONHCH 3 , have been produced by radiolytic reduction of Q by (CH 3 )2COH radicals. The absorption spectra and decay kinetics of Q.- were all closely similar to that produced from 2-methyl-1,4-naphthoquinone, with no evidence for unimolecular elimination of a leaving group in the semiquinone form, but immediate loss of leaving group upon two-electron reduction of Q to the hydroquinone. The redox equilibria between Q/Q.- and O2/O2.- were characterized, and reduction potentials of the couples Q/Q.- in water at pH 7.6 were calculated. The implications of these observations for the use of these compounds as bioreductive alkylating agents or as radiosensitizers with potential selective activity toward hypoxic cells are discussed

  1. A procedure for batch separation of 14C-hexose from 14C-sucrose

    International Nuclear Information System (INIS)

    Tarpley, L.; Vietor, D.M.

    1991-01-01

    This presentation describes a method for separating 14 C-hexose from 14 C-sucrose in extracts of plant tissue. Portions of ethanol extracts are treated with activated charcoal in microcentrifuge tubes. Aliquots are removed, ethanol evaporated and replaced with reaction mixture that phosphorylates hexose (HEPPS, K 2 HPO 4 , Mg(C 2 H 3 O 2 ) 2 , ovalbumen, Na 2 ATP, yeast hexokinase). After a time course, the hexokinase reaction is stopped (slowed considerably) to minimize effects of contamination enzyme activities. The stopping agent used is lyxose, a nonphosphorylable analogue of glucose. The strong anionic charge of phosphate introduced through the hexokinase action results in binding (> 95%) of hexose-phosphate to anion-exchange resin. Sucrose remains unbound (> 95%) in solution. This batch ion-exchange is performed in microcentrifuge tubes to allow many samples to be processed simultaneously. Recovery of radiolabel in extracts is complete (99%), and determinations are repeatable (cv = 23%). This method for routinely separating and quantifying 14 C-hexose and 14 C-sucrose in plant tissue extracts can contribute to the economy and feasibility of studies of 14 C-photoassimilate partitioning to soluble sugars within and among plant tissues

  2. Electron transfer in DNA duplexes containing 2-methyl-1,4-naphthoquinone

    OpenAIRE

    Bergeron, François; Houde, Daniel; Hunting, Darel J.; Wagner, J. Richard

    2004-01-01

    2-Methyl-1,4-naphthoquinone (menadione, MQ) was linked to synthetic oligonucleotides and exposed to near-UV light to generate base radical cations in DNA. This model system of electron transfer induced alkali-labile breaks at GG doublets, similar to anthraquinone and metallointercalators systems. In sharp contrast to other systems, the photolysis of MQ–DNA duplexes gave interstrand cross-links and alkali-labile breaks at bases on the complementary strand opposite the MQ moiety. For sequences ...

  3. 2-[(4-Bromophenylimino)methyl]-5-pentadecylphenol

    OpenAIRE

    Basavaraj Padmashali; Patchanita Thamyongkit; Amorn Petsom; Gadada Naganagowda

    2012-01-01

    2-[(4-Bromophenylimino)methyl]-5-pentadecylphenol has been synthesized by reaction of 2-hydroxy-4-pentadecylbenzaldehyde with 4-bromoaniline in 1,4-dioxane and its IR, 1H-NMR, 13C-NMR and MS spectroscopic data are presented.

  4. Reinvestigation of the synthesis and evaluation of [N-methyl-11C]vorozole, a radiotracer targeting cytochrome P450 aromatase

    International Nuclear Information System (INIS)

    Kim, Sung Won; Biegon, Anat; Katsamanis, Zachary E.; Ehrlich, Carolin W.; Hooker, Jacob M.; Shea, Colleen; Muench, Lisa; Xu Youwen; King, Payton; Carter, Pauline; Alexoff, David L.; Fowler, Joanna S.

    2009-01-01

    Introduction: We reinvestigated the synthesis of [N-methyl- 11 C]vorozole, a radiotracer for aromatase, and discovered the presence of an N-methyl isomer which was not removed in the original purification method. Herein we report the preparation and positron emission tomography (PET) studies of pure [N-methyl- 11 C]vorozole. Methods: Norvorozole was alkylated with [ 11 C]methyl iodide as previously described and also with unlabeled methyl iodide. A high-performance liquid chromatography (HPLC) method was developed to separate the regioisomers. Nuclear magnetic resonance (NMR) spectroscopy ( 13 C and 2D-nuclear Overhauser effect spectroscopy NMR) was used to identify and assign structures to the N-methylated products. Pure [N-methyl- 11 C]vorozole and the contaminating isomer were compared by PET imaging in the baboon. Results: Methylation of norvorozole resulted in a mixture of isomers (1:1:1 ratio) based on new HPLC analysis using a pentafluorophenylpropyl bonded silica column, in which vorozole coeluted one of its isomers under the original HPLC conditions. Baseline separation of the three labeled isomers was achieved. The N-3 isomer was the contaminant of vorozole, thus correcting the original assignment of isomers. PET studies of pure [N-methyl- 11 C]vorozole with and without the contaminating N-3 isomer revealed that only [N-methyl- 11 C]vorozole binds to aromatase. [N-methyl- 11 C]Vorozole accumulated in all brain regions with highest accumulation in the aromatase-rich amygdala and preoptic area. Accumulation was blocked with vorozole and letrozole consistent with reports of some level of aromatase in many brain regions. Conclusions: The discovery of a contaminating labeled isomer and the development of a method for isolating pure [N-methyl- 11 C]vorozole combine to provide a new scientific tool for PET studies of the biology of aromatase and for drug research and development.

  5. Metabolism of [14C]indole-3-acetic acid by the cortical and stelar tissues of Zea mays L. roots

    International Nuclear Information System (INIS)

    Nonhebel, H.M.; Hillman, J.R.; Crozier, A.; Wilkins, M.B.

    1985-01-01

    Reverse-phase high-performance liquid chromatography was used to analyse 14 C-labelled metabolites of idole-3-acetic acid (IAA) formed in the cortical and stelar tissues of Zea mays roots. After a 2-h incubation in [ 14 C]IAA, stelar segments had metabolised between 1-6% of the methanol-extractable radioactivity compared with 91-92% by the cortical segments. The pattern of metabolites produced by cortical segments was similar to that produced by intact segments bathed in aqueous solutions of [ 14 C]IAA. In contrast, when IAA was supplied in agar blocks to stelar tissue protruding from the basal ends of segments, negligible metabolism was evident. On the basis of its retention characteristics both before and after methylation, the major metabolite of [ 14 C]IAA in Zea mays root segments was tentatively identified by high-performance liquid chromatography as oxindole-3-acetic acid. (orig.)

  6. 14C2H4: distribution of 14C-labeled tissue metabolites in pea seedlings

    International Nuclear Information System (INIS)

    Giaquinta, R.; Beyer, E. Jr.

    1977-01-01

    The 14 C-metabolite distribution pattern following 14 C 2 H 4 metabolism in intact pea seedlings (Pisum sativum L.) was determined under various conditions. After a 24 hr exposure to 14 C 2 H 4 , the majority of 14 C-metabolites were water-soluble (60-70%) with lesser amounts in the protein (10-15%), lipid (1%), and insoluble (1-2%) fractions. Ion exchange chromatography of the water-soluble components into basic, neutral, and acidic fractions revealed a 50:40:10 distribution, respectively. Chromatography of the neutral fraction revealed two regions of radioactivity (Rf=0.38) and 0.63 which did not cochromatograph with twenty-two known sugars or neutral metabolites. Chromatograms of the basic fraction contained 3 regions of radioactivity. Similar distribution patterns were noted when 14 C 2 H 4 exposure was followed by a 6 hr air chase or when 5% CO 2 , an antagonist of ethylene action, was present during the exposure. Marked differences in the 14 C-metabolite distribution patterns were obtained when 14 CO 2 was substituted for 14 C 2 H 4 . These results indicate that the metabolic pathway involved in ethylene metabolism is different from that involved in intermediately carbon metabolism. (auth.)

  7. Preparation of D-[U-14C]galactose and α-D-[U-14C]galactose-1-phosphate

    International Nuclear Information System (INIS)

    Kolina, J.; Hromadkova, B.

    1989-01-01

    Optically pure D-[U- 14 C]galactose was prepared on a preparatory scale using the galactokinase enzyme. The suggested procedure allows to also prepare a α-D-[U- 14 C]galactose-1-phosphate and L-[U- 14 ]galactose giving good yield. The experiments proved that the raw fraction isolated from yeast of the Kluyveromyces fragilis strain or the Kluyveromyces lactis strain shows sufficient activity. Phosphorylation of D-[U- 14 C]galactose practically terminates after 30 mins of incubation. DL-[U- 14 C]galactose isolated using preparatory paper chromatography from the acid hydrolyzate of [U- 14 C] polysaccharide is a satisfactory radioactive precursor. The developed preparation procedure theoretically contributed towards the further elucidation of the problem of the proportional representation of galactose stereo-isomers in extracellular polysaccharide isolated from red algae. In this respect data in the literature differ and some sources state a significantly higher propertion of L-galactose. The experiments showed that [U- 14 C] polysaccharide isolated from the red algae Porphyridium cruentum prevalently contains D-[U- 14 C]galactose, which confirms the process of enzyme reaction. (author). 1 tab., 4 refs

  8. Root-uptake of 14C derived from acetic acid and 14C transfer to rice edible parts

    International Nuclear Information System (INIS)

    Ogiyama, Shinichi; Suzuki, Hiroyuki; Inubushi, Kazuyuki; Takeda, Hiroshi; Uchida, Shigeo

    2010-01-01

    Three types of culture experiments using paddy rice (Oryza sativa L.) were performed to examine root-uptake of 14 C in the form of acetic acid: double pot experiment (hydroponics), wet culture experiment (submerged sand medium), and chamber experiment (hydroponics and submerged sand medium). The 14 C radioactivity in the plant, mediums, and atmospheric carbon dioxide ( 14 CO 2 ) in the chamber were determined, and the distribution of 14 C in the plant was visualized using autoradiography. In the double pot experiment, the shoot of the plant and the lower root which was soaked in the culture solution had 14 C radioactivity, but the upper root which did not have contact with the solution had none. There were also 14 C radioactivity in the grains and roots in the wet culture experiment. Results of the chamber experiment showed that 14 CO 2 gas was released from the culture solution in both types of cultures. Results indicated that the 14 C-acetic acid absorbed by rice plant through its root would be very small. Most of the 14 C-acetic acid was transformed into gaseous forms either in the culture solution or rhizosphere. A relatively longer time would be needed to assimilate 14 C derived from acetic acid to grain parts after it was once absorbed by the shoot through the root. Availability of 14 C for the plant in sand culture was considered to be decreased compared with that for the plant in the hydroponics experiment. It was suggested that rice plant absorbed and assimilated 14 C through the plant roots not because of uptake of 14 C-acetic acid but because of uptake of 14 C in gaseous forms such as 14 CO 2 .

  9. Preclinical and clinical evaluation of O-[11C]methyl-L-tyrosine for tumor imaging by positron emission tomography

    International Nuclear Information System (INIS)

    Ishiwata, Kiichi; Tsukada, Hideo; Kubota, Kazuo; Nariai, Tadashi; Harada, Norihiro; Kawamura, Kazunori; Kimura, Yuichi; Oda, Keiichi; Iwata, Ren; Ishii, Kenji

    2005-01-01

    We performed preclinical and clinical studies of O-[ 11 C]methyl-L-tyrosine, a potential tracer for imaging amino acid transport of tumors by positron emission tomography (PET). Examinations of the radiation-absorbed dose by O-[ 11 C]methyl-L-tyrosine and the acute toxicity and mutagenicity of O-methyl-L-tyrosine showed suitability of the tracer for clinical use. The whole-body imaging of monkeys and healthy humans by PET showed low uptake of O-[ 11 C]methyl-L-tyrosine in all normal organs except for the urinary track and bladder, suggesting that the O-[ 11 C]methyl-L-tyrosine PET has the potential for tumor imaging in the whole-body. Finally, the brain tumor imaging was preliminarily demonstrated

  10. Reinvestigation of the synthesis and evaluation of [N-methyl-{sup 11}C]vorozole, a radiotracer targeting cytochrome P450 aromatase

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Sung Won [Medical Department, Brookhaven National Laboratory, Upton, NY 11973 (United States)], E-mail: swkim@bnl.gov; Biegon, Anat; Katsamanis, Zachary E. [Medical Department, Brookhaven National Laboratory, Upton, NY 11973 (United States); Ehrlich, Carolin W. [Johannes-Gutenberg Universitaet Mainz, Institut fuer Organische Chemie, Duesbergweg 10-14, Mainz (Germany); Hooker, Jacob M.; Shea, Colleen [Medical Department, Brookhaven National Laboratory, Upton, NY 11973 (United States); Muench, Lisa [National Institute on Alcoholism and Alcohol Abuse, Bethesda, MD (United States); Xu Youwen; King, Payton; Carter, Pauline; Alexoff, David L. [Medical Department, Brookhaven National Laboratory, Upton, NY 11973 (United States); Fowler, Joanna S. [Medical Department, Brookhaven National Laboratory, Upton, NY 11973 (United States); Department of Psychiatry, Mount Sinai School of Medicine, New York, NY (United States); Department of Chemistry, State University of New York at Stony Brook, Stony Brook, NY (United States)

    2009-04-15

    Introduction: We reinvestigated the synthesis of [N-methyl-{sup 11}C]vorozole, a radiotracer for aromatase, and discovered the presence of an N-methyl isomer which was not removed in the original purification method. Herein we report the preparation and positron emission tomography (PET) studies of pure [N-methyl-{sup 11}C]vorozole. Methods: Norvorozole was alkylated with [{sup 11}C]methyl iodide as previously described and also with unlabeled methyl iodide. A high-performance liquid chromatography (HPLC) method was developed to separate the regioisomers. Nuclear magnetic resonance (NMR) spectroscopy ({sup 13}C and 2D-nuclear Overhauser effect spectroscopy NMR) was used to identify and assign structures to the N-methylated products. Pure [N-methyl-{sup 11}C]vorozole and the contaminating isomer were compared by PET imaging in the baboon. Results: Methylation of norvorozole resulted in a mixture of isomers (1:1:1 ratio) based on new HPLC analysis using a pentafluorophenylpropyl bonded silica column, in which vorozole coeluted one of its isomers under the original HPLC conditions. Baseline separation of the three labeled isomers was achieved. The N-3 isomer was the contaminant of vorozole, thus correcting the original assignment of isomers. PET studies of pure [N-methyl-{sup 11}C]vorozole with and without the contaminating N-3 isomer revealed that only [N-methyl-{sup 11}C]vorozole binds to aromatase. [N-methyl-{sup 11}C]Vorozole accumulated in all brain regions with highest accumulation in the aromatase-rich amygdala and preoptic area. Accumulation was blocked with vorozole and letrozole consistent with reports of some level of aromatase in many brain regions. Conclusions: The discovery of a contaminating labeled isomer and the development of a method for isolating pure [N-methyl-{sup 11}C]vorozole combine to provide a new scientific tool for PET studies of the biology of aromatase and for drug research and development.

  11. Equivalent chain lengths of all C4-C23 saturated monomethyl branched fatty acid methyl esters on methylsilicone OV-1 stationary phase.

    Science.gov (United States)

    Kubinec, Róbert; Blaško, Jaroslav; Górová, Renáta; Addová, Gabriela; Ostrovský, Ivan; Amann, Anton; Soják, Ladislav

    2011-04-01

    Isomer mixtures of monomethyl branched saturated C7-C23 fatty acid methyl esters (FAME) were prepared by performing a methylene insertion reaction to the straight chain FAME and this study model was completed by using commercially available standards of C4-C7 FAME. The equivalent chain lengths (ECL) of all 220 C4-C23 monomethyl branched FAME on OV-1 stationary phase were measured, achieving an average repeatability of ±0.0004 ECL units. The monomethyl branched FAME was identified by GC on the basis of regularity of the fractional chain lengths (FCL) dependence on the number of carbon atoms (C(z)) of individual homologous series of methyl 2-, 3-, …, 21-FAME. The prediction of retention of the first homologues, having the new position of methyl group beginning at higher carbon atoms number, and analogously for the second, third, fourth, and other members of the homologous series, allowed the dependence FCL=f(C(z)) for the first and subsequent members of beginning homologous of monomethyl derivatives of FAME. The identification was confirmed by mass spectrometry. All of the methyl isomers of FAME, which could not be completely separated by gas chromatography due to having a methyl group in surroundings of the middle of the carbon chain, were resolved by mass spectrometry using deconvolution in a SIM-mode. Measured gas chromatographic and mass spectrometric data were applied for identification of the monomethyl branched saturated FAME in tongue coating. Copyright © 2011 Elsevier B.V. All rights reserved.

  12. An efficient synthesis of carbon-14 labelled vigabatrin

    International Nuclear Information System (INIS)

    Gill, H.S.

    1995-01-01

    Vigabatrin-[6- 14 C] ((R,S)-4-amino-5-hexenoic-[6- 14 C] acid) was synthesized by employing Wittig condensation of 1-(1-butenyl) -2-oxo-5-pyrrolidinecarboxaldehyde with methyl-[ 14 C]-triphenyl-phosphonium iodide as the key step. The synthetic sequence involved 3 steps and produced the title compound in 70% overall yield with a radiochemical purity of 100%. (author)

  13. Synthesis of disodium [benzene-U-{sup 14}C]-(4-chlorophenylthio)methylenediphosphonate, [benzene-U-{sup 14}C]-tiludronate

    Energy Technology Data Exchange (ETDEWEB)

    Burgos, Alain; Ellames, G.J. [Alnwick Research Centre (United Kingdom). Dept. of Metabolism and Pharmacokinetics

    1995-12-31

    Disodium [benzene-U-{sup 14}C]-(4-chlorophenylithio)methylenediphosphonate, [benzene-{sup 14}C]-Tiludronate, 2, has been prepared in six steps from [benzene-U-{sup 14}C]-acetanilide in an overall radiochemical yield of 41%. A key step in this transformation was the efficient conversion of [U-{sup 14}C]-4-chloroaniline to [benzene-U-{sup 14}C]-4-chlorophenylthiocyanate, 5, in 83% yield by treatment of the corresponding diazonium salt, 9 with iron(111) thiocyanate. It should be noted that formation of the isomeric [benzene-U-{sup 14}C]-4-chlorophenylisothiocyanate, 11, as a byproduct, was observed in only {approx} 1% yield. (author).

  14. Extraction of pentylbenzene from high molar mass alkanes (C14 and C17) by N-methyl-2-pyrrolidone

    International Nuclear Information System (INIS)

    Fandary, Mohamed S.; Al-Jimaz, Adel S.; Al-Kandary, Jasem A.; Fahim, Mohamed A.

    2006-01-01

    Equilibrium tie line data have been determined for the two ternary liquid systems: {tetradecane, or heptadecane + pentylbenzene + N-methyl-2-pyrrolidone (NMP)} over a temperature range of (298 to 328) K. The two systems studied exhibit type I liquid + liquid phase diagram. The effect of temperature and n-alkane chain length upon solubility, selectivity, and distribution coefficients were investigated experimentally

  15. 6-Methyl-1,2,4-benzenetriol, a new intermediate in penicillic acid biosynthesis in Penicillium cyclopium

    International Nuclear Information System (INIS)

    Sekiguchi, J.; Katayama, S.; Yamada, Y.

    1987-01-01

    Penicillic acid-negative mutants were obtained from a color mutant derived from Penicillium cyclopium NRRL 1888 through N-methyl-N'-nitro-N-nitrosoguanidine treatment. One mutant (SK2N6) accumulated 6-methyl-1,2,4-benzenetriol, which was not previously known to be a metabolite of P. cyclopium, in addition to orsellinic acid and orcinol. The radioactivity of [1- 14 C]acetic acid was rapidly incorporated into 6-methyl-1,2,4-benzenetriol in a culture of P. cyclopium SK2N6. Moreover, the radioactivity of [ 14 C]6-methyl-1,2,4-benzenetriol was efficiently incorporated into penicillic acid in a culture of P. cyclopium NRRL 1888. These data indicate that 6-methyl-1,2,4-benzenetriol is a precursor for penicillic acid biosynthesis. The results on the addition of 1,4-dihydroxy-6-methoxy-2-methylbenzene, 6-methoxy-2-methylbenzoquinone (1,4), and 1-O-methylorcinol to a culture of P. cyclopium SK2N6 indicated that only the former two compounds are converted to penicillic acid. Thus, a new portion of the penicillic acid biosynthetic pathway is proposed

  16. The crystal structure of zwitterionic 2-{[(4-iminiumyl-3-methyl-1,4-dihydropyridin-1-ylmethyl]carbamoyl}benzoate hemihydrate

    Directory of Open Access Journals (Sweden)

    C. S. Chidan Kumar

    2017-07-01

    Full Text Available The asymmetric unit of the title compound, C15H15N3O3·0.5H2O, comprises two 2-{[(4-iminiumyl-3-methyl-1,4-dihydropyridin-1-ylmethyl]carbamoyl}benzoate zwitterions (A and B and a water molecule. The dihedral angles between the pyridine and phenyl rings in the zwitterions are 53.69 (10 and 73.56 (11° in A and B, respectively. In the crystal, molecules are linked by N—H...O, O—H...O, C—H...O and C—H...π(ring hydrogen bonds into a three-dimensional network. The crystal structure also features π–π interactions involving the centroids of the pyridine and phenyl rings [centroid–centroid distances = 3.5618 (12 Å in A and 3.8182 (14 Å in B].

  17. Morphology and performance of poly(2-methoxy-5-(20-ethyl-hexyloxy)-p-phenylenevinylene) (MEH-PPV) : (6,6)-phenyl-C61-butyric acid methyl ester (PCBM) based polymer solar cells

    NARCIS (Netherlands)

    Liu, L.J.; Bavel, van S.S.; Wen, S.P.; Yang, X.N.; Loos, J.

    2013-01-01

    Polymer solar cells were fabricated based on composite films of poly(2-methoxy-5-(2-ethyl-hexyloxy)-1,4-phenylenevinylene) (MEH-PPV):fullerene derivative (6,6)-phenyl-C61-butyric acid methyl ester (PCBM) with weight blend ratio of 1:3, 1:4 and 1:5, spin-coated from chloroform (CF), chlorobenzene

  18. Effects of Cover Crops on the Movement and Fate of Soil-Applied 14C-Fonofos in a Soil-Plant-Water Microcosm

    International Nuclear Information System (INIS)

    Liang, T.T.; Lichtenstein, E.P.

    1981-01-01

    Full text: The effects of corn plants or a ''lawn'' of ryegrass on the movement and metabolism of soil-applied 14 C-(ring)-fonofos were studied in a microcosm which consisted of terrestrial and aquatic components. Artificial rain, applied to the fallow or plant covered soils, resulted in runoff that accumulated in aquaria containing lake bottom mud and aquatic organisms. The presence and the type of a cover crop had a considerable effect on the mobility and metabolism of soil—applied 14 C—fonofos. The insecticide plus its metabolites were least persistent in systems with fallow soils and most persistent in those with ryegrass. Within the terrestrial soil 14 C-compounds moved downwards and were also translocated via the root systems into the leaves of corn and ryegrass. Within the plant tops 86% of the recovered benzene—soluble 14 C-compounds were in the form of the detoxified methyl phenyl sulfone and 2% or less as fonofos. Rain caused a considerable runoff of fallow soil but much less of cropped soil into the aquaria. 14 C-compounds transported were primarily associated with the runoff soil and most of these were later found in the soil—lake mud sediments. 14 C—fonofos was the major constituent in soils and aquatic sediments while the major metabolite recovered from both the terrestrial and aquatic portion of the microcosm was methyl phenyl sulfone, its amounts ranging from 13% to 92% of all benzene—soluble radiocarbon. Relatively small amounts of the insecticidal oxygen analog of fonofos were recovered, the exception being in roots of corn and of ryegrass. (author)

  19. Human folate metabolism using 14C-accelerator mass spectrometry

    International Nuclear Information System (INIS)

    Arjomand, A; Bucholz, B A; Clifford, A J; Duecker, S R; Johnson, H; Schneider, P D; Zulim, R A.

    1999-01-01

    Folate is a water soluble vitamin required for optimal health, growth and development. It occurs naturally in various states of oxidation of the pteridine ring and with varying lengths to its glutamate chain. Folates function as one-carbon donors through methyl transferase catalyzed reactions. Low-folate diets, especially by those with suboptimal methyltransferase activity, are associated with increased risk of neural tube birth defects in children, hyperhomocysteinemic heart disease, and cancer in adults. Rapidly dividing (neoplastic) cells have a high folate need for DNA synthesis. Chemical analogs of folate (antifolates) that interfere with folate metabolism are used as therapeutic agents in cancer treatment. Although much is known about folate chemistry, metabolism of this vitamin in vivo in humans is not well understood. Since folate levels in blood and tissues are very low and methods to measure them are inadequate, the few previous studies that have examined folate metabolism used large doses of radiolabeled folic acid in patients with Hodgkins disease and cancer (Butterworth et al. 1969, Krumdieck et al. 1978). A subsequent protocol using deuterated folic acid was also insufficiently sensitive to trace a physiologic folate dose (Stites et al. 1997). Accelerator mass spectrometry (AMS) is an emerging bioanalytical tool that overcomes the limitations of traditional mass spectrometry and of decay counting of long lived radioisotopes (Vogel et al. 1995). AMS can detect attomolar concentrations of 14 C in milligram-sized samples enabling in vivo radiotracer studies in healthy humans. We used AMS to study the metabolism of a physiologic 80 nmol oral dose of 14 C-folic acid (1/6 US RDA) by measuring the 14 C-folate levels in serial plasma, urine and feces samples taken over a 150-day period after dosing a healthy adult volunteer

  20. 3,4-O-Isopropylidene-2-C-methyl-d-galactonolactone

    Directory of Open Access Journals (Sweden)

    N. Dai

    2010-02-01

    Full Text Available X-ray crystallography unequivocally confirmed the stereochemistry of the 2-C-methyl group in the title molecule, C10H16O6, in which the 1,5-lactone ring exists in a boat conformation. The use of d-galactose in the synthesis determined the absolute stereochemistry. The crystal exists as O—H...O hydrogen-bonded layers in the ab plane, with each molecule acting as a donor and acceptor for two hydrogen bonds.

  1. Bepaling van 14C in afvalwater

    NARCIS (Netherlands)

    Hiemstra YS; Kwakman PJM; Nissan LN; Aldenkamp FJ; LSO

    1998-01-01

    In opdracht van de Hoofdinspectie Milieuhygiene van het ministerie van VROM heeft LSO een methode ontwikkeld om 14C in afvalwater van nucleaire installaties te bepalen. De methode meet organisch gebonden-14C en anorganisch-14C in de vorm van carbonaat (14CO32-) in afvalwater. Het rapport

  2. Crystal structures of eight mono-methyl alkanes (C26–C32 via single-crystal and powder diffraction and DFT-D optimization

    Directory of Open Access Journals (Sweden)

    Lee Brooks

    2015-09-01

    Full Text Available The crystal structures of eight mono-methyl alkanes have been determined from single-crystal or high-resolution powder X-ray diffraction using synchrotron radiation. Mono-methyl alkanes can be found on the cuticles of insects and are believed to act as recognition pheromones in some social species, e.g. ants, wasps etc. The molecules were synthesized as pure S enantiomers and are (S-9-methylpentacosane, C26H54; (S-9-methylheptacosane and (S-11-methylheptacosane, C28H58; (S-7-methylnonacosane, (S-9-methylnonacosane, (S-11-methylnonacosane and (S-13-methylnonacosane, C30H62; and (S-9-methylhentriacontane, C32H66. All crystallize in space group P21. Depending on the position of the methyl group on the carbon chain, two packing schemes are observed, in which the molecules pack together hexagonally as linear rods with terminal and side methyl groups clustering to form distinct motifs. Carbon-chain torsion angles deviate by less than 10° from the fully extended conformation, but with one packing form showing greater curvature than the other near the position of the methyl side group. The crystal structures are optimized by dispersion-corrected DFT calculations, because of the difficulties in refining accurate structural parameters from powder diffraction data from relatively poorly crystalline materials.

  3. Metabolism of [ 14 C]GA 19 and [ 14 C]GA 53 by ecotypes of Betula ...

    African Journals Online (AJOL)

    Continuing with this line of research, we studied the metabolism of 14C-labelled GA19 and GA53. [14C]GA19 and [14C] A53 were applied to the apices of the northern ecotype (67º N) and to the leaves of the southern ecotype (64º N) of Betula pendula Roth. under different photoperiods and at different times in order to ...

  4. ARC (NSC 188491 has identical activity to Sangivamycin (NSC 65346 including inhibition of both P-TEFb and PKC

    Directory of Open Access Journals (Sweden)

    Hollingshead Melinda G

    2009-02-01

    Full Text Available Abstract Background The nucleoside analog, ARC (NSC 188491 is a recently characterized transcriptional inhibitor that selectively kills cancer cells and has the ability to perturb angiogenesis in vitro. In this study, the mechanism of action of ARC was further investigated by comparing in vitro and in vivo activity with other anti-neoplastic purines. Methods Structure-based homology searches were used to identify those compounds with similarity to ARC. Comparator compounds were then evaluated alongside ARC in the context of viability, cell cycle and apoptosis assays to establish any similarities. Following this, biological overlap was explored in detail using gene-expression analysis and kinase inhibition assays. Results Results demonstrated that sangivamycin, an extensively characterized pro-apoptotic nucleoside isolated from Streptomyces, had identical activity to ARC in terms of 1 cytotoxicity assays, 2 ability to induce a G2/M block, 3 inhibitory effects on RNA/DNA/protein synthesis, 4 transcriptomic response to treatment, 5 inhibition of protein kinase C, 6 inhibition of positive transcription elongation factor b (P-TEFb, 7 inhibition of VEGF secretion, and 8 activity within hollow fiber assays. Extending ARC activity to PKC inhibition provides a molecular basis for ARC cancer selectivity and anti-angiogenic effects. Furthermore, functional overlap between ARC and sangivamycin suggests that development of ARC may benefit from a retrospective of previous sangivamycin clinical trials. However, ARC was found to be inactive in several xenograft models, likely a consequence of rapid serum clearance. Conclusion Overall, these data expand on the biological properties of ARC but suggest additional studies are required before it can be considered a clinical trials candidate.

  5. An efficient synthesis of carbon-14 labelled vigabatrin

    Energy Technology Data Exchange (ETDEWEB)

    Gill, H.S. [Marion Merrell Dow Research Inst., Cincinnati, OH (United States)

    1995-12-31

    Vigabatrin-[6-{sup 14}C] ((R,S)-4-amino-5-hexenoic-[6-{sup 14}C] acid) was synthesized by employing Wittig condensation of 1-(1-butenyl) -2-oxo-5-pyrrolidinecarboxaldehyde with methyl-[{sup 14}C]-triphenyl-phosphonium iodide as the key step. The synthetic sequence involved 3 steps and produced the title compound in 70% overall yield with a radiochemical purity of 100%. (author).

  6. Effect of tolbutamide on 14C-sodium bicarbonate and 14C-alanine metabolism in isolated rat hepatocytes

    International Nuclear Information System (INIS)

    Kunjathoor, V.V.; Ye, Y.; Pillai, U.A.; Ferguson, P.W.; Medon, P.J.

    1990-01-01

    Tolbutamide (TOLB) is a sulfonylurea commonly used in the treatment of noninsulin-dependent diabetes mellitus. Studies have shown that TOLB affects gluconeogenesis and glycolysis from various substrates in the liver. Specifically, TOLB inhibits gluconeogenesis from lactate in a dose-dependent manner. In order to further clarify tolbutamide's mechanism of action, its effect on the incorporation of 14 C from NaH 14 CO 3 and 14 C-alanine into glucose, lactate or pyruvate in the presence of lactate was measured. Rat hepatocytes were incubated with lactate (2.0 mM) with or without TOLB (1.0 mM) in the presence of NaH 14 CO 3 or 14 C-alanine. TOLB inhibited the incorporation of C 14 from NaHCO 3 and alanine into glucose by 55 and 56%, respectively. TOLB did not alter the incorporation of C 14 from NaHCO 3 into lactate or pyruvate. TOLB did not affect the incorporation of 14 C from alanine into lactate but produced a pooling of 14 C as pyruvate. The authors data support studies demonstrating the TOLB produces its actions, in part, by increasing the concentration of fructose-2,6-bisphosphate and inhibiting pyruvate carboxylase

  7. Synthesis of 2-hydroxy-3-(2-methyl-propenyl-1,4-naphthoquinone and related oxime derivatives

    Directory of Open Access Journals (Sweden)

    Patricia S. Oliveira

    2012-06-01

    Full Text Available The condensation reaction of commercial 2-hydroxy-1 ,4-naphthoquinone 1 (lawsone with isobutyraldehyde 2 furnishs norlapachol 3 (2-hydroxy-3-(2-methyl-propenyl -1,4-naphthoquinone with yields ranging from 66 to 93% depending on the different conditions tested, and a reaction temperature factor determinant for the formation of the desired product. It was treated with hydroxylamine hydrochloride in alkaline (NaOH to provide the oxime 4 from regioselective modification of the carbonyl C-1 with 91% yield. The regioselectivity of the reaction can be explained by analyzing the different resonance structures which can be seen that the carbonyl C-4 is less electrophilic than C-1. In this work was also obtained the oxime 5, 6 and 7 from lapachol, αlpha and β-lapachone, respectively, in yields of 64-85%. The oximes of αlpha and β-norlapachone, 8 and 9 are in obtention. All the products were analyzed by IR and NMR, and were observed that oximes of lapachol and norlapachol are isolated as E/Z mixtures. Two-dimensional NOE-type experiments of the corresponding acylated derivative will be made to help identify the proportion of the mixture.

  8. Sources of C-14 generation and associated doses; Fuentes de generacion de C-14 y dosis asociadas

    Energy Technology Data Exchange (ETDEWEB)

    Amado, Valeria A; Biaggio, Alfredo L; Canoba, Analia C; Curti, Adriana R. [Autoridad Regulatoria Nuclear, Buenos Aires (Argentina)], E-mail: vamado@cae.arn.gov.ar

    2009-07-01

    C-14 is a radioactive isotope of C with a half-life of 5700 years that decays to N-14 by emission of beta radiation. It is naturally produced in the upper atmosphere by cosmic ray neutrons via the (n;p) reaction over N-14. Anthropogenic C-14 has been generated in the past by atmospheric nuclear weapon tests and it is currently produced during the operation of nuclear reactors. Once released this radionuclide behaves in the biosphere as the standard carbon cycle. Since the beginning of the industrial period the relationship Carbon-14/Stable Carbon has changed continuously, and so the dose incurred by the world population. In this paper the main anthropogenic activities that modified such relationship are presented and analyzed: the Suess effect and the generation of nuclear energy. It is concluded that the current trend of reduction of the total dose due to C-14 will continue during the next decades. Finally it is indicated that in order to prevent an excessive accumulation of this radionuclide in the biosphere, actions should be collectively implemented to be effective. (author) [Spanish] El C-14 es un isotopo radiactivo del C con un periodo de semidesintegracion igual a 5700 anios y que decae a N-14 por emision de radiacion beta. Se produce naturalmente en las altas capas de la atmosfera debido a la reaccion N-14(n,p)C-14 inducida por neutrones lentos de rayos cosmicos. El C-14 antropogenico se genero debido a los ensayos nucleares y actualmente es producido durante la operacion de los reactores nucleares. Una vez liberado se incorpora a la biosfera a traves del ciclo del carbono. A partir de los inicios del periodo industrial la relacion C-14/C-estable, y por ende la dosis debida a C-14 que recibiria la poblacion mundial, ha variado continuamente. El objetivo del presente trabajo es presentar y analizar los distintos factores antropogenicos que modifican la concentracion de C-14, en particular el efecto Suess y la generacion de energia nuclear. Se observa que las

  9. Preclinical and clinical evaluation of O-[{sup 11}C]methyl-L-tyrosine for tumor imaging by positron emission tomography

    Energy Technology Data Exchange (ETDEWEB)

    Ishiwata, Kiichi [Positron Medical Center, Tokyo Metropolitan Institute of Gerontology, Itabashi-ku, Tokyo 173-0022 (Japan)]. E-mail: ishiwata@pet.tmig.or.jp; Tsukada, Hideo [Central Research Laboratory, Hamamatsu Photonics K.K., Hamakita 434-8601 (Japan); Kubota, Kazuo [Department of Radiology, Division of Nuclear Medicine, International Medical Center of Japan, Shinjuku-ku, Tokyo 162-8655 (Japan); Nariai, Tadashi [Department of Neurosurgery, Tokyo Medical and Dental University, Bunkyo-ku, Tokyo 113-8519 (Japan); Harada, Norihiro [Department of Radiology, Division of Nuclear Medicine, International Medical Center of Japan, Shinjuku-ku, Tokyo 162-8655 (Japan); Kawamura, Kazunori [Positron Medical Center, Tokyo Metropolitan Institute of Gerontology, Itabashi-ku, Tokyo 173-0022 (Japan); SHI Accelerator Service Ltd., Shinagawa-ku, Tokyo 141-8686 (Japan); Kimura, Yuichi [Positron Medical Center, Tokyo Metropolitan Institute of Gerontology, Itabashi-ku, Tokyo 173-0022 (Japan); Oda, Keiichi [Positron Medical Center, Tokyo Metropolitan Institute of Gerontology, Itabashi-ku, Tokyo 173-0022 (Japan); Iwata, Ren [CYRIC, Tohoku University, Aoba-ku, Sendai 980-8578 (Japan); Ishii, Kenji [Positron Medical Center, Tokyo Metropolitan Institute of Gerontology, Itabashi-ku, Tokyo 173-0022 (Japan)

    2005-04-01

    We performed preclinical and clinical studies of O-[{sup 11}C]methyl-L-tyrosine, a potential tracer for imaging amino acid transport of tumors by positron emission tomography (PET). Examinations of the radiation-absorbed dose by O-[{sup 11}C]methyl-L-tyrosine and the acute toxicity and mutagenicity of O-methyl-L-tyrosine showed suitability of the tracer for clinical use. The whole-body imaging of monkeys and healthy humans by PET showed low uptake of O-[{sup 11}C]methyl-L-tyrosine in all normal organs except for the urinary track and bladder, suggesting that the O-[{sup 11}C]methyl-L-tyrosine PET has the potential for tumor imaging in the whole-body. Finally, the brain tumor imaging was preliminarily demonstrated.

  10. O6-alkylguanine-DNA alkyltransferase activity correlates with the therapeutic response of human rhabdomyosarcoma xenografts to 1-(2-chloroethyl)-3-(trans-4-methylcyclohexyl)-1-nitrosourea

    International Nuclear Information System (INIS)

    Brent, T.P.; Houghton, P.J.; Houghton, J.A.

    1985-01-01

    Immune-deprived female CBA/CaJ mice bearing xenografts of six different human rhabdomyosarcoma lines were treated with 1-(2-chloroethyl)-3-(trans-4-methylcyclohexyl)-1-nitrosourea (MeCCNU). Tumor responses were compared with levels of O 6 -methylguanine-DNA methyltransferase activity because of evidence indicating that repair of DNA interstrand cross-link precursors, mediated by the transferase, may be an important determinant of MeCCNU cytotoxicity. Levels of methyltransferase in tumor extracts were measured by determining the loss of O 6 -methylguanine from 3 H-labeled methylated DNA. Five of the six tumor lines examined showed either no response to MeCCNU or regrowth after an incomplete response. In each instance, the extent of tumor regression correlated with the level of O 6 -methylguanine-DNA methyltransferase activity in tumor extracts. These results suggest that O 6 -methylguanine-DNA methyltransferase levels in human tumor cells may be a clinically useful predictor of sensitivity to the chloroethylnitrosoureas

  11. Radiosynthesis and radiopharmacological evaluation of [N-methyl-11C]Org 34850 as a glucocorticoid receptor (GR)-binding radiotracer

    International Nuclear Information System (INIS)

    Wuest, Frank; Kniess, Torsten; Henry, Brian; Peeters, Bernardus W.M.M.; Wiegerinck, Peter H.G.; Pietzsch, Jens; Bergmann, Ralf

    2009-01-01

    The radiosynthesis of [N-methyl- 11 C]Org 34850 as a potential brain glucocorticoid receptor (GR)-binding radiotracer is described. The radiosynthesis was accomplished via N-methylation of the corresponding desmethyl precursor with [ 11 C]methyl triflate in a remotely controlled synthesis module to give the desired compound in a radiochemical yield of 23±5% (decay-corrected, based upon [ 11 C]CO 2 ) at a specific activity of 47±12 GBq/μmol (n=15) at the end-of-synthesis (EOS). The radiochemical purity after semi-preparative HPLC purification exceeded 95%. The total synthesis time was 35-40 min after end-of-bombardment (EOB). The radiotracer is rapidly metabolized in rat plasma leading to the formation of two more hydrophilic metabolites as the major metabolites. Radiopharmacological evaluation involving biodistribution and small animal PET imaging in normal Wistar rats showed that the compound [N-methyl- 11 C]Org 34850 is not able to sufficiently penetrate the blood-brain barrier. Therefore, compound [N-methyl- 11 C]Org 34850 seems not to be a suitable PET radiotracer for imaging rat brain GRs. However, involvement of Pgp or species differences requires further clarification to establish whether the radiotracer [N-methyl- 11 C]Org 34850 may still represent a suitable candidate for imaging GRs in humans

  12. Radiosynthesis and radiopharmacological evaluation of [N-methyl-11C]Org 34850 as a glucocorticoid receptor (GR)-binding radiotracer.

    Science.gov (United States)

    Wuest, Frank; Kniess, Torsten; Henry, Brian; Peeters, Bernardus W M M; Wiegerinck, Peter H G; Pietzsch, Jens; Bergmann, Ralf

    2009-02-01

    The radiosynthesis of [N-methyl-(11)C]Org 34850 as a potential brain glucocorticoid receptor (GR)-binding radiotracer is described. The radiosynthesis was accomplished via N-methylation of the corresponding desmethyl precursor with [(11)C]methyl triflate in a remotely controlled synthesis module to give the desired compound in a radiochemical yield of 23+/-5% (decay-corrected, based upon [(11)C]CO(2)) at a specific activity of 47+/-12 GBq/micromol (n=15) at the end-of-synthesis (EOS). The radiochemical purity after semi-preparative HPLC purification exceeded 95%. The total synthesis time was 35-40 min after end-of-bombardment (EOB). The radiotracer is rapidly metabolized in rat plasma leading to the formation of two more hydrophilic metabolites as the major metabolites. Radiopharmacological evaluation involving biodistribution and small animal PET imaging in normal Wistar rats showed that the compound [N-methyl-(11)C]Org 34850 is not able to sufficiently penetrate the blood-brain barrier. Therefore, compound [N-methyl-(11)C]Org 34850 seems not to be a suitable PET radiotracer for imaging rat brain GRs. However, involvement of Pgp or species differences requires further clarification to establish whether the radiotracer [N-methyl-(11)C]Org 34850 may still represent a suitable candidate for imaging GRs in humans.

  13. Crystal structure of (±-1-({[4-(allyloxyphenyl]sulfanyl}methyl-2-(diphenylthiophosphorylferrocene

    Directory of Open Access Journals (Sweden)

    Audric Michelot

    2015-08-01

    Full Text Available The title compound, [Fe(C5H5(C27H24OPS2], is built up from a ferrocene moiety substituted in the 1- and 2-positions by {[4-(allyloxyphenyl]sulfanyl}methyl and diphenylthiophosphoryl groups, respectively. The two S atoms lie on opposite sides of the cyclopentadienyl ring plane to which they are attached. In the crystal, C—H...S hydrogen bonds link the molecules into a ribbon running parallel to the (-110 plane. C—H...π interactions link the ribbons to form a three-dimensional network.

  14. Single-gap multi-harmonic buncher for NSC pelletron

    International Nuclear Information System (INIS)

    Sarkar, A.; Ghosh, S.; Barua, P.

    2001-01-01

    A single-gap multi-harmonic buncher, developed in collaboration with Argonne National Laboratory, has been installed in the pre-acceleration region of NSC Pelletron. This buncher is required for injecting bunched beam into the booster LINAC, presently under construction. A saw-tooth voltage generated across a single gap formed by a closely spaced pair of grids is used for bunching the dc ion beam produced by the Pelletron accelerator. This saw-tooth voltage is produced by adding a sine wave with its three higher harmonics in proper phase and amplitude. 28 Si beam has been bunched successfully using this buncher. The best FWHM of the bunched beam was 1.5 ns and the maximum efficiency of bunching was 50%. The bunching voltage had no steering effect on the beam. (author)

  15. Effect of oil refining processes on 14 C-tetrachlorvinphos residues in soya bean oil

    International Nuclear Information System (INIS)

    Farghaly, M.; Zayed, S.M.A.D.

    1986-01-01

    Crude soya bean oil extracted from grains treated with 14 C-tetrachlorvinphos and stored for 30 weeks was subjected to different refining processes. The effect of commercial refining processes, namely: alkali treatment, bleaching, winterization and deodorization on the nature and magnitude of the originally present residues was investigated. A high percentage (52%) of the residues was eliminated during alkali neutralization. No potentially toxic materials were detected among the identified degradation products. The obtained data showed that the ultimate degradation products were dimethyl phosphate and mono methyl phosphate.2 tab.,2 scheme

  16. Transfer of 14C to prenatal and neonatal rats from their mothers exposed to 14C compounds by ingestion

    International Nuclear Information System (INIS)

    Takeda, H.; Fuma, S.; Miyamoto, K.; Kuroda, N.; Inaba, J.

    2003-01-01

    The transfer of 14 C through placenta or milk was investigated and the radiation dose to fetal and newborn rats was estimated. Female rats at gestational stages or after delivery were exposed to 14 C in the form of sodium bicarbonate, thymidine and lysine by a single ingestion. Radioactivity in maternal tissues and conceptuses (placenta, fetal membrane and fetus) and in the newborn was determined at various times after ingestion. After exposure to these 14 C compounds, there was no significant difference between the 14 C concentration in the fetus and that in the maternal tissues, suggesting that the placenta has no effect in preventing or accelerating the placental transfer of 14 C. The concentration and content of 14 C in the fetus and newborn were, however, dependent on the chemical form of 14 C and on the prenatal or neonatal stage at the time of ingestion. The result of the dose estimation showed that 14 C-lysine gave significantly higher prenatal and neonatal doses than 14 C-sodium bicarbonate or 14 C-thymidine. (author)

  17. Analysis of loss of normal feedwater transient using RELAP5/MOD1/NSC; KNU1 plant simulation

    International Nuclear Information System (INIS)

    Kim, Hho Jung; Chung, Bub Dong; Lee, Young Jin; Kim, Jin Soo

    1986-01-01

    Simulation of the system thermal-hydraulic parameters was carried out following the KNU1(Korea Nuclear Unit-1) loss of normal feedwater transient sequence occurred on november 14, 1984. Results were compared with the plant transient data, and good agreements were obtained. Some deviations were found in the parameters such as the steam flowrate and the RCS(Reactor Coolant System) average temperature, around the time of reactor trip. It can be expected since the thermal-hydraulic parameters encounter rapid transitions due to the large reduction of the reactor thermal power in a short period of time and, thereby, the plant data involve transient uncertainties. The analysis was performed using the RELAP5/MOD1/NSC developed through some modifications of the interphase drag and the wall heat transfer modeling routines of the RELAP5/MOD1/CY018. (Author)

  18. 2-Bromo-2-methyl-N-p-tolylpropanamide

    Directory of Open Access Journals (Sweden)

    Rodolfo Moreno-Fuquen

    2011-06-01

    Full Text Available In the title molecule, C11H14BrNO, there is twist between the mean plane of the amide group and the benzene ring [C(=O—N—C...;C torsion angle = −31.2 (5°]. In the crystal, intermolecular N—H...O and weak C—H...O hydrogen bonds link molecules into chains along [100]. The methyl group H atoms are disordered over two sets of sites with equal occupancy.

  19. Kinetics and mechanism of polymerization of methyl methacrylate ...

    Indian Academy of Sciences (India)

    Homopolymerization of methyl methacrylate (MMA) was carried out in the presence of triphenylstibonium 1,2,3,4-tetraphenyl-cyclopentadienylide as an initiator in dioxane at 65°C ± 0·1°C. The system follows non-ideal radical kinetics ( ∝ [M]1.4 [I]0.44) due to primary radical termination as well as degradative ...

  20. SERS investigations on orientation of 2-bromo-3-methyl-1,4-dimethoxy-9,10-anthraquinone on silver nanoparticles.

    Science.gov (United States)

    Anuratha, M; Jawahar, A; Umadevi, M; Sathe, V G; Vanelle, P; Terme, T; Khoumeri, O; Meenakumari, V; Milton Franklin Benial, A

    2015-01-01

    Silver nanoparticles (Ag NPs) were prepared by solution combustion method with urea as fuel. Silver nanoparticles were characterized by UV-visible spectroscopy, X-ray diffraction (XRD) and scanning electron microscopy (SEM) techniques. Surface-enhanced Raman scattering (SERS) of 2-bromo-3-methyl-1,4-dimethoxy-9,10-anthraquinone (BMDMAQ) adsorbed on silver nanoparticles was investigated. The orientation of BMDMAQ on silver nanoparticles was inferred from nRs and SERS spectral features. Density functional theory (DFT) calculation was also performed to study the theoretical performance. The observed spectral features such as the high intensity of C-H out-of-plane bending mode and ring C-C stretching mode revealed that BMDMAQ adsorbed on silver surface through 'stand-on' orientation. Anthraquinone (AQ) derivatives have wide biomedical application which includes laxatives, antimalarials and antineoplastics used in the treatment of cancer. This present study would help to identify the interaction of drug molecules with DNA. Copyright © 2015 Elsevier B.V. All rights reserved.

  1. The Variation Analysis of DNA Methylation in Wheat Carrying Gametocidal Chromosome 3C from Aegilops triuncialis.

    Science.gov (United States)

    Wang, Dan; Zhao, Jieyu; Bai, Yan; Ao, You; Guo, Changhong

    2017-08-10

    Gametocidal (Gc) chromosomes can ensure their preferential transmission by killing the gametes without themselves through causing chromosome breakage and therefore have been exploited as an effective tool for genetic breeding. However, to date very little is known about the molecular mechanism of Gc action. In this study, we used methylation-sensitive amplified polymorphism (MSAP) technique to assess the extent and pattern of cytosine methylation alterations at the whole genome level between two lines of wheat Gc addition line and their common wheat parent. The results indicated that the overall levels of cytosine methylation of two studied Gc addition lines (CS-3C and CS-3C3C, 48.68% and 48.65%, respectively) were significantly increased when compared to common wheat CS (41.31%) and no matter fully methylated or hemimethylated rates enhanced in Gc addition lines. A set of 30 isolated fragments that showed different DNA methylation or demethylation patterns between the three lines were sequenced and the results indicated that 8 fragments showed significant homology to known sequences, of which three were homologous to MITE transposon (Miniature inverted-repeat transposable elements), LTR-retrotransposon WIS-1p and retrotransposon Gypsy , respectively. Overall, our results showed that DNA methylation could play a role in the Gc action.

  2. The Variation Analysis of DNA Methylation in Wheat Carrying Gametocidal Chromosome 3C from Aegilops triuncialis

    Directory of Open Access Journals (Sweden)

    Dan Wang

    2017-08-01

    Full Text Available Gametocidal (Gc chromosomes can ensure their preferential transmission by killing the gametes without themselves through causing chromosome breakage and therefore have been exploited as an effective tool for genetic breeding. However, to date very little is known about the molecular mechanism of Gc action. In this study, we used methylation-sensitive amplified polymorphism (MSAP technique to assess the extent and pattern of cytosine methylation alterations at the whole genome level between two lines of wheat Gc addition line and their common wheat parent. The results indicated that the overall levels of cytosine methylation of two studied Gc addition lines (CS–3C and CS–3C3C, 48.68% and 48.65%, respectively were significantly increased when compared to common wheat CS (41.31% and no matter fully methylated or hemimethylated rates enhanced in Gc addition lines. A set of 30 isolated fragments that showed different DNA methylation or demethylation patterns between the three lines were sequenced and the results indicated that 8 fragments showed significant homology to known sequences, of which three were homologous to MITE transposon (Miniature inverted–repeat transposable elements, LTR-retrotransposon WIS-1p and retrotransposon Gypsy, respectively. Overall, our results showed that DNA methylation could play a role in the Gc action.

  3. Metabolism of aspirin and procaine in mice pretreated with O-4-nitrophenyl methyl(phenyl)phosphinate or O-4-nitrophenyl diphenylphosphinate

    International Nuclear Information System (INIS)

    Joly, J.M.; Brown, T.M.

    1986-01-01

    Concentrations of [carboxyl- 14 C]procaine in blood of mice were increased threefold for 27 min by exposure to O-4-nitrophenyl diphenylphosphinate 2 hr prior to [carboxyl- 14 C]procaine injection ip, while there was no effect of O-4-nitrophenyl methyl(phenyl)phosphinate pretreatment. There was no effect of either organophosphinate on the primary hydrolysis of [acetyl-l- 14 C]aspirin when assessed by the expiration of [ 14 C]carbon dioxide; however, O-4-nitrophenyl diphenylphosphinate pretreatment produced transient increases in blood concentrations of both [carboxyl- 14 C]aspirin and [carboxyl- 14 C]salicylic acid following administration of [carboxyl- 14 C]aspirin. Liver carboxylesterase activity in O-4-nitrophenyl diphenylphosphinate pretreated mice was 11% of control activity. These results indicate the potential for drug interaction with O-4-nitrophenyl diphenylphosphinate but not with O-4-nitrophenyl methyl(phenyl)phosphinate. It appears that liver carboxylesterase activity has a minor role in hydrolysis of aspirin in vivo, but may be more important in procaine metabolism

  4. Effect of trimethylcolchicinic acid methyl ether d-tartrate (TMCA) on Hodgkin's and non-Hodgkin's lymphoma.

    Science.gov (United States)

    Stolinsky, D C; Jacobs, E M; Irwin, L E; Pajak, T F; Bateman, J R

    1976-01-01

    Trimethylcolchicinic acid methyl ether d-tartrate (TMCA; NSC-36351) was administered daily by mouth to 71 patients with malignant lymphomas. Partical (greater than 50%) responses were observed in eleven of 37 patients with Hodgkin's disesse, two of 22 patients with lymphocytic lymphoma, and one of two patients with mixed cell lymphoma. One complete and three partial responses were noted in nine patients with histiocytic lymphoma. Responses lasted from one to 91+ months (median: four months) and occurred in patients whose disease was resistant to alkylating agents, vinblastine, vincristine, procarbazine, prednisone or BCNU. Toxic effects included leukopenia, thrombocytopenia, nausea, diarrhea, stomatitis, alopecia and dermatitis.

  5. Comparison of the gravimetric, phenol red, and 14C-PEG-3350 methods to determine water absorption in the rat single-pass intestinal perfusion model

    OpenAIRE

    Sutton, Steven C.; Rinaldi, M. T. S.; Vukovinsky, K. E.

    2001-01-01

    This study was undertaken to determine whether the gravimetric method provided an accurate measure of water flux correction and to compare the gravimetric method with methods that employ nonabsorbed markers (eg, phenol red and 14C-PEG-3350). Phenol red, 14C-PEG-3350, and 4-[2-[[2-(6-amino-3-pyridinyl)-2-hydroxyethyl]amino]ethoxy]-methyl ester, (R)-benzene acetic acid (Compound I) were co-perfused in situ through the jejunum of 9 anesthetized rats (single-pass intestinal perfusion [SPIP]). Wat...

  6. Influence of a carbamate pesticide on growth, respiration (/sup 14/C)-carbon metabolism and symbiosis of a Rhizobium sp

    Energy Technology Data Exchange (ETDEWEB)

    Sekar, T; Balasubramanian, A [Tamil Nadu Agricultural Univ., Coimbatore (India)

    1979-04-01

    Addition of aldicarb (2 methyl-2(methyl thio) propionaldehyde-O-methyl carbamoyl oxime) in the growth medium enhanced the growth of Rhizobium sp. (cowpea group) at 2ppm level while an inhibition was observed at the normal (5 ppm) and higher (10 ppm) concentrations. Respiration of the cells was also inhibited by 5 and 10 ppm levels of the chemical eventhough a stimulation was observed at 2 ppm (lower) concentration. The insecticide, when incorporated at 5 and 10 ppm levels in the medium increased the /sup 14/C-glucose incorporation and considerably altered the assimilation of the radioactive carbon in different fractions of rhizobium cells. Soil application of this insecticide (Temik 10 G) reduced the number of nodules formed and the total nitrogen content in cowpea plants inoculated with the Rhizobium sp. but enhanced the dry matter production of cowpea plants.

  7. Root-uptake of {sup 14}C derived from acetic acid and {sup 14}C transfer to rice edible parts

    Energy Technology Data Exchange (ETDEWEB)

    Ogiyama, Shinichi [Office of Biospheric Assessment for Waste Disposal, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba-shi 263-8555 (Japan)], E-mail: ogiyama@nirs.go.jp; Suzuki, Hiroyuki [Graduate School of Pharmaceutical Sciences, Chiba University, 1-33 Yayoi-cho, Inage-ku, Chiba-shi 263-5522 (Japan); Inubushi, Kazuyuki [Graduate School of Horticulture, Chiba University, 648 Matsudo, Matsudo-shi 271-8510 (Japan); Takeda, Hiroshi; Uchida, Shigeo [Office of Biospheric Assessment for Waste Disposal, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba-shi 263-8555 (Japan)

    2010-02-15

    Three types of culture experiments using paddy rice (Oryza sativa L.) were performed to examine root-uptake of {sup 14}C in the form of acetic acid: double pot experiment (hydroponics), wet culture experiment (submerged sand medium), and chamber experiment (hydroponics and submerged sand medium). The {sup 14}C radioactivity in the plant, mediums, and atmospheric carbon dioxide ({sup 14}CO{sub 2}) in the chamber were determined, and the distribution of {sup 14}C in the plant was visualized using autoradiography. In the double pot experiment, the shoot of the plant and the lower root which was soaked in the culture solution had {sup 14}C radioactivity, but the upper root which did not have contact with the solution had none. There were also {sup 14}C radioactivity in the grains and roots in the wet culture experiment. Results of the chamber experiment showed that {sup 14}CO{sub 2} gas was released from the culture solution in both types of cultures. Results indicated that the {sup 14}C-acetic acid absorbed by rice plant through its root would be very small. Most of the {sup 14}C-acetic acid was transformed into gaseous forms either in the culture solution or rhizosphere. A relatively longer time would be needed to assimilate {sup 14}C derived from acetic acid to grain parts after it was once absorbed by the shoot through the root. Availability of {sup 14}C for the plant in sand culture was considered to be decreased compared with that for the plant in the hydroponics experiment. It was suggested that rice plant absorbed and assimilated {sup 14}C through the plant roots not because of uptake of {sup 14}C-acetic acid but because of uptake of {sup 14}C in gaseous forms such as {sup 14}CO{sub 2}.

  8. Method of preparing D-mannose(U-14C) from glucons(U-14C) separated from natural material

    International Nuclear Information System (INIS)

    Kucar, S.; Zemek, J.; Bilik, V.; Kolina, J.

    1981-01-01

    Glucans(U- 14 C) separated from green or blue-green algae are hydrolysed using diluted mineral acids in the presence of small amounts of molybdate ions to D-glucose(U- 14 C) which, at a temperature of 60 to 100 degC epimerizes to D-mannose(U- 14 C). The epimeric aldoses are separated from the reaction mixture by paper chromatography. (H.S.)

  9. Selective labelling of apolipoproteins A-I and C-I at methionine residues by (TH) methyl exchange

    Energy Technology Data Exchange (ETDEWEB)

    Hancock, W.S.; Harding, D.R.K.; Barling, P.M.; Sparrow, J.T.

    1985-01-01

    Apolipoproteins C-I and A-I were radioactively labelled with tritium by (TH)-methyl exchange. The methionine residues were first methylated with (TH)-methyl iodide at pH4 and the reaction products were purified by gel filtration and cation exchange chromatography. The products were then demethylated with 2-mercaptoethanol (6 M) at pH 8.6 to regenerate the apolipoproteins in an unmodified but tritiated form. The specific radioactivity for apolipoprotein C-I and A-I was 3.5 x 10W and 1.5 x 10X dpm/pmol respectively. The properties of (TH)-apolipoprotein C-I were examined by reversed phase HPLC and by incorporation into very low density lipoproteins (VLDL).

  10. Micro-syntheses for the use of carbon 13 or carbon 14. Micro-preparations of methyl alcohol, methyl iodide, and sodium acetate labeled in the methyl group

    International Nuclear Information System (INIS)

    Baret, C.; Pichat, L.

    1951-11-01

    Apparatus and technique are described in detail for (1) reduction of CO 2 to CH 3 OH with LiAlH 4 , (2) conversion of the methanol to CH 3 I by HI, (3) formation of the Mg Grignard reagent, and (4) addition of inactive CO 2 to form CH 3 COOH. All these operations have been carried out on 0.005 moles. Methyl-labeled Na acetate has been prepared in 67% yield based on the Ba 14 CO 3 used as starting material. (author) [fr

  11. Intramolecular Nicholas reactions in the synthesis of dibenzocycloheptanes. Synthesis of allocolchicine NSC 51046 and analogues and the formal synthesis of (-)-allocolchicine.

    Science.gov (United States)

    Djurdjevic, Sinisa; Yang, Fei; Green, James R

    2010-12-03

    The preparation of dibenzocycloheptyne-Co(2)(CO)(6) complexes by intramolecular Nicholas reactions of biaryl-2-propargyl alcohol-Co(2)(CO)(6) derivatives is described. Reductive decomplexation of the dibenzocycloheptyne-Co(2)(CO)(6) complexes affords the corresponding dibenzocycloheptenes, individual members of which have been employed in a formal total synthesis of (-)-allocolchicine, the preparation of 6,7-dihydro-3,4,9,10,11-pentamethoxy-5H-dibenzo[a,c]cyclohepten-5-one, and the enantioselective total syntheses of NSC 51046 and its 3,8,9,10-tetramethoxy regioisomer.

  12. 14C Records from Indonesian Sea

    International Nuclear Information System (INIS)

    Baresic, J.; Fallon, S.; Mazerat, J.

    2013-01-01

    To investigate ocean currents and past climate events affecting the Indonesian throughflow (ITF), a radiocarbon record from a Porites coral collected from Alor Island, Indonesia, was constructed. Porites corals are often used in paleoclimate research and water mass circulation studies in the Tropics because of their abundance in the region and growth rate of 8 - 20 mm/y. These characteristics allow reconstructions of past environmental changes on weekly to annual time scales. At this point radiocarbon coral results from Alor cover approximately 30 years. An age model was constructed using the sea surface temperature proxy δ18O. Alor radiocarbon results were compared with previous measurements obtained from Padang and Langkai corals. a14C values obtained from the Alor coral display a strong seasonal cycle, high values during Australian summer and low values during Australian winter. Higher a 14C summer values indicate inflow of waters enriched by 14C through Makassar Strait from the North Pacific Ocean and Java Sea surface water. Summer a14C values are also enhanced by summer stratification. Winter values indicate upwelling of deep Ocean waters within the research area and transport of 14C-depleted waters from the Banda Sea, which has input from the South Pacific Ocean (lower a14C than North Pacific). Therefore, the a14C coral record reflects the movement of enriched water from North Pacific to Indian Ocean through Makassar Strait during summer and upwelling of depleted surface waters from the Banda Sea during the winter. Lower a14C dips could be attributed to strong El Nino events, which would enhance surface water mixing and upwelling of low radiocarbon deep waters. Water transport from North Pacific Ocean decreases during El Nino events also contributing to lowering of a14C signal.(author)

  13. Influence of agronomic amendments on the fate of bound methyl parathion residues in soils

    International Nuclear Information System (INIS)

    Gerstl, Z.; Helling, C.S.

    1984-01-01

    The fate of [ring- 14 C] methyl parathion in a silt loam soil was monitored during a 49-day incubation period. At this point, 54% of the initial 14 C remained in the soil; of this, 13% was extractable with MeOH and 87% was bound residue. Soils were then treated with inorganic and organic amendments and incubated an additional 70 days. Release of methyl parathion bound residues could not be demonstrated, but mineralization of both bound and extractable 14 C to 14 CO 2 was seen. Slow, continuous production of CO 2 , all at comparable rates, occurred with the controls and with amendments H 2 SO 4 , (NH 4 ) 2 SO 4 , NH 4 OH, chitin, oat seedlings, and oat straw. Glucose and asparagine caused high rates of 14 CO 2 production. HgCl 2 gave very high initial rates of 14 CO 2 loss; the rate declined to that of the control only after 9-10 weeks. The lime treatment exceeded the controls after 1 week, declining only slightly with time. The effects of sewage sludge and dairy manure were similar to the controls except that: (a) sludge caused a very high initial loss of 14 CO 2 , and (b) both treatments gave an unaccountable loss of 14 C, perhaps as 14 CH 4 from anaerobic conditions. By 70 days, levels of extractable 14 C and bound 14 C had both declined twice as rapidly in certain amended soils as in unamended controls. (author)

  14. Third Conference on nonlinear science and complexity (NSC)

    CERN Document Server

    Machado, José; Baleanu, Dumitru; Dynamical Systems and Methods

    2012-01-01

    Nonlinear Systems and Methods For Mechanical, Electrical and Biosystems presents topics observed at the 3rd Conference on Nonlinear Science and Complexity(NSC), focusing on energy transfer and synchronization in hybrid nonlinear systems. The studies focus on fundamental theories and principles,analytical and symbolic approaches, computational techniques in nonlinear physical science and mathematics. Broken into three parts, the text covers:\\ Parametrical excited pendulum, nonlinear dynamics in hybrid systems, dynamical system synchronization and (N+1) body dynamics as well as new views different from the existing results in nonlinear dynamics. Mathematical methods for dynamical systems including conservation laws, dynamical symmetry in nonlinear differential equations and invex energies. Nonlinear phenomena in physical problems such as solutions, complex flows, chemical kinetics, Toda lattices and parallel manipulator. This book is useful to scholars, researchers and advanced technical members of industrial l...

  15. Synthesis of ethanol {sup 14}C-1; Synthese d'ethanol {sup 14}C-1

    Energy Technology Data Exchange (ETDEWEB)

    Wolff, R E; Pichat, L [Commissariat a l' Energie Atomique, Saclay (France). Centre d' Etudes Nucleaires

    1958-07-01

    The direct reduction by LiAlH{sub 4}, of a suspension of anhydrous sodium acetate in tetra-hydro-furfuryl-oxy-tetra-hydro-pyran is described. This study has shown that the ethanol thus obtained is impure and that the yields are erratic. On the contrary the reduction of acetyl chloride 1-{sup 14}C by LiAlH{sub 4}, in 'diethyl carbitol' leads to ethanol 1-{sup 14}C of satisfactory purity with a yield of about 71 percent. (author) [French] Une etude de la reduction directe par LiAlH{sub 4}, de l'acetate de soude anhydre en suspension dans le tetrahydrofurfuryloxytetrahydropyrane est decrite. Cette etude a montre que l'on obtient de l'ethanol souille d'impuretes, avec un rendement variable. Par contre, la reduction du chlorure d'acetyle {sup 14}C-1 par LiAlH{sub 4}, dans le 'diethyl carbitol' conduit a l'ethanol {sup 14}C-1 de purete convenable avec un rendement de l'ordre de 71 pour cent. (auteur)

  16. Simple automated preparation of O-[{sup 11}C]methyl-L-tyrosine for routine clinical use

    Energy Technology Data Exchange (ETDEWEB)

    Ishikawa, Yoichi [CYRIC Tohoku University, Aramaki, Aoba-ku, Sendai 980-8578 (Japan); Iwata, Ren [CYRIC Tohoku University, Aramaki, Aoba-ku, Sendai 980-8578 (Japan)]. E-mail: rencyric@cyric.tohoku.ac.jp; Furumoto, Shozo [TUBERO, Tohoku University, Sendai 980-8575 (Japan); Pascali, Claudio [National Cancer Institute, 20133 Milan (Italy); Bogni, Anna [National Cancer Institute, 20133 Milan (Italy); Kubota, Kazuo [International Medical Center, Tokyo 162-8655 (Japan); Ishiwata, Kiichi [Tokyo Metropolitan Institute of Gerontology, Tokyo 173-0022 (Japan)

    2005-07-01

    The previously reported preparation of O-[{sup 11}C]methyl-L-tyrosine ([{sup 11}C]MT), a promising tumor imaging agent, has been now considerably simplified and automated. Main changes were the use of [{sup 11}C]methyl iodide ([{sup 11}C]MeI) in the reaction with L-tyrosine disodium and the use of solid phase extraction on commercially available cartridges instead of HPLC for the final purification. An injectable saline solution of [{sup 11}C]MT was obtained within 30 min after EOB with radiochemical yield of ca. 60% (decay-corrected, based on [{sup 11}C]MeI). Radiochemical purity was over 97%. The automated preparation was carried out using a miniature module employing manifold valves.

  17. Intrinsic solubility estimation and pH-solubility behavior of cosalane (NSC 658586), an extremely hydrophobic diprotic acid.

    Science.gov (United States)

    Venkatesh, S; Li, J; Xu, Y; Vishnuvajjala, R; Anderson, B D

    1996-10-01

    The selection of cosalane (NSC 658586) by the National Cancer Institute for further development as a potential drug candidate for the treatment of AIDS led to the exploration of the solubility behavior of this extremely hydrophobic drug, which has an intrinsic solubility (S0 approaching 1 ng/ml. This study describes attempts to reliably measure the intrinsic solubility of cosalane and examine its pH-solubility behavior. S0 was estimated by 5 different strategies: (a) direct determination in an aqueous suspension: (b) facilitated dissolution; (c) estimation from the octanol/water partition coefficient and octanol solubility (d) application of an empirical equation based on melting point and partition coefficient; and (e) estimation from the hydrocarbon solubility and functional group contributions for transfer from hydrocarbon to water. S0 estimates using these five methods varied over a 5 x 107-fold range Method (a) yielded the highest values, two-orders of magnitude greater than those obtained by method (b) (facilitated dissolution. 1.4 +/- 0.5 ng/ml). Method (c) gave a value 20-fold higher while that from method (d) was in fair agreement with that from facilitated dissolution. Method (e) yielded a value several orders-of-magnitude lower than other methods. A molecular dynamics simulation suggests that folded conformations not accounted for by group contributions may reduce cosalane's effective hydrophobicity. Ionic equilibria calculations for this weak diprotic acid suggested a 100-fold increase in solubility per pH unit increase. The pH-solubility profile of cosalane at 25 degrees C agreed closely with theory. These studies highlight the difficulty in determining solubility of very poorly soluble compounds and the possible advantage of the facilitated dissolution method. The diprotic nature of cosalane enabled a solubility enhancement of > 107-fold by simple pH adjustment.

  18. The C-household of young broad-leaved and conifer tree species exposed to long-term carbon limitation by shading

    Science.gov (United States)

    Weber, Raphael; Hoch, Günter

    2017-04-01

    Non-structural carbohydrates (NSC, i.e. free sugars and starch) are regarded as freely available carbon (C) reserves in plants. They are often quantified to estimate a plant's C-balance, assuming that NSC are controlled by the net-balance between photo-assimilation and C-usage (respiration, growth and other sinks). Within a recent field experiment, we investigated the extent, to which C-reserves (NSC) can be formed in young trees against prevailing C-sink demands (growth) under C-limitation. A total of almost 1000 individuals of two-year-old tree saplings from 6 deciduous, broadleaved species and 4 evergreen conifer species were planted on a field side. Half of the trees per species were treated with long-term C-limitation by exposing them to continuous deep shade conditions (5% of natural PPFD) under a permanent shading tent. C gas-exchange, growth and NSC tissue concentrations were analyzed in shaded and unshaded saplings for two consecutive years. Three months after the beginning of the experiment, leaf photosynthesis acclimatized to the low light conditions, with leaves of shaded trees showing significantly higher SLA and lower light saturation and maximum photosynthesis. During the second season of the experiment, most species exhibited very strong reductions in NSC, but much less pronounced reductions in growth. In contrast, other species, with few exceptions, kept NSC concentrations similar to unshaded controls, while growth virtually stopped under deep shade. In conclusion, we found species-specific strategies in the trees' C-household after two years of C-limitation, that fall into two major carbon allocation strategies: 1) "C-spenders", which deplete C reserves in order to keep up significant growth, and 2) "C-savers", which reduce C sink activities to a minimum in order to store substantial amounts of C reserves. Overall, early-successional species tended to follow the first strategy, while late-successional species tended to save higher C reserve pools

  19. Identifying Glucokinase Monogenic Diabetes in a Multiethnic Gestational Diabetes Mellitus Cohort: New Pregnancy Screening Criteria and Utility of HbA1c.

    Science.gov (United States)

    Rudland, Victoria L; Hinchcliffe, Marcus; Pinner, Jason; Cole, Stuart; Mercorella, Belinda; Molyneaux, Lynda; Constantino, Maria; Yue, Dennis K; Ross, Glynis P; Wong, Jencia

    2016-01-01

    Glucokinase monogenic diabetes (GCK-maturity-onset diabetes of the young [MODY]) should be differentiated from gestational diabetes mellitus (GDM) because management differs. New pregnancy-specific screening criteria (NSC) have been proposed to identify women who warrant GCK genetic testing. We tested NSC and HbA1c in a multiethnic GDM cohort and examined projected referrals for GCK testing. Using a GDM database, 63 of 776 women had a postpartum oral glucose tolerance test suggestive of GCK-MODY. Of these 63 women, 31 agreed to undergo GCK testing. NSC accuracy and HbA1c were examined. Projected referrals were calculated by applying the NSC to a larger GDM database (n = 4,415). Four of 31 women were confirmed as having GCK-MODY (prevalence ∼0.5-1/100 with GDM). The NSC identified all Anglo-Celtic women but did not identify one Indian woman. The NSC will refer 6.1% of GDM cases for GCK testing, with more Asian/Indian women referred despite lower disease prevalence. Antepartum HbA1c was not higher in those with GCK-MODY. The NSC performed well in Anglo-Celtic women. Ethnic-specific criteria should be explored. © 2016 by the American Diabetes Association. Readers may use this article as long as the work is properly cited, the use is educational and not for profit, and the work is not altered.

  20. Characterization of a distonic isomer C6H5C+(OH)OCH2 of methyl benzoate radical cation by associative ion-molecule reactions

    Science.gov (United States)

    Dechamps, Noémie; Flammang, Robert; Gerbaux, Pascal; Nam, Pham-Cam; Nguyen, Minh Tho

    2006-03-01

    The C6H5C+(OH)OCH2 radical cation, formally a distonic isomer of ionized methyl benzoate, has been prepared by dissociative ionization of neopentyl benzoate, as earlier suggested by Audier et al. [H.E. Audier, A. Milliet, G. Sozzi, S. Hammerum, Org. Mass. Spectrom. 25 (1990) 44]. Its distonic character has now been firmly established by its high reactivity towards neutral methyl isocyanide (ionized methylene transfer) producing N-methyl ketenimine ions. Other mass spectrometric experiments and ab initio quantum chemical calculations also concur with each other pointing toward the existence of a stable distonic radical cation.

  1. Neurotoxic injury pathways in differentiated mouse motor neuron–neuroblastoma hybrid (NSC-34D) cells in vitro—Limited effect of riluzole on thapsigargin, but not staurosporine, hydrogen peroxide and homocysteine neurotoxicity

    Energy Technology Data Exchange (ETDEWEB)

    Hemendinger, Richelle A., E-mail: richelle.hemendinger@carolinashealthcare.org [ALS Translational Neuroscience Laboratory, Carolinas Medical Center, Charlotte, NC 28203 (United States); Carolinas Neuromuscular/ALS-MDA Center, Department of Neurology, Carolinas Medical Center, Charlotte, NC 28203 (United States); Armstrong, Edward J. [ALS Translational Neuroscience Laboratory, Carolinas Medical Center, Charlotte, NC 28203 (United States); Carolinas Neuromuscular/ALS-MDA Center, Department of Neurology, Carolinas Medical Center, Charlotte, NC 28203 (United States); Radio, Nick [ThermoScientific, Pittsburgh, PA (United States); Brooks, Benjamin Rix [ALS Translational Neuroscience Laboratory, Carolinas Medical Center, Charlotte, NC 28203 (United States); Carolinas Neuromuscular/ALS-MDA Center, Department of Neurology, Carolinas Medical Center, Charlotte, NC 28203 (United States); University of North Carolina School of Medicine-Charlotte Campus (United States)

    2012-01-15

    The neuroblastoma–spinal motor neuron fusion cell line, NSC-34, in its differentiated form, NSC-34D, permits examining the effects of riluzole, a proven treatment for amyotrophic lateral sclerosis (ALS) on cell death induction by staurosporine (STS), thapsigargin (Thaps), hydrogen peroxide (H{sub 2}O{sub 2}) and homocysteine (HCy). These neurotoxins, applied exogenously, have mechanisms of action related to the various proposed molecular pathogenetic pathways in ALS and are differentiated from endogenous cell death that is associated with cytoplasmic aggregate formation in motor neurons. Nuclear morphology, caspase-3/7 activation and high content imaging were used to assess toxicity of these neurotoxins with and without co-treatment with riluzole, a benzothiazole compound with multiple pharmacological actions. STS was the most potent neurotoxin at killing NSC-34D cells with a toxic concentration at which 50% of maximal cell death is achieved (TC{sub 50} = 0.01 μM), followed by Thaps (TC{sub 50} = 0.9 μM) and H{sub 2}O{sub 2} (TC{sub 50} = 15 μM) with HCy requiring higher concentrations to kill at the same level (TC{sub 50} = 2200 μM). Riluzole provided neurorescue with a 20% absolute reduction (47.6% relative reduction) in apoptotic cell death against Thaps-induced NSC-34D cell (p ≤ 0.05), but had no effect on STS-, H{sub 2}O{sub 2}- and HCy-induced NSC-34D cell death. This effect of riluzole on Thaps induction of cell death was independent of caspase-3/7 activation. Riluzole mitigated a toxin that can cause intracellular calcium dysregulation associated with endoplasmic reticulum (ER) stress but not toxins associated with other cell death mechanisms. -- Highlights: ► Calcium-dependent neurotoxins are potent cell death inducers in NSC-34D cells. ► Riluzole provides neurorescue against Thaps-induced NSC-34D cell death. ► Riluzole had no effect on neurotoxicity by STS, H{sub 2}O{sub 2} and Hcy. ► Riluzole reduces NSC-34D cell death independent of

  2. S-adenosyl-L-(l-14C)-homocysteine

    International Nuclear Information System (INIS)

    Thomas, H.J.; Montgomery, J.A.

    1987-01-01

    S-Adenosyl-L-(1- 14 C)-homocysteine was prepared from commercially available L-(1- 14 C)-methionine by conversion first to S-benzyl-L-(1- 14 C)-homocysteine which upon treatment with sodium in liquid ammonia gave the disodium salt of L-(1- 14 C)-homocysteine. Reaction of this sodium salt with 5'-O-tosyladenosine gave the title compound. (author)

  3. Synthesis of /sup 14/C-labeled felbamate from phenylacetic-(methylene-/sup 14/C) acid

    Energy Technology Data Exchange (ETDEWEB)

    Choi, Y.M.; Kucharczyk, N.; Sofia, R.D.

    1986-05-01

    A synthetic procedure for the preparation of 2-phenyl-1,3-propanediol-2-/sup 14/C dicarbamate, starting with phenylacetic-(methylene-/sup 14/C) acid was developed. The procedure from phenylacetic acid to 2-phenyl-1,3-propanediol dicarbamate has four steps via phenylmalonic acid and 2-phenyl-1,3-propanediol. The overall yield of all four steps was 28%.

  4. Microbiology and biogeochemistry of sediments and rhizosphere of mangroves: bacterial production, sulphate-reduction and methylation of mercury with methodological focus on incubation-extraction of {sup 14}C-leucine; Microbiologia e biogeoquimica de sedimentos e rizosfera de manguezais: producao bacteriana, sulfato-reducao e metilacao do mercurio com enfoque metodologico na incubacao-extracao de {sup 14}C-leucina

    Energy Technology Data Exchange (ETDEWEB)

    Feijo, Issabella Vitoria Abduche

    2015-07-01

    Mangroves are one of the most important ecosystems when it comes to cycling of various elements, including carbon and mercury. Microbiological processes that occur in sediment are essential for carbon mineralization, its conversion into biomass and for availability of mercury to the food chain. Sulfate-reducing bacteria are one of the main groups responsible for degradation of organic compounds in marine sediments and mercury methylation, especially in the rhizosphere of macrophyte. The aim of this study was to evaluate bacterial production (BP) over different sedimentary profiles as well as mercury methylation (% MeHg), sulfate reduction rates (SRR) and bacterial production in the rhizosphere of a ubiquitous mangrove tree. Radiochemical approaches were used to access bacterial production ({sup 14}C-leucine), sulfate reduction ({sup 35}SO{sub 4}) and mercury methylation ({sup 203}Hg). Study area was located at Coroa Grande (Sepetiba bay) and Jequia mangrove (Guanabara bay). Methodological studies using {sup 14}C-leucine as a tool to assess bacterial production in mangrove sediment were not found. In this context, we tested two leucine uptake methodologies for measuring bacterial production in mangrove sediments according to Baath et al. (2001) Soil Biol. Biochem., v.33,p. 1571-1574 and Fischer and Pusch (1999) Appl. Environ. Microbiol., v.6, p.4411-4418. Our results suggest that an adaptation of both techniques were suitable to measure BP in mangrove sediment. We also provided underlying parameters of the method such as saturation level and linearity of leucine incorporation that can be used as guidance for future studies in mangrove. Once the methodology was established, we accessed BP along a shallow sedimentary profile in three physiographic mangroves types: basin, fringe and riverine. BP was highly heterogeneous in different physiographic types of mangroves and along the sediment profiles.The mangrove located at Guanabara bay presented BP which was 50 times

  5. PPARs Expression in Adult Mouse Neural Stem Cells: Modulation of PPARs during Astroglial Differentiaton of NSC

    Directory of Open Access Journals (Sweden)

    A. Cimini

    2007-01-01

    Full Text Available PPAR isotypes are involved in the regulation of cell proliferation, death, and differentiation, with different roles and mechanisms depending on the specific isotype and ligand and on the differentiated, undifferentiated, or transformed status of the cell. Differentiation stimuli are integrated by key transcription factors which regulate specific sets of specialized genes to allow proliferative cells to exit the cell cycle and acquire specialized functions. The main differentiation programs known to be controlled by PPARs both during development and in the adult are placental differentiation, adipogenesis, osteoblast differentiation, skin differentiation, and gut differentiation. PPARs may also be involved in the differentiation of macrophages, brain, and breast. However, their functions in this cell type and organs still awaits further elucidation. PPARs may be involved in cell proliferation and differentiation processes of neural stem cells (NSC. To this aim, in this work the expression of the three PPAR isotypes and RXRs in NSC has been investigated.

  6. Isozyme-specific enzyme inhibitors. 14. 5'(R)-C-[(L-homocystein-S-yl)methyl]adenosine 5'-(beta,gamma-imidotriphosphate), a potent inhibitor of rat methionine adenosyltransferases.

    Science.gov (United States)

    Kappler, F; Vrudhula, V M; Hampton, A

    1987-09-01

    The title compound is a covalent adduct of L-methionine (Met) and beta,gamma-imido-ATP. In its synthesis the N-Boc derivative of 5'(R)-C-(aminomethyl)-N6-benzoyl-5'-O-tosyl-2',3'-O- isopropylidenadenosine was converted by the successive actions of CF3CO2H and HNO2 into the corresponding 5'(R)-C-hydroxymethyl derivative. Treatment of this with disodium L-homocysteinate led to attack of sulfur at C6', apparently via a 5',6'-epoxide, and to total stereoselective inversion at C5' to furnish, after debenzoylation, 5'(R)-C-(L-homocystein-S-ylmethyl)-2',3'-O-isopropylidene ade nosine. The 5' configuration was established by conversion of this into the known 5'(S)-C-methyl-2',3'-O-isopropylidene adenosine with Raney nickel. The alpha-amino acid residue was protected as an N-Boc methyl ester, after which the 5'-hydroxyl was phosphorylated with benzyl phosphate and dicyclohexylcarbodiimide. The phosphoanhydride bond with inorganic imidodiphosphate was then created by established methods. Finally, blocking groups were removed under conditions that gave the desired adduct with no racemization of its L-methionine residue. It was a potent inhibitor [KM(ATP)/Ki = 1080; KM(Met)/Ki = 7.7] of the M-2 (normal tissue) form of rat methionine adenosyltransferase and of the M-T (hepatoma tissue) form [KM(ATP)/Ki = 670; KM(Met)/Ki = 22]. Inhibitions were competitive with respect to ATP or to L-methionine, indicating a dual substrate site mode of binding to the enzyme forms.

  7. Direct preparation of 14C-labelled 5-allyl- and 5-propyl-2'-deoxyuridine from [2-14C]2'-deoxyuridine

    International Nuclear Information System (INIS)

    Ruth, J.L.; White, S.K.; Bergstrom, D.E.

    1982-01-01

    [2- 14 C]5-Allyl-2'-deoxyuridine was synthesized directly from [2- 14 C]2'-deoxyuridine using mercury, palladium, and 3-chloropropene. [2- 14 C]5-Propyl-2'-deoxyuridine was obtained by hydrogenation of the [ 14 C]5-allyl-2'-deoxyuridine. Advantages of the synthetic method and its application to the preparation of other radiolabeled 5-alkyl/alkenyl-2'-deoxyuridines are discussed. (author)

  8. New Insight into the Cleavage Reaction of Nostoc sp. Strain PCC 7120 Carotenoid Cleavage Dioxygenase in Natural and Nonnatural Carotenoids

    Science.gov (United States)

    Heo, Jinsol; Kim, Se Hyeuk

    2013-01-01

    Carotenoid cleavage dioxygenases (CCDs) are enzymes that catalyze the oxidative cleavage of carotenoids at a specific double bond to generate apocarotenoids. In this study, we investigated the activity and substrate preferences of NSC3, a CCD of Nostoc sp. strain PCC 7120, in vivo and in vitro using natural and nonnatural carotenoid structures. NSC3 cleaved β-apo-8′-carotenal at 3 positions, C-13C-14, C-15C-15′, and C-13′C-14′, revealing a unique cleavage pattern. NSC3 cleaves the natural structure of carotenoids 4,4′-diaponeurosporene, 4,4′-diaponeurosporen-4′-al, 4,4′-diaponeurosporen-4′-oic acid, 4,4′-diapotorulene, and 4,4′-diapotorulen-4′-al to generate novel cleavage products (apo-14′-diaponeurosporenal, apo-13′-diaponeurosporenal, apo-10′-diaponeurosporenal, apo-14′-diapotorulenal, and apo-10′-diapotorulenal, respectively). The study of carotenoids with natural or nonnatural structures produced by using synthetic modules could provide information valuable for understanding the cleavage reactions or substrate preferences of other CCDs in vivo and in vitro. PMID:23524669

  9. Synthesis of [14C]Zolpidem

    International Nuclear Information System (INIS)

    Allen, J.; Tizot, A.

    1986-01-01

    The synthesis of [ 14 C]Zolpidem, a new hypnotic agent having a non-benzodiazepine structure, is described. This compound was synthesised in a 64% overall radiochemical yield from potassium [ 14 C]cyanide and with a specific radioactivity of 56 mCi/mmol. It was used for pharmacokinetic and drug metabolism studies. (author)

  10. A convenient method for 14C-labeling of 2-methylthio-1-[4-N-α-ethoxycarbonylbenzyl)-amino-benzyl] -5-hydroxymethyl-2-[14C]-1H-imidazole and 1-[4-N-α-ethoxy-carbonylbenzyl)-aminobenzyl]-5-hydroxymethyl-2-[14C] -1H-imidazole as potential antihypertensives

    International Nuclear Information System (INIS)

    Nader Saemian; Gholamhossein Shirvani; Mohsen Javaheri; Sayed Sajad Oliyaee

    2012-01-01

    The key synthetic intermediate, (2-mercapto-1-(4-nitrobenzyl)-1H-imidazol-5-yl)methanol-[2- 14 C], has been synthesized by using one pot procedure from potassium[ 14 C]-thiocyanate. It was converted to two nonpeptide angiotensin II receptor antagonists, 2-methylthio-1-[4-N-α-ethoxycarbonyl benzyl)-aminobenzyl]-5-hydroxymethyl-1H-imidazole-[2- 14 C] and 1-[4-N-α-ethoxy-carbonylbenzyl)-aminobenzyl] -5-hydroxymethyl-1H-imidazole-[2- 14 C] via a 3-step sequence synthetic pathway. (author)

  11. Radiosynthesis of N-¹¹C-Methyl-Taurine-Conjugated Bile Acids and Biodistribution Studies in Pigs by PET/CT.

    Science.gov (United States)

    Schacht, Anna Christina; Sørensen, Michael; Munk, Ole Lajord; Frisch, Kim

    2016-04-01

    During cholestasis, accumulation of conjugated bile acids may occur in the liver and lead to hepatocellular damage. Inspired by our recent development of N-(11)C-methyl-glycocholic acid-that is, (11)C-cholylsarcosine-a tracer for PET of the endogenous glycine conjugate of cholic acid, we report here a radiosynthesis of N-(11)C-methyl-taurine-conjugated bile acids and biodistribution studies in pigs by PET/CT. A radiosynthesis of N-(11)C-methyl-taurine-conjugated bile acids was developed and used to prepare N-(11)C-methyl-taurine conjugates derived from cholic, chenodeoxycholic, deoxycholic, ursodeoxycholic, and lithocholic acid. The lipophilicity of these new tracers was determined by reversed-phase thin-layer chromatography. The effect of lipophilicity and structure on the biodistribution was investigated in pigs by PET/CT using the tracers derived from cholic acid (3α-OH, 7α-OH, 12α-OH), ursodeoxycholic acid (3α-OH, 7β-OH), and lithocholic acid (3α-OH). The radiosyntheses of the N-(11)C-methyl-taurine-conjugated bile acids proceeded with radiochemical yields of 61% (decay-corrected) or greater and radiochemical purities greater than 99%. PET/CT in pigs revealed that the tracers were rapidly taken up by the liver and secreted into bile. There was no detectable radioactivity in urine. Significant reflux of N-(11)C-methyl-taurolithocholic acid into the stomach was observed. We have successfully developed a radiosynthesis of N-(11)C-methyl-taurine-conjugated bile acids. These tracers behave in a manner similar to endogenous taurine-conjugated bile acids in vivo and are thus promising for functional PET of patients with cholestatic diseases. © 2016 by the Society of Nuclear Medicine and Molecular Imaging, Inc.

  12. Synthesis of (R,S)-[2,3-13C2]-1-(1'-methyl-2'-pyrrolidinyl)propan-2-one; {(R,S)-[2',3'-13C2]hygrinePound right bracePound

    International Nuclear Information System (INIS)

    Abraham, T.W.; Leete, Edward

    1996-01-01

    2-Ethoxy-1-methyl-5-pyrrolidinone (1) was reacted with ethyl [3,4- 13 C 2 ]-acetoacetate (2) in the presence of TiCl 4 to give ethyl [3,4- 13 C 2 ]-2-(1'-methyl-5'-oxo-2'-pyrrolidinyl)-3-oxobutanoate (3) in 85% yield. Decarboethoxylation of ethyl [3,4- 13 C 2 ]-2-(1'-methyl-5'-oxo-2'-pyrrolidinyl)-3-oxobutan-oate (3) was accomplished using NaCl and H 2 O in DMSO to give (R,S)-[2,3- 13 C 2 ]-1-(1'-methyl-5'-oxo-2'-pyrrolidinyl)propan-2-o ne (4) in 91% yield. Protection of the ketone as a ketal (ethylene glycol, H + ), followed by reduction of the amide to the amine using LiAlH 4 and subsequent deprotection of the ketal gave (R,S)-[2,3- 13 C 2 ]-1-(1'-methyl-2'-pyrrolidinyl)propan-2-one ((R,s)-[2', 3'- 13 C 2 ]Hygrine) (8) in 78% yield. (61% overall yield from ethyl [3,4- 13 C 2 ]acetoacetate). (Author)

  13. Prediction of methyl-side Chain Dynamics in Proteins

    International Nuclear Information System (INIS)

    Ming Dengming; Brueschweiler, Rafael

    2004-01-01

    A simple analytical model is presented for the prediction of methyl-side chain dynamics in comparison with S 2 order parameters obtained by NMR relaxation spectroscopy. The model, which is an extension of the local contact model for backbone order parameter prediction, uses a static 3D protein structure as input. It expresses the methyl-group S 2 order parameters as a function of local contacts of the methyl carbon with respect to the neighboring atoms in combination with the number of consecutive mobile dihedral angles between the methyl group and the protein backbone. For six out of seven proteins the prediction results are good when compared with experimentally determined methyl-group S 2 values with an average correlation coefficient r-bar=0.65±0.14. For the unusually rigid cytochrome c 2 no significant correlation between prediction and experiment is found. The presented model provides independent support for the reliability of current side-chain relaxation methods along with their interpretation by the model-free formalism

  14. A rapid microwave induced synthesis of [carboxyl-14C]-nicotinic acid (vitamin B3) and [carbonyl-14C]-nicotinamide using K14CN

    International Nuclear Information System (INIS)

    Ravi, S.; Mathew, K.M.; Sivaprasad, N.

    2008-01-01

    Microwave assisted direct aromatic substitution of 3-bromopyridine with K 14 CN as the cyanide source and catalytic amount of tetrabutylammonium bromide afforded [3- 14 C]-cyanopyridine 3 in 90% yield. Microwave assisted hydrolysis of 3 with a mixture of concentrated hydrochloric acid and propionic acid afforded [carboxyl- 14 C]-nicotinic acid in 95% yield whereas microwave assisted hydrolysis of 3 with a mixture of concentrated sulfuric acid and propionic acid afforded [carbonyl- 14 C]-nicotinamide in 85% yield. (author)

  15. Appraisal of the 14C-glycocholate acid test with special reference to the measurement of faecal 14C excretion

    International Nuclear Information System (INIS)

    Scarpello, J.H.B.; Sladen, G.E.

    1977-01-01

    The 14 C-glycocholate test, including the measurement of marker corrected faecal 14 C, has been assessed in the following groups of subjects: normal controls (18), patients with diarrhoea not attributable to altered bile acid metabolism (21), patients with diverticula of the small intestine (12), patients with previous resection of ileum and often proximal colon (34), and established ileostomists (10). Patients with diverticular disease had increased breath 14 CO 2 excretion, but normal faecal excretion of 14 C, and this test was more frequently abnormal than the Schilling test. Ileostomists excreted increased amounts of faecal 14 C, even when the ileum was intact and apparently normal. The pattern after resection was complex. Breath 14 C output was normal if the ileal resection was less than 25 cm in length, although some of these patients had increased faecal 14 C excretion if, in addition, at least 15 cm of proximal colon had been resected or by-passed. Longer ileal resections were associated with increased breath and/or faecal 14 C excretion, depending in part on the length of colon resected or by-passed and the 24 hour faecal volume. Fewer than half these patients had both increased breath and faecal excretion of isotope and faecal 14 C alone was occasionally normal with an ileal resection of 50 cm or more. The 14 C-glycocholate test was more frequently abnormal than the Schilling test in this group. The use of faecal marker correction had only a minor impact on the results. These data suggest that, in patients with ileal resection, faecal 14 C, like faecal weight, is determined by the extent of colonic resection as well as by the amount of ileum resected. (author)

  16. Synthesis of 14C-labelled milrinone

    International Nuclear Information System (INIS)

    Duncan, D.R.; Johnston, D.; Andrews, R.S.

    1985-01-01

    A synthetic procedure for producing 14 C-labelled milrinone, a potent new cardiotonic agent, is described. The synthesis was achieved in two steps from 1-(4-pyridyl)propan-2-one utilising [2- 14 C]cyanoacetamide as the source of the radiolabel. The overall chemical yield was 46% and the radiochemical yield 35%. (author)

  17. Behaviour of 14C-sulfadiazine and 14C-difloxacin during manure storage

    International Nuclear Information System (INIS)

    Lamshoeft, Marc; Sukul, Premasis; Zuehlke, Sebastian; Spiteller, Michael

    2010-01-01

    The persistence of sulfadiazine, difloxacin, and their metabolites has been investigated in stored manure. The manure collected from sulfadiazine ( 14 C-SDZ) and difloxacin ( 14 C-DIF) treated pigs contained N-acetylsulfadiazine (Ac-SDZ), 4-hydroxy-SDZ (4-OH-SDZ), and sarafloxacin (SARA) as the main metabolites, respectively along with their parent compounds. Manures were stored separately at 10 o C and 20 o C at various moisture levels. About 96-99% of the radioactivity remained in extractable parent compounds and their metabolites after 150 d of storage. The formation of non-extractable residue and the rate of mineralization were both negligible in manure containing SDZ and DIF. During storage SDZ concentration increased as a result of the deacetylation of Ac-SDZ, whose concentration decreased proportionally. Hence the environmental effects may be underestimated if the parent compound alone is considered for environmental risk assessment. About 11% and 14% of 4-OH-SDZ were lost after 20 and 40 d of storage; thereafter its concentration increased relatively, highlighting hydroxylation of SDZ. DIF degraded very slowly (7% loss after 150 d) during the storage of manure; in contrast the concentration of SARA decreased rapidly (72-90% loss after 150 d). Dilution of manure and storage at higher temperatures for a reasonable period of time enhanced the rate of reactions of SDZ, DIF and their related metabolites.

  18. 14C concentrations in tree stems, 1

    International Nuclear Information System (INIS)

    Kikata, Yoji; Yonenobu, Hitoshi; Morishita, Fumio; Hattori, Yoshiaki; Marsoen, S.N.

    1993-01-01

    The 14 C concentrations in trees sampled at various latitudes were measured with a Tandetron Accelerator Mass Spectrometer at Nagoya University. The growing periods of the parts for 14 C measurements were estimated by the relationship between meteorological conditions and the appearance of anatomical features of annual rings such as false rings, latewood formation, and so on. The following results were obtained: 1. The latitude dependence of the 14 C variation is found in tree stems as well as in the atmosphere. 2. The 14 C concentrations in tree stems are almost equal to those in the atmosphere at the latitude where the tree had grown and at the time when the sampled section is formed. Therefore the 14 C concentrations in the atmosphere are estimated by those of the tree stems. 3. The time when the 14 C concentration in the tree showed its maximum value has difference of 1 - 2 years with that of the latitude where the tree had grown. 4. This phenomena seemed to be related closely with the mechanism of global mixing of 14 CO 2 produced by atmospheric nuclear weapon tests. This mechanism causes a time lag of 14 C variation between northern and southern hemisphere. (author)

  19. Estimation of radiation dosage and transmutation effect of 14C involved in measuring rate of albumin synthesis with 14C-carbonate

    International Nuclear Information System (INIS)

    Yap, A.H.; Hafkenscheid, J.C.M.; Goossens, C.M.I.C.; Buys, W.C.A.M.; Binkhorst, R.A.; Van Tongeren, J.H.M.

    1975-01-01

    For direct measurement of the rate of albumin synthesis, Na 2 14 CO 3 was used intravenously. The assessment of the radiation hazard involved in the study was based on the knowledge of the minimum dose of Na 2 14 CO 3 necessary for a sufficient incorporation of 14 C in the guanidine-C of arginine in albumin to obtain measurable radioactivity. By measurement of expired 14 CO 2 and excreted 14 C-urea in the urine during a 5-hr period following intravenous administration of Na 2 14 CO 3 in five subjects, some quantitative data on 14 C retention and radiation dosage were obtained. In comparison with animal studies, the rate of expiration of 14 CO 2 in man is slower. About 50 percent of the total radioactivity injected was lost through the respiratory route in the first hour. The total amount of expired 14 C during the 5 hr of investigation was about 75 percent of the injected dose for the five subjects. The amount of 14 C excreted as urinary 14 C-urea during the 5 hr of investigation is very small in comparison with the expired 14 C; it was only about 0.5 percent of the dose injected. The total absorbed radiation dose after complete elimination of 14 C from the body was calculated with various assumptions. The extra risk of genetic damage due to disintegration of retained 14 C in comparison with that of natural 14 C in the body during 30 living years is about 50 percent. (U.S.)

  20. Facile syntheses of isotope-labeled chiral octahydroindole-2-carboxylic acid and its N-methyl analog

    International Nuclear Information System (INIS)

    Yinsheng Zhang

    2012-01-01

    We have synthesized deuterium and carbon-14 labeled enantiomerically pure octahydroindole-2-carboxylic acid (PD0140417), N-methyl octahydroindole-2-carboxylic acid (PD0348183) and their racemic analogs (PD0108405 and PD0338055). [ring-U- 14 C]PD0140417 was prepared from [ring-U- 14 C]benzoic acid in a seven-step synthesis in 6.2% overall radiochemical yield. [ 14 C]PD0348183 was prepared from [ 14 C]BaCO 3 in a five-step synthesis in 16% radiochemical yield. Additionally, [D]PD0108405 and [D]PD0338055 were synthesized by direct platinum-catalyzed hydrogenation with deuterium gas. (author)

  1. Study of α-monosubstituted methyl acetates by C-13 and H-1 Nuclear Magnetic resonance

    International Nuclear Information System (INIS)

    Silva, E.L.

    1987-01-01

    The substituents effects on the methylene and carbonyl carbons chemical shifts of some α-monosubstituted methyl acetates Z-CH 2 -COOMe(Z=H,Cl,Br,I,OME,SMe,NMe 2 and Me) is studied. Some data of Carbon 13 NMr in the light of the substituents empirical and electronic effects are shown. Solvent and concentration effects on the hydrogen-1 chemical shifts of methyl acetate, bromoacetate and Iodoacetate were interpreted in the light of the Cα-C(O)-bond rotational isomerism. (M.J.C.) [pt

  2. Transfer of {sup 14}C to prenatal and neonatal rats from their mothers exposed to {sup 14}C compounds by ingestion

    Energy Technology Data Exchange (ETDEWEB)

    Takeda, H.; Fuma, S.; Miyamoto, K.; Kuroda, N.; Inaba, J

    2003-07-01

    The transfer of {sup 14}C through placenta or milk was investigated and the radiation dose to fetal and newborn rats was estimated. Female rats at gestational stages or after delivery were exposed to {sup 14}C in the form of sodium bicarbonate, thymidine and lysine by a single ingestion. Radioactivity in maternal tissues and conceptuses (placenta, fetal membrane and fetus) and in the newborn was determined at various times after ingestion. After exposure to these {sup 14}C compounds, there was no significant difference between the {sup 14}C concentration in the fetus and that in the maternal tissues, suggesting that the placenta has no effect in preventing or accelerating the placental transfer of {sup 14}C. The concentration and content of {sup 14}C in the fetus and newborn were, however, dependent on the chemical form of {sup 14}C and on the prenatal or neonatal stage at the time of ingestion. The result of the dose estimation showed that {sup 14}C-lysine gave significantly higher prenatal and neonatal doses than {sup 14}C-sodium bicarbonate or {sup 14}C-thymidine. (author)

  3. Regulation of choline acetyltransferase expression by 17 β-oestradiol in NSC-34 cells and in the spinal cord.

    Science.gov (United States)

    Johann, S; Dahm, M; Kipp, M; Zahn, U; Beyer, C

    2011-09-01

    Motoneurones located in the ventral horn of the spinal cord conciliate cholinergic innervation of skeletal muscles. These neurones appear to be exceedingly affected in neurodegenerative diseases such as amyotrophic lateral sclerosis. The dysfunction of motoneurones is typically accompanied by alterations of cholinergic metabolism and signalling, as demonstrated by a decrease in choline acetyltransferase (ChAT) expression. 17 β-Oestradiol (E(2)) is generally accepted as neuroprotective factor in the brain under acute toxic and neurodegenerative conditions and also appears to exert a protective role for motoneurones. In the present study, we attempted to analyse the role of E(2) signalling on ChAT expression in the motoneurone-like cell line NSC-34 and in vivo. In a first step, we demonstrated the presence of oestrogen receptor α and β in NSC-34 cells, as well as in the cervical and lumbar parts, of the male mouse spinal cord. Subsequently, we investigated the effect of E(2) treatment on ChAT expression. The application of E(2) significantly increased the transcription of ChAT in NSC-34 cells and in the cervical but not lumbar part of the spinal cord. Our results indicate that E(2) can influence the cholinergic system by increasing ChAT expression in the mouse spinal cord. This mechanism might support motoneurones, in addition to survival-promoting mechanisms, in the temporal balance toxic or neurodegenerative challenges. © 2011 The Authors. Journal of Neuroendocrinology © 2011 Blackwell Publishing Ltd.

  4. Synthesis of 14C- and 2H-labeled 1,3 dihydro-3, 3-dimethyl-5-(1,4,5,6,- tetrahydro-6-oxo-3-pyridazinyl)-2H-indol-2-one (LY195115), an orally effective positive inotrope

    International Nuclear Information System (INIS)

    Robertson, D.W.; Krushinski, J.H.; Kau, D.

    1986-01-01

    The synthesis of 14 C- and 2 H-labeled 1,3-dihydro-3,3-dimethyl-5-(1,4,5,6-tetrahydro-6-oxo-3-pyridazinyl)-2H-indol -2-one (LY195115), an extremely potent, orally-effective cardiotonic with inotropic and vasodilator activities is described. The 14 C-label was introduced in the antepenultimate step by reaction of a β-chloroketone precursor with Na 14 CN; acid-catalyzed hydrolysis and cyclization with hydrazine provided the tetrahydropyridazinone bearing the 14 C-label in the oxo-carbon. 1,3-Dihydro-3,3-di(methyl-d 3 ) -2H-indol-2-one was prepared by exhaustive methylation of 1-acetyl-1,3-dihydro-2H-indol-2-one with sodium hydride and iodomethane-d 3 , followed by removal of the nitrogen protecting group. This labeled material was converted in two steps to [ 2 H 6 ]-LY195115. (author)

  5. Effects of Pseudomonas species on the release of bound 14C residues from soil treated with [14C]atrazine

    International Nuclear Information System (INIS)

    Khan, S.U.; Behki, R.M.

    1990-01-01

    The release of bound (nonextractable) 14 C residues from soil previously treated with [ 14 C]atrazine was investigated by incubation of the solvent-extracted soil with two species of Pseudomonas capable of metabolizing atrazine. The two species, 192 and 194, released bound 14 C residues from the soil. Addition of glucose, known to increase microbiological activities, to the incubated soil appeared to enhance the release of soil-bound 14 C residues, in particular in the presence of Pseudomonas species 192. The 14 C bound residues in soil, mainly present as the parent compound and its hydroxy and monodealkylated analogues, were released into the incubation mixture and were subsequently metabolized by the two species involving dechlorination and dealkylation

  6. Early incorporation and distribution of 14C-photosynthates after 14C-feeding for a brief period in tea plant

    International Nuclear Information System (INIS)

    Hakamata, Katsuhiro

    1981-01-01

    In order to clarify the early incorporation and distribution of 14 C-photosynthetic products in tea plants after 14 C-feeding for a brief period, 14 C-tracer experiments were performed, using the winter leaves, first crop shoots and young tea plants of a cultivar, Yabukita. As the results of the experiment on leaf disks by 14 C-Feeding for one minute, the 14 C-activity in the ethanol soluble fraction distributed in the anionic, cationic and neutral fractions in this order. When the time of feeding was extended to 10 min, the distribution in the cationic fraction decreased, and that in the neutral fraction increased. In the experiment on shoots, after the end of 10 min assimulation, the 14 C-activity in the ethanol soluble fraction distributed in the neutral, cationic and anionic fractions in this order. In course of time, the distribution in the cationic and anionic fractions decreased, and that in the neutral fraction increased. As the results of 14 C-feeding to young tea plants for 2.5 hours, 70 - 95% of the 14 C-activity in the ethanol soluble fraction distributed in the neutral fraction. Sucrose seemed to be the primary and early product of photosynthesis, and might be the principal carbohydrate form of translocation and reserve in tea plants. Raffinose and stachyose played almost the same role as sucrose. (Kako, I.)

  7. Solvent-free synthesis of C10 and C11 branched alkanes from furfural and methyl isobutyl ketone.

    Science.gov (United States)

    Yang, Jinfan; Li, Ning; Li, Guangyi; Wang, Wentao; Wang, Aiqin; Wang, Xiaodong; Cong, Yu; Zhang, Tao

    2013-07-01

    Our best results jet: C10 and C11 branched alkanes, with low freezing points, are synthesized through the aldol condensation of furfural and methyl isobutyl ketone from lignocellulose, which is then followed by hydrodeoxygenation. These jet-fuel-range alkanes are obtained in high overall yields (≈90%) under solvent-free conditions. Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  8. Metabolism of methyl-branched iodo palmitic acids in cultured hepatocytes

    International Nuclear Information System (INIS)

    Thomas, G.; Pepin, D.; Loriette, C.; Chambaz, J.; Bereziat, G.; Vidal, M.; Apparu, M.; Coornaert, S.

    1989-01-01

    The metabolic fate of methyl-branched iodo fatty acids was studied in primary culture of rat hepatocytes. We compared 16-iodo-2-R,S-methyl palmitic acid (2-Me), which can be β oxidized, with 16-iodo-3-R,S-methyl palmitic acid (3-Me) which can be β oxidized only after an initial α oxydation and with 16-iodo-2,2-dimethyl palmitic acid (2,2-Me 2 ) and 16-iodo-3,3-dimethyl palmitic acid (3,3-Me 2 ) which cannot be β oxidized at all. The normal fate of natural fatty acids was given by comparative experiments with [1- 14 C] palmitic acid. Monomethyl-branched iodo fatty acids were taken up in the same range as palmitic acid but more than dimethyl-branched iodo fatty acids. After a 15-h incubation, acido-soluble products (ASP) accounted for 75% of the radioactivity taken up as 16-iodo-2-methyl palmitic acid, 50% as other methyl-branched iodo fatty acids and only 30% as palmitic acid. Cultured hepatocytes, labelled for 3 h with the various fatty acids and reincubated for 12 h without fatty acid, secreted large amounts of free dimethyl-branched iodo fatty acids as compared to the monomethyl ones and palmitic acid. Only hepatocytes prelabelled with 16-[ 125 I]iodo-2,2-dimethyl palmitic acid exhibited an appreciable secretion of labeled triglycerides, but at a lower rate than with [1- 14 C] palmitic acid. Conversely, the 16-iodo-monomethyl palmitic acids remained chiefly in hepatocyte triglycerides. Minute amounts of 16-iodo-methyl-branched palmitic acids were found in hepatocyte or secreted phospholipids as compared with palmitic acid. (orig.)

  9. Genetic consequences of the 14C-decay

    International Nuclear Information System (INIS)

    Gracheva, L.M.; Korolev, V.G.

    1978-03-01

    There are only few investigations on the biological and genetic consequences of 14 C decay especially due to the long half-life of 14 C. Naturally, the consequences of the decay of 14 C incorperated in DNA is of particular interest. Due to the thus occuring conversion into nitrogen, either opening of the ribose residue ring and base occurs or conversion into base analogue. The present work gives a survey on the investigational results on this topic which were obtained by various authors on phages, bacteria, algae and animal cells, as well as on molecular level. It was shown that the transmutation for the occurence of a lethal effect is many times more effective than β-radiation. Investigations of the mutagenic effects and other genetic effects of the 14 C decay were carried out on micro-organisms, however also on higher forms of life, plants, insects and mice. An analysis of the mutations showed that transitions as well as transversions occur. As example for genetic effects of 14 C decay, the two following are named. In the case of mice which were exposed to 14 CO 2 atmosphere, it was seen that the number of polyptoidal chromosome sets in the first spermotacytes increased considerably, an increase of the chromosome conversion rate was however not observed. When treating gryllus larvae with 14 C, it was interesting to note that the crossing of 14 C-contained females with normal males produced viable eggs, whereas normal females after crossing with 14 C contained males, laid no more eggs. (MG) 891 MG [de

  10. Reviewing the Mid-First Millennium BC {sup 14}C 'warp' using {sup 14}C/bristlecone pine data

    Energy Technology Data Exchange (ETDEWEB)

    Taylor, R.E., E-mail: retaylor@ucr.edu [Department of Anthropology, University of California, Riverside, Riverside, CA (United States); Cotsen Institute of Archaeology, University of California, Los Angeles, CA (United States); Keck Carbon Cycle Accelerator Mass Spectrometry Laboratory, University of California, Irvine, CA (United States); Southon, John [Keck Carbon Cycle Accelerator Mass Spectrometry Laboratory, University of California, Irvine, CA (United States)

    2013-01-15

    AMS-based {sup 14}C measurements have been obtained on 53 dendrochronologically-dated Bristlecone pine (Pinus longaeva) wood samples in decadal increments spanning 2300-2750 cal BP with particular interest focused on the decades centered on 2405 cal BP and 2625 cal BP. In general, there is overall agreement with the current IntCal04/09 consensus calibration curve for this period. For the 2400-2410 cal BP interval, our Bristlecone-based {sup 14}C value is consistent with the {sup 14}C value obtained by Belfast on Irish oak for that decade but not on German oak values obtained by Seattle. Our {sup 14}C value for the 2620-2630 cal BP interval is consistent with the German oak (Heidelberg)-based {sup 14}C decadal value. The {sup 10}Be-based reconstruction of {sup 14}C variations over the 2620-2630 cal BP interval also supports the Heidelberg data although clearly additional clarifications are required before the current tree ring-based {sup 14}C and ice core-based {sup 10}Be data for this interval can be accurately interpreted and valid inferences obtained.

  11. Analysis of loss of offsite power transient using RELAP5/MOD1/NSC

    International Nuclear Information System (INIS)

    Kim, Hho Jung; Chung, Bub Dong; Lee, Young Jin; Kim, Jin Soo

    1986-01-01

    System thermal-hydraulic parameters and simulated, using the best-estimate system code(RELAP5/MOD1/NSC), based upon the sequence of events for the KNU1( Korea Nuclear Unit 1) loss of offsite power transient at 77.5% power which occurred on June 9,1981. The results are compared with the actual plant transient data and show good agreements. After the flow coastdown following the trips of both reactor coolant pumps, the establishment of natural circulation by the temperature difference between the hot and the cold legs is confirmed. The calculated reactor coolant flowrate closely approximate the plant data indicating the validity of relevant thermal-hydraulic models in the RELAP5/MOD1/NSC. Results also show that the sufficient heat removal capability is secured by the appropriate supply of the auxiliary feedwater without the operation of S/G PORVs. In addition, a scenario accident at full power, based upon the same sequence of events described above, is also analysed and the results confirmed that the safety of KNU1 is secured by the appropriate operation of the S/G PORVs coupled with the supply of auxiliary feedwater which ensures sufficient heat removal capability. The characteristics of the non-safety related components such as the turbine stop valve closing time, S/G PORV setting etc. are recognized to be important in the transient analyses on a bestestimate basis. (Author)

  12. Reirradiation and lomustine in patients with relapsed high-grade gliomas

    International Nuclear Information System (INIS)

    Arcicasa, Mauro; Roncadin, Mario; Bidoli, Ettore; Dedkov, Anatolyi; Gigante, Marco; Trovo, Mauro G.

    1999-01-01

    Purpose: The aim of this study was to evaluate the toxicity, response, and survival of patients with relapsed high-grade gliomas after radiation therapy (RT) combined with lomustine (CCNU). Methods and Materials: Thirty-one patients with relapsed gliomas at least 6 months after completion of RT were reirradiated. Twenty-four patients had a pathological diagnosis of high-grade gliomas, whereas 7 had a radiological diagnosis of relapsed malignant gliomas. The study focused on patients with high-grade relapsed gliomas. A total dose of 34.5 Gy was delivered in 23 fractions over 4.5 weeks. Oral administration of CCNU (130 mg/m 2 ) was begun at the same time as RT, and was repeated every 6 weeks until disease progression, or up to 12 courses. Results: Twelve of 24 patients had surgery before RT plus CCNU treatment. Median interval between RT courses was 14 months (range 6-73). All patients received a complete course of RT, and 22 of 24 patients received at least one course of CCNU. Objective responses were seen in 14 evaluable patients: 3 with partial response, 5 with stable disease, and 6 with progressive disease. Duration of partial response was 20, 9, and 8 months. Median time to progression and overall survival from the onset of retreatment were 8.4 months (range 1-22) and 13.7 months (range 1-63+), respectively. One case of G4 thrombocytopenia was observed. Five patients had G1 or G2 leucopenia and 3 patients had G3 leucopenia. Moderate nausea and vomiting were reported in 4 patients. One patient, after one course of CCNU, refused further chemotherapy. No significant difference in survival from relapse was found between patients who underwent surgery before RT plus CCNU and those who received only RT plus CCNU (p = 0.74). Conclusion: Overall, the acute toxicity was moderate, and patient compliance was good. Reirradiation of high-grade glioma was associated with modest subjective and objective response rates. It is remarkable that median overall survival from relapse

  13. Extraction of pentylbenzene from high molar mass alkanes (C{sub 14} and C{sub 17}) by N-methyl-2-pyrrolidone

    Energy Technology Data Exchange (ETDEWEB)

    Fandary, Mohamed S. [Chemical Engineering Department, College of Technological Studies, P.O. Box 3242, Salmyiah 22033 (Kuwait)]. E-mail: mfandary@yahoo.com; Al-Jimaz, Adel S. [Chemical Engineering Department, College of Technological Studies, P.O. Box 3242, Salmyiah 22033 (Kuwait); Al-Kandary, Jasem A. [Chemical Engineering Department, College of Technological Studies, P.O. Box 3242, Salmyiah 22033 (Kuwait); Fahim, Mohamed A. [Chemical Engineering Department, University of Kuwait, P.O. Box 5969, Safat 13060 (Kuwait)

    2006-04-15

    Equilibrium tie line data have been determined for the two ternary liquid systems: {l_brace}tetradecane, or heptadecane + pentylbenzene + N-methyl-2-pyrrolidone (NMP){r_brace} over a temperature range of (298 to 328) K. The two systems studied exhibit type I liquid + liquid phase diagram. The effect of temperature and n-alkane chain length upon solubility, selectivity, and distribution coefficients were investigated experimentally.

  14. Radiotracer technique for studying the fate of methyl parathion in desert locust

    International Nuclear Information System (INIS)

    Garg, A.K.; Sethi, G.R.; Bhatia, Parvathy

    1988-01-01

    The present study, using 14 C-labelled methyl parathion was intended for standardising the procedure of analysis of the insecticide and its metabolites in the desert locust, Schistocerca gregaria Forskal. (author). 5 refs

  15. 14C levels in Trombay environment

    International Nuclear Information System (INIS)

    Doshi, G.R.; Sadarangani, S.H.; Krishnamoorthy, T.M.

    1994-01-01

    The passive air sampling method has been used to measure the spatial distribution of the specific activity of 14 C in air samples collected within the Trombay complex. The samples collected within radial distance of about 0.5 km from Cirus showed 3 to 5 times higher specific activity of 14 C over the natural background level of 6.2 pCi/g C. The same decreased with the distance and approached the value of natural level at the site boundary (1.6 km). The specific activity of 14 C in leaf samples collected within the complex showed the similar pattern. (author). 6 refs., 2 tabs

  16. [14C]Virginiamycin residues in eggs

    International Nuclear Information System (INIS)

    Corpet, D.E.; Baradat, M.; Bories, G.F.

    1988-01-01

    Laying hens were fed ab libitum a diet supplemented at 40, 10, and 0 mg/kg with [ 14 C]virginiamycin, to determine whether or not virginamycin or its metabolites were transferred to the eggs. About 0.05% of the ingested 14 C dose was recovered in the eggs. Radiolabeled residues expressed in terms of virginiamycin equivalents were found to be 5.1 ng/g in the albumen and 31.8 ng/g in the yolk from hens fed a 10 mg/kg diet. No antibiotic activity could be detected in the eggs. Tentative identifications showed that in the albumen about 17% of the 14 C behaved chromatographically like virginiamycin and 18% was associated to the ovalbumin. In the yolk 31% of the 14 C was associated to proteins, 58% to fatty acids, and 4% to unsaponifiable matter

  17. Carbon-14 methylation of the 2-methylbutyryl side chain of mevinolin and its analogs

    International Nuclear Information System (INIS)

    Prakash, S.R.; Ellsworth, R.L.

    1988-01-01

    A one step procedure for the preparation of three labeled mevinolin analogs possessing the 2,2-dimethylbutyryloxy side chain is described. Three lactones were converted into potassium salts of their corresponding di or trihydroxy carboxylic acids from which anionic ester enolates were generated and alkylated with [ 14 ]methyl iodide. Workup and purification by reverse phase HPLC provided the three radiochemically pure mevinolin analogs. The labeled lactones were converted into ammonium salts of their corresponding di or trihydroxy acids. (author)

  18. Synthesis of 11C labelled methyl esters: transesterification of enol esters versus BF3 catalysed esterification-a comparative study

    International Nuclear Information System (INIS)

    Ackermann, Uwe; Blanc, Paul; Falzon, Cheryl L.; Issa, William; White, Jonathan; Tochon-Danguy, Henri J.; Sachinidis, John I.; Scott, Andrew M.

    2006-01-01

    C-11 labelled methyl esters have been synthesized via the transesterification of enol esters in the presence of C-11 methanol and 1,3 dichlorodibutylstannoxane as catalyst. This method leaves functional groups intact and allows access to a wider variety of C-11 labelled methyl esters compared to the BF 3 catalysed ester formation, which uses carboxylic acids and C-11 methanol as starting materials

  19. 14C emission from Swedish nuclear power plants and its effect on the 14C levels in the environment

    International Nuclear Information System (INIS)

    Stenstroem, K.; Erlandsson, Bengt; Hellborg, R.; Kiisk, M.; Persson, Per; Mattsson, Soeren; Thornberg, C.; Skog, G.

    2000-02-01

    The radionuclide 14 C is produced in all types of nuclear reactors mainly by neutron induced reactions in oxygen ( 17 O), nitrogen ( 14 N) and carbon ( 13 C). Part of the 14 C created is continuously released during normal operation as airborne effluents in various chemical forms (such as CO 2 , CO and hydrocarbons) to the surroundings. Because of the biological importance of carbon and the long physical half-life of 14 C, it is of interest to measure the releases and their incorporation into living material. The 14 C activity concentrations in annual tree rings and air around two Swedish nuclear power plants (Barsebaeck and Forsmark) as well as the background 14 C activity levels from two reference sites in southern Sweden during 1973-1996 are presented in this report. In order to verify the reliability of the method some investigations have been conducted at two foreign nuclear sites, Sellafield fuel reprocessing plant in England, and Pickering nuclear generating station in Canada, where the releases of 14 C are known to be substantial. Furthermore, results from some measurements in the vicinity of Paldiski submarine training centre in Estonia are presented. The results of the 14 C measurements of air, vegetation and annual tree rings around the two Swedish nuclear power plants show very low enhancements of 14 C, if at all above the uncertainty of the measurements. Even if the accuracy of the measurements of the annual tree rings is rather good (1-2%) the contribution of 14 C from the reactors to the environment is so small that it is difficult to separate it from the prevailing background levels of 14 C . This is the case for all sampling procedures: in air and vegetation as well as in annual tree rings. Only on a few occasions an actual increase is observed. However, although the calculations suffer from rather large uncertainties, the calculated release rate from Barsebaeck is in fair agreement with reported release data. The results of this investigation show

  20. Critical off-target effects of the widely used Rac1 inhibitors NSC23766 and EHT1864 in mouse platelets

    DEFF Research Database (Denmark)

    Dütting, Sebastian; Heidenreich, Julius; Cherpokova, Deya

    2015-01-01

    BACKGROUND: Platelet aggregation at sites of vascular injury is essential for normal hemostasis, but may also cause pathological vessel occlusion. Rho GTPases are molecular switches that regulate essential cellular processes and they have pivotal functions in the cardiovascular system. Rac1......, have been characterized in different cell types, demonstrating high specificity for Rac1 or Rac, respectively. OBJECTIVES: We sought to analyze the specificity of NSC23766 and EHT1864. METHODS: Platelet function was assessed in mouse wild-type and Rac1-deficient platelets by using flow cytometric...... function tests. Both inhibitors induced a Rac1-specific inhibition of platelet spreading, but also markedly impaired agonist-induced activation of Rac1(-/-) platelets. Furthermore, GPIb-mediated signaling was dramatically inhibited by NSC23766 in both wild-type and Rac1-deficient platelets. Importantly...

  1. ORIGIN OF PALMITIC ACID CARBON IN PALMITATES FORMED FROM HEXADECANE-1-C14 AND TETRADECANE-1-C14 BY MICROCOCCUS CERIFICANS

    Science.gov (United States)

    Finnerty, W. R.; Kallio, R. E.

    1964-01-01

    Finnerty, W. R. (University of Iowa, Iowa City), and R. E. Kallio. Origin of palmitic acid carbon in palmitates formed from hexadecane-1-C14 and tetradecane-1-C14 by Micrococcus cerificans. J. Bacteriol. 87:1261–1265. 1964.—Degradation of the palmitic acid moiety of cetyl palmitate and myristyl palmitate formed from hexadecane-1-C14 and tetradecane-1-C14 by Micrococcus cerificans was carried out. The patterns of C14 labeling in palmitic acid from cetyl palmitate showed that hexadecane is oxidized at the C1 position, and cetyl alcohol and palmitic acid thus formed are directly esterified. Palmitic acid arising from tetradecane and esterified to tetradecanol appeared to have been synthesized by the addition of two carbon atoms to an existing 14-carbon atom skeleton. Considerable mixing of C14 occurred in the C1 and C2 positions of palmitic acid thus synthesized. PMID:14188700

  2. Effect of washing and boiling on residues of pirimiphos-methyl in soybeans

    International Nuclear Information System (INIS)

    Sulistiawaty, M.; Anwar, E.

    1996-01-01

    The residues of pirimiphos-methyl (0-2-diethylamino-6-methyl-pyrimidine-4-il-o-dimethyl phos-phorothioate) in soybean grains were studied using 14 C-labelled-pirimiphos-methyl. Jute sock containing soybean grains were sprayed with pirimiphos-methyl and then stored at room temperature. The results indicated than residues of pirimiphos-methyl in soybeans before washing, after washing, and after washing + boiling at 0 week storage were: 1.0, 0.42, and 0.01%: then increased to 42.01, 30.75, and 10.02%, respectively, after 12 weeks, and finally decreased to 38.33, 27.01, and 6.10%, respectively, after 24 weeks storage. The residues of pirimiphos-methyl in washing water at 0 week storage was 0.41%, then increased to 8.01% after 24 weeks storage. The percentage was calculated based on the amount of residue found compared to the initial pirimiphos-methyl used. (author)

  3. Synthesis of 1-(4-methylsulfone-phenyl)-5-(4-fluoro-phenyl)-5-[14C]-1,2,3- triazole and 1-(4-sulfonamide-phenyl)-5-(4-fluoro-phenyl)-5-[14C]-1,2,3- triazole as novel carbon-14 anticonvulsant

    International Nuclear Information System (INIS)

    Saemian, N.; Shirvani, G.; Matloubi, H.

    2006-01-01

    Two 1,2,3-triazole anticonvulsants, 1-(4-methylsulfone-phenyl)-5-(4-fluoro-phenyl)-5-[ 14 C]-1,2,3-triazole and 1-(4-sulfonamide-phenyl)-5-(4- fluoro-phenyl)-5-[ 14 C]-1,2,3-triazole, both labeled with carbon-14 in the 5-position were prepared from para-fluoro-benzonitrile-[cyano- 14 C]. (author)

  4. Dicty_cDB: FC-BS14 [Dicty_cDB

    Lifescience Database Archive (English)

    Full Text Available FC (Link to library) FC-BS14 (Link to dictyBase) - - - Contig-U16399-1 FC-BS14E (Li...nk to Original site) - - - - - - FC-BS14E 534 Show FC-BS14 Library FC (Link to library) Clone ID FC-BS14 (Li.../dictycdb.biol.tsukuba.ac.jp/CSM/FC/FC-BS/FC-BS14Q.Seq.d/ Representative seq. ID FC-BS...14E (Link to Original site) Representative DNA sequence >FC-BS14 (FC-BS14Q) /CSM/FC/FC-BS/FC-BS14Q.Seq.... vs CSM-cDNA Score E Sequences producing significant alignments: (bits) Value FC-BS14 (FC-BS

  5. Estimates of methyl 13C and 1H CSA values (Δσ) in proteins from cross-correlated spin relaxation

    International Nuclear Information System (INIS)

    Tugarinov, Vitali; Scheurer, Christoph; Brueschweiler, Rafael; Kay, Lewis E.

    2004-01-01

    Simple pulse schemes are presented for the measurement of methyl 13 C and 1 H CSA values from 1 H- 13 C dipole/ 13 C CSA and 1 H- 13 C dipole/ 1 H CSA cross-correlated relaxation. The methodology is applied to protein L and malate synthase G. Average 13 C CSA values are considerably smaller for Ile than Leu/Val (17 vs 25 ppm) and are in good agreement with previous solid state NMR studies of powders of amino acids and dipeptides and in reasonable agreement with quantum-chemical DFT calculations of methyl carbon CSA values in peptide fragments. Small averaged 1 H CSA values on the order of 1 ppm are measured, consistent with a solid state NMR determination of the methyl group 1 H CSA in dimethylmalonic acid

  6. Role of DNA methylation in miR-200c/141 cluster silencing in invasive breast cancer cells

    Directory of Open Access Journals (Sweden)

    Wernet Peter

    2010-08-01

    Full Text Available Abstract Background The miR-200c/141 cluster has recently been implicated in the epithelial to mesenchymal transition (EMT process. The expression of these two miRNAs is inversely correlated with tumorigenicity and invasiveness in several human cancers. The role of these miRNAs in cancer progression is based in part on their capacity to target the EMT activators ZEB1 and ZEB2, two transcription factors, which in turn repress expression of E-cadherin. Little is known about the regulation of the mir200c/141 cluster, whose targeting has been proposed as a promising new therapy for the most aggressive tumors. Findings We show that the miR-200c/141 cluster is repressed by DNA methylation of a CpG island located in the promoter region of these miRNAs. Whereas in vitro methylation of the miR-200c/141 promoter led to shutdown of promoter activity, treatment with a demethylating agent caused transcriptional reactivation in breast cancer cells formerly lacking expression of miR-200c and miR-141. More importantly, we observed that DNA methylation of the identified miR-200c/141 promoter was tightly correlated with phenotype and the invasive capacity in a panel of 8 human breast cancer cell lines. In line with this, in vitro induction of EMT by ectopic expression of the EMT transcription factor Twist in human immortalized mammary epithelial cells (HMLE was accompanied by increased DNA methylation and concomitant repression of the miR-200c/141 locus. Conclusions The present study demonstrates that expression of the miR-200c/141 cluster is regulated by DNA methylation, suggesting epigenetic regulation of this miRNA locus in aggressive breast cancer cell lines as well as untransformed mammary epithelial cells. This epigenetic silencing mechanism might represent a novel component of the regulatory circuit for the maintenance of EMT programs in cancer and normal cells.

  7. Role of DNA methylation in miR-200c/141 cluster silencing in invasive breast cancer cells.

    Science.gov (United States)

    Neves, Rui; Scheel, Christina; Weinhold, Sandra; Honisch, Ellen; Iwaniuk, Katharina M; Trompeter, Hans-Ingo; Niederacher, Dieter; Wernet, Peter; Santourlidis, Simeon; Uhrberg, Markus

    2010-08-03

    The miR-200c/141 cluster has recently been implicated in the epithelial to mesenchymal transition (EMT) process. The expression of these two miRNAs is inversely correlated with tumorigenicity and invasiveness in several human cancers. The role of these miRNAs in cancer progression is based in part on their capacity to target the EMT activators ZEB1 and ZEB2, two transcription factors, which in turn repress expression of E-cadherin. Little is known about the regulation of the mir200c/141 cluster, whose targeting has been proposed as a promising new therapy for the most aggressive tumors. We show that the miR-200c/141 cluster is repressed by DNA methylation of a CpG island located in the promoter region of these miRNAs. Whereas in vitro methylation of the miR-200c/141 promoter led to shutdown of promoter activity, treatment with a demethylating agent caused transcriptional reactivation in breast cancer cells formerly lacking expression of miR-200c and miR-141. More importantly, we observed that DNA methylation of the identified miR-200c/141 promoter was tightly correlated with phenotype and the invasive capacity in a panel of 8 human breast cancer cell lines. In line with this, in vitro induction of EMT by ectopic expression of the EMT transcription factor Twist in human immortalized mammary epithelial cells (HMLE) was accompanied by increased DNA methylation and concomitant repression of the miR-200c/141 locus. The present study demonstrates that expression of the miR-200c/141 cluster is regulated by DNA methylation, suggesting epigenetic regulation of this miRNA locus in aggressive breast cancer cell lines as well as untransformed mammary epithelial cells. This epigenetic silencing mechanism might represent a novel component of the regulatory circuit for the maintenance of EMT programs in cancer and normal cells.

  8. 2C-Methyl- D- erythritol 2,4-cyclodiphosphate synthase from Stevia rebaudiana Bertoni is a functional gene.

    Science.gov (United States)

    Kumar, Hitesh; Singh, Kashmir; Kumar, Sanjay

    2012-12-01

    Stevia [Stevia rebaudiana (Bertoni)] is a perennial herb which accumulates sweet diterpenoid steviol glycosides (SGs) in its leaf tissue. SGs are synthesized by 2C-methyl-D-erythritol 4-phosphate (MEP) pathway. Of the various enzymes of the MEP pathway, 2C-methyl-D-erythritol 2,4-cyclodiphosphate synthase (MDS) (encoded by MDS) catalyzes the cyclization of 4-(cytidine 5' diphospho)-2C-methyl-D-erythritol 2-phosphate into 2C-methyl-D-erythritol 2,4-cyclodiphosphate. Complementation of the MDS knockout mutant strain of Escherichia coli, EB370 with putative MDS of stevia (SrMDS) rescued the lethal mutant, suggesting SrMDS to be a functional gene. Experiments conducted in plant growth chamber and in the field suggested SrMDS to be a light regulated gene. Indole 3-acetic acid (IAA; 50, 100 μM) down-regulated the expression of SrMDS at 4 h of the treatment, whereas, abscisic acid did not modulate its expression. A high expression of SrMDS was observed during the light hours of the day as compared to the dark hours. The present work established functionality of SrMDS and showed the role of light and IAA in regulating expression of SrMDS.

  9. Methionine kinetics in adult men: effects of dietary betaine on L-[2H3-methyl-1-13C]methionine

    International Nuclear Information System (INIS)

    Storch, K.J.; Wagner, D.A.; Young, V.R.

    1991-01-01

    The effects of a daily 3-g supplement of betaine on kinetic aspects of L-[2H3-methyl-1-13C]methionine (MET) metabolism in healthy young adult men were explored. Four groups of four subjects each were given a control diet, based on an L-amino acid mixture supplying 29.5 and 21.9 mg.kg-1.d-1 of L-methionine and L-cystine for 4 d before the tracer study, conducted on day 5 during the fed state. Two groups received the control diet and two groups received the betaine supplement. Tracer was given intravenously (iv) or orally. The transmethylation rate of MET (TM), homocysteine remethylation (RM), and oxidation of methionine were estimated from plasma methionine labeling and 13C enrichment of expired air. RM tended to increase (P = 0.14) but the TM and methionine oxidation were significantly (P less than 0.05) higher after betaine supplementation when estimated with the oral tracer. No differences were detected with the intravenous tracer. Methionine concentration in plasma obtained from blood taken from subjects in the fed state was higher (P less than 0.01) with betaine supplementation. These results suggest that excess methyl-group intake may increase the dietary requirement for methionine

  10. Excitation functions of the systems 12C+14C and 13C+12C

    International Nuclear Information System (INIS)

    Haindl, E.

    1975-01-01

    The excitation functions of the systems 12 C+ 14 C and 13 C+ 12 C are investigated for different exit channels. The excitation functions measured do not show correlated structures as in the system 12 C+ 12 C. (WL/AK) [de

  11. How fresh is maple syrup? Sugar maple trees mobilize carbon stored several years previously during early springtime sap-ascent.

    Science.gov (United States)

    Muhr, Jan; Messier, Christian; Delagrange, Sylvain; Trumbore, Susan; Xu, Xiaomei; Hartmann, Henrik

    2016-03-01

    While trees store substantial amounts of nonstructural carbon (NSC) for later use, storage regulation and mobilization of stored NSC in long-lived organisms like trees are still not well understood. At two different sites with sugar maple (Acer saccharum), we investigated ascending sap (sugar concentration, δ(13) C, Δ(14) C) as the mobilized component of stored stem NSC during early springtime. Using the bomb-spike radiocarbon approach we were able to estimate the average time elapsed since the mobilized carbon (C) was originally fixed from the atmosphere and to infer the turnover time of stem storage. Sites differed in concentration dynamics and overall δ(13) C, indicating different growing conditions. The absence of temporal trends for δ(13) C and Δ(14) C indicated sugar mobilization from a well-mixed pool with average Δ(14) C consistent with a mean turnover time (TT) of three to five years for this pool, with only minor differences between the sites. Sugar maple trees hence appear well buffered against single or even several years of negative plant C balance from environmental stress such as drought or repeated defoliation by insects. Manipulative investigations (e.g. starvation via girdling) combined with Δ(14) C measurements of this mobilized storage pool will provide further new insights into tree storage regulation and functioning. © 2015 The Authors. New Phytologist © 2015 New Phytologist Trust.

  12. Determination of 14CO2 in breath and 14C in stool after oral administration of cholyl-1-[14C]glycine: clinical application

    International Nuclear Information System (INIS)

    Roda, A.; Roda, E.; Aldini, R.; Mazzella, G.; Festi, D.; Sama, C.; Barbara, L.

    1977-01-01

    Twenty patients with intestinal bacterial overgrowth and 20 control subjects were investigated for bile acid deconjugation, by measuring 14 CO 2 in the breath after cholyl-1-[ 14 C]glycine administration. 14 CO 2 output/24 h was 11.0 +- 5.2% (mean +- SD) in controls and 54.2 +- 14.0% (mean +- SD) in bacterial-overgrowth patients (P 14 CO 2 excretion rate in 12 h, when normalized to 100% of the dose at the 12th hour, gave an even finer discrimination between the two groups (no false responses). 14 C in stool, analyzed in 20 malabsorption patients and 20 controls by two different techniques, was 6.6 +- 4% and 31.38 +- 20.7% (mean +- SD), respectively. Results by the two different techniques described here correlated well (r = 0.99). Bile acid malabsorption was in reasonable agreement (r = 0.67) with percentage of ''chenoid'' (chenodeoxycholic acid plus ursodeoxycholic acid) in the stool by gas-liquid chromatography; a poorer correlation was observed when ''choloid'' (cholic acid plus its epimers) were plotted vs. 14 C in stool

  13. The production of (14C) oxalate during the metabolism of (14C) carbohydrates in isolated rat hepatocytes.

    Science.gov (United States)

    Rofe, A M; James, H M; Bais, R; Edwards, J B; Conyers, R A

    1980-04-01

    Oxalate (14C) was produced during the metabolism of (U-14C) carbohydrates in hepatocytes isolated from normal rats. At 10 mM, the order of oxalate production was fructose > glycerol > xylitol > sorbitol greater than or equal to glucose in the ratio 10 : 4 : 3 : 1 : 1. This difference between oxalate production from fructose and glucose was reflected in their rates of utilisation, glucose being poorly metabolised in hepatocytes from fasted rats. Fructose was rapidly metabolised, producing glucose, lactate and pyruvate as the major metabolites. Glycerol, xylitol and sorbitol were metabolised at half the rate of fructose, the major metabolites being glucose, lactate and glycerophosphate. The marked similarity in the pattern of intermediary metabolites produced by these polyols was not, however, reflected in the rates of oxalate production. Hepatic polyol metabolism resulted in high levels of cytosolic NADH, as indicated by elevated lactate : pyruvate and glycerophosphate : dihydroxyacetone phosphate ratios. The artificial electron acceptor, phenazine methosulphate (PMS) stimulated oxalate production from the polyols, particularly xylitol. In the presence of PMS, the order of oxalate production was fructose greater than or equal to xylitol > glycerol > sorbitol in the ratio 10 : 10 : 6 : 2. The production of glucose, lactate and pyruvate from the polyols was also stimulated by PMS, whereas the general metabolism of fructose, including oxalate production, was little affected. Oxalate (14C) was produced from (1-14C), (2-14C) and (6-14C) but not (3,4-14C) glucose in hepatocytes isolated from non-fasted, pyridoxine-deficient rats. Whilst this labelling pattern is consistent with oxalate being produced by a number of pathways, it is suggested that metabolism via hydroxypyruvate is a major route for oxalate production from various carbohydrates, with perhaps the exception of xylitol, which appears to have an alternative mechanism for oxalate production. The observation that

  14. Incorporation of 14C-succinate in Synechococcus

    International Nuclear Information System (INIS)

    Doehler, G.

    1983-01-01

    The cyanobacterium Synechococcus (= Anacystis nidulans) was grown under normal air conditions (0.03 vol.% CO 2 ) and in low white light (0.5 x 10 3 μW/cm 2 ) at 37 0 C. Kinetics of 14 C incorporation into several soluble products and pigments were studied after adding 14 C-succinate during photosynthesis and in the dark using the autoradiographic method. Radioactivity was found mainly in glutamate and aspartate during the photosynthetic period independent on 3-(3',4'-dichlorphenyl)-1,1-dimethylurea preincubation. In the dark period 14 C label could also be detected in malate. Short-term kinetics experiments showed a decrease in 14 C label of glutamate and a parallel increase of aspartate. Results were discussed in respect to the interrupted tricarboxylic acid cycle. (author)

  15. 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.

  16. The 11C-radioisotopic study of methanol conversion on V-MCM-41; the influence of methyl iodide on the transformation

    International Nuclear Information System (INIS)

    Sarkadi-Priboczki, E.; Szelecsenyi, F.; Kovacs, Z.; Solmaz, A.; Balci, S.; Dogu, T.

    2007-01-01

    Complete text of publication follows. The MCM-41 mesoporous material has Lewis and even Bronsted acid sites to produce dimethyl ether with some hydrocarbons, while over metal modified MCM-41 mostly formaldehyde and dimethoxy methane (i.e. methylal) or methyl formate are produced. In present experiments V incorporated basically mild acid sites of MCM-41 was prepared by low temperature direct synthesis. The V-MCM-41 has enough main active Lewis sites (by V-) to form formaldehyde and also light Bronsted acid sites to let the adsorbed formaldehyde eliminate and afterwards, with methanol, to form dimethoxy methane in nonoxidative environment. This V-MCM-41 has been tested by ethanol conversion in non-oxidative environments too and diethoxy methane as main product was detected. In present work the methanol conversion, as well as the methanol co-reaction with methyl iodide are studied from the same V-MCM-41 sample using 11 C-technique. The 11 C-labelled radioactive methanol has been already applied for determination of methanol conversion rates on Cu-modified MCM-41. The V-MCM-41 was prepared by direct hydrothermal synthesis method. The adsorption rate of 11 C-methanol and, after the reaction, the desorption rate of the remaining 11 C-derivatives on catalyst were continuously detected by gamma detectors. The derivatives were analyzed by radio-gas chromatography (gas chromatograph with FID coupled on-line with a radioactivity detector). Both dimethyl ether and hydrocarbon formation are also in slight degrees according to weak Lewis and Bronsted acidities. Since the conversion was carried out without added oxygen gas, only the frame oxygen can take part into catalysis. In presence of non-radioactive methyl iodide, the radioactive methanol is converted to radioactive methyl iodide on V-MCM-41. The radio-GC analysis confirmed that the iodide induced change of the reaction performance was reversible i.e. the radioactive methyl iodide was regenerated to non-radioactive methyl

  17. Synthesis of carbon-13 and carbon-14 labeled paldimycin tri-sodium salt

    International Nuclear Information System (INIS)

    Hsi, R.S.P.; Witz, D.F.; Visser, J.; Stolle, W.T.; Ditto, C.L.

    1989-01-01

    Carbon-14 labeled paldimycin trisodium salt was prepared by addition of N-acetyl-L-cysteine to [ 14 C]paulomycin, the radioactive antibiotic produced by fermentation of Streptomyces paulus in the presence of L-methionine labeled with carbon-14 in the S-methyl group. Carbon-13 nuclear magnetic resonance (NMR) spectra of paulomycin produced when the fermentation was carried out in the presence of L-[S-methyl- 13 C]methionine showed that the isotope incorporation had occurred specifically at the methoxy group of ring C, i.e., the 2-deoxy sugar portion of paulomycin. With sustained slow feed of labeled precursors during the optimum antibiotic production period, carbon-14 isotope yields of up to 17.5% with specific activity of up to 11.4 μCi per milligram of paulomycin, and carbon-13 isotope yields of up to 24% with 17-fold isotope enrichment over natural abundance, were achieved. (author)

  18. Winter wheat optimizes allocation in response to carbon limitation

    Science.gov (United States)

    Huang, Jianbei; Hammerbacher, Almuth; Trumbore, Susan; Hartmann, Henrik

    2016-04-01

    • Plant photosynthesis is not carbon-saturated at current atmospheric CO2 concentration ([CO2]) thus carbon allocation priority is of critical importance in determining plant response to environmental changes, including increasing [CO2]. • We quantified the percentage of daytime net assimilation (A) allocated to whole-plant nighttime respiration (R) and structural growth (SG), nonstructural carbohydrates (NSC) and secondary metabolites (SMs) during winter wheat (Triticum aestivum) vegetative growth (over 4 weeks) at glacial, ambient, and elevated [CO2] (170, 390 and 680 ppm). • We found that R/A remained relatively constant (11-14%) across [CO2] treatments, whereas plants allocated less C to growth and more C to export at low [CO2] than elevated [CO2]; low [CO2] grown plants tended to invest overall less C into NSC and SMs than to SG due to reduced NSC availability; while leaf SMs/NSC was greater at 170 ppm than at 680 ppm [CO2] this was the opposite for root SMs/NSC; biomass, especially NSC, were preferentially allocated to leaves instead of stems and roots, likely to relieve C limitation induced by low [CO2]. • We conclude that C limitation may force plants to reduce C allocation to long-term survival in order to secure short-term survival. Furthermore, they optimized allocation of the available resource by concentrating biomass and storage to those tissues responsible for assimilation.

  19. 14C Behaviour in PWR coolant

    International Nuclear Information System (INIS)

    Sims, Howard; Dickinson Shirley; Garbett, Keith

    2012-09-01

    Although 14 C is produced in relatively small amounts in PWR coolant, it is important to know its fate, for example whether it is released by gaseous discharge, removed by absorption on ion exchange (IX) resins or deposited on the fuel pin surfaces. 14 C can exist in a range of possible chemical forms: inorganic carbon compounds (probably mainly CO 2 ), elemental carbon, and organic compounds such as hydrocarbons. This paper presents results from a preliminary survey of the possible reactions of 14 C in PWR coolant. The main conclusions of the study are: - A combination of thermal and radiolytic reactions controls the chemistry of 14 C in reactor coolant. A simple chemical kinetic model predicts that CH 3 OH would be the initial product from radiolytic reactions of 14 C following its formation from 17 O. CH 3 OH is predicted to arise as a result of reactions of OH . with CH 4 and CH 3 , and it persists because there is no known radiation chemical reduction mechanism. - Thermodynamic considerations show that CH 3 OH can be thermally reduced to CH 4 in PWR conditions, although formation of CO 2 from small organics is the most thermodynamically favourable outcome. Such reactions could be catalysed on active nickel surfaces in the primary circuit. - Limited plant data would suggest that CH 4 is the dominant form in PWR and CO 2 in BWR. This implies that radiation chemistry may be important in determining the speciation. - Addition of acetate does not affect the amount of 14 C formed, but the addition of large amounts of stable carbon would lead to a large range of additional products, some of which would be expected to deposit on fuel pin surfaces as high molecular weight hydrocarbons. However, the subsequent thermal decomposition reactions of these products are not known. - Acetate addition may represent a small input of 12 C compared with organic material released from CVCS resins, although the importance of this may depend on whether that is predominantly soluble

  20. Synthesis of (/sup 14/C)Zolpidem

    Energy Technology Data Exchange (ETDEWEB)

    Allen, J.; Tizot, A.

    1986-04-01

    The synthesis of (/sup 14/C)Zolpidem, a new hypnotic agent having a non-benzodiazepine structure, is described. This compound was synthesised in a 64% overall radiochemical yield from potassium (/sup 14/C)cyanide and with a specific radioactivity of 56 mCi/mmol. It was used for pharmacokinetic and drug metabolism studies.

  1. Transformation of the herbicide [14C]glufosinate in soils

    International Nuclear Information System (INIS)

    Smith, A.E.

    1989-01-01

    The degradation of 2 μg/g [ 14 C]glufosinate (DL-homoalan-4-ylmethylphosphinic acid) was studied in clay, clay loam, and sandy loam soils at 85% field capacity and at 20 degree C. Over a 4-week period the soils were extracted and analyzed for transformation products by radiochemical and gas chromatographic techniques. In all soils there was release of [ 14 C]carbon dioxide and formation of [ 14 C]-3-(hydroxymethylphosphinyl)propionic acid (MPPA) as major degradation products. Within 21 days, about 55% of the applied 14 C herbicide had been transformed to MPPA in the sandy loam and 19% to [ 14 C]carbon dioxide. After 28 days, approximately 45% of the 14 C herbicide had been transformed to MPPA in the clay and clay loam and 10% released as [ 14 C]carbon dioxide. At all samplings, other 14 C transformation products appeared to be insignificant

  2. Accelerator mass spectrometry analysis of 14C-oxaliplatin concentrations in biological samples and 14C contents in biological samples and antineoplastic agents

    Science.gov (United States)

    Toyoguchi, Teiko; Kobayashi, Takeshi; Konno, Noboru; Shiraishi, Tadashi; Kato, Kazuhiro; Tokanai, Fuyuki

    2015-10-01

    Accelerator mass spectrometry (AMS) is expected to play an important role in microdose trials. In this study, we measured the 14C concentration in 14C-oxaliplatin-spiked serum, urine and supernatant of fecal homogenate samples in our Yamagata University (YU) - AMS system. The calibration curves of 14C concentration in serum, urine and supernatant of fecal homogenate were linear (the correlation coefficients were ⩾0.9893), and the precision and accuracy was within the acceptance criteria. To examine a 14C content of water in three vacuum blood collection tubes and a syringe were measured. 14C was not detected from water in these devices. The mean 14C content in urine samples of 6 healthy Japanese volunteers was 0.144 dpm/mL, and the intra-day fluctuation of 14C content in urine from a volunteer was little. The antineoplastic agents are administered to the patients in combination. Then, 14C contents of the antineoplastic agents were quantitated. 14C contents were different among 10 antineoplastic agents; 14C contents of paclitaxel injection and docetaxel hydrate injection were higher than those of the other injections. These results indicate that our quantitation method using YU-AMS system is suited for microdosing studies and that measurement of baseline and co-administered drugs might be necessary for the studies in low concentrations.

  3. Appraisal of the /sup 14/C-glycocholate acid test with special reference to the measurement of faecal /sup 14/C excretion

    Energy Technology Data Exchange (ETDEWEB)

    Scarpello, J H.B.; Sladen, G E [Royal Hospital, Sheffield (UK). Academic Div. of Medicine

    1977-09-01

    The /sup 14/C-glycocholate test, including the measurement of marker corrected faecal /sup 14/C, has been assessed in the following groups of subjects: normal controls (18), patients with diarrhoea not attributable to altered bile acid metabolism (21), patients with diverticula of the small intestine (12), patients with previous resection of ileum and often proximal colon (34), and established ileostomists (10). Patients with diverticular disease had increased breath /sup 14/CO/sub 2/ excretion, but normal faecal excretion of /sup 14/C, and this test was more frequently abnormal than the Schilling test. Ileostomists excreted increased amounts of faecal /sup 14/C, even when the ileum was intact and apparently normal. The pattern after resection was complex. Breath /sup 14/C output was normal if the ileal resection was less than 25 cm in length, although some of these patients had increased faecal /sup 14/C excretion if, in addition, at least 15 cm of proximal colon had been resected or by-passed. Longer ileal resections were associated with increased breath and/or faecal /sup 14/C excretion, depending in part on the length of colon resected or by-passed and the 24 hour faecal volume. Fewer than half these patients had both increased breath and faecal excretion of isotope and faecal /sup 14/C alone was occasionally normal with an ileal resection of 50 cm or more. The /sup 14/C-glycocholate test was more frequently abnormal than the Schilling test in this group. The use of faecal marker correction had only a minor impact on the results. These data suggest that, in patients with ileal resection, faecal /sup 14/C, like faecal weight, is determined by the extent of colonic resection as well as by the amount of ileum resected.

  4. Labelling of the thymidine and deoxyctidine bases of DNA by (2-14C) deoxycytidine in cultured L1210 cells

    International Nuclear Information System (INIS)

    Karle, J.M.; Hoeraut, R.M.; Cysyk, R.L.

    1983-01-01

    Exposure of cultured L1210 cells to (2- 14 C) deoxycytidine and analysis of radioactivity incorporated into DNA-pyrimidines revealed that 2.7-5.5-fold more radioactivity is incorporated into DNA-thymine than into cytosine bases. Thus, the pathway involving deamination of deoxycytidylate to deoxyuridylate and methylation to thymidylate is highly favoured over successive phosphorlation to dCTP. Several modified and endogenous pyrimidines altered the labelling of DNA-thymine and DNA-cytosine with (2- 14 C)-deoxycytidine. 3-deazauridine at 0.1 mM caused a 56% increase in the labelling of DNA-thymine. Both thymidine and 3-deazauridine (>=10 μM) increased the specific activity to DNA-cytosine by 4-fold. Cytosine arabinoside (ara-C) (>= 10 μM) reduced the labelling of both DNA-cytosine and DNA-thymine. Excess cytidine (0.1 mM) reduced the labelling of DNA-cytosine by 40%. Tetrahydrouridine at concentrations up to 1 mM had no effect. (author)

  5. Effect of two organophosphorus insecticides on the growth, respiration and (14C)-glucose metabolism of Azobacter chroococcum Beij

    International Nuclear Information System (INIS)

    Balasubramanian, A.; Narayanan, R.

    1980-01-01

    The two organophosphorus insecticides, commonly applied to soil, viz., disulfoton (0,0-diethyl S-2-ethyl thio ethyl phosphorodithioate) and fensulfothion (0,0-diethyl 0-4-methyl sulphinyl phenyl phosphorothioate) did not affect the in vitro growth of Azotobacter chroococcum Beij., the free-living, nitrogen fixing soil bacterium, at 2 ppm (lower level), while the normal dose (5 ppm) and the higher level (10 ppm) suppressed the growth. Respiration of the organism (glucose oxidation) was adversely affected by the insecticides in the growth medium and the inhibition increased with the concentration of the chemical. Both the insecticides suppressed the assimilation of ( 14 C)-glucose in the cold-TCA soluble, hot-TCA soluble fractions and insoluble residue of the cells whereas the 14 C-incorporation in the alcohol soluble and alcohol-ether soluble fractions was enhanced indicating that the insecticides considerably altered the glucose metabolism of the bacterium. (author)

  6. Biotransformation of primary nicotine metabolites. I. In vivo metabolism of R-(+)-[14C-NCH3]N-methylnicotinium ion in the guinea pig

    International Nuclear Information System (INIS)

    Pool, W.F.; Crooks, P.A.

    1985-01-01

    The in vivo biotransformation and tissue distribution of the methylated nicotine metabolite R-(+)-[ 14 C-NCH 3 ]N-methylnicotinium acetate was studied in the guinea pig. The detection and quantification of 24-hr urinary metabolites after ip injection was determined by cation-exchange HPLC interfaced to a radiochemical flowthrough detector. The urinary metabolite profile consisted of five peaks. One eluted close to the void, and three coeluted with authentic standards of N-methylcotininium ion, N-methylnornicotinium ion, and N-methylnicotinium ion. A fifth, and as yet unidentified, metabolite was also detected. Tissue distribution of 14 C label after 24 hr was highest in the adrenal gland and epididymis followed by the gallbladder, bladder, kidney, spleen, and heart. No significant amounts of 14 C were found in the brain. The results indicate that N-methylcotininium ion and N-methylnornicotinium ion are both formed subsequent to the formation of N-methylnicotinium ion in the metabolism of R-(+)-nicotine in the guinea pig

  7. Synthesis of 11C-methylated inulin as a radiopharmaceutical for imaging brain edema and pulmonary edema

    International Nuclear Information System (INIS)

    Hara, Toshihiko; Iio, Masaaki; Inagaki, Keizo

    1988-01-01

    11 C-methylated inulin, supposedly useful for imaging of brain edema and pulmonary edema, was prepared using cyclotron produced 11 CO 2 . The synthesis consists of the production of 11 C-methyl iodide and its coupling with inulin alkoxide sodium in dimethylsulfoxide as solvent. 11 C labeled inulin was purified by alcohol precipitation. The radiochemical yield of pure 11 C-inulin was 34% of 11 CO 2 30 min after the end of bombardment. The blood clearance and body distribution of 11 C was observed in rabbits after i.v. injection of 11 C-inulin. The blood clearance curve was composed of a sum of three exponential functions. The gamma camera image showed that the 11 C activity in blood moved quickly to kidneys and urine and a small dose of radioactivity remained persistently in edematous tissues, i.e. the edematous lung tissues produced by oleic acid treatment. (orig.)

  8. Microwave-assisted pyrolysis of methyl ricinoleate for continuous production of undecylenic acid methyl ester (UAME).

    Science.gov (United States)

    Nie, Yong; Duan, Ying; Gong, Ruchao; Yu, Shangzhi; Lu, Meizhen; Yu, Fengwen; Ji, Jianbing

    2015-06-01

    Undecylenic acid methyl ester (UAME) was continuously produced from methyl ricinoleate using a microwave-assisted pyrolysis system with atomization feeding. The UAME yield of 77 wt.% was obtained at 500°C using SiC as the microwave absorbent and heating medium. The methyl ricinoleate conversion and UAME yield from microwave-assisted pyrolysis process were higher than those from conventional pyrolysis. The effect of temperature on the pyrolysis process was also investigated. The methyl ricinoleate conversion increased but the cracking liquid yield decreased when the temperature increased from 460°C to 560°C. The maximum UAME yield was obtained at the temperature of 500°C. Copyright © 2015 Elsevier Ltd. All rights reserved.

  9. European dendrochronoloy and C-14 dating of timber

    International Nuclear Information System (INIS)

    Fletcher, J.M.

    1975-01-01

    An account is given of the development of dendrochronology and C-14 dating in Europe. Corrections to raw C-14 dates, sampling and the uncertainty of C-14 ages of wood, and correlation of dates obtained by the two methods, are discussed. (U.K.)

  10. Crystal structure of 3-methyl-2,6-bis(4-methyl-1,3-thiazol-5-ylpiperidin-4-one

    Directory of Open Access Journals (Sweden)

    A. Manimaran

    2014-09-01

    Full Text Available In the title compound, C14H17N3OS2, the central piperidinone ring adopts a chair conformation and the thiazole rings are inclined to its mean plane by 80.16 (12 and 67.15 (12°. The O atom and methyl group C atom deviate significantly from the mean plane of the central piperidinone ring, by 0.8138 (2 and 0.3175 (2 Å, respectively. The dihedral angle between the thiazole rings is 51.88 (13°. In the crystal, molecules are linked via C—H...O hydrogen bonds, forming zigzag C(10 chains running parallel to [001].

  11. Synthesis of /sup 14/C-labelled milrinone

    Energy Technology Data Exchange (ETDEWEB)

    Duncan, D.R.; Johnston, D.; Andrews, R.S. (Stirling-Winthrop, Alnwick (UK). Research and Development Div.)

    1985-02-01

    A synthetic procedure for producing /sup 14/C-labelled milrinone, a potent new cardiotonic agent, is described. The synthesis was achieved in two steps from 1-(4-pyridyl)propan-2-one utilising (2-/sup 14/C)cyanoacetamide as the source of the radiolabel. The overall chemical yield was 46% and the radiochemical yield 35%.

  12. The DSS-14 C-band exciter

    Science.gov (United States)

    Rowan, D. R.

    1989-01-01

    The development and implementation of a C-band exciter for use with the Block IV Receiver-Exciter Subsystem at Deep Space Station 14 (DSS-14) has been completed. The exciter supplements the standard capabilities of the Block IV system by providing a drive signal for the C-band transmitter while generating coherent translation frequencies for C-band (5-GHz) to S-band (2.2- to 2.3-GHz) Doppler extraction, C-band to L-band (1.6-GHz) zero delay measurements, and a level calibrated L-band test signal. Exciter functions are described, and a general explanation and description of the C-band uplink controller is presented.

  13. Effect of level of dietary protein on the distribution of 14C-activity from exogenous 14C-inosine in chicks

    International Nuclear Information System (INIS)

    Masushige, Shoichi; Tadokoro, Tadahiro; Suzuki, Takao; Nakajima, Hisao.

    1983-01-01

    The effect of dietary protein level on the metabolic fate of intraperitoneally administered (exogeneous) 8- 14 C-inosine in chicks was studied. Three different protein level diets (low, standard and high) were prepared. Chicks were fed on these diets for 10 days, respectively and the following results were found: (1) RNA content of liver, small intestine and muscle in chicks fed on a low protein diet was decreased as compared to other diet groups, but no difference was observed in kidney or pancreas. (2) 14 C uptake by organs from exogeneous 8- 14 C-inosine was determined. The uptake of 14 C in kidney, pancreas and small intestine was higher than that in liver and muscle. Moreover, the uptake by tissues in the low protein groups was significantly higher than that in either the standard or high protein groups, but no difference was observed between these latter two groups. (3) The rate of incorporation of 14 C labelled purine by acid soluble materials and RNA was higher in kidney, pancreas and small intestine than in liver and muscle, and also higher in chicks fed on a low protein diet than in either the standard or high protein groups. (4) It was revealed that the 14 C-labelled purine rings from 8- 14 C-inosine were incorporated into AMP and GMP as constituents of RNA. (author)

  14. Microwave Assisted Synthesis and Unusual Coupling of Some Novel Pyrido[3,2-f][1,4]thiazepines

    Directory of Open Access Journals (Sweden)

    Mohamed M. Youssef

    2011-05-01

    Full Text Available 3-Amino-3-thioxopropanamide (1 reacted with ethyl acetoacetate to form 6-hydroxy-4-methyl-2-thioxo-2,3-dihydropyridine-3-carboxamide (2, which reacted with α-haloketones 3 to produce 2,3-disubstituted-8-hydroxy-6-methyl-2H,5H-pyrido[3,2-f]-[1,4]thiazepin-5-ones 4a-c. Benzoylation of 4c led to the formation of the dibenzoate derivative 9. Compounds 4a-c could be prepared stepwise through the formation of S-alkylated derivatives 10a-c. Compounds 2, 4a-c, 9 and 10a-c were prepared using microwave as a source of heat, and gave better yields in shorter times than those achieved by traditional methods. Coupling of 4a-c with arenediazonium chlorides proceeded unusually to give the 6-hydroxy-4-methyl-2-(arylazothieno[2,3-b]pyridin-3(2H-one ring contraction products 14. Structures of the newly synthesized compounds were proven by spectral and chemical methods.

  15. Tissue-specific and cation/anion-specific DNA methylation variations occurred in C. virgata in response to salinity stress.

    Directory of Open Access Journals (Sweden)

    Xiang Gao

    Full Text Available Salinity is a widespread environmental problem limiting productivity and growth of plants. Halophytes which can adapt and resist certain salt stress have various mechanisms to defend the higher salinity and alkalinity, and epigenetic mechanisms especially DNA methylation may play important roles in plant adaptability and plasticity. In this study, we aimed to investigate the different influences of various single salts (NaCl, Na2SO4, NaHCO3, Na2CO3 and their mixed salts on halophyte Chloris. virgata from the DNA methylation prospective, and discover the underlying relationships between specific DNA methylation variations and specific cations/anions through the methylation-sensitive amplification polymorphism analysis. The results showed that the effects on DNA methylation variations of single salts were ranked as follows: Na2CO3> NaHCO3> Na2SO4> NaCl, and their mixed salts exerted tissue-specific effects on C. virgata seedlings. Eight types of DNA methylation variations were detected and defined in C. virgata according to the specific cations/anions existed in stressful solutions; in addition, mix-specific and higher pH-specific bands were the main type in leaves and roots independently. These findings suggested that mixed salts were not the simple combination of single salts. Furthermore, not only single salts but also mixed salts showed tissue-specific and cations/anions-specific DNA methylation variations.

  16. Tissue-specific and cation/anion-specific DNA methylation variations occurred in C. virgata in response to salinity stress.

    Science.gov (United States)

    Gao, Xiang; Cao, Donghui; Liu, Jie; Wang, Xiaoping; Geng, Shujuan; Liu, Bao; Shi, Decheng

    2013-01-01

    Salinity is a widespread environmental problem limiting productivity and growth of plants. Halophytes which can adapt and resist certain salt stress have various mechanisms to defend the higher salinity and alkalinity, and epigenetic mechanisms especially DNA methylation may play important roles in plant adaptability and plasticity. In this study, we aimed to investigate the different influences of various single salts (NaCl, Na2SO4, NaHCO3, Na2CO3) and their mixed salts on halophyte Chloris. virgata from the DNA methylation prospective, and discover the underlying relationships between specific DNA methylation variations and specific cations/anions through the methylation-sensitive amplification polymorphism analysis. The results showed that the effects on DNA methylation variations of single salts were ranked as follows: Na2CO3> NaHCO3> Na2SO4> NaCl, and their mixed salts exerted tissue-specific effects on C. virgata seedlings. Eight types of DNA methylation variations were detected and defined in C. virgata according to the specific cations/anions existed in stressful solutions; in addition, mix-specific and higher pH-specific bands were the main type in leaves and roots independently. These findings suggested that mixed salts were not the simple combination of single salts. Furthermore, not only single salts but also mixed salts showed tissue-specific and cations/anions-specific DNA methylation variations.

  17. Structure of 14C and 14B from the C,1514(d ,3He)B,1413 reactions

    Science.gov (United States)

    Bedoor, S.; Wuosmaa, A. H.; Albers, M.; Alcorta, M.; Almaraz-Calderon, Sergio; Back, B. B.; Bertone, P. F.; Deibel, C. M.; Hoffman, C. R.; Lighthall, J. C.; Marley, S. T.; Mcneel, D. G.; Pardo, R. C.; Rehm, K. E.; Schiffer, J. P.; Shetty, D. V.

    2016-04-01

    We have studied the C,1514(d ,3He)B,1413 proton-removing reactions in inverse kinematics. The (d ,3He ) reaction probes the proton occupation of the target ground state, and also provides spectroscopic information about the final states in B,1413. The experiments were performed using C,1514 beams from the ATLAS accelerator at Argonne National Laboratory. The reaction products were analyzed with the HELIOS device. Angular distributions were obtained for transitions from both reactions. The 14C-beam data reveal transitions to excited states in 13B that suggest configurations with protons outside the π (0 p3 /2) orbital, and some possibility of proton cross-shell 0 p -1 s 0 d excitations, in the 14C ground state. The 15C-beam data confirm the existence of a broad 2- excited state in 14B. The experimental data are compared to the results of shell-model calculations.

  18. Synthesis of 1-benzyl-4-[(5,6-dimethoxy[2-14C]-1-indanon)-2-YL]-methylpiperidine hydrochloride (E2020-14C)

    International Nuclear Information System (INIS)

    Iimura, Youichi; Mishima, Mannen; Sugimoto, Hachiro

    1989-01-01

    1-Benzyl-4-[(5,6-dimethoxy[2- 14 C]-1-indanon)-2-yl]-methylpiperidine hydrochloride (E2020- 14 C), and acetylcholinesterase inhibitor for studying the pharmacokinetic profiles of E2020, was synthesized from 5,6-dimethoxy[2- 14 C]-1-indanone as the labelled starting material. (author)

  19. Temporal interactions in the Lewis lung tumour between cytotoxic drugs and acute or fractionated radiotherapy

    International Nuclear Information System (INIS)

    Stephens, T.C.; Adams, K.; Peacock, J.H.; Steel, G.G.

    1986-01-01

    Lewis lung tumours were treated in vivo with acute radiation (20 Gy) and 1-(2-chloroethyl)-3-(4-methyl cyclohexyl)-1-nitrosourea (MeCCNU, 10 mg . kg -1 ), cyclophosphamide (CY, 120 mg . kg -1 ) or cis-dichlorodiammine platinum (cis-Pt, 10 mg . kg -1 ) with time intervals ranging from simultaneous to 9 days in either sequence. Tumour response was measured by regrowth delay and combination responses were evaluated relative to calculated 'additivity envelopes'. With CY and cis-Pt, tumour volume response was approximately additive, whether the drugs were administered simultaneously, or up to 7 days before or after radiation. However, with simultaneous administration, MeCCNU and radiation were supra-additive in terms of volume response. In the fractionation studies, drugs were given either at the beginning or at the end of a regime of 5 daily 6 Gy doses. With CY and MeCCNU the drugs were more effective when given with the first radiation dose, but with cis-Pt either regime was equally effective. There was no evidence that repopulation could be exploited to improve therapeutic effect with any of the combination treatments used in this study. (Auth.)

  20. Calibration of 14C Histograms : A Comparison of Methods

    NARCIS (Netherlands)

    Stolk, Ad; Törnqvist, Torbjörn E.; Hekhuis, Kilian P.V.; Berendsen, Henk J.A.; Plicht, Johannes van der

    1994-01-01

    The interpretation of C-14 histograms is complicated by the non-linearity of the C-14 time scale in terms of Calendar years, which may result in clustering of C-14 ages in certain time intervals unrelated to the (geologic or archaeologic) phenomenon of interest. One can calibrate C-14 histograms for

  1. Formation and bio release of bound residues of [14 C]-lindane and [14 C]-parathion in two Brazilian soils

    International Nuclear Information System (INIS)

    Andrea, M.M. de.

    1992-01-01

    This work studied the extractable and bound residues formation of 14 C-lindane and 14 C-parathion immediately after application and after 3 months of interaction of the pesticides with the soils. Metabolism, bio release, and the possible bioavailability of bound residues were studied by employing bio meter flasks which allowed a relative comparison of the behaviour of the two different 14 C-pesticides, by a balance of the applied or present radiocarbon in the soils after the bio tests. (author)

  2. {sup 14}C emission from Swedish nuclear power plants and its effect on the {sup 14}C levels in the environment

    Energy Technology Data Exchange (ETDEWEB)

    Stenstroem, K.; Erlandsson, Bengt; Hellborg, R.; Kiisk, M.; Persson, Per [Lund Univ. (Sweden). Dept. of Nuclear Physics; Mattsson, Soeren; Thornberg, C. [Lund Univ., Malmoe (Sweden). Dept. of Radiation Physics; Skog, G. [Lund Univ. (Sweden). Dept. of Quaternary Geology

    2000-02-15

    The radionuclide {sup 14}C is produced in all types of nuclear reactors mainly by neutron induced reactions in oxygen ({sup 17}O), nitrogen ({sup 14}N) and carbon ({sup 13}C). Part of the {sup 14}C created is continuously released during normal operation as airborne effluents in various chemical forms (such as CO{sub 2}, CO and hydrocarbons) to the surroundings. Because of the biological importance of carbon and the long physical half-life of {sup 14}C, it is of interest to measure the releases and their incorporation into living material. The {sup 14}C activity concentrations in annual tree rings and air around two Swedish nuclear power plants (Barsebaeck and Forsmark) as well as the background {sup 14}C activity levels from two reference sites in southern Sweden during 1973-1996 are presented in this report. In order to verify the reliability of the method some investigations have been conducted at two foreign nuclear sites, Sellafield fuel reprocessing plant in England, and Pickering nuclear generating station in Canada, where the releases of {sup 14}C are known to be substantial. Furthermore, results from some measurements in the vicinity of Paldiski submarine training centre in Estonia are presented. The results of the {sup 14}C measurements of air, vegetation and annual tree rings around the two Swedish nuclear power plants show very low enhancements of {sup 14}C, if at all above the uncertainty of the measurements. Even if the accuracy of the measurements of the annual tree rings is rather good (1-2%) the contribution of {sup 14}C from the reactors to the environment is so small that it is difficult to separate it from the prevailing background levels of {sup 14}C . This is the case for all sampling procedures: in air and vegetation as well as in annual tree rings. Only on a few occasions an actual increase is observed. However, although the calculations suffer from rather large uncertainties, the calculated release rate from Barsebaeck is in fair agreement

  3. Methylation-associated down-regulation of RASSF1A and up-regulation of RASSF1C in pancreatic endocrine tumors

    International Nuclear Information System (INIS)

    Malpeli, Giorgio; Amato, Eliana; Dandrea, Mario; Fumagalli, Caterina; Debattisti, Valentina; Boninsegna, Letizia; Pelosi, Giuseppe; Falconi, Massimo; Scarpa, Aldo

    2011-01-01

    RASSF1A gene silencing by DNA methylation has been suggested as a major event in pancreatic endocrine tumor (PET) but RASSF1A expression has never been studied. The RASSF1 locus contains two CpG islands (A and C) and generates seven transcripts (RASSF1A-RASSF1G) by differential promoter usage and alternative splicing. We studied 20 primary PETs, their matched normal pancreas and three PET cell lines for the (i) methylation status of the RASSF1 CpG islands using methylation-specific PCR and pyrosequencing and (ii) expression of RASSF1 isoforms by quantitative RT-PCR in 13 cases. CpG island A methylation was evaluated by methylation-specific PCR (MSP) and by quantitative methylation-specific PCR (qMSP); pyrosequencing was applied to quantify the methylation of 51 CpGs also encompassing those explored by MSP and qMSP approaches. MSP detected methylation in 16/20 (80%) PETs and 13/20 (65%) normal pancreas. At qMSP, 11/20 PETs (55%) and 9/20 (45%) normals were methylated in at least 20% of RASSF1A alleles. Pyrosequencing showed variable distribution and levels of methylation within and among samples, with PETs having average methylation higher than normals in 15/20 (75%) cases (P = 0.01). The evaluation of mRNA expression of RASSF1 variants showed that: i) RASSF1A was always expressed in PET and normal tissues, but it was, on average, expressed 6.8 times less in PET (P = 0.003); ii) RASSF1A methylation inversely correlated with its expression; iii) RASSF1 isoforms were rarely found, except for RASSF1B that was always expressed and RASSF1C whose expression was 11.4 times higher in PET than in normal tissue (P = 0.001). A correlation between RASSF1A expression and gene methylation was found in two of the three PET cell lines, which also showed a significant increase in RASSF1A expression upon demethylating treatment. RASSF1A gene methylation in PET is higher than normal pancreas in no more than 75% of cases and as such it cannot be considered a marker for this neoplasm

  4. Boron-Catalyzed C3-Polymerization of ω-2-Methyl Allylarsonium Ylide and Its C3/C1 Copolymers with Dimethylsulfoxonium Methylide

    KAUST Repository

    Wang, De

    2016-03-01

    A novel arsonium ylide, ω-2-methylallylarsonium ylide, was synthesized and used as monomer for polyhomologation with triethyborane as initiator. It was found that the terminal methyl group leads to C3 polymerization. Furthermore, the copolyhomologation of arsonium ylide with dimethylsulfoxonium methylide is reported for the first time. (Chemical Equation Presented). © 2016 American Chemical Society.

  5. 1,4-Disilacyclohexa-2,5-diene

    DEFF Research Database (Denmark)

    Tibbelin, Julius; Wallner, Andreas; Emanuelsson, Rikard

    2014-01-01

    2,3,5,6-Tetraethyl-1,4-disilacyclohexa-2,5-dienes with either four chloro (1a), methyl (1b), or trimethylsilyl (TMS) (1c) substituents at the two silicon atoms were examined in an effort to design rigid compounds with strong neutral cross-hyperconjugation between π- and σ-bonded molecular segments......). Furthermore, 1,4-disilacyclohexadiene 1c absorbs strongly at 273 nm (4.55 eV), whereas 1a and 1b have no symmetry allowed excitations above 215 nm (below 5.77 eV). Thus, suitably substituted 1,4-disilacyclohexa-2,5-dienes could represent novel building blocks for the design of larger cross...

  6. How accurate is the 14C method

    International Nuclear Information System (INIS)

    Nydal, R.

    1979-01-01

    Radiocarbon daters have in recent years focussed their interest on accuracy and reliability of 14 C dates. The use of dates for resolving fine chronological structures that are not dateable otherwise has stressed this point. The total uncertainty in dating an event is composed of errors relating to dating of the sample, i.e. uncertainty in measured quantities, deviations from assumed content of 14 C in material when alive; and errors related to quality of sample material, i.e. contamination from carbon of different age, diffuse context between sample and event. Statistical variability in counting of 14 C activity gives the most important contribution to measurement uncertainty - increasing with age and shortage of sample material. Corrections for isotopic fractionation and reservoir effects must be performed, and - most important when dates are compared with historical ages - the dendrochronological calibration will correct for past variations in the atmospheric 14 C content. Future improvement of dating precision can however only be obtained by the combined efforts of both daters and submitters of samples, thus minimizing errors related to selection and handling of sample material as well as those related to the 14 C method and measurements. (Auth.)

  7. Clinical investigation of 14C-urea breath test

    International Nuclear Information System (INIS)

    Yu Yongli; Zhu Ruisen; Ji Hong; Luo Quanyong

    2000-01-01

    To investigate clinical value of 14 C-urea breath test ( 14 C-UBT) for the diagnosis of Helicobacter pylori(Hp), 70 patients were both performed gastroscopy (taking gastric mucosae biopsy for rapid urease test and histology) and 14 C-UBT (some patients by Hp-IgG or DNAHp test also) within two days. The positive cases of both rapid urease test and histology was defined as 'gold standard' of Hp-positive, whereas the negative cases of both rapid urease test and histology as 'gold standard' of Hp-negative. The sensitivity of 14 C-UBT was 93.2%, the specificity 73.1%, and the diagnostic accuracy 85.7%. The difference (comparing with 'gold standard') was not marked (x 2 = 0.9 0.05(1) 2 = 3.84, P>0.05). But the diagnostic accuracy of 14 C-UBT (85.7%) and Hp-IgG (50%) had a marked difference (x 2 13.80>x 0.01(1) 2 = 6.64, P 14 C-UBT was easy to operate, reliable and suitable for clinical application

  8. Rac1 plays a role in CXCL12 but not CCL3-induced chemotaxis and Rac1 GEF inhibitor NSC23766 has off target effects on CXCR4.

    Science.gov (United States)

    Mills, Shirley C; Howell, Lesley; Beekman, Andrew; Stokes, Leanne; Mueller, Anja

    2018-01-01

    Cell migration towards a chemotactic stimulus relies on the re-arrangement of the cytoskeleton, which is triggered by activation of small G proteins RhoA, Rac1 and Cdc42, and leads to formation of lamellopodia and actin polymerisation amongst other effects. Here we show that Rac1 is important for CXCR4 induced chemotaxis but not for CCR1/CCR5 induced chemotaxis. For CXCL12-induced migration via CXCR4, breast cancer MCF-7 cells are reliant on Rac1, similarly to THP-1 monocytes and Jurkat T-cells. For CCL3-induced migration via CCR1 and/or CCR5, Rac1 signalling does not regulate cell migration in either suspension or adherent cells. We have confirmed the involvement of Rac1 with the use of a specific Rac1 blocking peptide. We also used a Rac1 inhibitor EHT 1864 and a Rac1-GEF inhibitor NSC23766 to probe the importance of Rac1 in chemotaxis. Both inhibitors did not block CCL3-induced chemotaxis, but they were able to block CXCL12-induced chemotaxis. This confirms that Rac1 activation is not essential for CCL3-induced migration, however NSC23766 might have secondary effects on CXCR4. This small molecule exhibits agonistic features in internalisation and cAMP assays, whereas it acts as an antagonist for CXCR4 in migration and calcium release assays. Our findings strongly suggest that Rac1 activation is not necessary for CCL3 signalling, and reveal that NSC23766 could be a novel CXCR4 receptor ligand. Crown Copyright © 2017. Published by Elsevier Inc. All rights reserved.

  9. Fate of 14C-labelled compounds in marine environment

    International Nuclear Information System (INIS)

    Kale, S.P.; Raghu, K.; Sherkhane, P.D.; Murthy, N.B.K.

    1999-01-01

    Model ecosystems have played an important role in predicting environmental behavior of agrochemicals. The microcosms used in these studies generally include soil units containing usual biotic components common for that ecosystem. In present studies, scope of two such ecosystems has been extended to study the fate of 14 C-labelled pesticides in marine environment. 14 C-labelled pesticides used in these studies were chlorpyrifos, DDT and HCH. Two systems were developed in laboratory simulating marine environment to study the fate of these pesticides. The first system was developed in an all glass aquarium tank with marine sediments, seawater, clams and algae and is referred to as marine ecosystem. The second system was developed to permit the total 14 C-mass balance studies. It contained marine sediments under moist (60% water holding capacity) or flooded conditions and it is referred to as continuous flow system. Fate of 14 C-DDT was studied in marine ecosystem while degradation of 14 C-chlorpyrifos and 14 C-HCH was studied in continuous flow system. 14 C-DDT did not bioaccumulate in clams while at the end of 60 days 50% of the applied 14 C-activity was present in sediment fraction of marine ecosystem. 14 C-HCH degradation showed about 22-26% mineralization while 45-55% of the applied activity was recovered as organic volatiles. No significant bound residues were formed. 14 C-chorpyrifos underwent considerable degradation in marine environment. TCP was the major degradation product. (author)

  10. Mild synthesis of [N-methyl-11C]-isovaleroyl-(L)-carnitine. The usefulness of a tritium approach

    International Nuclear Information System (INIS)

    Angelini, G.; Carnevaletti, F.; Margonelli, A.; Corsi, G.; Ragni, P.; Fazio, F.; Todde, S.; Tinti, O.

    1999-01-01

    The title carnitine derivative was labelled both with [ 11 C]methyl iodide and [ 3 H]methyl iodide. The former was synthesized in order to improve the knowledge of the acyl carnitines fate in humans. The latter was synthesized, at approximately the same concentration level as that of the former, in order to optimize its radiosynthesis, taking advantage from the long half-life of the tritium

  11. Effect of two organophosphorus insecticides on the growth, respiration and (/sup 14/C)-glucose metabolism of Azobacter chroococcum Beij

    Energy Technology Data Exchange (ETDEWEB)

    Balasubramanian, A; Narayanan, R [Tamil Nadu Agricultural Univ., Coimbatore (India)

    1980-01-01

    The two organophosphorus insecticides, commonly applied to soil, viz., disulfoton (0,0-diethyl S-2-ethyl thio ethyl phosphorodithioate) and fensulfothion (0,0-diethyl 0-4-methyl sulphinyl phenyl phosphorothioate) did not affect the in vitro growth of Azotobacter chroococcum Beij., the free-living, nitrogen fixing soil bacterium, at 2 ppm (lower level), while the normal dose (5 ppm) and the higher level (10 ppm) suppressed the growth. Respiration of the organism (glucose oxidation) was adversely affected by the insecticides in the growth medium and the inhibition increased with the concentration of the chemical. Both the insecticides suppressed the assimilation of (/sup 14/C)-glucose in the cold-TCA soluble, hot-TCA soluble fractions and insoluble residue of the cells whereas the /sup 14/C-incorporation in the alcohol soluble and alcohol-ether soluble fractions was enhanced indicating that the insecticides considerably altered the glucose metabolism of the bacterium.

  12. Radioactive waste with 14C in Argentina

    International Nuclear Information System (INIS)

    Di Lello, D.S.

    2009-01-01

    14 C is a long half-life radioisotope, which is present in radioactive waste generated during the operation and decommissioning of nuclear power plants. 14 C can also be found in waste generated by medical diagnostic laboratories or any one generated by fields that deal with research and development (mainly connected with the biochemists area). According to international precedents the disposal of 14 C based on the final amount found in radioactive waste and its chemical form have conditioned the design and operation of the facilities (either because of the amount of it or the chemical form in which 14 C was present). We have to take into account that the design of facilities for radioactive waste disposal is included among the obligations of the National Radioactive Waste Management Program (PNGRR). It is absolutely necessary to count with enough information about the characteristics of any waste containing 14 C that is generated in Argentina, in order to be able to fulfil the requirements previously mentioned. The main characteristics of interest in the frame of the present project are: a) the principal reactions that take place for the formation of 14 C; b) The specific concentration of activity in materials where this radio nuclei is formed or is accumulated; c) To know which is the current step in the process of managing these wastes (in Argentina and all over the world). Either if it refers to bulk or conditioned storage, inside the generating facility; d) Transportation possibilities of 14 C under these conditions; e) The accumulated volume and the generation rate of this kind of waste in Argentina. This paper presents an initial collection and evaluation of the information related to the characteristics already mentioned, having gathered published material from the literature and information in the PNGRR up to this moment. The description of the characteristics of the radioactive waste containing 14 C from nuclear power plants, hospitals and research and

  13. Dicty_cDB: Contig-U16385-1 [Dicty_cDB

    Lifescience Database Archive (English)

    Full Text Available rrifsnl*kv***iynv*kg fgn*kih*r*inskke*kgekrngd*kieigndsfeikenwftfilq*nsc***iitnlf hkfsgsst***r*rnyqrvyq*sksi...knstrrifsnl*kv***iynv*kg fgn*kih*r*inskke*kgekrngd*kieigndsfeikenwftfilq*nsc***iitnlf hkfsgsst***r*rnyqrvyq*

  14. Microalgal fatty acid methyl ester a new source of bioactive compounds with antimicrobial activity

    Directory of Open Access Journals (Sweden)

    Arumugham Suresh

    2014-09-01

    Full Text Available Objective: To evaluate fatty acid composition and the antimicrobial activity of the major fraction of fatty acid methyl ester (FAME extracts from three microalgae collected from freshwater lakes in Theni District, Tamil Nadu, India. Methods: Antimicrobial study was carried out by well diffusion method against bacterial as well as fungal pathogens such as Escherichia coli, Staphylococcus aureus, Enterobacter sp., Klebsiella sp., Salmonella typhi, Fusarium sp., Cryptococcus sp., Candida sp., and Aspergillus niger and Aspergillus flavus. The FAME profiles were determined through gas chromatography with a flame ionization detector. Results: The FAME was found to be radial effective in inhibiting the radial growth of both bacterial and fungal pathogens. The FAME extracts exhibited the antibacterial activity against three clinical pathogens, namely, Escherichia coli, Salmonella typhi and Enterobacter sp. with the maximum zone of inhibition of 12.0 mm, 12.0 mm and 11.0 mm, respectively. The FAME showed moderate antifungal activity against Cryptococcus sp. (11.8 mm, Aspergillus niger (10.5 mm, Candida sp. (11.8 mm and Fusarium sp. (10.4 mm. Gas chromatography-flame ionization detector analysis revealed about 30 different FAMEs. Conclusions: We assume that the observed antimicrobial potency may be due to the abundance of erucic acid methyl ester (C22:0, arachidic acid methyl ester (C20:0, palmitic acid methyl ester (C16:0, cis-11-eicosenoicmethyl ester (C20:1, cis-11, 14-eicosadienoic acid methyl ester (C20:2 and linolenic acid methyl ester (C18:3 in FAMEs which appears to be promising to treat microbial diseases.

  15. Studies on dissipation and degradation of 14 C-DDT and 14 C-parathion in egyptian soil under field conditions

    International Nuclear Information System (INIS)

    Ezz El-Arab, A.; Mostafa, I.Y.

    1991-01-01

    The rates of dissipation and degradation of the insecticides DDT and parathion were studied under field conditionsm using 14 C-labelled chemicals. Over a period of 12 weeks, extractable, soil-bound and total 14 C-activity were recorded. In case of DDT, dissipation of 14 C-activity from soil showed a continuous and gradual increase reaching about 30% after 8 weeks and remained constant up to 12 weeks. The formation of DDE as a principal metabolite seems to be increasing with time ans accounted for approximately 25% of the extractable residues after 12 weeks. There was also a gradual significant increase in the formation of soil 14 C-bound residues which reached 12% of the total residues after the same period. On the other hand, parathion dissipation from the soil under the same conditions did not exceed 10% up to 12 weeks. The amount of 14 C-bound residues was found to contribute 33% of the applied dose. Analysis of the extractable fraction revealed that parathion was partly degraded by soil microorganisms into p-amino phenol, p-nitrophenol, paraoxon, amino parathion and aminoparaoxon in different percentages depending on the depth of soil. 2 fig.,1 tab

  16. 14C Carbofuran residue in rice-fish ecosystem model

    International Nuclear Information System (INIS)

    Sumatra, M.; Soekarna, D.; Suhanda; Kuswadi, A.N.

    1988-01-01

    14-C-carbofuran in the form of 14-C-Furada 3G was applied with doses of 0, 2, and 4 g/m2 to a rice-fish ecosystem model consisting of water, soil, rice, plant, and fish (Cyprinus carpio) in tanks of the size 1 m length, 1 m width, and 0.5 m depth. 14-C-carbofuran was released from 14-C-Furadan 3G, entered into the water, absorbed by plant root, and then distributed into the whole plant. A part of the 14-C-carbofuran was absorbed and retained by soil. In both doses of 4 and 2 g/m2, the 14-C-Furadan 3G was toxic to Cyprinus carpio under this experiment condition. (author). 5 refs, 5 figs, 6 tabs

  17. Effects of Qi-Fang-Xi-Bi-Granules on Cartilage Morphology and C/ebpα Promoter Methylation in Rats with Knee Osteoarthritis

    Directory of Open Access Journals (Sweden)

    Xinxin Wang

    2018-01-01

    Full Text Available Objective. To investigate the effects of Qi-Fang-Xi-Bi-Granules (QFXBGs on cartilage morphology and methylation of C/ebpα (CCAAT/enhancer binding proteinα at the promoter region. Methods. Knee osteoarthritis (KOA modeling was performed in rats in accordance with Hulth’s method, and control group received sham operation. Eight weeks after KOA modeling, the rats in the KOA modeling group were further divided into 6 groups. Each group was given the appropriate drug. After 8 weeks, half of the rats were used for Micro-CT scan, HE staining, ABH/OG staining, immunohistochemistry, and TUNNEL staining of the knee joint tissue, and the other half were used to examine C/ebpα promoter methylation. Results. The three dose groups of QFXBGs all showed lower degrees of surface fissures and flaking, thicker cartilage layer, and restored chondrocyte and subchondral bone morphology, compared with the KOA model group. C/ebpα-22 promoter methylation levels in the high- and low-dose groups were significantly higher than that in the KOA modeling group (p<0.05, while C/ebpα-2 promoter methylation level in the medium-dose group was significantly higher than that in the KOA modeling group (p<0.05. Conclusions. QFXBGs may alleviate articular cartilage degeneration through promoting C/ebpα-2 or C/ebpα-22 methylation at specific promoter sites.

  18. The automated radiosynthesis and purification of the opioid receptor antagonist, [6-O-methyl-11C]diprenorphine on the GE TRACERlab FXFE radiochemistry module.

    Science.gov (United States)

    Fairclough, Michael; Prenant, Christian; Brown, Gavin; McMahon, Adam; Lowe, Jonathan; Jones, Anthony

    2014-05-15

    [6-O-Methyl-(11)C]diprenorphine ([(11)C]diprenorphine) is a positron emission tomography ligand used to probe the endogenous opioid system in vivo. Diprenorphine acts as an antagonist at all of the opioid receptor subtypes, that is, μ (mu), κ (kappa) and δ (delta). The radiosynthesis of [(11)C]diprenorphine using [(11)C]methyl iodide produced via the 'wet' method on a home-built automated radiosynthesis set-up has been described previously. Here, we describe a modified synthetic method to [(11)C]diprenorphine performed using [(11)C]methyl iodide produced via the gas phase method on a GE TRACERlab FXFE radiochemistry module. Also described is the use of [(11)C]methyl triflate as the carbon-11 methylating agent for the [(11)C]diprenorphine syntheses. [(11)C]Diprenorphine was produced to good manufacturing practice standards for use in a clinical setting. In comparison to previously reported [(11)C]diprenorphine radiosyntheisis, the method described herein gives a higher specific activity product which is advantageous for receptor occupancy studies. The radiochemical purity of [(11)C]diprenorphine is similar to what has been reported previously, although the radiochemical yield produced in the method described herein is reduced, an issue that is inherent in the gas phase radiosynthesis of [(11)C]methyl iodide. The yields of [(11)C]diprenorphine are nonetheless sufficient for clinical research applications. Other advantages of the method described herein are an improvement to both reproducibility and reliability of the production as well as simplification of the purification and formulation steps. We suggest that our automated radiochemistry route to [(11)C]diprenorphine should be the method of choice for routine [(11)C]diprenorphine productions for positron emission tomography studies, and the production process could easily be transferred to other radiochemistry modules such as the TRACERlab FX C pro. Copyright © 2014 John Wiley & Sons, Ltd.

  19. Solvent effect on the rate and equilibrium of reaction between 10-phenylphenoxarsine and methyl iodide

    International Nuclear Information System (INIS)

    Gavrilov, V.I.; Gumerov, N.S.; Rakhmatullin, R.R.

    1990-01-01

    Effect of solvent nature on nucleophilic capacity of three-coordinated arsenic and the equilibrium state of 10-phenylphenoxarsine (PA) reaction with methyl iodide are studied. Kinetic investigations are carried out by the conductometry at 24,35,45 deg C. It is established that quaternization of PA with methyl iodide when substituting a solvent (ketone for alcohol) increases 3-14 times with simultaneous growth of the activation energy value. When transforming from aprotic solvents to protic ones PA interaction equilibrium with methyl iodide shifts to the side of arsonic salt formation

  20. 14C-Methylenebisphenylisocyanate (14C-MDI). Study of absorption after single dermal and intradermal administration in rats

    International Nuclear Information System (INIS)

    Leibold, E.; Hoffmann, H.D.; Hildebrand, B.

    1999-01-01

    The absorption, distribution and excretion of radioactivity was studied in groups of four male Wistar rats following a single dermal and intradermal administration of 14 C- Methylenebisphenylisocyanate ( 14 C-MDI) at nominal dose levels of 4.0 and 0.4 mg/cm 2 for dermal administration and 0.4 mg/animal for intradermal administration. These dose levels nominally corresponded to 40 and 4.0 mg/animal for dermal administration. Considering the animal weights, dose levels corresponded to about 140 and 14 mg/kg body weight (dermal administration) and 1.4 mg/kg body weight (intradermal administration). In the experiments with dermal administration, animals were exposed for 8 hours and sacrificed 8, 24 or 120 h after beginning of exposure. In the experiment with intradermal administration, animals were sacrificed 120 h after treatment. After dermal administration of 14 C-MDI, mean recoveries of radioactivity from all dose groups were in the range from 97.86 to 108.07% of the total radioactivity administered. Generally, the largest proportion of radioactivity was found at the application site and dressing. The total amount of radioactivity absorbed (including excreta, cage wash, tissues/organs and carcass) increased with increasing sacrifice time. Dermal absorption was very low and quantitatively similar at both dose levels; maximally ca. 0.9 % of the applied radioactivity was absorbed. After intradermal administration of 14 C-MDI, the mean recovery of radioactivity was 100.90 % of the radioactivity administered. The largest proportion of radioactivity was found at the application site. The total amount of radioactivity absorbed (including excreta, cage wash, tissues/organs and carcass) amounted to about 26 % of the radioactivity applied. Irrespective of the mode of administration of 1 4C -MDI, concentrations of radioactivity in tissues and organs generally were below 1 μg Eq/g at 120 h after administration. In summary, the results of this study comparing systemic

  1. Effect of alcohol consumption on the liver detoxication capacity as measured by [13C]methacetin- and [methyl-13C]methionine-breath tests.

    Science.gov (United States)

    Wutzke, Klaus D; Forberger, Anke; Wigger, Marianne

    2008-06-01

    The aim of this study was to investigate the hepatic microsomal and mitochondrial functions by using the 13CO2-breath test in healthy subjects either before or after the consumption of red wine. Fourteen adults received [13C]methacetin and [methyl-13C]methionine together with a standardised dinner. Expired air samples were taken over 6 h. After a wash-out period, the subjects consumed 0.4 ml ethanol/kg/day together with dinner over a 10-day period. Thereafter, 13C-tracer administration was repeated under identical conditions. The 13CO2-enrichments were measured by isotope ratio mass spectrometry. The mean cumulative percentage 13C-dose recovery (CPDR) after administration of [13C]methacetin and [methyl-13C]methionine either without or with red wine consumption amounted to 38.2+/-6.3 vs. 36.3+/-6.7% (p=0.363) and 9.5+/-3.3 vs. 8.8+/-2.5% (p=0.47), respectively. Moderate alcohol consumption does not induce significant short-term changes of the microsomal and the mitochondrial functions of the human liver in healthy subjects.

  2. Application of AMS 14C measurements to criminal investigations

    International Nuclear Information System (INIS)

    Nakamura, T.; Ohta, T.; Nishida, M.; Rakowski, A.; Ikeda, A.; Oda, H.; Kojima, S.

    2007-01-01

    14 C variations of atmospheric CO 2 as well as carbonaceous fraction of living materials, such as collagen from tooth and bone, tissue, skin, hair, nail, etc., of modern humans are influenced by 14 C produced artificially by nuclear bomb tests in the atmosphere from late 1950s to early 1960s. By careful investigation of 14 C concentration of tree rings and human body samples formed in this time intervals, we can establish a relationship of their 14 C concentrations with calendar year. By applying this relation to a sample whose 14 C concentration can be measured, we can estimate the formation age of the sample. In addition, sources of the chemicals that were used in some criminal cases can be possibly identified, by their carbon isotope ratios ( 13 C/ 12 C and 14 C/ 12 C). This method of age determination has been applied to a forensic study, i.e., two criminal cases of murder. For each case, by comparing the measured 14 C abundances of several pieces of hair and one tooth (the third molar) from the body with the annual change on concentrations of bomb-produced 14 C, the time of death of the body and the age of the victim were estimated. The estimated values were consistent with the real ones that were revealed by the confession of the real murderers. (author)

  3. {8-14C}-Adenine and {1-14C}-isopentenyl pyrophosphate - precursors for root-produced cytokinins in the tomato (Lycopersicon esculentum mill.)

    International Nuclear Information System (INIS)

    Dickinson, J.R.

    1985-01-01

    Following the detection of reasonable levels of biologically active cytokinin-like compounds in one-month-old tomato plants, the possible involvement of {8- 14 C}-adenine and {1- 14 C}-isopentenyl pyrophosphate in the biosynthetic pathway leading to an accumulation of free zeatin derivatives, was studied. Intact tomato plants were used for a time-course study involving the uptake of {8- 14 C}-adenine and the tentative identification of compounds into which the 14 C became incorporated. Using high performance liquid chromatography, radioactive trans-zeatin was identified as being present in the Dowex 50 root extract. The 12-hour time interval was used and the roots of the tomato plants were immersed in a more heavily radiolabelled medium. Modified separation techniques were used to achieve enhanced radioactivity recovery rates. This experiment demonstrated the presence of relatively high levels of tentatively identified radioactive zeatin in the Dowex 50 root and stem extracts. Radioactivity in the aqueous extracts was found not to be contributed by cytokinin nucleotides. A final experiment was carried out using decapitated root systems to determine if the root tissue alone could be implicated in the synthesis of cytokinins. Decapitated tomato root systems were supplied with either {8- 14 C}-adenine or {1- 14 C}-isopentenyl pyrophosphate. The ratio of incorporation of {1- 14 C}-isopentenyl pyrophosphate into identified cytokinins was higher than for {8- 14 C}-adenine. It was concluded that both adenine and isopentenyl pyrophosphate are involved in the biosynthetic pathway leading to an accumulation of free zeatin derivatives in tomato roots

  4. A comparative estimation of C.I. engine fuelled with methyl esters of punnai, neem and waste cooking oil

    Energy Technology Data Exchange (ETDEWEB)

    Subramaniam, D.; Avinash, A. [Department of Mechanical Engineering - K.S.Rangasamy College of Technology –Tiruchengode, 637215 Tamil Nadu (India); Murugesan, A. [Department of Mechatronics Engineering - K.S.Rangasamy College of Technology – Tiruchengode, 637215 Tamil Nadu (India)

    2013-07-01

    In this experimental study, performance, emission, and combustion characteristics of methyl esters of Punnai, Neem, Waste Cooking Oil and their diesel blends in a C.I. engine was experimentally examined. For the study, Punnai oil methyl esters (POME), neem oil methyl esters (NOME), and Waste Cooking Oil Methyl Esters (WCOME) were prepared by tranesterification process. The Bio diesel-diesel blends were prepared by mixing 10%, 30%, 50%, and 70% of bio diesel with diesel. The effects of three methyl esters and their diesel blends on engine performance, combustion, and exhaust emissions were examined at different engine loads. Experimental results concluded that up to 30% of methyl esters did not affect the performance, combustion, and emissions characteristics. On the other hand, above B30 (30% Bio diesel with 70% diesel) a reduction in performance, combustion, and emission characteristics were clear from the study.

  5. Analysis of DNA Methylation of Gracilariopsis lemaneiformis Under Temperature Stress Using the Methylation Sensitive Amplification Polymorphism (MSAP) Technique

    Science.gov (United States)

    Peng, Chong; Sui, Zhenghong; Zhou, Wei; Hu, Yiyi; Mi, Ping; Jiang, Minjie; Li, Xiaodong; Ruan, Xudong

    2018-06-01

    Gracilariopsis lemaneiformis is an economically important agarophyte, which contains high quality gel and shows a high growth rate. Wild population of G. lemaneiformis displayed resident divergence, though with a low genetic diversity as was revealed by amplified fragment length polymorphism (AFLP) and simple sequence repeat (SSR) analyses. In addition, different strains of G. lemaneiformis are diverse in morphology. The highly inconsistence between genetic background and physiological characteristics recommends strongly to the regulation at epigenetic level. In this study, the DNA methylation change in G. lemaneiformis among different generation branches and under different temperature stresses was assessed using methylation sensitive amplified polymorphism (MSAP) technique. It was shown that DNA methylation level among different generation branches was diverse. The full and total methylated DNA level was the lowest in the second generation branch and the highest in the third generation. The total methylation level was 61.11%, 60.88% and 64.12% at 15°C, 22°C and 26°C, respectively. Compared with the control group (22°C), the fully methylated and totally methylated ratios were increased in both experiment groups (15°C and 26°C). All of the cytosine methylation/demethylation transform (CMDT) was further analyzed. High temperature treatment could induce more CMDT than low temperature treatment did.

  6. Magnitude of 14C/12C variations based on archaeological samples

    International Nuclear Information System (INIS)

    Kusumgar, S.; Agrawal, D.P.

    1977-01-01

    The magnitude of 14 C/ 12 C variations in the period A.D. 5O0 to 200 B.C. and 370 B.C. to 2900 B.C. is discussed. The 14 C dates of well-dated archaeological samples from India and Egypt do not show any significant divergence from the historical ages. On the other hand, the corrections based on dendrochronological samples show marked deviations for the same time period. A plea is, therefore, made to study old tree samples from Anatolia and Irish bogs and archaeological samples from west Asia to arrive at a more realistic calibration curve. (author)

  7. [Variation of long-chain 3-hydroxyacyl-CoA dehydrogenase DNA methylation in placenta of different preeclampsia-like mouse models].

    Science.gov (United States)

    Han, Yiwei; Yang, Zi; Ding, Xiaoyan; Yu, Huan; Yi, Yanhong

    2015-10-01

    By detecting the variation of long-chain 3-hydroxyacyl-CoA dehydrogenase (LCHAD) DNA methylation in preeclampsia-like mouse models generated by different ways, to explore the roles of multifactor and multiple pathways in preeclampsia pathogenesis on molecular basis. Established preeclampsia-like mouse models in different ways and divided into groups as follows: (1) Nw-nitro-L-arginine-methyl ester (L-NAME) group: wild-type pregnant mouse received subcutaneous injection of L-NAME; (2) lipopolysaccharide (LPS) group: wild-type pregnant mouse received intraperitoneal injection of LPS; (3) apolipoprotein C-III (ApoC3) group: ApoC3 transgenic pregnant mouse with dysregulated lipid metabolism received subcutaneous injection of L-NAME; (4) β2 glycoprotein I (β-2GPI) group: wild-type pregnant mouse received subcutaneous injection of β-2GPI. According to the first injection time (on day 3, 11, 16 respectively), the L-NAME, LPS and ApoC3 groups were further subdivided into: pre-implantation (PI) experimental stage, early gestation (EG) experimental stage, and late gestation (LG) experimental stage. β-2GPI group was only injected before implantation. LCHAD gene methylation levels in placental were detected in different experimental stage. Normal saline control groups were set within wild-type and ApoC3 transgenic pregnant mice simultaneously. (1) CG sites in LCHAD DNA: 45 CG sites were detected in the range of 728 bp before LCHAD gene transcription start site, the 5, 12, 13, 14, 15, 16, 19, 24, 25, 27, 28, 29, 30, 31, 32, 34, 35, 43 CG sites were complex sites which contained two or more CG sequences, others were single site which contained one CG sequence. The 3, 5, 6, 11, 13, 14, 18, 28 sites in L-NAME, LPS, ApoC3 and β-2GPI groups showed different high levels of methylation; the 16, 25, 31, 42, 44 sites showed different low levels of methylation; other 32 sites were unmethylated. (2) Comparison of LCHAD gene methylation between different groups: the methylation levels

  8. DNA methylation in inflammatory genes among children with obstructive sleep apnea.

    Science.gov (United States)

    Kim, Jinkwan; Bhattacharjee, Rakesh; Khalyfa, Abdelnaby; Kheirandish-Gozal, Leila; Capdevila, Oscar Sans; Wang, Yang; Gozal, David

    2012-02-01

    Pediatric obstructive sleep apnea (OSA) leads to multiple end-organ morbidities that are mediated by the cumulative burden of oxidative stress and inflammation. Because not all children with OSA exhibit increased systemic inflammation, genetic and environmental factors may be affecting patterns of DNA methylation in genes subserving inflammatory functions. DNA from matched children with OSA with and without high levels of high-sensitivity C-reactive protein (hsCRP) were assessed for DNA methylation levels of 24 inflammatory-related genes. Primer-based polymerase chain reaction assays in a case-control setting involving 47 OSA cases and 31 control subjects were conducted to confirm the findings; hsCRP and myeloid-related protein (MRP) 8/14 levels were also assayed. Forkhead box P3 (FOXP3) and interferon regulatory factor 1 (IRF1) showed higher methylation in six children with OSA and high hsCRP levels compared with matched children with OSA and low hsCRP levels (P DNA methylation levels compared with children with OSA and low CRP levels and control subjects. IRF1 did not exhibit significant differences. FOXP3 DNA methylation levels correlated with hsCRP and MRP 8/14 levels and with apnea-hypopnea index (AHI), BMI z score, and apolipoprotein B levels. A stepwise multiple regression model showed that AHI was independently associated with FOXP3 DNA methylation levels (P gene, which regulates expression of T regulatory lymphocytes, is more likely to display increased methylation among children with OSA who exhibit increased systemic inflammatory responses. Thus, epigenetic modifications may constitute an important determinant of inflammatory phenotype in OSA, and FOXP3 DNA methylation levels may provide a potential biomarker for end-organ vulnerability.

  9. Preparation and HPLC isolation of L-[U-14C]tryptophan from enzyme hydrolysate labelled with 14C

    International Nuclear Information System (INIS)

    Novak, J.; Tintera, S.; Hromadkova, B.

    1990-01-01

    Tryptophan was obtained from biomass of the blue-green alga Synechococcus elongatus cultivated under 14 CO 2 . After partial purification, the protein fraction was subjected to enzymatic hydrolysis using pronase. Semipreparative isolation of L-[U- 14 C]tryptophan was accomplished on a HPLC column of Separon S Hema 1000 CM, 2% ethanol were added to the eluent, and a precolumn packed with the basic anion exchanger Spheron 1000 DEAE was used. Always after the passage of L-[U- 14 C]tryptophan, the precolumn was decoupled. The substance was collected in 96% ethanol. After removing the solvent by vacuum evaporation, the sample was analyzed on a column packed with Separon SIX C 18 in the eluent of 0.1M-NaH 2 PO 4 , 2% methanol. When the desired radiochemical purity was not attained, the sample was purified on Separon SIX C 18 using 2% methanol. The final radiochemical purity achieved by using this method is 98%. (P.A.). 5 figs., 2 tabs., 4 refs

  10. Methylation-sensitive amplified polymorphism-based genome-wide analysis of cytosine methylation profiles in Nicotiana tabacum cultivars.

    Science.gov (United States)

    Jiao, J; Wu, J; Lv, Z; Sun, C; Gao, L; Yan, X; Cui, L; Tang, Z; Yan, B; Jia, Y

    2015-11-26

    This study aimed to investigate cytosine methylation profiles in different tobacco (Nicotiana tabacum) cultivars grown in China. Methylation-sensitive amplified polymorphism was used to analyze genome-wide global methylation profiles in four tobacco cultivars (Yunyan 85, NC89, K326, and Yunyan 87). Amplicons with methylated C motifs were cloned by reamplified polymerase chain reaction, sequenced, and analyzed. The results show that geographical location had a greater effect on methylation patterns in the tobacco genome than did sampling time. Analysis of the CG dinucleotide distribution in methylation-sensitive polymorphic restriction fragments suggested that a CpG dinucleotide cluster-enriched area is a possible site of cytosine methylation in the tobacco genome. The sequence alignments of the Nia1 gene (that encodes nitrate reductase) in Yunyan 87 in different regions indicate that a C-T transition might be responsible for the tobacco phenotype. T-C nucleotide replacement might also be responsible for the tobacco phenotype and may be influenced by geographical location.

  11. Persistence of pirimiphos methyl residues in stored wheat

    International Nuclear Information System (INIS)

    Zennouche, B.; Bennaceur, M.

    1991-03-01

    The persistence of 14C pirimiphos methyl in stored wheat was investigated under local conditions during a storage period of 6 months. Surface, methanol extractable and bound residues were quantified. There was a gradual increase in the surface residues over the storage period. 27,97% of the applied amount was found in the surface residues and 54,16% in the extractable and bound residues one month after treatment. After 6 months storage, about 17,8% of the total quantity of the applied pirimiphos methyl remained on the surface and about 58,6% was present in the grains (extractable and bound residues). During cooking 10,91% of the extractable and bound residues were lost

  12. The bomb 14C transient in the Pacific Ocean

    Science.gov (United States)

    Rodgers, Keith B.; Schrag, Daniel P.; Cane, Mark A.; Naik, Naomi H.

    2000-04-01

    A modeling study of the bomb 14C transient is presented for the Pacific Ocean. A primitive equation ocean circulation model has been configured for a high-resolution domain that accounts for the Indonesian Throughflow (ITF). Four separate runs were performed: (1) seasonal forcing with 20 Sv of ITF transport, (2) seasonal forcing with 10 Sv of ITF transport, (3) seasonal forcing with no ITF transport, and (4) interannual forcing with 15 Sv of ITF transport. This study has two main objectives. First, it is intended to describe the time evolution of the bomb 14C transient. This serves as a tool with which one can identify the physical processes controlling the evolving bomb 14C distribution in the Pacific thermocline and thus provides an interpretive framework for the database of Δ14C measurements in the Pacific. Second, transient tracers are applied to the physical oceanographic problem of intergyre exchange. This is of importance in furthering our understanding of the potential role of the upper Pacific Ocean in climate variability. We use bomb 14C as a dye tracer of intergyre exchange between the subtropical gyres and the equatorial upwelling regions of the equatorial Pacific. Observations show that while the atmospheric Δ14C signal peaked in the early to mid-1960s, the Δ14C levels in the surface water waters of the subtropical gyres peaked near 1970, and the Δ14C of surface waters in the equatorial Pacific continued to rise through the 1980s. It is shown that the model exhibits skill in representing the large-scale observed features observed for the bomb 14C transient in the Pacific Ocean. The model successfully captures the basin-scale inventories of bomb 14C in the tropics as well as in the extratropics of the North Pacific. For the equatorial Pacific this is attributed to the model's high meridional resolution. The discrepancies in the three-dimensional distribution of bomb 14C between the model and data are discussed within the context of the dynamical

  13. Bioconcentration of 14 C-Carbofuran and 14 C- Lindane in fresh water Tilapia Nilitica and the bioavailability of their residues to rats

    International Nuclear Information System (INIS)

    Aly, M.A.S.; Afifi, L.M.

    1997-01-01

    Tilapia Nilotica were exposed to 14 C- carbofuran (125 MUg/1) and 14 C - lindane (80 MUg/1) for 96 h. Uptake period followed by 8 days depuration period. The bioconcentration factor (BCF) for carbofuran reached 32.4 at 12 h and 82 for lindane at 48 h. The amount of 14 C-activity found in fish treated with 14 C - carbofuran after the uptake period showed the following descending order: viscera > remaining parts > gills > muscles. In case of 14 C - lindane treated fish the recovered amount followed the order; remaining parts> viscera > gills muscles. During the depuration period, carbofuran residues taken up by fish were eliminated in 2 phases, an initial rapid phase followed by a slower gradual one. However, the rate of elimination in case of lindane was much slower especially during the first 2 days. At the end of the depuration period (8 days), the muscles (edible portion) contained 10% and 58% of 14 C -activity in case of carbofuran and lindane treated groups, respectively. Both insecticides proved to be bioavailable when rats were fed treated fish. Of the administered dose, 44.1% and 53.0% were excreted in urine and feces case of 14 C-carbofuran while in case of 14 C - lindane it was 30.9% and 41.7% for urine and feces, respectively. 2 figs., 2 tabs

  14. Comparison of the gravimetric, phenol red, and 14C-PEG-3350 methods to determine water absorption in the rat single-pass intestinal perfusion model.

    Science.gov (United States)

    Sutton, S C; Rinaldi, M T; Vukovinsky, K E

    2001-01-01

    This study was undertaken to determine whether the gravimetric method provided an accurate measure of water flux correction and to compare the gravimetric method with methods that employ nonabsorbed markers (eg, phenol red and 14C-PEG-3350). Phenol red,14C-PEG-3350, and 4-[2-[[2-(6-amino-3-pyridinyl)-2-hydroxyethyl]amino]ethoxy]-, methyl ester, (R)-benzene acetic acid (Compound I) were co-perfused in situ through the jejunum of 9 anesthetized rats (single-pass intestinal perfusion [SPIP]). Water absorption was determined from the phenol red,14C-PEG-3350, and gravimetric methods. The absorption rate constant (ka) for Compound I was calculated. Both phenol red and 14C-PEG-3350 were appreciably absorbed, underestimating the extent of water flux in the SPIP model. The average +/- SD water flux microg/h/cm) for the 3 methods were 68.9 +/- 28.2 (gravimetric), 26.8 +/- 49.2 (phenol red), and 34.9 +/- 21.9 (14C-PEG-3350). The (average +/- SD) ka for Compound I (uncorrected for water flux) was 0.024 +/- 0.005 min(-1). For the corrected, gravimetric method, the average +/- SD was 0.031 +/- 0.001 min(-1). The gravimetric method for correcting water flux was as accurate as the 2 "nonabsorbed" marker methods.

  15. Synthesis of {sup 14}C-labeled levamisole and {sup 13}C-labeled tetramisole

    Energy Technology Data Exchange (ETDEWEB)

    Feil, V.J. [US Department of Agriculture, Agricultural Research Service, Biosciences Research Lab., Fargo, ND (United States)

    1996-12-01

    The syntheses of {sup 14}C-ring labeled levamisole ([-]-2,3,5,6-tetrahydro-6-phenyl [{sup 14}C]-UL imidazo[2,1-b]thiazole) from acetophenone-ring-UL-{sup 14}C in 5 steps plus resolution with a 7.5% overall yield, and {sup 13}C{sub 6}-ring labeled tetramisole ([{+-}]-2,3,5,6-tetrahydro-6-phenyl [{sup 13}C{sub 6}]imidazo[2,1-b]thiazole) from benzene-{sup 13}C{sub 6} in 6 steps with a 9.0% overall yield are described. (author).

  16. Using plant growth modeling to analyse C source-sink relations under drought: inter and intra specific comparison

    Directory of Open Access Journals (Sweden)

    Benoit ePallas

    2013-11-01

    Full Text Available The ability to assimilate C and allocate NSC (non structural carbohydrates to the most appropriate organs is crucial to maximize plant ecological or agronomic performance. Such C source and sink activities are differentially affected by environmental constraints. Under drought, plant growth is generally more sink than source limited as organ expansion or appearance rate is earlier and stronger affected than C assimilation. This favors plant survival and recovery but not always agronomic performance as NSC are stored rather than used for growth due to a modified metabolism in source and sink leaves. Such interactions between plant C and water balance are complex and plant modeling can help analyzing their impact on plant phenotype. This paper addresses the impact of trade-offs between C sink and source activities and plant production under drought, combining experimental and modeling approaches. Two contrasted monocotyledonous species (rice, oil palm were studied. Experimentally, the sink limitation of plant growth under moderate drought was confirmed as well as the modifications in NSC metabolism in source and sink organs. Under severe stress, when C source became limiting, plant NSC concentration decreased. Two plant models dedicated to oil palm and rice morphogenesis were used to perform a sensitivity analysis and further explore how to optimize C sink and source drought sensitivity to maximize plant growth. Modeling results highlighted that optimal drought sensitivity depends both on drought type and species and that modeling is a great opportunity to analyse such complex processes. Further modeling needs and more generally the challenge of using models to support complex trait breeding are discussed.

  17. Measurement of C-14 distribution in forest around nuclear facilities

    International Nuclear Information System (INIS)

    Atarashi-Andoh, Mariko; Amano, Hikaru; Arakhatoon, Jahan

    2003-01-01

    A simple analytical method of C-14 measurement using fast bomb combustion and liquid scintillation counting (LSC) has been developed for measuring C-14 distribution in the terrestrial environment. Specific activities of C-14 in cedar leaves and soils collected from an area around nuclear facilities and control areas were measured using this method. Depth distribution of Cs-137 in soils was also measured at the same sampling sites and compared with the depth distribution of C-14. C-14 specific activity in cedar leaves examined around nuclear facilities exceeded that in the control areas by 8 to 30 mBq (g carbon) -1 . The depth distribution of C-14 in forest soil shows that C-14 has peak values in the top 10 cm of the soil profiles ascribed to the highest bomb C-14 level in the 1960's. The data were made available to assess the behavior of fallout C-14 in the surface environment. (author)

  18. Analysis of Δ14C variations in atmosphere

    International Nuclear Information System (INIS)

    Simon, J.; Sivo, A.; Richtarikova, M.; Holy, K.; Polaskova, A.; Bulko, M.; Hola, O.

    2005-01-01

    The Δ 14 C in the atmosphere have been measured and studied in two localities of Slovakia. The accomplished analysis proved the existence of the annual variations of the Δ 14 C with the attenuating amplitude and decreasing mean value. It seems to be logical and physically correct to describe the Δ 14 C time-dependence by the equation: y = Ae -at + Be -bt cos(ω 1 t + (φ)). The coefficients A, a, B, b, (φ) are listed in the table for both the localities. The observed variations of the Δ 14 C have a maximum in summer and minimum in winter .Probably it is caused by the higher requirement of the heat supply in winter season which is connected directly with the fossil CO 2 emissions and more intensive Suess effect. Summer maximum could be explained by the combination of the lower CO 2 emission rate and higher turbulent transport of the stratospheric 14 C to the troposphere. Using the Fourier harmonic analysis the amplitude spectra of the average annual variations were plotted. The obtained result shows that the variations have the high degree of symmetry. Furthermore, the obtained basic frequency ω 1 = 2π/12 [month -1 ] proves that the cyclic processes with the period of T = 12 [month] have a major influence on the 14 C amount in the troposphere. The presence of some higher-order harmonics is significant, but a physical interpretation has not yet been clear. In addition to the main frequency there are presented also 2ω 1 and 3ω 1 in Bratislava and 4ω 1 in Zlkovce data-set. The long-time average of the Δ 14 C in Zlkovce during years 1995-2004 is higher of about 6.6 o / oo than in Bratislava. It represents an unique evidence that the local CO 2 pollution affects the 14 C activity . The correlation on the level R 2 = 0,43 was found between Bratislava and Zlkovce atmospheric Δ 14 C data. (authors)

  19. C14 Assays and Autoradiographic Studies on the Rooster Comb

    Science.gov (United States)

    Balazs, Endre A.; Szirmai, John A.; Bergendahl, Gudrun

    1959-01-01

    The distribution of C14 was studied in various parts of the rooster comb following treatment with testosterone. The value of gas-phase assay of C14 in tissue has been demonstrated and the results compared with those of autoradiographic studies on the same tissue. The results of these experiments showed that androgen treatment significantly increases the rate of incorporation of C14 in various parts of the comb. The specific activity of carbon in the comb, cornea, and liver differed, depending on which precursor, viz. glucose-6-C14, glucose-1-C14, and glucuronolactone-U-C14, was administered. The highest values were obtained after the administration of glucose-6-C14; glucuronolactone-U-C14 gave the lowest specific activity. The specific activity of carbon in different parts of the comb showed considerable variation. Carbon assay of serial sections of the comb cut at various planes showed that the specific activity of carbon was highest in the mucoid layer. Both C14 assays and autoradiograms indicate that C14 is also present in other parts of the comb. As seen in autoradiography, the concentration of C14 was highest in the epithelium, in the blood vessel walls, and in the avascular collagenous tissue. These results, and indications from previous studies, suggest that the high specific activity of carbon in the mucoid layer is due mainly to the presence of C14-labelled hyaluronic acid. Autoradiograms and PAS staining suggest that a significant amount of C14 is also incorporated into the glycoproteins associated with the collagen fibers. PMID:13654453

  20. Organic compounds preparation with 14 C

    International Nuclear Information System (INIS)

    Shirvani, Gholam Hossein.

    1996-09-01

    Active urea is a basic reagent for the synthesis of active uric-8- 14 C acid. In our manner, activated Barium carbonate with specified activity was placed in a special furnace with ability of passing gases. Then, ammonia gas was passed through it at about 850 Degree C to obtain Barium Cyanamide. Reaction of the produced compound with CO 2 , and then acidification of the mixture, gave activated urea. Condensation of the urea with Ethylcyanoacetate, produce 6-Aminouracil which upon nitrosation, reduction and then condensation with urea, the desired Uric-8- 14 C acid was synthesized. (author). 148 refs.,

  1. Review of C-14 inventory for the SFR facility

    Energy Technology Data Exchange (ETDEWEB)

    Smith, Graham; Merino, Joan; Kerrigan, Emma

    2002-08-01

    The Swedish Radiation Protection Authority (SSI) is currently reviewing SKB's continuing assessment for disposal of radioactive waste to the SFR facility at Forsmark. Among the wastes disposed are reactor operating wastes. Among the relevant radionuclides is C-14, which is relatively difficult to measure and to control because of its mobility. This report documents a review of the C-14 inventory material submitted by SKB for the SFR-facility, to determine its validity and comment on the appropriate assumptions for C-14 content of wastes due to be disposed of to the SFR. The review is based on information provided by SSI as well as other relevant international experience. Conclusions are drawn upon: the chemical form of the C-14 in the waste from BWRs and PWRs; the production rate of C-14 in BWRs and PWRs and quantification of the source term in the IEX waste; the distribution of the C-14 in the IEX waste from BWR between the resins used for treatment of the primary cooling water and the resins used for treatment of the condensate water; quantification of the uncertainties. A suggestion is made that the C-14 inventory could be better developed based upon a mass balance assessment of all the C-14 produced in reactors, and its ultimate fate in effluent and solid wastes, taking account of the reactor specific operational factors identified in the review as relevant to C-14 inventory assessment.

  2. Review of C-14 inventory for the SFR facility

    International Nuclear Information System (INIS)

    Smith, Graham; Merino, Joan; Kerrigan, Emma

    2002-08-01

    The Swedish Radiation Protection Authority (SSI) is currently reviewing SKB's continuing assessment for disposal of radioactive waste to the SFR facility at Forsmark. Among the wastes disposed are reactor operating wastes. Among the relevant radionuclides is C-14, which is relatively difficult to measure and to control because of its mobility. This report documents a review of the C-14 inventory material submitted by SKB for the SFR-facility, to determine its validity and comment on the appropriate assumptions for C-14 content of wastes due to be disposed of to the SFR. The review is based on information provided by SSI as well as other relevant international experience. Conclusions are drawn upon: the chemical form of the C-14 in the waste from BWRs and PWRs; the production rate of C-14 in BWRs and PWRs and quantification of the source term in the IEX waste; the distribution of the C-14 in the IEX waste from BWR between the resins used for treatment of the primary cooling water and the resins used for treatment of the condensate water; quantification of the uncertainties. A suggestion is made that the C-14 inventory could be better developed based upon a mass balance assessment of all the C-14 produced in reactors, and its ultimate fate in effluent and solid wastes, taking account of the reactor specific operational factors identified in the review as relevant to C-14 inventory assessment

  3. Secretin enhances [14C]erythritol clearance in unanesthetized dogs

    International Nuclear Information System (INIS)

    Lewis, M.H.; Baker, A.L.; Dhorajiwala, J.; Moossa, A.R.

    1982-01-01

    To determine the effect of secretin infusion on clearance of inert markers into bile, unanesthetized dogs fitted with Thomas cannulas received continuous infusions of [ 14 C]erythritol and [ 3 H]inulin throughout study. Taurocholic acid administered sequentially at 9.0, 20.0, and 40.0 mumol/min enhanced [ 14 C]erythritol clearance, and GIH secretin (3 units/min) administered along with TCA (40.0 mumol/min) increased [ 14 C]erythritol clearance from 4.9 +/- 1.2 ml/10 min to 6.8 +/- 1.3 ml/10 min (P less than 0.001), but simultaneously measured [ 3 H]inulin clearance was unaltered. Secretin alone also increased [ 14 C]erythritol clearance but did not alter [ 3 H]inulin clearance. The increase in [ 14 C]erythritol clearance per unit increase in bile flow was less during secretin infusion than TCA. Thus, secretin increases [ 14 C]erythritol transport through restricted channels, probably distal to the canaliculi. [ 14 C]Erythritol may not be an accurate marker for canalicular bile flow in dogs during secretin infusion

  4. 1,4-Dimethyl-3-phenyl-3H-pyrazolo[3,4-c]isoquinolin-5(4H-one

    Directory of Open Access Journals (Sweden)

    Giuseppe Daidone

    2008-05-01

    Full Text Available The title compound, C18H15N3O, is the product of the thermal decomposition of the diazonium salt derived from 2-amino-N-methyl-N-(3-methyl-1-phenyl-1H-pyrazol-5-ylbenzamide. It is characterized by a trans orientation of the methyl groups with respect to the tricyclic ring system. The molecule has a nearly planar phenylpyrazolo[3,4-c]isoquinolin-5-one system, the largest deviation from the mean plane being 0.066 (2 Å for the O atom. The dihedral angle between the phenyl substituent and the heterotricycle is 67 (1°. The packing is stabilized by C—H...N hydrogen-bond interactions, with the formation of molecular chains along the c axis.

  5. Improved labeling strategy for 13C relaxation measurements of methyl groups in proteins

    International Nuclear Information System (INIS)

    Lee, Andrew L.; Urbauer, Jeffrey L.; Wand, A. Joshua

    1997-01-01

    Selective incorporation of 13 C into the methyl groups of protein side chains is described as a means for simplifying the measurement and interpretation of 13 C relaxation parameters.High incorporation (>90%) is accomplished by using pyruvate(3- 13 C, 99%) as the sole carbon source in the growth media for protein overexpression in E. coli. This improved labeling scheme increases the sensitivity of the relaxation experiments by approximately fivefold when compared to randomly fractionally 13 C-labeled protein, allowing high-quality measurements on relatively dilute (<1 mM)protein samples at a relatively low cost

  6. Programmed Application of Transforming Growth Factor β3 and Rac1 Inhibitor NSC23766 Committed Hyaline Cartilage Differentiation of Adipose-Derived Stem Cells for Osteochondral Defect Repair.

    Science.gov (United States)

    Zhu, Shouan; Chen, Pengfei; Wu, Yan; Xiong, Si; Sun, Heng; Xia, Qingqing; Shi, Libing; Liu, Huanhuan; Ouyang, Hong Wei

    2014-10-01

    Hyaline cartilage differentiation is always the challenge with application of stem cells for joint repair. Transforming growth factors (TGFs) and bone morphogenetic proteins can initiate cartilage differentiation but often lead to hypertrophy and calcification, related to abnormal Rac1 activity. In this study, we developed a strategy of programmed application of TGFβ3 and Rac1 inhibitor NSC23766 to commit the hyaline cartilage differentiation of adipose-derived stem cells (ADSCs) for joint cartilage repair. ADSCs were isolated and cultured in a micromass and pellet culture model to evaluate chondrogenic and hypertrophic differentiation. The function of Rac1 was investigated with constitutively active Rac1 mutant and dominant negative Rac1 mutant. The efficacy of ADSCs with programmed application of TGFβ3 and Rac1 inhibitor for cartilage repair was studied in a rat model of osteochondral defects. The results showed that TGFβ3 promoted ADSCs chondro-lineage differentiation and that NSC23766 prevented ADSC-derived chondrocytes from hypertrophy in vitro. The combination of ADSCs, TGFβ3, and NSC23766 promoted quality osteochondral defect repair in rats with much less chondrocytes hypertrophy and significantly higher International Cartilage Repair Society macroscopic and microscopic scores. The findings have illustrated that programmed application of TGFβ3 and Rac1 inhibitor NSC23766 can commit ADSCs to chondro-lineage differentiation and improve the efficacy of ADSCs for cartilage defect repair. These findings suggest a promising stem cell-based strategy for articular cartilage repair. ©AlphaMed Press.

  7. DNA methylation

    DEFF Research Database (Denmark)

    Williams, Kristine; Christensen, Jesper; Helin, Kristian

    2012-01-01

    DNA methylation is involved in key cellular processes, including X-chromosome inactivation, imprinting and transcriptional silencing of specific genes and repetitive elements. DNA methylation patterns are frequently perturbed in human diseases such as imprinting disorders and cancer. The recent...... discovery that the three members of the TET protein family can convert 5-methylcytosine (5mC) into 5-hydroxymethylcytosine (5hmC) has provided a potential mechanism leading to DNA demethylation. Moreover, the demonstration that TET2 is frequently mutated in haematopoietic tumours suggests that the TET...... proteins are important regulators of cellular identity. Here, we review the current knowledge regarding the function of the TET proteins, and discuss various mechanisms by which they contribute to transcriptional control. We propose that the TET proteins have an important role in regulating DNA methylation...

  8. Densities and speeds of sound for binary mixtures of (1,3-dioxolane or 1,4-dioxane) with (2-methyl-1-propanol or 2-methyl-2-propanol) at the temperatures (298.15 and 313.15) K

    International Nuclear Information System (INIS)

    Villares, A.; Martin, S.; Haro, M.; Giner, B.; Artigas, H.

    2004-01-01

    This paper reports densities and speeds of sound for the binary mixtures of (1,3-dioxolane or 1,4-dioxane) with (2-methyl-1-propanol or 2-methyl-2-propanol) at the temperatures (298.15 and 313.15) K. Excess volumes and excess isentropic compressibility coefficients have been calculated from experimental data and fitted by means of a Redlich-Kister type equation. The ERAS model has been used to calculate the excess volumes of the four systems at both temperatures

  9. NSC666715 and Its Analogs Inhibit Strand-Displacement Activity of DNA Polymerase β and Potentiate Temozolomide-Induced DNA Damage, Senescence and Apoptosis in Colorectal Cancer Cells.

    Directory of Open Access Journals (Sweden)

    Aruna S Jaiswal

    Full Text Available Recently approved chemotherapeutic agents to treat colorectal cancer (CRC have made some impact; however, there is an urgent need for newer targeted agents and strategies to circumvent CRC growth and metastasis. CRC frequently exhibits natural resistance to chemotherapy and those who do respond initially later acquire drug resistance. A mechanism to potentially sensitize CRC cells is by blocking the DNA polymerase β (Pol-β activity. Temozolomide (TMZ, an alkylating agent, and other DNA-interacting agents exert DNA damage primarily repaired by a Pol-β-directed base excision repair (BER pathway. In previous studies, we used structure-based molecular docking of Pol-β and identified a potent small molecule inhibitor (NSC666715. In the present study, we have determined the mechanism by which NSC666715 and its analogs block Fen1-induced strand-displacement activity of Pol-β-directed LP-BER, cause apurinic/apyrimidinic (AP site accumulation and induce S-phase cell cycle arrest. Induction of S-phase cell cycle arrest leads to senescence and apoptosis of CRC cells through the p53/p21 pathway. Our initial findings also show a 10-fold reduction of the IC50 of TMZ when combined with NSC666715. These results provide a guide for the development of a target-defined strategy for CRC chemotherapy that will be based on the mechanisms of action of NSC666715 and TMZ. This combination strategy can be used as a framework to further reduce the TMZ dosages and resistance in CRC patients.

  10. 14C analysis via intracavity optogalvanic spectroscopy

    International Nuclear Information System (INIS)

    Murnick, Daniel; Dogru, Ozgur; Ilkmen, Erhan

    2010-01-01

    A new ultra sensitive laser-based analytical technique, intracavity optogalvanic spectroscopy (ICOGS), allowing extremely high sensitivity for detection of 14 C-labeled carbon dioxide has recently been demonstrated. Capable of replacing accelerator mass spectrometers (AMS) for many applications, the technique quantifies zeptomoles of 14 C in sub micromole CO 2 samples. Based on the specificity of narrow laser resonances coupled with the sensitivity provided by standing waves in an optical cavity, and detection via impedance variations, limits of detection near 10 -1514 C/ 12 C ratios have been obtained with theoretical limits much lower. Using a 15 W 14 CO 2 laser, a linear calibration with samples from 5 x 10 -15 to >1.5 x 10 -12 in 14 C/ 12 C ratios, as determined by AMS, was demonstrated. Calibration becomes non-linear over larger concentration ranges due to interactions between CO 2 and buffer gas, laser saturation effects and changes in equilibration time constants. The instrument is small (table top), low maintenance and can be coupled to GC or LC input. The method can also be applied to detection of other trace entities. Possible applications include microdosing studies in drug development, individualized sub-therapeutic tests of drug metabolism, carbon dating and real time monitoring of atmospheric radiocarbon.

  11. [Determination methods for the content of methyl salicylate-2-O-beta-D-galactopyranoside (1-4)-beta-D-glucopyranoside].

    Science.gov (United States)

    He, Xiu-Feng; Xia, Peng-Fei; Wang, Ai-Guo; Liu, Dong; Zhao, Li-Min

    2012-07-01

    The paper is to report the establishment of three methods for determination of methyl salicylate-2-O-beta-D-galactopyranoside (1-4)-beta-D-glucopyranoside (MSG) by HPLC, UV or potentiometric titration. The results determined by the three methods turned out to be of no significant difference (P>0.05). The method was chosen according to MSG difference test demands.

  12. Radioactive methionine: determination, and distribution of radioactivity in the sulfur, methyl and 4-carbon moieties

    International Nuclear Information System (INIS)

    Giovanelli, J.; Mudd, S.H.

    1985-01-01

    A simple and inexpensive method is described for isolation and determination of [ 14 C]methionine in the non-protein fraction of tissues extensively labeled with 14 C. The effectiveness of the method was demonstrated by isolation of non-protein [ 14 C]methionine (as the carboxymethylsulfonium salt) of proven radiopurity from the plant Lemna which had been grown for a number of generations on (U- 14 C]sucrose and contained a 2000-fold excess of 14 C in undefined non-protein compounds. An advantage is that the isolated methioninecarboxymethlysulfonium salt is readily degraded to permit separate determination of radioactivity in the 4-carbon, methyl and sulfur moieties of methionine. During this work, a facile labilization of 3 H attached to the (carboxy)methylene carbon of methioninecarboxymethylsulfonium salt was observed. This labilization is ascribed to formation of a sulfur ylid. (Auth.)

  13. 15C-15F Charge Symmetry and the 14C(n,γ)15C Reaction Puzzle

    International Nuclear Information System (INIS)

    Timofeyuk, N.K.; Thompson, I.J.; Baye, D.; Descouvemont, P.; Kamouni, R.

    2006-01-01

    The low-energy reaction 14 C(n,γ) 15 C provides a rare opportunity to test indirect methods for the determination of neutron capture cross sections by radioactive isotopes versus direct measurements. It is also important for various astrophysical scenarios. Currently, puzzling disagreements exist between the 14 C(n,γ) 15 C cross sections measured directly, determined indirectly, and calculated theoretically. To solve this puzzle, we offer a strong test based on a novel idea that the amplitudes for the virtual 15 C→ 14 C+n and the real 15 F→ 14 O+p decays are related. Our study of this relation, performed in a microscopic model, shows that existing direct and some indirect measurements strongly contradict charge symmetry in the 15 C and 15 F mirror pair. This brings into question the experimental determinations of the astrophysically important (n,γ) cross sections for short-lived radioactive targets

  14. Behavior of 14C-BHC residues in rice grain

    International Nuclear Information System (INIS)

    Lee, S.R.; Kim, Y.H.

    1981-01-01

    γ-(U- 14 C)-BHC was applied to rice plants grown in a pot and its fate in the growth, polishing and oil-extraction processes of the grain was investigated. The 14 C-activity was absorbed and translocated widely in the plant and the recovery of applied 14 C-activity in the straw and grain was about 2.8%, of which 9.4% was found in the brown rice. The % partitioning of 14 C-residues in bran and polished rice was 12:88 and that in oil and oilcake was 37:63. Characterization of 14 C-residues the presence of γ-BHC, pentachlorocyclohexene, trichlorobenzene and hydrophilic metabolites, whose proportions were different in the straw and grain. (Author)

  15. Appearance of circulating and tissue 14C-lipids after oral 14C-tripalmitate administration in the late pregnant rat

    International Nuclear Information System (INIS)

    Argiles, J.; Herrera, E.

    1989-01-01

    Studies were performed to determine whether and/or how dietary lipids participate in maternal hypertriglyceridemia during late gestation in the rat. After oral administration of glycerol-tri(1-14C)-palmitate, total radioactivity in plasma increased more rapidly in 20-day pregnant rats than in either 19-day pregnant rats or virgin controls. At the peak of plasma radioactivity, four hours after the tracer was administered, most of the plasma label corresponded to 14C-lipids in triglyceride-rich lipoproteins (d less than 1.006), and when expressed per micromol of triglyceride, values were higher in pregnant than in virgin rats. The difference was less after 24 hours, although at this time the level of 14C-lipids in d less than 1.006 lipoproteins was still higher in 20-day pregnant rats than in virgins. Tissue 14C-lipids, as expressed per gram of fresh weight, were similar in pregnant and virgin rats, but the values in mammary glands were much higher in the former group. Estimated recovery of administered radioactivity four hours after tracer in total white adipose tissue, mammary glands, and plasma lipids was higher in pregnant than in virgin rats. No difference was found between 20-day pregnant and virgin rats either in the label retained in the gastrointestinal tract or in that exhaled as 14C-CO2 during the first four hours following oral administration of 14C-tripalmitate. These findings plus the known maternal hyperphagia, indicate that in the rat at late pregnancy triglyceride intestinal absorption is unchanged or even enhanced and that dietary lipids actively contribute to both maternal hypertriglyceridemia and lipid uptake by the mammary gland

  16. Accelerator mass spectrometry analysis of "1"4C-oxaliplatin concentrations in biological samples and "1"4C contents in biological samples and antineoplastic agents

    International Nuclear Information System (INIS)

    Toyoguchi, Teiko; Kobayashi, Takeshi; Konno, Noboru; Shiraishi, Tadashi; Kato, Kazuhiro; Tokanai, Fuyuki

    2015-01-01

    Accelerator mass spectrometry (AMS) is expected to play an important role in microdose trials. In this study, we measured the "1"4C concentration in "1"4C-oxaliplatin-spiked serum, urine and supernatant of fecal homogenate samples in our Yamagata University (YU) – AMS system. The calibration curves of "1"4C concentration in serum, urine and supernatant of fecal homogenate were linear (the correlation coefficients were ⩾0.9893), and the precision and accuracy was within the acceptance criteria. To examine a "1"4C content of water in three vacuum blood collection tubes and a syringe were measured. "1"4C was not detected from water in these devices. The mean "1"4C content in urine samples of 6 healthy Japanese volunteers was 0.144 dpm/mL, and the intra-day fluctuation of "1"4C content in urine from a volunteer was little. The antineoplastic agents are administered to the patients in combination. Then, "1"4C contents of the antineoplastic agents were quantitated. "1"4C contents were different among 10 antineoplastic agents; "1"4C contents of paclitaxel injection and docetaxel hydrate injection were higher than those of the other injections. These results indicate that our quantitation method using YU-AMS system is suited for microdosing studies and that measurement of baseline and co-administered drugs might be necessary for the studies in low concentrations.

  17. Accelerator mass spectrometry analysis of {sup 14}C-oxaliplatin concentrations in biological samples and {sup 14}C contents in biological samples and antineoplastic agents

    Energy Technology Data Exchange (ETDEWEB)

    Toyoguchi, Teiko, E-mail: tteiko@med.id.yamagata-u.ac.jp [Department of Pharmacy, Yamagata University Hospital, 2-2-2 Iida-Nishi, Yamagata-shi, Yamagata 990-9585 (Japan); Kobayashi, Takeshi; Konno, Noboru; Shiraishi, Tadashi [Department of Pharmacy, Yamagata University Hospital, 2-2-2 Iida-Nishi, Yamagata-shi, Yamagata 990-9585 (Japan); Kato, Kazuhiro; Tokanai, Fuyuki [Department of Physics, Faculty of Science, Yamagata University, 1-4-12 Kojirakawa-machi, Yamagata-shi, Yamagata 990-8560 (Japan)

    2015-10-15

    Accelerator mass spectrometry (AMS) is expected to play an important role in microdose trials. In this study, we measured the {sup 14}C concentration in {sup 14}C-oxaliplatin-spiked serum, urine and supernatant of fecal homogenate samples in our Yamagata University (YU) – AMS system. The calibration curves of {sup 14}C concentration in serum, urine and supernatant of fecal homogenate were linear (the correlation coefficients were ⩾0.9893), and the precision and accuracy was within the acceptance criteria. To examine a {sup 14}C content of water in three vacuum blood collection tubes and a syringe were measured. {sup 14}C was not detected from water in these devices. The mean {sup 14}C content in urine samples of 6 healthy Japanese volunteers was 0.144 dpm/mL, and the intra-day fluctuation of {sup 14}C content in urine from a volunteer was little. The antineoplastic agents are administered to the patients in combination. Then, {sup 14}C contents of the antineoplastic agents were quantitated. {sup 14}C contents were different among 10 antineoplastic agents; {sup 14}C contents of paclitaxel injection and docetaxel hydrate injection were higher than those of the other injections. These results indicate that our quantitation method using YU-AMS system is suited for microdosing studies and that measurement of baseline and co-administered drugs might be necessary for the studies in low concentrations.

  18. The synthesis of Org 3770 labelled with 3H, 13C and 14C

    International Nuclear Information System (INIS)

    Kaspersen, F.M.; Rooij, F.A.M. van; Sperling, E.G.M.; Wieringa, J.H.

    1989-01-01

    The syntheses of 1,2,3,4,10,14b-hexahydro-2-methylpyrazino[2,1-a]pyrido[2,3-c][2]benazepine (Org 3770) labelled with 3 H (and 2 H), 13 C and 14 C are described. Tritiated Org 3770 was prepared either by exchange under alkaline conditions with tritiated water or catalytic reductive dehalogenation of a chloro analogue with 3 H 2 . 13 C-labelled material was obtained in a seven-step synthesis starting from 13 C-labelled benzene whereas 14 C-Org 3770 was prepared in a three-step synthesis starting with 14 CO 2 . All labelled compounds were analyzed by TLC, HPLC, MS and NMR. (author)

  19. Evaluation of [14C] and [13C]Sucrose as Blood-Brain Barrier Permeability Markers.

    Science.gov (United States)

    Miah, Mohammad K; Chowdhury, Ekram A; Bickel, Ulrich; Mehvar, Reza

    2017-06-01

    Nonspecific quantitation of [ 14 C]sucrose in blood and brain has been routinely used as a quantitative measure of the in vivo blood-brain barrier (BBB) integrity. However, the reported apparent brain uptake clearance (K in ) of the marker varies widely (∼100-fold). We investigated the accuracy of the use of the marker in comparison with a stable isotope of sucrose ([ 13 C]sucrose) measured by a specific liquid chromatography-tandem mass spectrometry method. Rats received single doses of each marker, and the K in values were determined. Surprisingly, the K in value of [ 13 C]sucrose was 6- to 7-fold lower than that of [ 14 C]sucrose. Chromatographic fractionation after in vivo administration of [ 14 C]sucrose indicated that the majority of the brain content of radioactivity belonged to compounds other than the intact [ 14 C]sucrose. However, mechanistic studies failed to reveal any substantial metabolism of the marker. The octanol:water partition coefficient of [ 14 C]sucrose was >2-fold higher than that of [ 13 C]sucrose, indicating the presence of lipid-soluble impurities in the [ 14 C]sucrose solution. Our data indicate that [ 14 C]sucrose overestimates the true BBB permeability to sucrose. We suggest that specific quantitation of the stable isotope ( 13 C) of sucrose is a more accurate alternative to the current widespread use of the radioactive sucrose as a BBB marker. Copyright © 2017 American Pharmacists Association®. Published by Elsevier Inc. All rights reserved.

  20. A practical synthesis of long-chain iso-fatty acids (iso-C12–C19 and related natural products

    Directory of Open Access Journals (Sweden)

    Mark B. Richardson

    2013-09-01

    Full Text Available A gram-scale synthesis of terminally-branched iso-fatty acids (iso-C12–C19 was developed commencing with methyl undec-10-enoate (methyl undecylenate (for iso-C12–C14 or the C15 and C16 lactones pentadecanolide (for iso-C15–C17 and hexadecanolide (for iso-C18–C19. Central to the approaches outlined is the two-step construction of the terminal isopropyl group through addition of methylmagnesium bromide to the ester/lactones and selective reduction of the resulting tertiary alcohols. Thus, the C12, C17 and C18 iso-fatty acids were obtained in three steps from commercially-available starting materials, and the remaining C13–C16 and C19 iso-fatty acids were prepared by homologation or recursive dehomologations of these fatty acids or through intercepting appropriate intermediates. Highlighting the synthetic potential of the iso-fatty acids and various intermediates prepared herein, we describe the synthesis of the natural products (S-2,15-dimethylpalmitic acid, (S-2-hydroxy-15-methylpalmitic acid, and 2-oxo-14-methylpentadecane.

  1. Effects of Nutrient Deficiencies in Corn Plants on the In Vivo and In Vitro Metabolism of [14C] Diazinon

    International Nuclear Information System (INIS)

    Kunstman, J.L.; Lichtenstein, E.P.

    1981-01-01

    Full text: The effects of calcium, nitrogen, and magnesium deficiencies on the penetration, translocation, and the in vivo and in vitro metabolism of the insecticide [ 14 C] diazinon (diethyl-2-isopropyl-6-methyl-4-pyrimidinyl) in corn plants were investigated. On a per gram fresh weight basis only roots from nitrogen-deficient solutions contained less C while tops from plants grown in calcium-deficient solutions contained nearly four times more radiocarbon than those from complete nutrient solutions. Due to calcium or nitrogen deficiencies a reduced degradation occurred in roots as indicated by the relatively higher recoveries of diazinon and the lower recoveries of an unidentified, more polar 14 C-ring compound. No differencies in [ 14 C] diazinon degradation due to nutrient deficiencies were noticeable with corn tops. The metabolic activity of corn roots was due to a soluble enzyme. In studies with subcellular components from roots, specific activities increased from the homogenate (4.09%/mg of protein) to the 105000 g supernatant (7.77%/mg of protein). Subcellular components from calcium-deficient roots produced significantly less water-soluble radiocarbon (sp act., 0.60) than did control roots (sp act., 1.60), results similar to those observed with in vivo experiments. However, the 10000 g supernatant from root material deficient in nitrogen produced significantly more water—soluble radiocarbon (sp act., 2.85) than subcellular fractions from control roots. (author)

  2. Mild synthesis of [N-methyl-{sup 11}C]-isovaleroyl-(L)-carnitine. The usefulness of a tritium approach

    Energy Technology Data Exchange (ETDEWEB)

    Angelini, G.; Carnevaletti, F.; Margonelli, A.; Corsi, G. [Istituto di Chimica Nucleare - C.N.R., C.P. 10, Rome (Italy); Ragni, P. [Istituto di Chimica Nucleare -- C.N.R., C.P. 10 -- 00016 Monterotondo Stazione, Roma, (Italy); Fazio, F.; Todde, S. [Istituto di Neuroscienze e Bioimmagini - C.N.R., H.S. Raffaele, Milan (Italy); Tinti, O. [Sigma-Tau, Industrie Farmaceutiche Riunite S.p.A., Pomezia, Rome (Italy)

    1999-02-01

    The title carnitine derivative was labelled both with [{sup 11}C]methyl iodide and [{sup 3}H]methyl iodide. The former was synthesized in order to improve the knowledge of the acyl carnitines fate in humans. The latter was synthesized, at approximately the same concentration level as that of the former, in order to optimize its radiosynthesis, taking advantage from the long half-life of the tritium.

  3. Sources of C-14 generation and associated doses

    International Nuclear Information System (INIS)

    Amado, Valeria A.; Biaggio, Alfredo L.; Canoba, Analia C.; Curti, Adriana R.

    2009-01-01

    C-14 is a radioactive isotope of C with a half-life of 5700 years that decays to N-14 by emission of beta radiation. It is naturally produced in the upper atmosphere by cosmic ray neutrons via the (n;p) reaction over N-14. Anthropogenic C-14 has been generated in the past by atmospheric nuclear weapon tests and it is currently produced during the operation of nuclear reactors. Once released this radionuclide behaves in the biosphere as the standard carbon cycle. Since the beginning of the industrial period the relationship Carbon-14/Stable Carbon has changed continuously, and so the dose incurred by the world population. In this paper the main anthropogenic activities that modified such relationship are presented and analyzed: the Suess effect and the generation of nuclear energy. It is concluded that the current trend of reduction of the total dose due to C-14 will continue during the next decades. Finally it is indicated that in order to prevent an excessive accumulation of this radionuclide in the biosphere, actions should be collectively implemented to be effective. (author) [es

  4. Radiocarbon 14C differentiation of sparkling and carbonated wines

    International Nuclear Information System (INIS)

    Martin, G.E.; Krueger, H.W.; Burggraff, J.M.

    1985-01-01

    Specific 14 C-activities, percent of modern 14 C-activity, and calculated percent of fermentation CO 2 are presented for CO 2 contained in commercial sparkling wines, labeled as champagne or produced by the bulk (charmat) process. These data are given for the production years 1976-1982. The survey encompassed effervescent wines produced in Spain, Italy, West Germany, California, and New York. Addition of synthetic CO 2 to approximately 40 samples represented as sparkling wines was indicated by low 14 C-activities of CO 2 in these wines. Data for 14 C-activity were also presented for the ethanol distilled from sparkling wines for the years 1977-1980. In all cases, the 14 C-activity of ethanol was appropriate to the year of vintage

  5. Changes in the level of [14C]indole-3-acetic acid and [14C]indoleacetylaspartic acid during root formation in mung bean cuttings

    International Nuclear Information System (INIS)

    Norcini, J.G.; Heuser, C.W.

    1988-01-01

    Changes in the levels of [ 14 C]indole-3-acetic acid (IAA) and [ 14 C]indoleacetylaspartic acid (IAAsp) were examined during adventitious root formation in mung bean (Vigna radiata [L.] R. Wilcz. Berken) stem cuttings. IAAsp was identified by GC-MS as the primary conjugate in IAA-treated cuttings. During root formation in IAA-treated cuttings, the level of [ 14 C]IAAsp increased rapidly the first day and then declined; [ 14 C]IAA was rapidly metabolized and not detected after 12 hours

  6. Detection of DNA methylation changes in micropropagated banana plants using methylation-sensitive amplification polymorphism (MSAP).

    Science.gov (United States)

    Peraza-Echeverria, S; Herrera-Valencia, V A.; Kay, A -J.

    2001-07-01

    The extent of DNA methylation polymorphisms was evaluated in micropropagated banana (Musa AAA cv. 'Grand Naine') derived from either the vegetative apex of the sucker or the floral apex of the male inflorescence using the methylation-sensitive amplification polymorphism (MSAP) technique. In all, 465 fragments, each representing a recognition site cleaved by either or both of the isoschizomers were amplified using eight combinations of primers. A total of 107 sites (23%) were found to be methylated at cytosine in the genome of micropropagated banana plants. In plants micropropagated from the male inflorescence explant 14 (3%) DNA methylation events were polymorphic, while plants micropropagated from the sucker explant produced 8 (1.7%) polymorphisms. No DNA methylation polymorphisms were detected in conventionally propagated banana plants. These results demonstrated the usefulness of MSAP to detect DNA methylation events in micropropagated banana plants and indicate that DNA methylation polymorphisms are associated with micropropagation.

  7. Comparative in vitro metabolism of 1-14C-oleic acid and 1-14C-erucic acid in liver, heart and skeletal muscles of rats

    International Nuclear Information System (INIS)

    Bhatia, I.S.; Sharma, A.K.; Ahuja, S.P.

    1978-01-01

    In vitro oxidation of 14 C-oleic and 1- 14 C-erucic acid and their incorporation into lipids by liver, heart and skeletal muscles from female albino rats were studied. These tissues were obtained from rats maintained for 120 days on low fat diet or diets containing 15% mustard oil or 15% groundnut oil. In all these tissues from rats on different types of diets, the oxidation of 1- 14 C-erucic acid was lower than that 1- 14 C-oleic acid. There was little accumulation of lipids in heart after 120 days of feeding mustard oil. Oxidation of 1- 14 C-erucic acid was enhanced in liver, heart and skeletal muscles of rats conditioned to the mustard oil diet supplying erucic acid. Oxidation of erucic acid was maximum in liver and least in heart, whereas there were no differences in the oxidation of 1- 14 C-oleic acid in these tissues. Incorporation of 1- 14 C-oleic acid into triglycerides and phospholipids was not affected by the type of diet or tissues Incorporation of 1- 14 C-erucic acid was mainly into triglycerides of heart and skeletal muscles of rats not accustomed to mustard oil diet whereas these tissues from rats accustomed to mustard oil diets incorporated 1- 14 C-erucic acid both into the triglycerides and phospholipids. (author)

  8. Seasonal and inter-annual dynamics of growth, non-structural carbohydrates and C stable isotopes in a Mediterranean beech forest.

    Science.gov (United States)

    Scartazza, Andrea; Moscatello, Stefano; Matteucci, Giorgio; Battistelli, Alberto; Brugnoli, Enrico

    2013-07-01

    Seasonal and inter-annual dynamics of growth, non-structural carbohydrates (NSC) and carbon isotope composition (δ(13)C) of NSC were studied in a beech forest of Central Italy over a 2-year period characterized by different environmental conditions. The net C assimilated by forest trees was mainly used to sustain growth early in the season and to accumulate storage carbohydrates in trunk and root wood in the later part of the season, before leaf shedding. Growth and NSC concentration dynamics were only slightly affected by the reduced soil water content (SWC) during the drier year. Conversely, the carbon isotope analysis on NSC revealed seasonal and inter-annual variations of photosynthetic and post-carboxylation fractionation processes, with a significant increase in δ(13)C of wood and leaf soluble sugars in the drier summer year than in the wetter one. The highly significant correlation between δ(13)C of leaf soluble sugars and SWC suggests a decrease of the canopy C isotope discrimination and, hence, an increased water-use efficiency with decreasing soil water availability. This may be a relevant trait for maintaining an acceptable plant water status and a relatively high C sink capacity during dry seasonal periods. Our results suggest a short- to medium-term homeostatic response of the Collelongo beech stand to variations in water availability and solar radiation, indicating that this Mediterranean forest was able to adjust carbon-water balance in order to prevent C depletion and to sustain plant growth and reserve accumulation during relatively dry seasons.

  9. {sup 13}C-METHYL FORMATE: OBSERVATIONS OF A SAMPLE OF HIGH-MASS STAR-FORMING REGIONS INCLUDING ORION-KL AND SPECTROSCOPIC CHARACTERIZATION

    Energy Technology Data Exchange (ETDEWEB)

    Favre, Cécile; Bergin, Edwin A.; Crockett, Nathan R.; Neill, Justin L. [Department of Astronomy, University of Michigan, 500 Church Street, Ann Arbor, MI 48109 (United States); Carvajal, Miguel [Dpto. Física Aplicada, Unidad Asociada CSIC, Facultad de Ciencias Experimentales, Universidad de Huelva, E-21071 Huelva (Spain); Field, David [Department of Physics and Astronomy, University of Aarhus, Ny Munkegade 120, DK-8000 Aarhus C (Denmark); Jørgensen, Jes K.; Bisschop, Suzanne E. [Centre for Star and Planet Formation, Niels Bohr Institute, University of Copenhagen, Juliane Maries Vej 30, DK-2100 Copenhagen Ø (Denmark); Brouillet, Nathalie; Despois, Didier; Baudry, Alain [Univ. Bordeaux, LAB, UMR 5804, F-33270, Floirac (France); Kleiner, Isabelle [Laboratoire Interuniversitaire des Systèmes Atmosphériques (LISA), CNRS, UMR 7583, Université de Paris-Est et Paris Diderot, 61, Av. du Général de Gaulle, F-94010 Créteil Cedex (France); Margulès, Laurent; Huet, Thérèse R.; Demaison, Jean, E-mail: cfavre@umich.edu, E-mail: miguel.carvajal@dfa.uhu.es [Laboratoire de Physique des Lasers, Atomes et Molécules, UMR CNRS 8523, Université Lille I, F-59655 Villeneuve d' Ascq Cedex (France)

    2015-01-01

    We have surveyed a sample of massive star-forming regions located over a range of distances from the Galactic center for methyl formate, HCOOCH{sub 3}, and its isotopologues H{sup 13}COOCH{sub 3} and HCOO{sup 13}CH{sub 3}. The observations were carried out with the APEX telescope in the frequency range 283.4-287.4 GHz. Based on the APEX observations, we report tentative detections of the {sup 13}C-methyl formate isotopologue HCOO{sup 13}CH{sub 3} toward the following four massive star-forming regions: Sgr B2(N-LMH), NGC 6334 IRS 1, W51 e2, and G19.61-0.23. In addition, we have used the 1 mm ALMA science verification observations of Orion-KL and confirm the detection of the {sup 13}C-methyl formate species in Orion-KL and image its spatial distribution. Our analysis shows that the {sup 12}C/{sup 13}C isotope ratio in methyl formate toward the Orion-KL Compact Ridge and Hot Core-SW components (68.4 ± 10.1 and 71.4 ± 7.8, respectively) are, for both the {sup 13}C-methyl formate isotopologues, commensurate with the average {sup 12}C/{sup 13}C ratio of CO derived toward Orion-KL. Likewise, regarding the other sources, our results are consistent with the {sup 12}C/{sup 13}C in CO. We also report the spectroscopic characterization, which includes a complete partition function, of the complex H{sup 13}COOCH{sub 3} and HCOO{sup 13}CH{sub 3} species. New spectroscopic data for both isotopomers H{sup 13}COOCH{sub 3} and HCOO{sup 13}CH{sub 3}, presented in this study, have made it possible to measure this fundamentally important isotope ratio in a large organic molecule for the first time.

  10. Serum cystatin C and anti-N-methyl-D-aspartate receptor encephalitis.

    Science.gov (United States)

    Shu, Y; Chang, Y; Wu, H; Li, J; Cao, B; Sun, X; Wang, J; Peng, L; Hu, X; Yu, X; Qiu, W

    2018-05-01

    Cystatin C (CysC) is associated with many neurodegenerative disorders and autoimmune diseases, but its relationship with anti-N-Methyl-D-aspartate receptor (anti-NMDAR) encephalitis is unknown. Serum levels of CysC were determined in 66 patients with anti-NMDAR encephalitis and 115 healthy controls. Of the 66 patients, 30 had a follow-up evaluation at 3 months after admission. Association of CysC with anti-NMDAR encephalitis and its clinical parameters were evaluated in the patients. The serum levels of CysC were significantly lower in patients with anti-NMDAR encephalitis than in controls (0.70 ± 0.13 vs 0.83 ± 0.17 mg/mL, P anti-NMDAR encephalitis patients had significantly increased serum CysC levels (P anti-NMDAR encephalitis and its clinical parameters and that the changes in CysC levels correlate with therapeutic effect. Therefore, our findings provide new insights into the association between serum CysC and anti-NMDAR encephalitis. © 2018 John Wiley & Sons A/S. Published by John Wiley & Sons Ltd.

  11. 1H NMR spectra of N-methyl-4-tolyl-1-(4-bromonaphthylamine and N-phenyl-1-(4-bromonaphthylamine: a combined experimental and theoretical study

    Directory of Open Access Journals (Sweden)

    Sergiy I. Okovytyy

    2014-03-01

    Full Text Available Theoretical investigations of the conformational properties and 1H NMR chemical shifts for N-methyl-4-tolyl-1-(4-bromonaphthylamine and N-phenyl-1-(4-bromonaphthylamine are reported. The calculations were performed at the DFT level (PBE1PBE functional using magnetically consistent 6-31G## and STO##-3Gmag basis sets. Conformational properties of the amines were studied using potential energy surface scanning. Chemical shifts were calculated using the GIAO and CSGT methods and averaged in proportion to the population of the corresponding conformations. Solvent effects (CDCl3 were accounted via PCM method. The obtained results allowed to assign the 1H NMR signals for the naphthalene moiety, which could not be done based on the experimental data alone.

  12. Correction procedures for C-14 dates

    International Nuclear Information System (INIS)

    McKerrell, H.

    1975-01-01

    There are two quite separate criteria to satisfy before accepting as valid the corrections to C-14 dates which have been indicated for some years now by the bristlecone pine calibration. Firstly the correction figures have to be based upon all the available tree-ring data and derived in a manner that is mathematically sound, and secondly the correction figures have to produce accurate results on C-14 dates from archaeological test samples of known historical date, these covering as wide a period as possible. Neither of these basic prerequisites has yet been fully met. Thus the two-fold purpose of this paper is to bring together, and to compare with an independently based procedure, the various correction curves or tables that have been published up to Spring 1974, as well as to detail the correction results on reliable, historically dated Egyptian, Helladic and Minoan test samples from 3100 B.C. The nomenclature followed is strictly that adopted by the primary dating journal Radiocarbon, all C-14 dates quoted thus relate to the 5568 year half-life and the standard AD/BC system. (author)

  13. Promoter methylation and large intragenic rearrangements of DPYD are not implicated in severe toxicity to 5-fluorouracil-based chemotherapy in gastrointestinal cancer patients

    International Nuclear Information System (INIS)

    Savva-Bordalo, Joana; Henrique, Rui; Jerónimo, Carmen; Ramalho-Carvalho, João; Pinheiro, Manuela; Costa, Vera L; Rodrigues, Ângelo; Dias, Paula C; Veiga, Isabel; Machado, Manuela; Teixeira, Manuel R

    2010-01-01

    Severe toxicity to 5-fluorouracil (5-FU) based chemotherapy in gastrointestinal cancer has been associated with constitutional genetic alterations of the dihydropyrimidine dehydrogenase gene (DPYD). In this study, we evaluated DPYD promoter methylation through quantitative methylation-specific PCR and screened DPYD for large intragenic rearrangements in peripheral blood from 45 patients with gastrointestinal cancers who developed severe 5-FU toxicity. DPYD promoter methylation was also assessed in tumor tissue from 29 patients Two cases with the IVS14+1G > A exon 14 skipping mutation (c.1905+1G > A), and one case carrying the 1845 G > T missense mutation (c.1845G > T) in the DPYD gene were identified. However, DPYD promoter methylation and large DPYD intragenic rearrangements were absent in all cases analyzed. Our results indicate that DPYD promoter methylation and large intragenic rearrangements do not contribute significantly to the development of 5-FU severe toxicity in gastrointestinal cancer patients, supporting the need for additional studies on the mechanisms underlying genetic susceptibility to severe 5-FU toxicity

  14. Promoter methylation and large intragenic rearrangements of DPYD are not implicated in severe toxicity to 5-fluorouracil-based chemotherapy in gastrointestinal cancer patients

    Directory of Open Access Journals (Sweden)

    Savva-Bordalo Joana

    2010-09-01

    Full Text Available Abstract Background Severe toxicity to 5-fluorouracil (5-FU based chemotherapy in gastrointestinal cancer has been associated with constitutional genetic alterations of the dihydropyrimidine dehydrogenase gene (DPYD. Methods In this study, we evaluated DPYD promoter methylation through quantitative methylation-specific PCR and screened DPYD for large intragenic rearrangements in peripheral blood from 45 patients with gastrointestinal cancers who developed severe 5-FU toxicity. DPYD promoter methylation was also assessed in tumor tissue from 29 patients Results Two cases with the IVS14+1G > A exon 14 skipping mutation (c.1905+1G > A, and one case carrying the 1845 G > T missense mutation (c.1845G > T in the DPYD gene were identified. However, DPYD promoter methylation and large DPYD intragenic rearrangements were absent in all cases analyzed. Conclusions Our results indicate that DPYD promoter methylation and large intragenic rearrangements do not contribute significantly to the development of 5-FU severe toxicity in gastrointestinal cancer patients, supporting the need for additional studies on the mechanisms underlying genetic susceptibility to severe 5-FU toxicity.

  15. Thermal Decomposition of Potential Ester Biofuels. Part I: Methyl Acetate and Methyl Butanoate

    Energy Technology Data Exchange (ETDEWEB)

    Porterfield, Jessica P.; Bross, David H.; Ruscic, Branko; Thorpe, James H.; Nguyen, Thanh Lam; Baraban, Joshua H.; Stanton, John F.; Daily, John W.; Ellison, G. Barney

    2017-06-09

    Two methyl esters have been examined as models for the pyrolysis of biofuels. Dilute samples (0.06 - 0.13%) of methyl acetate (CH3COOCH3) and methyl butanoate (CH3CH2CH2COOCH3) were entrained in (He, Ar) carrier gas and decomposed in a set of flash-pyrolysis micro-reactors. The pyrolysis products resulting from the methyl esters were detected and identified by vacuum ultraviolet photoionization mass spectrometry. Complementary product identification was provided by matrix infrared absorption spectroscopy. Pyrolysis pressures in the pulsed micro-reactor were roughly 20 Torr and residence times through the reactors were approximately 25 - 150 µs. Reactor temperatures of 300 – 1600 K were explored. Decomposition of CH3COOCH3 commences at 1000 K and the initial products are (CH2=C=O and CH3OH). As the micro-reactor is heated to 1300 K, a mixture of (CH2=C=O and CH3OH, CH3, CH2=O, H, CO, CO2) appears. The thermal cracking of CH3CH2CH2COOCH3 begins at 800 K with the formation of (CH3CH2CH=C=O, CH3OH). By 1300 K, the pyrolysis of methyl butanoate yields a complex mixture of (CH3CH2CH=C=O, CH3OH, CH3, CH2=O, CO, CO2, CH3CH=CH2, CH2CHCH2, CH2=C=CH2, HCCCH2, CH2=C=C=O, CH2=CH2, HCΞCH, CH2=C=O). Based on the results from the thermal cracking of methyl acetate and methyl butanoate, we predict several important decomposition channels for the pyrolysis of fatty acid methyl esters, R CH2-COOCH3. The lowest energy fragmentation will be a 4-center elimination of methanol to form the ketene, RCH=C=O. At higher temperatures, concerted

  16. Application of AMS 14C measurements to criminal investigations

    International Nuclear Information System (INIS)

    Nakamura, T.; Ohta, T.; Nishida, M.; Ikeda, A.; Oda, H.; Kojima, S.; Niu, E.

    2005-01-01

    14 C variations of atmospheric CO 2 as well as carbonaceous materials of human body, such as collagen fractions from teeth and bone, tissue, hair, nail, etc., of modern humans dead or alive, are influenced by 14 C produced artificially by nuclear bomb tests in the atmosphere from late 1950s to early 1960s. By careful investigation of 14 C concentration of tree rings and human tissue samples formed in this time ranges, we can establish a relation between their 14 C concentrations and calendar year. By applying this relation to a sample whose 14 C concentration can be measured, we can estimate the formation age of the sample. In addition, sources of the drugs that were used in some criminal cases can be possibly identified by the analysis of their carbon isotope ratios ( 13 C/ 12 C and 14 C/ 12 C). This method of age determination was applied to a forensic study; i.e., to two similar cases of murder. One of the two cases is for a dead body of a modern human who was killed in 1978 and buried under the floor of the house owned by the murderer. The body was excavated in 2004 according to the confession by the murderer. 14 C abundances of several pieces of hair and one tooth (the third molar) from the body were measured with accelerator mass spectrometry (AMS), and compared with the annual change on concentrations of bomb-produced 14 C. The time of death of the body was estimated to be at around 1977, and her age was from 30 to 37 years old at that time. These estimations were consistent with the real values that were revealed after the case was solved by the confession of the real murderer who gave himself up to the police. For the other case, 14 C analysis was also consistent with the fact revealed by police investigations as well as by the confession of the real murderer.

  17. PANTHER solution to the NEA-NSC 3-D PWR core transient benchmark. Uncontrolled withdrawal of control rods at zero power

    Energy Technology Data Exchange (ETDEWEB)

    Kuijper, J.C.

    1994-10-01

    This report contains the results of PANTHER calculations for the ``NEA-NSC 3-D PWR Core Transient Benchmark: Uncontrolled Withdrawal of Control Rods at Zero Power``. PANTHER was able to model the benchmark problems without modifications to the code. All the calculations were performed in 3-D. (orig.).

  18. Final PANTHER solution to the NEA-NSC3-DPWR core transient benchmark. Uncontrolled withdrawal of control rods at zero power

    International Nuclear Information System (INIS)

    Kuijper, J.C.

    1996-10-01

    This report contains the final results of PANTHER calculations for the 'NEA-NSC 3-D PWR Core Transient Benchmark: Uncontrolled Withdrawal of Control Rods at Zero Power'. PANTHER was able to model the benchmark problems without modifications to the code. All the calculations were performed in 3-D. (orig.)

  19. PANTHER solution to the NEA-NSC 3-D PWR core transient benchmark. Uncontrolled withdrawal of control rods at zero power

    International Nuclear Information System (INIS)

    Kuijper, J.C.

    1994-10-01

    This report contains the results of PANTHER calculations for the ''NEA-NSC 3-D PWR Core Transient Benchmark: Uncontrolled Withdrawal of Control Rods at Zero Power''. PANTHER was able to model the benchmark problems without modifications to the code. All the calculations were performed in 3-D. (orig.)

  20. Final PANTHER solution to the NEA-NSC3-DPWR core transient benchmark. Uncontrolled withdrawal of control rods at zero power

    Energy Technology Data Exchange (ETDEWEB)

    Kuijper, J.C.

    1996-10-01

    This report contains the final results of PANTHER calculations for the `NEA-NSC 3-D PWR Core Transient Benchmark: Uncontrolled Withdrawal of Control Rods at Zero Power`. PANTHER was able to model the benchmark problems without modifications to the code. All the calculations were performed in 3-D. (orig.).

  1. X-ray diffraction, vibrational and quantum chemical investigations of 2-methyl-4-nitroanilinium trichloroacetate trichloroacetic acid

    Science.gov (United States)

    Arjunan, V.; Marchewka, Mariusz K.; Pietraszko, A.; Kalaivani, M.

    2012-11-01

    The structural investigations of the molecular complex of 2-methyl-4-nitroaniline with trichloroacetic acid, namely 2-methyl-4-nitroanilinium trichloroacetate trichloroacetic acid (C11H10Cl6N2O6) have been performed by means of single crystal and powder X-ray diffraction method. The complex was formed with accompanying proton transfer from trichloroacetic acid molecule to 2-methyl-4-nitroaniline. The studied crystal is built up of singly protonated 2-methyl-4-nitroanilinium cations, trichloroacetate anions and neutral trichloroacetic acid molecules. The crystals are monoclinic, space group P21/c, with a = 14.947 Å, b = 6.432 Å, c = 19.609 Å and Z = 4. The vibrational assignments and analysis of 2-methyl-4-nitroanilinium trichloroacetate trichloroacetic acid have also been performed by FTIR, FT-Raman and far-infrared spectral studies. More support on the experimental findings were added from the quantum chemical studies performed with DFT (B3LYP) method using 6-31G**, cc-pVDZ, 6-31G and 6-31++G basis sets. The structural parameters, energies, thermodynamic parameters and the NBO charges of 2M4NATCA were also determined by the DFT methods.

  2. Dating human DNA with the 14C bomb peak

    Energy Technology Data Exchange (ETDEWEB)

    Kutschera, Walter; Liebl, Jakob; Steier, Peter [VERA Laboratory, University of Vienna, Vienna (Austria)

    2013-07-01

    In 1963 the limited nuclear test ban treaty stopped nuclear weapons testing in the atmosphere. By then the addition from bomb-produced {sup 14}C had doubled the {sup 14}C content of the atmosphere. Through the CO{sub 2} cycle this excess exchanged with the hydrosphere and biosphere leading to a rapidly decreasing {sup 14}C level in the atmosphere. Today we are almost back to the pre-nuclear level. As a consequence all people on Earth who lived during the second half of the 20th century were exposed to this rapidly changing {sup 14}C signal. A few years ago, a group at the Department of Cell and Molecular Biology of the Karolinska Institute in Stockholm started to use the {sup 14}C bomb peak signal in DNA to determine retrospectively the age of cells from various parts of the human body (brain, heart, fat). In a collaboration with this group, we have studied the age of olfactory bulb neurons in the human brain. For this investigation, {sup 14}C AMS measurements were developed at VERA for very small carbon samples in the range from 2 to 4 micrograms. In the presentation the general concept of {sup 14}C bomb peak dating of human DNA and several applications are discussed.

  3. The vaporization enthalpies and vapor pressures of fatty acid methyl esters C18, C21 to C23, and C25 to C29 by correlation - gas chromatography

    International Nuclear Information System (INIS)

    Chickos, James S.; Zhao Hui; Nichols, Gary

    2004-01-01

    Vapor pressures and vaporization enthalpies for methyl heptadecanoate and methyl heneicosanoate to methyl octacosanoate exclusive of methyl tricosanoate are evaluated as a function of temperature over the temperature range T = 298.15-450 K by correlation gas chromatography. The results are generated by an extrapolative process using literature values for methyl tetradecanoate to methyl eicosanoate as standards. Relationships for calculating vapor pressures of the title compounds from T = 298.15 to 450 K are provided. Experimental fusion enthalpies are also reported for the methyl esters from methyl hexadecanoate to methyl octacosanoate excluding methyl tridecanoate. Vaporization enthalpies and fusion enthalpies adjusted for temperature to T = 298.15 K are combined to provide sublimation enthalpies. The results are compared to available literature values. A rationale for the linear relationship observed between enthalpies of vaporization and enthalpies of transfer from solution to the vapor is also provided

  4. Synthesis of (R,S)-[2,3-{sup 13}C{sub 2}]-1-(1`-methyl-2`-pyrrolidinyl)propan-2-one; {l_brace}(R,S)-[2`,3`-{sup 13}C{sub 2}]hygrinePound right bracePound

    Energy Technology Data Exchange (ETDEWEB)

    Abraham, T.W.; Leete, Edward [Minnesota Univ., Minneapolis, MN (United States). Dept. of Chemistry

    1996-05-01

    2-Ethoxy-1-methyl-5-pyrrolidinone (1) was reacted with ethyl [3,4-{sup 13}C{sub 2}]-acetoacetate (2) in the presence of TiCl{sub 4} to give ethyl [3,4-{sup 13}C{sub 2}]-2-(1`-methyl-5`-oxo-2`-pyrrolidinyl)-3-oxobutanoate (3) in 85% yield. Decarboethoxylation of ethyl [3,4-{sup 13}C{sub 2}]-2-(1`-methyl-5`-oxo-2`-pyrrolidinyl)-3-oxobutan-oate (3) was accomplished using NaCl and H{sub 2}O in DMSO to give (R,S)-[2,3-{sup 13}C{sub 2}]-1-(1`-methyl-5`-oxo-2`-pyrrolidinyl)propan-2-o ne (4) in 91% yield. Protection of the ketone as a ketal (ethylene glycol, H{sup +}), followed by reduction of the amide to the amine using LiAlH{sub 4} and subsequent deprotection of the ketal gave (R,S)-[2,3-{sup 13}C{sub 2}]-1-(1`-methyl-2`-pyrrolidinyl)propan-2-one ((R,s)-[2`, 3`-{sup 13}C{sub 2}]Hygrine) (8) in 78% yield. (61% overall yield from ethyl [3,4-{sup 13}C{sub 2}]acetoacetate). (Author).

  5. In vivo potentiation of 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea by the radiation sensitizer benznidazole

    International Nuclear Information System (INIS)

    Siemann, D.W.; Morrissey, S.; Wolf, K.

    1983-01-01

    Recent studies in mouse tumor systems have indicated a potential therapeutic advantage in combining the radiosensitizer misonidazole (MISO) with cancer chemotherapy drugs. One agent the antitumor activity of which has been enhanced to a greater extent than its hematological or gastrointestinal toxicities is the nitrosourea, 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea (CCNU). Recently, sensitizers more lipophylic than MISO have been reported to give greater tumor response enhancement when combined with CCNU. The present studies compared the potential therapeutic benefit of combining MISO (partition coefficient, 0.43) or benznidazole (BENZO) (partition coefficient, 8.5) in KHT sarcoma or RIF-1 tumor-bearing C3H mice. Both sensitizers were administered i.p. and given either 30 min before (BENZO) or simultaneously with (MISO) the chemotherapeutic agent. Survival of clonogenic tumor cells assessed 22 to 24 hr after treatment or in situ tumor growth delay were used as assays of tumor response. Normal tissue toxicity was determined using the drug dose yielding 50% animal lethality in 30 days end point. When combined with CCNU, doses of MISO (5.0 mmol/kg) or BENZO (0.3 mmol/kg) were found to yield approximately equivalent increases in both the tumor effect (enhancement ratio, approximately 1.8 to 2.0) and normal tissue toxicity (enhancement ratio approximately 1.3 to 1.4). Both sensitizers therefore led to a therapeutic benefit. However, although a approximately 10-fold lower dose of the more lipophylic sensitizer BENZO proved to be as effective as MISO at enhancing the tumoricidal effects of CCNU, this dose reduction did not result in a greater therapeutic gain for BENZO

  6. Two new C-methyl flavanones from the rhizomes and frond bases of Matteuccia struthiopteris

    Czech Academy of Sciences Publication Activity Database

    Zhang, D.; Li, S. B.; Li, Y. J.; Zhu, X. X.; Kmoníčková, Eva; Zídek, Zdeněk; Fu, M. H.; Fang, J.

    2013-01-01

    Roč. 15, č. 11 (2013), s. 1163-1167 ISSN 1028-6020 R&D Projects: GA MŠk(CZ) ME10116 Institutional support: RVO:68378041 Keywords : Onocleaceae * Matteuccia struthiopteris * C-methyl flavanones Subject RIV: FR - Pharmacology ; Medidal Chemistry Impact factor: 0.968, year: 2013

  7. A critical review of atmospheric 14 C activities

    International Nuclear Information System (INIS)

    Krajcar Bronic, I.; Horvatincic, N.; Baresic, J.; Obelic, B.; Vreca, P.

    2006-01-01

    14 C activity of atmospheric CO 2 has been measured at the Rudjer Boskovi Institute as a part of environmental monitoring in order to determine possible differences between clean-air sites, industrialized city and sites in the vicinity of nuclear power plant. Samples of CO 2 from the atmosphere have been collected by absorption of CO 2 on the saturated carbonate-free NaOH solution for a period of 1 month under stationary conditions. The obtained Na 2 CO 3 has been dissolved in HCl and the produced CO 2 used for CH 4 preparation by catalytic reaction with H 2 at 450 degrees Celsius. A gas proportional counter filled with CH 4 has been used for 14 C activity measurement. The method of collection of CO 2 does not require any power source and can be therefore used for sampling at the remote sites, such as mountains or forests. However,due to the lack of mixing of the Na OH solution, the absorption process is limited on the surface of the solution, and there exists the possibility of fractionation of carbon isotopes due to different reaction rate constants of 12 C and 13 C. A continuous record of atmospheric 14 CO 2 activity exists for the city of Zagreb (1986 to 2005), while shorter records (1-2 years) exist for several other sites of various characteristics: two clean-air sites (Mt. Medvednica, altitude about 1000 m a.s.l., for period 1995 to 1996, and the Plitvice National Park for period 2003 to 2005), and a site close to the Nuclear Power Plant Krsko (1984 to 1986).Within the bilateral Croatian-Slovene project we have recently measured also the stable isotope composition (δ13 C) of Na 2 CO 3 collected at two different sampling sites in order to determine seasonal fluctuations in both 14 C and 13 C isotope composition. Unexpectedly low δ13 C values have been obtained about (-25±2)0/00 instead of expected (-7±1)0/00. Such low values have been attributed to the carbon isotope fractionation during the CO 2 absorption on the highly alkaline medium because of

  8. 14CO2-assimilation, translocation of 14C, and 14C-carbonate uptake in different organs of spring barley plants in relation to adult-plant resistance to powdery mildew

    International Nuclear Information System (INIS)

    Hwang, B.K.; Ibenthal, W.-D.; Heitefuss, R.

    1986-01-01

    The cultivar Peruvian of spring barley, which is susceptible at all growth stages, and Asse, which exhibits adult-plant resistance to powdery mildew, were compared in 14 CO 2 assimilation, distribution of 14 C, and 14 C-carbonate uptake in different organs of healthy and infected plants. The reduction of 14 CO 2 assimilation in infected plants at the first and fourth leaf stages was greater in Peruvian than in Asse. In Peruvian, the 14 C which was fixed by the infected third leaf of plants with mildew on the lower 3 leaves remained in the third leaves with very little translocation to other parts of the plant. Infection of the lower three leaves at the fourth leaf stage reduced 14 CO 2 assimilation in noninfected fourth leaves of Asse less than that of Peruvian, but the flow of 14 C from the healthy fourth leaves into other plant parts such as leaf sheaths was markedly stimulated in Peruvian compared to Asse. Infection also reduced the uptake of 14 C-carbonate by seedling roots, the reduction being greater in Peruvian than Asse. A greater proportion of the 14 C absorbed by roots of Asse was translocated to the infected leaves than that of Peruvian. It was concluded that powdery mildew disrupted the normal pattern of photosynthesis and translocation of metabolites in a susceptible cultivar more markedly than in an adult-plant-resistant cultivar of spring barley. (author)

  9. Increase in the penetration of tracer compounds into the rat brain during 2-methyl-4-chlorophenoxyacetic acid (MCPA) intoxication

    International Nuclear Information System (INIS)

    Elo, H.A.; Ylitalo, P.; Kyoettilae, J.; Hervonen, H.

    1982-01-01

    The penetration of different intravenous tracer molecules such as 14 C-labelled 2-methyl-4-chlorophenoxyacetic acid ( 14 C-MCPA), 14 C-p-aminobenzoic acid ( 14 C-PABA), 14 C-sucrose, 14 C-antipyrine and iodinated ( 125 I) human albumin ( 125 I-HA) into the brain and cerebrospinal fluid (CSF) was studied in MCPA-intoxicated and control rats. Toxic subcutaneous doses of sodium salt of MCPA (200-500 mg/kg) increased highly the brain/plasma and CSF/plasma ratios of 14 C-MCPA and 14 C-PABA, as compared to the muscle/plasma ratio. Probenecid (200 mg/kg) did not affect the cerebral MCPA concentration in the intoxicated animals. The tissue/plasma ratios of 14 C-sucrose, 14 C-antipyrine and 125 I-HA were also increased in the brain and CSF of intoxicated animals, but the increases were less pronounced than those of 14 C-MCPA or 14 C-PABA. The results indicate that MCPA intoxication caused a selective damage of the blood-brain barrier in the brain areas studied. (author)

  10. Using atmospheric 14CO to constrain OH variability: concept and potential for future measurements

    Science.gov (United States)

    Petrenko, V. V.; Murray, L. T.; Smith, A. W.

    2017-12-01

    The primary source of 14C-containing carbon monoxide (14CO) in the atmosphere is via 14C production from 14N by secondary cosmic rays, and the primary sink is removal by OH. Variations in the global abundance of 14CO that are not explained by variations in 14C production are mainly driven by variations in the global abundance of OH. Monitoring OH variability via methyl chloroform is becoming increasingly difficult as methyl chloroform abundance is continuing to decline. Measurements of atmospheric 14CO have previously been successfully used to infer OH variability. However, these measurements are currently only continuing at one location (Baring Head, New Zealand), which is insufficient to infer global trends. We propose to restart global 14CO monitoring with the aim of providing another constraint on OH variability. A new analytical system for 14CO sampling and measurements is in development, which will allow to strongly reduce the required sample air volumes (previously ≥ 400 L) and simplify field logistics. A set of test measurements is planned, with sampling at the Mauna Loa Observatory. Preliminary work with a state-of-the-art chemical transport model is identifying the most promising locations for global 14CO sampling.

  11. NSC confirms principles for safety review on Radioactive Waste Burial Facilities

    International Nuclear Information System (INIS)

    Anon.

    1988-01-01

    The Nuclear Safety Commission authorized the scope of Principles for Safety Examination on Radioactive Waste Burial Facilities as suitable, the draft report for which was established by the Special Committee on Safety Standards of Radioactive Waste (Chairman Prof. Masao Sago, Science University of Tokyo) and reported on March 10 to the NSC. The principles include the theory that the facility must be controlled step by step, corresponding to the amount of radioactivity over 300 to 400 years after the burial of low-level solid radioactive waste with site conditions safe even in the event of occurrence of a natural disaster. The principles will be used for administrative safety examination against the application of the business on low-level radioactive waste burial facility which Japan Nuclear Fuel Industries, Inc. is planning to install at Rokkashomura, Aomori Prefecture. (author)

  12. Processing ix spent resin waste for C-14 isotope recovery

    International Nuclear Information System (INIS)

    Chang, F. H.; Woodall, K. B.; Sood, S. K.; Vogt, H. K.; Krochmainek, L. S.

    1991-01-01

    A process developed at Ontario Hydro for recovering carbon-14 (C-14) from spent ion exchange resin wastes is described. Carbon-14 is an undesirable by-product of CANDU 1 nuclear reactor operation. It has an extremely long (5730 years) half-life and can cause dosage to inhabitants by contact, inhalation, or through the food cycle via photosynthesis. Release of carbon-14 to the environment must be minimized. Presently, all the C-14 produced in the Moderator and Primary Heat Transport (PHT) systems of the reactor is effectively removed by the respective ion exchange columns, and the spent ion exchange resins are stored in suitably engineered concrete structures. Because of the large volumes of spent resin waste generated each year this method of disposal by long term storage tends to be uneconomical; and may also be unsatisfactory considering the long half-life of the C-14. However, purified C-14 is a valuable commercial product for medical, pharmaceutical, agricultural, and organic chemistry research. Currently, commercial C-14 is made artificially in research reactors by irradiating aluminum nitride targets for 4.5 years. If the C-14 containing resin waste can be used to reduce this unnecessary production of C-14, the total global build-up of this radioactive chemical can be reduced. There is much incentive in removing the C-14 from the resin waste to reduce the volume of C-14 waste, and also in purifying the recovered C-14 to supply the commercial market. The process developed by Ontario Hydro consists of three main steps: C-14 removal from spent resins, enrichment of recovered C-14, and preparation of final product. Components of the process have been successfully tested at Ontario Hydro's Research Division, but the integration of the process is yet to be demonstrated. A pilot scale plant capable of processing 4 m 3 of spent resins annually is being planned for demonstrating the technology. The measured C-14 activity levels on the spent resins ranged from 47

  13. Synthesis of 1-benzyl-4-((5,6-dimethoxy(2- sup 14 C)-1-indanon)-2-YL)-methylpiperidine hydrochloride (E2020- sup 14 C)

    Energy Technology Data Exchange (ETDEWEB)

    Iimura, Youichi; Mishima, Mannen; Sugimoto, Hachiro (Eisai Co., Ltd., Ibaraki (Japan). Tsukuba Research Labs.)

    1989-07-01

    1-Benzyl-4-((5,6-dimethoxy(2-{sup 14}C)-1-indanon)-2-yl)-methylpiperidine hydrochloride (E2020-{sup 14}C), and acetylcholinesterase inhibitor for studying the pharmacokinetic profiles of E2020, was synthesized from 5,6-dimethoxy(2-{sup 14}C)-1-indanone as the labelled starting material. (author).

  14. DNA methylation mediates the effect of maternal cognitive appraisal of a disaster in pregnancy on the child's C-peptide secretion in adolescence: Project Ice Storm.

    Directory of Open Access Journals (Sweden)

    Lei Cao-Lei

    Full Text Available Animal and human studies suggest that prenatal exposure to stress is associated with adverse health outcomes such as type 2 diabetes. Epigenetic modification, such as DNA methylation, is considered one possible underlying mechanism. The 1998 Quebec ice storm provides a unique opportunity to study an independent prenatal stressor on child outcomes. C-peptide is the best measure of endogenous insulin secretion and is widely used in the clinical management of patients with diabetes. The objectives of this study are to determine 1 the extent to which prenatal exposure to disaster-related stress (maternal objective hardship and maternal cognitive appraisal influences children's C-peptide secretion, and 2 whether DNA methylation of diabetes-related genes mediates the effects of prenatal stress on C-peptide secretion. Children's (n = 30 C-peptide secretion in response to an oral glucose tolerance test were assessed in blood at 13½ years. DNA methylation levels of selected type 1 and 2 diabetes-related genes were chosen based upon the genes associated with prenatal maternal objective hardship and/or cognitive appraisal levels. Bootstrapping analyses were performed to determine the mediation effect of DNA methylation. We found that children whose mothers experienced higher objective hardship exhibited higher C-peptide secretion. Cognitive appraisal was not directly associated with C-peptide secretion. DNA methylation of diabetes-related genes had a positive mediation effect of objective hardship on C-peptide secretion: higher objective hardship predicted higher C-peptide secretion through DNA methylation. Negative mediation effects of cognitive appraisal were observed: negative cognitive appraisal predicted higher C-peptide secretion through DNA methylation. However, only one gene, LTA, remained a significant mediator of cognitive appraisal on C-peptide secretion after the conservative Bonferroni multiple corrections. Our findings suggest that DNA

  15. Photosynthetic incorporation of 14C by Stevia rebaudiana

    International Nuclear Information System (INIS)

    Ferraresi, M. de L.; Ferraresi Filho, O.; Bracht, A.

    1985-01-01

    The photosynthetic incorporation of 14 by Stevia rebaudiana specimens was investigated. The 14 C incorporation, when the isotope was furnished to the plant in form of 14 CO 2 , was rapid. After 24 hours, the radioactivity has been incorporated into a great number of compounds including pigments, terpenes, glucose, cellulose and also stevioside and its derivatives. (M.A.C.) [pt

  16. Methylation of ribonucleic acid by the carcinogens dimethyl sulphate, N-methyl-N-nitrosourea and N-methyl-N′-nitro-N-nitrosoguanidine. Comparisons of chemical analyses at the nucleoside and base levels

    Science.gov (United States)

    Lawley, P. D.; Shah, S. A.

    1972-01-01

    1. The following methods for hydrolysis of methyl-14C-labelled RNA, and for chromatographic isolation and determination of the products, were investigated: enzymic digestion to nucleosides at pH6 or 8; alkaline hydrolysis and conversion into nucleosides; hydrolysis by acid to pyrimidine nucleotides and purine bases, or completely to bases; chromatography on Dowex 50 (NH4+ form) at pH6 or 8.9, or on Dowex 50 (H+ form), or on Sephadex G-10. 2. The suitability of the various methods for determination of methylation products was assessed. The principal product, 7-methylguanosine, was unstable under the conditions used for determinations of nucleosides. 3- and 7-Methyladenine and 3- and 7-methylguanine are best determined as bases; 1-methyladenine and 3-methylcytosine can be isolated as either nucleosides or bases; O6-methylguanine is unstable under the acid hydrolysis conditions used and can be determined as the nucleoside; 3-methyluracil was detected, but may be derived from methylation of the ionized form of uracil. 3. Differences between the patterns of methylation of RNA and homopolyribonucleotides by the N-methyl-N-nitroso compounds and dimethyl sulphate were found: the nitroso compounds were able to methylate O-6 of guanine, were relatively more reactive at N-7 of adenine and probably at N-3 of guanine, but less reactive at N-1 of adenine, N-3 of cytosine and probably at N-3 of uridine. They probably reacted more with the ribose–phosphate chain, but no products from this were identified. 4. The possible influences of these differences on biological action of the methylating agents is discussed. Nitroso compounds may differ principally in their ability to induce miscoding in the Watson–Crick sense by reaction at O-6 of guanine. Both types of agent may induce miscoding to a lesser extent through methylation at N-3 of guanine; both can methylate N atoms, presumably preventing Watson–Crick hydrogen-bonding. N-Methyl-N-nitrosourea can degrade RNA, possibly

  17. Residues of 14C-cyolane in cottonseed products

    International Nuclear Information System (INIS)

    Zayed, S.M.A.D.; Osman, A.Z.; Fakhr, I.M.I.; Bahig, M.E.

    1981-01-01

    The systemic insecticide cyolane [2-(0,0-diethylphosphoryl)-imino-1,3-dithiolane] was prepared from 14 C-ethanol, phosphorus oxychloride and 2-amino-1,3-dithiolane. Cotton plants were treated with two applications of the insecticide under conditions of local agricultural practice. 14 C-residues in the crude oil and cake of the harvested cotton seeds amounted to 1.63 and 0.014 mg/kg respectively. About 50% of the 14 C-activity present in the crude oil was found to be eliminated by simulated commercial processes used for refining of the oil. Alkali treatment and bleaching removed 16% and 25% of the radioactive residues respectively. Winterization of the bleached oil at 5-7 0 C for 3 days effected a further elimination of 13%. 14 C-residues in the cotton seed products and in the samples of the refined oil were characterized and the main constituents identified using chromatographic techniques. (author)

  18. Environmental background 14C levels in Japan in 1990s

    International Nuclear Information System (INIS)

    Fuma, Shoichi; Inoue, Yoshikazu; Miyamoto, Kiriko; Takeda, Hiroshi; Iwakura, Tetsuo; Arai, Kiyohiko; Kashida, Yoshihiko; Ichimasa, Yusuke

    2002-01-01

    For assessment of radiation doses due to 14 C released from nuclear facilities, it is necessary to know the background level of environmental 14 C originated from the natural cosmic-ray production and the past atmospheric nuclear weapons tests. The authors selected grapes as an indicator of 14 C levels in the environment including atmosphere, and determined the specific activities of 14 C in ethanol extracted from wine made from grapes cultivated in several prefectures or unknown places in Japan in each year from 1990 to 2000. The specific activities of 14 C were almost uniform all over Japan in each year, though they showed the weak tendency to slightly decrease with increasing population densities in the prefecture where the wine grapes were cultivated. It is considered that this small regional variation in the specific activities of 14 C arose from Suess effect, because population densities can be regarded as an index of the amount of CO 2 emission from fossil-fuel combustion. The specific activities of 14 C gradually decreased in the 1990s. That is, they were 260 mBq/gC in 1990, and became 244 mBq/gC in 2000. This 14 C level in 2000 was still about 7% higher than the pre-bomb level. The decrease in 14 C originated from the past atmospheric nuclear weapons tests could be described by a single exponential function with a half-time of 10.3 years in 1990s. This half-time was shorter than that in the Europe, Canada and the South Pacific. This difference in the decreasing rate between Japan and other countries may be explained by a fact that the amount of CO 2 emission from fossil-fuel combustion continued to increase in Japan in this period. The specific activities of 14 C in wine ethanol determined in this study showed good agreement with those in atmospheric CO 2 predicted by a mathematical model. They were also in the same levels as the 14 C specific activities in atmospheric CO 2 , tree leaves, grass and plant food in Japan and other countries, which were

  19. Inhibition of protein synthesis by N-methyl-N-nitrosourea in vivo

    Science.gov (United States)

    Kleihues, P.; Magee, P. N.

    1973-01-01

    1. The intraperitoneal injection of N-methyl-N-nitrosourea (100mg/kg) caused a partial inhibition of protein synthesis in several organs of the rat, the maximum effect occurring after 2–3h. 2. In the liver the inhibition of protein synthesis was paralleled by a marked disaggregation of polyribosomes and an increase in ribosome monomers and ribosomal subunits. No significant breakdown of polyribosomes was found in adult rat brains although N-methyl-N-nitrosourea inhibited cerebral and hepatic protein synthesis to a similar extent. In weanling rats N-methyl-N-nitrosourea caused a shift in the cerebral polyribosome profile similar to but less marked than that in rat liver. 3. Reaction of polyribosomal RNA with N-[14C]methyl-N-nitrosourea in vitro did not lead to a disaggregation of polyribosomes although the amounts of 7-methylguanine produced were up to twenty times higher than those found after administration of sublethal doses in vivo. 4. It was concluded that changes in the polyribosome profile induced by N-methyl-N-nitrosourea may reflect the mechanism of inhibition of protein synthesis rather than being a direct consequence of the methylation of polyribosomal mRNA. PMID:4774397

  20. Synthesis of phenobarbital {sup 14}C - 5 (1964); Synthese du phenobarbital {sup 14}C - 5 (1964)

    Energy Technology Data Exchange (ETDEWEB)

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

    1964-07-01

    Phenobarbital (Luminal), well known as a hypnotic agent, plays also an important role in the medical treatment of epilepsy. With the object of studying the metabolism of this medicament in the living system, the synthesis of phenobarbital marked in position 2 of the pyrimidinic ring has been effected. It has been necessary, in order to carry out to research into the metabolism of this product, to have a phenobarbital marked in position 5 of the pyrimidinic ring. This synthesis, making it possible to introduce C-14 into position 5 of the pyrimidinic ring, consists of seven stages starting from C-14 carboxyl benzoic acid having a specific activity of 25 mc/mM. The melting point of the final product is 172 - 173 deg. C and its specific activity is 11.15 mc/mM. The overall radioactive yield of the pure product, with respect to the original benzoic acid (10 mM) is of the order of 3 per cent. The purity of the product has been controlled by paper chromatography; it is of the order of 99 per cent. (author) [French] Le phenobarbital (Luminal) bien connu comme agent hypnotique, joue egalement un role important dans la medication anti-epileptique. Pour l'etude du metabolisme de ce medicament dans l'organisme vivant, nous avons synthetise le phenobarbital marque en position 2 du cycle pyrimidinique. Afin de poursuivre la recherche du metabolisme de ce produit, il a ete necessaire de disposer du phenobarbital marque en position 5 du cycle. pyrimidinique. Cette synthese, permettant l'introduction du {sup 14}C en position 5 du cycle pyrimidinique, comporte sept etapes, au depart de l'acide benzoique carboxyle {sup 14}C, d'une activite specifique de 25 mc/mM. Point de fusion du produit final: 172 - 173 deg. C Activite specifique: 11,15 mC/mM. Rendement total radioactif du produit pur, par rapport a l'acide benzoique de depart sur 10 mM, de l'ordre de 3 pour cent. La purete du produit a ete controlee par chromatographie sur papier; elle est de l'ordre de 99 pour cent. (auteur)

  1. Distribution of 14C in soil and rice plants following application of 14C - parathion to soil

    International Nuclear Information System (INIS)

    Andrea, M.M. de; Ruegg, E.F.

    1983-01-01

    Amount of residues of 14 C-parathion in soil rice plants after application of the insecticide to soil were determined in four systems studied during five weeks: pots of soil with and without plants and open or enclosed by a transparent cover. Measurements of amounts volatilized and 14 CO 2 evolution from the pesticide were made in closed system without plants. The bound residues in soil and plants were also determined. Results indicated that parathion half life in a Gley Humic soil was about two weeks. Very little radiocarbon was taken up by rice plants; of this, more was found in shoots of plants enclosed, probably by collection of the volatilized material by plants. About 6% and 4% of the 14 C-parathion were found as volatilized material and 14 CO 2 , respectively after five weeks. Bound residues varied very little and reached a maximum of 22% in soil and in plants amounted to less than 2% at the final of the experiment. (Author) [pt

  2. Synthesis of 14C labelled lidocaine (α-diethylamino acet-2,6-dimethylanilide)

    International Nuclear Information System (INIS)

    Zhou Zhentang; Qian Guojun; Lin Fenzhi; Zhuang Daoling; Zhang Yulong; He Zhanjun

    2002-01-01

    14 C-lidocaine was composed by 14 C-diethylamine reaction with ω-chloroacetic-2,6-dimethylaniline. 14 C-diethylamine was prepared from Ba 14 CO 3 via K 14 CN and 14 C-acetonitrile which was hydrogenated. Radiochemical purity of 14 C-diethylamine and 14 C-lidocaine is >99% by HPLC and TLC respectively. 14 C-lidocaine is needed for breath assay of mouse for measuring liver function

  3. FAST GC-FID METHOD FOR MONITORING ACIDIC AND BASIC CATALYTIC TRANSESTERIFICATION REACTIONS IN VEGETABLE OILS TO METHYL ESTER BIODIESEL PREPARATION

    Directory of Open Access Journals (Sweden)

    Renata Takabayashi Sato

    2016-04-01

    Full Text Available A fast gas chromatography with a flame ionisation detector (GC-FID method for the simultaneous analysis of methyl palmitate (C16:0, stearate (C18:0, oleate (C18:1, linoleate (C18:2 and linolenate (C18:3 in biodiesel samples was proposed. The analysis was conducted in a customised ionic-liquid stationary-phase capillary, SLB-IL 111, with a length of 14 m, an internal diameter of 0.10 mm, a film thickness of 0.08 µm and operated isothermally at 160 °C using hydrogen as the carrier gas at a rate of 50 cm s-1 in run time about 3 min. Once methyl myristate (C14:0 is present lower than 0.5% m/m in real samples it was used as an internal standard. The method was successful applied to monitoring basic and acidic catalysis transesterification reactions of vegetable oils such as soybean, canola, corn, sunflower and those used in frying process.

  4. Perdeuteration and methyl-selective 1H, 13C-labeling by using a Kluyveromyces lactis expression system

    International Nuclear Information System (INIS)

    Miyazawa-Onami, Mayumi; Takeuchi, Koh; Takano, Toshiaki; Sugiki, Toshihiko; Shimada, Ichio; Takahashi, Hideo

    2013-01-01

    The production of stable isotope-labeled proteins is critical in structural analyses of large molecular weight proteins using NMR. Although prokaryotic expression systems using Escherichia coli have been widely used for this purpose, yeast strains have also been useful for the expression of functional eukaryotic proteins. Recently, we reported a cost-effective stable isotope-labeled protein expression using the hemiascomycete yeast Kluyveromyces lactis (K. lactis), which allow us to express exogenous proteins at costs comparable to prokaryotic expression systems. Here, we report the successful production of highly deuterated (>90 %) protein in the K. lactis system. We also examined the methyl-selective 1 H, 13 C-labeling of Ile, Leu, and Val residues using commonly used amino acid precursors. The efficiency of 1 H- 13 C-incorporation varied significantly based on the amino acid. Although a high level of 1 H- 13 C-incorporation was observed for the Ile δ1 position, 1 H, 13 C-labeling rates of Val and Leu methyl groups were limited due to the mitochondrial localization of enzymes involved in amino acid biosynthesis and the lack of transporters for α-ketoisovalerate in the mitochondrial membrane. In line with this notion, the co-expression with branched-chain-amino-acid aminotransferase in the cytosol significantly improved the incorporation rates of amino acid precursors. Although it would be less cost-effective, addition of 13 C-labeled valine can circumvent problems associated with precursors and achieve high level 1 H, 13 C-labeling of Val and Leu. Taken together, the K. lactis system would be a good alternative for expressing large eukaryotic proteins that need deuteration and/or the methyl-selective 1 H, 13 C-labeling for the sensitive detection of NMR resonances

  5. Degradation and residues of trifluralin and metalaxyl in soils treated with 14C-trifluralin and 14C-metalaxyl, under laboratory conditions

    International Nuclear Information System (INIS)

    Musumeci, M.R.; Ruegg, E.F.

    1986-01-01

    The behavior of the herbicide 14 C-trifluralin and the fungicide 14 C-metalaxyl was studied under laboratory conditions in Red Latosol and Yellow Red Podzol soils in samples Kept flooded, sterilized and with humidity equivalent to 60% of the water field capacity. The degradation of both pesticides is discussed. (M.A.C.) [pt

  6. Radiolytic decomposition of organic C-14 released from TRU waste

    International Nuclear Information System (INIS)

    Kani, Yuko; Noshita, Kenji; Kawasaki, Toru; Nishimura, Tsutomu; Sakuragi, Tomofumi; Asano, Hidekazu

    2007-01-01

    It has been found that metallic TRU waste releases considerable portions of C-14 in the form of organic molecules such as lower molecular weight organic acids, alcohols and aldehydes. Due to the low sorption ability of organic C-14, it is important to clarify the long-term behavior of organic forms under waste disposal conditions. From investigations on radiolytic decomposition of organic carbon molecules into inorganic carbonic acid, it is expected that radiation from TRU waste will decompose organic C-14 into inorganic carbonic acid that has higher adsorption ability into the engineering barriers. Hence we have studied the decomposition behavior of organic C-14 by gamma irradiation experiments under simulated disposal conditions. The results showed that organic C-14 reacted with OH radicals formed by radiolysis of water, to produce inorganic carbonic acid. We introduced the concept of 'decomposition efficiency' which expresses the percentage of OH radicals consumed for the decomposition reaction of organic molecules in order to analyze the experimental results. We estimated the effect of radiolytic decomposition on the concentration of organic C-14 in the simulated conditions of the TRU disposal system using the decomposition efficiency, and found that the concentration of organic C-14 in the waste package will be lowered when the decomposition of organic C-14 by radiolysis was taken into account, in comparison with the concentration of organic C-14 without radiolysis. Our prediction suggested that some amount of organic C-14 can be expected to be transformed into the inorganic form in the waste package in an actual system. (authors)

  7. Studies on molecular structure, vibrational spectra and molecular docking analysis of 3-Methyl-1,4-dioxo-1,4-dihydronaphthalen-2-yl 4-aminobenzoate

    Science.gov (United States)

    Suresh, D. M.; Amalanathan, M.; Hubert Joe, I.; Bena Jothy, V.; Diao, Yun-Peng

    2014-09-01

    The molecular structure, vibrational analysis and molecular docking analysis of the 3-Methyl-1,4-dioxo-1,4-dihydronaphthalen-2-yl 4-aminobenzoate (MDDNAB) molecule have been carried out using FT-IR and FT-Raman spectroscopic techniques and DFT method. The equilibrium geometry, harmonic vibrational wave numbers, various bonding features have been computed using density functional method. The calculated molecular geometry has been compared with experimental data. The detailed interpretation of the vibrational spectra has been carried out by using VEDA program. The hyper-conjugative interactions and charge delocalization have been analyzed using natural bond orbital (NBO) analysis. The simulated FT-IR and FT-Raman spectra satisfactorily coincide with the experimental spectra. The PES and charge analysis have been made. The molecular docking was done to identify the binding energy and the Hydrogen bonding with the cancer protein molecule.

  8. Studies on residues of 14C malathion in soils

    International Nuclear Information System (INIS)

    Ghezal, F.; Bennaceur, M.

    1991-04-01

    The extractability, the mobility and formation of bound 14C labelled residues in two soils under normal conditions were investigated with malathion. Comparison is made between irradiated and autoclaved soils. The highest concentration of the product is found in the first section (0-4cm) after experiment. Three compounds were found in the soils. 14C malathion is decomposed to 14C02. The degradation is more important in organic matter rich soil. In rich soil, 50% of 14C product is degradated after 17 days. This percentage is only 10%, for poor soil. The 14CO 2 produced in non-sterile soil is 33,05%. This percentage is respectively 10,92% and 3,57% only for irradiated and autoclaved soils

  9. (a, deletion; b, methylation; c, overall alterations) of SLIT2, ROBO1

    Indian Academy of Sciences (India)

    author

    Table 3. Associations between alterations (a, deletion; b, methylation; c, overall alterations) of SLIT2, ROBO1/ ROBO2. genes in BC. *P≤0.05. SLIT2. ROBO1. ROBO2. SLIT2. ROBO1. ROBO2. SLIT2. ROBO1. ROBO2. D+. D-. D+. D-. D+. D-. M+. M-. M+. M-. M+. M-. A+. A-. A+. A-. A+. A-. SLIT2. D+. -. -. 21. 37. 4. 54. SLIT2. M+.

  10. A novel stereospecific synthesis of 14C labeled 1-glutamic acid

    International Nuclear Information System (INIS)

    Wurz, R.E.; Kepner, R.E.; Webb, A.D.

    1989-01-01

    A stereospecific synthesis of 4- 14 C-1-glutamic acid was completed in five steps from sodium 2- 14 C-acetate. The morpholine derived enamine of ethyl pyruvate was reacted with ethyl 2- 14 C-bromoacetate to give after hydrolysis diethyl 4- 14 C-2-oxoglutarate. The 2-oxoglutarate was reacted with hydroxylamine hydrochloride to give diethyl 4-14C-2-hydroxyiminoglutarate which was then reduced with a LiAlH4, (-)-N-methylephedrine and 3,5-dimethylphenol mixture to give 4- 14 C-1-glutamic acid. The 4- 14 C-1-glutamic acid was used in investigations into the biosynthesis of gamma-lactones in sherries

  11. METABOLISM OF [14C]GA19 AND [14C]GA53 BY ECOTYPES OF ...

    African Journals Online (AJOL)

    ADMIN

    hand, metabolism of [14C]GA53 was very limited in all day-length treatments and during both, day and night periods. ... compounds which are formed by covalent coupling of GAs to .... For each ecotype day-time and night-time metabolism of ...

  12. 5-Fluorouracil and 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea (CCNU) followed by hydroxyurea, misonidazole, and irradiation for brain stem gliomas: a pilot study of the Brain Tumor Research Center and the Childrens Cancer Group

    International Nuclear Information System (INIS)

    Levin, V.A.; Edwards, M.S.; Wara, W.M.; Allen, J.; Ortega, J.; Vestnys, P.

    1984-01-01

    Twenty-eight evaluable children with the diagnosis of brain stem glioma were treated with 5-fluorouracil and CCNU before posterior fossa irradiation (5500 rads); during irradiation, the children received hydroxyurea and misonidazole. The treatment was well tolerated, and minimal toxicity was produced. The median relapse-free survival was 32 weeks, and the median survival was 44 weeks. Analysis of covariates showed that, in patients between the ages of 2 and 19 years, survival was longest in the older children (P less than 0.02). Tumor histology, sex, extent of operation (if any), Karnofsky score, and radiation dose did not correlate with survival

  13. Measurements of 14C in ancient ice from Taylor Glacier, Antarctica constrain in situ cosmogenic 14CH4 and 14CO production rates

    Science.gov (United States)

    Petrenko, Vasilii V.; Severinghaus, Jeffrey P.; Schaefer, Hinrich; Smith, Andrew M.; Kuhl, Tanner; Baggenstos, Daniel; Hua, Quan; Brook, Edward J.; Rose, Paul; Kulin, Robb; Bauska, Thomas; Harth, Christina; Buizert, Christo; Orsi, Anais; Emanuele, Guy; Lee, James E.; Brailsford, Gordon; Keeling, Ralph; Weiss, Ray F.

    2016-03-01

    Carbon-14 (14C) is incorporated into glacial ice by trapping of atmospheric gases as well as direct near-surface in situ cosmogenic production. 14C of trapped methane (14CH4) is a powerful tracer for past CH4 emissions from ;old; carbon sources such as permafrost and marine CH4 clathrates. 14C in trapped carbon dioxide (14CO2) can be used for absolute dating of ice cores. In situ produced cosmogenic 14C in carbon monoxide (14CO) can potentially be used to reconstruct the past cosmic ray flux and past solar activity. Unfortunately, the trapped atmospheric and in situ cosmogenic components of 14C in glacial ice are difficult to disentangle and a thorough understanding of the in situ cosmogenic component is needed in order to extract useful information from ice core 14C. We analyzed very large (≈1000 kg) ice samples in the 2.26-19.53 m depth range from the ablation zone of Taylor Glacier, Antarctica, to study in situ cosmogenic production of 14CH4 and 14CO. All sampled ice is >50 ka in age, allowing for the assumption that most of the measured 14C originates from recent in situ cosmogenic production as ancient ice is brought to the surface via ablation. Our results place the first constraints on cosmogenic 14CH4 production rates and improve on prior estimates of 14CO production rates in ice. We find a constant 14CH4/14CO production ratio (0.0076 ± 0.0003) for samples deeper than 3 m, which allows the use of 14CO for correcting the 14CH4 signals for the in situ cosmogenic component. Our results also provide the first unambiguous confirmation of 14C production by fast muons in a natural setting (ice or rock) and suggest that the 14C production rates in ice commonly used in the literature may be too high.

  14. Electrolyte-gated transistors based on phenyl-C61-butyric acid methyl ester (PCBM) films: bridging redox properties, charge carrier transport and device performance.

    Science.gov (United States)

    Lan, Tian; Soavi, Francesca; Marcaccio, Massimo; Brunner, Pierre-Louis; Sayago, Jonathan; Santato, Clara

    2018-05-24

    The n-type organic semiconductor phenyl-C61-butyric acid methyl ester (PCBM), a soluble fullerene derivative well investigated for organic solar cells and transistors, can undergo several successive reversible, diffusion-controlled, one-electron reduction processes. We exploited such processes to shed light on the correlation between electron transfer properties, ionic and electronic transport as well as device performance in ionic liquid (IL)-gated transistors. Two ILs were considered, based on bis(trifluoromethylsulfonyl)imide [TFSI] as the anion and 1-ethyl-3-methylimidazolium [EMIM] or 1-butyl-1-methylpyrrolidinium [PYR14] as the cation. The aromatic structure of [EMIM] and its lower steric hindrance with respect to [PYR14] favor a 3D (bulk) electrochemical doping. As opposed to this, for [PYR14] the doping seems to be 2D (surface-confined). If the n-doping of the PCBM is pursued beyond the first electrochemical process, the transistor current vs. gate-source voltage plots in [PYR14][TFSI] feature a maximum that points to the presence of finite windows of high conductivity in IL-gated PCBM transistors.

  15. Forensic applications of 14C bomb-pulse dating

    International Nuclear Information System (INIS)

    Zoppi, U.; Skopec, Z.; Skopec, J.; Jones, G.; Fink, D.; Hua, Q.; Jacobsen, G.; Tuniz, C.; Williams, A.

    2004-01-01

    After a brief review of the basics of 14 C bomb-pulse dating, this paper presents two unique forensic applications. Particular attention is dedicated to the use of the 14 C bomb-pulse to establish the time of harvest of illicit drugs such as heroin and opium. Preliminary measurements of 14 C concentrations in milligram samples taken from seized drugs are presented. 14 C bomb-pulse dating can determine whether drug distribution originates from stockpiles or recent manufacture, and support the action of law enforcement authorities against criminal organisations involved in drug trafficking. In addition, we describe the dating of wine vintages for a number of authenticated single label vintage red wines from the Barossa Valley - South Australia. Our results show that radiocarbon dating can be used to accurately determine wine vintages and therefore reveal the addition of unrelated materials of natural and synthetic origin

  16. Forensic applications of 14C bomb-pulse dating

    Science.gov (United States)

    Zoppi, U.; Skopec, Z.; Skopec, J.; Jones, G.; Fink, D.; Hua, Q.; Jacobsen, G.; Tuniz, C.; Williams, A.

    2004-08-01

    After a brief review of the basics of 14C bomb-pulse dating, this paper presents two unique forensic applications. Particular attention is dedicated to the use of the 14C bomb-pulse to establish the time of harvest of illicit drugs such as heroin and opium. Preliminary measurements of 14C concentrations in milligram samples taken from seized drugs are presented. 14C bomb-pulse dating can determine whether drug distribution originates from stockpiles or recent manufacture, and support the action of law enforcement authorities against criminal organisations involved in drug trafficking. In addition, we describe the dating of wine vintages for a number of authenticated single label vintage red wines from the Barossa Valley - South Australia. Our results show that radiocarbon dating can be used to accurately determine wine vintages and therefore reveal the addition of unrelated materials of natural and synthetic origin.

  17. A high resolution method for {sup 14}C analysis of a coral from South China Sea: Implication for “AD 775” {sup 14}C event

    Energy Technology Data Exchange (ETDEWEB)

    Ding, Ping [State Key Laboratory of Isotope Geochemistry, Guangzhou Institute of Geochemistry, Chinese Academy of Sciences, 510640 Guangzhou (China); Shen, Chengde, E-mail: cdshen@gig.ac.cn [State Key Laboratory of Isotope Geochemistry, Guangzhou Institute of Geochemistry, Chinese Academy of Sciences, 510640 Guangzhou (China); State Key Laboratory of Nuclear Physics and Technology, Peking University, 100871 Beijing (China); Yi, Weixi; Wang, Ning [State Key Laboratory of Isotope Geochemistry, Guangzhou Institute of Geochemistry, Chinese Academy of Sciences, 510640 Guangzhou (China); Ding, Xingfang; Liu, Kexin; Fu, Dongpo [State Key Laboratory of Nuclear Physics and Technology, Peking University, 100871 Beijing (China); Liu, Weiguo [State Key Laboratory of Loess and Quaternary Geology, Institute of Earth Environment, The Chinese Academy of Sciences, 710075 Xi’an (China); Liu, Yi [CAS Key Laboratory of Crust-Mantle Materials and Environments, School of Earth and Space Sciences, University of Science and Technology of China, 230026 Hefei (China)

    2015-10-15

    A pre-heating method that improves the background and precision of {sup 14}C dating significantly was applied for fossil coral dating with high resolution in our lab in Guangzhou Institute of Geochemistry, Chinese Academy of Sciences (GIGCAS). The reaction tube is heated under 300 °C in a vacuum line before it is used for graphitization. The method can reduce the contamination absorbed in TiH{sub 2}, Zn and Fe power placed in the graphitization tube. With the pre-heating and average drilling method, bi-weekly resolution {sup 14}C dating in a fossil coral is carried out to investigate the “AD 775 {sup 14}C spike event”. Different from the tree ring {sup 14}C archives with the {sup 14}C spike of ∼15‰ (Δ{sup 14}C), the {sup 14}C spike in the coral shows an abrupt peak of 45‰ and two smaller spikes of Δ{sup 14}C > 20‰ in half a year in AD 776. And then, the {sup 14}C content in coral decreases gradually in AD 777. The peak time of the {sup 14}C spike event likely occurs in the summer of AD 776 according to the δ{sup 18}O variation in coral. High-resolution dating of {sup 14}C in coral provides not only a more detail process of the event than that from tree rings, but also the first report of the event from sea ecosystem. Both of them suggest an extraterrestrial origin of the event cause.

  18. Placental transfer of 14C-hexoprenaline

    International Nuclear Information System (INIS)

    Lipshitz, J.; Broyles, K.; Whybrew, W.D.; Ahokas, R.A.; Anderson, G.D.

    1982-01-01

    The placental transfer of a single intravenous injection of 14 C-hexoprenaline was studied in eight pregnant New Zealand white rabbits. Maternal and fetal blood was sampled intermittently for 60 minutes after the injection. An initial rapid decrease in the levels of 14 C-hexoprenaline in maternal blood was followed by a second slower phase, whereas fetal heart rate after the administration of a single maternal intravenous injection of hexoprenaline in the treatment of fetal distress is due to the action on the uterus and/or on maternal cardiovascular function, and not to direct stimulation of the fetus

  19. {sup 14}C-Methylenebisphenylisocyanate ({sup 14}C-MDI). Study of absorption after single dermal and intradermal administration in rats

    Energy Technology Data Exchange (ETDEWEB)

    Leibold, E.; Hoffmann, H.D.; Hildebrand, B

    1999-07-01

    The absorption, distribution and excretion of radioactivity was studied in groups of four male Wistar rats following a single dermal and intradermal administration of {sup 14}C- Methylenebisphenylisocyanate ({sup 14}C-MDI) at nominal dose levels of 4.0 and 0.4 mg/cm{sup 2} for dermal administration and 0.4 mg/animal for intradermal administration. These dose levels nominally corresponded to 40 and 4.0 mg/animal for dermal administration. Considering the animal weights, dose levels corresponded to about 140 and 14 mg/kg body weight (dermal administration) and 1.4 mg/kg body weight (intradermal administration). In the experiments with dermal administration, animals were exposed for 8 hours and sacrificed 8, 24 or 120 h after beginning of exposure. In the experiment with intradermal administration, animals were sacrificed 120 h after treatment. After dermal administration of {sup 14}C-MDI, mean recoveries of radioactivity from all dose groups were in the range from 97.86 to 108.07% of the total radioactivity administered. Generally, the largest proportion of radioactivity was found at the application site and dressing. The total amount of radioactivity absorbed (including excreta, cage wash, tissues/organs and carcass) increased with increasing sacrifice time. Dermal absorption was very low and quantitatively similar at both dose levels; maximally ca. 0.9 % of the applied radioactivity was absorbed. After intradermal administration of {sup 14}C-MDI, the mean recovery of radioactivity was 100.90 % of the radioactivity administered. The largest proportion of radioactivity was found at the application site. The total amount of radioactivity absorbed (including excreta, cage wash, tissues/organs and carcass) amounted to about 26 % of the radioactivity applied. Irrespective of the mode of administration of 1{sup 4C}-MDI, concentrations of radioactivity in tissues and organs generally were below 1 {mu}g Eq/g at 120 h after administration. In summary, the results of this

  20. DNA methylation-dependent regulation of TrkA, TrkB, and TrkC genes in human hepatocellular carcinoma

    Energy Technology Data Exchange (ETDEWEB)

    Jin, Wook [Laboratory of Molecular Disease and Cell Regulation, Lee Gil Ya Cancer and Diabetes Institute, Gachon University of Medicine and Science, Incheon (Korea, Republic of); Lee, Jong-Joo [Department of Environmental Medical Biology, Institute of Tropical Medicine, Brain Korea 21 Project for Medical Science, Yonsei University College of Medicine, 250 Seongsanno, Seodaemun-gu, Seoul 120-752 (Korea, Republic of); Kim, Min Soo [Laboratory of Molecular Disease and Cell Regulation, Lee Gil Ya Cancer and Diabetes Institute, Gachon University of Medicine and Science, Incheon (Korea, Republic of); Son, Byung Ho [Department of Surgery, Kangbuk Samsung Hospital, Sungkyunkwan University, School of Medicine, 108 Pyung-dong, Jongro-gu, Seoul 110-746 (Korea, Republic of); Cho, Yong Kyun, E-mail: choyk2004@hanmail.net [Division of Gastroenterology, Department of Internal Medicine, Kangbuk Samsung Hospital, Sungkyunkwan University, School of Medicine, 108 Pyung-dong, Jongro-gu, Seoul 110-746 (Korea, Republic of); Kim, Hyoung-Pyo, E-mail: kimhp@yuhs.ac [Department of Environmental Medical Biology, Institute of Tropical Medicine, Brain Korea 21 Project for Medical Science, Yonsei University College of Medicine, 250 Seongsanno, Seodaemun-gu, Seoul 120-752 (Korea, Republic of)

    2011-03-04

    Research highlights: {yields} Expression of TrkA, TrkB, and TrkC is significantly elevated in human hepatocellular carcinoma. {yields} Downregulation of Trks is correlated with their promoter hypermethylation. {yields} Inhibiting DNA methylation restored expression of Trks in normal liver cell lines. {yields} Trks promote the proliferation of hepatocellular carcinoma. {yields} Trks induce expression of the metastatic regulator, Twist. -- Abstract: The tropomyosin-related kinase (Trk) family of neurotrophin receptors, TrkA, TrkB and TrkC, has been implicated in the growth and survival of human cancers. Here we report that Trks are frequently overexpressed in hepatocellular carcinoma (HCC) from patients and human liver cancer cell lines. To unravel the underlying molecular mechanism(s) for this phenomenon, DNA methylation patterns of CpG islands in TrkA, TrkB, and TrkC genes were examined in normal and cancer cell lines derived from liver. A good correlation was observed between promoter hypermethylation and lower expression of TrkA, TrkB, and TrkC genes, which was supported by the data that inhibiting DNA methylation with 5-azacytidine restored expression of those genes in normal liver cell lines. Furthermore, Trks promoted the proliferation of HepG2 and induced expression of the metastatic regulator, Twist. These results suggest that Trks may contribute to growth and metastasis of liver cancer.

  1. DNA methylation-dependent regulation of TrkA, TrkB, and TrkC genes in human hepatocellular carcinoma

    International Nuclear Information System (INIS)

    Jin, Wook; Lee, Jong-Joo; Kim, Min Soo; Son, Byung Ho; Cho, Yong Kyun; Kim, Hyoung-Pyo

    2011-01-01

    Research highlights: → Expression of TrkA, TrkB, and TrkC is significantly elevated in human hepatocellular carcinoma. → Downregulation of Trks is correlated with their promoter hypermethylation. → Inhibiting DNA methylation restored expression of Trks in normal liver cell lines. → Trks promote the proliferation of hepatocellular carcinoma. → Trks induce expression of the metastatic regulator, Twist. -- Abstract: The tropomyosin-related kinase (Trk) family of neurotrophin receptors, TrkA, TrkB and TrkC, has been implicated in the growth and survival of human cancers. Here we report that Trks are frequently overexpressed in hepatocellular carcinoma (HCC) from patients and human liver cancer cell lines. To unravel the underlying molecular mechanism(s) for this phenomenon, DNA methylation patterns of CpG islands in TrkA, TrkB, and TrkC genes were examined in normal and cancer cell lines derived from liver. A good correlation was observed between promoter hypermethylation and lower expression of TrkA, TrkB, and TrkC genes, which was supported by the data that inhibiting DNA methylation with 5-azacytidine restored expression of those genes in normal liver cell lines. Furthermore, Trks promoted the proliferation of HepG2 and induced expression of the metastatic regulator, Twist. These results suggest that Trks may contribute to growth and metastasis of liver cancer.

  2. Preparation of pyridostigmine bromide labeled with carbon-14 and tritium

    Energy Technology Data Exchange (ETDEWEB)

    Kepler, J.A.; Twine, C.E.; Austin, R.D. (Research Triangle Inst., Research Triangle Park, NC (United States))

    1992-08-01

    [2-[sup 14]C]Pyridostigmine bromide was prepared in 17.6% radiochemical yield with specific activity of 18 mCi/mmol. The reaction sequence involved preparation of 2-furan[[sup 14]C]carboxylic acid by carbonation of 2-lithiofuran, followed by conversion to 2-amino[[sup 14]C]methylfuran by lithium aluminium hydride reduction of its carboxamide. Oxidative rearrangement of 2-amino[[sup 14]C]methylfuran gave 3-hydroxy[2-[sup 14]C]pyridine which was converted to [2-[sup 14]C]pyridostigmine bromide by reaction with dimethylcarbamyl chloride and quarternization with bromomethane. Pyridostigmine bromide labeled in the methyl group of the carbamate function was prepared in 73% yield with specific activity of 37.6 mCi/mmol by reaction of bis-3-pyridyl carbonate with [[sup 14]C]dimethylamine followed by quarternization with bromomethane. [6-[sup 3]H]-Pyridostigmine bromide with specific activity of 22.5 mCi/mmol was prepared by catalytic halogen-tritium replacement of 2,6-dibromo-3-dimethylcarbamyloxypyridine followed by quarternization with bromomethane and back-exchanging the labile 2-tritium. (author).

  3. Preparation of pyridostigmine bromide labeled with carbon-14 and tritium

    International Nuclear Information System (INIS)

    Kepler, J.A.; Twine, C.E.; Austin, R.D.

    1992-01-01

    [2- 14 C]Pyridostigmine bromide was prepared in 17.6% radiochemical yield with specific activity of 18 mCi/mmol. The reaction sequence involved preparation of 2-furan[ 14 C]carboxylic acid by carbonation of 2-lithiofuran, followed by conversion to 2-amino[ 14 C]methylfuran by lithium aluminium hydride reduction of its carboxamide. Oxidative rearrangement of 2-amino[ 14 C]methylfuran gave 3-hydroxy[2- 14 C]pyridine which was converted to [2- 14 C]pyridostigmine bromide by reaction with dimethylcarbamyl chloride and quarternization with bromomethane. Pyridostigmine bromide labeled in the methyl group of the carbamate function was prepared in 73% yield with specific activity of 37.6 mCi/mmol by reaction of bis-3-pyridyl carbonate with [ 14 C]dimethylamine followed by quarternization with bromomethane. [6- 3 H]-Pyridostigmine bromide with specific activity of 22.5 mCi/mmol was prepared by catalytic halogen-tritium replacement of 2,6-dibromo-3-dimethylcarbamyloxypyridine followed by quarternization with bromomethane and back-exchanging the labile 2-tritium. (author)

  4. Synthesis of two 14C-labeled catechol-o-methyltransferase inhibitors

    International Nuclear Information System (INIS)

    Karlsson, Carita; Honkanen, Erkki

    1991-01-01

    14 C-labelled 3-(3,4-dihydroxy-5-nitrophenylmethylidene)-2,4-pentanedione and 14 C-labelled E-N,N-diethyl-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)acrylamide have been synthesized from [carbonyl- 14 C]vanillin. (author)

  5. Synthesis of organic substances labelled with 14C and 35S

    International Nuclear Information System (INIS)

    Pichat, L.

    1958-01-01

    After a brief history of the development of the Section des Molecules marquees of the French Atomic Energy Commission, the author gives an outline of the synthesis of the following labelled compounds: benzene 14 C-6; phenyl-p-fluorophenyl, thienyl-2 β alanines β 14 C; noradrenaline β 14 C (arterenol β 14 C), dotriacontane 14 C-16-17, aminoethane sulfinic acid (hypotaurine 35 S). (author) [fr

  6. Structural Insights into the Methylation of C1402 in 16S rRNA by Methyltransferase RsmI.

    Directory of Open Access Journals (Sweden)

    Mohan Zhao

    Full Text Available RsmI and RsmH are conserved S-Adenosylmethionine (AdoMet-dependent methyltransferases (MTases that are responsible for the 2'-O-methylation and N4-methylation of C1402 in bacterial 16S rRNA, respectively. Methylation of m4Cm1402 plays a role in fine-tuning the shape and functions of the P-site to increase the decoding fidelity, and was recently found to contribute to the virulence of Staphylococcus aureus in host animals. Here we report the 2.20-Å crystal structure of homodimeric RsmI from Escherichia coli in complex with the cofactor AdoMet. RsmI consists of an N-terminal putative RNA-binding domain (NTD and a C-terminal catalytic domain (CTD with a Rossmann-like fold, and belongs to the class III MTase family. AdoMet is specifically bound into a negatively charged deep pocket formed by both domains by making extensive contacts. Structure-based mutagenesis and isothermal titration calorimetry (ITC assays revealed Asp100 and Ala124 are vital for AdoMet-binding. Although the overall fold of RsmI shows remarkable similarities to the characterized MTases involved in vitamin B12 biosynthesis, it exhibits a distinct charge distribution especially around the AdoMet-binding pocket because of different substrate specificity. The docking model of RsmI-AdoMet-RNA ternary complex suggested a possible base-flipping mechanism of the substrate RNA that has been observed in several known RNA MTases. Our structural and biochemical studies provide novel insights into the catalytic mechanism of C1402 methylation in 16S rRNA.

  7. [14C]Fluciclovine (alias anti-[14C]FACBC) uptake and ASCT2 expression in castration-resistant prostate cancer cells

    International Nuclear Information System (INIS)

    Ono, Masahiro; Oka, Shuntaro; Okudaira, Hiroyuki; Nakanishi, Takeo; Mizokami, Atsushi; Kobayashi, Masato; Schuster, David M.; Goodman, Mark M.; Shirakami, Yoshifumi; Kawai, Keiichi

    2015-01-01

    Introduction: trans-1-Amino-3-[ 18 F]fluorocyclobutanecarboxylic acid ([ 18 F]fluciclovine, also known as anti-[ 18 F]FACBC), is a tracer for positron emission tomography (PET) imaging for detection of tumors such as prostate cancer (PCa). Our previous study showed that ASCT2 (Na + -dependent amino acid transporter (AAT)) mediates fluciclovine uptake in androgen-dependent PCa cells; its expression is influenced by androgen, a key hormone in the progression of primary PCa and castration-resistant prostate cancer (CRPC). In this study, we investigated the uptake mechanisms and feasibility of [ 18 F]fluciclovine for CRPC in the androgen-dependent PCa cell line LNCaP and LNCaP-derivatives LNCaP-SF and LN-REC4. Methods: LNCaP-SF was established after long-term cultivation of LNCaP in steroid-free conditions, and LN-Pre and LN-REC4 were established from LNCaP inoculated in intact and castrated severe combined immunodeficient mice, respectively. Uptake and competitive inhibition experiments were performed with trans-1-amino-3-fluoro[1- 14 C]cyclobutanecarboxylic acid ([ 14 C]fluciclovine) to characterize the involvement of AATs in androgen-dependent PCa (LNCaP and LN-Pre) and CRPC-like (LNCaP-SF and LN-REC4) cell lines. AAT expression was analyzed by Western blotting, and [ 14 C]fluciclovine uptake in androgen-dependent PCa and CRPC-like cell lines were investigated in the presence or absence of dihydrotestosterone (DHT). Results: The contribution of Na + -dependent AATs to [ 14 C]fluciclovine uptake in all cell lines was 88−98%, and [ 14 C]fluciclovine uptake was strongly inhibited by L-glutamine and L-serine, the substrates for Na + -dependent alanine-serine-cysteine (system ASC) AATs, in the presence of Na + . DHT enhanced ASCT2 expression in LNCaP, LN-Pre, and LN-REC4, but not in LNCaP-SF, and the responses of ASCT2 expression to DHT correlated with [ 14 C]fluciclovine uptake. Conclusions: System ASC, especially ASCT2, could play a major role in [ 14 C

  8. Role for DNA methylation in the regulation of miR-200c and miR-141 expression in normal and cancer cells

    Energy Technology Data Exchange (ETDEWEB)

    Vrba, Lukas; Jensen, Taylor J.; Garbe, James C.; Heimark, Ronald L.; Cress, Anne E.; Dickinson, Sally; Stampfer, Martha R.; Futscher, Bernard W.

    2009-12-23

    BACKGROUND: The microRNA-200 family participates in the maintenance of an epithelial phenotype and loss of its expression can result in epithelial to mesenchymal transition (EMT). Furthermore, the loss of expression of miR-200 family members is linked to an aggressive cancer phenotype. Regulation of the miR-200 family expression in normal and cancer cells is not fully understood. METHODOLOGY/ PRINCIPAL FINDINGS: Epigenetic mechanisms participate in the control of miR-200c and miR-141 expression in both normal and cancer cells. A CpG island near the predicted mir-200c/mir-141 transcription start site shows a striking correlation between miR-200c and miR-141 expression and DNA methylation in both normal and cancer cells, as determined by MassARRAY technology. The CpG island is unmethylated in human miR-200/miR-141 expressing epithelial cells and in miR-200c/miR-141 positive tumor cells. The CpG island is heavily methylated in human miR-200c/miR-141 negative fibroblasts and miR-200c/miR-141 negative tumor cells. Mouse cells show a similar inverse correlation between DNA methylation and miR-200c expression. Enrichment of permissive histone modifications, H3 acetylation and H3K4 trimethylation, is seen in normal miR-200c/miR-141-positive epithelial cells, as determined by chromatin immunoprecipitation coupled to real-time PCR. In contrast, repressive H3K9 dimethylation marks are present in normal miR-200c/miR-141-negative fibroblasts and miR-200c/miR-141 negative cancer cells and the permissive histone modifications are absent. The epigenetic modifier drug, 5-aza-2'-deoxycytidine, reactivates miR-200c/miR-141 expression showing that epigenetic mechanisms play a functional role in their transcriptional control. CONCLUSIONS/ SIGNIFICANCE: We report that DNA methylation plays a role in the normal cell type-specific expression of miR-200c and miR-141 and this role appears evolutionarily conserved, since similar results were obtained in mouse. Aberrant DNA methylation

  9. 14C tebuconazole degradation in Colombian soils.

    Science.gov (United States)

    Mosquera, C S; Martínez, M J; Guerrero, J A

    2010-01-01

    Tebuconazole is a fungicide used on onion crops (Allium Fistulosum L) in Colombia. Persistence of pesticides in soils is characterized by the half-life (DT50), which is influenced by their chemical structure, the physical and chemical properties of the soil and the previous soil history. Based on its structural and chemical properties, tebuconazole should be expected to be relatively persistent in soils. Laboratory incubation studies were conducted to evaluate persistence and bond residues of 14C tebuconazole in three soils, two inceptisol (I) and one histosol (H). Textural classifications were: loam (101), loamy sand (102) and loam (H03), respectively. Data obtained followed a first-order degradation kinetics (R2 > or = 0.899) with DT50 values between 158 and 198 days. The production of 14CO2 from the 14C-ring-labelled test chemicals was very low and increased slightly during 63 days in all cases. The methanol extractable 14C-residues were higher than aqueous ones and both decreased over incubation time for the three soils. The formation of bound 14C-residues increased with time and final values were 11.3; 5.55 and 7.87% for 101, 102 and H03 respectively. Soil 101 showed the lowest mineralization rate and the highest bound residues formation, which might be explained by the clay fraction content. In contrast, an inverse behavior was found for soils 102 and H03, these results might be explained by the higher soil organic carbon content.

  10. Dose Consumptions of NSC KIPT Personnel during the Work that Includes Uranium

    International Nuclear Information System (INIS)

    Kurilo, Yu.P.; Mazilov, A.V.; Razsukovanny, B.N.

    2007-01-01

    The analysis of mean annual and maximal annual uranium concentrations in the air of NSC KIPT working premises is carried out in this paper; the high limit of possible external radiation of category A personnel engaged on works with uranium since 1961 to 2003 has been calculated. The numerical values of effective doses of internal and external radiation of personnel are determined on the basis of data acquired. It is shown that despite of breaking the principal of non excess that has taken place to be in the some years the mean value of total (external+internal) radiation during the given period of time did not exceed the effective dose limit established in Norms of radiating safety of Ukraine and that is equal to 20 mSv per year

  11. The methylation of the C-terminal region of hnRNPQ (NSAP1) is important for its nuclear localization

    International Nuclear Information System (INIS)

    Passos, Dario O.; Quaresma, Alexandre J.C.; Kobarg, Joerg

    2006-01-01

    Protein arginine methylation is an irreversible post-translational protein modification catalyzed by a family of at least nine different enzymes entitled PRMTs (protein arginine methyl transferases). Although PRMT1 is responsible for 85% of the protein methylation in human cells, its substrate spectrum has not yet been fully characterized nor are the functional consequences of methylation for the protein substrates well understood. Therefore, we set out to employ the yeast two-hybrid system in order to identify new substrate proteins for human PRMT1. We were able to identify nine different PRMT1 interacting proteins involved in different aspects of RNA metabolism, five of which had been previously described either as substrates for PRMT1 or as functionally associated with PRMT1. Among the four new identified possible protein substrates was hnRNPQ3 (NSAP1), a protein whose function has been implicated in diverse steps of mRNA maturation, including splicing, editing, and degradation. By in vitro methylation assays we were able to show that hnRNPQ3 is a substrate for PRMT1 and that its C-terminal RGG box domain is the sole target for methylation. By further studies with the inhibitor of methylation Adox we provide evidence that hnRNPQ1-3 are methylated in vivo. Finally, we demonstrate by immunofluorescence analysis of HeLa cells that the methylation of hnRNPQ is important for its nuclear localization, since Adox treatment causes its re-distribution from the nucleus to the cytoplasm

  12. Effect of endomycorrhizae on the bioavailability of bound 14C residues to onion plants from an organic soil treated with [14C]fonofos

    International Nuclear Information System (INIS)

    Nelson, S.D.; Khan, S.U.

    1990-01-01

    Uptake of bound 14 C residues from an organic soil treated with radiolabeled fonofos (O-ethyl S-phenyl ethylphosphonodithioate) by selected Glomus endomycorrhiza and onion roots was studied. The hyphae of endomycorrhizal associations were capable of removing 14 C residues from the soil and transporting them to onion plants. Bioavailability of soil-bound 14 C residues, as measured by 14 C residue content in onion, was increased 32 and 40% over that of nonmycorrhizal plants by hyphae of Glomus intraradices and Glomus vesiculiferium, respectively. The data suggest that under field conditions endomycorrhizal infection may greatly increase the bioavailability of soil-bound pesticide residues to plants

  13. Analysis of {sup 14}CO{sub 2} trapped {sup 14}C Sorbent, and {sup 14}C and {sup 3}H Radioactivity Determination in Resins and Oils from Nuclear Power Plants Using a Combustion Method

    Energy Technology Data Exchange (ETDEWEB)

    Ko, Young Gun; Kim, Chang Jong; Choi, Geun Sik; Chung, Kun Ho; Kang, Mun Ja [KAERI, Daejeon (Korea, Republic of)

    2016-05-15

    Tritium ({sup 3}H, T) generated in the heavy water and C fourteen ({sup 14}C) originated from the graphite moderator or structural materials of the nuclear power plant can cause acute and/or chronic harmful effects by inhalation and ingestion of these radionuclides owing to their binding affinity toward biomolecules and gas phase. {sup 3}H and {sup 14}C radioactivity in ion exchange resins and oils from nuclear power plants were determined by an oxidation (combustion) method. The 0.1 M HNO{sub 3} solution and the {sup 14}C sorbent trapped the {sub 3}H and {sup 14}C respectively in the gas from the combustion of samples. All samples were burned without ash in the combustion system. The reaction of CO{sub 2} and {sup 14}C sorbent was investigated by FT-IR analysis. The study demonstrated the different reaction mechanism according to the CO{sub 2} concentration. In the FT-IR study, it is clearly confirmed that CO{sub 2} from the burned 1 g of sample can be trapped in the {sup 14}C sorbent completely. During the reaction of CO{sub 2} and {sup 14}C sorbent, the temperature and the viscosity of {sup 14}C sorbent increased due to the decrease of enthalpy change and the bonding between each molecules of the sorbent. We expect that our FT-IR study could motivate the development of {sup 14}C sorbent and confirm the {sup 14}C trapping performance of the {sup 14}C sorbent.

  14. Prenatal exposure to maternal depressed mood and the MTHFR C677T variant affect SLC6A4 methylation in infants at birth.

    Directory of Open Access Journals (Sweden)

    Angela M Devlin

    2010-08-01

    Full Text Available Prenatal and early postnatal exposure to maternal depression may "program" childhood behavior via epigenetic processes such as DNA methylation. Methylenetetrahydro-folate reductase (MTHFR is an important enzyme in the generation of methyl groups for DNA methylation. The common MTHFR C677T variant is associated with depression in men and non-pregnant women, and with global changes in DNA methylation. This study investigated the effect of maternal MTHFR C677T genotype on antenatal maternal mood, and their impact on the gene-specific methylation in pregnant women and their newborn infants. The methylation status of SLC6A4, which encodes the transmembrane serotonin transporter, and BDNF, which encodes brain derived neurotrophic factor, were assessed because of their potential role in behaviour.Depressed mood was assessed by the Edinburgh Postnatal Depression Scale (EPDS and the Hamilton Rating Scale for Depression (HAM-D in women (n = 82, all taking folate during the 2(nd and 3(rd trimesters of pregnancy. The methylation status of SLC6A4 and BDNF were assessed in 3rd trimester maternal peripheral leukocytes and in umbilical cord leukocytes collected from their infants at birth. Women with the MTHFR 677TT genotype had greater 2(nd trimester depressed mood (p<0.05. Increased 2(nd trimester maternal depressed mood (EPDS scores was associated with decreased maternal and infant SLC6A4 promoter methylation (p<0.05, but had no effect on BDNF promoter methylation.These findings show that the MTHFR C677T variant is associated with greater depressed mood during pregnancy. We further showed that prenatal exposure to maternal depressed mood affects gene-specific DNA methylation patterns. These findings support the concept that alterations in epigenetic processes may contribute to developmental programming of behaviour by maternal depression.

  15. Metabolism of 14C-L-arginine and 14C-L-proline in excised burst buds and stem sections of citrus trees (Citrus unshiu Marc.)

    International Nuclear Information System (INIS)

    Kato, Tadashi; Yamagata, Makoto; Tsukahara, Sadao

    1985-01-01

    Arginine and proline, which are the major forms of soluble reserve N, were fed singly in uniformly labelled 14 C-form to excised 2-year-old stem sections with a new shoot, to wood sections, and to burst buds from a 21-year-old satsuma mandarin tree. Metabolism was studied by radioassay and autoradiography. In stem sections with a new shoot, both 14 C-compounds were metabolized to acidic and neutral components, insoluble components, and 14 CO 2 . This conversion occurred to a greater extent in sections fed with arginine than with proline. When 14 C-arginine was fed, the highest 14 C-activity in the cationic fraction of stem sections, bark, wood and new shoots was found in γ-guanidinobutyric acid, followed by γ-aminobutyric acid and proline; low levels of 14 C was also found in ornithine and trace amounts in citrulline. These findings demonstrate that arginine is metabolized by at least two routes: via ornithine and via γ-guanidinobutyric acid. In every organ, the major metabolic products of 14 C-proline were pyrrolidone-5-carboxlic acid, glutamic acid, aspartic acid, asparagine, an unidentified compound (U 5 in Fig. 4), γ-aminobutyric acid and arginine. The basic metabolic pathways in the conversion of Both 14 C-compounds were the same in burst buds, new shoot, bark and wood, although there was a slight difference autoradiographically. (author)

  16. The use of 14C ethanolamine as a precursor

    International Nuclear Information System (INIS)

    Madelmont, J.C.; Parry, D.; Godeneche, D.; Duprat, J.

    1985-01-01

    Two new 2 chloroethyl nitrosoureas were labelled on two positions by 14 C starting from Na 14 CN and using 14 C ethanolamine as intermediate, i.e. on the carbon 2 of the 2 chloro ethyl group and on the carbon 2 of the cysteamine part. (author)

  17. Crystal and molecular structure studies of (Z)-N-methyl-C-4-substituted phenyl nitrones by XRD, DFT, FTIR and NMR methods

    Science.gov (United States)

    Lasri, Jamal; Eltayeb, Naser Eltaher; Haukka, Matti; Alghamdi, Yousef

    2017-01-01

    (Z)-N-methyl-C-4-substituted phenyl nitrones -O+N(Me)=C(H)R (Z-2a R = 4-ClC6H4, Z-2b R = 4-NO2C6H4, Z-2c R = 4-CH3OC6H4) were synthesized and characterized by elemental analyses, FTIR, 1H, 13C and DEPT-135 NMR spectroscopy and also by single crystal X-ray diffraction (in the case of Z-2a and Z-2b). The geometries of the nitrone molecules Z-2a, Z-2b and Z-2c and their E-isomers; (E)-N-methyl-C-4-chlorophenyl nitrone E-2a, (E)-N-methyl-C-4-nitrophenyl nitrone E-2b and (E)-N-methyl-C-4-methoxyphenyl nitrone E-2c were optimized using density functional theory (DFT) at the B3LYP/6-311++G(d,p) level of theory. The theoretical vibrational frequencies obtained by DFT calculations are in good agreement with the experimental values. The electronics structures were described in terms of the distribution of the highest occupied molecular orbital (HOMO) and the lowest unoccupied molecular orbital (LUMO). Gauge independent atomic orbital (GIAO) method was used to calculate the NMR spectra, the correlation between the calculated and experimental chemical shifts is mostly in the range of 0.94-0.97 for 1H, whereas, the correlation for 13C is 0.99. Thermodynamics study showed that the Z-isomer is favoured than E-isomer with energy barrier of 7.1, 7.2 and 7.1 kcal/mol for Z-2a, Z-2b and Z-2c, respectively. The abundance of the most stable species Z-isomers is equal to 99.99% for all three compounds at 298 K in gas phase.

  18. Incorporation of U-/sup 14/C-glucose into the lipids U-/sup 14/C and sugars of Culex pipiens fatigans

    Energy Technology Data Exchange (ETDEWEB)

    Duggal, Rita Nanda; Subrahmanyam, D

    1983-11-01

    The role of U-/sup 14/C-glucose as a lipogenic precursor was examined in larvae and adults of C. pipiens fatigans. The pattern of incorporation of the radiocarbon was also examined in the sugars of these insects. It was found that on feeding of larvae and adults with /sup 14/C-glucose, the phospholipid fraction of the insects was associated with more than 70 per cent of the total lipid radiolabel. However, the percentage distribution of the phospholipid label in the different phospholipid fractions of the larvae and adults was different. Among the neutral lipids, a low but significant label in cholesterol was of considerable interest. The /sup 14/C-glucose was also converted to trehalose in both larvae and adults. However, the two stages differed in the utilization of glucose and trehalose. 5 figures, 16 refs.

  19. Monitoring of the 14C activity in the atmosphere

    International Nuclear Information System (INIS)

    Svingor, E.; Molnar, M.; Futo, I.; Rinyu, L.

    2006-01-01

    Complete text of publication follows. The distribution of atmospheric radiocarbon has been extensively investigated both in the Northern and Southern Hemisphere as well as in the Tropics for a number of decades. Systematic global observations of 14 CO 2 in the troposphere were made during and after atmospheric nuclear weapon tests in the 1950s and 1960s by several laboratories. Nowadays the monitoring of 14 C in regions adjacent to nuclear power plants (NPP) or sites of land-filled radioactive wastes has growing importance in determining the frequency and activity of anthropogenic 14 C released to the environment. On the other hand, the depletion of 14 C in the atmosphere gives information about the regional fossil fuel CO 2 contributions (Figure 1., Prague-Bulovka). The 14 C activity of the atmosphere has been monitored in the vicinity of Paks NPP by sampling environmental air monthly since 1994. Four differential sampling units collect air samples less than 2 km away from the 100- m-high stacks of Paks NPP (A-type stations), and for reference a sampler is operated at a station (B24) ca. 30 km away from Paks NPP. The highest 14 C values were measured at the site located less than 1km away from Paks NPP. The influence of the 14 C discharge in the environment decreases rapidly with the distance from the source and under normal operating conditions the effect of Paks NPP is negligible at a distance of 2.5km. In Figure 1. we have compared our data for Paks NPP measured during the time span of 2000 - 2005 with data from different European monitoring stations. (The 14 C activities are given in Δ values: Δ 14 C(% (A sample /A standard -1) x 1000.) In 2000-2001 the excess 14 C at Paks NPP compared to the B24 was 5-10 (per mille) but its Δ value didn't exceed the tropospheric background (1). With the growing traffic the inactive CO 2 emission (Suess effect) exceeded the influence of the NPP (2). After a cleaning tank incident at unit 2 of Paks NPP in April 2003 a 5

  20. Anthropogenic 14C in the natural (aquatic) environment

    International Nuclear Information System (INIS)

    Begg, F.H.

    1992-11-01

    Increasing global awareness of the radiological significance of 14 C releases from the nuclear and radiochemical industries has resulted in a number of studies within the last decade investigating the atmospheric releases and their effect on the terrestrial biosphere. The basis of this study was to determine the behaviour and environmental distribution of anthropogenically produced 14 C released to the aquatic environment from the nuclear fuel reprocessing plant at Sellafield. Most sampling was undertaken in the Irish Sea with smaller scale studies being carried out in the Bristol Channel and the Grand Union Canal. Within the study area, from Earnse Point 40 km south of Sellafield, northwards to the Clyde Sea area, preliminary studies on intertidal biota samples ie. mussels, winkles and seaweed indicated enriched 14 C specific activities in all the samples relative to the current ambient level of 115.4 pM. The highest activities were observed in the immediate vicinity of the discharge location; mussels with a measured activity of 787 pM, winkles of 613 pM and seaweed of 415 pM. The 14 C specific activity observed at most sites appeared to be organism dependent with mussels>winkles>seaweed. This is the result of differences in the uptake mechanisms of the organisms and indicates that the dissolved inorganic carbon and the particulate material within the water column are enriched in 14 C . However, on analysis of the biogeochemical fractions of the water column, enriched 14 C activities were observed only in the DIC fraction which could explain those activities found in the seaweed but not those in the mussels and winkles. Enriched 14 C activities were found in the phytoplankton, indicating that there is a source of enriched organic particulate material within the water column as a result of photosynthetic uptake of enriched DIC, however this will be a seasonal effect. Nevertheless, this enrichment is still not high enough to support the activities observed in the

  1. Preparation of 14-C-labelled 1,4-Dideoxy-1,4-imino-D-arabinitol: Cyanosilylation of Cyclic Imines using KCN in a One-Pot Synthesis

    DEFF Research Database (Denmark)

    Lundt, Inge; Malle, Birgitte Mølholm; Foged, Christian

    1999-01-01

    A new method for C-C bond formation was developed based on in situ cyanosilylation of cyclic Schiff bases using KCN, TMSCl, KI and ZnI2. This method was used to prepare the potent -glucosidase inhibitor 1,4-dideoxy-1,4-imino-D-arabinitol 14-C labelled at C-5.Keywords: in situ cyanosilylation; 14-C...

  2. Wetting, Solubility and Chemical Characteristics of Plasma-Polymerized 1-Isopropyl-4-Methyl-1,4-Cyclohexadiene Thin Films

    Directory of Open Access Journals (Sweden)

    Jakaria Ahmad

    2014-07-01

    Full Text Available Investigations on the wetting, solubility and chemical composition of plasma polymer thin films provide an insight into the feasibility of implementing these polymeric materials in organic electronics, particularly where wet solution processing is involved. In this study, thin films were prepared from 1-isopropyl-4-methyl-1,4-cyclohexadiene (γ-Terpinene using radio frequency (RF plasma polymerization. FTIR showed the polymers to be structurally dissimilar to the original monomer and highly cross-linked, where the loss of original functional groups and the degree of cross-linking increased with deposition power. The polymer surfaces were hydrocarbon-rich, with oxygen present in the form of O–H and C=O functional groups. The oxygen content decreased with deposition power, with films becoming more hydrophobic and, thus, less wettable. The advancing and receding contact angles were investigated, and the water advancing contact angle was found to increase from 63.14° to 73.53° for thin films prepared with an RF power of 10 W to 75 W. The wetting envelopes for the surfaces were constructed to enable the prediction of the surfaces’ wettability for other solvents. The effect of roughness on the wetting behaviour of the films was insignificant. The polymers were determined to resist solubilization in solvents commonly used in the deposition of organic semiconducting layers, including chloroform and chlorobenzene, with higher stability observed in films fabricated at higher RF power.

  3. Hydroxylation of methylated DNA by TET1 in chondrocyte differentiation of C3H10T1/2 cells

    Directory of Open Access Journals (Sweden)

    Ryo Ito

    2016-03-01

    Full Text Available DNA methylation is closely involved in the regulation of cellular differentiation, including chondrogenic differentiation of mesenchymal stem cells. Recent studies showed that Ten–eleven translocation (TET family proteins converted 5-methylcytosine (5mC to 5-hydroxymethylcytosine, 5-formylcytosine and 5carboxylcytosine by oxidation. These reactions constitute potential mechanisms for active demethylation of methylated DNA. However, the relationship between the DNA methylation patterns and the effects of TET family proteins in chondrocyte differentiation is still unclear. In this study, we showed that DNA hydroxylation of 5mC was increased during chondrocytic differentiation of C3H10T1/2 cells and that the expression of Tet1 was particularly enhanced. Moreover, knockdown experiments revealed that the downregulation of Tet1 expression caused decreases in chondrogenesis markers such as type 2 and type 10 collagens. Furthermore, we found that TET proteins had a site preference for hydroxylation of 5mC on the Insulin-like growth factor 1 (Igf1 promoter in chondrocytes. Taken together, we showed that the expression of Tet1 was specifically facilitated in chondrocyte differentiation and Tet1 can regulate chondrocyte marker gene expression presumably through its hydroxylation activity for DNA.

  4. Placental transfer of 14C-hexoprenaline

    International Nuclear Information System (INIS)

    Lipshitz, J.; Broyles, K.; Whybrew, W.D.; Ahokas, R.A.; Anderson, G.D.

    1982-01-01

    The placental transfer of a single intravenous injection of 14C-hexoprenaline was studied in eight pregnant New Zealand white rabbits. Maternal and fetal blood was sampled intermittently for 60 minutes after the injection. An initial rapid decrease in the levels of 14C-hexoprenaline in maternal blood was followed by a second slower phase, whereas fetal levels remained insignificant. The conclusion, therefore, is that the rapid improvement in fetal heart rate after the administration of a single maternal intravenous injection of hexoprenaline in the treatment of fetal distress is due to the action on the uterus and/or on maternal cardiovascular function, and not to direct stimulation of the fetus

  5. TMEM14C is required for erythroid mitochondrial heme metabolism.

    Science.gov (United States)

    Yien, Yvette Y; Robledo, Raymond F; Schultz, Iman J; Takahashi-Makise, Naoko; Gwynn, Babette; Bauer, Daniel E; Dass, Abhishek; Yi, Gloria; Li, Liangtao; Hildick-Smith, Gordon J; Cooney, Jeffrey D; Pierce, Eric L; Mohler, Kyla; Dailey, Tamara A; Miyata, Non; Kingsley, Paul D; Garone, Caterina; Hattangadi, Shilpa M; Huang, Hui; Chen, Wen; Keenan, Ellen M; Shah, Dhvanit I; Schlaeger, Thorsten M; DiMauro, Salvatore; Orkin, Stuart H; Cantor, Alan B; Palis, James; Koehler, Carla M; Lodish, Harvey F; Kaplan, Jerry; Ward, Diane M; Dailey, Harry A; Phillips, John D; Peters, Luanne L; Paw, Barry H

    2014-10-01

    The transport and intracellular trafficking of heme biosynthesis intermediates are crucial for hemoglobin production, which is a critical process in developing red cells. Here, we profiled gene expression in terminally differentiating murine fetal liver-derived erythroid cells to identify regulators of heme metabolism. We determined that TMEM14C, an inner mitochondrial membrane protein that is enriched in vertebrate hematopoietic tissues, is essential for erythropoiesis and heme synthesis in vivo and in cultured erythroid cells. In mice, TMEM14C deficiency resulted in porphyrin accumulation in the fetal liver, erythroid maturation arrest, and embryonic lethality due to profound anemia. Protoporphyrin IX synthesis in TMEM14C-deficient erythroid cells was blocked, leading to an accumulation of porphyrin precursors. The heme synthesis defect in TMEM14C-deficient cells was ameliorated with a protoporphyrin IX analog, indicating that TMEM14C primarily functions in the terminal steps of the heme synthesis pathway. Together, our data demonstrate that TMEM14C facilitates the import of protoporphyrinogen IX into the mitochondrial matrix for heme synthesis and subsequent hemoglobin production. Furthermore, the identification of TMEM14C as a protoporphyrinogen IX importer provides a genetic tool for further exploring erythropoiesis and congenital anemias.

  6. 14C Analysis of protein extracts from Bacillus spores.

    Science.gov (United States)

    Cappuccio, Jenny A; Falso, Miranda J Sarachine; Kashgarian, Michaele; Buchholz, Bruce A

    2014-07-01

    Investigators of bioagent incidents or interdicted materials need validated, independent analytical methods that will allow them to distinguish between recently made bioagent samples versus material drawn from the archives of a historical program. Heterotrophic bacteria convert the carbon in their food sources, growth substrate or culture media, into the biomolecules they need. The F(14)C (fraction modern radiocarbon) of a variety of media, Bacillus spores, and separated proteins from Bacillus spores was measured by accelerator mass spectrometry (AMS). AMS precisely measures F(14)C values of biological materials and has been used to date the synthesis of biomaterials over the bomb pulse era (1955 to present). The F(14)C of Bacillus spores reflects the radiocarbon content of the media in which they were grown. In a survey of commercial media we found that the F(14)C value indicated that carbon sources for the media were alive within about a year of the date of manufacture and generally of terrestrial origin. Hence, bacteria and their products can be dated using their (14)C signature. Bacillus spore samples were generated onsite with defined media and carbon free purification and also obtained from archived material. Using mechanical lysis and a variety of washes with carbon free acids and bases, contaminant carbon was removed from soluble proteins to enable accurate (14)C bomb-pulse dating. Since media is contemporary, (14)C bomb-pulse dating of isolated soluble proteins can be used to distinguish between historical archives of bioagents and those produced from recent media. Copyright © 2014 Elsevier Ireland Ltd. All rights reserved.

  7. 2-(5-Fluoro-3-isopropylsulfanyl-7-methyl-1-benzofuran-2-ylacetic acid

    Directory of Open Access Journals (Sweden)

    Hong Dae Choi

    2012-04-01

    Full Text Available The title compound, C14H15FO3S, was prepared by alkaline hydrolysis of ethyl 2-(5-fluoro-3-isopropylsulfanyl-7-methyl-1-benzofuran-2-ylacetate. In the crystal, molecules are linked via pairs of O—H...O hydrogen bonds, forming inversion dimers. These dimers are connected by weak C—H...O hydrogen bonds.

  8. The microdose rapid 14C urea breath test compares well with the original rapid 14 breath test

    International Nuclear Information System (INIS)

    Bellon, M.S.; Bartholomeusz, F.D.L.; Chatterton, B.E.

    2000-01-01

    Full text: The 14 C urea breath test (CUBT) is a sensitive test used in the detection of H. pylori infection. The rapid 14 CUBT using 185 KBq of 14 C urea showed a sensitivity of 100% when tested in 36 patients. The aim of this study was to compare the results of the 14 CUBT performed following the ingestion of 37KBq microdose 14 C urea capsule (Bicapsule, Trimed) with the earlier method which uses 185 KBq 14 C urea. 19 patients (nine female age 21-52 yrs) were studied. All subjects first underwent a 14 CUBT with the microdose capsule and a single 15 minute post ingestion sample. An hour later the test was repeated but with a dose of 185 KBq 14 C urea in liquid form. A normal result was taken as 2 = 0.92). This is shown above. The Rapid 14 CUBT performed following the microdose capsule whilst reducing patient radiation exposure is an accurate test for the detection of H. pylori. Copyright (2000) The Australian and New Zealand Society of Nuclear Medicine Inc

  9. Residues of 14C-paclobutrazol in mangoes

    International Nuclear Information System (INIS)

    Costa, Maria A.; Tornisielo, Valdemar L.; Castanho, Giuliane M.

    2009-01-01

    Paclobutrazol (PBZ) is a growth regulator used in agricultural systems whose purpose is the control of vegetative growth, stimulating the reproductive capacity of plants. This growth regulator remains active in soil for a long time and its half-life varies with the type of soil and climatic conditions, can severely affect the development of crops. This work aimed to study the residues / metabolites of 14 C-PBZ in mango pulp Tommy Atkins. The tests were performed with mangoes grown in pots stainless steel and application of 14 C-PBZ was performed by the soil projection of the crown, and the mangoes tested in two periods, one year and two years after application. To evaluate the levels of residues of 14 C-PBZ was realize the burning of 200 mg of pulp on biological oxidized and detached 14 CO 2 was detected by liquid scintillation spectrophotometer. The results were 1.65 % of residue of PBZ on fruit collected after two years of application and 4.30 % of residue of PBZ collected on fruit after a year of application and also can see that the product remained in the soil for more than one year, is translocated to the plant and reach the edible part, the pulp fruit. The identification of residual 14 C- PBZ/metabolites by thin-layer chromatography did not reveal any pattern of PBZ / metabolites due to the low activity detected in the samples. Therefore, another procedure was performed for extraction and then analyzed by high performance liquid chromatography (HPLC) for detection of metabolites in the PBZ of mango pulp. (author)

  10. Increased tumor uptake of 67Ga citrate following a course of picibanil (NSC-B116209)

    International Nuclear Information System (INIS)

    Okuyama, Shinichi; Matsuzawa, Taiju; Mishina, Hitoshi.

    1979-01-01

    Exposure to exponential dose schedules of OK-432, penicillin-inactivated preparation of streptococcus hemolyticus (NSC-B116209), resulted in an increased retention of 67 Ga citrate. Its uptake in footpad tumors of AH 109A was also increased. The results may suggest that pretreatment with OK-432 would increase tumor uptake of 67 Ga citrate and help scintigraphic delineation of malignancies in man. It may probably augment tumor concentration of anticancer chemotherapeutics, too. Thus, the tumor affinitive property of OK-432 can be taken advantage of in anticancer strategy as well as cancer detection by 67 Ga scanning. (author)

  11. Automated synthesis of 11C-carfentanil with 11C-choline module and micro PET imaging

    International Nuclear Information System (INIS)

    Zhang Jinming; Zhang Xiaojun; Tian Jiahe; Xu Zhihong; Xiang Xiaohui

    2011-01-01

    A simple modified home-made 11 C-choline module enabled to rapid and efficient synthesis 11 C-carfentanil ( 11 C-CFN) as CNS μ-opioid receptor imaging agent. The synthesis of 11 C-CFN was completed in a yield of 14.8 GBq within 18 min from 11 C-CO 2 on the choline module. The methylation took place from 4-piperidinecarboxylic acid, 4-[(1-oxopropyl) phenylamino]-l-(2-phenylethyl), sodium salt as precursor in DMSO solution. The radio- chemical yields were over 80% (n=55, decay-corrected and based on 11 CH 3 -triflate). The radiochemical purity was over 95% and the specific activities was over 1.4 × 10 14 Bq/g. The biologic activity of 11 C-CFN was confirmed with Micro PET/CT imaging. (authors)

  12. Agonists and partial agonists of rhodopsin: retinal polyene methylation affects receptor activation.

    Science.gov (United States)

    Vogel, Reiner; Lüdeke, Steffen; Siebert, Friedrich; Sakmar, Thomas P; Hirshfeld, Amiram; Sheves, Mordechai

    2006-02-14

    Using Fourier transform infrared (FTIR) difference spectroscopy, we have studied the impact of sites and extent of methylation of the retinal polyene with respect to position and thermodynamic parameters of the conformational equilibrium between the Meta I and Meta II photoproducts of rhodopsin. Deletion of methyl groups to form 9-demethyl and 13-demethyl analogues, as well as addition of a methyl group at C10 or C12, shifted the Meta I/Meta II equilibrium toward Meta I, such that the retinal analogues behaved like partial agonists. This equilibrium shift resulted from an apparent reduction of the entropy gain of the transition of up to 65%, which was only partially offset by a concomitant reduction of the enthalpy increase. The analogues produced Meta II photoproducts with relatively small alterations, while their Meta I states were significantly altered, which accounted for the aberrant transitions to Meta II. Addition of a methyl group at C14 influenced the thermodynamic parameters but had little impact on the position of the Meta I/Meta II equilibrium. Neutralization of the residue 134 in the E134Q opsin mutant increased the Meta II content of the 13-demethyl analogue, but not of the 9-demethyl analogue, indicating a severe impairment of the allosteric coupling between the conserved cytoplasmic ERY motif involved in proton uptake and the Schiff base/Glu 113 microdomain in the 9-demethyl analogue. The 9-methyl group appears therefore essential for the correct positioning of retinal to link protonation of the cytoplasmic motif with protonation of Glu 113 during receptor activation.

  13. Synthesis and characterization of 14C polyvinylphosphonic acid

    International Nuclear Information System (INIS)

    Stringer, O.D.; Charig, A.

    1989-01-01

    Ten mCi of 14 C ethylene was converted to 1.16 mCi of 14 C PVPA by oxidative phosphonation with phosphorus trichloride and molecular oxygen, dehydrohalogenation with triethylamine in ether, polymerization, and hydrolysis. The polymer had a specific activity of 12 uCi/mg and a radiochemical purity over 99%. (Author)

  14. Dating of groundwater with tritium and 14C

    International Nuclear Information System (INIS)

    Muennich, K.O.; Roether, W.; Thilo, L.

    1967-01-01

    Shallow groundwater can be dated with some accuracy on the basis of its bomb tritium content if the unsaturated soil cover and the aquifer itself is sufficiently homogeneous. A few examples from the Rhine valley are presented. The decrease in tritium level from the water table to a few metres below is nearly two orders of magnitude. Agreement between the measured or estimated variation of bomb tritium in rain during the past decade and the tritium found in shallow groundwater can be obtained if one takes into account that (a) practically no summer rain reaches the water table, and (b) water is mixed by diffusion. Both effects can also be observed in the soil moisture of the unsaturated soil above the water table. Carbon-14 increase in groundwater due to bombs is delayed compared to tritium, the reasons being delay in the biological system and exchange with the carbonate in the soil. Nevertheless lysimeters show a marked increase of 14 C, which depends on the plant cover, being high in a plant-covered lysimeter and low in a bare one. A simple model is presented, which allows the evaluation of the influence of exchange on the 14 C age obtained. It turns out that the deviation from the true age depends on the ratio of the carbonate content in the aquifer material to the carbonate content of the water, on the specific contact surface or the grain size but not on the groundwater velocity. On the basis of this model the experimental finding that 14 C ages are usually in agreement with other age estimates despite the loss by exchange is plausible owing to the fact that only material of sufficiently coarse grain size can make up a reasonable aquifer. Assuming only exchange with a monomolecular surface layer of the carbonate grains one finds that the 14 C age is likely to differ by not more than a factor of two in the most unfavourable case. Under natural conditions (steady state of cosmic-ray-produced 14 C) the 14 C content of shallow groundwater is hardly influenced at

  15. Synthesis of the muscle relaxant [14C]L-637,510

    International Nuclear Information System (INIS)

    O'Connor, S.P.; Ellsworth, R.L.; Gatto, G.

    1991-01-01

    The synthesis of (E)-3-(9-chloro-5,6-dihydro-11H-pyrolo(2,1-b)(3)-benzazepin-11-ylidene)-N,N-dimethyl-1- [3- 14 C]-propanamine (Z)-2-butenedioate(1:1) ([ 14 C]L-637,510), a potential muscle relaxant product for which 14 C-labeling was required for metabolism studies, is described. Introduction of the label in the 3-position of the propanamine side chain was accomplished in eight steps from sodium [ 14 C]cyanide with an overall radiochemical yield of 4.8%. (author)

  16. The effects of the oral administration of fish oil concentrate on the release and the metabolism of [14C]arachidonic acid and [14C]eicosapentaenoic acid by human platelets

    International Nuclear Information System (INIS)

    Hirai, A.; Terano, T.; Hamazaki, T.

    1982-01-01

    It has been suggested by several investigators that eicosapentaenoic acid (C20:5 omega 3, EPA) might have anti-thrombotic effects. In this experiment, the effect of the oral administration of EPA rich fish oil concentrate on platelet aggregation and the release and the metabolism of [ 1 - 14 C]arachidonic acid and [(U)- 14 C]eicosapentaenoic acid by human platelets was studied. Eight healthy male subjects ingested 18 capsules of fish oil concentrate (EPA 1.4 g) per day for 4 weeks. Plasma and platelet concentrations of EPA markedly increased, while those of arachidonic acid (C20:4 omega 6, AA) and docosahexaenoic acid (C22:6 omega 3, DHA) did not change. Platelet aggregation induced by collagen and ADP was reduced. Collagen induced [ 14 C]thromboxane B2 (TXB2) formation from [ 14 C]AA prelabeled platelets decreased. There was no detectable formation of [ 14 C]TXB3 from [ 14 C]EPA prelabeled platelets, and the conversion of exogenous [ 14 C]EPA to [ 14 C]TXB3 was lower than that of [ 14 C]AA to [ 14 C]TXB2. The release of [ 14 C]AA from [ 14 C]AA prelabeled platelets by collagen was significantly decreased. These observations raise the possibility that the release of arachidonic acid from platelet lipids might be affected by the alteration of EPA content in platelets

  17. Global DNA methylation analysis using methyl-sensitive amplification polymorphism (MSAP).

    Science.gov (United States)

    Yaish, Mahmoud W; Peng, Mingsheng; Rothstein, Steven J

    2014-01-01

    DNA methylation is a crucial epigenetic process which helps control gene transcription activity in eukaryotes. Information regarding the methylation status of a regulatory sequence of a particular gene provides important knowledge of this transcriptional control. DNA methylation can be detected using several methods, including sodium bisulfite sequencing and restriction digestion using methylation-sensitive endonucleases. Methyl-Sensitive Amplification Polymorphism (MSAP) is a technique used to study the global DNA methylation status of an organism and hence to distinguish between two individuals based on the DNA methylation status determined by the differential digestion pattern. Therefore, this technique is a useful method for DNA methylation mapping and positional cloning of differentially methylated genes. In this technique, genomic DNA is first digested with a methylation-sensitive restriction enzyme such as HpaII, and then the DNA fragments are ligated to adaptors in order to facilitate their amplification. Digestion using a methylation-insensitive isoschizomer of HpaII, MspI is used in a parallel digestion reaction as a loading control in the experiment. Subsequently, these fragments are selectively amplified by fluorescently labeled primers. PCR products from different individuals are compared, and once an interesting polymorphic locus is recognized, the desired DNA fragment can be isolated from a denaturing polyacrylamide gel, sequenced and identified based on DNA sequence similarity to other sequences available in the database. We will use analysis of met1, ddm1, and atmbd9 mutants and wild-type plants treated with a cytidine analogue, 5-azaC, or zebularine to demonstrate how to assess the genetic modulation of DNA methylation in Arabidopsis. It should be noted that despite the fact that MSAP is a reliable technique used to fish for polymorphic methylated loci, its power is limited to the restriction recognition sites of the enzymes used in the genomic

  18. Metabolism of L-[guanidinooxy-14C]canavanine in the rat

    International Nuclear Information System (INIS)

    Thomas, D.A.; Rosenthal, G.A.

    1987-01-01

    The metabolism of L-canavanine, a nonprotein amino acid with significant antitumor effects, was investigated. L-Canavanine, provided at 2.0 g/kg, was supplemented with 5 microCi of L-[guanidinooxy- 14 C]canavanine (58 microCi/mumol) and administered iv, sc, or orally to female Sprague-Dawley rats weighing approximately 200 g. 14 C recovery in the urine at 24 hr was 83, 68, or 61%, respectively, of the administered dose. Another 5-8% of the 14 C was expired as 14 CO 2 . The gastrointestinal tract contained 21% of orally administered 14 C. Serum, feces, tissues, and de novo synthesized proteins only accounted for a few percent of the original dose by any administrative route. Analysis of the 14 C-containing urinary metabolites revealed that [ 14 C] urea accounted for 88% of the urinary radioactivity for an iv injection, 75% for sc administration, and 50% following an oral dose. By all routes of administration, [ 14 C]guanidine represented 5% of the radioactivity in the urine and [ 14 C]guanidinoacetic acid accounted for 2%. Serum and urine amino acid analysis showed a markedly elevated ornithine level. Basic amino acids such as histidine, lysine, and arginine were also higher in the urine. Plasma ammonia levels were determined following oral canavanine doses of 1.0, 2.0, and 4.0 g/kg. A rapid but transient elevation in plasma ammonia was observed only at the 4.0 g/kg dose. This indicates that elevated plasma ammonia is not a likely cause of canavanine toxicity at the drug concentrations used in this study

  19. Working out microsyntheses for different chlorinated biphenyls and preparation of 2,2'-dichlorobiphenyl-14C and 2,4'-dichlorobiphenyl-14C

    International Nuclear Information System (INIS)

    Geuenich, H.H.

    1972-01-01

    The microsyntheses for the preparation of chlorated biphenyls starting with benzene were worked out. 2,2'-dichlorobiphenyl- 14 C and 2,4'-dichlorobiphenyl- 14 C were prepared. 42 mCi benzene- 14 C were converted into nitrobenzene with nitrating acid, which was reduced to aniline by tin(II) chloride/hydrochloric acid. Following the acetylation of aniline with acetic anhydride, it was monochlorated in glacial acetic acid with chloride of lime, and the chlorination mixture was chromatographically separated in columns. 5.8 mCi o'-chloroanaline were diazotized and converted in ammoniacal copper(I) salt solution. 2 μCi 2,2'-dichlorobiphenyl were obtained. (orig./LH) [de

  20. Fate and O-methylating detoxification of Tetrabromobisphenol A (TBBPA) in two earthworms (Metaphire guillelmi and Eisenia fetida).

    Science.gov (United States)

    Chen, Xian; Gu, Jianqiang; Wang, Yongfeng; Gu, Xueyuan; Zhao, Xiaopeng; Wang, Xiaorong; Ji, Rong

    2017-08-01

    Tetrabromobisphenol A (TBBPA) is the world's most widely used brominated flame retardant but there is growing concern about its fate and toxicity in terrestrial organisms. In this study, two ecologically different earthworms, Metaphire guillelmi and Eisenia fetida, were exposed to soil spiked with 14 C-labeled TBBPA for 21 days. M. guillelmi accumulated more TBBPA than E. fetida, evidenced by a 2.7-fold higher 14 C-uptake rate and a 1.3-fold higher biota-soil accumulation factor. Considerable amounts of bound residues (up to 40% for M. guillelmi and 18% for E. fetida) formed rapidly in the bodies of both earthworms. 14 C accumulated mostly in the gut of M. guillemi and in the skin of E. fetida, suggesting that its uptake by M. guillelmi was mainly via gut processes whereas in E. fetida epidermal adsorption predominated. The TBBPA transformation potential was greater in M. guillelmi than in E. fetida, since only 5% vs. 34% of extractable 14 C remained as the parent compound after 21 days of exposure. Besides polar metabolites, the major metabolites in both earthworms were TBBPA mono- and dimethyl ethers (O-methylation products of TBBPA). Acute toxicity assessments using filter paper and natural soil tests showed that the methylation metabolites were much less toxic than the parent TBBPA to both earthworms. It indicated that earthworms used O-methylation to detoxify TBBPA, and M. guillelmi exhibited the higher detoxification ability than E. fetida. These results imply that if only the free parent compound TBBPA is measured, not only bioaccumulation may be underestimated but also its difference between earthworm species may be misestimated. The species-dependent fate of TBBPA may provide a better indicator of the differing sensitivities of earthworms to this environmental contaminant. Copyright © 2017 Elsevier Ltd. All rights reserved.