bluuebunny/crossref_metadata_2025 huggingface dataset:
Constitutive activation of Stat5 promotes its cytoplasmic localization and association with PI3-kinase in myeloid leukemias
Authors: Harir Noria , Pecquet Christian , Kerenyi Marc , Sonneck Karoline , Kovacic Boris , Nyga Remy , Brevet Marie , Dhennin Isabelle , Gouilleux-Gruart Valerie , Beug Hartmut , Valent Peter , Lassoued Kaiss , Moriggl Richard , Gouilleux Fabrice
Published: October 2006

Persistent activation of Stat5 is frequently found in hematologic neoplasms. Studies conducted with constitutively active Stat5 mutants (Stat51*6 and cS5F) have shown that deregulated Stat5 activity promotes leukemogenesis. To investigate the oncogenic properties of these mutants, we used cS5F-expressing bone marrow cells which induce a multilineage leukemia when transplanted into recipient mice. Here, we show by immunocytochemistry that cS5F is localized mainly in the cytoplasmic compartment of leukemic cells, suggesting that the transforming nature of cS5F may be associated with a cytoplasmic function. In support of this hypothesis, we found that cS5F forms a complex with the p85 subunit of the phosphatidylinositol 3-kinase (PI3-K) and the scaffolding adapter Gab2 in leukemic bone marrow cells, resulting in the activation of Akt/PKB, a crucial downstream target of PI3-K. By using transducible TAT-Gab2 or TAT-Akt recombinant proteins, we were able to demonstrate that activation of the PI3-kinase/Akt pathway by cS5F molecules through Gab2 is essential for induction of cell growth. We also found that persistently phosphorylated Stat5 in primary cells from patients with myeloid leukemias has a cytoplasmic localization. These data suggest that oncogenic Stat5 proteins exert dual transforming capabilities not only as transcriptional activators but also as cytoplasmic signaling effectors.
Receptor activator of nuclear factor (NF)–κB ligand (RANKL) increases vascular permeability: impaired permeability and angiogenesis in eNOS-deficient mice
Authors: Min Jeong-Ki , Cho Young-Lai , Choi Jae-Hoon , Kim Yonghak , Kim Jeong Hun , Yu Young Suk , Rho Jaerang , Mochizuki Naoki , Kim Young-Myeong , Oh Goo Taeg , Kwon Young-Guen
Published: October 2006

Receptor activator of nuclear factor (NF)–κB ligand (RANKL) is emerging as an important regulator of vascular pathophysiology. Here, we demonstrate a novel role of RANKL as a vascular permeability factor and a critical role of endothelial nitric oxide synthase (eNOS) in RANKL-induced endothelial function. RANKL increased the vascular permeability and leukocyte infiltration in vivo and caused the breakdown of the blood-retinal barrier in wild-type mice but not in eNOS-deficient mice. In vitro, it increased endothelial permeability and reduced VE-cadherin–facilitated endothelial cell-cell junctions in a NO-dependent manner. RANKL also led to the activation of Akt and eNOS and to NO production in endothelial cells (ECs). These effects were suppressed by the inhibition of TRAF6, phosphoinositide 3′-kinase (PI3K), Akt, or NOS by genetic or pharmacologic means. Inhibition of the TRAF6-mediated NO pathway reduced EC migration and capillary-like tube formation in response to RANKL. Moreover, the effects of RANKL on ECs sprouting from the aorta, and neovessel formation in both the mouse Matrigel plug assay and corneal micropocket assay, were impaired in eNOS-deficient mice. These results demonstrate that RANKL promotes vascular permeability and angiogenesis by stimulating eNOS by a TRAF6-PI3K-Akt–dependent mechanism. These properties may be relevant to the pathogenesis of angiogenesis-dependent and inflammatory vascular diseases.
Genomic analysis reveals that Pseudomonas aeruginosa virulence is combinatorial
Authors: Lee Daniel G , Urbach Jonathan M , Wu Gang , Liberati Nicole T , Feinbaum Rhonda L , Miyata Sachiko , Diggins Lenard T , He Jianxin , Saucier Maude , Déziel Eric , Friedman Lisa , Li Li , Grills George , Montgomery Kate , Kucherlapati Raju , Rahme Laurence G , Ausubel Frederick M
Published: October 2006

Background

Pseudomonas aeruginosa is a ubiquitous environmental bacterium and an important opportunistic human pathogen. Generally, the acquisition of genes in the form of pathogenicity islands distinguishes pathogenic isolates from nonpathogens. We therefore sequenced a highly virulent strain of P. aeruginosa, PA14, and compared it with a previously sequenced (and less pathogenic) strain, PAO1, to identify novel virulence genes.

Results

The PA14 and PAO1 genomes are remarkably similar, although PA14 has a slightly larger genome (6.5 megabses [Mb]) than does PAO1 (6.3 Mb). We identified 58 PA14 gene clusters that are absent in PAO1 to determine which of these genes, if any, contribute to its enhanced virulence in a Caenorhabditis elegans pathogenicity model. First, we tested 18 additional diverse strains in the C. elegans model and observed a wide range of pathogenic potential; however, genotyping these strains using a custom microarray showed that the presence of PA14 genes that are absent in PAO1 did not correlate with the virulence of these strains. Second, we utilized a full-genome nonredundant mutant library of PA14 to identify five genes (absent in PAO1) required for C. elegans killing. Surprisingly, although these five genes are present in many other P. aeruginosa strains, they do not correlate with virulence in C. elegans.

Conclusion

Genes required for pathogenicity in one strain of P. aeruginosa are neither required for nor predictive of virulence in other strains. We therefore propose that virulence in this organism is both multifactorial and combinatorial, the result of a pool of pathogenicity-related genes that interact in various combinations in different genetic backgrounds.
Impairment of T cell interactions with antigen-presenting cells by immunosuppressive drugs reveals involvement of calcineurin and NF-κB in immunological synapse formation
Authors: Zeyda Maximilian , Geyeregger René , Poglitsch Marko , Weichhart Thomas , Zlabinger Gerhard J , Koyasu Shigeo , Hörl Walter H , Stulnig Thomas M , Watschinger Bruno , Saemann Marcus D
Published: October 2006

A stable supramolecular cluster in T cells at the contact site of APCs, the immunological synapse (IS), is essential for full T cell activation. Failure of IS maturation, as determined by defective relocalization of the TCR/CD3 complex at the T cell/APC contact site, is linked with T cell hyporesponsiveness. The effects of clinically used immunosuppressants on these critical events, however, are undefined. Here, we show that treatment of T cells with cyclosporin A, FK506, and dexamethasone, which are known to inhibit calcineurin and NF-κB, respectively, but not rapamycin, the inhibitor of mammalian target of rapamycin, selectively prevented TCR/CD3 relocalization into the IS, while relocalization of adhesion and cytoskeletal proteins as well as T cell/APC conjugate formation remained unaltered. The involvement of calcineurin and NF-κB in IS maturation was confirmed by using specific inhibitors of these molecules (FR901725, gossypol, SN50). FK778, as an inhibitor of DNA replication and also TCR/CD3-activated tyrosine kinases, globally abrogated cytoskeletal, adhesion, and signaling molecule relocalization, thereby preventing formation of an IS at an earlier, immature stage along with impaired, antigen-specific T cell/APC conjugate formation. Collectively, blocking IS formation at distinct stages may mediate effects on T cell activation of currently used immunosuppressants, apart from their capacity to block gene transcription, cytokine signaling, and DNA replication. Furthermore, these data imply novel functions of calcineurin and NF-κB for successful IS maturation.
Reversal of Glucocorticoids-Dependent Proopiomelanocortin Gene Inhibition by Leukemia Inhibitory Factor
Authors: Latchoumanin Olivier , Mynard Vanessa , Devin-Leclerc Jocelyne , Dugué Marie-Annick , Bertagna Xavier , Catelli Maria Grazia
Published: October 2006

We previously have described molecular mechanisms converging at the Nur response element-signal transducer and activator of transcription (STAT) composite site responsible for synergistic activation of the proopiomelanocortin (POMC) gene promoter by leukemia inhibitory factor (LIF) and CRH. In this study, we asked how glucocorticoids (GC), the physiological negative regulators of POMC gene expression, modulate this synergism. In the corticotroph cell line AtT-20, the response of the wild-type promoter to LIF+CRH was barely inhibited by GC, whereas a distal promoter subregion (−414/−293) encompassing the Nur response element-STAT site and devoid of the negative GC-responsive element located in the proximal domain, displayed a cooperative response to LIF + dexamethasone (DEX) and LIF+CRH+DEX treatments. LIF+CRH-stimulated ACTH secretion was also inefficiently inhibited by DEX in the same cell line. This study was focused thereafter on LIF+DEX cooperativity, which may be responsible, on the wild-type promoter, for lack of negative regulation by DEX of the LIF+CRH synergy. The STAT1–3 low-affinity site, in the context of the (−414/−293) subregion of the POMC promoter, was found necessary and sufficient for transcriptional synergism between activated GC receptor (GR) and STAT1–3. Moreover the activities of reporters specific for STAT1–3 or GR were reciprocally enhanced by DEX or LIF. Single and sequential chromatin immunoprecipitations revealed 1) a STAT-dependent corecruitment of coactivators after LIF and LIF+DEX stimulation and 2) a more lasting recruitment of both STAT3 and GR in the same enhanceosome on the endogenous POMC promoter after LIF+DEX joint stimulation than after the single one. Such events may be responsible for a lack of repressive property of GR unmasked on the whole POMC promoter during LIF+CRH stimulation and may contribute to the tonicity of the hypothalamic-pituitary-adrenal axis during inflammatory-infectious diseases.
Ethnicity and behaviour in organizations: A review of British research
Authors: Kenny Etlyn J. , Briner Rob B.
Published: October 2006

Research into the role of ethnicity in behaviour in US organizations has been the subject of several reviews. However no such review of British research has thus far been undertaken. Fifty‐four years' worth of selected occupational psychology, organizational behaviour and human resource management journals were therefore reviewed to identify the number and focus of articles relating to ethnicity in British organizations. On the basis of the review findings four key questions were addressed: (i) How much work has been done? (ii) Why has relatively little work been done? (iii) What have we learned about ethnicity and the British workplace? and, (iv) What do we still need to learn? The research shows that only a limited amount of research has been conducted and most of this focuses on a small number of topics. Six recommendations for future research are made: (i) studying ethnicity in a more careful and detailed way; (ii) developing theory; (iii) examining what happens to minority ethnic employees after selection; (iv) more research on minority ethnic professionals; (v) more qualitative research; and, (vi) a greater focus on specific ethnic groups. Recommendations to draw lessons from the way other disciplines have conceptualized and researched ethnicity are also discussed.
New Durable Sealant of Telechelic Polyacrylate
Authors: Masaoka Y , Nakagawa Y , Hasegawa T , Ando H
Published: October 2006

In this paper, we discuss the application possibilities of a novel telechelic acrylic polymer (NTP) which we have been developing as a versatile base polymer for sealants and adhesives. Due to its unique features, our NTP is expected to offer a variety of applications, including the one for sealants applied in contact with self-cleaning glass (SCG). Our discussion here focuses on the possibilities of this particular application. SCG possesses a photocatalyst layer which enables two reactions, i.e., lessening the contact angle of the glass surface and decomposing organic compounds on the glass surface, by reacting with sunlight. The reactions help wash off dust from the glass surface, mainly by rainwater, to maintain the clearness and beauty of the glass used for building windows in particular. Conventional sealants for this application often lack sufficient weatherability or risk, or a combination thereof contaminating the glass surface causing hydrophobicity. The NTP sealants, on the other hand, has no surface-polluting substances such as a low-molecular-weight silicone often contained in silicone sealants, while maintaining high weatherability. We have conducted our research to study the weatherability of the NTP sealants on SCG and the possible contamination of the SCG surface by the sealants. Our studies have found that the NTP sealants retain good adhesiveness after more than 10 000 h of exposure to UV irradiation (in a Super Xenon Weather Meter) at the interface between the sealant and the glass. We also have found almost no contamination on the SCG surface by the NTP sealants, demonstrated by the results of our tests conducted to measure the contact angles of sealant samples to the glass, through outdoor exposure for about two months.
A Comparison of Predictions From Probabilistic Crack Growth Models Inferred From Virkler's Data
Authors: Cross RJ , Makeev A , Armanios E
Published: October 2006

The significant variability observed in fatigue crack growth experiments requires application of probabilistic modeling techniques to fatigue analyses. In this work, philosophical and practical concerns for probabilistic modeling are discussed. Several probabilistic fatigue models are derived from the Virkler data and then used to make predictions under a different loading condition. This comparison of predictions demonstrates their sensitivity to the choice of model. In this effort a method for inference of random process parameters and corresponding confidence limits from highly statistically dependent observations is developed.
Woman, Buddhist, Entrepreneur: Gender, Moral Values, and Class Anxiety in Late Socialist Vietnam
Authors: Leshkowich Ann Marie
Published: October 2006

By the 1990s, Doi Moi had sparked both desire for profit and suspicion of wealth as a threat to traditional Vietnamese morality. This article explores how one successful businesswoman responded by attributing her prosperity to Buddhist piety. In rejecting the Confucian ethics favored by businessmen, she advanced an interpretation of traditional morality more accommodating of women and defended her class privilege as righteous. Her narrative draws attention to individual performances of class as a means both to justify one's own status and to contribute to the gendered, political, religious, and moral discourses through which class stratification comes to be seen as natural.
Generation and Characterization of Rabbit Embryonic Stem Cells
Authors: Wang Shufen , Tang Xianghui , Niu Yuyu , Chen Hongwei , Li Bin , Li Tianqing , Zhang Xiuzhen , Hu Zhixin , Zhou Qi , Ji Weizhi
Published: October 2006

We described the derivation of four stable pluripotent rabbit embryonic stem cell (ESC) lines, one (RF) from blastocysts fertilized in vivo and cultured in vitro and three (RP01, RP02, and RP03) from parthenogenetic blastocysts. These ESC lines have been cultivated for extended periods (RF >1 year, RP01 >8 months, RP02 >8 months, and RP03 >6 months) in vitro while maintaining expression of pluripotent ESC markers and a normal XY or XX karyotype. The ESCs from all lines expressed alkaline phosphatase, transcription factor Oct-4, stage-specific embryonic antigens (SSEA-1, SSEA-3, and SSEA-4), and the tumor-related antigens (TRA-1-60 and TRA-1-81). Similar to human and mouse ESCs, rabbit ESCs expressed pluripotency (Oct-4, Nanog, SOX2, and UTF-1) and signaling pathway genes (fibroblast growth factor, WNT, and transforming growth factor pathway). Morphologically, rabbit ESCs resembled primate ESCs, whereas their proliferation characteristics were more like those seen in mouse ESCs. Rabbit ESCs were induced to differentiate into many cell types in vitro and formed teratomas with derivatives of the three major germ layers in vivo when injected into severe combined immunodeficient mice. Our results showed that pluripotent, stable ESC lines could be derived from fertilized and parthenote-derived rabbit embryos.
Distinct Population of Hair Cell Progenitors Can Be Isolated from the Postnatal Mouse Cochlea Using Side Population Analysis
Authors: Savary Etienne , Hugnot Jean Philippe , Chassigneux Yolaine , Travo Cecile , Duperray Christophe , Van De Water Thomas , Zine Azel
Published: October 2006

In mammals, the permanence of hearing loss is due mostly to the incapacity of the cochlea to replace lost mechano-receptor cells (i.e., hair cells [HCs]). The generation of new HCs from a renewable source of progenitors is a principal requirement for developing a cell therapy within this sensory organ. A subset of stem cells, termed side population (SP), has been identified in several tissues of mammals. The ATP-binding cassette transporter Abcg2/Bcrp1 contributes to the specification of the SP phenotype and is proposed as a universal marker for stem/progenitor cells. A defining character of these SP cells is a high efflux capacity for Hoechst dye. Here, we demonstrate that Abcg2 transporter is expressed with two other stem/progenitor cell markers (i.e., Nestin and Musashi1) in distinct and overlapping domains of the supporting cells within the postnatal cochlea. We have developed and describe a fluorescence-activated cell sorting (FACS) technique that enables the purification of a discrete subpopulation of SP-supporting cells from the early postnatal mouse cochlea based on their ability to exclude Hoechst dye. These FACS-isolated cells can divide and express markers of stem/progenitor cells such as Abcg2, a determinant of the SP phenotype, and Musashi1, a neural stem/progenitor cell marker. These markers can differentiate cells expressing markers of HCs and supporting cells in vitro. Our observation that these SP cells are capable of differentiating into HC-like cells implies a possible use for such cells (i.e., the replacement of lost auditory HCs within damaged cochlea).
Identification of Candidate Murine Esophageal Stem Cells Using a Combination of Cell Kinetic Studies and Cell Surface Markers
Authors: Croagh Daniel , Phillips Wayne A. , Redvers Rick , Thomas Robert J.S. , Kaur Pritinder
Published: October 2006

The identification and characterization of esophageal stem cells are critical to our understanding of the biology of the esophageal epithelium in health and disease. However, the proliferative compartment within the mouse esophageal epithelium remains poorly characterized. Here, we report that the basal cells of the mouse esophagus can be separated into three phenotypically and functionally distinct subpopulations based on the expression of α6 integrin and transferrin receptor (CD71). Cells that express high levels of α6 integrin and low levels of CD71, termed α6briCD71dim, are a minor subpopulation of small and undifferentiated cells that are enriched for label-retaining cells and thus represent a putative esophageal stem cell population. Conversely, cells expressing high levels of both α6 integrin and CD71 (α6briCD71bri), the majority of basal esophageal cells, are enriched for actively cycling cells and therefore represent a transit-amplifying population. Kinetic analyses revealed that a third cell population, which is α6 integrin-dim and CD71-bright (α6dim), is destined to leave the basal layer and differentiate.
Fibroblast Growth Factor 2 Modulates Transforming Growth Factor β Signaling in Mouse Embryonic Fibroblasts and Human ESCs (hESCs) to Support hESC Self-Renewal
Authors: Greber Boris , Lehrach Hans , Adjaye James
Published: October 2006

Fibroblast growth factor 2 (FGF2) is known to promote self-renewal of human embryonic stem cells (hESCs). In addition, it has been shown that transforming growth factor β (TGFβ) signaling is crucial in that the TGFβ/Activin/Nodal branch of the pathway needs to be activated and the bone morphogenic protein (BMP)/GDF branch repressed to prevent differentiation. This holds particularly true for Serum Replacement-based medium containing BMP-like activity. We have reinvestigated a widely used protocol for conditioning hESC medium with mouse embryonic fibroblasts (MEFs). We show that FGF2 acts on MEFs to release supportive factors and reduce differentiation-inducing activity. FGF2 stimulation experiments with supportive and nonsupportive MEFs followed by genome-wide expression profiling revealed that FGF2 regulates the expression of key members of the TGFβ pathway, with Inhba, Tgfb1, Grem1, and Bmp4 being the most likely candidates orchestrating the above activities. In addition, restimulation experiments in hESCs combined with global expression analysis revealed downstream targets of FGF2 signaling in these cells. Among these were the same factors previously identified in MEFs, thus suggesting that FGF2, at least in part, promotes self-renewal of hESCs by modulating the expression of TGFβ ligands, which, in turn, act on hESCs in a concerted and autocrine manner.
Der Nachbargruppeneffekt bei Additionsreaktionen VI. Mitt.: Lactonisierung von Penten‐(4)‐säuren durch Jod
Authors: Campos M. de Moura , Amaral L. Do
Published: October 2006

Die Abhängigkeit der Lactonbildung von der Jodzugabe wird bei verschiedenen Penten‐(4)‐säuren und γ‐Methyl‐penten‐(4)‐säuren, die Alkyl‐gruppen in α‐Stellung enthalten, untersucht.

Die Größe des Alkylsubstituenten in α‐Stellung ist wichtig für das Zustandekommen des Lactons. Die Lactonausbeute erhöht sich durch die eingeführte Methylgruppe in γ‐Stellung des Moleküls.

Allylmalonsäuren unterliegen nicht der „Selbstlactonisierung”︁.
Darstellung einiger 2‐Alkyl‐4‐acylpyridinthiosemicarbazone. 1. Mitt.: Über Tuberkulostatika
Authors: Eilhauer H. D. , Meinicke K. H.
Published: October 2006

Es wird die Synthese einiger 2‐Alkyl‐4‐acylpyridine und deren Thiosemicarbazone beschrieben. Das 2‐Äthyl‐4‐acetyl‐pyridinthiosemicarbazon zeigte gegenüber dem unsubstituierten 4‐Acetylpyridinthiosemicarbazon keine charakteristische Verbesserung der tuberkulostatischen Wirkung.
Untersuchung der Fettsäuren des Öles aus dem Samen von Luffa echinata Roxb.
Authors: Srivastava K. C. , Tewari J. P.
Published: October 2006

Es wird gezeigt, daß das Öl aus Samen von Luffa echinata ähnlich zusammengesetzt ist wie das anderer Cucurbitaceensamen und daß als Fettsäuren hauptsächlich Öl‐ und Linolsäure vorkommen.
Beiträge zur Konstitution des Alkaloides Amurin und zur Polarographie der Cyclohexadienon‐Verbindungen
Authors: Maturová M. , Hruban L. , Šantavý F. , Wiegrebe W.
Published: October 2006

Die bisher für richtig gehaltene Strukturformel des Alkaloides Amurin wird durch chemische Umsetzungen widerlegt und ein neuer Strukturformel‐Vorschlag als Cyclohexadienon‐Derivat u. a. durch polarographische Untersuchungen des Amurins und authentischer Cyclohexadienon‐Abkömmlinge gestützt.
Polarographische Auswertung von Dünnschicht‐Chromatogrammen
Authors: Oelschläger H. , Volke J. , Lim G. T.
Published: October 2006

Dünnschicht‐chromatographische getrennte Substanzen, z. B. 2‐ und 3‐Nitro‐4‐acetamino‐phenetol, lassen sich schnell und mit großer Genauigkeit (± 3%) polarographisch in Gegenwart des in großen Überschuß vorhandenen Sorptionsmittels ohne Störung bestimmen, wenn das Aluminiumoxid oder Kieselgel vor Zugabe des Elektrolyten mit Dimethylformamid (DMF) geschüttelt worden ist. Durch diese Vorbehandlung wird eine vollständige Desorption des Depolarisators erzielt, eine erneute Adsorption tritt in DMF‐haltigen Elektrolyten nicht ein.
Über das Vorkommen von Isosakuranetin‐7‐rhamnosidoglucosid im Blatt von Monarda didyma L.
Authors: Brieskorn C. H. , Meister G.
Published: October 2006

Das Blatt von Monarda didyma enthält zu 0,02% ein Flavanon‐Glykosid. Sein Aglykon ist 5,7‐Dihydroxy‐4′‐methoxy‐flavanon. Als Zucker liegen Rhamnose und Glucose vor, die über das C‐7‐Hydroxyl des Flavanons gebunden sind. Entgegen anders lautenden Literaturangaben enthält das ätherische Öl von Monarda didyma kein Thymol.
Darstellung einiger Di‐ und Tricarbonsäure‐cetylester
Authors: Neissner R.
Published: October 2006

Direkte Veresterung einiger Di‐ und Tricarbonsäuren mit Cetylalkohol ergibt aus Aceton gut kristallisierende Ester, deren Schmelzpunkte zum Teil erheblich über den in der Literatur angegebenen Werten liegen. Durch Umsetzung der Säurechloride mit Cetylalkohol und Umkristallisieren aus Aceton werden die Schmelzpunkte der durch direkte Veresterung hergestellten Ester bestätigt. Der Citronensäure‐tricetylester wird erstmalig dargestellt.
Zur Biosynthese der Calycanthinalkaloide
Authors: Schütte H. R. , Maier B.
Published: October 2006

In Calycanthus floridus kommen Indol‐ und Chinolinalkaloide vergesellschaftet vor, zu deren Biosynthese eine gemeinsame Herkunft aus Tryptophan diskutiert wird. Zur Prüfung wurde Tryptophan‐[β‐14C] an Calycanthus floridus verabreicht. Die gleichen Einbauraten dieser Aminosäure in die Indol‐ und Chinolinalkaloide sprechen für Tryptophan als gemeinsamen Präcursor.
Phosphatase‐Modelle und ihr Verhalten gegenüber Substraten des intermediären Kohlenhydratstoffwechsels
Authors: Trapmann H. , Devani M.
Published: October 2006

Ionen der Metalle der IV. Nebengruppe des Periodensystems zeigen gegen‐über phosphathaltigen Substraten des Kohlenhydratstoffwechsels in saurem und alkalischem Milieu phosphatatische Eigenschaften; auch Verbindungen wie Adenosintri‐ und ‐monophosphorsäuren werden durch diese Metall‐Ionen dephosphoryliert. Unterschiedliche Katalysatormengen verändern den Substratumsatz; hierfür sind u. a. die Zusammensetzung der Metallhydroxide und der zerfallsfähigen Zwischenprodukte verantwortlich.
Dehydrierung einiger sekundärer Tetrahydroisochinoline mit Hg(II)‐ÄDTA
Authors: Knabe J. , Roloff H.
Published: October 2006

6,7‐Dimethoxy‐1‐phenyl‐ (II) und 6,7‐Dimethoxy‐1‐tert.butyl‐1,2,3,4‐tetrahydroisochinolin (III) lassen sich mit Hg(II)‐ÄDTA unter milden Bedingungen in Ausbeuten von 40% (II) und 85% (III) dehydrieren. Als Hauptprodukte entstehen dabei die entsprechenden 3,4‐Dihydroisochinoline neben einer geringen Menge der betreffenden Isochinoline.
Synthesen in der Reihe der 3,5‐Dioxo‐1,2,4‐oxadiazolidine, III. 19. Mitt. über Hydroxylamin‐Derivate
Authors: Zinner G. , Weber R.‐O.
Published: October 2006

Hydroxyharnstoffe lassen sich auch ohne Acidifizierung durch einen Phenyl‐Substituenten mit Chlorameisensäureäthylester in 3,5‐Dioxo‐1,2,4‐oxadiazolidine überführen; in einigen Fällen bleibt die Reaktion aber auf der Stufe der Äthoxycarbonyloxy‐harnstoffe stehen. Die Alkylierung der monosubstituierten Ringe mit Diazomethan erfolgt am N‐4, im Falle von unsubstituiertem N‐2 jedoch am O der benachbarten Oxo‐Gruppe. Weiter wird über die Ringschlußreaktion des 1,5‐Diphenyl‐3‐hydroxybiurets und Bildungswege des 2‐Phenylcarbamoyl‐4‐phenyl‐3,5‐dioxo‐1,2,4‐oxadiazolidins berichtet.
Untersuchungen an antibakteriellen Substanzen. (VII. Mitt.)
Authors: Goud A. Nagana , Jamkhandi P. S. , Rajagopal S.
Published: October 2006

Es wird die Synthese einiger 4‐(Phenylthio)‐chinazolinverbindungen, die am Phenylkern alkyl‐ und halogen‐substituiert sind, beschrieben. Zusammenhänge zwischen Struktur und antibakterieller Wirkung werden diskutiert.
Dehydrierung von tertiären Aminen mit Hg(II)‐ÄDTA 12. Mitt.: Synthese und Hofmann‐Abbau von 6,7‐Dimethoxy‐2‐methyl‐1,4‐bisbenzylisochinoliniumjodid
Authors: Knabe J. , Roloff H. , Shukla U. R.
Published: October 2006

Durch Synthese und Hofmann‐Abbau von 6,7‐Dimethoxy‐2‐methyl‐1,4‐bis‐benzyl‐isochinoliniumjodid (IX) wird gezeigt, daß der früher bei der Hg(II)‐ÄDTA‐Dehydrierung von 6,7 Dimethoxy‐2‐methyl‐1,1‐bisbenzyl‐1,2,3,4‐tetrahydroisochinolin erhaltenen Isochinoliniumverbindung nicht die Struktur IX zukommt. Da die 1,4‐Stellung der beiden Benzylgruppen in dem fraglichen Dehydrierungsprodukt bewiesen ist, steht damit fest, daß eine zusätzlich angenommene Methylgruppe tatsächlich vorhanden ist.
Zur Kritik des objektiven Mechanismus: Nietzsche und Hegel
Authors: Löw Reinhard
Published: October 2006

Kant is often incorrectly regarded as the father of objective mechanism, a theory of ontological realism in the 19th and 20th century. Nietzsche raised the objection that the notion of causality has its origin in the self‐experience of subjects ‐ so objectivity could not be claimed for mechanism at all. Physics as well as metaphysics is interpretation, not explanation of the world. Hegel likewise asserts the theoretical impregnance of „facts”︁, but here the difference between concept and thing is one which calls for its surmounting. Mechanism is one step in the development of the absolute idea; it is a necessary category, but, taken as the absolute, in itself contradictory. Ultimately the interpretation of nature is grounded in the way mankind wants to understand itself: as free or as a machine.
Politik und Wissenschaft im schwedischen Exil
Authors: Korlén Gustav
Published: October 2006

Politics and Scholarship Among Germans in Swedish Exile. The author's main source is H. Müssener's doctoral thesis on the fate of the about 5,000 refugees of German speech who left Hitler‐dominated Europe for Sweden during the fateful years 1933‐45. Thirty per cent left for political reasons. Only about 60 immigrants possessed an academic background. Well‐known is the Swedish influence on Willy Brandt, Bruno Kreisky, Herbert Wehner and others. But whereas the political refugees could count upon the solidarity and assistance of their Swedish party associates, the academics would find themselves moving in a milieu which was still strongly influenced by the pro‐German university tradition ever since the period of German cultural predominance following upon Bismarck's foundation of the Reich. Only two academics were awarded university professorships, the philosopher Ernst Cassirer in Gothenburg and the psychologist David Katz in Stockholm, who both had to cope with the prevalent positivistic orientation of Swedish philosophy. The pro‐German attitude of the German departments, coupled with their purely linguistic tradition, made it impossible for two prominent scholars to obtain a subsistence within the universities: Walter Berendsohn and Käte Hamburger. In 1952, however, Berendsohn was given a readership at the university of Stockholm and thanks to him the German Department soon became a centre for literary research, especially with regard to German literature in exile. Also in musicology immigrants have come to play an important part. After the war German literary critics and journalists, many of them by this time bi‐lingual (like Peter Weiss), contributed to the re‐establishment of cultural relations between Sweden and the German‐speaking countries.
Die Kosmogonie Anton von Zachs
Authors: Brosche Peter
Published: October 2006

In his “Cosmogenische Betrachtungen” (1804), Anton von Zach rediscovered — probably independently — some aspects of the theories of Kant and Laplace. More originally, he envisaged also the consequences of an era of heavy impacts in the early history of the Earth.
Romantischer Dilettantismus — Johann Wilhelm Ritter und die Begründung der Elektrochemie
Authors: Dietzsch Steffen
Published: October 2006

In this paper the psychological and historical problems of the german philosophy of nature at the time about 1800 are described. During this time the romantic philosopher and scientist of nature Ritter developed a new scientific branch of knowledge: the electrochemistry. Ritter represents exemplarily the type of a romantic dilettante. In this period, the problem of dilettantism got a new validity, especially by Goethe and Schiller: it was recognized as a positive power of human.

In the romantic dilettantism of Ritter three aspects are shown: 1st, romantic dilettantes are intellectual flaneurs; 2nd, romantic dilettantes confront facts and general provisions, which up to this moment are supposed to be paradox, and obtain by this method a synthesis; 3rd, romantic dilettantes favour the intuitive power.
Der kundige Laie und das naturkundliche illustrierte Flugblatt der frühen Neuzeit
Authors: Harms Wolfgang
Published: October 2006

The aim of this paper is to demonstrate how German and Latin illustrated broadsheets of the sixteenth and seventeenth centuries can serve as documents of the history of sciences and the dissemination of scientific knowledge. It shows how broadsheets were used as a means of conveying scientific observations and conclusions not only among scholars versed in Latin but, through the medium of the vernacular, between scholars and laymen, too. In the fields of medicine, astronomy, zoology and botany in particular, the illustrated broadsheet facilitated the rapid circulation of case histories and accounts of various scientific phenomena. Furthermore, it played an important role in breaking down the barriers that separated the scholar from the layman, who was otherwise far removed from the world of books.
Die Komplementarität von interner und externer Wissenschaftsgeschichte
Authors: Rapp Friedrich
Published: October 2006

In studies of the history of science two apparently diverging ‘ideal types’ can be distinguished. The internal analysis relies on methodology and on the philosophy of science and concentrates on the cognitive system and on the sequence of theories. The external analysis relies on sociology, the history of institutions, biographies, etc. and concentrates on the social system and on the interrelationship between science and society. Neither of the two approaches can claim to cover the whole truth and to give the only possible (causal) explanation, The cognitive content of scientific theories and the social process of bringing about and using them are by their very nature complementary.
Synthesis of (R)‐ and (S)‐amphetamine‐d3 from the corresponding phenylalanines
Authors: Gal Joseph
Published: October 2006

The synthesis of (R)‐(−)‐ and (S)‐(+)‐2‐amino‐1‐phenylpropane‐3,3,3‐d3 via a modification of a published procedure for the unlabelled compounds is described. The preparation of the (S)enantiomer involved in the first step the reduction of D‐phenyl‐alanine to (R)‐2‐amino‐3‐phenyl‐1‐propanol–1,1‐d2 with lithium aluminum deuteride. The reduction product was treated with p‐toluenesulfonyl chloride to give (R)‐3‐phenyl–2‐(4‐toluenesulfamoyl)propyl–1,1‐d2 4‐toluenesulfonate, which was reduced with lithium aluminum deuteride to (S)‐N‐(1‐methyl‐d3‐2‐phenethyl)‐4‐toluenesulfonamide. The latter compound was cleaved to (S)‐(+)‐2‐amino‐1‐phenylpropane‐3,3,3‐d3 using naphthalene anion radical. The overall yield in the sequence was 32.8%, the isotopic purity of the product was 99%, and the enantiomeric purity > 99%. The methyl ester of the amino acid could also be used as starting material in the synthesis.
Nouvelle methode de synthese des principaux metabolites des catecholamines marques au carbone 14
Authors: Pichat Louis , Tostain Jean
Published: October 2006

Methylsulfinylcarbanion used in large excess reacts with methyl (carboxyl 14C) vanillate 2 a, methyl (carboxyl 14C) isovanillate 2 b and methyl 3,4 dibenzyloxy (carboxyl 14C) benzoate 2 d to give 90 % yields of β‐ketosulfoxides 3 a, 3 b, 3 d. Submitted to the acid catalyzed Pummerer rearrangement these β‐ketosulfoxides lead to the formation of methyl hemimercaptals of phenylglyoxals 4 a, 4 b, 4 d in good yields. These β‐keto‐α‐hydroxy sulfides react with sodium hydroxide to give respectively : 2–(4–hydroxy‐3‐methoxyphenyl)‐2‐hydroxy (2–14C) acetic acid 5 a (V.M.A.); 2–(3‐hydroxy‐4‐methoxyphenyl)‐2‐hydroxy (2–14C) acetic acid 5 b (iso V.M.A.) in overall yields of 55 % based on vanillic and iso‐vanillic acids; and 2–(3,4 dibenzyloxyphényl)‐2 hydroxy (2–14C) acetic acid 5 d, hydrogenolysis of which gave 2–(3,4 dihydroxyphenyl)‐2‐hydroxy (2–14C) acetic acid (D.H.M.A.) in 61 % overall yield from 3,4 dihydroxy benzoic acid. The β‐keto‐α‐hydroxysulfides 4 a, 4 b, 4 d reduced with sodium borohydride give respectively 2‐(4‐hydroxy‐3‐methoxyphenyl) (2–14C) ethyleneglycol (H.M.P.G.) 6 a; 2–(3‐hydroxy‐4‐methoxyphenyl) (2–14C) ethyleneglycol 6 b (iso H.M.P.G.) in overall yields of 64 % and 60 % based on vanillic and isovanillic acids; and glycol 6 d the hydrogenolysis of which gave 2–(3,4‐dihydroxyphenyl) (2–14C) ethyleneglycol 6 c (D.H.P.G.) in yield of 64 % based on 3,4 dihydroxybenzoic acid.
A convenient synthesis of deuterium labelled diphenylhydantoin
Authors: Casey D. L. , Gwilt P. R. , Digenis G. A. , Perrier D. G.
Published: October 2006

A simple, inexpensive method for the synthesis of deuterated diphenylhydantoin is described. Ten deuterium atoms are introduced to the 5,5‐diphenyl moiety of the diphenylhydantoin molecule.
A study of chemical carcinogenesis 4. Synthesis of the carbon‐14 labelled carcinogens 5‐methylchrysene, 2‐methyl‐aniline and 3‐methyl‐2‐naphthylamine
Authors: Weiss Louis , Loy Myrna , Hecht Stephen S. , Hoffmann Dietrich
Published: October 2006

Procedures were developed for synthesis of the carcinogenic compounds 5‐methylchrysene‐5‐14C, 2‐methylaniline‐methyl‐14C and 3‐methyl‐2‐naphthyl‐amine‐methyl‐14C. In each case, label was introduced with 14CO2 and yields were acceptable for preparation of these compounds for metabolic studies.
Preparation of carbon‐13 C disulfide and carbon‐13C oxysulfide
Authors: Kerr Vernon N. , Ott Donald G.
Published: October 2006

Carbon‐13C disulfide was synthesized from methane‐13C with hydrogen sulfide in a heated quartz chamber. Carbon‐13C oxysulfide was made from carbon‐13C monoxide with elemental sulfur heated in the presence of sodium methylate.
11C‐labeled octanal and benzaldehyde
Authors: Tang D. Y. , Lipman A. , Meyer G.‐J. , Wan C‐N. , Wolf A. P.
Published: October 2006

The synthesis of octanal and benzaldehyde, labeled with 11C in the carbonyl position, is reported. Octanal was prepared via an insertion reaction of 11CO into the boroncarbon bond of B‐heptyl‐9‐BBN, followed by oxidative hydrolysis. Benzaldehyde was synthesized by the reaction of phenyl magnesium bromide with 11CO2, and subsequent reduction of the labeled benzoic acid to benzylalcohol which was then oxidized to the final product by CrO2Cl2. Both aldehydes were purified via GLPC, leading to radiochemical purities of > 99.5% in each case. The radiochemical yield for octanal and benzaldehyde was 30 ± 5% and 15 ± 5%, respectively. The overall synthesis time was 50 ± 10 min for each compound.
The synthesis of deuterium, tritium and carbon‐14 labelled nicotinanilides
Authors: Ayrey G. , Dunlop R. W. , Duncan J.
Published: October 2006

The preparations of nicotin[2′,4′,6,‐2H3]anilide, 4′‐Cl‐nicotin[2′,6′‐2H2]anilide, 4′‐X‐nicotin[ar‐3H]anilide, (X = H−, CH3‐, Cl‐ or No2‐) and[6‐14C]nicotin[ar‐3H]anilide are described.
Synthesis of six specifically deuterted indoles of biological interest
Authors: Hesselgren Torbjörn , Beck Olof
Published: October 2006

Procedures for the preparation of N‐methyl‐(α,α,ß,ß‐2H4)tryptamine, 5‐methoxy‐N‐methyl‐(α,α,ß,ß‐2H4)tryptamine, 5‐hydroxy‐N‐methYl‐(α,α,ß,ß‐2H4)tryptamine, (α,α,ß,ß‐2H4)tryptophol, 5‐methoxy‐(α,α,ß,ß‐2H4)tryptophol and 5‐hydroxy‐(α,α,ß,ß‐2H4)tryptophol are described. Deuterium was introduced by treatment with lithium aluminium deuteride of the appropriate indole‐3‐(N‐methylglyoxylamide) or ethyl indole‐3‐glyoxalate. The isotopic purity of the products was greater than 97.3%.
Preparation of [7,7‐2H2] lithocholic acid
Authors: Phillipou G. , Seaborn C. J. , Butler R. N.
Published: October 2006

Electrochemical deoxygenation of methyl 7‐keto‐lithocholate using deuterated reagents, followed by base hydrolysis is shown to give [7,7‐2H2] lithocholic acid in 60% overall yield and 86% 2H2 isotopic purity.
A synthesis of porphobilinogen‐11‐13C
Authors: Buldain Graciela , Valasinas Aldonia
Published: October 2006

Porphobilinogen‐11‐13C was prepared by using benzyl 3‐(β‐methoxycarbonylethyl)‐4‐ (methoxycarbonylmethyl)‐2‐pyrrolecarboxylate as a starting material. A Vilsmeier‐Haak formylation with N,N′‐dimethylform‐13C‐amide gave the 2‐formylpyrrole, which was transformed into its oxime, and the latter was hydrogenated to the hydrochioride of 5‐carboxyporphobilinogen dimethyl ester. The hydrochloride cyclized to 5‐carboxyporphobilinogen lactam at pH 9, and the latter was first decarboxylated and then saponified to give the title compound.
Synthesis of 3‐methyl‐15‐(p‐iodophenyl)‐pentadecanoic acid labelled with carbon‐14
Authors: Humbert T. , Luu‐Duc C. , Le Bars D. , Marsura A.
Published: October 2006

Methyl‐(p‐iodophenyl)‐pentadecanoic acid 4 labelled with carbon‐14 in the carboxyl group was obtained in 38% radiochemical yield in five steps from Na 14CN at a specific radioactivity of 0.084 mCi/mg, 38.6 mCi/mmol.
Improved conventional synthesis for 14C‐labeled polyglutamates of folic acid
Authors: Ferenz Catherine R. , Graham David Y.
Published: October 2006

The majority of folates existing in nature are of the pteroylpolyglutamyl form and are unable to support Lactobacillus casei growth until the δ‐linked glutamyls are digested by conjugase enzymes. Most studies involving folate absorption have utilized monoglutamyl forms of folate, primarily folic acid. Synthetic pteroylpolyglutamates prepared by solid phase or conventional synthesis provided conjugated materials with which to study the absorption and metabolism of natural derivatives; however, the synthetic hepataglutamates support microbiological growth prior to enzymatic hydrolysis where as the natural conjugates do not. Incomplete purification of intermediate peptides during the synthesis would be the most likely explanation of this growth phenomenon. A modified solution synthesis has been developed which improves upon intermediate peptide condensations, increases product yields, and provides a heptapeptide which does not support microbiological growth until after enzymatic hydrolysis.
Synthesis of deuterated β‐carotene
Authors: Bergen H. Robert , Olson James A.
Published: October 2006

The synthesis of 10,10′,19,19,19,19′,19′,19′‐2H8‐β‐carotene is described. The double condensation (C15+C10+C15=C40) of the Wittig salt of 9,9,9,10‐2H4‐β‐ionylidene ethanol with the symmetrical C10 dial 2,7‐dimethyl‐2,4,6‐octatrienedial led directly to 2H8‐β‐carotene. The symmetrical labelling pattern of this deuterated β‐carotene will function as a tracer for the study of β‐carotene metabolism in humans.
Synthesis of D3‐sulpiride and its (R) and (S) isomers
Authors: Al‐koutayni‐rifai M. , Jamet G. , Kerr R. R. , Jung L. , Koffel J. C.
Published: October 2006

Racemic d3‐sulpiride, (R)‐(+)‐d3‐sulpiride and (S)‐(−)‐d3‐sulpiride (with three deuterium atoms in the methoxy function ortho to the benzamide), as well as (R)‐(+)‐sulpiride and (S)(−)‐sulpiride were synthesized. The structures were characterized by melting points, IR, 1H‐NMR, GC‐MS and polarimetry. The measured [α]D20 was 65° in 5% DMF.
Investigation on solvent hydrogen transfer during the catalytic deuteration of N‐acetyl‐3,5‐di‐iodo‐L‐tyrosineamide
Authors: Oehlke J. , Niedrich H. , Zöpfl H.‐J. , Franke P.
Published: October 2006

During the catalytic dehalodeuteration of N‐acetyl‐3,5‐di‐iodo‐L‐tyrosine amide solvent hydrogen was incorporated instead of deuterium up to an order of 70%. The major part of the solvent hydrogen was shown to be introduced into the reaction product independently of the dilution of the reacting gas. This direct transfer depends on type of solvent and catalyst and on the catalyst‐to‐substrate ratio in the same manner as found from deuterations of 4‐halogenated phenylalanine derivatives and dehydroproline. The distribution of deuterium in the reaction products was determined by mass spectrometry.
Deuteraction of DL‐4‐hydroxyphenyllactic acid
Authors: Ten Brink H. J. , Jakobs C.
Published: October 2006

The preparation of [D2]‐labelled DL‐4‐hydroxyphenyllactic acid by acid catalyzed hydrogen exchange at the aromatic ring is reported. Spectrometric analysis of the product shows that the deuteration is regiospecific and quantitative, which makes the deuterated compound suitable as an internal standard in the stable isotope dilution analysis of its naturally occurring analog in biological samples.
Solid phase reduction of 99mTcO with zinc : A method for the preparation of difficult 99m complexes
Authors: Kremer C. , León A. , Gambino D. , Cartesio S. , Ures C. , Savio E. , Campos E. , Kremer E.
Published: October 2006

Two groups of compounds: aminoacids (glutamic acid, glutamine, glycine, lysine) and amines (ethylenediamine, diethylenetriamine, o–phenantroline, o–phenylenediamine) have been labelled with 99mTc by means of a solid phase reduction using fine powdered zinc as reducing agent. In all cases radiochemical purity in excess of 90% was obtained, with no evidence of colloid formation. Labelling yields were variable depending on the ligand used. The results show that the method presented allows to label with 99mTc some molecules for which the use of conventional techniques is not feasible.
Synthesis of 2,5,8‐trimethyl‐3,4‐dihydro‐1(2H)‐naphthalenone‐2‐d and 3,5,8‐trimethyl‐3,4‐dihydro‐1(2H)‐naphthalenone‐2,2‐d2
Authors: Eisenbraun E. J. , Dewprashad B. , Geno P. W. , Taylor A. R.
Published: October 2006

The synthesis of specifically labeled 2,5,8‐trimethyl‐3,4‐dihydro‐1(2H)‐naphthalenone‐2‐d and 3,5,8‐trimethyl‐3,4‐dihydro‐1(2H)‐naphthalenone‐2,2‐d2 through α‐proton exchange using neat trifluoroacetic acid‐d is described.
An efficient, high specific activity radioiodination of 5‐(1‐hydroxy/methoxy‐2‐iodoethyl)‐2′‐deoxyuridine by isotope exchange labelling in pivalic acid melt
Authors: Iwashina Takashi , Kumar Rakesh , Knaus Edward E. , Wiebe Leonard I.
Published: October 2006

Radioiodinated 5‐(1‐hydroxy‐2‐iodoethyl)‐2′‐deoxyuridine (1a) and 5‐(1‐methoxy‐2‐iodoethyl)‐2′‐deoxyuridine (2a) were prepared from the corresponding unlabelled nucleosides (1 and 2) by isotope exchange in a pivalic acid melt. Compound 1a was obtained in 71.3% to 26.3% radiochemical yield with a specific activity range of 77 to 2486 GBq/mmol, and 2a was prepared in 70.3% radiochemical yield at a specific activity of 100.6 GBq/mmol. Low temperatures and the mild reaction conditions encountered in the pivalic acid melt method, which reduce the extent of nucleoside decomposition, were essential for successful exchange radioiodination. Even under optimal conditions (70°C; 100 min), the order in which the reagents were mixed was critical to obtain high radiochemical yields and to minimize chemical decomposition of the nucleosides.
Synthesis of [2H]‐diethoxymethane as a convenient source of a [2H]‐methylene unit
Authors: Hanley John A. , Forsyth David A.
Published: October 2006

[2H]‐Diethoxymethane is prepared in one step from triethylorthoformate. Its usefulness as a precursor to [2H]‐formaldehyde is shown by the Diels Alder synthesis of a monolabelled bicyclic amine. The title compound should also be useful in the syntheses of other labelled compounds in which [2H]‐formaldehyde is a required reagent.
Enzymatic synthesis of [11C]N‐acetylserotonin
Authors: Mannens Geert , Slegers Guido , Goethals Patrick
Published: October 2006

An enzymatic synthesis of [11C] N‐acetylserotonin is described. [1‐11C] acetate is produced by reacting 11CO2 with methylmagnesium bromide and converted to [11C]acetylCoA by passage over a first enzyme reactor containing immobilized acetylcoenzyme A synthetase. The produced [11C]‐acetylCoA is converted to [11C]N‐acetylserotonin with a second enzyme reactor containing immobilized acetylcoenzyme A: arylamine N‐acetyltransferase. The labelled end product is purified by means of ionexchange chromatography and is obtained in a solution suitable for intravenous injection.

After irradiation with 18 MeV protons at 15 μA for 20 min, 25 mCi with a specific activity of 250 mCi/μmol were obtained. The whole synthesis starting from EOB takes 40 min.