Fucosidases du suc digestif d'Helix pomatia

Summary The-d-fucosidase and -l-fucosidase activities of digestive juice ofHelix pomatia have been studied.-d-fucosidase can be separated from-d-galactosidase by heat inactivation.     

Uptake of D-glucose anomers by rat retina

Summary Uptake ofd-glucose anomers by isolated rat retina was studied. After 3 min incubation at 37°C in the presence of or anomer (750 g/ml), a significantly greater uptake (1.32 mg/g wet tissue) of -anomer was observed compared with that of -d-glucose (1.11 mg/g wet tissue). This result and other data suggest that the carrier ford-glucose transport in the retina prefers the -anomer stereospecifically.Acknowledgment. The authors are grateful to Mr S. Suzuki for his technical assistance.     

Ein neues Verfahren zur Herstellung von 19-Norsteroiden

Summary The new methods for the production of 19-norsteroids described involve the conversion of 5-halogen-6-hydroxy-steroids into the corresponding 5-halogen-6:19-ethers either with lead tetraacetate or by the hypoiodite reaction^8,10. The 6:19-oxygen bridge is then opened reductively either directly or after oxidation of the 6:19-ethers to lactones or preferably after introduction of a ^4,6-3-oxo grouping. Acylolytic cleavage of the ⁴-3-oxo-6:19-ethers followed by alkaline hydrolysis gives ^4,6-3-oxo-19-hydroxy-steroids. The 19-hydroxycompounds formed are easily converted into 19-norsteroids by known methods.

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Über Steroide, 189. (vorläufige) Mitteilung; 188. Mitt. vgl.J. Kalvoda, J. Schmidlin, G. Anner undA. Wettstein, Exper.18, 398 (1962).     

The motion of the moon in the Romaka Siddhānta

Summary Formulae are fitted to the different sets of values, given by the translators, for the equation of centre for the motion of the moon according to the Romaka Siddhnta, as found in the Pañcasiddhntik of Varha Mihira.     

On the structure of the natural dipeptide N-acetyl-aspartyl-glutamic acid (NAAGA)

Riassunto Si descrive la sintesi dei due dipeptidi isomeri acido N-acetil--l-aspartil-l-glutammico (I) e acido N-acetil--l-aspartil-l-glutammico (II). Il loro confronto con il NAAGA, dipeptide precedentemente isolato dal tessuto nervoso di alcuni mammiferi, ha dimostrato l'identità del nuovo metabolita con il-dipeptide (II).     

Metabolism in Porifera. IX. Studies on the biological conversion of cholesterol into 19-nor-cholestanol by the spongeAxinella polypoides

Summary The conversion of cholesterol into 19-nor-5-cholestan-3-ol by the spongeAxinella polypoides involves a partial loss (40%) of the 3-hydrogen atom; moreover administration to the sponge of [4-¹⁴C]cholesterol tritiated at C-4 and C-7 showed that the 4- and 7-hydrogen atoms are retained in this conversion. A competitive uptake experiment, [4-¹⁴C]cholesterol vs. [7-³H₂]5-cholestanol, showed that the sponge utilized exclusively cholesterol for the production of 19-nor-5-cholestan-3-ol.Part of this work has been presented at the Nato Conference on Marine Natural Products (Jersey, Great Britain, October, 1976).-This contribution is part of the Programma finalizzato Oceanografia e Fondi marini-sottoprogetto Risorse biologiche C.N.R. Italy.     

Use of the exo-β-(1→3) glucanase from basidiomycete QM 806 in studies on yeast

Résumé L'exo--(13) glucanasem isolée duBasidiomycete QM 806 a été utilisée avec succès pour l'analyse des polysaccharides de la paroi cellulaire de la levureSaccharomyces cerevisiae et pour la formation de protoplastes à partir deSaccharomyces cerevisiae etWickerhamia fluorescens.

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Acknowledgments. We are indepted to MissE. Sigarlakie and MissE. Wespi for technical assistance during the course of this investigation.     

Rotatory dispersion curves of some decalones of microbiological origin

Zusammenfassung Die Rotationsdispersionskurven einiger optisch aktiver Dekalonderivate sind gemessen worden. Ihre Amplituden (a) und die Amplitudenbeiträge (a) der Substituenten werden im Rahmen der Oktantenregel diskutiert.

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Paper V of the series Optical Rotatory Dispersion. For Paper IV seeC. Djerassi andW. Klyne, Proc. Nat. Acad. Sci. Washington, in press (1962).     

Antitumor effect of β-elemene in non-small-cell lung cancer cells is mediated via induction of cell cycle arrest and apoptotic cell death

-Elemene is a novel anticancer drug, which was extracted from the ginger plant. However, the mechanism of action of -elemene in non-small-cell lung cancer (NSCLC) remains unknown. Here we show that -elemene had differential inhibitory effects on cell growth between NSCLC cell lines and lung fibroblast and bronchial epithelial cell lines. In addition, -elemene was found to arrest NSCLC cells at G2-M phase, the arrest being accompanied by decreases in the levels of cyclin B1 and phospho-Cdc2 (Thr-161) and increases in the levels of p27^kip1 and phospho-Cdc2 (Tyr-15). Moreover, -elemene reduced the expression of Cdc25C, which dephosphorylates/activates Cdc2, but enhanced the expression of the checkpoint kinase, Chk2, which phosphorylates/ inactivates Cdc25C. These findings suggest that the effect of -elemene on G2-M arrest in NSCLC cells is mediated partly by a Chk2-dependent mechanism. We also demonstrate that -elemene triggered apoptosis in NSCLC cells. Our results clearly show that -elemene induced caspase-3, –7 and –9 activities, decreased Bcl-2 expression, caused cytochrome c release and increased the levels of cleaved caspase-9 and poly(ADP-ribose) polymerase in NSCLC cells. These data indicate that the effect of -elemene on lung cancer cell death may be through a mitochondrial release of the cytochrome c-mediated apoptotic pathway.Received 12 January 2005; accepted 5 February 2005     

Steroidal sapogenins. XXX stereochemistry of the side chain

Zusammenfassung Die optischen Drehungen einiger 20, 25d; 20, 25l; 20, 25d; und 20, 25-l-Sapogenine wurden bestimmt. Die ersten drei Serien gaben übereinstimmend linksdrehende Werte, aber die letztere Gruppe erwies sich als rechtsdrehend.Die Struktur der vier Serien der Sapogenine folgte aus der Analyse dieser Befunde. Der mögliche Mechanismus bei der Entstehung dieser Verbindungen aus Pseudosapogeninen wurde besprochen. Die Autoren gelangen zum Schluss, dass sterische Faktoren an C₂₀ und C₂₅ die Richtung der Ringschliessung beeinflussen.

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Steroidal sapogenins. XXX stereochemistry of the side chain

     

Caractérisation de laβ-galactosidase d'Helix pomatia par immunoélectrophorèse

Summary Digestive juice ofHelix pomatia was studied by immunoelectrophoresis: after incubation with a chromogenic substrate, 5-bromo-4-chloroindol-3-yl--D-galactopyranoside, two-galactosidases were revealed.     

Identification of a major cytokinin in coconut milk

A major cytokinin found in coconut milk was isolted by using the tobacco callus growth-promoting assay as a guide during purification. The structure of the factor was determined to be 14-O-{3-O-[-d-galactopyranosyl-(12)--d--galactopyranosyl-(13)--L-arabinofuranosyl]-4-O-(-L-arabinofuranosyl)--d-galactopyranosyl}-trans-zeatin riboside [G₃A₂-ZR] by various NMR techniques, including heteronuclear multiple bond connectivity by 2D multiple quantum NMR (HMBC), as well as mass spectroscopy and sugar analysis. The optimum concentration of G₃A₂-ZR for cytokinin activity in the tobacco callus assay was estimated to be 5×10^–6 M, so that G₃A₂-ZR is one order of magnitude more potent than 1,3-diphenylurea and one order less potent than zeatin riboside. At least 20% of the cytokinin activity of coconut milk could be attributed to G₃A₂-ZR.     

The formation of androgens in human foetal liver in vitro

Zusammenfassung Nach Inkubation des homogenisierten Lebergewebes menschlicher, 7–20 Wochen alter, Foeten mit 3-Hydroxy-5-androsten-17-on wird die Bildung von Testosteron, 4-Androsten-3, 17-dion und 5-Androsten-3, 17-diol nachgewiesen.     

11β-methyl-19-norsteroids: Novel progestational hormones

Zusammenfassung Die Synthese von 3, 17-Diacetoxy-17-Äthinyl-11-Methylestr-4-en (XII) wird beschrieben. Die Substanz besitzt besonders starke Antifertilitätseigenschaften, wie sie sonst nur Mischungen von Hormonen eigen sind, welche für die Humanfertilität benutzt werden, jedoch ohne deren Nebenwirkungen.     

Butyrate-induced reactivation of the fetal globin genes: A molecular treatment for theβ-hemoglobinophaties

The inherited -hemoglobinopathies (sickle cell disease and thalassemia) are the result of a mutation in the adult () globin gene. The fetal globin chain, encoded by the globin genes, can substitute for the mutated or defective globin chain, but expression of the globin gene is developmentally inactivated prior to birth. Reinducing expression of the normal fetal globin genes is a preferred method of ameliorating sickle cell disease and the thalassemias. Stimulation of as little as 4–8% fetal globin synthesis in the bone marrow can produce >20% fetal hemoglobin in the peripheral circulation, due to enhanced survival of red blood cells containing both sickle and fetal hemoglobin, compared to those containing sickle hemoglobin alone. Butyric acid and butyrate derivatives are generally safe compounds which induce fetal hemoglobin production by stimulating the promoter of the fetal globin genes. An initial trial with the parent compound, delivered as Arginine Butyrate, has demonstrated rapid stimulation of fetal globin expression to levels that have been shown to ameliorate these conditions. Phase 1 trials of an oral butyrate derivative with a long plasma half-life have just begun. These agents now provide a specific new apporach for ameliorating these classic molecular disorders and merit further investigation in larger patient populations.     

The characteristic specificity of plasmocytoma lipids concerning their resistance to formdl-fractions with colloidal dextran

Zusammenfassung Papierelektrophoretische Lipiduntersuchungen von- und-Plasmacytom — Paraproteinseren nach Kolloidaldextranbelastung erfassen eine neue, in der Diagnostik des Plasmocytoms verwertbare Eigenschaft: die Paraproteinlipidkomponente (PL) vermag, entgegen den-Lipoproteinen, mit Dextran keine Assoziationsfraktion zu bilden.

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My thanks are due toJosipa Franjkovi for her technical assistance.     

β-Pyrrolo-L-alanine,a new antimetabolite of phenylalanine and tyrosine inEscherichia coli

Zusammenfassung -Pyrrolo-l-alanin, dessen Synthese beschrieben ist, hemmt das Wachstum vonE. coli B auf synthetischen Nährböden. Die Hemmung wird vonl-Phenylalanin undl-Tyrosin vollständig, vonl-Tryptophan teilweise, nicht aber von Histidin aufgehoben. Stämme vonE. coli, die gegen-Pyrrolo-l-alanin bzw.p-Fluorophenyl-dl-alanin resistent sind, zeigen gekreuzte Resistenz.     

Gender- and site-related effects on lipolytic capacity of rat white adipose tissue

Gender- and site-related differences in the lipolytic capacity, at the different steps of the adrenergic pathway, in gonadal and inguinal white adipose tissue (WAT), were assessed by studying _2A-adrenergic receptor (AR), ₃-AR and hormone-sensitive lipase (HSL) protein levels, and by determining the lipolytic response to different agents. Gonadal WAT showed a lower _2A/₃-AR ratio, a greater lipolytic capacity in response to AR agonists, and higher HSL activity and protein levels than inguinal WAT. In female rats, we found greater _2A-AR protein levels and _2A/₃-AR ratio compared to their male counterparts, but, on the other hand, a higher lipolytic response to -AR agonists and a greater lipolytic capacity at the postreceptor level, including a more activated HSL protein. Thus, the lipolytic capacity was clearly higher in gonadal than in inguinal WAT, at the different steps of the adrenergic pathway studied. Moreover, in both tissues, females showed a greater inhibition of lipolysis via ₂-AR, which was counteracted by the higher lipolytic capacity at the postreceptor level.Received 1 April 2003; received after revision 11 June 2003; accepted 23 June 2003     

Neurohypophyseal origin of a humoral factor restoring volume natriuresis in acutely hypophysectomized rats

Zusammenfassung Es wird gezeigt, dass die Natriumund Wasserausscheidung hypophysektomierter Ratten durch ein Hypophysenhinterlappenextrakt korrigiert werden kann. Es handelt sich dabei nicht um ADH und das natriuretische Prinzip scheint auch vom Oxytozin verschieden zu sein.

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The present results and conclusions were discussed in detail by one of the authors (B. L.) in his Purkynje Lecture on Interaction of hormonal and non-hormonal mechanisms of the body fluids volume regulation at the XIXth Meeting of the Czechoslovak Physiological Society, held in Prague on January 26–28, 1972.

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Acknowledgments. We wish to thank Mrs.E. Blaková for her skilled technical assistance.     

Sequential appearance of α, β, and γ-crystallins in embryonic and metamorphicRana pipiens

Zusammenfassung Immunelektrophoretische und Immundiffusions-Studien zeigen, dass die Linse vonRana pipiens während der Entwicklung (Embryonal-Stadium 25 nachShumway) -und -kristalline Substanzen enthalten. Diese und frühere Ergebnisse¹⁰ sprechen dafür, dass beide Substanzen gleichzeitig auftreten, und beweisen, dass -kristalline Substanzen in diesem Entwicklungsstadium alleine im Linsenepithel vorkommen, während die Kristalline die am spätesten nachweisbaren linsenspezifischen Proteine (Taylor-Kollros-Metamorphosestadium VI) in der Linsenentwicklung vonR. pipiens sind.