Polyribosome patterns in EMC-virus infected Krebs-2 cells and cell extracts

. -2, , . ¹⁴- in vitro ( ) , in vivo, . .     

Effects of ibotenic acid,quisqualic acid and their relatives on the excitability of an identifiable giant neurone of an African giant snail (Achatina fulica Férussac)

Summary An identifiable giant neurone, PON (periodically oscillating neurone), of Achatina fulica Férussac, inhibited by erythro--hydroxy-L-glutamic acid, was also inhibited by 2 relatives of -hydroxy glutamic acid, ibotenic acid and quisqualic acid. These substances similarly showed the effect on the neurone even in the chloride-free medium.The authors wish to thank Professor Emeritus T. Takemoto of Tohoku University, Dr H. Iwasaki of Takeda Chemical Co. and Professor C. H. Eugster of Zurich University for the donation of precious substances, and Miss H. Tamura for technical assistance.     

α-andβ-activity of O-methylated derivatives of norepinephrine and epinephrine

Summary Metanephrine, iso-metanephrine, normetanephrine and isonormetanephrine were tested for - and -activity on various tissues obtained from rats, guinea-pigs and cats. It was found that methylation of the hydroxyl groups of norepinephrine or epinephrine in either the 3-or 4-position markedly reduces or abolishes -and -activity with the exception of the nictitating membrane of the cat. This receptor seems to show a tissue difference.Acknowledgment. W. H. V. would like to thank the Federal Republik of Germany for the U. S. Senior Scientist Award which enabled him to work at the Department of Pharmacology, University of Mainz, and to conduct part of this work. W. H. V. would also like to thank Prof. Dr E. Muscholl, Mainz, for his hospitality, help and advice during this stay.     

Quantitative changes in β-adrenergic responses of isolated atria from hyper- and hypothyroid rats

Summary Concentration-response curves for the chronotropic and inotropic effects of isoprenaline, in the absence and presence of propranolol, were obtained on heart atria isolated from normo- or dysthyroid rats. Hyperthyroidism increased the chronotropic potency and efficacy of the -adrenergic agonist. The results are compatible with the view that thyroid hormone increases the density of functional -adrenoceptors in cardiac pacemaker tissue.This study was supported by the Swiss National Science Foundation grant No. 3.374.-0.78. We thank Dr Bachmann from the Central Laboratory of the University Hospital Bern for the estimation of plasma thyroxine levels.     

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     

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.     

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.     

Pregnancy specificβ 1 — a product of the syncytiotrophoblast

Summary Pregnancy specific ₁ (PSG) has been identified in vitro in trophoblast cultures and in vivo, using transmission electron microscopy, in the syncytiotrophoblast, PSG may, like other pregnancy proteins, have immunosuppressive properties.This study was supported by a grant from the Medical Research Council. We thank Dr.D. R. Abramovich for making available the first trimester placentae and MissWanda Emslie for help in the tissue culture studies.     

Defensive steroids from a carrion beetle (Silpha americana)

Summary The defensive anal effluent discharged bySilpha americana in response to disturbance contains a mixture of steroids stemming from a glandular annex of the rectum. The compounds have been characterized as 15-hydroxyprogesterone (1, principal component), 5-pregnan-15-ol-3, 20-dione (2), 5-pregnan-3, 15-diol-20-one (3), 5-pregnan-7, 15-diol-3,20-dione (4), 5-pregnan-3, 7, 15-triol-20-one (5), 5-pregnan-16-ol-3,20-dione (6), and 5-pregnan-3, 16-diol-20-one (7), none previously found in insects. Bioassays with jumping spiders showed compounds1 and6 to be feeding deterrents at the 1 g level.Paper No. 78 of the series: Defense Mechanisms of Arthropods. Study supported by NIH (Grants AI-02908, AI-12020). We thank Maura Malarcher and Maria Eisner for excellent technical help, and the Squibb Institute of Medical Research for samples of authentic reference compounds.     

Dopamine-β-hydroxylase activity in stroke-prone spontaneously hypertensive rats

Summary Dopamine--hydroxylase (DBH) activity was higher in the serum, the mesenteric artery and the cerebral cortex of 4-week-old stroke-prone spontaneously hypertensive rats (SHRSP), and lower in the nucleus tractus solitarii than it was in spontaneously hypertensive rats (SHR).The authors wish to thank Prof. Masao Sano (Nagoya University) for his aid in dissecting the nucleus tractus solitarii and the locus coeruleus.     

7α-hydroxylation of dehydroepiandrosterone in human testis and epididymis in vitro

Zusammenfassung Zerhackte menschliche Hoden und Epididymis wurden mit Dehydroepiandrosteron ohne Kofaktoren bebrütet und es wurden unter anderem 7-und 7-Hydroxydehydroepiandrosteron und 5-Androsten-3, 7, 17-triol charakterisiert. Die Ausbeute an 7-hydroxylierten Metaboliten war fast gleich in Hoden und Epididymis.

---

---

The authors wish to thank Mr.J. Novák for his excellent technical assistance. We are indebted to Dr.J. E. Jirásek for generous performance of histological control of tissue and to Dr.S. Röhling for his kind pernission of radioactivity measurements.     

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.     

A method for the isolation of ommochrome-containing granules from insect eyes

Summary A routine method for the preparation of pigment granules from insect eyes is reported. When viewed using an electron microscope, the isolated granules appear to be free from different structural elements, and there is very little contamination by membranous material. Ultrastructure and extinction spectra correspond to those found in situ.Acknowledgments. We thank Prof. Dr A. Fischer and Dr J. Rosenberg for their help in electron microscopic techniques. This work was supported by the Deutsche Forschungsgemeinschaft.     

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.     

Nerve growth factor selectively stimulates the degradation of chondromucoprotein in the embryonic cartilage in vitro

Summary Nerve growth factor specifically stimulates the degradation of chondromucoprotein in the chick embryonic cartilage cultivated in vitro, with little effect on chondromucoprotein, RNA, DNA and protein synthesis.Acknowledgment. I thank Dr Hiroshi Saito and Dr Yutaka Kasuya (University of Tokyo) for the generous gift of male mouse NGF.     

Evaluation of monoaminergic receptors in the genetically epilepsy prone rat

Summary The intensity of sound-induced convulsions in the genetically epilepsy-prone rat (GEPR) was reduced in a dose related fashion by intracerebroventricular administration of dobutamine, (₁ agonist), terbutaline (₂ agonist) or phenylephrine (₁ agonist). BHT-920 (₂ agonist) did not cause a dose-related decrease in sound-induced convulsion intensity. Binding studies showed that whole brain and receptor densities (B_max) were normal while the K_d was increased for the ligand in GEPR brain.Acknowledgment. We are most grateful to Boehringer Ingelheim for generously supplying BHT 920. We are also indebted to Ciba-Geigy Corporation for the gift of terbutaline hydrochloride and phentolamine hydrochloride. The work was supported in part by NIH grant NS 16829.     

Comparative analysis of human milk and human blood plasma by means of diffusion-in-gel methods

Zusammenfassung Mit Hilfe von Immunoelektrophorese und Doppeldiffusiontechnik wurden in Humanmilch an Blutplasmaproteinen serologisch identifiziert: Praealbumin, Albumin, Acid Seromucoid, ₁-Glykoprotein (3·5 S), Coeruloplasmin, Haptoglobin, ₂- oder-Lipoprotein, Transferrin, Fibrinogen, _2A-Globulin, _2M-Globulin und-Globulin.     

Hormonal rupture of larval diapause in the tickRhipicephalus sanguineus (Lat.)

Zusammenfassung Die Diapause von Larven der ZeckeRhipicephalus sanguineus (Lat.) wird durch- and-Ecdyson beendet.

---

---

We would like to thank Dr.J. B. Siddal for generously providing-ecdysone, Dr.T. Takemoto for-ecdysone and Dr.N. Krishnan for the juvenile hormone analogue,trans, trans-10, 11-epoxy faresenic acid methyl ester.     

Digestive enzymes in the gut and salivary gland of the larvae ofChilo auricilius Ddgn.

Summary Amylase, - and -glucosidase, - and -galactosidase, -fructosidase, trypsin, aminotripeptidase, leucine-aminopeptidase, prolinase, prolidase glycyl-L-leucine dipeptidase and glycylglycine dipeptidase are present in the 3rd instar larvae ofChilo auricilius.Dr Kishan Singh, Indian Institute of Sugarcane Research, Lucknow, is gratefully acknowledged for providing necessary facilities.     

The synthesis of ecdysone

Zusammenfassung Ecdyson, ein Häutungshormon der Insekten, wurde ausgehend von Ergosterin in 14 Stufen synthetisiert. Wesentliche Zwischenprodukte waren (20S)-2, 3-Diacetoxy-20-formyl-5-pregn-7-en-6-on und (22R)-2, 3-Diacetoxy-14, 22-dihydroxy-25-(tetrahydropyran-2-yloxy)-5-cholest-7-en-6-on.