Unterschiedliche Empfindlichkeit verschiedener Angiotensinderivate gegen Abbau durch Plasma oder Nierenhomogenat

Summary -Asp¹-Angiotensin II had a more pronounced action on the blood pressure of nephrectomized rats than the corresponding-compound.-Asp¹-Angiotensins were more slowly destroyed by rat serum, rat kidney homogenate, and human plasma than-compounds, especially-Asp¹-Angiotensin II amide.     

Exchange of tritium from randomly tritiated taurocholate by microbial bile salt oxidoreductases

Summary Tritium distribution on randomly labelled taurocholate (TC) was estimated at 28%, 4%, 1% and <0.5% on the hydrogens opposite the 3-, 7- and 12-OH groups and taurine moiety respectively. Anomalously,C. perfringens 3-hydroxysteroid dehydrogenase (3-HSDH) catalyzed tritium loss of 36% on formation of 7-, 12-dihydroxy-3-keto-5-cholanoate, implying additional losses of tritium at other sites by this enzyme.This work is supported by the National Cancer Institute.     

The synthesis of corticosteroids methylated at C21

Zusammenfassung Die Darstellung der beiden epimeren C₂₁-Methylderivate des 9-Fluorprednisolons wird beschrieben. 9-Fluor-21-methyl-1, 4-pregnadien-11, 17, 21B-triol-3, 20-dion-21-azetat ist ein hochwirksames entzündungshemmendes Steroid, vollkommen frei von Nebenwirkungen der Natrium- und Wasserretention des C₂₁-unsubstituierten 9-Fluorprednisolons.     

Précipitation de fractions protéiques du sérum par la chlorpromazine

Summary In vitro, the mixture Chlorpromazine-human serum gives modifications of the lipoproteins and the-globulins. These modifications are studied by paper electrophoresis, Tiselius-electrophoresis, and immuno-electrophoresis. Under the experimental conditions described, the selective precipitation of the ₁-globulins seems quite unexpected.     

17β-Hydroxymethyl-Steroide: Darstellung von Derivaten des 17α-Hydroxy-17β-hydroxymethyl-4-androsten-3-ons

Summary Starting from 17-hydroxy-17-hydroxymethyl-4-androsten-3-one, we synthesized 4-chloro-17-hydroxy-17-hydroxymethyl-4-androsten-3-one-17, 20-acetonide and 17-hydroxy-17-hydroxymethyl-1, 4-androstadien-3-one. 11, 17-dihydroxy-17-hydroxymethyl-4-androsten-3-one was obtained from cortisone via methyl-17-hydroxy-3, 11-dioxo-4-etienate.     

Levels ofα 1 in the spring and autumn seasons

Summary In a group of 84 pairs of 11-year-old children of both sexes, the level of the ₁-antitrypsin ( ₁-AT) were ascertained in the autumn and spring. Although the mean levels of ₁-AT in the two seasons hardly differed, the highly significant seasonal changes in the distribution curves of ₁-AT values were noted in boys, whereas the levels showed higher stability in girls.     

Evidence for the extranuclear localization of thymosins in thymus

A new radioimmunoassay has been developed for thymosin ₄ by generating rabbit polyclonal antibodies against the synthetic N-terminal peptide fragment 1–15 coupled to KLH. The synthetic analogue [Tyr¹²]-thymosin ₄ (1–15) was used as tracer. This radioimmunoassay, with a useful range of 10–1000 pmoles, showed cross-reactivity with the second homologous -thymosin of man and rat (thymosin ₁₀) but not of calf (thymosin ₉). This radioimmunoassay, together with an improved radioimmunoassay for the N-terminus of parathymosin , was employed for the measurement of the levels of thymosin ₄ and parathymosin in nuclear and extranuclear extracts of calf thymus. The bulk of these polypeptides was found in the extranuclear material whereas only traces were observed in the nuclear environment, which indicates the extranuclear localisation of - and -thymosins.     

16-β-methylprednisone from hecogenin

Zusammenfassung Es wird über die Herstellung des 16-Methylprednisons berichtet, welche vom Hecogenin ausgehend über ca. 15 Stufen durchgeführt wird. Als wichtige Zwischenstufe treten 5-Pregn-16-en-3-ol-11, 20-dion-Acetat und 16-Methylen-5-pregnan-3, 17-diol-11, 20-dion auf: letzteres wird durch eine stereospezifische katalytische Reduktion in das entsprechende 16-Methyl-derivat umgewandelt.     

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.     

Hydrolysis of N-phenylacetyl-α-methyl-α-amino acids by benzylpenicillinacylase

Summary Enzymatic hydrolysis of several racemic N-phenylacetyl--methyl--amino acids containing an additinal aliphatic, aromatic or polar substitutent on the chiral carbon atom, has been studied by using benzylpenicillincylase fromEscherichia coli A.T.C.C. 9637. Both the rate of hydrolysis and the stereoselectivity were found to be considerably lower than in the case of natural -amino acids. Steric and electronic factors in the side chains influencing the stereoselectivity are discussed.     

Incorporation of α-aminobutyric acid into ergostine byClaviceps purpurea

Summary Claviceps purpurea 275 F.I. fed with -aminobutyric acid produces ergostine with the corresponding -hydroxy--aminoacid undiluted by endogenous aminoacid. Almost all the -aminobutyric acid not incorporated into the ergostine remains unchanged in the medium. The significance of these results in the biosynthesis of ergot alkaloids is discussed.     

Interdependence between locomotor activity and duration of wakefulness in humans during isolation

Summary Locomotor activity was recorded in 14 subjects who lived singly in an isolation unit for 16 to 88 days. Their free-running circadian rhythms had a mean period of 25.9 h, with individual means in the duration of wakefulness () ranging from 12.1 to 22.9 h. Intraindividually, the hourly means of activity were negatively correlated with to such a degree that the total amount of activity per day remained constant irrespective of large variations in .     

Synthese von 22,26-Imino-cholestan-Derivaten

Summary 3, 16-diacetoxy-5-pregnane-20-one and the analogue pregn-5-ene derivative have been converted into (22R, 25R)-22, 26-imino-5-cholestane-3, 16-diol. The configuration at C-22 and C-25 was determined by transformation into the known (22R, 25R)-5-solanidane-3-one. Application of the Ruschig method led to (25R)-22,26-imino-5-cholest-22(N)-ene-3, 16-diol.

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Solanum-Alkaloide. XVI. Mitteilung. — XV. Mitteilung:K. Schreiber undH. Ripperger, Tetrahedron Letters Nr.27, 9 (1960).     

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.     

Effects of injury on the concentration ofα 1 andα 2 in the plasmas of male and female rats

Summary The effects of injury on the concentration of ₁-macroglobulin and ₂-macroglobulin in the plasmas of male and female rats has been investigated. At 5 days after injury to the male rats the ₁-macroglobulin concentration increased to 131% of its preinjury value. The ₂-macroglobulin concentration increased more rapidly to a maximum of 86 times its initial value. In the female rats ₂-macroglobulin increased only slightly and ₁-macroglobulin not at all.     

Stimulation of gastric secretion by prostaglandin F2 α in rats

Summary In rats with chronic gastric fistulas, prostaglandin F₂ stimulated the gastric acid secretion in graded doses of 50. 100, 200 and 400 g/kg b. wt, while higher doses above 1 mg/kg b. wt tended to inhibit significantly. The gastric antisecretory effect of prostaglandin E₁ could not be altered or modified by subsequent treatment of prostaglandin F₂ , while the latter alone without any prior treatment of the former, stimulated output of gastric juice, HCl and pepsin without significantly affecting the concentration of these components.Acknowledgement. The gift of the prostaglandin E₁ and prostaglandin F₂ is acknowledged to Dr J.E. Pike, Upjohn, USA. This paper was read at the IXth Annual Conference of the Indian Pharmacological Society held at Benares (1976) and abstracted in the Indian J. Pharmac.9, 73 (1977).     

Conversion of 17α-hydroxypregnenolone to cortisol

Zusammenfassung Nebennierenschnitte von Ratten, Meerschweinchen und Menschen synthetisierten 17-Hydroxyprogesteron, 11-Deoxycortisol und Cortisol aus 17-Hydroxypregnenolon. Diese Verbindung, als Ausgangsprodukt für die Cortisolsynthese, ist ebenso wirksam wie pregnenolon. Die Umwandlung von 17-Hydroxypregnenolon in Dehydroepiandrosteron verläuft weniger vollkommen als zu 17-Hydroxycorticoiden.     

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.     

Antagonism of V2-receptor effect of antidiuretic hormone by atrial natriuretic peptide in man

Summary Human -atrial natriuretic peptide (h-ANP) makes the urine of dehydrated volunteers hypotonic to plasma despite high circulating concentrations of antidiuretic hormone. Urinary dilution with h-ANP also occurs in subjects receiving indomethacin. Therefore, h-ANP antagonises effects of antidiuretic hormone on distal tubular V₂-receptors in man, probably without involving prostaglandins.     

Deuterium isotope effects in the ninhydrin reaction of primary amines

Summary The rate of development of Ruhemann's purple in the ninhydrin reaction of two deuterated primary amines, -d₂-p-tyramine and -d₂--phenylethylamine, is significantly reduced It appears to be a primary isotope effect and indicates that the cleavage of the carbon-hydrogen bond at the -position is involved in the rate-determining step of the color reaction.Acknowledgements. We thank Dr A.A. Boulton for his advice and encouragement and the Canadian Medical Research Councel and Saskatchewan Health for their continuing financial support.