The molecular structure of the benzilic acid rearrangement product of 3α, 17β-diacetoxy-11-hydroxy-12-oxo-5β-androst-9(11)-ene

Zusammenfassung Die Struktur desp-Brombenzoates des Benzilsäureumlagerungsproduktes von 3, 17-Diacetoxy-11-hydroxy-12-oxo-5-9(11)-androsten wurde durch dreidimensionale Röntgenstrukturanalyse eines Einkristalls als 3-p-Brombenzoat des 11-Carboxy-3, 11, 17-trihydroxy-13-C-nor-5-androstan 11a, 17-Laktons erkannt.     

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 .     

A postsynaptic α, 2-receptor: The alpha-adrenergic receptor of hamster white fat cells

Summary The effects of selected -agonists and -antagonists on theophylline-induced lipolysis were investigate in isolated hamster white fat cells ₂-Agonists (tramazoline, clonidine) inhibited theophylline-induced lipolysis while an ₂-agonist (methoxamine) was without any effect. The inhibitory effect of ₂-agonists was suppressed by yohimbine (₂-antagonist), whereas ₂-antagonists were inefficient. This result implies that the -adrenergic receptor of hamster fat cells is of the ₂-type, although located postsynaptically.Acknowledgments. This work was supported by grants from CNRS (ERA 412) and DGRST (grant No. 787 1078). We thank M. Dauzats for excellent technical assistance. We thank Prof. H. Schmitt for tramazoline and AR-C 239 and for helpful discussion.     

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.     

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).     

Axillary 5α-androst-16-en-3-one in men and women: Relationships with olfactory acuity to odorous 16-androstenes

Summary Axillary 5-androst-16-en-3-one (5-androstenone) levels were found to be significantly higher in men than in women but do not vary between left and right axillae, are not related to age, handedness or degree of hirsutism (in women) nor to anosmia to this steroid. In men (but not in women), levels are related linearly to axillary cholesterol concentrations but not to squalene. Olfactory thresholds for 5-androstenone varied widely, the lowest recorded being 0.2 ppb, but there was no difference in thresholds between men and women. Women (70%) found the smell repellant but anosmia did not differ greatly between men and women (9–20%). Anosmia to the smell of 5-androst-16-en-3-ol was most marked in women (90%) rather than in men (45%). Axillary 5-androstenone values were generally consistent with the musky or strong smells of male axillary extracts, compared with the sweet smell of those from female subjects.Supported by the Herbert Dunhill Trust.     

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.     

Age- and sex-related differences in the content of prothymosinα in rat tissues

Differences in the tissue content of prothymosin during the early postnatal development of male and female rats are reported. Thymus and spleen have been found to contain significantly higher amounts of prothymosin in the newborn and prepubertal animals, as compared to adults, whereas liver has been found to contain low levels of prothymosin throughout development. These findings indicate a functional association of prothymosin with the proliferating lymphoid tissues of the young rat.     

Responses of resistance and capacitance vessels at various frequency electrical stimulation of sympathetic nerves

Conclusion (1) The maximal reactions of cerebral resistance vessels arise at the stimulation frequency of 30 cps, the maximal reactions of capacitance vessels at the frequency of 10 cps. (2) Reactions of resistance vessels in the pulmonary lobe increase in the range of stimulation frequencies from 11–50 cps, maximal reactions of pulmonary capacitance vessels are observed at the frequency of 30–40 cps. (3) Reactions of resistance vessels situated below the abdominal aorta bifurcation increase progressively in the range of frequencies from 6–50 cps, the magnitude of capacitance vessel reaction reaching its maximum value at 20 cps.

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30 /, — 10 /. 50 /. 30–40 /, 20 /.

     

An epoxidation byCorynebacterium simplex

Zusammenfassung Während unserer Untersuchungen über die mikrobiologische Dehydrierung verschiedener 16-Methylsteroide durch Bakterienkulturen vonCorynebacterium simplex, wurde eine neue Art von Umwandlung beobachtet. Von 16-Methyl-9(11)-pregnen-17, 21-diol-3, 20-dion-21-acetat ausgehend, gelang es aus den Kulturfiltraten 16-Methyl-1, 4-pregnadien-9, 11-epoxy-17, 21-diol-3, 20-dion zu isolieren. In einigen Fällen wurde auch das4-Derivat dieser Verbindung als Nebenprodukt erhalten.     

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 oxidative metabolism ofα-chlorohydrin and the chemical induction of spermatocoeles

Summary -Chlorohydrin (I) is oxidatively metabolized to -chlorolactic acid (III) and oxalic acid (IV). Deposition of calcium oxalate within the renal tubules is responsible for the toxic effects of-chlorohydrin and a similar action on the epididymis or epididymal blood vessels could initiate the formation of spermatocoeles from this and other male antifertility agents.     

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.     

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.     

Distribution of C19-steroid conjugates in plasma protein fractions

Zusammenfassung Nach. i.v. Gabe von 7-³H-Dehydroepiandrosteron wurde menschliches Plasma einer präparativen Zonenelektrophorese unterworfen und in Albumine, ₁-, ₂-,- und-Globuline zerlegt. Aus den einzelnen Proteinfraktionen trennte man freie Steroide, Steroid-Sulfokonjugate und -Glukuronoside ab und untersuchte letztere Fraktionen auf ihren Gehalt an markierten C₁₉-Steroiden. Es zeigte sich, dass die Steroid-Sulfokonjugate vornehmlich in der Proteinfraktion der Albumine, die Steroid-Glukuronoside dagegen bevorzugt in der Proteinfraktion der ₁-Globuline auftraten.     

Eubotriol and eubol,new diterpenes fromSideritis euboea

Summary 2 new diterpenes Eubotriol (ent-kaur-16-ene-7, 15, 18triol) (I), and eubol (ent-kaur-16-ene-7-acetoxy-15, 18 diol) (II) have been isolated from Sideritis euboea Helder.This work was supported by National Research Council (C.N.R.), Roma.     

Identification of 3α, 17α, 21-trihydroxy-5α-pregnane (allotetrahydro-17α-hydroxy-cortexone) and 3α,21-dihydroxy-5α-pregnane (allo-tetrahydro-cortexone) in human urine

Résumé Le 3, 17, 21-trihydroxy 5-pregnane (allo-tétrahydro-17-hydroxy-cortexone) et le 3,21-dihydroxy 5-prégane (allo-tétrahydro-cortexone) ont été identifiés dans l'urine humaine. Ces composés avaient les mêmes migrations chromatographiques avant ou après acétylation ou oxydation que les respectifs stéroïdes de synthèse.     

X-ray research for polycrystals. The formation geometry of instrumental width of the diffractional line at the investigation of the polycrystals in the translucent X-rays

: , , , - , ().     

Tumor necrosis factor-α inhibits collagen synthesis in human and rat granulation tissue fibroblasts

The purpose of the study was to examine the effects of tumor necrosis factor- (TNF-) on collagen gene expression in rat and human granulation tissue fibroblast cultures. The cells were exposed to 0.1, 1, 10, or 100 ng/ml of TNF-, and the rate of collagen synthesis was measured as synthesis of protein-bound³H-hydroxyproline. Total cellular RNA was isolated from fibroblasts, and measurements of specific cellular RNAs from fibroblasts were performed by Northern blot hybridizations using³²P-labeled cDNA probes. In cultures of rat granulation tissue fibroblasts TNF- decreased³H-hydroxyproline production to about 75% of that in controls and it also decreased pro1(I) and pro1(III) collagen mRNA levels, maximally to 33% and 23% of the control levels, respectively. In cultures of human granulation tissue fibroblasts a similar inhibiting effect in the production of collagen was seen. TNF- decreased the production of³H-hydroxyproline to 56% of the control value with a dose of 100 ng/ml also having an inhibiting effect on pro1(I) collagen mRNA levels of up to 43% of the control level. However, no effect was seen on pro1(III) collagen mRNA levels.