Characterization of 17β-estradiol 3-(β-D-glucopyranoside) and 17-(α-D-glucopyranoside) as the metabolites of 17β-estradiol in the cultured ovaries of the silkworm,Bombyx mori

Summary The structures of the metabolites formed upon incubation of 17-estradiol with the ovaries of silkworm,Bombyx mori, have been determined as 17-estradiol 3-(-D-glucopyranoside) (1) and 17-(-D-glucopyranoside) (2) by spectroscopic means.     

A novel exocrine gland inside the thoracic appendages (‘gemmae’) of the queenless antDiacamma australe

Summary In the queenless antDiacamma australe, all workers eclose with a pair of tiny thoracic appendages (gemmae). These are sac-like and exhibit a distinct cuticular sculpturing, with minute pores opening on the outer surface. These pores are connected to glandular cells which completely fill the appendages, and thus an exocrine stignal is likely to be released. We discuss the social context of this signal: only one worker in each colony retains the gemmae.     

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.     

Dopamine-β-hydroxylase,adrenaline, noradrenaline and dopamine in the venous blood of adrenal gland of man: A comparison with levels in the periphery of the circulation

Summary In 10 human subjects plasma dopamine--hydroxylase activity was found in the adrenal vein blood to be as high as in the periphery of the circulation. Adrenaline concentration in the adrenal vein blood was in the mean 170 times, noradrenaline concentration 11 times and dopamine concentration little higher than levels in the periphery.This study was supported by the Deutsche Forschungsgemeinschaft.     

1-(3′-methoxy-4′-hydroxy benzyl) 6–7 dimethoxy isoquinoline,a major metabolite of papaverine

Zusammenfassung An Glukorons?ure gebundenes 1-(3′-Methoxy-4′-hydroxy-phenyl)-6, 7-dimethoxy-chinolin ist als Metabolit des Papaverins beim Menschen und bei S?ugetieren erkannt und isoliert worden. Ein in den Lebermikrosomen enthaltenes Ferment, dassauerstoff-und TPNH-abh?ngig ist, bewirkt die Methoxylspaltung, und ein weiteres Ferment übertr?gt die Glukurons?ure aus ihrer Verbindung mit Uridinphosphat auf die entstandene phenolische Verbindung.      

A simple synthesis of (E)-3-formylbut-2-enenitrile,and its use as a precursor of isotope-labelled zeatin and (±) dihydrozeatin

Summary (E)-3-Formylbut-2-enenitrile (4) is synthesized in 2 steps by reacting pyruvaldehyde dimethylacetal and acetonitrile in the presence of sodium methoxide, followed by acid hydrolysis to give 58% overall yield on distillation. The aldehyde4 can be stepwise and selectively reduced to (E)-3-hydroxymethylbut-2-enylamine (7a) in 37% total yield or exhaustivelyb reduced in 1 step to (±)-4-hydroxy-3-methylbutylamine (6) in 46% total yield. Compound7a and6 can be condensed with 6-chloropurine to give zeatin and (±)dihydrozeatin respectively. This provides a readily accessible method for isotope-labelled zeatin and its derivatives at side chain.Contribution No. 1064, Alberta Research CouncilProcess for the Preparation oftrans-3-formylbut-2-enenitrile S. Chen and J. MacTaggart, patent applicatioin registered in Canada and the United States of America.Acknowledgment. The author thanks Mr J. M. MacTaggart and Mrs C. M. Goulet for valuable experimental assistance and Dr R. M. Elofson for helpful discussions.     

2,2′-dihydroxy-6,6′-dinaphthyl disulphide (DDD) diazo blue B reactive granules in the parathyroid gland of the rat and toad

Zusammenfassung Granula in Parenchymzellen von Ratten und Kröten-Epithelkörperchen treten durch 2,2-Dihydroxy-6,6-dinaphthyl-disulfid (DDD) Diazo-Blau-B-gefärbt, deutlich hervor. Ihre Menge, Färbbarkeit und Verteilung unter verschiedenen Bedingungen scheinen für die zelluläre Sekretionstätigkeit charakteristisch zu sein.     

Conjugates of adenine 9-α-D-arabinofuranoside monophosphate (ara-AMP) with lactosaminated homologous albumin are not immunogenic in the mouse

Summary Conjugates of adenine-9--D-arabinofuranoside (ara-A) or of ara-A monophosphate (ara-AMP) with asialofetuin or with heterologous lactosaminated serum albumin (L-SA) are strong antibody inducers. But ara-AMP conjugates prepared with homologous L-SA are not immunogenic, at least in mice.Acknowledgments. This work was supported by Consiglio Nazionale delle Ricerche, Progetto finalizzato, Controllo crescita neoplasica, grant 800154596. Ara-AMP was a gift from Dr M. L. Black, Warner-Lambert Co (Ann Arbor, MI). The excellent technical assistance of Mr Goffredo Nanetti is gratefully acknowledged.     

The in vivo expression of the globin genes of theβ cistron in γ-,δ-, andδβ-thalassemia heterozygotes

There is considerable evidence suggesting that the switch from to and chain production after birth is due, in part, to silencing of the genes by stage-specific factors which bind to their promoters and to the competition from the adult ( and ) genes for a common enhancer element located in the locus control region. As a consequence one can expect that the increased Hb F production in adults with hereditary persistence of fetal hemoglobin or -thalassemia is directed mainly by -globin genes in cis to the deletion(s) responsible for these conditions. Here we review data on heterozygotes with -, -, or -thalassemia, who also had an^AT mutation, in cis or in trans, which was used as a marker of gene expression. The results show that a deletion affecting adult genes favors the expression of genes in cis, while the deletion of a single gene does not affect the expression of the gene in cis but leads to a faster switch postnatally.     

Purification and characterization of aβ-glucosidase (linamarase) from the haemolymph ofZygaena trifolii Esper, 1783 (Insecta,Lepidoptera)

Summary A -glucosidase (linamarase) was purified 52-fold with a recovery of 27% from the haemolymph of the larvae ofZygaena trifolii, ESPER, 1783 (Lepidoptera, Zygaenidae). The final enzyme preparation was found to be nearly homogeneous on both disc polyacrylamide gel electrophoresis and SDS-polyacrylamide gel electrophoresis. The molecular weight of the enzyme was determined to be about 130 kDa; it consisted of two subunits of about 66 kDa. The enzyme showed an optimum between pH 4.5 and 5 with linamarin and a broad optimum between pH 3.5 and 6.5 for p-nitrophenyl--D-glucoside; the temperature optimum was 40°C. The -glucosidase showed a high specificity for its endogenous substrates linamarin and lotaustralin. Among the other natural and artificial substrates tested, only prunasin and p-nitrophenyl--D-glucoside were hydrolyzed by the enzyme, whereas linustatin, salicin, cellobiose and trehalose were not. The enzyme is strongly inhibited by -glucosylpiperidine.     

Antagonism by haloperidol of the suppression of exploratory locomotor activity induced by the local application of(−)3-(3-hydroxyphenyl)-N-n-propylpiperidine into the nucleus accumbens of the rat

Summary The injection of (–)3-PPP into the nucleus accumbens, 10 g/side, produced a suppression of exploratory locomotor activity without affecting treadmill locomotion. Furthermore, the suppression of exploratory locomotor activity produced by (–)3-PPP was antagonized by the administration of haloperidol, 25–50 g/kg i.p.Acknowledgments. The figures were prepared by M. Kröning at the Department of Psychology, University of Göteborg. This work was supported by Torsten and Ragnar Söderberg's Foundation, Magn. Bergvall Foundation and Åke Wiberg Foundation.     

Pharmacodynamic profile of CQP 201-403, a novel 8α-amino-ergoline

Summary The profile of action in animals of CQP 201-403, a novel 8-amino-ergoline, is in most aspects that of a very potent dopaminomimetic, both as a prolactin secretion inhibitor, and at the levels of the CNS and the cardiovascular system. Qualitatively CQP 201-403 differs slightly from bromocriptine and apomorphine in its effects on the CNS (no influence on serotonin metabolism in the rat cortex; induction of masculine mounting behavior in rats) and the cardiovascular system of the dog (reflex tachycardia in response to a blood-pressure fall). In man the new compound proved to be highly active in lowering prolactin serum levels and to be more potent than bromocriptine (Parlodel^®).In memory of Dr Annemarie Closse, who died 14 June 1987.     

Edward Gresham’s Astrostereon,or A Discourse of the Falling of the Planet (1603), the Copernican paradox,and the construction of early modern proto-scientific discourse

This paper investigates the functioning of the ‘Copernican paradox’ (stating that the Sun stands still and the Earth revolves around the Sun) in the late sixteenth- and early seventeenth-century England, with particular attention to Edward Gresham's (1565–1613) little-known and hitherto understudied astronomical treatise – Astrostereon, or A Discourse of the Falling of the Planet (1603). The text, which is fully appreciative of the heliocentric system, is analysed within a broader context of the ongoing struggles with the Copernican theory at the turn of the seventeenth century. The article finds that apart from having a purely rhetorical function, the ‘Copernican paradox’ featured in the epistemological debates on how early modern scientific knowledge should be constructed and popularised. The introduction of new scientific claims to sceptical audiences had to be done both through mathematical demonstrations and by referring to the familiar concepts and tools drawn from the inventory of humanist education. As this article shows, Gresham's rhetorical techniques used for the rejection of paradoxicality of heliocentrism are similar to some of the practices which Thomas Digges and William Gilbert employed in order to defend their own findings and assertions.     

Localisation of acetylcholinesterase in rat myotubes in the presence of β-endorphin and β-endorphin-(1-27)

Summary In rat embryo skeletal myotubes, acetylcholinesterase is present, as multiple forms, and can be detected in deposits at the cell surface. Myotubes cultured in the presence of -endorphin, exhibit an increased predominance of the globular (precursor) forms of the enzyme, which are largely restricted to intracellular sites associated with nuclei. In the presence of -endorphin-(1-27), the relative proportions of the different forms of acetylcholinesterase is similar to that seen in the controls, but the enzyme is intracellular and has a characteristic focal localisation in the myotube.     

Portugal: Recent Information from the Department of International Relations of the Instituto Nacional de Investigação Cientifica,Lisboa (INIC)

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Portugal: Recent Information from the Department of International Relations of the Instituto Nacional de Investigação Cientifica, Lisboa (INIC)     

A stepwise model of polyreactivity of the T cell antigen-receptor (TCR): its impact on the self–nonself discrimination and on related observations (receptor editing,anergy, dual receptor cells)

The existence of antigen-receptors, BCR, and T cell antigen-receptors, that are “polyreactive”, necessitates a rethinking of its effect on two problems faced by the “adaptive” immune system: the self (S)–nonself (NS) discrimination and the determination of effector class. Here, we will concentrate on the impact of polyreactivity on the S–NS discrimination. The anti-S cells interacting with S (i.e., responding to Signal 1) are on the pathway to inactivation. Before irreversibility sets in, these cells can be activated by a second signal (Signal 2) from an effector T-helper (eTh). As these polyreactive anti-S cells express anti-NS specificities, they can be activated by recognition of NS-epitopes in the host’s normal immunogenic load with the potential to result in autoimmunity. This problem is delineated using a discrete structural model, the corollaries of which are: (1) a two-step pathway for the purging of anti-S cells (i.e., the S–NS discrimination), and (2) defensible contexts within which to view the phenomena of receptor editing, anergy, and dual receptor cells.