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.     

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.     

α-Actinin structure and regulation

Alpha-actinin is a cytoskeletal actin-binding protein and a member of the spectrin superfamily, which comprises spectrin, dystrophin and their homologues and isoforms. It forms an anti-parallel rod-shaped dimer with one actin-binding domain at each end of the rod and bundles actin filaments in multiple cell-type and cytoskeleton frameworks. In non-muscle cells, alpha-actinin is found along the actin filaments and in adhesion sites. In striated, cardiac and smooth muscle cells, it is localized at the Z-disk and analogous dense bodies, where it forms a lattice-like structure and stabilizes the muscle contractile apparatus. Besides binding to actin filaments alpha-actinin associates with a number of cytoskeletal and signaling molecules, cytoplasmic domains of transmembrane receptors and ion channels, rendering it important structural and regulatory roles in cytoskeleton organization and muscle contraction. This review reports on the current knowledge on structure and regulation of alpha-actinin.     

α- andβ-Guttiferins

Zusammenfassung Die Isolierung, Charakterisierung und antibiotischen Eigenschaften von-Guttiferin (I), C₃₃H₃₈O₈ (Smp. 113–115°), aus den Samenhülsen und vom nahe verwandten-Guttiferin (II), C₂₉H₃₆O₆ oder C_33–34H_38–40O₈ (Smp. 86–91°) (möglicherweise identisch mit-Gambogasäure), aus Gummigutt, dem harzigen Sekret vonGarcinia morella, wurden beschrieben und ihre Verwandtschaft zu Morellin und Moreollin, den beiden bekannten Pigmenten der Samenhülsen, dargelegt. Für I wurde eine Partialstruktur vorgeschlagen. Die Bildung derselben komplexen bromhaltigen Säure vom Smp. 199 bis 200° unter der Einwirkung von Natriumhypobromit auf I und II spricht ferner für deren nahe strukturelle Verwandtschaft.     

Scattering ofα-particles from nuclei

Zusammenfassung Nach einem Überblick über dieRutherfordsche Theorie der Ablenkung von -Teilchen im elektrostatischen Feld des Atomkernes wird auf kürzliche Streuexperimente hingewiesen. Die Streuung von -Teilchen an schweren Kernen ist einem optischen Beugungsphänomen ähnlich. Resonanzen wie sie in der Streuung an leichten Kernen beobachtet werden, sind akustischen Resonanzen vergleichbar.     

Extrahepatic 7α-hydroxylation of dehydroepiandrosterone

Zusammenfassung In verschiedenen Rattenorganen (Lunge, Niere, Milz, Blut, Muskelgewebe) konnte ein System nachgewiesen werden, das imstande ist,in vitro Dehydroepiandrosteron an der 7-Stellung zu hydroxylieren. Dies Ergebnis weist auf die allgemein mögliche extrahepatale und extraadrenale Steroidhydroxylation hin.     

Age distribution of circulatingα-interferon

Summary A sensitive radioimmunoassay showed that circulating -interferon in the plasma of healthy individuals was low in children and reached the highest level in the young adult, then declined gradually with age. Circulating -interferon was 0.201±0.059 ng/ml in males (n=19) and 0.184±0.076 ng/ml in females (n=14) at ages 30–39 years old. It was noted that circulating -interferon was maintained up to a certain level even in elderly individuals.     

Activation ofα-carbons of amides

Summary The reactions of Vilsmeir complexes of amides/imides with electrophiles afford the corresponding -substituted products in good yield.     

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.     

α-Amanitin: Inactivation by bovine lactoperoxidase

Summary The principle amatoxin, -amanitin, is found to be extremely sensitive toward lactoperoxidase catalyzed degradation, rather than iodination, of the indole nucleus. Extensive attenuation of inhibitor potency against eukaryotic DNA-dependent RNA polymerase II accompanies the treatment of -amanitin with lactoperoxidase, iodide and hydrogen peroxide.This work was supported in part by NIH grant 22147 and a grant from the University of Illinois.     

核受体LXRα靶基因研究进展

核受体的研究近几年已有飞速的发展。LXRα(Liver X Receptor α)是一种与脂类代谢有关的核受体。研究发现LXRa的靶基因具有调节脂类的吸收、运输、转化和生物合成的功能，此外，LXRα在糖类的代谢等方面也有重要的调控作用。研究结果表明LXRα与动脉粥样硬化的发生有非常密切的关系。目前利用LXRα为靶标进行抗动脉粥样硬化药物筛选已经成为一个重要的研究方法。     

Preferences of transmembrane helices for cooperative amplification of Gαs and Gαq signaling of the thyrotropin receptor

The majority of constitutively activating mutations (CAMs) of the thyroid-stimulating hormone receptor display a partially activated receptor. Thus, full receptor activation requires a multiplex activation process. To define impacts of different transmembrane helices (TMHs) on cooperative signal transduction, we combined single CAMs in particular TMHs to double mutations and measured second messenger accumulation of the G_αs and the G_αq pathway. We observed a synergistic increase for basal activity of the G_αs pathway, for all characterized double mutants except for two combinations. Each double mutation, containing CAMs in TMH2, 6 and 7 showed the highest constitutive activities, suggesting that these helices contribute most to G_αs-mediated signaling. No single CAM revealed constitutive activity for the G_αq pathway. The double mutations with CAMs from TMH1, 2, 3 and 6 also exhibited increase for basal G_αq signaling. Our results suggest that TMH2, 6, 7 show selective preferences towards G_αs signaling, and TMH1, 2, 3, 6 for G_αq signaling.     

α进制最小能量区间小波框架的构造

基于小波多尺度特征和信号多通道理论需要,本文对a进制最小能量区间小波框架进行了系统研究,其中a为任意大于等于2的正整数.首先,给出了a进制最小能量区间小波框架的定义,建立了a进制最小能量区间小波框架的充要条件;其次,我们设计了支撑长度为任意整数γ的a进制最小能量区间小波框架的构造算法,并构造性地给出了构造算法所涉及矩阵的表达式;最后,给出了最小能量区间小波框架的分解与重构算法,并构造了数值算例.     

Synthesis of a pregnancy-associatedα-macroglobulin by human leucocytes

Résumé Le sang des femmes enceintes peut contenir plusierus protéines sériques uniques en leur genre. Celle qui se présente le plus souvent est une -globuline de grand poids moléculaire. Un test in vitro utilisant l'incorporation de¹⁴C-glutamine ou³H-leucine dans la glycoprotéine a montré que celle-ci peut être synthétisée par des leucocytes.

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We thank Dr.J. E. O'Grady and Dr.A. Shephard for obtaining the blood samples. This work was supported by a grant from the Scottish Home and Health Department.     

Purification of 20α-hydroxysteroid dehydrogenase from human erythrocytes

Summary 20-hydroxysteroid dehydrogenase was found in the supernatant after hemolysis of human erythrocytes, and the enzyme was isolated from the membrane-free hemolysate on a DEAE-cellulose column. The NADPH-generating system was essential for the reaction.Acknowledgments. We wish to thank Dr A. Tomoda, Department of Biochemistry, Kanazawa University School of Medicine, and Dr T. Yubisui, Department of Biochemistry, Medical College of Oita, for their advice and useful discussions.     

α-Thioglycerol sensitive excitatory oxytocin receptors in fowl rectum

Summary The selective antagonism of the excitatory responses of oxytocin by -thioglycerol and its potentiation by Mg⁺⁺ indicate the presence of specific oxytocin receptors in fowl rectum. In addition, the sensitivity of the rectum to very small doses of oxytocin suggests a possible facilitatory role of neurohypophyseal hormones in oviposition.Acknowledgment. The authors wish to express their sincere thanks to Dr M.S. Sastry, Head of the Division and Dr C.M. Singh, Director of the Institute for providing the facilities and Mr Dev Singh for his technical assistance.     

α-L-aspartyl-L-alanine (a neural dipeptide) enhances synaptic transmission

Summary -L-aspartyl-L-alanine, a dipeptide found in the brain, increases the amplitude of the miniature endplate potentials (MEPPs) in phrenic nerve-diaphragm preparations from rats. The peptide also stimulates the appearance of a population of giant MEPPs.This work was supported by NSF grant BNS 79-00352 and NIH grant CA-27031 to R. Lim.     

Steroids and related natural products. 14α-Methyl testosterone

Zusammenfassung Eine Zwanzigstufenumwandlung von Isocholesterol (rohes Lanosterol) zu 14-Methyltestosteron wurde ausgeführt und die Reaktionsfolge von 3-Hydroxy-4,4,14-trimethyl-20-oxo-5-pregnan zu 14-Methyltestosteron beschrieben.

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Part XIV. Part XIII,G. P. Mueller andG. R. Pettit, Exper.18, 404 (1962).

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A preliminary report of this study was presented (August 27, 1962) at The Second International Symposium on the Chemistry of Natural Products, Prague (Czechoslovakia).

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This investigation was supported by PHS Research Grants CY-4074(C3) and CA 04074-05 from the National Cancer Institute, Public Health Service.     

Luteolytic potency of 16-phenoxy-derivatives of prostaglandin F2α

Summary The binding of 16-phenoxy derivatives of prostaglandin (PG) F₂ to rat luteal membranes, and also their abortifacient potency in pregnant rats, have been studied. Competitive binding studies with various PG-analogues were performed in ovaries of juvenile rats pretreated with PMSG and HCG, and in parallel studies the abortifacient potency of these substances was tested, in pregnant rats. It was observed that this class of derivatives bound to the PGF₂ receptor as well as, or even better than the parent compound PGF₂. Modifications in the carboxyl group at C-1 yielded derivatives with a higher affinity for the receptor, in decreasing order of effectiveness as follows:-COOR>COOH>OH. The data obtained from the binding studies also compared well with data on the abortifacient potency in pregnant rats. It is concluded that the addition of a phenoxy group to either the lower or upper side chain of PGF₂ may augment the binding to the receptor as well as the biological responses induced by the post receptor effect.