Inhibitory effect of cytokinins on PHA-induced human lymphocyte stimulation.

The inhibitory effect of various purine derivatives on PHA-induced human lymphocyte blast formation was studied. Two nucleoside cytokinins, N6-benzyladenosine and N6-isopentenyladenosine, inhibited blast formation at concentrations as low as 10(-6) M. However, the other cytokinins, which lacked the ribosyl residue at N9 position, had to be at the higher molar concentration of 10(-4) before they could induce the same inhibitory effect.     

Der Einfluß von Desoxycorticosteron auf die Azetylcholinwirkung am isolierten Froschherz

Summary The action of desoxycorticosteronglucoside was tested on the isolated frog-heart. In concentrations of 10^–6 to 10^–4 a small negative inotropic effect is prevailing. Acting together with acetylcholine, the substance diminishes or abolishes the negative inotropic and chronotropic action of acetylcholine. Eserin has no influence and the inhibition is also observed with cholinchloride and the carbaminoyl ester of choline. This inhibitory action bears a close resemblance to the inhibitory action of thiamin. In both cases a complex mechanism seems to be involved.     

Biological effects of trilostane in vitro on oocyte maturation and fertilization in the hamster

Summary The effects of the inhibition of steroidogenesis by trilostane on oocyte maturation were examined by studying spontaneous maturation and fertilization in vitro. 10^–6 M trilostane had no influence on the meiotic process, whether the oocytes were naked or not. At a concentration of 10^–6 M and 10^–7 M trilostane, low normal pronuclear formation and high polyspermy were found during in vitro fertilization. However, no retarded male pronuclear development could be detected in the trilostane-treated group. Thus, steroid producing activity within ova is apparently necessary to prevent multiple sperm penetration, but it has no effect on meiosis or the action of the so-called male pronucleus growth factor (MPGF).     

Role of adenosine A1 and A2 receptors in the regulation of aldosterone production in rat adrenal glands

Summary To investigate the roles of adenosine A₁ and A₂ receptors in the regulation of aldosterone production, we examined the effects of adenosine and adenosine agonists (N⁶-cyclohexyl adenosine; selective adenosine A₁ receptor agonist and 5-N-ethylcarboxamine adenosine; selective adenosine A₂ receptor agonist) on aldosterone and cyclic AMP production in rat adrenal capsular cells. Neither adenosine nor 5-N-ethylcarboxamine adenosine caused significant effects on basal aldosterone or cyclic AMP production. Also, adenosine (10^–3M) showed no consistent effects on aldosterone and cyclic AMP production induced by ACTH. On the other hand, N⁶-cyclohexyl adenosine exhibited a significant inhibition of basal aldosterone and cyclic AMP production at doses of 10^–4 M and 10^–3 M; furthermore, 10^–3 M N⁶-cyclohexyl adenosine inhibited aldosterone and cyclic AMP production stimulated by ACTH. These results suggest that adenosine A₁ receptors are coupled to and inhibit adenylate cyclase and may be involved in the inhibition of aldosterone production.     

Growth ofNostoc muscorum mutants in the presence of diuron (DCMU) and L-methionine-DL-sulfoximine

Summary Diuron (DCMU) is inhibitory to the photoautotrophic and photoheterotrophic growth of the N₂-fixing blue-green algaNostoc muscorum at concentrations of 1.0×10^–5 M and 2.0×10^–5 M, respectively. A mutant of this organism resistant to 5.0×10^–5 M DCMU under its photoheterotrophic growth conditions, with the ability to utilize DCMU as a carbon and nitrogen source for growth, and complete inability to grow photoautotrophically has been isolated. With the apparent defect in its photosynthetic ability, it is suggested that theDCMU ^r mutant lacks the step inhibited by 1.0×10^–5 M DCMU, and metabolizes DCMU by an existing enzyme system in the absence of such inhibition. That this enzyme may be glutamine synthetase (GS) is explained with the help of a L-methionine-DL-sulfoximine (MSO)-resistant mutant ofN. muscorum which is able to grow faster with 2.0×10^–5 DCMU and is known to contain an altered GS.Thanks are due to the Council of Scientific and Industrial Research, CSIR Complex, Govt. of India, New Delhi-110012, for appointing the author to the Scientists' Pool for undertaking researches on the physiological and genetic controls of nitrogen metabolism in blue-green algae, a part of which is presented in this literature.     

Caclium causes the biphasic dose-response curve for pancreatic amylase secretion

Summary High concentrations of bethanechol (10^–4 to 10^–3 M) were effective stimulants of amylase secretion from the mouse pancreas if incubations are performed in low [ca²⁺] (0.1 mM) solutions but not if normal Krebs solution (2.56 mM Ca²⁺) was used. This inhibitory effect of Ca²⁺ at high secretagogue concentrations did not appear to be mediated through the microtubules or microfilaments.     

Phosphoramidon enhances allatostatin-mediated inhibition of juvenile hormone biosynthesis in the corpora allta of the cockroach,Diploptera punctata

Use of the enkephalinase inhibitor phosphoramidon in the in vitro radiochemical assay for juvenile hormone biosynthesis enhanced allatostatin-mediated inhibition of hormone production by corpora allata of the cockroach,Diploptera punctata. Significant increases in inhibition in day 2 virgin female CA by AST 1 (at 10^–7 M) and AST 4 (10^–8–10^–7 M) were observed in the presence of phosphoramidon (10^–5M or greater). No significant increases in inhibition were seen in CA from day 6 mated females with AST 4 (10^–9–10^–7M) and phosphoramidon combined. Phosphoramidon alone had no effect on JH biosynthesis. Analysis of allatostatin content of the CA, as determined by ELISA, revealed that addition of phosphoramidon to the medium increased the endogenous allatostatin conten in CA of virgin and mated females. The similarity in primary structure between allatostatins and enkephalin-like peptides and their similar distribution makes it probable that phosphoramidon acts by preventing breakdown of allatostatins within the CA.     

Influence of environmental conditions on the amount of N2O released from activated sludge in a domestic waste water treatment plant

Waste water purification is characterized by intensive mineralization and nitrification processes. Because of the high O₂ demand, temporarily anaerobic conditions may be produced, and denitrification by nitrifying organisms as well as heterotropic denitrification may contribute to N₂O release. In situ measurements (1993–1994) suggest that N₂O is released from activated sludge in a domestic waste water treatment plant at an average rate of 1040 g m^–2h^–1 with a range between zero and 6198 g m^–2h^–1. The production of N₂O seems to be related to the concentration of NO ₂ ^– and NO ₃ ^– as well as to the pH. In the waste water about 75–200 g N₂O l^–1 is dissolved. This N₂O is released after discharge into the receiving waters. The N₂O is produced essentially by nitrification rather than by heterotropic denitrification. On a long-term scale the increasing use of mechanical-biological waste water purification plants world-wide may add increasingly to the anthropogenic production of N₂O, although the present amount of N₂O produced is negligible compared to its global terrestrial production.     

VIP and histamine H2 receptor activity in human fetal gastric glands

Summary Vasoactive intestinal peptide (VIP, EC₅₀=6.4×10^–10 M) and histamine (EC₅₀=3×10^–6 M) activated the cyclic AMP generating system in gastric glands isolated from two human fetuses at 23 weeks gestation. Histamine antagonism by the H₂ receptor blockers cimetidine (Ki=0.35×10^–6 M) and ranitidine (ki=0.51×10^–7 M) clearly characterized the histaminic activation as being of the H₂ type. It is suggested that these two vasoactive hormones may operate as neurocrine/paracrine regulators of the differentiation and/or function of the human gastric mucosa in utero.     

Die Wirkung von Spirolactonen und von Herzglykosiden auf den Natrium- und Kaliumtransport an Erythrocyten

Summary Experiments made on human red cells showed that spirolactones (SC 5233 and SC 9420) added to the sample as dry powder (10^–3 g/ml) exert an inhibitory action on the active transport of sodium and potassium across the cell membrane. Spirolactone at its saturation concentration in serum (1.5×10^–5 g/ml), however, was ineffective.The inhibitory action was not affected by aldosterone or hydrocortisone.Experiments involving exposure of red cells to spirolactone and a cardiac glycoside simultaneously led to the conclusion that these substances do not have the same mechanism of action. The inhibition caused by spirolactone added to the inhibition due to a supramaximal concentration of ouabain (5 × 10^–4).

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Diese Arbeit wurde unterstützt durch ein Stipendium der CIBA für naturwissenschaftliche, medizinische und technische Forschung.     

Effects of cycloheximide on protein synthesis in human lung tumors,regenerating rat liver and hepatomas

Summary 10^–4 M cycloheximide (CHM) inhibits leucine incorporation to about the same degree in slices of human lung tumors, rat hepatomas, regenerating livers and normal tissues. At 10^–6 M, CHM has a more pronounced effect on tumor tissue and regenerating liver than on normal tissues. 10^–8 M CHM stimulates protein synthesis in normal rat liver slices.     

Inhibition and sex specific induction of spawning by serotonergic ligands in the zebra musselDreissena polymorpha (Pallas)

Serotonin (5-hydroxytryptamine, 5-HT) stimulates spawning in the zebra mussel (Dressena polymorpha), a macrofouling European bivalve that has recently invaded North America. To develop methods of controlling zebra mussel spawning, two vertebrate serotonin antagonists, methiothepin and metergoline, known to bind with high affinity to snail 5-HT receptors, were tested for their ability to block 5-HT-induced spawning in zebra mussels. Methiothepin inhibited 5-HT-induced spawning at concentrations as low as 10^–6 M. Metergoline (10^–4 M) inhibited 5-HT-induced spawning; however, at lower concentrations (10^–8 to 10^–5 M), metergoline by itself significantly induced spawning in male, but not female zebra mussels. Metergoline (10^–5 M)-induced male spawning was inhibited by 10^–5 M methiothepin. Thus, methiothepin is the most effective inhibitor and metergoline the most powerful inducer of spawning yet tested in zebra mussels.     

Influence of cyclic nucleotides on protein synthesis in vascular smooth muscle

Summary The incorporation of leucice-¹⁴C into protein in bovine mesenteric arteries was augmented by cyclic GMP (10^–3 M) and decreased by cyclic AMP (10^–3 M). There was no effect of 5 AMP (10^–3 M). The phosphodiesterase inhibiting drugs theophylline (10^–3 M) and papaverine (5×10^–5 g/ml) both decreased the leucine-¹⁴C incorporation.We are indebted to Mrs.Lena Burlin for hear assistance. Finacial support has been provided by the Swedish State Medical Research Council (No. 04X-101X-4498).     

Activité antifibrillante chez l'animal d'un nouveau dérivé de la phényl-éthylamine

Summary A new synthetic phenyl-ethyl-amine derivative, the 2-[N- (3, 4-methylen-dioxyphenylethyl)-methylaminomethyl]-tetrahydrofuran, No. 11 081, exhibits a strong protective effect against cardiac fibrillation and arrhythmias produced by various experimental methods: against fibrillation due to aconitine 3 × 10^–8 on the isolated cat's heart, it is active in a concentration of 10^–6–2 × 10^–6. Against cardiac arrhythmias produced in the cat by adrenaline + CHCl₃ or cyclopropane, it shows a protective effect by 5–10 mg/kg i.v. and even perorally by 50 mg/kg. In these tests, the antifibrillatory activity of the new compound seems to be roughly the same as that of -fagarine, and higher than that of procaine.

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9^e communication sur les dérivés des alcoylène-imines; 8^e communication, cf. Exper.10, 261 (1954).     

Naringenin inhibition on expiants in vitro ofCichorium intybus (Chicory)

Riassunto La naringenina alla concentrazione di 10^–4 M inibisce in modo totale l'emissione di gemme in radici diCichorium intybus in vitro senza tuttavia bloccare completamente la callogenesi. A concentrazioni scalari minori (10^–5, 10^–6, 10^–7 M) questa sostanza causa una inibizione solo nella fase iniziale dell'esperienza.     

Fatty acid modulation of antiestrogen action and antiestrogen-binding protein in cultured lymphoid cells

Summary Nonsteroidal antiestrogens reversibly and specifically inhibited the proliferation of two estrogen receptornegative lymphoid cell lines (EL4 and Raji) in a dose-dependent manner. [³H]Thymidine incorporation of concanavalin A-stimulated primary splenocytes was also inhibited by 10^–6 M clomiphene (1-[4-(2-diethylaminoethoxy)phenyl]-1,2-diphenyl-2-chloroethylene). The antiproliferative effect could be prevented by the simultaneous presence in the growth medium of 10^–5 M linoleic acid or 10^–5 M arachidonic acid but not by 10^–6 M estradiol. Both lymphoid cell lines had high affinity antiestrogen-binding sites whose affinity could be altered by conditions of growth. Growth of EL4 cells in RPMI 1640 medium supplemented with charcoal-pretreated 5% fetal calf serum (charcoal-stripped medium) resulted in significantly higher affinity (K_d 0.54 nM±0.11 nM; n=6) than growth in medium supplemented with untreated serum (complete medium) (K_d=1.68 nM±0.48 nM; n=6) (p<0.001). This change in affinity was partly due to removal of fatty acids from the growth medium by charcoal pretreatment, since addition of 10^–5 M linoleic acid or 10^–5 M gamma-linolenic to charcoal-stripped medium decreased the affinity of the antiestrogen-binding protein. In contrast, growth in 10^–5 M stearic acid or 10^–5 M oleic acid did not significantly alter the affinity of the antiestrogen-binding protein, whereas 10^–5 M palmitic acid significantly increased its affinity. The same fatty acids were also tested for their intrinsic effects on EL4 cell proliferation. Oleic, linoleic and gamma-linolenic acids were growth stimulatory while stearic and palmitic acids were not. Thus linoleic and gamma-linolenic acids whose presence in the growth medium was associated with decreased affinity of [³H]tamoxifen (1-[4-(2-dimethylaminoethoxy)phenyl]-1,2-diphenylbut-1(Z)-ene) binding to the intracellular antiestrogen-binding protein were also growth stimulatory. Unsaturated fatty acids have previously been shown to inhibit binding of [³H]tamoxifen to the antiestrogen-binding protein in a cell-free system. The present observations demonstrate that unsaturated fatty acids also modify the affinity of the antiestrogen-binding protein in intact cells.     

Influence of turbulence on electrokinetic phenomena; experimental determination of the thickness of the diffuse part of the double layer

Zusammenfassung Durch Messungen in 10^–5, 10^–4 und 10^–3 N benzolischen Lösungen von Zn-di-i-propylsalizylat haben wir einen beträchtlichen Einfluss von Turbulenz auf Strömungsströme feststellen können. Dieser Einfluss kann ausgedrückt werden durch einen Faktorf, der in einem unserer Experimente einen Wert vonf=66 erreichte; aus den Werten vonf kann die Dicke der diffusen Doppelschicht in der Flüssigkeit berechnet werden.     

Melatonin antagonizes colchicine-induced mitotic arrest

Summary Melatonin, in concentrations up to 10^–3 M, showed no effect on mitosis in cultures of HeLa or KB cells. However, when melatonin at 10^–4 M was preincubated with HeLa cells prior to addition of 10^–7 M colchicine, a reduction in the mitotic index, in comparison to colchicine alone, was observed.This work was supported by PHS Grant No. CA 16425.     

Influence of atrazine (2-chloro-4-ethylamino-6-isopropylamino-s-triazine) on auxin metabolism of plants

Zusammenfassung Die Enzymaktivität der IES-peroxidase in Hafer-Koleoptilen wurde durch Atrazin in Konzentrationen von 10^–10–10^–21 M gehemmt, im Konzentrationsbereich von 10^–6–10^–8 M gesteigert. Atrazin förderte ferner das Wachstum von Sojabohnen-Kallusgewebe in Gegenwart von 5 mg/l Kinetin und 10^–10 bis 10^–18 M Atrazin im Nähragar. Diese Einwirkung von Atrazin auf den Wuchsstoffmetabolismus der Pflanzen gibt erste Anhaltspunkte, die zahlreich beobachteten Förderungen bzw. Hemmungen des Pflanzenwachstums unter dem Einfluss von Atrazin zu erklären. Die Resultate bilden weiterhin eine neue Grundlage für eine mögliche Interpretation des «Proteineffekts» der Triazine.     

Wirkungsverstärkung von Adrenalin und Noradrenalin durch Azetylcholin am isolierten Irisdilatator des Kaninchens

Summary Radial strips of the isolated iris of rabbits were suspended in streaming Tyrode's solution and their contractions were registered isometrically. The contractions produced by adrenaline or noradrenaline were increased after the administration of eserine or neostigmine. Acetylcholine in a concentration 5.10^–7–5.10^–6 M enhanced the effect of adrenaline and noradrenaline on both, the normal and the chronically denervated dilator muscle. Acetylcholine did not enhance the contractions by adrenaline and noradrenaline in the presence of atropine. Choline in a concentration of 5.10^–6 M had no effect whereas concentrations of 5.10^–5 M were slightly effective.