Inhibition sélective des «vraies» et «pseudo»-cholinestérases du rectus de grenouille

Summary The hydrolysis of acetylcholine chloride (0.01M) by frog's rectus extracts, is inhibited by low concentrations of 3318 CT (CI-50 3.2×10^–7) and high concentrations of D.F.P. (CI-50 1.3×10^–5). Inversely, the hydrolysis of butyrylcholine perchlorate is inhibited by low concentrations of D.F.P. (CI-50 3×10^–9) and high concentrations of 3318 CT (CI-50 3×10^–4). Both are inhibited by similar concentrations of neostigmine (CI-50 1.1×10^–7 and 1.5×10^–7). Frog's rectus thus contains true and pseudo-cholinesterases. The inhibitions produced by D.F.P. added to the muscle itself (and not the extract) correlates well with the potentiation of the corresponding ester. Sensitization to AcCh and to BuCh appears to be specifically related to the inhibition of Ac ChE for the former ester, of XChE for the second one.     

Effect of mercuric acetate on mobilization of N and P during germination and seedling growth ofCicer arietinum

Summary Mercuric acetate, at 5.0×10^–5 M, stimulates the mobilization of total nitrogen and phosphate reserves from cotyledons during seedling growth inCicer arietinum cv H208 whereas it suppresses the same process at 2.5×10^–4 M.Thanks are due to Dr D. Banerji for providing facilities and helpful suggestions.     

Determination of diel periodicity of sex pheromone release in three species of Lepidoptera by ‘closed-loop-stripping’

Summary By means of closed-loop-stripping and subsequent GC analyses the diel periodicity of release of (Z)-11-hexadecenyl acetate, (E)-8-dodecenyl acetate, and (Z)-9-tetradecenyl acetate, the main constituents of the respective sex pheromone blends ofMamestra brassicae, Cryptophlebia leucotreta andSpodoptera sunia females, was determined.Pheromones, 64. For the 63rd contribution we have taken from: Szöcs, G., Toth, M., Bestmann, H. J., Vostrowsky, O., Heath, R. R., and Tumlinson, J. H., Z. Naturforsch.42c (1987) 165; Pheromones, 62: Bestmann et al.¹³.     

Propriétés antiacétylcholinestérasiques du diiodométhylate debis-(diméthylamino-3-phénoxy)-1-3 propane,de ses dérivés phénoliques et des esters carbamiques correspondants

Summary Thein vitro anti-acetylcholinesterase properties ofbis-(dimethylamino-3-phenoxy)-1-3 propane dimethiodide (2842 CT) of two phenolics derivatives (3443 CT and 3116 CT) and of the two corresponding carbamic esters (3152 CT et 3113 CT) have been compared using human red blood corpuscles as enzyme source; under specified conditions, the Cl-50 are respectively 8 × 10^–7 M for 2842 CT, 3.5 × 10^–9 for the two phenolic compounds, and 1.5 × 10^–9 for the carbamic esters. The potencies of these phenols are very close to those of the carbamates, being a bit higher or lower depending on the concentration of the inhibitor and on the time of the readingThe two phenolic compounds, like 2842 CT, react readily with the enzyme contrarily to the carbamic esters which combine slowly. On the other hand the inhibition by the phenolic derivatives is as stable against washing as that by the carbamates. The carbamates, but not the phenols, show the slow displacement phenomenon.Some of these characteristics are compatible with the hypothesis that carbamic compounds could act through liberated phenolic functions but others indicate that carbamic groups have a role of their own.     

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.     

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.     

The Dead Sea — alive again

In the thirteen years of quantitative studies on the microbiology of the Dead Sea from 1980 onwards three distinct periods can be discerned. Mass development of the green unicellular algaDunaliella parva (up to 8,800 cells/ml) and red archaeobacteria (2×10⁷ cells/ml) was observed in 1980, following a dilution of the upper water layers by rain floods. This bloom disappeared at the end of 1982 as a result of a complete mixing of the water column. During the period 1983–1991 the lake was holomictic, and noDunaliella cells were observed. Viable bacteria were present during this period in very low numbers. Heavy rain floods during the winter of 1991–1992 caused a new stratification as the upper five meters of the water column became diluted to 70% of their normal salinity. In this upper water layerDunaliella reappeared (up to 3×10⁴ cells/ml at the beginning of May, rapidly declining to less than 40 cells/ml at the end of July), and a bloom of red archaeobacteria (3×10⁷ cells/ml) once more imparted a red coloration to the lake.     

Transfer of isolated nuclei into protoplasts ofAspergillus nidulans

Nuclei were isolated from protoplasts of a haploid auxotrophicAspergillus nidulans strain. Transformation of protoplasts prepared from a complementary haploid auxotrophic strain with these purified nuclei resulted in both heterokaryotic and diploid colonies. The nutritionally-complementing colonies appeared at a frequency of 5×10^–7 to 10^–8.     

Monoclonal antibodies to L-asparaginase

Summary Five hybridomas secreting monoclonal antibody toE. coli L-asparaginase were isolated. These monoclonal antibodies were classified into 3 different subclasses; Ig G₁ (1 clone), Ig G₂ (2 clones) and Ig G₃ (2 clones). One of them possessed anti-L-asparaginase neutralizing activity. Four antibodies examined demonstrated a linear Langmuir binding plot and binding affinities, with equilibrium dissociation constant (K_d) ranging between 2.5×10^–9M and 6.3×10^–10 M. The monoclonal antibodies should be useful probes for investigation of the enzyme activity.     

Effect of Ketamine hydrochloride on oxygen and glucose uptake by brain tissue in vitro

Resumen El clorhidrato de Ketamina (1×10^–3 M y 1×10^–4 M) incrementa el consumo de oxigeno de cortes de cerebro de rata incubados en Krebs-Ringer fosfato conteniendo 5 mM ó 100 mM de potasio. La droga no modifica el consumo de oxigeno de homogeneizado de cerebro total.     

Zur Stereochemie der Propandioldehydrase-Reaktion

Summary Propanedioldehydrase is shown to convert both (+)-(S)-2-²H-propanediol,3, and (–)-(R)-1-²H₂-propanediol,5, to specimens of deuterated propion-aldehyde, for which the (S)-configuration has been established. Thus, in the propanedioldehydrase reaction migration of hydrogen atoms from C–1 to C–2 always occurs with inversion of configuration.     

A potent attractant of zoospores ofAphanomyces cochlioides isolated from its host,Spinacia oleracea

A highly potent attractant of zoospores ofAphanomyces cochlioides, a causal fungus of the root rot disease of spinach (Spinacia oleracea), was isolated from spinach roots, and its structure was determined by spectroscopic evidence and chemical synthesis as cochliophilin A (5-hydroxy-6,7-methylenedioxyflavone,1). A chromosorb particle prepared by soaking in solution of1 showed a potent attracting activity toward the zoospores using concentrations of1 above 10^–9 or 10^–10 M.     

Bactericidal activity againstPseudomonas aeruginosa is acquired by cultured human monocyte-derived macrophages after uptake of myeloperoxidase

Myeloperoxidase (MPO) is an enzyme located within polymorphonuclear neutrophils capable of producting cytotoxic oxidant species that are particularly active against bacteria with polysaccharide capsules.Pseudomonas aeruginosa (10⁶ bacteria per 1 ml) are killed within 1 h in vitro by a MPO/H₂O₂/Cl^– system (48 mU=132 ng of MPO). The question arose as to whether human macrophages would acquire cytotoxic activity when loaded with this enzyme. Monocytes were therefore isolated from human blood and cultured for up to ten days to induce maturation to macrophages. These cells lost endogenous MPO within five days while H₂O₂ production in response to stimulation by phorbol myristate acetate (10^–6M) decreased to 23% within ten days. On the other hand, their capacity to take up exogenous MPO increased fourfold from day three to day ten. Human macrophages cultured from eight days (when both H₂O₂ production and MPO uptake were sufficient) were therefore used to study the effects of MPO uptake on cytocidal activity againstPseudomonas aeruginosa. After a 1 h MPO loading period, macrophages (5×10⁵ cells per ml) were incubated in the presence of bacteria (0.5 to 2×10⁶ bacteria per ml) for 2 h at 37°C. At a bacteria/macrophage ratio of 1, only 34.8±7.0% of bacteria survived (compared to killing by non-loaded macrophages), while 74.4±9.3% survived at a ratio of 4. From these results, we conclude that loading macrophages with exogenous MPO could enhance their microbicidal activity, suggesting a potentially useful therapeutic application.     

The effect of perchlorate ion and some pharmacological agents on the sensitivity of the frog (Rana pipiens) rectus abdominis to acetylcholine

Zusammenfassung Die Reaktion des mit Eserin vorbehandelten musculus rectus abdominis des Frosches auf Acetylcholin liess sich durch Oxotremorin (2.0·10^–5 M), Arecolin (2.0·10^–5M), Aceclidin (1.0·10^–4 M) und Carbachol (2.0·10^–7 M) verstärken, während Atropin (1.0·10^–5 M) hemmend wirkte. Perchlorationen in Konzentrationen über 2 · 10^–4 M sensibilisierten den Froschmuskel erheblich und reduzierten die Grenzdosis, bei der eine Potenzierung durch Substanzen mit muskarinähnlicher Wirkung beobachtet wird. Alle beschriebenen Reaktionen liessen sich durch Gehirnextrakte verstärken, in denen zuvor Acetylcholin durch Kochen in alkalischer Lösung zerstört worden war.

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This work was supported by NIH Grants No. NB 03007 and No. 5-F1-GM-22,905.     

Sex pheromone blend of the codling moth,Cydia pomonella: Evidence for a behavioral role of dodecan-1-ol

Summary Pheromone glands and effluvia of the codling moth female containE-8, E-10-dodecadien-1-ol as main component, accompanied by its geometric isomers, the corresponding acetate and aldehyde (both in gland extracts only),E-9-dodecen-1-ol and saturated alcohols of 10 to 18 carbons. Dodecan-1-ol as the most abundant secondary component (about 30% of the female blend) acts in the wind tunnel by widening the dose range over which codling moth males are optimally attracted toE-8, E-10-dodecadien-1-ol.This research was supported by the Swiss National Science Foundation. We thank W. Riggenbach for supplying moths and T. Wildbolz, P. Charmillot and M. Tóth for conducting field trials.     

Furan fatty acid steryl esters from the marine spongeDictyonella incisa which show inflammatory activity

Summary Three new furan fatty acids, (9Z, 19Z)-3, 6-epoxyhexacosa-3,5,19-tetraenoic acid (1a), (8Z, 11Z, 14Z, 17Z)-3, 6-epoxyeicosa-3,5,8,11,14,17-hexaenoic acid (2a), and (8Z, 11Z, 14Z, 17E)-3, 6-epoxyeicosa-3,5,8,11,14,17-hexaenoic acid (3a), and a new polyunsaturated fatty acid (5Z, 8Z, 11Z, 14Z, 17E)-eicosa-5,8,11,14,17-pentaenoic acid (6a), present in the spongeDictyonella incisa as the respective steryl esters, have been isolated as methyl esters and their structures have been determined by spectral and chemical analysis. The furan fatty acid esters have shown a high inflammatory activity, which suggests their potential role as feeding deterrents.     

Inhibition of mammalian acetylcholinesterase by phenylmethanesulfonyl fluoride

Resumen El fenilmentano sulfonil fluoro (FMSF) 4×10^–5 M inhibe a la acetilcolinesterasa (E. C. 3.1.1.7) de cerebro de rata en más de 50%, y 9×10^–4 M más de 90%. La constante de reacción inhibidor enzima es de 4.7×10² (1 mol^–1 min^–1). La colinesterasa (E. C. 3.1.1.8) de cerebro de rata es insensible a FMSF.

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Supported by NIMH Grant No. 1 RO3 MH 19125, by Comisión Nacional de Investigación Cientiffica Proyecto No. 80, and by Comisión de Investigación Cientiffica Universidad de Chile, Proyecto No. 95.     

Effect of strychnine on the electroretinogram of the isolated rabbit retina

Zusammenfassung Strychnin in einer Konzentration von 3×10^–6 bis 3,5×10^–5 M/l verursacht eine vorübergehende Vergrösserung derb-Welle des ERG der isolierten Kaninchennetzhaut, in einer Konzentration von 7×10^–5 bis 7×10^–4 M/l verkleinert es dieb-Welle. Aus den Ergebnissen wird geschlossen, dass die Substanz zumindest teilweise schon auf die Schicht des zweiten Neurons wirkt.     

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).     

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.