Sulfamidés et acides nucléiques

Summary The ribonucleic and thymonucleic acids are antisulphamide forEremothecium Ashbyii and for aSaccharomyces. This effect is due partly to purines, first of all to adenine, but not to any pyrimidines. ForSaccharomyces, the action of adenine is 1/10 of that of PAB acid. The suggestion is made that the bacteriostatic effect of the sulphamide is connected with the nucleic acids of the cytoplasma and the nucleus. Those are studied cytologically with help of the ribonuclease-method ofBrachet. Strong differences appear between the normal cells and the intoxicated ones.     

Über die trypanocide Wirksamkeit von Terephthalaniliden

Summary Compounds of the terephthalanilide series show, besides their antileukemic and bacteriostatic properties, considerable activity againstTrypanosoma brucei andT. congolense.      

Activité staphylostatique de composés du groupe des benzophénarsazines

Summary It is shown that certain compounds belonging to the group of angular benzophenarsazines display a high specific bacteriostatic activity towardsMicrococcus pyogenes var.aureus. This biological property provides a further ground of similarity between these compounds and one of their structural analogues, 3,4–5,6-dibenzocarbazole.     

Activité staphylostatique de quelques diphénols,naphtols et chalcones nouveaux

Summary Some substituted derivatives of resorcinol and-naphthol, and a chalkone derived from thiophene, namelyp-chlorobenzal(5-nitro-2-acetothienone), are shown to possess high bacteriostatic activity towardsMicrococcus pyogenes var.aureus; no such activity was found towardsEscherichia coli, even at higher concentrations.     

Über die hemmung des wachstums vonLactobacillus casei durch einige antiphlogistica

Summary A new method for the classification of antiphlogistics is described using the growth inhibition ofLactobacillus casei. In this test the fenamic acids and particularly the new class of the Cinnopentazon-antiphologistics (Scha 306, Scha 764 etc.) exhibit bacteriostatic properties of a medium intensity.

---

---

Alexander von Muralt zum 65. Geburtstag gewidmet.     

Über die bakteriostatische Wirkung von Anthocyanen und verwandten Stoffen

Summary Some anthocyanins and flavonols have been found to have no bacteriostatic effect on pathogenic micro-organisms.     

Coplanare Hetero-oligobasen (Phthalanilide), hochaktive Cytostatica

Summary Coplanar hetero-oligobases (phthalanilides), highly effective cytostatica. Bacteriometrical and physico- chemical tests on coplanar hetero-oligobases have shown the formation of a complex with DNA to be the cause of the cytostatic effect. For several of these compounds an evident correlation is demonstrated between bacteriostatic efficiency and reaction with DNA.

---

---

Ausgeführt mit Unterstützung durch den Krebsforschungsfonds des Kultusministeriums Nordrhein-Westfalen.     

Inattivazione della gramicidina dovuta alla conversione triptofano → N'-Formilchinurenina

Summary Treatment of gramicidin with ozone in formic acid leads to a tryptophan-N'-formylkynurenine conversion. Such a conversion causes a decrease of both bacteriostatic and haemolytic activities.     

o-Allyloxy-phenoxy-propanolamine,eine neue Gruppe adrenergischer β-Rezeptoren-Blocker

Summary The synthesis of a new class of adrenergic-receptor blocking agents based upon ao-allyloxy-phenoxy-propanolamine structure is described. The structure activity relationships were studied, and the structural elements responsible for an optimal pharmacological effect are discussed.     

The effect of X-rays and EMS on the behavior of the transposing element,TE98, inDrosophila melanogaster

Summary The sensitivity of TE98 (carryingw ^+R andrst ⁺) to X-rays does not differ significantly from the mutability ofcurled andkarmoisin loci. In addition no spontaneous mutants of TE98 were recovered, indicating its extreme stability. On the effect of EMS nowhite mutants were found supporting the view that thew ⁺ gene of TE98 is duplicated.     

Lipopeptaibols, a novel family of membrane active, antimicrobial peptides

Lipopeptaibols are members of a novel group of naturally occurring, short peptides with antimicrobial activity, characterized by a lipophilic acyl chain at the N-terminus, a high content of the turn/helix forming α-aminoisobutyric acid and a 1,2-amino alcohol at the C-terminus. The amino acid sequences range from 6 to 10 residues and the fatty acyl moieties from 8 to 15 carbon atoms. The peptide portion of lipopeptaibols can be shorter than those of the nonlipidated peptaibols that range from 10 to 19 amino acid residues. The longest peptides fold into a mixed 3₁₀/α helix, whereas the shortest peptides tend to adopt a β-turn/sheet structure. Using solution methodologies, a series of analogues of trichogin GA IV was synthesized which allowed determination of the minimal lipid chain and peptide main-chain lengths for the onset of membrane activity and exploitation of a number of spectroscopic techniques aimed at determining its preferred conformation under a variety of conditions and investigating in detail its mode of interaction with, and its effect on, the phospholipid membranes. Received 26 January 2001; received after revision 7 March 2001; accepted 15 March 2001     

Effects of the pyrimidine-containing cytochrome P-450 inhibitor,fenarimol, on the formation of 20-OH ecdysone in flies

Summary The effect of fenarimol, a pyrimidine-containing cytochrome P-450 inhibitor, was tested in vitro on brain-ring gland complexes ofCalliphora vicina (Dipt., Calliphoridae), and on microsomes prepared from the fat body of 0-h wandering stage larvae ofNeobellieria bullata (Dipt., Sacrophagidae). Fenarimol had no influence on the formation of ecdysone, but it was an effective inhibitor of cytochrome P-450-dependent ecdysone 20-monooxygenase.     

Über Lyco-marasmin,den Welkstoff ausFusarium lycopersiciSacc

Summary The effect of the wilt producing substance, lycomarasmine, isolated from cultures ofFus. lycopersici Sacc., is shown in three pictures. On hydrolysis lycomarasmine yields glycine, aspartic and (probably) pyruvic acid and ammonia. A hypothetical formula is given.     

1Alpha,25-dihydroxyvitamin D3 inhibits hepatic chromosomal aberrations, DNA strand breaks and specific DNA adducts during rat hepatocarcinogenesis

The possible promoting effect of streptozotocin (STZ; 65 mg/kg body weight, intraperitoneal)-induced diabetes during 2-acetylaminofluorene (2-AAF; 0.04% in basal diet)-initiated hepatocarcinogenesis and modulatory effect of 1α,25-dihydroxyvitamin D₃ (VD₃; 0.3 μg/0.1 ml in propylene glycol, per os) were investigated by monitoring chromosomal aberrations (CAs), DNA strand breaks and specific DNA adducts in rat liver. VD₃ treatment (twice a week) was started 4 weeks before the 2-AAF regimen and continued throughout the study. Aberrant metaphase chromosomes were counted from the regenerating hepatocytes 15, 30 or 45 weeks after STZ injection, while DNA strand break and adduct assays were performed 45 days post-STZ treatment. Dietary exposure to 2-AAF elicited a substantial increase in CAs and elevated the extent of DNA strand breaks and formation of N-(deoxyguanosin-8-yl)-2-aminofluorene. A promoting effect of STZ was evident from CAs coupled with DNA strand break analysis. VD₃ treatment substantially reducted 2-AAF+STZ-induced CAs as well as DNA strand breaks and adducts. Thus, VD₃ appears to be effective in suppressing liver-specific early chromosomal as well as DNA damage during the process of rat hepatocarcinogenesis initiated with 2-AAF and promoted by STZ contributing to its promise as a cancer chemotherapeutic agent. Received 27 April 2001; accepted 22 May 2001     

DNG1, a Dictyostelium homologue of tumor suppressor ING1 regulates differentiation of Dictyostelium cells

dng1 is a Dictyostelium homologue of the mammalian tumor suppressor ING gene. DNG1 protein localizes in the nucleus, and has a highly conserved PHD finger domain found in chromatin-remodeling proteins. Both dng1 disruption and overexpression impaired cell proliferation. In dng1-null cells, the progression of differentiation was delayed in a cell-density-dependent manner, and many tiny aggregates were formed. Exogenously applied cAMP pulses reversed the inhibitory effect caused by dng1 disruption on the aggregation during early development, but formation of tiny aggregates was not restored. dng1-overexpressing cells acquired the ability to undergo chemotaxis to cAMP earlier and exhibited enhanced differentiation. These phenotypes were found to be coupled with altered expressions of early genes such as cAMP receptor 1 (car1) and contact site A (csA). Furthermore, disordered histone modifications were demonstrated in dng1-null cells. These results suggest a regulatory role of dng1 in the transition of cells from growth to differentiation.Received 29 December 2004; received after revision 24 May 2005; accepted 26 May 2005     

Biological activity of flucycloxuron,a novel benzoylphenylurea derivative,onTenebrio molitor: comparison with diflubenzuron and triflumuron

Flucycloxuron, a novel benzoylphenylurea (BPU) derivative, exhibited insecticidal activity when injected into newly ecdysed pupae ofTenebrio molitor. Mortality occurs because of defective adult ecdysis. Treatment caused a reduction in both cuticle thickness and incorporation of¹⁴C-labelled precursor into chitin, although it had no significant effect on the protein synthesis. The potencies of other BPU compounds as inhibitors of chitin biosynthesis have been examined and results showed that diflubenzuron was less effective than either flucycloxuron or triflumuron.     

Zur Pharmakologie von Psilocybin,einem Wirkstoff ausPsilocybe mexicana Heim

Summary The active principle ofPsilocybe mexicana Heim, Psilocybin, is without marked effects on the isolated organs (seminal vesicle, intestine and auricle of the guinea pig; rat uterus) but exerts an actionin vivo which resembles a slight sympathetic stimulation. In unanaesthetized rabbits it produces mydriasis, tachycardia, tachypnea, hyperthermia and hyperglycemia, in unanaesthetized mice mydriasis and piloerection. The EEG (curarized rabbits) after 1–2 mg/kg Psilocybin shows an alerting pattern (disappearance of spindle activity and of slow waves). Spinal reflexes of the cat are predominantly enhanced. However, the motor activity of mice, rabbits and monkeys is unaffected or even slightly depressed. In anaesthetized cats and dogs Psilocybin affects blood pressure and heart rate, the effect depending on dosage and species.     

Hydroxyproline-rich glycoproteins in plant reproductive tissues: structure, functions and regulation

The plant reproductive process of pollination involves a series of interactions between the male gametophyte (the pollen grain or pollen tube) and extracellular matrix (ECM) molecules secreted by different cell types along the pollen tube growth pathway in the female organ, the pistil. These interactions are believed to signal and regulate the pollen tube growth process to effect successful delivery of the sperm cells to the ovules where fertilization takes place. Hydroxyproline-rich glycoproteins secreted by plant cells are believed to play a broad range of functions, ranging from providing structural integrity to mediating cell-cell interactions and communication. The pistil and pollen tube ECM is enriched in these highly glycosylated proteins. Our discussions here will focus on a number of these proteins for which most information has been available, from Nicotiana tabacum, its self-incompatible relative N. alata, and Zea mays. In addition, the regulation of the synthesis and glyco-modification of one of these proteins, TTS (transmitting tissue-specific) protein from N. tabacum will be discussed in the light of how differential glycosylation may be used to regulate molecular interactions within the ECM.     

Über die Wirkung von Diäthyläther auf die Aktivität der Glykogenphosphorylase und Phosphorylaseb-Kinase in Herz,Skeletmuskel und Leber der Ratte

Summary The rise of phosphorylasea activity and the activation of phosphorylaseb kinase in skeletal muscle of the rat in diethyl ether anaesthesia are inhibited by a blocker of the adrenergic receptors, pronethalol. This agent has no effect on the increased activity of liver phosphorylase under the same conditions. There are no effects of this anaesthetic on the phosphorylasea level in myocardium.