3,5-Dibromo-2′-chloro-4′-isothiocyanatosalicylanilide,a potent anthelminitic

Summary The compound, 3,5-dibromo-2-chloro-4-isothiocyanatosalicylanilide, has been tested against various nematode and cestode parasites in experimental and domestric animals. It shoved 100% activity againstAncylostoma ceylanicum, A. tubaeformis, Syphacia obvelata, Ascaridia galli, Toxocara spp.,Toxascaris sp.,Gnathostoma spinigerum, Hymenolepis nana, Raillietina spp. andTaenia spp. in doses 25–70 mg/kg given in single or multiple administrations.Acknowledgments. We express sincere thanks to Dr Nitya Nand, F.N.A., CDRI, Lucknow, for his keen interest in the work, to Dr B. N. Dhawan, F.N.A. for providing informations about general pharmacology of the compound, and to Dr R. K. Chatterjee and Dr P. K. Murthy for carrying out antifilarial sreening. Technical assistance of Mr S. C. Bhar and Mr S. Ram is acknowledged.     

Einbau des 2′,4,4′,6′-Tetrahydroxy-chalkon-2′-glucosid-[β-14C] in Isoflavone

Summary 2,4,4,6-Tetrahydroxychalcone-2-glucoside-[-¹⁴C] is incorporated into biochanin-A in chana germ (Cicer arietinum L.) without randomization of the radioactivity. Possibly a very low incorporation into formononetin occurs also. After administration of the chalcone a large part of the activity is bound to the acid insoluble residue of the cicer shoots (lignin-like substances) in an (as yet) undetermined manner. This binding also occurs in heat denatured homogenates.

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VI. Mitt. Zur Biogenese der Isoflavone. V. Mitt.H. Grisebach undG. Brandner, Biochim. biophys. Acta60, 51 (1962).     

Fever produced in rabbits by N6, O2′-dibutyryl adenosine 3′, 5′-cyclic monophosphate

Zusammenfassung Die Injektion von N⁶-2-O-Dibutyryl-adenosin-3 5-monophosphat in den lateralen Hirnventrikel von Kaninchen führt zu einer langanhaltenden Fieberreaktion, was vermuten lässt, dass zyklisches Adenosin-35-monophosphat als weiterer Mediator in der Genese des Fiebers fungiert.     

Research Articles¶Naturally occurring 2′-O-methylpurine nucleosides with hypotensive properties

2′-O-Methylinosine (1) has been isolated for the first time and shown to be an intrinsic hypotensive principle. Its probable in vivo precursor, 2′-O-methyladenosine (3), showed stronger and even orally potent hypotensive activity. Resistance of the methyladenosine (3) against adenosine deaminase is thought to contribute to its long-lasting activity. The effect of both nucleosides (1 and 3) was not accompanied with any significant change in heart rate, which is often observed with adenosine. Received 2 October 1997; accepted 28 October 1997     

Female sex pheromone of the longhorn beetleMigdolus fryanus Westwood: N-(2′S)-methylbutanoyl 2-methylbutylamine

The first known long-range female-released sex pheromone for the family Cerambycidae is reported fromMigdolus fryanus, a sugarcane pest in South America. Although two female-specific compounds, namely, N-(2S)-methylbutanoyl 2-methylbutylamine and N-formyll-isoleucine methyl esters were identified, field tests with synthetic chemicals revealed that only the amide was active and that the amino acid derivative neither increased or decreased trap catches by the amide. This is the first identification of amide as a sex pheromone.     

Regional pattern and heat-resistance of brain 5′-deoxy-5′-methylthioadenosine phosphorylase

Summary The distribution of 5-deoxy-5-methylthioadenosine (MTA) phosphorylase in 10 pig brain areas was determined. The observed regional differences of the enzymatic activity seem to reflect more the pattern of brain spermine distribution rather than that of spermidine. Moreover, comparative studies on the heat-resistance of MTA phosphorylase extracted from the whole brain of various species suggest structural differences in the enzyme molecules occurring in the brains of different animals.     

Synthesis of 5′-deoxypyridoxal derivatives

Summary A convenient synthesis of 5-deoxypyridoxal derivatives is described. The method involves catalytic hydrogenolysis of the corresponding 5-phosphorylated derivatives; products are obtained in high yields.Supported by PHS Grant No. 5429-16-9.     

Effects of N2, O2′-dibutyril cyclic GMP on the nucleoside phosphotransferase activity of the retina of the chick embryos

Summary In the retina of the chick embryo, 2 different forms of nucleoside phosphotransferase take part in the phosphorylation of thymidine. One is an unstable form with higher molecular weight. The other with lower m. wt is a stable form. This paper shows that N², O²-dibutyril cyclic GMP causes a marked decrement of the activity of the unstable nucleoside phosphotransferase.     

Effect of spike disease on the 5′-and 3′-nucleotidase activities in sandal plants

Summary In the sandal plant affected by spike disease, caused by mycoplasma-like organisms, the changes occurring in the 5-and 3-nucleotidase activities were studied and their possible significance discussed.     

A human homolog of the yeast gene encoding tRNA 2′-phosphotransferase: cloning,characterization and complementation analysis

The Saccharomyces cerevisiae TPT1 gene plays a role in removing the 2-phosphate from ligated tRNA during the maturation of pre-tRNA. Here we reported the cloning and characterization of the human TRPT1 gene as a homolog of yeast TPT1. The TRPT1 gene is located at human chromosome 11q13 and encodes a polypeptide of 253 amino acids. BLAST searches with its amino acid sequence revealed the ubiquitous occurrence of TRPT1 homologs and their functional relationships with the presence of the DUF60/KptA domain. Northern analysis demonstrated that the gene is primarily expressed in heart and skeletal muscle, with lower or undetectable levels in other tissues studied. A plasmid-shuffling experiment showed that the human TRPT1 gene could complement the tpt1 mutation in S. cerevisiaeReceived 19 March 2003; received after revision 25 April 2003; accepted 22 May 2003     

Formation of 4,4′-methylene-bis(2-chloroaniline)-DNA adducts in yeast expressing recombinant cytochrome P450s

N-Oxidation of 4,4-methylene-bis(2-chloroaniline) (MBOCA) may lead to formation of DNA adducts. To determine if cytochrome P450s are involved in the formation of MBOCA derived-DNA adducts, yeast strains expressing rodent P450s were exposed to MBOCA, and³²P-postlabelling of nucleotides from yeast genomic DNA was done. Chromatographic analysis on PEI cellulose showed that, upon exposure to MBOCA for 1 h, nine DNA adducts were formed in yeast expressing phenobarbital-inducible rabbit P450 2B5. With a 4-h-exposure, all adducts increased in parallel. In cell-free experiments, the incubation of MBOCA with phenobarbital-induced rat microsomal fraction followed by incubation with thymus DNA, led to the formation of more than ten DNA adducts. When yeast expressing 3-methylcholanthrene-inducible rat P450 1A1 was exposed to MBOCA, one major and two minor adducts were formed. No adducts were detected in control yeast. These results show that recombinant rabbit P450 2B5 exhibits a potential activation of MBOCA and that rat P450 1A1 has some effect. The use of yeast expressing recombinant P450s and the technique of³²P-postlabelling facilitates a simple search for chemicals with carcinogenic potential.     

Effect of glucose and phloretin-2′-β-D-glucose (phloridzin) on in vitro fertilization of mouse ova

Summary The fertilization ratio of mouse ova in vitro decreased when glucose concentration in the medium was lowered. However, the addition of phloretin-2--D-glucose (phloridzin), known as a glucose uptake inhibitor, restored the fertilization ratio back to the control level. The glucose moiety of the phloridzin seemed to be responsible for this effect.     

5′-Methyl-cytosine in the macronulear DNA ofBlepharisma japonicum

Summary Brief report on the presence of 5-methyl-cytosine as a minor base (0.56%) in the macronuclear DNA of the ciliate orotozoanBlepharisma japonicum. The evidence comes from electrophoresis of macronuclear DNA digested by appropriate restriction endonucleases and high-performance liquid chromatography     

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.      

Reaction of pyridoxal-5′-phosphate with γ-carboxyglutamic acid

Summary Pyridoxal-5-phosphate (PLP) reacts with -carboxyglutamic acid (Gla) to form a stable complex absorbing at 325 nm. It is suggested that a condensation occurs in which the formyl group of PLP reacts with the -amino group and the carbon atom of Gla to give a pyrrolidine derivative.     

Reduction of adenylylsulfate and 3′-phosphoadenylylsulfate in phototrophic bacteria

Summary Extracts of 14 species of phototrophic bacteria, partly grown with different sulfur compounds, were tested for their ability to form volatile sulfur compounds from adenylylsulfate (APS) and 3-phosphoadenylylsulfate (PAPS). The Rhodospirillum species showed marked activities with both APS and PAPS while the Rhodopseudomonas species seem to prefer PAPS. the Chromatiaceae exhibited the strongest activities with APS, whereas Chlorobium limicola had equally high activity with PAPS.We thank J. F. Imhoff for skilful assistance and the Deutsche Forschungsgemeinschaft for financial support.     

Crystal and molecular structure of 3, 3′-dibromobenzophenone

Résumé La structure du cristal de 3, 3-dibromobenzophénone a été définie par l'emploi de données obtenues par rayons X dans trois dimensions. Les distances et les angles de liaison ont été obtenus et l'on a trouvé que deux anneaux de phényle de la molécule ne sont pas dans le même plan, l'angle compris entre eux étant de 39,9°.     

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.     

Adenosine 3′,5′-cyclic monophosphate levels in maize roots

Summary Endogenous levels of adenosine 3,5-cyclic monophosphate (cAMP) in maize (cv. LG 11) root cells, grown in light and dark conditions, were found to be 309 and 387 pmoles/g of fresh tissue respectively.This investigation was partially supported by USA National Science Foundation grant No. CDP 8004200 to the senior author.