A new semisynthetic ergot peptide alkaloid: DCN 203-922

Summary We report the synthesis, stereochemistry and preliminary pharmacological evaluation of DCN 203-922, a novel ergot alkaloid of the cyclol type, which contains in its peptide moiety the uncommon amino acid L-allo-isoleucine.Part of this paper was reported by this author at the Herbstversammlung der Schweizerischen Chemischen Gesellschaft, Bern, in October 1986.     

Action and interaction of two alpha 1-adrenoceptor agonists, methoxamine and St 587, on the rabbit's blood pressure and EEG

In rabbits methoxamine reversed the vasopressor effect of St 587 and abolished the EEG synchronizing action of St 587. The interaction on the blood pressure could be ascribed either to the different chemical structures of St 587 and methoxamine or to partial agonistic properties of St 587. The interaction on the EEG appears to be more complex.     

Cyclic and linear vasopressin V1 and V1/V2 antagonists containing arginine in the 4-position

Summary Substitution of arginine for glutamine in the 4-position of a vasopressin V₁ antagonist has been reported to turn it into an agonist. We resynthesized this 4-arginine analog and synthesized additional cyclic and linear vasopressin antagonists containing a 4-arginine. The presence of a 4-arginine in the resynthesized and new analogs had relatively minor effects on their antivasopressin V₁ and V₂ antagonistic potencies.     

Self-labeling of human polymorphonuclear leucocyte myeloperoxidase with125iodine

In order to obtain a radioimmunoassay (RIA) technique for the measurement of human plasma myeloperoxidase (MPO), we purified the enzyme from polymorphonuclear granulocytes (neutrophils), and compared three methods of labeling it with¹²⁵Iodine: chloramine T, lactoperoxidase, and an original technique of self labeling based on the ability of the enzyme to oxidize and bind¹²⁵I in the presence of H₂O₂. The chloramine T technique produced a degraded protein, as well shown by a high non-specific binding of tracer to antibody. The lactoperoxidase technique did not succeed in labeling MPO with an adequate specific activity. In contrast, the self-labeling method gave a stable tracer with a specific activity of 23 Ci/gmg MPO (85 MBq), a satisfactory level of immunoreactivity, and a low-specific binding (3%). After labeling, purification of tracer was achieved by gel filtration chromatography in phosphate buffer (0.05 M; pH7) to which 0.1% poly-L-lysine was added. The labeled molecule remained stable for 40 days and could be used for RIA with a polyclonal antibody raised in rabbits.     

Volatile constituents of wolf (Canis lupus) urine as related to gender and season

Summary The volatile constituents of wolf urine were examined via capillary gas chromatography and compared among male, female, and castrate male. Several compounds including methyl isopentyl sulfide, 3,5-dimethyl-2-octanone, and acetophenone were clearly associated with the gender of the animal and many displayed a seasonal dependence. In addition, 2 long-chain aldehydes isolated from urine samples by an HPLC procedure also correlated with the endocrine status of the animal.This work was partially funded by the US Fish and Wildlife Service.We thank Dr Sharon L. Smith of IBM Instruments, Danbury, Connecticut, for recording spectra of some wolf urinary constitutents on an IBM Fourier-transform IR spectrometer.No such compounds were observed in any other animal species during our previous work with several mammals.     

Stimulation of histamine synthesis in rat mast cells by compound 48/80 in vitro

The histamine content of rat peritoneal fluid cells is doubled within 20 min by 0.5 microgram/ml of compound 48/80. Histamine catabolism inhibitors do not reproduce this effect; cells pre-incubated with alpha-fluoromethylhistidine are unresponsive to compound 48/80 which therefore activates pre-formed histidine decarboxylase rather than 'inducing' it. Non-mast cells showed no change after treatment with compound 48/80.     

Biology of halophilic bacteria,Part II

Archaebacteria (archaea) are comprised of three groups of prokaryotes: extreme halophiles, methanogens and thermoacidophiles (extreme thermophiles). Their membrane phospholipids and glycolipids are derived entirely from a saturated, isopranoid glycerol diether,sn-2,3-diphytanylglycerol (archaeol) and/or its dimer, dibiphytanyldiglyceroltetraether (caldarchaeol). In extreme halophiles, the major phospholipid is the archaeol analogue of phosphatidylglycerolmethylphosphate (PGP-Me); the glycolipids are sulfated and/or unsulfated glycosyl archaeols with diverse carbohydrate structure characteristic of taxons on the generic level. Biosynthesis of these archaeol-derived polar lipids occurs in a multienzyme, membrane-bound system that is absolutely dependent on high salt concentration (4 M). The highly complex biosynthetic pathways involve intermediates containing glycerol ether-linked C₂₀-isoprenyl groups which are reduced to phytanyl groups to give the final saturated polar lipids. In methanogens, polar lipids are derived both from archaeol and caldarchaeol, and thermoacidophiles contain essentially only caldarchaeol-derived polar lipids. The function of these membrane polar lipids in maintaining the stability, fluidity and ionic properties of the cell membrane of extreme halophiles, as well as the evolutionary implications of the archaeol and caldarchaeol-derived structures will be discussed.     

Cold exposure: Effects on hepatic tryptophan oxygenase and tyrosine aminotransferase,plasma tryptophan and tyrosine,and brain monoamines

Résumé L'exposition des souris à une basse temp'erature a abouti à la production rapide de tryptophane oxygénase et de tyrosine aminotransférase. Malgré l'augmentation de l'activité enzymatique, les niveaux plasmatiques de tryptophane et de tyrosine furent augmentés d'une manière significative pendant le temps de l'exposition. Les niveaux de norepinéphrine et de sérotonine du cerveau n'en ont cependant pas été affectés.

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Acknowledgment. The authors would like to thank Army SP'sM. Devine, T. Nielson, andG. Johnson for expert technical assistance.

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In counducting the research described in this report, the investigators adhered to the Guide for Laboratory Animal Facilities and Care, as promulgated by the Committee on the Guide for Laboratory Animal Facilities and Care of the Institute of Laboratory Animal Resources, National Academy of Sciences — National Research Council.