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At least 19 recordsLinked to original sources
PubMed1985

Clearance characteristics of des-AA fibrin and des-AABB fibrin, and thrombus-related uptake of des-AABB fibrin as compared to fibrinogen.

The following paper presents a short review of previous studies relating to the behaviour in man of radiolabelled fibrins des-AA and des-AABB, as compared to that of radiolabelled fibrinogen. Des-AA fibrin was eliminated with a half-life of 30 to 60 min in eight healthy controls, but its half-life was substantially shorter in eight fibrinaemic patients with no demonstrable fibrinolysis. Clearance of des-AABB fibrin was studied in thirteen patients with established venous thrombosis, all subjected to a concomitant fibrin(ogen) uptake test. There was no essential difference in its half-life in patients with a positive fibrinogen uptake test (n = 7) as compared to those with a negative test (n = 6). The metabolic half-life of des-AABB fibrin was 10 +/- 3.5 hrs. The uptake of labelled des-AABB fibrin by thrombi was similar to that of labelled fibrinogen during the first hours after injection, but only fibrinogen could reflect a continuous build-up of thrombi, due to its longer survival time.

Fibrin↗
PubMed1975

B-chain shortening of matrix-bound insulin with pepsin, II. Preparation and properties of camel des-pentapeptide (B26-30)- and des-PheB1-des-pentapeptide (B26-30)- insulin.

Digestion of matrix-bound camel insulin with pepsin was found to be restricted to the cleavage of the peptide bond between phenylalanine(B25) and tyrosine(B26). Purification of the camel des-pentapeptide(B26-30)-insulin obtained was achieved by gel filtration and ion exchange chromatography, yielding a molecularly uniform product. In the same way, camel des-PheB1-insulin prepared according to a method described for bovine insulin was hydrolyzed with pepsin and purified to give the des-PheB1-despentapeptide(B26-30)-insulin. The biological activity of these modified camel insulins was found to be as much reduced as the corresponding bovine insulin analogues. However, the reduced biological activity of camel des-PheB1-insulin (60%) was a contrast to the fully active bovine des-PheB1-insulin.

Amino Acids↗
PubMed1976

Synthetic metabolites of neurohypophyseal hormones. (Des-9-glycinamide)oxytocin and (des-9-glycinamide, des-8-leucine)oxytocin.

Syntheses and biological properties are reported for two analogs of oxytocin in which the glycinamide and the leucylglycinamide moiety, respectively, have been deleted from the parent hormone. Both [des-9-glycinamide]oxytocin and [des-9-glycinamide,des-8-leucine]oxytocin are weak agonists in the rat uterotonic and antidiuretic assays but possess no detectable rat pressor activity. In addition, [des-9-glycinamide]oxytocin is an inhibitor of the oxytocin-induced vasodepressor response in fowl but is a potent agonist in the hydroosmotic assay of the toad urinary bladder.

Animals↗
PubMed1994

Proteinuric potentials of angiotensin II, [des-Asp1]-angiotensin II, and [des-Asp1, des-Arg2]-angiotensin II in rats.

To compare proteinuric potentials among angiotensin II (ANG II) and its fragments, [des-Asp1]-angiotensin II (ANG III) and [des-Asp1, des-Arg2]-angiotensin II (ANG IV), the peptide was intravenously infused for 30 min at doses of 0.015, 0.05, 0.15, 0.45 and 1.45 nmol/kg body weight/min. The infusion of ANG II and ANG III increased the fractional clearance of albumin in a dose-dependent manner: most extensively for ANG II, and moderately for ANG III. In contrast, the infusion of ANG IV hardly showed any proteinuric action, even at the maximal dose of 1.45 nmol/kg body weight/min. These results denoted that the cleaving of the N-terminal aspartic acid1 from ANG II weakened the proteinuric action in the glomeruli, and the further cleaving of the N-terminal arginine from ANG III led to a complete loss of proteinuric action in the glomeruli.

Angiotensin II↗
PubMed1981

Identification of classical anaphylatoxin as the des-Arg form of the C5a molecule: evidence of a modulator role for the oligosaccharide unit in human des-Arg74-C5a.

A functionally active and potentially lethal fragment of the fifth component of complement (C5) is generated during complement activation in serum from animals of various species. This factor, termed the "classical" anaphylatoxin, was isolated from porcine serum and was identified chemically as the des-Arg derivative of the well-characterized C5a molecule. Unlike the C3a and C4a anaphylatoxins, porcine C5a does not require the COOH-terminal arginyl residue for spasmogenic activity. Further degradation of porcine des-Arg(74)-C5a by carboxypeptidase Y removed glycine-73 and leucine-72 and decreased the intrinsic spasmogenic activity by >90%. Hence, we conclude that, although the arginyl residue is not essential, the COOH-terminal sequence Leu-Gly-Arg contributes structural information that accounts for >90% of C5a activity. Human des-Arg(74)-C5a, like its porcine counterpart, has instrinsic anaphylatoxin activity; however, higher concentrations were needed to contract the guinea pig ileal tissue (i.e., 1 muM for human des-Arg(74)-C5a versus 1 nM for porcine des-Arg(74)-C5a). Furthermore, the des-Arg form of human C5a was only 0.1% as active as porcine des-Arg(74)-C5a for enhancing vascular permeability in guinea pig skin. In addition to these biological differences, numerous chemical differences exist between the human and porcine des-Arg(74)-C5a molecules, the most prominent feature being an oligosaccharide entity associated uniquely with the human C5a. When the oligosaccharide unit of human des-Arg(74)-C5a was removed by glycosidases, leaving a single glucosamine residue attached to the side chain of asparagine-64, activity was enhanced. The human des-Arg(74)-C5a molecule devoid of the complex oligosaccharide unit exhibited 10-fold stronger spasmogenic activity and 20- to 50-fold greater permeability-enhancing activity than did human des-Arg(74)-C5a containing the oligosaccharide. Consequently, the oligosaccharide associated with human C5a modulates or suppresses potentially harmful activities of this anaphylatoxin. The relatively high levels of spasmogenic activity associated with porcine des-Arg(74)-C5a indicate that this factor is poorly controlled by endogenous serum carboxypeptidase, whereas human C5a is virtually inactivated by the enzyme. Hence, the influence of this oligosaccharide in suppressing human des-Arg(74)-C5a activity is of major physiologic importance in protecting man from potentially toxic effects of this complement factor.

Amino Acid Sequence↗
PubMed1983

Diethylstilbestrol (DES) quinone: a reactive intermediate in DES metabolism.

The quinone of E-diethylstilbestrol (DES), a postulated metabolic intermediate derived from DES, has been synthesized by oxidation of DES in chloroform using silver oxide. The reaction product was structurally characterized by infrared, ultraviolet, nuclear magnetic resonance, and mass spectrometry. The product of oxidation of DES by hydrogen peroxide, catalyzed by horseradish peroxidase and also by rat uterine peroxidase, was shown to be identical with synthetic DES quinone based on identical u.v. spectra and on identical decomposition products. DES quinone was stable only in non-protic solvents such as chloroform. In acids, bases or protic solvents, DES quinone rearranged to Z,Z-dienestrol (beta-DIES). The half-life of DES quinone in water was approximately 40 min; in methanol it was approximately 70 min. Bacterial mutagenicity (Ames) tests did not indicate that DES quinone had mutagenic or genotoxic activity. However, DES quinone was found to bind to calf thymus DNA without any enzyme mediation at levels significantly above the binding of DES under the same conditions. Based on the binding of DES quinone to DNA, this intermediate must be considered as a possible carcinogenic metabolite of DES.

Animals↗
PubMed2003

Cardiac effects of ghrelin and its endogenous derivatives des-octanoyl ghrelin and des-Gln14-ghrelin.

The mechanisms underlying the cardiac activities of synthetic growth hormone secretagogues (GHS) are still unclear. The natural ligand of the GHS receptors, i.e. ghrelin, classically binds the GHS receptor and exerts endocrine actions in acylated forms only; its cardiovascular actions still need to be investigated further. In order to clarify these aspects, we studied the effects of either the synthetic peptidyl GHS hexarelin (1 microM), or the natural ghrelin (50 nM) and the endogenous ghrelin derivatives des-Gln14-ghrelin (1-100 nM) and des-octanoyl ghrelin (50 nM), on the tension developed by guinea pig papillary muscle and on L-type Ca2+ current (ICa) of isolated ventricular cells. The binding of these molecules to ventricular cell membrane homogenates was also studied. We observed that all peptides reduced the tension developed at low frequencies (60-120 beats/min) in a dose-dependent manner. No alteration in cardiac contractility was induced by des-Gln14-ghrelin or des-octanoylated ghrelin when the endocardial endothelium had been removed or after cyclooxygenase blockade. Pretreatment with tyramine (2 microM) had no effect on the inotropic response induced by des-Gln(14)-ghrelin. No significant effect on I(Ca) of isolated ventricular cells was observed in the presence of des-Gln14-ghrelin (100 nM). The order of potency on the tension of papillary muscle was: des-octanoyl ghrelin > ghrelin = des-Gln14-ghrelin > hexarelin. This gradient of potency was consistent with the binding experiments performed on ventricular membranes where either acylated or unacylated ghrelin forms, and hexarelin, recognized a common high-affinity binding site. In conclusion, ghrelin, des-Gln14-ghrelin and des-octanoyl ghrelin, show similar negative inotropic effect on papillary muscle; as des-octanoyl ghrelin is peculiarly devoid of any GH-releasing activity, the cardiotropic action of these molecules is independent of GH release. The binding studies and the experiments performed both on the isolated cells and on papillary muscle after endothelium removal or cyclooxygenase blockade indicate that the cardiotropic action of natural and synthetic ghrelin analogues reflects the interaction with a novel GHS receptor (peculiarly common for ghrelin and des-octanoyl ghrelin), leading to release of cyclooxygenase metabolites from endothelial cells, as indicated by direct measurement of prostacyclin metabolite 6-keto-PGF(1alpha).

Animals↗
PubMed1977

Stimulation of corticosteroid biosynthesis by angiotensin I [des-asp1]angiotensin I, angiotensin II and [des-asp1]-angiotensin II in bovine adrenal fasciculata cells.

The effect of angiotensin I (AI), angiotensin II (AII), [des-asp1]AI, [des-asp1]AII and [des-asp1-arg2]AII on corticosteroid production in isolated fasciculata cells from bovine adrenals has been studied. AII and [des-asp1]AII in concentrations ranging from 10(-9)M to 10(-6)M had a potent stimulatory effect on steroid biosynthesis. The dose-response curves for both peptides were identical. AI was about 3 times less potent than AII and [des-asp1]AII. The effect of AI was not due to its conversion to AII. [Des-asp1]AI was as active as AI. No significant conversion to [des-asp1]AII was observed. [Des-asp1-arg2]AII had only a minimal effect on steroidogenesis. The structural analog [sar1,-ala8]AII inhibited all angiotensins specifically and competitively. The affinity of the cellular binding site was higher for AII and [des-asp1]AII than for [sar1,ala8]ALL, but lower for AI and [des-asp1]AI than for the inhibitor. Combination of submaximal doses of AI and AII resulted in an additive effect on steroid production. By contrast, combination of maximal doses of both peptides had the same effect as AII alone. These data demonstrate a potent steroidogenic activity for AII as well as AI, [des-asp1]AI and [des-asp1]AII in bovine adrenal fasciculata cells. A common receptor site for all four peptides is suggested.

Adrenal Cortex Hormones↗
PubMed1993

The determination of diethylstilbestrol (DES) in the faeces and tissues of chickens treated with DES and in the faeces and tissue samples of calves, lambs and chickens collected from various areas of Turkey.

Diethylstilbestrol (DES) analyses were carried out on muscle, liver, kidney and faeces samples of 20 control and 20 experimental broilers to which 5 mg DES/day had been given orally for a period of 7 days. The treated samples were analysed using the Radioimmunoassay method. The removal time of DES from the tissues was determined. Five days following the final administration of DES, its faecal concentration was 151 ppb. However, 7 days after the final administration faecal DES concentrations increased again. On the first day after the final DES administration, DES concentrations in the liver, muscle and kidney were 0.78, 0.74 and 1.33 ppb, respectively. While these values measured on the final day were within the range of the control values. There was an increase of DES in plasma at the end of the experimental period. A total of 1811 muscle, liver, kidney and faeces samples of calves, lambs and chickens and feed samples collected from various areas in Turkey were analysed for the presence of DES. Positive samples for chicken feed was 36.9%. Also 1.9% of the chicken faeces samples were DES positive. All other samples were negative for DES.

Animals↗
PubMed1996

Low level cyclic adenosine 3',5'-monophosphate accumulation analysis of [des-His1, des- Phe6, Glu9] glucagon-NH2 identifies glucagon antagonists from weak partial agonists/antagonists.

[des-His1, des-Phe6,Glu9]Glucagon-NH2 is a newly designed glucagon antagonist. This analog has a binding IC50 of 48 nM (compared to glucagon IC50 of 1.5 nM) and demonstrates pure antagonism in an adenylate cyclase assay. Although the number of glucagon antagonists has grown rapidly recently, closer examination suggested that many of these antagonists retained very low, almost imperceptible levels of cAMP accumulation that were sufficient to elicit an in vivo biological response. To investigate more carefully this secondary biological signal, we measured cAMP accumulation in a revised assay using isolated hepatocytes in the presence of the phosphodiesterase (PDE) inhibitor Rolipram. The PDE inhibitors Rolipram and isobutyl-1-methylxanthine (IBMX) increased the sensitivity of the cAMP accumulation assay from approximately 10-fold for the native hormone to 35-fold above basal levels. On the other hand, amrinone, another PDE inhibitor, did not affect the cAMP accumulation caused by glucagon. The use of PDE inhibitors indicated that three glucagon analogs that had previously been reported to have strong antagonist properties in classical adenylate cyclase assays were actually weak partial agonists in this new assay system. [N alpha-Trinitrophenyl-His1, homo-Arg12]glucagon, [des-amino-His1,D-Phe4,Tyr5, Arg12, Lys17,18,Glu21]glucagon, and [des-His1,Glu9]glucagon-NH2 demonstrated 233%, 21%, and 5.5% cAMP accumulation relative to the native hormone in the presence of 25 microM Rolipram. On the other hand, [des-His1,des-Phe6,Glu9]glucagon-NH2, a newly designed glucagon antagonist, did not activate adenylate cyclase in the presence of Rolipram up to a maximal physiological concentration of 1 microM, indicating that it was a pure antagonist of glucagon-induced adenylate cyclase activity and also the first one in this class. This compound and others were tested in a glycogen phosphorylase assay. As [des-His1,des- Phe6,Glu9]glucagon-NH2 did not activate phosphorylase activity, it was chosen as our candidate for in vivo testing in streptozotocin-induced diabetic rats. An initial dose of 0.75 mg/kg was found to cause the greatest lowering of blood glucose levels (to 63% of the initial levels in 15 min) when the bolus was followed by continuous infusion of 25 micrograms/kgxmin for 1 h.

1-Methyl-3-isobutylxanthine↗
PubMed2002

Morphology of accessory sex organs from neonatally DES- and DES-dp-injected mouse.

The neonatal estrogen induces morphological changes in accessory sex organs. We have reported that papillary proliferation in prostates and squamous metaplasia of the epithelium in seminal vesicle occurred and inflammatory cells have emigrated to the lumen through the stroma and the epithelium of organs from neonatal mice treated with beta-estradiol 17-cypionate. In this study, we observed the different effect between neonatal DES and DES-dp on morphological changes in accessory sex organs of mice. After 25 weeks, neonatal estrogen injections induced the infiltration of inflammatory cells in the ventral prostate and squamous metaplasia in the epithelium of seminal vesicles. It was observed that the inflammatory cells have already infiltrated into prostates from DES-dp injected mice after 5 weeks. But DES did not cause the changes in prostates. DES induced organs from a half of mice to involute and inflammatory cell to infiltrate into the epithelium. But these were not seen in organs from another half of mice. DES-dp occurred similar effect of beta-estradiol 17-cypionate on the male accessory sex organs. It remained to be seen whether DES could have estrogen action on accessory sex organ.

Animals↗
PubMed1970

Structure des parois cellulaires des nocardia. I-isolement et composition des parois de Nocardia kirovani.

Nocardia kirovani cell walls possess a lipidic fraction, a lipolysaccharidic fraction and a peptidoglycan. The lipidic part is composed of glycerides, C(16) and C(18) free fatty acids, nocardic acids and of a carotenoid pigment. The lipopolysaccharidic part is composed of an arabinogalactan esterified by nocardic acids. The glycan strand consists of alternating 1-->4 linked N-acetylglucosamine and N-glycolylmuramic acid residues substituted by a peptide subunit in which the aminoacids Ala, Glu, meso-Dap are present in the molar proportions 1,7:1,2:1.

Journal Article↗
PubMed1971

Recherches sur les enzymes catalysant la biosynthese des acides phénoliques chez Quercus pedunculata (EHRH.): I - Formation des premiers termes des series cinnamique et benzöique.

Occurence of PAL, cinnamate-hydroxylase and p-coumarate-hydroxylase, is found in cell-free extracts from Quercus pedunculata roots; moreover, an enzyme system which catalyzes benzoïc acid formation from cinnamic acid is caracterized for the first time. Role of these enzymes and their interactions within the same organ are discussed.

Journal Article↗
PubMed1998

Colonoscopic screening in first-degree relatives of patients with 'sporadic' colorectal cancer: a case-control study. The Association Nationale des Gastroentérologues des Hôpitaux and Registre Bourguignon des Cancers Digestifs (INSERM CRI 9505)

BACKGROUND & AIMS: A screening policy has not been well defined in first-degree relatives of patients with sporadic colorectal cancer. This study estimated the risk of colorectal adenoma in a cohort of individuals with only 1 affected first-degree relative. METHODS: A total of 476 first-degree relatives (age, 40-74 years) of 195 patients with sporadic colorectal cancer were offered a colonoscopy. Each examined relative was matched with 2 controls for age, sex, symptoms, and center. The prevalence of colorectal adenomas was compared using a multiple logistic regression analysis. RESULTS: In 185 relatives, odds ratios were 1.5 (95% confidence interval [CI], 1.0-2.4) for adenomas, 2.5 for large adenomas (95% CI, 1.1-5.4), 1.2 for small adenomas (95% CI, 0.7-1.9), and 2.6 (95% CI, 1.3-5.1) for high-risk adenomas (> or = 1 cm in size and/or with a villous component). The prevalence of high-risk adenomas in relatives was higher when the index patient was younger than 65 years, was male, and had distal rather than proximal cancer. CONCLUSIONS: Subjects with only 1 affected first-degree relative are at increased risk for developing large adenomas.

Adenoma↗
PubMed2004

[The chemical entries of Charles Gerhardt in Dictionnaire universel des Sciences, des Lettres et des Arts by Marie-Nicolas Bouillet].

Charles Gerhardt (1816-1856) is known as the founder of modern organic chemistry. He wrote the chemical entries of the dictionary managed by Marie-Nicolas Bouillet (1798-1864), who was a philosopher. This great deal of work was done between 1849 and 1853. It accounts for didactic and militant purposes of Gerhardt. The whole entries set up a true treatise of chemistry, and reflect the synthetic mind of their author.

Chemistry↗
PubMed1990

[Validation and environmental control of preparation operations. Fifth communication of the Comite des Laboratoires et Services Officiels de Controle des Medicaments et de la Section des Pharmaciens de l'Industrie'-F.I.P, May 1990].

The many different check-points concerning the complementary activities of validation and monitoring of aseptically processed pharmaceutical preparations are described. The features are based on the official and current GMP guidelines. These are outlined in practical terms according to the personal experience of the authors and manufacturing specialists who were consulted.

Drug Industry↗