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  • Artikel  (30)
  • Coleoptera
  • Saccharomyces cerevisiae
  • kinetics
  • stability
  • Springer  (30)
  • American Geophysical Union
  • Copernicus
  • INGV
  • Institute of Electrical and Electronics Engineers (IEEE)
  • 1990-1994  (30)
  • Medizin  (30)
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  • Artikel  (30)
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  • 1
    Digitale Medien
    Digitale Medien
    Vergleich der biologischen Aktivität und Stabilität von Menadion und Menadiol bei Hühnerküken (1990)
    Springer
    European journal of nutrition 29 (1990), S. 219-228 
    Details
    ISSN: 1436-6215
    Schlagwort(e): Vitamin K ; Menadion ; Menadiol ; Bioverfügbarkeit ; Stabilität ; Geflügel ; vitamin K ; menadione ; menadiol ; bioavailability ; stability ; poultry
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Land- und Forstwirtschaft, Gartenbau, Fischereiwirtschaft, Hauswirtschaft , Medizin
    Beschreibung / Inhaltsverzeichnis: Summary A bioassay of vitamin K is described, based on the prothrombin clotting time of 3-week-old, vitamin-K-depleted, and cumatetralyl-sensitized male broiler chicks, using a homologous thrombokinase preparation. With this test it could be shown that the diacetate and dibutyrate esters of menadiol are vitamin-K-active. The bioactivity of menadione from these menadiolesters amounted to about 70 % of the standard menadione from a coated menadione sodium bisulfite (Dohyfral). Menadiol seems to be temperature-resistant under such conditions, whereby two uncoated MSB preparations lost about 60 % of their activity.
    Notizen: Zusammenfassung In einem biologischen Testverfahren an Cumatetralyl sensibilisierten Küken konnte in 3 Versuchen anhand des Parameters Thromboplastinzeit mit homologer Thrombokinase gezeigt werden, da\ Menadioldiacetat und Menadioldibutyrat Vitamin-K-wirksam sind. Die biologische Wirksamkeit von Menadion aus diesen Menadiolestern betrug ca. 70 % der Menadionaktivität aus gecoatetem Menadionbisulfit (Dohyfral®). Im Gegensatz zu 2 ungeschützten MSB-Präparationen, welche bei Wärmebelastung ca. 60 % ihrer ursprünglichen Wirkung verloren, waren die Menadiolester temperaturstabil.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02023079
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  • 2
    Digitale Medien
    Digitale Medien
    Biosynthesis of 1-alkenes in the defensive secretions ofTribolium confusum (Tenebrionidae); stereochemical implications (1990)
    Springer
    Cellular and molecular life sciences 46 (1990), S. 700-704 
    Details
    ISSN: 1420-9071
    Schlagwort(e): Coleoptera ; Tenebrionidae ; Tribolium confusum ; defesive secretion ; biosynthesis of 1-alkenes ; oxidative decarboxylation ; anti-elimination
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Medizin
    Notizen: Summary The terminally unsaturated hydrocarbons of the defensive secretion ofTribolium confusum are biosynthesized from fatty acids by oxidative decarboxylation. The process involves an enantiospecific cleavage of the C−H bond of thepro-(S) C(3)−H atom and simultaneous decarboxylation of the acid into an 1-alkene and carbon dioxide via ananti-periplanar transition state geometry (anti-elimination). The stereochemistry of this biotranformation is identical in all respects with the same reaction in higher plants. The mechanism seems to be of general importance for the biosynthesis of many vinylic substructures of natural products from oxygen-containing precursors.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01939939
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  • 3
    Digitale Medien
    Digitale Medien
    Cantharidin production in a blister beetle (1993)
    Springer
    Cellular and molecular life sciences 49 (1993), S. 171-174 
    Details
    ISSN: 1420-9071
    Schlagwort(e): Coleoptera ; Meloidae ; Epicauta funebris ; chemical defense ; biosynthesis ; terpenoid
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Medizin
    Notizen: Abstract Cantharidin, a potent defensive chemical, is present in all ten life stages of the blister beetleEpicauta funebris. The first five larval stages accumulate cantharidin as they feed and grow in size. When disturbed, they exude cantharidin in a milky oral fluid, not in hemolymph which adult beetles reflexively discharge from leg joints. Two subsequent larval stages and the pupa do not feed, grow, regurgitate, or change in their defensive reserves (110 μg cantharidin/insect, regardless of sex). Adult beetles kept in isolation for 60–90 d exhibit a pronounced sexual dimorphism in cantharidin production: the male biosynthesizes about 17 mg of the toxin, representing 10% of his live weight, whereas the female actually loses most of her defensive reserves. But in the wild a female beetle repeatedly acquires cantharidin as copulatory gifts from her mates.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01989424
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  • 4
    Digitale Medien
    Digitale Medien
    Avoidance of competition by spruce bark beetles,Ips typographus andPityogenes chalcographus (1993)
    Springer
    Cellular and molecular life sciences 49 (1993), S. 272-275 
    Details
    ISSN: 1420-9071
    Schlagwort(e): Semiochemical ; pheromone ; host selection ; competition ; Coleoptera ; Scolytidae
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Medizin
    Notizen: Abstract Bark beetles,Ips typographus andPityogenes chalcographus, attracted by synthetic or natural pheromone to Norway spruce logs,Picea abies, preferred to colonize uninfested logs rather than logs occupied by these beetles, probably as a means of avoiding intra-and interspecific competition. The aggregation pheromone components ofP. chalcographus, chalcogran and methyl (E, Z)-2,4-decadienoate, inhibited the attraction response ofI. typographus to its pheromone components (methyl butenol andcis-verbenol), while the converse was not true. However, verbenone released from colonized bark inhibited pheromonal response ofP. chalcographus.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01923539
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  • 5
    Digitale Medien
    Digitale Medien
    Potentiation of antifungal activity of sesquiterpene dialdehydes againstCandida albicans and two other fungi (1992)
    Springer
    Cellular and molecular life sciences 48 (1992), S. 1162-1164 
    Details
    ISSN: 1420-9071
    Schlagwort(e): Polygodial ; warburganal ; antifungal activity ; Candida albicans ; Saccharomyces cerevisiae ; Pityrosporum ovale ; enhancing effect ; antioxidants ; vitamin C ; BHA ; anethole
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Medizin
    Notizen: Abstract The antifungal activity of two drimane sesquiterpene dialdehydes, polygodial (1) and warburganal (2), alone and in combination with several other substances, was examined against three fungi,Candida albicans, Saccharomyces cerevisiae andPityrosporum ovale employing a broth dilution method. Anethole significantly synergized the activity of the two sesquiterpenoids againstC. albicans andS. cerevisiae however, it had only an, additive effect againstP. ovale. By contrast, two antioxidants, ascorbic acid (vitamin C) and BHA (butylated hydroxyanisole), noticeably enhanced the activity of the sesquiterpenoids againstP. ovale, but had no, effect againstC. albicans andS. cerevisiae.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01948015
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  • 6
    Digitale Medien
    Digitale Medien
    The polymerization of sickle hemoglobin in solutions and cells (1993)
    Springer
    Cellular and molecular life sciences 49 (1993), S. 110-117 
    Details
    ISSN: 1420-9071
    Schlagwort(e): Polymerization ; sickle hemoglobin ; sickle cell disease ; kinetics ; thermodynamics ; polymer domains ; nucleation
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Medizin
    Notizen: Abstract The polymerization of sickle hemoglobin occurs by the same mechanisms in solutions and in cells, and involves the formation of 14 stranded fibers from hemoglobin molecules which have assumed a deoxy quaternary structure. The fibers form via two types of highly concentration-dependent nucleation processes: homogeneous nucleation in solutions with hemoglobin activity above a critical activity, and heterogeneous nucleation in similarly supersaturated solutions which also contain hemoglobin polymers. The latter pathway is dominant, and creates polymer arrays called domains. The individual polymers bend, but also cross-link, and the resulting mass behaves as a solid. The concentration of polymerized hemoglobin increases exponentially unless clamped by rate limiting effects such as oxygen delivery.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01989414
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  • 7
    Digitale Medien
    Digitale Medien
    Effect of nystatin, amphotericin B and amphotericin B methyl ester on Saccharomyces cerevisiae with different lipid composition (1990)
    Springer
    Mycopathologia 112 (1990), S. 165-172 
    Details
    ISSN: 1573-0832
    Schlagwort(e): Nystatin ; amphotericin B ; amphotericin B methyl ester ; polyene antibiotics ; yeast ; Saccharomyces cerevisiae
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Medizin
    Notizen: Abstract Saccharomyces cerevisiae was cultured under anaerobiosis in semi-complete medium to which either palmitoleic or oleic acid was added. Cells were grown at 20 °C or 30 °C. The levels of total lipids, total sterols, and phospholipids were higher in cells grown at 20 °C than at 30 °C. The effects of nystatin (NYS), amphotericin B (AMB), and amphotericin B methyl ester (AME) were evaluated by determining cell viability and liberation of intracellular compounds. The loss of cell viability is higher in the first 30 minutes of incubation with the drugs and is the same regardless of the type of cells obtained. Low molecular weight compounds and ions such as K+ are liberated a few minutes after incubation with the drugs whereas proteins and substances absorbing at 260 nm are liberated later. Phosphate liberation comes after K+ and before compounds of higher molecular weights.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00436649
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  • 8
    Digitale Medien
    Digitale Medien
    Genetic and molecular approaches to synthesis and action of the yeast killer toxin (1990)
    Springer
    Cellular and molecular life sciences 46 (1990), S. 193-200 
    Details
    ISSN: 1420-9071
    Schlagwort(e): Saccharomyces cerevisiae ; protein toxin ; yeast toxin precursor ; protease processing ; lectin ; (1→6)-β-D-glucan ; receptor ; resistant mutants ; spheroplasts ; ion-permeable channels ; site-directed mutagenesis ; toxin functional domains
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Medizin
    Notizen: Summary The K1 killer toxin ofSaccharomyces cerevisiae is a secreted, virally-coded protein lethal to sensitive yeasts. Killer yeasts are immune to the toxin they produce. This killer system has been extensively examined from genetic and molecular perspectives. Here we review the biology of killer yeasts, and examine the synthesis and action of the protein toxin and the immunity component. We summarise the structure of the toxin precursor gene and its protein products, outline the proteolytic processing of the toxin subunits from the precursor, and their passage through the yeast secretory pathway. We then discuss the mode of action of the toxin, its lectin-like interaction with a cell wall glucan, and its probable role in forming channels in the yeast plasma membrane. In addition we describe models of how a toxin precursor species functions as the immunity component, probably by interfering with channel formation. We conclude with a review of the functional domains of the toxin structural gene as determined by site-directed mutagenesis. This work has identified regions associated with glucan binding, toxin activity, and immunity.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02027313
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  • 9
    Digitale Medien
    Digitale Medien
    E-myrcenol inIps duplicatus: An aggregation pheromone component new for bark beetles (1990)
    Springer
    Cellular and molecular life sciences 46 (1990), S. 1209-1211 
    Details
    ISSN: 1420-9071
    Schlagwort(e): Pheromone ; E-myrcenol ; ipsdienol ; Ips duplicatus ; Coleoptera ; Scolytidae ; Picea abies
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Medizin
    Notizen: Summary Males of the Eurasian bark beetleIps duplicatus, when feeding in host Norway spruce (Picea abies (L.) Karst.), produced and released ipsdienol andE-myrcenol, which we show to be aggregation pheromone components. Bioassays using walking beetles indicated thatE-myrcenol in synergistic combination with ipsdienol is essential for attraction. Synergism ofE-myrcenol and ipsdienol released at natural rates in the forest was also demonstrated with a new technique using mechanical slow-rotation of sticky traps.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01936939
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  • 10
    Digitale Medien
    Digitale Medien
    A comparison of pyridoxal 5′-phosphate dependent decarboxylase and transaminase enzymes at a molecular level (1991)
    Springer
    Cellular and molecular life sciences 47 (1991), S. 1104-1118 
    Details
    ISSN: 1420-9071
    Schlagwort(e): Transaminase ; decarboxylase ; serine hydroxymethyltransferase ; pyridoxal 5′-phosphate ; enzyme mechanism ; stereochemistry ; kinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Medizin
    Notizen: Abstract Pyridoxal 5′-phosphate is a coenzyme for a number of enzymes which catalyse reactions at Cα of amino acid substrates including transaminases, decarboxylases and serine hydroxymethyltransferase. Using the X-ray coordinates for a transaminase, aspartate aminotransferase, and the results of stereochemical and mechanistic studies for decarboxylases and serine hydroxymethyltransferase, an active-site structure for the decarboxylase group is constructed. The structure of the active-site is further refined through active-site pyridoxyllysine peptide sequence comparison and a 3-D catalytic mechanism for the L-α-amino acid decarboxylases is proposed. The chemistry of serine hydroxymethyltransferase is re-examined in the light of the proposed decarboxylase mechanism.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01918374
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  • 11
    Digitale Medien
    Digitale Medien
    Cardenolide glycosides from the adults and eggs ofChrysolina fuliginosa (Coleoptera: Chrysomelidae) (1992)
    Springer
    Cellular and molecular life sciences 48 (1992), S. 1023-1027 
    Details
    ISSN: 1420-9071
    Schlagwort(e): Chrysolina fuliginosa ; Coleoptera ; Chrysomelidae ; beetles ; cardenolides ; eggs ; glands ; chemical defence
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Medizin
    Notizen: Abstract Besides the known sarmentogenin 3-O-β-D-allopyranoside (1) and digitoxigenin-3-O-[β-D-xylopyranosyl-(1→4)-2′, 3′-di-O-acetyl-β-D-allopyranoside] (4), four new cardiac glycosides (2, 3, 5 and6) have been isolated from the defensive glands of adults ofChrysolina fuliginosa. The structures of the new compounds were determined by1H NMR at 600 MHz and FABMS. Compounds1–6, present in the adults ofC. fuliginosa, have also been identified in the eggs.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01919158
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  • 12
    Digitale Medien
    Digitale Medien
    Sexual dimorphism in the lipid fraction of the defensive secretion ofGastrophysa viridula (Coleoptera: Chrysomelidae) (1994)
    Springer
    Cellular and molecular life sciences 50 (1994), S. 766-770 
    Details
    ISSN: 1420-9071
    Schlagwort(e): Gastrophysa viridula ; Chrysomelidae ; Coleoptera ; chemical defence ; acetates ; hydrocarbons ; gas-liquid chromatography ; gas chromatography-mass spectrometry ; sexual dimorphism
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Medizin
    Notizen: Abstract The lipid fraction of the defensive secretion of adultGastrophysa viridula was analyzed by gas-liquid chromatography and gas chromatography-mass spectrometry. Three long chain acetates and two methyl-branched hydrocarbons were identified and their amounts in the secretion of single field-collected and laboratory-reared beetles determined. The composition of the secretion was affected by the sex, reproductive status, and age of the beetle. The ratio of (Z)-11-eicosenyl acetate to (Z)-13-docosenyl acetate ranged from 0.30 to 0.78 in male beetles and from 1.05 to 2.06 in female beetles. The biological significance of this sexual dimorphism is discussed.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01919379
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  • 13
    Digitale Medien
    Digitale Medien
    Female sex pheromone of the longhorn beetleMigdolus fryanus Westwood: N-(2′S)-methylbutanoyl 2-methylbutylamine (1994)
    Springer
    Cellular and molecular life sciences 50 (1994), S. 853-856 
    Details
    ISSN: 1420-9071
    Schlagwort(e): Migdolus fryanus ; Coleoptera ; Cerambycidae ; N-2′-methylbutanoyl 2-methylbutylamine ; N-formyll-isoleucine methyl ester ; sex pheromone ; chiral resolution ; dose-response
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Medizin
    Notizen: Abstract 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-(2′S)-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.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01956471
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  • 14
    Digitale Medien
    Digitale Medien
    Absorption of intramuscular phenobarbitone in children with severe falciparum malaria (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 107-110 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Phenobarbitone ; Cerebral malaria ; P.falciparum ; kinetics ; drug absorption ; children
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The absorption of intramuscular phenobarbitone 7 mg·kg−1 was studied in 11 Karen children aged between 1.7 and 11 y with severe falciparum malaria. Eight of the children were comatose. Clinical findings were compared with those in 9 further children with severe malaria of similar age range (four of whom were unconscious), who received an identical placebo. One child, who had received placebo, had repeated convulsions and died 1 h after admission to hospital. The remainder made an uncomplicated recovery. There were no convulsions subsequent to treatment, although the study was too small to assess anticonvulsant efficacy. There was no observable toxicity, but phenobarbitone recipients had a significant tendency to deepen in their level of coma or to become sleepy within the 4 h after drug administration. Phenobarbitone was rapidly absorbed, reaching a mean (range) peak concentration of 34.2 [29.3–42.6] μmol·l−1 in a median (range) of 4 (2.5–12) h. These values are comparable to those previously reported in healthy children and in children with febrile convulsions. Intramuscular phenobarbitone is well absorbed in children with severe malaria; the optimum prophylactic anticonvulsant dose remains to be determined.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00314929
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  • 15
    Digitale Medien
    Digitale Medien
    Kinetics of atrial natriuretic peptide in young and elderly subjects (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 449-452 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Atrial natriuretic peptide ; kinetics ; ageing
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary To study the influence of age on the kinetics of atrial natriuretic peptide (ANP) in man, human (99–126) ANP 2.0 μg·min−1 was infused IV for 60 min in 8 healthy young (18 to 25 y) and 9 healthy elderly (71 to 84 y) subjects. Both baseline ANP values and the levels at the end of infusion were higher in the elderly subjects. The mean residence time of ANP in the two age groups was not significantly different, whereas total body clearance (CL) was markedly diminished in the elderly as compared to the young subjects (mean±SD 3.1±1.0 l·min−1 and 6.2±4.1 l·min−1, respectively). The apparent volume of distribution at steady state was lower in the elderly than in the young, but the difference was not significant (mean±SD 44±19 and 103±111, respectively. The decrease in CL largely explained the higher ANP levels found in the elderly subjects. The MRT and the plasma half-life of the terminal phase did not differ between the two groups. In the elderly but not in the young subjects the calculated endogenous creatinine clearance was closely correlated with the CL (r=0.90, P〈0.001), thereby emphasizing the importance of the kidney in the metabolic clearance of ANP in the elderly.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00280134
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  • 16
    Digitale Medien
    Digitale Medien
    Interaction of talinolol and sulfasalazine in the human gastrointestinal tract (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 461-462 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Talinolol ; Sulfasalazine ; β-adrenoceptor-blocking drugs ; absorption ; drug interaction ; kinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The absorption of talinolol (TA) 50 mg was investigated without and together with the co-administration of sulfasalazine (SASP) 4 g in 11 healthy young volunteers, in order to clarify gastrointestinal transit of TA. Without SASP, the tmax of TA was 2.8 h, Cmax was 112 ng·ml−1 and the half life was 12 h; the AUCo-t was 958 ng·ml−1·h. In the case of concomitant administration of SASP, TA was found only in serum from 3 individuals, with a Cmax of 23 ng·ml−1 and a mean AUCo-t of 84 ng·ml−1·h. TA was not detectable in 5 subjects and it was at the limit of detection (2 ng·ml−1) in 3 subjects. Pharmacokinetic analysis was not possible in any of those individuals. The reason for the interaction appears to be the adsorption of TA by SASP. An interval of 2–3 h should elapse between giving SASP and other drugs.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00280137
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  • 17
    Digitale Medien
    Digitale Medien
    Bioavailability of controlled release carbamazepine estimated by mixed effect modelling (1993)
    Springer
    European journal of clinical pharmacology 44 (1993), S. 231-235 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Carbamazepine ; kinetics ; population pharmacokinetics ; bioavailability ; controlled release ; non-linear model
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The absorption properties of a conventional tablet of carbamazepine (T) and a controlled release form of carbamazepine (TCR) have been compared using a nonlinear mixed effect model (NONMEM). Plasma carbamazepine concentration data were obtained from an open, steady-state, crossover bioavailability study in which 494 measurements were obtained from 13 patients, with an equal number of samples per patient for each dosage form. The pharmacokinetic model used was a one-compartment open model with first-order absorption and elimination. The objective function was used as a measure of the goodness of fit of the model to the data. Body weight was an important determinant of carbamazepine clearance (CL) but not volume of distribution (V). Accounting for the interindividual variability in volume of distribution did not significantly influence the objective function. Including different rates of absorption (ka) for the two dosage forms resulted in a significant improvement in the objective function, as well as reducing the interindividual variability in the rate of absorption. Adding a parameter for relative bioavailability (f) of TCR improved the objective function statistically, but an unrealistic value for V was obtained, and the absorption and elimination rates appeared to be transposed in the classical “flip-flop” manner. Fixing V to the value obtained before introducing f did not change the objective function and permitted estimation of f without the confounding influence of excessive parameters. The final population parameter estimates (standard error of estimate) were: CL, 0.0522 (0.0019) l·h−1·kg−1; V, 63.7 (FIXED)l; kaT, 0.312 (0.064) h−1; kaTCR, 0.149 (0.016) h−1; f, 1.01 (0.0326); variance (additive) in CL, 0.291 (0.083) (l·h−1·kg−1)2; residual intrasubject error variance (additive), 0.572 (0.082) (mg·l−1)2. The 95% confidence interval of the extent of absorption (f) of 93.6%–107.4% was well within the generally accepted range of ±20%, while the rate of absorption of Tegretol CR was significantly slower than that of Tegretol, as expected for a controlled release product.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00271363
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  • 18
    Digitale Medien
    Digitale Medien
    Comparison of non-kinetic and kinetic approaches to individualization of gentamicin dosage (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 155-159 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Gentamicin ; Dosage ; kinetics ; dose individualization ; dose prediction
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary A prospective study was carried out in 40 acutely ill patients to compare the non-kinetic and kinetic approaches to individualization of the dosage regimen of gentamicin. The patients were divided into two equal groups. For the non-kinetic group, the doses were derived from the physician's personal experience, on a mg/kg basis, and by use of nomograms. The total daily dose ranged from 1.43 to 4.5 mg/kg. Based on serum concentration measurements, the dosage regimen for individual patient was calculated by Sawchuk-Zaske's method. The calculated doses were compared to the prescribed doses in each patient. Of the patients on empirically prescribed doses 65% received 36% more drug than the calculated dose and 20% received 36% less than the calculated dose. The calculated dosing intervals were greater than the recommended intervals in 60% of the patients. The gentamicin trough concentration was 〉 2 μg/ml in 70% of the patients. There was a significant tendency to overdosage of the patients. For the kinetic group, following administration of the calculated dose, the steady-state peak and trough concentrations in each patient were measured. The correlation of measured to predicted steady-state serum concentrations was excellent (r=0.9968, p〈0.05). About 85% of the served trough concentrations and 90% of the peak values fell within the therapeutic range. The mean of the prediction error (ME), mean absolute error (MAE), mean squared error (MSE), and root mean squared error (RMSE) of the trough and peak concentrations were calculated. The 95% confidence interval of the ME for the trough and peak concentrations included zero, which shows that the prediction was not significantly biased. A significant relationship between gentamicin clearance and the ratio of the peak and trough concentrations achieved to the administered dose (r=0.873, 0.916 for trough and peak, respectively) was found. The findings suggest that the individualized approach to dosage determination using pharmacokinetic principles, in conjunction with daily monitoring of serum gentamicin concentrations, may provide safe and effective therapy.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00280050
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  • 19
    Digitale Medien
    Digitale Medien
    Single and multiple dose pharmacokinetics of etizolam in healthy subjects (1991)
    Springer
    European journal of clinical pharmacology 40 (1991), S. 181-185 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Etizolam ; α-hydroxyetizolam ; healthy subjects ; kinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetics of etizolam, a new thienodiazepine derivative, has been examined after single and multiple (0.5 mg tablet) (0.5 mg b.d for 1 week) oral therapeutic doses in healthy volunteers. The single-dose kinetic profile of etizolam suggested that absorption after oral dosage was reasonably rapid, the maximum plasma concentration (Cmax) being attained within 0.5–2 h in all subjects. The mean elimination half-life (t1/2) averaged 3.4 h. Consistent with this, steady-state concentration were rapidly achieved and accumulation was extremely limited. Predicted average plasma concentrations (Cp) did not differ significantly from those actually measured at steady-state, suggesting that the kinetics of etizolam was linear, at least at therapeutic doses. The mean wash-out t1/2 was comparable to the elimination t1/2 of the single dose, which means that the drug probably has no effect on hepatic microsomal enzymes and other kinetic variables after repeated dosing. At steady state plasma concentrations of the main metabolite, α-hydroxyetizolam, were higher and disappeared more slowly (mean t1/2 8.2 h) than those of the parent compound. Taken with the fact that in animals the metabolite shows almost the same potency of pharmacological action as etizolam, this suggests that it may contribute significantly to the clinical effects of the parent compound. Based on the kinetic characteristics of the parent drug and its metabolite, etizolam can be regarded as a short-acting benzodiazepine, with elimination kinetics between those of short-intermediate derivatives and ultra-rapidly eliminated benzodiazepines.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00280074
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  • 20
    Digitale Medien
    Digitale Medien
    Comparative studies on species-specific reactivity between renin and angiotensinogen (1994)
    Springer
    Molecular and cellular biochemistry 131 (1994), S. 43-47 
    Details
    ISSN: 1573-4919
    Schlagwort(e): angiotensinogen ; kinetics ; recombinant protein ; renin ; species specificity ; transgenic mouse
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Chemie und Pharmazie , Medizin
    Notizen: Abstract The renin-angiotensin system (RAS) is the most important regulator of electrolyte homeostasis and blood pressure. Our recently generated transgenic mice carrying either the human renin (hREN) or human angiotensinogen (hANG) genes did not develop hypertension but dual gene strains obtained by cross-mating separate lines of mice exhibited a chronically sustained increase in blood pressure, suggesting the presence of species-specific reactivity between renin and angiotensinogen. In order to examine this specificity, the present study was designed to perform a strictly comparative study on hydrolysis of hANG by hREN and mouse submandibular renin (mREN)in vitro by using pure proteins. The recombinant hANG (rhANG) and the synthetic human-type tridecapeptide (hTDP), Asp-Arg-Val-Tyr-Ile-His-Pro-Phe-His-Leu-Val-Ile-His, corresponding to the N-terminal sequences of hANG, were used to determine the species specificity of recombinant hREN (rhREN) and mREN. While hTDP was cleaved by both rhREN with similar Km and with the same order of kcat, rhANG was cleaved by mREN with 16.7-fold higher Km and with 28.2-fold lower kcat than by rhREN. These results showed that kcat/Km value of mREN for rhANG was 468-fold lower than that for rhREN acting on rhANG.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01075723
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  • 21
    Digitale Medien
    Digitale Medien
    Variations in the kinetic response of several different phosphate-dependent glutaminase isozymes during acute metabolic acidosis (1991)
    Springer
    Molecular and cellular biochemistry 108 (1991), S. 113-123 
    Details
    ISSN: 1573-4919
    Schlagwort(e): phosphate-dependent glutaminase ; acute metabolic acidosis ; kinetics ; kidney tubules ; enterocytes ; hepatocytes ; brain tissue
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Chemie und Pharmazie , Medizin
    Notizen: Summary We describe the kinetic modifications to mitochondrial-membrane-bound phosphate-dependent glutaminase in various types of rat tissue brought about by acute metabolic acidosis. The activity response of phosphate-dependent glutaminase to glutamine was sigmoidal, showing positive co-operativity, the Hill coefficients always being higher than 2. The enzyme from acidotic rats showed increased activity at subsaturating concentrations of glutamine in kidney tubules, as might be expected, but not in brain, intestine or liver tissues. Nevertheless, when brain and intestine from control rats were incubated in plasma from acutely acidotic rats enzyme activity increased at 1 mM glutamine in the same way as in kidney cortex. The enzyme from liver tissue remained unaltered. S0.5 and nH values decreased significantly in kidney tubules, enterocytes and brain slices preincubated in plasma from acidotic rats. The sigmoidal curves of phosphate-dependent glutaminase shifted to the left without any significant changes in Vmax. The similar response of phosphate-dependent glutaminase to acute acidosis in the kidney, brain and intestine confirms the fact that enzymes from these tissues are kinetically identical and reaffirms the presence of an ammoniagenic factor in plasma, either produced or concentrated in the kidneys of rats with acute acidosis.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00233115
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  • 22
    Digitale Medien
    Digitale Medien
    Intracellular pH inSchizosaccharomyces pombe — Comparison withSaccharomyces cerevisiae (1993)
    Springer
    Molecular and cellular biochemistry 124 (1993), S. 131-140 
    Details
    ISSN: 1573-4919
    Schlagwort(e): Schizosaccharomyces pombe ; Saccharomyces cerevisiae ; H+-ATPase ; intracellular pH ; carboxy-seminaphthorhodafluor-1
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Chemie und Pharmazie , Medizin
    Notizen: Abstract We examined cytoplasmic pH regulation inSchizosaccharomyces pombe andSaccharomyces cerevisiae using pH-sensitive fluorescent dyes. Of several different fluorescent compounds tested, carboxy-seminaphthorhodafluor-1 (C.SNARF-1) was the most effective. Leakage of C.SNARF-1 fromS. pombe was much slower than leakage fromC. cerevisiae. Using the pH-dependent fluorescence of C.SNARF-1 we showed that at an external pH of 7, mean resting internal pH was 7.0 forS. pombe and 6.6 forS. cerevisiae. We found that internal pH inS. pombe was maintained over a much narrower range in response to changes in external pH, especially at acidic pH. The addition of external glucose caused an intracellular alkalinization in both species, although the effect was much greater inS. cerevisiae than inS. pombe. The plasma membrane H+-ATPase inhibitor diethylstilbestrol reduced both the rate and extent of alkalinisation, with an IC50 of approximately 35 μM in both species. Amiloride also inhibited internal alkalinisation with IC50's of 745 μM forS. cerevisiae and 490 μM forS. pombe.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00929205
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  • 23
    Digitale Medien
    Digitale Medien
    Expression of a functionally active cardiac fatty acid-binding protein in the yeast, Saccharomyces cerevisiae (1990)
    Springer
    Molecular and cellular biochemistry 98 (1990), S. 69-74 
    Details
    ISSN: 1573-4919
    Schlagwort(e): bovine heart fatty acid-binding protein ; H-FABPc ; heterologous gene expression ; Saccharomyces cerevisiae ; GALIO promoter
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Chemie und Pharmazie , Medizin
    Notizen: Summary The unicellular eukaryotic microorganism, Saccharomyces cerevisiae, transformed with a plasmid containing a cDNA fragment encoding bovine heart fatty acid-binding protein (H-FABP) under the control of the inducible yeast GAL10 promoter, expressed FABP during growth on galactose. The maximum level of immunoreactive FABP, identical in size to native protein as judged from SDS-polyacrylamide gel electrophoresis, was reached after approximately 16 hours of induction. Analysis of particulate and soluble subcellular fractions showed that FABP was exclusively associated with the cytosol. FABP expressed in yeast cells was functional as was demonstrated by its capacity to bind 14C-oleic acid in an in vitro assay. Growth of the transformants on galactose as the carbon source was significantly retarded at 37°C. Whereas the fatty acid pattern of total lipids was not altered in transformed cells, desaturation of exogenously added 14C-palmitic acid was significantly reduced both at 30 and 37°C. The lowest percentage of radioactively labeled unsaturated fatty acids was found in the phospholipid fraction.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00231369
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  • 24
    Digitale Medien
    Digitale Medien
    Enzymology of ADP-ribose polymer synthesis (1994)
    Springer
    Molecular and cellular biochemistry 138 (1994), S. 33-37 
    Details
    ISSN: 1573-4919
    Schlagwort(e): poly(ADP-ribose) polymerase ; structure ; chemistry ; kinetics ; automodification ; mechanism(s)
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Chemie und Pharmazie , Medizin
    Notizen: Abstract In this minireview, we summarize recent advances on the enzymology of ADP-ribose polymer synthesis. First, a short discussion of the primary structure and cloning of poly(ADP-ribose) polymerase (PARP) [EC 2.4.2.30], the enzyme that catalyzes, the synthesis of poly(ADP-ribose), is presented. A catalytic distinction between the multiple enzymatic activities of PARP is established. The direction of ADP-ribose chain growth as well as the molecular mechanism of the automodification reaction catalyzed by PARP are described. Current approaches to dissect ADP-ribose polymer synthesis into individual reactions of initiation, elongation and branching, as well as a partial mechanistic characterization of the ADP-ribose elongation reaction at he chemical level are also presented. Finally, recent developments in the catalytic characterization of PARP by site-directed mutagensis are also briefly summarized.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00928440
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  • 25
    Digitale Medien
    Digitale Medien
    Metals are directly involved in the redox interconversion of Saccharomyces cerevisiae glutathione reductase (1991)
    Springer
    Molecular and cellular biochemistry 101 (1991), S. 175-187 
    Details
    ISSN: 1573-4919
    Schlagwort(e): glutathione reductase ; Saccharomyces cerevisiae ; redox interconversion ; metals ; cell-free extracts
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Chemie und Pharmazie , Medizin
    Notizen: Summary Redox inactivation of glutathione reductase involves metal cations, since chelators protected against NADPH-inactivation, 3 µM EDTA or 10 µM DETAPAC yielding full protection. Ag+, Zn2+ and Cd2+ potentiated the redox inactivation promoted by NADPH alone, while Cr3+, Fe2+, Fe3+, Cu+, and Cu2+ protected the enzyme. The Zn2+ and Cd2+ effect was time-dependent, unlike conventional inhibition. Glutathione reductase interconversion did not require dioxygen, excluding participation of active oxygen species produced by NADPH and metal cations. One Zn2+ ion was required per enzyme subunit to yield full NADPH-inactivation, the enzyme being reactivated by EDTA. Redox inactivation of glutathione reductase could arise from the blocking of the dithiol formed at the active site of the reduced enzyme by metal cations, like Zn2+ or Cd2+. The glutathione reductase activity of yeast cell-free extracts was rapidly inactivated by low NADPH or moderate NADH concentrations; NADP+ also promoted rapid inactivation in fresh extracts, probably after reduction to NADPH. Full inactivation was obtained in cell-free extracts incubated with glucose-6-phosphate or 6-phosphogluconate; the inactivating efficiency of several oxidizable substrates was directly proportional to the specific activities of the corresponding dehydrogenases, confirming that redox inactivation derives from NADPH formed in vitro.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00229534
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  • 26
    Digitale Medien
    Digitale Medien
    Pharmaceutical development of a parenteral formulation of the novel anti-tumor agent carzelesin (U-80,244) (1994)
    Springer
    Investigational new drugs 12 (1994), S. 303-314 
    Details
    ISSN: 1573-0646
    Schlagwort(e): carzelesin (U-80,244) ; analytical characterization ; parenteral formulation ; stability ; degradation products
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The aim of this study was to design a parenteral dosage form for the investigational cytotoxic drag carzelesin. A stable formulation in PET (Polyethylene glycol 400/absolute ethanol/Tween 80, 6:3:1, v/v/v) was developed. The prototype, containing 0.50 mg carzelesin in 2.0 ml PET formulation, was found to be the optimal formulation in terms of solubility, stability and dosage requirements in phase I clinical trials. Quality control of the formulation showed that the pharmaceutical preparation of carzelesin in PET is not negatively influenced by the manufacturing process. Shelf life studies demonstrated that the formulation is stable for at least 1 year, when stored at −30°C in the dark. In addition, the stability of carzelesin in the PET formulation is discussed as a function of temperature, additives and after dilution in infusion fluids.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00873045
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  • 27
    Digitale Medien
    Digitale Medien
    Comparison of specific rates of hybridoma growth and metabolism in batch and continuous cultures (1992)
    Springer
    Cytotechnology 10 (1992), S. 147-155 
    Details
    ISSN: 1573-0778
    Schlagwort(e): batch culture ; continuous culture ; hybridoma ; kinetics ; specific rates
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Medizin , Werkstoffwissenschaften, Fertigungsverfahren, Fertigung
    Notizen: Abstract For the mouse hybridoma cell line VO 208, kinetics of growth, consumption of glucose and glutamine, and production of lactate, ammonia and antibodies were compared in batch and continuous cultures. At a given specific growth rate, different metabolic activities were observed: a 40% lower glucose and glutamine consumption rate, but a 70% higher antibody production rate in continuous than in batch culture. Much higher metabolic rates were also measured during the initial lag phase of the batch culture. When representing the variation of the specific antibody production rate as a function of the specific growth rate, there was a positive association between growth and antibody production in the batch culture, but a negative association during the transient phase of the continuous culture. The kinetic differences between cellular metabolism in batch and continuous cultures may be result of modifications in the physiology and metabolism of cells which, in continuous cultures, were extensively exposed to glucose limitations.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00570891
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  • 28
    Digitale Medien
    Digitale Medien
    Influence of inoculum age on hybridoma culture kinetics (1991)
    Springer
    Cytotechnology 5 (1991), S. 165-171 
    Details
    ISSN: 1573-0778
    Schlagwort(e): growth ; hybridoma ; inoculum age ; kinetics ; production
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Medizin , Werkstoffwissenschaften, Fertigungsverfahren, Fertigung
    Notizen: Abstract To determine the influence of the inoculum age on the kinetics of hybridoma growth and metabolism, spinner flasks have been inoculated with cells previously propagated in T flasks for 43, 52, 62 and 71 hr respectively. Increasing the age of the inoculum is found to result in a longer lag phase, in a lower maximum specific growth rate and in a reduced maximal cell density. During the growth phase specific rates of glucose and glutamine uptake and of ammonia and lactate production are similar. However, with the older inoculum, much higher metabolic activities are observed during the lag phase. The production of antibodies is delayed with increasing inoculum age, but the final antibody concentrations are similar, which indicates a higher specific antibody production rate when inoculating with older cells.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00365433
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  • 29
    Digitale Medien
    Digitale Medien
    Growth and protein production kinetics of a murine myeloma cell line transfected with the human growth hormone gene (1991)
    Springer
    Cytotechnology 5 (1991), S. 223-231 
    Details
    ISSN: 1573-0778
    Schlagwort(e): cell culture ; kinetics ; Ig promoter/enhancer ; plasmacytoma ; recombinant protein production
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Medizin , Werkstoffwissenschaften, Fertigungsverfahren, Fertigung
    Notizen: Abstract A model mammalian cell system for the production of recombinant proteins was investigated. Murine myeloma cells which had lost the ability to produce both heavy and light chain immunoglobulin molecules were transfected with a vector containing the immunoglobulin heavy chain promoter and enhancer elements linked to the human growth hormone gene. The growth kinetics of G32, a clonal isolate, were found to be similar to both the parent myeloma and hybridomas. However, production of hGH by G32 was growth associated, rather than as a secondary metabolite as is the case for hybridomas. In addition, G32 produced hGH at molar levels greater than most hybridomas.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00556292
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  • 30
    Digitale Medien
    Digitale Medien
    Biochemical characteristics of glucose-6-phosphate dehydrogenase variants among the Malays of Singapore with report of a new non-deficient (Gd Singapore) and three deficient variants (1991)
    Springer
    Journal of human genetics 36 (1991), S. 307-312 
    Details
    ISSN: 1435-232X
    Schlagwort(e): G6PD ; electrophoresis ; deficiency ; new variants ; kinetics ; inhibition
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Medizin
    Notizen: Summary Biochemical characteristics of one non-deficient fast G6PD variant (Gd Singapore) and six different deficient variants (three new, two Mahidol, one each of Indonesian and Mediterranean) were studied among the Malays of Singapore. TheGd Singapore variant had normal enzyme activity (82%) and fast electrophoretic mobilities (140% in TEB buffer, 160% in phosphate and 140% in Tris-HCl buffer systems respectively). This variant is further characterized by normalK m for G6P; utilization of analogues (Gal6P, 2dG6P; dAmNADP), heat stability and pH optimum. The other six deficient G6PD variants had normal electrophoretic mobility in TEB buffer with enzyme activities ranging from 1 to 12% ofGd B+. The biochemical characteristics identity them to be 2 Mahidol, 1 Indonesian and 1 Mediterranean variants and three new deficient variants.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01883603
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