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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 38 (1990), S. 625-627 
    ISSN: 1432-1041
    Keywords: antipyrine clearance ; apolipoproteins ; HDL ; A-I ; A-II ; B ; HDL2 cholesterol ; microsomal enzyme induction ; phenobarbital
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Serum high density lipoprotein (HDL) subfractions HDL2 and HDL3, apolipoproteins, and plasma antipyrine clearance (AP-CL) rate, an index of liver microsomal enzyme activity, were determined in 21 healthy subjects. High HDL cholesterol and HDL2 cholesterol concentrations and HDL cholesterol/cholesterol and HDL2/HDL3 cholesterol ratios were associated with high AP-CL. Phenobarbital enhanced antipyrine elimination and increased the apolipoprotein A-I/A-II ratio. Subjects who had high AP-CL had a more antiatherogenic HDL subfraction and apolipoprotein profile than those with low AP-CL.
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 47 (1994), S. 315-318 
    ISSN: 1432-1041
    Keywords: Coumarin ; Coumarin 7-hydroxylation ; interindividual variability ; polymorphism
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract One hundred healthy Turkish volunteers (70 male, 30 female) aged from 19 to 56 years were given 5 mg coumarin p.o. after an overnight fast. Urine samples were collected before and 2, 4 and 8 h after drug administration. The extent and rate of formation of 7-OH-coumarin (7OHC) was determined by the urinary excretion of the metabolite as measured with the fluorometric method. On average, 80% of 7OHC formed was excreted in 2 h. The total amount of 7OHC formed was 59.8% (21.5%) (mean and SD, n=100, range 17–100%) of the given dose. The percentage of 7OHC excreted during the first 2 h compared with the 7OHC excretion at 8 h was a constant and stable individual characteristic for the rate of the formation of 7OHC (‘2 h coumarin test’). Although four individuals had relatively slow coumarin test values (34–40%), no clear-cut polymorphism in the rate of 7OHC formation was found. However, 7OHC formation was lower in males and in cigarette smokers.
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 50 (1996), S. 133-137 
    ISSN: 1432-1041
    Keywords: Key words Coumarin ; Coumarin 7-hydroxylation ; Vegan diet ; Biotransformation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract Objective: Coumarin 7-hydroxylation was investigated in 21 Finnish vegans (20 females, one male) consuming a strict, uncooked vegan diet (“living food diet”) and in their matched omnivorous controls, by means of an in vivo coumarin test. Method: A capsule containing 5 mg of coumarin (Venalot®) was taken after an overnight fast, and urine samples were collected before and 2, 4 and 6 h after the drug administration. The extent and rate of urinary excretion of 7-hydroxycoumarin was determined using HPLC. Results: The total urinary excretion of 7-hydroxycoumarin during 6 h was 58 (range 23–85) and 64 (range 39–92)% of the administred dose in the vegan and control groups. The coumarin index (excretion of 7-hydroxycoumarin during the first 2 h as percentage of total excretion) was 72% in the vegan and 78% in the control groups. A negative correlation was observed between the coumarin index and the consumption of wheatgrass juice by the vegans (r = −0.60, P 〈 0.01, n = 21). Proportion of slow hydroxylators (excreting 7-hydroxycoumarin after 4 h) was not statistically different between the groups (5/21 in the vegans vs 8/20 in the controls). Conclusion: According to the present study, the clearly different dietary patterns and nutrient intakes between the vegans and the omnivores resulted in similar extent and rate of 7-hydroxycoumarin formation, indicating only a minor effect on coumarin hydroxylase (CYP2A6) activity by the plant substances in the uncooked vegan diet.
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 47 (1995), S. 461-464 
    ISSN: 1432-1041
    Keywords: Carbamazepine ; Oxcarbazepine ; Liver enzyme induction ; sex hormones ; sex hormone binding globulin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract The function of the hepatic P450 enzyme system was evaluated by measuring the kinetics of antipyrine and serum sex hormone levels were determined in 12 male patients with epilepsy during carbamazepine medication, and two and six months after changing their medication to oxcarbazepine. Antipyrine t1/2 increased and antipyrine CL decreased after the change reflecting normalisation of the liver P450 enzyme system function. Serum sex hormone binding globulin levels decreased, and serum dehydroepiandrosterone sulphate increased after the change. The results show that the carbamazepine-associated induction of the liver P450 enzyme system and changes in serum sex hormone balance can be avoided by replacing carbamazepine with oxcarbazepine.
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  • 5
    Electronic Resource
    Electronic Resource
    Springer
    Trees 11 (1997), S. 378-387 
    ISSN: 0931-1890
    Keywords: Key words Pinus sylvestris (L.) ; Electron microscopy ; Heavy metals ; Multi-stress-symptoms ; SO2
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Agriculture, Forestry, Horticulture, Fishery, Domestic Science, Nutrition
    Notes: Abstract  Injuries to needles of Scots pines (Pinus sylvestris L.) growing in nutrient-poor soils on the Kola Peninsula collected in April 1991 were studied on a gradient of increasing distances (10 – 115 km) from the Monchegorsk nickel smelter, Russia, which emits SO2, Ni and Cu. The condition of the mesophyll cells was quantified from needles of the two latest age classes using a light and an electron microscope. The damage to the ultrastructure consisted of multistress symptoms caused by excess sulphur, heavy metals, frost, acidic precipitation and ozone. Injuries were most commonly manifested in the form of dark, irregularly shaped chloroplasts with protrusions and light thylakoids and plastoglobuli. These symptoms gradually disappeared with increasing distance and decreasing deposition rate. Concentrations of sulphur, copper and nickel decreased towards more distant sites where normal levels of the latter two elements were reached. Sulphur concentrations remained above background throughout the distance gradient. In the closest plots to the smelter area, cell collapse under the stomata and epidermis related to acute SO2 and heavy metal effects was found, whereas further away symptoms were more diverse, pointing towards the effects of ozone, acidic deposition and thereby decreased frost tolerance. The additive multistress symptoms were clearly seen in the area up to 40 km from the smelter where needle Cu concentration was above 110 ppm, Ni concentration above 39 ppm and S concentration above 1343 ppm.
    Type of Medium: Electronic Resource
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  • 6
    ISSN: 1573-8477
    Keywords: apical dominance ; Gentianella ; grazing tolerance ; herbivory ; meristem allocation ; overcompensation ; shoot architecture
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract Meristem allocation models suggest that the patterns of compensatory regrowth responses following grazing vary, depending on (i) the number of latent meristems that escape from being damaged, and (ii) the activation sensitivity of the meristems in relation to the degree of damage. We examined the shape of compensatory responses in two late-flowering populations (59°20′N and 65°45′N) of the field gentian. Plants of equal initial sizes were randomly assigned to four treatment groups with 0, 10, 50 and 75% removal of the main stalk. The plants were clipped before flowering, and their performance was studied at the end of the growing season. The northern population showed a linear decrease in shoot biomass and fecundity with increasing biomass removal, while the response in the southern population was quadratic with maximum performance at the damage level of 50% clipping. This nonlinear shape depended upon the activation sensitivity of dormant meristems in relation to their position along the main stem. The highest plant performance was achieved by inflicting intermediate damage which induced regrowth from basally located meristems. In contrast, the topmost branches took over the dominance role of the main stem after minor apical damage (10% clipping). Consequently, the breakage of apical dominance is a necessary precondition of vigorous regrowth in this species. However, compensation in the field gentian is unlikely to be a mere incidental by-product of apical dominance. The ability to regrow from basally located meristems that escape from being damaged by grazing may well be a sign of adaptation to moderate levels of shoot damage.
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  • 7
    ISSN: 1573-8477
    Keywords: apical dominance ; bet-hedging ; compensatory continuum ; competition ; Erysimum ; monocarps ; nutrient availability ; overcompensation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract Contrary to the general expectation, the compensatory continuum hypothesis proposes that grazing may not always affect plant performance adversely. Instead, the effects may vary from negative (undercompensation) to positive (overcompensation), depending on the local availability of resources and the intensity of competition experienced by individual plants. We tested this hypothesis in a common garden experiment by growing tall wormseed mustard, Erysimum strictum, under a factorial design involving simulated grazing (0, 10, or 50% of the main stem clipped), supplemental fertilization and below-ground competition. The results supported the hypothesis. On an average, fertilization increased and competition decreased plant performance. Overcompensation was only observed among the fertilized plants growing free of competition. Simulated grazing increased seed yield 1.6 (10% clipping) and 1.4 times (50% clipping) as compared to unclipped plants when the plants were grown with fertilization and without competition. In contrast, clipping did not significantly increase seed yield in the plants grown without fertilization and/or with competition. The breakage of apical dominance provides a proximate mechanism of these regrowth responses. This is consistent with the fact that most plants (85%) had an unbranched shoot architecture in our study population. However, it is not clear why E. strictum has a relatively unbranched architecture in natural populations. We briefly discuss the alternative ecological factors – competition for light, adaptation to herbivory and optimal timing of flowering as a bet-hedging strategy in monocarpic plants – which might maintain unbranched architecture in this species.
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  • 8
    ISSN: 1573-904X
    Keywords: naproxen ; prodrugs ; solubility ; lipophilicity ; hydrolysis kinetics ; skin permeation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To synthesize and evaluate various novel aminoacyloxyalkyl esters of naproxen (3a-i) and naproxenoxyalkyl diesters of glutamic and aspartic acids (3j-m) as potential dermal prodrugs of naproxen. Methods. The prodrugs 3a-m were synthesized, and their aqueous solubilities, lipophilicities and hydrolysis rates were determined in a buffered solution and in human serum. The permeation of selected prodrugs across excised postmortem human skin was studied in vitro. Results. The aminoacyloxyalkyl prodrugs showed higher aqueous solubilities and similar lipid solubilities, in terms of octanol-buffer partition coefficients (log Papp) at pH 5.0, when compared with naproxen. At pH 7.4 the prodrugs were significantly more lipophilic than naproxen. Prodrugs3a-i showed moderate chemical stability in aqueous solutions at pH 5.0 and were rapidly converted to naproxen in human serum (t1/2 = 4−19 min). The selected aminoacyloxyalkyl prodrugs possessed a higher flux across the skin than naproxen, with a maximum enhancement of 3-fold compared to naproxen. Prodrugs 3j-mshowed poor aqueous solubility and permeation across the skin. Conclusions. Combinations of adequate aqueous solubility and lipophilicity of naproxen aminoacyloxyalkyl prodrugs having fast rates of enzymatic hydrolysis resulted in improved dermal delivery of naproxen.
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  • 9
    Electronic Resource
    Electronic Resource
    Springer
    Water, air & soil pollution 102 (1998), S. 389-405 
    ISSN: 1573-2932
    Keywords: air pollution ; heavy metals ; needle element content ; Pinus sylvestris ; XRF
    Source: Springer Online Journal Archives 1860-2000
    Topics: Energy, Environment Protection, Nuclear Power Engineering
    Notes: Abstract Concentrations of aluminium (Al), arsenic (As), calcium (Ca), cadmium (Cd), chlorine (Cl), chromium (Cr), copper (Cu), iron (Fe), potassium (K), magnesium (Mg), manganese (Mn), nickel (Ni), phosphorus (P), lead (Pb), sulphur (S), silicon (Si) and zinc (Zn) were measured by X-ray fluorescence spectrometry (XRF) in Scots pine needles collected from transects across Finnish Lapland and the Kola Peninsula in Russia. Ni, Cu, Fe, P and S concentrations were significantly higher in the needles collected in the vicinity of the smelters in Monchegorsk, whereas Mn and Zn decreased towards Monchegorsk. No distinct increase of S or decrease of Mn and Zn concentrations in the needles were observed when approaching Nikel. Foliar S concentrations were higher in C needles than in C+1 needles, even in plots close to the smelters. The effect of the emissions from the smelters was clearly seen in the needle chemistry up to 50 km away from smelters and was still perceivable over 100 km away.
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  • 10
    Electronic Resource
    Electronic Resource
    Chichester : Wiley-Blackwell
    Organic Magnetic Resonance 15 (1981), S. 53-56 
    ISSN: 0030-4921
    Keywords: Chemistry ; Analytical Chemistry and Spectroscopy
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Sodium borohydride reduction of methylphenobarbital leads to the formation of two different dihydroderivatives, reduced either in position 4 or position 6. The structures of the derivatives have been determined through analysis of the 1H and 13C NMR spectra of phenobarbital, methylphenobarbital and their derivatives. Detailed interpretation of the spectra and the resulting spectral parameters indicate conformations where the hydroxyl groups are axial and trans to the ethyl group. In these configurations the phenyl ring becomes equatorial. The results also allow an unambiguous assignment of the resonances of the phenyl carbons 2′(6′) and 3′(5′) of phenobarbital and the carbonyl carbons 4 and 6 of methylphenobarbital, differing interpretations having been previously advanced in the literature.
    Additional Material: 2 Ill.
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