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  • 1
    ISSN: 1520-4804
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Melbourne, Australia : Blackwell Science Pty
    Clinical and experimental pharmacology and physiology 27 (2000), S. 0 
    ISSN: 1440-1681
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: 1. The combined effects of the macrolide antibiotics erythromycin, josamycin, clarithromycin and YM17K (3,4′-dideoxy mycaminosyl tylonolide hydrochloride) on in vitro intracellular accumulation of vinblastine or cyclosporine (Cs)A and on the in vivo antitumour activity of vinblastine were investigated using mouse leukaemia P388 cells (P388/S) and anticancer drug-resistant (P388/ADR) cells. These effects were compared with those of a calcium antagonist (verapamil) or immunosuppressants (FK506 and CsA).2. All tested macrolide antibiotics increased the accumulation of both vinblastine and CsA in P388/ADR cells in a dose- dependent manner, but their potency was lower than that of verapamil, CsA or FK506.3. When vinblastine (200 μg/kg) was administered intraperitoneally with each of the macrolide antibiotics (10 or 100 mg/kg) or with verapamil (25 mg/kg) once a day for 10 days in P388/ADR-bearing mice, combined effects of vinblastine with the macrolide antibiotics (erythromycin, clarithromycin and YM17K) or verapamil were observed.4. The present study suggests that macrolide antibiotics may overcome anticancer drug resistance by inhibiting the binding of vinblastine or CsA to P-glycoprotein in P388/ADR cells.5. We believe that these results are encouraging for combination chemotherapy to overcome P-glycoprotein-dependent anticancer drug-resistant tumours in clinical practice.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1442-2042
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: To investigate whether rBAT gene products function as a crystine transporter component or as a transport activator, we microinjected several C–terminal deletion mutants of rBAT cRNA into Xenopus oocytes, and measured transport activity for arginine, leucine and cystine in the presence and absence of sodium. Wild type rBAT significantly stimulated the uptake of all 3 amino acids 10–20 fold compared to control mutants. On the other hand, no mutant, except a Δ511–685 mutant, stimulated the uptake of these amino acids. However, the Δ511–685 mutant significantly increased the uptake of arginine. In the presence of sodium, the Δ511–685 mutant also increased the uptake of leucine. The Δ511–685 mutant did not stimulate crystine uptake in the presence and absence of sodium. Furthermore, inhibition of L–arginine uptake by L–homoserine was seen only in the presence of sodium. These results suggest that mutant rBAT stimulates the endogenous amino acid transport system y+ in oocytes. Finally, rBAT gene products, as the primary cause of cystinuria, may function as activators of the amino acid transport system in renal brush border membrane.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1432-0851
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The cytotoxic activities of the PEC after an i.p. injection of agrimoniin, a tannin contained in Agrimonia pilosa Ledeb. were studied. The plastic nonadherent PEC had significantly higher NK cell activity than the untreated control, and the adherent PEC were cytostatic toward MM2 and MH134 cells. The adherent PEC did not cause tumor cell lysis by themselves, but were cytolytic against MM2 cells in the presence of anti-MM2 sera. In the course of these effects of PEC after the i.p. injection of agrimoniin, the augmentation of NK cell activity was the earliest reaction, reaching a peak at 2 days after the injection; then, cytostatic activity increased. The induction of antibody-dependent cell lytic activity was a later reaction, which reached a peak at 6 days after the injection.
    Type of Medium: Electronic Resource
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  • 5
    Electronic Resource
    Electronic Resource
    Springer
    European food research and technology 195 (1992), S. 550-554 
    ISSN: 1438-2385
    Source: Springer Online Journal Archives 1860-2000
    Topics: Process Engineering, Biotechnology, Nutrition Technology
    Description / Table of Contents: Summary Crude carthamine was obtainable through alkaline extraction, acidification, and cellulose adsorption. It was purified by column chromatography on Avicel cellulose and Toyo Pearl HW-40f. Using these techniques, the dye was purified up to about 3.5-fold at a final yield of 28.4% (mg carthamine·g dry flower−1: 5.22→1.48). On the basis of the experimental model data, an instruction manual for isolation and purification of carthamine is presented in order to standarize the bio-dye preparation at an economically pertinent cost.
    Notes: Zusammenfassung Rohes Carthamin kann durch alkalische Extraktion, Säuerung und Adsorption an Cellulose gewonnen werden. Der Farbstoff wird durch Säulenchromatographie auf Avicel-Cellulose und Toyo Pearl HW-40f gereinigt. Mit dieser Technik wird der Farbstoff 3,5fach konzentriert (auf rund 28,4%). Auf der Basis dieser experimentellen Daten ist die Isolierung und Reinigung des Carthamin zu standardisieren, und die Farbstoffgewinnung zu einem wirtschaftlichen Preis möglich.
    Type of Medium: Electronic Resource
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  • 6
    ISSN: 1438-2385
    Source: Springer Online Journal Archives 1860-2000
    Topics: Process Engineering, Biotechnology, Nutrition Technology
    Description / Table of Contents: Abstract A number of carbohydrates and related compounds was admixed with carthamin in an acidic buffer solution and the effect of the test chemicals on carthamin stability examined at low temperature. Monosaccharides were scarcely effective, although slightly accentuated values were obvious in thed-forms (d-form∶l-form=1.3∶1.0). Disaccharides were less effective for carthamin red preservation (dimer∶monomer=1.0∶1.8). However, a high level of colour conservation was observed with sugar alcohols. Both polyethylene glycol and glycerine very effectively protected carthamin from bleaching in solution: the colour preservation rates calculated were 91.3% and 83.8%, respectively, after 24 h incubation at 5° C in the dark. Gelatine was also effective for maintaining carthamin colour (preservation rate: 81.3%). The results are assessed in connection with utilizing carthamin as a herbal colorant of processed foods.
    Notes: Zusammenfassung Eine Zahl von Kohlenhydraten und verwandten Verbindungen wurden mit Carthamin in saurer Pufferlösung vermischt und die Wirkung auf dessen Stabilität bei niederer Temperatur getestet. Die Monosaccharide waren kaum effektiv, jedoch died-Form beschleunigte etwas stärker (d-Form∶l-Form=1.3∶1.0). Die Disaccharide waren weniger wirksam auf die Farberhaltung (Dimer∶Monomer=1.0∶1.8). Jedoch wurde eine gute Farbkonservierung mit Zuckeralkoholen beobachtet, sowohl Polyethyleneglycol und auch Glycerin schützten Carthamin sehr wirksam zu 91,3 bzw. 83,8% nach 24h Einwirkung. Auch Gelatine war sehr farberhaltend (81,3%). Die Resultate wurden in bezug auf ihre Verwendung von Carthamin als Farbe für industriell verarbeitete Lebensmittel beurteilt.
    Type of Medium: Electronic Resource
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  • 7
    ISSN: 1435-5604
    Keywords: Key words: hypophosphatemia ; Na-dependent phosphate cotransporter ; kidney ; mouse
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract: X-linked hypophosphatemic rickets (XLH) is known to impair renal adaptive response to Pi restriction. We investigated the effects of dietary Pi on the synthesis of renal sodium-dependent inorganic phosphate (Na/Pi) cotransporters (Npt1 and NaPi-7) in X-linked hypophosphatemic mice (Hyp). The NaPi-7 mRNA level in Hyp mice was reduced to 50% of that of normal mice while the Npt1 mRNA level was unchanged. After feeding a low-Pi diet, the amounts of NaPi-7 protein and mRNA were markedly increased in both normal and Hyp mice. In contrast, after feeding a high-Pi diet, the levels of protein and mRNA were largely decreased in both mice. Immunohistochemical analysis indicated that NaPi-7 staining was largely enhanced in the apical membrane of renal proximal tubular cells in the normal and Hyp mice fed the low-Pi diet. In contrast, NaPi-7 staining was decreased in both groups of rats fed the high-Pi diet. Npt1 immunoreactivity was detected in the apical membrane of proximal convoluted and straight tubular cells in Hyp and normal mice, and was unchanged regardless of dietary Pi manipulation in both mice. Thus, dietary regulation for the synthesis of the two cotransporters is not impaired in Hyp mice.
    Type of Medium: Electronic Resource
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  • 8
    ISSN: 1573-904X
    Keywords: tacrolimus ; disposition kinetics ; P-glycoprotein ; mdr la knockout mice ; brain distribution
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. This study was performed to evaluate the involvement of P-glycoprotein in disposition kinetics of tacrolimus (FK506), a substrate of P-glycoprotein, in the body. Methods. The blood and tissue concentrations of FK506 after i.v. or p.o. administration (2 mg/kg) to normal andmdrla knockout mice were measured by competitive enzyme immunoassay. Results. The blood concentrations in knockout mice were significantly higher than those in normal mice. The value of the total clearance (CLtot) for knockout mice (19.3 mL/min/kg) was about 1/3 of that for normal mice (55.8 mL/min/kg)(P 〈 0.001), although there was no significant difference in the distribution volume at the steady-state (Vdss) (about 4.6 L/kg) between both types of mice. FK506 rapidly penetrated the blood-brain barrier and the brain concentration reached a maximum, which was about 10 times higher in knockout mice than in normal mice, 1 hr after administration. The brain concentration in normal mice thereafter decreased slowly, whereas in knockout mice, an extremely high concentration was maintained for 24 hr. Conclusions. The pharmacokinetic behavior of FK506 in the tissue distribution is related with the function of P-glycoprotein encoded by themdr la gene. The brain distribution of FK506 is dominated by the P-glycoprotein-mediated drug efflux and presumably also by the binding to FK-binding proteins (immunophilins) in the brain.
    Type of Medium: Electronic Resource
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  • 9
    ISSN: 1437-7799
    Keywords: kidney ; phosphate ; hypophosphatemia ; mutation ; vitamin D ; transport
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Conclusion Recent investigations of X-linked hypophosphatemia support the concept that the kidney is intrinsically normal in this disorder, and that the characteristic phosphaturia is caused by a humoral factor. The mechanisms involved in the pathophysiology of X-linked hypophosphatemia, Hyp, and oncogenic hypophosphatemic osteomalacia are complex and are the results of mutations in a putative zinc metalloprotease. Inactivation inPHEX gene function initiates a series of events that result in severe perturbations in renal Pi transport and metabolism of vitamin D. There are a number of possible working models that could explain the experimental observations. However, our studies clearly show that a humoral factor (phosphatonin) inhibits the transcription of the type II Na+/Pi cotransporter gene (Fig. 4). Phosphatonin may be a key modulator of phosphate homeostasis.
    Type of Medium: Electronic Resource
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  • 10
    ISSN: 1437-7799
    Keywords: Na+-phosphate cotransporter ; dietary phosphate ; kidney ; rat
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Background Three types (typeI, II, andIII) of sodium-dependent phosphate cotransporters have recently been isolated and shown to be expressed in the mammalian kidney. Understanding of the functional roles and regulation of each transporter is still fragmented, however. Methods We analyzed the functional roles of each transporter by using antisense oligonucleotides in theXenopus oocytes expression system, and by localization in the proximal tubules of rat kidney using immunohistochemistry. Results Phosphate uptake in brush border membranes was increased by about 2 times in rats fed a low-phosphate, as compared with a high-phosphate, diet. Expression of typeI, II, andIII transporter mRNAs was observed in renal poly(A)+RNA, isolated from the rats fed a low-phosphate diet. Phosphate uptake increased about 2.5-fold inXenopus oocytes injected with the poly(A)+RNA, compared with those given RNA from rats fed a high-phosphate diet. Hybrid depletion of the typeII sodium-dependent phosphate transporter (NaPi-2), but not of the typeI (rNaPi-1) or typeIII transporters (PiT-1 and PiT-2), significantly decreased phosphate transport activity in oocytes injected with the poly(A)+RNA from each experimental group rat kidney. In rats fed the lowphosphate diet, NaPi-2 immunoreactivity increased markedly in the brush border membranes of renal proximal tubular cells, whereas rNaPi-1 protein was not changed. Conclusion This study suggests that the typeII transporter functions mainly as a sodium-dependent phosphate cotransporter, and is regulated by dietary phosphate in the rat kidney.
    Type of Medium: Electronic Resource
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