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Ohne Zusammenfassung 相似文献
997.
Lanreotide labeled with 99mTc: preparation,preclinical testing and comparison with (111)In-DTPA-octreotide 总被引:1,自引:0,他引:1
Laznicek M Laznickova A Trejtnar F Lorenc P Varvarigou A Bouziotis P Archimandritis S 《Anticancer research》2002,22(4):2125-2130
Somatostatin receptors are known to be present at a high density in a large number of tumors while (111)In-DTPA-octreotide has been routinely used in oncology for imaging somatostatin receptor-positive tumors and metastases. Lanreotide is another somatostatin receptor-specific peptide, shown to be effective in controlling the growth of some human tumors. The aim of this study was to label lanreotide with 99mTc by a direct labeling method and to evaluate the distribution and elimination characteristics of the labeled agent in rats. (111)In-octreotide was used as the reference radiopharmaceutical. For both radiolabeled-peptides the activity in blood and most organs decreased relatively rapidly with time. On the other hand, 99mTc-lanreotide was excreted mainly by the gastrointestinal tract to feces while (111)In-DTPA-octreotide was eliminated mostly into urine. The rat liver perfusion experiments showed that bile clearance of 99mTc-lanreotide was about three-order times higher than for (111)In-DTPA-octreotide. Analysis of the elimination mechanisms of 99mTc-lanreotide and (111)In-DTPA-octreotide in the perfused rat kidney confirmed that both peptides were eliminated mostly by glomerular filtration. Different protein binding of the agents ((111)In-DTPA-octreotide was only weakly bound, whereas 99mTc-lanreotide was strongly bound to proteins) resulted in substantially lower renal clearance of 99mTc-lanreotide when compared with (111)In-DTPA-octreotide. The results indicated that 99mTc-lanreotide could be of value for the scintigraphic imaging of specific tumors. 相似文献
998.
Effect of silybin and its congeners on human liver microsomal cytochrome P450 activities 总被引:6,自引:0,他引:6
Zuber R Modrianský M Dvorák Z Rohovský P Ulrichová J Simánek V Anzenbacher P 《Phytotherapy research : PTR》2002,16(7):632-638
Silybin and related flavonolignans form a major part of the Silybum marianum extract, silymarin, which has been used to treat liver diseases for hundreds of years. Although regarded as safe, many of the extract constituents remain thus far untested for their possible effects on liver biotransformation enzymes. Cytochromes P450 (CYP) are very important in this regard. We tested the effect of four flavonolignans: silybin, its hemisynthetic derivative dehydrosilybin, silydianin, and silycristin on three specific CYP activities: bufuralol 1'-hydroxylation (CYP2D6), p-nitrophenol hydroxylation (CYP2E1), and nifedipine oxidation (CYP3A4). All flavonolignans displayed dose-dependent inhibition of these activities with IC(50) values in the micromolar range. The inhibition was competitive or mixed as revealed by double reciprocal plots of kinetic experiments. However, the inhibition is not considered to be relevant for therapy because physiological concentrations of the individual flavonolignans do not exceed 0.5 microM. The data support the use of the extract as a dietary supplement. 相似文献
999.
Direct PCR detection of Burkholderia cepacia complex and identification of its genomovars by using sputum as source of DNA 总被引:4,自引:0,他引:4
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Drevínek P Hrbácková H Cinek O Bartosová J Nyc O Nemec A Pohunek P 《Journal of clinical microbiology》2002,40(9):3485-3488
We developed a nested PCR assay that detects the recA gene of the Burkholderia cepacia complex in sputum. The product of the first PCR round is also used to identify the genomovar of the pathogen. The protocol achieves high sensitivity and specificity with simple interpretation of genomovar status. 相似文献
1000.
Ershov PV Ugrumov MV Calas A Makarenko IG Krieger M Thibault J 《Journal of chemical neuroanatomy》2002,24(2):95-107
We evaluated the topographic relations between tyrosine hydroxylase (TH)- and/or aromatic L-amino acid decarboxylase (AADC)-immunoreactive neurons in the arcuate nucleus (AN), as well as between TH- and/or AADC-immunoreactive axons in the median eminence (ME) in rats at the 21st embryonic day, 9th postnatal day, and in adulthood. The double-immunofluorescent technique in combination with confocal microscopy was used. Occasional bienzymatic neurons but numerous monoenzymatic TH- or AADC-immunoreactive neurons were observed in fetuses. There was almost no overlap in the distribution of monoenzymatic neurons, and therefore few appositions were observed in between. In postnatal animals, numerous bienzymatic neurons appeared in addition to monoenzymatic neurons. They were distributed throughout the AN resulting in the increased frequency of appositions. Furthermore, specialized-like contacts between monoenzymatic TH- and AADC-immunoreactive neurons appeared. The quantification of the fibers in the ME showed that there were large specific areas of the monoenzymatic TH-immunoreactive fibers and bienzymatic fibers in fetuses, followed by the gradual reduction of the former and the increase of the latter to adulthood. The specific area of the monoenzymatic AADC-immunoreactive fibers in fetuses was rather low, and thereafter increased progressively to adulthood. The fibers of all the types were in apposition in the ME at each studied age. Close topographic relations between the neurons containing individual complementary enzymes of dopamine synthesis at the level of cell bodies and axons suggest functional interaction in between. 相似文献