Labeling of apigenin with 131I and bioactivity of 131I-apigenin in male and female rats

Apigenin (4′,5,7-trihydroxyflavone), one of the most common flavonoids, has been shown to possess a variety of biological activities including tumor growth inhibition and chemopreventation. In the present study, apigenin was labeled with ¹³¹I using iodogen method and investigated of its bioactivity. Radiolabeling yield is 98±0.2%, as determined by radio thin layer chromatography (RTLC), electrophoresis and radio high performance liquid chromatography (RHPLC). Besides, structure analysis of synthesized cold iodoapigenin complex were assessed with LCMS/MS and ¹H-NMR. Results of in vitro study indicated a high stability (3 hours) in human serum. Biodistrubition studies are performed in male and female albino Wistar rats. Biodistribution data related to the male rats showed significant uptake in the small intestine. The female rats biodistribution results indicated that the uptake of ¹³¹I-apigenin was high in the intestine and uterus.     

Radiolabeling of EGCG with 125I and its biodistribution in mice

The aim of the present study was to label EGCG with ¹²⁵I and to determine its radiopharmaceutical potential in mice. EGCG was labeled with ¹²⁵I using the iodogen method. The labeling yield and the radiochemical purity of ¹²⁵I–EGCG were determined by radio thin-layer chromatography (RTLC). The Labeling yield was approximately 89.4 %. The radiochemical purity was approximately 96.4 %. The biodistribution studies of the labeled compound (specific activity; 0.47 TBq/μg) were performed in male Kunming mice. The uptakes of ¹²⁵I–EGCG in some organs were determined at different time after injection to the mice. The radioactivity in each organ was counted and the percentage of injected activity per gram of tissue weight (%ID/g) for each organ and blood was calculated. Incorporation of radioactivity in the various tissue/organ was confirmed by microautoradiography. ¹²⁵I–EGCG uptake in the stomach and salivary gland was higher than other organ/tissue. The black silver grains was concentrated in the nucleus, cytoplasm, intercellular substance and capillaries of that various organs, and its unevenly distributed. Thus, ¹²⁵I–EGCG may be radiopharmaceutical for the imaging of the stomach and salivary gland.     

35Cl, 81Br and 127I NQR spectra of cyclopentadienyltitanium halides

NQR spectra of ³⁵Cl, ⁸¹Br and ¹²⁷I in cyclopentadienyltitanium halides Cp_nTiHal_4-n have been studied. Quadrupole coupling constants of the halogen atoms regularly increase with the increasing number of Cp rings in the molecule, which is apparently connected with the decreasing multiplicity of the TiHal bond. A sharp increase in the asymmetry parameters of the iodine atom on introduction of the Cp rings is evidence for an essential desymmetrization of the electron density in the molecule caused by this operation.     

Labeling of acetaminophen with I-131 and biodistribution in rats

The aim of the present study was to label acetaminophen (APAP) with I-131 and to determine its radiopharmaceutical potential in rats. Acetaminophen was labeled with I-131 using the iodogen method. The radiochemical purity of (131)I-APAP was determined by RTLC and paper electrophoresis. The labeling yield was 94 +/- 4%. The biodistribution studies of the labeled compound (specific activity; 56.60 GBq/mmol) were performed in male Albino Wistar rats. The uptake of (131)I-APAP in some organs were determined at different time after injection to the rats. The radioactivity in each organ was counted and the percentage of injected activity per gram of tissue weight (%ID/g) for each organ and blood was calculated. (131)I-APAP uptake in the lung, liver, kidneys, pancreas, blood, stomach and some brain region, were observed. Thus, (131)I-APAP may be radiopharmaceutical for the imaging of the brain.     

Adsorption of 125I on palladium coated silver wire

The adsorption of ¹²⁵I on palladium coated silver wires was studied in this paper. The experimental conditions, e.g., reaction volume, carrier concentration, reaction time, reaction temperature, pH of the reaction mixture, were systematically optimized to obtain quantitative adsorption of ¹²⁵I on palladium coated silver wires. The experiments were performed using potassium iodide 8–9 μg as carrier in a reaction volume of 100 μL incubated in ~50 °C water bath for ~1 h, and the pH of the reaction system was controlled at 2–2.5. The distribution of activity on palladium coated silver wire was uniform, and the source cores can be easily sealed by laser welding into titanium capsules.     

First results studying the transmutation of 129I, 237Np, 238Pu, and 239Pu in the irradiation of an extended natU/Pb-assembly with 2.52 GeV deuterons

An extended U/Pb-assembly was irradiated with an extracted beam of 2.52 GeV deuterons from the Nuclotron accelerator of the Laboratory of High Energies within the JINR in Dubna, Russia. The lay-out of this experiment and first results are reported. The Pb-target (diameter 8.4 cm, length 45.6 cm) is surrounded by a ^natU-blanket (206.4 kg) and used for transmutation studies of hermetically sealed radioactive samples of ¹²⁹I, ²³⁷Np, ²³⁸Pu and ²³⁹Pu. Estimates of transmutation rates were obtained as result of measurements of gamma-activities of the samples. Information about the spatial and energy distribution of neutrons in the volume of the lead target and the uranium blanket was obtained with sets of activation threshold detectors (Al, Y and Au) and solid state nuclear track detectors (SSNTD). An electronic ³He neutron detector was tested on-line. A comparison of experimental data with theoretical model calculations using the MCNPX program was performed yielding satisfactory results. Collaboration “Energy plus Transmutation” This work is dedicated to the cherished memory of Professor Vladimir Pavlovich Perelygin from the JINR in Dubna, Russia.     

Synthesis of thromboxane receptor antagonists with the potential to radiolabel with 125I

The synthesis of several thromboxane receptor antagonists is described along with their ability to inhibit aggregation of human platelets.     

Die gleichzeitige Bestimmung von 51Cr und 131J in doppelt markiertem Blut

Ohne Zusammenfassung     

Die Methoden zur schnellen Bestimmung wichtiger Radionuklide (89Sr, 90Sr, 131J und 89Cs)

Ohne Zusammenfassung     

Zur Bestimmung dos 131Jodgehaltes von Uran-Spaltprodukten

Ohne Zusammenfassung     

Determination of 129I in large soil samples after alkaline wet disintegration

Summary Large soil samples (up to 500 g) can conveniently be disintegrated by hydrogen peroxide in an utility tank under alkaline conditions to determine subsequently ¹²⁹I by neutron activation analysis. Interfering elements such as Br are removed already before neutron irradiation to reduce the radiation exposure of the personnel. The precision of the method is <10% (1 RSD). The accuracy was checked by determining ¹²⁹I also by the combustion method.     

Zur Bestimmung kleiner 131J-Gehalte in Regenwasser und Urin

Ohne Zusammenfassung     

Distribution of 131I-labeled recombinant human erythropoietin in maternal and fetal organs following intravenous administration in pregnant rats

The aim of the present study was to demonstrate the possible transplacental transmission of ¹³¹I labeled recombinant human erythropoietin (¹³¹I-rh-EPO) in pregnant rats and its distribution through maternal and fetal organs. Six Wistar Albino Rats in their pregnancy of 18 days were used ¹³¹I labeled recombinant human erythropoietin (specific activity = 2.4 μCi/IU) was injected into the tail vein of rats. After 30 minutes labeled erythropoietin infusion maternal stomach, kidney, lung, liver, brain and heart as well as fetus were removed. Then, the same organs were removed from each fetus. Measuring weight of maternal and fetal organs as well as placenta were followed by radioactivity count via Cd(Te) detector. ¹³¹I labeled recombinant human erythropoietin was found to be able to pass rat placenta and its distribution order in fetal organs was similar to those of maternal organs. Besides, as measurements were performed closer to cornu uteri, uptakes were decreasing in every fetus and its corresponding placenta.     

Zur Bestimmung des Conversionsfaktors von 131J in biologischem Material

Ohne Zusammenfassung     

Im Beitrag zur Bestimmung von 131J durch Extraktion

Ohne Zusammenfassung     

Synthesis and biodistribution of 99mTc(CO)3-DMSA-MIBI in mice

Mixed ligand fac-tricarbonyl complex of [^99mTc(CO)₃-DMSA-MIBI] has been prepared starting from the precursor [^99mTc(OH₂)₃(CO)₃]⁺. The complex can be obtained in good yield and purity in a two-step procedure by first attaching meso-2,3-dimercaptosuccinic acid (DMSA, HOOCCH(SH)CH(SH)COOH) with [^99mTc(OH₂)₃(CO)₃]⁺, followed by addition of MIBI [tetrakis-2-methoxyisobutylisonitrile (CH₃OC(CH₃)₂CH₂-N≡C) copper(I) tetrafluoroborate] solution. The complex was characterized by TLC and HPLC and was studied by means of octanol-water partition coefficient, electrophoresis, stability in vitro, and normal mice experiment. Biodistribution in mice demonstrated that the complex showed higher myocardial uptake after 0.5-hour p.i. The ratios of heart/liver (%ID/g) in the case of ^99mTc(CO)₃-DMSA-MIBI was higher (1.88) than that observed in case of ^99mTc-MIBI¹ (0.93) after 0.5-hour p.i. (P<0.05). Results showed that the complex may be developed to a novel myocardial perfusion-imaging agent.     

Experimental and theoretical investigations of the nuclear quadrupole resonance of 127I in orthoperiodic acid,H5IO6

Pure nuclear quadrupole resonance of ¹²⁷I in H₅IO₆ has been reported to occur at 44.976 MHz (m = ±$\text{3}\text{2}$?m = ±$\text{1}\text{2}$ transition) and 83.960 MHz (m = ±$\text{5}\text{2}$? m = ±$\text{3}\text{2}$ transition) at 296 K (ref. 1). Using an externally quenched frequency modulated super regenerative spectrometer Zeeman studies have been performed at 296 K on single crystals of H₅IO₆ growm from aqueous solution by observation of the ±$\text{sol3}\text{2}$?±$\text{1}\text{2}$ transition. The zero-splitting locus method has been employed for the determination of the EFG parameters. The data show that there are two physically inequivalent sites, having average asymmetry parameters, η, of 0.25, located in the unit cell. The maximum field gradient is found to lie along the short bond I-O(2) as suggested by Rama Rao and Weiss (ref. 1). The EFG parameters obtained by detailed molecular orbital calculations (CNDO/2 and INDO method) are compared with the experimental results.     

Measurement of the radioactivity of 238U, 226Ra, 210Pb, 228Th, 232Th, 228Ra, 137Cs and 40K in tea using gamma-spectrometry

The aim of the present work was to determine the concentration of radionuclides in all kinds of tea available at the local Egyptian market. Radioactivity of the nuclides ²³⁸U, ²²⁶Ra, ²¹⁰Pb, ²²⁸Th, ²³²Th, ²²⁶Ra, ¹³⁷Cs and ⁴⁰K were measured in tea by direct γ-ray spectrometry using HPGe detector and their mean values were 16.0±5.3, 3.1±0.7, 34.3±3.4, 3.4±1.2, 3.0±0.6, 3.1±0.8, 0.9±0.2 and 623±25 Bq·kg⁻¹, respectively.     

Radiolabeling of low molecular weight d-galactose-based glycodendrimer with technetium-99m and biodistribution studies

Glycodendrimers are neoglycoconjugates that can be considered as bioisosters of glycoproteins, since they can mimic the multivalent interactions of lectin-carbohydrate. The ability of glycodendrimers to present multivalent interactions with lectins as compared to a monovalent ligand is referred to as “cluster effect”. It is expected that, because of the cluster effect, glycodendrimers would result in a better association with lectins than mono-carbohydrate anchored systems. Radioisotopes are useful to evaluate biodistribution of molecules. This study is important to obtain information about molecule–receptor interactions. Indeed, such study can provide an exquisite tool to evaluate the affinity of certain molecules to specific areas in the body, leading to the development of new radiopharmaceuticals and/or drug delivery systems. Herein, we describe a d-galactose coated low molecular weight PAMAM G0 dendrimer that was successfully radiolabeled with technetium-99m. Biodistribution studies and scintigraphic images were performed in healthy mice. It was observed high liver uptake which was significantly reduced in blocking studies, indicating hepatic specificity. Therefore, low molecular weight glycodendrimer can be considered as useful platform for selective targeting of drugs to the liver and to assess hepatic function.