An oestrogen-derivative labeled with 99mTc and its radiopharmaceutical potential

An oestrogen derivative 3,17-a-oestradiolyl propyl 1,4,8,11-tetraazacyclotetradecanyl-1-(4-methylbenzoic acid)ester (ESTCPTA) that is 3,17-a-oestradiolyl propinol coupled to 1-(4-methylbenzoic acid)1,4,8,11-tetraazacyclotetradecane (CPTA) was synthesized in five steps. The product was purified by recrystallization in ethyl alcohol, and analysed by NMR and IR spectroscopy. ESTCPTA was labeled with ^99mTc and radio thin layer chromatography (RTLC) and radio-paper electrophoresis were used to determine the radiochemical yields. Specific activity was approximately 23.7 GBq/mmol and the labeling yield was over 95%. The biodistribution studies were performed on female Albino Wistar rats. The rats were sacricified by ether narcotization at certain time intervals and the activity of the organs was counted by a gamma counter. The activity per gram tissue was calculated and time activity curves were generated.     

Determination of the stability constants of uranyl complex with 8-hydroxyquinolinium sulfate

8-Hydroxyquinoline (8-HOQ) is known as an important chelating agent for several metal ions. This compound is practically insoluble in water. For this reason, in this study its water soluble sulfate salt has been used for complexing uranyl ions and the stability constants of the complex have been determined. The Irving-Rosotti method computing the Calvin-Bjerrum pH-titration data, was applied. Finally, the stability constants of the complex formed between (8-HOQN-H)₂SO₄ and uranyl ions were found to be lgK₁=8.25 and lgK₂=4.15, the overall stability constant being {ie55-1}.     

Determination of iodide in drinking water by isotope dilution analysis

The most suitable way of determination iodine-deficiency is to measure iodine concentrations in water and urine. For this reason, a method that can determine iodide concentrations in drinking water and suitable for routine analysis, is developed. Water samples have been collected from four Aegean localities: Izmir, Salihli, Ödemis and Tire situated in the western Turkey. The method is based on substochiometric isotope dilution analysis. Iodile concentrations vary within 9.86–85.14 μg/l ranges in the analyzed samples. Mean value is 44.92±22.07 μg/l.     

Study on labeling conditions of125I-synkavit by the iodogen method

Labeling conditions of synkavit (2-methyl-1,4-naphthoquinol disodium phosphate) with iodine-125 have been studied. In this study, labeling temperature, reaction time, successive using of iodogen coated tubes, iodogen amount and synkavit concentrations have been determined to get optimum conditions for maximum labeling. Final results showed that when the labeling temperature, reaction time, synkavit concentration, and iodogen amount were, at room temperature, 15 min (in the case of successive using of three iodogen coated tubes), 2 mg ml^–1 and 5 mg, respectively; labeling yield was 90% and specific activities of the order of 555 GBq mmol^–1 (15 Ci mmol^–1) have been obtained.     

Potentiometric and antimicrobial studies on the asymmetric Schiff bases and their binuclear Ni(II) and Fe(III) complexes; synthesis and characterization of the complexes

The protonation constants of two nitro-Schiff bases SB¹, SB² and three asymmetric tetradentate diimines H₂L¹, H₂L² and H₂L³ and the stability constants of their ML type binuclear Ni(II) and Fe(III) complexes have been determined potentiometrically. The asymmetric diimines are (2OH) RCHNC₆H₄CHNR′ (2OH) type compounds [where R = R′ = phenyl for H₂L¹; R = naphthyl, R′ = phenyl for H₂L² and R = R′ = naphthyl for H₂L³]. The effect of tautomeric forms on the acid-base properties of the diimines has been investigated and discussed. In addition, dimeric and binuclear Ni(II) and Fe(III) complexes of the diimines have been synthesized and characterized by physical and spectroscopic techniques. Also, in vitro antimicrobial activities of the diimines and the complexes have been evaluated against three bacteria: Micrococcus luteus (NRLL B-4375), Bacillus cereus (RSKK 863), Escherichia coli (ATCC 11230) and the fungus: Candida albicans (ATCC 10239).     

PHA-L lectin and carbohydrate relationship: conjugation with CdSe/CdS nanoparticles, radiolabeling and in vitro affinities on MCF-7 cells

This research aims to investigate the interaction between phytohemagglutinin-L (PHA-L) and sialic acid, which is abundant on the breast cancer cell (MCF-7) surface and displays monosaccharide characteristics, by experimental and computational methods. Experimentally, CdSe/CdS nanoparticles (QDs) were synthesized; PHA-L was conjugated with QDs and labeled with ¹²⁵I. Radiolabeling yield was found to be 97 ± 1.2 %. Afterwards, in vitro bioaffinities of radiolabeled PHA-L conjugated QDs have been investigated on MCF-7 cells and it has been observed that the cell incorporation increased with time. The results indicated that ¹²⁵I labeled QD-PHA-L conjugates represent significant affinity on MCF-7 cells. In the second step of the study, the crystal structure of carbohydrate interaction surface of PHA-L was extracted from the crystal structure of PHA-L. The interactions between this surface and sialic acid were calculated by computational tools. These calculations revealed specific interactions between PHA-L and sialic acid. Semi-empirical methods, PM3 and AM1, were used in these calculations. Significant outcomes have been obtained from the experimental and computational studies and these results demonstrated that PHA-L may be an effective agent for imagining MCF-7 cells.     

89Zr Labeled Fe3O4@TiO2 Nanoparticles: In Vitro Afffinities with Breast and Prostate Cancer Cells

In this study, Fe₃O₄@TiO₂ nanoparticles were synthesized as a new Positron Emission Tomography/Magnetic Resonance Imaging (PET/MRI) hybrid imaging agent and radiolabeled with ⁸⁹Zr. In addition, Fe₃O₄ nanoparticles were synthesized and radiolabeled with ⁸⁹Zr. Df-Bz-NCS was used as bifunctional ligand. The nanoconjugates were characterized with transmission electron microscopy, scanning electron microscopy, and dynamic light scattering. Radiolabeling yields were 100%. Breast and prostate cancer cell affinities and cytotoxicity were determined using in vitro cell culture assays. The results demonstrated that Fe₃O₄@TiO₂ nanoparticles are promising for PET/MR imaging. Finally, unlike Fe₃O₄ nanoparticles, Fe₃O₄@TiO₂ nanoparticles showed a fluorescence spectrum at an excitation wavelength of 250 nm and an emission wavelength of 314 nm. Therefore, in addition to bearing the magnetic properties of Fe₃O₄ nanoparticles, Fe₃O₄@TiO₂ nanoparticles display fluorescence emission. This provides them with photodynamic therapy potential. Therefore multimodal treatment was performed with the combination of PDT and RT by using human prostate cancer cell line (PC3). The development of ⁸⁹Zr-Df-Bz-NCS-Fe₃O₄@TiO₂ nanoparticles as a new multifunctional PET/MRI agent with photodynamic therapy and hyperthermia therapeutic ability would be very useful.     

Interaction between green tea extract and 99mTc-pertechnetate on in vivo distribution

People drink various types of tea without knowing the side effects of biological and chemical contents and radiopharmaceutical interactions. In current study, it is aimed to evaluate the effects of green tea extract in different extraction solvents on the radiolabeling of the blood constituents with ^99mTc and on the biodistribution of radiopharmaceutical sodium pertechnetate (Na^99mTcO₄) in male Wistar Albino rats. The extraction of green tea was performed in different solvents. Biodistribution studies were performed on male rats which were treated via gavage with green tea extract in different extraction solvents or saline (0.9 % NaCl) as a control group for 7 days. The radiolabeling of blood constituents performed incubating with SnCl₂ and ^99mTc. According to experimental results, radiolabeling blood components with ^99mTc were not modified in the usage of the different extraction solvents for green tea extraction, but a significant alteration (P < 0.05) of biodistribution of Na^99mTcO₄ was observed after treatment with green tea extract in distilled water. Although there is no considerable effect on radiolabeling of blood components, there is an outstanding change on the biodistribution studies especially with green tea extract in distilled water. The identified change monitored in this study may cause to reduce the risk of misdiagnosis and/or avoid the repetition of the examinations in nuclear medicine.