JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY

Perylene diimide derivatives are one of the G-quadruplex DNA interactive agents which are thought to be useful in application of cancer treatment Starting from this consideration, N-(2,6-diisopropylphenyl)-N'-(4-pyridyl)-perylene-3,4,9,10-tetracarboxylic diimide (PYPER) was synthesized, radioiodinated with I-131, and its radiopharmaceutical potentials were tested on a male Albino rabbit and male Albino Wistar rats. This compound was successfully radioiodinated with I-131 with a radioiodination yield of about 100%. Scintigraphic imaging with the radiiodinated compound (I-131-PYPER) was performed on a rabbit. Static images were obtained from posterior projection using a Diacan gamma camera at several time intervals. The scintigrams clearly showed that the radioiodinated compound was not quickly cleared from the metabolism, accumulating in the stomach over about 30 minutes. The clearance time of this compound was considerably longer than 5 hours. The results obtained in this study agreed with that of the biodistribution studies and indicated that I-131-PYPER might be used as a scintigraphic agent for examining stomach diseases

APPLIED RADIATION AND ISOTOPES

Fe3O4 magnetic graft-Lys-poly(HEMA) was synthesized, labeled with Tc-99m for the first time and its radiopharmaceutical potential was investigated using animal models in this study. Quality control procedures were carried out using thin layer radiochromatography. The labeling yield of radiolabeled polymer was found to be about 100%. Then, stability and lipophilicity were determined. The lipophilicity of Tc-99m labeled Fe3O4 graft-Lys-poly(HEMA) was found to be 3.77. The serum stability experiments demonstrated that approximately 100% of radiolabeled polymer existed as an intact complex in the rat serum within 240 min. Biodistribution of radiolabeled magnetic graft-Lys-poly(HEMA) was performed on female Albino Wistar rats by scintigraphy and biodistribution studies. High uptake was seen in the stomach, the pancreas, brain, ovarian, intestines and the breast

NUCLEAR MEDICINE AND BIOLOGY

The metabolic comparison of aniline- and phenol-phthaleins radiolabeled with (131)I ((131)I-APH and (131)I-PPH, respectively) has been investigated in this study. To compare the metabolic behavior of these phthaleins and their glucuronide conjugates radiolabeled with (131)I, scintigraphic and biodistributional techniques were applied using male Albino rabbits. The results obtained have shown that these compounds were successfully radioiodinated with a radioiodination yield of about 100%. Maximum uptakes of (131)I-APH and (131)I-PPH, which were metabolized as N- and O-glucuronides, were observed within 2 h in the bladder and in the small intestine, respectively. In the case of verification of considerably up taking of these compounds also by tumors developed in the small intestine and in the bladder tissues, these results can be expected to be encouraging to test these compounds, which will be radiolabeled with other radioiodines such as (125)I, (121)I and (124)I as imaging and therapeutic agents in nuclear medical applications. (C) 2008 Elsevier Inc. All rights reserved

JOURNAL OF NANOPARTICLE RESEARCH

Herein, we investigated the biological uptake, distribution, and radiopharmaceutical potential of a novel molecule based on 2-hydroxyethyl methacrylate (HEMA) and anilinephtalein (APH) in the metabolism of Albino Wistar rats. In order to achieve this, we synthesized APH using organic synthesis methods and copolymerized APH with HEMA using a common polymerization method, surfactant-free emulsion polymerization. In the presence of Fe3O4 particles, we obtained a new generation magnetic-nano-scale polymer, magnetic-poly(HEMA-APH). This new molecule was chemically identified and approved by several characterization methods using Fourier transform infrared spectroscopy, scanning electron microscope, energy dispersive X-ray spectroscopy, electron spin resonance, atomic force microscope, and Zeta particle-size analysis. To evaluate the biological activity in live metabolism and anti-cancer potential of mag-poly(HEMA-APH), molecule was radioiodinated by a widely used labeling technique, iodogen method, with a gamma diffuser radionuclide, I-131. Thin-layer radiochromatography experiments demonstrated that I-131 binded to nanopolymer with the labeling yield of 90 %. Lipophilicity and stability experiments were conducted to determine the condition of cold and labeled mag-poly(HEMA-APH) in rat blood and lipid medium. Results demonstrated that radioiodinated molecule stayed as an intact complex in rat metabolism for 24 h and experimental lipophilicity was determined as 0.12 +/- A 0.02. In vivo results obtained by imaging and biological distribution experiments indicated that mag-poly(HEMA-APH) labeled with I-131 [I-131-mag-poly(HEMA-APH)] highly incorporated into tissues of the uterus, the ovarian, the prostate, and the lungs in rat metabolism. Based on these results, it may be evaluated that novel mag-poly(HEMA-APH) molecule labeled with I-131 is a compound which has a significant potential for being used as an anti-cancer agent. Certain results can only be obtained whether this molecule is applied to adenocarcinoma cell models and tumor-bearing animals

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS

In this study, N-methacryloyl-l-phenylalanine (MAPA) containing poly(2-hydroxyethylmethacrylate) (HEMA)-based magnetic poly(HEMA-MAPA) nanobeads [mag-poly(HEMA-MAPA)] were radiolabeled with I-131 [I-131-mag-poly(HEMA-MAPA)], and the radiopharmaceutical potential of I-131-mag-poly(HEMA-MAPA) was investigated. Quality control studies were carried out by radiochromatographic method to be sure that I-131 binded to mag-poly(HEMA-MAPA) efficiently. In this sense, binding yield of I-131-mag-poly(HEMA-MAPA) was found to be about 95-100%. In addition to this, optimum radiodination conditions for I-131-mag-poly(HEMA-MAPA) were determined by thin-layer radiochromatography studies. In addition to thin-layer radiochromatography studies, lipophilicity (partition coefficient) and stability studies for I-131-mag-poly(HEMA-MAPA) were realized. It was determined that lipophilicities of mag-poly(HEMA-MAPA) and I-131-mag-poly(HEMA-MAPA) were 0.12 +/- 0.01 and 1.79 +/- 0.76 according to ACD/logP algorithm program, respectively. Stability of the radiolabeled compound was investigated in time intervals given as 0, 30, 60, 180, and 1440min. It was found that I-131-mag-poly(HEMA-MAPA) existed as a stable complex in rat serum within 60min. After that, biodistribution and scintigraphy studies were carried out by using albino Wistar rats. It was determined that the most important I-131 activity uptake was observed in the breast, the ovary, and the pancreas. Scintigraphy studies well supported biodistribution results. Copyright (c) 2013 John Wiley & Sons, Ltd

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY

The aim of this study was to investigate the I-131 and I-127 labeled linezolid and moxifloxacin effects of minimum inhibitory concentration, and minimum bactericidal concentration on mature biofilm and microorganism within the biofilm. Linezolid and moxifloxacin were labeled with I-131 and I-127 and chromatography studies were carried out with thin layer radiochromatograpy and high-pressure liquid radiochromatography techniques. Specific activities of radiolabeled LZD and MXF was found to be 53.3 +/- 3.1 and 127.3 +/- 1.1 MBq/A mu mol for [I-131]LZD and 7.6 +/- 0.02 and 55.6 +/- 0.8 MBq/A mu mol for [I-131]MXF, respectively. The minimum inhibitory concentration and Time-Kill of Linezolid and moxifloxacin alone and their I-131 and I-127 labeled forms were tested with a standard strain of meticillin-susceptible StaphylocA +/- ccus aureus. MIC values of LNZ and MXF were 2.96 nmol/mL (1 A mu g/ml) and 0.141 nmol/mL (0.062 A mu g/ml). Time Kills of MXF and LZD were found to be 0.06 and 1 mu g, respectively. Antibiotics labeled with beta-emitting radioactive molecule may be a new theranostics strategy for biofilm infections

ASIAN JOURNAL OF CHEMISTRY

In this study, the iodine content in breast milk was measured by Sandell-Kolthoff's method. The milk was obtained from 40 healthy mothers, aged 20 to 37, from the pediatric division of Ege University hospital. All mothers were from Aegean region of Turkey. Comparisons were made with commercial milk samples. Destruction of organic matter by using alkaline ash method was carried out prior to determination by Sandell-Kolthoff reaction based on iodine's catalytic effect on the Ce(IV)-As(III) system. The iodine concentration ranges were within 19.1 and 94.2 mu g/kg in breast milk samples. Results obtained in this study clearly showed that breast milk samples did not have iodine deficiency which can lead to goiter and iodine concentrations of market milk were at sufficient level in the Aegean region of Turkey

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY

Bleomycins (BLMs; BLM, A2, and B2) were labeled with I-131 and radiopharmaceutical potentials were investigated using animal models in this study. Quality control procedures were carried out using thin layer radiochromatography (TLRC), high performance liquid chromatography (HPLC), and liquid chromatography (LC/MS/MS). Labeling yields of radiolabeled BLMs were found to be 90, 68, and 71%, respectively. HPLC chromatograms were taken for BLM and cold iodinated BLM (I-127-BLM). Five peaks were detected for BLM and three peaks for I-127-BLM in the HPLC studies. Two peaks belong to isomers of BLM. The isomers of BLM were purified with using HPLC. Biological activity of BLM was determined on male Albino Wistar rats by biodistribution and scintigraphic studies were performed for BLMs by using New Zelland rabbits. The biodistribution results of I-131-BLM showed high uptake in the stomach, the bladder, the prostate, the testicle, and the spinal cord in rats. Scintigraphic results on rabbits agrees with that of biodistributional studies on rats. The scintigraphy of radiolabeled isomers (I-131-A2 and I-131-B2) are similiarly found with that of I-131-BLM

A radioanalytical technique for measurement of beta-glucuronidase activities

WOS: 000234024300022Phenolphthalein-glucuronide is a commonly used glucuronide conjugate for beta-glucuronidase measurements. The quantity of phenolphthalein liberated by beta-glucuronidase is measured spectrophotometrically. The detection limit of the quantity of phenolphthalein using spectrophotometry is a few mu g. In this study, a new radioanalytical technique for the measurement of beta-glucuronidase was applied which is 10(6) times more sensitive than the spectrophotometric technique. Radioiodinated phenolphthalein-glucuronide and phenyl-N-glucuronide were used in this study in which the beta-glucuronidase levels of some tissue samples were measured