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3 results on '"Katalin, Csige"'

2. In vivo investigation of Gallium-68 and Bismuth-205/206 labeled beta cyclodextrin for targeted alpha therapy of prostaglandin E2 receptor-expressing tumors in mice

Author

Katalin, Csige, Judit P, Szabó, Ibolya, Kálmán-Szabó, Noémi S, Dénes, Dezső, Szikra, Zita, Képes, Gábor, Opposits, Gábor, Méhes, István, Kertész, Ferenc, Fenyvesi, György, Trencsényi, and István, Hajdu

Subjects
Radioisotopes, Receptors, Prostaglandin, beta-Cyclodextrins, Pharmaceutical Science, Gallium Radioisotopes, Mice, SCID, Dinoprostone, Mice, Cell Line, Tumor, Neoplasms, Positron-Emission Tomography, Animals, Tissue Distribution, Bismuth
Abstract

Prostaglandin E2 (PGE2) molecule and its receptors play an important role in the development of malignancies and metastases therefore PGE2 may play a crucial role in the diagnosis and a new therapeutic target in the field of radionuclide therapy of PGE2-positive tumors. PGE2 form complexes with RAMEB (randomly-methylated-beta-cyclodextrin) with high affinity therefore the aim of this present study was to synthesize a PGE2-specific DOTAGA-RAMEB, which can be labeled with diagnostic and therapeutic isotopes also and binds to PGE2-positive tumors. DOTAGA-RAMEB was labeled with

Published
2022
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3. In vivo preclinical evaluation of the new 68Ga-labeled beta-cyclodextrin in prostaglandin E2 (PGE2) positive tumor model using positron emission tomography

Author

Judit P. Szabó, Éva Fenyvesi, Miklós Emri, Katalin Csige, István Kertész, Gábor Méhes, István Hajdu, Ferenc Fenyvesi, Lajos Szente, Miklós Vecsernyés, Milo Malanga, György Trencsényi, Adrienn Kis, and Ágnes Ráti

Subjects
chemistry.chemical_classification, Biodistribution, Cyclodextrin, medicine.diagnostic_test, Pharmaceutical Science, 02 engineering and technology, 021001 nanoscience & nanotechnology, 030226 pharmacology & pharmacy, Molecular biology, 03 medical and health sciences, 0302 clinical medicine, chemistry, In vivo, Positron emission tomography, medicine, Prostaglandin E2, 0210 nano-technology, Preclinical imaging, Ex vivo, Gamma counter, medicine.drug
Abstract

The cyclooxygenase-2 (COX-2)/prostaglandin E2 (PGE2) pathway plays an important role in tumor development and formation of metastases. It was earlier reported that cyclodextrin derivatives have a high affinity to form complexes with PGE2. Based on these results radiolabeled cyclodextrins – as new radiopharmaceuticals – may open a new pathway in the in vivo imaging and diagnosis of PGE2 positive tumors. The aims of this study were to synthetize the PGE2 specific 68Ga-labeled NODAGA-randomly methylated beta-cyclodextrin (68Ga-NODAGA-RAMEB) and investigate its tumor-targeting properties. NODAGA-RAMEB was labeled with Gallium-68 (68Ga), and the radiochemical purity (RCP%), partition coefficient (logP values), and in vitro-in vivo stability of 68Ga-NODAGA-RAMEB were determined. After intravenous injection of 68Ga-NODAGA-RAMEB the accumulation in organs and tissues was monitored in vivo by positron emission tomography (PET) and ex vivo by gamma counter in BxPC-3 and PancTu-1 tumor-bearing CB17 SCID mice. The RCP% of the newly synthesized 68Ga-NODAGA-RAMEB was higher than 98%. The molar activity was 15.34 ± 1.93 GBq/μmol. The logP of 68Ga labeled NODAGA-RAMEB was − 3.63 ± 0.04. Biodistribution studies showed high accumulation of 68Ga-NODAGA-RAMEB in PGE2 positive BxPC-3 tumors; approximately 15–20-fold higher radiotracer uptake was observed, than that of the background. 68Ga-labeled RAMEB is a promising radiotracer in PET diagnostics of PGE2 positive tumors.

Published
2020
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