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Synthesis and biological evaluation of Tc-99m tricarbonyl complex of O,O '-diethylethylenediamine-N,N '-di-3-propanoate as potential tumour diagnostic agent

Authorized Users Only
2016
Authors
Lakić, Mladen
Sabo, Ljubica
Ristić, Slavica
Savić, Aleksandar
Petričević, Saša
Nikolić, Nadežda
Vukadinović, Aleksandar
Janković, Drina
Sabo, Tibor
Vranješ-Đurić, Sanja
Article (Published version)
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Abstract
The extensive development of radiopharmaceuticals towards early tumour detection and treatment has increased the demand for new ligands with higher tumour selectivity. Research has been done on the potential of the novel O,O'-diethylethylenediamine-N,N'-di-3-propanoate (L) ligand as a radionuclide vehicle for tumour targeting. Under alkaline conditions, L hydrolyses and produces half ester ligand (L') and diacid ligand (L"), with characteristic donor atom array N, N, O. Ligand L was successfully labelled with Tc-99m at pH=9 by coordination with the octahedral fac-[Tc-99m(CO)(3)(H2O)(3)](+) intermediate, forming the main radioproduct fac-[(TcL)-Tc-99m'(CO)(3)] (Tc1). The Tc-99m complex showed a low lipophilic character (log P = 0.48) and low binding affinity to human serum albumin (2.51 +/- 0.48%). In vitro stability studies in saline and human plasma, as well as challenge studies with cysteine and histidine, revealed high stability of the complex during 24 h. Biodistribution studies of... Tc1 in female C57BL/6 mice bearing B16/F1 melanoma metastases showed significant tumour uptake: 9.81 +/- 1.19% ID g(-1) in the liver, 5.87 +/- 0.54% ID g(-1) in the lungs and 3.17 +/- 0.33% ID g(-1) in the ovary at 30 min post-injection. Favourable physicochemical properties, satisfactory in vitro/in vivo stability and biodistribution profile in the experimental metastatic melanoma model indicate the possible application of the radiolabelled ligand in tumour diagnosis. Copyright (C) 2015 John Wiley & Sons, Ltd.

Keywords:
eddp-type ligands / Tc-99m complex / Tc-99m carbonyl / metastatic melanoma / tumour diagnosis
Source:
Applied Organometallic Chemistry, 2016, 30, 2, 81-88
Publisher:
  • Wiley, Hoboken
Funding / projects:
  • Magnetic and radionuclide labeled nanostructured materials for medical applications (RS-45015)

DOI: 10.1002/aoc.3401

ISSN: 0268-2605

WoS: 000369872600003

Scopus: 2-s2.0-84955396715
[ Google Scholar ]
6
5
URI
https://cherry.chem.bg.ac.rs/handle/123456789/2045
Collections
  • Publikacije
Institution/Community
Hemijski fakultet
TY  - JOUR
AU  - Lakić, Mladen
AU  - Sabo, Ljubica
AU  - Ristić, Slavica
AU  - Savić, Aleksandar
AU  - Petričević, Saša
AU  - Nikolić, Nadežda
AU  - Vukadinović, Aleksandar
AU  - Janković, Drina
AU  - Sabo, Tibor
AU  - Vranješ-Đurić, Sanja
PY  - 2016
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/2045
AB  - The extensive development of radiopharmaceuticals towards early tumour detection and treatment has increased the demand for new ligands with higher tumour selectivity. Research has been done on the potential of the novel O,O'-diethylethylenediamine-N,N'-di-3-propanoate (L) ligand as a radionuclide vehicle for tumour targeting. Under alkaline conditions, L hydrolyses and produces half ester ligand (L') and diacid ligand (L"), with characteristic donor atom array N, N, O. Ligand L was successfully labelled with Tc-99m at pH=9 by coordination with the octahedral fac-[Tc-99m(CO)(3)(H2O)(3)](+) intermediate, forming the main radioproduct fac-[(TcL)-Tc-99m'(CO)(3)] (Tc1). The Tc-99m complex showed a low lipophilic character (log P = 0.48) and low binding affinity to human serum albumin (2.51 +/- 0.48%). In vitro stability studies in saline and human plasma, as well as challenge studies with cysteine and histidine, revealed high stability of the complex during 24 h. Biodistribution studies of Tc1 in female C57BL/6 mice bearing B16/F1 melanoma metastases showed significant tumour uptake: 9.81 +/- 1.19% ID g(-1) in the liver, 5.87 +/- 0.54% ID g(-1) in the lungs and 3.17 +/- 0.33% ID g(-1) in the ovary at 30 min post-injection. Favourable physicochemical properties, satisfactory in vitro/in vivo stability and biodistribution profile in the experimental metastatic melanoma model indicate the possible application of the radiolabelled ligand in tumour diagnosis. Copyright (C) 2015 John Wiley & Sons, Ltd.
PB  - Wiley, Hoboken
T2  - Applied Organometallic Chemistry
T1  - Synthesis and biological evaluation of Tc-99m tricarbonyl complex of O,O '-diethylethylenediamine-N,N '-di-3-propanoate as potential tumour diagnostic agent
VL  - 30
IS  - 2
SP  - 81
EP  - 88
DO  - 10.1002/aoc.3401
UR  - Kon_3001
ER  - 
@article{
author = "Lakić, Mladen and Sabo, Ljubica and Ristić, Slavica and Savić, Aleksandar and Petričević, Saša and Nikolić, Nadežda and Vukadinović, Aleksandar and Janković, Drina and Sabo, Tibor and Vranješ-Đurić, Sanja",
year = "2016",
abstract = "The extensive development of radiopharmaceuticals towards early tumour detection and treatment has increased the demand for new ligands with higher tumour selectivity. Research has been done on the potential of the novel O,O'-diethylethylenediamine-N,N'-di-3-propanoate (L) ligand as a radionuclide vehicle for tumour targeting. Under alkaline conditions, L hydrolyses and produces half ester ligand (L') and diacid ligand (L"), with characteristic donor atom array N, N, O. Ligand L was successfully labelled with Tc-99m at pH=9 by coordination with the octahedral fac-[Tc-99m(CO)(3)(H2O)(3)](+) intermediate, forming the main radioproduct fac-[(TcL)-Tc-99m'(CO)(3)] (Tc1). The Tc-99m complex showed a low lipophilic character (log P = 0.48) and low binding affinity to human serum albumin (2.51 +/- 0.48%). In vitro stability studies in saline and human plasma, as well as challenge studies with cysteine and histidine, revealed high stability of the complex during 24 h. Biodistribution studies of Tc1 in female C57BL/6 mice bearing B16/F1 melanoma metastases showed significant tumour uptake: 9.81 +/- 1.19% ID g(-1) in the liver, 5.87 +/- 0.54% ID g(-1) in the lungs and 3.17 +/- 0.33% ID g(-1) in the ovary at 30 min post-injection. Favourable physicochemical properties, satisfactory in vitro/in vivo stability and biodistribution profile in the experimental metastatic melanoma model indicate the possible application of the radiolabelled ligand in tumour diagnosis. Copyright (C) 2015 John Wiley & Sons, Ltd.",
publisher = "Wiley, Hoboken",
journal = "Applied Organometallic Chemistry",
title = "Synthesis and biological evaluation of Tc-99m tricarbonyl complex of O,O '-diethylethylenediamine-N,N '-di-3-propanoate as potential tumour diagnostic agent",
volume = "30",
number = "2",
pages = "81-88",
doi = "10.1002/aoc.3401",
url = "Kon_3001"
}
Lakić, M., Sabo, L., Ristić, S., Savić, A., Petričević, S., Nikolić, N., Vukadinović, A., Janković, D., Sabo, T.,& Vranješ-Đurić, S.. (2016). Synthesis and biological evaluation of Tc-99m tricarbonyl complex of O,O '-diethylethylenediamine-N,N '-di-3-propanoate as potential tumour diagnostic agent. in Applied Organometallic Chemistry
Wiley, Hoboken., 30(2), 81-88.
https://doi.org/10.1002/aoc.3401
Kon_3001
Lakić M, Sabo L, Ristić S, Savić A, Petričević S, Nikolić N, Vukadinović A, Janković D, Sabo T, Vranješ-Đurić S. Synthesis and biological evaluation of Tc-99m tricarbonyl complex of O,O '-diethylethylenediamine-N,N '-di-3-propanoate as potential tumour diagnostic agent. in Applied Organometallic Chemistry. 2016;30(2):81-88.
doi:10.1002/aoc.3401
Kon_3001 .
Lakić, Mladen, Sabo, Ljubica, Ristić, Slavica, Savić, Aleksandar, Petričević, Saša, Nikolić, Nadežda, Vukadinović, Aleksandar, Janković, Drina, Sabo, Tibor, Vranješ-Đurić, Sanja, "Synthesis and biological evaluation of Tc-99m tricarbonyl complex of O,O '-diethylethylenediamine-N,N '-di-3-propanoate as potential tumour diagnostic agent" in Applied Organometallic Chemistry, 30, no. 2 (2016):81-88,
https://doi.org/10.1002/aoc.3401 .,
Kon_3001 .

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