Botár, Richárd and Molnár, Enikő and Garda, Zoltán and Madarasi, Enikő and Trencsényi, György and Kiss, János and Kálmán, Ferenc Krisztián and Tircsó, Gyula (2022) Synthesis and characterization of a stable and inert Mn-II-based Zn-II responsive MRI probe for molecular imaging of glucose stimulated zinc secretion (GSZS). INORGANIC CHEMISTRY FRONTIERS, 9 (3). pp. 577-583. ISSN 2052-1545 (print); 2052-1553 (online)
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Abstract
A new potential Zn(II) responsive Mn(II)-based MRI CA candidate derived form pyclen-3,9-diacetate (3,9-PC2A) has been synthesized possessing a di-(2-picolyl)amine (DPA) moiety as an active arm. The PC2A-DPA ligand was found to form thermodynamically stable complex with Mn(II) (log KMnL=15.87(6) which translate into pMn of 8.79) which also posses an outstanding inertness towards Zn(II) ion triggered transmetallation (t1/2 at pH=6.0 is 64.5 h). The [Mn(PC2A-DPA)] complex has relatively high relaxivity (3.24 mM-1s-1 at 1.41 T and 37 oC) which is not affected by Zn(II) concentration directly, yet in the co-presence of Human Serum Albumin (HSA) relaxivity values (both r1p and r2p) increased significantly (12.14 mM-1s-1 at 1.41 T and 37 oC) owing to the efficient binding of the complex to the protein (log Kaff=3.5±0.1 M-1). The increase is large enough to visualize it by MR imaging on phantoms in vitro while in vivo MRI experiments confirmed that the glucose stimulated Zn(II) secretion (GSZS) can be visualized in a prostate of healthy mice.
| Item Type: | Article |
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| Additional Information: | Funding details: POC-012 Funding details: European Commission, EC Funding details: Magyar Tudományos Akadémia, MTA Funding details: Emberi Eroforrások Minisztériuma Funding details: European Regional Development Fund, FEDER, GINOP-2.3.2-15-2016-00008 Funding details: Debreceni Egyetem, DE Funding details: Nemzeti Kutatási Fejlesztési és Innovációs Hivatal, NKFI, 134694, FK-134551, K-120224 Funding text 1: The authors are thankful for the financial support from the Hungarian National Research, Development and Innovation Office (NKFIH K-120224, 134694 and FK-134551 projects), the University of Debrecen Innovation Fund (POC-012), and the János Bolyai Research Scholarship of the Hungarian Academy of Sciences (G. T. and F. K. K.). The research was supported by the ÚNKP-18-4 new national excellence program of the Ministry of Human Capacities (G. T. and F. K. K.) and by the EU and co-financed by the European Regional Development Fund under the project GINOP-2.3.2-15-2016-00008. Richárd Botár and Enikő Madarasi were also supported by the Doctoral School of Chemistry at the University of Debrecen, Debrecen, Hungary. The authors wish to thank the Translational Imaging Centre of Scanomed Ltd (Debrecen, Hungary) for the help pro- vided in the preclinical MRI imaging. The authors thank Prof. Imre Tóth (UD) for helpful discussions. |
| Uncontrolled Keywords: | BINDING; LIGANDS; COMPLEXES; ZINC; GLUCOSE; Magnetic Resonance Imaging; LACTATE; CONTRAST AGENTS; gadolinium; Molecular imaging; Thermodynamically stable; A-stable; MR Imaging; Human serum albumins; Synthesis and characterizations; Transmetallation; co-presence; RELAXATION RATES; Synthesised; Paramagnetic shift; Stable complexes; |
| Subjects: | Q Science / természettudomány > QD Chemistry / kémia > QD03 Inorganic chemistry / szervetlen kémia |
| SWORD Depositor: | MTMT SWORD |
| Depositing User: | MTMT SWORD |
| Date Deposited: | 12 Sep 2022 11:15 |
| Last Modified: | 12 Sep 2022 11:15 |
| URI: | http://real.mtak.hu/id/eprint/148309 |
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