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Ellipticine-aimed polymer-conjugated Auger electron emitter: multistage organelle targeting approach
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SYSNO ASEP 0360736 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Ellipticine-aimed polymer-conjugated Auger electron emitter: multistage organelle targeting approach Author(s) Sedláček, Ondřej (UMCH-V) RID, ORCID
Hrubý, Martin (UMCH-V) RID, ORCID
Studenovský, Martin (UMCH-V) RID, ORCID
Kučka, Jan (UMCH-V) RID, ORCID
Větvička, David (MBU-M)
Kovář, Lubomír (MBU-M)
Říhová, Blanka (MBU-M) RID
Ulbrich, Karel (UMCH-V) RIDSource Title Bioconjugate Chemistry. - : American Chemical Society - ISSN 1043-1802
Roč. 22, č. 6 (2011), s. 1194-1201Number of pages 8 s. Language eng - English Country US - United States Keywords ellipticine ; drug delivery ; radiotherapy Subject RIV CD - Macromolecular Chemistry R&D Projects GPP207/10/P054 GA ČR - Czech Science Foundation (CSF) GAP108/10/1560 GA ČR - Czech Science Foundation (CSF) IAAX00500803 GA AV ČR - Academy of Sciences of the Czech Republic (AV ČR) 1M0505 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) CEZ AV0Z40500505 - UMCH-V (2005-2011) AV0Z50200510 - MBU-M (2005-2011) UT WOS 000291568200024 DOI 10.1021/bc200064v Annotation We describe an ellipticine derivative-bound iodine-125 attached to hydrazide moieties containing poly[N-(2-hydroxypropyl)methacrylamide]. The system is completely stable at pH 7.4, while iodine-containing biologically active intercalator is released upon decrease of pH (25% intercalator released after 24 h incubation at pH 5.0—model of late endosomes). Both 2-N-(2-oxobutyl)-9-iodoellipticinium bromide and the noniodinated 2-N-(2-oxobutyl)ellipticinium bromide are potent intercalators, as proven by direct titration with DNA and ethidium displacement assay, and readily penetrate into cell nuclei, as proven by confocal microscopy. They retain chemotherapeutical antiproliferative properties of ellipticine against Raji, EL-4, and 4T1cells with IC50 in the range 0.27–8.8 μmol/L. Polymer conjugate of 2-N-(2-oxobutyl)-9-iodoellipticinium bromide is internalized into endosomes, releases active drug, possesses cytotoxic activity, and the drug accumulates in cell nuclei. Workplace Institute of Macromolecular Chemistry Contact Eva Čechová, cechova@imc.cas.cz ; Tel.: 296 809 358 Year of Publishing 2012
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