Synthesis and biodistribution studies of (3)H- and (64)Cu-labeled dendritic polyglycerol and dendritic polyglycerol sulfate.
Identifieur interne : 002784 ( Main/Exploration ); précédent : 002783; suivant : 002785Synthesis and biodistribution studies of (3)H- and (64)Cu-labeled dendritic polyglycerol and dendritic polyglycerol sulfate.
Auteurs : Kritee Pant [Allemagne] ; Dominic Gröger [Allemagne] ; Ralf Bergmann [Allemagne] ; Jens Pietzsch [Allemagne] ; Jörg Steinbach [Allemagne] ; Bim Graham [Australie] ; Leone Spiccia [Australie] ; Fannely Berthon [France] ; Bertrand Czarny [France] ; Laurent Devel [France] ; Vincent Dive [France] ; Holger Stephan [Allemagne] ; Rainer Haag [Allemagne]Source :
- Bioconjugate chemistry [ 1520-4812 ] ; 2015.
Descripteurs français
- KwdFr :
- Animaux, Chélateurs (), Composés aza (), Dendrimères (), Dendrimères (pharmacocinétique), Dendrimères (synthèse chimique), Femelle, Glycérol (), Marquage isotopique, Pipéridines (), Polymères (), Radio-isotopes du cuivre (), Radiochimie, Rats, Répartition dans les tissus, Souris, Stabilité de médicament, Sulfates (), Techniques de chimie synthétique, Tomographie par émission de positons, Tritium ().
- MESH :
- pharmacocinétique : Dendrimères.
- synthèse chimique : Dendrimères.
- Animaux, Chélateurs, Composés aza, Dendrimères, Femelle, Glycérol, Marquage isotopique, Pipéridines, Polymères, Radio-isotopes du cuivre, Radiochimie, Rats, Répartition dans les tissus, Souris, Stabilité de médicament, Sulfates, Techniques de chimie synthétique, Tomographie par émission de positons, Tritium.
English descriptors
- KwdEn :
- Animals, Aza Compounds (chemistry), Chelating Agents (chemistry), Chemistry Techniques, Synthetic, Copper Radioisotopes (chemistry), Dendrimers (chemical synthesis), Dendrimers (chemistry), Dendrimers (pharmacokinetics), Drug Stability, Female, Glycerol (chemistry), Isotope Labeling, Mice, Piperidines (chemistry), Polymers (chemistry), Positron-Emission Tomography, Radiochemistry, Rats, Sulfates (chemistry), Tissue Distribution, Tritium (chemistry).
- MESH :
- chemical , chemical synthesis : Dendrimers.
- chemical , chemistry : Aza Compounds, Chelating Agents, Copper Radioisotopes, Dendrimers, Glycerol, Piperidines, Polymers, Sulfates, Tritium.
- chemical , pharmacokinetics : Dendrimers.
- Animals, Chemistry Techniques, Synthetic, Drug Stability, Female, Isotope Labeling, Mice, Positron-Emission Tomography, Radiochemistry, Rats, Tissue Distribution.
Abstract
Dendritic polyglycerol sulfate (dPGS) is a biocompatible, bioactive polymer which exhibits anti-inflammatory activity in vivo and thus represents a promising candidate for therapeutic and diagnostic applications. To investigate the in vivo pharmacokinetics in detail, dPGS with a molecular weight of approx. 10 kDa was radiolabeled with (3)H and (64)Cu, and evaluated by performing biodistribution studies and small animal positron emission tomography (PET). (3)H-labeling was accomplished by an oxidation-reduction process with sodium periodate and [(3)H]-borohydride. (64)Cu-labeling was achieved by conjugation of isothiocyanate- or maleimide-functionalized copper(II)-chelating ligands based on 1,4-bis(2-pyridinylmethyl)-1,4,7-triazacyclononane (DMPTACN) to an amino functionalized dPGS scaffold, followed by reaction with an aqueous solution containing (64)CuCl2. Independent biodistribution by radioimaging and PET imaging studies with healthy mice and rats showed that the neutral dPG was quantitatively renally eliminated, whereas the polysulfated analogues accumulated mainly in the liver and spleen. Small amounts of the dPGS derivatives were slowly excreted via the kidneys. The degree of uptake by the reticuloendothelial system (RES) was similar for dPGS with 40% or 85% sulfation, and surface modification of the scaffold with the DMPTACN chelator did not appear to significantly affect the biodistribution profile. On the basis of our data, the applicability of bioactive dPGS as a therapeutic agent might be limited due to organ accumulation even after 3 weeks. The inert characteristics and clearance of the neutral polymer, however, emphasizes the potential of dPG as a multifunctional scaffold for various nanomedical applications.
DOI: 10.1021/acs.bioconjchem.5b00127
PubMed: 25891152
Affiliations:
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Rossendorf, Institute of Radiopharmaceutical Cancer Research, Bautzner Landstrasse 400, D-01328 Dresden, Germany.</nlm:affiliation><country xml:lang="fr">Allemagne</country><wicri:regionArea>†Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Bautzner Landstrasse 400, D-01328 Dresden</wicri:regionArea><wicri:noRegion>01328 Dresden</wicri:noRegion><wicri:noRegion>01328 Dresden</wicri:noRegion><wicri:noRegion>D-01328 Dresden</wicri:noRegion></affiliation></author><author><name sortKey="Pietzsch, Jens" sort="Pietzsch, Jens" uniqKey="Pietzsch J" first="Jens" last="Pietzsch">Jens Pietzsch</name><affiliation wicri:level="1"><nlm:affiliation>†Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Bautzner Landstrasse 400, D-01328 Dresden, Germany.</nlm:affiliation><country xml:lang="fr">Allemagne</country><wicri:regionArea>†Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Bautzner Landstrasse 400, D-01328 Dresden</wicri:regionArea><wicri:noRegion>01328 Dresden</wicri:noRegion><wicri:noRegion>01328 Dresden</wicri:noRegion><wicri:noRegion>D-01328 Dresden</wicri:noRegion></affiliation></author><author><name sortKey="Steinbach, Jorg" sort="Steinbach, Jorg" uniqKey="Steinbach J" first="Jörg" last="Steinbach">Jörg Steinbach</name><affiliation wicri:level="1"><nlm:affiliation>†Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Bautzner Landstrasse 400, D-01328 Dresden, Germany.</nlm:affiliation><country xml:lang="fr">Allemagne</country><wicri:regionArea>†Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Bautzner Landstrasse 400, D-01328 Dresden</wicri:regionArea><wicri:noRegion>01328 Dresden</wicri:noRegion><wicri:noRegion>01328 Dresden</wicri:noRegion><wicri:noRegion>D-01328 Dresden</wicri:noRegion></affiliation></author><author><name sortKey="Graham, Bim" sort="Graham, Bim" uniqKey="Graham B" first="Bim" last="Graham">Bim Graham</name><affiliation wicri:level="1"><nlm:affiliation>∥Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia.</nlm:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>∥Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052</wicri:regionArea><wicri:noRegion>VIC 3052</wicri:noRegion></affiliation></author><author><name sortKey="Spiccia, Leone" sort="Spiccia, Leone" uniqKey="Spiccia L" first="Leone" last="Spiccia">Leone Spiccia</name><affiliation wicri:level="1"><nlm:affiliation>⊥School of Chemistry, Monash University, Clayton, VIC 3800, Australia.</nlm:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>⊥School of Chemistry, Monash University, Clayton, VIC 3800</wicri:regionArea><wicri:noRegion>VIC 3800</wicri:noRegion></affiliation></author><author><name sortKey="Berthon, Fannely" sort="Berthon, Fannely" uniqKey="Berthon F" first="Fannely" last="Berthon">Fannely Berthon</name><affiliation wicri:level="1"><nlm:affiliation>#CEA-Saclay, Service d'Ingénierie Moléculaire de Protéines (SIMOPRO), Labex LERMIT, CEA-DSV-iBiTecS, 91191 Gif/Yvette Cedex, France.</nlm:affiliation><country xml:lang="fr">France</country><wicri:regionArea>#CEA-Saclay, Service d'Ingénierie Moléculaire de Protéines (SIMOPRO), Labex LERMIT, CEA-DSV-iBiTecS, 91191 Gif/Yvette Cedex</wicri:regionArea><wicri:noRegion>91191 Gif/Yvette Cedex</wicri:noRegion><wicri:noRegion>91191 Gif/Yvette Cedex</wicri:noRegion></affiliation></author><author><name sortKey="Czarny, Bertrand" sort="Czarny, Bertrand" uniqKey="Czarny B" first="Bertrand" last="Czarny">Bertrand Czarny</name><affiliation wicri:level="1"><nlm:affiliation>#CEA-Saclay, Service d'Ingénierie Moléculaire de Protéines (SIMOPRO), Labex LERMIT, CEA-DSV-iBiTecS, 91191 Gif/Yvette Cedex, France.</nlm:affiliation><country xml:lang="fr">France</country><wicri:regionArea>#CEA-Saclay, Service d'Ingénierie Moléculaire de Protéines (SIMOPRO), Labex LERMIT, CEA-DSV-iBiTecS, 91191 Gif/Yvette Cedex</wicri:regionArea><wicri:noRegion>91191 Gif/Yvette Cedex</wicri:noRegion><wicri:noRegion>91191 Gif/Yvette Cedex</wicri:noRegion></affiliation></author><author><name sortKey="Devel, Laurent" sort="Devel, Laurent" uniqKey="Devel L" first="Laurent" last="Devel">Laurent Devel</name><affiliation wicri:level="1"><nlm:affiliation>#CEA-Saclay, Service d'Ingénierie Moléculaire de Protéines (SIMOPRO), Labex LERMIT, CEA-DSV-iBiTecS, 91191 Gif/Yvette Cedex, France.</nlm:affiliation><country xml:lang="fr">France</country><wicri:regionArea>#CEA-Saclay, Service d'Ingénierie Moléculaire de Protéines (SIMOPRO), Labex LERMIT, CEA-DSV-iBiTecS, 91191 Gif/Yvette Cedex</wicri:regionArea><wicri:noRegion>91191 Gif/Yvette Cedex</wicri:noRegion><wicri:noRegion>91191 Gif/Yvette Cedex</wicri:noRegion></affiliation></author><author><name sortKey="Dive, Vincent" sort="Dive, Vincent" uniqKey="Dive V" first="Vincent" last="Dive">Vincent Dive</name><affiliation wicri:level="1"><nlm:affiliation>#CEA-Saclay, Service d'Ingénierie Moléculaire de Protéines (SIMOPRO), Labex LERMIT, CEA-DSV-iBiTecS, 91191 Gif/Yvette Cedex, France.</nlm:affiliation><country xml:lang="fr">France</country><wicri:regionArea>#CEA-Saclay, Service d'Ingénierie Moléculaire de Protéines (SIMOPRO), Labex LERMIT, CEA-DSV-iBiTecS, 91191 Gif/Yvette Cedex</wicri:regionArea><wicri:noRegion>91191 Gif/Yvette Cedex</wicri:noRegion><wicri:noRegion>91191 Gif/Yvette Cedex</wicri:noRegion></affiliation></author><author><name sortKey="Stephan, Holger" sort="Stephan, Holger" uniqKey="Stephan H" first="Holger" last="Stephan">Holger Stephan</name><affiliation wicri:level="1"><nlm:affiliation>†Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Bautzner Landstrasse 400, D-01328 Dresden, Germany.</nlm:affiliation><country xml:lang="fr">Allemagne</country><wicri:regionArea>†Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Bautzner Landstrasse 400, D-01328 Dresden</wicri:regionArea><wicri:noRegion>01328 Dresden</wicri:noRegion><wicri:noRegion>01328 Dresden</wicri:noRegion><wicri:noRegion>D-01328 Dresden</wicri:noRegion></affiliation></author><author><name sortKey="Haag, Rainer" sort="Haag, Rainer" uniqKey="Haag R" first="Rainer" last="Haag">Rainer Haag</name><affiliation wicri:level="3"><nlm:affiliation>‡Organische Chemie, Institut für Chemie und Biochemie, Freie Universität Berlin, Takustrasse 3, D-14195, Berlin, Germany.</nlm:affiliation><country xml:lang="fr">Allemagne</country><wicri:regionArea>‡Organische Chemie, Institut für Chemie und Biochemie, Freie Universität Berlin, Takustrasse 3, D-14195, Berlin</wicri:regionArea><placeName><region type="land" nuts="3">Berlin</region><settlement type="city">Berlin</settlement></placeName></affiliation></author></titleStmt><publicationStmt><idno type="wicri:source">PubMed</idno><date when="2015">2015</date><idno type="RBID">pubmed:25891152</idno><idno type="pmid">25891152</idno><idno type="doi">10.1021/acs.bioconjchem.5b00127</idno><idno type="wicri:Area/PubMed/Corpus">002D67</idno><idno type="wicri:explorRef" wicri:stream="PubMed" wicri:step="Corpus" wicri:corpus="PubMed">002D67</idno><idno type="wicri:Area/PubMed/Curation">002C92</idno><idno type="wicri:explorRef" wicri:stream="PubMed" wicri:step="Curation">002C92</idno><idno type="wicri:Area/PubMed/Checkpoint">002C92</idno><idno type="wicri:explorRef" wicri:stream="Checkpoint" wicri:step="PubMed">002C92</idno><idno type="wicri:Area/Ncbi/Merge">002479</idno><idno type="wicri:Area/Ncbi/Curation">002479</idno><idno type="wicri:Area/Ncbi/Checkpoint">002479</idno><idno type="wicri:Area/Main/Merge">002784</idno><idno type="wicri:Area/Main/Curation">002784</idno><idno type="wicri:Area/Main/Exploration">002784</idno></publicationStmt><sourceDesc><biblStruct><analytic><title xml:lang="en">Synthesis and biodistribution studies of (3)H- and (64)Cu-labeled dendritic polyglycerol and dendritic polyglycerol sulfate.</title><author><name sortKey="Pant, Kritee" sort="Pant, Kritee" uniqKey="Pant K" first="Kritee" last="Pant">Kritee Pant</name><affiliation wicri:level="1"><nlm:affiliation>†Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Bautzner Landstrasse 400, D-01328 Dresden, Germany.</nlm:affiliation><country xml:lang="fr">Allemagne</country><wicri:regionArea>†Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Bautzner Landstrasse 400, D-01328 Dresden</wicri:regionArea><wicri:noRegion>01328 Dresden</wicri:noRegion><wicri:noRegion>01328 Dresden</wicri:noRegion><wicri:noRegion>D-01328 Dresden</wicri:noRegion></affiliation></author><author><name sortKey="Groger, Dominic" sort="Groger, Dominic" uniqKey="Groger D" first="Dominic" last="Gröger">Dominic Gröger</name><affiliation wicri:level="3"><nlm:affiliation>‡Organische Chemie, Institut für Chemie und Biochemie, Freie Universität Berlin, Takustrasse 3, D-14195, Berlin, Germany.</nlm:affiliation><country xml:lang="fr">Allemagne</country><wicri:regionArea>‡Organische Chemie, Institut für Chemie und Biochemie, Freie Universität Berlin, Takustrasse 3, D-14195, Berlin</wicri:regionArea><placeName><region type="land" nuts="3">Berlin</region><settlement type="city">Berlin</settlement></placeName></affiliation></author><author><name sortKey="Bergmann, Ralf" sort="Bergmann, Ralf" uniqKey="Bergmann R" first="Ralf" last="Bergmann">Ralf Bergmann</name><affiliation wicri:level="1"><nlm:affiliation>†Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Bautzner Landstrasse 400, D-01328 Dresden, Germany.</nlm:affiliation><country xml:lang="fr">Allemagne</country><wicri:regionArea>†Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Bautzner Landstrasse 400, D-01328 Dresden</wicri:regionArea><wicri:noRegion>01328 Dresden</wicri:noRegion><wicri:noRegion>01328 Dresden</wicri:noRegion><wicri:noRegion>D-01328 Dresden</wicri:noRegion></affiliation></author><author><name sortKey="Pietzsch, Jens" sort="Pietzsch, Jens" uniqKey="Pietzsch J" first="Jens" last="Pietzsch">Jens Pietzsch</name><affiliation wicri:level="1"><nlm:affiliation>†Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Bautzner Landstrasse 400, D-01328 Dresden, Germany.</nlm:affiliation><country xml:lang="fr">Allemagne</country><wicri:regionArea>†Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Bautzner Landstrasse 400, D-01328 Dresden</wicri:regionArea><wicri:noRegion>01328 Dresden</wicri:noRegion><wicri:noRegion>01328 Dresden</wicri:noRegion><wicri:noRegion>D-01328 Dresden</wicri:noRegion></affiliation></author><author><name sortKey="Steinbach, Jorg" sort="Steinbach, Jorg" uniqKey="Steinbach J" first="Jörg" last="Steinbach">Jörg Steinbach</name><affiliation wicri:level="1"><nlm:affiliation>†Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Bautzner Landstrasse 400, D-01328 Dresden, Germany.</nlm:affiliation><country xml:lang="fr">Allemagne</country><wicri:regionArea>†Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Bautzner Landstrasse 400, D-01328 Dresden</wicri:regionArea><wicri:noRegion>01328 Dresden</wicri:noRegion><wicri:noRegion>01328 Dresden</wicri:noRegion><wicri:noRegion>D-01328 Dresden</wicri:noRegion></affiliation></author><author><name sortKey="Graham, Bim" sort="Graham, Bim" uniqKey="Graham B" first="Bim" last="Graham">Bim Graham</name><affiliation wicri:level="1"><nlm:affiliation>∥Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia.</nlm:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>∥Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052</wicri:regionArea><wicri:noRegion>VIC 3052</wicri:noRegion></affiliation></author><author><name sortKey="Spiccia, Leone" sort="Spiccia, Leone" uniqKey="Spiccia L" first="Leone" last="Spiccia">Leone Spiccia</name><affiliation wicri:level="1"><nlm:affiliation>⊥School of Chemistry, Monash University, Clayton, VIC 3800, Australia.</nlm:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>⊥School of Chemistry, Monash University, Clayton, VIC 3800</wicri:regionArea><wicri:noRegion>VIC 3800</wicri:noRegion></affiliation></author><author><name sortKey="Berthon, Fannely" sort="Berthon, Fannely" uniqKey="Berthon F" first="Fannely" last="Berthon">Fannely Berthon</name><affiliation wicri:level="1"><nlm:affiliation>#CEA-Saclay, Service d'Ingénierie Moléculaire de Protéines (SIMOPRO), Labex LERMIT, CEA-DSV-iBiTecS, 91191 Gif/Yvette Cedex, France.</nlm:affiliation><country xml:lang="fr">France</country><wicri:regionArea>#CEA-Saclay, Service d'Ingénierie Moléculaire de Protéines (SIMOPRO), Labex LERMIT, CEA-DSV-iBiTecS, 91191 Gif/Yvette Cedex</wicri:regionArea><wicri:noRegion>91191 Gif/Yvette Cedex</wicri:noRegion><wicri:noRegion>91191 Gif/Yvette Cedex</wicri:noRegion></affiliation></author><author><name sortKey="Czarny, Bertrand" sort="Czarny, Bertrand" uniqKey="Czarny B" first="Bertrand" last="Czarny">Bertrand Czarny</name><affiliation wicri:level="1"><nlm:affiliation>#CEA-Saclay, Service d'Ingénierie Moléculaire de Protéines (SIMOPRO), Labex LERMIT, CEA-DSV-iBiTecS, 91191 Gif/Yvette Cedex, France.</nlm:affiliation><country xml:lang="fr">France</country><wicri:regionArea>#CEA-Saclay, Service d'Ingénierie Moléculaire de Protéines (SIMOPRO), Labex LERMIT, CEA-DSV-iBiTecS, 91191 Gif/Yvette Cedex</wicri:regionArea><wicri:noRegion>91191 Gif/Yvette Cedex</wicri:noRegion><wicri:noRegion>91191 Gif/Yvette Cedex</wicri:noRegion></affiliation></author><author><name sortKey="Devel, Laurent" sort="Devel, Laurent" uniqKey="Devel L" first="Laurent" last="Devel">Laurent Devel</name><affiliation wicri:level="1"><nlm:affiliation>#CEA-Saclay, Service d'Ingénierie Moléculaire de Protéines (SIMOPRO), Labex LERMIT, CEA-DSV-iBiTecS, 91191 Gif/Yvette Cedex, France.</nlm:affiliation><country xml:lang="fr">France</country><wicri:regionArea>#CEA-Saclay, Service d'Ingénierie Moléculaire de Protéines (SIMOPRO), Labex LERMIT, CEA-DSV-iBiTecS, 91191 Gif/Yvette Cedex</wicri:regionArea><wicri:noRegion>91191 Gif/Yvette Cedex</wicri:noRegion><wicri:noRegion>91191 Gif/Yvette Cedex</wicri:noRegion></affiliation></author><author><name sortKey="Dive, Vincent" sort="Dive, Vincent" uniqKey="Dive V" first="Vincent" last="Dive">Vincent Dive</name><affiliation wicri:level="1"><nlm:affiliation>#CEA-Saclay, Service d'Ingénierie Moléculaire de Protéines (SIMOPRO), Labex LERMIT, CEA-DSV-iBiTecS, 91191 Gif/Yvette Cedex, France.</nlm:affiliation><country xml:lang="fr">France</country><wicri:regionArea>#CEA-Saclay, Service d'Ingénierie Moléculaire de Protéines (SIMOPRO), Labex LERMIT, CEA-DSV-iBiTecS, 91191 Gif/Yvette Cedex</wicri:regionArea><wicri:noRegion>91191 Gif/Yvette Cedex</wicri:noRegion><wicri:noRegion>91191 Gif/Yvette Cedex</wicri:noRegion></affiliation></author><author><name sortKey="Stephan, Holger" sort="Stephan, Holger" uniqKey="Stephan H" first="Holger" last="Stephan">Holger Stephan</name><affiliation wicri:level="1"><nlm:affiliation>†Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Bautzner Landstrasse 400, D-01328 Dresden, Germany.</nlm:affiliation><country xml:lang="fr">Allemagne</country><wicri:regionArea>†Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Bautzner Landstrasse 400, D-01328 Dresden</wicri:regionArea><wicri:noRegion>01328 Dresden</wicri:noRegion><wicri:noRegion>01328 Dresden</wicri:noRegion><wicri:noRegion>D-01328 Dresden</wicri:noRegion></affiliation></author><author><name sortKey="Haag, Rainer" sort="Haag, Rainer" uniqKey="Haag R" first="Rainer" last="Haag">Rainer Haag</name><affiliation wicri:level="3"><nlm:affiliation>‡Organische Chemie, Institut für Chemie und Biochemie, Freie Universität Berlin, Takustrasse 3, D-14195, Berlin, Germany.</nlm:affiliation><country xml:lang="fr">Allemagne</country><wicri:regionArea>‡Organische Chemie, Institut für Chemie und Biochemie, Freie Universität Berlin, Takustrasse 3, D-14195, Berlin</wicri:regionArea><placeName><region type="land" nuts="3">Berlin</region><settlement type="city">Berlin</settlement></placeName></affiliation></author></analytic><series><title level="j">Bioconjugate chemistry</title><idno type="eISSN">1520-4812</idno><imprint><date when="2015" type="published">2015</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term><term>Aza Compounds (chemistry)</term><term>Chelating Agents (chemistry)</term><term>Chemistry Techniques, Synthetic</term><term>Copper Radioisotopes (chemistry)</term><term>Dendrimers (chemical synthesis)</term><term>Dendrimers (chemistry)</term><term>Dendrimers (pharmacokinetics)</term><term>Drug Stability</term><term>Female</term><term>Glycerol (chemistry)</term><term>Isotope Labeling</term><term>Mice</term><term>Piperidines (chemistry)</term><term>Polymers (chemistry)</term><term>Positron-Emission Tomography</term><term>Radiochemistry</term><term>Rats</term><term>Sulfates (chemistry)</term><term>Tissue Distribution</term><term>Tritium (chemistry)</term></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Animaux</term><term>Chélateurs ()</term><term>Composés aza ()</term><term>Dendrimères ()</term><term>Dendrimères (pharmacocinétique)</term><term>Dendrimères (synthèse chimique)</term><term>Femelle</term><term>Glycérol ()</term><term>Marquage isotopique</term><term>Pipéridines ()</term><term>Polymères ()</term><term>Radio-isotopes du cuivre ()</term><term>Radiochimie</term><term>Rats</term><term>Répartition dans les tissus</term><term>Souris</term><term>Stabilité de médicament</term><term>Sulfates ()</term><term>Techniques de chimie synthétique</term><term>Tomographie par émission de positons</term><term>Tritium ()</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemical synthesis" xml:lang="en"><term>Dendrimers</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Aza Compounds</term><term>Chelating Agents</term><term>Copper Radioisotopes</term><term>Dendrimers</term><term>Glycerol</term><term>Piperidines</term><term>Polymers</term><term>Sulfates</term><term>Tritium</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacokinetics" xml:lang="en"><term>Dendrimers</term></keywords><keywords scheme="MESH" qualifier="pharmacocinétique" xml:lang="fr"><term>Dendrimères</term></keywords><keywords scheme="MESH" qualifier="synthèse chimique" xml:lang="fr"><term>Dendrimères</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Chemistry Techniques, Synthetic</term><term>Drug Stability</term><term>Female</term><term>Isotope Labeling</term><term>Mice</term><term>Positron-Emission Tomography</term><term>Radiochemistry</term><term>Rats</term><term>Tissue Distribution</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Animaux</term><term>Chélateurs</term><term>Composés aza</term><term>Dendrimères</term><term>Femelle</term><term>Glycérol</term><term>Marquage isotopique</term><term>Pipéridines</term><term>Polymères</term><term>Radio-isotopes du cuivre</term><term>Radiochimie</term><term>Rats</term><term>Répartition dans les tissus</term><term>Souris</term><term>Stabilité de médicament</term><term>Sulfates</term><term>Techniques de chimie synthétique</term><term>Tomographie par émission de positons</term><term>Tritium</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Dendritic polyglycerol sulfate (dPGS) is a biocompatible, bioactive polymer which exhibits anti-inflammatory activity in vivo and thus represents a promising candidate for therapeutic and diagnostic applications. To investigate the in vivo pharmacokinetics in detail, dPGS with a molecular weight of approx. 10 kDa was radiolabeled with (3)H and (64)Cu, and evaluated by performing biodistribution studies and small animal positron emission tomography (PET). (3)H-labeling was accomplished by an oxidation-reduction process with sodium periodate and [(3)H]-borohydride. (64)Cu-labeling was achieved by conjugation of isothiocyanate- or maleimide-functionalized copper(II)-chelating ligands based on 1,4-bis(2-pyridinylmethyl)-1,4,7-triazacyclononane (DMPTACN) to an amino functionalized dPGS scaffold, followed by reaction with an aqueous solution containing (64)CuCl2. Independent biodistribution by radioimaging and PET imaging studies with healthy mice and rats showed that the neutral dPG was quantitatively renally eliminated, whereas the polysulfated analogues accumulated mainly in the liver and spleen. Small amounts of the dPGS derivatives were slowly excreted via the kidneys. The degree of uptake by the reticuloendothelial system (RES) was similar for dPGS with 40% or 85% sulfation, and surface modification of the scaffold with the DMPTACN chelator did not appear to significantly affect the biodistribution profile. On the basis of our data, the applicability of bioactive dPGS as a therapeutic agent might be limited due to organ accumulation even after 3 weeks. The inert characteristics and clearance of the neutral polymer, however, emphasizes the potential of dPG as a multifunctional scaffold for various nanomedical applications.</div></front></TEI><affiliations><list><country><li>Allemagne</li><li>Australie</li><li>France</li></country><region><li>Berlin</li></region><settlement><li>Berlin</li></settlement></list><tree><country name="Allemagne"><noRegion><name sortKey="Pant, Kritee" sort="Pant, Kritee" uniqKey="Pant K" first="Kritee" last="Pant">Kritee Pant</name></noRegion><name sortKey="Bergmann, Ralf" sort="Bergmann, Ralf" uniqKey="Bergmann R" first="Ralf" last="Bergmann">Ralf Bergmann</name><name sortKey="Groger, Dominic" sort="Groger, Dominic" uniqKey="Groger D" first="Dominic" last="Gröger">Dominic Gröger</name><name sortKey="Haag, Rainer" sort="Haag, Rainer" uniqKey="Haag R" first="Rainer" last="Haag">Rainer Haag</name><name sortKey="Pietzsch, Jens" sort="Pietzsch, Jens" uniqKey="Pietzsch J" first="Jens" last="Pietzsch">Jens Pietzsch</name><name sortKey="Steinbach, Jorg" sort="Steinbach, Jorg" uniqKey="Steinbach J" first="Jörg" last="Steinbach">Jörg Steinbach</name><name sortKey="Stephan, Holger" sort="Stephan, Holger" uniqKey="Stephan H" first="Holger" last="Stephan">Holger Stephan</name></country><country name="Australie"><noRegion><name sortKey="Graham, Bim" sort="Graham, Bim" uniqKey="Graham B" first="Bim" last="Graham">Bim Graham</name></noRegion><name sortKey="Spiccia, Leone" sort="Spiccia, Leone" uniqKey="Spiccia L" first="Leone" last="Spiccia">Leone Spiccia</name></country><country name="France"><noRegion><name sortKey="Berthon, Fannely" sort="Berthon, Fannely" uniqKey="Berthon F" first="Fannely" last="Berthon">Fannely Berthon</name></noRegion><name sortKey="Czarny, Bertrand" sort="Czarny, Bertrand" uniqKey="Czarny B" first="Bertrand" last="Czarny">Bertrand Czarny</name><name sortKey="Devel, Laurent" sort="Devel, Laurent" uniqKey="Devel L" first="Laurent" last="Devel">Laurent Devel</name><name sortKey="Dive, Vincent" sort="Dive, Vincent" uniqKey="Dive V" first="Vincent" last="Dive">Vincent Dive</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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