Mattia Mazza1,2, Cyrille Alliot1,3, Corinne Sinquin4, Sylvia Colliec-Jouault4, Pascal E Reiller5, Sandrine Huclier-Markai1,2. 1. GIP ARRONAX, 1 rue Aronnax, CS 10112, F-44817 Nantes, CEDEX 3, France. 2. SUBATECH, 4 rue Alfred Kastler, BP 20722, F-44307 Nantes, CEDEX 3, France. 3. INSERM U892-8 quai Moncousu, BP 70721, F-44007 Nantes, CEDEX 1, France. 4. IFREMER, Institut français de recherche pour l'exploitation de la mer, rue de l'Ile d'Yeu, BP 21105, F-44311 Nantes, CEDEX 3, France. 5. DES-Service d'Etudes Analytiques et de Réactivité des Surfaces (SEARS), Université Paris-Saclay, CEA, F-91191 Gif sur Yvette, CEDEX, France.
Abstract
(1) Background: Exopolysaccharide (EPS) derivatives, produced by Alteromonas infernus bacterium, showed anti-metastatic properties. They may represent a new class of ligands to be combined with theranostic radionuclides, such as 47Sc/44Sc. The goal of this work was to investigate the feasibility of such coupling. (2) Methods: EPSs, as well as heparin used as a drug reference, were characterized in terms of molar mass and dispersity using Asymmetrical Flow Field-Flow Fractionation coupled to Multi-Angle Light Scattering (AF4-MALS). The intrinsic viscosity of EPSs at different ionic strengths were measured in order to establish the conformation. To determine the stability constants of Sc with EPS and heparin, a Free-ion selective radiotracer extraction (FISRE) method has been used. (3) Results: AF4-MALS showed that radical depolymerization produces monodisperse EPSs, suitable for therapeutic use. EPS conformation exhibited a lower hydrodynamic volume for the highest ionic strengths. The resulting random-coiled conformation could affect the complexation with metal for high concentration. The LogK of Sc-EPS complexes have been determined and showing that they are comparable to the Sc-Hep. (4) Conclusions: EPSs are very promising to be coupled with the theranostic pair of scandium for Nuclear Medicine.
(1) Background: Exopolysaccharide (n class="Disease">EPS) derivatives, produced by Alteromonas infernus bacterium, showed anti-metastatic properties. They may represent a new class of ligands to be combined with theranostic radionuclides, such as 47Sc/44Sc. The goal of this work was to investigate the feasibility of such coupling. (2) Methods:EPSs, as well as heparin used as a drug reference, were characterized in terms of molar mass and dispersity using Asymmetrical Flow Field-Flow Fractionation coupled to Multi-Angle Light Scattering (AF4-MALS). The intrinsic viscosity of EPSs at different ionic strengths were measured in order to establish the conformation. To determine the stability constants of Sc with EPS and heparin, a Free-ion selective radiotracer extraction (FISRE) method has been used. (3) Results:AF4-MALS showed that radical depolymerization produces monodisperse EPSs, suitable for therapeutic use. EPS conformation exhibited a lower hydrodynamic volume for the highest ionic strengths. The resulting random-coiled conformation could affect the complexation with metal for high concentration. The LogK of Sc-EPS complexes have been determined and showing that they are comparable to the Sc-Hep. (4) Conclusions: EPSs are very promising to be coupled with the theranostic pair of scandium for Nuclear Medicine.
Authors: Miroslav Pniok; Vojtěch Kubíček; Jana Havlíčková; Jan Kotek; Andrea Sabatie-Gogová; Jan Plutnar; Sandrine Huclier-Markai; Petr Hermann Journal: Chemistry Date: 2014-05-18 Impact factor: 5.236