Novel radical‐responsive MRI contrast agent based on paramagnetic liposomes | Zendy

Gløgård Christian | Zendy; Stensrud Gry | Zendy; Aime Silvio | Zendy

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Novel radical‐responsive MRI contrast agent based on paramagnetic liposomes

Author(s) -

Gløgård Christian,

Stensrud Gry,

Aime Silvio

Publication year - 2003

Publication title -

magnetic resonance in chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.483

H-Index - 72

eISSN - 1097-458X

pISSN - 0749-1581

DOI - 10.1002/mrc.1208

Subject(s) - chemistry , liposome , dithiothreitol , moiety , gadolinium , chelation , thiol , linker , radical , conjugated system , in vivo , cysteine , combinatorial chemistry , photochemistry , stereochemistry , organic chemistry , biochemistry , polymer , microbiology and biotechnology , computer science , biology , enzyme , operating system

A novel, radical responsive MRI contrast agent based on a gadolinium chelate conjugated to a liposome through a disulfide linker was synthesized, with the aim of pursuing the in vivo mapping of radicals. The liposome was prepared by incorporating a thiol‐activated phospholipid, which was subsequently reacted with a gadolinium chelate containing a free thiol group. The long reorientational motion of the supramolecular adduct endows the paramagnetic agent with a relaxivity significantly higher than that of the free complex. The disulfide bond represents a radical‐sensitive moiety and a large decrease in contrast efficacy ( T 1 relaxivity) is shown upon its cleavage. A preliminary assessment of the system was made by means of in vitro gamma‐irradiation and thiol–disulfide bond exchange with dithiothreitol. Both methods showed a clear dose‐dependent decrease in T 1 ‐relaxivity. Copyright © 2003 John Wiley & Sons, Ltd.

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