Development, synthesis, and 68 Ga-Labeling of a Lipophilic complexing agent for atherosclerosis PET imaging

Cardiovascular disease is the leading cause of mortality and morbidity worldwide. Atherosclerosis accounts for 50% of deaths in western countries. This multifactorial pathology is characterized by the accumulation of lipids and inflammatory cells within the vascular wall, leading to plaque formation...

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Published inEuropean journal of medicinal chemistry Vol. 176; p. 129
Main Authors Yong-Sang, Jennyfer, Dioury, Fabienne, Meneyrol, Vincent, Ait-Arsa, Imade, Idoumbin, Jean-Patrick, Guibbal, Florian, Patché, Jessica, Gimié, Fanny, Khantalin, Ilya, Couprie, Joël, Giraud, Pierre, Benard, Sébastien, Ferroud, Clotilde, Jestin, Emmanuelle, Meilhac, Olivier
Format Journal Article
LanguageEnglish
Published France 02.05.2019
Subjects
HDL
Imaging agents
Atherosclerosis
Radiochemistry
Positron emission tomography
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Summary:Cardiovascular disease is the leading cause of mortality and morbidity worldwide. Atherosclerosis accounts for 50% of deaths in western countries. This multifactorial pathology is characterized by the accumulation of lipids and inflammatory cells within the vascular wall, leading to plaque formation. We describe herein the synthesis of a PCTA-based Ga chelator coupled to a phospholipid biovector 1,2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE), which is the main constituent of the phospholipid moiety of High-Density Lipoprotein (HDL) phospholipid moiety. The resulting Ga-PCTA-DSPE inserted into HDL particles was compared to F-FDG as a PET agent to visualize atherosclerotic plaques. Our agent markedly accumulated within mouse atheromatous aortas and more interestingly in human endarterectomy carotid samples. These results support the potential use of Ga-PCTA-DSPE-HDL for atherosclerosis PET imaging.
ISSN:1768-3254