Abstract
Curcumin is a natural occurring molecule that has aroused much interest among researchers over the years due to its pleiotropic set of biological properties. In the nuclear medicine field, radiolabelled curcumin and curcumin derivatives have been studied as potential radiotracers for the early diagnosis of Alzheimer’s disease and cancer. In the present review, the synthetic pathways, labelling methods and the preclinical investigations involving these radioactive compounds are treated. The studies entailed chemical modifications for enhancing curcumin stability, as well as its functionalisation for the labelling with several radiohalogens or metal radionuclides (fluorine-18, technetium-99m, gallium-68, etc.). Although some drawbacks have yet to be addressed, and none of the radiolabelled curcuminoids have so far achieved clinical application, the studies performed hitherto provide useful insights and lay the foundation for further developments.
Highlights
Curcumin has attracted the attention of researchers since its isolation by Lampe in 1918 [1], it was only in the 1990s, after the first reports claiming for its antioxidant [2], anti-inflammatory [3], and anticancer [4] effects, that the interest in curcumin medical applications started to grow at a rapid pace
Curcumin [(E,E)-1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione] represents the biologically active ingredient of turmeric, a yellow colouring compound found in the rhizomes of Curcuma longa L., a plant belonging to the ginger family
This review aims to provide an up-to-date overview of the recent achievements radiopharmaceuticals based on curcuminoid structure
Summary
Thanks to its straightforward and quantitative production means of the low-energy medical cyclotrons, fluorine-18 [18F]F- directly available from the cyclotron target after proper activation and purification. The reaction proceeds in aprotic solvents according to an SN 2-mechanism, with halides or sulphonic ester (namely polar aprotic solvents according to an SN2-mechanism, with halides or sulphonic ester mesylate, tosylate and triflate) acting as leaving groups. The synthesis envisaged the addition of an alkyl chain the radionuclide to one of the curcumin phenolic groups. The labelling was first attempted containing the radionuclide to one of the curcumin phenolic groups. Thethe path entailed the reaction between (1) and activated [18F]F-, folcondensation of the product with the acetylacetone-boron complex of (3).
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