Microwave-assisted synthesis and 99mTc-radiolabeling of anti-inflammatory active curcumin derivatives for inflammation diagnosis and therapy

Abstract

Using a one-pot cyclo-condensation process under microwave irradiation, derivatives of curcumin have been created. Evaluation their anti-inflammatory efficacy showed that they had stronger properties than curcumin. Additionally, the most active derivative was radiolabeled with the diagnostic radioisotope technetium-99m and prepared with a high radiochemical yield (96.5 ± 0.09%) and in vitro stability of up to 6 h. The in-vivo study in inflamed mice showed that [99mTc]Tc-curcumin derivative accumulated with a high target to non-target ratio. The gathered information confirmed the efficacy of the [99mTc]Tc-curcumin derivative as a novel possible tracer for the identification and localization of inflammation.