Synthesis and Biological Evaluation of a Novel Glucosylated Derivative of Gadolinium Diethylenetriaminepentaacetic Acid for Tumor Magnetic Resonance Imaging.

Abstract

Cancer detection in early stage using a powerful and noninvasive tool is of high global interest. In this experiment, a small-molecular-weight glucose based derivative of Gd3+-1-(4-isothiocyanatobenzyl) diethylene tri amine penta acetic acid (Gd3+-p-SCN-Bn-DTPA-DG) as a novel potential MR imaging contrast agents was synthesized. Gd3+-p-SCN-Bn-DTPA-DG was synthesized with reacting of Glucosamine and 1-(4-isothiocyanatobenzyl) diethylene triamine penta acetic acid then loaded by gadolinium to make novel agent of functional MR imaging. The relaxivity, T 1, T 2 relaxation times, and cell toxicity of this contrast agent were studied. The results demonstrated that the sugar moieties linked to Gd3+-p-SCN-Bn-DTPA efficiently increase its cellular uptake in normal cells 25% and in cancereous cells upto 67%. The Gd3+-p-SCN-Bn-DTPA-DG significantly (p < 0.05) decreased MCF-7 tumor cell numbers without any significant toxicity on normal human kidney cells. Finally, it displayed an intense signal on T 1 weighted with respect to the unlabeled cells. Based on the findings from the present research Gd3+-p-SCN-Bn-DTPA-DG be a potential breast molecular imaging. However, further investigations by anticancer studies are in the pipeline.