Synthesis and biological evaluation of a novel Glucosylated Derivative of Gadolinium Diethylenetriaminepentaacetic acid for Tumor Magnetic Resonance Imaging

Document Type: Research article

Authors

1 Department of Medicinal Chemisry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran.

2 Medical Physics Department, Faculty of Medicine, Tehran University of Medical Sciences, Tehran,Iran.

3 Department of Radiopharmacy, Faculty of Pharmacy, Tehran University of Medical Sciences,Tehran, Iran.

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 tri amine penta acetic acid then loaded by gadolinium to make novel agent of functional MR imaging. The relaxivity, T1, T2 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. The Gd3+-p-SCN-Bn‐DTPA‐DG significantly decreased MCF-7 tumor cell numbers without any significant toxicity on normal human kidney cells. Finally, it displayed an intense signal on T1 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.

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