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Gadolinium chelate with DO3A conjugated 2-(diphenylphosphoryl)-ethyldiphenylphosphonium cation as potential tumor-selective MRI contrast agent

Paper ID Volume ID Publish Year Pages File Format Full-Text
6821 519 2012 7 PDF Available
Title
Gadolinium chelate with DO3A conjugated 2-(diphenylphosphoryl)-ethyldiphenylphosphonium cation as potential tumor-selective MRI contrast agent
Abstract

A series of organic cations, such as triphenylphosphonium (TPP), 2-(diphenylphosphoryl)-ethyldiphenylphosphonium (TPEP), represent molecular probes for imaging tumors. These organic cations have been labeled with 64Cu radioisotope for imaging tumors by positron emission tomograghy (PET). Among these organic cation ligands, TPEP was selected for extensive evaluation using magnetic resonance imaging (MRI) based on its higher tumor uptake and better Tumor/Background (T/B) ratios. This report presents the development of a new Gd(III) chelate [Gd(DO3A-xy-TPEP)]+ as a cationic MRI contrast agent. The contrast agent was synthesized and characterized in vitro and in vivo. In vitro cell viability showed low cytotoxicity at low [Gd] concentrations. Cell uptake experiment shows that the [Gd(DO3A-xy-TPEP)]+ has high affinity for tumor cells. The in vitro T1 relaxivity measured at 9.4 T is about 50% higher than those of contrast agents in clinical use: Gd-DTPA (Magnevist) and Gd-DOTA (Dotarem). In vivo imaging studies in tumor-bearing mice at 7.0 T demonstrated significant signal enhancement at the site of the tumors. [Gd(DO3A-xy-TPEP)]+ is a promising tumor-targeting MRI contrast agent for diagnostic imaging.

Keywords
Gadolinium complex; Contrast agent; Magnetic resonance imaging (MRI); Tumor targeting; DO3A conjugated cation
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Gadolinium chelate with DO3A conjugated 2-(diphenylphosphoryl)-ethyldiphenylphosphonium cation as potential tumor-selective MRI contrast agent
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Publisher
Database: Elsevier - ScienceDirect
Journal: Biomaterials - Volume 33, Issue 36, December 2012, Pages 9225–9231
Authors
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Subjects
Physical Sciences and Engineering Chemical Engineering Bioengineering
Get Full-Text Now
Don't Miss Today's Special Offer
Price was $35.95
You save - $31
Price after discount Only $4.95
100% Money Back Guarantee
Full-text PDF Download
Online Support
Any Questions? feel free to contact us