Abstract
BackgroundGadolinium-based contrast agents are widely used as a contrast agent for magnetic resonance imaging. Since gadolinium ions are toxic, many chelators are developed to bind gadolinium ions to prevent free gadolinium-associated disease. However, many reports indicated that linear chelator-based contrast agents are associated with nephrogenic systemic fibrosis (NSF) in patients with low kidney function. Therefore, the demand for stable macrocyclic chelator-based contrast agent is now increasing.Method1,4,7,10-Tetraazacyclododecane-1,4,7,10-tetraacetate (DOTA) was conjugated to lactobionic acid (LBA) through DCC-NHS coupling reaction. Gd3+ (gadolinium ion) was chelated to 1,4,7,10-Tetraazacyclododecane-1,4,7,10-tetraacetate-lactobionic acid (DOTA-LAE) and free Gd3+ was removed using a cation exchange column. In vitro cytotoxicity of contrast agent towards normal cells was measured using MTT assay. For in vivo MR imaging, contrast agents were intravenously injected to tumor-bearing mice and imaged by a MR imaging scanner.ResultsThis new macrocyclic gadolinium-based contrast agent showed enhanced in vitro paramagnetic properties compared to Gadovist. In addition, Gd-DOTA-LAE showed a 29% increased contrast enhancement of tumor tissue compared to normal tissue within 20 min past IV injection.ConclusionsWe developed a new macrocyclic T1-weighted MR contrast agent. This new contrast agent offers various opportunities for cancer detection and diagnosis.
Highlights
Gadolinium-based contrast agents are widely used as a contrast agent for magnetic resonance imaging
Gadolinium, manganese, iron oxide, and iron platinum-based Contrast agent (CA) are used for clinical application, because Gd3+-based Longitudinal relaxation time (T1) CAs have been proven its great safety in many clinical cases
Synthesis of Gd-DOTA-lactobionic acid-ethylenediamine (LAE) To synthesize Gd-DOTA-LAE (Fig. 1); carboxyl group of lactobionic acid was modified through the reaction with ethylenediamine to introduce primary amine on lactobionic acid (Fig. 1a) and p-DOTA was introduced to LAE
Summary
Gadolinium-based contrast agents are widely used as a contrast agent for magnetic resonance imaging. Since gadolinium ions are toxic, many chelators are developed to bind gadolinium ions to prevent free gadolinium-associated disease. Many reports indicated that linear chelator-based contrast agents are associated with nephrogenic systemic fibrosis (NSF) in patients with low kidney function. The demand for stable macrocyclic chelator-based contrast agent is increasing. Detection of cancer is essential for treatment and the survival rate of patients [1, 2]. Magnetic resonance imaging (MRI) is most frequently used imaging method for detection and diagnosis of cancer. MRI is a noninvasive method to detect soft tissue, such as organs, ligament, cartilage, and cancer regions without exposing to radiation. Gadolinium, manganese, iron oxide, and iron platinum-based CAs are used for clinical application, because Gd3+-based T1 CAs have been proven its great safety in many clinical cases
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