Dual-modal polypeptide-containing contrast agents for magnetic resonance/fluorescence imaging

ElsevierVolume 129, December 2022, 106161Bioorganic ChemistryHighlights•

Dual-modal MRI/FI gents were made by incorporation of Gd-DTPA and RhB to Laminin/Fibronectin receptor-targeting sequences.

Dual-modal MRI/FI gents possessed low cell cytotoxicity, high relativity, good tumor-targeting and good fluorescent property.

Dual-modal MRI/FI gents showed good performance of combined MRI with FI and improve the accuracy of tumor detection.

Abstract

Dual-modal magnetic resonance/fluorescent imaging (MRI/FI) attracts more and more attentions in diagnosis of tumors. A corresponding dual-modal imaging agent with sufficient tumor sensitivity and specificity should be matched to improve imaging quality. Tripeptide (RGD) and pentapeptide (YIGSR) were selected as the tumor-targeting groups and attached to gadolinium diethylenetriaminepentaacetic acid (Gd-DTPA) and rhodamine B (RhB), and then make two novel polypeptide-based derivatives (RGD-Gd-DTPA-RhB and YIGSR-Gd-DTPA-RhB), respectively. These derivatives were further characterized and their properties, such as cell uptake, cell cytotoxicity, MRI and FI assay, were measured. YIGSR-Gd-DTPA-RhB and RGD-Gd-DTPA-RhB had high relaxivity, good tumor-targeting property, low cell cytotoxicity and good red FI in B16F10 melanoma cells. Moreover, YIGSR-Gd-DTPA-RhB and RGD-Gd-DTPA-RhB possessed high uptake to B16F10 melanoma, and then achieve highly enhanced FI and MRI of tumors in mice for a prolonged time. Therefore, YIGSR-Gd-DTPA-RhB and RGD-Gd-DTPA-RhB can be applied as the potential agents for tumor targeted MRI/FI in vivo.

Keywords

Magnetic resonance imaging

Fluorescent imaging

Dual-modal imaging

YIGSR

RGD

RhB

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© 2022 Published by Elsevier Inc.

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