Manganese(III) porphyrin oligomers as high-relaxivity MRI contrast agents.

Bioorg Med Chem

School of Medicine, Zhejiang University City College, Zhejiang, Hangzhou 310015, PR China. Electronic address:

Published: April 2021

Manganese(III) porphyrins (MnPs) as MRI contrast agents (CAs) have drawn particular attention due to their high longitudinal relaxivity (r) and unique biodistribution. In this work, two MnP-based oligomers, MnPD and MnPT, were designed to further improve the relaxivity with ease of synthesis. The two compounds were fully characterized and their nuclear magnetic relaxation dispersion (NMRD) profiles were acquired with a fast field cycling NMR relaxometer. Both of the compounds exhibited extended high molar r at high fields, higher than that of Gd-DTPA, the first clinical gadolinium(III)-based MRI CA. The r value of per manganese atom increased with the increasing number of MnP building blocks, suggesting rotational correlation time (τ) played dominant role in the r dispersion. The toxicity of the two MnPs and the imaging effectiveness were estimated in vitro and in vivo. With good biocompatibility, significant contrast enhancement, and complete excretion in 24 h, MnPD and MnPT are both promising for high field clinical applications. The applied strategy also potentially provided a facile approach for creation of more MnP oligomer as efficient T MRI CAs.

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http://dx.doi.org/10.1016/j.bmc.2021.116090DOI Listing

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