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Molecules 2019, 24(8), 1477;

Preparation and Properties of Tumor-Targeting MRI Contrast Agent Based on Linear Polylysine Derivatives

Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, China
Author to whom correspondence should be addressed.
Received: 14 February 2019 / Revised: 10 April 2019 / Accepted: 14 April 2019 / Published: 15 April 2019
(This article belongs to the Section Macromolecular Chemistry)
PDF [2436 KB, uploaded 15 April 2019]


We developed a tumor-targeted contrast agent based on linear polylysine (PLL) by conjugating a small molecular imaging agent, fluorescent molecule and targeting agent amino phenylboronic acid onto the amino groups of polylysine, which can specifically target monosaccharide sialic acid residues overexpressing on the surface of tumor cell membranes. Further, 3,4,5,6-Tetrahydrophthalic anhydride (DCA) was attached to the free amino groups of the polylysine to change to a negative charge at physiology pH to lower the cytotoxicity, but it soon regenerated to a positive charge again once reaching the acidic intratumoral environment and therefore increased cell uptake. Laser confocal microscopy images showed that most of the polymeric contrast agents were bound to the cancer cell membrane. Moreover, the tumor targeting contrast agent showed the same magnetic resonance imaging (MRI) contrasting performance in vitro as the small molecule contrast agent used in clinic, which made it a promising tumor-targeting polymeric contrast agent for cancer diagnosis. View Full-Text
Keywords: magnetic resonance imaging (MRI); polylysine; tumor targeting; charge reversal magnetic resonance imaging (MRI); polylysine; tumor targeting; charge reversal

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Sun, X.; Cai, Y.; Xu, Z.; Zhu, D. Preparation and Properties of Tumor-Targeting MRI Contrast Agent Based on Linear Polylysine Derivatives. Molecules 2019, 24, 1477.

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