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Preparation and Properties of Tumor-Targeting MRI Contrast Agent Based on Linear Polylysine Derivatives
- Source :
- Molecules, Volume 24, Issue 8, Molecules, Vol 24, Iss 8, p 1477 (2019)
- Publication Year :
- 2019
- Publisher :
- MDPI AG, 2019.
-
Abstract
- 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.
- Subjects :
- magnetic resonance imaging (MRI)
MRI contrast agent
Contrast Media
Pharmaceutical Science
02 engineering and technology
01 natural sciences
Article
Madin Darby Canine Kidney Cells
Analytical Chemistry
law.invention
lcsh:QD241-441
chemistry.chemical_compound
Dogs
lcsh:Organic chemistry
Confocal microscopy
law
Neoplasms
Drug Discovery
Animals
Humans
Physical and Theoretical Chemistry
Phenylboronic acid
Cytotoxicity
Microscopy, Confocal
tumor targeting
010405 organic chemistry
Organic Chemistry
Hep G2 Cells
polylysine
021001 nanoscience & nanotechnology
Magnetic Resonance Imaging
Small molecule
0104 chemical sciences
Sialic acid
Membrane
chemistry
Chemistry (miscellaneous)
Polylysine
Biophysics
Molecular Medicine
0210 nano-technology
charge reversal
Subjects
Details
- ISSN :
- 14203049
- Volume :
- 24
- Database :
- OpenAIRE
- Journal :
- Molecules
- Accession number :
- edsair.doi.dedup.....2e6774ff11c403e3926d056d18ad0012