Cationic polyfluorenes for intracellular delivery of proteins

Org Biomol Chem. 2011 Oct 7;9(19):6513-8. doi: 10.1039/c1ob05874f. Epub 2011 Aug 16.

Abstract

Two cationic polyfluorene derivatives, quaternary amine 1 and guanidine 2 sheathed systems, were prepared as potential carriers to mediate import of proteins into cells without requiring covalent attachment to the protein. Neither polymer showed significant cytotoxicities (IC(50) 100 μM) when exposed to Clone 9 rat liver cells. Both polymers were shown to mediate import of a series of four proteins chosen because they have different pI values, sizes, and variable organic fluor attachments. Once inside the cells, the quaternary amine system 1 released more of its cargo into regions outside the lysosomes. In one exploratory experiment, pyrenebutyrate was shown to accelerate import of a protein system by polymer 1.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amines / chemical synthesis
  • Amines / chemistry
  • Amines / pharmacology*
  • Animals
  • CHO Cells
  • Cations / chemistry
  • Cell Survival / drug effects
  • Cells, Cultured
  • Cricetinae
  • Fluorenes / chemical synthesis
  • Fluorenes / chemistry
  • Fluorenes / pharmacology*
  • Guanidine / chemical synthesis
  • Guanidine / chemistry
  • Guanidine / pharmacology*
  • Molecular Structure
  • Polymers / chemical synthesis
  • Polymers / chemistry
  • Polymers / pharmacology*
  • Proteins / chemistry*
  • Rats
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Amines
  • Cations
  • Fluorenes
  • Polymers
  • Proteins
  • Guanidine