Novel lysosome targeted molecular transporter built on a guanidinium-poly-(propylene imine) hybrid dendron for efficient delivery of doxorubicin into cancer cells

Chem Commun (Camb). 2015 Feb 11;51(12):2403-6. doi: 10.1039/c4cc09829c.

Abstract

An efficient synthetic approach has been adopted to construct a new dendron-based octa-guanidine appended molecular transporter with a lysosomal targeted peptide-doxorubicin conjugate. The transporter alone (G8-PPI-FL) is found to be non-toxic, showed higher cellular uptake compared to Arg-8-mer and exhibited excellent selectivity towards lysosomes in cathepsin B expressing HeLa cells, while the Dox-conjugate showed significant cytotoxicity to cancer cells without affecting the non-cancerous cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antibiotics, Antineoplastic / chemistry*
  • Antibiotics, Antineoplastic / pharmacology
  • Apoptosis / drug effects
  • Arginine / chemistry
  • Cathepsin B / metabolism
  • Dendrimers / chemistry*
  • Doxorubicin / chemistry*
  • Doxorubicin / pharmacology
  • Drug Carriers / chemistry*
  • Guanidine / chemistry*
  • HeLa Cells
  • Humans
  • Lysosomes
  • Peptides / chemistry
  • Polypropylenes / chemistry*

Substances

  • Antibiotics, Antineoplastic
  • Dendrimers
  • Drug Carriers
  • Peptides
  • Polypropylenes
  • poly(propyleneimine)
  • Doxorubicin
  • Arginine
  • Cathepsin B
  • Guanidine