A novel tumor and mitochondria dual-targeted photosensitizer showing ultra-efficient photodynamic anticancer activities

Chem Commun (Camb). 2019 Jan 15;55(6):866-869. doi: 10.1039/c8cc09456j.

Abstract

We designed and synthesized a simple, but highly effective photosensitizer (G-Mito-Pc), which can precisely target the mitochondria of epidermal growth factor receptor (EGFR)-overexpressing cancer cells, to achieve dual targeting function at both cell and organelle levels in cancer therapy. We further explored the possible molecular mechanism of the enhanced bioactivity of G-Mito-Pc compared to that of the reference photosensitizer using molecular dynamics simulations on their interactions with a physiologically relevant mitochondrial membrane model.

MeSH terms

  • Cell Survival / drug effects
  • ErbB Receptors / genetics
  • ErbB Receptors / metabolism
  • HeLa Cells
  • Humans
  • Membrane Potential, Mitochondrial / drug effects
  • Microscopy, Confocal
  • Mitochondria / drug effects
  • Mitochondria / metabolism*
  • Molecular Dynamics Simulation
  • Neoplasms / drug therapy
  • Neoplasms / metabolism
  • Neoplasms / pathology
  • Photochemotherapy
  • Photosensitizing Agents / chemistry*
  • Photosensitizing Agents / metabolism
  • Photosensitizing Agents / pharmacology
  • Reactive Oxygen Species / metabolism
  • Thermodynamics

Substances

  • Photosensitizing Agents
  • Reactive Oxygen Species
  • ErbB Receptors