Intracellular Dual Fluorescent Lightup Bioprobes for Image-Guided Photodynamic Cancer Therapy

Small. 2016 Jul;12(28):3870-8. doi: 10.1002/smll.201600950. Epub 2016 Jun 20.

Abstract

An intracellular dual fluorescent light-up bioprobe with aggregation-induced emission features and endogenously producing photosensitizer protoporphyrin IX (PpIX) abilities is designed and synthesized. The bioprobe is nonemissive in physiological environment. However, the bioprobe can selectively light up cancer cells with blue fluorescence of tetraphenylene (TPE) and red fluorescence of PpIX, owing to the release of TPE and methyl aminolevulinate after targeted internalization by cancer cells. Moreover, upon endogenous generation and accumulation of PpIX in cancer cells, efficient photodynamic ablation of cancer cells after light irradiation is demonstrated with easy regulation for optimal therapeutic efficacy. The design of such dual fluorescent light-up bioprobes might provide a new opportunity for targeted and image-guided photodynamic cancer therapy.

Keywords: 5-aminolevulinic acid; AIE; endogenous photosensitizers; fluorescent lightup; photodynamic therapy.

MeSH terms

  • A549 Cells
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Fluorescence
  • Humans
  • Magnetic Resonance Spectroscopy
  • Microscopy, Fluorescence
  • Photochemotherapy / methods*
  • Photosensitizing Agents / chemistry*
  • Photosensitizing Agents / pharmacology
  • Protoporphyrins / chemistry
  • Protoporphyrins / pharmacology
  • Stilbenes / chemistry

Substances

  • Photosensitizing Agents
  • Protoporphyrins
  • Stilbenes
  • tetraphenylethylene
  • protoporphyrin IX