Hypericin-Apomyoglobin: An Enhanced Photosensitizer Complex for the Treatment of Tumor Cells

Paolo Bianchini*, Marco Cozzolino, Michele Oneto, Luca Pesce, Francesca Pennacchietti, Massimiliano Tognolini, Carmine Giorgio, Santi Nonell, Luigi Cavanna, Pietro Delcanale, Stefania Abbruzzetti, Alberto Diaspro, Cristiano Viappiani

*Corresponding author for this work

Research output: Indexed journal article Articlepeer-review

24 Citations (Scopus)

Abstract

Bioavailability of photosensitizers for cancer photodynamic therapy is often hampered by their low solubility in water. Here, we overcome this issue by using the water-soluble protein apomyoglobin (apoMb) as a carrier for the photosensitizer hypericin (Hyp). The Hyp-apoMb complex is quickly uptaken by HeLa and PC3 cells at submicromolar concentrations. Fluorescence emission of Hyp-apoMb is exploited to localize the cellular distribution of the photosensitizer. The plasma membrane is rapidly and efficiently loaded, and fluorescence is observed in the cytoplasm only at later times and to a lesser extent. Comparison with cells loaded with Hyp alone demonstrates that the uptake of the photosensitizer without the protein carrier is a slower, less efficient process, that involves the whole cell structure without preferential accumulation at the plasma membrane. Cell viability assays demonstrate that the Hyp-apoMb exhibits superior performance over Hyp. Similar results were obtained using tumor spheroids as three-dimensional cell culture models.

Original languageEnglish
Pages (from-to)2024-2033
Number of pages10
JournalBiomacromolecules
Volume20
Issue number5
Early online date17 Apr 2019
DOIs
Publication statusPublished - 13 May 2019

Keywords

  • Human serum-albumin
  • Photodynamic therapy
  • In-vitro
  • Fluorescence microscopy
  • Cancer
  • Spheroids
  • Accumulation
  • Hypocrellin
  • Mechanism
  • Proteins

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