Mitochondria-Targeting Polyamine–Protoporphyrin Conjugates for Photodynamic Therapy

Fargol Taba, Akira Onoda, Urara Hasegawa, Toshiaki Enoki, Yousuke Ooyama, Joji Ohshita, Takashi Hayashi

Research output: Contribution to journalArticlepeer-review

20 Scopus citations


Two polyamine derivatives of protoporphyrin IX (PPIX) were tested as photodynamic therapy (PDT) agents in HT29 colorectal cancer and HEP3B liver cancer cell lines. These compounds exhibit excellent singlet oxygen quantum yields and show strong in vitro PDT efficacy after 660 nm laser irradiation, whereas exogenous PPIX itself exhibits much weaker PDT effects. Confocal microscopy imaging studies reveal that a protoporphyrin derivative with eight amine moieties has excellent water solubility, and localizes mainly in the mitochondria of both HT29 and HEP3B cells, whereas the cellular distribution of a protoporphyrin derivative with four amine moieties is not as specific. This work demonstrates that polyamine moieties on macrocycles can enhance PDT efficacy by targeting mitochondria.

Original languageEnglish (US)
Pages (from-to)15-19
Number of pages5
Issue number1
StatePublished - Jan 8 2018

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry


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