Mitochondria‐Targeting Polyamine–Protoporphyrin Conjugates for Photodynamic Therapy |
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| Authors: | Dr. Fargol Taba Dr. Akira Onoda Dr. Urara Hasegawa Toshiaki Enoki Prof. Dr. Yousuke Ooyama Prof. Dr. Joji Ohshita Prof. Dr. Takashi Hayashi |
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| Affiliation: | 1. Department of Applied Chemistry, Graduate School of Engineering, Osaka University, Suita, Osaka, Japan;2. Department of Chemical Engineering, Kansas State University, Manhattan, KS, USA;3. Department of Applied Chemistry, School of Engineering, Hiroshima University, Higashi-Hiroshima, Japan |
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| Abstract: | 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. |
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| Keywords: | mitochondria photodynamic therapy polyamines porphyrins |
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