Activity Control of Photosensitizers for Photodynamic Therapy through DNA Recognition

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The purpose of this study is the activity control of photosensitizers for photodynamic therapy, which is a promising treatment of cancer and some non-malignant conditions. Berberine and palmatine can photosensitize the generation of singlet oxygen only when these photosensitizers bind to DNA. This study revealed the sequence specificity on the activity control of these photosensitizers, suggesting the possibility of design of sequence-specific photosensitizer. To apply this control mechanism for clinical using porphyrinoid photosensitizer, the electron donor connecting porphyrins were synthesized. The photoexcited states of these porphyrins were quenched via intramolecular electron transfer. The interaction with DNA inhibited the electron transfer quenching of these photoexcited porphyrins, leading to the singlet oxygen generation via photoenergy transfer to molecular oxygen. These findings demonstrated that the DNA-selective photosensitizers can be developed using electron donor connecting porphyrins.