Design and synthesis of heavy atom-free photosensitizers based on the biradical intersystem crossing mechanism and its application to photodynamic therapy

2020 Fiscal Year Final Research Report

• Project/Area Number: 16H04176
• Research Category: Grant-in-Aid for Scientific Research (B)
• Allocation Type: Single-year Grants
• Section: 一般
• Research Field: Bio-related chemistry
• Research Institution: Tokyo Institute of Technology
• Principal Investigator: YUASA HIDEYA 東京工業大学, 生命理工学院, 教授 (90261156)
• Project Period (FY): 2016-04-01 – 2021-03-31
• Keywords: 光増感剤 / 光線力学治療 / CT吸収 / ビフェニル誘導体 / 項間交差

Outline of Final Research Achievements

We succeeded in the development of biphenyl derivatives as a new intramolecular CT photosensitizer on the basis of our own triplet-producing mechanism. We exploited this photosensitizer for the photodynamic damage of cancer cells. We also found that the biphenyl photosensitizer can be excited by two-photon excitation with a near-infrared laser, which enables deep-tissue entry. Overall, we have accomplished almost all the goals first planned, except for animal experiments.

Free Research Field

生物有機化学

Academic Significance and Societal Importance of the Research Achievements

これまでの多くの増感剤は、分子量が500以上であり、チャネルタンパク質の孔、DNAメジャーグルーブ、酵素ポケットなど狭い空間に収まりにくく、増感剤の生体応用の選択肢が狭かった。研究代表者らが開発したビフェニル誘導体は分子量がグルコースを付けても435と非常に小さく、グルコース輸送体の孔などを標的にできる。そのため、今後、種々の生体応用が期待できる。また、医薬品としても体内滞留時間を短くできるなどの利点があげられる。