Screening for cancer stem cell-targeted dinuclear platinum(II) complex

2018 Fiscal Year Final Research Report

• Project/Area Number: 17K15436
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Multi-year Fund
• Research Field: Physical pharmacy
• Research Institution: Suzuka University of Medical Science
• Principal Investigator: Uemura Masako 鈴鹿医療科学大学, 薬学部, 助教 (70511997)
• Research Collaborator: Komeda Seiji
• Project Period (FY): 2017-04-01 – 2019-03-31
• Keywords: 白金錯体 / 次世代白金制がん剤 / 大腸がん / がん幹細胞 / グルタチオン

Outline of Final Research Achievements

Cancer stem cell (CSC) concept, that CSC is concerned in cancer relapse and metastasis, has emerged in recent years. We have developed a series of tetrazolato-bridged dinuclear platinum(II) complexes (tetrazolato-bridged complexes) which has been reported to exert in vivo antitumor efficacy on mouse colorectal cancer. In this research, we performed in vitro cytotoxicity study of tetrazolato-bridged complexes on CSC of human colorectal cancer. Among them, tetrazolato-bridged complexes with fluoromethyl group decreased sizes and numbers of CSC sphere, suggesting that they could show cytotoxicity on CSCs as well. These results would contribute to a development of tetrazolato-bridged complexes and a next generation platinum anti-cancer drug.

Free Research Field

生命錯体化学

Academic Significance and Societal Importance of the Research Achievements

in vivo 抗腫瘍効果が認められている白金錯体について、がん幹細胞に対するin vitro 細胞増殖抑制活性も示す可能性が示唆されたことは、非常に興味深い。また、この結果は、テトラゾラト架橋錯体の有効性を裏付ける作用機序を明らかにする上で重要な知見であり、テトラゾラト架橋錯体の更なる構造最適化に役立てることができる。従って、本研究の成果は、臨床におけるニーズに応える次世代白金制がん剤の設計に貢献すると考えられる。