4.6 Article

Selenium-Platinum Coordination Compounds as Novel Anticancer Drugs: Selectively Killing Cancer Cells via a Reactive Oxygen Species (ROS)-Mediated Apoptosis Route

Journal

CHEMISTRY-AN ASIAN JOURNAL
Volume 9, Issue 8, Pages 2295-2302

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/asia.201402256

Keywords

antitumor agents; cancer; coordination chemistry; reactive oxygen species; selenium

Funding

  1. National Basic Research Program of China [2013CB834502]
  2. National Natural Science Foundation of China [21074066]
  3. Foundation for Innovative Research Groups of the National Natural Science Foundation of China [21121004]
  4. Chinese Ministry of Education [113006A]
  5. Tsinghua University Initiative Scientific Research Program [2012Z02131]
  6. Importation and Development of High-Caliber Talents Project of Beijing Municipal Institutions
  7. NSFC-DFG [TRR 61]

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We report the preparation of selenium-containing platinum-based anticancer drug EG-Se/Pt. EG-Se/Pt was obtained from the coordination of selenium-containing molecules (EGSe) with cisplatin (CDDP). The structure of EG-Se/Pt was characterized by H-1 and Se-77 NMR spectroscopy, XPS, ESI-MS, and MALDI-TOF. In aqueous solution, EG-Se/Pt self-assembles to form spherical aggregates. EG-Se/Pt shows enhanced stability against dilution and high salt concentration compared with EG-Se. EG-Se/Pt induces cell apoptosis via reactive oxygen species (ROS), which leads to high selectivity between cancer cells and normal cells in cytotoxicity assays. More importantly, EG-Se/Pt effectively inhibits tumor growth in vivo in tumor-bearing mice. It is anticipated that tuning the ROS level through the assembly of selenium-containing molecules can be a general method to realize anticancer selectivity.

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