Radiosensitization of cancer cells by hydroxychalcones.

Radiation sensitization is significantly increased by proteotoxic stress, such as a heat shock. We undertook an investigation, seeking to identify natural products that induced proteotoxic stress and then determined if a compound exhibited radiosensitizing properties. The hydroxychalcones, 2',5'-dihydroxychalcone (D-601) and 2,2'-dihydroxychalcone (D-501), were found to activate heat shock factor 1 (Hsf1) and exhibited radiation sensitization properties in colon and pancreatic cancer cells. The radiosensitization ability of D-601 was blocked by pretreatment with α-napthoflavone (ANF), a specific inhibitor of cytochrome P450 1A2 (CYP1A2), suggesting that the metabolite of D-601 is essential for radiosensitization. The study demonstrated the ability of hydroxychalcones to radiosensitize cancer cells and provides new leads for developing novel radiation sensitizers.
AuthorsRory Pruitt, Nidhish Sasi, Michael L Freeman, Konjeti R Sekhar
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 20 Issue 20 Pg. 5997-6000 (Oct 15 2010) ISSN: 1464-3405 [Electronic] England
PMID20826087 (Publication Type: Journal Article, Research Support, N.I.H., Extramural)
CopyrightCopyright © 2010 Elsevier Ltd. All rights reserved.
Chemical References
  • 2',5'-dihydroxychalcone
  • 2,2'-dihydroxychalcone
  • Chalcones
  • Radiation-Sensitizing Agents
  • Adenocarcinoma (radiotherapy)
  • Cell Line, Tumor
  • Chalcones (pharmacology)
  • Colonic Neoplasms (radiotherapy)
  • Humans
  • Pancreatic Neoplasms (radiotherapy)
  • Radiation-Sensitizing Agents (pharmacology)

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