Radiosensitization of cancer cells by hydroxychalcones.

Pruitt R, Sasi N, Freeman ML, Sekhar KR
Bioorg Med Chem Lett. 2010 20 (20): 5997-6000

PMID: 20826087 · PMCID: PMC2946792 · DOI:10.1016/j.bmcl.2010.08.081

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.

Copyright © 2010 Elsevier Ltd. All rights reserved.

MeSH Terms (7)

Adenocarcinoma Cell Line, Tumor Chalcones Colonic Neoplasms Humans Pancreatic Neoplasms Radiation-Sensitizing Agents

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