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2,2'-Dihydroxychalcone, a glutathione transferase inhibitor, sensitises human colon adenocarcinoma cells to chlorambucil and melphalan, but not to actinomycin D

  • Authors:
    • Kenneth Goh
    • Yufan Chen
    • Lin Zheng
    • Laichun Ong
    • Yi Jin
    • Pierce Chow
    • Kai Zhang

  • View Affiliations

  • Published online on: July 1, 2008     https://doi.org/10.3892/mmr.1.4.575
  • Pages: 575-579
Metrics: Total Views: 0 (Spandidos Publications: | PMC Statistics: )
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Abstract

2,2'-Dihydroxychalcone (2,2'DHC) is a potent inhibitor of glutathione S-transferases (GSTs). Pre-treatment of human colon cancer cells by a non-toxic concentration of this GST inhibitor significantly sensitised cancer cells to chlorambucil and melphalan, which are substrates of glutathione (GSH) conjugation. However, sensitisation to actinomycin D, which has not been shown to be detoxified by GSH-related mechanisms, was not observed. These results further confirm the contribution of GSH-related mechanisms to drug resistance by increased detoxification of drugs. 2,2'DHC inhibited GST activity and the transport of GSH conjugates by cancer cells. Its combined effects on GST and glutathione conjugate export (GS-X) pump may provide more potent sensitisation of cancer cells to chemotherapeutic drugs.

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July-August 2008
Volume 1 Issue 4

Print ISSN: 1791-2997
Online ISSN:1791-3004

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  • Journal Metrics
  • Impact Factor: 3.4
  • Ranked Medicine Research and Experimental
    (total number of cites)
  • CiteScore: 7.6
  • CiteScore Rank: Q1: #82/347 Biochemistry, Genetics and Molecular Biology
  • Source Normalized Impact per Paper (SNIP): 0.647
  • SCImago Journal Rank (SJR): 0.781
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Spandidos Publications style
Goh K, Chen Y, Zheng L, Ong L, Jin Y, Chow P and Zhang K: 2,2'-Dihydroxychalcone, a glutathione transferase inhibitor, sensitises human colon adenocarcinoma cells to chlorambucil and melphalan, but not to actinomycin D. Mol Med Rep 1: 575-579, 2008.
APA
Goh, K., Chen, Y., Zheng, L., Ong, L., Jin, Y., Chow, P., & Zhang, K. (2008). 2,2'-Dihydroxychalcone, a glutathione transferase inhibitor, sensitises human colon adenocarcinoma cells to chlorambucil and melphalan, but not to actinomycin D. Molecular Medicine Reports, 1, 575-579. https://doi.org/10.3892/mmr.1.4.575
MLA
Goh, K., Chen, Y., Zheng, L., Ong, L., Jin, Y., Chow, P., Zhang, K."2,2'-Dihydroxychalcone, a glutathione transferase inhibitor, sensitises human colon adenocarcinoma cells to chlorambucil and melphalan, but not to actinomycin D". Molecular Medicine Reports 1.4 (2008): 575-579.
Chicago
Goh, K., Chen, Y., Zheng, L., Ong, L., Jin, Y., Chow, P., Zhang, K."2,2'-Dihydroxychalcone, a glutathione transferase inhibitor, sensitises human colon adenocarcinoma cells to chlorambucil and melphalan, but not to actinomycin D". Molecular Medicine Reports 1, no. 4 (2008): 575-579. https://doi.org/10.3892/mmr.1.4.575