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Histone Deacetylase Inhibitors from Burkholderia thailandensis

  1. Author:
    Klausmeyer, P.
    Shipley, S. M.
    Zuck, K. M.
    McCloud, T. G.
  2. Author Address

    [Klausmeyer, P; Shipley, SM; Zuck, KM; McCloud, TG] NCI Frederick, Nat Prod Support Grp, SAIC Frederick Inc, Frederick, MD 21702 USA.;Klausmeyer, P (reprint author), NCI Frederick, Nat Prod Support Grp, SAIC Frederick Inc, Frederick, MD 21702 USA;klausmeyerp@mail.nih.gov
    1. Year: 2011
    2. Date: Oct
  1. Journal: Journal of Natural Products
    1. 74
    2. 10
    3. Pages: 2039-2044
  2. Type of Article: Article
  3. ISSN: 0163-3864
  1. Abstract:

    Bioactivity-guided fractionation of an extract of Burkholderia thailandensis led to the isolation and identification of a new cytotoxic depsipeptide and its dimer. Both compounds potently inhibited the function of histone deacetylases 1 and 4. The monomer, spiruchostatin C (2), was tested side by side with the clinical depsipeptide FK228 (1, Istodax, romidepsin) in a murine hollow fiber assay consisting of 12 implanted tumor cell lines. Spiruchostatin C (2) showed good activity toward LOX IMVI melanoma cells and NCI-H522 non small cell lung cancer cells. Overall, however, FK228 (1) showed a superior in vivo antitumor profile in comparison to the new compound.

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External Sources

  1. DOI: 10.1021/np200532d
  2. WOS: 000296206500002

Library Notes

  1. Fiscal Year: FY2011-2012
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