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Histone deacetylase inhibitors from Burkholderia thailandensis.


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.

SUBMITTER: Klausmeyer P 

PROVIDER: S-EPMC3204006 | biostudies-literature | 2011 Oct

REPOSITORIES: biostudies-literature

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Histone deacetylase inhibitors from Burkholderia thailandensis.

Klausmeyer Paul P   Shipley Suzanne M SM   Zuck Karina M KM   McCloud Thomas G TG  

Journal of natural products 20111003 10


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  ...[more]

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