Journal of natural products (Washington, D.C.), 2011-10, Vol.74 (10), p.2039-2044
2011
Details
- Autor(en) / Beteiligte
- Titel
- Histone Deacetylase Inhibitors from Burkholderia thailandensis
- Ist Teil von
- Journal of natural products (Washington, D.C.), 2011-10, Vol.74 (10), p.2039-2044
- Ort / Verlag
- Northbrook, IL: American Chemical Society and American Society of Pharmacognosy
- Erscheinungsjahr
- 2011
- Link zum Volltext
- Quelle
- Alma/SFX Local Collection
- Beschreibungen/Notizen
- 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.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0163-3864eISSN: 1520-6025DOI: 10.1021/np200532dTitel-ID: cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_3204006
- Format
- –
- Schlagworte
- Animals, Antibiotics, microbial producers, chemotherapic agents, antiseptics, disinfecting agents, Antineoplastic Agents - chemistry, Antineoplastic Agents - isolation & purification, Antineoplastic Agents - pharmacology, Applied microbiology, Biological and medical sciences, Burkholderia - chemistry, Burkholderia thailandensis, Chemotherapic agents, Depsipeptides - chemistry, Depsipeptides - isolation & purification, Depsipeptides - pharmacology, Drug Screening Assays, Antitumor, Fundamental and applied biological sciences. Psychology, Histone Deacetylase Inhibitors - chemistry, Histone Deacetylase Inhibitors - isolation & purification, Histone Deacetylase Inhibitors - pharmacology, Humans, Mice, Microbiology, Molecular Structure, National Cancer Institute (U.S.), United States