Origin and bioactivities of thiosulfinated FK228
| Autor: | Xiangyang Liu, Liang Xue, Grant C. Currens, Yi-Qiang Cheng |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
Pharmacology
Burkholderia thailandensis biology 010405 organic chemistry Silica gel Organic Chemistry Pharmaceutical Science biology.organism_classification 01 natural sciences Biochemistry 0104 chemical sciences Chemistry 010404 medicinal & biomolecular chemistry chemistry.chemical_compound chemistry Cell culture Class I Histone Deacetylases Drug Discovery Molecular Medicine Fermentation broth Human cancer |
| Zdroj: | MedChemComm. 10:538-542 |
| ISSN: | 2040-2511 2040-2503 |
| DOI: | 10.1039/c9md00060g |
| Popis: | During a large laboratory-scale purification of FK228 from the fermentation broth of Burkholderia thailandensis MSMB43, a small amount of thiosulfinated FK228 (TS-FK228) was unexpectedly purified only after the broth was mixed with silica gel. Evidence supports the postulations that TS-FK228 was derived from FK228 through spontaneous chemical reaction with silica gel, and TS-FK228 existed as two isomers 1 and 2. TS-FK228 demonstrated similar inhibitory activity and profile against human class I histone deacetylases but exhibited a much higher antiproliferative activity against representative human cancer cell lines when compared to FK228. |
| Databáze: | OpenAIRE |
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