2. Academic Validation
  3. Origin and bioactivities of thiosulfinated FK228

Origin and bioactivities of thiosulfinated FK228

  • Medchemcomm. 2019 Mar 25;10(4):538-542. doi: 10.1039/c9md00060g.
Xiangyang Liu 1,  Grant C Currens 1,  Liang Xue 2,  Yi-Qiang Cheng 1
Affiliations

Affiliations

  • 1 UNT System College of Pharmacy , University of North Texas Health Science Center , 3500 Camp Bowie Blvd , Fort Worth , TX 76107 , USA . Email: [email protected] ; ; Tel: +817 735 0165.
  • 2 Alcon NMR laboratory at Novartis , 6201 South Fwy , Fort Worth , TX 76134 , USA.
PMID: 31057733 DOI: 10.1039/c9md00060g
Abstract

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.

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