Identification of trichostatin derivatives from Streptomyces sp. CPCC 203909

Bioorg Med Chem Lett. 2015 Feb 1;25(3):562-5. doi: 10.1016/j.bmcl.2014.12.030. Epub 2014 Dec 19.

Abstract

Four new trichostatin analogues (1-4) and six known analogues have been isolated from the rice fermentation of the Streptomyces sp. CPCC 203909. The structures and absolute configurations of these compounds were determined by extensive spectroscopic analysis including 2D NMR and electronic circular dichroism (ECD) calculations based on the quantum-mechanical time-dependent density functional theory (TDDFT). Compounds 2, 5-7, 9, and 10 up-regulated the transcriptional activity of human high density lipoprotein receptor (CLA-1) with EC50 values of 0.38-78.83μM.

Keywords: Atherosclerosis; Human high density lipoprotein receptor; Streptomyces sp.; Trichostatin analogues.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line
  • Cell Survival / drug effects
  • Circular Dichroism
  • HEK293 Cells
  • HeLa Cells
  • Hep G2 Cells
  • Humans
  • Hydroxamic Acids / chemistry*
  • Hydroxamic Acids / isolation & purification
  • Hydroxamic Acids / pharmacology
  • Magnetic Resonance Spectroscopy
  • Molecular Conformation
  • Quantum Theory
  • Receptors, Lipoprotein / genetics
  • Receptors, Lipoprotein / metabolism
  • Streptomyces / chemistry*
  • Streptomyces / metabolism
  • Transcription, Genetic / drug effects

Substances

  • Hydroxamic Acids
  • Receptors, Lipoprotein