FR901512, a novel HMG-CoA reductase inhibitor produced by an agonomycetous fungus No. 14919. II. Taxonomy of the producing organism, fermentation, isolation and physico-chemical properties

J Antibiot (Tokyo). 2004 Apr;57(4):264-70. doi: 10.7164/antibiotics.57.264.

Abstract

Novel compounds FR901512 and FR901516 were isolated from the fermentation broth of agonomycete strain No. 14919. FR901512 and FR901516 possess unique tetralin ring in their structure. These compounds were potent inhibitors of the cholesterol synthesis in human hepatoma cell line Hep G2. FR901512 shows strong 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitory activity with an IC50 value of 0.95 nM.

MeSH terms

  • Cell Line, Tumor
  • Cholesterol / metabolism
  • Esters / chemistry
  • Esters / isolation & purification
  • Esters / pharmacology
  • Fungi / chemistry
  • Fungi / classification
  • Fungi / metabolism*
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / chemistry
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / isolation & purification*
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / pharmacology
  • Inhibitory Concentration 50
  • Molecular Structure
  • Tetrahydronaphthalenes / chemistry
  • Tetrahydronaphthalenes / isolation & purification*
  • Tetrahydronaphthalenes / pharmacology

Substances

  • Esters
  • FR901512
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors
  • Tetrahydronaphthalenes
  • Cholesterol