A novel bone resorption inhibitor, A-75943 isolated from Streptomyces sp. SANK 61296

J Antibiot (Tokyo). 1998 Jun;51(6):531-8. doi: 10.7164/antibiotics.51.531.

Abstract

A novel bone resorption inhibitor, A-75943, was isolated from Streptomyces sp. SANK 61296. Its structure was determined to be (1"S,2'R,3"S,4S',5"S)-2-[(3",5"- dimethyl-2"-oxocyclohexan-1"-yl)-6'-oxotetrahydropyran-4'-yl ]acetamide by spectral analyses and chemical conversion of cycloheximide. A-75943 inhibited bone resorption in vitro in a concentration-dependent manner with an IC50 of 0.35 microM, and also displayed an inhibitory effect on bone resorption in thyroid and parathyroid-extracted rats.

MeSH terms

  • Animals
  • Bone Density / drug effects*
  • Bone Resorption / drug therapy*
  • Fermentation
  • In Vitro Techniques
  • Male
  • Mass Spectrometry
  • Pyrans / chemical synthesis*
  • Pyrans / chemistry*
  • Pyrans / pharmacology*
  • Rats
  • Rats, Wistar
  • Spectrophotometry, Infrared
  • Streptomyces / classification
  • Streptomyces / metabolism*

Substances

  • Pyrans
  • A 75943