Ferroverdins, inhibitors of cholesteryl ester transfer protein produced by Streptomyces sp. WK-5344. I. Production, isolation and biological properties

J Antibiot (Tokyo). 1999 Dec;52(12):1101-7. doi: 10.7164/antibiotics.52.1101.

Abstract

Streptomyces sp. WK-5344, a soil isolate, was found to produce structurally related inhibitors of cholesteryl ester transfer protein (CETP). New active compounds, designated ferroverdins B and C, were isolated along with known ferroverdin A from the fermentation broth by solvent extraction, ODS column chromatography and silica gel column chromatography. All ferroverdins showed a dose-dependent inhibitory activity against human CETP. The IC50 values were 21, 0.62 and 2.2 microM for ferroverdins A, B and C, respectively, indicating that ferroverdin B is one of the most potent CETP inhibitors of microbial origin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Bacteria / drug effects
  • Carrier Proteins / antagonists & inhibitors*
  • Cholesterol Ester Transfer Proteins
  • Dose-Response Relationship, Drug
  • Fermentation
  • Ferrous Compounds / isolation & purification*
  • Ferrous Compounds / pharmacology
  • Glycoproteins*
  • Humans
  • Nitroso Compounds / isolation & purification*
  • Nitroso Compounds / pharmacology
  • Streptomyces / classification
  • Streptomyces / metabolism*

Substances

  • CETP protein, human
  • Carrier Proteins
  • Cholesterol Ester Transfer Proteins
  • Ferrous Compounds
  • Glycoproteins
  • Nitroso Compounds
  • ferroverdin B
  • ferroverdin C
  • ferroverdin