Production of 8-demethylgeldanamycin and 4,5-epoxy-8-demethylgeldanamycin from a recombinant strain of Streptomyces hygroscopicus

J Nat Prod. 2005 Apr;68(4):607-10. doi: 10.1021/np0496744.

Abstract

Two new geldanamycin derivatives produced by genetic engineering of Streptomyces hygroscopicus strain K309-27-1 were isolated and characterized. Removal of the 8-methyl group of geldanamycin was achieved by replacing the AT4 domain of the polyketide synthase with a malonyl AT domain. The resulting strain produced 8-demethyl geldanamycin (2) and 4,5-epoxy-8-demethylgeldanamycin (3). The structures of both molecules were elucidated through interpretation of 1D and 2D NMR data as well as comparison with authentic geldanamycin derivatives. Compounds 2 and 3 displayed moderate cytotoxicity against the human breast cancer cell line SK-BR-3.

Publication types

  • Comparative Study

MeSH terms

  • Antibiotics, Antineoplastic / chemistry
  • Antibiotics, Antineoplastic / isolation & purification*
  • Antibiotics, Antineoplastic / pharmacology
  • Benzoquinones
  • Cell Line, Tumor
  • Genetic Engineering*
  • Humans
  • Lactams, Macrocyclic
  • Molecular Structure
  • Quinones / chemical synthesis*
  • Quinones / chemistry
  • Quinones / isolation & purification*
  • Quinones / pharmacology
  • Streptomyces* / chemistry
  • Streptomyces* / genetics
  • Streptomyces* / metabolism
  • Structure-Activity Relationship

Substances

  • 4,5-epoxy-8-demethylgeldanamycin
  • 8-demethylgeldanamycin
  • Antibiotics, Antineoplastic
  • Benzoquinones
  • Lactams, Macrocyclic
  • Quinones
  • geldanamycin