Isolation and characterization of antibiotic NC0604, a new analogue of bleomycin

J Antibiot (Tokyo). 2008 Dec;61(12):747-51. doi: 10.1038/ja.2008.88.

Abstract

NC0604, a new analogue of bleomycin, was isolated from fermentation broth of Streptomyces verticillus var. pingyangensis n.var. The structure of NC0604 was elucidated by spectroscopic analyses. NC0604 had the same kernel structure as bleomycin, but a different terminal amine moiety determined as amidepropyl spermidine. NC0604 exhibited antibacterial activity against a wide range of bacterial species and showed cytotoxicity in vitro against human HepG(2), KB, MCF-7, HCT116, BGC-823 and MCF-7/DOX cells with IC(50) values of 1.18, 1.21, 1.41, 1.83, 2.02, 1.45 muM, respectively. The antitumor activity of NC0604 against these cells was 3~9 times higher than that of bleomycin; and the pulmonary toxicity of NC0604 was much lower than that of bleomycin.

MeSH terms

  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / isolation & purification
  • Anti-Bacterial Agents / pharmacology*
  • Anti-Bacterial Agents / toxicity
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / isolation & purification
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / toxicity
  • Bleomycin / analogs & derivatives*
  • Bleomycin / isolation & purification
  • Bleomycin / pharmacology
  • Bleomycin / toxicity
  • Cell Line, Tumor
  • Culture Media / chemistry*
  • Gram-Negative Bacteria / drug effects
  • Gram-Positive Bacteria / drug effects
  • Humans
  • Inhibitory Concentration 50
  • Microbial Sensitivity Tests
  • Spectrum Analysis
  • Streptomyces / metabolism*

Substances

  • Anti-Bacterial Agents
  • Antineoplastic Agents
  • Culture Media
  • Bleomycin