Spoxazomicins A-C, novel antitrypanosomal alkaloids produced by an endophytic actinomycete, Streptosporangium oxazolinicum K07-0460(T)

J Antibiot (Tokyo). 2011 Apr;64(4):303-7. doi: 10.1038/ja.2011.16. Epub 2011 Mar 9.

Abstract

Three novel antitrypanosomal alkaloids, named spoxazomicins A-C, were isolated by silica gel column chromatography and HPLC from the culture broth of a new endophytic actinomycete species, Streptosporangium oxazolinicum K07-0460(T). The structures of the spoxazomicins were elucidated by NMR and X-ray crystal analyses and shown to be new types of pyochelin family antibiotic. Spoxazomicin A showed potent and selective antitrypanosomal activity with an IC₅₀ value of 0.11 μg ml⁻¹ in vitro without cytotoxicity against MRC-5 cells (IC₅₀=27.8 μg ml⁻¹).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Actinobacteria / metabolism*
  • Alkaloids / chemistry
  • Alkaloids / isolation & purification
  • Alkaloids / pharmacology*
  • Cell Line
  • Chromatography / methods
  • Chromatography, High Pressure Liquid / methods
  • Humans
  • Inhibitory Concentration 50
  • Oxazoles / chemistry
  • Oxazoles / isolation & purification
  • Oxazoles / pharmacology*
  • Phenols / chemistry
  • Phenols / isolation & purification
  • Phenols / pharmacology*
  • Silica Gel
  • Thiazoles / chemistry
  • Thiazoles / isolation & purification
  • Thiazoles / pharmacology*
  • Trypanocidal Agents / chemistry
  • Trypanocidal Agents / isolation & purification
  • Trypanocidal Agents / pharmacology*

Substances

  • Alkaloids
  • Oxazoles
  • Phenols
  • Thiazoles
  • Trypanocidal Agents
  • spoxazomicin A
  • spoxazomicin B
  • spoxazomicin C
  • Silica Gel
  • pyochelin