Frenolicins C-G, pyranonaphthoquinones from Streptomyces sp. RM-4-15

J Nat Prod. 2013 Aug 23;76(8):1441-7. doi: 10.1021/np400231r. Epub 2013 Aug 14.

Abstract

Appalachian active coal fire sites were selected for the isolation of bacterial strains belonging to the class actinobacteria. A comparison of high-resolution electrospray ionization mass spectrometry (HRESIMS) and ultraviolet (UV) absorption profiles from isolate extracts to natural product databases suggested Streptomyces sp. RM-4-15 to produce unique metabolites. Four new pyranonaphthoquinones, frenolicins C-F (1-4), along with three known analogues, frenolicin (6), frenolicin B (7), and UCF76-A (8), were isolated from the fermentation of this strain. An additional new analogue, frenolicin G (5), along with two known compounds, deoxyfrenolicin (9) and UCF 13 (10), were isolated from the fermentation supplied with 18 mg/L of scandium chloride, the first example, to the best of our knowledge, wherein scandium chloride supplementation led to the confirmed production of new bacterial secondary metabolites. Structures 1-5 were elucidated on the basis of spectral analysis and chemical modification. While frenolicins are best known for their anticoccidial activity, the current study revealed compounds 6-9 to exhibit moderate cytotoxicity against the human lung carcinoma cell line (A549) and thereby extends the anticancer SAR for this privileged scaffold.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Actinobacteria / chemistry*
  • Appalachian Region
  • Drug Screening Assays, Antitumor
  • Humans
  • Molecular Structure
  • Naphthoquinones / chemistry
  • Naphthoquinones / isolation & purification*
  • Naphthoquinones / pharmacology
  • Pyrones / chemistry
  • Pyrones / isolation & purification*
  • Pyrones / pharmacology
  • Spectrometry, Mass, Electrospray Ionization
  • Streptomyces / chemistry
  • Structure-Activity Relationship

Substances

  • Naphthoquinones
  • Pyrones
  • UCF76-A
  • frenolicin C
  • frenolicin B
  • deoxyfrenolicin