Bioactive polyketides isolated from agar-supported fermentation of Phomopsis sp. CMU-LMA, taking advantage of the scale-up device, Platotex

Phytochemistry. 2013 Sep:93:170-5. doi: 10.1016/j.phytochem.2013.02.012. Epub 2013 Apr 9.

Abstract

Phomopsis sp. CMU-LMA was cultivated on agar-supported fermentation (Ag-SF) using the scale-up prototype Platotex. In total nine compounds were isolated from the ethyl acetate extract of the culture. Among them, compounds LMA-P1, Sch-642305, DHTO and LMA-P2 had already been reported in our previous work on liquid state fermentation. The trihydroxybenzene lactone cytosporone D and dothiorelone A has been recently isolated from Phomopsis and Magnaporthe species. In addition, three compounds were isolated consisting in the reduced methoxy derivative of Sch-642305 (1), a hydroxylated derivative of LMA-P2 (2) and a linear ethyl ester polyketide (3) similar to the previously reported LMA-P3. Antimicrobial activity and inhibition of Escherichia coli DnaG primase were investigated. Cytosporone D inhibited the E. coli DnaG primase, a Gram-negative antimicrobial target, with an IC50 of 0.25 mM.

Keywords: Antimicrobial; DnaG primase; Fungal secondary metabolites; Phomopsis; Polyketide; Sch-642305.

MeSH terms

  • Agar / metabolism
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / isolation & purification
  • Anti-Bacterial Agents / pharmacology*
  • Ascomycota / chemistry*
  • Ascomycota / metabolism
  • Bioreactors
  • DNA Primase / antagonists & inhibitors*
  • DNA Primase / metabolism
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / isolation & purification
  • Enzyme Inhibitors / pharmacology*
  • Escherichia coli / drug effects*
  • Escherichia coli / enzymology
  • Escherichia coli / metabolism
  • Fermentation
  • Microbial Sensitivity Tests
  • Models, Molecular
  • Molecular Structure
  • Polyketides / chemistry
  • Polyketides / isolation & purification
  • Polyketides / pharmacology*
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Enzyme Inhibitors
  • Polyketides
  • Agar
  • DNA Primase