Isolation and biological activity of thielocins: novel phospholipase A2 inhibitors produced by Thielavia terricola RF-143

J Antibiot (Tokyo). 1995 Feb;48(2):106-12. doi: 10.7164/antibiotics.48.106.

Abstract

Thielocins A2 alpha, A2 beta, A3, B1, B2 and B3 were isolated as a novel family of phospholipase A2 inhibitors from the fermentation broth of Thielavia terricola RF-143 together with thielavins and thielocins A1 alpha and A1 beta. The most potent inhibitory activity (IC50 = 0.0033 microM) against rat group II phospholipase A2 was shown by thielocin A1 beta. Against human group II phospholipase A2, thielocin B3 (IC50 = 0.076 microM) was the most potent.

MeSH terms

  • Animals
  • Ascomycota / metabolism*
  • Chromatography, High Pressure Liquid
  • Chromatography, Ion Exchange
  • Fermentation
  • Humans
  • Magnetic Resonance Spectroscopy
  • Phospholipases A / antagonists & inhibitors*
  • Phospholipases A2
  • Rats
  • Xanthenes / isolation & purification*
  • Xanthenes / pharmacology

Substances

  • Xanthenes
  • Phospholipases A
  • Phospholipases A2