Spartinoxide, a new enantiomer of A82775C with inhibitory activity toward HLE from the marine-derived Fungus Phaeosphaeria spartinae

Nat Prod Commun. 2010 Jul;5(7):1071-6.

Abstract

The fungus Phaeosphaeria spartinae is an endophyte of the marine alga Ceramium sp. Investigation of this marine-derived fungus led to the isolation of spartinoxide (1), which is the enantiomer of the known compound A82775C (2). Additionally, the known metabolites 4-hydroxy-3-prenyl-benzoic acid (4) and anofinic acid (5) were obtained. The structures of all compounds were established from extensive spectroscopic investigations. Compounds 1, 4 and 5 were assayed against the enzymes human leukocyte elastase (HLE), trypsin, acetylcholinesterase and cholesterolesterase. Compounds 1 and 4 showed potent inhibition of HLE with IC50 values of 1.71 +/- 0.30 microg/mL (6.5 microM) and 1.67 +/- 0.32 microg/mL (8.1 microM), respectively.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Ascomycota / chemistry
  • Enzyme Activation / drug effects
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology*
  • Glycosides / chemistry*
  • Glycosides / pharmacology*
  • Humans
  • Leukocyte Elastase / antagonists & inhibitors*
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Stereoisomerism

Substances

  • Enzyme Inhibitors
  • Glycosides
  • Leukocyte Elastase