Enzyme Inhibitory Radicinol Derivative from Endophytic fungus Bipolaris sorokiniana LK12, Associated with Rhazya stricta

Molecules. 2015 Jul 3;20(7):12198-208. doi: 10.3390/molecules200712198.

Abstract

Endophytes, living inside plant tissues, play an essential role in plant growth and development, whilst producing unique bioactive secondary metabolites. In the current study, the endophytic fungus Bipolaris sorokiniana LK12 was isolated from the leaves of ethno-medicinal and alkaloidal rich Rhazya stricta. The bulk amount of ethyl acetate extract of fungus was subjected to advance column chromatographic techniques, which resulted in the isolation of a new radicinol derivative, bipolarisenol (1). It was found to be a derivative of radicinol. The structure elucidation was carried out by the combined use of 1D and 2D nuclear magnetic resonance, infrared spectroscopy, mass, and UV spectrometric analyses. The bipolarisenol was assessed for its potential role in enzyme inhibition of urease and acetyl cholinesterase (AChE). Results showed that bipolarisenol significantly inhibited the AChE activity with low IC50 (67.23 ± 5.12 µg·mL-1). Bipolarisenol inhibited urease in a dose-dependent manner with high IC50 (81.62 ± 4.61 µg·mL-1). The new compound also showed a moderate anti-lipid peroxidation potential (IC50 = 168.91 ± 4.23 µg·mL-1). In conclusion, endophytes isolated from medicinal plants possess a unique potential to be considered for future drug discovery.

Keywords: Bipolaris sorokiniana LK12; Rhazya stricta; bipolarisenol; enzyme inhibition; lipid peroxidation; radicinol.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apocynaceae / microbiology*
  • Ascomycota / chemistry*
  • Enzyme Inhibitors / isolation & purification*
  • Enzyme Inhibitors / pharmacology
  • Lipid Peroxidation / drug effects
  • Pyrones / chemistry*

Substances

  • Enzyme Inhibitors
  • Pyrones
  • radicinol