Inhibitory lignans against NFAT transcription factor from Acanthopanax koreanum

Arch Pharm Res. 2004 Jul;27(7):738-41. doi: 10.1007/BF02980142.

Abstract

Three lignans isolated from the roots of A. koreanum (Araliaceae), namely eleutheroside E (1), tortoside A (2), and hemiariensin (4), were evaluated for their ability to inhibit NFAT transcription factor. Of these compounds, compound 4, possessing a diarylbutane skeleton, exhibited potent inhibitory activity against NFAT transcription factor (IC50: 36.3 +/- 2.5 microM). However, the activities of 1 (IC50: > 500 microM) and 2 (IC50: 136.1 +/- 9.4 microM), which possess bisaryldioxabicyclooctane skeletons, were lower. As the lignan derivatives of the same skeletons, hinokinin (5) and (-)-yatein (6) with diarylbutane skeletons and (+)-syringaresinol (3) with a bisaryldioxabicyclooctane skeleton were also studied for their inhibitory effects on NFAT transcription factor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Buffers
  • Chromatography, High Pressure Liquid
  • Chromatography, Thin Layer
  • DNA-Binding Proteins / genetics*
  • Eleutherococcus / chemistry*
  • Humans
  • Indicators and Reagents
  • Jurkat Cells
  • Lignans
  • Magnetic Resonance Spectroscopy
  • NFATC Transcription Factors
  • Nuclear Proteins / genetics*
  • Spectrophotometry, Ultraviolet
  • Transcription Factors / genetics*
  • Transcription, Genetic / drug effects

Substances

  • Buffers
  • DNA-Binding Proteins
  • Indicators and Reagents
  • Lignans
  • NFATC Transcription Factors
  • Nuclear Proteins
  • Transcription Factors