Phenolic constituents with inhibitory activity against NFAT transcription from Desmos chinensis

Arch Pharm Res. 2005 Dec;28(12):1345-9. doi: 10.1007/BF02977900.

Abstract

Six phenolic constituents, 2-methoxybenzyl benzoate (1), negletein (2), 2',3'-dihydroxy-4',6'-dimethoxydihydrochalcone (3), 5,6-dihydroxy-7-methoxy-dihydroflavone (4), astilbin (5), and quercitrin (6) were isolated from the methanol extract of the dried leaves of Desmos chinensis. Their structures were elucidated from spectral and chemical data. Of these constituents, compounds 2 (IC50: 3.89 +/- 0.39 microM) and 3 (IC50: 9.77 +/- 0.26 microM) exhibited potent inhibitory activity against nuclear factor of activated T cells (NFAT) transcription factor, and compound 1 (IC50: 28.4 +/- 2.62 microM) exhibited moderate inhibitory activity.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Annonaceae*
  • Benzoates / chemistry
  • Benzoates / isolation & purification
  • Benzoates / pharmacology
  • Benzyl Compounds / chemistry
  • Benzyl Compounds / isolation & purification
  • Benzyl Compounds / pharmacology
  • Cell Survival / drug effects
  • Chalcones / chemistry
  • Chalcones / isolation & purification
  • Chalcones / pharmacology
  • Flavanones / chemistry
  • Flavanones / isolation & purification
  • Flavanones / pharmacology
  • Flavones / chemistry
  • Flavones / isolation & purification
  • Flavones / pharmacology
  • Flavonols / chemistry
  • Flavonols / isolation & purification
  • Flavonols / pharmacology
  • Humans
  • Inhibitory Concentration 50
  • Jurkat Cells
  • Methanol / chemistry
  • NFATC Transcription Factors / antagonists & inhibitors*
  • NFATC Transcription Factors / metabolism
  • Phenols / chemistry
  • Phenols / isolation & purification
  • Phenols / pharmacology*
  • Plant Extracts / chemistry
  • Plant Extracts / isolation & purification
  • Plant Extracts / pharmacology
  • Plant Leaves / chemistry
  • Plants, Medicinal / chemistry
  • Quercetin / analogs & derivatives
  • Quercetin / chemistry
  • Quercetin / isolation & purification
  • Quercetin / pharmacology

Substances

  • 2',3'-dihydroxy-4',6'-dimethoxydihydrochalcone
  • 2-methoxybenzyl benzoate
  • Benzoates
  • Benzyl Compounds
  • Chalcones
  • Flavanones
  • Flavones
  • Flavonols
  • NFATC Transcription Factors
  • Phenols
  • Plant Extracts
  • negletein
  • astilbin
  • quercitrin
  • Quercetin
  • flavanone
  • Methanol