Phenolic compounds isolated from Psoralea corylifolia inhibit IL-6-induced STAT3 activation

Planta Med. 2012 Jun;78(9):903-6. doi: 10.1055/s-0031-1298482. Epub 2012 May 9.

Abstract

Inhibiting interleukin-6 (IL-6) has been postulated as an effective therapy in the pathogenesis of several inflammatory diseases. In this study, seven flavonoids were isolated from the methanol extracts of Psoralea corylifolia by bioactivity-guided fractionation. The structures of bakuchiol (1), bavachinin (2), neobavaisoflavone (3), corylifol A (4), corylin (5), isobavachalcon (6), and bavachin (7) were determined by spectroscopic analysis (1H-, 13C- NMR and MS). We demonstrated that compounds 1-7 showed an inhibitory effect on IL-6-induced STAT3 promoter activity in Hep3B cells with IC50 values of 4.57 ± 0.45, 3.02 ± 0.53, 2.77 ± 0.02, 0.81 ± 0.15, 1.37 ± 0.45, 2.45 ± 0.13, and 4.89 ± 0.05 µΜ, respectively. These compounds also inhibited STAT3 phosphorylation induced by IL-6 in Hep3B cells. Overall, several flavonoids from P. corylifolia might be useful remedies for treating inflammatory diseases by inhibiting IL-6-induced STAT3 activation and phosphorylation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology*
  • Cell Line
  • Drug Evaluation, Preclinical / methods
  • Flavones / chemistry
  • Flavones / isolation & purification
  • Flavones / pharmacology
  • Flavonoids / chemistry*
  • Flavonoids / isolation & purification
  • Flavonoids / pharmacology*
  • Humans
  • Inhibitory Concentration 50
  • Interleukin-6 / pharmacology*
  • Isoflavones / chemistry
  • Isoflavones / isolation & purification
  • Isoflavones / pharmacology
  • Molecular Structure
  • Phenols / chemistry
  • Phenols / isolation & purification
  • Phenols / pharmacology
  • Phosphorylation / drug effects
  • Plant Extracts / pharmacology
  • Plants, Medicinal / chemistry
  • Promoter Regions, Genetic
  • Psoralea / chemistry*
  • STAT3 Transcription Factor / genetics
  • STAT3 Transcription Factor / metabolism*
  • Structure-Activity Relationship
  • Tyrosine / metabolism

Substances

  • Anti-Inflammatory Agents
  • Flavones
  • Flavonoids
  • Interleukin-6
  • Isoflavones
  • Phenols
  • Plant Extracts
  • STAT3 Transcription Factor
  • STAT3 protein, human
  • bavachin
  • corylifol A
  • corylin
  • neobavaisoflavone
  • Tyrosine
  • bakuchiol
  • bavachinin