Strong antihyperglycemic effects of water-soluble fraction of Brazilian propolis and its bioactive constituent, 3,4,5-tri-O-caffeoylquinic acid

Biol Pharm Bull. 2004 Nov;27(11):1797-803. doi: 10.1248/bpb.27.1797.


To clarify the suppression of postprandial blood glucose rise via alpha-glucosidase (AGH) inhibitory action by natural compounds, propolis was examined in this study. A single oral administration of propolis extract (50% methanol fraction on XAD-2 column chromatography) in Sprague-Dawley rats demonstrated a potent antihyperglycemic effect with the significant AUC(0-120 min) reduction of 38% at a dose of 20 mg/kg compared to that of controls. Among the active compounds isolated from the fraction, 3,4,5-tri-caffeoylquinic acid was found to be a prominent candidate that exerts the effect and shows a strong maltase-specific inhibition with an IC(50) value of 24 microM. In addition, the noncompetitive inhibition power apparently increased with the number of caffeoyl groups bound to quinic acid.

MeSH terms

  • Administration, Oral
  • Animals
  • Area Under Curve
  • Blood Glucose / drug effects
  • Brazil
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / pharmacology*
  • Male
  • Plant Extracts / chemistry
  • Plant Extracts / pharmacology
  • Plant Leaves / chemistry
  • Propolis* / chemistry
  • Quinic Acid / analogs & derivatives*
  • Quinic Acid / chemistry
  • Quinic Acid / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Solubility
  • Time Factors
  • Water


  • Blood Glucose
  • Hypoglycemic Agents
  • Plant Extracts
  • caffeoylquinic acid
  • Quinic Acid
  • Water
  • Propolis