Suppressive effects of 3-O-methylquercetin on ovalbumin-induced airway hyperresponsiveness

Wun-Chang Ko, Chwen Ming Shih, Mei Chun Chen, Ya Hsin Lai, Jun Hao Chen, Chien Ming Chen, Chun Nan Lin

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27 Citations (Scopus)


Rhamnus nakaharai Hayata (Rhamnaceae) has been used as a folk medicine in Taiwan for treating constipation, inflammation, tumors, and asthma. 3-O-Methylquercetin (3-MQ), a main constituent of the plant, has been reported to inhibit total cAMP-and cGMP-phosphodiesterase (PDE) of guinea pig trachealis at low concentrations. 3-MQ has been also reported to more selectively inhibit PDE3 than PDE4 with a low Km value. Therefore we were interested in investigating its suppressive effects on ovalbumin (OVA)-induced airway hyperresponsiveness in vivo and in vitro. 3-MQ (3-30 μmol/kg, i.p.) significantly suppressed the enhanced pause (Penh) value induced by aerosolized methacholine (50 mg/mL) in sensitized mice after secondary allergen challenge. 3-MQ (3-30 μmol/kg, i.p.) also significantly suppressed total inflammatory cells, macrophages, neutrophils, and eosinophils, but not lymphocytes. In addition, 3-MQ (3 μmol/kg, i.p.) significantly decreased the secretion of TNF-α, and at the highest dose (30 μmol/kg, i.p.) even decreased the secretions of IL-4, IL-5, and TNF-α. 3-MQ (1-10 μM) as well as Ro 20-1724 (3-30 μM), a selective PDE4 inhibitor, significantly attenuated OVA (100 μg/ mL)-induced contractions. 3-MQ (30 μM) as well as milrinone (1 -10 μM), a selective PDE3 inhibitor, significantly enhanced baseline contractions in isolated guinea pig left and right atria. However, neither 3-MQ nor milrinone significantly affected baseline beating rate in the right atria. 3-MQ (3-30 μmol/kg, i.p.) did not significantly affect systolic pressure in conscious mice. In conclusion, 3-MQ has both anti-inflammatory and bronchodilating effects, and has the potential for use in the treatment of asthma at a dose without affecting blood pressure.

Original languageEnglish
Pages (from-to)1123-1127
Number of pages5
JournalPlanta Medica
Issue number12
Publication statusPublished - Dec 2004


  • 3-O-Methylquercetin
  • Asthma
  • Cytokines
  • Inflammatory cells
  • Ovalbumin-sensitized mice
  • Rhamnaceae
  • Rhamnus nakaharai

ASJC Scopus subject areas

  • Drug Discovery
  • Analytical Chemistry
  • Molecular Medicine
  • Complementary and alternative medicine
  • Pharmacology
  • Pharmaceutical Science
  • Organic Chemistry


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