Relaxant effects of quercetin methyl ether derivatives in isolated guinea pig trachea and their structure-activity relationships

Wun-Chang Ko, Shih W. Kuo, Joen Rong Sheu, Chien Huang Lin, Shu-Huey Tzeng, Chi Ming Chen

Research output: Contribution to journalArticle

15 Citations (Scopus)

Abstract

In the present study, we attempted to compare quercetin methyl ethers and to look for the structure-activity relationships, which may be helpful for synthesizing more active compounds for the treatment of asthma. Four present and two previously studied quercetin methyl ethers concentration- dependently relaxed histamine (30 μM), carbachol (0.2 μM) and KCl (30 mM) induced precontraction. According to their IC25 values to histamine- induced precontraction, the potency order was quercetin 3,3',4',5,7- pentamethyl ether (QPME), quercetin 3-methyl ether > quercetin, quercetin 3,4',7-trimethyl ether (ayanin) > quercetin 4'-methyl ether (tamarixetin), quercetin 3,3',4',7-tetramethyl ether (QTME). Therefore, the methylation at 3, at 5, and at both 3 and 7 positions of the A or/and C ring of quercetin nucleus may increase their tracheal relaxant activity. However, the methylation at the 3' and at the 4' position of the B ring of quercetin nucleus may decrease their tracheal relaxant activity.

Original languageEnglish
Pages (from-to)273-275
Number of pages3
JournalPlanta Medica
Volume65
Issue number3
Publication statusPublished - 1999

ASJC Scopus subject areas

  • Plant Science
  • Organic Chemistry
  • Drug Discovery
  • Pharmacology

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