Relaxant effects of petasins in isolated guinea pig trachea and their structure-activity relationships

W. C. Ko, C. B. Lei, Y. L. Lin, C. F. Chen

Research output: Contribution to journalArticle

18 Citations (Scopus)

Abstract

In the present study, we attempted to compare four petasins, isolated from Petasites formosanus Kitamura, and to look for structure-activity relationships, which may be helpful for synthesizing more active compounds for the treatment of asthma. Four petasins, including petasin, isopetasin, S-petasin and S-isopetasin, concentration-dependently relaxed histamine (10 μM)-, carbachol (0.2 μM)-, KCl (30 mM)-, and leukotriene D4 (10 nM)-induced precontractions of isolated guinea pig trachealis. The IC50 values strongly showed that the relaxant effects of the sulfur-containing petasins, S-petasin and S-isopetasin, were more potent than those of non-sulfur-containing petasins, petasin and isopetasin. S-Isopetasin, with IC50 values around 10 μM, selectively relaxed carbachol- and KCl-induced precontractions, and had almost no effects (IC50s > 300 μM) on histamine- and leukotriene D4-induced precontractions. However, S-petasin, with IC50 values about 6-9 μM, non-selectively relaxed the precontractions induced by all these contractile agents. The influence of isomerization of either petasin to isopetasin or S-petasin to S-isopetasin on the relaxant effects is not clear.

Original languageEnglish
Pages (from-to)650-652
Number of pages3
JournalPlanta Medica
Volume66
Issue number7
DOIs
Publication statusPublished - 2000

Fingerprint

trachea (vertebrates)
structure-activity relationships
Structure-Activity Relationship
Trachea
guinea pigs
inhibitory concentration 50
carbachol
leukotrienes
Guinea Pigs
histamine
Petasites
isomerization
asthma
sulfur
Leukotriene D4
Inhibitory Concentration 50
Carbachol
Histamine
petasin
Isomerization

ASJC Scopus subject areas

  • Plant Science
  • Drug Discovery
  • Organic Chemistry
  • Pharmacology

Cite this

Relaxant effects of petasins in isolated guinea pig trachea and their structure-activity relationships. / Ko, W. C.; Lei, C. B.; Lin, Y. L.; Chen, C. F.

In: Planta Medica, Vol. 66, No. 7, 2000, p. 650-652.

Research output: Contribution to journalArticle

Ko, W. C. ; Lei, C. B. ; Lin, Y. L. ; Chen, C. F. / Relaxant effects of petasins in isolated guinea pig trachea and their structure-activity relationships. In: Planta Medica. 2000 ; Vol. 66, No. 7. pp. 650-652.
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