title: Actions of Artemisia vulgaris extracts and isolated sesquiterpene lactones against receptors mediating contraction of guinea pig ileum and trachea.
abstract: OBJECTIVE
  The present study evaluates the Philippine medicinal plant Artemisia vulgaris for antagonistic activity at selected biogenic amine receptors on smooth muscle of the airways and gastrointestinal tract in order to explain its traditional use in asthma and hyperactive gut.
  
  
  METHODS
  The antagonistic activity of chloroform crude extract (AV-CHCl(3)) and methanol crude extract (AV-MeOH) of Artemisia vulgaris was studied against concentration-response curves for contractions of the guinea pig ileum and trachea to 5-hydroxytrptamine (5-HT(2) receptors), methacholine (M(3) muscarinic receptors), histamine (H(1) receptors) and β-phenylethylamine (trace amine-associated receptors, TAAR1).
  
  
  CONCLUSIONS
  The Artemisia vulgaris chloroform (AV-CHCl(3)) and methanol (AV-MeOH) extract showed histamine H1 antagonism in the ileum and trachea. Further analysis of AV-CHCl(3) isolated two major components, yomogin and 1,2,3,4-diepoxy-11(13)-eudesmen-12,8-olide. Yomogin, a sesquiterpene lactone, exhibited a novel histamine H1 receptor antagonism in the ileum.
  
  
  CONCLUSIONS
  The presence of a specific, competitive histamine receptor antagonist and smooth muscle relaxant activity in Artemisia vulgaris extracts on the smooth muscle in ileum and trachea explains its traditional use in the treatment of asthma and hyperactive gut.
authors.affiliation: Welsh School of Pharmacy, Cardiff University, King Edward VII Avenue, Cardiff CF10 3NB, UK.
authors.forename: Gaudencio M
authors.initials: GM
authors.lastname: Natividad
authors.forename: Kenneth J
authors.initials: KJ
authors.lastname: Broadley
authors.forename: Benson
authors.initials: B
authors.lastname: Kariuki
authors.forename: Emma J
authors.initials: EJ
authors.lastname: Kidd
authors.forename: William R
authors.initials: WR
authors.lastname: Ford
authors.forename: Claire
authors.initials: C
authors.lastname: Simons
mesh_terms: D000818:Animals; D019306:Artemisia / Q000737:chemistry; D002725:Chloroform / Q000737:chemistry; D004305:Dose-Response Relationship, Drug; D006168:Guinea Pigs; D006634:Histamine H1 Antagonists / Q000494:pharmacology; D007082:Ileum / Q000187:drug effects* / Q000378:metabolism; D066298:In Vitro Techniques; D007783:Lactones / Q000494:pharmacology; D008297:Male; D000432:Methanol / Q000737:chemistry; D009119:Muscle Contraction / Q000187:drug effects*; D009126:Muscle Relaxation / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects* / Q000378:metabolism; D018377:Neurotransmitter Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D010946:Plants, Medicinal; D043587:Receptor, Muscarinic M3 / Q000187:drug effects / Q000378:metabolism; D043562:Receptors, G-Protein-Coupled / Q000187:drug effects / Q000378:metabolism; D011969:Receptors, Histamine H1 / Q000187:drug effects / Q000378:metabolism; D044348:Receptors, Serotonin, 5-HT2 / Q000187:drug effects / Q000378:metabolism; D045787:Sesquiterpenes, Eudesmane / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D012997:Solvents / Q000737:chemistry; D014132:Trachea / Q000187:drug effects* / Q000378:metabolism; D000095383:Trace Amine-Associated Receptors
chemical_list: D002725:Chloroform; D006634:Histamine H1 Antagonists; D007783:Lactones; D000432:Methanol; D018377:Neurotransmitter Agents; D010936:Plant Extracts; D043587:Receptor, Muscarinic M3; D043562:Receptors, G-Protein-Coupled; D011969:Receptors, Histamine H1; D044348:Receptors, Serotonin, 5-HT2; D045787:Sesquiterpenes, Eudesmane; D012997:Solvents; D000095383:Trace Amine-Associated Receptors; C434252:1,2,3,4-diepoxy-11(13)-eudesmen-12,8-olide; C117320:yomogin