title: Direct inhibition of calcineurin by caffeoyl phenylethanoid glycosides from Teucrium chamaedrys and Nepeta cataria.
abstract: BACKGROUND
  Teucrium chamaedrys L. and Nepeta cataria L. (Lamiaceae) are species with traditional uses that relate to the treatment of inflammation. Extracts of both species were found to inhibit calcineurin; an important regulator of T-cell mediated inflammation that has received little attention in ethnopharmacological research.
  
  
  METHODS
  Extracts and isolated compounds were tested against calcineurin in its calmodulin-activated and basal un-activated state. Active compounds were isolated using Sephadex LH-20 gel filtration and HPLC then identified using NMR spectroscopy.
  
  
  CONCLUSIONS
  Activity-guided fractionation of Teucrium chamaedrys and Nepeta cataria led to the isolation of the caffeoyl phenylethanoid glycosides teucrioside, verbascoside and lamiuside A (teupolioside). The three compounds inhibited calcineurin both in the presence and absence of calmodulin, suggesting a direct interaction with calcineurin. Calcineurin inhibition should be considered as a potential mode of action when investigating the immunomodulatory activity of caffeoyl phenylethanoid glycoside containing plants.
authors.affiliation: Royal Botanic Gardens, Kew, Richmond, Surrey TW9 3AB, UK. T.Prescott@kew.org
authors.forename: Thomas A K
authors.initials: TA
authors.lastname: Prescott
authors.forename: Nigel C
authors.initials: NC
authors.lastname: Veitch
authors.forename: Monique S J
authors.initials: MS
authors.lastname: Simmonds
mesh_terms: D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D002109:Caffeic Acids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D019703:Calcineurin / Q000378:metabolism; D065095:Calcineurin Inhibitors; D002147:Calmodulin / Q000378:metabolism; D005591:Chemical Fractionation; D002850:Chromatography, Gel; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D005960:Glucosides / Q000494:pharmacology; D006027:Glycosides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D007700:Kinetics; D009682:Magnetic Resonance Spectroscopy; D027521:Nepeta / Q000737:chemistry; D010636:Phenols / Q000494:pharmacology; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D018515:Plant Leaves; D018547:Plant Stems; D010946:Plants, Medicinal; D031367:Teucrium / Q000737:chemistry; D059808:Polyphenols
chemical_list: D000893:Anti-Inflammatory Agents; D002109:Caffeic Acids; D019703:Calcineurin; D065095:Calcineurin Inhibitors; D002147:Calmodulin; D004791:Enzyme Inhibitors; D005960:Glucosides; D006027:Glycosides; D010636:Phenols; D010936:Plant Extracts; C040618:teucrium extract; C058956:acteoside; D059808:Polyphenols