title: In vivo anti-inflammatory activity of caffeoylquinic acid derivatives from Solidago virgaurea in rats.
abstract: BACKGROUND
  Solidago virgaurea L. (Asteraceae) is traditionally used as an anti-inflammatory for the treatment of various symptoms including cystitis. However, little is known concerning the constituents responsible for this activity and the mechanism of their action.
  
  
  OBJECTIVE
  To assess the anti-inflammatory activity of the phenolic-rich fraction of S. virgaurea aerial parts in rats, isolate and assess the activity of the major compounds present.
  
  
  METHODS
  An HPLC method was developed for the analysis of the phenolic-rich fraction (EtFr). The in vivo anti-inflammatory activity of the EtFr and four isolated compounds (at 25 and 50 mg/kg) were assessed in adult male rats using the carrageenan-induced rat paw oedema model. The levels of the pro-inflammatory cytokines (TNF-α and IL-1β) were measured using ELISA.
  
  
  RESULTS
  3,5-O-Dicaffeoylquinic acid (1), 3,4-O-dicaffeoylquinic acid (2), 3,4,5-O-tricaffeoylquinic acid (3) and 4,5-O-dicaffeoylquinic acid (4) were isolated from EtFr. Compound 3 (50 mg/kg) showed a highly significant activity in inhibiting the oedema volume after 3 h (88% of the activity of indomethacin at 10 mg/kg). The EtFr and the isolated compounds largely inhibited the excessive production of the inflammatory mediators TNF-α and IL-1β.
  
  
  CONCLUSIONS
  This is the first report of 3,4,5-tri-O-caffeoylquinic acid (3) in Solidago species. The tricaffeoylquinic acid (3) showed a significantly higher activity than the other three dicaffeoylquinic acids (1, 2, 4) and indomethacin in reduction of TNF-α and IL-1β concentrations (8.44 ± 0.62 and 5.83 ± 0.57 pg/mL compared to 12.60 ± 1.30 and 52.91 ± 5.20 pg/mL induced by indomethacin, respectively).
authors.affiliation: a Department of Pharmacognosy, Faculty of Pharmacy , Cairo University , Cairo , Egypt.|b Pharmaceutical Biology Department, Faculty of Pharmacy and Biotechnology , GUC , Cairo , Egypt.
authors.forename: Amira
authors.initials: A
authors.lastname: Abdel Motaal
authors.affiliation: a Department of Pharmacognosy, Faculty of Pharmacy , Cairo University , Cairo , Egypt.
authors.forename: Shahira M
authors.initials: SM
authors.lastname: Ezzat
authors.affiliation: c Department of Pharmacology, Faculty of Pharmacy , Ein Shams University , Cairo , Egypt.
authors.forename: Mariane G
authors.initials: MG
authors.lastname: Tadros
authors.affiliation: a Department of Pharmacognosy, Faculty of Pharmacy , Cairo University , Cairo , Egypt.
authors.forename: Hesham I
authors.initials: HI
authors.lastname: El-Askary
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000302:isolation & purification; D004305:Dose-Response Relationship, Drug; D004487:Edema / Q000188:drug therapy / Q000378:metabolism; D018836:Inflammation Mediators / Q000037:antagonists & inhibitors* / Q000378:metabolism; D008297:Male; D010936:Plant Extracts / Q000008:administration & dosage* / Q000737:chemistry / Q000302:isolation & purification; D011801:Quinic Acid / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D011897:Random Allocation; D051381:Rats; D017207:Rats, Sprague-Dawley; D036624:Solidago
chemical_list: D000893:Anti-Inflammatory Agents; D018836:Inflammation Mediators; D010936:Plant Extracts; C472707:caffeoylquinic acid; D011801:Quinic Acid
keywords: Asteraceae; IL-1β; TNF-α; goldenrod; tricaffeoylquinic acid