Topical anti-inflammatory activity of Eupatilin, a lipophilic flavonoid from mountain wormwood ( Artemisia umbelliformis Lam.).
Eupatilin (5,7-dihydroxy-3',4',6-trimethoxyflavone) is the major lipophilic flavonoid from Artemisia umbelliformis Lam. and Artemisia genipi Weber, two mountain wormwoods used for the production of the celebrated alpine liqueur genepy. The topical anti-inflammatory activity of eupatilin was investigated using the inhibition of the Croton-oil-induced dermatitis in the mouse ear as the end point. The oedematous response and the leukocyte infiltration were evaluated up to 48 h after the induction of phlogosis, comparing eupatilin with hydrocortisone and indomethacin as representatives of steroid and non-steroid anti-inflammatory drugs, respectively. At maximum development, eupatilin significantly reduced edema in a dose-dependent manner (ID(50) = 0.28 micromol/cm(2)), showing an anti-inflammatory potency comparable to that of indomethacin (ID(50) = 0.26 micromol/cm(2)) and only 1 order of magnitude lower than that of hydrocortisone (ID(50) = 0.03 micromol/cm(2)). Within 48 h, eupatilin (0.30 micromol/cm(2)) caused a global inhibition of the oedematous response (42%) higher than that of an equimolar dose of indomethacin (18%) and fully comparable to that of 0.03 micromol/cm(2) of hydrocortisone (55%). Moreover, the effect of eupatilin on the granulocytes infiltrate (32% inhibition) was similar to that of indomethacin (35% inhibition) and comparable to that of hydrocortisone (42% reduction), as confirmed by histological analysis. When our results are taken together, they show that eupatilin is endowed with potent in vivo topical anti-inflammatory activity, qualitatively similar to that of hydrocortisone and intermediate in terms of potency between those of steroid and non-steroid drugs.
Giangaspero
Anna
A
Dipartimento dei Materiali e delle Risorse Naturali, Università di Trieste, 34127 Trieste, Italy.
Ponti
Cristina
C
Pollastro
Federica
F
Del Favero
Giorgia
G
Della Loggia
Roberto
R
Tubaro
Aurelia
A
Appendino
Giovanni
G
Sosa
Silvio
S
D000287:Administration, Topical; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage*; D019306:Artemisia / Q000737:chemistry*; D003436:Croton Oil; D003877:Dermatitis, Contact / Q000188:drug therapy / Q000473:pathology; D004423:Ear; D004487:Edema / Q000188:drug therapy; D005419:Flavonoids / Q000008:administration & dosage* / Q000302:isolation & purification; D006098:Granulocytes / Q000473:pathology; D008297:Male; D051379:Mice
D000893:Anti-Inflammatory Agents; D005419:Flavonoids; C045325:eupatilin; D003436:Croton Oil