title: Pharmacological reports about gastroprotective effects of methanolic extract from leaves of Solidago chilensis (Brazilian arnica) and its components quercitrin and afzelin in rodents.
abstract: Solidago chilensis Meyenmost (Asteraceae), popularly known as "Brazilian arnica" or "arnica-do-campo," is widely used in the folk medicine to treat gastric disorders. Based on this, the gastroprotective activity of S. chilensis methanolic extract was investigated. Besides, a phytochemical study allowed isolation of two flavonoids (quercitrin and afzelin). The gastroprotective effects were investigated in acute gastric ulcer models, and the antisecretory activity was assessed in vivo and in vitro. The adhered mucus levels, reduced glutathione (GSH) content and myeloperoxidase (MPO) activity were quantified in ulcerated tissues. The contribution of isolated compounds in extract effects was evaluated, and its doses were calculated according to its yield. To evaluate the in vivo healing properties of S. chilensis methanolic extract, a chronic gastric ulcer was induced in mice by 10 % acetic acid. Evaluation of tumor necrosis factor (TNF) levels was also performed at the site of the acetic acid-induced gastric ulcer. In parallel, effects on cell viability and cell proliferation of fibroblasts (L929 cells) were determined by in vitro trials. Firstly, the S. chilensis methanolic extract (100 or 300 mg/kg) reduced the ulcer area induced by ethanol/HCl in mice when compared to the vehicle group. Moreover, the S. chilensis extract (300 mg/kg) prevented the mucus depletion, the increase in MPO activity and the decrease in the GSH levels in the ulcerated gastric tissue. The S. chilensis extract also was able to decrease the indomethacin-induced gastric ulcer in rats at a dose of 100 mg/kg. The antisecretory effect of the extract (100 mg/kg, intraduodenal (i.d.)) was confirmed by the reduction in the volume and acidity in parallel to an increase in the pH of gastric content. In addition, quercitrin (1.38 mg/kg, but not 0.46 mg/kg) and afzelin (0.026 and 0.078 mg/kg) decreased the ethanol/HCl-induced gastric ulcer. In this model, quercitrin (1.38 mg/kg) prevented the depletion of gastric GSH content and both quercitrin (1.38 mg/kg) and afzelin (0.078 mg/kg) reduced the MPO activity. These compounds also inhibited the H(+),K(+)-ATPase activity at a concentration of 1-100 μg/ml. In addition, the participation of quercitrin and afzelin in these effects also was confirmed. Furthermore, after 4 days of the treatment, an oral administration of S. chilensis methanolic extract (100 mg/kg) reduced the area of the gastric ulcer induced by acetic acid and the regeneration of the gastric mucosa was accompanied by a reduction in gastric TNF levels. The healing properties of the extract also were confirmed by enhancement of proliferation and coverage of scratched wounds in a fibroblast monolayer. Together, our results confirmed the gastroprotective effect of S. chilensis methanolic extract as well as its gastric healing potential and provided some support to the traditional use of S. chilensis for prevention and treatment of gastric lesions in complementation to its known anti-inflammatory properties.
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas (PPGCF), Universidade do Vale do Itajaí (UNIVALI), Rua Uruguai, 458, Centro, 88302-202, Itajaí, SC, Brazil.
authors.forename: Mariel
authors.initials: M
authors.lastname: de Barros
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas (PPGCF), Universidade do Vale do Itajaí (UNIVALI), Rua Uruguai, 458, Centro, 88302-202, Itajaí, SC, Brazil.
authors.forename: Luisa
authors.initials: L
authors.lastname: Mota da Silva
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas (PPGCF), Universidade do Vale do Itajaí (UNIVALI), Rua Uruguai, 458, Centro, 88302-202, Itajaí, SC, Brazil.
authors.forename: Thaise
authors.initials: T
authors.lastname: Boeing
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas (PPGCF), Universidade do Vale do Itajaí (UNIVALI), Rua Uruguai, 458, Centro, 88302-202, Itajaí, SC, Brazil.
authors.forename: Lincon Bordignon
authors.initials: LB
authors.lastname: Somensi
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas (PPGCF), Universidade do Vale do Itajaí (UNIVALI), Rua Uruguai, 458, Centro, 88302-202, Itajaí, SC, Brazil.
authors.forename: Benhur Judah
authors.initials: BJ
authors.lastname: Cury
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas (PPGCF), Universidade Federal do Paraná (UFPR), Centro Politécnico, Jardim das Américas, 81531-970, Curitiba, PR, Brazil.
authors.forename: Ligia
authors.initials: L
authors.lastname: de Moura Burci
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas (PPGCF), Universidade do Vale do Itajaí (UNIVALI), Rua Uruguai, 458, Centro, 88302-202, Itajaí, SC, Brazil.
authors.forename: José Roberto
authors.initials: JR
authors.lastname: Santin
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas (PPGCF), Universidade do Vale do Itajaí (UNIVALI), Rua Uruguai, 458, Centro, 88302-202, Itajaí, SC, Brazil. sfaloni@gmail.com.
authors.forename: Sérgio Faloni
authors.initials: SF
authors.lastname: de Andrade
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas (PPGCF), Universidade do Vale do Itajaí (UNIVALI), Rua Uruguai, 458, Centro, 88302-202, Itajaí, SC, Brazil.
authors.forename: Franco Delle
authors.initials: FD
authors.lastname: Monache
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas (PPGCF), Universidade do Vale do Itajaí (UNIVALI), Rua Uruguai, 458, Centro, 88302-202, Itajaí, SC, Brazil.
authors.forename: Valdir
authors.initials: V
authors.lastname: Cechinel-Filho
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology; D000897:Anti-Ulcer Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D005260:Female; D005347:Fibroblasts / Q000187:drug effects / Q000378:metabolism / Q000473:pathology; D005753:Gastric Mucosa / Q000187:drug effects* / Q000378:metabolism / Q000473:pathology; D005978:Glutathione / Q000378:metabolism; D017506:H(+)-K(+)-Exchanging ATPase / Q000378:metabolism; D006863:Hydrogen-Ion Concentration; D008362:Mannosides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000432:Methanol / Q000737:chemistry*; D051379:Mice; D008517:Phytotherapy; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D018515:Plant Leaves; D010946:Plants, Medicinal; D044945:Proanthocyanidins / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D054328:Proton Pump Inhibitors / Q000494:pharmacology; D011794:Quercetin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D011817:Rabbits; D017208:Rats, Wistar; D036624:Solidago / Q000737:chemistry*; D012997:Solvents / Q000737:chemistry*; D013276:Stomach Ulcer / Q000139:chemically induced / Q000378:metabolism / Q000473:pathology / Q000517:prevention & control*; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism; D014945:Wound Healing / Q000187:drug effects*
chemical_list: D000893:Anti-Inflammatory Agents; D000897:Anti-Ulcer Agents; D008362:Mannosides; D010936:Plant Extracts; D044945:Proanthocyanidins; D054328:Proton Pump Inhibitors; D012997:Solvents; D014409:Tumor Necrosis Factor-alpha; C012526:quercitrin; C477954:afzelin; D011794:Quercetin; D017506:H(+)-K(+)-Exchanging ATPase; D005978:Glutathione; D000432:Methanol
keywords: Afzelin; Fibroblasts; H+,K+-ATPase; Healing gastric ulcer; Quercitrin; Solidago chilensis