title: The effects of baicalein on gastric mucosal ulcerations in mice: Protective pathways and anti-secretory mechanisms.
abstract: Many flavonoids have been shown to present good results for the treatment of gastric ulcers. Baicalein, a bioactive flavonoid derived from the Scutellaria baicalensis Georgi root, possesses several biological effects, such as anti-inflammatory and antioxidant. This study was conducted to assess the gastroprotective properties of baicalein. Anti-ulcerogenic assay was performed using the protocol of ulcer induced by ethanol/HCl in mice; then, the role of presynaptic α2-receptors, sulfhydryl (SH) compounds, nitric oxide (NO), prostaglandin (PG) and ATP-sensitive K+(KATP) channels in gastroprotection of baicalein was investigated. The levels of reduced glutathione (GSH) and the myeloperoxidase (MPO) activity were measured in the gastric mucosa. Parameters of gastric secretion (volume, [H+] and pH) were determined with or without the presence of the secretagogue agent histamine, as well as mucus in gastric contents, by the pylorus ligation model. In vitro H+,K+-ATPase activity was also determined. Baicalein (10, 30 and 100 mg/kg) exhibited a dose related gastroprotective effect (P < 0.001) against acidified ethanol-induced lesions. The intraperitoneal treatment of mice with a α2-adrenoreceptor antagonist (yohimbine; 2 mg/kg), a SH compounds blocker (N-ethylmaleimide, NEM; 10 mg/kg), a non-selective inhibitor of NO synthase (Nw-nitro-L-arginine methyl ester hydrochloride, L-NAME; 10 mg/kg), a non-selective inhibitor of cyclo-oxygenase (indomethacin; 10 mg/kg) or a KATPchannel blocker (glibenclamide; 10 mg/kg) was able to reverse (P < 0.001) the gastroprotective response caused by baicalein (30 mg/kg). Baicalein (30 mg/kg; P < 0.05) was able to increase GSH levels and decreasing MPO activity. The intraduodenal treatment with baicalein (30 and 100 mg/kg) significantly increased (P < 0.05) the gastric mucus secretion. Additionally, the treatment with baicalein reduced (30 and 100 mg/kg; P < 0.05) the secretion volume and total acid secretion, and also increased (10, 30 and 100 mg/kg; P < 0.001) the pH value, after pylorus ligature. Baicalein (30 mg/kg) was also effective in inhibiting the effects of histamine on gastric secretion (volume, [H+] and pH; P < 0.001). Baicalein at 10 and 30 μg/mL showed anti-H+,K+-ATPase activity. In conclusion, the present results provide convincing evidence that baicalein could be used as a cytoprotective (preventive effect) and anti-ulcerogenic (anti-secretory effect) agent in the gastric ulcers.
authors: Departamento de Fisiologia, Universidade Federal de Sergipe, Av. Marechal Rondon, Cidade Universitária, CEP 49100-000 São Cristóvão, Sergipe, Brazil.
authors: Ana Roseli S
authors: AR
authors: Ribeiro
authors: Departamento de Fisiologia, Universidade Federal de Sergipe, Av. Marechal Rondon, Cidade Universitária, CEP 49100-000 São Cristóvão, Sergipe, Brazil.
authors: José Diego
authors: JD
authors: do Nascimento Valença
authors: Departamento de Fisiologia, Universidade Federal de Sergipe, Av. Marechal Rondon, Cidade Universitária, CEP 49100-000 São Cristóvão, Sergipe, Brazil.
authors: Jeferson
authors: J
authors: da Silva Santos
authors: Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade do Vale do Itajaí, Rua Uruguai, 458, CEP 88302-202 Itajaí, Santa Catarina, Brazil.
authors: Thaise
authors: T
authors: Boeing
authors: Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade do Vale do Itajaí, Rua Uruguai, 458, CEP 88302-202 Itajaí, Santa Catarina, Brazil.
authors: Luisa Mota
authors: LM
authors: da Silva
authors: Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade do Vale do Itajaí, Rua Uruguai, 458, CEP 88302-202 Itajaí, Santa Catarina, Brazil.
authors: Sérgio Faloni
authors: SF
authors: de Andrade
authors: Instituto de Tecnologia e Pesquisa-ITP, Universidade Tiradentes, Av. Murilo Dantas, 300, CEP 49032-490 Aracaju, Sergipe, Brazil.
authors: Ricardo L C
authors: RL
authors: Albuquerque-Júnior
authors: Departamento de Fisiologia, Universidade Federal de Sergipe, Av. Marechal Rondon, Cidade Universitária, CEP 49100-000 São Cristóvão, Sergipe, Brazil. Electronic address: sthomazzi@gmail.com.
authors: Sara Maria
authors: SM
authors: Thomazzi
mesh_terms: D000818:Animals; D000431:Ethanol; D005260:Female; D044950:Flavanones / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*; D005750:Gastric Juice / Q000378:metabolism; D005753:Gastric Mucosa / Q000187:drug effects / Q000378:metabolism* / Q000473:pathology*; D005978:Glutathione / Q000378:metabolism; D017506:H(+)-K(+)-Exchanging ATPase / Q000378:metabolism; D006851:Hydrochloric Acid; D054086:KATP Channels / Q000378:metabolism; D008297:Male; D051379:Mice; D009195:Peroxidase / Q000378:metabolism; D011453:Prostaglandins / Q000378:metabolism; D020011:Protective Agents / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*; D013270:Stomach / Q000187:drug effects; D013276:Stomach Ulcer / Q000139:chemically induced / Q000188:drug therapy / Q000473:pathology
chemical_list: D044950:Flavanones; D054086:KATP Channels; D011453:Prostaglandins; D020011:Protective Agents; D000431:Ethanol; C006680:baicalein; D009195:Peroxidase; D017506:H(+)-K(+)-Exchanging ATPase; D005978:Glutathione; D006851:Hydrochloric Acid
keywords: Baicalein; Flavonoids; Gastric ulcer; Gastroprotection