In vivo inhibition of gastric acid secretion by the aqueous extract of Scoparia dulcis L. in rodents.
The freeze-dried aqueous extract (AE) from the aerial parts of Scoparia dulcis was tested for its effects on experimental gastric hypersecretion and ulcer in rodents. Administration of AE to animals with 4h pylorus ligature potently reduced the gastric secretion with ED(50)s of 195 mg/kg (rats) and 306 mg/kg (mice). The AE also inhibited the histamine- or bethanechol-stimulated gastric secretion in pylorus-ligated mice with similar potency suggesting inhibition of the proton pump. Bio-guided purification of the AE yielded a flavonoid-rich fraction (BuF), with a specific activity 4-8 times higher than the AE in the pylorus ligature model. BuF also inhibited the hydrolysis of ATP by H(+),K(+)-ATPase with an IC(50) of 500 microg/ml, indicating that the inhibition of gastric acid secretion of Scoparia dulcis is related to the inhibition of the proton pump. Furthermore, the AE inhibited the establishment of acute gastric lesions induced in rats by indomethacin (ED(50)=313 mg/kg, p.o.) and ethanol (ED(50)=490 mg/kg, p.o.). No influence of the AE on gastrointestinal transit allowed discarding a possible CNS or a cholinergic interaction in the inhibition of gastric secretion by the AE. Collectively, the present data pharmacologically validates the popular use of Scoparia dulcis in gastric disturbances.
Mesía-Vela
Sonia
S
Natural Products Section, Department of Pharmacology, Escola Paulista de Medicina, Universidade Federal de São Paulo, 04044-020 Rua 03 de Maio 100, São Paulo, SP, Brazil. sm2418@columbia.edu
Bielavsky
Monica
M
Torres
Luce Maria Brandão
LM
Freire
Sonia Maria
SM
Lima-Landman
Maria Teresa R
MT
Souccar
Caden
C
Lapa
Antonio José
AJ
D000818:Animals; D000897:Anti-Ulcer Agents / Q000494:pharmacology; D003433:Crosses, Genetic; D004353:Drug Evaluation, Preclinical; D005260:Female; D005744:Gastric Acid / Q000378:metabolism*; D005745:Gastric Acidity Determination; D005753:Gastric Mucosa / Q000187:drug effects* / Q000378:metabolism; D008026:Ligation; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008810:Mice, Inbred C57BL; D008517:Phytotherapy; D010936:Plant Extracts / Q000494:pharmacology*; D011708:Pylorus / Q000601:surgery; D051381:Rats; D017208:Rats, Wistar; D036721:Scoparia / Q000737:chemistry*; D013270:Stomach / Q000187:drug effects; D014867:Water / Q000737:chemistry*
D000897:Anti-Ulcer Agents; D010936:Plant Extracts; D014867:Water