Evaluation of the antiulcerogenic activity profile of a flavonol diglucoside from Equisetum palustre L.
BACKGROUND
The aerial parts of Equisetum palustre L. are used to treat peptic ulcer disease in Turkey. In a previous study, a flavonol diglucoside i.e., kaempferol 3-O-1''-beta-D-glucopyranosyl-3-O-1'''-beta-D-glucopyranoside (KGG) was isolated as the major antiulcerogenic constituent from the plant.


OBJECTIVE
The present study was undertaken to evaluate the antiulcer activity profile of KGG using various in vivo experimental ulcer models as well as by assessing gastric biochemical parameters.


METHODS
KGG was obtained from the ethanol extract of the aerial parts of the plant by successive chromatographical methods. The activity profile of the compound was investigated using several ulcerogenesis models such as indomethacin-, indomethacin plus HCl/EtOH-, cysteamine-, serotonin-, N(G)-nitro-L-arginine methyl ester plus EtOH-, diethyldithiocarbamate-, N-ethylmaleimide plus EtOH-, water immersion and restraint stress-, pyloric ligation-induced ulcers. In addition, effects of KGG on the biochemical parameters of gastric juice; i.e., inhibition of titratable gastric acidity, acid output, gastric pH, gastric secretion volume and peptic activity were studied.


RESULTS
KGG exerted statistically significant gastroprotective activity against indomethacin-, indomethacin plus HCl/EtOH- and N-ethylmaleimide plus EtOH-induced ulcerogenesis. Moreover, KGG demonstrated weak activity against N(G)-nitro-L-arginine methyl ester plus EtOH, water immersion and immobilization-induced stress, pyloric ligation-induced and diethyldithiocarbamate-induced gastric ulcer models, and also it was ineffective in the prevention of ulcers induced by serotonin and cysteamine. On the other hand, among the gastric biochemical parameters studied, KGG was only found to increase the gastric acid pH from 2.03 to 3.35.


CONCLUSIONS
Results of this investigation have clearly demonstrated that KGG was found to improve the cytoprotective mechanisms of the gastric mucosa. On the other hand, a weak activity profile was observed on the parameters affecting the gastric acidity (water immersion and restraint-induced-, pyloric ligation-induced-ulcerogenesis and titratable acidity).
Yesilada
Erdem
E
Yeditepe University, Faculty of Pharmacy, Department of Pharmacognosy, Kayişdaği 34755, Istanbul, Turkey. yesilada@yeditepe.edu.tr
Gurbuz
Ilhan
I
D000818:Animals; D000897:Anti-Ulcer Agents / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D004353:Drug Evaluation, Preclinical / Q000379:methods; D020829:Equisetum; D005260:Female; D044948:Flavonols / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D005753:Gastric Mucosa / Q000187:drug effects / Q000473:pathology; D005960:Glucosides / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D008297:Male; D051379:Mice; D035261:Plant Components, Aerial; D010936:Plant Extracts / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D051381:Rats; D017207:Rats, Sprague-Dawley; D013276:Stomach Ulcer / Q000473:pathology / Q000517:prevention & control*
D000897:Anti-Ulcer Agents; D044948:Flavonols; D005960:Glucosides; D010936:Plant Extracts