The guaianolide type
sesquiterpene lactones chlorojanerin, 13-acetyl
solstitialin A and
solstitialin A were identified as the anti-ulcerogenic components of the
chloroform extract of the aerial parts of Centaurea solstitialis ssp. solstitialis (Asteraceae). In this study, these compounds were investigated by using various in vivo
ulcer models in rats and mice.
Chlorojanerin was shown to be significantly effective in preventing the induction of lesions by
ethanol- (EtOH-) (both oral and subcutaneous administration),
indomethacin-,
indomethacin plus HCl/EtOH-,
N(G)-nitro-l-arginine methyl ester plus EtOH-,
N-ethylmaleimide plus EtOH-, water immersion and restraint stress, and
serotonin, as well as inhibiting titratable gastric acidity and
acid output, and increasing gastric pH, but was ineffective in the prevention of
ulcers induced by pyloric
ligation,
diethyldithiocarbamate, and
cysteamine, and had no effect on gastric secretion volume or peptic activity. A mixture of 13-acetyl
solstitialin A (95%) and
solstitialin A (5%) was found to be significantly effective against EtOH-induced lesions on
oral administration but was ineffective when administered subcutaneously. This mixture was also found to be effective in preventing lesions induced by EtOH,
indomethacin,
indomethacin plus HCl/EtOH,
N(G)-nitro-l-arginine methyl ester plus EtOH,
N-ethylmaleimide plus EtOH, water immersion and restraint stress,
serotonin and
cysteamine, as well as inhibiting titratable gastric acidity and titratable
acid output, and gastric pH, but was found ineffective against the pyloric
ligation-induced and
diethyldithiocarbamate-induced ulcerogenesis models, as well as gastric secretion volume and peptic activity. On the other hand, active compounds did not show any toxic effect on acute toxicity (3 days administration) evaluation tests in mice.