[Protective effects of teprenone and gefarnate against taurocholate/hydrochloric acid-induced acute gastric mucosal lesions in rats].
To evaluate the effects of teprenone on acute gastritis, its inhibitory effects on gastric mucosal damage were compared to that of gefarnate in taurocholate/hydrochloric acid-induced acute gastric mucosal lesions in rats. After oral administration of 160 mM taurocholic acid and 250 mM hydrochloric acid, hemorrhage and erosion were macroscopically observed in the gastric mucosal surface layer. Edema in the submucosal tissue and decreased PAS staining in the mucosa were histomorphologically observed. Concerning macroscopic findings, pretreatment with teprenone at a dose of 50 mg/kg or more significantly reduced pathological changes in the mucosa of the fundic glandular area. However, gefarnate slightly inhibited these changes in at a dose of 50 mg/kg and significantly inhibited them at a dose of 200 mg/kg. With regards to histomorphological findings in the fundic glandular area, teprenone slightly inhibited erosion at a dose of 50 mg/kg, and it significantly and slightly inhibited the decrease in PAS staining in this area at doses of 50 and 200 mg/kg, respectively. Gefarnate at doses of 50 and 200 mg/kg showed significant inhibition of decreased PAS staining in the fundic glandular area. In the pyloric mucosa, decreased PAS staining was slightly inhibited by teprenone at both doses but not by gefarnate at either dose. The differences between teprenone and gefarnate observed in this model appear to be due to their differences in mucus production ability. These results suggest that teprenone was more effective than gefarnate for the treatment of gastritis.
Katoh
Y
Y
Department of Applied Drug Research, Eisai Co., Ltd., Tokyo, Japan.
Tanaka
M
M
Kawashima
H
H
D000208:Acute Disease; D000818:Animals; D000897:Anti-Ulcer Agents / Q000008:administration & dosage*; D004195:Disease Models, Animal; D004224:Diterpenes / Q000008:administration & dosage*; D004305:Dose-Response Relationship, Drug; D005753:Gastric Mucosa / Q000473:pathology; D005756:Gastritis / Q000139:chemically induced / Q000473:pathology / Q000517:prevention & control*; D005778:Gefarnate / Q000008:administration & dosage*; D006851:Hydrochloric Acid; D008297:Male; D009093:Mucus / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D013656:Taurocholic Acid
D000897:Anti-Ulcer Agents; D004224:Diterpenes; D005778:Gefarnate; D013656:Taurocholic Acid; D006851:Hydrochloric Acid; C031049:geranylgeranylacetone