Ito M, Tanaka T, Suzuki Y
Jpn J Pharmacol. 1986 May;41(1):117-25. doi: 10.1254/jjp.41.117.
The effects of teprenone on quantitative changes in gastric mucus glycoprotein during the healing process of acetic acid-induced ulcer in rats were investigated in comparison to those of cimetidine and proglumide. When estimated on the 15th day after operation, teprenone (50 and 100 mg/kg X 2/day, p.o.) significantly decreased the ulcer index by approx. 30%. On the other hand, cimetidine (100 mg/kg X 2/day, p.o.) and proglumide (500 mg/kg X 2/day, p.o.) did not significantly affect it. The high-molecular-weight glycoprotein (HMG, molecular weight of 2 X 10(6) or more) concentration in the gastric mucus of the control group (non-medicated ulcer rats) was 48.7% lower than that of the normal group (non-medicated rats without ulcer). On the contrary, the lower-molecular-weight glycoprotein (LMG, molecular weight between 5 X 10(5) and 2 X 10(6)) concentration of the control group was 95.3% higher than that of the normal group. Teprenone (at both doses) remarkably increased the concentration and secretion of the HMG. In contrast, those of the LMG were decreased by this drug. Cimetidine significantly decreased both the concentration and secretion of the total glycoprotein (HMG + LMG). Proglumide showed only slight increases in the concentration and secretion of the HMG, although it pronouncedly increased the total glycoprotein secretion. These results indicate that teprenone may strengthen the defensive force of gastric mucosa by increasing the HMG with a polymeric structure. In contrast, cimetidine may weaken the mucosal defense.
将替普瑞酮与西咪替丁和丙谷胺相比较,研究了替普瑞酮对大鼠醋酸诱导溃疡愈合过程中胃黏液糖蛋白定量变化的影响。术后第15天评估时,替普瑞酮(50和100mg/kg×2/天,口服)使溃疡指数显著降低约30%。另一方面,西咪替丁(100mg/kg×2/天,口服)和丙谷胺(500mg/kg×2/天,口服)对此无显著影响。对照组(未用药的溃疡大鼠)胃黏液中高分子量糖蛋白(HMG,分子量为2×10⁶或更高)浓度比正常组(未用药的无溃疡大鼠)低48.7%。相反,对照组低分子量糖蛋白(LMG,分子量在5×10⁵和2×10⁶之间)浓度比正常组高95.3%。替普瑞酮(两种剂量)均显著增加HMG的浓度和分泌。相比之下,该药物使LMG的浓度和分泌降低。西咪替丁显著降低总糖蛋白(HMG+LMG)的浓度和分泌。丙谷胺虽然显著增加总糖蛋白分泌,但仅使HMG的浓度和分泌略有增加。这些结果表明,替普瑞酮可能通过增加具有聚合结构的HMG来增强胃黏膜的防御能力。相比之下,西咪替丁可能会削弱黏膜防御。