Okabe S, Takeuchi K, Mori Y, Furukawa O, Yamada Y
Nihon Yakurigaku Zasshi. 1986 Dec;88(6):467-76. doi: 10.1254/fpj.88.467.
We studied the effects of KT1-32 (sodium guaiazulene 3-sulfonate) on development of various acute gastric lesions and duodenal ulcers induced in rats. Male Donryu or Sprague-Dawley rats (220-270 g), fasted (but allowed free access to water) for 24 or 48 hr before the experiments, were used. KT1-32 (dissolved in distilled water, 10-100 mg/kg), given p.o. or intraduodenally (i.d.), dose-dependently inhibited the development of gastric lesions induced by HCl X ethanol (60% ethanol in 150 mM HCl), HCl X aspirin (aspirin 100 mg/kg in 150 mM HCl) or aspirin (150 mg/kg in pylorus-ligated preparation) and Shay ulcers (14 hr pylorus ligation). KT1-32 (30 and 100 mg/kg), given p.o. twice (9.5 hr apart), significantly inhibited the development of duodenal ulcers induced by mepirizole (200 mg/kg, s.c.), but did not inhibit gastric lesions developed simultaneously. KT1-32 (30 and 100 mg/kg), given p.o. or i.d., significantly reduced gastric acid secretion when examined using pylorus ligation preparations. KT1-32 (100 mg/kg, i.d.) had no effect on basal and suppressed duodenal HCO3- secretion by mepirizole. These results suggest that KT1-32 is a promising drug for the treatment of gastritis and peptic ulcers.
我们研究了KT1-32(愈创木薁磺酸钠)对大鼠各种急性胃损伤和十二指肠溃疡形成的影响。选用雄性唐利大鼠或斯普拉格-道利大鼠(体重220-270克),在实验前禁食(但可自由饮水)24或48小时。KT1-32(溶于蒸馏水,10-100毫克/千克),经口服或十二指肠内给药,剂量依赖性地抑制了由盐酸X乙醇(150毫摩尔盐酸中的60%乙醇)、盐酸X阿司匹林(150毫摩尔盐酸中的100毫克/千克阿司匹林)或阿司匹林(幽门结扎制备中150毫克/千克)诱导的胃损伤以及应激性溃疡(幽门结扎14小时)的形成。KT1-32(30和100毫克/千克),口服给药两次(间隔9.5小时),显著抑制了美吡拉敏(200毫克/千克,皮下注射)诱导的十二指肠溃疡的形成,但未抑制同时出现的胃损伤。使用幽门结扎制备进行检测时,口服或十二指肠内给予KT1-32(30和100毫克/千克)可显著减少胃酸分泌。十二指肠内给予KT1-32(100毫克/千克)对基础十二指肠碳酸氢根分泌无影响,且可抑制美吡拉敏引起的十二指肠碳酸氢根分泌减少。这些结果表明,KT1-32是一种有前景的治疗胃炎和消化性溃疡的药物。