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。
