STUDIES ON ANTIULCER EFFECTS OF A NEW COMPOUND, ZINC L-CARNOSINE (Z-103)
STUDIES ON ANTIULCER EFFECTS OF A NEW COMPOUND, ZINC L-CARNOSINE (Z-103)
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DOI：
10.1254/fpj.95.5_257
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发表时间：
1990-05-01
影响因子：
--
通讯作者：
OKABE, S
中科院分区：
文献类型：
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作者：
SEIKI, M;UEKI, S;OKABE, S
采用大鼠胃、十二指肠急性损伤模型，研究了L-肌肽锌（Z-103）的抗溃疡作用。Z-103对各种胃功能的影响，例如，同时检测抗酸剂（体外）、抗胃蛋白酶（体外）、胃液分泌、粘膜电位差（PD）和粘液含量。口服Z-103可预防水浸应激、组胺、盐酸-阿司匹林、盐酸-乙醇诱导的胃损伤，也可剂量依赖性预防美吡唑诱导的十二指肠溃疡。在体外，Z-103的抗酸作用大于碳酸氢钠;此外，其抗消化作用的效力（IC 50 =8.7 mM）高于其他几种药物（碳酸氢钠、蔗糖硫酸盐和乙酰氨基铝）。Z-103（100 mg/kg）单独灌胃给药倾向于增加PD，并且还显著抑制阿司匹林引起的PD降低。此外，用10和30 mg/kg（p.o.）显著防止胃粘膜中粘液含量的减少以及口服乙醇引起的粘膜损伤。另一方面，Z-103对基础（幽门结扎制备）和组胺刺激的胃分泌（Heidenhain袋制备）均不那么有效。结果表明，Z-103可用于治疗人类胃溃疡和十二指肠溃疡。
We investigated the anti-ulcer effects of zinc L-carnosine (Z-103) using several acute experimental models of gastric and duodenal lesions in rats. Effects of Z-103 on various gastric functions, e.g., antacid (in vitro), anti-pepsin (in vitro), gastric secretion, mucosal potential difference (PD) and mucus contents were also examined. Z-103 given orally prevented development of gastric lesions induced by water immersion stress, histamine, HCl-aspirin, HCl-ethanol and also duodenal ulcers induced by mepirizole in a dose-dependent manner. In vitro, Z-103 had a greater antacid effect than sodium bicarbonate; and moreover, the potency of its anti-peptic action (IC50=8.7 mM) was higher than those of several other drugs (sodium bicarbonate, sucrose sulfate and aceglutamide aluminum). Intragastric treatment of Z-103 (100 mg/kg) alone tended to increase PD, and it also significantly inhibited the decrease in PD induced by aspirin. In addition, pretreatment with Z-103 at 10 and 30 mg/kg (p.o.) significantly prevented the decrease in mucus contents in the gastric mucosa and also mucosal lesions by oral administration of ethanol. On the other hand, Z-103 was not so effective on both basal (pylorus-ligation preparation) and histamine-stimulated gastric secretion (Heidenhain pouch preparation). The results suggest that Z-103 is useful for the treatment of gastric and duodenal ulcers in humans.