Suzuki Y, Hayashi M, Ito M, Yamagami I
Jpn J Pharmacol. 1976 Aug;26(4):471-80. doi: 10.1254/jjp.26.471.
Anti-ulcer effects of cetraxate, a new compound possessing anti-plasmin, anti-casein and anti-trypsin actions were investigated by using experimental gastric ulcer models in rats. Cetraxate, 300 mg/kg p.o. showed significant inhibitory effects of 65.3%, 70.0%, 30.2%, and 67.1% against aucte types of ulcers producing by aspirin, phenylbutazone, indomethacin, and pyloric ligature (Shay's ulcer), respectively. These effects were greater than those obtained by gefarnate and aluminum sucrose sulfate may be mainly attributed to the protecting action of this drug on gastric mucosa. Ctraxate further revealed remarkable inhibitory effects on chronic types of ulcers produced by acetic acid, clamping, and clamping-cortisone. In acetic acid ulcer in particular, cetraxate was found to have a dose-dependent inhibitory effect at doses over 50 mg/kg. Of test drugs including L-glutamine and methylmethionine sulfonium chloride, cetraxate showed the most remarkable inhibitory effect on beta-glucuronidase activity in ulcer tissue of these three types of ulcers. These findings suggest that cetraxate may prevent the connective tissue in the ulcer location from decomposition due to lysosomal enzymes such as beta-glucuronidase, thereby accelerating the recovery from ulcer.
利用大鼠实验性胃溃疡模型，对具有抗纤溶酶、抗酪蛋白和抗胰蛋白酶作用的新化合物西曲酸酯的抗溃疡作用进行了研究。口服300mg/kg的西曲酸酯对阿司匹林、保泰松、吲哚美辛和幽门结扎（ Shay溃疡）引起的急性溃疡类型分别显示出65.3%、70.0%、30.2%和67.1%的显著抑制作用。这些作用大于吉法酯和硫酸铝蔗糖所产生的作用，可能主要归因于该药物对胃黏膜的保护作用。西曲酸酯对乙酸、钳夹和钳夹 - 可的松引起的慢性溃疡类型也显示出显著的抑制作用。特别是在乙酸溃疡中，发现西曲酸酯在剂量超过50mg/kg时具有剂量依赖性抑制作用。在包括L - 谷氨酰胺和氯化甲基蛋氨酸在内的受试药物中，西曲酸酯对这三种溃疡类型的溃疡组织中的β - 葡萄糖醛酸酶活性显示出最显著的抑制作用。这些发现表明，西曲酸酯可能防止溃疡部位的结缔组织因β - 葡萄糖醛酸酶等溶酶体酶的分解，从而加速溃疡的恢复。
