Umetsu T, Kimura K, Sanai K, Iwaki K
Eur J Pharmacol. 1980 May 30;64(1):69-77. doi: 10.1016/0014-2999(80)90370-2.
The effect of proglumide on the rate of incorporation of (3H)-N-acetylglucosamine into glycoproteins (GP synthesis) in the glandular stomach in normal, fasting and aspirin-treated rats was studied. GP synthesis was significantly reduced by fasting. In Donryu rats, administration of aspirin (100 mg/kg) significantly decreased GP synthesis and induced the concurrent development of gastric erosions in the corpus, but not in the antrum, where no erosion was detected. Meanwhile, in Wistar rats little or no decrease of GP synthesis was observed in the glandular stomach and only slight erosions were found in the corpus. A negative linear correlation was found between the area of erosions and GP synthesis in the corpus of Donryu rats. Pretreatment with proglumide accelerated GP synthesis in the normal glandular stomach and restored the GP decrease caused by fasting. Gastric erosions induced by aspirin were also inhibited by proglumide and the GP decrease in the corpus was prevented. These results suggest that decreased synthesis of glycoproteins may be associated with the development of erosions induced by aspirin and that proglumide may partly exert its anti-erosive activity by stimulating glycoprotein synthesis in the glandular stomach.
研究了丙谷胺对正常、禁食和阿司匹林处理的大鼠腺胃中(3H)-N-乙酰葡糖胺掺入糖蛋白的速率(GP合成)的影响。禁食显著降低了GP合成。在东ryu大鼠中,给予阿司匹林(100mg/kg)显著降低了GP合成,并在胃体同时诱发了胃糜烂,但在胃窦未检测到糜烂。同时,在Wistar大鼠中,腺胃中GP合成几乎没有或没有降低,仅在胃体发现轻微糜烂。在东ryu大鼠胃体中,糜烂面积与GP合成之间呈负线性相关。丙谷胺预处理可加速正常腺胃中的GP合成,并恢复禁食引起的GP降低。丙谷胺还可抑制阿司匹林诱导的胃糜烂,并防止胃体中GP降低。这些结果表明,糖蛋白合成减少可能与阿司匹林诱导的糜烂的发生有关,丙谷胺可能通过刺激腺胃中的糖蛋白合成部分发挥其抗糜烂活性。