Tepperman B L, Soper B D
Can J Physiol Pharmacol. 1986 May;64(5):515-20. doi: 10.1139/y86-085.
These studies were designed to examine the changes in the characteristics of prostaglandin E2 (PGE2) binding to porcine oxyntic mucosa in the response to oral ingestion of salicylates. Either acetylsalicylic acid (ASA) or salicylic acid (SA) was administered to conscious pigs (100 mg/kg in 30 mL of an equimolar concentration of NaHCO3) once a day for 1, 3, 10, or 20 days. In control experiments a similar volume of 0.3 M NaHCO3 was administered for similar durations. Mucosal ulceration and the characteristics of the binding of [3H]PGE2 to a 30 000 X g membrane preparation of oxyntic mucosa were examined. Generation of mucosal PGE2 was measured by radioimmunoassay. ASA treatment resulted in an increase in the number and severity of mucosal ulcers and a decrease in PGE2 levels within the first treatment day. By day 20 the degree of ulceration had decreased in spite of a persistent reduction of mucosal PGE2 generation. A variable degree of ulceration was observed in SA-treated animals. In control animals only a single class of binding sites for [3H]PGE2 was evident. After 3 days of ASA treatment a second class of binding sites with a high affinity dissociation constant appeared. There was a decrease in the high affinity binding of [3H]PGE2 after 20 days of ASA ingestion. Low affinity binding was not altered. ASA treatment resulted in a significant increase in specific binding capacities for both families of binding sites. SA treatment did not consistently alter PGE2 binding characteristics from control at any time period studied.(ABSTRACT TRUNCATED AT 250 WORDS)
这些研究旨在检测口服水杨酸盐后,前列腺素E2(PGE2)与猪胃黏膜结合特性的变化。每天给清醒的猪灌服乙酰水杨酸(ASA)或水杨酸(SA)(100mg/kg,溶于30mL等摩尔浓度的NaHCO3中),持续1、3、10或20天。在对照实验中,给猪灌服相同体积的0.3M NaHCO3,持续相同时间。检测胃黏膜溃疡情况以及[3H]PGE2与胃黏膜30000×g膜制剂的结合特性。采用放射免疫分析法测定胃黏膜PGE2的生成量。ASA处理导致在处理的第一天胃黏膜溃疡数量和严重程度增加,且PGE2水平降低。到第20天时,尽管胃黏膜PGE2生成持续减少,但溃疡程度有所减轻。在SA处理的动物中观察到不同程度的溃疡。在对照动物中,仅可见一类[3H]PGE2结合位点。ASA处理3天后,出现了具有高亲和力解离常数的第二类结合位点。摄入ASA 20天后,[3H]PGE2的高亲和力结合减少。低亲和力结合未改变。ASA处理导致两类结合位点的特异性结合能力均显著增加。在研究的任何时间段内,SA处理均未持续改变PGE2的结合特性(摘要截短至250字)