Mohsen A Q, Mulvey D, Priddle J D, Parsons D S, Jewell D P
Gut. 1987 Mar;28(3):346-52. doi: 10.1136/gut.28.3.346.
Olsalazine (ADS) is the azo-linked dimer of 5-aminosalicylic acid (5-ASA). It is of value for the management of patients with ulcerative colitis but may be associated with increasing diarrhoea in a few. This study examines the effect of 5-ASA and ADS on small intestinal transport systems of the rat. Krebs-Ringer-bicarbonate solution was circulated through the lumen of a jejunal segment and the appearance of fluid, glucose and lactate on the serosal surface was shown to be linear over a two hour period. Addition of 5-ASA (10 mmol/l) or ADS (5 mmol/l and 10 mmol/l) caused a significant inhibition both of fluid transport (p less than 0.001), and of the appearance of glucose (p less than 0.001) and lactate (p less than 0.001 for 5 mmol/l and 10 mmol/l ADS, p less than 0.01 for 10 mmol/l 5-ASA). The uptake of glucose by rings of rat jejunum was shown to be markedly reduced by ADS. Experiments substituting glucose with either sucrose of 2-aminoisobutyric acid showed that ADS (5 mmol/l, 10 mmol/l) also inhibited the serosal appearance of fructose and the amino acid. These results show that 5-ASA and ADS, at concentrations which could be expected in the jejunum of patients receiving therapeutic doses, are able to inhibit small intestinal transport systems. The resulting increase in load on the diseased colon could be important for the pathogenesis of diarrhoea.
奥沙拉嗪（ADS）是5-氨基水杨酸（5-ASA）的偶氮连接二聚体。它对溃疡性结肠炎患者的治疗有价值，但少数患者可能会出现腹泻加重的情况。本研究考察了5-ASA和ADS对大鼠小肠转运系统的影响。 Krebs-Ringer碳酸氢盐溶液在空肠段腔内循环，结果显示在两小时内，浆膜表面液体、葡萄糖和乳酸的出现呈线性关系。添加5-ASA（10 mmol/L）或ADS（5 mmol/L和10 mmol/L）会显著抑制液体转运（p<0.001），以及葡萄糖（p<0.001）和乳酸的出现（5 mmol/L和10 mmol/L的ADS，p<0.001；10 mmol/L的5-ASA，p<0.01）。结果表明，ADS可显著降低大鼠空肠环对葡萄糖的摄取。用蔗糖或2-氨基异丁酸替代葡萄糖的实验表明，ADS（5 mmol/L，10 mmol/L）也会抑制果糖和氨基酸在浆膜表面的出现。这些结果表明，在接受治疗剂量的患者空肠中预期会出现的浓度下，5-ASA和ADS能够抑制小肠转运系统。患病结肠负荷的增加可能对腹泻的发病机制很重要。
