Effect of bisacodyl on the uptake of monosaccharides by isolated enterocytes.

Drug-nutrient interactions Pub Date : 1986-01-01
M Moretó, J M Planas, C de Gabriel
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Abstract

Diphenolic laxatives are known to alter nutrient absorption and secretion in the small and large intestine. We have studied the effect of 0.75 mM bisacodyl on sugar transport in isolated chicken intestinal epithelial cells. Results show that (1) bisacodyl inhibits Na+-dependent alpha-methyl-glucoside (alpha-MG) accumulation by 45% after 40-minute incubation. (2) The drug reduces initial (1 minute) alpha-MG influx by 60%. This effect is much lower than that exerted by 0.15 mM phlorizin (90% inhibition). (3) Bisacodyl also reduces Na+-independent sugar flux through the basolateral membrane since initial 2-deoxy-glucose influx is reduced 67% by the drug. The effect of the drug on this pathway is lower than that exerted by theophylline (7.5 mM). The addition of bisacodyl or theophylline (plus 20 microM phlorizin to inhibit the apical sugar transport system) to cells preloaded with 3-oxy-methyl-glucose allowed calculation of the initial sugar efflux rate. This was found to be lower after theophylline addition than after the addition of bisacodyl, thus confirming that bisacodyl exerts an incomplete inhibition of the Na+-independent sugar transport system. It is concluded that the direct effects of bisacodyl on both apical and basolateral sugar transport pathways may explain in part the inhibitory effects of the drug on the intestinal absorption of sugars.

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bisacodyl对分离肠细胞摄取单糖的影响。
众所周知,二酚类泻药可以改变小肠和大肠的营养吸收和分泌。本实验研究了0.75 mM双碱对离体鸡肠上皮细胞糖转运的影响。结果表明:(1)经孵育40分钟后,bisacodyl抑制Na+依赖性α -甲基-葡萄糖苷(α - mg)积累45%。(2)该药使初始(1分钟)α - mg内流减少60%。这种抑制作用远低于0.15 mM的苯并菌素(90%)。(3)由于初始的2-脱氧葡萄糖内流被药物减少67%,Bisacodyl还减少了通过基底外侧膜的Na+独立糖通量。该药对该通路的影响小于茶碱(7.5 mM)。在预先装载了3-氧-甲基葡萄糖的细胞中加入双草酰或茶碱(加上20微米的苯连菌素以抑制顶端糖运输系统),可以计算初始糖外排速率。结果发现,添加茶碱后,这一比例低于添加双碱后,从而证实了双碱对Na+非依赖性糖转运系统具有不完全抑制作用。由此可见,比沙代碱对糖的根尖和底外侧转运途径的直接作用可能部分解释了该药物对糖的肠道吸收的抑制作用。
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