Hardcastle J, Hardcastle P T, Kelleher D K, Henderson L S, Fondacaro J D
J Rheumatol. 1986 Jun;13(3):541-6.
Mucosal auranofin (AF) caused a concentration dependent inhibition of fluid, Na+, glycine and galactose transport by everted sacs of rat small intestine (IC50 = 2 X 10(-4) M). Inhibition of nutrient absorption was not due to reduced fluid uptake since a similar reduction in fluid uptake induced by a mucosal osmotic load failed to alter glycine transport. Inhibitory effects of AF were not observed when metabolism was reduced, suggesting that carrier mediated entry processes were unaltered. AF inhibited Na+, K+-ATPase activity in isolated enterocytes (IC50 = 2 X 10(-4) M), without affecting Mg2+-dependent ATPase activity. Our studies suggest that the actions of AF on small intestinal absorption may result from inhibition of the Na+ pump.
黏膜金诺芬(AF)对大鼠小肠外翻囊泡的液体、钠离子、甘氨酸和半乳糖转运产生浓度依赖性抑制作用(半数抑制浓度[IC50]=2×10⁻⁴M)。营养物质吸收的抑制并非由于液体摄取减少,因为由黏膜渗透负荷引起的类似液体摄取减少并未改变甘氨酸转运。当代谢降低时未观察到AF的抑制作用,这表明载体介导的进入过程未改变。AF抑制分离肠上皮细胞中的钠钾ATP酶活性(IC50=2×10⁻⁴M),而不影响镁依赖性ATP酶活性。我们的研究表明,AF对小肠吸收的作用可能是由于抑制钠泵所致。