Tenenhouse H S, Lee J, Harvey N
Department of Pediatrics, McGill University-Montreal Children's Hospital Research Institute, Quebec, Canada.
Am J Physiol. 1991 Sep;261(3 Pt 2):F420-6. doi: 10.1152/ajprenal.1991.261.3.F420.
The present study was undertaken to examine the interaction of phosphonoformic acid (PFA) with the Na(+)-sulfate cotransporter and the effect of thyroid hormone (triiodothyronine; T3) on Na(+)-dependent sulfate transport and Na(+)-dependent PFA binding in mouse renal brush-border membrane vesicles. PFA inhibits Na(+)-dependent sulfate transport in a competitive manner [apparent inhibitory constant (Ki) = 4.3 +/- 1.1 mM]. T3 administered in pharmacological doses significantly stimulates Na(+)-dependent sulfate transport in renal brush-border membranes compared with vehicle-treated controls. Although T3 has no effect on Na(+)-dependent glucose transport, T3 also stimulates Na(+)-dependent phosphate transport. Kinetic studies demonstrate that T3 increases the apparent maximal velocity (Vmax) for Na(+)-sulfate cotransport without changing the apparent Michaelis constant (Km). T3 does not significantly affect either Na(+)-dependent PFA binding or the phosphate- and sulfate-displaceable components of Na(+)-dependent PFA binding. Finally, Na(+)-dependent brush-border membrane sulfate transport is unchanged in phosphate-deprived mice that exhibit increased Na(+)-phosphate cotransport and in X-linked Hyp mice that exhibit impaired Na(+)-phosphate cotransport. The present results demonstrate that 1) PFA is a competitive inhibitor of Na(+)-sulfate cotransport, 2) T3 stimulates Na(+)-dependent sulfate, as well as Na(+)-dependent phosphate transport, but has no effect on PFA binding, and 3) phosphate deprivation and the X-linked Hyp mutation do not influence Na(+)-sulfate cotransport.(ABSTRACT TRUNCATED AT 250 WORDS)
本研究旨在检测膦甲酸(PFA)与钠-硫酸盐共转运体的相互作用,以及甲状腺激素(三碘甲状腺原氨酸;T3)对小鼠肾刷状缘膜囊泡中钠依赖性硫酸盐转运和钠依赖性PFA结合的影响。PFA以竞争性方式抑制钠依赖性硫酸盐转运[表观抑制常数(Ki)=4.3±1.1 mM]。与溶剂处理的对照组相比,给予药理剂量的T3可显著刺激肾刷状缘膜中钠依赖性硫酸盐转运。虽然T3对钠依赖性葡萄糖转运没有影响,但T3也能刺激钠依赖性磷酸盐转运。动力学研究表明,T3增加了钠-硫酸盐共转运的表观最大速度(Vmax),而不改变表观米氏常数(Km)。T3对钠依赖性PFA结合或钠依赖性PFA结合的磷酸盐和硫酸盐可置换成分均无显著影响。最后,在表现出钠-磷酸盐共转运增加的低磷小鼠和表现出钠-磷酸盐共转运受损的X连锁低磷血症小鼠中,钠依赖性刷状缘膜硫酸盐转运没有变化。目前的结果表明:1)PFA是钠-硫酸盐共转运的竞争性抑制剂;2)T3刺激钠依赖性硫酸盐以及钠依赖性磷酸盐转运,但对PFA结合没有影响;3)磷酸盐缺乏和X连锁低磷血症突变不影响钠-硫酸盐共转运。(摘要截短至250字)