Department of Medicine, University of Chicago, Chicago, IL 60637, USA.
Am J Physiol Cell Physiol. 2013 Jul 1;305(1):C78-89. doi: 10.1152/ajpcell.00339.2012. Epub 2013 Apr 17.
Nephrolithiasis remains a major health problem in Western countries. Seventy to 80% of kidney stones are composed of calcium oxalate, and small changes in urinary oxalate affect risk of kidney stone formation. Intestinal oxalate secretion mediated by the anion exchanger SLC26A6 plays an essential role in preventing hyperoxaluria and calcium oxalate nephrolithiasis, indicating that understanding the mechanisms regulating intestinal oxalate transport is critical for management of hyperoxaluria. Purinergic signaling modulates several intestinal processes through pathways including PKC activation, which we previously found to inhibit Slc26a6 activity in mouse duodenal tissue. We therefore examined whether purinergic stimulation with ATP and UTP affects oxalate transport by human intestinal Caco-2-BBe (C2) cells. We measured [¹⁴C]oxalate uptake in the presence of an outward Cl⁻ gradient as an assay of Cl⁻/oxalate exchange activity, ≥50% of which is mediated by SLC26A6. We found that ATP and UTP significantly inhibited oxalate transport by C2 cells, an effect blocked by the PKC inhibitor Gö-6983. Utilizing pharmacological agonists and antagonists, as well as PKC-δ knockdown studies, we observed that ATP inhibits oxalate transport through the P2Y₂ receptor, PLC, and PKC-δ. Biotinylation studies showed that ATP inhibits oxalate transport by lowering SLC26A6 surface expression. These findings are of potential relevance to pathophysiology of inflammatory bowel disease-associated hyperoxaluria, where supraphysiological levels of ATP/UTP are expected and overexpression of the P2Y₂ receptor has been reported. We conclude that ATP and UTP inhibit oxalate transport by lowering SLC26A6 surface expression in C2 cells through signaling pathways including the P2Y₂ purinergic receptor, PLC, and PKC-δ.
肾结石仍然是西方国家的一个主要健康问题。70%到 80%的肾结石由草酸钙组成,尿液中草酸的微小变化会影响肾结石形成的风险。阴离子交换器 SLC26A6 介导的肠道草酸分泌在防止高草酸尿症和草酸钙肾结石形成中起着至关重要的作用,这表明了解调节肠道草酸转运的机制对于高草酸尿症的治疗至关重要。嘌呤能信号通过包括 PKC 激活在内的途径调节几种肠道过程,我们之前发现 PKC 激活可抑制小鼠十二指肠组织中 Slc26a6 的活性。因此,我们研究了用 ATP 和 UTP 刺激嘌呤能是否会影响人肠 Caco-2-BBe (C2) 细胞的草酸转运。我们在存在外向 Cl⁻梯度的情况下测量了 [¹⁴C]草酸的摄取,作为 Cl⁻/草酸交换活性的测定,其中至少有 50%是由 SLC26A6 介导的。我们发现 ATP 和 UTP 可显著抑制 C2 细胞的草酸转运,该作用被 PKC 抑制剂 Gö-6983 阻断。利用药理学激动剂和拮抗剂以及 PKC-δ 敲低研究,我们观察到 ATP 通过 P2Y₂受体、PLC 和 PKC-δ 抑制草酸转运。生物素化研究表明,ATP 通过降低 SLC26A6 的表面表达来抑制草酸转运。这些发现与炎症性肠病相关高草酸尿症的病理生理学相关,其中预计会出现超生理水平的 ATP/UTP,并且已经报道了 P2Y₂受体的过表达。我们得出结论,ATP 和 UTP 通过包括 P2Y₂嘌呤能受体、PLC 和 PKC-δ 在内的信号通路降低 C2 细胞中 SLC26A6 的表面表达来抑制草酸转运。