The University of Melbourne, Department of Medicine, St. Vincent’s Hospital, VIC, Australia.
Nephrol Dial Transplant. 2011 Jan;26(1):100-10. doi: 10.1093/ndt/gfq355. Epub 2010 Jun 23.
Diabetic nephropathy is the leading cause of kidney failure in the developed world. Tranilast has been reported to not only act as an anti-inflammatory and anti-fibrotic compound, but it also exerts anti-oxidative stress effects in diabetic nephropathy. Thioredoxin-interacting protein (Txnip) is the endogenous inhibitor of the anti-oxidant thioredoxin and is highly up-regulated in diabetic nephropathy, leading to oxidative stress and fibrosis. In this study, we aimed to investigate whether tranilast exerts its anti-oxidant properties through the inhibition of Txnip.
Heterozygous Ren-2 rats were rendered diabetic with streptozotocin. Another group of rats were injected with citrate buffer alone and treated as non-diabetic controls. After 6 weeks of diabetes, diabetic rats were divided into two groups: one group gavaged with tranilast at 200 mg/kg/day and another group with vehicle.
Diabetic rats had a significant increase in albuminuria, tubulointerstitial fibrosis, peritubular collagen IV accumulation, reactive oxygen species (ROS) and macrophage infiltration (all P < 0.05). These changes were associated with an increase in Txnip mRNA and protein expression in the tubules and glomeruli of diabetic kidney. Treatment with tranilast for 4 weeks significantly attenuated Txnip up-regulation in diabetic rats and this was associated with a reduction in ROS, fibrosis and macrophage infiltration (all P < 0.05).
This is the first study to demonstrate that tranilast not only has anti-inflammatory and anti-fibrotic effects as previously reported but also attenuates the up-regulation of Txnip and oxidative stress in diabetic nephropathy.
糖尿病肾病是发达国家肾衰竭的主要原因。已有报道称曲尼司特不仅具有抗炎和抗纤维化作用,而且在糖尿病肾病中还具有抗氧化应激作用。硫氧还蛋白相互作用蛋白(Txnip)是抗氧化剂硫氧还蛋白的内源性抑制剂,在糖尿病肾病中高度上调,导致氧化应激和纤维化。在这项研究中,我们旨在研究曲尼司特是否通过抑制 Txnip 发挥其抗氧化特性。
杂合 Ren-2 大鼠用链脲佐菌素制成糖尿病。另一组大鼠仅注射柠檬酸盐缓冲液作为非糖尿病对照。糖尿病 6 周后,将糖尿病大鼠分为两组:一组给予 200mg/kg/天的曲尼司特灌胃,另一组给予载体。
糖尿病大鼠的蛋白尿、肾小管间质纤维化、肾小管周围胶原 IV 积聚、活性氧(ROS)和巨噬细胞浸润均显著增加(均 P<0.05)。这些变化与糖尿病肾脏中 Txnip mRNA 和蛋白表达的增加有关。曲尼司特治疗 4 周可显著抑制糖尿病大鼠 Txnip 的上调,这与 ROS、纤维化和巨噬细胞浸润的减少有关(均 P<0.05)。
这是第一项表明曲尼司特不仅具有先前报道的抗炎和抗纤维化作用,而且还可减轻糖尿病肾病中 Txnip 上调和氧化应激的研究。