Department of Applied Pharmacology 1, Applied Pharmacology Research Laboratories, Astellas Pharma Inc, Miyukigaoka 21, Tsukuba, Ibaraki 305-8585, Japan.
Transpl Immunol. 2010 May;23(1-2):18-23. doi: 10.1016/j.trim.2010.02.003. Epub 2010 Mar 3.
Acute rejection following renal transplantation has become manageable with the introduction of calcineurin inhibitors, FK506 and cyclosporine A. However, chronic allograft dysfunction accompanied by renal interstitial fibrosis, which induces graft loss, remains unresolved. Here, we evaluated the effect of FR276457, a pan-histone deacetylase (HDAC) inhibitor, on interstitial fibrosis in the injured kidneys of a rat model of unilateral ureteral obstruction. The injured kidneys, harvested on Day 14 following the operation, showed progression of interstitial fibrosis, increases of hydroxyproline contents, and mRNA expression of collagen type Ialpha1 and monocyte chemotactic protein 1 (MCP-1). However, these changes were found to be prevented with daily oral administration of FR276457. In addition, given that MCP-1 is believed to contribute to progressive fibrosis, we investigated the direct effect of FR276457 on MCP-1 production by activated THP-1 cells in vitro. Results showed that FR276457 administration decreased MCP-1 production in these cells in a concentration-dependent manner. Findings from the present study suggested that a pan-HDAC inhibitor may exert a prophylactic effect against renal interstitial fibrosis by inhibiting MCP-1 production.
肾移植后急性排斥反应随着钙调神经磷酸酶抑制剂(FK506 和环孢素 A)的引入而变得可控。然而,伴有肾间质纤维化的慢性移植物功能障碍导致移植物丢失,仍未得到解决。在这里,我们评估了 pan-histone deacetylase(HDAC)抑制剂 FR276457 对单侧输尿管梗阻大鼠模型损伤肾脏间质纤维化的影响。术后第 14 天采集损伤肾脏,结果显示间质纤维化进展,羟脯氨酸含量增加,胶原 Ialpha1 和单核细胞趋化蛋白 1(MCP-1)mRNA 表达增加。然而,发现每日口服 FR276457 可预防这些变化。此外,鉴于 MCP-1 被认为有助于进行性纤维化,我们在体外研究了 FR276457 对激活的 THP-1 细胞中 MCP-1 产生的直接影响。结果表明,FR276457 以浓度依赖性方式降低这些细胞中 MCP-1 的产生。本研究结果表明,pan-HDAC 抑制剂通过抑制 MCP-1 的产生可能对肾间质纤维化发挥预防作用。