Peng Fangyuan, Feng Jinghan, Zhang Xinni, Ren Ting, Zeng Qi, Sun Qian, Zou Zhouping, Ding Xiaoqiang, Jia Ping
Division of Nephrology, Zhongshan Hospital, Fudan University, Shanghai, China.
Shanghai Medical Center of Kidney, Shanghai, China.
J Cell Mol Med. 2025 Jul;29(14):e70730. doi: 10.1111/jcmm.70730.
Inflammatory responses play a critical role in cisplatin-induced acute kidney injury (AKI). Farnesoid X receptor (FXR) has been shown to mitigate kidney dysfunction, but its mechanism remains unclear. This study aims to explore whether FXR reduces cisplatin-induced AKI by modulating inflammation. Using a mouse model of AKI, we demonstrated that cisplatin-induced obvious inflammation in the kidney, evidenced by increased macrophage and neutrophil infiltration, elevated expression of pro-inflammatory cytokines, including interleukin-1 beta (IL-1β), IL-6, C-X-C motif chemokine ligand (CXCL) 1, 2, 5, 20, and C-C motif chemokine ligand (CCL) 2, and activation of the toll-like receptor 4 (Tlr4)/nuclear factor-kappa B (NF-κB) pathway. RNA sequencing further corroborated these findings, revealing upregulation of inflammation-related genes and activation of several inflammatory pathways in the kidney after cisplatin administration. Pretreatment with GW4064 (a FXR agonist) reduced inflammatory cytokine expression, immune cell infiltration, and Tlr4/NF-κB activation, alleviating kidney injury. However, proximal tubule-specific FXR knockout worsened renal inflammation and increased NF-κB activity. In vitro, GW4064 decreased pro-inflammatory cytokine production, suppressed Tlr4/NF-κB signalling, and reduced apoptosis in cisplatin-treated renal tubular epithelial cells. Together, these findings demonstrate that FXR significantly alleviates cisplatin-induced renal inflammation via suppressing Tlr4/NF-κB signalling. FXR activation may represent a promising therapeutic strategy to mitigate cisplatin-induced AKI.
炎症反应在顺铂诱导的急性肾损伤(AKI)中起关键作用。法尼酯X受体(FXR)已被证明可减轻肾功能障碍,但其机制仍不清楚。本研究旨在探讨FXR是否通过调节炎症来减轻顺铂诱导的AKI。使用AKI小鼠模型,我们证明顺铂可诱导肾脏明显炎症,表现为巨噬细胞和中性粒细胞浸润增加、促炎细胞因子表达升高,包括白细胞介素-1β(IL-1β)、IL-6、C-X-C基序趋化因子配体(CXCL)1、2、5、20和C-C基序趋化因子配体(CCL)2,以及Toll样受体4(Tlr4)/核因子-κB(NF-κB)通路的激活。RNA测序进一步证实了这些发现,揭示了顺铂给药后肾脏中炎症相关基因的上调和几种炎症通路的激活。用GW4064(一种FXR激动剂)预处理可降低炎症细胞因子表达、免疫细胞浸润和Tlr4/NF-κB激活,减轻肾损伤。然而,近端小管特异性FXR基因敲除会加重肾脏炎症并增加NF-κB活性。在体外,GW4064可减少顺铂处理的肾小管上皮细胞中促炎细胞因子的产生,抑制Tlr4/NF-κB信号传导,并减少细胞凋亡。总之,这些发现表明FXR通过抑制Tlr4/NF-κB信号传导显著减轻顺铂诱导的肾脏炎症。FXR激活可能是减轻顺铂诱导的AKI的一种有前景的治疗策略。