Phuagkhaopong Suttinee, Sukwattanasombat Jidapha, Suknuntha Kran, Power Christopher, Wonganan Piyanuch, Vivithanaporn Pornpun
Department of Pharmacology, Faculty of Medicine, Chulalongkorn University and King Chulalongkorn Memorial Hospital, Bangkok, Thailand.
Interdisciplinary Program in Pharmacology, Graduate School, Chulalongkorn University, Bangkok, Thailand.
PLoS One. 2025 Jan 14;20(1):e0317281. doi: 10.1371/journal.pone.0317281. eCollection 2025.
Cadmium is a non-essential element and neurotoxin that causes neuroinflammation, which leads to neurodegenerative diseases and brain cancer. To date, there are no specific or effective therapeutic agents to control inflammation and alleviate cadmium-induced progressive destruction of brain cells. Fluoroquinolones (FQs), widely used antimicrobials with effective blood-brain barrier penetration, show promise in being repurposed as anti-inflammatory drugs. Therefore, we aimed to test the efficacy of repurposed FQs for the treatment of cadmium-induced inflammation using cultures of U-87 MG human astrocytes and primary human astrocytes. Both FQs abrogated cadmium-induced interleukin (IL)-6 and IL-8 release from human astrocytes in a concentration and time-dependent manner, although levofloxacin had a stronger inhibitory effect than moxifloxacin. The downregulation of inflammatory cytokine release occurred with a concomitant reduction in cadmium-induced elevations in p65 nuclear factor-κB (NF-κB) and extracellular signal-regulated kinases (ERKs) 1/2 phosphorylation. Additionally, levofloxacin treatment significantly alleviated cadmium-induced activation of phosphorylated NF-κB translocation and toll-like receptor (TLR)-4/signal transducer and activator of transcription (STAT) 3 signaling. Transcriptome analysis revealed that modulation of inflammation-related pathways was the most enriched after FQ treatment. Our data suggest that FQs, particularly levofloxacin, attenuate the inflammatory process mediated by cadmium in human astrocytes. These effects may be mediated, at least in part, by inhibition of immune pathways regulated by TLR4, STAT3, ERK MAPK, and NF-κB.
镉是一种非必需元素和神经毒素,可引发神经炎症,进而导致神经退行性疾病和脑癌。迄今为止,尚无特异性或有效的治疗药物来控制炎症并减轻镉诱导的脑细胞渐进性破坏。氟喹诺酮类药物(FQs)是广泛使用的抗菌药物,具有有效的血脑屏障穿透能力,有望被重新用作抗炎药物。因此,我们旨在使用U-87 MG人星形胶质细胞和原代人星形胶质细胞培养物来测试重新利用的FQs治疗镉诱导的炎症的疗效。两种FQs均以浓度和时间依赖性方式消除了镉诱导的人星形胶质细胞中白细胞介素(IL)-6和IL-8的释放,尽管左氧氟沙星的抑制作用比莫西沙星更强。炎症细胞因子释放的下调伴随着镉诱导的p65核因子-κB(NF-κB)和细胞外信号调节激酶(ERKs)1/2磷酸化升高的降低。此外,左氧氟沙星治疗显著减轻了镉诱导的磷酸化NF-κB易位和Toll样受体(TLR)-4/信号转导和转录激活因子(STAT)3信号通路的激活。转录组分析显示,FQ治疗后炎症相关途径的调节最为丰富。我们的数据表明,FQs,尤其是左氧氟沙星,可减轻镉在人星形胶质细胞中介导的炎症过程。这些作用可能至少部分是通过抑制由TLR4、STAT3、ERK MAPK和NF-κB调节的免疫途径来介导的。