de Camargo Elaine Aparecida, da Silva Glenda Nicioli, de Castro Marcondes João Paulo, Martins David Corrêa, Nadruz Wilson, Schreiber Roberto, Salvadori Décio, Salvadori Daisy Maria Fávero
Department of Pathology, Medical School, UNESP - São Paulo State University, Rubião Junior, Botucatu, SP, 18618-687, Brazil.
School of Pharmacy, UFOP - Federal University of Ouro Preto, Ouro Preto, MG, Brazil.
Arch Toxicol. 2025 Jun 6. doi: 10.1007/s00204-025-04101-4.
Angioplasties using drug-eluting stents remain the most common and effective intervention for coronary artery disease. However, in-stent restenosis (ISR) continues to be the leading cause of stent failure following percutaneous coronary intervention, accounting for 5-10% of all clinical intervention procedures. This study aimed to investigate the potential molecular mechanisms involved in the development of in-stent restenosis. The cytotoxicity, genotoxicity, and transcriptional changes induced by sirolimus, paclitaxel, and mechanical stress were assessed in human coronary artery endothelial and smooth muscle cell lines. Both drugs were similarly effective in suppressing cell growth in these cell lines at different stages of the cell cycle. However, while paclitaxel primarily induced apoptosis, sirolimus caused cell death mainly through necrosis. Additionally, both drugs exhibited genotoxic effects, primarily increasing the levels of oxidized DNA nucleotide bases. Transcriptome analysis identified 23 differentially expressed genes with known biological functions in the chemically treated groups. Interestingly, transcriptomic alterations were also observed in coronary cells subjected solely to mechanical stress. In conclusion, our data confirm that sirolimus and paclitaxel inhibit cell proliferation through distinct mechanisms. Nonetheless, their genotoxic potential appears to act as a stimulus for cell proliferation, thereby increasing the risk of restenosis.
使用药物洗脱支架的血管成形术仍然是治疗冠状动脉疾病最常见且有效的干预手段。然而,支架内再狭窄(ISR)仍是经皮冠状动脉介入治疗后支架失效的主要原因,占所有临床干预手术的5%-10%。本研究旨在探究支架内再狭窄发生发展过程中潜在的分子机制。在人冠状动脉内皮细胞和平滑肌细胞系中评估了西罗莫司、紫杉醇和机械应力诱导的细胞毒性、遗传毒性及转录变化。这两种药物在细胞周期的不同阶段对这些细胞系中细胞生长的抑制效果相似。然而,紫杉醇主要诱导细胞凋亡,而西罗莫司主要通过坏死导致细胞死亡。此外,两种药物均表现出遗传毒性作用,主要是增加氧化型DNA核苷酸碱基的水平。转录组分析在化学处理组中鉴定出23个具有已知生物学功能的差异表达基因。有趣的是,在仅受机械应力作用的冠状动脉细胞中也观察到了转录组改变。总之,我们的数据证实西罗莫司和紫杉醇通过不同机制抑制细胞增殖。尽管如此,它们的遗传毒性潜力似乎会刺激细胞增殖,从而增加再狭窄的风险。