Lee Min-Ho, Hong Il, Kim Mingoo, Lee Byung-Hoon, Kim Ju-Han, Kang Kyung-Sun, Kim Hyung-Lae, Yoon Byung-Il, Chung Heekyoung, Kong Gu, Lee Mi-Ock
College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea.
Toxicology. 2008 Jul 10;249(1):75-84. doi: 10.1016/j.tox.2008.04.011. Epub 2008 Apr 22.
Methotrexate (MTX) is used to treat a variety of chronic inflammatory and neoplastic diseases. However, it can induce hepatotoxicity such as microvesicular steatosis and necrosis. To explore the mechanisms of MTX-induced hepatic steatosis, we used microarray analysis to profile the gene expression patterns of mouse liver after MTX treatment. MTX was administered orally as a single dose of 10mg/kg (low dose) or 100 mg/kg (high dose) to ICR mice, and the livers were obtained 6 h, 24 h, and 72 h after treatment. Serum alanine aminotransferase, aspartate aminotransferase and triacylglycerol levels were not significantly altered in the experimental animals. Signs of steatosis were observed at 24 h after administration of high dose of MTX. From microarray data analysis, 908 genes were selected as MTX-responsive genes (P<0.05, two-way ANOVA; cutoff > or =1.5-fold). Database for Annotation, Visualization and Integrated Discovery (DAVID) analysis revealed that the predominant biological processes associated with these genes are response to unfolded proteins, phosphate metabolism, and cellular lipid metabolism. Functional categorization of these genes identified 28 genes involved in lipid metabolism that was interconnected with the biological pathways of biosynthesis, catabolism, and transport of lipids and fatty acids. Taken together, these data provide a better understanding of the molecular mechanisms of MTX-induced steatogenic hepatotoxicity, and useful information for predicting hepatotoxicity through pattern recognition.
甲氨蝶呤(MTX)用于治疗多种慢性炎症性疾病和肿瘤性疾病。然而,它可诱发肝毒性,如微泡性脂肪变性和坏死。为了探究MTX诱导肝脂肪变性的机制,我们使用微阵列分析来描绘MTX处理后小鼠肝脏的基因表达模式。将MTX以10mg/kg(低剂量)或100mg/kg(高剂量)的单剂量口服给予ICR小鼠,并在处理后6小时、24小时和72小时获取肝脏。实验动物的血清丙氨酸氨基转移酶、天冬氨酸氨基转移酶和三酰甘油水平未发生显著改变。在给予高剂量MTX后24小时观察到脂肪变性的迹象。通过微阵列数据分析,选择了908个基因作为MTX反应性基因(P<0.05,双向方差分析;截断值≥1.5倍)。注释、可视化和综合发现数据库(DAVID)分析显示,与这些基因相关的主要生物学过程是对未折叠蛋白的反应、磷酸盐代谢和细胞脂质代谢。对这些基因的功能分类鉴定出28个参与脂质代谢的基因,这些基因与脂质和脂肪酸的生物合成、分解代谢及转运的生物学途径相互关联。综上所述,这些数据为更好地理解MTX诱导的致脂肪性肝毒性的分子机制提供了依据,并为通过模式识别预测肝毒性提供了有用信息。