Department of Pharmacology and Toxicology, Radboud University Nijmegen Medical Centre, Nijmegen, The Netherlands.
PLoS One. 2012;7(11):e49524. doi: 10.1371/journal.pone.0049524. Epub 2012 Nov 14.
Drug-induced liver injury (DILI) is the leading cause of acute liver failure. Currently, no adequate predictive biomarkers for DILI are available. This study describes a translational approach using proteomic profiling for the identification of urinary proteins related to acute liver injury induced by acetaminophen (APAP). Mice were given a single intraperitoneal dose of APAP (0-350 mg/kg bw) followed by 24 h urine collection. Doses of ≥275 mg/kg bw APAP resulted in hepatic centrilobular necrosis and significantly elevated plasma alanine aminotransferase (ALT) values (p<0.0001). Proteomic profiling resulted in the identification of 12 differentially excreted proteins in urine of mice with acute liver injury (p<0.001), including superoxide dismutase 1 (SOD1), carbonic anhydrase 3 (CA3) and calmodulin (CaM), as novel biomarkers for APAP-induced liver injury. Urinary levels of SOD1 and CA3 increased with rising plasma ALT levels, but urinary CaM was already present in mice treated with high dose of APAP without elevated plasma ALT levels. Importantly, we showed in human urine after APAP intoxication the presence of SOD1 and CA3, whereas both proteins were absent in control urine samples. Urinary concentrations of CaM were significantly increased and correlated well with plasma APAP concentrations (r = 0.97; p<0.0001) in human APAP intoxicants, who did not present with elevated plasma ALT levels. In conclusion, using this urinary proteomics approach we demonstrate CA3, SOD1 and, most importantly, CaM as potential human biomarkers for APAP-induced liver injury.
药物性肝损伤(DILI)是急性肝衰竭的主要原因。目前,尚无充分的 DILI 预测生物标志物。本研究描述了一种使用蛋白质组学分析鉴定与对乙酰氨基酚(APAP)诱导的急性肝损伤相关的尿蛋白的转化方法。将小鼠单次腹腔内给予 APAP(0-350 mg/kg bw),然后收集 24 小时尿液。APAP 剂量≥275 mg/kg bw 导致肝中央小叶坏死,并显著升高血浆丙氨酸氨基转移酶(ALT)值(p<0.0001)。蛋白质组学分析鉴定出急性肝损伤小鼠尿液中 12 种差异表达的蛋白质(p<0.001),包括超氧化物歧化酶 1(SOD1)、碳酸酐酶 3(CA3)和钙调蛋白(CaM),它们是 APAP 诱导肝损伤的新型生物标志物。SOD1 和 CA3 的尿水平随血浆 ALT 水平升高而升高,但在给予高剂量 APAP 而无血浆 ALT 水平升高的小鼠中,已存在尿 CaM。重要的是,我们在 APAP 中毒后的人类尿液中发现了 SOD1 和 CA3,而在对照尿液样本中则没有这两种蛋白质。在人类 APAP 中毒者中,CaM 的尿浓度显著升高,与血浆 APAP 浓度呈良好相关(r=0.97;p<0.0001),而这些患者的血浆 ALT 水平并未升高。总之,使用这种尿液蛋白质组学方法,我们证明 CA3、SOD1 以及最重要的 CaM 是潜在的人类 APAP 诱导肝损伤生物标志物。