Department of Drug Safety Sciences, Division of Clinical Pharmacology, Nagoya University Graduate School of Medicine, Nagoya, Japan.
Department of Pathology and Laboratory Medicine, Institute of Biomedical Sciences, Tokushima University Graduate School, Tokushima, Japan.
Lab Invest. 2017 Jul;97(7):833-842. doi: 10.1038/labinvest.2017.22. Epub 2017 Mar 6.
Drug-induced liver injury (DILI) is a major concern in drug development and clinical drug therapy. Since the underlying mechanisms of DILI have not been fully understood in most cases, elucidation of the hepatotoxic mechanisms of drugs is expected. Although enalapril (ELP), an angiotensin-converting enzyme inhibitor, has been reported to cause liver injuries with a low incidence in humans, the precise mechanisms by which ELP causes liver injury remains unknown. In this study, we established a mouse model of ELP-induced liver injury and analyzed the mechanisms of its hepatotoxicity. Mice that were administered ELP alone did not develop liver injury, and mice that were pretreated with a synthetic glucocorticoid dexamethasone (DEX) and a glutathione synthesis inhibitor l-buthionine-(S,R)-sulfoximine (BSO) exhibited liver steatosis without significant increase in plasma alanine aminotransferase (ALT). In mice pretreated with DEX and BSO, ALT levels were significantly increased after ELP administration, suggesting that hepatic steatosis sensitized the liver to ELP hepatotoxicity. An immunohistochemical analysis showed that the numbers of myeloperoxidase-positive cells that infiltrated the liver were significantly increased in the mice administered DEX/BSO/ELP. The levels of oxidative stress-related factors, including hepatic heme oxygenase-1, serum hydrogen peroxide and hepatic malondialdehyde, were elevated in the mice administered DEX/BSO/ELP. The involvement of oxidative stress in ELP-induced liver injury was further supported by the observation that tempol, an antioxidant agent, ameliorated ELP-induced liver injury. In conclusion, we successfully established a model of ELP-induced liver injury in DEX-treated steatotic mice and demonstrated that oxidative stress and neutrophil infiltration are involved in the pathogenesis of ELP-induced liver injury.
药物性肝损伤(DILI)是药物开发和临床药物治疗中的一个主要关注点。由于在大多数情况下尚未完全了解 DILI 的潜在机制,因此人们期望阐明药物的肝毒性机制。虽然血管紧张素转换酶抑制剂依那普利(ELP)已被报道在人类中引起低发生率的肝损伤,但 ELP 引起肝损伤的确切机制仍不清楚。在这项研究中,我们建立了 ELP 诱导的肝损伤小鼠模型,并分析了其肝毒性的机制。单独给予 ELP 的小鼠未发生肝损伤,而预先用合成糖皮质激素地塞米松(DEX)和谷胱甘肽合成抑制剂 L-丁硫氨酸-(S,R)-亚砜(BSO)预处理的小鼠则表现出肝脂肪变性,而血浆丙氨酸氨基转移酶(ALT)没有明显升高。在预先用 DEX 和 BSO 预处理的小鼠中,给予 ELP 后 ALT 水平显着升高,表明肝脂肪变性使肝脏对 ELP 肝毒性敏感。免疫组织化学分析显示,给予 DEX/BSO/ELP 的小鼠肝脏中浸润的髓过氧化物酶阳性细胞数量显着增加。给予 DEX/BSO/ELP 的小鼠肝组织血红素加氧酶-1、血清过氧化氢和肝丙二醛等氧化应激相关因子的水平升高。抗氧化剂替米洛尔改善 ELP 诱导的肝损伤的观察结果进一步支持了氧化应激参与 ELP 诱导的肝损伤。总之,我们成功地在 DEX 处理的脂肪变性小鼠中建立了 ELP 诱导的肝损伤模型,并证明氧化应激和中性粒细胞浸润参与了 ELP 诱导的肝损伤的发病机制。