Dai Wen-Zhang, Bai Zhao-Fang, He Ting-Ting, Zhan Xiao-Yan, Li Qiang, Zhao Jing, Xiao Xiao-He
School of Pharmacy, Hunan University of Chinese Medicine Changsha 410208, China Department of Hepatology, the Fifth Medical Center of Chinese PLA General Hospital Beijing 100039, China.
Department of Hepatology, the Fifth Medical Center of Chinese PLA General Hospital Beijing 100039, China.
Zhongguo Zhong Yao Za Zhi. 2022 Oct;47(19):5299-5305. doi: 10.19540/j.cnki.cjcmm.20220421.704.
Excess acetaminophen(APAP) can be converted by the cytochrome P450 system to the toxic metabolite N-acetyl-p-benzoquinoneimine(NAPQI), which consumes glutathione(GSH). When GSH is depleted, NAPQI covalently binds with proteins, inducing mitochondrial dysfunction and oxidative stress and thereby leading to hepatotoxicity. Schisandrin C(SinC) is a dibenzocyclooctadiene derivative isolated from Schisandra chinensis. Although there is some evidence showing that SinC has hepatoprotective activity, its protective effect and mechanism on APAP-induced liver injury remain unclear. In this paper, an acute liver injury mouse model was established by intraperitoneal injection of APAP at a dose of 400 mg·kg~(-1) to evaluate the effect of SinC administration on the APAP-induced liver injury and its mechanism through an animal experiment. At the same time, a potential candidate drug was provi-ded for traditional Chinese medicine(TCM) prevention and treatment of overdose APAP-induced liver injury. In the APAP-induced liver injury mouse model, we found that SinC can relieve hepatic histopathological lesions and significantly reduce the activities of alanine aminotransferase(ALT), aspartate aminotransferase(AST) and alkaline phosphatase(ALP). It was also capable of increasing the content of GSH and superoxide dismutase(SOD) and decreasing the levels of total bilirubin(TBIL), direct bilirubin(DBIL), malondialdehyde(MDA), interleukin-6(IL-6) and tumor necrosis factor-α(TNF-α). Further analysis showed that SinC decreased the content of CYP2 E1 in liver tissues at protein and mRNA levels and increased nuclear factor erythroid 2-related factor 2(Nrf2) and the expression of its downstream targets(including HO-1, NQO1 and GCLC). Taken together, the above results indicate that SinC can alleviate APAP-induced liver injury by reducing the expression of CYP2 E1, suppressing apoptosis, improving inflammatory response and activating the Nrf2 signaling pathway to inhibit oxidative stress.
过量的对乙酰氨基酚(APAP)可被细胞色素P450系统转化为有毒代谢产物N-乙酰对苯醌亚胺(NAPQI),后者会消耗谷胱甘肽(GSH)。当GSH耗尽时,NAPQI会与蛋白质共价结合,诱导线粒体功能障碍和氧化应激,从而导致肝毒性。五味子醇甲(SinC)是从五味子中分离出的一种二苯并环辛二烯衍生物。虽然有一些证据表明SinC具有肝保护活性,但其对APAP诱导的肝损伤的保护作用及机制仍不清楚。本文通过腹腔注射400 mg·kg⁻¹剂量的APAP建立急性肝损伤小鼠模型,通过动物实验评估给予SinC对APAP诱导的肝损伤的影响及其机制。同时,为中药预防和治疗过量APAP诱导的肝损伤提供了一种潜在的候选药物。在APAP诱导的肝损伤小鼠模型中,我们发现SinC可减轻肝脏组织病理学损伤,并显著降低丙氨酸转氨酶(ALT)、天冬氨酸转氨酶(AST)和碱性磷酸酶(ALP)的活性。它还能够增加GSH和超氧化物歧化酶(SOD)的含量,并降低总胆红素(TBIL)、直接胆红素(DBIL)、丙二醛(MDA)、白细胞介素-6(IL-6)和肿瘤坏死因子-α(TNF-α)的水平。进一步分析表明,SinC在蛋白质和mRNA水平上降低了肝脏组织中CYP2E1的含量,并增加了核因子红细胞2相关因子2(Nrf2)及其下游靶点(包括HO-1、NQO1和GCLC)的表达。综上所述,上述结果表明SinC可通过降低CYP2E1的表达、抑制细胞凋亡、改善炎症反应和激活Nrf2信号通路以抑制氧化应激来减轻APAP诱导的肝损伤。