Hepatocellular carcinoma (HCC) is one of the most common cancers and a leading cause of death worldwide. Increased thioredoxin reductase (TrxR) levels were recently identified as possible prognostic markers for HCC. Here, four gold(III) complexes 1b-4b bearing Schiff base ligands were synthesized, characterized, and screened for antitumor activity against HCC. All complexes triggered significant antiproliferative effects against HCC cells, especially the most active complex 1b induced HepG2 cells apoptosis by activating the endoplasmic reticulum stress (ERS). 1b could clearly inhibit the TrxR enzyme activity to elevate reactive oxygen species (ROS), mediate ERS and lead to mitochondrial dysfunction. Notably, treatment of 1b improved the CCl₄-induced liver damage in vivo by down-regulation of TrxR expression and inflammation level.

肝细胞癌（HCC）是世界上最常见的癌症之一，也是主要的死亡原因。硫氧还蛋白还原酶（TrxR）水平的增加最近被确定为可能的肝癌预后标志物。在这里，合成，表征和筛选针对HCC的抗肿瘤活性的四个带有Schiff碱配体的金（III）配合物1b-4b。所有复合物均通过激活内质网应激（ERS）引发了对HCC细胞的显着抗增殖作用，尤其是活性最高的复合物1b诱导的HepG2细胞凋亡。1b可以明显抑制TrxR酶的活性，从而提高活性氧（ROS），介导ERS并导致线粒体功能障碍。值得注意的是，治疗1b通过下调TrxR表达和炎症水平改善了体内CCl ₄诱导的肝损伤。