Many cancer cells critically rely on antioxidant systems for cell survival and are vulnerable to further oxidative impairment triggered by agents generating reactive oxygen species (ROS). Therefore, the classical design and development of inhibitors that target antioxidant defense enzymes such as thioredoxin reductase (TrxR) can be a promising anticancer strategy. Herein, it is shown that a gold(I) complex containing an oleanolic acid derivative (4 b ) induces apoptosis of ovarian cancer A2780 cells by activating endoplasmic reticulum stress (ERS). It can inhibit TrxR enzyme activity to elevate ROS, mediate ERS and mitochondrial dysfunction, and finally leads to cell cycle arrest and apoptosis of A2780 cells. Notably, this complex inhibits A2780 xenograft tumor growth accompanied by increased ERS level and decreased TrxR activity in tumor tissues.

中文翻译：

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通过抑制TrxR和激活ROS介导的ERS，含有齐墩果酸衍生物作为潜在抗卵巢癌药物的Gold（I）配合物。

许多癌细胞严重依赖抗氧化剂系统来维持细胞存活，并且易受产生活性氧（ROS）的试剂触发的进一步氧化损伤的影响。因此，针对抗氧化防御酶（如硫氧还蛋白还原酶（TrxR））的抑制剂的经典设计和开发可能是一种有前途的抗癌策略。在此，表明含有齐墩果酸衍生物的金（I）络合物（4b）通过激活内质网应激（ERS）诱导卵巢癌A2780细胞凋亡。它可以抑制TrxR酶的活性以升高ROS，介导ERS和线粒体功能障碍，最终导致A2780细胞的细胞周期停滞和凋亡。值得注意的是，这种复合物抑制了A2780异种移植肿瘤的生长，并伴随着肿瘤组织中ERS水平的提高和TrxR活性的降低。