Lu Xiaodan, Liu Fuyao, Chen Hongming, Cai Haojie, Zhang Lei, Li Jing
MOE International Joint Research Laboratory on Synthetic Biology and Medicines, School of Biology and Biological Engineering, South China University of Technology, Guangzhou, China.
J Appl Toxicol. 2025 Mar;45(3):418-431. doi: 10.1002/jat.4710. Epub 2024 Oct 22.
Hyperuricemia, a prevalent condition, is typically preceded by disturbances in purine metabolism and is frequently associated with hyperlipidemia and other dysfunctions of metabolism. WN1703 demonstrated an inhibitory activity against xanthine oxidoreductase (XOR) that was comparable to febuxostat in our prior investigation. In this study, we assessed the cardiovascular safety of WN1703 in a chronic hyperuricemia rat model induced by potassium oxonate in combination with hypoxanthine. We investigated the changes in cardiovascular biomarkers in chronic hyperuricemia rats treated with febuxostat and WN1703, including creatine kinase (CK), CK-MB, B type natriuretic peptide (BNP), Corin protein (CRN), Neprilysin (NEP), myeloperoxidase (MPO), 8-hydroxy-2-deoxyguanosine (8-OHdG), tumor necrosis factor (TNF-α), interleukin-1β (IL-1β), and interleukin-8 (IL-8). Additionally, we validated the potential mechanism of cardiac injury induced by WN1703 in H9C2 cells, guided by cardiotoxicity predictions from the cardioToxCSM database and network pharmacology. We observed that excessively rapid urate-lowering, oxidative stress, and inflammation could disrupt myocardial functional homeostasis and increase the risk of cardiovascular injury in hyperuricemia rats, and WN1703 treatment effectively reduced the levels oxidative stress marker 8-OHdG and inflammatory factor TNF-α. Despite the absence of organic damage to the heart with prolonged treatment of febuxostat and WN1703, potential hazard of cardiovascular injury could be associated with the modulation of the TGFβ and RHO/ROCK signaling pathways by febuxostat and WN1703. This could offer new insights into the mechanisms underlying the adverse effects caused by XOR inhibitors.
高尿酸血症是一种常见病症,通常在嘌呤代谢紊乱之前出现,并且常与高脂血症及其他代谢功能障碍相关。在我们之前的研究中,WN1703表现出对黄嘌呤氧化还原酶(XOR)的抑制活性,与非布司他相当。在本研究中,我们在氧嗪酸钾联合次黄嘌呤诱导的慢性高尿酸血症大鼠模型中评估了WN1703的心血管安全性。我们研究了用非布司他和WN1703治疗的慢性高尿酸血症大鼠心血管生物标志物的变化,包括肌酸激酶(CK)、肌酸激酶同工酶MB(CK-MB)、B型利钠肽(BNP)、Corin蛋白(CRN)、中性肽链内切酶(NEP)、髓过氧化物酶(MPO)、8-羟基-2'-脱氧鸟苷(8-OHdG)、肿瘤坏死因子(TNF-α)、白细胞介素-1β(IL-1β)和白细胞介素-8(IL-8)。此外,在cardioToxCSM数据库和网络药理学的心脏毒性预测指导下,我们在H9C2细胞中验证了WN1703诱导心脏损伤的潜在机制。我们观察到,尿酸降低过快、氧化应激和炎症会破坏高尿酸血症大鼠的心肌功能稳态并增加心血管损伤风险,而WN1703治疗有效降低了氧化应激标志物8-OHdG和炎症因子TNF-α的水平。尽管长期使用非布司他和WN1703对心脏没有器质性损伤,但心血管损伤的潜在风险可能与非布司他和WN1703对TGFβ和RHO/ROCK信号通路的调节有关。这可能为XOR抑制剂引起不良反应的潜在机制提供新的见解。