Chen Min, Wang Xiaodong, Hu B O, Zhou Jian, Wang Xin, Wei Wei, Zhou Hua
Department of Cardiovascular Medicine, Shanghai East Hospital, Tongji University School of Medicine, Shanghai 200120, China.
J Biosci. 2018 Dec;43(5):857-865.
Oxidative stress and apoptosis is involved in hypoxia-reoxygenation (H/R) induced myocardial injury. Increased expression of uncoupling protein 2 (UCP2), a cationic carrier protein, has protective effect against H/R injury. The present study aimed to find candidate drugs for H/R induced cardiac damage by identifying compounds regulating UCP2 expression. Here, among six natural compounds, ursolic acid (UA) had the most significant induction effect on UCP2 expression in H9c2 cells under H/R conditions. Subsequently, we found that UA significantly attenuated cell apoptosis and Caspase 3 activity, but increased nitric oxide (NO) release under H/R conditions. Additionally, UA pretreatment also decreased reactive oxygen species (ROS) production and malondialdehyde (MDA) content, but increased superoxide dismutase (SOD) activity. H/R caused a notable increase in the phosphorylation of p38, which was weakened by UA pretreatment. Moreover, p38 inhibitor (SB203580) showed the similar effects on H/R cells as UA pretreatment, while UCP2 knockdown had the reverse biological effects. More importantly, the effects of UA or p38 inhibitor exposure were partially rescued by UCP2 knockdown. Collectively, our data suggested the functions of UA on UCP2 expression and on the protection of H/Rstimulated H9c2 cells may be attributed to p38 signaling pathway.
氧化应激和细胞凋亡参与了缺氧复氧(H/R)诱导的心肌损伤。解偶联蛋白2(UCP2)是一种阳离子载体蛋白,其表达增加对H/R损伤具有保护作用。本研究旨在通过鉴定调节UCP2表达的化合物来寻找治疗H/R诱导的心脏损伤的候选药物。在此,在六种天然化合物中,熊果酸(UA)在H/R条件下对H9c2细胞中UCP2表达的诱导作用最为显著。随后,我们发现UA显著减轻了细胞凋亡和半胱天冬酶3活性,但在H/R条件下增加了一氧化氮(NO)的释放。此外,UA预处理还降低了活性氧(ROS)的产生和丙二醛(MDA)含量,但增加了超氧化物歧化酶(SOD)活性。H/R导致p38磷酸化显著增加,而UA预处理减弱了这种增加。此外,p38抑制剂(SB203580)对H/R细胞的作用与UA预处理相似,而UCP2基因敲低则产生相反的生物学效应。更重要的是,UCP2基因敲低部分挽救了UA或p38抑制剂处理的效应。总体而言,我们的数据表明UA对UCP2表达以及对H/R刺激的H9c2细胞的保护作用可能归因于p38信号通路。