Department of Cardiology, Nanjing Lishui People's Hospital, Zhongda Hospital Lishui Branch, Southeast University, Nanjing, 211200, China.
Department of Cardiology, The Second Affiliated Hospital of Guangxi Medical University, Nanning, 530007, Guangxi Zhuang Autonomous Region, China.
Naunyn Schmiedebergs Arch Pharmacol. 2019 Sep;392(9):1121-1130. doi: 10.1007/s00210-019-01661-y. Epub 2019 May 9.
It has been found that use of drugs which upregulate the PI3K/Akt pathway can effectively reduce cardiomyocyte apoptosis which has been induced by coronary microembolization (CME). However, whether this functional protein is able to be modified through pretreatment via nobiletin (NOB) in models of CME has not yet been investigated. Therefore, this study set out to explore the cardioprotective effect of NOB on rats with myocardial injuries induced by CME and also explored the potential mechanism which underlies this cardioprotective effect. The study used 40 Sprague-Dawley (SD) rats, which were randomized into four groups: the sham, CME, CME+NOB, and CME+NOB+LY294002 (LY) groups. Twelve hours after surgery, levels of microinfarct, serum c-troponin I (cTnI), cardiac function, apoptotic index, and oxidative stress [superoxide dismutase (SOD) and malondialdehyde (MDA)] were measured for rats in each group. Western blot analysis was performed to detect any protein involved in the PI3K/Akt pathway. Nobiletin improved cardiac dysfunction which had been induced by CME, decreased serum level of cTnI and MDA, and increased serum SOD activities. In addition, nobiletin inhibited myocardial apoptosis, which may be connected to downregulated apoptotic index, upregulated Bcl-2, and cleaved caspase-3 and Bax, while it increased protein levels in phosphorylated Akt. However, when nobiletin was co-administered with LY294002, a PI3K (phosphatidylinositol 3-kinase)/Akt inhibitor, all of the previously mentioned effects were blocked. Nobiletin is able to inhibit cardiomyocyte apoptosis and can consequently attenuate CME-induced myocardial injuries. These functions are realized through the activation of the PI3K/Akt signaling pathway as well as by reducing oxidative stress.
现已发现,使用上调 PI3K/Akt 通路的药物可有效减少冠状动脉微栓塞 (CME) 诱导的心肌细胞凋亡。然而,尚未研究过这种功能蛋白是否可以通过预处理来改变 CME 模型中的诺比汀 (NOB)。因此,本研究旨在探讨 NOB 对 CME 诱导的心肌损伤大鼠的心脏保护作用,并探讨其潜在机制。该研究使用 40 只 Sprague-Dawley (SD) 大鼠,将其随机分为四组:假手术组、CME 组、CME+NOB 组和 CME+NOB+LY294002 (LY) 组。手术后 12 小时,测量每组大鼠的微梗死面积、血清 c-肌钙蛋白 I (cTnI)、心功能、细胞凋亡指数和氧化应激 [超氧化物歧化酶 (SOD) 和丙二醛 (MDA)]。通过 Western blot 分析检测参与 PI3K/Akt 通路的蛋白质。诺比汀改善了 CME 引起的心脏功能障碍,降低了血清 cTnI 和 MDA 水平,提高了血清 SOD 活性。此外,诺比汀抑制心肌细胞凋亡,可能与凋亡指数下调、Bcl-2 上调和 cleaved caspase-3 和 Bax 下调有关,同时上调磷酸化 Akt 蛋白水平。然而,当诺比汀与 PI3K (phosphatidylinositol 3-kinase)/Akt 抑制剂 LY294002 合用时,上述所有作用均被阻断。诺比汀能够抑制心肌细胞凋亡,从而减轻 CME 诱导的心肌损伤。这些功能是通过激活 PI3K/Akt 信号通路和减少氧化应激来实现的。