Zhai R F, Liu Q
Department of Critical Care Medicine, The Second Affiliated Hospital, Hengyang Medical School, University of South China, Hengyang City, Hunan Province, China.
J Physiol Pharmacol. 2024 Oct;75(5). doi: 10.26402/jpp.2024.5.07. Epub 2024 Dec 4.
Baicalin, a predominant bioactive flavonoid derived from the traditional Chinese medicinal herb Scutellaria baicalensis Georgi, has garnered significant attention. Ferroptosis, a relatively novel form of programmed cell death, implicates critical signaling pathways, notably those involving nuclear factor E2-related factor 2 (Nrf2) and glutathione peroxidase 4 (Gpx4). Consequently, this study aims is to elucidate whether baicalin mitigates intestinal tissue damage by modulating the Nrf2-Gpx4 signaling pathway in the context of intestinal ischemia-reperfusion (II/R) injury, thereby influencing iron deposition. For this purpose it was established an II/R rat model and a cellular hypoxia-glucose deficiency/reoxygenation (OGD/R) model and administered BA to the II/R rats and OGD/R model cells. It was utilized HE staining and probe staining techniques to assess intestinal injury and iron overload, respectively and employed RT-qPCR to measure the mRNA expression levels of inflammation-related genes (interleukin-1β, interferon-γ, interleukin-4, and interleukin-10) and iron deficiency-related genes (Nrf2, Gpx4, and xCT). The cell counting kit-8 (CCK-8) assay is employed to assess cell viability, while fluorescent probes are utilized to evaluate mitochondrial membrane potential. Colorimetric methods are applied to quantify intracellular oxidative stress-related indicators (reactive oxygen species (ROS) and malondialdehyde (MDA)) levels. Flow cytometry is used to determine cell membrane lipid ROS levels. Immunofluorescence techniques are implemented to examine intestinal tight junction proteins, such as ZO-1 and Occludin. Additionally, protein immunoblotting is conducted to measure markers of iron deposition (Gpx4 and xCT). In in vivo studies, BA treatment mitigated intestinal damage in II/R rats, inhibited intestinal iron ion overload, and elevated inflammatory levels and oxidative stress. Furthermore, BA treatment reduced the loss of tight junction proteins ZO-1 and Occludin expression levels induced by II/R. In vitro studies demonstrated that BA significantly attenuated OGD/R-induced iron overload, decreased cell viability, and mitigated mitochondrial membrane potential loss. Mechanistically, BA exerts its protective effect against iron overload-induced cellular damage by activating the Nrf2-Gpx4 signaling pathway. However, these effect was significantly counteracted by the use of Nrf2-GPX4 pathway inhibitors. The positive regulation of Nrf2-Gpx4 by BA can reduce ferroptosis and alleviate II/R in rats.
黄芩苷是一种从传统中药黄芩中提取的主要生物活性黄酮类化合物,已受到广泛关注。铁死亡是一种相对较新的程序性细胞死亡形式,涉及关键信号通路,尤其是那些涉及核因子E2相关因子2(Nrf2)和谷胱甘肽过氧化物酶4(Gpx4)的信号通路。因此,本研究旨在阐明黄芩苷是否通过在肠道缺血再灌注(II/R)损伤的情况下调节Nrf2-Gpx4信号通路来减轻肠道组织损伤,从而影响铁沉积。为此,建立了II/R大鼠模型和细胞缺氧缺糖/复氧(OGD/R)模型,并将黄芩苷给予II/R大鼠和OGD/R模型细胞。分别利用苏木精-伊红(HE)染色和探针染色技术评估肠道损伤和铁过载,并采用逆转录定量聚合酶链反应(RT-qPCR)检测炎症相关基因(白细胞介素-1β、干扰素-γ、白细胞介素-4和白细胞介素-10)和铁缺乏相关基因(Nrf2、Gpx4和xCT)的mRNA表达水平。采用细胞计数试剂盒-8(CCK-8)法评估细胞活力,同时利用荧光探针评估线粒体膜电位。采用比色法定量细胞内氧化应激相关指标(活性氧(ROS)和丙二醛(MDA))水平。流式细胞术用于测定细胞膜脂质ROS水平。采用免疫荧光技术检测肠道紧密连接蛋白,如闭合蛋白(ZO-1)和闭锁蛋白(Occludin)。此外,进行蛋白质免疫印迹以检测铁沉积标记物(Gpx4和xCT)。在体内研究中,黄芩苷治疗减轻了II/R大鼠的肠道损伤,抑制了肠道铁离子过载,并提高了炎症水平和氧化应激。此外,黄芩苷治疗减少了II/R诱导的紧密连接蛋白ZO-1和Occludin表达水平的丧失。体外研究表明,黄芩苷显著减轻了OGD/R诱导的铁过载,降低了细胞活力,并减轻了线粒体膜电位丧失。机制上,黄芩苷通过激活Nrf2-Gpx4信号通路对铁过载诱导的细胞损伤发挥保护作用。然而,使用Nrf2-GPX4通路抑制剂可显著抵消这些作用。黄芩苷对Nrf2-Gpx4的正向调节可减少铁死亡并减轻大鼠的II/R。