Rumex japonicus Houtt (RJH) is a valuable plant used in traditional medicine to treat several diseases, such as scabies and jaundice. In this study, Jurkat cell growth inhibitory extracts of R. japonicus roots were subjected to bioassay-guided fractionation, resulting in the isolation of three naphthalene derivatives (3-5) along with one anthraquinone (6) and two phenolic compounds (1 and 2). Among these compounds, 2-methoxystypandrone (5) exhibited potent anti-proliferative effects on Jurkat cells. Analysis by flow cytometry confirmed that 2-methoxystypandrone (5) could significantly reduce mitochondrial membrane potential and promote increased levels of mitochondrial reactive oxygen species (ROS), suggesting a strong mitochondrial depolarization effect. Real-time quantitative polymerase chain reaction (qPCR) analysis was also performed, and the results revealed that the accumulation of ROS was caused by reduced mRNA expression levels of heme oxygenase (HO-1), catalase (CAT), glutathione peroxidase (GPx), and superoxide dismutase (SOD). In addition, 2-methoxystypandrone (5) triggered strong apoptosis that was mediated by the arrest of the G0/G1 phase of the cell cycle. Furthermore, 2-methoxystypandrone (5) downregulated p-IκB-α, p-NF-κB p65, Bcl₂, and Bcl-xl and upregulated BAX proteins. Taken together, these findings revealed that 2-methoxystypandrone (5) isolated from RJH could potentially serve as an early lead compound for leukemia treatment involving intracellular signaling by increasing mitochondrial ROS and exerting anti-proliferative effects.

中文翻译：

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羊蹄根活性成分通过诱导线粒体损伤和细胞凋亡抑制 Jurkat T 细胞增殖 1。

Rumex japonicus Houtt (RJH) 是一种有价值的植物，在传统医学中用于治疗多种疾病，例如疥疮和黄疸病。在这项研究中，对刺参根的Jurkat 细胞生长抑制提取物进行了生物测定引导的分级分离，从而分离出三种萘衍生物 ( 3-5 ) 以及一种蒽醌 (6) 和两种酚类化合物 ( 1和2 ) ). 在这些化合物中，2-methoxystypandrone ( 5 ) 对 Jurkat 细胞表现出有效的抗增殖作用。流式细胞术分析证实 2-methoxystypandrone ( 5) 可显着降低线粒体膜电位并促进线粒体活性氧 (ROS) 水平升高，表明线粒体具有很强的去极化作用。还进行了实时定量聚合酶链反应 (qPCR) 分析，结果表明 ROS 的积累是由血红素加氧酶 (HO-1)、过氧化氢酶 (CAT)、谷胱甘肽过氧化物酶 (GPx) 的 mRNA 表达水平降低引起的和超氧化物歧化酶 (SOD)。此外，2-methoxystypandrone ( 5 ) 触发了由细胞周期的 G0/G1 期停滞介导的强烈细胞凋亡。此外，2-methoxystypandrone ( 5 ) 下调 p-IκB-α、p-NF-κB p65、Bcl ₂和 Bcl-xl 并上调 BAX 蛋白。综上所述，这些发现表明，从 RJH 中分离出的 2-methoxystypandrone ( 5 ) 可能作为白血病治疗的早期先导化合物，涉及通过增加线粒体 ROS 和发挥抗增殖作用而进行的细胞内信号传导。