Colin Ratledge Center of Microbial Lipids, Shandong University of Technology, School of Agriculture Engineering and Food Science, Zibo 255000, China.
Department of Botany and Microbiology, Faculty of Science, Al-Azhar University, Assiut 71524, Egypt.
Biomed Res Int. 2020 Oct 14;2020:8256809. doi: 10.1155/2020/8256809. eCollection 2020.
Human liver cancer has emerged as a serious health concern in the world, associated with poorly available therapies. The genus contains vital medicinal plants with miraculous healing properties and a wide range of bioactivities. In this study, different crude extracts of Royle were prepared and screened against Human Hepatocarcinoma (HepG2) cell lines. The water/ethanolic extract of Royle (BLE) exhibited significant antiproliferative activity against the HepG2 cancer cell line with an IC value of 47 g/mL. The extract decreased the clonogenic potential of HepG2 cells in a dose-dependent manner. It induced apoptotic cell death in HepG2 cells that were confirmed by cytometric analysis and microscopic examination of cellular morphology through DAPI-stained cells. Biochemical evidence of apoptosis came from elevating the intracellular ROS level that was accompanied by the loss of mitochondrial membrane potential. The mechanism of apoptosis was further confirmed by gene expression analysis using RT-qPCR that revealed the decline in Bcl-2 independent of p53 mRNA and a rise in CDK1 while downregulating CDK5, CDK9, and CDK10 mRNA levels at 48 h of BLE treatment. The most active fraction was subjected to HPLC which indicated the presence of berberine (48 g/mL) and benzoic acid (15.8 g/mL) as major compounds in BLE and a trace amount of luteolin, rutin, and gallic acid. Our study highlighted the importance of the most active BLE extract as an excellent source of nutraceuticals against Human Hepatocarcinoma that can serve as an herbal natural cure against liver cancer.
人肝癌已成为全球严重的健康问题，相关治疗方法有限。该属植物含有具有神奇治疗特性和广泛生物活性的重要药用植物。在这项研究中，我们制备了 Royle 的不同粗提取物并对人肝癌（HepG2）细胞系进行了筛选。Royle 的水/乙醇提取物（BLE）对 HepG2 癌细胞系表现出显著的抗增殖活性，IC 值为 47μg/mL。该提取物以剂量依赖性方式降低 HepG2 细胞的集落形成能力。它在 HepG2 细胞中诱导凋亡细胞死亡，这通过流式细胞术分析和通过 DAPI 染色细胞的细胞形态学的显微镜检查得到证实。凋亡的生化证据来自于升高细胞内 ROS 水平，伴随着线粒体膜电位的丧失。通过 RT-qPCR 的基因表达分析进一步证实了凋亡机制，该分析显示 Bcl-2 依赖性 p53 mRNA 的下降以及 CDK1 的增加，同时下调 BLE 处理 48 小时时的 CDK5、CDK9 和 CDK10 mRNA 水平。最活跃的馏分通过 HPLC 进行分析，表明 BLE 中存在小檗碱（48μg/mL）和苯甲酸（15.8μg/mL）作为主要化合物，以及芦丁、芸香苷和没食子酸的痕量。我们的研究强调了最活跃的 BLE 提取物作为针对人肝癌的极好的营养保健品来源的重要性，它可以作为治疗肝癌的天然草药疗法。
