Selc Michal, Jakic Kristina, Macova Radka, Babelova Andrea
Centre for Advanced Material Application, Slovak Academy of Sciences, Bratislava, Slovakia.
Department of Nanobiology, Cancer Research Institute, Biomedical Research Center, Slovak Academy of Sciences, Bratislava, Slovakia.
Discov Oncol. 2025 Aug 8;16(1):1502. doi: 10.1007/s12672-025-03380-8.
Silybum marianum (milk thistle) is a plant for centuries well known for its hepatoprotective effects. The extract from seeds, silymarin, and its major compound, silibinin, are well studied for their hepatoprotective and antifibrotic effects. The role of other minor compounds, such as isosilybin B, remains underexplored.
This study aimed to compare the cytotoxic and antifibrotic properties of IB with those of silibinin and silymarin in vitro. It focuses on evaluating the cytotoxic effect of these substances on tumor and non-tumor liver cells. Moreover, antifibrotic potential of the three substances was determined in healthy liver cells treated with TGF-β1.
Isosilybin B exhibits greater cytotoxicity toward liver cancer cells while being less toxic to non-tumor hepatocytes compared to silibinin. At non-toxic concentrations, isosilybin B induced cell cycle arrest at the G1 phase in two types of liver cancer cells. In contrast, it did not impact the cell cycle of non-tumor cells under the same experimental conditions. In the model of liver fibrosis in vitro induced by TGF-β1, isosilybin B reduced the mRNA expression of pro-fibrotic genes as well as ALT level in the culture medium more effectively than silibinin.
Obtained results suggest that isosilybin B represents a promising anticancer agent for the treatment of liver cancer. Moreover, its anti-fibrotic properties emphasize its potential for treatment of many other liver diseases, which underline the strong potential of isosilybin B in future anticancer and antifibrotic therapeutic strategies.
水飞蓟是一种几个世纪以来因其肝脏保护作用而闻名的植物。种子提取物水飞蓟素及其主要化合物水飞蓟宾的肝脏保护和抗纤维化作用已得到充分研究。其他次要化合物,如异水飞蓟宾B的作用仍未得到充分探索。
本研究旨在比较异水飞蓟宾B与水飞蓟宾和水飞蓟素在体外的细胞毒性和抗纤维化特性。重点评估这些物质对肿瘤和非肿瘤肝细胞的细胞毒性作用。此外,在经转化生长因子-β1处理的健康肝细胞中测定了这三种物质的抗纤维化潜力。
与水飞蓟宾相比,异水飞蓟宾B对肝癌细胞表现出更大的细胞毒性,而对非肿瘤肝细胞的毒性较小。在无毒浓度下,异水飞蓟宾B诱导两种肝癌细胞的细胞周期停滞在G1期。相比之下,在相同实验条件下,它对非肿瘤细胞的细胞周期没有影响。在由转化生长因子-β1诱导的体外肝纤维化模型中,异水飞蓟宾B比水飞蓟宾更有效地降低了促纤维化基因的mRNA表达以及培养基中的谷丙转氨酶水平。
所得结果表明,异水飞蓟宾B是一种有前途的治疗肝癌的抗癌药物。此外,其抗纤维化特性突出了其治疗许多其他肝脏疾病的潜力,这强调了异水飞蓟宾B在未来抗癌和抗纤维化治疗策略中的强大潜力。