In the last few decades, targeting cancer by the use of dietary phytochemicals has gained enormous attention. The plausible reason and believe or mind set behind this fact is attributed to either lesser or no side effects of natural compounds as compared to the modern chemotherapeutics, or due to their conventional use as dietary components by mankind for thousands of years. Silibinin is a naturally derived polyphenol (a flavonolignans), possess following biochemical features; molecular formula C₂₅H₂₂O₁₀, Molar mass: 482.44 g/mol, Boiling point 793 °C, with strikingly high antioxidant and anti-tumorigenic properties. The anti-cancer properties of Silibinin are determined by a variety of cellular pathways which include induction of apoptosis, cell cycle arrest, inhibition of angiogenesis and metastasis. In addition, Silibinin controls modulation of the expression of aberrant miRNAs, inflammatory response, and synergism with existing anti-cancer drugs. Therefore, modulation of a vast array of cellular responses and homeostatic aspects makes Silibinin an attractive chemotherapeutic agent. However, like other polyphenols, the major hurdle to declare Silibinin a translational chemotherapeutic agent, is its lesser bioavailability. After summarizing the chemistry and metabolic aspects of Silibinin, this extensive review focuses on functional aspects governed by Silibinin in chemoprevention with an ultimate goal of summarizing the evidence supporting the chemopreventive potential of Silibinin and clinical trials that are currently ongoing, at a single platform.

在过去的几十年里，通过使用膳食植物化学物质来靶向癌症已经引起了极大的关注。这一事实背后的合理原因和信念或思维定势归因于与现代化学疗法相比，天然化合物的副作用较小或没有副作用，或者归因于人类数千年来将其作为饮食成分的常规用途。水飞蓟宾是一种天然衍生的多酚（一种黄酮木脂素），具有以下生化特征；分子式 C ₂₅ H ₂₂ O ₁₀, 摩尔质量：482.44 g/mol，沸点 793 °C，具有非常高的抗氧化和抗肿瘤特性。水飞蓟宾的抗癌特性由多种细胞途径决定，包括诱导细胞凋亡、细胞周期停滞、抑制血管生成和转移。此外，水飞蓟宾控制异常 miRNA 表达的调节、炎症反应以及与现有抗癌药物的协同作用。因此，大量细胞反应和稳态方面的调节使水飞蓟宾成为一种有吸引力的化学治疗剂。然而，与其他多酚一样，将水飞蓟宾宣布为转化化学治疗剂的主要障碍是其较低的生物利用度。在总结了水飞蓟宾的化学和代谢方面，