Anti-cancer Effects of Silibinin: The Current Status in Cancer Chemoprevention

  • Dominique Reed
  • Komal Raina
  • Rajesh AgarwalEmail author


The naturally occurring flavonolignan Silibinin (also known as Silybin) is a bioactive constituent of silymarin isolated from the seeds of the milk thistle plant (Silybum marianum L. Gaernt.), a member of the Asteraceae family. The milk thistle plant is a part of the native vegetation in Southern Europe, Southern Russia, Asia Minor and Northern Africa. This multi-functional flavonolignan possesses strong hepatoprotective, cardioprotective, neuroprotective, immune-modulatory, antidotal and anti-neoplastic properties. To date, over 600 peer-reviewed research reports and limited clinical trials have evaluated the anti-oncogenic efficacy of silibinin to combat tumor growth, angiogenesis, and metastasis. As a promising agent, silibinin mediates a wide-range of potent chemopreventive and anti-cancer activities in several frequently diagnosed epithelial malignancies, including skin, colon, prostate and lung. In addition, several combinatorial anti-cancer strategies of silibinin with other therapeutics exhibit synergistic interactions to suppress drug-induced toxic effects and chemoresistance. In this chapter, the pre-clinical and clinical efficacy of silibinin and/or silymarin derivatives against several cancers will be reviewed. Moreover, the chapter will summarize silibinin effects on key signaling pathways, such as: transforming Growth Factor beta (TGFβ), epidermal growth factor receptor (EGFR), insulin-like growth factor-1 receptor (IGF-1R), and NF-κB (nuclear factor-kappa B), which are crucial to the anti-cancer activity of silibinin in cancer prevention, disease progression/recurrence and reversal of drug resistance.


Silibinin Skin cancer Bladder cancer Colorectal cancer Prostate cancer Non-small lung cancer Cancer stem cells 


Conflict of Interest

Rajesh Agarwal is one of the founders and shareholders of a biotech company ProTechSure Scientific, Inc. that licensed Silibinin from UCD, and developed and marketed (OTC) its skin formulation as Difinsa53.

Grant Support

Supported by NCI R01 grants CA140368 and CA195708 (to RA), R01 grant CA201112 (to KR), and R01 CA195708S (to DR).


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© Springer Nature Switzerland AG 2020

Authors and Affiliations

  1. 1.Department of Pharmaceutical SciencesSkaggs School of Pharmacy and Pharmaceutical Sciences, University of Colorado Anschutz Medical CampusAuroraUSA
  2. 2.Department of Pharmaceutical SciencesSouth Dakota State UniversityBrookingsUSA
  3. 3.University of Colorado Cancer Center, University of Colorado Denver-Anschutz Medical CampusAuroraUSA

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