Anti-cancer and Other Health-Promoting Effects of Silibinin and Silibinin Derivatives 2023

Dear Colleagues, 

The flavonolignan silibinin (or silybin) is considered the major bioactive component of silymarin, an extract of Silybum marianum (milk thistle) seeds that was classified by the World Health Organization in the 1970s as official medicine with health-promoting properties. The well-known hepatoprotective, anti-inflammatory, and anti-fibrotic effects of silibinin have supported the therapeutic use of silymarin for the treatment of liver illnesses such as alcoholic liver disease, nonalcoholic liver disease, drug-induced liver injury, cirrhosis, viral hepatitis, and mushroom poisoning in the last 50 years.  

In the last decade, an ever-growing number of preclinical studies have illuminated the potential anti-cancer effects of silibinin. Silibinin has been shown to exert significant tumoricidal activity against cultured cancer cells and xenografts, to enhance the efficacy of other anti-cancer therapeutic agents, to reduce the toxicity of cancer treatments, and to prevent and overcome the emergence of cancer drug resistance. However, the achievement of a bona fide, clinically relevant anti-cancer activity of silibinin remains controversial in human trials. Thus, whereas no significant anti-tumor activity of silibinin has been reported in prostate cancer tissues, certain silibinin-containing formulations have been successfully applied to lung cancer patients with established brain metastases, providing highly significant survival advantages, low toxicity and reversible secondary effects, and compatibility with the standard of care.  

To encompass the remarkable breadth of ongoing investigation on silibinin and cancer, research articles, review articles, as well as short communications covering a wide range of topics related to the therapeutic application of silibinin as an anti-cancer treatment, including but not exclusive to molecular mechanisms, signaling pathways, metabolism, preclinical studies, drug formulations, analogues, drug combinations, immune response, and clinical trials are welcomed for inclusion in this Special Issue of Pharmaceuticals. 

Dr. Elisabet Cuyàs
Dr. Javier A. Menendez
Dr. Joaquim Bosch-Barrera
Guest Editors

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• molecular mechanisms of action
• cellular mechanisms of action
• metabolism and bioavailability
• drug development
• analogs
• preclinical studies
• metastasis
• immune system
• clinical trials
• epidemiology