Silibinin is the main therapeutic constituent of silymarin, which is comprised of a group of flavonoids and flavonolignans.
Silybin is naturally contained in the milk thistle plant (Silybum marianum). Milk thistle has a long history of therapeutic use that dates back to Ancient Greece.
Traditional uses of Silybum marianum include treating disorders of the gallbladder and liver, however it is now used for many more indications.
Milk thistle extract (silymarin) is being studied for anticancer, antidiabetic, anti-inflammatory and cardiovascular-enhancing effects. These studies usually involve using milk thistle as an adjunct therapy to existing conventional treatments.
In sum, silymarin is considered the active ingredient in milk thistle and silibinin is thought to be the most therapeutically useful component in the silymarin complex. Consequently, silibinin is being independently studied for its possible therapeutic effects.



- Supports liver health & detox
- Anti-oxidant & anti-inflammatory properties
- Improves insulin sensitivity & cholesterol
Silymarin and Silibinin: What’s the Difference?
Related Topics
Silymarin was historically extracted from the milk thistle plant.
It now exists as a homogenous extract of flavonolignans found in milk thistle seeds. A flavonolignan is a compound that is part lignan and part flavonoid.
Lignans are constituents that form a class of propyl phenol dimers that exhibit antiandrogenic and antioxidant properties. Flavonoids constitute a class of more than 600 plant pigmentation agents that demonstrate antioxidant, cardiotonic, hepatoprotective, anti-inflammatory and other properties.
Silymarin and silibinin have both been shown to induce hepatoprotective properties. Neither have been studied enough to determine their specific mechanisms of action. However, current evidence suggests that silibinin acts diversely by:
- Promoting liver cell regeneration by encouraging ribosomal RNA synthesis;
- Inhibiting the alteration of stellate hepatocytes into myofibroblasts, thereby suppressing collagen deposition to prevent cirrhosis;
- Regulating cell membrane stability and permeability, preventing toxins from entering liver cells;
- Scavenging ROS (reactive oxygen species) like heavy metal trace elements, free radicals and environmental toxins;
Most of the therapeutic benefits of silibinin are believed to stem from its antioxidant capacities. Clinical-grade silymarin extracts are known to possess roughly ten times the antioxidant strength of vitamin E. By effectively scavenging oxidative agents, silibinin supplementation may stave off sickness and reduce the physical effects of aging.
Possible Health Benefits of Silibinin
Milk thistle plants, particularly the seeds, have been used to improve human health and well-being for millennia. Although silymarin has a long history of medicinal use, there is currently not enough evidence to definitively attribute any preventive or curative effects to silymarin or its constituents.
However, silymarin and milk thistle extract are commonly used to treat a number of conditions, including jaundice, cirrhosis, NAFLD (non-alcoholic fatty liver disease), menopause symptoms and some forms of viral hepatitis.
Further clinical studies are underway to examine the many health benefits attributed to silibinin and silymarin supplementation. Silibinin is being investigated for its capacity to:
- Decrease triglycerides, LDL and total cholesterol levels in patients with type II diabetes;
- Increase fatty acid storage, thereby encouraging glucose utilization and lowering blood glucose levels;
- Increase insulin and leptin sensitivity and potentially act against the development of obesity;
- Improve overall lipid profiles, which may reduce the risk of atherosclerosis, coronary artery disease and heart disease;
- Act against various cancer cell lines to inhibit angiogenesis, induce apoptosis, control cell cycle activities and prevent metastasis.
There are other possible therapeutic benefits associated with silibinin and/or milk thistle supplementation. Clinical research and experimentation continues.
Dangers of Milk Thistle Supplementation
Milk thistle has been used for thousands of years and is not usually associated with any severe side effects. Milk thistle is generally well tolerated by humans.
Studies involving silymarin supplementation for up to 41 months have not noted any serious side effects. However, there are no standardized silymarin or silibinin dosages. Toxicity is known to be very low in adults.
In rare instances, mild side effects may include headaches and fleeting gastrointestinal distress because of silibinin ingestion. The more serious concerns about safety stem from possible drug interactions. Individuals taking prescription medications that are affected by liver metabolism should speak with their doctor before taking milk thistle.
Silibinin and other silymarin constituents are known to affect activities in the cytochrome p450 enzyme pathway of the liver. P450 substrate agents may interact negatively with Silybum marianum supplementation.
Also, because milk thistle extracts suppress PPAR? (peroxisome proliferator-activated reactor gamma), individuals suffering from diabetes should discuss supplementation with their endocrinologist before taking milk thistle or silymarin.
Milk thistle extract supplements are also known galactogogues. Galactogogues stimulate increases in lactation (milk production). As such, silibinin and/or milk thistle supplementation may not be appropriate for pregnant or nursing women. Be sure to speak with your doctor before taking milk thistle.
Finally, do not take silibinin or silymarin with medications used to treat autoimmune diseases or conditions. All supplementation programs should be discussed with a doctor before being implemented. Possible life-threatening side effects may result from improper silibinin supplementation.
- Reina M, Martinez A. Silybin and 2,3-Dehydrosilybin Flavonolignans as Free Radical Scavengers. J Phys Chem B. 2015 Aug 10. [Epub ahead of print]
- Deep, Gagan et al. "Angiopreventive Efficacy of Pure Flavonolignans from Milk Thistle Extract against Prostate Cancer: Targeting VEGF-VEGFR Signaling." Ed. Surinder K. Batra. PLoS ONE 7.4 (2012): e34630. PMC. Web. 10 Aug. 2015.
- Post-White J1, Ladas EJ, Kelly KM. Advances in the use of milk thistle (Silybum marianum). Integr Cancer Ther. 2007 Jun; 6(2):104-9.
- Brantley, Scott J. et al. "Two Flavonolignans from Milk Thistle (Silybum Marianum) Inhibit CYP2C9-Mediated Warfarin Metabolism at Clinically Achievable Concentrations." The Journal of Pharmacology and Experimental Therapeutics 332.3 (2010): 1081–1087. PMC. Web. 8 Aug. 2015.
- Rosso N1, Marin V, Giordani A, Persiani S, Sala F, Cavicchioli L, Rovati LC, Tiribelli C. The pros and the cons for the use of Silybin-rich oral formulations in treatment of liver damage (NAFLD in particular). Curr Med Chem. 2015 Jul 29.
- Abenavoli L Non-alcoholic fatty liver disease and beneficial effects of dietary supplements. World J Hepatol. 2015 Jun 28;7(12):1723-4.
- Bosch-Barrera J1, Menendez JA2. Silibinin and STAT3: A natural way of targeting transcription factors for cancer therapy. Cancer Treat Rev. 2015 Jun;41(6):540-6.
- Kazazis CE1, Evangelopoulos AA2, Kollas A3, Vallianou NG3. The therapeutic potential of milk thistle in diabetes. Rev Diabet Stud. 2014 Summer;11(2):167-74.
- Bosch-Barrera J1, Menendez JA2. Silibinin and STAT3: A natural way of targeting transcription factors for cancer therapy. Cancer Treat Rev. 2015 Jun;41(6):540-6.
- Huang C1, Huang R, Chang W, Jiang T, Huang K, Cao J, Sun X, Qiu Z. The expression and clinical significance of pSTAT3, VEGF and VEGF-C in pancreatic adenocarcinoma. Neoplasma. 2012;59(1):52-61.
- Ebrahimpour Koujan S1, Gargari BP2, Mobasseri M3, Valizadeh H4, Asghari-Jafarabadi M5. Effects of Silybum marianum (L.) Gaertn. (silymarin) extract supplementation on antioxidant status and hs-CRP in patients with type 2 diabetes mellitus: a randomized, triple-blind, placebo-controlled clinical trial. Phytomedicine. 2015 Feb 15;22(2):290-6.
Article last updated on: April 28th, 2018 by Nootriment
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