Silymarin: A Potent Antioxidant,

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Silymarin: A Potent Antioxidant,

Liver Protector, and Anti-Cancer Agent

 

Silymarin is a unique flavonoid complex—containing silybin, silydianin, and

silychrisin—that is derived from the milk thistle plant. These unique

phytochemicals from the milk thistle have been the subject of decades of

research into their beneficial properties.

 

Milk thistle's common name comes from the white markings on the leaves, its

milky white sap, and its traditional use by nursing mothers to increase milk.

But it is best known for its use as a liver protectant and decongestant, which

can be traced to the Greeks and Pliny the Elder (23-79AD), who wrote that it was

excellent for " carrying off bile. " The famous English herbalist Culpepper

(1616-1654) used milk thistle to cleanse the liver and spleen, and to treat

jaundice and gallstones.1

 

 

 

 

In the U.S., the Eclectics—a prominent group of American doctors who practiced

during the 20th century—used it for liver problems, and to treat varicose veins,

menstrual problems, and spleen and kidney disorders. The plant was also

cultivated as a food, providing leaves for salad, seeds for a coffee-like drink,

and flowers, which were eaten as artichokes are today.1

 

In 1968, a group of German scientists discovered the active flavonoid complex

silymarin, which provides milk thistle's medicinal benefits.2

 

 

Since then, hundreds of studies have been done on silymarin, and it is approved

in the German Commission E Monographs (the most accurate information available

on the safety and efficacy of herbs) as a supportive treatment for inflammatory

liver conditions such as cirrhosis, hepatitis, and fatty infiltration caused by

alcohol and other toxins.3

 

Silymarin is used to:

 

Regenerate liver cells damaged by alcohol or drugs

Decongest the liver (A liver decongestant stimulates bile flow through the

liver and gallbladder, thus reducing stagnation and preventing gallstone

formation and bile-induced liver damage.)

Increase the survival rate of patients with cirrhosis4

Complement the treatment of viral hepatitis5

 

Protect against industrial poisons, such as carbon tetracholoride (a

colorless gass that leaks into air, water and soil near manufacturing and waste

sites)6

Protect the liver against pharmaceuticals that stress the liver, such as

acetaminophen and tetracycline1

Antidote and prevent poisoning from the death cap mushroom, Amanita

phalloides 7,8,9

 

How does silymarin work?

 

As an antioxidant, silymarin scavenges for free radicals that can damage

cells exposed to toxins. Silymarin has been said to be at least ten times more

potent in antioxidant activity than vitamin E.10-12

It increases glutathione in the liver by more than 35% in healthy subjects

and by more than 50% in rats.13 Glutathione is responsible for detoxifying a

wide range of hormones, drugs, and chemicals. High levels of glutathione in the

liver increases its capacity for detoxification.

Silymarin also increases the level of the important antioxidant enzyme

superoxide dismutase in cell cultures.14

It stimulates protein synthesis in the liver, which results in an increase in

the production of new liver cells to replace the damaged ones.15

Silymarin inhibits the synthesis of leukotrienes (mediators of inflammation,

which can result in psoriasis, among other things).16

 

Scientific studies

 

As we've seen, silymarin has proved to be successful in treating alcohol-related

liver disease. In one study, researchers assessed the benefits of milk thistle

extract on 170 patients, 91 of them alcoholics with liver cirrhosis. Subjects

received 140 mg. silymarin three times a day for 41 months. The four-year

survival rate was 58 percent in the silymarin group and 39 percent in the

placebo group. The reduced death rate among those taking silymarin was most

pronounced in the alcoholic cirrhosis subgroup. There were no side effects from

silymarin.4

 

This study is significant for several reasons. Since there were no side effects,

the results support the idea that long-term treatment is beneficial and not

likely to be harmful. These results also indicate that silymarin may be

particularly effective for patients with alcohol-induced liver damage.

 

Effective in fighting several cancers

 

Although German scientists first discovered the protective effects of silymarin

on liver function in the late 1960s, its impressive cancer-fighting properties

were just discovered in the last decade. While it is not surprising that an

antioxidant like silymarin would have anti-cancer effects, the molecular effects

of silymarin that give it powerful anti-cancer properties have amazed even the

scientific community. In the last few years, researchers have begun to discover

exactly why silymarin has such broad anti-cancer properties.

 

Among the most promising cancer fighting strategies that researchers are trying

to develop are angiogenesis inhibitors (which stop the proliferation of blood

vessels that feed tumors), cell cycle regulators, and selective promoters of

cancer cell death. Amazingly, silymarin has been shown to possess all of these

abilities. A review of research into silymarin's effects on prostate cancer

(published February 4, 2004) concluded that silymarin has a huge potential to

interfere with many molecular events involved in cancer cell growth,

progression, and angiogenesis. The authors also stated that silymarin has

recently entered clinical trials in prostate cancer patients because of " its

non-toxic and mechanism-based strong preventive/therapeutic efficacy. " 17

 

Because of this you would expect silymarin to have activity against a broad

range of cancer types, and an examination of the literature shows that silymarin

has impressive effects against prostate18, colon19, ovarian20, skin21, lung22,

breast23, and cervical cancers24 in preliminary studies. In the cases of

prostate and ovarian cancer, human clinical trials are currently underway both

in the USA and Europe.

 

Offers hope for the prevention of cancer … and as an adjunct treatment

 

The novel and unique ways that silymarin fights cancer means that it may offer

hope not only for the prevention of cancer, but also for the treatment of

cancer, both alone and when combined with existing cancer drugs. This is because

silymarin has shown direct tumor killing properties of its own, and is also

synergistically effective with two popular chemotherapy agents, doxorubicin and

cisplatin.25,26,17

 

Why isn't silymarin being hailed as a cancer drug in the medical world?

 

With such an impressive list of accomplishments you would expect silymarin to be

quickly developed as a broad-spectrum cancer fighter. But as a natural, herbal

product that has been used for more than 30 years primarily for liver problems,

it has a strike against it. If it were a new drug that had been developed and

patented by a pharmaceutical company, it would be hailed as a potential

breakthrough in the fight against cancer. But no pharmaceutical company wants to

spend millions of dollars doing research on an herb that can't be patented.

 

Unfortunately, interest in researching silymarin's efficacy at fighting cancer

in humans has only been promoted by a small group of dedicated scientists who

have recognized silymarin's novel, powerful, and multiple cancer fighting

properties. One can only hope that silymarin's natural origins don't condemn it

to becoming only a scientific curiosity.

 

Silybin/Phospholipid Complex (Silyphos)

 

Two recent innovations in silymarin supplementation have greatly enhanced the

benefits we can obtain from silymarin. The first was the discovery that silybin,

one of several flavonoids found in the " silymarin fraction " extracted from milk

thistle, is the most potent constituent. Because of this, techniques were

developed to further purify silymarin to obtain pure silybin. Because silybin is

now recognized as the active flavonoid in silymarin, most recent research has

utilized pure silybin rather than silymarin itself.

 

One of the inherent problems with oral silymarin or silybin supplementation is

its very poor absorption. Recently, a new complex of silybin and natural

phospholipids was developed. This improved product is known by the name of

Silyphos. By complexing silybin with phospholipids, scientists were able to make

silybin into a much more soluble and better-absorbed form.

 

This silybin/phospholipid complex (Silyphos) was found to have significantly

improved bioavailability, up to ten times better absorption, and greater

effectiveness.27,28,29 This dramatically enhances the benefits of silybin,

because typical silymarin extracts and silybin are very poorly utilized when

taken orally.

 

How safe is silymarin?

 

Milk thistle has been safely used as a medicinal herb for centuries. Although

its effects can be quite dramatic, it is gentle and well tolerated.

 

Speak with your health care professional if you have cancer and are on

chemotherapy drugs, before taking this or any other herb. Studies show that some

chemotherapy drugs have a synergistic effect with silymarin and may increase the

drug's effects. If you're taking drugs known to cause liver damage (like

acetaminophen), silymarin may help repair and prevent future damage.

 

An antidote to environmental toxins

 

James Duke, Ph.D., a leading authority on healing herbs, says " Even if you don't

have liver damage or liver disease, milk thistle helps improve liver function by

helping the liver remove toxins from your body. " 30 In this modern world filled

with environmental and chemical toxins, silymarin is an antioxidant you just

might want to add to your nutritional supplement regimen.

 

While milk thistle and silymarin have had decades of very positive results for

protecting the liver, recent studies into silybin's remarkable anti-cancer

properties have provided even more compelling reasons to consider

supplementation. And now, with the advent of the more potent and much better

utilized Silybin/Phospholipid Complex (Silyphos), the amazing benefits contained

within the milk thistle are available to everyone.

 

References

 

1. Presser, Arthur. Pharmacist's Guide to Medicinal Herbs. Smart Publications,

Petaluma, CA, 2000.pp 259-260.

 

2. Wagner, H., et al. " The Chemistry of Silymarin (Silybin), the Active

Principle of the Fruits of Silybum marianum. " Arzneim-Forsch Drug Res. 1968;

18:688-96.

Abstract

 

3. Blumenthal M, Busse W Goldberg A, eds. The Complete German Commission E

Monographs. 1998; Austin, TX: American Botanical Council; Boston: Integrative

Medical Communications.

 

4. Ferenci P, et al. Randomized, controlled trial of silymarin treatment in

patients with cirrhosis of the liver. J Hepatol 1989;9:105-13.

Abstract

 

5. Berenguer J and Carrasco D. Double-blind trial of silymarin versus placebo in

the treatment of chronic hepatitis. Muench Med Wochenschr 1977; 119, 240-260.

 

6. Wagner H. Plant constituents with antihepatotoxic activity. Natural Products

as Medicinal Agents (Beal JL and Reinhard E, eds.) 1981; Hippokrates-Verlag,

Stuttgart, Germany.

 

7. Faulstich H, et al. Silybin inhibition of amatoxin uptake in the perfused rat

liver. Arzneim-Forsch Drug Res 1980;30:452-4

Abstract

 

8. Tuchwever B, et al. Prevention of silybin of phalloidin induced acute

hepatoxicity. Toxicol Appl Pharmacol 1979;51:265-75.

Abstract

 

9. Catalina MV, Nunez O, Ponferrada A, Menchen L, Matilla A, Clemente G, Banares

R. [Liver failure due to mushroom poisoning: clinical course and new treatment

perspectives] [Article in Spanish] Gastroenterol Hepatol. 2003;

Aug-Sep;26(7):417-20.

Abstract

 

10. Awang D. Milk thistle. Can Pharm J 1993; 422, 403-404.

 

11. Wagner H. Antihepatotoxic flavonoids. Plant Flavonoids in Biology and

medicine: Biochemical, Pharmacological, and Structure-Activity Relationships.

1986; Alan R. Liss, New York, pp. 545-558.

 

12. Adzet T. Polyphenolic compounds with biological and pharmacological

activity. Herbs Spices Med Plants 1986;1,167-184.

 

13. Valenzuela A, et al. Selectivity of silymarin on the increase of the

glutathione content in different tissues of the rat. Planta Medica 1989; 55,

420-422.

Abstract

 

14. Muzes G, et al. Effect of the bioflavonoid silymarin on the in vitro

activity and expression of super oxide dismutase (SOD) enzyme. 1991; Acta

Physiol Hungarica 78, 3-9.

Abstract

 

15. Fiebrich G and Koch H. Silymarin, an inhibitor of lipoxygenase. Experientia

1979; 35,148-150.

 

16. Nassuato G, Iemmolo RM, Strazzabosco M, et al. Effect of silibinin on

biliary lipidcomposition: experimental and clinical study. J Hepatol 1991; 12:

290-5.

 

17. Singh RP, Agarwal R, Prostate cancer prevention by silibinin, Curr Cancer

Drug Targets. 2004 Feb;4(1):1-11).

Abstract

 

18. Zi X, Agarwal R. Silibinin decreases prostate-specific antigen with cell

growth inhibition via G1 arrest, leading to differentiation of prostate

carcinoma cells: implications for prostate cancer intervention. Proc Natl Acad

Sci USA 1999; 96: 7490-7495.

Abstract

 

19. Yang SH, Lin JK, Chen WS, Chiu JH.Anti-angiogenic effect of silymarin on

colon cancer LoVo cell line. J Surg Res. 2003; Jul;113(1):133-8.

Abstract

 

20. Gallo D, Giacomelli S, Ferlini C, Raspaglio G, Apollonio P, Prislei S, Riva

A, Morazzoni P, Bombardelli E, Scambia G. Antitumour activity of the

silybin-phosphatidylcholine complex, IdB 1016, against human ovarian cancer. Eur

J Cancer. 2003; Nov;39(16):2403-10.

Abstract

 

21. Singh RP, Agarwal R, Flavonoid antioxidant silymarin and skin cancer,

Antioxid Redox Signal. 2002 Aug;4(4):655-63.

Abstract

 

22. Sharma G, Singh RP, Chan DC, Agarwal R, Silibinin induces growth inhibition

and apoptotic cell death in human lung carcinoma cells, Anticancer Res. 2003

May-Jun;23(3B):2649-55.

Abstract

 

23. Zi X, Feyes DK, Agarwal R, Anticarcinogenic effect of a flavonoid

antioxidant, silymarin, in human breast cancer cells MDA-MB 468: induction of G1

arrest through an increase in Cip1/p21 concomitant with a decrease in kinase

activity of cyclin-dependent kinases and associated cyclins, Clin Cancer Res.

1998 Apr;4(4):1055-64.

Abstract

 

24. Bhatia N, Zhao J, Wolf DM, Agarwal R, Inhibition of human carcinoma cell

growth and DNA synthesis by silibinin, an active constituent of milk thistle:

comparison with silymarin, Cancer Lett. 1999 Dec 1;147(1-2):77-84.

Abstract

 

25. Scambia G, De Vincenzo R, Ranelletti FO, et al, Antiproliferative effect of

silybin on gynaecological malignancies: synergism with cisplatin and

doxorubicin, Eur J Cancer. 1996 May;32A(5):877-82.

Abstract

 

26. Dhanalakshmi S, Agarwal P, Glode LM, Agarwal R, Silibinin sensitizes human

prostate carcinoma DU145 cells to cisplatin- and carboplatin-induced growth

inhibition and apoptotic death, Int J Cancer. 2003 Sep 20;106(5):699-705.

Abstract

 

27. Morazzoni P, Montalbetti A, Malandrino S, Pifferi G, Comparative

pharmacokinetics of silipide and silymarin in rats, Eur J Drug Metab

Pharmacokinet. 1993 Jul-Sep;18(3):289-97.

Abstract

 

28. Schandalik R, Gatti G, Perucca E, Pharmacokinetics of silybin in bile

following administration of silipide and silymarin in cholecystectomy patients,

Arzneimittelforschung. 1992 Jul;42(7):964-8.

Abstract

 

29. Comoglio A, Tomasi A, Malandrino S, Poli G, Albano E., Scavenging effect of

silipide, a new silybin-phospholipid complex, on ethanol-derived free radicals,

Biochem Pharmacol. 1995 Oct 12;50(8):1313-6

Abstract

 

 

30. Duke, James. A. The Green Pharmacy. Rodale Press. 1977.

 

 

 

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