Silymarin
Description
Milk thistle (Silybum marianum) was named Silybum by Dioscorides in 100 AD for its large purple thistle-like flower heads. Since ancient times, the plant was valued for its nutritional and medicinal properties. The name “milk thistle” refers to the white streaks along the leaf veins, in legend resulting from the spilling of a drop of breast milk from the Virgin Mary - hence “marianum”.
The root has been eaten like parsnip, the leaves like artichoke and the seeds roasted for a coffee-like beverage.
The part of the plant used today is the seeds. Milk thistle seeds are harvested and the active bioflavonoids are extracted by methyl alcohol. The solution is filtered and evaporated under vacuum. The final defatted suspension is dried in a ventilation oven. The active component is standardized at 80% silymarin.
Method of Action
The active substances are 3 potent liver protective bioflavonoids: silybin, silydianin and silychristin known collectively as Silymarin.
The mechanism of action of silymarin involves: altering the membranes of hepatic cells to inhibit passage of toxins; increasing cellular regeneration by stimulating protein synthesis; antioxidant activity including the inhibition of inflammatory enzymes. Silymarin counteracts the toxic effects of a wide variety of poisons, including alcohol, carbon tetrachloride, acetaminophen overdose, and the Deathcap mushroom (Amanita phalloides). Recent research further indicates that silymarin protects against glutathione (an antioxidant) depletion in liver cells.
Silymarin scavenges free radicals and leukotrienes.
These protective mechanisms appear to work prophylactically as well as curatively.
Therapeutic Approaches
By the Middle Ages the seed of the Milk Thistle was commonly used to treat “melancholy” i.e. liver diseases [which could include: acute, chronic hepatitis, toxins, jaundice, or fatty degeneration of the liver]; to promote the flow of bile; a general tonic for: thestomach, spleen, gallbladder and female organs; as well as for psoriasis and varicose veins.
In the last 30 years, especially in Europe, and Germany in particular, its efficacy regarding liver diseases has resulted in numerous clinical studies, publications and product development.
Directions for use usually range between 300-600 mg./day, sometimes together with other herbs, acting as bio-enhancing agents, such as: dandelion root, turmeric, artichoke, and schisandra.
In this day and age, concentration is upon alcohol-induced liver disease (cirrhosis).
Milk Thistle fruit has approval status by the German Commission E for dyspepsia and liver disease e.g. cirrhosis.
References:
Blumenthal, M (Ed.): The Complete German Commission E Monographs: Therapeutic Guide to Herbal Medicines. American Botanical Council. Austin, TX. 1998.
Toxicity Factors
No known toxicity, even in large doses.
Therapeutic dosages tend to be within the range of 140 - 210 mg three times daily.
A sensitive patient, or someone trying the latest, higher bioavailability products, may encounter mild side-effects: typically, headache and gastrointestinal tract upsets brought on by increased hepatobiliary stimulation.
The German Commission E status of the herb is "null" or neutral i.e. while it is not approved, there is no documented risk. There may also be some concern over the claims made by manufacturers i.e. they are unproven.
References:
Blumenthal, M (Ed.): The Complete German Commission E Monographs: Therapeutic Guide to Herbal Medicines. American Botanical Council. Austin, TX. 1998.
References
Alarcon-de-la-Lastra-AC et al: Gastroprotection induced by silymarin, the hepatoprotective principle of Silybum marianum in ischemia-reperfusion mucosal injury: role of neutrophils. Planta-Med. 1995 Apr; 61(2): 116-9.
Anderson-D; Yu-TW; Phillips-BJ; Schmezer-P: The effect of various antioxidants and other modifying agents on oxygen-radical-generated DNA damage in human lymphocytes in the COMET assay. Mutat-Res. 1994 May 1; 307(1): 261-71.
Bartholomaeus-AR; Bolton-R; Ahokas-JT: Inhibition of rat liver cytosolic glutathione S-transferase by silybin. Xenobiotica. 1994 Jan; 24(1): 17-24.
Bindoli, A et al., Inhibitory action of silymarin on lipid peroxide formation in rat liver mitochondria amnd micrososmes. Biochem Pharmacol. 1977, 26: 2,405-2,409.
Brown, D.J. Phytotherapy Review and Commentary: Silymarin. Townsend Letter for Doctors, November 1994 and July 1995.
Bulfoni, A & Gobbato, F: Evaluation of the therapeutic activity of silymarin in alcoholic hepatology. Gazz. Med. Ital. 1979, 138: 597-608.
Campos, R. et al. (1989) Silybin Dihemisuccinate protects against glutathione depletion andlipid peroxidation induced by acetaminophen on rat liver. Planta Medica. 55:417.
Canini, F. et al. (1985) The use of silymarin in the treatment of alcoholic hepatic stenosis. Clin. Ther. 114:307-314.
Castiella-A & Arenas-JI: Utility of silymarin in the cyclopeptide syndrome [letter]. J-Hepatol. 1994 Dec; 21(6): 1148.
Faulstich, H et al., Silybin inhibition of amatoxin uptake in the perfued rat liver. Arznheim-Fi=orsch. Drug Res. 1980, 30: 452-454.
Ferenci, P. et al. (1989) Randomized controlled trial of silymarin treatment in patients with cirrhosis of the liver. J. Hepat. 9:105.
Foster, S. Milk thistle: Silybum marianum. Botanical Series No. 305, American Botanical Council, Austin, TX. 1991.
Foster, S. Milk thistle: herbal seeds and medicinal needs. Better Nutrition for Today’s Living,1995 (April):64-7.
Gatti-G & Perucca-E: Plasma concentrations of free and conjugated silybin after oral intake of a silybin-phosphatidylcholine complex (silipide) in healthy volunteers. Int-J-Clin-Pharmacol-Ther. 1994 Nov; 32(11): 614-7.
German Commission E Monograph: Cardui Mariae fructus (Milk Thistle fruit). 1996.
Gershbein-LL: Action of dietary trypsin, pressed coffee oil, silymarin and iron salt on 1,2-dimethylhydrazine tumorigenesis by gavage. Anticancer-Res. 1994 May-Jun; 14(3A): 1113-6.
Hall-PM; Plummer-JL; Ilsley-AH; Ahern-MJ; Cmielewski-PL; Williams-RA: The pathology of liver injury induced by the chronic administration of alcohol and 'low-dose' carbon tetrachloride in Porton rats. J-Gastroenterol-Hepatol. 1994 May-Jun; 9(3): 250-6.
Hruby, C. (1984) Silibinin in the treatment of DeathcapFungus poisoning. Forum 6:23.
Kim-DH; Jin-YH; Park-JB; Kobashi-K: Silymarin and its components are inhibitors of beta-glucuronidase. Biol-Pharm-Bull. 1994 Mar; 17(3): 443-5.
Koch, HP et al. (1985) Silymarin: Potent inhibitor of cyclic AMP phosphodiesterase. Meth. Find. Espt. Clin Pharm. 7:409.
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Miguez-MP; Anundi-I; Sainz-Pardo-LA; Lindros-KO: Hepatoprotective mechanism of silymarin: no evidence for involvement of cytochrome P450 2E1. Chem-Biol-Interact. 1994 Apr; 91(1): 51-63.
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Mowrey, D. (1990) Guaranteed Potency Herbs. A Compilation of writings on the subject.
Mowrey, D. (1986) The Scientific Validation ofHerbal Medicine. Cormorant Books.
Palasciano, G. et al : The effect of silymarin on plasma levels of malondialdehyde in patients receiving long-term treatment with psychotropic drugs. Curr. Ther. Res. 1994,55:537-45.
Pifferi-G; Pace-R; Conti-M: Synthesis and antihepatotoxic activity of silybin 11-O-phosphate. Farmaco. 1994 Jan; 49(1): 75-6.
Schandalik-R; Perucca-E: Pharmacokinetics of silybin following oral administration of silipide in patients with extrahepatic biliary obstruction. Drugs-Exp-Clin-Res. 1994; 20(1): 37-42.
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Sierralta-A; Jeria-ME; Figueroa-G; Pinto-J; Araya-JC; San-Juan-J; Grinbergs-J; Valenzuela-E.[Mushroom poisoning in the IX region. Role of Amanita gemmata] Rev-Med-Chil. 1994 Jul; 122(7): 795-802.
Valenzuela, A et al., Selectivity of silymarin on the increase of the glutathione content in different tissues of the rat. Planta Med. 1989, 55: 420-422.
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