65666-07-1

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• Description

  Silymarin(65666-07-1) is a kind of flavonoid complex consisting of silybin, silydianin, and silychrisin, derived from the milk thistle plant. It is a kind of potent antioxidant, anti-cancer agent as well as liver protecting agent. It has a lot of pharmaceutical functions. For example: (1) Promotes healthy liver function and general health; (2) Strengthen the normal cellular defense system to protect the liver tissue; (3) Help to eliminate the toxin accumulating in the liver; (4) Increase the survival rate of patients of cirrhosis; (5) Protect our body against industrial poisons; (6) Antidote against the death cap mushroom. Silymarin exerts its pharmaceutical effects through various mechanism including scavenging free radicals, increasing glutathione (has detoxifying effect) level in the liver, increasing the levels of antioxidant enzymes such as superoxide dismutase, stimulating liver protein synthesis and inhibiting the synthesis of leukotrienes. ;

• Physical properties

  Silymarin is obtained from silybum marianum (milk thistle), an edible plant that has been used medicinally for centuries as a herbal medicine for the treatment of liver related disorders. The plant is native to the Mediterranean andis widely found in Europe and North America. It also grows in India, China, South America and Australia. This herb is approved for sale in Canada in different products and gains an annual business of 180 million in Germany.
  
  Silymarin is a polyphenolic flavonoid, extracted using 95% ethanol, from the seeds of the milk thistle. The plant consists of approximately 70-80% of silymarin flavonolignans and approximately 20-30% undefined fraction. The most prevalent component is Silybin (50-60% of Silymarin). It consists of seven flavonoglignans (silibinin, isosilibinin, silychristin, isosilychristin and silydianin) and a flavonoid (taxifolin). ;

• Pharmacokinetics

  Silymarin is insoluble in water and is often administered in a capsulated form. It is absorbed orally, with peak plasma concentration in 6-8 hr. But, the oral absorption of silymarin is only about 23-47% leading to low bioavailability. The poor water solubility and bioavailability led to the development of enhanced formulations like silipide (Siliphos) a complex of silymarin and phosphatidylcholine which is ten times more bioavailable.;

• Mechanism of action

  Silymarin's hepatoprotective effects are accomplished by several mechanisms which include antioxidant, inhibition of lipid peroxidation, enhanced hepatocyte regeneration, enhanced liver detoxification and protection from glutathione depletion, antiinlammatory effects including inhibition of leukotriene, prostaglandin synthesis and kupffer cells, mast cell stabilization. slowing of fibrosis by reducing conversion of hepatic stellate cells.
  Silymarin is a naturally-occurring polyphenolic flavonoid compound. Silymarin is derived from the seeds of the milk thistle plant. It has inhibitory effects on melanogenesis in a spontaneously immortalized mouse melanocyte cell line, Mel-Ab. In one study (Choo et al., 2009), silymarin was shown to significantly prevent melanin production in a dose-dependent manner with an IC50 value of 28.2 μg/ml, without effects on cell viability (Choo et al., 2009). Also, silymarin inhibits the L-DOPA oxidation activity of the rate-limiting melanogenic enzyme tyrosinase in cell based-systems but it does not directly affect cell-free tyrosinase activity (Choo et al., 2009). Furthermore, silymarin decreases the expression of tyrosinase protein (Choo et al., 2009). ;

• Uses

  In the United States, milk thistle(65666-07-1) is most commonly used to treat viral infections and cirrhosis of the liver. Milk thistle (Silybum marianum) was used in classical Greece to treat liver and gallbladder diseases and to protect the liver against toxins. It recently has been investigated for use as a cytoprotectant, an anticarcinogen, and a supportive treatment for liver damage from Amanita phalloides poisoning. Its active ingredient is silymarin, found primarily in the seeds. Silymarin undergoes enterohepatic recirculation, which results in higher concentrations in liver cells than in serum.It is made up of components called flavonolignans, the most common being silybin. ;

• Side effects

  Silymarin has very low toxicity and has been shown a good safety profile. At high doses it has a laxative effect due to increased bile secretion, adverse effects related to GI tract were reported in 2-10% patients in a clinical trial.;

• References

  http://www.smart-publications.com/articles/silymarin-a-potent-antioxidant-liver-protector-and-anti-cancer-agent/page-2
  http://172.16.24.181/www.mediherb.com/media/797348/silymarin-pds.pdf ;

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