Silymarin.Milk Thistle and applications.
Article Content:
- .Botanical Basic Data of Milk Thistle.
- .Phytochemicals of milk thistle.
- .History of Silymarin and foundation.
- .Modern Application and function of Silymarin and silybin.
- .Dosage and Administration.
- .Milk Thistle:Pharmacology.
- .The Awesome Power of the Milk Thistle.
- .How Search engine think about Milk Thistle.
- .Research Update of Silybum Marianum.Silymarin
Modern Application and function of Silymarin and silybin.
1.Silymarin as inhibitor of Beta-glucuronidase:
Silymarin, a commercial crude drug used as a hepatoprotective, was found to inhibit beta-glucuronidase activityof the feces of a healthy human and of a human with colon cancer. Silymarin and silybin protected the increase in enzyme activity in the serum of the treated rats.
2.Silibinin Anti Free radicals:
Silibinin dihemisuccinate (SDH) is a flavonoid of plant origin with hepatoprotective effects which have been partially attributed to its ability to scavenge oxygen free radicals. The studies showed that SDH has an inhibitory effect, which is dependent on its concentration and the magnitude of lipid peroxidation.
This work supports the reactive oxygen species scavenger action ascribed to SDH.
3.Hepatoprotective:
The hepatoprotective activity of the drug is said to be based on two mechanisms:
1. Silymarin alters the structure of the outer membrane of the hepatocytes in such a way as to prevent penetration of the liver toxin into the interior of the cell.
2. Silymarin stimulate the action of nucleolar polymerase A, resulting in ribosomal protein synthesis and, thus stimulates the regenerative ability of the liver and formation of new hepatocytes.
The involvement of the alcohol-inducible cytochrome P450 2E1 in the hepatoprotective mechanism of the plant flavonoid extract silymarin, and its main active component silybin, was investigated in isolated hepatocytes.
Contrary to earlier reports we found no evidence for an interaction of silymarin or silybin with cytochrome P450 2E1. This suggests that the antioxidant and free radical scavenging properties may account for most of the therapeutic effect of these compounds.
The untoward effect of silymarin on cultured cells may have consequences when considering long-term prescription of this therapeutic agent.
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.
Changes of concentration, total content of histones and relative portions of histone fractions were investigated in the liver of rats after administration of the hepatoprotective substance silymarin (70 mg/kg) and after gamma-irradiation of the whole body at a dose of 3 Gy. The results document that silymarin administration 1 hour before irradiation had a positive effect which was observed in all the investigated parameters in hour 30 after irradiation. But the radioprotective effect of silymarin was only temporary while until day 7 after irradiation histone variations were identical or still larger than after irradiation without silymarin administration.
4.Liver injury protection of silymarin:
Historically, this herb has been used in Europe as a liver tonic, and current phytotherapy indicates its use in a whole range of liver and gallbladder conditions including hepatitis and cirrhosis. It may also have value in the treatment of chronic uterine problems.
Today, milk thistle is the main remedy used in Western herbal medicine to protect the liver and its many metabolic activities, and help renew its cells. Milk thistle is used in the treatment of hepatitis and jaundice, as well as in conditions where the liver is under stress whether from infection, excess alcohol, or from chemotherapy prescribed to treat diseases such as cancer. In this last instance, milk thistle can help to limit damage done to the liver by chemotherapy and speed up recovery from side effects once the treatment is completed.
Milk Thistle is unique in its ability to protect the liver and has no equivalent in the pharmaceutical drug world. In fact, in cases of poisoning with Amanita mushrooms, which destroy the liver, milk thistle is the only treatment option. It has been so dramatically effective that the treatment has never been disputed, even by the traditional medical community.
In multiple human, animal, and laboratory studies, it has shown differing degrees of effectiveness for protecting the liver from damage caused by alcohol, chemicals, drugs, diseases, and poisonous plants.
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 and other chemicals in milk thistle are believed to protect liver cells in several different ways:
Strong antioxidant:Silymarin has antioxidant properties. Antioxidants are thought to prevent or lessen damage to body cells that is caused by a chemical process called oxidation.
Silymarin scavenges free radicals and leukotrienes,silymarin shows very strong properties of antioxidant, reduce the chance of liver cells damage by free radicals,protect liver cell membrane, owes anti-radiation functions and could be used to inhibiting peritonitis.
Anti-inflammatory:effects of silymarin help keep liver cells from swelling in response to injury.
Silymarin seems to encourage the liver to grow new cells, while discouraging the formation of inactive fibrous tissue.
By changing the outside layer of liver cells, silymarin may also keep certain harmful chemicals from getting into liver cells.
Milk thistle may also cause the immune system to be more active.
Prevent liver damge:Silymarin especially could be applied to reduce the damge of liver from over dose of alcohol drink.for the silymarin can shape a membrane,and prevent poison things,silymarin especially certain detoxifiying function for some disease caused by poison.
Cure liver disease:Silymarin owes functions to strengthen and restore functions of liver. By prompt and stimulate the synthesis of protein,silymarin can prompt cell of liver recover and restore,stimulate new cell growth.as for functions above,silymarin show good functions to protect and stabilize liver cells,can be used to treat for hepatitis,hepatocirrhosis,hepatomegaly and other liver disease, hepatitis patients recover sooner after silymarin taken.
Adjust the bile secretion:Silymarin can djust the bile secretion,since help the lipid and fat metabolism,tonify the five organs including stomach,spleen,gallbladder,kidney and liver.
Detoxifying:Silymarin can be used to detoxifying the poison for liver from certain prescription medicine.
Shape Liver Index:Silymarin Show good effects for treatment of GOT,GPT or ALT,AST.
Treatment for C-hepatitis:Silymarin show good improvement for patients of C-hepatitis,as for this properties,Silymarin could be used especially to treatment of patients without good result from common prescription medicines.
Treatment for chronic hepatitis:Silymarin can be good remedy for the patients of chronic hepatitis,if the Liver Index high long terms,result can be got to help lower the liver cell damage and protect liver cancerization.
Safety: GCE and other agencies proved that Silymarin is a good herb medicine for liver protection with high safety.
These protective mechanisms appear to work prophylactically as well as curatively. Milk thistle was approved in 1986 as a treatment for liver disease and it is widely used to treat alcoholic hepatitis, alcoholic fatty liver, cirrhosis, liver poisening and viral hepatitis. It has also been shown to protect the liver against medications such as acetaminophen, a non-aspirin pain reliever.
The ability of silymarin (800 mg/d) to prevent psychotropic drug-induced (phenothiazines and butyrophenones) liver damage was evaluated in a double-blind placebo-controlled trial.
Silymarin and Its Liver protection Mechanism:
The active ingredient, or liver-protecting compound in milk thistle is known as silymarin. This substance, which actually consists of a group of compounds called flavonolignands, helps repair liver cells damaged by alcohol and other toxic substances by stimulating protein synthesis. By changing the outside layer of liver cells, it also prevents certain toxins from getting inside. Silymarin also seems to encourage liver cell growth. It can reduce inflammation (important for people with liver inflammation or hepatitis), and has potent antioxidant effects. Antioxidants are thought to protect body cells from damage caused by a chemical process called oxidation. Our Milk Thistle is not standardized to an exact amount (as it is made from pure dried natural herbs. Milk Thistle naturally contains about 70 - 80% Silymarin (and many other constituents thought to work in harmony).
Silymarin is known to protect the liver by altering and strengthening the structure of outer cell membranes of hepatocytes (liver cells), preventing toxins from entering the liver cells, and by stimulating the regenerative ability of the liver and the formation of new hepatocytes through the activation of an enzyme nucleolar polymerase A, which leads to the increase in ribosomal protein synthesis and cell division.
Silymarin, as an anti-oxidant, may also reduce damages to liver cells caused by chronic use of certain prescription drugs. The silybin component of sillymarin has been related to cholesterol-lowering effects. Through the capability to increase bile solubility, sylimarin may also help prevent or alleviate gallstones.
As a natural flavonoids with strong antioxidant properties,scientists from Germany earliest proved that silymarin with properties of inhibiting 5-lipoxyenase(this enzyme prompt oxidation inside body),also could prompt the liver cell secrete more Glutathione (GSH,a kind of enzyme with antioxidant properties) and stabilize the liver cell membrance.
Once Silymarin conbined with the liver cell, the detoxifying functions of the liver cells stronger and could better prevent damage from poisonous matter,Same time, the antioxidant properties of silymarin show strong detoxifying function and could lower and decrease the concentration of the poisonous matter effectively.
Silymarin owes good functions of prompting liver cell repair and rebirth,increase the synthesis of protein from liver cells.
Dose: 12-15 grams per day of powdered seed is recommended for making infusions or other preparations to be taken orally. For standardized extract, 200-400 mg of silymarine per day is recommended.
Side Effects: No side effects are known for crude preparation, as milk thistle is a food, and a relative of artichoke. For standardized extract with high concentration of sylimarine, a mild laxative effect has been observed occasionally.
Liver disease from alcohol:
A comprehensive review by the U.S. Agency for Healthcare Research and Quality (AHRQ) recently identified 16 scientific studies on the use of milk thistle for the treatment of various forms of liver disease. A European standardized extract of milk thistle was used in most of the trials. Problems in study design (such as small numbers of participants, variations in the causes of liver disease, and differences in dosing and duration of milk thistle therapy) made it difficult to draw any definitive conclusions. However, five of seven studies evaluating milk thistle for alcoholic liver disease found significant improvements in liver function. Those with the mildest form of the disease appeared to improve the most. Milk thistle was less effective for those with severe liver disease such as cirrhosis. Cirrhosis is characterized by scarring and permanent, non-reversible damage to the liver. It is often referred to as end-stage liver disease.
Milk Thistle has been found in recent years to be a major player in the treatment of Liver Disease. Because it helps lower enzyme levels and facilitates the liver in its process of detoxifying the body. Among all known herbal remedies, Milk Thistle finds its place as the leader in herbs to treat liver disease. Physicians have prescribed Milk Thistle for Hepatitis to keep down inflammation, Cirrhosis to soften the liver, Liver Cancer to aid in detoxification, and many dysfunctions of the Gall Bladder System. It also helps protect the liver for those individuals that are taking prescription medications known to elevate liver enzymes.
5.Silymarin reduced lipoperoxidative hepatic damage:
Some Researchers have previously established a model for micronodular cirrhosis by feeding Wistar rats alcohol, in the Lieber-DeCarli liquid diet, and exposing them to 'low-dose' carbon tetrachloride (CCl4) vapour for 10 weeks. Micronodular cirrhosis developed in all animals after 5-7 weeks of treatment. The simultaneous administration of silymarin, a putative hepatoprotective agent, in the liquid diet, did not alleviate or prevent the chronic liver injury. The histopathological features of the liver injury are described, with particular emphasis on the presence of small epithelial cells ('progenitor or stem cell'), which appear to be playing a role in liver regeneration.
The naturally occurring hepatoprotective compound silybin is a potent inhibitor of glutathione S-transferase isoenzymes.
6.Plasma concentrations of silybin:
Plasma concentrations of silybin were evaluated in healthy volunteers by using a sensitive and specific HPLC method. Free silybin concentrations reached a peak of 141 +/- 31 ng/ml (mean +/- SEM) at 2.4 hours after dosing and declined thereafter with a half-life of about 2 hours. Peak concentrations of conjugated silybin were greater (255 +/- 35 ng/ml) and occurred at a later time (about 3.8 hours). The elimination of conjugated drug tended to be slower than that of free drug.
After oral intake of silipide, silybin undergoes extensive conversion to conjugated derivative(s) which are retained in the circulation at relatively large concentrations.
Plasma concentrations of free and conjugated silybin after oral intake of a silybin-phosphatidylcholine complex (silipide) in healthy volunteers.
7.Medicinal Action and Traditional uses:
Milk thistle flower heads, boiled and eaten like artichokes, were useful as a spring tonic after the winter months when people had been deprived of fresh vegetables. They were also taken to increase breast-milk production, and were considered excellent for melancholia (depression), which was traditionally associated with the liver. Gerard stated in his Herball of 1597, "My opinion is that this (milk thistle) is the best remedy that grows against all melancholy diseases."
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.
8. Silymarin proved against hepatotoxicity
Milk thistle acts in a similar fashion to detoxify other synthetic chemicals that find their way into our bodies, from acetaminophen and alcohol to heavy metals and radiation.
In recent years, considerable emphasis has been placed on identifying new cancer chemopreventive agents which could be useful for human populations. Silymarin, an anti-oxidant flavonoid isolated from artichoke, has been shown to possess significant activity against hepatotoxicity and other pharmacological and physiological disorders. We assessed the effect of skin application of silymarin. Treatment resulted in significant inhibition of TPA-induced epidermal ODC activity in a. dose- and time-dependent manner.
Our data suggest that silymarin could be a useful anti-tumor promoting agent capable of ameliorating the tumor promoting effects of a wide range of tumor promoters.
Agarwal-R; Katiyar-SK; Lundgren-DW; Mukhtar-H: Inhibitory effect of silymarin, an anti-hepatotoxic flavonoid, on 12-O-tetradecanoylphorbol-13-acetate-induced epidermal ornithine decarboxylase activity and mRNA in SENCAR mice. Carcinogenesis.
9. Promotes milk secretion:
As its name implies, it promotes milk secretion and is perfectly safe to be used by all breast feeding mothers.Milk thistle has some estrogen-like effects that may stimulate the flow of breast milk in women who are breast-feeding infants. It may also be used to start late menstrual periods. Milk thistle's estrogen-like effect may also have some usefulness for men with prostate cancer.
10. Viral hepatitis:
Despite the fact that milk thistle is widely used in the treatment of hepatitis (particularly hepatitis C), results from four viral hepatitis studies were contradictory. Some found improvements in liver enzyme activity while others failed to detect these benefits. None of the studies compared milk thistle with interferon or other medications for viral hepatitis.
11.Cancer:
Preliminary laboratory studies also suggest that active substances in milk thistle may have anti-cancer effects. One active substance known as silymarin has strong antioxidant properties and has been shown to inhibit the growth of human prostate, breast, and cervical cancer cells in test tubes. Further studies are needed to determine whether milk thistle is safe or effective for people with these forms of cancer.
12.High cholesterol:
One animal study found that silymarin (an active compound in milk thistle) worked as effectively as the cholesterol-lowering drug probucol, with the additional benefit of substantially increasing HDL ("good") cholesterol. Further studies in people are needed.
13.Inflammation:
Milk Thistle is also a Demulcent, meaning that it soothes and moistens the mucus membranes, kidney and bladder irritations and inflammations in general. Being a demulcent, it also greatly softens and moistens the skin. Patients with skin problems ranging from acne to severe eczema have reported a clearing of skin impurities, healing of redness and inflammation, a dramatic softening and moistening of dry, cracking skin, and a noticeable glow and radiance to the skin quality.
14.The Bowels:
Milk Thistle is a gentle and mild laxative due to its ability to increase bile secretion and flow in the intestinal tract. This herb can have actions ranging from lubrication and softening of the stools to a mild laxative effect, to actually balancing individuals that alternate between diarrhea and constipation. (In patients with stools that alternate between constipation and diarrhea, Oriental Medicine would most likely suspect liver involvement.) This formula has been seen to improve bowel regularity and stool consistency in individuals with this type of alternating presentation. This is due to the astringent nature of the Dandelion Root combined with the softening and moistening nature of the Milk Thistle).
15.Gall Bladder Disease:
Milk thistle may prevent inflammation of the gall-bladder ducts and clear up jaundice.Because Milk Thistle is both a demulcent and it stimulates bile flow, it is a natural for treating a wide array of Gall Bladder diseases and Symptoms. Milk Thistle can calm down an inflamed Gall Bladder while at the same time clearing out any stagnation that might be present. When using Milk Thistle to combat Gall Bladder symptoms, it is important to verify that there are no Gall Stones present which would be too large for the gall bladder to pass. The only way that this can be known is to visit your local physician and get a clearance from them to proceed.
16.Cytoprotectant:
Studies of the use of milk thistle as a cytoprotectant in humans have been limited. In one study,49 of 200 workers exposed to toluene or xylene for five to 20 years developed persistent elevations in transaminase levels; 30 of these heterogeneous patients were treated with Legalon, whereas the others were not treated. In the Legalon group, transaminase activity decreased and platelet count increased when compared with the untreated group. Patients two to 21 years of age with acute lymphoblastic leukemia who are receiving hepatotoxic chemotherapy are being recruited for a second phase randomized pilot trial of silymarin.
17.Anticarcinogen:
Researchers are investigating the use of milk thistle's active ingredients for the prevention and treatment of cancer. Two additional animal studies on prostate cancer chemoprevention and treatment are ongoing, and a third phase trial in human prostate cancer patients with rising prostate-specific antigen also is under way.
18.Amanita phalloides poisoning:
The A. phalloides mushroom, called the "death cap," produces severe nausea, vomiting, and watery diarrhea within five to 12 hours of ingestion. This often causes hypovolemia and hypoglycemia. Silymarin inhibits the binding of the toxins in the mushroom to hepatocytes and interrupts the enterohepatic circulation of the toxins.36 Several journals have published case reports of silymarin treatment (intravenously and orally) for A. phalloides poisoning in humans, but the largest series37 followed only 18 patients. In every case, silymarin was used in combination with other agents, usually being added when standard treatment appeared to fail. The relative contribution of silymarin to these treatment regimens is unknown. The intravenous form of silymarin was used in these studies, but it is not available in the United States.
Milk thistle is the only known antidote for death cap mushroom (Amanita phalloides) poisoning. Ingesting this deadly mushroom can destroy the liver by shutting down protein production in liver cells. Milk thistle neutralizes these toxins and protects the liver. Milk thistle may also be helpful in acetaminophen overdosage.
19.Psoriasis:
Because the liver neutralizes certain toxins associated with psoriasis attacks, milk thistle is believed to help prevent psoriasis outbreaks by promoting proper liver function.
Several other dermatological uses for the herb are currently under investigation. The antioxidant properties of the herb may have a healing effect on skin wounds and burns. Milk thistle has also been proposed as a cosmetic agent to retain skin tone and quality. Further studies are needed to prove the efficacy of the herb for these applications.
20.Lactation Problems:
Milk thistle is frequently prescribed for breastfeeding mothers to promote increased breast milk secretion. Although the herb is considered safe for nursing mothers, it should be acquired from a reputable source and prescribed by an herbalist, naturopathic physician, or other healthcare professional familiar with its use.
21.Hiv Treatment:
Milk thistle is sometimes prescribed for HIV-positive patients to protect the liver from diseases such as hepatitis and from the hepatotoxic effects of other medications prescribed for HIV treatment.
Reference:
1.Silymarin.Milk Thistle and applications.
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