Milk Thistle is the dry mature fruit of the genus Silybum marianum (L.) Gaertn. The monomer components extracted from milk thistle, such as silymarin and silybin have a wide range of pharmacological activities, such as anti-oxidation, liver protection, anti-inflammatory, hypolipidemic, anti-cancer and neuroprotective effects.
1. Study on chemical constituents of Milk Thistle
The milk thistle contains a large amount of flavonoids, represented by silymarin. Silymarin is mainly a kind of flavonoids with C9 substituents, ie condensation with dihydroflavonol and phenylpropanoid derivatives. The flavonoid lignans, the current research shows that silymarin is mainly composed of flavonoid lignans and unknown oxidized polyphenols such as silibinin, silibinin, silibinin and silibinin. composition. . In addition, flavonoid lignan compounds such as silibinin, silibinin, Silygermin, Neosilygermin A, and Neosilygermin B were isolated from silymarin. Also contained in the fruit of milk thistle is 5,7-dihydroxychromone, polyhydroxychroman-4-one, apigenin, ginseng flavin, eriomycin, kaempferol, naringenin Other flavonoids such as quercetin and taxol.
Only five triterpenoids are currently obtained from the fruit of the milk thistle. Ejaz Ahmed is equal to three three separated from the milk thistle in 2006.
The terpenoids are Mariane, Marianoside A, and Marianoside B, respectively. In 2007, the research team isolated two new triterpenoids, Silymin A and Silymin B, from the milk thistle.
1.3 Fatty acid compounds
Milk thistle contains a lot of fatty acids, its fatty acid content can reach 26% ~ 31%, including linoleic acid 50% ~ 54%, oleic acid 23% ~ 29%, palmitic acid 7% ~ 8%.
2 Study on pharmacological activity of milk thistle
The study found that silymarin has antioxidant, hepatoprotective, anti-inflammatory, hypolipidemic, anti-cancer and neuroprotective effects. Its main active role is the synthesis of silybin and silymarin (including silybin and silymarin). Ning, Shuifeijingting and other compounds).
2.1 Antioxidant effect
The activity of silymarin antioxidation may be related to its ability to inhibit the production of xanthine oxidase and cytochrome P-450 enzymes that produce oxygen free radicals. In addition, silymarin can also react with hydroxyl radicals, and silymarin can inhibit the release of O2- by human neutrophils by inhibiting the activity of protein kinase c and NADPH oxidase. However, silymarin did not remove the role of O2-formation. These properties of silymarin can be used to protect the peroxidation of membrane lipids and to inhibit cell membrane degradation.
2.2 Liver protection
The protective effect of silymarin on acute or chronic hepatitis caused by drugs has been confirmed in animal models such as rats and mice. Intraperitoneal or intravenous injection of silymarin can protect against liver damage caused by various hepatotoxic substances, such as carbon tetrachloride, ethanol, galactosamine, alcohol, and the like.
● 2.2.1 Liver damage caused by carbon tetrachloride Carbon tetrachloride causes hepatic lobular necrosis and fatty metamorphosis by inducing peroxidation of unsaturated fatty acids on membrane phospholipids. Rats that were modeled by carbon tetrachloride were 2 times longer than those of the blank rats. This indicates that silymarin can inhibit the peroxidation caused by carbon tetrachloride, protect its inhibitory activity against hepatocyte enzymes and enhance the activity of enzymes in serum.
● 2.2.2 Liver damage caused by galactosamine It has been found that silymarin can reduce the increase of enzyme levels in rat serum caused by medium dose; it can also reduce histology and ultrastructure in cells and subcellular structures. damage.
● 2.2.4 Liver damage caused by thioacetamide After injection of high thioacetamide in rats, hepatic cell degeneration is caused, which is similar to human cirrhosis, accompanied by nodule formation. And necrosis of liver parenchymal cells. After injection of silymarin, the survival rate of the animal can be improved, and the activity of the enzyme in the serum can be enhanced.
● 2.2.5 Liver damage caused by alcohol When a large amount of alcohol is given to experimental animals, the active oxygen such as peroxide, hydroxyl radical and hydrogen peroxide can be aggregated, resulting in oxidation of protein and DNA, resulting in lipid peroxidation. reaction. Treatment with silymarin can significantly improve liver damage status after administration of large doses of alcohol to the animal causing liver damage. The above studies have shown that silymarin can not only treat liver disorders, but also prevent lipid peroxidation caused by various toxic substances.
2.3 Hypolipidemic effect
Silymarin has the effect of regulating and promoting lipoprotein metabolism. Silymarin is mainly used for hyperlipidemic rats. For normal rats, administration of silybin does not affect serum cholesterol levels. The hypolipidemic effect of silymarin and its polyphenols is mainly reflected in the reduction of cholesterol levels in the liver and plasma of hyperlipidemic rats.
2.4 Anticancer activity
In recent years, studies have found that silymarin has good inhibitory effects on several types of cancer, such as skin cancer, breast cancer, cervical cancer, prostate cancer and kidney cancer.
● 2.4.1 Skin cancer Silibinin has a certain inhibitory effect on actinic keratosis, epidermoid tumor (A431 cell line), basal cells and squamous cell carcinoma.
● 2.4.2 Breast cancer There are few reports on the efficacy of silybin preparations for breast cancer. Some studies have found that silymarin and silybin inhibit the DNA synthesis and cell proliferation of breast cancer cells in a time-dependent manner.
● 2.4.3 Lung cancer Silibinin inhibits the growth of (SCLC) SHP-77 and (NSCLC) A-549 cells and accelerates the apoptosis of these cells. Silibinin is achieved by inhibiting MMPs-mediated cell invasion and the urokinase plasminogen activator of the PI3K-Akt and MAPK signaling pathways.
● 2.4.4 Kidney cancer Silibinin has the effect of inhibiting the proliferation of renal cancer cells both in vivo and in vitro. Silibinin inhibits DNA synthesis in SN12K1RCC cells at lower concentrations (2-40 μM), and accelerates apoptosis at higher concentrations (80-200 μM).
● 2.4.5 Bladder Cancer Silibinin has a very significant therapeutic effect on bladder cancer. In the study of human bladder transitional cell papilloma RT-4, it was found that silibinin can reduce protein and mRNA levels in survivin. Silibinin also accelerates the rate of apoptosis in RT4 cells.
● 2.4.6 Prostate cancer studies have found that the effect of silybin on PC-3 cells is by overexpressing an insulin-like growth factor regulatory protein, IGFBP-3, which acts on PC-3 cells by inhibiting IGF-I. effect. Subsequent studies have found that the effect of silybin on PC-3 model mice is mainly to inhibit tumor growth. Both silymarin and silybin inhibit the secretion of androgen-stimulated cells and the secretion of PSA cells, human glandular kallikrein, immunophilin, FKBP51 and the like.
2.5 Anti-inflammatory effect
The anti-inflammatory action of silymarin is achieved by stabilizing mast cells, inhibiting neutrophil migration, inhibiting Kuppefer cells and inhibiting leukotrienes, inhibiting 5-lipoxygenase, and inhibiting prostaglandin production.
2.6 Other effects
In recent years, scholars of various countries have paid more and more attention to the treatment of silymarin for neurodegeneration and neurotoxicity. Studies have found that the neuroprotective effect of silymarin is achieved by combating the neurotoxicity of the midbrain-mixed neuronal cells induced by lipopolysaccharide. Scholars have found that dehydroglucosinolate has antimalarial activity in vitro, and silymarin derivatives have been made into related drugs to delay the spread of Plasmodium falciparum worldwide. In addition, scholars have found that silymarin has a significant anti-aging effect.
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