Ursolic acid is a triterpenoid compound found in natural plants. It has various biological effects such as sedative, anti-inflammatory, antibacterial, anti-diabetic, anti-ulcer, and lowering blood sugar. Ursolic acid also has obvious antioxidant functions. , and therefore are widely used as pharmaceutical and
Cosmetic Raw Materials.
The Function of Ursolic Acid 1 Hepatoprotective and anti-hepatitis effects
The clinical manifestations of ursolic acid are that it can significantly and rapidly reduce alanine aminotransferase and serum aminotransferase, subside jaundice, increase appetite, resist fibrosis and restore liver function. It has the characteristics of quick effect, short course of treatment and stable effect.
Indian scholar Saraswat et al. found that ursolic acid (5-20 mg·kg) has a protective effect on liver toxicity in rats caused by CC1. Pretreatment with ursolic acid can significantly increase the survival rate of rat liver cells. In experiments, it was observed that ursolic acid has an anti-cholestasis effect, and bile flow and its contents are increased. Based on the mechanism of action of CC1, it is speculated that the therapeutic mechanism of ursolic acid on damaged liver cells may be similar to that of its isomer oleanolic acid, which is to protect and stabilize the biofilm system of liver cell membranes and organelles, making them permeable and active. The transport function returns to normal, the movement and distribution of ions and water inside and outside the cells are also restored, and the regeneration ability is restored one after another, promoting the repair of necrotic hepatocytes in the central area of the liver lobule.
2. Anti-tumor effect
Ursolic acid also has resistance to a variety of carcinogens and carcinogens. Studies have found that ursolic acid can significantly inhibit the proliferation of HL-60 cells and induce their apoptosis; it can significantly improve the phagocytic function of macrophages in mice. It can inhibit the proliferation of human tongue squamous cell carcinoma cell line TSCCa. The inhibitory dose of half of the growth of TSCCa cells is about 12.5 μmol·L-1, showing a certain dose-effect relationship within 24 hours; in situ hybridization shows that ursolic acid has an inhibitory effect on TSCCa cells. The cell inhibitory effect is related to the inhibition of in situ expression of nuclear transcription factors. . In vivo experiments have proven that ursolic acid can significantly enhance the body's immune function. This shows that ursolic acid has extensive anti-tumor effects, and ursolic acid is very likely to become a low-toxic and effective new anti-cancer drug.
Ursolic acid has preventive and inhibitory effects on various stages of tumor formation and growth, inhibits tumor formation and growth, and induces cancer cell differentiation. Li J et al. have proven through experiments and clinical trials that ursolic acid can resist DNA mutations and inhibit the initiation of cancer. Moreover, ursolic acid can resist gene mutations induced by carcinogens such as benzopyrene and aflatoxin Bl. Wang Peng's experiment used an early antibody (EBV-EA) activation test to screen inhibitors of skin cancer carcinogens and found that ursolic acid has almost the same inhibitory effect as retinoic acid on TPA-induced EBV-EA activation in Raji cells, and makes The survival rate of Raji cells is higher; the isotope-labeled phenanthrene compound 3H-PDB2 is used to prove that ursolic acid does not affect the binding of TPA to the receptor, not by competing for the TPA site, but effectively blocking the binding of carcinogens to the receptor. The latter link comes into play. Studies by Guevara et al. have shown that ursolic acid can reduce the number of polychromatin-induced micronucleated red blood cells by 76%. Ohigachi et al.'s research results show that ursolic acid has an inhibitory effect on EBA-EA activation in Raji cells induced by phorbol ester (TPA), which is almost the same as retinoic acid. The survival rate of Raji cells is higher than that of the retinoic acid-treated group. The mechanism is Effectively blocks the link between TPA and receptors. H. Ursolic Acid and others found that ursolic acid can significantly inhibit the cancer-promoting effect of TPA on dimethylbenzanthracene (DMBA)-induced skin cancer in mice. The mechanism is that TPA can induce epidermal ornithine decarboxylase (ODC). With enhanced activity, ursolic acid can inhibit the above-mentioned links, thereby causing polyamine depletion, inhibiting growth, causing cells to accumulate at an early stage and differentiate.
3 antioxidant
Ursolic acid is a powerful antioxidant. Experiments have shown that ursolic acid can inhibit the activities of 5-lipoxygenase and cyclooxygenase during the metabolism of arachidonic acid, and prevent the production of prostaglandins and leukotrienes. This may be because ursolic acid inhibits inflammatory reactions and inhibits lipid metabolism. cause of oxides. Subbaramaiah et al. have shown that ursolic acid can inhibit the transcription of cyclooxygenase in human mammary epithelial cells, thereby inhibiting prostaglandin production.
The antioxidant effect of ursolic acid has a positive effect on the human body's anti-aging, skin freckle removal, and pigment removal. Among the 29 Japanese patents on ursolic acid from 1983 to 2004, 10 were about the application of ursolic acid in skin beauty and health care. As a cosmetic, ursolic acid has stable properties, the color and smell do not change over time, and it has It has a good touch feeling, so it is widely used in beauty and skin care products.
4 Antibacterial, anti-inflammatory and antiviral
Tapondjou et al. confirmed through acetic acid twisting test and hot plate test that ursolic acid and hydroxyursolic acid have similar anti-inflammatory and antibacterial effects. Ursolic acid can inhibit the production of superoxide induced by formylmethionyl-leucyl-phenylalanine (fMLP) and arachidonic acid respectively. When ursolic acid and fMLP were added to the cell culture medium, ursolic acid inhibited the tyrosine phosphorylation of 45 ku protein induced by fMLP in a dose-dependent manner. Ursolic acid also has trypanocidal activity. After incubation for 2 hours at a concentration of 2 g·L, the activity of Trypanosoma cruzi flagellates was completely inhibited.
Ursolic acid can cause a decrease in cell viability. Wang Peng proved that ursolic acid induces genomic DNA cleavage, indicating that its mechanism of inducing cell death is through apoptosis. Ursolic acid can inhibit the proliferation of human acute promyelocytic leukemia cells (HL-60), killing half of HL-60 cells. The growth inhibitory dose (IC50) is 8.26 μm and can induce concurrent apoptosis.
5. Effects of lowering blood lipids, anti-atherosclerosis, and lowering blood sugar
Ursolic acid can reduce blood cholesterol (44%) and B-lipoprotein levels (50%) in rabbits and rats, and has blood lipid-lowering and anti-atherosclerotic effects. Ursolic acid can improve symptoms such as liver and kidney yin deficiency, tinnitus, dry mouth, insomnia, irritability, numbness in limbs, cold sensitivity, and constipation caused by dyslipidemia. The total effective rate of blood lipid efficacy is 95%.
6. Inhibitory effect on HIV
Human immunodeficiency virus (HIV) is the causative agent of acquired immunodeficiency syndrome (AIDS). Tian Ying et al. demonstrated through clinical trials that ursolic acid has a strong inhibitory effect on HIV-1 protease activity, and its 50% inhibitory concentration (IC50) is 8 μmol/L. HIV-1 protease is a homodimer enzyme. Ursolic acid may inhibit the activity of HIV-1 protease by inhibiting the dimerization of HIV-1 protease, thereby inhibiting the function of HIV protease.
Ursolic acid and its malonic acid derivatives can inhibit HIV-1 protease with (IC50) of 8 and 6 μmol/L respectively.
7. Anti-diabetic, anti-ulcer
8. Sedative and stabilizing effects
Ursolic acid has obvious stabilizing and cooling effects on the central nervous system
9. Enhance immune function
Contact Now
