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Pharmacological efficacy
Source:未知 Release Time:2011-12-25 23:10
Pharmacological efficacy Ursolic acid is present in a natural plant triterpenoids, have a calming, anti-inflammatory, antibacterial, anti-diabetic, anti-ulcer, lower blood sugar and other biological effects, ursolic acid also has significa
Pharmacological efficacy
Ursolic acid is present in a natural plant triterpenoids, have a calming, anti-inflammatory, antibacterial, anti-diabetic, anti-ulcer, lower blood sugar and other biological effects, ursolic acid also has significant antioxidant , which is widely used as a pharmaceutical and cosmetic raw materials. 1 liver, the role of anti-hepatitis clinical manifestations of ursolic acid significantly and rapidly reduce alanine aminotransferase, serum transaminases, jaundice subsided, appetite, anti-fibrosis and restore liver function, with quick, short duration, stable and characteristics. Indian scholars have found that ursolic Saraswat, etc. (5 ~ 20 mg · kg) of CC1-induced liver toxicity in rats has a protective effect. For pretreatment with ursolic acid significantly increased the survival rate of rat liver cells, and observed in experiments with anti-ursolic acid effect of cholestasis, bile flow and its contents are increased. Presumably by the mechanism of action of CC1 ursolic acid on the treatment of liver cell damage may be related to the mechanism of isomer oleanolic acid similarity, to protect and stabilize liver cell membranes and organelles of the biofilm system to changes in permeability and active transport function returned to normal intracellular ion and water movement and distribution has also come to recovery, regeneration have been restored, and promote the central lobular necrosis of liver cells to repair the area. "A class of drugs against hepatitis medicine ursolic acid and its preparation of research and development" project made significant progress to be included in the 2002 national "863" program, funded by national research funding 100 million, a major national research projects (2002AA2Z3217 .) 2 anti-tumor effect of ursolic acid is also a variety of carcinogens, tumor promoters are resistant to the effects, the researchers found that ursolic acid significantly inhibited HL-60 cell proliferation and induce apoptosis; make the mouse macrophage function was significantly improved, can inhibit tongue squamous cell carcinoma cell line TSCCa cell proliferation, half of TSCCa cell growth inhibitor is about 12.5 μmol · L-1, at 24h in the performance of a certain dose-effect relationship; in situ hybridization TSCCa ursolic acid on cells in vitro and in situ inhibition of nuclear transcription factor expression. . In vivo tests proved ursolic can significantly enhance the immune function. Shows anti-tumor effect of ursolic acid widely, ursolic acid toxicity is likely to become an effective new anti-cancer drugs. Ursolic acid on the growth of the various stages of tumor formation, prevention and inhibition, inhibition of tumor formation, growth and differentiation induced by cancer cells. Li J, etc. through experiments and clinical trials proved ursolic acid resistant mutations in DNA, inhibition of cancer initiation and ursolic acid to fight carcinogens such as benzopyrene, aflatoxin Bl-induced mutations. Peng test for early antibody (EBV-EA) activation to experimental skin cancer screening inhibitors of tumor promoters and found that ursolic acid on TPA-induced EBV-EA activation in Raji cells with retinoic acid has almost the same inhibitory effect, and to higher survival rate of Raji cells; the use of isotope labeled compounds 3H-PDB2 Buddha ester proved ursolic acid does not affect the TPA receptor binding, not by competition TPA sites, but effectively blocked the receptor carcinogens part of combination play. Guevara and other studies have shown that ursolic acid to make more mutagen-induced micronuclei chromatin 76% reduction in the number of red blood cells. Ohigachi other studies showed that ursolic acid on phorbol ester (TPA)-induced activation of EBA-EA in Raji cells was inhibited, the degree of retinoic acid is almost the same, Raji cells by retinoic acid treatment group compared with the survival rate is higher, the mechanism is effectively block the TPA and the receptor binding part of the role. Ng such that H Bear ursolic acid significantly inhibited the TPA on DMBA (DMBA)-induced tumor promotion in mouse skin cancer, the mechanism is TPA can induce epidermal ornithine decarboxylase (ODC) activity increased, ursolic acid can inhibit the above link, which led to polyamine depletion, growth was inhibited, the cells accumulate in the early stage, and the emergence of differentiation. 3 oxidation of ursolic acid is a strong antioxidant. Experiments show that ursolic acid inhibits the metabolism of arachidonic acid, 5 - lipoxygenase, cyclooxygenase activity, to prevent generation of prostaglandins and leukotrienes, which may inhibit the inflammatory response of ursolic acid, inhibit lipid peroxidation material reasons. Subbaramaiah and other studies have shown that ursolic acid inhibits human breast epithelial cells in the transcription of cyclooxygenase, and thus inhibition of prostaglandin production. Antioxidant effect of ursolic acid on the human body anti-aging, skin cream, tattoo removal has a positive effect. Japan 1983-2004 years of the ursolic acid in 29 patents, with 10 of ursolic acid on the skin beauty care applications, as cosmetics, ursolic acid stable, color and odor not change with time, and there good sense of touch, so skin care products in a wide range of applications. 4 anti-bacterial, anti-inflammatory and anti-virus Tapondjou so by acetic acid writhing test and hot plate test confirmed that ursolic acid and hydroxy-ursolic acid has a similar anti-inflammatory antimicrobial effect. Ursolic acid can inhibit the formyl-methionine, respectively, aminoacyl - leucyl - phenylalanine (fMLP) and arachidonic acid-induced superoxide generation. Ursolic acid and fMLP added to cell culture medium, ursolic acid dose-dependently inhibited the fMLP-induced 45 ku protein tyrosine phosphorylation. Ursolic acid also has to kill trypanosome activity, in the concentration of 2 g · L incubated for 2 h, Trypanosoma cruzi amastin activity was completely inhibited. Ursolic acid can lead to decreased cell viability. Peng proved ursolic acid-induced genomic DNA showed that the splitting mechanism of induction of cell death by apoptosis, ursolic acid inhibits human acute promyelocytic leukemia cells (HL-60) proliferation of HL-60 cells, half of the the amount of growth inhibitor (IC50) of 8.26 μm, and were able to induce apoptosis. 5 lipid-lowering, anti-atherosclerosis, lower blood sugar ursolic acid can reduce blood cholesterol in rabbits and rats (44%) and B-lipoprotein levels (50%), with lipid-lowering, anti-atherosclerosis the role. Ursolic acid can improve dyslipidemia induced liver and kidney, tinnitus, dry mouth, less sleep, irritability, limb numbness cold, it embolism, blood total effective rate was 95%. 6 pairs of inhibition of HIV human immunodeficiency virus (HIV) is the acquired immune deficiency syndrome (AIDS) of the pathogenic factor. Tian Ying proven through clinical trials such as ursolic acid on HIV-1 protease activity has a strong inhibitory effect, its 50% inhibitory concentration (IC50) of 8 μmol / L. HIV-1 protease is a homodimeric enzyme, ursolic acid may be through inhibition of HIV-1 protease dimerization to inhibit HIV-1 protease activity, thus inhibiting HIV protease play a role. Ursolic acid and malonic acid derivatives can inhibit HIV-1 protease (IC50) were 8 and 6μmol / L. 7 anti-diabetic, anti-ulcer 8 calm, stability and the central nervous system effects of ursolic acid significantly enhanced stability and cooling effect immune function 9
Ursolic acid is present in a natural plant triterpenoids, have a calming, anti-inflammatory, antibacterial, anti-diabetic, anti-ulcer, lower blood sugar and other biological effects, ursolic acid also has significant antioxidant , which is widely used as a pharmaceutical and cosmetic raw materials. 1 liver, the role of anti-hepatitis clinical manifestations of ursolic acid significantly and rapidly reduce alanine aminotransferase, serum transaminases, jaundice subsided, appetite, anti-fibrosis and restore liver function, with quick, short duration, stable and characteristics. Indian scholars have found that ursolic Saraswat, etc. (5 ~ 20 mg · kg) of CC1-induced liver toxicity in rats has a protective effect. For pretreatment with ursolic acid significantly increased the survival rate of rat liver cells, and observed in experiments with anti-ursolic acid effect of cholestasis, bile flow and its contents are increased. Presumably by the mechanism of action of CC1 ursolic acid on the treatment of liver cell damage may be related to the mechanism of isomer oleanolic acid similarity, to protect and stabilize liver cell membranes and organelles of the biofilm system to changes in permeability and active transport function returned to normal intracellular ion and water movement and distribution has also come to recovery, regeneration have been restored, and promote the central lobular necrosis of liver cells to repair the area. "A class of drugs against hepatitis medicine ursolic acid and its preparation of research and development" project made significant progress to be included in the 2002 national "863" program, funded by national research funding 100 million, a major national research projects (2002AA2Z3217 .) 2 anti-tumor effect of ursolic acid is also a variety of carcinogens, tumor promoters are resistant to the effects, the researchers found that ursolic acid significantly inhibited HL-60 cell proliferation and induce apoptosis; make the mouse macrophage function was significantly improved, can inhibit tongue squamous cell carcinoma cell line TSCCa cell proliferation, half of TSCCa cell growth inhibitor is about 12.5 μmol · L-1, at 24h in the performance of a certain dose-effect relationship; in situ hybridization TSCCa ursolic acid on cells in vitro and in situ inhibition of nuclear transcription factor expression. . In vivo tests proved ursolic can significantly enhance the immune function. Shows anti-tumor effect of ursolic acid widely, ursolic acid toxicity is likely to become an effective new anti-cancer drugs. Ursolic acid on the growth of the various stages of tumor formation, prevention and inhibition, inhibition of tumor formation, growth and differentiation induced by cancer cells. Li J, etc. through experiments and clinical trials proved ursolic acid resistant mutations in DNA, inhibition of cancer initiation and ursolic acid to fight carcinogens such as benzopyrene, aflatoxin Bl-induced mutations. Peng test for early antibody (EBV-EA) activation to experimental skin cancer screening inhibitors of tumor promoters and found that ursolic acid on TPA-induced EBV-EA activation in Raji cells with retinoic acid has almost the same inhibitory effect, and to higher survival rate of Raji cells; the use of isotope labeled compounds 3H-PDB2 Buddha ester proved ursolic acid does not affect the TPA receptor binding, not by competition TPA sites, but effectively blocked the receptor carcinogens part of combination play. Guevara and other studies have shown that ursolic acid to make more mutagen-induced micronuclei chromatin 76% reduction in the number of red blood cells. Ohigachi other studies showed that ursolic acid on phorbol ester (TPA)-induced activation of EBA-EA in Raji cells was inhibited, the degree of retinoic acid is almost the same, Raji cells by retinoic acid treatment group compared with the survival rate is higher, the mechanism is effectively block the TPA and the receptor binding part of the role. Ng such that H Bear ursolic acid significantly inhibited the TPA on DMBA (DMBA)-induced tumor promotion in mouse skin cancer, the mechanism is TPA can induce epidermal ornithine decarboxylase (ODC) activity increased, ursolic acid can inhibit the above link, which led to polyamine depletion, growth was inhibited, the cells accumulate in the early stage, and the emergence of differentiation. 3 oxidation of ursolic acid is a strong antioxidant. Experiments show that ursolic acid inhibits the metabolism of arachidonic acid, 5 - lipoxygenase, cyclooxygenase activity, to prevent generation of prostaglandins and leukotrienes, which may inhibit the inflammatory response of ursolic acid, inhibit lipid peroxidation material reasons. Subbaramaiah and other studies have shown that ursolic acid inhibits human breast epithelial cells in the transcription of cyclooxygenase, and thus inhibition of prostaglandin production. Antioxidant effect of ursolic acid on the human body anti-aging, skin cream, tattoo removal has a positive effect. Japan 1983-2004 years of the ursolic acid in 29 patents, with 10 of ursolic acid on the skin beauty care applications, as cosmetics, ursolic acid stable, color and odor not change with time, and there good sense of touch, so skin care products in a wide range of applications. 4 anti-bacterial, anti-inflammatory and anti-virus Tapondjou so by acetic acid writhing test and hot plate test confirmed that ursolic acid and hydroxy-ursolic acid has a similar anti-inflammatory antimicrobial effect. Ursolic acid can inhibit the formyl-methionine, respectively, aminoacyl - leucyl - phenylalanine (fMLP) and arachidonic acid-induced superoxide generation. Ursolic acid and fMLP added to cell culture medium, ursolic acid dose-dependently inhibited the fMLP-induced 45 ku protein tyrosine phosphorylation. Ursolic acid also has to kill trypanosome activity, in the concentration of 2 g · L incubated for 2 h, Trypanosoma cruzi amastin activity was completely inhibited. Ursolic acid can lead to decreased cell viability. Peng proved ursolic acid-induced genomic DNA showed that the splitting mechanism of induction of cell death by apoptosis, ursolic acid inhibits human acute promyelocytic leukemia cells (HL-60) proliferation of HL-60 cells, half of the the amount of growth inhibitor (IC50) of 8.26 μm, and were able to induce apoptosis. 5 lipid-lowering, anti-atherosclerosis, lower blood sugar ursolic acid can reduce blood cholesterol in rabbits and rats (44%) and B-lipoprotein levels (50%), with lipid-lowering, anti-atherosclerosis the role. Ursolic acid can improve dyslipidemia induced liver and kidney, tinnitus, dry mouth, less sleep, irritability, limb numbness cold, it embolism, blood total effective rate was 95%. 6 pairs of inhibition of HIV human immunodeficiency virus (HIV) is the acquired immune deficiency syndrome (AIDS) of the pathogenic factor. Tian Ying proven through clinical trials such as ursolic acid on HIV-1 protease activity has a strong inhibitory effect, its 50% inhibitory concentration (IC50) of 8 μmol / L. HIV-1 protease is a homodimeric enzyme, ursolic acid may be through inhibition of HIV-1 protease dimerization to inhibit HIV-1 protease activity, thus inhibiting HIV protease play a role. Ursolic acid and malonic acid derivatives can inhibit HIV-1 protease (IC50) were 8 and 6μmol / L. 7 anti-diabetic, anti-ulcer 8 calm, stability and the central nervous system effects of ursolic acid significantly enhanced stability and cooling effect immune function 9
