The pharmacological effects of ligustrum

Pharmacological effects

1. Hypolipidemic and anti-arteriosclerosis

Ligustrum lucidum 20g / only mixed with feedstuffs for feeding, rabbits with experimental hyperlipidemia can reduce serum cholesterol and triglyceride levels, and reduce aortic plaque and coronary atherosclerotic plaque formation . Ligustrum lucidum ingredients oleanolic acid 30mg/kg mixed with beverages fed rats, 0.4% oleanolic ester suspension 0.5ml fed to rabbits, hyperlipidemia rats, rabbits have lipid-lowering effects. Oleanolic acid 30, 60mg/kg added to the feed fed to Japanese quail for 8 weeks, significantly reduced serum total cholesterol, lipid peroxide, arterial wall total cholesterol content, reduce the incidence of atherosclerosis.

2 hypoglycemic

Oleanolic acid 50,100mg/kg subcutaneous injection, for 7 consecutive days, can reduce blood glucose in normal mice, have a preventive and therapeutic effect on alloxan-induced diabetes in mice, but also against adrenaline or glucose-induced mouse blood glucose Increased.

3. Anti-hepatic injury

Oleanolic acid at 30, 50, and 100 mg/kg subcutaneously inhibited the elevation of rat serum glutamate-pyruvic transaminase (SGPT) induced by carbon tetrachloride. Rats that had not been treated with carbon tetrachloride were treated with oleanolic acid. Subcutaneous injections of 50 and 100 mg/kg acid can also reduce SGPT. Oleanolic acid 70mg/kg subcutaneous injection, can reduce the liver damage caused by carbon tetrachloride, histological observation, liver cell vacuolar degeneration, osteoporosis, hepatocyte necrosis, lobular interstitial inflammation, are lighter than the corresponding control group . Oleanolic acid 2mg / subcutaneous injection, 6-9 weeks of continuous, high fat foods and carbon tetrachloride caused by liver cirrhosis have a preventive effect. Electron microscopy observations of carbon tetrachloride liver injury rats, oleanolic acid 20mg / subcutaneous injection only, can make liver cells mitochondrial swelling and endoplasmic reticulum vesicles are reduced.

4. Effect on the body's immune function

4.1 Effect on non-specific immunity

4.1.1 Increased number of peripheral white blood cells Ligustrum lucidum can significantly increase the number of peripheral white blood cells, and its effective component is oleanolic acid. Alcohol extracts can restore cyclopentamide (cy)-induced leukopenia in mice. Steamed Ligustrum 480mg/kg had no effect on leukocytes in normal mice, but it could correct the decline of leukocytes caused by prednisolone (25mg/kg, ip). 4.1.2 Effect on the phagocytic function of the reticuloendothelial system The macrophage viability was observed by the clearance rate of the foreign matter in the blood. It was found that 240mg/kgx5d of Ligustrum lucidum can significantly increase the clearance index of iv carbon particles in mice and enhance the activity of the reticuloendothelial system; Ligustrum lucidum 480mg/kg, the effect was not obvious. Ligustrum lucidum decoction 12.5g/kgx7d, no significant effect on the clearance index, and 25g/kgx7d significantly inhibited the phagocytic activity of the reticuloendothelial system.

4.2. Effect on Specific Immunity

4.2.1 Effect on cellular immune function Ligustrum lucidum can significantly increase T lymphocyte function. The 0.02ml aqueous extract of Ligustrum lucidum significantly enhanced the proliferation of lymphocytes induced by appropriate amount of PHA, COA and PWM in vitro, and also significantly enhanced the local graft-versus-host response (GUH) induced by xenogeneic (human) lymphocytes in rats. This may be due in part to the elimination or attenuation of the effects of suppressor T cells. Ligustrum lucidum polysaccharides (LLPS) enhanced the proliferation of mouse spleen lymphocytes stimulated by ConA: 3H-TdR incorporation (Cpm) 10mg/kg dose group (39308.1±6208) compared to the control group (17959±4508) Increase of about 120%, P <0.01, 50mg/kg administration group (2979 ± 3625) increased by about 70% compared to the control group, p <0.07. Ligustrum lucidum decoction promotes delayed hypersensitivity caused by SRBC. Shows that Ligustrum lucidum can enhance cellular immune function. Oleanolic acid 40mg, 3 times a day, taking 1-2 months, to improve the immune function of cancer patients, macrophage phagocytosis and blood lymphocyte rosette significantly increased by the skin bubble method.

Ligustrum lucidum induces M both in water extracts and alcohol extracts. The effect of IL-1, and the effect of the aqueous extract over the alcohol extract, reveals that the immune boosting effect of Ligustrum lucidum may be related to the induction of M. -IL-1 related. At the same time, Ligustrum lucidum promotes the activity of T cells by enhancing the activity of cell surface receptors. For the low immune function caused by high Ts activity, Ligustrum lucidum may be a good immunomodulatory drug.


Ligustrum lucidum fruit (13 photos)

4.2.2 Effect on humoral immune function Ligustrum lucidum has the function of enhancing humoral immunity. Ligustrum lucidum decoction for 7 consecutive days ig12.5 ~ 25g/kg, can make the mouse immune organs thymus, spleen weight increased; large doses can increase adult rat spleen weight. Steamed Ligustrum lucidum 240mg/kg, 480mg/kg × 7 days can significantly make C57BL mice spleen, thymus, abdominal lymph nodes, adrenal weight gain. The polysaccharide of Ligustrum lucidum was injected once a day. A total of 100 mg/kg on the 7th day increased the spleen weight of LACA mice by approximately 40% compared to the control group. 50 mg/kg increased the spleen weight of mice by approximately 30% compared with the control group. Ligustrum lucidum decoction can significantly increase the mouse serum hemolysin antibody activity, can also increase the normal mouse serum IgG content, and anti-Cy immunosuppressive effect; steamed Ligustrum lucidum can significantly inhibit the prednisolone immunosuppressive effect , also can increase the serum IgG in mice, and can increase the IgG content in prednisolone immunosuppressed mice, but can still clearly indicate that the mouse can record the activity of serum albumin antibody; the polysaccharide of Ligustrum lucidum is caused by the inhibition of Cy50mg/kgip. Inhibition of lymphocyte proliferation was inhibited in the tumor-bearing mice (S180), and the polysaccharides of Ligustrum lucidum significantly inhibited the immunosuppressive effects of Cy.

4.3 Inhibitory effects on allergies Ligustrum lucidum decoction 12.5, 25g/kgig mice for 7d; same dose 5dig rats, different doses of Ligustrum lucidum on mice or rats passive skin allergic reactions (PCA) showed obvious The inhibitory effect. Ligustrum lucidum decoction can reduce the percentage of rat mast cell degranulation, and increase the capillary permeability of rat skin induced by histamine; before administration of antigen, it can inhibit DNCB-induced contact dermatitis in mice; Subsidiary 25 g/kg administration after antigen challenge also significantly inhibited DNCB-induced contact epithelium in mice; reduced active and reverse passive Arthus responses in rats; Ligustrum lucidum 20g/kg significantly reduced total serum complement in guinea pigs. The results showed that Ligustrum lucidum had a significant inhibitory effect on type I, II and IV allergy.

5. Anti-inflammatory effect

A variety of experimental inflammation models confirmed Ligustrum lucidum 12.5g/kg, 25g/kg daily ig, for 5 consecutive days, p-xylene caused mouse ear swelling, acetic acid-induced increase in capillary permeability of the mouse's peritoneal cavity Adenosine, egg white, and formaldehyde-induced rat footpad swelling were all significantly inhibited; Ligustrum lucidum 20g/kg×3d ig significantly reduced the release of PGE from inflamed tissues of rats; Ligustrum lucidum 20g/kg×7 Japan can inhibit the proliferation of rat's cotton ball granulation tissue, accompanied by an increase in adrenal weight. Its anti-inflammatory mechanism may involve the following aspects: 1 activate the pituitary-adrenocortical system, promote the release of corticosteroids; 2 inhibit PGE synthesis or release. In addition, Ligustrum lucidum can reduce the serum complement activity of guinea pigs and increase the capillary permeability of rat skin induced by histamine, an inflammation mediator. Therefore, the anti-inflammatory mechanism of Ligustrum lucidum may also include the above-mentioned effects.

6. Anti-cancer, anti-mutation

Oleanolic acid has anti-tumor effect on mouse sarcoma-180. Ligustrum lucidum decoction 12.5, 25g/kg gavage, oleanolic acid 50, 100mg/kg subcutaneously, significantly inhibited the increase of micronucleus rate in mice bone marrow caused by cyclophosphamide and urethane.

7. The role of the endocrine system

Research shows that there are both estrogen-like and also androgen-like substances in Ligustrum lucidum. After radioimmunoassay, Ligustrum lucidum contains testosterone.

Glossy privet

428.31 pg/g, estradiol 139.02 pg/g. It is shown that Ligustrum lucidum has both testosterone-like and estradiol-like hormone analogues, that is, the same drug has bidirectional regulation. The traditional Chinese medicines such as Ligustrum lucidum that produced kidney yin produced estrogen-like effects on the vaginal mucous membrane of obese mice. The number of large follicles in the ovary of the rabbits in the medication group increased significantly, and estrogen increased.

8. Effect on hematopoietic system

Ligustrum lucidum promotes erythroid hematopoiesis. Using diffusion box plasma clot method, Ligustrum lucidum promotes CFU-E growth. CFU-E/5×l4 was 128.6±11.4 (8), CFU-E/femur was 62040±5450 (8), CFU-E in femur was significantly higher than that in NS group, but CFU-D was significantly reduced. After morphological analysis of mouse bone marrow cells after administration, the percentage of erythroid cells in Ligustrum lucidum was 47.3±2.99(6), which was higher than that of NS37.3±2.86(6) group, and the percentage of granular cells was 37.6±3.96(6), which was lower than that of NS group 46.6±6.26(6). The ratio of grain to red also changes accordingly.

9. Protection against chromosome damage caused by cyclophosphamide

Protection of chromosome damage caused by cyclophosphamide and urethane

Micronucleus test proved Ligustrum lucidum decoction pol2.5g/kg25.0g/(kg.d)×6, oleanolic acid ih50mg/kg, 100mg/(kg·d)×7 pairs cyclophosphamide ip50mg/ (kg · d) × 2, urethane 500 mg / (kg · d) × 4, ip caused by chromosomal damage in mice have a protective effect, can reduce the micronucleus rate.

10. Anti-HpD photochlorination

Ligustrum lucidum can counteract the photooxidation of HpD and its application in vivo can significantly reduce the photosensitivity of HpD to mouse skin. Ligustrum lucidum 60mg crude drug / ml, can significantly reduce the HpD5ug/ml combined with light 10min caused by the increase of erythrocyte MDA content, inhibition rate was 57.7%, significantly inhibited the activity of erythrocyte membrane acetylcholinesterase inhibition rate of 49.O At 120 mg/ml, the antagonistic rate was 53.3%, mice ipHpD 20 mg/kg, exposure to light 4 h, Ligustrum lucidum 20g crude drug/kg, ip 1 times, significantly reduced the photosensitivity of the ear. Ligustrum lucidum produced 3.5 times lower efficiency than 1O2 in the control group.

11. Other effects

Ligustrum lucidum also has the functions of cardiovascular system, such as dilating coronary vessels, dilating peripheral vessels, diuresis, cough, laxation, and antibacterial. Oleanolic acid has some cardiac and diuretic effects; mannitol has a slowing down effect; it also contains a large amount of glucose; these may be related to its strong effect.

Determination of content

Take about 1g of the product coarsely, accurately weighed, add ethanol 50ml, heat reflux for 30 minutes, let cool, filter, dregs plus ethanol above, and then repeat the reflux 2 times, the combined filtrate, evaporated to dryness, the residue plus absolute ethanol Dissolve in slight heat, transfer to a 10ml volumetric flask, add ethanol to the mark, shake, and use as a test solution. In addition, the reference substance of oleanolic acid was precisely weighed, and 0.5 mg of solution was added per 1 ml of absolute ethanol.

Glossy privet

As a control solution. According to the TLC (Appendix VI B) test, 2 μl of the test solution and 4 μl of the control solution and 8 μl of the control solution were accurately pipetted on the same silica gel G-laminate plate to cyclohexane-acetone-ethyl acetate ( 5:2:1) as a developing agent, unfold it, take it out, dry it, spray it with 10% ethanol solution of sulfuric acid, heat it at 100°C until the spot is clear, take it out, and cover it with a glass plate of the same size on a thin plate. Fix with tape, and scan according to thin layer chromatography (Appendix VI B Thin layer scan method), wavelength: λ<[S]>=530nm, λ<[R]>=700nm, measure the absorbance integral value of the sample The reference absorbance integrated value, calculated, that is, too. The product contains oleanolic acid (C30H48O3) not less than 0.60%.


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